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EMDEX Limited Chris 5ive Consulting Inc.
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ii | EMDEX 2014/2015 EMDEX 2014/2015 | iii
Y o utn!ers EMDEX Vols 1 & 2

a n k
Thur EMDEX Par
Based on the WHO Model Formulary & Nigeria’s Essential Drug List
The Complete Drug Formulary for Nigeria’s Healthcare Professionals
to all o Edited by:
National Reach Entire Healthcare Coverage Great Value
Dear EMDEX User,

Chris C. Obi, B.Pharm., M.Sc., CDE
The following companies provide ongoing support for the research, writing and production of EMDEX every year. Join us in saying Certificate in Paediatric Patient Care
thank you to them. Certified Injection & Immunization Pharmacist
Please prescribe, stock and/or recommend our EMDEX Partner Brands daily. Thank you.
Diabetes Educator Graduate Certificate (Michener Institute, Toronto)
- EMDEX Team.
ADAPT Certificate in Patient Care Skills (University of Waterloo)
AFRAB chem DORTEMAG MANOLA PLACEWARE
Certificate in Oncology for Pharmacists (Part I, University of Toronto)
AGARY DRUGFILED MARK QUADRANT Member, DIA (Drug Information Association, USA)
ALPHA PHARMACY E-GLOBA MAY & BAKER RAINBOW TROUT
Consultant Editors & Contributors
EMDEX
ALRANGE Limited ELBE ME CURE RAPHA
AL-TINEZ EMBASSY MEDHEIGHT RANBAXY The publishers gratefully acknowledge the expert reviews & contributions by:
ARTEPHARM EMZOR MEGA LIFESCIENCES RAJRAB
ASPEN EVANS MICHELLE ROHI Joshua F. Eniojukan, PhD, FPCPharm.
ATSI FIDSON MICRONOVA SALEM GATE Professor of Clinical Pharmacy and Pharmacy Practice,
AWARD GLOBAL FOUNDATION MIRAFLASH SANOFI PASTEUR
Faculty of Pharmacy, Niger Delta University,
BARATA GAUZE MOPSON SEAGREEN
Wilberforce Island, Bayelsa State
BAKANGIZO GETZ NALIS SHREAZER
BCN GENEITH NANCIL SIEBEL
BETA Drugs GLENMARK NASDMU Limited SOCIETY FOR FAMILY
Dr. Olubiyi F Adesina, MB.ChB (Ife), FMCP (Nig), MNSEM
B.G. Pharma GLOBAL Healthcare NECTAR HEALTHCARE HEALTH (SFH) Consultant Endocrinologist/Diabetologist,
BIO-FACTORS GLOBAL ORGANICS NEMEL SOFAK Federal Medical Centre, Abeokuta, Ogun State
BIOFEM GOLDMOORE Int’l N.G.C. STANDARD GENERICS
BOLAR GREENLIFE NEW HEALTHWAY STERLING Mrs. L.O. Ladipo-Clegg, R.N., RPN. R.M.,B.Sc.,M.Ed.,PGDHM.,
BOND GSK NEW HEIGHT SUPERIOR
MBA Finance, MNIM
CANOPUS West Africa HELP Pharma NEXT GENERATION SYLKEN
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Psychiatric/Mental Health Nursing,
CEENEK HUGO NOMEDI TETA Federal Neuro-Psychiatric Hospital, Yaba, Lagos State
C.G BIOSTADT ICHIE BENSON NOVARTIS TIOPHARM
CHI Pharma JAWA OCULUS TISCO Mrs. Ifeoma C. Orabueze, B.Pharm., M.Sc., PhD (in view)
COPAC JB Pharma ONIFAM VATICAN BELLS Department of Pharmacognosy,
CRYSTAL FOODS & DRUGS JOPAN PACMAI VINCO Faculty of Pharmacy, University of Lagos, Lagos State, Nigeria
DABAK JUHEL PEMASON VISKO
DANA KAKAKI CHEMIST PHARMABASE VITABIOTICS
DANBOL Technologies KAYHELT PHARMACY PLUS VITA HEALTH
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DIGITAL Healthcare LIFEBACK PHILIPS ZOLON
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DIVINE Fertility Drugs L’PACEMAKER PINNACLE ZOOMOTA
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TOGETHER, WE WILL CONTINUE TO IMPROVE HEALTHCARE IN NIGERIA. Web address: www.EmdexOnline.com
See EMDEX Paediatric Drug Guide for details on medication use in children & adolescents
EMDEX 2014/2015 | Get your EMDEX Vol. 3 (Drug Comparisons & Therapeutic Details) at no extra charge Register at www.EmdexOnline.com for free access to EMDEX Online
iv | EMDEX 2014/2015 EMDEX 2014/2015 | v
Contents
EMDEX Vols 1 & 2
Based on the WHO Model Formulary & Nigeria’s Essential Drug List Nigeria’s National Drug Policy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
The Complete Drug Formulary for Nigeria’s Healthcare Professionals Essential drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Drug revolving fund (DRF). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Editor/CEO Rational use of drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18
General Advice to Prescribers. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 20
Chris C. Obi, B.Pharm., M.Sc., CDE
Rational approach to therapeutics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 20
Certificate in Paediatric Patient Care
Variation in dose response. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 21
Certified Injection & Immunization Pharmacist
Diabetes Educator Graduate Certificate (Michener Institute, Toronto) Adherence (compliance) with drug treatment. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 22
ADAPT Certificate in Patient Care Skills (University of Waterloo) Adverse effects and interactions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 24
Certificate in Oncology for Pharmacists (Part I, University of Toronto) Prescription writing . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 26
Member, DIA (Drug Information Association, USA) 1. C
entral nervous system (CNS) drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 28
EMDEX
1.1 Drugs used in anxiety and sleep disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 29
Head of Office Marketing Coordinator
1.2 Drugs used in psychotic disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 32
Chinelo Ikechukwu, HND Nefishetu Apoh, OND
(0802-306-0065) (0805-366-0525) 1.3 Antidotes to antipsychotic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 40
1.4 Drugs used in mood disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 41
Sales/Marketing Production Team
Chijioke Nzewi (0802-448-6816) Chris Uzoh 1.4.1 Drugs used in depressive disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 41
Fatimah Anyebe (0802-717-5953) Jacchin Odoemena 1.4.2 Drugs used in bipolar disorders . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 48
Victor Ekechi (0803-350-1827 Monday Udu 1.5 Obsessive-compulsive disorders and panic attacks. . . . . . . . . . . . . . . . . . . . . . . . . . 51
Assistant Editor (Trainee) Drug Information Representative 1.6 Antiparkinson drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51

Chibueze Okonkwo, B.Pharm, MPSN Gerald W. Ugodi, B.Pharm, MPSN 1.6.1 Drugs used in parkinsonism. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51
1.6.2 Drugs used in essential tremor and related disorders. . . . . . . . . . . . . . . . . . . . . . 55
1.7 Anticonvulsants (Antiepileptics). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 55
Important Information: 1.8 Analgesics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 66
The World Health Organization (WHO) has generously permitted us to
1.8.1 Non-opioid analgesics and antipyretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 67
adopt WHO Model Formulary in the preparation of EMDEX. This permission
1.8.2 Opioid analgesics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 75
does not, however, imply WHO endorsement nor recommendation of the
products of pharmaceutical companies which are featured in this publication. 1.9 Drugs used in substance dependence programes. . . . . . . . . . . . . . . . . . . . . . . . . . . 81
The Editor and the Publishers have taken time to ensure the accuracy and currency 1.10 Drugs used in migraine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 81
of the information contained in this book as at the time of going to Press. We do not 1.10.1 Acute migraine attack . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 82
however warrant the completeness and correctness of the information contained 1.10.1.1 Analgesics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 82
in the book and shall not be liable for any damages resulting from its use.
1.10.1.2 Ergot alkaloids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83
For all inquiries, please contact Editor at: editor@EmdexOnline.com
1.10.1.3 Antiemetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83
1.10.2 Migraine prophylaxis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83
Print-Production assisted by Ken U. Obi | Cover Design & Graphics by Dennis Ugwu 2. D
rugs for musculoskeletal and joint diseases. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 85
2.1 Antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 86
2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs). . . . . . . . . . . . . . . . . . . . . . . . . . 86
Published since 1991 by EMDEX Limited (formerly Lindoz Products Ltd), Lagos,
Nigeria, in association with Chris 5ive Consulting Inc., Mississauga, ON Canada. 2.1.2 Disease-modifying antirheumatic drugs (DMARDs). . . . . . . . . . . . . . . . . . . . . . . 101
vi | EMDEX 2014/2015 EMDEX 2014/2015 | vii
2.1.3 Other antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 104 4.8 Anti-inflammatory drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 171
2.2 Drugs used in gout . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106 4.9 Miscellaneous. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 173
2.2.1 Acute gout. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106 5. C
ardiovascular system drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 174
2.2.2 Chronic gout. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106 5.1 Drugs used in heart failure. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 175
2.3 Skeletal muscle relaxants (antispasmodics) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 107 5.2 Diuretics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 179
2.4 Muscle relaxants (peripherally acting) and cholinesterase inhibitors . . . . . . . . 109 5.2.1 Low-ceiling diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 179
2.4.1 Muscle relaxants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109 5.2.2 High-ceiling (or Loop) diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 182
2.4.2 Cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109 5.2.3 Potassium-sparing diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 185
2.5 Drugs affecting bone structure and mineralization. . . . . . . . . . . . . . . . . . . . . . . . . 111 5.2.4 Osmotic diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188
2.6 Topical antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 112 5.3 Antihypertensive drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188
2.7 Enzymes and miscellaneous anti-inflammatory agents. . . . . . . . . . . . . . . . . . . . . 113 5.3.1 Beta–adrenoceptor blocking drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 190
3. D
rugs used in anaesthesia . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 116 5.3.2 Vasodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 195
3.1 General anaesthetics and oxygen . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 117 5.3.3 Alpha-adrenoceptor blocking drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 196
3.1.1 Intravenous agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 117 5.3.4 Centrally acting antihypertensive drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 198
EMDEX
3.1.2 Volatile inhalational agents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 119 5.3.5 Angiotensin–converting enzyme (ACE) inhibitors. . . . . . . . . . . . . . . . . . . . . . . . 200
3.1.3 Inhalational gases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 121 5.3.6 Angiotensin receptor blockers (ARBs). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 206
3.2 Preoperative medication and sedation for short-term procedures. . . . . . . . . . . 121 5.3.7 Calcium–channel blockers . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 212
3.3 Muscle relaxants and cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . 124 5.3.8 Diuretics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 221
3.3.1 Muscle relaxants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 124 5.4 Antiarrhythmic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 222
3.3.2 Cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 127 5.5 Antianginal drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 227
3.4 Local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 128 5.6 Antithrombotic drugs and myocardial infarction. . . . . . . . . . . . . . . . . . . . . . . . . . . 230
3.5 Analgesics and opioid antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 130 5.7 Lipid-regulating drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 234
3.6 Blood substitutes and solutions for correcting fluid imbalance. . . . . . . . . . . . . . 131 5.8 Vasoprotectives . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 239
3.7 Others . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 131 5.9 Peripheral vasodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 240
4. D
rugs used in gastrointestinal diseases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 133 6. D
rugs affecting blood and nutrition. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .241
4.1 Antacids and other antiulcer drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 134 6.1 Anti-anaemia drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 242
4.1.1 Antacids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .136 6.1.1 Drugs used in iron-deficiency and megaloblastic anaemias. . . . . . . . . . . . . . . 243
4.1.2 Ulcer healing drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 141 6.1.2 Drugs used in neutropenia. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 252
4.2 Antispasmodic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 153 6.1.3 Drugs used in hypoplastic, haemolytic, and renal anaemias. . . . . . . . . . . . . . . 252
4.3 Other smooth muscle relaxants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 155 6.1.4 Drugs used in sickle cell disease. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 253
4.4 Drugs used in diarrhoea . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 156 6.2 Drugs affecting coagulation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 253
4.4.1 Oral rehydration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 156 6.2.1 Anticoagulants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 254
4.4.2 Medicines for diarrhoea in children. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 157 6.2.2 Reversal of anticoagulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257
4.4.3 Antimotility drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 158 6.3 Antifibrinolytics and haemostatics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 258
4.4.4 Adsorbents and bulk-forming drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 161 6.4 Blood products and plasma substitutes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
4.4.5 Antidiarrheal microorganisms. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 162 6.4.1 Plasma substitutes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
4.5 Laxatives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 163 6.4.2 Plasma fractions for specific use. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
4.6 Antiemetic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 165 6.5 Vitamins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 263
4.7 Antihaemorrhoidal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 170 6.6 Minerals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 274
viii | EMDEX 2014/2015 EMDEX 2014/2015 | ix
6.7 Appetite Stimulants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277 9.1.3 Antileprosy drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 407
6.8 Solutions for correcting water, electrolyte and acid-base disturbances. . . . . . 277 9.1.4 Antituberculosis drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 410
6.8.1 Oral electrolyte solutions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277 9.2 Systemic antifungal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .418
6.8.1.2 Oral potassium . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277 9.3 Antiprotozoal drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
6.8.2 Parenteral electrolyte solutions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 278 9.3.1 Antimalarial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
6.8.3 Water . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 282 9.3.1.1 Artemisinin-based combination therapies (ACTs). . . . . . . . . . . . . . . . . . . . . . . 428
6.9 Peritoneal dialysis solution. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 282 9.3.1.2 Drugs for the treatment of severe malaria. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 440
6.10 Parenteral nutrition. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .283 9.3.1.3 Agents for chemoprophylaxis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 444
7. D
rugs acting on the respiratory tract. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 286 9.3.1.4 Other antimalarial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 447
7.1 Antiasthmatic and drugs for chronic obstructive pulmonary disease. . . . . . . . 287 9.3.2 Antiamoebic, antigiardial and antitrichomonal drugs. . . . . . . . . . . . . . . . . . . . . 452
7.1.1 Bronchodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 290 9.3.3 Antileishmanial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 458
7.1.2 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 297 9.3.4 Antitrypanosomal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 462
7.1.3 Prophylactic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 300 9.3.4.1 African trypanosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 462
7.2 Expectorants and cough suppressants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 302 9.3.4.2 American trypanosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 464
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Compound Cough Preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 303 9.3.5 Antipneumocystosis and antitoxoplasmosis drugs. . . . . . . . . . . . . . . . . . . . . . . 465
7.3 Other drugs acting on the respiratory tract . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 309 9.4 Anthelmintics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
8. A
ntiallergics and drugs used in anaphylaxis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 310 9.4.1 Intestinal anthelmintics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
8.1 Antihistamines. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 312 9.4.1.1 Cestode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
8.2 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 318 9.4.1.2 Intestinal nematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 471
8.3 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 319 9.4.1.3 Tissue nematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 474
9. A
nti-infective drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 321 9.4.2 Antifilarials. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 475
9.1 Antibacterial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 323 9.4.2.1 Loiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 475
9.1.1 Beta-lactam drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 323 9.4.2.2 Lymphatic filariasis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 476
9.1.1.1 Penicillins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 324 9.4.2.3 Onchocerciasis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 477
9.1.1.2 Cefalosporins. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 346 9.4.3 Trematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 478
9.1.1.3 Other beta-lactam antibacterials . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 365 9.4.3.1 Schistosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 478
9.1.2 Other antibacterials. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 367 9.4.3.2 Fluke infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 479
9.1.2.1 Chloramphenicol. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 367 9.5 Antiviral drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 480
9.1.2.2 Quinolones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 369 9.5.1 Herpes and cytomegalovirus infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 480
9.1.2.3 Tetracyclines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 382 9.5.2 Antiretroviral drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 482
9.1.2.4 Macrolides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 385 9.5.2.1 Nucleoside reverse transcriptase inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . 485
9.1.2.5 Aminoglycosides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 392 9.5.2.2 Non-nucleoside reverse transcriptase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . 491
9.1.2.6 Nitroimidazoles. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 395 9.5.2.3 Protease inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 493
9.1.2.7 Nitrofurantoin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 397 9.5.2.4 Fixed-dose combinations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 496
9.1.2.8 Spectinomycin . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 397 9.5.3 Other antivirals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 498
9.1.2.9 Sulfonamides and trimethoprim. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 398 10. E
ndocrine system drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 500
9.1.2.10 Lincosamides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 404 10.1 Antidiabetic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 501
9.1.2.11 Vancomycin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 406 10.1.1 Insulins. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 501
9.1.2.12 Furazolidone. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 407 10.1.2 Oral antidiabetic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 506
x | EMDEX 2014/2015 EMDEX 2014/2015 | xi
10.1.2.1 Sulfonylureas. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 507 11.4.4 Drugs used for overactive bladder (OAB) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 572
10.1.2.2 Biguanides. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 510 12. A
ntineoplastic and immunosuppressive drugs, and drugs used in palliative care. . .
10.1.2.3 Thiazolidinediones . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 513 573
10.1.2.4 Dipeptidyl peptidase-4 (DPP-4) inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . 516 12.1 Cytotoxic (antineoplastic) drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .574
10.1.2.5 Alpha glucosidase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 517 12.1.1 Alkylating drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 575
10.1.2.6 Weight-loss agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 518 12.1.2 Cytotoxic antibiotics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 577
10.1.3 Diabetes supplies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519 12.1.3 Antimetabolites and related therapy. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 580
10.2 Thyroid hormones and antithyroid drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519 12.1.4 Vinca alkaloids and etoposide. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 583
10.2.1 Thyroid hormones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519 12.1.5 Other antineoplastic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 585
10.2.2 Antithyroid drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 520 12.2 Immunosuppressive drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 590
10.3 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 522 12.2.1 Cytotoxic immunosuppressants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 590
10.4 Sex hormones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 530 12.2.2 Corticosteroids and other immunosuppressants. . . . . . . . . . . . . . . . . . . . . . . . 591
10.4.1 Estrogens (Female sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 530 12.2.3 Interferons. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 595
10.4.2 Progestogens (Female sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 533 12.3 Sex hormones and antagonists used in malignant diseases. . . . . . . . . . . . . . . . 596
12.4 Drugs used in palliative care. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 601
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10.4.3 Androgens (Male sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 536
10.5 Drugs acting on pituitary ovarian axis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 537 13. O
phthalmological preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 602
10.5.1 Anti-estrogens (Ovulation inducers). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 537 13.1 Anti–infective drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 603
10.5.2 Anterior pituitary hormones (Gonadotrophins). . . . . . . . . . . . . . . . . . . . . . . . . 538 13.2 Anti-Inflammatory/Anti-allergic/Anti-infective drugs. . . . . . . . . . . . . . . . . . . . . . 608
10.5.3 Posterior pituitary hormones . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 541 13.3 Mydriatics and cycloplegics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 614
10.6 Other Endocrine Drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 543 13.3.1 Antimuscarinics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 614
11. D
rugs used in obstetrics, gynaecology and urinary-tract disorders. . . . . . . . . . . . 546 13.3.2 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 615
11.1 Drugs used in obstetricts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 547 13.4 Drugs used in glaucoma. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 616
11.1.1 Oxytocics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 547 13.4.1 Miotics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 617
11.1.2 Antioxytocics (tocolytics). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 551 13.4.2 Beta-blockers . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 617
11.1.3 Nausea and vomiting in pregnancy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 551 13.4.3 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 618
11.2 Genital anti-infectives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 552 13.4.4 Carbonic anhydrase inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 619
11.2.1 Antifungal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 552 13.4.5 Prostaglandin analogue . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 619
11.2.2 Other anti-infective drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 554 13.5 Local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 620
11.3 Contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 554 13.6 Miscellaneous eye preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 620
11.3.1 Oral hormonal contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 555 14. E
ar, nose and throat (ENT) drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 623
11.3.2 Injectable hormonal contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 561 14.1 Ear drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 624
11.3.3 Intrauterine devices. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 563 14.1.1 Anti-infective and/or Anti-inflammatory drugs. . . . . . . . . . . . . . . . . . . . . . . . . . 624
11.3.4 Barrier methods & lubricants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 565 14.1.2 Preparations for the removal of ear wax . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 626
11.3.5 Implantable contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 566 14.2 Nasal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 626
11.3.6 Natural methods & pregnancy test kits. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 567 14.2.1 Intranasal corticosteroids (INCS). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .626
11.4 Drugs for genito-urinary disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 567 14.2.2 Intranasal decongestants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 627
11.4.1 Drugs used in benign prostatic hypertrophy (BPH). . . . . . . . . . . . . . . . . . . . . . 567 14.2.3 Systemic nasal decongestants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 628
11.4.2 Drugs used in urological pain. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 570 14.2.4 Preparations for the cauterisation of nose . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 632
11.4.3 Drugs used in erectile dysfunction (ED). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 570 14.3 Throat drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 632
xii | EMDEX 2014/2015 EMDEX 2014/2015 | xiii
15. D
ermatological drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 634 17.1.2 Vaccines for specific groups of individuals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 682
15.1 Anti-infective skin preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 635 17.1.2.1 Cholera vaccine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 682
15.1.1 Antibacterial preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 635 17.1.2.2 Influenza vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 683
15.1.2 Antifungal preparations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 638 17.1.2.3 Meningococcal meningitis vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 683
15.1.3 Scabicides and pediculicides. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 647 17.1.2.4 Mumps vaccine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 684
15.1.4 Antiviral preparations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 648 17.1.2.5 Rabies vaccine (inactivated). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 685
15.2 Anti-inflammatory and antipruritic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 649 17.1.2.6 Rotavirus vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 686
15.3 Astringents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 655 17.1.2.7 Rubella vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 687
15.4 Preparations for acne. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 655 17.1.2.8 Typhoid vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 688
15.4.1 Topical preparations for acne . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 656 17.1.2.9 Varicella vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 689
15.4.2 Oral preparations for acne. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 657 17.1.2.10 Yellow fever vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 690
15.5 Preparations for psoriasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 658 17.2 Sera and immunoglobulins (Passive immunity). . . . . . . . . . . . . . . . . . . . . . . . . . . 690
15.6 Preparations for actinic keratosis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 659 17.2.1 Anti-D immunoglobulin (human) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 691
15.7 Preparations for warts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 659 17.2.2 Antitetanus immunoglobulin (human) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 692
EMDEX
15.8 Ultraviolet blocking agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 660 17.2.3 Antivenom immunoglobulins. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 692
15.9 Hair growth stimulants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 661 17.2.4 Diphtheria antitoxin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 693
15.10 Other dermatologicals . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 661 17.2.5 Hepatitis B immunoglubulin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 693
16. D
isinfectants and antiseptics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 662 17.2.6 Rabies immunoglobulin (human) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 695
16.1 Aldehydes . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 663 17.2.7 Others. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 695
16.2 Cationic surfactants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 664 18. D
ental formulary. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 696
16.3 Chlorhexidine salts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 664 18.1 Local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 697
16.4 Chlorine and its compounds. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 665 18.1.1 Injectable local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 697
16.5 Dyes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 665 18.1.2 Agents for surface application . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 697
16.6 Hydrogen peroxide. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 665 18.2 Analgesics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
16.7 Iodine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 665 18.2.1 Non-opioid analgesics and antipyretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
16.8 Methylated spirits. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 666 18.2.2 Opioid analgesics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
16.9 Phenols and related substances. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 666 18.2.3 Non-steroidal anti-inflammatory drugs (NSAIDs). . . . . . . . . . . . . . . . . . . . . . . . 698
16.10 Potassium permanganate. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 668 18.3 Vitamin preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
16.11 Alcohol. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 668 18.4 Anti-infective drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
17. I mmunological products and vaccines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 669 18.4.1 Antibacterials. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 698
17.1 Vaccines (Active immunity). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 670 18.4.2 Antifungals . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 699
17.1.1 Vaccines for universal immunization . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 671 18.4.3 Antivirals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 700
17.1.1.1 BCG vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 671 18.5 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 700
17.1.1.2 Diphtheria, pertussis and tetanus vaccines . . . . . . . . . . . . . . . . . . . . . . . . . . . 672 18.6 Mouthwashes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 700
17.1.1.3 Haemophilus influenzae type b vaccine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 675 18.7 Drugs used in treating orofacial pathologies. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 701
17.1.1.4 Hepatitis vaccines. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 676 18.8 Others. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 701
17.1.1.5 Measles vaccines. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 679 19. A
ntidotes and other substances used in poisoning. . . . . . . . . . . . . . . . . . . . . . . . . . . 703
17.1.1.6 Pneumococcal vaccine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .680 19.1 General care and non-specific treatment . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 704
17.1.1.7 Poliomyelitis vaccines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 681 19.2 Specific antidotes . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 705
xiv | EMDEX 2014/2015 EMDEX 2014/2015 | xv
19.2.1 Paracetamol overdosage. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 705 MANUFACTURERS AND/OR IMPORTERS . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 872
19.2.2 Opioid analgesic overdosage . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 706 General Index . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 884
19.2.3 Organophosphate and carbamate poisoning. . . . . . . . . . . . . . . . . . . . . . . . . . . 706
19.2.4 Iron poisoning and iron and aluminium overload. . . . . . . . . . . . . . . . . . . . . . . 707
19.2.5 Heavy metal poisoning. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 707
19.2.6 Methaemoglobinaemia. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 709
19.2.7 Cyanide poisoning . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 709
19.2.8 Heparin overdosage. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 710
19.2.9 Anticoagulant overdosage. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 710
20. D
iagnostic agents and medical equipment. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 711
20.1 Diagnostic Agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 712
20.1.1 Gastric Function. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 712
20.1.2 Myasthenia gravis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 712
20.1.3 Ophthalmology. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 712
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20.1.4 Radio-constrast media. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 713
20.1.5 Tuberculosis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 716
20.1.6 Endocrine Disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 717
20.2 Medical Equipments. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 717
21. N
atural Health Products (NHPs) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 718
21.1 Multivitamin and Minerals with or without Amino Acids . . . . . . . . . . . . . . . . . . 719
21.2 Dietary Supplements for Diabetes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 738
21.3 Herbal preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 739
21.4 Probiotics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 750
Appendix 1: I nteractions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 751
Appendix 2: P
regnancy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 814
Appendix 3: Breastfeeding . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 823
Appendix 4: R
enal impairment. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 829
Appendix 5: H
epatic impairment. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 835
Appendix 6: Abbreviations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 839
Appendix 7: Guide to drug administration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 846
1. Introduction. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 847
2. Nursing process in drug administration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 848
3. Guidelines for safe and effective administration of medications. . . . . . . . . . . . . . 849
4. The seven “Rights” of drug administration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 850
5. Documentation of drug administration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 851
6. Calculation of dosages. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 851
7. Understanding the various routes of drug administration. . . . . . . . . . . . . . . . . . . . 852
8. Other routes of drug administration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 871
INDEX OF PHARMACEUTICAL
Nigeria’s National Drug Policy | 17
Nigeria’s National Drug Essential drugs

Definition:
Policy
These are drugs needed for health care of the majority of the population and therefore be available
at all times in adequate amount, in suitable dosage forms and above all at affordable prices.
It was introduced to correct inbalance in the supply and demand of drugs. It must be based on
prevalent diseases. There must be a committee of people with access to the patients like nurses,
The National Drug Policy for Nigeria presents a formal frame work for meeting the nations drug drug needs doctors, pharmacists, health record officers, etc
through a number of political, administrative, professional, technical, legislative and managerial mechanisms.
The key issues which the policy addresses include: It must also be based on the experience of personnel working in the facility, with financial
• Rationale for a national drug policy in Nigeria resources available.
• Drug situation in Nigeria
Criteria for Selecting Essential Drug List (EDL)
• Implementation strategies encompassing the selection and supply of essential drugs, registration
of medicines, drug quality control, regulations on prescribing and dispensing, legislation and drug For a drug to be included in the EDL, it must satisfy the following criteria based on the philosophy
control administration. of EDL. The drug to be included in the list must:
• Drug information and promotion 1. Satisfy the needs of the great majority of patients/clients at all levels of health care delivery.
• Rational drug use 2. It must have sufficient evidence of efficacy and safety from controlled clinical studies as well as from
• Health education and self medication experience during use.
• Monitoring and evaluation 3. It must be presented in relevant dosage form with reseasonable shelf-life by Nigerian standard and
• Research and development; and financing of drug needs. environmental conditions. Expiry dates and batch numbers must be featured.
The goal of the policy is the constant availability of effective, affordable, safe and good quality drugs in all 4. It must be capable of being manufactured by accredited pharmaceutical companies using locally
sectors of the national health care system as well as an improved quality of health care through rational sourced or imported raw materials or may be imported in bulk cheaply.
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use of drugs. The objectives are: 5. Must be preferably selected in generic form and not trade brand names. The International Non-
• To stimulate awareness at all government decision-making levels as well as among the public about proprietory (generic) Nomenclature (INN) for drugs or pharmaceutical substances should be used
the adverse effects of an unsatisfactory drug situation on health and the national economy whenever available e.g. Metronidazole not Flagyl
• To improve the selection, procurement, storage and distribution of drugs 6. There must be valid certification from local institution, country of origin and World Health
• To promote research and development Organization (WHO).
• To enhance local capacity in manufacturing of drugs, basic chemicals and pharmaceutical industries. 7. Where there are many members of a group, consider frequency of administration, ease of
• To develop an effective system of drug distribution procurement and cost-effectiveness.
• To ensure coordination among the various administrative arms of the government with regard to 8. Preference should be given to drugs with better risk ratio
drug control and drug supply system 9. As much as possible choose simple component drug like paracetamol and not with caffeine, but if
• To develop a drug monitoring and information system and prevent wastes and misuse of drugs. combined choose those that have been known and acceptable.
10. Drugs of the same pharmacodynamic group can be interchanged preferably they have favourable
Definition: A national drug policy is an expression of the way drugs are to be selected, procured, local experience.
distributed, produced, used, regulated and controlled in order to solve the priority health 11. Those with unproven or doubtful therapeutic effects are to be excluded.
problems.
Advantages of EDL
For effective implementation, the formulation of a national drug policy should be undertaken • Proliferation is curbed since fewer drugs are being dealt with in the health care delivery system.
by a multisectorial committee embrasing those responsible for health and national planning as • It is easier for practitioners to familiarize themselves with pharmacological properties and names as
well as those responsible for industrial and fiscal policies of the nation. The goals of the policy will generic rather than trade names would be used.
depend on the emphasis given to these multisectorial aspects within the national development • Drug utilization can be monitored easily at various levels of health care.
• It is easier for drug control agency to formulate strategies for quality assurance and monitoring
plan. For example, the aim of a drug policy from the health perspective will normally be to ensure
• It helps to quantify and estimate true drug needs.
availability of adequate supply of safe, effective and good quality drugs to meet health needs of • It encourages local manufacture and reduces unnecessary expenses with the bulk purchasing
the population. From the social point of view, emphasis will be on providing adequate supply system.
of affordable drugs, whereas, from the perspective of the industrial and trade sector, the main
goal will be to meet the drug demand through development of local pharmaceutical industries Limitations of EDL
• New drugs cannot be easily tried because of the protocol for recognition and inclusion.
that are able to expand on domestic and foreign market, creating employment oppourtunities
• Uncommon diseases cannot be catered for, and consequently, not every patient/client can be
and contributing to the balance of payment through exports and/or import substitution. It is satisfied
because of such varying emphasis that different and sometimes contradictory national drug
policies can be found to exist independently. It is pertinent to know that once drugs cannot be Drug revolving fund (DRF)
considered as ordinary commodities floating around freely in the market situations, countries in
need of formulating national drug policies are best advised to accord priority to their health needs. This concept came about as a result of ‘out of stock’ syndrome which affected most Federal
hospitals in the country. This programme was initiated by Federal Ministry of Health to ensure
In conclusion, a good and balanced drug policy requires a prior analysis of the health needs and ready availability of vital drugs like paracetamol injections, diazepam, infusions, analgesics,
demand for drugs. Basic knowledge on this policy is paramount for all health workers that are antimalaria drugs, etc.
involved in the implementation of this policy.
DRF involves a fixed capital which is recycled to purchase drugs that should be available at every
point in time. The operator of the programme which is usually pharmacist must not give room
for exemption because the actual money may not be realized.
Other people in the health team are involved e.g. Nurses, Accountant but the pharmacist is the
accounting officer.
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18 | Nigeria’s National Drug Policy Nigeria’s National Drug Policy | 19
Objectives • The packages used in dispensing the drug will maintain the potency
• The drugs are dispensed with adequate and clear instructions to the user.
Primarily, the objective of this programme is to:
• Generate enough income from charges on drug to ensure continuous replacement of initial stock Features of irrational use of drug
• Ensure that the drug charges are affordable • Prescribing expensive newer drug when less expensive better known ones will be equally safe for use
(extravagant prescribing)
Role of Nurses/Midwives in Drug Revolving Fund (DRF) • Prescribing many drugs when very few will be appropriate and effective (polypharmacy)
It is the attitude of the health workers that will determine whether the drugs are used judiciously. • Drugs taken without regard to advised frequencies or specified dosage (Failure in compliance)
It is very important as a nurse to exhibit high sense of professional competency and proficiency • It can lead to failure in therapy, risk in drug safety, various treatment complications including drug
resistance and/or sensitivities.
in this scheme so her role is multi-dimentional. It cuts across various nursing cadres of nursing
• Wastage in drug use
personnel commencing from Assistant Director Nursing Service (ADNS) who is a member of
the DRF committee to the student nurse who observe the act of dispensing or administration The role of nurses in ensuring rational drug use
of drug to the patient. • Ensure that the patient takes the drugs (compliance with utilization)
• As a member of DRF committee charged with the responsibility for the provision of information, • Proper labelling of drugs, i.e. writing patient’s name will prevent mismatching of drugs
procurement, pricing and cost recovery, the nurse should insist on a rational approach to pricing of • Ensure that prescribed frequency, time intervals and appropriate route are adhered to
drugs received from source to ensure that the cost of drugs to the patient is equitable and affordable • Observation of special condition associated with medication
and on a graded proportional mark up that has been agreed upon. • Documentation of drugs given for continuity
• As a ward manager, she should have regular information on drugs including drug inventory, current Contributed by:
cost of normal therapeutic regimen as a guide to both the prescriber and the dispenser. She should
enforce proper storage of drugs to maintain their potency. During periodic ward drug inventory, she
reviews the expiry date of drugs and uses her good sense of judgement to recommend those drugs Mrs L.O. Oladipo-Clegg, R.N., RPN. R.M.,B.Sc.,M.Ed.,PGDHM.,MBA Finance
nearing expiry dates and if possible being distributed to other sections to avoid deterioration and Assistant Director Nursing Education/Head of School of Post Basic Psychiatric/Mental Health
wastage of drugs. Nursing, Federal Neuro-Psychiatric Hospital, Yaba, Lagos, Nigeria
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• As a practitioner, she informs the accounting officers of the new admissions/discharges to ensure
that the patients are duely billed in line with the hospital policy on DRF. She educates the patient on
the need for strict compliance to the regimen of the treatment even after discharge for maximum
derivation of the intended therapeutic result and also extend the information to the family members
for better supervision. Once patients are placed on drugs, it is the duty of the nurse to administer
the right drug to right patient at right time, in the right dosage form in a conducive environment
followed up by constant observation of the reaction to the dispensed drugs. All activities must be
properly documented and communicated to the physician in order to assess the progress of the
treatment.
• As a controller, she maintains accurate documentation of drugs, drugs collected from pharmacy and
insist on the physician to prescribe drug from EDL.She also maintains accurate recording of individual
patient drug charts in the wards. Accurate and strict documentation of recording will portray her
value for accountability and reduce pilfering to the bearest minimum in her ward.
• As a councillor she educates the patient and the relatives on the DRF scheme. The need for prompt
payment to ensure constant availability of drugs and this will reduce the incidence of purchasing
fake, expired, substandard drugs by patient and their relatives from private retailer. With constant
availability of drugs, life threatening situations will be tackled, time will be saved and manpower will
be conserved.
• As a professional educator, the nurse is a reliable resource person in all forms of continuous
education programme like seminars, workshops, symposium to update the knowledge of her
colleagues on EDL and DRF. She should also capitalize on any informal oppourtunity to diseminate
appropriate information on the schemes. Should also consider it a priority to impact knowledge on
the EDL & DRF schemes to all her students in various training programmes to facilitate the success
of the scheme. She should conduct research on DRF and forward findings to appropriate quater for
appraisal and implementation.
• As a coordinator, she advocates for cooperation in mutual professional respect among the
physicians, nurses, pharmacists and pharmacy dispensers to provide solid and vital information for
planning, implementation, improvement on DRF in respect of drug procurement or drug purchasing
quality assurance, good dispensing/patient counselling practice so that this loudable success can be
achieved.
Rational use of drugs

It can be defined as judicious use of drug, and focuses on appropriate adoption of drug therapy.
It comprises of rational prescribing, dispensing, and utilization of drugs.
Rational prescribing: Selecting best drug from the available ones and must be given in adequate
dose and regimen.
Rational dispensing: Means that the following must be accomplished:
• The effective form of drug is delivered to the right patient in the prescribed dosage and quantity
General Advice to Prescribers | 21
General Advice to
duration of treatment are suitable for each patient. Drug treatment should be individualized to the
needs of each patient.
• Prescription writing . The prescription is the link between the prescriber, the pharmacist (or dispenser)
and the patient so it is important for the successful management of the presenting medical
Prescribers
condition. This item is covered in more detail in the following section.
• Giving information, instructions and warnings . This step is important to ensure patient adherence and
is covered in detail in the following section.
• Monitoring treatment . Evaluation of the follow up and the outcome of treatment allows the stopping
- Rational approach to therapeutics
of it (if the patient’s problem is solved) or to reformulate it when necessary. This step gives rise to
- Variation in dose response important information about the effects of drugs contributing to building up the body of knowledge
- Adherence (compliance) with drug treatment of pharmacovigilance, needed to promote the rational use of drugs.
- Adverse effects and interactions
- Prescription writing Variation in dose response
- Sample prescription
Success in drug treatment depends not only on the correct choice of drug but on the correct
Rational approach to therapeutics dose regimen. Unfortunately drug treatment frequently fails because the dose is too small or
produces adverse effects because it is too large. This is because most texts, teachers and other
Drugs should only be prescribed when they are necessary, and in all cases the benefit of admin- drug information sources continue to recommend standard doses.
istering the medicine should be considered in relation to the risks involved. Bad prescribing
habits lead to ineffective and unsafe treatment, exacerbation or prolongation of illness, distress The concept of a standard or ‘average’ adult dose for every medicine is firmly rooted in the mind of
and harm to the patient, and higher cost. The Guide to Good Prescribing; Geneva: WHO; 1994, most prescribers. After the initial ‘dose ranging’ studies on new drugs, manufacturers recommend a
provides undergraduates with important tools for training in the process of rational prescribing. dosage that appears to produce the desired response in the majority of subjects. These studies are
usually done on healthy, young male Caucasian volunteers, rather than on older men and women
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The following steps will help to remind prescribers of the rational approach to therapeutics.
with illnesses and of different ethnic and environmental backgrounds. The use of standard
1. Define the patient’s problem doses in the marketing literature suggest that standard responses are the rule, but in reality
Whenever possible, making the right diagnosis is based on integrating many pieces of information: there is considerable variation in drug response. There are many reasons for this variation which
the complaint as described by the patient; a detailed history; physical examination; laboratory include adherence (see below), drug formulation, body weight and age, composition, variation
tests; X-rays and other investigations. in absorption, distribution, metabolism and excretion, variation in pharmacodynamics, disease
variables, genetic, and environmental variables.
This will help in rational prescribing, always bearing in mind that diseases are evolutionary
processes. Drug formulation
2. Specify the therapeutic objective Poorly formulated drugs may fail to disintegrate or to dissolve. Enteric-coated drugs have been
known to pass through the gastrointestinal tract intact. In drugs with a narrow therapeutic to
Doctors must clearly state their therapeutic objectives based on the pathophysiology underlying
toxic ratio, changes in absorption can produce sudden changes in drug concentration. For such
the clinical situation. Very often physicians must select more than one therapeutic goal for each
drugs, quality control surveillance should be carried out.
patient.
Body weight and age
3. Selecting therapeutic strategies
Although the concept of varying the dose with the body weight or age of children has a long
The selected strategy should be agreed with the patient; this agreement on outcome, and how
tradition, adult doses have been assumed to be the same irrespective of size or shape. Yet adult
it may be achieved, is termed concordance. The selected treatment can be non-pharmacological
weights vary two to threefold, while a large fat mass can store large excesses of highly lipid soluble
and/or pharmacological; it also needs to take into account the total cost of all therapeutic options.
drugs compared to lean patients of the same weight.
a) Non-pharmacological treatment
Age changes can also be important. Adolescents may oxidize some drugs relatively more rapidly
It is very important to bear in mind that the patient does not always need a drug for treatment of than adults, while the elderly may have reduced renal function and eliminate some drugs more
the condition. Very often, health problems can be resolved by a change in life style or diet, use of slowly.
physiotherapy or exercise, provision of adequate psychological support, and other non-pharma-
DOSE CALCULATION IN CHILDREN
cological treatments; these have the same importance as a prescription drug, and instructions
must be written, explained and monitored in the same way. Children’s doses may be calculated from adult doses by using age, body weight, or body surface
area, or by a combination of these factors. The most reliable methods are those based on body
b) Pharmacological treatment
surface area.
• Selecting the correct group of drugs . Knowledge about the pathophysiology involved in the clinical
situation of each patient and the pharmacodynamics of the chosen group of drugs, are two of the Body weight may be used to calculate doses expressed in mg/kg. Young children may require a
fundamental principles for rational therapeutics. higher dose per kilogram than adults because of their higher metabolic rates. Other problems
• Selecting the drug from the chosen group . The selection process must consider benefit/risk/cost need to be considered. For example, calculation by body weight in an overweight child may
information. This step is based on evidence about maximal clinical benefits of the drug for a given
result in much higher doses being administered than necessary; in such cases, dose should be
indication (efficacy) with the minimum production of adverse effects (safety). It must be remembered
calculated from an ideal weight, related to height and age.
that each drug has adverse effects and it is estimated that up to 10% of hospital admissions in
industrialized countries are due to adverse effects. Not all drug-induced injury can be prevented but Nomograms are available to allow body surface values to be calculated from a child’s height
much of it is caused by inappropriate selection of drugs. In cost comparisons between drugs, the cost and weight.
of the total treatment and not only the unit cost of the drug must be considered.
• Verifying the suitability of the chosen pharmaceutical treatmentfor each patient . The prescriber must Where the dose for children is not readily available, prescribers should seek specialist advice
check whether the active substance chosen, its dosage form, standard dosage schedule and standard before prescribing for a child.
22 | General Advice to Prescribers General Advice to Prescribers | 23
Physiological and pharmacokinetic variables be related to the patient, the disease, the doctor, the prescription, the pharmacist or the health
system and can often be avoided.
Drug absorption rates may vary widely between individuals and in the same individual at different
times and in different physiological states. Drugs taken after a meal are delivered to the small Patients’ perceptions of the risk and severity of adverse drug reactions may differ from the health
intestine much more slowly than in the fasting state, leading to much lower drug concentrations. care provider and may affect adherence.
In pregnancy gastric emptying is also delayed, while some drugs may increase or decrease gastric
Low-cost strategies for improving adherence increase effectiveness of health interventions and
emptying and affect absorption of other drugs.
reduce costs. Such strategies must be tailored to the individual patient.
Drug distribution
Health care providers should be familiar with techniques for improving adherence and they
Drug distribution varies widely: fat-soluble drugs are stored in adipose tissue, water-soluble drugs should employ systems to assess adherence and to determine what influences it.
are distributed chiefly in the extracellular space, acidic drugs bind strongly to plasma albumin
Patient reasons
and basic drugs to muscle cells. Hence variation in plasma-albumin concentration, fat content
or muscle mass may all contribute to dose variation. With very highly albumin bound drugs like In general, women tend to be more adherent than men, younger patients and the very elderly
warfarin, a small change of albumin concentration can produce a big change in free drug and a are less adherent, and people living alone are less adherent than those with partners or spouses.
dramatic change in drug effect. Specific education interventions have been shown to improve adherence. Patient disadvantages
such as illiteracy, poor eyesight or cultural attitudes (for example preference for traditional
Drug metabolism and excretion
or alternative medicines and suspicion of modern medicine) may be very important in some
Drug metabolism is affected by genetic, environmental, and disease-state factors. Drug acetylation individuals or societies; as may economic factors. Such limitations or attitudes need to be
shows genetic polymorphism, whereby individuals fall clearly into either fast or slow acetylator discussed and taken account of.
types. Drug oxidation, however, is polygenic, and although a small proportion of the population
Disease reasons
can be classified as very slow oxidizers of some drugs, for most drugs and most subjects there is
a normal distribution of drug metabolizing capacity. Conditions with a known worse prognosis (for example cancer) or painful conditions (for example
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rheumatoid arthritis) elicit better adherence than asymptomatic ‘perceived as benign’ conditions
Many drugs are eliminated by the kidneys without being metabolized. Renal disease or toxicity
such as hypertension.
of other drugs on the kidney can therefore slow excretion of some drugs.
Doctor reasons
Pharmacodynamic variables
Doctors may cause poor adherence in many ways—by failing to inspire confidence in the
There is significant variation in receptor response to some drugs, especially central nervous system
treatment offered, by giving too little or no explanation, by thoughtlessly prescribing too many
responses, for example pain and sedation. This can be because of genetic factors, tolerance, drug
medicines, by making errors in prescribing, or by their overall attitude to the patient.
interactions, and drug dependence.
The doctor-patient interaction
Disease variables
There is considerable evidence that this is crucial to concordance. ‘Satisfaction with the interview’
Both liver disease and kidney disease can have major effects on drug response, chiefly by the
is one of the best predictors of good adherence. Patients are often well informed and expect a
effect on metabolism and elimination respectively (increasing toxicity), but also by their effect
greater say in their health care. If they are in doubt or dissatisfied they may turn to alternative
on plasma albumin (increased free drug also increasing toxicity). Heart failure can also affect
options, including ‘complementary medicine’. There is no doubt that the drug ‘doctor’ has a
metabolism of drugs with rapid hepatic clearance (for example lidocaine, propranolol). Respiratory
powerful effect on inspiring confidence and perhaps contributing directly to the healing process.
disease and hypothyroidism can impair drug oxidation.
Prescription reasons
Enviromental variables
Many aspects of the prescription may lead to non-adherence (non-compliance). It may be illegible
Many drugs and environmental toxins can induce the hepatic microsomal enzyme oxidizing
or inaccurate; it may get lost; it may not be refilled as intended or instructed for a chronic disease.
system or cytochrome P450 oxygenases, leading to more rapid metabolism and elimination and
Also, the prescription may be too complex; the greater the number of medicines the poorer the
ineffective treatment. Environmental pollutants, anaesthetic drugs and other compounds such as
adherence, while multiple doses also decrease adherence if more than two doses per day are
pesticides can also induce metabolism. Diet and nutritional status also affect pharmacokinetics.
given. Not surprisingly adverse effects like drowsiness, impotence or nausea reduce adherence
For example in infantile malnutrition and in malnourished elderly populations drug oxidation
and patients may not admit to the problem.
rates are decreased, while high protein diets, charcoal cooked foods and certain other foods act
as metabolizing enzyme inducers. Chronic alcohol use induces oxidation of other drugs, but Pharmacist reasons
in the presence of high circulating alcohol concentrations drug metabolism may be inhibited. The pharmacist’s manner and professionalism, like the doctor’s, may have a positive influence on
adherence, or a negative one, raising suspicions or concerns. This has been reported in relation
Adherence (compliance) with drug treatment to generic drugs when substituted for brand-name drugs. Pharmacist information and advice
can be a valuable reinforcement, as long as it agrees with the doctor’s advice.
It is often assumed that once the appropriate drug is chosen, the prescription correctly written
and the medication correctly dispensed, that it will be taken correctly and treatment will be The health care system
successful. Unfortunately this is very often not the case, and physicians overlook one of the most The health care system may be the biggest hindrance to adherence. Long waiting times, uncaring
important reasons for treatment failure—poor adherence (compliance) with the treatment plan. staff, uncomfortable environment, unreliable drug supplies and so on, are all common problems
There are sometimes valid reasons for poor adherence—the drug may be poorly tolerated, may in many settings, and have a major impact on adherence. An important problem is the distance
cause obvious adverse effects or may be prescribed in a toxic dose. Failure to adhere with such a and accessibility of the clinic from the patient. Some studies have confirmed the obvious, that
prescription has been described as ‘intelligent non-compliance’. Bad prescribing or a dispensing patients furthest from the clinic are least likely to adhere to treatment in the long term.
error may also create a problem, which patients may have neither the insight nor the courage Recommendations
to question. Even with good prescribing, failure to adhere to treatment is common. Factors may • Review the prescription to make sure it is correct.
• Spend time explaining the health problem and the reason for the drug. Interactions may occur when one drug alters the absorption, distribution or elimination of
• Establish good rapport with the patient. another drug, such that the amount which reaches the site of action is increased or decreased.
• Explore problems, for example difficulty with reading the label or getting the prescription filled.
• Encourage patients to bring their medication to the clinic, so that tablet counts can be done to Drug-drug interactions are some of the commonest causes of adverse effects. When two drugs
monitor compliance. are administered to a patient, they may either act independently of each other, or interact with
• Encourage patients to learn the names of their medicines, and review their regimen with them. Write each other. Interaction may increase or decrease the effects of the drugs concerned and may
notes for them. cause unexpected toxicity.
• Keep treatment regimens simple.
• Communicate with other health care professionals, to develop a team approach and to collaborate As newer and more potent drugs become available, the number of serious drug interactions is
on helping and advising the patient. likely to increase. Remember that interactions which modify the effects of a drug may involve
• Involve the partner or another family member. non-prescription drugs, non-medicinal chemical agents, and social drugs such as alcohol,
• Listen to the patient. marijuana, tobacco, and traditional remedies, as well as certain types of food for example
grapefruit juice. The physiological changes in individual patients, caused by such factors as age
Adverse effects and interactions and gender, also influence the predisposition to ADRs resulting from drug interactions.
Adverse drug reactions The following table lists drugs under the designation of specific cytochrome P450 isoforms. A
drug appears in a column if there is published evidence that it is metabolized, at least in part,
An adverse drug reaction (ADR) may be defined as ‘any response to a drug which is noxious, via that isoform. Alterations in the rate of the metabolic reaction catalyzed by that isoform are
unintended and occurs at doses normally used for prophylaxis, diagnosis, or therapy…’. ADRs are likely to have effects on the pharmacokinetics of the drug.
therefore unwanted or unintended effects of a medicine, including idiosyncratic effects, which
occur during its proper use. They differ from accidental or deliberate excessive dosage or drug Incompatibilities between drugs and intravenous fluids
maladministration (see section 19 for the treatment of poisoning). Drugs should not be added to blood, amino acid solutions or fat emulsions. Certain drugs, when
ADRs may be directly linked to the properties of the drug in use, the so-called ‘A’ type reactions. added to intravenous fluids, may be inactivated by pH changes, by precipitation or by chemical
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An example is hypoglycaemia induced by an antidiabetic drug. ADRs may also be unrelated to reaction. Benzylpenicillin and ampicillin lose potency after 6–8 hours if added to dextrose
the known pharmacology of the drug, the ‘B’ type reactions including allergic effects, for example solutions, due to the acidity of these solutions. Some drugs bind to plastic containers and tubing,
anaphylaxis with penicillins. for example diazepam and insulin. Aminoglycosides are incompatible with penicillins and
heparin. Hydrocortisone is incompatible with heparin, tetracycline, and chloramphenicol.
Thalidomide marked the first recognized public health disaster related to the introduction of a
new drug. It is now recognized that clinical trials, however thorough, cannot be guaranteed to Cytochrome P450 Drug Interaction Table
detect all adverse effects likely to be caused by a drug. Health workers are thus encouraged to SUBSTRATES
record and report to their national pharmacovigilance centre any unexpected adverse effects CYP3A4, 5, 7
Amlodipine
with any drug to achieve faster recognition of serious related problems. Chlorphenamine
Ciclosporin
Major factors predisposing to adverse effects Diazepam
CYP2C19 CYP2D6 Erythromycin
It is well known that different patients often respond differently to a given treatment regimen. Amitriptyline
CYP2C9
Amitriptyline Haloperidol
CYP2B6 Ibuprofen
For example, in patients taking combinations of drugs known to interact, only a small number Cyclophosphamide
Clomipramine
Phenytoin
Clomipramine CYP2E1 Indinavir
CYP1A2 Cyclophosphamide Codeine Alcohol Methadone
show any clinical evidence of interactions. In addition to the pharmaceutical properties of the Efavirenz
Diazepam
Sulfamethoxazole
Haloperidol Paracetamol Nifedipine
drug therefore, there are characteristics of the patient which predispose to ADRs. Methadone Tamoxifen
Phenobarbital Tamoxifen Quinidine
Warfarin
Phenytoin Timolol Quinine
EXTREMES OF AGE Ritonavir
Saquinavir
The very old and the very young are more susceptible to ADRs. Drugs which commonly cause Tamoxifen
problems in the elderly include hypnotics, diuretics, non-steroidal anti-inflammatory drugs, Verapamil
Vincristine
antihypertensives, psychotropics and digoxin.
INHIBITORS
All children, and particularly neonates, differ from adults in their response to drugs. Some drugs 3A4
are likely to cause problems in neonates (for example morphine), but are generally tolerated in 2D6 Clarithromycin
Chlorphenamine Erythromycin
children. Other drugs (for example valproic acid) are associated with increased risk of ADRs in Clomipramine Grapefruit juice
1A2 2C9
children of all ages. Other drugs associated with problems in children include chloramphenicol Ciprofloxacin
2B6 2C19
Isoniazid
Haloperidol 2E1 Indinavir
Methadone Nelfinavir
(grey baby syndrome), antiarrhythmics (worsening of arrhythmias), acetylsalicylic acid (Reye Quinidine Ritonavir
syndrome). Ritonavir Saquinavir
Verapamil
INTERCURRENT ILLNESS. INDUCERS
3A4
If besides the condition being treated the patient suffers from another disease, such as kidney, 2B6 2E1 Carbamazepine
1A2 2C9
liver or heart disease, special precautions may be necessary to prevent ADRs. The genetic make-up Tobacco
Phenobarbital 2C19
Rifampicin
2D6 Alcohol Phenobarbital
of the individual patient may also predispose to ADRs. Rifampicin Isoniazid Phenytoin
Rifampicin
DRUG INTERACTIONS. Adverse effects caused by traditional medicines
Interactions (see also Appendix 1) may occur between drugs which compete for the same receptor Patients who have been or are taking traditional herbal remedies may develop ADRs. It is not
or act on the same physiological system. They may also occur indirectly when a drug-induced always easy to identify the responsible plant or plant constituent. Refer to the drug and toxicology
disease or a change in fluid or electrolyte balance alters the response to another drug. information service if available or to suitable literature.
The effect of food on drug absorption Narcotics and controlled substances
Food delays gastric emptying and reduces the rate of absorption of many drugs; the total amount The prescribing of a medicinal product that is liable to abuse requires special attention and
of drug absorbed may or may not be reduced. However, some drugs are preferably taken with may be subject to specific statutory requirements. Practitioners may need to be authorized to
food, either to increase absorption or to decrease the irritant effect on the stomach. prescribe controlled substances; in such cases it might be necessary to indicate details of the
authority on the prescription.
Prescription writing In particular, the strength, directions and the quantity of the controlled substance to be dispensed
A prescription is an instruction from a prescriber to a dispenser. The prescriber is not always a should be stated clearly, with all quantities written in words as well as in figures to prevent
doctor but can also be a paramedical worker, such as a medical assistant, a midwife or a nurse. The alteration. Other details such as patient particulars and date should also be filled in carefully to
dispenser is not always a pharmacist, but can be a pharmacy technician, an assistant or a nurse. avoid alteration.
Every country has its own standards for the minimum information required for a prescription,
and its own laws and regulations to define which drugs require a prescription and who is entitled
to write it. Many countries have separate regulations for prescriptions for controlled drugs such
as opioid analgesics.
The following guidelines will help to ensure that prescriptions are correctly interpreted and
leave no doubt about the intention of the prescriber. The guidelines are relevant for primary
care prescribing; they may, however, be adapted for use in hospitals or other specialist units.
Prescription form
The most important requirement is that the prescription be clear. It should be legible and indicate
precisely what should be given. The local language is preferred.
EMDEX
The following details should be shown on the form:
• The prescriber’s name, address and telephone number. This will allow either the patient or the
dispenser to contact the prescriber for any clarification or potential problem with the prescription.
• Date of the prescription. In many countries the validity of a prescription has no time limit, but in
some countries pharmacists do not dispense drugs on prescriptions older than 3 to 6 months.
• Name, form and strength of the drug. The International Nonproprietary Name of the drug should
always be used. If there is a specific reason to prescribe a special brand, the trade name can be added.
Generic substitution is allowed in some countries. The pharmaceutical form (for example ‘tablet’, ‘oral
solution’, ‘eye ointment’) should also be stated.
• The strength of the drug should be stated in standard units using abbreviations that are
consistent with the Système Internationale (SI). ‘Microgram’ and ‘nanogram’ should not, however,
be abbreviated. Also, ‘units’ should not be abbreviated. Avoid decimals whenever possible. If
unavoidable, a zero should be written in front of the decimal point.
• Specific areas for filling in details about the patient including name, address and age.
Directions
Directions specifying the route, dose and frequency should be clear and explicit; use of phrases
such as ‘take as directed’ or ‘take as before’ should be avoided.
For preparations which are to be taken on an ‘as required’ basis, the minimum dose interval should
be stated together with, where relevant, the maximum daily dose. It is good practice to qualify
such prescriptions with the purpose of the medication (for example ‘every 6 hours as required
for pain’, ‘at night as required to sleep’).
It is good practice to explain the directions to the patient; these directions will then be reinforced
by the label on the medicinal product and possibly by appropriate counselling by the dispenser.
It may be worthwhile giving a written note for complicated regimens although it must be borne
in mind that the patient may lose the separate note.
Quantity to be dispensed
The quantity of the medicinal product to be supplied should be stated such that it is not confused
with either the strength of the product or the dosage directions.
Alternatively, the length of the treatment course may be stated (for example ‘for 5 days’).
Wherever possible, the quantity should be adjusted to match the pack sizes available. For liquid
preparations, the quantity should be stated in millilitres (abbreviated as ‘ml’) or litres (preferably
not abbreviated since the letter ‘l’ could be confused with the figure ‘1’).
1.1 Drugs used in anxiety and sleep disorders | 29
1. Central nervous system 1.1 Drugs used in anxiety and insomnia.

sleep disorders Good Sleep Hygiene Measures
The most widely used anxiolytics and hyp- • Maintain a regular schedule for bedtime and awak-
(CNS) drugs
notics are the benzodiazepines. Treatment of ening. Go to bed only when sleepy.
anxiety should be limited to the lowest effec- • Avoid daytime naps or going to bed too early in
evening. Reserve the bedroom for sleep & sexual
tive dose for the shortest possible time. The
activity (no TV).
cause of insomnia should be established and • Avoid caffeine & nicotine especially within 4-6hrs
1.1 Drugs used in anxiety and sleep disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 29 appropriate treatment for underlying factors of bedtime. Do not drink alcohol (especially within
instituted before hypnotics are considered. 4hrs of bedtime), since it causes fragmented sleep
1.2 Drugs used in psychotic disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 32 Hypnotics may be of value for a few days but • Avoid heavy meals before going to bed, but a light
1.3 Antidotes to antipsychotic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 40 rarely longer than a week. carbohydrate snack before bedtime is acceptable
Tolerance and dependence (both physical and • Do not eat chocolate or large amounts of sugar
1.4 Drugs used in mood disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .41 psychological) and subsequent difficulty in before bedtime. Avoid drinking excessive amounts
of fluid in the evening
1.4.1 Drugs used in depressive disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 41 withdrawing the drug may occur after regular
• Take “water pills” in the morning or early afternoon
use for more than a few weeks. Patients with • Exercise regularly during the day, but avoid vigor-
1.4.2 Drugs used in bipolar disorders . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 48 chronic anxiety, alcohol or drug dependence ous exercise within 3 hrs of retiring (eg. a walk after
1.5 Obsessive-compulsive disorders and panic attacks. . . . . . . . . . . . . . . . . . . . . . . . . . 51 or those with personality disorders are more supper is a great idea)
likely to become dependent. Anxiolytics and • Minimize noise, light & extreme temperature in
1.6 Antiparkinson drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51 hypnotics should be prescribed in carefully the bedroom. Develop relaxing bedtime rituals
1.6.1 Drugs used in parkinsonism. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51 individualized dosage and use should be (eg. reading, listening to music)
limited to control of acute conditions such as • Get the clock out of visible range to avoid
EMDEX
1.6.2 Drugs used in essential tremor and related disorders. . . . . . . . . . . . . . . . . . . . . . 55 panic attacks and acute anxiety and severe, watching!
• Get out of bed & go to another room if unable
1.7 Anticonvulsants (Antiepileptics). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 55 incapacitating insomnia. There is usually no
to sleep within 20 minutes. Return when sleepy.
justification for prolonging treatment with
1.8 Analgesics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 66 (Source: RxFiles. Sleep: Sedative comparison chart. Available
anxiolytics and hypnotics for more than one
from: http://www.rxfiles.ca/)
1.8.1 Non-opioid analgesics and antipyretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 67 to two weeks.
If used for longer periods, withdrawal should
1.8.2 Opioid analgesics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 75 BROMAZEPAM
be gradual by reduction of the dose over a pe-
1.9 Drugs used in substance dependence programes. . . . . . . . . . . . . . . . . . . . . . . . . . . 81 riod of weeks or months, as abrupt discontinu- Indications: Acute tension and anxiety states;
ation may produce confusion, toxic psychosis, difficulties in interpersonal contact, insomnia,
1.10 Drugs used in migraine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 81
convulsions or a condition resembling delirium anxious depressive reactions; functional distur-
1.10.1 Acute migraine attack . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 82 tremens. The benzodiazepine withdrawal syn- bances in the cardiovascular, respiratory, GI and
1.10.1.1 Analgesics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 82 drome may develop at any time up to 3 weeks genitourinary systems.
after stopping a long-acting benzodiazepine Contra-indications, Precautions, Adverse
1.10.1.2 Ergot alkaloids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83 but may occur within a few hours in the case of effects, Nursing action, and Advice to pa-
1.10.1.3 Antiemetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83 a short-acting one. The syndrome is character- tients: See under Diazepam.
ized by insomnia, anxiety, loss of appetite and Dose: Usually 1.5-3 mg 2-3 times daily; may
1.10.2 Migraine prophylaxis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 83 bodyweight, tremor, perspiration, tinnitus and be increased depending on response
perceptual disturbances. These symptoms may and/or severity.
be similar to the original complaint and encour- POM Apo-Bromazepam (Lahams)
age further prescribing. Some symptoms may Tablets, Bromazepam 1.5 mg (white scored bev-
continue for weeks or months after stopping el-edged tab. marked ‘APO B-1.5’); 3 mg (pink scored
benzodiazepines. bevel-edged tab. marked ‘APO B-3’).
Patients should be warned that their ability Pack: 100’s.
to drive or operate machinery may be im- POM BRAZEPAM® (Theodor)
paired and that the effects of alcohol may be Tablets, Bromazepam 1.5 mg (yellow tab.); 3 mg
enhanced. (rose pink tab.).
Temazepam, Oxazepam and Lorazepam Pack: 30’s; 500’s.
have intermediate half-lives (reduced daytime POM BROMATAN® (May & Baker)
sedation), no active metabolites and are good Tablets, Bromazepam 1.5 mg, 3 mg
sedative choices especially for the elderly. Zo- Pack: 30’s
piclone has lower incidence of tolerance and POM JUXOTAN® (Juhel)
withdrawal compared to benzos and may be Tablet, Bromazepam 3 mg; pink scored biconvex tab.
the preferred sedative agent for some patients. 3 mg - 100’s; 1000’s.
Use the lowest effective dose and for no more
POM LEKAM® (Taylek)
than 3-4 weeks. Advise patient to discontinue Tablets, Bromazepam 1.5 mg, 3 mg.
gradually to minmize incidence of rebound 1.5 mg - 3 x 10’s.
30 | 1.1 Drugs used in anxiety and sleep disorders 1.1 Drugs used in anxiety and sleep disorders | 31
3 mg - 3 x 10’s. and call button); supervise ambulation. marked ‘ROCHE 5’. NITRAZEPAM
• Relieve dry mouth with frequent sips of water, hard 5 mg - 12; 96; 500. Pharmacology: It rapidly induces sleep, last-
POM LENITIN® (Dizpharm)
candy or sugarless gum. Injection, Diazepam 10 mg per 2 mL.
Tablet, Bromazepam 3 mg ing 6-8 hours, but accumulation of the drug
• Advise patient to make position changes slowly as Pack: 10.
POM LEXOTAN® (Swipha) fainting may occur, especially in elderly; to avoid occurs, since its plasma t½ is 20-31 hours. It is
POM VINCOPAM®-5 (Vinco) nontoxic in overdose and for this reason has
Tablets, Bromazepam 1.5 mg, 3 mg; scored tabs. abrupt discontinuation after prolonged use.
Tablet, Diazepam 5 mg; scored yellow biconvex tab. become very popular. A drug with a shorter
1.5 mg - 30; 500. • Inform patient drug is not for everyday stress
marked ‘D5’.
3 mg - 30; 500. and should not be used for more than 4 months t½ should replace nitrazepam as the hypnotic
5 mg - 1000’s (in tamper-proof tin)
without doctor’s prescription; not to use more than of first choice.
POM TALEN® (Swipha) prescribed amount, may be habit forming. POM ZEDAPAM® (Neimeth) Indications: Short-term management of
Tablet, Bromazepam 1.5 mg; 3 mg. • Warn patient to avoid activities that require mental Tablet, Diazepam 5 mg. insomnia
1.5 mg - 30, 500 alertness and physical coordination until the CNS 5 mg - 20’s; 1000’s. Contra-indications, Precautions, Adverse
3 mg - 30, 500 effects of the drug are established; to avoid alcohol
and other CNS depressants, unless prescribed.
effects, Nursing action, and Advice to pa-
FLUNITRAZEPAM tients: See under Diazepam.
DIAZEPAM • Monitor patient on long-term medication for
signs of dependency or withdrawal symptoms
Pharmacology: It is readily absorbed from Dose: Adult, 5-10 mg at night. To be swal-
Drug subject to international control under the Conven- the GIT, 77 to 80% protein bound, extensively
namely headache, nausea, vomiting, muscle pain, lowed whole or dissolved in liquid.
tion on Psychotropic Substances (1971). metabolised in the liver and excreted mainly in
weakness.
POM Nitrazepam (Kayhelt)
Indications: short-term treatment of anxiety Dose: Anxiety, by mouth, ADULT 2 mg 3 urine as metabolites. It has long t½ and hence,
Tablet, Nitrazepam 5 mg
and insomnia; status epilepticus, recurrent times daily increased if necessary to a tendency to cause cumulative and residual 5 mg - 10’s
seizures; febrile convulsions, adjunct in acute 15–30 mg daily in divided doses; EL- effects such as excessive drowsiness.
alcohol withdrawal (section 1.7); premedica- Indication: Short-term management of POM Nitrazepam (Vitabiotics)
DERLY (or debilitated) half adult dose.
insomnia Tablets, Nitrazepam 5 mg
tion (section 3.2) Insomnia, by mouth, ADULT 5–15 mg
EMDEX
5 mg - 250’s
Contra-indications: Respiratory depression; at bedtime. Contra-indication, Precautions, Adverse
acute pulmonary insufficiency; sleep apnoea; effects, Nursing action, and Advice to pa- POM SWIDON® (Swipha)
POM Diazepam (WMF 24.3) Tablet, Nitrazepam 5 mg; off-white scored tab
severe hepatic impairment; myasthenia gravis tients: See under Diazepam.
Tablets , (scored), Diazepam 2 mg, 5 mg. 5 mg - 10.
Precautions: Respiratory disease, muscle weak- Dose: Adult, 0.5-1 mg at night
ness, history of alcohol or drug abuse, marked POM Diazepam (EDL 27.2) POM SOMNAPAM® (Vitabiotics)
POM ROHYPNOL® (Swipha)
personality disorder; pregnancy (Appendix 2); Tablets , (scored), Diazepam 2 mg, 5 mg. Tablet, Nitrazepam 5 mg.
Tablet, Flunitrazepam 1 mg; scored tab.
breastfeeding (Appendix 3); reduce dose in elderly POM Apo-Diazepam (Lahams) 1 mg - 30. 5 mg - 20’s.
or debilitated and in hepatic impairment (avoid if Tablets, Diazepam 5 mg (yellow, scored bevel-edged
severe, Appendix 5), renal impairment (Appendix tab. marked ‘APO 5’); 10 mg (blue, scored bev- LORAZEPAM ZOPICLONE
4); avoid prolonged use and abrupt withdrawal; el-edged tab. marked ‘APO 10’). Pharmacology: Zopiclone is a cyclopyrrolone
Therapeutic category: Antianxiety Agent;
Pack: 1000’s with actions similar to benzodiazepines namely
porphyria; interactions: Appendix 1 Anticonvulsant; Antiemetic; Benzodiazepine;
Adverse effects: Drowsiness and light-head- POM CALMPOSE® (Ranbaxy) Sedative. hypnotic, sedative, anxiolytic, anticonvulsant
edness the next day; confusion and ataxia (es- Injection, Diazepam 10 mg per 2 mL. Pharmacology: Lorazepam is an intermedi- and muscle relaxant. It shortens sleep onset
pecially in the elderly); amnesia; dependence; Pack: 100 x 2 mL. latency and causes minimal residual effects
ate-acting benzodiazepine, effective orally,
paradoxical increase in aggression; muscle POM DEZOPAM® (JB Pharma) IM or IV. Following oral administration, a the following morning - it does not accumulate
weakness; occasionally headache, vertigo, Tablet, Diazepam 5 mg peak concentration occurs at 2 hours and this significantly on repeated dosing and has short
salivation changes, GI disturbances, visual 5 mg - 10’s (in blister) corresponds to the time when clinical effects apparent half-life. The site of action, as with
disturbances, dysarthria, tremor, changes in are maximal.The elimination t½ is 12 hours other cyclopyrrolones, is however different
POM Diazepam (Emzor)
libido, incontinence, urinary retention; blood Tablets, Diazepam 2 mg, 5 mg, 10 mg; all yellow and conjugation with glucuronide to form an from that of benzodiazepines.
disorders and jaundice; skin reactions; raised scored tabs. inactive substance is the major mechanism of Indications: Short term treatment of insomnia,
liver enzymes. lorazepam clearance. Time to peak plasma con- including difficulties in falling asleep, nocturnal
POM Diazepam (Juhel)
Advice to patients: May cause drowsiness. centration following IM administration is about awakening and early awakening, transient,
Tablet, Diazepam 5 mg.
Ability to operate machinery or drive may be 5 mg - 1000. 3 hours while IV administration is followed by situational or chronic insomnia, and insomnia
impaired. Avoid alcoholic beverages. See Good Injection, Diazepam 10 mg per 2 mL; in 2-mL amp. a “latency of action” of about 5 minutes prior to secondary to psychiatric disturbances, in situ-
Sleep Hygiene in clinical notes above Pack: 2 mL x 10’s (in amps). the onset of clinical effects. May be useful drug ations where the insomnia is debilitating or is
Nursing action: in the elderly and in liver disease, since it is not causing severe distress for the patient.
POM DIAZOOM® (Zoomota)
• Give with food or milk to reduce GI upset; may hydroxylated or demethylated. Contra-indications: Myasthenia gravis; res-
Injection, Diazepam 5 mg per mL; in 2 mL amp.
crush tablet if patient has difficulty swallowing - Indications: Anxiety disorders and short-term piratory failure; severe sleep apnoea syndrome;
Pack: 2 mL x 10’s (in amps)
avoid crushing s-r medications. severe hepatic impairment; pregnancy, lacta-
relief of the symptoms of anxiety or insomnia.
• Ensure patient swallows medication. POM IZEP® (Chanmedi) tion, children.
• Give IV slowly (not more than 5 mg per minute); Injection, Diazepam 10 mg per 2 mL. Contra-indications, Precautions, Adverse ef-
fects, Nursing action and Advice to patients: Precautions: Elderly, hepatic & renal insuf-
monitor respirations frequently. Pack: 1 x 100’s.
• Observe the IV injection site for phlebitis; do not See under Diazepam. ficiency (reduce dose); Psychiatric disorders;
inject into small veins to minimize the risk of POM VALINEX–5® (Vitabiotics) Dose: By mouth, Anxiety, 2 -3 mg in divided History of drug abuse. May impair ability to
extravasation Tablet, Diazepam 5 mg; yellow tablet. drive or operate machinery. Limit treatment
doses. Insomnia, 1-2 mg usually at
• IM injection is painful and absorption is variable; 5 mg – 20’s; 1000’s. duration to <4 wk to minimise risk of depend-
bedtime; short-term use only.
IV route is more reliable. POM VALIUM® (Swipha) ence and tolerance. Avoid abrupt discontinu-
• Provide safety measures (i.e., side rails, night light, Tablets, Diazepam 5 mg, light-yellow scored tab. ation of therapy.
EMDEX 2014/2015 | Get your EMDEX Vol. 3 (Drug Comparisons & Therapeutic Details) at no extra charge See EMDEX Paediatric Drug Guide for details on medication use in children & adolescents
32 | 1.2 Drugs used in psychotic disorders 1.2 Drugs used in psychotic disorders | 33
Interactions: May enhance CNS depressant thought disorder, hallucinations and delusions are caused most frequently by the piperazine • In some patients especially schizophrenic patients,
effects of alcohol, hypnotics, opioid analgesics, and prevent relapse. They are usually less effec- phenothiazines such as fluphenazine, the buty- drugs may be given by injection as depot prepara-
TCAs. Reduced hypnotic effect with CYP3A4 tive in apathetic, withdrawn patients, but they rophenones such as haloperidol, and the depot tions to prevent the problem of non-compliance.
inducers such as rifampicin, phenytoin and can sometimes have an activating influence. preparations; the newer ‘atypical’ antipsychotics • Occasionally, a patient’s paranoia may extend to
drugs they are given. They may think that the
carbamazepine. Increased hypnotic effect with Patients with acute schizophrenia generally cause fewer extrapyramidal symptoms than
staff are trying to poison them thereby refusing
CYP3A4 inhibitors e.g. erythromycin, clarithro- respond better than those with chronic symp- other antipsycotics. Although easily recognized, the drugs.
mycin, ketoconazole, itraconazole, ritonavir. toms. In the acute phase chlorpromazine may extrapyramidal symptoms are not so easy to • Drug education should commence while the pa-
Adverse effects: Most common is metal- be administered by intramuscular injection in predict because they depend on the dose and tient is on admission to prevent non-compliance
lic or bitter after-taste. Less commonly, GI a dose of 25–50 mg which can be repeated patient susceptibility as well as the drug. when the patient gets back home. This may lead
disturbances including nausea & vomiting; every 6–8 hours while observing the patient Extrapyramidal symptoms consist of parkinso- to relapse if treatment is stopped. Relatives may
headache, dizziness, drowsiness, dry mouth. for possible hypotension. In most cases, nian-type symptoms including tremor which have to be involved. Contact numbers to call for
Especially in the elderly, irritability, confusion, however, the intramuscular injection is not may occur gradually; dystonia (abnormal face information if problem arises should be made
available to the patient or the relatives.
depressed mood, aggressiveness, incoordina- needed and patients can be treated with an and body movements) and dyskinesia, which
• The nurse should observe the effects of drug
tion, anterograde amnesia may occur. Rarely, oral dose. Haloperidol may be administered may appear after only a few doses; akathisia treatment and document.
mild increase in liver enzymes, allergic-type in the acute phase. (restlessness), which may occur after large • On discharge, care should be taken not to prescribe
reactions such as rash, urticaria. MAINTENANCE THERAPY initial doses and may resemble an exacerbation excessive quantities of drugs if there is a suicide risk
Advice to patients: May cause drowsiness. of the condition being treated; and tardive
Ability to operate machinery or drive may be Long-term treatment for schizophrenia may dyskinesia (an orofacial dyskinesia), which
be necessary after the first episode to prevent CHLORPROMAZINE
impaired. Avoid alcoholic beverages. See Good usually takes longer to develop but may de-
the manifest illness from becoming chronic. Warning: Owing to the risk of contact sensiti-
Sleep Hygiene in the clinical notes above velop on short-term treatment with low Doses;
The lowest possible dose of antipsychotic drug zation, pharmacists, nurses, and other health
Administration: May be taken with or without short-lived tardive dyskinesia may occur after
EMDEX
that will prevent major exacerbations of florid workers should avoid direct contact with chlor-
meals prior to be bedtime. Swallow whole withdrawal of the drug. Parkinsonian symp-
symptoms is used for long-term management. promazine; tablets should not be crushed and
without sucking, chewing or breaking. toms are usually reversible on withdrawal of
Too rapid a dose reduction should be avoided. solutions should be handled with care
Dose: May be taken with or without food. To the drug and may be suppressed by anticho-
Intramuscular depot preparations such as Indications: Schizophrenia and other psy-
be swallowed whole without sucking, linergic (antimuscarinic) drugs but they may
fluphenazine decanoate may be used as an chotic disorders, mania, psychomotor agita-
chewing or breaking. unmask or worsen tardive dyskinesia. Tardive
alternative to oral maintenance therapy espe- tion and violent behaviour; adjunct in severe
By mouth, Adult, Short-term treatment dyskinesia is usually associated with long-term
cially when compliance with oral treatment is anxiety
of insomnia, Adult, 7.5 mg at bedtime. treatment and high dosage of an antipsychotic,
unreliable. Exacerbations of illness in patients Contra-indications: Impaired consciousness
Elderly, Hepatic & Renal Insufficiency: particularly in elderly patients (see section
on maintenance drug therapy can be precip- due to CNS depression; bone-marrow depres-
Initially, 3.75 mg at bedtime; may be 1.6.2). There is no established treatment for
itated by stress. sion; phaeo-chromocytoma
increased to 7.5 mg daily depending tardive dyskinesias, which may be irreversible
Withdrawal of maintenance drug treatment Precautions: Cardiovascular and cerebrovascu-
on response and tolerance on withdrawing therapy. However, withdrawal
requires careful surveillance since it is not pos- lar disorders, respiratory disease, parkinsonism,
Children (<18 years): Not recom- at the earliest signs of tardive dyskinesia may
sible to predict the course of the disease and epilepsy, acute infections, pregnancy (Appen-
mended halt its full development. Treatment of all pa-
the patient may suffer a relapse if treatment is dix 2), breastfeeding (Appendix 3), renal and
POM Apo-Zopiclone (Lahams)
tients on antipsychotics must be carefully and
withdrawn inappropriately. Further, the need hepatic impairment (avoid if severe; Appen-
Tablet, Zopiclone 7.5 mg; blue, scored film-coated regularly reviewed.
for continuation of treatment may not be dices 4 and 5), history of jaundice, leukopenia
oval tab. marked ‘APO-7.5’. Neuroleptic malignant syndrome (hypo-
evident on withdrawal of treatment because (blood counts if unexplained fever or infection);
7.5 mg - 100’s. thermia, fluctuating levels of consciousness,
relapse may be delayed for several weeks. hypothyroidism, myasthenia gravis, prostatic
muscular rigidity, and autonomic dysfunction
hypertrophy, angle-closure glaucoma; elderly
1.2 Drugs used in psychotic disorders ADVERSE EFFECTS with pallor, tachycardia, labile blood pressure,
(particularly in very hot or very cold weather);
sweating and urinary incontinence) is a rare
Treatment of psychotic disorders is both Adverse effects are very common with long- avoid abrupt withdrawal; patients should re-
adverse effect of haloperidol and chlorprom-
pharmacological and psychosocial. Individual term administration of antipsychotic medicines main supine and the blood pressure monitored
azine. It is managed by discontinuing the
and community programmes for relearning (see under individual drugs). Treatment of all for 30 minutes after intramuscular injection;
antipsychotic, correcting fluid and electrolyte
old skills and developing new ones and for patients on antipsychotics must be carefully interactions: Appendix 1.
defects, and giving bromocriptine and some-
learning to cope with the illness should be and regularly reviewed. Hypotension and Adverse effects: Extrapyramidal symptoms
times dantrolene.
initiated. Classes of antipsychotic drugs include interference with temperature regulation, and on prolonged administration, occasionally
phenothiazines (for example chlorpromazine), neuroleptic malignant syndrome (see below) General points on administration of potentially irreversible tardive dyskinesias (see
butyrophenones (for example haloperidol), drugs to psychiatric patients notes above); hypothermia (occasionally py-
and bone-marrow depression are the most
thioxanthenes (for example flupentixol) and • Two nurses should always be concerned with drug
life-threatening adverse effects of antipsy- rexia), drowsiness, apathy, pallor, nightmares,
administration
newer ‘atypical’ neuroleptics including clozap- chotics. Hypotension and interference with dizziness, excitement, insomnia, headache,
• Patient compliance is an important issue in a
ine and risperidone. The various antipsychotic temperature regulation are dose-related. They psychiatric set up. It is necessary to ensure that confusion, depression; more rarely, agitation,
drugs do not, in general, differ in their antipsy- can result in dangerous falls and hypothermia patients take medication. This is because patient EEG changes, convulsions, nasal congestion;
chotic activity, but differ in range and quality in the elderly and this must be considered may not swallow the drugs only to spit them out anticholinergic symptoms including dry
of adverse effects (see below). before prescribing these drugs for patients when not observed by the nurse. mouth, constipation, blurred vision, difficulty
ACUTE PHASE TREATMENT over 70 years of age. • In the wards, many psychiatric patients are am- in micturition; hypotension, tachycardia and
Extrapyramidal symptoms are the most trou- bulant, so drugs may be administered at a central arrhythmias; ECG changes; respiratory depres-
The administration of chlorpromazine or point and not drug round.
blesome adverse effects of antipsychotics and sion; menstrual disturbances, galactorrhoea,
haloperidol will relieve symptoms such as
gynaecomastia, impotence, weight gain; mania, psychomotor agitation, violent reactions such as acute dystonia; parkinso- cation.
sensitivity reactions such as agranulocytosis, behaviour, and severe anxiety (ad- nian-like side effects and akathisia are rare, • Increase intake of fluids and bulk in diet to avoid
leukopenia, leukocytosis, haemolytic anaemia, junct), by mouth, ADULT initially 25 and no case of tardive dyskinesia has been constipation, especially in elderly.
photosensitization, contact sensitization and mg 3 times daily (or 75 mg at night) reported. Unlike other neuroleptics, clozapine • Offer sips of water or chewing gum for dry mouth.
• Inform patient weekly blood tests is mandatory to
rashes, jaundice and alterations in liver func- adjusted according to response to produces little or no prolactin elevation and
monitor for agranulocytosis; to report sore throat,
tion; neuroleptic malignant syndrome; lupus usual maintenance dose of 75–300 hence, does not have adverse effects such as malaise, fever, bleeding, mouth sores or any other
erythematosus-like syndrome; with prolonged mg daily (but up to 1 g daily may be gynaecomastia, amenorrhoea, galactorrhoea, signs of infection.
high dosage, corneal and lens opacities, and required in psychoses); and impotence. • Advise patient to rise from sitting or lying positions
purplish pigmentation of the skin, cornea and ELDERLY (or debilitated) third to half Indications: Schizophrenia in patients who slowly and to avoid standing still for long periods;
retina; intramuscular injection may be painful adult Dose; are non-responsive to or intolerant of classical to avoid driving or other hazardous activities;
and cause hypotension and tachycardia (see CHILD (childhood schizophrenia and neuroleptic. seizures may occur.
Precautions) and nodule formation. autism) 1–5 years, 500 µg/kg every Contra-indications: Previous hypersensi- • Benign, self-limiting temperature elevations some-
times occur during the first 3 weeks of treatment.
Advice to patients: May cause drowsiness. 4–6 hours (maximum 40 mg daily); tivity to clozapine, history of drug–induced
• Teach patient to avoid OTC preparations (cough
Ability to operate machinery or drive may be 6–12 years, third to half adult dose granulocytopenia/agranulocytosis; impaired or cold remedies), alcohol or CNS depressants;
impaired. Avoid alcoholic beverages. Avoid ex- (maximum 75 mg daily) bone marrow function; uncontrolled epilepsy; not to stop taking medication abruptly because
cessive exposure to sunlight. Avoid rising from For relief of acute symptoms, by deep alcoholic and other toxic psychoses, drug EPS may occur.
sitting or lying position rapidly or engaging in IM injection, ADULT 25–50 mg every intoxication, comatose conditions; circulatory Administration: To be taken with meals; Swallowed
strenous activity. See Good Sleep Hygiene in 6–8 hours; CHILD 500 µg/kg every collapse and/or CNS depression of any causes; whole without sucking, chewing or breaking. in IV,
clinical notes above 6–8 hours (1–5 years, maximum 40 severe hepatic, renal, or cardiac failure; preg- hypotensive crisis posses as a threat as patient are
Nursing action: mg daily; 6–12 years, maximum 75 nancy, breast-feeding. strongly advised to remain in recumbent position
• Give with full glass of water, milk or with food to mg daily) (see also Precautions and Precautions: Before starting treatment, a white prior and 30-60minutes after IV administration. In
EMDEX
reduce GI upset. IM, if irritation occurs at the site of injection, Nor-
Adverse effects) blood cell (WBC) count and a differential blood
• IM injection may sting; give deep IM only in upper mal saline or 2% Procaine should be diluted with
POM Chlorpromazine (WMF 24.1)
must be performed to ensure that only patients further IM doses.
outer quadrant of buttocks and massage slowly to
Tablet, Chlorpromazine HCl 100 mg. with normal leucocyte findings will receive the Dose: By mouth, initially, 12.5 mg 1-2 times
prevent sterile abscess. Avoid SC injection.
• Observe for orthostatic hypotension, especially Oral liquid, Chlorpromazine HCl 25 mg per 5 mL drug. After starting treatment, WBC count must daily on first day (elderly 12.5 mg
with parenteral administration; keep patient su- Injection, Chlorpromazine HCl 25 mg per mL; in be monitored weekly for 18 weeks and there- once daily); followed by 25-50 mg on
pine for 1 hour after IM injection. Teach patient that 2-mL amp. after at least monthly as long as the patient is the second day; increased slowly as
orthostatic hypotension is common, therefore, to POM Chlorpromazine (EDL 27.5) on the drug. Withdraw treatment if leucocyte required by 25-50 mg daily (elderly 25
rise from sitting or lying positions slowly. Tablets, Chlorpromazine HCl 100 mg. count falls below 3000/mm3 and/or the ab- mg) over 2-3 weeks to 300 mg daily
• Supervise ambulation, until patient becomes Oral liquid, Chlorpromazine HCl 25 mg per 5 mL solute neutrophil granulocyte count drops
stabilized on medication.
in divided doses (larger dose at night;
Injection, Chlorpromazine HCl 25 mg per mL; in below 1500/mm3; patients should report any up to 200 mg daily may be given as a
• Relieve dry mouth with chewing gum or sips of 2-mL amp. kind of infection or fever; avoid drugs which
water. single dose at bedtime
POM Chlorpromazine (Kayhelt) depress leucopoiesis; patients with history of Therapeutic dose range for psychotic
• Increase fluid and bulk in diet to prevent consti-
pation; dilute liquid preparations with water, fruit Tablet, Chlorpromazine HCI 100 mg seizures; cardiovascular, renal or hepatic dis- patients, 300-450 mg daily (max. 900
juice or milk before oral administration. orders, reduce Dose (avoid if severe); prostatic mg) in divided doses; maintenance
POM CHLOPROMOX® (Beta Drugs)
• Avoid contact of oral solution or injection with skin enlargement, paralytic ileus and narrow–angle dose, 150-300 mg daily.
Injection, Chlorpromazine HCl 25 mg per mL; in 2
and clothing (contact dermatitis). mL amp.
glaucoma (due to its anticholinergic activity);
• Teach patient not to involve in strenuous exercise avoid in children; avoid abrupt withdrawal. POM CLOPEX® (Reals)
Pack: 2 mL x 10’s. Tablet, Clozapine 50 mg.
or stand still for long periods to avoid fainting. Adverse effects: Granulocytopenia and
• Teach patient not to stop taking drug abruptly POM CLOPROZINE® (Shrezar) 50 mg - 10’s (in strips)
agranulocytosis; fatigue, drowsiness, sedation,
(may cause EPS) unless informed by the physician; Injection, Chlorpromazine HCl 25 mg per mL; in 2 POM LEPONEX® (Novartis)
headache; extrapyramidal symptoms, EEG
to avoid alcohol and other CNS depressants, may mL amp Tablets, Clozapine 25 mg, 100 mg.
Pack: 2 mL x 10’s changes, reduce seizure threshold; dry mouth,
cause increased drowsiness. Antacids can only be
taken 2 hours before or after this drug. blurred vision, hypersalivation; tachycardia
POM MENAX® (Vixa) and postural hypotension (with or without FLUPHENAZINE
• Observe extrapyramidal symptoms of akathisia
Injection, Chlorpromazine HCl 25 mg/mL; in 2 mL syncope); ECG changes rarely cardiac arrhyth-
(inability to sit still and no pattern to movements),
amp. Indications: Maintenance treatment of schiz-
tardive dyskinesia (bizarre movement of the jaw, mias, pericarditis, and myocarditis; respiratory ophrenia and other psychoses
Pack: 2 mL x 10’s.
mouth, tongue, and extremities), pseudoparkin- depression or arrest; GI disturbances, urinary Contra-indications: Children; confusional
sonism (rigidity, tremors, pill rolling and shuffling incontinence and urinary retention; benign states; impaired consciousness due to CNS
gait). CLOZAPINE
hyperthermia; rarely hyperglycaemia and depression; parkinsonism; intolerance to
• Withhold therapy and notify the physician if patient A potentially serious adverse reaction caused by increases in CPK values. antipsychotics; depression; bone-marrow
develops jaundice, symptoms of blood dyscrasias Clozapine therapy is granulocytopenia and agran-
(fever, sore throat, infection, cellulitis, weakness),
Advice to patients: May cause drowsiness. depression; phaeochromocytoma; marked
ulocytosis. In view of this risk, the use of Clozapine Ability to operate machinery or drive may be
persistent extrapyramidal reactions, or any such should be limited to schizophrenic patients who cerebral artherosclerosis.
reactions during pregnancy or in children. impaired. Avoid alcoholic beverages. See Good Precautions: Treatment requires careful
are nonresponsive to or intolerant of conventional
• Advise patient to report urine retention or consti- antipsychotic drug treatment and in whom regular Sleep Hygiene in clinical notes above monitoring for optimum effect; initial small
pation; drug may turn urine pink or red. haematological examinations can be performed. Nursing action: test dose as adverse effects are prolonged;
• Photosensitivity reactions can be prevented with • Ensure patient swallows medication; check for extrapyramidal symptoms occur frequently;
sun screening agents and protective clothing. Pharmacology: Clozapine is unique in that it possible hoarding.
when transferring from oral to depot therapy,
Dose: Schizophrenia and other psychoses, produces virtually no major extrapyramidal • Supervise ambulation until stabilised on medi-
dosage by mouth should be reduced gradually; POM Fluphenazine (EDL 27.5) • Increase fluid intake to prevent constipation and breastfeeding.
cardiovascular and cerebrovascular disorders, Injection, Fluphenazine (as decanoate) 25 mg per give sips of water or chewing gum for dry mouth. Precautions: May exacerbate preexisting di-
respiratory disease, epilepsy, acute infections, mL; in 1-mL amp. • Teach patient not to withdraw drug abruptly to abetes; dyslipidemia. Prostatic hypertrophy,
pregnancy (Appendix 2), breast-feeding (Ap- avoid EPS; to avoid OTC preparations or alcoholic paralytic ileus (has anticholinergic activity).
POM Fluphenazine (Alpha)
beverages and to report impaired vision, jaundice,
pendix 3), renal and hepatic impairment (avoid Injection, Fluphenazine 25 mg per mL; in 1-mL amp. Patients with elevated hepatic transaminases,
tremors, muscle twitching.
if severe; Appendices 4 and 5), history of jaun- POM MODICAT® (Shrezar) • Warn patient to avoid hazardous activities that hepatic impairment or hepatitis (discontinue).
dice, leukopenia (blood counts if unexplained Injection, Fluphenazine (as decanoate) 25 mg per mL require mental alertness and physical coordination, History of blood dyscrasias, myelosuppres-
fever or infection); hypothyroidism, myasthenia Pack: 1 mL x 10’s and to make position changes slowly to avoid sion, seizures or factors which may lower
gravis, prostatic hypertrophy, angle-closure orthostatic hypotension. seizure threshold. Discontinue if neuroleptic
glaucoma; elderly (particularly in very hot or • Observe closely for extrapyramidal symptoms of malignant syndrome occurs. Discontinue or
HALOPERIDOL
very cold weather); interactions: Appendix 1. akathisia, tardive dyskinesia and pseudoparkin- reduce dose if tardive dyskinesia occurs. Co-ad-
Indication: Schizophrenia and other psychotic sonism.
Adverse effects: As for Chlorpromazine ministration with drugs known to increase QTc
disorders, mania, short-term adjunctive man- Dose: Schizophrenia and other psychoses,
Hydrochloride (see above), but less sedating interval esp. in elderly, patients with congenital
agement of psychomotor agitation, violent mania, short-term adjunctive man-
and fewer hypotensive and anticholinergic long QT syndrome, CHF, cardiac hypertrophy,
behaviour, and severe anxiety. agement of psychomotor agitation,
symptoms; higher incidence of extrapyramidal hypokalaemia or hypomagnesaemia. Preg-
Contra-indications: Impaired consciousness violent behaviour, and severe anxiety,
symptoms (most likely to occur a few hours nancy. May cause somnolence and dizziness
due to CNS depression; bonemarrow depres- by mouth, ADULT initially 1.5–3 mg
after injection and continue for about 2 days and therefore may affect ability to drive or
sion; phaeochromocytoma; porphyria; basal 2–3 times daily or 3–5 mg 2–3 times
but may be delayed); systemic lupus erythe- operate machinery. Discontinuation symptoms
ganglia disease. daily in severely affected or resistant
matosus; pain at injection site, occasionally (avoid abrupt withdrawal).
Precautions: Cardiovascular and cerebrovascular patients (up to 30 mg daily in resist-
erythema, swelling, nodules; inappropriate Interactions: Alcohol and other centrally act-
disorders, respiratory disease, parkinsonism, ant schizophrenia); ELDERLY (or debil-
antidiuretic hormone secretion, oedema. ing drugs; may enhance the effects of certain
epilepsy, acute infections, pregnancy (Appen-
EMDEX
Advice to patients: May cause drowsiness. itated) initially half adult dose; CHILD antihypertensive agents; may antogonize the
dix 2), breast-feeding (Appendix 3), renal and initially 25–50 µg/kg daily in 2 divided
Ability to operate machinery or drive may be effects of levodopa and dopamine agonists.
hepatic impairment (avoid if severe; Appendices doses (maximum 10 mg daily).
impaired. Avoid alcoholic beverages. See Good CYP1A2 inducers such as carbamazepine and
4 and 5), history of jaundice, leukopenia (blood Acute psychotic conditions, by IM
Sleep Hygiene in clinical notes above smoking may increase olanzapine clearance.
count required if unexplained fever or infection); injection, ADULT initially 2–10 mg,
Nursing action: CYP1A2 inhibitors such as ciprofloxacin and
• Give injection into large muscle mass; to minimise hypothyroidism, myasthenia gravis, prostatic subsequent doses every 4–8 hours fluvoxamine can inhibit olanzapine clearance.
postural hypotension, give injection and keep hypertrophy, angle-closure glaucoma; also sub- according to response (up to every Charcoal can reduce bioavailability by 50-60%.
patient recumbent or seated for 30 min. arachnoid haemorrhage and metabolic distur- hour if necessary) to total maximum Adverse effects: Weight gain; Elevated plasma
• Use a dry needle (to avoid solution becoming bances such as hypokalaemia, hypocalcaemia, of 18 mg; severely disturbed patients levels of cholesterol, glucose, triglyceride
cloudy) of at least 21G due to the viscosity or hypo-magnesaemia; elderly (particularly in may require initial dose of up to 18
fluphenazine decanoate or enanthate injection,
& prolactin; Glucosuria; Increased appetite.
very hot or very cold weather); children and mg; ELDERLY (or debilitated) initially
which is an oily solution. Somnolence, Dizziness, Akathisia, Parkinson-
adolescents; avoid abrupt withdrawal; patients half adult dose.
• Supervise ambulation until patient is stabilised ism, Dyskinesia. Orthostatic hypotension,
should remain supine and the blood pressure CHILD not recommended.
on medication; patient should not stand for long Bradycardia, QTc prolongation. Mild, transient
monitored for 30 minutes after intramuscular
periods at a time; avoid strenuous activities as POM Haloperidol (WMF 24.1) anticholinergic effects including constipation &
fainting may occur. injection; interactions: Appendix 1.
Tablets, Haloperidol 2 mg, 5 mg. dry mouth. Transient, asymptomatic elevations
• Increase fluid intake to prevent constipation and Adverse effects: As for Chlorpromazine HCl Injection, Haloperidol 5 mg per mL; in 1-mL amp. of hepatic transaminases. Asthenia, Fatigue,
give sips of water or chewing gum for dry mouth. (see above), but less sedating and fewer
POM Haloperidol (EDL 27.5) Oedema. Rash, Photosensitivity reaction,
• Avoid contact of oral solution or injection with skin hypotensive and anticholinergic symptoms;
Tablets, Haloperidol 2 mg, 5 mg. Alopecia. Blood dyscrasias.
(contact dermatitis). pigmentation and photosensitivity reactions
• Teach patient not to withdraw drug abruptly to Injections, Haloperidol 5 mg per mL; in 1-mL amp. Advice to patients: May cause drowsiness.
rare; EPS are common, particularly acute dys-
avoid EPS; to avoid OTC preparations or alcoholic Ability to operate machinery or drive may be
tonia and akathisia (especially in thyrotoxic POM Apo-Haloperidol (Lahams)
beverages and to report sore throat, malaise, fever, Tablets, Haloperidol 5 mg (green, scored bev- impaired. Avoid alcoholic beverages. See Good
patients); rarely weight loss, hypoglycaemia,
bleeding, mouth sores. el-edged tab. marked ‘APO 5’); 10 mg (light green, Sleep Hygiene in clinical notes above
inappropriate antidiuretic hormone secretion.
• Advise patient to report urine retention or consti- scored bevel-edged tab. marked ‘APO 10’). Dose: By mouth, Adult, Schizophrenia, Ini-
pation. Drug may turn urine pink or red. Advice to patients: May cause drowsiness.
5 mg - 1000’s tially, 10 mg/day.
• Photosensitivity reactions can be prevented with Ability to operate machinery or drive may be 10 mg - 500’s. Manic episode (Monotherapy): Initially
sunscreening agents and protective clothing. impaired. Avoid alcoholic beverages. See Good
15 mg as a single daily dose. Combi-
Dose: Maintenance in schizophrenia and other Sleep Hygiene in clinical notes above OLANZAPINE nation therapy: Initially 10 mg daily.
psychoses, by deep IM injection into Nursing action:
Therapeutic category: Atypical antipsychotic Preventing recurrence in bipolar disor-
gluteal muscle, ADULT test Dose of • Give PO with food or milk.
• Give IM inj into large muscle mass using 21G, Indications: Acute & maintenance treatment der, Initially 10 mg/day
12.5 mg (6.25 mg in elderly), then of schizophrenia & other psychoses. Alleviates Note: Daily dosages for schizophrenia, manic ep-
2-in needle; not more than 3 mL per inj site; keep
after 4–7 days 12.5–100 mg repeated secondary affective symptoms commonly isode & recurrence prevention in bipolar disorder
patient lying down for at least 30 min after inj.
at intervals of 2–5 weeks, adjusted • Do not use injection that is markedly discoloured; associated with schizophrenia & related disor- may be individually titrated within the range 5-20
according to response. slight yellowing of injection is common. ders. Treatment of moderate to severe manic
mg/day. Doses >10 mg should be given only after
CHILD not recommended. • Supervise ambulation until patient is stabilised clinical reassessment. Max: 20 mg daily.
episode. Prevention of recurrence in patients
on medication; patient should not stand for long Elderly (>65 years): May use a lower
POM Fluphenazine (WMF 24.1) with bipolar disorder.
periods at a time; avoid strenuous activities as starting dose of 5 mg/day if neces-
Injection, Fluphenazine (as decanoate or enantate) Contra-indications: Hypersensitivity to the
25 mg per mL; in 1-mL amp. fainting may occur. sary.
olanzapine; Narrow-angle glaucoma; Avoid
Children & adolescents (<18 years): activity and notify the doctor. chewing gum for dry mouth. 4 mg - 3 x 10’s
Not recommended. • Pimozide should be reserved for cases where other • Warn patient to avoid hazardous activities if drowsy
POM RISPERDAL® (Janssen-Cilag)
Administration: May be given with or without agents have failed because it may cause serious or dizzy, and to make position changes slowly to
Tablets, Risperidone 1 mg, white oblong tab.; 2 mg,
food; absorption not affected by food. Avoid abrupt adverse effects; patient and his family should be avoid orthostatic hypotension.
pale orange oblong tab.; 3 mg, yellow oblong tab.;
discontinuation; gradually taper dose. well informed before commencement of therapy. • Teach patient not to stop taking drug abruptly,
4 mg, green oblong tab.
• Observe closely for extrapyramidal symptoms of may cause EPS; to avoid alcohol and other CNS de-
POM LANZEP® (Pharmabase) 1 mg - 6.
akathisia, tardive dyskinesia and pseudoparkin- pressants which may cause increased drowsiness.
Tablets, Olanzepine 5 mg (yellow tab.), 10 mg (sunset 2 mg - 20.
sonism. • Monitor and observe for extrapyramidial effects,
yellow tab.); both f-c tabs. 3 mg - 20.
Dose: Adult and child (above 12 years), by orthostatic blood pressure changes for 3-5 days
Pack: 3 x 10’s (in blisters) after starting or increasing dose. POM Risperidon Sandoz (Novartis)
mouth, initially 1-2 mg daily; then
POM OLANZA® (PharmacyPlus) increased as needed every other day Dose: By mouth, Adult and child >15 years, Tablet, Risperidone 1 mg; white, oval f-c tab
Tablets, Olanzepine 5 mg, 10 mg; f-c tab to 7-16 mg daily. Max. dose: 20 mg initially 1 mg twice daily; increased to Pack: 20’s; 50’s; 100’s
5 mg - 1 x 14’s; 2 x 14’s daily or 0.3 mg/kg b.wt. daily. 2 mg twice daily on Day 2 and 3 mg
10 mg - 1 x 14’s; 2 x 14’s twice daily on Day 3. THIORIDAZINE
POM Pimozide (EDL 27.3.2/Restricted List)
POM OLEANZ® (Synergy) Maintenance dose: 2-4 mg twice daily Therapeutic category: Antipsychotic/Anx-
Tablets, Pimozide 4 mg, 10 mg.
Tablets, Olanzapine 2.5 mg, 5 mg, 7.5 mg, 10 mg; (max.: 8 mg twice daily). Doses >5 mg iolytic.
f-c tabs. twice daily may increase the risk of Pharmacology: Thioridazine is used as a
RISPERIDONE
2.5 mg - 10’s EPS and may only be used if benefit sedative especially in the elderly due to its low
5 mg - 10’s Therapeutic category: Antipsychotic Agent considered to outweigh risk. propensity to cause extrapyramidal side–ef-
7.5 mg - 10’s Indications: Acute and chronic schizophrenia, Elderly, Patients with renal and liver fects. At medium and high doses, thioridazine
10 mg - 10’s and other psychotic conditions, in which posi- disease, initially, 0.5 mg twice daily; is effective in controlling severe symptoms of
POM PREXAL® (Joswe/Afrab) tive and/or negative symptoms are prominent; individually adjusted with 0.5 mg psychotic and non–psychotic mental disorder.
EMDEX
Caplets, Olanzapine 5 mg, 10 mg; f-c caplets. also alleviates affective symptoms associated twice daily increments to 1-2 mg It has a strong atropine-like action. Retinal
Pack: 30’s. with schizophrenia. twice daily. damage may occur in high dosage.
Contra-indications: Known hypersensitivity to Not recommended in child <15 yrs. Indications: Schizophrenia and related psy-
POM REXOLAN® (Fidson)
risperidone; breast-feeding; children <15 years. choses, tranquillisation and emergency control
Tablets, Olanzapine 5 mg, 7.5 mg, 10 mg; f-c tabs. POM AMIDREX® (Pharmabase)
Pack: 3 x 10’s. Precautions: Orthostatic hypotension (al- in behaviour disturbances, agitation in elderly
pha-blocking effect); cardiovascular disease; Tablets, Risperidone 1 mg, 2 mg; f-c tabs.
1 mg - 3 x10’s patients, short-term adjunctive treatment of
PIMOZIDE hypotension (reduce Dose); high Dose may severe anxiety.
2 mg - 3 x 10’s
cause tardive dyskinesia (give a benzodiaze- Contra-indications: Comatose states or severe
Therapeutic category: Neuroleptic Agent POM RESICALM® (Phillips)
pine for more sedation instead of increasing depression of the CNS; history of hypersensi-
Pharmacology: Pimozide is a long–acting and Tablet, Risperidone 0.5 mg; green f-c oval scored
Dose); Parkinson’s disease or epilepsy; weight tivity to other ‘phenothiazines’ and of blood
potent antipsychotic with more selective do- tab. marked “A” on one side and “50” on the reverse.
gain; mental alertness may be impaired; he- dyscrasia; severe cardiovascular disease, chil-
pamine receptor blocker than chlorpromazine 0.5 mg - 10’s.
patic and renal impairment; pregnancy. dren <1 year of age.
and, therefore, is less sedative. Tablet, Risperidone 1 mg; white f-c oval scored tab.
Adverse effects: Insomnia, agitation, anxiety, Precautions: Narrow-angle glaucoma, pros-
Indications: Suppression of severe motor and marked “A” on one side and “51” on the reverse.
headache; somnolence, fatigue, dizziness, 1 mg - 10’s. tatic hypertrophy, cardiovascular disease; road
phonic tics in patients with Tourette’s disorder.
impaired concentration, constipation, dys- Tablet, Risperidone 2 mg; light-orange f-c oval scored users; liver disease; pregnancy, breast-feeding.
Contra-indications, Precautions, Adverse
pepsia, nausea, abdominal pain, blurred tab. marked “A” on one side and “52” on the reverse. Adverse effects: Nausea, sedation; anticho-
effects: See under Chlorpromazine.
vision, erectile dysfunction, ejaculatory dys- 2 mg - 10’s.
linergic effects such as nasal stuffiness, dry
Advice to patients: May cause drowsiness. Tablet, Risperidone 3 mg; yellow f-c oval scored
function, orgasmic dysfunction, rhinitis, rash; mouth; allergic skin reactions; neuroleptic
Ability to operate machinery or drive may be tab. marked “A” on one side and “53” on the reverse.
low incidence and severity of extra pyramidal malignant syndrome such as muscular rigidity -
impaired. Avoid alcoholic beverages. See Good 3 mg - 10’s.
symptoms (reversible upon Dose reduction discontinue the drug; jaundice, weight change,
Sleep Hygiene in clinical notes above. Since Tablet, Risperidone 4 mg; green f-c oval scored tab.
and/or administration of antiparkinson drug); hyperthermia.
Pimozide may cause serious adverse effects, marked “A” on one side and “54” on the reverse.
rarely neuroleptic malignant syndrome 4 mg - 10’s. Advice to patients: May cause drowsiness.
the patient and his family should be thoroughly
(discontinue all antipsychotic medication); Tablet, Risperidone 6 mg; white f-c oval scored tab. Ability to operate machinery or drive may be
informed before a decision is taken, to or not
occasionally orthostatic dizziness, orthostatic marked “A” on one side and “56” on the reverse. impaired. Avoid alcoholic beverages. Avoid
to, take the drug.
hypotension and reflex tachycardia (especially 6 mg - 10’s. excessive exposure to sunlight. See Good Sleep
Nursing action:
• Supervise ambulation until patient becomes sta- with high initial Doses); hyperprolactinaemia POM RESPAL® (Joswe/Afrab) Hygiene in clinical notes above
bilized on medicadtion. (with galactorrhoea, menstrual disturbances, Tablets, Risperidone 2 mg, 4 mg; f-c tabs. Nursing action:
• Give sips of water or chewing gum to relieve dry amenorrhoea, gynaecomastia); rarely water Pack: 20’s • Dilute liquid preparations with water or fruit juice
mouth. intoxication with hyponatraemia and seizures. just before giving.
POM RESPIDOZ® (Zoomota)
• Advise patient not to involve in strenous exercise Advise to patients: Ability to drive or operate • Keep patient lying down for at least 30 min after
Tablet , (2 mg), Risperidone 2 mg; peach tab.
to avoid fainting. machinery may be impaired. IM inj.
2 mg - 3 x 10’s (in blisters).
• Warn patient to avoid abrupt discontinuation of Nursing action: • Supervise ambulation until patient is stabilised
Tablet , (3 mg), Risperidone 3 mg; yellow tab.
therapy and not to exceed the prescribed dose. • Supervise ambulation until patient is stabilised on medication; patient should not stand for long
• ECG examination before and periodically during on medication; patient should not stand for long periods at a time; avoid strenuous activities as
therapy is recommended; monitor for prolongd periods at a time; avoid strenuous activities as POM RISDONE® (Reals) fainting may occur.
Q-T interval. fainting may occur. Tablet, Risperidone 1 mg, 2 mg, 4 mg; uncoated tabs. • Increase fluid/bulk intake to prevent constipation;
• Pimozide may lower the seizure threshold; monitor • Increase bulk and fluid in diet if constipation or 1 mg - 3 x 10’s give sips of water or chewing gum for dry mouth.
patient on anticonvulsants for increased seizure urinary retention occurs; offer sips of water or 2 mg - 3 x 10’s • Warn patient to avoid hazardous activities if drowsy
40 | 1.3 Antidotes to antipsychotic drugs 1.4 Drugs used in mood disorders | 41
or dizzy, and to rise from sitting or lying positions seizure threshold). Narrow angle glaucoma, • Dystonic reactions involve an acute spasm of tonic reaction does not respond. For pseudo-
slowly to avoid orthostatic hypotension. myasthenia gravis or prostatic hypertrophy muscle group. The high-potency neuroleptic parkinsonism and akathisia, oral benztropine
• Teach patient not to withdraw drug abruptly to (has weak anticholinergic effects). Renal & he- drugs, such as fluphenazine and haloperidol, 1–2 mg twice daily or benzhexol 2 mg three or
avoid EPS; to avoid OTC preparations or alcoholic patic impairment, diabetes, phaeochromocy- are more likely to cause dystonic reactions than four times daily represent usual starting doses,
beverages and to report sore throat, malaise, fever, the low–potency drugs such as thioridazine and
toma. May impair temp. regulatory mechanism. with the maximum Doses usually being 6 mg
bleeding, mouth sores. chlorpromazine. Usually brief and most responsive
• Avoid contact of liquid preparations with skin and Interactions: As with other antipsychotic to treatment. and 15 mg respectively. Occasionally, some
clothing to prevent contact dermatitis; wear glove drugs, may potentiate CNS depressant effects • Pseudoparkinsonism resembles Parkinson’s dis- patients may require up to 8 mg of benztropine
when diluting liquid dosage forms. of alcohol, hypnotics, opioids or other anal- ease and is of two forms, akinesia and tremor. It is or 20 mg of benzhexol daily, but peripheral
• Photosensitivity reactions can be prevented with gesics. May enhance anticholinergic effects more commonly seen in the elderly, is more likely anticholinergic effects become troublesome
sunscreening agents and protective clothing. of TCA, antiparkinsonian drugs. Antagonised to be caused by the low–potency neuroleptic at these doses.
Dose: Adult, 25-600 mg daily depending on effects of dopaminergic drugs such as lev- drugs, and is generally responsive to treatment.
Anticholinergic prophylaxis (as adjunctive
the indication; up to a max. 800 mg odopa. Reverses antihypertensive effect of • Akathisia is often difficult to distinguish from
psychotic agitation; this can result in the neuro- treatment to neuroleptic therapy) is justified
daily. guanethidine. Lithium (enhanced extrapyram- when the patient has a history of EPS or is
leptic Dose being increased, thus worsening the
Child (1 year and above), 1-4 mg/kg idal side-effects). Antacids. given a high–potency neuroleptic. Prophylaxis
akathisia. It is the most common and troublesome
body-wt. daily. See lit. for details. Adverse effects: Drowsiness, sedation, an- of all EPS, and is caused more by the high potency is not indicated when low–potency neuroleptic
POM APO-THIORIDAZINE® (Lahams) ticholinergic effects (dry mouth, constipation), neuroleptic drugs. drugs are given or when the neuroleptic dose
Tablet, Thioridazine HCl 100 mg; dark green, f-c tab. insomnia, depression, convulsion, agitation, is very low.
Tardive dyskinesia is a late–appearing effect
marked ‘100’ tachycardia, postural hypotension, impaired
that looks like an EPS but in aetiology and The duration of anticholinergic prophylaxis
100 mg - 100 glucose tolerance, akathisia, muscle weakness,
treatment is opposite to EPS. It typically ap- depends on the dose and potency of the neu-
POM THIORIL® (Hovid) anorexia, rash, amenorrhoea, fatigue, increased
pears upon neuroleptic Dose reduction or dis- roleptic drug as well as on the patient response.
Tablets, Thioridazine HCl 25 mg, 100 mg; f-c tabs. prolactin levels, extrapyramidal side effects.
continuation, improves when the neuroleptic
EMDEX
Advice to patients: May cause drowsiness. After about 3 months, the anticholinergic drug
25 mg - 1000 Dose is increased, worsens with administration
100 mg - 1000. Ability to operate machinery or drive may be dose should be reduced gradually, and if no
of anticholinergic drugs, and may persist for EPS recur, the drug should be discontinued.
impaired. Avoid alcoholic beverages. Avoid
months or years after neuroleptic drugs are
TRIFLUOPERAZINE excessive exposure to sunlight. See Good Sleep
discontinued. BENZHEXOL
Therapeutic category: Antipsychotic; Anxio- Hygiene in clinical notes above
lytic; Anti-emetic. Dose: By mouth, Adult, Schizophrenia, 2-5 Anticholinergic Drugs Used in EPS: Ben- See under Section 1.6.1
Pharmacology: Trifluoperazine, a piperazine mg twice daily; may be incereased zhexol, Benztropine and Biperiden are all
phenothiazine tranquilliser, inhibits dopamine to 15 mg daily after a week. Further anticholinergic drugs used in the treatment of
EPS but not tardive dyskinesia (see notes above); BIPERIDEN
D2 receptors in the brain. It has weak anticho- increases of 5 mg may be made at
linergic, hypotensive and sedative effects but intervals of >3 days if necessary benztropine has also antihistaminic properties. See under Section 1.6.1
strong extrapyramidal and antiemetic effects. Child: Initially, max. 5 mg daily in Benzhexol (trihexyphenidyl) and benztropine
It controls severely disturbed, agitated or divided doses; may be increased at in- are two most commonly used drugs. They are 1.4 Drugs used in mood disorders
violent behaviour but may also be used for tervals of >3 days based on age, body equal in efficacy and adverse effects, but three
weight and severity of symptoms. differences should be noted: 1.4.1 Drugs used in depressive disorders
nonpsychotic anxiety.
Anxiety, Nausea and Vomiting, Adult, • Both are available as 2 mg tablets, but benztropine 1.4.2 Drugs used in bipolar disorders
Indications: At high dosage, for the treat-
ment of symptoms and prevention of relapse 1-2 mg twice daily; may be increased is twice as potent as benzhexol. Mood disorders can be classified as depression
in schizophrenia and in other psychoses, to max. 6 mg daily according to the • The duration of effect of benztropine is longer (unipolar disorder) and mania; alternating
severity of the symptoms. Short-term than benzhexol, allowing benztropine to be Dosed episodes of mania and depression (manic de-
especially of the paranoid type, but not in
use in anxiety not exceeding 12 once daily or at most twice daily. Benzhexol must pression) are termed bipolar disorder.
depressive psychoses; also as an adjunct in be Dosed at least three times daily. When benztro-
the short term management of severe psycho- weeks. Electroconvulsive therapy (ECT) has been
pine is given once daily, it should be given in the
motor agitation and of dangerously impulsive Child: 3-5 yr: max 1 mg daily in morning. Bedtime dosing is of no value since the shown to be rapidly effective in the urgent
behaviour, for example, mental subnormality. divided doses; 6-12 yr: max 4 mg daily extrapyramidal tracts shut down during sleep and treatment of severe depression. Counselling
At low dosage, as an adjunct in the short term in divided doses. EPS is not present during the night. and psychotherapy have an important role in
management of anxiety states, depressive Elderly: Genrally, reduce initial dose • Benzhexol, unlike benztropine, is subject to abuse treating some forms of depression.
symptoms secondary to anxiety, and agitation; by about half and increase gradually. since it may cause euphoria along with other
also indicated in the symptomatic treatment of POM Apo-Trifluoperazine (Lahams)
possible CNS intoxication symptoms including 1.4.1 Drugs used in depressive
confusion, delirium, and psychosis Biperiden is disorders
nausea and vomiting. Tablet, Trifluoperazine HCl 5 mg; deep blue, film- rarely used, but is virtually identical to benzhexol.
Contra-indications: Comatose states; bone coated tab. marked ‘5’. Tricyclic and related antidepressants and
marrow depression, blood dyscrasias, severe 5 mg - 1000’s. Parenteral anticholinergic drugs such as selective serotonin reuptake inhibitors (SSRIs)
liver disease, hypersensitivity to phenothi- benztropine or biperiden are used only for are the most widely used drugs in the treat-
azines, prolactin dependent tumours. Preg- 1.3 Antidotes to antipsychotic drugs acute dystonic reactions and for single dose ment of depressive disorders. The response to
nancy (1st trimester), lactation. treatments for other EPS to determine if the antidepressant therapy is usually delayed with
Extrapyramidal symptoms (EPS) are the most
Precautions: Elderly (reduce initial dose by symptoms are drug responsive. Benztropine a lag period of up to two weeks and at least six
important adverse effect in terms of frequency
about half ). CVD including arrhythmias. May 2 mg IM will exert its effect within 20 mins, weeks before maximum improvement occurs.
and the reason for patient’s non–compliance
worsen Parkinson’s disease and effects of lev- while the effect of IV administration will be It is important to use doses that are sufficiently
with neuroleptic therapy. There are three
odopa may be reversed. Epilepsy (may lower apparent within a few minutes. A second IM high for effective treatment, but not so high
categories of EPS:
dose after 20-30 mins is appropriate if the dys-
42 | 1.4.1 Drugs used in depressive disorders 1.4.1 Drugs used in depressive disorders | 43
as to cause toxic effects. Low doses should be SSRIs may increase suicidal ideation, especially hypomania or mania, confusion or delirium the initial phase and as maintenance against
used for initial treatment in the elderly. The use in children and adolescents. (particularly in elderly), headache, interference potential relapse/recurrence; panic disorder
of more than one antidepressant at a time is Selective Serotonin Reuptake Inhibitors (SSRIs) with sexual function, blood sugar changes; with or without agoraphobia.
not recommended since this does not enhance include citalopram, fluoxetine, fluvoxamine, increased appetite and weight gain (occasional Contra-indications, Precautions, Adverse ef-
effectiveness and it may result in enhanced paroxetine, sertraline. weight loss); endocrine adverse effects such fects, Nursing action, and Advice to patients
adverse effects or interactions. Nursing action: as testicular enlargement, gynaecomastia and See under fluoxetine.
Patients should be reviewed every 1–2 weeks • Antidepressants galactorrhoea; convulsions, movement disorders Dose: To be taken as a single daily dose with
at the start of treatment. Treatment should be • Give with food or milk to reduce GI upset; may and dyskinesias, dysarthria, paraesthesia, taste or without food.
continued for at least 4 weeks (6 weeks in the increase fluid intake (if urinary retention occurs) distrubances, tinnitus, fever, agranulocytosis, By mouth, Adult, Initially 20 mg once
elderly) before considering whether to change or bulk in diet (if constipation occurs), especially leukopenia, eosinophilia, purpura, thrombo- daily; may gradually increase dose af-
to another antidepressant due to lack of effi- in children and elderly. cytopenia, hyponatraemia (may be due to ter 3-4 weeks depending on patient’s
• Ensure patient swallows PO medication; may crush
cacy. In the case of a partial response, treat- inappropriate antidiuretic hormone secretion); response and tolerance (Max: 60 mg
the medication if patient cannot swallow.
ment may be continued for a further 2 weeks • Relieve dry mouth with gum, hard candy or fre-
abnormal liver function test In overdose (high daily
(elderly patients may take longer to respond). quent sips of water. rate of fatality—see notes above), excitement, Counsel patient that initial improve-
Remission usually occurs after 3–12 months. • Assist with ambulation, raise side rails as safety restlessness, marked anticholinergic effects; ment may only be noticable from 2nd
Treatment at full therapeutic dose should be measures particularly in the elderly as drowsiness, severe symptoms including unconsciousness, week of continuous treatment. Min.
continued for at least 6 months, but preferably dizziness may occur. convulsions, myoclonus, hyperreflexia, hypoten- treatment duration: 6 months.
up to 12 months after resolution of symptoms • May increase appetite; observe weight changes. sion, acidosis, respiratory and cardiac depression Elderly (>65 years): 20 mg once daily;
(about 12 months in the elderly). Treatment • Monitor all relevant parameters: BP, blood, liver with arrhythmias. may be increased to a max. 40 mg
should not be withdrawn prematurely oth- and mental status. Advice to patients: May cause drowsiness. daily.
• Observe for EPS (rigidity, dystonia, akathisia) par-
erwise symptoms are likely to recur. Patients Ability to operate machinery or drive may be Children and adolescents (<18 years
ticularly in the elderly.
EMDEX
with a history of recurrent depression should • Inform patient that therapeutic effect may take impaired. Avoid alcoholic beverages. of age): Not recommended
continue to receive maintenance treatment 2-3 weeks. Nursing action: see notes above Hepatic impairment: use lower end of
(for at least 5 years and possibly indefinitely). • Warn patient that drug may cause drowsiness, diz- Dose: Depression, by mouth , ADULT initially the dose range.
Lithium may be used as an alternative for ziness, blurred vision; driving or other activities re- 75 mg (elderly and adolescents 30–75 Administration: May administer without regards
maintenance treatment (see section 1.4.2). The quiring alertness should be avoided. Patient should mg) daily in divided doses or as a to meals
dose should be reduced gradually over about also avoid alcohol and other CNS depressants. single dose at bedtime increased Note: In panic disorder, a lower initial starting dose
• Advise patient not to discontinue drug abruptly (10 mg/day) is recommended to minimise the
4 weeks—longer if withdrawal symptoms gradually as necessary to 150–200
after long-term use; may cause withdrawal symp- potential worsening of panic symptoms, which is
emerge (6 months in patients who have been mg daily; CHILD under 16 years not generally recognised to occur early in the treatment
toms including nausea, headache, malaise.
on long-term maintenance treatment). recommended for depression. of this disorder.
Tricyclic and related antidepressants can be Administration: May administer with or without
AMITRIPTYLINE Withdrawal symptoms: Discontinuation of
divided into those with more or less sedative meals. the total daily dose can be given at bedtime
Thearpeutic category: Tricyclic antidepressant because of its sedative effects. for minority of
citalopram should be gradual over a period of
effect. Those with sedative properties include at least 1-2 weeks in order to reduce the risk
amitriptyline and those with less sedative Indications: Moderate to severe depression. patients who experience difficulty sleeping with
Contra-indications: Recent myocardial in- bedtime dosing, the dose should be given in the of withdrawal reactions (namely dizziness,
effects include imipramine. These drugs are morning. sensory disturbances, sleep disturbances,
most effective in the treatment of depression farction, arrhythmias (especially heart block);
manic phase in bipolar disorders; severe liver agitation or anxiety, nausea and/or vomiting,
associated with psychomotor and physiolog- POM Amitriptyline (WMF 24.2.1)
disease; children; porphyria. Tablet, Amitriptyline HCl 25 mg.
tremor and headache). If withdrawal symptoms
ical disturbances. Adverse effects include an- occur following a decrease in the dose or upon
ticholinergic (more correctly amtimuscarinic) Precautions: Cardiac disease (see Contra-indi- POM Amitriptyline (EDL 27.3.1)
cations above), history of epilepsy; pregnancy discontinuation of treatment, previously pre-
symptoms of dry mouth, blurred vision, consti- Tablet, Amitriptyline HCl 25 mg. scribed dose may be reinstated followed by a
pation and urinary retention. Arrhythmias and (Appendix 2); breastfeeding (Appendix 3);
elderly; hepatic impairment (Appendix 5); POM Amitriptyline (Kakaki). more gradual decrease in dose.
heart block can occur. Minimal quantities of Tablet, Amitriptyline 25 mg
tricyclic antidepressants should be prescribed thyroid disease; phaeo-chromocytoma; history POM LECITAL® (Joswe/Afrab)
25 mg - 28’s; 500’s
of mania, psychoses (may aggravate psychotic Tablet , (20 mg), Citalopram (as HBr) 20 mg.
at any one time because their cardiovascular
symptoms); angle-closure glaucoma, history POM Amitriptyline (Kayhelt) 20 mg - 30’s (in blister).
effects are dangerous in overdose. Amitripty- Tablet, Amitriptyline HCI 25 mg; f-c tab Tablet , (40 mg), Citalopram (as HBr) 40 mg.
line in overdosage is associated with a high of urinary retention; concurrent ECT; avoid
25 mg - 10’s 40 mg - 30’s (in blister).
rate of fatality. abrupt withdrawal; anaesthesia (increased risk
Syrup, Citalopram (as HBr) 10 mg per 5 mL.
The SSRIs include fluoxetine. They characteris- of arrhythmias and hypotension); interactions: POM Apo-Amitriptyline (Lahams)
Pack: 120 mL amber glass bottle.
Appendix 1. Tablets, Amitriptyline HCl 25 mg (yellow f-c tab.
tically cause gastrointestinal disturbances,
Adverse effects: Sedation, dry mouth, blurred marked ‘25’); 50 mg (brown f-c tab. marked ‘50’).
sleep disturbances and hypersensitivity Pack: 1000’s.
ESCITALOPRAM
reactions including rash (may be a sign of an vision (disturbance of accommodation, increased
Therapeutic category: Antidepressant, SSRI.
impending serious systemic reaction and dis- intra-ocular pressure), constipation, nausea, POM TRIPTEX® (Chanmedi)
Pharmacology: Escitalopram is a potent
continuation should be considered) but they difficulty in micturition; cardiovascular adverse Tablet, Amitriptyline 25 mg.
25 mg - 1000’s. selective serotonin reuptake inhibitor (SSRI).
are less sedating and have fewer anticholin- effects particularly with high dosage including
It is the active isomer of citaloprram. Absorp-
ergic (antimuscarinic) and cardiotoxic effects ECG changes, arrhythmias, postural hypoten-
CITALOPRAM tion is almost complete and independent of
than tricyclic antidepressants. The SSRIs are sion, tachycardia, syncope; sweating, tremor,
food intake with a mean Tmax of 4 hours after
less toxic in overdose than the older tricyclic rash and hypersensitivity reactions (urticaria, Therapeutic category: Antidepressant, SSRI.
multiple dosing. As with racemic citalopram,
compounds, but there is some concern that photosensitivity); behavioural disturbances; Indications: Treatment of depressive illness in
the absolute bio-availability of escitalopram is difficulty in sleeping, drowsiness, dry mouth, fe- POM CITANEW® (CG Biostadt) WITHDRAWAL: Dizziness, nausea, anxiety,
about 80%. Escitalopram is metabolised in the ver, sinusitis, headache, increased or decreased Tablets, Escitalopram (as oxalate) 5 mg, 10 mg, 20 headaches, paraesthesia, sleep disturbances,
liver to the demethylated and didemethylated appetite, increased sweating, sexual difficulties mg; f-c tabs. fatigue, agitation, tremor, and sweating may
metabolites, both of which are active. Biotrans- like decreased sexual ability or libido & ejacula- 5 mg - 14’s occur if withdrawn abruptly.
10 mg - 14’s
formation of escitalopram to the demethylated tory delay, change in taste, tremor and weight POM Fluoxetine (WMF 24.2.1)
20 mg - 14’s
metabolite is mediated primarily by CYP2C19. changes. Rarely visual disturbance, confusion, Tablet or Capsule, Fluoxetine (as HCl) 20 mg
Elimination is by both the hepatic (metabolic) agitation, skin rash, itching, suicidal thoughts, POM Escitalopram (Kayhelt)
and the renal routes. vomiting. Tablet, Escitalopram (as oxalate) 10 mg; f-c tab. POM Fluoxetine (EDL 27.3.1)
10 mg - 1 x 10’s (in blisters) Capsule, Fluoxetine 20 mg.
Indications: Major depressive episodes; panic Dose: Administer as a single daily dose, with
disorder with or without agoraphobia; social or without food. POM FLUTEX® (Fidson)
FLUOXETINE Capsule, Fluoxetine (as HCl) 20 mg.
anxiety disorder (social phobia); generalised By mouth, Adult, Major depressive
anxiety disorder; obsessive-compulsive dis- episodes, Usually 10 mg once daily; Therapeutic category: SSRI, antidepressant 20 mg - 10’s (in blister).
order. may increase to a max. 20 mg daily Indications: Moderate to severe major de-
Contra-indications: Concomitant treatment depending on patient response. pression IMIPRAMINE
with or within 2 weeks of withdrawal of Usually 2-4 weeks are necessary to Contra-indications: Manic phase Therapeutic category: Tricyclic antidepressant
MAO-inhibitors due to the risk of serotonin obtain antidepressant response. After Precautions: Epilepsy, cardiac disease, bleed- Indications: Depressive states of varying aeti-
syndrome with agitation, tremor, hyperther- the symptoms resolve, treatment ing disorders, diabetes mellitus, susceptibility ology and symptomatology including masked
mia etc. for at least 6 months is required for to angle-closure glaucoma; history of mania forms; panic attacks; chronic painful condi-
Precautions: Children and adolescents <18 consolidation of the response. (discontinue if patient entering manic phase); tions; Pavor nocturnus, nocturnal enuresis.
years; seizures or history of seizures; history Panic disorder with or without agora- concurrent ECT (prolonged seizures reported); Contra-indications: Hypersensitivity to tri-
of mania/hypomania; sucidal or history of phobia, initially 5 mg daily for the first pregnancy (Appendix 2); breastfeeding (Ap- cyclic antidepressants of the dibenzazepine
EMDEX
suicide-related events; co-administration week; then increase to 10 mg daily. pendix 3); hepatic impairment (Appendix 5); group; acute stage of myocardial infarction; hy-
with other serotonergic agents; St. John’s Max. 20 mg daily avoid abrupt withdrawal; children and adoles- persensitivity to sulphites in parenteral admin.
wort; avoid abrupt discontinuation; he- Maximum effectiveness is reached cents (increased risk of suicide); interactions: Precautions: CV disturbances, AV block
patic and renal impairment; may impair ability after about 3 months. The treatment Appendix 1. (grades I - III); narrow-angle glaucoma, distur-
to drive or operate machinery; pregnancy, lasts several months. Adverse effects: GI disturbances, anorexia with bances of micturition, lowered convulsion thresh-
lactation.Avoid combinations with irreversible Social anxiety disorder, Usually 10 mg weight loss, postural hypotension, pharyngitis, old, electro-convulsion therapy, severe hepatic or
non-selective MAOIs e.g. phenelzine; reversible once daily; may adjust dose after 2-4 dyspnoea, headache, sleep disturbances, renal damage, tumours of the adrenal medulla,
selective MAO-A inhibitor e.g. moclobem- weeks as needed. Max. 20 mg daily. dizziness, ataxia, tremor, convulsions (consider hyperthyroidism or concomitant treatment
ide; reversible non-selective MAO-inhibitor Social anxiety disorder is a disease discontinuation), altered blood glucose control with thyroid preparations; risk of suicide; sur-
e.g. linezolid; irreversible selective MAO-B with a chronic course, and treatment in people with diabetes, taste disturbances, gical intervention; pregnancy, breast-feeding;
inhibitor e.g. selegiline. Increased risk of for 12 weeks is recommended to urinary retention and frequency, sexual dysfunc- road users; blood count, hepatic and renal
serotonin syndrome with other serotonergic consolidate response. tion, galactorrhoea, arthralgia, myalgia, visual function tests during long-term therapy.
agents e.g. tramadol, sumatriptan and other Generalised anxiety disorder, Initially disturbances, photosensitivity, chills, increased Adverse effects: Anticholinergic or mild CNS
triptans. Increased risk of seizure with other 10 mg once daily; may increase up to sweating, dry mouth, alopecia, rash (may be effects; sinus tachycardia, postural hypoten-
medications that can lower seizure threshold a max. 20 mg daily. sign of serious systemic reaction—consider dis- sion; Occasionally, disturbances of micturition,
e.g. antidepressants (tricyclics, SSRIs), neuro- Obsessive-compulsive disorder, Initially continuation), urticaria, angioedema, vasculitis, mania or hypomania, symptoms of delirium,
leptics (phenothiazines, thioxanthenes and 10 mg once daily; may increase up to anaphylaxis; yawning, idiosyncratic hepatitis, activation of psychotic symptoms, arrhythmias,
butyrophenones), mefloquine, bupropion and a max. 20 mg daily pulmonary fibrosis, restleness, akathisia, hal- conduction disorders, allergic skin reactions;
tramadol. Increased risk of bleeding when Elderly (>65 years of age): Half the lucinations, manic reactions, confusion, agita- blood dyscrasias, hepatitis.
used with drugs that affect coagulation e.g. usually recommended dose tion, anxiety, depersonalisation, panic attacks, Advice to patients and Nursing action: See
aspirin, NSAIDs, oral anticoagulants. Increased Children and adolescents (<18 years): suicidal ideation, hyponatraemia, movement under Amitriptyline.
drowsiness with alcohol; Lithium, tryptophan, Not recommended. disorders and dyskinesias, bleeding disorders Dose: By mouth, Adult, initially 25-75 mg
St. John’s wort. Renal dysfunction: No dosage including ecchymosis; serotonin syndrome, daily for out-patients and 75 mg daily
Serum levels may be reduced by CYP2C19 adjustment in mild or moderate renal eythema multiforme leading to Stevens-John- for hospitalised patients: increased
inducers (e.g. carbamazepine, rifampin, impairment. son syndrome or toxic epidermal necrolysis stepwise to 150-200 mg daily. Mainte-
phenytoin). Serum levels may be increased Reduced hepatic function: Initially also reported. nance, 50-100 mg daily.
by CYP2C19 inhibitors (e.g. omeprazole, 5 mg daily for the first two weeks in Advice to patients: May cause drowsiness. Elderly and children: initially, 10 mg
esomeprazole, fluvoxamine, lansoprazole, mild or moderate hepatic impair- Ability to operate machinery or drive may be daily. See lit. for details.
ticlopidine or cimetidine). Escitalopram is ment. Not more than 10 mg per day. impaired. Avoid alcoholic beverages.
POM Apo-Imipramine (Lahams)
CYP2D6 inhibitor and may cause increased Note: Avoid abrupt discontinuation. Gradually Dose: Depression, by mouth, ADULT initially Tablet, Imipramine HCl 25 mg; light-brown f-c tab.
serum levels of drugs metabolised by this reduce dose over a period of at least one to two 20 mg once daily increased as nec- marked ‘25’.
enzyme e.g. flecainide, propafenone and weeks in order to reduce the risk of discontinuation essary after 3 weeks to a max. of 80 25 mg - 1000’s.
symptoms. If intolerable symptoms occur following mg daily (ELDERLY 60 mg daily); usual
metoprolol; antidepressants such as desip- POM Imipramine (Kayhelt)
a discontinuation, resume the previously prescribed maintenance range 20–60 mg once
ramine, clomipramine and nortriptyline or dose and then reduce at a more gradual rate. Tablet, Imipramine HCI 25 mg
antipsychotics like risperidone, thioridazine daily (ELDERLY 20–40 mg once daily).
(Additional information sourced from Cipralex® monograph: Note: Consider the long duration of action of fluox- POM SPARDYSK® (Zolon)
and haloperidol.
http://www.medicines.org.uk/) etine when adjusting dosage. Tablets, Imipramine HCI 25 mg, 75 mg; f-c tabs.
Adverse effects: Nausea, diarrhea, restlessness,
25 mg - 3 x 10’s (in blisters) by 7-14 days after starting treatment and phar- diarrhoea, restlessness, hallucinations and POM SEROXAT® (GSK)
75 mg - 3 x 10’s (in blisters) macokinetics do not appear to change during hypomania, rash, including urticaria accompa- Tablet , (20 mg), Paroxetine (as HCl) 20 mg; white
long-term therapy. nied by pruritus or angio-oedema have been scored oval f-c tab. marked ‘Seroxat 20’.
MOCLOBEMIDE Paroxetine inhibits the hepatic cytochrome reported; Extrapyramidal reactions have been 20 mg - 2 x 15’s.
Tablet , (30 mg), Paroxetine (as HCl) 30 mg; blue
Therapeutic category: MAOI, Antidepressant p450 enzyme and this may enhanc plasma reported infrequently; Dystonic movement
scored oval f-c tab. marked ‘Seroxat 30’.
Pharmacology: Moclobemide is a MAOI. It acts levels of those co-administered drugs which face, tongue and eyes have also been reported; 20 mg - 2 x 15’s.
through reversible inhibition of monoamine are metabolised by this isozyme such as cer- rarely abnormalities of liver function tests
oxidase type A (RIMA). he metabolism of nor- tain tricyclic antidepressants, phenothiazine and hyponatraemia; dry mouth, constipation, SERTRALINE
epinephrine and serotonin is decreased leading neuroleptics and type 1c anti-arrhythmics. somnolence may occur.
Therapeutic category: SSRI, Antidepressant.
to increased concentrations of these neuronal Long-term treatment with Paroxetine has Advice to patients: Abrupt discontinuation
Pharmacology: The principal belief of the mon-
transmitters in the cerebral neurotransmitter shown antidepressant efficacy is maintained of therapy may cause dizziness, sensory dis-
oamine theory of depression is that depressive
system. for periods of at least one year. turbance (e.g. paraesthesia), anxiety, sleep
symptoms arise because of central deficiency
Moclobemide relieves symptoms such as dys- Indications: Adults: Treatment of symptoms disturbances including vivid dreams), agita-
of one or both the neurotransmitters serotonin
phoria, exhaustion, lack of drive and inability of depressive illness of all types including tion, tremor, nausea, sweating and confusion;
(5-HT) and noradrenaline (norepinephrine).
to concentrate. reactive and severe depression accompanied gradual discontinuation by dose-tapering or
By selectively blocking serotonin reuptake,
Indications: Treatment of depressive syn- by anxiety; following an initial satisfactory alternate day dosing should be considered.
sertraline increases the availability of this
dromes; it improves the quality of sleep but response, continued therapy is effective in Dose: To be administered once daily in the
neurotransmitter and this accounts for its an-
does not impair alertness. preventing relapse of depression. Treatment morning with food; tablet should
tidepressant activity. It is devoid of stimulant,
Contra-indications: Hypersensitivity to the of symptoms and prevention of relapse of ob- beswallowed whole, not chewed.
sedative or anticholinergic activity. It has no
drug; acute confusional states; children. sessive compulsive disorder (OCD), generalized By mouth, Adults, Depression, gener-
affinity for muscarinic (cholinergic), serotoner-
Precautions: Thyrotoxicosis or pheochromo- anxiety disorder, and also panic disorder with alized anxiety disorder, post traumatic
gic, dopaminergic, adrenergic, histaminergic,
EMDEX
cytoma. or without agoraphobia. Treatment of social stress disorder, 20 mg daily; may be in-
GABA or benzodiazepine receptors. They do not
Adverse effects: Nervousness, sleep dis- anxiety disorder/social phobia and post-trau- creased weekly in 10 mg increments,
cause weight gain. Sertraline is slowly absorbed
turbances, dizziness, agitation, feelings of matic stress disorder. up to a max. 50 mg per day.
after oral administration. Food slightly increases
anxiety, dry mouth, nausea, feeling of fullness, Children and adolescents: Not recommended Social Anxiety Disorder/Social Phobia,
sertraline bioavailability and it is recommended
diarrhoea, constipation. for treatment of children with depression. 20 mg dailymay be increased weekly
that sertraline capsules be administered with
Advice to patients: May be given with food Contra-indications: Hypersensitivity to par- in 10 mg increments as required, up
meals. It is extensively metabolised in the liver
to lessen GI upset oxetine or excipients. Avoid co-administration to a max. 50 mg/day.
and less than 0.2% is excreted unchanged in
Dose: By mouth, initially, 150 mg twice daily; with MAOIs or within 2 weeks of terminating Obsessive Compulsive Disorder, Initially
the urine. It has elimination half-life of about
reduced to 150 mg once daily if the treatment with MAOIs, and also thioridazine. 20 mg daily; may be increased weekly
26 hours and is thus suitable for once-daily
patient’s response is good. Precautions: MAOIs: not recommended for in 10 mg increments to 40 mg daily;
administration.
In severe depression, up to 600 mg use in combination with MAOIs or within two up to a max. 50 mg daily.
Indications: Treatment of symptoms of de-
daily in divided Doses; Doses should weeks of terminating treatment with MAO Panic disorder, Initially 10 mg daily
pression in patients with or without a history
not be raised until after the first week. inhibitors; History of mania; Patients receiv- increased weekly in 10 mg incre-
of mania; prophylaxis against recurrence of
To be taken at the end of meals. ing oral anticoagulants; Cardiac conditions; ments to 40 mg daily according to
depression.
POM AURORIX® (Swipha) Epilepsy; Seizures; ECT; Use during pregnancy the patient’s response; up to a max.
Contra-ndications: Hypersensitivity to ser-
Tablet, Moclobemide 150 mg; scored tab. and lactation; Ability to drive/use machines 50 mg per day.
traline.
150 mg - 30. may be impaired. Elderly: Increased plasma concentra-
Precautions: MAOI (sertraline should not be
Interactions: Food/antacids: no effect on ab- tions may occur. Start at the usual
used in combination with a MAOI or within 14
PAROXETINE sorption and pharmacokinetics of Paroxetine; adult starting dose and may increase
days of discontinuing treatment with a MAOI);
Therapeutic category: Antidepressant; SSRI Tryptophan: may cause ‘serotonin syndrome’ in weekly 10 mg increments to a max.
Pimozide (avoid co-administration); hepatic
Pharmacology: Paroxetine is a potent and se- resulting in a combination of agitation, 40 mg daily according to the patient’s
insufficiency (use a lower or less frequent dose);
lective inhibitor of 5-hydroxytryptamine re-up- restlessness and GI symptoms including diar- response.
renal insufficiency (proportion of unchanged
take (5-HT, serotonin) and its antidepressant rhoea; Drug metabolising enzyme inducers/ Children: Not recommended.
drug excreted in the urine is small and may
action and efficacy in the treatment of OCD inhibitors: may affect metabolism and phar- Renal/hepatic impairment: Increased
not necessitate dosage adjustment); children,
and panic disorder is thought to be related to macokinetics of Paroxetine; Alcohol: avoid plasma concentrations may occur in
pregnancy, lactation; driving a car or operating
its specific inhibition of 5-HT re-uptake brain concomitant use; MAOIs; Lithium: monitor severe renal impairment (ClCr <30
machinery.
neurones. Paroxetine is chemically unrelated lithium levels when co-administered; Pheny- mL/min) or hepatic impairment. Use
Adverse effects: Nausea, diarrhoea/loose
to the tricyclic, tetracyclic and other available toin/anticonvulsants: may increase incidence lower end of the dosage range.
stools, dyspepsia, tremor, dizziness, insomnia,
antidepressants. of adverse effects; Warfarin: may result in in- Administration: May be given without regards to
meals, but in the presence of GI upset take with food. somnolence, sweating, dry mouth and male
The principal metabolites are polar conjugated creased bleeding in the presence of unaltered
Note: A low initial starting dose is recommended sexual dysfunction (principally ejaculatory
products of oxidation and methylation which prothrombin times.
to avoid worsening of symptoms during early delay).
are readily cleared and have no pharmacologi- Adverse effects: Most commonly nausea,
treatment of panic disorder. May adjust dose as Advice to patients: Notify physician if you
cal activity. It is well absorbed after oral dosing somnolence, sweating, tremor, asthenia, needed within 2-3 weeks of initiation of therapy are currently on another antidepressant drug;
and undergoes first-pass metabolism; elimina- dry mouth, insomnia, sexual dysfunction and thereafter based on response and tolerance. alert physician if you are pregnant or intend
tion half-life is variable but is generally about (including impotence and ejaculation disor- Treatment may last several months for depression becoming pregnant while on this drug; avoid
one day. Steady state systemic levels attained der(s), dizziness, constipation, diarrhoea and and may be even longer for OCD and panic disorder alcoholic drinks; weight loss may occur, but it
decreased appetite; Also dizziness, vomiting, to ensure patient is free of symptoms.
48 | 1.4.2 Drugs used in bipolar disorders 1.4.2 Drugs used in bipolar disorders | 49
is usually minimal. is the mainstay of treatment but its narrow 5); renal impairment (Appendix 4); cardiac 400–600 mg daily.
Nursing action: See notes above. therapeutic range is a disadvantage. Valproic disease (see also Contra-indications); skin re- Administration: Take with food to reduce GI upset.
Dose: By mouth, initially 50 mg once daily acid (sodium valproate) is effective and carba- actions (see Adverse effects); history of blood POM Carbamazepine (WMF 24.2.2)
(either in the morning or evening); mazepine may also be used. disorders (blood counts before and during Tablets, Carbamazepine 100 mg, 200 mg.
increased if necessary in 50 mg incre- Treatment of depressive episodes in bipolar treatment); glaucoma; pregnancy (Appendix
POM Carbamazepine (EDL 27.3.2)
ments to a max. 200 mg daily over a disorders will mostly involve combination 2 [neural tube screening]); breastfeeding
Tablets, Carbamazepine 100 mg, 200 mg; scored tab.
period of weeks. Maintenance Dose, treatment using either lithium or sodium val- (Appendix 3); avoid sudden withdrawal; inter-
50-100 mg; Doses of ≥150 mg should proate together with a tricyclic antidepressant. actions: Appendix 1. See section 1.7 for the proprietary preparations of
not be used for >8 weeks Increased adverse effects are a problem which BLOOD, HEPATIC OR SKIN DISORDERS: Patients Carbamazepine.
Elderly, usual adult dose. may compromise treatment. or their carers should be told how to recognize
Administration: May be given without regards to Lithium prophylaxis should usually only be signs of blood, liver or skin disorders, and LITHIUM
meals, but in the presence of GI upset take with food. undertaken with specialist advice and the advised to seek immediate medical attention Indications: Treatment and prophylaxis of
POM INOSERT® (IPCA) likelihood of recurrence considered. Long-term if symptoms such as fever, sore throat, rash, mania, prophylaxis of bipolar disorder and
Tablets, Sertraline (as HCl) 50 mg, 100 mg; f-c tabs. lithium therapy has been associated with thy- mouth ulcers, bruising or bleeding develop. recurrent depression.
50 mg - 10’s; 14’s. roid disorders and mild cognitive and memory Leukopenia which is severe, progressive and Contra-indications: Renal impairment (Ap-
100 mg - 10’s; 14’s. impairment. Patients should continue the associated with clinical symptoms requires pendix 4); cardiac insufficiency; conditions with
POM SERLIFT® (Ranbaxy) treatment for longer than 3 to 5 years only if withdrawal (if necessary under cover of suit- sodium imbalance such as Addison disease.
Tablets, Sertraline (as HCl) 25 mg, 50 mg; f-c tabs. benefit persists. able alternative). Precautions: Measure serum-lithium concen-
25 mg - 10 x 10’s (in blister) Withdrawal appears to produce high levels Adverse effects: Dizziness, drowsiness, head- tration about 4 days after starting treatment,
50 mg - 10 x 10’s (in blister). of relapse. If lithium is to be discontinued, ache, ataxia, blurred vision, diplopia (may be then weekly until stabilized, then at least every
POM SETRAL® (PharmacyPlus) the dose should be reduced gradually over associated with high plasma concentrations); 3 months; monitor renal function and thyroid
EMDEX
Tablet, Setraline (as HCl) 50 mg, 100 mg. a few weeks and patients should be warned GI intolerance including nausea and vomiting, function every 6–12 months on stabilized
50 mg - 2 x 14`s . of possible relapses if discontinued abruptly. anorexia, abdominal pain, dry mouth, diarrhoea regimens—risk of hypothyroidism (see below);
100 mg - 2 x 14’s. Lithium salts have a narrow therapeutic/toxic or constipation; commonly, mild transient maintain adequate fluid and sodium intake;
POM ZOLOFT® (Pfizer)
ratio and should only be prescribed if there generalized erythematous rash (withdraw if reduce dose or discontinue in diarrhoea, vom-
Capsule, Sertraline (as HCl) 50 mg; orange/yellow are facilities for monitoring serum lithium worsens or is accompanied by other symp- iting and intercurrent infection (especially if
cap. in blister pack. concentrations. Doses are adjusted to achieve toms); leukopenia and other blood disorders associated with profuse sweating); psoriasis
50 mg - 15. serum-lithium concentrations of 0.4–1 mmol/ (including thrombocytopenia, agranulocytosis (risk of exacerbation); pregnancy (Appendix
litre (lower end of range for maintenance and aplastic anaemia); cholestatic jaundice, 2); breastfeeding (Appendix 3); elderly (reduce
POM ZOSERT® (Synergy)
Tablet, Sertraline (as HCl) 25 mg, 50 mg, 100 mg; therapy and the elderly) on samples taken 12 hepatitis, acute renal failure, Stevens-Johnson dose); diuretic treatment, myasthenia gravis;
f-c tabs. hours after the preceding dose. The optimum syndrome (erythema multiforme), toxic epider- surgery; avoid abrupt withdrawal (see notes
25 mg - 10’s (in blister) range for each patient should be determined. mal necrolysis, alopecia, thromboembolism, above); interactions: Appendix 1
50 mg - 10’s (in blister) Overdosage, usually with serum-lithium con- arthralgia, fever, proteinuria, lymph node en- Advice to patients:Patients should maintain
100 mg - 10’s (in blister) centration of over 1.5 mmol/litre may be fatal largement, arrhythmias, heart block and heart adequate fluid intake and avoid dietary
and toxic effects include coarse tremor, ataxia, failure, dyskinesias, paraesthesia, depression, changes which reduce or increase sodium
1.4.2 Drugs used in bipolar disorders dysarthria, nystagmus, renal impairment and impotence, male infertility, gynaecomastia, ga- intake. Patients should be advised to seek med-
Treatment of bipolar disorders has to take convulsions. If any of these effects occur, lactorrhoea, aggression, activation of psychosis, ical attention if symptoms of hypothyroidism
account of three stages: treatment of the acute treatment should be stopped, serum-lithium photosensitivity, pulmonary hypersensitivity, (for example, feeling cold, lethargy) develop
episode, continuation phase and prophylaxis concentration determined and in mild over- hyponatraemia, oedema, disturbances of bone (women are at greater risk).
to prevent further episodes. Lithium is effec- dosage large amounts of sodium salts and metabolism with osteomalacia also reported; Adverse effects: GI disturbances, fine tremor,
tive in acute mania but symptomatic control fluid should be given to reverse the toxicity; in confusion and agitation in elderly. renal impairment (particularly impaired urinary
of the florid symptoms with an antipsychotic severe toxicity, haemodialysis may be required. Advice to patients: May cause drowsiness. concentration and polyuria), polydipsia, leuko-
or benzodiazepine is often necessary whilst For patients who are unresponsive to or Ability to operate machinery or drive may be cytosis, weight gain and oedema (may respond
waiting for the antimania drug to exert its ef- intolerant of lithium, carbamazepine may be impaired. Avoid alcoholic beverages. to dose reduction); hyperparathyroidism and
fect. Benzodiazepines may be given during the used in the prophylaxis of bipolar disorder Nursing action: hypercalcaemia reported; signs of intoxication
particularly in those with rapid cycling man- • Give with food or milk to minimize GI distress. include blurred vision, muscle weakness, in-
initial stages until lithium becomes effective
ic-depressive illness (more than four affective • Relieve dry mouth with frequent sips of water,
but they should not be used for long periods creasing gastrointestinal disturbances (anorexia,
episodes per year). gum or hard candy.
because of the risk of dependence. Lithium • Advise patient to avoid driving or potentially
vomiting, diarrhoea), increased CNS disturbances
may be given concurrently with antipsychotics hazardous activities that require mental alertness. (mild drowsiness and sluggishness, increasing
and treatment with the antipsychotic should CARBAMAZEPINE to giddiness with ataxia, coarse tremor, lack of
• Observe patient for excessive sedation; do not
be tailed off as lithium becomes effective. Indications: Prophylaxis of bipolar disorder un- discontinue suddenly when treating seizures or co-ordination, dysarthria) and require withdrawal
Alternatively, lithium therapy may be delayed responsive to or intolerant of lithium; epilepsy, status epilepticus. of treatment; with severe overdosage (serum
until the patient’s mood is stabilized with trigeminal neuralgia (section 1.7). Dose: Prophylaxis of bipolar disorder, by concentrations above 2 mmol/litre), hyperreflexia
the antipsychotic. However, there is a risk of Contra-indications: AV conduction abnor- mouth, ADULT initially 400 mg daily and hyperextension of the limbs, convulsions,
neurotoxicity and increased extrapyramidal malities; history of bone-marrow depression; in divided doses increased until toxic psychoses, syncope, renal failure, circula-
disorders when lithium and antipsychotics porphyria. symptoms are controlled to a max. of tory failure, coma, occasionally death; goitre,
are used concurrently (Appendix 1). Lithium Precautions: Hepatic impairment (Appendix 1.6 g daily; usual maintenance range raised antidiuretic hormone concentration,
50 | 1.4.2 Drugs used in bipolar disorders 1.5 Obsessive-compulsive disorders and panic attacks | 51
hypothyroidism, hypo-kalaemia, ECG changes, history of severe hepatic dysfunction; pancre- mg/kg daily). (occasional weight loss); endocrine adverse
and kidney changes may occur. atitis; porphyria. POM Valproic acid (WMF 24.2.2)
effects such as testicular enlargement, gy-
Nursing action: Precautions: Monitor liver function before Tablets, Sodium valproate 200 mg, 500 mg; e-c naecomastia and galactorrhoea; convulsions,
• Give with meals to decrease GI upset. and during therapy (Appendix 5), especially in tablets (Gastro-resistant tablets). movement disorders and dyskinesias, dysar-
• Ensure adequate fluid intake of 2-3 litres daily to patients at most risk (those with metabolic dis- thria, paraesthesia, taste disturbances, tinnitus,
prevent dehydration during the initial treatment POM Valproic acid (EDL 27.3.2)
orders, degenerative disorders, organic brain fever, agranulocytosis, leukopenia, eosinophilia,
period; salt intake should also be adjusted to com- Tablets, Sodium valproate 200 mg, 500 mg; e-c tabs.
disease or severe seizure disorders associated purpura, thrombocytopenia, hyponatraemia
pensate for losses through sweating or diarrhoea. See section 1.7 for the proprietary preparations of
• Teach patient to avoid tasks requiring psychomotor
with mental retardation); ensure no undue (may be due to inappropriate antidiuretic hor-
potential for bleeding before starting and Sodium valproate. mone secretion); abnormal liver function test,
co-ordination until the CNS effects are known.
• Advise patient to report to physician at the earli- before major surgery or anticoagulant therapy; diarrhoea; hair loss reported.
est signs of toxicity namely diarrhoea, vomiting, renal impairment (Appendix 4); pregnancy 1.5 Obsessive-compulsive disorders Dose: Phobic and obsessional states, by
drowsiness, muscular weakness, ataxia. He should (Appendix 2 [neural tube screening]); breast- and panic attacks mouth, ADULT initially 25 mg daily,
expect transient nausea, polyuria, thirst, and dis- feeding (Appendix 3); SLE; false-positive urine usually at bedtime (ELDERLY 10 mg
comfort during first few days of therapy. Obsessive-compulsive disorders can be treated
tests for ketones; avoid sudden withdrawal; with a combination of pharmacological, behav- daily) increased over 2 weeks to
• Monitor therapy; regular Lithium blood level interactions: Appendix 1. 100–150 mg daily; CHILD not usually
determinations are mandatory due to the narrow ioural and psychological treatments.
BLOOD OR HEPATIC DISORDERS: Patients or Antidepressants such as clomipramine which recommended
therapeutic margin of safety.
their carers should be told how to recognize Administration: May administer with or without
• Monitor blood glucose closely in diabetics. inhibit reuptake of serotonin have been found meals. the total daily dose can be given at bedtime
Dose: Treatment of mania (general guidelines signs of blood or liver disorders, and advised to be effective. Panic attacks may be treated
to seek immediate medical attention if symp- because of its sedative effects. for minority of
only, see also note below) by mouth , with behavioural or cognitive therapy. If this patients who experience difficulty sleeping with
ADULT initially 0.6–1.8 g daily (elderly toms including malaise, weakness, anorexia, management fails, drug therapy may be tried. bedtime dosing, the dose should be given in the
300–900 mg daily lethargy, oedema, vomiting, abdominal pain, Some tricyclic antidepressants including clo- morning.
EMDEX
Prophylaxis of mania, bipolar disorder drowsiness, jaundice, or spontaneous bruising mipramine, or SSRIs can reduce frequency of
or bleeding develop PANCREATITIS. Patients or POM Clomipramine (WMF 24.4)
and recurrent depression (general attacks or prevent them completely. Capsules, Clomipramine HCl 10 mg, 25 mg.
guidelines only, see also note below), their carers should be told how to recognize Benzodiazepines may be used in panic attacks
by mouth , ADULT initially 0.6–1.2 g signs of pancreatitis and advised to seek im- resistant to antidepressants.
mediate medical attention if symptoms such as 1.6 Antiparkinson drugs
daily (elderly 300–900 mg daily).
Note: Different preparations vary widely in bioavail- abdominal pain, nausea and vomiting develop; CLOMIPRAMINE 1.6.1 Drugs used in parkinsonism
ability; a change in the preparation used requires the discontinue sodium valproate if pancreatitis 1.6.2 Drugs used in essential tremor and related
Indications: Phobic and obsessional states; disorders
same precautions as initiation of treatment. Dosage diagnosed.
panic attacks.
of lithium depends on the preparation chosen since Advice to patients: May cause drowsiness.
different preparations vary widely in bioavailability. Contra-indications: Recent myocardial in- 1.6.1 Drugs used in parkinsonism
Ability to operate machinery or drive may be
Dosage should be adjusted to achieve a serum-lith- farction, arrhythmias (especially heart block);
impaired. Avoid alcoholic beverages. The use of pharmacotherapy will depend upon
ium concentration of 0.4–1 mmol/litre (lower end manic phase in bipolar disorders; severe liver
Adverse effects: GI irritation, nausea, increased the degree of incapacity of the patient and is
of range for maintenance therapy and in elderly) disease; children; porphyria.
appetite and weight gain, hyperammonaemia; generally not justified until symptoms compro-
on samples taken 12 hours after a dose and 4–7 Precautions: Cardiac disease (see Contra-indi-
days after starting treatment, then every week until ataxia, tremor; transient hair loss (regrowth mise working ability and social relationships;
cations above), history of epilepsy; pregnancy
dosage has remained unchanged for 4 weeks, then may be curly); oedema, thrombocytopenia, although levodopa is used in the early stages
(Appendix 2); breastfeeding (Appendix 3);
every 3 months thereafter.Note: Different prepara- inhibition of platelet aggregation; impaired in some patients. Close supervision is then
elderly; hepatic impairment (Appendix 5);
tions vary widely in bioavailability; a change in the hepatic function and rarely fatal hepatic failure needed to ensure that treatment regimens
thyroid disease; phaeochromocytoma; history
preparation used requires the same precautions as (see Precautions—withdraw treatment imme- are tolerated and that appropriate changes are
initiation of treatment. of mania, psychoses (may aggravate psychotic
diately if malaise, weakness, lethargy, oedema, made to the regimen as the disease progresses.
symptoms); angle-closure glaucoma, history of
POM Lithium (WMF 24.2.2) abdominal pain, vomiting, anorexia, jaundice, The most effective form of therapy is a com-
urinary retention; concurrent electroconvulsive
Tablet/Capsule, Lithium carbonate 300 mg. drowsiness); sedation reported and also in- bination of levodopa and a peripheral do-
therapy; avoid abrupt withdrawal; anaesthesia
creased alertness; behavioural disturbances; pa-decarboxylase inhibitor, such as carbidopa.
POM Lithium (EDL 27.3.2/Restricted List) (increased risk of arrhythmias and hypoten-
Tablet/Capsule, Lithium carbonate 300 mg. rarely pancreatitis (measure plasma amylase if The response to levodopa with carbidopa is a
sion); interactions: Appendix 1.
acute abdominal pain), extrapyramidal symp- compromise between increased mobility and
POM LITHOSUN® (Synergy) Adverse effects: Sedation, dry mouth, blurred
toms, leukopenia, pancytopenia, red cell hy- adverse effects. Dyskinesias may be dose lim-
Tablets, Lithium carbonate 250 mg, 300 mg; white vision (disturbance of accommodation, in-
poplasia, fibrinogen reduction; irregular men- iting and increasingly frequent with increased
scored tabs. creased intra-ocular pressure), constipation,
strual periods, amenorrhoea, gynaecomastia, duration of treatment. Many factors including
250 mg - 10 x 10’s nausea, difficulty in micturition; cardiovascular
300 mg - 10 x 10’s hearing loss, Fanconi syndrome, dementia, tolerance and progression of the disease may
adverse effects particularly with high dosage
toxic epidermal necrolysis, Stevens-Johnson result in complications after 2–5 years of treat-
POM LITHOSUN SR® (Synergy) including ECG changes, arrhythmias, postural
syndrome (erythema multiforme), vasculitis, ment. ‘End-of-dose’ deterioration occurs when
Tablet, Lithium carbonate 400 mg; uncoated s-r tab. hypotension, tachycardia, syncope; sweating,
hirsutism, and acne reported. there is a reduced duration of benefit from a
400 mg - 10 x 10’s tremor, rash and hypersensitivity reactions
Dose: Acute mania, by mouth, ADULT initially dose, resulting in disability and dystonias. The
(urticaria, photosensitivity); behavioural dis-
700 mg daily in divided doses, ‘on-off’ phenomenon is characterized by large
VALPROIC ACID turbances; hypomania or mania, confusion
increased as quickly as possible to variations in motor performance, with normal
Indications: Acute mania; epilepsy (section or delirium (particularly in elderly), headache,
achieve the optimal response (max- function during the ‘on’ period, and weakness
1.7) interference with sexual function, blood sugar
imum 70 mg/kg daily but monitor and restricted mobility during the ‘off’ period.
Contra-indications: Active liver disease, family changes; increased appetite and weight gain
patient closely if dose greater than 52
52 | 1.6.1 Drugs used in parkinsonism 1.6.1 Drugs used in parkinsonism | 53
Amelioration of these effects can sometimes (‘end-of-dose’ effects) and (‘on-off’ effects) rapid or pounding heartbeat, confusion, eye Ability to operate machinery or drive may
be achieved by administering levodopa in a after prolonged treatment (see notes above); pain, rash, fever or heat intolerance occurs. be impaired. Avoid strenous activities in hot
sustained-release preparation or in a greater neuroleptic malignant syndrome, on sudden Observe caution when performing hazardous weather.
number of fractionated doses throughout the withdrawal; rarely hypersensitivity. tasks or those that require alertness such as Nursing action:
day. Psychiatric symptoms including disruption Dose: Parkinsonism, by mouth , ADULT driving, as drug may cause drowsiness. Avoid • Administer with or after meals to minimize GI up-
of sleep, vivid dreams and hallucinations are expressed in terms of levodopa, alcohol and other CNS depressants. May set; may give with fluids other than water.
characteristic adverse effects that may occur initially 100 mg (with carbidopa 10 cause dry mouth - adequate fluid intake or • Give I.V. injection slowly. Keep patient in a re-
cumbent position as parenteral dose may cause
at any time, especially in the elderly, and may mg) twice daily, increased by 100 mg chewing gum may relieve. Difficult urination
transient postural hypotension and coordination
require dose reduction or withdrawal of (with carbidopa 10 mg) every few or constipation may occur - notify physician disturbances.
levodopa. days as necessary, to a maximum of if effects persist; may increase susceptibility • Relieve dry mouth with ice cubes, cool drinks or
Treatment for idiopathic parkinsonism is often levodopa 1.5 g to heat stroke. hard sweets.
initiated with a dopamine receptor agonist Administration: Optimum daily Dose must be Nursing action: • Warn patient to avoid activities that require alert-
such as bromocriptine [not on WHO Model determined for each patient by careful monitoring • Tolerated best if given in 3 daily doses and with ness, as the drug may cause drowsiness.
List]. Supplementary use of amantadine [not and be taken after meals. food; high doses may be divided into 4 doses, at • Teach patient not to stop taking drug abruptly; to
Note: Carbidopa 70–100 mg daily is necessary for meal times and at bed time. be tapered off over 1 week.
on WHO Model List], bromocriptine or the
full inhibition of peripheral dopa-decaboxylase. • Patients may be switched to sustained-action • Notify physician if urinary hesitancy or retention
monoamine-oxidase-B inhibitor, selegiline
capsules when stabilised on conventional dosage occurs
[not on WHO Model List] can be of value either POM Carbidopa plus Levodopa (WMF 9)
forms. • Teach patient to avoid cold or cough medications
to enhance the effect of levodopa or to reduce Tablets, Carbidopa 10 mg, Levodopa 100 mg; Carbi-
dopa 25 mg, levodopa 250 mg. Dose: Adult, by mouth, initially 1-2 mg daily; with lcohol and antihistamines except otherwise
‘end-of-dose’ fluctuations and ‘on-off’ effects. increased by 2 mg increments at in- instructed by physician.
Anticholinergic (more correctly termed anti- POM Carbidopa plus Levodopa (EDL 17.1) tervals of 3-5 days. Maintenance: 5-15 • Observe patient closely for adverse reactions espe-
Tablet, Carbidopa 10 mg, Levodopa 100 mg; Carbi- cially in the elderly and debilitated patients (inform
muscarinic) drugs such as biperiden are usu- mg daily in 3-4 divided doses.
EMDEX
dopa 25 mg, levodopa 250 mg. the doctor immediately). Because of possibility of
ally sufficient in drug-induced parkinsonism.
POM Benzhexol (EDL 17.1 & 27.1) dizziness, help patient into bed.
POM SYNDOPA® (Synergy)
Tablets, Benzhexol HCl 2 mg, 5 mg. • May increase susceptibility to heat stroke; advise
Tablet , (100/10 mg), Levodopa 100 mg, carbidopa
LEVODOPA plus CARBIDOPA patient to limit activities during hot weather.
10 mg. POM APO-TRIHEX® (Lahams)
Indications: All forms of parkinsonism other Pack: 10’s Tablets, Benzhexol HCl 2 mg, white scored tab. Dose: Drug-induced extrapyramidal symp-
than drug-induced. Tablet , (100/25 mg), Levodopa 100 mg, carbidopa marked ‘APO TRM’; 5 mg, white scored tab. marked toms, parkinsonism, by mouth,
Contra-indications: Concurrent use of MAOIs; 25 mg. ‘APO 5’ ADULT, as biperiden hydrochloride,
angleclosure glaucoma; confirmed or sus- Pack: 10’s 2 mg - 500 initially 1 mg twice daily, increased
pected malignant melanoma. Tablet , (250/25 mg), Levodopa 250 mg, carbidopa 5 mg - 100, 500. gradually to 2 mg 3 times daily; usual
Precautions: Pulmonary disease, peptic ul- 25 mg. maintenance dose 3–12 mg daily in
POM OXAZOL® (PharmacyPlus)
Pack: 10’s divided doses.
ceration, CVD (including previous myocardial Tablet, Benzhexol 2 mg, 5 mg.
infarction); diabetes mellitus, osteomalacia, 2 mg - 1000’s. Drug-induced extrapyramidal symp-
BENZHEXOL
open-angle glaucoma, history of melanoma 5 mg - 1000’s. toms, parkinsonism, by IM injection or
(risk of activation), psychiatric illness (avoid if Synonym: Trihexyphenidyl HCl slow IV injection, Adult, as biperiden
POM PBENZ® (Pharmabase)
severe); close monitoring of hepatic, haema- Therapeutic category: Anticholinergic Agent; lactate, 2.5–5 mg repeated as neces-
Tablet, Benzhexol HCI 5 mg; uncoated tab.
tological, psychiatric, cardiovascular, and renal Anti-Parkinson’s Agent. 5 mg - 1000’s (in jar) sary to maximum 20 mg in 24 hours.
function required in long-term therapy; elderly: Indications: Extrapyramidal syndrome (but
POM Biperiden (WMF 9)
avoid rapid dose increases; warn patients not tardive dyskinesia) induced by drugs such
BIPERIDEN Tablet, Biperiden HCl 2 mg
to resume normal activities gradually; avoid as phenothiazines and reserpine; adjunctive Injection, Biperiden lactate 5 mg per mL; in 1-mL
treatment of Parkinson’s disease. Indications: Drug-induced extrapyramidal
abrupt withdrawal; pregnancy (toxicity in an- amp.
Contra-indications: Hypersensitivity to symptoms (but not tardive dyskinesias) and
imals) (Appendix 2), breastfeeding (Appendix
benzhexol or any component; narrow-angle adjunctive treatment of parkinsonism. POM Biperiden (EDL 17.1 & 27.1)
3); interactions: Appendix 1. Tablet, Biperiden HCl 2 mg
glaucoma; pyloric or duodenal obstruction; Contra-indications: Angle-closure glaucoma;
Adverse effects: Nausea, anorexia and vom- Injection, Biperiden (as lactate) 5 mg per mL; in
achalasia; myasthenia gravis. untreated urinary retention; prostatic hypertro-
iting, particularly at the start of treatment; 1-mL amp.
Precautions: Urinary retention; cardiac, renal phy; myasthenia gravis; GI obstruction.
postural hypotension at the start of treatment,
or hepatic disorders; elderly; hot weather or Precautions: Elderly; CVD, hepatic or renal im-
particularly in elderly and those receiving BROMOCRIPTINE
during exercise. pairment; avoid abrupt withdrawal; pregnancy
antihypertensives; excessive drowsiness and Indications: Parkinsons disease, but not
Adverse effects: Constipation, dry mouth; and breast-feeding; interactions: Appendix 1.
sudden onset of sleep (warn patient of these drug-induced extrapyramidal symptoms;
decreased sweating; dry nose, throat or skin; Adverse effects: Drowsiness, dry mouth,
effects); confusion, vivid dreams, dizziness, endocrine disorders, section 10.6.
less commonly decreased flow of breast milk, constipation, blurred vision; hesitancy of mic-
tachycardia, arrhythmias; reddish discoloration Contra-indications, Precautions, Adverse
difficulty in swallowing, orthostatic hypoten- turition, dizziness, tachycardia, arrhythmias;
of body fluids; insomnia, headache, flushing, GI effects, Nursing action, Advice to patients
sion, tachycardia, drowsiness, blurred vision, confusion, excitement, agitation, hallucina-
bleeding, peripheral neuropathy; taste distur- and available preparations: See Bromocriptine
weakness, difficult urination, nausea, vomiting, tions, and psychiatric disturbances with high
bances, pruritis, rash, liver enzyme changes; in section 10.6.
loss of memory, rash. dosage, especially in the elderly and other
psychiatric symptoms including psychosis, Dose: By mouth, 1.25mg daily, preferably
Advice to patients: Take after meals or with susceptible patients, may require withdrawal
depression, hallucinations, delusions and neu- in the evening, for the 1st week;
food if GI upset occurs; do not discontinue drug of treatment; impaired memory.
rological disturbances including dyskinesias increased gradually by 1.25 mg/day
abruptly; notify physician if adverse GI effects, Advice to patients: May cause drowsiness.
may be doselimiting; painful dystonic spasms each week in 2-3 divided doses for 6 -
54 | 1.6.1 Drugs used in parkinsonism 1.6.2 Drugs used in essential tremor and related disorders | 55
8 weeks. A further increase by 2.5mg/ effectiveness of ropinirole. No interaction with 1.6.2 Drugs used in essential tremor 1.7 Anticonvulsants (Antiepileptics)
day each week may be required to domperidone. Estrogens may reduce clearance and related disorders Control of epilepsy
achieve adequate therapeutic re- of ropinirole. Ropinirole may potentiate do- ESSENTIAL TREMOR
sponse; usual range is 10 -40 mg per paminergic side effects of levodopa and may Treatment should always be started with a
day. To be taken with food. cause or exacerbate pre-exisiting dyskinesias. It can be treated with beta-blockers such as single drug, but the choice of an antiepileptic
Administration: May be taken with or without Adverse effects: Extreme sleepiness and/ propranolol (120 mg daily) (section 1.8) which can only be made on an individual basis and
meals. or sudden sleep attacks, nausea, vomiting, may be of value if the tremor results in physical will depend on the efficacy of the drug and the
abdominal pain, dyspepsia, dizziness (includ- or social disability. patient’s tolerance of treatment. If a drug fails
See section 10.6 for the preparations of Bromocriptine.
ing vertigo), orthostatic hypotension and leg DYSTONIAS to control the seizures after it has been used in
oedema; others are confusion, hallucinations, full therapeutic dosage for an adequate period,
ROPINIROLE If no identifiable cause is found and the patient or if it is not tolerated, it should be gradually
fainting. Rarely, especially at high doses, signs does not go into spontaneous remission, a trial
Therapeutic category: Non-ergoline dopa- of pathological gambling, increased libido and substituted with another with the first drug
mine agonist, Antiparkinsonian drug. of levodopa should be given to determine being withdrawn only when the new regimen
hypersexuality. whether the patient has dopamine-responsive
Pharmacology: Parkinson’s disease (PD) is Advice to patients: Take with food to minimise is mainly established. If monotherapy is ineffec-
characterised by a marked dopamine defi- dystonia. If there is no response within three tive, two drugs should be given in combination
GI upset. Swallow whole. Do not crush or chew. months, the drug should be withdrawn and
ciency in the nigral striatal system. Ropinirole RLS patients should take at bedtime. May and several regimens may need to be tried
alleviates this deficiency by stimulating striatal small Doses of an anticholinergic drug such as before the most appropriate is found.
cause drowsiness which can be intensified by biperiden should be given. The dosage may be
dopamine receptors - shown high relative in alcohol. Ability to drive or operate machinery Initial dose of the drug of choice should be de-
vitro specificity and full intrisic activity at the D2 increased gradually and up to 16 mg daily may termined on the basis of the degree of urgency,
may be impaired. be tolerated. In patients who fail to respond to
and D3 dopamine receptor subtypes, binding Dose: By mouth, Parkinson’s disease (PD), the size and age of the patient. It should be in-
with higher affinity to D3 than to D2 or D4 recep- either levodopa or an anticholinergic, other creased gradually until an effective response is
Adult (>18 years), initially 0.25 mg drugs including diazepam, baclofen, carba-
EMDEX
tor subtypes. It acts in the hypothalamus and 3 times daily for one week; may obtained. All antiepileptics commonly produce
pituitary to inhibit the secretion of prolactin. mazepine or phenothiazines may be of value. neurological adverse effects at too high a dose,
increase by 0.75 mg/day at weekly in- Psychological treatments have also been used
Ropinirole is absorbed rapidly and almost tervals for the first 4 weeks as follows: and patients should be monitored closely for
completely with a bioavailability of approx. successfully in the management of dyskinesias. adverse effects to help in accurate dose titra-
Week-1 Week-2 Week-3 Week-4
50% and Tmax of about 1.5 hours. It is highly CHOREA tion. Except for phenytoin, it is rarely useful to
mg/dose 0.25 tid 0.5 tid 0.75 tid 1 tid
lipid soluble, has large volume of distribution Choreiform movements can be induced by measure plasma-drug concentrations as an aid
mg/day 0.75 1.5 2.25 3
and low plasma protein binding. Ropinirole is certain drugs including levodopa, phenytoin to dose adjustment. Non-compliance because
metabolised by the cytochrome P450 enzyme Further weekly increments of upto 3 and antipsychotic drugs. Huntington disease of inappropriate dosing and overdosing is a
CYP1A2 and excreted mainly in the urine, both mg/day may be needed depending is the most common of the hereditary choreas. major impediment to effective antiepileptic
ropinirole & its metabolites. on response & tolerance. Therapeu- Drug treatment is symptomatic and does not treatment. Patients should ideally remain un-
Indications: Monotherapy (without Levodopa) tic response may occur at 3-9 mg/ alter the progression of the disease. The aim of der supervision throughout treatment.
for idiopathic Parkinson’s disease; as adjunct to day; doses >24 mg/day not recom- therapy is to reduce dopaminergic transmis- WITHDRAWAL
levodopa to control “on-off” fluctuations which mended. sion which results from excessive or enhanced
may permit a reduction in the total daily dose Restless leg syndrome (RLS), Adult, Treatment is normally continued for a min-
cholinergic activity. Antipsychotic drugs antag- imum of two years after the last seizure.
of levodopa; treatment of moderate to severe initially 0.25 mg once daily for 2 days, onize dopamine and usually lessen the chorea
primary Restless Legs Syndrome (RLS). taken upto 3 hours before bedtime; Withdrawal should be extended over a period
temporarily. Tetrabenazine [not included on of several months because abrupt withdrawal
Contra-indications: Hypersensitivity to may increase to 0.5 mg once daily for WHO Model List], the dopamine-depleting
ropinirole; pregnancy; lactation (may inhibit the remainder of week 1 if tolerated. can lead to complications such as status epilep-
drug, is used to control movement disorders ticus. In patients receiving several antiepileptic
lactation). May increase further by 0.5 mg at in Huntington chorea and related disorders.
Precautions: As with other dopamine agonists, weekly intervals (e.g. 1 mg once daily drugs, only one drug should be withdrawn
may cause sudden “sleep attacks” with or for week 2, 1.5 mg once daily for week TICS at a time. Many adult patients relapse once
without prior feeling of drowsiness; caution 3, etc). Max. 4 mg/day. Tics which resemble choreiform movements treatment is withdrawn and it may be justified
patients about driving or operating machinery; Note: Discontinue gradually in PD patients over a are commonly associated with anxiety. to continue treatment indefinitely, particularly
may cause and/or exacerbate pre-exisiting 7 day period. Reduce frequency of administration However, in the more complex multiple tic when the patient’s livelihood or lifestyle can be
dyskinesia in patients treated with L-dopa for from 3 times daily to twice daily for 4 days, then disorder, Tourette syndrome, treatment with endangered by recurrence of a seizure.
once daily for 3 days. May discontinue in RLS patients
PD (reduce dose of levodopa); avoid abrupt antipsychotic drugs may be required. PREGNANCY AND BREASTFEEDING
with doses upto 4 mg once daily without tapering.
withdrawal of therapy; hepatic or renal impair- TARDIVE DYSKINESIA Untreated epilepsy during pregnancy may
ment; children; elderly ( increased incidence of (Additional information sourced from Requip® monograph:
http://www.medicines.org.uk/) It is associated with chronic administration cause harm to the fetus; there is therefore no
hallucination). justification for abrupt withdrawal of treatment
Interactions: CNS depressants (e.g. alcohol); of antipsychotic drugs. It is characterized by
POM RONIROL® (CG Biostadt) involuntary, repetitive, choreiform movement although withdrawal of therapy may be an
CYP 1A2 inducers (e.g. cigarette smoking, Tablets, Ropinirole (as HCl) 0.25 mg, 1 mg, 2 mg; option if the patient has been seizure-free
rifampin) may increase metabolic clearance of of the cheek, mouth and fingers. The first step
f-c tabs. for at least 2 years; resumption of treatment
ropinirole; CYP 1A2 inhibitors (e.g ciprofloxacin, of treatment should always be discontinuation
0.25 mg - 21’s may be considered after the first trimester.
erythromycin, fluvoxamine) may decrease met- 1 mg - 21’s of the antipsychotic drug or dosage reduction
if the underlying psychotic disorder permits. If antiepileptics are continued in pregnancy,
abolic clearance of ropinirole; Dopamine antag- 2 mg - 21’s.
monotherapy with the lowest effective dose
onists (e.g. butyrophenones, metoclopramide, is preferred, with adjustment made to take
phenothiazines, thioxanthenes) may reduce account of changes in plasma-drug concen-
56 | 1.7 Anticonvulsants (Antiepileptics) 1.7 Anticonvulsants (Antiepileptics) | 57
tration associated with pregnancy. There is an Phenobarbital or phenytoin is widely used sure, and the correction of any hypoglycae- actions (see Adverse effects); history of blood
increased risk of birth defects with the use of for tonic seizures, and valproate for atonic mia; maintenance of the airway and assisted disorders (blood counts before and during
antiepileptics, particularly carbamazepine, seizures, and for atypical absence seizures. ventilation are crucial even when the seizures treatment); glaucoma; pregnancy (important
valproate and phenytoin. However, if there MYOCLONIC SEIZURES are controlled, because the drugs used in its see notes above; Appendix 2); breastfeeding
is good seizure control, there is probably no management may also depress respiration. (see notes above; Appendix 3); avoid sudden
advantage in changing pregnant patients’ an- Valproate is widely used and most effective The use of parenteral thiamine [not included withdrawal;
tiepileptic drugs. In view of the risks of neural for juvenile myoclonic seizures. However, both on WHO Model List] should be considered if interactions: Appendix 1.
tube and other defects, patients who may be- valproate and this type of seizure are associ- alcohol abuse is suspected; pyridoxine should BLOOD, HEPATIC OR SKIN DISORDERS: Patients
come pregnant should be informed of the risks ated with a high relapse rate and it is often be administered if the status epilepticus is or their carers should be told how to recognize
and referred for advice, and pregnant patients necessary to continue therapy indefinitely. likely to be responsive to pyridoxine. signs of blood, liver or skin disorders, and
should be offered counselling and antenatal Other myoclonic seizures are often resistant to IV diazepam is often effective in status epi- advised to seek immediate medical attention
screening. To counteract the risk of neural treatment and some do not have an epileptic lepticus. Diazepam, which acts rapidly, should if symptoms such as fever, sore throat, rash,
tube defects, adequate folate supplements are basis. Valproate can be of value in this case be administered first and should be followed mouth ulcers, bruising or bleeding develop.
advised for women before and during preg- and other antiepileptic drugs may be useful immediately by a loading dose of pheny- Leukopenia which is severe, progressive and
nancy. In view of the risk of neonatal bleeding in intractable cases. toin which has a longer-acting effect. When associated with clinical symptoms requires
associated with carbamazepine, phenobarbital INFANTILE SPASM (INFANTILE MYOCLONIC cannulation is impossible, diazepam may be withdrawal (if necessary under cover of suit-
and phenytoin, prophylactic phytomena-dione EPILEPSY) administered rectally as a solution (absorption able alternative).
(vitamin K1) is recommended for the neonate Infantile spasms, which are often associated from suppositories is too slow for treatment of Adverse effects: Dizziness, drowsiness, head-
and the mother before delivery. Antiepileptic with severe brain damage, can be resistant to status epilepticus). IV phenobarbital is also ache, ataxia, blurred vision, diplopia (may
drugs can be continued during breastfeeding antiepileptic drugs. Vigabatrin [not included effective but is more likely to cause respira- be associated with high plasma levels); GI
(see also Appendix 3). on WHO Model List] or valproate (alone or tory depression; it is used in refractory cases intolerance including nausea and vomiting, an-
EMDEX
DRIVING with clonazepam [not included on WHO Model but should be avoided in patients who have orexia, abdominal pain, dry mouth, diarrhoea
List]) are used. recently received oral phenobarbital. Rectal or constipation; commonly, mild transient
Regulations are in place in many countries paraldehyde may also be used; it causes little generalized erythematous rash (withdraw if
which may, for example, restrict driving by FEBRILE CONVULSIONS respiratory depression and is therefore useful worsens or is accompanied by other symp-
patients with epilepsy to those whose seizures Brief febrile convulsions usually respond to where facilities for resuscitation are poor. toms); leukopenia and other blood disorders
are controlled. Further, antiepileptic and anti- sponging with tepid water and by giving an If seizures continue despite treatment, general (including thrombocytopenia, agranulocytosis
convulsant drugs may cause CNS depression, antipyretic such as paracetamol (section anaesthesia may be required. The underlying and aplastic anaemia); cholestatic jaundice,
particularly in the early stages of treatment 1.8.1). Recurrent febrile convulsions or pro- cause must be identified and remedied in all hepatitis, acute renal failure, Stevens-Johnson
and patients affected by adverse effects such longed convulsions (those lasting 15 minutes cases. syndrome (erythema multiforme), toxic epider-
as drowsiness or dizziness should not operate or longer) are treated with diazepam, either Nursing action: mal necrolysis, alopecia, thromboembolism,
machinery or drive. rectally in solution or by intravenous injection, • Anticonvulsants arthralgia, fever, proteinuria, lymph node en-
Choice of antiepileptic in management of to prevent possible brain damage. • Give with food or milk to reduce GI upset. largement, arrhythmias, heart block and heart
convulsive disorders Intermittent prophylaxis, with diazepam ad- • Maintain good oral hygiene for hydantoins e.g. failure, dyskinesias, paraesthesia, depression,
ministered at the onset of fever, may prevent phenytoin sodium.
GENERALIZED TONIC-CLONIC, SIMPLE PARTIAL impotence, male infertility, gynaecomastia,
• Monitor patient’s blood, liver and kidney pa-
AND COMPLEX PARTIAL SEIZURES recurrence of febrile convulsions but only in galactorrhoea, aggression, activation of psy-
rameters as indicated and notify doctor of any
a small proportion of children and its routine abnormalities. chosis, photosensitivity, pulmonary hypersen-
Carbamazepine, phenobarbital, phenytoin, use in this way is not recommended. Use of sitivity, hyponatraemia, oedema, disturbances
• Notify doctor of abnormal changes in behaviour
and valproate are widely used in the treatment antiepileptics for continuous prophylaxis is of bone metabolism with osteomalacia also
and mood.
of these conditions. However, each of these controversial; it is probably indicated in only • Discontinue drug if you notice allergic reactions (in- reported; confusion and agitation in elderly.
drugs is associated with dose-related and a small proportion of children including those cluding red, raised rash), blood dyscrasia (including Nursing action: See notes above.
idiosyncratic adverse effects and monitoring whose first seizure occurred during the first fever, sore throat, bruising, rash, jaundice); report Dose: Generalized tonic-clonic seizures,
of haematological and hepatic function is 14 months of life, or who already have evident promptly to doctor. partial seizures, by mouth, ADULT
often advised, particularly for carbamazepine neurological abnormalities, or who have had • Advise patient to avoid driving or other activities
initially 100–200 mg 1–2 times daily,
and valproate. that require alertness.
previous prolonged or focal convulsions. increased gradually according to
ABSENCE SEIZURES Phenobarbital may be used for this purpose response to usual maintenance dose
CARBAMAZEPINE
Both ethosuximide and valproate are widely but careful clinical monitoring and dosage of 0.8–1.2 g daily in divided doses;
adjustment are necessary in order to minimize Therapeutic category: Neurotropic and psy-
used in the treatment of absence seizures in some cases 1.6–2 g daily may be
the risk of adverse effects. Valproate, although chotropic agent
(petit mal) and are usually well tolerated. needed.
effective, is not recommended because of the Indications: Generalized tonic-clonic and
However, ethosuximide can, rarely, cause lupus ELDERLY reduce initial dose; CHILD
greater risk of hepatotoxicity in young children. partial seizures; trigeminal neuralgia; bipolar
erythematosus and psychoses which call for 12–18 years, initially 100–200 mg
disorder (section 1.4.2).
immediate, but cautious, discontinuation. Ab- Status epilepticus 1–2 times daily, increased gradu-
Contra-indications: AV conduction abnor-
sence seizures are commonly associated with ally to usual maintenance dose of
Status epilepticus is a medical emergency malities; history of bonemarrow depression;
tonic-clonic seizures and valproate is preferred 400–600 mg 2–3 times daily; CHILD
which carries a high mortality rate. Initial man- porphyria.
since it is effective in both disorders. 1 month–12 years, initially 5 mg/
agement includes positioning the patient to Precautions: Hepatic impairment (Appendix
kg at night or 2.5 mg/kg twice daily,
TONIC SEIZURES, ATONIC SEIZURES AND ATYP- avoid injury, supporting respiration including 5); renal impairment (Appendix 4); cardiac
increased by 2.5–5 mg/kg every 3–7
ICAL ABSENCE SEIZURES provision of oxygen, maintaining blood pres- disease (see also Contra-indications); skin re-
days if necessary; usual maintenance
dose 5 mg/kg 2–3 times daily (up to Tablets, Carbamazepine 200 mg, 400 mg; s–r, f–c tremor, changes in libido, incontinence, uri- should be told how to recognize signs of blood
20 mg/kg daily may be needed). divisible tabs. nary retention; blood disorders and jaundice; disorders, and advised to seek immediate
Trigeminal neuralgia, by mouth, 200 mg - 50 hypotension and apnoea, pain and thrombo- medical attention if symptoms such as fever,
ADULT initially 100 mg 1–2 times 400 mg - 30. phlebitis (with injection). sore throat, mouth ulcers, bruising or bleeding
daily increased gradually according POM ZEPTOL® (Synergy) Advice to patients: May cause drowsiness. develop.
to response; usual dose 200 mg 3–4 Tablets, Carbamazepine 200 mg, 400 mg. Ability to operate machinery or drive may be Advice to patients: May cause drowsiness.
times daily with up to 1.6 g daily in 200 mg - 10’s impaired. Avoid alcoholic beverages. Ability to operate machinery or drive may be
some patients. 400 mg - 10’s Nursing action: See under Diazepam in Sec- impaired. Avoid alcoholic beverages.
Note: Plasma concentration for optimum response POM ZEPTOL CR® (Synergy) tion 1.1. Adverse effects: GI disturbances including
4–12 mg/litre (17–50 micromol/litre). Tablet, Carbamazepine 200 mg, 300 mg, 400 mg; Dose: Status epilepticus or emergency man- anorexia, hiccups, nausea and vomiting,
POM Carbamazepine (WMF 5) controlled release tabs. agement of recurrent epileptic seizures, epigastric pain (particularly during initial
Tablets, (scored), Carbamazepine 100 mg, 200 mg. 200 mg - 10’s by slow IV injection (at rate of 5 mg/ treatment); weight loss, drowsiness, dizziness,
Tablets, (chewable), Carbamazepine 100 mg, 200 mg. 300 mg - 10’s minute), ADULT 10–20 mg, repeated ataxia, headache, depression, mild euphoria;
Oral liquid, Carbamazepine 100 mg/5 mL. 400 mg - 10’s
if necessary after 30–60 minutes; may rarely, rash including Stevens-Johnson syn-
POM Carbamazepine (EDL 3) be followed by IV infusion to maxi- drome (erythema multiforme), systemic lupus
DIAZEPAM
Tablets, Carbamazepine 100 mg, 200 mg. mum 3 mg/kg over 24 hours; by slow erythematosus, disturbances of liver and renal
Drug subject to international control under the Conven- IV injection, CHILD 200 to 300 µg/kg function (see Precautions), haematological
POM Apo-Carbamazepine (Lahams)
tion on Psychotropic Substances (1971). (or 1 mg per year of age); by rectum disorders including leukopenia, agranulocy-
Tablet, Carbamazepine 200 mg; white, dou-
ble-scored bevel-edged tab. marked ‘APO 200’. Therapeutic category: Sedative/anticon- as solution, ADULT and CHILD over tosis, aplastic anaemia, thrombocytopenia,
200 mg - 100’s; 500’s. vulsant 10 kg, 500 µg/kg, ELDERLY 250 µg/kg; pancytopenia; gum hyperplasia, swelling
Indications: Status epilepticus; emergency repeated if necessary every 12 hours; of tongue, irritability, hyperactivity, sleep
EMDEX
POM CARBAMAL® (PharmacyPlus)
management of recurrent seizures; febrile if convulsions not controlled, other disturbances, night terrors, aggressiveness,
Tablets, Carbamazepine 200 mg, 400 mg; uncoated
tabs. convulsions; seizures associated with poison- measures should be instituted psychosis, increased libido, myopia, vaginal
200 mg - 10’s; 10 x 10’s; 500‘s; 1000’s (in blisters) ing and drug withdrawal; adjunct in acute Febrile convulsions (preferred bleeding, also reported.
400 mg - 10’s; 10 x 10’s (in blisters) alcohol withdrawal; premedication (section treatment), by rectum as solution [in- Nursing action: See notes above.
Oral suspension, Carbamazepine 100 mg per 5 mL; 3.2); anxiety disorders (section 1.1) jection solution may be used], CHILD Dose: Absence seizures, by mouth, ADULT
yellow susp. Contra-indications: Respiratory depression; over 10 kg, 500 µg/kg (maximum 10 and CHILD >6 years initially 500 mg
Pack: 100 mL mg), with dose repeated if necessary. daily, increased by 250 mg at intervals
acute pulmonary insufficiency; sleep apnoea;
POM CARBAMAL CR® (PharmacyPlus) severe hepatic impairment; myasthenia gravis; Febrile convulsions (alternative treat- of 4–7 days to a usual dose of 1–1.5
Tablets, Carbamazepine 200 mg, 400 mg; extend- avoid injections containing benzyl alcohol in ment), by slow IV injection, CHILD g daily (occasionally, up to max. of 2
ed-release uncoated tabs. neonates. 200–300 µg/kg (or 1 mg per year of g daily); CHILD <6 years initially 250
200 mg - 10 x 10’s
Precautions: Respiratory disease, muscle age). mg daily, increased gradually to usual
400 mg - 10 x 10’s Drug or alcohol withdrawal, by slow dose of 20 mg/kg daily.
weakness, history of alcohol or drug abuse,
POM Carbamazepine (Dabak) IV injection (at rate of 5 mg/minute), Administration: Daily doses of 1 g and above should
marked personality disorder; pregnancy (see
Tablet, Carbamazepine 200 mg; white round tab. ADULT 10 mg; higher doses may be be taken as 2 or more divided doses.
notes above; Appendix 2); breast-feeding (see
200 mg - 1000`s. required depending on severity of Note: Plasma concentration for optimum
notes above; Appendix 3); reduce dose in el-
symptoms. response 40–100 mg/L (300–700 micromol/L).
POM CARTOL® (Vixa) derly or debilitated and in hepatic impairment
Tablet, Carbamazepine 200 mg (avoid if severe, Appendix 5), renal impairment Seizures associated with poisoning, POM Ethosuximide (WMF 5)
200 mg - 1 x 10’s; 10 x 10’s (Appendix 4); avoid prolonged use and abrupt by slow IV injection (at rate of 5 mg/ Capsule, Ethosuximide 250 mg.
withdrawal; when given intravenously facili- minute), ADULT 10–20 mg. Oral liquid, Ethosuximide 250 mg/5 mL.
POM CARZEPIN® (Hovid)
Tablet, Carbamazepine 200 mg ties for reversing respiratory depression with POM Diazepam (WMF 5) POM Ethosuximide (EDL 3)
200 mg - 500’s. mechanical ventilation must be at hand (see Injection, Diazepam 5 mg/mL; in 2-mL ampoule. Tablet or Capsule, Ethosuximide 250 mg.
below); porphyria; interactions: Appendix 1. Oral liquid, Ethosuximide 250 mg per 5 mL.
POM EPICAR® (Reals) POM Diazepam (EDL 3)
Tablet, Carbamazepine 200 mg PRECAUTIONS FOR IV INFUSION: IV infusion of Injection, Diazepam 5 mg per mL; in 2-mL amp.
diazepam is potentially hazardous (especially GABAPENTIN
200 mg - 10’s See Diazepam in Section 1.1 for the proprietary
if prolonged) calling for close and constant Therapeutic category: Anticonvulsant.
POM GAMAPIN®-200 (Pharmabase) preparations.
observation and best carried out in a specialist Indications: As adjunctive therapy for partial
Tablet, Carbamazepine BP 200 mg; uncoated tab.
centre with intensive care facilities. Prolonged seizures with and without secondary gener-
intravenous infusion may lead to accumulation ETHOSUXIMIDE alization in adult and children (>6 years); as
POM KAMAZIPIN® (Kayhelt) and delay recovery. Indications: Absence seizures. monotherapy for partial seizures with and
Tablet, Carbamazepine 200 mg; uncoated tab. Adverse effects: Drowsiness and light-head- Precautions: Hepatic or renal impairment; without secondary generalization in adult and
200 mg- 10’s (in blisters)
edness the next day; confusion and ataxia blood counts and hepatic and renal function adolescent (>12 years); peripheral neuropathic
POM TEGRETOL® (Novartis) (especially in the elderly); amnesia; depend- tests recommended; pregnancy (see notes pain such as painful diabetic neuropathy and
Tablets, Carbamzepine 200 mg; white scored tab. ence; paradoxical increase in aggression; above; Appendix 2); breast-feeding (see notes post-herpetic neuralgia in adult.
marked ‘GEIGY’ and ‘GK’. muscle weakness; occasionally headache, above; Appendix 3); avoid sudden withdrawal; Contra-indications: Hypersensitivity to gab-
200 mg - 20; 100. porphyria; interactions: Appendix 1. apentin and/or excipients.
vertigo, salivation changes, GI disturbances,
POM TEGRETOL CR® (Novartis) skin reactions, visual disturbances, dysarthria, BLOOD DISORDERS: Patients or their carers Precautions: Gradual withdrawal over a period
of one week as sudden or abrupt withdrawal 3 times daily from day 3. PHENOBARBITAL 5–10 mg/kg at a rate of not more
may precipitate status epilepticus. May impair Recommended adult dose of Methyl- than 30 mg/minute.
Drug subject to international control under the Conven-
ability to perform skilled tasks. Monitor for cobalamin for peripheral neuropa- tion on Psychotropic Substances (1971).
Note: For therapeutic purposes phenobarbital
signs of suicidal ideation and behaviours. thies is 1500 mcg/day in 3 divided and phenobarbital sodium may be considered
Acute pancreatitis (discontinue). Patients with doses. Therapeutic category: Sedative/anticonvulsant equivalent in effect. Plasma concentration for
mixed seizures (not effective against primary Administration: To be given orally with or without Indications: Generalized tonic-clonic seizures; optimum response 15–40 mg/litre (65–170
generalized seizures such as absences and food. Dosage withdrawal should be gradual over a partial seizures; neonatal seizures; febrile con- micromol/litre).
may aggravate such seizures). Elderly; Children; minimum of 1 week. vulsions; status epilepticus (see notes above).
POM Phenobarbital (WMF 5)
Pregnancy & lactation; Renal dysfunction. May POM BIOPENTIN® (Biofem) Contra-indications: Porphyria; absence
Tablets, Phenobarbital 15-100 mg.
impair ability to perform skilled tasks. Tablet, Gabapentin 300 mg, methylcobalamin 500 seizures. Oral liquid, Phenobarbital (or as sodium salt) 15
Interactions: Morphine (increased CNS de- mcg; f-c tab. Precautions: Elderly, debilitated, children mg/5 mL
pression such as somnolence); antacids con- Pack:10 x10’s; 3 x 10’s (in blisters) (may cause behavioural changes); impaired Injection, Phenobarbital sodium 200 mg/mL.
taining aluminium and magnesium (reduced renal function (Appendix 4) or hepatic function
MAGNESIUM SULFATE POM Phenobarbital (EDL 3)
absorption of gabapentin, space out by at (Appendix 5), respiratory depression (avoid if Tablets, Phenobarbital 15 mg, 30 mg, 60 mg.
least 2 hours). See under section 11.1 severe); pregnancy (see notes above; Appendix Oral liquid, Phenobarbital 15 mg per 5 mL.
Adverse effects: GI upset e.g. N & V, dyspep- 2); breastfeeding (see notes above; Appendix
3); avoid sudden withdrawal; interactions: POM Phenobarbitone (Emzor)
sia; Somnolence, dizziness, ataxia, headache,
PARALDEHYDE Tablets, Phenobarbitone 15 mg, 30 mg, 60 mg; white
nystagmus, tremor; diplopia, vertigo; fatigue, Appendix 1.
biconvex tabs.
fever; rhinitis; reduced WBC count, weight gain; Therapeutic category: Hypnotic/anticon- Advice to patients: Advice to patients: May Pack: 100; 1000.
infection; anorexia, increased appetite. vulsant cause drowsiness. Ability to operate machin-
Indications: Status epilepticus. ery or drive may be impaired. Avoid alcoholic POM Phenobarbitone (Mopson)
Dose: By mouth, Epilepsy, Adult & child (≥ 12
EMDEX
Precautions: Bronchopulmonary disease or beverages. Tablet, Phenobarbitone 30 mg.
years), initially 300 mg once daily on Pack: 1000.
1st day; 300 mg 2 times daily on 2nd hepatic impairment, colitis, road users, avoid Adverse effects: Sedation, mental depres-
Syrup, Phenobarbitone 15 mg per 5 mL.
day; 300 mg 3 times daily on 3rd day. plastic syringes. sion, ataxia, nystagmus; allergic skin reactions Pack: 60 mL.
May increase dose by 300 mg/day Adverse effects: Injection is painful; skin including rarely, exfoliative dermatitis, toxic
rashes. epidermal necrolysis, Stevens-Johnson syn- POM Phenobarbitone (Vitabiotics)
every 2-3 days based on response &
Nursing action: Tablets, Phenobarbitone 30 mg.
tolerance up to a max. 3600 mg/day. drome (erythema multiforme); paradoxical
• Administer I.M. injection in a Z-track method deep 30 mg - 1000’s.
Child (≥ 6 years), initially 10-15 mg/ excitement, restlessness and confusion in the
into a mass of muscle, to prevent tissue sloughing. elderly; irritability and hyperactivity in children; POM PITROFIN® (Mopson)
kg/day; may increase to a max. 25-35
• Observe closely for respiratory depression; advise Tablet, Phenobarbitone 30 mg
mg/kg/day. megaloblastic anaemia (may be treated with
patient to avoid driving and other activities that 30 mg - 1000’s
Peripheral neuropathic pain, Adult, require alertness.
folic acid); osteomalacia; status epilepticus (on
Elixir, Phenobarbitone 15 mg per 5 mL
may titrate as above or start 300 mg 3 • May cause drug depecdence and severe with- treatment withdrawal); hypotension, shock,
Pack: 60 mL
times daily; up to max. 3600 mg/day. drawal symptoms. laryngospasm and apnoea (with intravenous
Elderly & renal impairment: Dosage • Avoid contact with rubber and plastic; use glass injection). PHENYTOIN
adjustment based on creatinine syringe and bottle for parental dose. Nursing action:
• Do not use paraldehyde if it has a brownish colour • Institute safety measures to avoid injuries; observe Indications: Generalized tonic-clonic seizures;
clearance.
or an odour of acetic acid, or if the container has patient for excessive sedation and respiratory partial seizures; status epilepticus.
Note: The total daily dose should be divided in three
single doses, the maximum time interval between been open longer than 24 hours. Always use fresh depression. Contra-indications: Porphyria; avoid par-
the doses should not exceed 12 hours to prevent supply and avoid exposure to air. • Warn patient not to discontinue drug abruptly enteral use in sinus bradycardia, sinoatrial
breakthrough convulsions. Dose: By deep IM injection, as a single dose, but to inform physician immediately if adverse block, second- and third-degree heart block,
Adult , 5-10 mL; up to a max. 20 mL reactions occur. Stokes-Adams syndrome.
(Additional information sourced from Neurontin® monograph: • Teach patient that drug may cause physical and
http://www.medicines.org.uk) daily (do not give more than 5 mL at Precautions: Hepatic impairment (reduce
psychological dependence and he/she should not
any one site). dose; Appendix 5); pregnancy (important, see
alter dose without notifying physician.
POM OVABA® (CG Biostadt) Child ( up to 3 months), as a single notes above; Appendix 2); breast-feeding (see
Dose: Generalized tonic-clonic seizures, partial
Capsules, Gabapentin 100 mg, 300 mg, 400 mg. dose, 0.5 mL; 3 - 6 months, 1 mL; 6 -12 notes above; Appendix 3); diabetes mellitus;
100 mg - 30’s seizures, by mouth, ADULT 60–180 mg
months, 1.5 mL; 1-2 years, 2 mL; 3-5 monitor blood counts; hypotension and heart
300 mg - 30’s at night; CHILD up to 8 mg/kg daily.
years, 3-4 years, 6-12 years, 5-6 mL. failure (caution with parenteral use); IV ad-
400 mg - 30’s Febrile convulsions, by mouth, CHILD
By IV infusion, not recommended. ministration—resuscitation facilities must be
up to 8 mg/kg daily
By rectum, Adult, 5-10 mL; admin- available; injection solution alkaline (irritant to
GABAPENTIN plus METHYLCOBALAMIN Neonatal seizures, by IV injection
istered as a 10% enema in normal tissues); interactions: Appendix 1.
Indications: Treatment of diabetic and non-di- (dilute injection 1 in 10 with water
saline. May also be diluted with BLOOD OR SKIN DISORDERS: Patients or their
abetic neuropathic pain and post-herpetic for injections), NEONATE 5–10 mg/
arachis oil or olive oil 1:2 and given as carers should be told how to recognize signs
neuralgia. kg every 20–30 minutes up to plasma
retention enema of blood or skin disorders and advised to seek
Contra-indications, Precautions, Interac- concentration of 40 mg/litre
Child, as for IM dose. immediate medical attention if symptoms such
tions, Adverse effects: See under Gabapentin. Status epilepticus, by IV injection
POM Paraldehyde (EDL 3) as sore throat, rash, mouth ulcers, bruising or
Dose: By mouth, Adult, initially 1 tablet once (dilute injection 1 in 10 with water for
Injection, Paraldehyde in 5-mL, 10-mL amps. bleeding develop. Leukopenia which is severe,
daily on day 1; increased to 1 tablet injections), ADULT 10 mg/kg at a rate
progressive or associated with clinical symp-
twice daily on day 2 and then 1 tablet of not more than 100 mg/minute (up
toms requires withdrawal (if necessary under
to maximum total dose of 1 g); CHILD
cover of suitable alternative). daily in 2 divided doses, increased Indications: Treatment of central and peripheral Hepatic impairment: No dosage
Adverse effects: Gastric intolerance, head- gradually according to clinical neuropathic pains in adults. Adjunctive therapy adjustment.
ache, sleeplessness, agitation (during initial response and plasma-phenytoin con- in adults with partial seizures with or without Administration: May be taken with or without meal
phase); sedation, confusion, blurred vision, centration; usual dose range 4–8 mg/ secondary generalization. Generalized anxiety Dosage adjustment in renal impairment:
ataxia, nystagmus, diplopia, slurred speech, kg daily (maximum 300 mg daily). disorder (GAD) in adults. Total daily dose
CC (mL/min)
cerebellar-vestibular symptoms, behavioural Status epilepticus, by slow IV injection Contra-indications: Hypersensitivity to any regimen Start. dose Max.dose Dose
disorders, hallucinations, hyperglycaemia (may or by IV infusion (with BP and ECG component of the preparation; Pregnancy (mg/day) (mg/day)
be signs of overdosage); gingival hyperplasia, monitoring), ADULT 15 mg/kg at a & Lactation. Counsel women child bearing >60 doses 150 600 2-3 divided
acne, coarse facies, hirsutism, fever, hepatitis, rate of not more than 50 mg/min- potential on effective contraception. >30 - <60 doses 75 300 2-3 divided
neurological changes (peripheral neuropathy, ute, as a loading dose; maintenance Precautions: Avoid use in patients with rare >15 - <30 doses 25-50 150 1-2 divided
choreiform movements, impaired cognition, doses of about 100 mg by mouth hereditary problems of galactose intolerance, <15 25 75 once daily
increased seizure frequency); osteomalacia, or by slow IV injection should be the Lapp lactase deficiency or glucose-galac- Note: Discontinuation of pregabalin: In all indications,
rickets (associated with reduced plasma cal- given thereafter at intervals of 6–8 tose malabsorption. Diabetes (may need to it is recommended this should be done gradually
cium levels); lymph-node enlargement; ver- hours, monitored by measurement adjust dose of hypoglycaemic medications if over a minimum of 1 week.
tigo; rashes (discontinue; if mild re-introduce of plasma concentrations; rates and patient gains weight). Dizziness, somnolence POM LIGABA® (Mega lifesciences)
cautiously, but discontinue if recurrence); very dose reduced according to weight; (may affect ability to drive or operate machin- Capsules, Pregabalin 25 mg, 50 mg, 75 mg, 300 mg.
rarely, Stevens-Johnson syndrome (erythema CHILD 15 mg/kg as a loading dose at ery). Blurred vision (regular vision check is Pack: 3 x 10’s (in blisters)
multiforme), systemic lupus erythematosus, rate of 1 mg/kg/minute (not exceed- recommended). CVD (may cause CHF). Renal
POM LYRICA® (Pfizer)
toxic epidermal necrolysis; rarely blood disor- ing 50 mg/minute); NEONATE 15–20 impairment; Elderly; Children. Capsules, Pregabalin 25 mg, 75 mg.
ders including megaloblastic anaemia (may be mg/kg as a loading dose at rate of Interactions: May potentiate CNS depressant 25 mg - 28’s (in blister)
treated with folic acid), leukopenia, thrombocy- 1–3 mg/kg/minute. effects of oxycodone, lorazepam, ethabol. 75 mg - 28’s (in blister)
EMDEX
topenia, agranulocytosis with or without bone Note: Plasma concentration for optimum response Adverse effects: Most commonly dizziness and
10–20 mg/litre (40–80 micromol/litre). The pres- POM PREGASAFE® (Phillips)
marrow depression; IV administration—cardi- somnolence. Less commonly increased appe- Capsules, Pregabalin 25 mg, 50 mg, 75 mg, 150
ovascular and CNS depression (particularly if ence of both the 25 mg/5 mL and the 30 mg/5 mL tite, euphoric mood, confusion, decreased li-
strengths of the oral liquid on the same market mg, 300 mg.
administered too rapidly) with arrhythmias, bido, irritability, ataxia, disturbance in attention, Pack: 10’s (in blisters)
should be avoided to prevent confusion in prescrib-
hypotension and cardiovascular collapse, ing and dispensing
abnormal coordination, memory impairment,
alterations in respiratory function (including tremor, dysarthria, paraesthesia, blurred vision, TOPIRAMATE
respiratory collapse). POM Phenytoin (WMF 5) diplopia, vertigo, dry mouth, constipation, vom-
Tablets, Phenytoin sodium 25 mg, 50 mg, 100 mg. Therapeutic category: Anticonvulsant; An-
Advice to patients: May cause drowsiness. iting, flatulence, erectile dsyfunction, fatigue, timigraine preparation.
Tablet, (chewable), Phenytoin 50 mg.
Ability to operate machinery or drive may be peripheral oedema, feeling drunk, oedema, Pharmacology: Topiramate is a sulfamate
Capsules, Phenytoin sodium 25 mg, 50 mg, 100 mg.
impaired. Avoid alcoholic beverages. Patient Oral liquid, Phenytoin 25-30 mg/5 mL. . abnormal gait, increased weight. substituted monosaccharide. It produces
should take medication with plenty of water. Injection, Phenytoin sodium 50 mg/mL; in 5-mL vial. Dose: By mouth, Adult, usually 150-600 mg anticonvulsant activity through the following
Nursing action: daily in 2-3 divided doses. May be three actions: Blockade of state-dependent
• Give orally, after meals, in divided doses to prevent POM Phenytoin Sodium (EDL 3) taken with or without food.
Tablets or Capsules, Phenytoin sodium 25 mg, 50 sodium channel resulting in decreased num-
averse GI reactions; advise patient not to stop Neuropathic pain, Initially 150 mg/
drug abruptly (seizures may occur) and also not mg, 100 mg. ber of action potentials produced by sustained
daily in 2-3 divided doses; depending neuronal depolarization. It increases the activity
to change brand or dosageform without notifyig POM EPITOIN® (Hovid) on patient’s response and tolerance, of GABA (an inhibitory neurotransmitter) at
physician. Capsule, Phenytoin sodium 100 mg
• Discontinue drug if rash appears and notify the
may increase to 300 mg/day after a GABAA receptors. It antagonizes the ability of
100 mg - 1000.
physcian. 3-7 days interval; if necessary, further kainate to activate the kainate/AMPA subtype of
• Stress the importance of oral hygiene and regular POM FRATIN® (Embassy) increase to a max. 600 mg/day after excitatory amino acid (glutamate) receptor, but
dental examintion to minimise the development Capsule, Phenytoin sodium 100 mg. an additional 7-day interval had no apparent effect on the activity of NMDA
of gingival hyperplasia. Pack: 10 x 10’s (in blisters). Epilepsy, Initially 150 mg/day in 2-3 di- at the NMDA receptor subtype. Additionally,
• Caution patient on the use of other drugs or POM Phenytoin Sodium (Alpha) vided doses; depending on patient’s topiramate causes inhibition of some isoen-
alcoholic beverages without first seeking the Injection, Phenytoin sodium 250 mg; solution for response and tolerance, may increase
physician’s advice. Alcohol may diminish the effect zymes of carbonic anhydrase (much weaker
injection. to 300 mg/day after 1 week. Max: 600 inhibitor than Acetazolamide), but this action
of the drug
mg/day after an additional 1 week. does not contribute much to its anticonvulsant
• Patient should avoid activities that require mental
PREGABALIN Generalised anxiety disorder, Initially
alertness and physical coordination until the CNS activity.
effects of the drug are established. Therapeutic category: Anticonvulsant. 150 mg/day in 2-3 divided doses; Absorption of topiramate is rapid and extensive.
• Drug may colour urine pink, red, or reddish-brown. Pharmacology: Pregabalin is a GABA analogue. depending on patient’s response and Cmax of 1.5 mcg/mL is achieved in 2-3 hours
Dose: Generalized tonic-clonic seizures, partial It binds to an auxiliary subunit (alpha delta tolerance, may increase to 300 mg/ (Tmax) after oral administration of 100 mg. Com-
seizures, by mouth, ADULT initially protein) of voltage-gated calcium channels in day after 1 week. May increase further pared to other antiepileptic drugs, topiramate
3–4 mg/kg daily (as a single dose or in the central nervous system, potently displacing to 450 mg/day after another 1 week. has long plasma half-life, linear pharmacoki-
2 divided doses), increased gradually gabapentin. It is rapidly absorbed when given Max: 600 mg/day after an additional netics, predominantly renal clearance, absence
at intervals of 2 weeks as necessary in a fasted state with the oral bioavailability 1 week of significant protein binding, and lack of
(with plasma-phenytoin concentra- reaching >90%. Metabolism in humans is mini- Chlidren and adolescents (12-17 years): clinically relevant active metabolites. It is not a
tion monitoring); usual dose 200–500 mal and approx. 98% is excreted unchanged in Not recommended. potent inducer of drug metabolizing enzymes,
mg daily; CHILD initially 3–5 mg/kg the urine. Its clearance is directly proportional Elderly (>65 years): Adjust dose based can be administered without regard to meals,
to creatinine clearance. on creatinine clearance
and routine monitoring of plasma topiramate slowly at 1- or 2-week intervals by 25- VALPROIC ACID forme), vasculitis, hirsutism and acne reported.
concentrations is not necessary. 50 mg/day, in 2 divided doses. Usual Synonym: Sodium valproate. Advice to patients: Take with food or milk;
Indications: Monotherapy in adults and chil- range: 100-200 mg/day in 2 divided Indications: All forms of epilepsy; acute mania do not chew, break or crush the tablet or
dren (>6 years) with partial seizures with or doses. Max. 500 mg/day in 2 divided (section 1.4.2). capsule to avoid local irritation of the mouth
without secondary generalised seizures, and doses. Contra-indications: Active liver disease, family and throat; do not administer with carbonated
primary generalised tonic-clonic seizures. Children (>6 years): initially 0.5-1 mg/ history of severe hepatic dysfunction; pancre- drinks as it may irritate the mouth and throat;
Adjunctive therapy in children adults and chil- kg nightly for 1 week. Increase slowly atitis; porphyria. report any sore throat, fever or fatigue, bleed-
dren (>2 years) with partial onset seizures with at 1- or 2-week intervals by 0.5-1 mg/ Precautions: Monitor liver function before and ing or bruising that is severe or that persists;
or without secondary generalization or primary kg/day, in 2 divided doses. Usual during first 6 months of therapy (Appendix 5), may cause drowsiness, impair judgement or
generalized tonic-clonic seizures. Treatment range: 100 mg/day or 2 mg/kg/day in especially in patients at most risk (children co-ordination.
of seizures associated with Lennox-Gastaut 2 divided doses. under 3 years of age, those with metabolic dis- Nursing action:
syndrome. Prophylaxis of migraine headache; Adjunctive therapy epilepsy, Adult, orders, degenerative disorders, organic brain • Administer tablets or capsules whole; give elixir
not recommended for acute treatment. initially 25-50 mg nightly for 1 week. alone and do not dilute it.
disease or severe seizure disorders associated
Contra-indications: Hypersensitivity to any Increase slowly at 1- or 2-week inter- • Instruct patient not to discontinue drug abruptly
with mental retardation, or multiple antiep- after a long period of use, since convulsions may
ingredient of the product. Not indicated for vals by 25-50 mg/day, in 2 divided ileptic therapy); ensure no undue potential occur.
migraine prophylaxis in pregnancy or women doses. Usual range: 200-400 mg/day for bleeding before starting and before major Dose: All forms of epilepsy, by mouth, ADULT
of child bearing age without adequate con- in 2 divided doses. Max. 800 mg/day surgery or anticoagulant therapy; renal im- and CHILD over 12 years, initially
traception. in 2 divided doses. pairment (Appendix 4); pregnancy (important 600 mg daily in 2 divided doses,
Precautions: Discontinue gradually at the rate Children (≥2 years): initially 25 mg/ see notes above; Appendix 2 (neural tube preferably after food, increased by
of 100 mg/day at weekly intervals. Maintain ad- kg nightly for 1 week. Increase slowly screening)); breastfeeding (see notes above; 200 mg daily at 3-day intervals to
equate hydration to reduce the risk of nephro- at 1- or 2-week intervals by 1-3 mg/ Appendix 3); systemic lupus erythematosus; maxi. of 2.5 g daily in divided doses;
EMDEX
lithiasis especially in those with predisposition. kg/day, in 2 divided doses to achieve false-positive urine tests for ketones; avoid usual maintenance dose 1–2 g daily
Ensure proper hydration before and during optimal response. Usual range: 5-9 sudden withdrawal; interactions: Appendix 1. (20–30 mg/kg daily); CHILD up to 20
activities or exposure to warm temperatures. mg/kg/day in 2 divided doses. Max. BLOOD OR HEPATIC DISORDERS: Patients or kg, initially 20 mg/kg daily in divided
Monitor for signs of suicide. Monitor for acute 30 mg/kg/day. their carers should be told how to recognize doses, may be increased provided
myopia and increased intraocular pressure Migraine prophylaxis, Adult (>16 signs of blood or liver disorders, and advised plasma concentrations monitored
(discontinue if symptoms occur). Decrease years), initially 25 mg nightly for to seek immediate medical attention if symp- (above 40 mg/kg daily also monitor
in serum bicarbonate levels and associated 1 week. Increase slowly at 1-week toms including loss of seizure control, malaise, clinical chemistry and haematological
metabolic acidosis may occur (measure serum intervals by 25 mg/day, in 2 divided weakness, anorexia, lethargy, oedema, vomit- parameters); CHILD under 12 years,
bicarbonate periodically). Weight loss; lactose doses. Usual range: 50-100 mg/day in ing, abdominal pain, drowsiness, jaundice, or over 20 g, initially 400 mg daily in
or sucrose intolerance. May impair ability to 2 divided doses. Max. 200 mg/day in spontaneous bruising or bleeding develop. divided doses, increased until control
drive or operate machinery. Renal or hepatic 2 divided doses. PANCREATITIS: Patients or their carers should (usually in range of 20–30 mg/kg
dysfunction (clearance may be decreased). Children: Not recommended be told how to recognize signs of pancreatitis daily); maximum 35 mg/kg daily.
Pregnancy, lactation. Renal impairment: Lower doses. and advised to seek immediate medical at- Note: Plasma concentrations in therapeutic range
Interactions: Use with other AEDs e.g. carba- Patients on haemodialysis: administer tention if symptoms such as abdominal pain, of 40–100 mg/litre (280 to 700 micromol/litre); not
mazepine, phenytoin may decrease plasma level a supplemental dose of approx. one- nausea and vomiting develop; discontinue generally considered useful in assessing control, but
of topiramate. Coadministration with valproic half the daily dose in divided doses at sodium valproate if pancreatitis diagnosed. higher levels associated with increased incidence
acid may increase risk of hyperammonemia the beginning and completion of the Adverse effects: GI irritation, nausea, increased of adverse effects; indicator of compliance, dose
with or without encephalopathy. Increased haemodialysis procedure. appetite and weight gain, hyper-ammonaemia; change or co-medication.
drowsiness may occur with alcohol and other Hepatic impairment: May adjust dose. ataxia, tremor; transient hair loss (regrowth POM Valproic acid (WMF 5)
CNS depressants. Decreased contraceptive Elderly: May need dosage adjustment may be curly); oedema, thrombocytopenia, Tablets, (enteric-coated), Sodium valproate 200
efficacy in women on combined oral contracep- depending on renal function. inhibition of platelet aggregation; impaired mg, 500 mg.
tives. Monitor digoxin and lithium levels when Note: Discontinue gradually to minimize the poten- hepatic function and rarely fatal hepatic failure Tablets, (crushable), Valproic acid 100 mg.
coadministered with topiramate. Monitor for tial for seizures or increased seizure frequency. Daily Oral liquid, Valproic acid 200 mg/5 mL.
(see Precautions: withdraw treatment immedi-
glycaemic control in patients on oral antidia- dosages should be decreased in weekly intervals
by 50-100 mg in adults with epilepsy and by 25-50
ately if malaise, weakness, lethargy, oedema, POM Sodium Valproate (EDL 3)
betic agents. Increased risk of nephrolithiasis abdominal pain, vomiting, anorexia, jaundice, Tablets, Sodium valproate 100 mg, 200 mg, 500 mg;
mg in adults receiving topiramate at doses up to
with carbonic anhydrase inhibitors. 100 mg/day for migraine prophylaxis. In children, drowsiness or loss of seizure control); sedation enteric-coated tablets.
Adverse effects: Nausea, diarrhea, abdomi- gradual withdrawal over a 2-8 week period is rec- reported and also increased alertness; behav- Oral liquid, Sodium valproate 200 mg per 5 mL.
nal pain; anorexia, weight loss; somnolence, ommended. ioural disturbances; rarely pancreatitis (see POM ENCORATE® (Synergy)
fatigue, pyrexia, oligohidrosis, nervousness, Precautions: measure plasma amylase if acute Tablets, Sodium valproate 200 mg, 300 mg, 500
(Additional information sourced from Topamax® monograph:
paraesthesia, dizziness; abnormal vision, http://www.medicines.org.uk/) abdominal pain), extrapyramidal symptoms, mg; e-c tabs.
diplopia; depression, confusion, mood swings; blood disorders (see Precautions: leukopenia, 200 mg - 10’s
metabolic acidosis; nasopharyngitis; nephro- POM HITOP® (CG Biostadt) pancytopenia, red cell hypoplasia, fibrinogen 300 mg - 10’s
lithiasis; anemia. Tablets, Topiramate 25 mg, 50 mg, 100 mg. 500 mg - 10’s
reduction); irregular periods, amenorrhoea,
Dose: Topamax can be taken without regard 25 mg - 30’s gynae-comastia, hearing loss, Fanconi syn- POM EPILIM® (Sanofi-Aventis)
to meals. 50 mg - 30’s Tablet, Sodium valproate 200 mg; e-c tab.
drome, dementia, toxic epidermal necrolysis,
Monotherapy epilepsy, Adult, initially 100 mg - 30’s 200 mg – 100’s
Stevens-Johnson syndrome (erythema multi-
25 mg nightly for 1 week. Increase Tablet (CR), Sodium valproate 500 mg; controlled-re-
66 | 1.8 Analgesics 1.8.1 Non-opioid analgesics and antipyretics | 67
lease tab. • The main goals of pain management are to reduce, Adjuvant therapy for mild to moderate pain including headache
500 mg – 100’s control, and prevent pain. Adjuvant therapy can enhance analgesic and acute migraine attacks (section 1.9) and for
Syrup, Sodium valproate 200 mg per 5 mL; red syrup. • A full assessment of the pain should be undertaken efficacy, treat concurrent symptoms, and/or reducing fever, including post-immunization
Pack: 300 mL and where possible, the underlying cause should provide independent analgesic activity for pyrexia. Paracetamol is particularly useful in
be determined and treated.
POM EPIVAL® (PharmacyPlus) specific types of pain. Examples include: patients in whom salicylates or other NSAIDs
• Use of nondrug measures in combination with
Tablet, Sodium valproate 200 mg; e-c tab. • Anticonvulsants (gabapentin), Tricyclic antidepres- are contraindicated, such as asthmatics and
drug therapy
200 mg - 10 x 10’s. sants (amitriptyline), Ketamine, and Clonidine for those with a history of peptic ulcer, or for
• Analgesics should be administered at regular
neuropathic pain. children under the age of 16 years in whom
POM VALCONTIN® (Phillips) intervals (“around the clock”) especially for pain
• Benzodiazepines for painful muscle spasms
Tablet , (200 mg), Sodium valproate 133.5 mg, that is expected to be constant. PRN dosing should salicylates should be avoided because of the
• In cancer patients, bisphosphonates and radiation
valproic acid 58 mg; white to off-white scored f-c be used for breakthrough pain only. risk of Reye syndrome. It is generally preferred
therapy may be useful adjuvants in managing
tab. marked “VLC”. • Potential adverse effects and interactions involving to acetylsalicylic acid, particularly in the elderly,
bone pain.
200 mg - 10 x 10’s (in aluminium strip) analgesics should be anticipated and managed because it is less irritant to the stomach. Unlike
Tablet , (300 mg), Sodium valproate 200 mg, valproic accordingly.
1.8.1 Non-opioid analgesics acetylsalicylic acid and other NSAIDs, paraceta-
acid 87 mg; white to off-white f-c caplet marked • The choice and dose of analgesic should match the
pain severity and should be individualised. Use of and antipyretics mol has little anti-inflammatory activity which
“VLC” on one side and “300” on the reverse.
300 mg - 10 x 10’s (in aluminium strip) stepwise WHO analgesic ladder is recommended. limits its usefulness for long-term treatment of
Non-opioid analgesics with anti-inflammatory
Tablet , (500 mg), Sodium valproate 333 mg, valproic • Oral analgesics should be used whenever possible pain associated with inflammation; however it
activity include salicylates such as acetyl-sali-
acid 145 mg; white to off-white scored f-c caplet to avoid painful routes of administration. Avoid IM is useful in the management of osteoarthritis,
cylic acid and other nonsteroidal anti-inflam-
marked “VLC” if possible especially in children. a condition with only a small inflammatory
• Equianalgesic doses should be used when switch- matory drugs such as ibuprofen. Non-opioid
500 mg - 10 x 10’s (in aluminium strip) component. In normal doses adverse effects
ing from one opioid to another. analgesics with little or no anti-inflammatory
are rare, but overdosage with a single dose
• Adjuvant therapy may be used at any point on activity include paracetamol.
1.8 Analgesics of 10–15 g is particularly dangerous because
EMDEX
the analgesic ladder e.g., anticonvulsants for Acetylsalicylic acid
1.8.1 Non-opioid analgesics and antipyretics it may cause hepatocellular necrosis and, less
neuropathic pain.
1.8.2 Opioid analgesics The principal effects of acetylsalicylic acid are frequently, renal tubular necrosis.
Non-drug treatments for pain anti-inflammatory, analgesic, antipyretic and
Pain may be modified by psychological factors • Sweet solutions such as sucrose and glucose can ACETYLSALICYLIC ACID
and attention to these is essential in pain man- antiplatelet. Oral doses are absorbed rapidly
reduce procedural pain in neonates and young
infants, especially single painful procedure. Exam- from the gastrointestinal tract; rectal absorp- Synonym: Aspirin; ASA.
agement. Drug treatment aims to modify the
ple is 2 mL of 25% Sucrose solution given with a tion is less reliable but suppositories are useful Therapeutic category: Analgesic; Anti-inflam-
peripheral and central mechanisms involved in
dropper <2 minutes before procedure. Suckling in patients unable to take oral dosage forms. matory Agent; Antipyretic; NSAID.
the development of pain. Neuropathic pain may
from breast/pacifier may be a healthier option. Acetylsalicylic acid is used for the management Indications: Mild to moderate pain includ-
respond only partially to conventional analgesics;
• Immobilisation by splinting, bandaging or ele- of mild to moderate pain such as headache, ing dysmenorrhoea, headache; pain and
treatment can be difficult and includes the use vation can alleviate pain and promote healing in acute migraine attacks (section 1.9), transient inflammation in rheumatic disease and other
of carbamazepine (section 1.7) for trigeminal musculoskeletal injury. musculo-skeletal pain and dysmenorrhoea, musculoskeletal disorders (including juvenile
neuralgia and amitriptyline (section 1.4.1) for • Physical measures may be used as appropriate
and for reducing fever. Although it may be used arthritis); pyrexia; acute migraine attack (sec-
diabetic neuropathy andpostherpetic neuralgia. namely Heat and/or Cold stimulation (avoid in
in higher doses in the management of pain and tion 1.9); antiplatelet (section 5.6).
Non-opioid analgesics (section 1.8.1) are neonates), Massage, Pressure, Swaddling (for ne-
onates). Example cold compress for sprains, warm inflammation of rheumatoid arthritis, other Contra-indications: Hypersensitivity (includ-
particularly suitable for musculoskeletal pain
compress for earache. NSAIDs are preferred because they are likely ing asthma, angioedema, urticaria or rhinitis)
whereas the opioid analgesics (section 1.8.2)
• Behavioural measures such as exercise, relaxation, to be better tolerated. Acetylsalicylic acid is to acetylsalicylic acid or any other NSAID;
are more suitable for moderate to severe
play therapy. also used for its antiplatelet properties (section children and adolescents under 16 years (Reye
visceral pain. Non-opioid analgesics which
• Cognitive measures such as distraction may also 5.6). Adverse effects with analgesic doses are syndrome—see also notes above); previous
also have anti-inflammatory actions include be effective. generally mild but include a high incidence or active peptic ulceration; haemophilia and
salicylates and other nonsteroidal antiinflam-
Selecting effective analgesic agent of gastrointestinal irritation with slight blood other bleeding disorders; not for treatment
matory drugs (NSAIDs); they can reduce both
A stepwise approach using WHO analgesic loss, bronchospasm and skin reactions in hy- of gout.
pain and inflammation of chronic inflammatory
ladder is recommended. The choice and dose persensitive patients, and increased bleeding Precautions: Asthma, allergic disease; renal
disorders such as rheumatoid arthritis, but
of the analgesic is based on pain severity. time. Anti-inflammatory doses are associated impairment (Appendix 4); hepatic impairment
they do not alter or modify the disease process
Balanced analgesia or multimodal analgesia with a much higher incidence of adverse (Appendix 5); pregnancy (Appendix 2); breast-
itself. For the management of rheumatoid
is the use of multiple analgesics with different reactions, and they also cause mild chronic feeding (Appendix 3); elderly; G6PD-defi-
arthritis disease-modifying antirheumatic
mechanisms or sites of action. This has been salicylism which is characterized by tinnitus ciency; dehydration; interactions: Appendix 1.
drugs (DMARDs) may favourably influence the
shown to improve pain relief and reduce opioid and deafness. Acetylsalicylic acid should be Adverse effects: Generally mild and infre-
disease process (section 2.1.2).
consumption and thereby their adverse effects. avoided in children under 16 years, unless quent for lower doses, but common with
The pain and inflammation of an acute attack
Example is the combination of Paracetamol specifically indicated (for example juvenile anti-inflammatory doses; GI discomfort or
of gout is treated with a NSAID (section 2.2.1)
and NSAID. arthritis), because of an association with Reye nausea, ulceration with occult bleeding (oc-
or colchicine [not included on WHO Model List];
• Step 1 (Mild pain) - Non-opioids e.g., Paracetamol syndrome (encephalopathy and liver damage); casionally major haemorrhage); also other
a xanthine-oxidase inhibitor (section 2.2.2) is
and NSAIDs. it should particularly be avoided during fever haemorrhage (including subconjunctival);
used for long-term control of gout. • Step 2 (moderate pain) - “Weak” opioids (e.g., or viral infection in children and adolescents. hearing disturbances such as tinnitus (rarely
Guidelines for pain management Codeine, Tramadol) ± Non-opioids. deafness), vertigo, confusion, hypersensitivity
• Step 3 (Severe pain) - “Strong” opioids (e.g., Mor- Paracetamol
See EMDEX Paediatric Drug Guide for detailed reactions (angioedema, bronchospasm and
phine) ± Non-opioids. Paracetamol is similar in analgesic and anti-
guidelines for pain and fever management in children. rash); increased bleeding time; rarely oedema,
pyretic efficacy to acetylsalicylic acid. It is used
68 | 1.8.1 Non-opioid analgesics and antipyretics 1.8.1 Non-opioid analgesics and antipyretics | 69
myocarditis, blood disorders (particularly Injection, Acetylsalicylic acid 0.5 g; powder for OTC HEDEX® (GSK) 5); renal impairment; alcohol dependence;
thrombocytopenia). injection. Tablet, Acetylsalicylic acid 500 mg; white cap- breastfeeding (Appendix 3); overdosage:
Advice to patients: May administer with meals Pack: 6’s, 20’s sule-shaped tab. section 19.2.1; interactions: Appendix 1.
to lessen GI upset. Oral solution, Acetylsalicylic acid 500 mg, 1000 mg; Adverse effects: Rare but rashes and blood
OTC MYOPRIN® (Michelle Lab)
powder for reconstitution.
Nursing action: Tablet, Acetylsalicylic acid 75 mg disorders reported; important: liver damage
Pack: Sachets 20’s
• Administer with food, milk, antacid, or large glass 75 mg - 10 x 10’s (in blisters) (and less frequently renal damage) following
of water to minimize GI distress. OTC Aspirin (BCN) overdosage.
OTC NASMOPRIN® (NASDMU)
• Watch for bleeding gums or any signs of GI bleed- Tablet, Acetylsalicylic acid 300 mg. Advice to patients: Do not take more than
Tablet, Acetylsalicylic acid 300 mg; white shallow
ing particularly in patients on large doses and/or 300 mg - 1000.
concave tab. marked “NASMOPRIN” on one side and 500 mg x 8 tablets per day (i.e., >4g/day). May
prolonged therapy.
• Co-administration with alcohol, steroids or other
OTC Aspirin (Dizpharm) “NASDMU” on the reverse. cause severe liver damage if taken in overdose
Caplet, Acetylsalicylic acid 300 mg. 300 mg - 1000. or with alcoholic beverages.
NSAIDs may increase risk of GI bleeding.
300 mg – 1000. Nursing action:
• Teach patient to avoid other OTC medications OTC PHENSIC® (GSK)
unless on doctor’s or pharmacist’s supervision. OTC Aspirin (Gemini) Tablet, Acetylsalicylic acid 300 mg; white tab. marked • Give with food or milk to reduce GI upset if
• Advise patient to notify physician if ringing in ears Tablet, Acetylsalicylic acid 300 mg. ‘PHENSIC’ on both sides. necessary.
or persistent GI pain occurs. 300 mg - 30; 100. 300 mg – 4 x 15 (in blister). • Large doses, prolonged use or excessive consump-
• Encourage patient to use soft tooth brush. tion of alcohol can cause liver damage.
OTC Aspirin (Hochiez) OTC PROPON® (Pharchem) • Warn patient to avoid use in high fever, fever
Dose: Mild to moderate pain, pyrexia, by
Tablet, Acetylsalicyclic acid 75 mg Tablet, Acetylsalicylic acid 300 mg; pink scored tab. persisting longer than 3 days, or recurrent fever
mouth with or after food, ADULT 75 mg - 28’s’; 100’s. marked ‘PIL’. without consulting a doctor.
300–900 mg every 4–6 hours if 300 mg - 10 x 10’s; 1000’s. • Teach patient symptoms of overdosage namely
necessary; maximum 4 g daily; CHILD OTC Aspirin (Juhel)
Tablet, Acetylsalicylic acid 300 mg. OTC STOP-EKE® (GoldMoore) nausea, vomiting, abdominal pain; to report to
under 16 years not recommended doctor immediately.
300 mg - 1000. Tablet, Acetylsalicylic acid BP 300 mg; f-c tab.
EMDEX
Mild to moderate pain, pyrexia, by Dose: Post-immunization pyrexia, by mouth,
300 mg - 10 x 10’s.
rectum, ADULT 600–900 mg inserted OTC Aspirin (May & Baker) INFANT 2–3 months, 60 mg followed
every 4 hours if necessary; max. 3.6 Tablet, Acetylsalicylic acid 300 mg. OTC TOPTABS® (SKG)
by a second dose, if necessary, 4–6
g daily; CHILD under 16 years not 300 mg - 1000. Tablet, Acetylsalicylic acid 350 mg, caffeine 30 mg;
white uncoated tab. marked with an ‘AXE’ and ‘TREE’
hours later; warn parents to seek
recommended. OTC Aspirin (Rajrab) medical advice if pyrexia persists after
logo on one face.
Inflammatory arthritis, by mouth with Tablet, Aspirin 300 mg; white scored tab. marked
Pack: 25 x 2’s. second dose.
or after food, ADULT 4–8 g daily in with company logo. Mild to moderate pain, pyrexia, by
divided doses in acute conditions; 300 mg - 1000’s
ASPIRIN plus CODEINE mouth, ADULT 0.5–1 g every 4–6
up to 5.4 g daily may be sufficient in OTC Aspirin (Ranbaxy) hours, maximum 4 g daily; CHILD <3
Indications: Headache, rheumatic and nerve
chronic conditions. Tablet, Acetylsalicylic acid 300 mg. months see note below, 3 months–1
pain; colds and feverish conditions.
Juvenile arthritis, by mouth with or 300 mg – 1000. year 60–125 mg, 1–5 years 120–250
Precautions: Peptic ulcer disease; avoid alco-
after food, CHILD up to 130 mg/kg OTC Aspirin (Sofak) mg, 6–12 years 250–500 mg, these
hol. Prolonged use of high Doses of Codeine
daily in 5–6 divided doses in acute Tablet, Acetylsalicylic acid 300 mg doses may be repeated every 4–6
can lead to dependence.
conditions; 80–100 mg/kg daily in 300 mg - 1000’s hours if necessary (maximum 4 doses
Adverse effects: Constipation, nausea, vomit-
divided doses for maintenance. in 24 hours).
OTC CAFENOL® (GSK) ing, dizziness, drowsiness.
OTC Acetylsalicylic acid (WMF 2.1) Tablet, Acetylsalicylic acid 300 mg; white scored tab. Advice to patients: May administer with Mild to moderate pain, pyrexia, by rec-
Tablets, Acetylsalicylic acid 100-500 mg. marked ‘CAFENOL’. meals, if GI upset occurs. tum, ADULT 0.5–1g; CHILD 1–5 years
Suppositories, Acetylsalicylic acid 50-150 mg. 300 mg - 60; 200. Dose: Adult and children over 12 years, 1-2 125–250 mg, 6–12 years 250–500
OTC Acetylsalicylic acid (EDL 2.3) OTC CAFEPRIM® (Pharchem) tabs up to 4 times a day if necessary; mg; doses inserted every 4–6 hours
Tablet (or Capsule), Acetylsalicylic acid 300 mg. Tablet, Acetylsalicylic acid 300 mg, caffeine 15 mg; not exceeding 8 tablets within 24 if necessary, maximum 4 doses in 24
white scored tab. marked ‘PIL’. hours. Not recommended for children hours.
OTC ALABUKUN® (Copac) Note: Infants under 3 months should not be given
Pack: 10 x 10’s; 1000’s. <12 years.
Oral powder, Acetylsalicylic acid 760 mg, caffeine 60 paracetamol unless advised by a doctor; a dose of 10
mg; white powder. OTC DISPRIN® (Reckitt Benckiser). OTC BEECODEEN® (BCN) mg/kg (5 mg/kg if jaundiced) is suitable.
Pack: 10 x 10’s. Soluble Tablet, Aspirin 300 mg; white scored tab. Tablet, Aspirin 400 mg, codeine phosphate 8 mg
marked ‘DISPRIN’. OTC Paracetamol (WMF 2.1)
OTC ALAGBIN® Plus (P.Z.) Pack: 50; 1000.
300 mg -3. Tablets, Paracetamol 100-500 mg
Tablet, Acetylsalicylic acid 500 mg, caffeine anhy- Oral liquid, Paracetamol 125 mg/5 mL.
drous 30 mg. OTC DRASTIN® Plus(P.Z.) PARACETAMOL Suppositories, Paracetamol 100 mg.
Pack: 20; 200 Tablet, Acetylsalicylic acid 420 mg, caffeine anhy- Synonym: Acetaminophen.
drous 30 mg. OTC Paracetamol (EDL 2.3)
OTC ALKA-SELTZER® (Gemini) Therapeutic category: Non-narcotic analgesic
Pack: 30; 100; 150. Tablets, Paracetamol 125 mg, 500 mg.
Tablet (soluble), Acetylsalicylic acid 324 mg. and antipyretic. Oral liquid, 125 mg per 5 mL.
324 mg – 30 OTC EMPIRIN® (Emzor) Indications: Mild to moderate pain including Suppository, Paracetamol 100 mg.
Tablet, Acetylsalicylic acid 300 mg; white plain dysmenorrhoea, headache; pain relief in Injection, Paracetamol 150 mg per mL.
OTC ANACIN® (SKG)
biconvex tab. osteoarthritis and soft tissue lesions; pyrexia
Tablet, Acetylsalicylic acid 300 mg; white biconvex OTC ACEPOL® (SKG)
300 mg – 1000. including post-immunization pyrexia; acute
tab. marked with a broad arrow on both sides. Suspension, Paracetamol 120 mg per 5 mL; viscous,
Tablet, Acetylsalicylic acid 75 mg
300 mg - 72 x 2’s. migraine attack (section 1.9.1). reddish liquid.
75 mg - 100’s (in blister); 100’s (in jars)
Precautions: Hepatic impairment (Appendix Pack: 60 mL.
POM ASPEGIC® (Sanofi-Aventis)
POM AEKNIL® (Olpharm) Tablet, Paracetamol 500 mg & light blue capsule shell marked ‘LAPAR’. OTC PAINAX® (Evans)
Injection, Paracetamol IP 150 mg per mL; IM (with 500 mg - 8 x 12’s; 1000’s (in blisters) 500 mg - 10 x 10’s. Tablet, Paracetamol 500 mg; white/pink scored tab.
Lignocaine) in 2 mL ampoules and 15 mL vials. Syrup, Paracetamol 125 mg per 5 mL Syrup, Paracetamol 125 mg per 5 mL; pink syrup marked ‘LX’.
Pack: 2 mL x 10’s; 2 mL x 100’s; 15 mL x 25’s. Pack: 60 mL; 2 L Pack: 60 mL 500 mg - 20; 100; 1000.
Dose: By deep IM injection (preferably into the glu- Injection, Paracetamol 150 mg per mL
OTC LEADAMOL® (Leady) OTC PANADOL® (GSK)
teal muscles), Adults, 2 mL every 4-6 hours. Pack: 2 mL x 10’s (in amp); 15 mL x 25’s (in amber
Tablet, Paracetamol 500 mg; white, scored cylindrical Tablet, Paracetamol 500 mg; white round flat tab.
Child: ½ to 1 mL every 4-6 hours. vials)
tab. marked “LEADAMOL”. marked ‘PANADOL’ on both sides.
Infusion, Paracetamol 1000 mg, sodium chloride
OTC AVIPOL® (Fidson) 500 mg - 100’s; 1000’s 500 mg - 20; 100; 500.
900 mg; in 100 mL.
Suspension, Paracetamol 120 mg per 5 mL. Syrup, Paracetamol 125 mg per 5 mL Chewable tablet, (Children’s), Paracetamol 125 mg;
Pack: 100 mL
Pack: 60 mL. Pack: 60 mL; 2 L pink cherry flavoured tab.
OTC DUNAMOL® (Topway) 125 mg - 20; 100.
OTC BARBIMOL® (Juhel) OTC M & B 5® (May & Baker)
Tablet, Paracetamol 500 mg.
Paediatric tablet, Paracetamol BP 125 mg; orange Tablet, Paracetamol 500 mg. OTC PANAGREEN® (Greenlife)
500 mg - 96’s.
scored biconvex tablet marked ‘P/125’ and ‘Juhel’ 500 mg - 20; 200. Tablet, (Extra), Paracetamol 500 mg, caffeine 30 mg.
Syrup, Paracetamol 125 mg per 5 mL.
on the reverse. Syrup, Paracetamol 120 mg per 5 mL. Pack: 20 x 10’s.
Pack: 60 mL..
125 mg – 10 x 10’s. Pack: 60 mL. Suppositories, Paracetamol 125 mg, 250 mg.
Syrup, Paracetamol BP 125 mg per 5 mL. OTC EASADOL® (May & Baker) 125 mg - 2 x 5’s; 20 x 5’s.
OTC MANTRA® (Jawa)
Pack: 60 mL in amber bottle. Caplet, Paracetamol 500 mg 250 mg - 2 x 5’s; 20 x 5’s.
Caplet, Paracetamol 500 mg.
500 mg - 20’s; 100’s Dose: Child (upto 7 kg or 3 to 6 months), 125 mg 3
OTC BNS 500® (Goldmoore) Drops, Paracetamol 100 mg per 0.6 mL.
times daily; upto 10 kg or 6 to 12 months,
Tablet, Paracetamol 500 mg. OTC EMCAP® (Emzor) Pack: 15 mL x 10’s
125 mg 4 times daily; above 10 kg or above
Pack: 10 x 10’s; 96’s. Caplet, Paracetamol 500 mg; white scored cap- Syrup, Paracetamol 120 mg per 5 mL.
1 year, 250 mg 3 times daily. Not recom-
sule-shaped tab. marked ‘EMZOR’. Pack: 60 mL.
OTC BONADOL® (Bond) mended for Children below 3 months.
500 mg - 100; 1000.
EMDEX
Syrup, Paracetamol 120 mg per 5 mL. OTC MATHEWDOL® (Daily Need) Injection, Paracetamol 150 mg per mL; in 2 mL amp.
Caplet, (Extra), Paracetamol 500 mg, caffeine 30 mg.
Pack: 60 mL Syrup, Paracetamol Syrup BP. Pack: 10 x 5 x 2 mL.
Pack: 200.
Pack: 60 mL. Dose: Adults and Child (>10 years), 600 mg 3 times
OTC BOSKA® (Orange Drugs) Oral suspension, Paracetamol 120 mg per 5 mL;
daily; Child (<10 years), 300 mg 3 times
Tablet, Paracetamol 500 mg, caffeine 30 mg alcohol-free suspension. OTC MAXIPOL® (Avro) daily. Infants: 5 mg/kg b. wt 3 times daily.
Pack: 2 x 10’s Pack: 60 mL. Suspension (alcohol free), Paracetamol 120 mg per 5
ml; pleasantly flavoured susp. OTC PANCEMOL® (Neimeth)
OTC BRADMOL® (Bradford) POM ENDAPEN® (Standard Generics)
Pack: 60 mL. Tablet, Paracetamol 500 mg.
Syrup, Paracetamol 120 mg per 5 mL. Injection, Paracetamol CP 150 mg, benzyl alcohol
500 mg - 20’s; 96’s; 1000’s.
Pack: 60 mL. 2% v/v OTC MEDIK 55® (Orange Drugs) Syrup, Paracetamol 120 mg per 5 mL.
Pack: 10 x 2 m amps; 10 x 5 mL. Tablet, Paracetamol 500 mg, caffeine 30 mg
OTC CANNON® (Orange Drugs) Pack: 60 mL.
Pack: 2 x 10’s Oral drops, Paracetamol 100 mg per mL.
Caplet, Paracetamol 500 mg, caffeine 30 mg POM EUMOL® (Beta Drugs)
Pack: 2 x 10’s Injection, Paracetamol 150 mg per 15 mL. OTC MERACAF® (Justeen) Pack: 7.5 mL bottle with 0.8 mL dropper.
Pack: 15 mL x 50’s vials. Tablet, Paracetamol 500 mg, caffeine 25 mg
OTC CEENEMOL® (Ceenek) OTC PANDA® (Joswe/Afrab)
Pack: 2 x 10’s. Tablet, Paracetamol 500 mg.
Tablet, Paracetamol 500 mg; white scored tab. OTC FEBRILIX® (BCN)
marked “P500 CEENEK”. Syrup, Paracetamol 125 mg per 5 mL. OTC MICPOL® (Mopson) 500 mg - 96; 1000.
500 mg – 1000’s Pack: 60 mL Suspension, Paracetamol 120 mg per 5 mL. Syrup, Paracetamol 125 mg per 5 mL.
Oral suspension, Paracetamol 125 mg per 5 mL; Pack: 60 mL, 2 L. Pack: 60 mL amber bottle.
OTC FERIDOL® (Therapeutic) Drops, Paracetamol 100 mg per mL.
pinkish coloured suspension.
Caplet, Paracetamol 500 mg. OTC Moko Paracetamol (New Healthway) Pack: 15 mL amber bottle with dropper.
Pack: 60 mL (in amber coloured PET bottle)
500 mg - 100’s; 1000’s. Tablet, Paracetamol 500 mg. Injection, Paracetamol 150 per mL.
POM CETAL® (Juhel) Drops, Paracetamol 100 mg per mL. 500 mg - 8 x 12’s; 1 x 1000’s.
Suppository, Paracetamol 120 mg. Pack: 15 mL. Elixir, Paracetamol 120 mg per 5 mL. OTC PANDA SAF® (Afrab-chem)
Pack: 60 mL. Syrup, Paracetamol 125 mg per 5 mL
OTC CIKAMOL® (Michelle Lab) OTC FRADOL® (Embassy) Pack: 60 mL
Tablet, Paracetamol 500 mg Tablet, Paracetamol 500 mg. OTC NACEMOL® (NASDMU)
500 mg - 8 x 12’s (in blisters); 1000’s (in jars) 500 mg - 100’s. Tablet, Paracetamol 500 mg; white scored tab. POM PARABETA-P® (Beta Drugs)
marked ‘P/500’ on one side and ‘NASDMU’ on the Injection, Paracetamol 150 mg per mL; in 2 mL amp.
OTC DAGA® (NGC) POM GG MOL® (Geneith) Pack: 2 mL x 100’s.
reverse.
Tablet, Paracetamol 500 mg Injection, Paracetamol 150 mg per 2 mL.
500 mg - 96; 1000. OTC Paracetamol (Agary)
500 mg - 5 x 4’s; 50 x 4’s Pack: 2 mL x 10’s
Syrup, Paracetamol 125 mg per 5 mL OTC NGC®-Valgin (NGC) Tablet, Paracetamol 500 mg.
OTC KAKA® (Embassy) 500 mg - 96’s
Pack: 60 mL Tablet, Acetaminophen 500 mg
Tablet, Paracetamol 500 mg.
500 mg - 100 x 10’s OTC Paracetamol (Ceenek)
OTC DEPENDOL® (Strides Vital) Pack: 100’s.
Tablet, Paracetamol 500 mg; white tab. marked Tablet (forte), Paracetamol 500 mg, caffeine 30 mg. OTC NOVADEX® (SKG) Tablet, Paracetamol 500 mg.
‘P/500’ on one side. Pack: 10 x 10’s. Tablet, Paracetamol 500 mg; white scored tab. 500 mg - 1000’s; 12 x 8’s (in blisters).
500 mg - 96. marked ‘P500’ on one side and ‘NOVADEX’ on the OTC Paracetamol (Dizpharm)
OTC LAPAR® (Mecure)
reverse. Caplet, Paracetamol 500 mg.
OTC Dr. Meyer’s Painkil® (Farmex) Tablet, Paracetamol 500 mg; white tab. marked
500 mg - 96’s; 50 x 2’s; 1000’s. 500 mg - 1000.
Syrup, Paracetamol 125 mg per 5 mL. ‘LAPAR’ and ‘500’.
Elixir, Paracetamol 125 mg per 5 mL; reddish purple
Pack: 60 mL. 500 mg - 8 x 12’s; 1 x 1000’s.
viscous liquid. OTC Paracetamol (Emzor)
Capsule, Paracetamol 500 mg; white powder in white
OTC DRUGAMOL® (Drugfield) Pack: 60 mL in amber bottle. Tablet, Paracetamol 500 mg; white scored tab.
marked “EMZOR”. 500 mg - 96’s; 1000’s. Caplet, Paracetamol 500 mg, Caffeine 25 mg. Pack: 2 x 10’s
500 mg - 96; 1000. Pack: 20.
OTC PARACURE® (Elbe) POM SUREX® (Vixa)
Syrup, Paracetamol 125 mg per 5 mL; clear pink
Capsule, Paracetamol. OTC PR® (BCN) Injection, Paracetamol 300 mg per 2 mL.
syrup.
Tablet, Paracetamol 500 mg; easy to swallow tab Infusion, Paracetamol 1 g per 100 mL; white liquid
Pack: 60 mL: 2 L. OTC PARADANA® (Dana)
marked “PR”. Pack: 1 bottle.
Syrup, Paracetamol 125 mg per 5 mL
OTC Paracetamol (Fidson) 500 mg - 2’s (in blisters); 100’s (in carton).
Pack: 60 mL OTC SWIPHAMOL® (Swipha)
Tablet, Paracetamol 500 mg; white tab. marked
POM PRAZAR® (Shrezar) Tablet, Paracetamol 500 mg.
“P/500” on one side. OTC PARAFEN® (Justeen)
Injection, Paracetamol 150 mg; in 2-mL amp 500 mg - 20’s; 200’s.
500 mg - 1000’s. Tablet, Paracetamol 500 mg, Caffeine 30 mg.
Pack: 2 mL x 10’s (in amps)
Pack: 200’s. OTC THERACIN® (Therapeutic)
OTC Paracetamol (Gauze)
OTC RAMOL® (Rapha) Tablet, Paracetamol 500 mg; white scored tab.
Oral liquid, Paracetamol 120 mg per 5 mL OTC PARAGESIC® (Vitabiotics)
Caplet, Paracetamol 500 mg; white scored caplet marked ‘THERACIN’.
Pack: 60 mL; 2 L Tablet, Paracetamol 500 mg.
marked “P500” on one side and “Rapha-Pharm” on 500 mg - 20; 100; 1000.
500 mg - 8 x 12’s
OTC Paracetamol (Goz) the reverse. Syrup, Paracetamol 120 mg per 5 mL.
Suspension, Paracetamol 120 mg per 5mL
Syrup, Paracetamol BP 120 mg per 5 mL. 500 mg - 12 x 8’s Pack: 60 mL; 100 mL; 200 mL; 1L; 2 L.
Pack: 60 mL
Pack: 60 mL; 2 L
OTC PROFECH® (Shrezar) OTC ULTIMOL® (Dizpharm)
POM PARAGOL® (Global Organics)
POM Paracetamol (Jawa) Tablet, Paracetamol 500 mg, caffeine (anhydrous) Syrup, Paracetamol 125 mg per 5 mL; cherry fla-
Infusion, Paracetamol 10 mg per mL; in water for
Injection, Paracetamol 100 mg 30 mg voured syrup.
injection.
Pack: 2 x 10’s (in blisters) Pack: 60 mL.
OTC Paracetamol (Jopan) Pack: 100 mL (in FFS bottle)
Caplet, Paracetamol 500 mg; yellow scored caplet OTC REMIDOL® (Ranbaxy) OTC UNCLE JOE® (Medreich)
OTC PARAKAF® (Diamond Remedies)
marked ‘JOPAN’ on one side and ‘P/500’ on the Tablet, Paracetamol 500 mg. Capsule, Paracetamol 500 mg.
Caplet, Paracetamol 500 mg; white tab. marked
reverse. 500 mg - 12 x 8. 500 mg - 24’s.
EMDEX
‘PARAKAF’ on both sides.
500 mg - 1000’s. Tablet (Extra), Paracetamol 500 mg, caffeine 30 mg.
500 mg - 2 x 10. OTC RICHDOL® (Richygold)
Tablet, Paracetamol 500 mg; white scored tab. Pack: 24’s.
Caplet (Extra), Paracetamol 500 mg, caffeine (anhy- Caplet, Paracetamol 500 mg.
marked ‘JOPAN’ on one side and ‘P/500’ on the
drous) 30 mg. 500 mg - 10 x 10’s. OTC VINCOPARA® (Vinco)
reverse.
Pack: 200. Injection, Paracetamol 150 mg per mL. Tablet or Caplet, Paracetamol 500 mg; white tab.
500 mg - 8 x 12’s (in blisters); 1000’s
Pack: 10 x 2 mL amp.; 50 x 15 mL vial. 500 mg - 96’s; 1000’s
OTC PARAKID® (Richygold)
OTC Paracetamol (Juhel) Dose: By IM or slow IV injection, Adult and Child
Tablet, Paracetamol 125 mg. OTC ZAPAR® (Mecure)
Tablet, Paracetamol 500 mg. (>10 years), 2-3 mL; Child (<10 years), 1-2
125 mg - 5 x 2 x 10’s. Tablet, Paracetamol 500 mg, Caffeine 30 mg; white
500 mg - 96; 1000. mL; Infant, 0.5 mL. May be repeated 4 hourly
tab. marked ‘MECURE’.
Injection, Paracetamol 300 mg per 2 mL. OTC PARAMEDROL® (Transpharm) depending on severity till temperature
Pack: 2 x 10’s.
Pack: 2 mL x 100’s. Tablet, Paracetamol 500 mg. returns to normal.
Caplet, Paracetamol 500 mg, Caffeine 30 mg; white
Dose: Adult, 300-900 mg daily in divided doses. 500 mg - 12 x 8 (in blisters); 100; 250; 500; 1000.
OTC Robert Paracetamol® (P.Z.) oval caplet marked ‘MECURE’.
Child (>6 years), 150-450 mg daily in di-
POM PARANEROS® (Neros) Tablet, Paracetamol 500 mg. Pack: 20 x 10’s.
vided doses.
Injection(IM/IV), Paracetamol 150 mg per mL 500 mg - 20; 100. Capsule, Paracetamol 500 mg, Caffeine 30 mg; yellow
OTC Paracetamol (Neimeth) Pack: 2 mL; 30 mL. Syrup, Paracetamol 125 mg per 5 mL and green capsule marked ‘ZAPAR’.
Tablet, Paracetamol 500 mg. Pack: 60 mL. Pack: 2 x 10’s.
500 mg - 20. OTC PARANEROS® Extra (Neros)
Capsule, Paracetamol BP 500 mg, Caffeine (anhy- OTC SAKURA® Extra (Orange Drugs) OTC ZIMOL® Extra (Justeen)
Syrup, Paracetamol 120 mg per 5 mL.
drous) BP 30 mg. Caplet, Paracetamol 500 mg, caffeine 30 mg Tablet, Paracetamol 500 mg, Caffeine 30 mg.
Pack: 60 mL.
Pack: 1 x 10’s; 2 x 10’s. Pack: 2 x 10’s; 20 x 10’s Pack: 20 x 10’s.
POM Paracetamol (Nemel)
POM PARAVIT-H® (Mark) OTC SARIDON P® (Swipha) Compound Paracetamol Preparations
Tablet, Paracetamol 500 mg; white tab. marked
Injection, Paracetamol 150 mg, benzyl alcohol 2% Tablet, Paracetamol 500 mg; white scored tab.
“P/500” on one side and “NEMEL” on the reverse. OTC LADINAX® (Orange Drugs)
per mL marked ‘SARIDON-P’.
500 mg - 8 x 12’s (in blisters); 1000’s (in tin). Tablet, Paracetamol 500 mg, Hyoscyamus extract 19
Pack: 5 mL; 50 mL; 30 mL; 100 mL (in amps) 500 mg - 20; 100; 200.
mg, Papaverine HCI 25 mg.
OTC Paracetamol (Nomagbon) Syrup, Paracetamol 120 mg per 5 mL.
OTC PASTIN® Extra (Juhel) Pack: 2 x 10’s
Elixir, Paracetamol 125 mg per 5 mL; pink viscous Pack: 60 mL.
Tablet, Paracetamol 500 mg, caffeine 30 mg. Indications: Relieving painful menstruation (dys-
syrup.
Pack: 200; 1000. OTC SETAMOL® (Hovid) menorrhea) and colic.
Pack: 60 mL in glass bottle.
Tablet, Paracetamol 500 mg; f-c tab. Dose: Adult 1-2 tablets 3 times daily.
OTC Paracetamol (Pharchem) OTC PENSTOP® (Rajrab) 500 mg - 10 x 10.
Tablet, Paracetamol 500 mg; white tab. marked OTC RIXANAL® (RichyGold)
Syrup, Paracetamol.
“P500” on one side and company logo on the reverse. OTC STALPARA® (GoldMoore) Tablet, Paracetamol 500 mg, Guaranine 30 mg
OTC Paracetamol (Taylek) 500 mg - 96’s; 1000’s. Tablet, Paracetamol 500 mg, caffeine (anhydrous) 30 Pack: 2 x 10’s (in blisters).
Tablet, Paracetamol 500 mg. Elixir, Paracetamol 125 mg per 5 mL; 60-mL pack has mg; uncoated tab.
500 mg - 1000’s. company logo on the cap. Pack: 20 x 10’s. PARACETAMOL plus
Pack: 60 mL; 2 L ACETYLSALICYLIC ACID
OTC Paracetamol (Watson) OTC STRIMOL® Extra (Strides Vital)
Caplet, Paracetamol 500 mg. OTC PENTAX® (Vitabiotics) Tablet, Paracetamol, Caffeine. See under the preparations below.
500 mg - 10 x 10’s; 1000’s Syrup, Paracetamol 125 mg per 5 mL Pack: 200’s.
Pack: 60 mL. OTC DRUCEDRIN® (Drugfield)
OTC PARABOL® (Efunpo) OTC SUDREX® (Orange Drugs)
Capsule, Acetaminophen 250 mg, aspirin 250 mg,
Tablet, Paracetamol 500 mg. OTC PENTAX Plus® (Vitabiotics) Tablet, Paracetamol 500 mg, caffeine 30 mg
Caffeine 65 mg.
74 | 1.8.1 Non-opioid analgesics and antipyretics 1.8.2 Opioid analgesics | 75
Pack: 10 x 10’s; 500’s (in blisters) HCl 12.5 mg; clear, colourless, non-viscous liquid. OTC IBUDOL® (Elbe) daily dose may be given as a sustained-release
Pack: 60 mL in amber bottle. Tablet, Ibuprofen, paracetamol, caffeine. preparation (designed for twice daily admin-
OTC LAILA® (Orange Drugs)
Pack: 1 x 10’s. istration) every 12 hours. Additional doses of
Granules, Paracetamol 250mg, acetylsalicylic acid OTC JUCCAN® (Juhel)
500mg; in sachet. Tablet, Paracetamol 500 mg, diphenhydramine OTC IBUMED® Plus (Sterling drugs) morphine can be given for breakthrough pain
Dose: Adult, 1 sachet 3 times daily. 25 mg Capsule, Paracetamol 325 mg, Ibuprofen 200 mg, every 4 hours if necessary, using immediate-re-
Child (1-5 years): ¼ sachet 3 times daily; 6-13 Caffeine (anhydrous) 30 mg. lease morphine tablets or solution; the dose
OTC Moko Teething Mixture (New Healthway)
years, ½ sachet 3 times daily. Pack: 4 x 10’s should be about one-sixth of the total daily
Syrup, Diphenhydramine HCl 6.25 mg, paracetamol
POM NIMEDEX® (Embassy) 120 mg per 5 mL. OTC IBUPAC® (Pacmai) dose of oral morphine. The regular dose should
Tablet, Acetaminophen 325 mg, aspirin 250 mg, Pack: 100 mL Tablet, Ibuprofen 400 mg; paracetamol 325 mg; then be reviewed and adjusted according to
caffeine (anhydrous) 30 mg; uncoated tab. uncoated tab. the need for additional doses—increments
OTC Piccan Teething Remedy (Kensington)
Pack: 2 x 10’s Pack: 10 x 10’s (in blisters) should be made to the dose, rather than the
Mixture, Paracetamol 2.4%, Diphenhydramine HCl
POM PARADEX® (Embassy) 0.25%; colourless mixture in amber bottle. OTC IBUREC® (GoldMoore) frequency of administration.
Tablet, Acetaminophen 500 mg, aspirin 250 mg; Capsule, Paracetamol 325 mg, ibuprofen 200 mg, Equianalgesic doses of opioids
OTC SAMREX® Baby Mixture (Sofak)
uncoated tab. caffeine 30 mg. It is possible to achieve equal analgesic ef-
Syrup, Paracetamol 125 mg, dill oil 0.1 mL, chlorphe-
Pack: 2 x 20’s Pack: 10’s.
niramine maleate 1 mg per 5 mL. fects with both weak and strong opioids, at
Dose: Adult, 4 to 6 capsules per day.
OTC ZAIKI AFTER 5® (Orange Drugs) Pack: 60 mL adequate doses. Equianalgesic doses should
Granules, Acetylsalicylic acid 450 mg, paracetamol Dose: Child (<6 months): 2-5 mL 2 times daily; 6 OTC PENTAX® Extra (Vitabiotics) be used when changing from one opioid to
275 mg, caffeine 50 mg; in sachet. months - 1 year, 2.5-5 mL; >2 years 5-10 Caplet, Paracetamol 325 mg, Ibuprofen 200 mg, another.
Dose: Adult, 1 sachet 3 times daily. mL 2 times daily Caffeine 30 mg. • Morphine: 30-60 mg oral; 10 mg parenteral
Child (1-5 years): ¼ sachet 3 times daily; 6-13 Pack: 2 x 10’s • Codeine: 200 mg oral; 120 mg parenteral
years, ½ sachet 3 times daily. PARACETAMOL plus IBUPROFEN • Fentanyl: 0.1 mg (100 µg) parenteral, oral prepa-
OTC PRABUMOL® (Shrezar)
EMDEX
Indications: For the relief of pains of minor and ration not available
Capsule, Paracetamol 325 mg, ibuprofen 200 mg,
PARACETAMOL plus OPHENADRINE middle intensity such as headache, neuralgia, caffeine 30 mg Choice of opioid in children
See under the preparations below. myalgia, arthalgia, toothache, dysmenorrhea; Pack: 2 x 10 x 10’s
See EMDEX Paediatric Drug Guide for detailed
less effective in postoperative and postpartum information.
OTC ANOROL® (Hovid) pain; as antipyretic in the treatment of fever; 1.8.2 Opioid analgesics
Tablet, Paracetamol 450 mg, orphenadrine 35 mg; relief of signs and symptoms of rheumatoid As stated above, opioids have equal analgesic
Morphine is effective in relieving moderate to
white scored tab. marked “HD”. arthritis and osteoarthrisits. effects at adequate doses. Factors to be con-
Pack: 10 x 10’s (in blisters) severe pain, particularly of visceral origin; there
Contra-indications: Hypersensitivity to sidered in selecting an agent include severity
is a large variation in patient response. Weaker
OTC COMBIGELSIC® (Crystal) Ibuprofen, Paracetamol & Caffeine; indi- & duration of pain, route of administration, and
opioids such as codeine are suitable for mild
Tablet, Paracetamol 500 mg, orphenadrine citrate viduals with the syndrome of nasal polyps, side effect profile.
to moderate pain.
35 mg angioedema and bronchospastic reactivity to Morphine is the preferred agent for severe
aspirin or other NSAIDs. Codeine is an opioid analgesic much less
OTC COMPIPOMAL® (Watson) pain in children due to its demonstrated
Adverse effects: Large doses taken for a long potent than morphine and much less liable,
Tablet, Paracetamol 450 mg, ophenadrine citrate efficacy and relative safety. Oral formulations
35 mg; white tab. period can cause gastic distress, hemolytic in normal Doses, to produce adverse effects
are available as immediate-release (IR) or sus-
anaemia, agranulocytosis, urticaria,rash, fever, including dependency. It is effective for mild
tained-release (SR). It can also be given IV and
PARACETAMOL plus CODEINE hypoglycemia, drowsiness, severe hepatic to moderate pain but is too constipating for
because of its short half-life, it is usually used
damage and may lead to death. long-term use.
See under the preparations below. in children with acute or episodic severe pain
Dose: Adult: 4 to 6 capsules per day i.e. 2 Morphine remains the most valuable anal- e.g., during sickle cell crisis.
CD PARACODIN® (Vitabiotics) capsules to be taken 2-3 times daily. gesic for severe pain. In addition to pain relief
Codeine has minimal intrinsic analgesic effect
Tablet, Paracetamol 500 mg, caffeine 30 mg, codeine Child (≥5 years), 1-2 capsules per day. it confers a state of euphoria and mental de-
and depends on conversion to morphine by
phosphate 8 mg tachment; repeated administration may cause
OTC COMBIFEN® (Juhel) hepatic CYP2D6 enzymes for most of its anal-
Pack: 1 x 20’s
Capsule, Paracetamol 325 mg, Ibuprofen 200 mg, dependence and tolerance, but this should not
gesic effect. Genetic polymorphism produces
Caffiene 30 mg. be a deterrent in the control of pain in termi-
wide variability in CYP2D6 function namely:
PARACETAMOL plus DIPHENHYDRAMINE/ Pack: 20’s; 100’s nal illness (see also section 12.4). Regular use
CHLORPHENIRAMINE • Poor metabolizers - people with little or no CYP2D6
Syrup, Paracetamol 120 mg, Ibuprofen 100 mg may also be appropriate for certain cases of function. Codeine is largely ineffective in these
See under the preparations below. per 5 mL. non-malignant pain, but specialist supervision people due to their inability to metabolize codeine
Pack: 60 mL (in amber PET bottle) is required. In usual doses common adverse to morpine, and this includes about 3% of African
OTC BONABABE® (Bond) OTC IBUCAP® (Shalina) effects include nausea, vomiting, constipation Americans.
Baby Teething Mixture, Paracetamol 120 mg, Conc. Capsule, Ibuprofen 200 mg, Paracetamol 325 mg, and drowsiness; larger doses produce respira- • Ultra-rapid metabolizers - people with exaggerated
Dill water 0.05 mL, Diphenhydramine HCI 6.25 mg Caffeine 30 mg. tory depression and hypotension. CYP2D6 function. Children in this group chew
per 5 mL. Pack: 10’s; 20’s; 10 x 10’s; 25 x 10’s. up codeine rapidly and this can potentially lead
Pack: 60 mL. Morphine is given by mouth as an oral solution, to unexpected morphine overdose and toxicity.
Dose: 1-2 caps three times daily.
Indications: For problems associated with teething, immediate-release tablet, or sustained-release • Codeine may interact with drugs that affect the
fever, pain and restlessness. OTC IBEX® (Medreich) tablet for chronic pain treatment. Pain should CYP2D6 system. 2D6 inhibitors (e.g., some mac-
Dose:1 teaspoonful (5 mL) three times daily. Capsule, Ibuprofen 200 mg, Paracetamol 325 mg, be controlled using immediate-release prepa- rolides) may reduce codeine effectiveness while
Caffeine 30 mg. rations first. The total morphine requirement 2D6 inducers (e.g., some anticonvulsants) may
OTC Happy Days (SKG) Pack: 24’s (in blister).
over 24 hours can then be established and the enhance codeine toxicity.
Oral liquid, Paracetamol 120 mg, diphenhydramine
76 | 1.8.2 Opioid analgesics 1.8.2 Opioid analgesics | 77
There have been cases of respiratory depres- attack; where risk of paralytic ileus. FENTANYL postoperative analgesia (section 3.5).
sion and deaths in children with sleep apnoea Precautions: Renal and hepatic impairment Therapeutic category: Narcotic analgesic. Contra-indications: Avoid in acute respiratory
who took codeine after tonsillectomy and/or (Appendices 4 and 5); dependence; pregnancy Indications: Sedation, relief of pain, preopera- depression, acute alcoholism, and where risk
adenoidectomy, prompting Black Box Warning (Appendix 2); breastfeeding (Appendix 3); tive medication, adjunct to general or regional of paralytic ileus; also avoid in raised intracra-
on codeine-containing products. overdosage: section 19.2.2; interactions: anaesthesia. nial pressure or head injury (affects pupillary
On June 6, 2013, Health Canada announced it Appendix 1. Contra-indications: Hypersensitivity to fenta- responses vital for neurological assessment);
is no longer recommending the use of codeine Adverse effects: Constipation particularly nyl or any component; increased intracranial avoid injection in phaeochromocytoma.
and codeine-containing products in children troublesome in long-term use; dizziness, nau- pressure; severe respiratory depression; severe Precautions: Renal and hepatic impairment
below 12 years of age. sea, vomiting; difficulty with micturition; ure- liver or renal insufficiency. (Appendices 4 and 5); reduce dose or avoid in
To avoid the unpredictable analgesic effect teric or biliary spasm; dry mouth, headaches, Precautions: Bradycardia; rapid I.V. infusion elderly and debilitated; dependence (severe
and the potential for toxicity, Morphine is the sweating, facial flushing; in therapeutic doses, may result in skeletal muscle and chest wall withdrawal symptoms if withdrawn abruptly);
opioid of choice for acute pain management codeine is much less liable than morphine to rigidity, impaired ventilation, respiratory hypothyroidism; convulsive disorders; de-
in children. produce tolerance, dependence, euphoria, distress, apnoea, bronchoconstriction, laryn- creased respiratory reserve and acute asthma;
Tramadol is an atypical opioid analgesic with sedation or other adverse effects. gospasm; inject slowly over 3 - 5 minutes; hypotension; prostatic hypertrophy; preg-
SNRI (serotonin and norepinephrine reuptake Dose: Mild to moderate pain, by mouth, non-depolarizing skeletal muscle relaxant nancy (Appendix 2); breastfeeding (Appendix
inhibitor) activity. It is a weak opioid with less ADULT 30–60 mg every 4 hours when may be required. 3); overdosage: section 19.2.2; interactions:
opioid side effects namely constipation, res- necessary, to a max. of 240 mg daily; Adverse effects: Hypotension, bradycardia, Appendix 1.
piratory depression, addictive effects. It may CHILD 1–12 years, 0.5–1 mg/kg every respiratory depression, CNS depression, drows- Advice to patients: Avoid alcohol, may cause
be preferred to Codeine in older children with 4–6 hours when needed; max. 240 iness, nausea, vomiting, constipation, cardiac drowsiness, impaired judgement or coordina-
moderate pain due to the variability in CYP2D6 mg daily. arrhythmias. tion; may cause physical and psychological
function, an enzyme responsible for the con- CD Codeine (WMF 2.2) Nursing action: dependence with prolonged use.
EMDEX
version of codeine to the active drug morphine. Tablet, Codeine phosphate 30 mg. • Monitor respirations of newborns exposed to drug Adverse effects: Nausea, vomiting (particularly
The oral dose of tramadol in children is 1 to 2 during labour. in initial stages) constipation; drowsiness; also
DIHYDROCODEINE • Monitor cardiovascular and respiratory status, dry mouth, anorexia, spasm of urinary and
mg/kg every four to six hours, maximum dose
B.P., pulse rate. biliary tract; bradycardia, tachycardia, palpita-
of 400 mg per day. Indications: Moderate to severe pain especially • For better analgesic effect, give before patient has
indicated in painful conditions where an alert tion, euphoria, decreased libido, rash, urticaria,
Pethidine (Meperidine) is not usually rec- intense pain.
pruritus, sweating, headache, facial flushing,
ommended for use in children. May cause patient is desired, viz. sciatica, osteoarthritis, • Monitor bladder function in postoperative patient.
chronic rheumatoid arthritis, arthritis of the • Respiratory depression, hypotension, profound vertigo, postural hypotension, hypothermia,
neurotoxicity. Increased risk of seizures due to hallucinations, confusion, dependence, miosis;
accumulation of active metabolite in patients spine, peripheral vascular disease, post–herpetic sedation, and coma may result if used with other
neuralgia, paget’s disease, malignant disease, narcotic analgesics, general anaesthetics, tran- larger doses produce respiratory depression,
with renal disease. hypotension, and muscle rigidity.
post–operative pain. quilizers, alcohol, sedatives, hypnotics, TCAs, or
Side effects of opioids
Contra-indications: Respiratory depression;
MAOIs. The doses of the above drugs should be Nursing action:
The CNS effects are responsible for the drowsi- reduced if they have to be used together. • Administer I.V. slowly over 3-5 minutes preferably
obstructive airways disease.
ness and in large doses, may cause respiratory Dose: Sedation for minor procedures/anal- as a dilute solution with sterile water.
Precautions: Asthma (avoid during an attack); • Monitor respiratory and mental status, B.P., CNS
suppression and hypotension. Combination gesia, by IM, IV, Adult and Child (>12
reduce dose in elderly, hypothyroidism, chronic depression. Do not give drug if respirations are
with alcohol or other central depressants can years), 0.5-1 mcg/kg/dose; may be
hepatic disease and in renal insufficiency; avoid below 12 /minute.
worsen these effects and can be fatal. increased in major procedures
alcohol; pregnancy; history of drug dependence • Assist with ambulation; patient should avoid
Other side-effects associated with opioid Child (1-12 years), 1-2 mcg/kg/dose;
or abuse. activities requiring alertness.
use include nausea, vomiting, constipation. may repeat at 30-60 minute intervals. • Inform patient to avoid alcohol containing prepa-
Adverse effects: Constipation, nausea, vomit-
Combination of stool softeners and stimulant Preoperative sedation, adjunct to re- rations except on doctor’s order.
ing, headache and vertigo.
laxatives is usually given with chronic opioids gional anaesthesia, postoperative pain, • Laxative or stool softener may be administered to
Advice to patients: : May cause drowsiness.
to counter the constipation. by IM, IV, Adult, 50-100 mcg/dose. relieve constipation.
Ability to operate machinery or drive may be
Addiction potential is low in the presence Adjunct to general anaesthesia, by IM, Dose: Acute pain, by SC injection (not
impaired. Avoid alcoholic beverages.
of genuine chronic pain, this has however IV, Adult, 2-50 mcg/kg. suitable for oedematous patients) or
Dose: By mouth, 30mg (1 tab) every 4-6
been observed in adolescents with sickle cell CD Fentanyl (EDL 2.1) by IM injection ADULT 10 mg every 4
hours, preferably with or after food
anaemia. Injection, Fentanyl (as citrate) 0.05 mg per mL; in hours if necessary (15 mg for heavier
Child (4-12 years): 0.5-1 mg per kg
Opioid analgesic overdosage 1-mL amp. well-muscled patients); INFANT up
b.wt every 4-6 hours
to 1 month 150 µg/kg, 1–12 months
See under section 19.2.2 Child (<4 years): Not recommended. CD Fentanyl (Alpha)
200 µg/kg; CHILD 1–5 years 2.5–5 mg,
By IM or deep SC injection, up to 50 Injection, Fentanyl citrate 0.05 mg per mL; in 10-
mL amps. 6–12 years 5–10 mg
mg every 4–6 hours.
CODEINE Chronic pain, by mouth (immedi-
Injection should be restricted to
MORPHINE ate-release tablets) or by SC injection
Drug subject to international control under the Single patients unable to be treated with
(not suitable for oedematous
Convention on Narcotic Drugs (1961). the tablets. Drug subject to international control under the Single patients) or by IM injection 5–20 mg
Indications: Mild to moderate pain; diarrhoea CD Dihydrocodeine (EDL 2.1) Convention on Narcotic Drugs (1961). regularly every 4 hours; dose may
(section 4.3.2). Tablet, Dihydrocodeine (as tartrate) 30 mg. Indications: Severe pain (acute and chronic); be increased according to need; oral
Contra-indications: Respiratory depression, Injection, Dihydrocodeine 50 mg per mL; in 1-mL dose should be approximately double
myocardial infarction, acute pulmonary
obstructive airways disease, acute asthma amp.
oedema; adjunct during major surgery and corresponding IM dose; by mouth
78 | 1.8.2 Opioid analgesics 1.8.2 Opioid analgesics | 79
(sustained release tablets), titrate mg 3-4 hourly; doses in excess of Injection, Pentazocine (as lactate) 30 mg per mL; mouth; sweating, headache, dizziness, asthe-
dose first using immediate-release 30 mg IV or 60 mg IM, SC are not in 1-mL amp. nia, restlessness, somnolence. Less commonly
preparation, then every 12 hours recommended. Pack: 1 mL x 10’s. palpitations, respiratory depression, convul-
according to daily morphine require- Child (>1 year): upto 1 mg/kg SC, IM; CD ZOPENT® (Greenlife) sions (usually after rapid IV injection).
ment (see notes above) up to 0.5 mg/kg 4-6 hourly. Injection, Pentazocine (as lactate) 30 mg per mL. Advice to patients: Avoid driving or operating
Myocardial infarction, by slow IV injec- Pack: 2 x 5 x 1 mL. machinery until the full effect of drug wears
CD Pentazocine (EDL 2.1)
tion (2 mg/minute), 10 mg followed Tablet, Pentazocine (as HCl) 25 mg off. Slow-release forms should be swallowed
by a further 5–10 mg if necessary; Capsule, Pentazocine (as HCl) 50 mg PETHIDINE whole, not chewed/crushed.
elderly or debilitated patients, reduce Injection, Pentazocine (as lactate) 30 mg per mL; Synonym: Meperidine HCl. Dose: By mouth, Adult, 50-100 mg every 4-6
dose by half. in 1-mL amp. Indications: Moderate to severe pain including hours; not exceeding 400 mg/day.
Acute pulmonary oedema, by slow IV CD ENTHAL® (Neros) postoperative pain and the pain of labour. By IV or IM injection (over 2-3 min-
injection (2 mg/minute), 5–10 mg. Injection, Pentazocine (as lactate) 30 mg per mL. Contra-indications, Precautions, etc.: See utes), 50-100 mg every 4-6 hours;
Administration: Sustained-release tablets should be Pack: 2 x 5 x 1 mL. under morphine. may be increased to a max. 400 mg
taken at regular intervals and not on an as-needed Nursing action: See under Morphine. daily depending on age and severity
basis for episodic or breakthrough pain. Sustained-re- CD FORTWIN® (Ranbaxy)
Injection, Pentazocine lactate 30 mg per mL
Dose: By IM/SC/PO/slow IV, 25-100 mg, re- of pain.
leased tablets should not be crushed.
Pack: 100 x 1 mL. peated 3-4 hourly if necessary; up to Not recommended for children <12
Note: The doses stated above refer equally to mor-
phine sulfate and hydrochloride. Sustained-release 150 mg in severe pain. Reduce dose years.
CD NOPRAZ® (Pharmgate) in IVinjection.
capsules designed for once daily administration are Injection, Pentazocine 30 mg. POM AMADOL® (Eutrix)
also available [not included on WHO Model List]; con- Pack: 2 x 5’s. CD Pethidine (EDL 2.1) Injection, Tramadol (as HCI) 50 mg per mL; clear,
sult manufacturer’s literature. Dosage requirements Tablet, Pethidine 50 mg colourless solution in transparent amp.
should be reviewed if the brand of controlled-release CD PENTABETA® (Beta Drugs) Injection, Pethidine (as HCl) 50 mg per mL; in 1-mL,
EMDEX
preparation is altered. Injection, Pentazocine (as lactate) 30 mg, sodium POM BG TRAGESIC® (BG Pharmacy)
2-mL amps. Capsule, Tramadol (as HCl) 50 mg.
chloride 2.8 mg per mL.
CD Morphine (WMF 2.2) Pack: 1 mL x 10’s (in flint glass amp) 50 mg - 10 x 10’s (in blisters)
Tablet, Morphine sulfate 10 mg. TRAMADOL
Tablets (prolonged release), Morphine sulfate 10 mg, CD PENTWIN® (Ichie-Benson) POM DOLMA® (Vatican Bells)
Pharmacology: Tramadol is an analgesic with
30 mg, 60 mg. Injection, Pentazocine (as lactate) 30 mg per mL; Capsule, Tramadol (as HCl) 50 mg; green and yellow
a dual mode of action. It is an opioid analgesic coloured caps.
Oral liquid, Morphine HCl or sulfate 10 mg/5 mL. in 1 mL amp.
with a low affinity for opioid receptors; also act 50 mg - 10’s.
Injection, Morphine HCl or sulfate 10 mg/mL; in Pack: 1 mL x 2 x 5’s.
by blocking the reuptake of noradrenaline and
1-mL ampoule. CD PENTAFORT® (Pharmabase) POM DOLOREN® (Taylek)
serotonin at synapses in the descending neural
CD Morphine (EDL 2.1) Injection, Pentazocine BP 30 mg (as lactate) per mL; Tablet, Tramadol HCI 50 mg; white, round tab.
pathways which inhibit pain responses in the 50 mg - 10’s; 30’s; 50’s-
Tablet (immediate release), Morphine 10 mg. in 1-mL amp.
spinal cord - this non–opioid action contributes Tablet, (SR), Tramadol HCI 100 mg; prolonged-re-
Tablets (modified release), Morphine 30 mg, 60 mg. Pack: 1 mL x 2 x 5’s.
significantly to the analgesic effect. Due to its lease tab.
Injection, Morphine (as sulfate or HCl) 10 mg, 15 mg CD PENTAGIV® (Foundation)
per mL; in 1-mL amps.
dual mode of action, tramadol may have less Injection, Tramadol HCI 100 mg per 2 mL.
Injection, Pentazocine (as lactate) 30 mg per mL pronounced opioid adverse effects at thera- Pack: 2 mL x 5 x 10’s amps
CD Morphine (Alpha) Pack: 10 x 1 mL amps peutic doses. Sedation, nausea and dry mouth
Injection, Morphine sulfate in 10 mg per mL; in POM DOMADOL® (Phillips)
CD PENTALAB® (Embassy) may be common but it causes less respiratory Capsule, Tramadol (as HCl) 50 mg.
1-mL amp. Injection, Pentazocine (as lactate) 30 mg per mL. depression than parenteral morphine, nalbu- 50 mg - 10’s (in blisters).
Pack: 1 mL x 10’s. phine, buprenorphine or pentazocine. It may Injection, Tramadol (as HCl) 50 mg per mL; in water
PENTAZOCINE
CD PENTAJECT® (Diamond Remedies) also be less likely to induce constipation than for injection.
Indications: Moderate to severe pain. other opioid analgesics. It has little euphoric Pack: 1-mL; 2-mL amps
Injection, Pentazocine (as lactate) 30 mg
Contra-indications: Respiratory depression, 30 mg - 1 mL x 10’s (in amps) effect and therefore lower abuse potential POM GENMADOL® (Next Generation)
raised intracranial pressure and head injury. than other opioids.
CD PENTOZOX® (Zoomota) Capsule, Tramadol HCI 50 mg; hard gelatin cap.
Narcotic dependence. Indications: Moderate to severe pain. 50 mg - 10’s
Injection, Pentazocine (as lactate) 30 mg per mL.
Precautions: Respiratory depression, obstruc- Contra-indications: Hx of hypersensitivity to Injection, Tramadol HCI 50 mg per mL; water for
tive respiratory conditions, or cyanosis; renal or tramadol or any of the components; hyper- injection.
hepatic impairment; Pregnancy; MI. CD PHARMAWIN® (Pharmabox) Pack: 2 mL
sensitivity to opioids; acute intoxication with
Adverse effects: Sedation, dizziness and occa- Injection, Pentazocine 30 mg per 1 mL; clear colour-
less liquid in brown amp. alcohol, hypnotics, analgesics, opioids, or other POM LIFAGIN® (Jubilee)
sional euphoria, lightheadedness, nausea and CNS acting drugs; concurrent use with MAOIs; Capsule, Tramadol HCl 50 mg.
Pack: 10’s (in amps)
vomiting, visual disturbances, constipation and hx of addiction; pregnancy, lactation. 50 mg - 10’s.
respiratory disturbances. CD PILAT® (May & Baker) Precautions: Impaired renal or hepatic func-
Advice to patients: Avoid alcohol, may cause Injection, Pentazocine (as Lactate salt) 30 mg per mL; POM PENGESIC® (Hovid)
tion (reduce dose); history of epilepsy or those Capsule, Tramadol HCI 50 mg; green/pale yellow cap.
drowsiness, impaired judgement or coordina- in 1-mL clear glass amp.
Pack: 10 x 10’s. susceptible to seizures; elderly patients and 50 mg - 500’s; 10 x 10’s (in blisters)
tion; may cause physical and psychological those with chronic respiratory disorders; may
dependence with prolonged use; will cause CD SOSEGON® (GSK) POM PLAZADOL® (Crystal)
impair ability to drive or operate machinery
withdrawal in patients currently dependent Injection, Pentazocine (as lactate) 30 mg per mL; clear Capsule, Tramadol 50 mg.
especially in conjunction with alcohol; opiate 50 mg - 2 x 10’s.
on narcotics. odourless to pale yellow solution.
Pack: 1 mL x 5’s.
dependence. Injection, Tramadol 50 mg per mL; in 2 mL amp.
Nursing action: See under Morphine. Adverse effects: Sedation, nausea and dry Pack: 2 mL x 5’s (in amps).
Dose: Adult, by IM, SC, or IV injection, 30-60 CD ZOCINE® (Fidson)
80 | 1.8.2 Opioid analgesics 1.9 Drugs used in substance dependence programes | 81
POM RAJTRADOL® (Seagreen) 50 mg - 2 x 10’s. 1.9 Drugs used in substance difficulty with micturation, spasm of urinary
Capsules, Tramadol HCI 50 mg, 100 mg Injection, Tramadol 50 mg per mL; in 2 mL amp. dependence programes and biliary tract, bradycardia, tachycardia,
50 mg - 10’s Pack: 2 mL x 5’s (in amps). palpitation, dysphoria, mood changes, de-
100 mg - 10’s The management of opioid dependence
POM TRAMAL® (Bolar) requires medical, social, and psychological creased libido or potency, rash, urticaria,
POM RGI Tramadol (RichyGold) Capsule, Tramadol HCl 50 mg. treatment; access to multidisciplinary care is pruritus, sweating, headache, facial flushing,
Capsule, Tramadol HCl 50 mg. 50 mg - 10’s vertigo, postural hypotension, hypothermia,
valuable. Treatment with opioid substitutes
Tablet SR, Tramadol HCl 100 mg; prolonged-release hallucinations, confusion, miosis, larger doses
POM SAMPLEX® (Crowther) should be initiated under the supervision of
tab. produce respiratory depression, hypotension,
Injection, Tramadol HCl 50 mg per mL. an appropriately qualified healthcare worker as
100 mg - 10’s
Pack: 5’s part of an established treatment programme. and muscle rigidity.
Injection, Tramadol HCl 100 mg per 2 mL; solution
for injection in 2-mL amp. Methadone, an opioid agonist, can be substi- Dose: Adjunct in treatment of opioid depend-
POM SETRADOL® (Sequoia)
Capsule, Tramadol 50 mg Pack: 5 amps tuted for opioids such as diamorphine (heroin), ence, by mouth, initially 10–40 mg
50 mg - 10 x 10’s. to prevent the onset of withdrawal symptoms; daily, increased by up to 10 mg daily
POM TRAMBETA® (Beta Drugs) (max. weekly increase 30 mg) until no
POM TRA-N® (Pharmabase) Capsule, Tramadol HCI 50 mg it is itself addictive and should only be pre-
scribed for those who are physically dependent signs of withdrawal or intoxication;
Injection, Tramadol HCI 50 mg (equiv. to Tramadol 50 mg - 1 x 10’s
on opioids. Methadone is administered in a usual dose range 60–120 mg daily;
base 44.09 mg) per mL.
POM TRAMED® (Geneith) CHILD not recommended (see Precau-
Pack: 2 mL x 5’s.
Capsule, Tramadol HCl 50 mg. single daily dose; the dose is determined by
the degree of dependence. tions above).
POM TRABILIN® (Oculus) Injection, Tramadol HCl 100 mg per 2 mL. Note: The final strength of the methadone mixture
Capsule, Tramadol HCl 50 mg. Pack: 2 mL x 10 x 10’s (in amps) Buprenorphine is a partial opioid agonist and to be dispensed to the patient should be specified
50 mg - 20’s. may be used as an alternative to methadone; on the prescription. Care is required in prescribing
POM TRAMEZ® (Mecure)
Injection, Tramadol HCl 50 mg per mL; in 2 mL amp. it should be prescribed only for those who and dispensing the correct strength because any
Capsule, (50 mg), Tramadol 50 mg; yellow/green cap.
Pack: 2 mL x 5’s.
EMDEX
marked ‘TRAMEZ 50’. are already physically dependent on opioids. confusion could lead to an overdose; this prepa-
POM TRABILIN® (Oculus) 50 mg - 1 x 10’s. It can be used as substitution therapy for pa- ration should be dispensed only after dilution as
Capsule, Tramadol (as HCl) 50 mg Capsule, (100 mg), Tramadol (as HCl) 100 mg; green/ appropriate.
tients with moderate opioid dependence; in
Injection, Tramadol HCI 50 mg per mL; in 2-mL amp. yellow cap. marked “TRAMEZ 100”. patients dependent on high doses of opioids, CD Methadone (WMF 24.5)
Pack: 2-mL x 5 amps. 100 mg - 1 x 10`s; 100`s. Concentrate for oral liquid, Methadone HCl 5 mg/
buprenorphine may precipitate withdrawal
POM TRADYL® (Reals) POM TRAMZOR ®(Zolon) due to its partial antagonist properties; it is also mL; 10 mg/mL.
Capsule, Tramodol HCI 50 mg. Capsule, Tramadol HCI 50 mg; hard gelatin cap addictive and in these patients the opioid dose Oral liquid, Methadone 5 mg/5 mL; 10 mg/5 mL.
50 mg - 1 x 10’s; 5 x 10’s. should be reduced gradually before initiating
POM TRAMZOR-SR® (Zolon)
Injection, Tramodol HCI 50 mg per mL; in 2 mL amp.
Capsule, Tramadol HCI (in timed release form) 100 therapy with buprenorphine. 1.10 Drugs used in migraine
Pack: 2 mL x 5’s.
mg; hard gelatin s-r cap 1.10.1 Acute migraine attack
POM TRAFLASH® (Miraflash) METHADONE 1.10.2 Migraine prophylaxis
POM TRD-CONTIN® (Phillips)
Capsules, Tramadol HCl 50 mg, 100 mg
Tablet, Tramadol (as HCl) 100 mg; white oblong Drug subject to international control under the Single Chronic recurrent headache is associated
50 mg- 1 x 10’s
scored f-c tab. marked “TRD-CONTIN 100”. Convention on Narcotic Drugs (1961). with many disorders, both somatic and
100 mg- 1 x 10’s
100 mg - 5 x 10`s (in blisters) psychogenic. An accurate diagnosis must
POM TRAMADEX® (Embassy) Indications: adjunct in treatment of opioid
POM TRUNAL-DX® (Reals) consequently be made before appropriate
Capsule, Tramadol 50 mg. dependence.
Retard tablet, Tramadol HCI 100 mg; s-r tab. treatment can be initiated for migraine. Un-
50 mg - 10’s. Contra-indications: Acute respiratory depres-
100 mg - 1 x 10’s treated, migraine attacks last for several hours
Injection, Tramadol 50 mg per mL; in 1 mL and 2 sion, acute alcoholism, risk of paralytic ileus;
Dose: Adult, initially 100 mg twice daily; may and sometimes for as long as 3 days.
mL amps. raised intracranial pressure or head injury (af-
increase upto 200 mg twice daily. Max. Migraine headache is frequently accompa-
Pack: 5’s. fects pupillary responses vital for neurological
400 mg daily. nied by GI disturbance including nausea and
POM Tramadol (Jawa) assessment).
POM UPMADOL® (Award Global) vomiting. The headache may be preceded
Injection, Tramadol HCl 100 mg per 2 mL Precautions: Renal and hepatic impairment
Capsules, Tramadol HCI 50 mg, 100 mg or accompanied by aura (classical migraine)
Pack: 2 mL x 10’s (Appendices 4 and 5), risk of toxicity in children
Pack: 10’s (in blisters) which is characterised by visual disturbances
POM Tramadol (Juhel) and non-dependant adults or if tolerance in-
POM URGENDOL® (Phillips)
such as flickering lines and fragmented vision
Injection, Tramadol HCl 100 mg per 2 mL; in 2-mL correctly assessed in dependent adults; severe
Capsule, Tramadol HCI 50 mg or sensory disturbances such as tingling or
amp. withdrawal symptoms on abrupt withdrawal;
50 mg - 10’s numbness; rarely, hemiparesis or impaired
Pack: 2 mL x 5 x 10’s hypothyroidism, convulsive disorders, de-
Injection, Tramadol HCI 50 mg per mL. consciousness may occur. Migraine without
creased respiratory reserve and acute asthma;
POM Tramadol (N.C.I) Pack: 1 mL; 2 mL aura (common migraine) is the more common
Capsule, Tramadol (as HCl) 50 mg; yellow/green cap. hypotension, prostatic hypertrophy; preg-
POM VISKODOL® (Visko) form occurring in about 75% of patients who
50 mg - 1 x 10’s. nancy (Appendix 2), breast-feeding (Appendix
Injection, Tramadol 50 mg experience migraine.
Capsule, Tramadol 100 mg 3); overdosage section 19.2.2, interactions:
50 mg - 2 mL x 10’s. Emotional or physical stress, lack of or excess
Pack: 10 x 100’s. Appendix 1
sleep, missed meals, menstruation, alcohol and
POM Tramadol (Vinco) POM VTRAM® (Nelpharm) INCOMPATIBILITY: Syrup preserved with
specific foods including cheese and chocolate
Capsule, Tramadol (as HCl) 50 mg. Capsule, Tramadol HCl 50 mg hydroxybenzoate (parabens) esters may be
50 mg - 1 x 10’s are often identified as precipitating factors; oral
50 mg - 10 x 1 x 10’s. incompatible with methadone HCl.
contraceptives may increase the frequency of
POM V-TRAM® (Nalis) Adverse effects: Nausea, vomiting, consti-
POM TRAMADOSE® (Crystal) attacks. Avoidance of precipitating factors can
Capsule, Tramadol HCI 50 mg; hard gelatin cap pation; drowsiness; also dry mouth, anorexia,
Capsule, Tramadol 50 mg. prevent or reduce the frequency of attacks.
82 | 1.10.1 Acute migraine attack 1.10.1.2 Ergot alkaloids | 83
Women taking combined oral contraceptives avoided in cerebrovascular or cardiovascular Precautions: Hepatic impairment (Appendix mouth preferably with or after food,
who experience an onset or increase in fre- disease. 5); renal impairment; alcohol dependence; ADULT 400–600 mg at first sign of
quency of headaches should be advised of Products which contain barbiturates or pregnancy (Appendix 2) and breastfeeding attack, may be repeated every 6–8
other contraceptive measures. codeine are undesirable since they may (Appendix 3); overdosage: section 19.2.1; hours if necessary, maximum 2.4 g
The two principal strategies of migraine man- cause physical dependence and withdrawal interactions: Appendix 1. daily; CHILD 8–12 years 200 mg at
agement are treatment of acute attacks and headaches. Adverse effects: Rare, but rashes, blood dis- first sign of attack, may be repeated
prevention of attacks. orders (including thrombocytopenia, leuko- every 6–8 hours if necessary.
1.10.1.1 Analgesics penia, neutropenia) reported; important: liver See section 2.1.1 for the proprietary preparations of
1.10.1 Acute migraine attack damage (and less frequently renal damage) Ibuprofen.
ACETYLSALICYLIC ACID following overdosage.
1.10.1.1 Analgesics
1.10.1.2 Ergot alkaloids Synonym: Aspirin; ASA. Dose: Treatment of acute migraine attack, by
Indications: Acute migraine attacks; tension mouth, ADULT 0.5–1 g at first sign 1.10.1.2 Ergot alkaloids
1.10.1.3 Antiemetics
headache; pyrexia, mild to moderate pain of attack, may be repeated every
Treatment of acute attacks may be non-specific ERGOTAMINE
and inflammation (section 1.8.1); antiplatelet 4–6 hours if necessary, maximum 4
using simple analgesics; if nausea and vomit-
(section 5.6). g daily; CHILD 6–12 years 250–500 POM Ergotamine (EDL 6)
ing are features of the attack, an antiemetic
Contra-indications: Hypersensitivity (includ- mg at first sign of attack, may be re- Tablet, Ergotamine tartrate 2 mg.
drug may be given. Treatment is generally by
ing asthma, angioedema, urticaria or rhinitis) peated every 4–6 hours if necessary,
mouth; some drugs are available as suppos-
itories which may be used if the oral route to acetylsalicylic acid or any other NSAID; maximum 4 doses in 24 hours. 1.10.1.3 Antiemetics
children and adolescents under 16 years (Reye Treatment of acute migraine attack,
is not effective (poor oral bioavailability, or
syndrome, see section 1.8.1); active peptic by rectum, ADULT and CHILD over 12 METOCLOPRAMIDE
absorption from the gut impaired by vomit-
ulceration; haemophilia and other bleeding years 0.5–1 g at first sign of attack,
ing), or not practicable (patient unable to take Indications: Nausea and vomiting associated
EMDEX
disorders; not for treatment of gout. may be repeated every 4–6 hours if
drugs orally). Excessive use of antimigraine with migraine; nausea and vomiting in GI
Precautions: Asthma, allergic disease; previous necessary, maximum 4 doses in 24
medication (analgesics, 5HT1 agonists [not disorders and cytotoxic therapy (section 4.6)
peptic ulceration; renal impairment (Appendix hours; CHILD 6–12 years 250–500
included on WHO Model List] and ergotamine Contra-indications: GI obstruction, haemor-
4); hepatic impairment (Appendix 5); preg- mg at first sign of attack, may be re-
[not included on WHO Model List]) is associated rhage or perforation; 3–4 days after GI surgery;
nancy (Appendix 2); breastfeeding (Appendix peated every 4–6 hours if necessary,
with medication overuse headache (analge- phaeochromocytoma.
3); elderly; G6PD-deficiency; dehydration; max. 4 doses in 24 hours.
sic-induced headache); therefore, increasing Precautions: Hepatic or renal impairment
consumption of these medicines needs careful interactions: Appendix 1. POM Paracetamol (WMF 7.1) (Appendices and 5); elderly; children and
management. Adverse effects: Generally mild and infrequent Tablets, Paracetamol 300-500 mg young adults; pregnancy (Appendix 2) and
Simple analgesics including NSAIDs (nonsteroi- but high incidence of GI irritation with slight breastfeeding (Appedix 3); epilepsy; porphyria;
See section 1.8.1 for the proprietary preparations of
dal anti-inflammatory drugs) can be effective asymptomatic blood loss, increased bleeding Paracetamol. interactions: Appendix 1.
in mild to moderate forms of migraine if taken time; bronchospasm and skin reactions in Adverse effects: Extrapyramidal effects (espe-
early in the attack; most migraine headaches hypersensitive patients; see also section 1.8.1. cially in children and young adults) drowsiness,
Dose: Treatment of acute migraine attack, IBUPROFEN restlessness, diarrhoea; prolonged administra-
respond to paracetamol, acetylsalicylic acid
or an NSAIDs such as ibuprofen. Peristalsis by mouth preferably with or after Indications: Acute migraine attacks, tension tion, see section 4.5.
is often reduced during migraine attacks food, ADULT 300–900 mg at first sign headache; mild to moderate pain and inflam- Dose: Nausea and vomiting of migraine, by
and, if available, a dispersible or effervescent of attack, may be repeated every mation, pyrexia (section 2.1.1) mouth or by IM injection, ADULT
preparation of the drug is preferred because of 4–6 hours if necessary; maximum Contra-indications: Hypersensitivity (includ- single dose of 10–20 mg at first sign
enhanced absorption compared with a conven- 4 g daily; CHILD under 16 years not ing asthma, angioedema, urticaria or rhinitis) of attack preferably 10–15 minutes
tional tablet. The risk of Reye syndrome due to recommended. to acetylsalicylic acid or any other NSAID; active before antimigraine drug;ADOLES-
acetylsalicylic acid in children can be avoided Treatment of acute migraine attack, peptic ulceration. CENT single dose of 5–10 mg (5 mg if
by giving paracetamol instead. by rectum, ADULT 600–900 mg Precautions: Hepatic or renal impairment body weight <60 kg).
An antiemetic such as metoclopramide, inserted at first sign of attack, may be (Appendices 4 and 5); preferably avoid if history
repeated every 4 hours if necessary; See section 4.6 for the proprietary preparations of
given as a single dose orally or by intramuscular of peptic ulceration; cardiac disease; elderly;
Metoclopramide.
injection at the onset of a migraine attack, maximum 3.6 g daily; CHILD under 16 pregnancy and breastfeeding (Appendices 2
preferably 10–15 minutes before the analgesic, years not recommended. and 3); coagulation defects; allergic disorders;
is useful not only in relieving nausea but also POM Acetylsalicylic acid (WMF 7.1) interactions: Appendix 1 1.10.2 Migraine prophylaxis
in restoring gastric motility, thus improving Tablets, Acetylsalicylic acid 300-500 mg. Adverse effects: GI disturbances including Prophylactic treatment for migraine should be
absorption of the analgesic. nausea, diarrhoea, dyspepsia, GI haemor- considered for patients in whom:
See section 1.8.1 for the proprietary preparations of
Specific antimigraine drugs, such as the 5HT1 rhage; hypersensitivity reactions including • treatment of acute migraine attacks is ineffective
Acetylsalicylic acid.
agonist sumatriptan [not included on the rash, angioedema, bronchospasm; headache, or not possible;
WHO Model List], are used when analgesics dizziness, nervousness, depression, drowsi- • the frequency of migraine attacks is increasing;
PARACETAMOL ness, insomnia, vertigo, tinnitus, renal failure; • migraine attacks occur more than once or twice
are ineffective; they act on 5HT (serotonin)
Synonym: Acetaminophen. rarely hepatic damage; very rarely exfoliative a month;
1B/1D receptors and can be used during the • the severity or duration of migraine attacks is
established headache phase of an attack. Ergot Indications: Acute migraine attacks, tension dermatitis, purpura; prolonged administration,
disabling.
alkaloids should no longer be used; they are headache; mild to moderate pain, pyrexia see section 2.1.1.
Prophylaxis can reduce the severity and fre-
associated with many sideeffects and must be (section 1.8.1). Dose: Treatment of acute migraine attack, by
quency of attacks but does not eliminate them
84 | 1.10.2 Migraine prophylaxis
completely; additional symptomatic treatment phaeochromocytoma.
is still needed. However, long-term prophy- Precautions: 1st-degree AV block; renal impair-
laxis is undesirable and treatment should be ment (Appendix 4); liver disease (Appendix 5);
reviewed at 6-monthly intervals. pregnancy (Appendix 2), breastfeeding (Appen-
Of the many drugs that have been advocated dix 3); portal hypertension; diabetes mellitus;
for migraine prophylaxis, beta-adrenoceptor myasthenia gravis; history of hypersensitivity
antagonists (beta-blockers) are most fre- [increased reaction to allergens, also reduced
quently used. Propranolol, a non-selective response to epinephrine (adrenaline)]; inter-
beta-blocker and other related compounds actions: Appendix 1.
with similar profile such as atenolol are gener- Adverse effects: Bradycardia, heart failure,
ally preferred. Tricyclic antidepressants, such as hypotension, conduction disorders, bronchos-
amitriptyline (section 1.4.1) or calcium-chan- pasm, peripheral vasoconstriction, exacerba-
nel blocking drugs such as verapamil (section tion of intermittent claudication and Raynaud
5.5) may be of value. phenomenon, GI disturbances, fatigue, sleep
disturbances including nightmares; rarely,
PIZOTIFEN rash, dry eyes (reversible), sexual dysfunction,
exacerbation of psoriasis.
POM Pizotifen (EDL 6)
Tablets, Pizotifen (as hydrogen malate) 0.5 mg,
Dose: Prophylaxis of migraine, by
1.5 mg. mouth, ADULT initially 40 mg 2–3
Oral liquid, Pizotifen (as hydrogen malate) 0.25 mg times daily, increased by same
per mL. amount at weekly intervals if neces-
sary; usual range 80–160 mg daily;
PROPRANOLOL CHILD under 12 years, 20 mg 2–3
Indications: Prophylaxis of migraine. times daily.
Contra-indications: Asthma or history of ob- POM Propranolol (WMF 7.2)
EMDEX
structive airways disease, uncontrolled heart Tablets, Propranolol HCl 20 mg, 40 mg.
failure, Prinzmetal angina, marked bradycardia,
POM Propranolol (EDL 6)
hypotension, sick sinus syndrome, 2nd- or 3rd-de- Tablets, Propranolol (as HCl) 40 mg, 80 mg.
gree AV block, cardiogenic shock, metabolic
acidosis, severe peripheral arterial disease; See section 5.3.1 for the proprietary preparations of
Propranolol.
EMDEX 2014/2015 | Get your EMDEX Vol. 3 (Drug Comparisons & Therapeutic Details) at no extra charge
2. Drugs for
musculoskeletal and
joint diseases
2.1 Antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 86
2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs). . . . . . . . . . . . . . . . . . . . . . . . . . 86
2.1.2 Disease-modifying antirheumatic drugs (DMARDs). . . . . . . . . . . . . . . . . . . . . . . 101
2.1.3 Other antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 104
2.2 Drugs used in gout . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106
2.2.1 Acute gout. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106
2.2.2 Chronic gout. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 106
2.3 Skeletal muscle relaxants (antispasmodics) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 107
2.4 Muscle relaxants (peripherally acting) and cholinesterase inhibitors . . . . . . . . 109
2.4.1 Muscle relaxants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109
EMDEX
2.4.2 Cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 109
2.5 Drugs affecting bone structure and mineralization. . . . . . . . . . . . . . . . . . . . . . . . . 111
2.6 Topical antirheumatic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 112
2.7 Enzymes and miscellaneous anti-inflammatory agents. . . . . . . . . . . . . . . . . . . . . 113
86 | 2.1 Antirheumatic drugs 2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs) | 87
2.1 Antirheumatic drugs cyclo-oxygenase, which is involved in the produc- Pharmacology: Celecoxib is a NSAID that rhea, initially 400 mg, followed by an
tion of prostaglandins. works by inhibition of prostaglandin synthesis, additional 200 mg dose if needed on
2.1.1 Nonsteroidal anti-inflammatory drugs (NSAIDs)
2.1.2 D isease-modifying antirheumatic drugs Indication: Relief of pain and inflammation primarily via inhibition of cyclooxygenase-2 the first day; then 200 mg twice daily
(DMARDs) associated with rheumatoid arthritis, osteoar- (COX-2), and at therapeutic concentrations as needed.
2.1.3 Other anti-rheumatic drugs thritis or ankylosing spondylitis. in humans, celecoxib does not inhibit the Familial Adenomatous Polyposis (FAP),
Contra-indications, Precautions, Adverse ef- cyclooxygenase-1 (COX-1) isoenzyme. Peak by mouth, 400 mg twice per day
2.1.1 Non-steroidal anti-inflammatory fects, Nursing action, and Advice to patients: plasma levels of celecoxib occur approx. 3 Child: Not recommended in those
drugs (NSAIDs) see under Diclofenac. hours after an oral dose. High fat meal may <18 years.
Dose: By mouth, Adult, 100 mg twice daily. delay peak plasma levels by about 1-2 hours Administration: May be taken with or without
NSAIDs, including ibuprofen, have analgesic, meals. For patients with difficulty swallowing, may
Should be taken with food. To be with an increase in total absorption (AUC) of
anti-inflammatory and antipyretic properties. open capsule and mix contents in a teaspoon with
swallowed whole with a sufficient 10-20%. Doses up to 200 mg bid can be admin-
In single doses NSAIDs have analgesic activity applesauce before taking.
quantity of liquid. istered without regard to meals. Higher doses
comparable to that of paracetamol. In regular
POM Aceclofenac (Crystal)
(400 mg bid) should be administered with food POM CELEBREX® (Pfizer)
full dosage, they have a lasting analgesic and Capsule, Celecoxib 200 mg.
Tablet, Aceclofenac 100 mg; white tab. to improve absorption. It is primarily metabo-
anti-inflammatory effect, which makes them 200 mg – 10’s (in blister).
100 mg – 10 x 10’s (in strips). lised via CYP2C9 to inactive metabolites and
useful for continuous or regular pain due to
less than 3% of unchanged drug is recovered
inflammation. Differences in anti-inflammatory POM ACEFEN® (Barata) DICLOFENAC
in the urine and feces.
activity between different NSAIDs are small but Tablet, Aceclofenac 100 mg; f-c tab
Indications: Inflammatory and degenerative
100 mg – 3 x 10’s (in blisters) Indications: Osteoarthritis; rheumatoid ar-
there is considerable variation in individual forms of rheumatism; acute musculoskeletal
thritis. Management of acute pain; treatment
patient response and in the incidence and type POM ACLOTAS® SR (Phillips) disorders; acute gout; post-operative and
of primary dysmenorrhea. For the regression
of adverse effects. Ibuprofen has fewer adverse Tablet, Aceclofenac 200 mg; f-c sustained-release post-traumatic inflammation and swelling;
and reduction in number of adenomatous
effects than other NSAIDs but its anti-inflam-
EMDEX
tab. painful and/ or inflammatory conditions in
colorectal polyps, which may lead to the
matory properties are weaker. Diclofenac and 200 mg – 10’s (in blisters).
gynaecology e.g. dysmenorrhoea; renal and
development of colorectal cancer in patients
naproxen (neither of which is included on the POM ACYCOR® (Reals) biliary colic; as an adjunct in severe painful
with familial adenomatous polyposis (PAP);
WHO Model List) combine moderately potent Tablet, Aceclofenac 100 mg; f-c tab. inflammatory infections of the ear, nose, or
as an adjunct to usual care (e.g., endoscopic
anti-inflammatory activity with a relatively low 100 mg – 1 x 10’s throat.
surveillance, surgery).
incidence of adverse effects (but incidence is Contra-indications: Avoid use in the pres-
POM ALGIC® (Phillips) Contra-indications: Hypersensitivity to any
higher than that for ibuprofen). Tablet, Aceclofenac 100 mg; f-c tab ence of peptic ulcers, pregnancy, lactation,
ingredient of the product; known sulfona-
Ibuprofen is used in the treatment of mild to 100 mg – 10’s (in blisters) mide hypersensitivity. ASA or NSAID induced hypersensitivity (e.g. with asthma attacks,
moderate pain and in the management of pain POM DABANAC® (Dabak) asthma, urticaria or allergic-type reactions. skin reactions, acute rhinitis) to acetylsalicylic
and inflammation in rheumatoid arthritis and Tablet, Aceclofenac 100 mg; f – c tab. Pregnancy; lactation. acid or other non-steroid anti-inflammatory
juvenile arthritis. It may also be of value in the 100 mg – 2 x 10’s (in blisters). Precautions: Compromised cardiac function agents, severe disorders of liver function or
less well-defined conditions of back pain and and other conditions predisposing to fluid haemopoietic disorders.
POM DURAFENAC® (Visko)
soft-tissue disorders. Ibuprofen is also used to Tablet, Aceclofenac 100 mg retention. Severe kidney or liver disease. Poor Precautions: History of peptic ulcer, unex-
reduce pain in children. With all NSAIDs caution Pack: 3 x 10’s CYP2C9 metabolizers may have abnormally plained GI disorders; liver or kidney damage;
should be exercised in the treatment of the high plasma levels of the drug. high blood pressure; elderly. NSAID or ASA
elderly, in allergic disorders, during pregnancy POM KAYFENAC® (Kayhelt)
Interactions: Warfarin (monitor anticoagulant induced asthma, hayfever, nasal polyps or
Tablet, Aceclofenac 100 mg; uncoated tab
and breastfeeding. In patients with renal, car- activity especially in the elderly). CYP2C9 chronic airways infections.
100 mg – 10’s (in blisters)
diac or hepatic impairment, the dose should inhibitors e.g. fluconazole (reduced metabolic Adverse effects: GI upsets, upper abdominal
be kept as low as possible and renal function POM MICRONAC® SR (Micronova) clearance). Antacids (aluminium and magne- pain, eructation, nausea, diarrhoea, light-head-
should be monitored. NSAIDs should not be Tablet, Aceclofenac 200 mg; f-c sustained-release edness or headaches. Rarely, GI bleeding;
sium) may reduce the extent of absorption.
given to patients with active peptic ulceration tab.
Adverse effects: GI disorders, abdominal pain, nephrotoxicity; hypersensitivity reactions such
200 mg – 30’s.
and should preferably not be used in those diarrhea, dyspepsia. as skin rash and pruritus, asthma attacks and a
with a history of the disease. The commonest POM ZERODOL® (IPCA) Advice to patients: Advise to report signs or tendency to oedema may arise.
adverse effects are generally gastrointestinal Tablet, Acelofenac 100 mg; f-c tab. symptoms of GI ulceration or bleeding, skin Advice to patients: May take with meals if GI
including nausea, vomiting, diarrhoea, and 100 mg – 10’s. upset occurs
rash, unexplained weight gain, or edema to
dyspepsia; hypersensitivity reactions including + Paracetamol their physicians. Inform about warning signs Nursing action:
anaphylaxis, bronchospasm, and rash have and symptoms of hepatotoxicity (e.g., nausea, • Administer whole, do not crush nor split tablet; give
POM ALGIC P® (Phillips)
been reported, as has fluid retention. fatigue, lethargy, pruritus, jaundice, right upper with food or milk to minimize GI distress.
Tablet, Aceclofenac 100 mg, paracetamol 500 mg;
• Give with a full glass of water to enhance ab-
Prevention of NSAID-associated ulcers f-c tab quadrant tenderness, and “flu-like” symptoms)
sorption, keep patient upright for 30 min. Advise
Pack: 10’s (in blisters) and to stop therapy and see doctor if such patient to report any signs of blood in stool and
See under Section 4.1
symptoms occur. to avoid other medications namely aspirin, other
ACETYLSALICYLIC ACID Dose: Osteoarthritis, by mouth, 200 mg/day NSAIDs, alcohol, paracetamol, unless prescribed.
ACECLOFENAC given as a single dose or as 100 mg • Teach patient symptoms of peptic ulceration which
See under Section 1.8.1
Pharmacology: Aceclofenac is an orally admin- twice per day. are common with NSAIDs; relieve symptoms with
istered phenylacetic acid derivative (related to Rheumatoid arthritis, by mouth, 100- antacid.
diclofenac) with analgesic and anti-inflammatory CELECOXIB 200 mg twice per day. • Advise patient to avoid driving or any hazardous
properties. It is a potent inhibitor of the enzyme Therapeutic category: NSAID, COX-II inhibitor Acute pain and primary dysmenor- activities if dizziness, drowsiness occurs.
88 | 2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs) 2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs) | 89
Dose: By mouth, 75-150 mg daily in 2-3 max. daily dose of 150 mg. By IM injection, Tablet, Diclofenac potassium 50 mg; yellow tab. POM JOFENAC® (Jopan)
divided doses depending on the Adult only, 1 or 2 ampoules per day for not 50 mg – 10 x 10’s. Tablet, Diclofenac sodium 50 mg; f-c tab.
indication; up to 200 mg in dysmen- more than 2 days Max. daily dose: 150 mg. Pack: 1 x 10’s
POM DICLOGEN® (Geneith)
orrhoea and migraine attacks. Special patients population: Patients with estab- Tablet, Diclofenac sodium 100 mg; f-c tab.
Injection, Diclofenac sodium 75 mg per 3 mL
lished heart disease or cardiovascular risk factors 100 mg – 1 x 10’s
By deep I.M. injection, 75 mg once
should only receive doses up to max. 100 mg daily OTC DICLOLAB® (Embassy)
daily or 75 mg twice daily in severe POM KALFEN® (Justeen)
if treated for more than 4 weeks. Cream, Diclofenac diethylammonium 1.16% equiv.
cases for not more than 2 days. Injection, Diclofenac sodium 75 mg per 3 mL.
to Diclofenac sodium 1 %.
Child (>1 year): 0.5-2 mg/kg daily. POM CIKAFLAM® (Michelle Lab) Pack: 3 mL x 5’s.
Pack: 30 g.
Tablet, Diclofenac sodium 50 mg
POM Diclofenac (EDL 2.4) Dose: Apply 2-3 times a day at the affected area. OTC LABDIC® Relief Gel (Embassy)
50 mg – 100’s; 10 x 10’s (in blisters)
Tablets, Diclofenac 25 mg, 100 mg. Gel, Diclofenac diethylammonium 1.16% equiv.
POM DICLOMAX®-50 (Zoomota)
Gel, Diclofenac 1%. POM CLOFENAC® (Hovid) to Diclofenac sodium 1%, Methyl salicylate 8%,
Tablet, Diclofenac (as Na+) 50 mg; e-c extended
Injection, Diclofenac 25 mg per mL. Tablets, Diclofenac 50 mg, 100 mg. Menthol 2%.
release yellow tab.
50 mg – 20; 100 Pack: 30 g.
POM ABITREN® (Dizpharm) 50 mg – 10 x 10’s
100 mg – 20; 100. Dose: Apply 2-3 times a day at the affected area.
Tablet, Diclofenac sodium 100 mg; s-r tab. Tablet (SR), Diclofenac sodium 100 mg; s-r, pink POM DICLOPLUS® (Eutrix)
100 mg – 10, 20. POM LOFNAC® (Greenlife)
f-c tab. Tablet (retard), Diclofenac potassium 50 mg.
Tablets, Diclofenac (as sodium salt) 50 mg, 100 mg;
POM B-FENAC® (Boucia) 100 mg – 10 x 10 (in blisters); 100’s. 50 mg – 10’s
e-c tabs.
Retard tablet, Diclofenac sodium 100 mg; s-r tab POM DABAPAIN® (Dabak) POM DICLORAN®(Hochiez) Injection, Diclofenac (as sodium salt) 25 mg per mL;
100 mg – 1 x 10’s (in blisters) Tablet, Diclofenac potassium 50 mg; yellow tab. Injection, Diclofenac 75 mg per 3 mL in 3 mL amp.
POM BENTREN-SR® (Ichie-Benson) 50 mg – 10’s (in blisters). Pack: 3 mL x 10’s.
POM DICLOSAL® (Strides Vital) Suppository, Diclofenac sodium.
Tablet, Diclofenac sodium 100 mg; s-r tab. POM DELVAC® (Al-Tinez) Injection, Diclofenac 75 mg per 3 mL; in ampoule. Gel, Linseed oil 3%, Diclofenac diethylamine 1.16%
EMDEX
100 mg – 3 x 10’s Tablet, Diclofenac sodium 100 mg; yellow coloured Pack: 3 mL x 10’s. (equiv. to Diclofenac sodium 1%), Methyl salicylate
POM BETAREN® (Pemason) e-c oval tab.
OTC DICLOSEED® (Crystal) 10%, Menthol 5%.
Tablets, Diclofenac (as sodium) 25 mg, ochre tab.; 50 100 mg – 100’s.
Gel, Diclofenac diethylamine 1.16%, methyl salicy- Pack: 30 g tube.
mg, reddish-brown tab. OTC DEMO-4® (Beta Drugs) late 10 %, menthol 5%; white gel in a tube. Administration: Apply 3-4 times a day.
25 mg – 30’s; 100’s. Gel, Diclofenac diethylamine 1.16% equiv. to Di- Pack: 20 g.
50 mg – 30’s; 50’s. POM MAXIT® (CG Biostadt)
clofenac sodium 1.00%, methyl salicylate 10.00%,
Tablets, (Retard), Diclofenac (as sodium) 75 mg, 100 POM DICLOTAB® (Joswe/Afrab) Tablets, Diclofenac potassium 50 mg, 75 mg; f-c tabs.
menthol 5.00%, oleum lini (containing predom-
mg, pink tabs. Tablet, Diclofenac sodium 50 mg; e-c tab. 50 mg – 20’s (in blister)
inantlyalfa-linolenic acid) 3.00%, benzyl alcohol
75 mg – 28’s; 56’s. 50 mg – 20`s. 75 mg – 20’s (in blister)
1.00%; gel base.
100 mg – 10’s. Dose: Pain and soft tissue inflammation, by mouth,
Pack: 30 g. POM DIGIFLAM® (Digitall) Adult, 75-150 mg daily in 2-3 divided doses,
POM CANODOL® (Canopus) POM DICLODASE® (Pharmgate) Tablet, Diclofenac potassium 50 mg; f-c tab. depending on severity.
Tablet, Diclofenac potassium 50 mg Tablet, Diclofenac (as K+) 50 mg 50 mg – 1 x 10’s; 10 x 10’s Child (>14 years), 75-100 mg daily in 2-3
50 mg – 10 x 10’s 50 mg – : 2 x 10’s; 10 x 10’s POM DYNAPAR AQ® (Synergy) divided doses.
Injection, Diclofenac Sodium 25 mg per mL; in 3 Primary dysmenorrhea, 50-150 mg daily in
POM CATAFLAM®(Novartis) POM Diclofenac (Alpha)
mL amp 2-3 divided doses
Tablets, Diclofenac potassium 25 mg, 50 mg; s-c tabs Injection, Diclofenac 25 mg per mL.
Pack: 3 mL x 5’s (in blister). Not recommended in children <14 years.
Capsule, Diclofenac potassium 50 mg; soft cap.
Oral suspension, Diclofenac free acid 1.8 mg per mL POM Diclofenac (Crystal) POM MEDIFEN® (Embassy)
Tablet, Diclofenac potassium 100 mg POM ELAFEN® (Jopan)
Oral drops suspension, Diclofenac resinate (equiv. Caplet, Diclofenac potassium 100 mg Tablet (retard), Diclofenac sodium 100 mg.
to 0.5 mg diclofenac potassium per drop =1.5%) POM Diclofenac (Drugfield) 100 mg – 1 x 10’s. 100 mg – 10’s.
15 mg per mL. Capsule, Diclofenac (as sodium salt) 50 mg
Suppositories, Dicofenac potassium 12.5 mg, 25 OTC FAST HEAT® (Award Global) POM MEFINAC® (Embassy)
50 mg – 1 x 10’s; 10 x 10’s (in blisters) Tablet (retard), Diclofenac sodium 100 mg; s-r tab.
mg, 75 mg Gel, Diclofenac diethylamine 11.6 mg equiv. to Cream, Diclofenac diethylamine 1.16% (equiv. to
Solution for injection, Diclofenac potassium 75 mg Diclofenac sodium 1%), Linseed oil (containing pre- 100 mg – 10 x 10’s (in blisters).
Diclofenac sodium 10 mg
per 3 mL Pack: 20 g dominantly alfa-linolenic acid 3%), methyl salicylate OTC MIRAPAIN® (Miraflash)
Indications: Short-term treatment in the following 10%, menthol 5%. Gel, Diclofenac diethylamine BP 1.16% eq. to Di-
acute conditions: Post-traumatic and post-operative POM Diclofenac (Embassy) Pack: 30 gm. clofenac sodium BP 1.00%, linseed oil BP 3.00%,
pain, inflammation and swelling, e.g. due to sprains Injection, Diclofenac (as sodium) 75 mg per 2 mL. methyl salicylate BP 10.00 %, menthol BP 5.00%.
Pack: 10’s. POM FENAL® (Geneith)
or following dental or orthopaedic surgery. Painful Pack: 30 g.
Tablets, Diclofenac potassium 50 mg, 100 mg; f-c tabs
and/or inflammatory conditions in gynaecology, POM Diclofenac (Jawa) 50 mg – 10 x 10 (in blister) OTC MOVEON® (Canopus)
e.g. primary dysmenorrhoea or adnexitis. Migraine Injection, Diclofenac (as Na+) 75 mg per 3 mL. 100 mg – 10 x 10 (in blister) Gel, Diclofenac diethylamine1.16% equiv. to di-
attacks. Painful syndromes of the vertebral column, Pack: 3 mL x 10’s
non-articular rheumatism. As an adjuvant in severe POM FLOTAC® (Norvatis) clofenac sodium 1%.
painful inflammatory infections of the ear, nose or POM Diclofenac (Nemel) Capsule, Diclofenac cholestyramine 140 mg complex Pack: 50 mg
throat, e.g. pharyngo-tonsillitis, otitis. Tablet, Diclofenac (as sodium) 100 mg; s-r tab equiv. to Diclofenac sodium 75 mg. POM NACAM® (Nosak)
Dose: By mouth, Adults, 50 – 150 mg/day in divided 100 mg – 10 x 10’s (in blisters) 75 mg – 20’s Injection, Diclofenac (as Na+) 25 mg.
doses. (Dysmenorrhoea and migraine at- POM Diclofenac Potassium (Kayhelt) Dose: Adult, by mouth, 1-2 caps daily; according to
tacks: up to 200 mg/day). the severity of the disease. POM NALIDON® (Vixa)
Tablet, Diclofenac potassium 50 mg; e-c tab Tablets, Diclofenac (as Sodium) 25 mg, 50 mg;
Adolescents >14 years: 50 – 100 mg/day, 50 mg – 10’s (in blisters) POM GLOPHAC® (Goldmoore) coated tabs.
with max. daily dose of 150 mg.
POM Diclofenac Potassium (N.C.I) Injection, Diclofenac sodium 75 mg. 25 mg – 10’s.
Children >1 year: 0.5 to 2 mg/kg/day, with a
50 mg – 10’s. POM PAC-50® (Pacmai) Retard tablet, Diclofenac sodium 100 mg. POM DICLOCETAMOL® (Next Generation)
Injection, Diclofenac sodium 75 mg/3 mL. Tablet, Diclofenac potassium 50 mg; f-c tabs. 100 mg – 10; 100 Tablet, Diclofenac potassium 50 mg, paracetamol
Pack: 3 mL x 10’s. 50 mg – 1 x 12’s (in blisters) Injection, Diclofenac sodium 25 mg per mL; in 3 500 mg; f-c tab.
mL amp Pack: 1 x 10’s; 10 x 10’s
POM NERODIC® (Neros) POM PENAC® (Pemason)
Pack: 3 mL x 5’s.
Tablet, Diclofenac potassium 50 mg Injection, Diclofenac sodium 75 mg per 3 mL; amber POM Diclofenac Plus Paracetamol (Crystal)
50 mg – 2’s (in blisters) coloured amp. marked “PENAC” OTC VOLTAREN Emulgel® (Novartis) Tablet, Paracetamol 500 mg, diclofenac sodium
Pack: 3-mL x 10 x 10’s Gel, Diclofenac diethylammonium 1.16% (equiv. to 50 mg
POM NOAK SR® (Pharmaplus)
Diclofenac sodium 1%); oily emulsion in an aq. gel. Pack: 10’s (in blisters)
Tablet, Diclofenac sodium 100 mg; slow release tab. POM PYROFEN® (Standard Generics)
Pack: 20 g (in tube)
100 mg – 3 x 10’s (in blisters) Injection, Diclofenac sodium 75 mg per 3 mL. POM DICLO-P® (Vinco)
Caplet, Diclofenac sodim 50 mg, Paracetamol 500
POM NORMELGEN® (E-Globa) POM RADIKLO® (Seagreen) Indications: Localised rheumatic diseases; pain and
mg.
Injection, Diclofenac sodium 75 mg per 3 mL. Tablet, Diclofenac sodium 50 mg, 100 mg; e-c tab. inflammation due to sprains, strains, etc.
Pack: 10 x 10 (in blisters).
Pack: 3-mL x 10’s (in amps) 50 mg – 1 x 10’s; 2 x 10’s (in blisters) Dose: 2-4 mg applied locally to the skin 3-4 times
Dose: Adults, 2 caplets 2 or 3 times daily; depending
100 mg – 1 x 10’s; 2 x 10’s (in blisters) daily and rubbed in gently.
POM OFENIN® (Beta Drugs) on severity.
Injection, Diclofenac sodium 75 mg per 3 mL; in amp. POM RHEUMASTOP® (Manola) OTC VOLTINAC® (GoldMoore) Children >12 years, 1 caplet 2 or 3 times
Pack: 5’s; 10’s; 100’s. Plaster, Diclofenac diethylammonium 120 mg; Gel, Diclofenac diethylammonium 1.16% (equiv. to daily; depending on severity.
opaque plaster with pale yellow adhensive with Diclofenac sodium 1%), Oleum lini 3%, Menthol 5%
POM OLFEN® (Oculus) POM DICLOMOL® (Therapeutic)
menthol odour. w/w, Methyl salicylate 10%.
Lactabs, Diclofenac sodium 25 mg, 50 mg Caplet, Diclofenac sodium 50 mg, acetaminophen
Pack: 5 plasters per carton. Pack: 30 g tube.
25 mg – 30 500 mg.
Application method: Clean affected parts of sweats Administration: Apply to the affected site 3-4 times
50 mg – 20. 50 mg – 2 x 10’s
and moistures After taking off the middle part of the daily with rubbing till the film disappears.
Rectocaps, Diclofenac sodium 50 mg, 100 mg. Dose: Adult (>12 years): One caplet to be taken 3-4
linear, apply the exposed plaster to the middle of
50 mg – 10 POM VOLVENAC® (Hochiez) times daily. Child (6-12 years): One caplet
EMDEX
the affected body part. Pull off the remaining liners
100 mg – 5. Injection, Diclofenac 75 mg per 3 mL twice daily; 4-6 years, ½ caplet twice daily.
in a manner to closely cover the affected area. By
Depocaps, (SR), Diclofenac sodium 100 mg; as s-r Pack: 3 mL x 10 amps.
applying slight pressure to the covered area, attach OTC LABDIC Relief MR® (Embassy)
pellets.
the plaster completely over the surface. (In case that POM ZOFLAM® (Bakangizo) Tablet, Paracetamol 500 mg, diclofenac sodium
100 mg – 10; 20.
application part is narrow like finger arthritis, you Tablet, Diclofenac potassum 50 mg (as enteric coated) 50 mg, chlorzoxazone 250 mg;
Depotabs, (SR), Diclofenac sodium 75 mg
can cut the plaster into several parts). 50 mg – 10 x 10’s (in blisters) uncoated tab.
75 mg – 10’s; 30’s (in blisters)
Pack: 2 x 10’s.
Injection, Diclofenac sodium 75 mg, Lidocaine HCl POM RHEUMATIN-K® (Pharmaplus) POM ZOFLAM-S® (Bakangizo)
20 mg; in 2 mL amp. Tablet, Diclofenac potassium 50 mg Injection, Diclofenac sodium 75 mg per 3 mL; clear POM LOFNAC® Plus (Greenlife)
Pack: 2 mL x 5’s. 50 mg – 20’s (in blisters) liquid in transparent amp. Tablet, Diclofenac sodium 50 mg (as e-c granules),
Dose: Adults, 50-150 mg per day depending on the Pack: 5’s amp Paracetamol 500 mg.
OTC RUFENAC® (Shalina)
severity.Lactab, Rectocap and Depocaps Pack: 10’s (in bisters).
Gel, Diclofenac diethylammonium salt 1.16% w/w POM ZOLTEROL® SR (Goben)
Adult, by mouth, initially 150mg daily, in 2-3 Dose: Adult & child >12 years, 1 tablet 3 times daily.
equiv. to Diclofenac sodium 1.0% w/w, methyl Tablet, (75 mg), Diclofenac sodium 75 mg; pale pink,
divided doses. Both Lactab and Depocaps Not recommended for children under the
salicylate 3.0% w/w, menthol 2.0% w/w. triangular f-c, s-r tab. marked ‘CCM’.
are taken unchewed with a glass of water age of 12. Do not crush or chew. Swallow
Pack: 30 g. 75 mg – 30’s; 100’s.
before meals. To prevent nocturnal pain whole with a full glass of water.
Tablet, (100 mg), Diclofenac sodium 100 mg; pale
and morning stiffness, one Rectocap rectal POM SOOTHYS DICOPAD® (Korlyns)
red, round f-c, s-r tab. marked ‘CCM’. POM PENAC® (Pemason)
capsule (50 or 100mg) before retiring can Patch, Diclofenac sodium 140 mg
100 mg – 30’s; 100’s. Tablet, Paracetamol 500 mg, diclofenac potassium
be combined with the use of Lactab tablets Pack: 1 patch/foil; 10 foils/box
Dose: To be swallowed whole with liquid, not 50 mg
during the day.Child (>1 year): 1-3 mg/kg/ Directions: Remove the protective film while apply-
crushed or chewed. Pack: 10’s (in blisters); 10’s (in box)
day By deep intragluteal injection in the ing to the affected area. For severe or chronic cases,
Adult, 75-100 mg every morning and
upper external quadrant, Severe pain, up plaster should be changed daily. In case of sweat, POM RADIKLO® Forte (Seagreen)
evening (i.e. 100-150 mg daily)Elderly and
to 2 injections per day can be given with swab up the pained area before treating. Firmly affix Tablet, Paracetamol 500 mg, diclofenac potassium
patients with low b.wt, initially 75-150 mg
an interval of several hours, changing the with an adhesive tape or elastic bandage around 50 mg; uncoated tab
daily. For chronic treatment and in mild
injection sites. A change is made to Lactab joint areas to secure the plaster. Pack:10 x 1 x 10’s
cases, 75 mg once daily. If symptoms are
tablets after the severe pain has faded.
POM TAMAFAST® (Tamar & Pharez) most severe during the night or in the POM RUFEDOL® (Shalina)
Gel, Diclofenac sodium B.P. 10 mg per g
Tablet, Diclofenac potassium 50 mg morning, take preferably in the evening. Tablet, Diclofenac sodium 50 mg, Paracetamol 500
Pack: 20 g; 50 g in tubes.
Dose: Depending on the size of the area to be 50 mg – 1 x 10’s mg; yellow tab.
treated, apply 2-3 g 3-4 times daily and DICLOFENAC plus PARACETAMOL Pack: 10’s.
OTC TOPIRAX® (Nemel)
rub in lightly. Gel, Diclofenac diethylamine 1.16%(eq. to diclofenac See under the preparations below. POM UPFENAC® (Award Global)
POM OSTEIFEN® (N.C.I) sodium 1%), Linseed oil 3.0%, Methyl salicylate 10%, Tablet, Paracetamol 500 mg, diclofenac potassium
Tablet, Diclofenac potassium 50 mg Menthol 5%, Benzyl alcohol 1% in gel base. POM Paracetamol plus Diclofenac (N.C.I) 50 mg
50 mg – 1 x 10’s Pack: 30 g x 12’s (in tube) Tablet, Diclofenac sodium 50 mg, Paracetamol Pack: 10 x 10’s (in blisters)
POM TORANAC® (Solidum) 500 mg POM VOLVENAC-P®(Hochiez)
OTC OSTEO® Gel (Goldmoore) Pack: 2 x 10’s
Gel, Diclofenac diethylamine Tablet, Diclofenac potassium 50 mg; e-c tab. Caplet, Diclofenac potassium 50 mg, paracetamol
50 mg – 100’s POM DICLO-K® (Global) 500 mg
POM OSTEO® (Goldmoore) Tablet, Diclofenac potassium 50 mg, paracetamol Pack: 1 x 10’s (in blisters)
Tablet, Diclofenac potassium 50 mg; f-c tab. POM VOLTAREN® (Novartis)
Tablet, Diclofenac sodium 25 mg; e–c tab. 500 mg POM ZARFENAC-P® (Shrezar)
50 mg – 12’s (in blisters). Pack: 10 x 10’s; 2 x 10’s (in blisters)
25 mg – 30. Caplet, Paracetamol 500 mg, diclofenac potassium
50 mg allergic disorders; interactions: Appendix 1. POM BRUSTAN-N® (Ranbaxy) Tablet, Ibuprofen 400 mg; s-c tab.
Pack: 1 x 10’s (in blisters) Adverse effects: GI disturbances including Tablet, Ibuprofen BP 400 mg; f-c tab. 400 mg – 1 x 10’s; 50 x 10’s.
nausea, diarrhoea, dyspepsia, ulceration, 400 mg – 24 x 10’s.
+ B Vitamins POM Ibuprofen (Dortemag)
and haemorrhage; hypersensitivity reactions Oral suspension, Ibuprofen 100 mg per 25 mL, ace-
Syrup, Ibuprofen 100 mg per 5 mL
POM ATABION DICLO® (Mark) sulfame potassium 2.5 mg
including rash, angioedema, bronchospasm; Pack: 100 mL
Tablet, Diclofenac sodium 50 mg, Vitamin B1 50 mg, Pack: 60 mL; 100 mL
Vitamin B6 100 mg, Vitamin B12 100 mcg; f-c tab. headache, dizziness, nervousness, depres- POM Ibuprofen (Emzor)
sion, drowsiness, insomnia, vertigo, tinnitus, POM BUFFER 400® (Hochiez)
Pack: 100’s Capsules/Tablets, Ibuprofen 200 mg, 400 mg
photosensitivity, haematuria; fluid retention Caplet, Ibuprofen 400 mg; coated tab.
200 mg – 20; 1000.
OTC CRISTAMET® (Crystal)
(rarely precipitating congestive heart failure POM BUPROL® (Hovid)
Tablet, Vitamin B1 50 mg, Vitamin B6 100 mg, Vitamin POM INBU 200® (Strides Vital)
B12 100 mcg, diclofenac sodium 50 mg; f-c tab.
in elderly), raised blood pressure, renal failure; Tablets, Ibuprofen 200 mg, 400 mg; f-c tabs.
Tablet, Ibuprofen 200 mg; pink s-c tab. marked
rarely hepatic damage, alveolitis, pulmonary 200 mg – 500’s; 10 x 100’s (in blisters).
‘IBU 200’.
POM DICLO-NEUROBIN® (Biofem) eosinophilia, pancreatitis, visual disturbances, 400 mg – 500’s; 1000’s.
200 mg – 2 x 10’s; 1000’s.
Tablet, Diclofenac sodium 50 mg, Vitamins B1 50 mg, erythema multiforme (Stevens-Johnson POM EBU® (Mecure)
Vitamin B6 50 mg, Vitamin B12 1 mg; f-c tab. POM INBU 400® (Strides Vital)
syndrome), toxic dermal necrolysis (Lyell syn- Tablet, Ibuprofen 200 mg; red s-c tab.
Pack: 20’s. Tablet, Ibuprofen 400 mg; pink s-c tab. marked
Indications: Analgesic, antineuritic and anti-inflam- drome), colitis, aseptic meningitis. 200 mg – 2 x 10’s.
‘IBU 400’.
Advice to patients and Nursing action: See Caplet, Ibuprofen 400 mg; oblong s-c orange tab
matory. Back pain, neck pain, arm pain, radiculitis, 400 mg – 2 x 15’s; 1000’s.
under Diclofenac 400 mg – 1 x 10’s.
peripheral neuropathy of diverse etiology, facial neu-
Dose: Mild to moderate pain, pyrexia, inflam- Capsule, Ibuprofen 400 mg; light blue/dark blue cap. POM LAM® (Dana)
ralgias, diabetic neuropathy, intercostal neuralgia,
marked ‘EBU-400’. Suspension, Ibuprofen 100 mg per 5 mL
herpetic neuralgia, alcoholic neuropathy, diabetic matory musculoskeletal disorders,
400 mg – 1 x 10’s. Pack: 100 mL
neuropathy, carpal tunnel syndrome, fibromyalgia, by mouth with or after food, ADULT
spondylitis. 1.2–1.8 g daily in 3–4 divided doses, POM EMPROFEN® (Emzor) POM MAKUPAR® 200 (Goldmoore)
EMDEX
Dose: 1 tablet 2-3 times per day; to be taken with increased if necessary to max. 2.4 Capsules, Ibuprofen 200 mg, 400 mg Tablet, Ibuprofen 200 mg.
meals. Pack: 1 x 10’s; 3 x 10’s; 10 x 10’s
g daily (3.2 g daily in inflammatory POM MD-Ibuprofen (O’Nell)
POM DOLO-META B® (Vixa) disease); maintenance dose of 0.6–1.2 POM ESEFEN® (GoldMoore) Syrup, Ibuprofen 100 mg per 5 mL
Tablet, Vit B1 50 mg, B6 100 mg, B12 100 mcg, Di- g daily may be sufficient. Tablets, Ibuprofen 200 mg, 400 mg; s-c tabs. Pack: 100 mL
clofenac sodium 50 mg. Juvenile arthritis, by mouth with or 200 mg – 2 x 10; 10 x 10; 1000’s.
Pack: 10 x 10’s; 100’s. 400 mg – 10 x 10; 25 x 10; 50 x 10’s. POM MEDPROFEN® (Embassy)
after food, CHILD over 7 kg, 30–40 Tablets, Ibuprofen 200 mg, 400 mg.
POM DOLOPAIN® (Embassy) mg/kg daily in 3–4 divided doses POM GENAFEN® (Geneith) 200 mg – 20’s; 1000’s.
Tablet, Diclofenac sodium 50 mg, vitamin B1 50 mg, Pain in CHILDREN (not recommended Tablets, Ibuprofen 200 mg, 400 mg.
vitamin B6 100 mg, vitamin B12 100 mcg; uncoated 200 mg – 2 x 10’s POM NIPROFEN® (Award Global)
for child under 7 kg), by mouth with Capsule, Ibuprofen 400 mg
tab. or after food, 20–40 mg/kg daily in 400 mg – 1 x 10’s
Pack:100’s Syrup, Ibuprofen 100 mg per 5 mL. 400 mg – 2 x 10’s; 1 x 10’s
divided doses or 1–2 years 50 mg 3–4
Indications: Musculoskeletal and joint disorders, Pack: 100 mL POM PIBUFEN® (Shrezar)
inflammation, pain, neuralgia and neuritis (Neu-
times daily, 3–7 years 100 mg 3–4
POM IBUDEX® (Pemason) Tablet, Ibuprofen 400 mg; s-c tab
ropathies). times daily, 8–12 years 200 mg 3–4
Tablet, Ibuprofen 400 mg; white oblong scored tab. 400 mg – 1 x 10’s; 50 x 1 x 10’s; 10 x 10’s (in blisters)
Dose: Adult: One tablet thrice daily times daily.
400 mg – 10 x 10’s (in blisters) POM PROFEN® (Jopan)
POM UPBION® (Award Global) POM Ibuprofen (WMF 2.1) Caplet, Ibuprofen 400 mg Tablet, Ibuprofen 200 mg; pink s-c tab.
Tablet, Diclofenac sodium 50 mg, vitamin B1 50 mg, Tablets, Ibuprofen 200 mg, 400 mg. 400 mg – 50’s; 100’s (in blisters) 200 mg – 2 x 10’s (in blisters); 1 x 1000’s (in jar).
vitamin B6 100 mg, vitamin B12 100 mcg; uncoated POM Ibuprofen (EDL 2.4) Caplet, Ibuprofen 400 mg; orange f-c caplet.
tab. POM IBULAB® (Embassy)
Tablets or Capsules, Ibuprofen 200 mg, 400 mg Tablets, Ibuprofen 200 mg, 400 mg. 400 mg – 1 x 10’s; 10 x 10’s (in blisters).
Pack: 10’s
POM ACTIFEN® (Diamond Remedies) 200 mg – 2 x 10’s. POM RECFEN® (GoldMoore)
Tablet, Ibuprofen 200 mg; pink s-c tab. marked 400 mg – 20’s. Tablets, Ibuprofen 200 mg, 400 mg; s-c tabs.
IBUPROFEN
‘IBU 200’. POM IBUMED® (Sterling drugs) 200 mg – 1 x 10’s.
Indications: Pain and inflammation in rheu- 200 mg – 2 x 10. 400 mg – 1 x 10’s.
Suspension, Ibuprofen 100 mg per 5 mL
matic disease and other musculo-skeletal
POM ASKAFEN® (Diamond Remedies) Pack: 100 mL POM REPROFEN® (Reals)
disorders including juvenile arthritis; mild to
Tablet, Ibuprofen 200 mg; s-c tab. POM IBUNEX® (Titan) Oral suspension, Ibuprofen 100 mg per 5 mL
moderate pain including dysmenorrhoea, Pack: 100 mL.
200 mg – 2 x 10. Tablet, Ibuprofen 200 mg.
headache; pain in children; acute migraine Indications: Relief of fever including fever caused
attack (section 1.9.1). POM BEFLAM® (Bentos) 200 mg – 1000.
by immunisation; relief of pain from teething and
Contra-indications: Hypersensitivity (includ- Capsule, Ibuprofen 200 mg; pink/pink cap. marked POM IBUPAIN® Forte (Adler) toothache, earache, sore throats, headache and
ing asthma, angioedema, urticaria or rhinitis) “Beflam” and “Bentos”. Tablet, Ibuprofen 400 mg. minor aches and sprains.
to acetylsalicylic acid or any other NSAID; active POM BENBRUFEN® (Nichben) 400 mg – 12. Dose: Child (6-12 months), 2.5 mL 3-4 times in 24
peptic ulceration. Capsule, Ibuprofen 200 mg hours; 1-3 years, 5 mL 3 times in 24 hours;
POM IBUPARA® (RichyGold)
Precautions: Renal impairment (Appendix 4); 200 mg – 1 x 10’s; 10 x 1 x 10’s; 50 x 1 x 10’s 4-6 years, 7.5 mL 3 times in 24 hours; 7-9
Capsule, Ibuprofen, Paracetamol.
years, 10 mL 3 times in 24 hours; 10-12 years,
hepatic impairment (Appendix 5); preferably POM BRUPAED® (Pharmabase) POM Ibuprofen (Afrab-Chem) 15 mL 3 times in 24 hours.
avoid if history of peptic ulceration; cardiac dis- Syrup, Ibuprofen 100 mg per 5 mL; in a flavoured Suspension, Ibuprofen 100 mg per 5 mL.
ease; elderly; pregnancy (Appendix 2); breast- syrupy base. POM REXIFEN® (SKG)
Pack: 100 mL.
feeding (Appendix 3); coagulation defects; Pack: 100 mL. Paediatric suspension, Ibuprofen 100 mg per 5 mL.
POM Ibuprofen (Diamond Remedies) Pack: 100 mL.
POM S-FEN® (Greenlife) driving and performance of other skilled tasks). POM MAXINDO® (Goldmoore) Pack: 10’s (in blisters)
Oral suspension, Ibuprofen 100 mg per 5 mL; fla- Prolonged use may cause corneal deposits and Capsule, Indomethacin.
POM KETOVAIL® (May & Baker)
voured syrup base retinal disturbances including that of macula POM METHACIN® (Hovid) Capsule, Ketoprofen 200 mg; controlled-release
Pack: 100 mL (advise patient to discontinue medication Tablet, Indometacin 25 mg; f-c tab. pellets in pink/white cap. marked “KETOVAIL 200”
POM TABALON® (NGC) promptly and to notify physician if visual dis- 25 mg – 1000 in black.
Tablet, Ibuprofen 400 mg turbances occur). History of gastro-intestinal Capsule, Indometacin 25 mg. 200 mg – 2 x 7’s; 20 x 7’s.
400 mg – 5 x 4’s; 25 x 4’s ulceration or bleeding; elderly. 25 mg – 10 x 10; 500; 1000. Dose: Adult, by mouth, 200 mg once daily.
POM TABUFEN® (Fidson) Adverse effects: GI reactions including nausea, POM NAXA®-25 (Jubilee) POM ORUCOTE® (May & Baker)
Tablet, Ibuprofen 400 mg. diarrhoea, dyspesia, vomiting, abdominal pain Capsule, Indomethacin 25 mg; yellow cap. Gel, Ketoprofen 2.5 g per 100 g; non-greasy,
or constipation; occasionally GI haemorrhage 25 mg – 100’s; 1,000’s. non-staining gel with cooling effect.
POM VPL-Ibuprofen (Vixa)
and ulceration (give with food or milk to Indications: Acute, painful musculoskeletal con-
Oral suspension, Ibuprofen 100 mg per 5 mL; syrupy POM ROMACID® (Geneith)
minimize such effects). CNS effects namely ditions caused by trauma such as sports injuries,
base. Capsule, Indometacin 25 mg.
headache, dizziness, and tinnitus; less com- sprains, strains and contusions.
100 mg – 100 mL in amber colored bottle. 25 mg – 10’s; 1000’s.
Dose: Usually about 15 g per day; to be applied 2
monly somnolence, fatigue and confusion.
POM ZEDFEN® (Justeen) to 4 times daily to the skin in the painful or
Others include renal failure, hepatic damage, KETOPROFEN inflamed region for up to 7 days.
Tablet, Ibuprofen BP 400 mg.
400 mg – 1 x 10’s. hyperkalaemia, Stevens-Johnson syndrome. Indications: Rheumatoid arthritis, osteoar- Note: To be avoided in patient with ex-
See also under Precautions. thritis, gout, ankylosing spondylitis, acute udative dermatoses, eczema, sores and
INDOMETACIN Advice to patients and Nursing action: See articular and periarticular disorders (bursitis, infected skin lesions or broken skin. Safety
under Diclofenac. capsulitis, synovitis, tendinitis), fibrositis, cervi- in children is not yet established.
Synonym: Indomethacin.
Dose: By mouth, moderate to severe rheuma- cal spondylitis, low back pain (strain, lumbago, POM ORUJECT® (May & Baker)
Pharmacology: Indometacin is a NSAID with
toid arthritis (including acute flares of sciatica), painful musculo-skeletal conditions Injection, Ketoprofen 50 mg per mL; in 2 mL amp.
anti-inflammatory, antipyretic and analgesic
EMDEX
chronic disease), ankylosing spondylitis and dysmenorrhoea.
properties. It is a potent inhibitor of prostaglan- POM ORUVAIL® (Sanofi-Aventis)
and osteoarthritis, 25 mg 2-3 times Contra-indications, Precautions, etc.: See
din synthesis; its mode of action may be due Capsule, Ketoprofen 200 mg; white/pink cap. marked
daily; increased according to patient’s under Indometacin.
to a decrease of prostaglandins in peripheral ‘ORUVAIL 200’ in blue holding white pellets.
needs by 25-50 mg at weekly inter- Advice to patients and Nursing action: See 200 mg – 14’s.
tissues. See notes above.
vals up to a max. 150-200 mg daily. under Diclofenac.
Indications: Acute and chronic musculoskeletal
Acute painful shoulder (bursitis or tend- Dose: Adult, by mouth, 100-200 mg daily in KETOROLAC
and arthritic disorders such as rheumatoid
initis), 75-150 mg daily in 3-4 divided 2-4 divided doses; 200 mg once daily Therapeutic category: NSAID.
arthritis, juvenile rheumatoid arthritis, osteoar-
doses. Usual course of therapy is 7-14 for the s-r prep., to be taken with Indications: Short-term management of mod-
thritis, ankylosing spondylitis, lumbago, gout,
days. Discontinue gradually. food, depending on patient weight erate to severe pain.
degenerative joint disease of the limbs, inflam-
Acute gout, 50 mg 3 times daily until and severity of symptoms. Contra-indications: Hypersensitivity to ke-
mation and pain following orthopaedic surgery
pain is treatable, then rapidly reduce By deep IM injection, 100 mg every torolac trometamol, aspirin or other NSAIDs;
or dental procedures; fever, dysmenorrhoea.
the dose to complete cessation of 12 hours; up to a max. 200 mg in 24
Contra-indications: History of hypersensitivity acute peptic ulcer or recent GI bleeding or
the drug. hours. perforation; history of peptic ulcer disease or GI
to aspirin or other NSAIDs including those in
Dysmenorrhoea, up to 75 mg daily as Child: Not recommended for child bleeding; severe renal impairment or patients
whom asthmatic attacks, angioedema, urti-
a single or in divided doses. <12 years. at high risk of renal failure; suspected or con-
caria or rhinitis have been precipitated by as-
Child: Not recommended for child Note: Avoid IV use. Limit injection to firmed cerebrovascular bleeding, hemorrhagic
pirin or any other NSAIDS. Children <14 years;
<14 years. the acute stage of disease. diathesis, incomplete hemostasis and those at
active peptic ulcer; pregnancy, breast-feeding.
Precautions: May mask the signs and symp- POM Indometacin (EDL 2.4) POM Ketoprofen (EDL 2.4) high risk of bleeding; concomitant use of other
toms of infection (use with in existing infection). Capsule, Indometacin 25 mg. Gel, Ketoprofen 2.5% NSAIDs and probenecid; labour & delivery;
Fluid retention and peripheral oedema may POM ARTHRACID® (Strides Vital) lactation; hypovolaemia or dehydration; avoid
POM APO-KETO SR® (Lahams)
occur with Indometacin like other NSAIDs (use Capsule, Indometacin 25 mg. Tablet, (Slow-release), Ketoprofen 200 mg; white, e-c
epidural or intrathecal administration.
cautiously in cardiac dysfunction, hypertension 25 mg – 10 x 10’s. s-r tab. marked ‘APO’ on one side and ‘200’ on reverse. Precautions: Patients receiving anticoagulant
or other conditions pre-disposing to fluid 200 mg – 100’s. therapy and patients with hemophilia; may
POM DOLOCIN® (Ranbaxy)
retention). May prolong bleeding time, so use Capsule, Indometacin 25 mg inhibit platelet aggregation and prolong
POM KETONAL® (Taylek)
with caution in coagulation disorders. Severe 25 mg – 10’s; 1000’s. bleeding time, therefore, avoid giving before
Tablet Retard, Ketoprofen 150 mg.
hepatic reactions including jaundice and fatal 150 mg – 20. surgery; patients with haemostasis disorders;
POM EMBACID® (Embassy)
hepatitis may occur with Indometacin as with Dose: Adult, by mouth, 150 mg twice daily; to be cardiac decompensation, acute renal failure,
Capsule, Indometacin 25 mg.
other NSAIDs (discontinue therapy if abnormal 25 mg – 100’s; 1000’s. taken at 12 hourly intervals with food. hypertension or other conditions associated
liver test persists or worsens). Prolonged use Injection, Ketoprofen 50 mg per mL; in 2 mL amp. with fluid retention; impaired hepatic function
may lead to renal disorders including acute POM INDOBETA-25® (Beta Drugs) Pack: 2 mL x 10’s. or history of hepatic disease; children under
nephritis with haematuria, proteinuria and oc- Capsule, Indometacin 25 mg. Cream, Ketoprofen 50 mg per g. 16 years.
casionally nephrotic syndrome. May aggravate POM INDOCET® (Adler) Pack: 30 g (in tube). Interactions: Anticoagulants, other NSAIDs,
depression or other psychiatric disturbances, Capsule, Indometacin 25 mg. Dose: Apply to the affected site 3-4 times daily. methotrexate, lithium, probenecid, furo-
epilepsy and parkinsonism. May cause drows- 25 mg – 30. POM KETONAL DUO® (Taylek) semide, ACE inhibitors, antiepileptic drugs,
iness and alteration in motor coordination POM Indometacin (Emzor) Capsule, Ketoprofen 150 mg; modified-release psychoactive drugs.
(counsel patient on the possible effect on Capsule, Indometacin 25 mg hard pellets. Adverse effects: Edema, hypertension, pruri-
tus, rash, nausea, dyspepsia, GI pain, diarrhoea, drowsiness. severe renal failure; history of cerebrovascular No dose reduction is required in
constipation, flatulence, GI fullness, vomiting, Adverse effects: GI disturbances; diarrhoea bleeding or other bleeding disorders; severe patients with mild to moderate renal
stomatitis, purpura, cephalgia, drowsiness, or skin rash (discontinue); peptic ulceration, heart failure. impairment
dizziness, swelling; pain on injection site. See GI bleeding, headache, drowsiness, dizziness, Precautions: Avoid coadministration with Hepatic impairment: No dose reduc-
BOC for the full listing. nervousness, visual disturbances, thrombocy- other NSAIDs including COX-2 inhibitors; tion is required in patients with mild
Dose: For the short-term management of pain, topenia, haemolytic anaemia. history of GI disease (ulcerative colitis, Crohn’s to moderate hepatic impairment.
initially 30 or 60 mg IM; then 15 or 30 Advice to patients: Administer after meals disease); history of hypertension and/or mild to (Additional information sourced from Mobic monograph: http://
mg every 6 hours if necessary. Max. or with food, milk or antacids to reduce GI moderate CHF as fluid retention and oedema www.medicines.org.uk/EMC/medicine/293/SPC/Mobic)
daily dose is 120 mg (upto 150 mg in irritation. may occur; discontinue at the first appearance
the first day of treatment if needed). Nursing action: See under Diclofenac. of skin rash, mucosal lesions, or any other sign POM MEFLEX® (Al-Tinez)
30-mg (IM) dose is optimal dose for Dose: By mouth, Adult, initially 500 mg; of hypersensitivity; monitor diuresis and renal Tablet, Meloxicam 7.5 mg; f-c tab
Pack: 2 x 10’s (in blisters)
relieving moderate post-operative followed by 250 mg every 6 hours as function especially in high risk patients e.g.
pain (upto 90-mg dose for severe required. elderly; may induce sodium, potassium and POM MELOCAP® (Evans)
pain). water retention; may impair ability to drive or Tablets, Meloxicam 7.5 mg, 15 mg.
POM HOSTAN® (Hovid) Injection, Meloxicam 5 mg per mL; in 3-mL amp.
Note: Total duration of use (IV and IM) should not operate machinery; pregnancy (avoid in 3rd
Tablet, Mefenamic acid 500 mg. Pack: 3-mL x 1’s
exceed 5 days. Hypovolemia should be corrected trimester), lactation.
500 mg – 10 x 10; 500; 1000. Dose: Adult, by IM injection, 1 ampoule once daily.
prior to the administration; IV bolus must be given Interactions: Other NSAIDs; Corticosteroids
over no less than 15 seconds. IM injection should POM PONREX® (Embassy) POM Meloxicam (Crystal)
(increased risk of bleeding or GI ulceration);
be given deeply and slowly. Onset of analgesic Tablet, Mefenamic acid 500 mg; uncoated tab. Tablet, Meloxicam 7.5 mg
effect is 30 minutes and maximum effect occurs 500 mg – 10 x10’s. Anticoagulant such as warfarin or heparin
(increased risk of bleeding); SSRIs (increased 7.5 mg – 10’s (in blisters)
in 1-2 hourus after IV or IM. Duraction of analgesic
POM UREMINE® (Vixa) risk of bleeding); may reduce effect of diuretics POM Meloxicam (Dabak)
effect is usually 4-6 hours. For breakthrough pain,
EMDEX
Tablet, Mefanamic acid 500 mg.
do not increase the dose or the frequency; consider and other antihypertensive drugs; Calcineurin Tablet, Meloxicam 7.5 mg
Pack: 10 x 10’s. 7.5 mg – 1 x 10’s
adding low-dose opioid to the regimen, unless inhibitors e.g. cyclosporin, tacrolimus (in-
contrai-indicated. creased risk of nephrotoxicity); Methotrexate
MELOXICAM POM XOBIX® (CG Biostadt)
POM KETANOV MD® (Ranbaxy) (reduced tubular secretion of MTX leading to its Tablets, Meloxicam 7.5 mg, 15 mg.
Therapeutic category: NSAID, oxicam. increased plasma concn); may cause decreased
Tablet,(Mouth dissolving), Ketorolac trometamol 7.5 mg – 10’s
10 mg
Pharmacology: Meloxicam, an oxicam deriv- renal excretion of lithium; increased clearance 15 mg – 10’s
ative, is a member of the enolic acid group with cholestyramine.
POM REMOPAIN® (Reals) of nonsteroidal anti-inflammatory drugs Adverse effects: Dyspepsia, nausea, vomit- NAPROXEN
Injection, Ketorolac trometamol 10 mg, 30 mg per (NSAIDs). It has anti-inflammatory, analgesic
mL; in amps. ing, abdominal pain, constipation, flatulence, Indications: Rheumatoid arthritis, osteoarthri-
and antipyretic properties. Meloxicam in- diarrhoea; Headache, dizziness, somnolence;
Pack: 10 mg/mL 5’s; 30 mg/mL x 5’s tis, ankylosing spondylitis, acute musculoskel-
Dose: Single dose: By IM injection, Adult (<65 yr):
hibits prostaglandin synthesis by reducing Sodium and water retention, hyperkalaemia; etal disorders and dysmenorrhoea, acute gout,
60 mg; >65 yr with renal impairment &/or cyclooxygenase enzyme activity. This results increased blood pressure; oedema. Rarely juvenile arthritis.
<50 kg, 30 mg. in decreased production of prostaglandins, skin rash; visual disturbance including vision Contra-indications, Precautions, Adverse ef-
By IV injection, Adult (<65 yr): 30 mg; >65 yr known inflammation mediators. blurred; GI haemorrhage, ulceration or per- fects, Nursing action, and Advice to patients:
with renal impairment &/or <50 kg, 15 mg. Well absorbed from the GI tract, with absolute foration. See under Diclofenac.
Repeated dosing: By IM/IV injection, Adult bioavailability of 89% following oral adminis-
(<65 r): 30 mg every 6 hours. Max. 120 mg/
Dose: The total daily amount should be Dose: By mouth, Adult, 0.5-1.0 g daily in 2
tration. Tmax is 5-6 hours with oral solid dosage taken as a single dose, with water or
day; 65 yr with renal impairment &/or <50 divided doses.
forms (tablets). 99% bound to plasma proteins; another liquid, during a meal. Unde-
kg, 15 mg every 6 hours. Max: 60 mg/day. Acute musculoskeletal disorders and
achieves concns in synovial fluid approx. half sirable effects may be minimised by dysmenorrhoea, initially 500 mg, then
of those in the plasma. Undergoes extensive using the lowest effective dose for
MEFENAMIC ACID 250 mg 6-8 hourly as required; up to a
hepatic biotransformation to inactive metab- the shortest duration necessary to
Indications: Mild to moderate pain including max. daily dose of 1250 mg after the
olites, mediated via mainly CYP2C9. Excreted control symptoms.
headache, dental pain, postoperative and first day.
equally in urine and faeces in the form of By mouth, Adult, Exacerbations of
postpartum pain, dysmenorrhoea; rheumatic Acute gout, initially 750 mg, then 250
inactive metabolites. osteoarthrosis, 7.5 mg/day; may be
disorders such as osteoarthritis and rheuma- mg 8 hourly until attack is over.
Indications: Short-term symptomatic treat- increased to max. 15 mg/day.
toid arthritis. Child, (over 5 years): Juvenile arthritis,
ment of exacerbations of osteoarthrosis. Long Rheumatoid arthritis, ankylosing spon-
Contra-indications: Hypersensitivity to me- 5 mg/kg b.wt. twice daily.
term symptomatic treatment of rheumatoid dylitis, 15 mg/day; may be reduced
fenamic acid; cross-sensitivity to aspirin and arthritis or ankylosing spondylitis. POM Naproxen (EDL 2.4)
other NSAIDs; intestinal ulceration or inflam- based on therapeutic response to 7.5 Tablet, Naproxen 250 mg
Contra-indications: Hypersensitivity to mg/day. Do not exceed the dose of
matory bowel disease; avoid use in children meloxicam, other NSAIDs, aspirin; history of POM Apo-Naproxen (Lahams)
<14 years. 15 mg/day.
asthma, nasal polyps, angioneurotic edema Children (<16 years): Not recom- Caplet, Naproxen 500 mg; yellow scored cap-
Precautions: Impaired renal or liver function; or urticaria following use of aspirin or other sule-shaped tab. marked ‘APO 500’.
elderly with dehydration and renal disease; mended. 500 mg – 100’s.
NSAIDs; 3rd trimester of pregnancy; children Elderly: For long term treatment of
diarrhoea or skin rash (discontinue); bronchial (<16 years); history of GI bleeding or perfo- rheumatoid arthritis and ankylosing POM BUTROXEN® (JB Pharma)
asthma or allergic disease; factors associated ration related to NSAIDs therapy; active, or Tablet, Naproxen 500 mg
with peptic ulcer disease such as alcoholism, spondylitis, 7.5 mg per day.
history of recurrent peptic ulcer/haemorrhage; Renal impairment: Do not exceed 7.5 500 mg – 50’s
smoking, corticosteroid therapy; may cause severely impaired liver function; non-dialysed mg per day in severe renal failure. POM CEDAX® (Vixa)
Tablet, Naproxen 500 mg NIMESULIDE 100 mg – 12 x 20’s (in blisters). yet established.
500 mg – 2 x 10’s Pharmacology: Nimesulide is a NSAIDs of the POM SUGAM® (Jawa) POM FELGIN®-20 (Jubilee)
POM HOPROXEN® (Hovid) sulfonanilide class. It has anti-inflammatory Suspension, Nimesulide 50 mg per 5 mL. Capsule, Piroxicam 20 mg; maroon/maroon cap.
Tablet, Naproxen 250 mg; yellow tab. activity similar to or greater than that of Indo- Pack: 60 mL x 20’s. 20 mg – 100’s.
250 mg – 500’s. metacin, diclofenac, piroxicam and ibuprofen; POM FELOXIN® (Diamond Remedies)
POM NAXEN® (Swipha) the analgesic efficacy is similar to that of PIROXICAM Capsule, Piroxicam 20 mg; bright red cap. marked
Tablets, Naproxen 250 mg, 500 mg. ibuprofen and less than that of Indometacin; Indications: Rheumatoid arthritis, juvenile with brand name and strength.
250 mg – 20’s; 200’s. the antipyretic effect is superior to that of In- rheumatoid arthritis, osteoarthritis (arthrosis, 20 mg – 10 x 10.
500 mg – 20’s; 100’s. dometacin, ibuprofen, aspirin and paracetamol. degenerative joint disease), ankylosing spon- POM FELVIN® (Greenlife)
POM RAPROX® (Seagreen) It acts through a variety of mechanisms which dylitis, acute musculoskeletal disorders includ- Capsule, Piroxicam 20 mg.
Tablet, Naproxen 500 mg includes selective cyclo-oxygenase 2 inhibi- ing tendinitis, sprains and low back pain; acute 20 mg – 10 x 10 (blister).
500 mg – 2 x 10’s tion. Oral drug absorption is nearly complete gout, post–operative pain and post-traumatic
POM FELXICAM® (Hovid)
and concomitant administration of food may pain; primary dysmenorrhoea in patients 12
POM RELEV® (Swipha) Capsule, Piroxicam 20 mg.
Tablet, Naproxen (as sodium) 250 mg. decrease the rate, but not the extent, of ab- years and above; fever and pain associated with 20 mg – 100; 1000; 10 x 10 (blister).
250 mg – 20’s; 200’s. sorption of nimesulide. It is extensively bound acute upper respiratory tract inflammation.
to plasma proteins, extensively metabolised Contra-indications, Precautions, Adverse ef- POM FLEXODENE® (Neimeth)
POM RELEV® Rapid (Swipha) Capsules, Piroxicam 10 mg, 20 mg.
and excreted mainly in the urine. fects, Nursing action, and Advice to patients:
Tablet, Naproxen sodium 550 mg; yellow, oblong, 10 mg – 20’s; 100’s.
half scored tab. marked ‘SWIPHA’ on one side and
Indications: Treatment of a variety of painful See under Diclofenac. 20 mg – 10’s; 50’s.
‘RLV 550’ on the reverse. inflammatory conditions including, oste- Dose: By mouth, initially 20 mg daily as a sin- Tablet (Dispersible), Piroxicam 20 mg.
550 mg – 20’s; 100’s. oarthritis, rheumatoid arthritis, oncology, gle dose; maintainance dose, 10-30 20 mg – 10’s; 50’s.
Dose: Adults, Usually 550-1100 mg daily in 2 divided post-operative trauma, sports injuries, ENT mg daily as single or divided doses. Injection, Piroxicam 20 mg per mL.
EMDEX
doses at 12 hour intervals; may be increased disorders, dental surgery, bursitis/tendintis, See also under preparations below. Pack: 10’s; 50’s.
to 1650 mg/day depending on response thrombophlebitis, upper airways inflammation POM Apo-Piroxicam (Lahams) POM GEVICAM® (Geneith)
and tolerance.Analgesic and antipyretic, and gynaecological disorders. Capsule, Piroxicam 20 mg; maroon cap. marked Capsule, Piroxicam 20 mg.
Initially 550 mg, followed thereafter by Contra-indications: Active peptic ulcer dis- ‘APO 20’. 20 mg – 10’s (in blister)
275 mg at 6-8 hour intervals. Rheumatoid
ease, moderate to sever hepatic impairment, 20 mg – 100’s.
arthritis, osteoarthritis and ankylosing POM GLOXICAM® (Hochiez)
spondylitis, Initially 550-1100 mg daily in 2
severe renal failure; pregnancy, breast-feeding.
POM ARTRITE® (Strides Vital) Capsule, Piroxicam 20 mg.
divided doses at 12 hour intervals. Mainte- Precautions: Renal impairment, cirrhosis of Capsule, Piroxicam 20 mg; red cap. marked ‘ARTRITE’ 20 mg – 10 x 10’s.
nance treatment: 550-1100 mg per day, in liver, CHF, renovascular disease or those who 20 mg – 10 x 10’s.
2 divided doses at 12 hour intervals. Adjust are volume or salt depleted. Periodic liver POM INTACAM® 20 (RichyGold)
POM CICAM® (Justeen) Capsule, Piroxicam 20 mg.
morning and evening doses based on the function tests are required for prolonged
predominant symptoms i.e. night time pain Capsule, Piroxicam BP 20 mg. 20 mg – 10 x 10’s; 1 x 10’s.
therapy (discontinue drug immediately if liver
or morning stiffness.Alternatively, 550-1100 Pack: 10 x 10’s.
test worsens). POM JUROXICAM® (Juhel)
mg given as a single dose in the morning Adverse effects: GI disturbances namely epi- POM CIKADENE® (Michelle Lab) Capsule, Piroxicam 20 mg; maroon red cap. marked
or evening.Migraine headaches, Prophy- Capsule, Piroxicam 20 mg ‘Juhel 20’.
gastralgia, heartburns, nausea, diarrhoea and
laxis: 550 mg twice daily; discontinue if no 20 mg – 100’s; 10 x 10’s (in blisters) 20 mg – 10 x 10’s; 1000’s.
improvement within 4-6 weeks. Treatment: vomiting; dermatological reactions including
825 mg at the first symptom of an impend- rash and pruritus; CNS effects such as dizziness, POM FELDENE® (Pfizer) POM MAIXICAN® (Pacmai)
ing attack; may take additional 275-550 somnolence and headache. Occasionally, Capsules, Piroxicam 10 mg, maroon/blue cap.; 20 Capsule, Piroxicam 20 mg; hard gelatin caps.
mg during the day, if necessary, but not excessive perspiration, flushing, hyperexcita- mg, maroon cap. Both marked ‘PFIZER’ and ‘FEL 20 mg – 10 x 10’s (in blisters)
before ½ hour after the initial dose. Uterine bility and sleep disorders. Rarely, a rise in liver 10’ or ‘FEL 20’.
POM MAXCAM® (Goldmoore)
relaxation and analgesia in the postpartum 10 mg – 20; 100.
enzyme levels. Capsule, Piroxicam 20 mg.
non-nursing mother, in dysmenorrhea and 20 mg – 10; 50.
Dose: By mouth, Adult, 100 mg twice daily; Tablet (Dispersible), Piroxicam 20 mg, white oblong
20 mg – 10 x 10’s; 1 x 10’s (in blisters).
following IUD insertion, 550 mg initially, increased if necessary to 200 mg
followed thereafter by 275 mg at 6-8 hour tab. marked ‘PFIZER’ and ‘FEL 20’. POM MF-20® (Embassy)
twice daily 20 mg – 10; 50. Capsule, Piroxicam 20 mg.
intervals. Reducing menstrual blood loss,
825-1375 mg per day in 2 doses on the first POM ASKANYM® (Diamond Remedies) Injection, Piroxicam 20 mg per mL; in 1 mL amp. 20 mg – 10 x 10’s; 1 x 10’s (in blisters).
day of menstrual bleeding. 550-1100 mg Tablet, Nimesulide 100 mg; uncoated tab. Pack: 10; 50.
Gel, Piroxicam 0.5%; clear pale yellow gel in tube. POM NEUROXICAM® (Drugfield)
per day thereafter in 2 doses, as needed, for 100 mg – 2 x 10’s.
Pack: 25 g; 50 g. Gel, Piroxicam 5 mg
no longer than 5 days. Acute gout, initially
POM NIMICA® (IPCA) Indications: Osteoarthritis (arthrosis, degenerative 5 mg – 25 g
825 mg, followed in 8 hours with 550 mg
Tablet, Nimesulide BP 100 mg. joint disease), post traumatic or acute musculoskel- Capsule, Piroxicam 20 mg
and thereafter 275 mg at 8 hour intervals
100 mg – 10’s. etal disorders including tendonitis, tenosynovitis, 20 mg – 1 x 10’s; 10 x 10’s (in blisters)
until the attack has passed.
Suspension, Nimesulide 50 mg per 5 mL. periathritis, sprains, strains and low back pain. Injection, Piroxicam 20 mg per mL; in 1mL amp
Children: For juvenile rheumatoid arthritis,
Pack: 30 mL; 60 mL. Dose: Usually about 1 g gel (i.e., 5 mg piroxicam) Pack: 1 mL x 100’s
Usually 11 mg/kg daily in 2 divided doses at
12 hour intervals. Analgesic and antipyretic POM NIPAN® (Pharmabox) to be applied to the affected site 3-4 times POM PEMAXICAM® (Pemason)
use in children, initially 11 mg/kg, followed Tablet, Nimesulide 100 mg; light yellow oblong tab. daily. Capsule, Piroxicam 20 mg; sugar-free.
by 2.75-5.5 mg/kg at 8 hour intervals; not ex- 100 mg – 20’s; 100’s. Note: No occlusive dressing should be em- 20 mg – 100’s
ceeding 16.5 mg/kg/day after the first day. ployed. Rub in the gel leaving no residue on
POM ONAXO® (Diamond Remedies) the skin. Do not apply to the eyes, mucosa POM PIKADENE® (Diamond Remedies)
Tablet, Nimesulide 100 mg; uncoated tab. or to open skin lesion. Safety in children not Capsule, Piroxicam 20 mg
100 | 2.1.1 Non-steroidal anti-inflammatory drugs (NSAIDs) 2.1.2 Disease-modifying antirheumatic drugs (DMARDs) | 101
20 mg – 10 x 20’s; 100’s TENOXICAM pain, nausea, diarrhea and constipation, gas- may be life threatening; careful monitoring
POM Piroxicam (Embassy) Therapeutic category: NSAID, COX-II inhibitor. trointestinal bleeding. Skin and soft tissue: is needed to avoid severe toxicity. Blood dis-
Injection, Piroxicam 20 mg; in 1 mL amp. Pharmacology: Tenoxicam, a thienothiazine Itching, rash, erythema, urticaria rarely occur. orders (bone marrow suppression) can occur
Pack: 1 mL x 10’s (in amps) derivative of the oxicam class, is a NSAID. It has Renal: Increased BUN and serum creatinine during treatment with many DMARDs; blood
anti-inflammatory, analgesic and antipyretic levels. CNS: Dizziness, headache, vertigo. Liver counts should be carried out before and during
POM PIROXILEX® (Med Impex)
Capsule, Piroxicam 20 mg. activities and it also prevents platelet aggre- and Biliary Tract: Increase SGOT, SGPT, Gamma treatment, and patients should be advised to re-
20 mg – 1 x 10’s (in blisters). gation. Tenoxicam exerts its anti-inflammatory GT and bilirubin levels. Rarely, hematopoetic port without delay any unexplained symptom
Dose: By mouth, Adult, 20 mg once daily. Because effects by inhibiting preferentially, cyclooxy- system side effects including decreased hemo- such as bleeding, bruising, purpura, infection,
of the long half life, dosage changes should genase enzyme and subsequent prostaglandin globin levels and granulocytopenia. sore throat or fever. It has been suggested
be made after 2 weeks of therapy.In acute production in arachidonic acid metabolism. It Dose: Adult, by mouth, rheumatic disease, 20 that combinations of DMARDs may be more
musculoskeletal conditions, initially 40 mg has greater inhibitory effect on cycloxygenase mg daily. Acute musculoskeletal disor- effective than single drugs but increased tox-
once daily for 2 days followed by 20 mg ders, 20 mg daily for 7 days; max. 14 icity may be a problem; whether used alone
II (COX II) than cycloxygenase I (Cox I). It has
daily for 1 to 2 weeks. In acute gout, 40 mg days. Not recommended for children. or in combination, they should be prescribed
may be given for 5 to 7 days. no therapeutic effect on lipooxygenase en-
zyme. Its ability to inhibit leucocyte functions By IV or IM injection, for initial treat- only by specialists to ensure that they are used
Children: Not recommended.
including phagocytosis and histamine release ment for 1-2 days, 20 mg once a day; safely and to best advantage.
POM PIXAM® (Foundation) and to eliminate active oxygen radicals in the may be reduced to 10 mg daily for
Capsule, Piroxicam 20 mg.
Sulfasalazine has a beneficial anti-inflam-
inflammation site, contributes to its anti-in- maintenance. matory effect and is considered by some
20 mg – 10 x 10’s. In acute attacks of gouty arthritis, 40
flammatory activity. The pharmacokinetic rheumatologists to be a first-line DMARD,
POM PIXICAM® (Fil) profile of Tenoxicam after parenteral admin- mg daily for the first 2 days followed but it is poorly tolerated by about 25% of
Capsule, Piroxicam 20 mg. istration is similar to that observed following by 20 mg daily for 5 days. patients. Adverse reactions include blood
20 mg – 10 x 10’s (in blister).
oral administration, however, higher plasma POM COTIXIL® (Neros) disorders, hepatotoxicity, skin reactions and
EMDEX
POM PROTEGE® (Mecure) concentrations are achieved within the first 2 Tablet, Tenoxicam 20 mg; f-c tab. GI disturbances.
Capsule, Piroxicam 20 mg; red cap. marked ‘PROTEGE’. hours after parental administration. 20 mg – 2 x 8’s (in blisters).
20 mg – 10 x 10’s. Methotrexate, an immunosuppressant, is
Indication: Management of pain and in- POM REGACAM® (Lifeback) considered to be a first-line DMARD; at the
POM REUMADENE® (L.B.S.) flammation in rheumatic disease and other Capsule, Tenoxicam 20 mg low doses used for rheumatoid arthritis it is
Capsule, Piroxicam 20 mg. musculoskeletal disorders. 20 mg – 10’s; 30’s well tolerated but there remains the risk of
Contra-indications: Hypersensitivity to the
POM RICAM® (GoldMoore) POM TORAXIL® (Solidum) blood disorders and of hepatic and pulmonary
Capsule, Piroxicam 20 mg. drug; active peptic ulcer or inflammatory
Tablet, Tenoxicam 20 mg; e-c tab. toxicity.
Pack: 10 x 10’s; 1 x 10’s (in blister). disease of the gastrointestinal tract; acute 20 mg – 10’s; 30’s.
asthmatic attacks; history of gastric or du- Other immunosuppressant drugs, including
POM ROXIDEN® (Fil) azathioprine, are generally reserved for use
odenal ulcers, gastrointestinal hemorrhage 2.1.2 Disease-modifying
Capsule, Piroxicam 20 mg. in patients with severe disease who have
Dose: Acute musculoskeletal disorders, 40 mg daily
and chronic gastritis. Avoid use in patients antirheumatic drugs
with known aspirin and other NSAID induced failed to respond to other DMARDs, especially
for 2 days followed by 20 mg daily for 1 to (DMARDs)
asthma, rhinitis, urticaria and angioedema. in those with extra-cellular manifestations
2 weeks. Acute Gout, 40 mg daily for 5 to
Fatal anaphylactoid reactions have occurred The process of cartilage and bone destruction such as vasculitis. Immunosuppressants are
7 days. Rheumatic disorders, 20 mg daily;
maintenance 10-30 mg. in such individuals. which occurs in rheumatoid arthritis may be used in psoriatic arthritis. Adverse reactions
For Juvenile arthritis, Children >6 years Precautions: Before anesthesia or surgery, reduced by the use of a diverse group of drugs include blood disorders, alopecia, nausea and
(weight <15 kg): 5 mg daily; 16 to 25 kg: Tenoxicam should not be given to patients at known as DMARDs (disease-modifying anti- vomiting.
10 mg daily; 25-45 kg: 15 mg daily; >46 kg: risk of renal failure or to patients with increased rheumatic drugs). DMARDs include chloroquine,
The antimalarial chloroquine is less effective
20 mg daily.
risk of bleeding, because of an increased risk of penicillamine, sulfasalazine and immunosup-
than most other DMARDs, but as it is generally
POM ROXY GEL® (Bond) acute renal failure and possibility of impaired pressants (azathioprine, methotrexate).
better tolerated it may be preferred in the
Gel, Piroxicam 0.5% homeostasis. Prostaglandin inhibition may Treatment should be started early in the course treatment of mild rheumatoid arthritis. Chloro-
Pack: 20 g affect the kidneys adversely; monitor renal of the disease, before joint damage starts. Treat- quine should not be used for psoriatic arthritis.
POM SERIOXICAM® (E-Globa) function especially in elderly or patients at ment is usually initiated with a NSAID when the Because long-term therapy can result in retin-
Capsule, Piroxicam 20 mg risk of developing renal failure such as hepatic diagnosis is uncertain and the disease course opathy ophthalmological examinations should
20 mg – 100’s cirrhosis, congestive heart failure, volume de- unpredictable. However, when the diagnosis, be conducted before and during treatment.
POM UGESIC® (Adler) pletion, concomitant treatment with diuretic progression and severity of rheumatic disease
Penicillamine is not a first-line drug and its
Tablet, Piroxicam 20 mg or medicines of known nephrotoxic potential. have been confirmed, a DMARD should be
use is limited by significant adverse effects in-
20 mg – 10’s Safety of Tenoxicam administration in patients introduced.
cluding blood disorders, proteinuria, and rash.
younger than 18 years of age and in pregnant DMARDs do not produce an immediate
POM UPHAXICAM® (Goben) Corticosteroids (section 10.3) are potent
Capsules, Piroxicam USP 10 mg (peach/pink cap.); 20
or nursing women has not been established. improvement but require 4–6 months of
Interactions: Concurrent treatment with anti-inflammatory drugs but their place in the
mg (light green/orange cap.). treatment for a full response. Their long-term
salicylate or other NSAIDs should be avoided treatment of rheumatoid arthritis remains con-
10 mg – 10’s; 10 x 10’s; 500’s; 1000’s. use is limited by toxicity and loss of efficacy. If
20 mg – 10’s; 10 x 10’s; 500’s; 1000’s. because of increased risk of undesirable gas- troversial. Their usefulness is limited by adverse
one drug does not lead to objective benefit
trointestinal reactions. Avoid co-administration effects and their use should be controlled by
POM ZOXICAM® (Bakangizo) within 6 months, it should be discontinued
with potassium-sparing diuretics, lithium. specialists. Corticosteroids are usually reserved
Capsule, Piroxicam 20 mg and another DMARD substituted. Adverse
Adverse effects: GIT: Heartburn, epigastric for use in patients with severe disease which
20 mg – 10 x 10’s (in PVC blisters) reactions with DMARDs occur frequently and
has failed to respond to other antirheumatic
102 | 2.1.2 Disease-modifying antirheumatic drugs (DMARDs) 2.1.2 Disease-modifying antirheumatic drugs (DMARDs) | 103
drugs, or where there are severe extra-articular Tablet, Azathioprine 50 mg. to be taken with a meal or a glass of milk. Contra-indications: Lupus erythematosus
effects such as vasculitis. Corticosteroids are Adjust dose gradually to achieve optimum Precautions: Monitor throughout treatment
POM Azathioprine (Alpha)
also used to control disease activity during response. Maintenance: usually 200-400 mg including blood counts and urine tests; re-
Tablet, Azathioprine 5 mg.
initial therapy with DMARDs. Although corti- (equiv. 155-310 mg base) daily. nal impairment (Appendix 4); concomitant
5 mg – 56’s.
costeroids are associated with bone loss this nephrotoxic drugs (increased risk of toxicity);
METHOTREXATE
appears to be doserelated; recent studies have CHLOROQUINE pregnancy (Appendix 2); breastfeeding (ap-
suggested that a low dose of a corticosteroid Indications: Rheumatoid arthritis; malignant pendix 3); avoid concurrent gold, chloroquine
Indications: Rheumatoid arthritis (including
started during the first two years of moderate disease (section 12.1.3) or immunosuppressive treatment; avoid oral
juvenile arthritis); malaria (section 9.4.1).
to severe rheumatoid arthritis may reduce the Contra-indications: Pregnancy (Appendix 2) iron within 2 hours of a dose; patients hy-
Contra-indications: Psoriatic arthritis.
rate of joint destruction. The smallest effective and breastfeeding (Appendix 3); immunodefi- persensitive to penicillin may react rarely to
Precautions: Monitor visual acuity throughout
dose should be used, such as oral prednisolone ciency syndromes; significant pleural effusion penicillamine; interactions: Appendix 1.
treatment; warn patient to report immediately
7.5 mg daily for 2–4 years only, and at the end or ascites. BONE MARROW SUPPRESSION: Patients should
any unexplained visual disturbances; hepatic
of treatment the dose should be tapered off Precautions: Monitor throughout treatment be warned to report immediately any signs or
impairment; renal impairment (Appendix
slowly to avoid possible long-term adverse including blood counts and hepatic and symptoms of bone marrow suppression, for
4); pregnancy (Appendix 2); breastfeeding
effects. Relatively high doses of a corticoster- renal function tests; renal impairment (avoid example unexplained bruising or bleeding,
(Appendix 3); neurological disorders in-
oid, with cyclophosphamide, may be needed if moderate or severe, see also Appendix 4); purpura, infection, sore throat.
cluding epilepsy; severe GI disorders; G6PD
to control vasculitis. hepatic impairment (avoid if severe; see also Adverse effects: Initially nausea (reduced if
deficiency; elderly; may exacerbate psoriasis
Appendix 5); reduce dose or withdraw if acute taken before food or on retiring, and if initial
and aggravate myasthenia gravis; porphyria;
AZATHIOPRINE infection develops; for woman or man, contra- dose is increased gradually), anorexia, fever and
interactions: Appendix 1.
Indications: Rheumatoid arthritis in cases ception during and for at least 6 months after skin reactions; taste loss (mineral supplements
Adverse effects: GI disturbances, headache,
that have failed to respond to chloroquine or treatment; peptic ulceration, ulcerative colitis, not recommended); blood disorders including
skin reactions (rash, pruritus); less frequently
EMDEX
penicillamine; psoriatic arthritis; transplant diarrhoea, ulcerative stomatitis; advise patient thrombocytopenia, leukopenia, agranulocy-
ECG changes, convulsions, visual changes,
rejection (section 12.2); inflammatory bowel to avoid self-medication with salicylates or tosis and aplastic anaemia; proteinuria, rarely
retinal damage, keratopathy, ototoxicity, hair
disease (section 4.7). other NSAIDs; warn patient with rheumatoid haematuria (withdraw immediately); haemo-
depigmentation, alopecia, discoloration of
Contra-indications: Hypersensitivity to azathio- arthritis to report cough or dyspnoea; inter- lytic anaemia, nephrotic syndrome, lupus
skin, nails and mucous membranes; rarely
prine or mercaptopurine. actions: Appendix 1. erythematosus-like syndrome, myasthenia-like
blood disorders (including thrombocytopenia,
Precautions: Monitor for toxicity throughout agranulocytosis, aplastic anaemia); mental BONE MARROW SUPPRESSION: Patients should syndrome, polymyositis (rarely with cardiac
treatment; monitor full blood counts frequently; changes (including emotional disturbances, be warned to report immediately any signs or involvement), dermatomyositis, mouth ulcers,
hepatic impairment (Appendix 5); renal impair- psychosis), myopathy (including cardio-myo- symptoms of bone marrow suppression, for stomatitis, alopecia, bronchiolitis and pneumo-
ment (Appendix 4); elderly (reduce dose); preg- pathy and neuromyopathy), acute generalized example unexplained bruising or bleeding, nitis, pemphigus, glomerulonephritis (Good-
nancy (Appendix 2); breastfeeding (Appendix 3); exanthematous pustulosis, exfoliative derma- purpura, infection, sore throat. pasture syndrome) and erythema multiforme
interactions: Appendix 1. titis, erythema multiforme (Stevens-Johnson Adverse effects: Blood disorders (bone mar- (Stevens-Johnson syndrome) also reported;
BONE MARROW SUPPRESSION: Patients syndrome), photosensitivity, and hepatic dam- row suppression), liver damage, pulmonary male and female breast enlargement reported;
should be warned to report immediately any age; important: arrhythmias and convulsions toxicity; GI disturbances—if stomatitis and rash (early rash disappears on withdrawing
signs or symptoms of bone marrow suppres- in overdosage. diarrhoea occur, stop treatment; renal failure, treatment—reintroduce at lower dose and
sion, for example unexplained bruising or Dose: Administered on expert advice. skin reactions, alopecia, osteoporosis, arthral- increase gradually; late rash is more resistant—
bleeding, purpura, infection, sore throat. Note: All doses in terms of chloroquine base.Rheu- gia, myalgia, ocular irritation, precipitation of either reduce dose or withdraw treatment).
Adverse effects: Hypersensitivity reactions matoid arthritis, by mouth, ADULT 150 mg daily; diabetes. Dose: Administered on expert advice
requiring immediate and permanent with- maximum 2.5 mg/kg daily; CHILD up to 3 mg/kg Dose: Administered on expert advice Rheumatoid arthritis, by mouth,
drawal include malaise, dizziness, vomiting, daily. o avoid excessive dosage in obese patients Rheumatoid arthritis, by mouth, ADULT initially 125–250 mg daily
the dose of chloroquine should be calculated on ADULT 7.5 mg once weekly (as a before food for 1 month, increased
diarrhoea, fever, rigors, myalgia, arthralgia,
the basis of lean body weight
rash, hypotension and interstitial nephritis; single dose or divided into 3 doses of by similar amounts at intervals of not
dose-related bone marrow suppression; liver POM Chloroquine (WMF 2.4) 2.5 mg given at intervals of 12 hours), less than 4 weeks to usual mainte-
impairment, cholestatic jaundice; hair loss Tablets, Chloroquine (as sulfate or phosphate) 100 adjusted according to response; max. nance of 500–750 mg daily in divided
and increased suceptibility to infections and mg, 150 mg. total dose of 20 mg once weekly. doses; maximum 1.5 g daily; ELDERLY
Note: Chloroquine base 150 mg is approximately Note: The doses are weekly doses and care is re- initially up to 125 mg daily before
colitis in patients also receiving corticosteroids;
equivalent to chloroquine sulfate 200 mg or chlo- quired to ensure that the correct dose is prescribed
nausea; rarely pancreatitis and pneumonitis. food for 1 month increased at inter-
roquine phosphate 250 mg. and dispensed.
hepatic venoocclusive disease; also herpes vals of not less than 4 weeks; max. 1 g
zoster infection. See Section 9.4.1 for the proprietary preparations of POM Methotrexate (WMF 2.4) daily; CHILD 8–12 years initially 2.5–5
Chloroquine. mg/kg daily, gradually increased to
Dose: Administered on expert advice Rheu- Tablet, Methotrexate (as sodium salt) 2.5 mg.
matoid arthritis, by mouth, initially, POM Methotrexate (Alpha)
usual maintenance of 1 5–20 mg/kg
Hydroxychloroquine
1.5–2.5 mg/kg daily in divided doses, Tablet, Methotrexate 2.5 mg. daily at intervals of 4 weeks over a
adjusted according to response; POM HCQS® (Hochiez) period of 3–6 months.
2.5 mg – 10’s.
Tablet, Hydroxychloroquine (as sulfate) 200 mg;
maintenance 1–3 mg/kg daily; con- POM Penicillamine (WMF 2.4)
f-c tab.
sider withdrawal if no improvement 200 mg – 10’s.
PENICILLAMINE Capsule or tablet, Penicillamine 250 mg.
within 3 months. Dose: By mouth, Adult, 400-600 mg (equiv. to Indications: Severe rheumatoid arthritis;
POM Azathioprine (WMF 2.4) 310-465 mg base) daily in divided doses; copper and lead poisoning (section 19.2.3).
104 | 2.1.3 Other antirheumatic drugs 2.1.3 Other antirheumatic drugs | 105
SULFASALAZINE lactation. Capsule, Glucosamine sulphate 250 mg, 500 mg treatment for 4 weeks even if pain subsides.
Indications: Severe rheumatoid arthritis; ul- Dose: By mouth, Adult, 2 capsules twice 250 mg: 100’s; 500’s (in bottle)
daily. To be taken with food. 500 mg – 60’s (in bottle) SODIUM HYALURONATE
cerative colitis and Crohn disease (section 4.7).
Contra-indications: Hypersensitivity to salic- OTC ZINAXIN® (Swipha) OTC GEVOLOX® Plus (CG Biostadt) Synonym: Hyaluronic acid
ylates and sulfonamides; severe renal impair- Capsule, HMP-33 Ginger extract 255 mg Tablet, Glucosamine sulphate 500 mg, chondroitin Pharmacology: Synovial fluid, which is vis-
ment; child under 2 years; porphyria. Pack: 30. sulphate 400 mg. co-elastic owing to its contents of hyaluronic
Pack: 2 x 10’s. acid, is present in all synovial joints, especially
Precautions: Monitor blood counts and liver
function during first 3 months of treatment; CHONDROITIN plus GLUCOSAMINE OTC GLUCOTIN-DS® (SKP) in the large weight joints, where it provides
monitor renal function regularly; renal impair- Indications: General – Anti-arthritic. Joint – Capsule, Glucosamine (as sulfate) 375 mg, chon- a normal, painless movement owing to its
ment (Appendix 4); pregnancy (Appendix 2); Osteoarthritis; Rheumatoid arthritis, Fractures, droitin (as sulfate) 100 mg, vitamin D3 40 IU, calcium synovial and shock-absorbing properties. It is
breastfeeding (Appendix 3); history of allergy; amino acid chelate 300 mg (eq. 60 mg elemental responsible for supplying nourishment to the
Otosclerosis, Low backache, Ankylosing
calcium); white cap. joint cartilage. In degenerative joint diseases
G6PD deficiency; slow acetylator status; inter- spondylitis, Arthritis due to sport injury/active Pack: 30’s
actions: Appendix 1. lifestyle. Eyes – For Uveitis, that is an inflamma- like osteoarthritis, the visco-elasticity of the
Dose: 1-2 capsules daily after meal
tory disease of the iris and focusing muscle. joint synovium is considerably impaired, which
BONE MARROW SUPPRESSION: Patients should
It is useful also in preventing changes in the OTC JOINTACE® (Adler) reduces its shock-absorbing effect. The me-
be warned to report immediately any signs or Tablet, Glucosamine sulfate potassium 750 mg,
vitreous humour (substance within the eye) chanical load of joint and disintegration of joint
symptoms of bone marrow suppression, for Methyl sulfonylmethane (msm) 200 mg, vitamin
and thus protecting the retina from release. cartilage is so increased that it leads to pain
example unexplained bruising or bleeding, C 50 mg, vitamin D3 200 IU, manganese sulfate 9.3
Contra-indications: Hypersensitivity to Glu- and restricted movement at the affected joint.
purpura, infection, sore throat. mg (equiv. to elemental Mn 3 mg), sodium borate
cosamine and Chondroitin sulphate. Sodium hyaluronate is injected intra-articularly
Adverse effects: Nausea, diarrhoea, head- 4.4 mg (equiv. to elemental Boron 0.5 mg), copper
Precautions: Allergy to shellfish; Pregnancy/ sulfate 2 mg (equiv. to elemental Cu 0.5 mg), zinc to supplement natural hyaluronic acid in the
ache, loss of appetite; fever; blood disorders
Lactation; Impaired renal and hepatic function. sulfate monohydrate 8.24 mg (equiv. to elemental synovial fluid. These injections may reduce
(including Heinz body anaemia, megaloblastic
EMDEX
Adverse effects: GI disturbances, diarrhea, Zn 3 mg; f-c tab. pain over 1–6 months but they are associated
anaemia, leukopenia, neutropenia, thrombocy-
nausea and heartburn. Pack: 30’s. with short-term increase in knee inflammation.
topenia); hyper-sensitivity reactions (including Dose: One tablet twice a day.
Dose: See under preparations below. Indications: Pain and restricted movement in
rash, urticaria, erythema multiforme (Ste- Gel, Chingati satva 5% (Glucosamine sulfate so- degenerative and traumatic changes of knee
vens-Johnson syndrome), exfoliative dermatitis, OTC ARTHOCARE® (Fidson) dium), Nilgiri taila 1%, Lemon grass oil 2%, Ginger joints and other synovial joints.
epidermal necrolysis, pruritus, photo-sensiti- Capsule, Chondroitin sulphate 200 mg, Glucosamine oil 0.5%, Clove oil 0.5%, Camphor 3%, Pudina taila
Contra-indications: Hypersensitivity to the
zation, anaphylaxis, serum sickness, interstitial HCl 250 mg. 5%, Capsicum 0.03.
Dose: Dosage requirement are usually based Pack: 30 g. drug.
nephritis, lupus erythematosus-like syndrome);
on b. wt: Up to 60 kg – 2 caps twice Administration: Apply sufficient quantity on the af- Precautions: Avoid injection into blood vessels
lung complications (including eosinophilia,
a day; >60 kg – 3 caps twice a day. To fected area with gentle massage for a few minutes till and surrounding tissue. Not recommended for
fibrosing alveolitis); ocular complications
be taken after food. the gel gets absorbed; may be repeated as needed. use in children, pregnancy and breastfeeding
(including periorbital oedema); stomatitis,
Prophylactic use: 2 capsules 1-2 times or in patients with inflammatory joint diseases
parotitis; ataxia, aseptic meningitis, vertigo, OTC JOINT RENEW® (Sylken)
daily after food. Capsule, Glucosamine 1500 mg, Chondroitin 1200 like rheumatoid arthritis.
tinnitus, alopecia, peripheral neuropathy, in-
Note: It requires 1-2 weeks for the effects of Artho- mg, Methylsuphonyl methane (MSM) 300 mg Adverse effects: Local side effects like pain,
somnia, depression, hallucinations; renal effects
care to appear. Once the desired effects have been Pack: 30’s; 90’s (in bottle) heat sensation, reddening and swelling can
(including proteinuria, crystalluria, haematuria);
achieved, the dosage can be reduced. Arthocare Dose: 3 caps daily occur at the treated joint. Placing an ice pack
oligospermia; rarely acute pancreatitis, hepa-
should be used for a mininium of 2-4 weeks to
OTC MAXIFLEX® (Alpha)
on the treated joint for 5 to 10 minutes would
titis; urine may be coloured orange; some soft
experience optimal results. It takes around 8 weeks reduce the occurrence of such side effects
contact lenses may be stained. Tablet, Chondroitin, glucosamine, antioxidants.
to 6 months to repair damaged cartilage. Dose: By intra-articular injection, 20 mg once
Dose: Administered on expert advice OTC MOBICAR® (Canopus)
OTC ARTHRITISCARE® (Al-Tinez) a week; up to 3 to 5 injections into
Rheumatoid arthritis, by mouth as Capsule, Glucosamine sulfate 500 mg, chondroitin
Capsule, Glucosamine sulfate 250 mg the affected joint.
gastro-resistant tablets, ADULT ini- sulfate 400 mg; black oblong cap containing white
250 mg – 10 x 10’s (in blisters) Note: In case of joint effusion, an aspiration of effu-
tially 500 mg daily, increased by 500 oily viscous mass.
sion, resting of the joint as well as placing an ice pack
mg at intervals of 1 week to a max. of OTC BONECARE® (JB Pharma) Pack: 3 x 10’s (in blisters)
and/or the intra-articular administration of corticos-
2–3 g daily in divided doses. Capsule, Glucosamine sulphate 250 mg, chondroitin teroids is advised. 2-3 days thereafter, the treatment
OTC Nature’s Field Joint Renew (Sylken)
sulphate 200 mg, fish oil 250 mg (providing omega with Sodium hyaluronate 20 mg is started As long
POM Sulfasalazine (WMF 2.4) Capsule, Glucosamine 1100 mg, Chondroitin 1200
3 nutrients – 150 mg of EPA and 130 mg of DHA). as the sterile pack is not opened, the contents and
Tablet, Sulfasalazine 500 mg. mg, Methylsulphonylmethane (MSM) 300 mg.
Pack: 3 x 10’s (in blister). the surface of the prefilled syringe are sterile. The
Pack: 30’s; 90’s
Dose: 2 capsules daily prior to meal. prefilled syringe is taken out from the sterile pack,
Dose: 3 capsules daily
2.1.3 Other antirheumatic drugs OTC BONEFLEX® (Geneith) the cap is removed from Leurlock connection, a
OTC URAH® (Neimeth) suitable canula (e.g. 19 or 21 G) is fixed and this is
Capsule, Glucosamine sulphate 250 mg, chondroitin
HYDROXYMETHOXYPHENYL COMPOUND Cream, Glucosaemine (as sulfate) 8%, menthol, locked by a slight rotation. Before injection, the air
sulphate 200 mg, omega-3 fish oil 300 mg.
curcuma longa (tumeric) extract. bubble is removed from the injection.
(Standardised Ginger Extract) Pack: 3 x 10’s (in blisters)
Pack: 50 g.
Indications: Treatment of rheumatic and OTC COSAMID® Plus (Hovid) Indications: For the treatment of osteoarthritis, POM SYNJECT® (Fidson)
arthritic pain; may be used as an alternative Capsule, Glucosamine sulphate 250 mg, chondroitin joint and muscle pains, and for the rehabilitation Injection, Sodium hyaluronate 20 mg per 2 mL; a
or supplement to the NSAIDs. sulphate 200 mg of cartilage; also useful for osteoporosis in post visco-elastic solution for injection into the knee joint
Contra-indications: Hypersensitivity to ginger Pack:10 x 10’s (in blisters menopausal women. gap sterilized by autoclaving.
or other component of the drug; GI bleeding. Administration: Apply 1-3 times daily to affected Pack: 1 prefilled syringe in sterile pack.
OTC COSAMINE® (Hovid) joints. Rub sufficiently to cover joint area. Continue
Precautions: Children <12 years; pregnancy,
106 | 2.2 Drugs used in gout 2.3 Skeletal muscle relaxants (antispasmodics) | 107
2.2 Drugs used in gout • Discontinue if nausea or vomiting occurs; if used for son syndrome) or toxic epidermal necrolysis, PROBENECID
acute attack, discontinue as soon as pain resolves vasculitis, hepatitis, renal impairment and, very Therapeutic category: Uricosuric agent.
2.2.1 Acute gout or if nausea, vomiting or diarrhoea occurs.
2.2.2 Chronic gout rarely, seizures; GI disorders; rarely malaise, Indications:Gout prophylaxis, hyper-uricae-
Dose: Acute gout, by mouth, adult 0.5–1 mg headache, vertigo, drowsiness, visual and taste mia; prolongation of beta-lactam effect (i.e.,
Gout is a familial metabolic disease character- initially, followed by 500 µg every 2–3 disturbance, hypertension, alopecia, hepatotox- serum levels)
ized by recurrent episodes of acute arthritis hours until relief of pain is obtained, icity, paraesthesia, neuropathy, gynaecomastia, Contra-indications: Renal uric acid calculi,
due to deposits of monosodium urate in joint or vomiting or diarrhoea occurs; blood disorders (including leukopenia, throm- blood dyscrasia; initiation of therapy during
and cartilage. Formation of uric acid calculi in maximum total dose 6 mg; the course bocytopenia, haemolytic anaemia and aplastic acute attack; children under 2 years.
the kidneys may also occur. Gout is associated should not be repeated within 3 days anaemia). Precautions: History of peptic ulceration, re-
with high serum levels of uric acid, a poor sol- Prevention of gout attacks during initial Nursing action: nal impairment, pregnancy; ensure adequate
uble substance that is the major end product treatment with allopurinol, adult 500 • Administer after meals with plenty of water. Patient fluid intake.
of purine metabolism. µg 2–3 times daily continuing for at should increase fluid intake to about 3-4 litres daily.
Adverse effects: GI upset, sore gums, dizziness,
Treatment of gout and hyperuricemia consists least 1 month after hyperuricaemia • Discontinue the drug and contact physician at first
sign of rash, painful urination, blood in urine, irri-
headache, skin rashes, urinary frequency.
of a two–step approach. The first step is to has been corrected.
tation of the eyes, or swelling of the lips or mouth. Nursing action:
terminate the acute attack and resolve the POM Colchicine (EDL 2.4) • Teach patient to avoid hazardous activities, if • Administer with food, milk or antacid to minimize
pain. Once the acute attack is resolved, the Tablet, Colchicine 0.5 mg. drowsiness occurs; alcohol decreases effectiveness GI distress.
goal is to gradually reduce the serum uric acid of the drug. • Encourage patient to drink plenty of fluids to
concentration. 2.2.2 Chronic gout • Colchicine or NSAID ( not aspirin or salicylates) may reduce the risk of uric acid stones.
be prescribed to prevent acute gouty attacks which • Do not initiate therapy until acute attack subsides;
For long-term control of gout in patients who it has no analgesic or anti-inflammatory action and
2.2.1 Acute gout have frequent acute attacks, the presence of
may occur in first 6 weeks of therapy.
therefore of no value in acute attack.
Dose: Prophylaxis of gout, by mouth, ADULT
Acute attacks of gout are usually treated with tophi, or chronic gouty arthritis, the xanthine • Tell patient with gout to avoid alcohol and aspirin
EMDEX
initially 100 mg daily as a single
high doses of a NSAID such as indometacin oxidase inhibitor allopurinol may be used or other salicylates because they increase urate
dose, preferably after food, then level and may precipitate gout respectively. Par-
(150–200 mg daily in divided doses); ibuprofen to reduce production of uric acid. Treatment
adjusted according to plasma or acetamol may be used for pain.
has weaker anti-inflammatory properties than for chronic gout should not be started until
urinary uric acid concentration; usual • The frequency and severity of acute attacks may
other NSAIDs and is therefore less suitable for after an acute attack has completely subsided,
maintenance dose in mild conditions increase during the first 6-12 months of therapy;
treatment of gout. Salicylates, including acetyl- usually 2–3 weeks. The initiation of allopurinol Colchicine or another anti-inflammatory agent may
100–200 mg daily, in moderately
salicylic acid are also not suitable because they treatment may precipitate an acute attack be prescribed during first 3-6 months of therapy to
severe conditions 300–600 mg
may increase plasma-urate concentrations. and therefore a suitable NSAID or colchicine prevent such attacks.
daily, in severe conditions 700–900
Colchicine [not included on WHO Model List] [not included on WHO Model List] should be • Provide low purine diet, restricting liver, kidneys,
mg daily; doses over 300 mg daily
is an alternative for those patients in whom used as a prophylactic and continued for at sardines, peas.
given in divided doses.Prophylaxis of • Probenecid is preferred to Sulphinpyrazone
NSAIDs are contraindicated. Its use is limited least one month after the hyperuricaemia has
hyperuricaemia, by mouth, ADULT becuase it has lower incidence of GI and haema-
by toxicity with high doses. It does not induce been corrected. If an acute attack develops
maintenance doses as for acute gout, tological adverse reactions.
fluid retention and can therefore be given to during treatment for chronic gout, then al-
adjusted according to response, started Dose: By mouth, Adult, Hyperuricaemia with
patients with heart failure; it can also be given lopurinol should continue at the same dosage
24 hours before cancer treatment and gout, initially 250 mg twice daily; in-
to patients receiving anticoagulants. and the acute attack should be treated in its
continued for 7–10 days afterwards; creased after a week to 500 mg twice
own right. Treatment for chronic gout should
COLCHICINE CHILD under 15 years 10–20 mg/kg daily; then, up to a max. 2-3 g daily in
be continued indefinitely to prevent further
daily (max. 400 mg daily). 2-4 divided doses.
Indications: Acute gout; short-term proph- attacks of gout. Note: Initiate 2–3 weeks after acute attack has Prolong penicillin serum levels, 500 mg
ylaxis during initial therapy with allopurinol. subsided and administer a suitable NSAID (not
ALLOPURINOL 4 times daily.
Contra-indications: Pregnancy (Appendix 2). ibuprofen or a salicylate) or colchicine from the start
Gonorrhoea, 1 g 30 minutes before
Precautions: Elderly; gastrointestinal disease; Indications: Prophylaxis of gout; prophylaxis of allopurinol treatment and continue for at least 1
month after hyperuricaemia corrected. Penicillin, Ampicillin or Amoxicillin.
cardiac impairment; hepatic impairment; renal of hyperuricaemia associated with cancer
impairment (Appendix 4); breastfeeding (Ap- chemotherapy. POM Allopurinol (WMF 2.3) POM Probenecid (EDL 2.4)
pendix 3); interactions: Appendix 1. Contra-indications: Acute gout; if an acute Tablet, Allopurinol 100 mg. Tablet, Probenecid 500 mg.
Adverse effects: N & V, abdominal pain; ex- attack occurs while receiving allopurinol, con- Injection, Probenecid 100 mg per mL.
POM Allopurinol (EDL 2.4)
cessive doses may cause severe diarrhoea, GI tinue prophylaxis and treat attack separately.
Tablet, Allopurinol 100 mg. 2.3 Skeletal muscle relaxants
haemorrhage, rash, renal and hepatic damage; Precautions: Ensure adequate fluid intake of
rarely peripheral neuritis, myopathy, alopecia, 2–3 litres daily; pregnancy (Appendix 2); breast- POM Allopurinol (Alpha) (antispasmodics)
inhibition of spermatogenesis; with prolonged feeding (Appendix 3); renal impairment (Ap- Tablets, Allopurinol 100 mg, 200 mg. Drugs that affect skeletal muscle function fall
treatment, blood disorders. pendix 4); hepatic impairment (Appendix 5); POM Allopurinol (Dizpharm) into 2 major therapeutic groups:
Nursing action: withdraw treatment if rash occurs, reintroduce Tablet,, Allopurinol 100 mg. • Neuromuscular blockers which are used during
• Administer on empty stomach to enhance absorp- if rash is mild but discontinue immediately if it 100 mg – 100. surgical procedures and in intensive care units to
tion; but for maintenance therapy, give with meals recurs; interactions: Appendix 1. cause paralysis (see section 3.3).
POM ZYLORIC® (GSK)
to reduce GI effects. Adverse effects: Rash (see Precautions above), • Spasmolytics which are used to reduce spasticity
Tablet, Allopurinol 100 mg; white tab. marked ‘ZY-
• Monitor fluid I&O; teach patient to increase fluid in a variety of neurological conditions.
hypersensitivity reactions occur rarely and LORIC 100’ and ‘Coded U4A’.
intake to about 3-4 litres daily. Members of the first group, as their name
• Tell patient to avoid alcohol and OTC preparations
include fever, lymphadenopathy, arthralgia, eo- 100 mg – 50.
sinophilia, erythema multiforme (Stevens-John- implies, interfere with transmission at the
containing alcohol.
108 | 2.3 Skeletal muscle relaxants (antispasmodics) 2.4 Muscle relaxants (peripherally acting) and cholinesterase inhibitors | 109
neuromuscular end plate and are not CNS– 25% in ambulatory patients. Requires close per day Precautions: Impaired kidney or liver function;
active drugs. Because they are used primarily patient monitoring during the early stages for Children: 1 tablet per day; maximum 2 road users and operators of machineries; preg-
as an adjunct to general anaesthesia, they are adverse effects as well as for benefit. Quinine tablets per day. nancy, breast-feeding, children.
discussed under anaesthetic drugs in chapter is very toxic in overdosage and accidental Adverse effects: Drowsiness, fatigue, dizziness,
3, section 3.3. fatalities have occurred in children. ORPHENADRINE dry mouth, nausea, slight reduction in blood
Therapeutic category: Skeletal Muscle Relax- pressure; in high doses, muscle weakness,
Drugs in the second group have traditionally
METHOCARBAMOL ant; Anticholinergic Agent. insomnia, hypotension, bradycardia.
been called “centrally acting muscle relaxants
Therapeutic category: Skeletal muscle Indications: Pain due to spasm of voluntary Dose: Painful muscle spasms, by mouth, 2-4
but dantrolene, a member of the group, has
relaxant. muscle in injury, strains, sprains. mg 3 times daily; increased to 2-4 mg
no central effects.
Indications: Symptomatic relief of muscular Contra-indications: Glaucoma, urinary reten- 4 times daily in severe cases.
Antispasmodic drugs tion, myasthenia gravis, breast-feeding. Spasticity due to neurological disorders,
spasm.
Spasticity is characterized by an increase Contra-indications: Coma or pre-coma, brain Precautions: Tachycardia, pregnancy, elderly. by mouth, initially 6 mg in 3 divided
in tonic stretch reflexes and flexor muscle damage, epilepsy, myasthenia gravis, glau- Adverse effects: Dry mouth, nausea, blurred doses; increased stepwise at half-
spasms together with muscle weakness. It is coma, tachycardia. vision, dizziness, confusion, tremor. weekly or weekly intervals by 2-4 mg
often associated with cerebral palsy, multiple Precautions: May cause drowsiness, avoid Nursing action: up to an optimal daily dose of 12-24
sclerosis, and stroke. extravasation, history of seizures. • Administer whole, do not crush sustained release mg in 3–4 doses; max. 36 mg daily.
product. Administration: Tablets can be taken with or with-
These conditions often involve abnormal Adverse effects: Drowsiness, skin rash, urti-
• May cause drowsiness, impair judgement or out meals and the course should not be altered so as
function of the bowel and bladder, as well as caria, angioneurotic oedema, lightheadness, co-ordination. Advise patient to avoid alcohol and to prevent delayed onset of action or adverse effects
skeletal muscle. This section deals with skeletal allergic reactions. hazardous activities.
muscle spasticity only while chapter 4, section Advice to patients: : May cause drowsiness. • Raise bed rails, institute safety measures, assist POM SIRDALUD® (Novartis)
4.2, deals with bowel spasms. Ability to operate machinery or drive may be with ambulation. Tablets, Tizanidine HCl 2 mg, 6 mg (all scored tabs);
EMDEX
impaired. Avoid alcoholic bever-ages. • Instruct patient to notify physician if urinary 4 mg (cross-scored tab.).
Drug therapy may ameliorate some of the hesitancy or retention occurs. Patient should void
Nursing action:
symptoms of spasticity by modifying the • Give with food or milk to minimize GI distress. before taking the drug. 2.4 Muscle relaxants (peripherally
stretch reflex arc or by interfering directly • May cause drowsiness, impair judgement or • Give patient cool drinks or chewng gum to relieve acting) and cholinesterase
with skeletal muscle excitation – contraction co-ordination. Advise patient to avoid alcohol and dry mouth. inhibitors
coupling. The major disadvantage of treatment hazardous activities. Dose: By mouth, 150-300 mg daily in divided
2.4.1 Muscle relaxants
with these drug is that reduction in muscle • Inform patient that drug may turn urine brown, doses; up to 400 mg daily if neces-
2.4.2 Cholinesterase inhibitors
tone can cause a loss of splinting action of the black or green. sary. Not recommended for children.
spastic leg and truck muscles and sometimes • Tell patient to notify physician of rash, itching, or Administration: May administer with or without
nasal congestion. meals 2.4.1 Muscle relaxants
lead to an increase in disability.
Dose: See lit. Muscle relaxants used in surgery include sux-
Diazepam can be used in patients with muscle OTC Orphenadrine (EDL 2.4)
OTC Methocarbamol (EDL 2.5) Tablet, Orphenadrine citrate 100 mg. amethonium, alcuronium, and vecuronium; for
spasm of almost any origin, including local
Tablet, Methocarbamol 750 mg. Injection, Orphenadrine Citrate 30 mg per mL; in further details see section 3.3.1.
muscle trauma. However, it produces sedation
1 mL amp.
in most patients at the doses required to signif- OTC DORBAXIN® (Xcel)
icantly reduce muscle tone. Other benzodiaz- Tablet, Methocarbamol 500 mg; f-c tab. OTC CRISTAGELSIC® (Crystal)
2.4.2 Cholinesterase inhibitors
epines can be used. Muscle-relaxant doses of 500 mg – 10 x 1 x 10’s (in blisters) Tablet, Orphenadrine citrate 100 mg MYASTHENIA GRAVIS
benzodiazepines are similar to anxiolytic doses Indications: As an adjunct to rest, physical therapy 100 mg – 20’s
Cholinesterase inhibitors, such as neostigmine
and other measures for the relief of discomfort
(see section 1.1). OTC LUSECOR® (Coriander) and pyridostigmine, are used in the symp-
associated with acute, painful, musculoskeletal
Orphenadrine, a congener of diphenhy- Tablet, Orphenadrine (as citrate) 100 mg; extend- tomatic treatment of myasthenia gravis. They
conditions.
ed-release tab. act by inhibiting acetylcholinesterase, thereby
dra – mine, is an anticholinergic agent with Dose: By mouth, Adult, Initially 3 tablets 4 times
100 mg – 20’s.
weak antihistaminic, anaesthetic, and skeletal daily; Maintenance dosage: 2 tablets 4 prolonging the action of acetylcholine, and thus
muscle-relaxant properties. Tizanidine is a times daily. OTC ORPHETAB® (Laider) enhancing neuromuscular transmission; this
centrally acting skeletal muscle relaxant; its Note: 6 g a day are recommended for the first 48 to Tablet, Orphenadrine citrate 100 mg. produces at least a partial improvement in most
72 hours of treatment; may increase to 8 g per day in 100 mg – 20’s (in blisters). myasthenic patients but complete restoration of
major site of action is in the spinal cord. It pref-
severe conditions. Thereafter, the dosage can usually
erentially inhibits polysynaptic mechanisms With Paracetamol muscle strength is rare. Unless the patient has
be reduced to approx. 4 g per day.
responsible for excessive muscle tones, mainly difficulty in swallowing, cholinesterase inhibi-
OTC HORGESIC® (Hovid)
by reducing the release of excitatory amino OTC Methocarbamol (Visko) tors are given by mouth. Pyridostigmine has a
Tablet, Orphenadrine citrate 35 mg, paracetamol
acids from interneurones. The drug does not Tablet, Methocarbamol 500 mg slower onset (usually within 30–60 minutes), but
450 mg
Pack: 1 x 10’s. a longer duration of effect than neostigmine;
affect neuromuscular transmission. Pack: 1000’s.
With Paracetamol it also tends to cause fewer muscarinic effects
Other skeletal antispasticity drugs include
TIZANIDINE such as diarrhoea, abdominal cramps, and
Dantrolene (which acts directly on skeletal OTC DORBAXIN® Forte (Xcel)
Tablet, Methocarbamol 400 mg, paracetamol 500 Indications: Painful muscle spasms associated excess salivation, so is usually preferred. Doses
muscle and produces fewer central adverse
mg; uncoated tab. with static and functional disorders of the spine should be carefully adjusted to avoid precipitat-
effects) and Baclofen (which inhibits transmis-
Pack: 10 x 1 x 10’s (in blisters) and following surgery; spasticity due to neuro- ing a cholinergic crisis due to overdosage; this
sion at spinal level and also depresses the CNS).
Indications: Relief of discomfort associated with logical disorders such as chronic myelopathy, must be differentiated from a myasthenic crisis
Quinine salts are also effective in reducing the acute, painful musculoskeletal conditions, and fever. due to disease progression, and consequent
cerebro-vascular accidents.
frequency of nocturnal leg cramps by about Dose: Adult, 2 tablets per day; maximum 3 tablets
110 | 2.4.2 Cholinesterase inhibitors 2.5 Drugs affecting bone structure and mineralization | 111
underdosage; the principal effect in both cases for hypersensitivity reactions. arrhythmias, hypotension, agitation, excessive PAMIDRONATE
is increased muscle weakness. Dose: Myasthenia gravis, by mouth as dreaming, weakness eventually leading to
neostigmine bromide, ADULT initially POM PAMIRED® (Phillips/Dr. Reddy’s)
In myasthenic crisis, if the patient has difficulty fasciculation and paralysis; thrombophlebitis;
Infusion, Disodium pamidronate equiv. to anhydrous
in breathing and in swallowing, the cholinest- 15–30 mg at suitable intervals rash associated with bromide salt. disodium pamidronate 30 mg; powder for reconsti-
erase inhibitor must be given by intramuscular throughout the day (usual duration of Nursing action: tution in single-dose vial.
or subcutaneous injection; neostigmine is action 2–4 hours), gradually increased • Give on an empty stomach for better absorption. Pack: 1’s (in a sterile single-dose vial).
until desired response obtained, total • Observe patient for bronchospasm, hypotension, Indications: Moderate or severe hypercalcemia
usually preferred. To reduce muscarinic effects, respiratory depression, headache, dizziness and
atropine (section 3.2) should also be given. daily dose within range 75–300 mg, associated with malignancy, with or without bone
taken at appropriate intervals when convulsions (discontinue therapy and inform the metastases. Patient should be adequately hydrated
For the use of neostigmine in surgery, see doctor if these occur). throughout the treatment. Safety and efficacy of
max. strength required, but doses
section 3.3. • Monitor patient’s VS, respiration. Pamidronate in the treatment of hypercalcemia
above 180 mg daily not usually toler- • Evaluate patient’s therapeutic response namely associated with hyperparathyroidism or with
A corticosteroid such as prednisolone (section ated; NEONATE, initially 1–2 mg every increased muscle strength, hand grasp, improved other non-tumor related conditions has not been
10.3), is used for the treatment of myasthenia 4 hours, 30 minutes before feeds; gait. established. Treatment of patients with moderate to
gravis; addition of azathioprine (section 12.2) CHILD up to 6 years, initially 7.5 mg, Dose: Myasthenia gravis, by mouth, ADULT severe Paget’s disease of bone. Treatment of osteo-
may allow a dose reduction of both the corti- 6–12 years, initially 15 mg, total daily initially 30–120 mg at suitable inter- lytic bone metastases of breast cancer and osteolytic
costeroid and of the anticholinesterase. dose usually 15–90 mg in divided vals throughout the day, gradually lesions of multiple myeloma, in conjunction with
doses at appropriate intervals. increased until desired response ob- standard antineoplastic therapy.
NEOSTIGMINE Myasthenia gravis, by SC or IM tained; total daily dose within range Contra-indications: Hypersensitivity to bisphos-
Indications: Myasthenia gravis; reversal of injection as neostigmine metilsulfate, 0.3–1.2 g, taken at appropriate inter- phonates.
ADULT 1–2.5 mg as required, total Precautions: Avoid rapid rates of infusion and bolus
non-depolarizing block, postoperative urinary vals when max. strength required, but
injections (may cause nephrotoxicity as a result of
retention (section 3.3) daily dose 5–20 mg; NEONATE 50–250 doses above 450 mg daily not usually deposition of calcium-bisphosphonate complexes
EMDEX
Contra-indications: Recent intestinal or µg every 4 hours, 30 minutes before advisable in order to avoid acetylcho- in the kidney). Cardiac disease (potential for fluid
bladder surgery; mechanical intestinal or uri- feeds (not usually required beyond 8 line receptor down-regulation; CHILD overload). Monitor serum calcium, electrolytes,
nary tract obstruction; after suxamethonium; weeks of age); CHILD 200–500 µg as up to 6 years initially 30 mg, 6–12 phosphate, magnesium and creatinine and CBC,
pneumonia; peritonitis. required. years initially 60 mg; total daily dose differential and hematocrit/hemoglobin. Anemia,
Precautions: Asthma; urinary tract infections; usually 30–360 mg in divided doses leukopenia or thrombocytopenia (monitor carefully
POM Neostigmine (WMF 20.2)
cardiovascular disease including arrhythmias at appropriate intervals. in the first 2 weeks following treatment). Not recom-
Tablet, Neostigmine bromide 15 mg.
mended for use in children.
(especially bradycardia, vagotonia, recent MI Injection, Neostigmine metilsulfate 500 µg/mL, in Myasthenia gravis, by IM injection,
Interactions: Avoid mixing with calcium containing
or AV block); hyperthyroidism; hypotension; 1-mL amp; 2.5 mg/mL, in 1-mL amp. ADULT 2 mg every 2–3 hours;
infusion solutions, such as Ringer’s solution; give
peptic ulcer; epilepsy; parkinsonism; renal im- POM Neostigmine (EDL 17.2) NEONATE 50–150 µg before feeds as a single IV solution using separate infusion line.
pairment (Appendix 4); pregnancy (Appendix Tablet, Neostigmine bromide 15 mg. (but neostigmine usually preferred); Adverse effects: Fever and influenzae like symp-
2) and breastfeeding (Appendix 3); interac- CHILD, total daily dose 1–12 mg toms (sometimes accompanied by malaise, rigors,
POM Neostigmine (Alpha)
tions: Appendix 1. given in divided doses at appropriate fatigue and flushes) are common during treatment
Tablet, Neostigmine 15 mg.
Adverse effects: Increased salivation, nausea 15 mg – 140’s
intervals. with disodium pamidronate but generally resolve
and vomiting, abdominal cramps, diarrhoea; spontaneously. Severe local reactions and throm-
Injection, Neostigmine 2.5 mg per mL; in 1 mL amp. POM Pyridostigmine (WMF 20.2)
signs of overdosage include bronchocon- bophlebitis have followed administration as a
Tablet, Pyridostigmine bromide 60 mg. bolus injection. Rare CNS effects include agitation,
striction, increased bronchial secretions, PYRIDOSTIGMINE Injection, Pyridostigmine bromide 1 mg/mL, 1-mL confusion, dizziness, somnolence and insomnia.
lacrimation, excessive sweating, involuntary Indications: Myasthenia gravis. ampoule. Seizures have been precipitated in a few patients. In
defecation and micturition, miosis, nystag- Contraindications: Recent intestinal or blad- addition to hypocalcaemia and hypophosphataemia
POM Pyridostigmine (EDL 17.2)
mus, bradycardia, heart block, arrhythmias, der surgery; mechanical intestinal or urinary Tablet, Pyridostigmine bromide 60 mg. (which are common) hypomagnesaemia and rarely
hypotension, agitation, excessive dreaming, tract obstruction; after suxamethonium; hypernatraemia and hyperkalaemia or hypokalae-
weakness eventually leading to fasciculation pneumonia; peritonitis. 2.5 Drugs affecting bone structure mia have occurred. Hypotension and hypertension
and paralysis; thrombophlebitis reported; rash have been reported.
Precautions: Asthma; urinary tract infection; CVD and mineralization
associated with bromide salt. Dose: By slow IV infusion (over 2-8 hours),
including arrhythmias (especially bradycardia or Bisphosphonates inhibit the action of the
Nursing action: 15-90 mg at a rate not exceeding 15
atrioventricular block); hyperthyroidism; hypoten- osteoclasts (bone cells that remove osseous
• Administer with food or milk if GI upset occurs mg/hr. May be given as a single slow
(absorption is better on an empty stomach).
sion; peptic ulcer; epilepsy; parkinsonism; avoid or bone tissues by removing its mineralized infusion or in divided doses given on
• Observe patient for bronchospasm, hypotension, intravenous injection; renal impairment (Appen- matrix) and thereby prevent the resorption of consecutive days.
respiratory depression, headache, dizziness and dix 4); pregnancy (Appendix 2) and breastfeeding bone. They include Alendronate, Pamidro- Preparation of solution: Pamired is reconsti-
convulsions (discontinue therapy and inform the (Appendix 3); interactions: Appendix 1. nate, Risedronate, Etidronate, etc. tuted by adding 10 mL of sterile water for in-
doctor if these occur). Adverse effects: Muscarinic effects generally
• Monitor patient’s VS, respiration.
jection, to each vial, resulting in a solution of 30
weaker than with neostigmine: increased ALENDRONATE
• Evaluate patient’s therapeutic response namely mg/10 mL or 60 mg/10 mL. The reconstituted
salivation, nausea and vomiting, abdominal
increased muscle strength, hand grasp, improved POM ALENDOMAX® (Joswe/Afrab) solution is stable for up to 24 hrs when stored
cramps, diarrhoea; signs of overdosage include
gait. Caplet, Alendronic acid (as sodium salt) 70 mg. below 25oC. Avoid freezing. The drug should
bronchoconstriction, increased bronchial
• Notify physician if nausea, vomiting, muscle be completely dissolved before the solution
weakness, severe abdominal pain, or difficulty in
secretions, lacrimation, excessive sweating, POM RALENOST® (Ranbaxy)
is withdrawn.
breathing occurs. involuntary defecation and micturition, Tablet, Alendronic acid (as sodium) 70 mg
• Aropine sulphate and adrenaline should be ready miosis, nystagmus, bradycardia, heart block, 70 mg – 3 x 4’s
112 | 2.6 Topical antirheumatic drugs 2.7 Enzymes and miscellaneous anti-inflammatory agents | 113
2.6 Topical antirheumatic drugs Pack: 4 g; 25 g. Pack: 4 g; 25 g. on the indication and the response obtained.
Liniment, same as for ointment Treatment beyond two weeks duration is not
OTC HOTGEL® (Al-Tinez)
METHYL SALICYLATE Pack: 100 mL. recommended and therapy should be reviewed
Gel, Methylsalicylate 2.8 g, menthol 1.2 g
Therapeutic category: Counter irritant Pack: 20 g OTC SEFSIL® (Reals) after this time.
Indications: Relief of pain, swelling, stiffness Ointment, Gaultheria fragrantissima wall OTC BUCLOMEN® (JB Pharma)
OTC Moko Nerve Liniment (New Healthway)
associated with rheumatism and other mus- (Wintergreen oil) 24.0%, Mentha piperata (Menthol) Gel, Oleum lini (containing predominantly linolenic
Emulsion, Ammonium chloride 1.88 g, ammonium
6.0%, Cinnamomum camphora 5.5%, Eucalyptus
culo-skeletal disorders. bicarbonate 3.75 g, ammonium solution 2.6 mL, acid) 3%, diclofenac diethylammonium salt equiv.
globulus labill 5.0%, Pinus longifolia Roxb. 5.0%, to diclofenac sodium 1%, methyl salicylate 10%,
Precautions: Avoid contact with eyes, mucous turpentine oil 12.5 g.
Pitychotis ajowan 2.0%; in ointment base
membranes, broken or irritated skin. Pack: 200 mL. menthol 5%, benzyl alcohol 1%.
Pack: 7 g; 12 g Pack: 30 g tube
Administration: Apply generously and gently OTC MALPASS® (Neros)
massage 3-4 times daily. OTC Soothys Range of Patches (Korlyns) OTC CAPSIFENAC® (Phillips)
Spray, Menthol 5.83 g, camphor 4.17 g, methysa-
Patches, Diclofenac, menthol. Gel, Capsaicin (as Capsicum oleoresin) 0.025%,
OTC Methyl Salicylate (EDL 12.4) licylate 37.3 g per 100 g; in 80 mL spray solution.
Pack: 100 g/80 mL x 6’s (in cans). OTC SPORTGESIC® (Neimeth) Diclofenac diethylamine 1.16%, LevoMenthol 1%,
Ointment or Liniment, Methyl salicylate 4-20%
Administration: Spray onto the painful area (no Ointment, Methyl salicylate 15% Methylsalicylate 3%; in a gel base.
OTC Methyl Salicylate Compound (EDL 14.2) longer than 3 seconds), 4-5 times daily; may use for Pack: 35 g tube Pack: 10 g; 20 g (in tubes)
Ointment, Liniment, Embrocation or Inhalation, Vari- 5-7 days. Shake well before use.
OTC SPRANE® (Fidson) OTC NEUROGESIC® Extra (Drugfield)
ous Formulations of the approved active ingredients
OTC MOOV® (Jawa) Ointment, Methylsalicylate, capsaicin, menthol Ointment, Methylsalicylate 15%, menthol 5%, di-
and strengths as specified in the EDL.
Spray, Gaultheria fragrantissima, Mentha vridis Pack: 20 g (in tube). clofenac diethylamine 1.16% equiv. to diclofenac
OTC BAM-BAM® (Jawa) Pack: 150 mL sodium 1%; greaseless and stainless ointment
Ointment, Methyl salicylate 5%, menthol 5.5%, pine OTC TRANSVASIN® (Olpharm) Pack: 25 g; 35 g.
Ointment, Pinus roxburghii, Eucalyptus globutus
oil 0.5%, oleoresin capsicum 0.3%, eucalyptus oil Ointment (Heat rub), Diethylamine salicylate, hydrox-
Pack: 25 g; 50 g OTC ZETGEL® (Fidson)
yethyl salicylate, methyl nicotinate.
EMDEX
3%, camphor 11%.
OTC NEUROGESIC® (Drugfield) Pack: 40 g. Gel, Diclofenac diethylammonium (equiv. to Di-
Pack: 4 g (in metal tin); 25 g (in bottle).
Ointment, Methylsalicylate, menthol; greaseless Spray, Diethylamine salicylate, hydroxethyl salicylate, clofenac sodium 1% w/w), Methyl salicylate 10%
OTC BAUME LEOPARD® (Shalina) ointment. methyl nicotinate. w/w, Linseed oil ( containing a-linolenic acid)
Cream, Methyl salicylate 7% w/w, menthol 7% w/w, Pack: 35 mg. Pack: 125 mL. 3%w/w, Menthol 5% w/w.
oil of turpentine 7% w/w, camphor 10% w/w, euca- Pack: 20 g tube.
lyptus oil 14.5% w/w, thymol 1% w/w, lemon grass POM Nomagesic Balm (Nomagbon) OTC ULTIMAX® (Hovid) Dose: Apply thin film to affected area 2-3 times daily.
5% w/w, peppermint oil 1.5% w/w, citronella oil 1% Ointment, Methyl Salicylate 52.36 %, camphor 2.62%, Cream, Methyl salicylate 25.5%, menthol 3.3%, euca- Avoid excessive use.
w/w, cinnamon oil 1% w/w. eucalyptus oil 2.64 %, menthol 10.46 % per 25 g; lyptus oil 10%; pale green, opaque cream.
yellow ointment. Pack: 15 g; 30 g
Pack: 30 g
Pack: 25 g glass bottle 2.7 Enzymes and miscellaneous
OTC BENGAY® (Pfizer/Neimeth) OTC UPHEAT® Plus (Award Global) anti-inflammatory agents
Ointment, Methylsalicylate 15%, menthol 10%; OTC NOWW-NOWW ®(Jawa) Cream, Methyl salicylate 20%, menthol 10%, cam-
greaseless and stainless. Ointment, Methyl salicylate 20%, menthol 10%, phor 5%, eucalyptus oil 2%, cinnamon oil 0.4%. HYALURONIDASE
Pack: 35 g; 85 g (in tubes). oleoresin capsicum 1.5%, camphor oil 5%. Pack: 25 g
Pack: 25 g tube. Pharmacology: Hyaluronidase is an enzyme
OTC Cartwright’s Nerve & Bone® (BCN) OTC VILICIN® (Daily Need) which modifies the permeability of connective
Liniment, Turpentine oil 12.5%, oleic acid 2.5%, am- OTC Pain Doctor (SKG) Ointment, Methylsalicylate, menthol. tissue through the hydrolysis of hyaluronic
Ointment, Menthol 5.91% w/w, Eucalyptus oil 0.97% Pack: 25 g.
monium bicarbonate 3.75%, ammonium chloride acid, a polysaccharide found in the intercel-
1.875%, strong ammonia solution 2.50%. w/w, Methyl Salicylate 12.80% w/w, Turpentine oil
lular ground substance of connective tissue,
Pack: 150 mL. 1.47% w/w.Pack: 35 g. DICLOFENAC plus CAPSAICIN
plus METHYLSALICYLATE and of certain specialized tissues, such as the
OTC DEEP HEAT® (Kensington) OTC OSTEO Balm® (GoldMoore) umbilical cord and vitreous humor. Hydrolysis
Ointment, Pudina Ka Phool (Mentha piperita) 6% Indications: Relief from pain and inflammation
Cream, Eucalyptus oil 1.97% w/w, Turpentine oil associated with musculoskeletal disorders of hyaluronic acid causes temporary decrease
w/w, Karpoor (Cinnamonum camphora) 5.5% w/w,
1.47% w/w, Menthol 5.91%, Methylsalicylate 12.8%
such as sprains, strains, tendonitis, bursitis, in the viscosity of the cellular cement resulting
w/w; chalky cream. Tarpin Ka Tel (Pinus longifolia oil) 5% w/w, Ajowan
ka Phool (Ptychotis ajowan) 2% w/w, Wintergreen head, neck and shoulder pain, sciatica, muscle in enhanced diffusion of injected fluids or of
Aerosol spray, Methylsalicylate 1%, Methyl nicotinate localized transudates or exudates, thus facilitat-
1.6%, Hydroxyl ethyl salicylate 5%; in pressurized Oil (Gaultheria procumbens) 24% w/w, Nilgiri Ka tel stiffness, loint pain, backache and lumbago.
(Eucalyptus oil) 5% w/w. Contra-indications: Hypersensitivity to ing their absorption. When no spreading factor
container.
Pack: 12 g. NSAIDs and other ingredients of the prepa- is present, material injected subcutaneously
OTC DEEP RELIEF® (Embassy) spreads very slowly, but hyaluronidase causes
POM RELEEV® (Unique) ration.
Cream, Menthol 5.91%, eucalyptus oil 1.91%, methyl- rapid spreading.
salicylate 12.8%, turpentine 1.47%. Ointment, Methylsalicylate Precautions: Wash your hands thoroughly after
Pack: 20 g. each use. Avoid contact with the eyes. Do not Indications: To enhance permeation of sub-
Pack: 30 g.
apply to open wounds. cutaneous or intramuscular injections, local
POM Galways Nerve & Bone® (SKG) POM REUMEX® (Afrab-chem) anaesthetics and subcutaneous infusions and
Lotion, Methyl salicylate 160 mg, camphor 24 mg, Adverse effects: Skin rash, itching and redness.
Liniment, Turpentine oil 12.5%, ammonium bicar- to promote resorption of excess fluids and
bonate 3.7%, ammonium chloride 1.87%, strong menthol 100 mg, eucalyptus oil 20 mg, capsicum Dose: Adult: Apply 3 or 4 times daily and
rub in gently; amount depends on blood in the tissues.
ammonium solution 2.50%, oleic acid 2.50%. oleoresin 5 mg per 1 mL
Pack: 50 mL the size of affected area. Child: Not Contra-indications: Hypersensitivity to hyalu-
OTC HEATOL® (P.Z.) recommended. ronidase or bovine proteins. Avoid IV injection
Ointment, Camphor synthetic 26%, peppermint oil OTC ROBB® (P.Z.) because the enzyme is rapidly inactivated. Not
Ointment, Camphor synthetic 11%, menthol crys- Note: Wash hands after application, unless
13%, cajaput oil 10%, menthol crystals 8%, clove for use in inflammation due to insect bites or
oil 5%. tals 5.5%, methyl salicylate 4%, eucalyptus oil 1%, they are the site being treated. Do not massage
vigorously. The duration of treatment depends stings or for anaesthetic procedures in cases of
pumilio pine oil 0.5%.
114 | 2.7 Enzymes and miscellaneous anti-inflammatory agents 2.7 Enzymes and miscellaneous anti-inflammatory agents | 115
unexplained premature labour. Avoid injection nausea, vomiting) may occur. Discontinue if hyper- POM CEEMORAL® (N.C.I) tration at the site of infection and prevention of
into or around an infected or acutely inflamed sensitivity (rash, redness) occurs. Rarely sputum Tablet, Trypsin, chymotrypsin formation of adhesions.
area because of the danger of spreading a cruentum, bleeding may occur. Pack: 3 x 10’s Dose: By mouth, 1-2 lacs Armour units (AU) 4 times
localized infection. Avoid direct application Dose: Adults, initially 2 tablets 4 times daily; one daily; to be swallowed ½ hour before meals.
POM G-TRYP® (Greenlife)
tablet 4 times daily as maintenance dose.
to cornea. Tablet, Trypsin plus Chymotrypsin (6:1) 50,000 Ar- POM KOTASE® (Al-Tinez)
Dosage adjustment is based on the age
Precautions: Discontinue if sensitization oc- or severity.
mour units; e-c tab. Tablet, Bromelain 20,000 units (40 mg), Crystalline
curs. Patients with infections; renal impairment. Pack: 3 x 10’s trypsin 2,500 units (1 mg); green s-c tab.
Pregnancy, lactation. POM CHYMOTASE® (PharmacyPlus) Description: Proteolytic enzymes speed the healing Pack: 100’s.
Tablet, Bromelain 40 mg, crystalline trypsin 1 mg; of damaged tissue. Trypsin & Chymotrypsin are Indications: Relief of symptoms related to inflam-
Adverse effects: Occasionally, allergic reac-
red, green enteric s-c tab. released and absorbed in the small intestine. The mations such as edema, swelling, pain, eruption and
tions may occur and rarely, accompanied by Pack: 10’s (in blisters) enteric coating protects the enzymes from the resolutions of inflammation resulting from areolitis,
symptoms of shock. Local irritation, infection, Indications: Relief of inflammatory symptoms destructive activity of the acid in the stomach and thrombosis, haematoma, fracture distortion, internal
bleeding and bruising occur rarely. (edema, swelling, pain, redness) in fracture, distor- promotes intestinal absorption. hemorrhoids, external hemorrhoids, and prolapse,
Dose: Adults, children and the elderly: tion, internal haemorrhoid, external haemorrhoid, Indications: Resolution of acute inflammatory post-operative hemorrhoids.
Adjunct in hypodermoclysis, 1500 IU incarcerated haemorrhoid, proctoptosis or after oedema associated with accidental and surgical Dose: By mouth, Adults, initially 2 tablets 4 times
for every 500-1,000 mL of fluid for SC haemorrhoidal operation, breast congestion, mas- trauma, episiotomies, in pelvic inflammatory daily. Maintenance 1 tablet 4 times daily.
admin. titis, haematocele, embolism. disorders, intervertebral disc herniation (sciatica), Reduce the dosage according to the age
Facilitate SC/IM injections, 1500 IU Dose: Adults, initially 2 tablets 4 times a day; then 1 thrombophlebitis, vasectomies and reduction in & b.wt.
tablet 4 times a day as maintenance dose. viscosity of mucus and sputum associated with
dissolved directly in the soln to be POM MEDMORAL® (Embassy)
Adjust dose based on the patient’s age and bronchitis, rhinitis and sinusitis, dental extraction
injected. symptoms. Do not chew because tablets are and surgery, enhancement of antibiotic concen-
Tablet, Trypsin/Chymotrypsin 50,000 units.
Enhance diffusion of local anaesthetics, Pack: 30’s.
enteric coated.
1500 IU is mixed with the quantity of
EMDEX
local anaesthetic soln to be used. OTC BROMAPLEX® (Crystal)
Tablet, Bromelain 40 mg, trypsin 1 mg.
Enhance diffusion of local anaesthetic
Pack: 10 x 10’s.
in ophthalmology, 15 IU/mL of local
anaesthetic soln. POM BROMTASE® (Eutrix)
Enhance dispersal of extravasated flu- Tablet, Bromelain 40 mg, crystallized trypsin 1 mg;
white enteric s-c tab.
ids or blood, 1500 IU in 1ml water for
Indications: Relief of inflammatory symptoms
injections or normal saline infiltrated (edema, swelling, pain, rubefaction) in: frature,
into the affected area as soon as pos- sprain, internal pile, external piles, incarcerated piles,
sible after the extravasation is noted. after proctoptosis and haemorrhoidectomy, mastitis,
Note: Reconstitute immediately before use with the haematoma, thrombosis.
1 mL normal saline or mix directly in the soln to be Precautions: Blood disorder; severe hepatic or
injected with hyaluronidase. renal disorder. Discontinue if rash or redness occurs
(Additional information sourced from Hyalase monograph (hypersensitivity).
available from: http://www.medicines.org.uk/) Adverse effects: Constipation, diarrhoea; occasion-
ally anorexia, gastric discomfort, vomiting, nausea
POM HYDASE® (Mark) may occur; rash or redness (discontinue).
Injection, Hyaluronidase 1,500 I.U.; powder for Dose: Adults, Initially 2 tablets 4 times daily;
reconstitution in amp. plus 1 mL isotonic NaCl soln one tablet 4 times daily as mainte-
as solvent nance dose. Dosage adjustments is
Pack: 6’s
based on the age or severity.
TRYPSIN plus BROMELAIN
TRYPSIN plus CHYMOTRYPSIN
See under the preparations below
See under the preparations below.
POM BROMLEY® (Next Generation)
OTC CHEMZYME® (Adler)
Tablet, Bromelain 40 mg, crystalline trypsin 1 mg;
Tablet, Trypsin-chymotrypsin
red coated tab
Pack: 10 x 10’s (in blisters) POM CHYMORAL® Forte (Atsi)
Indications: Relief of symptoms related to inflam- Tablet, Trypsin plus Chymotrypsin (6:1) 100,000
mations such as oedema, swelling, pains. armour units; sunset yellow e-c tab.
Contra indications: Severe hepatic and renal dys- Pack: 3 x 10’s.
function; blood disorders, peptic ulcer, abnormalities Indications: Relief of inflammatory oedema, hemat-
of blood clotting, brown atrophy, progressive liver cir- oma, pain associated with accidental and surgical
rhosis; accompanying infections (proper antibiotics trauma, episiotomies, pelvic inflammatory disorders,
or chemotherapeutics may be used in combination). post-caesarean section, hysterectomy, fractures,
Adverse effects: Occasionally GI disorders namely muscle and tendon injuries, intervertebral disc
constipation, diarrhoea, anorexia, gastric discomfort, herniation (sciatica) and to reduce necrotic damage.
vomiting, and nausea; local stimulating reactions Dose: By mouth, Adult, 1 tablet 4 times a day; to
(redness, pain), systemic reactions(fever, headache, be swallowed whole 30 mins before meals.
3.1 General anaesthetics and oxygen | 117
3. Drugs used in
This section describes drugs used in anaesthesia. The Intravenous induction using thiopental is
reader is referred to WHO. Model Prescribing Informa- rapid and excitement does not usually occur.
tion. Drugs used in Anaesthesia. Geneva: WHO; 1989 Anaesthesia persists for about 4–7 minutes;
for more detailed information.
anaesthesia
large or repeated doses severely depress res-
To produce a state of prolonged full surgical piration and delay recovery.
anaesthesia reliably and safely, a variety of Anaesthesia with ketamine persists for up to
3.1 General anaesthetics and oxygen . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 117 drugs is needed. Special precautions and close 15 minutes after a single intravenous injection
monitoring of the patient are required. These and is characterized by profound analgesia. It
3.1.1 Intravenous agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 117 drugs may be fatal if used inappropriately and may be used as the sole agent for diagnostic
3.1.2 Volatile inhalational agents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 119 should be used by non–specialized personnel and minor surgical interventions. Subanaes-
only as a last resort. Irrespective of whether thetic concentrations of ketamine may be used
3.1.3 Inhalational gases . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 121 a general or conduction (regional or local) to provide analgesia for painful procedures of
3.2 Preoperative medication and sedation for short-term procedures. . . . . . . . . . . 121 anaesthetic technique is used, it is essential short duration such as the dressing of burns, ra-
that facilities for intubation and mechanically diotherapeutic procedures, marrow sampling
3.3 Muscle relaxants and cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . 124 assisted ventilation are available. A full pre- and minor orthopaedic procedures. Recovery
3.3.1 Muscle relaxants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 124 operative assessment is required including, from ketamine anaesthesia is associated
if necessary, appropriate fluid replacement. with a high incidence of hallucinations and
3.3.2 Cholinesterase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 127 other emergence reactions, such as delirium.
Anaesthesia may be induced with an intrave-
3.4 Local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 128 nous barbiturate, parenteral ketamine, or a Ketamine is of particular value in children, in
volatile agent. Maintenance is with inhalational whom hallucinations are believed to be less
3.5 Analgesics and opioid antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 130
significant.
EMDEX
agents often supplemented by other drugs
3.6 Blood substitutes and solutions for correcting fluid imbalance. . . . . . . . . . . . . . 131 given intravenously. Specific drugs may be
THIOPENTAL
3.7 Others . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 131 used to produce muscle relaxation. Various
drugs may be needed to modify normal phys- Synonym: Thiopentone Sodium.
iological functions or otherwise to maintain Therapeutic category: Anticonvulsant; Barbi-
the patient in a satisfactory condition during turate; General Anaesthetic; Sedative.
surgery. Indications: Induction of anaesthesia prior
to administration of inhalational anaesthetic;
LONG-TERM MEDICATION:
anaesthesia of short duration.
The risk of stopping long-term medication Contra-indications: Inability to maintain
before surgery may be greater than the risk airway; hypersensitivity to barbiturates; car-
of continuing it. It is essential that the anaes- diovascular disease; dyspnoea or obstructive
thetist is told of all drugs that the patient is respiratory disease; myotonic dystrophy;
(or has been) taking; for further advice see porphyria.
section 6.2 (drugs affecting coagulation), Precautions: Reconstituted solution is highly
section 10.3 (corticosteroids), section 11.3.1 alkaline—extravasation can result in extensive
(hormonal contraceptives), and section 10.1 tissue necrosis and sloughing; cardiovascular
(diabetic patients). disease; intraarterial injection causes intense
pain and may result in arteriospasm; hepatic
3.1 General anaesthetics and oxygen impairment (Appendix 5); pregnancy (Appen-
3.1.1 Intravenous agents dix 2); breastfeeding (Appendix 3); interac-
3.1.2 Volatile inhalational agents tions: Appendix 1.
3.1.3 Inhalational gases Adverse effects: Rapid injection may result in
severe hypotension and hiccup; arrhythmias,
3.1.1 Intravenous agents myocardial depression, cough, laryngeal
spasm, sneezing, allergic reactions, rash, in-
IV anaesthetics may be used alone to produce
jection-site reactions.
anaesthesia for short surgical procedures but
Advice to patients: Warn patient not to
are more commonly used for induction only.
perform skilled tasks, for example operating
They can produce apnoea and hypotension
machinery, driving, for 24 hours and also to
and thus facilities for adequate resuscitation
avoid alcohol for 24 hours.
must be available. They are contraindicated
Nursing action:
if the anaesthetist is not confident of being
• Test dose may be given to assess patient’s
able to maintain an airway. Before intubation is
reaction to drug.
attempted, a muscle relaxant must be given. In-
• Monitor vital signs every 3-5 minutes during
dividual requirements vary considerably; lesser
I.V. administration.
dosage is indicated in the elderly, debilitated
• Make emergency resuscitative equipment
or hypovolaemic patients.
118 | 3.1.1 Intravenous agents 3.1.2 Volatile inhalational agents | 119
and oxygen available; maintain airway. accompanied by irrational behaviour (effects Injection, Ketamine (as HCl) 50 mg/mL; in 10-mL vial. vials should be discarded after 12 hours.
• Avoid extravasation as necrosis may occur. rarely persist for more than few hours but can POM Ketamine (EDL 1.1) • Observe closely for signs of significant hypo-
• Monitor for respiratory distress; in general recur at any time within 24 hours); transient Injection, Ketamine (as HCl) 10 mg per mL in 20 mL tension or bradycardia; may be treated with
anaesthesia, atropine sulfate may be given elevation of pulse rate and blood pressure vial; 50 mg per mL in 10 mL vial; 100 mg per mL increased rate of fluid administration, pressor
as premedication to prevent laryngeal spasm. common, arrhythmias have occurred; hypo- in 5 mL vial. agents, elevation of lower extremeties, or
• Place patient in Sim’s position if vomiting, to tension and bradycardia occasionally reported. POM Elfa Ketamin (Mark)
atropine.
prevent from aspirating vomitus. Advice to patients: Warn patient not to Injection, Ketamin HCl 50 mg • Apnoea may occur during induction and will
Dose: Induction, by IV injection usually as perform skilled tasks, for example operating Pack: 10 mL x 25’s. require ventilatory support if it persists for
a 2.5% (25 mg/mL) solution over machinery, driving, for 24 hours and also to longer than 60 seconds.
POM Ketamine (Alpha)
10–15 seconds, ADULT 100–150 mg avoid alcohol for 24 hours. • Avoid abrupt discontinuation if infusion prior
Injection, Ketamine HCl 50 mg; in 10 mL vial.
(reduced in elderly or debilitated Nursing action: Administer I.V. for over 1 min- to weaning or daily wake up assessments; it
patients), followed by a further ute; inject the dose directly into vein or into IV POM Ketamine (Jawa) can cause rapid awakening, anxiety, agitation,
100–150 mg if necessary according infusion containing free flowing compatible Injection, Ketamine HCl 50 mg and resistance to mechanical ventilation.
to response after 30–60 seconds; solution. Pack: 10 mL Dose: Induction, by IV injection, healthy
or up to 4 mg/kg (maximum 500 • Monitor vital signs before, during and after POM KETMIN® (Embassy) Adult, 1.5-2.5 mg/kg at a rate of 2-4
mg); CHILD 2–7 mg/kg repeated if anaesthesia. Injection, Ketamine (as HCl) 50 mg per mL mL every 20 seconds; adjust dose ac-
necessary according to response after • Because of rapid induction, patient should be Pack: 10 mL x 25’s. cording to response. Child (3-8 years):
60 seconds. physically supported during administration. POM RETAMINE® (Goldmoore) usually about 2.5mg/kg.
Reconstitution: Solutions containing 25 mg/mL • Maintain clear airway and keep resuscitation Injection, Ketamine 10 mg. Maintenance, by IV infusion, Adult,
should be freshly prepared by mixing 20 mL of water equipment ready for use. usually 4-12 mg/kg/h; adjust dose
for injections with the contents of the 0.5-g ampoule • Start supportive respiration if respiratory de- PROPOFOL to maintain depth of anaesthesia
EMDEX
or 40 mL with the 1-g ampoule. Any solution made
pression occurs, using mechanical support if Therapeutic category: General anaesthetic; required.
up over 24 hours previously or in which cloudiness,
precipitation or crystallization is evident should
possible rather than administering analeptics. Sedative Child (3-8 years):usually 9-15 mg/kg/h
be discarded. • Provide a quiet environment and ensure Indications: Induction and maintenance of Sedation during intensive care, by IV
that patient is not disturbed during recovery general anaesthesia; sedation of ventilated infusion, Adult, usually 0.3-4 mg/kg/h;
POM Thiopental (WMF 1.1) phase to reduce emergent reactions. adjust dose according to depth of
Injection, Thiopental (as sodium salt) 0.5 g, 1 g; adult patient receiving intensive care.
• Patient may become excited and suffer from Contra-indications: Hypersensitivity to sedation required.
powder for injection in ampoules.
hallucination when recovering from anaes- Propofol or Propofol’s emulsion which contains Note: Not recommended for ICU sedation in children
POM Thiopental Sodium (EDL 1.1) thesia; diazepam may be prescribed. of all ages and for anaesthesia in children <3 years.
soybean oil, egg lecithin, and glycerol.
Injections, Thiopental (as sodium salt) 0.5 g, 1.0 g, 2.5 • Ketamine is a potent hallucinogen that can Precautions: Monitor for signs of hypotension, POM DIPRIVAN® (Reals)
g; powder for IV injection in amps. readily produce dissociative anaesthesia (i.e., airway obstruction and oxygen desaturation, Injection, (emulsion), Propofol 10 mg per mL.
POM Thiopental Sodium (Alpha) patient feels detached from environment). disorders of fat metabolism (1ml preparation POM NEPOL® (Next Generation)
Injection, Thiopental sodium 0.5 g, 1.0 g; powder The dissociative effect and hallucinatory side contains 0.1g fat); cardiac, respiratory, renal or Injection, Propofol 200 mg per 20 mL.
for injection. effects have resulted in the abuse of this drug. hepatic impairment; avoid in pregnancy and Pack: 5 amps (in box)
Dose: Induction, by IM injection, ADULT and obstetric anaesthesia; breast-feeding (safety to
KETAMINE POM NIRFOL® (Jawa)
CHILD 6.5–13 mg/kg (10 mg/kg neonate not established); epilepsy (convulsion Injection, Propofol 1%.
Indications: Induction and maintenance of usually produces 12–25 minutes of may occur); bradycardia; contains no antimicro- Pack: 20 mL (vial).
anaesthesia; analgesia for painful procedures anaesthesia); maintenance, 50–100% bial preservative and should be used within 6
of short duration. of induction dose as required. POM POFOL® (Alpha)
hours of opening and dilution (dilution should
Contra-indications: Thyrotoxicosis; hyper- Induction, by IV injection over at least Injection, Propofol 10 mg per mL; in 20 mL amps
be done aseptically); elderly. & 50 mL vials.
tension (including pre-eclampsia); history of 1 minute, ADULT and CHILD 1–4.5 Adverse effects: Hypotension, transient ap-
cerebrovascular accident, cerebral trauma, mg/kg (2 mg/kg usually produces noea; post-operative fever, nausea, vomiting
intracerebral mass or haemorrhage or other 5–10 minutes of anaesthesia); main- 3.1.2 Volatile inhalational agents
and headache, rarely convulsion, anaphylaxis,
cause of raised intracranial pressure; eye injury tenance 50–100% of induction dose discolouration of urine, pain on injection, One of the volatile anaesthetics, ether, halo-
and increased intraocular pressure; psychi- as required. thrombosis and phlebitis; sexual disinhibition thane (with or without nitrous oxide), must
atric disorders, particularly hallucinations; Induction, by IV infusion of a solution on recovery from anaesthesia; pulmonary be used for induction when IV agents are con-
porphyria. containing 1 mg/mL, ADULT and oedema. traindicated and particularly when intubation
Precautions: Supplementary analgesia often CHILD total induction dose 0.5–2 mg/ Nursing action: Drug should be administered is likely to be difficult.
required in surgical procedures involving vis- kg; maintenance (using microdrip only by persons who are familiar with airway Full muscle relaxation is achieved in deep
ceral pain pathways (morphine may be used infusion), 10–45 µg/kg/minute, rate management and the administration of I.V. anaesthesia with ether [no longer included on
but addition of nitrous oxide will often suf- adjusted according to response. anaesthetics. WHO Model List]. Excess bronchial and salivary
fice); administer an antisialogogue to prevent Analgesia, by IM injection, ADULT and • Do not mix with other drugs or blood prod- secretion can be avoided by premedication
excessive salivation leading to respiratory dif- CHILD initially 4 mg/kg. ucts; may be diluted only with D5W before with atropine. Laryngeal spasm may occur
ficulties; during recovery, patient must remain Note: For diagnostic procedures and other proce- infusion (avoid dilution below 2 mg/mL); during induction and intubation. Localized
undisturbed but under observation; pregnancy dures not involving intense pain.
give over 3-5 min. Use only glass containers capillary bleeding can be troublesome and
(Appendix 2); interactions: Appendix 1. Dilution and Administration: According to manu-
facturer’s directions.
for mixing, not stable in plastic. postoperative nausea and vomiting are fre-
Adverse effects: Hallucinations and other • Tubing and any unused portions of propofol quent; recovery time is slow particularly after
emergence reactions during recovery possibly POM Ketamine (WMF 1.1)
120 | 3.1.2 Volatile inhalational agents 3.1.3 Inhalational gases | 121
prolonged administration. hospital (high risk of arrhythmias); pregnancy in heart rate; Respiratory depression, rarely emergency management of injuries, during
If intubation is likely to be difficult, halothane (Appendix 2) and breastfeeding (Appendix 3); bronchospasms; Disturbance of the liver postoperative physiotherapy and for refractory
is preferred. It does not augment salivary or interactions: Appendix 1. function, icterus, & liver damage; Shivering, pain in terminal illness.
bronchial secretions and the incidence of Adverse effects: Arrhythmias; bradycardia; nausea, and vomiting upon waking from the Contra-indications: Demonstrable collection
postoperative nausea and vomiting is low. respiratory depression; hepatic damage. anaesthesia; Malignant hyperthermia; irrita- of air in pleural, pericardial or peritoneal space;
Severe hepatitis, which may be fatal, some- Dose: Induction, using specifically calibrated tion of mucous membranes accompanied by intestinal obstruction; occlusion of middle
times occurs; it is more likely in patients who vaporizer, gradually increase inspired coughing, respiratory depression, and rarely ear; arterial air embolism; decompression
are repeatedly anaesthetized with halothane gas concentration to 2–4% (ADULT) laryngospasms; increase in WBC count; Rash. sickness; chronic obstructive airway disease,
within a short period of time. or 1.5–2% (CHILD) in oxygen or Advice to patients: May impair ability to per- emphysema.
nitrous oxide–oxygen form skilled tasks (patient to avoid such tasks Precautions: Minimize exposure of staff; preg-
ETHER, ANAESTHETIC Maintenance, ADULT and CHILD for 24 hours following anaesthesia). nancy (Appendix 2); interactions: Appendix 1.
0.5–2%. Dose: Individualised according to patient’s Adverse effects: Nausea and vomiting; after
Deleted from the current WHO Model Formulary. need and response. prolonged administration megaloblastic anae-
Drug subject to international control under the United POM Halothane (WMF 1.1)
Inhalation, Volatile liquid POM AERRANE® (Alpha)
mia, depressed white cell formation; peripheral
Nations Convention against Illicit Traffic in Narcotic
Liquid for Inhalation, Isoflurane 250 mL; clear col- neuropathy.
Drugs and Psychotropic Substances (1988). POM Halothane (EDL 1.1)
ourless liquid in an amber bottle with black cap and Dose: Anaesthesia, ADULT and CHILD nitrous
Indications: Induction and maintenance of Inhalation, Halothane 250 mL; liquid in bottle.
purple ring around the neck. oxide mixed with 25–30% oxygen
anaesthesia (administered from many types POM FLUOTHANE® (Reals) Pack: 1 x 6’s Analgesia, 50% nitrous oxide mixed
of vaporizers). Halothane 0.01% w/w;, Colourless volatile liquid, with 50% oxygen.
POM HALOCARBON® (Alpha)
Contra-indications: Severe liver disease; non-explosive and non-flammable in the concen-
Injection, Isoflurane 250 mL. POM Nitrous oxide (WMF 1.1)
diabetes mellitus; impaired kidney function; tration usually used.
Inhalation gas.
EMDEX
raised cerebrospinal fluid pressure. Pack: 250 mL.
3.1.3 Inhalational gases POM Nitrous Oxide (EDL 1.1)
Precautions: Risk of potentially fatal convul- POM Halothane (Alpha)
sions in febrile patients; pregnancy (Appendix Injection, Halothane 250 mL. Nitrous oxide is used for the maintenance of Inhalation, Medicinal gas.
2); interactions: Appendix 1. anaesthesia. It is too weak to be used alone,
ISOFLURANE but it allows the dosage of other anaesthetic OXYGEN
Fire Hazard: Diathermy must not be used when agents to be reduced. It has a strong analgesic
Indications: Volatile halogenated anaesthetic Indications: To maintain an adequate oxygen
ether/oxygen mixtures in use and operating action.
for general inhalation anaesthesia. tension in inhalational anaesthesia.
theatre and its equipment should be designed
to minimize risk of static discharge, particularly Contra-indications: Hypersensitivity to hal- Oxygen should be added routinely during FIRE HAZARD: Avoid use of cautery when
in hot, dry climates. ogenated anaesthetics; known or suspected anaesthesia with inhalational agents, even oxygen is used with ether; reducing valves on
Adverse effects: Transient postoperative ef- genetic disposition toward malignant hyper- when air is used as the carrier gas, to protect oxygen cylinders must not be greased (risk of
fects include impairment of liver function and thermia; history of malignant hyperthermia, against hypoxia. Oxygen is also used in the explosion).
leukocytosis; nausea and vomiting; capillary liver dysfunction, jaundice or unexplained management of anaphylaxis (section 8.1), Precautions: interactions: Appendix 1.
bleeding. fever, leucocytosis, or eosinophilia after previ- myocardial infarction (section 5.6), and severe Adverse effects: Concentrations greater than
Dose: Induction, Adult and Child, up to 15% ous halogenated anaesthetic administration; acute asthma (section 7.1). 80% have a toxic effect on the lungs leading
in inspired gases. obstetric operation. Identification of cylinders for inhalation gases to pulmonary congestion, exudation and
Maintenance of light anaesthesia, Precautions: Closely monitor respiration & atelectasis.
assist if necessary; hepatic disease; coadmin- An ISO standard (International Standard 32,
Adult and Child 3–5% in air (with or Dose: Concentration of oxygen in inspired
istration with respiratory depressants e.g. Gas cylinders for medical use, 1977) requires
without muscle relaxants); up to 10% anaesthetic gases should never be
narcotic premedication; myasthenia gravis; that cylinders containing nitrous oxide should
for deep anaesthesia. less than 21%.
hypovolaemic, hypotensive and debilitated bear the name of the contents in legible and
POM Anaesthetic Ether (EDL 1.1) permanent characters and, preferably, also POM Oxygen (WMF 1.1)
patients (reduce dose). Inhalation, Medicinal gas.
Inhalation, Anaesthetic ether 500 mL; liquid in bottle.
Interactions: Nonselective MAOIs (stop 15 the chemical symbol N2O. The neck, from the
days prior to surgery); alpha– and beta– sym- valve to the shoulder, should be coloured blue. POM Oxygen (EDL 1.1)
HALOTHANE Cylinders containing oxygen intended for Inhalation, Medicinal gas.
pathomimetics e.g. epinephrine (risk of serious
Indications: Induction and maintenance of ventricular arrhythmia due to increase in heart medical use should bear the name of the con-
anaesthesia. rate); beta-blockers may intensify –ve inotropic tents in legible and permanent characters and, 3.2 Preoperative medication
Contra-indications: History of unexplained effects by blocking cardiovascular compensa- preferably, also the chemical symbol O2 . The and sedation for short-
jaundice or pyrexia following previous expo- tory mechanism (discontinue gradually before neck, from the valve to the shoulder, should term procedures
sure to halothane; family history of malignant be coloured white. Cylinders containing nitrous Pre-anaesthetic medication is often advisable
surgery or use beta-sympathomimetic agents);
hyperthermia; raised cerebrospinal fluid pres- oxide and oxygen mixtures should be similarly prior to both conduction and general anaes-
Isoniazid may increase hepatotoxic effect (stop
sure; porphyria. labelled, and the neck coloured white and blue. thetic procedures.
1 week before and for 15 days afterwards);
Precautions: Anaesthetic history should be Sedatives improve the course of subsequent
Indirect sympathomimetics; Muscle relaxing
carefully taken to determine previous exposure NITROUS OXIDE anaesthesia in apprehensive patients. Diaz-
agents; Ca2+ antagonists (particularly dihydro-
and previous reactions to halothane (at least 3 Indications: Maintenance of anaesthesia in epam and promethazine are effective. Diaze-
pyridine derivatives) may lead to marked hypo-
months should be allowed to elapse between combination with other anaesthetic agents pam can be administered by mouth, by rectum,
tension; Morphine analgesics may potentiate
each re-exposure); avoid for dental proce- (halothane, ether, or ketamine) and muscle or by intravenous injection. Promethazine,
respiratory depression; Pregnancy & lactation.
dures in patients <18 years unless treated in relaxants; analgesia for obstetric practice, for which has antihistaminic and antiemetic prop-
Adverse effects: Arterial hypotension; Increase
122 | 3.2 Preoperative medication and sedation for short-term procedures 3.2 Preoperative medication and sedation for short-term procedures | 123
erties as well as a sedative effect, is of particular chest pain, allergic reactions, constiaption. Precautions: Respiratory disease; muscle care units (ICU); induction and maintenance
value in children. • Observe for tachycardia if patient has cardiac weakness and myasthenia gravis; history of of anaesthesia; as an induction agent in inha-
A potent analgesic such as morphine (section problems. alcohol or drug abuse; marked personality lation anaesthesia or a sleep-inducing com-
3.5) should be administered preoperatively to • Drug causes urine retention and urinary hes- disorder; elderly or debilitated patients (ad- ponent in combined anaesthesia, including
patients in severe pain or for analgesia during itancy; patient should void before receiving verse effects more common in these groups); total intravenous anaesthesia; ataralgesia in
and after surgery. the drug. hepatic impairment (Appendix 5) or renal combination with ketamine in children.
Anticholinergic (more correctly antimuscarinic) Dose: Premedication, by IV injection, ADULT failure (Appendix 4); pregnancy (Appendix 2) Contra-indications: Hypersensitivity to ben-
drugs such as atropine are also used before 300–600 µg immediately before and breastfeeding (Appendix 3); close observa- zodiazepines; acute narrow-angle glaucoma.
general anaesthesia. They inhibit excessive induction of anaesthesia, CHILD 20 tion required until full recovery after sedation; Precautions: Elderly and debilitated patients;
bronchial and salivary secretions induced, in µg/kg (maximum 600 µg); by SC or IM porphyria; interactions: Appendix 1. obstructive pulmonary disease, chronic renal
particular, by ether and ketamine. IM adminis- injection, ADULT 300–600 µg 30–60 Adverse effects: CNS effects common and failure or CHF, myasthenia gravis; first three
tration is most effective, but oral administration minutes before induction; CHILD 20 include drowsiness, sedation, confusion, months of pregnancy, premature infants and
is more convenient in children. Lower doses µg/kg (maximum 600 µg). amnesia, vertigo, and ataxia; hypotension, neonates, breast–feeding.
should be used in cardiovascular disease or Intraoperative bradycardia, by IV bradycardia, or cardiac arrest, particularly in Adverse effects: Rarely respiratory depression,
hyperthyroidism. injection, ADULT 300–600 µg (larger elderly or severely ill patients; also paradoxical apnoea, respiratory arrest and/or cardiac arrest;
doses in emergencies); CHILD 1–12 reactions, including irritability, excitability, anaphylactoid reactions and skin reactions in
ATROPINE years 10–20 µg/kg. hallucinations, sleep disturbances; pain and isolated cases.
Therapeutic category: Anticholinergic Agent; Control of muscarinic side-effects of thromboembolism on IV injection. Nursing action: Give IM deep into a large
Antidote, Organophosphate Poisoning. neostigmine in reversal of competitive Advice to patients: Warn patient not to muscle mass.
Indications: To inhibit salivary secretions; to neuromuscular block, by IV injection, perform skilled tasks, for example operating • Oxygen and resuscitation equipment should
inhibit arrhythmias resulting from excessive ADULT 0.6–1.2 mg; CHILD under machinery, driving, for 24 hours and also to be ready for use during IV infusion.
EMDEX
vagal stimulation; to block the parasympath- 12 years (but rarely used) 20 µg/kg avoid alcohol for 24 hours. • Rapid dosage has been associated with
omimetic effects of anti-cholinesterases such (maximum 600 µg) with neostigmine Dose: Premedication, by mouth 2 hours be- respiratory arrest, particularly in the elderly.
as neostigmine; organophosphate poisoning 50 µg/kg. fore surgery, ADULT and CHILD over • Monitor IV infusion and avoid extravasation.
(section 19.2.3); mydriasis and cycloplegia POM Atropine (WMF 1.3)
12 years, 5–10 mg. • Observe BP, pulse, respiration and airway
(section 13.3). Injection, Atropine sulfate 1 mg/mL; in 1-mL am- Sedation, by slow IV injection imme- integrity.
Contra-indications: Angle-closure glaucoma; poule. diately before procedure, ADULT and • Provide assistance with ambulation, until
myasthenia gravis; paralytic ileus, pyloric ste- CHILD over 12 years, 200 µg/kg. drowsy period is over. Teach patient to avoid
POM Atropine (EDL 1.3)
nosis; prostatic enlargement. Administration: Absorption following IM in- hazardous activities that require alertness or
Injection, Atropine (as sulfate) 0.5 mg, 1 mg per mL;
Precautions: Down syndrome, children, in 1ml amps. jection slow and erratic; route should only be physical co-ordination.
elderly; ulcerative colitis, diarrhoea; hyperthy- used if oral or IV administration not possible. Dose: Premedication before an operation,
POM Atropine (Alpha) Slow IV injection into large vein reduces risk of by IM injection, Adult: 0.07-0.1 mg/
roidism; heart failure, hypertension; pyrexia;
Injection, Atropine sulfate 600 mcg per mL; clear &
pregnancy (Appendix 2) and breastfeeding thrombophlebitis. Resuscitation equipment kg b.wt., depending on the age and
colourless solution in 1-mL amp.
(Appendix 3); interactions: Appendix 1 must be available. condition of the patient; usually
Pack: 10 x 10’s
DURATION OF ACTION: Since atropine has a POM Diazepam (WMF 1.3)
about 5 mg.
shorter duration of action than neostigmine, POM REOPAN® (Vixa) Child: 0.15-0.20 mg/kg IM; by rectal
Tablet, Diazepam 5 mg.
Injection, Atropine 0.5 mg/mL. route, 0.35-0.45 mg/kg.
late unopposed bradycardia may result; close Injection, Diazepam 5 mg/mL; in 2-mL ampoule.
Pack: 0.5 mL x 10’s.
monitoring of the patient is necessary. Elderly and debilitated patients,
POM Diazepam (EDL 1.3)
Adverse effects: Dry mouth; blurred vision, 0.025-0.05 mg/kg IM.
DIAZEPAM Injection, Diazepam 5 mg per mL; in 2-mL amp.
photophobia; flushing and dryness of skin, Doses should be administered about
rash; difficulty in micturition; less commonly Drug subject to international control under the Conven- See under section 1.1 for the proprietary preparations 30 minutes before induction of
tion on Psychotropic Substances (1971). of Diazepam. anaesthesia (20-30 minutes by rectal
arrhythmias, tachycardia, palpitations; confu-
sion (particularly in elderly); heat prostration Indications: Premedication before major or route in children).
and convulsions, especially in febrile children. minor surgery; sedation with amnesia for en- MIDAZOLAM Basal sedation in diagnostic or surgical
Advice to patients: Maintain good oral doscopic procedures and surgery under local Therapeutic category: Benzodiazepine interventions under local anaesthesia,
hygiene habits because lack of saliva may anaesthesia; in combination with pethidine anxiolytic. by IV injection, initially 2.5 mg 5-10
increase chance of cavities. Observe caution [not included on WHO Model List], when anaes- Pharmacology: Midazolam is a new benzo- minutes before the operation; further
while driving or performing other tasks requir- thetic not available, for emergency reduction diazepine available for IV use. It is given as doses of 1 mg may be given, upto a
ing alertness, as drug may cause drowsiness, of fractures; epilepsy (section 1.7); anxiety water-soluble drug and does not damage max. total dose of 5 mg.
dizziness, or blurred vision. Notify physician if disorders (section 1.1). veins on injection. It has an elimination half- Sedation in ICU, by IV injection, load-
rash, flushing, or eye pain occurs, or if difficulty Contra-indications: Central nervous system life of 2 hours and no active metabolites. In ing dose, 0.03-0.3 mg/kg; mainte-
in urinating, constipation, or sensitivity to light depression or coma; shock; respiratory de- comparison with diazepam, it has greater nance dose, 0.03-0.2 mg/kg per hour.
becomes severe or persists. pression; acute pulmonary insufficiency; sleep amnesic properties. Induction and maintenance of an-
Nursing action: Relieve dry mouth with fre- apnoea; acute alcohol intoxication; severe Indications: Premedication before induction aesthesia, by IV injection, induction,
quent sips of water, gum, hard candy. hepatic impairment; marked neuromuscular of anaesthesia; basal sedation before diag- 10-15 mg; maintenance, according to
• Advise patient to avoid hazardous activities respiratory weakness including unstable my- nostic or surgical interventions under local individual patient’s needs.
if drowsiness occurs; to report blurred vision, asthenia gravis. anaesthesia; long-term sedation in intensive Intravenous anaesthesia in combina-
tion with ketamine, by IV continuous
124 | 3.3 Muscle relaxants and cholinesterase inhibitors 3.3.1 Muscle relaxants | 125
infusion, 0.03-0.1 mg/kg per hour; surgery to be carried out under light anaesthe- interactions: Appendix 1. blockade shown by hand grip, head lift and
with narcotics, 0.03-0.3 mg/kg per sia. They should never be given until it is certain Adverse effects: Histamine release, causing al- ability to cough.
hour. that general anaesthesia has been established lergic reactions, such as wheal and flare effects • Avoid IM injection; causes too much tissue
Ataralgesia in combination with and ventilation must be mechanically assisted at site of injection, flushing, bronchospasm irritation.
ketamine, by IM injection, Child, 0.15- until they have been completely inactivated. (anaphylactoid reactions reported); transient Dose: Adult and children over 1 month, by
0.20 mg/kg. Suxamethonium is the only widely used de- hypotension, slight increase in heart rate or IV injection, 0.3-0.6 mg/kg b.wt. pro-
POM DORMICUM® (Swipha) polarizing muscle relaxant. It produces rapid, decreased pulse rate. duces adequate relaxation for about
Injection, Midazolam HCl 5 mg per mL, in 1 mL and complete paralysis, which is very short-lasting Dose: Muscle relaxation, by IV injection, 15-35 min.
3 mL amps; 5 mg per 5 mL, in 5 mL amp.; 50 mg per in most patients and is of particular value ADULT initially 200–250 µg/kg, then Endotracheal intubation, by IV injec-
10 mL, in 10 mL amp. for laryngoscopy and intubation. Should 30–50 µg/kg as required for mainte- tion, 0.5-0.6 mg/kg b.wt.
paralysis be prolonged, ventilation must be nance; CHILD initially 125–200 µg/kg, Long surgical procedures including
POM Midazolam (Alpha)
Injection, Midazolam 1 mg, 2 mg, 5 mg per mL assisted until muscle function is fully restored. then 50 µg/kg for maintenance. cardiopulmonary bypass, initially by IV
Suxamethonium normally produces a phase I POM Alcuronium (WMF 20)
injection, 0.3-0.6 mg/kg b.wt.; then,
MORPHINE (depolarizing) neuromuscular block. After high Injection, Alcuronium chloride 5 mg/mL, 2-mL by IV infusion, 0.3-0.6 mg/kg/hour.
ampoule. Administration: Give undiluted as a bolus injec-
doses or prolonged use, the nature of the block
See under section 3.5 tion; not for IM injection, too much tissue irritation;
changes to a phase II (non-depolarizing) block; administration requires the use of infusion pump.
this phase II block (also known as dual block) ATRACURIUM
PROMETHAZINE is associated with prolonged neuromuscular Therapeutic category: Non-depolarising POM Atracurium (EDL 1.4)
Indications: Premedication prior to surgery; blockade and apnoea. neuromuscular blocking agent; Sekeletal Injection, Atracurium 10 mg per mL.
antiemetic (section 4.5). Alcuronium is a non-depolarizing muscle muscle relaxant. POM Atracurium (Alpha)
Contra-indications: Child under 1 year; im- Pharmacology: Atracurium prevents acetyl- Injection, Atracurium besilate 10 mg per mL; clear
EMDEX
relaxant with a duration of action of about 30
paired consciousness due to cerebral choline from binding to the receptors on the colourless soln in colourless transparent amps.
minutes. Its effects may be rapidly reversed 25 mg/2.5 mL – 10 x 5’s
depressants or of other origin; porphyria. after surgery by the anticholinesterase neostig- muscle end plate, thus blocking depolarization.
It is also a non–depolarizing blocker with a 50 mg/5 mL – 10 x 5’s
Precautions: Prostatic hypertrophy, urinary mine, provided atropine is given to prevent
retention; glaucoma; epilepsy; hepatic impair- excessive autonomic activity. Vecuronium, duration of action of 15 to 35 minutes. See POM HAMELN® (Alpha)
ment (Appendix 5); pregnancy (Appendix 2) a non-depolarizing muscle relaxant, has a notes above. Injection, Atracurium 10 mg per mL.
and breastfeeding (Appendix 3); interactions: shorter duration of action (20–30 minutes); it Indications: In anaesthesia to relax skeletal POM TRACRIUM® (GSK)
Appendix 1. causes minimal adverse cardiovascular effects. muscles during a wide range of surgical pro- Injection, Atracurium besylate 10 mg per mL; clear,
Adverse effects: Drowsiness (rarely para- cedures and to facilitate controlled ventilation; faintly yellow solution in 2.5 mL and 5 mL glass amps.
doxical stimulation in children); headache; REVERSAL OF BLOCK for endotracheal intubation where subsequent
anticholinergic effects such as dry mouth, Cholinesterase inhibitors, such as neostig- maintenance of muscle relaxation is required; PANCURONIUM
blurred vision, urinary retention. mine, are used at the end of an operation for maintenance of muscle relaxation during Therapeutic category: Non-depolarising Neu-
Advice to patients: Warn patient not to to reverse the muscle paralysis produced by Caesarean section following intubation with ro-muscular Blocker; Skeletal Muscle Relaxant.
perform skilled tasks, for example operating non-depolarizing blocking drugs, such as al- a rapid-onset agent such as suxamethonium. Indications: As an adjunct to general anaes-
machinery, driving, for 24 hours. curonium and vecuronium. Neostigmine must Contra-indications: Hypersensitivity to atra- thesia, to facilitate tracheal intubation and
Dose: Premedication, by mouth 1 hour before not be used with depolarizing blocking drugs, curium besylate. to provide skeletal muscle relaxation during
surgery, CHILD over 1 year 0.5–1 mg/ such as suxamethonium, since neostigmine will Precautions: Should only be administered surgery or mechanical ventilation.
kg. prolong the muscle paralysis. Neostigmine is with adequate general anaesthesia and un- Contra-indications: Hypersensitivity to
Premedication, by deep IM injection 1 also used to treat postoperative non-obstruc- der the supervision of an anaesthetist with pancuronium or any component; pre-existing
hour before surgery, ADULT 25 mg. tive urinary retention. facilities for endotracheal intubation and tachycardia.
For use of cholinesterase inhibitors in myasthe- artificial ventilation; myasthenia gravis, other Precautions: Administration is I.V. only and
POM Promethazine (WMF 1.3)
Oral liquid, Promethazine HCl 5 mg/5 mL. nia gravis, see section 20.2. neuromuscular diseases and severe electrolyte should be done by experienced clinicians.
disorders; severe cardiovascular disease (ad- Ventilation must be supported during neu-
POM Promethazine (EDL 1.3) minister slowly); should be flushed through the
Oral liquid for children, Promethazine (as HCl) 5 mg 3.3.1 Muscle relaxants romuscular blockade. Electrolyte imbalance
vein after injection and same applies to other alters blockade. Myasthenia gravis or other
per 5 mL.
ALCURONIUM agents co-administered through the same neuromuscular diseases; pre-existing pulmo-
See under section 8.1 for the proprietary preparations site; pregnancy.
Indications: Muscle relaxation during surgery. nary, hepatic or renal disease; elderly.
of Promethazine. Adverse effects: Skin flushing and transient
Contra-indications: Respiratory insufficiency Adverse effects: Increased B.P. and pulse, tach-
hypotension due to histamine release; rarely ycardia, hypertension, rash, itching, excessive
or pulmonary disease; dehydrated or severely
3.3 Muscle relaxants and bronchospasm and anaphylactoid reactions. salivation, muscle weakness, bronchospasm,
ill patients; myasthenia gravis or other neuro-
cholinesterase inhibitors Advice to patients: May be difficult to talk hypersensitivity reaction, oedema.
muscular disorders.
because of head and neck muscle blockade Nursing action: See under Suxamethonium.
3.3.1 Muscle relaxants Precautions: Renal or hepatic impairment (see
(patient should be reassured). Dose: See lit.
3.3.2 Cholinesterase inhibitor Appendices 4 and 5); possibly increase dose in
Nursing action: Assess vital signs of BP, pulse,
Muscle relaxants used in surgery are classified patient with burns; electrolyte disturbances; POM Pancuronium (EDL 1.4)
respiration and airway, until patient is fully
according to their mode of action as depo- possibly decrease dose in respiratory acidosis Injection, Pancuronium (as bromide) 2 mg per mL;
recovered. Keep airway clear.
larizing or non–depolarizing neuromuscular or hypokalemia; history of asthma; pregnancy in 2-mL amp.
• Monitor recovery from neuromuscular
blocking drugs. Their use allows abdominal (Appendix 2) and breastfeeding (Appendix 3); POM Pancuronium (Alpha)
126 | 3.3.1 Muscle relaxants 3.3.2 Cholinesterase inhibitors | 127
Injection, Pancuronium 2 mg per mL; in 2 mL amp. normal and will soon subside. doses of 5-10 mg. Initial doses may 3.3.2 Cholinesterase inhibitors
Dose: Muscle relaxation, by IM injection, be reduced to 10-15 mg, according
SUXAMETHONIUM INFANT up to 4–5 mg/kg; CHILD up to to the depth of muscle relaxation NEOSTIGMINE
Synonym: Succinylcholine 4 mg/kg; maximum 150 mg. needed. Therapeutic category: Cholinergic agent;
Therapeutic category: Cholinergic Agent; Muscle relaxation, by IV injection, Child (>1 year): Initially 300-500 mcg Antidote, Neuromuscular blocking agent;
Depolarising Neuromuscular Blocker; Skeletal ADULT and CHILD 1 mg/kg, followed per kg, then 60-100 mcg per kg as Diagnostic agent, Myasthenia gravis.
Muscle Relaxant. if necessary by supplements of 0.5–1 required. Indications: Counteract effect of non-depo-
Indications: Brief muscular paralysis during mg/kg at 5–10 minute intervals; Premature infant and neonate, 200- larizing muscle relaxants administered during
endotracheal intubation, endoscopy and INFANT 2 mg/kg. 250 mcg per kg, then 40-50 mcg per surgery; postoperative non-obstructive urinary
electroconvulsive therapy. Muscle relaxation (prolonged proce- kg as required. retention; myasthenia gravis (section 2.4.2).
Contra-indications: Inability to maintain clear dures), by IV infusion, ADULT 2.5–4 Elderly: Same initial doses as for adult Contra-indications: Recent intestinal or
airway; personal or family history of malignant mg/minute of solution containing but the maintenance doses should be bladder surgery; mechanical intestinal or uri-
hyperthermia; neurological disease involving 1–2 mg/mL; maximum 500 mg/hour; reduced and intervals between them nary tract obstruction; after suxamethonium;
acute wasting of major muscle, prolonged child reduce infusion rate according increased. pneumonia; peritonitis.
immobilization (risk of hyperkalaemia); per- to body weight. Administration – May also be given IM; admin- Precautions: Asthma; urinary tract infections;
sonal or family history of congenital myotonic POM Suxamethonium (WMF 20)
ister IV undiluted over 60-90 seconds and flush CVD, including arrhythmias (especially brady-
disease; Duchenne muscular dystrophy; Injection, (Solution for injection), Suxamethonium IV cannula with NS or D5W. cardia or AV block); vagotonia; hypotension;
myasthenia gravis; glaucoma, ocular surgery; chloride 50 mg/mL; in 2-mL ampoule. POM Tubocurarine (Alpha) peptic ulcer; epilepsy; parkinsonism; hyper-
liver disease; burns; low plasma cholinester- Injection (Powder for solution for injection), Suxame- Injection, Tubocurarine 10 mg per mL. thyroidism; avoid before halothane adminis-
ase activity (including severe liver disease); thonium chloride. tration has been stopped; maintain adequate
NOTE: Powder formulation recommended; POM Tubocurarine (GSK)
hyperkalaemia. ventilation (respiratory acidosis predisposes
EMDEX
Injection, Tubocurarine chloride 10 mg per mL; clear
Precautions: Digitalis toxicity or recent digital- liquid requires refrigerated storage. to arrhythmias); renal impairment (Appendix
colourless, or faintly coloured sterile solution.
ization; cardiac, respiratory or neuromuscular POM Suxamethonium (EDL 1.4) 4); pregnancy and breastfeeding (Appendices
disease; paraplegia, spinal cord inury, or severe Injection, Suxamethonium (as chloride) 50 mg per VECURONIUM 2 and 3); interactions: Appendix 1.
trauma; severe sepsis (risk of hyperkalaemia); mL; solution for injection in 2-mL amp. Adverse effects: Increased salivation and
Indications: Muscle relaxation during surgery.
prolonged apnoea on repeated injection (in- Injection, Suxamethonium (as chloride); powder for bronchial secretions, nausea and vomiting,
injection in vial. Contra-indications: Respiratory insufficiency
fusion preferred for long surgical procedures); abdominal cramps, diarrhoea; allergic reac-
or pulmonary disease; dehydrated or severely
hepatic impairment (Appendix 5); renal im- POM Suxamethonium (Alpha) tions, hypotension.
ill patients; myasthenia gravis or other neuro-
pairment; pregnancy (Appendix 2); children; Injection, Suxamethonium 50 mg per mL; 2 mL amp. Dose: Reversal of non-depolarizing block, by
muscular disorders.
interactions: Appendix 1. intravenous injection over 1 minute,
Precautions: Renal impairment (Appendix 4);
Adverse effects: Postoperative muscle pain, TUBOCURARINE ADULT 2.5 mg, followed if necessary
hepatic impairment; possibly increase dose in
particularly in patients ambulant after opera- Therapeutic category: Non-depolarising Neu- by supplements of 500 µg to maxi-
patient with burns; electrolyte disturbances;
tion, and more common in females; myoglo- romuscular blocker; Skeletal muscle relaxant. mum total dose of 5 mg; CHILD 40
possibly decrease dose in respiratory acidosis
binuria; myoglobinaemia; prolonged apnoea; Pharmacology: Tubocurarine prevents acetyl- µg/kg (titrated using peripheral nerve
or hypokalemia; history of asthma; severe
increased intra-ocular pressure; hyperkalae- choline from binding to the receptors on the stimulator).
obesity (maintenance of adequate airway and
mia; bradycardia, hypotension, arrhythmias, muscle end plate, thus blocking depolarization. Note: To reduce muscarinic effects atropine sulfate
ventilation support); pregnancy and breast-
particularly with halothane (however, with See notes above. by intravenous injection (ADULT 0.6–1.2 mg, CHILD
feeding (Appendices 2 and 3); interactions: 20 µg/kg) with or before neostigmine.
repeated doses tachycardia, hypertension); Indications: Non-depolarising muscle relaxant Appendix 1. Postoperative urinary retention, by
increased salivary, bronchial and gastric se- of medium to long duration mainly indicated as Adverse effects: Minimal release of histamine SC or IM injection, ADULT 500 µg
cretions; transient rise in intragastric pressure; an adjunct to anaesthesia to secure muscular (rarely hypersensitivity reactions including (catheterization required if urine not
hypersensitivity reactions including flushing, relaxation in surgery and obstetrics. bronchospasm, hypotension, tachycardia, passed within 1 hour).
rash, urticaria, bronchospasm, and shock (more Contra-indications: Respiratory insufficiency, oedema, erythema, pruritus).
common in women, in history of allergy, or in renal or hepatic impairment, hypersensitivity POM Neostigmine (WMF 20)
Dose: Intubation, by IV injection, ADULT and
asthmatics); rarely, malignant hyperthermia to curare–like drugs, asthma. Injection, Neostigmine metilsulfate 500 µg/mL, in
CHILD over 5 months, 80–100 µg/kg;
(often fatal). Precautions: Myasthenia gravis or myasthenic 1-mL ampoule; 2.5 mg/mL, in 1-mL ampoule.
maintenance of relaxation 20–30 µg/
Nursing action: Monitor vital signs of BP, pulse, syndrome; gross obesity, myopathy and POM Neostigmine (EDL 1.4)
kg; CHILD under 4 months, initially
respiration, until patient is fully recovered. after poliomyelitis (reduce dose); endocrine Injection, Neostigmine (as methylsulfate) 2.5 mg per
10–20 µg/kg, followed by increments
• Keep airway clear and make the emergency dysfunction; patients with family history of mL; in 1-mL amp.
according to response.
equipment available. hyperpyrexia and drug reactions; hypokalae- Muscle relaxation, by IV infusion, POM Neostigmine Methysulphate (Alpha)
• Check strength of patient’s hand grip as he mia; pregnancy and lactation. ADULT , initial bolus 40–100 µg/kg Injection, Neostigmine methylsulphate 2.5 mg in 1
recovers from anaesthesia; drug is given by Adverse effects: Transient hypotension, mL; clear colourless solution.
then 0.8–1.4 µg/kg/minute.
slowl IV over 1-2 minutes only by qualified profound muscle relaxation with prolonged Pack: 10 amps
person, usually an anaesthesiologist, who will POM Vecuronium (WMF 20)
apnoea, circulatory depression, ganglionic POM PROSTIGMIN® (Swipha)
determine neuromuscular blockade. Injection, (Powder for solution for injection), Vecuro-
block, histamine release. nium chloride, 10-mg vial. Injection, Neostigmine (as sulfate) 0.5 mg per mL.
• Provide reassurance if communication is Nursing action: See under Suxamethonium.
difficult during recovery from neuromuscular Dose: By IV injection, initially 15-30 mg; may POM Vercuronium (Alpha)
blockade. be maintained by supplementary Injection, Vercuronium; powder for injection.
• Reassure him that post-operative stiffness is
128 | 3.4 Local anaesthetics 3.4 Local anaesthetics | 129
3.4 Local anaesthetics bupivacaine 0.5% in glucose can be used but 0.25–0.5% solution, ADULT (female) Adverse effects: With excessive dosage or
Drugs used for conduction anaesthesia (also the latter is often chosen because of its longer up to 60 mg (maximum 12 mL) following intravascular injection, light-head-
termed local or regional anaesthesia) act by duration of action. Caudal block in surgery, using edness, dizziness, blurred vision, restlessness,
causing a reversible block to conduction along 0.25–0.5% solution, ADULT up to 150 tremors and, occasionally, convulsions rapidly
BUPIVACAINE mg (maximum 30 mL). followed by drowsiness, unconsciousness and
nerve fibres. Local anaesthetics are used very
widely in dental practice, for brief and super- Indications: Infiltration anaesthesia; periph- Caudal block in labour, using respiratory failure; cardiovascular toxicity
eral and sympathetic nerve block; spinal 0.25–0.5% solution, ADULT (female) includes hypotension, heart block and cardiac
ficial interventions, for obstetric procedures,
and for specialized techniques of regional anaesthesia; postoperative pain relief. up to 100 mg (maximum 20 mL). arrest; hypersensitivity and allergic reactions
Contra-indications: Adjacent skin infection, Note: Use lower doses for debilitated or elderly, or also occur; epidural anaesthesia occasionally
anaesthesia calling for highly developed skills. in epilepsy, or acute illness Do not use solutions
Where patient cooperation is required the inflamed skin; concomitant anticoagulant complicated by urinary retention, faecal
containing preservatives for spinal, epidural, caudal, incontinence, headache, backache or loss of
patient must be psychologically prepared to therapy; severe anaemia or heart disease;
or IV regional anaesthesia.
accept the proposed procedure. Facilities and spinal or epidural anaesthesia in dehydrated perineal sensation; transient paraesthesia and
equipment for resuscitation should be readily or hypovolaemic patient. POM Bupivacaine (WMF 1.2) paraplegia very rare.
Precautions: Respiratory impairment; hepatic Injection, Bupivacaine HCl 0.25%, 0.5%; in vials. Advice to patients: Advise patient of possible
available at all times. Local anaesthetic injec- Injection for spinal anaesthesia, Bupivacaine HCl
tions should be given slowly in order to detect impairment (Appendix 5); epilepsy; porphyria; temporary loss of sensation and motor activity
0.5% in 4 mL ampoule to be mixed with 7.5% following epidural or spinal anaesthesia. See
inadvertent intravascular injection. myasthenia gravis; pregnancy (Appendix 2)
glucose solution.
and breastfeeding (Appendix 3); interactions: also under Bupivacaine.
LOCAL INFILTRATION: Appendix 1. POM Bupivacaine (EDL 1.2) Nursing action: See under Bupivacaine.
Many simple surgical procedures that neither Adverse effects: With excessive dosage or Injection, Bupivacaine (as HCl) 0.25%, 0.5% with Dose: Plain Solutions
involve the body cavities nor require muscle Epinephrine (Adrenaline) 1 in 200,000; in 10-mL amp. Local infiltration and peripheral nerve
following intravascular injection, light-head-
relaxation can be performed under local infil- edness, dizziness, blurred vision, restlessness, POM ALCAINE® Plain (Alpha) block, using 0.5% solution, ADULT up
EMDEX
tration anaesthesia. Lower-segment caesarean tremors and, occasionally, convulsions rapidly Injection, Bupivacaine HCl 0.25%, 0.5%; in 20 mL to 250 mg (up to 50 mL).
section can also be performed under local followed by drowsiness, unconsciousness amps. Local infiltration and peripheral nerve
infiltration anaesthesia. The local anaesthetic and respiratory failure; cardiovascular toxity POM ALCAINE® Heavy (Alpha) block, using 1% solution, ADULT up to
drug of choice is lidocaine 0.5% with or with- includes hypotension, heart block and cardiac Injection, Bupivacaine HCl 0.5%, Glucose 7.5%; in 250 mg (up to 25 mL).
out epinephrine. No more than 4 mg/kg of arrest; hypersensitivity and allergic reactions 10 mL amp. Surface anaesthesia of pharynx, larynx,
plain lidocaine or 7 mg/kg of lidocaine with also occur; epidural anaesthesia occasionally trachea, using 4% solution, ADULT
POM DURACAIN® Plain (Alpha)
epinephrine should be administered on any complicated by urinary retention, faecal Injection, Bupivacaine HCI 0.5% per 20 mL 40–200 mg (1–5 mL).
one occasion. The addition of epinephrine incontinence, headache, backache or loss of Pack: 10’s (in vials) Surface anaesthesia of urethra, using
(adrenaline) diminishes local blood flow, slows perineal sensation; transient paraesthesia and 4% solution, ADULT 400 mg (10 mL).
POM DURACAINE® Heavy (Alpha) Spinal anaesthesia, using 5% solution
the rate of absorption of the local anaesthetic, paraplegia very rare. Injection, Bupivacaine HCI 21.12 mg per 4 mL
and prolongs its effect. Care is necessary when Advice to patient: Do not chew food in (with glucose 7.5%), ADULT 50–75 mg
Pack: 10’s (in ampoules)
using epinephrine for this purpose since, in anaesthetised region to prevent traumatizing (1–1.5 mL).
excess, it may produce ischaemic necrosis. tongue, lip, or buccal mucosa. LIDOCAINE Solutions containing epinephrine
It should not be added to injections used in Nursing action: Monitor BP, pulse, respiration Local infiltration and peripheral nerve
Synonym: Lignocaine.
digits or appendages. during treatment; if used as local anaesthetic block, using 0.5% solution with
Therapeutic category: Local Anaesthetic;
SURFACE ANAESTHESIA: in labour, fetal heart rate should be monitored. epinephrine, ADULT up to 400 mg (up
Antiarr-hythmic Agent.
• Check solution for particles. to 80 mL).
Topical preparations of lidocaine are available Indications: Surface anaesthesia of mucous
• For epidural block, test dose should be given Local infiltration and peripheral
and topical eye drop solutions of tetracaine membranes; infiltration anaesthesia; periph-
to verify needle or catheter placement. nerve block, using 1% solution with
(section 13.5) are used for local anaesthesia of eral and sympathetic nerve block; dental
Administration should be done only by ex- epinephrine, ADULT up to 400 mg (up
the cornea and conjunctiva. anaesthesia; spinal anaesthesia; IV regional
perienced clinicians. to 40 mL).
anaesthesia; arrhythmias (section 5.4).
REGIONAL BLOCK: • Onset of anaesthesia depending on route of Dental anaesthesia, using 2% solution
Contra-indications: Adjacent skin infection,
A regional nerve block can provide safe and administration is within 4-10 minutes; dura- with epinephrine, ADULT 20–100 mg
inflamed skin; concomitant anticoagulant
effective anaesthesia but its execution requires tion of action is 1.5-8.5 hours. (1–5 mL).
therapy; severe anaemia or heart disease; Note: Maximum safe doses of lidocaine for ADULT
considerable training and practice. Neverthe- • Keep resuscitative equipment and drugs
spinal or epidural anaesthesia in dehydrated and CHILD are: 0.5% or 1% lidocaine, 4 mg/kg; 0.5%
less, where the necessary skills are available, available.
or hypovolaemic patient. or 1% lidocaine + epinephrine 5 µg/mL (1 in 200
techniques such as axillary or ankle blocks Dose: Local infiltration, using 0.25% solution,
Precautions: Bradycardia, impaired cardiac 000), 7 mg/kg.
can be invaluable. Either lidocaine 1% or ADULT up to 150 mg (up to 60 mL)
conduction; severe shock; respiratory impair- Use lower doses for debilitated, or elderly, or in
bupivacaine 0.5% is suitable. Bupivacaine has Peripheral nerve block, using 0.25% epilepsy, or acute illness.
ment; renal impairment (Appendix 4); hepatic
the advantage of a longer duration of action. solution, ADULT up to 150 mg (up to Do not use solutions containing preservatives for
impairment (Appendix 5); epilepsy; porphyria;
60 mL); using 0.5% solution, ADULT spinal, epidural, caudal, or intravenous regional
SPINAL ANAESTHESIA: myasthenia gravis; avoid (or use with great
up to 150 mg (up to 30 mL). anaesthesia.
care) solutions containing epinephrine (adre-
This is one of the most useful of all anaesthetic Lumbar epidural block in surgery, using
analine) for ring block of digits or append- POM Lidocaine (WMF 1.2)
techniques and can be used widely for surgery 0.5% solution, ADULT 50–100 mg Injection, Lidocaine HCl 1%, 2%; in vial.
ages (risk of ischaemic necrosis); pregnancy
of the abdomen and the lower limbs. It is a ma- (10–20 mL). Injection for spinal anaesthesia, Lidocaine HCl 5%
jor procedure requiring considerable training Lumbar epidural block in labour, using in 2-mL ampoule to be mixed with 7.5% glucose
and practice. Either lidocaine 5% in glucose or solution.
130 | 3.5 Analgesics and opioid antagonists 3.6 Blood substitutes and solutions for correcting fluid imbalance | 131
Topical forms, Lidocaine HCl 2–4%. 3.5 Analgesics and opioid antagonists dependence. 3.6 Blood substitutes and solutions
POM Lidocaine (EDL 1.2) Opioid analgesics, such as morphine, may Dose: Premedication, by SC or IM injection 1 for correcting fluid imbalance
Injection, Lidocaine (as HCl) 1%, 2%; in vial. be used to supplement general anaesthesia, hour before surgery, ADULT 150–200 Fluid requirements must be assessed before,
Injection, Lidocaine (as HCl) 5%; for spinal anaes- usually in combination with nitrous oxide–ox- µg/kg; by IM injection 1 hour before during and after major surgery. Replacement
thesia.. surgery, CHILD 50–100 µg/kg. fluids should correspond as nearly as possible
ygen and a muscle relaxant. Repeated doses of
Injection, Lidocaine (as HCl) 1, 2% plus Epinephrine Intra-operative analgesia, by IV
intra-operative analgesics should be given with in volume and composition to those lost. Blood
(Adrenaline) 1:200,000; in vials. injection, ADULT and CHILD 100 µg/
Cream or Ointment, Lidocaine (as HCl) 2-5%. care, since respiratory depression may persist transfusion is essential to restore oxygen-car-
into the postoperative period. kg, repeated every 40–60 minutes as rying capacity when more than 15% of the
Gel or Solution, Lidocaine (as HCl) 2-4%.
required. circulating blood volume is lost but should
Spray, (Aerosol), Lidocaine (as HCl) 10%. The specific opioid antagonist naloxone will
Dental Cartridges, Lidocaine HCl 2% plus Epineph-
Postoperative analgesia, by IM injec- be avoided whenever screening for human
immediately reverse this respiratory depres- tion, ADULT 150–300 µg/kg every 4
rine (Adrenaline) 1:80,000. immunodeficiency viruses and hepatitis B
sion but the dose may need to be repeated. hours, CHILD 100–200 µg/kg; or by
POM ADRELID® (Shrezar) Other resuscitative measures must also be virus is impracticable. Isotonic sodium chloride
IV infusion ADULT 8–10 mg over 30 solution may be used for short-term volume re-
Injection, Lidocaine 2%, adrenaline 0.01 mg per available. It is important to remember that minutes, then 2–2.5 mg/hour. placement. Plasma expanders such as dextran
50 mL naloxone will also antagonize the analgesic
Pack: 1 x 25’s
effect of opioids. CD Morphine (WMF 1.5) 70 or polygeline may be useful. Provided renal
Injection , Morphine (as HCl or sulfate) 10 mg/mL, function is maintained, fluid is most simply
POM Lidocaine (Alpha) Paracetamol and nonsteroidal anti-inflam- in 1-mL ampoule. replaced by intravenous administration of
Injection, Lidocaine 1%, 2%; in 50 mL vials.
matory drugs may be useful alternatives (or sodium chloride solution (sodium chloride
CD Morphine (EDL 1.3)
POM Lidocaine (Jawa) adjuncts) for the relief of postoperative pain; Injection, Morphine (as sulfate or HCl) 10 mg, 15 mg 9 mg/mL, 0.9%) or the more physiologically
Injection, Lindocaine HCl 2% they do not affect respiration and gastrointes- per mL; in 1-mL amps. appropriate compound solution of sodium
Pack: 30 mL x 6’s tinal motility. lactate. In emergency cases, there is usually an
EMDEX
CD Morphine (Alpha)
POM LIGA® (Geneith) For further information on opioid analgesics, existing fluid deficit, which must be assessed
Injection, Morphine (as sulfate) 10 mg per mL; in
Injection, Lignocaine see section 1.8.2; for paracetamol (see section and corrected before surgery. Isotonic glu-
1 mL amp
POM Lignocain (Canopus) 1.8.1) and nonsteroidal anti-inflammatory cose/sodium chloride mixtures (most com-
OPIOID ANTAGONISTS
Injection, Lignocaine drugs (see section 2.1.1). monly glucose 4%/ sodium chloride 0.18%)
Pack: 1 x 100’s are preferred in children to avoid the danger
OPIOID ANALGESICS NALOXONE
POM Lignocaine (Zolon) of sodium overload and hypoglycaemia.
Indications: To counteract respiratory depres-
Injection,Lidocaine HCl 2% MORPHINE When fluids are administered intravenously
sion induced by opioids during anaesthesia;
Pack: 30 mL (in vials.) for more than 24 hours, potassium chloride is
Drug subject to international control under the Single opioid overdosage (see also section 19.2.3).
required to prevent potassium depletion. In
POM ZARLIDO® (Shrezar) Convention on Narcotic Drugs (1961). Precautions: Dependence on opioids; cardio-
Injection, Lidocaine HCl 2% order to avoid serious arrhythmias, especially
vascular disease.
Pack: 50 mL x 1’s (in vials) Indications: Adjunct during major surgery; in patients with impaired renal function, the
Adverse effects: Nausea and vomiting; hyper-
postoperative analgesia; pain, myocardial required dose of potassium should be de-
tension and hypotension reported; left ven-
LIDOCAINE plus EPINEPHRINE infarction, acute pulmonary oedema (section termined, whenever possible, by monitoring
tricular failure; pulmonary oedema; seizures;
Indications: Surface anaesthesia of mucous 1.8.2). plasma concentrations of potassium.
arrhythmias such as ventricular tachycardia or
membranes; infiltration anaesthesia; periph- Contra-indications: Acute respiratory de- See also sections 6.5 (Plasma substitutes) and
fibrillation, particularly in pre-existing cardiac
eral and sympathetic nerve block; dental pression; increased intracranial pressure, 6.10 (Solutions for correcting water, electrolyte,
disease.
anaesthesia; spinal anaesthesia; IV regional head injury or brain tumour; severe hepatic and acid-base disturbances).
Dose: Opioid-induced respiratory depression,
anaesthesia; arrhythmias (section 5.4). impairment (Appendix 5); adrenocortical
by IV injection, ADULT 100–200 µg,
Dose: See under Lidocaine above. insufficiency; hypothyroidism; convulsive 3.7 Others
repeated every 2–3 minutes to obtain
disorders; acute alcoholism, delirium tremens;
POM Lidocaine (WMF 1.2) required response; CHILD initially 10 VASOCONSTRICTORS
diverticulitis and other spastic conditions of
Injection, Lidocaine HCl 1%, 2% plus Epinephrine µg/kg, if no response followed by 100 The sympathetic block from spinal or epidural
colon; recent surgery on biliary tract; diarrhoea
1:200,000; in vial. µg/kg. anaesthesia may cause hypotension. Such
Dental cartridge, Lidocaine HCl 2% plus Epinephrine due to toxins.
Opioid-induced respiratory depression hypotension is managed by giving IV fluids
1:80,000; in vial. Precautions: Asthma, emphysema, or heart
at birth, by SC, IM, or IV injection, (usually prophylactically) and oxygen, and
failure secondary to chronic lung disease;
POM ADREXYL® (Pharmabase) NEONATE 10 µg/kg immediately after elevating legs and giving a pressor drug such
ability to maintain airway; if used in biliary
Injection, Lidocaine 20 mg, adrenaline (as bitartrate) delivery. as ephedrine. In addition to vasoconstriction,
0.0125 mg per mL; in a multidose vial.
colic, antispasmodic needed; renal impairment
Pack: 50 mL. (Appendix 4); pregnancy (Appendix 2); breast- POM Naloxone (WMF 1.5) ephedrine also accelerates the heart rate
feeding (Appendix 3); overdosage: section Injection (Solution for injection), Naxolone HCl 400 and can therefore counter bradycardia (but
POM LABCALIN® (Embassy) 19.2.3; interactions: Appendix 1. µg/mL, in 1-mL ampoule. atropine sulfate is used to reverse persistent
Injection, Lignocaine 2%, epinephrine; in 30 mL vial. bradycardia).
Adverse effects: Respiratory depression; ano- POM Naloxone (EDL 2.2)
POM LIGA ADR® (Geneith) rexia, nausea, vomiting, constipation; euphoria, Injection, Naloxone (as HCl) 0.4 mg per mL; in 1-mL
Injection, Lignocaine, Adrenaline dizziness, drowsiness, confusion, headache; dry amp. EPHEDRINE
mouth; spasm of urinary and biliary tract; cir- POM Naloxone (Alpha) Indications: Prevention of hypotension during
culatory depression, hypotension, bradycardia, Injection, Naloxone HCl 400 mcg; in 1 mL amp. delivery under spinal or epidural anaesthesia.
palpitations; miosis; allergic reactions; physical Precautions: Hyperthyroidism; diabetes mel-
132 | 3.7 Others
litus; ischaemic heart disease, hypertension; Dose: To prevent hypotension during delivery
angle-closure glaucoma; renal impairment under spinal anaesthesia, by slow IV
(Appendix 4); pregnancy (Appendix 2) and injection of solution containing 3 mg/
breastfeeding (Appendix 3); interactions: mL, ADULT 3–6 mg (maximum single
Appendix 1. dose 9 mg), repeated if necessary
Adverse effects: Anorexia, hypersalivation, every 3–4 minutes; max. cumulative
nausea, vomiting; tachycardia (also in fetus), dose 30 mg.
arrhythmias, anginal pain, vasoconstriction POM Ephedrine (WMF 1.2)
with hypertension, vasodilation with hypoten- Injection, Ephedrine HCl 30 mg/mL, in 1-mL am-
sion; dyspnoea; headache, dizziness, anxiety, poule.
restlessness, confusion, tremor; difficulty in
POM Ephedrine (Alpha)
micturition; sweating, flushing; changes in
Injection, Ephedrine 30 mg per mL; in 1 mL amp.
blood-glucose concentration.
EMDEX
4. Drugs used in
gastrointestinal
diseases
4.1 Antacids and other antiulcer drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 134
4.1.1 Antacids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 136
4.1.2 Ulcer healing drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 141
4.2 Antispasmodic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 153
4.3 Other smooth muscle relaxants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 155
4.4 Drugs used in diarrhoea . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 156
4.4.1 Oral rehydration. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 156
4.4.2 Medicines for diarrhoea in children. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 157
4.4.3 Antimotility drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 158
4.4.4 Adsorbents and bulk-forming drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 161
EMDEX
4.4.5 Antidiarrheal microorganisms. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 162
4.5 Laxatives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 163
4.6 Antiemetic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 165
4.7 Antihaemorrhoidal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 170
4.8 Anti-inflammatory drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 171
4.9 Miscellaneous. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 173
134 | 4.1 Antacids and other antiulcer drugs 4.1 Antacids and other antiulcer drugs | 135
4.1 Antacids and other antiulcer drugs neutralizing capacity is lacking. Liquid prepa- Source: Schuster B. Gastrointestinal acid suppression drugs: GI bleeding and ulceration may occur with
rations are more effective than solids. Evidence, Tips and Pearls. RxFiles, 2014 Mar. Available NSAID use. To avoid this, the NSAID should be
4.1.1 Antacids from: www.rxfiles.ca (login required)
4.1.2 Ulcer healing drugs Aluminium – and magnesium-containing stopped but this is not always possible. A pro-
antacids (for example aluminium hydroxide, How to administer PPIs ton pump inhibitor or an H2–receptor antago-
Gastric and duodenal ulcer, or peptic ulcer nist at twice the usual dose may be considered
disease (PUD), Zollinger–Ellison Syndrome (ZE), and magnesium hydroxide), being relatively Once-daily dosing Give 30 mins before breakfast
insoluble in water, are long-acting if retained Give 30 mins before breakfast and
for protection against NSAID-associated gastric
and gastro–oesophageal reflux disease (GORD/ Twice-daily dosing and duodenal ulcers.
in the stomach. They are suitable antacids super
GERD) or heartburn are upper gastrointestinal
disorders sharing a common abnormality: too for most purposes. Magnesium-containing PEPTIC ULCER: Patients who must continue NSAID therapy
much acid and pepsin activity for the degree antacids have a laxative effect whereas alumin- after ulcer development may take high-dose
ium-containing antacids may be constipating. Peptic ulceration involves the stomach, duo- H2-receptor antagonists concomitantly, but
of local tissue resistance. Hydrolytic and denum, and lower oesophagus. General and
proteolytic digestion of the exposed mucosa Histamine2 receptor antagonists (H2RAs) de- ulcers tend to heal more slowly with H2-re-
inexpensive measures like introducing healthy ceptor antagonists if NSAIDs are continued. A
occur followed by inflammation, necrosis, and crease acid secretion by inhibiting histamine-2 life-style, stopping smoking and taking antacids
ulceration. receptors on gastric parietal cells. Gastric proton-pump inhibitor such as omeprazole
can promote healing, but relapse is common. is more effective but it is also more expensive.
Management options include:
pH begins to increase within 30 minutes of The possibility of malignant disease should be
• Lifestyle changes administration and the effect lasts for 6 hours. considered in all patients over the age of 40 In patients who can discontinue NSAID ther-
• Antacids Tachyphylaxis or diminution of the response years who are suspected of having an ulcer. apy after ulcer development, treatment with
• Histamine2-receptor antagonists (H2RAs) after prolonged use is a drawback to chronic an H2-receptor antagonist is effective, but a
• Proton Pump Inhibitors (PPIs) use. May be useful for uncomplicated GORD/ Gastric and duodenal ulcers are healed by 4–8 treatment period of up to 8 weeks may be
• Prokinetic agents GERD; best given 30 minutes before meal. weeks treatment with H2-receptor antagonists necessary. A proton pump inhibitor usually
but there is a high rate of relapse (greater than produces the most rapid healing. After healing,
Lifestyle changes recommended include: Treatment of undiagnosed dyspepsia with 70% over 2 years) requiring maintenance
EMDEX
• Avoid large meals (small frequent feeding rec- H2-receptor antagonists may be acceptable continued prophylaxis is required.
ommended) therapy. Relapses can be prevented very
in younger patients but care is required in successfully by eradicating Helicobacter pylori Prevention of NSAID-associated ulcers
• Limit foods and drinks that tend to trigger
older people because their symptoms may be which is causally associated with most peptic Moderate GI
symptoms such as spicy foods, citrus juices,car- Low GI Risk High GI Risk
bonated beverages, alcohol, caffeine, chocolate, caused by gastric cancer. ulcers (except those related to NSAID use).
Risk
Alternate
NSAID
peppermint, etc H2-receptor antagonists therapy can promote Eradication of H. pylori reduces the relapse Low CV Risk NSAID alone + PPI or
therapy OR
• Avoid eating or drinking within 2 hours prior to COXIB + PPI or
healing of NSAID-associated ulcers (particularly rate to about 4–8%. This is undoubtedly Misoprostol
Misoprostol
bedtime duodenal). Treatment also reduces the risk of costeffective compared to the alternatives of High CV Avoid NSAIDs.
• Smoking cessation Naproxen Naproxen
acid aspiration in obstetric patients at delivery long-term maintenance therapy with low-dose Risk (Low
+ PPI or + PPI or
Alternate
• Head of bed elevation (not with pillows) dose ASA therapy OR
• Chewing gum stimulates secretion of bicarbonate
(Mendelson syndrome). H2-receptor antagonists or repeated treatment required)
Misoprostol Misoprostol
COXIBs
containing saliva which can have neutralizing Proton pump inhibitors (PPIs) inhibit acid of recurrent ulcers. It is recommended that Note: For patients with hx of ulcers, consider H. pylori testing
the presence of H. pylori is confirmed before and eradication prior to NSAID therapy. See below for the
effect on gastric acid. secretion by blocking Na +–K +-ATPase, the classifications of risks of NSAID GI toxicity.
final common pathway of parietal cell acid starting eradication treatment, particularly High GI Risk:
Antacids can provide quick but brief sympto-
secretion, often called the proton pump. PPIs for gastric ulcers. The urea breath test is used • Hx of previous complicated ulcer
matic relief. They work by neutralizing gastric • More than 2 risk factors (see below)
have greater efficacy than H2RAs and unlike widely to test for H. pylori, but false negative
pH and thereby decreasing the exposure of the Moderate GI Risk (i.e., 1-2 risk factors)
H2RAs, the effect of PPIs does not diminish results may occur if used soon after proton • Age >65 years
esophageal mucosa to gastric acidity during • High dose NSAID
with chronic use. They are usually administered pump inhibitors or antibacterials. Eradication
episodes of reflux. May be useful for on demand • History of uncomplicated ulcer
once daily, 30 minutes before breakfast. When regimens are based on a combination of • Concurrent ASA (including low dose), corticosteroids, or
relief but prolonged use should be avoided
BID dosing is indicated, the second dose has to an acid-reducing (‘antisecretory’) drug and anticoagulants.
due to potential adverse effects. For instance, Low GI Risk
be taken 30 minutes before supper. Bioavaila- antibacterials. • No risk factors
increased plasma levels of Aluminum in infants
can cause osteopaenia, microcytic anaemia bility of PPIs is decreased if they are not taken The following model eradication regimen Source: Schuster B, Regier L, Jensen B. Oral acid suppression:
comparison chart. RxFiles, 2014 May. Available from: www.
and neurotoxicity. before meals. is suggested on the basis of its efficacy and rxfiles.ca (login required).
There may be potential risk with long term use simplicity (only doses suitable for adults are DYSPEPSIA:
Antacids are often used to relieve symptoms in
of PPIs. For instance, hypochlorhydria (i.e., acid shown):
ulcer dyspepsia and in non-erosive gastro-oe- Dyspepsia covers pain, fullness, early satiety,
suppression associated with H2RAs or PPIs) may omeprazole 40 mg daily for 1 week
sophageal reflux; they are also sometimes used bloating, and nausea. It can occur with gastric
increase rates of community-acquired pneu- plus
in functional (non-ulcer) dyspepsia but the evi- and duodenal ulceration and gastric cancer
monia in adults and children, gastroenteritis metronidazole 400 mg three times daily
dence of benefit is uncertain. Antacids are best but most commonly it is of uncertain origin.
in children, and candidemia and necrotizing for 1 week
given when symptoms occur or are expected,
enterocolitis in preterm infants. plus Patients with non-ulcer dyspepsia should be
usually between meals and at bedtime, 4 or
amoxicillin 500 mg three times daily for advised to avoid smoking, alcohol and aggra-
more times daily; additional doses may be re- Standard doses of PPIs
1 week vating foods, and to eat small regular meals
quired up to once an hour. Conventional doses PPIs are equally effective at standard doses (see below);
to aid digestion. Non-ulcer dyspepsia tends to
for example 10 mL 3 or 4 times daily of liquid there may be slight variation in patient response. The decision on choosing an eradication regimen
Omeprazole, Rabeprazole & be self-limiting but antacids and H2-receptor
magnesium–aluminium antacids promote 20 mg OD for a particular country should take into account
Esomeprazole antagonists are often used to suppress gas-
ulcer healing, but less well than antisecretory Lansoprazole 30 mg OD
local resistance to antibacterials, cost and availa-
tric acid; Helicobacter pylori eradication does
drugs (such as an H2-receptor antagonist); Pantoprazole 40 mg OD bility of the necessary drugs.
not improve symptoms in cases of non-ulcer
proof of a relationship between healing and NSAID-ASSOCIATED ULCERS: dyspepsia. Prompt investigation is important
136 | 4.1.1 Antacids 4.1.1 Antacids | 137
in the presence of severe symptoms such as phosphate diet or prolonged therapy); hyper- systematically with magnesium posing a risk OTC ALMAC® (Hovid)
bleeding, dysphagia, or weight loss. aluminaemia—resulting in osteomalacia, en- to patients with renal failure. It is excreted in Tablet, (Chewable), Magnesium trisilicate 250 mg,
cephalopathy, dementia, microcytic anaemia faeces, some Alminium and Magnesium may dried aluminium hydroxide 125 mg, simeticone
GASTRO-OESOPHAGEAL REFLUX DISEASE 30 mg; white scored tab. with peppermint flavour.
(GORD/GERD): (in chronic renal failure treated with aluminium also be excreted in breast milk. Simethicone is
Pack: 10 x 10 (blister).
hydroxide as phosphate-binding agent). an antifoam/antigas agent. It acts by lowering
Gastro-oesophageal reflux disease (includ- Suspension, Magnesium hydroxide 200 mg, alumin-
Nursing action: surface tension and when administered by ium hydroxide 200 mg, simeticone 30 mg per 5 mL;
ing non-erosive gastro-oesophageal reflux • Administer after shaking liquid. Dose should be mouth, causes bubbles of gas in the GIT to white opaque suspension with peppermint flavour.
and erosive oesophagitis) is associated with followed by water. Tablets should be thoroughly coalesce thus aiding their dispersion. It is Pack: 100 mL.
symptoms which include heartburn, acid chewed before swallowing with water. excreted in the faeces. Dose: Adult, 1-2 tabs to be chewed after or between
regurgitation, and sometimes difficulty in • May increase fluid, bulk in diet to prevent con-
Indications: Symptomatic relief of: GI disorders meals and at bedtime OR 10-20 mL suspen-
swallowing (dysphagia); oesophageal inflam- stipation sion 4 times daily to be taken 20 mins to 1
• Advise patient not to take oral drugs within 1-2
associated with hyperacidity such as peptic
mation (oesophagitis), ulceration, and stricture ulcer, dyspepsia, gastro-esophageal reflux hour after meals and at bedtime.
formation may occur and there is an associa- hours of taking an antacid; may impair absorption
of other drugs. disease, gastritis; Pyrosis and heartburn in preg- OTC ANTACIDIN® (Embassy)
tion with asthma. nancy; Flatulence and abdominal discomfort Suspension, Aluminium hydroxide paste equiv. to
• Patient should notify the physician if relief is not
The management of gastro-oesophageal re- obtained or if there are any signs to suggest bleed- due to excess GI gas. Dried aluminium hydroxide 300 mg, Magnesium
flux disease includes drug treatment, lifestyle ing from the GIT. Contra-indications: Known hypersensitivity to hydroxide paste equiv. to Magnesium hydroxide
changes and, in some cases, surgery. Initial • Laxative or stool softener may be given if consti- any of its constituents; Colostomy or ileostomy; 150 mg, Simethicone 125 mg, Oxethazaine 10 mg
pation becomes troublesome; may alternate with per 5 mL
treatment is guided by the severity of symp- Renal failure or impairment; Appendicitis or
magnesuim-containing antacids (if patient does Pack: 100 mL; 200 mL.
toms and treatment is then adjusted according undiagnosed rectal and gastrointestinal bleed- Dose: 5-10 mL to be taken as required.
not have renal disease).
to response. • May rupture enteric-coated tablet causing prema- ing; Ulcerative colitis, chronic diarrhea; Gastric
outlet obstruction OTC AVROCID® (Avro)
For mild symptoms of gastro-oesophageal ture release of drugs into the stomach; separate
EMDEX
Precautions: Patients with decreased GI mo- Suspension, Activated methylpolysiloxane 125 mg,
reflux disease, initial management may include doses by 1 hour.
magnesium hydroxide 100 mg, dried aluminium hy-
the use of antacids. H2-receptor antagonists Dose: Dyspepsia, gastro-oesophageal reflux, tility; kidney disease.
droxide gel 468.1 mg per 5 ml; pleasantly flavoured.
suppress acid secretion and they may relieve by mouth, ADULT 1–2 tablets chewed Interactions: May inhibit the absorption of Pack: 200 ml
symptoms and permit reduction in antacid 4 times daily and at bedtime or 5–10 phenothiazine (especially chlorpromazine);
May decrease the absorption of quinolones, OTC DISOGEL® (PharmacyPlus)
consumption. For refractory cases and in mL suspension 4 times daily between
Chewable tablet, Deglycyrrhizinated liquorice equiv.
patients with severe symptoms or proven meals and at bedtime; CHILD 6–12 tetracycline, chenodiol, antimuscarinics, cou-
to Liquorice 400 mg, dried Aluminium hydroxide
or severe pathology, for example Barrett oe- years 5 mL up to three times daily. marin, diazepam, chlordiazepoxide, vitamin gel 250 mg, Magnesium hydroxide 250 mg, Sime-
sophagus, a short-course of a proton-pump Hyperphosphataemia, by mouth, A, isoniazid, digoxin and phosphates thereby thicone 40 mg.
inhibitor is needed initially. ADULT 2–10 g daily in divided doses lessening their effectiveness; May increase Pack: 15 x 10’s
with meals. levodopa absorption, increasing the risk of Suspension, Deglycyrrhizinated liquorice equiv. to
ZOLLINGER–ELLISON SYNDROME: toxicity; May cause premature release of en- Liquorice 400 mg, Aluminium hydroxide gel paste
Administration: Do not take other medicines within
Management of Zollinger–Ellison syndrome 2–4 hours of aluminium hydroxide preparations. May teric-coated drugs. equiv. to dried Aluminium hydroxide 250 mg,
requires high dose H2-receptor antagonist be taken with water to reduce constipating adverse Adverse effects: Mild diarrhea, constipation, Magnesium hydroxide paste equiv. to Magnesium
treatment. The proton pump inhibitors are more effects. Tablets should be swallowed wholw without fatigue and very rarely weight loss. hydroxide 250 mg, Simethicone 40 mg.
effective particularly for cases resistant to other sucking, chewing or breaking. Pack: 175 mL
Nursing action: See under Aluminum Hy-
treatment but they are more expensive. OTC Aluminium Hydroxide (WMF 17.1) droxide. OTC GASCOL® (Fidson)
Tablet, Aluminium hydroxide 500 mg. Dose: Peptic ulcer, 2 to 4 tabs to be repeated Suspension, Magaldrate 540 mg, Simethicone 100
4.1.1 Antacids Oral liquid, Aluminium hydroxide 320 mg/5 mL. if necessary. Gastric hyperacidity, 1 to mg per 5 mL.
2 tabs between meals or as required. Pack: 150 mL.
OTC Aluminium Hydroxide (EDL 20.1) Advice to patients: Take with a small amount of
ALUMINIUM HYDROXIDE Tablet, (chewable), Aluminium hydroxide 500 mg Heartburn of Pregnancy, 1 to 2 tabs
water or fruit juice; take 1-2 hours apart from other
Indications: Ulcer and non-ulcer dyspepsia; Mixture, Aluminium hydroxide mixture B.P. before breakfast and between meals oral medications.
gastro-oesophageal reflux; hyperphos-pha- OTC NEUTRACID® (Afrab-Chem) or as required. Dose: 5-10 mL between meals and at bedtime; not
taemia Tablet, Aluminium hydroxide 500 mg; white scored To be chewed and swallowed with exceeding 90 mL in a 24-hour period.
Contra-indications: hypophosphataemia; un- tab. marked afrab. water or milk.
OTC GG CID® (Geneith)
diagnosed gastrointestinal or rectal bleeding; See also under the proprietary prepara-
Suspension, Aluminium hydroxide 200 mg, magne-
appendicitis; porphyria. ALUMINIUM HYDROXIDE plus tions below. sium hydroxide 200 mg, simethicone 50 mg.
Precautions: Impaired renal function and MAGNESIUM HYDROXIDE (WITH
OR WITHOUT SIMETICONE) OTC ACIGUARD® (Unique) Pack: 200 mL
renal dialysis (Appendix 4); hepatic impair- Suspension, Dried aluminium hydroxide 300 mg,
Synonym: Magaldrate plus Activated Dimet- OTC LOCID® (Interpharma)
ment (Appendix 5); constipation; dehydration; Magnesium hydroxide 100 mg, Magensium trisili-
icone. Suspension, Dried aluminium hydroxide 325 mg
fluid restriction; GI disorders associated with cate 150 mg, Simeticone 25 mg per 5 mL. eqiuv. to Alumimium HCl 248.62 mg, magnesium
Therapeutic category: Antacid, antigas agent. Dose: Adult, 10-20 mL 3-4 times daily after meals.
decreased bowel motility or obstruction; in- hydroxide 100 mg, activated polymethylsiloxane
Pharmacology: Magaldrate is a combination Child: 5-10 mL 3-4 times daily after meals.
teractions: Appendix 1. 125 mg.
of Aluminium and Magnesium hydroxides
Adverse effects: Constipation; intestinal ob- OTC ACTAL® (GSK) Pack: 200 mL.
and sulphates. Simethicone, an antigas, is
struction (large doses); hypo-phosphataemia Tablet, Aluminium hydroxide 200 mg, magnesium OTC MAALOX® (Sanofi-Aventis)
activated dimethylpolysiloxane. Magaldrate as
with increased bone resorption, hypercalciuria hydroxide 150 mg; white tab. marked ‘ACTAL’. Suspension, Aluminium HCl, Magnesium HCl
an antacid neutralizes hydrochloric acid in the Pack: 20; 400.
and risk of osteomalacia (patients on low Pack: 150 mL; 350 mL.
gastic secretions. Magaldrate may be absorbed
138 | 4.1.1 Antacids 4.1.1 Antacids | 139
Tablet, Aluminium HCl, Magnesium HCl 2.5 mL twice daily. OTC SIMELOX® (Neros) Pack: 100 mL; 200 mL.
Pack: 10’s; 50’s (in blisters) Doses to be taken 15 mins after meals. Tablet, Dry aluminum hydroxide gel 400 mg, Magne-
sium hydroxide 400 mg, Simethicone 40 mg. MAGNESIUM TRISILICATE plus
OTC MAALOX® Plus (Sanofi-Aventis) OTC POLYCROL® Forte (Swipha) ALUMINIUM HYDROXIDE
Pack: 10 x 8’s.
Tablet, Aluminium HCl, Magnesium HCl, Sime- Tablet, Aluminium hydroxide gel (dried) 400 mg,
thicone. magnesium hydroxide 200 mg, activated me- OTC STOMACID® (Pharmgate) Indications: Gastric hyperacidity, indigestion,
Pack: Blisters 10’s; 50’s thyl-polysiloxane 25 mg. Suspension, Dried aluminium hydroxide gel 200 heartburn.
Suspension, Aluminium HCl, Magnesium HCl, Pack: 10. mg, magnesium trisilicate 200 mg, magnesium Advice to patients: Dose should be followed
Simethicone Dose: Adult, One tablet; Child (6-12 years), ½ a tablet. hydroxide 100 mg, sodium alginate 100 mg, sim- with water. Tablets should be thoroughly
Pack: 150 mL; 350 mL. To be chewed after meals and at bedtime. ethicone 25 mg. chewed before swallowing with water.
Gel, Aluminium hydroxide gel 4.75 mL, Magnesium Pack: 200 mL Nursing action: See under Aluminium Hy-
OTC MAGSIL® (Leady-pharm)
hydroxide 100 mg, Activated methylpolysiloxane droxide.
Tablet, Dried aluminium hydroxide 250 mg, magne- OTC ULGICID® (Phillips/Prisma)
125 mg per 5 mL.
sium trisilicate 500 mg; uncoated white tab. Chewable tablet, Alginic acid 200 mg, Magnesium Dose: Adult, 1-2 tabs to be chewed or sucked
Pack: 100 mL.
Pack: 2 X 10's; 500’s
Dose: 5-10 mL between meals or at bedtime
hydroxide 250 mg, Dried aluminium hydroxide after meals or as required.
Suspension, Magnesium trisilicate 250 mg, light 250 mg, Magnesium trisilicate 250 mg, Activated Child (6-12 years), half the adult dose.
magnesium carbonate 250 mg, sodium bicarbo- OTC POLYFORT® (Swipha) dimethicone 125 mg.
nate 250 mg Chewtab, Activated Methypolysiloxane 25 mg, alu- Pack: 3 x 10’s (in blisters). OTC Magnesium Trisilicate plus Aluminium
Pack: 100 mL; 190 mL; 2 L minium hydroxide 400 mg, magnesium hydroxide Suspension, Alginic acid 200 mg, Magnesium Hydroxide (EDL 20.1)
200 mg. hydroxide 250 mg, Dried aluminium hydroxide Tablet, (chewable), Magnesium trisilicate 250 mg,
OTC MAYOCID® (Crystal) Aluminium hydroxide 120 mg.
Pack: 10’s. 250 mg, Magnesium trisilicate 250 mg, Activated
Suspension, Alginic acid 200 mg, activated dime- Mixture, Aluminium hydroxide plus Magnesium
Suspension, Activated Methypolysiloxane 125 mg, dimethicone 125 mg per 15 mL.
thicone 125 mg, magnesium hydroxide 250 mg, trisilicate mixture B.P.
aluminium hydroxide 4.5 mL, magnesium hydrox- Pack: 200 mL.
magnesium trisilicate 250 mg, aluminium hydroxide
ide 100 mg. Dose: Adult, 15 mL (or 1 tablet) twice daily. OTC Magnesium Trisilicate (EDL 20.1)
250 mg.
EMDEX
Pack: 100 mL. Child, 5 mL twice daily. Tablet , (chewable), Magnesium trisilicate 500 mg
Pack: 200 mL.
OTC POLYGEL® (Shalina) OTC UNIGEL® (Sterling drugs) Mixture, Magnesium trisilicate 250 mg per 5 mL.
OTC MD-Antacid® (O’Nell)
Tablet (chewable), Dried aluminium hydroxide gel Suspension, Magaldrate 400 mg, simethicone 20 OTC ANTASIL® (Pharma–Deko)
Suspension, Dried aluminum hydroxide 250 mg,
300 mg, magnesium aluminium silicate hydrate mg per 5 mL. Tablet, Dried aluminium hydroxide gel 250 mg,
magnesium hydroxide 250 mg, dimethicone 125
50 mg, magnesium hydroxide 25 mg, simethicone Pack:100 mL; 200 mL magnesium trisilicate 500 mg.
mg per 15 mL; red susp.
25 mg; erythrosine supra coloured, peppermint Indications: Magaldrate is a common antacid drug Suspension, Dried aluminium hydroxide gel 310 mg,
Pack: 200 mL.
oil flavour. that is used for the treatment of duodenal and magnesium trisilicate 620 mg.
Dose: Adult: 15 mL; Child, 5 mL. To be taken twice
Pack: 20 x 10’s gastric ulcers and esophagitis from gastroesoph-
daily. OTC BENSIL® (Nichben)
Suspension, Simethicone 50 mg, magnesium hydrox- ageal reflux.
OTC ACDT® Zero (Mecure) ide 250 mg per 5 mL, dried aluminium hydroxide Simethicone is an oral anti-foaming agent used to Suspension, Magnesium trisilicate 250 mg, mag-
Suspension, Dried aluminium hydroxide gel 9.5 mL, gel 250 mg; erythrosine & tartrazine coloured, reduce bloating, discomfort and pain caused by nesium carbonate 250 mg, sodium bicarbonate
magnesium hydroxide 200 mg, activated polyme- mint flavour. excess gas in the stomach or intestinal tract. It is 250 mg.
thyl-siloxane 250 mg per 10 mL; slightly pink susp. Pack: 120 mL; 200 mL. a mixture of polydimethylsiloxane and silica gel. Pack: 200 mL; 2 L
Pack: 10 x 10 unit doses OTC BENTICIL® (Bentos)
OTC RELCER® (Glenmark)
Tablet, Deglycyrhizinated liquorice equiv. to liquo- MAGNESIUM HYDROXIDE Suspension, Magnesium trisilicate 250 mg, light
OTC NOMACID® (Nomagbon)
Suspension, Dimethicone 5 mg, aluminium hy- rice 4 g, dried aluminium hydroxide gel 250 mg, Therapeutic category: Antacid; Laxative. magnesium carbonate 250 mg, sodium bicarbonate
droxide 100 mg, magnesium hydroxide 250 mg, magnesium hydroxide 250 mg, simethicone 40 mg; Indications: Ulcer and non-ulcer dyspepsia; 250 mg per 5 mL.
magnesium trisilicate 250 mg per 5 mL; cream susp. uncoated tab. gastro-oesophageal reflux. Pack: 200 mL.
Pack: 200 mL glass bottle. Pack: 10’s Dose:Adult, 1-2 teaspoonful 3-4 times daily;
Contra-indications: Severe renal impairment.
Gel, Aluminium hydroxide gel 6 g, magnesium Child, 1-3 teaspoonful 3-4 times daily.
OTC NUGENE® (Synergy) Precautions: Renal impairment (Appendix
hydroxide 80 mg, simethicone 100 mg, deglycyr- OTC DANACID® (Dana)
Suspension, Alginic acid 70 mg, magnesium hy- 4); hepatic impairment (Appendix 5); interac-
rhizinated liquorice equiv. to liquorice 400 mg Tablet, Magnesium trisilicate 250 mg, dried alumin-
droxide 85 mg, dried aluminium hydroxide 85 mg, per 5 mL. tions: Appendix 1.
magnesium trisilicate 85 mg, activated dimethicone ium hydroxide 120 mg; peppermint flavour
Pack: 180 mL; 500 mL. Adverse effects: Diarrhoea; in renal impair-
50 mg per 5 mL. Pack: 12 x 8’s; 1000’s
ment—hypermagnesaemia resulting in loss of Suspension, Dried aluminium hydroxide 400 mg,
Pack: 200 mL OTC ROSIL® (Richygold)
deep tendon reflexes and respiratory depres- magnesium hydroxide 100 mg, simethicone 125
Dose: Adult, 15 mL twice daily. Suspension, Alginic acid 200 mg, magnesium hy-
droxide 250 mg, dried aluminium hydroxide 250
sion, with other symptoms including nausea, mg per 5 mL
Child: 5 mL twice daily.
mg, magnesium trisilicate 250 mg, simethicone vomiting, flushing of skin, thirst, hypotension, Pack: 200 mL
OTC POLYCAINE® (Therapeutic) 125 mg per 15 mL. drowsiness, confusion, muscle weakness,
Tablet, Oxethazaine 5 mg, magnesium carbonate 86 OTC DIGICID® (Strides Vital)
Pack: 200 mL. bradycardia, coma and cardiac arrest. Tablet, Magnesium trisilicate, Aluminium hydroxide.
mg, dried aluminium hydroxide 125 mg. Dose: Dyspepsia, gastro-oesophageal reflux,
Pack: 3 x 10’s (in blister) OTC RULOX® (SKG) Pack: 96’s.
Suspension, Dried aluminium hydroxide gel 468.1
by mouth, ADULT 5–10 mL repeated
Dose: Adult (>12 years), 2 tablets 4 times daily. OTC EMBAMAG® (Embassy)
Child (6-12 years), 2 tablets twice daily. mg, magnesium hydroxide 100 mg, activated according to patient’s needs.
Tablet, Magnesium trisilicate 250 mg, aluminum
Suspension, Oxethazaine 10 mg, magnesium methylpolysiloxane 125 mg per 5 mL; pinkish ho- OTC Magnesium Hydroxide (WMF 17.1) hydroxide 120 mg.
hydroxide 250 mg, aluminium hydroxide 250 mg, mogenous susp. Oral liquid, Magnesium hydroxide equiv. to magne- Pack: 20’s; 1000’s.
simethicone 50 mg per 5 mL. Pack: 100 mL; 200 mL in amber bottles. sium oxide 550 mg/10 mL.
Pack:100 mL; 200 mL Dose: 5-10 mL to be taken between meals and at OTC EMTRISIL® (Emzor)
Dose: Adult (>12 years), 10ml twice daily bedtime. OTC ATRACID® (Crystal) Suspension, Magnesium trisilicate 250 mg, light
Child (6-12 years), 5ml twice daily; 2-6 years, Suspension, Magnesium hydroxide, Alginic acid. magnesium carbonate 250 mg, sodium bicarbonate
140 | 4.1.1 Antacids 4.1.2 Ulcer healing drugs | 141
250 mg per 5 mL Dose: Adult, 10-20 mL 3-4 times daily. ach thereby relieving indigestion. Exerts a mild 4.1.2 Ulcer healing drugs
Pack: 180 mL; 2 L. laxative action at higher dosages. It makes urine
OTC PEPTOMAG® (Topway)
alkaline, and may help in the treatment of urinary CIMETIDINE
OTC GESTID® (Ranbaxy) Suspension, Magnesium trisilicate 250 mg, light
infections and relief associated discomfort.
Tablet, Dried aluminium hydroxide 300 mg, magne- magnesium carbonate 250 mg, sodium bicarbonate Therapeutic category: Histamine H2-receptor
sium trisilicate 50 mg, magnesium hydroxide 25 mg, 250 mg per 5 mL. OTC BONABABE® Gripe (Bond) antagonist.
activated polymethylsiloxane 10 mg. Pack: 200 mL. Mixture, Dill. oil 0.005 mL, Sodium bicarbonate 50 Indications: Duodenal ulcer, benign gastric
Pack: 5 x 4’s. Dose: To be taken 3 to 4 times daily mg, Sodium citrate 0.05 mg, Ginger tincture 0.00215
ulcer, recurrent and stomal ulceration, Oesoph-
Dose: 1-2 tabs 4 times daily; to be chewed and Adult: 15-30 mL mL per 5 mL.
swallowed after meals or as required. Child (6-12 years): 5 mL; >12 years, 5-15 mL Pack: 200 mL.
ageal reflux disease and other conditions where
Suspension, Dried aluminium hydroxide gel USP 4.75 Indications: Quick and effective relief from wind reduction of gastric acid is beneficial such as
OTC POLYCIL® (Therapeutic) persistent dyspeptic symptoms particularly
mL, magnesium hydroxide USP 100 mg, activated pains, digestive upset and flatulence.
Tablet (Chewable), Polymethylsiloxane 10 mg, alu- meal-related.
polymethylsiloxane 125 mg, carboxymethylcellulose Dose: Newborn infant, ½ teaspoonful; 1–6 months,
minium hydroxide 300 mg, magnesium trisilicate
sodium 50 mg per 5 mL. 1 teaspoonful; 6 months – 2 years, 2 tea- Contra-indication: Hypersensivity to cime-
50 mg, magnesium hydroxide 25 mg.
Pack: 100 mL; 200 mL. spoonfuls; >2 years, 2-3 teaspoonfuls. tidine.
Pack: 10 x 8’s (in blisters).
Dose: Adult, 5-10 mL 3-4 times daily after meals. Precautions: Reduce dose in renal and hepatic
OTC Grip Water (Vitabiotics)
Child (5-12 years), 5 mL after every meal. OTC POLYCIN® (Therapeutic) impairment; avoid I.V. injection in high dosage
Syrup, Dill oil 0.005 mL, sodium bicarbonate 50 mg,
Suspension, Activated polymethylsiloxane 125 mg, and in cardiovascular impairment; pregnancy,
OTC GETOSIL® (Vitahealth) fennel oil 0.0007 mL
magnesium hydroxide 100 mg, aluminium hydrox-
Chewable tablet, Dried aluminium hydroxide 300 mg, Pack: 200 mL breast feeding.
ide gel 4.70 ml per 5 mL.
magnesium trisilicate 50 mg, magnesium hydroxide Adverse effects: Diarrhoea, dizziness, rash,
Pack: 100 mL; 200 mL. OTC Infant’s Gripe water (Gauze)
25 mg, simethicone 10 mg. tiredness. Gynaecomastia, occasional re-
Oral liquid, Sodium bicarbonate 50 mg, Dill oil 0.0036
Pack: 4’s (in 50 pouches) OTC STOPACID® (Afrab-Chem) versible liver damage, confusion. Very rarely
mL per 5 mL
Tablet, Magnesium hydroxide 600 mg, aluminium
OTC JAWASIL® (Jawa) Pack: 200 mL interstitial nephritis, acute pancreatitis, throm-
EMDEX
hydroxide (dry gel) 500 mg, simethicone 32.50 mg.
Suspension, Magnesium trisilicate 300 mg, dried alu- bocytopaenia, headache, myalgia, arthralgia.
Pack: 2 x 10’s; 10 x 10’s (in blisters). OTC Liver Salt (Embassy)
minium hydroxide gel 600 mg, magnesium hydrox- Advice to patients: Take with or immediately
Dose: Adults: 1-2 tablets to be chewed 3-4 times Effervescent powder, Sodium bicarbonate 380 mg,
ide 200 mg, dimethylpolysiloxane 50 mg per 10 mL. after meals; take 1 hour before or 2 hours after
daily. Child (6-12 yrs): ½-1 tablet to be citric acid 420 mg per g; orange flavoured yellow
Pack: 100 mL; 200 mL.
chewed 3-4 times daily. powder. antacids; may cause drowsiness, impaired
Dose: Adult, 10-20 mL 3-4 times daily
Child, 5-15 mL 3-4 times daily.
Pack: 5’s (in sachets) judgement, or coordination; avoid smoking
OTC SUPERMAG® (Mopson)
Indications: Symptomatic relief of indigestion, cigarette, excessive alcohol, pepper, caffeine,
Suspension, Mist. Magnesium Trisilicate BPC.
OTC JULISIL® (Juhel) flatulence, nausea. harsh spices/high temperatures of foods.
Pack: 180 mL, 2 L.
Suspension, Magnesium trisilicate 250 mg, Light Dose: Adult, 5 g every 2-3 hours as needed; Max. 30 Nursing action: Give with meals so that the
magnesium carbonate 250 mg, Sodium bicarbonate g in 24 hours.
SODIUM BICARBONATE drug’s peak effect occurs at the proper time
250 mg per 5 mL Child: Not recommended
Pack: 200 mL. Therapeutic category: Antacid and carmin- Note: Do not take any other medication 1 to 2 hours (peak inhibition of gastric acid secretion occurs
ative. after taking this medication. at 1 and 3 hours after dosing in fasting subjects
OTC Magnesium Trisilicate (Ceenek) and approximately 2 hours in non-fasting sub-
Oral suspension, Magnesium trisilicate 250 mg, so- Indications: Symptomatic relief of wind, grip- OTC MAGCID® (Gauze)
ing pain, colic, dyspepsia. jects; this correlates well with the time food is
dium carbonate 250 mg, light magnesium carbonate Suspension, Sodium bicarbonate 250 mg, magne-
Nursing action: Patient should chew tablet be- no longer in the stomach offering a buffering
250 mg per 5 mL sium trisilicate 250 mg, light mag. carbonate 250
Pack: 200 mL fore swallowing and drink a full glass of water. mg per 5 mL. effect). If needed, give antacids 1 hr before or
• Taking antacid with milk may cause milk-al- Pack: 200 mL 1 hr after cimetidine.
OTC Magnesium Trisilicate Comp. (Emzor) • Cigarette smoking may increase gastric acid
Tablet (Chewable), Magnesium trisilicate 300 mg, kali syndrome; teach patient the symptoms OTC Mist Magnesium Trisilicate (Gauze)
namely confusion, headache, nausea, vomit- secretion and worsen disease; making the
aluminium hydroxide 250 mg. Oral Liquid, Sodium bicarbonate 250 mg, magne-
Pack: 500; 1000. ing, anorexia, urinary stones, hypercalcemia sium trisilicate 250 mg, Light Mag. Carbonate 250
drug less effective.
Mixture, Magnesium trisilicate 250 mg per mL and to avoid such combination. mg per 5 mL • Advise patient to avoid pepper, caffeine,
Pack: 180 mL. • Advise patient to report to the doctor if symp- Pack: 200 mL; 2 L alcohol, spices, very hot or cold foods that
toms persist after 2 weeks of starting therapy; seem to worsen the condition.
OTC Nomagbon Magnesium (Nomagbon) OTC Moko Bicarbonate of Soda (New Healthway)
if indigestion is accompanied by chest pain, • Inform patient that drug may cause drows-
Oral Liquid, Mag. trisilicate 500 mg, light mag. car- Powder, Sodium bicarbonate 100 g per packet.
bonate 500 mg, sodium bicarbonate 500 mg per dyspnea, diarrhea, dark, tarry stools. iness, dizziness and if affected, to avoid
OTC SODAMINT® (Juhel) activities that require alertness.
10 mL; white susp. • Patients on sodium-restricted diet should Tablet, Sodium bicarbonate 300 mg. Dose: By mouth, 400 mg twice daily at
Pack: 200 mL glass bottle avoid sodium bicarbonate containing antac- 300 mg – 1000. breakfast and bedtime or 200 mg 3
OTC Magnesium Trisilicate (Pharchem) ids unless prescribed.
Dose: New born infant, 2.5 mL; 1-6 months, 5 OTC Woodward’s Gripe Water® (SKG) times daily with meals and 400mg at
Suspension, Magnesium trisilicate 500 mg, light
magnesium carbonate 500 mg, sodium bicarbonate mL; 6 months – 2 years, 10 mL; 2 years
Oral liquid, Sodium bicarbonate 50 mg, Terpeneless bedtime (1 g/day).
dill seed oil 2.14 mg; Ginger tincture 0.368 mL per Acute treatment, 800 mg at bedtime.
500 mg, conc. peppermint emulsion 0.25 mL, d/s and above, 10-15 mL. 5 mL. Duration of therapy is 4 weeks (6
chloroform water 5 mL per 10 mL. The above doses may be repeated as Pack: 100 mL; 150 mL.
required up to 6 times daily. weeks in benign gastric ulceration).
OTC Moko Mist. Mag. Trisilicate® (New Healthway)
Suspension, Magnesium trisilicate 250 mg, light
Maintenance therapy, 400 mg at
OTC ACICARE® (JB Pharma). bedtime.
magnesium carbonate 250 mg, sodium bicarbonate Granules, Sodium bicarbonate 2.8 g, Tartaric acid
250 mg per 5 mL. Persistent acid-related dyspeptic symp-
1.33 g, Citric acid 0.82 g per 5 gm; orange flavour.
Pack: 200 mL. toms, 400 mg twice daily for 4 weeks.
Indications: Reduces the acid content of the stom-
142 | 4.1.2 Ulcer healing drugs 4.1.2 Ulcer healing drugs | 143
Oesophageal reflux disease, 400 400 mg – 1 x 20`s (in blister) in response to the decreased acid secretion. tro-esophageal reflux disease (GERD):
mg 4 times daily with meals and at POM BETAMETIDINE® (Beta Drugs) Esomeprazole is acid labile and is administered 20 mg once daily in patients without
bedtime. Tablet, Cimetidine 400 mg. orally as enteric-coated granules. Absorption of esophagitis. If symptoms control has
Zollinger-Ellison syndrome and other 400 mg – 1 x 20’s. esomeprazole is rapid, with peak plasma levels not been achieved after 4 weeks, the
hypersecretory conditions, 1.6 g or Injection, Cimetidine 200 mg per 2 mL. occurring approximately 1-2 hours after dose. patient should be further investi-
more daily in divided doses. Pack: 2 mL x 10’s. Esomeprazole is completely metabolised by gated. Once symptoms have resolved,
Note: H2-receptor blockers are now taken POM DUODIN® (L.B.S.) the cytochrome P450 system (CYP). subsequent symptom control can
in the night (nocte) for more effective ulcer Tablets, Cimetidine 200 mg, f-c tab. marked with Indications: Gastroesophageal Reflux Disease be achieved using an on demand
healing. Antacids are taken during daytime to maker’s name and logo; 400 mg, capsule-shaped (GERD): Treatment of erosive reflux esophagi- regimen taking 20 mg once daily,
neutralise acidity. tab. marked with maker’s name. tis; Long-term management of patients with when needed.
Pack: 10 x 6; 10 x 10; 500; 1000. healed esophagitis to prevent relapse; Symp- In combination with appropriate anti-
POM Cimetidine (EDL 20.7.1)
Tablets, Cimetidine 200 mg, 400 mg. POM GLOBA® (E-Globa) tomatic treatment of gastroesophageal reflux bacterial therapeutic regimens for the
Injection, Cimetidine 100 mg per mL; in 2-mL amp. Tablet, Cimetidine 200 mg. disease (GERD). In combination with appropri- eradication of Helicobacter pylori and
200 mg – 1 x 20’s. ate antibacterial therapeutic regimens for the – Healing of Helicobacter pylori associ-
POM Cimetidine (Kakaki)
eradication of Helicobacter pylori and healing ated with duodenal ulcer: 20 mg with
Tablets, Cimetidine 200 mg, 400 mg POM GMETIDINE® (Onifam)
200 mg – 60’s Tablet, Cimetidine 400 mg of Helicobacter pylori associated duodenal 1 g Amoxicillin and 500 mg Clarithro-
400 mg – 60’s 400 mg – 1 x 20’s ulcer; Prevention of relapse of peptic ulcers mycin, all twice daily for 7 days.
in patients with Helicobacter pylori associated – Prevention of relapse of peptic ulcers
POM ALTRAMET® (Taylek) POM MAITIDINE® (Pacmai)
ulcer disease. in patients with Helicobacter pylori
Tablets, Cimetidine 200 mg, 400 mg. Injection, Cimetidine 200 mg per 2 mL
Pack: 2 x 10’s (in amps)
Contra-indications: Hypersensitivity to eso- associated ulcer disease: 20 mg with 1
200 mg – 10 x 10’s.
400 mg – 5 x 10’s. meprazole, substituted benzimidazoles or any g Amoxicillin and 500 mg Clarithro-
EMDEX
POM PACIDINE® (Al-Tinez) other constituents of the formulation. mycin, all twice daily for 7 days.
Injection, Cimetidine HCl 200 mg per 2 mL.
Tablet, Cimetidine 400mg; white, oblong f-c tab. Precautions: In the presence of any alarm Children: No experience with esome-
Pack: 50’s.
400 mg – 100’s.
symptom (e.g. significant unintentional weight prazole in children
POM Apo-Cimetidine (Lahams)
POM RAJCIMETI® (Seagreen) loss, recurrent vomiting, dysphagia, haemate- Impaired renal function: Dose
Tablets, Cimetidine 200 mg, pale green, f-c tab.
Tablet, Cimetidine 400 mg; uncoated tab mesis or melaena) and when gastric ulcer is adjustment is not required in patients
marked ‘APO 200’; 400 mg, pale green, oblong f-c
400 mg – 1 x 20’s; 1 x 10’s (in blisters) suspected or present, malignancy should be with impaired renal function. Due to
tab. marked ‘APO 400’.
200 mg – 100’s; 1000’s POM TAGAMET® (GSK) excluded, as treatment with esomeprazole limited experience in patients with
400 mg – 100’s; 500’s. Tablets, Cimetidine 200 mg, pale green f-c tab.; may alleviate symptoms and delay diagnosis. severe renal insufficiency, such pa-
400 mg, pale green oblong f-c tab. Both marked Patients on long term treatment (particularly tients should be treated with caution.
POM ASTOP® (Chanmedi)
TAGAMET, SK & F and tab. strength. those treated for more than 1 year) should be Impaired hepatic function: Dose
Tablet, Cimetidine 200 mg.
200 mg – 56 kept under regular surveillance. Pregnancy adjustment is not required in patients
200 mg – 1000’s.
400 mg – 20.
and lactation. with mild to moderate liver impair-
POM CEMTAB® (Fil Pharma) Injection, Cimetidine 200 mg per 2 mL.
2 mL x 10.
Adverse effects: Headache, abdominal pain, ment. For patients with severe liver
Tablets, Cimetidine 200 mg, 400 mg; f-c tabs.
200 mg – 10 x 10’s; 500’s diarrhoea, flatulence, nausea/vomiting, con- impairment, a dose of 20 mg should
POM ULCEMET® (Pharmaplus) stipation. Less commonly Dermatitis, pruritus, be used.
400 mg – 10 x 10’s; 500’s
Tablet, Cimetidine 200 mg; f-c tab. urticaria, dizziness, dry mouth. Elderly: Dose adjustment not
POM CETILAB® (Embassy) 200 mg – 20’s
Nursing action: Administer whole, 30 mins required.
Tablets, Cimetidine 200 mg, 400 mg.
200 mg – 20’s.
POM ZICONET® (Elbe) before eating. POM ESOFAG® (Micronova)
Tablet, Cimetidine 400 mg. • Advise patient to avoid alcohol, salicylates,
400 mg – 20’s Tablets, Esomeprazole (as Magnesium trihydrate) 20
ibuprofen; may cause GI irritation. mg, 40 mg; e-c tab.
POM CETIDINE® (Medreich) ESOMEPRAZOLE • Discontinue medication and notify doctor if 20 mg – 10's
Tablet (200 mg), Cimetidine 200 mg; pale green
Therapeutic category: Gastric acid secretion patient reports severe diarrhoea. 40 mg – 10's
round f-c tab.
Tablet, (400 mg), Cimetidine 400 mg; pale green
inhibitor, PPI. Dose: The tablets should be swallowed POM ESOMEGA® (Biostadt)
oblong f-c tab. Pharmacology: Esomeprazole, the S-isomer whole with liquid. The tablets should Capsules, Esomeprazole magnesium trihydrate 20
Injection, Cimetidine 200 mg per 2 mL. of omeprazole, reduces gastric acid secretion not be chewed or crushed. mg, 40 mg; delayed-release cap.
Pack: 2 mL x 10’s. through a specific targeted mechanism of ac- Gastro-esophageal Reflux Disease 20 mg – 2 x 7`s .
tion. It is a specific inhibitor of the acid pump (GERD) 40 mg – 2 x 7`s .
POM CETIMED® (Embassy)
Tablets, Cimetidine 200 mg, 400 mg. in the parietal cell. Esomeprazole is a weak – Treatment of erosive reflux esophagi- POM ESOMEP® (Nosak)
200 mg – 20’s. base and is concentrated and converted to the tis: 40 mg once daily for 4 weeks. Tablets, Esomeprazole 20 mg, 40 mg; reddish-brown
400 mg – 20’s. active form in the highly acidic environment An additional 4 weeks treatment is e-c tabs.
of the secretory canaliculi of the parietal cell, recommended for patients in whom 20 mg – 1 x 10’s (in blister)
POM CIMETAG® (Hovid)
where it inhibits the enzyme H+K+-ATPase (the esophagitis has not healed or who 40 mg – 1 x 10’s (in blister)
Tablets, Cimetidine 200 mg, 400 mg.
200 mg – 10 x 10 (blister) acid pump) and inhibits both basal and stimu- have persistent symptoms. POM ESOZ®(Glenmark)
400 mg – 10 x 10 (blister). lated acid secretion. Food intake had no signif- – Long-term management of patients Tablet, (20 mg), Esomeprazole (as magnesium trihy-
icant influence on the effect of esomeprazole with healed esophagitis to prevent drate) 20 mg; e-c tab.
POM Cimetidine (Pharmabox)
on intragastric acidity. During treatment with relapse: 20 mg once daily. 20 mg – 10’s
Tablet, Cimetidine 400 mg.
antisecretory drugs serum gastrin increases – Symptomatic treatment of gas- Tablet, (40 mg) – Esomeprazole (as magnesium
trihydrate) 40 mg; e-c tab. POM FAMOTAB®(Hovid) or to discontinue the drug according to the swallowing the capsule, open it and swallow the
40 mg – 10’s Tablet, Famotidine 40 mg; square, light orange, importance of the drug to the mother. content immediately without chewing or crushing
f-c tab. Children: Safety and efficacy are not established the pellets. No dosage adjustment is necessary in
POM GERDRIC® (Carebliss)
40 mg – 10 x 10 (blister). in children <18 yrs. elderly or renal impairment patients. Adjust dosage
Capsule, Esomeprazole 20 mg; e-c cap
in case of severe liver impairment.
20 mg – 2 x 7’s POM FONTYNA® (Vixa) Liver impairment: Consider dosage reduction in
Tablet, Famotidine 40 mg; square, light orange severe cases of hepatic impairment. POM ENDOLAN®-30 (Embassy)
POM NEXIUM® (Reals)
f-c tab. Elderly: Doses >30 mg daily should be admin- Capsule, Lansoprazole 30 mg; e-c granules.
Tablets, Esomeprazole (as Magnesium trihydrate) 20
40 mg – 2 x 10’s (in blister). istered only if additional acid suppression is 30 mg – 10 x 10’s.
mg, light pink f-c tab. marked ‘20 mg’ on one side and
‘AEH’ on the reverse; 40 mg, pink f-c tab. marked ‘40 POM KOTIDINE® (Al-Tinez) needed. POM GLANSOPREX® (Global Healthcare)
mg’ on one side and ‘AEI’ on the reverse. Both contain Tablets, Famotidine 20 mg, blue f-c tab.; 40 mg, light Dysphagia: For patients with difficulty in swal- Capsule, Lansoprazole 30 mg; e-c granules in a cap.
esomeprazole as enteric-coated pellets (MUPS). green f-c tab. lowing, capsule can be opened and pellets can 30 mg – 4 x 7’s.
20 mg – 30’s; 1000’s be swallowed immediately, without crushing
POM NEXPRO® (Zoomota) POM LANSODEX® (Sales gates)
40 mg – 1000’s. or chewing the pellets.
Tablet, (20 mg), Esomeprazole (as magnesium) 20 Capsule, (SR), Lansoprazole 30 mg
mg; f-c tab. containing enteric-coated pellets. POM MEDILAC® (Crystal) Adverse effects: Diarrhea, nausea, abdominal 30 mg – 2 x 7’s (in blisters)
20 mg – 1 x 10’s Tablet, Famotidine 40 mg. pain, headache and skin rashes may occur.
POM LANSOGUARD® (Pharmabase)
Tablet, (40 mg), Esomeprazole (as magnesium) 40 40 mg – 10 x 10’s. Nursing action: Administer capsule whole 30 Capsule, Lansoprazole 30 mg; e-c granules in a cap.
mg; rose pink tab. containing enteric-coated pellets. min before eating for best results.
POM ULDAN® (Dana) 30 mg – 2 x 7’s.
40 mg – 1 x 10’s. • Advise patient to avoid alcohol, salicylates,
Tablet, Famotidine 20 mg; f-c tab.
POM LANSOPAL® (PharmacyPlus)
POM RACIPER® (Ranbaxy) 20 mg – 1 x 10’s’; 10 x 10’s (in blisters) ibuprofen; may cause GI irritation.
Capsule, Lansoprazole 30 mg; delayed-release e-c
Caplets, Esomeprazole magnesium 20 mg, 40 mg. • Discontinue medication and notify doctor if granules in capsule.
20 mg – 2 x 7’s. LANSOPRAZOLE patient reports severe diarrhoea. 30 mg – 28’s
EMDEX
40 mg – 2 x 7’s. Dose: Duodenal ulcer, Short term treatment,
Therapeutic category: Gastric acid secretion
15-30 mg once daily for 4 weeks; POM LANZOSIL® (Fidson)
POM ZOLERIC® (Kayhelt) inhibitor, PPI.
Capsule, Lansoprazole 30 mg; e-c granules contained
Capsules, Esomeprazole (as magnesium trihydrate) Pharmacology: Lansoprazole is a substituted Maintenance of healed duodenal
in red/white cap.
20 mg, 40 mg; e-c pellets benzimidazole proton pump inhibiotor. It ulcer, 15 mg once daily. 30 mg – 14’s.
20 mg – 2 x 7’s suppresses gastric acid secretion by the specific Eradication of H. pylori to prevent DU
40 mg – 2 x 7’s recurrence, Suggested regimens: POM LANZOTEC® (Joswe/Afrab)
inhibition of the (H+, K+) ATPase enzyme system
Triple therapy: 30 mg Lansoprazole, Capsules, Lansoprazole 15 mg, 30 mg; e-c pellets
(acid pump) at the surface of gastric parietal
FAMOTIDINE 1 g Amoxicillin and 500 mg clar-
in caps.
cells, resulting in the blocking of the final 15 mg – 14
Therapeutic category: Antihistamine, H 2 step of acid production and so the inhibition ithromycin, all given b.i.d. (every 12 30 mg – 14.
blocker. of both basal and stimulated acid secretion hours) for two weeks. Alternatively,
Indications: Duodenal ulcer and gastric ulcer. regardless of the stimulus. The enteric coated Lansoprazole 30 mg b.i.d. on days POM LAPROZ® (Mecure)
Contra-indications: Hypersensitivity to fa- Capsule, Lansoprazole 30 mg.
pellet formulation ensures that the drug is 1-4, Azithromycin 500 mg once daily
motidine, nursing mothers. 30 mg – 2 x 7’s.
absorbed only after it leaves the stomach, with on days 2-4, and Tinidazole 2000 mg
Precautions: Children; renal impairment an absolute bioavailability over 80%, a plasma once on day 4. POM MILAN® (Elbe)
(reduce the dosage usually by half when cre- half-life of 1.5 hrs, and a duration of action >24 Dual therapy: 30 mg Lansoprazole Capsule, Lansoprazole.
atinine clearance mL/min.); pregnancy (avoid and 1 g Amoxicillin t.i.d. for 2 weeks. Pack: 1 x 2 x 30’s.
hrs. It is extensively metabolised in the liver
during the first trimester). into two inactive metabolites that undergo Active benign gastric ulcer, Short term H. pylori regimen
Adverse effects: Rarely headache, dizziness, significant biliary excretion. treatment, 30 mg once daily for up to POM LADACIN® (Nomedi)
constipation and diarrhoea; dry mouth, nausea Indications: Short-term treatment of active 8 weeks. Combipack, Each kit contains Lansoprazole (delayed
and/or vomiting, rash, abdominal discomfort duodenal ulcer; Maintenance of healed duo- Erosive esophagitis, Short term treat- release) cap; e-c granules + Tinidazole 500 mg: f-c
or distension, anorexia, and fatigue. denal ulcer; Eradication of H. pylori infection to ment, 30 mg once daily for 8 weeks; tab in quinine yellow colour + Clarithromycin 500
• Nursing action: Give with meals or liquids. prevent DU recurrence; Short-term treatment additional 8 weeks may be needed mg; f-c tab in sunset yellow FCF colour.
If needed, give antacids 1 hr before or 2 hr of active benign gastric ulcer; Short-term for patients who do not heal. In case Indications: For the eradication of H.pylori in active
after famotidine. treatment of erosive esophagitis; Maintenance of recurrence consider another 8 chronic gastritis, duodenal and gastric ulcers.
• Advise patient to avoid pepper, caffeine, weeks. Healing maintenance: 15 mg Contra-indications: Hypersensitivity to Lansopra-
of healing of erosive esophagitis; Long-term
alcohol, spices, aspirin, very hot or cold foods zole or Tinidazole or Clarithromycin.
treatment of pathological hypersecretory con- once daily.
that seem to worsen the condition. Adverse effects: Most common side effects include
ditions including Zollinger-Ellison syndrome. Pathological hypersecretory conditions nausea, diarrhea, abdominal pain and constipation.
• Cigarette smoking may increase gastric acid Contra-indications: Hypersensitivity to Lan- including ZE syndrome: The dosage Gastrointestinal: tongue discoloration, stomati-
secretion and worsen disease; making the soprazole. should be individualized according tis, diarrhea. Hypersensitivity: urticaria, pruritis,
drug less effective. Precautions: As with other antiulcerants symp- to the desired patient response for rash, flushing, sweating, dryness of mouth, fever,
• Advise patient not to take drug for longer tomatic response to treatment with Lansopra- as long as needed. The usual starting burning sensation, thirst, salivation, angioedema.
than 8 weeks except if ordered by the phy- zole does not preclude gastric malignancy. dose is 60 mg once daily. Daily doses Darkened urine; Palpitations; Transient neutropenia,
sician. Pregnancy and Lactation: Use during pregnancy >120 mg should be administered in leukopenia.
Dose: By mouth, duodenal or gastric ulcer, 40 divided doses. Dose: One pack contains two capsules of lanprazole
if clearly needed. It is not known if Lansopra- (30 mg), two tablets of tinidazole (500 mg)
mg at night; Maintenance (duodenal zole is excreted in human breast milk, the Administration: For best result take the capsules
ulcer), 20 mg at night; the doses may 30 minutes before meals. Use the drug within one and two tablets of clarithromycin (250 mg).
physician should decide to discontinue nursing One pack is for one day treatment. From
be increased if necessary. month from opening date. If you have difficulty in
this specially designed pack, one capsule healing erosive oesophagitis: 20mg 20 mg – 14’s (in blisters) term management of patients with
of lansoprazole, one tablet of tinidazole daily. healed reflux oesophagitis the rec-
POM EPRAZOLE® (Next Generation)
and one tablet of clarithromycin is to be Duration of treatment: In patients ommended dose is 10 mg once daily
Capsule, Omeprazole 20 mg
taken in the morning and similarly one with duodenal ulcer, gastric ulcer or which may be increased to 20-40 mg
20 mg – 30’s
each in the evening. The duration of therapy
reflux oesophagitis, symptoms relief Injection, Omeprazole (as sodium) 40 mg + Sterilised once daily if needed.
recommend is for 7 days.
is rapid and healing occurs within 2 water for injection 10 mL in vial. Symptomatic GERD, 10-20 mg once
weeks in most cases. For those pa- Combipack: 10 mL x 1's (in amber glass amp) + WFI daily for 4 weeks. If symptom control
OMEPRAZOLE as diluent in 10 mL vial
tients who may not have fully healed is not achieved after 4 week-treat-
Therapeutic category: Gastric acid secretion
after the initial course, healing usually POM EUCID® (Didachons) ment with Losec 20 mg once daily,
inhibitor, PPI.
occurs during a further 2 week treat- Capsule, Omeprazole 20 mg; e-c granules. further investigation is recom-
Pharmacology: Omeprazole, a proton pump
ment period with duodenal ulcer, POM GASTRODAN® (Dana) mended.
inhibitor (PPI), is an acid-activated pro-drug. It
and a further 4 week treatment for Capsule, Omeprazole 20 mg; delayed-release e-c Zollinger-Ellison syndrome, Adjust
inhibits H+K+ATPase of the gastric pump. With
patients with gastric ulcer or reflux granules in a cap. dose individually and continue treat-
a pKa of about 4.0, it selectively accumulates
oesophagitis. 20 mg – 1 x 14’s (in blisters) ment as long as clinically indicated.
in acid spaces of pH <4.0. This level of acidity
In patients refractory to other treat- Initial treatment, 60 mg daily. Main-
is achieved only in the secretory canaliculus POM GLOMEPREX® (Global Healthcare)
ment regimens, 40 mg omeprazole Capsule, Omeprazole 20 mg; delayed-release e-c tenance dose, Losec 60-20 mg daily.
of the parietal cell when the cell is secreting
once daily has been used and healing granules in a cap. Divide daily dose if it exceeds 80 mg.
acid. After accumulation in this acid space,
achieved usually within 4 weeks in 20 mg – 4 x 7’s. POM MEPAX® (Elbe)
acid activation converts omeprazole to cationic
patients with duodenal ulcer and Capsule, Omeprazole.
sulphonamide, which then binds covalently POM LOMAC® (Vitahealth)
within 8 weeks in patients with gas- Capsules, Omeprazole 10 mg, 20 mg; e-c granules. Pack: 2 x 15’s.
to cysteine on the luminal face of the gastric
tric ulcer or reflux oesophagitis. 10 mg – 10’s
H +K +ATPase thereby inhibiting the gastric
EMDEX
POM MEPRASIL® (Fidson)
Zollinger-Ellison syndrome, initially 60 20 mg – 10’s (in strip); 14’s; 28’s (in bottles); 1000’s
pump. As this action inhibits the final stage Capsule, Omeprazole 20 mg; e-c granules in green
mg once daily; adjusted according cap. marked ‘MEPRASIL 20 mg’.
of gastric acid formation, there is effective POM LOSEC® (Reals)
to individual response. In refractory 20 mg – 14’s.
inhibition of both basal and stimulated acid Capsules, Omeprazole 10 mg, 20 mg, 40 mg.
cases, 20-120 mg daily; doses above Injection, Omeprazole (as Sodium salt) 40 mg per
secretion irrespective of the stimulus to acid Dose: Duodenal ulcer, 20-40 mg once daily
80 mg should be divided during vial; in 10 mL amber coloured vial.
formation. The onset of action is rapid, and for 2-4 weeks. To prevent relapse, the
administration.
reversible control of gastric acid secretion is recommended dose is 10 mg once POM MEPROL® (Chanmedi)
Maintenance Therapy: The safety of Capsule, Omeprazole 20 mg.
achieved with once a day dosing. daily which may be increased to 20-
omeprazole in long term treatment 20 mg – 10 x 10’s.
Indications: Treatment of heartburns (pyro- 40 mg once daily if needed.
of indicated ailments has been
sis); gastroesophageal reflux disease (GORD); Gastric ulcer, 20-40 mg once daily for POM MEZOL®-C (Embassy)
established. Patients have been
stress ulceration; gastric and duodenal ulcers; 4-8 weeks. For prevention of relapse Capsule, Omeprazole 20 mg; e-c granules.
treated for upward of 3 years with
Zollinger-Ellison syndrome; acid related disor- in poorly responsive patients, 20-40 20 mg – 10’s.
omeprazole with out any harzadous
ders; prophylaxis in long-term NSAID therapy mg once daily. POM MIRAPRAZOLE® (Miraflash)
clinical results.
and acid aspiration. NSAID associated ulcers, 20 mg once Capsule, Omeprazole 20 mg; e-c pellets in a cap.
Eradication of H. pylori, 20 mg daily
Contra-indications: Pregnancy and lactation. daily for 4-8 weeks. For prevention of 20 mg – 2 x 7’s.
with Amoxicillin 500 mg t.d.s and
Precautions: Rule out malignancy prior to NSAID associated ulcers, 20 mg once
Metronidazole 400 mg b.d for 7 days. POM Oka-Omeprazole (Placeware)
treatment. Pregnancy, lactation, children. daily. Capsules, Omeprazole 10 mg, 20 mg.
Alternatively, 20 mg daily with Amox-
Adverse effects: Nausea, headache, diarrhoea, Helicobacter pylori eradication regi- 10 mg – 1 x 10’s.
icillin 500 mg t.d.s and Clarithromycin
contipation and flatulence which are mild and mens in peptic ulcer, Triple therapy 20 mg – 10 x 10’s
500 mg b.d for 7 days.
transient. regimens: Losec 20 mg, amoxicillin 1
See also under the proprietary prepara- POM OMEBET® (Geneith)
Nursing action: Give about 30 mins before g and clarithromycin 500 mg, all twice
tions below. Tablet, Omeprazole 20 mg
meal. daily for one week or Losec 20 mg, 20 mg – 10 x 2 x 7’s
Administration: Omeprazole should be taken im-
• Capsules should be swallowed whole; not mediately before meal, preferably in the morning. clarithromycin 250 mg and metroni-
chewed, crushed or opened. dazole 400 mg (or tinidazole 500 mg), POM OMECAP® (Onifam)
The capsule should be swallowed whole with liquid;
Capsule, Omeprazole 20 mg; almost white e-c pellets
• Advise patient to avoid alcohol, salicylates, the contents should not be chewed or crushed. For all twice dailly for one week.
in transparent pink cap.
ibuprofen; may cause GI irritation. patients with difficulties in swallowing, the capsule Dual therapy regimens: Losec 40-80 20 mg – 2 x 7’s; 3 x 10’s
• Discontinue medication and notify doctor if may be opened and the contents swallowed or mg daily with amoxicillin 1.5 g daily
patient reports severe diarrhoea. suspended in a slightly acidic fluid e.g. juice, yoghurt in divided doses for two weeks. In POM OMEFAST® (Greenlife)
or soured milk. The suspension should be taken clinical studies, daily doses of 1.5-3 Capsule, Omeprazole 20 mg; e-c granules in a cap.
Dose: By mouth, Adult, Active duodenal ulcer,
within half an hour. Alternatively, the contents can 20 mg – 2 x 7’s.
20 mg/day usually for 2 weeks and g of amoxicillin have been used or
be swallowed by sucking the capsule.
up to 4 – 8 weeks in severe cases. Losec 40 mg once daily and clarithro- POM OMEFLUX® (Mecure)
Gastric ulcer, 20 mg/day for up to POM Omeprazole (EDL 20.7.1) mycin 500 mg three times a day for Capsule, Omeprazole 20 mg; pellets in transparent/
4 – 8 weeks. Tablets, Omeprazole 10 mg, 20 mg. two weeks. pink cap. marked ‘OMEFLUX’.
Injection, Omeprazole (as Sodium salt) 40 mg; pow- Reflux oesophagitis, 20 mg once 20 mg – 2 x 7’s.
Erosive oesophagitis, heartburn, symp-
der for injection in vial.
toms associated with GORD, 20mg/day daily for 4-8 weeks. For severe reflux POM OMEPRAZAR® (Shrezar)
for up to 4-8 weeks depending on the POM EMPEROLE® (Pharmaplus) oesophagitis, Losec 40 mg once daily Capsule, Omeprazole 20 mg; e-c pellets
type of oesophagitis. Maintenance of Capsule, Omeprazole 20 mg for 8 weeks is recommended. For long 20 mg – 2 x 10’s (in blisters)
Injection, Omeprazole sodium (lyophilized) equiv. to Capsule, Omeprazole 20 mg; delayed-release e-c Omeprazole 20 mg, 2 tablets of Tinidazole 500 mg 40 mg – 1 x 10’s; 10 x 10’s
omeprazole 40 mg pellets. & 2 tablets of Clarithromycin 250 mg. Injection, Pantoprazole sodium (lyophilised) equiv.
40 mg – 1 vial + 10 mL diluent 20 mg – 2 x 10’s (in blisters) Indications: Eradication of H. pylori in active chronic to Pantoprazole 40 mg per vial
gastritis, duodenal and gastric ulcers. Pack: 1 vial + 10 mL diluent
POM Omeprazole (Hochiez) POM PRAZOCAP® (N.C.I)
Dose: One kit daily for 7 days. One capsule of
Capsule, Omeprazole 20 mg. Capsule, Omeprazole 20 mg. POM ULCOSTOP® (Taylek)
Omeprazole, one tablet of Tinidazole and
20 mg – 2 x 10’s. Tablet, Pantoprazole 40 mg; gastro-resistant tab
POM Omeprazole (Taylek) one tablet of Clarithromycin to be taken
40 mg – 10’s; 14’s; 28’s; 100’s (in blisters)
Capsules, Omeprazole 10 mg,20 mg; gastro-resist- POM PRAZODEX® (Crystal) in the morning and similarly one each in
ant cap. Capsule, Omeprazole 20 mg. the evening. POM VPL-Pantoprazole (Vixa)
10 mg – 2 x 7’s (in blisters) 20 mg – 1 x 14’s. Injection, Pantoprazole (as sodium) 40 mg per vial.
POM ULSAKIT® (Emzor)
20 mg – 2 x 7’s (in blisters) Pack:1 vial x 1 amps.
POM PRAZOLE® (Jawa) Capsule, Omeprazole 20 mg + Tinidazole 500 mg +
POM OMESEC® (Goben) Capsule, Omeprazole 20 mg Clarithromycin 250 mg. H. pylori regimen
Capsule, Omeprazole 20 mg; light brown cap. 20 mg – 10 x 14’s Pack: 7 x 6’s.
POM PANTRAFAR® (Neros)
marked ‘OMESEC 20’ in black, holding e-c pellets.
POM PROBITOR® (Fil) Tablet, Pantoprazole 40 mg; yellow, f-c gastro-re-
Pack: 20 mg – 2 x 7’s; 4 x 7’s; 10 x 7’s (in blisters). PANTOPRAZOLE sistant tab.
Capsule, Omeprazole 20 mg; e-c pellets in a cap.
POM OMEZ® (Phillips/Dr. Reddy’s) 20 mg – 2 x 7’s. Therapeutic category: Gastric acid secretion 40 mg – 1 x 10’s (in blisters).
Capsule, Omeprazole 20 mg; e-c granules. inhibitor, PPI. Combination therapy in H. pylori +ve patients:
POM PROTOLOC®-20 (Synergy)
20 mg – 10’s.
Capsule, Omeprazole 20 mg.
Indications :Treatment of duodenal and gas- Treat for 1 to 2 weeks:
Injection, Omeprazole (as sodium) 40 mg; lyophilised tric ulcer caused by moderate and severe gastro • Pantrafar 1 tablet twice daily + Amoxicillin 1000 mg
20 mg – 10’s.
powder for reconstitution in a single-dose vial. esophageal reflux diseases (GERD).Combination twice daily + Clarithromycin 500 mg twice daily.
Pack: 1’s. POM RAMEZOLE® (Pharmabox) • Pantrafar 1 tablet twice daily + Metronidazole 500
treatment with appropriate antibiotics for the
Dose: For slow IV injection (over a period of 5 Capsule, Omeprazole 20 mg; reddish brown/pink mg twice daily + Clarithromycin 500 mg twice daily.
eradication of Helicobacter pylori causing pep-
EMDEX
minutes), each single-dose vial containing cap. filled with white to light brown e-c granules. • Pantrafar 1 tablet daily + Amoxicillin 1000 mg twice
lyophilized powder of Omeprazole 40 mg tic ulcer. Contra-indications: Renal or hepatic
daily + metronidazole 500 mg twice daily.
should be reconstituted with 10 mL of water POM SOLCER® (Strides Vital) dysfunction; Hypersensitivity to any of the
for injection. The resulting concentration is Injection, Omeprazole 40 mg. ingredients; Pregnancy, lactation.
40 mg – 1 x 1’s. RABEPRAZOLE
4 mg/mL of Omeprazole. Precautions: Mild dyspepsia with slow di-
For IV infusion (over a period of 20-30 Therapeutic category: Gastric acid secretion
POM SOLIPRAX® (Solidum) gestion of psychological origin. Malignant
minutes), the single-dose vial should be Capsule, Omeprazole 20 mg; delayed-release e-c inhibitor, PPI.
gastroduodenal ulcer or esophagitis. Elderly
dissolved in either 100 mL of NaCl injection granules in capsule. Pharmacology: Mechanism of Action – Rabe-
or in renal insufficiency (do not exceed 1
(0.9% w/v) or 100 mL of Glucose IV infusion 20 mg – 14’s prazole belongs to the class of anti-secretory
tablet daily).
(5%w/v). No other solvent should be used compounds, the substituted benzimidazoles,
for the infusion. POM SOMECID®-20 (Diamond Remedies) Interactions: May decrease the absorption
that do not exhibit anticholinergic or H2 his-
Note: The reconstituted solution should be used Capsule, Omeprazole 20 mg; e-c granules in cap. of other drugs which depend on the low
20 mg – 2 x 7’s (in blisters). tamine antagonist properties, but suppress
within 3 hours of preparation; discard any unused gastric pH level e.g. ketoconazole. Possibility
gastro acid secretion by the specific inhibition
portion and avoid refrigeration. POM STROZOLE® (Global Organics) of interaction with other drugs of the same
of the H+/K+-ATPase enzyme (the acid or proton
Capsule, Omeprazole 20 mg; e-c granules. cytochrome P450 oxydase system.
POM OLIT® (Interpharma) pump). The effect is dose-related and leads to
Capsule, Omeprazole 20 mg 20 mg – 2 x 7’s Adverse effects: Headache, diarrhea. Rarely
inhibition of both basal and stimulated acid
20 mg – 2 x 10’s nausea, abdominal pain, flatulence, skin rash,
POM UGAZOLE® (Visko) secretion irrespective of the stimulus. Animal
Capsule, Omeprazole pruritus, dizziness, fever, blurred vision.
POM OMEZOLE® (Hovid) studies indicate that after administration,
Pack: 2 x 7’s Dose: see below.
Capsule, Omeprazole 20 mg; e-c pellets in hard rabeprazole sodium rapidly disappears from
gelatin cap. marked ‘Omezole/Hovid’. POM ULCERTRET®-20 (Pharmabase) POM PANTAKIND® (Phillips) both the plasma and gastric mucosa. As a
20 mg – 4 x 7 (in alu-alu blisters). Capsule, Omeprazole 20 mg. Tablet, Pantoprazole (as sodium) 40 mg; e-c tab. weak base, rabeprazole is rapidly absorbed
20 mg – 2 x 7’s. 40 mg – 6 x 10’s (in blisters)
POM OMIT® (Micronova) following all doses and is concentrated in the
Capsule, Omeprazole 20 mg; e-c granules cap. POM VIPRAX® 20 (Vinco) POM PANTRAFAR® (Neros) acid environment of the parietal cells. Rabep-
20 mg – 10’s; 14’s Capsule, Omeprazole 20 mg. Tablet, Pantoprazole 40 mg; yellow, f-c gastro-re- razole is converted to the active sulfonamide
20 mg – 10 x 2 x 10’s. sistant tab. form through protonation and it subsequently
POM OMIZAC® (Zoomota)
40 mg – 1 x 10’s (in blisters). reacts with the available cysteines on the
Capsule, Omeprazole 20 mg; grey/white cap. POM ZUDON® (Synergy) Dose: Take 1 hour before breakfast. Normal dose:
20 mg – 10’s. Capsule, Omeprazole 20 mg; e-c granules in a cap. proton pump.
1-2 tablets daily. Duodenal ulcer, Treat
20 mg – 14’s continuously for 2 weeks; Gastric ulcer, Indications: Treatment of active duodenal
POM OMPRAXIN® (Vixa)
Capsule, Omeprazole 20 mg gastroesophageal reflux disease (GERD), ulcer; active benign gastric ulcer; symptomatic
H. pylori regimen
20 mg – 2 x 7’s; 2 x 10’s Treat for 4 weeks. erosive or ulcerative gastro-oesophageal reflux
POM HELICLAM® (Tamar & Pharez) Elderly or Renal insufficiency: Max. 1 tablet disease (GORD); Gastro-Oesophageal Reflux
POM OXZOMOL® (Beta Drugs) Kit, Omeprazole 20 mg + clarithromycin 500 mg + daily. Disease long – term management (GORD
Capsule, Omeprazole 20 mg; e-c pellets in a cap. amoxicillin.
POM PENTOP G® (Geneith) Maintenance).
20 mg – 2 x 7’s
POM OMEFAST® Plus (Greenlife) Tablet, Pantoprazole 40 mg. Contra-indications: Hypersensitivity to
POM PERRY®-20 (Embassy) Each kit contains, Clarithromycin 250 mg (blue f-c rabeprazole, or substituted benzimidazoles;
Capsule, Omeprazole 20 mg. tab.) + Tinidazole 500 mg (blue f-c tab.) + Omepra- POM TOPRAZOLE® (Shrezar)
Pregnancy and during breast feeding.
20 mg – 2 x 7’s. zole 20 mg (e-c granules in cap.) Tablet, Pantoprazole (as sodium sesquihydrate) 40
mg;e-c tab
Precautions: Symptomatic response to
POM PINNAZOLE® (Pinnacle) Pack: 2 Combi kits. Each kit contains 2 capsules of therapy with rabeprazole sodium does not
preclude the presence of gastric or oesoph- Tablet, Rabeprazole (as sodium) 20 mg; e-c tab Pack: 6 x 10’s. may be repeated every 6–8 hours
ageal malignancy, therefore the possibility 20 mg – 2 x 14’s (in blisters) or by IV infusion, 25 mg/hour for 2
of malignancy should be excluded prior to POM BAROLE® (Mega Lifesciences) RANITIDINE hours, may be repeated every 6–8
commencing treatment. Hepatic dysfunction. Capsules, Rabeprazole (as sodium salt) 10 mg, 20 mg; Therapeutic category: Histamine H2-receptor hours.
Ability to drive and operate complex machin- e-c granules in caps. antagonist. Duodenal ulceration associated with H.
ery may be impaired. 10 mg – 3 x 10’s; 10 x 10’s Indications: Benign gastric and duodenal ul- pylori, see notes above
Adverse effects: Most commonly headache, 20 mg – 3 x 10’s; 10 x 10’s ceration, gastro-oesophageal reflux, Zollinger– Prophylaxis of NSAID-induced gastric or
diarrhoea and nausea. Others include rhinitis, Injection, Rabeprazole sodium 20 mg; sterile freeze- Ellison syndrome, other conditions where duodenal ulcer, by mouth, ADULT 300
dried powder for reconstitution.
abdominal pain, asthenia, flatulence, pharyn- gastric acid reduction is beneficial. mg twice daily
Pack: 1’s (in vial).
gitis, vomiting, nonspecific pain/back pain, Contra-indications: Porphyria. Gastro-oesophageal reflux disease, by
dizziness, flu like symptoms, infection, cough, POM PARIET® (Janssen-Cilag) Precautions: Hepatic impairment (Appendix mouth, ADULT 150 mg twice daily or
constipation and insomnia. Rash, myalgia, Tablets, Rabeprazole (as Na) 10 mg, 20 mg; gas- 5); renal impairment (Appendix 4); pregnancy 300 mg at night for up to 8 weeks, or
chest pain, dry mouth, dyspepsia, nervous- tro-resistant tabs. if necessary 12 weeks (moderate to
10 mg – 14’s
ness, somnolence, bronchitis, sinusitis, chills, middle-aged or older patients and those whose severe, 600 mg daily in 2–4 divided
20 mg – 14’s.
eructation, leg cramps, urinary tract infection, symptoms change—may mask symptoms of doses for up to 12 weeks); long-term
arthralgia and fever. In isolated cases, anorexia, POM PROMTO® (Zoomota) gastric cancer; interactions: Appendix 1. treatment of healed gastro-oesoph-
gastritis, weight gain, depression, pruritus, vi- Tablets, Rabeprazole 10 mg, 20 mg Adverse effects: Diarrhoea and other GI dis- ageal reflux disease, 150 mg twice
sion or taste disturbances, stomatitis, sweating, 10 mg – 10’s (in blisters) daily.
turbances, headache, dizziness, rash, tiredness,
leucocytosis have been observed. acute pancreatitis, bradycardia, AV block, Zollinger–Ellison syndrome, by mouth,
Nursing action: Administer whole, in the POM RABEFAST® (Biofem) confusion, depression; rarely hallucinations ADULT 150 mg 3 times daily; up to 6 g
morning about 30-60 mins before breakfast. Tablet, Rabeprazole sodium 20 mg; e-c tab. (particularly in the elderly or the very ill), daily in divided doses has been used.
EMDEX
• Advise patient to avoid alcohol, salicylates, 20 mg – 10 x 10’s’ 3 x 10’s hypersensitivity reactions (including fever, Gastric acid reduction (prophylaxis
NSAIDs; may cause GI irritation. POM RABELOC® (Interpharma) arthralgia, myalgia, anaphylaxis), blood disor- of acid aspiration) in obstetrics, by
• Discontinue medication and notify doctor if Tablet, Rabeprazole (as sodium salt) 20 mg. ders (including agranulocytosis, leukopenia, mouth, ADULT 150 mg at onset of
patient reports severe diarrhoea. 20 mg – 10’s pancytopenia, thrombocytopenia), hepatitis, labour, then every 6 hours; surgical
Dose: Adult/Elderly, Active Duodenal Ulcer and Injection, Rabeprazole (as sodium salt) 20 mg. tachycardia, agitation, visual disturbances, procedures, by IM or slow IV injection,
Active Benign Gastric Ulcer, 20 mg to Pack: 1’s (in vial) ADULT 50 mg 45–60 minutes before
erythema multiforme, alopecia, gynaecomastia
be taken once daily in the morning. POM RABEKIND® (Phillips) and impotence; very rarely interstitial nephritis. induction of anaesthesia (IV injection
Some patients with active duodenal Tablet, Rabeprazole sodium 20 mg; e-c tab. Advice to patients: It may take several days diluted to 20 mL and given over at
ulcer may respond to one 10 mg 20 mg – 6 x 10’s (in blisters) before this medicine begins to relieve stomach least 2 minutes), or by mouth, 150 mg
tablet to be taken once daily in the POM RABITAB® (Micronova) pain; antacids may be taken with ranitidine 2 hours before induction of anaesthe-
morning. Tablet, Rabeprazole 10 mg, 20 mg; e-c tab. unless otherwise instructed by the physician; sia, and also, when possible on the
Most patients with active duodenal wait 30-60 minutes between taking the antacid preceding evening.
POM RAZO® (Phillips/Dr. Reddy’s)
ulcer heal within 4 weeks. A few Tablet, Rabeprazole sodium 20 mg; e-c tab. and ranitidine; may cause drowsiness, impair Prophylaxis of stress ulceration, ADULT
refractory patients may require an 20 mg – 10’s. judgement, or co-ordination. Avoid smoking initial slow IV injection of 50 mg
additional 4 weeks of therapy to Dose: Erosive or Ulcerative Gastroesophageal Reflux as this may increase gastric acid secretion and diluted to 20 mL and given over at
achieve healing. Most patients with Disease (GERD), 20 mg once daily for 4-8 worsen disease. least 2 minutes then by continuous
active benign gastric ulcer heal within weeks; may give an additional 8 weeks Nursing action: Administer with meals for IV infusion, 125–250 µg/kg per hour
6 weeks. A few refractory patients course if necessary. Maintenance: 20 mg prolonged effect. may give antacids 1 hr before (may be followed by 150 mg twice
may require an additional 6 weeksof once daily. or 1 hr after ranitidine. daily by mouth when oral feeding
therapy to achieve healing. Duodenal Ulcers, 20 mg once daily after • See also under Cimetidine. commences).
morning meal for upto 4 weeks. Note: H2 – receptor blockers are taken in the night
Erosive or Ulcerative Gastro-Oesopha- Dose: Benign gastric and duodenal ulceration,
Hypersecretory conditions like Zollinger for more effective ulcer healing. Antacids are taken
geal Reflux Disease (GORD), 20 mg to Ellison Syndrome, initially 60 mg once daily; by mouth, ADULT 150 mg twice daily
be taken once daily for 4-8 weeks. or 300 mg at night for 4–8 weeks, during daytime to neutralise acidity.
adjust dose according to response. May
Gastro-oesophageal reflux Disease increase to 100-120 mg daily and continue up to 6 weeks in chronic episodic POM Ranitidine (WMF 17.1)
Long-term Management (GORD Main- treatment for upto one year. dyspepsia, and up to 8 weeks in Tablet, Ranitidine (as HCl) 150 mg
tenance), For long-term management, NSAID-associated ulceration (in Oral liquid, Ranitidine (as HCl) 75 mg/5 mL.
H. pylori regimen Injection, Ranitidine 25 mg/mL; in 2-mL ampoule.
a maintenance dose 10-20 mg once NSAID-associated duodenal ulcer
daily can be used depending upon POM ELICORID® (Solidum) 300 mg can be given twice daily for POM Ranitidine (EDL 20.7.1)
patient’s response. Kit, Rabeprazole 20 mg (e-c tab) + Amoxicillin 1000
4 weeks to achieve a higher healing Tablets, Ranitidine 150 mg, 300 mg.
mg (capsule) + Clarithromycin 500 mg (f-c tab).
Not recommended for use in children. No rate); CHILD (peptic ulcer) 2–4 mg/kg Injection, Ranitidine (as HCl) 25 mg per mL; in
Pack: 42’s (Kit containing 7 days of therapy). 2-mL amp.
dosage adjustment is necessary for patients Dose: Adult, 20 mg Rabeprazole, 1 g Amoxicllin and twice daily, maximum 300 mg daily.
with renal or hepatic impairment. 500 mg Clarithromycin; all given twice daily Benign gastric and duodenal ulcera- POM ACILOC® (Interpharma)
POM ACERID® (Solidum) for 7 days. To be taken before meals. tion, reflux oesophagitis, Zollinger– Tablets, Ranitidine 150 mg, 300 mg; both are f-c tabs.
Tablet, Rabeprazole sodium 20 mg; e-c tab. Ellison syndrome, by IM injection, 150 mg – 10 x 10’s.
POM PYLOREST® (Biofem) 300 mg – 2 x 10’s.
20 mg – 30’s Tablet, Rabeprazole 20 mg, Amoxicillin 1 g, Clar-
ADULT 50 mg every 6–8 hours or by
ithromycin 500 mg. slow IV injection, 50 mg diluted to 20 POM APO-RANITIDINE® (Lahams)
POM BEPRAZOLE® (Barata)
mL and given over at least 2 minutes,
152 | 4.1.2 Ulcer healing drugs 4.2 Antispasmodic drugs | 153
Tablets, Ranitidine 150 mg, white f-c tab. marked f–c tab. marked ‘GLAXO’ and ‘ZANTAC 150’; 300 mg, 16 weeks treatment may be given in any one year. with food or 200 mcg twice daily with food.
‘APO 150’; 300 mg, white, scored, oblong f-c tab. white, capsule–shaped, f–c tab., marked ‘GLAXO’ on
POM PYLORID® (GSK)
marked ‘APO 300’. one face and ‘ZANTAC 300’ on the other. 4.2 Antispasmodic drugs
Tablet, Ranitidine bismuth citrate 400 mg; light blue
150 mg – 100. 150 mg – 20; 60.
octagonal capsule shaped f-c tab. The smooth muscle relaxant properties of an-
300 mg – 100. 300 mg – 10; 30.
Effervescent Tablets, Ranitidine (as HCl) 150 mg, 300 ticholinergic (more correctly termed antimus-
POM BITIDINE® (Pharmabox) MUCOSAL PROTECTIVE AGENTS
mg; white to pale yellow, round, flat, bevel–edged carinic) and other antispasmodic drugs may be
Tablets, Ranitidine (HCl) 150 mg, 300 mg; white
tabs which effervesce on dissolution in water to Sucralfate useful in dyspepsia, irritable bowel syndrome,
f-c tabs.
give a clear, grapefruit/orange flavoured solution. and in diverticular disease. The gastric antise-
150 mg – 5 x 10’s. Sucralfate, or aluminum sucrose sulphate, is a
Effervescent Granules, Ranitidine (as HCl) 150 mg, cretory effects of conventional anticholinergic
300 mg – 5 x 10’s. sulphated disaccharide developed for use in
300 mg; white to pale yellow, free flowing granules
drugs are of little practical significance since
POM HISTAC® (Ranbaxy) which effervesce on dissolution in water to give a peptic ulcer disease.
clear, grapefruit/orange flavoured solution. dosage is limited by atropine-like adverse
Tablets, Ranitidine (as HCl) 150 mg, 300 mg; both
Injection, Ranitidine (as HCl) 25 mg per mL; 2 mL
It binds selectively to necrotic ulcer tissue, effects. Moreover they have been superseded
are f-c tabs.
150 mg – 10’s aqueous solution in amp. where it may act as a bile to acid, pepsin, and by more powerful and specific antisecretory
300 mg – 10’s. barrier. In addition, sucralfate may directly drugs, including the histamine H2-receptor
POM ZYNOL® (Elbe) absorb bile salts. It is effective in the healing of antagonists.
POM PEPTACID® 75 (Joswe/Afrab) Tablet, Ranitidine 300 mg.
duodenal ulcers. It is not absorbed systemically,
Effervescent tablet, Ranitidine (as HCl) 75 mg. Anticholinergics that are used for GI smooth
and few adverse effects have been reported.
Dose: Dissolve each tablet in 100-150 mL of water RANITIDINE BISMUTH CITRATE muscle spasm include atropine and hyoscine
before drinking. The dosage is 1g 4 times daily on an empty
Synonym: Ranitidine bismutrex. butylbromide.
For relief of symptoms, take one dose. stomach (at least 1 hour before meals). It also
Therapeutic category: Histamine H2-Receptor Nursing action: – Anticholinergics
To prevent symptoms, take one dose 30 to 60 requires an acid pH to be activated and so
Antagonist. • Give with or after meals to prevent GI upset;
minutes before eating food or drinking bev- should not be administered simultaneously
EMDEX
Indications: Treatment of duodenal ulcer and may give with fluids other than water. Hard
erages that cause heartburn. Can be used with antacids or an H2–receptor antagonist.
up to twice daily (up to 2 tablets in 24 hours benign gastric ulcer; also used in eradication candy, frequent drinks, sugarless gum may be
Not recommended for children <12 years. regimen for Helicobacter pylori with other Colloidal Bismuth Compounds needed to relieve dry mouth.
drugs. Like sucralfate, these compounds seem to • Monitor patient for urinary retention (may
POM PEPTACID® 150 (Joswe/Afrab)
Contra-indications: Moderate to severe renal work by selective binding to an ulcer and by palpate bladder); constipation (increase flu-
Effervescent tablet, Ranitidine (as HCl) 150 mg
impairment; long-term (maintenance) therapy; coating it to protect the ulcer from acid and ids, bulk, exercise); mood changes.
POM PEPTARD® (Neimeth) porphyria; pregnancy, breast-feeding. pepsin. Tripotassium dicitrato bismuthate has • Advise patient to avoid driving or other
Tablet, Ranitidine 150 mg. been shown to be superior to placebo in the hazardous activities as drowsiness may oc-
Precautions: May mask symptoms of gastric
150 mg – 60’s. cur. OTC medications for cough & cold with
carcinoma (exclude malignancy before ther- healing of both duodenal and gastric ulcers.
POM RANIT®-300 (Mecure) apy); renal impairment, elderly (excreted via alcohol, antihistamines should be avoided
Carbenoxolone
Tablet, Ranitidine 300 mg. the kidneys). unless prescribed by doctor.
Carbenoxolone, a synthetic derivative of gly-
POM RANITAL® (Taylek) Adverse effects: May cause blackening of the
cyrrhizinic acid (an extract from liquorice), is DICYCLOMINE plus DIMETHICONE
Tablets, Ranitidine (as HCl) 150 mg, 300 mg stools and tongue (due to bismuth); rarely
effective in healing both gastric and duodenal Synonym: Dicycloverine plus Simethicone
OTC Ranitidine (Embassy)
hypersensitivity reactions including pruritus,
ulcers. Its mechanism of action may involve Therapeutic category: Anticholinergic/Anti-
Tablet, Ranitidine 300 mg skin rash, anaphylaxis; GI disturbances; head-
an increase in the production, secretion, and muscarinic agent; Antispasmodic.
300 mg – 1 x 10’s ache; transient changes in the liver enzymes;
viscosity of intestinal mucus. Its clinical useful- Indications: Irritable bowel syndrome; relief of
mild anaemia.
POM RANIVAN® (Evans) ness has been limited by aldosterone–like side intestinal, renal, biliary, uterine & infant colics.
Advice to patients: May cause blackening of
Tablets, Ranitidine 150 mg, 300 mg. effects such as hypertension, fluid retention,
the stools and tongue. Contra-indications: Hypersensitivity; Glau-
150 mg – 100’s. and hypokalaemia. The concurrent adminis-
300 mg – 10’s. Nursing action: See under Ranitidine. coma; children <6 months.
tration of spironolactone controls the fluid Adverse effects: Nausea, vomiting, consti-
Dose: By mouth, Duodenal ulcer, 400 mg
POM ULCERDIN® (N.C.I) retention but also abolishes the ulcer–healing pation; confusion, blurred vision, diplopia,
twice daily for 4 weeks; may be
Tablet, Ranitidine 300 mg; white tabs. effect; thiazides prevent sodium retention mydriasis, cycloplegia, increased ocular ten-
extended for another 4 weeks if
300 mg – 1 x 10’s. without abolishing the beneficial effect in
required. sion; rash, urticaria, itching; urinary retention;
POM ULTICER® (Medreich) peptic disease. tachycardia, palpitations.
Benign gastric ulcer, 400 mg twice
Tablets, Ranitidine (as HCl) 150 mg, 300 mg. daily for 8 weeks Dose: Child (6 months – 2 years): 10-20
150 mg – 30’s OTHER ULCER HEALING DRUGS drops 3-4 times daily; >2 years, 1 mL
Eradication of H. pylori (combination
300 mg – 30’s
therapy), 400 mg twice daily plus Misoprostol is a prostaglandin analogue 3-4 times daily. Administer 15 mins
Injection, Ranitidine (as HCl) 50 mg per 2 mL; in 2
mL amps. Amoxycillin 1 g twice daily plus particularly useful in the prevention of before food.
Pack: 2 mL x 10’s. Metronidazole 400 mg twice daily NSAID-induced gastric ulcers. It is a synthetic OTC CENTWIN® (Al-Tinez)
for a total of 4-8 weeks. prostaglandin E1 analogue that replaces the Suspension, Dicyclomine 10 mg, dimethicone 40 mg
POM ZANIDEX® (Pemason) Note: Not recommended for children. Ranitidine protective prostaglandins consumed with per mL; yellow susp.
Tablet, (150 mg), Ranitidine (as HCl) 150 mg; ivory tab bismuth citrate is not indicated for long-term (main-
Caplet, (300 mg), Ranitidine (as HCl) 300 mg; ivory prostaglandin-inhibiting therapies, e.g. non- Pack: 10 mL with calibrated dropper.
tenance) therapy; more than two 8-week courses steroidal anti-inflammatory drugs. It is taken
caplet. in any one year should be avoided because of the
orally and usually adult dosage is 200 mcg 4 HYOSCINE N-BUTYLBROMIDE
POM ZANTAC® (GSK) possibility of accumulation of bismuth. If 4-week
courses of therapy are given, up to a maximum of times daily with food. If not tolerated, the dose Synonym: Scopolamine
Tablets, Ranitidine (as HCl) 150 mg, white, round
may be decreased to 100 mcg 4 times daily Therapeutic category: Anticholinergic/Anti-
154 | 4.2 Antispasmodic drugs 4.3 Other smooth muscle relaxants | 155
muscarinic Agent; Antispasmodic. 10 mg – 10’s; 100’s OTC Hyoscine-N-Butylbromide (Pemason) utes before feeding.
Pharmacology: Hyoscine N-butylbromide Injection, Hyoscine-N-butylbromide 10 mg per mL;
OTC BUSCO-J® (Juhel) POM BUSCOMIN®(Drugfield)
inhibits muscarinic actions of acetylcholine on 1-mL amp. marked “Pemason Hyoscine”.
Tablet, Hyoscine-N-butylbromide 10 mg. Drops, Homatropine methylbromide 2 mg per mL
autonomic effectors innervated by postgangli- Pack: 1 mL amps; 10 x 10’s
10 mg – 100’s; 500’s. Pack: 15 mL (in bottle with dropper)
Injection, Hyoscine-N-butylbromide 20 mg per mL;
onic cholinergic neurons. It has a special site of
OTC BUSCOMAC® (Pacmai) 1-mL amp. marked “Pemason Hyoscine”. POM NOSPAMIN® (Afrab-Chem)
action at the parasympathetic ganglia in the Tablet, Hyoscine – N-butylbromide 10 mg Pack: 1-mL amps x 10 x 10’s Tablet, Homatropine methylbromide 10 mg.
walls of the viscera. Because of this, it exerts a 10 mg – 10 x 10’s (in blisters) 10 mg – 20; 100; 500.
specific antispasmodic action on the smooth POM LOCIN® (Beta Drugs)
Injection, Hyoscine butylbromide 20 mg per mL; Syrup, Homatropine methylbromide
Injections, Hyoscine N-butylbromide 10 mg, 20 mg
muscle of the GI, biliary and urinary tracts, this clear, colourless solution. 5 mg per 5 mL.
per 1-mL ampoule.
action being produced long before side effects Pack: 10 x 1 mL amps per box.
Pack: 1-mL x 10’s. Pack: 6 mL.
characteristic of atropine-like substances OTC BUSMOCALM® (Neros)
Paediatric drops, Homatropine methylbromide 2
occur, hence, no side effects on the CNS or OTC MOSCINE® (GoldMoore) mg per mL.
Tablet, Hyoscine butylbromide 10 mg.
salivary glands are observed when the drug is Syrup, Hyoscine-N-butylbromide 5 mg per 5 mL. Pack: 15 mL (with dropper).
Pack: 60 mL.
administered in therapeutic doses.
POM CHANSCOPAN® (Chanmedi) VALETHAMATE
Indications: Gastric and duodenal ulcers, POM ORYCINE® (GoldMoore)
Tablet, Hyoscine N-Butyl bromide 10 mg.
gastrointestinal spasm and hypermotility, py- Injection, Hyoscine butylbromide 20 mg; in 1-mL Therapeutic category: Anticholinergic agent.
10 mg – 10 x 10’s.
lorospasm in infants, postoperative vomiting, amp Description: It is a smooth muscle relaxant, an
spastic constipation, biliary dyskinesia and OTC CINEX® (Vixa) Pack: 10 x 1 mL. anticholinergic agent with peripheral actions
Tablet, Hyoscine-N-butylbromide 10 mg similar to those of atropine.
spasm of urinary tract, delayed relaxation of OTC REXOPAN® (Greenlife)
10 mg – 10 x 10’s Indications: Musculo-skeletal disorders:
the lower uterine segment, dysmenorrhoea. Tablet, Hyoscine butylbromide 10 mg.
Injection, Hyoscine butylbromide 10 mg; in amp.
Contra-indications: Glaucoma, urinary reten- 10 mg – 10 x 10’s (in blisters). Smooth muscles spasms, especially in delayed
EMDEX
tion, mechanical stenoses in the GIT, tachycar- POM COLIPAN® (NGC) dilation of cervix.
OTC SPASMIN® (Therapeutic)
dia, megacolon. Tablet, Hyoscine-N-butylbromide 10 mg; sug- Gastrointestinal tract: Symptomatic relief of
Drops, Hyoscine butylbromide 2 mg per 5 mL.
ar-coated tab. GI, biliary & ureteric colic.
Precautions: Patients over 40 years (may cause Pack: 15 mL.
Pack: 20’s; 100’s
glaucoma); prolonged administration (toler- Contra-indications: Cardiac insufficiency, Se-
Elixir, Hyoscine-N-butylbromide 5 mg per 5mL
ance may develop); asthma; hypertension; Pack: 100 mL. HOMATROPINE METHYLBROMIDE vere Hypertension, Glaucoma, Thyrotoxicosis,
myasthenia gravis; ulcerative colitis; urinary Therapeutic category: Antimuscarinic agent; Prostatic enlargement, GI obstruction, paralytic
retention; reflux oesophagitis may be aggra- OTC COLOSPAN® (Hovid) ileus, acute GI haemorrhage, ulcerative colitis,
Antispasmodic.
Tablet, Hyoscine butylbromide 10 mg; s-c tab. toxic megacolon.
vated; paralytic ileus or pyloric stenosis (may Indications: Treatment of gastro-intestinal
10 mg – 2 x 20’s; 10 x 20’s (in blisters)
lead to obstruction); pregnancy, breastfeeding, spasms and as adjunct in the treatment of Precautions: Avoid use in thyrotoxicosis, car-
children, elderly. OTC HYOMIDE® (Goben) peptic ulcer. diac disease. Pregnancy, Breastfeeding, Elderly.
Interactions: Tricyclic antidepressants, aman- Tablet, Hyoscine butylbromide 10 mg; white f-c tab. Adverse effects: Blurred vision, impaired
Contra-indications: Myasthenia gravis; closed
10 mg – 100 x 10’s (in blisters). alertness, dryness of mouth, flushing, urinary
tadine, some antihistamines, phenothiazines, or nervous angle glaucoma.
Dose: Adult, by mouth, 10-20 mg 3-4 times daily. retention, vomiting, nervousness, giddiness,
butyrophenones (these drugs have anticholin- In dysmenorrhoea, start treatment 2 days Precautions: Acute myocardial infarction,
ergic properties and co-administration may en- thyrotoxicosis, cardiac insufficiency. palpitation, drug rash, fetal tachycardia and
before the expected onset of the period and
hance the effect of hyoscine). Alcohol or other continue for three days after menstruation Interactions: Co-administration with other headache.
CNS depressants; MAOIs; Sympathomimetics. has begun antimuscarinic drugs such as atropine, hyosine, Dose: see below.
Adverse effects: Dry mouth and skin; increased Children (6-12 years), 10 mg 3 times daily antihistamines, butyrophenones, phenothi- POM OSDIL® (Synergy)
pulse rate; transient disturbance of accommo- OTC Hyoscine butylbromide (Dabak) azine, and TCAs may potentiate the effects of Injection, Valethamate bromide 8 mg; in 1-mL amp.
dation which can affect vision; constipation; Tablet, Hyoscine butylbromide 10 mg homatropine. Pack: 1 mL x 1’s(in amp).
photophobia; urinary urgency and retention. 10 mg – 10 x 10’s; 1 x 500’s Adverse effects: Mydriasis, cycloplegia; Dose: By IM or IV injection, GI, Biliary or Ureteric
Occasionally nausea, vomiting and giddiness, prolonged use may lead to cardiovascular Colic, 4-8 mg.
POM Hyoscine butylbromide (Vixa) By deep IM injection, In delayed dilation of
particularly in the elderly. side effects such as bradycardia followed by
Tablet, Hyoscine butylbromide 10 mg cervix, when the os-uterus has dilated 2-4 cm,
Nursing action: See notes above. Injection, Hyoscine butylbromide 20 mg per mL relaxed tachycardia with palpitation; in high 8 mg; if required repeat after 20 minutes.
Dose: By mouth, Adult and child (>6 years), doses urinary urgency, difficulty and retention, Children: Not Applicable.
10-20 mg 3-5 times daily. OTC Hyoscine (Embassy)
constipation due to reduction in gut motility
Injection, Hyoscine butylbromide BP 20 mg per mL.
Child (<6 years): not recommended. (paralytic ileus) may occur; dryness of mouth;
Pack: 10 x 1 mL ampoule in a unit carton. 4.3 Other smooth muscle relaxants
By S.C., I.M. or slow I.V., acute spasm, difficulty in swallowing.
20 mg, repeated after 30 minutes if OTC Hyoscine (Geneith) Dose: By mouth, Adult, 10-20 mg 3-4 times DROTAVERINE
required. Tablet, Hyoscine butylbromide 10 mg; white daily; Child (up to 3 months), 2-4
coated tab Indications: Spasms of smooth muscles in
POM Hyoscine N-Butylbromide (EDL 20.4) drops 3-4 times 3-6 months, 4-6 drops
10 mg – 10 x 10’s. cholelithiasis, nephrolithiasis, cholecystitis,
Tablet, Hyoscine N-butylbromide 10 mg. 3-4 times daily; 6-12 months, 6-9
OTC Hyoscine (N.C.I.)
pyelitis, cystitis, vescal tenesmus. As adjuvant
Oral liquid, Hyoscine N-butylbromide 1 mg per mL drops 3-4 times daily; 1-3 years, 2.5
Tablet (solid), Hyoscine butylbromide 10 mg in ventricular and duodenal ulcer, cardia and
Injection, Hyoscine N-butylbromide 20 mg per mL; mL 2-3 times daily; 3-6 years, 5 mL
10 mg – 10 x 10’s pylorus spasm, irritable colon syndrome, hy-
in 1-mL amp. 2-3 times daily; 6-12 years, 10 mg 2-3
pertension, angina pectoris, and intermittent
OTC BOXCOTAB® (Pharmabox) OTC Hyoscine-N-Butylbromide (Pemason) times daily.
claudication. Also effective in dysmenorrhoea,
Tablet, Hyoscine butylbromide 10 mg; s-c tab. Tablet, Hyoscine-N-butylbromide 10 mg Note: Infant doses are to be taken 10-15 min-
strong labour pains, tetanus uteri, imminent
156 | 4.4 Drugs used in diarrhoea 4.4.2 Medicines for diarrhoea in children | 157
abortion. cases of chronic diarrhoea have non-infectious solution should continue to be offered once Precautions: Renal impairment.
Contra-indications: Severe liver, renal and causes including gluten-sensitivity, inherited dehydration has been controlled, for as long as Adverse effects: Vomiting—may indicate too
cardiac insufficiency. metabolic disorders or inflammatory bowel the child continues to have diarrhoea. rapid administration; hypernatraemia and
Adverse effects: Headache, dizziness, nausea, disease. Plan C: severe dehydration. Hospitalization is hyperkalaemia may result from overdose in
palpitation, and hypotension may occur. Bloody diarrhoea is usually a sign of invasive necessary, but most urgent priority is to start renal impairment or administration of too
Dose: Adult, by mouth, usually 120-240 mg enteric infection and should be treated with rehydration. In hospital (or elsewhere), if the concentrated a solution.
daily in 3 divided doses; by SC or an appropriate anti-infective agent. child can drink, oral rehydration solution must Dose: Fluid and electrolyte loss in acute
IM injection, 40-240 mg daily in 1-3 be given pending, and even during, intrave- diarrhoea, by mouth , ADULT 200–400
divided doses. 4.4.1 Oral rehydration nous infusion (20 mL/kg every hour by mouth mL solution after every loose motion;
Acute stone colic, by IV injection, 40-80 Replacement of fluid and electrolytes orally before infusion, then 5 mL/kg every hour by INFANT and CHILD according to Plan
mg can be achieved by giving oral rehydration mouth during intravenous rehydration). For A, B or C (see notes above).
Child (1-6 years), by mouth, 40-120 salts—solutions containing sodium, potas- IV supplementation, it is recommended that OTC Oral Rehydration Salt (EDL 20.6.1)
mg daily in 2-3 divided doses; >6 sium, citrate and glucose. Acute diarrhoea in compound solution of sodium lactate (or, Powder, Glucose anhydrous 13.5 g, Potassium
years, 80-200 mg daily in 2-5 divided children should always be treated with oral if this is unavailable, sodium chloride 0.9% chloride 1.5 g, Sodium citrate dihydrate 2.9 g (or
doses. rehydration solution according to plans A, B, intravenous infusion) (see section 26.2) is Sodium bicarbonate 2.5 g), Sodium chloride 2.6 g
administered at a rate adapted to the child’s per litre of solution.
POM NO-SPA® (Sanofi-Aventis) or C as shown (see also section 4.4.2).
Tablet, Drotaverine HCl 40 mg.
Treatment of dehydration: age (infant under 12 months: 30 mL/kg over OTC EMZOLYTE® ORS (Emzor)
40 mg – 20’s; 100’s. 1 hour then 70 mL/kg over 5 hours; child over Oral Rehydration salt, (20.5 g), Sodium chloride 2.60
WHO recommendations
Tablet (forte), Drotaverine 80 mg. 12 months: the same amounts over 30 minutes g, potassium chloride 1.50 g, sodium citrate 2.90 g,
80 mg – 20’s According to the degree of dehydration, health dextrose 13.50 g
and 2.5 hours respectively). If the IV route is
Injection, Drotaverine HCl 20 mg per mL; in 2-mL professionals are advised to follow one of 3 Pack: 3’s; 30’s; 60’s
unavailable, a nasogastric tube is also suitable
EMDEX
amp. management plans.
Pack: 5’s; 25’s. for administering oral rehydration solution at a OTC KOSYLITE® (Gauze)
Plan A: no dehydration. Nutritional advice, rate of 20 mL/kg every hour for 6 hours. If the Oral dry syrup, Glucose (anhydrous) 20 gm, sodium
+ Paracetamol + Codeine increased fluid intake (soup, rice, water and child vomits, the rate of administration of the citrate 2.9 gm, sodium chloride 3.5 gm, potassium
POM NO-SPALGIN® (Sanofi-Aventis) yoghurt, or even water) and zinc supplemen- oral solution should be reduced. Reassess the chloride 1.5 gm per 27.9 gm sachet.
tation (section 4.4.2) at home are sufficient. Pack: 3’s (in sachets)
Tablet, Paracetamol 500 mg, drotaverine 40 mg, child’s status after 3 hours (6 hours for infants)
codeine phosphate 8 mg. For infants aged under 6 months who have and continue treatment as appropriate with OTC ORALDOZ® (Global Healthcare)
Pack: 12’s (in blisters) not yet started taking solids, oral rehydration plan A, B or C. Oral rehydration salts (20.5 g), Sodium chloride 2.6
solution must be presented before offering gm, potassium chloride 1.5 g, sodium citrate 2.9 g,
4.4 Drugs used in diarrhoea milk. Mother’s milk or dried cow’s milk must ORAL REHYDRATION SALTS anhydrous glucose 13.5 g; orange-flavoured.
be given without any particular restrictions. Pack: 20.5 g x 3’s.
4.4. Oral rehydration Composition of glucose salt solution (mmol/litre):
4.4.2. Medicines for diarrhoea in children In the case of mixed breast-milk/formula OTC Oral Rehydration Salt (CHI)
sodium 75 mmol/litre
4.4.3. Antimotility drugs feeding, the contribution of breastfeeding Paediatric dispersible tablet (20.5 g), Sodium chloride
chloride 65 mmol/litre 2.6 g, potassium chloride 1.5 g, sodium citrate 2.9 g,
4.4.4. Adsorbents and bulk-forming drugs must be increased. Parents should be advised
4.4.5. Antidiarrheal microorganisms about circumstances in which they should seek glucose, anhydrous 75 mmol/litre anhydrous glucose 13.5 g; colour and flavour.
further advice. potassium 20 mmol/litre Pack: 1 x 2's (in blisters).
See EMDEX Paediatric Drug Guide chapter 2 for the
detailed information on Management of Childhood citrate 10 mmol/litre OTC Oral Rehydration Salt (Crystal)
Plan B: moderate dehydration. Whatever
Diarrhoea. Total osmolarity. 245 mOsm/litre Sachet, Dextrose (anhydrous) 20 g, sodium citrate
the child’s age, a 4-hour treatment plan is
Composition of glucose salt solution (grams/litre): 2.90 g, sodium chloride 3.50, potassium chloride
Acute diarrhoeal diseases are a leading cause applied to avoid short-term problems. It is 1.50 g.
sodium chloride. 2.6 g/litre of clean water
of childhood morbidity and mortality; frail recommended that parents are shown how Pack: 3 sachets
to give approximately 75 mL/kg of oral rehy- sodium citrate 2.9 g/litre of clean water
and elderly patients are also at risk. In adults potassium chloride 1.5 g/litre of clean water OTC ORASALT® (Megapharm)
acute diarrhoea is the most frequent health dration solution over a 4-hour period, and it
Powder, Sodium chloride 2.6 g, glucose anhydrous
problem of travellers to developing countries is suggested that parents should be watched glucose (anhydrous) 13.5 g/litre of clean water
13.5, potassium chloride 1.5 g, trisodium citrate
and is increasingly common among HIV-in- to see how they cope at the beginning of the When glucose and sodium citrate are not available, they may dihydrate 2.9 g per litre.
treatment. A larger amount of solution can be be replaced by:
fected persons. Assessment and correction Pack: 1 x 3’s (in sachets)
of dehydration and electrolyte disturbance given if the child continues to have frequent sucrose (common sugar) 27 g/litre of clean wate
is the priority in all cases of acute diarrhoea. stools. In case of vomiting, rehydration must be sodium bicarbonate 2.5 g/litre of clean water 4.4.2 Medicines for diarrhoea
Symptomatic relief (section 4.3.2) in adults may discontinued for 10 minutes and then resumed in children
be warranted in some cases but antidiarrhoeals at a slower rate. Breastfeeding should be Note: The solution may be prepared either from
continued on demand; other children should prepackaged sugar/salt mixtures or from bulk ZINC SULFATE
should never be used in children since they do substances and water. Solutions must be freshly
not reduce fluid and electrolyte loss and may receive milk and nutritious food as normal after Indications: Adjunct to oral rehydration ther-
completing the 4 hours of oral rehydration. The prepared, preferably with recently boiled and cooled
cause adverse effects. water. Accurate weighing and thorough mixing and apy in acute diarrhoea.
Diarrhoea persisting for longer than a month child’s status must be reassessed after 4 hours Precautions: Acute renal failure (may accumu-
dissolution of ingredients in the correct volume of
is known as chronic diarrhoea. A mild malab- to decide on the most appropriate subsequent clean water is important. Administration of more late); interactions: Appendix 1.
sorption syndrome, tropical enteropathy, is ap- treatment. Zinc supplementation should begin concentrated solutions can result in hypernatraemia. Adverse effects: Abdominal pain, dyspepsia,
parent in most healthy indigenous populations as soon as the child can eat and has completed Indications: Dehydration from acute diar- nausea, vomiting, diarrhoea, gastric irritation,
of tropical countries. However the majority of 4 hours of rehydration. Oral rehydration rhoea. gastritis; irritability, headache, lethargy.
158 | 4.4.3 Antimotility drugs 4.4.3 Antimotility drugs | 159
Dose: Adjunct to oral rehydration therapy in CODEINE
acute diarrhoea, by mouth, INFANT
Drug subject to international control under the Single
under 6 months, 10 mg (elemental Convention on Narcotic Drugs (1961).
zinc) daily for 10–14 days; CHILD 6
months–5 years, 20 mg (elemental Indications: Short-term symptomatic relief of
zinc) daily for 10–14 days. acute diarrhoea in adults; pain (section 1.8.2).
Administration: Zinc sulfate tablets may be dis- Contra-indications: Children; conditions
persed in breastmilk, in oral rehydration solution or where inhibition of peristalsis should be
in water on a small spoon; older children may chew avoided; abdominal distension; acute diar-
tablets or swallow them with water. rhoeal conditions such as ulcerative colitis or
OTC Zinc sulfate (WMF 17.5.2) antibiotic-associated colitis; acute respiratory
Tablet, Zinc sulfate 10 mg per unit dosage form. depression.
Oral liquid, Zinc sulfate 10 mg per unit dosage form. Precautions: Tolerance or dependence may
OTC Zinc sulfate (EDL 20.6.2) occur with prolonged use; elderly and debili-
Tablet, Zinc sulfate 10 mg per unit dosage form. tated patients; hepatic impairment (Appendix
Oral liquid, Zinc sulfate 10 mg per unit dosage form. 5); renal impairment (Appendix 4); pregnancy
OTC Zinc Sulphate Paediatric (CHI)
Dispersible tablet, Elemental zinc (as Zinc sulfate overdosage: see section 19.2.2; interactions:
monohydrate) 20 mg. Appendix 1.
Pack: 1 x 10's (in blisters) Adverse effects: Nausea, vomiting, consti-
pation, drowsiness; respiratory depression
Zinc gluconate
EMDEX
and hypotension (large doses); dependence;
See under section 6.6 difficulty with micturition; ureteric or biliary
spasm; dry mouth, sweating, headache, facial
4.4.3 Antimotility drugs flushing, vertigo, bradycardia, tachycardia,
palpitations, hypothermia, hallucinations,
Opioids such as codeine are used in the dysphoria, mood changes, miosis, decreased
symptomatic relief of uncomplicated, acute libido or potency, rash, urticaria, pruritus;
diarrhoea in adults but not in young children. convulsions (large doses).
They act on opioid receptors in the gut wall and Dose: Symptomatic relief of acute diarrhoea,
decrease bowel motility. In dehydration, fluid by mouth, ADULT 30 mg 3–4 times
and electrolyte replacement (section 6.10) are daily
of primary importance.
CD Codeine (WMF 17.5.3)
Diphenoxylate and Loperamide Tablet, Codeine phosphate 30 mg.
Both are phenylpiperidine derivatives that
CD Codeine (EDL 20.6.3)
are used to reduce the motility of the gut. In Tablet, Codeine phosphate 30 mg.
acute diarrhoeas, they are used as adjuncts to
fluid and electrolyte replacement but are not DIPHENOXYLATE plus ATROPINE
recommended for young children.
Indications: Diarrhoea
As an antidiarrheal drug, diphenoxylate is Contra-indications: Hypersensitivity to di-
usually used in combination with atropine phenoxylate or atropine; infectious diarrhoea;
(Lomotil®). The adult dosage is 2 tablets pseudomembranous colitis; obstructive jaun-
every 6 hours until the diarrhoea is controlled. dice; child under 2 year.
Loperamide (Imodium®) does not have the Precautions: Pregnancy, lactation; hepatic or
sedative or respiratory depressant effects of renal disease; ulcerative colitis.
diphenoxylate. The usual dose is 4mg to start Adverse effects: Anticholinergic effects such
and then 2mg after each diarrhoeal stool for as constipation, blurred vision, dry mouth
up to 5 days. orskin; drowsiness.
Propantheline Dose: Adult, by mouth, 1 tablet 4 times daily.
If no improvement within 48 hours, it
Anticholinergic (antimuscarinic) drugs di-
is unlikely to be effective.
minish intestinal motility. They sometimes
have a beneficial effect on diarrhoea, but are CD Diphenoxylate plus Atropine (EDL 20.6.3)
frequently of great value in relieving colicky Tablet, Diphenoxylate HCl 2.5 mg, Atropine sulfate
abdominal pain if this is an accompaniment 25 mcg.
Note: Atropine is included in the formulation to
to the diarrhoea (see section 4.2). They should
deter abuse of Diphenoxylate.
not be used for primary treatment.
160 | 4.4.3 Antimotility drugs 4.4.4 Adsorbents and bulk-forming drugs | 161
LOPERAMIDE POM COLOSEAL® (Hovid)
Therapeutic category: Antidiarrhoeal. Capsule, Loperamide HCI 2 mg
2 mg – 10 x 10’s (in blisters)
Indications: Symptomatic control of acute and
chronic diarrhoea when inhibition of peristalsis OTC DIAFLUSH® (Embassy)
is indicated; to decrease the volume ileostomy Capsule, Loperamide 2 mg.
discharge. 2 mg – 10’s.
Suspension, Loperamide 2 mg per 5 mL.
Contra-indications: Child under 2 years;
Pack: 30 mL.
acute dysentery; acute ulcerative colitis or
pseudomembranous colitis associated with OTC IMODIUM® (Janssen-Cilag)
broad-spectrum antibiotics; conditions in Capsule, Loperamide HCl 2 mg.
which inhibition of peristalsis should be 2 mg – 6; 240.
avoided such as acute diarrhoea due to inges- OTC LERAMIDE® (Lifeback)
tion of poison. Capsule, Loperamide (as HCI) 2 mg.
Precautions: Infants (approprate fluid and 2 mg – 10 x 10’s (in blisters).
electrolyte replacement therapy should be OTC LODIUM® (Vixa)
given); acute diarrhoea (discontinue therapy Capsule, Loperamide 2 mg
if no improvement within 48 hours); hepatic 2 mg – 1 x 10’s
dysfunction (monitor closely for CNS toxicity); OTC LOMEDIUM® (Neros)
pregnancy, breast-feeding. Capsule, Lopermide HCl 2 mg.
Interactions: CNS depressants, phenothi- 2 mg – 2 x 10’s (in blisters).
azines, TCAs may ptentiate the adverse effects.
EMDEX
OTC LOPESHAL® (Shalina)
Adverse effects: Hypersensitivity reactions
Tablet, Loperamide HCI 2 mg.
(including skin rash); abdominal pain, dis- 2 mg – 25 x 6’s.
tension or discomfort; nausea and vomiting;
constipation, tiredness, drowsiness, dry mouth. POM LOPRAD® (Seagreen)
Advice to patients: Do not take more than 8 Capsule, Loperamide HCI 2 mg; hard gelatin cap
2 mg – 10 x 10’s
capsules in 24 hours; may cause drowsiness.
Nursing action: Relieve dry mouth with sips POM LOPRAZAR® (Shrezar)
of water, hard candy. Capsule, Loperamide HCl 2 mg; hard-gelatin cap
• Therapy for chronic diarrhoea should not Pack: 1 x 10’s (in blisters)
exceed 10 days; if acute diarrhoea lasts longer POM PALOMIDE® (Mark)
than 48 hours, discontinue therapy and con- Capsule, Loperamide HCI 2 mg
sult physician. 2 mg – 1 x 10's
• Advise patient to avoid driving or operating OTC RGI Loperamide® (GoldMoore)
machinery if he feels dizzy or drowsy. Capsule, Loperamide 2 mg.
• Monitor children for signs of dehydration, 2 mg – 10’s.
CNS problems.
Dose: Acute diarrhoea, Adult, by mouth, 4.4.4 Adsorbents and bulk-
initially 4 mg, followed by 2 mg after forming drugs
each loose stool; Child (>5 years), by Kaolin and Pectin are adsorbents and their
mouth, 2 mg, followed by 2 mg after action is through their ability to adsorb com-
each loose stool. pounds from solution, presumably binding
Chronic diarrhoea, Adult and child (>5 potential intestinal toxins.
years), by mouth, initially 4 mg daily Attapulgite is a magnesium aluminium
(2 mg for child); adjusted between phyllo-silicate; it is an adorbent used in com-
2-12 mg daily until 1-2 solid stools a bination with pectin in certain ant-diarrheal
day are obtained. preparations.
Maximum dose for acute and chronic
diarrhoea is 16 mg (8 capsules) daily ATTAPULGITE plus PECTIN
for adult and for a child, 6 mg (3 Indications: Symptomatic treatment of non-
capsules) per 20 kg b. wt. specific diarrhea.
OTC Loperamide (EDL 20.6.3) Contra-indication: Constipation
Tablet, Loperamide 2 mg. Adverse effects: Large doses may cause fecal
Capsule, Loperamide 2 mg impaction.
OTC CIKADIUM® (Michelle Lab)
Dose: Adult & Child >12 years, 2 tablets
Capsule, Loperamide HCI 2 mg following each defecation (max. 12
2 mg – 6’s (in blisters) tabs/day); Child 6-12 years, 1 tablet
162 | 4.4.5 Antidiarrheal microorganisms 4.5 Laxatives | 163
following each defecation (max. 6 Suspension, Light kaolin 2 g, light mag. carbonate directly or mixed with water or beverage. Avoid 0.25-1 hour (rectal). It is metabolised in the liver
tabs/day) 500 mg, sodium bicarbonate 500 mg per 10 mL; mixing in hot liquids or liquids which contain alcohol. and the conjugated metabolites are excreted
cream susp. For continous enteral feeding, the drug may be added in milk, bile and urine.
OTC NEO ENTROSTOP® (Orange Drugs) Pack: 200 mL glass bottle. to the nutrient solution at the time of preparation.
Tablet, Activated colloidal attapulgite 650 mg, Indications: Treatment of constipation (pre-
Pectin 50 mg. OTC NEIPEC® (Neimeth) ferred for constipation caused by narcotic
Suspension, Kaolin light 1 g per 5 mL. 4.5 Laxatives analgesics); bowel clearance before surgery,
OTC DIAPET® Plus (Maxim) Pack: 60 mL. A balanced diet, including adequate fluid labour or radiological examination.
Capsule, Attapulgite 42%, active carbon 10%, Psidii
folium extract (guava leaves) 10%, Curcumee do- intake and fibre is of value in preventing Contra-indications: Abdominal pain, nausea,
SULPHAGUANIDINE plus constipation. vomiting, or other symptoms of appendicitis
mesticee rhizoma extract (Turmeric rhizome) 8%, NEOMYCIN plus KAOLIN
Coicis semen (Coix seed) 17%, Chebulae fructus Before prescribing laxatives, it is important or acute surgical abdomen; rectal fissures or
Therapeutic category: Antidiarrhoeal
extract (Tropical almond fruit) 3%, Granati peri- to be sure that the patient is constipated and ulcerated haemorrhoids; intestinal obstruction.
Indications: Diarrhoea of bacteria origin,
carpium extract (Pomegranate fruit peel) 3% and that the constipation is not secondary to an Precautions: Children, abdominal pain,
other additives to 100%. gastroenteritis and food poisoning.
underlying undiagnosed complaint. It is also pregnancy.
Indications: Diarrhoea; to decrease frequency Contra-indications: Ulcerative colitis, intesti-
important that the patient understands that Interactions: Milk, antacids (decreased effect).
of bowel movement, adsorb toxins. nal obstruction.
bowel habit can vary considerably in frequency Decreased effect of warfarin.
Dose: Adult, 2 capsules 2 times daily Precautions: Prolonged use may cause over-
without doing harm. For example some people Adverse effects: Mild abdominal cramps,
Acute diarrhea, 2 capsules 2 times growth of non-susceptible micro-organisms.
consider themselves constipated if they do not nausea, vomiting, rectal burning, vertigo,
with 1 hour interval. Not recom- Dose: Adult and child (>12 years), by mouth,
have a bowel movement each day. A useful electrolyte and fluid imbalance.
mended for children <5 years. initially 30 mL, followed by 15 mL 4
definition of constipation is the passage of hard Advice to patients:To be swallowed whole
times daily.
stools less frequently than the patient’s own without sucking, chewing or breaking.
KAOLIN Child (<12 years): See lit.
normal pattern and this should be explained to Nursing action:
EMDEX
Indications: Mild chronic diarrhoea. POM IVAX® (BCN) the patient since misconceptions about bowel • Increased pH may dissolve the enteric coating
Contra-indications: Obstructive bowl lesions. Suspension, Sulphaguanidine 0.7 g, Neomycin sul- leading to GI distress; do not crush or chew enteric
habits have led to excessive laxative use which coated drug product. Administer tablets 2 hours
Adverse effects: Constipation. fate 53.33 mg, Light kaolin 1.05 g per 5 mL.
Pack: 60 mL in turn has led to hypokalaemia. prior to, or 4 hours after antacids.
Nursing action: Administer after shaking
suspension. Laxatives should generally be avoided except • Insert suppository as high as possible into the
• Do not use for more than 2 days; not a 4.4.5 Antidiarrheal microorganisms where straining will exacerbate a condition rectum; position against the rectal wall, not
replacement for specific therapy for the Saccharomyces boulardii is a tropical strain such as angina or increase the risk of rectal embedded in faecal matter because it may
underlying cause. of yeast which has been shown to maintain bleeding as in haemorrhoids. Laxatives are of cause delay in onset of action.
• May reduce absorption of other PO drugs; and restore the natural flora in the large and value in drug-induced constipation, for the • Teach patient to use for short term treatment
separate administration times by at least 2 small intestine. It is classified as a probiotic expulsion of parasites after anthelminthic and prevent abuse; prolonged use may cause
hours. used in treating diarrhea of various etiology. treatment and to clear the alimentary tract loss of bowel tone.
Dose: Adult, 30 mL every 4-6 hours. Probiotics are dietary supplements contain- before surgery and radiological procedures. • Tell patient that dietary intake of bulk found
Child, 5-30 mL every 4-6 hours. ing potentially beneficial bacteria or yeasts. Prolonged treatment of constipation is some- in cereals, fresh fruits and vegetables improve
S. boulardii has been shown to be non-path- times necessary. bowel movement.
OTC DIAMIX® (Gauze) • Onset of action is 6-10 hours (oral) and 25
Liquid, Light kaolin 1.6 gm per 10 mL ogenic, non-systemic (remains in the GI tract), There are many different laxatives. These
and grows at the unusually high temperature include bulk-forming laxatives which relieve to 60 minutes (rectal); time administration
Pack: 60 mL; 2 L
of 37°C. It is available as a probiotic in a ly- constipation by increasing faecal mass and of drug so as not to intefere with scheduled
POM DIASTOP® (Afrab-Chem) activities or sleep.
ophilized form. stimulating peristalsis, stimulant laxatives
Suspension, Kaolin light 200 mg. • Inform patient not to use medication if symp-
Pack: 100 ml OTC FLORANORM® (Phillips/Prisma)
which increase intestinal motility and often
cause abdominal cramp, faecal softeners toms of appendicitis occur namely abdominal
Dose: Adult & child >12 years: 15-30 ml every 4-6 Oral powder, Saccharomyces boulardii 250 mg; in
which lubricate and soften impacted faeces pain, nausea, vomiting.
hours; 6-12 years, 10-15 ml every 4-6 hours; sachet.
3-6 years, 5-10 ml every 4-6 hours; <3 years, and osmotic laxatives which act by retaining Dose: By mouth, Adult, 10 mg at night;
Pack: 10 sachets.
not recommended. fluid in the bowel by osmosis. Bowel cleansing increased to 15-20 mg if necessary.
Indications: Treatment of diarrhoea, Travel-
solutions are used before colonic surgery, Child: 5 mg.
OTC Galways ADM (SKG) ler’s diarrhoea, viral diarrhoea in children and
colonoscopy or radiological examination to By rectum, Adult, 10 mg in the morn-
Suspension, Light kaolin 6 g, diarex 250 mg per 30 antibiotic associated diarrhoea; Treatment of
ensure that the bowel is free of solid contents; ing. Child: 5 mg.
mL; white fruit flavoured susp. irritable bowel syndrome; Treatment and pre-
Pack: 60 mL in amber bottle. vention of digestive complications following they are not a treatment for constipation. OTC Bisacodyl (EDL 20.5)
Dose: By mouth, Adult, 30 mL; Child (<3 years), 2.5 antibiotic therapy; diarrhoea, colitis, candidi- Tablet, Bisacodyl 5 mg.
mL; 3-6 years, 10 mL; 6-12 years, 15ml. asis; Prevention of diarrhoea during continous BISACODYL Suppositories, Bisacodyl 5 mg, 10 mg.
To be taken at half-hourly intervals until
enteral feeding in adults; Prevention of vaginal Therapeutic category: Stimulant laxative. OTC APO-BISACODYL® (Lahams)
symptoms abate; usually 3-4 doses should
be sufficient. Shake before use.
yeast infections. Pharmacology: Stimulates persistalsis by Tablet, Bisacodyl 5 mg; yellow e-c tab. marked ‘5’.
Contra-indications: Antifungal antibiotics, directly irritating the smooth muscle of the 5 mg – 1000.
OTC Moko Mist Kaolin (New Healthway) quinoline derivatives. intestine, possibly the colonic intramural OTC Bisacodyl (Alpha)
Suspension, Light kaolin 1000 mg, sodium bicar- Adverse effects: Occasional flatulence. plexus; alters water and electrolyte secretion Suppository, Bisacodyl 10 mg
bonate 250 mg, light magnesium carbonate 250
Dose: Adult & child, by mouth, 1-2 sachets producing net intestinal fluid accumulation 10 mg – 10 x 12’s
mg per 5 mL.
twice daily. and laxation. Less than 5% is absorbed system-
OTC BISCOLAX® (Adler)
OTC Nomagbon Kaolin (Nomagbon) Directions for use: May be taken before or after food, ically. Onset of action is 6-10 hours (oral) and
164 | 4.5 Laxatives 4.6 Antiemetic drugs | 165
Tablet, Bisacodyl 5 mg; e–c tab. Indications: Constipation. component. kalaemia (with prolonged use or overdosage).
5 mg – 100. Contra-indications: Appendicitis, faecal im- Precautions: Renal impairment, elderly. Nursing action: Before giving for constipa-
OTC CONLAX® (Greenlife) paction, intestinal obstruction or perforation. Advice to patients: Dilute dose in water or tion, determine if patient has adequate fluid
Suppository, Bisacodyl USP 10 mg. Avoid enema in children under 2 years. juice, shake well. intake, exercise and diet; tell patient about
10 mg – 5’s. Precautions: Elderly or debilitated patients Nursing action: Shake suspension thoroughly; dietary sources of bulk including fresh fruits
OTC MEDLAX® (Embassy)
(due to susceptibility to lipid pneumonitis give with at least a glass of water. and vegetables.
Tablet, Bisacodyl 5 mg. through aspiration, absorption, and trans- • Encourage patient to take adequate fluids, • Use for short-term treatment because drug
5 mg – 10’s. port from intestinal mucosa); children, rectal exercise and increased bulk in diet (viz fresh is very potent and gives thorough, strong
bleeding. fruits and vegetables). bowel action 6-10 hours after administration.
LACTULOSE Adverse effects: Nausea, vomiting, diarrhoea • Warn patient that frequent or prolonged use • Give oral dose in the morning or evening;
Therapeutic category: Osmotic laxative. in excessive use; abdominal cramps; decreased may cause dependence, or loss of bowel tone. cramping, rectal bleeding, nausea, vomiting
Indications: Chronic constipation, regulation absorption of nutrients and fat-soluble vi- • Don’t give oral drugs 1 to 2 hours before or may be due to overdosage (discontinue drug).
of bowel movement, in case of abuse of tamins. after administration of magnesuim hydroxide. • Teach patient that faeces and urine may turn
laxative, constipation in liver disease and par- Nursing action: Give with fruit juices or car- • Onset of action is 4-8 hours; time adminis- yellowish brown in colour.
aplegia, anal fissures and hemorrhoids, chronic bonated drinks to disguise taste preferably tration of drug so as not to interfere with • Patient should not use in the presence of of
liver disease (cirrhosis of the liver), hyperam- at bedtime. scheduled activities or sleep. symptoms of appendicitis namely abdominal
moniemia, porto-systemic encephalopathy, • May delay passage of food from stomach (do Dose: By mouth, constipation, Adult, 15-60 pain, nausea and vomiting.
salmonella carriers; as a prophylactic against not give with meals or immediately after); mL. Child (2-6 years), 5-15 mL. • Notify the physician if constipation is not
infection by pathogenic strains of E. coli. more effective on an empty stomach. relieved or if symptoms of electrolyte imbal-
Contra-indications: Intolerance to the galac- • Encourage patient to take adequate fluids, MAGNESIUM SULFATE ance occur viz muscle cramps, pain, weakness,
tose, lactose and suspected ileus. exercise and increased bulk in diet (viz fresh Synonym: Epsom Salts dizziness and excess thirst.
EMDEX
Precautions: Diabetics (75 mL contains about fruits, vegetables, cereals). Therapeutic category: Saline Laxative; Dose: Constipation, by mouth, ADULT
3 g of lactose); Pregnancy, lactation. Dose: By mouth, Constipation, Adult, 15-30 Antacid. 2–4 tablets, usually at night; initial
Adverse effects: Meteorism and flatulence mL. Pharmacology: Magnesium sulfate is a saline dose should be low, then gradually
may occur during the initial days of the treat- By rectum, 60-150 mL as enema per laxative. When taken by mouth in dilute solu- increased; CHILD over 6 years, half
ment (for about 3 days). day. Child, 5-15 mL at bedtime or 30- tion it reduces the normal absorption of water the adult dose in the morning (on
Dose: By mouth, Constipation, Adult, initially 60 mL as enema per day. from the intestine with the result that the bulky doctor’s advice).
Note: Avoid enema in children under 2 years. fluid contents distend the bowel, active reflex
15-30 mL daily. Maintenance: 10-15 OTC Senna (WMF 17.6)
mL daily. OTC Liquid Paraffin (EDL 20.5) peristalsis is excited, and evacuation of the Tablet, total Sennosides (calculated as Sennoside
Child (≤ 14 years): initially 5-15 mL Oral emulsion, Liquid Paraffin 5 mL per 10 mL contents of the intestine follows. B) 7.5 mg.
daily. Maintenance: 5-10 mL daily Indication: Rapid bowel evacuation.
OTC Liquid Paraffin (Nomagbon) OTC Senna (EDL 20.5)
Infants: initially 5-15 mL daily. Mainte- Liquid, Paraffin; colourless liquid Contra-indications: See under Mg(OH)2. Tablets and Granules
nance: 5 mL daily Pack: 200 mL. Precautions: Renal and hepatic impairment,
Cirrhosis of the liver, initially 30-45 mL elderly, use only occasionally. 4.6 Antiemetic drugs
OTC Moko Liquid Paraffin (New Healthway)
every 1-2 hours until desired laxative Advice to patients and Nursing action: See
Liquid, Liquid Paraffin BP; clear colourless viscous Metoclopramide has antiemetic properties
effect is achieved. Maintenance: 30- liquid.
under Magnesium Hydroxide.
Dose: 5 – 10 g in a tumblerful of water or and also stimulates upper gastrointestinal
45 mL 3-4 times daily. Pack: 200 mL.
10-20 mL, followed by a tumblerful of motility. Metoclopramide is effective against
Disturbed intestinal flora (with long-
water, preferably before breakfast. nausea and vomiting associated with GI
term antibiotic use), Adult, 15-30 mL MAGNESIUM HYDROXIDE
disorders or migraine, following surgery and
daily. Child: 5-10 mL daily. Synonym: Milk of Magnesia; MOM; Magnesia OTC ANDREW’S LIVER SALT® (GSK) chemotherapy and is also effective against
POM LACTOBER® (CG Biostadt) Magma. Granules (effervescent), Magnesium sulfate 5 g per
radiation-induced nausea and vomiting. Com-
Syrup, Lactulose syrup BP 68% w/v. Therapeutic category: Saline Laxative; sachet
Pack: 10; 50.
bining metoclopramide with corticosteroids
Pack: 120 mL. Antacid. (such as dexamethasone) can improve its
POM OSMOWIN® (Phillips) Pharmacology: Promotes bowel evacuation OTC Moko Epsom Salt (New Healthway) antiemetic effect in chemotherapy-induced
Syrup, Lactulose concentrate equiv. to lactulose 10 by causing osmotic retention of fluid which Powder, Magnesium sulfate 25 g per satchet. nausea and vomiting.
g per 15 mL distends the colon with increased peristaltic OTC Moko Mist Alba (New Healthway) Metoclopramide may be useful in the man-
Pack: 100 mL; 200 mL (with measuring cups) activity; reacts with hydrochloric acid in the Suspension, Magnesium sulfate 80 g. agement of gastro-oesophageal reflux and
stomach to form magnesium chloride. Onset of gastroparesis, as well as preoperatively in the
LIQUID PARAFFIN laxative action is 4-8 hours. The absorbed mag- SENNA prevention of aspiration syndromes. It is also
Pharmacology: Liquid paraffin is a mineral nesium ions (up to 30%) are usually excreted by Therapeutic category: Stimulant laxative. used to facilitate intubation of the small bowel
oil which is minimally absorbed by the GIT. It kidneys, unabsorbed drug is excreted in faeces. Indications: Constipation; acts in 8–12 hours. during radiographic examinations. Metoclo-
is a lubricant laxative. It mixes with and coats Indications: Short-term treatment of occa- Contra-indications: Intestinal obstruction; pramide is not effective in the prevention or
the intestinal contents, preventing colonic sional constipation and symptoms of hyper- undiagnosed abdominal symptoms. treatment of motion sickness.
reabsorption of faecal water and increasing acidity. Precautions: Avoid prolonged use unless Metoclopramide may cause acute dystonic
water retention in the stool. This leads to the Contra-indications: Colostomy or ileostomy, indication for prevention of faecal impaction; reactions with facial and skeletal muscle
formation of soft oily faeces. Onset of action intestinal obstruction, faecal impaction, renal breastfeeding (Appendix 3). spasms and oculogyric crises. These reactions
is 6-8 hours. failure, appendicitis, hypersensitivity to any Adverse effects: Abdominal discomfort; hypo- are most common in the young (especially girls
166 | 4.6 Antiemetic drugs 4.6 Antiemetic drugs | 167
and young women) and the elderly; they occur Interactions: May potentiate the sedative impairment, severe renal insufficiency. Pack: 1 x 10’s; 3 x 10’s
shortly after the start of treatment and subside effects of CNS depressants and alcohol. Interactions: Anticholinergic drugs (may an- POM OMIT-D® (Micronova)
within 24 hours of drug withdrawal. Adverse effects: Somnolence and GI distur- tagonise the anti-dyspeptic effect of domperi- Capsule, Omeprazole (as e-c granules) 20 mg, Dom-
Promethazine is a phenothiazine that in bances; allergic skin reactions; fatigue; extrap- done). Antacids may lower oral bioavailability iperidone (as pellets) 10 mg
addition to D2 dopaminergic blockade has yramidal symptoms in the elderly (reduce dose of domperidone. Indications: Dyspepsia, gastro-oesophageal reflux
pronounced histamine H1 and muscarinic or discontinue). Adverse effects: Transient intestinal cramps;in- disease (GERD/GORD).
receptor blocking properties. It is effective in Advice to patients: May cause drowsiness. crease in the plasma prolactin level which may Dose: 1 capsule twice a day.
the prevention and treatment of vertigo and ability to opoerate machinery and drive may cause galactorrhoea and gynaecomastia; rarely
motion sickness. Promethazine may be useful be impaired. Avoid alcoholic beverages. To be allergic reactions such as rash and urticaria. DOMPERIDONE plus RABEPRAZOLE
in the prevention and treatment of postoper- taken preferably after meals. Dose: Post-prandial stomach discomfort, See under the preparations below.
ative and drug-induced nausea and vomiting. Dose: Vestibular disorders, 25 mg 3 times Adult & Child ≥16 years, Up to 10 mg
It has limited effect on chemotherapy-induced daily or 75 mg once daily. 3 times daily and at bedtime. Maxi- POM PERBLOC-DSR® (Tamar & Pharez)
mild to moderate emesis. To be taken half an hour before mum duration of course of treatment Caplet, Rabeprazole 20 mg, domperidone 30 mg
Chlorpromazine has a powerful sedative and travelling and to be repeated every 2 weeks. Pack: 10 x 1 x 10's.
antiemetic action, the latter probably mediated 6 hours if necessary in prophylaxis of Nausea and vomiting, Adult & Child Pharmacology: See under Domperidone and
by the chemoreceptor trigger zone. It is of motion sickness. ≥16 years, Up to 10 mg 3 times daily Rabeprazole.
Indications: GERD; Dyspepsia; Nausea associated
particular value in the treatment of vomiting See lit. for other indications and doses. and at bedtime. Maximum duration
with acid peptic disorders (APDs).
associated with uraemia, radiation sickness POM STUGERON® (Janssen-Cilag)
of course of treatment 48 hours. Contra-indications: Hypersensitivity to rabeprazole,
and disseminated malignant disease, where Tablet, Cinnarizine 25 mg. Children <16 years: Not recom- domperidone, or substituted benzimidazoles; Severe
its sedative property may also be appropriate. 25 mg – 50. mended. hepatic and/or renal impairment, prolactin-releasing
It is ineffective in motion sickness. Capsule, (forte), Cinnarizine 75 mg; red/yellow cap. Note: Oral doageforms should be taken before pituitary tumour (prolactinoma). Avoid in conditions
EMDEX
Cyclizine is a histamine H1-receptor antagonist 75 mg – 20. meals. If taken after meals absorption of the drug when stimulation of the gastric motility could be
which causes less sedation than promethazine can be delayed. Reduce dose in renal insufficiency. harmful, like gastrointestinal hemorrhage, mechani-
and has anti–motion sickness activity. It is ef- DOMPERIDONE (Updated based on Motilium monograph available from: http:// cal obstruction or perforation. Severe hepatic or renal
www.medicines.org.uk/) dysfunction; Pregnancy and breastfeeding.
fective in nausea and vomiting of other causes Warnings: Cardiac effects of Domperidone: Domperi- Precautions: Hepatic or renal dysfunction.
such as vertigo and nausea associated with done use may be associated with an increased risk of se- Interactions: Drugs that depend on gastric pH for
POM MOTILIUM® (Janssen-Cilag)
Meniere’s disease. rious ventricular arrhythmias or sudden cardiac death. Tablet, Domperidone 10 mg; f-c tab. absorption e.g. ketoconazole. Anticholinergic drugs
Like cyclizine, meclozine is an antihistamine The risk may be higher in patients older than 60 years 10 mg – 30. may decrease the effect of domperidone. Azole
with anti–motion sickness activity. It is less and at daily doses of more than 30 mg. Domperidone antifungals and macrolides.
sedative than promethazine and is usually should be used at the lowest effective dose in adults and POM REAMOTIL® (Reals) Adverse effects: Headache, abdominal pain, diar-
children. Use of domperidone and other drugs which Suspension, Domperidone 1 mg per mL; flavoured rhea, flatulence, constipation, dry mouth, dizziness,
available in combination with pyridoxine.
prolong QTc intervals requires that caution be exercised syrup base. rash, peripheral edema. Rarely increased prolactin
Prochlorperazine is a phenothiazine indicated Pack: 30 mL.
in patients who have existing prolongation of cardiac levels.
in the prophylaxis and treatment of vertigo
conduction intervals, particularly QTc, patients with Dose: Adult, by mouth, 1 capsule per day. To be
and nausea associated with Meniere’s disease. significant electrolyte disturbances or underlying cardiac DOMPERIDONE plus OMEPRAZOLE swallowed whole, before breakfast in the
It is used in both acute and chronic forms of diseases such as congestive heart failure. morning.
vertigo. See under the preparations below.
Ondansetron is a potent, highly selective Therapeutic category: Antinauseant; Proki-
netic agent POM LIMZER® (Mega Lifesciences) ITOPRIDE
5–HT3 (Serotonin) receptor–antagonist. Acti-
Pharmacology: Domperidone is a dopamine Capsule, Omeprazole (as e-c pellets) 20 mg, Dom- Therapeutic agent: Antiemetic; Prokinetic
vation of these 5–HT3 receptors in both the peridone (as s-r pellets) 30 mg.
antagonist with anti-emetic properties similar agent
peripheral and CNS by chemotherapeutic Pack: 10 x 10’s; 3 x 10’s
to those of metoclopramide and phenothi- Pharmacology: Itopride activates gastrointes-
agents and radiotherapy initiates a vomiting Indications: Enteric coated Omeprazole and
azines. Unlike these other drugs, however, tinal propulsive motility due to its dopamine D2
reflex. Ondansetron blocks the initiation of Domperidone capsules combines omeprazole,
domperidone does not readily cross the blood antagonizing activity and acetyl cholinesterase
this reflex. a proton pump inhibitor which inhibits the
– brain-barrier and hence, is less likely to cause inhibitory activity. Itopride activates acetylcho-
secretion of acid in the stomach and domperi- line release and inhibits its degradation.
CINNARIZINE central effects such as sedation and dystonic
done, a dopamine antagonist which works as Indications: Functional dyspepsia, non-ulcer
Indications: Vestibular disorders such as ver- reactions. It acts at the chemoreceptor trigger
an upper gatrointestinal prokinetic agent. It is dyspepsia (chronic gastritis) i.e. sensation of
tigo, tinnitus, giddiness, nausea, and vomiting zone and so is unlikely to be effective in motion
useful in the treatment of gastroesophageal bloating, early satiety, upper abdominal pain
in Meniere’s syndrome; prophylaxis of motion sickness and other vestibular disorders.
reflux disease (GERD) and dyspepsia caused or discomfort, anorexia, heartburn, nausea
sickness; vascular spasms and arteriosclerosis Indications: Post-prandial symptoms of full-
by gastroparesis and gastro-esophageal reflux. and vomiting.
as in Raynaud’s disease, vascular headache, ness, nausea, epigastric bloating and belching
Formulation of Domperidone (30 mg) as Contra-indications: Hypersensitivity to Ito-
migraine. that is occasionally accompanied by epigastric
sustained release pellets enables once daily pride or any of the excipients. Avoid use in
Contra-indications: Hypersensitivity to the discomfort and heartburn. Nausea and vomit-
administration of the drug. conditions where increase in GI motility could
drug or any component; porphyria. ing of less than 48 hours duration.
Dose: Adult: One capsule once daily before be harmful e.g. GI hemorrhage, mechanical
Precautions: Pregnancy, breast-feeding; el- Contra-indications: GI haemorrhage, mechan-
meal. obstruction or perforation.
derly (may suffer extrapyramidal symptoms on ical obstruction or perforation; prolactinoma
(prolactin-releasing pituitary tumour); preg- POM OMEDOM® (Nalis) Precautions: Itopride enhances the action of
prolonged therapy); hypotension (high doses); acetylcholine and may produce cholinergic
nancy, breastfeeding. Capsule, Omeprazole (as e-c pellets) 20 mg, domi-
somnolence may occur at the start of therapy. peridone (as f-c pellets) 10 mg side effects. Pregnancy, elderly.
Precautions: Infants under 1 year, hepatic
168 | 4.6 Antiemetic drugs 4.6 Antiemetic drugs | 169
Interactions: Due to its gastrokinetic effects, beverages. POM METOPRONE® (Beta Drugs) Elderly, as for younger adults
it may influence the absorption of co-admin- Nursing action: Administer about 30-60 min Injection, Metoclopramide HCl BP 5 mg per per mL; Child (>4 years), by slow IV injection
istered oral drugs esp. drugs with a narrow before meals for better absorption. in 2-mL amp. or by IV infusion over 15 minutes, 5
therapeutic index, sustained-release or enter- • Relieve dry mouth with frequent sips of water, Pack: 2-mL x 10’s; 2-mL x 100’s mg/m2; then, 4 mg by mouth every 8
ic-coated formulations. Anticholinergic drugs gum, hard candy. POM PEZOL® (Pemason) hours for up to 5 days.
may antagonize some of its effects. • Advise patient to avoid harzadous activities Injection, Metoclopramide 5 mg per mL; in 2-mL
POM ALFASETRON® (Alpha)
Adverse effects: Diarrhoea, constipation, until stabilised on medication; alcohol, other amp. marked “Pezol”.
Tablet, Ondansetron 8 mg; yellow oblong tab.
abdominal pain, increased saliva and nausea; CNS depressants that may increase sedative Pack: 2-mL x 10 x 10’s
Injection, Ondansetron 2 mg per mL; aqueus solution
dizziness, headache and tremor; rash, redness effects of the drug. POM SIVOPRAMIDE® (Adpharm) for injection in 4 mL amp.
and itching; jaundice, leukopenia and thrombo- • Notify physician if involuntary movements Injection, Metoclopramide 10 mg per 2 mL.
POM ONSTRON® (Shrezar)
cytoopenia; anaphylactoid reaction; increased occur. Pack: 1 x 100’s.
Injection, Ondansetron ( as HCl) 2 mg per mL
prolactin level and gynecomastia. Dose: Nausea and vomiting, gastro-oesoph- Pack: 5 amp x 4 mL
Dose: Adult, by mouth, 50 mg 3 times daily ageal reflux, gastroparesis, by mouth ONDANSETRON
Therapeutic category: Antiemetic. POM OSETRON® (Phillips/Dr. Reddy’s)
Take at least 1 hour before meals or by IM injection or by slow IV
Tablet, Ondansetron (as HCl) 8 mg; f-c tab.
Elderly: May reduce dose injection (over 1–2 minutes), ADULT Indications: Nausea and vomiting induced
8 mg – 10’s.
POM DYNETIC® (Biostadt)
10 mg 3 times daily; YOUNG ADULT by cytotoxic chemotherapy and radiotherapy; Injection, Ondansetron (as HCl) 2 mg per mL; in 4
Tablet, Itopride HCI 50 mg 15–19 years (under 60 kg) 5 mg 3 post–operative nausea and vomiting (PONV). mL amp.
50 mg – 10’s times daily; CHILD up to 1 year (up Precautions: Pregnancy and breast–feeding. Pack: 4 mL x 1’s.
to 10 kg) 1 mg twice daily, 1–3 years Adverse effects: Constipation, headache, a
POM SETRONAX® (Strides Vital)
METOCLOPRAMIDE (10–14 kg) 1 mg 2–3 times daily, 3–5 sensation of flushing or warmth in the head Injection, Ondansetron 2 mg per mL; in 4 mL amp.
Therapeutic category: Antiemetic; Prokinetic years (15–19 kg) 2 mg 2–3 times daily, and epigastrium; occasional alteration in liver Pack: 4 mL x 5’s.
EMDEX
agent. 5–9 years (20–29 kg) 2.5 mg 3 times enzymes; rarely hypersensitivity reactions.
daily, 9–14 years (30 kg and over) 5 Dose: Adult, Highly Emetogenic chemother- POM ZOFRAN® (GSK)
Indications: Nausea and vomiting in GI dis- Tablets, Ondansetron HCl 4 mg, 8 mg; both are
orders and treatment with cytotoxics (section mg 3 times daily (usual max. 500 µg/ apy, e.g., regimens containing cisplatin:
yellow, oval, f–c tabs marked ‘GLAXO’ on one face,
12.1) or radiotherapy; gastro-oesophageal kg daily, particularly for children and Initially by slow IV injection or 15 and ‘4’ and ‘8’ respectively on the other.
reflux; gastroparesis; premedication and post- young adults minute infusion of 8 mg immediately Injection, Ondansetron HCl 2 mg per mL; aqueous
operatively; aid to GI intubation; nausea and Premedication, by slow IV injection, before chemotherapy, followed by a solution in 2 mL and 4 mL amps.
vomiting in migraine (section 1.9). ADULT 10 mg as a single dose. continuous IV infusion of 1 mg/hour
NOTE: In children (and in some countries, pa- Aid to GI intubation, by mouth or by for up to 24 hours or by a further two PROCHLORPERAZINE
tients under 20 years) use restricted to severe IM injection or by slow IV injection, doses of 8 mg given by slow IV injec- Therapeutic category: Antiemetic; Antipsy-
intractable vomiting of known cause, vomiting ADULT 10–20 mg as a single dose tion or 15 minute infusion four hours chotic Agent.
of radiotherapy and chemotherapy, aid to GI 5–10 minutes before examination; apart; then 8 mg by mouth every 8 Pharmacology: Prochlorperazine acts on the
intubation, premedication. YOUNG ADULT (15–19 years), 10 mg; hours for up to 5 days. chemoreceptor zone to inhibit nausea and
Contra-indications: GI obstruction, haemor- CHILD under 3 years 1 mg, 3–5 years Less Emetogenic chemotherapy, e.g., vomiting. See notes above.
rhage or perforation; 3–4 days after GI surgery; 2 mg, 5–9 years 2.5 mg, 9–14 years regimens containing cyclophospha- Indications: Vertigo due to Menier’s disease
convulsive disorders; phaeochromocytoma. 5 mg. mide, doxorubicin, carboplatin: By slow and other labyrinthe disorders, severe nausea
Note: High dose metoclopramide with cytotoxic IV injection or 15 minute infusion of
Precautions: Elderly, children and young and vomiting; migraine.
chemotherapy, see section 12.1. 8 mg, immediately before chemo-
adults; hepatic impairment (Appendix 5); renal Contra-indications: Comatose states, bone
impairment (Appendix 4); may mask underlying POM Metoclopramide (WMF 17.2) therapy, or 8mg by mouth 1-2 hours marrow depression, liver damage.
disorders such as cerebral irritation; avoid for Tablet, Metoclopramide HCl 10 mg. before chemotherapy; then 8 mg by Precautions: Undiagnosed and prolonged
3–4 days after GI surgery; pregnancy (Appen- Injection, Metoclopramide HCl 5 mg/mL; in 2-mL mouth every 8 hours for up to 5 days vomiting; warn patients of impaired judge-
ampoule. Radiotherapy induced Nausea & Vom-
dix 2); breastfeeding (Appendix 3); Parkinson ment and dexterity.
disease; epilepsy; depression; porphyria; POM Metoclopramide (EDL 20.2) iting: By mouth, 8 mg every 8 hours, Interactions: CNS depressants, alcohol, anal-
interactions: Appendix 1. Tablet, Metoclopramide (as HCl) 10 mg. the first dose to be taken 1-2 hours gesics,antihypertensives, antidepre – ssants,
Adverse effects: Extrapyramidal symptoms (es- Oral liquid, Metoclopramide (as HCl) 5 mg per 5 mL before starting radiotherapy; the du- anticonvulsants, antidiabetics.
pecially in children and young adults; see notes Injection, Metoclopramide (as HCl) 5 mg per mL; ration of treatment depends on the Adverse effects: CNS disturbances, anticholin-
in 2-mL amp. length of the course of radiotherapy.
above); tardive dyskinesias on prolonged use; ergic effects, allergic effects and extrapyram-
hyperprolactinaemia; drowsiness, restlessness, POM HEPDIN® (Justeen) Post-operative nausea and vomiting idal symptoms – occur rarely at low dosage.
dizziness, headache, diarrhoea, depression, Injection, Metoclopramide 10 mg per 2 mL. (PONV), Prevention, 4 mg as a single Advice to patients: May cause drowsiness.
hypotension and hypertension reported; rarely, Pack: 2 mL x 10’s. dose by slow IV injection at induction; ability to opoerate machinery and drive may
neuroleptic malignant syndrome; rashes, pruri- POM MEDERAX® (Vixa)
alternatively, 8 mg by mouth 1 hour be impaired. Avoid alcoholic beverages.
tus, oedema; cardiac conduction abnormalities Tablet, Metoclopramide (as HCl) 10 mg. prior to anaesthesia followed by 2 fur- Nursing action: Dilute oral solution with fruit
following IV administration; rarely methaemo- Syrup, Metoclopramide (as HCl) 5 mg per 5 mL ther 8 mg doses at 8 hourly intervals. juice, milk, carbonated drink, or water.
globinaemia (more severe in G6PD deficiency). Injection, Metoclopramide (as HCl) 5 mg per mL; Treatment, 4 mg as a single dose by • Give IM deep; avoid SC route. Do not mix with
Advice to patients: Advice to patients: May in 2-mL amp. slow IV injection other drugs in the same syringe.
cause drowsiness. ability to opoerate machin- POM Metoclopramide-10 (Embassy) There is no experience of PONV in • Observe closely for orthostatic hypotension
ery and drive may be impaired. Avoid alcoholic Injection, Metoclopramide HCl BP 10 mg per mL. children and limited experience in especially when given IV.
the elderly.
170 | 4.7 Antihaemorrhoidal drugs 4.8 Anti-inflammatory drugs | 171
• Avoid skin contact with oral solution or injec- absorption. and hamamelis with lubricants, vasoconstric- Dose: 1 suppository night and morning, and
tion, contact dematitis has occured. • Give IM deep into a large muscle mass and tors or mild antiseptics, in the form of topical after defecation.
• Warn patient that drug may cause drowsiness, rotate injection sites. Avoice SC route. ointments, creams and suppositories, are used Not recommended for children.
impair judgement and co-ordination. • IV dose must be diluted to a max. concentra- to provide symptomatic relief. Local anaesthet- POM ANUPROCT® (Pharma-Deko)
• Inform patient that drug may cause photo- tion of 25-50 mg/9 mL and infused at max. ics are included in some preparations to relieve Suppository, As above.
sensitivity, to avoid excessive sunlight. rate of 25 mg/2 minute. Rapid IV administra- pain. Corticosteroids may be combined in such
• Observe for extrapyramidal symptoms; advise tion may cause a transient fall in BP. preparations (but should only be used after OTC ANUSOL® (Bolar)
Rectal ointment, Bismuth subgallate 22.5 mg, bis-
patient to notify physician of involuntary • Coffee or tea may reduce drowsiness; give exclusion of infection); they are suitable for
muth oxide 8.75 mg, zinc oxide 107.5 mg
movements or feelings of restlessness. chewing gum or ice chips to relieve dry occasional short-term use, but prolonged use Pack: 25 g
Dose: By mouth, nausea and vomiting, acute mouth. can cause atrophy of the anal skin. Suppositories, Bismuth subgallate 59 mg, bismuth
attack, 20 mg initially then 10 mg Dose: Nausea and vomiting, by mouth, Anal and perianal pruritus, soreness and exco- oxide 24 mg, zinc oxide 296 mg
after 2 hours; prevention, 5-10 mg 2-3 ADULT 25 mg at night, increased riation occur commonly in patients suffering Pack: 10’s
times daily. to 50–75 mg at night or 25 mg 2–3 from haemorrhoids, fistulas, and proctitis.
Child (>10 kg), 0.25 mg/kg 2-3 times times daily if necessary; maximum, These conditions are best treated by applica- PREDNISOLONE plus CINCHOCAINE
daily. Not recommended for child 100 mg in 24 hours. Nausea and vom- tion of bland ointments, suppositories, and Indications: Local treatment of haemorrhoids,
<10 kg. iting, by deep IM injection or by slow dusting–powders. Adjustment of diet to avoid proctitis, anal fissures.
See lit. for details. IV injection (diluted to 2.5 mg/mL in hard stools is also helpful. Dose: Insert 1 suppository daily after a bowel
POM Prochlorperazine (EDL 20.2)
water for injections), ADULT 12.5–25 movement, for 5-7 days (in severe
mg, repeated at intervals of not less Bland Soothing Preparations contain mild as-
Tablets, Prochlorperazine (as maleate) 5 mg, 25 mg. cases initially 2-3 times daily)
than 4 hours (usual maximum, 100 tringents such as bismuth subgallate or oxide,
Oral liquid, Prochlorperazine (as mesylate) 5 mg Ointment, apply twice daily for 5-7
mg in 24 hours). zinc oxide, balsam peru may give symptomatic
per 5 mL days (3-4 times daily on 1st day if nec-
EMDEX
Injection, Prochlorperazine (as mesylate) 12.5 mg per Motion sickness, prevention, by mouth, relief in haemorrhoids.
essary), then once daily for a few days
mL; in 1-mL, 2-mL amps. ADULT 20–25 mg at bedtime on night Vasoconstrictors such as phenylephrine after symptoms have cleared.
before travel, repeated on the morn- may also be included in the preparations for
PROMETHAZINE POM SCHERIPROCT ® (Bayer Schering)
ing of travel if necessary; CHILD 2–5 haemorrhoids.
Suppository/Rectal Ointment, Prednisolone caproate,
Therapeutic category: Antiemetic; Antihista- years, 5 mg at night and on morning Vasoprotectives such as Diosmin are used in cinchocaine HCl.
mine, H1 Blocker; Sedative. of travel, if necessary; 5–10 years, 10 treating haemorrhoids (see section 5.8). Pack: 12 Suppositories/Pack; 10 g Ointment/tube.
Indications: Nausea, vomiting, labyrinthine mg at night and on morning of travel,
disorders, motion sickness; premedication if necessary. Local Anaesthetics are used to relieve pain POM PROCTO-GLYVENOL® (Novartis)
associated with haemorrhoids, and pruritus Suppository, Tribenoside 400 mg, lignocaine HCI
(section 3.2). POM Promethazine (WMF 17.2) ani. They include lignocaine and pramoxine. 40 mg.
Contra-indications: Porphyria; child under 2 Tablets, Promethazine HCl 10 mg, 25 mg Rectal cream, Tribenoside 5%, lignocaine HCI 2%.
years (risk of respiratory depression). They should not be used for longer than 2
Oral liquid, Promethazine HCl 5 mg/5 mL. Pack: 30 g.
Precautions: Prostatic hypertrophy; urinary weeks since they may cause sensitisation of
Injection, Promethazine HCl 25 mg/mL; in 2-mL
retention; glaucoma; pyloroduodenal obstruc- ampoule. the anal skin.
DIOSMIN
tion; hepatic disease (Appendix 5); epilepsy; Corticosteroids such as Betamethasone and
POM Promethazine (EDL 20.2) See under section 5.8.
elderly and children (more susceptible to Tablets, Promethazine HCl 10 mg, 25 mg; or Promet- Hydrocortisone are often combined with anti-
adverse effects); pregnancy (Appendix 2); hazine theoclate 25 mg. biotics, local anaesthetics, and soothing agents
breastfeeding (Appendix 3); interactions: Oral liquid, Promethazine HCl 5 mg per 5 mL. for short–term use in haemorrhoids but not in 4.8 Anti-inflammatory drugs
Appendix 1. Injection, Promethazine HCl 25 mg per mL; in 1-mL, the presence of herpes infection.
Ulcerative colitis and Crohn disease are chronic
Adverse effects: Drowsiness, dizziness, seda- 2-mL amps.
Administration: Suppository should be in- inflammatory diseases of the intestinal tract.
tion (but paradoxical stimulation may occur, See Section 8.1 for the proprietary preparations of serted into the rectum night and morning and Effective management requires drug therapy,
especially with high doses or in children and Promethazine. after a bowel movement. attention to nutrition, and in severe or chronic
elderly); headache, nightmares, confusion,
Rectal Ointments and creams are applied night active disease, surgery.
psychomotor impairment; urinary retention,
dry mouth, blurred vision, GI disturbances; ex-
4.7 Antihaemorrhoidal drugs and morning and after a bowel movement, TREATMENT OF ACUTE ATTACKS OF ULCERA-
trapyramidal effects; hypersensitivity reactions; Haemorrhoids are enlarged or varicose veins externally or by rectum using a rectal nozzle. TIVE COLITIS AND CROHN DISEASE
rashes, photo-sensitivity reactions; jaundice; of the tissues at the anus or rectal outlet. They Acute attacks of mild to moderate severity
are the most frequent cause of rectal bleeding. HYDROCORTISONE plus ASTRINGENTS
blood disorders; cardiovascular adverse ef- (WITH OR WITHOUT LIDOCAINE) affecting the rectum (proctitis) or the rectosig-
fects—after injection; venous thrombosis at Anal and perianal pruritus, soreness and exco- moid (distal colitis) require local treatment with
site of IV injection; pain on IM injection. riation occur commonly in patients suffering Rectal suppository or ointment (EDL 20.3)
a corticosteroid (such as hydrocortisone) or
Advice to patients: May cause drowsiness, from haemorrhoids, fistulas and proctitis. an aminosalicylate (such as sulfasalazine).
impair judgement and coordination; may Careful local toilet with attention to any minor BENZYLBENZOATE plus BISMUTH More extensive disease or disease not respon-
cause photosensitivity, sunscreening agent faecal soiling, adjustment of the diet to avoid OXIDE plus BALSAM PERU B.P.C. sive to local treatment requires oral therapy;
plus RESORCINOL plus ZINC OXIDE
and protective clothing may be used; avoid hard stools, the use of bulk-forming materials plus BISMUTH SUBGALLATE an oral aminosalicylate alone can sometimes
excessive sunlight; notify physician of invol- such as bran and a high residue diet are helpful. Suppository, 33 mg + 24 mg + 49 mg + 24 mg + 296 be used in mild disease affecting the colon
untary movements or feelings of restlessness. Soothing preparations containing mild astrin- mg + 59 mg respectively. but addition of an oral corticosteroid for 4–8
Nursing action: Give with food or milk to gents such as bismuth subgallate, zinc oxide Indications: Haemorrhoids and other ano-rectal weeks is usually necessary. Because of the risk
reduce GI distress; food may slightly reduce conditions. of intestinal perforation, rectal administration
172 | 4.8 Anti-inflammatory drugs 4.9 Miscellaneous | 173
of hydrocortisone must be used with extreme HYDROCORTISONE BLOOD DISORDERS: Patients should be advised over 2 years, 40–60 mg/kg daily in
caution in patients with severe ulcerative dis- Indications: Ulcerative colitis, proctitis, proc- to report any unexplained bleeding, bruising, acute attack.
ease and should not be given to such patients tosigmoiditis; anaphylaxis (section 8); skin purpura, sore throat, fever or malaise occur- Ulcerative colitis, Crohn colitis, by
without conducting a thorough proctological (section 15.3); adrenocortical insufficiency ring during treatment; blood count should rectum (suppositories, used alone
examination. Severe extensive or fulminant (section 10.3) be performed and sulfasalazine stopped or in conjunction with oral therapy),
disease needs hospital admission and intra- Contra-indications: Use of enemas in bowel immediately if there is suspicion or evidence ADULT 0.5–1 g morning and evening
venous corticosteroid administration; other obstruction, bowel perforation, or extensive of blood disorder. after a bowel movement; By rectum
therapy may include IV fluid and electrolyte fistulas; untreated infections. Adverse effects: Nausea, headache, exacer- (retention enema), ADULT 3 g at night
replacement, blood transfusion, and possibly Precautions: Proctological examination re- bation of colitis; diarrhoea, loss of appetite, retained for at least an hour; CHILD
parenteral nutrition and antibacterials. quired before treatment; systemic absorption fever, blood disorders (including Heinz body not a suitable formulation.
Metronidazole may be beneficial in the may occur (see section 10.3); prolonged use anaemia, megaloblastic anaemia, leukopenia, POM Sulfasalazine (WMF 17.3)
treatment of active Crohn disease particularly should be avoided; pregnancy (Appendix 2); neutropenia, thrombocytopenia); hypersen- Tablet, Sulfasalazine 500 mg.
with perianal involvement, possibly through breastfeeding (Appendix 3); interactions: sitivity reactions (including rash, urticaria, Suppository, Sulfasalazine 500 mg.
its antibacterial activity. Other antibacterials Appendix 1. Stevens-Johnson syndrome (erythema mul- Retention enema, Sulfasalazine.
should be given if specifically indicated (for Adverse effects: Local pain or burning sen- tiforme), exfoliative dermatitis, epidermal
example, sepsis associated with fistulas and sation; rectal bleeding (reported with use of necrolysis, pruritus, photo-sensitization, 4.9 Miscellaneous
perianal disease) and for managing bacterial enema); exacerbation of untreated infections; anaphylaxis, serum sickness, interstitial ne-
OTC DIGESTZYME® (Embassy)
overgrowth in the small bowel. suppositories may stain fabrics; systemic ad- phritis, lupus erythematosus-like syndrome); Syrup, Pepsin (1:3000) 10 mg, Diastase (1:1200)
verse effects (section 10.3). lung complications (including eosinophilia, 50 mg
Immunosuppressant drugs can be useful in fibrosing alveolitis); ocular complications
Dose: Ulcerative colitis, proctitis, by rectum Pack: 200 mL
patients with chronically active disease, par- (including periorbital oedema); stomatitis,
(suppositories), ADULT 25 mg twice Description: Enzymes have specific role in digestive
EMDEX
ticularly in patients unresponsive to corticos- parotitis; ataxia, aseptic meningitis, vertigo, process. Their action is similar to lock and key pro-
daily for 2 weeks; may be increased
teroids or those with corticosteroid-dependent tinnitus, alopecia, peripheral neuropathy, cess. Each enzyme has specific and particular sub-
to 25 mg 3 times daily or 50 mg
disease. Methotrexate (section 12.1.3) is some- insomnia, depression, hallucinations; kidney strate to act on. E.g., Amylases act on carbohydrates,
twice daily in severe cases; in factitial
times used to treat Crohn disease unresponsive reactions (including proteinuria, crystalluria, lipase acts on fats, and proteases act on proteins. Di-
proctitis treatment may be required gestzyme contains carbohydrate digesting enzyme,
to immunosuppressants. haematuria); oligospermia; rarely acute pancre-
for 6–8 weeks. fungal diastase (1:1200) derived from Aspergilus
MAINTENANCE OF REMISSION Ulcerative colitis, ulcerative proctitis, atitis, hepatitis; urine may be coloured orange; oryzae (1 g of fungal diastase digests 1200 mg of
Sulfasalazine is most effective in the main- ulcerative proctosigmoiditis, by rectum some soft contact lenses may be stained. carbohydrate and pepsin, the protein digesting
tanance of remission of ulcerative colitis, but (retention enema), ADULT 100 mg at Dose: Ulcerative colitis, by mouth, ADULT 1–2 enzyme (1 g of pepsin digests 3000 mg of protein).
it is not so useful in Crohn disease. Corticos- night for 21 days or until clinica and g 4 times daily in acute attack until Each teaspoonful of Digestzyme digests 90 g of food.
teroids are not suitable for maintenance of proctological remission; if no clinical remission, reducing to maintenance Indications: For quick relief from belching, flatu-
and proctological improvement after dose of 500 mg 4 times daily; CHILD lence and abdominal discomfort. It aids digestion,
remission because of their adverse effects.
over 2 years, 40–60 mg/kg daily in exerts mild laxative action, prevents gas formation,
In resistant or frequently relapsing cases of 21 days, discontinue; treatment for
acute attack, reducing to mainte- and enhances absorption of fats and fat soluble
inflammatory bowel disease azathioprine 2–3 months may be required for vitamins.
2–2.5 mg/kg daily or mercaptopurine 1–1.5 proctological remission; when used nance dose of 20–30 mg/kg daily.
Dose: Adult, 5 ml (one teaspoonful) immediately
mg/kg daily given under close supervision for more than 21 days, discontinue Active Crohn disease, by mouth, after meals.
may be helpful. Methotrexate 15 mg weekly, gradually using 100 mg every other ADULT 1–2 g 4 times daily in acute Child: ½ the adult dose.
is sometime used to maintain remission in night for 2–3 weeks. attack until remission occurs; CHILD
Crohn disease. POM Hydrocortisone (WMF 17.3)
ADDITIONAL TREATMENTS Suppository, Hydrocortisone acetate 25 mg
Retention enema, Hydrocortisone.
Laxatives are required to facilitate bowel move-
ment when proctitis is present. Antimotility SULFASALAZINE
drugs such as codeine and antispasmodic
Indications: Ulcerative colitis; Crohn disease;
drugs should not be used in active ulcerative
severe rheumatoid arthritis (section 2.1.2).
colitis because they can precipitate paralytic
Contra-indications: Hypersensitivity to salic-
ileus and megacolon. Diarrhoea resulting from
ylates or sulfonamides; child under 2 years;
reduced bile salt absorption may improve with
porphyria; intestinal or urinary obstruction;
colestyramine [not included on WHO Model
severe renal impairment Precautions: renal
List]. General nutritional care and appropriate
impairment (Appendix 4); hepatic impairment;
supplements are essential. High-fibre or low
G6PD deficiency; slow acetylator status; moni-
residue diets should be used as appropriate.
tor blood counts and liver function initially and
Irritable bowel syndrome during remission at monthly intervals for first 3 months; monitor
of ulcerative colitis requires avoidance of a kidney function initially and at intervals dur-
high-fibre diet and possibly treatment with ing treatment; history of allergy; pregnancy
an antispasmodic. (Appendix 2) and breastfeeding (Appendix 3);
5.1 Drugs used in heart failure | 175
5. Cardiovascular system 5.1 Drugs used in heart failure Digoxin, a cardiac glycoside, increases the
Treatment of heart failure aims to relieve strength of cardiac muscle contractions and in-
symptoms, improve exercise tolerance, reduce creases cardiac output. In mild heart failure, di-
drugs
incidence of acute exacerbations, and reduce goxin inhibits the sympathetic nervous system
and produces arterial vasodilation. It produces
mortality. Drugs used to treat heart failure due
to left ventricular systolic dysfunction include symptomatic improvement, increases exercise
tolerance, and reduces hospitalization, but it
ACE inhibitors, diuretics, cardiac glycosides
and vasodilators. In addition, measures such does not reduce mortality. It is considered for
5.1 Drugs used in heart failure. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 175 as weight reduction, moderate salt restriction, patients with atrial fibrillation and for selected
and appropriate exercise should be introduced. patients who remain symptomatic despite
5.2 Diuretics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 179
treatment with an ACE inhibitor, a diuretic, and
5.2.1 Low-ceiling diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 179 The primary treatment of heart failure is with a suitable beta-blocker.
angiotensin-converting enzyme inhibitors
5.2.2 High-ceiling (or Loop) diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 182 (ACE inhibitors) such as enalapril which can Vasodilators are used in heart failure to reduce
be used in all stages of chronic heart failure to systemic vascular resistance. Isosorbide dini-
5.2.3 Potassium-sparing diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 185 trate (section 5.5) produces mainly venous dil-
prevent further deterioration and progression
5.2.4 Osmotic diuretics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188 of heart disease. atation, which reduces left ventricular preload,
leading to a reduction in pulmonary conges-
5.3 Antihypertensive drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188 A thiazide diuretic such as hydrochlorothi- tion and dyspnoea. Hydralazine (section
5.3.1 Beta–adrenoceptor blocking drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 190 azide is used in the management of mild to 5.3.2) produces mainly arterial vasodilation,
moderate heart failure when the patient has which reduces left ventricular afterload, and
5.3.2 Vasodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 195 mild fluid retention and severe pulmonary increases stroke volume and cardiac output.
EMDEX
5.3.3 Alpha-adrenoceptor blocking drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 196 oedema is not present; however thiazides are Isosorbide dinitrate and hydralazine can be
ineffective if renal function is poor. In these used in combination when an ACE inhibitor
5.3.4 Centrally acting antihypertensive drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 198 patients, and in more severe fluid retention, cannot be used, but this combination may be
5.3.5 Angiotensin–converting enzyme (ACE) inhibitors. . . . . . . . . . . . . . . . . . . . . . . . 200 a loop diuretic such as furosemide (section poorly tolerated.
5.2.2) is required. In severe fluid retention, IV
5.3.6 Angiotensin receptor blockers (ARBs). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 206 furosemide produces relief of breathlessness Dopamine, an inotropic sympathomimetic,
may be given for short periods in the treatment
5.3.7 Calcium–channel blockers . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 212 and reduces preload sooner than would be
expected from the time of onset of diuresis. Hy- of severe heart failure. Dosage is critical; at
5.3.8 Diuretics . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 221 pokalaemia may develop, but is less likely with low doses it stimulates myocardial contrac-
the shorter-acting loop diuretics than with the tility and increases cardiac output, however,
5.4 Antiarrhythmic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 222
thiazides; care is needed to avoid hypotension. higher doses (more than 5 µg/kg per minute)
5.5 Antianginal drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 227 cause vasoconstriction, with a worsening of
A combination of a thiazide and a loop diuretic heart failure.
5.6 Antithrombotic drugs and myocardial infarction. . . . . . . . . . . . . . . . . . . . . . . . . . . 230 may be required to treat refractory oedema.
5.7 Lipid-regulating drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 234 The combination often produces a synergistic CAPTOPRIL
effect on solute and water excretion, which
5.8 Vasoprotectives . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 239 relieves symptoms in the diuretic-resistant See under section 5.3.5
5.9 Peripheral vasodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 240 heart failure patient. However, the combination
POM Captopril (EDL 10.4)
may produce excessive intravascular volume Tablets, Captopril 12.5 mg, 25 mg.
depletion and electrolyte disturbances includ-
ing potentially life-threatening hypokalaemia. DIGOXIN
The aldosterone antagonist spironolactone Therapeutic category: Cardiac glycoside;
(section 5.2.3) may be considered for patients Anti-arrhythmic agent.
with severe heart failure who are already re- Indications: Heart failure; arrhythmias (sec-
ceiving an ACE inhibitor and a diuretic; a low tion 5.4)
dose of spironolactone (usually 25 mg daily) Contra-indications: Hypertrophic obstructive
reduces symptoms and mortality rate in these cardiomyopathy (unless also severe heart fail-
patients. Close monitoring of serum creatinine ure); Wolff-Parkinson-White syndrome or other
and potassium is necessary with any change in accessory pathway, particularly if accompanied
treatment or in the patient’s clinical condition. by atrial fibrillation; ventricular tachycardia or
The beta-blockers bisoprolol and carvedilol fibrillation; intermittent complete heart block;
[not included on WHO Model List] can be used second-degree AV block.
in stable heart failure and left-ventricular sys- Precautions: Recent myocardial infarction; sick
tolic dysfunction. Treatment with beta-blockers sinus syndrome; severe pulmonary disease;
should only be undertaken by those expe- thyroid disease; elderly (reduce dose); renal
rienced in the management of heart failure. impairment (Appendix 4); avoid hypokalaemia;
avoid rapid IV administration (nausea and
176 | 5.1 Drugs used in heart failure 5.1 Drugs used in heart failure | 177
risk of arrhythmias); pregnancy (Appendix Injection, (100 mcg), Digoxin 0.1 mg per mL; in dobutamine or sodium metabisulfate, or any flow, frequency of ectopic activity, heart rate, and
2); breastfeeding (Appendix 3); interactions: 1-mL amp component of the preparation; idiopathic (whenever possible) measurements of cardiac
Appendix 1. Injection, (250 mcg), Digoxin 0.25 mg per mL; in hypertrophic subaortic stenosis (IHSS); hypo- output, central venous pressure, and/or pulmonary
Adverse effects: Usually associated with ex- 2-mL amp. volaemic conditions; cardiac arrhythmias such capillary wedge pressure.
cessive dosage and include anorexia, nausea, POM Digoxin (Kakaki) as atrial fibrillation. (Additional information sourced from Dobutamine monograph
[1] http://www.medicines.org.uk; [2] https://www.clinicalkey.
vomiting, diarrhoea, abdominal pain; visual Tablet, Digoxin 250 mcg Precautions: Long-term use of intravenous com; [3] http://www.uptodate.com)
disturbances, headache, fatigue, drowsiness, 250 mcg – 28’s; 1000’s inotropic therapy without a specific indica-
confusion, dizziness, delirium, hallucinations, POM LANOXIN® (GSK) tion or for reasons other than palliation is POM Dobutamine Concentrate (Alpha)
depression; arrhythmias, heart block; rarely Tablet, Digoxin 0.25 mg; scored tab. potentially harmful and should be avoided. Injection, Dobutamine HCl 12.5 mg per mL; sterile
rash, intestinal ischaemia; gynaecomastia on Pack: 20. Cardiac disease including acute myocardial solution for injection in 20 mL clear glass amps.
long-term use; thrombocytopenia reported. Injection, Digoxin 0.25 mg per mL; in 2 mL amp. infarction, unstable angina, or severe coronary Pack: 20 mL x 1’s; 20 mL x 5’s; 20 mL x 10’s (glass
Advice to patients: Do not discontinue artery disease. Renal dysfunction. May alter amps in cartons).
POM LANOXIN-PG® (GSK)
medication without checking with physician; Tablet, Digoxin 0.0625 mg; blue tab. potassium levels. Tachyphylaxis may occur if
notify physician if loss of appetite or visual Pack: 20. given continuously for >72 hours. Pregnancy, DOPAMINE
changes occur. Elixir, Digoxin 0.05 mg per 5 mL; yellow coloured breastfeeding, children, elderly. Therapeutic category: Sympathomimetic.
Nursing action: Give with or without food; elixir. To be used undiluted. Interactions: Inhalational hydrocarbon anes- Indications: Cardiogenic shock in MI or cardiac
tablet may be crushed and mixed with food Pack: 60 mL. thetics e.g. Halothane; Beta-blockers; primarily surgery.
or fluids. venous acting vasodilators e.g. nitrates, sodium Contra-indications: Tachyarrhythmia, ven-
• Give IV infusion slowly over at least 5 minutes with DOBUTAMINE nitroprusside. Do not mix with alkaline solutions tricular fibrillation; ischaemic heart disease;
close monitoring. Therapeutic category: Adrenergic cardiac e.g. Sodium bicarbonate. phaeochromocytoma; hyperthyroidism.
• Obtain baseline data before giving first dose stimulant; Inotrope Adverse effects: Increased HR and BP; head- Precautions: Correct hypovolaemia before,
EMDEX
namely heart rate and rhythm, BP, and electrolytes. Pharmacology: Dobutamine is a beta-1-selec- and maintain blood volume during treat-
ache; anginal pain; palpitations; hypotension,
• Loading dose may need to be reduced if patient tive intravenous inotrope. It acts primarily by ventricular tachycardia, arrhythmia exacerba- ment; correct hypoxia, hypercapnia, and
has received cardiac glycoside within the previous
stimulating beta1-adrenergic receptors, causing tion. Bronchospasm, shortness of breath, chest metabolic acidosis before or at same time as
2-3 weeks.
• Apical-radial pulse should be taken for a full minute increased contractility and heart rate, with pain, fatigue. Fever, phlebitis at the injection starting treatment; low dose in shock due to
and significant changes reported to the physician. little effect on beta2 – or alpha-receptors. The site. Rarely hypokalemia, myoclonic spasm, myocardial infarction; history of peripheral
• Withhold drug and notify physician if pulse rate increased myocardial contractility and stroke paresthesias, skin necrosis. vascular disease (increased risk of ischaemia
falls below 60 beats/minute; may be sign of digitalis volume result in increased cardiac output with Dose: Rate of infusion should be individu- of extremities); breastfeeding (Appendix 3);
toxicity. Other noncardiac signs of toxicity include modest chronotropic effects. The inotropic alized depending on the patient’s elderly; interactions: Appendix 1.
nausea, vomiting, anorexia, visual disturbances, effects are dose-dependent. Dobutamine response to therapy and the adverse Adverse effects: Nausea and vomiting;
blurred vision, confusion, and depression. is structurally related to isoproterenol and peripheral vasoconstriction; hypotension
reactions experienced. Titrate dosage
• Monitor serum potassium and encourage patient
dopamine but differs in possessing more po- based on hemodynamic response, with dizziness, fainting, flushing; tachycardia,
to eat potassium-rich foods to avoid hypokalaemia
viz banana, orange juice.
tent inotropic and vasodilatory effects; it also including systemic blood pressure, ectopic beats, palpitations, anginal pain; head-
• Dosage should be reduced by 20-25% when has less alpha-1 agonist, dopaminergic and urine flow, frequency of ectopic ache, dyspnoea; hypertension particularly in
changing from oral to parenteral therapy. chronotropic effects relative to dopamine. activity, heart rate, and (whenever overdosage.
Dose: Heart failure, by mouth, ADULT 1–1.5 Secondary hemodynamic effects include possible) measurements of cardiac Nursing action: Administer into large vein
mg in divided doses over 24 hours decreases in systemic vascular resistance (after- output, central venous pressure, to prevent the possibility of extravasation;
for rapid digitalization or 250 µg load) and ventricular filling pressure (preload); and/or pulmonary capillary wedge monitor continuously for free flow; in case
1–2 times daily if digitalization less elevation of systolic blood pressure; increases pressure. of extravasation, due to the short half-life of
urgent; maintenance 62.5–500 µg in coronary blood flow and myocardial oxygen Adult, by continuous IV infusion, dopamine, withdrawal of drug is often the
daily (higher dose may be divided), consumption. It does not cause release of nor- Initially 0.5 – 1 mcg/kg/min; then only necessary treatment. Use phentolamine
according to renal function and heart epinephrine from sympathetic nerve endings. titrated every few minutes. Usual as antidote; mix 5 mg with 9 mL of NS; inject a
rate response; usual range 125–250 Administration is via continuous IV infusion; dosage range is 2-20 mcg/kg/min. small amount of this dilution into extravasated
µg daily (lower dose more appropri- onset of action is 1-2 mins while peak effect Administration: Concentrate for injection must be area; blanching should reverse immediately.
ate in elderly takes 10-20 mins. Metablised in the tissues diluted before administration as per manufacturer’s Monitor site; repeat the antidote if blanching
Emergency loading dose, by IV infusion and liver; excretion is mainly by the kidney as directions. should recur.
the metabolites and conjugates. Elimination Administer diluted solution by IV infusion into a • Monitor B.P., pulse rate, urine output, temperature
over at least 2 hours, ADULT 0.75–1
half-life is 2-3 mins. large vein using a controlled infusion device. frequently during infusion.
mg. Premixed bags of dobutamine in D5W solutions may
Indications: Short-term management of • Observe patient for adverse effects and notify
Note: Infusion dose may need to be reduced if exhibit a pink color that, if present, will increase with doctor immediately if they occur; dosage may need
digoxin or other cardiac glycoside given in previous cardiac decompensation due to depressed time. This color change is due to slight oxidation of to be adjusted or discontinued.
2 weeks. contractility resulting from organic heart the drug, but there is no significant loss of potency. Dose: Cardiogenic shock, by IV infusion into
POM Digoxin (WMF 12.4) disease or cardiac surgery. Cardiogenic shock Do not administer dobutamine simultaneously with
large vein, ADULT initially 2–5 µg/kg/
Tablets, Digoxin 62.5 µg, 250 µg. characterised by heart failure with severe solutions containing sodium bicarbonate or strong
alkaline solutions (incompatible).
minute; gradually increased by 5–10
Oral liquid, Digoxin 50 µg/mL. hypotension and in case of septic shock.
Infusion of dobutamine should be started at a low µg/kg/minute according to blood
Injection, Digoxin 250 µg/mL; in 2-mL ampoule. Dobutamine stress echocardiography is used
rate and titrated frequently to reach the optimal pressure, cardiac output and urine
POM Digoxin (EDL 10.4) as an alternative in patients who cannot un-
dosage. Dosage titration is guided by the patient’s output; seriously ill patients up to
Tablets, Digoxin 0.0625 mg, 0.125 mg, 0.25 mg dergo a period of exercise.
response, including systemic blood pressure, urine 20–50 µg/kg/minute.
Oral liquid, Digoxin 0.05 mg per mL; in 60-mL bottle. Contra-indications: Hypersensitivity to
178 | 5.1 Drugs used in heart failure 5.2 Diuretics | 179
POM Dopamine (WMF 12.4) nia, muscle cramps, rash and renal impairment; raemic alkalosis, hypercalcaemia; hyperglycaemia, hyperkalaemia. Other electrolyte disturbances
Injection, Dopamine HCl 40 mg/mL; in 5-mL am- rarely, vomiting, dyspepsia, abdominal pain, hyper-uricaemia, gout; rashes, photosensitivity; al- include hypercalcaemia (thiazides), hypocal-
poule. constipation, peptic ulcer, glossitis, stomatitis, tered plasma lipid concentration; rarely impotence caemia (loop diuretics) and hypomagnesaemia
POM Dopamine (EDL 10.4/Restricted List) ileus, anorexia, pancreatitis, liver damage, (reversible); blood disorders (including neutropenia, (thiazide and loop diuretics).
Injection, Dopamine (as HCl) 40 mg per mL; in chest pain, palpitations, arrhythmias, Raynaud thrombocytopenia); pancreatitis, intrahepatic Symptoms of fluid and electrolyte imbalance
5-mL vial. syndrome, angioedema, bronchospasm, rhin- cholestasis; acute renal failure; hypersensitivity include dry mouth, thirst, gastrointestinal
POM Dopamine (Alpha) orrhoea, dry mouth, sore throat, pulmonary reactions (pneumonitis, pulmonary oedema, severe disturbances (including nausea, vomiting),
Injection, Dopamine HCl 40 mg per mL; in 5 mL amp. infiltrates, paraesthesia, vertigo, nervousness, skin reactions). weakness, lethargy, drowsiness, restlessness,
Pack: 100’s. depression, confusion, drowsiness, insomnia, Dose: Heart failure, by mouth, ADULT initially seizures, confusion, headache, muscle pains
dream abnormalities, pruritus, urticaria, alo- 25 mg daily on rising, increasing to or cramps, hypotension (including postural
POM Dopamine Concentrate (Alpha)
Injections, Dopamine HCI 200 mg, 800 mg per 5 mL pecia, flushing, impotence, gynaecomastia, 50 mg daily if necessary; ELDERLY hypotension), oliguria, arrhythmias.
Stevens-Johnson syndrome, toxic epidermal initially 12.5 mg daily.
necrolysis, exfoliative dermatitis, pemphigus, ELDERLY
ENALAPRIL POM Hydrochlorothiazide (WMF 12.4)
taste disturbance, tinnitus, blurred vision; elec- Tablet (scored), Hydrochlorothiazide 25 mg The elderly are more susceptible to electrolyte
Indications: Heart failure (with a diuretic);
trolyte disturbances and hypersensitivity-like imbalance than younger patients. Treatment
prevention of symptomatic heart failure in
reactions (including fever, myalgia, arthralgia, 5.2 Diuretics should begin with a lower initial dose of the
patients with left ventricular dysfunction;
eosinophilia, and photosensitivity) reported. diuretic (commonly about 50% of the adult
hypertension (section 5.3). 5.2.1 Low-ceiling diuretics
Dose: Heart failure, asymptomatic left ven- dose) and then adjusted carefully according
Contra-indications: Hypersensitivity to ACE 5.2.2 High-ceiling (or Loop) diuretics
tricular dysfunction, by mouth, ADULT, to renal function, plasma electrolytes and
inhibitors (including angioedema); renovascu- 5.2.3 Potassium-sparing diuretics
initially 2.5 mg daily under close 5.2.4 Osmotic diuretics
diuretic response.
lar disease; pregnancy (Appendix 2).
medical supervision, increased over
Precautions: Use with diuretics; hypotension
EMDEX
2–4 weeks to usual maintenance dose Diuretics increase urinary excretion of water 5.2.1 Low-ceiling diuretics
with first doses, especially in patients on diu- and electrolytes and are used to relieve
20 mg daily in 1–2 divided doses; Note: Low-ceiling diuretics include thiazide diuretics and
retics, on a low-sodium diet, on dialysis, if dehy- oedema associated with heart failure, ne-
maximum 40 mg daily. non-thiazide diuretics such as Indapamide.
drated, or with heart failure; peripheral vascular phrotic syndrome or hepatic cirrhosis. Some
disease or generalized atherosclerosis (risk of POM Enalapril (WMF 12.4) diuretics are used at lower doses to reduce
Tablet, Enalapril 2.5 mg. Thiazide diuretics, such as hydrochloro-
clinically silent renovascular disease); use with raised blood pressure. Osmotic diuretics are
See preparations under section 5.3.5 thiazide, are moderately potent and act by
great care in severe or symptomatic aortic mainly used to treat cerebral oedema, and also inhibiting sodium and chloride reabsorption at
stenosis; monitor renal function before and to lower raised intraocular pressure.
FUROSEMIDE the beginning of the distal convoluted tubule.
during treatment; renal impairment (reduce
Most diuretics increase urine volume by inhib- They produce diuresis within 1–2 hours of oral
dose, see also Appendix 4); hepatic impairment POM Furosemide (WMF 12.4) iting the reabsorption of sodium and chloride administration and most have a duration of
(Appendix 5); possibly increased risk of agran- Tablet, Furosemide 40 mg.
ions in the renal tubule; they also modify renal action of 12–24 hours.
ulocytosis in collagen vascular disease; history Injection, Furosemide 10 mg/mL; in 2-mL ampoule.
handling of potassium, calcium, magnesium Thiazide diuretics are used in the management
of idiopathic or hereditary angioedema (use See under section 5.2.2. and urate. Osmotic diuretics act differently; of oedema associated with mild to moderate
with care or avoid); breastfeeding (Appendix
they cause an increase in urine volume by an congestive heart failure, renal dysfunction or
3); interactions: Appendix 1.
HYDROCHLOROTHIAZIDE osmotic effect. hepatic disease; however, thiazides are not
USE WITH DIURETICS: Risk of very rapid falls in
Indications: Heart failure; hypertension (sec- Although loop diuretics are the most potent effective in patients with poor renal function
blood pressure in volume-depleted patients;
tion 5.3); oedema (section 5.2.1). their duration of action is relatively short, whilst (creatinine clearance of less than 30 mL per
treatment should therefore be initiated with
Contra-indications: Severe renal or severe thiazide diuretics are moderately potent but minute). In severe fluid retention a loop diuretic
very low doses. High-dose diuretic therapy
hepatic impairment; hyponatraemia, hypercal- produce diuresis for a longer period. Potassi- may be necessary.
(furosemide dose greater than 80 mg daily)
caemia, refractory hypokalaemia, symptomatic um-sparing diuretics have a relatively weak In hypertension, a thiazide diuretic is used at
should be discontinued, or dose significantly
hyperuricaemia; Addison disease. diuretic effect. Carbonic anhydrase inhibitors a low dose to lower blood pressure with very
reduced, at least 24 hours before starting enal-
Precautions: Renal impairment (Appendix 4); are weak diuretics which are rarely used for little biochemical disturbance; the maximum
april (may not be possible in heart failure—risk
hepatic impairment (Appendix 5); pregnancy their diuretic effect and are principally used therapeutic effect may not be seen for several
of pulmonary oedema). If high-dose diuretic
(Appendix 2); breastfeeding (Appendix 3); to lower intraocular pressure in glaucoma weeks. Higher doses should not be used
cannot be stopped, medical supervision ad-
elderly (reduce dose); electrolytes may need to (section 13.4.4). because they do not necessarily increase
vised for at least 2 hours after administration
be monitored with high doses or in renal im- ELECTROLYTE IMBALANCE the hypotensive response but may cause
or until blood pressure stable.
pairment; may aggravate diabetes mellitus and marked changes in plasma potassium, sodium,
ANAPHYLACTOID REACTIONS: Avoid enalapril gout; may exacerbate systemic lupus erythe- The adverse effects of diuretic therapy are
mainly due to the fluid and electrolyte imbal- magnesium, uric acid, glucose, and lipids. If a
during dialysis with high-flux polyacrilonitrile matosus; porphyria; interactions: Appendix 1.
ance induced by the drugs. Hyponatraemia is thiazide alone does not lower blood pressure
membranes and during low-density lipo- Adverse effects: Fluid and electrolyte imbalance
an adverse effect of all diuretics. The risk of adequately, it may be combined with another
protein apheresis with dextran sulfate; also leading to dry mouth, thirst, gastrointestinal dis-
hypokalaemia, which may occur with both antihypertensive such as a beta-adrenoceptor
withhold before desensitization with wasp or turbances (including nausea, vomiting), weakness,
thiazide and loop diuretics, depends more antagonist (section 5.3).
bee venom. lethargy, drowsiness, seizures, headache, muscle
Adverse effects: Dizziness, headache; less pains or cramps, hypotension (including postural on the duration of action than on potency Urinary excretion of calcium is reduced by thi-
commonly, nausea, diarrhoea, hypotension hypotension), oliguria, arrhythmias; hypokalaemia, and is thus greater with thiazides than with azide diuretics and this property is occasionally
(severe in rare cases), dry cough, fatigue, asthe- hypomagnesaemia, hypo-natraemia, hypochlo- loop diuretics (when given in equipotent utilized in the treatment of idiopathic hyper-
doses). Potassium-sparing diuretics can cause calciuria in patients with calcium-containing
180 | 5.2.1 Low-ceiling diuretics 5.2.1 Low-ceiling diuretics | 181
calculi. Paradoxically, thiazide diuretics are POM Bendroflumethiazide (Kakaki) POM REGROTON® (Novartis) respectively.
used in the treatment of diabetes insipidus, Tablet, Bendroflumethiazide 5 mg Tablet, Chlortalidone 50 mg, reserpine 0.25 mg. 25 mg – 10 x 10’s; 500’s.
since in this disease they reduce urine volume. 5 mg – 28’s; 1000’s Pack: 20, 100.
POM Hydrochlorothiazide (Drugfield)
Thiazide diuretics, especially in high doses, pro- Tablet, Hydrochlorothiazide 25 mg
CHLORTALIDONE plus RESERPINE HYDROCHLOROTHIAZIDE 25 mg – 3 x 10’s; 10 x 10’s (in blisters)
duce a marked increase in potassium excretion
Therapeutic category: Diuretic/antihyper- Indications: Oedema; diabetes insipidus; hy-
which may cause hypokalaemia; this is dan-
tensive pertension (see also section 5.3); heart failure INDAPAMIDE
gerous in patients with severe coronary artery
Indications: Hypertension (section 5.1). Therapeutic category: Diuretic, Antihyper-
disease and those being treated with cardiac
Contra-indications: Anuria, severe renal or Contra-indications: Severe renal or severe tensive.
glycosides. In hepatic failure hypokalaemia
hepatic failure, refractory hypokalaemia and hepatic impairment; hyponatraemia, hypercal- Indication: Essential hypertension.
can precipitate encephalopathy, particularly in
hyponatraemia, hypercalcaemia, symptomatic caemia, refractory hypokalaemia, symptomatic Contra-indications: Hypersensitivity to sulfona-
alcoholic cirrhosis. Potassium-sparing diuretics
hyperuricaemia, overt depression, parkinson’s hyperuricaemia; Addison disease. mides; Severe renal failure; Hepatic encephalopa-
are a more effective alternative to potassium
disease, epilepsy, electroconvulsive therapy, Precautions: Renal impairment (Appendix 4), thy or severe hepatic failure; Hypokalemia.
supplements for preventing of hypokalaemia
phaeo-chromocytoma, co-medication with hepatic impairment (Appendix 5); pregnancy Combination treatments: Indapamide may
induced by thiazide diuretics; however, sup-
MAO inhibitors, acute peptic ulcer, ulcerative (Appendix 2), breastfeeding (Appendix 3); elbe combined with all nonthiazide antihy-
plementation with potassium in any form is
colitis. derly; electrolytes may need to be monitored pertensive agents, with ß-blockers, calcium
seldom necessary with the smaller doses of
Precautions: Coronary or cerebral arter- with high doses or in renal impairment; may channel blockers, and ACE inhibitors.
diuretics used to treat hypertension.
io-sclerosis, renal dysfunction; periodic serum aggravate diabetes mellitus and gout; may Drug combinations to be avoided: Lithium,
Indapamide is a non-thiazide sulfonamide electrolyte determinations (in the event of exacerbate SLE; porphyria; interactions: non-antiarrhythmic drugs causing wave burst
diuretic. It is a low-ceiling diuretic like thiazides. potassium depletion give potassium medica- Appendix 1. arrhythmia (astemizole, bepridil, IV erythro-
tion under surveillance); hypomagnesaemia, Adverse effects: Hypokalaemia, hypo-mag- mycin, halofantrine, pentamidine, sultopride,
BENDROFLUAZIDE
EMDEX
hyponatraemia, hyperuricaemia, impaired nesaemia, hyponatraemia, hypo-chloraemic terfenadine, vincamine).
Synonym: Bendroflumethiazide. glucose tolerance, hyperlipidaemia, history alkalosis (for symptoms of fluid and electrolyte Precautions: Pregnancy, lactation. Monitoring
Therapeutic category: Thiazide diuretic. of peptic ulcer or depression; acute erosive imbalance see introductory notes); hypercal- of potassium and uric acid serum levels is
Pharmacology: Bendrofluazide is a thiazide gastritis, gall-stones, heart failure, fresh myo- caemia; hyperglycaemia; hyperuricaemia, gout; recommended, especially in subjects with a
duuretic that increases urine excretion of cardial infarction, sinus bradycardia, disorders rash, photosensitivity; altered plasma lipid con- predisposition or a sensitivity to hypokalemia
sodium and water by inhibiting sodium re- of cardiac conduction, operations; pregnancy, centration; rarely impotence (reversible), blood and in patients with gout. History of allergy
absorption in the cortical diluting site of the lactation; road-users. disorders (including neutropenia, thrombocyto- to sulfonamide derivatives (monitor closely).
ascending loop of Henle. Adverse effects: Depression, anxiety states, GI penia); pancreatitis, intra-hepatic cholestasis and Adverse effects: Feeling of fatique (asthenia),
Indications: Oedema, hypertension. upsets, postural hypotension, disturbances af- hypersensitivity reactions (including pneumo- headache, pins and needles affecting the ex-
Contra-indications: Severe renal dysfunction, fecting potency; hypokalaemia, hyponatraemia, nitis, pulmonary oedema, severe skin reactions) tremities. Allergic-type symptoms, rare cases of
hypercalcaemia. hypomagnasaemia, hyperuricaemia, hyper-gly- also reported; acute renal failure. skin rashes. Feeling of dizziness when changing
Precautions: Potassium supplement may be caemia, rise in blood lipid levels, thrombocy- Dose: Hypertension, by mouth, ADULT 12.5 from a lying to a standing position (orthostatic
required, diabetes, pregnancy, breast feeding, topenia, changes in the blood count; sinus mg daily increased to 25–50 mg daily hypotension). Risk of dehydration increased in
elderly. bradycardia, GI ulceration; disturbances affecting if necessary. the elderly and in heart failure patients. Nausea,
Adverse effects: Hypokalaemia, gout, fatigue, ejaculation, galactorrhoea, gynaecomastia; car- Oedema, by mouth, ADULT initially constipation, dry mouth. Changes in blood
blood dyscrasias, rash, hyperglycaemia diac arrhythmia, parkinsonism. 25 mg daily on rising, increasing to parameters can occur, particularly an excessive
Nursing action: Administer in the morning Advice to patients: May be taken with food 50 mg daily if necessary; ELDERLY fall in potassium, especially in the elderly or
to avoid interference with sleep or nocturia. or milk; take early in the day to avoid nocturia; initially 12.5 mg daily malnourished individuals.
• Advise patient to take drug with food to prevent may cause drowsiness, impair judgement Severe oedema in patients unable Dose: One tablet daily.
nausea, and to eat food rich in potassium viz and coordination; impotence, gynaecomastia to tolerate loop diuretics, by mouth, Note: The tablet should be swallowed with water
tomatoes, bananas, oranges.
may occur but reversible; photosensitivity ADULT up to 100 mg either daily or and should not be chewed. A single dose every 24
• Teach patient to avoid sudden posture changes,
but to rise slowly to avoid orthostatic hypotension.
may occur. on alternate days (maximum 100 mg hours, preferably in the morning on account of the
Nursing action: Administer drug in the morn- daily). diuretic effect of this drug in order to avoid possible
• Observe patient for glycosuria (if diabetic); monitor
ing to avoid sleep disturbance or nocturia. Nephrogenic diabetes insipidus, by waking during the night
blood sugar.
• Watch for signs of hypokalaemia, for example, • Teach patient to rise slowly to sitting or standing mouth, ADULT initially up to 100 mg POM INDICONTIN® (Phillips)
muscle weakness and cramps. position to avoid orthostatic hypotension. daily. Caplet, Indapamide 1.5 mg; f-c cap marked “INC”
• Elderly patients are especially susceptible to • Advise patient to eat high-potassium diet such as 1.5 mg – 1000’s; 10 x 10’s (in blisters)
citrus fruits, tomatoes, bananas. POM Hydrochlorothiazide (WMF 16)
excessive diuresis.
• Observe for mental depression and alert family Tablet (scored), Hydrochlorothiazide 25 mg POM NATRILIX®SR (Servier Int’l)
Dose: Oedema, initially 5-10 mg in the
members to report any symptoms; observe for Tablet, Indapamide 1.5 mg.
morning daily or on alternate days; POM Hydrochlorothiazide (EDL 14)
signs of hypokalaemia (muscle weakness and Pack: 10’s; 30’s; sustained-release f-c tab.
maintenance, 2.5-10 mg 1-3 times Tablets, Hydrochlorothiazide 25 mg, 50 mg
cramps) which can be relieved with potassium
weekly. sparing diuretics; blood sugar may increase in the POM CIKADREX® (Michelle Lab) METOLAZONE
Hypertension, 2.5-5 mg in the morn- diabetic and hence, insulin requirement. Tablet, Hydrochlorothiazide 25 mg
Therapeutic category: Diuretic, Thiazide-re-
ing. Dose: By mouth, Adult, initially ½ tablet daily 25 mg – 100’s; 10 x 10’s (in blisters)
lated.
POM Bendrofluazide (EDL 14) according to the patient’s needs POM HYDREX® (Juhel) Pharmacology: Metolazone is a quinazoline
Tablets, Bendrofluazide 2.5 mg, 5 mg. Maintenance, not more than 1 tablet Tablet, Hydrochlorothiazide BP 25 mg; white, diuretic with properties generally similar to
daily. scored tab. marked ‘HCT/25’ and ‘JHL’ on both faces
182 | 5.2.2 High-ceiling (or Loop) diuretics 5.2.2 High-ceiling (or Loop) diuretics | 183
the thiazide diuretics. Like thiazides, it is a pain, xerostomia, constipation; Photosensitivity, use can produce severe dehydration with the the ears, severe abdominal pain or sore throat and
sulfonamide derivative and acts to inhibit pruritus, purpura, rash, skin necrosis; Neuropa- possibility of circulatory collapse. Furosemide fever (these may indicate furosemide toxicity).
sodium reabsorption in the distal tubules thy, paresthesia, weakness; Impotence; Blurred may cause hyperuricaemia and precipitate • Check for signs of confusion especially in the
causing increased excretion of sodium and vision; BUN increased, glucosuria; Haematolog- attacks of gout. Rapid high-dose injection or elderly.
water, as well as, potassium and hydrogen ical effects e.g. aplastic anaemia or hypoplastic infusion of furosemide may cause tinnitus and Dose: Oedema, by mouth, ADULT initially
ions. The increased delivery of sodium to the anaemia, agranulocytosis, leukopaenia, or even permanent deafness. 40 mg daily on rising; maintenance,
distal tubular exchange site results in increased thrombocytopaenia. 20–40 mg daily; may be increased
potassium excretion. Unlike thiazide diuretics, Advice to patients: Take early in the day to FUROSEMIDE to 80 mg daily or more in resistant
metolazone does not decrease the GFR or the avoid frequent urination at night. Avoid exces- oedema; CHILD 1–3 mg/kg daily
Synonym: Frusemide.
renal plasma flow and is therefore able to pro- sive exposure to sunlight. Alcoholic beverages (maximum 40 mg daily).
Indications: Oedema; oliguria due to renal
duce diuresis in patients with impaired renal may potentiate orthostatic hypotensive effect. Acute pulmonary oedema, by slow IV
failure.
function. Diuresis and saluresis usually begin Dose: Adult, by mouth, Peripheral oedema, or injection, ADULT 20–50 mg, if neces-
Contra-indications: Renal failure with anuria;
within one hour and may persist for 24 hours oedema associated with heart failure sary increase by 20-mg steps every 2
precomatose states associated with liver
or more. For most patients, adjusting the daily or renal disease (e.g., nephrotic syn- hours; if effective single dose is more
cirrhosis.
dose can vary the duration of effect. High doses drome), Initially 5-10 mg once daily than 50 mg, consider using slow IV
Precautions: Monitor electrolytes particularly
may prolong the effect. (2.5 mg if combo with loop diuretic). infusion at a rate not exceeding 4 mg/
potassium and sodium; hypotension; elderly
Oral absorption is incomplete. Highly protein May increase up to 20 mg/day based minute; CHILD 0.5–1.5 mg/kg daily
(reduce dose); pregnancy (Appendix 2); correct
bound; crosses the placenta and is found in on response and tolerance. (maximum 20 mg daily)
hypo-volaemia before using in oliguria; renal
breast milk. Undergoes minimal metabolism; Hypertension, Initially 2.5-5 mg once Oliguria (glomerular filtration rate
impairment (Appendix 4), hepatic impairment
excreted mainly as unchanged drug in the daily; may adjust as needed based on less than 20 mL/minute), by slow IV
(Appendix 5); prostatic enlargement; interac-
urine. Time to peak plasma level is approx. response. infusion at a rate not exceeding 4 mg/
tions: Appendix 1.
EMDEX
8 hours. Administration: Administer once daily preferably minute, ADULT initially 250 mg over 1
Adverse effects: Hypokalaemia, hypo-mag-
Indications: Treatment of oedema accompa- early in the day to avoid nocturia. May be taken hour; if urine output not satisfactory
nesaemia, hyponatraemia, hypo-chloraemic
nying congestive heart failure and renal dis- with or without food. during hour after first dose, infuse
alkalosis (for symptoms of fluid and electrolyte
eases, including the nephrotic syndrome and 500 mg over 2 hours then, if no
POM METOZ® (Al-Tinez) imbalance, see introductory notes), increased
states of diminished renal function. Treatment Tablets, Metolazone 2.5 mg, 5 mg. satisfactory response during hour
calcium excretion, hypovolaemia, hyperglycae-
of hypertension. 2.5 mg – 10’s after second dose, infuse 1 g over 4
mia (but less often than with thiazide diuretics);
Contra-indications: Hypersensitivity to metola- 5 mg – 10’s hours; if no response after third dose,
temporary increase in plasma cholesterol and
zone or any of the components; anuria, hepatic dialysis probably necessary; effective
triglyceride concentration; less commonly
coma or pre-coma (hepatic encephalopathy). 5.2.2 High-ceiling (or Loop) diuretics dose (up to 1 g) can be repeated
hyperuricaemia and gout; rarely rash, photo-
Precautions: Sulfonamide allergy. Monitor Loop diuretics, or high-ceiling diuretics, such as every 24 hours.
sensitivity, bone marrow depression (withdraw Note: Dose to be diluted in suitable amount of
and correct electrolyte imbalance (to reduce furosemide, are the most potent and rapidly treatment), pancreatitis (with large parenteral
produce an intense dose-dependent diuresis infusion fluid, depending on hydration of patient.
risk of metabolic alkalosis). Hepatic or renal doses), tinnitus and deafness (with rapid ad-
impairment. Hypovolemia or hypotension of relatively short duration. Oral furosemide ministration of large parenteral doses and in POM Furosemide (WMF 16)
(may increase risk of orthostatic hypotension produces diuresis within 30–60 minutes of Tablet, Furosemide 40 mg.
renal impairment; deafness may be permanent
administration, with the maximum diuretic Injection, Furosemide 10 mg/mL; in 2-mL amp.
and falls). May cause hyperglycemia, increased if other ototoxic drugs taken).
glucose tolerance, and glycosuria (monitor effect in 1–2 hours. The diuretic action lasts for Advice to patients: May be taken with food POM Furosemide (EDL 14)
blood and urine sugar levels especially in 4–6 hours. Intravenous furosemide produces or milk to minimise GI upset; rise slowly from Tablet, Furosemide 40 mg.
diabetes patients). Reduced clearance of uric diuresis within 5 minutes, with the maximum a lying or sitting position to minimise dizziness, Injection, Furosemide 10 mg per mL; in 2-mL amp.
acid may precipitate gout or hyperuricaemia. diuretic effect in 20–60 minutes and diuresis lightheadedness, or fainting, also use extra care POM Furosemide (Crystal)
Photosensitivity. Systemic lupus erythemato- complete within 2 hours. when exercising, standing for long period of Tablet, Furosemide 40 mg; uncoated tab
sus (SLE). Pregnancy, breastfeeding. Loop diuretics inhibit reabsorption from the time, and during hot weather; take last dose 40 mg – 25 x 10’s (in blisters)
Interactions: Antihypertensive agents; Cardiac ascending loop of Henlé in the renal tubule of day early in the evening to prevent nocturia. POM Furosemide (Dabak)
glycosides (monitor potassium levels); Lithium. and are useful, particularly in situations where Nursing action: Give oral and IM doses in the Furosemide 40 mg
Other drugs known to cause hypokalaemia e.g. rapid and effective diuresis is needed such as morning to prevent nocturia; second doses 40 mg – 1 x 1000’s
Corticosteroids. Antidiabetic agents (monitor reduction of acute pulmonary oedema due to should be given in early afternoon; give IV
left ventricular failure . They are also used to POM Furosemide (Kakaki)
for blood glucose changes). Probenecid; slowly over 1-2 minutes.. Tablet, Furosemide 40 mg
NSAIDs; Thioridazine; MAOIs; Carbamazepine; treat oedema associated with renal and hepatic • Parenteral therapy should only be used in children 40 mg – 28’s; 1000’s
Haloperidol. disorders and are used in high doses in the when oral route is not possible.
Adverse effects: Electrolyte disturbances e.g. management of oliguria due to chronic renal • Monitor serum potassium, watch for signs of POM Furosemide (Pemason)
insufficiency. Loop diuretics may be effective hypokalaemia, e.g., muscle weakness and cramps. Injection, Furosemide 20 mg per amp.
hyponatraemia, hypokalaemia, hypochlo-
in patients unresponsive to thiazide diuretics. • Monitor weight and I & O daily; in high doses, POM Apo-Furosemide (Lahams)
raemia and hypomagnesaemia; Precipitation
Because of their shorter duration of action, monitor hearing; check BP lying and standing, to Tablet, Furosemide 40 mg; yellow, scored bev-
of gout or hyperuricaemia; Impaired glucose monitor postural hypotension (furosemide is a very
tolerance, glycosuria, and hyperglycemia in the risk of hypokalaemia may be less with el-edged tab. marked ‘APO 40’.
potent loop diuretic). 40 mg – 1000.
diabetic patients; Lipid abnormalities; Orthos- loop diuretics than with thiazide diuretics; if • Advise patient to eat high potassium diet; to limit
tatic hypotension; CNS effects namely dizziness, required, potassium-sparing diuretics may be alcohol intake and strenous exercise in hot weather POM CIKAMIDE® (Michelle Lab)
lightheadedness, headache, fatigue, malaise; GI used for prevention of hypokalaemia. Loop di- to prevent exacerbating orthostatic hypotension. Tablet, Furosemide 40 mg
disturbances e.g. nausea, vomiting, abdominal uretics may cause hypovolaemia and excessive • Instruct patient to immediately report ringing in 40 mg – 10 x 10’s (in blisters)
184 | 5.2.2 High-ceiling (or Loop) diuretics 5.2.3 Potassium-sparing diuretics | 185
POM DIUREMID® (Hovid) ing is >99%. 80% is cleared through hepatic TORSEMIDE plus SPIRONOLACTONE Tablet, Torsemide 10 mg, Spironolactone 25 mg;
Tablet, Furosemide 40 mg metabolism (mainly inactive metabolites) and Therapeutic category: Loop diuretic; Aldos- f-c tab.
40 mg – 40; 1000. 20% in the urine as unchanged drug. Elimina- Pack: 30’s
terone antagonist.
POM FRUMED® (Fill Pharma) tion half-life is about 3.5 hours. Pharmacology: Torsemide, a sulfonylurea
Tablet, Furosemide 40 mg Indications: Oedema associated with CHF, re- loop diuretic, increases the urinary excretion
5.2.3 Potassium-sparing diuretics
40 mg – 500. nal disease (including chronic renal failure), or Potassium-sparing diuretics include amiloride
of sodium, chloride and water by inhibiting the
Injection, Furosemide 20 mg per 2 mL; in 2-mL hepatic disease; Hypertension alone or in com- and spironolactone; they are weak diuretics
Na+K+2Cl – carrier system in the loop of Henle. It
amber ampoule. bination with other antihypertensive agents. and reduce potassium excretion and increase
does not significantly alter glomerular filtration
POM Furosemide (Alpha) Contra-indications: Hypersensitivity to torse- sodium excretion in the distal tubule. Amiloride
rate, renal plasma flow, or acid-base balance. It
Tablet, Furosemide 40 mg. mide or to sulfonylureas; anuria. acts about 2 hours after oral administration,
markedly impairs the kidney’s ability to excrete
40 mg – 28’s. Precautions: Hepatic disease with cirrhosis reaching a peak in 6–10 hours and persisting
dilute urine during water diuresis.
Injection, Furosemide 25 mg; in 2 mL amp. and ascites as sudden alterations of fluid and for about 24 hours. Spironolactone, which acts
Spironolactone, as a competitive aldosterone
electrolyte balance may precipitate hepatic by antagonising aldosterone, has a relatively
POM FUZIL® (Beta Drugs) antagonist, increases sodium excretion whilst
Injection, Furosemide 20 mg per amp; sterile solution coma. Ototoxicity. Monitor for signs of elec- slow onset of action requiring 2–3 days to
reducing potassium loss at the distal renal
for injection. trolyte imbalance, hypovolemia, or pre-renal achieve maximum diuretic effect, and a similar
tubule. It has a gradual and prolonged action.
azotemia. May cause alterations in the lab. period of 2–3 days for diuresis to cease after
POM LABMID® (Embassy) Patients with liver disease have high levels
values of calcium, magnesium, BUN, creatinine discontinuation of treatment.
Injection, Frusemide 20 mg per 2 mL; in 2 mL amp. of aldosterone which allows accumulation of
and uric acid, glucose and serum lipids. Preg- Amiloride may be used alone, but its principal
Pack: 50’s. sodium in the distal convoluted tubules and
nancy, lactation. use is in combination with a thiazide or a loop
POM LOPEN® (Vixa) collecting ducts. Torsemide combination with
Interactions: Salicylates; Indometacin; diuretic to conserve potassium during treat-
Tablet, Furosemide 40mg an aldosterone antagonist or potassium-spar-
Probenecid; Lithium; Methotrexate; NSAIDs; ment of congestive heart failure or hepatic
40 mg – 10 x 10’s ing diuretic achieves a more efficient diuresis
EMDEX
Risperidone. cirrhosis with ascites.
Injection, Furosemide 20 mg/2 mL. in such patients.
Adverse effects: Dizziness, headache, nau- Spironolactone is used in the treatment of
Pack: 2 mL x 10’s. Indications: Oedema associated with second-
sea, weakness, vomiting, hyperglycemia, ex- refractory oedema due to heart failure, hepatic
POM RENIX® (Reals) ary hyperaldosteronism in liver cirrhosis, con-
cessive urination, hyperuricemia, hypokalemia, cirrhosis (with or without ascites), nephrotic
Tablet, Frusemide 40 mg; uncoated tab. gestive heart failure, and nephrotic syndrome.
excessive thirst, hypovolemia, impotence, syndrome and ascites associated with malig-
40 mg – 10 x 10’s (in a blister). Hypertension with hyperaldosteronism.
esophageal hemorrhage, and dyspepsia. nancy. It is frequently given with a thiazide or
Contra-indications: Hypersensitivity to Tor-
POM SIVOMIDE® (Adpharm) Dose: Adult, by mouth, Congestive heart fail- a loop diuretic, helping to conserve potassium
Injection, Frusemide 20 mg per 2 mL. semide, sulfonylureas or to Spironolactone;
ure, initially 10-20 mg once daily; may in those at risk from hypokalaemia. A low dose
Pack: 1 x 1000’s. Anuria; Acute renal insufficiency; significant
increase gradually by doubling dose of spironolactone is beneficial in severe heart
impairment of renal excretory function (glo-
POM SUPAVIN® (Justeen) until the desired diuretic response is failure in patients who are already taking an
merular filtration rate <10 mL/min); hyperkal-
Injection, Furosemide 10 mg per 2 mL. obtained. Max. daily dose: 200 mg. ACE inhibitor and a diuretic. Spironolactone is
aemia and Addison’s diseasse.
Chronic renal failure, initially 20 mg used in the diagnosis and treatment of primary
Precautions: Torsemide: Hepatic disease with
once daily; may increase gradually hyperaldosteronism; presumptive evidence for
TORSEMIDE cirrhosis and ascites. Tinnitus and hearing loss
by doubling dose until the desired diagnosis is provided by correction of hypokal-
(usually reversible) may occur. Alterations in the
Therapeutic category: Loop diuretic, Anti- diuretic response is obtained. Max. aemia and of hypertension
laboratory values of Calcum, Magnesium, Blood
hypertensive. daily dose: 200 mg. The most dangerous adverse effect of potas-
Urea Nitrogen (BUN), Creatinine and Uric Acid,
Pharmacology: Torsemide, a sulfonylurea loop Hepatic cirrhosis, initially 5-10 mg sium-sparing diuretics, such as amiloride or
Glucose and serum Lipids. Symptomatic gout.
diuretic, acts at Na+/K+/2Cl– reabsorptive pump once-daily, administered together spironolactone, is hyperkalaemia, which can be
Spironolactone: Hyperkalaemia, hypona-
at ascending loop of Henle; interferes with the with an aldosterone antagonist or life-threatening. These diuretics are thus best
tremia. Reversible hyperchloraemic metabolic
chloride-binding cotransport system causing a potassium-sparing diuretic; may avoided or used very carefully in patients who
acidosis, and increases in blood urea. Preg-
increased excretion of water, sodium, chloride, increase gradually by doubling dose have or may develop hyperkalaemia, such
nancy, lactation.
magnesium, and calcium. It does not signifi- until the desired diuretic response is as those with renal failure, patients receiv-
Interactions: Cholestyramine, probenecid,
cantly alter GFR, renal plasma flow, or acid-base obtained. Max. single dose: 40 mg. ing other potassium-sparing diuretics and
indometacin, ACE inhibitors, corticosteroids,
balance.It is twice as potent as furosemide, Hypertension, initially 5 mg once patients taking ACE inhibitors or potassium
NSAIDs, salicylates, digoxin, potassium sup-
and provides a longer duration of action, thus daily; may increase up to a max. 10 supplements.
plements.
allowing for a 24-hour dosage interval. It is mg once daily after 4-6 weeks based Adverse effects: Dizziness, headache, nausea,
effective in the treatment of mild to moderate on BP response. Additional antihy- AMILORIDE
weakness, vomiting, excessive urination, hype-
essential hypertension, and in the reduction pertensive agent may be added if Indications: Oedema associated with heart
ruricaemia, excessive thirst and hypovolaemia.
of edema associated with congestive heart necessary. failure or hepatic cirrhosis (with ascites), usually
Others include gynaecomastia, impotence,
failure, renal disease and hepatic cirrhosis. Note: Thiazide-type diuretics are preferred in the with thiazide or loop diuretic.
diarrhoea and dyspepsia.
Following oral administration torsemide is rap- treatment of hypertension. Contra-indications: Hyperkalaemia; renal
Dose: Adult, usually 1 tablet once daily.
idly absorbed with about 80% bioavailability. (Additional information sourced from Torsemide monograph in Note: Thiazide-type diuretics are preferred in the failure.
Onset of diuretic effect (oral) is within 1 hour [1] https://www.clinicalkey.com [2] http://www.uptodate.com) treatment of hypertension. Precautions: Monitor electrolytes, particu-
while peak effect takes 1-2 hours and duration larly potassium; renal impairment (Appendix
(Additional information sourced from Torsemide monograph in
about 6-8 hours. Food may delay Tmax by POM TORSINEX® (Micronova) 4); diabetes mellitus; elderly (reduce dose);
[1] https://www.clinicalkey.com [2] http://www.uptodate.com)
approx. 30 mins. Peak antihypertensive effect Tablets, Torsemide 10 mg, 20 mg, 100 mg; uncoated
pregnancy (Appendix 2) and breastfeeding
takes 4-6 weeks (up to 12 weeks). Protein bind- tab.
POM TORSINEX® Plus (Micronova) (Appendix 3); interactions: Appendix 1.
186 | 5.2.3 Potassium-sparing diuretics 5.2.3 Potassium-sparing diuretics | 187
Adverse effects: Hyperkalaemia, hypo- Pack: 10 x 3’s; 10 x 10’s congestive heart failure; nephrotic syndrome; 25 mg – 28’s
na-treamia (for symptoms of fluid and elec- hepatic cirrhosis with ascites and oedema; 50 mg – 28’s; 100’s
POM APO-AMILZIDE® (Lahams)
trolyte imbalance see introductory notes), ascites associated with malignancy; primary 100 mg – 28’s
Tablet, Amiloride HCl 5 mg, hydrochlorothiazide 50
diarrhoea, constipation, anorexia; paraes- mg; peach, scored diamond-shaped tab. marked hyperaldosteronism. POM APO-SPIRO® (Lahams)
thesia, dizziness, minor psychiatric or visual ‘APO 5/50’. Contra-indications: Hyperkalaemia; hypon- Tablet, Spironolactone 25 mg; tan scored tab.
disturbances; rash, pruritus; rise in blood urea Pack: 100’s. atraemia; moderate renal impairment; Addison marked ‘APO25’.
nitrogen. disease. 25 mg – 500.
POM CARDURETIC® (Fidson)
Nursing action: See under Spironolactone. Tablet, Amiloride HCl 5 mg, hydrochlorothiazide Precautions: Monitor blood urea nitrogen POM ROLACTONE® (Rohi)
Dose: Oedema, used alone, by mouth, initially 50 mg. and plasma electrolytes (discontinue if hy- Tablets, Spironolactone 25 mg, 50 mg, 100 mg
10 mg daily in 1 or 2 divided doses, Pack: 3 x 10’s; 10 x 10’s (in blisters). perkalaemia); elderly (reduce dose); diabetes 25 mg – 100’s
adjusted according to response (max- mellitus; renal impairment (Appendix 4); 50 mg – 100’s
POM CIKARETIC® (Michelle Lab)
imum 20 mg daily). hepatic impairment; pregnancy (Appendix 2); 100 mg – 100’s
Tablet, Amiloride (as HCI 5 mg, hydrochlorothiazide
Combined with a thiazide or a loop 50 mg breastfeeding (Appendix 3); porphyria; high POM SPIROTAC® (Hovid)
diuretic, by mouth, initially 5 mg daily, Pack: 100’s; 10 x 10’s (in blisters) doses carcinogenic in rodents; interactions: Tablet, Spironolactone 25 mg.
increasing to 10 mg if necessary Appendix 1. 25 mg – 1000.
POM EMBATIC® (Embassy)
(maximum 20 mg daily). Tablet, Amiloride 5 mg, hydrochlorothiazide 50 mg. Adverse effects: Hyperkalaemia, hyponatrae-
Pack: 10 x 10’s. mia, hyperchloraemic acidosis, dehydration (for TRIAMTERENE plus
POM Amiloride (WMF 16) HYDROCHLOROTHIAZIDE
Tablet, Amiloride hydrochloride 5 mg. symptoms of fluid and electrolyte imbalance
POM GRENURETIC® (Greenlife) Pharmacology: Triamterene is a potassium
see introductory notes); transient increase in
Tablet, Amiloride HCl 5 mg, hydrochlorothiazide sparing diuretic that inhibits sodium reabsorp-
AMILORIDE plus 50 mg.
blood urea nitrogen; diarrhoea; gynaecomastia,
HYDROCHLOROTHIAZIDE menstrual irregularities; impotence, hirsutism, tion and potassium excretion by direct action
EMDEX
Synonym: Co-amilozide deepening of voice; rash, ataxia, fever, hepa- on the distal tubule. Hydrochlorothiazide is a
Therapeutic category: Diuretic/antihyper- POM JURETIC® (Juhel) totoxicity. thiazide diuretic that increases urine excretion
Tablet, Amiloride HCl 5 mg, hydrochlorothiazide 50 of sodium and water by inhibiting sodium
tensive Nursing action: Give with meals if nausea
mg; orange scored diamond-shaped tablet marked reabsorption at the beginning of the distal
Indications: Oedema of cardiac origin; hepatic ‘5/50’ on one side and ‘Juhel’ on the reverse. occurs; may slightly reduce absorption.
cirrhosis with ascites and oedema; CHF; hyper- • Give in the morning to avoid interference with convoluted tubule. Traimterene has weak diu-
Pack: 10 x 10’s (in blister); 500’s (in jars).
tension (section 5.3.8). sleep. retic effect when used on its own. It is used as
POM MODUTAB® (Onifam) • Diuretic effect may be delayed 2-3 days and maxi- adjunct with thiazide or loop diuretic instead
Contra-indications: Hyperkalaemia, renal
Tablet, Amiloride 5 mg, hydrochlorthiazide 80 mg mum hypotensive effect may be delayed 2-3 weeks. of giving potassuim supplements.
insufficiency, potassium supplementation, Pack: 3 x 10’s • Advise patient to avoid potassium-rich food like Indications: Treatment of hypertension, alone
Diabetes mellitus. oranges, bananas.
Precautions: Impaired hepatic function, preg- POM NORMORETIC® (Neimeth) or in combination with other antihypertensive
• Weigh patient daily and monitor I&O throughout
nancy, breast-feeding. Tablet, Amiloride HCl 5 mg, hydrochlorothiazide drugs; control of oedema in cardiac failure,
therapy (effect of drug on fluid loss may determine
50 mg. cirrhosis of the liver or the nephrotic syndrome.
Adverse effects: Headache, weakness, nau- the reduction in the number of times it is admin-
Pack: 10; 100; 200. Contra-indications: Hyperkalaemia, progres-
sea, rash, dizziness; orthostatic hypotension, istered per day).
impotence. POM PEMARETIC® (Pemason) • Monitor for signs of confusion especially in elderly; sive renal failure, potassium supplements or
Advice to patients: May be taken with food or Tablet, Amiloride HCl 5 mg, hydrochlorothiazide 50 may institute safety measures if necessary. other potassium-conserving drugs.
milk to prevent nausea; take early in the day to mg; crimson coloured, diamond shaped tab. “Pema” Dose: Oedema, by mouth, ADULT 100–200 Precautions: Hepatic or renal insufficiency; pa-
Pack: 10 x 10’s (in blisters) mg daily, increased if necessary to 400 tients predisposed to gout (both components
avoid nocturia or sleep disturbance; avoid salt
substitutes and potassium rich foods such as POM ZORETIC® (Emzor) mg daily in resistant oedema; usual can elevate uric acid levels); diabetic patients
oranges and bananas unless otherwise ordered Tablet, Amloride HCI 5 mg, hydrochlorothiazide maintenance dose 25–200 mg daily; (thiazide diuretics can provoke hyperglycaemia
by the physician; report any muscle cramps, 50 mg. CHILD initially 1–3 mg/kg daily in 1–2 and glycosuria); pregnancy, breast-feeding.
weakness, nausea, or dizziness; use caution Pack: 10 x 10’s (in blister) divided doses. Interactions: Lithium (avoid co-administration
when operating machinery or performing Primary hyperaldosteronism, by as thiazides reduce the excretion of lithium).
AMILORIDE plus METHYCLOTHIAZIDE mouth, ADULT, diagnosis, 400 mg Adverse effects: Nausea, vomiting, diarrhoea,
other tasks requiring alertness; photosensitiv-
ity reactions may occur with skin rash, redness, daily for 3–4 weeks (see notes above); muscle cramps, weakness, dizziness, headache,
POM LOMETAZID® (Mark)
itching or sunburn; may increase blood glucose Tablet, Methyclothiazide 5 mg, Amiloride (as HCl preoperative management, 100–400 dry mouth, rash; rarely, photosensitivity reac-
levels in diabetics. dihydrate) 10 mg; faintly yellow tab. mg daily; if not suitable for surgery, tion, anaphylaxis.
Nursing action: See under Spironolactone. Pack: 30’s (in 2 blisters). give lowest effective dose for long- Advice to patients: May be taken with food or
Dose: Adult, 1-2 tabs daily; up to a max. 4 Dose: By mouth, Adult, usually ½-1 tablet daily. term maintenance. milk to minimise nausea; take early in the day
tabs. daily. Not recommended for Children: Not recommended Adjunct in severe heart failure, by to avoid nocturia; take the last dose of multiple
Elderly: Dosage should be carefully adjusted mouth, ADULT usually 25 mg daily. doses early in the evening unless instructed
children. to renal function and clinical response. otherwise; increased sensitivity to sunlight
POM Amiloride plus Hydrochlorothiazide (EDL 14) POM Spironolactone (WMF 16)
Tablet, Spironolactone 25 mg. may occur with skin rash, redness, itching, or
Tablet, Amiloride (as HCl) 5mg, hydrochlorothiazide SPIRONOLACTONE sunburn; may increase blood glucose levels
50 mg. Therapeutic category: Potassium Sparing POM Spironolactone (EDL 14) in diabetics; notify physician if weakness,
POM ADURETIC® (Mark) Diuretic; Antihypertensive. Tablets, Spironolactone 25 mg, 50 mg.
headache, joint swelling, or nausea becomes
Tablet, Amiloride HCI 5 mg, hydrochlorothiazide Indications: Refractory oedema in CHF; ad- POM Spironolactone (Kakaki) severe or persist; may impart a blue fluorescent
50 mg. junct to ACE inhibitor and diuretic in severe Tablets, Spironolactone 25 mg, 50 mg, 100 mg. colour to urine.
188 | 5.2.4 Osmotic diuretics 5.3 Antihypertensive drugs | 189
Nursing action: See also under Hydrochlorothi- urticaria, hypersensitivity reactions; extrava- as 140–159 mmHg systolic blood pressure such as atenolol are effective in all grades of
azide & Amiloride. sation may cause oedema, skin necrosis, and 90–99 mmHg diastolic blood pressure, hypertension, and are particularly useful in
Dose: Adult only, In hypertension, initially, 1-2 thrombophlebitis; rarely, acute renal failure Grade 2 hypertension 160–179 mmHg systolic angina and following myocardial infarction;
tabs daily; adjust according to the pa- (large doses). and 100–109 mmHg diastolic and Grade 3 they should be avoided in asthma, chronic ob-
tients needs up to a max. 4 tabs daily. Dose: Test dose if patient oliguric or renal hypertension more than 180 mmHg systolic structive pulmonary disease, and heart block.
In Oedema, initially, 1 tab. twice daily function is inadequate, by IV infusion, and more than 110 mmHg diastolic. The aim Beta-blockers, especially in combination with
after meals; may be increased to 3 as a 20% solution, 200 mg/kg body of treatment in most patients is an optimal a thiazide, are best avoided in patients with
tabs daily, 2 tabs after breakfast and 1 weight infused over 3–5 minutes; target systolic blood pressure less than 140 diabetes or those at high risk of developing
tab. after lunch. repeat test dose if urine output less mmHg and diastolic blood pressure less than diabetes.
Maintenance dose, 1 tab. daily or 2 than 30–50 mL/hour; if response 85 mmHg. For patients with diabetes the aim Angiotensin-converting enzyme inhibitors
tabs on alternate days. inadequate after second test dose, is systolic blood pressure less than 130 mmHg (ACE inhibitors) such as enalapril are effec-
Elderly: As for the adult. re-evaluate patient. and diastolic blood pressure less than 80 tive and well tolerated by most patients. They
POM DYAZIDE® (GSK)
Raised intracranial or intraocular pres- mmHg. In some patients these targets are not can be used in heart failure, left ventricular
Tablet, Triamterene 50 mg, hydrochlorothiazide sure, by IV infusion, as a 20% solution possible despite adequate treatment; however, dysfunction and diabetic nephropathy, but
25 mg; peach-coloured, half-scored, circular tab. infused over 30–60 minutes, ADULT any decrease in blood pressure reduces the risk should be avoided in renovascular disease and
marked ‘SKF E93’. 0.25–2 g/kg; CHILD 0.5–1.5 g/kg. of cardiovascular disease. in pregnancy. The most common adverse affect
Cerebral oedema, by IV infusion, as a Lifestyle changes should be introduced for is a dry persistent cough.
5.2.4 Osmotic diuretics 20% solution infused rapidly, ADULT all patients; they include weight reduction,
and CHILD 1 g/kg body weight. Dihydropyridine calcium-channel blockers
Osmotic diuretics, such as mannitol, are ad- reduction in alcohol intake, reduction of die- such as amlodipine are useful for isolated
Pharmaceutical precautions: Solutions containing
ministered in sufficiently large doses to raise tary sodium, stopping tobacco smoking, and systolic hypertension, in populations un-
more than mannitol 15% may crystallize during
the osmolarity of plasma and renal tubular reduction in saturated fat intake. The patient
EMDEX
storage, crystals must be redissolved by warming responsive to other antihypertensives (for
fluid. Osmotic diuretics are used to reduce solution before use and solution must not be used if should eat a healthy nutritious diet including example Africans). Short-acting formulations
or prevent cerebral oedema, to reduce raised any crystals remain; intravenous administration sets adequate fruit and vegetables and should of nifedipine should be avoided as they may
intraocular pressure or to treat disequilibrium must have a filter; mannitol should not be adminis- exercise regularly. These measures alone may evoke reflex tachycardia and cause large vari-
syndrome. Mannitol is also used to control tered with whole blood or passed through the same be sufficient in mild hypertension, but patients ations in blood pressure.
intraocular pressure during acute attacks of transfusion set as blood. with moderate to severe hypertension will also
require specific antihypertensive therapy. Drugs acting on the central nervous system
glaucoma. Reduction of cerebrospinal and POM Mannitol (WMF 16)
are also effective antihypertensive drugs. In
intraocular fluid pressure occurs within 15 Injectable solution, Mannitol 10%, 20%. Drug treatment of hypertension particular, methyldopa is effective in the treat-
minutes of the start of infusion and lasts for 3–8 POM Mannitol (EDL 26.2) There are no significant differences between ment of hypertension in pregnancy.
hours after the infusion has been discontinued; Infusions, Mannitol 10%, 20%. the major groups of antihypertensive drugs A single antihypertensive drug is often not
diuresis occurs after 1–3 hours.
POM Mannitol (Dana) in terms of efficacy, side-effects and quality of adequate and other antihypertensive drugs
Circulatory overload due to expansion of Infusion, Mannitol 10 %, 20 %; in water for injection. life although some differences in response are are usually added in a stepwise manner until
extracellular fluid is a serious adverse effect Pack: PVC pouches of 500 mL seen related to age or ethnic group. Therefore, blood pressure is controlled.
of mannitol; as a consequence, pulmonary antihypertensive treatment should be selected
oedema can be precipitated in patients with 5.3 Antihypertensive drugs according to the individual’s clinical needs, Hypertensive emergencies
diminished cardiac reserve, and acute water any conditions that render certain drugs less In situations where immediate reduction of
5.3.1 Beta–adrenoceptor blocking drugs
intoxication may occur in patients with inade- suitable for the individual, and the availability blood pressure is essential and treatment by
5.3.2 Vasodilators
quate urine flow. 5.3.3 Alpha-adrenoceptor blocking drugs and cost of drugs. mouth is not possible, intravenous infusion of
5.3.4 Centrally acting antihypertensive drugs In the absence of compelling indications for sodium nitroprusside is effective. Over-rapid
MANNITOL 5.3.5 Angiotensin-converting enzyme inhibitors reduction in blood pressure is hazardous and
another class of drug, thiazide diuretics, such as
Indications: Cerebral oedema; raised intraoc- (ACEIs) can lead to reduced organ perfusion and cer-
5.3.6 Angiotensin-receptor blockers (ARBs)
hydrochlorothiazide (see also section 5.2.1),
ular pressure (emergency treatment or before ebral infarction.
5.3.7 Calcium-channel blockers should usually be considered for antihyperten-
surgery). Hypertension in pregnancy
5.3.8 Diuretics (see also section 5.2) sive therapy; they are particularly indicated in
Contra-indications: Pulmonary oedema; in-
the elderly. They have few adverse effects in This is defined as a sustained diastolic blood
tracranial bleeding (except during craniotomy); Management of hypertension (See also
low doses, but in large doses they may cause pressure of 90 mmHg or more. Drug therapy
severe congestive heart failure; metabolic EMDEX Vol. 3 for details on Management of
a variety of unwanted metabolic effects (prin- for chronic hypertension during pregnancy re-
oedema with abnormal capillary fragility; se- Hypertension in Blacks)
cipally potassium depletion), reduced glucose mains controversial. If diastolic blood pressure
vere dehydration; renal failure (unless test dose Treatment of hypertension should be inte- tolerance, ventricular ectopic beats and impo- is greater than 95 mmHg, methyldopa is the
produces diuresis). grated into a programme to manage all factors tence; they should be avoided in gout. These safest drug. Beta-blockers should be used with
Precautions: Monitor fluid and electrolyte that increase the risk of cardiovascular events effects can be reduced by keeping the dose as caution in pregnancy, since they can restrict
balance; monitor renal function. (such as stroke and MI); the overall risk of low as possible; higher doses do not produce fetal growth if used for an extended period;
Adverse effects: Fluid and electrolyte imbal- CVD should be assessed for all patients with an increased reduction in blood pressure. intrauterine growth restriction is minimized if
ance (for symptoms see introductory notes); hypertension. Treatment is often life-long. Thiazides are inexpensive and, when used in use is limited to the third trimester. ACE inhib-
circulatory overload, acidosis; pulmonary Hypertension was formerly classified as mild, combination, can enhance the effectiveness itors are contraindicated in pregnancy since
oedema particularly in diminished cardiac moderate or severe, but a grading system is of many other classes of antihypertensive drug. they may damage fetal and neonatal blood
reserve; chills, fever, chest pain, dizziness, visual now preferred. Grade 1 hypertension is defined
disturbances; hypotension or hypertension; Beta-adrenoceptor antagonists (beta-blockers) pressure control and renal function. Women
190 | 5.3.1 Beta–adrenoceptor blocking drugs 5.3.1 Beta–adrenoceptor blocking drugs | 191
who are taking these drugs and become (oculomucocutaneous syndrome—reversible Tablet, Atenolol 25 mg. ATENOLOL plus HYDROCHLOROTHIAZIDE
pregnant should have their antihypertensive on withdrawal). 25 mg – 10’s.
POM CARDIOLAB Plus® (Embassy)
therapy changed immediately. Advice to patients: Avoid abrupt withdrawal POM INTERNOLOL® (Reals) Tablet, Atenolol 25 mg, hydrochlorothiazide 25 mg.
Pre-eclampsia and eclampsia. If pre-eclampsia of the drug; adhere to dosage regimen; watch Tablet, Atenolol 50 mg. Pack: 10’s.
or severe hypertension occurs after week 36 of for postural hypotension; take at the same 50 mg – 3 x 10’s (in strips).
pregnancy, delivery is the treatment of choice. time each day; may mask diabetes symptoms; POM RATENOL® (Seagreen) BISOPROLOL
For acute severe hypertension in pre-eclampsia notify physician if any adverse effects occur; Tablets, Atenolol 50 mg, 100 mg Therapeutic category: Antihypertensive;
or eclampsia, intravenous hydralazine can use with caution while driving or performing 50 mg – 28’s ß1-blocker.
be used. Magnesium sulfate (section 11.1) is tasks requiring alertness; may be taken without 100 mg – 28’s
Pharmacology: Bisoprolol is a highly ß1-se-
the treatment of choice to prevent eclamptic regard to meals.
POM TELOL® (Medreich) lective adrenoceptor antagonist with low
convulsions in eclampsia and severe pre-ec- Nursing action: Administer tablet whole or Tablets, Atenol 25 mg, 50 mg; white f-c tabs. ß2-receptor affinity. It has nointrinsic sympa-
lampsia. crushed before meal or at bedtime. 25 mg – 10’s (in blisters) thomimetic activity nor membrane-stabilising
• Counsel that the drug should be withdrawn grad- 50 mg – 10’s (in blisters)
ually to prevent worsening of condition; to avoid properties. It reduces blood pressure, and
5.3.1 Beta–adrenoceptor hazardous activities if dizziness occurs. POM TENOLOL® (IPCA) by blockade of the cardiac ß1-receptors, it
blocking drugs • Monitor BP, apical and radial pulses, fluid I&O,daily Tablets, Atenolol 50 mg, 100 mg; f-c tabs. reduces cardiac action, and hence myocardial
weight, respirations, and circulation in extremeties 100 mg – 1000. oxygen demand. The mechanism of action of
ATENOLOL before and during therapy. ß1-adrenergic blocking agents in hypertension
POM TENORMIN® (Reals)
Therapeutic category: Antihypertensive; • Teach patient to take pulse at home and when to Tablets, Atenolol 50 mg, 100 mg; orange f-c tab. is not clear, but it is known that bisoprolol
Antianginal Agent; Beta-adrenergic Blocker. report to the doctor. marked ‘TENORMIN and ICI’. reduces the heart rate and depresses plasma
Indications: Hypertension; angina (section • Atenolol may mask the sympoms hypoglycaemia.
POM TERNOLOL® (Hovid)
renin levels.
5.5); arrhythmias (section 5.4); migraine proph- Dose: Hypertension, by mouth, ADULT 50 Bisoprolol is rapidly absorbed after oral
EMDEX
mg once daily (higher doses rarely Tablet, Atenolol 100 mg.
ylaxis (section 1.9.2). 50 mg – 10’s; 14’s. administration in man and excreted predom-
Contra-indications: History of asthma or bron- necessary). inantly via the urine as unaltered substance
100 mg – 10’s; 14’s.
chospasm (unless no alternative, then with POM Atenolol (WMF 12.3) and metabolites. In man 50% of a dose is
extreme caution and under specialist super- Tablets, Atenolol 50 mg, 100 mg ATENOLOL plus CHLORTALIDONE metabolised in the liver while the other 50% is
vision); uncontrolled heart failure, Prinzmetal POM Atenolol (EDL 10.3) Therapeutic category: Antihypertensive/ eliminated unchanged via the kidneys. None of
angina, marked bradycardia, hypotension, Tablets, Atenodol 50 mg, 100 mg. Diuretic. the metabolites found in man has ß1-receptor
sick sinus syndrome, second – or third-degree Pharmacology: Atenolol is a cardioselective blocking action. In man, the plasma elimination
POM APO-ATENOL® (Lahams)
atrioventricular block, cardiogenic shock; beta-blocker and chlortalidone is a diuretic. half life is 0-12 hours, resulting in a duration
Tablet, Atenolol 100 mg; white scored tab. marked
metabolic acidosis; severe peripheral arterial ‘APO A100’. The combination produces a 24-hour antihy- of action of 24 hours. Because of its moderate
disease; phaeochromocytoma (unless used 100 mg – 500. pertensive effect after a single oral dose. hepatic metabolism, it is subject only to a very
with alpha-blocker). Indication: Management of hypertension. small hepatic first pass metabolism. Therefore,
Precautions: Avoid abrupt withdrawal espe- POM ATEDOSE® (Crystal)
Contra-indications, Precautions, etc.: See bisoprolol displays a high bioavailability of 90%
Tablet, Atenolol 50 mg.
cially in ischaemic heart disease; history of Atenolol after an oral dose.
50 mg – 2 x 14’s.
obstructive airways disease (use with caution Dose: By mouth, one tablet daily. Indications: Mild to moderate hypertension
and monitor lung function—see also Con- POM ATELOL® (Zoomota) and angina pectoris.
Not recommended for children. May
traindications above); pregnancy (Appendix 2); Tablets, Atenolol 50 mg, 100 mg; white to off white Contra-indications, Precautions, Adverse
tabs. reduce dose in elderly and in renal
breastfeeding (Appendix 3); first-degree atri- failure effects: See under Atenolol.
50 mg – 10 x 10’s.
oventricular block; liver function deteriorates 100 mg – 10 x 10’s. Advice to patients: Take on an empty stom-
in portal hypertension; reduce dose in renal POM COTENIDONE® (Alpha)
ach or with breakfast. Do not discontinue
POM Atenolol (Alpha) Tablets, Atenolol 50 mg, chlortalidone 12.5 mg;
impairment (Appendix 4); diabetes mellitus medication abruptly; may cause exacerbation
Tablets, Atenolol 25 mg, 50 mg, 100 mg. Atenolol 100 mg, chlortalidone 25 mg.
(small decrease in glucose tolerance, masking of angina pectoris in patients suffering from
of symptoms of hypoglycaemia); history of POM Atenolol (Hochiez) POM HYPORETIC® (Reals) ischaemic heart disease. Discontinuation
hypersensitivity (increased reaction to aller- Tablet, Atenolol 50 mg. Tablet, Atenolol 100 mg, chlortalidone 25 mg; of therapy should be gradual, and patients
50 mg – 10 x 10’s. uncoated tab.
gens, also reduced response to epinephrine should be advised to limit the extent of their
(adrenaline)); myasthenia gravis; interactions: POM Atenolol (Kakaki) physical activity during the period in which
Appendix 1. Tablets, Atenolol 50 mg, 100 mg POM LARETIC® (Lifeback) the medicine is being discontinued. See also
Adverse effects: GI disturbances (nausea, 50 mg – 28’s Tablet, Atenolol 100 mg, chlorthalidone 25 mg; under Atenolol.
vomiting, diarrhoea, constipation, abdom- 100 mg – 28’s uncoated tab.
Dose: By mouth, Hypertension and angina, in-
inal cramp); fatigue; cold hands and feet; POM BETACARD® (Emzor) POM TENORETIC® (Reals) itially 5 mg once daily in the morning;
exacerbation of intermittent claudication and Tablets, Atenolol 50 mg, 100 mg. Tablet, Atenolol 100 mg, chlortalidone 25 mg; f-c tab. increased to 10 mg daily according
Raynaud phenomenon; bronchospasm; brad- Pack: 10’s; 100’s. marked ‘TENORETIC’. to individual response. Up to max. 20
ycardia, heart failure, conduction disorders, POM TENORIC® (Hochiez) mg daily may be needed.
POM BITENOL® (Standard Generics)
hypotension; sleep disturbances, including Tablets, Atenolol 50 mg, 100 mg. Tablet, Atenolol 100 mg, chlortalidone 25 mg; f-c tab. Reduce dose in severe renal or he-
nightmares; depression, confusion; hypogly- 50 mg – 2 x 14’s Pack: 14’s. patic impairment and in elderly.
caemia or hyperglycaemia; exacerbation of 100 mg – 2 x 14’s POM B-COR® (Joswe/Afrab)
psoriasis; rare reports of rashes and dry eyes Tablets, Bisoprolol fumarate 5 mg, 10 mg; f-c tabs.
POM CARDIOLAB® (Embassy)
192 | 5.3.1 Beta–adrenoceptor blocking drugs 5.3.1 Beta–adrenoceptor blocking drugs | 193
Pack: 30’s thyrotoxicosis. Myocardial infarction. Prophy- current use with indomethacin may reduce the NEBIVOLOL
POM CONCOR® (Biofem) laxis of migraine. antihypertensive efficacy of β-blockers. May Therapeutic category: Antihypertensive,
Tablet, (5 mg), Bisoprolol 5 mg; light yellow heart- Contra-indications: Hypersensitivity to me- reduce clearance of lidocaine. May increase β-blocker
shaped f-c tab scored on both sides. toprolol or to any of the components; 2nd effects of hypoglycaemics. Efficacy may be Pharmacology: Nebivolol is a lipophilic
5 mg – 30’s (in blister) or 3rd degree AV block; sick-sinus syndrome; reduced by isoprenaline. Concurrent use with β-receptor blocker administered clinically as
Tablet, (10 mg), Bisoprolol 10 mg; light orange heart- uncontrolled heart failure; clinically relevant digoxin may lead to additive bradycardia. a racemic mixture of equal proportion of two
shaped f-c tab scored on both sides. sinus bradycardia. Severe peripheral arterial Adverse effects: Dizziness, headache, brady- enantiomers, SRRR-nebivolol (or d-nebivolol)
10 mg – 30’s (in blister). circulatory disorders; cardiogenic shock; severe cardia, orthostatic hypotension (occasionally and RSSS-nebivolol (or l-nebivolol). It combines
POM CORBIS® (Phillips) asthma or history of severe bronchospasm; with syncope), fatigue, dyspnoea on exertion. two pharmacological activities:
Tablets, Bisoprolol (as fumarate) 2.5 mg, 5 mg, 10 hypotension; untreated phaeochromocytoma; GI disturbances namely nausea, vomiting, • It is a competitive and selective β-receptor antago-
mg; f-c tabs. metabolic acidosis. Pregnancy (2nd and 3rd abdominal pain. Rarely heart failure, cardiac nist: this effect is attributed to the SRRR-enatiomer
2.5 mg – 10’s (in strips). trimesters). Avoid use in myocardial infarction arrhythmias, palpitation; oedema, Raynaud’s (d-enantiomer).
5 mg – 10’s (in strips). complicated by significant bradycardia, first phenomenon; bronchospasm, diarrhoea • It has mild vasodilating properties due to an inter-
10 mg – 10’s (in strips). action with the L-arginine/nitric oxide pathway.
degree heart block, systolic hypotension (less or constipation; disturbances of libido and
Nebivolol reduces heart rate and blood pressure
than 100 mmHg) and/or severe heart failure. potency; decreased alertness, somnolence
METOPROLOL at rest and during exercise. In healthy volunteers
Precautions: Avoid abrupt drug withdrawal, or insomnia, paraesthesia, rhinitis; cold exit has no significant effect on maximal exercise or
Therapeutic category: Cardioselective be- esp. in patients with ischaemic heart disease. tremities, skin rash, blurred vision, dry eyes, endurance. Nebivolol has no intrinsic sympathico-
ta-adrenergic blocking agent. History of heart failure or patients with poor oculomucocutaneous syndrome. mimetic activity and at pharmacological doses has
Pharmacology: Metoprolol selectively inhibits cardiac reserve e.g. diuretics and/or digitalisa- Dose: By mouth, Adult, Hypertension, Imme- no membrane stabilising effect. It is also devoid
β-adrenergic receptors with a relatively greater tion. Bronchospastic disease, hepatic impair- diate-release preparation: Initially, of alpha-adrenergic antagonism at therapeutic
blocking effect on beta1-receptors (i.e. those ment, AV conduction disorders. May aggravate 50-100 mg daily in single or 2 divided doses. Metabolized in the liver via CYP2D6 pathway;
EMDEX
mediating adrenergic stimulation of heart rate bradycardia and symptoms of peripheral doses; may increase weekly to a max. excreted both in urine (38%) and faeces (48%) and
and contractility and release of free fatty acids arterial circulatory disorders. An α-blocker 400 mg daily depending on response. has a half-life of 12-19 hours.
from fat stores) than on beta2-receptors which should be given concurrently in patients with Maintenance: 100-200 mg daily; up to Indications: Treatment of essential hyper-
are chiefly involved in broncho and vasodila- phaeochromocytoma. May mask signs of acute a max. 400 mg daily. tension.
tion. It has no membrane-stabilising effect nor hypoglycaemia by inhibition of sympathetic Extended-release preparation: 25- Contra-indications: Hypersensitivity to Ne-
partial agonist (intrinsic sympathomimetic) nerve functions. May mask symptoms of hyper- 100 mg once daily. bivolol and sulfonamides; hepatic dysfunction;
activity. The stimulant effect of catecholamines thyroidism. Caution when used in patients with Angina pectoris, 50-100 mg 2-3 times pregnancy and lactation. Cardiogenic shock,
on the heart is reduced or inhibited by meto- history of cardiac failure or those with minimal daily. uncontrolled heart failure, sick sinus syndrome
prolol. This leads to a decrease in heart rate, cardiac reserve. Anaesthetic agents with little Cardiac arrhythmias, 50 mg 2-3 times; including SA block, 2nd and 3rd degree heart
cardiac contractility and cardiac output. or no negative inotropic activity should be increased to 300 mg daily in divided block, history of bronchospasm & bronchial
It is absorbed readily and completely from the preferred in patients on beta-blocker. May doses if needed. asthma.
GI tract (oral); reaching peak plasma concen- impair ability to drive or operate machinery. Adjunct in hyperthyroidism, 50 mg 4 Dose: Adult, by mouth, 5 mg once daily,
trations after 1.5-2 hr. Bioavailability increases May antagonize effect of adrenaline, e.g. in the times daily. preferably at the same time of the
if given with food. Distributed widely, crosses treatment of anaphylaxis drug caused by other Prophylaxis of migraine, 100-200 mg day, with or without meals.
the placenta and enters breast milk. Pro- agents. Myasthenia gravis; history of psychiat- daily in divided doses (morning and May increase dose q2 wks if necessary
tein-binding: 12%. Extensively metabolised by ric disorder. Pregnancy, lactation. evening). up to a max. 40 mg/day.
CYP2D6. Excretion is via urine (as metabolites Note: The BP lowering effect becomes evident after
Interactions: Additive effect with catecho- Myocardial infarction, Early inter-
and unchanged drug). Elimination half-life: 3-4 1-2 weeks of treatment. Occasionally, the optimal
lamine-depleting drugs e.g. reserpine and vention: 50 mg every 6 hours for 48 effect is reached only after 4 weeks.
hr (fast hydroxylators), 7 hr (poor hydroxylators MAOls. May antagonise β1-adrenergic stim- hours, preferably within 12 hours of
). Poor metabolisers (approx. 10%) show higher ulating effects of sympathomimetics e.g. the onset of chest pain. POM NEBILONG® (Micronova)
plasma concentrations and slower elimination adrenaline. Additive negative effects on SA or Maintenance: 200 mg daily given in Tablet, Nebivolol HCl equiv. to Nebivolol 5 mg.
than extensive metabolisers. 5 mg – 84’s
AV nodal conduction with cardiac glycosides, divided doses; to be continued for at
Because of variation in rates of metabolism, the non-dihydropyridine calcium-channel blockers least 3 months.
dose of metoprolol should always be adjusted NEBIVOLOL plus
(verapamil, diltiazem). Paradoxical response Reduce dose in hepatic impairment. HYDROCHLOROTHIAZIDE
to the individual requirements of the patient. to epinephrine may occur. Increased plasma Administration: Extended release tablets may be
As the therapeutic response, adverse effects concentrations with CYP2D6 inhibitors (e.g. divided in half; do not crush or chew. Administer POM NEBILONG-H® (Micronova)
and relative cardioselectivity are related to immediate release tablets with or immediately Tablet, Nebivolol HCl equiv to Nebivolol 5 mg, Hy-
bupropion, cimetidine, diphenhydramine,
plasma concentration, poor metabolisers may following food. drochlorothiazide 12.5 mg.
fluoxetine, hydroxychloroquine, paroxetine, Pack: 30’s
require lower than normal doses. Dosage ad- propafenone, quinidine, ritonavir, terbinafine, (Additional information sourced from Metoprolol monograph
Dose:Adult, by mouth, 1 tablet once daily, preferably
justment is not routinely required in the elderly thioridazine). Increased risk of hypotension and
http://www.medicines.org.uk)
each morning.
or in patients with renal failure, but dosage may heart failure with myocardial depressant (-ve
need to be reduced in patients with significant POM METAP-XL® (Micronova)
inotropic) general anaesthetics (e.g. diethyl Tablet, (25 mg), Metoprolol succinate 23.75 mg PROPRANOLOL
hepatic dysfunction when metoprolol elimina- ether). Reduced plasma levels with rifampicin. equiv. to Metoprolol tartrate 25 mg; extended-re- Therapeutic category: Antihypertensive; An-
tion may be impaired. May increase negative inotropic and negative lease tab. tianginal Agent; Antiarrhythmic Agent; ß-Adren-
Indications: Hypertension and angina pectoris, chronotropic effect of anti-arrhythmic drugs Tablet, (50 mg), Metoprolol succinate 47.5 mg equiv. ergic Blocker.
cardiac arrhythmias, especially supraventricu- e.g. quinidine and amiodarone. Propafenone to Metoprolol tartrate 50 mg; extended-release tab.
Pharmacology: Propranolol is a non-selective
lar tachyarrhythmias. Adjunct to treatment of may increase serum levels of metoprolol. Con-
194 | 5.3.1 Beta–adrenoceptor blocking drugs 5.3.2 Vasodilators | 195
beta-adrenergic receptor-blocking agent Dysrhythmias, anxiety, tachycardia, blocking properties. The alpha-blocking effect Child: Not recommended.
without intrinsic sympathomimetic activity. It hypertrophic obstructive cardiomyopa- results in decrease in peripheral vascular resist- By IV injection (bolus injection), 50
abolishes the responsiveness of myocardium thy and thyrotoxicosis, 10-40 mg 3-4 ance and a rapid reduction in blood pressure. mg over at least 1 minute; repeated,
and coronary vessels to endogenous and times a day Concurrent beta-blockade protects the heart if necessary, at 5 minute intervals
exogenous catecholamines, reduces the im- Post myocardial infarction, initially 40 from reflex sympathetic drive normally in- until a satisfactory response occurs;
pulse-generating activity of sinus node and mg 4 times a day for 2-3 days starting duced by peripheral vasodilation. maximum 200 mg.
prolongs AV conduction time. Increased atrial between days 5 and 21 after the Indications: For rapid control of blood By IV infusion, 2 mg (2 mL of infusion
and ventricular contraction rate is stopped, infarction; then, 80 mg twice a day to pressure in severely hypertensive patients solution) per minute, until a satisfac-
refraction period is prolonged, myocardial improve compliance including severe Hypertension of pregnancy tory response is obtained; usual effec-
oxygen demand is diminished, arterial blood Phaechromocytoma (use only with an and for use in anaesthesia where a hypotensive tive dose range 50-200 mg, increased
pressure is reduced. alpha-adrenoceptor blocker), Preop- technique is indicated; also in hypertensive in phaeochromocytoma.
Indications: Angina pectoris, cardiac arrhyth- erative: 60 mg daily for 3 days. episodes following acute myocardial infarction. In hypertension of pregnancy, 20 mg
mias, hypertension. Non-operable malignant cases, 30 mg Contra-indications: Second or third degree per hour; may be doubled every 30
Contra-indications: Bronchial asthma, bron- daily. heart block, cardiogenic shock and other con- minutes to a maximum 160 mg per
chitis with bronchospasm, allergic hay fever, By IV injection, Adult, Emergency ditions associated with severe and prolonged hour.
sinus bradycardia or partial heartblock, diabe- treatment of cardiac dysrhythmias hypotension or severe bradycardia; asthma or In hypertensive episodes following
tes, metabolic acidosis, after prolonged fasting. and thyrotoxic crisis only, initially 1 a history of obstructive airways disease; liver acute MI, 15 mg per hour; gradually
Precautions: CHF, late pregnancy, breast-feed- mg (1 mL) injected over one minute; dysfunction. increased to a maximum 120 mg per
ing, elderly, liver disease, renal impairment, repeated at 2-minute intervals Precautions: Late pregnancy, breast-feeding, hour.
avoid abrupt withdrawal in angina. up to a max. dose of 10 mg in con- use during anaesthesia; stop and do not Note: The Infusion solution is made by diluting the
Adverse effects: Bradycardia, AV block, lung scious patients or 5 mg in anaesthe- re-start if liver injury occurs or the patient is contents of 2 ampoules (200 mg) to 200 mL with
EMDEX
oedema, insomnia, tiredness, abdominal pains, sised patients. jaundiced. Sodium Chloride and Dextrose Injection B.P. or 5%
Dextrose Intravenous Infusion B.P. The resultant
allergic reactions, G1 disturbances, CHF, cold POM Propranolol (EDL 10.3)
Interactions: Class 1 antiarrhythmic agents,
infusion solution contains 1 mg/1 mL of labetalol.
extremities, blood disorders, rashes. Tablets, Propranolol (as HCl) 40 mg, 80 mg calcium antagonists of the verapamil type;
Advice to patients: Do not discontinue bronchodilators, cardiac glycoside, noradren- POM Labetalol (EDL 10.3)
abruptly; notify physician if CHF symptoms POM Propranolol (Kakaki) aline, adrenaline, tricyclic antidepressants, Tablets, Labetalol (as HCl) 100 mg, 200 mg.
Tablet, Propranolol 40 mg Injection, Labetalol (as HCl) 5 mg per mL; in 20-mL
become worse or side-effects develop; take cimetidine.
40 mg – 28’s; 1000’'s amp
at the same time each day; may mask diabetes Adverse effects: Postural hypotension (if
symptoms; consult pharmacist or physician POM Apo-Propranolol (Lahams) patients are allowed to assume the upright
before taking with other adrenergic drugs Tablet, Propranolol HCl 40 mg; green scored tab. position within 3 hours of receiving the 5.3.2 Vasodilators
marked ‘APO 40’.
(e.g., cold medications); use with caution while labetalol injection; headache, tiredness, tin-
40 mg – 1000’s. HYDRALAZINE
driving or performing tasks requiring alertness. gling sensation in the scalp, tremor, difficulty
Nursing action: Give with a full glass of water POM CIKANOLOL® (Michelle Lab) in micturition, ejaculatory failure, epigastric Therapeutic category: Peripheral vasodilator/
on empty stomach; co-administration with Tablet, Propranolol (as HCI) 40 mg pain, nausea, vomiting, liver dysfunction, rash. antihypertensive.
aluminium containing antacids may reduce 40 mg – 10 x 10’s (in blisters). Advice to patients: Do not stop medication Indications: In combination therapy in mod-
GI absorption. POM INDERAL® (Reals) without aid of physician; may mask signs and erate to severe hypertension, hypertensive
• Sudden withdrawal can exacerbate angina and Tablets, Propranolol HCl 10 mg, 40 mg, 80 mg; all symptoms of diabetes; dizziness is a common crises; hypertension associated with pregnancy
myocardial infarction; inform the outpatient to pink, round, bi–convex, f–c tabs marked ‘ICI’ on one side effect, avoid alcohol. (including preeclampsia or eclampsia); heart
avoid abrupt withdrawal of the drug but to report side, and tab. name and strength on the reverse. Nursing action: Administer orally, crush or failure (section 5.1).
any unpleasant reactions to the physician. Injection, Propranolol HCl 1 mg per mL; in 1 mL Contra-indications: Idiopathic systemic lu-
allow patient to swallow whole; if administered
• Instruct patient to make positon changes slowly printed glass amp. pus erythematosus, severe tachycardia, high
to prevent fainting.
IV, keep patient recumbent for 3 hours.
POM JUNOLOL® (Juhel) • Instruct patient to check with the doctor before output heart failure, myocardial insufficiency
• Patient’s therapeutic response may be evaluated
Tablet, Propranolol HCl BP 40 mg; pink scored using OTC products such as cold remedies or nasal due to mechanical obstruction, cor pulmonale,
by looking at BP, apical and radial pulses, fluid
I&O, daily weight, respirations,and circulation in biconvex tablet marked ‘PNL/40’ on one side and decongestants. dissecting aortic aneurysm, porphyria.
‘Juhel’ on the reverse. • Inform patient that dizziness may be minimized Precautions: Hepatic impairment (Appendix
extremeties before and during therapy.
40 mg – 10 x 10’s; 500’s. by rising slowly and avoiding sudden position 5); renal impairment (reduce dose, Appendix 4);
• Propranolol may mask the sympoms of shock and
changes as well as hazardous activities. coronary artery disease (may provoke angina,
hypoglycaemia. POM PROP-10® (Fidson)
• Monitor BP (standing and sitting or supine), api-
Dose: By mouth, Adult, Hypertension, initially Tablet, Propranolol HCl 10 mg avoid after MI until stabilized); cerebrovascular
cal/radial pulse; advise patient not to stop drug
80 mg twice a day, increased at 10 mg – 1000’s.
abruptly in order not to exacerbate angina and MI. disease; pregnancy (Appendix 2); breastfeed-
weekly intervals according to re- POM PROPIRAL® (Vatican Bells) Dose: By mouth, initially 100 mg twice daily ing (Appendix 3); occasionally over-rapid blood
sponse; usual dose range is 160–320 Tablet, Propranolol 10 mg. with food, increased fortnightly pressure reduction even with low parenteral
mg per day. 10 mg – 10’s. where required to 200 mg twice daily; doses; interactions: Appendix 1.
Angina, anxiety, migraine, and essen- up to 400 mg twice daily; maximum Adverse effects: Tachycardia, palpitations,
tial tremor, initially 40 mg 2-3 times LABETALOL up to 2400 mg in severe, refractory postural hypotension; fluid retention; gastroin-
daily, increased at weekly intervals Synonym: Ibidomide. hypertension and hypertension of testinal disturbances including anorexia, nau-
according to response; usual dose Therapeutic category: Antihypertensive pregnancy sea, vomiting, diarrhoea, rarely constipation;
range is 80-160 mg per day except in Pharmacology: Labetalol has both be- Elderly: Initially 50 mg twice daily. dizziness, flushing, headache; abnormal liver
angina which is 120-240 mg per day. ta-adrenoceptor as well as alpha-adrenoceptor function, jaundice; systemic lupus erythema-
196 | 5.3.3 Alpha-adrenoceptor blocking drugs 5.3.3 Alpha-adrenoceptor blocking drugs | 197
tosus-like syndrome, particularly in women POM APRESOLINE® (Novartis) zoline compund that is a selective inhibitor of Note: Increases in dose beyond 4 mg increase the
and slow acetylators; nasal congestion, agita- Tablets, Hydralazine HCl 25 mg (yellow s-c tab. the alpha1(postjunctional) subtype of alpha likelihood of excessive postural effects including
tion, anxiety, polyneuritis, peripheral neuritis, marked ‘GF and CIBA’); 50 mg (deep pink s-c tab. adrenergic receptors. Doxazosin and Prazosin syncope, postural dizziness/vertigo and postural
rash, fever, paraesthesia, arthralgia, myalgia, marked ‘HG and CIBA’). have similar abilities to antagonise pressor hypotension. If administration is discontinued for
25 mg – 100. several days, therapy should be restarted using the
increased lacrimation, dyspnoea; raised plasma effects of Phenylephrine (an alpha1 agonist).
Injection, Hydralazine HCl 20 mg; powder in amp. initial dosing regimen.
creatinine, proteinuria, haematuria; blood Pack: 5. The antihypertensive effect of doxazosin results
disorders including haemolytic anaemia, leu- from a decrease in systemic vascular resistance, POM CARDURA® (Pfizer)
kopenia, thrombocytopenia. POM HADAZ® (Goldmoore) with little change in cardiac output. Maximum Tablets, Doxazosin (as mesylate) 2 mg, 4 mg.
Injection, Hydralazine HCl 20 mg per mL. 2 mg – 10’s (blister)
Advice to patients: Report flu-like symptoms; effect usually occurs 2-6 hours after dosing. Bio-
4 mg – 10’s (blister).
rise slowly from sitting/lying position; take availability is approximately 65%, reflecting first
SODIUM NITROPRUSSIDE POM CARDURA® XL (Pfizer)
with meals. pass metabolism of doxazosin by the liver. Food
Nursing action: Give oral drug with meals Indications: Hypertensive crisis (when treat- doesn’t have significant effect on doxazosin Tablets, Doxazosin (as mesylate) 4 mg, 8 mg; con-
to increase absorption; give IV dose in a ment by mouth not possible). bioavailability. No major pharmacokinetic dif- trolled-release tabs).
Contra-indications: Severe hepatic impair- 4 mg – 30’s (blister)
recumbent position; keep for 1 hr after ad- ferences in the elderly and in renal insufficiency.
ment; compensatory hypertension; severe 8 mg – 30’s (blister).
ministration. Indications: Treatment of hypertension; may
• Monitor BP closely with IV use; check IV site for vitamin B12 deficiency; Leber optic atrophy. be used alone or in combination with diuret- POM Doxazosin (Alpha)
extravasation. Precautions: Impaired pulmonary function; ics, beta-adrenergic blocking agents, calcium Tablets, Doxazosin mesylate 2 mg, 4 mg.
• Aid with ambulation; rising may cause orthostasis. hypothyroidism; renal impairment (Appendix channel blockers or ACE inhibitors. Benign 2 mg – 28’s.
• Watch the patient for signs of lupus erythema- 4); ischaemic heart disease, impaired cerebral 4 mg – 28’s.
prostatic hyperplasia (BPH) – see Section 11.4.
tosus-like syndrome (sore throat, fever, skin rash, circulation; hyponatraemia; raised intracranial Contra-indications: Sensitivity to quinazo- POM PENCOR® (Mark)
muscle and joint aches), and report to doctor pressure; elderly; hypothermia; monitor blood lines; severe liver dysfunction; history of or- Tablet, Doxazosin mesylate equiv. to Doxazosin2
immediately.
EMDEX
pressure and blood-cyanide concentration, thostatic hypotension; children below 12 years. mg, 4 mg.
• Emphasize the need to comply with drug regimen.
also blood-thiocyanate concentration if given 2 mg – 10 x 10’s (in blisters)
• Advise patient not to discontinue drug suddenly Precautions: To decrease likelihood of exces-
for more than 3 days; avoid sudden withdrawal 4 mg – 10 x 10’s (in blisters)
but to report adverse reactions to the physician. sive hypotension and syncope, initiate therapy
• Tell patient to avoid OTC preparations unless (reduce infusion over 15–30 minutes to avoid with the 1 mg dose and adjust dose slowly;
prescribed by the doctor. rebound effects); pregnancy (Appendix 2); PRAZOSIN
other antihypertensive agents; impaired he-
Dose: Hypertension, by mouth, ADULT 25 mg breastfeeding (Appendix 3); interactions: patic function or drugs that influence hepatic Synonym: Furazosin.
twice daily, increased if necessary to Appendix 1. metabolism; pregnancy and lactation. Therapeutic category: Antihypertensive;
maximum 50 mg twice daily. Adverse effects: Severe hypotension; effects Adverse effects: Orthostatic hypotension Alpha-adrenergic Blocker.
Hypertensive crisis (including during associated with over-rapid reduction in blood with syncope and other symptoms of lowered Pharmacology: Prazosin relaxes both arterial
pregnancy), by slow IV injection, pressure include headache, dizziness; retching, B.P. such as dizziness, lightheadedness or and venous smooth muscles probably by
ADULT 5–10 mg diluted with 10 mL abdominal pain; perspiration; palpitations, appre- vertigo especially at initiation of therapy or at blocking postsynaptic alpha receptors. It
sodium chloride 0.9%; if necessary hension, retrosternal discomfort; rarely reduced the time of dose increases; headache, weak- causes a decrease in total peripheral vascular
may be repeated after 20–30 minutes platelet count, acute transient phlebitis. ness,oedema, somnolence, nausea, rhinitis; less resistance. The antihypertensive effect is a
(see also Precautions). Adverse effects associated with excessive con- frequently GI symptoms,tremor, rash, pruritus. direct result of peripheral vasodilation. BP is
Hypertensive crisis (including during centration of cyanide metabolite include tachy- Advice to patients: Avoid driving or harzadous lowered in both the supine and standing po-
pregnancy), by IV infusion, ADULT cardia, sweating, hyperventilation, arrhythmias, tasks for 24 hours after the first dose, after sitions. While Prazosin could be used alone in
initially 200–300 µg/minute; mainte- marked metabolic acidosis (discontinue infusion a dosage increase and after interruption of mild hypertension, it is more often employed
nance usually 50–150 µg/minute and give antidote, section 19.2.7). therapy when treatment is resumed. Sit or lie in combination with beta–blockers or diuretics.
Hypertensive crisis (including during Dose: Hypertensive crisis, by IV infusion, down if dizziness or other symptoms of low- It is always started cautiously with low doses
pregnancy), by IM injection, ADULT ADULT initially 0.3–1.5 µg/kg/minute, ered BP occur. Rise from sitting or lying positon because of orthostatic hypotension and syn-
12.5 mg every 2 hours as necessary. increased gradually to 0.5–6 µg/kg/ carefully to minimize orthostatic hypotension. cope which may be severe after the first dose.
minute; maximum dose 8 µg/kg/min- Report to physician if dizziness or palpitations Indications: Essential (primary) hyperten-
POM Hydralazine (WMF 12.3)
ute; stop infusion if response unsatis- are bothersome. sion and secondary hypertension of varied
Tablets, Hydralazine HCl 25 mg, 50 mg.
Injection, (Powder for injection), Hydralazine HCl 20 factory after 10 minutes at maximum Nursing action: Administer first dose at aetiology.
mg; in ampoule. dose; lower doses in patients already bedtime to minimize effect of orthostatic hy- Contra-indications: Sensitivity to quinazo-
being treated with antihypertensives. potension; tablet may be crushed or chewed. lines.
POM Hydralazine (EDL 10.3)
• Advise patient not to drive or operate machinery Precautions: Pregnancy, breast-feeding; not
Tablets, Hydralazine (as HCl) 25 mg, 50 mg. POM Sodium nitroprusside (WMF 12.3)
Injection, Hydralazine (as HCl) 20 mg; powder in amp Infusion, (Powder for infusion), Sodium nitroprusside until stabilized on medication; to make position recommended for Children under 12 years;
50 mg; in ampoule. changes slowly. postural hypotension, dizziness, weakness,
POM Hydralazine (Mark) • Observe patient daily for oedema in feet, legs. rarely loss of consciousness; elderly.
Injection, Hydralazine HCI 20 mg per mL; in water • Monitor pulse, I&O (note fluid retention), daily Adverse effects: Dizziness, headache, drows-
for injection. 5.3.3 Alpha-adrenoceptor weight (inform doctor of any increase), BP (stand-
blocking drugs iness, lack of energy, weakness, orthostatic
Pack: 2 mL x 10's (in ampoules) ing/sitting). hypotension, nausea.
POM APREDIN® (Embassy) Dose: Hypertension, initially 1 mg once daily; Advice to patients: Rise from sitting/lying
DOXAZOSIN
Injection, Hydralazine (as HCl) 20 mg per mL; in increased after 1-2 to weeks to 2 mg carefully; may cause dizziness or drowsiness;
2-mL amp. Therapeutic category: Alpha adrenergic once daily, and thereafter if necessary
blocker/vasodilator. report if painful, persistent erection occurs;
Pack: 2 mL x 10’s (in amps) to 4 mg, 8 mg, and max. 16 mg daily.
Pharmacology: Doxazosin mesylate is a quina- avoid alcoholic beverages.
198 | 5.3.4 Centrally acting antihypertensive drugs 5.3.4 Centrally acting antihypertensive drugs | 199
Nursing action: See under Doxazosin. as rashes; CVS disorders such as orthostatic amenorrhoea; urine darkens on standing. Tablet, Methyldopa 250 mg.
Dose: Hypertension, 0.5 mg at bedtime ini- hypotension; others such as alopecia, hyperg- Advice to patients: May cause urine discol- 250 mg – 100’s.
tially; increasing to 0.5 mg 2-3 times lycaemia, muscle spasm, weakness. ouration; notify physician of unexplained POM FADOPA® (Pharmabox)
daily; then 1 mg 2-3 times daily. Advice to patients: See also under Prazosin. prolonged general tiredness, fever, or jaundice; Tablet, Methyldopa (anhydrous) 250 mg; f-c tab.
Maintenance, 3-20 mg in divided Nursing action: Administer with food if nausea rise slowly from prolonged sitting or lying 250 mg – 10 x 10’s.
doses. occurs and in the morning to prevent nocturia. position and avoid sudden position changes POM GIMET® (Geneith)
See lit. for details. • Monitor weight daily to determine fluid loss. to minimize orthostatic hypotension. Tablet, Methyldopa 250 mg.
• Observe BP standing, sitting and lying because Nursing action: Administer drug before meal.
POM APO-PRAZO® (Lahams) postural hypertension may occur. POM KETHA® (Vixa)
• Give IV injection by infusion over 30 minutes.
Tablet, Prazosin HCl 5 mg; white, scored, dia- • Advise patient to eat food rich in potassium viz Tablet, Methyldopa 250mg
• Transient sedation or depression may be common
mond-shaped tab. marked ‘APO P5’. tomatoes, bananas, oranges. 250 mg – 10 x 10’s; 100’s.
for first 72 hours of therapy (usually disappears
5 mg – 100. • Observe for signs of hypokalaemia such as muscle over time); assist with ambulation. POM Methyldopa (Embassy)
POM MINIPRESS® (Pfizer) weakness and cramps. • Dry mouth can be relieved with chewing gum Tablet, Methyldopa (anhydrous) 250 mg; f-c tab
Tablet, Prazosin HCl 1 mg; scored tab. • See also under Prazosin. or ice chips.
1 mg – 30; 100. Dose: By mouth, initially one tab. once daily • Teach patient not to discontinue medication POM Methyldopa (GoldMoore)
usually in the morning; increase after abruptly (this may cause headache, raised BP, Tablet, Methyldopa.
PRAZOSIN plus HYDROCHLOROTHIAZIDE 2 weeks to 2-4 tabs daily in 2 divided insomnia, tremors, nausea and sweating). POM Methyldopa (Hochiez)
doses if necessary • Advise patient not to drive or operate machinery
Indications: Treatment of mild to moderate Tablet, Methyldopa 250 mg
See lit. for details. until stabilized on medication; to make position 250 mg – 10’s
hypertension in ambulatory patients. changes slowly; to avoid OTC preparations unless
Contra-indications, Precautions, etc.: See POM Prazosin plus Polythiazide (EDL 10.3) prescribed by physician. POM Methyldopa (Pemason)
under Prazosin plus Hydrochlorothiazide. Tablet, Prazosin (as HCl) 0.5 mg, polythiazide 0.25 mg Dose: Hypertension in pregnancy, by mouth, Tablet, Methyldopa (anhydrous) 250 mg
Dose: By mouth, one tablet twice daily; may 250 mg – 100’s
EMDEX
POM MINIZIDE® (Pfizer) ADULT initially 250 mg 2–3 times
be increased to 2 tablets twice daily Tablet, Prazosin HCl 0.5 mg, polythiazide 0.25 mg. daily; if necessary, gradually increased POM MICRODOPA® (Strides Vital)
to get desired results. Pack: 30; 100; 500. at intervals of 2 or more days, maxi- Tablet, Methyldopa 250 mg.
POM MINIPLUS® (Neimeth) mum 3 g daily. 250 mg – 10 x 10’s.
Tablet, Prazosin (as HCl) 0.5 mg, hydrochlorothiazide 5.3.4 Centrally acting POM Methyldopa (WMF 12.3) POM SIVODOPAL® (Adpharm)
12.5 mg. antihypertensive drugs Tablet, Methyldopa 250 mg. Tablet, Methyldopa 250 mg
Pack: 60’s; 500’s. 250 mg – 10 x 10’s.
METHYLDOPA POM Methyldopa (EDL 10.3)
PRAZOSIN plus POLYTHIAZIDE Tablets, Methyldopa 250 mg, 500 mg.
Indications: Hypertension in pregnancy. RESERPINE plus CLOPAMIDE plus
Therapeutic category: Antihypertensive/ POM Apo-Methyldopa (Lahams) DIHYDROERGOCRISTINE
Contra-indications: Depression; active liver
diuretic disease; phaeochromocytoma, porphyria. Tablet, Methyldopa 250 mg; yellow, f-c tab. marked Therapeutic category: Antihypertensive
Pharmacology: Prazosin causes a decrease Precautions: Hhistory of hepatic impairment ‘APO 250’. Pharmacology: Reserpine exerts its effect
in total peripheral vascular resistance. Its 250 mg – 1000’s. through a central action; clopamide is a diu-
(Appendix 5); renal impairment (Appendix 4);
vasodilator effect is related to blockade of blood counts and liver-function tests advised; POM ALDOMEXIN® (Nichben) retic of the thiazide type promoting water and
postsynaptic alpha-1-adrenoceptors. Unlike history of depression; positive direct Coomb Tablet, Methyldopa (anhydrous) 125 mg, 250 mg. sodium excretion; dihydroergocristine inhibits
non-selective alpha-adrenergic blockers, the test in up to 20% of patients (affects blood the hypertensive response to stress. The blood
POM ALDOPRES® (Standard Generics)
antihypertensive action of prazosin is not cross-matching); interference with laboratory Tablets, Methyldopa 250 mg, 500 mg
pressure is usually reduced after 4-7 days and
accompanied by reflex tachycardia. The antihy- tests; pregnancy (Appendix 2) and breastfeed- 250 mg – 10x 10’s (in blisters) optimum effect is achieved after 1-4 weeks.
pertensive effect is a direct result of peripheral ing (Appendix 3); interactions: Appendix 1. 500 mg – 10 x 10’s (in blisters) Indications: Essential hypertension of all
vasodilation. BP is lowered in both the supine Adverse effects: Sedation, dizziness, lighthead- grades of severity.
POM BONDOMET® (Bond)
and standing positions. Polythiazide belongs edness, postural hypotension, weakness, fatigue, Contra-indications: Hypersensitivity to any of
Tablet, Methyldopa 250 mg ; f-c tab
to the benzothiadiazine family of diuretic/ headache, fluid retention and oedema, sexual 250 mg – 10 x 10’s (in blisters) the components and to sulfonamides (Clopa-
antihypertensive agents. Its mechanism of dysfunction; impaired concentration and memory, mide belongs to this group); hypokalaemia
action results in an interference with the renal POM CALDOPA® (Drugfield) resistant to therapy; severe liver or renal dis-
depression, mild psychosis, disturbed sleep and Tablet, Methyldopa 250 mg
tubular mechanism of electrolyte reabsorption. nightmares; drug fever, influenza-like syndrome; orders; severe cardiovascular disease; history
Indications: Treatment of hypertension. nausea, vomiting, constipation, diarrhoea, dry of mental depression; active peptic ulcer;
Contra-indications: Sensitivity to the compo- POM CELODOPA® (JB Pharma) pregnancy, breast-feeding.
mouth, stomatitis, sialadenitis; liver function im-
nent drugs; anuria. Tablets, Methyldopa (anhydrous) 250 mg, 500 mg. Precautions: Diabetes; gout; check serum
pairment, hepatitis, jaundice, rarely fatal hepatic
250 mg –10 x 10’s (in blisters) potassium level regularly; impaired renal func-
Precautions: Postural hypotension; fluid or necrosis; bone-marrow depression, haemolytic 500 mg – 10 x 10’s (in blister)
electrolyte imbalance, hyperuricaemia, latent anaemia, leukopenia, thrombocytopenia, eo- tion; road users due to fatigue or orthostatic
diabetes mellitus and insulin requirements sinophilia; parkinsonism; rash (including toxic POM DOPAFLASH® (Miraflash) hypotension.
in diabetics due to the thiazide; pregnancy, Tablet, Methyldopa Interactions: Corticosteriods, NSAIDs, lithium,
epidermal necrolysis); nasal congestion; black or
breastfeeding. Pack: 10 x 10’s oral anticoagulants, MAOIs, Alcohol, CNS de-
sore tongue; bradycardia, exacerbation of angina;
Adverse effects: GI disturbances such as myalgia, arthralgia, paraesthesia, Bell palsy; pan- POM DOPATAB® (Hovid) pressants, levodopa.
nausea, jaundice; CNS disturbances such as creatitis; hypersensitivity reactions including lupus Tablet, Methyldopa 250 mg; f-c tab. Adverse effects: GI disturbances, electrolyte
dizziness; haematological reactions such as erythematosus-like syndrome, myocarditis, per- 250 mg – 1000 disturbances (hypokalaemia); orthostatic
agranulocytosis; dermatological reactions such icarditis; gynaecomastia, hyper-prolactinaemia, POM DOPATYL® (Embassy) hypotension; fatigue; muscle weakness; na-
200 | 5.3.5 Angiotensin–converting enzyme (ACE) inhibitors 5.3.5 Angiotensin–converting enzyme (ACE) inhibitors | 201
sal congestion; rarely mental depression or stopped for a few days, if possible, before ini- tration times by 1 to 2 hours). Phenothiazines Pharmacology: Enalapril is an ACE inhibitor. It
thrombocytopenia. tiating treatment with ACE inhibitors. The first (increased hypotensive effects). Potassium is a prodrug and undergoes biotransformation
Advice to patients: May cause drowsiness; do dose should preferably be taken at bedtime. preparations or potassium-sparing diuretics to Enalaprilat in the liver. It is eliminated prin-
not drive or operate machinery. Avoid alcoholic Time for onset of hypotensive effect after oral (co-administration may result in elevated po- cipally in the urine with some faecal excretion.
beverages. administration is about 1-1.5 hours (Capto- tassium levels). Time for onset of hypotensive effect after oral
Nursing action: Give with food or milk. pril); within 6 hours (Lisinopril) and about 1 Adverse effects: Tachycardia, chest pain, palpi- administration is about about 1 hour.
• Monitor BP (standing and sitting/supine); weigh
hour (Enalapril). Enalapril is a prodrug and tations, insomnia, headache, dizziness, fatigue, Indications: Hypertension; heart failure
patient daily and notify physician of any weight malaise, rash, pruritus, alopecia, abdominal (section 5.1).
gain. undergoes biotransformation to Enalaprilat
in the liver. It is eliminated principally in the pain, vomiting, nausea, diarrhoea, constipation, Contra-indications: Hypersensitivity to ACE
• Observe for mental depression and alert family to
urine with some faecal excretion. Captopril anorexia, paraesthesias, oliguria, transient cough, inhibitors (including angioedema); renovascu-
report symptoms.
• Advise patient to rise slowly from sitting or lying is about 50% metabolised and 95% excreted hypotension, hyperkalaemia. lar disease; pregnancy (Appendix 2).
position to minimize orthostatic hypotension. in urine within 24 hours. Lisinopril is well Nursing action: Give 1 hr before meal or 2 Precautions: Use with diuretics; hypotension
• Inform patient that drug may cause drowsiness, absorbed and is unaffected by food in the hr after meal; food decreases absorption of with first doses, especially in patients on diu-
impair judgement and coordination; impotence, stomach. It is almost entirely excreted in urine captopril 30-40%. retics, on a low-sodium diet, on dialysis, if dehy-
gynaecomastia may occur but is reversible. • Watch for hypotensive effect within 1-3 hours of drated, or with heart failure; peripheral vascular
as unchanged drug.
• Dry mouth can be relieved by chewing gum or first dose or new higher dose; advise patient to disease or generalized atherosclerosis (risk of
ice cube chips. These drugs may cause impairment of renal make position changes slowly. clinically silent renovascular disease); use with
• Advise patient to avoid OTC preparations unless function which may progress and become • Monitor patient’s BP and pulse rate frequently,
great care in severe or symptomatic aortic
on prescription. severe. At particular risk are those with pre-ex- and report excessive perspiration, vomiting and
diarrhoea.
stenosis; monitor renal function before and
Dose: By mouth, initially 1 tab. daily; in- isting renal disease or impairment, the elderly,
• Advise patient to check with doctor before taking during treatment; renal impairment (reduce
creased to 2-3 tabs daily in severe hy- and those with bilateral renal artery stenosis.
any other drug including OTC medications. dose, see also Appendix 4); hepatic impairment
EMDEX
pertension. Maintenance, 1 tab daily Concomitant treatment with NSAIDs or po-
Dose: Mild to moderate hypertension, by (Appendix 5); possibly increased risk of agran-
or every other day. Dosage should tassium-sparing diuretics and use of potassi-
mouth, 12.5 mg twice daily; usual ulocytosis in collagen vascular disease; history
not be increased more frequently um-containing salt substitutes may increase
maintenance dose 25 mg twice daily; of idiopathic or hereditary angioedema (use
than once per week. the risk. Renal function and electrolytes should
increased at 2-4 week intervals if with care or avoid); breastfeeding (Appendix
POM Reserpine plus Clopamide plus Dihydro- be checked before starting treatment with an 3); interactions: Appendix 1.
necessary up to a maximum 50 mg
ergocristine (EDL 10.3) ACE inhibitor, and monitored during treatment. USE WITH DIURETICS: Risk of very rapid falls in
twice daily.
Tablet, Reserpine 0.1 mg, clopamide 5.0 mg, dihy- blood pressure in volume-depleted patients;
CAPTOPRIL CHF, initially 6.25-12.5 mg 3 times
dro-ergocristine 0.5 mg. treatment should therefore be initiated with
daily in conjunction with cardiac
Reserpine + Dihydroergotoxine Therapeutic category: Antihypertensive very low doses. High-dose diuretic therapy
glycoside and diuretic therapy; initial
+ Hydrochlorothiazide Pharmacology: Captopril is a specific com- (furosemide dose greater than 80 mg daily)
dose depends upon patient’s fluid/
petitive inhibitor of angiotensin 1-converting should be discontinued, or dose significantly
POM SINEPRESS®(Taylek) electrolyte status
enzyme, the enzyme responsible for the reduced, at least 24 hours before starting enal-
Tablet, Dihyroergotoxine mesylate 0.6 mg, reserpine Not recommended for children.
0.1 mg, hydrochlorothiazide 10 mg; coated tab. conversion of angiotensin I to angiotensin april (may not be possible in heart failure—risk
II. Angiotensin, an octapeptide, is a potent POM Captopril (EDL 10.3)
Pack: 50; 500. of pulmonary oedema). If high-dose diuretic
Dose: By mouth, usually 1-2 tabs daily; increased if endogenous vasoconstrictor substance and Tablets, Captopril 12.5 mg, 25 mg, 50 mg.
cannot be stopped, medical supervision ad-
necessary to 3 tabs daily. also stimulates aldosterone secretion from POM ACERIDEX® (Pemason) vised for at least 2 hours after administration
the adrenal cortex, thereby contributing to Tablet, Captopril 25 mg; white tab. or until blood pressure stable.
5.3.5 Angiotensin–converting sodium and fluid retention and potassium loss. 25 mg – 90’s (in a blister). ANAPHYLACTOID REACTIONS: Avoid enalapril
enzyme (ACE) inhibitors Captopril causes a decrease in angiotensin II POM APO-CAPTO® (Lahams) during dialysis with high-flux polyacrilonitrile
ACE inhibitors inhibit the conversion of angio- and an increase in plasma renin activity (PRA). Tablets, Captopril 12.5 mg, white, double-scored, membranes and during low-density lipo-
tensin I to angiotensin II (a potent vasoconstric- It produces a reduction in peripheral arterial oblong tab. marked ‘APO 12.5’; 25 mg, white, dou- protein apheresis with dextran sulfate; also
tor); this results in lower levels of angiotensin resistance in hypertensive patients. ble-scored tab. marked ‘APO 25’. withhold before desensitization with wasp or
Indications: Management of hypertension 12.5 mg – 100’s
II which causes an increase in plasma renin bee venom.
and treatment of CHF; also in hypertensive 25 mg – 100’s.
activity and a reduction in aldosterone se- Adverse effects: Dizziness, headache; less
cretion. They also prevent the degradation of crisis, diabetic nephropathy, postmyocardial POM CAPTEZ® (Jubilee) commonly, nausea, diarrhoea, hypotension
Bradykinin (a vasodilator). Examples include infarction for prevention of ventricular failure. Tablet, Captopril 25 mg; white scored tab. (severe in rare cases), dry cough, fatigue, asthe-
Captopril, Enalapril, Lisinopril, Ramipril, Contra-indications: Hypertensensivity to POM Captopril (Kakaki) nia, muscle cramps, rash and renal impairment;
Perindopril Erbumine. captopril and other ACE inhibitors. Tablet, Captopril 50 mg rarely, vomiting, dyspepsia, abdominal pain,
Precautions: Renal impairment (reduce dos- 50 mg – 56’s constipation, peptic ulcer, glossitis, stomatitis,
They are used in hypertension, and in conges- age); severe hypotension may occur in patients
tive heart failure (usually starting with a low POM SIVOPRIL® (Adpharm) ileus, anorexia, pancreatitis, liver damage,
who are taking diuretics, who are sodium and/ chest pain, palpitations, arrhythmias, Raynaud
dose e.g. 6.25 mg captopril). Other uses include Tablet, Captopril 25 mg.
or volume depleted and also in elderly (initiate 25 mg – 2 x 14’s. syndrome, angioedema, bronchospasm, rhin-
hypertensive crisis, diabetic nephropathy, lower doses and monitor closely when starting
myocardial infarction. orrhoea, dry mouth, sore throat, pulmonary
therapy in these patients). ENALAPRIL infiltrates, paraesthesia, vertigo, nervousness,
These drugs may cause very rapid falls in Interactions: NSAIDs esp. indomethacin (re- depression, confusion, drowsiness insomnia,
Synonym: Enalaprilat.
BP in some patients and it is therefore rec- duced hypotensive effect). Antacids (reduced dream abnormalities, pruritus, urticaria, alo-
Therapeutic category: Antihypertensive.
ommended that diuretic therapy should be bioavailability of captopril – separate adminis- pecia, flushing, impotence, gynaecomastia,
Stevens-Johnson syndrome, toxic epidermal POM ENCARD® (Laider) Contra-indications: Hypersensitivity to ACE 5 mg – 2 x 14’s (in blisters)
necrolysis, exfoliative dermatitis, pemphigus, Tablets, Enalapril (as maleate) 5 mg, 10 mg. inhibitors; history of angioneurotic oedema 10 mg – 2 x 14’s (in blisters).
taste disturbance, tinnitus, blurred vision; elec- 5 mg – 5 x 10’s (in blisters) either hereditary or idiopathic or associated POM GRESTAT® (Greenlife)
trolyte disturbances and hypersensitivity-like 10 mg – 5 x 10’s (in blisters) with previous ACE inhibitors. Tablets, Lisinopril (dihydrate) 5 mg, 10 mg, 20 mg.
reactions (including fever, myalgia, arthralgia, POM ENVAS® (Interpharma) Precautions: Volume depleted patients and 5 mg – 2 x 14’s (in blisters).
eosinophilia, and photosensitivity) reported. Tablets, Enalapril maleate 2.5 mg, 5 mg, 10 mg CHF (symptomatic hypotension may occur); 10 mg – 2 x 14’s (in blisters).
Nursing action: Stop any diuretic 2-3 days 2.5 mg – 10 x 10’s ischaemic heart or cerebrovascular disease; 20 mg – 2 x 14’s (in blisters).
before beginning enalapril therapy to help 5 mg – 10 x 10’s history of angioedema; patients undergoing POM HIPRIL® (Strides Vital)
10 mg – 10 x 10’s
reduce the risk of hypotension; a diuretic desensitisation treatment and certain haemo- Tablets, Lisinopril 5 mg, 10 mg, 20 mg.
may be added later if enalapril alone fails to POM LOTRIAL® (Solidum) dialysis procedures (anaphylactoid reactions 5 mg – 10’s.
control the BP. Tablets, Enalapril (as maleate) 5 mg, 10 mg; f-c may occur); renal impairment (reduce dose or 10 mg – 10’s.
• Monitor BP and pulse regularly. scored tabs avoid); surgery/anaesthesia (hypotension may 20 mg – 10’s.
• Advise patient to comply with drug schedule; also 5 mg – 30’s; 100’s occur); pregnancy and breastfeeding. POM INTERPRIL® (Reals)
not to discontinue drug suddenly but to report 10 mg – 30’s; 100’s
Interactions: Diuretics, other anti-hyperten- Tablets, Lisinopril 5 mg, 10 mg.
adverse reaction to the doctor. POM NURIL® (Synergy) sives, probenecid (increased hypotensive 5 mg – 3 x 10’s (in strips).
• Notify physician if swelling of the face, extremities, Tablets, Enalapril maleate USP 5 mg, 10 mg; un- 10 mg – 3 x 10’s (in strips).
lips, tongue, or glottis occurs (angioedema).
effects). Aspirin, indomethacin (decreased
coated tabs. effect of lisinopril). Potassium supplements, po-
• Watch for hypotensive effects within 1-3 hours POM ISOPRIL® (Korlyns)
of first dose or new higher dose. Advise patient POM OLINAPRIL® (Taylek) tassium-sparing diuretics (increased potassium Tablet, (5 mg), Lisinopril (anhydrous) 5 mg; pink
to avoid sudden postural changes to minimize Tablets, Enalapril 5 mg, 10 mg. levels). Allopurinol (increased hypersensitivity scored tab. marked “ISP-5”.
orthostatic hypotension. 5 mg – 20’s. reactions). 5 mg – 2 x 14’s.
• Advise patient to check with doctor or pharmacist 10 mg – 20’s. Adverse effects: Nausea, headache, fatigue, Tablet, (10 mg), Lisinopril (anhydrous) 10 mg; sky-
EMDEX
before taking OTC medications. cough, rash, diarrhoea, orthostatic effects, blue scored tab. marked “ISP”.
POM REOMIN® (Theodor)
• Enalapril is similar to captopril and other ACE inhib- 10 mg – 2 x 14’s.
Tablets, Enalapril maleate USP 5 mg, 10 mg, 20 mg; asthenia, GI irritation; rarely angioneurotic
itors, but has a longer duration of action.
white round tabs. oedema (discontinue); palpitations; abdominal POM KUINOPRIL® (Drugfield)
Dose: Hypertension, by mouth, initially 5 mg Pack: 20’s (in blisters). Tablets, Lisinopril 5 mg, 10 mg
pain, dry mouth, hepatitis, alopecia, cholestatic
once daily; lower initial dose if used 5 mg – 1 x 30’s (in blisters)
POM ROLAPRIL® (Adpharm) jaundice; increases (usually reversible) in blood
in addition to diuretic or in renal 10 mg – 1 x 30’s (in blisters)
Tablet, Enalapril maleate 10 mg urea, serum creatinine, liver enzymes and se-
impairment; usual maintenance dose
10 mg – 3 x 10’s rum bilirubin; thrombocytopenia, neutropenia, POM LIPRIL® (Medreich)
20 mg once daily; maximum 40 mg
granulocytosis, hyperkalaemia. Tablet, (2.5 mg), Lisinopril 2.5 mg; blue tab.
once daily. POM VASORETEC® (Joswe/Afrab)
Advice to patients: See under Enalapril. 2.5 mg – 28’s (in blisters)
Tablets, Enalapril maleate 5 mg, 10 mg, 20 mg
POM Enalapril (WMF 12.3) Nursing action: See under Enalapril. Tablet, (5 mg), Lisinopril 5 mg; white tab.
5 mg – 20
Tablet, Enalapril 2.5 mg. Dose: Hypertension, initially 10 mg once 5 mg – 28’s (in blisters)
10 mg – 20
Tablet, (10 mg), Lisinopril 10 mg; yellow tab.
POM AFAPRIL® (Afrab-Chem) 20 mg – 20. daily (lower starting dose required
Tablet, Enalapril maleate 5 mg, 10 mg POM MEPAWAT® (Watson)
in patients with renal impairment, Tablet, (20 mg), Lisinopril 20 mg; orange tab.
Pack: 30’s (in blisters). Tablet, Enalapril 5 mg, 10 mg. renovascular hypertension, volume or 20 mg – 28’s (in blisters)
POM APO-ENALAPRIL® (Lahams)
salt depleted patients, when diuretics
POM LISIN® (Mecure)
Tablets, Enalapril maleate 5 mg, white, scored, bar- ENALAPRIL plus cannot be discontinued, and some
HYDROCHLOROTHIAZIDE Tablets, Lisinopril 5 mg, 10 mg, 20 mg.
rel-shaped tab. marked ‘APO E5’; 10 mg, rust red tab. elderly patients); usual maintenance
marked ‘APO E 10’. dose 10-20 mg daily. Adjust dosage POM LISINOPIN® (Geneith)
POM ENARETIC® (Pharma Ethics) Tablets, Lisinopril 10 mg, 20 mg.
5 mg – 100 Tablet, Enalapril 10 mg, hydrochlorothiazide 25 mg. according to blood pressure response
10 mg – 100 upto a max. 80 mg daily. 10 mg – 1 x 10’s
Pack: 3 x 10’s 20 mg – 1 x 10’s
POM ENALADEX® (Pemason) CHF, initially 2.5 mg once daily; usual
Tablet, (5 mg), Enalapril (as maleate) 5 mg; white tab. LISINOPRIL maintenance dose 5-20 mg daily. To POM Lisinopril (Alpha)
5 mg – 30’s. be used together with diuretics and Tablets, Lisinopril 5 mg (scored tab), 10 mg, 20 mg.
Therapeutic category: Antihypertensive. 5 mg – 28’s.
Tablet, (10 mg), Enalapril (as maleate) 10 mg; pink
Pharmacology: Lisinopril is an ACE inhibitor. appropriate digitalis.
tab. Acute myocardial infarction (within 24 10 mg – 28’s.
10 mg – 30’s.
Time for onset of hypotensive effect after oral 20 mg – 28’s.
administration is within 6 hours. Lisinopril is hours in haemodynamically stable
POM Enalapril (Alpha) patients), initially 5 mg, followed POM Lisinopril (Crystal)
well absorbed and is unaffected by food in the
Tablets, Enalapril 2.5 mg, 5 mg, 10 mg. by 5 mg after 24 hours; then 10 mg Tablet, Lisinopril (as dihydrate) 10 mg; uncoated tab.
stomach. It is almost entirely excreted in urine 10 mg – 3 x 10’s (in blisters)
2.5 mg – 28’s. after 48 hours and 10 mg once daily
as unchanged drug.
5 mg – 28’s. thereafter. POM LISINOTAB® (Lifeback)
10 mg – 28’s. Indications: Essential and renovascular hyper-
tension; congestive heart failure (CHF) as an Renal complications, 10-20 mg once Tablets, Lisinopril (as dihydrate) 5 mg, 10 mg; un-
POM Enalapril (Drugfield) daily. coated tabs.
adjunctive treatment with diuretics and where
Tablet, Enalapril (as maleate) 10 mg 5 mg – 2 x 14’s
appropriate digitalis; haemodynamically stable POM Lisinopril (EDL 10.3) 10 mg – 2 x 14’s
patients within 24 hours of an acute myocar- Tablets, Lisinopril 5 mg, 10 mg.
POM ENAPROX® (Crystal) dial infarction (AMI); renal complications of POM LISORIL® (IPCA)
POM GAPRIL® (Pharmabase) Tablets, Lisinopril 2.5 mg, 5 mg, 10 mg, 20 mg
Tablet, Enalapril 10 mg. diabetes. Tablets, Lisinopril 5 mg, 10 mg; uncoated tabs. Pack: 14’s.
10 mg – 10 x 10’s.
POM LISPRIL® (Zoomota) LISINOPRIL plus Tablet, Lisinopril 5 mg, hydrochlorothiazide 12.5 nia, headache, disturbances of mood and/or
Tablet, (5 mg), Lisinopril 5 mg; white tab. HYDROCHLOROTHIAZIDE mg; uncoated tab. sleep have been reported. Less often, taste
5 mg – 3 x 10’s (in blisters). Therapeutic category: Antihypertensive/ Pack: 3 x 10’s (in blisters). impairment, epigastric discomfort, nausea,
Tablet, (10 mg), Lisinopril dihydrate equiv. to Lisino- Diuretic. abdominal pain, and rash. Reversible increases
POM MORVAL-D® (Embassy)
pril 10 mg; white tab. Indications: Treatment of essential hyperten- Tablet, Lisinopril 5 mg, hydrochlorothiazide 12.5 mg in blood urea and creatinine; Proteinuria may
10 mg – 3 x 10’s (in blisters).
sion for patients in whom combination therapy Pack: 10’s. occur. Rarely, angioneurotic oedema and de-
POM MORVAL® (Embassy) is appropriate. creases in hemoglobin, red cells, and platelets.
POM NEPIN H® (Nosak)
Tablets, Lisinopril 5 mg, 10 mg. Contra-indications: Hypersensitivity to any Dose: Hypertension, 4 mg once a day in the
Tablet, Lisinopril 5 mg, hydrochlorothiazide 12.5
5 mg – 10’s. component of the preparation; anuria; history mg; uncoated tab. morning; may be increased to 8 mg
10 mg – 10’s. of angioedema relating to ACE inhibitor, Pack: 2 x 10’s. once daily after 1 month. To be taken
POM NEPIN® (Nosak) hereditary or idiopathic angioedema; hyper- before food.
POM PEMAPRIL®-Plus (Pemason)
Tablets, Lisinopril 5 mg, 10 mg; uncoated tabs. sensitivity to sulphonamide derived drugs; Stable coronary artery disease, Initially
Tablet, Lisinopril 10 mg, hydrochlorothiazide 12.5
5 mg – 3 x 10’s (in blisters) pregnancy and lactation. 4 mg once daily for 2 weeks, then in-
mg; white oblong scored tab. marked “Pema-P”.
10 mg – 3 x 10’s (in blisters). Precautions: Symptomatic hypotension es- Pack: 10 x 10’s; 100’s. creased to 8 mg once daily, depend-
POM NOSTRES®-5 (Pharmgate) pecially in the presence of fluid or electrolytes Caplet, Lisinopril anhydrous 10 mg, hydrochlorothiazide ing on renal function and provided
Tablets, Lisinopril 5 mg, 10 mg. imbalance, e.g. volume depletion (monitor 12.5 mg; uncoated cap. that the 4 mg dose is well tolerated.
5 mg – 2 x 14’s serum electrolytes periodically); avoid in renal Pack: 2 x 14’s (in blisters) Elderly: 2 mg once daily for one week,
10 mg – 2 x 14’s insufficiency; impaired hepatic function or pro- then 4 mg once daily the next week,
POM TOROPRIL-H® (Toro)
POM PEMAPRIL® (Pemason) gressive liver disease (alterations of fluid and Tablet, Lisinopril (anhydrous) 20 mg, hydrochloro- before increasing the dose up to 8
Caplet, (5 mg), Lisinopril 5 mg; white oblong scored electrolyte balance may precipitate hepatic thiazide 12.5 mg. mg once daily depending on renal
tab. marked “PEMA-5”. coma); surgery/anaesthesia (hypotension may function. Increase dose only if the
POM ZESTORETIC® (Reals)
EMDEX
5 mg – 2 x 14's (in blisters). occur); thiazides may impair glucose tolerance previous lower dose is well tolerated.
Tablet, Lisinopril 20 mg, hydrochlorothiazide 12.5 mg
Caplet, (10 mg), Lisinopril 10 mg; white oblong, (dosage of insulin and other antidiabetic Pack: 20 x 28. Congestive heart failure, Initially 2 mg
scored tab. marked “PEMA-10”. agents may be adjusted); thiazides may pre-
in the morning; may be increased to 4
cipitate hyperuricaemia and/or gout. PERINDOPRIL mg once blood pressure acceptability
POM PRILAS® (Seagreen) Interactions: Potassium supplements, potas- Therapeutic category: Long-acting ACE inhib- has been demonstrated. Elderly: start
Tablets, Lisinopril 5 mg, 10 mg; uncoated tabs sium-sparing agents, or potassium-containing treatment at 2 mg daily.
5 mg – 2 x 14’s itor, Antihypertensive.
salt substitutes (may cause increased serum Indications: Essential hypertension; Stable cor-
10 mg – 2 x 14’s POM COVERSYL® (Servier Int’l)
potassium). Lithium (co-administration reduces onary artery disease; Congestive heart failure. Tablet, Perindopril (as terbutylamine salt) 4 mg;
POM RANOPRIL® (Ranbaxy) the renal clearance of lithium). Indomethacin, Contra-indications: Children (under 15 scored tab.
Tablets, Lisinopril (as dihydrate) Ph. Eur. 5 mg, 10 other NSAIDs, tubocurarine. 4 mg – 10’s; 30’s.
years of age); Pregnancy; Lactation; History
mg, 20 mg. Adverse effects: Dizziness, headache,
5 mg – 10 x 10’s (in blister) of hypersensitivity to perindopril, including
non-productive and persistent cough, fatigue, angioneurotic oedema type reactions. Avoid RAMIPRIL
10 mg – 10 x 10’s (in blister)
hypotension including orthostatic hypoten- combination with potassium-sparing diuretics, Indications: Ramipril is a long-acting angi-
sion, diarrhoea, nausea, vomiting, dry mouth, potassium salts, lithium and estramustine. otensin-converting enzyme inhibitor (ACEI)
POM SINOPRIL® (Chanmedi) rash, gout, palpitations, chest discomfort,
Tablets, Lisinopril 5 mg, 10 mg, 20 mg.
Precautions: Assess renal function before and indicated in mild to moderate hypertension;
muscle cramps and weakness, paraesthesia, during treatment where appropriate. Renovas- cardiac failure following myocardial infarction.
5 mg – 3 x10’s. asthenia and impotence; rarely, hypersensi-
10 mg – 3 x 10’s. cular hypertension; Surgery/Anesthesia. Renal Contra-indications, Precautions, etc: see
tivity/ angioedema. failure (adjust dose in accordance with the under Enalapril.
20 mg – 3 x 10’s.
Advice to patients: See under Enalapril. creatinine clearance). Symptomatic hypoten- Dose: Hypertension, Usually 2.5-10 mg once
POM TAMAPRIL® (Tamar & Pharez) Nursing action: See under Enalapril.
Tablets, Lisinopril dihydrate 5 mg, 10 mg
sion especially in volume-depleted patients, daily. Initially (for patients not on
Dose: Hypertension, usually one tablet once those receiving diuretics, or with the first two diuretics) 2.5 mg once daily; may be
5 mg – 3 x 10's daily; may be increased to two tablets
10 mg – 3 x 10's doses. In diuretic-treated patients, stop the increased to 5 mg and up to a max.
once daily if the desired therapeutic diuretic 3 days before starting perindodopril. 10 mg once daily at intervals of 1-2
POM TOSURIL® (Solidum) effect is not achieved after 2 to 4 A diuretic may later be given in combination if weeks based on patient response. If
Tablets, Lisinopril dihydrate 5 mg, 10 mg; uncoated weeks.
tabs. necessary; potassium-sparing diuretics are not used in addition to diuretic: discon-
Note: To be taken at approximately the same time
5 mg – 30’s recommended. Combination with neuroleptics tinue the diuretic for 2-3 days before
each day. Not recommended for children.
10 mg – 30’s. or imipramine-type drugs may increase the hy- starting the Ramipril to minimize the
POM ALSTORETIC® (Reals) potensive effect. Serum lithium concentrations incidence of hypotension. If diuretic
POM ZESTRIL® (Reals) Tablet, Lisinopril 5 mg, hydrochlorothiazide 12.5 may rise during lithium therapy. cannot be discontinued, use initial
Tablets, Lisinopril 5 mg, 10 mg, 20 mg. mg; uncoated tab.
5 mg – 28 Advice to patients: To stop taking the medi- dose of 1.25 mg once daily.
10 mg – 28 cation and see the doctor immediately if they Prophylaxis after myocardial infarc-
20 mg – 28. POM KUINOPRIL® (Drugfield) experience signs/symptoms of angioedema: tion (started in hospital 3 to 10 days
Tablet, Lisinopril 10 mg, hydrochlorothiazide 12.5 mg swelling of the face, lips, tongue and/or lar- after infarction), initially 2.5 mg twice
POM ZISTY® (Reals) Pack: 3 x 10’s (in blisters)
Tablets, Lisinopril 5 mg, 10 mg; uncoated tabs.
ynx, which results in difficulty in breathing or daily, increased after 2 days to 5 mg
Tablet, Lisinopril 20 mg, hydrochlorothiazide 12.5 mg
5 mg – 2 x 14’s (in blisters). swallowing. twice daily; maintenance 2.5–5 mg
10 mg – 2 x 14’s (in blisters). Adverse effects: Dry cough, fatigue, asthe- twice daily
POM LISPRIL® Plus (Zoomota)
206 | 5.3.6 Angiotensin receptor blockers (ARBs) 5.3.6 Angiotensin receptor blockers (ARBs) | 207
Note: If initial 2.5-mg dose not tolerated, give 1.25 RAMIPRIL plus HYDROCHLOROTHIAZIDE is used together with Hydrochlorothiazide, treatment.
mg twice daily for 2 days before increasing to 2.5 Indications: Essential hypertension for pa- the reduction in blood pressure is additive. Administration: May be administered with or with-
mg twice daily, then 5 mg twice daily; withdraw if An increased antihypertensive effect is also out food. Dosage must be individualized.
tients in whom combination therapy is
2.5 mg twice daily not tolerated. seen when Candesartan cilexetil is combined (Additional information sourced from: 1. Candesartan cilexetil
appropriate.
Administer with half a glass of liquid during with Amlodipine or Felodipine. Agents that monograph http://www.medicines.org.uk/emc/medicine/26586/
Contra-indication: Avoid use during preg-
or after meals. block the renin-angiotensin-aldosterone sys-
SPC/Candesartan+Cilexetil; 2. RxFiles ACEI-ARB Comparison
nancy and lactation. http://www.rxfiles.ca/rxfiles/uploads/documents/members/
POM CARDIOPRIL® (Phillips/Dr. Reddy’s) Dose: Essential hypertension, Adult, usually tem (RAAS) including Candesartan, have less CHT-HTN-ace-arb.pdf)
Capsules, Ramipril BP 5 mg, 10 mg. one tablet once daily; to be taken at pronounced antihypertensive effect in black
5 mg – 10’s. patients (usually a low-renin population) than POM ADVANT® (Getz)
approx. the same time each day. May
10 mg – 10’s. in non-black patients. Tablets, Candesartan cilexetil 8 mg, 16 mg.
be increased to 2 tablets once daily
Indication: Treatment of hypertension, alone 8 mg – 14’s (in blisters)
POM LIFACE® (Lifeback) after 2 to 4 weeks if adequate thera- 16 mg – 14’s; 28’s (in blisters)
Tablets, Ramipril 2.5 mg, 5 mg; uncoated tabs. peutic response is not achieved. or in combination with other antihypertensive
2.5 mg – 3 x10’s agents.
5 mg – 3 x10’s POM PREFACE-H® (Al-Tinez) CANDESARTAN plus
Contra-indications: Hypersensitivity, preg- HYDROCHLOROTHIAZIDE
Tablet, Ramipril 2.5 mg, hydrochlorothiazide 12.5
POM PREFACE® (Al-Tinez) mg; uncoated tab nancy, lactation, severe hepatic impairment,
and children aged below 1 year. Avoid co-ad- See under the preparations below.
Tablets, Ramipril 2.5 mg, 5 mg; uncoated tabs Pack: 10’s (in blisters)
2.5 mg – 10’s (in blisters) ministration with Aliskiren in patients with
POM THIAPRIL® (May & Baker) POM ADVANTEC® (Getz)
5 mg – 10’s (in blisters) diabetes mellitus or renal impairment.
Tablet, Ramipril 5mg, hydrochlorothiazide 12.5 mg. Tablet, Candesartan cilexetil 16 mg, Hydrochloro-
POM RAMITACE® (May & Baker) Precautions: Renal impairment; Co-admin- thiazide 12.5 mg
Pack: 30’s.
Tablets, Ramipril 2.5 mg, 5 mg, 10 mg. istration with ACE inhibitors in heart failure Pack: 28’s (in blisters)
2.5 mg – 30’s. POM TOPRIL-H® (Zolon) (monitor renal function and serum potassium); Indications: Treatment of hypertension. The
EMDEX
5 mg – 30’s. Tablet, Ramipril 2.5 mg, hydrochlorothiazide 12.5 mg Patients on haemodialyis because of reduced fixed dose combination is not indicated for
10 mg – 30’s. Pack: 10’s; 30’s.
plasma volume and activation of RAAS (moni- initial therapy.
POM TOPRIL® (Zolon) POM TRITAZIDE® (Sanofi-Aventis) tor BP); Aortic and mitral valve stenosis; Correct Dose: By mouth, Adult, one tablet per day with or
Tablets, Ramipril 2.5 mg, Ramipril 5 mg. Tablet, Ramipril 5 mg, hydrochlorothiazide 25 mg. hypovolaemia before initiating therapy e.g. without food. To minimize dose dependent
Pack: 10’s; 30’s. Pack: 28’s (in blisters) in patients on diuretics or salt restricted diet; side effects, it is usually appropriate to begin
patients with primary hyperaldosteronism. combination therapy after a patient has
POM TRITACE® (Sanofi-Aventis)
Tablets, Ramipril 1.25 mg, 2.5 mg, 5 mg, 10 mg
5.3.6 Angiotensin receptor Interactions: Not significantly metabolized failed to achieve the desired effect with
blockers (ARBs) monotherapy.
1.25 mg – 30’s by cytochrome P450 and has no effect on the
2.5 mg – 30’s hepatic enzymes. Co-administration with po- POM NECSARTAN® (Nectar Healthcare)
5 mg – 30’s CANDESARTAN tassium-sparing diuretics, potassium supple- Tablet, Candesartan cilexetil 16 mg, Hydrochlorothi-
10 mg – 28’s Therapeutic class: Antihypertensive, Angio- ments, salt substitutes containing potassium, azide 12.5 mg; uncoated tab.
Capsule, Ramipril 10 mg tensin II antagonist. Dose: Adult, by mouth, one tablet once daily, with
or other medicinal products that may increase
10 mg – 28’s or without food.
Pharmacology: Candesartan cilexetil is a prod- potassium levels (e.g. heparin) may lead to Note: Antihypertensive effect is usually attained
rug which is rapidly and completely converted increases in serum potassium in hypertensive within 4-5 weeks of initiation of treatment. Combi-
RAMIPRIL plus FELODIPINE to the active substance, Candesartan by ester patients. Co-administration with NSAIDs may nation therapy should normally be used only after
Indications: Essential hypertension, in patients hydrolysis during absorption from the gastro- reduce antihypertensive effect, and may also a patient has failed to achieve the desired effect
adequately controlled on ramipril or felodipine intestinal tract. worsen renal function especially in the elderly. with monotherapy.
alone. Candesartan blocks the vasoconstrictor and May cause reversible increases in serum lithium
Contra-indications, Precautions, etc: see aldosterone effects of angiotensin II by se- concentrations and toxicity. LOSARTAN
under Enalapril and Felodipine. lectively blocking the binding of angiotensin Adverse effects: Dizziness/vertigo, headache, Therapeutic category: Antihypertensive,
Dose: See under preparations below. II to the AT1 receptor in many tissues, such hyperkalaemia, hyponatraemia, tachycardia, Angiotensin II receptor antagonist.
POM TRIAPIN® (Sanofi-Aventis) as vascular smooth muscle and the adrenal palpitation, respiratory infection; renal im- Pharmacology: Angiotensin II is the primary
Tablet, Ramipril 5 mg, Felodipine 5 mg; pro- gland. It does not inhibit ACE, which converts pairment, including renal failure in susceptible vasoactive hormone of the renin-angiotensin
longed-release tab. angiotensin I to angiotensin II and degrades patients. Rarely dyspepsia, nausea, cough, system. It is formed from angiotensin 1 in a
Pack: 28’s bradykinin. The incidence of cough associated myalgia, angioedema, rash, urticaria, pruritus; reaction catalyzed by angiotensin converting
Dose: Adult (including elderly), max. one tab. once with its use is lower compared to ACE inhibi- abnormal liver enzymes, metabolic disorders; enzyme (ACE, kininase II). It is a potent vaso-
daily. To be swallowed whole. Do not divide, tors. The antagonism of the angiotensin II (AT1) leukopenia, neutropenia and agranulocytosis. constrictor and is an important component
crush or chew. receptors results in dose related increase in Dose: By mouth, Adult, usually 8-16 mg in the pathophysiology of hypertension. It
POM TRIAPIN MITE® (Sanofi-Aventis) plasma renin levels, angiotensin I and II levels once daily; up to a max. 32 mg once also stimulates aldosterone secretion by the
Tablet, Ramipril 2.5 mg, Felodipine 2.5 mg; pro- and also a decrease in plasma aldosterone daily. Start with 4 mg once daily in adrenal cortex. Losartan and its principal active
longed-release tab. concentration. After the first dose of Cande- patients with mild to moderate renal metabolite block the vasocontrictor and aldos-
Pack: 28’s sartan cilexetil, onset of antihypertensive effect or hepatic impairment. Adjust dose terone-secreting effects of angiotensin II by
Dose: Adult (including elderly), one tab. once daily;
occurs within 2 hours. With continuous treat- based on blood pressure response. selectively blocking the binding of angiotensin
may increase to max. 2 tabs once daily. To
be swallowed whole. Do not divide, crush
ment, maximum reduction in blood pressure Most of the antihypertensive effect is II to the AT1 receptor found in many tissues (e.g.
or chew. is attained within four weeks. The estimated present within 2 weeks and maximal vascular smooth muscle, adrenal gland). Both
absolute bioavailability is 15% and is not blood pressure reduction is gener- losartan and its principal active metabolite do
affected by meals. When Candesartan cilexetil ally obtained within 4 to 6 weeks of
not exhibit any partial agonist activity at the Tablet, Losartan potassium 25 mg, 50 mg; f-c tab Tablet, Losartan potassium 50 mg, hydrochlorothi- effects, Advice to patients: See under Losartan.
AT1 receptor and have much greater affinity 25 mg – 3 x 10’s azide 12.5 mg; white round tab. Dose: Adult, by mouth, initially 20 mg once
(about 1000-fold) for the AT1 receptor than for 50 mg – 3 x 10’s Pack: 10’s. daily; may increase up to a max. 40
the AT2 receptor. POM Losartan (Korlyns) POM LOSATRUST-H® (Al-Tinez) mg/day if needed.
Indications: Mild to moderate hypertension Tablet, (25 mg), Losartan potassium 25 mg; white f-c Tablets, Losartan (as K+) 50 mg, hydrochlorothiazide Note on dosage adjustment: The antihypertensive
alone or in combination with other anti-hyper- tab. marked "2L" on one side. 12.5 mg; f-c tab. effect may take up to 2 weeks after initiating therapy
tensive agents. To reduce the risk of stroke in 25 mg – 7’s; 28’s Pack: 10 x 10’s and maximum BP lowering effect may take up to 8
Tablet, (50 mg), Losartan potassium 50 mg; white f-c weeks. This should be considered during dosage
patients with hypertension and left ventricular POM LOTAN H® (Korlyns)
tab. marked "3L" on one side. titration.
hypertrophy. For the treatment of diabetic Tablet, Losartan potassium 50 mg, hydrochlorothi-
50 mg – 28’s POM OLMEZAAR® (Micronova)
nephropathy in type 2 diabetes. Tablet, (100 mg), Losartan potassium 100 mg; white
azide 12.5 mg; yellow f-c tab.
Contra-indications: Hypersensitivity to any Tablets, Olmesartan medoxomil 20 mg, 40 mg;
f-c tab. marked "4L" on one side. POM Losartan (Vatican-Bells) f-c tabs.
component of the preparation; pregnancy 100 mg – 28’s Tablet, Losartan potassium 50 mg; f-c tab 20 mg – 30’s
(discontinue immediately if pregnancy is
POM LOSATRUST® (Al-Tinez) POM RETIZIDE® (Solidum) 40 mg – 30’s
detected).
Tablets, Losartan (as K+) 25 mg, 50 mg; f-c tabs. Tablet, (25/12.5 mg), Losartan potassium 25 mg, POM OLVANCE®(Ranbaxy)
Precautions: History of hepatic or renal im- 25 mg – 10 x 10’s hydrochlorothiazide 12.5 mg Tablets, Olmesartan medoxomil 20 mg, 40 mg; f-c tab
pairment (may use lower dose). Symptomatic 50 mg – 10 x 10’s Pack: 30’s
hypotension may occur in volume depleted 20 mg – 2 x 7’s (in blisters)
Tablet, (50/25 mg), Losartan potassium 50 mg, 40 mg – 2 x 7’s (in blisters)
patients or those on high-dose diuretics (may POM LOSIUM® (Interpharma)
hydrochlorothiazide 25 mg
Tablet, Losartan (as K+) 50 mg. POM OLVANCE HCT® (Ranbaxy)
use lower starting dose of losartan). Lactation. Pack: 30’s.
50 mg – 10’s Tablet, (20 mg), Olmesartan medoxomil 20 mg,
Adverse effects: Dizziness (dose-related POM SARCOL-H® (Nomedi)
orthostatic effects); Headache, back pain, myal- POM LOZATAN® (Pharma Ethics) hydrochlorothiazide 12.5 mg; f-c tab
Tablet, Losartan potassium 50 mg, hydrochlorothi-
EMDEX
Tablets, Losartan potassium 25 mg, 50 mg. Pack: 7’s; 2 x 7’s
gia, asthenia/fatigue, GI disturbances, transient azide 12.5 mg.
25 mg – 3 x 10’s Tablet, (40 g), Olmesartan medoxomil 40 mg, hydro-
elevation of liver enzymes, impaired renal Pack: 1 x 10’s (in blisters) chlorothiazide 12.5 mg; f-c tab
50 mg – 3 x 10’s
function, taste disturbances and hyperkala- Pack: 7’s; 2 x 7’s
POM XAVOR-DIU® (Biostadt)
emia. Rarely rash, angioedema, neutropenia; POM PRESARTAN® (IPCA)
Tablet, Losartan potassium 50 mg, hydrochlorothi- POM ORION® (Biostadt)
does not cause bradykinin accumulation so Tablets, Losartan (as K+) 25 mg, 50 mg; f-c tabs.
azide 12.5 mg. Tablet, Olmesartan medoxomil 10 mg, 20 mg, 40 mg.
incidence of cough observed is significantly 25 mg – 14’s.
Pack: 1 x 10’s (in blisters). Pack: 1 x 10’s (in blister pack)
50 mg – 14’s.
less than that of ACE inhibitors.
Dose: Initially, 50 mg once daily for most pa- POM RETISAR® (Solidum) OLMESARTAN TELMISARTAN
tients with or without food. Maximal Tablets, Losartan potassium 25 mg, 50 mg; f-c tabs.
Pharmacology: Olmesartan is an angiotensin Therapeutic category: Antihypertensive,
antihypertensive effect is attained 25 mg – 30’s
50 mg – 30’s. II receptor blocker (ARB). It blocks the vasocon- Angiotensin II antagonist.
3-6 weeks after initiation of therapy. strictor effects of angiotensin II by selectively Pharmacology: Telmisartan is a specific an-
May increase dose to 100 mg once POM ROSART® (Ranbaxy) blocking the binding of angiotensin II to the AT1
Tablets, Losartan potassium 25 mg, 50 mg; f-c tabs. giotensin II receptor (type AT1) antagonist. It
daily depending on tolerance and receptor in vascular smooth muscle. Its action
25 mg – 5 x 10’s (in blisters). displaces angiotensin II from its binding site
response. is, therefore, independent of the pathways
50 mg – 5 x 10’s (in blisters). at the AT1 receptor, thus inhibiting the vaso-
Elderly (>75 years): Initially 25 mg for angiotensin 11 synthesis. Angiotensin II constrictive effects of angiotensin II. Plasma
once daily. Same lower starting POM SIVOZOSAN® (Adpharm) is formed from angiotensin I in a reaction aldosterone levels are also decreased by tel-
dose in moderate to severe renal Tablet, Losartan potassium 50 mg catalyzed by angiotensin converting enzyme
50 mg – 5 x 10’s. misartan. After the first dose of telmisartan, the
impairment (i.e., creatinine clearance (ACE, kininase II). Angiotensin II is the principal antihypertensive activity gradually becomes
<20 mL/min) and volume depleted POM XAVOR® (Biostadt) pressor agent of the renin-angiotensin system evident within 3 hours; the maximum reduc-
patients (including patients on Tablet, Losartan potassium 50 mg; f-c tab. (RAS), with effects that include vasoconstriction in blood pressure is generally attained 4 to
diuretics). 50 mg – 10’s (in blisters). tion, stimulation of synthesis and release of 8 weeks after the start of treatment.
POM ANGIZAAR® (Micronova) aldosterone, cardiac stimulation and renal It is rapidly absorbed with a mean absolute
Tablets, Losartan potassium 25 mg, 50 mg; f-c tabs. LOSARTAN plus HYDROCHLOROTHIAZIDE reabsorption of sodium. An AT2 receptor is bioavailability of about 50%. >99.5% bound to
25 mg – 30’s. found also in many tissues, but this receptor is
POM ANGIZAAR-H® (Micronova) plasma protein. Metabolism is by glucuronida-
50 mg – 30’s. not known to be associated with cardiovascular
Tablet, Losartan potassium 50 mg, hydrochlorothi- tion to form inactive metabolites. Excreted in
POM COZVENYL® (Salem Gates) azide 12.5 mg; f-c tab. homeostasis. Olmesartan has more than a the faeces mainly as unchanged drug; urinary
Tablet, Losartan potassium 50 mg Pack: 30’s. 12,500 fold greater affinity for the AT1 receptor excretion is <1% of dose. Terminal elimination
50 mg – 3 x 10’s
POM COZVENYL® Plus (Salem Gates) than for the AT2 receptor. half-life is >20 hours.
POM LOSAKAL® (Zoomota) Tablet, Losartan potassium 50 mg, hydrochlorothi- Bioavailability is approx. 26%. It undergoes Indications: Treatment of essential hyper-
Tablets, Losartan (as K+) 25 mg, 50 mg; pink tabs. azide 12.5 mg; f-c tab. minimal hepatic metabolism and is excreted tension.
25 mg – 4 x 7’s Pack: 3 x 10’s in urine (35-50%) and bile/feces (50-65%); has Contra-indications: Hypersensitivity; severe
50 mg – 4 x 7’s. a half-life of about 13 hours. hepatic impairment; biliary obstructive disor-
POM LOSAKIND-H® (Phillips)
Tablet, Losartan potassium 50 mg, hydrochlorothi- Indications: Treatment of hypertension, alone ders; pregnancy, lactation.
POM LOSARGEN® (JB Pharma)
Tablet, Losartan (as K+) 50 mg; f-c tab. azide 12.5 mg; f-c tab or in combination with other antihypertensive Precautions: Correct volume and/or sodium
50 mg – 10 x 10’s. Pack: 3 x 10’s agents. depletion before initiating treatment e.g. in
Contra-indications, Precautions, Adverse patients on diuretic therapy or salt restricted
POM LOSAKIND® (Phillips) POM LOVAZIDE® (Vatican Bells)
diet. Closely monitor serum K esp. in patients
+ POM CO-MICARDIS® (Gemini) elderly; CHF. Monitor the electrolytes; Post-MI. 6 hours.
at risk of hyperkalaemia e.g. elderly, DM, ACEIs, Tablet, (40/12.5 mg) Telmisartan 40 mg, hydrochlo- Female patients of child bearing age (consider Indications: Treatment of hypertension, heart
etc. Renal or hepatic impairment. Combination rothiazide 12.5 mg; double-layered tab. alternatives); breastfeeding. failure (NYHA class II-IV). Reduction of cardio-
with ACEIs, i.e. dual blockade of RAAS. Aortic Pack: 28’s Adverse effects: Peripheral oedema, dizziness, vascular mortality in clinically stable patients
Tablet, (80/12.5 mg), Telmisartan 80mg, hydrochlo-
or mitral stenosis, or obstructive hypertrophic headache, orthostatic hypotension, syncope, with left ventricular failure or left ventricular
rothiazide 12.5 mg; double-layered tab.
cardiomyopathy. Pack: 28’s fatigue and back pain; exacerbation of angina; dysfunction after a recent (12 hours – 10 days)
Interactions: Avoid co-administration with Notes: Co-Micardis 40 mg/12.5 mg may be admin- MI; hyperkalemia. myocardial infarction.
potassium-sparing diuretics or potassium istered in patients whose blood pressure is not Dose: By mouth, initially 40/5 mg once Contra-indications: Hypersensitivity to val-
supplements. Lithium, NSAIDs, thiazide or adequately controlled by Micardis 40 mg daily; may be increased up to a max. sartan, pregnancy.
loop diuretics. Co-Micardis 80 mg/12.5 mg may be administered 80/10 mg once daily after 4 weeks of Precautions: Symptomatic hypotension in vol-
Adverse effects: Abdominal pain, diarrhoea, in patients whose blood pressure is not adequately therapy. ume depleted patients e.g. those on diuretics
dyspepsia, flatulence, vomiting; Upper res- controlled by Micardis 80 mg Add-on therapy: For patients not adequately con- and elderly (may withhold diuretic during initi-
The maximum antihypertensive effect is generally trolled on Telmisartan or Amlodipine monotherapy,
piratory tract infection including pharyngitis ation). Acute renal failure may occur in patients
attained with Co-Micardis 4-8 weeks after the start start 40/5 mg once daily.
and sinusitis; Anaemia, hyperkalaemia, de- of treatment.
with renal artery stenosis. Hepatic dysfunction.
pression, insomnia, orthostatic hypotension, Replacement therapy: May switch patients tak- Women of child bearing age (discontinue as
increase in hepatic enzymes. Rarely erythema, POM PINASARTAN® (Pinnacle) ing Telmisartan/Amlodipine as separate tablets soon as pregnancy is detected); children and
angioedema, drug eruption, toxic skin erup- Tablets, Telmisartan 40 mg, hydrochlorothiazide to the component doses of the combo pill. adolescents <18 years.
12.5 mg; f-c tab.
tion, eczema. POM ARBITEL-AM® (Micronova) Adverse effects: Headache, dizziness, fatigue;
Pack: 3 x 10’s
Dose: Adult, usually 40 mg once daily; may Dose: Adult, Administer once daily with liquid, with
Tablet, Telmisartan 40 mg, Amlodipine besilate 5 upper respiratory tract infection, cough;
increase up to a max. 80 mg once mg; f-c tab. diarrhoea, abdominal pain, nausea; rhinitis,
or without food in patients whose BP is not
daily. adequately controlled by Telmisartan alone. sinusitis, pharyngitis; back pain, arthralgia;.
EMDEX
Renal impairment: Initially 20 mg/day. Individual dose titration with each of the VALSARTAN Others include angioedema, oedema, asthenia,
Mild to moderate hepatic impair- two components is recommended before Therapeutic category: Antihypertensive; insomnia, rash, decreased libido, vertigo.
ment: Max. 40 mg once daily; avoid in changing to the fixed dose combination. Angiotensin II receptor blocker (ARB) Dose: Adult, by mouth, Hypertension, initially
severe hepatic disease. POM SARTEL-H® (Phillips) Pharmacology: Valsartan is an orally active, 80-160 mg once daily (in patients
(Additional information sourced from Micardis monograph: Tablets, (40/12.5 mg), Telmisartan 40 mg, hydrochlo- potent, and specific angiotensin II (Ang II) re- who are not volume depleted); lower
http://www.medicines.org.uk/) rothiazide 12.5 mg; uncoated bilayer tab. ceptor antagonist. It blocks the vasoconstrictor dose if on diuretic.
Pack: 10’s (in blisters). and aldosterone-secreting effects of angio- Majority of effects within 2 weeks,
POM ARBITEL® (Micronova) Tablets, (80/25 mg), Telmisartan 80 mg, hydrochlo- tensin II at various receptor sites; selectively maximal effects in 4-6 weeks. May
Tablets, Telmisartan 20 mg, 40 mg, 80 mg; uncoated rothiazide 25 mg. blocks the binding of angiotensin II to the AT1 increase dose to 160-320 mg/day or
tab. Pack: 10’s (in blisters). receptors in vascular smooth muscle and the a diuretic may be added. Max. 320
40 mg – 30’s.
80 mg – 30’s.
adrenal glands. The increased plasma levels mg/day.
TELMISARTAN plus AMLODIPINE
of Ang II following AT1 receptor blockade with Heart failure, initially 40 mg twice
POM CILZEC® (Mega Lifesciences) Therapeutic category: Antihypertensive valsartan may stimulate the unblocked AT2 daily; may increase up to a max. 320
Tablet, Telmisartan 20 mg, 40 mg, 80 mg; white or Pharmacology: Telmisartan plus Amlodipine receptor, which appears to counterbalance the mg/day in divided doses.
off-white uncoated tabs. is a synergistic antihypertensive combo: an- effect of the AT1 receptor. Post-MI therapy in left ventricular dys-
Pack: 3 x 10’s. giotensin II receptor antagonist plus calcium Valsartan does not inhibit ACE (also known as function, initially 20 mg twice daily, 12
POM HYPOTEL (Shrezar) channel blocker. Telmisartan blocks the effect kininase II), which converts Ang I to Ang II and hours after MI; increase within 7 days
Tablets, Telmisartan 20 mg, 40 mg; uncoated tabs of angiotensin II in the vascular smooth muscle degrades bradykinin. Since there is no effect to 40 mg twice daily and then titrate
10 mg – 3 x 10 x 10’s and the adrenal gland, lowering the BP. It is on ACE and no potentiation of bradykinin or up to a max. 160 mg twice daily as
20 mg – 3 x 10 x 10’s 42-58% absorbed following oral admin; me- substance P, angiotensin II antagonists are tolerated.
POM MICARDIS® tabolized by the liver; excreted unchanged in unlikely to be associated with coughing.
feces and has a T½ of about 24 hrs. Amlodipine POM DIOVAN® (Novartis)
Tablets, Telmisartan 20 mg, 40 mg, 80 mg. In most patients, after administration of a Tablet, (40 mg), Valsartan 40 mg; yellow scored tab.
works by inhibiting the transmembrane influx single dose, onset of antihypertensive activity
POM SARTEL® (Phillips) marked ‘DO’ on one side and ‘NVR’ on reverse.
Tablet, Telmisartan 40 mg, 80 mg; uncoated tab. of Ca2+ into coronary vascular smooth muscle occurs within 2 hours and the peak reduction 40 mg – 28’s
40 mg – 10’s (in blisters). and cardiac muscle. It is 64-90% bioavailable; of blood pressure is achieved within 4-6 hours. Tablet, (80 mg), Valsartan 80 mg; pale red scored
80 mg – 10’s (in blisters). metabolized mainly in the liver by CYP3A4; ex- The antihypertensive effect persists over 24 tab. marked ‘D/V’ on one side and ‘NVR’ on reverse.
creted in the urine and has a T½ of 30-50 hours. hours after dosing. During repeated dosing, 80 mg – 28’s
TELMISARTAN plus Indications: Hypertension, alone or with other the maximum reduction in blood pressure Tablet, (160 mg), Valsartan 160 mg; grey-orange
HYDROCHLOROTHIAZIDE antihypertensive agents. May also be used as scored tab. marked ‘DX/DX’ on one side and ‘NVR’
with any dose is generally attained within
initial therapy in patients who need multiple on reverse
POM ARBITEL-H® (Micronova) 2-4 weeks and is sustained during long-term 160 mg – 28’s
Tablet, Telmisartan 40 mg, hydrochlorothiazide 12.5 drugs to achieve their BP goals. therapy. Valsartan has no notable effects on Tablet, (320 mg), Valsartan 320 mg; dark-grey violet
mg; uncoated bilayered tab. Contra-indications: Hypersensitivity to any of total cholesterol, fasting triglycerides, fasting scored tab. marked ‘DXL’ on one side and ‘NVR’ on
Pack: 30’s the ingredients. Avoid in 2nd & 3rd trimester serum glucose or uric acid. reverse.
POM CILZEC® Plus (Mega Lifesciences) of pregnancy as it can cause injury to the Undergoes minimal hepatic metabolism 320 mg – 28’s
Tablet, Telmisartan 40 mg, hydrochlorothiazide developing fetus. (about 20%); eliminated mainly by biliary POM CARVALS® (Ranbaxy)
12.5 mg. Precautions: Renal and hepatic impairment; excretion in faeces (83%) and renally in urine Caplets, Valsartan 80 mg, 160 mg; brown, scored f-c
Pack: 3 x 10`s. salt & volume depleted patients including the (13%), mainly as unchanged drug. Half-life is
212 | 5.3.7 Calcium–channel blockers 5.3.7 Calcium–channel blockers | 213
caplets marked “V1” and “V2” respectively. Pack: 30’s weight (inform doctor of any increase), BP, res- POM Amlodipine (Nelpharm)
80 mg – 3 x 10’s piration. Tablets, Amlodipine besilate 5 mg, 10 mg
160 mg – 3 x 10’s 5.3.7 Calcium–channel blockers Dose: Angina, by mouth, ADULT initially 5 5 mg – 10 x 10’s
mg once daily; maximum 10 mg once 10 mg – 10 x 10’s.
POM JOLTAN® (Joswe/Afrab) These agents (Amlodipine, Isradipine,
Tablets, Valsartan 80 mg, 160 mg; f-c tabs daily. POM AMLODIX® (Eutrix)
Nifedipine, Lacidipine) interfere with the
80 mg – 30’s Hypertension, by mouth, ADULT Tablets, Amlodipine (as besylate) 5 mg, 10 mg; white
action of intracellular calcium on both smooth
160 mg – 30’s initially 5 mg once daily; maximum 10 scored uncoated tabs.
and cardiac muscles. They are also used in the 5 mg – 3 x 10’s
mg once daily.
treatment of Angina. The common adverse 10 mg – 3 x 10’s
VALSARTAN plus
HYDROCHLOROTHIAZIDE effects which result from reflex responses to POM Amlodipine (WMF 12.3)
peripheral vasodilation, can be countered by Tablet, Amlodipine 5 mg. POM AMLODREX® (Juhel)
See under the individual preparations below Note: Tablets from various suppliers may contain Tablet, Amlodipine 5 mg, hydrochlorothiazide
beta-blockers (flushing, headache) or diuretics
different salts (e.g. amlodipine besilate, amlodipine 12.5 mg.
POM Co-DIOVAN® (Novartis)
(fluid retention).
maleate, and amlodipine mesilate) but the strength POM AMLONG® (Elbe)
Tablet, (80/12.5 mg), Valsartan 80 mg, hydrochloro- Nifedipine has more influence on vessels and is expressed in terms of amlodipine (base); tablets Tablet, (5 mg), Amlodipine 5 mg; white scored tab.
thiazide 12.5 mg; light orange, f-c tab. marked ‘HGH’ less on the myocardium, and has no antiar- containing different salts are considered inter- marked ‘AM/5’
on one side and ‘CG’ on reverse. rhythmic properties when compared with changeable. 5 mg – 30’s; 100’s
Pack: 28’s Verapamil. POM Amlodipine (EDL 10.3) Tablet, (10 mg), Amlodipine 10 mg; white scored
Tablet, (160/12.5 mg), Valsartan 160 mg, hydrochlo-
Tablets, Amlodipine (as besylate) 5 mg, 10 mg. tab. marked ‘AM/10’
rothiazide 12.5 mg; dark red f-c tab. marked ‘HHH’
AMLODIPINE 10 mg – 30’s; 100’s
on one side and ‘CG’ on reverse. POM Amlodipine (Visko)
Pack: 28’s Therapeutic category: Antihypertensive/ Tablets, Amlodipine 5 mg, 10 mg POM AMLOPRES® (Standard Generics)
Tablet, (160/25 mg), Valsartan 160 mg, hydrochloro- anti-angina 5 mg – 1 x 10’s. Tablets, Amlodipine besylate 5 mg, 10 mg
EMDEX
thiazide 25 mg; brown-orange, f-c tab. marked ‘HXH’ Indications: Hypertension, angina (see also 10 mg – 1 x 10’s. 5 mg – 2 x 14’s
on one side and ‘NVR’ on reverse. section 5.5). 10 mg – 2 x 14’s
Pack: 28’s POM ACEDIPIN® (Chanmedi)
Contra-indications: Cardiogenic shock, unsta- Tablets, Amlodipine 5 mg, 10 mg. POM AMLOTAB® (Onifam)
Tablet, (320/12.5 mg), Valsartan 320 mg, hydrochlo- ble angina, significant aortic stenosis.
rothiazide 12.5 mg; pink f-c tab. marked ‘HIL’ on one 5 mg – 10 x 10’s. Tablets, Amlodipine besilate 5 mg, 10 mg.
Precautions: Hepatic impairment (Appendix 10 mg – 10 x 10’s. 5 mg – 2 x 14’s
side and ‘NVR’ on reverse.
Pack: 28’s 5); pregnancy (Appendix 2), breastfeeding 10 mg – 2 x 14’s
POM AMBES® (Nosak)
Tablet, (320/25 mg), Valsartan 320 mg, hydrochloro- (Appendix 3); interactions: Appendix 1. POM AMLOTEN® (Rohi)
Tablets, Amlodipine (as besilate) 5 mg, 10 mg;
thiazide 25 mg; yellow f-c tab. marked ‘CTI’ on one Adverse effects: Abdominal pain, nausea; pal- uncoated tabs. Tablets, Amlodipine 5 mg, 10 mg
side and ‘NVR’ on reverse. pitation, flushing, oedema; headache, dizziness, 5 mg – 1 x 10’s (in blister) 5 mg – 100’s
Pack: 28’s sleep disturbances, fatigue; less commonly GI 10 mg – 1 x 10’s (in blister). 10 mg – 100’s
Indications: Treatment of hypertension in patients disturbances, dry mouth, taste disturbances,
whose blood pressure is not adequately controlled POM AMDEPIN® (Interpharma) POM AMLOTRUST® (Al-Tinez)
hypotension, syncope, chest pain, dyspnoea, Tablets, Amlodipine (as besilate) 2.5 mg, 5 mg, 10
by monotherapy. Tablets, Amlodipine (as besylate) 5 mg, 10 mg
rhinitis, mood changes, tremor, paraesthesia, 5 mg – 10’s mg; uncoated tab.
Dose: Adult, by mouth, 1 tablet daily; either 80
mg/12.5 mg or 160 mg/12.5 mg or 320
increased sweating, urinary disturbances, impo- 10 mg – 10’s. 2.5 mg – 10’s (in blisters)
mg/12.5 mg may be used. Following dose tence, gynaecomastia, weight changes, myalgia, 5 mg – 10’s (in blisters)
POM AMDICOR® (Neros) 10 mg – 10’s (in blisters)
titration sequence for the individual com- arthralgia, muscle cramps, visual disturbances,
Tablet, Amlodipine 5 mg
ponents, may increase dose to 160 mg/25 tinnitus, pruritus, rashes (including isolated re- 5 mg – 3 x 10’s (in blisters). POM AMLOVAR® (Neimeth)
mg or 320 mg/25 mg once daily depending ports of erythema multiforme), alopecia, purpura, Tablets, Amlodipine besylate 5 mg, 10 mg.
response and tolerance. Max. 320 mg/25 and skin discoloration; very rarely gastritis, pan- POM AMEDIN® (Medreich) 5 mg – 10’s; 100’s.
mg per day. creatitis, hepatitis, jaundice, cholestasis, gingival Tablets, Amlodipine (as besylate) 5 mg, 10 mg 10 mg – 10’s; 100’s.
The maximum antihypertensive effect is 5 mg – 20’s
hyperplasia, MI, arrhythmias, vasculitis, coughing, POM AMLOVIN® (Vinco)
seen within 2 to 4 weeks in most patients. 10 mg – 20’s
hyperglycaemia, thrombocytopenia, peripheral Tablets, Amlodipine 5 mg, 10 mg
POM CARVALS® H (Ranbaxy) neuropathy, angioedema, and urticaria. POM AMICON® (JB Pharma) Pack:10’s
Caplet, (80/12.5 mg), Valsartan 80 mg, hydrochlo- Advice to patients: Do not discontinue Tablets, Amlodipine (as besilate) 5 mg, 10 mg.
rothiazide 12.5 mg; white f-c caplet marked “VH1” 5 mg – 10 x 10’s (in blisters) POM AMVAZ® (Phillips/Dr. Reddy’s)
abruptly; report any dizziness, shortness of Tablets, Amlodipine maleate BP equiv. to Amlodipine
Pack: 3 x 10’s 10 mg-10 x 10’s (in blisters)
breath; palpitations, or oedema. 5 mg, 10 mg; uncoated tabs.
Caplet, (160/25 mg), Valsartan 160 mg, hydrochlo-
Nursing action:Administer once daily with or POM AMICRON® (JB Pharma) 5 mg – 2 x 14’s.
rothiazide 25 mg; white f-c caplet marked “VH3” Tablets, Amlodipine besylate 5 mg, 10 mg
Pack: 3 x 10’s without food. 10 mg – 2 x 14’s.
• Advise patient not to drive or operate machinery 5 mg – 1 x 10’s
POM JOLTAN® Plus (Joswe/Afrab) until stabilized on medication; to make position 10 mg – 1 x 10’s POM ASOMEX® (Fidson)
Tablets, (80/12.5 mg), Valsartan 80 mg, hydrochloro- changes slowly to prevent orthostatic hypotension. Tablets, Amlodipine (as besilate) 1.25 mg, 2.5 mg, 5
POM AMLODIP® (Pharmabase) mg; uncoated tabs.
thiazide 12.5 mg; f-c tab. • Advise patient to avoid OTC preparations unless Tablets, Amlodipine 5 mg, 10 mg
Pack: 30’s on prescription. 1.25 mg – 10’s
5 mg – 10 x 10’s 2.5 mg – 10’s
Tablets, (160/12.5 mg), Valsartan 160 mg, hydrochlo- • Teach patient to observe and report irregular 10 mg – 10 x 10’s
rothiazide 12.5 mg; f-c tab. heartbeat, shortness of breath, swelling of feet 5 mg – 10’s
Pack: 30’s and hands, severe dizziness, constipation, nausea, POM Amlodipine (Jawa) POM BG VASCOL® (BG Pharmacy)
Tablets, (160/25mg), Valsartan 160 mg, hydrochlo- hypotension. Tablet, Amlodipine besilate 5 mg Tablets, Amlodipine (as besylate) 5 mg, 10 mg.
rothiazide 25 mg; f-c tab. • Monitor pulse, I&O (note fluid retention), daily 5 mg – 10 x10’s. 5 mg – 10’s; 30’s; 100’s
10 mg – 10’s; 30’s; 100’s white to off white tab. marked ‘C’ on one side and 5 mg – 3 x 10’s; 10 x 10’s disease, heterozygous familial and nonfamilial
‘59’ on the reverse. 10 mg – 3 x 10’s; 10 x 10’s hypercholesterolemia, homozygous familial
POM CADIPROT® (Solidum)
10 mg – 20’s (in blisters). hypercholesterolemia, elevated serum TG
Tablets, Amlodipine (as besilate) 5 mg, 10 mg; f-c POM S-AMLO® (Pharma Ethics)
tabs. POM LODIPRESS® (Coriander) Tablets, Amlodipine besilate 2.5 mg, 5 mg. levels and primary dysbetalipoproteinemia.
5 mg – 30’s; 100’s Tablet, Amlodipine (as besylate) 5 mg; white tab. 2.5 mg – 3 x 10’s Contra-indications: Active liver disease or
10 mg – 30’s; 100’s. marked ‘Lod’ on one side and ‘5’ on the reverse. 5 mg – 3 x 10’s unexplained persistent elevations of serum
POM CERADIPINE® (Carebliss) POM LODIVASC® (May & Baker) POM S-NUMLO® (Apple Pharma) transaminases; Hypersensitivity to any com-
Tablets, Amlodipine besylate 5 mg, 10 mg; uncoated Tablets, Amlodipine besylate 5 mg, 10 mg Tablets, Amlodipine (as besilate) 2.5 mg, 5 mg ponent of the medication; Pregnancy and in
tab. Pack: 100’s 2.5 mg – 10’s . nursing mothers.
Pack: 10 x 10’s 5 mg – 10’s. Precautions: Women of childbearing age
POM LOFRAL® (Oculus)
POM CIKAVASC® (Michelle Lab) Tablets, Amlodipine 5 mg, 10 mg. POM STAMLO® (Phillips/Dr. Reddy’s) (adequate contraceptive measures should be
Tablets, Amlodipine besylate 5 mg, 10 mg 5 mg – 10’s; 30’s Tablets, Amlodipine (as besilate) 5 mg, 10 mg; used). Very rare cases of rhabdomyolysis with
5 mg – 10 x 10’s 10 mg – 10’s; 30’s uncoated tabs. acute renal failure secondary to myoglobinuria
10 mg – 100’s; 10 x 10’s (in blisters) 5 mg – 10’s. have been reported with the Atorvastatin and
POM LOPIN®-10 (Greenlife)
10 mg – 10’s. other HMG-CoA reductase inhibitors. Due to
POM CORVADIL® (Phillips) Tablet, Amlodipine (as besilate) 10 mg; uncoated tab.
Tablets, Amlodipine (as besilate) 5 mg, 10 mg. 10 mg – 1 x 10’s; 3 x 10’s; 10 x 10’s. POM SWIVASC® (Swipha) the risk of myopathy with HMG-CoA reductase
Tablets, Amlodipine (as besilate) 5 mg, 10 mg; f-c tabs inhibitors, patients should be advised to report
POM DEROX® (Hovid) POM MIRAVASC® (Miraflash) promptly unexplained muscle pain, tender-
5 mg – 10’s
Tablet, (5 mg), Amlodipine (as besilate) 5 mg; light Tablets, Amlodipine (as besilate) 5 mg, 10 mg;
10 mg – 10’s ness, or weakness, particularly if accompanied
yellow scored tab. uncoated tabs.
5 mg – 1 x 4’s; 2 x 14’s; 7 x 14’s 5 mg – 2 x 14’s (in blisters). POM TADIP®(Tamar & Pharez)
by malaise or fever.
Tablet, (10 mg), Amlodipine (as besilate) 10 mg; light 10 mg – 2 x 14’s (in blisters). Tablet, Amlodipine (as besilate) 5 mg Interactions: Atorvastatin may increase the
EMDEX
orange scored tab. 5 mg – 3 x 10’s risk of myopathy if co-administered with
POM LOVAPINE® (Crystal) cyclosporine, fibric acid derivatives, niacin,
10 mg – 1 x 4’s; 2 x 14’s; 7 x 14’s
Tablets, Amlodipine 5 mg, 10 mg.
AMLODIPINE plus LISINOPRIL erythromycin, and azole antifungals.
POM DILOPAX® (Korylns) 5 mg – 3 x 10’s.
Tablet, (5 mg), Amlodipine 5 mg; white tab. marked Adverse effects: Thrombocytopenia, allergic
10 mg – 3 x 10’s. POM CO-DILOPRIL® (Korlyns)
“DPX-5”. reaction, Quinke’s oedema, urticaria, abdom-
POM NAMLODIPINE®(NASDMU) Tablet, Amlodipine (as besilate) 5 mg, Lisinopril 5
5 mg – 2 x 14’s (in blister). inal pain, weight gain, back pain, jaundice,
Tablet, Amlodipine 5 mg; marked “NAMLO” on one mg; yellow oblong tab. marked ‘CDL’.
Tablet, (10 mg), Amlodipine 10 mg; white tab. Pack: 3 x 10’s (in blisters). dizziness, headache, dry mouth.
marked “DPX-10”. side and “NASDMU” on reverse side. Dose: Not recommended for initial therapy.
10 mg – 2 x 14’s 5 mg – 3 x 10’s
AMLODIPINE plus ATORVASTATIN The usual starting dose is 5 mg/10
POM DIPLOFAB® (FAB) POM NORDEXA® (Vixa) mg (Amlodipine/Atorvastatin respec-
Tablets, Amlodipine (as besilate) 5 mg, 10 mg. Therapeutic category: Long-acting calcium
Tablets, Amlodipine besylate 5 mg, 10 mg. tively) once daily; if greater BP control
5 mg – 1 x 10’s channel blocker, Synthetic lipid-lowering
5 mg – 10’s is needed, 10 mg/10 mg (Amlodipine/
10 mg – 1x 10’s agent.
10 mg – 10’s Atorvastatin respectively) can be
Pharmacology: Amlodipine inhibits the trans-
POM FEPILAT® (Evans) POM NORVASC® (Pfizer) administered.
membrane influx of calcium ions into vascular
Tablets, Amlodipine (as besilate) 5 mg, 10 mg; Tablets, Amlodipine besylate 5 mg, 10 mg; white
smooth muscle and cardiac muscle. It is a pe- POM CADUET® (Pfizer)
uncoated tabs. scored emerald-shaped tab.
ripheral arterial vasodilator that acts directly on Tablet, (5 mg/10 mg), Amlodipine (as besilate) 5 mg,
5 mg – 10’s (in blister) 5 mg – 10; 100
vascular smooth muscle to cause a reduction in Atorvastatin (as calcium salt) 10 mg; white, oval tab.
10 mg – 10’s (in blister) 10 mg – 10; 100.
Tablet, (10 mg/10 mg), Amlodipine (as besilate)
peripheral vascular resistance and reduction in
POM HOCHIVAX® (Hochiez) POM NORVATAB®(Embassy) 10 mg, Atorvastatin (as calcium salt) 10 mg; blue,
Tablet, Amlodipine (as besilate) 10 mg
blood pressure. Atorvastatin is a selective, com- oval tab.
Tablets, Amlodipine (as besylate) 5 mg, 10 mg. petitive inhibitor of HMG-CoA reductase, the
5 mg – 10’s; 100’s. 10 mg – 3 x 10 x 10’s
rate-limiting enzyme that converts HMG-CoA AMLODIPINE plus VALSARTAN
10 mg – 10’s; 100’s. POM ORKAL® (Taylek) to mevalonate, a precursor of sterols including
POM HYPERCOR® (Nomedi) Tablets, Amlodipine 5 mg, 10 mg Pharmacology: Amlodipine, a calcium channel
cholesterol. Atorvastatin lowers plasma choles-
Tablets, Amlodipine (as besilate) 5 mg, 10 mg 5 mg – 30’s (in blisters) blocker, acts by inhibiting the transmembrane
10 mg – 30’s (in blisters) terol and lipoprotein levels by inhibiting HMG-
5 mg – 1 x 10’s (in blisters) influx of calcium ions into the coronary vascular
CoA reductase and cholesterol synthesis in the
10 mg – 1 x 10’s (in blisters) POM JUVASC® (Juhel) smooth muscle and cardiac muscle. Extensively
liver and by increasing the number of hepatic
Tablet, Amlodipine besylate 5 mg. metabolized to inactive metabolites via CYP3A4.
POM K-AMLOD® (Kayhelt) LDL receptors on the cell-surface to enhance
Tablets, Amlodipine (as besilate) 5 mg, 10 mg; 5 mg – 10 x 10’s (in blisters); 500’s (in jars). 10% of unchanged drug and 60% of amlodipine
uptake and catabolism of LDL.
uncoated tab POM PEMALOD® (Pemason)
metabolites are excreted in urine. Elimination
Indications: For use in hypertensive patients
5 mg – 10’s (in blisters) Tablets, Amlodipine 5 mg, 10 mg half-life is approx. 30-50 hours.
with additional risk factors; specifically patients
10 mg – 10’s (in blisters) Valsartan is an orally active, potent and specific
POM PILOVAS® (Geneith) for whom treatment with both amlodipine
POM KARDAM® (Phillips)
angiotensin II receptor antagonist. It selectively
Tablets, Amlodipine (as besilate) 5 mg, 10 mg. and atorvastatin is appropriate for prevention
Tablet, (5 mg), Amlodipine (as besilate) 5 mg; white blocks the binding of angiotensin II to the
5 mg – 3 x 10’s of cardiovascular events. Amlodipine is indi-
to off white tab. marked ‘C’ on one side and ‘58’ on 10 mg – 3 x 10’s
AT1 receptor in vascular smooth muscle and
cated for hypertension, chronic stable angina,
the reverse. the adrenal glands, antagonizes the vasocon-
POM RELODIPIN® (Reals) and vasospastic angina while Atorvastatin
5 mg – 10’s (in blisters). strictor and aldosterone-secreting effects of
Tablet, (10 mg), Amlodipine (as besilate) 10 mg; Tablets, Amlodipine 5 mg, 10 mg is indicated for prevention of cardiovascular
angiotensin II at these receptors.
Valsartan does not inhibit ACE, also known Pack: 28’s multiforme and vasculitis. Depression of AV felodipine. Enzyme inhibitors (e.g. cimetidine,
as kininase II, which converts angiotensin I to Tablet, (10/160 mg), Amlodipine (besilate) 10 mg, conduction and bradycardia; moderate and erythromycin, itraconazole, ketoconazole and
angiotensin II and degrades bradykinin. Since Valsartan 160 mg; f-c tab. transient increased liver transaminases. certain flavonoids present in grapefruit juice)
there is no effect on ACE and no potentiation Pack: 28’s Dose: see below. may increase plasma concentration of felodip-
Tablet, (5/320 mg), Amlodipine (besilate) 5 mg,
of bradykinin or substance P, angiotensin II POM CASCOR®-XL (Ranbaxy)
ine. Enzyme inducers (e.g. phenytoin, carba-
Valsartan 320 mg; f-c tab.
antagonists are unlikely to be associated with Pack: 28’s Capsules, Diltiazem HCl USP 120 mg, 180 mg; ex- mazepine, rifampicin and barbiturates) may
coughing. Tablet, (10/320 mg), Amlodipine (besilate) 10 mg, tended-release capsules. decrease plasma concentrations of felodipine.
Minimally metabolized and primarily excreted Valsartan 320 mg; f-c tab. 120 mg – 3 x 10’s; 6 x 10’s (in blisters). Adverse effects: Flushing, headache, pal-
in faeces (83%) and urine (13%), mainly as Pack: 28’s 180 mg – 3 x 10’s; 6 x 10’s (in blisters). pitations, dizziness, fatigue, gravitational
unchanged drug. The half-life of valsartan is Dose: By mouth, Adult, Hypertension, Usually 180- oedema, rash and pruritus, gum hyperplasia,
6 hours. AMLODIPINE plus VALSARTAN 240 mg once a day; may adjust dose over angiodema, aggravation of angina on initiation
plus HYDROCHLOROTHIAZIDE 14 days as needed and tolerated, not ex-
Indications: Treatment of essential hyper- of therapy.
ceeding 540 mg once daily. Patients above
tension POM EXFORGE® HCT (Novartis) Advice to patients: Tablets should be swal-
60 years may respond to 120 mg.
Contra-indications: Hypersensitivity to the Tablet, Amlodipine (besylate) 5 mg, Valsartan 160 Angina, Initially 120 mg once daily, which lowed whole; do not chew, suck or break
active substances or to any of the excipients; mg, Hydrochlorothiazide 12.5 mg may be titrated over 7-14 days to doses of tablets.
pregnancy. Pack: 28’s upto 480 mg once daily. Nursing action: See under Amlodipine.
Precautions: Salt and/or volume depletion; Tablet, Amlodipine (besylate) 10 mg, Valsartan 160 Dose: Hypertension, initially 5 mg (elderly
mg, Hydrochloride 12.5 mg POM DILCONTIN® XL (Phillips)
Hyperkalaemia; Renal artery stenosis; Renal 2.5 mg) once daily in the morning;
Pack: 28’s Tablet, (90 mg), Diltiazem HCl 90 mg; white/grey f-c
impairment; Hepatic impaiment; Aortic and round tab. marked ‘DXL’ on one side and ‘90’ on the the dose may be increased or another
Tablet, Amlodipine (besylate) 5 mg, Valsartan 160
mitral valve stenosis, obstructive hypertrophic mg, Hydrochlorothiazide 25 mg reverse, in a controlled-release system. antihypertensive agent added if
cardiomyopathy. Heart failure or recent MI. Pack: 28’s 90 mg – 10 x 10’s (in blisters). necessary. Maintenance: 5-10 mg
EMDEX
Breastfeeding. Tablet, Amlodipine (besylate) 10 mg, Valsartan 160 Tablet, (120 mg), Diltiazem HCl 120 mg; white/grey once daily. Doses higher than 20 mg
Adverse effects: Dizziness, headache, somno- mg, Hydrochlorothiazide 25 mg f-c round tab marked ‘DXL’ on one side and ‘120’ on generally not required.
lence, orthostatic hypotension; tachycardia, Pack: 28’s the reverse, in a controlled-release system. Angina pectoris, initially 5 mg once
palpitations; exacerbation of angina, MI; Tablet, Amlodpine (besylate) 10 mg, Valsartan 320 120 mg – 10 x 10’s (in blisters). daily in the morning; increased if
mg, Hydrochlorothiazide 25 mg Tablet, Diltiazem HCl 180 mg; pink f-c, scored caplet
peripheral oedema; nasopharyngitis, URTI; needed to 10 mg once daily.
Pack: 28’s marked ‘DXL 180’, in a controlled-release system.
diarrohoea, nausea, abdominal pain, consti- Note: Tablets should be swallowed whole with
pation, dry mouth; cough, pharyngolaryngeal water, administered in the morning. Not indicated
DILTIAZEM for use in children.
pain; vertigo; tinnitus. Rarely hypersensitivity, FELODIPINE
visual disturbances, rash, erythema, joint swell- Therapeutic category: Calcium channel POM PLENDIL® (Reals)
blocker, non-dihydropyridine; Antihyperten- Therapeutic category: Antihypertensive/
ing, back pain, arthralgia, erectile dysfunction, Tablets, Felodipine 2.5 mg, 5 mg, 10 mg.
sive; Anti-anginal agent. Anti-angina
polyuria.
Indications: For the treatment of mild to mod- Pharmacology: Felodipine is a highly vascular LACIDIPINE
Dose: Adult, by mouth, initially 5 mg/80
erate essential hypertension; management selective calcium antagonist, which in thera-
mg or 5 mg/160 mg once daily in Therapeutic category: Antihypertensive.
of chronic stable angina and angina due to peutic doses has no direct effect on cardiac
patients whose BP is not adequately Pharmacology: Lacidipine is a specific and
coronary artery spasm. contractility or condition. As a result of arterior
controlled with the individual potent calcium antagonist, with a predominant
Contra-indications: Pregnancy and lactation. dilatation, it lowers systemic vascular resist-
components (lower dose for volume selectivity for calcium channels in the vascular
Bradycardia (<50 bpm), 2nd or 3rd degree heart ance and arterial blood pressure. Coronary
depleted patients). May increase smooth muscle. Its main action is to dilate
block, sick sinus syndrome, decompensated blood flow is increased due to dilatation of
dose after 2-4 weeks up to a max. 10 peripheral arterioles, reducing peripheral vas-
cardiac failure, patients with left ventricular both epicardial arteries and arterioles.
mg/320 mg per day. cular resistance and lowering blood pressure.
dysfunction following MI. Indications: Management of hypertension;
Elderly (>65 years): caution when Lacidipine is rapidly but poorly absorbed from
Precautions: Reduced left ventricular func- prophylaxis of chronic stable angina.
increasing dose. the GIT following oral dosing. It undergoes ex-
tion; Mild bradycardia, 1st degree AV block or Contra-indications: Pregnancy; hyper-sen-
Children and adolescents: Not recom- tensive first pass metabolism in the liver. Peak
prolonged PR interval; Acute porphyria. Use sitivity to felodipine or the ingredient; un-
mended for use in patients <18 years. plasma concentrations are reached between
with other drugs that can cause bradycardia compensated heart failure; acute myocardial
Renal impairment: No dosage adjustment for 30 and 150 minutes. The drug is eliminated
or other anti-arrhythmic agents. infarction; unstable angina pectoris.
mild to moderate renal impairment. primarily by hepatic metabolism and it is not
Interactions: Alpha-blockers; blood levels of Precautions: May precipitate significant hypo-
Hepatic impairment: Lower doses may be associated with either induction or inhibition
carbamazepine, cyclosporin, and theophylline tension which may result in myocardial ischaemia
considered in hepatic impairment or biliary of hepatic enzymes. Approximately 70% of the
may be increased when given with diltiazem; (withdraw if ischaemic pain or cardiogenic shock
obstructive disorders. administered dose is eliminated as metabolites
H2-antagonists may increase serum levels of occurs after initiating therapy). Avoid co-ad-
POM DRULOVASK®(Drugfield) in the faeces and the remainder as metabolites
diltiazem; Alcohol. ministration with grapefruit juice (may inhibit
Caplet, Amlodpine (as besilate) 5 mg, 10 mg in the urine.
Adverse effects: Occasionally, nausea, head- metabolism of felodipine leading to increased
Pack: 10’s; 30’s Indications: Treatment of hypertension either
ache, oedema of the legs, flushing, hypo- plasma concentration). Breast-feeding; hepatic
alone or in combination with other antihyper-
POM EXFORGE® (Novartis) tension, fatigue, GI disturbance and gingival impairment.
tensive agents e.g. Beta-blockers and diuretics.
Tablet, (5/80 mg), Amlodipine (besilate) 5 mg, Val- hyperplasia which disappear on cessation of Interactions: Co-administration with sub-
sartan 80 mg; f-c tab. Contra-indication: Hypersensitivity to lac-
treatment. Serious skin reactions such as ex- stances which interfere with the CYP3A4 en-
Pack: 28’s idipine.
foliative dermatitis and allergic skin reactions, zyme system may affect plasma concentrations
Tablet, (5/160 mg), Amlodipine (besilate) 5 mg, Precautions: Liver failure (antihypertensive ef-
such as angioneurotic oedema, erythema of dihydropyridine calcium antagonists such as
Valsartan 160 mg; f-c tab.
fect may be increased); Cardiac abnormalities; channels in the SA node, AV node, and vascula- Barbiturates e.g. Phenobarbital; Macrolide not administer through arteries or small peripheral
pregnancy, breast-feeding. ture, nicardipine and other members of the di- antibiotics e.g. Clarithromycin, Erythromycin; veins, such as those on the dorsum of the hand or
Interactions: Other antihypertensive agents hydropyridine group predominantly act on the Beta-blockers e.g. Metoprolol, Propranolol; wrist. If administering through a peripheral vein,
e.g. diuretics and beta-blockers (co-adminis- vasculature, making these agents more potent Protease inhibitors; Rifampicin; Anaesthetic the infusion site should be changed every 12 hours
to minimize the risk of peripheral venous irritation.
tration may have additive hypotensive effect). peripheral vasodilators. Nicardipine is available agents.
Monitor blood pressure and heart rate during and
Cimetidine (co-administration may increase for oral and IV administration. Highly protein Adverse effects: Flushing, peripheral oedema, after the infusion; avoid too rapid or excessive blood
plasma level of lacidipine). bound (>95%). Onset of action is 30-120 mins headache, dizziness, asthenia, fatigue, hy- pressure drop during treatment.
Adverse effects: Headache, flushing, oedema, (oral), 10 mins (IV); hypotensive effect approx. 20 potension, palpitations, nausea, vomiting, Visually inspect parenteral products for particulate
dizziness and palpitation; less commonly, mins. Duration ≤8 hours. Undergoes extensive abdominal pain, orthostatic hypotension; matter and discoloration prior to administration
asthenia, skin rash (including erythema and hepatic metabolism (major CYP3A4 substrate) less commonly drowsiness, dyspnoea, par- whenever solution and container permit. Dilute
itching), gastric upset, nausea and polyuria; and elimination is mainly renal (60%) and faecal aesthesia, syncope, nervousness, insomnia, ampules prior to infusion according to manufac-
few cases of chest pain and gingival hyper- (35%) as metabolites; <1% as unchanged drug tremor, rash, hypokalaemia, cardiac rhythm turer’s directions. Note the recommended final
concentration (usually 0.1-0.2 mg/mL). Nicardipine
plasia which are common with other calcium in the urine. Elimination half-life is biphasic due abnormalities, polyuria; Injection site reaction
injection is compatible with the following IV solu-
antagonists. to saturable first-pass metabolism, with the including phlebitis, venous thrombosis, local tions: dextrose (5%) water, dextrose (5%) water and
Dose: By mouth, Adult, initially 4 mg once initial half-life approx. 2-4 hours and a terminal irritation, swelling, extravasation, and rarely sodium chloride (0.45%), dextrose (5%) water and
daily; increased if necessary to 6 mg half-life of 11.5 hours. vascular impairment. sodium chloride (0.9%), dextrose (5%) water with 40
once daily after about 3–4 weeks (i.e. Indications: Short-term treatment of hyper- Nursing action: Administer through a central mEq potassium chloride, sodium chloride (0.45%),
enough time for full pharmacological tension when oral therapy is not feasible or or large peripheral vein to reduce the possi- and sodium chloride (0.9%).
effect to be realised). desirable; Treatment of hypertensive urgency bility of extravasation, venous thrombosis, Not compatible with sodium bicarbonate (5%), or
In liver disease, reduce dose to 2 mg or hypertensive emergency, except in the phlebitis, local irritation, swelling, and rarely lactated ringer’s solution.
once daily. setting of acute heart failure. Postoperative hy- vascular impairment. Avoid arteries and small (Additional information sourced from Nicardipine monograph
EMDEX
In renal disease, no dosage modifi- pertension, in the absence of supraventricular peripheral veins, such as those on the dorsum sourced from [1] https://www.clinicalkey.com/ [2] http://www.
uptodate.com/)
cation required (not excreted by the tachycardia or a recent myocardial infarction. of the hand or wrist. Change peripheral infu-
kidneys). Contra-indications: Hypersensitivity to sion sites every 12 hours to minimize the risk POM BINICAPIN® (Alpha)
In the elderly, initially 2 mg once nicardipine or other dihydropyridines; acute of venous irritation. Monitor blood pressure Injection, Nicardipine HCI (KP) 1.0 mg, Additive
daily; increased to 4-6 mg daily if stroke or intracranial haemorrhage; advanced and heart rate during and after the infusion; (isotonic agent): D-Sorbitol (KP) 48.0 mg, Additive
necessary as above. aortic stenosis; hypotension (systolic <90 avoid too rapid or excessive blood pressure (pH controlling agent): Citric acid hydrate (KP)
Note: Lacidipine should be taken at the same time mmHg); acute myocardial infarction, unstable drop during treatment. 0.525 mg, Additive (pH controlling agent): Sodium
each day, preferably in the morning. It can be taken or acute attacks of angina; bradycardia; car- Dose: Adult, Short-term treatment of hydroxide (KP) 0.090 mg Additive (Solvent): Water
at any time relative to food. diogenic shock. hypertension when oral therapy is for injection(KP) 0.090 mg per 10 mL.
Pack:10 mL x 10 amps
POM LACIPIL® (GSK) Precautions: Renal impairment (reduced renal not feasible or desirable; treatment of
Tablets, Lacidipine 2 mg, white, circular, f–c tab. clearance with increased risk of accumulation & hypertensive urgency or hypertensive
marked ‘2’ on one side; 4 mg, white, f–c, oval, bicon- NIFEDIPINE
toxicity); hepatic disease (use lower dose as it is emergency, except in the setting of
vex tab. scored on both sides. extensively metabolised in the liver); heart fail- acute heart failure, by continuous IV Indications: Hypertension.
ure; gastroesophageal reflux disease (GERD) or infusion, Initially 5 mg/hour; increase Contra-indications: Cardiogenic shock;
NICARDIPINE hiatal hernia associated with reflux esophagitis infusion rate by 2.5 mg/hour (every 5 advanced aortic stenosis; within 1 month of
Therapeutic category: Calcium channel (may relax the lower esophageal sphincter like mins for rapid BP reduction or every myocardial infarction; unstable or acute attacks
blocker, Dihydropyridine; Antihypertensive. other CCBs); pheochromocytoma; angina; por- 15 mins for gradual titration), up to a of angina; porphyria.
Pharmacology: Nicardipine is a selective tal hypertension (IV admin at high dose may max. 15 mg/hour. Decrease infusion Precautions: Stop if ischaemic pain occurs
calcium channel blockers with mainly vascular increase hepatic venous pressure); pregnancy, rate to 3 mg/hour when target BP is or existing pain worsens shortly after starting
effects. Its mechanism of action and clinical breast-feeding, children, elderly. achieved and switch to oral therapy treatment; poor cardiac reserve; heart failure or
effects closely resemble those of nifedipine and Interactions: Nicardipine is a major substrate as soon as possible. significantly impaired left ventricular function;
the other dihydropyridines (amlodipine, felodip- of CYP3A4; a substrate and inhibitor of P-gly- Postoperative hypertension, in the reduce dose in hepatic impairment (Appendix
ine), except that nicardipine is more selective for coprotein; a strong inhibitor of CYP2D6; also absence of supraventricular tachycar- 5); diabetes mellitus; may inhibit labour; preg-
cerebral and coronary blood vessels. It does not inhibits the CYP isoenzymes 2C19, 3A4, and dia or a recent myocardial infarction, nancy (Appendix 2); breastfeeding (Appendix
intrinsically decrease myocardial contractility 2C8. Generally, avoid combinations with strong by IV infusion, Initially 10 mg/hour for 3); avoid grapefruit juice (may affect metabo-
and has a longer half-life than nifedipine. Similar CYP3A4 inhibitors & inducers. Modify therapy 5 mins; titrate as needed to 12.5 mg/ lism); interactions: Appendix 1.
to nifedipine, nicardipine inhibits the influx of or avoid combinations with the following: hour for 5 mins, then up to 15 mg/ Adverse effects: Headache, flushing, dizziness,
extracellular calcium across the cell membranes Alpha-blockers e.g. Alfuzosin, Tamsulosin; Stat- hour for a max. 15 mins. If target BP lethargy; tachycardia, palpitations; gravita-
of myocardial and vascular smooth muscle ins e.g. Atorvastatin, Lovastatin, Simvastatin; achieved, reduce dose to 3 mg/hour tional oedema (only partly responsive to diu-
without changing serum calcium concentra- Orally inhaled corticosteroids e.g. Budesonide, IV for 15 mins and then adjust by retics); rash (erythema multiforme reported),
tions and inhibits intracellular phosphodiester- Fluticasone; Salmeterol; 5-alpha reductase 1-2.5 mg/hour to maintain BP control. pruritus, urticaria; nausea, constipation or
ase. Unlike nifedipine, however, nicardipine has inhibitors e.g. Sildenafil, Tadalafil, Vardenafil; Elderly: Initiate at the lower end of the diarrhoea; increased frequency of micturition;
greater selectivity for vascular smooth muscle Thioridazine; Vincristine; Amiodarone; Azole dosage range and adjust cautiously eye pain, visual disturbances; gum hyperplasia;
than for cardiac muscle. Thus, nicardipine antifungal agents e.g. Itraconazole; Carba- based on clinical response. paraesthesia, myalgia, tremor; impotence,
relaxes the peripheral vasculature with little or mazepine, Phenytoin; Codeine; Citalopram, Administration: Administer by slow IV infusion. To gynaecomastia; depression; telangiectasis;
no negative inotropic effect. While verapamil Fluoxetine; Cimetidine; Clopidogrel; Colchicine; reduce the risk of infusion-site reactions, administer cholestasis, jaundice.
and diltiazem exert balanced effects on calcium Diclofenac; Digoxin; Doxorubicin; Fentanyl; through large peripheral veins or central veins. Do Nursing action: Administer with or without
220 | 5.3.7 Calcium–channel blockers 5.3.8 Diuretics | 221
meals. 20 mg – 2 x 14’s POM NIFETAB® (Onifam) slowly to prevent orthostatic hypotension.
• Sustained release products should be given with Tablet, (30 mg), Nifedipine 30 mg; prolonged-release, Tablet, Nifedipine 20 mg; extended-release tab. • Advise patient to limit caffeine intake and to avoid
food and not crushed or chewed. pink f-c tab. 20 mg – 3 x 10’s alcohol and OTC drugs unless prescribed.
• Advise patient not to drive or operate machinery 30 mg – 2 x 14’s • Signs of CHF such as swelling of hands and feet
POM NIFLOPIN® SR (Pharmabase)
until stabilized on medication; to make position or shortness of breath should be reported to the
POM CORACTEN® (GSK) Tablet, Nifedipine 20 mg; extended release tab.
changes slowly to prevent orthostatic hypotension. physician.
Capsule, (spansule), Nifedipine 20 mg; s-r light- 20 mg – 5 x 10’s
• Advise patient to limit caffeine intake and to avoid • Monitor BP closely.
brown/red capsule, containing yellow pellets.
alcohol and OTC drugs. POM ZENUSIN®-20 SR (Occulus) Dose: By mouth, Angina, 80-120 mg 3 times
• Patient should notify physician if angina pain is POM FLADIPINE® (Miraflash) Tablet, Nifedipine 20 mg; sustained-release tab. daily; Hypertension, 240-480 mg daily
not reduced when taking this drug, and if irregular Tablet, (Retard), Nifedipine 20 mg. 20 mg – 30’s. in 2-3 divided doses;
heartbeat, shortness of breath, swelling, dizziness, 20 mg – 10 x 10’s (in blister) Supraventricular tachyarrhythmias,
POM ZODIPINE® (Bakangizo)
constipation, nausea, or hypotension occurs.
POM FRAPINE® (Embassy) Tablet, Nifedipine 20 mg 40-120 mg 3 times daily.
• Advise patient not to stop therapy without phy-
sician’s advice.
Tablet, Nifedipine 20 mg. By slow IV injection over 2 mins (3
20 mg – 10’s. VERAPAMIL mins in elderly ), Supraventricular
Dose: Hypertension, by mouth (as sus-
tained-release tablets), ADULT usual POM HARTIPIN® (Kayhelt) Therapeutic category: Antianginal Agent; An- tachyarrhythmias, 5-10 mg; a second
range 20–100 mg daily in 1–2 divided Tablet, Nifedipine 20 mg; sustained-release f-c tab. tiarrhythmic Agent,Class IV; Antihypertensive; dose of 10 mg may be given 15-30
doses, according to manufacturer’s 20 mg – 3 x 10’s; 10 x 10’s Calcium Channel Blocker. mins after the initial dose if patient
directions. POM MEDIPINE® (Evans) Pharmacology: Verapamil inhibits calcium ion tolerates, but does not respond to
Note: Prescribers should be aware that different Tablet, Nifedipine 20 mg. influx across cardiac and smooth muscle cells, initial dose.
formulations of sustained-release tablets may not 20 mg – 30’s; 100’s. thus decreasing myocardial contractility and Note: I.V. administration should preferably be done
have the same clinical effect; if possible, the patient oxygen demand, and dilates coronary arteries with close BP and ECG monitoring.
POM NIF® (Pharma Ethics)
should be maintained on the same brand. and arterioles. POM Verapamil (Alpha)
EMDEX
Retard tablet, Nifedipine 20 mg.
Short-acting formulations of nifedipine should 20 mg – 3 x 10’s Indications: Angina pectoris (vasospastic Tablets, Verapamil 40 mg, 80 mg, 120 mg.
be avoided in hypertension, particularly in ,chronic stable, unstable), hypertension, su- 40 mg – 28’s
POM NIFE-D® (Zoomota) 80 mg – 28’s
patients who also have angina, since their praventricular tachyarrhythmias.
Tablet, Nifedipine 20 mg; sustained-release purple 120 mg – 28’s.
use may be associated with large variations in tab. Contra-indications: Sinus bradycardia;
blood pressure and reflex tachycardia, possi- 20 mg – 10 x 10’s. ventricular tachycardia; 2nd or 3rd degree AV POM Verapamil (Sanofi)
bly leading to myocardial or cerebrovascular block; cardiogenic shock; artrial fibrillation or Tablets, Verapamil HCl 40 mg, 80 mg; coated tabs.
POM NIFECARD® (Taylek) flutter associated with accessory conduction 40 mg – 100; 1000.
ischaemia.
Retard tablet, Nifedipine 20 mg. 80 mg – 100; 1000.
pathways; hypersensitivity to verapamil or
POM Nifedipine (EDL 10.3) 20 mg – 50. Injection, Verapamil HCl 2.5 mg per mL; in 2 mL amp.
Slow-release tablet, Nifedipine 20 mg.
any component.
POM NIFECARD XL® (Taylek) Pack: 5; 25.
Precautions: I.V. administration should be
POM ACEFEX® (Chanmedi) Tablet, Nifedipine 30 mg; extended release tab. done with ECG and B.P. monitoring plus facil-
Tablet, Nifedipine 20 mg. 30 mg – 30’s. 5.3.8 Diuretics
ities for resustation and cardioversion. Preg-
20 mg – 10 x 10’s. See also section 5.2
POM NIFEDIN® (Pemason) nancy (avoid during the Ist half ), breast-feed-
POM ADALAT XL® (Bayer Schering) Tablets, (Retard), Nifedipine 10 mg, 20 mg; s-r pink ing; hepatic or renal impairment; hypotension;
Tablets, Nifedipine 30 mg, 60 mg. f-c tabs. avoid abrupt withdrawal. AMILORIDE plus
30 mg – 2 x 14’s 10 mg – 10 x 10’s. Adverse effects: Constipation, headache, HYDROCHLOROTHIAZIDE
60 mg – 2 x 14’s 20 mg – 3 x 10’s.
dizziness, orthostatic hypotension, peripheral See under section 5.2.3
POM ARCONIFED® (Strides Vital) POM Nifedipine (Zolon) oedema; impairment of liver or kidney function
Capsule, Nifedipine 10 mg. Tablets, Nifedipine 10 mg, 20 mg; f-c extended especially in high doses; bradycardia; Ist, 2nd or POM Amiloride plus Hydrochlorothiazide (EDL
10 mg – 10 x 10’s release tabs. 3rd degree A-V block. 10.3)
10 mg – 3 x 10’s (in blisters) Advice to patients: Sustained release products Tablet, Amiloride (as HCl) 2.5 mg, hydrochlorothiazide
POM APO-NIFED-PA® (Lahams) 20 mg – 3 x 10’s (in blisters)
Tablet, (prolonged action), Nifedipine 20 mg; grey- should be taken with food and not crushed; 25 mg.
ish-pink, f-c tab. marked ‘APO’ on one side and ‘20’ POM Nifedipine (Zoomota) limit caffeine intake; notify physician if angina
on reverse. Tablet, Nifedipine 20 mg; f-c tab. pain is not reduced when taking this drug ,or HYDROCHLOROTHIAZIDE
20 mg – 100’s. if irregular heartbeat or shortness of breath Indications: Alone in mild hypertension, and
POM NIFEDOSE® (Crystal)
POM CARDOVASC® (May & Baker) Capsule, Nifedipine 20 mg. occurs. in combination with other drugs in moderate
Tablet, (Retard), Nifedipine. 20 mg – 3 x 10’s; 10 x 10’s. Nursing action: Give before meals, at bedtime. to severe hypertension; heart failure (section
Pack: 5 x 10’s. • Taking sustained-release tablets with food may 5.1); oedema (section 5.2.1).
POM NIFEGEM® Retard (Gemini)
Tablet, (XL), Nifedipine. decrease rate and extent of absorption, but allows Contra-indications: Severe renal or severe
Tablet, Nifedipine 20 mg.
Pack: 3 x 10’s. smaller fluctuations of peak and trough blood hepatic impairment; hyponatraemia, hypercal-
20 mg – 20; 56; 100.
levels. Do not crush sustained-release drug prod- caemia, refractory hypokalaemia, symptomatic
POM CARDIPIN-SR® (Ichie-Benson) uct; administer around-the-clock to promote less
POM NIFENDAL® (Pharmabox)
Tablet, Nifedipine 20 mg; s-r tab. hyperuricaemia; Addison disease.
Tablet, Nifedipine 20 mg; orange f-c tab. variation in peak and trough serum levels.
20 mg – 10’s • Give I.V. dose slowly over at least 3 minutes to Precautions: Renal and hepatic impairment
POM NIFEPRESS® (Coriander) minimize the risk of adverse reactions. (Appendices 4 and 5); pregnancy (Appendix 2)
POM CAREDIN LA® (Medreich)
Capsule, Nifedipine 20 mg; s-r pellets in a cap. • Advise patient not to drive or operate machinery until and breastfeeding (Appendix 3); elderly; elec-
Tablet, (20 mg), Nifedipine 20 mg; prolonged-release,
20 mg – 14’s stabilized on medication; to make position changes trolytes may need to be monitored with high
pink f-c tab.
222 | 5.4 Antiarrhythmic drugs 5.4 Antiarrhythmic drugs | 223
doses or in renal impairment; may aggravate valvular or myocardial disease, and in the (beta-blocker) (but not sotalol) and pacing; unpredictable; avoid rapid IV administration or
diabetes mellitus and gout; may exacerbate elderly. Warfarin is preferred to acetylsalicylic antiarrythmic drugs (including lidocaine) overdose (may precipitate circulatory collapse);
systemic lupus erythematosus; porphyria; acid in preventing emboli. If atrial fibrillation should be avoided because they can further perform chest X-ray before treatment; renal
interactions: Appendix 1. began within the previous 48 hours and there prolong the QT interval. impairment; heart failure.
Adverse effects: Fluid and electrolyte imbalance does not appear to be a danger of throm- Bradyarrhythmias Interactions: Due to long half-life of amiodar-
leading to dry mouth, thirst, GI disturbances boembolism, antiarrhythmic drugs, such as one, interaction may still occur several weeks
(including nausea, vomiting), weakness, lethargy, procainamide or quinidine, may be used to Sinus bradycardia (less than 50 beats/minute) after discontinuation of therapy. Oral antico-
drowsiness, seizures, headache, muscle pains terminate the fibrillation or to maintain sinus associated with acute myocardial infarction agulant (enhanced anticoagulant effect due
or cramps, hypotension (including postural rhythm after cardioversion. may be treated with atropine. Temporary pac- to inhibition of its metabolism). Antiepileptics
hypotension), oliguria, arrhythmias; hypokal- ing may be required in unresponsive patients. (metabolism of phenytoin inhibited with pos-
Atrial flutter Drugs are of limited value for increasing the
aemia, hypomagnesaemia, hyponatraemia, sible symptoms of phenytoin toxicity). Avoid
hypochloraemic alkalosis, hypercalcaemia; hy- Digoxin will sometimes slow the ventricular sinus rate long term in the presence of intrinsic co-administration with TCAs, antihistamines
perglycaemia, hyper-uricaemia, gout; rash, pho- response. Reversion to sinus rhythm is best sinus node disease and permanent pacing is (astemizole and terfenadine), antimalarials
tosensitivity; altered plasma lipid concentration; achieved by direct current electrical shock. usually required. (chloroquine, halofantrine, quinine, meflo-
rarely impotence (reversible); blood disorders If the arrhythmia is long-standing, treatment Cardiac arrest quine, hydroxychloroquine), antipsychotics
(including neutropenia, thrombocytopenia); with an anticoagulant should be considered (pheno-thiazines, haloperidol, pimozide), and
before cardioversion to prevent emboli. In cardiac arrest, epinephrine (adrenaline) is
pancreatitis, intrahepatic cholestasis; acute renal given by intravenous injection in a dose of 1 cisapride due to increased risk of ventricular
failure; hypersensitivity reactions (pneumonitis, Intravenous verapamil reduces ventricular arrhythmias. Beta-blockers and calcium-chan-
fibrillation during paroxysmal (sudden onset mg (10 mL of 1 in 10 000 solution) as part of the
pulmonary oedema, severe skin reactions). procedure for cardiopulmonary resuscitation. nel blockers (increased risk of bradycardia, AV
Dose: Hypertension, by mouth, ADULT 12.5 and intermittent) attacks of atrial flutter. An block and myocardial depression). Lithium
mg daily increased to 25–50 mg daily initial intravenous dose may be followed (increased risk of hypothyroidism). Cimetidine
AMIODARONE
EMDEX
if necessary. by oral treatment; hypotension may occur (increased plasma concentration of amiodar-
with high doses. It should not be used for Therapeutic category: Antiarrhythmic Agent,
POM Hydrochlorothiazide (WMF 12.3) Class III. one). Cardiac glycosides (increased plasma
tachyarrhythmias where the QRS complex is concentration of digoxin).
Tablet (scored), Hydrochlorothiazide 25 mg wide unless a supraventricular origin has been Pharmacology: Amiodarone is a Class III anti-
arrhythmic that inhibits adrenergic stimulation, Adverse effects: Phototoxicity, skin reactions,
See under section 5.2 for the proprietary preparations. established beyond doubt. If the flutter cannot visual disturbances, anaphylaxis on rapid
be restored to sinus rhythm, antiarrhythmics prolongs the action potential and refractory
period in myocardial tissue; decreases A-V injection, pulmonary fibrosis, interstitial pneu-
5.4 Antiarrhythmic drugs such as quinidine can be used. monitis, hypotension, hypothyroidism or hy-
conduction and sinus node function. It is ad-
Treatment of arrhythmias requires precise diag- Paroxysmal supraventricular tachycardia perthyroidism; GI, haematologic, neurological,
ministered orally or by IV infusion.Unlike oral
nosis of the type of arrhythmia, and electrocar- In most patients this remits spontaneously or amiodarone, IV amiodarone may act relatively hepatic, cardiac, CNS, and respiratory effects.
diography is essential; underlying causes such can revert to sinus rhythm by reflex vagal stim- rapidly. Amiodarone has a very long half – life Advice to patients: Take with food; use sun-
as heart failure require appropriate treatment. ulation. Failing this, intravenous injection of a (extending to several weeks) and only needs screen or stay out of sun to prevent burns;
betaadrenoceptor antagonist (beta-blocker) to be given once daily (but high doses may may wear sunglasses if photophobia occurs;
Antiarrhythmic drugs must be used cautiously do not discontinue abruptly; notify physician
since most drugs that are effective in treat- or verapamil may be effective. Verapamil and cause nausea unless divided).It is not consid-
a beta-blocker should never be administered ered a first – line antiarrhythamic due to high if persistent dry cough or shortness of breath
ing arrhythmias can provoke them in some occurs (may be signs of respiratory failure).
circumstances; this arrhythmogenic effect is concomitantly because of the risk of hypoten- incidence of adverse reactions.
sion and asystole. Indications: Treatment of arrhythmias particu- Nursing action: Divide oral loading dose
often enhanced by hypokalaemia. When an- into three equal doses and give with meals to
tiarrhythmic drugs are used in combination, Ventricular tachycardia larly those refractory to other therapy or when
other drugs are contra-indicated; may be used minimize GI upset. Maintenance dose may be
their cumulative negative inotropic effects Very rapid ventricular fibrillation causes pro- given once daily, but may be divided into two
may be significant, particularly if myocardial for paroxysmal supraventricular, nodal and
found circulatory collapse and must be treated doses and given with meals if GI upset occurs.
function is impaired. ventricular tachycardias, atrial fibrillation and
immediately with direct current shock. In more • Monitor liver-function and thyroid-function tests,
flutter, ventricular fibrillation. BP and heart rate; report any significant changes
Atrial fibrillation stable patients intravenous lidocaine or pro-
Contra-indications: Hypersensitivity to to the physician.
The increased ventricular rate in atrial fibrillation cainamide may be used. After sinus rhythm is
amiodarone; severe sinus node dysfunction; • Observe closely for adverse reactions including
can be controlled with a beta-adrenoceptor restored, drug therapy to prevent recurrence of
marked sinus bradycardia except if pacemaker pulmonary toxicity. Advise patient to use a sun-
antagonist (beta-blocker) or verapamil. ventricular tachycardia should be considered;
is fitted; thyroid disease; avoid IV use in severe screen to prevent photosensitivity.
Digoxin slows the ventricular response and a beta-adrenoceptor antagonist (beta-blocker)
respiratory failure; iodine sensitivity; sino-atrial Dose: By mouth, 200 mg 3 times daily for 1
or verapamil may be effective.
is particularly appropriate if atrial fibrillation heart block; pregnancy and breast-feeding; cir- week reduced to 200 mg twice daily
is accompanied by congestive heart failure. Torsades de pointes is a special form of ventricu- culatory collapse; severe arterial hypotension. for a further week; maintenance,
Intravenous digoxin is rarely of value for lar tachycardia associated with prolongation Precautions: Hospitalize patients while in- usually 200 mg daily or the minimum
rapid control of the ventricular rate because of the QT interval; it may be congenital but is itiating therapy; perform liver-function and required to control the arrhythmia.
response may take many hours. If adequate often druginduced. Initial treatment with intra- thyroid-function tests before therapy and POM AMIODAR® (Micronova)
control at rest or during exercise cannot be venous infusion of magnesium sulfate (usual then every 6 months; elderly are predisposed Tablet, Amiodarone hydrochloride 100 mg, 200 mg;
achieved readily verapamil may be introduced dose 2 g over 10–15 minutes, repeated once if to toxic effects; due to extensive tissue distri- uncoated tab.
with digoxin, but it should be used with necessary) together with temporary pacing is bution and long half-life, the time arrhythmia Pack: 30’s
caution if ventricular function is impaired. usually effective. Prolonged QT interval may be will reocccur following discontinued therapy
POM CORDARONE® (Sanofi)
Anticoagulants are indicated especially in treated with a beta-adrenoceptor antagonist or interaction with subsequent therapy is Tablet, Amiodarone 200 mg; white scored tab
224 | 5.4 Antiarrhythmic drugs 5.4 Antiarrhythmic drugs | 225
200 mg – 30; 50. and heart failure); Wolff-Parkinson-White • Do not crush controlled release capsules; consti- grade of atrioventricular block or any other
syndrome or other accessory pathway, par- pation can be managed with proper diet or bulk type of conduction disturbances, severe
ATENOLOL ticularly if accompanied by atrial fibrillation; laxatives or water; give chewing gum or hard candy myocardial depression, acute porphyria or
ventricular tachycardia or fibrillation; inter- to relieve the discomfort of dry mouth. hypovolaemia.
Indications: Arrhythmias; angina (section 5.5);
• Advise patient to avoid alcohol, and OTC drugs
hypertension (section 5.3); migraine prophy- mittent complete heart block; second-degree Precautions: Lower dosage in congestive
(unless on prescription).
laxis (section 1.9.2). atrioventricular block. • Instruct patient to make position changes gradu- heart failure and following cardiac surgery;
Contra-indications: History of asthma or Precautions: Recent MI; sick sinus syndrome; ally and to avoid hazardous activities if drowsiness bradycardia, hepatic impairment (Appendix
bronchospasm (unless no alternative, then with severe pulmonary disease; thyroid disease; or blurred vision occurs. 5), severe respiratory depression; elderly; preg-
extreme caution and under specialist super- elderly (reduce dose); renal impairment (Ap- • Monitor pulse, I&O (note fluid retention), daily nancy (Appendix 2), breastfeeding (Appendix
vision); uncontrolled heart failure, Prinzmetal pendix 4); avoid hypokalaemia; avoid rapid weight (inform doctor of rapid increase), BP, 3); interactions: Appendix 1.
angina, marked bradycardia, hypotension, sick IV administration (nausea and risk of arrhyth- respiration. Adverse effects: Dizziness, paraesthesia,
sinus syndrome, second – and third-degree mias); pregnancy (Appendix 2); breastfeeding • Notify physician of urinary retention or worsening drowsiness, confusion, apnoea, respiratory
CHF.; if pulse rate is below 60 beats/minute or
atrioventricular block, cardiogenic shock; (Appendix 3); interactions: Appendix 1. depression, coma, seizures, and convulsions,
above 120 beats/minute.
metabolic acidosis; severe peripheral arterial Adverse effects: Usually associated with ex- hypotension, arrhythmias, heart block, cardi-
Dose: By mouth, 300-800 mg in divided
disease; phaeochromocytoma (unless used with cessive dosage and include anorexia, nausea, ovascular collapse and bradycardia (may lead
doses.
alpha-blocker). vomiting, diarrhoea, abdominal pain; visual to cardiac arrest); nystagmus often an early
Precautions: Avoid abrupt withdrawal espe- disturbances, headache, fatigue, drowsiness, POM Disopyramide (EDL 10.2) sign of lidocaine overdosage; hypersensitivity
cially in ischaemic heart disease; history of confusion, dizziness, delirium, hallucinations, Tablet or Capsule, Disopyramide 100 mg, 150 mg reported.
obstructive airways disease (use with caution depression; arrhythmias, heart block; rarely Nursing action: Administer I.M. injection in
and monitor lung function—see also Contrain- rash, intestinal ischaemia; gynaecomastia on EPINEPHRINE deltoid muscle; aspirate to avoid intravascular
dications above); pregnancy (Appendix 2); long-term use; thrombocytopenia reported. Synonym: Adrenaline. administration. Check site regularly for infiltra-
EMDEX
breastfeeding (Appendix 3); first-degree atri- Dose: Atrial fibrillation, by mouth, ADULT Indications: Cardiac arrest; anaphylaxis (section or extravasation.
oventricular block; liver function deteriorates 1–1.5 mg in divided doses over 24 tion 8.2). • Local thrombophlebitis may occur in patients
in portal hypertension; reduce dose in renal hours for rapid digitalization or 250 Precautions: Heart disease, hypertension, receiving prolonged I.V. infusions; check I.V. site
impairment (Appendix 4); diabetes mellitus µg 1–2 times daily if digitalization less arrhythmias, cerebrovascular disease; hyper- regularly for infiltration or extravasation.
thyroidism, diabetes mellitus; angle-closure • Monitor patient’s response, especially B.P. and
(small decrease in glucose tolerance, masking urgent; maintenance 62.5–500 µg
serum electrolytes, BUN, and creatinine and notify
of symptoms of hypoglycaemia); history of daily (higher dose may be divided), glaucoma; second stage of labour; interac-
physician of any abnormalities.
hypersensitivity (increased reaction to aller- according to renal function and heart tions: Appendix 1. • Discontinue drug and notify physician immediately
gens, also reduced response to epinephrine rate response; usual range 125–250 Adverse effects: Anxiety, tremor, tachycardia, if toxic signs such as dizziness, confusion occur;
(adrenaline); myasthenia gravis; interactions: µg daily (lower dose more appropri- headache, cold extremities; nausea, vomiting, continued infusion may lead to seizures and coma.
Appendix 1. ate in elderly). sweating, weakness, dizziness, hyperglycae- Dose: Ventricular arrhythmias, by IV injection,
Adverse effects: GI disturbances (nausea, Emergency control of atrial fibrillation, mia also reported; in overdosage arrhythmias, ADULT, loading dose of 50–100 mg
vomiting, diarrhoea, constipation, abdominal by IV infusion over at least 2 hours, cerebral haemorrhage, pulmonary oedema. (or 1–1.5 mg/kg) at a rate of 25–50
cramp); fatigue; cold hands and feet; exacerba- ADULT 0.75–1 mg. Dose: Caution: different dilutions of epineph- mg/minute, followed immediately
tion of intermittent claudication and Raynaud Note: Infusion dose may need to be reduced if rine injection are used for different by IV infusion of 1–4 mg/minute,
phenomenon; bronchospasm; bradycardia, digoxin or other cardiac glycoside given in previous routes of administration with ECG monitoring of all patients
heart failure, conduction disorders, hypoten- 2 weeks. Cardiac arrest, by IV injection through (reduce infusion dose if required for
sion; sleep disturbances, including nightmares; POM Digoxin (WMF 12.2) a central line using epinephrine injec- longer than 24 hours).
depression, confusion; hypoglycaemia or Tablets, Digoxin 62.5 µg, 250 µg. tion 1 in 10 000 (100 µg/mL), ADULT Important: Following IV injection lidocaine has
hyperglycaemia; exacerbation of psoriasis; rare Oral liquid, Digoxin 50 µg/mL. 1 mg (10 mL), repeated at 3-minute a short duration of action (of 15–20 minutes). If it
reports of rashes and dry eyes (oculomucocu- Injection, Digoxin 250 µg/mL; in 2-mL ampoule. intervals if necessary. cannot be given by IV infusion immediately, the
Note: If central line not in place, same dose is given initial IV injection of 50–100 mg can be repeated
taneous syndrome—reversible on withdrawal).
DISOPYRAMIDE via peripheral vein, then flushed through with at if necessary once or twice at intervals of not less
Dose: Arrhythmias, by mouth, ADULT 50 mg than 10 minutes.
Therapeutic category: Class I-A anti-arrhyth- least 20 mL sodium chloride 0.9% injection (to
once daily, increased if necessary to
expedite entry into circulation).
50 mg twice daily or 100 mg once mic agent. POM Lidocaine (WMF 12.2)
daily. Indications: Treatment and prevention of POM Epinephrine (WMF 12.2) Injection, Lidocaine HCl 20 mg/mL; in 5-mL ampoule.
ventricular arrhythmias. Injection, Epinephrine (as acid tartrate or HCl) 100 POM Lidocaine (EDL 10.2)
POM Atenolol (WMF 12.2) µg/mL; in 10-mL ampoule.
Contra-indications: Complete heart block. Injection, Lidocaine (as HCl) 20 mg per mL; in 5-mL
Tablets, Atenolol 50 mg, 100 mg.
Precautions: Cardiac failure, partial heart POM Adrenaline (Alpha) amp.
See preparations under section 5.3.1 block, renal or hepatic impairment, glaucoma, Injection, Epinephrine 1 mg per mL (1: 1000); clear See under section 3.4 for preparations.
urinary retention, myasthenia gravis. colourless soln in colourless transparent 1-mL amp.
DIGOXIN Adverse effects: Anticholinergic effects, GI up- Pack: 10 x 10’s
set, skin rashes, CNS disturbances, muscle ache PROCAINAMIDE
Indications: Supraventricular arrhythmias,
and weakness, hypoglycaemia, hypokalaemia. LIDOCAINE Indications: Severe ventricular arrhythmias,
particularly atrial fibrillation; heart failure
(section 5.1). Nursing action: Administer around-the-clock Indications: Ventricular arrhythmias (espe- especially those resistant to lidocaine or those
rather than 4 times/day (i.e, 12-6-12-6, not cially after myocardial infarction); local anaes- appearing after MI; atrial tachycardia, atrial
Contra-indications: Hypertrophic obstructive
9-1-5-9) to promote less variation in peak and thesia (section 3.4). fibrillation; maintenance of sinus rhythm after
cardiomyopathy (unless also atrial fibrillation
trough serum levels. Contra-indications: Sino-atrial disorder, any cardioversion of atrial fibrillation.
226 | 5.4 Antiarrhythmic drugs 5.5 Antianginal drugs | 227
Contra-indications: Torsades de pointes, sys- POM Procainamide (WMF 12.2) cardia, second – and third-degree AV block, • unstable angina (acute coronary insufficiency),
temic lupus erythematosus, heart block, heart Injection, procainamide HCl 100 mg/mL; in 10-mL sinoatrial block, sick sinus syndrome; car- which is considered to be an intermediate stage
failure, hypotension. ampoule. diogenic shock; history of heart failure or between stable angina and myocardial infarction
Precautions: Elderly, renal impairment (Ap- significantly impaired left ventricular function • Prinzmetal angina (variant angina), caused by
POM Procainamide (EDL 10.2)
coronary vasospasm, in which attacks occur at rest.
pendix 4), hepatic impairment (Appendix 5), Tablet, Procainamide (as HCl) 250 mg. (even if controlled by therapy); atrial flutter or
asthma, myasthenia gravis, pregnancy; breast- Injection, Procainamide (as HCl) 100 mg per mL; in fibrillation complicating Wolff-Parkinson-White Management depends on the type of angina
feeding (Appendix 3); use only under specialist 10-mL amp. syndrome; porphyria. and may include drug treatment, coronary
supervision; interactions: Appendix 1. Precautions: First-degree AV block; acute artery bypass surgery, or percutaneous translu-
Adverse effects: Nausea, vomiting, diarrhoea, PROPRANOLOL phase of myocardial infarction (avoid if brad- minal coronary angioplasty.
anorexia, rashes, pruritus, urticaria, flushing, See under section 5.3.1 ycardia, hypotension, left ventricular failure); Stable angina
fever, myocardial depression, heart failure, hepatic impairment (Appendix 5); children
Drugs are used both for the relief of acute pain
angioedema, depression, dizziness, psychosis; POM Propranolol (EDL 10.2) (specialist advice only); pregnancy (Appendix
and for prophylaxis to reduce further attacks;
blood disorders include leukopenia, haemo- Tablets, Propranolol (as HCl) 10 mg, 40 mg 2); breastfeeding (Appendix 3); avoid grapefruit
Injection, Propranolol (as HCl) 1 mg per mL; in amp. they include organic nitrates, beta-adreno-
lytic anaemia and agranulocytosis after pro- juice (may affect metabolism); interactions:
ceptor antagonists (beta-blockers), and calci-
longed treatment; lupus erythematosus-like Appendix 1.
QUINIDINE um-channel blockers.
syndrome; high plasma procainamide concn Verapamil and Beta-Blockers: Both verapamil
may impair cardiac conduction. Indications: Suppression of supraventricular and beta-blockers have cardio-depressant NITRATES
Advice to patients: Do not discontinue arrhythmias and ventricular arrhythmias; main- activity, and their use together may lead to Organic nitrates have a vasodilating effect; they
therapy unless instructed by physician; notify tenance of sinus rhythm after cardioversion of bradycardia, heart block and left ventricular are sometimes used alone, especially in elderly
physician or pharmacist if soreness of mouth, atrial fibrillation. failure, particularly in patients with myocardial patients with infrequent symptoms. Tolerance
throat or gums, unexplained fever, or symp- Contra-indications: Complete heart block insufficiency. Treatment with beta-blockers leading to reduced antianginal effect is often
EMDEX
toms of upper respiratory tract infection occur; Precautions: Partial heart block; extreme care should be discontinued at least 24 hours before seen in patients taking prolongedaction nitrate
do not chew sustained release tablets. in uncompensated heart failure, myocarditis, IV administration of verapamil. formulations. Evidence suggests that patients
Nursing action: Do not crush sustained release severe myocardial damage; myasthenia gravis; Adverse effects: Constipation; less commonly should have a ‘nitrate-free’ interval to prevent
drug product. acute infections or fever (symptoms may mask nausea, vomiting, flushing, headache, dizzi- the development of tolerance. Adverse effects
• Administer IM injection in deltoid muscle; aspirate hypersensitivity reaction to quinidine); preg- ness, fatigue, ankle oedema; rarely allergic such as flushing, headache, and postural
to avoid intravascular administration. nancy (Appendix 2); breastfeeding (Appendix reactions (erythema, pruritus, urticaria, an- hypotension may limit nitrate therapy but
• Give IV slowly as rapid injection can cause hypo- 3); interactions: Appendix 1. gioedema, Stevens-Johnson syndrome); myal- tolerance to these effects also soon develops.
tension; check IV site regularly for infiltration or Adverse effects: Hypersensitivity reactions, gia, arthralgia, paraesthesia, erythromelalgia; The short-acting sublingual formulation of
extravasation. Keep patient supine for IV admin-
nausea, vomiting, diarrhoea, rashes, ana- increased prolactin concentration; gynaeco- glyceryl trinitrate i is used both for prevention
istration if hypotension occurs.
• Monitor BP, pulse, respiration (observe for respira- phylaxis, purpura, pruritus, urticaria, fever, mastia and gingival hyperplasia on long-term of angina before exercise or other stress and
tory depression). thrombocytopenia, agranulocytosis after treatment; with high doses, hypotension, heart for rapid treatment of chest pain. A sublingual
• Monitor serum electrolytes especially potassium as prolonged treatment, psychosis, angioedema, failure, bradycardia, heart block, and asystole tablet of isosorbide dinitrate is more stable
hypokalaemia predisposes patients to arrhythmias. hepatotoxicity, respiratory difficulties; car- (due to negative inotropic effect). in storage than glyceryl trinitrate and is useful
• Monitor BP closely in the elderly as they may diac effects include myocardial depression, Dose: Supraventricular arrhythmias, by in patients who require nitrates infrequently; it
experience hypotension more readily. heart failure, ventricular arrhythmias and mouth, ADULT 40–120 mg 3 times has a slower onset of action, but effects persist
Dose: Ventricular arrhythmias, by mouth, hypotension; cinchonism including tinnitus, daily. Supraventricular arrhythmias, for several hours.
ADULT up to 50 mg/kg daily in impaired hearing, vertigo, headache, visual by IV injection, ADULT 5–10 mg
divided doses every 3–6 hours, BETA-BLOCKERS
disturbances, abdominal pain, and confusion; over 2 minutes (preferably with ECG
preferably controlled by monitoring lupus erythematosus-like syndrome. monitoring); ELDERLY 5–10 mg over 3 Beta-adrenoceptor antagonists (beta-block-
plasma procainamide concentration Dose: Initial test dose of 200 mg to detect minutes; in paroxysmal tachyarrhyth- ers), such as atenolol, block beta-adrenergic
(therapeutic concentration usually hypersensitivity to quinidine. mias, further 5 mg may be given after receptors in the heart, and thereby decrease
within range 3–10 µg/mL). Arrhythmias, by mouth, ADULT 200– 5–10 minutes if required. heart rate and myocardial contractility and oxy-
Atrial arrhythmias, higher doses may 400 mg 3–4 times daily; increased if gen consumption, particularly during exercise.
POM Verapamil (WMF 12.2)
be required. necessary in supraventricular tach- Beta-blockers are first-line therapy for patients
Tablets, Verapamil HCl 40 mg, 80 mg.
Ventricular arrhythmias, by slow IV ycardia to 600 mg every 2–4 hours Note: Sustained-release (prolonged-release) tablets
with effortinduced chronic stable angina; they
injection, ADULT 100 mg at rate not (maximum 3–4 g daily); frequent ECG are available. A proposal to include such a product in improve exercise tolerance, relieve symptoms,
exceeding 50 mg/minute, with ECG monitoring required. a national list of essential drugs should be supported reduce the severity and frequency of angina
monitoring; may be repeated at by adequate documentation. attacks, and increase the anginal threshold.
POM Quinidine (WMF 12.2)
5-minute intervals until arrhythmia Injection, Verapamil HCl 2.5 mg/mL; in 2-mL am- Beta-blockers should be withdrawn gradually
Tablet, Quinidine (as sulfate) 200 mg.
controlled; maximum 1 g. poule.
Note: Quinidine sulfate 200 mg = quinidine bisul- to avoid precipitating an anginal attack; they
Ventricular arrhythmias, by IV infusion, fate 250 mg. should not be used in patients with underlying
ADULT 500–600 mg over 25–30 min- 5.5 Antianginal drugs coronary vasospasm (Prinzmetal angina). Be-
utes with ECG monitoring, reduced to VERAPAMIL The three main types of angina are: ta-blockers may precipitate asthma and should
maintenance dose of 2–6 mg/minute; Indications: Supraventricular arrhythmias; • stable angina (angina of effort), where ather- not be used in patients with a history of asthma
if further antiarrhythmic treatment by angina (section 5.5). osclerosis restricts blood flow in the coronary or bronchospasm. Some, including atenolol,
mouth required, allow interval of 3–4 Contra-indications: Hypotension, brady-
vessels; attacks are usually caused by exertion and
have less effect on beta2 (bronchial) receptors
hours after infusion. relieved by rest
228 | 5.5 Antianginal drugs 5.5 Antianginal drugs | 229
and are therefore relatively cardioselective. Treatment is similar to that for unstable angina, followed by 50 mg after 12 hours, which contains no wadding. No more than 100
Although the cardio-selective beta-blockers except that a calcium-channel blocker is used then 100 mg daily. tablets should be dispensed at one time, and any
have less effect on airways resistance they are instead of a beta-blocker. unused tablets should be discarded 8 weeks after
POM Atenolol (WMF 12.1) opening the container.
not free of this effect and should be avoided Nursing action: – Antianginals Tablets, Atenolol 50 mg, 100 mg.
in patients with asthma or bronchospasm; • Monitor orthostatic B/P, pulse. Headache, POM Glyceryl Trinitrate (EDL 10.1)
in rare situations where there is no suitable light-headedness, decreased B/P may indicate a POM Atenolol (EDL 10.1) Tablet, (Sublingual), Glyceryl trinitrate 0.5 mg.
need for decreased dosage. Tablets, Atenolol 50 mg, 100 mg.
alternative a cardioselective beta-blocker can POM Glyceryl trinitrate (Kakaki)
• Advise patient to avoid OTC products (unless Injection, Atenolol 0.5 mg per mL; in amp.
be given with extreme caution under specialist Tablet, Glyceryl trinitrate 500 mcg
prescribed by doctor), alcohol, smoking, sodium See preparations under section 5.3.1
supervision. intake and to make position changes slowly to 500 mcg – 100’s
Beta-blockers should not be given to patients prevent fainting. To adhere to non-drug measures Parenteral Nitroglycerine
who have incipient ventricular failure, sec- such as weight control, diet and exerxise. GLYCERYL TRINITRATE
POM MYONIT® (Synergy)
ond – or third-degree AV block, or peripheral Synonym: Nitroglycerine; Nitroglycerol; NTG. Injection, Nitroglycerine 5 mg per mL.
vascular disease. ATENOLOL Indications: Prophylaxis and treatment of Pack: 5 mL; 10 mL (in amps).
Beta-blockers should be used with caution in Indications: Angina and myocardial infarction; angina.
diabetes. Beta-blockers can produce hyper- arrhythmias (section 5.4); hypertension (sec- Contraindications: Hypersensitivity to ni- ISOSORBIDE DINITRATE
glycaemia or they can enhance the hypogly- tion 5.3); migraine prophylaxis (section 1.9.2). trates; hypotension; hypovolaemia; hyper- Synonym: ISD; ISDN.
caemic effect of insulin and may precipitate Contra-indications: History of asthma or bron- trophic obstructive cardiomyopathy, aortic Indications: Prophylaxis and treatment of
hypoglycaemia. chospasm (unless no alternative, then with stenosis, cardiac tamponade, constrictive peri- angina; heart failure (section 5.1).
extreme caution and under specialist super- carditis, mitral stenosis; marked anaemia; head Contra-indications: Hypersensitivity to
CALCIUM-CHANNEL BLOCKERS vision); uncontrolled heart failure, Prinzmetal trauma; cerebral haemorrhage; angle-closure nitrates; hypotension; hypovolaemia; hyper-
A long-acting dihydropyridine calcium channel angina, marked bradycardia, hypotension, sick glaucoma.
EMDEX
trophic obstructive cardiomyopathy, aortic
blocker (such as amlodipine, section 5.3) can sinus syndrome, second – and third-degree AV Precautions: Severe hepatic or renal impair- stenosis, cardiac tamponade, constrictive peri-
be added to betablocker treatment if necessary block, cardiogenic shock; metabolic acidosis; ment; hypothyroidism; malnutrition; hypother- carditis, mitral stenosis; marked anaemia; head
for control of moderate stable angina. For severe peripheral arterial disease; phaeochro- mia; recent history of myocardial infarction; trauma; cerebral haemorrhage; angle-closure
those in whom a beta-blocker is inappropriate, mocytoma (unless used with alpha-blocker). interactions: Appendix 1. glaucoma.
verapamil may be given as an alternative to Precautions: Avoid abrupt withdrawal espe- Adverse effects: Throbbing headache; flush- Precautions: Severe hepatic or renal impair-
treat stable angina. Calcium-channel blockers cially in ischaemic heart disease; history of ing; dizziness, postural hypotension; tachycar- ment; hypothyroidism; malnutrition; hypother-
interfere with the inward movement of cal- obstructive airways disease (use with caution dia (paradoxical bradycardia also reported). mia; recent history of myocardial infarction;
cium ions through the slow channels in heart and monitor lung function—see also Con- Advice to patients: Notify physician if no relief interactions: Appendix 1.
and vascular smooth muscle cell membranes, tra-indications above); pregnancy (Appendix after 3 sublingual doses; do not swallow or
leading to relaxation of vascular smooth mus- 2); breastfeeding (Appendix 3); first-degree chew sublingual form; do not change brands TOLERANCE: Patients taking isosorbide dini-
cle. Myocardial contractility may be reduced, AV block; liver function deteriorates in portal without notifying your physician or pharmacist; trate for the long-term management of angina
the formation and propagation of electrical hypertension; reduce dose in renal impairment take oral nitrate on an empty stomach with a may often develop tolerance to the antiangi-
impulses within the heart may be depressed (Appendix 4); diabetes mellitus (small decrease full glass of water. nal effect; this can be avoided by giving the
and coronary or systemic vascular tone may in glucose tolerance, masking of symptoms of Nursing action: Teach paient to take sublin- second of 2 daily doses of longer-acting oral
be diminished. Calcium-channel blockers are hypoglycaemia); history of hypersensitivity gual tablet at first sign of attack. He should presentations after an 8-hour rather than a
used to improve exercise tolerance in patients [increased reaction to allergens, also reduced wet the tablet with saliva, place it under the 12-hour interval, thus ensuring a nitrate-free
with chronic stable angina due to coronary ath- response to epinephrine (adrenaline)]; myas- tongue until completely absorbed, and sit interval each day.
erosclerosis or with abnormally small coronary thenia gravis; interactions: Appendix 1. down and rest. Adverse effects: Throbbing headache; flush-
arteries and limited vasodilator reserve. Adverse effects: GI disturbances (nausea, • 8 – to 12-hour nitrate-free interval is needed each ing; dizziness, postural hypotension; tachycar-
vomiting, diarrhoea, constipation, abdominal day to prevent tolerance. dia (paradoxical bradycardia also reported).
Calcium-channel blockers can also be used in • Advise patient to report to the physician if symp- Advice to patients: Do not chew or crush sub-
patients with unstable angina with a vasos- cramp); fatigue; cold hands and feet; exacerba-
toms are not relieved 15 minutes after taking lingual or sustained release dosage form; notify
pastic origin, such as Prinzmetal angina, and tion of intermittent claudication and Raynaud
sublingual dosage form; also to take drug before physician if no relief from sublingual tablets
in patients in whom alterations in cardiac tone phenomenon; bronchospasm; bradycardia, stressful activities such as exercise, sexual activities.
heart failure, conduction disorders, hypoten- after 15 minutes; do not change brands with-
may influence the angina threshold. • Tell patient to avoid hazardous activities if dizziness
out consulting your pharmacist or physician.
sion; sleep disturbances, including nightmares; occurs and to make position changes slowly to
Unstable angina depression, confusion; hypoglycaemia or Nursing action: Administer oral form with
prevent fainting.
Unstable angina requires prompt aggressive hyperglycaemia; exacerbation of psoriasis; rare • Instruct patient to avoid alcohol as it may cause plenty of water on an empty stomach, either
treatment to prevent progression to myocar- reports of rashes and dry eyes (oculomucocu- increased hypotension. 30 min before or 1 to 2 hours after meals;
dial infarction. taneous syndrome—reversible on withdrawal). • Drug may cause headche which can be relieved oral tablet should be swallowed whole while
Dose: Angina, by mouth, ADULT 50 mg once with aspirin or paracetamol. chewable tablet should be chewed thoroughly
Initial treatment is with acetylsalicylic acid Dose: Angina, sublingually, ADULT 0.5–1 mg,
daily, increased if necessary to 50 mg before swallowing.
to inhibit platelet aggregation, followed by repeated as required. • 8 – to 12-hour nitrate-free interval is needed each
heparin. Nitrates and beta-blockers are given to twice daily or 100 mg once daily.
day to prevent tolerance.
relieve ischaemia; if beta-blockers are contrain- Myocardial infarction (early interven- POM Glyceryl trinitrate (WMF 12.1) • Ensure that patient does not confuse sublingual
dicated, verapamil is an alternative, provided tion within 12 hours), by IV injection Sublingual tablet, Glyceryl trinitrate 500 µg. with oral form.
over 5 minutes, ADULT 5 mg, then Note: Glyceryl trinitrate tablets are unstable. They
left ventricular function is adequate. • Headache can be relieved with aspirin or paraceta-
by mouth 50 mg after 15 minutes, should therefore be dispensed in glass or stainless mol; advise patient to take drug before stressful
Prinzmetal angina steel containers, and closed with a foil-lined cap
230 | 5.6 Antithrombotic drugs and myocardial infarction 5.6 Antithrombotic drugs and myocardial infarction | 231
activities; also not to discontinue drug abruptly to Dose: Angina, by mouth, ADULT 80–120 Early administration of beta-blockers such as as warfarin (section 6.2). Treatment of acute is-
prevent vasospasm, and to make position changes mg 3 times daily (120 mg 3 times atenolol (section 5.5) have been shown to reduce chaemic stroke includes use of acetylsalicylic
slowly to prevent fainting. daily usually required in Prinzmetal both early mortality and the recurrence rate of acid 150–300 mg as a single dose given within
• Advise patient to avoid alcohol; to avoid hazardous angina). myocardial infarction; initial intravenous admin- 48 hours of onset, and, in selected patients,
activities since dizziness or orthostatic hypotension
POM Verapamil (WMF 12.1)
istration is followed by long-term oral treatment anticoagulants such as heparin. Long-term
may occur.
Tablets, Verapamil HCl 40 mg, 80 mg. (unless the patient has contraindications). therapy with acetylsalicylic acid 75–150 mg
Dose: Angina (acute attack), sublingually,
Note: Sustained-release (prolonged-release) tablets ACE inhibitors (section 5.1) have also been daily reduces the risk of having another stroke.
ADULT 2.5–10 mg, repeated as
required. are available. A proposal to include such a product in shown to be beneficial in initial management Antiplatelet drugs are not used in the manage-
a national list of essential drugs should be supported (unless patient has contra-indications) when ment of haemorrhagic stroke, because they can
Angina prophylaxis, by mouth, ADULT
by adequate documentation.
20–240 mg daily in divided doses (see given within 24 hours, and if possible contin- exacerbate bleeding. Treatments include careful
advice on Tolerance above). See preparations under section 5.3.7 ued for at least 5–6 weeks. lowering of very high blood pressure and surgery
If arrhythmias occur, they should be treated ag- where appropriate.
POM Isosorbide dinitrate (WMF 12.1)
5.6 Antithrombotic drugs and gressively, but the likelihood decreases rapidly Acetylsalicylic acid is normally given for at least
Sublingual tablet, Isosorbide dinitrate 5 mg.
myocardial infarction over the first 24 hours after infarction. Ventricu- one year after coronary artery bypass surgery.
POM Isosorbide Dinitrate (EDL 10.1)
Anticoagulants prevent thrombus formation lar fibrillation should be treated immediately It is also given to patients with prosthetic
Tablet, Isosorbide dinitrate 10 mg.
Tablet, (Sublingual), Isosorbide dinitrate 5 mg.
or the extension of an existing thrombus. For with a defibrillator; if this is ineffective alone, heart valves who have had cerebral embolism
further details see section 6.2 (drugs affecting the antiarrhythmic drug lidocaine (section 5.4) despite warfarin treatment.
POM APO-ISDN® (Lahams) coagulation). should be given.
Tablet, Isosorbide dinitrate 10 mg; white,
Antiplatelet drugs also help to inhibit thrombus All patients should be closely monitored for ACETYLSALICYLIC ACID
scored bevel-edged tab. marked ‘APO 10’.
10 mg – 1000. formation by decreasing platelet aggregation. hyperglycaemia; those with diabetes mellitus Indications: Prophylaxis of cerebrovascular
EMDEX
Thrombolytics (fibrinolytics) such as strep- or raised blood-glucose concn should receive disease or MI; pyrexia, pain, inflammation
POM ISOBID® (Hovid)
tokinase are used to break up thrombi; they insulin. (section 1.8.1); migraine (section 1.9.1).
Tablet, Isosorbide dinitrate 10 mg.
10 mg – 1000. are used to treat acute myocardial infarction, Contra-indications: Hypersensitivity (includ-
Long-term management
extensive deep vein thrombosis, major pulmo- ing asthma, angioedema, urticaria or rhinitis)
POM MONOCONTIN OD® (Phillips) Acetylsalicylic acid should be given to all pa- to acetylsalicylic acid or any other NSAID;
Tablet, Isosorbide mononitrate 50 mg; pink f-c tab. nary embolism and acute arterial occlusion.
tients in a dose of 75–150 mg daily by mouth, children and adolescents under 16 years (Reye
marked ‘MM’. Myocardial infarction unless it is contraindicated. The prolonged syndrome, see section 1.8.1); active peptic
Management of myocardial infarction includes antiplatelet effect has been shown to reduce ulceration; haemophilia and other bleeding
VERAPAMIL the rate of reinfarction.
two phases: disorders.
Indications: Angina, including stable, unsta- • initial management of the acute attack Precautions: Asthma; uncontrolled hyperten-
Treatment with beta-blockers should be con-
ble, and Prinzmetal; arrhythmias (section 5.4). • long-term management, including prevention of sion; pregnancy (Appendix 2); breast-feeding
tinued for at least 2–3 years. Verapamil is some-
Contra-indications: Hypotension, brady- further attacks. (Appendix 3); see also section 1.8.1; interac-
times useful if a beta-blocker cannot be used.
cardia, second – and third-degree AV block, Initial management tions: Appendix 1.
sinoatrial block, sick sinus syndrome; car- ACE inhibitors such as enalapril (section 5.1)
Oxygen (section 3.1.3) should be given to all Advice to Patients: To be be taken whole once
diogenic shock; history of heart failure or should also be used since they reduce mortal-
patients, except those with severe chronic daily, with a full glass of water. Do not lie down
significantly impaired left ventricular function ity, particularly in patients with left ventricular
obstructive pulmonary disease. for 15-30 minutes after taking the drug. Do not
(even if controlled by therapy); atrial flutter or dysfunction.
halve, break or chew the tablet. Wait for 2 hours
fibrillation complicating Wolff-Parkinson-White Pain and anxiety are relieved by slow intrave- Nitrates (section 5.5) may be required for between taking the drug and taking an antacid
syndrome; porphyria. nous injection of an opioid analgesic such as patients with angina. for heartburn. Do not keep the medicine in
Precautions: First-degree AV block; acute morphine (section 1.8.2). Metoclopramide your mouth for more than the time required for
The use of statins (section 5.7) may also
phase of myocardial infarction (avoid if brad- (section 4.6) may also be given by intramuscu- swallowing. Do not exceed the recommended
be considered in patients with high risk of
ycardia, hypotension, left ventricular failure); lar injection to prevent and treat nausea and dosage. If you have forgotten to take a dose
recurrence.
hepatic impairment (Appendix 5); children vomiting caused by morphine. at the specified time, take it as soon as you
(specialist advice only); pregnancy (Appendix Stroke
Acetylsalicylic acid 150–300 mg by mouth remember but never take two doses together.
2); breastfeeding (Appendix 3); avoid grapefruit (preferably chewed or dispersed in water) is Stroke (cerebrovascular accident) may be Adverse effects: Bronchospasm; gastro-intes-
juice; interactions: Appendix 1. given immediately for its antiplatelet effect. ischaemic or haemorrhagic; precise diagnosis tinal haemorrhage (rarely major), also other
Adverse effects: Constipation; less commonly is essential, as management for the two types haemorrhage (for example sub-conjunctival);
nausea, vomiting, flushing, headache, dizzi- Thrombolytic drugs such as streptokinase
of stroke is quite different. see also section 1.8.1.
ness, fatigue, ankle oedema; rarely allergic help to restore perfusion and thus relieve
myocardial ischaemia; they should ideally be Primary prevention of both types of stroke Dose: Prophylaxis of cerebrovascular disease
reactions (erythema, pruritus, urticaria, an- or myocardial infarction, by mouth,
given within 1 hour of infarction (use after 12 includes reduction of high blood pressure,
gioedema, Stevens-Johnson syndrome); myal- ADULT 75–100 mg daily.
hours requires specialist advice). Antibodies stopping smoking, weight reduction, and
gia, arthralgia, paraesthesia, erythromelalgia;
to streptokinase appear 4 days after use and cholesterol reduction. Atrial fibrillation, acute POM Acetylsalicylic acid (WMF 12.5)
increased prolactin concentration; gynaeco-
streptokinase should not be given to the pa- myocardial infarction, and valvular disease Tablet, Acetylsalicylic acid 100 mg.
mastia and gingival hyperplasia on long-term
tient again after this time. may produce embolism and ischaemic stroke.
treatment; with high doses, hypotension, heart POM Acetylsalicylic acid (EDL 16.2)
Prophylaxis in patients at risk of ischaemic
failure, bradycardia, heart block, and asystole Nitrates (section 5.5) may also be given to Tablet, Acetylsalicylic acid 75 mg.
stroke includes antiplatelet drugs such as
(due to negative inotropic effect). relieve ischaemic pain. OTC ASACARD® (Hochiez)
acetylsalicylic acid or oral anticoagulants such
232 | 5.6 Antithrombotic drugs and myocardial infarction 5.6 Antithrombotic drugs and myocardial infarction | 233
Tablet, Acetylsalicylic 75 mg. medically treated patients eligible for thrombo- MI or Non-STEMI), initially 300 mg as bleeding; haemorrhagic stroke, history of
75 mg – 28’s; 100’s. lytic therapy. Prevention of atherothrombotic a loading dose, followed by 75 mg cerebrovascular disease (especially recent or if
OTC ASPIRIN® Cardio (Bayer Schering) and thromboembolic events (including stroke) once daily; give in combination with residual disability); coma; severe hypertension;
Tablet, Acetylsalicylic acid 100 mg; e-c tab. in adult patients with atrial fibrillation who have ASA 75-325 mg qDay. coagulation defects; bleeding diatheses, aortic
100 mg – 3 x 10’s at least one risk factor for vascular events, are not Treatment of ST segment elevation ACS dissection; risk of GI bleeding such as recent
OTC MICROPIRIN® (Pemason)
suitable for treatment with Vitamin K antagonists (STEMI), initially 300 mg as a loading history of peptic ulcer, oesophageal varices,
Caplet, Acetylsalicylic acid 75 mg; e-c caplet. (VKA) and who have a low bleeding risk; given in dose (in patients ≤75 years), then 75 ulcerative colitis; acute pancreatitis; severe
combination with ASA. mg once daily in combination with liver disease; acute pulmonary disease with
POM VASOPRIN® (Juhel) Contra-indications: Hypersensitivity to clopi- ASA 75-325 mg qDay; with or without cavitation; previous allergic reactions.
Tablet, Acetylsalicylic acid 75 mg.
dogrel or excipients; severe hepatic impairment; thrombolytics. Loading dose not rec- Precautions: Risk of bleeding from any inva-
Pack: 30’s; 100’s; 500’s.
active pathological bleeding such as peptic ul- ommended in patients >75 years. sive procedure, including injection; external
See also under section 1.8.1 for the preparations cer or intracranial haemorrhage. Avoid use dur- Prevention of thromboembolic events chest compression; pregnancy (Appendix 2);
ing the first 7 days after acute ischaemic stroke. patients with AF, 75 mg once daily in abdominal aneurysm or where thrombolysis
CLOPIDOGREL Precautions: Clopidogrel alone or in combi- combination with ASA. may give rise to embolic complications such
Therapeutic category: Antiplatelet agent nation with ASA may increase risk of bleeding (Additional information sourced from Plavix monograph avail- as enlarged left atrium with atrial fibrillation
Pharmacology: Clopidogrel is a prodrug, one (monitor patient for bleeding or unusual able from: http://www.medicines.org.uk/EMC/medicine/24207/ (risk of dissolution of clot and subsequent
bruising). May prolong bleeding time in SPC/Plavix+75mg+tablets/) embolization); diabetic retinopathy (small risk
of whose metabolites is an inhibitor of platelet
aggregation. Clopidogrel must be metabolised trauma patients or those undergoing surgery of retinal haemorrhage); recent or concurrent
POM CLOPACIN® (Oculus)
by CYP450 enzymes to produce the active (discontinue Clopidogrel 5 days prior to sur- anticoagulant treatment.
Tablet, Clopidogrel 75 mg; f-c tab.
metabolite that inhibits platelet aggregation. gery). Discontinuing therapy prematurely may 75 mg – 14’s; 28’s; 30’s; 50’s; 84’s; 90’s; 100’s (in Adverse effects: N & V; bleeding, usually lim-
The active metabolite of clopidogrel selectively increase risk of cardiovascular events. Avoid blisters) ited to site of injection but internal bleeding
EMDEX
inhibits the binding of adenosine diphosphate coadministration with inhibitors of CYP2C19 including intracranial haemorrhage may occur
POM INSTACLOP® (Ranbaxy)
(ADP) to its platelet P2Y12 receptor and the sub- (see Interactions). Hepatic and renal dysfunc- (if serious bleeding occurs, discontinue infu-
Tablet, Clopidogrel 75 mg
sequent ADP-mediated activation of the glyco- tion. Pregnancy and lactation. 75 mg – 3 x 10’s
sion—coagulation factors may be required);
protein GPIIb/IIIa complex, thereby inhibiting Interactions: Co-administration with ASA, hep- hypotension, arrhythmias (particularly in my-
arin, glycoprotein IIb/IIIa inhibitors or non-ste- POM JOVEX® (Joswe/Afrab) ocardial infarction); allergic reactions including
platelet aggregation. Due to the irreversible Tablet, Clopidogel 75 mg.
binding, platelets exposed are affected for the roidal anti-inflammatory drugs (NSAIDs) in- rash, flushing, uveitis, anaphylaxis; fever, chills,
cluding Cox-2 inhibitors may increase bleeding 75 mg – 30’s back or abdominal pain; Guillain-Barré syn-
remainder of their lifespan (approximately 7-10
days) and recovery of normal platelet function risk. Monitor patient carefully for any signs POM NOPLAT® (Nomedi) drome reported rarely.
occurs at a rate consistent with platelet turno- of bleeding including occult bleeding. Avoid Tablet, Clopidogrel (as bisulfate) 75 mg; f-c tab Dose: Thrombosis, by IV infusion, ADULT 250
ver. Platelet aggregation induced by agonists use with oral anticoagulants. Clopidogrel is POM PIDOGREL®(Zolon) 000 units over 30 minutes, followed
other than ADP is also inhibited by blocking metabolized to its active metabolite mainly Tablet, Clopidogrel (as bisulfate) 75 mg; f-c tab. by 100 000 units every hour for 12–72
the amplification of platelet activation by by CYP2C19 and inhibition of this hepatic 75 mg – 3 x 10’s hours according to condition with
released ADP. It is rapidly absorbed following enzyme may reduce its efficacy. Inhibitors of monitoring of clotting parameters.
POM PLAGERINE® (Micronova)
oral dosing. The mean peak plasma levels of un- CYP2C19 include omeprazole and esomeprazole, Myocardial infarction, by IV infu-
Tablet, Clopidogrel bisulfate 75 mg; f-c tab.
changed Clopidogrel occured approx. 45 mins fluvoxamine, fluoxetine, moclobemide, voricona- 75 mg – 30’s sion, ADULT 1 500 000 units over 60
after dosing. Undergoes extensive hepatic zole, fluconazole, ticlopidine, ciprofloxacin, minutes.
cimetidine, carbamazepine, oxcarbazepine and POM RIDLOR® (Mega lifesciences)
metabolism via multiple enzyme pathways. Tablet, Clopidogrel (as bisulphate) 75 mg; f-c tab POM Streptokinase (WMF 12.5)
Effectiveness of Clopidogrel is dependent on chloramphenicol. Proton Pump Inhibitors (PPIs) Injection, (Powder for injection), Streptokinase 1.5
75 mg – 3 x 10’s
conversion to an active thiol metabolite by namely omeprazole and esomeprazole which million IU in vial.
the CYP450 system, mainly the CYP2C19. It is are also inhibitors of CYP2C19 may reduce
CLOPIDOGREL plus ASPIRIN POM DICLAIR-ST® (Mark)
excreted in urine and faeces; has a half-life of the effectiveness of Clopidogrel. Pantoprazole
Injections, Streptokinase 750,000 IU, 1,500,000 IU;
approx. 6 hours. and lansoprazole appear to have less effect on POM ASAGREL® (Zolon) sterile, lyophillized white powder for injection in vials
clopidogrel metabolism. Tablet, Clopidogrel 75 mg, aspirin 75 mg
Indications: Prevention of atherothrombotic Reconstitution and dilution:
Adverse effects: GI bleeding, diarrhoea, nau- Pack: 3 x 10’s • Add 5 mL normal saline or 5% dextrose solution slowly to
events (e.g., MI, stroke, vascular death) in adult
sea, dyspepsia, abdominal pain; headache, the vacuum packed vial, directing the needle point to the
patients suffering from a recent myocardial POM CLOSPRIN® (Teta)
wall of the vial. Abolish residual vacuum by briefly loosening
infarction (from a few days until less than 35 fatigue, dizziness; bruising, rash, pruritus, skin Tablet, Clopidogrel (as bisulfate) 75 mg, Acetylsali- the needle from the syringe.
days), ischaemic stroke (from 7 days until less bleeding (purpura); epistaxis, arthralgia, hae- cylic acid 75 mg; e-c tab. • Tilt and roll the vial gently-avoid shaking-until reconsti-
matoma, haematuria, flu-like symptoms. Rarely Pack: 10’s tution is complete.
than 6 months) or established peripheral arterial • Once the powder is completely dissolved, transfer the con-
disease. Treatment of acute coronary syndrome in neutropaenia, serious haemorrhage, serum tent of the vial into 45 mL of normal saline or 5 % dextrose
sickness, anaphylactoid reaction. STREPTOKINASE
adult patients suffering from non-ST segment el- solution and infuse over 60 minutes.
evation ACS (unstable angina or non-Q-wave MI), Dose: Adult and elderly, by mouth: Indications: Life-threatening deep-vein • Because Diclair contains no preservatives, it should be re-
Prevention of thromboembolic events thrombosis, pulmonary embolism, acute ar- constituted immediately before use. However, the solution
including patients undergoing a stent placement may be used, for direct intravenous administration, within
following percutaneous coronary intervention, (MI, CVA, PVD) in patients with recent terial thromboembolism; acute MI. eight hours following reconstitution if stored at 2-7OC.
in combination with acetylsalicylic acid (ASA). MI, stroke or established peripheral Contra-indications: Repeat use of strepto- • Do not add any other medication to the container of Diclair.
Treatment of ACS in patients with ST segment arterial disease, 75 mg once daily kinase beyond 4 days of first administration; POM DURAKINASE® (Alpha)
elevation acute MI, in combination with ASA in Treatment of Non-ST segment elevation recent haemorrhage, surgery (including Injection, Streptokinase 1.5 million IU; off-white
ACS (unstable angina or non-Q-wave dental), parturition, trauma; heavy vaginal
234 | 5.7 Lipid-regulating drugs 5.7 Lipid-regulating drugs | 235
lyophilied powder in a vial. of day of drug administration. pain, tenderness, or weakness. density Lipoprotein (LDL). It also increases high
Pack: 1’s Indications: Hypercholesterolaemia – As an Dose: By mouth, initially 10 mg once daily; density Lipoprotein (HDL). Clofibrate is readily
adjunct to diet for reduction of elevated total-C, may be increased up to a max. 80 absorbed following oral dosage and is hydro-
5.7 Lipid-regulating drugs LDL-C, apolipoprotein B, and TG in adults with mg once daily depending on goal of lysed to the active acid. The plasma half-life is
The primary aim of therapy is to reduce pro- primary hypercholesterolaemia, including therapy and patient response. approximately 16 hours (which may increase
gression of atherosclerosis and to improve familial hypercholesterolaemia or combined Note: To be given as a single dose at any time to 60-190 hours in renal failure) and the drug
(mixed) hyperlipidaemia when response to diet of the day, with or without food. Adjustment of is excreted via the kidneys. Some 91 – 97% is
survival in patients with established CVD,
and other nonpharmacological measures is inad- dosage should be made at intervals of 4 weeks or bound to serum albumin, and may displace
to reduce premature cardiac morbidity and more. The patient should be placed on a standard
mortality in people at high risk of CV events equate; to reduce total-C and LDL-C in adults with other similarly bound drugs. The volume of
cholesterol-lowering diet before and during during
and to prevent pancreatitis due to hyper-tri- homozygous familial hypercholesterolaemia as treatment.
distribution is 5-9 litres; non enters the CSF.
glyceridaemia. Beta-hydroxy-beta-methyl- an adjunct to other lipid-lowering treatments; it Concimitant administration of cholestyramine
also raises HDL-C and lowers the LDL/HDL and POM LIPITOR® (Pfizer) does not impair absorption of Clofibrate.
glutaryl-coenzyme A (HMG Co A) reductase
total cholesterol/HDL ratios. Prevention of CVD Tablets, Atorvastatin calcium 10 mg, 20 mg; white, Indications: Management of severe hyper-
inhibitors, often referred to as ‘statins’, are elliptical, f-c tabs.
potent and effective lipid-lowering drugs with in patients estimated to have a high risk for a first lipo-proteinaemia when diet alone has failed;
10 mg – 30’s (in blister)
a good tolerability profile. Examples of these cardiovascular event, as an adjunct to correction 20 mg – 30’s (in blister) exudative diabetic retinopathy and the hyper-li-
drugs include simvastatin, pravastatin, lovas- of other risk factors. poproteinaemia accompanying diabetes; xan-
Contra-indications: Hypersensitivity to any POM ATORVAST® (Joswe/Afrab) thomata associated with hyper-lipoproteinamia;
tatin, fluvastatin, and atorvastatin. Statins
component of this medication, active liver Tablets, Atorvastatin 10 mg, 20 mg, 40 mg. chronic hyperfibrinogenaemia associated with
have been shown to reduce the incidence of 10 mg – 30’s.
fatal and non-fatal MI, stroke and mortality disease or unexplained persistent elevations occlusive vascular disease.
20 mg – 30’s.
(all causes), as well as the need for coronary of serum transaminases exceeding 3 times 40 mg – 30’s. Contra-indications: Acute impairment of
bypass surgery. They are recommended for the upper limit of normal, myopathy, during renal, bilary or hepatic function; patients with
EMDEX
pregnancy, while breast-feeding. POM ATROLIP® (Geneith) a history of, or existing, gall bladder disease or
1o and 2o prevention of atherosclerotic CVD in Tablets, Atorvastatin (as Ca2+) 10 mg, 20 mg.
high-risk patients. Precautions: With any statin, patients should stones (it may increase the lithogenicity of bile
10 mg – 10 x 10’s
promptly report muscle pain, tenderness, or 20 mg – 10 x 10’s
and raise the frequency of gallstone formation);
ATORVASTATIN weakness. Discontinue drug if myopathy is pregnancy and breast feeding.
suspected, if creatinine phosphokinase (CPK) POM AVSTAT®-10 (Fidson) Precautions: Myopathy. In patients with low
Pharmacology: Atorvastatin is a selective, Tablet, Atorvastatin (as Ca) 10 mg; f-c tab.
competitive inhibitor of HMG-CoA reductase, levels rise markedly, or if the patient has risk serum albumin levels, for example those with
10 mg – 3 x 10’s.
the rate-limiting enzyme that converts 3-hy- factors for rhabdomyolysis. Perform liver nephrotic syndrome, high levels of unbound
droxy-3-methylglutaryl-coenzyme A to me- function tests before the initiation of treat- POM ATORSTAT® (PharmacyPlus) clofibrate may give rise to myalgia and raised
ment, at 12 weeks after initiation of therapy Tablet,s Atorvastatin calcium 10 mg, 20 mg serum creatinine kinase levels. Renal impair-
valonate, a precursor of sterols, including cho-
or elevation of dose and periodically (eg six 10 mg – 10’s ment; Children.
lesterol. Pharmacologic inhibition of HMG-CoA 20 mg – 10’s
reductase blocks the synthesis of endogenous monthly) thereafter. Interactions: Anticoagulants (halve the dose
cholesterol in the liver, causing a compensatory Interactions: Atorvastatin is metabolized by POM CHOVASTIN® (Korlyns) of the anticoagulant when administered
CYP 3A4. Coadministration with CYP 3A4 in- Tablets, Atorvastatin calcium 10 mg, 20 mg; f-c tabs. concomitantly). Clofibrate may displace other
increase in the activity of hepatic LDL receptors
leading to enhanced clearance of LDL-choles- hibitors (e.g. ciclosporin, macrolide antibiotics POM LIPIVASTIN® (Neros) acidic drugs such as phenytoin or sulphony-
terol from the blood. These two mechanisms including erythromycin and clarithromycin, Tablets, Artovastatin (as calcium) 10 mg, 20 mg; lureas e.g. tolbutamine, from protein binding
lead to reduction in circulating LDL-C and total nefazodone, azole antifungals including itra- f-c tabs. sites and thereby potentiate the effect of such
cholesterol. Atorvastatin is rapidly absorbed conazole, Grapefruit juice and HIV protease 10 mg – 3 x 10’s (in blister) drugs. The risk of serious muscle toxicity is
inhibitors) can lead to increased plasma levels 20 mg – 3 x 10’s (in blister) increased with combinations such as Fibrates
after oral administration; maximum plasma
concentrations occur within 1 to 2 hours. Ex- of atorvastatin and increased risk of myopathy. POM STORVAS® (Ranbaxy) + Statins or Fibrates + Fibrates.
tent of absorption increases in proportion to Diltiazem may cause increase in exposure to Caplets, Atorvastatin calcium 10 mg, 20 mg; white Adverse effects: Transient slight abdominal
atorvastatin dose. The absolute bioavailability atorvastatin. Ezetimibe, Fibrates (especially f-c caplet. discomfort, nausea and looseness of the bow-
of atorvastatin (parent drug) is approx. 14% gemfibrozil) may increase risk of myopathy. 10 mg – 3 x 10’s. els, and impotence, headache, drowsiness, skin
Inducers of CYP 3A4 (eg efavirenz, rifampin, 20 mg – 3 x 10’s. rashes, pruritus; rarely cardiac arrhythmias and
and the systemic availability of HMG-CoA
reductase inhibitory activity is approximately St. John’s Wort) may cause reduced plasma POM TULIP® (Taylek) myositis-like syndrome comprising myalgia,
30%. The low systemic availability is attributed concentrations of atorvastatin. Antacids con- Tablets, Atorvastatin (as calcium salt) 10 mg, 20 mg, myopathy, muscle cramps and sometimes
to presystemic clearance in GI mucosa and/or taining magnesium and aluminium hydroxides; 40 mg, 80 mg; f-c tabs. rhabdomyolysis.
hepatic first-pass metabolism. Although food Warfarin; Fusidic Acid. 10 mg – 3 x10’s (in blisters) Advice to patients: If GI upset occurs, may be
Adverse effects: Abdominal pain, dyspepsia, 20 – 3 x10’s (in blisters) taken with food; notify physician of chest pain,
decreases the rate and extent of drug absorp- 40 mg – 3 x10’s (in blisters)
tion by approx. 25% and 9%, respectively, as nausea, flatulence, constipation, diarrhoea; shortness of breath, irregular heart beat, severe
80 mg – 3 x10’s (in blisters)
assessed by Cmax and AUC, LDL-C reduction Headache; Asthenia; Insomnia; Arthralgia, pain stomach pain with nausea and vomiting, per-
is similar whether atorvastatin is given with in extremity, musculoskeletal pain, muscle sistent fever, sore throat, or unusual bleeding
CLOFIBRATE
or without food. Plasma atorvastatin concen- spasms, myalgia, joint swelling; Nasopharyn- or bruising; adhere to prescribed diet.
gitis; Hyperglycemia; Pharyngolaryngeal pain, Therapeutic category: Antilipemic Agent; Dose: Adult (including the elderly), by
trations are lower (approx. 30% for Cmax and
epistaxis. Liver function test abnormal; blood Fibrate. mouth, 20-30 mg/kg b.wt daily in
AUC) following evening drug administration
creatine phosphokinase increased. Pharmacology: Clofibrate lowers serum 2 or 3 divided doses after meals as
compared with morning. However, LDL-C
Advice to patients: Avoid taking grapefruit cholesterol and triglyceride levels by reducing follows: Over 65 kg, 2 g daily; 50-65
reduction is the same regardless of the time
juice; report promptly any unexplained muscle very low density lipoprotein (VLDL) and low kg, 1.5 g daily; Child: not usually
236 | 5.7 Lipid-regulating drugs 5.7 Lipid-regulating drugs | 237
recommended for children but where cholesterol. Fluvastatin exerts its main effect a dosge change; lipid lowering effects are additive of hereditary muscular disorders; history of
necessary, by mouth 20-30 mg/kg in the liver, which is also the main organ for when fluvastatin is combined with a bile acid bind- muscular toxicity with another HMG-CoA
b.wt. its metabolism. The inhibition of cholesterol ing resin or niacin, however, it must be administered reductase inhibitor or fibrate; alcohol abuse;
Note: Clofibrate should not be used until diet alone biosynthesis reduces the cholesterol in heat least 2 hours following these drugs. Asian patients; concomitant use of fibrates.
has failed and should be given together with an patic cells, which stimulates the synthesis of POM LESCOL® (Novartis) Precautions: Perform LFTs before and at 12
appropriate diet. Patient’s adherence and response low density lipoprotein (LDL) receptors and Capsules, Fluvastatin 20 mg, 40 mg. weeks following both the initiation of therapy
to treatment should be monitored regularly and in
thereby increases the uptake of LDL particles. and any elevation of dose, and periodically
some patients, it may take several months before a ROSUVASTATIN
reduction in blood cholesterol is seen. If, however,
The ultimate result of these mechanisms is a (e.g. semiannually) thereafter; discontinue if
an adequate response has not been observed after reduction of the plasma cholesterol concen- Therapeutic category: Antilipemic Agent; serum transaminase level exceeds 3 x ULN.
3 months, Clofibrate should be discontinued. tration. Fluvastatin is absorbed rapidly and HMG-CoA Reductase Inhibitor. Substantial alcohol consumption and/or
completely (98%) after oral administration to Pharmacology: Rosuvastatin is a synthetic have a history of liver disease. Patients with
POM ATROMID-S® (Reals)
fasted volunteers. In a fed state, the drug is lipid-lowering agent. It is a selective and competi- predisposing factors for myopathy e.g. renal
Capsule, Clofibrate 500 mg; red cap.
absorbed at a reduced rate. More than 98% tive inhibitor of HMG-CoA reductase, the rate-lim- impairment, advanced age, and inadequately
FENOFIBRATE of the circulating drug is bound to plasma iting enzyme that converts 3-hydroxy-3-methyl- treated hypothyroidism. Advise patient to
proteins, and this binding is unaffected by glutaryl coenzyme A to mevalonate, a precursor report unexplained muscle pain, tenderness
Therapeutic category: Antilipemic Agent;
drug concentration. Food does not affect its for cholesterol. The primary site of action of or weakness, particularly if accompanied by
Fibrate.
absorption and its plasma concentration is rosuvastatin is the liver, the target organ for malaise or fever. Increased risk of myopathy
Indications: Hypercholesterolaemia and
neither affected by age nor gender. Hepatic cholesterol lowering. Rosuvastatin increases with concomitant use of ciclosporin or other
hypertri-glyceridaemia alone or combined in
insufficiency can cause accumulation of the the number of hepatic LDL receptors on the lipid-lowering agents e.g. fibrates (avoid use
patients unresponsive to dietary and other
drug since it is metabolised in the liver and cell-surface, enhancing uptake and catabolism of with Gemfibrozil), niacin. Proteinuria predictive
non-drug therapeutic measures (e.g. weight
eliminated primarily via the biliary route. LDL and it inhibits the hepatic synthesis of VLDL, of active or progressive liver disease (monitor
EMDEX
reduction or increased physical activity), par-
Indications: Primary hypercholesterolaemia in thereby reducing the total number of VLDL and renal function routinely).
ticularly when there is evidence of associated
patients who do not respond to dietary control. LDL particles. Interactions: Ciclosporin (avoid combination);
risk factors.
Contra-indications: Hypersensitivity to flu- It reduces elevated LDL-cholesterol, total Vitamin K antagonists e.g. warfarin (coadmin-
Contra-indications, Precautions, Adverse
vastatin; active liver disease or unexplained, cholesterol and triglycerides and increases istration may result in increased INR – monitor
effects, Advice to patients and Nursing
persistent elevations in serum transaminases; HDL-cholesterol. It takes 1-2 weeks to achieve INR); Ezetimibe; Gemfibrozil and other lipid-low-
action: see under Clofibrate.
pregnancy, breast feeding and in women of therapeutic response and maximum response ering products (increased risk of myopathy);
Dose: see below.
childbearing potential unless they are using is usually achieved by 4 weeks. Tmax is approx. Protease inhibitors e.g. ritonavir, lopinavir
POM COLESTRIM® (Megalife sciences) effective contraception during the therapy 5 hours after oral administration and absolute (concomitant use may strongly increase rosu-
Tablet, Fenofibrate (micronized) 160 mg; ob- period. bioavailability is approx. 20%. It is taken up vastatin exposure – avoid); Antacid containing
long-shaped white tab. Precautions: See under Simvastatin. extensively by the liver and has a volume of dis- aluminium and magnesium hydroxide (de-
160 mg – 3 x 10’s (in blisters) Interactions: Food (no significant interaction). crease in rosuvastatin plasma concentration);
tribution of approx. 134 L. Approximately 90%
POM Fenofibrate (Zolon) Cholestyramine and other bile-acid-sequester- is bound to plasma proteins, mainly to albumin. Erythromycin (decrease in rosuvastatin levels
Tablet, Fenofibrate (in beta cyclodextrin) 160 mg; ing agents (clinically significant additive effect, Rosuvastatin undergoes limited metabolism due to increase in gut motility caused by eryth-
f-c tab. the two drugs should be administered at least (approx. 10%) via mainly CYP2C9. Approx. 90% romycin); Oral contraceptive/HRT (increase in
160 mg – 3 x 10’s 4 hours apart). Rifampicin (reduction in the of the dose is excreted unchanged in the faeces hormonal plasma levels).
POM FENO-TG® (Synergy) bioavailability of fluvastatin by about 50%). (consisting of absorbed and non-absorbed Adverse effects: Constipation, nausea, ab-
Tablet, Fenofibrate 160 mg; f-c tab. Adverse effects: Dyspepsia, insomnia, nausea, active substance) and the remaining part is dominal pain; myalgia; asthenia; headache,
160 mg – 10’s. abdominal pain, headache. excreted in urine. dizziness; diabetes mellitus; pruritus, rash and
Dose: By mouth, Adult, 160 mg once daily. To be Advice to patients: Avoid prolonged exposure Indications: As an adjunct to diet, exercise, and urticaria. Rarely myopathy (including myositis)
swallowed whole during a meal. Dietary to the sun other ultraviolet light; report unex- weight reduction in treatment of hyper-choles- and rhabdomyolysis; pancreatitis; hypersensi-
measures initiated before therapy should
plained muscle pain or weakness, especially if terolaemia. As an adjunct to correction of other tivity reactions including angioedema.
be continued.
Elderly: same as adult dose. accompanied by fever or malaise. risk factors in prevention of major cardiovascu- Dose: Before treatment initiation the patient
Renal impairment: Reduce dose. Nursing action: Administer without regard lar events in high risk patients. should be placed on a standard
to meals. Contra-indications: Hypersensitivity to any cholesterol-lowering diet that should
POM STANLIP® (Ranbaxy) • See also under Simvastatin. component of this product; active liver disease continue during treatment. May be
Caplet, Fenofibrate 160 mg; white f-c cap marked Dose: By mouth, 20-40 mg once daily to be including unexplained, persistent elevations of administered at any time of day, with
‘RX 901’
taken in the evening or at bedtime; serum transaminases and any serum transami- or without food.
160 mg – 3 x 10’s
adjusted according to patient’s re- nase elevation exceeding 3 x ULN); severe renal By mouth, Treatment of hypercholeste-
FLUVASTATIN sponse at an interval of not less than impairment (ClCr <30 mL/min); myopathy; rolaemia, Adult, initially 5-10 mg once
4 weeks up to a maximum 40 mg coadministration with ciclosporin; pregnancy daily; may adjust dose after 4 weeks,
Therapeutic category: Antilipemic Agent;
twice daily at very high cholesterol and lactation and in women of childbearing if necessary. Max. 40 mg daily.
HMG-CoA Reductase Inhibitor.
levels. potential not using appropriate contraceptive Prevention of cardiovascular events, 20
Pharmacology: Fluvastatin, a fully synthetic Note: Patient should be placed on standard Choles- measures. mg daily.
Cholesterol – lowering agent, is a competitive terol-lowering diet before and during treatment with Avoid 40 mg dose in patients with pre-dis- Children and adolescents (10 to 17
inhibitor of HMG-CoA reductase, which is fluvastatin; may be taken without regard to meals;
posing factors for myopathy/rhabdomyolysis: years): initially 5 mg daily; may in-
responsible for the conversion of HMG-CoA to adjust dosage as needed in response to periodic
moderate renal impairment (ClCr <60 mL/min) crease up to a max. 20 mg once daily.
mevalonate, a precursor of sterols, including lipid determinations during the first 4 weeks after
; hypothyroidism; personal or family history Children (<10 years): Not recom-
238 | 5.7 Lipid-regulating drugs 5.8 Vasoprotectives | 239
mended. SIMVASTATIN • Combination with other hypolipidemic agents Tablet, Simvastatin 20 mg; f-c tab
Elderly (>70 years): initially 5 mg once Therapeutic category: Antilipemic Agent; may be required to achieve optimal reductions of 20 mg – 3 x 10’s; 10 x 10’s
daily; may adjust based on response LDL cholesterol.
HMG-CoA Reductase Inhibitor. POM SIMSTATIN® (Barata)
and tolerance. • Diet, weight reduction, and exercise should be
Pharmacology: Simvastatin is a cholester- attempted to control hypercholesterolemia before
Tablets, Simvastatin 10 mg, 20 mg, 40 mg; f-c tabs
Renal insufficiency (mild to moder- ol-lowering agent derived synthetically from Pack: 2 x 14’s (in blisters)
the institution of simvastatin therapy.
ate): initially 5 mg once daily. Avoid a fermentation product to Aspergillus terreus. • Advise patient to continue with the diet and exer- POM SIMVAT-10® (Fidson)
40 mg dose in moderate renal impair- After oral ingestion, simvastatin is converted to cise regimen during therapy. Tablet, Simvastatin 10 mg; f-c tab.
ment. Not recommended in patients the active N-hydroxyacid form which compet- Dose: Prevention of cardiovascular events, 10 mg – 3 x 10’s (in blisters).
with severe renal impairment. itively inhibits 3-hydroxy-3-methylglutaryl-co- by mouth, ADULT initially 20–40 mg POM SIMVOR® (Ranbaxy)
Hepatic impairment: Not recom- enzyme A (HMG-CoA) reductase, an enzyme once daily at night, adjusted at inter- Tablets, Simvastatin USP 5 mg, 10 mg, 20 mg; f-c
mended in patients with active liver which catalyzes an early and rate-limiting vals of at least 4 weeks (maximum 80 tablets.
disease. step in the biosynthesis of cholesterol. This mg once daily at night). 5 mg – 5 x 10’s (in blister)
Race (Asians): initially 5 mg once results in the reduction of total plasma cho- Note: Maximum simvastatin dose of 10 mg daily 10 mg – 5 x 10’s (in blister)
daily. 40 mg dose not recommended. lesterol, low-density lipoprotein (LDL) and very with concomitant ciclosporin, danazol, fibrate or 20 mg – 5 x 10’s (in blister).
Patients with pre-disposing factors to low-density lipoprotein (VLDL) – cholesterol lipid-lowering dose of nicotinic acid; maximum 20
POM ZOSTA® (Synergy)
myopathy: initially 5 mg once daily. mg daily with concomitant amiodarone or verapamil;
concentrations. In addition, simvastatin mod- Tablet, Simvastatin 10 mg.
40 mg dose not recommended. maximum 40 mg daily with concomitant diltiazem.
erately lowers HDL-cholesterol and reduces Muscle effects: Discontinue simvastatin if myopathy
(Additional information sourced from Crestor monograph: http:// plasma triglycerides. is suspected and creatine kinase is elevated (more
www.medicines.org.uk) Indications: Prevention of cardiovascular than 5 times upper limit of normal), or severe mus- 5.8 Vasoprotectives
events in patients with high cardiovascular risk cular symptoms present; simvastatin should not Diosmin is a bioflavonoid used with Hesperi-
POM AURITZ® (Mega lifesciences)
due to atherosclerotic cardiovascular disease be started if creatine kinase is elevated in patients
EMDEX
Tablets, Rosuvastatin (as Calcium salt) 5 mg, 10 mg, din to control internal symptoms of hemor-
or diabetes mellitus. at high risk of muscle effects. There is an increased
20 mg; f-c tabs rhoids. It is used orally as a phlebotropic drug
Contra-indications: Active liver disease (or risk of myopathy if simvastatin is given at high
Pack: 3 x 10’s in the treatment of venous disease, i.e., chronic
persistently abnormal liver function tests); por- dosage or with a fibrate, with lipid-lowering doses
POM AURORA® (Biostadt) of nicotinic acid, or with immunosuppressants such venous insufficiency (CVI) and hemorrhoidal
phyria; pregnancy (Appendix 2); breastfeeding disease (HD), in acute or chronic hemorrhoids,
Tablets, Rosuvastatin 5 mg, 10 mg, 20 mg; f-c tabs. as ciclosporin—monitor liver function, and creatine
(Appendix 3). kinase in symptomatic patients. Risk of rhabdomy- in place of rubber-band ligation, in combina-
POM ROBESTAR® (Novartis) Precautions: History of liver disease or with a olysis (rare) may be increased in renal impairment tion with fiber supplement, or as an adjuvant
Tablet, Rosuvastatin 20 mg; brown f-c tab. high alcohol intake (use should be avoided in and hypothyroidism. therapy to hemorrhoidectomy, in order to
20 mg – 7’s; 14’s; 15’s; 20’s; 28’s; 30’s; 42’s; 50’s; 56’s; active liver disease)—monitor liver function at
60’s; 84’s; 90’s; 98’s; 100’s (in blisters). POM Simvastatin (WMF 12.6) reduce secondary bleeding.
initiation of treatment, 12 weeks after or if dose
Tablets, Simvastatin 5 mg, 10 mg, 20 mg, 40 mg. (Source: http://en.wikipedia.org/wiki/Diosmin).
POM ROLIP® (CG Biostadt) increased, and 6-month intervals thereafter
Tablets, Rosuvastatin (as Ca2+) 5 mg, 10 mg, 20 mg; (discontinue if serum transaminase concentra- POM CIPRIDE® (Vixa)
Preparations containing Diosmin
f-c tabs. tion rises to, and persists at, 3 times the upper Tablet, Simvastatin 10 mg
5 mg – 10’s limit of the reference range); hypothyroidism 10 mg – 2 x 10’s POM DAFLON® 500 (Servier Int’l)
10 mg – 10’s Tablet, Micronised purified flavonoid fraction 500 mg
(see Muscle Effects below); increased risk of my- POM GIMVASTAT®-10 (Pharmabase)
20 mg – 10’s corresponding to: Diosmin 450 mg (90%), flavonoids
opathy or rhabdomyolysis—patients should Tablet, Simvastatin 10 mg; yellow f-c tab. marked
expressed as hesperidin 50 mg (10%).
POM ROSUDEX® (Zolon) be advised to report unexplained muscle pain ‘PBL 10’.
Pack: 30’s.
Tablets, Rosuvastatin (as Calcium salt) 10 mg, 20 (see Muscle Effects below); renal impairment 10 mg – 3 x 10’s (in blisters).
Pharmacology: Daflon 500 is a vascular protector
mg; f-c tabs (Appendix 4); avoid grapefruit juice; interac- POM MOSTEN® (Seagreen) and venotonic. It acts on the return vascular system
10 mg – 3 x 10’s tions: Appendix 1. Tablets, Simvastatin 10 mg, 20 mg; f-c tabs. reducing venous distensibility and venous stasis;
20 mg – 3 x 10’s 10 mg – 2 x 10’s (in blisters) in the microcirculation, it normalizes capillary
Adverse effects: Muscle effects including
POM ROSUTIN® (Solidum) myalgia, myopathy, myositis, rhabdomyolysis 20 mg – 2 x 10’s (in blisters) permeability and reinforces capillary resistance.
Tablet, Rosuvastatin calcium 20 mg; f-c tab. (see muscle effects below); abdominal pain, Micronization of Daflon increases its GI absorption
POM NOVICOR® (Nomedi)
20 mg – 30’s compared with nonmicronized diosmin (urinary
flatulence, constipation, dyspepsia, diarrhoea, Tablets, Simvastatin 10 mg, 20 mg
excretion 57.9% vs 32.7%).
POM ROVISTA® (Getz) nausea, vomiting, pancreatitis, raised serum 10 mg – 1 x 10’s (in blisters)
Indications: Treatment of organic and idiopathic
Tablets, Rosuvastatin (as calcium salt) 5 mg, 10 mg, transaminases, hepatitis, jaundice, headache, 20 mg – 1 x 10’s (in blisters)
chronic venous disease of the lower limbs with the
20 mg; f-c tabs. dizziness, asthenia, peripheral neuropathy, POM SIMKAD® (Embassy) following symptoms: heavy legs, pain, nocturnal
5 mg – 10’s (in blisters) paresthesia, anaemia, pruritus, alopecia, rash Tablet, Simvastatin 10 mg. cramps, edema. Treatment of hemorrhoids and
10 mg – 10’s (in blisters) and hypersensitivity reactions (including an- 10 mg – 10’s. acute hemorrhoidal attacks.
20 mg – 10’s (in blisters) Precautions: Pregnancy & lactation.
gioedema and anaphylaxis). POM SIMLO® (IPCA)
POM ROZVAS (Shrezar) Advice to patients: Promptly report any unex- Advice to patients: In acute hemorrhoids, patient
Tablets, Simvastatin EP 5 mg, 10 mg, 20 mg, 40 should report if symptoms do not disappear within
Tablets, Rosuvastatin 10 mg, 20 mg; f-c tabs plained muscle pain, tenderness or weakness, mg; f-c tabs.
10 mg – 3 x 10 x 10’s 15 days. In venous circulation disorders, treatment
especially if accompanied by malaise or fever; Pack: 14’s.
20 mg – 3 x 10 x 10’s should be combined with a healthy lifestyle. Avoid
follow prescribed diet; take with meals. exposure to the sun, heat, excessive standing and
POM SIMTAB® (Onifam)
POM TURBOVAS® (Micronova) Nursing action: Administer as a single dose in Tablet, Simvastatin 20 mg. being overweight. Walking and wearing special
Tablets, Rosuvastatin calcium 5 mg, 10 mg; f-c tabs. the evening with meals. 20 mg – 10 x 10’s support stockings stimulate blood circulation.
• Liver enzyme elevations may be observed during Adverse effects: Some cases of minor gastrointes-
simvastatin therapy. POM SIMTIN® (Hovid)
240 | 5.9 Peripheral vasodilators
tinal and autonomic disorders have been reported, 5.9 Peripheral vasodilators
not requiring discontinuation of treatment.
Dose: Oral route. The tablets should be taken XANTINOL NICOTINATE
at meals times. Synonym: Xantinol niacinate
Venous insufficiency, 2 tablets daily, Therapeutic category: Peripheral vasodilator,
one at midday and one in the evening purine derivative.
Acute hemorrhoidal attack, 6 tablets Pharmacology: Xantinol nicotinate, an ester
daily for 4 days, then 4 tablets daily of theophylline and nicotinic acid (niacin), acts
for the next 3 days. as a peripheral vasodilator. After absorption in
POM PILICON® (Therapeutic) the body, xantinol nicotinate rapidly degrades
Tablet, Diosmin 150 mg. to nicotinic acid (cation) and xantinol (anion).
150 mg – 24’s (in blisters). The xantinol ion facilitates the transport of
nicotinic acid into the cells thereby improving
ETHANOLAMINE OLEATE the activity of the nicotinic acid. Xantinol
Indications: For use as a sclerosing agent in nicotinate has been shown to enhance cell
the treatment of small, uncomplicated varicose metabolism and oxygen supply in the brain.
veins in the lower extremities. The boost in glucose metabolism and ATP
Contra-indications: Inability to walk, acute levels are particularly beneficial in old age
phlebitis, oral contraceptive use, obese legs, characterized by decrease in cerebral blood
known hypersensitivity to Ethanolamine oleate flow and cerebral metabolism.
or benzyl alcohol. Superficial thrombophlebitis Indications: Management of peripheral and
and deep vein thrombosis in the region of the cerebral vascular disorders including cerebral
varicose veins. Marked arterial, cardiac or renal insufficiency; Short-term memory disorders.
disease. Uncontrolled metabolic disorders Contra-indications: Severe hemorrhage,
such as diabetes mellitus. Patients with local pregnancy, recent myocardial infraction, recent
EMDEX
or systemic infections. cerebrovascular accidents, severely compro-
Precautions: Care should be taken to ensure mised cardiac function, lactation.
that the injection does not leak into perivenous Precautions: Combination with ganglion
tissue which could cause sloughing, ulceration blocking & sympatholytic agents should be
and in severe cases, necrosis. Pregnancy & avoided. Patients with liable blood pressure
lactation. or active peptic ulceration; Elderly; Cardiac
Adverse effects: Burning, cramping sensation, insufficiency, Pulmonary oedema, Oliguria
urticaria. Allergic reactions and anaphylaxis and Anuria.
have been reported following use of sclerosing Adverse effects: Flushing, generalized itch-
agents. ing, rash, abdominal pain, hypoglycemia,
Dose: Adult, by slow IV injection directly into hypotension.
the varicose vein, 2 – 5 mL, divided Dose: By mouth, Adult, Cerebrovascular
between 3 or 4 sites. disorders, peripheral vascular disease,
Child: Not recommended. 3 g daily.
POM Ethanolamine Oleate (Alpha) (References: Loriaux SM, Deijen JB, Orlebeke JF, De Swart
Injection, Ethanolamine oleate 5%; clear pale yellow JH. The effects of nicotinic acid and xanthinol nicotinate on
human memory in different categories of age. Psychopharma-
liquid in transparent colourless amp.
cology; Dec 1985. Available from: http://link.springer.com/
Pack: 10 x 10’s article/10.1007%2FBF00432500).
POM PLACOMP® Retard (Visko)

Tablet, Xantinol nicotinate 500 mg.
Pack: 10 x 10’s.
6. Drugs affecting blood
and nutrition
6.1 Anti-anaemia drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 242
6.1.1 Drugs used in iron-deficiency and megaloblastic anaemias. . . . . . . . . . . . . . . 243
6.1.2 Drugs used in neutropenia. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 252
6.1.3 Drugs used in hypoplastic, haemolytic, and renal anaemias. . . . . . . . . . . . . . . 252
6.1.4 Drugs used in sickle cell disease. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 253
6.2 Drugs affecting coagulation. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 253
6.2.1 Anticoagulants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 254
6.2.2 Reversal of anticoagulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257
6.3 Antifibrinolytics and haemostatics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 258
6.4 Blood products and plasma substitutes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
6.4.1 Plasma substitutes. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
6.4.2 Plasma fractions for specific use. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
6.5 Vitamins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 263
EMDEX
6.6 Minerals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 274
6.7 Appetite Stimulants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277
6.8 Solutions for correcting water, electrolyte and acid-base disturbances. . . . . . 277
6.8.1 Oral electrolyte solutions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277
6.8.1.2 Oral potassium . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 277
6.8.2 Parenteral electrolyte solutions. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 278
6.8.3 Water . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 282
6.9 Peritoneal dialysis solution. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 282
6.10 Parenteral nutrition. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 283
242 | 6.1 Anti-anaemia drugs 6.1.1 Drugs used in iron-deficiency and megaloblastic anaemias | 243
6.1 Anti-anaemia drugs about 100–200 mg/100 mL per day or 2 g/100 to vitamin B12 deficiency. • Encourage diet rich in vitamin B12 viz egg, yolk,
mL over 3–4 weeks. After the haemoglobin Preparations containing a ferrous salt and fo- fish, organ meat.
6.1.1 Drugs used in iron-deficiency and megaloblas-
tic anaemias has risen to normal, treatment should be lic acid are used for the prevention of megalo- Dose: By mouth, Vitamin B12 deficiency due
6.1.2 Drugs used in neutropenia continued for a further 3 months to replenish blastic anaemia in pregnancy. The low doses of to inadequate diet, Adult, 50-150 mcg
6.1.3 Drugs used in hypoplastic, haemolytic, and the iron stores. folic acid in these preparations are inadequate or more daily; to be taken between
renal anaemias Iron intake in the evening has been reported for the treatment of megaloblastic anaemias. meals.
IRON-DEFICIENCY ANAEMIA to improve its absorption. Iron intake with Child: 30-50 mcg twice daily
PREVENTION OF NEURAL TUBE DEFECTS By IM injection, initially 1 mg
Anaemia has many different aetiologies. It meals may reduce bioavailability but improve
tolerability and adherence. An adequate intake of folic acid before con- repeated 10 times at intervals of 2-3
occurs when the haemoglobin concentration ception and during early pregnancy reduces days.
falls below the normal range for the age and If adverse effects occur, either the dosage can the risk of neural tube defects in babies. There- Maintanance: 1 mg every month.
sex of the individual. It is essential that a correct be reduced or an alternative iron salt used, but fore, women planning a pregnancy should Note: Hydroxocobalamin is now preferred to cy-
diagnosis is made before initiating therapy. Any an improvement in tolerance may be due to receive sufficient folic acid before conception anocobalamin because it is retained in the body
serious underlying cause of iron-deficiency lower content of elemental iron. Gastrointesti- and in the first 12 weeks of pregnancy; folic longer and for maintenance therapy, it can be given
anaemia, including gastric erosion and GI nal irritation may occur with iron salts. Nausea acid may be given as a food or a medicinal at intervals of up to 3 months.
cancer, should be excluded before giving iron and epigastric pain are dose-related. Iron supplement in a dose of 400–500 µg daily. A POM Hydroxocobalamin (EDL 16.1)
replacement. Prophylaxis with iron salts is preparations taken orally may be constipating, woman who has not received supplementary Injection, Hydroxocobalamin 1 mg per mL; in amp.
justifiable in individuals who have additional particularly in the elderly, occasionally leading folic acid and suspects that she might be preg- POM BINOX-12® (Beta Drugs)
risk factors for iron deficiency (for example to faecal impaction. Oral iron may exacerbate nant should start taking folic acid at once and Injection, Vitamin B12 1 mg per 2 mL; sterile solution
dietary deficiency). diarrhoea in patients with inflammatory bowel continue until week 12 of pregnancy. in 2-mL ampoule.
Prophylaxis may also be appropriate in malab- disease but care is also needed in patients with Pack: 2-mL x 10’s; 2-mL x 100’s.
Women at increased risk of giving birth to a
EMDEX
sorption, menorrhagia, after subtotal or total intestinal strictures and diverticular disease.
Iron as iron dextran (a complex of ferric hy- baby with neural tube defects (for example POM CATOMIN® (Goldmoore)
gastrectomy, and in haemodialysis patients. history of neural tube defect in a previous Injection, Vitamin B12.
Supplementation with iron and folic acid is rec- droxide with dextrans) [not included on WHO
Model List] or iron sucrose (a complex of ferric child) should receive a higher dose of folic acid POM COBIVITA® (Vixa)
ommended by WHO for all pregnant women; of approximately 5 mg daily, starting before
hydroxide with sucrose) [not included on WHO Injection, Vitamin B12.
in addition, where prevalence of anaemia is conception and continuing for 12 weeks after
above 40%, it is recommended that women of Model List] may be given parenterally if the Vitamin B12 + Haemoglobin
patient cannot tolerate oral iron, or does not conception. Women taking antiepileptic med-
child-bearing age and breastfeeding women ication should be counselled by their doctor OTC DE-DEON’S B12® (Daily Need)
should be given 3 months of iron and folic acid take it reliably or if there is continuing severe
before starting folic acid. Syrup, Haemoglobin, Vitamin B12.
supplementation. blood loss or malabsorption. Many patients Pack: 60 mL.
with chronic renal failure who are receiving Dose: By mouth, Adult, 10 mL twice daily; Child, 5
Low birth-weight infants such as preterm ne- haemodialysis (and some on peritoneal di- 6.1.1 Drugs used in iron-deficiency mL daily. May be taken pure or mixed with
onates should receive iron supplementation alysis) require intravenous iron on a regular and megaloblastic anaemias water to form a pleasant taste.
from 2 to 23 months. Iron supplementation basis. Parenteral iron may cause more harm
should also be given to all children between CYANOCOBALAMIN OTC AVROHB® (Avro)
than benefit. With the exception of patients Syrup, Haemoglobin 500 mg, Malt extract 100 mg,
6 and 23 months if their diet does not include on haemodialysis the haemoglobin response Synonym: Vitamin B12
Cyanocobalamin (Vitamin B12) 20 mcg per 5 mL.
foods fortified with iron or if prevalence of is not significantly faster with the parenteral Therapeutic category: Water Soluble Vitamin. Pack: 200 mL.
anaemia is above 40%. Children aged 24 route than the oral route. Indications: Treatment of pernicious anae- Dose: Adult, 10 mL 4 times daily
months and above should receive a 3-month mia and other vitamin B12 deficiency states; Child (2-5 years): 5 mL 2 times daily;
course of iron supplementation (with folic MEGALOBLASTIC ANAEMIAS
increased vitamin B12 requirements due to 6-12 years, 5 mL 4 times daily.
acid if above 5 years) if the local prevalence of Megaloblastic anaemias result from a lack of pregnancy, thyrotoxicosis, haemorrhage, liver
anaemia is above 40%. either vitamin B12 (hydroxocobalamin) or folate or kidney disease. OTC Dr. Jenkin’s Syrup of Haemoglobin (Gauze)
or both. The clinical features of folate-deficient Oral liquid, Haemoglobin 500 mg, vitamin B12 20 mcg,
Ferrous salts should be given orally wherever Contra-indications: Hypersensitivity to cyano-
malt 100 mg per 5 mL
possible. They differ only marginally in effi- megaloblastic anaemia are similar to those of cobalamin or any component, cobalt; patients
Pack: 200 mL
ciency of absorption and thus the choice of vitamin B12 deficiency except that the accom- with hereditary optic nerve atrophy.
panying severe neuropathy does not occur; it Adverse effects: Itching, diarrhoea, peripheral OTC HB 12 (United African Lab)
preparation is usually decided by incidence of
is essential to establish the underlying cause in vascular thrombosis. Liquid, Haemoglobin 500 mg, Vitamin B12 20 mcg,
adverse effects and cost. Ferric salts are much Malt extract 100 mg per 5 mL.
less well absorbed. The oral dose of elemental every case. Hydroxocobalamin is used to treat Advice to patients: Pernicious anaemia will
Pack: 400 mL in bottle .
iron for treatment of irondeficiency anaemia in vitamin B12 deficiency whether due to dietary require treatment for life.
adults should be 100–200 mg daily with meals. deficiency or malabsorption including perni- Nursing action: Administer with fruit juice OTC HS 12® (Teta)
cious anaemia (due to a lack of intrinsic factor, to disguise taste and with food for better Syrup, Haemoglobin 500 mg, Vitamin B12 20 mcg
The approximate elemental iron content of which is essential for vitamin B12 absorption). absorption. per 5 mL
various ferrous salts is ferrous fumarate 210 mg • Oral therapy is markedly inferior to paren-
Pack: 200 mL
(68 mg iron), ferrous gluconate 300 mg (35 mg Folate deficiency due to poor nutrition,
pregnancy, antiepileptics or malabsorption teral therapy due to poor absorption; IV is OTC PINEWOOD HB12 ®(Nancil)
iron), ferrous succinate 100 mg (35 mg iron), not recommended due to problem of rapid Syrup, (forte), Haemoglobin 700 mg, vitamin B12
ferrous sulfate 300 mg (60 mg iron), and dried is treated with folic acid but this should never
elimination (Hydroxocobalamin is retained in 5 mcg
ferrous sulfate 200 mg (65 mg iron). be administered without vitamin B12 in undiag-
the body longer than Cyanocobalamin and is Pack: 200 mL
nosed megaloblastic anaemia because of the
The haemoglobin concentration should rise by risk of precipitating neurological changes due generally preferred).
244 | 6.1.1 Drugs used in iron-deficiency and megaloblastic anaemias 6.1.1 Drugs used in iron-deficiency and megaloblastic anaemias | 245
Methylcobalamin constipation namely increased bulk and fluid nancy and lactatioin, illness, blood loss or mcg, Vitamin B13.0 mg, Vitamin B6 2.0 mg, Copper
in the diet. general weakness, 15-30 mL daily sulphate 2.51 mg equiv. to 1.0 mg of copper, Zinc
POM BIOBETIC® (Biofem)
• Percentage of elemental iron in Child: 5 mL 1-3 times daily. sulphate 24.7 mg equiv. to 10.0 mg of zinc, Di-cal-
Capsule, Methylcobalamin 1500 mcg, Alpha lipoic
cium phosphate 339.5 mg equiv. to to 100.0 mg of
acid 300 mg, chromium (as polynicotinate) 25 Ferrous gluconate 12% OTC BRADFEREX® (Bradford)
calcium, Manganese sulphate 5.50 mg equiv. to 2.0
mcg, Selenium (as selenomethionine) 40 mcg, Zinc Ferrous sulfate 20% (32% in dried salt) Tonic, Ferric ammonium citrate 69 mg (equiv. to
mg of Manganese.
(as ascorbate) 3.15 mg, Calcium D-pantothenate Ferrous fumarate 33% elemental iron 14 mg), cyanocobalamin 2.5 mcg,
Pack: 30’s; 120’s (in blister); 250’s; 500’s.
12.5 mg, Vitamin B6 3 mg, Folic acid 1.5 mg; hard vitamin B1 2 mg, vitamin B2 500 mcg, nicotinamide
Dose: Iron-deficiency anaemia, by mouth, Tonic, Ferric ammonium citrate 69 mg equiv. to 14.0
gelatin cap. 5.0 mg, folic acid 200.0 mcg per 5 mL
mg elemental iron, Folic acid 0.5 mg, Vitamin B12
ADULT elemental iron 100–200 mg Pack: 200 mL
POM MEBAAL® (Megalife sciences) (Cyanocobalamin) 5 mcg, Vitamin B1 2 mg, Vitamin B2
daily in divided doses. 1 mg, Vitamin B6 2 mg, Nicotinamide 5 mg per 5 mL.
Tablets, Methylcobalamin 500 mcg, 1500 mcg; OTC BRADFERON® (Bradford)
brown tabs. Prevention of iron deficiency anaemia Tonic, Ferric ammonium citrate 250 mg, vitamin Pack: 200 mL
Pack: 3 x 10’s (in those at particular risk), by mouth, B12 (cyanocobalamin) 2.5 mcg, Folic acid 200 mcg, Dose: By mouth, Adult, 15 mL 3 times daily
Indications: Peripheral neuropathy, dementia, ADULT (woman) elemental iron vitamin B2 2.0 mg, Nicotinamide 5.0 mg per 5 mL. Child, 5 mL 3 times daily.
alcoholism. 60 mg daily; CHILD under 5 years Pack: 200 mL OTC EPITONE® (BCN)
Dose: One tab. 1-2 times daily elemental iron 2 mg/kg (maximum 30
OTC CHROMAFOL® (Reals) Mixture, Ferrous gluconate 225 mg, calcium gluco-
mg) daily, over 5 years elemental iron Capsule, Ferrous sulphate 150 mg (as sustained nate 200 mg, manganese glycero-phosphate 6 mg,
FERROUS SALTS 30 mg daily; in women and children vitamin B1 0.7 mg, vitamin B2 0.4 mg, nicotinamide
released form), Folic acid 5 mg.
Synonym: Oral iron; Ferrous Fumarate, Ferrous over 5 years, folic acid may also be Pack: 3 x 10’s 6 mg per 10 mL.
Gluconate, Ferrous Sulfate, Ferrous Succinate; given. Pack: 200 mL.
OTC COCOFER® (Zoomota) Dose: Adult and child over 12 years, 10 mL 3 times
Ferric Ammonium Citrate. OTC Ferrous salts (WMF 10.1) Syrup, Iron (III) hydroxide polymaltose complex daily; 5-12 years, 5 mL 3 times daily. To be
Indications: Iron-deficiency anaemia. Tablet, Ferrous salt equiv. to 60 mg iron. equiv. to elemental iron 50 mg per 5 mL; dark taken after meals. Not recommended for
Contra-indications: Haemosiderosis, haemo-
EMDEX
Oral liquid, Ferrous sulfate equiv. to 25 mg iron/mL. brown liquid. child <5 years
chromatosis; any form of anaemia not caused Pack: 150 mL.
OTC Ferrous Sulfate (EDL 16.1) OTC FALBITONE® (Vitahealth)
by iron deficiency; patients receiving repeated Tablet, Ferrous sulfate 200 mg equiv. to 60 mg iron. Dose: Adult, 100-200 mg daily.
blood transfusions; parenteral iron therapy. Child (1-2 years), 50-100 mg daily. Capsule, Ferrous fumarate 150 mg, Vitamin A 1000
Precautions: Should not be administered for OTC Ferric Ammonium Citrate (EDL 16.1) IU, Vitamin C 30 mg, Vitamin E 3 mg, Folic acid 2
Mixture, Ferric ammonium citrate 400 mg per 5 mL. OTC DETONIC® (Afrab-Chem) mg, Vitamin B1 nitrate 2 mg, Vitamin B2 1.5 mg,
longer than 6 months; pregnancy; peptic ulcer, Mixture, Ferrous Gluconate 120 mg, Folic acid 0.3 Vitamin B6 2 mg, Nicotinamide 10 mg, Vitamin B12 5
regional enteritis, ulcerative colitis, intestinal OTC AMIRON® (Ceenek) mg, Vitamin B12.0 mg, Vitamin B2 1.0 mg, Vitamin B6 mcg, Magnesium oxide 60 mg, Zinc sulphate 5 mg,
strictures, diverticula; overdosage: see section Liquid, Ferric ammonium citrate 200 mg, Vitamin B12 2.0 mg, Vitamin B12 5.0 mcg per 5 mL. Copper sulphate 1.5 mg, Manganese sulphate 1.5
19.2.4; interactions: Appendix 1. 5 mcg, Folic acid 0.5 mg per 5 mL Pack: 200 mL. mg Calcium phosphate dibasic 75 mg, Potassium
Adverse effects: Constipation, diarrhoea, dark Pack: 200 mL Dose: Adult and Child above 12 years, 5-10 mL twice iodide 0.05 mg.
stools, nausea, epigastric pain, GI irritation; Dose: Adult, Treatment, 10 mL 3 times daily daily. Child (6-12 yrs), 5 mL twice daily. Pack: 3 x 10’s; 10 x 10’s; 12 x 10’s (in packs); 250’s
Prophylaxis, 5 mL 1-2 times daily (in jars)
long-term or excessive administration may OTC DETONIC® Plus (Afrab-chem)
Child (5-12 years): 5 mL 1-2 times daily
cause haemosiderosis. Syrup, Ferrous gluconate (equiv. to elemental iron OTC FAMARON® (Sofak)
Advice to patients: Although iron prepara- OTC ASTYFER® (Fidson) 14 mg) 120 mg, thiamine HCI 2 mg, riboflavin Tonic, Ferrous ammonium citrate 200 mg, folic acid
tions are best absorbed on an empty stomach Syrup, Ferrous glycine sulfate 275 mg, L-Histadine 4 5-phosphate 1 mg, pyridoxine HCI 2 mg, cyano- 200 mcg, vitamin B2 3 mcg, per 5 mL.
mg, L-Lysine 25 mg, Thiamine 5 mg, Riboflavin 3 mg, cobalamin 5 mcg, folic acid 0.30 mg, L-lysine HCI 8 Pack: 100 mL; 200 mL
they may be taken after food to reduce GI ad-
Pyridoxine 1.5 mg, Folic acid 0.5 mg, Nicotinamide mg, L-phenylalanine 1.60 mg, L-threonine 1.40 mg,
verse effects; do not take with milk or antacids; 25 mg, Cyanocobalamin 2.5 mcg, Dexpanthenol OTC FEFODAN® (Dana)
L-tryptophan 1.60 mg, ginseg extract 25 mg,calcium
they may discolour stools. Liquid preparations 2.5 mg per 10 mL. pantothenate 1 mg per 5 mL Capsule, Dried ferrous sulphate 150 mg (equiv. to 45
containing iron salts should be well diluted Pack: 200 mL. Pack: 200 mL mg elemental iron in timed-release form), folic acid
with water (and if possible swallowed through Dose: Adult and Child (over 12 years), 10 mL twice 0.5 mg; sustained-release cap.
OTC Dr. Meyer’s Ferovital® (Vitabiotics) Pack: 1 x 15’s; 2 x 15’s (in blisters)
a drinking straw to prevent discoloration of the daily; 7-12 years, 2.5 mL twice daily; 2-6
years, 2.5 mL once a day. Syrup, Ferric ammonium citrate 50 mg (equiv. to Indications: Haematinic preparation of prophylaxis
teeth). Keep out of reach of children.
elemental iron 10 mg), Folic acid 200 mcg, Vitamin of iron and folic acid deficiency during pregnancy.
Nursing action: Administer between meals OTC BENTONIC® (Bentos) B12 5 mcg, Vitamin B1 3 mg, Vitamin B2 0.5 mg, Vitamin
but may give with food because of GI upset; for Capsule, Ferrous fumarate 43 mg, Folic acid 0.5 mg, B6 2 mg, Nicotinamide 5 mg, Zinc sulphate 7 mg, OTC FEFODAN-Z® (Dana)
best absorption give with fruit juice. Vitamin B12 1.0 mg, Vitamin B2 1.0 mg, Vitamin B6 1.5 Copper sulphate 0.2 mg. Capsule, Dried ferrous sulphate 150 mg equiv. to
• Tell patient not to crush tablets but to take mg, Vitamin B12 5 mcg, Vitamin C 25 mg, Vitamin E Pack: 200 mL. 45 mg of elemental iron in timed-release form),
it whole. 3 mg, Nicotinamide 15 mg, Zinc sulphate 0.3 mg, Dose: Adult, 5-10 mL 2 times daily. Zin sulphate monohydrate 61.8 mg (equiv. to 22.5
• Give oral liquid preparation with straw to Magnesium sulphate 0.3 mg. Child (>6 years): 5-10 mL 2 times daily; 2-6 mg of elemental zinc in timed-release form), Folic
Pack: 3 x 10’s years, 5 mL 1-2 times daily; <2 years, 2.5 mL acid 0.5 mg.
prevent discolouration of tooth enamel.
Syrup, Ferrous gluconate 120 mg, Vitamin B1 1 mg, 2 times daily. Pack: 1 x 15’s’ 2 x 15’s (in blisters)
• Teach patient to avoid reclining position for Indications: Haematinic preparation of prophylaxis
Vitamin B2 1 mg, Vitamin B6 2 mg, Nicotinamide 5
15-30 minutes after drug to avoid oesopha- mg per 5 mL. OTC Dr. Meyer’s Liquid Iron® (Adler) of iron and folic acid deficiency during pregnancy.
geal corrosion; to take medication at least 1 Pack: 200 mL. Mixture, Ferric ammonium citrate 200 mg, Folic acid
200 mcg, Vitamin B12 3 mcg per 5 mL. OTC FEGEM® (Zolon)
hr before bedtime to avoid corrosion in the Dose: Adult, 5 mL 1-3 times daily or 1-2 capsules
Pack: 100 mL; 200 mL. Tablet, Iron Polymaltose, Folic acid.
stomach. 1-3 times daily. Pack: 10’s.
• Do not give antacids, eggs, milk; if these have As nutritional supplement & in menstruation, OTC EMZORON® (Emzor) Syrup, Iron Polymaltose (equiv. to 50 mg elemental
been eaten, delay administration for an hour. 5 mL daily or 1 capsule daily. In times of Capsule, Ferrous fumarate equiv. to 14.5 mg Iron).
• Teach patient dietary measures for preventing increased requirement, prophylaxis in preg- elemental iron, Folic acid 0.3 mg, Vitamin B12 3.0 Pack: 150 mL.
OTC FEGLO® (Zoomota) Tonic, Ferric ammonium citrate 50 mg, folic acid 200 200 mg – 30’s; 100’s; 1000’s. OTC HEMATONE® (Sofak)
Tablet, Ferrous gluconate 300 mg equiv. to 35 mg mg, vitamin B12 5 mcg, vitamin B1 3 mg, vitamin B2 Tonic, Ferric ammonium citrate 85 mg, folic acid 250
OTC FOLFER® (Al-Tinez)
elemental Iron; red s-c tab. 0.5 mg, vitamin B6 2 mg, nicotinamide 5 mg, zinc mcg, vitamin B12 5 mcg, vitamin B1 2 mg, vitamin B2
Capsule, Ferrous fumarate 182 mg, folic acid 0.5 mg
300 mg – 1,000’s. sulphate 7 mg, copper sulphate 0.2 mg per 5 mL. 2 mg, vitamin B6 2 mg, zinc 5 mg, copper 0.4 mg,
Pack: 200 mL nicotinamide 5 mg per 5 mL
OTC FERBELAN® (Evans)
OTC FOLIGROW® (Shrezar) Pack: 200 mL
Capsule, (forte), Iron as dried Ferrous sulphate (equiv- OTC FERRODAN® (Dana)
Capsule, Iron, minerals & vitamins
alent to 30 mg elemental iron) 100 mg, Zinc (from Syrup, Ferric ammonium citrate (equiv. to 41mg of OTC IRNOFOL® (JB Pharma)
Pack: 3 x 10 x 10’s
zinc sulphate) 12 mg, Manganese (from manganese elemetal iron), Vitamin B12 5 mcg, Folic acid 0.50 Syrup, Ferrous glycine sulphate 275 mg, L-histidine
sulphate) 2.0 mg, Copper (from copper sulphate) 1.5 mg per 5 mL. OTC GAVIRON® (Gauze) HCI H2O 4 mg, L-lysine HCl 25 mg, Thiamine HCI 5
mg, Vitamin B1 2 mg, Vitamin B2 2 mg, Vitamin B12 5 Pack: 200 mL Liquid, Ferric ammonium citrate 200 mg, folic acid mg, Riboflavin (Riboflavin sodium phosphate) 3 mg,
mg, Nicotinamide 15 mg, Folic acid 2 mg. 200 mg, cyanocobalamin (B12) 3 mcg per 5 mL Pyridoxine HCI 1.5 mg, Folic acid 0.5 mg, Nicotina-
OTC FERROL® (Strides Vital)
Pack: 30’s; 250’s (in blisters) Pack: 200 mL mide 25 mg, Cyanocobalamin 2.5 mg, Dexpanthenol
Tablet, Ferrous sulfate.
Tonic, Ferric ammonium citrate 46.5 mg, vitamin B1 2.5 mcg per 10 mL; syrupy base.
Pack: 1000’s. OTC GLORON® (Richygold)
2 mg, vitamin B2 500 mcg, vitamin B12 2500 mcg, Pack: 200 mL
nicotinamide 5 mg per 5 mL. Syrup, Ferric ammonium citrate 160 mg (equiv. to Indications: Pregnancy, lactation, anemia (due to
OTC FERROLAB-12® (Embassy)
Pack: 100 mL elemental iron 32 mg), cyanocobalamin 7.5 mcg, helminthiasis, haemorrhoids, anal fissures, chronic
Capsule, Ferrous fumarate 200 mg, folic acid 100 mg,
folic acid 0.5 mg per 5 mL. gastric ulcers, iron deficiency anaemia in hookworm
vitamin B12 100 mcg.
OTC FERILEX® Junior (Therapeutic) Pack: 200 mL.
Pack: 30’s. disease, haemorrhoids, infective hepatitis, malaria,
Syrup, Ferric ammonium citrate 30 mg, folic acid 200
OTC GOZFERON® (Goz) post surgical conditions, nutritional anemia in
mcg, vitamin B12 5 mcg per 5 mL; dark red syrup. OTC FERRON-6® (Justeen)
Oral liquid, Ferric Ammonium Citrate B.P 69 mg elderly patients, tuberculosis, malabsorption
Pack: 100 mL; 200 mL; 750 mL. Tablet, Ferrous sulfate BP 200 mg.
(equiv. to 14 mg of elemental iron) per 5 mL; in a syndromes.
Pack: 1 x 1000’s.
OTC FERILEX® (Therapeutic) pleasantly flavoured base. OTC IRON DEX® (Geneith)
Liquid, Ferric ammonium citrate 200 mg (equiv. to OTC FERROTOGEN® (Bond) Pack: 100 mL; 200 mL; 750 mL
EMDEX
Capsule, Ferric ammonium citrate 160 mg, Vitamin
40 mg free elemental iron) per 5 mL. Tonic, Ferric ammonium citrate 70 mg (equiv. to
OTC HAEM-F® (Interpharma) B12 7.5 mcg, Folic acid 0.5 mg, Zinc 20.61 mg.
Pack: 100 mL; 200 mL. 14.35 mg of elemental iron), folic acid 0.12 mg,
Capsule, Ferrous fumarate, cyanocobalamin, folic Pack: 3 x 10’s
vitamin B1 0.50 mg, vitamin B2 0.50 mg, vitamin Mixture, Ferric ammonium citrate 160 mg, Vitamin
OTC FERITAB® (Chanmedi) acid, zinc sulfate.
B6 0.33 mg, vitamin B12 0.075 mg, nicotinamide 5 B12 7.5 mcg, Folic acid 0.5 mg per 15 mL.
Tablet, Ferrous sulphate 200 mg Pack: 30’s.
mg per 5 mL. Pack: 200 mL
200 mg – 1000’s Syrup, Ferric ammonium citrate 200 mg, cyanoco-
Dose: Infants (up to 2 years) – As directed by
balamin 5 mg, folic acid 1 mg per 15 mL. OTC IRONOGLOBIN® (Therapeutic)
OTC FERITAB® Plus (Chanmedi) the physician. Child (2 – 12 years): 1 or 2
Pack: 200 mL. Syrup, Iron III polymaltose 5 mg (equiv. to 10 mg of
Tablet, Ferrous sulphate 200 mg, Folic acid 0.125 mg teaspoonful ( 5 – 10 mL).
Dose: Adult 15 mL 1-2 times daily. elemental iron), Vitamin B1 2 mg, Vitamin B2 1.5 mg,
Pack: 1000’s
OTC FERROTONE® (Mega Lifesciences) Vitamin B6 2 mg, Vitamin B12 5 mcg, Nicotinamide
OTC HEM-9® (Siebel)
OTC FERITAN® (Diamond Remedies) Capsule, Ferrous fumarate 162 mg, Folic acid 0.75 15 mg, L-lysine 62.5 mg, Folic acid 300 mcg, Zinc
Capsule, Ferrous fumarate 150 mg, zinc sulfate
Capsule, Ferrous fumarate 300 mg; red cap. marked mg, Vitamin B12 7.5 mcg; red vanilla flavoured ob- sulphate 15 mg.
monohydrate 50 mg, Lysine HCl 25 mg, glycine 10
‘FERITAN’. long-shaped cap. marked ‘FERROTONE’. Pack: 100 mL; 200 mL; 1 L.
mg, vitamin B1 (thiamine nitrate) 5 mg, vitamin B2
300 mg – 3 x 10. Pack: 10 x 10’s.
(riboflavin) 3 mg, vitamin B6 (pyridoxine HCl) 1.5 OTC JAWARON® (Jawa)
Dose: One capsule daily. In pregnancy, one capsule
OTC FERITAN® Plus (Diamond Remedies) mg, vitamin B12 (cyanocobalamin) 2.5 mcg, vitamin Capsule, Ferrous fumarate 150 mg, vitamin A 1500
two times daily.
Syrup, Ferric ammonium citrate equiv. to elemental C (ascorbic acid) 33.3. mg, folic acid 5 mg, copper IU, vitamin C 30 mg, vitamin E 3 mg, vitamin B1 2
iron 41 mg, Folic acid 500 mcg, Vitamin B12 5 mcg, OTC Ferrous Gluconate (Emzor) sulphate pentahydrate 2.2 mg, dried magnesium mg, vitamin B2 2 mg, vitamin B6 2 mg, vitamin B12
Vitamin B1 2 mg, Vitamin B2 1.5 mg per 5 mL; fla- Tablet, Ferrous gluconate 300 mg; red s-c tab. sulphate 50 mcg, selenium as selenious acid 50 mcg, 5 mcg, nicotinamide 10 mg, folic acid 2 mg, lysine
voured syrupy base 300 mg – 100; 1000. choline bitartrate 50 mg, potassium iodide 1 mg. monohydrochloride 100 mg, zinc sulfate 5 mg,
Pack: 200 mL Pack: 2 x 15’s copper sulfate 1.5 mg, manganese sulfate 1.5 mg,
OTC Ferrous Sulfate (Emzor)
OTC FEROBIN® (Fidson) Tablet, Ferrous sulfate 300 mg; s-c red tab. OTC HEMAFOLIN® (Neimeth) calcium phosphate 75 mg, magnesium oxide 60 mg,
Syrup, Ferric ammonium citrate 200 mg (equiv. to 300 mg – 1000’s. Capsule, Iron (as sulfate) 18 mg, vitamin B1 1.5 mg, potassium iodide 0.05 mg.
43 mg of Elemental iron), Folic acid 0.5 mg, vitamin vitamin B2 2 mg, vitamin B6 2 mg, vitamin C 75 mg, Pack – 20; 30; 120; 250.
OTC Ferrous Sulfate (Phamatex) Dose: Prophylaxis, 1 capsule daily. Treatment, 1
B1 2.0 mg, vitamin B2 1.0 mg, vitamin B6 2.0 mg, vi- vitamin B12 3 mcg, niacinamide 20 mg, folic acid
Tablet, Ferrous sulfate 200 mg capsule 2 times daily.
tamin B12 5 mcg, nicotinamide 5.0 mg, zinc 1.0 mg, 400 mg
200 mg – 1000 Mixture, Ferrous gluconate 120 mg, vitamin B1 1
manganese 1.5 mg per 5 mL. Pack – 30; 90.
Pack: 110 mL; 200 mL. OTC Ferrous Sulphate (Jopan) Dose: One capsule to be taken once daily. mg, vitamin B2 1 mg, vitamin B6 2 mg, vitamin B12 1
Dose: Adult, 5 mL 3-4 times daily; adjusted gradually Tablet, Dried ferrous sulphate 200 mg equiv. to 60 mcg, nicotinamide 5 mg, zinc sulfate 15 mg, lysine
OTC HEMFERON-400® (Ranbaxy) monohydrochloride 200 mg per 5 mL.
based on need and tolerance. mg of elemental iron; sugar coated tab.
Mixture, Ferric ammonium citrate 400 mg per 5 mL. Pack: 100 mL; 200 mL.
Pack: 50’s x 2; 100’s; 100’s (in blisters)
OTC FEROGLOBIN B12® (Adler) Pack: 180 mL. Dose: Adult, 10-20 mL twice daily.
Tonic, Iron & Vitamin preparation OTC FERSOLATE® (Evans) Child (6-12 years), 5ml twice daily.
OTC IB® Tonic (Bond)
Pack: 200 mL Tablet, Dried ferrous sulfate 200 mg, copper sulfate
Tonic, Ferric ammonium citrate 200 mg, vitamin B1 OTC JUFERON® (Juhel)
Capsule, Iron & Vitamin preparation 2.5 mg, manganese sulfate 2.5 mg; dark red s-c tab.
2 mg, vitamin B2 1 mg per 5 mL. Syrup, Ferric ammonium citrate 200 mg, Folic acid
Pack: 30’s Pack: 100; 1000.
Pack: 200 mL. 0.5 mg, Vitamin B12 5.0 mcg per 5 mL.
Dose: Adult, one tablet 3 times a day during or
OTC FEROVITA® (Strides Vital) Dose: Child (2 – 5 years): ½ teaspoonful twice daily. Pack: 200 mL.
immediately after meals.
Tablet, Ferrous sulfate. 5 – 12 years: 1 teaspoonful two times daily.
Pack: 3 x 10’s. OTC FESULF® (Therapeutic) Should be taken neat or mixed with water, OTC KING TONIC® (SKG)
Tablet, Dried ferrous sulphate BP 200 mg (equiv. to preferably after meal. Mixture, Ferrous fumarate 45.539 mg, thiamine
OTC FEROVITAL® (Vitabiotics) HCI 3.5 mg, riboflavin 1 mg, pyridoxine HCI 2 mg,
65 mg elemental iron); bright red and brown tab.
nicotinamide 15 mg, calcium D-pantothenate 6 mg, 7.5 mcg, Lysine HCl 50 mg, Niacinamide 45 mg, Syrup, Ferric ammonium citrate 200 mg (equiv. to Riboflavin sodium phosphate) 3 mg, Pyridoxine HCl
vitamin B12 2 mg. Panthenol 5 mg, Pyridoxine HCl 1.5 mg, Flavoured elemental iron 41 mg), vitamin B12 5 mcg, folic acid 1.5 mg, Ferrous glycine sulphate 275 mg, (Equivalent
Pack: 100 mL; 200 mL syrupy base per 15 mL. 0.50 mg, sorbitol solution 1.75 g per 5 mL. to elemental iron 47mg), L-Histidine HcL H20 4 mg,
Dose: Adult and child (over 12 years), 15 mL twice Pack: 200 mL Pack: 100 mL; 200 mL. l-Lysine HcL 25 mg, Thiamine HCl 5 mg, Riboflavin
daily; under 7 years, 5 mL twice daily; 7–12 Dose: Adult, Treatment, 10 mL 3 times a day; proph- (as Riboflavin sodium phosphate) 3 mg, Pyridoxine
OTC MUMFER®(Glenmark)
years, 10 mL twice daily. ylaxis, 5 mL 1-2 times daily. HCl 1.5 mg, Folic acid 0.5 mg, Nicotinamide 25 mg,
Chewable tablet, Iron (III)-hydroxide polymaltose
Child (5-12 years), 5 mL 1-2 times daily. Cyanocobalamin 2.5 mcg, Dexpanthenol 2.5 mg,
OTC LADY’S OWN® TONIC (SKG) complex equiv. to elemental iron 100 mg, folic
Folic acid 0.5 mg, Nicotinamide 25 mg, Cyanoco-
Tonic, Iron (as Ferrous fumarate) 95.238 mg, thiamine acid 500 mcg. OTC RED-IRON® (Richygold)
balamin 2.5 mcg, Dexpanthenol 2.5 mg per 10 mL.
HCI 1 mg, riboflavin 1 mg, pyridoxine HCI 5 mg, nic- Pack:10’s Tonic, Iron (as ferrous gluconate) 173 mg (equiv. to
Pack: 200 mL
otinamide 15 mg, calcium D-pantothenate 12 mg, Syrup, Iron (III)-hydroxide polymaltose complex 20 mg elemental iron), folic acid 500 mcg per 5 mL.
cyano-cobalamin 0.004 mg, zinc (as zinc sulphate) equiv. to elemental iron 50 mg; in a syrupy base. Pack: 200 mL. OTC ZOLOFER® (Maydon)
4 mg per 5 mL. Pack:100 mL; 150 mL. Syrup, Ferrous glycine sulphate 275 mg, L-histidine
OTC REMYTONE® (Bond)
Pack: 100 mL; 200 mL HCI monohydrate 4 mg, L-lysine HCI 25 mg, thiamine
OTC NECTAFER-Z® (Nectar Healthcare) Capsule, Ferrous fumarate 150 mg equiv. to elemen-
Dose: Children (7–12 years): One teaspoonful, three HCI 5 mg, riboflavin ( as riboflavin sodium phos-
Syrup, Iron (III)hydroxide polymaltose complex tal iron 49 mg, L-histidine HCl H2O 25 mg, glycine
times daily. phate) 3 mg, pyridoxine HCI 1.5 mg, folic acid 0.5
(equiv. to elemental iron) 50 mg, folic acid 0.5 mg, 10 mg, thiamine nitrate 5 mg, riboflavine 3 mg, pyr-
mg, nicotinamide 25 mg, cyanocobalamin 2.5 mcg,
OTC LIPROFER® (Pharmgate) cyanocobalamin (vitamin B12) 7.5 mcg, zinc sulphate idoxine HCI 1.5 mg, cyanocobalamin 2.5 mcg, folic
dexpanthenol 2.5 mg per 10 mL; caramel colour.
Syrup, Ferric ammonium citrate 150 mg, Protein (equiv. to elemental zinc) 0.5 mg per 5 mL. acid 0.5 mg, ascorbic acid 40 mg; hard gelatin cap.
hydrolysate liquid (20%) 1 g, L-lysine monohy- Pack: 200 mL Pack: 30’s
dro-chloride 50 mg, Niacinamide 45 mg, D-pan- Liquid, Ferrous glycine sulphate 275 mg, L-histidine FERROUS SALT plus FOLIC ACID
OTC NOMATONE® (Nomagbon) Indications: Prevention of iron and folic acid
thenol 5 mg, Pyridoxine HCl 1.5 mg, Folic acid 1.0 HCl H2O 25 mg, thiamine HCI 5 mg, roboflavin 3
Syrup, Ferric ammonium citrate 400 mg, Vitamin B1
mg, Cyanocobalamin 7.5 mcg, Zinc sulphate (10 mg mg, pyridoxine HCI 1.5 mg, nicotinamide 25 mg, deficiencies in pregnancy.
2.5 mg, Vitamin B2 0.5 mg, Vitamin B6 1 mg, Vitamin
elemental Zn) 44 mg. dexpanthenol 2.5 mg, cyanocobalamin 2.5 mcg, Precautions: Low doses of folic acid in the
B12 5 mg, Folic acid 0.5 mg, Vitamin C 5 mg, Nico-
EMDEX
Pack: 200 mL. folic acid 0.5 mg combination preparations above are inade-
tinamide 5 mg per 5 mL; dark brown viscous syrup.
OTC MD-12® (O’Nell) Pack: 200 mL (in glass bottle) OTC REVITONE® (Pharma–Deko) quate for treatment of megaloblastic anaemia;
Syrup, Ferric ammonium citrate 70 mg (eq. to ele- Syrup, Ferrous gluconate 200 mg, vitamin B1 0.2 overdosage: see section 19.2.4; interactions:
OTC OROFER® (Apple)
mental iron 14 mg), vitamin B12 20 mcg, folic acid
Capsule, Iron (III) polymaltose complex equiv. to
mg, vitamin B2 0.16 mg, cyanocobalamin 0.25 mg. Appendix 1.
0.5 mg per 5 mL. Pack: 200 mL. Adverse effects: see Ferrous salts.
elemental iron 100 mg, folic acid 550 mcg.
OTC Mecure’s Blood Tonic (Mecure) Pack: 10’s. OTC RGI Ferrous Sulfate (Richygold) Dose: Severe anaemia, by mouth, ADULT
Tablet, Ferrous sulfate BP 200 mg; red s-c tab. Syrup, Iron (III) polymaltose complex equiv. to ele- Tablet, Dried ferrous sulfate 200 mg equiv. to 65 mg elemental iron 120 mg daily with folic
200 mg – 1 x 1000’s. mental iron 50 mg per 5 mL. elemental iron; s-c tab. acid 400 µg daily for 3 months; CHILD
Syrup, Vitamin B12 0.005 mg, Folic acid 0.5 mg, Ferric Pack: 150 mL bottle. <2 years elemental iron 25 mg daily
OTC RHYDRON® (Mark)
ammonium citrate 200 mg (40 mg elemental iron) Dose: Adult: 5 mL 2-3 times daily with folic acid 100–400 µg daily for 3
Syrup, Iron choline citrate 310 mg, Folic acid 0.75 mg,
per 5 mL; brown syrup Child: 5 mL 1-2 times daily months, 2–12 years elemental iron 60
Cyanocobalamin 3.5 mcg, L-lysine monohydrochlo-
Pack: 200 mL. Infant: Initially 2.5 mL 1-2 times daily; may
ride 70 mg per 5 mL. mg daily with folic acid 400 µg daily
be increased to 5 mL 1-2 times daily if
OTC MEKOVITA-IRON® (Neros)
necessary.
Pack: 200 ml for 3 months
Capsule, Ferrous fumarate 150 mg (equiv.to elemen- Dose: Adult: 10-15 ml once daily. Prevention of iron and folic acid
tal iron 49 mg), L-histidine HCl H2O 4 mg, L-lysine HCl
Note: Syrup may be mixed with fruit or vege- Child (5-12 years): 5-10 ml once daily; 2-5
table juices or other liquids if desired. deficiencies in pregnancy, by mouth,
25 mg, Glycine 10 mg, Thiamine nitrate 5 mg, Ribofla- years, 5 ml once daily. ADULT the equivalent of about 100
vin 3 mg, Pyridoxine HCl 1.5 mg, Cyanocobalamine OTC OSTOFER® (Sterling drug) OTC SULFETONE® (Fil Pharma) mg elemental iron with 350–400 µg
2.5 mcg, Folic acid 0.5 mg, Ascorbic acid 40 mg Syrup, Iron (III) hydroxide polymaltose complex
Pack: 3 x 10`s (in blisters)
Tablet, Ferrous sulfate (dried) 200 mg (equiv. 60 mg folic acid daily throughout pregnancy.
equiv. to Folic acid 0.750 mg per 5 mL; flavour iron); s-c tab.
Syrup, Ferrous sulphate 7H20 6000 mg, L-histidine syrupy base. OTC Ferrous salt plus Folic acid (WMF 10.1)
200 mg – 100; 1000.
HCl H2O 80 mg, L-lysine HCl 500 mg, Glycine 200 Tablets, Ferrous salt equiv. to 60 mg iron, folic acid
mg, Thiamine HCl 100mg, Riboflavin (as riboflavin OTC Pharchem Blood Tonic (Pharchem) OTC TATORON® (Global Healthcare) 400 µg.
phosphate) 60 mg, Pyridoxine HCl 30 mg, Nicotina- Oral liquid, Ferric ammonium citrate 69 mg (equiv. to Syrup, Ferric ammonium citrate 200 mg (equiv. to
mide 500 mg, Cyanocobalamine 50 mcg, Folic acid 14 mg elemental iron), vitamin B1 1 mg, vitamin B6 2 elemental iron 35 mg), Folic acid 500 mcg, Vitamin OTC Evergreen Folic acid and Vitamin B12 (Carrot-
10mg, Dexpanthenol 50 mg per 200 mL. mg, folic acid 0.25 mg, nicotinamide 15 mg per 5 mL. B12 5 mcg, Vitamin B12 mg, Vitamin B2 1.5 mg. Top)
Pack: 200 mL bottle. Pack: 200 mL. Tablet, Folic acid 800 mcg, Vitamin B3 mcg.
Pack: 200 mL.
Dose: Adult, 10 mL 3 times daily after meals.Child: Dose: Adult, 15 mL 2 times daily. Dose: One tablet to be taken daily
OTC MEROMIN® (Sterling drugs) 5 mL 3 times daily after meals.
OTC TONIVITE® (Crystal) OTC FE-FOLIC® (Tamar & Pharez)
Syrup, Ferous glycine sulphate (equiv. to elemental
OTC PHARMAGLOBIN® (Pharmabox) Capsule, Ferric ammonium citrate 200 mg, vitamin Capsule, Dried Ferrous Sulphate + Folic Acid
iron 47 mg) 275 mg, L-histidine HCl H2O 4 mg,
Syrup, Ferric ammonium citrate 250 mg (eq. to B12 5 mcg, folic acid 0.5 mg Pack: 3 x 10’s
L-Lysine HCI 25 mg, , Thiamine HCl (as Riboflavin
sodium phosphate) 3 mg, Pyridoxine HCl 1.5 mg, element iron 50 mg), folic acid 0.5 mg, vitamin B12 5 Pack: 30’s POM FEROSOFT-FA® (CG Biostadt)
Folic acid 0.5 mg, Nicotinamide 25 mg, Cyanoco- mcg, sorbitol solution (70%) 1.5 g per 15 mL. Syrup, Ferric ammonium citrate 200 mg, vitamin B12 Chewable tablet, Iron (III) hydroxide polymaltose
balamin 2.5 mcg, Dexpanthenol 2.5 mg per 10 mL; Pack: 200 mL 5 mcg, folic acid 0.5 mg per 5 mL. complex eq. to elemental iron 100 mg, folic acid
flavour syrupy base. Dose: Adult, 15 mL 2 times daily. Pack: 200 mL 0.35 mg
OTC RANFERON-12® (Ranbaxy) OTC ZOGLOBIN® (Emzor) Pack: 4 x 5’s
OTC MIRAMALT® (Miraflash)
Capsule, Ferrous fumarate 305 mg (equiv. elemental Syrup, Ferrous glycine sulphate 275 mg (Equivalent Dose: Treatment of deficiency, Adult, child (>12
Syrup, Protein Hydrolysate (20%) 1 g, Ferric ammo-
iron 100 mg), folic acid 0.75 mg, cyanocobalamin 5 to elemental iron 47 mg), L-Histidine Hcl H20 4 mg, years), nursing & lactating women, 1-3 tabs
nium citrate (elemental iron 32 mg) 150 mg, Zinc
mcg, ascorbic acid 75 mg, zinc sulfate 5 mg. l-Lysine HcL 25 mg, Thiamine HCl 5 mg, Riboflavin(as daily. Prevention of deficiency, 1 tablet daily.
sulphate 44 mg, Folic acid 1 mg, Cyanocobalamin
Pack: 30’s; 120’s.
POM FOLIRON® (Medreich) received supplemental erythropoietin therapy; 400–500 µg daily before conception logical involvement, by IM injection,
Capsule, Dried ferrous sulfate 150 mg (equiv. 47 mg Iron deficiency because of other reasons e.g. be- and during the first twelve weeks of ADULT and CHILD initially 1 mg on
elemental iron), Folic acid 500 mcg; clear, transpar- fore and after sugery, final stages of pregnancy, pregnancy alternate days until no further im-
ent sustained-release capsule marked ‘FOLIRON’ intolerance, non-responsiveness or non-com- Prevention of recurrence of neural tube provement occurs, then 1 mg every
containing mixture of red, pale-yellow and white
pliance to oral iron therapy, malabsorption. defect, by mouth, ADULT 5 mg daily 2 months.
pellets (‘tiny time pills’).
Pack: 15’s; 30’s; 250’s; 1000’s. Contra-indications: Iron overload, hypersen- (reduced to 4 mg daily, if suitable Prophylaxis of macrocytic anaemias, by
sitivity to iron sucrose complex or any of its preparation available) from at least 4 IM injection, ADULT and CHILD 1 mg
OTC JADURON® (Onifam) ingredients, and non-iron deficiency anemias. weeks before conception until twelfth every 2–3 months.
Tonic, Iron 160 mg, vitamin B12 7.5 mg, folic acid
Precautions: Periodic monitoring of hemoglo- week of pregnancy. Tobacco amblyopia and Leber optic
0.5 mg
Pack: 200 mL
bin, hematocrit, serum ferritin and transferrin OTC Folic acid (WMF 10.1)
atrophy, by IM injection, ADULT and
saturation recommended; pregnancy, child, Tablets, Folic acid 1 mg, 5 mg. CHILD 1 mg daily for 2 weeks, then
OTC VITAFERON® Plus (Leady Pharma) elderly. 1 mg twice weekly until no further
Capsule, Ferric ammonium citrate B.P 65.12 mg Adverse effects: Hypotension, headache, vom- OTC Folic acid (EDL 16.1) improvement, then 1 mg every 1–3
equiv. to 14.0 mg elemental iron), Ferrous Fumarate Tablet, Folic acid 5 mg
iting, nausea, dizziness, joint aches, paresthesia, months.
46.153 mg equiv. to 14.0 mg elemental iron), Folic
abdominal and muscle pain, edema and cardi- OTC Folic acid (Dana)
acid B.P 0.75 mg, Cyanocobalamin B.P. (Vit B12) 2.7 POM Hydroxocobalamin (WMF 10.1)
ovascular collapse, especially when injection is Tablet, Folic acid 5 mg; uncoated tab.
mcg, Thiamine HCl B.P. (Vit B1) 1.5 mg, Riboflavin Injection, Hydroxocobalamin 1 mg/mL; in 1-mL
administered in higher doses or rapidly. Pack: 1000’s (in jar).
plain B.P. (Vit B2) 2.0 mg, Pyridoxine HCl B.P (vit B6), ampoule.
Nicotinamide B.P (Vit PP), Ascorbic acid B.P. (Vit C) Dose: By slow IV injection or infusion, 100 OTC Folic Acid (Emzor)
POM Hydroxocobalamin (EDL 16.1)
30.0 mg, a-Tocopheryl acetate (Vit E) 6.0 mg, Calcium mg iron 1-3 times per week depend- Tablet, Folic acid 5 mg; yellow tab. marked EMZOR.
Injections, Hydrocobalamin 1 mg per mL.
carbonate 23.0 mg equiv., to 92.1 mg of CaOTC ing on the haemoglobin level. The 5 mg – 1000.
Capsule, Ferrous Fumarate (equiv. to 14.0 mg total treatment regimen is 1,000mg in OTC Folic Acid (Evans) IRON DEXTRAN
EMDEX
elemental iron) 46.153 mg, Folic acid B.P 0.75 mg, 10 doses; may be repeated if required. Tablet, Folic acid 5 mg; deep yellow tab.
Cyanocobalamin B.P. (Vit B12) 2.7 mcg, Thiamine HCl Therapeutic category: Iron salt.
B.P. (Vit B1) 1.5 mg, Riboflavin plain B.P. (Vit B2) 2.0 POM FEROSOFT-S® (CG Biostadt) 5 mg – 100; 1000.
Indications: Treatment of microcytic hy-
mg, Ascorbic acid B.P. (Vit C) 30.0 mg, a-Tocopheryl Injection, Ferric sucrose complex (HPL) equiv. to ele- OTC Folic Acid (Juhel) pochromic anaemia resulting from iron defi-
acetate (Vit E) 6.0 mg, Calcium carbonate (equiv., to mental iron 100 mg per 5 mL; an aqueous complex Tablet, Folic acid 5 mg. ciency in whom oral administration is infeasible
92.1 mg of Ca). 23.0 mg, magnesium oxide (equiv. to of iron (III)-hydroxide with sucrose in amps. 5 mg – 1000.
Pack: 5’s
or ineffective.
49.8 mg of Mg) 82.5 mg, manganese sulphate (equiv.
to 4.4 mg of Mn) 12.0 mg, Zinc sulphate (equiv. to OTC Folic Acid (Ulticare-Lyka) Contra-indications: Hypersensitivity to iron
26.7 mg of Zn) 66.0 mg FOLIC ACID Tablet, Folic acid 5 mg. dextran, all anaemias not related with iron
Pack:30’s; 100’s 5 mg – 100; 1000. deficiency, haemochromatosis, haemolytic
Indications: Treatment of folate-deficiency
Tonic, Ferric ammonium citrate (equiv. to 14.0 mg OTC Folic Acid (Vitabiotics) anaemia.
megaloblastic anaemia; prevention of neural
elemental iron) 65.12 mg, Folic acid B.P 0.5 mg, Tablets, Folic acid 5 mg. Precautions: History of allergy, asthma, hepatic
Cyanocobalamin B.P. (Vit B12) 2.5 mcg, Thiamine tube defect in pregnancy (see notes above).
5 mg – 1000’s impairment, rheumatoid arthritis; not recom-
HCl B.P. (Vit B1) 2.0 mg, Riboflavin plain B.P. (Vit B2) Contra-indications: Should never be given
POM Folic acid + B12 (Vitabiotics)
mended in children below 4 months of age; test
1.0 mg, Pyridoxine HCl B.P (vit B6) 2.0, Nicotinamide without vitamin B12 in undiagnosed megalo-
Tablet, Folic acid 5 mg, vitamin B12 dose should be given; elderly.
B.P (Vit PP) 5.0 mg blastic anaemia or other vitamin B12 deficiency
Pack: 100’s Interactions: Decreased effect with chloram-
Pack: 100 mL; 200 mL. states because risk of precipitating subacute
phenicol.
OTC ZEEFEE® (Phillips/Prisma) combined degeneration of the spinal cord; OTC FOLTABS® (Ranbaxy)
Adverse effects: Anaphylaxis with respiratory
Syrup, Elemental iron 40 mg (derived from iron folatedependent malignant disease. Tablet, Folic acid 5 mg.
5 mg – 100; 1000. difficulties and cardiovascular collapse (give
protein succinylate 800 mg), vitamin B12 5 mcg, folic Precautions: Women receiving antiepileptic
test dose); urticaria, leukocytosis, dizziness, fe-
acid 1000 mcg per 15 mL. therapy need counselling before starting folic
Pack: 200 mL bottle. HYDROXOCOBALAMIN ver, headache, pain, sweating; GI disturbances
acid; interactions: Appendix 1.
Dose: 15 mL twice daily. including metallic taste; staining of skin at the
Nursing action: Teach patient dietary sources Synonym: Vitamin B12.
site of I.M. injection, phlebitis; discolouration
OTC ZOGLOBIN® (Emzor) of folic acid: beans, nuts, fruits, fresh vegetable, Indications: Megaloblastic anaemia due to
of urine; arthralgia.
Syrup, Ferrous glycine sulphate (equivalent to ele- organ meats. vitamin B12 deficiency.
Nursing action: Administer a test dose of 0.5
mental iron 47mg) 275mg, L-Histidine Hcl H20 4mg, • Co-administration with oral contraceptives, Precautions: Except in emergencies, should
l-Lysine Hcl 25mg, Thiamine HCl 5 mg, Riboflavin(as mL IV or IM and observe the patient for at least
alcohol may cause increased folic acid de- not be given before diagnosis confirmed;
Riboflavin sodium phosphate) 3mg, Pyridoxine HCl 1 hour before giving the remaining portion;
mand. monitor serum potassium levels—arrhythmias
1.5mg, Folic acid 0.5mg, Nicotinamide 25mg, Cyano- keep adrenaline ready.
• Inform patient that urine may turn bright secondary to hypokalaemia in early therapy.
cobalamin 2.5mcg, Dexpanthenol 2.5mg. • Inject deeply into the upper outer quadrant
yellow. Adverse effects: Nausea, headache, dizziness;
Pack: 200 mL of the buttock (do not give into arm or other
Indications: Treatment of iron deficiency anaemia, Dose: Treatment of folate-deficiency, megalo- fever, hypersensitivity reactions including rash
areas); use the Z-track technique to avoid
megaloblastic anaemia, anaemia due to pregnancy, blastic anaemia, by mouth, ADULT 5 and pruritus; pain at injection site; hypokalae-
leakage into the subcutaneous tissue and
anaemia associated with infections and repeated mg daily for 4 months (in pregnancy mia during initial treatment
staining of the skin; skin staining may also
haemorrhage. continued to term); up to 15 mg daily Dose: Megaloblastic anaemia without neuro-
be minimised by using a separate needle to
may be necessary in malabsorption logical involvement, by IM injection,
withdraw the drug from the ampoule.
FERRIC SUCROSE COMPLEX states. ADULT and CHILD initially 1 mg 3
• IV injection should be handled by an experi-
Indications: Iron deficiency anemia in pa- Prevention of first occurrence of times a week for 2 weeks, then 1 mg
enced clinician and patient should be allowed
tients on chronic hemodialysis and who have neural tube defect, by mouth, ADULT every 3 months.
to rest in a recumbent position for about 15-
Megaloblastic anaemia with neuro-
252 | 6.1.2 Drugs used in neutropenia 6.1.4 Drugs used in sickle cell disease | 253
30 minutes after IV administration to prevent FILGRASTIM ficiency must be evaluated and corrected if Note: The SC maintenance dose is approx. 20-35%
orthostatic hypotension. Synonym: G-CSF; Granulocyte Colony Stmu- necessary; sudden stabbing migraine-like pain lower than the IV dose. When changing from one
• Encourage improved nutrition in rich dietary is a warning of hypertensive crisis; ischaemic route of administration to the other, the same
lating Factor.
iron sources viz meat, dark green leafy vege- heart disease; thrombocytosis; malignant dose should be used and then adjust according to
Indications: See the notes above. weekly haemglobin measurements to keep the Hb
tables, beans, eggs Contra-indications: Hypersensitivity to disease; chronic liver failure; dialysis heparin
within the target range. See lit. for more detailed
Dose: By IM, I.V., a test dose of 0.5 mL (0.25 filgrastim. Avoid in patients with severe con- requirements may increase; pregnancy, information.
mL in infants) should be given prior genital neutropenia (kostmen’s syndrome) breast-feeding.
to starting iron dextran therapy. Interactions: ACE inhibitors (antagonism of POM WEPOX® (Olpharm)
with abnormal cytogenetics. Not to be used to Injections, Erythropoietin 4000 IU, 10000 IU, 20000
See lit. for details. increase the dose of cytotoxic chemotherapy hypotensive effect and increased risk of hy-
IU; in pre-filled syringes.
Note: Administration – Use Z-track tech- beyond established dosage regimen. perkalaemia).
nique for IM administration (deep into the Precautions: Pregnancy and breast-feeding; Adverse effects: Dose-dependent increase
upper outer quadrant of buttock); may be in B.P. or aggravation of hypertension; flu-like
6.1.4 Drugs used in sickle cell disease
monitor leucocyte count, platelet count and
administered IV bolus at rate not exceeding haemoglobin. symptoms such as muscular aches from 60-90 POM DREPANOSTAT® (Bolar)
50mg/minute or diluted in 250-1000 mL NS mins after I.V. injection (may be reduced by Capsule, Hydroxymethylbenzoic acid 10 mg
Adverse effects: Musculoskeletal pain (usually
and infused over 1-6 hours; infuse initial 25 controlled with standard analgesics); urinary giving I.V. injection over 5mins.); headache, 10 mg – 30’s (in box)
mL slowly, observe for allergic reactions; have abnormalities predominantly mild to moder- seizures, rash, oedema; hyperkalaemia; hyper- Pharmacology: Red cells falciformation inhibi-
adrenaline ready. ate dysuria; reversible and dose-dependent sensitivity reactions. tor. Prevents the destruction of falciformed red
elevations of liver enzymes and serum uric Advice to patients: Notify physician if any cells. Lessens any pains.
POM Iron Dextran (EDL 16.1/Restricted List)
acid; rarely, allergic-type reactions; transient severe headache develops. Active absorption at duodenal level. Mainly
Injection, Iron dextran equivalent to 50 mg iron per
mL; in 2-mL amp. decreases in blood pressure (not requiring Nursing action: Do not shake vial. an acetylation reaction and secondarily a
clinical treatment). • Advise patient to avoid hazardous activities glucoro-conjugated reaction at liver level.
EMDEX
POM B-DEXTRON® (Beta Drugs) Elimination is mainly through urinary tract.
Advice to patients: Possible bone pain. until stabilized on medication.
Injection, Iron dextran equal to elemental Iron 50 mg. Indications: Treatment and prevention of
Pack: 5 mL x 100 ampoules. Nursing action: Do not shake vial; not to be Dose: See under the preparations below.
mixed with sodium chloride solutions. sickle cell disease acute crisis in SS, SC, asso-
POM FERODEX® (Standard Generics) POM EPOKINE® (Alpha)
• Give paracetamol to relieve bone pain ciated or not with haemolytic anaemia linked
Injection (IM), Iron dextran complex 250 mg per 5 Injection, Erythropoetin alpha (recombinant) 4000
Dose: By SC injection or IV infusion, 5 mcg IU/0.4 mL. to a thalassaemia.
mL; in water for injection. Contra-indications: Prior hypersensitivity to
(500,000 units)/kg daily started at POM EPOSINO® (Olpharm)
POM Iron Dextran (Pemason) least 24 hours after cytotoxic chemo- hydroxymethylbenzoic acid
Injection, Iron dextran 250 mg per 5 mL; in amps Injection, Epoetin α (recombinant human erythropo- Adverse effects: Very rare cases of cutaneous
therapy, continued until neutrophil etin) 4000 IU, 6000 IU, 10,000 IU; clear transparent
marked “Pemason Iron Dextran” allergies may occur related to individual pre-
Pack: 5 mL x 10 x 10’s
count is in normal range, usually for liquid in vials & pre-filled syringes.
up to 14 days. disposition.
POM Iron Dextran (Pharmabox) POM EPREX® (Janssen-Cilag) Dose: By mouth, Basic treatment of crisis,
Note: To be administered only by those experienced
Injection, Elemental iron (as iron dextran complex) Injection(Vials), Epoetin alfa 2000 units, 4000 units Adults, 3 capsules together thrice a
in its use.
per mL; in 1 mL vials.
50 mg per mL. day.
POM NEUPOGEN® (Swipha) Dose: Anaemia associated with chronic renal failure,
POM ONOPAIN® (Vixa) by SC injection (max. 1 mL per injection site
Children: 2 capsules together thrice
Injection, Filgrastim 300 mcg (30 million units) per
Injection, Iron dextran 250 mg per 5 mL. mL; 480 mcg (48 million units) per 1.6 mL. ) or IV injection over 1-5 minutes, initially a day
300 mcg/mL in 1ml vial. 50 units/kg 3 times per week; adjusted Infants: 1 capsule thrice a day mixed
6.1.2 Drugs used in neutropenia 480 mcg/1.6 mL in 1.6 mL vial. according to Hb response and urgency of with a spoonful of food.
Filgrastim (recombinant human granulocyte anaemia correction in steps of 25 units/kg Prevention of crisis, Adults and chil-
– colony stimulating factor) is indicated for the 6.1.3 Drugs used in hypoplastic, at 4-week intervals; max. dose 240 units/kg dren, 2 capsules together twice a day
haemolytic, and 3 times per week. Infants: 1 capsule twice a day mixed
reduction in the duration of neutropenia and
Maintenance dose: The dose has to be
the incidence of febrile neutropenia in patients renal anaemias with a spoonful of food.
adjusted individually to maintain a packed
treated with established cytotoxic chemo- cell volume of 30-35 volume % (i.e., Hb
therapy for non-myeloid malignancy and the EPOETIN ALFA level of 10-12 g /100 mL). The maintenance 6.2 Drugs affecting coagulation
reduction in the duration of neutropenia and Synonym: EPO; Erythropoietin; r-HuEPO. dose is approx. half the dose administered 6.2.1 Anticoagulants
its clinical sequelae in patients undergoing Therapeutic category: Recombinant human in the correction phase. Cancer patients on 6.2.2 Reversal of anticoagulation
myeloblastic therapy followed by bone marrow erythropoietin. Chemotherapy, by SC injection (max.1 mL Anticoagulants are used to prevent thrombus
transplantation. Indications: Anaemia associated with eryth- per injection site), initially 150 units/kg 3 formation or extension of an existing throm-
ropoietin deficiency in chronic renal failure; times per week for up to 3 months. Monitor
In patients, children or adults, with severe bus in the slower-moving venous side of the
haematocrit weekly when adjusting dose.
congenital cyclic or idiopathic neutropenia to increase the yield of autologous blood in circulation, where the thrombus consists of a
Withhold dose if haematocrit rises above
with AUC of less than or equal to 0.5 x 10 a/L normal individuals and to shorten the period of 40% until it falls to 36%; then reduce dose fibrin web enmeshed with platelets and red
and a history of severe or recurrent infections, anaemia in cancer patients on chemotherapy. by 25% when treatment is resumed and cells. They are therefore used widely in the
long-term administration of filgrastim is in- Contra-indications: Hypersensitivity to al- adjust to maintain the desired haematocrit. prevention and treatment of deep-vein throm-
dicated to increase neutrophil counts and to bumin (human) or mammalian cell-derived Reduce dose if the initial dose of r-HuEPO bosis in the legs, prophylaxis of embolization
reduce the incidence and duration of infection products; uncontrolled hypertension. includes a very rapid rise in haematocrit in rheumatic heart disease and atrial fibrillation
related incidents. Precautions: Porphyria, hypertension, history (more than 4% in any 2-week period). and to prevent thrombi forming on prosthetic
of seizures; prior to and during therapy, other Doses in excess of 150 units/kg 3 times daily heart valves.
not recommended.
causes of anaemia such as iron or folate de-
254 | 6.2.1 Anticoagulants 6.2.1 Anticoagulants | 255
Heparin is a parenteral anticoagulant that intravenous injection. Indications: Prevention of various throm- the arterial line of the circuit at the
initiates anticoagulation rapidly but has a short ANTICOAGULANTS IN PREGNANCY bo-embolic diseases following orthopaedic and beginning of the dialysis session. This
duration of action. The low molecular weight Oral anticoagulants are teratogenic and should general surgery; treatment of deep-vein throm- is usually sufficient for a four hour
heparins have a longer duration of action. not be given in the first trimester of pregnancy. bosis; prevention of clotting in extracorporeal session but if fibrin rings are found for
For patients at high risk of bleeding, heparin Women at risk of pregnancy should be warned circulation during haemodialysis. example after a longer than normal
is more suitable than low molecular weight of this danger since stopping warfarin before Contra-indications: Hypersensitivity to either session, a further dose of 0.5-1 mg/kg
heparin because its effect can be terminated the sixth week of gestation may largely avoid enoxaparin, heparin or its derivatives;acute may be given.
rapidly by stopping the infusion. the risk of fetal abnormality. Oral anticoagu- septic endocarditis, haemorrhagic stroke, Note: How to administer:
For the treatment of deep venous thrombosis lants cross the placenta with the risk of placen- conditions with a high risk of uncontrolled 1. Hold syringe with needle pointing away,
and pulmonary embolism heparin is given as tal or fetal haemorrhage, especially during the haemorrhage. slightly raised.
an intravenous loading dose followed by con- last few weeks of pregnancy and at delivery. Precautions: Renal or hepatic insufficiency, 2. Rotate syringe until numbers are clearly
tinuous intravenous infusion (using an infusion Therefore, if at all possible, oral anticoagulants history of peptic ulcer, arterial hypertension, visible.
pump) or by intermittent SC injection. An oral should be avoided in pregnancy, especially in diabetic retinopathy, recent CNS or oph- 3. Remove needle cap.
anticoagulant is started at the same time as the first and third trimester. Difficult decisions thalmologic surgery, spinal anaesthesia and 4. Depress plunger until edge of black plunger
heparin. The heparin needs to be continued may have to be made, particularly in women epidural block; history of heparin-induced is level with marking corresponding to
for at least 5 days, until the oral anticoagulant with prosthetic heart valves or with a history thrombocytopenia; avoid using low molecular recommended dose.
has taken effect and the INR (international of recurrent venous thrombosis or pulmonary weight heparins 5. Insert whole lenght of the needle vertically
normalized ratio) has been in the therapeutic embolism. interchangeably; avoid use in lactation and into a skin fold ( of the abdomen) held
range for 2 consecutive days. Laboratory mon- HAEMOPHILIA during the first trimester of pregnancy. Do between the thumb and index finger.
itoring is essential on a daily basis. Heparin is Desmopressin [not included on WHO Model not administer IM. 6. Do not release the skin fold until the
also used in regimens for the management List] by injection may aid haemostasis and be Interactions: Avoid co-administration with injection is complete.
EMDEX
of myocardial infarction, the management useful in mild forms of haemophilia. For minor substances that enhance the risk of haem- 7. Do not rub the injection site.
of unstable angina, acute peripheral arterial procedures including dental surgery, it may orrhage such as systemic salicylates, aspirin,
occlusion and in dialysis. circumvent the need for factor VIII. For the use systemic NSAIDs, ticlopidine. Use cautiously POM Enoxaparin (EDL 16.2)
Injection, Enoxaparin 100 mg per mL.
In patients undergoing general surgery, of factor VIII and factor IX in haemophilia, see with oral anticoagulants, systemic glucocorti-
low-dose heparin by SC injection is used to section 6.4.2. coids , dextran 40. POM CLEXANE® (Sanofi-Aventis)
prevent postoperative deep-vein thrombosis Adverse effects: Heamorrhage, thrombocyto- Injection, Enoxaparin 100 mg per mL; in 0.2 mL (20
and pulmonary embolism in high risk patients 6.2.1 Anticoagulants penia, haematoma, irritation at injection site, mg), 0.4 mL (40 mg), 0.6 mL (60 mg) and 0.8 mL (80
(those with obesity, malignant disease, history Nursing action: – Anticoagulants erythema, ecchymosis; rarely allergic reactions mg) ready-to-use prefilled syringes.
20 mg/0.2 mL – 2’s
of deep-vein thrombosis or pulmonary em- • Give at same time each day to maintain steady which may require stopping therapy.
40 mg/0.4 mL – 2’s; 10’s
bolism, patients over 40 years, those with an blood levels. Nursing action: Administer by deep SC in- 60 mg/0.6 mL – 2’s
established thrombophilic disorder or those • Do not massage area or aspirate when giv- jection; avoid IM injection which may cause 80 mg/0.8 mL – 2’s
undergoing major or complicated surgery). It ing SC injection; give in abdomen between bleeding.
is also of value in high-risk medical patients, • The prefilled syringe is ready for immediate POM CUTENOX® (Fidson)
pelvic bone, rotate sites; do not pull back
Injection, Enoxaparin sodium 100 mg per mL; in 0.2
for example obesity, heart failure, when con- on plunger; leave in for 10 sec; apply gentle use. Injection should be made preferably
mL (20 mg), 0.4 mL (40 mg), 0.6 mL (60 mg) and 0.8
fined to bed. pressure for 1 min. when the patient is lying down, in the sub- mL (80 mg) ready-to-use prefilled syringes.
If haemorrhage occurs it is usually sufficient • Avoid all IM injections that may cause cutaneous cellular tissue of the abdomen.
to withdraw heparin, but if rapid reversal of bleeding. • Instruct patient to avoid use of aspirin con- HEPARIN SODIUM
the effects of heparin is required, protamine • May withhold drug during active bleeding taining products due to increased risk of
Indications: Treatment and prophylaxis of
sulfate is a specific antidote. e.g. menstruation, depending on condition. bleeding.
deep-vein thrombosis and pulmonary em-
Oral anticoagulants take at least 48–72 hours • Monitor patient’s blood parameters: Hct, • Advise patient to use soft toothbrush to
bolism.
for the anticoagulant effect to develop fully; if platelets, occult blood in stools, prothrom- avoid bleeding gums; to report any signs of
Contra-indications: Hypersensitivity to hep-
an immediate effect is needed, heparin must bin time. bleeding.
arin; haemophilia and other haemorrhagic
be given concomitantly. Warfarin is indicated • Watch for signs of increasing B/P; bleeding Dose: By SC injection, Prevention of deep-vein
disorders, thrombocytopenia, peptic ulcer,
in DVT, pulmonary embolism, for patients with gums, petechiae, ecchymosis; black, tarry thrombosis, patients with moderate risk
recent cerebral haemorrhage, severe hyperten-
atrial fibrillation who are at risk of embolization stools; haematuria; fever, skin rash, urticaria. of thrombo-embolism, 20 mg (0.2 mL)
sion, severe liver or renal disease, after major
and for those with mechanical prosthetic • Tell patient to report any signs of bleeding: 2 hours before surgery, then 20 mg
trauma or recent surgery (especially to eye or
heart valves (to prevent emboli developing gums, under skin, urine, stools. (0.2 mL) every 24 hours for 7-10 days;
nervous system), acute bacterial endocarditis.
on the valves); oral anticoagulants should not • Advise patient to avoid OTC medications Patients with high risk of thrombo-
Precautions: Hepatic impairment (Appendix
be used in cerebral thrombosis or peripheral due to adverse drug interactions, except on embolism, 40 mg (0.4 mL) 12 hours
5) and renal failure (Appendix 4); elderly;
arterial occlusion as first-line therapy. The main doctor’s prescription. before surgery, then 40 mg (0.4 mL)
hypersensitivity to low molecular weight
adverse effect of oral anticoagulants is haem- • Instruct patient to use soft-bristle toothbrush every 24 hours for 7-10 days.
heparins; spinal or epidural anaesthesia—risk
orrhage. Prothrombin time (usually reported as to avoid bleeding gums, avoid contact sports Treatment of deep-vein thrombosis,
of spinal haematoma; pregnancy (Appendix
INR, international normalized ratio) should be and use electric razor. 1 mg/kg every 12 hours and during
2); diabetes mellitus, acidosis, concomitant
checked on a daily basis initially then at longer 10 days.
potassium-sparing drugs—increased risk of
intervals depending on response. ENOXAPARIN Prevention of clotting in extracorpor-
hyperkalaemia; interactions: Appendix 1.
If severe haemorrhage occurs, stop warfarin Therapeutic category: Anticoagulant. eal circulation during haemodialysis,
Adverse effects: Immune-mediated thrombo-
and give phytomenadione (vitamin K) by slow usually 1 mg/kg; to be introduced in
256 | 6.2.1 Anticoagulants 6.2.2 Reversal of anticoagulation | 257
cytopenia usually developing 6 to 10 days after Injection, Heparin sodium (derived from bovine prothrombin time should be deter- injection, ADULT 10–20 mg; severe
commencement of therapy (requires immediate intestinal mucosa) 10 USP units per mL; sterile mined before the initial dose is given. haemorrhage, ADULT, by slow IV
withdrawal of heparin); haemorrhage, skin necro- solution in amp. Prophylaxis and treatment of throm- injection, 5–10 mg.
sis, hypersensitivity reactions including urticaria, Pack: 2 mL (in amp.) bo-embolic disorders, by mouth, Haemorrhagic disease of the new-
Indications: Heparin Lock Flush Sodium USP is
angioedema and anaphylaxis; osteoporosis after ADULT usual induction dose is 10 born, treatment, by IV or IV injection,
intended to maintain patency of an indwelling
prolonged use and rarely alopecia. venipuncture device designed for intermittent in- mg daily for 2 days, according to the NEONATE 1 mg with further doses if
Nursing action: Do not massage area or jection or infusion therapy or blood sampling. May individual patient; the subsequent necessary at 8-hour intervals.
aspirate when giving SC injection; avoid IM be used following initial placement of the device in dose depends upon the prothrombin Haemorrhagic disease of the newborn,
injection which may cause bleeding. the vein. Not to be used for anticoagulant therapy time; the usual daily maintenance prophylaxis, by IM injection, NEONATE
• Inspect the patient’s gum for bleeding and in the neonate. dose is 3–9 mg taken at the same 0.5–1 mg as single dose or by mouth,
regularly; notify physician immediately of time each day. 2 mg followed by a 2nd dose after
petechiae, epistaxis, bruises on arms or legs, WARFARIN SODIUM 4–7 days and for breastfed babies a
POM Warfarin sodium (WMF 10.2)
malaena stools, haematuria, haematemesis. Indications: Prophylaxis of embolization in Tablets, Warfarin sodium 1 mg, 2 mg, 5 mg. third dose after 1 month.
• Tell patient to avoid OTC medications contain- rheumatic heart disease and atrial fibrillation; POM Phytomenadione (WMF 10.2)
ing aspirin and other salicylates. prophylaxis after insertion of prosthetic heart POM Warfarin sodium (EDL 16.2)
Tablets, Warfarin sodium 1 mg, 5 mg. Tablet, Phytomenadione 10 mg.
• Withhold drug during active bleeding as in valve; prophylaxis and treatment of venous Injection, Phytomenadione 10 mg/mL; in 5-mL
menstruation. thrombosis and pulmonary embolism; tran- POM Warfarin (Alpha) ampoule.
• Advise patient to use soft toothbrush to sient ischaemic attacks. Tablets, Warfarin sodium 1 mg, 3 mg, 5 mg.
1 mg – 28’s POM Phytomenadione (EDL 4.2)
avoid bleeding gums; to report any signs of Contra-indications: Pregnancy (see notes Injection, Phytomenadione 10 mg per mL; in 1-mL
3 mg – 28’s
bleeding. above and Appendix 2); peptic ulcer, severe amp.
5 mg – 28’s
Dose: Treatment of deep-vein thrombosis and hypertension, bacterial endocarditis. 5 mg – 500’s.
EMDEX
pulmonary embolism: by IV injection, Precautions: Hepatic impairment (Appendix See the preparations under section 6.5
ADULT loading dose of 5000 units 5) or renal failure (Appendix 4), recent surgery,
6.2.2 Reversal of anticoagulation
(10 000 units in severe pulmonary breastfeeding (Appendix 3); avoid cranberry PROTAMINE SULFATE
embolism) followed by continuous juice (risk of potentiating anticoagulant effect); PHYTOMENADIONE Indications: Antidote to overdosage with
IV infusion of 15–25 units/kg/hour or interactions: Appendix 1. heparin.
Indications: Antagonist to warfarin; proph-
by SC injection of 15 000 units every Adverse effects: Haemorrhage; hypersensi- Precautions: If used in excess protamine has
ylaxis against haemorrhagic disease of the
12 hours; laboratory monitoring is tivity, rash, alopecia, diarrhoea, unexplained an anticoagulant effect; allergic reactions
newborn.
essential, preferably on a daily basis drop in haematocrit, ‘purple toes’, skin necrosis, increased in persons at risk including previous
Precautions: Reduce dose in elderly; hepatic
and dose adjusted accordingly; by IV jaundice, hepatic dysfunction, nausea, vomit- treatment with protamine or protamine insulin,
impairment; not an antidote to heparin; preg-
injection, SMALL ADULT and CHILD, ing and pancreatitis. fish allergies, men who are infertile or who have
nancy (Appendix 2); interactions: Appendix 1.
lower loading dose, then by continu- Advice to patients: Do not take with food; had a vasectomy.
Adverse effects: Hypersensitivity reactions
ous IV infusion, 15–25 units/kg/hour report any signs of bleeding; avoid hazardous Adverse effects: Nausea, vomiting, lassitude,
including flushing, dyspnoea, bronchospasm,
or by SC injection, 250 units/kg every activities; use soft tooth brush; urine may turn flushing, hypotension, bradycardia, dyspnoea,
dizziness, hypotension and respiratory or
12 hours. red/orange; be sure of other drugs and foods allergic reactions (including angioedema,
circulatory collapse which may be due to
Prophylaxis in general surgery, by SC to avoid. Notify physician if urine turns dark anaphylaxis).
polyethoxylated castor oil surfactant in some
injection, ADULT 5000 units 2 hours brown or if red or tar black stools occur. Nursing action: For IV use only; administer
injection formulations rather than due to
before surgery, then every 8–12 Nursing action: Give alone and not with food slowly because rapid IV infusion causes hy-
phytomenadione.
hours for 7 days or until patient is (food and enteral feeding that contain vita- potension.
Nursing action: Check the brand name labels
ambulant (monitoring not needed); min K may cause inadequate anticoagulation • Monitor vital signs continually.
for administration route restrictions, e.g., Ko-
during pregnancy (with monitoring) due to the neutralizing effect of vitamin K on • Protamine sulfate may act as anticoagulant
nakion® MM may be admnistered by slow IV
5000–10 000 units every 12 hours warfarin); may give tablet whole or crushed. in very high doses.
injection or by IV infusion in D5W but not for
(important: not intended to cover • Avoid IM injection that may cause bleeding; • Observe for heparin rebound associated with
IM injection. While Konakion® may be admin-
prosthetic heart valve management also avoid ear-piercing, circumcision; do not anticoagulation and bleeding.
istered by IM or slow IV injection but not for IV
in pregnancy, which requires special- give during active bleeding e.g. menstruation. Dose: Heparin overdose, by IV injection over
infusion. It contains polyethoxylated castor oil
ist management). • Advise patient to use soft toothbrush to approximately 10 minutes, 1 mg
which should not be diluted.
POM Heparin sodium (WMF 10.2) avoid bleeding gums; to report any signs of neutralizes 80–100 units heparin
• Assist with checking prothrombin time (PT)
Injection, Heparin sodium 1000 units/mL, 5000 units/ bleeding namely bleeding gums, bruises on when given within 15 minutes; if
to determine dosage effectiveness.
mL, 25 000 units/mL; in 1-mL ampoules. arms or legs, petechiae, nosebleeds, melena, longer time, less protamine needed
• Observe patient closely for signs of adverse
tarrystools, haematuria, haematemesis. as heparin is rapidly excreted.
POM Heparin sodium (EDL 16.2) reactions viz weakness, dyspnoea, tachycar-
Female patient should report if menses is
Injections, Heparin sodium 1000 units, 25000 units dia and hypotension which may gradually POM Protamine sulfate (WMF 10.2)
per mL; in amps. heavier than usual.
progress to shock; report them to physician. Injection, Protamine sulfate 10 mg/mL; in 5-mL
• Watch for skin rash and fever; may indicate ampoule.
POM Heparin (Alpha) Dose: Warfarin-induced hypoprothrombinae-
adverse reaction.
Injection, Heparin sodium 5000 IU per mL; 5 mL vials mia; no bleeding or minor bleeding, by POM Protamine (EDL 4.2)
• Advise patient to avoid the use of other drugs
Heparin Lock Flush Solution
slow IV injection, ADULT 500 µg or by Injection, Protamine sulfate 10 mg per mL; in 5-mL
except on prescription; to avoid hazardous
mouth, ADULT up to 5 mg; moderate amp.
POM CLOTFLUSH® (Phillips/Prisma) activities.
haemorrhage, by mouth or by IM POM Protamine (Alpha)
Dose: NOTE: Wherever possible, the base-line
258 | 6.3 Antifibrinolytics and haemostatics 6.4 Blood products and plasma substitutes | 259
Injection, Protamin sulfate 10 mg per mL; in 5-mL I.V. slowly over 1 hour to avoid hypotension Note: For IV infusion, tranexamic acid injection may secretion of antidiuretic hormone.
amp. (dilution is in NS or D5W). be mixed with most solutions for infusion such as When fluids are administered intravenously
• Parenteral drug product should be inspected electrolyte solutions, carbohydrate solutions, amino for more than 24 hours, potassium chloride is
Menadione
visually for particulate matter and discolour- acid solutions and Dextran solutions. The mixture required to prevent potassium depletion. In
POM KEMI®-3 (Beta Drugs) should be prepared the same day the solution is
ation prior to administration. order to avoid serious arrhythmias, especially
Injection, Menadione sodium bisulfite. to be used. Heparin may be added to tranexamic
Pack: 2 mL x 100 amps. • Teach patient/family to report signs of bleed- acid injection. Tranexamic acid injection should in patients with impaired renal function, the
Indications: For the prevention and treatment of ing in skin or stools (melaena). NOT be mixed with blood. The drug is a synthetic required dose of potassium should be de-
haemorrhage or threatened haemorrhage as a result • Advise patient to change position slowly to amino acid, and should NOT be mixed with solutions termined, whenever possible, by monitoring
of severe hypoprothrombinaemia; necessary for the minimise orthostatic hypotension. containing penicillin. plasma concentrations of potassium.
production of blood clotting factors. Dose: Acute bleeding syndrome due to POM TREXAMIN® (CG Biostadt)
See also section 6.8 (solutions correcting water,
elevated fibrinolytic activity, Adult, by Capsules, Tranexamic acid 250 mg, 500 mg electrolyte, and acid-base disturbances).
6.3 Antifibrinolytics and haemostatics mouth, 5 g during first hour; followed 250 mg – 100’s (in blister)
Aminocaproic Acid or Epsilon Aminocaproic continuously by 1 g per hour for ap- 500 mg – 20’s (in blister) 6.4.1 Plasma substitutes
Acid (EACA) is a synthetic inhibitor of fibrinol- prox. 8 hours or until bleeding stops. Dose: By mouth, Adult, 500-1000 mg 3-4 times daily; Dextran 70 and polygeline are macromolecu-
By IV infusion, 4-5 g in 250 mL of dosage adjustment based on patient’s age
ysis used clinically as adjunctive therapy in lar substances which are metabolized slowly;
diluent during first hour; followed by and severity of symptoms.
haemophilia, as therapy for bleeding from Injections, Tranexamic acid 250 mg, 500 mg per 5 they may be used to expand and maintain
fibrinolytic therapy, and as prophylaxis for continuous infusion at the rate of 1g blood volume in shock arising from conditions
mL; in amps.
rebleeding from intracranial aneurysms. per hour in 50 mL of diluent; continue such as burns or septicaemia. They are rarely
250 mg/5 mL x 10’s
for 8 hours or until bleeding stops. 500 mg/5 mL x 10’s. needed when shock is due to sodium and
It is rapidly absorbed orally and is cleared from Max. daily dose (by mouth or I.V.):
the body by the kidney. The usual oral dose Dose: By IV or IM injection, 250-500 mg daily; may water depletion as, in these circumstances,
30 g. be given in 1-2 divided doses. the shock responds to water and electrolyte
EMDEX
of EACA is 6 g 4 times a day. When the drug Note: In the management of acute bleeding syn-
is administered intravenously, a 5 g loading POM XAMIC® (Zoomota) repletion.
dromes, oral dosage regimens are the same as the
dose should be infused over 30 minutes to I.V. dosage regimens. Diluents for I.V. infusion include Injection, Tranexamic acid BP 500 mg. Plasma substitutes should not be used to
avoid hypotension. dextrose 5% or 0.9% sodium chloride. Rapid I.V. 500 mg – 5 mL x 5’s (in amps). maintain plasma volume in conditions such
injection (IVP) should be avoided since hypotension, Dose: By IV injection, 10 mg/kg b.wt together with
Adverse effects of the drug include intravascu- as burns or peritonitis where there is loss of
bradycardia, and arrhythmia may result. replacement therapy.
lar thrombosis from inhibition of plasminogen plasma protein, water and electrolytes over
activator, hypotension, myopathy, abdominal POM Aminocaproic acid (EDL 16.3) periods of several days. In these situations,
6.4 Blood products and
discomfort, diarrhoea, and nasal stuffiness. Tablet, Aminocarproic acid (ACA) 500 mg. plasma or plasma protein fractions containing
Injection, Aminocaproic acid 100 mg, Lipid throm-
plasma substitutes
large amounts of albumin should be given.
Tranexamic acid is often prescribed for boplastin (TPT) 2 mg per mL; in 5-mL, 10-mL amps. 6.4.1 Plasma substitutes
excessive bleeding. It is an antifibrinolytic 6.4.2 Plasma fractions for specific use
Plasma substitutes may be used as an imme-
that competitively inhibits the activation of TRANEXAMIC ACID diate short-term measure to treat massive
Fluid requirements must be assessed before, haemorrhage until blood is available, but
plasminogen to plasmin, a molecule respon- Therapeutic category: Antifibrinolytic agent. during and after major surgery. Replacement large volumes of some plasma substitutes
sible for the degradation of fibrin. Fibrin is the Indications: Short-term use (2-8 days) for fluids should correspond as nearly as possible can increase the risk of bleeding by depleting
basic framework for the formation of a blood haemorrhage or risk of haemorrhage in in volume and composition to those lost. coagulation factors. Dextran may interfere with
clot in hemostasis. It has roughly 8 times the increased fibrinolysis. Local fibrinolysis as Blood transfusion is essential to restore oxygen blood group cross-matching or biochemical
antifibrinolytic activity of an older analogue, occurs in: prostatectomy and bladder surgery; carrying capacity when more than 15% of the measurements and these should be carried
Aminocaproic acid menorrhagia; epistaxis; conisation of the cervix; circulating blood volume is lost but should out before the infusion is started.
(Source: http://en.wikipedia.org/wiki/Tranexamic_acid) surgical procedures and dental extractions in be avoided whenever screening for human
haemophiliacs. Long-term management of immunodeficiency viruses and hepatitis B Plasma substitutes are often used in very ill
hereditary angioneurotic oedema. virus is impracticable. Isotonic sodium chloride patients whose condition is unstable. There-
AMINOCAPROIC ACID
Contra-indications: Defective colour vision, solution may be used for short-term volume re- fore, close monitoring is required and fluid
Synonym: Epsilon Aminocaproic Acid. and electrolyte therapy should be adjusted
Therapeutic category: Haemostatic agent. subarachnoid haemorrhage, active intravas- placement. Plasma expanders such as dextran
cular clotting, severe renal failure. 70 or polygeline may be useful. Provided renal according to patient’s condition at all times.
Indications: Severe haemorrhage associated
with excessive fibrinolysis. Precautions: Renal insufficiency (risk of function is maintained, fluid is most simply
accumulation); upper urinary tract bleeding DEXTRANS 70
Contra-indications: Severe renal impairment; replaced by intravenous administration of so-
intravascular coagulation. (increased risk of ureteral obstruction due to dium chloride solution (sodium chloride 9 mg/ Dextran is a representative plasma substitute. Various
Precautions: Renal impairment (reduce dose); clot formation); history of thrombo-embolic mL, 0.9%) or the more physiologically appro- preparations can serve as alternatives (polygeline 3.5%
haemophiliacs. disease. Eye examination recommended priate compound solution of sodium lactate. infusion is considered equivalent).
Interactions: Oral contraceptives (increased during prolonged use. Discontinue if changes In emergencies, there is usually an existing fluid Indications: Short-term blood volume ex-
toxicity). in colour vision occur. Avoid IV injection rate deficit which must be assessed and corrected pansion.
Adverse effects: Diarrhoea, headache, hypo- >1 mL per minute due to risk of hypotension. before surgery. Isotonic glucose/sodium Contra-indications: Severe congestive heart
tension, dizziness, erythema, skin rash, nau- Pregnancy, lactation. chloride mixtures (most commonly glucose failure, renal failure; bleeding disorders such as
sea, heartburn, conjunctival suffusion, nasal Adverse effects: GI disturbances (e.g. nausea, 4%/sodium chloride 0.18%) are preferred in thrombocytopenia and hypofibrinogenaemia.
stuffiness, diuresis, muscle pain and weakness. vomiting, and diarrhoea); giddiness, hypoten- children but injudicious use of such fluids may Precautions: Cardiac disease, liver disease, or
Nursing action: Rapid I.V. administration of sion (due to rapid IV injection). cause dilutional hyponatraemia, especially renal impairment; monitor urine output; avoid
the undiluted drug is not recommended; give Dose: See under preparations below. following illness or injury which increase the haematocrit falling below 25–30%; where
260 | 6.4.1 Plasma substitutes 6.4.2 Plasma fractions for specific use | 261
possible, monitor central venous pressure; 3.5% solution. Monitor patient for anaphylactic or anaphy- is also available.
can interfere with blood group cross-matching POM Polygeline (WMF 11.1)
lactoid reactions and protocol for managing
and biochemical tests—take samples before Infusion, Polygeline 3.5% with electrolytes. anaphylaxis should be in place. Anaphylactic FACTOR VIII CONCENTRATE
start of infusion; monitor for hypersensitivity or anaphylactoid reactions caused by gelatin
POM Polygeline (EDL 9.2) Plasma fractions should comply with the WHO Re-
reactions; pregnancy (Appendix 2). solutions may either be histamine-mediated quirements for the Collection, Processing and Quality
Injection, Polygeline 3.5% solution with suitable
Adverse effects: Hypersensitivity reactions or histamine independent. Histamine release Control of Blood, Blood Components and Plasma
electrolyte; in a 500-mL bottle.
including fever, nasal congestion, joint pains, can be prevented by the use of a combination Derivatives (Revised 1992). WHO Technical Report
urticaria, hypotension, bronchospasm—rarely POM Polygelin (Alpha) of H1 – and H2-receptor blockers. Prophylactic Series, No. 840, 1994, Annex 2 Factor VIII concentrate
severe anaphylactoid reactions; transient Injection, Polygeline. administration of corticosteroids has not been is a complementary preparation and a representative
increase in bleeding time. proven effective. coagulation factor preparation. Various preparations
Nursing action: Ensure patient is well hydrated SUCCINYLATED GELATIN Interactions: Avoid mixing with Fat emulsions. can serve as alternatives.
at the start of therapy. Therapeutic category: Gelatin agent, colloidal May cause false high values with the following Indications: Control of haemorrhage in hae-
• Discontinue dextran if urine specific gravity plasma substitute. tests: Erythrocyte sedimentation rate, specific mophilia A.
is low, and/or if oliguria or anuria occurs, or Pharmacology: Succinylated gelatin (also gravity of urine, nonspecified plasma protein Precautions: Intravascular haemolysis after
if there is a precipitous rise in central venous known as Modified Fluid Gelatin) is a colloi- assays e.g., by the biuret method. large or frequently repeated doses in patients
pressure or sign of circulatory overloading. dal plasma substitute available as a 4% w/v Adverse effects: Rarely anaphylactic or ana- with blood groups A, B, or AB (less likely with
• Note that Dextran may interfere with analysis solution for infusion. The solution in water for phylactoid reactions (observe patient and have high potency, highly purified concentrates).
of blood grouping, cross matching, bilirubin, injection also contains NaCl. When used in the corrective measures in place). Local erythema, Adverse effects: Allergic reactions including
blood glucose, and protein; therefore ensure treatment of hypovolaemia, it produces signifi- nausea, vomiting, dyspnoea, bronchospasm, chills, fever.
that blood for investigation is obtained before cant increases in blood volume, cardiac output, coughing, wheezing, headache, flushing, urti- Dose: Haemophilia A, by slow IV infusion,
drug therapy commences. stroke volume, blood pressure, urinary output caria, hypotension, hpertension, tachycardia, ADULT and CHILD according to
EMDEX
• Observe closely for signs of anaphylaxis espe- and oxygen delivery. It promotes osmotic di- fever, chills. patient’s needs.
cially during early phase of infusion. uresis, thereby helping to protect the kidneys Dose: See product literature.
from the adverse effects of hypovolaemia. The POM Factor VIII concentrate (WMF 11.2)
Dose: Short-term blood volume expansion, by
Dried, Factor VIII concentrate
rapid IV infusion, ADULT 500–1000 elimination half-life is about 4 hours, majority 6.4.2 Plasma fractions for specific use
mL initially, followed by 500 mL if of the dose being eliminated by renal excretion
Factor VIII is essential for blood clotting and FACTOR IX COMPLEX (COAGULATION
necessary; total dosage should not within 24 hours. FACTORS II, VII, IX, X) CONCENTRATE
the maintenance of effective haemostasis;
exceed 20 mL/kg during the initial 24 Electrolyte concentrations: Sodium: 154
von Willebrand factor is a mediator in platelet Plasma fractions should comply with the WHO
hours; if required 10 mL/kg daily may mmol/L; chloride: 120 mmol/L.
aggregation and also acts as a carrier for fac- Requirements for the Collection, Processing and
be given for a further 2 days (treat- pH: 7.4±0.3. Theoretical Osmolarity: 274 mOs-
tor VIII. Blood coagulation factors VII, IX, and Quality Control of Blood, Blood Components
ment should not continue for longer mol/L. Gelation Point: ≤3°C. and Plasma Derivatives (Revised 1992). WHO
X are essential for the conversion of factor II
than 3 days); CHILD total dosage Indications: Colloidal plasma volume substi- Technical Report Series, No. 840, 1994, Annex 2
(prothrombin) to thrombin. Deficiency in any
should not exceed 20 mL/kg. tute for prophylaxis and treatment of relative Factor IX complex concentrate is a complementary
of these factors results in haemophilia. Bleed-
or absolute hypovolaemia; prophylaxis of preparation and a representative coagulation factor
POM Dextran 70 (WMF 11.1) ing episodes in haemophilia require prompt
hypotension e.g., during induction of epi- preparation. Various preparations can serve as alter-
Injectable solution, Dextran 6%. treatment with replacement therapy. Factor natives.
dural or spinal anaesthesia; haemodilution;
POM Dextran 70 (EDL 9.2) VIII, used for the treatment of haemophilia
extracorporeal circulation; vehicle solution for Indications: Replacement therapy for factor
Intravenous infusion, Dextran 6% in NaCl IV infusiion A, is a sterile freeze-dried powder containing
compatible medicaments e.g., insulin. IX deficiency in haemophilia; bleeding due to
7.5%;500-mL bottle. the blood coagulation factor VIII fraction
Contra-indications: Hypersensitivity to gel- deficiencies of factors II, VII or X.
prepared from pooled human venous plasma.
atin, hypervolaemia, hyperhydration, severe Contra-indications: Disseminated intravascu-
POLYGELINE Standard factor VIII preparations also contain
cardiac insufficiency, recent event of cardiac lar coagulation
von Willebrand factor and may be used to
Deleted from the current WHO Model Formulary. infarction, severe disturbances of blood coag- Precautions: Risk of thrombosis (probably less
treat von Willebrand disease. Highly purified
Polygeline is a representative partially degraded gelatin. ulation, severe renal insufficiency. risk with highly purified preparations).
Various preparations can serve as alternatives. preparations, including recombinant factor
Precautions: Known allergic diseases eg, Adverse effects: Allergic reactions including
VIII, are available; they are indicated for the
Indications: Correction of low blood volume. asthma; hypernatraemia; haemorrhagic diath- chills, fever.
treatment of haemophilia A but do not contain
Contra-indications: Severe congestive heart esis; left or right ventricular insufficiency; pa- Dose: Haemophilia B, by slow IV infusion,
sufficient von Willebrand factor for use in the
failure; renal failure. tients with blood coagulation disorders, renal ADULT and CHILD according to pa-
management of von Willebrand disease.
Precautions: Blood samples for cross-match- insufficiency, chronic liver diseases. Monitor tient’s needs and specific preparation
haematocrit, platelet count, serum electrolyte Factor IX Complex is a sterile freeze-dried
ing should be taken before infusion; haem- used.
concentrations and signs of hypocalcaemia. concentrate of blood coagulation factors II,
orrhagic diasthesis; congestive heart failure, Treatment of bleeding due to defi-
(e.g., tetany, paraesthesia); then corrective VII, IX and X derived from fresh venous plasma.
renal impairment, hypertension, oesophageal ciencies in factor II, VII or X as well as
measures should be taken. Because the prod- Factor IX complex which is used for the treat-
varices; interactions: Appendix 1. IX, by slow IV infusion, ADULT and
uct does not substitute lost plasma protein, ment of haemophilia B may also be used for
Adverse effects: Hypersensitivity reactions in- CHILD according to patient’s needs.
it is advisable to check the plasma protein the treatment of bleeding due to deficencies
cluding urticaria—rarely severe anaphylactoid POM Factor IX complex (WMF 11.2)
concentrations 6-12 hours after an operation. of factor II, VII, and X. High purity preparations
reactions; transient increase in bleeding time. Dried, Factor II, VII, IX, and X.
May be used during pregnancy where plasma of factor IX which do not contain clinically
Dose: Correction of low blood volume, by IV
volume replacement is indicated, after carefully effective amounts of factor II, VII, and X are
infusion, initially 500–1000 mL of a
weighing benefits & potential risks. available. A recombinant factor IX preparation
262 | 6.4.2 Plasma fractions for specific use 6.5 Vitamins | 263
HUMAN ALBUMIN HUMAN NORMAL IMMUNOGLOBULIN should be in a hospital with adequate facilities for patients with acute corneal lesions should be
Synonym: Normal Human Serum Albumin; monitoring the infusion as well as the condition for referred to a hospital on an emergency basis.
Normal immunoglobulin – Normal immunoglobulin which it is being administered, until the patient is
Salt Poor Albumin. solution is administered by intravenous infusion for pri-
In women of child-bearing age there is a need
stable, when treatment at home can be considered to balance the possible teratogenic effects
Therapeutic category: Plasma Volume Ex- mary immuno-deficiencies and immunomodulation in after formal training in an expert centre.
pander; Blood Product Derivative. autoimmune disease including Guillain-Barre syndrome of vitamin A should they be pregnant with
Indications: In emergency, to prevent or and Kawasaki disease. Solutions for intramuscular and POM Human normal immunoglobulin (WMF 11.2) the serious consequences of xerophthalmia.
subcutaneous injection are used for primary immune Injection, Normal immunoglobulin for IV use, 5%, Where there are severe signs of xerophthalmia
treat hypovolaemic syndromes and to avoid
deficiency. Normal immunoglobulin should be used in 10% protein solution. high dose treatment as for patients over 1 year
occurence of cardiovascular collapse; nuclear Injection, Normal immunoglobulin for IM use, 16%
hospital settings where specialist supervision is available. should be given. When less severe symptoms
jaundice in the newborn; as replacement ther- protein solution
Normal immunoglobulin (human, polyvalent) – are present (for example night blindness) a
apy, to increase the albumin fraction in serum Plasma fractions should comply with the Requirements Injection, Normal immunoglobulin for SC use, 15%,
or correct protein deficiency in conditions such 16% protein solution. much lower dose is recommended. Vitamin A
for the Collection, Processing and Quality Control of
as serious hepatic disorders, decompensated Blood, Blood Components and Plasma Derivatives Note: Formulations from different manufacturers therapy should also be given during epidemics
nephrotic syndrome, chronic condition in burn (Revised 1992). WHO Technical Report Series No. 840, vary and should not be regarded as equivalent; of measles to reduce complications.
cases; cerebral oedema. 1994, Annexe 2. consult individual manufacturer’s product literature. Vitamin B is composed of widely differing
Contra-indications: Volaemic overload, POM Normal immunoglobulin (EDL 22.1) substances which are, for convenience, classed
Indications: Replacement therapy in primary as ‘vitamin B complex’. Thiamine (vitamin B1) is
asystolia, severe deterioration of general Injection, Immunoglobulin 30 mg, 165 mg per mL.
immunodeficiency, Kawasaki disease. used orally for deficiency due to to inadequate
circulation.
Precautions: Monitor vital signs; interactions: POM GAMMAPLEX® (Alpha) dietary intake. Severe deficiency may result in
Precautions: Dehydration (alternate with
Appendix 1. Solution for Infusion, Human normal immunoglobulin
‘beri-beri’. Chronic dry ‘beri-beri’ is character-
suitable rehydrating solution), circulatory 2.5 g, 5 g, 10 g
Adverse effects: Nausea, vomiting, headache ized by peripheral neuropathy, muscle wasting
overload (check central venous BP and pul-
(may develop 24 hours after infusion); dizzi- and weakness, and paralysis; wet ‘beri-beri’ is
monary capillary pressure regularly); should 6.5 Vitamins
EMDEX
ness, dry mouth, chills, sweating, hypothermia, characterized by cardiac failure and oedema.
be injected alone (normal diluents are saline
fever, eczema, rash, urticaria, hypotension, Vitamins are used for the prevention and Wernicke-Korsakoff syndrome (demyelination
and glucose solutions).
wheezing; anaphylactoid reactions also re- treatment of specific deficiency states or when of the CNS) may develop in severe deficiency.
Interactions: Not to be mixed with other
ported; with immunomodula-tory doses also the diet is known to be inadequate. It has Thiamine is given by intravenous injection in
medications.
immune haemolysis, aseptic meningism, in- often been suggested but never convincingly doses of up to 300 mg daily (parenteral prepa-
Nursing action: Administer IV slowly (rapid
creased plasma viscocity, hypercoagulopathy, proved, that subclinical vitamin deficiencies rations may contain several B group vitamins)
infusion may cause hypotension).
renal impairment. cause much chronic ill-health and liability to as initial treatment in severe deficiency states.
• Monitor vital signs carefully; observe for
Dose: NOTE: National recommendations may infections. This has led to enormous consump- Potentially severe allergic reactions may occur
signs of vascular overload e.g. heart failure
vary. Consult individual manufactur- tion of vitamin preparations, which have no during, or shortly after parenteral administra-
or pulmonary oedema.
er’s product literature for dose and more than placebo value. Most vitamins are tion, therefore intravenous injections should
• Discard unused or cloudy solutions.
administration recommendations comparatively non-toxic but prolonged ad- be administered slowly (over 10 minutes) and
• Watch out for allergic reactions such as
for specific diseases; recommended ministration of high doses of retinol (vitamin should be used only if parenteral treatment is
urticaria, rash, pyrexia, rigor or chill and im-
doses may vary to those listed below. A), ergocalciferol (vitamin D2) and pyridoxine essential. Facilities for resuscitation should be
mediately inform physician.
For replacement therapy in primary (vitamin B6) may have severe adverse effects. immediately available. Riboflavin (vitamin B2)
• Watch for haemorrhage or shock if used after
immune deficiencies: Initial loading Retinol (vitamin A) is a fat-soluble substance deficiency may result from reduced dietary in-
surgery or injury.
intravenously in divided doses until stored in body organs, principally the liver. Pe- take or reduced absorption due to liver disease,
Dose: By IV infusion (20 drops per minute),
serum IgG level is >6 g/l. Maintenance riodic high-dose supplementation is intended alcoholism, chronic infection or probenecid
shock, 125-150 mL.
doses by IV, SC or IM routes: normally to protect against vitamin A deficiency which therapy. It may also occur in association
Child: 1-2 mL/kg b.wt.
0.4 – 0.8 g/Kg/ month for children and is associated with ocular defects particularly with other deficiency states such as pellagra.
Serious burns, double the dosage on
adults. Dose to be titrated depending xerophthalmia (including night blindness Pyridoxine (vitamin B6) deficiency is rare as
1st day and the normal dosage on the
on inter-current infections or trough which may progress to severe eye lesions and the vitamin is widely distributed in foods, but
subsequent days.
serum IgG level. Intravenous doses blindness), and an increased susceptibility to deficiency may occur during isoniazid therapy
Nuclear jaundice in the newborn ,
may be given at one, two, three or infections, particularly measles and diarrhoea. and is characterized by peripheral neuritis. High
10-15 mL associated with exchange
four week intervals. SC doses may be Universal vitamin A distribution involves the doses are given in some metabolic disorders,
transfusion.
given at one, two, three, four or seven periodic administration of supplemental doses such as hyperoxaluria and it is also used in
Replacement therapy, 125-250 mL
day intervals. to all preschool-age children with priority given sideroblastic anaemia. Pyridoxine and thi-
daily.
For immuno-modulation in autoim- to age groups, 6 months to 3 years, or regions amine also have a role in status epilepticus
Child: 2-5 mL/kg b. wt daily.
mune conditions: Max. recommended at greatest risk. All mothers in high-risk regions (see section 1.7). Nicotinic acid inhibits the
Newborn: 5-15 mL/kg b.wt daily.
dose is 2g/Kg over at least 48 hours. should also receive a high dose of vitamin A synthesis of cholesterol and triglyceride and is
POM Human albumin (EDL 9.2) Depending on specific autoimmune within 8 weeks of delivery. Since vitamin A is used in some hyper-lipidaemias. Nicotinic acid
Injection, Human albumin 20% solution. disease: 0.4 g/Kg/day for 5 days or associated with a teratogenic effect it should and nicotinamide are used to prevent and treat
POM ZENALB® (Alpha) 0.8 – 1 g/Kg the first day and repeated be given in smaller doses (no more than 10 nicotinic acid deficiency (pellagra).
Injection, Human albumin 20% solution once if indicated. 000 units/day) to women of child-bearing Nicotinamide is generally preferred as it does
Administration: Infusion rates of <8 g per hour are age. It is also used in the treatment of active
recommended. Immunoglobulin should be admin-
not cause vasodilation. Hydroxo-cobalamin
xerophthalmia. Doses of vitamin A should is the form of vitamin B12 used to treat vitamin
istered under the supervision of an immunologist
be administered orally immediately upon B12 deficiency due to dietary deficiency or
or other experienced physician. In general, this
diagnosis of xerophthalmia and thereafter malabsorption (see section 6.1).
264 | 6.5 Vitamins 6.5 Vitamins | 265
Folic acid is essential for the synthesis of DNA Children 0.3-1 mg weakness, headache, nausea, constipation, dry Dose: Adult & child >10 years, 5 mL 1-2 times daily.
and certain proteins. Deficiency of folic acid Adults 1-1.3 mg mouth, muscle and bone pain, metallic taste. Child (1-5 years): 2.5 mL daily; 6-10 years,
or vitamin B12 is associated with megaloblas- Vitamin B1 Interactions: Larger doses may be needed for 2.5 mL 1-2 times daily
Deficiency:
(Thiamine)
tic anaemia. Folic acid should not be used in Children 5.0-50 mg patients on barbiturates, anticonvulsants due OTC BVC® (Bond)
undiagnosed megaloblastic anaemia unless Adults 200-300 mg to hepatic enzyme induction. Thiazide diuretics Syrup, Ascorbic acid 100 mg per 5 mL.
vitamin B12 is administered concurrently, Children 1.0-1.8 mg
(increased risk of hypercalcaemia). Reduced Pack: 100 mL
otherwise neuropathy may be precipitated intestinal absorption with cholestyramine. Dose: Infants, 5 mL 3 times daily.
Vitamin B2 Adults 0.3-1 mg Child (1 – 5 years): 5 mL 3 times daily; 6 – 12
(see section 6.1). Supplementation with folic (Riboflavin) Deficiency:
Adverse effects: Hypercalcaemia, hyperphos-
years, 10 mL 3 times daily.
acid 400 µg daily is recommended for women Adults 5.0-30 mg
pha-taemia; Pruritus, rash, urticaria; Nephrocal-
of child-bearing potential in order to reduce Children 0.3-0.6 mg
cinosis, renal impairment. OTC CEENVITE-C® (Ceenek)
the risk of serious neural tube defects in their Dose: By mouth, Adult, initially 1 mcg daily Syrup, Ascorbic acid 100 mg per 5 mL.
Adults 1.0-2.0 mg
offspring (see section 6.1). Vitamin B6 (0.5 mcg/day in elderly); adjust based Pack: 100 mL
Deficiency:
Ascorbic acid (vitamin C) is used for the pre- (Pyridoxine HCl) on response & plasma calcium levels. OTC CEEVITE® (Fidson)
Children 20-50 mg
vention and treatment of scurvy. Claims that Maintenance: 0.25-1 mcg daily. Tablet, Ascorbic acid 100 mg; white tab. marked
Adults 50-400 mg
ascorbic acid is of value in the treatment of (Additional information sourced from One-Alpha monograph: ‘CEEVITE’ on one side and ‘100’ on the reverse.
Children 0.3-2 mcg 100 mg – 1000’s.
common colds are unsubstantiated. http://www.medicines.org.uk/)
Vitamin B12 Adults 2.0-3.0 mcg
The term vitamin D covers a range of com- OTC CELGARD C® (Evans)
(cyanocobalamin Deficiency: POM MEDI-a® (Megalife sciences)
pounds including ergocalciferol (vitamin D2) Tablet, Ascorbic acid 100 mg
and colecalciferol (vitamin D3). These two Adults 50-1,000 mcg Capsules, Alfacalcidol 0.25 mcg, 1 mcg; off white, Syrup, Ascorbic acid 100 mg per 5 mL
Children 50-200 mg oval-shaped softgel cap. Pack: 100 mL
compounds are equipotent and either can Vitamin C
(Ascorbic acid) Pack: 10 x 10’s (in blister)
be used to prevent and treat rickets. Simple Adults 250-1,000 mg
POM CEVETA® (Vixa)
EMDEX
deficiency of vitamin D occurs in those who Vitamin D Children 2.5-5 mcg
ASCORBIC ACID Injection, Vitamin C 500 mg/5 mL.
have an inadequate dietary intake or who fail (Cholecalciferol) Adults 25-50 mcg Pack: 5 mL x 100’s.
Synonym: Vitamin C
to produce enough colecalciferol (vitamin D3) Children 3.0-15 mg
Indications: Prevention and treatment of OTC CHEWETTE C® (Hovid)
in their skin from the precursor 7-dehydro- Adults 50-200 mg Tablet, (Orange flavour), Vitamin C 100 mg; orange
Vitamin E scurvy.
cholesterol in response to ultraviolet light. Deficiency: tab. marked ‘CHEWETTE 100’ on one side.
Adverse effects: GI disturbances reported
Children with dark skin must continue vitamin Children 1,000-2,000 mg 100 mg – 60 x 12.
with large doses.
D prophylaxis for up to 24 months because of * Formulations containing various specified amounts of Tablet, (Black currant), Vitamin C 100 mg; purple
Dose: Prophylaxis of scurvy, by mouth, ADULT
their inability to produce enough in their skin. vitamins are accepted provided the formulations satisfy the coloured tab. marked ‘CHEWETTE 100’ on one side.
vitamin requirements of the age and the physiological state and CHILD 25–75 mg daily 100 mg – 150.
Dark skin with a high melanin content must be
of the intended user. Treatment of scurvy, by mouth, ADULT Dose: 300-400 mg per day.
exposed to daylight longer than light skin in
and CHILD not less than 250 mg daily
order to obtain the same synthesis of vitamin OTC CITRAMIN® (Afrab-Chem)
in divided doses.
D3. Vitamin D is also used in deficiency states ALFACALCIDOL Tablet, (chewable), Vitamin C 100 mg; orange
See also under the preparations below. flavoured
caused by intestinal malabsorption or chronic Synonym: Vitamin D analogue.
liver disease and for the hypocalcaemia of OTC Ascorbic acid (WMF 27) 100 mg – 1000’s
Pharmacology: Alfacalcidol (1α-hydroxyvita- Syrup, Ascorbic acid 100 mg per 5 mL.
hypoparathyroidism. Tablets, Ascorbic acid 50 mg.
min D3) undergoes 25-hydroxylation in the liver Pack: 100 mL
Vitamin K is necessary for the production of to form 1,25-dihydroxyvitamin D3 (Calcitriol) – OTC Ascorbic acid (EDL 28.1) Drops, Vitamin C 100 mg per mL; orange flavoured
blood clotting factors (see section 6.2.2). the active form of vitamin D which regulates Tablet, Ascorbic acid 100 mg. Pack: 15 mL in amber glass bottle with dropper
calcium & phosphate metabolism. Unlike the Oral liquid, Ascorbic acid 100 mg per 5 mL
Approved Doses for Vitamins
OTC CITRUS-C® (Jopan)
(Source: Nigeria’s Standard Treatment Guidelines, 2008) parent vitamin D, it does not require renal OTC ASCO-J® (Juhel) Tablet, Ascorbic acid 100 mg; white tab. marked
Vitamin
Age Group/
Daily Dosage
hydroxylation. In renal disease, impairment of Tablets, Vitamin C 100 mg; 500 mg. ‘JOPAN’ on one side and ‘CITRUS/100’ on the reverse.
Physiological State 1α-hydroxylation can lead to the disturbances 100 mg – 50; 500; 1000. 100 mg – 1000’s.
Biotin Adults 100-300 mg in mineral metabolism found in several disor- 500 mg – 100. Chewable tablet, Ascorbic acid 100 mg; orange
ders, including renal bone disease, hypoparath- Syrup, Ascorbic acid 100 mg per 5 mL. coloured tab. marked ‘JOPAN’ on one side and ‘CIT-
Children 40-200 mcg
Folic acid Pack: 100 mL in amber bottle. RUS/100’ on the reverse.
Adults 200-5,000 mcg yroidism, neonatal hypocalcaemia and vitamin
D dependent rickets. Alfacalcidol in relatively OTC ASCORBION C® (Mopson) OTC EM-VIT-C® (Emzor)
15-30 mg
Adults small doses is indicated in such conditions. Tablet, Vitamin C 100 mg. Tablet, Ascorbic acid 100 mg.
(prophylaxis)
Indications: Hypocalcaemia, renal osteodys- 100 mg – 50, 100, 1000. 100 mg – 100; 1000
Nicotinamide Deficiency: Syrup, Vitamin C 300 mg per 5 mL.
trophy, hypoparathyroidism, rickets or osteo- Tablet, (Chewable), Ascorbic acid 100 mg.
50-250 mg Pack: 100 mL. 100 mg – 10 x 30; 100; 1000.
Adults
(therapeutic) malacia, hypophosphataemia.
Contra-indications: Hypersensitivity; Hyper- OTC ASCORPIL® (Pharchem) Syrup, Ascorbic acid 100 mg per 5 mL.
Children 0.5-3.5 mg Pack: 100 mL; 2 L.
Pantothenic acid calcaemia, metastatic calcification. Tablet, Ascorbic acid 100 mg; white/pink scored
Adults 1.0-7 mg
Precautions: Monitor serum calcium & phos- tab. marked ‘PIL’. OTC ESOCEE® (Jawa)
Children 1,500-5,000 units 100 mg – 100’s; 1000’s.
phate levels regularly; CHF patients on digitalis Syrup, Ascorbic acid 100 mg per 5 mL.
Adults 5,000-10,000 U
(hypercalcaemia may cause arrhythmia); neph- OTC AVRO-C® (Avro) Pack: 100 mL x 20’s
Vitamin A Pregnancy 5,000-6,000 units Drops, Ascorbic acid 100 mg per mL.
rolithiasis. Educate patient about symptoms of Syrup, Vitamin C 300 mg per 5 mL; clear yellow syrup
Lactation 5,000-10,000 U Pack: 15 mL
hypercalcaemia namely polyuria, polydipsia, with characteristic taste.
Deficiency 25,000-50,000 U Pack: 100 mL.
OTC GARYCEE® (Agary) Injection, Ascorbic acid 500 mg/5 mL. OTC Vitamin C (Ceenek) COD LIVER OIL
Oral tablet, Ascorbic acid 100 mg Pack: 1x 100’s Tablet (white), Ascorbic acid 100 mg Indications: Treatment of vitamin A and vita-
100 mg – 1000’s 100 mg – 1000’s
OTC SOFA-C® (Sofak) min D related deficiencies.
Chewable tablet, Ascorbic acid 100 mg; orange
flavoured tab. containing Aspartame .
Tablet, Ascorbic acid 100 mg; white/orange tab OTC Vitamin C (Dizpharm) Dose: By mouth, Adult, 1 capsule 3 times
100 mg – 100’s; 1000’s Tablet, Ascorbic acid 100 mg. daily.
100 mg – 1000’s
Syrup, Ascorbic acid 100 mg per 5 mL 100 mg – 100; 1000.
OTC GG Vitamin C (Geneith) Pack: 100 mL OTC ADCOD® (Canopus)
OTC Vitamin C (Emzor) Capsule, Cod liver oil 1000 mg
Tablet, Vitamin C 50 mg, glucose 150 mg.
OTC TACORANGE® (SKG) Tablet, Ascorbic acid 100 mg; white to off-white tab Pack: 3 x 10’s
Pack: 3 x 8’s
Syrup, Vitamin C 100 mg per 5 mL; clear yellow syrup 100 mg – 100; 1000.
OTC Healthilife Style Vitamin C® (Biofem) with xteristic odour and taste. Syrup, Ascorbic acid 100 mg per 5 mL; clear yellow OTC BLUE SEA 300® (Embassy)
Tablet, (Chewable), Ascorbic acid 500 mg Pack: 100 mL in amber bottle. orange flavoured syrup. Capsule, Cod liver oil 300 mg.
Dose: As dietary supplement, child (<12 years), 2.5-5 Pack: 100 mL; 2 L. 300 mg – 2 x 15’s.
OTC High Potency Vitamin C (Bio-factor)
mL daily; >12 years, 10 mL daily. OTC BLUE SEA 1000® (Embassy)
Tablet, Vitamin 1000 mg OTC Vitamin C (Gauze)
Treatment, child (<12 years), 2.5-5 mL 3 Capsule, Cod liver oil 1000 mg
Oral liquid, Ascorbic acid 40 mg per 5 mL
OTC LIMVIT® (Ranbaxy) times daily; above 12 years, 10 mL 3 times 1000 mg – 2 x 15’s (in blisters)
Pack: 100 mL; 2 L
Syrup, Ascorbic acid 100 mg per 5 mL daily.
Pack: 100 mL. OTC Vitamin C (Goz) OTC Cod Liver Oil (Crowther)
OTC TAMIN-C® (Leady) Capsule, Cod liver 1000 mg.
Syrup, Ascorbic acid BP 40 mg per 5 mL.
OTC MEGA C (Sylken) Tablet, Ascorbic acid 100 mg; uncoated white, scored Pack: 5 x 6’s
Pack: 100 mL; 2 L
Tablet, Vitamin C 1000 mg, Rose hips powder (Rosae cylindrical tab
pseudofructus) seed. 100 mg – 100’s; 1000’s OTC Vitamin C (Juhel) OTC Cod Liver Oil (Geneith)
Pack: 100’s Syrup, Ascorbici acid 100 mg per 5 mL Tablet, Ascorbic acid 100 mg; orange flavoured or Capsule, Cod Liver Oil BP 300 mg.
Dose: 1 tablet daily Pack: 100 mL; 2 L plain tab.
EMDEX
OTC CODLIVER® Plus (Pinnacle)
100 mg – 100; 1000. Capsule, Codliver oil 1000 mg, Vitamin B1 (thiamine
OTC Moko C (New Healthway) OTC TOP-CEE® (Nemel)
Tablet, Ascorbic acid 100 mg; white & orange tab. Tablet (chewable), Ascorbic acid 100 mg POM Vitamin C (Mark) mononitrate) 1 mg, Vitamin B2 (riboflavin) 1 mg,
100 mg – 100’s; 1000’s 100 mg – 10 X 30’s; 100’s; 1000’s Injection, Vitamin C 500 mg per 5 mL. Vitamin B6 1 mg, Nicotinamide 15 mg, Aloe vera 5 mg.
Syrup, Ascorbic acid 100 mg per 5 mL. OTC DIPSEAS® (N.C.I)
OTC TOPVITE-C® (Topway) OTC Vitamin C (Nomagbon)
Pack: 100 mL. Capsules (softgels), Cod liver oil 300 mg, 1000 mg
Syrup (orange), Ascorbic acid 100 mg per 5 mL. Syrup, Ascorbic acid 100 mg per 5 mL; yellow syrup
OTC Nature’s Field Mega C (Sylken) Pack: 100 mL. Pack: 100 mL (in glass bottle) 300 mg – 2 x 15’s
Tablet, Ascorbic acid 1000 mg, Rosehips 25 mg Tablet (chewable), Ascorbic acid 100 mg. 1000 mg – 2 x 15’s
100 mg – 100’s. OTC Vitamin C MKP (Neros)
Pack: 10’s; 30’s; 100’s OTC Fresh & Pure Cod Liver Oil (Embassy)
Effervescent tablet, Ascorbic acid 1000 mg.
Dose: 1 tablet daily. Liquid, Vitamin A 7000 IU, vitamin D 800 IU, vitamin E
OTC VINCOCEE® (Vinco) 1000 mg – 10’s (in tube).
OTC NATUREVIT-C® (Al-Tinez) Tablet, Vitamin C 100 mg; white tab. Dose: Dissolve the tablet in 200 mL of water. 1 IU, Omega 3 1.8 g of which EPA 0.83 g., DHA 0.74 g.
Chewable tablet, Vitamin C 500 mg; available in 100 mg – 100’s, 1000’s Adult: 1 tablet daily Pack: 170 mL
lemon, orange & pineapple flavours. Child: ½ tablet daily. OTC GLOCOD® (GoldMoore)
OTC VITA-ACE® (Mecure)
500 mg – 25 x 4’s. Capsule, Cod liver oil 1000 mg.
Tablet, Ascorbic acid 100 mg; orange tab. OTC ZING C (Mecure)
OTC NAVIC® (NASDMU) 100 mg – 1 x 100’s; 1 x 1000’s. Liquid, Vitamin C 500 mg, glucose 8 g per 10 mL; 1000 mg – 2 x 15’s.
Chewable tablet, Ascorbic acid 100 mg; marked Syrup, Vitamin C 100 mg per 5 mL; slightly yellowish light yellowish orange syrup in unit dosage pack. OTC GOLDEN SEA® (Award Global)
“NAVIC” on one side and “NASDMU” on reverse side. syrup. Capsule, Cod liver oil 1000 mg
Vitamin C + Aspartame
100 mg – 1000’s Pack: 100 mL. 1000 mg – 2 x 15’s (in blisters)
OTC Vitamin C (Ceenek)
OTC NEROCEE® (Neros) POM VITABETA-C® (Beta Drugs) POM MD Cod Liver Oil (O’Nell)
Tablet, Ascorbic acid 100 mg , aspartame 2 mg.
Tablet, Ascorbic acid 100 mg. Injection, Vitamin C 100 mg per mL; in 5 mL amp Liquid, Vitamin A 700 IU, vitamin D 800 IU, vitamin
100 mg – 1000’s.
100 mg – 10’s. Pack: 5 mL x 100 amps. E 1 IU, Omega-3 1.8 g (eq. to EPA 0.83 g, DHA 0.74
Vitamin C + Glucose g) per 10 mL.
OTC RAPHA-C® (Rapha) OTC VITABOL® (Efunpo)
Tablet, Ascorbic acid 100 mg Tablet (chewable), Ascorbic acid 100 mg; orange OTC GLUCO-C® (E-Globa) Dose: Adult and child (>1 year): 10 mL daily; 7-12
100 mg – 1 x 1000’s (in PVC Jar) 100 mg – 100’s (in jar). Tablet, (Adult), Vitamin C 50 mg, Glucose 150 mg; months, 5 mL daily; 0-6 months, 2.5 mL
chewable orange flavoured tab. daily. May taken alone or mixed with twice
OTC RAMINE-C® (Seagreen) OTC VITACEE® (Pharma-Deko) its quantity of milk or orange juice.
Pack: 20 x 24’s
Effervescent tablet, Ascorbic C 1000 mg; orange Syrup, Vitamin C.
Dose: 10-20 tablets a day; hold to dissolve slowly OTC Nutrihealth Cod Liver Oil (Hovid)
flavour tab. Pack: 100 mL.
in the mouth. Capsule , Vitamin A 600 IU, vitamin D 60 IU
1000 mg – 12 x 4’s; 5 x 4’s (in box); 20’s (in tube) Dose: Child and adult, 5-15 mL daily.
Tablet, (Child), Vitamin C 10 mg, Glucose 100 mg; Pack: 100’s.
Drops, Vitamin C 100 mg per mL.
OTC REDOXON® (Swipha) chewable orange flavoured tab.
Pack: 15 mL. OTC OCEANIC® (Elbe)
Effervescent tablet, Ascorbic acid 1 g; orange tab. Pack: 40 x 10’s
Dose: Child (<1 year), 0.3 mL daily; >1 year, 0.6 Capsules, Cod liver Oil 300 mg, 1000 mg.
1 g – 10. Dose: 6 tablets a day.
mL daily. Pack: 1 x 30 softgels.
OTC REJUVA-G® (N.C.I) Doses should be dropped on the back of the OTC Vitamin C + Glucose (Neros)
Capsule, Ascorbic acid 50 mg, Nicotinamide 10 mg, tongue or mixed with milk, fruit juices and Lozenge, Vitamin C 50 mg, glucose 150 mg. POM SECOD® 300 (GoldMoore)
Vitamin B6 1 mg; brown cap. Capsule, Cod liver oil 300 mg.
other liquids.
Pack: 2 x 15’s. 300 mg – 2 x 15’s.
OTC Vitamin C (Afrab-Chem)
POM SIVO-C® (Adpharm) OTC SILVACOD® (Justeen)
Tablet, Ascorbic acid 100 mg.
Capsule, Codliver oil 300 mg. necessary in steps of 250 nanograms poparathyroidism, by mouth, ADULT Prevention, 1 mg IM immediately
300 mg – 10 x 10’s at intervals of 2–4 weeks; usual dose 2.5 mg (100 000 units) daily; CHILD up post-partum; Treatment, 1 mg/kg IM
OTC Supa-Nova Cod Liver Oil® (SKG) 0.5–1 microgram daily; dosage in to 1.5 mg (60 000 units) daily. daily for 1-3 days.
Liquid , Vitamin A 7000 IU, vitamin D 800 IU, vitamin children not established Note: The dosage in neonates should not exceed 5
POM Ergocalciferol (WMF 27)
E 1 IU. Established postmenopausal osteo- mg during the first few days of life because of the
Tablet or capsule, Ergocalciferol 1.25 mg (50 000
Pack: 150 mL. porosis, 250 nanograms twice daily immaturity of the hepatic enzyme system.
units).
Dose: By mouth, Adult, 10ml daily; child (1-6 (monitor plasma-calcium concentra- Oral liquid, Ergocalciferol 250 µg/mL (10 000 units/ POM Phytomenadione (EDL 4.2)
months), 2.5 mL daily; 6-12 months, 5 mL tion and creatinine). mL). Injection, Phytomenadione 10 mg per mL; in 1-mL
daily; over 12 months, 5-10 mL daily. Note: If there is no plain vitamin D tablet available amp.
Note: If infant is fed with dried milk, use half of the POM MEDITROL® (Mega Lifesciences)
for the treatment of simple deficiency, calcium and
above prescribed doses. Capsule, Calcitriol 0.25 mg. POM KAVITA® (Vixa)
ergocalciferol tablets may be used but the calcium
0.25 mg – 6 x 5’s. Injection, Vitamin K3.
OTC TAVON® (Justeen) is unnecessary.
Capsules, Codliver oil 300 mg, 1000 mg. POM KONAKION® (Swipha)
CYANOCOBALAMIN POM Ergocalciferol (EDL 28.1)
300 mg – 10 x 10’s Injection, Phytomenadione 10 mg per mL; in 1-mL
Tablets or Capsules, Ergocalciferol 0.25 mg (10,000
1000 mg – 2 x 15’s See Cyanocobalamin in Section 6.1. amp
units), 1.25 mg (50,000 units).
Pack: 25.
OTC Tenderwell Cod Liver Oil (Diamond Remedies) Oral liquid, Ergocalciferol 250 mcg per mL.
Capsules, Cod liver oil 300 mg, 1000 mg; green/ POM Cyanocobalamin (EDL 28.1) POM Phytomenadione (Alpha)
yellow coloured caps. Tablet, Cyanocobalamin 50 mcg FOLIC ACID Injection, Vitamin K1 10 mg per mL; in 1 mL amp.
Pack: 2 x 15.
ERGOCALCIFEROL See Folic acid in Section 6.1.1. PYRIDOXINE
OTC TOCOD-E® (N.C.I)
Capsule, Cod liver oil 1000 mg, tocopheryl acetate
Synonym: Vitamin D2 Synonym: Vitamin B6
OTC Folic acid (EDL 28.1)
Indications: Prevention of vitamin D de-
EMDEX
10 mg. Tablet, Folic acid 5 mg. Indications: Treatment of pyridoxine defi-
Pack: 2 x 15’s. ficiency; vitamin D deficiency caused by ciency due to metabolic disorders; isoniazid
malabsorption or chronic liver disease; hypoc- NICOTINAMIDE neuropathy; sideroblastic anaemia
OTC Vital’s Cod Liver Oil (Strides Vital)
alcaemia of hypoparathyroidism. Precautions: interactions: Appendix 1.
Capsules, Cod liver oil 300 mg, 1000 mg; oval shaped Indications: Treatment of pellagra.
Contra-indications: Hypercalcaemia; meta- Adverse effects: Generally well tolerated,
natural coloured soft gelatin cap. containing clear Dose: Treatment of pellagra, by mouth,
yellow oily liquid. static calcification. but chronic administration of high doses may
ADULT up to 500 mg daily in divided
300 mg – 10 x 10’s Precautions: Ensure correct dose in infants; cause peripheral neuropathies.
doses.
1000 mg – 2 x 15’s. monitor plasma calcium at weekly intervals Advice to patients: Dietary sources of pyri-
in patients receiving high doses or those with OTC Nicotinamide (WMF 27) doxine include red meats, bananas, potatoes,
Compound preparations Tablet, Nicotinamide 50 mg.
renal impairment; nausea and vomiting—may yeast, lima beans, whole grain cereal; do not
OTC AQUAMARINE® (Adler) indicate overdose and hypercalcaemia; preg- exceed recommended doses.
Capsule, Omega-3 fish oil 540 mg, Cod liver oil 540 nancy and breast-feeding (Appendices 2 and PHYTOMENADIONE
mg, Vitamin E 11 mg. Nursing action: Stress importance of com-
3); interactions: Appendix 1. Synonym: Vitamin K1 pliance and good nutrition if prescribed for
Pack: 3 x 20’s.
Adverse effects: Symptoms of overdosage Therapeutic category: Fat Soluble Vitamin. maintenance therapy to prevent reoccurence
Liquid, Omega-3 fish oil 4.52 g, Cod liver oil 4.52 g,
Vitamin E 11 mg per 100 mL. include anorexia, lassitude, nausea and vomit- Indications: Prevention and treatment of of deficiency.
Pack: 250 mL. ing, diarrhoea, weight loss, polyuria, sweating, haemorrhage or threatened haemorrhage as • Explain that Pyridoxine when used in combi-
headache, thirst, vertigo, and raised concentra- a result of severe hypoprothrombinaemia due, nation therapy with isoniazid has a specific
OTC CLO-BKO® (Strides Vital) for instance, to overdosage of anticoagulants;
Capsule, Cod liver oil, Vitamin B complex.
tions of calcium and phosphate in plasma and therapeutic purpose and is not “just a vitamin”,
urine; tissue calcification may occur if dose of haemorrhage in the newborn. and therefore the need for adhering to ther-
Pack: 3 x 10’s
1.25 mg continued for several months. Contra-indications: Avoid in patients with apeutic regimen.
CALCITRIOL Nursing action: Teach patient early symptoms pronounced diathesis; hypersensitivity to the • Advise patient to avoid vitamin supplements,
of hypercalcaemia and to report them namely drug; neonates and infants, late pregnancy. unless directed by the doctor.
Synonym: 1,25-Dihydroxycholecalciferol.
weakness, fatigue, somnolence, headache, Precautions: Restrict I.V. administration for • Teach patient dietary sources of vitamin B6.
Therapeutic category: Vitamin D analogue.
anorexia, dry mouth, metallic taste, nausea, emergency use only, and it should be given Dose: Deficiency states, by mouth, ADULT
Indications: Established postmenopausal
vomiting, cramps, diarrhoea, muscle pain, bone very slowly; G6PD deficiency and vitamin E 25–50 mg up to 3 times daily
osteoporosis; renal osteodystrophy in pa-
pain, and irritability. deficiency (risk of haemolysis). Isoniazid neuropathy, prophylaxis, by
tients with chronic renal failure, particularly
• Advise patient on the dietary sources of Interactions: Decreased effect of warfarin mouth, ADULT 10 mg daily.
those undergoing hemodialysis; post-surgical
vitamin D viz egg yolk, dairy products, cod, sodium, dicumarol. Isoniazid neuropathy, treatment, by
hypoparathyroidism; idiopathic hypopa-
sardines and salmon. Adverse effects: Rarely severe shock-like re- mouth, ADULT 50 mg 3 times daily.
ra-thyroidism; vitamin D dependent rickets;
Dose: Prevention of vitamin D deficiency, by actions; sweating, dyspnoea, pain, tenderness Sideroblastic anaemia, by mouth,
hypophosphatemic vitamin D-resistant rickets.
mouth, ADULT and CHILD 10 µg (400 at injection site. ADULT 100–400 mg daily in divided
Contra-indications, Precautions, etc: See
units) daily. Dose: In severe, life-threatening haemorrhage doses.
under Ergocalciferol.
Treatment of vitamin D deficiency, during anticoagulant therapy, by slow
Dose: By mouth, renal osteodystrophy, POM Pyridoxine (WMF 27)
by mouth, ADULT 1.25 mg (50 000 IV injection, 10 mg; increased up to
initially 250 nanograms daily, or on al- Tablet, Pyridoxine HCl 25 mg.
units) daily for a limited period; CHILD 20 mg as required.
ternate days (in patients with normal
75–125 µg (3000–5000 units) daily. Haemorrhage or threatened haemor- POM Vitamin B6 (EDL 28.1)
or only slightly reduced plasma-cal- Tablets, Pyridoxine (as HCl) 10 mg, 20 mg, 50 mg
Hypocalcaemia associated with hy- rhage in newborn or premature infants,
cium concentration), increased if
OTC HAEMOPLEX® (Dabak) child-bearing age) 200 000 units on POM Riboflavine (Adler) OTC ATABION® (Mark)
Syrup, Pyridoxine HCl 1.5 mg, niacinamide 45 mg, diagnosis, repeated next day and Tablet, Riboflavin 5 mg Tablet, Thiamine mononitrate 100 mg, Pyridoxine
cyanocobalamine 7.5 mcg per 15 mL. then after 2 weeks; ADULT (woman of 5 mg – 50. HCl 200 mg, Cyanocobalamin 200 mcg; f-c tab.
Pack: 1 x 200 mL child-bearing age, see notes above), Pack: 10 x 10’s (in blisters).
severe signs of xerophthalmia, as for SULBUTIAMINE OTC META B FORT® (Vixa)
RETINOL Tablet, Vitamin B1 100 mg, B6 200 mg, B12 200 mcg.
other adults; less severe cases (for Sulbutiamine is a precursor of thiamine (vitamin B1)
Synonym: Vitamin A example, night blindness), 5000–10 Pack: 1 x 10’s; 1 x 10’s
Indications: Prevention and treatment of vita- 000 units daily for at least 4 weeks or OTC ARCALION® 200 (Servier Int’l) OTC NEUROBION® (Biofem)
min A deficiency; prevention of complications up to 25 000 units weekly. Tablet, Sulbutiamine 200 mg; coated tab. Tablet, Thiamine disulfide 100 mg, Pyridoxine HCl
of measles. Note: Oral vitamin A preparations are preferred 200 mg – 20’s; 30’s. 200 mg, Cyanocobalamin 200 ug; white, shiny, round
Precautions: Pregnancy (teratogenic; see for the prevention and treatment of vitamin A Indications: Certain states of transient fatique coated tabs, steeply convexed on both sides.
notes above and Appendix 2); breastfeeding deficiency. However, in situations where patients in adults (over 15 years old). Pack: 20’s (in blister); 10 x 10’s
(Appendix 3). have severe anorexia or vomiting or are suffering Contra-indication: History of allergy to any of Injection, Thiamine HCl 100 mg, Pyridoxine HCl 100
Adverse effects: No serious or irreversible from malabsorption, a water-miscible injection the ingredients. mg, Cyanocobalamin 1000 µg; in ampoules.
preparation may be administered intramuscularly. Pack: 3’s.
adverse effects in recommended doses; high Precautions: Contains lactose and should
intake may cause birth defects; transient POM Retinol (WMF 27) be avoided in galactosemia, the syndrome of OTC NEUROSANBE® (Zoomota)
increased intracranial pressure in adults or a Tablet, (sugar-coated), Retinol (as palmitate) 10 malabsorption of glucose and galactose or Tablet, Thiamine mononitrate (Vitamin B1) 100 mg,
tense and bulging fontanelle in infants (with 000 IU. a deficit in lactase (rare metabolic diseases). Pyridoxine HCl (Vitamin B6) 200 mg, Cyanocobalamin
high dosage); massive overdose can cause Capsules, Retinol (as palmitate) 50,000 IU, 100,000 Avoid during pregnancy and breastfeeding. (Vitamin B12) 200 mcg; f-c tab.
IU, 200 000 IU. Pack: 10 x 10’s (in strips)
rough skin, dry hair, enlarged liver, raised Adverse effects: Skin allergy, digestive disor-
Oral solution, (oily), Retinol (as palmitate) 100 000 Tablet, Thiamine mononitrate (Vitamin B1) 100 mg,
erythrocyte sedimentation rate, raised serum IU/mL; in multidose dispenser.
ders, agitation, headaches, tremor and malaise;
Pyridoxine HCl (Vitamin B6) 100 mg, Cyanocobalamin
EMDEX
calcium and raised serum alkaline phosphatase Water-miscible injection, Retinol (as palmitate) 100 contains sunset yellow (avoid in those allergic (Vitamin B12) 5000 mcg; s-c tab.
concentrations. 000 units/mL; in 2-mL ampoule. to dyes). Pack: 10 x 10’s (in strips)
Advice to patients: Avoid use of mineral oil Dose: By mouth, Adult only, 2-3 tablets daily.
POM Retinol (EDL 28.1) OTC NEUROTAB® (United African Lab)
when taking drug; take with food for better To be swallowed whole with a large
Tablets or Capsules, Vitamin A 1.5 mg (5000 IU), 7.5 Tablet, Vitamin B1 100 mg, Vitamin B12 200 mcg.
absorption; notify physician of nausea, vom- mg (25,000 IU), 15 mg (50,000 IU). glass of water, dividing the doses
Pack: 10’s
iting, anorexia, malaise, drying or cracking of between the morning and midday
skin or lips, irritability, headache, or loss of hair. OTC AQUAVIT®-A (Synergy) meals. Duration of treatment is lim- OTC RE-B® Forte (Mark)
Nursing action: Do not give by IV push; pa- Capsule, Vitamin A USP (as palmitate) 50,000 IU Tablet, Thiamine mononitrate 250 mg, Pyridoxine
ited to 4 weeks.
(equiv. to retinol 15 mg ) in water soluble form. HCl 250 mg, Cyanocobalamin 100 mcg; film-coated
tients receiving more than 25,000 units per
Pack: 3 x 10’s (in blisters). tab.
day should be closely monitored for toxicity. THIAMINE
POM AROVIT® (Swipha) Pack: 10 x 10’s (in blisters).
• Teach patient nutritional sources of vitamin A Synonym: Vitamin B1 Dose: By mouth, 2-3 tablets daily for 7-10 days.
viz yellow and deep green leafy vegetables, Tablet, (Chewable), Synthetic Vitamin A 50,000 IU;
Indications: Prevention and treatment of Maintenance dose: 1 tablet daily.
orange coated tab.
liver and egg yolk. vitamin B1 deficiency.
Dose: Prevention of vitamin A deficiency OTC ARVITA® (Rohi) OTC SPADOSE® (Crystal)
Precautions: Parenteral administration (see
Capsule, Vitamin A (as palmitate) 25000 IU Tablet, Thiamine mononitrate (vitamin B1) 50 mg,
(universal or targeted distribution notes above); breastfeeding (Appendix 3).
Pack: 1 x 24’s pyridoxine HCI (vitamin B6) 100 mg, cyanocobalamin
programmes), by mouth, INFANT Advice to patients: Dietary sources include (vitamin B12) 100 mcg.
under 6 months, 50 000 units, 6–12 legumes, pork, beef, whole grains, yeast, fresh Pack: 10’s; 100’s
months, 100 000 units every 4–6 RIBOFLAVIN
vegetables.
months, preferably at measles vacci- Synonym: Vitamin B2 Dose: Mild chronic thiamine deficiency, by VITAMIN B COMPLEX
nation; CHILD over 1 year (preschool), Indications: Vitamin B2 deficiency. mouth, ADULT 10–25 mg daily. Indications: General deficiency states of the
200 000 units every 4–6 months; Advice to patients: Take with food (absorption
OTC Thiamine (WMF 27) B-Vitamins; supplementation of diet; adjuct
ADULT, 200 000 units every 6 months; is enhanced by food); large doses may cause
Tablet, Thiamine HCl 50 mg. to treatment withbroad spectrum antibiotics.
ADULT pregnant woman, maximum bright yellow or orange urine; dietary sources
OTC Vitamin B1 (EDL 28.1)
Dose: 1-2 tabs daily or 5-10 mL syrup daily.
of 10 000 units daily or maximum 25 of riboflavine include liver, kidney, dairy
Tablets, Thiamine (as HCl) 25 mg, 50 mg. Infants and Young Children: 2.5 mL
000 units weekly; ADULT MOTHERS, products, green vegetables, eggs, whole grain
daily. Older Children (School age):
200 000 units at delivery or within 8 cereals, yeast, mushroom.
VITAMIN B12 plus VITAMIN 2.5-5 mL daily
weeks of delivery. Dose: Treatment of vitamin B2 deficiency, by B6 plus VITAMIN B1
Note: An additional dose should be given the next mouth, ADULT and child up to 30 mg OTC Vitamin B Complex (EDL 28.1)
day in hospitalized children with measles infection. Indications: Vitamin B6 deficiency symptoms, Tablet or Capsule or Syrup, See the EDL-approved
daily in divided doses.
Treatment of xerophthalmia, by adjuvant in neuralgias and neuritis, sciatica, doses of various vitamins at the beginning of this
Prophylaxis of vitamin B2 deficiency,
mouth, INFANT under 6 months, 50 lumbago. Chronic intoxications, especially chapter.
by mouth, ADULT and child 1–2 mg
000 units on diagnosis, repeated next alcoholism. As adjuvant in radiation injuries. OTC AFRABLEX® (Afrab-Chem)
daily.
day and then after 2 weeks; 6–12 Interaction: Increased pyridoxine will decrease Tablet or Syrup, Vitamin B Complex.
POM Riboflavin (WMF 27) levodopa effect.
months, 100 000 units immediately Tablets, Riboflavin 5 mg. POM BACO® (Award Global)
on diagnosis, repeated next day and Dose: By mouth, 1-2 tabs to be taken with
Injection,Vitamin B1 10 mg, vitamin B6 1 mg, vitamin
then after 2 weeks; CHILD over 1 POM Riboflavin (EDL 28.1) liquid every day.
B2 1.37 mg, nicotinamide 15 mg, calcium pantoth-
year and ADULT (except woman of Tablet, Riboflavin 5 mg By IM injection, 1 amp. daily. enate 0.5 mg per mL.
Pack: 2 mL x 10’s Pack: 2 mL x 100’s. mark on one side. eral oil. Delayed absorption of iron. Increased
Pack: 1000’s. effect of oral anticoagulants.
OTC B-BES® (GoldMoore) OTC EM-B-PLEX® (Emzor)
Dose: Adult, one tablet 3 times daily. Adverse effects: Rarely nausea, diarrhoea,
Tablet, Vitamin B1 1 mg, Vitamin B2 1 mg, Vitamin B6 Tablet, Vitamin B Complex.
Child, one tablet 1-2 times daily. intestinal cramps.
1 mg, Nicotinamide 15 mg; s-c tab. Pack: 100’s
Pack: 3 x 10’s. Syrup, Vitamin B Complex. OTC Vitamin B Complex (Gauze) Nursing action: Advise patient to swallow
Pack: 100 mL; 2 L. Oral liquid, Vitamin B1 5 mg, thiamine HCI 2 mg, capsule whole, not crushed or chewed.
OTC BECOMBEE® (Ranbaxy)
Vitamin B2 (ribloflavin) 2mg, nicotinamide 10 mg • Teach patient symptoms of Vitamin E toxicity
Syrup, Vitamin B Complex. POM GOL-B® (Geneith)
per 5 mL. which include blurred vision, diarrhoea, diz-
Pack: 180 mL. Injection, Vitamin B Complex.
Pack: 100 mL; 2 L
ziness, flu-like symptoms, nausea, headache.
OTC BECOPLEX® (Vitabiotics) POM LABOPLEX® (Embassy)
OTC Vitamin B Complex (Jawa) • Teach patient the dietary sources of Vitamin
Syrup, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6 Injection, Vitamin B complex; in 10 mL vial.
Syrup, Vitamin B1 5 mg, Vitamin B2 2 mg, Vitamin B6 E viz dark green leafy vegetable, nuts, eggs,
2 mg, nicotinamide 20 mg per 5 mL
OTC LIVERCAP® (Embassy) 2 mg, Nicotinamide 20 mg per 5 mL. liver, palm oil, vegetable oils, diary products.
Pack: 100 mL
Capsule, Vitamin B1 6 mg, vitamin B2 6 mg, vitamin Pack: 100 mL x 20’s. Dose: By mouth, Adult, Prophylaxis, 100-300
OTC BECOTONE® (Rajrab) B6 6 mg, nicotinamide 30 mg. mg daily. Treatment, 300-600 mg
OTC Vitamin B Complex (Juhel)
Tablet, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6 Pack: 10’s.
Tablet, Vitamin B Complex. daily.
2 mg, nicotinamide 20 mg; company logo marked
OTC Moko B Complex (New Healthway) Pack: 1000’s
on both sides of the tab. OTC ENAT-400® (Megalife sciences)
Syrup, Thiamine (as HCl) 7.5 mg, riboflavin 2.75 Syrup, Vitamin B1 5 mg, Vitamin B2 2 mg, Nicotina-
Pack: 100’s; 1000’s. Capsule, Vitamin E 400 IU; transparent, oval-shaped
mg, pyridoxine (as HCl) 2.3 mg, nicotinamide 25 mide 20 mg, Pyridoxine 2 mg per 5 mL.
Syrup, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6 softgel cap.
mg per 5 mL. Pack: 100 mL in amber bottle.
2 mg, nicotinamide 20 mg per 5 mL; 100-mL pack 400 IU – 3 x 10’s (in blister)
Pack: 100 mL
marked “RAJRAB” on the cap. OTC Vitamin B Complex (Mopson)
Pack: 100 mL; 2 L Tablet, Vitamin B11.0 mg, vitamin B2 1.0 mg, nico- OTC EPHYNAL® (Swipha)
OTC NABCO® (NASDMU)
Tablet (Chewable), DL alpha-tocopherol acetate 100
EMDEX
Tablet, Vitamin B11 mg, vitamin B2 1 mg, vitamin B6 tinamide 15 mg.
OTC BECOVIX® (Neimeth) mg; cream coloured tab.
0.5 mg, nicotinamide 15 mg; yellow deep concave Pack: 1000.
Tablet, Vitamin B complex. 100 mg – 100.
tab. marked ‘NABCO’ on one side and ‘NASDMU’ on Syrup, Vitamin B1 5 mg, vitamin B2 2.0 mg, vitamin B6
Pack: 100’s.
the reverse. 2.0 mg, nicotinamide 20 mg. OTC EVITOL®(Dizpharm)
Syrup, Vitamin B complex.
Pack: 100’s; 1000’s. Pack: 100 mL, 2 L. Tablet, dl-alpha tocopherol acetate 25 mg (25 IU).
Pack: 100 mL.
OTC Vitamin B Complex (Nomagbon) 25 mg – 25’s.
POM PEMACOMB® (Pemason)
OTC BECOZYM® (Swipha)
Injection, Vitamin B1 10 mg, Vitamin B2 1.37 mg, Syrup, Vitamin B1 5 mg, Vitamin B2 2 mg, Vitamin OTC EYVITINA® (Rohi)
Syrup, Vitamin B Complex; yellow syrup.
Vitamin B 6 1 mg, Niacinamide 15 mg, Sodium B6 2 mg, Nicotinamide 20 mg per 5 mL; yellow Capsule, Tocopherol acetate 100 mg
POM BICOMP® (Fil Pharma) panthotenate 0.5 mg per mL; in 10 mL-vial marked viscous syrup. Pack: 1 x 24’s
Injection, Vitamin B 1 10 mg, vitamin B 2 0.5 mg, “Pemacomb” Pack: 100-mL (in glass bottle).
vitamin B6 1 mg, nicotinamide 10 mg, D-panthenol Pack: 10 mL x 50’s. OTC NATE® (Strides Vital)
OTC Vitamin B Complex (Vitabiotics) Capsule, Vitamin E
1 mg per mL Injection, Vitamin B1 10 mg, Vitamin B2 1.37 mg,
Tablet, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6 Pack: 30’s.
Pack: 10 mL vial. Vitamin B6 1 mg, Nicotinamide 15 mg, Sodium pan-
2 mg, nicotinamide 20 mg.
thotenate 0.5 mg; 2-mL amp. marked “Pemacomb” OTC NATURE CARE® (Al-Tinez)
POM BIO-COMBI® (E-Globa) Pack: 100’s.
Pack: 2-mL x 10 x 10’s. Capsule, Vitamin E 1,000 IU; oblong soft capsule filled
Injection, Vitamin B Complex 10 mL per vial. Syrup, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6
Pack: 10 mL x 50’s OTC SOFA-B® (Sofak) 2 mg, nicotinamide 20 mg. with pale yellow solution.
Syrup, Vitamin B1 5 mg, vitamin B2 2 mg, vitamin B6 Pack: 100 mL. Pack: 50’s; 100’s.
OTC BIOVIT® (Daily Need) Dose: By mouth, Adult, 100-1000 IU per day.
2 mg, nicotinamide 20 mg per 5 mL.
Syrup, Vitamin B Complex. OTC ZEST-UP® (Mecure)
Pack: 100 mL OTC Nature’s Field® Vitamin E (Sylken)
Pack: 180 mL. Tablet, Vitamin B-complex; yellow s-c tab.
Dose: Children: 2.5 mL to 5 mL, two times daily Softgel, Vitamin E (as DL-alpha tocopheryl acetate)
Pack: 3 x 10’s; 500’s
OTC BITOPLEX® (Goldmoore) Adult: 5 mlL to 10 mL, two times daily 1000 IU
Syrup, Nicotinamide 20 mg, Vitamin. B6 2 mg, Vitamin
Syrup, Thiamine HCl 5 mg, riboflavin sodium phos- B1 5 mg, Vitamin B2 5 mg; slightly yellowish syrup. Dose: 1 softgel daily
OTC THERAPLEX® (Therapeutic)
phate 2 mg, pyridoxine HCl 2 mg, nicotinamide 20 Pack: 100 mL.
Syrup, Vitamin B1 3mg, vitamin B2 1 mg, nicotinamide OTC NEWVIT-E® (Pharmabox)
mg per 5 mL
10 mg, vitamin in B6 1 mg; in flavoured base. Capsule, Vitamin E USP 1000 IU (as dl-a-tocopheryl
Pack: 100 mL POM ZARBECO® (Shrezar)
OTC Vitamin B Complex (Dizpharm) Injection, Vitamin B-complex per 10 mL acetate 1000 IU); pale yellow, transparent soft
POM CATOPLEX® (GoldMoore) Pack: 1 x 10’s capsule.
Tablet, Vitamin B1 1 mg, Vitamin B2 1 mg, nicotina-
Injection, Vitamin B1 10 mg, Vitamin B2 1.37 mg, Pack: 50’s.
mide 15 mg; orange-yellow tab. marked ‘B.Co.’
Vitamin B6 1 mg, Nicotinamide 15 mg, Sodium Dose: By mouth, 100-1000 I.U. per day.
D-pantothenate 0.5 mg per mL.
Pack: 100’s; 1000’s. VITAMIN E
Pack: 100 x 2 mL. OTC Vitamin B Complex (Emzor) Synonym: Tocopherols OTC Nutrihealth Vitamin E® (Hovid)
Tablet, Vitamin B Complex; orange-yellow tab. Therapeutic category: Fat Soluble Vitamin; Capsules, d-alpha tocopherol 200 IU
POM COBIS® (Vixa) 200 IU – 50.
marked ‘EMZOR’. Topical Vitamin.
Injection, Vitamins B1 20 mg, B2 4 mg, B6 10 mg,
Pack: 100’s; 1000’s Indications: Vitamin E deficiency resulting OTC SANTA-E® (Zoomota)
Nicotinamide 100 mg, Sodium pantothenate 10 mg.
Syrup, Vitamin B Complex; yellow orange-flavoured from impaired absorption, increased require- Caplet, α-tocopheryl acetate 400 mg
syrup. 400 mg – 25’s (in strips)
ments due to diet rich in polyunsaturated fats;
POM COXON-B® (Beta Drugs) Pack: 100 mL; 2 L.
supplement to parenteral feeding; haemolytic OTC TOCOVID® SupraBio (Hovid)
Injection, Vitamin B1 20 mg, vitamin B2 2.74 mg,
OTC Vitamin B Complex (Evans) anaemia due to Vitamin E deficieny. Capsule, (50 mg), d-α-tocotrienol 15.38 mg, d-y-to-
vitamin B6 2 mg, nicotinamide 30 mg, sodium pan-
Tablet, Vitamin B1 5 mg, B2 2 mg, B6 2 mg, nicotinamide Interactions: Decreased absorption with min- cotrienol 28.20 mg, d-α-tocotrienol 6.42 mg,
tothiocyanate 1 mg per 2 mL ampoule.
20 mg; mottled yellow biconvex tab. with a triangular d-α-tocopherol 22.90 IU, plant squalene 12.82 mg,
274 | 6.6 Minerals 6.6 Minerals | 275
phytosterol complex 5.12 mg, phytocarotenoid Sodium fluoride. Availability of adequate • Phytic acid (in bran and whole cereals), tan- OTC CALCEVIT® (Shalina)
complex 90 µg. fluoride confers significant resistance to dental nins in tea, dietary fibre, and laxatives may Tablet, Calcium carbonate 1.25 g from an organic
Pack: 3 x 10’s; 6 x 10’s caries. It is now considered that the topical ac- decrease absorption of calcium. source (oyster shell) equiv. to elemental calcium 500
Capsule, (100 mg), d-α-tocotrienol 30.76 mg, tion of fluoride on enamel and plaque is more • Dietary sources include milk, yoghurt, cheese, mg, Vitamin D3 250 IU; f-c tab.
d-y-tocotrienol 56.24 mg, d-α-tocotrienol 12.84 mg, Pack: 10 x 15’s
important than the systemic effect. Where the legumes, soya beans, spinach, deep green
d-α-tocopherol 45.80 IU, plant squalene 25.64 mg,
fluoride content of the drinking water is less leafy vegetables. OTC CALCI-D® (Neros)
phytosterol complex 10.24 mg, phytocarotenoid
than 700 µg per litre, daily administration of • Percentage of elemental calcium in: Caplet, Calcium carbonate 750 mg (equiv. to Ca2+
complex 180 µg.
fluoride tablets or drops is a suitable means Calcium gluconate....... 9% 300 mg), Vitamin D 60 IU; f-c caplet.
Pack: 30’s; 60’s
Capsule, (200 mg), d-α-tocotrienol 61.52 mg, d-y-to- of supplementation. Systemic fluoride sup- Calcium lactate.............. 13%
Dose: By mouth, Adult, 1 caplet 3 times daily.
cotrienol 112.80 mg, d-α-tocotrienol 25.68 mg, plements should not be prescribed without Calcium citrate............... 21% Child: 1 caplet 2 times daily.
d-α-tocopherol 91.60 IU, plant squalene 51.28 mg, reference to the fluoride content of the local Calcium carbonate....... 40%
phytosterol complex 20.48 mg, phytocarotenoid water supply; infants need not receive fluoride Dose: Usually 500-1000 mg elemental OTC CALCIFER® (SKP)
complex 360 µg. Capsule, HVP Calcium chelate 20% 300 mg, Calcium
supplements until the age of 6 months at the calcium daily; up to 2000 mg daily in
Pack: 30’s carbonate 270 mg, Magnesium oxide 100 mg,
earliest. Dentifrices which incorporate sodium severe cases.
Calcium ascorbate 50 mg, HVP Iron chelate 10%
OTC Vitamin E (Embassy) fluoride are a convenient source of fluoride. Child (3-7 years): ½ adult dose. 30 mg, Vitamin E 15 IU, Magnesium stearate 9 mg,
Capsule, Vitamin E acetate 1000 IU; soft gelatin cap. Individuals who are either particularly caries OTC Calcium (EDL 28.2) Manganese sulfate 5 mg, Copper Sulfate 2.5 mg,
Pack: 5 x 10’s (in blisters) prone or medically compromized may be given Tablet, Calcium carbonate 600 mg. Vitamin B12 1% 1 mg, Folic acid 10% 0.8 mg, Vitamin
additional protection by the use of fluoride Tablet, Calcium lactate 300 mg. D3 10 mcg, Silicon dioxide 10 mg; white cap.
6.6 Minerals rinses or by application of fluoride gels. Rinses Pack: 30’s
Calcium gluconate. Calcium supplements are OTC CALCITONE® (Adler) Dose: 1capsule daily after meal.
may be used daily or weekly; daily use of a
usually only required where dietary calcium Capsule, Calcium
less concentrated rinse is more effective than Pack: 100’s; 1000’s. OTC CALCIMAX® (Adler)
EMDEX
intake is deficient. This dietary requirement weekly use of a more concentrated one. High- Capsule, Calcium, zinc, vitamin D2.
varies with age and is relatively greater in strength gels must be applied on a regular OTC Calcium Lactate (Emzor) Pack: 30’s.
childhood, pregnancy and lactation due to basis under professional supervision; extreme Tablet, Calcium lactate 300 mg; white biconvex tab. Suspension, Calcium carbonate 150 mg, magnesium
an increased demand, and in old age, due to 300 mg – 500’s; 1000’s. hydroxide 25 mg, vitamin B3 200 i.u. per 5 mL.
caution is necessary to prevent the child from
impaired absorption. In osteoporosis, a calcium swallowing any excess. OTC Calcium Lactate (Juhel) Pack: 100 mL.
intake which is double the recommended For the use of iron preparations in the treat- Tablet, Calcium Lactate 300 mg. OTC CALCITONE-D® (Adler)
daily amount reduces the rate of bone loss. In ment of anaemia see section 6.1. 300 mg – 100. Capsule, Calcium, vitamin D
hypocalcaemic tetany calcium gluconate must OTC Calcium Lactate (Adler) Pack: 100’s; 1000’s.
be given parenterally but plasma calcium must ORAL CALCIUM Tablet, Calcium lactate 300mg. OTC CEECAL® (Joswe/Afrab)
be monitored. Calcium gluconate is also used Indications: Osteoporosis of various origin; 300 mg – 100’s; 1000’s. Effervescent Tablet, Vitamin C 1000 mg, Calcium
in cardiac resuscitation. prevention of pre – and post-menopausal bone carbonate 625 mg, Vitamin D 300 IU., Vitamin B6 5 mg
OTC CALCIUM-SANDOZ® (Novartis)
Iodine is among the body’s essential trace demineralisation; rickets and osteomalacia Tablet (effervescent), Calcium lactate gluconate 2.94 OTC EFFCAL® (Ranbaxy)
elements. The recommended intake of iodine in addition to specific therapy; latent tetany, g plus calcium carbonate 0.30 g (equiv. to 500 mg
is 150 mcg daily (200 mcg daily in pregnant Effervescent tablet, Calcium (as Carbonate) BP 400
increased demand for calcium in pregnant ionizable calcium). mg, Vitamin D3 200 IU; available in orange and
and breast-feeding women); in children the and breast-feeding women, and in growing OTC Ca-C 1000 SANDOZ® (Novartis) lemon flavours.
recommended intake of iodine is 50 µg daily for children; allergic conditions (supportive Pack: 10’s (in tube); 25 x 2’s (in strips).
Effervescent tablet, Calcium lactate gluconate 1 g, cal-
infants under 1 year, 90 mcg daily for children treatment). cium carbonate 0.327 g (equiv. to elemental calcium Dose: 1-2 tablets per day.
aged 2–6 years, and 120 µg daily for children Contra-indications: Hypercalcaemia e.g. in 260 mg), Vitamin C (ascorbic acid) 1 g OTC FIZCAL-D® (Seagreen)
aged 7–12 years. Deficiency causes endemic hyperparathyroidism, vitamin D overdosage, Pack: 10’s Effervescent tablet, Calcium carbonate 625 mg,
goitre and results in endemic cretinism (char- severe hypercalciuria, severe renal failure. Cholecalciferol (Vitamin D3) 200 IU.
OTC CALCIVIT® (Therapeutic)
acterized by deaf-mutism, intellectual deficit, Precautions: Mild hypercalciuria, mild to Pack: 12 x 4’s; 5 x 4’s (in box); 20’s (in tube)
Tablet, Calcium lactate.
spasticity and sometimes hypothyroidism), moderate renal impairment, history of urinary
impaired mental function in children and OTC CLAM-TONE® (Greenlife) OTC OSTEOFORTE® (SKP)
calculi, high doses of vitamin D. Tablet, Calcium lactate pentahydrate 300 mg Capsule, Calcium amino acid chelate 20% 773 mg, Di-
adults and an increased incidence of still-births Interactions: Tetracycline, fluoride prepa- Pack: 100’s, 1000’s calcium phosphate 83 mg, Vitamin D3 (10,000 I.U/g)
and perinatal and infant mortality. Iodine and rations, Vitamin D, milk and milk products, 4 mg, Magnesium amino acid chelate 34 mg, Zinc
Dose: Hypocalcaemia, 2-3 tablets daily Treatment
iodides may suppress neonatal thyroid func- digitalis preparations. oxide 10.2 mg, Manganese amino acid chelate 20%
of calcium depletion, 2 tablets 3 times daily
tion and in general iodine compounds should Adverse effects: Mild GI disturbances such as Prevention of osteoporosis in women, 3-5 10 mg, Copper amino acid chelate 2 mg; white cap.
be avoided in pregnancy. Where it is essential bloating, contipation or diarrhoea. tablets daily. Pack: 30’s
to prevent neonatal goitre and cretinism, Advice to patients: Do not take calcium Child (1-8 years): 1 tablet daily; 9-18 years, 2 Dose: 1capsule daily after meal.
iodine should not be witheld from pregnant supplements within 1-2 hours of taking other tablets daily; 19-50 years, 2 tablets; 50 years OTC PURECAL® (Phillips/Prisma)
women. Control of iodine deficiency largely medicine by mouth or eating large amounts
and above, 3 tablets daily Chewable tablet, Calcium 320 mg, Phosphorus
depends upon salt iodization with potassium Pregnant & Lactating women, 2 tablets daily (source milk) 137.5 mg.
of fiber-rich foods; do not drink large amounts
iodide or potassium iodate and through dietary of alcohol or caffeine-containing beverages. With Vitamin D and other Minerals Pack: 3 x 10’s (in blisters).
diversification. In areas where iodine deficiency Dose: 1-2 tablets daily.
• Nursing action: Calcium carbonate requires OTC CAL D3® (Embassy) Suspension, Calcium 160 mg, Phosphorus (source
disorders are moderate to severe, iodized oil food for absorption; calcium citrate is best Tablet, Calcium lactate 500 mg, vitamin D3 250 IU milk) 69 mg, Vitamin D3 200 mg per 5 mL.
given either before or at any stage of preg- absorbed regardless of food. Pack: 30’s. Pack: 200 mL.
nancy is found to be beneficial.
276 | 6.6 Minerals 6.7 Appetite Stimulants | 277
CALCIUM GLUCONATE and ADULT 380 mg (aged over 45 unbalanced or restricted diets; Prolonged sugar coated tab.
Indications: Hypocalcaemic tetany. years or with nodular goitre, 76 mg parenteral feeding; Acute or chronic diarrhea. Pack: 3 x 10’s; 1 x 10’s
but see also Precautions) (provides up Treatment for Zinc deficiency. Indications: As a source of vitamins for prevention/
Contra-indications: Conditions associated
to 3 years protection). Digestive disorders e.g. Anorexia, dyspepsia, correction of dietary deficiency in case of convales-
with hypercalcaemia and hypercalciuria (for cence, low caloric & restricted diets etc.
example some forms of malignant disease). Iodine deficiency, by mouth, ADULT mild constipation, nausea and vomiting dur-
Precautions: Monitor plasma calcium concen- (except during pregnancy) and CHILD ing pregnancy. Insomnia, asthenia, headache.
GLUTODINE plus ARGININE
tration; renal impairment; sarcoidosis; history above 6 years, 400 mg once a year; Recurrent infections in respiratory tract, diges-
ADULT during pregnancy, single dose tive tract and of the skin. Xeroderma, delayed Therapeutic category: Orexigenic
of nephrolithiasis; interactions: Appendix 1.
of 200 mg; INFANT under 1 year, sin- healing of wound (burn and decubitus ulcer). Description: An oral solution containing a
Adverse effects: GI disturbances; bradycardia,
gle dose of 100 mg; CHILD 1–5 years, Xerophthalmia, cormeal ulcer, nuctalopia. combination of Glutodine (Cyproheptadine
arrhythmia; injection-site reactions; peripheral
200 mg once a year. Precautions: Avoid use in active gastro-duo- plus α-Ketoglutarate) and Arginine aspartate
vasodilation; fall in blood pressure.
denal ulcer or nausea. Allow a 2-3 hour interval indicated for anorexia and asthenia.
Dose: Hypocalcaemic tetany, by slow IV injec- POM Iodine (WMF 27.2)
between administration of Zinc and other Indications: Treatment of all processes where
tion, ADULT 1 g (2.2 mmol) followed Capsule, Iodine 200 mg.
drugs containing calcium, iron and copper. it is necessary to restor the intake of basic
by continuous IV infusion of about 4 Oral or injectable liquid, Iodized oil 1 mL (480 mg
Interactions: Concomitant use of tetracycline, elements involved in an energising activa-
g (8.8 mmol) daily. iodine), 0.5 mL (240 mg iodine) in ampoule; 0.57 mL
(308 mg iodine) in dispenser bottle. ciprofloxacin, drugs containing iron, copper, tion; asthenia and psychoasthenia, anorexia,
POM Calcium gluconate (WMF 27) malnutrition, convalescence, reduction of
Note: Iodized oil may also be given by mouth. decreases the GI absorption of zinc.
Injection, Calcium gluconate 100 mg/mL; in 10-mL intellectual capacity, slow growth, adynamia,
ampoule. Adverse effects: Rarely stomach discomfort
SODIUM FLUORIDE during the first few days of treatment. school fatigue.
POM Calcium gluconate (Alpha) Dose: Nutritional supplement, ½-2 tablets Contra-indications: Pregnancy & lactation;
Indications: Prevention of dental caries.
Injection, Calcium gluconate 10% (2.2 mmol Ca2+ in daily as needed. infants.
Contra-indications: Not for areas where
EMDEX
10 mL); in 10-mL amp.
Treatment for deficiency, based on Precautions: Renal and hepatic impairment;
Pack: 10 mL x 10’s drinking water is fluoridated or where fluorine
patient’s need and tolerance; reduce Elderly; Prostate hypertrophy; Narrow angle
content is naturally high.
POM CATOSIUM® (GoldMoore) dose as symptoms improve glaucoma. May impair ability to drive or op-
Adverse effects: In recommended doses
Injection, Calcium gluconate 10%. Administer in 2 divided doses, to be erate machinery.
toxicity unlikely; occasional white flecks on
Pack: 50 x 10 mL.
taken after meals. Adverse effects: Drowsiness; dry mouth.
teeth at recommended doses; rarely yellow-
Calcium Chloride Injection For Child: Crush the tablets, add some Dose: See below.
ish-brown discoloration if recommended doses
POM Calcium chloride (Alpha) are exceeded. sugar then dissolve in warm water POM DYNAMOGEN® (Oculus)
Injection, Calcium chloride BP 14.7% (5 mmol of Ca2+ Nursing action: Tablets may be dissolved in before use. Oral solution, Glutodine 3 mg (Cyproheptadine 1
in 5 mL); in 10-mL amp. the mouth or sucked and taken preferably in mg + α-Ketolutarate 2 mg), Arginine aspartate 1 g,
OTC FARZINCOL® (Neros) Saccharose 4.224 g per 10 mL.
Pack: 10 mL x 10’s the evening. Tablet, Zinc gluconate 70 mg (equiv. to 10 mg of Pack: 10 ml x 20’s
• When using mouthwashes, rinse mouth for Zinc). Dose: Adult, by mouth, 10 mL 3 times daily.Children:
IODINE 1 minute and spit out (most effective when 70 mg – 10 x 10’s. 10 mL twice daily. To be taken preferably 30
Indications: Prevention and treatment of used immediately after brushing teeth). mins before main meals.
iodine deficiency. Avoid eating, drinking, or rinsing mouth for 6.7 Appetite Stimulants
Contra-indications: Breastfeeding (Appendix 15 minutes after use. Cyproheptadine is a serotonin and histamine 6.8 Solutions for correcting
3). • Avoid giving with milk or dairy products. antagonist with anticholinergic and sedative water, electrolyte and
Precautions: Over 45 years old or with nodular Dose: Prevention of dental caries, as oral properties. Also has calcium channel-blocking acid-base disturbances
goitre (especially susceptible to hyperthyroid- rinse, CHILD over 6 years, 10 mL property.
6.8.1 Oral electrolyte solutions
ism when given iodine supplements—iodized 0.05% solution daily or 10 mL 0.2% Pizotifen has an appetite-stimulating ac-
6.8.2 Parenteral electrolyte solutions
oil may not be appropriate); may interfere with solution weekly. tion suitable for increasing body weight in 6.8.3 Water
thyroid-function tests; pregnancy (see notes Note: Fluoridated toothpastes are also a convenient underweight anorectic patients. In elderly
above and Appendix 2). source of fluoride for prophylaxis of dental caries. people, pizotifen has been shown to improve 6.8.1 Oral electrolyte solutions
Adverse effects: Hypersensitivity reactions; POM Sodium fluoride (WMF 27) disturbed mood by alleviating symptoms such
goitre and hypothyroidism; hyperthyroidism. as hopelessness, feeling of dejection or op- 6.8.1.1 Oral rehydration – See section 4.4.1
In any appropriate topical formulation.
6.8.1.2 Oral potassium
Dose: Endemic moderate to severe iodine defi- Note: Sodium fluoride may be used in any appro- pression, asthenia, anxiety, restlessness, sleep
ciency, by IM injection, ADULT women priate topical formulation. disturbances, and impairment of concentration
of child-bearing age, including any or memory. Also used for the prophylaxis of 6.8.1.2 Oral potassium
POM Sodium fluoride (EDL 28.2) Compensation for potassium loss is necessary
stage of pregnancy, 480 mg once Tablet, Sodium fluoride 2.2 mg. equiv. to 1 mg migraine.
each year; by mouth, ADULT during in patients taking digoxin or antiarrhythmic
fluoride
pregnancy and one year postpartum, CYPROHEPTADINE drugs where potassium depletion may induce
See section 18.6 for Sodium flouride mouthwash. arrhythmias. It is also necessary in patients
300–480 mg once a year or 100–300
See also under Section 8.1 with secondary hyperaldosteronism (renal
mg every 6 months; women of child-
bearing age, 400–960 mg once a year ZINC GLUCONATE artery stenosis, liver cirrhosis, the nephrotic
OTC UPFINE® (Award Global)
or 200–480 mg every 6 months. Indications: Dietary supplement of Zinc: In syndrome, severe heart failure) and those
Tablet, Cyproheptadine HCI 4 mg, vitamin A (as
Iodine deficiency, by IM injection, case of: Rickets, low birth weight; Pregnancy, acetate) 1600 IU, vitamin D3 200 IU, thiamine HCI
with excessive loss of potassium in the faeces
INFANT up to 1 year, 190 mg; CHILD lactation and convalescence; Vegetarism, 2 mg, riboflavin 2 mg, cyanocobalamin 1 mcg, (chronic diarrhoea associated with intestinal
nicotinamide 15 mg, calcium pantothenate 5 mg; malabsorption or laxative abuse).
278 | 6.8.2 Parenteral electrolyte solutions 6.8.2 Parenteral electrolyte solutions | 279
Measures to compensate for potassium loss • Include potassium rich food in the diet viz ill patients it is often helpful to monitor the ing insulin infusion.
may also be required in the elderly since they banana, orange juice, avocado pears, carrots. right atrial (central) venous pressure. If glucose or sugar cannot be given orally to
often take inadequate amounts in the diet • Advise patient to avoid OTC products viz Chronic hyponatraemia should ideally be man- treat hypoglycaemia, glucose 50% may be
(but see warning on use in renal insufficiency, antacids, vitamin preparations and salt sub- aged by fluid restriction. However, if sodium given intravenously into a large vein through
below). Measures may also be required during stitutes unless on prescription. chloride is required, the deficit should be a large-gauge needle; this concentration is very
long-term administration of drugs known to Dose: Prevention of hypokalaemia (see notes corrected slowly to avoid risk of osmotic demy- irritant on extravasation and it is also viscous
induce potassium loss (for example, corticos- above), by mouth, ADULT 20–50 elination syndrome; the rise in plasma-sodium and difficult to administer. Larger volumes
teroids). Potassium supplements are seldom mmol daily after meals. concentration should not exceed 10 mmol/ of less concentrated glucose solutions (10%
required with the small doses of diuretics Potassium depletion (see notes litre in 24 hours. In severe hyponatraemia, or 20%) can be used as alternatives and are
given to treat hypertension. Potassium-sparing above), by mouth, ADULT 40–100 intravenous infusion of sodium chloride 1.8% less irritant.
diuretics (rather than potassium supplements) mmol daily in divided doses after may be used with caution. Sodium hydrogen carbonate (sodium bicar-
are recommended for prevention of hypokal- meals: adjust dose according to se- The more physiologically appropriate com- bonate) is used to control severe metabolic
aemia due to diuretics such as furosemide or verity of deficiency and any continu- pound solution of sodium lactate can be used acidosis (as in renal failure). Since this condition
the thiazides when these are given to eliminate ing loss of potassium. instead of isotonic sodium chloride solution is usually attended by sodium depletion, it is
oedema (see section 5.2.3). POM Potassium chloride (WMF 26.1)
during surgery or in the initial management reasonable to correct this first by the adminis-
For the prevention of hypokalaemia doses of Powder for solution. of the injured or wounded. tration of isotonic sodium chloride intravenous
potassium chloride 2 to 4 g (approx. 25 to 50 Sodium chloride and glucose solutions are infusion, provided the kidneys are not primarily
mmol) daily by mouth are suitable in patients POM Potassium chloride (EDL 26.1) indicated when there is combined water and affected and the degree of acidosis is not so
Tablet, (slow-release), Potassium chloride 600 mg
taking a normal diet. Smaller doses must be sodium depletion. A 1:1 mixture of isotonic severe as to impair renal function. In these
Oral Solution, Potassium chloride 5%, 10%, 20%.
used if there is renal insufficiency (common sodium chloride and 5% glucose allows some circumstances, isotonic sodium chloride alone
in the elderly) otherwise there is a danger of POM Apo-K (Lahams) of the water (free of sodium) to enter body cells is usually effective as it restores the ability of
EMDEX
hyperkalaemia. Tablet, Potassium chloride 600 mg; orange, f-c which suffer most from dehydration while the the kidneys to generate bicarbonate. In renal
slow-release tab. marked ‘APO-K 600’.
Larger doses may be required in established sodium salt with a volume of water determined acidosis or in severe metabolic acidosis of any
600 mg – 1000’s.
potassium depletion, the quantity depending by the normal plasma Na+ remains extracel- origin, for example blood pH <7.1, sodium hy-
on the severity of any continuing potassium lular. Combined sodium, potassium, chloride, drogen carbonate (1.4%) may be infused with
loss (monitoring of plasma potassium and
6.8.2 Parenteral electrolyte solutions and water depletion may occur, for example, isotonic sodium chloride when the acidosis
Solutions of electrolytes are given intrave-
specialist advice required). with severe diarrhoea or persistent vomiting; remains unresponsive to correction of anoxia
nously, to meet normal fluid and electrolyte
Potassium depletion is frequently associated replacement is carried out with sodium chlo- or fluid depletion; a total volume of up to 6
requirements or to replenish substantial
with metabolic alkalosis and chloride depletion ride IV infusion 0.9% and glucose IV infusion litres (4 litres of sodium chloride and 2 litres of
deficits or continuing losses, when the patient
and these disorders require correction. 5% with potassium as appropriate. sodium hydrogen carbonate) may be necessary
is nauseated or vomiting and is unable to take
Glucose solutions (5%) are mainly used to in the adult. In severe shock due for example
POTASSIUM CHLORIDE adequate amounts by mouth.
replace water deficits and should be given to cardiac arrest, metabolic acidosis may
The nature and severity of the electrolyte
Indications: Prevention and treatment of alone when there is no significant loss of develop without sodium depletion; in these
imbalance must be assessed from the history
hypokalaemia (see notes above). electrolytes. Average water requirement in circumstances sodium hydrogen carbonate
and clinical and biochemical examination of
Contra-indications: Severe renal impairment; a healthy adult are 1.5 to 2.5 litres daily and is best given in a small volume of hypertonic
each individual. Sodium, potassium, chloride,
plasma potassium concentration above 5 this is needed to balance unavoidable losses solution (for example 50 mL of 8.4% solution in-
magnesium, phosphate, and water depletion
mmol/litre. of water through the skin and lungs and to travenously); plasma pH should be monitored.
can occur singly and in combination with or
Precautions: Elderly, mild to moderate renal provide sufficient for urinary excretion. Water Sodium hydrogen carbonate is also used in the
without disturbances of acid-base balance.
impairment (close monitoring required, Ap- depletion (dehydration) tends to occur when emergency management of hyperkalaemia.
Isotonic solutions may be infused safely into a
pendix 4), history of peptic ulcer; important: these losses are not matched by a comparable Intravenous potassium chloride in sodium
peripheral vein. More concentrated solutions,
special hazard if given with drugs liable to intake, as for example may occur in coma or chloride infusion is the initial treatment for the
for example 20% glucose, are best given
raise plasma potassium concentrations such as dysphagia or in the elderly or apathetic who correction of severe hypokalaemia when suf-
through an indwelling catheter positioned in
potassium-sparing diuretics, ACE inhibitors or may not drink water in sufficient amount on ficient potassium cannot be taken by mouth.
a large vein.
ciclosporin, for other interactions: Appendix 1. their own initiative. Potassium chloride concentrate may be added
Sodium chloride in isotonic solution provides
Adverse effects: Nausea and vomiting, GI Excessive loss of water without loss of elec- to sodium chloride 0.9% infusion, thoroughly
the most important extracellular ions in near
irritation. trolytes is uncommon, occurring in fevers, mixed, and given slowly over 2 to 3 hours with
physiological concentrations and is indicated
Nursing action: Administer with plenty of hyperthyroidism, and in uncommon water-los- specialist advice and ECG monitoring in diffi-
in sodium depletion which may arise from
water and with food to minimize GI distress; ing renal states such as diabetes insipidus or cult cases. Repeated measurements of plasma
conditions such as gastroenteritis, diabetic
advise patient to completely dissolve powder hypercalcaemia. The volume of glucose solu- potassium are necessary to determine whether
ketoacidosis, ileus and ascites. In a severe
or effervescent tablet in glass of water or juice. tion needed to replace deficits varies with the further infusions are required and to avoid
deficit of from 4 to 8 litres, 2 to 3 litres of iso-
• Sustained release and wax matrix tablets severity of the disorder, but usually lies within the development of hyperkalaemia which is
tonic sodium chloride may be given over 2 to
must be swallowed whole and not allowed the range of 2 to 6 litres. especially likely to occur in renal impairment.
3 hours; thereafter infusion can usually be at
to dissolve in the mouth, not to be crushed Glucose solutions are also given in regimens Initial potassium replacement therapy should
a slower rate.
or chewed. with calcium, bicarbonate, and insulin for the not involve glucose infusions because glucose
Excessive administration should be avoided;
• Teach patient to report symptoms of hyper- emergency treatment of hyperkalaemia. They may cause a further decrease in the plasma-po-
the jugular venous pressure should be as-
kalaemia viz lethargy, confusion, diarrhoea, are also given, after correction of hyperglycae- tassium concentration.
sessed; the bases of the lungs should be exam-
vomiting, fainting, and decreased output. mia, during treatment of diabetic ketoacidosis,
ined for crepitations, and in elderly or seriously
when they must be accompanied by continu-
280 | 6.8.2 Parenteral electrolyte solutions 6.8.2 Parenteral electrolyte solutions | 281
GLUCOSE Infusion, Dextrose water 5%, 10% Injection, (Concentrate for Infusion), Potassium ADULT and CHILD a strong solution
Synonym: Dextrose chloride 15%; clear & colourless soln in 10-mL amp. (up to 8.4%) or by continuous IV
GLUCOSE plus SODIUM CHLORIDE Pack: 8 x 5’s infusion, ADULT and CHILD a weaker
Indications: Fluid replacement without sig-
nificant electrolyte deficit (see notes above); Indications: Fluid and electrolyte replacement. solution (usually 1.4%), an amount
Precautions: Restrict intake in impaired SODIUM CHLORIDE appropriate to the body base deficit
treatment of hypoglycaemia (see Oral Glucose
in section 6.11). renal function, cardiac failure, hypertension, Synonym: Normal saline. (see notes above).
Precautions: Diabetes mellitus (may require peripheral and pulmonary oedema, toxaemia Indications: Electrolyte and fluid replacement.
POM Sodium hydrogen carbonate (WMF 26.2)
additional insulin). of pregnancy. Precautions: Restrict intake in impaired renal
Injectable solution, Sodium hydrogen carbonate
Adverse effects: Glucose injections, especially Adverse effects: Administration of large doses function (Appendix 4), cardiac failure, hyper- 1.4% isotonic (equiv. to Na+ 167 mmol/L, HCO3 –
if hypertonic, may have a low pH and cause may give rise to oedema. tension, peripheral and pulmonary oedema, 167 mmol/L).
venous irritation and thrombophlebitis; fluid Nursing action: See under Glucose. toxaemia of pregnancy. Solution, Sodium hydrogen carbonate 8.4% (equiv.
and electrolyte disturbances; oedema or water Dose: Fluid replacement, by IV infusion, Adverse effects: Administration of large to Na+ 1000 mmol/L, HCO3 – 1000 mmol/L); in 10-
ADULT and CHILD determined on doses may give rise to sodium accumulation mL ampoule.
intoxication (on prolonged administration or
rapid infusion of large volumes of isotonic the basis of clinical and, whenever and oedema. POM Sodium hydrogen carbonate (EDL 26.2)
solutions); hyperglycaemia (on prolonged possible, electrolyte monitoring (see Nursing action: Avoid excessive adminis- Injection, Sodium hydrogen carbonate 8.4% (equiv.
administration of hypertonic solutions). notes above). tration to Na+ 1000 mmol/L and HCO3 – 1000 mmol/L); in
Nursing action: Control infusion carefully, Dose: Fluid and electrolyte replacement, 10-mL amp.
POM Glucose plus sodium chloride (WMF 26.2)
note that maximal rate of infusion is 0.5g/ by IV infusion, ADULT and CHILD POM Sodium Bicarbonate (Alpha)
Injectable solution, Glucose 4%, sodium chloride
kg b.wt hourly; do not infuse concentrated 0.18% (equiv. to Na+ 30 mmol/L, Cl – 30 mmol/L).
determined on the basis of clinical Injection, Sodium hydrogen carbonate 8.4%; in 10
solutions rapidly, may cause hyperglycaemia and, whenever possible, electrolyte mL amp.
POM Glucose plus Sodium Chloride (EDL 26.2) monitoring (see notes above).
and fluid shift.
EMDEX
Infusion, Glucose 4.3%, Sodium chloride 0.18%.
• Do not give Dextrose without saline solutions POM Sodium chloride (WMF 26.2) SODIUM LACTATE,
Infusion, Glucose 5%, Sodium chloride 0.9%. COMPOUND SOLUTION
in blood transfusions; may cause clumping Injectable solution, Sodium chloride 0.9% isotonic
POM Dextrose Saline (Dana) (equiv. to Na+ 154 mmol/L, Cl– 154 mmol/L). Synonym: Hartmann’s solution; Ringer’s lac-
of blood cells.
Infusion, Dextrose (anhydrous) 5%, sodium chloride tate injection.
• Observe closely for signs of overloading 0.9 g, water for injection in normal saline per 100 mL. POM Sodium chloride (EDL 26.2) Indications: Pre – and perioperative fluid and
where fluid intake is restricted. Pack: 500 mL Injection, Sodium chloride 0.9% (equiv. to Na+ 154
electrolyte replacement; hypovolaemic shock.
• Check infusion site regularly to prevent Infusion, Dextrose (anhydrous) 4.3%, sodium chlo- mmol/L and Cl– 154 mmol/L).
Injection, Sodium chloride 0.45% (equiv. to Na+ 77 Contra-indications: Metabolic or respiratory
irritation or extravasation and phlebitis; ride 0.18 g, water for injection q.s per 100 mL.
mmol/L and Cl– 77 mmol/L). alkalosis; hypocalcaemia or hypochlorhydria.
change site immediately if there is sign of Pack: 500 mL
Precautions: Restrict intake in impaired renal
extravasation. POM Dextrose Saline (Juhel) POM Normal Saline (Dana)
function, cardiac failure, hypertension, pe-
• Monitor I&O, VS, temperature (increasing Infusion, Dextrose 5% in normal saline. Infusion, Sodium chloride 0.9 g, water for injection
ripheral and pulmonary oedema, toxaemia of
fever may be sign of infection). Pack: 500 mL; 1000 mL q.s per 100 mL
Pack: 100 mL; 500 mL pregnancy; interactions: Appendix 1.
Dose: Fluid replacement, by IV infusion,
Adverse effects: Excessive administration may
ADULT and CHILD determined on POTASSIUM CHLORIDE POM Normal Saline (Juhel) cause metabolic alkalosis; administration of
the basis of clinical and, whenever Indications: Electrolyte imbalance; see also Infusion,Sodium chloride 0.9%.
large doses may give rise to oedema.
possible, electrolyte monitoring (see oral potassium (section 6.8.1.2). Pack: 500 mL; 1000 mL
Nursing action: Administer I.V. slowly to
notes above). Precautions: For IV infusion the concn of solu- POM Normal Saline (Watson) prevent pain at infusion site; check for ex-
Treatment of hypoglycaemia, by IV tion should not usually exceed 3.2 g (43 mmol)/ Infusion, Sodium chloride 0.9% travasation.
infusion of 50% glucose solution into litre; specialist advice and ECG monitoring (see • Observe patient closely for symptoms of
a large vein, ADULT, 25 mL (see also notes above); renal impairment (Appendix 4); SODIUM HYDROGEN CARBONATE alkalosis viz irritability, confusion, twitching,
notes above). interactions: Appendix 1. Synonym: Sodium bicarbonate hyper-reflexia, slow respiration, cyanosis,
POM Glucose (WMF 26.2) Adverse effects: Cardiac toxicity on rapid Indications: Metabolic acidosis. irregular pulse.
Injectable solution, Glucose 5%; 10% (isotonic); 50% infusion. Contra-indications: Metabolic or respiratory • Avoid in patient with severe acidosis because
(hypertonic). Dose: Electrolyte imbalance, by slow IV infu- alkalosis, hypocalcaemia, hypochlorhydria. rapid replacement of serum bicarbonate is
POM Glucose (EDL 26.2) sion, ADULT and CHILD depending on Precautions: Restrict intake in impaired renal required and sodium lactate is slowly metab-
Infusion, Dextrose 5, 10, 50% in water for injection the deficit or the daily maintenance function (Appendix 4), cardiac failure, hyperten- olised to bicarbonate by the liver.
requirements (see also notes above). sion, peripheral and pulmonary oedema, tox- Dose: Fluid and electrolyte replacement or
POM Dextrose (Dana) Administration: Must be diluted and thoroughly
Infusion, Dextrose (anhydrous) 5%, 10%, 50% per aemia of pregnancy; monitor electrolytes and hypovolaemic shock, by IV infusion,
mixed before use and administered according to
100 mL in water for injection. acid-base status; interactions: Appendix 1. ADULT and CHILD determined on
manufacturer’s directions.
5% – 500 mL (in PVC Pouches) Adverse effects: Excessive administration may the basis of clinical and, whenever
10% – 1000 mL (in PVC Pouches) POM Potassium chloride (WMF 26.2) cause hypokalaemia and metabolic alkalosis, possible, electrolyte monitoring (see
50% – 100 mL (in PVC Pouches) Solution, Potassium chloride 11.2% (equiv. to K+ 1.5 especially in renal impairment; large doses may notes above).
mmol/mL, Cl– 1.5 mmol/mL); in 20-mL ampoule. give rise to sodium accumulation and oedema.
POM Dextrose (Juhel) POM Compound sodium lactate solution (WMF
Infusions, Dextrose 5%, 50% in WFI. POM Potassium chloride (EDL 26.2) Nursing action: Check IV site regularly to 26.2)
5% – 500 mL; 1000 mL. Injection, Potassium chloride 15% (equiv. to K+ 2 avoid extravasation which may cause tissue Injectable solution, Compound solution of sodium
50% – 100 mL. mmol/L and Cl– 2 mmol/L). sloughing, ulceration and necrosis. lactate.
POM Dextrose 5% (Watson) POM Potassium Chloride (Alpha) Dose: Metabolic acidosis, by slow IV injection,
282 | 6.8.3 Water 6.10 Parenteral nutrition | 283
POM Compound sodium lactate solution (EDL POM Water for injection (EDL 26.2) bowel disease. but if more than 180g is given per day, frequent
26.2) Injection, Water for injection in 2 mL, 5 mL, 10 mL, Precautions: Care required with technique to monitoring of blood glucose is required and
Injection, Compound Sodium Lactate Solution BP. 20 mL & 50 mL amps or vials. reduce risk of infection; warm dialysis solution insulin may be necessary. Fat emulsions
POM Ringer’s Lactate (Dana) POM Water for injection (Dortemag) to body temperature before use; some drugs have the advantages of a high energy to fluid
Injection, Sodium lactate 1.5 g, sodium chloride 3.0 Pack: 10 mL x 100’s may be removed by dialysis. volume ratio, neutral pH, and iso-osmolarity
g, potassium chloride 0.2 gm, calcium chloride 0.135
POM Sterilised Water for Injection (Jawa)
Adverse effects: Infection, including peritoni- with plasma and provide essential fatty acids
g, water for injection q.s per 100 mL. tis; hernia; haemoperitoneum; hyperglycae- (e.g. Intralipid).
Injection, Water for injection
Pack: 500 mL mia, protein malnutrition; blocked catheter. PN therapy commences with a regimen that
Pack: 5 mL, 10 mL
POM Ringer Lactate Solution (Juhel) Dose: Individualized according to clinical will supply per 24 hrs approx 25-33% of the
POM IVEE AQUA STERILE® (Dortemag)
Infusion, Ringer lactate solution. condition, and based on blood patient’s calculated energy and protein re-
Injection, Water for injection
Pack: 500 mL. results. quirements. Following each 24-hour period,
Pack: 10 mL
POM Intraperitoneal dialysis solution (WMF 23)
the therapy is advanced as tolerated. Thus, the
DARROW’S SOLUTION average adult patient will receive 100% of the
6.9 Peritoneal dialysis solution Parenteral solution, Intraperitoneal dialysis solution
Indications: Dehydration by loss of intestinal Solutions for peritoneal dialysis are prepara- of appropriate composition. estimated goal for energy and nitrogen at the
fluid, Correction of metabolic acidosis, hypo- tions for intraperitoneal use which contain end of the third or forth day.
POM Intraperitoneal Dialysis Fluid BPC (EDL 13)
kalaemia in diabetic coma. electrolytes in a similar concentration to that Commerably available PN solutions include
Parenteral solution, Intraperitoneal dialysis solution
Contra-indications: Acute renal insufficiency, in plasma, and also contain glucose or another of appropriate composition. Aminoplasmal (L5, 10 or Ped), Aminoplex (5,
hyperkalaemia, alkalosis. suitable osmotic agent. Peritoneal dialysis 12, 14, 24), FreAmine, Intralipid (10%, 20%).
Precautions: Pregnancy, Normal Circulation solutions always contain sodium, chloride, 6.10 Parenteral nutrition Potential complications of PN include hydro-
and diuresis to be restored before infusion. and hydrogen carbonate or a precursor; they Parenteral nutrition (PN) is indicated only thorax, pneumothorax, catherter embolism,
Dose: 1 Litre over a period of 5 hours; max. of may also contain calcium, magnesium, and when adequate nutritional intake cannot be arterial puncture, air embolism, myocardial
EMDEX
40-80 mL per kg body weight daily by rarely potassium. provided by the oral route. Candidates for perforation, sepsis, thrombosis, hyper-hypo-
slow IV infusion or SC injection. In renal failure haemodialysis is the preferred PN include patients suffering GI disease or glycaemia, hyperammonaemia, hypokalaemia,
POM Darrow’s Solution (EDL 26.2) method to correct the accumulation of toxins, injury or who are undernourished and are hypo-magnesaemia, hypocalcaemia acidosis/
Injection, Darrow’s Solution BP, Half strength & Full electrolytes and fluid. Peritoneal dialysis is less being prepared for surgery, chemotherapy or alkalosis.
strength. efficient than haemodialysis, but it is preferred radiation therapy. PN is also indicated in major
FAT EMULSIONS
POM Darrows Solution (Dana) in children, diabetic patients, and patients with surgery, trauma or burns, prolonged coma or
Injection, Sodium lactate 1.475 g, sodium chloride unstable cardiovascular disease; it is also used refusal to eat and in some patients with renal Indications: As a source of calories and essen-
1.0 g, potassium chloride 0.65 g, water for injection in patients who can manage their condition, or hepatic failure. tial fatty acids for patients requiring parenteral
q.s per 100 mL; half strength. or those who live far from a dialysis centre. It To maintain energy balance and tissue synthe- nutrition for extended periods of time (usually
Pack: 500 mL; 1000 mL is unsuitable for patients who have had signif- sis, human beings require adequate sources for more than 5 days) and as a source of essen-
Solution, Sodium lactate 2.95 g, sodium chloride 2.0 icant abdominal surgery. of protein, carbohydrates, fats, electrolytes, tial fatty acids for prevention of essential fatty
g, potassium chloride 1.30 g, water for injection q.s acid deficiency.
In peritoneal dialysis, the solution is infused vitamins, minerals and water. Thus, any total
per 100 mL; full strength. Contra-indications: Avoid use in patients with
Pack: 500 mL; 1000 mL into the peritoneal cavity, where exchange feeding concept must account for all seven ba-
of electrolytes takes place by diffusion and sic categories. The components of PN solution disturbances of normal fat metabolism such as
POM Darrow’s Solution (Dizpharm) convection, and excess fluid is removed by include (see Table 6A below). pathologic hyperlipemia, lipoid nephrosis or
Infusion, Potassium Chloride, Sodium Chloride and acute pancreatitis if accompanied by hyper-
osmosis, using the peritoneal membrane as Table 6A – Nutrient Substrates in PN Solution
Sodium Lactate. lipidemia. Severe liver damage, pulmonary
Full Strength: 500 mL
an osmotic membrane. There are two forms Sources
of peritoneal dialysis: Energy Dextrose, Intravenous fat emulsions disease, anemia or blood coagulation disor-
Half Strength: 500 mL
• continuous ambulatory peritoneal dialysis (CAPD), Nitrogen Crystalline amino acids, protein hydrolysates ders, or when there is danger of fat embolism.
POM Darrow’s Solution (Juhel) in which dialysis is performed manually by the Precautions: Monitor patient’s ability to elimi-
Infusion, Darrow’s solution half strength. patient several times each day. Electrolytes Injectable salts of sodium, potassium, magnes- nate the infused fat thru regular determination
Pack: 500 mL. • automated peritoneal dialysis (APD), in which sium, calcium, Chloride, Phosphate, acetate. of serum triglycerides. Avoid overdosage.
dialysis is performed by machine overnight. Monitor liver function tests (discontinue if
MANNITOL Vitamins Injectable fat-soluble vitamins (A, D, E, K)
The main complication of peritoneal dialysis and water-soluble vitamins (B1, B2, B6, B12, abnormal); platelet count esp. in children.
is peritonitis, which often results from poor C, nicotnic acid, pantothenic cid, biotin, Adverse effects: Sepsis at injection site, throm-
See Osmotic Diuretics section 5.2.4
exchange technique; infections of the catheter folic acid). bophlebitis. Less frequently, dyspnea, cyanosis,
exit site may also occur, again because of poor Trace Commercially available or extemporaneous
Minerals preparations including iron, zinc, copper, allergic reactions, hyperlipemia, hypercoagu-
6.8.3 Water technique. With long-term dialysis progressive manganese, chromium, iodide, selenium. lability, nausea, vomiting, headache, flushing,
structural changes to the peritoneal membrane Water Sterile water for injection. increase in temperature, sweating, sleepiness,
WATER FOR INJECTIONS occur, ultimately resulting in dialysis failure.
Protein is given as mixtures of essential and pain in the chest and back, slight pressure over
Indications: In preparations intended for the eyes, dizziness, and irritation at the site of
non-essential synthetic L-amino acids. Energy
parenteral administration and in other sterile INTRAPERITONEAL DIALYSIS SOLUTION infusion. Rarely, thrombocytopenia in neonates;
is provided for the utilisation of amino acids
preparations. Indications: To correct electrolyte imbalance delayed adverse reactions such as hepatomeg-
for tissue maintenance. A mixture of fat (30 –
POM Water for injection (WMF 6.10.3) and fluid overload, and to remove metabolites, 50%) and carbohydrate gives better utilisation aly, jaundice due to central lobular cholestasis,
Injection, Sterile distilled water free from pyrogens; in renal failure. of amino acid solutions than glucose alone. splenomegaly, thrombocytopenia, leukopenia,
in 2-mL, 5-mL, 10-mL ampoules. Contra-indications: Abdominal sepsis; previ- Glucose is the preferred source of carbohydrate transient increases in liver function tests, and
ous abdominal surgery; severe inflammatory
284 | 6.10 Parenteral nutrition 6.10 Parenteral nutrition | 285
overloading syndrome (focal seizures, fever, Dose: Adult: 200-800 mL IV per day treat negative nitrogen balance in infants and Infants <10 kg b.wt, 2.0 to 2.5 g/kg/
leukocytosis, hepatomegaly, splenomegaly Child: 0.2-0.25 g of Nitrogen/kg b.wt. young pediatric patients where day
and shock). Drip Rate: 15-20 drops initially fol- • the alimentary tract, by the oral, gastrostomy, For infants and young children >10 kg
Dose: To be administered as a part of IV nu- lowed by 30-40 drops per minute. or jejunostomy route, cannot or should not be b.wt, 20 – 25 g/day for the first 10 kg
trition via perpheral vein or by central used, or adequate protein intake is not feasible of b.wt plus 1 – 1.25 g/day for each kg
POM MEKOAMIN®-S (Neros) by these routes;
venous infusion. Infusion, L-Isoleucine 750 mg, L-Lysine HCI 3.075 mg, of b.wt over 10 kg.
• gastrointestinal absorption of protein is impaired;
Dosage dependent on patient’s L-Tryptophan 250 mg, L-Threonine 750 mg, L-Valine or
See product literature for details.
response and ability to eliminate 825 mg, L-Phenylalanine 1,200 mg, L-Methionine Note: The objective of nutritional management of
• protein requirements are substantially increased
the administered fat. Daily dosage 1,000 mg, L-Leucine 1,700 mg, Glycine 1,425 mg, infants and young paediatric patients is the provi-
as with extensive burns.
should not exceed 2.5 g of fat/kg b.wt L-Histidine 550 mg, Xylitol 12,500 mg, Excipients sion of sufficient amino acid and caloric support for
Dosage, route of administration, and concom- protein synthesis and growth.
Infused fat should make up no more sq. for 250 mL.
itant infusion of non-protein calories are de- The total daily dose depends on daily protein
than 60% of the total caloric input Pack: 250 mL (in bottle).
pendent on various factors, such as nutritional requirements and on the patient’s metabolic
to the patient. Carbohydrate and a Indications: Amino acids supply in the follow-
and metabolic status of the patient, anticipated and clinical response. The determination of
source of amino acids should com- ing conditions: hypoproteinemia, malnutrition,
duration of parenteral nutritional support, and nitrogen balance and accurate daily body
prise the remaining caloric input. pre and post operations.
vein tolerance. weights, corrected for fluid balance, are prob-
Administration: Follow manufacturer’s directions. Contra-indications: Hepatic coma; severe
Contra-indications: Hypersensitivity to one ably the best means of assessing individual
Do not use any bag in which there appears to be an renal disorder or hyperazotemia; abnormality
or more amino acids present in the solution; protein requirements.
oiling out on the surface of the emulsion. Parenteral of amino acid metabolism.
Untreated anuria, hepatic coma, inborn errors Dosage should also be guided by the patient’s
drug products should be inspected visually for Adverse effects: Fever, infection of the infu-
particulate matter and discoloration prior to admin- of amino acid metabolism. fluid intake limits and glucose and nitrogen
sion site, thrombosis, hypervolemia, nausea,
istration. Whenever solution and container permit. Precautions: Clinical evaluation and periodic tolerances, as well as by metabolic and clinical
vomiting, chest pain, tachycardia may be
laboratory determinations are necessary to
EMDEX
(Additional information sourced from Intralipid® monograph observed. If there are signs of hypersensitiv- response.
available from: http://www.accessdata.fda.gov/drugsatfda_docs/ monitor changes in fluid balance, electrolyte
ity such as skin rash, the infusion should be (Additional information sourced from Trophamine® monograph
label/2007/017643s072,018449s039lbl.pdf) concentrations, and acid-base balance. See
discontinued. available from: http://www.accessdata.fda.gov/drugsatfda_docs/
product literature for details. label/2004/19018scs018_trophamine_lbl.pdf)
POM Fat Emulsion (Pemason) Dose: By slow IV infusion, Adult, usually
Dose: Recommended dosages:
Infusion, (10%), Soybean oil 10 g, egg lecithin 1.2 30-40 drops/min. May adjust dosage
g, glycerol 2.2 g per 100 mL; white, homogenous based on the age, b. wt. and status of
emulsion marked “10% Fat Emulsion Injection” the patient.
Pack: 500 mL (in glass vial)
POM TROPHAMINE® 6% (Alpha)
Infusion, (20%), Soybean oil 20 g, egg lecithin 1.2
Injection, L-Isoleucine 490 mg, L-Leucine 840 mg,
g, glycerol 2.2 g per 100 mL; white, homogenous
L-Lysine acetate 690 mg (as L-Lysine 490 mg),
emulsion marked “20% Fat Emulsion Injection”
L-Methionine 200 mg, L-Phenylalanine 290 mg,
Pack: 500 mL (in glass vial)
N-acetyl-L-Tyrosine 120 mg (all L-Tyrosine 144 mg),
L-Proline 410 mg, L-Serine 230 mg, Glycine 220 mg,
AMINO ACID INJECTIONS L-Threonine 250 mg, L-Tryptophan 120 mg, L-Valine
See under the preparations below. 470 mg, L-Histidine 290 mg, L-Tyrosine 44 mg,
L-Alanine 320 mg, L-Arginine 730 mg, L-Aspargic
POM ASTYMIN-SN® (Fidson) acid 190 mg, L-Glutamic acid 300 mg, Aminoethyl
Infusion, Each mL contains: L-Isoleucine 5.6 mg, sulfonic acid 15 mg, HCI-L-Cysteine 20 mg, Sodium
L-Leucine 12.5 mg, L-Lysine HCl 11 mg, L-Methionine bisulfite (as an antioxidant) 50 mg, Water for injec-
3.5 mg, L-Phenylanine 9.35 mg, L-Threonine 6.5 tion qs 100 mL
mg, L-Tryptophan 1.3 mg, L-Valine 4.5 mg, L-Alanine Pack: 200 mL
6.2 mg, L-Arginine HCl 9.55 mg, L-Aspartic acid 3.8 Pharmacology: TrophAmine provides a
mg, L-Cysteine HCl 1.45 mg, L-Glutamic acid 6.5 mixture of essential and nonessential amino
mg, L-Histidine HCl H2O 8.11 mg, L-Proline 3.3 mg, acids as well as taurine and a soluble form
L-Serine 2.2 mg, L-Tyrosine 0.35 mg, Glycine 10.7 mg, of tyrosine, N-Acetyl-L-Tyrosine (NAT). This
Xylitol 50 mg, Water for injections q.s. amino acid composition has been specifically
Pack: 200 mL (in type-1 bottle).
formulated to provide a well-tolerated nitrogen
Indications: Internal medicine – Persistent source for nutritional support and therapy for
pyrexial states, Severe malnutrition, Malignant infants and young pediatric patients. When
diseases, Malabsorption in G.I. disorders. Sur- administered in conjunction with cysteine HCl,
gery – Pre & Post operative conditions, Burns, TrophAmine results in the normalization of the
Accidental trauma, Fracture of long bones. plasma amino acid concentrations to a profile
Contraindications: Cardiac insufficiency, consistent with that of a breast-fed infant.
irreversible liver damage Indications: Nutritional support of infants (in-
Precautions: Signs of intolerance and including those of low birth weight) and young
creased renal losses resulting in amino acids pediatric patients requiring TPN via either
disequilibrium are possible, if infusion rate is central or peripheral infusion routes; Parenteral
too high. nutrition to prevent nitrogen and weight loss or
7.1 Antiasthmatic and drugs for chronic obstructive pulmonary disease | 287
7. Drugs acting on the 7.1 Antiasthmatic and drugs egies for avoiding common triggers such as:
for chronic obstructive • Indoor allergens such as house dust mites in
pulmonary disease bedding, carpets and stuffed furniture; pollution
and pet dander
respiratory tract
7.1.1 Bronchodilators • Outdoor allergens such as pollens and moulds
7.1.2 Corticosteroids • Tobacco smoke
7.1.3 Prophylactic drugs • Cold air
Definition of asthma: • Emotional stress including anger or fear,
7.1 Antiasthmatic and drugs for chronic obstructive pulmonary disease. . . . . . . . 287 The US National Heart, Lung and Blood Institute • Physical exercise
• NSAIDs (e.g., Aspirin); Beta-blockers (e.g., Pro-
7.1.1 Bronchodilators. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 290 (NHLBI) defined asthma as a chronic inflamma-
pranolol).
tory disorder of the airways characterised by
7.1.2 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 297 recurrent episodes of coughing (particularly Treatment objectives
7.1.3 Prophylactic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 300 at night or early in the morning), wheezing, Asthma cannot be cured but can be con-
breathlessness, and chest tightness. These trolled through proper treatment and patient
7.2 Expectorants and cough suppressants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 302 education.
episodes are usually associated with wide-
Compound Cough Preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 303 spread but variable airflow obstruction that is The goal of chronic asthma management is to
often reversible either spontaneously or with achieve and maintain control of the disease.
7.3 Other drugs acting on the respiratory tract . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 309 This can be achieved through a continuous
treatment.
Obstruction of airflow is caused by bronchos- cycle of ATM:
pasm (smooth muscle contraction), airway • Assessment for asthma control,
• Treatment to achieve control, and
oedema and formation of thick & dry mucous
• Monitoring to maintain control.
plugs.
EMDEX
The treatment objectives have been broadly
Airway inflammation and
classified into 2 namely:
remodelling in asthma
• Reduction of impairment from frequent and/
Current pathophysiology of asthma indicates or severe asthma symptoms as well as prevent
that airway inflammation is not limited to limitations of the patient’s activity due to such
severe asthma. Inflammation can be present symptoms (e.g., cough, chest tightness, wheezing,
in mild, moderate and severe asthma. or shortness of breath).
As the asthma progresses, the inflammatory • Reduction of risk of asthma exacerbations, poor
processes can lead to structural changes in lung development and pharmacologic adverse
the airways described as airway remodelling. effects.
The fallout of these changes is the thickening Stepwise approach for managing
of the airway wall as well as changes in the chronic asthma
epithelial tissues lining the bronchial passages. Asthma can be divided by its severity into inter-
Remodelling means that the reversibility of mittent, mild persistent, moderate persistent,
airflow obstruction following asthma episodes and severe persistent. Treatment is initiated
in some patients may be incomplete (even with based on asthma severity (see Table 1).
treatment). A stepwise approach to pharmacologic therapy
Consequences of airway remodelling in- is recommended and the goal is to achieve
clude bronchial hyperresponsiveness, airway control as quickly as possible. This is achieved
oedema, mucous hypersecretion. Remodelling by starting the patient on a treatment most
or persistent changes in the airway structures appropriate to the severity of their asthma
may predispose patients to asthma exacerba- symptoms. Control is achieved and maintained
tions and even death from airway obstruction. by stepping up treatment as needed and step-
Asthma triggers ping down when possible to reduce adverse
Exposure to aeroallergens, irritants or pol- effects from the medications.
lutants can increase the risk for asthma Prior to making any changes to the treatment
symptoms in young children. They may also regimen, it is important to assess the patient’s
be contributory factors in difficult-to-control compliance with the current medication, their
or a worsening asthma condition. Identifying inhalation technique and presence of triggers
and reducing exposure to risk factors should (e.g., allergens or pollutants) that may be
be included in the written Asthma Action Plan, worsening the condition.
specific for the individual patient. Recommendations for treatments in the differ-
Avoidance measures should be recommended ent steps are outlined in Table 1 (i.e., for adults
with the following objectives: reduce expo- and children >5 years).
sure to potential triggers, improve control of Please refer to Chapter 13 of EMDEX Paediatric Drug
asthma, and reduce medication needs. Guide for Asthma Management in children <5 years.
Work with the patient/family to develop strat-
288 | 7.1 Antiasthmatic and drugs for chronic obstructive pulmonary disease 7.1 Antiasthmatic and drugs for chronic obstructive pulmonary disease | 289
Table-1: TREATMENT OF CHRONIC ASTHMA: ADULTS AND CHILDREN OVER 5 YEARS instruction in the use of pressurized (aerosol) Oral: The oral route is used when administra-
Preferred treatments in bold print inhalation (using a metered-dose inhaler) to tion by inhalation is not possible. Systemic
Steps Long‐term preventive (daily medications) Quick relief
obtain optimum benefit from their medica- adverse effects occur more frequently when a
tion. For the proper use of the pressurised drug is given orally rather than by inhalation.
Short‐acting inhaled
metered-dose aerosol inhalers: Drugs given by mouth for the treatment of
beta2‐agonist as needed
for symptoms. Intensity of • Shake the aerosol canister before each use and asthma include beta2-agonists, corticosteroids,
treatment will depend on remove the cap. leukotriene-receptor antagonists [not included
STEP 1
None needed. severity of attack. Inhaled • After exhaling as completely as possible, place the on the 15th WHO Model List], and theophylline
Intermittent asthmaa
beta2‐agonist or sodium mouthpiece of the inhaler well into the mouth and
cromoglicate or a leukotriene [not included on the 15th WHO Model List].
close the lips firmly around it.
receptor antagonist before Parenteral: Drugs such as beta2-agonists, cor-
• Tilt your head back slightly to form as straight
exercise or exposure to allergen
a channel as possible to maximise the depth of ticosteroids, and aminophylline [not included
Short‐acting inhaled beta2 airway penetration by the drug. on the 15th WHO Model List] may be given
Either inhaled corticosteroidb (beclometasone, 100‐250
STEP 2 agonistc as needed for • Inhale deeply and slowly through the mouth while
Mild persistent asthma
µg twice daily) or sodium cromoglicate or modified‐release
symptoms (not to exceed 3‐4 by injection in acute severe asthma when
theophylline or a leukotriene receptor antagonist
times daily)
simultaneously actuating the inhaler. A higher administration by nebulization is inadequate
concentration of the drug will be deposited in the
Inhaled corticosteroid (beclometasone, 100‐500 µg twice
or inappropriate. If the patient is being treated
lung after a slow inhalation as compared to a fast
daily) inhalation because more drug reaches the airways in the community, urgent transfer to hospital
plus if needed
instead of impacting on the large airways. The should be arranged.
either Short‐acting inhaled
STEP 3 depth of inhalation also enhances the amount of Asthma during Pregnancy & Breastfeeding
Long‐acting bronchodilators (long‐acting inhaled beta2‐ beta2‐agonistd as needed for
Moderate persistent drug retained by the lung.
asthma
agonist or modified‐release theophylline) or a leukotriene symptoms (not to exceed 3‐4 Poorly controlled asthma in pregnant women
receptor antagonist or long‐acting oral beta2‐agonist times daily) • Hold your breath for about 5-10 seconds (or as
or
can have an adverse effect on the fetus,
long as is comfortable) after inhalation to prevent
EMDEX
High‐dose inhaled corticosteroid (beclometasone, over 1 exhaling particles of drug which would normally
resulting in perinatal mortality, increased
mg daily in divided doses)
deposit in the lung due to gravitational effects. prematurity and low birth weight. For this
High‐dose inhaled corticosteroid (beclometasone, over 1 • Remove the mouthpiece and exhale slowly reason, using medications to obtain optimal
mg daily in divided doses) • Allow 5-10 minutes for the first inhaled dose to take control of asthma during pregnancy is justified.
plus effect and repeat the above procedure if a second Administration of drugs by inhalation during
Long‐acting inhaled beta2‐agonist twice daily Short‐acting inhaled inhalation is prescribed.
STEP 4 plus if needed beta2‐agonistf as needed for
pregnancy has the advantage that plasma
Severe persistent asthma Modified‐release theophyllinee or a leukotriene receptor symptoms (not to exceed 3‐4
• Clean the inhaler thoroughly; remove the metal drug concentrations are not likely to be high
antagoniste or long‐acting oral beta2‐agoniste or oral times daily) canister and rinse the plastic case and cap thor- enough to have an effect on the fetus. Acute
corticosteroid in the lowest dose possible, best given as a oughly under running water at least once a week.
exacerbations should be treated aggressively
single morning dose (use soluble tablets if necessary for • Air-dry the plastic case and cap; and put the metal
younger children) canister back into the case with a twisting motion,
in order to avoid fetal hypoxia; if available, ox-
and then put the cap back on. ygen should be given immediately to maintain
If control of asthma is not achieved or is lost, consider stepping up treatment, however, first
STEP UP adequate oxygenation.
review patient medication technique and compliance. • Do not store the inhaler near heat or an open flame
because its contents are under pressure. Inhaled drugs, oral prednisolone and oral the-
If control of asthma is maintained for at least 3 months, gradually decrease maintenance
STEP DOWN It is important to check that patients continue ophylline can be taken during breastfeeding.
treatment to determine the minimum level of treatment required.
NOTE: Inhaled corticosteroids given through metered‐dose inhalers should be administered with large‐volume spacer
to use their inhalers correctly as inadequate Chronic obstructive pulmonary disease
devices (an face‐mask if appropriate); inhaled bronchodilators given through metered‐dose inhalers may also be technique may be mistaken for drug failure.
administered with large‐volume spacer devices if necessary. If patient is unable to take inhaled drugs even with large‐
Decline in lung function in chronic obstructive
volume spacer devices and face‐mask if appropriate, then consider administration via a nebulizer
Use of spacers: pulmonary disease (COPD), chronic bronchitis,
Spacing devices provide a space between the or emphysema, is reduced by cessation of
a. Patients with intermittent asthma but severe exacerbations should be treated as having moderate persistent asthma
b. Alternative to inhaled corticosteroids less effective.
inhaler and the mouth. They may be of benefit smoking. Infection can complicate chronic
c. Alternatives to short‐acting inhaled beta2‐agonist are inhaled ipratropium, short‐acting oral beta2‐agonist and short‐acting for patients such as the elderly, small children, obstructive pulmonary disease and may be
theophylline; these alternatives have slower onset of action or higher risk of side‐effects. and asthmatics who find inhalers difficult to prevented by vaccination, for example, with
d. Alternatives to short‐acting inhaled beta2‐agonist are inhaled ipratropium, short‐acting oral beta2‐agonist and short‐ acting
use, or for those who have difficulty synchro- the influenza vaccine (section 17.1.2.1).
theophylline; these alternatives have slower onset of action or higher risk of side‐effects.
e. Also can be used as alternative to long‐acting inhaled beta2‐agonist if necessary (although long‐acting inhaled beta2‐agonist nizing their breathing with administration of A limited trial of a high-dose inhaled corti-
is preferred). the aerosol. A large-volume spacing device is costeroid or an oral corticosteroid is recom-
f. Alternatives to short‐acting inhaled beta2‐agonist are inhaled ipratropium, short‐acting oral beta2‐agonist and short‐acting also recommended for inhalation of high doses
theophylline; these alternatives have slower onset of action or higher risk of side‐effects mended for patients with moderate airflow
of corticosteroids to reduce oropharyngeal obstruction to ensure that asthma has not
Assess level of asthma control in 2-6 weeks Asthma medications: Methods deposition which can cause candidosis. The
of administration
been overlooked. Chronic obstructive pul-
and adjust treatment based on level of asthma use of metered dose inhalers with spacers is monary disease may be helped by an inhaled
control. Follow-up with patient in 1-6 month Inhalation: The main advantage of delivering less expensive and may be as effective as use short-acting beta2-agonist or an anticholiner-
intervals, considering 3 month interval if step drugs directly into the airways via inhalation of nebulizers, although drug delivery may be gic (antimuscarinic) bronchodilator (ipratro-
down in therapy is anticipated. Inhaled corti- is that high concentrations can be delivered affected by choice of spacing device. pium bromide), used as required; when the
costeroids may be reduced by 25-50% every more effectively and rapidly to the airways, and Breath-actuated devices, including dry powder airways obstruction is more severe, regular
3 months to lowest dose needed to maintain systemic adverse effects avoided or minimized. inhalers, are also available. ipratropium bromide should be added. A
control. Patient should be referred if asthma Solutions for nebulization are available for use
INSTRUCTIONS FOR THE USE METERED-DOSE long-acting beta2-adrenoceptor agonist, for
is not responding to treatment. Consider re- in acute severe asthma. They are administered
INHALERS (MDI) example, salmeterol [not included on the 15th
ferral for children <5 years if control is not over a period of 5–10 minutes from a nebulizer,
It is important that patients receive careful WHO Model List] is added in those who remain
achieved at step 2. usually driven by oxygen in a hospital setting.
290 | 7.1.1 Bronchodilators 7.1.1 Bronchodilators | 291
symptomatic or have 2 or more exacerbations theophylline, may benefit from a slow intrave- and prevention of EIB. Increasing use of SABA enediamine) which is 20 times more soluble in
in a year; if these measures fail to improve nous infusion of aminophylline. treatment or the use of SABA >2 days a week water than theophylline alone. It is used rarely
symptoms, theophylline can be tried. The use of epinephrine (adrenaline) in asthma for symptom relief (not prevention of EIB) by slow intravenous injection for the manage-
Moderate to severe disease may be treated has generally been superseded by beta2-selec- generally indicates inadequate asthma control ment of severe asthma attacks.
with an inhaled corticosteroid and a long-act- tive adrenoceptor agonists. and the need for initiating or intensifying an- Anticholinergic (antimuscarinic)
ing beta2-adrenoceptor agonist; if no benefit ti-inflammatory therapy. Regularly scheduled, bronchodilators
is seen after 4 weeks, treatment should be Treatment should never be delayed for inves- daily, chronic use of SABA is not recommended.
tigations, patients should never be sedated SAA (Short-acting anticholinergics e.g.,
discontinued. Exacerbations of chronic ob- When salbutamol is given by inhalation, at
and the possibility of pneumothorax should Ipratropium) inhibit muscarinic cholinergic
structive pulmonary disease are treated with doses in the range of 100–200 µg, the effect
be considered. Patients who deteriorate fur- receptors and reduce intrinsic vagal tone of
nebulized bronchodilators and oxygen if nec- can last as long as 4 hours thus making it
ther despite treatment may need intermittent the airway. Ipratropium bromide provide short-
essary; a short course of an oral corticosteroid suitable for both the treatment (see tables on
positive pressure ventilation. term relief in chronic asthma, but short-acting
should be given for increased breathlessness. treatement of chronic asthma) and prevention
beta2-agonists (SABA) work more quickly and
Infection requires antibacterial treatment. Medications used for asthma management of asthma. Salbutamol can also be taken orally
are usually preferred; ipratropium bromide is
Long-term oxygen therapy prolongs survival Medications for asthma management are in a dose of 2–4 mg up to 4 times daily but is
also added to standard treatment regimens
in patients with severe chronic obstructive categorized into two general classes: less effective and causes more adverse effects.
where asthma is life-threatening or when an
pulmonary disease and hypoxaemia. • Long-term control medication, and It can also be given by injection for severe
acute attack does not respond to standard
Acute exacerbation of asthma • Quick-relief medication. bronchospasm.
therapy. Ipratropium bromide is also used as
Quick-relief medications are used to treat acute Cardiovascular adverse effects (arrhythmias,
Severe asthma can be fatal and must be a bronchodilator in chronic obstructive pul-
symptoms and exacerbations. They include palpitations, and tachycardia) may occur with
treated promptly and energetically. Acute se- monary disease.
SABA (short-acting beta2-agonist), Anticho- salbutamol, but are generally infrequent with
vere asthma attacks require hospital admission inhaled preparations. Hypokalaemia may
linergics, Oral systemic corticosteroids, etc. SALBUTAMOL
EMDEX
where resuscitation facilities are immediately also result from beta2-adrenoceptor agonist
Long-term control medications are used daily
available. therapy. Particular caution is required in severe Salbutamol is a representative beta2-adrenoceptor ago-
to achieve and maintain control of persistent
Severe asthma is characterized by persistent asthma because this effect may be potentiated nist. Various drugs can serve as alternatives.
asthma. They include ICS (inhaled corticoster-
dyspnoea (even at rest) that is poorly relieved by concomitant treatment with xanthines (for ex-
oids), LABA (long-acting beta2-agonist), etc. Synonym: Albuterol.
by bronchodilators, exhaustion, a high pulse ample, theophylline), corticosteroids, or diuretics
rate (usually more than 120/minute), a high See under sections 7.1.1, 7.1.2, & 7.1.3 below. Therapeutic category: Selective beta2-ago-
and by hypoxia. Plasma potassium concentrations nist; Bronchodilator, Sympathomimetic.
respiratory rate, and a very low peak expira- should be monitored in severe asthma.
References: Indications: Prophylaxis and treatment of
tory flow.
1) WHO Model Formulary, 2008 edition. Long-acting beta2-agonist or LABAs (e.g., Salmet- asthma.
As asthma becomes more severe, wheezing
2) Fahy JV, Corry DB, Boushey HA. Airway erol and Formoterol) are inhaled bronchodilators Precautions: Hyperthyroidism, myocardial
may be absent. Patients should be given
inflammation and remodelling in asthma. that have a duration of bronchodilation of at insufficiency, arrhythmias, susceptibility
oxygen 40–60% (if available) (see also section
Curr Opin Pulm Med. 2000 Jan;6(1): 15-20 least 12 hours after a single dose. Not for use as to QT-interval prolongation, hypertension,
3.1.3). Patients should also be given a beta2-ag-
3) Fanta CH. An overview of asthma man- monotherapy for long-term control of asthma. pregnancy (high doses should be given by
onist, salbutamol or terbutaline [not included
agement. In: UpToDate, Basow, DS (Ed), Recommended for use in combination with ICSs inhalation because parenteral use can affect
on the 15th WHO Model List] via a nebulizer,
UpToDate, Waltham, MA, 2013. [updated for long-term control and prevention of symp- the myometrium and possibly cause cardiac
preferably driven by oxygen. In emergencies
2013 Mar 12; cited 2013 Aug 14]. Available toms in moderate or severe persistent asthma problems; see also notes above); breastfeeding
where a nebulizer is not available, salbutamol,
from: http://www.uptodate.com/. Login (Step 3 care or higher in children ≥5 years of age (Appendix 3); diabetes mellitus—especially IV
100 µg by aerosol inhalation can be repeated
required. and adults). Of the adjunctive therapies available, administration (monitor blood glucose; ke-
10–20 times, preferably using a large-volume
4) National Heart, Blood and Lung Institute. LABA is the preferred therapy to combine with ICS toacidosis reported); interactions: Appendix 1.
spacing device. If life-threatening features are
Guidelines for diagnosis and management in youths ≥12 years of age and adults. Adverse effects: Hypokalaemia after high
present or the response to the beta2-agonist
of asthma. US National Institute of Health, doses (see notes above); arrhythmias, tachy-
is poor, ipratropium bromide can be added Xanthines
2007. Available from: http://www.nhlbi. cardia, palpitations, fine tremor (usually hands),
to the nebulizer. Patients should also be given Xanthines include theophylline and amino-
nih.gov/guidelines/asthma/asthgdln.pdf muscle cramps, headache, insomnia, behav-
a corticosteroid; in adults, the recommended phylline; they relax bronchial smooth muscle
5) British Guideline on the Management ioural disturbances in children; paradoxical
doses are: prednisolone, 30–60 mg by mouth or (relieving bronchospasm) and also stimulate
of Asthma. BTS/SIGN (British Thoracic bronchospasm, urticaria and angioedema also
hydrocortisone, 200 mg (preferably as sodium respiration. Theophylline has a narrow margin
Society/Scottish Intercollegiate Guidelines reported; slight pain on IV injection.
succinate) intravenously; and for children, between therapeutic and toxic effects. At thera-
Network). [updated 2012 Jan; cited 2013 Advice to patients: Do not exceed recom-
prednisolone, 1–2 mg/kg by mouth (1–4 years, peutic doses some patients experience nausea
Aug 21]. Available from: http://www.sign. mended dosage; rinse mouth with water
maximum, 20 mg; 5–15 years, maximum, 40 and diarrhoea and when plasma concentrations
ac.uk/pdf/sign101.pdf following each inhalation to help with dry
mg) or hydrocortisone, 100 mg (preferably exceed the recommended range of 10–20
as sodium succinate) intravenously. In case throat and mouth; follow specific instructions
7.1.1 Bronchodilators mg/litre (55–110 micromol/litre) arrhythmias accompanying inhaler; if more than one inha-
of vomiting, the parenteral route may be pre- and convulsions, which may be fatal, can
ferred for the first dose. Beta2-adrenoceptor agonists (beta2- lation is necessary, wait at least 1 full minute
occur. Monitoring of plasma concentrations is between inhalations. May cause nervousness,
adrenoceptor stimulants)
Most patients do not benefit from the addition therefore recommended. Theophylline is some- restlessness, insomnia; if these effects continue
of intravenous aminophylline or a parenteral Short-acting beta2-agonist or SABAs (e.g., times used to treat asthma and stable chronic after dosage reduction, notify physician; also
beta2-agonist; both cause more adverse effects Salbutamol, Terbutaline) are bronchodilators obstructive pulmonary disease. notify physician if palpitations, tachycardia,
than nebulized beta2-agonists. Nevertheless, that relax smooth muscle. They are the treat- Theophylline is given by injection as amino- chest pain, muscle tremors, dizziness, head-
an occasional patient who has not been taking ment of choice for relief of acute symptoms phylline (a mixture of theophylline and ethyl-
ache, flushing or if breathing difficulty persists. Respirator solution for use in nebulizers, Salbutamol afoate) 25 mcg, fluticasone (as propionate) 125 mcg. per minute. Higher dosages may be used
Nursing actions: Before using, the inhaler (as sulfate) 5 mg/mL. Pack: 120 doses x 1’s especially in patients with respiratory failure.
must be shaken well. Aerosol Inhalation, (25/250 mcg), Salmeterol (as xin- Child: Not recommended.
POM Salbutamol (EDL 15.1)
• Relieve dry mouth with sips of water or gum. afoate) 25 mcg, fluticasone (as propionate) 250 mcg. Preparation of Ventolin Solution for infusion: A
Tablets, Salbutamol (as sulfate) 2 mg, 4 mg
Pack: 120 doses x 1’s suitable solution for infusion may be prepared by
• Do not exceed prescribed dose. Observe Oral liquid, Salbutamol (as sulfate) 2 mg per 5 mL.
Dose: Asthma, Adult & adolescent (>12 years), 2 diluting 5 mL of Ventolin solution for intravenous
patient for wheezing after administration; if Aerosol Inhalation, Salbutamol 100 mcg per me-
inhalations of Salmeflo-50 or Salmeflo-125 infusion in 500 mL of an infusion solution such as
this occurs, call physician. tered dose.
or Salmeflo-250 twice daily. Sodium Chloride and Dextrose Injection B.P to pro-
• Teach patient how to use metered dose Injection, Salbutamol (as sulfate) 50 mcg per mL;
Child (>4 years): 2 inhalations of Salmeflo-50 vide a salbutamol dose of 10 mcg per mL of solution.
in 5-mL amp.
inhaler. or Salmeflo-125 or Salmeflo-250 twice daily.
Respirator solution for use in nebulizers, Salbutamol Salbutamol + Beclometasone
Dose: Chronic asthma (when inhalation is (as sulfate) 5 mg/mL. POM SPALMOTIL® (Mark)
ineffective), by mouth, ADULT 2–4 mg POM SALBAIR-B® Transhaler (Phillips/Lupin)
Note: Oral Salbutamol treatment should only be Tablet, Salbutamol (as sulfate) 2 mg; white/almost
3 or 4 times daily; in some patients Inhalation, Salbutamol BP 100 mcg, Beclometasone
considered when inhaled asthma therapy is not white tab.
dipropionate BP 50 mcg per actuation.
up to maximum of 8 mg 3 or 4 times feasible. 2 mg – 3 x 20’s (in blisters).
Pack: Canister of 200 metered doses.
daily; CHILD under 2 years, 100 µg/ Indications: Treatment of asthma once the need for
POM AEROLINE® (Jubilee) POM SULBUMOL® (Evans)
kg 4 times daily, 2–6 years, 1–2 mg Inhalation, Salbutamo 100 mcg per dose. Inhalation, Salbutamol. inhaled corticosteroid and bronchodilator therapy
3–4 times daily, 6–12 years, 2 mg 3–4 Pack: 200 metered doses. has been established.
times daily. POM VENTAMOL® (Hovid) Contra-indications, Precautions, etc: see under
Severe acute bronchospasm, by slow POM ASMALYN® (Mopson) Tablets, Salbutamol 2 mg, 4 mg. Becometasone and Salbutamol.
Syrup, Salbutamol 2 mg per 5 mL. 2mg – 10 x 10 (blister). Dose: Adult, 2 inhalations 3-4 times daily, titrated to
IV injection, ADULT 250 µg, repeated
Pack: 100 mL, 2 L. 4 mg – 1000 lowest effective dose.
if necessary. Syrup, Salbutamol 2 mg per 5 mL
Relief of acute bronchospasm, by POM BRONCHOREST® (Synergy) Children, 1-2 inhalations 2-4 times daily.
Pack: 100 mL.
EMDEX
aerosol inhalation, ADULT 100–200 Syrup, Salbutamol (as sulfate) 2 mg per 5 mL. Salbutamol + Ipratropium
Pack: 60 mL POM VENTOLIN® (GSK)
µg (1–2 puffs); CHILD 100 µg (1 POM SALBAIR-I® Transhaler (Phillips/Lupin)
Tablets, Salbutamol (as Sulfate) 2 mg, pink tab.
puff ) increased to 200 µg (2 puffs) POM DATRONID® (Pharmabase)
marked ‘AH 1K’ and ‘2’; 4 mg, pink tab. marked ‘AH Inhalation, Salbutamol (as sulfate) 100 mcg, Ipratro-
if necessary; by IM or SC injection, Inhaler, Salbutamol 100 mcg per dose. pium bromide 20 mcg per actuation.
2k’ and ‘4’.
ADULT 500 µg repeated every 4 hours Pack: 200 metered doses in a canister. Pack: Canister of 200 metered doses.
2 mg – 20; 100; 500.
if necessary. POM Dr. Meyer’s Asmacare® (Farmex) 4 mg – 20; 100, 500. Indications: Chronic obstructive pulmonary disease
Prophylaxis of exercise-induced Syrup, Salbutamol 2 mg Syrup, Salbutamol (as Sulfate) 2 mg per 5 mL; (COPD) in patients on regular aerosol bronchodila-
bronchospasm, by aerosol inhalation, Pack: 100 mL fruit-flavoured, sugar– and colouring-free syrup. tors who continue to have evidence of bronchos-
ADULT 200 µg (2 puffs); CHILD 100 µg Pack: 150 mL. pasm and who require a second bronchodilator.
POM JAWABUTAMOL® (Jawa) Inhaler, Salbutamol 100 mcg per dose; metered-dose Contra-indications, Precautions, etc: see under
(1 puff ) increased to 200 µg (2 puffs) Syrup, Salbutamol sulfate aerosol. Ipratropium and Salbutamol.
if required. Pack: 100 mL x 20’s Dose: 2 inhalations 4 times a day; may take ad-
Pack: 200-dose unit.
Chronic asthma (as adjunct in stepped ditional inhalations as required but not
POM SALBAIR® Transhaler (Phillips/Lupin) POM ZOTREX® (Fil Pharma)
treatment), by aerosol inhalation, Inhalation, Salbutamol 100 mcg/dose. exceeding 12 inhalations in 24 hours.
ADULT 100–200 µg (1–2 puffs) up to Tablets, Salbutamol (as sulfate) 2 mg, 4 mg.
Pack: Canister of 200 metered doses. 2 mg – 1000.
3–4 times daily; CHILD 100 µg (1 puff ) SALBUTAMOL plus THEOPHYLINE
POM SALBU-J® (Juhel) 4 mg – 1000.
3–4 times daily, increased to 200 µg (2
Tablet, Salbutamol 4 mg. Other Preparations of Salbutamol POM BROMINOL-F® (N.C.I)
puffs) 3–4 times daily if necessary.
Syrup, Salbutamol 2 mg per 5 mL. Tablet, Salbutamol 2 mg, Theophylline 120 mg;
Severe acute asthma or chronic For Parenteral Use: white tab.
bronchospasm unresponsive to con- POM SABUMALIN® (Novartis)
Pack: 10 x 10’s
ventional treatment, by inhalation of Inhaler, Salbutamol (as sulphate) 100 mg per dose; POM VENTOLIN® (GSK)
nebulized solution, ADULT and CHILD metered-dose aerosol Injection, Salbutamol sulfate 500 mg per mL; colour- POM Salbutamol plus Theophylline (Crystal).
Pack: 200-dose unit. less or faintly straw-coloured solution in a 1ml clear, Tablet, Salbutamol (as sulphate) 2 mg, theophylline
over 18 months, 2.5 mg repeated up
neutral glass amp. (anhydrous) 120 mg.
to 4 times daily; may be increased POM Salbutamol (Emzor)
Tablet, Salbutamol 4 mg; white scored tab. marked Solution for IV infusion, Salbutamol sulfate 1000
to 5 mg if necessary—medical
‘EMZOR 4’. mcg/mL (5 mg per 5 mL); colourless or faintly straw- SALBUTAMOL plus THEOPHYLINE
assessment should be considered coloured solution in a 5 mL clear neutral glass amp. plus CHLORPHENIRAMINE
4 mg – 500.
since alternative therapy may be Note: To be diluted to 50% of the original strength
indicated; CHILD under 18 months, POM Salbutamol (Teta) POM ASMANOL® (Vitabiotics)
before administration.
Inhaler, Salbutamol (as sulfate) 2 mg per 1 mL Tablet, Salbutamol 2 mg, Theophyline 60 mg, Chlor-
clinical efficacy uncertain (transient Parenteral preparations of Ventolin® should not be
Pack: 200’s (with inhalation adapter) pheniramine maleate 2 mg.
hypoxaemia may occur—consider administered in the same syringe or infusion as any
Pack: 24’s (in blisters).
oxygen supplementation). POM Salbutamol (Vitabiotics) other medication.
Indications: For both suppressive and therapeutic
Tablet, Salbutamol (as sulfate) 4 mg. Dose: In severe bronchospasm and status asthmati-
POM Salbutamol (WMF 25.1) use. It is used as a bronchodilator for bronchial
4 mg – 500’s. cus, by SC or IM injection, Adult, 500 mcg (8
Tablets, Salbutamol (as sulfate) 2 mg, 4 mg asthma and for reversible of bronchospasm that may
mcg/kg b.w.), repeated every 4 hours as re-
Oral liquid, Salbutamol 2 mg/5 mL occur in association with bronchitis and emphysema
POM SALMEFLO® (Evans) quired. By slow IV injection, adult, 250 mcg
Injection, Salbutamol (as sulfate) 50 µg/mL; in 5-mL (chronic obstructive pulmonary disease).
Aerosol Inhalation, (25/50 mcg), Salmeterol (as xin- (4 mcg/kg b.wt.), repeated if necessary.By
ampoule. Contra-indications: Sensitivity to any of the
afoate) 25 mcg, fluticasone (as propionate) 50 mcg. IV inusion, Adult, initially 5 mcg per minute,
Inhalation (aerosol), Salbutamol (as sulfate) 100 ingredients; porphyria. Hypertension, myocardial
Pack: 120 doses x 1’s adjusted according to patient response and
µg/dose. insufficiency and hyperthyroidsm.
Aerosol Inhalation, (25/125 mcg), Salmeterol (as xin- heart-rate usually in the range of 3-20 mcg
Dose: Adult, 1 tablet 3 times daily or taken when on effective maintenance doses of long act- POM ESIFLO® Transhaler (Phillips/Lupin) phodiesterase, the enzyme that degrades
asthmatic attack threatens; may increase ing beta agonists and inhaled corticosteroids; Aerosol Inhalation, (25/125 mcg), Salmeterol (as cyclic AMP. It contains theophylline and ethyl-
to 2 tablets 3 times daily in severe cases. Patients who are symptomatic on current xinafoate) 25 mcg, Fluticasone propionate 125 mcg enediamine (2:1). See notes above.
inhaled corticosteriod therapy; Patients on per actuation. Indications: Severe airways obstruction, status
SALMETEROL Pack: Canister of 120 metered doses.
regular bronchodilator therapy who require asthmaticus.
Dose: Adults and adolescents 12 years and older, 2
Therapeutic category: Long acting selective inhaled corticosteriods.Treatment of Chronic Contra-indications: Uncontrolled arrhyth-
puffs twice daily.
beta2-agonist; Bronchodilator. Obstructive Pulmonary Disease (COPD) in- Aerosol Inhalation, (25/250 mcg), Salmeterol (as mias, hyperthyroidism, peptic ulcers, uncon-
Indications: Long-term regular treatment cluding chronic bronchitis and emphysema. xinafoate) 25 mcg, Fluticasone propionate 250 mcg trolled seizure disorders, hypersensitivity to
of reversible airways obstruction in asthma Contra-indications: Hypersensitivity. per actuation. xanthines or any component.
(including patients with nocturnal asthma Precautions: Avoid use in acute attacks (fast Pack: Canister of 120 metered doses. Precautions: Children, elderly, cardiac and
and exercise-induced asthma) and chronic and short acting bronchodilator e.g. salbuta- Dose: Adults and adolescents 12 years and older, 2 liver diseases, history of peptic ulceration,
bronchitis. mol is required); avoid abrupt discontinuation puffs twice daily. breast-feeding, fever, epilepsy. Drug clearance
Precautions: Thyrotoxicosis, pregnancy, of therapy in patients with asthma due to risk POM SERETIDE EVOHALER® (GSK) is accelerated in smokers (may need to adjust
lactation. of excerbation; active or quiescent pulmonary Aerosol Inhalation, (25/50 mcg), Salmeterol 25 mcg, dose).
Interactions: Non-selective beta-blockers such tuberculosis; high doses and prolonged use fluticasone 50 mcg. Interactions: Drugs which increase the half-
as propranolol; cardioselective beta-blockers. may cause systemic effects namely Cushing’s Aerosol Inhalation, (25/125 mcg), Salmeterol 25 mcg, life of aminophylline include propranolol,
Adverse effects: Tremor, paradoxical bron- syndrome, Cushingoid features, adrenal fluticasone 125 mcg. erythromycin, ciprofloxacin and contraceptive
chospasm (discontinue treatment imme- Aerosol Inhalation, (25/250 mcg), Salmeterol 25 mcg,
suppression, growth retardation in children steroids. Drugs which shorten the half-life of
fluticasone 250 mcg.
diately), headache, subjective palpitations, and adolescents, decrease in bone mineral aminophylline are phenytoin, carbamazepine,
Dose: By inhalation, Reversible Obstructive Airways
hypokalaemia. density, cataract and glaucoma. Monitor height barbiturates, rifampicin. Hence, adjustment of
Disease (ROAD), Adults and adolescents 12
Advice to patients: Do not use to treat acute of children on prolonged therapy regularly. years and older, 2 inhalations of 25/50 mcg dose is necessary when any of these drugs is
EMDEX
symptoms; do not exceed the prescribed dose Patients transferring from oral steroid therapy or 25/125 mcg or 25/250 mcg twice daily. co-administered with aminophylline to guide
of salmetrol; do not stop using inhaled or oral to inhaled fluticasone therapy should be Adults 18 years and older: may double dose against toxicity.
cortcosteroids without medical advise even monitored for possibility of impaired adrenal for up to 14 days. Adverse effects: GI irritation, stimulation of the
if you “feel better”; shake well before using. response (withdrawal of systemic therapy Children 4 years and older: 2 inhalations of CNS, visual disorders, hypotension, hyperther-
Avoid spraying in eyes; remove the canister should be gradual). History of diabetes mellitus 25/50 mcg twice daily. mia, convulsions, headache, palpitation, tach-
and rinse the plastic case and cap under warm Children under 4 years: not recommended.
(may increase blood sugar levels). Pregnancy ycardia; collapse and sudden death if injected
Chronic Obstructive Pulmonary Disease
water and dry daily. Store the canister with and lactation rapidly; pain at i.m. injection site.
(COPD), Adult, 2 inhalations of 25/125 mcg
nozzle end down. Interactions: Avoid co-administration with to 25/250 mcg twice daily. Advice to patients: Take oral dose with a full
Nursing actions: Before using, the inhaler ritonavir (may greatly increase fluticasone No dosage adjustement is required in el- glass of water; capsule forms may be opened
must be shaken well. plasma concentrations), and beta blockers. derly, renal or hepatic impairment. and sprinkled on soft foods; notify physician if
• Relieve dry mouth with sips of water or gum. Adverse effects: Paradoxical bronchospasm may nausea, vomiting, severe GI pain, restlessness
POM SERETIDE ACCUHALER® (GSK)
• Not to be used for the relief of acute attacks. occur with an immediate increase in wheezing or irregular heartbeat occurs; do not drink or
Aerosol Inhalation, (50/100 mcg), Salmeterol 50 mcg,
• Monitor lung sounds, pulse, B.P. after dosing; discontinue medication and treat fluticasone 100 mcg. eat large quantities of caffeine-containing bev-
• Do not exceed prescribed dose. Observe for immediately with a fast and short acting inhaled Aerosol Inhalation, (50/250 mcg), Salmeterol 50 mcg, erages or food (colas, coffee, chocolate); do not
wheezing after administration and notify bronchodilator). Salmeterol, a beta-agonist, fluticasone 250 mcg. chew or crush enteric coated or sustained re-
physician if it occurs. may cause tremor, subjective palpitations and Aerosol Inhalation, (50/500 mcg), Salmeterol 50 mcg, lease products; take at regular intervals; notify
• Teach patient how to use metered dose headache; Cardiac arrhythmias (including atrial fluticasone 250 mcg. physician if insomnia, nervousness, irritability,
inhaler. fibrillation, supraventricular tachycardia and Dose: By inhalation, Reversible Obstructive Airways palpitations, seizures occur; do not change
Dose: By inhalation, 50 mcg (2 inhalations) Disease (ROAD), Adults and adolescents 12
extrasystoles); Arthralgia and hypersensitivity brands or doses without consulting physician.
twice daily; increased to 100 mcg years and older, 1 inhalation of 50/100 mcg
reactions including rash, oedema, angioedema, or 50/250 mcg or 50/500 mcg twice daily.
Check with doctor or pharmacist before taking
(4 inhalations) twice daily in more oropharyngeal irritations; Rarely, muscle cramps, other drugs including OTC medications.
Adults 18 years and older: may double dose
severe airways obstruction. hyperglycaemia. Fluticasone propionate, a corti- for up to 14 days. Nursing actions: Administer orally with a
Child: (>4 years): 2 inhalations twice costeroid, may cause hoarsness and candidiasis Children 4 years and older: 1 inhalation of full glass of water after meals to decrease GI
daily. (thrush) of the mouth and throat; Rarely, hyper- 50/100 mcg twice daily. upset, although food may delay absorption; do
Not recommended for child <4 yrs. sensitivity reactions, respiratory symptoms Children <4 years: not recommended. not crush sustained release or enteric coated
(dyspnoea and/or bronchospasm) and very Chronic Obstructive Pulmonary Disease drug products.
POM SEREVENT® (GSK)
rarely, anaphylactic reactions. Possible systemic (COPD), Adult, 1 inhalation of 50/250 mcg • IV dose should be diluted in D5W to prevent
Aerosol inhalation, Salmeterol (as the hydroxynaph-
to 50/500 mcg twice daily.
thoic acid salt) 25 mcg per dose (actuation); in effects include Cushing’s syndrome, Cushingoid the burning effect; use only clear solution;
No dosage adjustement is required in el-
pressurised metered-dose inhaler. Each canister features, adrenal suppression, growth retardation avoid IM inj, may cause pain and tissue
derly, renal or hepatic impairment.
provides 120 actuations. in children and adolescents, decrease in bone damage.
mineral density, cataract and glaucoma; Rarely, AMINOPHYLLINE • Encourage patient to drink adequate fluids to
SALMETEROL plus FLUTICASONE hyperglycaemia, anxiety, sleep disorders and decrease mucous viscosity.
Synonym: Theophylline ethylenediamine.
Indications: Treatment of Reversible Ob- behavioural changes, including hyperactivity and • Advise patient to avoid hazardous activities
Therapeutic category: Bronchodilator.
structive Airways Disease (ROAD) including irritability (predominantly in children). because dizziness may occur.
Pharmacology: Aminophylline relaxes the
asthma in children and adults, where use of Dose: See under the preparations below. Dose: By mouth, 100-300 mg 3 – 4 times
smooth muscle of the bronchial airways and
a combination (bronchodilator and inhaled Counsel patient to rinse mouth after daily after food.
pulmonary blood vessels by inhibitng phos-
corticosteriod) is appropriate namely Patients each use. By slow IV injection (over 20 mins),
296 | 7.1.1 Bronchodilators 7.1.2 Corticosteroids | 297
200-500 mg (5 mg/kg) in 10-20 mL Dose: Adult usually 1 tab. 2-4 times daily; or during the night. Not recommended dose.
of water. ½-1 tab. at bedtime in some patients. for child <12 years of age. POM Ipratropium bromide (EDL 15.1)
Child: 5 mg/kg. Child (over 5 years) and sensitive POM FRANOL® (Sanofi-Aventis) Inhalation, (aerosol), Ipratropium (as bromide) 20
POM Aminophylline (EDL 15.1)
adults, one-half the usual adult dose; Tablet, Ephedrine HCl 11 mg, theophylline 120 mg µg/metered dose.
Injection, Aminophylline 25 mg per mL. 2-5 years, 2-5 mL 3-4 times daily. Pack: 100’s.
Not recommended for children <2
POM ASMADEX® (Orange Drugs)
7.1.2 Corticosteroids
POM Aminophylline (Alpha) years.
Injection, Aminophylline 25 mg per mL; in-10 mL Tablet, Theophylline 150 mg, ephedrine HCI 10 mg Corticosteroids are anti-inflammatory medica-
amp. POM MARAX® (Neimeth) Pack: 2 x 10’s tions that reduce airway hyperresponsiveness,
Tablet, Hydroxyzine HCl 10 mg, ephedrine sulfate 25 Dose: Adult, 1 tablet 2-3 times daily; Child: ¼-1 tablet inhibit inflammatory cell migration and activa-
POM ASTHAMED® (Fil Pharma) mg, theophylline 130 mg, 2-3 times daily depending on age.
Tablet, Aminophylline BP 100 mg; f-c tab. tion, and block late phase reaction to allergen.
Pack: 20, 100.
100 mg – 500’s. POM ASMANOL-F® (Vitabiotics) INHALED CORTICOSTEROIDS
Syrup, Hydroxyzine HCl 2.5 mg, ephedrine sulfate
Injection, Aminophylline 25 mg per mL; in 10-mL Tablet, Ephedrine HCl 16 mg, theophylline 60 mg,
6.25 mg, theophylline 32.5 mg per 5 mL. Inhaled Corticosteriods (ICSs), such as beclo-
amp. chlorphenamine maleate 2 mg
Pack: 100 mL. metasone, are the most consistently effective
Pack: 50’s.
POM BETAPHYLLINE® (Beta Drugs) long-term control medication at all steps of
Injection, Aminophylline 25 mg per mL; in 10-mL EPHEDRINE plus THEOPHYLLINE Theophylline + Salbutamol
care for persistent asthma, and ICSs improve
amp. Therapeutic category: Antiasthmatic, bron- POM RISMANOL-F® (Richygold)
Pack: 10 mL x 50 amps.
asthma control more effectively in both chil-
chodilator Tablet, Theophylline (anhydrous) 100 mg, salbu-ta- dren and adults than leukotriene receptor an-
POM DIPMIN® (Mark). Indications: Suppression and symptomatic mol 2 mg; uncoated tab.
tagonists (LTRAs) or any other single, long-term
Injection, Aminophylline 250 mg per 10 mL treatment of bronchial asthma; bronchos- Pack: 10 x 10’s; 500’s.
Dose: Adult and Child (1-12 years), ½ or 1 tablet 3
control medication do. They are recommended
POM LABOPHYLINE® (Embassy) pasm associated with chronic bronchitis and for the long-term control of asthma in patients
times daily.
EMDEX
Injection, Aminophylline 25 mg per mL. emphysema. using a beta2-adrenoceptor agonist more than
Pack: 50’s. Contra-indications: Hypersensitivity to any of once a week over a 3-month period and some
EPINEPHRINE
the components; porphyria, unstable angina, episodes affect sleep and activity. Regular use
POM MAMIN® (Vixa)
Injection, Aminophylline 25 mg/mL. arrhythmias, severe hypertension, coronary See under section 8.2 of inhaled corticosteroids reduces the risk of
Pack: 10 mL x 50’s. disease, pregnancy. exacerbations of asthma.
Precautions: Renal disease, chest infection, Corticosteroids must be used regularly to
POM SIVOLLINE® (Adpharm) IPRATROPIUM BROMIDE
smoking, phaeochromocytoma, prostate dis- obtain maximum benefit. Symptom control
Injection, Aminophylline 250 mg per 10 mL.
ease, diabetes, cardiac or liver disease, peptic Indications: Chronic asthma; chronic obstruc-
Pack: 1 x 50’s. tive pulmonary disease. is usually effective after 3–7 days treatment.
ulcer, agitation, hyperthyroidism, glaucoma, Long-term high-dose regimens of inhaled
elderly or lactation. Precautions: Prostatic hypertrophy; glau-
EPHEDRINE plus HYDROXYZINE coma (standard doses unlikely to be harmful; corticosteroids are preferred for the treatment
plus THEOPHYLLINE Interactions: Cimetidine, erythromycin, of severe persistent asthma because they
ciprofloxacin, oral contraceptives, tricyclics, reported with nebulized drug, particularly in
Therapeutic category: Antiasthmatic reduce the need for the long-term use of oral
sympathomimetics; anticonvulsants; diltiazem, association with nebulized salbutamol; care
Pharmacology: As a vasoconstrictor, ephed- corticosteroids and also have fewer systemic
verapamil, digoxin; rifampicin; sulphinpyra- needed to protect patient’s eyes from drug
rine relieves congestion occuring in bronchial adverse effects.
zone; diuretics; corticosteroids; guanethidine powder or nebulized drug); medical super-
asthma. It is a bronchodilator. Theophylline is Local adverse effects from inhaled corticoster-
or methyldopa; interferons; MAOIs. vision necessary for first dose of nebulized
a bronchospasmolytic. Hydroxyzine modifies oids include oropharyngeal candidosis, dys-
Adverse effects: Palpitations and changes in solution (risk of paradoxical bronchospasm).
the central stimulatory action of ephedrine phonia, and occasional coughing from upper
the heart beat, flushing, giddiness, headache, Adverse effects: Occasionally, dry mouth;
preventing excessive excitation. airway irritation. The use of spacing devices
tremor, anxiety, restlessness, muscle weakness, rarely, urinary retention, constipation; tachy-
Indications: Prophylactic and sympto- reduces oropharyngeal deposition and thus
nausea, vomiting, indigestion, increased thirst, cardia and atrial fibrillation reported.
matic treatment of bronchial asthma and of reduces the incidence of candidosis; rinsing
sweating and problem passing water. Dose: Chronic asthma or chronic obstructive
bronchospasm associated with respiratory the mouth with water or brushing teeth after
Advice to patients: To be taken with a full pulmonary disease, by aerosol inha-
disorders. using an inhaled corticosteroid may also be
glass of water; notify physician if nausea, lation, ADULT 20–40 µg, 3–4 times
Contra-indications: CVS disease, hyperthy- helpful. Coughing may be reduced by the use
vomiting, seizures, insomnia, irritability, severe daily; CHILD up to 6 years, 20 µg 3
roidism, hypertension; hypersensitivity to the of a beta2-agonist before using a corticosteroid
GI pain, restlessness, or irregular heart beat times daily, 6–12 years, 20–40 µg 3
drug, early pregnancy. inhaler. The risk for systemic effects of inhaled
occurs; do not drink or eat large quantities of times daily.
Precautions: Elderly males; prostatic hyper- corticosteroids is small and is dependent upon
caffeine-containing beverages or food (colas, Chronic obstructive pulmonary disease,
trophy; road users. the dose and potency of the corticosteroid,
coffee, chocolate); take at regular intervals. Do by inhalation of nebulized solution,
Interactions: CNS depressants, alcohol. as well as its bioavailability and the plasma
not take within 2 hours of bedtime to avoid ADULT 250–500 µg 3–4 times daily.
Adverse effects: Palpitation; gastric irritation half-life of its systemically absorbed fraction.
insomnia. Adjunct in acute bronchospasm, by in-
due to theophylline esp. when given on an Systemic effects are rare and include skin thin-
Nursing actions: Encourage patient to drink halation of nebulized solution, ADULT
empty stomach; insomnia, dryness of throat ning and easy bruising, a small increased risk of
adequate fluids (2 litres per day) to decrease 500 µg repeated as required; CHILD
and nose; headache, sweating. glaucoma and cataracts, adrenal suppression,
mucous viscosity. up to 6 years 125–250 µg, maximum
Advice to patients: May cause drowsiness; do decrease of bone metabolism and growth
• Advise patient to avoid hazardous activities 1 mg daily, 6–12 years 250 µg, maxi-
not drive or operate machinery. May also cause retardation in children (see also section 10.3).
if dizziness occurs. mum 1 mg daily.
wakefulness or nervousness; do not take within See Table 2 above for the Estimated Equipotent Daily
2 hours of bedtime to avoid insomnia. Avoid Dose: 1 tablet 3 times daily plus 1 tab at POM Ipratropium bromide (WMF 25.1)
Doses for Inhaled Corticosteroids for Adults and
alcoholic beverages. bedtime for patients who get attacks Inhalation, (aerosol), Ipratropium 20 µg/metered
298 | 7.1.2 Corticosteroids 7.1.2 Corticosteroids | 299
Children ≥12 years. requirements are reduced to a minimum. Oral following measures are recommended: wash in warm water and dry thoroughly; rinse
doses should be given as a single dose in the • Advise patients to use spacers with nonbreath-ac- mouth and throat after use to prevent Candida
SYSTEMIC CORTICOSTEROIDS morning to reduce the disturbance to the tivated metered-dose inhalers (MDIs) to reduce infection; report sore throat or mouth lesions
Oral corticosteroids (sections 8.3 and 10.3) circadian cortisol secretion. Dosage should local side effects. to physician.
• Advise patients to rinse the mouth (rinse and spit)
may be used as “maximum therapy” to achieve always be adjusted to the lowest dose which Nursing actions: Administer by inhalation;
after inhalation.
control of a patient’s asthma. This may be useful controls symptoms. • Use the lowest dose of ICS that maintains asthma
instruct patient to wait for one minute before
either when initiating long-term therapy for Safety Issues for ICS and LABA control. taking subsequent puffs where necessary and
a patient with uncontrolled asthma or as a • Consider adding a LABA, or alternative adjunctive to hold his breath after inhalation to enhance
short “rescue” course at any stage for acute ICSs are the preferred long-term control ther- action of drug.
therapy, to a low or medium dose of ICS rather
exacerbation. apy in children of all ages and adults. Most than using a higher dose of ICS to maintain • Check mucous membranes for signs of
Long-term oral corticosteroid therapy may be benefits in mild or moderate asthma occur at asthma control. fungal infection; advise patient to gargle/
required to control severe persistent asthma, the low–to medium-dose ranges. Higher doses Daily use of LABA generally should not exceed rinse mouth after use to prevent oral fungal
but its use is limited by the risk of significant may further reduce the risk of exacerbations 100 mcg Salmeterol or 24 mcg Formoterol. infection..
adverse effects. but the risk of adverse effects increases with LABA not recommended for treatment of acute • Relieve dry mouth with sips of water or gum.
In these cases, high-dose inhaled corticos- the dose. symptoms or exacerbations and should not be • Teach patient proper inhalation techniques.
teroids should be continued so that oral To reduce the potential for adverse effects, the used as monotherapy for longterm control. Dose: Chronic asthma, by aerosol inhalation
Instruct patient not to stop ICS therapy while (standard dose inhaler), ADULT 200
Table-2: ESTIMATED COMPARATIVE DAILY DOSAGES FOR INHALED CORTICOSTEROIDS FOR YOUTHS ≥12
YEARS OF AGE AND ADULTS
taking LABA. µg twice daily or 100 µg 3–4 times
daily (in more severe cases, initially
Low Daily Dose Medium Daily Dose High Daily Dose BECLOMETASONE
Drug
Adult Adult Adult
600–800 µg daily); CHILD 50–100 µg
Synonym: Beclomethasone. 2–4 times daily or 100–200 µg twice
EMDEX
Beclomethasone HFA
40 or 80 mcg/puff 80–240 mcg >240–480 mcg >480 mcg
Therapeutic category: Corticosteroid; Anti-in- daily.
flammatory Agent. Chronic asthma, by aerosol inhalation
Budesonide DPI
90, 180, or 200 mcg/inhalation 180–600 mcg >600–1,200 mcg >1,200 mcg
Indications: Chronic asthma not controlled (high dose inhaler), ADULT 500 µg
by short-acting beta2-adrenoceptor agonists. twice daily or 250 µg 4 times daily; if
Flunisolide
250 mcg/puff 500–1,000 mcg >1,000–2,000 mcg >2,000 mcg
Precautions: see notes above; active or qui- necessary may be increased to 500
escent tuberculosis; systemic therapy may µg 4 times daily; CHILD not recom-
Flunisolide HFA
80 mcg/puff 320 mcg >320–640 mcg >640 mcg
be required during periods of stress or when mended.
airway obstruction or mucus prevent drug See also under the preparations below.
Fluticasone
HFA/MDI: 44, 110, or 220 mcg/puff 88–264 mcg >264–440 mcg >440 mcg
access to smaller airways; not for relief of acute POM Beclometasone (WMF 25.1)
DPI: 50, 100, or 250 mcg/inhalation 100–300 mcg >300–500 mcg >500 mcg symptoms; monitor height of children receiv- Inhalation (aerosol), Beclometasone dipropionate 50
Mometasone DPI
ing prolonged treatment—if growth slowed, µg/dose; 250 µg/dose.
200 mcg/inhalation 200 mcg 400 mcg >400 mcg review therapy; interactions: Appendix 1.
POM Beclometasone (EDL 26.1)
Adverse effects: Oropharyngeal candidosis,
Triamcinolone acetonide Aerosol Inhalation, Beclomethasone (as dipro-pion-
75 mcg/puff 300–750 mcg >750–1,500 mcg >1,500 mcg cough and dysphonia (usually only with high ate) 50 mcg, 250 mcg per metered dose.
doses); adrenal suppression, growth retar-
Key: DPI, dry powder inhaler; HFA, hydrofluoroalkane; MDI, metered-dose inhaler POM BECOTIDE 50® (GSK)
Notes: dation in children and adolescents, impaired
bone metabolism, glaucoma and cataract Aerosol Inhalation, Beclometasone dipropionate 50
• The most important determinant of appropriate dosing is the clinician’s judgment of the patient’s response to therapy. The
clinician must monitor the patient’s response on several clinical parameters and adjust the dose accordingly. The stepwise mcg per dose; metered-dose aerosol.
(with high doses, but less frequent than with
approach to therapy emphasizes that once control of asthma is achieved, the dose of medication should be carefully titrated Dose: Adult, 4 inhalations (200 mcg) twice a day or
to the minimum dose required to maintain control, thus reducing the potential for adverse effect.
systemic corticosteroids); paradoxical bron- 2 inhalations (100 mcg) 3-4 times daily; in
• Some doses may be outside package labeling, especially in the high-dose range. cho-spasm—requires discontinuation and more severe cases, initially 600-800 mcg per
• MDI dosages are expressed as the actuator dose (the amount of the drug leaving the actuator and delivered to the patient), alternative therapy (if mild, may be prevented day reducing according to response.
which is the labeling required in the United States. This is different from the dosage expressed as the valve dose (the amount
by inhalation of beta2-adrenoceptor agonist Child, 1-2 inhalations (50-100 mcg) 2-4
of drug leaving the valve, not all of which is available to the patient), which is used in many European countries and in some
scientific literature. DPI doses are expressed as the amount of drug in the inhaler following activation. or by transfer from aerosol to powder inhala- times daily, according to the response.
• Comparative dosages are based on published comparative clinical trials (Adams et al. 2005; Barnes et al. 1998; Kelly 1998; tion); rarely, urticaria, rash, angioedema; very
Lasserson et al. 2005; Pedersen and O’Byrne 1997). The rationale for some key comparisons is summarized as follows: rarely, anxiety, sleep disorders and behavioural BUDESONIDE
— The high dose is the dose that appears likely to be the threshold beyond which significant hypothalamic-pituitary– drenal
changes. Indications: Bronchial asthma requiring
(HPA) axis suppression is produced, and, by extrapolation, the risk is increased for other clinically significant systemic
effects if used for prolonged periods of time (Martin et al. 2002; Szefler et al. 2002). CANDIDOSIS: Candidosis can be reduced by maintenance treatment with glucocorticoids
— The low– and medium-doses reflect findings from dose-ranging studies in which incremental efficacy within the low– to use of a spacing device (see notes above); for control of the underlying airways inflam-
medium-dose ranges was established without increased systemic effect as measured by overnight cortisol excretion. The rinsing the mouth with water after inhalation mation.
studies demonstrated a relatively flat dose-response curve for efficacy at the medium-dose range; that is, increasing the
may help to prevent candidosis. Contra-indications: Hypersensitivity to
dose of high-dose range did not significantly increase efficacy but did increase systemic effect (Adams et al. 2001; Martin budesonide.
et al. 2002; Szefler et al. 2002). Advice to patients: Shake thoroughly before
— The dose for budesonide and fluticasone MDI or DPI are based on recently available comparative data. These new using; inhaled beclo-methasone makes many Adverse effects: Mild irritation in the throat,
data, including meta-analyses, show that fluticasone requires one-half the microgram dose of budesonide DPI to achieve asthmatics cough, to reduce chance, inhale coughing, and hoarseness, candida infection in
comparable efficacy (Adams et al. 2005; Barnes et al. 1998; Nielsen and Dahl 2000). drug slowly or use prescribed inhaled bron- the oropharynx, contact dermatitis, urticaria.
chodilator 5 minutes before beclomethasone Nursing actions: Teach patient how to use
Source: National Heart, Blood and Lung Institute. Guidelines for diagnosis and management of asthma. US
National Institute of Health, 2007. Available from: http://www.nhlbi.nih.gov/guidelines/asthma/asthgdln.pdf is used; keep inhaler clean and unobstructed, Turbuhaler.
• Monitor patient for bronchospasm; stop med-
300 | 7.1.3 Prophylactic drugs 7.1.3 Prophylactic drugs | 301
ication and give a bronchodilator. adjunctive therapy with ICSs, but for youths 12 5 mL. Adverse effects: Headache; abdominal pain;
• Corticosteroids may mask symptoms of viral years of age and adults, they are not preferred upper respiratory infection; GI disturbances
infection; monitor patient closely. adjunctive therapy compared to the addition MONTELUKAST namely diarrhoea, nausea, vomiting; fever,
• Discontinue medication if IOP increases. of LABAs. Therapeutic category: Leukotriene receptor rash; dizziness, drowsiness. Rarely hypersen-
Dose: The dose is individual and should be Very rarely Churg-Strauss syndrome has antagonist. sitivity reactions including anaphylaxis; in-
adjusted to the smallest dose main- occurred in association with the use of leukot- Pharmacology: Montelukast sodium is a com- creased bleeding tendency; abnormal dreams;
taining symptom control. riene receptor antagonists; this reaction has petitive, selective and orally active leukotriene fatigue, malaise, oedema; arthralgia, myalgia
Adult: The usual dosage range is 200- often followed the reduction or withdrawal D4 (cysteinyl leukotriene CysL T1) receptor including muscle cramps; tremor, dry mouth;
800 mcg daily divided into 2-4 admin- of oral corticosteroid therapy. Prescribers and antagonist. The cysteinyl leukotrienes (LTC4, Churg-Strauss syndrome.
istrations. In severe cases, doses up to patients should be alert to the development LTD4, LTE4) are products of arachidonic acid Dose: By mouth, Adult and children (≥15
1600 mcg may be required. At daily of eosinophilia, vasculitic rash, worsening metabolism and are released from various years of age), Asthma or seasonal
doses up to 400mcg the whole dose pulmonary symptoms, cardiac complications, cells, including mast cells and eosinophils. allergic rhinitis, 10 mg tablet once
may be given at one occasion. or peripheral neuropathy. These eicosanoids bind to cysteinyl leukotriene daily, to be taken in the evening; 6 to
Child (3-7 years): 100-400 mcg either MAST CELL STABILISERS (CysL T) receptors and the resultant effects 14 years of age, 5 mg chewable tablet
once daily or divided in 2-4 adminis- correlate with the pathophysiology of asthma, daily; 2 to 5 years of age, 4 mg chew-
trations; 7 years and above: 100-800 Sodium cromoglycate and Ketotifen are not including airway edema, bronchoconstriction, able tablet or one sachet of pediatric
mcg daily divided into 2-4 adminis- bronchodilators but prevent broncho-con- and altered cellular activity associated with the granules (4 mg) daily.
trations. Daily dose of up to 400 mcg striction in patients with extrinsic or allergic inflammatory process. Montelukast has been Children (6 months to 2 years of age),
may be given at one occasion. asthma. They stabilise sensitised mast cells shown to inhibit bronchoconstriction due to Asthma, One sachet of pediatric
and inhibit the release of bronchoconstrictor inhaled LTD4 at doses as low as 5 mg; it has no granules (4 mg) daily, to be taken in
POM BUDECORT® (Vitahealth) agents including histamine, serotonin and
Inhalers, Budesonide 100 mcg, 200 mcg; suspended agonist activity. Bronchodilation was observed the evening.
EMDEX
slow-reacting substance. within 2 hours of oral administration. The No dosage adjustment required for
in propellant HFA-134a.
Mast cell stabilisers are useful in extrinsic bronchodilation effect caused by a β-agonist the elderly as well as in renal or mild
Pack: 200 metered doses (in canisters)
(allergic) asthma, particularly in children and was additive to that caused by montelukast. to moderate hepatic impairment.
POM PULMICORT® (Reals) young adults and can prevent exercise-in- Montelukast is rapidly absorbed following oral Administration: To be taken with or without food.
Turbohalers, Budesonide 100 mcg, 200 mcg, 400 mcg duced asthma.Intrinsic asthma and chronic administration, with mean oral bioavailability Advise patient to take once daily regularly, whether
per dose; dry powder inhaler.
obstructive airways disease are not indications of 64%. Plasma protein binding is >99%. Ex- symptoms are controlled or worsening. For asthma,
for these drugs. tensively metabolised in the liver via mainly
the dose should be taken in the evening. For sea-
HYDROCORTISONE sonal allergic rhinitis, the time of administration may
CYP2C8 and to a lesser extent by CYP 3A4 & be individualized to suit patient needs. Patients with
See under section 10.3 KETOTIFEN
2C9. Excretion is mainly via the bile. both asthma and seasonal allergic rhinitis should
Therapeutic category: Anti-asthmatic/Anti- Indications: Indicated in adults and pediatric take only one tablet or sachet daily in the evening.
7.1.3 Prophylactic drugs histamine. patients 6 months of age and older for the (Additional information sourced from Singulair monograph
Indications: Long-term prevention of bron- prophylaxis and chronic treatment of asthma available from: http://www.medicines.org.uk/)
Sodium cromoglicate chial asthma, allergic bronchitis, asthmatic including Prevention of day and night time
Sodium cromoglicate [not included on the symptoms associated with hay fever. symptoms; Treatment of aspirin-sensitive asth- POM MONTIGET® (Getz)
15th WHO Model List] may be helpful in asthma Precautions: Withdraw anti-asthmatic drugs matic patients; Prevention of exercise-induced Tablet, Montelukast (as sodium salt) 10 mg; f-c tab.
with an allergic basis, but it is difficult to predict already in use gradually; co-administration bronchoconstriction. Also in adults and pedi- 10 mg – 14’s (in blisters).
who might benefit. In adults, prophylaxis with with oral anti-diabetic agents; pregnancy, atric patients 2 years of age and older, for the Chewable tablets, Montelukast (as sodium salt) 4
sodium cromoglicate is generally less effective breast-feeding. mg, 5 mg
relief of symptoms of seasonal allergic rhinitis.
than prophylaxis with inhaled corticosteroids. Interactions: Sedatives, hypnotics, antihista- 4 mg – 14’s (in blisters)
Contra-indications: Hypersensitivity to the 5 mg – 14’s (in blisters)
Sodium cromoglicate is of value in the pre- mines, alcohol. drug or any of its components. Avoid use in Paediatric granules, Montelukast (as sodium salt)
vention of exercise-induced asthma, a single Adverse effects: Sedation, dry mouth, slight acute asthma attacks including status asth- 4 mg.
dose being inhaled 30 minutes beforehand; dizziness, weight gain. maticus. 4 mg – 14’s (in sachets)
however, exercise-induced asthma may indi- Nursing actions: May cause drowsiness; warn Precautions: Avoid abrupt substitution for
cate poor disease control and should prompt patient to avoid hazardous tasks requiring inhaled or oral corticosteroids (if indicated, SODIUM CROMOGLICATE
assessment of the patient. mental alertness or physical coordination. the dose of inhaled corticosteroid may be Synonym: Sodium cromoglycate
Sodium cromoglicate is of no value for the Dose: By mouth, Adult, 2 mg 1-2 times daily; reduced gradually). Does not block bronchoc- Therapeutic category: Anti-allergic/anti-
treatment of acute attacks of asthma. max. 4 mg daily in 2 divided doses if onstrictor response to aspirin or other NSAIDs asthmatic
LEUKOTRIENE RECEPTOR ANTAGONISTS necessary. in aspirin-sensitive asthmatic patients. Not Indications: Prophylaxis of asthma; prevention
Child (6 months – 3 years), 0.5 mg recommended as monotherapy for exercise-in-
The leukotriene receptor antagonists [not of exercise-induced asthma.
twice daily; >3 years, 2 mg 1-2 times duced asthma. Rare cases of Churg-Strauss
included on the 15th WHO Model List], Precautions: Pregnancy (appropriate to use;
daily. syndrome; monitor for eosinophilia, vasculitic
including montelukast, pranlukast, and see notes above and Appendix 2); breastfeed-
zafirlukast, block the effects of cysteinyl leu- POM ZADITEN® (Novartis) rash, worsening pulmonary symptoms, cardiac ing (Appendix 3).
kotrienes in the airways. LTRAs are alternative, Capsule, Ketotifen (as hydrogen fumarate) 1mg; complications, and/or neuropathy. Pregnancy, Adverse effects: Coughing, transient bron-
white cap. marked ‘CS’. breastfeeding. chospasm.
but not preferred, therapy for the treatment Tablet, Ketotifen (as hydrogen fumarate) 1 mg; white
of patients who require step 2 care (for mild Interactions: Hepatic enzyme inducers such Advice to patients: Do not discontinue
scored tab. Coded ‘ZADITEN 1’. as phenytoin, phenobarbital or rifampicin
persistent asthma). LTRAs also can be used as Elixir, Ketotifen (as hydrogen fumarate) 1 mg per
abruptly; not effective for acute relief of symp-
(monitor for decreased anti-asthmatic effect).
302 | 7.2 Expectorants and cough suppressants Compound Cough Preparations | 303
toms; must be taken on regularly scheduled 7.2 Expectorants and cough Dose: Adult, 5-10 mL 3 times daily. OTC RHINATHIOL® Promethazine (Sanofi-Aventis)
basis. suppressants Child (6-12 years): 5 mL 3-4 times Syrup, Carbocisteine 100 mg, promethazine HCl 2.5
Nursing actions: Advise patient to clear as daily; 2-6 years, 2.5 mL 3-4 times a mg per 5 mL.
much mucous as possible before inhalation BROMHEXINE day. Pack: 125 mL
Indications: Unproductive and irritative coughs in
treatments. POM DILABRON® (Vitahealth)
See under preparations below. adults and children aged over 2 years.
• Teach patient proper inhalation technique Expectorant, Bromhexine 4.0 mg, guaiphenesin 50.0 Precaution: May impair ability to drive or operate
(see Aerosol Instructions in section 7.1.1). OTC BROMEX® (Reals) mg, menthol 0.5 mg, terbutaline 1.25 mg. machinery.
• Relieve irritating throat with sips of water Elixir, Bromhexine HCl 4 mg per 5 mL. Pack: 100 mL Dose: Adult, 45-60 mL daily. Child (12-15 years):
or gargle. Pack: 100 mL. 30-45 mL daily; 2.5-12 years, 20-30 mL
POM MUCODIL® (Medreich)
Dose: Prophylaxis of asthma and exercise-in- Indications: Conditions associated with congestion Syrup, Terbutaline (as sulfate) 2.5 mg, bromhexine (as
daily; 2-2.5 years, 15-20 mL daily; <2 years,
duced asthma, by aerosol inhalation, of the bronchi such as emphysema with bronchitis, not recommended. To be taken with food.
HCl) 8 mg, guaifenesin 100 mg per 5 mL.
ADULT and CHILD 10 mg 4 times chronic inflammatory pulmonary conditions, bron- Pack: 100 mL.
daily, increased in severe cases or chiectasis, and bronchospasm, asthma. DEXTROMETHORPHAN
Dose: Infant, 1.25 mL; Child (<5 years), 2.5 mL; 5-10
during periods of risk to 6–8 times BROMHEXINE plus GUAIFENESIN OTC Dextromethorphan (EDL 15.2)
years, 5 mL. plus SALBUTAMOL
daily; additional doses may be taken Adult & Child (>10 years), 10-20 mL Oral liquid, Dextromethorphan (as HBr) 15 mg
before exercise; when stabilized, may May repeat above dosages 3 times a day. POM AIRMAX® (Zeenat) per 5 mL
be possible to reduce to maintenance Tablet, Salbutamol sulphate 2 mg, Guaiphenesin
of 5 mg 4 times daily. OTC VISOLVON® (Vixa) GUAIFENESIN
100 mg, Bromhexine HCl 4 mg; white round tabs.
Tablet, Bromohexine HCl 8 mg
Pack: 10 x 10’s (in blister) Pharmacology: Guaiphenesin has an expec-
8 mg – 10 x 10’s
ZAFIRLUKAST Syrup, Salbutamol 1 mg, Guaiphenesin 50 mg, Bro- torant action which increases the output of
Therapeutic category: Leukotriene receptor OTC BRONCHOLYTE® (NGC) mhexine 2 mg per 5 mL.
respiratory tract fluid by reducing adhesiveness
EMDEX
Elixir, Bromhexine HCl 4 mg per 5 mL Pack: 100 mL (in brown amber plastic bottle)
antagonist (LTRA). and surface tension. It reduces the viscosity of
Pack: 100 mL
Indications: Prophylaxis of asthma. POM ASCOREX®(Glenmark) tenacious sputum. The increased flow of less
Contra-indications: Hypersensitivity to the Liquid, Salbutamol (as sulfate) 1 mg, Bromhexine HCl viscid secretions promotes ciliary action and
BROMHEXINE plus TERBUTALINE 2mg, Guaifenesin 50 mg, Menthol 0.5 mg per 5 mL.
drug; history of moderate or severe renal plus GUAIFENESIN facilitates the removal of mucus. Guaiphenesin
Pack: 100 mL
impairment; hepatic impairment or cirrhosis; Pharmacology: Terbutaline sulfate is a di- is readily absorbed from the GI tract. It is me-
Indications: For the symptomatic relief in the
children under 12 years of age; breast-feeding. rect-acting sympathomimetic agent which treatment of productive cough associated with tabolised and excreted in the urine.
Precautions: Elderly, pregnancy, renal impair- selectively stimulates B0 receptors producing bronchospasm in various respiratory disorders like Indications: As an expectorant for the symp-
ment, labile or unstable asthma. bronchodilation. Bromhexine is a mucolytic pneumonia COPD, bronchial asthma, emphysema, tomatic relief of cough due to colds and minor
Interactions: Warfarin (monitor prothrombin and mucokinetic. It reduces sputum viscosity acute & chronic bronchitis, etc. upper respiratory infections.
time closely). Theophylline, erythromycin and by breaking down the tenacious network Dose: Adult & Children (>12 years), 10 mL 3 times Contra-indications: Hypersensitivity to
terfenadine may cause decreased plasma lev- of mucopolysaccharides fibres abundant daily. guaiphenesin and bisulphites.
els of zafirlukast. Aspirin may cause increased Children (6-12 years): 5 mL 3 times daily; 2-5 Precautions: Acute porphyria. Dosage for
in mucoid sputum. It also facilitates ciliary
plasma level of zafirlukast. years, 2.5 mL 3 times daily.
clearance of the sputum. Guaifenesin is an children under 2 years must be individualized.
Not recommended for children <2 years.
Adverse effects: Headache; GI disturbances expectorant, which acts by enhancing the Adverse effects: GI discomfort, nausea, vom-
including nausea, vomiting, diarrhoea, abdom- output of respiratory tract fluid. By increasing POM NECTALLIN® (Nectar Healthcare) itting. Rarely, diarrhoea, drowsiness, stomach
inal pain; hypersensitivity reactions including Syrup, Bromhexine (as HCl) 2 mg, Salbutamol (as pain.
the volume of secretions in the respiratory
urticaria and angioedema; rashes including Sulphate) 1 mg, Guaiphenesin 50 mg, Menthol 0.5 Dose: By mouth, Adult, 10-20 mL every 4
tract, it facilitates sputum removal by ciliary mg per 5 mL; flavoured syrup base.
blistering.. action and coughing. hours; not to exceed 120 mL a day.
Pack: 100 mL
Nursing actions: Give before meals for best Indications: Symptomatic treatment of CHILD (2-6 years), 2.5-5 mL every 4
Indications: For symptomatic management of all
absorption. Advise patient to take with a cough associated with expectoration and/ productive cough including asthmatic cough. hours; not to exceed 30 mL a day;
full glass of water to reduce GI upset; food or bronchospasm e.g. cough associated with Dose: Adult, 2 teaspoonfuls (10 mL) 6-12 years, 5-10 mL every 4 hours; not
reduces bioavailability and should be avoided respiratory infections, bronchitis and pulmo- Children (2-6 years.): 1 teaspoonful (5 mL); to exceed 60 mL a day.
if possible. nary congestion. >6 years, 1-2 teaspoonfuls (5-10 mL) Note: To help loosen mucus in the lungs, patients
• Advise patient to avoid hazardous activities Contra-indications: Hypersensitivity to sym- should drink a glass of water after each dose.
if dizziness occurs. pathomimetic amines; thyrotoxicosis, cardiac CARBOCISTEINE OTC FENACOL ®(Hovid)
• Zafirlukast is not recommended during lac- patients with arrhythmia, first trimester of Syrup, Guaiphenesin 100 mg per 5 mL; dark brown
See under preparations below.
tation and in acute asthma. pregnancy, hepatic damage, peptic ulcer and liquid with peppermint flavour.
Dose: By mouth, Adult and Child >12 years, patients with bleeding problems. OTC RHINATHIOL® (Sanofi-Aventis) Pack:120 mL; 240 mL.
20 mg twice daily. Precautions: Cardiovascular disease; uncon- Syrup, Carbocisteine 250 mg per 5 mL.
Child <12 years: not recommended. trolled diabetes mellitus. Pack: 125 mL. Compound Cough Preparations
Note: Higher doses are not recommended. As Adverse effects: Terbutaline use may be asso- Indications: Bronchial congestion especially during Advice to patients: Some of the preparations
food may reduce the bioavailability, administer acute episodes of bronchitis. contain ingredients that may cause drowsiness;
ciated with tremor, irritability, headache and
without meals. Dose: Adult, 15 mL 3 times daily. avoid alcoholic beverages.
dizziness particular in the elderly; guaifenesin Syrup, (Infant), Carbocisteine 100 mg per 5 mL.
POM ACCOLATE® (Reals) may cause nausea and vomiting; bromhexine OTC AFIDIL® (Ranbaxy)
Pack: 125 mL.
Tablet, Zafirlukast 20 mg. may cause epigastric discomfort and more Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine
Dose: Child (>5 years): 5 mL 3 times daily; 2-5 years,
rarely nausea. 5 mL 2 times daily. HCl 30 mg per 5 mL.
304 | Compound Cough Preparations Compound Cough Preparations | 305
Pack: 100 mL. guaifenesin 50 mg, racementhol 1 mg per 5 mL. Tablet, Extract glycrrh. 49.95 mcg,menthol 5.99 mcg, OTC DIPHENKOF® (Leady)
Dose: 12 years and above, 10 mL 3 times daily; 6-12 Indications: Cough expectorant. tincture of capsicum 0.011 mL, oil pini pumil 0.001 Expectorant, (Adult), Diphenhyramine HCI 12.5 mg,
years, 7.5 mL 3 times daily. mL, eucalyptus oil 0.02 mL, creosote 0.002 mL, anise ammonium chloride 130 mg, sodium citrate 57 mg,
OTC CADIPHEN® (Interpharma)
oil 0.001 mL, mentholated peppermint oil 0.001 menthol 1.1 mg per 5 mL.
OTC AGISEPT® (Phillips) Syrup, Chlorpheniramine maleate 2 mg, Guaifenesin
mL per tablet; mottled brown flat/plain tab. with Pack: 100 mL; 2 L
Lozenge, 2,4-dichlorobenzyl alcohol 1.2 mg, amyl- (Glyceryl guaiacolate) 80 mg, Ammonium chloride
menthol taste Syrup, (Children), Diphenhyramine HCI 7.0 mg,
metacresol 0.6 mg; in sugar base. 100 mg, Sodium citrate 44 mg, Levo-menthol 0.8
Pack: 20. sodium citrate 28.5 mg
Pack: 4 x 6’s mg, Terpin hydrate 4 mg, Tolu balsam 6 mg, Vasaka
Dose: Adult and child over 10 years, 1-2 tabs to be Pack: 100 mL; 2 L
Indications: Antiseptic lozenges for the relief of syrup 0.133 mL per 5 mL.
sucked 4 or more times a day or as required.
cough and treatment of minor throat and mouth Pack: 100 mL. OTC D-KOFF® (Jawa)
infections. Dose: Adults: 10 mL 3-4 times a day. OTC COLDEX® (Al-Tinez) Syrup, Diphenhydramine HCl, bromhexine HCl, am-
Dose: Dissolve one lozenge slowly in the mouth Child: 2.5-5 mL 3-4 times a day based on Tablet, Acetaminophen 500 mg, dextromethorphan monium chloride, sodium citrate, menthol.
every 2-3 hours. age. HBr 15 mg, loratadine 5 mg; f-c tab Pack: 100 mL x 20’s.
OTC AVROCOF® (Avro) OTC CEENELYN® (Ceenek) OTC DIOGOLYN® (Gauze)
Indications: For treatment of influenza symptoms
Syrup, Diphenhydramine HCl 14.0 mg, ammonium Syrup (Expectorant), Diphenhydramin HCl 14 mg, Oral liquid, Chlorpheniramine maleate 2.0 mg,
such as cough, fever, headache, muscular pain,
chloride 135.0 mg, sodium citrate 57.0 mg, menthol ammonium chloride 135 mg, sodium citrate 57 mg, ephedrine HCI 6.0 mg, sodium citrate 40 mg, am-
bone and joint pain, nasal congestion, runny nose
1.1 mg per 5 mL. menthol 1.1 mg. monium chloride 80 mg, menthol 2.0 mg per 5 mL.
and allergic rhinitis.
Pack: 100 mL. Pack: 100 mL. Pack: 100 mL; 2 L
Dose: Adult and children over 12 years old: 1 caplet
Paediatric syrup, Diphenhydramine HCl 7 mg, men- Dose: Adult, 10 mL every 3-4 hours.
with time OTC Dr. Meyer’s Coflin® Expectorant (Vitabiotics)
thol 0.55 mg per 5 mL. Child (1-5 years): 2.5 mL every 3-4 hours;
Children 6-12 years: ½ caplet each time Expectorant, Diphenhydramine HCI 14 mg, am-
Pack: 100 mL. 6-12 years, 5 mL every 3-4 hours.
monium chloride 135 mg, sodium citrate 57 mg,
OTC CORILYN-P® (Phillips)
OTC AVROLIN® (Avro) OTC CHERICOF® (Ranbaxy) menthol 1.1 mg per 5 mL.
Syrup, Diphendramine HCl 14.08 mg, ammonium
Syrup, (Expectorant), Ammonium chloride 30.0 mg, Syrup, Chlorpheniramine 2 mg, dextromethorphan Pack: 100 mL.
EMDEX
chloride 139 mg, sodium citrate 57.03 mg, racemen-
Ipecacuanha liquid extract BPC 10.0 µL, Liquorice 10 mg, phenylpropanolamine 12.5 mg per 5 mL.
thol 1.5 mg per 5 mL. OTC Dr. Meyer’s Coflin® Linctus (Vitabiotics)
extract B.P.C 50.0 mg, Peppermint oil 6.9 µL, Aniseed Pack: 100 mL
Linctus, Chlorpheniramine maleate 2 mg, menthol
oil 2.6 µL per 5 mL. Dose: Adult, 10 mL 3-4 times daily. OTC COSCOPIN® (Apple)
6 mg, ephedrine HCI 5 mL, ammonium chloride 80
Pack: 100 mL. Child (2-6 years), 2.5 mL 3-4 times daily; 6-12 Linctus, Noscapine 7.0 mg, Ammonium chloride
mg, sodium citrate 40 mg
years, 5 mL 3-4 times daily. 28 mg, Sodium citrate 3.25 mg, Chlorphenamine
OTC BENYLIN® (NGC) Pack: 100 mL
maleate 2 mg per 5 mL.
Expectorant, Diphenhydramine HCl 14.0 mg, ammo- OTC CODEPECT® (Megalife sciences)
Pack: 100 mL. OTC Dr. Meyer’s Coflin® with Codeine (Vitabiotics)
nium chloride 135 mg per 5 mL. Capsule, Codeine (as phosphate) 10 mg, glyceryl
Pharmacology: Coscopin contains Noscapine, an Syrup, Diphenhydramine HCI 13.50 mg, codeine
Pack: 100 mL guacolate 100 mg; red, oval-shaped softgel cap.
alkaloid, which acts centrally to suppress contin- phosphate 10.95 mg, sodium citrate 54.40 mg,
Pack: 10 x 10’s (in blister).
OTC BENYLIN® with Codeine (NGC) uous and irritating cough. Noscapine is a potent menthol 1.10 mg per 5 mL.
Linctus, Diphenhydramine HCl 13.5 mg, codeine OTC COFEX® (SKG) and long-lasting (upto 4 hours) antitussive agent Pack: 100 mL.
phosphate 10.95 mg, sodium citrate 54.4 mg, men- Syrup, Chlorpheniramine maleate 2 mg, Ammonium which is non-constipating, non-habit forming and Dose: Adult, 10 mL. Child (6-12 years): 5 mL; 1-5
thol 1.1 mg per 5 mL. chloride 50 mg, Ipecacuanha tincture 0.1 mL, Anise non-sedative. It has a weak bronchodilator property years: 2.5 mL To be taken every 3-4 hours.
Pack:100 mL water conc. 0.1 mL, Sodium citrate 50 mg, Citirc and stimulates the respiratory centre. It suppresses
all kinds of cough without interfering with patient’s OTC Dr. Meyer’s Cofmix® Junior (Farmex)
acid 10 mg, Menthol 1 mg; flavoured, reddish liquid.
OTC BENYLIN® for Children (NGC) ability to cough and bring up sputum voluntarily. Syrup, Diphenhydramine HCl 7 mg, sodium citrate
Pack: 100 mL in amber bottle.
Linctus, Diphenhydramine HCl 7 mg, sodium citrate Ammonium chloride and sodium citrate help in 28.5 mg, menthol 0.25 mg per 5 mL.
28.5 mg per 5 mL. OTC COFLAX® (Drugfield) liquefying and expectoration of mucous with normal Pack: 100 mL.
Pack: 100 mL Syrup, Diphenhydramine HCI 13.50 mg, codeine cough reflex, which is not blocked by Noscapine. OTC EMZOLYN® (Emzor)
phosphate 10.50 mg, ammonium chloride 100 mg, Chlorpheniramine maleate is an antihistamine
OTC BONAKOFF® (Bond) Syrup, Diphenhydramine HCl 14 mg, menthol 1.1 mg,
sodium citrate 50 mg, menthol 1.10 mg per 5 mL. which is used for the symptomatic treatment of
Expectorant, Diphenhydramine HCI 15 mg, sodium ammonium chloride 135 mg, sodium citrate 57 mg
Pack:100 mL cough and common cold.
citrate 50 mg, ammonium chloride 125 mg, menthol per 5 mL; pleasantly flavoured syrup in tamper-proof
1 mg per 5 mL; flavoured vehicle. OTC COF OFF® (Mecure) Indications: For suppression of continuous and bottle with company logo.
Pack: 100 mL Syrup (Adult), Diphenhydramin HCl 14 mg, ammo- irritating cough and for facilitation of expectoration; Pack: 100 mL; 2 L.
Indications: Reduces bronchial and nasal con- nium chloride 135 mg, menthol 1.1 mg per 5 mL; whooping cough. Paediatric Syrup, Diphenhydramine HCl 7 mg, men-
gestion. orange coloured syrup Dose: Adults: 10-20 mL 3-4 times daily. thol 0.55 mg per 5 mL; pleasantly flavoured syrup in
Dose: Child (1 – 5 years): 2.5 mL every 3 – 4 hours. Pack: 100 mL. Child: 5-10 mL 2-3 times daily. tamper-proof bottle with company logo.
6 – 12 years: 5 mL every 3 – 4 hours. Syrup (children), Diphenhydramin HCl 7 mg, sodium Paediatric suspension, Noscapine 1.83 mg, Ammo- Pack: 100 mL.
citrate 28.5 mg per 5 mL; pink coloured syrup. nium chloride 7 mg, Sodium citrate 0.67 mg per mL.
OTC BRADCUFF® (Bradford) Pack: 50 mL. OTC EVAPHEN® Linctus with Codene (Evans)
Pack: 100 mL.
Liquid, Ammonium chloride 135 mg, ammonium Dose: Child (1-3 years): 1.25-2.5 mL 2-3 times daily; Linctus, Diphenydramine HCl 13.50 mg, Ammonium
bicarbonate 62.5 mg, diphenhydramine HCl 6.25 OTC COFTA® (Evans) 3-12 years, 3.75-5 mL 2-3 times daily. chloride 120 mg, Sodium citrate 54.44 mg, Codeine
mg per 5 mL. Syrup, Ipecacuanha tincture 100l, liquorice extract phosphate 10.95 mg, Menthol 1.10 mg per 5 mL.
Pack: 100 mL 250l, ammonia q.s, peppermint oil 6.9l, aniseed oil OTC Crystal Cough & Cold (Crystal) Pack: 100 mL
2.6l per 5 mL; dark brown thick and good tasting Syrup, Diphenhydramine HCl 14 mg, ammonium Indications: For the relief of coughs, especially for
OTC BRONCHICUM® (Sanofi-Aventis) chloride 140 mg, trisodium citrate 59 mg, citric acid
liquid. dry and irritating cough.
Elixir, Thyme fluid extract 5 g, Primula root fluid monohydrate 6 mg, menthol 10 mg per 5 mL
Pack: 60 mL. Dose: Adults and child (≥12 years):10 mL every
extract 2.5 g. Pack: 100 mL
Dose: Adult, 10-15 mL 3-4 times daily.Child (6 3-4 hours
Pack: 100 mL bottle. Dose: Adult, 15-30 mL 3-4 times daily.
months-2 years), 2.5 mL 3-4 times daily; 2-10
years, 5 mL 3-4 times daily; 10-15 years, 10 Child (1-6 years): 5 mL 2-3 times daily; >6 OTC GAUZENOL-F® (Gauze)
POM BROZELIN® (Phillips)
mL 3-4 times daily. years, 5-10 mL 2-3 times daily. Expectorant, Diphenhydramine HCI 12.5 mg, sodium
Syrup, Ambroxol HCl 30 mg, salbutamol 2 mg,
306 | Compound Cough Preparations Compound Cough Preparations | 307
citrate 57 mg, ammonium chloride 120 mg, menthol tive symptoms and for the treatment of hay fever OTC LINCTIFED P® (SKG) Pack: 100 mL
1.5 mg, ephedrine HCI 6 mg per 5 mL. and other allergic conditions affecting the upper Paediatric Syrup, Codeine phosphate 3 mg, guaiphen- Indications: Help to naturally relief throat irritations
Pack:100 mL; 2 L respiratory tract. esin 50 mg, pseudoephedrine HCl 12 mg, triprolidine associated with dry and stubborn coughs. Also use-
Warning: May cause drowsiness, if affected. do not HCl 0.6 mg. ful for the relief of bronchial congestion.
OTC GREENLIN® (Greenlife)
drive or operate machinery. Avoid alcoholic drink. Pack: 60 mL. Dose: Children (2-5 years): 5 mL 2 to 3 times daily;
Syrup, Dextromethorphan (as HCl) 10 mg, guaiphen-
Dose: Adults; 5 mL – 10 mL Dose: Child (6-12 years), 10 mL 3 times daily; 2-5 6-12 years, 10 mL 2 to 3 times daily; >12
esin 50 mg per 5 mL; yellow sugar-free syrup.
Children (6-12 years); 5 mL years, 5 mL 3 times daily. years, 15 mL 2 to 3 times daily
Pack: 100 mL.
(1-5 years);2.5 mL. To be taken 3 times a Not recommended for children <1 year.
Dose: Adult & child (>12 years): 5-10 mL 4 times OTC LIXYPED® (May & Baker)
day after meal or when the cough is severe. Paediatric syrup, Diphenhydramine HCl 7.0 mg,
daily; <12 years, not recommended. Linctus, Promethazine HCl 1.5 mg, pholcodeine 1.5
sodium citrate 28.5 mg, menthol 0.55 mg per 5 mL.
Paediatric syrup, Dilute acetic acid BP 0.42 mL per 5 OTC KOFREST® (Crowther) mg, ethanol 3.8% per 5 mL
Pack: 100 mL.
mL; red sugar-free syrup. Syrup, Wet, Dry & Asthmatic cough. Pack: 100 mL
Dose: Children (1-5 years): 5 mL every 3 to 4 hours;
Pack: 100 mL. Pack: 100 mL.
OTC MAYSEDYL® (May & Baker) 6-12 years, 10 mL every 3 to 4 hours.
Dose: Child (3 months – 1 year): 2½ mL; 1-2 years, 5
OTC KOFSIL® with Codeine (Nosak) Linctus, Promethazine HCl 3.6 mg, codeine 9 mg, Syrup, Diphenhydramine HCl 13.5 mg, codeine phos-
mL; >2½ years, 10 mL. May repeat as needed
Suspension, Ammonium chloride 87 mg. sodium ephedrine HCl 7.2 mg per 5 mL. phate 10.95 mg, sodium citrate 54.4 mg, menthol
every 2-3 hours.
citrate 43 mg, diphenhydramine 15 mg, codeine Pack: 100 mL. 1.1 mg per 5 mL.
OTC GREENTUS® (Greenlife) phosphate 15 mg, menthol crystals 2 mg per 5 mL Pack:100 mL
OTC MELROSUM® (Sanofi-Aventis) Dose: Children (1-5 years): 2.5 mL every 3 to 4 hours;
Syrup, Guaiphenesin 50 mg per 5 mL; yellow, honey Pack: 100 mL
Syrup, Mel (honey), tinct. grindelia 0.2 mL, pimpinella 6-12 years, 5 mL every 3 to 4 hours.
& lemon flavoured syrup. Dose: Adult, 10 mL. Child (6-12 years): 5 mL; 1-5
0.2 mL, tinct. primrose 1 mL, tinct. rose 1 mL, tinct. Not recommended for children <1 year.
Pack: 100 mL years, 2.5 mL. May repeat doses every 4-5
thyme 1.2 mL per 100 mL.
Dose: Adult & child (>12 years): 10-20 mL; 6 to 12 hours as needed.
Pack: 100 mL OTC Nosak Baby Cough Syrup (Nosak)
years, 10 mL; 2-6 years, 5 mL; <2 years, not
OTC KOMIX® (Orange Drugs) Indications: Catarrhal disease of the respiratory Syrup, Squill oxymel 0.1 mL, Ipecacuanha tincture
recommended. Above dosages may be
Sachet, Dextromethorphan HBr 15 mg, guaifenesin organs, especially in delicate patients, children & 0.1 mL, Sodium citrate 43 mg, Anise water conc 0.1
EMDEX
repeated 3-4 times daily.
100 mg, chlorpheniramine maleate 2 mg per 7 mL pregnant women. mL, Menthol crystals 1 mg per 5 mL.
OTC JULYN® (Juhel) Pack: Sachet of 7 mL. Dose: Adult, 15 mL 3 times daily. Child (>12 years): Pack: 100 mL.
Syrup, Diphenhydramine HCl 14 mg, ammonium Dose: Adult, 1-2 sachets 3 times daily; Child (6-12 10 mL 3 times daily; >5 years, 5 mL 3 times Indications: Relief of irritating cough; nasal and
chloride 135 mg, sodium citrate 57 mg, menthol years): 1 sachet 3 times daily daily; 1-3 years, 2.5 mL 3 times daily. chest congestion; teething troubles.
1.1 mg per 5 mL. Dose: Child (3 months – 1 year): 2.5 mL 3 times daily;
OTC KOSLYN® (Gauze) OTC MEXATRIL® (Tandem) 2-5 years, 5 mL 3 times daily; 6-12 years, 5-10
Syrup, Diphenhydramine HCI 14 mg, ammonium Syrup, Dextromethorphan HBr 8 mg, guaifenesin 20 mL 3-4 times daily.
Paediatric syrup, Diphenhydramine HCl 7 mg, sodium
chloride 135 mg, sodium citrate 57 mg, menthol mg, chlorpheniramine maleate 1 mg, menthol 1.1
citrate 28.5 mg per 5 mL.
1.1 mg per 5 mL mg, ascorbic acid 10 mg per 5 mL. OTC OSADEX® (Greenlife)
Pack: 100 mL; 2 L Pack: 100 mL Mixture, Chlorpheniramine maleate 2 mg, am-
OTC JULYN® with Codeine (Juhel) Dose: Adult and child (>12 years), 10 mL 3 times monium chloride 70 mg, sodium citrate 40 mg,
OTC KOSLYN® Baby Cough Syrup (Gauze) Levo-menthol 1 mg per 5 mL.
Syrup, Diphenhydramine HCl 14 mg, codeine daily; 2-12 years, 2.5-5 mL 3 times daily.
Oral Liquid, Chlorpheniramine maleate 2 mg, sodium Pack: 100 mL.
phosphate 10.95 mg, ammonium chloride 132 mg,
citrate 28.5 mg, menthol 0.55 mg per 5 mL OTC Moko Cough Syrup (New Healthway) Dose: Adult & child (>10 years), 5 mL; 5-10 years,
sodium citrate 57 mg, menthol 1.1 mg per 5 mL
Pack: 100 mL; 2 L Syrup, Sodium citrate 62.5 mg, ammonium chloride 2.5 mL; 2-5 years, 1.25-2.5 mL. May repeat
Pack: 100 mL
1.05 mg, menthol 3.125 mg, chlorpheniramine 2.125 3 times daily.
OTC KUFDRYL® (Therapeutic)
OTC KOFAREST® (Al-Tinez) mg per 5 mL.
Syrup, Diphenhydramine HCl 15mg ammonium OTC OSINEX® (Neimeth)
Syrup, Salbutamol (as sulfate) 2 mg, ambroxol (as Pack: 100 mL.
chloride 130 mg, menthol 1.10 mg per 5 mL. Syrup, Chlorpheniramine, dextromethorphan,
HCl) 30 mg, guaifenesin 100 mg, menthol 5 mg per
Advice to patients: May cause drowsiness; avoid OTC NEIMELYN® (Neimeth) guaiphensin, phenyephephrine.
10 mL; yellow syrup.
alcoholic beverages Syrup, Diphenhydramine. Pack: 100 mL; 1 L.
Pack: 100 mL
Pack: 100 mL.
Indications: Productive cough associated with OTC KIDI KUFDRYL® (Therapeutic) OTC PIRITON® Adult Expectorant (Evans)
bronchospasm in conditions such as bronchitis, Syrup, Diphenhydramine HCl 7.5 mg, menthol 0.55 OTC NEOFYLIN® (Mopson) Linctus, Chlorpheniramine maleate 2 mg, Ammo-
COPD, emphysema, bronchial asthma. mg, sodium citrate 28.5 mg. Syrup, Chlorphenamine maleate 2 mg, ammonium nium chloride 100 mg, Sodium citrate 44 mg per
Dose: Adult and Child (≥12 years), 10-20 mL 3-4 chloride 50 mg, sodium citrate 50 mg, citric acid 10
OTC KUF RELIEF® (Embassy) 5 mL.
times daily. mg, ipecacuanha tincture 0.1 mL per 5 mL
Tablet, Paracetamol 325 mg, ammonium chloride Pack: 100 mL
Pack: 100 mL, 2 L. Indications: Piriton expectorant linctus is an effec-
OTC KOFAREST-PD® (Al-Tinez) 100 mg, chlorpheniramine maleate 2 mg, sodium
Syrup, Salbutamol (as sulfate) 1 mg, ambroxol (as citrate 25 mg. OTC NOMALYN® (Nomagbon) tive expectorant for use in upper respiratory tract in-
HCl) 15 mg, guaifenesin 50 mg, menthol 2 mg per Pack: 48 x 4’s. Syrup (Adult), Diphenhydramine HCl 10 mg, am- fections including the common cold and bronchitis.
5 mL; yellow syrup. monium chloride 100 mg, sodium citrate 50 mg, Dose: Adult (≥12 years): 5 – 10 mL 3 – 4 times daily.
Pack: 60 mL OTC LABOCOF® (Embassy)
menthol 1 mg per 5 mL; pink viscous syrup OTC PIRITON Children Expectorant® (Evans)
Indications: See under Kofarest®. Tablet, Chlorpheniramine 4 mg, dextromethorphan
Pack: 100 mL (in glass bottle). Linctus, Chlorpheniramine maleate 1 mg, Ammo-
Dose: Child (2-6 years), 5 mL 3 times daily; 6-12 years, 10 mg.
Syrup, (Children), Diphenhydramine HCl 5 mg, Tolu nium chloride 50 mg, Sodium citrate 22 mg per 5 mL.
10 mL 3-4 times daily. Pack: 4’s.
syrup 0.1 mL, sodium citrate 25 mg, menthol 0.05 Pack: 100 mL
OTC LINCTIFED F® (SKG) mg per 5 mL; pink viscous syrup Dose: Children 6 – 12 years: One teaspoonful (5 mL)
OTC KOFMED® (Sterling Drug)
Syrup, Codeine Phosphate 7.5 mg, guaiphenesin Pack: 100 mL (in glass bottle) three to four times daily.
Syrup, Diphenhydramine hydrochloride 14.2 mg,
ammonium chloride 130 mg, sodium citrate 62.0 100 mg, pseudoephedrine HCl 20 mg, triprolidine
OTC NOVALYN® (SKG) OTC RABLYN® (Rajrab)
mg, menthol crystal 1.1 mg per 5 mL. HCl 1.25 mg per 5 mL.
Linctus, Ipecacuanha liquid extract 0.15 mL, purified Liquid, Diphenhydramine HCl 13 mg, ammonium
Pack: 100 mL Pack: 60 mL.
honey 1.12 g, glycerol 0.75 mL, citric acid 50 mg, chloride 130 mg, sodium citrate 57 mg, menthol
Indications: For the relief of cough and its conges- Dose: Adult and child >12 years, 10 mL 3 times daily
lemon oil 0.6 µl, lime oil 1.25 µl 1 mg; in 100-mL PET bottle marked “RAJRAB” on
308 | Compound Cough Preparations 7.3 Other drugs acting on the respiratory tract | 309
the cap. Pack: 60 mL; 100 mL in amber bottles. 1.1 mg per 5 mL. mia, hypoxaemia, anaemia, seizures).
Pack: 100 mL; 2 L Dose: Child (6-12 year s): 10 mL 3 times daily; 2-5 Pack: 100 mL Indications: Neonatal apnoea in preterm
years, 5 mL 3 times daily. infants.
OTC RichyGold Cough & Cold (Richygold) OTC ZUBES® Cough Syrup (P.Z.)
Syrup, Diphenhydramine HCl 14 mg, ammonium OTC TUSSYLIN® (Afrab-Chem) Paediatric Syrup, Ipecacuanha liquid extract 0.0119 Precautions: Cardiovascular disorders, hepatic
chloride 140 mg, trisodium citrate 59 mg, citric acid Syrup, Ammonium chloride 135 mg, diphenhydramine mL, Squill Vinegar 0.1124 mL. or renal impairment.
monohydrate 6 mg, menthol 1 mg per 5 mL. HCl 14 mg, sodium citrate 57 mg, mentol 1.1 mg per Dose: Child (>6 months), 2.5 mL in water every 4 Adverse effects: Lethargy (physical sign of
Pack: 100 mL amber bottle. 5 mL. hours; 2-6 years, 5 mL every 4 hours. withdrawal); feeding intolerance; irritabil-
Dose: By mouth, Adults, 15-30 mL 3-4 times daily. Pack: 100 mL. ity, excessive CNS stimulation, tachycardia
OTC ZUBES® Soothing Cough Mixture (P.Z)
Children (1-6 yrs), 5 mL 2-3 times daily; 6 yrs Dose: Adult, 15-30 mL 2-3 times daily.
Syrup, Mentol 16 mg, aniseed oil 11 mg, peppermint (early sign of toxicity), hyperglycaemia or
& above, 5-10 mL 2-3 times daily. Child (>12 years): 5 mL 2-3 times daily
Paediatric Syrup, Diphenhydramine HCl 7 mg,
oil 8 mg. hypoglycaemia; rarely acidosis, disseminated
OTC RichyGold Cough Expectorant (Richygold) Dose: Adult and child (>12 years), 5-20 mL every intravascular coagulation, haemorrhage, lung
sodium citrate 28.5 mg, methol 0.55 mg per 5 mL
Syrup, Diphenhydramine maleate 2 mg, ammonium 6 hours. oedema, gastritis, renal failure, retinopathy of
Pack: 100 mL.
chloride 100 mg, sodium citrate 60 mg, menthol 1.5 Child (6-12 years), 5 mL every 6 hours. prematurity, sepsis.
Dose: Child (1-5 years): 5 mL 3 times daily; >6 years,
mg per 5 mL
10 mL 3 times daily. Dose: NOTE: All doses expressed as caffeine
Pack: 100 mL amber bottle. 7.3 Other drugs acting on the
Not recommended for children <1 year. citrate.
Dose: By mouth, Adults, 15 mL 3-4 times daily respiratory tract
Child (1-5 years): 2.5 mL 3 times daily; 6-12 OTC TUXIL® (Fidson) Neonatal apnoea, by mouth, or by
years, 5-10 mL 3-4 times daily. Syrup, Cetirizine HCl 1.5 mg, menthol 1.0 mg per IV injection, NEONATE 20 mg/kg as
CAFFEINE CITRATE
5 mL a loading dose, then 5 mg/kg once
OTC SOFA-LIN® (Sofak)
Pack: 100 mL Caffeine citrate, a respiratory stimulant, is used daily starting 24 hours after loading
Syrup, Diphenhydramine HCI 7 mg, citric acid 3 mg,
Indications: Symptomatic relief of sneezing, itching, for neonatal apnoea in preterm infants (born dose; continue for 4–5 days after
ammonium chloride 70 mg, sodium citrate 29.5 mg,
watery eyes (lacrimation), runny nose (rhinorrhea), less than 35 weeks gestastional age and under cessation of apnoea.
menthol 0.55 mg per 5 mL
EMDEX
itchy eyes and/or itching associated with seasonal Note: Caffeine citrate 2 mg = caffeine base 1 mg.
Pack: 100 mL 2 kg). It is preferred over theophylline, as caf-
(e.g. hay fever), allergic rhinitis or other upper res-
Dose: 2.5 – 5 mL every 4 hours. feine has a better safety profile and does not POM Caffeine citrate (WMF 25.2)
piratory allergies.
Liquid, Diphenhydramine HCI 14 mg, sodium citric require routine drug level monitoring. Other Injection, Caffeine citrate 20 mg/mL (equiv. to 10 mg
Dose: Children (<5 years): 5 mL every 8 hours; 6-12
59 mg, ammonium chloride 140 mg, citric acid 6 mg, causes of neonatal apnoea should be sought caffeine base/mL).
years, 10 mL every 8 hours.
menthol 1.1 mg per 5 mL Oral liquid, Caffeine citrate 20 mg/mL (equiv. to 10
and treated before treatment with caffeine is
Pack: 100 mL OTC TUXIL-4® (Fidson) mg caffeine base/mL).
Syrup, Cetirizine HCI 1.5 mg, guaifenesin 50 mg,
started (e.g. sepsis, hypothermia, hypoglycae-
OTC TIXYLIX® (May & Baker)
acetaminophen 125 mg, dextromethorphan HBr 5
Linctus, Promethazine HCl 1.5 mg, pholcodeine 1.5
mg, menthol 2 mg per 5 mL.
mg, ethanol 3.8% per 5 mL.
Pack: 100 mL
Pack: 100 mL.
Indications: Effective for the relief of fever often
Dose: Child (3-5 years): 5 mL 2-3 times daily; 6-10
associated with cough, cold and allergy; loosens
years, 5-10 mL 2-3 times daily.
mucus (phlegm) and makes expectoration easier.
OTC TUSSEX® (Medreich) Dose: CHILD (4-12 years): 10 mL every 8 hours.
Syrup, Dextramethorphan 10 mg, guaiafenesin 100
OTC TUXIL-C® (Fidson)
mg, paracetamol 250 mg, menthol 1.50 mg per 5 mL.
Syrup, Diphenhydramine HCl 7 mg, pholcodine 2
Pack: 100 mL (in amber bottle).
mg, sodium citrate 27 mg, menthol 2 mg per 5 mL.
Dose: Adult, 5-10 mL 4 times daily.
Pack: 100 mL
Child (6-12 years): 5 mL 3-4 times daily; 2-6
Indications: Effective relief of children’s dry, tickling
years, 2.5 mL 3-4 times daily.
and unproductive cough; suppresses coughing.
Not recommended for children <2 years
Dose: CHILD (4-12 years): 5-10 mL every 8 hours.
OTC TOPLIN® (Topway)
OTC TUXIL-D® (Fidson)
Syrup (Children), Diphenhydramine HCl 7 mg, sodium
Syrup, Cetirizine HCI, ephedrine HCI, ammonium
citrate 28.5 mg per 5 mL.
chloride, sodium citrate, menthol.
Pack: 100 mL.
Pack: 100 mL.
Syrup (Adult), Diphenhydramine HCl 14 mg, ammo-
Dose: Adult and Child (>12 years), 10 mL 3 times a
nium chloride 170.0 mg, sodium citrate 57.0 mg,
day; 6-12 years, 5 mL 3 times a day; 1-5 years,
menthol 1.1 mg per 5 mL.
2.5 mL 3 times a day.
Pack: 100 mL.
OTC TUXIL-N® (Fidson)
OTC TUSSIREX-F® (SKG)
Syrup, Chlorpheniramine maleate, ephedrine HCI,
Syrup, Codeine Phosphate 7.5 mg, potassium guai-
ammonium chloride, sodium citrate, menthol.
acolsulphonate 120 mg, pseudoephedrine HCl 20
Pack: 100 mL.
mg, triprolidine HCl 1.25 mg per 5 mL; yellow syrup.
Dose: Adult and Child (>12 years), 10 mL 3 times a
Pack: 60 mL; 100 mL in amber bottles.
day; 6-12 years, 5 mL 3 times a day; 1-5 years,
Dose: Adult and child >12 years, 10 mL 3 times daily
2.5 mL 3 times a day.
OTC TUSSIREX-P® (SKG)
OTC XPEL® (Dana)
Paediatric Syrup, Codeine phosphate 5 mg, potassium
Liquid, Diphenhydramine HCI 14 mg, ammonium
guaiacolsulphonate 60 mg, pseudoephedrine HCl 12
chloride 135 mg, sodium citrate 57 mg, menthol
mg, triprolidine HCl 0.6 mg per 5 mL
| 311
8. Antiallergics and drugs Antiallergics and drugs of urticaria or for severe skin reactions. Oral
used in anaphylaxis corticosteroids are also used to relieve severe
exacerbations in chronic urticaria, but long-
The H 1-receptor antagonists are generally
used in anaphylaxis
term use should be avoided.
referred to as antihistamines. They inhibit the
wheal, pruritus, sneezing and nasal secretion Corticosteroids may be used topically to reduce
responses that characterize allergy. Antihista- inflammation in allergic rhinitis but should only
mines thus relieve the symptoms of allergic be used systemically for this condition when
reactions, such as urticaria, allergic rhinitis, symptoms are disabling.
and allergic conjunctivitis; they also control Adverse effects associated with long-term use
pruritus in skin disorders, such as eczema. of corticosteroids include inhibition of growth
8.1 Antihistamines. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 312 Antihistamines are used to treat drug allergies, in children, disturbances of electrolyte balance
food allergies, insect stings and some of the leading to oedema, hypertension and hypokal-
8.2 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 318 symptoms of anaphylaxis and angioedema. aemia, with osteoporosis, spontaneous frac-
8.3 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 319 Drug treatment and other supportive care tures, skin thinning, increased susceptibility
should not be delayed in critically ill patients to infection, mental disturbances and diabetes
(see Allergic Emergencies below). Specific mellitus. For further information on the disad-
precipitants should be sought and if identified, vantages of corticosteroids, see section 10.3.
further exposure avoided and desensitization Allergic emergencies
considered.
Anaphylactic shock and conditions such as
In practice, all antihistamines are equally angioedema are medical emergencies that
EMDEX
effective in relieving the symptoms of allergic can result in cardiovascular collapse and death.
reactions and differ mainly in the intensity of They require prompt treatment of laryngeal
sedative and anticholinergic (more correctly oedema, bronchospasm and hypotension.
antimuscarinic) effects. Selection of an antihis- Atopic individuals are particularly susceptible.
tamine should thus be based on the intended Insect stings and certain foods including eggs,
therapeutic use, the likely adverse reactions, fish, cow’s milk protein, peanuts and tree nuts
and the cost. Drowsiness and sedation are are a risk for sensitized persons. Therapeutic
particular disadvantages of the older antihis- substances particularly associated with ana-
tamines such as chlorphenamine; patients phylaxis include blood products, vaccines, hy-
should be warned against driving or operating posensitizing (allergen) preparations, antibac-
machinery. Newer antihistamines do not cause terials (especially penicillins), iron injections,
significant sedation. Other central nervous heparin, and neuromuscular blocking drugs.
depressants, including alcohol, barbiturates, Acetylsalicylic acid and other nonsteroidal
hypnotics, opioid analgesics, anxiolytics and antiinflammatory drugs (NSAIDs) may cause
neuroleptics, may enhance the sedative effects bronchoconstriction in leukotrienesensitive
of antihistamines. Since antihistamines inter- patients. In the case of drug allergy, anaphy-
fere with skin tests for allergy, they should be laxis is more likely to occur after parenteral
stopped at least one week before such tests. administration. Resuscitation facilities should
Corticosteroids, such as dexamethasone, always be available when injecting a drug
hydrocortisone, or prednisolone, suppress associated with a risk of anaphylactic reactions.
or prevent almost all symptoms of inflam- Anaphylactic reactions may also be associated
mation associated with allergy. The route of with additives and excipients in foods and
administration depends on the particular type medicines. It is wise to check the full formula
of allergic condition. For example, for a mild of preparations which may contain allergenic
allergic skin reaction, the best therapy may be fats or oils.
the use of a corticosteroid ointment or cream.
If the skin reaction does not respond to topical First-line treatment of a severe allergic reaction
corticosteroid therapy, it may be necessary to includes administering epinephrine (adrena-
give a corticosteroid orally. line), keeping the airway open (with assisted
respiration if necessary), and restoring blood
Allergic reactions of limited duration and with pressure (laying the patient flat, raising the
mild symptoms, such as urticaria or allergic feet). Epinephrine (adrenaline) should be
rhinitis, usually require no treatment. If on the given immediately by intramuscular injection
other hand, symptoms become persistent, to produce vasoconstriction and bronchodila-
antihistamines constitute the mainstay of tion and injection should be repeated if neces-
treatment. However, oral corticosteroids may sary at 5-minute intervals until blood pressure,
be required for a few days in an acute attack pulse and respiratory function have stabilized.
312 | 8.1 Antihistamines 8.1 Antihistamines | 313
If there is cardiovascular shock with inadequate over at least 20 minutes. OTC CET-10® (Juhel) Nursing considerations: Give with meals if GI
circulation, epinephrine (adrenaline) must Tablet, Cetirizine 10 mg. upset occurs; may slightly reduce absorption.
be given cautiously by slow IV injection of a 8.1 Antihistamines 10 mg – 10 x 10’s; 500’s. Do not crush or chew sustained release drug
dilute solution. Oxygen administration is also OTC CETRIDAN® (Dana) product.
of primary importance. CETIRIZINE Tablet, Cetirizine HCI 10 mg; f-c tab. • Give IV slowly; if adverse reactions occur,
Therapeutic category: Antihistamine, H 1- 10 mg – 1 x 10’s; 3 x 10’s (in blisters) discontinue drug and notify physician.
An antihistamine such as chlorphenamine by
slow IV injection is a useful adjunctive treat- blocker, Non-sedating. OTC CIKAZINE® (Michelle Lab) • Relieve dry mouth with chewing gum or
ment given after epinephrine (adrenaline) Pharmacology: Cetirizine is a piperazine Tablet, Cetirizine 10 mg frequent sips of water.
injection and continued for 24 to 48 hours to derivative and metabolite of hydroxyzine. It is 10 mg – 100’s; 10 x 10’s (in blisters) • Raise bed rails, institute safety measures; may
reduce the severity and duration of symptoms a non-sedating antihistamine reported to be assist with ambulation.
OTC JAWAZINE® (Jawa)
and to prevent relapse. The onset of action of long-acting and with some mast-cell stabilising Capsule, Cetirizine HCl 10 mg. • Advise patient to avoid alcohol and driving.
an IV corticosteroid such as hydrocortisone is activity. It appears to have a low potential for 10 mg – 10 x 10’s (in blisters). Dose: Allergy, by mouth, ADULT 4 mg every
delayed by several hours but it should be given drowsiness in usual doses and to be virtually 4–6 hours (maximum 24 mg daily);
OTC HISTACET® (Medreich) CHILD under 1 year not recom-
to help prevent later deterioration in severely free of antimuscarinic activity. It diminishes Tablet, Cetirizine 10 mg; white scored tab. marked
affected patients. or abolishes the major actions of histamine in mended, 1–2 years 1 mg twice daily,
“M+”.
the body by competitive reversible blockade of 10 mg – 2 x 10’s. 2–5 years 1 mg every 4–6 hours
Further treatment of anaphylaxis may include (maximum 6 mg daily), 6–12 years 2
histamine H1-receptor sites on tissues. Does not Syrup, Cetirizine 5 mg per 5 mL; clear colourless
intravenous fluids, an intravenous vasopressor mg every 4–6 hours (maximum 12
inactivate the histamine or prevent its synthe- liquid.
such as dopamine, intravenous aminophylline Pack: 60 mL. mg daily).
sis or release. H1 receptors are responsible for
[not included on WHO Model List] or injected or Allergic reactions, anaphylaxis (ad-
vasodilation, increased capillary permeability, OTC ZIN-TEN® (Nelpharm)
nebulized bronchodilator, such as salbutamol. junct), by SC, IM, or IV injection, ADULT
flare and itch reactions in the skin, and to some Tablet, Cetirizine HCl 10 mg
EMDEX
Steps in the management of anaphylaxis: extent for contraction of smooth muscle in the 10 mg – 100’s 10–20 mg (maximum 40 mg in 24
1. Sympathomimetic bronchi and GI tract. hours); CHILD 1 month–1 year 250
OTC ZYNCET® (Phillips)
Epinephrine (adrenaline) by IM injection Indications: To alleviate conditions such as µg/kg (maximum 2.5 mg), 1–5 years
Tablet, Cetrizine (as HCl) 10 mg.
using epinephrine injection 1 in 1000, urticarial rashes and nasal allergy; to relieve Syrup, Cetirizine HCl 5 mg per 5 mL. 2.5–5 mg, 6–12 years 5–10 mg
ADULT and ADOLESCENT, 500 µg (0.5 symptoms of allergic rhinitis (hayfever), rhin- Pack: 60 ml (in amber coloured glassbottle). Dilution and Administration: Give IV injection
mL); INFANT under 6 months 50 µg (0.05 orrhoea and sneezing (and ocular symptom over 1 minute; if necessary, injection solution can
mL); CHILD 6 months–6 years 120 µg (0.12 be diluted with sodium chloride 0.9% injection.
such as conjustivitis). CHLORPHENAMINE
mL), 6–12 years 250 mcg (0.25 mL) Contra-indications: Potentially harzadous Synonym: Chlorpheniramine. OTC Chlorphenamine (WMF 3)
Note: The above doses may be repeated several ventricular arrhythmias have occurred when Tablet, Chlorphenamine (as hydrogen maleate) 4 mg.
times if necessary at 5-minute intervals, according
Therapeutic category: Antihistamine, H 1
non-sedating antihistamines (such as Astem- Injection, Chlorphenamine (as hydrogen maleate)
to blood pressure, pulse, and respiratory function. Blocker. 10 mg/mL; in1-mL ampoule.
izole and Terfenadine) have been given con- Indications: Symptomatic relief of allergy,
2. If circulation inadequate, by slow IV
comitantly with drugs liable to interfere with allergic rhinitis (hay fever) and conjunctivitis, OTC Chlorphenamine (EDL 18.2)
injection using epinephrine injection 1 in Tablet, Chlorphenamine maleate 4 mg.
hepatic metabolism, with other potentially urticaria, insect stings and pruritus of allergic
10 000 (given at a rate of 1 mL/minute), Oral liquid, Chlorphenamine maleate 2 mg per 5 mL.
arrhythmogenic drugs and with those likely origin; adjunct in the emergency treatment of
ADULT 500 µg (5 mL); CHILD 10 µg/kg Injection, Chlorphenamine maleate 10 mg per mL;
to cause electrolyte imbalance. Antihista- anaphylactic shock and severe angioedema.
(0.1 mL/kg), given over several minutes. in 1-mL amp.
mines may suppress the cutaneous histamine Precautions: Prostate enlargement, urinary
3. Vital functions
response to allergen extracts and should be retention; ileus or pyloroduodenal obstruc- OTC ALLERGIN® (Afrab-Chem)
Maintain an open airway; give oxygen by Tablet, Chlorphenamine maleate 4 mg; light pink
stopped several days before skin testing. An- tion; glaucoma; child under 1 year; pregnancy
mask, restore blood pressure (lay patient scored tab marked with the maker’s symbol.
tihistamines should not be given to neonates (Appendix 2); breastfeeding (Appendix 3);
flat, raise feet). Pack: 1000.
owing to their increased susceptibility to renal impairment (Appendix 4); hepatic im-
4. Antihistamine such as chlorphenamine Syrup, Chlorphenamine maleate 2 mg per 5 mL.
antimuscarinic effects. pairment (Appendix 5); epilepsy; interactions:
by IV injection over 1 minute, ADULT Pack: 60 mL; 2 L.
Adverse effects: Rarely, use of non-sedating Appendix 1
10–20 mg, repeated if required (maximum OTC ANTIHIST® (Therapeutic)
antihistamines may be associated with ven- Adverse effects: Drowsiness (rarely paradoxical
total dose 40 mg in 24 hours), CHILD 1 Tablet, Chlorphenamine maleate 4 mg; yellow
tricular arrhythmias which has limited their stimulation with high doses, or in children or
month–1 year 250 µg/kg (maximum 2.5 scored tab.
use. Others are convulsion, sweating, myalgia, elderly), hypotension, headache, dizziness,
mg), 1–5 years 2.5–5 mg, 6–12 years 5–10 4 mg – 100; 1000.
paraesthesias, extrapyramidal effects, tremor palpitations, psychomotor impairment, urinary
mg repeated if necessary up to 4 times daily. POM BETAFEMINE® (Beta Drugs)
sleep disturbances, depression, tinnitus, hy- retention, dry mouth, blurred vision, GI distur-
5. Corticosteroids such as hydrocortisone Injection, Chlorpheniramine 10 mg per mL; in 1
potension and hair loss, nausea, vomiting and bances; liver dysfunction; blood disorders; also
by slow IV injection, ADULT 100–300 mg; mL amp.
diarrhoea or epigastric pain. rash and photosensitivity reactions, sweating
CHILD up to 1 year, 25 mg; 1–5 years, 50 Pack: 1 mL x 100 amps.
Dose: Adult and Child (>6 years), by mouth, and tremor, hypersensitivity reactions (includ-
mg; 6–12 years, 100 mg.
10 mg once daily or 5 mg twice daily. ing bronchospasm, angiodema, anaphylaxis); OTC CHLORPHEN® (Emzor)
6. Intravenous fluids: start infusion with Tablet, Chlorpheniramine maleate 4 mg.
Child (2-6 years), Seasonal allergic injections may be irritant.
sodium chloride (0.5–1 litre during the first 4 mg – 1000’s.
rhinitis, 5 mg once daily or 2.5 mg Advice to patients: May cause drowsiness;
hour). Syrup, Chlorphenamine maleate 2 mg per 5 mL.
twice daily. swallow whole, do not crush or chew sustained
7. If the patient has asthma-like symptoms, Pack: 2 L.
Reduce dose by half in renal impair- release product; avoid alcohol, may impair
give salbutamol 2.5–5 mg by nebulization
ment. judgement and coordination. POM Chlorpheniramine-10 (Embassy)
or aminophylline 5 mg/kg by IV injection Injection, Chlorpheniramine maleate 10 mg per mL;
clear colourless liquid in 1 mL amp. stenosing peptic ulcer; symptomatic prostatic 4 mg – 1 x 3’s; 3 x 10’s DIMETHINDENE
Pack: 10 x 10’s. hypertrophy; bladder neck obstruction; pylo- Syrup, Cyproheptadine 2 mg per 5 mL; pale yellow Therapeutic category: Antihistamine, H1-re-
roduodenal obstruction; elderly, debilitated syrup.
OTC Chlorpheniramine (Emzor) ceptor antagonist.
patients; predisposition to urinary retention. Pack: 100 mL; 200 mL.
Tablet, Chlorpheniramine maleate 4 mg Indications: Indicated as symptomatic treat-
Pack: 10 x 10’s (in blister). Precautions: Pregnancy; children under 2 OTC ASKA-APET® (Diamond Remedies) ment of allergic reactions, urticaria, allergies
years; driving a car or operating machinery; Tablet, Cyproheptadine HCI 4 mg; uncoated tab. of the upper respiratory tract such as hay
OTC Chlorpheniramine (FAB)
patients with a history of bronchial asthma, in- 4 mg – 3 x 10’s (in blisters).
Syrup, Chlorpheniramine maleate 2 mg per 5 mL. fever and perenial rhinitis, food and drug al-
Pack: 60 mL creased intra-ocular pressure, hyperthyroidism, OTC CETOPRON® (Richygold) lergies, pruritus of various origins, insect bite,
cardiovascular disease, or hypertension due to Caplet, Cyproheptadine 4 mg; s-c tab. and pruritus in eruptive skin diseases such as
OTC Chlorphenamine (Juhel)
its atropine-like action; lower respiratory tract Pack: 3 x 10’s. chicken pox.
Tablet, Chlorphenamine maleate 4 mg.
4 mg – 1000. symptoms including acute asthma. OTC CYPENI® (Therapeutic) Contra-indications: Hypersensitivity to dime-
Interactions: MAOIs (enhance the anticholin- Syrup, Cyproheptadine HCl 2 mg, liquid glucose thindene maleate or any of its components.
OTC Chlorpheniraminme (Vitabiotics) ergic effects of antihistamines). Alcohol and 1.50 g, L-lysine monohydrochloride 50 mg per 5 mL. Precautions: Glaucoma, bladder neck ob-
Tablet, Chlorphenamine maleate 4 mg. other CNS depressants such as hypnotics, Pack: 100 mL; 200 mL. struction (eg, prostatic hypertrophy), chronic
4 mg – 1000’s
sedatives, tranquillisers. obstructive pulmonary disease. May impair
OTC CYPRIGOLD® (Therapeutic)
OTC CPM® (Dana) Adverse effects: CNS effects such as drowsi- ability to drive or operate machinery. Preg-
Syrup, Cyproheptadine HCl 2 mg, L-lysine 50 mg
Tablet, Chlorpheniramine maleate 4 mg ness (often transient); integumentary reaction liquid glucose 1.5 g per 5 mL. nancy, lactation; infants <1 year old (may cause
4 mg – 1000’s (in jar) such as urticaria and excessive perspiration;
Syrup, Chlorpheniramine maleate 2 mg per 5 mL
Pack: 100 mL; 200 mL. sleep apnea).
effects on special senses such as blurred Adverse effects: Drowsiness or fatigue, dry
Pack: 60 mL OTC CYPRODAN® (Dana)
vision, tinnitus; cardiovascular effects such as Tablet, Cyproheptadine HCI 4 mg; uncoated tab mouth, headahce and dizziness or vertigo. Ex-
OTC ECOPLEX® (Synergy) hypotension, anaphylactic shock, tachycardia; citement especially in children, muscle spasm
4 mg – 3 x 10’s
EMDEX
Syrup, Chlorpheniramine maleate 2.5 mg, ammo- haematological effects such as leucopenia, Syrup, Cyproheptadine HCI 2 mg per 5 mL and respiratory impairment may also occur.
nium chloride 125 mg, sodium citrate 55 mg per agranulocytosis; effects on digestive system
5 mL.
Pack: 100 mL Dose: Adult, by mouth, 20-40 drops 3 times
such as epigastric distress, anorexia; effect on Dose: By mouth, Adult, 4 mg 3 times daily. daily
Pack: 100 mL.
respiratory system such as nasal stuffiness; Child, 2 mg 3 times daily. Infant & children (>1 year): 10-20
OTC HISTINE® (Fidson) others such as fatigue, rigors, headache. drops 3 times daily.
OTC CYPRON® (Orange Drugs)
Tablet, Chlorphenamine maleate 4 mg. Advice to patients: May cause drowsiness; Caplet, Cyproheptadine HCI 4 mg.
4 mg – 100’s. OTC FENISTIL® (Novartis)
may stimulate appetite, avoid alcohol and Pack: 3 x 10’s
Oral drops, Dimethindene maleate 0.1%
POM MINEX-T® (Vixa) other CNS depressants; may impair judgement Pack: 1 x 20 mL bottle
OTC GENAPET® (Geneith)
Injection, Chlorpheniramine maleate 10 mg/mL and coordination. Tablet, Cyproheptadine 4 mg.
Pack: 1 mL x 10’s. Dose: In allergy and pruritus, Adult, by mouth, DIMETHINDENE plus PHENYLEPHRINE
4-20 mg daily in 3-4 divided doses or OTC NOVO GOLD® (N.C.I)
OTC NISE® (Jawa) Pharmacology: Dimethindene is a sedating
Caplet, Cyproheptadine HCl 4 mg; yellow caplet.
Syrup, Chlorphenamine maleate 2 mg per 5 mL as often as necessary; up to a max. 32
4 mg – 3 x 10’s. antihistamine with potent H 1-antagonistic
mg daily.
OTC NARAMIN® (NASDMU)
OTC ORAXIN® (Al-Tinez)
activity and mast cell stabilizing property.
Tablet, Chlorpheniramine maleate 4mg; marked “4 Child (7-14 years), usually 4 mg 2-3
Syrup, Cyproheptadine (as HCl) 2 mg, peptone 25 Phenylephrine belongs to the class of topical
mg” on one side and plain on the reverse. times a day according to the patient’s
mg, lysine (as HCl) 150 mg per 5 mL. sympathomimetic agents used as nasal decon-
4 mg – 1000’s weight and response; up to a max. 16
Pack: 100 mL; 200 mL. gestants. The combination provides quick and
mg a day; 2-6 years, initially 2 mg 2-3
OTC PIRITON® (Evans) Dose: Adult, 10 mL 3 times daily. lasting relief from stuffy and runny nose due to
times a day according to the patient’s Child (<3 years): 2.5 mL 2 times daily; 4-7
Tablet, Chlorphenamine maleate 4 mg; light yellow allergy or infection.
biconvex tab. marked ‘PIRITON’. weight and response; up to a max. 12 years, 2.5 mL 3 times daily; 7-14 years, 5 Indications: Common colds, acute and chronic
4 mg – 50’s; 500’s. mg a day. mL 3 times daily. rhinitis; seasonal (hay fever) and non-seasonal
Syrup, Chlorphenamine maleate 2 mg per 5 mL. In vascular headache and migraine,
OTC RICHAPETEE® (Richygold) allergic rhinitis; acute and chronic sinusitis; pre
Pack: 150 mL. Treatment and prophylaxis, initially
Tablet, Cyproheptadine 4 mg. & post operative care for nasal surgery; adju-
4 mg, repeated if necessary after an Syrup, Cyproheptadine 4 mg per 5 mL. vant in cases of acute otitis media.
CYPROHEPTADINE hour; not exceeding 8 mg within a
OTC SUPER APETI® (Shalina) Contra-indications: Hypersensitivity to any of
Therapeutic category: Antihistamine, H 1 4-to 6-hour period.
Tablet, Cyproheptadine HCl 4 mg. its components.
Blocker. Maintenance, 4 mg every 4 to 6 hours.
4 mg – 20’s. Precautions: Atrophic rhinitis; MAO inhibitors;
Pharmacology: Cyproheptadine is a serotonin As an appetite stimulant, Adult and Syrup, Cyproheptadine HCl 2 mg per 5 mL. Heart disease, high blood pressure, thyroid
and histamine antagonist with anticholinergic adolescent, usually 12 mg a day; Pack: 120 mL. disease, or glaucoma, and/or are taking anti-
and sedative properties. higher doses are not recommended.
OTC SUPERLIFETI® (Jubilee) depressants.
Indications: Allergy and pruritus; migraine Child (7-14 years), a max. 12 mg a day;
Tablet, Cyproheptadine (as HCl) 4 mg. May cause rebound congestion if used con-
headache; appetite stimulant. 2-6 years, a max. 8mg a day.
4 mg – 10’s. tinuously for longer than 1 week.
Contra-indications: Therapy of an acute asth- OTC ALPHA APETI® (Embassy) Syrup, Cyproheptadine (as HCl) 2 mg per 5 mL Dose: Adult and child >6 years: Instil 1-2
matic attack; newborn or premature infants; Tablet, Cyproheptadine 4 mg. drops into each nostril 3 times a day.
OTC TAVO-APPETI® (Justeen)
nursing mothers; known sensitivity to cypro- 4 mg – 20’s. Application: After blowing the nose
Tablet, Cyproheptadine HCl BP 4 mg.
heptadine or drugs with similar chemical struc- carefully, while standing or sitting,
OTC APITOL® (Mecure) Pack: 2 x 10’s.
ture; concurrent use with MAOIs; glaucoma; Tablet, Cyproheptadine 4 mg; white tab. bend your head, instil drops in each
nostril and hold your head back a 60 mg – 10’s (in blisters) dine derivative, structurally related to azata- Syrup, Loratadine 1 mg per mL
few minutes to distribute the drugs 120 mg – 10’s; 100’s dine. It exhibits potent, long acting H1-anti- Pack: 30 mL
throughout the nose. 180 mg – 10’s. thistamine activity with no central sedative OTC LORATYN® (Hovid)
OTC VIBROCIL® (Novartis) OTC FEXIDINE® (Strides Vital) or anticholinergic effects. In man, nasal and Tablet, Loratadine 10 mg
Nasal drops, Dimethindene maleate 0.025%, Phe- Tablets, Fexofenadine 120 mg, 180 mg. other signs and symptoms of allergic rhinitis 10 mg – 2 x 10’s; 10 x 10’s (in blisters); 100’s; 500’s
nylephrine 0.25%. 120 mg – 1 x 10’s are relieved rapidly after oral administration. (in bottle)
Pack: 10 ml bottle 180 mg – 1 x 10’s. Indications: Relief of symptoms associated OTC LORAX® (Al-Tinez)
with seasonal and perennia allergic rhinitis Tablet, Loratadine 10 mg; uncoated tab
FEXOFENADINE LEVOCETIRIZINE such as sneezing, nasal discharge and itching 10 mg – 10’s (in blisters)
Therapeutic category: Antihistamine, H 1 Therapeutic category: Antihistamine and ocular itching and burning; for the relief of Syrup, Loratadine 5 mg per 5 mL
Blocker, Non-sedating. Pharmacology: The 2nd generation H1 recep- symptoms associated with idiopathic chronic Pack: 100 mL
Pharmacology: Fexofenadine, a non-sedating tor antagonist Cetirizine consists of equal urticaria and other allergic dermatologic OTC LORFAST® (Interpharma)
H1 antihistamine, is an active metabolite of ter- quantities of two enantiomers, Levocetirizine disorders. Tablet, Loratidine 10 mg
fenadine. It competitively blocks the histamine (R-enantiomer) and Dextrocetirizine (S-enen- Contra-indications: Hypersensitivity to lorati- 10 mg – 3 x 10’s
H1-receptor on effector cells in the GIT, blood tiomer). Levocetirizine is the more active dine or other components of the preparation.
OTC LORINET® (Strides Vital)
vessels and respiratory tract; does not readily enantiomer, accounting for most of the clinical Precautions: Severe liver impairment; safety Tablet, Loratidine 10 mg.
cross the BBB, and so causes less drowsiness antihistaminic activity of racemic Cetirizine. It and efficacy in children below 2 years not es- 10 mg – 1 x 10’s.
than 1st-generation antihistamines. It is rapidly is rapidly and extensively absorbed, minimally tablished; pregnancy, nursing mothers.
metabolized in the liver and is excreted mainly OTC LOTIN® (Medreich)
absorbed following oral administration and is Interactions: Alcohol, erythromycin, keto-
Tablet, Loratidine 10 mg.
excreted mainly in the bile, about 10% being in urine with a half-life of 7-8 hours in adults. conazole, procarbazine, other anti-histamines. 10 mg – 2 x 10’s.
excreted unchanged in the urine. It does not Indications: Symptomatic treatment of allergic Adverse effects: Headache, fatigue, som- Syrup, Loratidine 5 mg per 5 mL.
EMDEX
undergo hepatic biotransformation. rhinitis and chronic urticaria. nolence, dry mouth, nasal dryness, dyspnea, Pack: 60 mL.
Indications: Relief of symptoms of allergic Contra-indications: Hypersensitivity to lev- palpitations, anxiety, depression; very rarely
ocetirizine, cetirizine or its parent compound OTC NECTADINE® (Nectar Healthcare)
rhinitis and chronic idiopathic urticaria. alopecia, anaphylaxis, abnormal hepatic func-
Chewable tablet, Loratidine 10 mg
Contra-indications: Hypersensitivity to any hydroxyzine and any other component of the tion and supraventricular tachyarrhythmias. 10 mg – 1 x 10’s; 10 x 10’s (in blisters)
component of the preparation. formulation. Dose: Adult & child (>12 years): 10 mg once
Precautions: Renal insufficiency, hepatic in- daily. Child (6-12 years or weight OTC RETIDINE®-10 (Vixa)
Precautions: Elderly; Renal & hepatic impair-
sufficiency, concurrent administration of CNS >30 kg), 10 mL once daily; 2-6 years Tablet, Loratadine 10 mg.
ment; Cardiovascular disease; Pregnancy & 10 mg – 10 x 10’s.
lactation; Children. depressants, patients with urinary retention, (weight <30 kg), 5 mL once daily; <2
Interactions: Co-administration with Erythro- bladder neck obstruction, or prostatic hyper- years, not recommended.
PROMETHAZINE
mycin or Ketoconazole may increase its plasma trophy, angle-closure glaucoma. Pregnancy,
OTC ALLGEST® (Canopus) Therapeutic category: Antihistamine, H 1
level (possibly due to increased GI absorption/ lactation. Tablet, Loratidine 10 mg
Interactions: Increased risk of drowsiness if Blocker; Antiemetic; Sedative.
decreased biliary excretion). Aluminium and 10 mg – 10 x 10’s
taken with alcohol; tricyclic antidepressants Pharmacology: Promethazine is a long-acting
Magnesium hydroxide containing antacids OTC ATADYN® (PharmacyPlus)
e.g. amitriptyline; narcotics e.g. morphine, antihistamine with additional anti-emetic
may reduce its GI absorption. May potenti- Tablet, Loratidine10 mg; uncoated tab.
codeine; benzodiazepines e.g. diazepam; se- effects.
ate the effects of anticholinergics and CNS 10 mg – 10’s (in blister)
dating antihistamines e.g. chlorpheniramine. Indications: Symptomatic treatment of allergic
depressants. Syrup, Loratidine 5 mg per 5 mL; yellow tab.
Adverse effects: Headache, abdominal pain, conditions of the respiratory tract and skin such
Adverse effects: Most commonly headache, Pack: 100 mL.
dry mouth, fatigue, inflammation of the throat as sensitisation reactions to drugs or foreign
drowsiness, nausea and dizziness. Rarely OTC LORAT® (Embassy)
(pharyngitis), sleepiness, weakeness or loss of proteins, anaphylactic reactions; prevention
fatigue, insomnia, nervousness and sleep Tablet, Loratidine 10 mg.
strenght (asthenic), migraine. and treatment of nausea and vomiting espe-
disorder. 10 mg – 10’s.
Dose: Adult and child >12 years, 5 mg once cially motion sickness.
Dose: By mouth, Adult & Children (>12
daily in the evening. OTC LORATADIN® (E-Globa) Contra-indications: Hypersensitivity to pro-
years), Seasonal allergic rhinitis, 120
Children aged 6-12 years: 5 mg once Tablet, Loratadine (micronized) 10 mg methazine or any component; narrow-angle
mg once daily. 10 mg – 10 x 10’s (in blisters)
daily in the evening glaucoma.
Chronic idiopathic urticaria, 180 mg
To be swallowed whole with liquid, OTC Loratidine (Afrab-Chem) Precautions: Pregnancy, road users.
once daily.
with or without food. Tablet, Loratadine 10 mg Contra-indications: Hypersensitivity to pro-
Children (<12 years): Not recom-
Not recommended for children <6 10 mg – 2 x 10’s; 10 x 10’s methazine or any component; narrow-angle
mended. Syrup, Loratidine 5 mg per 5 mL.
years. glaucoma.
Elderly: adult dose. Pack: 60 mL. Interactions: Alcohol, CNS depressants, MAOIs.
May be taken with or without food. OTC CERIZINE® (Apple Pharma)
OTC Loratidine (Crystal) Adverse effects: Drowsiness, dizziness, disori-
OTC FENODIN® (JB Pharma) Tablet, Levocetirizine dihydrochloride 5 mg; f-c tab.
Tablet, Loratidine 10 mg; uncoated tab entation, photosensitive skin reactions.
Tablet, Fexofenadine (as HCl) 120 mg. Pack: 10’s (in strips)
10 mg – 10’s (in blisters) Advice to patients: May cause drowsiness,
120 mg – 1 x 10’s (in blister) impair judgement and coordination; may
LORATIDINE OTC Loratidine (Neros)
OTC FEXET® (Zoomota) Tablet, Loratidine 10 mg. cause photosensitivity, sunscreening agent
Therapeutic category: Antihistamine, H 1
Tablet, Fexofenadine HCI 30 mg, 60 mg, 120 mg, 10 mg – 1 x 10`s. and protective clothing may be used; avoid
180 mg Blocker, Non-sedating.
excessive sunlight; notify physician of invol-
30 mg – 10’s (in blisters) Pharmacology: Loratadine is a cyprohepta- OTC Loratidine (Zeenat)
untary movements or feelings of restlessness.
318 | 8.2 Sympathomimetics 8.3 Corticosteroids | 319
Nursing considerations: Give with food or Pack: 100 mL routes of administration. phosphate), ADULT 0.5–24 mg; CHILD
milk to reduce GI distress; food may slightly OTC Promethazine (Gauze) Anaphylaxis, by IM or SC injection 200–400 µg/kg.
reduce absorption. Oral liquid, Promethazine HCI 5 mg per 5 mL of 1:1000 epinephrine injection, see POM Dexamethasone (WMF 3)
• Give IM deep into a large muscle mass and Pack: 100 mL; 2 L Steps in the Management of Anaphy- Injection, Dexamethasone phosphate (as disodium
rotate injection sites. Avoice S.C route. laxis for doses. salt) 4 mg/mL; in 1-mL ampoule.
OTC PROMEGAN® (Bond)
• IV dose must be diluted to a max. concentra- Elixir, Promethazine HCl 5 mg per 5 mL.
Anaphylaxis, by slow IV injection of
POM Dexamethasone (EDL 18.1)
tion of 25-50 mg/9 mL and infused at max. Pack: 100 mL 1:10 000 epinephrine injection. This
Injection, Dexamethasone (as sodium phosphate) 4
rate of 25 mg/2 minute. Rapid IV administra- route should be reserved for severely mg/mL; in 1-mL ampoule.
tion may cause a transient fall in BP. OTC PROTHAZIN® (Ranbaxy) ill patients when there is doubt about
Syrup, Promethazine HCl 5 mg per 5 mL. See the preparations under section 10.3
• Coffee or tea may reduce drowsiness; give the adequacy of circulation and
Pack: 100 mL.
chewing gum or ice chips to relieve dry absorption from the intramuscular
mouth. OTC ROPHEGAN® (May & Baker) site, see Steps in the Management of HYDROCORTISONE
Dose: By mouth, 25 mg at bedtime; Elixir, Promethazine HCl 5 mg per 5 mL. Anaphylaxis for doses. Indications: Adjunct in the emergency
increased to 50-75 mg at bedtime if Pack: 60 mL treatment of anaphylaxis; inflammatory skin
POM Epinephrine (WMF 3)
necessary. POM SIVOTZINE® (Adpharm) conditions (section 15.2); inflammatory bowel
Injection, Epinephrine (as HCl or hydrogen tartrate)
Allergy: 10-20 mg 2-3 times daily. Injection, Promethazine 50 mg per 2 mL. 1 mg/1 mL; in 1-mL ampoule.
disease (section 4.7); adrenocortical insuffi-
Child (6 months – 1 year): 5-10 mg Pack: 2 mL x 100’s ciency (section 10.3).
POM Epinephrine (EDL 15.1 & 18.1) Contra-indications: Not relevant to emer-
daily; 1-5 years, 5-15 mg daily; 5-10 POM ZATROX® (Vixa) Injection, Epinephrine (as acid tartrate or HCl) 1 mg gency use but for contra-indications relating
years, 10-25 mg daily; or the lower Injection, Promethazine (as HCl) 25 mg per mL; clear per mL (1 in 1000); in 1-mL amp.
dose twice daily. colourless solution in 2-mL amp. to long-term use see section 10.3.
By deep IM injection or slow IV injec- POM Adrenaline (Alpha) Precautions: Not relevant to emergency use
EMDEX
Injection, Epinephrine 1 mg per mL (1: 1000); clear but for precautions relating to long-term use
tion, see lit. 8.2 Sympathomimetics
colourless soln in colourless transparent 1-mL amp. see section 10.3.
OTC Promethazine (EDL 18.2) Pack: 10 x 10’s.
EPINEPHRINE Adverse effects: For adverse effects associated
Tablets, Promethazine HCl 10 mg, 25 mg.
Oral liquid, Promethazine HCl 5 mg per 5 mL. Synonym: Adrenaline with long-term corticosteroid treatment see
8.3 Corticosteroids section 10.3.
Injection, Promethazine HCl 25 mg per mL; in 1 mL, Indications: Severe anaphylactic reaction;
2 mL amps. severe angioedema; cardiac arrest (section 5.4). Dose: Anaphylaxis, by slow IV injection as a
DEXAMETHASONE single dose, see Steps in the Manage-
OTC AVOMAC® (Pacmai) Precautions: Hyperthyroidism, hypertension,
Indications: Adjunct in the emergency treatment of Anaphylaxis.
Tablet, Promethazine HCI 25 mg diabetes mellitus, heart disease, arrhythmias,
ment of anaphylaxis; short-term suppression
25 mg – 5 x 20’s (in blisters) cerebrovascular disease; second stage of labour; POM Hydrocortisone (WMF 3)
of inflammation in allergic disorders; for other
elderly INTERACTIONS: Severe anaphylaxis in Injection (Powder for injection), Hydrocortisone (as
OTC CEZINE® (Medreich) indications see section 10.3. sodium succinate) 100 mg; in vial.
Tablets, Promethazine (as HCl) 10 mg, 25 mg patients on non-cardioselective beta-blockers
Contra-indications: Untreated systemic
Syrup, Promethazine (as HCl) 5 mg per 5 mL for example propranolol, may not respond to POM Hydrocortisone (EDL 18.1)
infection (unless condition lifethreatening);
Pack: 60 mL; 100 mL. adrenaline injection calling for IV injection of Injection, Hydrocortisone (as sodium succinate) 100
administration of live virus vaccines.
salbutamol (section 7.1.1). Furthermore, adren- mg; powder for reconstitution in vial.
POM CIMAX® (Beta Drugs) Precautions: Increased susceptibility to and
aline may cause severe hypertension in those See the preparations under section 10.3
Injection, Promethazine HCl 50 mg; sterile solution severity of infection; activation or exacerbation
of Promethazine HCl in water for injections free receiving beta-blockers.
of tuberculosis, amoebiasis, strongyloidiasis;
from dissolved air. Patients on tricyclic antidepressants are consid- PREDNISOLONE
risk of severe chickenpox in non-immune
Pack: 2-mL x 100 amps. erably more susceptible to arrhythmias, calling
patient (varicella-zoster immunoglobulin Prednisolone is representative corticosteroid. Various
for a much reduced dose of adrenaline. Other
POM NOZIN® (Geneith) required if exposed to chickenpox); avoid drugs can serve as alternatives.
Injection, Promethazine 50 mg per 2 mL. interactions: see Appendix 1.
exposure to measles (normal immunoglobulin
Adverse effects: Tachycardia and arr-hyth- Indications: Short-term suppression of in-
POM PEMAMETH® (Pemason) possibly required if exposed); diabetes mellitus;
mias, hypertension, tremor, anxiety, sweating, flammation in allergic disorders; longerterm
Injection, Promethazine HCl 50 mg per 2 mL; in 2-mL peptic ulcer; hypertension; corneal perforation;
nausea, vomiting, weakness, hyperglycaemia, suppression (section 10.3); malignant disease
amp. marked “Pemameth injection” for further precautions relating to long-term
dizziness, pulmonary oedema have all been (section 12.2.2); eye (section 13.2).
Pack: 2-mL x 10 x 10’s use of corticosteroids see section 10.3.
reported; headache common. Contra-indications: Untreated systemic
OTC PHENERIL® (Vitabiotics) Adverse effects: Nausea, dyspepsia, malaise,
Nursing considerations: Read the labels to infection; administration of live virus vaccines.
Syrup, Promethazine HCl 5 mg hiccups; hypersensitivity reactions including
make sure you are using correct concentration, Precautions: Increased susceptibility to and
Pack: 60 mL. anaphylaxis; perineal irritation after intrave-
route and dosage. severity of infection; activation or exacerbation
nous administration; for adverse effects asso-
OTC Promethazine (Drugfield) • Shake before using; rotate IM/SC inj sites; of tuberculosis, amoebiasis, strongyloidiasis;
Syrup, Promethazine HCI 5 mg
ciated with long-term corticosteroid treatment
massage after injection. risk of severe chickenpox in non-immune
5 mg – 60 mL see section 10.3.
• Monitor injection site for tissue damage. patient (varicella–zoster immunoglobulin
Dose: Allergy (short-term use), by mouth,
OTC Promethazine (Emzor) • Warn patient to avoid the use of OTC Adren- required if exposed to chickenpox); avoid
ADULT usual range 0.5–10 mg daily as
Syrup, Promethazine HCl 5 mg per 5 mL. aline inhalation products; beta2-adrenergic exposure to measles (normal immunoglobulin
a single dose in the morning; CHILD
Pack: 60 mL; 100 mL; 2 L. agents for inhalation are preferred. possibly required if exposed); diabetes mellitus;
10–100 µg/kg daily.
OTC Promethazine (FAB) Dose: Caution: Different dilutions of epineph- peptic ulcer; hypertension; corneal perforation;
Anaphylaxis, by slow IV injection
Syrup, Promethazine (as HCl) 5 mL per 5 mg. rine injection are used for different for further precautions relating to long-term
or infusion (as dexamethasone
320 | 8.3 Corticosteroids
use of corticosteroids see section 10.3. ADULT and CHILD, initially up to
Adverse effects: Nausea, dyspepsia, malaise, 10–20 mg daily as a single dose in
hiccups; hypersensitivity reactions including the morning (in severe allergy up to
anaphylaxis; for adverse effects associated 60 mg daily as a short course of 5–10
with long-term corticosteroid treatment see days).
section 10.3. POM Prednisolone (WMF 3)
Dose: Allergy (short-term use), by mouth, Tablets, Prednisolone 5 mg, 25 mg.
EMDEX
9. Anti-infective drugs
9.1 Antibacterial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 323
9.1.1 Beta-lactam drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 323
9.1.1.1 Penicillins . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 324
9.1.1.2 Cefalosporins. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 346
9.1.1.3 Other beta-lactam antibacterials . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 365
9.1.2 Other antibacterials. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 367
9.1.2.1 Chloramphenicol. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 367
9.1.2.2 Quinolones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 369
9.1.2.3 Tetracyclines . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 382
9.1.2.4 Macrolides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 385
9.1.2.5 Aminoglycosides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 392
9.1.2.6 Nitroimidazoles. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 395
9.1.2.7 Nitrofurantoin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 397
9.1.2.8 Spectinomycin . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 397
9.1.2.9 Sulfonamides and trimethoprim. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 398
EMDEX
9.1.2.10 Lincosamides . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 404
9.1.2.11 Vancomycin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 406
9.1.2.12 Furazolidone. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 407
9.1.3 Antileprosy drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 407
9.1.4 Antituberculosis drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 410
9.2 Systemic antifungal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 418
9.3 Antiprotozoal drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
9.3.1 Antimalarial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 427
9.3.1.1 Artemisinin-based combination therapies (ACTs). . . . . . . . . . . . . . . . . . . . 428
9.3.1.2 Drugs for the treatment of severe malaria. . . . . . . . . . . . . . . . . . . . . . . . . . . 440
9.3.1.3 Agents for chemoprophylaxis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 444
9.3.1.4 Other antimalarial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 447
9.3.2 Antiamoebic, antigiardial and antitrichomonal drugs. . . . . . . . . . . . . . . . . . 452
9.3.3 Antileishmanial drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 458
9.3.4 Antitrypanosomal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 462
9.3.4.1 African trypanosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 462
9.3.4.2 American trypanosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 464
9.3.5 Antipneumocystosis and antitoxoplasmosis drugs. . . . . . . . . . . . . . . . . . . . 465
9.4 Anthelmintics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
9.4.1 Intestinal anthelmintics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
9.4.1.1 Cestode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 467
9.4.1.2 Intestinal nematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 471
9.1 Antibacterial drugs | 323
9.4.1.3 Tissue nematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 474 9.1 Antibacterial drugs should be avoided in children;
• Duration of therapy depends on the nature
9.4.2 Antifilarials. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 475 9.1.1 Beta-lactam drugs of the infection and the response to treatment.
9.4.2.1 Loiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 475 9.1.2 Other antibacterials Courses should not be unduly prolonged be-
9.1.3 Antileprosy drugs cause they encourage resistance, they may lead
9.4.2.2 Lymphatic filariasis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 476 9.1.4 Antituberculosis drugs. to side-effects and they are costly. However,
in certain infections such as tuberculosis or
9.4.2.3 Onchocerciasis . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 477 See EMDEX Vol. 3 for the detailed coverage of An- chronic osteomyelitis it is necessary to treat for
ti-infective Agents prolonged periods. Conversely a single dose
9.4.3 Trematode infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 478
of an antibacterial may cure uncomplicated
9.4.3.1 Schistosomiasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 478 Choice of a suitable antibacterial drug. urinary-tract infections.
Choice of an antibacterial drug is based on
9.4.3.2 Fluke infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 479 the identity of the likely pathogen and its Superinfection. In general, broad-spectrum
antibacterial sensitivity, and factors relating antibacterial drugs such as the cefalosporins
9.5 Antiviral drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 480 are more likely to be associated with adverse
to the patient (for example history of allergy,
9.5.1 Herpes and cytomegalovirus infections. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 480 renal and hepatic function, immune status, reactions related to the selection of resistant
severity of illness, ethnic origin, and age). organisms for example fungal infections or
9.5.2 Antiretroviral drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 482
antibiotic-associated colitis (pseudomem-
9.5.2.1 Nucleoside reverse transcriptase inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . 485 Antibacterial policy. Local policies often branous colitis); other problems associated
limit the availability of antibacterials to with superinfection include vaginitis and
9.5.2.2 Non-nucleoside reverse transcriptase inhibitors. . . . . . . . . . . . . . . . . . . . . 491 achieve reasonable economy consistent with pruritus ani.
9.5.2.3 Protease inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 493 adequate cover, and to reduce the develop-
ment of resistant organisms. A policy may
9.1.1 Beta-lactam drugs
EMDEX
9.5.2.4 Fixed-dose combinations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 496 allow a range of drugs for general use and
permit other drugs only on the advice of a 9.1.1.1 Penicillins
9.5.3 Other antivirals. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 498 9.1.1.2 Cephalosporins and imipenem with cilas-
microbiologist or physician responsible for
tatin
the control of infectious diseases.
Before starting therapy. The following should Beta-lactam drugs
be considered before starting antimicrobial Beta-lactam antibiotics including penicillins,
therapy: cefalosporins and carbapenems share a
• Viral infections should not be treated with anti- common structure; they are bactericidal,
bacterials. However, antibacterials are occasion- their mechanism of action resulting from
ally helpful in controlling secondary bacterial in- inhibition of peptidoglycan, a mucopeptide
fection (for example acute necrotising ulcerative in bacterial cell walls. Benzylpenicillin and
gingivitis secondary to herpes simplex infection);
phenoxymethylpenicillin are active against
• Where possible samples should be taken for cul-
ture and sensitivity testing; ‘blind’ antibacterial susceptible strains of Gram-positive bacteria
prescribing for unexplained pyrexia usually leads and Gram-negative bacteria, spirochaetes,
to further difficulty in establishing the diagnosis; and actinomycetes, but are inactivated by
• Knowledge of prevalent organisms and their penicillinase and other betalactamases.
current sensitivity is of great help in choosing an Benzathine benzylpenicillin and procaine
antibacterial before bacteriological confirmation benzylpenicillin are long-acting prepara-
is available; tions which slowly release benzylpenicillin on
• The dose of an antibacterial varies according to a injection. A range of penicillins with improved
number of factors including age, weight, hepatic
stability to gastric acid and penicillinases
function, renal function, and severity of infection.
The prescribing of the so-called ‘standard’ dose have been produced by substitution of the
in serious infections may result in failure of treat- 6-amino position of 6-aminopenicillanic
ment; therefore it is important to prescribe a dose acid. Cloxacillin is an isoxazoyl penicillin
appropriate to the condition. An inadequate dose which is resistant to staphylococcal peni-
may also increase the likelihood of antibacterial cillinase. Broad-spectrum penicillins such
resistance. On the other hand, for an antibacterial as ampicillin are acid-stable and active
with a narrow margin between the toxic and against Gram-positive and Gram-negative
therapeutic dose (e.g. an aminoglycoside) it is
bacteria, but are inactivated by penicillinase.
also important to avoid an excessive dose and
Beta-lactamase inhibitors such as clavulanic
the concentration of the drug in the plasma may
need to be monitored; acid are often necessary to provide activity
• The route of administration of an antibacterial against beta-lactamases produced by a wide
often depends on the severity of the infection. range of both Gram-negative and Gram-pos-
Life-threatening infections require intravenous itive bacteria.
therapy. Antibacterials that are well absorbed
Cefalosporins are classified by generation,
can be given by mouth even for some serious in-
fections. Whenever possible painful IM injections
with the first generation agents having
324 | 9.1.1.1 Penicillins 9.1.1.1 Penicillins | 325
Gram-positive and some Gram-negative therapeutic concentrations need to be sus- ited compared to benzylpenicillins. Cloxacillin co-amoxiclav than with amoxicillin alone and
activity; the second generation drugs have tained for several hours. Used mainly in the is more stable to staphylococcal β-lactamase the combination is contraindicated in patients
improved Gram-negative activity and the treatment of gonorrhea and syphilis, and in than Flucloxacillin. with a history of hepatic dysfunction associ-
third generation cefalosporins have a wider the follow-on treatment of patients requiring Following oral administration, Flucloxacillin ated with the drug.
spectrum of activity, although may be less prolonged therapy after initial treatment with is better absorbed and achieves mean peak Group 4: Penicillins active against P. aerug-
active against Gram-positive bacteria than first benzylpenicillin. They are also used in the plasma levels about twice those of Cloxacillin. inosa
generation drugs, but they are active against prophylaxis of rheumatic fever. Absorption is reduced when given with food.
Gram-negative Enterobacteriaceae and Pseu- Piperacillin is an acyl derivative of ampicillin
Intramuscular injection, particularly of ben- Flucloxacillin is also more slowly eliminated used mainly for its activity against Ps. aerugi-
domonas aeruginosa. zathine penicillin, may produce local pain than Cloxacillin. nosa. It is available in fixed combination with
Carbapenems are semisynthetic derivatives or tenderness, and accidental intravascular They are usually used in combination therapy β-lactamase inhibitor (i.e. Tazobactam). The
of Streptomyces cattleya. They have a broad injection of procaine penicillin may produce (e.g. Ampicillin plus Cloxacillin) in treating combination helps overcome the resistance
spectrum of activity and are stable to most acute agitation, hallucinations and collapse. infections involving susceptible Staph. aureus. due primarily to their hydrolysis by β-lacta-
penicillinases. They should be reserved for Procaine penicillin must not be given intra- mases found in many species of Enterobac-
severe infections resistant to other antibiotics. Group 4: Extended-Spectrum Penicillins
venously. Very severe and potentially fatal teriaceae.
reactions resembling those of anaphylactic Aminopenicillins have greater acid stability
9.1.1.1 Penicillins and enhanced activity against Gram-negative Both piperacillin and tazobactam are not orally
shock, but non-allergic in character, may oc- absorbed and usually administered IV. Clinical
The penicillins in clinical use may be divided cur, probably due to accidental entry into the bacteria compared to benzylpenicillins. The
aminopenicillins are acid stable and can be uses include uncomplicated and complicated
into six major groups: vascular system at the site of injection and skin and skin structure infection; postpartum
blockage of pulmonary and cerebral capillar- given orally. Ampicillin is the least well ab-
•Group 1: Benzylpenicillin and its long-acting sorbed, about one-third of the dose appearing endometritis or pelvic inflammatory disease;
parenteral forms e.g. Benzylpenicillin, Benza- ies by crystals of the suspension. Reactions community-acquired pneumonia (moderate
in the urine as active drug, and absorption is
EMDEX
thine penicillin and Procaine Penicillin. due to liberated procaine may include acute severity); nosocomial pneumonia (moderate
anxiety, hypertension, tachycardia, vomiting, further reduced by food. Amoxicillin, an ester
•Group 2: Orally absorbed penicillins similar to of ampicillin, is much better absorbed and not to severe); appendicitis and peritonitis.
audiovisual hallucinations and acute psychotic
benzylpenicillin e.g. Phenoxymethylpenicillin. disturbance. The most severe reactions may significantly affected by food, peak plasma Common side effects may include rash, pruri-
•Group 3: Penicillins that are relatively stable lead to convulsions and cardiac arrest. levels generally being at least twice those tus, and gastrointestinal effects. Pseudomem-
to staphylococcal β-lactamase, but which achieved by equivalent doses of ampicillin. branous colitis may also occur.
Group 2: Orally absorbed Penicillins resem- The aminopenicillins (e.g. Ampicillin) may be
have no useful activity against Gram-negative bling Benzylpenicillin Penicillins may cause encephalopathy due to
bacilli e.g. Cloxacillin, Flucloxacillin, Nafcillin. administered by parenteral routes, but the es- cerebral irritation. This rare, but serious adverse
Methicillin is no longer in use. Phenoxymethylpenicillin (aka Penicillin ters (e.g. Amoxicillin) are given by mouth only. effect may result from very high doses or in
V) is more acid stable than benzylpenicillin Amoxicillin has a spectrum of activity essen- severe renal failure. Penicillins should not be
•Group 4: Compounds with enhanced activity and is absorbed after oral administration,
against certain Gram-negative bacilli, including tially identical to that of ampicillin, but is bac- given by intrathecal injection because they
producing therapeutically useful plasma pen- tericidal to susceptible Gram-negative bacilli can cause encephalopathy which may be fatal.
many enterobacteria and Haemophilus influ- icillin concentrations. Absorption is better after
enzae, but which are inactivated by staphylo- at rather lower concentrations. Amoxicillin HYPERSENSITIVITY
administration in the fasting state. It exhibits with its superior absorption characteristics has
coccal and many enterobacterial β-lactamases. lower activity than benzylpenicillin against The most important adverse effect of penicil-
Examples include the aminopenicillins such as largely displaced ampicillin for oral therapy,
Gram-positive cocci and are distinctly less except against the enterococci. Amoxicillin lins is hypersensitivity which causes rashes and,
ampicillin and amoxicillin. active against Gram-negative bacteria. Group occasionally anaphylaxis, which can be fatal. A
is preferred to ampicillin for the treatment of
•Group 5: Penicillins active against Pseu- 2 penicillins lack stability to β-lactamase. some infections including otitis media and careful history should be taken with regard to
domonas aeruginosa. Examples include the Phenoxymethylpenicillin may be prescribed for respiratory-tract and urinary-tract infections. previous allergic reactions. If rash develops,
carboxypenicillins such as Piperacillin. many indications for which benzylpenicillin is another antimicrobial should be substituted.
Oral ampicillin commonly cause gastrointesti- Allergic reactions to penicillins occur in 1–10%
•Group 6: Penicillins resistant to enterobacterial suitable, including streptococcal pharyngitis nal side effects while the ester (i.e. Amoxicillin)
β-lactamase. Temocillin is currently the only and skin sepsis, but is not recommended for of exposed individuals, while anaphylactic re-
is more likely to cause upper abdominal actions occur in fewer than 0.05% of treated pa-
member of this group (not available in Nigeria). initial therapy of serious infections. This is discomfort, nausea and vomiting. Amoxicillin,
due to the unpredictable oral absorption and tients. Individuals with a history of anaphylaxis,
Group 1: Benzylpenicillin and its Long-Act- being better absorbed, is less likely to cause di- urticaria, or rash immediately after penicillin
ing Parenteral Forms variability in plasma concentrations. It is not arrhea. Taking amoxicillin with food will reduce
appropriate for infections caused by H. influ- administration are at risk of immediate hy-
Benzylpenicillin (aka Penicilli G), the first nat- the incidence of upper abdominal symptoms. persensitivity to a penicillin. These individuals
enzae or Gram-negative bacteria, and is not
urally produced penicillin, is poorly absorbed recommended for the treatment of gonorrhea, Amoxicillin-clavulanic acid combination – should not receive a penicillin, a cefalosporin
orally and must be given by injection. It is still a syphilis or leptospirosis. Clavulanic acid is a beta-lactamase inhibitor. or another beta-lactam antibiotic. Patients who
useful antibiotic but is inactivated by bacterial It has no significant antibacterial activity but are allergic to one penicillin will be allergic to
beta-lactamases. Because the plasma half-life Group 3: Antistaphylococcal β-Lactama- in combination with amoxicillin widens amox- them all because the hypersensitivity is related
is short, insoluble salts of penicillin were pre- se-Stable icillin’s spectrum of activity and allows its use to the basic penicillin structure and about 10%
pared that act as intramuscular depots for the They possess improved activity against pen- against amoxicillin-resistant strains of bacteria. of penicillin-sensitive patients will be allergic
release of penicillin into the bloodstream e.g. icillinase-producing strains of Staph. aureus. It is used in respiratory tract, genito-urinary and to cefalosporins and other beta-lactams.
procaine penicillin and benzathine penicillin. They are acid-stable and may therefore be abdominal infections, cellulitis, animal bites, Individuals with a history of a minor rash (a
Benzathine penicillin and Procaine pen- given by mouth as well as by injection. Their and dental infections. non-confluent rash restricted to a small area
icillin – Depot preparations are used when microbiological activity profile is however lim- Cholestatic jaundice is more common with of the body) or a rash occurring more than
72 hours after penicillin administration are and sensitivity before the first dose (therapy Capsule, Amoxicillin (as trihydrate) 250 mg. for reconstitution.
possibly not allergic to penicillin and in these may begin pending test results); ensure patient Powder for oral liquid, Amoxicillin (as trihydrate) 125 Pack: 60 mL.
individuals a penicillin should not be withheld is not allergic to penicillins. mg per 5 mL.
POM Amoxicillin (Greenlife)
unnecessarily for a serious infection; however, • Give with food to prevent GI distress; administer Injection, Amoxicillin (as sodium salt) 250 mg, 500
Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg
around-the-clock (in equal interval) rather than mg; powder in vials.
the possibility of an allergic reaction should be 250 mg – 10 x 10’s
borne in mind and facilities should be available 3 times/day to promote less variation in peak POM AMONEX® (Vixa) 500 mg – 10 x 10’s
and trough serum levels. Shake suspension well Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg
for treating anaphylaxis. POM AMOXYNOVA® (SKG)
before each dose. 250 mg – 10 x 10’s; 1000’s.
References: • Monitor closely for signs of superinfection espe- Capsule, Amoxicillin (as trihydrate) 250 mg.
500 mg – 10 x 10’s; 1000’s.
1) Bush K. β-lactam antibiotics: penicillins. In: cially with large doses and prolonged therapy. 250 mg – 10 x 10’s.
Syrup, Amoxicillin (as trihydrate) 125 mg per 5 mL.
Finch RG, Greenwood D, Norrby SR, Whit- • Advise patient to report immediately if rash, fever, Suspension, Amoxicillin 125 mg per 5 mL; dry powder
Pack: 60 mL; 100 mL.
or chills occur. Rash is the most common allergic for reconstitution.
ley RJ, eds. Antibiotic and chemotherapy. Injection, Amoxicillin (as trihydrate) 1000 mg; in vial.
9th ed. Available from: www.clinicalkey. reaction. Pack: 10’s; 25’s; 50’s. POM Apo-Amoxi (Lahams)
• Advise patient to report diarrhoea; may be symp- Capsules, Amoxicillin trihydrate 250 mg (scarlet and
com (login required) POM AMOVIN® (Evans)
tom of pseudomembranous colitis which can be gold no.2 capsule marked ‘APO 250’); 500 mg (scarlet
life-threatening. Tablets, Amoxicillin/Clavulanic.
AMOXICILLIN and gold no.2 capsule marked ‘APO 500’).
Dose: Infections due to sensitive organisms, 375 mg – 20’s.
250 mg – 100’s.
Synonym: Amoxycillin 625 mg – 14’s.
by mouth, ADULT and CHILD over 10 500 mg – 100’s.
Therapeutic category: Penicillin antibiotic. Suspension, Amoxicillin/Clavulanic 228.5 mg per
years, 250 mg every 8 hours, doubled 5 mL
Powder for oral suspension, Amoxicillin trihydrate 125
Indications: Urinary-tract infections, upper in severe infections; CHILD up to 10 mg/5 mL, 250 mg/5 mL.
Injection, Amoxicillin/Clavulanic 600 mg; powder
respiratory-tract infections, bronchitis; pneu- years, 125 mg every 8 hours, doubled for injection in vials.
Pack: 100 mL.
monia; otitis media; dental abscess and other in severe infections. POM AVROMOX® (Avro)
oral infections; osteomyelitis; Lyme disease; POM AMOXICAP® (Hovid)
EMDEX
Severe or recurrent purulent respirato- Suspension, Amoxicillin 125 mg per 5 mL; dry powder
endocarditis prophylaxis; post-splenectomy Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg
ry-tract infections, by mouth, ADULT 3 250 mg – 10 x 10 (blister)
for reconstition.
prophylaxis; gynaecological infections; gonor- g every 12 hours 500 mg – 10 x 10 (blister) POM BARBIMOX® (Juhel)
rhoea; Helicobacter pylori eradication (section Pneumonia, by mouth, ADULT 0.5–1 g Capsule, Amoxicillin 500 mg.
4.1); anthrax. every 8 hours. POM AMOXIGRAN® (Hovid)
Syrup, Amoxicillin (as tryhydrate) 125 mg per 5 mL;
Contra-indications: Hypersensitivity to peni- Suspension, Amoxicillin (as trihydrate) 125 mg per
Dental abscess (short course), by dry powder for reconstitution.
cillins (see notes above). 5 mL, 250 mg per 5 mL; granules for reconstitution.
mouth, ADULT 3 g repeated once 125 mg/5 mL – 100 mL Pack: 100 mL.
Precautions: History of allergy (see notes after 8 hours. 250 mg/5 mL – 100 mL POM BAXIME® (Bakangizo)
above); renal impairment (Appendix 4); ery- Urinary-tract infections (short course),
POM AMOXIL® (GSK) Capsule, Amoxicillin 500 mg
thematous rashes common in glandular fever, by mouth, ADULT 3 g repeated once
Capsule, Amoxicillin (as trihydrate) 250 mg; maroon/ 500 mg – 10 x 10’s (in blisters)
cytomegalovirus infection, chronic lymphatic after 10–12 hours. Suspension, Amoxicillin 250 mg per 5 mL
gold cap. marked with cap name and strength.
leukaemia, and possibly HIV infection; maintain Uncomplicated genital chlamydial Pack: 60 mL; 100 mL
250 mg – 16; 100.
adequate hydration with high doses (risk of infection, non-gonococcal urethritis, Syrup, Amoxicillin (as trihydrate) 125 mg per 5 POM BENMOXYL® (Nichben)
crystalluria); pregnancy and breastfeeding by mouth, 500 mg every 8 hours for mL in a sucrose-free sorbitol base; powder for Capsule, Amoxycillin (trihydrate) 500 mg.
(Appendices 2 and 3); interactions: Appendix 1. 7 days. reconstitution. 500 mg – 10 x 10’s (in blisters).
Adverse effects: Nausea and vomiting, Gonorrhoea (short course), by mouth, Pack: 100 mL. Suspension, Amoxicillin (as trihydrate) 125 mg per 5
diarrhoea; rashes (hypersensitivity or toxic ADULT 3 g as a single dose (with Injection, Amoxicillin (as sodium salt) 250 mg, 500 mL; powder for reconstitution.
response; may be serious reaction—discon- probenecid 1 g). mg; powder in vials. Pack: 100 mL.
tinue treatment); hypersensitivity reactions 250 mg – 10
Otitis media, by mouth, ADULT 1 g POM BG CLAV® (BG Pharma)
including urticaria, angioedema, anaphylaxis, 500 mg – 10.
every 8 hours; CHILD 40 mg/kg daily Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic
serum sickness-like reactions, haemolytic in 3 divided doses (maximum 3 g POM AMOXITAB® (Hovid) acid (as clavulanate potassium) 125 mg; f-c tab.
anaemia, interstitial nephritis (see also notes daily) Tablet, Amoxicillin (as trihydrate) 125 mg; flavoured 625 mg – 10’s; 7’s (in blisters)
above); rarely, antibiotic-associated colitis; Note: Except for gonorrhoea and for other short- tab.
125 mg – 100; 1000; 10 x 10 (blister). POM BLISCLAV 625® (Carebliss)
neutropenia, thrombocytopenia, coagulation course therapies, treatment should be continued
Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic
disorders; rarely, CNS disorders including for a minimum of 48-72 hours after patient becomes POM Amoxicillin (Afrab-Chem) acid (as clavulanate potassium) 125 mg.
convulsions associated with high doses or asymptomatic or evidence of bacterial eradication Suspension, Amoxicillin (as trihydrate) 125 mg Pack: 2 x 7’s
impaired renal function. has been obtained. In stuborn or severe infections, per 5 mL, 250 mg per 5 mL; dry powder for oral
large doses and prolonged therapy may be required. reconstitution POM CIKAMOX® (Michelle Lab).
Advice to patients: Report diarrhoea promptly;
A minimum of 10 days of treatment is recommended 125 mg/5 mL – 100 mL. Capsule, Amoxicillin (as trihydrate) 250 mg, 500 mg
entire course of medication (10-14 days) should for any infection caused by haemolytic streptococci 250 mg – 100’s; 10 x 10’s (in blisters)
be taken to ensure eradication of organism; 250 mg/5 mL – 100 mL.
to prevent the occurrence of acute rheumatic fever 500 mg – 100’s; 10 x10’s (in blisters)
should be taken in equal intervals around- or glomerulonephritis. POM Amoxicillin (Drugfield) Suspension, Amoxicillin (as trihydrate) 125 mg per 5
the-clock to maintain adequate blood levels; Capsule, Amoxicillin 250 mg. mL; dry powder for reconstitution.
POM Amoxicillin (WMF 6.2.1) Syrup, Amoxicillin 125 mg per 5 mL; dry powder for
may interfere with oral contraceptives; females Pack: 1 x 100 mL
Capsules/tablets, Amoxicillin (anhydrous) 250 mg, reconstitution.
should report symptoms of vaginitis; paediat- 500 mg. POM CIMOXIL® (Jubilee)
ric drops may be placed on child’s tongue or Oral liquid, Amoxicillin (anhydrous) 125 mg/5 mL; POM Amoxicillin (Emzor) Capsule (250 mg), Amoxicillin (as trihydrate) 250 mg;
added to formula, milk, etc. powder for reconstitution. Capsule, Amoxicillin 250 mg. maroon/maroon cap. marked ‘CIMOXIL 250’.
Nursing action: Obtain specimens for culture Suspension, Amoxicillin 125 mg per 5 mL; dry powder 250 mg – 15’s; 100’s; 500’s; 1000’s.
POM Amoxicillin (EDL 5.3)
Capsule (500 mg), Amoxicillin (as trihydrate) 500 mg; POM IPCAMOX® (IPCA) Suspension, Amoxicillin 125 mg, 250 mg per 5 mL. crystalluria); hepatic impairment (Appendix
maroon/maroon cap. marked ‘CIMOXIL 500’. Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg Pack: 60 mL; 100 mL. 5); pregnancy (Appendix 2); breastfeeding
500 mg – 15’s; 100’s. 250 mg – 10’s; 500’s; 1000’s. (Appendix 3); interactions: Appendix 1.
POM REICHAMOX® (Medreich)
Powder for oral suspension, Amoxicillin trihydrate 500 mg – 10’s; 500’s; 1000’s. Adverse effects: Nausea and vomiting,
Capsules, Amoxicillin 250 mg, 500 mg.
equiv. to 125 mg, 250 mg per 5 mL; off-white, crys- Syrup, Amoxicillin (as tryhydrate) BP 125 mg per 5
Syrup, Amoxicillin 125 mg per 5ml; dry powder for diarrhoea; rashes (hypersensitivity or toxic
talline powder which produces a yellow suspension mL; dry powder for reconstitution.
reconstitution. response—may be serious, discontinue treat-
with a fruity odour on reconstitution. Pack: 60 mL; 100 mL.
Syrup (forte), Amoxicillin 250 mg per 5ml; dry powder ment); hypersensitivity reactions including
Pack: 100 mL in glass bottle.
POM JAWAMOX® (Jawa) for reconstitution. urticaria, angioedema, anaphylaxis, serum
POM CP-CILLIN® (Crowther) Capsule, Amoxicillin 500 mg. Paediatric drops, Amoxicillin 125 mg per 1.25 mL; in
sickness-type reaction, haemolytic anaemia,
Injection, Amoxicillin 500 mg; dry powder for recon- 500 mg – 10 x 10’s. a glass bottle with plastic screw-on pipette.
stitution + WFI as diluent. Syrup, Amoxicillin 125 mg per 5 mL; dry powder for
interstitial nephritis (see also notes above);
POM SOLAMOX® IM / IV (Solution Pharma) rarely, antibiotic-associated colitis; neutrope-
Pack: 10 x 1’s reconstitution.
Injection, Amoxicillin (as trihydrate) 500 mg. nia, thrombocytopenia, coagulation disorders;
Pack: 100 mL.
POM DRAMOXILIN® (Drugfield) dizziness, headache, convulsions (particularly
POM SUMOX® (Superior)
Capsule, Amoxycillin (as trihydrate) 250 mg, 500 mg POM LAMOX® (Mecure)
Capsule, Amoxicillin trihydrate 500 mg with high doses or in renal impairment); hep-
250 mg – 10 x 10’s (in blisters) 500’s (in bulk) Capsule, Amoxicillin 500 mg; yellow/maroon capsule
500 mg – 10 x 10’s (in blisters) 500’s (in bulk) marked ‘LAMOX’.
Injection, Amoxicillin 500 mg atitis, cholestatic jaundice; Stevens-Johnson
Dry suspension, Amoxycillin (as trihydrate) 125 mg 500 mg – 2 x 10’s; 10 x 10’s. POM THAMOXILL® (Therapeutic) syndrome, toxic epidermal necrolysis, exfolia-
per 5 mL; dry powder for oral reconstitution. Suspension, Amoxicillin 125 mg per 5 mL; dry powder Suspension, Amoxicillin 125 mg per 5 mL. tive dermatitis, vasculitis reported; superficial
Pack: 100 mL for reconstitution. staining of teeth with suspension; phlebitis at
POM TRIMOX® (Elbe)
Pack: 100 mL injection site.
POM DRIMOX® (Fidson) Capsule, Amoxicillin 500 mg.
Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg POM MAXMOX® (GoldMoore) Advice to patients: See also under Amoxicillin.
250 mg – 10 x 10. Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg POM VITAMOX® (Strides Vital) Nursing action: Two 250 mg tablets are not
EMDEX
500 mg – 10 x 10. 250 mg – 10 x 10’s. Capsules, Amoxicillin (as trihydrate) 250 mg, 500 equivalent to one 500 mg tablet (both tablet
Syrup, Amoxicillin 125 mg per 5 mL; dry powder for 500 mg – 10 x 10’s. mg; maroon/yellow caps marked with brand name sizes contain equivalent clavulanate, i.e., 125
reconstitution. and strength.
POM MD-Amoxicillin (O’Nell)
mg); potassium content: 0.16 mEq of potas-
Pack: 60 mL; 100 mL. 250 mg – 10 x 10’s.
Suspension, Amoxicillin (as trihydrate) 125 mg per 5 500 mg – 10 x 10’s. sium per 31.25 mg of clavulanic acid.
POM EMBAMOX® (Embassy) mL; dry powder for reconstitution. • See also under Amoxicillin.
Injection, Amoxicillin sodium equiv. to Amoxicillin Pack: 100 mL POM WINPEN® (Interpharma) Dose: NOTE. All doses expressed as amoxicillin.
500 mg; in a vial. Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg Infections due to susceptible be-
POM MIRAMOX® (Miraflash) 250 mg – 10 x 10’s.
Pack: 50’s (in vials). ta-lactamase producing organisms,
Suspension, Amoxicillin (as trihydrate) 125 mg per 500 mg – 10 x 10’s.
POM EMMOX® (Emzor) 5 mL. by mouth, ADULT and CHILD over 12
Suspension, Amoxicillin 125 mg per 5 mL; dry powder
Capsule, Amoxicillin trihydrate 500 mg. Pack: 100 mL for reconstitution. years, 250 mg every 8 hours, doubled
Pack: 10 x 10’s (in blisters). Pack: 100 mL. in severe infections; CHILD under
POM MOXACEN® (Elbe) 1 year, 20 mg/kg daily in 3 divided
Suspension, Amoxicillin trihydrate 125 mg/5 mL,
Capsule, Amoxicillin 500 mg. POM ZIMAMAOX® (Gauze)
250 mg/5 mL. doses; 1–6 years, 125 mg every 8
Pack: 100 mL bottle. Oral dry syrup, Amoxicillin trihydrate 125 mg per
POM MOXYCARE® (Dizpharm) hours; 6–12 years, 250 mg every 8
5 mL
Suspension, Amoxicillin (as trihydrate) 125 mg per hours.
POM FABMOX® (FAB) Pack: 100 mL
5 mL. Severe dental infections, by mouth,
Syrup, Amoxicillin 125 mg per 5 mL.
Pack: 100 mL.
AMOXICILLIN plus CLAVULANIC ACID ADULT 250 mg every 8 hours for 5
POM FLOXIMOX® (Evans)
Capsule, Amoxicillin 500 mg.
POM NEOMOX® (Mopson)
Synonym: Co-amoxiclav. days.
Capsule, Amoxycillin (as trihydrate) 250 mg Infections due to susceptible be-
500 mg – 100’s.
250 mg – 10 x 10’s Therapeutic category: Penicillin antibiotic.
Indications: Infections due to beta-lactamase ta-lactamase producing organisms, by
POM FRAXYL® (Embassy) Powder for oral suspension, Amoxycillin (as trihydrate) IV injection over 3–4 minutes, ADULT
Capsules, Amoxicillin 250 mg, 500 mg. 125 mg per 5 mL. producing bacteria (where amoxicillin alone
not appropriate) including respiratory-tract and CHILD over 12 years, 1 g every 8
250 mg – 100’s. Pack: 100 mL
500 mg – 100’s. infections, otitis media, genito-urinary and hours, increased to 1 g every 6 hours
POM NOXIL® (Geneith) in severe infections; NEONATE and
Suspension, Amoxicillin 125 mg per 5 mL. abdominal infections, cellulitis, animal bites,
Capsule, Amoxicillin 500 mg. PREMATURE INFANT 25 mg/kg every
Pack: 100 mL. severe dental infections, Haemophilus influ-
500 mg – 10’s (in blister). 12 hours; INFANT up to 3 months, 25
POM GLOMOXYL® (Hochiez) Injection, Amoxicillin sodium equiv. to Amoxicillin enzae osteomyelitis, and surgical prophylaxis.
Contra-indications: Hypersensitivity to pen- mg/kg every 8 hours; CHILD 3 months
Capsule, Amoxicillin (as trihydrate) 500 mg 250 mg, 500 mg; powder for reconstitution in vials
500 mg – 10 x 10’s. 250 mg – 10’s with WFI icillins (see notes above); history of penicillin to 12 years, 25 mg/kg every 8 hours
500 mg – 10’s with WFI – or amoxicillin with clavulanic acid-associated increased to 25 mg/kg every 6 hours
POM HOSPIMOX® (Afrab-Chem) in more severe infections.
Syrup (125 mg/5 mL), Amoxicillin trihydrate equiv. POM PEMOXIL® (Pemason) jaundice or hepatic dysfunction.
Precautions: History of allergy (see notes Surgical prophylaxis, by IV injection,
to: 125 mg Amoxicillin per 5 mL; dry powder for Injection, Amoxycillin sodium 500 mg per 5 mL;
oral syrup. water for injection. above); renal impairment (Appendix 4); ery- ADULT 1 g at induction, with up to
Pack: 100 mL bottle. thematous rashes common in glandular fever, 2–3 further doses of 1 g every 8 hours
POM RANOXYL® (Ranbaxy) if increased risk of infection.
Syrup (250 mg/5 mL), Amoxicillin trihydrate equiv. cytomegalovirus infection, chronic lymphatic
Capsules, Amoxicillin (as trihydrate) 250 mg, 500 mg Reconstitution and Administration: According to
to: 250 mg Amoxicillin per 5 mL; dry powder for leukaemia, and possibly HIV infection; maintain
250 mg – 10 x 10’s; 1000’s. manufacturer’s directions.
oral syrup.
500 mg – 10 x 10’s; 1000’s. adequate hydration with high doses (risk of
Pack: 100 mL bottle. See also under the proprietary preparations below.
POM Amoxicillin plus Clavulanic acid (WMF 6.2.1) Suspension, (156.25 mg/5 mL), Amoxicillin (as tab. to 2 years), 0.15 mL/kg twice daily; 2-6 years
Tablet, Amoxicillin 500 mg, clavulanic acid 125 mg trihydrate)125 mg, clavulanic acid (as potassium 625 mg – 3 x 5’s (in blisters). (13-21 kg), 2.5ml twice daily; 7-12 years (22-
salt) 31.25 mg per 5 mL; powder for reconstitution. 40 kg), 5 mL twice daily. Severe infections,
POM Amoxicillin plus Clavulanic acid (EDL 5.3) POM AUGULAB® (Embassy)
Pack: 100 mL. double the above doses.
Tablet/Capsule, Amoxicillin (as trihydrate) 250 mg, Suspension, Amoxicillin (as trihydrate) 200 mg,
Dose: By mouth, child (7-12 years), 10 mL 3 times Note: Not recommended for children under 2
Clavulanic acid (as potassium salt) 125 mg. Clavulanic acid (as clavulanate potassium) 28.5 mg;
daily; 2-7 years, 5ml 3 times daily; 9 months months old. To minimise potential gastrointestinal
Powder for oral liquid, Amoxicillin (as trihydrate) 125 dry powder for reconstitution
– 2 years, 2.5 mL 3 times daily before or with intolerance, administer at the start of a meal. Ab-
mg, clavulanic acid (as potassium salt) 31.25 mg. Pack: 100 mL.
meals. Exact children’s doses are based on sorption is optimised when taken at the start of a
Injection, (600 mg), Amoxicillin (as sodium salt) 500
b.wt., usually 20-40 mg/kg b.wt. per day di- POM AUGLOCEF® (Vixa) meal. Duration of therapy should be appropriate
mg, clavulanic acid (as potassium salt) 100 mg;
vided in 3 equal doses depending on sever- Tablet, Amoxicillin 500 mg, Clavulanate potassium to the indication and should not exceed 14 days
powder for injection in vial.
ity of infection. Treatment must not exceed 125 mg. without review.
Injection, (1.2 g), Amoxicillin 1 g, clavulanic acid 200
14 days without medical re-examination. Pack: 2 x 8’s.
mg; powder for injection in vial. POM AUGMEX® (Vitahealth)
Reconstitution: Shake well the bottle containing Tablet, Amoxicillin 250 mg, Clavulanate potassium
Tablet, Amoxicillin (as trihydrate) 500 mg, potassium
POM Amoxicillin plus Clavulanic Acid (Kayhelt) the powder, add 86 mL of water in two portions 125 mg.
clavulanate equiv. to clavulanic acid 125 mg; f-c tab
Tablet, Amoxicillin (as trihydrate) 250 mg, Diluted po- (or first to 2/3 and then to the mark) each time Pack: 3 x 8’s.
Pack: 14’s
tassium clavulanate equiv. to clavulanic acid 125 mg shaking well.
POM AUGLOCEF® (Vixa) Dry syrup, Amoxicillin (as trihydrate) 250 mg, Clavu-
Pack: 1 x 7 Suspension forte, (312.5 mg/5ml), Amoxicillin (as
Granules, (156.25 mg), Amoxicillin (as trihydrate) 125 lanic acid (as potassium clavulanate) 62.5 mg per 5
Oral suspension, (228.5 mg), Amoxicillin (as trihy- trihydrate) 250 mg, clavulanic acid (as potassium
mg, Clavulanic acid (as potassium) 31.25 mg mL; powder for reconstitution
drate) 200 mg, Diluted potassium clavulanate equiv. salt) 62.5 mg per 5ml; powder for reconstitution.
Pack: 100 mL
to clavulanic acid 28.5mg per 5 mL. Pack: 100 mL. POM AUGMENTIN® (GSK) Injection, Amoxicillin (as sodium salt) 1000 mg,
Pack: 100 mL Dose: By mouth, child (7-12 years), 5 mL 3 times daily; Tablet, (375 mg), Amoxicillin (as trihydrate) 250 mg, Clavulanic acid (as potassium clavulanate) 200
Oral suspension, (457 mg), Amoxicillin (as trihydrate) 2-7 years, 2.5 mL 3 times daily; 9 months – 2 clavulanic acid (as potassium salt)125 mg; white oval mg per vial.
400 mg, Diluted potassium clavulanate equiv. to years, use the normal suspension (156.25 f-c tab. marked ‘AUGMENTIN’ on one side. Pack: Class vials
EMDEX
clavulanic acid 57 mg per 5 mL. mg/5 mL Exact children’s doses are based Pack: 21.
Pack: 100 mL on b.wt., usually 20-40 mg/kg but per Dose: Mild to moderate infections, Adult and Child POM CALMENTINE® (Maydon)
day divided in 3 equal doses depending >12 years, 375 mg tab. 3 times a day; Severe Tablet, (375 mg), Amoxicillin (as trihydrate) 250
POM AMCLAVIN® (Seagreen) on the severity of infection. Treatment infections, 625 mg tab. 3 times a day or 2 375 mg, clavulanic acid (as potassium clavulanate) 125
Tablet, (375 mg), Amoxicillin (as trihydrate) 250 must not exceed 14 days without medical mg tabs 3 times a day. mg; f-c tab.
mg, Clavulanic acid (as clavulanate potassium) 125 re-examination. Suspension, (156 mg), Amoxicillin (as trihydrate) 125 Pack: 10’s.
mg; f-c tab. Reconstitution: Shake well the bottle containing mg, clavulanic acid (as potassium salt) 31.25 mg; Tablet, (625 mg), Amoxicillin (as trihydrate) 500
Tablet, (625 mg), Amoxicillin (as trihydrate) 500 the powder, add 85 mL of water in two portions sugar-free fruit flavoured powder for reconstitution mg, clavulanic acid (as potassium clavulanate) 125
mg, Clavulanic acid (as clavulanate potassium) 125 (or first to 2/3 and then to the mark) each time with aspartame. mg; f-c tab.
mg; f-c tab. shaking well. Pack: 100 mL. Pack: 7’s.
Suspension, (156.25 mg), Amoxicillin (as trihydrate) Suspension, (457 mg/5 mL), Amoxicillin 400 mg, Dose: Child: usually 25 mg/kg/day in divided doses Dry syrup,(228.5 mg/5 mL) Amoxicillin (as trihydrate)
125 mg, Clavulanic acid (as clavulanate potassium) Clavulanic acid 57 mg. every 8 hours as follows: Under 1 year (e.g., 200 mg, clavulanic acid (as potassium clavulanate)
31.25 mg per 5 mL Pack: 70 mL. 7.5 kg), 2 mL 3 times a day; 1-6 years (10-18 28.5 mg per 5 mL.
Suspension, (312.5 mg), Amoxicillin (as trihydrate) Injection, (600 mg), Amoxicillin 500 mg, clavulanic kg), 5 mL 3 times a day; over 6 years (18-40 Pack: 30 mL; 60 mL; 70 mL; 100 mL (in amber glass
250 mg, Clavulanic acid (as clavulanate potassium) acid 100 mg. kg), 10 mL 3 times a day. bottle).
62.5 mg per 5 mL Pack: 5’s. Injection, Amoxicillin (as sodium salt) 500 mg, clavu-
Injection, (1.2 g), Amoxicillin 1 g, clavulanic acid POM CHLODI® (Zolon)
POM AMOCLAVISOL® (Solution Pharma) lanic acid (as potassium salt) 100 mg; powder in vial.
200 mg. Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic
Tablet (625 mg), Amoxicillin 500 mg, Clavulanic
Pack: 5’s. POM AUGMENTIN® BD (GSK) acid (as potassium clavulanate) 125 mg; f-c tab.
acid 125 mg.
Tablet (625 mg), Amoxicillin (as trihydrate) 500 mg, Pack: 2 x 7’s (in blisters)
Pack: 2 x 8’s. POM AMOXCLAX® (Diamond Remedies) clavulanic acid (as potassium salt)125 mg; white oval
Injection, Amoxicillin 1000 mg, clavulanic acid Tablet, (1000 mg), Amoxicillin trihydrate equiv to POM CLAMOVID® (Hovid)
f-c tab. marked ‘AUGMENTIN’.
200 mg Amoxicillin (anhydrous) 875 mg, Clavulanic acid (as Tablet, (625 mg), Amoxycillin (as trihydrate) 500
Dose: Mild to moderate infections, Adult and Child
Pack: 1.2 g. clavulanate potassium) 125 mg. mg, clavulanic acid (as potassium clavulanate) 125
>12 years, 625 mg 2 times a day; Severe
Pack:2 x 7’s mg; oblong, white f-c tab with shadow convex face.
POM AMOCLAVISOL-S® (Solution Pharma) infections, 1 g tab. 2 times a day.
Tablet, (625 mg), Amoxicillin trihydrate equiv to Pack: 3 x 5’s (in blisters)
Powder for oral suspension, Amoxicillin (as trihydrate) Tablet (1 g), Amoxicillin (as trihydrate) 875 mg, clavu-
Amoxicillin (anhydrous) 500 mg, Clavulanic acid (as Granules, (156.25 mg), Amoxycillin (as trihydrate)
200 mg, Clavulanic acid (as potassium clavulanate) lanic acid (as potassium salt) 125 mg; white oval f-c
clavulanate potassium) 125 mg. 125 mg, clavulanic acid (as potassium clavulanate)
28.5 mg per 5 mL; white to yellowish white crystal- tab. marked AC either side of a break line on one
Pack:2 x 7’s 31.25 mg per 5 mL
line powder for reconstitution to an almost white to side and AC only on the other side.
Oral suspension, Amoxicillin (as trihydrate) 200 mg, Pack:100 mL
yellow homogenous susp. with a strawberry flavour. Dose: See under 625 mg tablet above.
Pack: 100 mL. Clavulanic acid (as clavulanate potassium) 28.50 Syrup (228 mg/5 mL), Amoxicillin (as trihydrate) 200 POM CLAMOXIN® (Greenlife)
mg per 5 mL. mg, clavulanic acid (as potassium salt) 28.5 mg per Dry powder for oral suspension ,(125 mg)Amoxi-
POM AMOKSIKLAV® (Taylek) Pack: 100 mL 5 mL; aspartame-containing powder for suspension. cillin (as trihydrate) 125 mg, clavulanate acid (as
Tablet, (375 mg), Amoxicillin (as trihydrate) 250 mg,
POM AQUACLAV® (Pinnacle) Dose: Mild to moderate infections, Child (2-6 years clavulanate potassium) 31.25 mg per 5 mL after
clavulanic acid (as potassium salt) 125 mg.
Tablet, Amoxicillin (as trihydrate) 500 mg, Diluted or 13-21 kg), 5 mL twice daily; 7-12 years (22- reconstitution.
375 mg – 15’s.
potassium clavulanate equiv. to Clavulanic acid 40 kg), 10ml twice daily. Severe infections, Pack: 60 mL; 100 mL.
Tablet, (625 mg), Amoxicillin (as trihydrate) 500 mg,
125 mg; f-c tab. double the above doses. Dry powder for oral suspension, (312.5 mg), Amox-
clavulanic acid (as potassium salt) 125 mg.
Pack: 14’s Syrup (457 mg/5 mL), Amoxicillin (as trihydrate) 400 icillin (as trihydrate) 250 mg, clavulanic acid (as
625 mg – 15’s.
mg, clavulanic acid (as potassium salt) 57 mg per 5 clavulanate potassium) 62.50 mg per 5 mL after
Tablet, (1 g), Amoxicillin 875 mg, Clavulanic acid POM AUGBACTAM® (Neros) mL; aspartame-containing powder for suspension. reconstitution.
125 mg. Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic Dose: Mild to moderate infections, Child (2 months Pack: 100 mL
1 g – 10’s. acid (as clavulanate potassium) 125 mg; film-coated
POM CLANEKSI® (Zoomota) reconstitution. side and ‘63’ on the reverse. Tablet, (625 mg), Amoxicillin (as trihydrate) 500
Injection (0.6 g), Amoxicillin 0.5 g, Clavulanic acid Pack: 30 mL; 60 mL; 75 mL; 100 mL. 375 mg – 5’s (in blisters) mg, Clavulanic acid (as clavulanate potassium) 125
100 mg. Suspension, (312.5 mg), Amoxicillin USP 250 mg, Tablet, (625 mg), Amoxicillin 500 mg, Clavulanic acid mg; f-c tab.
0.6 g – 6’s (in vial). clavulanic acid 62.5 mg per 5 mL; powder for 125 mg; white oval shaped f-c tab. marked ‘A’ on one Pack: 2 x 7’s
Injection (1.2 g), Amoxicillin 1 g, Clavulanic acid reconstitution. side and ‘64’ on the reverse. Oral suspension, (228.5 mg), Amoxicillin (as tri-
200 mg. Pack: 30 mL; 60 mL; 75 mL; 100 mL. 625 mg – 5’s (in blisters). hydrate) 200 mg, Clavulanic acid (as clavulanate
1.2 g – 6’s (in vial). Injection, (300 mg), Amoxicillin (as sodium salt) Ph. Caplet, (1000 mg), Amoxicillin 875 mg, Clavulanic potassium) 28.50 mg per 5 mL; dry powder for
Eur. 250 mg, clavulanic acid (as potassium salt) USP acid 125 mg; white f-c scored caplet marked ‘A’ on reconstitution.
POM CLAVATIN® (SKG)
50 mg; powder in vial. one side and ‘65’ on the reverse. Pack: 100 mL
Suspension, (228.5 mg/5 mL), Amoxicillin 200 mg,
300 mg – 5 mL vial 1000 mg – 5’s (in blisters).
Clavulanic acid (as the K+ Salt) 28.5 mg per 5 mL; POM NOSCLAV® (Geneith)
Injection, (1.2 g), Amoxicillin (as sodium salt) Ph. Eur.
white, flavoured powder for reconstitution. POM KOPLIMENTINE® (E-Globa) Tablet, (375 mg), Amoxicillin 250 mg, clavulanic
1 g, clavulanic acid (as potassium salt) USP 200 mg;
Pack: 100 mL in amber bootle. Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic acid 125 mg.
powder in vial.
acid (as potassium salt) 125 mg; white f-c tab. 375 mg – 21’s
POM CLAVICIN® (Strides Vital) 1.2 g – 20 mL vial
625 mg – 3 x 4’s. Tablet, (625 mg), Amoxicillin 500 mg, clavulanic
Injection, (600 mg), Amoxicillin 500 mg, Clavulanic
POM FLEMING® (Medreich) acid 125 mg.
acid 100 mg. POM LOXACLAV® (May & Baker)
Tablet, (375 mg), Amoxycillin (as trihydrate) 250 mg, 625 mg – 2 x 7’s
Pack: 1 g vial. Caplet, (375 mg), Amoxicillin (as trihydrate) 250 mg,
Clavulanic acid (as potassium clavulanate) 125 mg. Dry syrup, (156.25), Amoxicillin (as trihydrate) 125
Injection, (1.2 g), Amoxicillin 1000 mg, Clavulanic clavulanic acid (as clavulanate potassium) 125 mg;
375 mg – 2 x 10’s; 10 x 10’s. mg, Clavulanic acid (as clavulanate potassium)
acid 200 mg. caplet marked “MBN” and “375”.
Tablet, (625 mg), Amoxycillin (as trihydrate) 500 mg, 31.25 mg per 5 mL
Pack: 1 g vial. 375 mg – 20’s.
Clavulanic acid (as potassium clavulanate) 125 mg; Dry syrup, (228.5 mg), Amoxicillin (as trihydrate)
Caplet, (625 mg), Amoxicillin (as trihydrate) 500 mg,
POM CLAXY® (Global Organics) white oval f-c tab. 200 mg, Clavulanic acid (as clavulanate potassium)
Clavulanic acid (as clavulanate potassium) 125 mg;
Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic 625 mg – 2 x 10’s; 10 x 10’s. 28.5 mg per 5 mL.
white f-c caplet marked “MBN” and “625”.
acid (as clavulanate potassium) 125 mg; f-c tab Suspension, (156 mg/5 mL), Amoxycillin (as tri- Injection, (600 mg), Amoxicillin 500 mg, Clavulanic
EMDEX
625 mg – 3 x 4’s.
Pack: 2 x 7’s (in blisters) hydrate) 125 mg, Clavulanic acid (as potassium acid 100 mg; powder in vial
Suspension, (156 mg/5 mL), Amoxicillin (as tri-
clavulanate) 31.25 mg per 5 mL. Pack: 10’s with 10 mL sterile water for injection.
POM DAFRACLAV® (Dafra) hy-drate) 125 mg, Clavulanic acid (as clavulanate
Pack: 100 mL. Injection, (1.2 mg), Amoxicillin 1000 mg, clavulanic
Tablet, Amoxicillin (as trihydrate) 500 mg, Potassium potassium) 31.5 mg per 5 mL; dry granules for
Suspension, (228.5 mg/5 mL), Amoxycillin (as acid 200 mg; powder in vial.
clavulanate equiv to Clavulanic acid 125 mg; white reconstitution.
trihydrate) 200 mg, Clavulanic acid (as potassium Pack: 10’s with 20 mL WFI.
f-c tab. Pack: 100 mL.
clavulanate) 28.5 mg per 5 mL.
Pack: 2 x 10’s; 3 x 15’s (in blisters). Suspension, (228 mg/5 mL), Amoxicillin (as tri- POM NOVAMENTINE® (Micronova)
Pack: 70 mL.
Powder for oral suspension, Amoxicillin trihydrate hy-drate) 200 mg, Clavulanic acid (as clavulanate Tablet, (375 mg), Amoxicillin (as trihydrate) 250 mg,
Injection, (600 mg), Amoxycillin (as sodium salt) 500
equiv. to Amoxicillin 400 or 200 mg, Potassium potassium) 28.5 mg per 5 mL; dry granules for Potassium clavulanate equiv. to Clavulanic acid
mg, Clavulanic acid (as potassium clavulanate) 100
clavulanate equiv. to Clavulanic acid 57 or 28 mg. reconstitution. 125 mg; f-c tab.
mg; sterile powder for reconstitution in vials.
Pack: 70 mL bottle. Pack: 70 mL. Pack: 10’s
Injection, (1.2 g), Amoxycillin (as sodium salt) 1 g,
Tablet, (625 mg), Amoxicillin(as trihydrate) 500 mg,
POM DAMOCLAV® (Dabak) Clavulanic acid (as potassium clavulanate) 200 mg; POM MENTCLAV® (Mark)
Potassium clavulanate equiv. to Clavulanic acid
Suspension, Amoxicillin 200 mg, clavulanic acid sterile powder for reconstitution in vials. Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic
125 mg; f-c tab.
28.5 mg acid (as clavulanate potassium) 125 mg; f-c tab.
POM HOCHMENTIN® (Hochiez) Pack: 10’s
Pack: 1 x 70 mL Pack: 7 x 2’s
Tablet, Amoxicillin 500 mg, Clavulanic acid 125 Tablet, (1000 mg), Amoxicillin (as trihydrate) 875
Suspension, Amoxicillin (as trihydrate) 200 mg,
POM DIGICLAV® (Digitall) mg; f-c tab. mg, Potassium clavulanate equiv. to Clavulanic acid
Clavulanic acid (as clavulanate potassium) 28.5
Tablet, (625 mg), Amoxicillin (as trihydrate) 500 mg, Pack: 2 x 7’s. 125 mg; f-c tab.
mg per 5 mL.
Clavulanic acid (as clavulanate potassium) 125 mg. Pack: 7’s
POM INDCLAV® (Manola) Pack: 100 mL
625 mg – 14’s Tablet, (375 mg), Amoxicillin 250 mg, clavulanic POM OXCLAV® (Pharmabase)
Tablet, (375 mg), Amoxicillin (as trihydrate) 250 mg, POM MOXIKIND-CV® (Phillips)
acid 125 mg; white to off – white coloured elliptical Tablet, (625 mg), Amoxicillin (as trihydrate) 500 mg,
Clavulanic acid (as clavulanate potassium) 125 mg. Tablet, (375 mg), Amoxicillin (as trihydrate) 250
biconvex f-c tab. Clavulanic acid (as clavulanate potassium) 125 mg;
375 mg – 20’s mg, Clavulanic acid (as clavulanate potassium) 125
Pack white f-c tab.
Suspension, (228 mg/5 mL), Amoxicillin (as tri- mg; f-c tab
Tablet, (625 mg), Amoxicillin 500 mg, clavulanic 625 mg – 2 x 7’s (in blisters).
hy-drate) 200 mg, Clavulanic acid (as clavulanate Pack: 2 x 6’s
acid 125 mg; white to offwhite coloured oblong Dry syrup, (228.5 mg/5 mL), Amoxicillin (as tri-
potassium) 28.5 mg per 5 mL. Tablet, (625 mg), Amoxicillin (as trihydrate) 500
biconvex f-c tab. hydrate) 200 mg, Clavulanic acid (as clavulanate
Pack: 70 mL mg, Clavulanic acid (as clavulanate potassium) 125
Pack: potassium) 28.5 mg per 5 mL; dry powder for
Suspension, (156 mg/5 mL), Amoxicillin (as tri- mg; f-c tab.
Tablet, (1000 mg), Amoxicillin 875 mg, clavulanic reconstitution.
hy-drate) 125 mg, Clavulanic acid (as clavulanate Pack: 2 x 6’s
acid 125 mg; white to off-white coloured oblong Pack: 100 mL.
potassium) 31.25 mg per 5 mL. Tablet, (1000 mg), Amoxicillin (as trihydrate) 875
biconvex f-c tab. Injection, Amoxicillin 1000 mg, clavulanic acid 200
Pack: 100 mL mg, Clavulanic acid (as clavulanate potassium) 125
Pack mg; milky-white powder with water for dilution.
mg; f-c tab.
POM ENHANCIN® (Ranbaxy) Pack: 1.2 g x 1’s (in vial)
POM JUMENTIN® (Juhel) Pack: 2 x 6’s
Tablet, (375 mg), Amoxicillin 250 mg, clavulanic acid Dry syrup, Amoxicillin (as trihydrate) 200 mg, POM PACMENTIN® (Pacmai)
125 mg; f-c tab. POM MYCLAV® (Phillips)
clavulanic acid (as clavulanate potassium) 28.5 mg Tablet, (375 mg), Amoxycillin trihydrate equiv. to
375 mg – 20. Tablet, (375 mg), Amoxicillin 250 mg, clavulanic acid
per 5 mL. Amoxicillin 250 mg; Potassium clavulanate equiv.
Tablet, (625 mg), Amoxicillin 500 mg, clavulanic acid 125 mg; f-c tab.
Pack: 100 mL. to Clavulanic acid 125 mg; f-c tab
125 mg; f-c tab. Tablet, (625 mg), Amoxicillin 500 mg, clavulanic acid
Pack: 2 x 6’s
625 mg – 20. POM KOACT® (Phillips) 125 mg; f-c tab.
Tablet, (625 mg), Amoxycillin trihydrate equiv. to
Suspension, (156.25 mg), Amoxicillin USP 125 mg, Tablets, (375 mg), Amoxicillin 250 mg, Clavulanic acid Pack: 6’s; 7’s; 10’s (in strips)
Amoxicillin 500 mg; Potassium clavulanate equiv.
clavulanic acid 31.25 mg per 5 mL; powder for 125 mg; white oval shaped f-c tab. marked ‘A’ on one
POM NECTACLAV® (Nectar Healthcare) to Clavulanic acid 125 mg; f-c tab
Pack: 2 x 6’s POM V-MOX-CA® (Nalis) Flucloxacillin (as sodium salt) BP 250 mg; caramel/ • Give IV intermittently to prevent vein irritation.
Oral suspension, (228.5 mg), Amoxycillin (as tri- Tablet, (625 mg), Amoxicillin (as trihydrate) 500 maroon capsule. • Mix with sterile water and give directly IV; al-
hydrate) 200 mg; Clavulanic acid (as potassium mg, Clavulanic acid (as clavulanate potassium) 125 Dry powder for oral suspension, Amoxicillin (as trihy- ternatively, mix with 0.9% NS; solutions for IV
clavulanate) 28.5 mg per 5 mL. mg; f-c tab drate) BP 125 mg, Flucloxacillin (as sodium salt) BP infusion will be inactivated by dextrose at room
Pack: 70 mL Oral suspension, Amoxicillin (as trihydrate) 200 mg, 125 mg per 5 mL. temperature.
Clavulanic acid (as clavulanate potassium) 28.5 mg Dry powder for injection, Amoxicillin (as sodium • Administer around-the-clock (in equal interval)
POM PEMACLAV® (Pemason)
per 5 mL; dry powder for reconstitution. salt) BP 250 mg, Flucloxacillin (as sodium salt) BP rather than 4 times/day to promote less variation
Tablet, (1000 mg), Amoxicillin 875 mg, Clavulanic
250 mg; in vial. in peak and trough serum levels.
acid 125 mg; white oblong scored tab. POM VULAMOX® (Quadrant)
Indications, Contra-indications, Precautions, etc: • Ampicillin and gentamicin should not be mixed in
1000 mg – 7 x 2’s (in blisters). Injection, (IV), Amoxicillin (as sodium salt) 1 g, Clavu-
see under Amoxicillin and Flucloxacillin. the same IV tubing or administered concurrently.
Tablet, (625 mg), Amoxycillin 500 mg, Clavulanic acid lanic acid (as clavulanate potassium) 200 mg; vials
Dose: Depends on the age, weight, renal function of • Monitor closely for signs of superinfection espe-
125 mg; white oblong scored tab. of sterile off-white powder.
the patient, the site and severity of infection cially with large doses and prolonged therapy
POM XYMENTIN® (Global Healthcare) and the suspected organisms. namely fever, sore throat, fatigue, diarrhoea.
Tablet, (375 mg), Amoxycillin 250 mg, Clavulanic
Tablet, (625 mg), Amoxicillin (as trihydrate) 500 mg, Adults (including the elderly), by mouth, 500 • Advise patient to report immediately if rash, fever,
acid 125 mg.
Clavulanic acid (as potassium clavulanate) 125 mg; mg every 8 hours ½ to 1 hour before meals. or chills occur. Rash is the most common allergic
POM PEMACLAV® (Pemason) white oval f-c tab. By IM Injection, 500 mg-1 g every 8 hours. reaction.
Caplet, Amoxicillin 800 mg, clavulanic acid 125 mg 625 mg – 2 x 7’s In severe infections the dosage may be Dose: Severe infections due to sensitive organ-
Capsule, Amoxycillin 500 mg, clavulanic acid 125 mg Tablet, (1000 mg), Amoxicillin 875 mg, clavulanic increased. By IV Injection, 500 mg-1 g every isms, by IM, by slow IV injection or by
125 mg 8 hours. In severe infections the dosage may IV infusion, ADULT 500 mg every 4–6
POM PLENATIN® (Placeware) be increased By lV infusion, As required by
1000 mg – 14’s hours; CHILD under 10 years, half the
Tablet, (625 mg), Amoxicillin 500 mg, Clavulanic the severity of the infection.
Dry syrup, Amoxicillin (as trihydrate) 250 mg,
125 mg; f-c tab. Children (up to 2 years), by mouth, 125 mg
adult dose.
Clavulanic acid (as potassium clavulanate) 62.5
625 mg – 7`s (in blisters).
mg per 5 mL. every 8 hours ½ an hour before meals; 2-10 Meningitis, by slow IV injection,
Tablet, (1000 mg), Amoxicillin 875 mg, clavulanate ADULT 1–2 g every 3–6 hours (maxi-
EMDEX
Pack: 100 mL. years: 250 mg every 8 hours ½ an hour
125 mg before meals. mum 14 g daily); CHILD 150–200 mg/
POM ZALAVIN® (Pharmgate)
POM RAPICLAV® (IPCA) kg daily in divided doses.
Tablet, (625 mg), Amoxicillin 500 mg, Clavulanate
Tablet, (375 mg), Amoxicillin 250 mg, Clavulanic acid AMPICILLIN Listerial meningitis (in combination
potassium 125 mg.
125 mg; f-c tab. Synonym: Aminobenzylpencillin. with another antibacterial), by IV
625 mg – 2 x 7’s
375 mg – 3’s; 21’s. infusion, ADULT 12 g daily in divided
Suspension, (228.5 mg), Amoxicillin 200 mg, clavula- Therapeutic category: Penicillin antibiotic.
Tablet, (625 mg), Amoxicillin 500 mg, Clavulanic acid doses every 4–6 hours for 10–14 days;
125 mg; f-c tab.
nate potassium 28.5 mg per 5 mL; dry syrup. Indications: Mastoiditis; gynaecological infec-
Pack: 100 mL (in bottle). tions; septicaemia; peritonitis; endocarditis; NEONATE under 7 days, 50–100 mg/
625 mg – 3’s; 21’s.
POM ZEROCLAV® (PharmacyPlus) meningitis; cholecystitis; osteomyelitis. kg every 12 hours; NEONATE 7–21
POM SUPRICLAV® (Canopus) Contra-indications: Hypersensitivity to peni- days, 50–100 mg/kg every 8 hours;
Tablet, (625 mg), Amoxicillin (as trihydrate) 500
Tablet, Amoxicillin (as trihydrate) 500 mg, Clavulanic NEONATE 21–28 days, 50–100 mg/
mg, Clavulanic acid (as clavulanate potassium) 125 cillins (see notes above).
acid (as Potassium) 125 mg. kg every 6 hours; CHILD 1 month–12
mg; f-c tab. Precautions: History of allergy (see notes
625 mg – 10’s; 2 x 7’s.
Pack: 2 x 7’s (in aluminium blisters) above); renal impairment (Appendix 4); ery- years 50 mg/kg every 4–6 hours
Suspension, Amoxicillin (as trihydrate) 125 mg, Clavu-
Suspension, (228.5 mg), Amoxicillin (as trihydrate) thematous rashes common in glandular fever, (maximum 2 g every 4 hours).
lanic (as Potassium) 31.25 mg per 5 mL
200 mg, Clavulanic acid (as clavulanate potassium) Reconstitution and administration: According to
Pack: 30 mL acute or chronic lymphocytic leukaemia, and
28.5 mg per 5 mL; after reconstitution. manufacturer’s directions.
Injection, Amoxicillin (as sodium salt) 1000 mg,
Suspension, (457 mg), Amoxicillin (as trihydrate) 400 cytomegalovirus infection; pregnancy and
Clavulanic acid (as clavulanate potassium) 200 mg; breastfeeding (Appendices 2 and 3); interac- POM Ampicillin (WMF 6.2.1)
mg, Clavulanic acid (as clavulanate potassium) 57
white to cream white dry powder for injection in tions: Appendix 1. Injections, Ampicillin (as sodium salt) 500 mg, 1 g;
mg per 5 mL; after reconstitution.
20-mL vial. Adverse effects: Nausea and vomiting, powder for reconstitution in vials.
Pack: 1.2 g x 1’s (in vials) POM ZEROCLAV XR® (PharmacyPlus).
diarrhoea; rashes (hypersensitivity or toxic POM AFRAMPI® (Afrab-Chem)
Tablet, Amoxicillin (as trihydrate) 1000 mg, clavulanic
POM SYNOCLAV® (Synergy) response—may be serious reaction, discon- Capsule, Ampicillin 250 mg.
acid (as clavulanate potassium) 62.5 mg; f-c tab.
Tablet, (625 mg), Amoxicillin (as trihydrate) 500 mg, tinue treatment); hypersensitivity reactions 250 mg – 10’s; 500’s (in blister).
Pack: 1 x 7’s (in aluminium blisters)
clavulanic acid (as potassium) 125 mg; f-c tab. including urticaria, angioedema, anaphylaxis, Suspension, Ampicillin 125 mg per 5 mL.
625 mg – 1 x 10’s POM ZICLAV® (Chanmedi) Pack: 100 mL.
serum sickness-like reaction, haemolytic anae-
Tablet, (1000 mg), Amoxicillin (as trihydrate) 875mg, Tablet, (625 mg), Amoxicillin + Clavulanic acid.
clavulanic acid (as potassium) 125 mg; f-c tab. 625 mg – 2 x 7’s.
mia, interstitial nephritis (see also notes above); POM ALPHAPIN® (GoldMoore)
1000 mg – 1 x 10’s Suspension, (228 mg), Amoxicillin + Clavulanic acid rarely, antibiotic-associated colitis; neutrope- Suspension, Ampicillin (as trihydrate) BP 125 mg
Oral suspension, Amoxicillin (as trihydrate) 200 mg, (228 mg per 5 mL). nia, thrombocytopenia, coagulation disorders. per 5 mL.
clavulanic acid (as potassium) 28.5 mg per 5 mL; Advice to patients: See labels 9 and 23 in POM AMCILLIN® (Embassy)
POM ZOCLAV® (Bakangizo)
powder for reconstitution. App. 6. Capsule, Ampicillin 250 mg.
Injection, Amoxicillin (as sodium salt) 1000 mg, Clavu-
Pack: 75 mL.
lanic acid (as clavulanate potassium) 200 mg
Nursing action: Ask patient about allergy to 250 mg – 100’s.
POM TAMA-CLAV® (Tamar & Pharez) Pack: 1 x 10’s (in vials) penicillins; obtain specimen for C&S test; give Injection, Ampicillin 1 g.
Injection, (600 mg), Amoxicillin (as sodium salt) 600 orally on an empty stomach (i.e., 1 hour prior Pack: 10’s.
mg, Potassium clavulanate 100 mg. AMOXICILLIN plus FLUCLOXACILLIN to, or 2 hours after meals) to increase total POM AMDIFAB® (FAB)
Pack: 1's (in vial). absorption; with a full glass of water. Shake Syrup, Ampicillin 125 mg per 5 mL.
Injection, (1.2 g), Amoxicillin (as sodium salt) 1000 See under the preparations below. suspension well before each dose.
mg, Potassium clavulanate 200 mg. • Avoid IM or IV use except in severe infection or POM AMPI-PIKURU® (Goldmoore)
Pack: 1's (in vial) POM ESPAPEN® (Medreich) when patient can’t take oral dose. Injection, Ampicillin.
Capsule, Amoxicillin (as trihydrate) BP 250 mg,
POM AMPICAP® (Hovid) Suspension, Ampicillin (as trihydrate) 125 mg per Capsule (500 mg), Ampicillin 500 mg. with beta-lactamase and competitively inhibits
Capsules, Ampicillin (as trihydrate) 250 mg, black and 5 mL. 500 mg – 10’s (in blister); 1000’s the activity of beta-lactamases; thus cloxacillin
scarlet cap. marked ‘HD’ on one end and ‘AP 250’ on Pack: 1 x 100 mL. Injection, Ampicillin (as Na+) 500 mg. when given in combination with ampicillin
the other; 500mg. Pack: 100’s protects the latter from the destruction by
POM EMCILLIN® (Emzor)
250 mg – 10 x 10 (blister)
Capsule, Ampicillin (as trihydrate) 250 mg, 500 mg; POM NOXILIN® (Geneith) beta-lactamase. The sparing of ampicillin by
500 mg – 10 x 10 (blister).
red/black caps marked ‘EMZOR’ and cap strength. Injection, Ampicillin sodium 500 mg. this mechanism increases the availability of
POM AMPICARE® (Dizpharm) Pack: 10’s x 2; 10’s x 100; 10’s x 50 ampicillin at the site of infection. This serves
POM PEMACILLIN® (Pemason)
Capsule, Ampicillin (as trihydrate) 250 mg. Suspension, Ampicillin (as trihydrate) 125 mg per 5 to retain the broad antibacterial spectrum of
Injection, Ampicillin sodium 1 gm per vial; white
250 mg – 1000. mL; dry powder for reconstitution.
crystalline powder in 5 mL vials. ampicillin against Gram-positive as well as
Suspension, Ampicillin (as trihydrate) 125 mg per Pack: 100 mL.
5 mL.
Pack: 5 mL x 10 x 10’s. Gram-negative organisms including those that
POM GLOCILLIN® (Richygold) produce beta-lactamase.
Pack: 60 mL. POM REICHLIN® (Medreich)
Capsules, Ampicillin (as trihydrate) 250 mg, 500 mg. Indications: Infections of the respiratory
Capsules, Ampicillin (as trihydrate) 250 mg, black and
POM AMPICEE® (Ranbaxy) 250 mg – 10 x 10’s (in blister). tract, ear, nose and throat (ENT), urinary tract,
maroon capsule marked ‘Ampi-250’; 500 mg, black
Capsule, Ampicillin (as trihydrate) 250 mg. 500 mg – 10 x 10’s (in blister).
and maroon capsule marked ‘Ampi-500’. gastro-intestinal tract, skin and soft-tissue;
250 mg – 10 x 10; 10 x 100; 1000. Injection, Ampicillin (as sodium salt) BP 500 mg.
Suspension, Ampicillin (as trihydrate) 125 mg per
Pack: 10 x 100. septicaemia, pelvic infections, endocarditis
POM JAWACILIN® (Jawa) Suspension, Ampicillin (as trihydrate) 125 mg per 5 and orthopaedic infections.
5 mL
Syrup, Ampicillin 125 mg per 5 mL; dry powder for mL; dry powder for reconstitution. Contra-indications: History of hypersensitivity
Pack: 60 mL.
reconstitution. Pack: 100 mL. to penicillins, cephalosporins, penicillin deriv-
POM Ampicillin (Rajrab) Pack:100 mL.
POM ROSCILLIN® (Ranbaxy) atives or penicillamine.
Capsule, Ampicillin (as trihydrate) 250 mg; capsule
POM LAMPICIN® (Mecure) Capsules, Ampicillin (as trihydrate) 250 mg, 500 mg. Precautions: History of GI disease especially
marked “AMPI 250”.
Capsule, Ampicillin 250 mg; black/red capsule 250 mg – 10’s; 20’s; 500’s; 1000’s. antibiotic associted colitis (ampicillin like other
250 mg – 100’s
EMDEX
marked ‘LAMPICIN’. 500 mg – 10’s; 20’s; 500’s; 1000’s. penicillins may cause pseudomembranous
POM AMPITAB® (Hovid) 250 mg – 10 x 10’s.
POM VITACILLIN® (Strides Vital) colitis). May cause skin rash in patients with
Tablets, Ampicillin (as trihydrate) 125 mg (orange Suspension, Ampicillin 125 mg per 5 mL; dry powder
scored tab. marked ‘HOVID’); 250 mg (yellow scored for reconstitution.
Capsules, Ampicillin (as trihydrate) 250 mg, 500 infectious mononucleosis. Renal impairment.
mg; red/black caps marked with brand name and Interactions: Bacteriostatic antibiotics such
tab. marked ‘HOVID’); 500 mg (yellow tab. with Pack: 100 mL
strenght. as tetracyclines, erythromycin or sulpho-
shallow convex faces). All the tablets are flavoured.
POM LINOX®-500 (Beta Drugs) 250 mg – 10 x 10’s. namides may antagonise the bactericidal
125 mg – 1000; 10 x 10 (blister)
Injection, Ampicillin 500 mg. 500 mg – 10 x 10’s.
250 mg – 100; 1000; 10 x 10 (blister) effect of penicillin (avoid co-administration).
Pack: 1 x 10 vials. Dry Syrup , Ampicillin (as trihydrate) 125 mg per 5
500 mg – 1000. Probenecid decreases renal tubular secretion
mL; dry powder for reconstitution in amber bottle.
POM MAXICILLIN® (Richygold) of penicillins resulting in increased and more
POM AMPY-250® (Diamond Remedies) Pack: 100 mL.
Capsules, Ampicillin (as trihydrate) 250 mg, 500 mg. prolonged penicillin concentrations. Allopu-
Capsule, Ampicillin (as trihydrate) 250 mg. Injections, Ampicillin 0.5 g, 1 g; in vials.
250 mg – 10 x 10’s rinol (increased incidence pof skin rash). Oral
Pack: 50. 0.5 g – 50’s
500 mg – 10 x 10’s.
1 g – 50’s. contraceptives (decreased efficacy of oral con-
POM AVROCLOX® (Avro)
POM MD-Ampicillin (O’Nell) traceptives due to reduction in enterohepatic
Suspension, Ampicillin (as trihydrate) 125 mg, Cloxa- POM ZIMACILLIN® (Gauze)
Suspension, Ampicillin (as trihydrate) 125 mg per 5 circulation of oestrogens. Advise patient to use
cillin (as sodium salt) 125 mg per 5 mL; dry powder Oral dry syrup, Ampicillin trihydrate 125 mg per 5 mL
mL; dry powder for reconstitution. alternative or additional method of contracep-
for reconstitution. Pack: 100 mL
Pack: 100 mL
tion while taking ampicillin).
POM AZINA® (Vixa)
Capsules, Ampicillin (as trihydrate) 250 mg, 500 mg.
POM MEDAMPI® (Embassy) AMPICILLIN plus CLOXACILLIN Adverse effects: GI reactions such as nausea,
Capsules, Ampicillin 250 mg, 500 mg. vomiting, diarrhoea, pseudomembranous
250 mg – 10 x 10’s; 1000’s.
250 mg – 100’s.
Therapeutic category: Penicillin antibiotic
500 mg – 10 x 10’s; 1000’s. Pharmacology: Ampicillin, an amino-penicillin colitis, cholestatic jaundice; neutropenia; an-
500 mg – 100’s. aphylaxis, serum sickness-like reactions, skin
Syrup, Ampicillin (as Trihydrate) 125 mg per 5 mL. and cloxacillin, an isoxazolyl penicillin have
Suspension, Ampicillin 125 mg per 5 mL.
Pack: 60 mL; 100 mL.
an identical mode of action i.e., they inhibit rash, hives, itching; oral candidiasis.
Pack: 100 mL.
Injection, Ampicillin sodium 500 mg/vial.
bacterial cell wall synthesis. This results in the Advice to patients and Nursing action: See
Pack: 50 vials/box. POM MIRAPICIN® (Miraflash) under Ampicillin.:
Oral suspension, Ampicillin (as trihydrate) 125 mg
weakening of the bacterial cell wall and cell
POM BARBICILLIN® (Juhel) lysis. Ampicillin is susceptible to degradation Dose: By mouth, 0.5-1 g 6 hourly or more
per 5 mL; powder for reconstitution. frequently according to the severity
Capsule, Ampicillin (as trihydrate) 250 mg. by ß-lactamases and is therefore inactive
Pack: 100 mL
250 mg – 100; 1000.
against strains producing this enzyme. The of the infection.
Suspension, Ampicillin (as trihydrate) 125 mg per 5 POM NAMPICILLIN ®(NASDMU) By IM Injection, 0.5-1 g 6 hourly
mL; dry powder for reconstitution.
combination displays synergy against some
Capsule, Ampicillin (as trihydrate) 250 mg; black/ By IV Injection, 0.5-1 g 4-6 hourly; up
Pack: 60 mL; 100 mL. maroon cap. marked ‘NAMPI 250 mg’. ß-lactamase producing organisms as clox-
acillin protects ampicillin from enzymatic to 12 g by IV infusion.
Pack: 100; 1000.
POM BENCILLIN® (Nichben) destruction by ß-lactamases by binding them. Child: 1 month – 2 years, by mouth,
Capsule, Ampicillin 250 mg. POM NEMECILLIN® (Nemel)
Most staphylococci and many strains of E.coli, 1/4 adult dose; 2-10 years, 1/2 adult
250 mg – 100’s; 1000’s. Capsule, Ampicllin 250 mg dose.
Dry syrup, Ampicillin 125 mg per 5 mL. H. influenzae, M. catarrhalis, N.gonorrhoeae,
Syrup, Ampicillin trihydrate 125 mg per 5 mL; dry Neonates: Oral drops, 0.6 mL (90 mg)
Pack: 60 mL. powder. Salmonella and Shigella are resistant to ampi-
cillin as beta-lactamases produced by these susp. 4 hourly.
POM CIKACILLIN® (Michelle Lab) POM NOCILLIN® (Geneith) strains inactivate ampicillin. Cloxacillin forms By IM Injection, 75 mg 8 hourly
Capsule, Ampicillin (as trihydrate) 250 mg. Capsule, (250 mg), Ampicillin 250 mg. By IV Injection, 75 mg 8 hourly.
a relatively stable enzyme substrate complex
250 mg – 100’s; 10 x 10’s (in blisters) 250 mg – 10 x 10’s (in blister)
POM Ampicillin plus Cloxacillin (EDL 5.3) POM CIKACLOX® (Michelle Lab) Injection, Ampicillin 250 mg, cloxacillin 250 mg. POM NEMECLOX® (Nemel)
Capsule, Ampicillin 250 mg, cloxacillin 250 mg Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin Pack: 1’s (in vial). Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin
Powder for oral liquid, Ampicillin 125 mg, cloxacillin (as sodium salt) 250 mg. (as sodium salt) 250 mg
POM FRACLOX® (Embassy)
125 mg per 5 mL. Pack: 10 x 10’s (in blisters) Pack: 10 x 10’s (in blisters)
Capsule, Ampicillin 250 mg, cloxacillin 250 mg.
Neonatal drops, Ampicillin 60 mg, cloxacillin 30 mg Suspension, Ampicillin (as trihydrate) 125 mg, Clox-
POM PILOXAL ®(Quadrant)
per 0.6 mL. acillin (as sodium salt) 125 mg per 5 mL. POM GENICLOX® (Geneith)
Injection, Ampicillin 250 mg, Cloxacillin (as sodium
Neonatal injection, Ampicillin 50 mg, cloxacillin 25 Pack: 1 x 100 mL Capsule, Ampicillin 250 mg, cloxacillin 250 mg
salt) 250 mg per vial
mg per vial. 500 mg – 10 x 10’s (in blister).
POM CILLINOX® (Afrab-Chem)
Injection, Ampicillin (as sodium salt) 250 mg, cloxacil- Injection, Ampicillin 250 mg, cloxacillin 250 mg POM REICHLOX® (Medreich)
Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin
lin (as sodium salt) 250 mg; powder in vial. Pack: 5 x 10’s Capsule, Ampicillin 250 mg, cloxacillin 250 mg; black/
(as sodium) 250 mg.
purple capsule.
POM ACILOX® (Mopson) Pack: 10 x 10’s (in blister). POM GLOPICLOX® (Hochiez)
Dry syrup, Ampicillin 125 mg, cloxacillin 125 mg per
Capsule, (500 mg), Ampicillin (as trihydrate) 250 mg, Oral suspension: Ampicillin (as trihydrate) 125 mg, Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin
5 mL; powder for preparing fruit flavoured syrup.
Cloxacillin (as sodium salt) 250 mg Cloxacillin (as sodium) 125 mg per 5 mL; powder (as sodium salt) 250 mg.
Neonatal drops, Ampicillin 60 mg, cloxacillin 30 mg
Pack: 10 x 10’s for reconstitution. 500 mg – 10 x 10’s.
per 0.6 mL; powder for preparing 8 mL of sugar free
Powder for oral suspension, Ampicillin (as trihydrate) Pack: 100 mL.
POM JAWACLOX®(Jawa) oral suspension.
125 mg, Cloxacillin (as sodium sat) 125 mg Oral drops: Ampicillin (as trihydrate) 60 mg, Clox-
Capsule, Ampicillin 250 mg, cloxacillin 250 mg Injection, Ampicillin 250 mg, cloxacillin 250 mg;
Pack: 100 mL acillin (as sodium) 30 mg per 0.6 mL; powder for
500 mg – 10 x 10’s in vial.
reconstitution.
POM ALUCLOX® (May & Baker) Syrup, Ampicillin 250 mg, cloxacillin 250 mg per 5
Pack: 12 mL amber bottle. POM RIAMCLOX® (Richygold)
Capsule, Ampicillin 250 mg, cloxacillin 250 mg mL; dry powder for reconstitution.
Capsule, (250 mg), Ampicillin (as trihydrate) 250 mg,
Pack: 10 x 10’s. POM CLOXAPEN® (Rajrab) Pack: 100 mL.
cloxacillin (as sodium) 250 mg.
Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin Neonatal drops, Ampicillin 60 mg, cloxacillin 30 mg
POM AMPICLOX® (GSK) Pack: 10’s; 1000’s.
(as sodium) 250 mg; capsule marked “CLOXAPEN per 0.6 mL.
Capsule, Ampicillin 250 mg, cloxacillin 250 mg Injection, Ampicillin (as sodium) 250 mg, cloxacillin
EMDEX
500”. Pack: 8 mL.
500 mg – 12; 100. (as sodium) 250 mg.
500 mg – 100’s Injection, Ampicillin 250 mg, cloxacillin 250 mg;
Syrup, Ampicillin 125 mg, cloxacillin 125 mg per 5 mL
in vial. POM ROSCILOX® (Ranbaxy)
Pack: 60 mL; 100 mL. POM CLOXFAB® (FAB)
Pack: 10’s; 50’s. Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin
Neonatal drops, Ampicillin 60 mg, cloxacillin 30 mg Syrup, Ampicillin 125 mg, Cloxacillin 125 mg per 5 mL
(as sodium) 250 mg.
per 0.6 mL. Pack: 100 mL POM LABOCLOX® (Embassy)
500 mg – 25 x 4’s; 24 x 10’s; 500’s.
Pack: 8 mL. Injection, Ampicillin 250 mg, cloxacillin 250 mg.
POM COMPI-CLOX® (Drugfield) Suspension, Ampicillin (as trihydrate) 125 mg, clox-
Injection, Ampicillin 250 mg (as sodium salt), cloxacil- Pack: 50’s.
Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin acillin (as sodium) 125 mg per 5 mL.
lin 250 mg (as sodium salt); powder in vial.
(as sodium) 250 mg. POM LACLOX® (Mecure) Pack: 60 mL.
Pack: 10.
500 mg – 500’s Capsule, Ampicillin 250 mg, Cloxacillin 250 mg; Injection, Ampicillin 250 mg, cloxacillin 250 mg;
Neonatal Injection, Ampicillin 50 mg (as sodium
Oral suspension, Ampicillin (as trihydrate) 125 mg, purple/black capsule marked ‘LACLOX’. in vial.
salt), cloxacillin 25 mg (as sodium salt); powder in
Cloxacillin (as sodium salt) 125 mg per 5 mL; dry Pack: 2 x 10’s; 10 x 10’s. Pack: 1.
single dose vial.
powder for reconstitution. Suspension, Ampicillin 125 mg, cloxacillin 125 mg
Pack: 10. POM SYNACLOX® (Synergy)
Neonatal drops, Ampicillin (as trihydrate) 60 mg, per 5 mL; dry powder for reconstitution
Capsule, Ampicillin 250 mg, cloxacillin 250 mg.
POM AMPY-CLOXA® (Diamond Remedies) Cloxacillin (as sodium) 30 mg per 0.5 mL Pack: 100 mL
Suspension, Ampicillin 125 mg, cloxacillin 125 mg
Capsule, Ampicillin (trihydrate) 250 mg, cloxacillin
POM CP-CLOX® (Crowther) POM LINACLOX® (E-Globa) per 5 mL.
(as sodium salt) 250 mg.
Injection, Ampicillin 250 mg, cloxacillin 250 mg; ry Injection, Ampicillin 250 mg, Cloxacillin 250 mg;
POM THAMICLOX® (Therapeutic)
POM BARBICLOX® (Juhel) powder for reconstitution + WFI as diluent. white dry powder in vial.
Dry powder, Ampicillin (as trihydrate) 125 mg, Clox-
Capsule, Ampicillin (anhydrous) 250 mg, cloxacillin Pack: 10 x 1’s Pack: 1 x 10’s; 100’s.
acillin (as sodium salt) 125 mg per 5 mL.
(as sodium salt) 250 mg.
POM CRISTACLOX® (Crystal) POM LOXIN® (Neimeth) 250 mg – 100 mL.
500 mg – 100; 1000.
Capsule, Ampicillin 250 mg, cloxacillin 250 mg Capsule, Ampicillin 250 mg, cloxacillin (as sodium)
Syrup, Ampicillin (anhydrous) 125 mg, cloxacillin (as POM VANCLOX® (Evans)
Pack: 10 x 10’s 250 mg.
sodium salt) 125 mg per 5 mL. Capsule, Ampicillin 250 mg, cloxacillin 250 mg.
Pack: 60 mL; 100 mL. 500 mg – 100’s.
POM EMZOCLOX® (Emzor) 500 mg – 100’s.
Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin POM MAXACLOX® (GoldMoore)
POM BECTALUX® (Bentos) POM VITACLOX® (Strides Vital)
(as sodium salt) 250 mg; pink/black cap marked Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin
Capsule, Ampicillin 250 mg, Cloxacillin 250 mg Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin
‘EMZOR’ and ‘500’. (as sodium) 250 mg.
Syrup, Ampicillin 125 mg, Cloxacillin 125 mg per (as sodium salt) 250 mg; black/maroon cap. marked
500 mg – 10 x 2; 10 x 50; 10 x 100; 1000. Pack: 10 x 10’s (in blister).
5 mL. ‘VITACLOX’
Suspension, Ampicillin (as trihydrate) 125 mg, cloxa-
POM MEDICLOX® (Embassy) 500 mg – 10 x 10.
POM BENPICLOX® (Nichben) cillin (as sodium salt) 125 mg per 5 mL; dry powder
Capsule, Ampicillin 250 mg, cloxacillin 250 mg. Injection, Ampicillin 250 mg, cloxacillin 250 mg; in
Capsule, Ampicillin 250 mg, Cloxacillin 250 mg for reconstitution.
Pack: 10 x 10’s. 500 mg vial.
Syrup, Ampicillin 125 mg, Cloxacillin 125 mg per Pack: 60 mL.
Pack: 50’s.
5 mL; powder for preparing fruit-flavoured syrup. Drops, Ampicillin (as trihydrate) 60 mg, Cloxacillin POM MIRACLOX® (Miraflash)
(as sodium salt) 30 mg per 0.6 mL. Oral suspension, Ampicillin 125 mg, cloxacillin 125 POM ZAPOX® (Elbe)
POM CAPICLOX® (Dizpharm)
mg per 5 mL; powder for reconstitution. Capsule, Ampicillin 250 mg, cloxacillin 250 mg
Capsule, Ampicillin (as trihydrate) 250 mg, Cloxacillin POM FECLOX® (Fidson)
(as sodium salt) 250 mg. Capsule, Ampicillin 250 mg, cloxacillin 250 mg Pack: 100 mL
POM ZICLAX® (Chanmedi)
500 mg – 100. 500 mg – 100. POM NAMPICLOX® (NASDMU) Capsule (500 mg), Ampicillin 250 mg, Cloxacillin
Suspension, Ampicillin (as trihydrate) 125 mg, Clox- Suspension, Ampicillin 125 mg, cloxacillin 125 mg Capsule, Ampicillin 250mg, Cloxacillin 250 mg; 250 mg.
acillin (as Sodium salt) 125 mg per 5 mL. per 5 mL; dry powder for reconstitution. marked “NAMPI”
Pack: 60 mL; 100 mL. Pack: 60 mL; 100 mL. POM ZICLOX® (SKG)
Pack: 10 x 10’s
Capsule, Ampicillin 250 mg, Cloxacillin 250 mg. quantities of ampicillin and sulbactam. release of endotoxins); rarely, non-allergic (em- doses, vary the injection site.
500 mg – 10 x 10’s. Indications: Sultamicillin is given orally as bolic-toxic) reactions; pain and inflammation Administer by deep intramuscular injection
Suspension, Ampicillin (as trihydrate) 125 mg, Cloxa- tablets containing sultamicillin tosilate or as at injection site. into the outer, upper quadrant of the buttock
cillin (as sodium salt) 125 mg per 5 mL; dry powder oral suspension containing sultamicillin. It Nursing action: Before giving drug, ask patient or into Hochstetter’s ventrogluteal field. In
for reconstition.
is used in the treatment of infections where if he has had any allergic reactions to this drug children the midlateral aspect of the thigh
POM ZIMACLOX® (Gauze) beta-lactamase-producing organisms might or penicillins generally; scratch test may be (quadriceps femoris muscle) is preferable.
Oral dry syrup, Ampicillin (as trihydrate) 125 mg, occur, including uncomplicated gonorrhoea, done to assess allergy; obtain specimen for C&S Only use the deltoid muscle for injections, if
Cloxacillin sodium 125 mg per 5 ml otitis media, and respiratory-tract and uri- test, therapy may begin pending test results. its muscle mass is well developed; keep well
Pack: 100 mL • Administer by deep IM inj in large muscle mass;
nary-tract infections. away from the radial nerve.
POM ZOOMPICLOX® (Zoomota) Dose: By mouth, usually 375-750 mg of aspirate to avoid intravascular inj. Shake well The maximal volume tolerated at a given
Capsule, Ampicillin (as trihydrate) 250 mg, cloxacillin sultamicillin (equivalent to 147-294 before injection. injection site is 5 mL. Consequently, no more
(as sodium) 250 mg; pink/black cap. • Never give IV – inadvertent IV administration has
mg of sulbactam and 220 – 440 mg of than 5 mL of the injectable suspension should
Pack: 10 x 10’s (in blisters). caused instant cardiac arrest and death.
ampicillin) twice daily. • Tell patient to report any rash, fever or chills; fever,
be applied at any one site.
Suspension, Ampicillin (as trihydrate) 125 mg,
Uncomplicated gonorrhoea, a single eosinophilia are common allergic reactions; very POM Benzathine benzylpenicillin (WMF 6.2.1)
cloxacillin (as sodium) 125 mg; cream powder for
reconstitution. dose of sultamicillin 2.25 g with slow absorption time makes allergic reactions Injection (1.2 MU), Benzathine benzylpenicillin 0.9
Pack: 50 mL x 1. probenecid 1 g may be used. difficult to treat. g (equiv. to benzylpenicillin 0.72 g = 1.2 million IU);
Injection, Ampicillin (as sodium) 250 mg, cloxacillin When parenteral therapy is necessary • Large doses and prolonged therapy may give powder for injection in 5-mL vial.
(as sodium) 250 mg; white powder for reconstitu- a combined preparation of ampicillin rise to superimposed infection; teach patient Injection (2.4 MU), Benzathine benzylpenicillin 1.8
tion in vial. with sulbactam is given. symptoms namely sore throat, fever fatigue and g (equiv. to benzylpenicillin 1.44 g = 2.4 million IU);
Pack: 1 vial + 10 mL water for injection as diluent to report such symptoms. powder for injection in 5-mL vial.
(Source: Ampicillin with sulbactam. Martindale – The Complete
• Encourage patient to have extra fluid intake if
Drug Reference [Online]. Available from: http://www.thomsonhc. POM Benzathine benzylpenicillin (EDL 5.3)
diarrhoea occurs.
EMDEX
AMPICILLIN plus FLUCLOXACILLIN com/hcs/librarian/ND_T/HCS/ND_PR/Main/CS/A4B526/ Injection (1.2 MU), Benzathine benzylpenicillin 0.9
DUPLICATIONSHIELDSYNC/51B92E/ND_PG/PRIH/ Dose: Streptococcal pharyngitis; primary
g (equiv. to benzylpenicillin 0.72 g = 1.2 million IU);
POM BETALOX® (Medreich) ND_B/HCS/SBK/2/ND_P/Main/PFActionId/hcs.common. prophylaxis of rheumatic fever, by
RetrieveDocumentCommon/DocId/10-c/ContentSetId/30/ powder for injection in 5-mL vial.
Capsule, Ampicillin (as trihydrate) BP 250 mg, flu- deep IM injection, ADULT and CHILD
SearchTerm/SULBACIN). Injection (2.4 MU), Benzathine benzylpenicillin 1.8
cloxacillin (as sodium) BP 250 mg over 30 kg, 900 mg as a single dose; g (equiv. to benzylpenicillin 1.44 g = 2.4 million IU);
Dry powder for oral suspension, Ampicillin (as trihy-
POM SULBACIN® (Phillips) CHILD under 30 kg, 450–675 mg as a powder for injection in 5-mL vial.
drate) 125 mg, flucloxacillin (as magnesium) 125
mg per 5 mL. Tablet, (375 mg): Sultamicillin 375mg equiv. to single dose.
POM RETARPEN® (Carrot-Top)
Sulbactam 147 mg, ampicillin 220 mg. Secondary prophylaxis of rheumatic Injection, Benzathine penicillin 0.6 m.u., 1.2 m.u., 2.4
Indications, Contra-indications, Precau- Pack: 4’s fever, by deep IM injection, ADULT m.u.; powder for reconstitution in vials.
tions, etc: see under Ampicillin and Cloxacillin. Injection, (1.5 g), Sulbactam 500 mg, ampicillin and CHILD over 30 kg, 900 mg once Pack – Single packs of 1 vial (+ solvent).
Dose: Depends on the age, weight, renal function 1000 mg every 3–4 weeks; CHILD under 30 kg,
of the patient, the site and severity of infec- Injection, (0.75 g), Sulbactam 250 mg, ampicillin
tion and the suspected organisms. Adults
450 mg once every 3–4 weeks. BENZYLPENICILLIN
500 mg
(including the elderly), by mouth, 500 mg Early syphilis, by deep IM injection, Synonym: Penicillin G; Crystalline Penicillin.
every 8 hours ½ to 1 hour before meals. BENZATHINE BENZYLPENICILLIN ADULT 1.8 g as a single dose, divided Indications: Pneumonia; throat infections;
Children (<2 years), by mouth, 125 mg between 2 sites. otitis media; Lyme disease; streptococcal en-
Synonym: Penicillin G Benzathine; Benzathine
every 8 hours ½ an hour before meals; Late syphilis, by deep IM injection, docarditis; meningococcal disease; necrotizing
2-10 years: 250 mg every 8 hours ½ an hour penicillin.
ADULT 1.8 g, divided between two enterocolitis; necrotizing fasciitis; leptospirosis;
before meals. Indications: Streptococcal pharyngitis; diph-
sites, once weekly for 3 consecutive neurosyphilis; anthrax; relapsing fever; actino-
theria; syphilis and other treponemal infec-
weeks. mycosis; brain abscess; gas gangrene; cellulitis;
AMPICILLIN plus SULBACTAM tions (yaws, pinta, bejel); rheumatic fever
Congenital syphilis (where no evidence osteomyelitis.
Synonym: Sultamicillin prophylaxis.
of CSF involvement), by deep IM injec- Contra-indications: Penicillin hyper-sensitivity
Pharmacology: The sodium salts of ampicillin Contra-indications: Penicillin hypersensitiv-
tion, CHILD up to 2 years, 37.5 mg/kg (see notes above); avoid intrathecal route (see
and sulbactam may be given IM or IV in the ity (see notes above); intravascular injection;
as a single dose. notes above).
treatment of infections due to beta-lactama- neurosyphilis.
Yaws, pinta, and bejel, by deep IM Precautions: History of allergy (see notes
se-producing organisms. Doses are expressed Precautions: History of allergy (see notes
injection, ADULT 900 mg as a single above); renal failure (Appendix 4); heart failure;
in terms of the equivalent amounts of am- above); renal failure (Appendix 4); pregnancy
dose; CHILD 450 mg as a single dose. pregnancy and breastfeeding (Appendices 2
picillin and sulbactam; available injections and breastfeeding (Appendices 2 and 3); inter- How to Use: For deep intramuscular injection. For
actions: Appendix 1. and 3); interactions: Appendix 1.
contain ampicillin and sulbactam in the ratio i.m. injections suspend the content of the 600,000
Adverse effects: Hypersensitivity reactions Adverse effects: Hypersensitivity reactions
2:1, respectively. The usual dose is ampicillin 1 I.U. (0.6 M.U.)vial in at least 2 mL of water for injec-
including urticaria, fever, joint pains, rashes, tions, that of the 1.2 M.U. vial in at least 3 mL of water including urticaria, fever, joint pains, rashes,
g with sulbactam 500 mg every 6 hours; doses angioedema, anaphylaxis, serum sickness-like
may be doubled in severe infections. angioedema, anaphylaxis, serum sickness-like for injections and that of the 2.4 M.U. vial in at least
reaction, haemolytic anaemia, interstitial 5 mL of water for injections. reactions, haemolytic anaemia, interstitial
For oral use sultamicillin (as tosilate) may be nephritis (see also notes above); diarrhoea,
nephritis (see also notes above); neutropenia, Shake vigorously for 20 seconds and apply
given. Sultamicillin is a prodrug of ampicillin antibiotic associated colitis; neutropenia,
thrombocytopenia, coagulation disorders immediately using a needle of at least 0.9 mm
and of the beta-lactamase inhibitor sulbactam; thrombocytopenia, coagulation disorders, CNS
and CNS toxicity (associated with high dosage strenght. Withdraw no more than one dose.
it consists of the two compounds linked as toxicity, including convulsions, coma, and en-
or severe renal failure); Jarisch-Herxheimer Only use freshly prepared suspensions. Before
a double ester. During absorption from the cephalopathy (associated with high dosage, or
reaction (during treatment for syphilis and injecting the dose, aspirate to be sure needle
GI tract it is hydrolysed, releasing equimolar severe renal failure); electrolyte disturbances;
other spirochaete infections, probably due to bevel is not in a blood vessel. When repeating
Jarisch-Herxheimer reaction (during treatment then 30 mg/kg 3 times daily for 3 Injection, Crystalline penicillin. infection; by IM injection, 250 mg
for syphilis and other spirochaete infections, days; by IM injection or slow IV injec- POM SIVOSTALINE® (Adpharm) every 4–6 hours, doubled in severe
probably due to release of endotoxins); in- tion, CHILD over 2 years, 120–180 mg/ Injection, Benzylpenicillin 100,000 IU. infection; by slow IV injection or IV in-
flammation, phlebitis or thrombophlebitis at kg (to a maximum of 1.44 g) daily in Pack: 1 x 10’s fusion, 1–2 g every 6 hours; CHILD up
injection sites. 4–6 divided doses for 10–14 days to 2 years, quarter adult dose; CHILD
POM VITATEX® (Jubilee)
Advice to patients: Report any rash or short- Reconstitution and administration: According 2–10 years, half adult dose.
Injections, Benzylpenicillin (as potassium salt) 0.125
ness of breath. to manufacturer’s directions. Intravenous route
g (200,000 i.u), 0.25 g (400,000 i.u), 0.3 g (500,000 POM Cloxacillin (WMF 6.2.1)
Nursing action: Determine whether the preferred for neonates and infants; doses over 1.2
i.u), 0.5 g (800,000 i.u), 0.625 g (1000,000 i.u); in vials. Capsules, Cloxacillin (as sodium salt) 500 mg, 1 g.
g by IV route only.
patient is allergic to penicillins prior to ad- Powder for oral liquid, Cloxacillin (as sodium salt)
Note: Administer IM by deep injection in the upper
ministration. outer quadrant of the buttock; administer injection CLOXACILLIN 125 mg/5 mL.
• Obtain specimen for C&S test; therapy may begin Powder for injection, Cloxacillin (as sodium salt) 500
around-the-clock to promote less variation in peak Indications: Infections due to beta-lactama-
pending test results. mg; in vial.
and trough levels; while IM route is preferred route of se-producing staphylococci including impe-
• Dosage should be modified in renal impairment.
administration, large doses should be administered tigo, cellulitis and other soft-tissue infections; POM Cloxacillin (EDL 5.3)
• Tell patient to report any rash, fever or chills; fever,
by continuous IV infusion; determine volume and pyomyositis; staphylococcal endocarditis, Capsule, Cloxacillin 250 mg.
eosinophilia are common allergic reactions; very
rate of fluid administration required in a 24-hour Oral liquid, Cloxacillin 125 mg per 5 mL.
slow absorption time makes allergic reactions septicaemia, pneumonia, septic arthritis, and
period, add appropriate daily dosage to this fluid. Injection, Cloxacillin 250 mg, 500 mg; powder for
difficult to treat. osteomyelitis; otitis externa.
• Large doses and prolonged therapy may give POM Benzylpenicillin (WMF 6.2.1) injection in vials.
Contra-indications: Hypersensitivity to peni-
rise to superimposed infection; teach patient Injection, Benzylpenicillin (as sodium potassium salt) cillins (see notes above). POM Apo-Cloxi (Lahams)
symptoms namely sore throat, fever fatigue and 600 mg (= 1 million IU), 3 g (= 5 million IU); powder Precautions: History of allergy (see notes Oral liquid, Cloxacillin sodium 125 mg per 5 mL.
to report such symptoms. for injection in vials.
above); renal and hepatic impairment (Ap- POM BENCLOXA® (Nichben)
• Encourage patient to take adequate fluids if
POM Benzylpenicillin (EDL 5.3) pendices 4 and 5); heart failure; pregnancy Capsule, Cloxacillin sodium 500 mg
EMDEX
diarrhoea occurs.
Injection, Benzylpenicillin (as sodium or potassium and breastfeeding (Appendices 2 and 3); 500 mg – 10 x 10’s (in blisters)
Dose: Mild to moderate infections due to salt) 0.6 g (1 million units), 3 g (5 million units);
sensitive organisms, by IM injection or interactions: Appendix 1. POM CLOXACAP® (Hovid)
powder in vials.
by slow IV injection or by IV infusion, Adverse effects: Nausea and vomiting, diar- Capsules, Cloxacillin (as trihydrate) 250 mg, 500 mg.
ADULT 2.4–4.8 g daily in 4 divided POM BALITIN® (Vixa) rhoea; hypersensitivity reactions including 250 mg – 10 x 10 (blister)
Injection, Crystalline Penicillin. urticaria, fever, joint pain, rashes, angioedema, 500 mg – 10 x 10 (blister).
doses, with higher doses in severe
Pack: 10 vials/pack. anaphylaxis, serum sickness-like reactions,
infections (see also below); NEONATE POM Cloxacillin (Emzor)
under 1 week 50 mg/kg daily in 2 POM BENCRSTAL® (E-Globa) haemolytic anaemia, interstitial nephritis (see Capsule, Cloxacillin 250 mg
divided doses, 1 to 4 weeks 75 mg/ Injection, Benzyl penicillin (as potassium salt); white also notes above); neutropenia, thrombo- 250 mg – 100.
kg daily in 3 divided doses; CHILD 1 sterile crystalline powder for reconstitution. cytopenia, coagulation disorders; antibiot- Suspension, Cloxacillin 125 mg per 5 mL
Pack: 10’s (in vial) ic-associated colitis; hepatitis and cholestatic Pack: 60 mL.
month–12 years, 100 mg/kg daily in
4 divided doses, with higher doses in POM BENYCIN® (Beta Drugs) jaundice—may be delayed in onset; electrolyte POM Cloxacillin (Food & Pharma)
severe infections (see also below). Injection, Benzylpenicillin potassium 0.125 g disturbances; pain, inflammation, phlebitis or Dry syrup, Cloxacillin; powder for reconstitution.
Bacterial endocarditis, by slow IV injec- (200,000 i.u.)/vial; 0.25 g (400,000 i.u.)/vial; 0.313 g thrombo-phlebitis at injection sites. Pack: 60 mL; 100 mL.
tion or by IV infusion, ADULT 7.2–14.4
(500,000 i.u.)/vial; 0.5 g (800,000 i.u.)/vial; 0.625 g Advice to patients: Take 1 hour before or 2
(1,000,000 i.u.)/vial; white sterile crystalline powder, POM EMBACLOX® (Embassy)
g daily in 6 divided doses hours after meals;take the entire medication
which is very soluble in water. Capsule, Cloxacillin 500 mg.
Meningococcal disease, by slow IV as prescribed, do not skip doses. 500 mg – 100’s.
injection or by IV infusion, ADULT up POM CRYSGEN® (Geneith) Nursing action: Find out if patient is allergic
Injection, Benzylpenicillin sodium 1 mega unit. to penicillins; obtain specimen for C&S test; POM PAN Cloxacillin (Alpha)
to 14.4 g daily in divided doses; PRE- Injection, Cloxacillin sodium 500 mg; white to almost
MATURE INFANT and NEONATE under POM CRYSTAL Q® (Quadrant)
therapy may begin pending test result.
• Administer around-the-clock (in equal interval) to white powder in a colourless transparent vial with
1 week 100 mg/kg daily in 2 divided Infusion, Benzylpenicillin 1,000,000 IU (1 mega) blue cap.
lessen peak and trough levels.
doses; NEONATE 1–4 weeks 150 mg/ per vial Pack: 1 x 50’s
• Oral dose may cause GI upset and food may inter-
kg daily in 3 divided doses; CHILD POM Crystalline Penicillin (Pharmabox) fere with absorption, so give 1 to 2 hours before
1 month–12 years, 180–300 mg/kg Injection, Benzyl penicillin sodium 1,000,000 IU (eq. meals or 2 to 3 hours after. Shake suspension well FLUCLOXACILLIN
daily in 4–6 divided doses. to 0.6 G Benzyl penicillin); white crystalline powder before each dose. Therapeutic category: Penicillin antibiotic.
Suspected meningococcal disease for reconstitution. • Advise patient to take each dose with a full glass Indications: Treatment of infections caused
(before transfer to hospital), by IM Pack: 1’s (in vial) of water, not fruit juice or carbonated beverage, by Gram-positive organisms including penicil-
injection or by slow IV injection, because acid will inactivate the drug.
POM PEMAPEN® (Pemason) linase-producing staphylococci. They include
• Large dose and prolonged therapy may give rise to
ADULT and CHILD over 10 years, 1.2 g; Injection, Benzylpenicillin K 1,000,000 IU; white skin and soft tissue infections, bone infections,
superinfection; advise patient to report sore throat,
INFANT under 1 year, 300 mg; CHILD 1 crystalline powder in 5 mL vials.
fever and fatigue which indicate superinfection. respiratory tract/ENT infections and other
to 9 years, 600 mg. Pack: 5 mL x 10 x 10’s. infections such as endocarditis, meningitis,
• Advise patient to report immediately if rash, fever,
Neurosyphilis, by slow IV injection, POM SACOPEN® (GoldMoore) or chills occur. Rash is the most common allergic septicaemia.
ADULT 1.8–2.4 g every 4 hours for 2 Injection, Benzylpenicillin (as potassium) 0.12 g reaction. Contra-indications: History of penicillin
weeks. (200,000 i.u), 0.24 g (400,000 i.u), 0.3 g (500,000 Dose: Infections due to susceptible beta-lacta- hypersensitivity; should not be administered
Congenital syphilis, by slow IV injec- i.u), 0.48 g (800,000 i.u), 0.6 g (1000,000 i.u), 1.2 g mase-producing staphylococci, by subconjunctivally or as eye drops.
tion, CHILD up to 2 years, 30 mg/kg (2000,000 i.u), 3.0 g (5000,000 i.u). mouth, ADULT 250-500 mg every Adverse effects: Occasional rashes, transient
twice daily for the first 7 days of life, POM SALITIN® (Vixa) 6 hours, depending on severity of diarrhoea or indigestion.
Advice to patients, Nursing action: See under and to minimise GI distress, may be given 1-2 hours ture infections; Bacterial septicaemia; Bacterial angioedema, anaphylaxis, serum sickness-like
Cloxacillin. before or 2-3 hours after meals with a full glass of infections in neutropenic adults & children in reaction, haemolytic anaemia, interstitial
Dose: Adult, by mouth, 250 mg every 8 water NOT juice (Acid inactivates the drug). combination with an aminoglycoside; Appen- nephritis (see also notes above); neutropenia,
hours; increased to 500 mg every 6 • Tell patient to report any rash, fever or chills; rash dicitis complicated by rupture with peritonitis thrombocytopenia, coagulation disorders
is the most common allergic reaction.
hours in severe infections. and/or abscess formation in children. and CNS toxicity (associated with high doses
• Large doses and prolonged therapy may cause
Doses to be taken ½-1 hour before superimposed infection; advise patient to report Contra-indications: Hypersensitivity to and severe renal failure); Jarisch-Herxheimer
meals. sore throat, fever and fatigue which indicate penicillins, cephalosporins or b-lactamase reaction (during treatment for syphilis and
By slow IM injection, 250 mg every 8 superinfection. inhibitors. other spirochaete infections, probably due to
hours; increased to 500 mg every 6 • Encourage patient to take adequate fluids if Precautions: Perform periodic assessment release of endotoxins); rarely, non-allergic (em-
hours in severe infections. diarrhoea occurs of hematopoietic, renal & hepatic function. bolic-toxic) reactions; pain and inflammation
Add 1.5 mL water for injection to the • Renal and haematologic systems should be evalu- Pregnancy & lactation. at injection site.
250 mg vial. ated periodically during prolonged therapy. Interactions: Probenecid can prolong the Advice to patients: Notify physician if skin
By slow IV injection or infusion (3-4 Dose: Infections due to sensitive organisms, antibacterial effect. May reduce excretion rash, itching, hives, or severe diarrhoea occurs.
minutes), 250-500 mg every 4-6 by mouth, ADULT 500 mg every 6 of methotrexate. May prolong the action of Nursing action: Before administration, confirm
hours; may be increased up to 8 g hours increased up to 1 g every 6 neuromuscular blocking agents. that patient is not allergic to penicillins.
daily in severe infections. hours in severe infections; CHILD Adverse effects: Most commonly diarrhoea, • Obtain specimen for C&S test; therapy may begin
Dissolve 250-500 mg in 5-10 mL water up to 1 year, 62.5 mg every 6 hours; nausea, vomiting, and rash. pending test results.
for injection. CHILD 1–5 years, 125 mg every 6 Dose: Administration should be by slow IV • Give deep I.M. into a large muscle mass using
hours; CHILD 6–12 years, 250 mg the upper outer quadrant of buttocks in adults
Child, by any route, 0-2 years: ¼ adult injection (over at least 3-5 mins) or
every 6 hours. and midlateral thigh in small children. Avoid S.C
dose; 2-10 years: ½ adult dose. slow IV infusion (over 20-30 mins). route. Do not massage injection site. Rotate the
Alternatively, for children, 25-50 mg/ Secondary prophylaxis of rheumatic Adult & Children (>12 years): 2.25-4.5 injection site.
EMDEX
kg daily in divided doses; increased in fever, by mouth, ADULT 500 mg twice g 6-8 hourly. • Never give IV – inadvertent IV administration has
severe infections. daily; CHILD 1–5 years, 125 mg twice Neutropenia, 4.5 g given 6 hourly in caused death, due to CNS toxicity from procaine.
daily; CHILD 6–12 years, 250 mg twice combination with an aminoglycoside. • Tell patient to report any rash, fever or chills; rash
POM FLOXAPEN® (GSK) daily. Children (<12 years): Neutropenia, 90 is the most common allergic reaction; allergic
Capsules, Flucloxacillin (as Na+ salt) 250 mg, 500 mg Administration: Phenoxymethylpenicillin should
mg/kg 6 hourly, in combination with reactions are difficult to treat due to slow ab-
Syrup,Flucloxacillin (as Na+ salt) 125 mg, 250 mg per be taken at least 30 minutes before or 2 hours
an aminoglycoside; not exceeding 4.5 sorption rate.
5 mL; powder for preparing fruit flavoured syrup. after food. • Large doses and prolonged therapy may cause
Injection, Flucloxacillin (as sodium salt) 250 mg, 500 g 6 hourly.
POM Phenoxymethylpenicillin (WMF 6.2.1) superimposed infection; teach patient symptoms
mg; powder in vials. Complicated appendicitis, Child (2-12
Tablet, Phenoxymethylpenicillin (as potassium namely sore throat, fever fatigue and to report
years), 112.5 mg/kg 8 hourly; not such symptoms.
PHENOXYMETHYLPENICILLIN salt) 250 mg.
exceeding 4.5 g 8 hourly. • Renal and haematologic systems should be evalu-
Powder for oral liquid, Phenoxymethylpenicillin (as
Synonym: Penicillin V potassium salt) 250 mg/5 mL. Elderly: Adjust dose based on renal ated periodically during prolonged therapy.
Therapeutic category: Oral penicillin anti- function. • Encourage patient to have extra fluid intake if
biotic. POM Phenoxymethylpenicillin (EDL 5.3) Note: The above doses represent sum of piperacillin diarrhoea occurs.
Indications: Streptococcal pharyngitis; otitis Tablet, Phenoxymethylpenicillin (as potassium + tazobactam. Limit use in children to those with Dose: Infections due to sensitive organisms,
salt) 250 mg. neutropenia or complicated appendicitis. by deep IM injection, ADULT 0.6 to
media; cellulitis; mouth infections; secondary
Oral liquid, Phenoxymethylpenicillin 250 mg per
prophylaxis of rheumatic fever; post-splenec- POM TAZPEN® (Strides Vital) 1.2 g daily.
5 mL
tomy prophylaxis. Injection, Piperacillin 4 g, Tazobactam 500 mg; in vial Pneumonia, by deep IM injection
Contra-indications: Hypersensitivity to pen- POM Penicillin V Potassium (Embassy) Pack: 4.5 g x 1’s. CHILD 50 mg/kg daily for 10 days
icillins (see notes above); serious infections Tablet, Penicillin V Potassium 500,000 I.U. Syphilis, by deep IM injection, ADULT
POM ZOPETUM® (Canopus)
(see notes above). Injection, Piperacillin (as sodium salt) 4 g, Tazobac- 1.2 g daily for 10 to 15 days, or up to 3
PIPERACILLIN plus TAZOBACTAM weeks in late syphilis.
Precautions: History of allergy (see notes tam (as sodium salt) 500 mg; white to off white dry
above); pregnancy and breastfeeding (Appen- Therapeutic category: Penicillin antibiotic. powder for injection in 30 mL vial. Neurosyphilis, by deep IM injection,
dices 2 and 3); interactions: Appendix 1. Pharmacology: Piperacillin is a broad spec- Pack: 4.5 g x 1’s (in vials). ADULT 1.2 g daily (together with
Adverse effects: Hypersensitivity reactions in- trum, semisynthetic penicillin active against probenecid 500 mg 4 times daily by
cluding urticaria, joint pain, rash, angioedema, many gm+ve and gm-ve aerobic and anaerobic PROCAINE BENZYLPENICILLIN mouth) for 10–14 days.
anaphylaxis (see notes above); nausea and bacteria. It exerts bactericidal activity by inhi- Synonym: Penicillin G Procaine; Aqueous Congenital syphilis, by deep IM injec-
diarrhoea. bition of both septum and cell wall synthesis. Procaine Penicillin G, APPG; Procaine penicillin. tion, CHILD up to 2 years, 50 mg/kg
Advice to patients: .Take on an empty stom- Tazobactam is a penicillanic acid sulphone Therapeutic category: Penicillin antibiotic. daily for 10 days.
ach 1 hour before or 2 hours after meals; take derivative with potent b-lactamase inhibitory Indications: Syphilis; anthrax; pneumonia; Reconstitution and Administration: According to
until gone, do not skip doses; report any properties. In combination, tazobactam en- diphtheria; cellulitis; mouth infections; bites. manufacturer’s directions.
rash or shortness of breath; shake liquid well hances and extends the antibiotic spectrum Contra-indications: Hypersensitivity to peni- See also under the individual preparations below.
before use. of piperacillin to include many beta-lactamase cillins (see notes above); intravascular injection.
Nursing action: Obtain history of allergic producing bacteria normally resistant to it and Precautions: History of allergy (see notes POM Procaine benzylpenicillin (WMF 6.2.1)
reactions from patient. other beta-lactam antibiotics. above); renal failure (Appendix 4); breastfeed- Powder for injection, Procaine penicillin 1 g (= 1
Indications: Lower respiratory tract infec- million IU), 3 g (= 3 million IU); in vials.
• Obtain specimen for C&S test; therapy may begin ing (Appendix 3); interactions: Appendix 1.
pending test results. tions; UTIs (complicated and uncomplicated); Note: Procaine benzylpenicillin is not recommended
Adverse effects: Hypersensitivity reactions as first-line treatment for neonatal sepsis except in
• Give on an empty stomach for best absorption; Intra-abdominal infections; Skin and skin struc- including urticaria, fever, joint pains,rashes,
346 | 9.1.1.2 Cefalosporins 9.1.1.2 Cefalosporins | 347
settings with high neonata mortality, when given POM PROMACAIN® (Geneith) include Cefuroxime. upper and lower respiratory tract infections.
by trained health workers in cases where hospital Injection, Procaine penicillin 3 MIU, benzylpenicillin Note: Groups 3 corresponds to the 2nd-gen-
care is not achievable. 1 MIU.
Cefdinir shares similar structure and activity
eration. with Cefixime but is more active against
Procaine Penicillin Fortified POM PROPEN Q® (Quadrant) Cefuroxime is available as the sodium salt for Staphylococci.
Note: Procaine benzylpenicillin (aka, procaine Injection, Procaine penicillin 3,000,000 IU, penicillin injection and as the ester (Cefuroxime axetil)
penicillin) is a combination of benzylpenicillin with potassium (sodium) 1,000,000 IU per vial. Cefpodoxime is available as prodrug ester,
for oral use. The ester is rapidly hydrolyzed on Cefpodoxime proxetil which is hydrolyzed
the local anaesthetic agent procaine. The combina-
tion helps in reducing the pain caused by large IM POM REMPEN® (Strides Vital) passage through the intestinal mucosa to lib- in the small intestine to liberate the parent
injection of penicillin. It is hydrolysed after deep IM Injection, Fortified procaine penicillin 4 MU; in vials. erate cefuroxime. Food increases bioavailability compound. Food increases bioavailability, but
injection releasing benzylpenicillin slowly into the Pack: 100’s. by about 50%. antacids and H2-receptor antagonists reduce
circulation thereby prolonging its action. POM ROCAPEN® (Embassy) Clinical uses include urinary, soft-tissue and absorption. It is used mainly for the treatment
Procaine penicillin fortified is Procaine penicillin + Injection, Procaine penicillin fortified 3.6 m.u. pulmonary infections, as well as septicemia, of upper and lower respiratory tract infections
Benzylpenicillin potassium (or sodium). The fortified Pack: 50’s.
form can exert both the prompt action due to the
and as a single-dose treatment (with probene- in children and adults.
high initial concentration produced by the soluble POM SIVOCAINE® (Adpharm) cid) of gonorrhea due to β-lactamase-pro- •Group 6: Parenteral compounds with activity
benzylpenicillin potassium (or sodium) salt and the Injection, Benzylpenicillin, Procaine penicillin; in ducing strains. It has been widely used for against Pseudomonas aeruginosa. They vary
prolonged action of the insoluble procaine penicillin vials. surgical prophylaxis. Also indicated for surgical
Pack: 1 x 50’s. widely in their spectrum of activity against
salt which is hydrolysed slowly to benzylpenicillin. prophylaxis. other bacterial species. Available products
POM ELIUM® (Jubilee) 9.1.1.2 Cefalosporins •Group 4: Parenteral compounds with potent include Cefepime, Ceftazidime.
Injection, Procaine penicillin 3,000,000 I.U, penicillin antimicrobial activity and resistance to a wide Cefepime should be reserved for serious
potassium (or sodium) 1,000,000 I.U. The classification of cefalosporins by “genera- range of β-lactamases. Available products
Pack: 4,000,000 I.U. in vials. tions” is now being replaced by new grouping infections especially those involving resistant
include Cefotaxime, Ceftriaxone. Gram-negative organisms. Dose should be
EMDEX
POM FORTICAINE® (E-Globa)
outlined below: Note: Groups 4-6 correspond to the 3rd-gen- adjusted in renal impairment, but hepatic im-
Injection, Procaine penicillin fortified 3 g, Ben- •Group 1: Parenteral compounds of moderate eration. pairment does not affect the pharmacokinetic
zylpenicillin 1,000,000 IU; white dry powder for antimicrobial activity and susceptible to hy- Cefotaxime is available as the sodium salt properties.
reconstitution. drolysis by a wide variety of enterobacterial
Pack: 1 x 10’s; 100’s
for parenteral administration. It is widely Ceftazidime has antimicrobial activity profile
β-lactamases. Available products include distributed, achieving therapeutic concen-
Cefalotin, Cefazolin. similar to Cefotaxime. It is more active against
POM GLOPEN® (GoldMoore) trations in sputum, lung tissue, pleural fluid,
Injection, Procaine penicillin 3,000,000 I.U, penicillin Note: Groups 1 & 2 correspond to the 1st-gen- Ps. aeruginosa including gentamicin-resistant
peritoneal fluid, prostatic tissue and cortical strains but less active against Staph. aureus.
potassium (or sodium) 1,000,000 I.U. eration. bone. Superinfection with Ps. aeruginosa may Preparations containing arginine have replaced
Pack: 4,000,000 I.U. in vials
Group 1 has limited clinical use. Cefazolin is occur in the course of treatment. Used widely those with sodium carbonate making it less
POM LIFEFORT® (Justeen) used mainly in surgical prophylaxis, especially in neutropenic patients, respiratory infection,
Injection, Procaine benzylpenicillin fortified 4 m.u.
painful on IM injection. Used in combination
in biliary tract (because of the moderately high meningitis, intra-abdominal sepsis, osteomy- with an aminoglycoside, to treat a wide range
Pack: 1 x 10’s.
concentrations achieved in bile), orthopedic, elitis, typhoid fever, urinary tract infection, of severe urinary, respiratory and wound
POM LYREN® (Vixa) cardiac and gynecological surgery. neonatal sepsis and gonorrhea. infections, mostly due to enterobacteria or
Injection, Procaine Penicillin.
•Group 2: Oral compounds of moderate anti- The antimicrobial activity and clinical uses of Ps. aeruginosa.
POM NIXA-G® (Beta Drugs) microbial activity and moderately resistant to Ceftriaxone are similar to those of Cefotaxime. Note: Groups 4-6 correspond to the 3rd-gen-
Injection, Procaine penicillin 3,000.000 I.U., penicillin some enterobacterial β-lactamases. Available The long half-life of Ceftriaxone offers the ad- eration.
potassium (or sodium) 1,000.000 I.U.; in 4,000.000 products include Cefaclor, Cefadroxil, Ce- vantage of once-daily administration. It is used
I.U. vials. •Group 7: Compounds characterized by activity
falexin, Cefprozil. in the treatment of acute bacterial meningitis against methicillin-resistant staphylococci.
POM PAULIO® Fortified Procaine Penicillin (Pacmai) Note: Groups 1 & 2 correspond to the 1st-gen- and as an alternative to rifampicin (rifampin) Note: Some members of Groups 6 & 7 are of-
Injection, Benzylpenicillin sodium 1,000,000 I.U, eration. in the prophylaxis of meningococcal disease. ten referred to as the 4th and 5th generation
Procaine penicillin BP 3,000,000 I.U per vial.
Pack: 1 x 10’s in vials. Group 2 agents are used widely in treating •Group 5: Oral compounds (often achieved cefalosporins.
upper respiratory, urinary, soft tissue and var- by esterification) resistant to a wide range HYPERSENSITIVITY
POM PEMACAIN® (Pemason) ious other infections. They may also be used of β-lactamases. Most exhibit potent activ-
Injection, Procaine penicillin 4,000,000 units per 10 as alternatives in penicillin-allergic patients ity against enterobacteria; activity against Immediate allergic reaction (within 1 hour
mL; in 10-mL vial marked “Pemacain”.
for treating streptococcal, pneumococcal and Gram-positive cocci is variable. Available prod- of administration) may occur in 0.5–10% of
Pack: 10 mL x 10 x 10’s. patients treated with cefalosporins and is
staphylococcal infections. ucts include Cefdinir, Cefixime, Cefpodoxime.
POM Procaine Penicillin Fortified (Neimeth) Note: Groups 4-6 correspond to the 3rd-gen- usually characterised by flushing, urticaria,
Injection, Penicillin G Procaine crystalline 3 m.u.,
Cefaclor and Cefprozil are useful in respiratory angioedema, rhinitis, bronchospasm, and
infections because of their activity against H. eration.
buffered penicillin G potassium crystalline 1 m.u; anaphylactic shock. Delayed reactions may
powder in vial. influenzae. Cefadroxil and Cefalexin share Cefixime is an oral cefalosporin available as also develop from hours to days after admin-
4 m.u. – 50. similar antimicrobial activity profile and are the anhydrous compound or the trihydrate. istration and mostly consist of maculopapular
not suitable for use in H. influenzae infections. Oral absorption is slow and incomplete. rash, urticarial and/or angioedema.
POM Procaine Penicillin (Pharmabox)
Injection, Procaine penicillin 3 g (= 3 million IU), •Group 3: Parenteral compounds of moderate Achieves poor concentrations in the CSF even
in the presence of inflamed meninges. Activity Cross-allergy with penicillins may occur in
Benzyl penicillin 0.6 g (= 1 million IU); dry powder antimicrobial activity resistant to a wide range about 10% of patients, more commonly those
for reconstitution. of β-lactamases. Some are available as esters against Staph. aureus is poor. Effective for the
treatment of uncomplicated gonorrhoea, who react to a variety of drugs. Cefalosporins
Pack: 4 MU x 1’s (in vials). for oral administration. Available products should generally be avoided in patients with
history of IgE-mediated or serious reaction to • Large doses or prolonged therapy may cause extended-spectrum beta-lactamases (ESBL) Capsule, Cefadroxil 500 mg
penicillins. superinfection; monitor for signs and ask patient and chromosomal cephalosporinases, such as 500 mg – 12’s; 20’s
to report same. AmpC type enzymes. Oral suspension, Cefadroxil 125 mg, 250 mg, 500
References: • Monitor urine output; decreasing amount of urine mg per 5 mL.
1) Romano, A. Cephalosporin allergy: clinical Absorption is almost complete following oral
may indicate nephrotoxicity, notify physician Pack: 60 mL; 100 mL
manifestations and diagnosis. In: UpTo- administration, with or without food. Peak
Dose: By mouth, Adult, Bronchitis and pneu- POM ODOXIL® (Phillips/Lupin)
Date, Basow, DS (Ed), UpToDate, Waltham, concentrations are similar to those of cefalexin
monia, usually 750 mg in 2-3 divided Tablet, Cefadroxil USP equiv. to anhydrous Cefadroxil
MA, 2014. but plasma concentrations are more sustained.
doses daily. 1000 mg; extended release f-c tab.
2) Greenwood D. β-lactam antibiotics: About 20% bound to plasma proteins. Plasma
Sinusitis, 10-day treatment is recom- 100 mg – 5’s.
cefalosporins. In: Finch RG, Greenwood D, half-life is about 1.5 hours and is prolonged in
mended. Dry syrup, Cefadroxil 125 mg per 5 mL; powder for
Norrby SR, Whitley RJ, eds. Antibiotic and patients with renal impairment. reconstitution.
For more severe infections,or those
chemotherapy. 9th ed. Available from: Distributed widely to body tissues and fluids, Pack: 60 mL.
caused by less susceptible organisms,
www.clinicalkey.com (login required) but does not penetrate in the CSF and should Dry syrup (DS), Cefadroxil 250 mg per 5 mL; powder
the dose may be doubled.
not be used for treatment of meningitis. It for reconstitution.
Do not exceed total daily dosage of
CEFACLOR crosses the placenta and appears in breast milk. Pack: 60 mL.
4 g.
More than 90% excreted as unchanged drug in
Therapeutic category: Oral Cephalosporin Acute gonococcal urethritis in male and
the urine within 24 hours. CEFALEXIN
antibiotic (2nd Generation). female, a single dose of 3 g combined
Indications: Upper respiratory tract infections Synonym: Cephalexin
Indications: Bactericidal antibiotic which with Probenecid 1 g.
(acute and chronic otitis media and sinusitis, Therapeutic category: Cephalosporin antibi-
is active against both Gram-positive and CHILD: Usually 20 mg/kg/day in 2 di-
pharyngitis, tonsillitis, laryngitis); Lower respira- otic(1st Generation).
Gram-negative organisms including coag- vided doses; may be doubled in more
tory tract infections (acute and chronic bronchi- Indications: Cefalexin is a bactericidal anti-
ulase-positive, coaguluase-negative and severe infections or those caused by
tis, bronchopneumonia, bacterial pneumonia); biotic which is active against a wide range of
penicillinase-producing strains of staphyloc- less susceptible organisms.
EMDEX
Urogenital tract infections (uncomplicated gram-positive and gram-negative organisms.
coci and beta-lactamase-producing, ampicil- Note: Dosage adjustment in renal impairment may
not be necessary. and complicated urinary tract infections such Indicated for the following conditions, when
lin-resistant strains of haemophilus influenza
as cystitis, pyelonephritis, adnexitis, urethritis, caused by susceptible bacteria: Respiratory
among others. Indicated in both lower and POM CECLOR® (CHI/Eli Lilly) prostatitis, salpingitis); Skin and soft tissue tract infections; Ear, nose and throat infections;
upper respiratory tract infections such as acute Capsules, Cefaclor (as monohydrate) 250 mg, 375
infections (abscesses, furuncles, impetigo, Urinary tract infections; Gynaecological and
and chronic bronchitis, pharyngitis, tonsillitis, mg; white and purple caps.
pyodermia, erysipelas, lymphadenitis, wound obstetric infections; skin, soft-tissue and bone
pneumonia, sinusitis, etc.; skin and soft tissue 250 mg – 15’s.
375 mg – 10’s. infections); Bone and joint infections (osteo- infections; Gonorrhoea and in dental proce-
infections such as carbuncules, boils, impetigo;
Suspension, Cefaclor (as monohydrate) 187 mg per 5 myelitis). Not recommended for use in severe dures (as temporary replacement of penicillin
genito-urinary tract infections such as cystitis,
mL; strawberry flavoured granules for reconstitution. systemic infections in which β-lactamase-stable prophylaxis in patients with heart disease who
pyelonephritis, etc.; bone and joint infections
Pack: 50 mL multidose plastic bottle. cephalosporins are more effective. are undergoing dental treatment).
such as osteomyelitis; gonococcal urethritis.
Contra-indications, precautions, interac- Contra-indications, Precautions, etc: See
Contra-indications: Hypersensitivity to ceph- POM VERCEF® (Ranbaxy)
Capsule, Cefaclor 250 mg. tions, adverse effects: See under Cefalexin. under cefuroxime.
alosporin antibiotics.
250 mg – 5 x 3’s (in blister) Dose: By mouth, Adult (>40 kg with normal Advice to patients: See also under Cefuroxime.
Precautions: Hypersensitivity to penicillin;
Suspension, (125 mg), Cefaclor 125 mg per 5 mL; renal function), 1-2 g once daily or in Nursing action: Obtain specimens for C&S
pregnancy (use only if the benefits outweigh
granules for reconstitution. 2 equal divided doses per day; may tests prior to the first dose.
the risks). Pack: 100 mL. increase or double dose in severe • Administer on an empty stomach (i.e, 1 hour
Interactions: Loop diuretics, aminoglycosides Suspension, (250 mg), Cefaclor 250 mg per 5 mL; infections. Max. daily dose: 4 g. prior to, or 2 hours after meals) to increase total
(increased nephrotoxicity). granules for reconstitution. absorption; may give with meals to reduce GI
Children (<40 kg with normal renal
Adverse effects: Hypersensitivity reactions Pack: 100 mL. upset if needed.
function), 25-50 mg/kg once daily or
in about 1.5% of patients; pruritus, urticaria • Reconstituted oral suspension should be stored in
in 2 equal divided doses (at 12 hour
and positive Coomb’s test in less than 1 in 200 CEFADROXIL a refrigerator and should be used within 14 days;
intervals) per day; may increase in
patients. GI disturbances including diarrhoea Therapeutic category: Oral cephalosporin keep tightly closed and shake well before using.
severe infections up to 100 mg/kg. • Give around-the-clock in equal intervals to pro-
rarely occur. antibiotic (1st Generation). Duration: Treatment should be applied over 7 mote less variation in peak and trough serum
Nursing action: Obtain specimen for C&S tests Pharmacology: Cefadroxil is a 1st-generation to 10 days but in any case for 2 to 3 further days
before first dose; therapy may begin pending concentrations.
cephalosporin antibiotic that is the para-hy- after regression of the acute symptoms. Treatment • Teach patient to report sore throat, easy bruis-
test results. droxy derivative of cefalexin, and is used over at least 10 days is necessary in infections with ing, bleeding, joint pain; may be signs of blood
• Before administration, confirm that patient is not similarly in the treatment of mild to moderate Streptococcus pyogenes. dyscrasias.
allergic to cephalosporins or penicillins. Administration: May be taken with or without food,
susceptible Gram-positive and Gram-negative • Persistent diarrhoea may be sign of pseudomem-
• Administer capsule with meals if needed to de- give with food if GI upset occurs. The reconstituted
bacterial infections. It inhibits bacterial wall branous colitis; notify physician.
crease GI symptoms. suspension should be taken with a liberal quantity
synthesis of actively dividing cells by binding • With prolonged therapy monitor renal, hepatic,
• Reconstituted oral suspension should be stored in of fluid. Capsules and film-coated tablets should be
to one or more penicillin-binding proteins. and haematologic functions periodically.
a refrigerator and should be used within 14 days; swallowed whole without chewing, with lots of fluid.
keep tightly closed and shake well before using. The result is formation of a defective cell wall Dose: By mouth, 250 mg 6hourly or 500 mg
Additional information sourced from Cefadroxil monograph 8-12 hourly; increased to 1 g 8 hourly
• Dosage adjustment is necessary in renal im- that is osmotically unstable, and bacterial cell available from: http://www.medicines.org.uk/)
pairmemt. lysis. Has limited activity against some types or 1.5 g 6 hourly in severe or deep-
• Tell patient to take the entire medication as pe- of beta-lactamase (e.g. TEM-1) but it is inacti- POM BIODROXIL® (Novartis)
seated infections.
scribed, even after he feels better; to report any vated by beta-lactamases that can efficiently Tablet, Cefadroxil 1000 mg; f-c tab. Child: usually 25-60 mg/kg/day
skin rash, persistent diarrhoea. 1000 mg – 10’s; 12’s; 20’s increased to 100 mg/day (max. 4g/
hydrolyse cephalosporins, such as many of the
day) in chronic, severe or deep-seated 125 mg/5 mL – 100 mL pregnancy and breastfeeding (but appro- mg once daily depending on the
infections. 250 mg/5 mL – 100 mL priate to use, see Appendices 2 and 3); false type of infection. To be taken with or
0-1 year, 25-60 mg/kg/day; 1-2 years, POM CEPHAXIN® (Fidson) positive urinary glucose (if tested for reducing without food. Duration is between
62.5-125 mg 4 times daily or 125-250 Capsules, Cefalexin 250 mg, 500 mg. substances) and false positive Coombs’ test; 5-10 days depending on the severity
mg twice daily; 3-6 years, 125-250 Suspension, Cefalexin 125 mg per 5 mL. interactions: Appendix 1. of infection.
mg 4 times daily or 250-500 mg twice Pack: 60 mL; 100 mL. Adverse effects: Diarrhoea, nausea, rash, elec- Note: For adult patients with creatinine clearance
daily; 7-12 years, 250-500mg 4 times trolyte disturbances, cholestatic hepatitis, pain less than 30 mL/min, the dose should be 300 mg
POM CEPOREX® (GSK)
daily or 500 mg-1 g twice daily. and inflammation at injection site; antibiot- given once daily.
Tablet, Cefalexin 500 mg; pink f-c tab.
Note: For most acute infections, treatment should Suspension, Cefalexin 125 mg, 250 mg per 5 mL; dry ic-associated colitis; less commonly vomiting, POM RANICEF® (Fidson)
continue for at least two days after signs have granule for oral, orange-flavoured and coloured headache, dizziness, fever; rarely confusion Tablet, Cefdnir 300 mg
returned to normal and symptoms have subsided, suspension. (following large doses in renal impairment), 300 mg – 10’s
but in chronic, recurrent or complicated urinary tract Suspension, Cefdnir 125 mg, 250 mg per 60 mL
POM JULEXIN® (Juhel) arthritis, serum sickness-like syndrome, neu-
infection and Syhilis, treatment for two weeks (giving
1 g twice daily) is recommended. Tablet, Cefalexin 500 mg. rotoxicity including seizures, blood disorders POM RTIST® (Synergy)
500 mg – 100’s. (including neutropenia, eosinophilia, throm- Capsule, Cedinir 300 mg.
For gonorrhoea, a single dose of 3 g with 1 g Suspension, Cefalexin 125 mg per 5 mL; powder for bocytopenia, leucopenia, thrombocythaemia, 300 mg – 10’s.
probenecid for males or 2 g with 0.5 g probene- reconstitution. haemolytic anaemia, bleeding), renal impair- Oral suspension, Cedinir 125 mg per 5 mL; powder
cid for females is usually effective. Concurrent Pack: 100 mL. ment including interstitial nephritis, allergic for reconstitution.
administration of probenecid delays excretion POM KEFLEX® (CHI/Eli Lilly) reactions including urticaria, anaphylaxis, an- Pack: 60 mL.
of Cefalexin and raises the serum levels by Indications: Acute bacterial otitis media; Acute max-
Capsules, Cefalexin 250 mg; white and green cap. gioedema, and bronchial obstruction, abnor-
50-100%. illary sinusitis; Pharyngitis/tonsilitis; Uncomplicated
250 mg – 15. mal liver function tests; erythema multiforme skin and skin structure infections.
POM Axcel Cefalexin (Dortemag) Suspension, Cefalexin 125 mg per 5 mL; strawberry and toxic epidermal necrolysis also reported. Contra-indications, Precautions, etc: see under
EMDEX
Capsule, (250 mg), Cefalexin (as monohydrate) 250 flavoured granules for reconstitution. Dose: Surgical prophylaxis, by deep IM Cefixime.
mg; pink/ruby red cap. Pack: 100 mL.
injection, by IV injection (over at least Dose: Child, by mouth, all infections, 14 mg/kg; up
250 mg – 10 x 10’s; 100 x 10’s; 1000’s. POM PALITREX® (Mark) 3–5 minutes) or by IV infusion, ADULT to a max. dose of 600 mg per day.
Capsule, (500 mg), Cefalexin (as monohydrate) 500 Capsules, Cefalexin (as monohydrate) 250 mg, 500 1 g as a single dose at induction of Note: Once daily dosing for 10 days is as effective
mg; pink/rpurple cap. mg; light blue/dark blue cap. as BID dosing. In skin infections, twice daily dosing
anaesthesia, or after cord clamping
500 mg – 10 x 10’s; 50 x 10’s; 500’s. 250 mg – 16’s (in 2 blisters) should be used. May be administered without
Suspension, Cefalexin (as monohydrate) 125 mg per in caesarean section, repeated if
500 mg – 16’s (in 2 blisters) regard to meals.
5 mL; white granules which form beige susp. with necessary if surgery lasts over 3 Paediatric patients (6 mths-12 yrs):
Powder for oral suspension, Cefalexin (as mono-hy-
fruity flavour on reconstitution. drate) 250 mg per 5 mL; violet, vanilla and fruit hours; CHILD 25 mg/kg (maximum 1
Type of infection Dosage Duration
125 mg – 60 mL (in glass bottle). flavoured suspension. g dose) as a single dose at induction
Acute bacterial otitis 7mg/kg q 12 h or
Pack: 100 mL. of anaesthesia, repeated if necessary media 14mg/kg q 24 h
5 to 10 days
POM CEFAMOR® (Interpharma)
Capsule, Cefalexin 500 mg. if surgery lasts over 3 hours. Acute maxilliary 7mg/kg q 12 h or
POM SPORIDEX® (Ranbaxy) Note: Further doses may be given every 6–8 hours 5 to 10 days
500 mg – 5 x 20’s. sinusitis 14mg/kg q 24 h
Capsules, Cefalexin 250 mg, 500 mg. postoperatively for 24 hours if necessary, or for up
Suspension, Cefalexin 125 mg per 5 mL; dry granules 7mg/kg q 12 h or
250 mg – 24 x 10’s; 24 x 20’s (blister). to 5 days in continued risk of infection (consult
Pharyngitis/Tonsilitis
14mg/kg q 24 h
5 to 10 days
for oral suspension. 500 mg – 24 x 10’s; 24 x 20’s (blister).
Pack: 100 mL. manufacturer’s literature). Uncomplicated skin &
Suspension (125 mg), Cefalexin 125 mg mg per 5 mL 7mg/kg q 12 h 10 days
Reconstitution and Administration: According skin structure
POM CEFASIL® (Crystal) Pack: 60 mL; 100 mL. to manufacturer’s directions; intramuscular ad-
Capsule, Cefalexin 500 mg. Suspension, (250 mg), Cefalexin 250 mg per 5 mL. ministration may be painful and should be avoided CEFEPIME
Pack: 10 x 10’s. Pack: 60 mL; 100 mL. where possible.
Paediatric Drops, Cefalexin 100 mg per mL Therapeutic category: Cephalosporin antibi-
POM CEFF® (Phillips) Pack: 10 mL. POM Cefazolin (WMF 6.2.1) otic, parenteral (4th Generation).
Capsules, Cefalexin 250 mg, 500 mg Powder for injection, Cefazolin (as sodium salt) 1 Pharmacology: Cefepime is a bactericidal
250 mg – 10’s CEFALOTIN g; in vial. agent that acts by inhibition of bacterial cell
500 mg – 10’s. wall synthesis. It binds to one or more of the
Syrup, (Forte), Cefalexin 250 mg per 5 mL; dry pow- POM CELLOZINA® (Strides Vital)
POM CEFLEN® (Strides Vital) penicillin-binding proteins (PBPs) which in
der for reconstitution. Injection, Cefazolin 1 g; in vial.
Injection, Cefalotin 1 g; in vial. turn inhibits the final transpeptidation step of
250 mg – 100 mL.
Dry syrup, Cefalexin 125 mg per 5 mL; dry powder CEFDINIR peptidoglycan synthesis in bacterial cell walls,
CEFAZOLIN
for reconstitution. Description: Cefdinir is a semi-synthetic, thus inhibiting cell wall biosynthesis. Bacteria
Therapeutic category: Cephalosporin antibi- eventually lyse due to ongoing activity of cell
125 mg – 100 mL. broad-spectrum 3rd generation cefalosporin
otic (1st Generation). wall autolytic enzymes (autolysis and murein
POM CELEXIN® (Hovid) Indications: Prophylaxis of infection in sur- (Group 5).
See under preparations below. hydrolases) while cell wall assembly is arrested.
Tablets, Cefalexin 250 mg, 500 mg; f-c tabs. gery; see notes above.
250 mg – 40; 100. Indications: Community acquired pneumonia; It is highly resistant to hydrolysis by most
Contra-indications: Cephalosporin hypersen- beta-lactamases and has a broad spectrum
500 mg – 40; 100. Acute exacerbation of chronic bronchitis; Up-
Suspension, Cefalexin 125 mg per 5 mL; dry granules
sitivity (see section 9.1.1). of in vitro activity covering a wide range of
Precautions: Sensitivity to beta-lactam per respiratory tract infections (Acute maxillary
for oral susp. sinusitis, Pharyngitis and Tonsillitis); Skin and gram-positive and gram-negative bacteria.
antibacterials (avoid if history of immediate Absorption via IM is rapid and complete.
POM CEPHAFLASH® (Miraflash) hypersensitivity reaction—see section 9.1.1); soft tissue infections.
Oral suspension, Cefalexin 125 mg, 250 mg per 5 mL; Dose: Adult recommended dose varies from It crosses blood-brain barrier; attains high
moderate renal impairment (Appendix 4); concentrations in the inflammatory fluid and
powder for reconstitution. either 300 mg every 12 hours or 600
bronchial mucosa. Undergoes minimal hepatic 7-21 days; usually longer courses are Pack: 1 vial containing dry powder + 1 amp of Dry syrup, Cefixime (as trihydrate ) 50 mg per 5 mL;
metabolism and is excreted mainly in the urine required if Pseudomonas and shorter sterile WFI. dry powder for reconstitution.
as unchanged drug. Elimination half-life is 2 duration (7-10 days) in absence of Pack: 30 mL.
POM ULTIME® (Micronova)
hours and time to peak effect is 1-2 hours (IM) Pseudomonas. Injection (250 mg), Cefepime (as HCl with L-Arginine) POM BIOXIME® (Biofem)
and 0.5 hour (IV). Community-acquired (including pseu- 250 mg in vials Capsule, Cefixime 200 mg; white to slightly yellow
Indications: Treatment of nosocomial and domonal), by IV injection, 1-2 g every Injection (500 mg), Cefepime (as HCl with L-Arginine) powder in a yellow cap.
community-acquired pneumonia caused by 12 hours for 10 days. 500 mg in vials 200 mg – 6’s
Streptococcus pneumoniae, Pseudomonas aerug- Complicated and uncomplicated Injection (1 g), Cefepime (as HCl with L-Arginine)
POM BIOXIME-P® (Biofem)
1 g in vials
inosa, Klebsiella pneumoniae, or Enterobacter urinary tract infections (mild-to-mod- Granules, Cefixime 50 mg; granules for suspension
Pack: Vials of 250 mg; 500 mg; 1 g
species, methicillin-susceptible Staphyloccoci, erate), by IM or IV injection, 0.5-1 g in sachet
Haemophilus catarrhalis; complicated urinary every 12 hours for 7-10 days; Severe: 50 mg – 12’s
CEFIXIME
tract infections, including pyelonephritis caused by IV injection, 2 g every 12 hours for POM CEFIRAZ-D® (Diamond Remedies)
by E. coli, Klebsiella pneumoniae, or Proteus mi- 10 days. Indications: Uncomplicated gonorrhoea,
Tablet, Cefixime (as trihydrate) equiv. to Cefixime
rabilis; skin and skin structure infections caused Uncomplicated skin and skin structure upper and lower respiratory tract infections.
(anhydrous) 200 mg; lake of sunset yellow.
by Streptococcus pyogenes or methicillin-sus- infections (moderate to severe), by IV Contra-indications: Cefalosporin hypersensi- 200 mg – 1 x 10’s; 10 x 1 x 10’s
ceptible Staphylococci, other beta-haemolytic injection, 2 g every 12 hours for 10 tivity (see section 9.1.1).
Precautions: Sensitivity to beta-lactam POM CEFIZIM® (Reals)
species; complicated intra-abdominal infections days. Tablet, Cefixime (as trihydrate) 200 mg; f-c tab.
including peritonitis and biliary tract infections Complicated intra-abdominal infec- antibacterials (avoid if history of immediate
Pack: 1 x 4’s; 1 x 10’s; 2 x 10’s; 10 x 10’s.
(in combination with metronidazole) caused tions (in combination with metroni- hypersensitivity reaction—see section 9.1.1); Indications: Treatment of respiratory tract infections
by E. coli, sensitive P. aeruginosa, K. pneumoniae, dazole), by IV injection, 2 g every 12 moderate renal impairment (Appendix 4); (pharyngitis, tonsillitis, acute bronchitis, acute exac-
Enterobacter species, or Bacteroides fragilis. hours for 7-10 days. pregnancy and breastfeeding (but appro- erbation of chronic bronchitis, otitis media, sinusitis);
EMDEX
Contra-indications: Hypersensitivity to Dosage adjustment in renal dysfunction (Cre- priate to use, see Appendices 2 and 3); false Urinary tract infections (acute uncomplicated cysti-
cefepime, other cephalosporins, penicillins, atinine clearance ≤60 mL/min): Dosage should positive urinary glucose (if tested for reducing tis, gonococcal urethritis) and biliary tract infections.
substances) and false positive Coombs’ test; Dose: Adult & Child >12 years, 400 mg daily, given
other beta-lactam antibiotics, or any compo- be adjusted to compensate for the slower rate either as a single dose or in 2 divided doses.
nent of the formulation. of renal elimination. The recommended initial interactions: Appendix 1.
Adverse effects: Diarrhoea, nausea and Child: 8 mg/kg daily administered as single
Precautions: History of penicillin allergy espe- dose should be the same as in patients with dose or in 2 divided doses.
cially IgE-mediated reactions (eg, anaphylaxis, normal renal function. The recommended vomiting, abdominal discomfort, headache;
Child (<6 months): Not recommended.
angioedema, urticaria); Superinfection includ- maintenance doses in adult patients with renal rarely, antibiotic-associated colitis (particu- Child weighing >50 kg or >12 years should
ing C. difficile-associated diarrhea (CDAD) insufficiency are summarized in below larly with higher doses); allergic reactions be treated with the recommended adult
and pseudomembranous colitis, especially including rashes, pruritus, urticaria, serum dose. The usual course of treatment is
Creatinine
in patients on prolonged treatment; History Clearance (mL/ Recommended Maintenance Schedule sickness-like reactions, fever and arthralgia, 7-14 days
of gastrointestinal disease, especially colitis; min) and anaphylaxis; erythema multiforme, toxic Dosage in Renal impairment:
Adjust dosage in renal impairment (CrCl ≤60 >60 (normal epidermal necrolysis reported; transient hep- Creatinine clearance Dose
500 mg
mL/minute) due to increased risk of enceph-
recommended
q12h
1 g q12h 2 g q12h 2 g q12h atitis, cholestatic jaundice; eosinophilia and * >60 mL/min Normal dose
dosing schedule)
alopathy, myoclonus, and seizures; History of blood disorders (including thrombocytopenia,
500 mg * 21-60 mL/min or on 75% standard dose
seizure disorder, especially with renal impair- 30-60 1 g q24h 2 g q24h 2 g q24h leucopenia, agranulocytosis, aplastic anaemia haemodialysis (i.e., 300 mg daily)
q24h
ment; Pregnancy, Breast-feeding. and haemolytic anaemia); reversible interstitial
500 mg 500 mg * 20 mL/min or on 50% standard dose
11-29 1 g q24h 2 g q24h nephritis, hyperactivity, nervousness, sleep
Interactions: Cephalosporins (4th Generation) q24h q24h peritonealdialysis (i.e., 200 mg daily)
may enhance the nephrotoxic effect of Amino- 250 mg 250 mg 500 mg disturbances, hallucinations, confusion, hyper-
<11 1 g q24h Standard dosing interval is recommended.
glycosides (monitor renal function); Cephalo-
q24h q24h q24h tonia, and dizziness.
(Additional information sourced from Cefepime monograph Dose: Uncomplicated anogenital gonorrhoea, POM CEFIZIM® (Reals)
sporins may enhance the anticoagulant effect http://www.uptodate.com/) Oral Suspension, Cefixime USP equiv. to anhydrous
of Vitamin K Antagonists (e.g., Warfarin); Antibi- by mouth, ADULT 400 mg as a single
dose. Cefixime 50 mg per 5 mL; powder for reconstitution
otics may diminish the therapeutic effect of live POM CEFEPEN® (Strides Vital) Pack: 50 mL.
attenuated typhoid vaccine (Ty21a) (postpone Injection, Cefepime 1 g; in vial. POM Cefixime (WMF 6.2.1)
Capsule, Cefixime 400 mg. POM DAXIMIN® (Dabak)
vaccination for at least 24 hours after cessation POM CIFZAR® (Shrezar) Tablets (Dispersable), Cefixime (as trihydrate) 100
of antibacterial therapy). Injection, Cefepime (as HCl) 1 g per vial POM ARCERIN® (JB Pharma) mg, 400 mg; f-c tabs.
Adverse effects: Diarrhea, nausea, vomiting; Pack: 1 vial with 10 mL diluent Tablet, Cefixime (as trihydrate) 400 mg; f-c tab 100 mg – 10’s (in blisters).
Local pain, phlebitis and inflammation at the 400 mg – 1 x 10’s 400 mg – 7’s (in blisters).
POM GATRID® (Nosak)
site of injection; Skin rash, pruritus; Headache,
Injection, Cefepime (as HCl with L-Arginine) 250 mg, POM BIOTAX-O® (Olpharm) POM FIXIME® (Pharmgate)
fever, dizziness; Elevations in hepatic enzymes. 1000 mg; dry powder for reconstitution in vials. Tablet, (100 mg), Cefixime (as trihydrate) 100 mg; Tablets, Cefixime 100 mg, 400 mg.
Less frequently, anaphylaxis, colitis, oral dispersible tab. 100 mg – 1 x 10’s.
thrush, seizures, urticaria, vaginitis, electrolyte POM NOVAPIME® (Phillips/Lupin)
100 mg – 10’s 400 mg – 1 x 10’s.
changes; Transient elevations of blood urea Injections, Cefepime 500 mg, 1 g; powder for recon-
Tablet, (200 mg), Cefixime (as trihydrate) 200 mg;
stitution in vials. POM GIXIM® (Greenlife)
nitrogen, serum creatinine, bilirubin; throm- uncoated tab.
Pack: 1’s + sterile water for injection. Tablet, Cefixime (as trihydrate) 200 mg.
bocytopenia, encephalopathy, decreased 200 mg – 10’s
Paediatric tablet, Cefixime (as trihydrate) 50 mg; 200 mg – 1 x 10’s.
haematocrit. POM Q-PIME® (Phillips)
Injection, Cefepime HCI (sterile) equiv. to Cefepime dispersible tab. POM GRAMOCEF-O® (Micronova)
Dose: Adult, Pneumonia (Nosocomial), by IV
1 g, 2 g per vial 50 mg – 10’s Capsule, Cefixime (as trihydrate) 100 mg, 200 mg,
injection, 1-2 g every 8-12 hours for
400 mg. 200 mg – 10’s (cephalosporinases that are poorly inhibited by gitis. Treatment or prophylaxis of infections in
100 mg – 10's Suspension, Cefixime (as trihydrate) 100 mg per 5 beta lactamase inhibitors) producers are 100% patients with reduced resistance.
200 mg – 10’s. mL; dry powder for reconstitution. resistant to cefixime and the combination. Contra-indications: Hypersensitivity to ceph-
400 mg – 10’s. Pack: 50 mL. Oral absorption of cefixime is about 40-50%, alosporins.
Oral suspension, Cefixime (as trihydrate) 50 mg, 100
POM ZOFIXIME® (Zolon) with or without food. Eliminated mainly as Precautions: Penicillin hypersensitivity, severe
mg per 5 mL; powder for reconstitution.
Suspension, Cefixime (anhydrous) 100 mg per 5 mL. unchanged drug in the urine. Serum protein renal failure, pregnancy, breast feeding.
Pack: 100 mL.
Pack: 100 mL. binding is approximately 30%. Interactions: Loop diuretics, aminoglycosides
POM IXIME® (Phillips/Lupin) Dose: Children: The recommended dose is 8 mg/kg/ Indications: Respiratory tract infections e.g. (increased nephrotoxicity). Probenecid may
Tablet, Cefixime USP equiv. to anydrous Cefixime day of the suspension. This may be adminis-
bronchitis, bronchiectasis, pneumonia; ENT decrease cephalosporin elimination.
400 mg; f-c tab. tered as a single dose or may be given in two
400 mg – 1 x 6’s. divided doses as 4 mg/kg every 12 hours
infections; Chronic maxillary sinusitis; Chronic Adverse effects: See under Cefuroxime.
otitis media; Urinary tract infections; Acute • Nursing action: Give IV after diluting in NS, D5W, or
Oral suspension, Cefixime USP equiv. to anhydrous Pediatric dosage chart
uncomplicated and complicated urinary tract sterile H2O for inj as ordered; confirm that patient
Cefixime 100 mg per 5 mL; powder for reconsti- Patient wt. Dose/Day Dose/day Dose/Day
infection. is not allergic to cephalosporins or penicillins
tution. (kg) mg mL tsp of susp.
prior to use.
Pack: 60 mL. 6.25 50 2.5 ½ Contra-indications: Hypersensitivity to ceph-
• Check injection site for induration, sterile abscess
Indications: Uncomplicated UTIs; Otitis media; 12.5 100 5 1 alosporin antibiotics. and tissue sloughing; change site every 3 days.
Pharyngitis and Tonsilitis; (Note: Penicillin is the 18.75 150 7.5 1½ Precautions: Hypersensitivity to penicillins; • Do not admix with aminoglycosides in same
usual drug of choice in the treatment of S. pyogenes 25 200 10 2
Superinfection leading to overgrowth of
31.25 250 12.5 2½ bottle/bag.
infections, including the prophylaxis of rheumatic
37.5 300 15 3 clostridia and antibiotic-associated diarrhoea. • Teach patient to report sore throat, easy bruis-
fever. Cefixime is generally effective in the eradica-
tion of S. pyogenes from the nasopharynx, however, Children weighing more than 50 kg or older Pregnancy, lactation. ing, bleeding, joint pain; may be signs of blood
than 12 years should be treated with the Adverse effects: Diarrhoea, stool changes, dyscrasias.
data establishing the efficacy of cefixime in the
recommended adult dose. nausea, abdominal pain, dyspepsia, vomiting • Decreasing amount of urine may indicate nephro-
subsequent prevention of rheumatic fever are not
EMDEX
Reconstitution directions for oral suspension: and flatulence, headache, dizziness, allergies in toxicity, notify physician; discontinue drug if severe
available). Acute bronchitis and acute exacerbations
Method – Tap the bottle several times to loosen diarrhoea occurs, may indicate pseudomembra-
of chronic bronchitis; Uncomplicated multi drug the form of rash, pruritus, drug fever, arthralgia,
powder contents prior to reconstitution. Initially, nous colitis.
resistant and quinolone resistant typhoid fever; including rare cases of urticaria or angioedema,
add some water below the mark on the bottle and • Observe for signs and symptoms of anaphylaxis
Uncomplicated gonorrhea (cervical/urethral). erythema multiforme, Stevens-Johnson syn-
shake well. Then, adjust the volume up to the mark during first dose.
Dose: Adult (>50 kg or >12 years), by mouth, drome, thrombocytosis, thrombocytopenia,
on the bottle by adding more water. After mixing, • Monitor closely for signs of superinfection.
400 mg once daily or every 12 hours.
the suspension may be kept for 14 days at room tem- leucopenia, hypereosinophilia, neutropenia. Dose: Adult, by IM or IV injection, 1 g 12
Uncomplicated cervical/urethral gonoccocal
infections, 400 mg as a single oral dose. perature or under refrigerator without significant aqranulccytcsis, transient rises in liver transam- hourly; up to a max. 12 g daily in 3-4
Child: 8 mg/kg/day as a single dose or in 2 loss of potency. Keep the bottle tightly closed. Shake inases, alkaline phosphatase and jaundice can doses.
divided doses, as 4 mg/kg every 12 hours. well before use. Dicard unused portion after 14 days. also occur. Gonorrhoea (males and females), 1 g
Uncomplicated multidrug resistant and Tablet, Cefixime 400 mg. Dose: Adults and Children over 10 years, by IM as single dose.
quinolone resistant typhoid fever in children, 400 mg – 1 x 10’s (in blisters) mouth, One tablet twice daily; usually Premature babies and Newborns: 50
20 mg/kg/24 hours in divided BID doses Dose: Children up to 12 years: Usually 8 mg/kg/day for 7-14 days. mg/kg daily in 2 doses.
for 7 days. given as a single dose or in two divided
doses. Not recommended for use in children References: Infants and children: 50-100 mg/kg
POM NEFIXIME® (Nectar Healthcare) aged less than 6 months. 1) Deepti R, Deepthi N. Extended-spectrum daily in 2-4 doses; up to a max. 200
Tablet, Cefixime (as trihydrate) 400 mg; f-c tab. ß-lactamases in gram negative bacteria. mg/kg daily in 3-4 doses.
400 mg – 10’s POM ZOOCEF® (Zoomota)
Tablets, Cefixime (as trihydrate) 100 mg, 200 mg; Journal of Global Infectious Diseases; POM CEFOMIC® (L.B.S.)
Oral suspension, Cefixime (as trihydrate) 100 mg per
5 mL; dry powder for reconstitution. uncoated dispersible cream tabs. 2010 Aug 17. Available from: http://www. Injections, Cefotaxime (as sodium salt) 500 mg, 1 g;
Pack: 60 mL 100 mg – 1 x 10’s (alu-alu strip) jgid.org/article.asp?issn=0974-777X;- powder in vials with water for injection as diluent.
200 mg – 1 x 10’s (alu-alu strip) year=2010;volume=2;is- Pack: 1.
POM OCEFIX® (Swipha) Suspension, Cefixime (as trihydrate) 100 mg per 5 sue=3;spage=263;epage=274;aulast=Ra-
Tablets, Cefixime (as trihydrate) 200 mg, 400 mg; POM CEFOTAMAX® (Strides Vital)
mL; dry powder for reconstitution. wat Injection, Cefotaxime 1 g.
f-c tabs. Pack: 50 mL.
200 mg – 10’s POM GRAMOCEF-CV® (Micronova) Pack: 1 g (in vial)
400 mg – 10’s Tablet, Cefixime (as trihydrate) 200 mg, diluted Potas- POM Cefotaxime (Jawa)
CEFIXIME plus CLAVULANIC ACID
Dry syrup , Cefixime (as trihydrate) 100 mg per 5 mL; sium clavulanate equiv. to Clavulanic acid 125 mg. Injection, Cefotaxime 1 g
dry powder for reconstitution. Pharmacology: Extended spectrum be- Pack: 1 x 10’s Pack: 10’s
Pack: 50 mL ta-lactamases (ESBLs) limit the efficacy of
ß-lactams. including extended-spectrum ceph- CEFOTAXIME POM Cefotaxim Panpharma (Alpha)
POM SPORFIX® (Nomedi) Injection, Cefotaxime sodium 500 mg, 1000 mg
Capsule, Cefixime (as trihydrate) 400 mg
alosporins. Deepti et al showed that the activity Therapeutic category: Cephalosporin antibi-
400 mg – 5’s; 6 x 10’s. of extended-spectrum cephalosporins against otic (3rd Generation). POM CLAFORAN® (May & Baker)
Dry suspension, Cefixime (as trihydrate) 100 mg per ESBL-producing organisms is enhanced by the Indications: Infections of the respiratory Injections, Cefotaxime (as sodium salt) 500 mg, 1 g;
5 mL; powder for reconstitution. presence of clavulanic acid. The combination powder in vials with water for injection.
tract; kidneys; urinary tract and reproductive
Pack: 30 mL (in PET bottle with plastic P.P. cap). of Cefixime and Clavulanate has the advantage organs including gonorrhoea; bones, joints, POM EFTAX® (Quadrant)
POM ZEFI® (Nosak) of oral administration and offers an out-patient soft tissues and skin such as infected burns Injection, Cefotaxime (as sodium salt) 0.5 g, 1 g or
Tablets, Cefixime (as trihydrate) 100 mg, 200 mg; treatment option for uncomplicated commu- and wounds; ear, nose and throat. Abdominal 2 g per vial.
uncoated dispersible tabs. nity acquired infections caused by non-AmpC Directions for use: IM injection: 500 mg vial – dilute
Infections; infections in gynaecology and
100 mg – 10’s ESBL producing gram negative bacteria. AmpC with 2 mL of aqueous dilute and shake vigorously.
obstetrics; septicaemia, endocarditis, menin- IV injection: Normally given by slow IV injection. 500
mg – dissolve in 10 mL of water for injection by first structure infections. Tablet, Cefpodoxime 100 mg; f-c tab.100 mg – 10’s abdominal pain, mild diarrhea, and nausea/
dissolving the contents of the vial in approx. 3 mL Contra-indiations, Precautions, etc: see (in blisters) vomiting; Overgrowth by non-susceptible
of the water for injection and then withdrawing the under Cefixime. Suspension, Cefpodoxime 40 mg per 5 mL; granules bacteria or fungi. Transient elevation of
dissolved contents into a 10 mL syringe containing Dose: Adults (age 13 years and olderly): for reconstitution. hepatic enzymes. Rarely allergic reactions,
the remaining water for injection. Pack: 50 mL; 100 mL.
Total dai- seizures; haematological reactions e.g. mild
IV infusion: Vial contents should be dissolved in ly dose
Dose Freq Duration
POM TAMBAC® (Interpharma) eosinophilia, leukopenia, and neutropenia.
a suitable volume of fluid and given as a rapid IV
Acute community 12 Dry syrup, Cefpodoxime (as Proxetil) 50 mg per 5 mL. IM administration may cause pain, temper-
infusion over 30 mins or suitably diluted into the acquired pneumonia
400 mg 200 mg
hours
14 days
Pack: 60 mL ature elevation or tenderness while IV or IM
drip tubing. Solutions must be used within 30 mins
Acute bacterial exc-
of preparation. erbations of chronic 400 mg 200 mg
12
10 days POM VISKOBACT® (Visko) administration may produce local swelling,
hours
POM FOTARAN® (Pharmabox) bronchitis Tablet, Cefpodoxime proaxetil 200 mg. inflammation, burning, paresthesia, phlebitis
Injection, Cefotaxime sodium USP 1 g; white or
Uncomplicated or thrombophlebitis.
gonorrhea (Men and
light-yellowish crystalline powder in vial + 4 mL women) and rectal 200 mg Single dose
CEFRADINE Dose: Adult, by deep IM injection or slow
water for injection in ampoule. gonococcal infections Synonym: Cephradine IV injection (over 3-5 mins) or by IV
(women)
Pack: 1’s; 5; 10’s; 20’s; 50’s; 100’s (plus water for Therapeutic category: Cephalosporin antibi- infusion, 0.5 – 1 g every 6 hours; may
12
injection in amouples) Skin & skin structure 800 mg 800 mg
hours
7-14 days otic, 1st Generation. increase frequency to 4-hourly or in-
POM KLAFOMED® (Embassy) Pharyngitis and
200 mg 100 mg
12
5-10 days
Pharmacology: Cefradine is a first-generation crease dose in severe infection. Max.
tonsilitis hours dose: 8 g per day.
Injection, Cefotaxime sodium 1 g. cephalosporin antibiotic available in both oral
Uncomplicated uri- 12 Renal impairment: Adjust dose as follows:
Pack: 1’s.
nary tract infection
200 mg 100 mg
hours
7 days and injectable forms. The antibacterial spec-
trum and susceptibility to β-lactamases are Creatinine Clearance >20 mL/min: 500 mg
POM NITAXIM® (Mark)
Child (2 months – 12 years): 8-10 mg/ almost identical to those of cefalexin. It acts by every 6 hours.
Injection, Cefotaxime 250 mg, 500 mg, 1 g.
kg b.wt in two divided doses for 5-10 inhibiting the third and final stage of bacterial Creatinine Clearance 5 – 20 mL/min: 250 mg
EMDEX
POM NICOL® (Justeen) days. every 6 hours.
cell wall synthesis by preferentially binding
Injection, Cefotaxime 1 g. Acute otitis media, 5 mg/kg q12h to specific penicillin-binding proteins (PBPs) Creatinine Clearance <5 mL/min: 250 mg every
Pack: 1’s. for 5 days; Max. 200 mg/dose or 400 located inside the bacterial cell wall. Gener- 12 hours.
POM NITAXIM® (Mark) mg/day. ally, first-generation cephalosporins are more Patients on chronic, intermittent hemodialysis:
Injection, Cefotaxime (as Na) 1 g. Pharyngitis and/or tonsillitis, 5 mg/kg active against gram-positive organisms than 250 mg initially, repeat at 12 hours and after
Pack: 1 g (in vial) + 5 mL diluent q12h for 5-10 days; Max. 100 mg/dose 36 – 42 hours.
are 2nd– and 3rd-generation cephalosporins,
POM ORITAXIM® (Interpharma) or 200 mg/day. but they have relatively little activity against Administration: For IM injection: Add 2 mL of dilu-
Injection, Cefotaxime (as Na) 1000 mg. Acute maxillary sinusitis, 5 mg/kg gram-negative species. Clinical use is similar ent to each 500 mg vial or 4 mL of diluent to each 1
Pack: 1’s (in vial) q12h for 10 days; Max. 200 mg/dose g vial; use Sterile Water for Injection (SWI) as diluent.
to that of cefalexin, but it has been largely
or 400 mg/day. For IV injection: Direct IV: Add 5 mL of diluent to each
POM REFTAX® (Ranbaxy) superseded by later cephalosporins. 500 mg vial or 10 mL of diluent to each 1 g vial; use
Injections, Cefotaxime (as Na) 1 g, 2 g; powder for POM CEFADOX® (Micronova) Almost completely absorbed orally. A 500 mg SWI, D5W; NaCl Injection as diluent.
reconstitution in vials. Tablets, Cefpodoxime (proxetil) 100 mg, 200 mg. oral dose achieves a concentration of about Inject slowly over 3-5 minutes or give through tubing.
1 g – 10’s 100 mg – 10’s. 18–20 mg/L after 1 hour (vs 10–12 mg/L Continuous or Intermittent IV Infusion: Add 10-20
2 g – 10’s. 200 mg – 10’s. achieved by 1g IM dose within 2 hours). The mL of SWI or a suitable infusion fluid to each 1 g
POM TOX® (Embassy) POM CEFDOXIM® (Digitall) peak is delayed and reduced by food, but the vial, to prepare solution. Withdraw entire contents;
Injection, Cefotaxime 1 g. Tablet, Cefpodoxime proxetil 200 mg. half-life is not altered. The plasma half-life is transfer to an IV infusion container.
Pack: 1’s. 200 mg – 1 x 10’s around 1 h and protein binding low. Excreted Do not mix with other antibiotics and avoid use with
Lactated Ringer Injection.
POM TRAFORAN® (E-Globa) POM CEPODEM® (Ranbaxy) unchanged in the urine mostly in the first 6
Injection, Cefotaxime sodium 1 g. Tablet, Cefpodoxime proxetil 200 mg hour, and some in the bile. The parenteral forms POM Cephradine (Crystal)
Pack: Box of 1 vial + 1 amp. 5 mL solvent. 200 mg – 10’s may give rise to local pain or thrombophlebitis. Injection, Cephradine 1 g.
Oral suspension, Cefpodoxime proxetil 40 mg per 5 Indications: Treatment of infections due to Pack: 1 g x 1’s (in vials)
POM ZETAX® (Justeen)
Injection, Cefotaxime 1 g.
mL; powder for reconstitution. susceptible microorganisms namely Respira-
Pack: 100 mL. tory tract infections including pharyngitis, CEFTAZIDIME
Pack: 1’s.
POM DOXCEF® (Sequoia) tonsillitis, and non-lobar pneumonia; Urinary Therapeutic category: Cephalosporin antibi-
CEFPODOXIME Tablets, Cefpodoxime (as Proxetil) 100 mg, 200 mg; tract infections; Skin and Skin structure infec- otic (3rd Generation).
both f-c tabs. tions; Perioperative prophylaxis. Indications: Infections due to sensitive bac-
Description: Cefpodoxime proxetil is a prod-
100 mg – 10’s. Contra-indications: Ccephalosporin hy- teria, especially those due to Pseudomonas
rug of the active metabolite Cefpodoxime,
200 mg – 10’s. persensitivity or to any component of the spp. and including those resistant to amino-
a semisynthetic, third generation cephalo-
POM SAFETUM® (Nosak) preparation. glycosides.
sporin. It is stable in the presence of lactamase
Tablets, Cefpodoxime (as proxetil) 100 mg, 200 Precautions: Hypersensitivity to penicillins; Contra-indications: Cefalosporin hypersensi-
enzyme.
mg; f-c tabs. renal disease. Prolonged use of antibiotics tivity (see section 9.1.1); porphyria.
Indications: Lower respiratory tract infections
100 mg – 1 x10’s may result in overgrowth of non-susceptible Precautions: Sensitivity to beta-lactam
(community acquired pneumonia, acute exac-
200 mg – 1 x10’s organisms. Pregnancy, breastfeeding. antibacterials (avoid if history of immediate
erbation of chronic bronchitis); Sexually trans- Suspension, Cefpodoxime (as proxetil) 50 mg per 5 Interactions: Loop diuretics (increased risk of hypersensitivity reaction—see section 9.1.1);
mitted diseases (Acute, uncomplicated urethral mL; dry powder for reconstitution.
nephrotoxicity); Probenecid. renal impairment (Appendix 4); pregnancy
and cervical gonorrhea, acute uncomplicated Pack: 100 mL
Adverse effects: GI disturbances including and breastfeeding (but appropriate to use,
ano-rectal infections in women); Skin and skin
POM ORELOX® (Sanofi-Aventis) see Appendices 2 and 3); false positive urinary
glucose (if tested for reducing substances) Injection, Ceftazidime 1 g per vial antibiotic-associated colitis (particularly with POM Ceftriaxone (EDL 5.3)
and false positive Coombs’ test; interactions: Pack: 1 vial with 10 mL diluent higher doses); allergic reactions including Injection, Ceftriaxone 250 mg, 500 mg, 1 g.
Appendix 1. POM Ceftazidime (Jawa) rashes, pruritus, urticaria, serum sickness-like POM ALCEF® (Synergy)
Adverse effects: Diarrhoea, nausea, vomit- Injection, Ceftazidime 1 g reactions, fever and arthralgia, and anaphy- Injection, Ceftriaxone (as Na+) 1 g; powder for re-
ing, abdominal discomfort, headache; rarely, Paxk: 10’s laxis; erythema multiforme, toxic epidermal constitution in vial.
antibiotic-associated colitis (particularly with necrolysis reported; transient hepatitis and Combipack: 1 g x 1’s + 10 mL WFI as diluent.
POM FORTUM Monovial® (GSK)
higher doses); allergic reactions including Injections, Ceftazidime (as pentahydrate) 500 mg, cholestatic jaundice; eosinophilia and blood POM AUROXONE® (Phillips)
rashes, pruritus, urticaria, serum sickness-like 1 g; white to faintly yellow powder in vials which disorders (including thrombocytopenia, leu- Injection, Ceftriaxone 250 mg, 500 mg, 1000 mg,
reaction, fever and arthralgia, and anaphylaxis; effervesces on dissolution. kopenia, agranulocytosis, aplastic anaemia, 2000 mg; white to yellowish-orange crystalline
erythema multiforme, toxic epidermal necrol- Pack: 1; 5. and haemolytic anaemia); reversible interstitial powder.
ysis reported; transient hepatitis, cholestatic nephritis, hyperactivity, nervousness, sleep 250 mg – 10’s.
POM K-ZIDIME® (Justeen)
jaundice; eosinophilia and blood disorders disturbances, confusion, hypertonia and 500 mg – 20’s.
Injection, Ceftazidime 1 g.
(including thrombocytopenia, leukopenia, dizziness; calcium ceftriaxone precipitates in 1000 mg – 30’s.
Pack: 1’s.
2000 mg – 50’s.
agranulocytosis, aplastic anaemia, and haemo- urine (particularly in very young, dehydrated,
POM TAZIDIME® (Solution Pharma)
lytic anaemia); reversible interstitial nephritis; or those who are immobilized) or in gall blad- POM AXONE® (Interpharma)
Injection, Ceftazidime 1 g; white to off-white crys-
nervousness, sleep disturbances, confusion, der—consider discontinuation if symptomatic; Injection, Ceftriaxone (as Na+) 1000 mg
talline powder.
hypertonia, and dizziness. rarely prolongation of prothrombin time, Pack: 1’s (in vial)
Nursing action: See under Cefotaxime. pancreatitis. POM BAKAZONE® (Bakangizo)
POM Vaxcel Ceftazidime (Dortemag)
Dose: Infections due to susceptible organisms, Nursing action: See under Cefotaxime. Injection, Ceftriaxone sodium 1 g; vial containing
Injections, Ceftazidime 250 mg, 500 mg, 1 g, 2 g;
by deep IM injection or by IV injection white to faintly yellow powder.
Dose: Infections due to susceptible organisms, off white powder
or IV infusion, ADULT 1 g every 8 by deep IM injection, by IV injection Pack: 1 vial + 10 mL WFI + 3.5 mL
Pack: 1’s (in vial)
EMDEX
hours or 2 g every 12 hours, or in (over at least 2–4 minutes) or by IV in- POM BAXCEF® IV/IM (Global Healthcare)
severe infections (including immuno- POM ZIDIM® (Medreich) fusion, ADULT 1 g daily; severe infec- Injection, Ceftriaxone 125 mg; 250 mg; 500 mg; 1 g.
Injections, Ceftazidime (as pentahydrate) 500 mg, 1
compromised), 2 g every 8– 12 hours tions 2–4 g daily; INFANT and CHILD
g, 2 g; sterile powder reconstitution in vials. POM BGCEF® (BG Pharma)
or 3 g every 12 hours (ELDERLY usual Pack: 1’s. under 50 kg 20–50 mg/kg daily; up Injection, Ceftriaxone (as sodium salt) 1 g; plus
maximum 3 g daily); NEONATE and to 80 mg/kg daily in severe infections diluents (lidocaine injection 1% 5 mL and sterilised
INFANT up to 2 months, 25–60 mg/ CEFTRIAXONE (doses of 50 mg/kg and over by IV water for injection 10 mL) in vials.
kg daily in 2 divided doses; CHILD infusion only); by IV infusion (over 60 Pack:1 g vial
Indications: Serious infections due to sensitive
over 2 months, 30–100 mg/kg daily in minutes), NEONATES 20–50 mg/kg
bacteria, including septicaemia, pneumonia, POM BIOCEF® (Biofem)
2–3 divided doses (IV route recom- daily (maximum 50 mg/kg daily). Injection, Ceftriaxone (as Na+) 1 g; powder for recon-
and meningitis; osteomyelitis, septic arthritis;
mended for children). Uncomplicated gonorrhoea and stitution in a vial + WFI as diluent
Haemophilus influenzae epiglottis; surgical
Pseudomonal lung infection in cystic gonococcal conjunctivitis, by deep IM Pack: 1’s (in vial) + solvent.
prophylaxis; prophylaxis of meningococcal
fibrosis, by deep IM injection or by IV injection, ADULT 125 mg as a single
meningitis; shigellosis, invasive salmonello- POM BIOPHIN® (Zolon)
injection or IV infusion, ADULT 100– dose (also used with doxycycline and
sis; endocarditis; gonococcal conjunctivitis; Injection, Ceftriaxone sodium 1g; white to yellow
150 mg/kg daily in 3 divided doses. metronidazole to treat pelvic inflam- powder in a vial plus 3.5 mL Lidocaine 1% as solvent
gonorrhoea; pelvic inflammatory disease;
Infections in immunocompromised, matory disease).
Lyme disease. POM CAMECIN® (Crystal)
cystic fibrosis, or meningitis, by IV Neonatal gonococcal conjunctivitis, by
Contra-indications: Cefalosporin hyper-sen- Injection, Ceftriaxone 1 g.
injection or IV infusion, CHILD over IM injection, NEONATE 50 mg/kg as a
sitivity (see section 9.1.1); porphyria; neonates Pack: 1’s (in vial).
2 months up to 150 mg/kg daily in 3 single dose (maximum 125 mg). Injection, Ceftriaxone 1000 mg; white crystalline
with jaundice, hypoalbumi-naemia, acidosis or
divided doses (maximum 6 g daily). Disseminated gonococcal infection, by substance in a vial
impaired bilirubin binding.
Reconstitution and Administration: According to deep IM injection or by IV injection, Pack: 1’s (in vial) +1 amp. WFI (10 mL) + 1 amp. 1%
manufacturer’s directions. Intramuscular doses over Precautions: Sensitivity to beta-lactam
ADULT 1 g daily for 7 days. Lidocaine soln
1 g divided between more than one site. antibacterials (avoid if history of immediate
Surgical prophylaxis, by deep IM injec-
hypersensitivity reaction—see also section POM CAMTAXONE® (Mark)
POM Ceftazidime (WMF 6.2.1) tion or by IV injection (over at least Injection, Each vial contains ceftriaxone (as sodium
9.1.1); severe renal impairment (Appendix 4);
Powder for injection, Ceftazidime (as pentahydrate) 2–4 minutes), ADULT 1 g at induction. salt) 500 mg, 1 g.
250 mg; in vial.
hepatic impairment if accompanied by renal
Colorectal surgery (with antibacterial Each diluent ampoule contains 2 or 3.5 mL water for
impairment (Appendix 5); premature neonates;
POM BESTUM® (Zoomota) active against anaerobes), by deep IM injection and also contains 20-35 mg (1%) lidocaine
may displace bilirubin from serum albumin;
Injection, Ceftazidime 1 g; white powder for recon- injection or by IV injection (over at HCI for only intramuscular administration.
treatment longer than 14 days, renal failure, Each diluent ampoule contains 5 or 10 mL water for
stitution in vials. least 2–4 minutes), or by IV infusion, 2
dehydration or concomitant total parenteral injection for IV administration.
Pack: 1’s (in vial) + 10 mL diluent g as a single dose.
nutrition—risk of ceftriaxone precipitation in
Reconstitution and Administration: According to POM CEFAX® SKG)
POM BETAZIDIME® (Strides Vital) gallbladder; pregnancy and breastfeeding (but manufacturer’s directions. Intramuscular doses over Injections, Ceftriaxione (as Na+) 500 mg, 1 g; in vials.
Injection, Ceftazidime 1 g; in vial. appropriate to use, see Appendices 2 and 3); 1 g divided between more than one site. Administer 500 mg – 1’s (in vial) + WFI
POM CEFAZID® (Olpharm) false positive urinary glucose (if tested for re- by intravenous infusion over 60 minutes in neonates 1 g – 1’s (in vial) + WFI
Injections, Ceftazidime (as pentahydrate) 250 mg, ducing substances) and false positive Coombs’ (see also Contraindications).
500 mg, 1 g; in vials. test; interactions: Appendix 1. POM CEFEREX® (Greenlife)
POM Ceftriaxone (WMF 6.2.1) Injection, Ceftriaxone 1 g, Lidocaine 1% 3.5 mL as
Pack: 1’s (in vials) Adverse effects: Diarrhoea, nausea and Powder for injection, Ceftriaxone (as sodium salt) diluent.
POM CEFTAZAR® (Shrezar) vomiting, abdominal discomfort, headache; 250 mg, 1 g; in vial. Combi pack: 15 mL x 1’s (in vial) + 3.5 mL Lidocaine
injection BP. POM CETAFOR® (Dafra) and Lidocaine HCI 1% 5 mL. Injection, (IM), Ceftriaxone (as Na salt) 1 g; white to
Injection (0.5 g), Ceftriaxone (disodium) equiv. to Combipack: 1 g x 1's + diluents (10 mL sterile water pale yellow crystalline powder for reconstitution +
POM CEFIN® (Pharmabox)
Ceftriaxone 0.5 g; sterile dry powder for IM injection. for injection + 5 mL Lidocaine 1% in amps). 3.5 mL lidocaine 1% as diluent.
Injection, (500 mg), Ceftriaxone (as Na+) 500 mg;
Pack: 1’s (in vial) + 2 mL 1% Lidocaine solution for Pack: 1 g x 1’s (in vial) + diluents (in amps)
white to light yellow powder for reconstitution + POM ODICEF® I.M/I.V (Phillips/Prisma)
injection in amp. Injection, (IV), Ceftriaxone (as Na salt) 1 g; white to
5 mL WFI. Injections, Ceftriaxone 250 mg, 500 mg, 1 g; dry
Injection (1 g), Ceftriaxone (disodium) equiv. to pale yellow crystalline powder for reconstitution +
500 mg – 1’s; 5’s; 10’s; 20’s; 100’s powder for reconstitution in vials.
Ceftriaxone 1 g; sterile dry powder for IM injection. 10 mL water for injection as diluent.
Injection, (1 g), Ceftriaxone (as Na+) 1 g; white to Pack: 1’s (in vial) + WFI (in amp.)
Pack: 1’s (in vial) + 4 mL 1% Lidocaine solution for Pack: 1 g x 1’s (in vial) + diluents (in amps)
light yellow powder for reconstitution + 10 mL WFI.
injection in amp. POM OFRAMAX® (Ranbaxy)
1 g – 1’s; 5’s; 10’s; 20’s; 100’s POM STARXON® (Reals)
Injections, Ceftriaxone (as Na+) 250 mg, 500 mg, 1 g;
POM CEVMID® (Vixa) Injection, Ceftriaxone (as Na+) 1 g; in vial + solvent
POM CEFITHER® (Crowther) powder for reconstitution.
Injection, Ceftriaxone sodium 1 g . in amp.
Injection, Ceftriaxone (as Na+)1 g; dry powder for Pack: 10’s
Pack: 1’s (in vial) + 1 ampoule of 4 mL of 1% lidocaine
reconstitution + WFI as diluent. POM CLOCEFTRI® (E-Globa)
POM Oka-Ceftriaxone (Placeware) solution (IM).
Pack: 5 x 1’s. Powder for injection, Ceftriaxone sodium equiv. to
Injection (IM/IV), Ceftriaxone 1 g. 1’s (in vial) + 1 ampoule of 10 mL WFI (IV).
Ceftriaxone (anhydrous) 1 g; 5 mL Lidocaine 1% (IM)
POM CEFOXIN® (Onifam) Pack: 1 g (in vial) + WFI as diluent
and 10 mL WFI (IV) as diluents. POM SUMOCEF® (Nosak)
Injection, Ceftriaxone 1 g; powder for reconstitution
POM Oka-Ceftriaxone (Placeware) Injection, Ceftriaxone (as Na+) 1000 mg; in vial + 5 mL
in vial. POM DUOCEF® (Korlyns)
Injection, Ceftriaxone 250 mg; 500 mg. Lidocaine HCI injection 1% w/v as diluent.
Pack: 1 x 10’s (without diluent) Injection, Ceftriaxone (as Na+) 1 g; in vial.
250 mg – 1’s (in vial)
POM SYCEPH® (Geneith)
POM CEFTAP® (Tamar & Pharez) POM DUOCEF® (Korlyns) 500 mg – 1’s (in vial).
Injection ,(500 mg), Ceftriaxone 500 mg.
Injection, Ceftriaxone 1 g. Injection, Ceftriaxone 1 g; white powder
POM ONECEF® (Justeen) Injection, (1 g), Ceftriaxone 1 g.
Pack: 1's (in vial) Pack: 1’s (in vial) + 1 amp. solvent.
Injections, Ceftriaxone 250 mg, 1 g.
POM Teva-Ceftriaxone (Dizpharm)
POM Ceftriaxone (Crystal) POM EBECEF® (Elbe) Pack: 1’s.
EMDEX
Injection, Ceftriaxone (as sodium) 1000 mg
Injection, Ceftriaxone sodium 500 mg, 1000 mg Injection, Ceftriaxone 1 g.
POM ONGEN® (Pharma Ethics) 1000 mg – 1 g
Pack: 1 g x 1 vial.
POM Ceftriaxone (Jawa) Injection, Ceftriaxone 1 g; dry powder for reconsti-
POM TINAM® (Jubilee)
Injection, Ceftriaxone 1 g POM EUBESTIC® (Next Generation) tution + WFI as diluent.
Injections, Ceftriaxone (as Na+) 500 mg, 1 g
Pack: 10’s Injection, Ceftriaxone sodium equiv. to Ceftriaxone Pack: 1 g x 1’s (in vial)
anhydrous 1 g per vial POM TOROCEF®-1 (Zoomota)
POM Ceftriaxone (Gauze) POM PEMATRIAXONE® (Pemason)
Pack: 250 mg; 500 mg; 1 g; 2 g (vials) Injection, Ceftriaxone (as Na+) 1 g; cream coloured
Injection, Ceftriaxone (as sodium salt) 1 g per vial Injection, Ceftriaxone 1 g; white crystalline powder
sterile crystalline powder in glass vial.
Pack: 10 x 1's (vials) POM FACEFIN® (Al-Tinez) in 10 mL vials with 1% Lidocaine soln and WFI as
Pack: 1’s (in vial) + 10 mL WFI
Injection, Ceftriaxone (as Na+) 250 mg, 500 mg, 1 g; diluents.
POM Ceftriaxone (Quadrant)
white to slightly yellowish crystalline powder in vials. Pack: 1 g x 10’s. POM TRIAMAX® (Eutrix)
Injection, Ceftriaxone (as sodium salt) 250 mg, 500
Injection, Ceftriaxone (as Na+) 1 g; white to pale
mg or 1.0 g per vial. POM GLOCEFTRI® (E-Globa) POM PHARMAXONE® (Solution Pharma)
yellow powder for reconstitution.
Injection, Ceftriaxone sodium 1 g, lidocaine 1% 5 mL Injection, Ceftriaxone sodium 1 g; white to off-white
POM Ceftriaxone (Superior)
as diluent, sterile water for injection 10 mL per vial crystalline powder. POM TRIKAXON® (Neros)
Injection, Each pack contains ceftriaxone sodium 1
Pack: 1’s (in vial). Injection (IV), Ceftriaxone 1 g
gm (powder for injection), lidocaine 3.6 mL (1%), POM HOCHEFIN® (Hochiez)
Pack: 1’s (in vial) + 1 amp. 10 mL WFI.
sterile water injection 10 mL. Injection, Ceftriaxone (as sodium) 1 g POM POWERCEF (Zoomota)
Reconstitution: For IM administration: Reconstitute Pack: 1’s (in vial) + 10 mL WFI (IV) + 5 mL 1% Lido- Injections, Ceftriaxone (as Na+) 500 mg, 1 g; white POM TRIXONE® (L.B.S.)
with 3.6 mL, 1% lidocaine HCl injection. Each 1 mL caine HCl injection (IM) powder for reconstitution in vials. I.M. Injection, Ceftriaxone 500 mg + 2 mL lidocaine
of solution contains approx. 250 mg of ceftriaxone. 500 mg – 1’s (in vial) + 5 mL diluent 1%; 1 g + 3.5 mL lidocaine 1%.
POM HOFTREX® (Hovid)
For IV administration: Reconstitute with 9.6 mL of 1 g – 1’s (in vial) + 10 mL diluent I.V. Injection, Ceftriaxone 500 mg + 5 mL WFI; 1 g
Injections, (IM/IV), Ceftriaxone (as sodium salt) 0.25
water for injection. Each 1 mL of solution contains + 10 mL WFI.
g, 0.5 g, 1 g per vial POM ROCEPHIN® (Swipha)
approx. 100 mg of ceftriaxone. Discard any unused Pack: 1’s.
0.25 g – 1’s + WFI I.M. Injection, Ceftriaxone 250 mg + 1 mL Lidocaine
portion.
0.5 g – 1’s + WFI 1%; 500 mg + 2 mL lidocaine 1%; 1g + 3.5 mL POM TROXONE® (Embassy)
POM Ceftriaxone MJ (Fidson) 1 g – 1’s + WFI lidocaine 1%. Injection, Ceftriaxone 1 g.
Injection, Ceftriaxone (as Na+) 0.5, 1 g; powder re- I.V. Injection, Ceftriaxone 1 g + 10 mL WFI. Pack: 1’s.
POM LENDACIN® (Taylek)
constitution in vials.
Injections, Ceftriaxone 250 mg, 1 g, 2 g; in vials. POM ROFIN® (N.C.I) POM Vaxcel Ceftriaxone (Dortemag)
Pack: 1’s vial.
Pack: 10’s. Injection, Ceftriaxone 1 g. Injections, Ceftriaxone (as Na+) 250 mg, 500 mg, 1 g,
POM CEFZONE® (Evans) 1 g – 1 x 10’s. 2 g; dry white crystalline powder.
POM MESPORIN® IM/IV (Oculus)
Injections, Ceftriaxone (as Na+) 250 mg, 500 mg, 1 g; Pack: 1’s (in vial)
Injection, Ceftriaxone 250 mg, 500 mg, 1000 mg POM ROPHEX® (Pharmabase)
sterile dry powder for reconstitution in vials.
Pack: 1’s (in vial) + 1 amp. 1% Lidocaine HCI soln. Injection, Ceftriaxone (as Na+) 1 g; powder for re- POM XAPO® (Justeen)
250 mg – 1’s + diluent
constitution in vial. Injections, Ceftriaxone 1 g.
500 mg – 1’s + diluent POM MONOTAX® (Olpharm)
Pack: 15 mL vial + 10 mL ampoule of WFI. Pack: 1’s.
1 g – 1’s + diluent Injection, Ceftriaxone (as Na+) 125 mg, 250 mg, 500
mg, 1 g; dry powder for reconstitution in vials + POM SAFE-TAX® (Global Organics) POM ZARCEF® (Shrezar)
POM CELLTRIAXON® (Strides Vital)
diluents in amps. Injection, Ceftriaxone (as sodium salt) 1 g; plus Injection, (IV), Ceftriaxone (as sodium salt) 250 mg;
Injection, Ceftriaxone 1 g; in 1 g vial.
Pack: 1’s. diluents namely Lidocaine 1% 5 mL and sterilised powder for reconstitution in vial
POM CEPHAROX® (May & Baker) water for injection 10 mL in ampoules. Pack: 1 g x 1's (in vial) + 10 mL sterilized WFI
POM NEFZON® (Mark)
Injection, Ceftriaxone (as Na+) 1 g; powder for recon- Pack:1 g x 1's (in vial) + diluents Injection, (IM), Ceftriaxone (as sodium salt) 1 g;
Injection, Ceftriaxone (as sodium salt)) 1 g; plus
stitution in a vial + ampoule of 10 mL WFI as solvent. powder for reconstitution in vial.
diluents namely Sterile water for injection 10 mL POM SONICEF® (Sonicx)
Pack: 1 g x 1's (in vial) + 5 mL Lidocaine HCI 1% Precautions: Penicillin-sensitivity; hepatic or Combipack: 1.5 g x 1's (in vial) + 1 ampoule of 10 Child (>5 years): 125 mg 2 times daily
renal dysfunction; Vitamin K deficiency states; mL WFI. doubled in otitis media if necessary.
POM ZETRAXONE® (Pharmgate)
Injection, Ceftriaxone 1 g. Superinfection especially with prolonged use, Adult: By IM or IV injection, usually
Pack: 1’s. monitor for overgrowth of nonsusceptible CEFUROXIME 750 mg 3 times daily increased to 1.5
organisms; history of colitis. Therapeutic category: Cephalosporin antibi- g 3 times daily IV if necessary.
POM ZORICEF® (Crystal)
Adverse effects: Inflammation at injection otic (2nd Generation). Child: 30-100 mg/kg/day in 3-4
Injection, Ceftriaxone 1 g.
Pack: 1’s (in vial). site with pain and tenderness; Hypersen- Indications: Cefuroxime is resistant to most divided doses (2-3 divided doses in
sitivity including pruritus, fever or chills. GI beta-lactamases and is active against a wide neonates).
POM ZOXON® (Medreich) disturbances e.g. diarrhoea, nausea, vomiting, range of Gm+ve and Gm-ve organisms. Indi- Gonorrhoea, single dose of 1.5 g (2 x
Injection, (250 mg), Ceftriaxone 250 mg; sterile,
stomatitis, glossitis. Heamatological changes cations include: Respiratory tract infections 750 mg IM in two sites).
crystalline powder for reconstitution in vial.
Pack: 1’s (in vial) + 1 ampoule of 1 mL 1% Lidocaine e.g. Eosinophilia, heamatoma, or bleeding, such as acute and chronic bronchitis; upper See lit. for details.
HCl solution for IM injection. thrombocytopenia, neutropenia, leucopenia, respiratory tract infections such as ear, nose
POM Cefuroxime (EDL 5.3)
1’s (in vial) + 1 ampoule of 5 mL WFI. granulocytopenia, and haemolytic anaemia. and throat infections; Genito-urinary tract Tablets, Cefuroxime (as axetil) 125 mg, 250 mg,
Injection, (500 mg), Ceftriaxone 500 mg; sterile, Exanthema, allergic dermatitis, pruritus, urti- infections such as pyelonephritis; skin and 500 mg
crystalline powder for reconstitution in vial. caria, oedema, erythema multitiform. Head- soft-tissue infections such as impetigo; Bone Oral liquid, Cefuroxime (as axetil) 125 mg per 5 mL.
Pack: 1’s (in vial) + 1 ampoule of 2 mL 1% Lidocaine aches and dizziness, increase in liver enzymes, and joint infections such as osteomyelitis; Injection, Cefuroxime (as sodium salt) 250 mg,
HCl solution for IM injection. oliguria, and increase in serum creatinine, obstetric and gynaecological infections such 750 mg
1’s (in vial) + 1 ampoule of 8 mL WFI. mycosis of the genital tract, fever, shivering. as pelvic inflammatory diseases; Gonorrhoea
Injection ,(1 g), Ceftriaxone 1 g; sterile, crystalline POM ALTACEF® (Phillips)
Rarely, agranulocytosis , anaphylactic or ana- and other infections such as septicaemia and Tablets, Cefuroxime axetil 250 mg, 500 mg
powder for reconstitution in vial.
Pack: 1’s (in vial) + 1 ampoule of 3.5 mL 1% Lidocaine phylactoid reactions. meningitis.
POM AXACEF® (Medreich)
HCl solution for IM injection. Dose: By slow IV (2-4 mins) or IM injection, Also as prophylactic against infection in abdom-
Tablets, Cefuroxime (as axetil) 250 mg, 500 mg;
EMDEX
1’s (in vial) + 1 ampoule of 10 mL WFI. Adult, usually 1.5 g (Ceftriaxone 1 g + inal, pelvic, orthopaedic, cardiac, pulmonary, white f-c tabs.
Sulbactam 0.5 g) to 3 g (Ceftriaxone 2 oesophageal and vascular surgery where there
Reconstituted solution is pale yellow to amber POM Axcel Cefuroxime (Dortemag)
g + Sulbactam 1 g) every 6 hours. Not is increased risk from infection.
solution and each gram of Ceftriaxone contains Capsule , Cefuroxime 250 mg
exceeding 4 g of Sulbactam per day. Contra-indications: Hypersensitivity to cephalo-
approx. 3.6 mmol Na+. Injection, Cefuroxime 1.5 g
Children: See lit. for details. sporin antibiotics.
Duration is usually 7-10 days de- Precautions: Hypersensitivity to penicillins, POM BIOXETIL® (Biofem)
CEFTRIAXONE plus SULBACTAM Tablet, Cefuroxime (as naxetil) 250 mg; f-c tab.
pending on type and severity of the pregnancy, breast feeding.
Pharmacology: Ceftriaxone is a broad-spec- Interactions: Loop diuretics, aminoglycosides 250 mg – 12’s
infection.
trum semi-synthetic third-generation ceph- Administration: Administer by slow IV injection (increased nephrotoxicity). Injection, Cefuroxime (as Na+) 750 mg; white to off
alosporin with a potent bactericidal activity (2-4 mins) to minimize local inflammatory reactions white powder or crystalline powder + WFI as diluent.
Adverse effects: Hypersensitivity reactions, GI Pack: 1’s (in vial) + WFI as solvent
against a wide range of gram– positive in the vein. lM injection without Lidocaine solution disturbances, positive coomb’s test, candidosis,
and gram-negative bacteria. Sulbactam, a is painful. pain at injection site, transient increase of liver POM BUROXIM® (JB Pharma)
derivative of the basic penicillin nucleus, is References: enzyme levels, headache. Tablets, Cefuroxime axetil 250 mg, 500 mg; f-c tabs.
an irreversible inhibitor of β-lactamase. It is 1) Xin X, Jian L, Xia X, Jia B, Huang W, Li C, Advice to patients: Report prolonged di-
administered in combination with β-lactam 500 mg – 1 x 10’s (in blisters)
Wang C, Zhou L, Sun X, Tang X, Huang arrhoea; entire course of medication (10-14
antibiotics to overcome the effects of β-lacta- Y, Zhu Y, Zhang W. A multicentre clinical days) should be taken to ensure eradication POM CALEDO® (Next Generation)
mase. Xin et al showed that the addition of study on the injection of ceftriaxone/ of organism; should be taken in equal intervals Tablet, Cefuroxime axetil 500 mg; f-c tab.
sulbactam to ceftriaxone treatment not only sulbactam compared with cefoperazone/ around-the-clock to maintain adequate blood 500 mg – 10’s (in blisters)
augments the activity of ceftriaxone against sulbactam in the treatment of respiratory levels; may interfere with oral contraceptives;
Oral suspension, Cefuroxime axetil 125 mg per 5 mL
β-lactamase-producing bacteria but also Pack: 50 mL
and urinary tract infections. Annals of females should report symptoms of vaginitis.
maintains its cost-effectiveness (once or twice Clinical Microbiology and Antimicrobials Nursing action: Obtain specimens for C&S POM CEFANEL® XL (Nalis)
daily administration). 2013, 12:38. tests prior to the first dose; administer around- Tablet, Cefuroxime axetil 500 mg; f-c tab
Indications: Treatment of the infections the-clock to promote less variation in peak and Oral suspension, Cefuroxime axetil 125 mg per 5 mL
caused by susceptible bacteria such as sepsis; POM Ceftriaxone plus Sulbactam (Crystal)
Injection, Ceftriaxone (as Sodium salt) 1 g, Sulbactam trough serum levels. POM CEFDIUM® (Solidum)
meningitis; abdominal infections (peritonitis, • Cefuroxime axetil tablet may be crushed to aid Tablets, Cefuroxime axetil 250 mg, 500 mg; f-c tabs.
(as Sodium salt) 500 mg; powder for injection in vial
infections of the biliary and gastrointestinal swallowing but it has a bitter taste that is too 250 mg – 10’s
+ 10 mL WFI as diluent in ampoule.
tracts); infections of the bones, joints, soft tis- Combipack: 1.5 g x 1's (in vial) + 1 ampoule of 10 difficult to mask, even with food. 500 mg – 10’s
sue, skin and of wounds; infections in patients mL WFI. • Give deep IM into a large muscle mass, such as
POM CEFOGEN® (Interpharma)
with impaired defence mechanisms; renal gluteus or lateral aspect of thigh.
POM SYCEPH-SB® (Geneith) Injection, Cefuroxime (as Na) 750 mg.
and urinary tract infections; respiratory tract • Total daily dosage is the same for IM or IV adminis-
Injection, Ceftriaxone (as sodium salt) 1 g, Sulbactam Pack: 1’s (in vial)
infections, particularly pneumonia and ear, tration and depends on susceptibility of organisms
(as sodium salt) 0.5 g; plus diluents namely Lidocaine and severity of infection. POM CEFUJET® (Evans)
nose and throat infections; genital infections, HCI 1% 5 mL and Sterile water for injection10 mL. • See also under Cefaclor. Injection, Cefuroxime (as Na) 750 mg; in vial.
including gonorrhoea; perioperative prophy- Combipack: 1.5 g x 1's + diluents Dose: By mouth (Cefuroxime axetil), usually
laxis of infections. POM CEFUNAT® (Evans)
POM ZARCEF-S® (Shrezar) 250 mg 2 times daily doubled in Tablets, Cefuroxime axetil 250 mg, 500 mg.
Contra-indications: Hypersensitivity to
Injection, Ceftriaxone (as Sodium salt) 1 g, Sulbactam bronchitis and pneumonia; 250 mg – 10’s.
cephalosporins or penicillins (sulbactam is a (as Sodium salt) 500 mg; powder for injection in vial UTIs, 125 mg 2 times daily; Uncompli- 500 mg – 10’s.
penicillin derivative). + 10 mL WFI as diluent in ampoule. cated gonorrhoea, single dose of 1 g.
364 | 9.1.1.2 Cefalosporins 9.1.1.3 Other beta-lactam antibacterials | 365
POM CEFUROXA® (N.C.I) POM DIGICEF® (Digitall) Injection,Cefuroxime (as Na ) 750 mg
+
POM ZIVA® (Vatican Bells)
Tablet, Cefuroxime axetil 250 mg; white tab. Suspension, Cefuroxime (as axetil) 125 mg per 5 mL Pack size: 10’s Dry Syrup, Cefuroxime axetil 125 mg per 5 mL.
250 mg – 1 x 10’s Pack: 100 mL Pack: 100 mL.
POM MICROCEF® (Micronova)
POM CEFUROX® (Fidson) POM EMBACEF® (Embassy) Tablets, Cefuroxime (as axetil) 250 mg, 500 mg;
Tablets, Cefuroxime (as axetil) 250 mg, 500 mg; Tablet, Cefuroxime axetil 250 mg; f-c tab. f-c tabs. 9.1.1.3 Other beta-lactam
f-c tabs. 250 mg – 1 x 10’s 250 mg – 10’s. antibacterials
250 mg – 10’s 500 mg – 10’s. Imipenem is a carbapenem broad-spectrum
POM EXIME® (Chanmedi)
500 mg – 10’s. antibiotic. As it is partially inactivated by enzy-
Tablet, Cefuroxime axetil 250 mg, 500 mg POM MIRAXIM® (Miraflash)
POM Cefuroxime (Crystal) 250 mg – 10 x 10’s Tablet, Cefuroxime (as axetil) 500 mg. matic activity in the kidney, it is administered
Tablet, Cefuroxime axetil 250 mg; uncoated tab 500 mg – 10 x 10’s
POM PEFUXINE® (Pemason)
with cilastatin which inhibits the renal metab-
250 mg – 10’s (in blisters) olism of imipenem. It is active against many
POM FUCE® (Canopus) Tablets, Cefuroxime axetil 250 mg, 500 mg; white
Tablet, (Dispersable), Cefuroxime axetil 500 mg aerobic and anaerobic Gram-positive and
Tablets, Cefuroxime axetil 250 mg, 500 mg; f-c tabs. oblong scored tabs.
250 mg – 10’s (in blisters) 250 mg – 5 x 2’s (in blisters) Gram-negative bacteria; in some areas it is kept
POM Cefuroxime (Jawa) 500 mg – 10’s (in blisters) 500 mg – 5 x 2’s (in blisters) in reserve for the treatment of infections due
Injection, Cefuroxime 750 mg Dry syrup, Cefuroxime axetil 125 mg to Acinetobacter spp. and Ps aeruginosa, which
POM PULMOCEF® (Geneith)
Pack: 10’s Pack: 60 mL are resistant to other more usual treatments.
Tablets, Cefuroxime (as axetil) 125 mg, 250 mg, 500
POM Cefuroxime (Vitahealth) POM FUCETAP® (Tamar & Pharez) mg; f-c tabs. Meropenem is another carbapenem antibiotic
Injections, Cefuroxime (as sodium) 0.75 g, 1.5 g Tablets, Cefuroxime axetil 250 mg, 500 mg 125 mg – 1 x 10’s with broad spectrum antibacterial coverage.
per vial. 250 mg – 1 x 10's 250 mg – 1 x 10’s It is relatively stable to human dehydropep-
0.75 g – 10’s (in box) 500 mg – 1 x 10's 500 mg – 1 x 10’s
tidase-1(DHP-1) compared to Imipenem and
1.5 g – 10’s (in box) Injection,Cefuroxime sodium 750 mg; powder in vial.
POM FUROXICEF® (May & Baker) therefore does not require the addition of a
EMDEX
Pack: 1’s (in vial) + 10 mL WFI in amp.
POM Cefuroxime MJ (Fidson) Injection, Cefuroxime (as Na+) 750 mg; powder for DHP-1 inhibitor.
Injections, Cefuroxime (as Na) 500 mg, 750 mg, 1.5 reconstitution in a vial + 6 mL WFI as solvent (in amp). POM QUINCEF® (Neros)
g; in vials. Tablets, Cefuroxime (as Axetil) 125 mg, 250 mg, 500 IMIPENEM plus CILASTATIN
POM FUROXETIL® (May & Baker)
Pack: 1’s (in vials). mg; f-c tabs.
Tablet, Cefuroxime (as Axetil) 250 mg.
125 mg – 2 x 5’s (in blisters). Imipenem with cilastatin is a complementary antibac-
POM Cefuroxime (Nosak) 250 mg – 10’s.
250 mg – 2 x 5’s (in blisters). terial combination for use only when there is significant
Tablets, Cefuroxime (as axetil) 250 mg, 500 mg; Suspension, Cefuroxime (as Axetil) 125 mg per 5 mL;
500 mg – 2 x 5’s (in blisters). resistance to other drugs on the WHO Model List.
f-c tabs. dry granules for reconstitution.
Granules, Cefuroxime (as Axetil) 125 mg; in sachet.
Suspension, Cefuroxime (as axetil) 125 mg per 5 mL; Pack: 100 mL.
125 mg – 10’s (sachets). Therapeutic category: Carbapenem antibiotic
dry powder for reconstitution. Indications: Severe aerobic and anaerobic
POM G-ROXIM® (Greenlife) Powder for oral suspension, Cefuroxime (as Axetil)
Pack: 50 mL Gram-positive and Gram-negative infections
Tablets, Cefuroxime (as axetil) 250 mg, 500 mg; 125 mg per 5 mL
POM CEFUXIME® (Phillips) f-c tabs. Pack: 50 mL. in hospital (not indicated for CNS infections),
Caplet, (125 mg), Cefuroxime axetil 125 mg; white 250 mg – 10’s.
POM ROXICEF® (Medreich)
including infections caused by resistant Pseu-
to off-white caplet marked “A32”. 500 mg – 10’s domonas and Acinetobacter spp.
Injections, Cefuroxime (as Na) 250 mg, 750 mg; sterile
Caplet, (250 mg), Cefuroxime axetil 250 mg; white Injection, Cefuroxime 750 mg; sterile dry powder Precautions: Sensitivity to beta-lactam
powder for reconstitution in vials.
to off-white caplet marked “A33”. for injection. antibacterials (avoid if history of immediate
250 mg – 10’s.
Caplet, (500 mg), Cefuroxime axetil 500 mg; white Combi pack: 1’s (in vial) + 10-mL amp. WFI.
750 mg – 10’s. hypersensitivity reaction—see also section
to off-white caplet marked “A34”.
POM KEFSTAR® (Zoomota)
POM UTRINOX® (Pharmgate)
9.1.1); renal impairment (Appendix 4); CNS dis-
Tablets, Cefuroxime (as axetil) 125 mg, 250 mg, 500 orders, such as epilepsy; pregnancy (Appendix
250 mg – 10’s (in blisters) Tablet, Cefuroxime axetil 250 mg, 500 mg
mg; brilliant blue f-c tabs. 2); breastfeeding (Appendix 3); interactions:
500 mg – 10’s (in blisters). 250 mg – 1 x 10’s
125 mg – 4’s; 10’s Appendix 1.
500 mg – 1 x 10’s
POM CEFUZAR® (Shrezar) 250 mg – 10’s.
Suspension, Cefuroxime axetil 125 mg per 5 mL. Adverse effects: Nausea, vomiting, diarrhoea;
Injection, Cefuroxime (as sodium salt) 750 mg per vial 500 mg – 10’s.
Pack: 100 mL antibiotic-associated colitis; taste disturbances;
Pack: 1 vial with 10 mL diluent Suspension, Cefuroxime (as axetil) 125 mg per 5 mL;
cream coloured granules for reconstitution. POM Vaxcel Cefuroxime (Dortemag) tooth or tongue discoloration, hearing loss;
POM CEROXIM® (Ranbaxy) blood disorders, positive Coombs’ test; allergic
Pack: 50 mL. Injections, Cefuroxime (as Na+) 250 mg, 750 mg, 1
Tablets, Cefuroxime (as Axetil) 125 mg, 250 mg, 500
Injection, Cefuroxime (as Na +) 750 mg; cream g; white or almost white to faintly yellow powder reactions (see section 9.1.1) including rash,
mg; f-c tabs.
coloured powder in vial. Pack: 1’s (in vial) pruritus, urticaria, erythema multiforme (Ste-
Pack: 10’s; 5 x 10’s.
750 mg – 1’s + syringe & needle + diluent. vens-Johnson syndrome), fever, anaphylactic
POM ZINACEF® (GSK)
POM CEFTYL® (Dafra) reactions, rarely toxic epidermal necrolysis,
POM KEFUROX® (Phillips/Prisma) Injection, Cefuroxime (as Na+) 250 mg, 750 mg; white
Tablets, Cefuroxime axetil 250 mg, 500 mg; f-c tabs exfoliative dermatitis; myoclonic activity, con-
Tablets, Cefuroxime (as Axetil) 250 mg, 500 mg; to faintly yellow powder in vials.
f-c tabs. 750 mg – 5. vulsions, confusion, and mental disturbances;
250 mg – 10’s (in blister) slight increase in liver enzymes and bilirubin,
POM ZINNAT® (GSK)
POM CLITEX® (Pharmabase) 500 mg – 10’s (in blister). rarely hepatitis; increases in serum creatinine
Tablets, Cefuroxime (as axetil) 125 mg, 250 mg, 500
Suspension, Cefuroxime axetil 250 mg per 5 mL; Injections, Cefuroxime (as Na+) 750 mg, 1.5 g; dry and blood urea; red coloration of urine in
mg; white f-c capsule-shaped tabs. marked ‘GLAXO’
white dry powder in an amber-coloured bottle. powder for reconstitution in vials.
and ‘125’, ‘250’ and ‘500’ respectively. children; erythema, pain and induration, and
Pack: 100 mL. 750 mg – 1’s
1.5 g – 1’s.
Pack: 10; 50. thrombophlebitis at injection sites.
Injection, Cefuroxime (as Na+) 750 mg.
Suspension, Cefuroxime (as axetil) 125 mg per 5 mL; Dose: NOTE: All doses are in terms of imipe-
Pack: 15 mL vial + 10 mL WFI (in amp).
POM LICAFUR® (Zolon) granules for oral suspension in multidose bottle. nem.
366 | 9.1.1.3 Other beta-lactam antibacterials 9.1.2 Other antibacterials | 367
Infections due to susceptible organisms, otherapy or in combination with antiviral injection, reconstitute with sterile water for injec- For parenteral use, chloramphenicol sodium
by IV infusion, ADULT 1–2 g daily (in or antifungal agent for empiric treatment of tion (5 mL per 250 mg Meropenem) which gives an succinate, which is freely soluble and un-
3–4 divided doses); less susceptible presumed infections in adult with febrile approx. concentration of 50 mg/mL. Reconstituted dergoes hydrolysis in the tissues with the
organisms, ADULT up to 50 mg/kg neutropenia. solutions are clear and colourless or pale yellow. For liberation of chloramphenicol, can be injected
IV infusion, reconstitute with compatible infusion
daily (maximum 4 g daily) in 3–4 Contra-indications: Hypersensitivity to mer- intravenously or in small volumes intramuscu-
fluid (50 to 200 ml).
divided doses; CHILD over 3 months, openem or other beta-lactams. larly. The plasma concentrations after adminis-
60 mg/kg daily (maximum 2 g daily) Precautions: Monitor for overgrowth of POM BOTAPEM® (Zolon) tration by these routes are unpredictable, and
in 4 divided doses; CHILD over 40 kg, non-susceptible organisms; also renal, he- Injection, Meropenem (as trihydrate) 500 mg, approximate to only 30–70% of those obtained
Sodium carbonate 104 mg; sterile white powder.
adult dose. patic and hematopoietic functions, during after the same dose by the oral route.
Pack: 500 injection pack in a carton.
Reconstitution and Administration: According prolonged use. History of seizures and other The half-life of chloramphenicol is considerably
to manufacturer’s directions. The intramuscular CNS disorders. Pregnancy, lactation. POM MIPENEM® (Fidson) prolonged if paracetamol is given concurrently,
preparation must not be administered intravenously. Interactions: May reduce concentration of Injections, Meropenem 500 mg, 1g; in vials and co-administration of these drugs should
The infusion preparation must not be administered
valproic acid or divalproex sodium (avoid POM NURONEM® (Ranbaxy) be avoided.
intramuscularly.
co-administration). Injection, (500 mg), Meropenem (as trihydrate) 500 Induction of liver microsomal enzymes, for
POM Imipenem plus Cilastatin (WMF 6.2.1) Adverse effects: Thrombocythaemia; head- mg, Sodum carbonate 104 mg; white powder which example by phenobarbital or rifampicin,
Powder for injection, Imipenem (as monohydrate) ache; nausea, vomiting, diarrhoea, abdominal forms a clear colourless or pale yellow solution on diminishes blood levels of chloramphenicol;
250 mg with cilastatin (as sodium salt) 250 mg. pain; increase in serum transaminases, alkaline reconstitution. conversely, chloramphenicol, which inhibits
Powder for injection, Imipenem (as monohydrate) Pack: 500 mg (in vial)
phosphatase, lactic dehydrogenase; rash, hepatic microsomal oxidases, potentiates the
500 mg with cilastatin (as sodium salt) 500 mg. Injection, (1 g), Meropenem (as trihydrate) 1 g,
pruritis, urticaria; inflammation, pain. Less activity of other drugs such as phenytoin.
Sodium carbonate 208 mg; white powder which
POM ALPHAPENEM® (Alpha) frequently seizures, paraesthesia, pseudomem- Glossitis, associated with overgrowth of Can-
forms a clear colourless or pale yellow solution on
Injection, Imipenem 500 mg, Cilastatin 500 mg; white branous colitis, oral and vaginal candidiasis; dida albicans, is fairly common if the course of
reconstitution..
EMDEX
to pale yellow powder in a colourless transparent anaphylaxis. treatment exceeds 1 week.
Pack: 1 g (in vial)
vial with a red cap.
Dose: The dosage and duration of therapy Chloramphenicol exerts a dose-related but
Pack: 1 x 10’s POM POSPENEM® (Alpha)
shall be established depending on Injection, Meropenem (as trihydrate) 500 mg, sodium
reversible depressant effect on the marrow of
POM BACQURE® (Ranbaxy) type and severity of infection and the all those treated. Rarely, aplasia may occur with
carbonate 104 mg (dry sterile); white to pale yellow
Injection, (250 mg), Imipenem 250 mg, Cilastatin condition of the patient. oral and even ophthalmic administration and
crystalline powder in a colourless transparent vial.
250 mg; in vial.
Adult, by IV infusion, Pneumonia, Reconstitution: Dissolve in more than 100 mL may be potentiated by cimetidine.
Injection (500 mg), Imipenem 500 mg, Cilastatin
UTI, gynaecological infections such as of 0.9% NaCl infusion or D5W. Water for injection Chloramphenicol should not be used systemi-
endometritis, skin and skin structure should not be used because it is not isotonic. cally for minor infections. The daily dose should
500 mg; in vial.
Pack: 1’s (in vial). infections, 500 mg every 8 hours. not normally exceed 2 g, and the duration of
Nosocomial pneumonias, peritonitis, 9.1.2 Other antibacterials the course should be limited (e.g. 10 days).
MEROPENEM presumed infections in neutropenic pa- 9.1.2.1 Chloramphenicol Children: Infants given large doses may de-
Pharmacology: Meropenem is a carbapenem tients, septicaemia, 1 g every 8 hours. 9.1.2.2 Quinolones velop exceedingly high plasma levels of the
antibiotic for parenteral use. It is relatively Cystic fibrosis, up to 2 g every 8 hours. 9.1.2.3 Tetracyclines drug because of their immature conjugation
stable to human dehydropeptidase-1(DHP-1) Meningitis, 2 g every 8 hours 9.1.2.4 Macrolides and excretion mechanisms. A life-threatening
Child (>3 months – 12 years): 10-20 9.1.2.5 Aminoglycosides disorder called the ‘gray baby’ syndrome,
compared to Imipenem and therefore does
mg/kg every 8 hours; child >50 kg, 9.1.2.6 Metronidazole characterized by vomiting, refusal to suck and
not require the addition of a DHP-1 inhibitor. 9.1.2.7 Nitrofurantoin
It readily penetrates the cell wall of most adult dose. abdominal distention followed by circulatory
9.1.2.8 Spectinomycin
Gram-positive & Gram-negative bacteria and Child (4-18 years) with cystic fibrosis, collapse, may appear when the plasma con-
9.1.2.9 Sulfonamides and trimethoprim
binds with penicillin-binding protein (PBP) 25-40 mg/kg every 8 hours; Meningi- 9.1.2.10 Lincosamides centration exceeds 20 mg/L.
resulting in inhibition of cell wall synthesis. tis, 40 mg/kg every 8 hours. 9.1.2.11 Vancomycin Thiamphenicol is a chloramphenicol analog
Elderly: No dosage adjustment for the elderly with
The ease with which it penetrates bacterial that is generally less active than chloram-
normal renal function or creatinine clearance values
cell walls, its high level of stability to all serine >50 mL/min.
9.1.2.1 Chloramphenicol phenicol but is equally active against Str.
beta-lactamases and its marked affinity for Hepatic impairment: No dosage adjustment Chloramphenicol is available as the free com- pyogenes, Str. pneumoniae, H. influenzae and N.
the penicillin-binding protein (PBP) explain required. pound (which is extremely bitter) or as the pal- meningitidis, including some strains resistant
the potent bactericidal action of Meropenem Renal impairment: Reduce dose in patients mitate ester for oral administration; as the free to chloramphenicol. It is more actively bacte-
against a broad spectrum of aerobic and with creatinine clearance <51 mL/min. as compound for topical use; and as the sodium ricidal against Haemophilus and Neisseria spp.
anaerobic bacteria. Metabolized by hydrolysis shown below: succinate for injection. Suspensions for oral ad- Unlike chloramphenicol, it is not a substrate
of the beta-lactam ring to micobiologically ministration to children contain chloramphen- for hepatic glucuronyl transferase; it is not
Creatinine Dose
inactive metabolite. Renally excreted (about Clearance based on unit doses of: Frequency icol palmitate, a tasteless and bacteriologically eliminated by conjugation, and its half-life is
70% of the dose excreted unchanged within 12 (mL/min). 500 mg, 1 g, 2 g
inert compound, which is hydrolyzed in the gut not affected by phenobarbital induction. It
hours); faecal excretion accounts for about 2%. 26-50 1 unit dose q12 hrs to liberate chloramphenicol. Pancreatic lipase exerts a greater dose-dependent reversible de-
Indications: Pneumonias and nosocomial 10 – 25 ½ unit dose q12 hrs is deficient in neonates and, because of poor pression of hemopoiesis and immunogenesis
pneumonias, urinary tract infections, intra-ab- <10 ½ unit dose q24 hrs hydrolysis, the palmitate should be avoided. than chloramphenicol, and has been used for
dominal infections, gynaecological infections In very young infants, deficient ability to form its immunosuppressive effect.
Administration: Give Meropenem as an IV bolus
such as endometritis, skin and skin structure glucuronides, and low glomerular and tubular Adult dosage by mouth is 1.5–3 g per day in
injection (5-20 mL) over approx. 5 minutes or by IV
infections, meningitis, septicaemia. As mon- infusion over approx. 15-30 minutes. For bolus IV excretion greatly prolong the plasma half-life. divided doses depending on severity of infec-
368 | 9.1.2.1 Chloramphenicol 9.1.2.2 Quinolones | 369
tion. Therapeutic doses (1–1.5 g) are likely to • Encourage adequate intake of fluids. Injection, Chloramphenicol 1 g per vial. Suspension, Chloramphenicol 125 mg per 5 mL.
depress erythropoiesis in the elderly or others • Observe closely for superinfection by nonsuscep- Pack: 1 g x 10’s (in vial). Pack: 100 mL.
with impaired renal function. tible organisms.
POM CEFANAM® (Elbe) POM ELISCA® (Medreich)
Dose: Infections due to susceptible organisms Injection, Chloramphenicol. Capsule, Chloramphenicol 250 mg; ivory cap.
References: (not susceptible to other antimicrobi-
1) Wilcox MH. Chloramphenicol and thia- Dry syrup, Chloramphenicol 125 mg per 5 mL; yellow
als), by mouth or by IV injection or IV POM CHLOMACOL® (Geneith)
suspension.
mphenicol. In: Finch RG, Greenwood D, infusion, ADULT and CHILD 50 mg/ Capsule, Chloramphenicol 250 mg.
Injection, Chloramphenicol sodium succinate BP
Norrby SR, Whitley RJ, eds. Antibiotic and kg daily in 4 divided doses; up to
250 mg – 10 x 10’s.
equiv. to Chloramphenicol 1 g; dry powder for
chemotherapy. 9th ed. Available from: 100 mg/kg daily in divided doses in POM CHLORACETIN® (Hochiez) reconstitution in a vial.
www.clinicalkey.com (login required) severe infections such as meningitis, Injection, Chloramphenicol (as sodium succinate)
POM LORASIN® (Vixa)
septicaemia, and haemophilus epiglot- 1 g; in vial.
CHLORAMPHENICOL Capsule, Chloramphenicol 250 mg; white or slight
Pack: 10’s; 25’s; 50’s.
titis (reduce high doses as soon as yellow odourless powder in capsule.
Indications: Severe life-threatening infections, clinically indicated); NEONATE under POM CHLORAF® (Afrab-chem) 250 mg – 10 x 10’s; 1000’s.
particularly those caused by Haemophilus 2 weeks 25 mg/kg daily in 4 divided Suspension, Chloramphenicol (as palmitate) 125 Injection, Chloramphenicol sodium succinate 1 g.
influenzae, and typhoid fever; also, pneumonia; doses; INFANT 2 weeks to 1 year 50 mg per 5 mL. Pack: 10’s.
cerebral abscess; mastoiditis; rickettsia; relaps- mg/kg daily in 4 divided doses. Pack: 60 mL; 100 mL.
POM MEDIPHENICOL® (Jubilee)
ing fever; gangrene; granuloma inguinale; lis- Epidemics of meningococcal meningi- POM Chloramphenicol (Emzor) Capsule, Chloramphenicol 250 mg.
teriosis; plague; psitticosis; tularaemia; Whipple tis, by IM injection (of oily injection), Capsule, Chloramphenicol palmitate 250 mg; white Injection, Chloramphenicol sodium succinate BP
disease; septicaemia; meningitis. ADULT 3 g as a single dose, repeated cap. marked ‘EMZOR’ and ‘250’. equiv. to Chloramphenicol 1 g; in vial.
Contra-indications: Pregnancy (Appendix after 48 hours if necessary; INFANT 250 mg – 1000’s Pack: 1 g x 1’s (in vial).
2); porphyria. 1–8 weeks 250 mg as a single dose, POM NAMPHENICOL ®(NASDMU)
POM Chloramphenicol (Jawa)
Precautions: Avoid repeated courses and pro-
EMDEX
2–11 months 500 mg as a single dose; Injection, Chloramphenicol 1 g Capsule, Chloramphenicol 250 mg; cream coloured
longed use; reduce dose in hepatic impairment child 1–2 years 1 g as a single dose, Pack: 10 x 50’s (in vials) cap. marked ‘NAMPHE 250 mg’.
(Appendix 5) and severe renal impairment 3–5 years 1.5 g as a single dose, 6–9 Pack: 500.
POM Chloramphenicol (Mopson)
(Appendix 4); blood counts required before years 2 g as a single dose, 10–14 years Suspension, Chloramphenicol palmitate 125 mg POM RICHPHENICOL® (GoldMoore)
and during treatment; monitor plasma concen- 2.5 g as a single dose, over 15 years per 5 mL Injection, Chloramphenicol (as sodium succinate) 1 g
trations in neonates (see below); breastfeeding as for adult; dose repeated after 48 Pack: 100 mL Pack: 1 g in vial.
(Appendix 3); interactions: Appendix 1. hours if necessary. POM Chloramphenicol (Nichben) POM SIVOPHENICAL® (Adpharm)
Adverse effects: Bone marrow depression— Reconstitution and Administration: According to
Capsule, Chloramphenicol 250 mg. Capsule, Chloramphenicol 250 mg
reversible and irreversible aplastic anaemia manufacturer’s directions. The oily injection is for 250 mg – 1 x 10’s; 1 x 1000’s.
250 mg – 20’s; 100’s.
(with reports of leukaemia), anaemia, leu- intramuscular use only (see notes above).
Syrup, Chloramphenicol (as palmitate) 125 mg
kopenia and thrombocytopenia; nocturnal Note: Plasma concentration monitoring required
per 5 mL THIAMPHENICOL
haemoglobinuria; peripheral neuritis and in neonates and preferred in those under 4 years
Pack: 60 mL
optic neuritis; nausea, vomiting, diarrhoea, of age, in the eldely, and in hepatic impairment; POM GBACTIN® (Greenlife)
recommended peak plasma-chloramphenicol POM Chloramphenicol (Onifam) Tablets, Thiamphenicol 250 mg, 500 mg.
dry mouth, stomatitis, glossitis; headache,
concentration (approx. 1 hour after IV injection or Capsule, Chloramphenicol 250 mg. 250 mg – 2 x 8’s.
depression; hypersensitivity reactions includ- infusion) 15–25 mg/litre; pre-dose ‘trough’ concen- 250 mg – 10 x 10’s 500 mg – 3 x 8’s.
ing, rashes, urticaria, fever, angioedema and tration should not exceed 15 mg/litre.
rarely anaphylaxis; grey syndrome (vomiting, POM Chloramphenicol (Pacmai)
greenish diarrhoea, abdominal distension, POM Chloramphenicol (WMF 6.2.2) Capsule, Chloramphenicol 250 mg; hard-gelatin cap. 9.1.2.2 Quinolones
Capsule, Chloramphenicol 250 mg. 250 mg – 10 x 10’s
hypothermia, pallid cyanosis, irregular respira- There are 4 groups of quinolones based on
Oral liquid, Chloramphenicol (as palmitate) 150
tion, circulatory collapse) may follow excessive POM CHLORAPHIN® (Vitabiotics) their antibacterial activity and spectrum.
mg/5 mL.
doses in neonates with immature hepatic Suspension, Chloramphenicol (as palmitate) 125
Powder for injection, Chloramphenicol (as sodium Group 1: Compounds with a narrow antibacte-
metabolism; also reported in infants born to mg per 5 mL
succinate) 1 g; in vial. rial spectrum directed mainly against Entero-
Pack: 100 mL
mothers treated in late pregnancy. Oily suspension for injection, Chloramphenicol (as bacteriaceae e.g. Nalidixic acid.
Advice to patients: Take on empty stomach; sodium succinate) 500 mg/mL; in 2-mL ampoule. POM CHLOROCAP® (Embassy)
take with food if GI upset occurs, at evenly Capsule, Chloramphenicol 250 mg. Group 2: Fluoroquinolones, which exhibit po-
POM Chloramphenicol (EDL 5.3/Restricted List) tent activity against Gram-negative bacilli in-
spaced intervals (every 6 hours around-the- 250 mg – 100’s; 1000’s.
Capsule, Chloramphenicol 250 mg.
clock); notify physician of persistent sore cluding Ps. aeruginosa and many Gram-positive
Oral liquid, Chloramphenicol (as palmitate) 150 POM CHLOZAR® (Shrezar)
throat, tiredness, or unusual bleeding or mg per 5 mL.
bacteria excluding Streptococcus pneumoniae.
Injection, Chloramphenicol (as sodium succinate) 1 g
bruising. Injection, Chloramphenicol (as sodium succinate) 1 Pack: 50 vials These compounds are characterized by a 6-flu-
Nursing action: g; powder in vial. orine atom and often by a 7-piperazinyl group.
POM CLOR®-250 (Mecure) Examples include Ciprofloxacin, Norfloxacin,
• Obtain specimen for C&S test before first dose; POM CAFCHLOR® (Embassy) Capsule, Chloramphenicol 250 mg; white capsule
therapy may begin pending test results. Ofloxacin, Pefloxacin.
Injection, Chloramphenicol (as sodium salt) 1 g. marked ‘CLOR.250’.
• Administer around-the-clock in equal intervals Pack: 50’s. 250 mg – 10 x 10’s. Group 3: Compounds with improved activity
to promote less variation in peak and trough against Str. pneumoniae and Staph. aureus.
serum levels. POM CAFON-250® (Beta Drugs) POM DALCOL® (Justeen)
Capsule, Chloramphenicol BP 250 mg; white or slight Capsule, Chloramphenicol BP 250 mg. Some derivatives do not contain a fluorine
• For I.V. use, give slowly over at least 60 seconds
and check injection site for signs of irritation or yellow, odourless powder in capsule. 250 mg – 1 x 10’s. atom. Examples include Gatifloxacin, Levoflox-
phlebitis. Pack: 10 x 10’s (in blister); 1000’s (in tin). acin, Sparfloxacin.
POM Dr. Meyer’s Clofencol® (Farmex)
370 | 9.1.2.2 Quinolones 9.1.2.2 Quinolones | 371
Group 4: Compounds with properties similar disease (with doxycycline and metronidazole); photosensitivity, hyper-sensitivity reactions Pseudomonal lower respiratory-tract
to those of groups 2 and 3 and additional legionnaires’ disease; meningitis (including including fever, urticaria, angioedema, ar- infection in cystic fibrosis, by mouth,
activity against anaerobes. Examples include meningococcal meningitis prophylaxis); RTIs— thralgia, myalgia, and anaphylaxis; blood ADULT 750 mg twice daily; CHILD
Gemifloxacin, Moxifloxacin. including pseudomonal infections in cystic disorders (including eosinophilia, leukopenia, 5–17 years (see Precautions) up to
Most quinolones are rapidly absorbed when fibrosis, but not pneumococcal pneumonia; thrombocytopenia); disturbances in vision, 20 mg/kg twice daily (maximum 1.5
given orally, although there is considerable UTIs; bone and joint infections; septicaemia; taste, hearing and smell, tinnitus; tenosynovitis; g daily).
variation among different compounds. Ab- anthrax; skin infections; otitis externa; proph- tachycardia, hypotension, oedema, syncope, Surgical prophylaxis, by mouth,
sorption is inhibited by co-administration with ylaxis in surgery. hot flushes and sweating; also isolated re- ADULT 750 mg 60–90 minutes before
antacids containing divalent metals, such as Contra-indications: History of tendon disor- ports of tendon inflammation and damage procedure.
magnesium, calcium and iron, with which they ders related to quinolone use (see also below). (especially in the elderly and in those taking Prophylaxis of meningococcal menin-
form insoluble chelates. Precautions: History of epilepsy or conditions corticosteroids—see also above), haemolytic gitis, by mouth, ADULT 500 mg as a
that predispose to seizures, G6PD deficiency, anaemia, renal failure, interstitial nephritis, single dose.
Fluoroquinolones are not recommended myasthenia gravis (risk of exacerbation), preg- and hepatic dysfunction (including hepatitis
during pregnancy, for lactating women or for POM Ciprofloxacin (WMF 6.2.2)
nancy (Appendix 2), breastfeeding (Appendix and cholestatic jaundice); if psychiatric, neuro- Tablet, Ciprofloxacin (as HCl) 250 mg.
children unless there are overriding reasons for 3), children or adolescents (see below); avoid logical or hypersensitivity reactions (including
their use. Bone and joint arthropathies occur exposure to excessive sunlight (discontinue if severe rash) occur discontinue. POM Ciprofloxacin (EDL 5.3)
mainly in elderly patients when a steroid is Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg.
photosensitivity occurs); rarely, tendon dam- Advice to patients: May be taken with food
co-administered. QTc prolongation and/or Injection, Ciprofloxacin (as lactate) 2 mg per mL; in
age—see below; renal impairment (Appendix to minimize upset to stomach; avoid antacids 50-mL, 100-mL vials.
torsade de pointes has resulted in restriction on 4); avoid excessive alkalinity of urine and en- containing magnesium or aluminium, or Note: Not recommended in children and growing
the use of sparfloxacin. Rarely, tendon rupture sure adequate fluid intake as risk of crystalluria; products containing zinc or iron within 4 hours adolescents.
(especially of the Achilles tendon) may occur interactions: Appendix 1. before or 2 hours after dosing; may cause
EMDEX
especially with ciprofloxacin and levofloxacin. POM ALPHA-CIPRO® (Alpha)
USE IN CHILDREN: Ciprofloxacin causes dizziness or drowsiness; drink fluid liberally.
Caplet, Ciprofloxacin 500 mg.
Nalidixic acid (i.e. Group 1) has very limited arthropathy in the weight-bearing joints of Nursing action: Obtain specimen for C&S test 500 mg – 10’s (in blisters); 100’s (in tin)
clinical use mainly for urinary tract infection. immature animals and is therefore generally before first dose; therapy may begin pending Infusion, Ciprofloxacin 2 mg per mL
Adult oral dose is 900 mg – 1 g every 6 hours not recommended in children and growing test results. Pack: 100 mL
for 7 days. Severe excitatory states, including adolescents. However, the significance of this
• Administer oral dose preferably 2 hours after a meal
(food does not affect absorption but may delay POM BACTACIP® (Foundation)
acute psychoses and convulsions, are usually effect in humans is uncertain and in some spe- peak serum levels); may administer with food to Tablet, Ciprofloxacin 500 mg.
observed in patients receiving high dosages. It cific circumstances short-term use of ciproflox- 500 mg – 10’s.
should be avoided in patients with psychiatric minimize GI upset.
acin in children may be justified. Ciprofloxacin • Advise patient not to take antacid within 2 hr of POM BIOTRICIN® (Next Generation)
disorders or epilepsy. is used for pseudomonal infections in cystic using medication. Tablet, Ciprofloxacin HCl 500 mg; f-c tab
Fluoroquinolones (i.e. Groups 2-4) are available fibrosis (for children over 5 years), and for treat- • Give plenty of fluids to maintain proper hydration 500 mg – 1 x 10’s; 1 x 14’s; 10 x 10’s
in both oral and parenteral formulations but ment and prophylaxis of inhalational anthrax. and urine output.
• Administer by slow IV infusion over 60 minutes POM CEFRODEN® (May & Baker)
because they are well absorbed when given TENDON DAMAGE: Tendon damage (including
to reduce the risk of venous irritation (burning, Caplet, Ciprofloxacin 500 mg.
by mouth, many infectious diseases can be rupture) has been reported rarely in patients 500 mg – 10’s.
pain, erythema and swelling); final concentration
treated successfully with oral therapy. receiving quinolones. Tendon rupture may
for administration should not exceed 2 mg/mL. POM CENOX® (Elbe)
Ciprofloxacin is available as the hydrochloride occur within 48 hours of starting treatment. • Prolonged use may result in overgrowth of Caplet, Ciprofloxacin 500 mg; white caplet.
for oral administration and as the lactate for Healthcare workers should be aware that: non-susceptible organisms; monitor patient for 500 mg – 10’s.
• quinolones are contra-indicated in patients with a symptoms.
intravenous use. It is the most active quinolone Infusion, Ciprofloxacin 200 mg per 100 mL.
history of tendon disorders related to quinolone • Advise patient not to drive or operate machinery
against Ps. aeruginosa but has poor activity use;
Pack: 1 x 100 mL.
against anaerobes. It should be avoided in if dizziness occurs.
• elderly patients are more prone to tendinitis; Dose: Infections due to susceptible organisms, POM CEPHARD® (Watson)
suspected or confirmed infections caused by • the risk of tendon rupture is increased by the Caplet, Ciprofloxacin 250 mg, 500 mg; white.
Str. pneumoniae. by mouth, ADULT 250–750 mg twice
concomitant use of corticosteroids; Pack: 10’s; 20’s.
• if tendinitis is suspected, the quinolone should be daily.
Levofloxacin is the active component of Shilgellosis, by mouth, ADULT 500 mg POM CIFLAXIN® (Drugfield)
discontinued immediately.
ofloxacin. twice daily for 3 days. Infusion, Ciprofloxacin 200 mg, sodium chloride 900
Adverse effects: Nausea, vomiting, dyspepsia,
References: Cholera, by mouth, ADULT 1 g as a mg, water for injection q.s per 100 mL
abdominal pain, flatulence, diarrhoea (rarely Pack: 100 mL
1) Appelbaum PC, Bryskier A. Quinolones. In: antibiotic-associated colitis), pancreatitis, single dose.
Finch RG, Greenwood D, Norrby SR, Whit- dysphagia, tremor, hyperglycaemia, headache, Acute uncomplicated cystitis, by POM CIFRAN® (Ranbaxy)
ley RJ, eds. Antibiotic and chemotherapy. mouth, ADULT 100 mg twice daily for Tablets, (as HCl) 250 mg, 500 mg; both are f-c tabs.
dizziness, sleep disorders, rash (rarely erythema
9th ed. Available from: www.clinicalkey. 3 days. 250 mg – 5 x 10’s; 5 x 20’s; 10 x 10’s.
multiforme (Stevens-Johnson syndrome) and 500 mg – 5 x 10’s; 5 x 20’s; 10 x 10’s.
com (login required) toxic epidermal necrolysis), and pruritus; Gonorrhoea and gonococcal conjunc-
Infusion (IV), Ciprofloxacin (as lactate) 2 mg per mL;
vasculitis, erythema nodosum, petechiae, tivitis, by mouth, ADULT 500 mg as a
in 100 mL plastic bottle.
CIPROFLOXACIN haemorrhagic bullae; less frequently ano- single dose. Pack: 100 mL.
Indications: Gastroenteritis—including rexia, increase in blood urea and creatinine; Chancroid, by mouth, ADULT 500 mg
twice daily for 3 days. POM CIFRAN OD® (Ranbaxy)
cholera, shigellosis, travellers’ diarrhoea, cam- drowsiness, restlessness, asthenia, depression, Tablets, Ciprofloxacin 500 mg, 1000 mg; extended
pylobacter and salmonella enteritis; typhoid; confusion, hallucinations, convulsions, paraes- Pelvic inflammatory disease, by mouth,
release f-c tablets.
gonorrhoea; chancroid; pelvic inflammatory thesia, hypoesthesia, movement disorders; ADULT 500 mg twice daily.
1000 mg – 2 x 5’s (in blister). POM CIPROF® (Diamond Remedies) cap Tablet, Ciprofloxacin 500 mg; white oblong f-c tab.
Caplet, Ciprofloxacin 500 mg; white caplet marked 500 mg – 10’s (in blisters) 500 mg – 100’s.
POM CIKAFLOXIN® (Michelle Lab)
‘CF 500’ on one side and ‘TWL’ on the reverse.
Caplet, Ciprofloxacin (as HCI) 500 mg POM CIPROTAB® (Fidson) POM QUINTOR® (Zoomota)
500 mg – 10.
500 mg – 10’s (in blisters) Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg;
Infusion, Ciprofloxacin 200 mg per 100 mL; clear,
250 mg – 10’s. cream f-c tabs.
POM CIPAD® (Jawa) almost colourless to pale yellow solution in 100 mL
500 mg – 10’s. 250 mg – 10’s; 500’s
Tablet, Ciprofloxacin 500 mg infusion bottle.
Infusion, Ciprofloxacin 0.2 g per 100 mL; clear almost 500 mg – 1 x 10’s.
500 mg – 50 x 10 x10’s Pack: 100 mL.
colourless to pale yellow solution.
POM RAPIDFLOX® (Evans)
POM CIPINE® 500 (Synergy) POM CIPROFIT® (O’Nell) Pack: 100 mL
Tablets, Ciprofloxacin 250 mg, 500 mg.
Tablet, Ciprofloxacin (as HCl) 500 mg; f-c tab. Tablet,Ciprofloxacin 500 mg.
POM CIPROXAMED® (Embassy) 250 mg – 14’s.
500 mg – 5 x 10’s.
POM CIPROFLOX® (Orange Drugs) Tablet, Ciprofloxacin 500 mg. 500 mg – 14’s.
POM CIPOCIL® (Justeen) Tablet, Ciprofloxacin 250 mg 500 mg – 10’s. Infusion, Ciprofloxacin 200 mg per 100 mL.
Tablet, Ciprofloxacin 500 mg. 250 mg – 10’s (in blister) Pack: 100 mL.
POM CIPROZAR® (Shrezar)
Pack: 1 x 10’s. Caplet, Ciprofloxacin 500 mg
Tablet, Ciprofloxacin (as HCI) 500 mg; f-c tab POM SHALCIP® (Shalina)
POM CIPRAJ® (Rajrab) 500 mg – 1 x 10’s (in blisters) IV infusion, Ciprofloxacin 200 mg per 100 mL; clear
Tablet, Ciprofloxacin 500 mg; tab. marked “CIPRAJ POM Ciprofloxacin (Dana) almost colourless to pale yellow solution.
POM CYPLOX® (Medreich)
500” Injection, (IV), Ciprofloxacin (as lactate) 200 mg, Pack: 100 mL (infusion bottle).
Tablets, Ciprofloxacin (as HCl) 250 mg.
500 mg – 10’s sodium chloride 0.9 g, water for injection q.s per
POM TAMAFLEX® (Tamar & Pharez)
100 mL POM DEPMAX® (Dana)
POM CIPRO® (Joswe/Afrab) Tablets, Ciprofloxacin 250 mg, 500mg
Pack: PVC Pouches of 100 mL. Tablets, Ciprofloxacin (as HCI) 250 mg, 500 mg;
Tablets, Ciprofloxacin HCl 250 mg, 500 mg, 750 mg. 250 mg – 1 x 10's
f-c tabs.
250 mg – 10’s POM Ciprofloxacin (E-Globa) 500 mg – 1 x 10's
Pack: 10 x 10’s; 1 x 10’s (in blisters); 100’s; 1000’s (in jar)
EMDEX
500 mg – 10’s IV infusion, Ciprofloxacin 200 mg per 100 mL.
POM THERAFLOX® (Therapeutic)
750 mg – 10’s. Pack: 100 mL x 1’s. POM ELCIP® (GoldMoore)
Caplet, Ciprofloxacin 500 mg.
Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg;
POM CIPROBOND® (Bond) POM Ciprofloxacin (Pemason) 500 mg – 10’s.
f-c tabs.
Caplets, Ciprofloxacin (as HCI) 250 mg, 500 mg Infusion, Ciprofloxacin 0.2 g, sodium chloride 0.9 g
250 mg – 2 x 10’s. POM TREXIP® (Greenlife)
250 mg – 2 x 10’s (in blisters) per 100 mL; water for injection
500 mg – 1 x 10’s. Tablet, Ciprofloxacin 500 mg; f-c tab.
500 mg – 2 x 10's (in blisters)
POM Ciprofloxacin (Superior) 500 mg – 10’s (in blister)
POM EUFLOX® (Eutrix)
POM CIPRO-J® (Juhel) Tablet, Ciprofloxacin 500 mg; f-c tab. Injection, Ciprofloxacin 0.2% w/v, Sodium chloride
Tablet, Ciprofloxacin (as HCl) 500 mg; white, oblong
Caplet, Ciprofloxacin 500 mg; white scored caplet 500 mg – 10 x 10’s (in blisters) 0.9% w/v.
f-c tab.
marked ‘Cipro/500’ on one side and ‘Juhel’ on the Pack: 100 mL.
POM CIPROFUSION® (Hochiez) 500 mg – 100’s.
reverse.
Injection, Ciprofloxacin 0.2 g, Sodium chloride 0.9 g POM VITAPRO® (Strides Vital)
500 mg – 10’s (in blister); 100’s (in tins). POM GECIP® (Geneith)
Pack: 100 mL. Tablet, Ciprofloxacin HCl 500 mg; white capsule
Infusion, (IV), Ciprofloxacin 2 mg per mL. Tablet, Ciprofloxacin (as HCl) 500 mg; f-c tab.
shaped tab. marked ‘VITAPRO’ on one side and
Pack: 100 mL. POM CIPROGATE® (Pharmgate) 500 mg – 10 x 10’s
scored on the reverse.
IV infusion, Ciprofloxacin 200 mg per 100 mL. IV Infusion, Ciprofloxacin 200 mg per 100 mL.
POM CIPROLIFE® (Jawa) 500 mg – 1 x 10’s.
Pack: 100 mL x 1’s. Pack: 100 mL x 1’s
Infusion, Ciprofloxacin 200 mg per 100 mL.
POM ZOCIP® (Bakangizo)
Pack: 100 mL x 1’s (in vial). POM CIPROGEM® (Gemini) POM GLOXIN®-500 (Pharmabase)
Tablet, Ciprofloxacin 500 mg
Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg; Tablet, Ciprofloxacin (as HCI) 500 mg; f-c tab.
POM CIPROBIOTIC® ((Fil Pharma)) 500 mg – 1 x 14’s; 1 x 10’s
lacquer-coated tabs. Pack: 2 x 7’s (in blisters).
Tablets, Ciprofloxacin (as HCl) 250 mg, 500 mg, 750 Injection, Ciprofloxacin 200 mg per 100 mL
250 mg – 10’s; 100’s
mg; film-coated tabs. POM INTERFLOX® (Reals) Pack: 100 mL
500 mg – 10’s; 50’s
250 mg – 1 x 10’s Tablet, Ciprofloxacin (as HCI) 250 mg; f-c tab.
POM ZYPROX® (Mecure)
500 mg – 1 x 10’s POM CIPROLEX® (Med Impex) 250 mg – 3 x 4’s.
Tablet, Ciprofloxacin 500 mg; white, oblong film-
750 mg – 1 x 10’s. Tablet, Ciprofloxacin (as HCl) 500 mg; f-c tab. Caplet, Ciprofloxacin (as HCI) 500 mg; f-c tab.
coated caplet marked ‘ZYPROX MECURE’.
500 mg – 1 x 10’s (in blister). 500 mg – 3 x 4’s.
POM CIPROCAN® (Canopus) 500 mg – 2 x 7’s (in blisters).
Infusion, Ciprofloxacin 200 mg per 100 mL.
Injection, Ciprofloxacin 200 mg per 100 mL POM KRISTAB® (Crystal)
Pack: 100 mL in bottle.
Pack: 100 mL Tablet, Ciprofloxacin 500 mg. CIPROFLOXACIN plus TINIDAZOLE
POM CIPROBACT® (Vinco) 500 mg – 1 x 10’s.
POM CIPROCHEM® (Adler) See under the preparations below.
Tablet, Ciprofloxacin (as HCI) 500 mg; f-c tab Infusion, Ciprofloxacin 200 mg/100 mL.
Tablet, Ciprofloxacin 500 mg.
Pack: 100 mL bottle.
500 mg – 10’s. POM CIPROPAN® (Jopan) POM CIPCOM® (Vatican Bells)
Infusion, Ciprofloxacin Caplet, Ciprofloxacin 500 mg; white f-c caplet POM MIRA-CIPRO®(Miraflash) Tablet, Ciprofloxacin 500mg, Tinidazole 600mg;
Pack: 100 mL. marked ‘JOPAN’ on one side and ‘CP/500’ on the Injection, Ciprofloxacin 200 mg, sodium chloride white caplet.
reverse. 0.9% w/v; in water for injection. Pack: 20’s.
POM CIPRODAC® (Interpharma)
500 mg – 10 x 10’s (in blisters). Pack: 100 mL
Tablet, (250 mg), Ciprofloxacin (as HCl) 250 mg. POM CIPROSTAT+ TN® (Sterling)
Pack: Blister of 10’s. POM CIPROPERTH® (Pemason) POM ORACIP® (Global Organics) Tablet, Ciprofloxacin (as HCl) 500 mg, tinidazole
Tablet, (500 mg), Ciprofloxacin (as HCl) 500 mg. Tablet, Ciprofloxacin 500 mg; white oval scored tab. Injection, Ciprofloxacin (as lactate) 200 mg, sodium 600 mg; f-c tab.
Pack: Blister of 10’s. 500 mg – 14’s (in blisters). chloride 0.9%, water for injection q.s. 100 mL Pack: 10’s (in blisters)
Infusion, Ciprofloxacin 200 mg per 100 mL. Pack: 100 mL
Pack: Bottle of 100 mL. POM CIPROSOFT® (Award Global) POM CIPROX-T® (Teta)
Capsule, Ciprofloxacin (as HCI) 500 mg; soft gelatin POM PROX® (Al-Tinez)
Tablet, Ciprofloxacin (as HCI) 500 mg, tinidazole Acute exacerbations of chronic bronchitis. POM GEMFLOX® (Zolon) flammation in a tendon occurs. May exacerbate
600 mg; f-c tab. Contra-indications: Hypersensitivity to Tablet, Gemifloxacin (as mesylate) 320 mg; f-c tab. muscle weakness in persons with myasthenia
Pack: 10’s quinolones or to any component of the gravis. Avoid in known history of myasthenia
POM CIPTA® (Award Global) preparation. LEVOFLOXACIN gravis. Monitor for anaphylactic reactions,
Tablet, Ciprofloxacin HCI 500 mg, tinidazole 600 Precautions: Maintain adequate hydration Therapeutic category: Antibiotic, Fluoro- hematologic & renal toxicities, and hepato-
mg; f-c tab. to prevent formation of highly concentrated quinolone toxicity. Discontinue immediately if signs
Pack:1 x 10’s (in blisters) urine and crystalluria. Fluoroquinolones may Warnings: Fluoroquinolones, including Levo- and symptoms of hepatitis occur . Caution in
POM GALCIPRO TN (SKG) cause QT prolongation and should not be floxacin, are associated with an increased risk CNS disorders including seizures. Evaluate for
Caplets, Ciprofloxacin 500 mg, Tinidazole 600 mg; used in history of QTc prolongation, uncor- of tendinitis and tendon rupture in all ages. Clostridium difficile-associated colitis if diarrhea
white to off-white oblong rectangular scored tab. rected hypokalaemia, hypomagnesaemia, or This risk is further increased in older patients occurs. Prolongation of the QT interval and
marked ‘CPX TN’. co-administration of other drugs known to usually over 60 years of age, in patients taking isolated cases of torsade de pointes have been
Pack: 10’s prolong the QT interval. Phototoxicity (avoid corticosteroid drugs, and in patients with reported. Avoid use in patients with known
POM TREXIP-TZ® (Greenlife) excessive sunlight). Tendon inflammation or kidney, heart or lung transplants. Fluoro- prolongation, those with hypokalemia, and
Tablet, Ciprofloxacin 500 mg, tinidazole 600 mg; rupture especially with concurrent corticos- quinolones may exacerbate muscle weakness with other drugs that prolong the QT interval.
sunset yellow. teroids and in the elderly. Superinfection with in persons with myasthenia gravis and should Interactions: Absorption may be decreased
Pack: 1 x 10’s. non-susceptible organisms. Renal impairment; be avoided in patients with a known history of when given within 2 hours of multivalent
POM ZYFLOX® (Nalis) Elderly (>65 years). CNS disorder e.g. seizures. myasthenia gravis. cation-containing agents such as antacids,
Tablet, Ciprofloxacin (as HCI) 500 mg, tinidazole CNS stimulation (e.g. tremors, restlessness, Pharmacology: Levofloxacin is a synthetic metal cations or didanosine. May enhance
600 mg; f-c tab light-headedness, confusion, hallucinations, antibacterial agent of the fluoroquinolone effect of Warfarin (monitor patient for signs of
paranoia, depression, nightmares, and insom- class and is the L-isomer of the racemate, oflox- bleeding). Monitor blood glucose in patients
GEMIFLOXACIN nia). History of myasthenia gravis. Diabetes acin. The mechanism of action of levofloxacin on antidiabetic agents.
EMDEX
Therapeutic category: Fluoroquinolone (monitor for hypoglycaemia). and other fluoroquinolone antimicrobials Adverse effects: Most common include
antibiotic. Interactions: QTc-prolonging agents (e.g. involves inhibition of bacterial topoisomerase nausea, headache, diarrhea, insomnia, consti-
Pharmacology: Gemifloxacin is an oral artemether/lumefantrine, halofantrine, azith- IV and DNA gyrase (both of which are type II pation and dizziness.
once daily fluoroquinolone antimicrobial. It romycin, clarithromycin, mefloquine, etc). Class topoisomerases), enzymes required for DNA Dose:
is bactericidal via inhibition of DNA gyrase III antiarrhythmics e.g. amiodarone, sotalol. replication, transcription, repair and recombi- Type of Infection.
Dose every Duration
Preparations containing divalent or trivalent nation. Commonly susceptible species include: 24 hours (days)
(topoisomerase II), an enzyme responsible
Nosocomial pneumonia 750 mg 7-14
for counteracting the excessive supercoiling cations e.g. multivitamin/minerals, antacids, Gram-positive bacteria – Enterococcus faecalis,
Community-acquired
of DNA during replication or transcription iron, zinc, etc. Sucralfate. Antidiabetic agents. Staphylococcus aureus (methicillin-susceptible pneumonia: 7-14 day regimen
500 mg 7-14
and topoisomerase IV, an enzyme that helps Corticosteroids (increased risk of tendon rup- isolates), Staphylococcus epidermidis (methi- Community-acquired
750 mg 5
separate the daughter DNA molecules. Group ture). Non-steroidal Anti-Inflammatory Drugs cillin-susceptible isolates), Staphylococcus pneumonia: 5-day regimen
4 quinolones (e.g. Gemifloxacin and Moxi- (NSAIDs). Warfarin (enhanced anticoagulation). saprophyticus, Streptococcus pneumoniae (in- Acute bacterial sinusitis 750 mg 5
floxacin) have antibacterial spectrum similar Adverse effects: Most commonly diarrhea, cluding multi-drug resistant isolates [MDRSP]), or 10-14 regimen 500 mg 10-14
to those of groups 2 (e.g. Ciprofloxacin) and nausea, vomiting, abdominal pain, rash, Streptococcus pyogenes. Gram-negative bacteria Acute bacterial exacerbation of
500 mg 7
chronic bronchitis
3 (e.g. Levofloxacin), and have additional headache, dizziness. Haematological changes; – Enterobacter cloacae, Escherichia coli, Haemo-
Complicated skin and skin
activity against anaerobes. Like other Fluo- increased hepatic enzymes; overgrowth of philus influenzae, Haemophilus parainfluenzae, structure infections (SSSI)
750 mg 7-14
roquinolones, gemifloxacin exhibits concen- non-susceptible bacteria or fungi. Less com- Klebsiella pneumoniae, Legionella pneumo- Uncomplicated SSSI 500 mg 7-10
tration-dependent pharmacodynamics; and monly photosensitivity, anorexia, arthralgia, phila, Moraxella catarrhalis, Proteus mirabilis, Chronic bacterial prostatitis 500 mg 28
against gram-negative organisms, a prolonged azotemia, constipation, dyspepsia, eczema, Pseudomonas aeruginosa, Serratia marcescens. Complicated UTI or Acute
electrolyte changes, flatulence, gastritis, Other bacteria – Chlamydophila pneumoniae, 750 mg 5
post-antibiotic effect (PAE). pyelonephritis: 5-day regimen
Rapidly absorbed from the GI tract, can be nervousness, pseudomembranous colitis, dys- Mycoplasma pneumoniae. Complicated UTI or Acute
250 mg 10
administered without regard to meals. Time geusia, tendinitis or tendon rupture, Vaginitis, Indications: Treatment of adults (≥18 years pyelonephritis: 10-day regimen
to peak plasma level within 0.5 to 2 hours after visual impairment, xerostomia. of age) with infections caused by designated, Uncomplicated UTI 250 mg 3
a 320-mg oral dose. Absolute bioavailability Advice to patients: Drink lots of fluid to pre- susceptible bacteria. Pneumonia (nosocomial Note: Administer at least 2 hours before or 2 hours
approx. 71%; significantly reduced by antacids. vent over concentration of urine. Avoid driving and community-acquired); Acute bacterial si- after antacids containing magnesium, aluminum,
Highly protein bound (about 60-70%). Less or operating machinery until CNS effects are nusitis; Acute bacterial exacerbation of chronic as well as sucralfate, metal cations such as iron and
than 10% administered dose metabolized established. Avoid excessive exposure to sun- bronchitis; Skin and skin structure infections multivitamin preparations with zinc or didanosine,
light and/or wear sunscreen. (complicated and uncomplicated); Chronic chewable/buffered tablets.
in the liver; cytochrome P450 enzymes not
involved. Excreted primarily as unchanged Dose: Adult, by mouth, 320 mg once daily for bacterial prostatitis; Urinary tract infections (Additional information sourced from Levaquin® monograph
(complicated and uncomplicated); Acute available from: http://www.levaquin.com/)
drug in the faeces and remainder in the urine. 5–7 days.
Mean plasma elimination half-life approx. 7 Administration: May be given with or without food, pyelonephritis.
including milk. Administer at least 2 hours before POM AVOXIN® (Joswe/Afrab)
hours (range 4-12 hours). Contra-indications: Hypersensitivity to Levo- Tablet, Levofloxacin 250 mg.
or 3 hours after aluminum/magnesium-containing floxacin or other quinolones.
No dosage adjustment required in hepatic 250 mg – 7’s.
antacids, ferrous sulfate, dietary supplements Precautions: Increased risk of tendinitis and
impairment; clearance is reduced and plasma containing iron, magnesium, or zinc (such as multi-
tendon rupture esp. in older patients usually POM CELEVOX® (JB Pharma)
elimination is prolonged in patients with renal vitamins), sucralfate. Tablet, Levofloxacin (as hemihydrate) 500 mg; f-c tab.
insufficiency. over 60 years of age, in patients taking corti-
(Additional information sourced from Gemifloxacin monograph 500 mg – 10’s (in blister)
Indications: Community-acquired pneumonia; [1] https://www.clinicalkey.com/ [2] http://www.uptodate.com/)
costeroids, and in patients with kidney, heart
or lung transplants. Discontinue if pain or in- POM DEVOFLOXIN® (Drugfield)
Infusion, Levofloxacin 500 mg, dextrose 5000 mg, q.s. 100 mL Tablet, Levofloxacin hemihydrate 500 mg; f-c tab treatment; history of symptomatic arrhyth-
water for injection q.s per 100 mL Pack: 100 mL (in FFS bottle) 500 mg – 14’s mias; conditions and/or other medications
Pack: 100 mL associated with QT prolongation; Electrolyte
POM LEVOLAB® (Embassy) POM S-FLOX® (Kayhelt)
POM EVAXIN® (Global Heathcare) Injection, Levofloxacin 500 mg per 100 mL Tablets, Levofloxacin 250 mg, 500 mg; f-c tabs. disturbances, particularly in uncorrected hy-
Tablet, Levofloxacin hemihydrate 500 mg; f-c tab. Pack: 100 mL bottle. 250 mg – 10’s (in blisters) pokalaemia; Patients below 18 years of age;
500 mg – 1 x 10’s (in blisters) 500 mg – 10’s (in blisters) Pregnancy and lactation.
POM LEVOMAX® (Pharmgate)
Infusion, (IV), Levofloxacin hemihydrate 500 mg Precautions: Elderly and women with higher
Tablet, Levofloxacin 500 mg POM TAVANIC® (Sanofi-Aventis)
per 100 mL. risk of QTc prolongation; patients with ongoing
500 mg – 1 x 7’s; 1 x 10’s Tablets, Levofloxacin 250 mg; 500 mg.
Pack: 100 mL FFs (bottle for Intravenous infusion)
IV Infusion, Levofloxacin 500 mg per 100 mL 250 mg – 5’s (in blisters) proarrhythmic conditions; potassium-de-
POM FLOXIUM® (Solidum) Pack: 100 mL x 1’s 500 mg – 5’s (in blisters) pleting drugs; hepatic dysfunction; patients
Tablet, Levofloxacin 500 mg; f-c scored tab. IV infusion, Levofloxacin 5 mg per mL; solution for with CNS disorders which may predispose
POM LEVOPAC® (Geneith)
500 mg – 7’s infusion in 100 mL vial. to seizures or lower the seizure threshold;
Injection, Levofloxacin 500 mg.
Pack: 100 mL. myasthenia gravis; tendon inflammation and
POM GLEVO® (Glenmark)
POM LEVOSTAT® (Sterling drugs) rupture may occur with quinolones esp. with
Tablet, Levofloxacin 500 mg; red f-c tab. POM TERLEV® (Micro Nova)
Caplet, Levofloxacin 500 mg
Pack: 2 x 5’s. Tablets, Levofloxacin (as hemihydrate) 250 mg, 500 concurrent corticosteroids; renal dysfunction,
Infusion, Levofloxacin 500 mg per 100 mL. mg, 750 mg; f-c tabs. maintain adequate fluid intake as dehydration
Pack: 100 mL POM LEVOTIL® (May & Baker) 250 mg – 10’s may increase the risk of renal failure; advise
Caplet, Levofloxacin 500 mg. 500 mg – 10’s patient to avoid prolonged exposure to sun-
POM L-FLOX® (PharmacyPlus)
500 mg – 10’s. 750 mg – 10’s.\
Tablet, (500 mg), Levofloxacin 500 mg; f-c tab. light/UV; May impair ability to drive or operate
500 mg – 1 x 10’s; 10 x 10’s (in blisters) POM LEVOWAT® (Watson) POM UNOFLOX® (Barata) machinery.
Tablet, (750 mg), Levofloxacin (as hemiydrate) Tablet, Levofloxacin 500 mg. Tablet, Levofloxacin hemihdrate 500 mg; f-c tab Interactions: Administer 4 hours before or 8
EMDEX
750 mg 500 mg – 10’s (in blisters) hours after ferrous sulfate, dietary supplements
750 mg – 10 x 1 x 10’s POM LEVOX® (Laider)
Tablet, Levofloxacin (as hemihydrate) 500 mg. POM ZARLOX® (Shrezar) containing zinc, magnesium, or iron, or alumi-
IV Infusion, Levofloxacin 500 mg per 100 mL.
Pack: 100 mL 500 mg – 10’s (in blister) Tablets, Levofloxacin hemihydrate 250 mg, 500 num/magnesium-containing antacids; Avoid
mg; f-c tabs co-administration with QTc interval prolonging
POM LEFLOCARD® (Eutrix) POM LEVOXIN® (Evans) 250 mg – 1 x 10’s; 10 x 10’s
Tablets, Levofloxacin 250 mg, 500 mg. drugs such as antiarrhythmics classes IA & III,
Caplet, Levofloxacin 500 mg. 500 mg – 1 x 10’s; 10 x 10’s phenothiazines, haloperidol, erythromycin,
500 mg – 10’s (in blister) 250 mg – 7’s.
500 mg – 7’s. TCAs, etc; co-administration with NSAIDs
POM LEFOVID® (Hovid) MOXIFLOXACIN may increase the risk of CNS stimulation and
Tablet, Levofloxacin hemihydrates 250 mg, 500 POM LEXAMIN® (Korlyns) Therapeutic category: Fluoroquinolone
Tablet, Levofloxacin 500 mg.
seizures.
mg; f-c tabs. antibiotic. Adverse effects: Nausea, vomiting, GI and
250 mg – 1 x 10’s; 3 x 10’s (in blisters) 500 mg – 1 x 12’s (in blister)
Infusion, Levofloxacin (hemihydrate, NaCl) 500 mg
Pharmacology: Moxifloxacin is a synthetic abdominal pains, diarrhoea; Superinfections
500 mg – 1 x 10’s; 3 x 10’s (in blisters) broad spectrum 8-methoxyfluoroquinolone
per 100 mL; clear solution. due to resistant bacteria or fungi e.g. oral
POM LEVOBLISS® (Carebliss) Pack: 100 mL x 1’s. antibacterial agent. The bactericidal action and vaginal candidiasis; Headache, dizziness;
Tablet, Levofloxacin hemihydrate 500 mg; f-c tab of moxifloxacin results from the inhibition of Increase in transaminases. Rarely pruritus,
POM LIFEFLOX® (Lifeback)
500 mg – 10’s both type II topoisomerases (DNA gyrase and rash, arthralgia, myalgia, tendonitis, hepatitis;
Tablets, Levofloxacin 500 mg, 750 mg; f-c tabs.
POM LEVO CEF® (BG Pharmacy) 500 mg – 2 x 5’s topoisomerase IV) required for bacterial DNA CVS & CNS problems, allergic reactions, blood
Tablet, Levofloxacin (as hemihydrate) 500 mg. 750 mg – 2 x 5’s replication, transcription and repair. Moxiflox- dyscrasia.
500 mg – 10’s. acin has in vitro activity against a wide range Dose: To be swallowed whole with sufficient
POM LIVITA® (Vitahealth) of Gm+ve and Gm-ve pathogens. It exhibits a
POM LEVOC® (Fidson) Tablet, Levofloxacin hemihydrate 500 mg; f-c tab fluid and without regard to meals.
Infusion, Levofloxacin 400 mg per 100 mL. concentration dependent killing rate. By mouth, Adult, 400 mg once every
500 mg – 1 x 10’s
Pack: 100 mL Following oral administration moxifloxacin is 24 hours; duration depends on the
POM LOXACIN® (Vixa) rapidly and almost completely absorbed with type of infection
POM LEVODOSE® (Crystal) Tablet, Levofloxacin 500 mg absolute bioavailability of approx. 91%. It is
Tablet, Levofloxacin 500 mg. 500 mg – 1 x 10’s Daily Dose Duration
mainly bound to serum albumin. Moxifloxacin Infection
500 mg – 1 x 10’s. (mg) (days)
POM LOXOF® (Ranbaxy) undergoes Phase II biotransformation and is Acute bacterial sinusitis 400 10
POM LEVOFAB® (FAB) Tablet, (250 mg), Levofloxacin 250 mg; f-c tab. excreted via renal and biliary/faecal pathways Acute bacterial exacerbation of
Tablet, Levofloxacin hemihydrate 500 mg 250 mg – 10’s (in blister). 400 5
as unchanged drug as well as in the form of chronic bronchitis
500 mg – 7’s (calender pack) Tablet, (500 mg), Levofloxacin 500 mg; f-c tab. Community-acquired
inactive metabolites. 400 7-14
500 mg – 10’s (in blister). pneumonia
POM LEVOFLOX® (Coriander) Indications: Treatment of adults (>18 years
Uncomplicated skin and skin
Caplet, Levofloxacin 500 mg POM MAFLOXIN® (Pemason) of age) with infections caused by susceptible 400 7
structure infections
500 mg – 10’s (in blister) Caplet, Levofloxacin (as hemihydrate) 500 mg; white strains: Acute bacterial sinusitis; Acute bacterial
oblong scored tab. By IV infusion (over a period of 60
POM Levofloxacin (Biostadt) exacerbation of chronic bronchitis; Community
500 mg – 7’s (in blisters) minutes), when switching from IV to
Tablet, Levofloxacin 500 mg; f-c tab. acquired pneumonia; Uncomplicated skin and
oral, no dosage adjustment is neces-
500 mg – 1 x 10’s (in blisters) POM NIRLIV® (Jawa) skin structure infections.
sary. Avoid IM, intrathecal, intraperito-
POM LEVOGOL® (Global Organics)
Infusion, Levofloxacin 500 mg. Contra-indications: Hypersensitivity to
500 mg – 100 mL (in vial). neal or SC administration.
Infusion, Levofloxacin (as hemihydrate) 500 mg, moxifloxacin or other quinolones; history of
tendon disease/disorder related to quinolone (Additional information sourced from Avelox monograph: http://
glucose (anhydrous) 5% w/v, water for injection POM SEVOXACIN® (Next Generation)
www.medicines.org.uk/) medication, do not skip doses; do not take Tablet, Norfloxacin 400 mg; f-c tab. marked ‘APO 200’.
with antacids. 400 mg – 1 x 10’s (in blister). 200 mg – 100.
POM AVELON® (Bayer Schering) Nursing action:
Tablet, Moxifloxacin 400 mg. POM ASKARIVID® (Diamond Remedies)
• Give 1 hr before or 2 hr after meals. OFLOXACIN Tablet, Ofloxacin 200 mg; uncoated tab.
400 mg – 5’s; 10’s. • Antacids and iron products may hinder absorption.
IV Infusion, Moxifloxacin 400 mg per 250 mL.
Therapeutic category: Quinolone Antibiotic. 200 mg – 10’s (in blister).
• Encourage patient to increase fluid intake to avoid Indications: Bacterial infections due to oflox-
Pack: 250 mL. crystallization in kidneys. POM B-FLOX® (Boucia)
acin sensitive pathogens: respiratory tract Tablet, Ofloxacin 200 mg; f-c tab
POM MICROMAX® (Micronova) • Advise patient to avoid hazardous activities which
infections including ENT infections; infections 200 mg – 10’s
Tablet, Moxifloxacin (as HCI) 400 mg; f-c tab require alertness and good coordination.
• Assist with ambulation if dizziness occurs. of soft tissue and skin; infections of the abdom-
400 mg – POM BGVID® (BG Pharmacy)
• Advise limited intake of foods and drugs that inal cavity including the pelvis, minor bacterial
POM MOXIF® IV (Zoomota) Tablet, Ofloxacin 200 mg; f-c tab.
contain alcohol, milk, dairy products, vegetables, enteritis; infections of the kidneys, urinary tract 200 mg – 10’s (in blister)
IV Infusion, Moxifloxacin 400mg/100ml; colourless sodium bicarbonate and antacids. and genital organs including gonorrhoea.
solution. Contra-indications: Hypersensitivity to oflox- POM DABAFLOX® (Dabak)
Dose: Treatment, by mouth, 400 mg 2 times
Pack: 100 mL flexi bottle. Tablets, Ofloxacin 200 mg
daily: UTI, 7-10 days; Uncomplicated acin or other quinolone-carboxylic acid deriv-
POM MOXIGET® (Getz) Pack: 2 x 7’s
acute cystitis, 3-7 days; Chronic ative; epileptics, children and adolescents in
Tablet, Moxifloxacin 400 mg; f-c tab relapsing UTI, up to 12 weeks; Acute the growth phase, pregnancy, breast feeding. POM ECOFLOCIN® (Pinnacle)
400 mg – 5’s (in blisters) bacterial gastroenteritis, 5 days. Interactions: Preparations containing divalent Tablet, Ofloxacin 200 mg; f-c tab.
POM MOXIGET® IV (Getz) Acute gonococcal urethritis, pharyngi- or trivalent cations such as antacids, haematin- 200 mg – 10’s (in blisters).
IV Infusion, Moxifloxacin (as HCI) 400 mg per 250 mL. tis, proctitis or cervicitis, 800 mg as a ics (cause attenuation of the ofloxacin effect). POM ENDOVID®-200 (Embassy)
Pack: 250 mL single dose. See also under Ciprofloxacin. Tablet, Ofloxacin 200 mg; f-c tab
POM MOXIMED® (Evans) Typhoid fever, 400 mg 3 times daily Adverse effects: Allergic reactions, haemor- 200 mg – 1 x 10’s.
EMDEX
Tablet, Moxifloxacin (as HCl) 400 mg; f-c tabs. for 14 days. rhages, CVS disturbances, pain in joints and POM EUTRIXIN® (Eutrix)
400 mg – 5’s. Prophylaxis: Sepsis of profound Neutro- muscles, blood dyscrasias, GI disturbances; Tablet, Ofloxacin 200 mg; white, oblong f-c tab.
penia, 400 mg 3 times daily; transient rise of serum creatinine, liver enzymes
POM P-MOXIN® (Pinnacle) POM FLOBACIN® (Justeen)
Tablet, Moxifloxacin (as HCI) 400 mg; f-c tab Bacterial gastroenteritis, 400 mg daily, and bilirubin levels.
Tablet, Ofloxacin BP 200 mg.
400 mg – 10’s (in blisters) 24 hours before arrival and 48 hours Advice to patients: Report any skin rash or Pack: 1 x 10’s.
after leaving endemic areas. allergic reactions; avoid excessive sunlight; do
not take with food; do not take within 2 hours POM FLOVID® (Hovid)
NALIDIXIC ACID POM E-NOR®-200 (Embassy)
of any products including antacids which con- Tablet, Ofloxacin 200 mg; f-c tab
Therapeutic category: Quinolone antibiotic. Tablet, Norfloxacin BP 400 mg. 200 mg – 1 x 10’s; 10 x 10’s
400 mg – 1 x 10’s. tain zinc, magnesium, or aluminium.
See clinical notes above. Nursing action: See under Ciprofloxacin. POM FLOXAN® (Pharmabox)
POM NARACIN® (Seagreen) Tablet, Ofloxacin 200 mg; white, oval, f-c tab.
Dose: By mouth, Adult, Uncomplicated cysti-
POM NALDIX® (Adler) Tablet, Norfloxacin 400 mg; f-c tab 200 mg – 10’s; 100’s; 500’s; 1000’s.
Tablet, Nalidixic acid 400 mg – 1 x 10’s tis, 200 mg twice daily for 3-7 days de-
Pack: 10 x 10`s pending on the organism; extended POM FLOXUR (Zoomota)
POM NORBACTIN® (Ranbaxy) to 10 days in complicated UTI. Tablets, Ofloxacin 200 mg, 400 mg; white f-c tabs.
Tablet, Norfloxacin USP 400 mg. Uncomplicated urethral and cervical 200 mg – 10’s (in blister)
NORFLOXACIN 400 mg – 5 x 10’s; 10 x 10’s.
gonorrhoea, 400 mg as a single dose. 400 mg – 10’s (in blister)
Therapeutic category: Quinolone antibiotic.
POM NORDANA® (Dana) Nongonococcal urethritis/cervicitis due POM GFLOX® (Greenlife)
Indications: Broad spectrum bactericidal
Tablet, Norfloxacin 400 mg; f-c tab to Chlamydia trachomatis, 200-300 Tablet, Ofloxacin 400 mg; f-c extended-release tab.
agent for urinary tract infections; acute bac- 400 mg – 1 x 10’s; 10 x 10’s (in blisters)
terial gastroenteritis; gonococcal urethritis, mg twice daily for 7 days. 400 mg – 1 x 10’s
pharyngitis, proctitis or cervicitis; typhoid POM NORFEN® (Interpharma) Lower respiratory tract infections, 400 POM LOXAT® (Pharmaplus)
fever; prophylaxis of sepsis in neutropaenic Tablet, Norfloxacin 400 mg; f-c tab. mg twice daily for 7-10 days. Tablet, Ofloxacin 200 mg; f-c tab.
400 mg – 10’s. Uncomplicated skin & soft-tissue infec- 200 mg – 10’s
patients, bacterial gastroenteritis.
Contra-indications: Hypersensitivity to nor- POM NORXIN® (Pharmabox) tions, 400 mg twice daily for 10 days.
POM LOXINTER® (Reals)
floxacin or to other quinolone antibacterials. Tablet, (200 mg), Norfloxacin 200 mg; orange cap. Typhoid fever caused by susceptible Tablet, Ofloxacin 200 mg; f-c tab.
Precautions: Reduce dose in renal impairment; containing white powder. organism, 200-400 mg twice daily for Pack: 3 x 10’s; 10 x 10’s (in blisters).
pregnancy, breast-feeding; not recommended
200 mg – 10’s; 100’s; 500’s 7-14 days.
Tablet, (400 mg), Norfloxacin 400 mg; blue/white Dosing in renal impairment based on creati- POM MEVID® (Jubilee)
for prepubertal children; history of convulsions. cap. containing white powder. Tablets, Ofloxacin 200 mg, 400 mg.
Interactions: Probenecid, nitrofurantion, the- nine clearance (CC):
400 mg – 10’s; 100’s; 500’s POM NEFLOX® (Nelpharm)
ophylline, cyclosporine, sucralfate. CC (mL/min) Dose Interval
POM SURFLOX® (Medreich) 10-50 adult dose 24 hourly Tablet, Ofloxacin 200 mg
Adverse effects: GI, neuropsychiatric and 200 mg – 1 x 10’s
Tablet, Norfloxacin 400 mg; orange f-c tab. marked <10 ½ adult dose 24 hourly
skin reactions including nausea, headache,
“Surflox 400” on one side and “M+” on the reverse. POM OFAXIN® (Mecure)
dizziness, rash, and diarrhoea. POM Ofloxacin (EDL 5.3/Restricted List)
Advice to patients: Tablets should be taken POM UREKACIN® (Vixa) Tablet, Ofloxacin 200 mg.
Tablet or Capsule, Ofloxacin 200 mg
at least 1 hour before or 2 hours after a meal Tablet, Norfloxacin 400 mg. Injection , Ofloxacin 100 mg/50 mL, 200 mg/100ml. POM OFLEXIN® (Adler)
Pack: 10’s.
with a glass of water; patients receiving nor- Infusion, Ofloxacin 200 mg per 100 mL.
POM APO-OFLOX® (Lahams)
floxacin should be well hydrated; take all the POM ZEFLOX® (Fil Pharma) Pack: 100 mL.
Tablet, Ofloxacin 200 mg; light yellow, oval, f-c tab.
POM OFLODAN® (Dana) 400 mg – 10’s Adverse effects: Gastric pain, nausea, vomiting; Pack: 5.
Tablet, Ofloxacin 200 mg; f-c tab allergic skin reactions and photosensitivity;
POM VOXIN® (Geneith) POM PEFLOBID® (Interpharma)
200 mg – 10’s (in blisters) muscular and/or joint pain, tendinitis, rupture
Tablet, Ofloxacin 200 mg Tablet, Pefloxacin (as methanesulfonate dihydrate)
POM OFLODEX® (Pemason) 200 mg – 4 x 10’s of Achilles tendon; thrombocytopenia and 400 mg.
Caplet, Ofloxacin 200 mg. neutropenia; neurological disorders (head- 400 mg – 10 x 10’s.
POM ZANOCIN® (Ranbaxy)
aches, insomnia, myoclonia, convulsions). Infusion, Pefloxacin (as methanesulfonate dihydrate)
POM OFLOFLOX® (O’Nell) Tablets, Ofloxacin 100 mg, 200 mg; both are f-c tabs.
Advice to patients: Can be taken without 400 mg per 100 mL.
Tablet, Ofloxacin 400 mg. 100 mg – 10 x 10’s; 5 x 20’s.
regards to meals. Pack: 5.
200 mg – 10 x 10’s; 5 x 20’s.
POM OFLOHANS® (Visko) Dose: Adult, by mouth, Gonococcal urethritis,
Tablets, (OD), Ofloxacin 400 mg, 800 mg; extended POM PEFLOMED® (Evans)
Tablet, Ofloxacin 200 mg
release f-c tabs. 800 mg as a single dose; Tablet, Pefloxacin 400 mg.
200 mg – 1 x 10’s
400 mg – 2 x 5. Gonococcal infection in women, 400 400 mg – 14’s.
POM OFLOHANS-D® (Visko) 800 mg – 2 x 5. mg twice daily for 5 days; POM PEFLOTAB® (Fidson)
Tablet, Ofloxacin 400 mg Infusion, Ofloxacin 2 mg per mL; in 100 mL plastic Chancroid and cystitis, 800 mg as a Tablet, Pefloxacin (as mesylate dihydrate) 400 mg
400 mg – 10 x 10’s bottle.
single dose; 400 mg – 10.
Pack: 1.
POM OFLOMED® (Evans) Salpingitis and endometritis, 400 mg
POM PEMAX® (Pharmabox)
Tablet, Ofloxacin 200 mg. POM ZOIXF® (Bakangizo) twice daily for 10 days; Tablet, Pefloxacin (as methanesulfonate dihydrate)
200 mg – 14’s. Tablet, Ofloxacin 20 mg Urinary tract infection (pyelonephritis), 400 mg; white rectangular f-c tab.
20 mg – 1 x 14’s (in blisters) 400 mg twice daily for 10-20 days. 400 mg – 10’s; 1000’s.
POM OFLOMORE® (Crystal)
Tablet, Ofloxacin 200 mg. Typhoid fever and bacterial diarrhoea,
PEFLOXACIN POM PERIKACIN® (Vixa)
200 mg – 1 x 10’s. 400 mg twice daily for 7 days; Tablet, Pefloxacin (as mesitate dehydrate) 400 mg;
Pharmacology: Pefloxacin is a synthetic fluo- Surgical abdominal infections, 400 mg scored f-c tab.
POM OFLOVIN® (Vinco)
EMDEX
Tablet, Ofloxacin 200 mg; f-c tab roquinolone antibiotic. It can be administered twice daily (include ampicillin if Strep- 400 mg – 10’s; 50’s.
200 mg – 10’s both orally and intravenously, and has a broad tococci or metronidazole if anaero- Injection, Pefloxacin (as mesitate dehydrate) 400 mg
spectrum of in vitro activity against gm-ve bic); Peritonitis, 400 mg twice daily per 5 mL; solution for infusion in amp.
POM Ofloxacin-200 (Neros) organisms and staphylococci. It is rapidly and Pack: 5’s.
(include ampicillin I.V. if Streptococci);
Tablet, Ofloxacin 200 mg; f-c tab.
nearly completely absorbed after oral adminis- Hepatic abscess, 400 mg twice daily POM PINOX® (Elbe)
tration; metabolised in the liver to norfloxacin (include metronidazole if anaerobic). Tablet, Pefloxacin.
POM OLOX® (Medreich) and pefloxacin N-oxide; excreted in the urine as To be taken with meals to avoid GI Pack: 10 x 10’s.
Tablets, Ofloxacin 200 mg, 400 mg; f-c tabs. unchanged product and the glucuronide and disturbances
Pack: 10’s; 20’s; 100’s (in blisters)
N-oxide metabolites. Serum levels not affected By slow IV injection (one hour), 400 SPARFLOXACIN
POM ONIFLO® (Onifam) by renal impairment. mg, diluted in 250 mL of isotonic Therapeutic category: Quinolone antibiotic
Tablet, Ofloxacin 200 mg Indications: Complicated UTIs; nosocomial glucose solution, twice daily (one Pharmacology: Sparfloxacin is a fluoro-
200 mg – 1 x 10’s lower respiratory tract infections (RTIs); septi- injection in the morning and one in quinolone antibacterial agent with activity
POM OXAFLOX®(Hugo) caemia and surgical infections; gynaecological the evening). against a broad range of gm-ve and gm+ve
Tablet, Ofloxacin 200 mg infections; soft-tissue infections; intra-abdom- organisms including S. pneumoniae. It pre-
POM ABAKTAL® (Taylek)
200 mg – 10 x 1 inal infections; bone and joint infections; men- Tablet, Pefloxacin 400 mg. vents bacterial growth primarily by inhibiting
POM OXAVID® (May & Baker) ingitis; ENT infections; cystitis; gonorrhoea; 400 mg – 10’s; 10 x 10’s. the action of DNA gyrase.
Caplet, Ofloxacin 200 mg; scored caplet marked also in infections in immuno-compromised Injection, Pefloxacin 400 mg per 5 mL It is readily absorbed after oral administra-
“MBN” and “Flox 200”. patients; febrile episodes in neutropenic pa- Pack: 10’s. tion. Oral bioavailability is 90%. It penetrates
200 mg – 10’s; 10 x 10’s. tients; prevention of septicaemia produced extensively into the tissue. Peak concentra-
POM CRIFLACIN® (Crystal)
POM RADOFLOX® (Seagreen)
by gram-negative bacilli in neutropenic cancer Tablet, Pefloxacin 400 mg. tion in bronchopulmonary tissues, alveolar
Tablet, Ofloxacin 200 mg; f-c tab patients. See also under the dose. 400 mg – 1 x 10’s. macrophages and sputum exceed plasma
200 mg – 1 x 10’s Contra-indications: Hypersensitivity to concentration. It is about 40% bound to plasma
pefloxacin and the quinolone derivatives; POM FLOXAL® (Pharmabase)
POM SIVOCIN® (Adpharm) Tablet, Pefloxacin 400 mg (as Pefloxacin methane proteins. The drug has a long elimination half
children up until the end of the growth period; life of about 15-20 hours and is excreted mainly
Tablet, Ofloxacin 200 mg sulphonate dihydrate); f-c tab.
200 mg – 1 x 10’s.
glucose-6-phosphate-dehydrogenase defi- 400 mg – 2 x 7’s (in blisters). by non-renal mechanisms.
ciency; pregnancy lactation; previous history Elimination of the drug is mainly via metabo-
POM TARIVID® (Sanofi-Aventis) of tendinopathy with fluoroquinolone. POM LOXAPEF® (May & Baker)
Tablet, Ofloxacin 200 mg; f-c tab. Caplet, Pefloxacin 400 mg; scored caplet marked lism to its inactive acyglucuronide derivative
Precautions: Photosensitisation reaction and subsequent faecal excretion. The presence
200 mg – 10’s; 100’s. “MBN” and “PEF 400”.
(avoid exposure to sunlight or UV radiation 400 mg – 10’s; 5 x 10’s. of food has no influence on absorption or
POM TOROFLOX® (Toro) during treatment); tendinitis (discontinue excretion of Sparfloxacin.
Tablet, Ofloxacin 200 mg. treatment); severe hepatic insufficiency (ad- POM PEFLAC® (Al-Tinez)
Tablet, Pefloxacin mesilate 400 mg
Indications: Community acquired pneumonia;
200 mg – 10’s; 100’s. just dose).
400 mg – 2 x 7’s Lower respiratory tract infections including
POM TRAFLOX® (NGC) Interactions: Antacids containing aluminium acute exacerbations of chronic obstructive
Caplet, Ofloxacin 200 mg; f-c tab. and/or magnesium gel (absorption of peflox- POM PEFLACINE® (May and Baker) pulmonary diseases; Sinusitis; Gonococcal and
200 mg – 10’s; 100’s acin is decreased). Theophylline (co-admin- Tablet, Pefloxacin 400 mg; coated tab.
non-gonococcal urethritis.
istration will prolong the serum half-life of 400 mg – 50.
POM UROSTAT® (Tamar & Pharez) Injection, Pefloxacin 400 mg per 5 mL. Contra-indications: Infants, children and
Tablet, Ofloxacin 400 mg theophylline).
382 | 9.1.2.3 Tetracyclines 9.1.2.3 Tetracyclines | 383
growing adolescents because of the risk of ar- POM SPARBACT® (IPCA) toin and barbiturates decrease the half-life of erythema (discontinue treatment); photo-sen-
thropathy; history of hypersensitivity reactions Table, Sparfloxacin 200 mg; f-c tab. doxycycline through enzyme induction. The sitivity; hypersensitivity reactions; headache
to it and other quinolones; history of photo- 200 mg – 6’s efficiency of oral contraceptives is reduced by and visual disturbances; hepato-toxicity, blood
sensitivity reactions; Patients with known QT POM SPARDIUM® (Solidum) tetracyclines, as with many other broad-spec- disorders, pancreatitis, and antibiotic-associ-
prolongation and in patients receiving drugs Tablet, Sparfloxacin 200 mg; f-c scored tab. trum antibiotics. ated colitis reported; staining of growing teeth
known to prolong the QT interval. 200 mg – 6’s and occasional dental hypoplasia.
They are used as part of multidrug regimens
Precautions: Signs of photosensitivity (skin POM SPARFLOX 200® (Fidson) for the management of gastritis and peptic Advice to patients: See labels 6, 9, 11 and 27.
burning, redness, rash, itching, dermatitis, Tablet, Sparfloxacin 200 mg; f-c tab. ulcer disease associated with H. pylori. Their Avoid unnecessary exposure to sunlight. Take
blister); pain, inflammation or tendon rupture; 200 mg – 1 x 10’s. activity against malaria has become important until gone; do not skip doses.
pregnancy, lactation. for prophylaxis following the rapid increase Nursing action: Obtain specimens for C&S
POM SPARMAX® (Elbe)
Interactions: Digoxin; avoid co-administration Tablet, Sparfloxacin. of chloroquine– and mefloquine-resistant tests prior to the first dose; administer around-
with QT prolonging drugs (e.g. Terfenadine, Pack: 10 x 10’s. Plasmodium falciparum. the-clock in equal intervals to promote less
Astemizole, Erythromycin, Class 1A and 111 variation in peak and trough serum levels.
anti-arrhythmic agents); antacids (containing POM SPLOX® (Mecure) Doxycycline is rapidly absorbed from the upper • May give with meals to decrease GI upset; with a
Tablet, Sparfloxacin 200 mg. gastrointestinal tract and food, especially dairy full glass of water.
Aluminium/Magnesium), ferrous sulfate and
sucralfate may reduce absorption. POM ZAGAM® (Vixa) products, reduces peak serum concentrations • Tablets or capsules should not be taken within an
Adverse effects: GI disturbances (diarrhoea, Tablet, Sparfloxacin 200 mg by 20%. Alcohol also delays absorption. It is hour of bed time because dysphagia may occur.
200 mg – 1 x 10’s widely used due to its once-daily administra- • Give drug 2 hours before or after laxative or iron
nausea and vomiting); CNS effects (Insomnia products and 3 hours after antacid or kaolin-pectin
and other sleep disorders); photosensitivity; tion and safety in renal insufficiency.
products.
tendinitis or tendon rupture; rarely, convul- 9.1.2.3 Tetracyclines Minocycline absorption is not affected signifi- • Anti-emetic may be given if nausea or vomiting
sions; prolongation of QT interval. Tetracyclines are broad-spectrum, essentially cantly by food but is reduced by co-administra- persists.
EMDEX
Dose: Its long elimination half-life permits bacteriostatic agents. They are against many tion with milk. Its use is associated with higher Dose: Infections due to susceptible organisms,
once daily dosage. Gram-positive and Gram-negative bacteria, incidence of vestibular side effects, tissue by mouth, ADULT and CHILD over 8
Lower respiratory tract infections: 400 chlamydiae, mycoplasmas, rickettsiae, coxiel- discoloration and skin pigmentation compared years, 200 mg on first day then 100
mg as a single loading dose on day lae, spirochetes and some mycobacteria. None to other tetracyclines. Caution is advised when mg daily; in severe infections, 200
1, followed by 200 mg once daily for is active against Pseudomonas aeruginosa, used for long-term management of acne. mg daily.
10 days. Proteus spp. or Providencia spp. Tetracycline absorption is reduced by approx. Syphilis, by mouth, 100 mg twice daily
Sinusitis: 400 mg loading dose Absorption of oral tetracyclines occurs largely 50% when taken with food. Its use may aggra- for 14 days; late latent syphilis 100 mg
followed by 200 mg once daily for 5 in the proximal small bowel, but may be dimin- vate existing renal insufficiency. Dehydration twice daily for 28 days.
days. ished by the simultaneous presence of food, and salt loss from diuretic therapy may worsen Uncomplicated genital chlamydia,
Sexually transmitted diseases: Gono- milk or cations, which form nonabsorbable nephrotoxicity. non-gonococcal urethritis, by mouth,
coccal urethritis – single dose of 200 tetracycline chelates. Cimetidine and presum- 100 mg twice daily for 7 days (14 days
mg; Non-gonococcal urethritis – 200 References:
ably other H2-receptor antagonists also impair in pelvic inflammatory disease).
mg loading dose followed by 100 mg 1) Chopra I. Tetracyclines. In: Finch RG,
absorption of tetracyclines by interfering with Louse and tick-borne relapsing fevers,
daily for 6 days. Greenwood D, Norrby SR, Whitley RJ,
their dissolution, which is pH dependent. Dox- by mouth, 100 mg or 200 mg as a
Note: Elimination of Sparfloxacin is prolonged in eds. Antibiotic and chemotherapy. 9th
ycycline and minocycline are better absorbed single dose.
patients with moderate to severe renal dysfunction. ed. Available from: www.clinicalkey.com
and may be administered with food. Cholera, by mouth, ADULT 300 mg as
In patients with creatinine clearance <30 mL/min, (login required)
a single dose; CHILD over 8 years, 100
urinary excretion and renal clearance is decreased A unique feature of tetracyclines is deposition mg as a single dose.
significantly. The dosage of Sparfloxacin should and persistence in areas where bone is being DOXYCYCLINE
Administration: Capsules should be swallowed
therefore be adjusted accordingly with moderate laid down. They should be avoided in young Indications: RTIs, including pneumonia and whole with plenty of fluid while sitting or standing
to severe renal dysfunction.
children and during late pregnancy. chronic bronchitis; UTIs; syphilis; chlamydia, to prevent oesophageal irritation. May be given with
Patients with severe renal insufficiency, should
receive a dosage of 200 mg every alternate day (or The most important adverse effect is gas- mycoplasma, and rickettsia; prostatitis; lym- milk or food to counter gastric irritation.
100 mg daily). trointestinal intolerance, reported for all phogranuloma venereum; PID (with met- POM Doxycycline (WMF 6.2.2)
Sparfloxacin pharmacokinetics are unchanged in tetracyclines. Nausea and vomiting may be ronidazole); Lyme disease; brucellosis (with Capsule or tablet, Doxycycline (as HCl) 100 mg
the elderly and in the presence of hepatic dysfunc- due to a direct irritant effect of the drug on rifampicin); leptospirosis, scrub typhus and
POM Doxycycline (EDL 5.3)
tion. Hence, elderly patients and those with hepatic the gastric mucosa, but diarrhea is probably travellers’ diarrhoea; psittacosis; cholera;
dysfunction do not require dosage adjustment. Capsule, Doxycycline (as hyclate) 100 mg.
the result of disturbance of the normal flora. melioidosis; plague; anthrax; Q fever; malaria
POM GLOSPARCYN® (Global Healthcare) (section 9.3.1). POM CYCLODOX® (Superior)
Antibiotic-associated enterocolitis caused
Tablet, Sparfloxacin 200 mg; f-c tab. Contra-indications: Pregnancy (Appendix 2); Capsule, Doxycycline hyclate 100 mg; dark green
by Clostridium difficile toxin. Superinfection coloured capsule.
200 mg – 1 x 10’s. with resistant organisms including Clostridium children (see notes above); porphyria; systemic
100 mg – 10 x 10’s
POM GSPAR® (Greenlife) difficile Candida, Proteus or Pseudomonas spp. lupus erythematosus.
Tablet, Sparfloxacin 200 mg; f-c tab. Staph. aureus enterocolitis. Precautions: Avoid exposure to sunlight or POM DOXAC® (Al-Tinez)
200 mg – 1 x10’s (in blister) sunlamps—photosensitivity reported; renal Capsule, Doxycycline (as hyclate) 100 mg
Drug interactions include complexes with impairment (Appendix 4); hepatic impairment 100 mg – 10 x 10’s (in blisters)
POM SLOXIN 200® (Pharmabase) divalent and trivalent cations together with (Appendix 5); breastfeeding (Appendix 3);
Tablet, Sparfloxacin 200 mg; f-c tab. POM DOXIN® (Geneith)
chelation by iron-containing preparations. interactions: Appendix 1. Capsule, Doxycycline 100 mg.
200 mg – 7’s. The anticonvulsants carbamazepine, pheny- Adverse effects: GI disturbances; anorexia, Pack: 10 x 10’s (in blister)
384 | 9.1.2.3 Tetracyclines 9.1.2.4 Macrolides | 385
POM DOXYCAP® (Hovid) Capsule, Minocycline HCl 200 mg; orange and purple • Monitor patient for signs of superinfection. POM Tetracycline (Emzor)
Capsule, Doxycycline (as HCl) 100 mg capsule marked ‘APO 100’. Dose: By mouth, 250 mg 4 times daily; Capsule, Tetracycline HCl 250 mg; yellow/red cap.
100 mg – 10 x 10 (blister). 200 mg – 100’s. increased to 250 mg 6-8 times daily in marked ‘EMZOR’.
severe infections. 250 mg – 1000
POM DOXYCILLIN® (Goben)
Tablet, Doxycycline HCl 100 mg; green f-c tab. TETRACYCLINE Not recommended for children <12 POM Tetracycline (Juhel)
100 mg – 100’s; 500’s; 1000’s. Synonym: TCN. years. Capsule, Tetracycline 250 mg.
Capsule, Doxycycline HCl 100 mg; dark green cap. Therapeutic category: Antibiotic Note: To be swallowed with adequate amount of 250 mg – 100’s; 1000’s.
marked ‘UPHA/DOX’. Pharmacology: Tetracyclines are broad-spec- fluid while sitting or standing to prevent gastric
POM Tetracycline (Nemel)
100 mg – 100’s; 500’s; 1000’s. trum antibiotics and are bacteriostatic. They irritation.
Capsule, Tetracycline HCI 250 mg; red/yellow cap.
POM Doxycyclin (Neros) exert bacteriostatic effect by binding to the POM Tetracyline (EDL 5.3)
POM Tetracycline (Rajrab)
Capsule, Doxycycline (as hyclate) 100 mg. 30S ribosomal subunit of microorganisms, thus Capsule or tablet, Tetracycline (as HCl) 250 mg
Capsule, Tetracycline 250 mg; capsule marked
100 mg – 10 x 10’s. inhibiting protein synthesis. They are deposited Injection, Tetracycline 100 mg, 250 mg; powder for
“TETRA 250”.
in growing bone and teeth (being bound to cal- injection in vials.
POM Doxycycline-100 (Embassy) 250 mg – 100’s.
Capsule, Doxycycline 100 mg. cium) causing staining and should not be given POM BETRA® (Bentos)
to children under 12 years or pregnant women. POM TETRAMAC® (Geneith)
Capsule, Tetracycline HCl 250 mg.
POM DOXYDAN® (Dana) Capsule, Tetracycline 250 mg.
Indications: Infections of the ear, nose and 250 mg – 10’s.
Capsule, Doxycycline 100 mg 250 mg – 10’s; 1000’s.
100 mg – 10 x 10’s (in blisters) throat, respiratory tract, GI tract, liver, geni- POM CIKACYCLINE® (Michelle Lab)
to-urinary tract; veneral diseases. POM TETRARICH® (Goldmoore)
Capsule, Tetracycline (as HCI) 250 mg.
POM DOXYTAB®(Hovid) Contra-indications: Hypersensitiviy to tetra- Capsule, Tetracycline.
250 mg – 10 x 10’s (in blisters); 1000’s (in jars)
Tablet, Doxycycline (as HCl) 100 mg; f-c tab. cyclines; pregnancy, children under 12 years; POM TETRIN® (Medreich)
100 mg – 250; 1000. POM LATETRA® (Mecure)
Kidney disease, systemic lupus erythematosus. Capsule, Tetracycline HCl BP 250 mg; maroon/
Capsule, Tetracycline HCl 250 mg; red/yellow capsule
EMDEX
POM EURODOX® (Beta Drugs) Precautions: Breast-feeding; overgrowth of marked ‘LATETRA’.
yellow cap.
Capsule, Doxycycline 100 mg. nonsusceptible organisms. Avoid use with 250 mg – 10’s (in blister); 1000’s (in HDPE jars)
250 mg – 10 x 10’s.
100 mg – 10 x 10’s (in blisters). penicillins.
Interactions: Milk products, calcium, mag- POM LETAN®-250 (Beta Drugs) 9.1.2.4 Macrolides
POM INTERDOXIN® (Reals)
Capsule, Tetracycline HCl 250 mg.
Capsule, Doxycycline (as hyclate) 100 mg. nesium, and iron salts, antacids containing Clarithromycin: It is more stable to gastric acid
250 mg – 10 x 10’s; 1000’s.
100 mg – 1 x 10’s; 5 x 10’s (in blisters). aluminium hydroxide or silicate, should not be than erythromycin; It is rapidly absorbed orally
given for at least 30 mins following admin. of POM LIFLIN® (Jubilee) and absorption is not affected by food. Activity
POM OXYDOX® (Neimeth)
tetracycline due to the decrease in antibiotic Capsule, Tetracycline (as HCl) 250 mg.
Capsule, Doxycycline 100 mg against susceptible common pathogens is two
100 mg – 6’s; 60’s absorption. Oral contraceptives (decrease POM MAXCYCLIN® (Richygold) to four times greater than that of erythromycin
contraceptive effectiveness and increased risk Capsule, Tetracycline (as HCl) 250 mg. A. Clarithromycin is well tolerated, producing
POM PEXIN® (Pemason)
of breakthrough bleeding). Pack: 10 x 10’s; 1000’s. little gastrointestinal disturbance and only
Capsule, Doxycycline 100 mg
Adverse effects: GI disturbances; overgrowth POM MEDICYCLINE® (Embassy) transient changes in some liver function tests.
POM TENUTAN®(Sanofi) of resistant organisms; photosensitivity and Capsule, Tetracycline 250 mg. Erythromycin: The acid lability of erythromy-
Capsule, Doxycycline HCl 100 mg
dermatological reactions. 250 mg – 100’s; 1000’s.
100 mg – 8; 100; 500. cin base necessitates administration in a form
Advice to patients: Take 1 hour before or 2
POM TETRADOX® (Ranbaxy)
POM NACYCLINE®(NASDMU) giving protection from gastric acid. Delayed
hours after meals with adequate amounts of Capsule, Tetracycline HCl 250 mg; yellow/red cap.
Capsule, Doxycycline (as HCl) 100 mg. and incomplete absorption is obtained from
fluid, capsules or tablets should be swallowed marked ‘NACY 250 mg’.
100 mg – 10 x 10’s; 500’s. coated tablets and there is important inter –
whole while sitting or standing; avoid taking Pack: 1000.
Tablet, Doxycycline (as Hyclate) 100 mg and intra-individual variation, adequate levels
antacids, iron, or dairy products within 2
100 mg – 10’s; 500’s. POM SALMYCIN 250® (Strides Vital) not being attained at all in a few subjects. Food
hours of taking tetracyclines; report persistent Capsule, Tetracycline 250 mg.
POM UNIDOXY® (Vixa) delays absorption of erythromycin base.
nausea, vomiting, yellow colouring of skin or 250 mg – 10 x 10’s.
Capsule, Doxycycline 100 mg. Interaction with the hepatic metabolism of
eyes, dark urine, or pale stools; avoid prolonged
100 mg – 10 x 10’s. POM SIVOCYCLINE® (Adpharm) other drugs can result in clinically significant
exposure to sunlight and UV light. Take until
Tablet, Tetracycline 250 mg potentiation of the action of carbamazepine,
POM VETROCAP® (Crystal) gone; do not skip doses.
250 mg – 10 x 10’s; 1 x 1000’s. ciclosporin (cyclosporine), methylpredniso-
Capsule, Doxycyline 100 mg. Nursing action: Obtain specimens for C&S
100 mg – 10 x 10’s. POM TERAFEN® (Vixa) lone, theophylline, midazolam, terfenadine
tests prior to the first dose; administer around-
Capsule, Tetracycline 250 mg. and warfarin, and in adverse responses to
POM VIBRAMYCIN® (Pfizer) the-clock in equal intervals to promote less
Pack: 10 x 10’s. digoxin and ergot alkaloids.
Capsule, Doxycycline (as HCl) 100 mg; green cap. variation in peak and trough serum levels.
• Administer on an empty stomach with a full glass
Oral administration, especially of large doses,
marked ‘PFIZER’ and ‘VBM100’. POM TETRA-250® (Ranbaxy)
100 mg – 6; 50. of water; separate iron products, antacid, dairy commonly causes epigastric distress, nausea
Capsule, Tetracycline HCl 250 mg
products or kaolin/pectin by at least 2 hr. 250 mg – 10 x 10; 10 x 100; 100 and vomiting, which may be severe. Solutions
POM ZILLINE® (Chanmedi) • Give at least an hour before bedtime to prevent are very irritant: intravenous infusions almost
Capsule, Doxycycline 100 mg. oesophagitis. POM TETRACAP® (Fil Pharma) invariably produce thrombophlebitis.
100 mg – 1 x 500’s. • Anti-emetic may be given if nausea or vomiting Capsule, Tetracycline HCl BP 250 mg
Transient auditory disturbances have been de-
persists. 250 mg – 10 x 10 (in blister)
scribed after intravenous administration of the
MINOCYCLINE • Explain to the patient that effectiveness of the drug POM Tetracycline (Embassy) lactobionate salt, and occasionally in patients
is reduced when taken with milk or other dairy Capsule, Tetracycline 250 mg.
POM Apo-Minocycline (Lahams) with renal and hepatic impairment in whom
products, food, antacids or iron products. 250 mg – 1000’s.
386 | 9.1.2.4 Macrolides 9.1.2.4 Macrolides | 387
oral dosage has produced high plasma levels. dizziness, headache, drowsiness, agitation, Pack: 30 mL. Pack: 60 mL
The estolate is particularly prone to give rise anxiety, hyperactivity; photosensitivity; hep- POM Azithromycin (Crystal) POM GLOTHROX® (Global Healthcare)
to liver abnormalities, consisting of upper atitis, interstitial nephritis, acute renal failure, Capsule, Azithromycin 250 mg Capsule, Azithromycin (as dihydrate) 250 mg.
abdominal pain, fever, hepatic enlargement, asthenia, paraesthesia, arthralgia, convulsions, 250 mg – 6’s 250 mg – 1 x 6’s.
a raised serum bilirubin, pale stools and dark mild neutropenia, thrombocytopenia, tinnitus, Oral suspension, Azithromycin dihydrate 200 mg Dry syrup, Azithromycin (as dihydrate) 200 mg
hepatic necrosis, hepatic failure, tongue discol- per 5 mL per 5 mL.
urine and eosinophilia. The condition is rare
oration, and taste disturbances. Pack: 15 mL.
and usually seen 10–20 days after the initia- POM Azithromycin (Emzor)
tion of treatment, with complete recovery on Advice to patients: Not to be taken at the Suspension, Azithromycin (as dihydrate) 200 mg. POM GREMAX® (Greenlife)
stopping the drug. Recurrence of symptoms same time as aluminium– or magnesium-con- 200 mg – 15 mL Caplet, Azithromycin (as dihydrate) 250 mg.
can be induced by giving the estolate but not taining indigestion remedies. Capsules should 250 mg – 1 x 10’s; 2 x 10’s.
POM Azithromycin (Onifam)
be taken at least 1 hour before or 2 hours after Suspension, (600 mg), Azithromycin (as dihydrate)
the base or stearate. Tablet, Azithromycin (as dihydrate) 500 mg
food; oral suspension can be taken with food. 200 mg per 5 mL.
Roxithromycin: A semisynthetic derivative 500 mg – 1 x 3’s
Pack: 15 mL bottle.
of erythromycin A formulated for oral use. Dose: Uncomplicated genital chlamydial infec-
tions or trachoma, by mouth, ADULT POM Azithromycin (Zolon)
Activity against common pathogens is com- POM JAWAZITHRO® (Jawa)
Tablet, Azithromycin (as dihydrate) 250 mg, 500
parable to that of erythromycin. Absorption is over 45 kg, 1 g as a single dose; under Capsules, Azithromycin 250 mg, 500 mg.
mg; f-c tab.
45 kg, 20 mg/kg as a single dose. 250 mg – 2 x 3’s.
not affected by food. Oral administration with 500 mg – 1 x 3’s.
POM AZITREX® (Tamar & Pharez)
antacids or H2-receptor antagonists does not POM Azithromycin (WMF 6.2.2) Tablet, Azithromycin 500 mg
significantly affect bioavailability. Capsules, Azithromycin 250 mg, 500 mg POM JUTROMAX® (Juhel)
500 mg – 3’s
Adverse effects include mostly GI disturbance Oral liquid, Azithromycin 200 mg/5 mL. Capsule, Azithromycin (as dihydrate) 250 mg;
Suspension, Azithromycin 200 mg per 5 mL
white cap.
(abdominal pain, nausea and diarrhea). Head- POM Azithromycin (EDL 5.3/Restricted List) Pack: 15 mL
ache, weakness, dizziness, rash and reversible 250 mg – 6's; 24's.
Capsule, Azithromycin 250 mg.
EMDEX
POM AZOD® (Micronova) Suspension, Azithromycin 200 mg per 5 mL.
changes in liver function tests and increased Tablet, Azithromycin 250 mg, 500 mg; f-c tab
POM AZET® (Reals) POM MIRAZITH® (Miraflash)
eosinophils and platelets have also been Capsule, Azithromycin (as dihydrate) 250 mg.
described. POM AZODAY® (Pharma Ethics) Capsule, Azithromycin 250 mg
250 mg – 1 x 6’s. Caplet, Azithromycin 500 mg. 250 mg – 2 x 7’s
Azithromycin: A semi-synthetic derivative of POM AZGLO® (Global Organics) 500 mg – 1 x 3’s (in blister) Suspension, Azithromycin 200 mg per 5 mL
erythromycin A, supplied as the dihydrate for Tablet, Azithromycin (as dihydrate) 500 mg; f-c tab Pack: 15 mL; 50 mL
POM BUTROMAX® (JB Pharma)
oral administration. It is less potent than eryth- 500 mg – 3’s Capsules, Azithromycin (as dihydrate) 250 mg, POM RAZITRO® (Seagreen)
romycin A against Gram-positive isolates, but 500 mg Capsule, Azithromycin 250 mg
POM AZIAGIO® (Phillips)
is more active against Gram-negative bacteria. 250 mg – 1 x 6’s. 250 mg – 6’s
Tablets, Azithromycin 250 mg, 500 mg, 1000 mg;
It is four times more potent than erythromy- f–c tabs 500 mg – 1 x 6’s.
cin A against H. influenzae, N. gonorrhoeae POM ROXIMAX® (Solidum)
250 mg – 1 x 6’s (in blisters) Suspension, Azithromycin (as dihydrate) 200 mg per
Tablets, Azithromycin dihydrate 250 mg, 500 mg;
and Campylobacter spp., and twice as active 500 mg – 1 x 3’s (in blisters) 5mL; dry powder for reconstitution.
f-c tabs.
against Mor. catarrhalis. It also exhibits superior 500 mg – 1 x 1’s (in blisters) Pack: 30 mL.
250 mg – 7’s
potency against Enterobacteriaceae, notably Dose: Upper & lower respiratory tract infections, Adult,
POM AZIFAST® (Crowther) 500 mg – 4’s
Esch. coli, Salmonella enterica serotypes, and by mouth, 500 mg once daily for 3 days or
Tablet, Azithromycin 250 mg; f-c tab. Suspension, Azithromycin 200 mg per 5 mL.
500 mg once on day 1, followed by 250 once
Shigella spp. Azithromycin is well tolerated 250 mg – 10 x 6’s 200 mg – 5ml
daily for next 4 days.
with little gastrointestinal disturbance. Dry syrup, Azithromycin 200 mg per 5 mL. Child: 10 mg/kg once daily for 3 days. Acne, POM SUITROX® (Taylek)
References: Pack: 10 x 1’s 500 mg once daily for 3 days, then 4 days Tablets, Azithromycin 250 mg, 500 mg; f-c tabs
1) Bryskier A. Macrolides. In: Finch RG, POM AZILIDE® (Geneith) interval; continue for a total of 12 weeks. 250 mg – 4’s; 6’s; 12’s; 24’s; 50’s; 100’s (in blisters)
Greenwood D, Norrby SR, Whitley RJ, Tablets, Azithromycin 250 mg, 500 mg. Skin/skin structure infection, Adult, 500 mg 500 mg – 2’s; 3’s; 6’s; 12’s; 24’s; 30’s; 50’s;100’s (in
250 mg – 1 x 6’s once daily for 3 days. blisters)
eds. Antibiotic and chemotherapy. 9th
500 mg – 1 x 3’s Child: 10 mg/kg once daily for 3 days. Geni- Injection, Azithromycin 100 mg, 200 mg per 5 mL;
ed. Available from: www.clinicalkey.com tal ulcer disease (chancroid), Non-gonococcal
Suspension, (300 mg), Azithromycin 100 mg per 5 mL powder for oral suspension.
(login required) urethritis and cervicitis, Adult, 1 g as single 100 mg – 20 mL
Pack: 15 mL
Suspension (1200 mg), Azithromycin 200 mg per 5 mL dose. Gonococcal urethritis and cervicitis, 200 mg – 15 mL; 20 mL; 22.5 mL; 30 mL; 37.5 mL
AZITHROMYCIN Pack: 30 mL Adult, 2 g as single dose. Typhoid/paraty-
phoid, Adult, 1 g once daily for 5 days. POM VATROMAX® (Vixa)
Indications: Uncomplicated genital chlamydial
POM AZIPHAR® (Neros) Child: 20 mg/kg once daily for 5 days. Capsules, Azithromycin 250 mg, 500 mg
infections and trachoma. 250 mg – 1 x 10’s
Caplets, Azithromycin (as dihydrate) 250 mg, 500 Diarrhea, Cholera, Shigellosis, Adult: 1-1.5 g
Contra-indications: Hepatic impairment mg; f-c caplets. 500 mg – 1 x 10’s
as single dose.
(Appendix 5). 250 mg – 1 x 6’s (in blister) Child: 20 mg/kg single dose. Dental infec- POM WATAZET® (Watson)
Precautions: Pregnancy (Appendix 2) and 500 mg – 1 x 3’s (in blister). tion, Adult, 500 mg once daily for 3 days. Caplet, Azithromycin 250 mg; pink tab.
breastfeeding (Appendix 3); prolongation of Child: 10 mg/kg once daily for 3 days. Eye in-
POM AZITH® (Zoomota) POM XITH® (Pacmai)
QT interval (ventricular tachycardia reported); fection (trachoma), Adult, 1 g as single dose.
Tablets, Azithromycin (as dihydrate) 250 mg, 500 Tablet, Azithromycin (as dihydrate) 250 mg; f-c tab.
interactions: Appendix 1. mg; f-c yellow tabs. Child: 20 mg/kg single dose.
Adverse effects: See under Erythromycin (but 250 mg – 1 x 6’s (in blisters)
250 mg – 6’s POM CIDALIX® (Tamar & Pharez)
fewer GI effects); also anorexia, dyspepsia, 500 mg – 3’s Tablets, Azithromycin 250 mg, 500 mg POM ZITHROMAX® (Pfizer)
flatulence, constipation, pancreatitis; syncope, Suspension, Azithromycin (as dihydrate) 200 mg Oral suspension, Azithromycin 200 mg per 5 mL. Caplet, Azithromycin (as dihydrate) 250 mg; white
per 5 mL; pre-constituted susp. in flavoured base. cap. marked ‘PFIZER’ and Azithromycin ‘250 mg’.
250 mg – 4’s; 6’s; 24’s. cin is widely distributed throughout the body, POM CEEMACIN® (Pinnacle) 250 mg – 1 x 14’s
Suspension, (600 mg), Azithromycin (as dihydrate) generally achieving higher concentrations in Tablet, Clarithromycin 500 mg; f-c tab. 500 mg – 2 x 5’s (in blisters)
200 mg per 5 mL; powder for reconstitution with a tissues and organs (including the lung and 500 mg – 2 x 7’s (in blisters)
POM KLABAX® (Ranbaxy)
cherry/banana flavour. tonsils) than in blood. It is excreted principally POM CLAR® (Zolon) Tablets, Clarithromycin 250 mg, 500 mg; f-c tabs.
Pack: 15 mL.
by the liver and kidneys. Tablet, Clarithromycin 250 mg, 500 mg; f-c tab 250 mg – 25 x 4’s
POM ZITHROLIDE® (Nosak) Indications: Upper respiratory tract infections 250 mg – 1 x 10’s 500 mg – 10 x 10’s.
Tablets, Azithromycin (as dihydrate) 250 mg, 500 – sinusitis and pharyngitis; Lower respiratory 500 mg – 1 x 10’s Suspension (125 mg), Clarithromycin 125 mg per 5 mL
mg; f-c tabs. tract infections – pneumonia, acute and Pack: 100 mL.
POM CLARET® (Global Healthcare)
Suspension, Azithromycin (as dihydrate) 200 mg per Suspension (250 mg), Clarithromycin 250 mg per 5 mL
chronic bronchitis; Disseminated mycobac- Tablet, Clarithromycin 500 mg; f-c tab.
5 mL; in flavoured syrupy base. Pack: 100 mL.
terial infections due to Mycobacterium avium 500 mg – 2 x 7’s (in blisters).
POM Zmax® (Pfizer) or Mycobacterium intracellulare; Skin and skin POM KLARIMAX® (Lintak)
POM CLARICIN® (Lifeback)
Suspension, Azithromycin (as dihydrate) 2 g; ex- structure infections. Tablet, Clarithromycin 500 mg
Tablet, Clarithromycin 500 mg; f-c tab.
tended release powder for oral suspension. Contra-indications: Hypersensitivity to clar- 500 mg – 2 x 7’s (in blisters)
Pack: 2 g (60 mL) x 1’s. Suspension, Clarithromycin 250 mg per 5 mL; dry
ithromycin; pregnancy.
Description: Zmax is an extended release micro- POM CLARIDEX® (Salem Gates) powder for reconstitution.
sphere formulation. It provides a full course of Precautions: Hepatic and renal impairment; Pack: 50 mL.
Tablet, Clarithromycin 500 mg; f-c tab
antibacterial therapy in a single dose. Each bottle Superinfection; history of hypersensitivity to 500 mg – 2 x 7’s; 1 x 10’s (in blisters)
other macrolides; lactation; children. POM KLATRIL® (Reals)
contains 2 g of azithromycin to be reconstituted Dry syrup, Clarithromycin 125 mg per 5 mL.
Interactions: CYP3A4 substrates (avoid Tablet, Clarithromycin 500 mg.
with 60 mL of water and the entire contents are Pack:100 mL
administered orally as a single dose. co-administration with statins e.g. Atorvasta- POM MACLAR® 500 (Glenmark)
Indications: Acute bacterial sinusitis due to Haemo- POM CLARIDOSE® (Crystal)
tin, Lovastatin & Simvastatin); Theophylline; Tablet, Clarithromycin 500 mg; f-c tab.
philus influenzae, Moraxella catarrhalis or Streptococ- Caplet, Clarithromycin 500 mg; orange-coloured
Warfarin; Digoxin; Zidovudine; Terfenadine; 500 mg – 3 x 4's
caplet.
EMDEX
cus pneumoniae. Community-acquired pneumonia Pimozide; Astemizole.
due to Chlamidophyla pneumoniae, Haemophilus 500 mg – 2 x 7’s (in aluminium foil). POM NOVIBAXIN® (Nomedi)
Adverse effects: Nausea, vomiting, diarrhoea, Tablet, Clarithromycin 250 mg, 500 mg
influenzae, Mycoplasma pneumoniae or Streptococcus POM CLARIGEN® (Geneith)
pneumoniae, in patients appropriate for oral therapy. abdominal pain and stomatitis and headache; 250 mg – 1 x 10’s (in blisters)
Tablet, Clarithromycin 250 mg.
Advice to patients: Use within 12 hours of reconsti- rarely, allergic reactions e.g. urticaria, mild 500 mg – 1 x 10’s (in blisters)
250 mg – 1 x 10’s
tution. Shake bottle well before use. Take the entire skin eruptions, anaphylaxis, Stevens-Johnson POM THROMYC® (Pharmabase)
contents of the bottle on an empty stomach (at least Syndrome and thrombocytopenia; taste per- POM CLARIMAC® (Pacmai)
Tablet, Clarithromycin 500 mg; f-c tab
1 hour before or 2 hours after food). Report to your version; transient CNS side-effects including Tablet, Clarithromycin 500 mg; f-c tabs.
physician if vomiting occurs within the first hour of 500 mg – 1 x 10’s (in blisters)
anxiety, dizziness, insomnia, hallucinations
taking the medication. and confusion; pseudomembranous colitis; POM CLARIX® (Vinco) ERYTHROMYCIN
Dose: By mouth, Adult, 2 g as a single dose. Tablets, Clarithromycin 250 mg, 500 mg.
hepatic dysfunction. Indications: Alternative to penicillin in hyper-
To be taken on an empty stomach (at least 250 mg – 10 x 2 x 10’s.
1 hour before or 2 hours following a meal)
Nursing action: Obtain specimen for C&S test sensitive patients; sinusitis; otitis externa; oral
500 mg – 10 x 1 x 10’s.
within 12 hours of reconstitution. before first dose; therapy may begin pending infections; cholera; respiratory tract infections
Children: Not recommended. test results. POM CLARITHRAMAX® (Vixa) (including pneumonia, legionnaires’ disease);
• Administer 12 hrly with a full glass of water; may Tablet, Clarithromycin 500 mg syphilis; chancroid; chlamydia; neonatal
POM ZYCIN® (Interpharma) give with food to reduce GI upset. 500 mg – 1 x 10’s.
Caplet, Azithromycin 250 mg. chlamydial conjunctivitis; non-gonococcal
• Advise patients on Atorvastatin, Lovastatin or
250 mg – 6’s POM Clarithromycin (Biostadt) urethritis; prostatitis; lymphogranuloma ve-
Simvastatin to withhold such statins for the du-
Tablet, Clarithromycin 500 mg nereum; campylobacter enteritis; relapsing
ration of the antibiotic therapy. Monitor patient
CLARITHROMYCIN Pack: 1 x10’s (in blisters) fever; skin infections; diphtheria; diphtheria
on Amlodipine for increased hypotensive effect
Oral suspension, Clarithromycin 125 mg per 5 mL and whooping cough prophylaxis; Q fever in
Therapeutic category: Macrolide antibiotic. • Prolonged use may result in overgrowth of nonsus-
Pack: 60 mL
Pharmacology: Clarithromycin is a semi-syn- ceptible organisms; monitor patient for symptoms children.
thetic derivative of erythromycin A. It exerts
such as fever, sore throat, fatigue. POM Clarithromycin (Kayhelt) Contra-indications: Hypersensitivity to eryth-
Dose: Adults and children over 12 years: Usu- Tablet, Clarithromycin 500 mg; f-c tab romycin or other macrolides; porphyria.
its antibacterial action by binding to the 50S
ally 250 mg twice daily for 7 days. 500 mg – 10’s (in blisters) Precautions: Hepatic impairment (Appendix
ribosomal sub-unit of susceptible bacteria
In severe infections, 500 mg twice POM CLARIWIN® (Strides Vital) 5) and renal impairment (Appendix 4); predis-
and suppresses protein synthesis. It is active
daily for up to 14 days. Tablet, Clarithromycin 500 mg. position to QT interval prolongation (including
against a wide variety of aerobic and anaerobic
Children 6 months – 12 years: 7.5 mg 500 mg – 1 x 10’s. electrolyte disturbances and concomitant use
gram-positive and gram-negative organisms.
per kg of b.wt every 12 hours. of drugs that prolong the QT interval); preg-
The MICs of clarithromycin are generally two- POM FASCAR® (Mark)
Note: Renal Impairment: Dosage adjustments are nancy (not known to be harmful); breastfeed-
fold lower than the MICs of erythromycin. Tablet, Clarithromycin 500 mg.
required in patients with severe renal impairment. ing (Appendix 3); interactions: Appendix 1.
Clarithromycin is well absorbed from the GIT. 500 mg – 10’s
Creatinine clearance <30 mL/min: 250 mg once Adverse effects: Nausea, vomiting, abdominal
It undergoes substantial first pass metabolism daily for mild to moderately severe infections POM JOCLAR® (Joswe/Afrab)
and its systemic bioavailability is about 55% Caplet, (250 mg), Clarithromycin 250 mg; f-c caplet. discomfort, diarrhoea (and antibiotic-associ-
and 250 mg twice daily in more severe in- ated colitis); less frequently urticaria, rashes,
after a 250 mg dose. Clarithromycin undergoes fections.
Pack: 14’s in HDPE jar.
rapid biotransformation to produce the micro- Caplet, (500 mg), Clarithromycin 500 mg; f-c caplet. and other allergic reactions (rarely, anaphy-
biologically active 14 hydroxy (R) metabolite, POM ACEM-500® (Fil Pharma) Pack: 14’s; 20’s in HDPE jar. laxis); reversible hearing loss after large doses;
which achieves peak plasma concentration Tablet, Clarithromycin 500 mg; f-c tab. cholestatic jaundice, infantile hypertrophic
POM KALECIN® (Neros)
500 mg – 10’s (in blister). pyloric stenosis, cardiac effects (including chest
within 3 hours of administration. Clarithromy- Caplets, Clarithromycin 250 mg, 500 mg; f-c tabs.
pain and arrhythmias), myasthenia-like syn- Injection, Erythromycin (as lactobionate) 500 mg; 250 mg per 5 mL; dry powder for reconstitution. 500 mg – 10’s
drome, erythema multiforme (Stevens-John- powder for injection in vial. 125 mg/5 mL – 100 mL
POM ETOCIN® (Interpharma)
son syndrome) and toxic epidermal necrolysis. 250 mg/5 mL – 100 mL.
POM APO-ERYTHRO® (Lahams) Tablets, Erythromycin (as stearate) 500 mg.
Advice to patients: Take until gone, do not Tablets, Erythromycin base 250 mg, oval pink, f-c POM ERYTHRO-TEVA® (Dizpharm) 500 mg – 10 x 10’s.
skip doses; report to physician if persistent di- tab. marked ‘APO 250’; 500 mg, white oval, f-c tab. Tablets, Erythromycin (as stearate) 250 mg, 500 mg. Syrup, Erythromycin (as ethylsuccinate) 200 mg per
arrhoea occurs; drug absorption is unaffected marked ‘APO 500’. 250 mg – 10. 5 mL; dry powder for syrup.
by food. Gastro-resistant tablets and capsules 250 mg – 100 500 mg – 10. Pack: 100 mL.
should be swallowed whole. 500 mg – 100. Suspension, Erythromycin (as ethylsuccinate) 125
POM FABTHROCIN® (FAB)
mg, 200 mg, 400 mg per 5 mL.
Nursing action: Administer around-the-clock POM BARBIMYCIN® (Juhel) Syrup, Erythromycin 250 mg 5 mL.
Pack: 60 mL.
in equal intervals to promote less variation in Suspension, Erythromycin (as ethylsuccinate) 125 mg Pack: 100 mL
peak and trough serum levels. per 5 mL; dry powder for reconstitution. POM ERYTHRO® Kid (Fidson)
POM LABCIN-500® (Embassy)
• Do not crush enteric coated drug product; GI Pack: 60 mL. Dry Syrup, Erythromycin (as ethylsuccinate) 250
Capsule, Erythromycin 500 mg.
upset, including diarrhoea, is common; can give mg per 5 mL; strawberry flavoured dry powder for
POM EDITROMYCIN® (Nalis) 500 mg – 10 x 10’s.
with food to decrease GI upset; give with a full reconstitution
Tablet, Erythromycin stearate equiv. to erythromycin
glass of water, encourage adequate fluid intake if Pack: 100 mL bottle. POM MD-Erythromycin (O’Nell)
500 mg; f-c tab
diarrhoea occurs; advise patient not to take fruit Suspension, Erythromycin (as ethylsuccinate) 125 mg
POM Erythomycin (Ceenek)
juice with medication. POM ERIXYN®(Vinco) per 5 mL; dry powder for reconstitution.
Dry syrup, Erythromycin (as ethylsuccinate) 125 mg
• Give IV infusion over 60 minutes; it may be very Tablets, Erythromycin stearate 250 mg, 500 mg. Pack: 100 mL
per 5 mL; pinkish granules for reconstitution
irritating to the vein; if phlebitis/pain occur with 250 mg – 10 x 1 x 10’s.
Pack: 60 mL; 100 mL POM Moko Erythromycin® (New Healthway)
used dilution, consider diluting further (e.g, 1:5), if 500 mg – 10 x 1 x 10’s.
Suspension, Erythromycin 125 mg per 5 mL; dry
fluid status of the patient will tolerate, or consider POM Erythromycin (Kayhelt)
POM ERITHRIN® (Biostadt) powder for oral suspension.
administering in larger available vein. Tablet, Erythromycin (as stearate) 500 mg; f-c tab.
Tablets, Erythromycin (as stearate) 250 mg, 500 Pack: 100 mL.
EMDEX
• Avoid IM inj or IV push. 500 mg – 10’s (in blisters)
mg; f-c tabs
• Monitor for symptoms of superinfection namely POM PAMETA® (Jopan)
250 mg – 10 x 10’s POM Erythromycin-500 (Neros)
fever, sore throat, fatigue. Caplet, Erythromycin (as stearate) 500 mg; f-c cap.
500 mg – 10 x 10’s Caplet, Erythromyicn (as stearate) 500 mg; f-c caplet.
• Instruct patient to report complaints such as nau- 500 mg – 1 x 10’s
Suspension, Erythromycin ethylsuccinate 200 mg 500 mg – 1 x 10’s; 10 x 10’s (in blisters).
sea, abdominal pain, and fever.
per 5 mL POM RYCIN® (Medreich)
Dose: Infections due to sensitive organisms, POM Erythromycin (Evans)
Pack: 60 ml. Tablets, Erythromycin (as stearate) 250 mg, 500 mg;
by mouth, ADULT and CHILD over Tablets, Erythromycin (as stearate) 250 mg, 500
white f-c tabs marked ‘RYCIN’.
8 years, 250–500 mg every 6 hours; POM EROGRAN® (Hovid) mg; f-c tabs.
Granule, Erythromycin ethylsuccinate 200 mg 250 mg – 10’s (in blisters) POM RYPED® (Medreich)
up to 4 g daily in severe infections;
Pack: 100 mL. 500 mg – 10’s (in blisters) Suspension, Erythromycin (as ethylsuccinate) 125
CHILD up to 2 years, 125 mg every 6
mg, 250 mg per 5 mL; dry powder for reconstitution.
hours, doubled in severe infections; POM EROMYCIN® (Fidson) POM Erythromycin (Nichben)
125 mg/5 mL – 100 mL
CHILD 2–8 years, 250 mg every 6 Tablets, Erythromycin (as ethylsuccinate) 250 mg, Tablets, Erythromycin (as stearate) 250 mg, 500 mg.
250 mg/5 mL – 100 mL.
hours, doubled in severe infections. 500 mg. Oral suspension, Erythromycin (as ethylsuccinate)
250 mg – 30’s. 125 mg per 5 mL; powder for reconstitution. POM RYTHROGEN® (Geneith)
Early syphilis, by mouth, ADULT 500
500 mg – 30’s. Pack: 60 mL; 100 mL. Tablet, Erythromycin 500 mg.
mg 4 times daily for 14 days; late la-
tent syhphilis, ADULT 500 mg 4 times POM EROTAB® (Hovid) POM Erythromycin (Pemason) POM STRICIN® (Strides Vital)
daily for 30 days. Tablets, Erythromycin (as stearate) 250 mg, 500 mg; Tablet, Erythromycin stearate 500 mg Tablets, Erythromycin stearate 250 mg, 500 mg.
Uncomplicated genital chlamydia, both f-c tabs. 500 mg – 10 x 10’s Pack: 10 x 10’s.
250 mg – 10 x 10 (blister).
non-gonococcal urethritis, chancroid, POM Erythromycin (Pharmabox) POM THROTAL® (Mopson)
500 mg – 10 x 10 (blister).
by mouth, ADULT 500 mg 4 times Tablet, Erythromycin (as stearate) 500 mg; f-c tab. Capsule, Erythromycin estolate 250 mg
daily for 7 days (14 days in lym- POM ERYCIN® (Ranbaxy) 250 mg – 10 x 10’s
POM Erythromycin (Vatican Bells)
phogranuloma venereum). Suspension, Erythromycin (as ethylsuccinate) 125 Caplet, Erythromycin estolate 500 mg
Tablet, Erythromycin estolate 250 mg; uncoated tab.
mg per 5 mL. 500 mg – 10 x 10’s
Severe infections, by IV infusion, Oral suspension, Erythromycin estolate 125 mg
Pack: 60 mL. Powder for oral suspension, Erythromycin estolate
ADULT and CHILD 50 mg/kg daily per 5 mL
125 mg per 5 mL
by continuous infusion or in divided POM ERYLID® (Nosak)
POM Erythromycin (United African Lab) Pack: 100 mL
doses every 6 hours. Tablet, Erythromycin (as stearate) 500 mg; f-c tab
Tablet, Erythromycin 500 mg.
Suspension, Erythromycin (as ethylsuccinate) 200 POM ZERITAB® (Chanmedi)
POM Erythromycin (WMF 6.2.2) 500 mg – 10’s.
mg per 5 mL Tablets, Erythromycin stearate 250 mg, 500 mg.
Capsule or tablet, Erythromycin (as stearate or ethyl Suspension, Erythromycin 125 mg per 5 mL.
250 mg – 10 x 10’s.
succinate) 250 mg. POM ERYMYCIN® (Global Organics) Pack: 60 mL.
500 mg – 10 x 10’s.
Powder for oral liquid, Erythromycin (as stearate or Tablet, Erythromycin stearate equiv. to Erythromycin
POM ERYTHROMYCIN ES® (Dortemag)
ethyl succinate) 125 mg/5 mL. 500 mg; f-c tab. POM ZINEZINE® (Elbe)
Tablet, Erythromycin ethylsuccinate 400 mg; orange
Powder for injection, Erythromycin (as lactobionate) 500 mg – 10 x 10’s; 1 x 10’s Tablet, Erythromycin stearate.
colour, 18.8 mm elongated tab.
500 mg; in vial. Pack: 1 x 10 x 10’s.
POM ERYTHR-500® (Vixa) 400 mg – 10 x 10’s (in blisters)
POM Erythromycin (EDL 5.3) Tablet, Erythromycin 500 mg
POM ERYTHRONEZ® (Al-Tinez) ROXITHROMYCIN
Capsules or tablets, Erythromycin (as stearate or 500 mg – 1 x 10’s
Tablets, Erythromycin stearate 250 mg, 500 mg;
ethylsuccinate) 250 mg, 500 mg; enteric/film-coated. POM ERYTHREAL® (Reals) f-c tabs. Description: Roxithromycin, derived from
Oral liquid, Erythromycin (as stearate or ethylsucc-in- Dry Syrup, Erythromycin (as ethylsuccinate) 125 mg, 250 mg – 10’s erythromycin, is a semi-synthetic macrolide
ate) 125 mg per 5 mL.
392 | 9.1.2.5 Aminoglycosides 9.1.2.5 Aminoglycosides | 393
antibiotic. It is used to treat respiratory tract, for systemic infections. Excretion is mainly by Neomycin is the most likely of all the aminogly- • Increase fluid intake (to minimize irritation of the
urinary and soft tissue infections. the kidney and accumulation occurs in renal cosides to damage the kidneys and the audi- renal tubules) unless contraindicated.
impairment. tory branch of the eighth nerve. This has almost • Provide supervised ambulation, other safety meas-
(Source: http://en.wikipedia.org/wiki/Roxithromycin)
Use of gentamicin should be restricted to entirely restricted it to topical and oral use. ures for patients with nausea, vomiting, dizziness,
headache (vestibular dysfunction).
POM ROXATHRO® (Vixa) trained health personnel and care must be Streptomycin is used mainly in the treatment • Monitor renal function namely output, specific
Capsule, Roxithromycin 500 mg taken to ensure correct dosage and duration of tuberculosis. The most common serious toxic gravity, urinarysis, BUN and creatinine levels;
500 mg – 1 x 10’s of treatment are not exceeded, because most effect is vestibular disturbance, which is related report any signs of decreasing renal function to
adverse effects are dose related. The most to total dosage and excessive blood concen- the physician.
SPIRAMYCIN important adverse effects are ototoxicity and • Observe for superinfection, i.e., prolonged fever
trations, and hence to the age of the patient
Therapeutic category: Macrolide antibiotic nephrotoxicity and they are most common and the state of renal function. Depression of and other signs of infection especially of the upper
Pharmacology: Spiramycin is a first generation in the elderly and in patients with renal im- vestibular function by streptomycin has been
respiratory tract.
macrolide antibiotic produced by Streptomyces pairment. These groups and, if possible, all • Hearing should be tested before, during, and after
used in the treatment of patients suffering from treatment in patient at risk for ototoxicity; notify
ambofaciens and contains a 16-membered patients should be monitored for ototoxicity Ménière’s disease. doctor if patient complains of tinnitus, vertigo or
lactone ring. Erythromycin and roxithro- by audiometry. If there is impairment of renal
References: hearing loss.
mycin are 14-membered-ring macrolides function the dose interval must be increased; in • Bicarbonate may be ordered together with
whereas azithromycin, an azalide, is the only severe renal impairment, the dose should also 1) Loverin AM, Reeves DS. Aminoglyco-
gentamicin when treating UTI to alkalinize urine;
15-membered-ring macrolide in clinical use. be reduced. Serum concentration monitoring sides and aminocyclitols. In: Finch RG,
alkaline medium enhances effect of gentamicin.
Spiramycin exhibits and antibacterial spectrum avoids both excessive and subtherapeutic Greenwood D, Norrby SR, Whitley RJ,
Dose: Infections due to susceptible organisms,
characteristic of the macrolide family, which concentrations and can prevent toxicity and eds. Antibiotic and chemotherapy. 9th
by IM injection or by slow IV injection
includes Gram-negative and Gram-positive ensure efficacy. If possible serum concen- ed. Available from: www.clinicalkey.com
(over at least 3 minutes) or by IV
cocci, Parvobacteriaceae, Legionella spp., trations should be monitored in all patients, (login required)
infusion,
EMDEX
Chlamydia spp., Mycoplasma Pneumoniae. It is but must be measured in infants, the elderly, ADULT 3–5 mg/kg daily in divided
inactive against Gram-negative rods (Entero- GENTAMICIN
in obesity, in cystic fibrosis, in high-dosage doses every 8 hours; NEONATE up
bacteriaceae) Macrolides bind to the large regimens, in renal impairment, or if treatment Indications: Pneumonia; cholecystitis; peri- to 2 weeks, 3 mg/kg every 12 hours;
subunit of prokaryotic ribosomes and disturb lasts for longer than 7 days. tonitis; septicaemia; acute pyelonephritis; CHILD 2 weeks–12 years, 2 mg/kg
protein synthesis. Spiramycin appears to offer Simultaneous exposure to other potentially prostatitis; otitis externa; skin and soft tissue every 8 hours.
advantages over most other macrolides in nephrotoxic drugs, such as vancomycin, am- infections; pelvic inflammatory disease (with Pelvic inflammatory disease, by IV
terms of its good tolerability and lack of phar- photericin B, cefalosporins, angiotensin-con- clindamycin); endocarditis; meningitis; lister- injection, ADULT 1.5 mg/kg every 8
macokinetic interactions with other drugs, as verting enzyme inhibitors and non-steroidal iosis; tularaemia; brucellosis; plague; surgical hours.
well as its relatively long half-life, which allows anti-inflammatory agents, increases the prophylaxis; eye (section 13.1). Endocarditis (as part of combination
twice-daily administration. likelihood of nephrotoxicity. Contra-indications: Myasthenia gravis. therapy), by IM injection or by IV
Indications: Treatment of infections due Neuromuscular blockade is more likely in Precautions: Renal impairment (Appendix injection (over at least 3 minutes),
to susceptible organisms including ENT, patients who are also receiving muscle relax- 4), neonates, infants and elderly (dosage ADULT 1 mg/kg every 8 hours.
bronchopulmonary and skin infections. In ants or anesthetics, or who are suffering from adjustment and monitor renal, auditory, and Surgical prophylaxis, by IV injection,
certain cases, prevention of meningococcal myasthenia gravis. vestibular function, and serum-gentamicin ADULT 5 mg/kg as a single dose at
meningitis. Aminoglycosides are the mainstay of the treat- concentrations); avoid prolonged use; con- induction (with clindamycin).
Contra-indications: Hypersensitivity to mac- ment of severe sepsis caused by enterobacteria ditions characterized by muscular weakness; Note: One hour (peak) concentrations should not
rolides; avoid co-administration with rye ergot and some other Gram-negative aerobic bacilli. obesity (use ideal bodyweight to calculate dose exceed 5–10 mg/litre (3–5 mg/litre for endocarditis);
derivatives. For the treatment of severe sepsis of unde- and monitor serum-gentamicin concentration pre-dose (trough) concentration should be less than
Precautions: Nausea, vomiting, diarrhoea, termined cause they are often administered closely); see notes above; pregnancy (Appendix 2 mg/litre (less than 1 mg/litre for endocarditis).
allergic reactions. in combination with agents active against 2); breastfeeding (Appendix 3); interactions: POM Gentamicin (WMF 6.2.2)
Dose: Adult, by mouth, one tab. 2-3 times Gram-positive or anaerobic bacteria as ap- Appendix 1. Injection, Gentamicin (as sulfate) 10 mg/mL, 40 mg/
daily. propriate. Some are also used for a number of Adverse effects: Vestibular and auditory dam- mL; in 2-mL vials.
specialized infections, including endocarditis, age, nephrotoxicity; rarely, hypo-magnesaemia
POM ROVAMYCIN® (Sanofi-Aventis) POM Gentamicin (EDL 5.3)
respiratory infections and tuberculosis. on prolonged therapy; antibiotic-associated Injections, Gentamicin (as sulfate) 10 mg, 40 mg per
Tablet, Spiramycin 3 M.I.U.; coated tab.
3 M.I.U – 10. colitis, stomatitis; also, nausea, vomiting, rash, mL; in 2-mL vials.
Gentamicin is almost unabsorbed from the
blood disorders.
POM SPIRACIN® (Al-Tinez) alimentary tract, but well absorbed after intra- POM CHANMYCIN® (Chanmedi)
Advice to patients: Report any dizziness or
Tablet, Spiramycin 3,000,000 IU; f-c tab muscular injection. In systemic Ps. aeruginosa Injection, Gentamicin 80 mg.
sensations of ringing or fullness in ears.
Pack: 2x 5’s (in blisters) infections it is advisable to combine gen- 80 mg – 2 mL x 10 x 10’s.
Nursing action: Obtain specimens for C&S
tamicin with an antipseudomonal penicillin or POM EVRIL® (Medreich)
tests prior to the first dose.
9.1.2.5 Aminoglycosides cefalosporin, owing to likelihood of gentamicin • Administer IM injection in large muscle area at Injections, Gentamicin (as sulfate) 40 mg, 80 mg,
Aminoglycosides including gentamicin resistance. Loading and maintenance doses of uniform intervals to maintain blood level; rotate 280 mg per 2 mL; clear and colourless solution for
are bactericidal and active against some gentamicin are based on the patient’s weight inj sites. injection in 2 mL amps.
and renal function (for example, using a nom- • Give IV after diluting in NS or D5W as ordered; ob- Pack: 10’s; 100’s.
Gram-positive and many Gram-negative or-
ganisms including Pseudomonas aeruginosa. ogram) with adjustments based on plasma serve IV infusion site for inflammation; discontinue POM GENTA® (Strides Vital)
gentamicin concentration. High doses are used and apply warm compress to an inflamed site. Injections, Gentamicin 80 mg, 280 mg per 2 mL;
Aminoglycosides are not absorbed from the
occasionally for serious infections. • Give other antibiotic drugs at least 1 hour before in amps.
gut and must therefore be given by injection or after gentamicin.
394 | 9.1.2.5 Aminoglycosides 9.1.2.6 Nitroimidazoles | 395
Pack: 100’s. POM SIVOMYCINE® (Adpharm) g/day. Injection, Streptomycin 5 g.
Injection, Gentamicine 80 mg, 280 mg per 2 mL. (Additional information sourced from Nivemycin monograph
5 g – 10’s.
POM GENTALAB® (Embassy)
80 mg/2 mL – 1 x 10’s; 1 x 100’s available from http://www.medicines.org.uk/)
Injection, Gentamicin 140 mg. POM SEPTOMINE® (Shrezar)
280 mg/2 mL – 1 x 10’s; 1 x 100’s
Pack: 10’s. Injection, Streptomycin (as sulphate) 1 g in a vial
POM TAMAN® (Beta Drugs) POM Neomycin (EDL 5.3) Pack: 1’s; 50’s vials
POM GENTALEK® (Taylek) Table, Neomycin 500 mg.
Injection, Gentamicin 40 mg (40,000 units) per mL;
Injection, Gentamicin sulfate 40 mg per mL; in 2 Oral liquid, Neomycin 100 mg per 5 mL. POM SIVOTOMYCIN® (Ad[harm)
in 2-mL glass ampoule.
mL amp. Injection, Streptomycin sulfate 5 g
Pack: 10’s x 1-mL; 5’s x 2-mL; 10’s x 2-mL; 50’s x 2-mL; POM Neomycin (Rajrab)
Pack: 50’s. Pack: 1 x 50’s
100’s x 2-mL. Tablet, Neomycin (as sulphate) 500 mg; scored tab.
POM Gentamicin (Embassy) Injection, Gentamicin 280 mg per 2 mL; in 2-mL marked with company logo. POM Streptomycin (Pharmabox)
Injection, Gentamicin 80 mg per 2 mL. glass ampoule. 500 mg – 100’s Injection, Streptomycin (as sulfate) 5 g; white or
Pack: 10 mL. almost white powder which forms clear solution
NEOMYCIN STREPTOMYCIN on reconstitution.
POM Gentamicin (Jawa)
Therapeutic category: Aminoglycoside Pack: 5 g x 10’s (in vials)
Injection, Gentamicin 80 mg per 2 mL Therapeutic category: Antibiotic.
Pack: 20 x 10 x 10’s antibiotic. Indications: Treatment of tuberculosis in
Pharmacology: Neomycin acts by binding to 9.1.2.6 Nitroimidazoles
POM Gentamicin (Juhel) combination with other drugs; other infections
Injection, Gentamicin (as sulfate) 80 mg per 2 mL; polysomes, inhibiting protein synthesis and where patients are allergic to or have failed to The available 5-nitroimidazoles include
in 2-mL amp. generating errors in the transcription of the respond to penicillin. metronidazole, tinidazole, ornidazole, secni-
Pack: 2 mL x 5 x 10’s. genetic code. Only about 3% of an oral dose is Contra-indications: Myasthenia gravis. dazole. They possess excellent activity against
absorbed, the remainder being rapidly excreted Precautions: Pregnancy, renal impairment, anaerobic bacteria, including Bacteroides spp.,
POM Gentamicin (Pharmabox)
Injection, Gentamicin (as sulfate) 280 mg per 2 mL. by the kidneys as unchanged drug. T1/2 in elderly Clostridium spp., Prevotella spp. and Fusobac-
healthy adults is approx. 2-3 hours. Oral doses terium spp. They are also active against some
EMDEX
Pack: 2 mL x 100’s Interactions: Ototoxic diuretics such as fruse-
of 3 g produce peak plasma concentrations of mide. See under Gentamicin. susceptible protozoa including T. vaginalis,
POM GENTAZET® (Geneith) up to 4 μg/mL. See also the clinical notes above. Giardia lamblia, Entamoeba histolytica, Balan-
Injections, Gentamicin (as sulfate) 80 mg, 280 mg per Adverse effects: Vestibular and auditory
Indications: Pre-operative sterilisation of the damage; nephrotoxicity, neuromuscular block- tidium coli and Blastocystis hominis.
2 mL; clear liquid in amps.
80 mg/2 mL – 1 x 10’s bowel; hepatic coma. ade, rash, nausea, vomiting, fever, headache, Metronidazole is available for oral adminis-
280 mg/2 mL – 1 x 10’s Contra-indications: Hypersensitivity to amino- drowsiness. tration or as a suppository; also formulated
glycosides; Intestinal obstruction; Myasthenia Advice to patients: Report any unusual symp- as the hydrochloride for intravenous use, and
POM IBUTEX® (Jubilee)
gravis; Infants under 1 year; Renal or hepatic toms of hearing loss, dizziness, roaring noises, as the benzoate in an oral suspension and
Injections, Gentamicin BP 80 mg, 280 mg per 2 mL;
in ampoules.
disease. or fullness in ears. a dental gel. Alcohol should not be taken
Pack: 10’s; 50’s 100’s. Precautions: Impaired GI motility may lead to Nursing action: Obtain specimens for C&S during and for 48 h after therapy because of
increased intestinal absorption and higher risk tests prior to the first dose. a possible disulfiram-like reaction, nor should
POM KALMYCIN® (Justeen) of toxicity; Elderly; Neuromuscular disorders • Administer IM injection in large muscle area at it be combined with formulations containing
Injection, Gentamicin (as sulfate) 80 mg per 2 mL.
and Parkinsonism; Avoid prolonged therapy; uniform intervals to maintain blood level; rotate alcohol. It enhances the anticoagulant effect
Pack: 2 mL x 1’s (in flint vials).
Monitor regularly the auditory, vestibular and inj sites.
of warfarin and may impair the clearance of
POM LUTEMIS® (Quadrant) renal functions. • IV inj is not recommended.
phenytoin and lithium. Phenytoin may increase
Injection, Gentamicin (as sulphate) 80 mg per 2 mL. Interactions: Additive toxicity with nephrotoxic • See also under Gentamicin.
the metabolism of metronidazole. Plasma con-
Pack: 2 mL amp agents (e.g. amphotericin) or ototoxic agents (e.g. Dose: See under section 9.1.4.
centrations are decreased by the concomitant
POM METHACINE® (E-Globa) loop diuretics) or non-depolarising muscle relax- POM Streptomycin (EDL 5.10) administration of phenobarbital. The drug
Injection, Gentamicin 80 mg per 2 mL; clear colour- ants. May enhance the effects of anticoagulants. Injection, Streptomycin sulfate 1 g, 5 g; powder should be avoided in pregnancy, especially
less solution for injection in 2-mL amps. Adverse effects: Nausea, vomiting, diarrhoea, in vials.
Pack: 2 mL x 10’s; 100’s.
during the first trimester and particularly if
increased salivation, stomatitis, nephrotoxicity, POM LINASTREP® (E-Globa) high doses are being administered. Use during
POM MYLLIN® (Vixa) ototoxicity, rise in serum levels of hepatic Injection, Streptomycin 5 g; white powder in vials. the 2nd and 3rd trimesters may be acceptable
Injection, Gentamicin 280 mg/2 mL, 80 mg/2 mL. enzymes and bilirubin, blood dyscrasias, Pack: 1 x 10’s; 100’s if alternative therapies for trichomoniasis have
Pack: 2 mL x 10’s. haemolytic anaemia, confusion, paraesthesia,
POM MATOSTREP® (GoldMoore) failed, but single-dose (2 g oral) therapy should
POM PADEX® (Justeen) disorientation, nystagmus, hypersensitivity Injections, Streptomycin (as sulfate) 1 g (1 million be avoided.
Injection, Gentamicin (as sulfate) 80 mg per 2 mL. reactions including dermatitis, pruritus, drug units), 5 g (5 million units).
fever and anaphylaxis. The drug may cause the breast milk to taste
Pack: 1 x 100’s. Pack: 1 g; 5 g.
Malabsorption syndrome, superinfection, bitter. Breast feeding should be discontinued
POM PAULIO® Gentamycin (Pacmai) POM O-STREPS® (Beta Drugs) until 24 h after the last dose to allow excretion
Injection, Gentamicin (as sulphate) 80 mg per 2 mL electrolyte disturbances especially on pro-
Injections, Streptomycin (as Sulfate) 1 g (1 million of the drug. It appears safe when given to nurs-
Pack: 1 x 10’s amp. longed use. units), 5 g (5 million units) per vial; white or almost
Dose: By mouth, Adult, Pre-operative sterilisa- ing mothers at doses of up to 400 mg every 8 h.
white powder, freely soluble in water.
POM PEGENT® (Pemason) Adverse effects may include unpleasant
tion of the bowel, 1 g every hour for 4 Pack: 100’s (in vials).
Injection, Gentamicin 80 mg per 2 mL; in 2-mL amp.
hours; then 1 g every 4 hours for 2-3 sharp, metallic taste, furry tongue, glossitis
marked “Pegent”. POM PAULIO® Streptomycin (Pacmai)
Pack: 2 mL x 10 x 10’s. days before the operation. and stomatitis. Stomatitis may be associated
Injection, Streptomycin (as sulphate) 5 g per vial.
Hepatic coma, up to 4-12 g/day in Pack:1 x 10’s in vials with overgrowth of Candida spp. during treat-
POM REGENTA® (GoldMoore) divided doses usually for 5–7 days. ment. Gastrointestinal disturbances include
Injection, Gentamicin 280 mg per 2 mL; in 2 mL amp. POM REPTOCIN® (Embassy) nausea, vomiting, abdominal discomfort and
Chronic hepatic insufficiency, up to 4
396 | 9.1.2.6 Nitroimidazoles 9.1.2.7 Nitrofurantoin | 397
diarrhea. Pseudomembranous colitis has also hepatitis, jaundice, thrombocytopenia, aplastic Surgical prophylaxis, by rectum, ticaria, rash, sialadenitis, pruritus, angioedema;
been reported. anaemia, myalgia, arthralgia; peripheral neu- ADULT 1 g 2 hours before surgery; up anaphylaxis reported; rarely, cholestatic
Tinidazole has antibacterial and antiproto- ropathy, epileptiform seizures, leukopenia, on to 3 further doses of 1 g may be given jaundice, hepatitis, exfoliative dermatitis;
zoal activity similar to that of metronidazole. prolonged or high dosage regimens. every 8 hours for high-risk proce- erythema multiforme, pancreatitis, arthralgia;
Side effects are infrequent and transient and Advice to patients: Tablets should be swal- dures; CHILD 5–10 years 500 mg 2 blood disorders; pulmonary reactions (pulmo-
may include nausea, vomiting, diarrhea and lowed whole with water, during or after food; hours before surgery; up to 3 further nary fibrosis; possible association with lupus
a metallic taste. Disulfiram-like reactions can suspension best taken one hour before food doses of 500 mg may be given every erythematosus-like syndrome); peripheral
occur with alcohol. (or on an empty stomach). Avoid alcoholic 8 hours for high-risk procedures. neuropathy; benign intracranial hypertension;
beverages. Surgical prophylaxis by IV infusion (if transient alopecia.
Ornidazole has antimicrobial activity closely Dose: Anaerobic infections (usually treated rectal administration inappropriate), Advice to patients: Take with food or milk;
resembling that of metronidazole and tinida- for 7 days), by mouth, ADULT 800 mg ADULT 500 mg at induction; up to 3 may discolour urine to a dark yellow or brown
zole; also shares similar adverse effect profile. initially then 400 mg every 8 hours or further doses of 500 mg may be given colour; notify physician if fever, chest pain,
The dosing interval should be doubled in 500 mg every 8 hours; CHILD 7.5 mg/ every 8 hours for high-risk proce- persistent, nonproductive cough, or difficulty
patients with severe hepatic impairment, but kg every 8 hours. dures; CHILD 7.5 mg/kg at induction; in breathing occurs.
it is unnecessary to reduce the dose in patients Anaerobic infections, by IV infusion up to 3 further doses of 7.5 mg/kg Nursing action: Administer around-the-clock
with impaired renal function. over 20 minutes, ADULT 500 mg every may be given every 8 hours for high- in equal intervals to promote less variation in
Secnidazole has properties similar to those of 8 hours; CHILD 7.5 mg/kg every 8 risk procedures. peak and trough serum levels.
metronidazole. It is rapidly absorbed after oral hours. POM Metronidazole (WMF 6.2.2)
• Give with meals or milk to reduce GI upset.
administration and is distinguished by having Anaerobic infections, by rectum, • Continue treatment for 3 days after sterile urine
Tablets, Metronidazole 200-500 mg.
the longest plasma half-life (18 hours) of clini- ADULT and CHILD over 10 years 1 specimen have been obtained.
Oral liquid, Metronidazole (as benzoate) 200 mg/5
cally used nitroimidazole drugs. It is used in the • Observe closely for superinfection.
g every 8 hours for 3 days, then 1 g mL.
Dose: Acute uncomplicated urinary-tract infec-
EMDEX
treatment of intestinal amebiasis, giardiasis, every 12 hours; CHILD up to 1 year, Injection, Metronidazole 500 mg in 100-mL bag.
trichomoniasis and bacterial vaginosis. 125 mg every 8 hours for 3 days, then Suppositories, Metronidazole 500 mg, 1 g tions, by mouth, ADULT 100 mg every
every 12 hours; 1–5 years 250 mg; 12 hours or 50 mg every 6 hours with
References: POM Metronidazole (EDL 5.3) food for 7 days; CHILD over 3 months,
1) Jenks PJ. Nitroimidazoles. In: Finch RG, 5–10 years 500 mg. Tablets, Metronidazole 200 mg, 400 mg.
Bacterial vaginosis, by mouth, ADULT 3 mg/kg daily in 4 divided doses.
Greenwood D, Norrby SR, Whitley RJ, Oral liquid, Metronidazole (as benzoate) 200 mg/5
2 g as a single dose or 400–500 mg mL. Severe recurrent urinary-tract infection,
eds. Antibiotic and chemotherapy. 9th by mouth, ADULT 100 mg every 6
twice daily for 5–7 days. Injection, Metronidazole 500 mg in 100-mL bottle.
ed. Available from: www.clinicalkey.com hours with food for 7 days (dose
(login required) Pelvic inflammatory disease, by mouth, See section 9.3.2 for the proprietary preparations of
ADULT 400–500 mg twice daily for reduced to 200 mg daily in divided
Metronidazole.
14 days. doses, if severe nausea).
METRONIDAZOLE Prophylaxis of urinary-tract infections
Indications: Anaerobic bacterial infections, Leg ulcers and pressure sores, by
9.1.2.7 Nitrofurantoin (see Precautions), by mouth, ADULT
including gingivitis and other oral infections, mouth, ADULT 400 mg every 8 hours
for 7 days. Nitrofurantoin is bactericidal in vitro to most 50–100 mg at night; CHILD over 3
pelvic inflammatory disease (with ceftriaxone months, 1 mg/kg at night.
Acute ulcerative gingivitis, by mouth, Gram-positive and Gram-negative urinary-tract
and doxycycline), tetanus, septicaemia, peri-
200–250 mg every 8 hours for 3 days; pathogens and it is used to treat acute and POM Nitrofurantoin (WMF 6.2.2)
tonitis, brain abscess, necrotizing pneumonia,
CHILD 1–3 years, 50 mg every 8 hours recurrent urinary-tract infections. It is also Tablet, Nitrofurantoin 100 mg.
antibiotic-associated colitis, leg ulcers and
for 3 days; 3–7 years, 100 mg every 12 used prophylactically in chronic urinary-tract POM Nitrofurantoin (EDL 5.3)
pressure sores and surgical prophylaxis; bac-
hours for 3 days; 7–10 years, 100 mg infections. Tablets, Nitrofurantoin 50 mg, 100 mg.
terial vaginosis; skin and soft tissue infections,
animal bites (with doxyxline); tissue nematode every 8 hours for 3 days.
Acute oral infections, by mouth, NITROFURANTOIN 9.1.2.8 Spectinomycin
infections (section 9.4.1.3); trichomonal vagi-
ADULT 200 mg every 8 hours for 3–7 Indications: Urinary-tract infections.
nitis, amoebiasis, and giardiasis (section 9.3.2); Spectinomycin is active against Gram-negative
days; CHILD 1–3 years 50 mg every 8 Contra-indications: Impaired renal function
Helicobacter pylori eradication (section 4.1). organisms including Neiserria gonorrhoea. It is
hours for 3–7 days; 3–7 years 100 mg (Appendix 4); infants less than 3 months;
Contra-indications: Chronic alcohol depend- not suitable for the treatment of syphilis and
every 12 hours; 7–10 years 100 mg G6PD-deficiency including breastfeeding of
ence. patients being treated for gonorrhoea should
every 8 hours. affected infants (Appendix 3); pregnancy, at
Precautions: Disulfiram-like reaction with be observed for evidence of syphilis. It should
Antibiotic-associated colitis, by mouth, term (Appendix 2); porphyria.
alcohol; hepatic impairment and hepatic be used only when alternative therapies are
800 mg initially then 400 mg 3 times Precautions: Pulmonary disorders or hepatic
encephalopathy (Appendix 5); pregnancy (Ap- inappropriate.
daily for 10 days. impairment (Appendix 5); monitor lung and
pendix 2); breastfeeding (Appendix 3); clinical
Surgical prophylaxis, by mouth, ADULT liver function on long-term therapy (discon-
and laboratory monitoring in courses lasting SPECTINOMYCIN
400–500 mg 2 hours before surgery; tinue if lung function deteriorates); neurolog-
longer than 10 days; interactions: Appendix 1. Indications: Uncomplicated and disseminated
up to 3 further doses of 400–500 ical or allergic disorders; anaemia; diabetes
Adverse effects: Nausea, vomiting, unpleasant gonorrhoea (see notes above); adult and ne-
mg may be given every 8 hours for mellitus; elderly and debilitated; vitamin B and
metallic taste, furred tongue and gastrointesti- onatal gonococcal conjunctivitis; chancroid.
high-risk procedures; CHILD 7.5 mg/ folate deficiency; false positive urinary glucose
nal disturbances; rarely, headache, drowsiness, Precautions: Renal impairment; pregnancy
kg 2 hours before surgery; up to 3 (if testing for reducing substances); urine may
dizziness, ataxia, darkening of urine, erythema and breastfeeding.
further doses of 7.5 mg/kg may be be coloured yellow or brown.
multiforme, pruritus, urticaria, angioedema, Adverse effects: Nausea, headache, dizziness,
given every 8 hours for high-risk Adverse effects: Dose-related GI disorders;
and anaphylaxis; abnormal liver function tests, fever, chills, insomnia, urticaria; rarely, anaphy-
procedures. nausea; hypersensitivity reactions including ur-
398 | 9.1.2.9 Sulfonamides and trimethoprim 9.1.2.9 Sulfonamides and trimethoprim | 399
laxis; pain at injection site. The reason is probably blocking of sodium arthralgia, myalgia, vasculitis, and systemic Tablet, (Forte),Co-trimoxazole 960 mg.
Nursing action: Since Spectinomycin is channels, thus disturbing the sodium–po- lupus erythematosus. 960 mg – 10; 100.
ineffective in the treatment of syphilis and tassium balance. The effect is reversible by Nursing action: Obtain specimen for C&S tests Suspension, Co-trimoxazole 240 mg per 5 mL; milky
may mask symptoms, all patients should be supplementing sodium intake and restricting before first dose; therapy may begin pending white with banana flavour/aroma.
Pack: 50 mL.
tested for syphilis at the time of diagnosis and potassium. test results.
3 months later. • Give on an empty stomach 1 hr before or 2 hr POM BENCOTRIM® (Nichben)
The usefulness of other sulfonamides is limited
• For I.M. use only; use 20G needle for the admin- after meals with a full glass of water to maintain Tablet, Sulfamethoxazole 400 mg, Trimethoprim
by increasing incidence of bacterial resistance adequate hydration. Encourage patient to increase 80 mg
istration. The 4-g dose (10 mL) should be divided
into two 5-mL injections and given one in each and they are being replaced by antibiotics that fluid intake to avoid crystallization in kidneys. Suspe9nsion, Sulfamethoxazole 200 mg, Trimethop-
buttocks. are more active and safer. • Observe for signs of superinfection namely fever, rim 40 mg per 5 mL.
• Reconstituted solution should be used within 24 References: sore throat, fatigue.
POM BENTRIM® (Bentos)
hours at room temperature; shake vial vigorously 1) Swedberg G, Sundström L. Diaminopy- • Signs of blood dyscrasias include skin rash, sore
Tablet, Sulfamethoxazole 400 mg, trimethoprim
before use. throat, fever, or mouth sore and should be reported
rimidines. In: Finch RG, Greenwood D, 80 mg
Dose: Uncomplicated gonococcal infections immediately to the physician
Norrby SR, Whitley RJ, eds. Antibiotic and • Note that the “DS” or “DF” product means “double
480 mg – 10 x 20’s; 1000’s.
and chancroid, by deep IM injection, chemotherapy. 9th ed. Available from: Suspension, Sulfamethoxazole 200 mg;Trimethoprim
strength”.
ADULT 2 g as a single dose (may be www.clinicalkey.com (login required) 40 mg per 5 mL,
• Monitor patient for allergic reactions.
increased to 4 g as a single dose Pack: 50 mL; 2 L.
Dose: Severe infections due to susceptible
divided between 2 injection sites CO-TRIMOXAZOLE POM BONATRIM® (Bond)
organisms (not susceptible to other
in difficult to treat cases and where Tablet, Trimethoprim 80 mg, sulfamethoxazole
Synonym: Sulfamethoxazole plus Trimethop- antibacterials), by mouth or by IV in-
there is known antibiotic resistance 400 mg
rim; SMZ-TMP. fusion, ADULT sulfamethoxazole 800
Disseminated gonococcal infections, Paediatric oral suspension,Trimethoprim 40 mg,
Indications: Urinary-tract infections; respira- mg with trimethoprim 160 mg every
by deep IM injection, ADULT 2 g twice sulfamethoxazole 200 mg per 5 mL.
EMDEX
tory-tract infections including bronchitis, 12 hours, increased to sulfamethoxa- Pack: 50 mL.
daily for 7 days.
pneumonia, infections in cystic fibrosis; ty- zole 1.2 g with trimethoprim 240 mg,
Neonatal gonococcal conjunctivitis, by POM CADIPRIM® (Interpharma)
phoid fever; melioidosis; listeriosis; brucellosis; every 12 hours in more severe infec-
deep IM injection, neonate 25 mg/kg Tablet, Co-trimoxazole 480 mg.
granuloma inguinale; neonatal chlamydial tions; by mouth, CHILD 6 weeks–5
(maximum 75 mg) as a single dose. 480 mg – 10 x 10’s.
conjunctivitis; otitis media; skin infections, an- months, sulfamethoxazole 100 mg
Suspension, Co-trimoxazole 240 mg per 5 mL
POM Spectinomycin (WMF 6.2.2) imal bites; Pneumocystis carinii (Pneumocystis with trimethoprim 20 mg every 12 Pack: 50 mL; 100 mL.
Powder for injection, Spectinomycin (as HCl) 2 g; jiroveci) pneumonia (section 9.3.5). hours; 6 months–5 years, sulfameth-
in vial. Contra-indications: Hypersensitivity to sulfo- oxazole 200 mg with trimethoprim POM CHEMOTRIM® (Afrab-Chem)
Tablet, Co-trimoxazole 480 mg; average size (13 mm),
POM TOGAMYCIN® (Pfizer) namides or trimethoprim; porphyria. 40 mg every 12 hours; 6–12 years,
golden yellow scored tab. marked ‘afrab’.
Injection, Spectinomycin (as HCl) 2 g; 1 vial contain- Precautions: Renal impairment (avoid if se- sulfamethoxazole 400 mg with tri- Pack: 1000.
ing sterile powder for reconstitution + water for vere; Appendix 4); hepatic impairment (avoid methoprim 80 mg every 12 hours; by Suspension, Co-trimoxazole 240 mg per 5 mL; cream,
injection as diluent in amp. if severe; Appendix 5); maintain adequate fluid IV infusion, CHILD sulfamethoxazole moderately thick.
Pack: 2 g vial + amp. with diluent (3.2 mL). intake (to avoid crystalluria); avoid in blood 30 mg/kg daily with trimethoprim 6 Pack: 60 mL; 100 mL.
disorders (unless under specialist supervision); mg/kg daily in 2 divided doses.
9.1.2.9 Sulfonamides and POM CIKACOTRIM® (Michelle Lab)
monitor blood counts and discontinue imme- POM Sulfamethoxazole plus Trimethoprim Tablet, Sulfamethoxazole 400 mg, trimethopirm
trimethoprim diately if blood disorder develops; rash—dis- (WMF 6.2.2) 80 mg
Co-trimoxazole is a 1:5 mixture of trimethop- continue immediately; predisposition to folate Tablets, Sulfamethoxazole 100 mg with trimeth- Pack: 10 x 10’s (in blisters); 1000’s (in jars)
rim and sulfamethoxazole. These combinations deficiency or hyperkalaemia, elderly; asthma; oprim 20 mg; Sulfamethoxazole 400 mg with
POM CLOBOTEL®-960 (Geneith)
exhibit the activity of, and synergy between, G6PD deficiency; pregnancy (Appendix 2); trimethoprim 80 mg.
Tablet, Co-trimoxazole 960 mg.
the two components. They may also mutually breastfeeding (Appendix 3); avoid in infants Oral liquid, Sulfamethoxazole 200 mg with trimeth-
cross-suppress the emergence of resistance. under 6 weeks; interactions: Appendix 1. oprim 40 mg/5 mL. POM COPTRINE® (Drugfield)
As well as lowering the concentration required Adverse effects: Nausea, diarrhoea; headache; Injection, Sulfamethoxazole 80 mg with trimethop- Tablet, Sulfamethoxazole 400 mg, trimethoprim
rim 16 mg/mL; in 5-mL and 10-mL ampoules. 80 mg
to inhibit growth, the mixture is often bacte- hyperkalaemia; rash (very rarely including
ricidal when the individual components are Stevens-Johnson syndrome, toxic epidermal POM Co-trimoxazole (EDL 5.3)
Paediatric suspension, Sulfamethoxazole 200 mg,
bacteriostatic. necrolysis, photosensitivity)—discontinue Tablet, Sulfamethoxazole 400 mg, trimethoprim
trimethoprim 40 mg per 5 mL.
immediately; less commonly vomiting; very 80 mg.
The antimicrobial spectrum covers pathogens Pack: 50 mL
rarely glossitis, stomatitis, anorexia, liver dam- Oral liquid, Sulfamethoxazole 200 mg, trimethoprim
susceptible to the individual agents and is 40 mg per 5 mL. POM CO-TRIGEM® (Gemini)
expanded by synergistic interaction. Some age (including jaundice and hepatic necrosis),
pancreatitis, antibiotic-associated colitis, POM AVROTRIM® (Avro)
organisms that are refractory to many other an- Pediatric Suspension, Co-trimoxazole 240 mg per 5
myocarditis, cough and shortness of breath, Tablet, Co-trimoxazole 480 mg; white scored tab.
tibiotics remain susceptible to co-trimoxazole. marked “AVRO/AVT’
mL; banana flavoured susp.
pulmonary infiltrates, aseptic meningitis,
Hyperkalemia is a potential complication of depression, convulsions, peripheral neurop- 480 mg – 100’s; 1000’s. POM Cotrimoxazole (Ceenek)
therapy with high-dose trimethoprim (20 Suspension, Co-trimoxazole 240 mg per 5 mL. Tablet, Sulfamethoxazole 400 mg, trimethoprim
athy, ataxia, tinnitus, vertigo, hallucinations, Pack: 50 mL.
mg/kg per day) in patients with AIDS and may 80 mg
hypoglycaemia, blood disorders (including 480 mg – 1000’s; 10 x 100’s (in blisters)
also develop in about 20% of patients under leukopenia, thrombocytopenia, megaloblas- POM BACTRIM® (Swipha)
Paediatric suspension, Sulfamethoxazole 200 mg,
standard therapy with co-trimoxazole, and in tic anaemia, eosinophilia), hyponatraemia, Tablet, Co-trimoxazole 480 mg; white scored tab.
trimethoprim 40 mg per 5 mL
up to 85% of patients with renal insufficiency. renal disorders including interstitial nephritis,
480 mg – 20.
Pack: 50 mL
POM Co-Trimoxazole (Dizpharm) 960 mg – 2 x 10’s, 1 x 10000’s Tablet, Sulfamethoxazole 400 mg, trimethoprim Suspension, Co-trimoxazole 240 mg per 5 mL
Tablet, Co-trimoxazole 480 mg. Paediatric suspension, Co-trimoxazole 240 mg per 5 80 mg; marked “NACOTRIM/480 on one side and Pack: 50 mL; 1000 mL; 2500 mL.
480 mg – 10 x 100; 1000. mL; pink raspberry flavoured suspension “NASDMU”on reverse side.
POM SEPOX® (Dana)
Suspension, Co-trimoxazole 240 mg per 5 mL. Pack: 50 mL. 480 mg – 1000’s; 10 x 10’s
Tablet, Sulphamethozaxole 400 mg, trimethoprim
Pack: 50 mL.
POM GARYTRIM® (Agary) POM NECOTRIM® (Neimeth) 80 mg; uncoated tab.
POM Co-trimoxazole (Goz) Tablet, Trimethoprim 80 mg, sulfamethoxazole Tablet, Co-trimoxazole 480 mg. Pack: 1000’s; 100’s (in jar) 10 x 10’s (in blisters)
Suspension, Co-trimoxazole 240 mg per 5 mL. 400 mg 480 mg – 20’s. Paediatric suspension, Sulphamethozaxole 200 mg,
Pack: 50 mL in amber bottle. Suspension, Co-trimoxazole 240 mg per 5 mL trimethoprim 40 mg per 5 mL.
POM JAWATRIM® (Jawa)
Pack: 60 mL. Pack: 50 mL.
POM Co-trimoxazole (Evans) Suspension, Sulfamethoxazole 200 mg, Trimethop-
Tablet, Trimethoprim 80 mg, sulfamethoxazole rim 40 mg per 5 mL; pink coloured. POM OPTRIM® (Topway) POM SEPTRIN® (GSK)
400 mg Pack: 50 mL. Tablet, Sulfamethoxazole 400 mg, Trimethoprim 80 Tablet, Co-trimoxazole 480 mg; white tab. coded
Pack: 100’s; 1000’s mg; round flat tab. marked ‘TOPWAY’ on one side ‘Y2B’ and marked with tab. and maker’s names.
POM JUTRIM® (Juhel)
Suspension, Trimethoprim 40 mg, sulfamethoxazole and ‘OPTRIM/480’ on the reverse. Suspension, Co-trimoxazole 240 mg per 5 mL
Tablets, Co-trimoxazole 480 mg; white scored bi-
200 mg per 5 mL 480 mg – 100’s; 1000’s.
convex tablet marked ‘Jutrim 480’ on one side and POM SHALPHATRIM® (Shalina)
Pack: 50 mL Suspension, Sulfamethoxazole 200 mg, Trimethop-
‘Juhel’ on the reverse. Tablet, Sulfamethoxazole 400 mg, Trimethoprim
rim 40 mg per 5 mL.
POM Co-trimoxazole (Mopson) 480 mg – 10 x 100’s; 1000’s. 80 mg; white scored tab. marked ‘Shalphatrim 480’
Pack: 50 mL; 2 L.
Tablet, Trimethoprim 80 mg, sulfamethoxazole Suspension, Co-trimoxazole 240 mg per 5 mL 480 mg – 10 x 10’s.
400 mg Pack: 50 mL; 100 mL. POM PANTRIM® (Jopan) Suspension, Sulfamethoxazole 200 mg, Trimeth-
Pack: 1000’s Tablet, Trimethoprim 80 mg, sulfamethoxazole 400 oprim 40 mg per 5 mL; pink coloured susp. with
POM KIDITRIM® (Therapeutic)
Suspension, Trimethoprim 40 mg, sulfamethoxazole mg; white scored tab. marked ‘JOPAN’ on one side mango flavour.
Suspension, Sulfamethoxazole 200 mg, Trimethop-
200 mg per 5 mL and ‘COTRIM/480’ on the reverse. Pack: 50 mL.
rim 40 mg per 5 mL.
Pack: 50 mL; 2 L 480 mg – 10 x 10’s (in blisters); 1000’s.
EMDEX
Pack: 50 mL. POM SULFAB® (FAB)
Caplet, Sulfamethoxazole 800 mg, Trimethoprim 160
POM Co-trimoxazole (Neimeth) Syrup, Sulfamethoxazole 200mg, trimethoprim 40
POM LATRIM® (Mecure) mg; white scored caplet marked ‘JOPAN’
Tablet, Co-trimoxazole 480 mg mg per 5 mL
Tablet, (480 mg), Co-trimoxazole 480 mg; white 960 mg – 10 x 10’s (in blisters).
480 mg – 500. Pack: 50 mL.
scored tab. marked ‘COTRI’ and ‘480’.
Suspension, Co-trimoxazole 240 mg per 5 mL POM PARKAPRIM® (Pharma–Deko)
480 mg – 10 x 10’s; 1 x 1000’s. POM SUMEZOL® (Watson)
Pack: 50 mL. Tablet, Co-trimoxazole 480 mg; white uncoated plain
Caplet, (960 mg), Co-Trimoxazole 960 mg; white Tablet, Co-trimoxazole 480 mg; white.
tab. marked ‘PARKAPRIM’.
POM Co-trimoxazole (Vitabiotics) oblong tab. marked ‘LATRIM’ and ‘960’. Pack: 10 x 10’s, 1000’s.
480 mg – 20; 1000.
Tablet, Sulfamethoxazole 400 mg,trimethoprim 960 mg – 1 x 10’s.
Suspension, Co–trimoxazole 240 mg per 5 mL; pink POM SUPRIM® (Hovid)
80 mg Suspension, Sulfamethoxazole 200 mg, trimethoprim
coloured well flavoured suspension. Tablets, Co-trimoxazole 480 mg, 960 mg.
Pack: 1000’s 40 mg; pink susp.
Pack: 50 mL; 2 L. 480 mg – 10 x 10 (blister)
Suspension, Sulfamethoxazole 200 mg,trimethoprim Pack: 50 mL
960 mg – 10 x 10 (blister).
40 mg per 5 mL POM PILTRIM® (Pharchem)
POM LOXAPRIM® (May & Baker) Suspension, Co-trimoxazole 240 mg per 5 mL
Pack: 50 mL Tablet, Co-trimoxazole 480 mg.
Tablet, Co-trimoxazole 480 mg; scored tab. marked Pack: 60 mL; 100 mL.
Suspension, Co-trimoxazole 240 mg per 5 mL
POM COTIBEL® (Geneith) “M&B 480 mg” on one side and “Loxaprim” on the
POM TAVTRIM® (Justeen)
Tablet, Co-trimoxazole 960 mg. reverse. POM PRIMPEX® (SKG)
Tablet, Co-trimoxazole BP 480 mg.
480 mg – 10 x 10’s. Tablet, Co-trimoxazole 480 mg; white scored tab.
POM COTRIZOL® (Ranbaxy) Pack: 10 x 10’s.
Suspension, Co-trimoxazole 240 mg per 5 mL marked ‘SKG D3A’.
Pack: 50 mL. 480 mg – 20’s; 100’s. POM TECOTRIM® (Richygold)
480 mg – 500; 1000
Caplet (DS), Co-trimoxazole 960 mg; white scored Tablet, (480 mg) Sulfamethoxazole 400 mg, trimeth-
Suspension, Co-trimoxazole 240 mg per 5 mL. POM MAXCOTRIM® (Richygold)
caplet marked ‘SKG G3A’. oprim 80 mg.
Pack: 50 mL; 100 mL. Tablet, Co-trimoxazole 480 mg.
960 mg – 1 x 10’s. Pack: 1 x 10’s; 2 x 10’s; 100 x 10’s.
480 mg – 10 x 10’s; 1 x 1000’s.
POM COTROX® (Vitabiotics) Suspension, Co-trimoxazole 240 mg per 5 mL; pink Tablet, (960 mg) Sulfamethoxazole 800 mg, trimeth-
Suspension, Co-trimoxazole 240 mg per 5 mL POM MD-Co-trimoxazole (O’Nell) syrup flavoured suspension with odour of aniseed. oprim 160 mg.
Pack: 60 mL. Tablet, Trimethoprim 80 mg, sulfamethoxazole 400 Pack: 50 mL; 100 mL (in amber bottles). Pack: 1 x 10’s; 2 x 10’s; 100 x 10’s.
mg; scored tab. marked ‘MD-Co-Trimoxazole’.
POM Dr. Meyer’s Biotrim® (Farmex) POM RAPHATRIM® (Rapha) POM TPRIM-480® (Justeen)
Paediatric suspension, Trimethoprim 40 mg, sul-
Suspension, Sulfamethoxazole 200 mg, trimethoprim Tablet, Sulfamethoxazole 400 mg, trimethoprim Tablet, Co-trimoxazole BP 480 mg.
famethoxazole 200 mg per 5 mL.
40 mg per 5 mL 80 mg Pack: 10 x 10’s; 1000’s.
Pack: 50 mL
Pack: 50 mL Pack: 1 x 10 x 10
POM TRIMAC® (Swipha)
POM MOKOTRIM® (New Healthway)
POM EMBATRIM® (Embassy) POM R-COTRIM® (Strides Vital) Tablet (DS), Trimethoprim 160 mg, sulfamethoxazole
Tablet, Trimethoprim 80 mg, sulfamethoxazole
Tablet, Co-trimoxazole 480 mg. Tablet, Co-trimoxazole 480 mg. 800 mg
400 mg
480 mg – 100’s; 1000’s. 480 mg – 100’s; 1000’s. Pack: 10’s; 100’s
480 mg – 2 x10’s; 1 x1000’s.
Tablet (forte), Co-trimoxazole 960 mg. Tablet, (DS), Co-trimoxazole 960 mg. Paediatric syrup, Trimethoprim 40 mg, sulfamethox-
Tablet, (Double Strenght), Trimethoprim 160 mg,
960 mg – 240’s. 960 mg – 100’s; 1000’s. azole 200 mg per 5 mL.
sulfamethoxazole 800 mg.
Pack: 50 mL
POM EMTRIM® (Emzor) 960 mg – 2 x10’s; 1 x1000’s. POM RANCOTRIM® (Ranbaxy)
Tablet, Co-trimoxazole 480 mg; white scored bicon- Suspension, Trimethoprim 40 mg, sulfamethoxazole Tablet, Co-trimoxazole 480 mg. POM VINCOTRIM® (Vinco)
vex tab. marked ‘EMZOR’. 200 mg per 5 mL 480 mg – 10’s; 1000’s. Tablet, Co-trimoxazole 480 mg.
480 mg – 2 x 10’s, 1 x 10000’s. Pack: 50 mL Tablet (forte), Co-trimoxazole 960 mg. 480 mg – 10 x 10 x 10’s; 1000’s.
Tablet, (DS), Co-trimoxazole 960 mg 960 mg – 10’s; 500’s.
POM NACOTRIM® (NASDMU) POM ZIMATRIM® (Gauze)
Oral Liquid, Sulfamethoxazole 200 mg, trimethoprim deficiency; elderly; asthma; G6PD deficiency; Tablet, Sulfadimidine 500 mg; white biconvex tab. SULFATHIAZOLE plus SULFADIAZINE
40 mg per 5 mL pregnancy (Appendix 2); breastfeeding (Ap- 500 mg – 1000. plus SULFAMERAZINE
Pack: 50 mL; 2 L pendix 3); avoid in infants under 6 weeks; POM Sulfadimidine (Vitabiotics)
Synonym: Trisulfonamide.
POM ZOTRIM® (Fidson) interactions: Appendix 1. Tablet, Sulfadimidine 500 mg. Indications: Acute infections by pneumococci,
Tablet, Co-trimoxazole 480 mg. Adverse effects: Nausea, vomiting, diarrhoea, 500 mg – 500. meningococci, etc.; infections susceptible to
Suspension, Co-trimoxazole 240 mg per 5 mL headache; hypersensitivity reactions including sulfonamides like bacillery dysentery, UTI.
Pack: 50 mL. rashes, pruritus, photosensitivity reactions, SULFAMETHOXAZOLE Contra-indications: Acute intermittent
exfoliative dermatitis, and erythema nodosum; Synonym: Sulphamethoxazole porphyria; sensitivity to other sulfonamides;
PHTHALYLSULFATHIAZOLE rarely, erythema multiforme (Stevens-Johnson Description: Sulfamethoxazole is a sulfon- infants under 6 months; pregnancy.
Therapeutic category: Antibacterial syndrome) and toxic epidermal necrolysis; sys- amide antibacterial. It inhibits synthesis of Precautions: Renal dysfunction; maintain
Pharmacology: A sulfonamide which is spar- temic lupus erythematosus, myocarditis, serum dihydrofolic acid which is essential for survival slightly alkaline urine and high fluid intake.
ingly absorbed after oral administration; its sickness; crystalluria—resulting in haematuria, of bacteria cell. Development of bacterial re- Adverse effects: See under sulfathiazole.
bacteriostatic activity in the bowel is 2-4 times oliguria, anuria; blood disorders including sistance has limited its use as a single agent and Advice to patients: See also under Sulfadim-
as great as that of succinylsulfathiazole. granulocytopenia, agranulocytosis, aplastic is available mainly as a combination product idine.
Indications: Treatment of acute phase of anaemia, purpura—discontinue immediately; with Trimethoprim. Nursing action: See under Cotrimoxazole.
shigellosis (bacillary dysentery). also reported, liver damage, pancreatitis, anti- See also Sulfamethoxazole plus Trimethoprim Dose: Acute infections, Adult, initially 2 g;
Contra-indications: Acute intermittent por- biotic-associated colitis, eosinophilia, cough Dose: Susceptible infections, Adult, by mouth, then, 1 g 4-6 hourly daily.
phyria, sensitivity to other sulfonamides. and shortness of breath, pulmonary infiltrates, initially 2 g, then 1 g twice daily. For Child (up to 12 yrs), initially 1 g; then,
Dose: Adult, 1.5 g 3-4 times daily. aseptic meningitis, depression, convulsions, severe infections, 1 g 3 times daily. 0.5 g 4-6 hourly.
ataxia, tinnitus, vertigo, dizziness, hallucina- Administer on an empty stomach. Infants (6 mths – 1 yr), initially 0.5 g;
POM DIASTOP-HS® (Afrab-Chem)
Tablet, Phthalysulfathiazole 500 mg; cream yellowish tions, and electrolyte disturbances. then, 0.25 g 4-6 hourly.
POM SULPHVIN® (Efunpo)
EMDEX
scored tab. marked ‘afrab’. Dose: Prevention of recurrences of rheumatic See lit. for details.
Tablet, Sulfamethoxazole 500 mg; white tab.
fever, by mouth, ADULT 1 g daily; 500 mg – 96’s; 1000’s POM NOVA-3-SULFA® (SKG)
POM Phthalysulfathiazole (Emzor)
Tablets, Phthalylsulfathiazole 500 mg. CHILD 500 mg daily. Tablets, Sulfathiazole 185 mg, sulfadiazine 185 mg,
500 mg – 1000. POM Sulfadiazine (WMF 6.2.2) SULFATHIAZOLE sulfamerazine 130 mg; white tab. marked ‘SKG’ on
Tablet, Sulfadiazine 500 mg. one side and ‘NOVA-3-SULFA’ on the reverse.
POM Phthalylsulfathiazole (Vitabiotics) Indications: Treatment of acute infections by Pack: 500’s.
Tablet, Phthalylsulfathiazole 500 mg. Injection, Sulfadiazine (as sodium salt) 250 mg in pneumococci, meningococci, beta-haemolytic
500 mg – 500. 4-mL ampoule. streptococci, E. coli; also bacillary dysentery, POM SULPHATRIAD® (May & Baker)
urinary tract infections; as an adjunct to treat- Tablets, Sulfathiazole 185 mg, sulfadiazine 185 mg,
POM TALIDINE® (SKG) SULFADIMIDINE sulfamerazine 130 mg.
Tablet, Phthalylsulphathiazole 500 mg; white scored ment with penicillin.
Indications: Treatment of acute infections Pack: 500’s.
tab. marked ‘TALIDINE’. Precautions: Renal dysfunction; maintain a
500 mg – 500’s in securitainer. caused by pneumococci, streptococci, staphylo- high fluid intake and a slightly alkaline urine to
cocci, gonorrhoea; also urinary tract infections TRIMETHOPRIM
prevent crystal deposition in the urinary tract.
POM THALAL® (Strides Vital) due to susceptible organisms, prophylactic Indications: Urinary-tract infections; bron-
Tablet, Phthalylsulfathiazole 500 mg. Adverse effects: Nausea, vomiting, mental
agent in meningo-coccal meningitis especially chitis.
500 mg – 100’s. changes, cyanosis, drug fever, drug rashes,
during epidemics. Contra-indications: Blood disorders; por-
blood dyscrasias, crystal deposition in the
POM THALAZOLE® (May & Baker) Contra-indications: Acute intermittent porphyria.
urinary tract.
Tablet, Phthalylsulfathiazole 500 mg; white scored phyria or sensitivity to other sulfonamides; Precautions: Renal impairment (avoid if se-
Advice to patients: See also under Sulfadim-
tab. marked ‘THALAZOLE’. pregnancy, infants under six weeks vere, Appendix 4); pregnancy (Appendix 2);
500 mg – 500’s. idine.
Precautions: Renal dysfunction. breastfeeding (Appendix 3); predisposition
Nursing action: See under Cotrimoxazole.
POM ZITRIM® (Chanmedi) Adverse effects: Nausea and vomiting, mental to folate deficiency; elderly; blood counts
Dose: Acute infections, Adult, initially 2 g;
Tablet, Sulfamethoxazole 400 mg, Trimethoprim changes, cyanosis, drug fever, drug rashes, on long-term therapy (but practical value
then, 1 g 4-6 hourly daily.
80 mg crystalluria. not proven); neonates (specialist supervision
480 mg – 10 x 10’s.
Child (up to 6 yrs), initially 1 g; then,
Advice to patients: Drink plenty of fluids; take required); interactions: Appendix 1.
0.5 g 4-6 hourly.
on an empty stomach; avoid prolonged expo- Adverse effects: Rashes, pruritus; depression
SULFADIAZINE Infants (6 mths-1 yr), initially 0.5 g;
sure to sunlight or wear protective clothing and of haematopoiesis; GI disturbances including
then 0.25 g 4-6 hourly.
Indications: Prevention of recurrences of sunscreen; notify physician if rash, difficulty in nausea and vomiting; hyperkalaemia; rarely
rheumatic fever; toxoplasmosis (section 9.3.5). POM BENTHIAZOLE® (Bentos) erythema multiforme and toxic epidermal
breathing, severe or persistent fever, or sore
Contra-indications: Hypersensitivity to sulfo- Tablet, Sulphathiazole 500 mg necrolysis, photosensitivity and other allergic
throat occurs. Dose: Bacillary dysentry, Adult, 1500 mg 3-4 times
namides; porphyria. Nursing action: See under Cotrimoxazole. reactions including angioedema and anaphy-
daily. Child (6-12 years): ½ adult dose; 3-5
Precautions: Hepatic impairment (avoid if Dose: Acute infections, Adult, initially 2 g; laxis; aseptic meningitis.
years, ¼ adult dose.
severe; Appendix 5); renal impairment (avoid then, 1 g 4-6 hourly. Dose: Acute infections, by mouth, ADULT
if severe; Appendix 4); maintain adequate fluid POM THIAZAMIDE® (May & Baker) 200 mg every 12 hours; CHILD 6
Child (up to 6 yrs), initially 1 g; then,
intake (to avoid crystalluria); avoid in blood Tablet, Sulfathiazole 500 mg; white scored tab. weeks–5 months, 25 mg twice daily;
0.5 g 4-6 hourly. marked ‘M & B 760’.
disorders (unless under specialist supervision); Infants (6 mths to 1 yr), initially 0.5 g; 6 months–5 years, 50 mg twice daily;
500 mg – 500’s.
monitor blood counts and discontinue imme- then, 0.25 g 4-6 hourly. 6–12 years, 100 mg twice daily.
diately if blood disorder develops; rashes—dis- Acute infections, by slow IV injection
continue immediately; predisposition to folate POM Sulfadimidine (Emzor)
or by IV infusion, ADULT 200 mg
404 | 9.1.2.10 Lincosamides 9.1.2.10 Lincosamides | 405
every 12 hours; CHILD under 12 years, 1) Greenwood D. Lincosamides. In: Finch ADULT 150–300 mg every 6 hours; Capsule, Clindamycin HCl 150 mg.
8 mg/kg daily in 2–3 divided doses. RG, Greenwood D, Norrby SR, Whitley RJ, up to 450 mg every 6 hours in severe 150 mg – 10’s; 16’s.
Chronic infections and prophylaxis, eds. Antibiotic and chemotherapy. 9th infections; CHILD 3–6 mg/kg every 6 Injection, Clindamycin (as phosphate) 150 m per mL;
by mouth, ADULT 100 mg at night; ed. Available from: www.clinicalkey.com hours; by deep IM injection or by IV in 2 mL ampoule.
CHILD 1–2 mg/kg at night. (login required) infusion, ADULT 0.6–2.7 g daily in 2–4
LINCOMYCIN
POM Trimethoprim (WMF 6.2.2)
divided doses, increased up to 4.8 g
CLINDAMYCIN daily in life-threatening infections; Indications: Severe infections due to suscep-
Tablets, Trimethoprim 100 mg, 200 mg.
Indications: Staphylococcal bone and joint single doses over 600 mg by IV infu- tible microorganisms: bone and connective
infections, pyomyositis; necrotizing fasciitis; sion only; single doses by IV infusion tssue infections, respiratory tract infections,
9.1.2.10 Lincosamides urogenital infections, skin and soft tissue
peritonitis; endocarditis prophylaxis; pelvic not to exceed 1.2 g; NEONATES 15–20
Clindamycin is a semisynthetic derivative of mg/kg daily; CHILD over 1 month, infections.
inflammatory disease (with gentamicin);
lincomycin. It is a bacteriostatic antibacterial 15–40 mg/kg daily in 3–4 divided Contra-indications: Hypersensitivity to linco-
pneumonia.
with activity against Gram-positive aerobes doses; severe infections, at least 300 mycin or clindamycin, moiliasis, severe liver or
Contra-indications: Diarrhoeal states; avoid
and a wide range of anaerobes. Aqueous sus- mg daily, regardless of weight. kidney damage.
injections containing benzyl alcohol in neo-
pensions are stable for up to 2 weeks at room Pelvic inflammatory disease, by IV infu- Precautions: GI diseases esp. colitis; asthma;
nates; porphyria
temperature. Capsules contain clindamycin sion, ADULT 900 mg every 8 hours. history of allergies; newborn, pregnancy; peri-
Precautions: Discontinue immediately if diar-
hydrochloride, which has a very bitter taste; Endocarditis prophylaxis (for proce- odic LFT and blood counts – during prolonged
rhoea or colitis develop; hepatic impairment
the syrup contains a suspension of the ester, dures under local or no anaesthetic), by therapy. See also under Clindamycin.
(Appendix 5); renal impairment (Appendix 4);
clindamycin palmitate, which is palatable for mouth, ADULT 600 mg, 1 hour before Adverse effects: See under Clindamycin.
monitor liver and renal function on prolonged
children. Clindamycin phosphate, which is procedure. Advice to patients: See also under Clindamycin.
therapy and in neonates and infants; elderly;
more soluble at neutral pH and less irritating Endocarditis prophylaxis (for proce- Nursing action: See under Clindamycin.
females; pregnancy (Appendix 2); breastfeed-
EMDEX
than the hydrochloride, is used parenterally. dures under general anaesthetic), by IV Dose: By mouth, Adult and child >14 years,
ing (Appendix 3); avoid rapid IV administration;
The palmitate and phosphate salts are inactive infusion, ADULT 300 mg over at least 500 mg 3-4 times daily, depending on
in vitro and must be hydrolyzed to liberate 10 minutes, at induction or 15 min- the severity of the infection.
Adverse effects: Diarrhoea (discontinue
clindamycin. utes before procedure, then 150 mg 6 Child (>1month), 30 mg/kg daily in
treatment); nausea, vomiting, abdominal dis-
Oral absorption is not depressed or delayed by hours later by mouth or infusion. 3-4 divided doses; increased to 60
comfort, oesophagitis, antibiotic-associated
food. The palmitate is rapidly and completely mg/kg daily in 3-4 divided doses in
colitis; rashes, pruritus, urticaria, and rarely POM Clindamycin (WMF 6.2.2)
hydrolyzed in the gut. In contrast, clindamycin more serious infections.
anaphylaxis; Stevens-Johnson syndrome, exfo- Capsule, Clindamycin 150 mg.
phosphate is absorbed intact after intramuscu- By IM injection, 600 mg 12-24 hourly.
liative and vesiculobullous dermatitis; jaundice Injection, Clindamycin (as phosphate) 150 mg/mL.
lar injection and relatively slowly hydrolyzed by Child (>1 month), 10 mg/kg 12-24
and altered liver function tests; neutropenia,
alkaline phosphatases. POM Clindamycin (EDL 5.3) hourly.
eosinophilia, agranulocytosis, and thrombocy- Capsule, Clindamycin (as HCl) 150 mg.
Clinical use is limited because of adverse By IV infusion (over 1 hour), 600 mg
topenia; pain, induration, and abscess after IM Injection, Clindamycin (as phosphate) 150 mg/mL.
effects. Antibiotic-associated colitis can occur 2-3 times daily diluted in 250 mL of
injection; thrombophlebitis after IV injection.
with a wide range of antibacterials, but occurs POM CLAMYCEF® (Korlyns) saline or glucose solution.
Advice to patients: Report any severe diar-
most frequently with clindamycin. It may be Capsule, Clindamycin HCl 150 mg; pink /chocolate Child (>1 month), 10-20 mg/kg daily
rhoea immediately and do not take antidiar- coloured cap.
fatal and is most common in women and the in 2-3 divided doses.
rheal medication; take each oral dose with a 150 mg – 10 x 10’s.
elderly; it can develop during or after treat- Max. daily dose is 8 g
full glass of water; finish all medication; do
ment with clindamycin. Patients should dis- POM CLAMYSOL® (Korlyns) Not recommended for children <1
not skip doses.
continue treatment immediately if diarrhoea Capsules, Clindamycin HCl 150 mg, 300 mg; red caps. month
Nursing action: Obtain specimen for C&S tests
develops. Clindamycin is recommended for 150 mg – 10’s (in blisters) Note: Lincomycin should not injected IV as a bo-
before first dose; therapy may begin pending 300 mg – 1 x 10’s.
the treatment of staphylococcal bone and joint lus. Intravenous doses are given on the basis of 1
test results. Injection, Clindamycin (as phosphate) 150 mg per mg of lincocin diluted in not less than 100 mL of
infections and for intra-abdominal sepsis. It is • Administer oral dosage form with a full glass of
also used for endocarditis prophylaxis when a mL; in 2 mL & 4 mL amps. appropriate solution and infused over a period of
water; may give with food to minimize GI irritation. Pack: 2 mL x 5’s; 4 mL x 5’s. not less than one hour. Severe cardiopulmonary
penicillin is not appropriate. • Reconstituted oral suspension is stable for 2 weeks reactions have occurred when this drug has been
at room temperature; it should not be refrigerated, POM CLEMARIN® Plus (Teta)
Lincomycin has antibacterial activity similar to given at greater than the recommended concen-
as it will thicken. Vaginal tablet, Clindamycin (as phosphate) 100 mg,
that of clindamycin but generally less potent. miconazole nitrate 100 mg
tration and rate.
• Give around-the-clock in equal intervals to pro-
It is less well absorbed than clindamycin. Food Pack: 1 x 6’s (in a carton with an applicator) POM BIOCINE® (Drugfield)
mote less variation in peak and trough serum
significantly delays and decreases absorption, levels. Capsule, Lincomycin (as HCI) 500 mg
the mean peak plasma level from a dose given POM CLIMYCIN® (Taylek)
• Administer deep IM injection and rotate sites. 500 mg – 2 x 10’s
Capsule, Clindamycin HCl 150 mg
immediately after a meal being only about half • Give IV by infusion only; observe daily for phlebitis Syrup, Lincomycin (as HCI) 250 mg per 5 mL
Injection, Clindamycin (as phosphate) 150 mg per
the fasting levels. and vein irritation during IV therapy. mL; in 2 mL amp.
250 mg – 100 mL
Nausea, vomiting and abdominal cramps may • Discontinue drug and notify physician immediately Injection, Lincomycin HCI 300 mg per mL; in 2 mL
occur. Diarrhea affects at least 10% of patients, if persistent diarrhoea and severe abdominal POM Clindamycin (Zolon) vials
usually within a few days of oral or parenteral cramps develop; these may be symptoms of Capsule, Clindamycin HCI equiv. to Clindamycin 150 Pack: 2 mL amp
pseudomembranous colitis which may end fatally. mg, 300 mg; hard gelatin cap.
administration. It is more common in older POM CIKALINCO® (Michelle Lab)
• Observe for symptoms of superinfection namely 150 mg – 10’s (in blisters)
patients and uncommon in children. Capsule, Lincomycin (as HCI) 500 mg
fever, sore throat, fatigue. 300 mg – 10’s (in blisters)
500 mg – 10’s; 12’s (in blisters)
References: Dose: Osteomyelitis or peritonitis, by mouth, POM DALACIN C® (Pfizer)
406 | 9.1.2.11 Vancomycin 9.1.2.12 Furazolidone | 407
POM KIPOCIN® (Vixa) causes pain and necrosis and is not used. hours; ELDERLY (over 65 years), 500 Administer with food; avoid
Capsule, Lincomycin 500 mg Slow IV infusion over at least 100 min is rec- mg every 12 hours or 1 g once daily; tyramine-containing foods such as
500 mg – 3 x 4’s ommended. Dosage should be adjusted to NEONATE up to 1 week, 15 mg/kg in- cheese, yoghurt.
POM LICOGEN® (Geneith) give a peak concentration of 25–40 mg/L and itially, then 10 mg/kg every 12 hours, POM UPFURAN® (Award Global)
Capsule, Lincomycin 500 mg. a trough of 5–10 mg/L. 1–4 weeks, 15 mg/kg initially, then 10 Capsule, Furazolidone 100 mg
POM LIFCOCIN® (Jubilee) Indicated for systemic infections which cannot mg/kg every 8 hours; CHILD over 1 100 mg – 10’s (in blisters)
Capsule, Lincomycin (as HCl monohydrate) 500 mg. be treated with other effective, less toxic anti- month, 10 mg/kg every 6 hours.
POM UREX® (Geneith)
500 mg – 12’s. microbials. It is used to treat serious infections Antibiotic-associated colitis, by mouth,
Capsule, Furazolidine 100 mg
Injection, Lincomycin (as HCl monohydrate) 300 mg due to Gram-positive cocci including meticil- ADULT 125–500 mg every 6 hours for 100 mg – 10 x 1 x 10
per mL; in 1 mL & 2 mL vials. lin-resistant staphylococcal infections, brain 7–10 days; CHILD 1 month–5 years
POM LINCOCIN® (Pfizer) abscess, meningitis and septicaemia. 5 mg/kg every 6 hours; over 5 years 9.1.3 Antileprosy drugs
Capsule, Lincomycin (as HCl) 500 mg 62.5 mg every 6 hours.
Vancomycin is potentially nephrotoxic and Note: Injection can be used to prepare solution for Leprosy is a chronic mycobacterial infection
500 mg – 12’s; 100’s
Syrup, Lincomycin 250 mg per 5 mL
ototoxic, and the risk can be potentiated by oral administration. due to Mycobacterium leprae, which is a
Pack: 60 mL prolonged treatment (>3 weeks), and concur- Endocarditis prophylaxis (for proce- slow-growing intracellular bacillus that infil-
Injection, Lincomycin (as HCl) 300 mg per mL; in rent therapy with an aminoglycoside or a loop dures under general anaesthetic), by trates the skin, peripheral nerves, the nasal and
2 mL vial. diuretic e.g. Furosemide. IV infusion, ADULT 1 g over at least other mucosa, and the eyes; it affects people of
References: 100 minutes then gentamicin 120 all ages and both sexes. The incubation period
POM LINCOLECIN® (Pharmabox)
Capsule, (250 mg), Lincomycin (as HCl) 250 mg; dark 1) Woodford N. Glycopeptides. In: Finch mg at induction or 15 minutes before between infection and appearance of leprosy
blue/light blue cap. filled with white powder. RG, Greenwood D, Norrby SR, Whitley RJ, procedure. is normally between 2 to 10 years, but may
250 mg – 10’s; 100’s; 500’s; 1000’s. eds. Antibiotic and chemotherapy. 9th Note: Plasma concentration monitoring required; be up to 20 years. It is transmitted from per-
EMDEX
Capsule, (500 mg), Lincomycin (as HCl) 500 mg; dark ed. Available from: www.clinicalkey.com peak plasma concentration (measured 2 hours after son-to-person when bacilli are shed from the
blue/light blue cap. filled with white powder. infusion) should not exceed 30 mg/litre; pre-dose nose; most individuals have natural immunity
(login required)
500 mg – 10’s; 100’s; 500’s; 1000’s. (trough) concentration should not exceed 5–10 mg/ and symptoms are suppressed. For treatment
litre (10–15 mg/litre in endocarditis).
POM Lincomycin (Al-Tinez) VANCOMYCIN purposes patients may be classified as having
Capsule, Lincomycin 500 mg Indications: Meticillin-resistant staphylococcal
POM Vancomycin (WMF 6.2.2) paucibacillary (PB) or multibacillary (MB)
500 mg – 10 x 10’s (in blisters) Powder for injection, Vancomycin (as HCl) 250 mg; leprosy. The 2 forms may be distinguished
pneumonia; septicaemia related to vascular in vial.
POM Lincomycin (Greenlife) catheter; meningitis; antibiotic-associated coli- by skin smears, but facilities are not always
Capsule, Lincomycin HCl 500 mg. tis; endocarditis prophylaxis (with gentamicin). POM CELOVAN® (Strides Vital) available to process them and their reliability
500 mg – 10’s. Precautions: Avoid rapid infusion (risk of Injection, Vancomycin 500 mg. is often doubtful. In practice, most leprosy
anaphylactoid reactions, see Adverse effects);
Pack: 1 g vial. programmes classify and choose a regimen
POM Lincomycin (Hochiez)
rotate infusion sites; renal impairment (Ap- POM VANZAR® (Shrezar) based on number of skin lesions; these are PB
Capsule, Lincomycin (as HCI) 500 mg
pendix 4); elderly; history of deafness—avoid; Injection, Vancomycin (as HCl) 500 mg per vial leprosy (1–5 skin lesions) and MB leprosy (more
POM Lincomycin (Neros) Pack: 1 vial than 5 skin lesions).
Capsule, Lincomycin 500 mg. plasma-vancomycin concentration measured
500 mg – 1 x 10’s; 10 x 10’s (in blisters). after 3 or 4 doses (earlier if renal impairment), Medicines used in the treatment of leprosy
blood counts, urinalysis, and renal function 9.1.2.12 Furazolidone should always be used in combination; this is
POM NELOREN® (Taylek) essential to prevent the emergence of resist-
tests—use only in hospital setting; monitor
Capsule, Lincomycin HCl 500 mg. FURAZOLIDONE
auditory function and plasma-vancomycin ance. Rifampicin is now combined with dap-
500 mg – 12; 16; 100.
concentrations in elderly or in renal impair- Synonym: Furazolidine. sone to treat PB leprosy and rifampicin and
Injection, Lincomycin HCl 300 mg per mL; in 2 mL
amp. ment; pregnancy (Appendix 2); breastfeeding Therapeutic category: Anti-infective; Anti- clofazimine are now combined with dapsone
Pack: 10’s. (Appendix 3); interactions: Appendix 1. septic. to treat MB leprosy. The WHO Programme for
Adverse effects: Nephrotoxicity including Indications: Treatment of bacterial or proto- the Elimination of Leprosy currently provides,
POM PEMCOCIN® (Pemason)
renal failure and interstitial nephritis; ototox- zoal diarrhoea and enteritis caused by suscep- free of charge, oral multidrug therapy in col-
Capsule, Lincomycin HCl 500 mg
icity (discontinue if tinnitus occurs); blood tible organisms. our-coded blister packs (MDT blister packs)
disorders; nausea, chills, fever, eosinophilia, Contra-indications: Hypersensitivity; infants to improve patients’ adherence to treatment.
9.1.2.11 Vancomycin
anaphylaxis, rashes, including exfoliative der- (<1 month). Avoid combination with alcohol Any patient with a positive skin smear should
Vancomycin is a tricyclic glycopeptide avail- matitis, erythema multiforme (Stevens-John- (disulfiram-like reaction). Potential hyperten- be treated with the oral multidrug therapy
able as the water-soluble hydrochloride for son syndrome), toxic epidermal necrolysis, sive crisis with MAO inhibitors; Sympathomi- (MDT) regimen for MB leprosy. The regimen for
intravenous infusion or oral administration. and vasculitis; phlebitis; on rapid infusion, metics including nasal decongestants. PB leprosy should never be given to a patient
Antibacterial activity is limited to Gram-pos- severe hypotension (with shock, cardiac arrest), Precautions: Avoid alcoholic beverages dur- with MB leprosy. If diagnosis classification in
itive species, including methicillin-resistant wheezing, dyspnoea, urticaria, pruritus, flushing or within 4 days after therapy. Pregnancy, a particular patient is not possible the MDT
strains of staphylococci (MRSA). ing of the upper body (‘red man’ syndrome), lactation. regimen for MB leprosy must be used.
It is very poorly absorbed from the GI tract and pain and muscle spasm of back and chest. Adverse effects: Hypersensitivity reactions; Lepra reactions are episodes of sudden
large concentrations of unaltered drug are Dose: Serious staphylococcal infections, by nausea, vomiting, headache, malaise, orthos- increase in the activity of leprosy and are
found in the feces after oral administration. IV infusion, ADULT 500 mg over at tatic hypotension, dizziness, drowsiness, rash; often accompanied by neuritis; reactions
Rapid infusion (<1 h) or bolus administration least 60 minutes every 6 hours or 1 disulfiram-like reaction with alcohol. must always be treated promptly to prevent
is dangerous. The IM route of administration g over at least 100 minutes every 12 Dose: Adult, 100 mg 4 times daily usually for permanent nerve damage and disability.
2-5 days; 10 days for giardiasis.
408 | 9.1.3 Antileprosy drugs 9.1.3 Antileprosy drugs | 409
Leprosy multidrug therapy should continue months for MB leprosy. mg once daily and 300 mg once a reduced or treatment discontinued temporarily
during a lepra reaction without interruption. For patients who cannot take rifampicin month; CHILD 10–14 years 50 mg if low levels of Hb, WBC or RBC are obtained.
This reduces the frequency and severity of on alternate days and 150 mg once • Withhold therapy if rash develops and report to
because of allergy, other diseases, or rifampic-
lepra reactions. a month; CHILD under 10 years, see the physician; antihistamines may be prescribed
in-resistant leprosy, and for patients who for dapsone-induced allergic dermatitis.
Type 1 lepra reactions, or reversal reactions, refuse to take clofazimine, there are alternative notes above; continue treatment for
• Persistent sore throat, fever, malaise or fatigue
are delayed hypersensitivity reactions and may regimens which incorporate ofloxacin and 12 months.
should be reported to the physician.
occur in either PB or MB leprosy. If there is no minocycline [not included on WHO Model List]. Type 2 lepra reaction (erythema • Nursing mothers should be advised to report
nerve damage, type 1 reactions may be treated nodosum leprosum), by mouth, ADULT cyanosis in infants as this may indicate high
with analgesics such as acetylsalicylic acid or CLOFAZIMINE and CHILD 200–300 mg daily in 2 or sulphone level.
paracetamol. If there is nerve involvement cor- 3 divided doses for maximum of 3 Dose: Paucibacillary leprosy (in combination
Therapeutic category: Antibiotic; Leprostatic
ticosteroids, such as oral prednisolone should months; 4–6 weeks treatment may be with rifampicin, see notes above), by
agent.
be used in addition to analgesics. required before effect is seen. mouth, ADULT 100 mg daily; CHILD
Indications: Multibacillary (MB) leprosy; type
2 lepra reactions. POM Clofazimine (WMF 6.2.3) under 10 years, see notes above;
The type 2 lepra reaction, also known as ery-
Precautions: Pre-existing GI symptoms Capsules, Clofazimine 50 mg, 100 mg. 10–14 years 50 mg daily; continue
thema nodosum leprosum (ENL), is an antibody
(reduce dose, increase dose interval or dis- treatment for 6 months.
response to dead leprosy bacteria and occurs POM Clofazimine (EDL 5.6)
continue if symptoms develop during treat- Capsules, Clofazimine 50 mg, 100 mg. Multibacillary leprosy (in combination
only in MB leprosy. Therapy for type 2 reactions
ment); liver and renal impairment; pregnancy; with rifampicin and clofazimine, see
may include analgesics, such as acetylsalicylic
breastfeeding (Appendix 3); may discolour soft DAPSONE notes above), ADULT 100 mg daily;
acid or paracetamol, and a corticosteroid, such
contact lenses. CHILD under 10 years, see notes
as oral prednisolone. In patients not respond- Synonym: Diaminodiphenylsulphone; DSS.
Adverse effects: Reversible discoloration of above; 10–14 years 50 mg daily; con-
ing to a corticosteroid, clofazimine may be Therapeutic category: Antibiotic; Leprostatic
skin, hair, cornea, conjunctiva, tears, sweat, tinue treatment for 12 months.
EMDEX
used. Severe type 2 lepra reactions should be Agent.
treated under medical supervision in hospital. sputum, faeces, and urine; dose-related GI Pharmacology: Dapsone is a sulphone bac- POM Dapsone (WMF 6.2.3)
symptoms including pain, nausea, vomiting, teriostatic with mechanism of action similar Tablets, Dapsone 25 mg, 50 mg, 100 mg.
If a patient does not respond to lepra reaction
diarrhoea, weight loss, GI bleeding; severe to that of the sulfonamides. It inhibits folic POM Dapsone (EDL 5.6)
treatment within 6 weeks or seems to become
mucosal and submucosal oedema, with pro- acid biosynthesis in susceptible organisms. Tablets, Dapsone 50 mg, 100 mg.
worse, the patient must be sent immediately to
longed treatment with high doses—may be See notes above.
the nearest specialist centre. Neuritis may occur
severe enough to cause subacute small-bowel Indications: Paucibacillary (PB) and multibac- RIFAMPICIN
during or independently of lepra reactions. It
obstruction (see also Precautions); dry skin, illary (MB) leprosy. Indications: Paucibacillary leprosy; multi-
can be successfully treated with a 12-week
acne-like eruptions, rashes, pruritus, photo- Contra-indications: Hypersensitivity to sul- bacillary leprosy; meningitis; tuberculosis
course of oral prednisolone; if patients do
sensitivity, decreased sweat production; dry fones; severe anaemia. (section 9.1.4)
not respond, specialist centre treatment is
eyes; rarely headache, drowsiness, dizziness, Precautions: Anaemia (treat severe anaemia Contra-indications: Hypersensitivity to rifa-
required.
taste disorders, elevation of blood-glucose before therapy, and monitor blood counts mycins; jaundice.
TREATMENT REGIMENS concentration. during treatment); susceptibility to haemolysis Precautions: Reduce dose in hepatic im-
The recommended regimen for pauciba-cillary Advice to patients: Drug may cause a red including G6PD deficiency (including breast- pairment (Appendix 5); liver function tests
leprosy in adults (50–70 kg) is rifampicin 600 to brownish-black discolouration of the skin, feeding affected infants); pregnancy (Appendix and blood counts required in liver disorders,
mg once monthly and dapsone 100 mg daily. conjunctiva, tears, sweat, urine, faeces, and 2); breastfeeding (Appendix 3); porphyria; alcohol dependency, elderly, and on prolonged
Children aged 10–14 years may be given ri- nasal secretions; although reversible, may take interactions: Appendix 1. therapy; renal impairment (if dose above 600
fampicin 450 mg once monthly and dapsone months to years to disappear after therapy is mg daily); pregnancy (Appendix 2); breastfeed-
BLOOD DISORDERS: On long-term treatment
50 mg daily. Appropriate dose adjustments are completed; take with meals; dry skin can be ing (Appendix 3); porphyria; discolours soft
patients and their carers should be told how
required for younger children. For example, relieved with skin oil or cream. contact lenses; important: advise patients on
to recognize blood disorders and advised to
dapsone 25 mg daily and rifampicin 300 mg Nursing action: Advise patient to take the oral contraceptives to use additional means;
seek immediate medical attention if symptoms
once a month. Treatment is continued for 6 drug with meals. interactions: Appendix 1.
• If patient complains of colicky or burning abdom- such as fever, sore throat, rash, mouth ulcers,
months for PB leprosy. purpura, bruising or bleeding develop. NOTE: Resumption of rifampicin treatment
inal pain or any other GI symptoms, report this to
The recommended regimen for multiba-cillary the doctor, who may reduce the dose or increase Adverse effects: Haemolysis and methae- after a long interval may cause serious im-
(MB) leprosy in adults (50–70 kg) is rifampicin the interval between doses. moglobinaemia; allergic dermatitis (rarely munological reactions, resulting in renal
600 mg and clofazimine 300 mg, both given • Use cautiously in GI dysfunction, such as abdomi- including toxic epidermal necrolysis and the impairment, haemolysis, or thrombocyto-
once a month together with clofazimine 50 nal pain and diarrhoea. Stevens-Johnson syndrome); rarely, hepatitis penia—discontinue permanently if serious
mg and dapsone 100 mg, both daily. Children • Warn patient that clofazimine may cause a red and agranulocytosis; ‘dapsone syndrome’ adverse effects occur.
aged 10–14 years may be given rifampicin to brownish-black discolouration of skin, body resembling mononucleosis—rare hypersen- LIVER DISORDERS: Patients or their carers
fluids, and excrement. Reassure patient that the should be told how to recognize signs of liver
450 mg and clofazimine 150 mg, both once sitivity reaction with symptoms including
unsightly skin discolouration is reversible but may
a month together with clofazimine 50 mg rash, fever, jaundice, and eosinophilia; gas- disorders and advised to discontinue treat-
not disappear until several months or years after
every other day and dapsone 50 mg daily. therapy is completed. trointestinal irritation; tachycardia, headache, ment and seek immediate medical attention if
Appropriate dosage adjustments are required • Recommend application of skin oil or cream to help nervousness, insomnia, blurred vision, paraes- symptoms such as persistent nausea, vomiting,
for younger children. For example, dapsone reverse skin dryness or ichthyosis. thesia, reversible peripheral neuropathy, and malaise or jaundice develop.
25 mg daily, clofazimine 50 mg twice a week, Dose: Multibacillary leprosy (in combination psychoses reported. Adverse effects: Severe GI disturbances
and clofazimine 100 mg and rifampicin 300 mg with dapsone and rifampicin, see Nursing action: Frequent blood tests are including anorexia, nausea, vomiting, and
once a month. Treatment is continued for 12 notes above), by mouth, ADULT 50 required during early therapy; dosage may be diarrhoea (antibiotic-associated colitis re-
410 | 9.1.4 Antituberculosis drugs 9.1.4 Antituberculosis drugs | 411
ported); headache, drowsiness; rashes, fever, organisms may produce disease and this often Unsupervised and alternative regimens as set CAPREOMYCIN
influenza-like syndrome and respiratory symp- occurs if immune status is altered. out in the following tables may be adminis-
Capreomycin is a complementary list medi-
toms, collapse, shock, haemolytic anaemia, Tuberculosis is the most prevalent infectious tered as specified.
cine for the treatment of multidrug-resistant
acute renal failure, and thrombocytopenic disease of adults and causes 26% of avoidable Additional reserve antituberculosis drugs (ami- tuberculosis which should be used in special-
purpura—more frequent with intermittent adult deaths in the developing world. More kacin, p-aminosalicylic acid, capreo-mycin, ized centres adhering to WHO standards for
therapy; alterations of liver function—jaundice than 80% of tuberculosis cases are pulmonary cycloserine, ethionamide, kanamycin, tuberculosis control.
and potentially fatal hepatitis (doserelated; do (PTB). At least 30% of patients who are infected levofloxacin, or ofloxacin) for the treatment
not exceed maximum daily dose of 600 mg); POM Capreomycin (WMF 6.2.4)
with HIV will also develop active tuberculosis. of multidrug-resistant tuberculosis should be
also reported, oedema, muscular weakness Powder for injection, Capreomycin 1000 mg; in vial.
The increase in resistant strains and poor com- used in specialized centres adhering to WHO
and myopathy, exfoliative dermatitis, toxic pliance which may contribute to resistance and standards for TB control.
epidermal necrolysis, pemphigoid reactions, CYCLOSERINE
treatment failure has led to the development of PROPHYLAXIS
leukopenia, eosinophilia and menstrual dis- regimens with directly supervised treatment. Cycloserine is a complementary list medicine
turbances; urine, tears, saliva, and sputum Directly observed treatment, short-course Worldwide, an important predisposing cause for the treatment of multidrug-resistant
coloured orange-red. (DOTS) therapy which lasts for 6 or 8 months, of immunosuppression leading to tubercu- tuberculosis which should be used in special-
Advice to patients: Take dose at least 30 min- given under direct observation is one of the losis is human immunodeficiency virus (HIV) ized centres adhering to WHO standards for
utes before a meal, since absorption is reduced most important components of the WHO infection; it increases susceptibility to primary tuberculosis control.
by food. May discolour urine, tears, sweat, or strategy against tuberculosis. infection and increases the reactivation rate
of tuberculosis. Preventative antituberculosis POM Cycloserine (WMF 6.2.4)
other body fluids to a red-orange colour; soft
Simplified drug regimens and intermittent Capsule or tablet, Cycloserine 250 mg.
contact lenses may be permanently stained; therapy of such persons is recommended.
report to physician any severe or persistent therapy have been introduced to improve com-
pliance. WHO does not generally recommend Chemoprophylaxis with isoniazid can prevent ETHAMBUTOL
flu-like symptoms, nausea, vomiting, dark urine the development of clinically apparent disease
EMDEX
or pale stools, or unusual bleeding or bruising. twice weekly regimens. If a patient receiving a Indications: Tuberculosis, in combination with
twice weekly regimen misses a dose of tablets, in persons in close contact with infectious other drugs (see notes and tables above).
Dose: Paucibacillary leprosy (in combination patients, and also prevent the reactivation of
with dapsone; see notes above), by the missed dose represents a bigger fraction of Contra-indications: Optic neuritis; children
the total number of treatment doses than if the previously dormant disease in other persons under 5 years—unable to report symptomatic
mouth, ADULT 600 mg once a month; at high risk particularly those who are immu-
CHILD under 10 years, see notes patient was receiving a three times weekly or visual disturbances; severe renal impairment.
daily dose regimen. Therefore, there is a greater nodeficient. Precautions: Visual disturbances—ocular
above; 10–14 years 450 mg once
a month; continue treatment for 6 risk of treatment failure with twice weekly Where the disease remains highly prevalent examination recommended before and dur-
months. regimens. Fixed-dose combination tablets routine immunization of infants within the first ing treatment (see note below); reduce dose
Multibacillary leprosy (in combination incorporating 2 or more drugs are also used year of age with BCG vaccine is cost-effective. in renal impairment (Appendix 4)—monitor
with dapsone and clofazimine; see to improve compliance and decrease medica- However, there is no evidence that BCG will plasma ethambutol concentration if creatinine
notes above), by mouth, ADULT 600 tion errors; they should be used unless one of protect children older than 15 years of age. clearance less than 30 mL/minute; elderly;
mg once a month under supervision; the components cannot be given because of Infants born to HIV-positive mothers should be pregnancy (not known to be harmful); breast-
CHILD under 10 years, see notes resistance or intolerance. vaccinated during the first year of life, provided feeding (Appendix 3).
above; 10–14 years 450 mg once a The modern short-course therapy is usually in they have no clinical signs suggestive of HIV. NOTE: Patients should report visual distur-
month under supervision; continue 2 phases. The initial phase (2 months) involves DIAGNOSIS bances immediately and discontinue treat-
treatment for 12 months. the concurrent use of at least 3 drugs to reduce ment; children who are incapable of reporting
The tuberculin test has limited diagnostic symptomatic visual changes accurately should
POM Rifampicin (WMF 6.2.3)
the bacterial population rapidly and prevent value. A positive tuberculin test indicates
drug-resistant bacteria emerging. The second be given alternative therapy, as should, if
Capsules/Tablets, Rifampicin 150 mg, 300 mg. previous exposure to mycobacterial antigens possible, any patient who cannot understand
continuation phase (4–6 months) involves through infection with one of the tubercle
POM Rifampicin (EDL 5.6) fewer drugs and is used to eliminate any warnings about visual adverse effects.
Tablets/Capsules, Rifampicin 150 mg, 300 mg. bacilli, or BCG vaccination. The tuberculin test Adverse effects: Optic neuritis—reduced
remaining bacteria and prevent recurrence. does not distinguish between tuberculosis and
See section 9.1.4 for the proprietary preparations of Direct observation of therapy is considered visual acuity and red/green colour blindness
other mycobacterial infection, between active (early changes usually reversible, prompt
Rifampicin. essential to ensure compliance in the initial and quiescent disease, or between acquired withdrawal may prevent blindness); peripheral
phase and also useful in the continuation infection and seroconversion induced by BCG
phase if patients are receiving rifampicin. Five neuritis—especially in legs; gout; rarely, rash,
9.1.4 Antituberculosis drugs vaccination. pruritus, urticaria, thrombocytopenia.
antituberculosis drugs, isoniazid, rifampicin,
Tuberculosis is a chronic infectious disease pyrazinamide, streptomycin (which are bac- Advice to patients: Report any visual changes
caused primarily by Mycobacterium tuberculosis AMIKACIN
tericidal) and ethambutol (which is bacterio- or rash to physician; may cause stomach upset,
or sometimes M. bovis. Infection is usually static) are used in various combinations as part Amikacin is a complementary list medicine for take with food; do not take within 2 hours of
due to inhalation of infected droplet nuclei of WHO-recommended treatment regimens. In the treatment of multidrug-resistant tuber- aluminium-containing antacids.
with the lung generally being the first organ supervised regimens change of drug regimen culosis which should be used in specialized Nursing action: Obtain specimen for C&S test
affected, but the primary infection is usually should be considered only if the patient fails centres adhering to WHO standards for tuber- including sputum before treatment.
asymptomatic. Infection and inflammatory to respond after 5 months of DOTS. culosis control.. • Administer with meals to minimise GI upset; give
responses resolve with the development of antiemetic if vomiting occurs. Antacids should not
Isoniazid, rifampicin, and pyrazinamide are POM Amikacin (WMF 6.2.4) be used within 2 hr of medication.
acquired immunity. Surviving bacteria may Powder for injection, Amikacin 1000 mg; in vial.
become dormant or in susceptible patients, components of all antituberculosis drug • Emphasize the need to comply with dosage and
regimens currently recommended by WHO. appointments to prevent relapse; to avoid alco-
progress to active primary disease; dormant
holic beverages.
• Advise periodic visual testing before and during multiforme, purpura usually during first weeks HCl 800 mg and isoniazid 300 mg Dose: Tuberculosis, continuation phase of
therapy; reassure patient that visual disturbances of treatment; peripheral neuropathy; blood dis- daily. 8-month regimen (see notes and tables
will clear weeks to months after therapy. orders including agranulocytosis, haemolytic POM Isoniazid plus ethambutol (WMF 6.2.4)
above), by mouth, ADULT and CHILD
• Monitor regularly the serum uric acid and observe anaemia, aplastic anaemia; optic neuritis, toxic thioacetazone 2.5 mg/kg daily and
Tablets, Isoniazid 150 mg with ethambutol 400 mg
patient for symptoms of gout. isoniazid 5 mg/kg daily.
psychoses, and convulsions; hepatitis (espe-
Dose: Tuberculosis (as part of a 6- or 8-month
cially over age of 35 years and regular users of ISONIAZID plus THIOACETAZONE POM INAZONE-450® (Vitabiotics)
regimen; see notes and tables above),
alcohol)—withdraw treatment; also reported, Tablet, Isoniazid 300 mg, thioacetazone 150 mg.
by mouth, ADULT 15 mg/kg daily or Deleted from the current WHO Model Formulary.
systemic lupus erythematosus-like syndrome, Pack: 500’s.
30 mg/kg 3 times a week; CHILD 20 Indications: Tuberculosis, in combination with
pellagra, hyperreflexia, difficulty with mictu-
mg/kg daily or 30 mg/kg 3 times a other drugs (see notes and tables above). KANAMYCIN
rition, hyperglycaemia and gynaecomastia.
week. Contra-indications: See Isoniazid; hepatic
Nursing action: Obtain specimen for C&S test Kanamycin is a complementary list medicine
Note: ‘Peak’ concentration (2–2.5 hours after dose)
including sputum before treatment. impairment; renal impairment; HIV infection—
should be 2–6 mg/litre (7–22 micromol/litre); ‘trough’ for the treatment of multidrug-resistant
(pre-dose) concentration should be less than 1 mg/ • Advise patient to take with food if GI irritation thioacetazone associated with high incidence
tuberculosis which should be used in special-
litre (4 micromol/litre). occurs; better absorbed on an empty stomach. of serious, sometimes fatal cutaneous hy-
• Advise against use with alcohol as it may exacer- ized centres adhering to WHO standards for
persensitivity reactions, including exfoliative
POM Ethambutol (WMF 6.2.4) bate isoniazid-induced hepatitis. tuberculosis control.
dermatitis.
Tablets, Ethambutol (as HCl) 100-400 mg. • Pyridoxine may be given to prevent peripheral POM Kanamycin (WMF 6.2.4)
Precautions: See Isoniazid; determine efficacy
neuropathy, especially in malnourished patients. Powder for injection, Kanamycin 1000 mg; in vial.
POM Ethambutol (EDL 5.10) and toxicity of thioacetazone – geographical
• Emphasize the need to comply with dosage and
Tablets, Ethambutol (as HCl) 100-500 mg. differences; hypersensitivity reactions – with-
appointments to prevent relapse.
draw treatment; interactions: Appendix 1. OFLOXACIN
• Monitor hepatic function and notify doctor imme-
ETHIONAMIDE diately if symptoms of hepatic impairment occur Adverse effects: See Isoniazid; thioacetazone Ofloxacin (and levofloxacin) are complemen-
EMDEX
Ethionamide is a complementary list medi- namely fatigue, loss of appetite, nausea, dark urine, causes the following—nausea, vomiting, di- tary list medicines for the treatment of multi-
cine for the treatment of multidrug-resistant or yellowing of eyes. arrhoea; hypersensitivity reactions including drug-resistant tuberculosis which should be
tuberculosis which should be used in special- Dose: Tuberculosis, treatment (as part of a conjunctivitis, vertigo, rashes; fatal exfoliative used in specialized centres adhering to WHO
ized centres adhering to WHO standards for 6- or 8-month regimen; see notes and dermatitis, acute hepatic failure reported; standards for tuberculosis control.
tuberculosis control. tables above), by mouth, ADULT and also, agranulocytosis, thrombocytopenia and
CHILD 5 mg/kg (4–6 mg/kg) daily POM Ofloxacin (WMF 6.2.4)
aplastic anaemia.
POM Ethionamide (WMF 6.2.4) (maximum, 300 mg daily), or 10 mg/
Tablets, Ethionamide 125 mg, 250 mg. Recommended 6-month treatment regimens for tuberculosisa
kg 3 times weekly.
Tuberculosis, treatment in critically ill Medicine Initial phase (2 months) Continuation phase (4 months)
ISONIAZID
patients unable to take oral therapy Isoniazid 5 mg/kg daily 5 mg/kg daily
Synonym: Isonicotinic acid hydrazide; INH. (as part of a combination therapy), by + 10 mg/kg daily 10 mg/kg daily
Indications: Tuberculosis treatment, in combi- IM injection, ADULT 200–300 mg as Rifampicin 25 mg/kg daily
nation with other drugs (see notes and tables + 15 mg/kg daily
single daily dose; CHILD 10–20 mg/ Pyrazinamide 15 mg/kg dailyc
above); tuberculosis prophylaxis. kg daily. together with
Contra-indications: Drug-induced hepatic Tuberculosis, prophylaxis, by mouth, Streptomycinb
disease. ADULT 300 mg daily for at least or
Ethambutol
Precautions: Hepatic impairment (monitor 6 months; CHILD 5 mg/kg daily
hepatic function; Appendix 5); malnutrition, (maximum 300 mg daily) for at least Isoniazid 10 mg/kg 3 times weekly 10 mg/kg 3 times weekly
chronic alcohol dependence, chronic renal + 10 mg/kg 3 times weekly 10 mg/kg 3 times weekly
6 months. Rifampicin 35 mg/kg 3 times weekly
failure (Appendix 4), diabetes mellitus, and HIV + 15 mg/kg 3 times weekly
infection—prophylactic pyridoxine 10 mg daily POM Isoniazid (WMF 6.2.4)
Pyrazinamide 30 mg/kg 3 times weekly
Tablets, Isoniazid 100-300 mg. together with
required because risk of peripheral neuritis;
Tablet, (scored), Isoniazid 50 mg. Streptomycinb
epilepsy; slow acetylator status (increased or
risk of adverse effects); history of psychosis; POM Isonaizid (EDL 5.10) Ethambutol
pregnancy (not known to be harmful); breast- Tablets, Isonaizid 100-300 mg
Recommended 8-month treatment regimen for tuberculosisa
feeding (Appendix 3); porphyria; interactions:
Appendix 1. ISONIAZID plus ETHAMBUTOL Medicine Initial phase (2 months) Continuation phase (6 months)
LIVER DISORDERS: Patients or their carers Indications: Tuberculosis, in combination with Isoniazid 5 mg/kg daily 5 mg/kg daily
should be told how to recognize signs of liver other drugs (see notes and tables above). + 10 mg/kg daily
disorder, and advised to discontinue treat- Contra-indications: Preparation not suita- Rifampicin 25 mg/kg daily
+ 15 mg/kg daily
ment and seek immediate medical attention if ble for use in children; see Ethambutol and Pyrazinamide 15 mg/kg dailyc
symptoms such as nausea, vomiting, malaise Isoniazid. together with
or jaundice develop. Precautions: See Ethambutol and Isoniazid. Streptomycinb
Adverse effects: See Ethambutol and Isoniazid. or
Adverse effects: GI disorders including nausea Ethambutol 5 mg/kg daily
and vomiting, diarrhoea and pain, also consti- Dose: Tuberculosis, continuation phase of
8-month regimen (see notes and Unless otherwise indicated, doses are suitable for both adults and children.
a
pation, dry mouth; hyper-sensitivity reactions b
Streptomycin always replaces ethambutol in meningeal TB.
including fever, rashes, joint pain, erythema tables), by mouth, ADULT ethambutol c
Ethambutol 20 mg/kg recommended in children.
Tablets, Ofloxacin 200 mg, 400 mg. Adverse effects: Hepatotoxicity including 500 mg – 1000. POM MYCOBUTIN® (Alpha)
fever, anorexia, hepatomegaly, splenomeg- Capsule, Rifabutin 150 mg; opaque brown cap.
POM Pyrazinamide (Strides Vital)
P-AMINOSALICYLIC ACID aly, jaundice, liver failure; nausea, vomiting; containing red-violet powder.
Tablet, Pyrazinamide 500 mg.
flushing; dysuria; arthralgia; gout; sideroblastic 150 mg – 1 x 30’s.
p-aminosalicylic acid is a complementary list 500 mg – 1000’s.
medicine for the treatment of multidrugre- anaemia; rash, photosensitivity.
RIFAMPICIN
sistant tuberculosis which should be used in Nursing action: Obtain specimen for C&S test RIFABUTIN
including sputum before treatment. Synonym: Rifampin.
specialized centres adhering to WHO standards Therapeutic category: Antibiotic; Antituber-
• Administer with meals to minimise GI upset. Therapeutic category: Antibiotic; Antituber-
for tuberculosis control. culous agent.
• Emphasize the need to comply with dosage and culous agent.
Indications: Treatment of mycobacterial
POM P-aminosalicylic acid (WMF 6.2.4) appointments to prevent relapse; to avoid alco- Indications: Tuberculosis, in combination
holic beverages. infections such as Mycobactrium avium com-
Tablet, P-aminosalicylic acid 500 mg. with other drugs (see notes and tables above);
Granules, P-aminosalicylic acid 4 g; in sachet. • Dosage may be reduced in renal insufficiency as plex (MAC) especially in late-stage HIVS/AIDS;
leprosy (section 9.1.3); meningitis.
the drug is virtually excreted in urine. Pulmonary TB in combination regimen. Proph-
Contra-indications: Hypersensitivity to rifa-
PYRAZINAMIDE • Monitor hepatic function and blood uric acid ylaxis of MAC infections in immunosuppressed
mycins; jaundice.
before and during therapy. patients with CD4 count <75/microlitre.
Synonym: Pyrazinoic acid amide. • Notify physician immediately if signs of gout and Precautions: Reduce dose in hepatic im-
Precautions: Avoid use for MAC prophylaxis
Indications: Tuberculosis, in combination with of hepatic impairment occur namely fever, loss pairment (Appendix 5); liver function tests
in patients with active tuberculosis. Periodic
other drugs (see notes and tables above). of appetite, malaise, nausea, vomiting, darkened and blood counts required in liver disorders,
monitoring of WBC & platelet counts and
Contra-indications: Severe hepatic impair- urine, pale stools. alcohol dependency, elderly, and on prolonged
hepatic enzymes recommended (may cause
ment; porphyria. Dose: Tuberculosis (as part of a 6- or 8-month therapy; renal impairment (if dose above 600
neutropenia and rarely, thrombocytopenia).
Precautions: Hepatic impairment (monitor he- regimen; see notes and tables above), mg daily); pregnancy (Appendix 2); breast-
Severe renal impairment i.e. ClCr <30 mL/min
patic function; Appendix 5); renal impairment; by mouth, ADULT and CHILD 25 mg/ feeding (Appendix 3); porphyria; discolours
(reduce dose by 50%); severe hepatic dysfunc-
EMDEX
diabetes mellitus (monitor blood glucose— kg daily or 35 mg/kg 3 times weekly. soft contact lenses; important: advise patients
tion. Myositis, uveitis & bloody diarrhea with or
may change suddenly); gout; pregnancy on hormonal contraceptives to use additional
POM Pyrazinamide (WMF 6.2.4) without cramps (patient to notify physician);
(Appendix 2) and breastfeeding (Appendix 3). Tablet, Pyrazinamide 400 mg. means; interactions: Appendix 1.
Pregnancy, lactation, children.
LIVER DISORDERS: Patients or their carers Tablet, (dispersible), Pyrazinamide 150 mg NOTE: Resumption of rifampicin treatment
Interactions: May reduce the efficacy of OCs
should be told how to recognize signs of liver Tablet, (scored), Pyrazinamide 150 mg. after a long interval may cause serious im-
and other CYP3A substrates, e.g. itraconazole,
disorder, and advised to discontinue treat- munological reactions, resulting in renal
POM Pyrazinamide (EDL 5.10) clarithromycin, saquinavir. Coadministration
ment and seek immediate medical attention if Tablet, Pyrazinamide 400 mg. impairment, haemolysis, or thrombocytopenia
with fluconazole and clarithromycin may
symptoms such as persistent nausea, vomiting, – discontinue permanently if serious adverse
POM PYRAZIN® (Hovid) increase plasma levels of rifabutin.
malaise or jaundice develop. effects occur.
Tablet, Pyrazinamide 500 mg. Adverse effects:GI upset such as nausea,
TREATMENT REGIMENS BY CATEGORY OF TUBERCULOSIS DIAGNOSIS vomiting; increase of liver enzymes, jaundice; LIVER DISORDERS: Patients or their carers
leucopenia, thrombocytopenia and anemia should be told how to recognize signs of liver
Category I: New pulmonary disease (smear-positive or smear-negative with extensive involvement of parenchyma), disorders and advised to discontinue treat-
concomitant severe HIV disease, and new severe extra-pulmonary disease (co-administration with isoniazid increases
Initial phase1 (antibacterials administered daily or 3 times weekly2): frequency); arthralgia and myalgia, rarely my- ment and seek immediate medical attention if
Isoniazid + rifampicin + pyrazinamide + ethambutol (or streptomycin) for 2 months ositis or uveitis. Also fever, rash and rarely other symptoms such as persistent nausea, vomiting,
Continuation phase1 (antibacterials administered daily or 3 times weekly): malaise or jaundice develop.
Isoniazid + rifampicin for 4 months (or isoniazid + ethambutol for 6 months but less effective than isoniazid + rifampicin).
hypersensitivity reactions such as eosinophilia,
bronchospasm and shock might occur, as has Adverse effects: Severe GI disturbances
Category II: Previously treated smear-positive pulmonary disease which has relapsed, or failed3 to respond, or if been seen with other antibiotics. Skin discol- including anorexia, nausea, vomiting, and di-
treatment was interrupted
Initial phase1 (antibacterials administered daily or 3 times weekly): oration may occur. arrhoea (antibiotic-associated colitis reported);
Isoniazid + rifampicin + pyrazinamide + ethambutol + streptomycin for 2 months. Advice to patients: See under Rifampicin. headache, drowsiness; rashes, fever, influen-
then: Dose: Adult, as a single agent: Prophylaxis za-like syndrome and respiratory symptoms,
Isoniazid + rifampicin + pyrazinamide + ethambutol for 1 month. collapse, shock, haemolytic anaemia, acute
Continuation phase1 (antibacterials administered daily or 3 times weekly):
of MAC infection in immunodepressed
Isoniazid + rifampicin + ethambutol for 5 months. patients, 300 mg once daily; may give renal failure, and thrombocytopenic purpura—
as 150 mg twice daily with food if more frequent with intermittent therapy;
Category III: New smear-negative pulmonary disease (other than in Category I) and less severe extra-pulmonary
disease nausea, vomiting or other GI upset alterations of liver function—jaundice and po-
Initial phase1 (antibacterials administered daily or 3 times weekly2): isoniazid + rifampicin + pyrazinamide + ethambutol4 occurs. tentially fatal hepatitis (dose related; do not ex-
for 2 months. In combination regimens: Non-tu- ceed maximum dose of 600 mg daily); oedema,
Continuation phase1 (antibacterials administered daily or 3 times weekly): isoniazid + rifampicin for 4 months (or isoniazid
berculous mycobacterial disease: 450- muscular weakness and myopathy, exfoliative
+ ethambutol for 6 months but less effective than isoniazid + rifampicin)
600 mg for up to 6 months after –ve dermatitis, toxic epidermal necrolysis, pem-
Category IV: Chronic and multidrug-resistant tuberculosis (MDR-TB) (smear–positive despite supervised re- phigoid reactions, leukopenia, eosinophilia
treatment)5
cultures are obtained.
Specially designed standardized or individualized regimens recommended Chronic, multidrug-resistant pulmo- and menstrual disturbances reported; urine,
nary tuberculosis, 300-450 mg for tears, saliva, and sputum coloured orange-red.
1
Drug intake should be directly obseverd in patients who are smear positive during the initial phase, and always when rifampicin is
given. up to 6 months after –ve sputum Nursing action: Obtain specimen for C&S test
2
Drug sensitivity testing recomended before prescribing Category II treatment in failure cases; patients with MDR-TB should be cultures are obtained. including sputum before treatment.
prescribed Category IV regimen • Give on an empty stomach (i.e., 1 hour prior to or
3
Omit ethambutol in initial phase if disease is not complicated by cavitary disease or concomitant HIV disease, and in patients infected Eldery: No dosage adjustment recommended.
with fully susceptible bacilli or young children with primary tuberculosis Renal impairment (ClCr <30 mL/min): reduce 2 hours after meals) to increase total absorption;
4
Early culture and sensitivity testing recommended for contacts of patients with MDR-TB it may, however, be given with meals if GI irritation
dose by 50%.
occurs; give antiemetic if vomiting occurs.
• Advise against use with alcohol as it may increase RIFAMPICIN plus ISONIAZID isoniazid 5 mg/kg, and ethambutol 15 Dose: Tuberculosis(as part of a 6-month
risk of hepatotoxicity. Indications: Tuberculosis (see notes and mg/kg daily; alternatively, rifampicin regimen; see notes and tables above),
• Monitor hepatic function and serum uric acid 10 mg/kg, isoniazid 10 mg/kg, and by mouth, ADULT rifampicin 10 mg/
tables above).
regularly. ethambutol 30 mg/kg 3 times a week; kg, isoniazid 5 mg/kg, pyrazinamide
• Observe for signs of hepatic impairment namely fe- Contra-indications: see under Rifampicin
and Isoniazid. CHILD rifampicin 10 mg/kg, isoniazid 25 mg/kg, and ethambutol 15 mg/
ver, loss of appetite, fatigue, malaise, jaundice, dark
urine, liver tenderness, and report to the physician. Precautions: Combined preparation usually 5 mg/kg, and ethambutol 20 mg/kg kg daily.
• Warn patient about possible discolouration of not suitable for use in children; see under daily; alternatively rifampicin 10 mg/ POM Rifampicin plus Isoniazid plus Pyrazinamide
the urine, tears, sweat, or other body fluids to a Rifampicin and Isoniazid. kg, isoniazid 10 mg/kg, and ethambu- plus Ethambutol (WMF 6.2.4)
red-orange colour; soft contact lenses may be Adverse effects: see under Rifampicin and tol 30 mg/kg 3 times a week. Tablets, Rifampicin 150 mg, isoniazid 75 mg, pyrazi-
permanently stained. Isoniazid. namide 400 mg, and ethambutol 275 mg.
POM Rifampicin plus Isoniazid plus Ethambutol
• The newborns of rifampicin-treated mothers may
Dose: Tuberculosis (as part of a 6-month reg- (WMF 6.2.4) POM AKuriT®-4 (Ranbaxy)
suffer haemorrhage.
imen; see notes and tables above), by Tablet, Rifampicin 150 mg, Isoniazid 75 mg, Etham- Tablet, Rifampin 150 mg, Isoniazid 75 mg, Pyraz-
Dose: Tuberculosis (as part of a 6- or 8-month butol 275 mg.
mouth, ADULT 10 mg/kg (rifampicin) inzmide 400 mg, Ethambutol HCl 275 mg; f-c tab.
regimen; see introductory notes and
and 5 mg/kg (isoniazid) daily. Pack: 10 x 3 x 3’s; 15 x 6’s; 8 x 28’s; 1000’s; 500’s; 100’s.
tables above), by mouth, ADULT and RIFAMPICIN plus ISONIAZID
Tuberculosis (as part of a 6-month reg-
CHILD 10 mg/kg daily or 3 times plus PYRAZINAMIDE
imen; see notes and tables above), by STREPTOMYCIN
weekly (maximum dose, 600 mg Indications: Tuberculosis, in combination with
mouth, ADULT 10 mg/kg (rifampicin) Indications: Tuberculosis, in combination
daily). other drugs (see notes and tables above).
Administration: Take dose at least 30 minutes
and 10 mg/kg (isoniazid) 3 times a with other drugs (see notes and tables above);
week. Contra-indications: Combined preparation
before a meal, as absorption is reduced when taken tularaemia; plague; brucellosis.
not suitable for use in children; see Rifampicin,
with food. POM Rifampicin plus Isoniazid (WMF 6.2.4) Contra-indications: Hearing disorders; myas-
Isoniazid, and Pyrazinamide.
Tablets, Rifampicin 60 mg with isoniazid 30 mg; thenia gravis; pregnancy (Appendix 2)
EMDEX
POM Rifampicin (WMF 6.2.4) Precautions: See Rifampicin, Isoniazid, and
Capsules or tablets, Rifampicin 150 mg, 300 mg Rifampicin 150 mg with isoniazid 75 mg; Rifampicin Precautions: Children—painful injection,
Pyrazinamide.
300 mg with isoniazid 150 mg; Rifampicin 60 mg avoid use if possible; renal impairment
POM Rifampicin (EDL 5.10) with isoniazid 60 mg (For intermittent use three Adverse effects: See Rifampicin, Isoniazid, and
(Appendix 4), infants, and elderly (dosage
Tablets/Capsules, Rifampicin 150 mg, 300 mg times weekly); Rifampicin 150 mg with isoniazid Pyrazinamide.
adjustment and monitor renal, auditory, and
150 mg (For intermittent use three times weekly). Dose: Tuberculosis (as part of a 6-month reg-
POM DERIFAMPI® (Embassy) vestibular function, and plasma streptomycin
imen; see notes and tables above), by
Capsule, Rifampicin 300 mg. POM Rifampicin plus Isoniazid (EDL 5.10) concentrations); breastfeeding (Appendix 3);
mouth, ADULT rifampicin 10 mg/kg,
POM LARIF® (Mecure) Tablets, Rifampicin 150 mg, Isoniazid 100 mg; Ri- interactions: Appendix 1.
fampicin 300 mg, Isoniazid 150 mg. isoniazid 5 mg/kg, and pyrazinamide
Capsule, Rifampicin 300 mg; red capsule marked Adverse effects: Vestibular and auditory
25 mg/kg daily or rifampicin 10 mg/
‘LARIF’. POM AKuriT® (Ranbaxy) damage, nephrotoxicity; hypersensitivity
kg, isoniazid 10 mg/kg, and pyrazina-
300 mg – 10 x 10’s Tablet, Rifampicin 150 mg, Isoniazid 75 mg; f-c tab. reactions—withdraw treatment; paraesthesia
mide 35 mg/kg 3 times a week.
Pack: 15 x 6’s; 10 x 6’s; 1000’s; 500’s & 100’s. of mouth; rarely, hypomagnesaemia on pro-
POM RECIN® (Strides Vital)
Capsule, Rifampicin 300 mg. POM Rifampicin plus Isoniazid plus Pyrazinamide longed therapy; antibiotic-associated colitis;
POM AKuriT®-Kid (Ranbaxy)
300 mg – 10 x 10’s. (WMF 6.2.4) also, nausea, vomiting, rash; rarely, haemolytic
Tablet, Rifampin 60 mg, Isoniazid 30 mg; uncoated
Tablets, Rifampicin 60 mg, isoniazid 30 mg, and anaemia, aplastic anaemia, agranulocytosis,
POM RIFABON® (Bond) dispersible tab.
pyrazinamide 150 mg; Rifampicin 150 mg, isoniazid thrombocytopenia; pain and abscess at in-
Capsule, Rifampicin 300 mg Pack: 15 x 6’s; 10 x 6’s; 1000’s; 500’s and 100’s.
75 mg, and pyrazinamide 400 mg; Rifampicin 150
jection site.
POM R-CINEX® Kid (Ranbaxy) mg, isoniazid 150 mg, and pyrazinamide 500 mg
Tablet, Rifampin 100 mg, Isoniazid 100 mg; uncoated (For intermittent use three times weekly). Dose: Tuberculosis (as part of a 6- or 8-month
POM RIFACAP® (Hovid) regimen; see notes and tables above),
Capsule, Rifampicin 300 mg dispersible tab.
POM AKuriT-Z® (Ranbaxy) by deep IM injection, ADULT and
300 mg – 10 x 10 (blister) Pack: 10’s.
Tablet, Rifampin 150 mg, Isoniazid 75 mg, Pyrazina-
CHILD 15 mg/kg daily or 3 times a
POM Rifampicin-INH (Neros) mide 400 mg; f-c tab.
POM RIFACIN® (Fil Pharma) week (patients over 60 years or those
Capsule, Rifampicin 150 mg, Isoniazid 100 mg Pack: 15 x 6’s; 10 x 6’s; 1000’s; 500’s & 100’s.
Capsule, Rifampicin BP 300 mg weighing less than 50 kg may not
Pack: 1 x 25’s; 10 x 10’s.
POM TIBITAR® (Bond) tolerate doses above 500–750 mg
POM RIFALAB® (Embassy)
Capsule, Rifampicin 150 mg, isoniazid 100 mg, daily).
Capsule, Rifampicin 300 mg. RIFAMPICIN plus ISONIAZID
plus ETHAMBUTOL pyrazinamide 250 mg. Note: One hour (peak) concentration should be
300 mg – 10 x 10’s.
Caplet, (forte), Rifampicin 300 mg, isoniazid 150 mg Indications: Tuberculosis (see notes and 15–40 mg/litre; pre-dose (trough) concentration
Pack: 2 x 10’s. RIFAMPICIN plus ISONIAZID plus should be less than 5 mg/litre (less than 1 mg/litre
tables above). PYRAZINAMIDE plus ETHAMBUTOL
in renal impairment or those over 50 years).
POM Rifampicin (Neros) Contra-indications: see Rifampicin, Isoniazid, Indications: Tuberculosis (see notes and
Capsule, Rifampicin 300 mg. and Ethambutol. tables above). POM Streptomycin (WMF 6.2.4)
300 mg – 10 x 10’s (in blisters). Precautions: see Rifampicin, Isoniazid, and Powder for injection, Streptomycin (as sulfate) 1
Contra-indications: Combined preparation
Ethambutol g; in vial.
POM RIFOSTAN® (Standard Generics) not suitable for use in children; see Rifampicin,
Capsule, Rifampicin 300 mg; odourless reddish Adverse effects: see Rifampicin, Isoniazid, and Isoniazid, Pyrazinamide, and Ethambutol HCl. POM Streptomycin (EDL 5.10)
brown or brownish crystallin powder in capsule. Ethambutol. Precautions: See Rifampicin, Isoniazid, Pyrazi- Injection, Streptomycin (as sulfate) 1 g, 5 g; powder
Dose: Tuberculosis (as part of an 8-month reg- for injection in vials.
namide, and Ethambutol HCl.
imen; see notes and tables above), by Adverse effects: See Rifampicin, Isoniazid, See preparations under Streptomycin in section 9.1.2.5
mouth, ADULT rifampicin 10 mg/kg, Pyrazinamide, and Ethambutol.
418 | 9.2 Systemic antifungal drugs 9.2 Systemic antifungal drugs | 419
BCG VACCINE struation). Recurrent infection may be treated AMPHOTERICIN B POM Amphotericin B (EDL 5.11.2)
with clotrimazole 500-mg pessary (as a single Indications: Life-threatening fungal infections Injection, Amphotericin B 50 mg; powder for injec-
See under section 17.1.1.1 tion in vial.
dose) every week for 6 months. including histoplasmosis, coccidioidomyco-
Fluconazole, an orally active synthetic imida- sis, paracoccidioidomycosis, blastomycosis, POM Amphotericin B (Evans)
TUBERCULIN PURIFIED aspergillosis, cryptococcosis, mucormycosis, Injection, Amphotericin B 50 mg; freeze-dried pow-
PROTEIN DERIVATIVE zole derivative, possesses fungistatic activity
sporotrichosis, and candidosis; leishmaniasis der for reconstitution.
against dermatophytes, yeasts and other
See under section 17.3 Pack: 1’s (in vial).
pathogenic fungi. It is widely used in the treat- (section 9.3.3).
ment of serious gastrointestinal and systemic Precautions: Close medical supervision
CLOTRIMAZOLE
9.2 Systemic antifungal drugs mycoses as well as in the management of throughout treatment and initial test dose
superficial infections. Fluconazole is also used required (see note, below); renal impairment See under section 11.2
Fungal infections can be superficial or systemic. (Appendix 4); hepatic and renal function tests;
to prevent fungal infections in immunocom-
Superficial infections affect only the skin, hair, blood counts and plasma electrolyte (including
promised patients. FLUCONAZOLE
nails or mucous membranes whereas systemic potassium and magnesium concentration)
fungal infections affect the body as a whole. Flucytosine is a synthetic fluorinated pyrim- Indications: Systemic mycoses including
monitoring; pregnancy (Appendix 2); breast-
idine with a narrow spectrum of antifungal histoplasmosis, non-meningeal coccidioi-
Systemic fungal infections are sometimes feeding (Appendix 3); avoid rapid infusion
activity, particularly against Cryptococcus and do-mycosis, paracoccidioidomycosis and blas-
caused by inhalation, ingestion or inoculation (risk of arrhythmias); interactions: Appendix 1.
Candida spp. In susceptible fungi, it is con- tomycosis; treatment and, in AIDS and other
of primary pathogens, and sometimes by op- ANAPHYLAXIS: Anaphylaxis occurs rarely with
verted to fluorouracil by cytosine deaminase. immunosuppressed patients, prophylaxis of
portunistic invasion of commensals in patients intravenous amphotericin B and a test dose is
Flucytosine is myelosupp-ressive and plasma cryptococcal meningitis; prevention of fungal
with lowered host resistance. They are increas- advisable before the first infusion. The patient
concentrations above 75 µg/mL are associated infections in immuno-compromised patients;
ing in prevalence not only because of the should be observed for about 30 minutes after
with myelotoxicity. oesophageal and oropharyngeal candidosis,
pandemic of HIV infection, but also because of the test dose.
EMDEX
the rise in illicit intravenous drug use in many Griseofulvin is a fungistatic antibiotic derived vaginal candidosis and systemic candidosis.
Adverse effects: Fever, headache, anorexia, Precautions: Renal impairment (Appendix 4);
countries, and greater use of broad spectrum from Penicillium griseofulvum with selective
weight loss, nausea and vomiting, malaise, pregnancy (Appendix 2); breastfeeding (Ap-
antibiotics and invasive medical procedures. activity against the dermatophytes causing
diarrhoea, muscle and joint pain, dyspepsia, pendix 3); monitor liver function—discontinue
In immunodeficient patients systemic fungal ringworm, Microsporum canis, Trichophyton
and epigastric pain; renal function distur- if signs or symptoms of hepatic disease (risk of
infections are often disseminated. rubrum and T. verrucosum. It has no activity
bances including hypokalaemia, hypomag- hepatic necrosis; Appendix 5); susceptibility
against pityriasis versicolor or candida infec-
Amphotericin B is a lipophilic polyene antibi- nesaemia and renal toxicity; blood disorders; to QT interval prolongation; interactions:
tions. Griseofulvin is deposited selectively in
otic; it is fungistatic against a broad spectrum cardiovascular toxicity (including arrhythmias); Appendix 1.
keratin precursor cells of skin, hair and nails
of pathogenic fungi, including Candida spp., neurological disorders (including peripheral Adverse effects: Nausea, vomiting, abdominal
where it disrupts the mitotic apparatus of
Aspergillus spp., Cryptococcus neoformans , neuropathy); abnormal liver function (discon- pain, dyspepsia, flatulence, diarrhoea; head-
fungal cells thus preventing fungal invasion
Histoplasma capsulatum, Blastomyces derma- tinue treatment); rash; anaphylactoid reactions ache, taste disturbance, hepatic disorders,
of newly-formed cells. It is unsuitable for
titidis, Coccidioides immitis, Paracoccidioides (see above); pain and thrombophlebitis at dizziness, seizures, alopecia, pruritus; rash
prophylactic use. Close attention should be
brasiliensis, Mucor, Absidia and Phicopes spp.; injection site. (withdraw treatment); angioedema, anaphy-
given to hygiene and to possible reservoirs of
it is active against algal Prototheca spp. and Advice to patients: Report any cramping, mus- laxis, bullous lesions, toxic epidermal necrolysis
reinfection in clothing, footware and bedding.
against the Leishmania protozoa. It is used cle weakness, or pain at or near injection site. and erythema multiforme (Stevens-Johnson
for the empirical treatment of serious fungal Nystatin, a polyene antifungal antibiotic Nursing action: Obtain specimen for C&S test syndrome) reported (severe skin reactions
infections and is used in conjunction with derived from Streptomyces noursei, is effective including sputum before treatment. more common in AIDS); hyperlipidaemia,
flucytosine to treat cryptococcal meningitis against infections caused by a wide range of • Give a test dose and monitor patient’s pulse,
leukopenia, thrombocytopenia, hypokalaemia.
and systemic candidosis. yeasts and yeast-like fungi. It is poorly ab- respiration, temperature, BP for about 30 minutes
Advice to patients: May take with food; com-
sorbed from the gastrointestinal tract and it is prior to the amphotericin B infusion; avoid rapid
Amphotericin B has to be administered paren- injection which may cause circulation collapse plete full course of therapy; contact physician
not absorbed from the skin or mucous mem-
terally as there is little or no absorption from (usually 4– to 6-hourly infusion required). or pharmacist if side effects develop.
branes when applied topically. It is used for the
the gastrointestinal tract; amphotericin B can • Reconstitute the dry form with 10 mL of sterile wa- Nursing action: Oral bioavailability of flucona-
treatment of candidosis, but is less effective
be nephrotoxic. Duration of therapy depends ter only. Do not use if solution contains precipitate. zloe is greater than 90% and is unaffected by
for prevention or treatment of candidosis in
on the initial severity of the infection and the • Give antipyretic, antihistamine or antiemetic as gastric pH; dosage is the same for oral or I.V use.
immunocompromised patients. premedication to prevent adverse effects fever, • Administer with food to reduce GI upset; shake oral
clinical response of the patient. In some infec-
tions a satisfactory response is only obtained Potassium iodide aqueous oral solution is a chills, headache as needed. suspension before each use.
clear liquid with a characteristic, strong salty • Monitor for signs of hypokalaemia (muscle weak- • I.V. fluconazole may be administered by continous
after several months of continuous treatment.
taste. It is effective against sporotrichosis and ness, cramping, drowsiness, anorexia, etc.). infusion at a rate not exceeding 200 mg/hour;
Lipid formulations of amphotericin B for intra- • Dose: Systemic fungal infections, by IV infusion,
subcutaneous phycomycosis, which are fun- do not connect in series with other infusions to
venous infusion [not included on WHO Model ADULT and CHILD initial test dose of 1 mg over prervent air embolism; do not add any other drugs
List] are significantly less toxic, however, lipid gal infections caused by Sporothrix schenckii 20–30 minutes, then 250 µg/kg daily, gradually to the solution.
formulations are very much more expensive. and Basidiobolus haptosporus respectively. In increased up to 1 mg/kg daily or in severe infection, • Advise patient that prolonged treatment may be
subcutaneous sporotrichosis, amphotericin B up to 1.5 mg/kg daily or on alternate days. needed to control infection and prevent relapse,
Clotrimazole is an imidazole antifungal which
is often effective in patients unable to tolerate Note: Prolonged treatment usually necessary; if even if symptoms abate in first few days of therapy.
is effective in short courses for the treatment
iodides. Itraconazole, by mouth has been tried interrupted for longer than 7 days, recommence at • Dosage should be adjusted in renal failure as the
of vaginal candidosis. Treatment involves in- 250 µg/kg daily and increase gradually.
as an alternative to potassium iodide in both drug is excreted unchanged by the kidneys.
sertion of pessaries (vaginal tablets) or cream
cutaneous and extracutaneous sporotrichosis. POM Amphotericin B (WMF 6.3) Dose: Systemic mycoses, by mouth or by IV
high into the vagina (including during men-
In phycomycosis, fluconazole may be effective. Powder for injection, Amphotericin B 50 mg; in vial. infusion, ADULT 200 mg daily for at
least 6 months; CHILD over 2 years Capsules, Fluconazole 50 mg, 150 mg, 200 mg Capsule, Fluconazole 50 mg, 150 mg; hard cap Compound preparations
3–6 mg/kg daily for at least 6 months. 50 mg – 4’s (in strip) Pack: 1’s; 3’s; 7’s; 10’s; 14’s; 20’s; 28’s; 30’s; 42’; 50’s;
POM DAZEL® Kit (Olpharm)
Cryptococcal meningitis (following 150 mg – 1’s (in strip) 100’s
Combipack, Fluconazole 150 mg (1 uncoated tablet)
amphotericin B induction therapy), 200 mg – 4’s (in strip)
POM FLUZOL®-150 (Embassy) + Azithromycin 1 g (1 f-c tablet) + Secnidazole 1 g
Tablets , Fluconazole 100 mg; dispersible tab.
by mouth or by IV infusion, ADULT Capsule, Fluconazole 150 mg. (2 f-c tablets).
800 mg daily for 2 days, then 400 mg 150 mg – 1 x 10’s. Indications: Syndromic management of STDs in
Injection (IV), Fluconazole 2 mg per mL.
daily for 8 weeks; CHILD 6–12 mg/kg women with symptoms such as vaginal or introital
Pack: 100 mL POM FLUZOLE® (Bond)
daily (every 72 hours in NEONATES itch plus discharge with or without yellow or green
Capsule, Fluconazole 50 mg
POM DIFLUCAN® (Pfizer) frothy, malodorous discharge.
up to 2 weeks old, every 48 hours in 50 mg – 10’s (in blisters)
Capsule, Fluconazole 50 mg. Dose: By mouth, Adult female, Azithromycin 1 g as
NEONATES 2–4 weeks old) 50 mg – 3; 30. single dose plus Secnidazole 2 g as single
POM FLUZON® (Interpharma)
Prevention of relapse of cryptococcal Suspension, Fluconazole 50 mg per 5 mL; powder Tablets, Fluconazole 100 mg, 150 mg. dose (1 g tablet x 2) plus Fluconazole 150
meningitis in AIDS patients after com- for reconstitution. 100 mg – 5 x 4’s mg as single dose.
pletion of primary therapy, by mouth, 150 mg – 10 x 2’s. Administration: Give Azithromycin tablet 1-2 hours
POM FLUCAMED® (Drugfield)
ADULT 200 mg daily or by IV infusion, before food; Fluconazole tablet before or after food
Capsules, Fluconazole 50 mg, 200 mg POM FUNAZOL® (Al-Tinez)
ADULT 100–200 mg daily. and Secnidazole tablets with food.
50 mg – 3’s; 10’s (in blisters) Capsule, Fluconazole 50 mg; light blue cap. filled
Systemic candidosis (in patients unable 200 mg – 10’s (in blisters) with white or light brown powder. POM FLUDAZOLE® (Nomedi)
to tolerate amphotericin B), by mouth Oral suspension, Fluconazole 10 mg per mL; powder 50 mg – 3’s (in a box) Tablet, Each kit contains Fluconazole 150 mg +
or by IV infusion, ADULT 400 mg as for reconstitution. Ornidazole750 mg; f-c tab
POM FOSFO® (Vixa)
initial dose, then 200 mg daily for Pack: 35 mL Indications: Treatment of anaerobic infections
Capsules, Fluconazole 50 mg, 150 mg. both pre & post operatively, bacterial vaginosis,
at least 4 weeks; CHILD 6–12 mg/kg POM FLUCAMIL® (Miraflash) 50 mg – 1 x 10’s
daily (every 72 hours in NEONATES up amoebic dysentery, amoebic liver abscess, vaginal
Capsule, Fluconazole 50 mg 150 mg – 1 x 3’s
EMDEX
to 2 weeks old, and every 48 hours in candidiasis (vaginal yeast infection due to candida),
50 mg – 1 x 3’s; 1 x10’s (in blisters)
POM GVFLUC® (Greenlife) oropharyngeal and esophageal candidiasis, crypto-
NEONATES 2–4 weeks old).
POM FLUCOMARK® (Mark) Capsule, Fluconazole 150 mg; light turquoise red cap. coccal meningitis.
Oesophageal and oropharyngeal can- Capsule, Fluconazole 150 mg Dose: One tablet of Fluconazole and 2 tablets of
150 mg – 1’s.
didosis, by mouth or by IV infusion, 150 mg – 10 x 1 Oral suspension, Fluconazole 50 mg per 5 mL; orange Ordinazole as a single oral dose. Both the
ADULT 200 mg as an initial dose, Injection, Fluconazole 200 mg, sodium chloride 0.9 flavoured powder for reconstitution. partners should be treated with this dose
then 100 mg daily until symptoms gm per 100 mL. Pack: 35 mL. to minimize recurrence.
resolved; up to 400 mg daily in very POM FLUTIN® (Nomedi)
POM FLUCOMOL® (Crystal) POM JUCONAZOLE® (Juhel)
resistant infections; CHILD 3–6 mg/ Capsule, Fluconazole 50 mg. Combipack, Each kit contains Fluconazole 150 mg (1
Capsule, Fluconazole 50 mg.
kg on the first day, then 3 mg/kg 50 mg – 1 x 10’s. f-c tab); titanium dioxide colour + Tinidazole 1000
daily (every 72 hours in NEONATES POM LUCON® (Medreich) mg (2 f-c tabs); quinoline yellow colour.
up to 2 weeks old, every 48 hours in POM Fluconazole (Novartis) Capsules, Fluconazole 50 mg, 150 mg, 200 mg Indications: Management of vaginal candidiasis,
Capsule, Fluconazole 200 mg; white/purple cap. vaginal trichomoniasis and bacterial vaginosis.
NEONATES 2–4 weeks old). POM NOVACAN® (Lintak)
200 mg – 7’s; 10’s; 14’s; 20’s; 30’s; 50’s; 100’s Dose: One tablet of fluconazole and two tablets of
Vaginal candidosis, by mouth, ADULT Tablet, Fluconazole 150 mg.
150 mg as a single dose. POM Fluconazole (Solution Pharma) tinidazole as a single dose given by mouth;
Capsule, Fluconazole 200 mg; white-blue cap. POM PROCONAZOLE® (Kayhelt) without food.
Prevention of fungal infections in im- Tablet, Fluconazole 200 mg; uncoated tab
200 mg – 1 x 10’s.
munocompromised patients, by mouth 200 mg – 10 x 10’s
Suspension, Fluconazole 10 mg per 5 ml; dry white FLUCYTOSINE
or by IV infusion, ADULT 50–400 mg to off-white powder which yields an orange fla- POM TAMACON® (Tamar & Pharez) Indications: Adjunct to amphotericin B (or
daily adjusted according to risk; com- voured susp. Capsules, Fluconazole 50 mg, 200 mg fluconazole) in cryptococcal meningitis; ad-
mence treatment before anticipated Pack: 50 mL. 50 mg – 1 x 10's
onset of neutropenia and continue junct to amphotericin B in systemic candidosis.
POM Fluconazole (Zeenat) 200 mg – 1 x 10’s
for 7 days after neutrophil count in Precautions: Elderly; renal impairment (Ap-
Eye drop, Fluconazole 0.3% w/v POM ULTRA-FLU® (Tamar & Pharez) pendix 4); also use with amphotericin B (both
desirable range; CHILD according to Pack: 5 mL. Capsule, Fluconazole 150 mg. nephrotoxic); liver– and kidney function tests
extent and duration of neutropenia, 150 mg – 2’s
3–12 mg/kg daily (every 72 hours in POM FLUCOSTAT® I.V. (Fidson) and blood counts required (weekly in renal
NEONATE up to 2 weeks old, every Injection, Fluconazole 2 mg per mL; sterile solution POM VULCAN®-50 (Alvid) impairment or in blood disorders); pregnancy
in iso-osmotic NaCl diluent. Capsule, Fluconazole 50 mg; cap. marked ‘VULCAN’ (Appendix 2); breastfeeding (Appendix 3);
48 hours in NEONATE 2–4 weeks old);
Pack: 100 mL; 200 mL. in a circular direction. interactions: Appendix 1.
max. 400 mg daily.
POM FLUCOSYD® (Neimeth) 50 mg – 6’s. Adverse effects: Rash, nausea, vomiting and
POM Fluconazole (WMF 6.3) Capsule, Fluconazole 50 mg. diarrhoea; alterations in liver function tests; less
POM ZINAZOLE® (Chanmedi)
Capsule, Fluconazole 50 mg. 50 mg – 3’s; 30’s. Tablets, Fluconazole 50 mg, 200 mg. frequently, confusion, hallucinations, convulsions,
Oral liquid, Fluconazole 50 mg/5 mL. Oral suspension, Fluconazole 50 mg per 5 mL; pow-
Injection, Fluconazole 2 mg/mL; in vial.
200 mg – 1 x 10’s . headache, sedation, vertigo; blood disorders
der for reconstitution. including leukopenia, potentially fatal thrombo-
Pack: 35 mL. POM ZOOFLUCAN® (Zoomota)
POM Fluconazole (EDL 5.11.2) cytopenia and aplastic anaemia.
Infusion, Fluconazole 2 mg per mL; in 100 mL bottle;
Capsules, Fluconazole 50 mg, 150 mg. POM FLUCOVID® (Hovid) Dose: Systemic candidosis and cryptococcosis,
yellow solution.
Injection, Fluconazole 2 mg per mL; solution for IV Capsule, Fluconazole 150 mg Pack: 100 mL. by IV infusion (over 20–40 minutes),
injection in 0.9% NaCl. 150 mg – 1 x 10’s; 1 x 4’s (in blisters) ADULT and CHILD 200 mg/kg daily in
POM COTOZAL® (Evans) POM FLUNOC® (Taylek) 4 divided doses, for usually no more
than 7 days (at least 4 months in Dose: Superficial fungal infections, by mouth, Tablets, Griseofulvin 125 mg, 500 mg; white f-c antacids, H2 antagonists such as cimetidine.
cryptococcal meningitis); extremely ADULT 0.5–1 g (but not less than 10 biconvex tabs. marked ‘GLAXO’ and ‘GRISOVIN 125’ Adverse effects: Nausea, abdominal pain,
sensitive organisms, 100–150 mg/kg mg/kg) daily with food in single or and ‘GRISOVIN 500’ respectively. headache, dyspepsia, constipation, (diarrhoea
daily in 4 divided doses. divided doses; CHILD 10 mg/kg daily 125 mg – 20; 1000. and vomiting with oral liquid), dizziness,
500 mg – 20; 250.
Systemic candidosis, initial treatment with food in single or divided doses. fatigue; hypersensitivity reactions such as
or after IV therapy, by mouth, ADULT Note: Duration of treatment depends on the in- POM KRISOVIN® (Goben) rash, pruritus, urticaria and angio-oedema;
and CHILD 50–150 mg/kg daily in 4 fection and thickness of keratin at site of infection; Tablets, Griseofulvin 125 mg (white scored tab.); 500 decreased libido, impotence; abnormal hepatic
divided doses. at least 4 weeks for skin and hair, at least 6 weeks mg (convex tab. marked ‘UP 500’). function.
Note: For plasma concentration monitoring blood for scalp ringworm and in severe infection, up to 3 125 mg – 10’s; 10 x 10’s; 50 x 10’s.
Advice to patients: Take with food; report
should be taken shortly before starting next infusion months; 6 months for fingernails and 12 months or 500 mg – 100’s; 500’s; 1000’s.
more for toenails.
any unusual fatigue, anorexia, nausea and/
(or before next dose by mouth); plasma concentra- POM MARVIN-500® (Pemason) or vomiting, jaundice, dark urine or pale stool
tion for optimum response 25–50 mg/litre—should POM Griseofulvin (WMF 6.3) Tablet, Griseofulvin 500 mg (possible symptoms of liver impairment).
not be allowed to exceed 80 mg/litre. Tablets or capsules, Griseofulvin 125 mg, 250 mg
POM RECGRISO® (GoldMoore) Nursing action: Administer capsule whole
POM Flucytosine (WMF 6.3) POM ARTCIN® (Embassy) Tablet, Griseofulvin 500 mg. after full meal to ensure absorption.
Capsule, Flucytosine 250 mg. Tablet, Griseofulvin 500 mg; white tab. marked Pack: 20’s. • Advise patient that prolonged treatment may be
Infusion, Flucytosine 2.5 g in 250 mL. ‘logo C’ needed to control infection and prevent relapse,
POM RECIN®-500 (Vixa) even if symptoms abate in first few days of therapy.
500 mg – 20’s; 100’s; 1000’s.
GRISEOFULVIN Tablet, Griseofulvin 500 mg. • See also under Ketoconazole.
POM CIKASOLVIN® (Michelle Lab) Pack: 10’s; 20’s (in blisters).
Indications: Fungal infections of the skin, Dose: By mouth, Vulvovaginal candidosis, 200
Tablet, Griseofulvin 500 mg
scalp, hair and nails where topical treatment POM REFUCIL® (Reals) mg morning and evening for 1 day;
500 mg – 100’s; 10 x 10’s (in blisters)
Tablet, Griseofulvin 500 mg. Oral candidosis, 100 mg daily for 15
has failed or is inappropriate.
POM ERECIN-500® (Vixa) Pack: 10 x 10’s; 2 x 10’s (in blisters).
EMDEX
Contra-indications: Severe liver disease days;
Tablet, Griseofulvin 500 mg; uncoated tab. Suspension, Griseofulvin 125 mg per 5 mL.
(Appendix 5); pregnancy (avoid pregnancy Pityriasis versicolor, 200 mg daily
500 mg – 10’s; 20’s (in blisters).
during and for 1 month after treatment; men POM RYSOVIN-500® (Beta Drugs) for 7 days;
should not father children within 6 months of POM FESOVIN® (Embassy) Tablet, Griseofulvin 500 mg. Tinea corporis and tinea cruris, 100
Tablet, Griseofulvin 500 mg. 500 mg – 20’s (in blister). mg daily for 15 days (or 200 mg twice
treatment; Appendix 2); porphyria; systemic
500 mg – 20’s. daily for 7 days);
lupus erythematosus (risk of exacerbation). POM VITAFULWIN® (Strides Vital)
Precautions: Pre-existing hepatic insufficiency POM G-CIN® (Greenlife) Tablet, Griseofulvin 500 mg; white scored tab. Tinea pedis and tinea manuum, 100
(closely monitor hepatic function throughout Tablet, Griseofulvin 500 mg. marked ‘GRISEO 500’. mg daily for 30 days (or 200 mg twice
treatment); blood disorders (monitor blood 500 mg – 20’s. 500 mg – 20’s. daily for 7 days); Onychomycosis, 200
count weekly during first month of treatment); POM GENEVIN® (Geneith) POM ZEXAN® (Elbe) mg daily for 3 months (or a course
breastfeeding (Appendix 3); interactions: Tablet, Griseofulvin 500 mg. Tablet, Griseofulvin 500 mg. of 200 mg twice daily for 7 days,
Appendix 1. 500 mg – 20’s (in blister). Pack: 2 x 15’s. subsequent courses repeated after
Adverse effects: Headache, nausea, vomiting, POM GRENIN® (Jubilee)
21-day interval; finger nails 2 courses,
diarrhoea, rashes, dizziness, fatigue reported; Tablet, Griseofulvin 500 mg; white tab. marked with ITRACONAZOLE toenails 3 courses). Histoplasmosis,
leukopenia, hepatotoxicity; sleep disturbances; the logo ‘C’. Therapeutic category: Antifungal agent, 200 mg 1-2 times daily.
photosensitivity; systemic lupus erythema- 500 mg – 20’s; 100’s; 1000’s. systemic. Systemic fungal infections where other
tosus, toxic epidermal necrolysis, erythema Pharmacology: Itraconazole is a triazole antifungal drugs are inappropriate
POM GRIFULVIN® (Dizpharm)
multiforme; peripheral neuropathy; confusion Tablet, Griseofulvin 125 mg. derivative active against infections with der- or in effective, 200 mg once daily
and impaired coordination. 125 mg – 100. matophytes, yeast, Aspergillus spp and various (candidiasis 100-200 mg once daily);
Advice to patients: Take with fatty meal for other yeasts and fungi. Oral bioavailability is increased in invasive or disseminated
POM Griseofulvin (Hochiez) disease and cryptococcal meningitis
better absorption; avoid exposure to sunlight; Tablet, Griseofulvin 500 mg; round, white tabs.
maximal when it is given immediately after a
if patient gets headache, it usually goes away full meal. It is extensively metabolized by the to 200 mg twice daily.
500 mg – 20’s
with continued therapy; may cause dizziness, liver and should be avoided in patients with a Not recommended for the child and
POM Griseofulvin (Hovid) history of liver disease. elderly.
drowsiness, and impair judgement; do not
Tablets, Griseofulvin 125 mg, 500 mg; f-c tabs.
drive or perform other hazardous activities; Indications: Vulvovaginal candidosis, pityriasis POM CANDITRAL®(Glenmark)
125 mg – 1000
effect of alcohol enhanced by the drug; do 500 mg – 20; 500. versicolor, dermatophytoses, fungal keratitis, Capsule, Itraconazole 100 mg; in a pellet formulation.
not take if pregnant; if you become pregnant, oral candidosis; may also be used in systemic 100 mg – 4’s.
discontinue immediately. POM Griseofulvin (Neros) fungal infections (including aspergillosis, can-
Tablet, Griseofulvin 500 mg POM CONAZOLE® (Joswe/Afrab)
Nursing action: Advise patient that prolonged didiasis, and cryptococcosis) where other an- Capsule, Itraconazole 100 mg; in a pellet formulation.
treatment may be needed to control infection tifungal drugs are inappropriate or ineffective.
and prevent relapse, even if symptoms abate POM Griseofulvin (Zeenat) Contra-indications: Pregnancy; hypersensi- POM IKINN® (Nalis)
Oral suspension, Griseofulvin 125 mg per 5 mL Capsule, Itraconazole 100 mg; f-c hard gelatin cap
in first few days of therapy. tivity to any component.
• Most effectively absorbed and causes least GI Pack:100 mL Precautions: Patients with history of liver POM ITRACAP® (Kayhelt)
distress when given after high-fat meal. POM GRISOLEX® (Med Impex) disease; breast-feeding; renal impairment (bi- Capsule, Itraconazole 100 mg; coated beads in cap.
• Tell patient to keep skin clean and dry and to avoid Tablet, Griseofulvin BP 500 mg. oavailability may be reduced); children; elderly. 100 mg – 3 x 10’s (in blisters)
intense sunlight. 500 mg – 1 x 10’s (in blister). Interactions: Avoid co-administration with POM Itraconazole (Biostadt)
• Advise patient to avoid alcoholic beverages.
POM GRISOVIN® (GSK) astemizole, terfenadine, cisapride, rifampicin, Capsule, Itraconazole 100 mg
100 mg – 1 x 4’s (in blisters) high pH of gastric contents (it requires acidity 200 mg – 10 x 10’s (in blisters). NYSTATIN
POM ITRANOX® (Alpha) for dissolution and absorption). POM Ketoconazole (Nosak) Therapeutic category: Oral nonabsorbed
Tablet, Itraconazole 100 mg; white or almost white • Give with acidic products such as fruit juice to aid Tablet, Ketoconazole 200 mg; uncoated tab. antifungal agent.
dissolution and absorption of ketoconazole.
oblong f-c tablets.
POM KETOFUNG® (Drugfield)
Indications: Oral, oesophageal, intestinal,
100 mg – 10 • Advise patient to take oral suspension with straw,
to avoid contact with the teeth and to drink a Caplet, Ketoconazole 200 mg vaginal, and cutaneous candidosis.
POM IZOLE® (Hovid) glass of water immediately after; nausea may be 200 mg – 3 x 10’s Precautions: Pregnancy and breastfeeding
Capsule, Itraconazole 100 mg; opaque blue/pink minimised if drug is divided into 2 doses; Cream, Ketoconazole 2% (Appendices 2 and 3).
transparent cap • Advise patient to avoid driving or other hazardous Pack: 20 g Adverse effects: Nausea, vomiting, diarrhoea
100 mg – 7 x 4’s activities if dizziness occurs. at high doses; oral irritation and sensitization;
POM KETOGATE® (Pharmgate)
• Teach patient symptoms of liver dysfunction rash and rarely, erythema multiforme (Ste-
POM NECTRANOX® (Nectar Healthcare) Tablet, Ketoconazole 200 mg.
viz unusual fatigue, jaundice, dark urine or pale vens-Johnson syndrome).
Capsule, Itraconazole 100 mg; hard gelatin cap. 200 mg – 2 x 10’s.
stools, anorexia, vomiting and to notify physician Nursing action: Nystatin is quite safe when
if they occur. POM KETORAL®-200 (Embassy)
used orally, vaginally or topically, but advise
POM SPORANOX® (Janssen-Cilag) Dose: By mouth, Adult, Vaginal candidosis, Tablet, Ketoconazole 200 mg.
Capsule, Itraconazole 100 mg; pellets in a blue/ Pack: 1 x 10’s in a monocarton. patient to report redness, swelling, or irritation.
200-400 mg once daily with meals • Vaginal tablets can be used by pregnant women up
pink cap. for 5 days. POM MEKOZORAL® (Neros) to 6 weeks before term to treat maternal infection
100 mg – 4; 15 (in blisters).
Pityriasis versicolor, 200 mg once daily Tablet, Ketoconazole 200 mg. that may cause thrush in newborns.
POM TRANAZOLE® (Barata) with meals for 5 – 10 days. 200 mg – 2 x 10’s. • Continue therapy during menstruation.
Capsule, Itraconazole 100 mg; hard gelatin cap. Skin, GI and systemic infections, 200- • Instruct patient to wash applicator thoroughly
POM NITOZOL® (Pharmabox)
100 mg – 10’s (in blisters) 400 mg once daily with meals usually after each use.
Tablet, Ketoconazole 200 mg.
for 14 days or at least one week after • Explain to the patient that the following factors can
KETOCONAZOLE POM NIZORAL® (Janssen-Cilag ) predispose to vaginal infection: Use of antibiotics,
EMDEX
the symptoms have cleared and
Therapeutic category: Antifungal agent. Tablet, ketoconazole 200 mg; white scored tab. oral contraceptives, and corticosteroids; diabetes;
cultures become negative marked ‘JANSSEN’ and ‘K over 200’. reinfection by sexual patner; and tight-fitting
Pharmacology: Ketoconazole is an imida- Child (upto 15 kg), 20 mg 3 times 200 mg – 10, 30. panty hose.
zole-dioxolane antimycotic which acts by daily; Suspension, Ketoconazole 100 mg per 5 mL • For treatment of oral candidiasis (thrush): Be sure
inhibiting purine transport and DNA, RNA, 15-30 kg, 100 mg once daily; above Pack: 100 mL. the mouth is clean of food debris before adminis-
and protein synthesis; it increases cell wall 30 kg, 200 mg once daily. tering drug, then tell patient to hold suspension
POM VACTORAL® (Evans)
permeability, making the fungus more suscep- in mouth for several minutes before swallowing.
POM FANZOL® (Seagreen) Tablet, Ketoconazole 200 mg.
tible to osmotic pressure. It is effective orally 200 mg – 10’s; 100’s.
When treating infants, swab medication on oral
Tablet, Ketoconazole 200 mg
and has a broad-spectrum of activity against mucosa. Instruct patient on good oral hygiene
200 mg – 10’s
dermatophytes, yeasts and other pathogenic POM WATZOLE® (Watson) techniques. Inform patient overuse of mouthwash
fungi. Much larger doses may be needed to POM FUNGRAL® (Medreich) Tablet, Ketoconazole 200 mg. may alter flora and promote infection
Tablet, Ketoconazole USP 200 mg. • Advise patient to continue the medication for
treat fungal meningitis.
MICONAZOLE the prescribed duration even if symptoms abate.
Indications: Fungal infections of the skin, hair, POM INTERZOL® (Reals) • Instruct patient on careful hygiene for affected
nails; yeast infection of the mouth such as oral Tablet, Ketoconazole 200 mg; f-c tab. Therapeutic category: Antifungal Agent.
areas
thrush,; vaginal candidosis; systemic mycotic 200 mg – 5 x 10’s; 10 x 10’s (in a blister). Pharmacology: Miconazole is a synthetic • Not effective against systemic infections
infections; prophylactic against mycotic infec- POM KATHAMIDE® (Vixa) imidazole derivative which acts by inhibiting Dose: Oral candidosis, by mouth, ADULT and
tions in patients with reduced host defences Tablet, Ketoconazole 200 mg purine transport and DNA, RNA, and protein CHILD over 1 month, 100 000 units
e.g. cancer patients. 200 mg – 100’s synthesis; it increases cell wall permeability, after food 4 times daily usually for
Contra-indications: Hypersensitivity to the making the fungus more susceptible to os- 7 days; continue for 48 hours after
POM KATMAC® (Pharmabase)
drug; acute or chronic liver disease. motic pressure. It has high fungicidal activity lesions have resolved.
Tablet, Ketoconazole 200 mg
Precautions: Monitor liver enzyme levels for 200 mg – 1 x10’s against dermatophytes, yeasts and dimorphic Intestinal and oesophageal candidosis,
patients with history of liver disease; acute fungi as well as bactericidal activity against by mouth, ADULT 500 000 units 4
POM KETACON® (Strides Vital) Gram-positive bacilli and cocci.
porphyria, pregnancy. Tablet, Ketoconazole 200 mg. times daily; CHILD over 1 month 100
Interactions: Avoid co-administration with al- Indications: Oral and intestinal candidiasis. 000 units 4 times daily; continue for
200 mg – 2 x 10’s.
cohol or hepatotoxic drugs such as terfenadine, Precautions: Pregnancy. 48 hours after clinical cure.
cisapride, astemizole, cyclosporine, isoniazid or POM KETAZOL® (Shalina) Adverse effects: Nausea, diarrhoea. Vaginal candidosis, vaginal adminis-
Tablet, Ketoconazole 200 mg; f-c tab. Nursing action: May give with meal to lessen
rifampin. Antacids, anticholinergics, antispas- tration, ADULT insert 1–2 pessaries at
200 mg – 10’s. GI distress; antiemetic may be needed to pre-
modics, histamine H2-receptor antagonists or night for at least 2 weeks
omeprazole may decrease the absorption and POM Ketoconazole (Crystal) vent nausea and vomiting.
Tablet, Ketoconazole 200 mg • Encourage good personal hygiene, hand-washing POM Nystatin (WMF 6.3)
hence the antifungal effect of Ketoconazole Tablets, Nystatin 100 000 IU, 500 000 IU.
200 mg – 10’s (in blisters) and nail care.
(give about 2-hour interval). Lozenge, Nystatin 100 000 IU.
• Inform patient that adequate therapeutic response
Adverse effects: Occasionally nausea and POM Ketoconazole (Hovid) may take weeks or months. Pessary, Nystatin 100 000 IU.
vomiting; idiosyncratic liver reaction (discon- Tablet, Ketoconazole 200 mg; white scored tab. • See also under Ketoconazole.
marked ‘H/D’. POM Nystatin (EDL 5.11.2)
tinue if occur). Dose: See lit.
200 mg – 10 x 10. Tablet, Nystatin 500,000 units
Nursing action: Administer 2 hours prior to Oral liquid, Nystatin 100,000 units per mL.
antacids or other drugs that increase gastric POM Miconazole (EDL 5.11.2)
POM Ketoconazole (Korlyns) Lozenges, Nystatin 100,000 units
Tablet, Miconazole 250 mg.
pH to prevent decreased absorption due to the Tablet, Ketoconazole 200 mg; scored tab. marked ‘KK’ Pessary, See under Section 11.2
426 | 9.2 Systemic antifungal drugs 9.3 Antiprotozoal drugs | 427
POM Nystatin (Al-Tinez) on the species. When given orally, the drug primarily by hepatic CYP2C19, CYP2C9 and 6 mg/kg
Invasive Aspergillos 400mg q12h 200mg q12h
Vaginal tablet, Nystatin 100,000 IU concentrates in skin and nails at levels associ- CYP3A4 isoenzymes. q12h
Pack:1 x 12’s; 10’s ated with fungicidal activity. Indications: Treatment of invasive aspergillo- Candidemia and 6 mg/kg 400 mg 400 mg
invasive candidiasis q12h q12h q12h
POM Nystatin (Crystal) Indications: Treatment of ringworm (tinea sis; candidaemia in non-neutropinic patients; Esophageal
Oral suspension, Nystatin 100,000 IU corporis, tinae cruris and tinea pedis) and yeast fluconazole-resistant serious invasive Candida candidiasis 6 mg/kg
Pack: 30 mL infections of the skin caused by the genus infections (including C. krusei); serious fungal Scedosporiosis and q12h
Fusariosis
POM MYCOSOP® (Alpha) candida where oral therapy is considered ap- infections caused by Scedosporium spp. &
Oral suspension, Nystatin 100,000 IU per mL; yellow propriate owing to the site, severity or extent of Fusarium spp. Used mainly in patients with pro- Maintenance Dose Regimen (after first 24
susp. with pleasant cherry taste in 30-mL bottle + the infection; onychomycosis (fungal infection gressive, possibly life-threatening infections. hours)
calibrated 1-mL dropper. of the nail) caused by dermotophyte fungi. Contra-indications: Hypersensitivity to Oral dose
Pack: 30 mL x 45’s Oral terbinafine is not effective in pityriasis voriconazole or its excipients. Co-administra- Infection IV dose Patients
Patients <40 kg
versicolor; the topical form is recommended. tion with CYP3A4 substrates e.g. terfenadine, ≥40 kg
POTASSIUM IODIDE Precautions: Severe liver dysfunction or astemizole, cisapride, pimozide, quinidine Invasive 4mg/kg 200mg
100mg q12h
Aspergillosis q12h q12h
Indications: Sporotrichosis; subcutaneous impaired renal function (reduce dose) ; preg- (QTc prolongation). Other CYP3A4 substrates Candidemia
phycomycosis; thyrotoxicosis (section 10.2). nancy, breast feeding. e.g. ergotamine, dihydroergotamine, siroli- 3-4mg/ 200mg
and invasive 100mg q12h
kg*q12h q12h
Contra-indications: Hypersensitivity to Interactions: Rifampicin, cimetidine mus. CYP3A4 inducers e.g. carbamazepine, candidiasis
iodides; pregnancy (Appendix 2); breast-feed- Adverse effects: GI symptoms such as fullness, rifampicin, phenobarbital, ritonavir, efavirenz Esophageal 200mg 100mg
candidiasis– q12h q12h
ing (Appendix 3); acute bronchitis or active mild abdominal pain; skin reactions such as (reduced levels of voriconazole). Avoid co-ad- Scedosporiosis 4mg/kg 200mg
tuberculosis. rash, urticaria. ministration with St. John’s Wort. Children 100mg q12h
and Fusariosis q12h q12h
Precautions: Addison disease; cardiac disease; Nursing action: Teach patient symptoms of (<2 years). *Dose depends on the severity and nature of the infection.
hyperthyroidism; myotonia congenita; renal liver dysfunction viz unusual fatigue, jaundice, Precautions: Hypersensitivity to other azoles. Maintenance dosage adjustment: Depending
EMDEX
impairment. dark urine or pale stools, anorexia, vomiting Proarrhythmic conditions e.g. congenital or on response and tolerance, may increase dose
Adverse effects: Goitre, hypothyroidism, and to notify physician if they occur. acquired QT-prolongation, cardiomyopathy, from 200 mg q12h to 300 mg q12h (patients
hyperthyroidism; hypersensitivity reactions; io- Dose: By mouth, Adult, 125 mg twice a day sinus bradycardia, existing symptomatic ar- >40 kg) or from 100 mg q12h to 150 mg q12h
dism characterized by metallic taste, increased or 250 mg once a day; duration of rhythmias, concomitant medication known to (patients <40 kg). IV maintenance dose of 4
salivation, coryza–like symptoms and irrita- treatment depends on the indication prolong QT interval. Infusion-related reactions, mg/kg q12h may be reduced to 3 mg/kg q12h
tion and swelling of the eyes (resulting from and severity Tinea pedis: 2-6 weeks predominantly flushing and nausea (may stop if not tolerated. Duration of therapy should be
prolonged administration); also gastrointes- Tinea corporis, cruris: 2-4 weeks treatment). Monitor hepatic and renal func- based on the severity of the patients’s under-
tinal disturbances and diarrhoea; pulmonary Cutaneous candidiasis: 2-4 weeks tions regularly. Avoid sunlight. Pregnancy & lying disease, recovery from immunosuppres-
oedema, bronchitis; skin reactions; depression, Onychomycosis: 6 weeks – 3 months lactation. Women of child-bearing potential sion, and clinical response.
insomnia, impotence, headache reported. Child: not yet recommemded. must always use effective contraception during
POM VFEND® (Pfizer)
Dose: Sporotrichosis and subcutaneous phy- POM Terbinafine (EDL 5.11.2/Restricted List)
treatment. May cause blurred vision (avoid
Tablet, Voriconazole 50 mg; white f-c tab.
comycosis, by mouth, ADULT initially Tablet, Terbinafine (as HCl) 250 mg. driving or operating machinery). 50 mg – 14’s.
1 mL 3 times daily, increased by 1 Interactions: Voricanozole is a substrate and Caplet, Voriconazole 200 mg; white f-c cap-
mL daily, depending on tolerance, to POM EXIFINE® (Phillips/Dr. Reddy’s) inhibitor of CYP2C19, CYP2C9 and CYP3A4. sule-shaped tab.
Tablet, Terbinafine (as HCl) 250 mg; uncoated tab.
10 mL daily; continue treatment for There is potential for Voricanozole to affect, 200 mg – 14’s.
250 mg – 4’s (in blister).
at least 4 weeks after resolution or or be affected by other drugs, metabolised by Powder for IV infusion, Voriconazole 200 mg;
stabilization of lesions. POM TERBIMAX® (Evans) these enzymes. lyophilized powder for reconstitution in a single
Note: If signs of iodism occur, suspend treatment Tablet, Terbinafine 250 mg. Adverse effects: Most commonly visual dis- use vial.
temporarily and restart after a few days at lower 250 mg – 10’s. Pack: 200 mg x 1’s (in single use vial).
turbances, headache, abdominal pain, nausea,
dosage. vomiting, diarrhoea, rash, fever, peripheral
POM Potassium iodide (WMF 6.3)
VORICONAZOLE
edema. Less common are back pain, elevated 9.3 Antiprotozoal drugs
Saturated solution, Potassium iodide. Therapeutic category: Systemic antifungal liver function tests, pancytopenia, bone marrow 9.3.1 Antimalarial drugs
agent, triazole derivative. depression, leukopenia, thrombocytopenia, 9.3.2 Antiamoebic, antigiardial and antitrichomonal
TERBINAFINE Pharmacology: Voriconazole is a triazole purpura, anaemia, dizziness, confusional state, drugs
Therapeutic category: Broad spectrum anti- broad-spectrum antifungal agent. Like other tremor, agitation, paraesthesia, acute respiratory 9.3.3 Antileishmanial drugs
azole antifungal agents, voriconazole acts by 9.3.4 Antitrypanosomal drugs
fungal agent distress syndrome, pulmonary oedema, res-
inhibiting the CYP 450-dependent enzyme 9.3.5 Antipneumocystosis and antitoxoplasmosis
Pharmacology: Terbinafine is an allylamine piratory distress, chest pain, acute renal failure, drugs
which has a broad spectrum of antifungal 14α-sterol demethylase, thus inhibiting a crit- pruritus, maculopapular rash, photosensitivity
activity. It acts by interfering specifically with ical step in the ergosterol biosynthesis pathway skin reaction, alopecia, exfoliative dermatitis,
that is essential for a functional fungal cell wall 9.3.1 Antimalarial drugs
fungal sterol biosynthesis at an early step hypoglycaemia, hypokalaemia, gastroenteritis,
resulting in a deficiency in ergosterol, intra- membrane as well as for sustained growth. It influenza-like illness, hypotension, thrombo- See the detailed Guidelines for the Management of
is rapidly absorbed after oral administration; phlebitis, jaundice, mood disorders, Injection Malaria in Nigeria in EMDEX Vol. 3.
cellular accumulation of squalene and fungal
cell death. At low concentrations terbinafine is Cmax is achieved 1-2 hours after dosing in the site reaction/inflammation.
fasted state. It is recommended that voricona- 9.3.1.1 Artemisinin-based combination therapies
fungicidal against dermatophytes, moulds and Loading Dose Regimen (first 24 hours): (ACTs)
certain dimorphic fungi. The activity against zole be given at least 1 hour before or at least Oral dose 9.3.1.2 Drugs for the treatment of severe malaria
yeasts is fungicidal or fungistatic, depending 1 hour after a meal. Absorption is not affected Infection IV dose Patients Patients 9.3.1.3 Agents for chemoprophylaxis
by changes in gastric pH. Metabolism occurs ≥40 kg <40 kg
9.3.1.4 Other antimalarial drugs
428 | 9.3.1.1 Artemisinin-based combination therapies (ACTs) 9.3.1.1 Artemisinin-based combination therapies (ACTs) | 429
9.3.1.1 Artemisinin-based Tablet, Artemether 20 mg, Lumefantrine 120 mg. yellow tab. marked ‘MBN’ on one side and ‘ART’ on >14-24 3 ½ ½ ½ ½ ½ ½
combination therapies (ACTs) Pack: 1 x 6’s. the reverse. >24-34 4.5 ¾ ¾ ¾ ¾ ¾ ¾
Injection, Artemether 80 mg; in oily base. Pack: 12’s (in a sachet). >34 6 1 1 1 1 1 1
ARTEMETHER plus LUMEFANTRINE Pack: 1 mL x 6’s (in amp).
POM ARTELUMEX® (Vitabiotics) POM Artemether plus Lumefantrine (Crystal)
Therapeutic category: Antimalarial; Artemis- POM ACTPRO AL® (Synergy) Tablet, Artemether 20 mg, lumefantrine 120 mg. Tablet, Artemether 80 mg, lumefantrine 480 mg;
inin-based combination therapy (ACT). Tablet, Artemether 20 mg, lumefantrine 120 mg. Pack: 3 x 8’s. light yellow tab. marked "Crystal Artemether 80 +
Indications: Treatment of uncomplicated Pack: 2 x 6’s Lumefantrine 480 mg"
POM ARTEMEF® (Evans)
Tablet, (Forte), Artemether 80 mg, lumefantrine
malaria caused by P. falciparum alone or with Tablet, Artemether 20 mg, lumefantrine 120 mg; POM ARTERINE® (Hochiez)
480 mg
other Plasmodium spp. in areas with significant uncoated tab. Tablet, (Forte), Artemether 80 mg, lumefantrine
Pack: 1 x 6’s
drug resistance (see also notes in EMDEX Vol. 3). Pack: 8’s (in blister) 480 mg
Suspension, Artemether 180 mg, lumefantrine 1080
Contra-indications: Breastfeeding (Appendix Dose Pack: 1 x 6’s
mg per 60 mL.
3); history of arrhythmias, of clinically relevant Pack: 60 mL Therapy regime (Tablets) Oral suspension, Artemether 180 mg, lumefantrine
Body Total
Day1 Day 2 Day 3 1080 mg per 60 mL.
bradycardia, and of congestive heart failure ac- POM AMATEM® (Elbe) weight (kg) (tablets)
0h 8h 24h 36h 48h 60h
companied by reduced left ventricular ejection Tablet, Artemether 20 mg, lumefantrine 120 mg; ≥5<15 6 1 1 1 1 1 1 POM ARTHEGET® (Zoomota)
fraction; family history of sudden death or of yellow tab. marked “AMATEM” ≥15<25 12 2 2 2 2 2 2 Tablet, Artemether 20 mg, lumefantrine 120 mg.
congenital prolongation of QTc interval (also Pack: 24’s ≥25<35 18 3 3 3 3 3 3 Pack: 24’s (in blisters).
see Precautions). Tablet, Artemether 80 mg, lumefantrine 480 mg; ≥35 24 4 4 4 4 4 4 Oral suspension, (Junior), Artemether 15 mg, lume-
Precautions: First trimester of pregnancy; yellow tab. marked “AMATEM” fantrine 90 mg per 5 mL; powder for reconstitution.
Pack: 6’s POM ARTEMEFAN® (Diamond Remedies) Pack: 90 mL.
electrolyte disturbances, concomitant admin-
Suspension, Artemether 180 mg, lumefantrine Tablet, Artemether 80 mg, lumefantrine 480 mg.
istration of drugs that prolong QT interval; Pack: 6’s (in blister) POM ARTHEGET® DS (Zoomota)
1080 mg; dry powder which turns light yellow on Tablet, Artemether 40 mg, lumefantrine 240 mg.
monitor patients unable to take food (greater
EMDEX
reconstitution. POM ARTEMELUM® (Juhel) Pack: 8’s; 12’s; 24’s (in blisters).
risk of recrudescence); severe renal impairment Pack: 60 mL Tablet, Artemether 20 mg, lumefantrin 120 mg.
(Appendix 4) or hepatic impairment (Appendix POM ARTHEGET® EZ (Zoomota)
POM AQUAMAL® (Pinnacle) Tablet, (Forte), Artemether 80 mg, lumefantrin
5); interactions: Appendix 1. 480 mg. Tablet, Artemether 80 mg, lumefantrine 480 mg.
Adverse effects: Abdominal pain, anorexia, Suspension, Artemether 180 mg, lumefantrine 1080 Pack: 6’s (in blisters).
mg per 60 mL Suspension, Artemether 180 mg, lumefantrin 1080
diarrhoea, nausea and vomiting; headache, mg per 60 mL; yellow powder for reconstitution. POM ARTHEMED® (Fidson)
Pack: 60 mL
dizziness, sleep disorders; palpitation; ar- Pack: 60 mL. Tablet, Artemether 20 mg, lumefantrine 120 mg.
thralgia, myalgia; cough; asthenia, fatigue; POM AQUAMAL® QS (Pinnacle) Pack: 1 x 12’s (in blister)
Tablet, Artemether 80 mg, lumefantrine 480 mg. POM Artemetin Beta Plus (Beta Drugs)
pruritus, rash. Tablet, Artemether 80 mg, lumefantrine 480 mg;
Pack: 6’s (in blisters) POM ARTORONATE® (Toro)
Dose: Treatment of uncomplicated falciparum f-c tab. Tablet, Artemether 40 mg, lumefantrine 250 mg.
malaria, by mouth, ADULT and CHILD POM ARCOFAN® (Pharmgate) Pack: 6’s (in blisters)
over 12 years and body weight over Tablet, Artemether 20 mg, Lumefantrine 120 mg Oral suspension, Artemether 180 mg, lumefantrine POM ARTRIN® (Medreich)
35 kg, initially 4 tablets followed by Pack: 3 x 8’s 1080 mg per 60 mL Tablet, Artemether 20 mg, lumefantrine 120 mg.
5 further doses of 4 tablets each at POM ARCOFAN® DS (Pharmgate) Pack: 60 mL POM ASKAMETHER® (Diamond Remedies)
8, 24, 36, 48 and 60 hours (total 24 Tablet, Artemether 80 mg, Lumenfantrine 480 mg. POM Artemether-Plus (Neros) Tablet, Artemether 20 mg, lumefantrine 120 mg
tablets over 60 hours); Pack: 1 x 6’s. Oral suspension, Artemether 180 mg, lumefantrine Pack: 3 x 8’s (in blisters)
CHILD body weight 5–14 kg, initially POM ARENAX® Plus (Swipha) 1080 mg per 60 mL; powder for reconstitution. POM AUROTHER® (Nalis)
1 tablet followed by 5 further doses Tablet, Artemether 20 mg, lumefantrine 120 mg Pack: 60 mL bottle. Tablet, (forte), Artemether 80 mg, lumefantrine
of 1 tablet each at 8, 24, 36, 48 and 60 Pack: 2 x 12’s; 3 x 8’s. Dose: Add potable water to 60 mI mark, shake 480 mg
hours (total 6 tablets over 60 hours); well before use. Take orally with meal. The
POM ARMETRINE® (Estate drugs) dosage for children is based on their b.wt POM BG MAL® (BG Pharmacy)
body weight 15–24 kg, initially 2 Tablet, Artemether 20 mg, lumefantrine 120 mg. Tablet, Artemether 20 mg, lumefantrine 120 mg.
tablets followed by 5 further doses of Dose (mL)
Pack: 3 x 8’s. Body weight Pack: 3 x 8’s; 1 x 6’s.
Day 1 Day 2 Day 3
2 tablets each at 8, 24, 36, 48 and 60 Tablet ,(Plus), Artemether 40 mg, lumefantrine
POM ART-LUF® (Goldmoore) 5 kg 7 mL 7 mL 7 mL
hours (total 12 tablets over 60 hours); >5-7.5 kg 10 mL 10 mL 10 mL 240 mg
Tablet, Artemether 20 mg, lumefantrine 120 mg.
body weight 25–34 kg, initially 3 >7.5-10 kg 14 mL 14 mL 14 mL Pack: 3 x 8’s; 1 x 6’s.
Pack: 3 x 8’s (in blisters) Tablet, (Forte), Artemether 80 mg, lumefantrine
tablets followed by 5 further doses of >10-15 kg 20 mL 20 mL 20 mL
3 tablets each at 8, 24, 36, 48 and 60 POM ARTEFAN® (Solution Pharma) Tablet, Artemether 80 mg, lumefantrine 480 mg 480 mg
Tablet, Artemether 40 mg, lumefantrine 240 mg; Pack: 3 x 8’s; 1 x 6’s.
hours (total 18 tablets over 60 hours). Pack: 1 x 6’s (in blister).
yellowish tab. Dose: Take orally with meal. Adult Suspension, Artemether 180 mg, lumefantrine 1080
Administration: Take tablets with food; repeat dose
Pack: 1 x 12’s (in blisters). mg per 60 mL.
if vomiting occurs within 1 hour of administration. Therapy regime (tablets)
Suspension, Artemether 180 mg, lumefantrine Total Pack: 60 mL.
Day 1 Day 2 Day 3
POM Artemether plus Lumefantrine (WMF 6.5.3) 1080 mg (tablets)
0h 8h 24h 36h 48h 60h POM CANTHREM® (Canopus)
Tablet, Artemether 20 mg with lumefantrine 120 mg Pack: 60 mL. 6 1 1 1 1 1 1 Tablet, Artemether 20 mg, Lumefantrine 120 mg
POM Artemether plus Lumefantrine (EDL 5.7) POM ARTEFORTH® (PharmacyPlus) Children (based on body weight) Pack: 3 x 8’s.
Tablet, Artemether 20 mg, lumefantrine 120 mg. Tablet, Artemether 80 mg, lumefantrine 480 mg Therapy regime (Tablets)
Body Total POM CELOLUTHER® (JB Pharma)
Oral liquid, Artemether 15 mg, lumefantrine 90 mg Pack: 6’s (in blisters). Day 1 Day 2 Day 3
wt (kg) (tablets) Tablet, Artemether 20 mg, lumefantrine 120 mg.
per 5 mL. 0h 8h 24h 36h 48h 60h
POM ARTELUM® (May & Baker) Pack: 3 x 8’s (In blister).
10-14 1.5 ¼ ¼ ¼ ¼ ¼ ¼
POM ACITHER® (Foundation) Tablet, Artemether 40 mg, lumefantrine 240 mg; Suspension, Artemether 180 mg, lumefantrine 1080
mg per 60 mL; dry powder for reconstitution. Tablet, Artemether 20 mg, lumefantrine 120 mg reconstitution. Pack: 60 mL.
Pack: 60 mL. Pack: 60 mL. Suppository, Artemether 20 mg, lumefantrine 120
POM DRUTEMAL® Plus (Drugfield)
Oral suspension, (80/480 mg), Artemether 80 mg, mg.
POM CO-ARTESIANE® (Dafra) Tablet, Artemether 40 mg, lumefantrine 240 mg
lumefantrine 480 mg per 5 mL Pack: 1 x 6’s.
Oral Suspension, Artemether 15 mg, lumefantrine Pack: 12’s (in blisters)
Pack: 60 mL Tablet, (Dispersible), Artemether 20 mg, lumenfan-
90 mg per 5 mL; dry powder for reconstitution with Tablet, (DS), Artemether 80 mg,lumefantrine 480 mg
trine 120 mg
water to form yellow susp. with coconut flavour. Pack: 6’s (in blisters) POM GVITHER® Plus (Seagreen)
Pack: 6’s
Pack: 60 mL; 120 mL. Oral suspension, Artemether 20 mg, lumefantrine Dispersible tablet, Artemether 20 mg, lumefantrine
Dose: For Infant and Children Only (5-14 kg or 6
Dose: Child, by mouth, usually, 4 mg Artemether/kg 120 mg per 5 mL; after reconstitution. 120 mg
months to 3 years of age)
b. wt in combination with Lumefantrine per Pack: 60 mL Pack: 6’s
day for 3 consecutive days as follows: 5 kg, Tablet, (20/120 mg), Artemether 20 mg, lumefantrine Weight
Total Therapy regime (Tablets)
POM DUOTHER® (Pharma Ethics) (Kg)
7 mL once daily; 7.5 kg, 10 mL once daily; 120 mg; f-c tab
Tablet , (dispersible), Artemether 20 mg, lumefan- Day 1 Day 2 Day 3
10 kg, 14 mL once daily; 15 kg, 20 mL once Pack: 3 x 8’s (in blisters)
trine 120 mg. 0h 8h 24h 36h 48h 60h
daily. To be repeated for 3 consecutive days. Tablet, (40/240 mg), Artemether 40 mg, lumefantrine 5-14 6
Pack: 4 x 6’s
240 mg; f-c tab 1 1 1 1 1 1
POM COARTEM® (Novartis)
POM ERITHER-L® (Onifam) Pack: 2 x 6’s (in blisters)
Tablet, Artemether 20 mg, lumefantrine 120 mg Note: Second dose to be taken strictly after 8 hours
Tablet, Artemether 20 mg, lumefantrine 120 mg Tablet, (80/480 mg), Artemether 80 mg, lumefantrine
Pack: 24’s of first dose. After each dose, give your child fatty
Pack: 3 x 8’s 480 mg; f-c tab
Indications: Treatment of acute uncomplicated meal or something to eat or drink
Plasmodium falciparum malaria. POM FABITHER® (FAB) POM LUFART® (E-Globa)
Dose: Tablet, Artemether/lumefantrine 140 mg POM HATHERLEY® (Next Generation)
Tablet, Artemether 20 mg, lumefantrine 120 mg;
Therapy regime (Tablets) Pack: 3 x 8’s (calendar pack) Tablet, Artemether 80 mg, lumefantrine 480 mg
Body wt Total light yellow tab marked “CL”
Day 1 Day 2 Day 3 Suspension, Artemether/lumefantrine 1260 mg/60 Pack: 6’s
(kg) (tablets) Pack: 3 x 8’s
0h 8h 24h 36h 48h 60h mL Oral suspension, Artemether 180 mg, lumefantrine
EMDEX
≥5<15 6 1 1 1 1 1 1 Pack: 60 mL 1080 mg per 60 mL POM LUFART QS® (E-Globa)
≥15<25 12 2 2 2 2 2 2 Pack: 1 bottle Tablet, Artemether 40 mg, lumefantrine 240 mg
≥25<35 18 3 3 3 3 3 3 POM FAMTER® (Maydon) Pack: 1 x 6’s (in blisters).
Suspension, Artemether 20 mg, lumefantrine 120 POM HILACT® Plus (CG Biostadt)
≥35 24 4 4 4 4 4 4 Tablet, Artemether 80 mg, lumefantrine 480 mg.
mg. Tablet, Artemether 20 mg, lumefantrine 120 mg.
POM COATAL® (Geneith) Pack: 1 bottle in each box. Pack: 24’s. POM LUTHER® (Hovid)
Tablet, Artemether 20 mg, lumefantrine 120 mg Direction for reconstitution: To make 60 mL sus- Tablet, (40/240 mg), Artemether 40 mg, lumefan-
POM KART-LU® (Kayhelt)
Pack: 10 x 24’s. pension, add 45 mL water, tighten cap, invert bottle trine 240 mg
Tablet, (40/240 mg), Artemether 40 mg, lumefantrine
Tablet, (forte), Artemether 80 mg, lumefantrine and shake until uniforms suspension is formed. Then Pack: 2 x 6’s
240 mg; f-c tab
480 mg. slowly, add more water up to the 60 mL arrow mark Tablet, (80/480 mg), Artemether 80 mg, lumefan-
Pack: 6’s (in blisters)
Pack: 10 x 6’s and shake well. Use only boiled and cooled water. trine 480 mg
Tablet, (80/480 mg), Artemether 80 mg, lumefantrine
Oral suspension, Artemether, lumefantrine; powder Use the prepared suspension within 7 days. Pack: 1 x 6’s
480 mg; f-c tab
for reconstitution. POM FAVERID® Junior (Solidum) Pack: 6’s (in blisters) POM LUMAL® (SKG)
Granules, Artemether 20 mg, lumefantrine 120 mg; Tablet, Artemether 20 mg, lumefantrine 120 mg; Tablet, Artemether 40 mg, lumefantrine 240 mg;
in sachets. POM LA-TESEN®(Afrab-Chem)
dispersible tab. yellow scored tab. marked ‘40/240’ on one side and
Pack: 10 x 6’s Oral drops, Artemether 20 mg, lumefantrine 120 mg.
Pack: 12’s ‘LE’ on the reverse.
Pack: 8 mL with dropper.
POM CO-DABAMAL® (Dabak) Pack: 12’s
POM FAVERID® Senior (Solidum) Suspension, Artemether 20 mg, lumefantrine 120
Tablet, Artemether 20 mg, lumefantrine 120 mg Tablet, Artemether 80 mg, lumefantrine 480 mg;
Tablet, Artemether 80 mg, lumefantrine 480 mg; mg per 5 mL.
Pack: 24’s (in blister) yellow scored tab. marked ‘80/480’ on one side and
f-c tab. Pack: 60 mL.
Tablet, (Forte), Artemether 80 mg, lumefantrine ‘LDS’ on the reverse.
Pack: 6’s Tablet, Artemether 40 mg, lumefantrine 240 mg
480 mg Pack: 6’s
Pack: 12’s.
Pack: 1 x 6’s POM HAVAX® (Embassy) Oral suspension, Artemether 180 mg, lumefantrine
Suspension, Artemether 180 mg, lumefantrine 1080 POM LAROT® (Canopus) 1080 mg per 60 mL; yellow granular powder.
POM COFETRAN® (Chanmedi) mg per 60 mL Tablet, Artemether 80 mg, Lumefantrine 480 mg Pack: 60 mL
Tablet, Artemether 20 mg, lumefantrine 120 mg. Pack: 60 mL Pack: 1 x 6’s
Pack: 2 x 12’s. POM LUMERAX® (IPCA)
POM GLOATEM® (Global Healthcare) POM LOKMAL® (Emzor) Tablet, Artemether 20 mg, lumefantrine 120 mg.
POM COMBISUNATE® (Nalis) Tablet, Artemether 20 mg, lumefantrine 120 mg; Tablet, (20/120 mg), Artemether 20 mg, Lumefan- Pack: 8’s.
Tablet ,(20/120 mg), Artemether 20 mg, lumefantrine f-c tabs. trine 120 mg
120 mg; yellow uncoated tab. POM LUMETHER® (Therapeutic)
Pack: 4 x 6’s (in blisters). Pack: 6 x 2’s; 6 x 4’s (in blister)
Pack: 6’s; 8’s; 12’s; 18’s; 24’s (in blisters) Adult, Artemether 20 mg, lumefantrine 120 mg.
Tablet, (Dispersible) Artemether 20 mg, lumefan- Caplet, (80/480 mg), Artemether 80 mg, Lumefan-
Tablet ,(40/240 mg), Artemether 40 mg, lumefantrine Pack: 24’s (in blister)
trine 120 mg trine 480 mg
240 mg; yellow uncoated tab. Paediatric dispersible tablet, Artemether 10 mg,
Pack: 24’s Pack: 6’s (in blister)
Pack: 24’s (in blisters) lumefantrine 60 mg.
Tablet, (40/240 mg)), Artemether 40 mg, lumefan- Paediatric suspension, Artemether 180 mg, Lumefan-
Caplet, (60/360 mg), Artemether 60 mg, lumefantrine Pack: 24’s (in blister)
trine 240 mg trine 1080 mg per 60 mL.
360 mg; yellow uncoated caplet. Pack: 2 x 6’s (in blisters). Pack: 60 mL POM MALAGARD® (Crowther)
Pack: 6’s (in blisters) Tablet, (80/480 mg), Artemether 80 mg, lumefantrine Tablet, Artemether 20 mg, lumefantrine 120 mg
Caplet, (80/480 mg), Artemether 80 mg, lumefantrine POM LONART® (Greenlife)
480 mg; f-c tab. Pack: 3 x 8’s.
480 mg; yellow uncoated caplet. Tablet, Artemether 20 mg, lumefantrine 120 mg
Pack: 6’s (in blisters) Pack: 3 x 8’s. POM MALASTOP® (Mark)
Oral suspension, (20/120 mg), Artemether 20 mg,
Oral suspension, Artemether 180 mg, lumefantrine Tablet, Artemether 20 mg, lumefantrine 120 mg
POM COMBISUNATE® Dispersible (Nalis) lumefantrine 120 mg per 5 mL; dry powder for
1080 mg per 60 mL. Pack: 3 x 8’s
Oral suspension, Artemether 180 mg, lumefantrine Tablet, Artemether 40 mg, lumefantrine 240 mg POM ZOOMAL® (Zoomota) powder for reconstitution in sachets.
1080 mg per 60 mL Pack: 12’s Dispersible tablet, (20/120 mg), Artemether 20 mg, Combipack: 6’s (3 Artesunate sachets + 3 Amodi-
lumefantrine 120 mg aquine sachets)
POM MALFANTRIN® Plus (N.C.I) POM SMT® (Jubilee)
Pack: Dose: Child (1-6 years), 1 Amodiaquine sachet +
Capsule, Artemether 40 mg, lumefantrine 240 mg. Tablet, Artemether 20 mg, lumefantrine 120 mg
Dispersible tablet, (80/480 mg), Artemether 80 mg, 1 Artesunate sachet to be dissolved in 30
Pack: 2 x 10’s. Pack: 16’s.
lumefantrine 480 mg mL water and taken once daily for 3 con-
POM MENFANCIL® (Pacmai). POM SOMAL® (Jopan) Pack: secutive days.
Tablet, Artemether 80 mg, lumefantrine 480 mg; Tablet ,(Forte), Artemether 80 mg, lumefantrine 480 Oral suspension, Artemether 180 mg, lumefantrine Paediatric Powder, Amodiaquine 75 mg + Artesunate
f-c tab. mg; yellow scored tab. marked ‘JOPAN’ 1080 mg; light yellow granules. 25 mg; powder for reconstitution in sachets.
Pack: 1 x 6’s (in blisters) Pack: 1 x 6’s (in blisters). Pack: Combipack: 6’s (3 Artesunate sachets + 3 Amodi-
Tablet, Artemether 20 mg, lumefantrine 120 mg; aquine sachets)
POM MENFANCIL® Kid (Pacmai) Dose: Child (<1 year), 1 Amodiaquine sachet + 1
yellow scored tab. marked ‘JOPAN’ ARTESUNATE plus AMODIAQUINE
Tablet, Artemether 40 mg, lumefantrine 240 mg; Artesunate sachet to be dissolved in 30
Pack: 3 x 8’s (in blisters). Note: Available as a fixed-dose formulation
f-c tab. mL water and taken once daily for 3 con-
Pack: 2 x 6’s (in blisters) POM SOMAL® Plus (Jopan) with tablets containing 25/67.5 mg, 50/135 secutive days.
Suspension, Artemether 180 mg, lumefantrine Tablet, Artemether 40 mg, lumefantrine 240 mg; mg or 100/270 mg of artesunate and amodi-
1080 mg yellow scored tab. marked ‘JOPAN’ aquine. Blister packs of separate scored tablets POM ARMACT® (Medreich)
Pack: 60 mL Pack: 2 x 6’s (in blisters). containing 50 mg of artesunate and 153 mg Tablets, Artesunate 50 mg + Amodiaquine HCl 200
mg equiv. 153.1 mg Amodiaquine base.
POM NANCIMAL QS® (Teta) POM TAMA-ACT® (Tamar & Pharez) base of amodiaquine, respectively, are also
Dose: Based on body weight, 4 mg/kg Artesunate
Tablet, Artemether 80 mg, lumefantrine 480 mg; Tablet, Artemether 40 mg, lumefantrine 240 mg available. According to WHO, the combination + 10 mg/kg Amodiaquine HCl to be taken
uncoated tab. Pack: 2x 6's is effective only where 28-day cure rates with simultaneously once daily for 3 consec-
Pack: 1 x 6’s (in blisters) amodiaquine monotherapy exceeded 80%. utive days
POM TAMETHER® (Vixa)
POM NARTEL® (NASDMU) Tablet, (20/120 mg), Artemether 20 mg, lumefantrine Continued availability of chloroquine and amo-
EMDEX
1st day 2nd day 3rd day
Tablet, Artemether 40mg, lumefantrine 240 mg; 120 mg; light yellow tab. marked ‘TAMETHER’ on diaquine monotherapies may worsen resist-
Child under 1 year (<10
marked “NART” on one side and “NASDMU” on both sides. ance and reduce efficacy of the combination. kg)
½ tablet ½ tablet ½ tablet
reverse side. Pack: 24’s Dose: WHO recommends a target dose of 4 Child (1-7 years) (weight
Pack: 12’s Tablet ,(40/240 mg), Artemether 40 mg, lumefantrine 1 tablet 1 tablet 1 tablet
mg/kg/day artesunate and 10 mg/ 10-20 kg)
Suspension, Artemether 180 mg, lumefantrine 1080 240 mg kg/day amodiaquine once a day for 3 Child (7-13 years) (weight
2 tablets 2 tablets 2 tablets
mg; cap with NASDMU logo. Pack: 12’s 21-40 kg)
days, with a therapeutic dose range
Pack: 60 mL Tablet ,(80/480 mg), Artemether 80 mg, lumefan- Adult (>14 years) 4 tablets 4 tablets 4 tablets
trine 480 mg. between 2–10 mg/kg/day artesunate
POM NIMARTEM® (Neimeth) Administration: Swallow the tablet with a little
Pack: 6’s and 7.5–15 mg/kg/dose amodi-
Tablet, Artemether 20 mg, lumefantrine 120 mg water after a meal. Tablets should be crushed and
Powder, Artemether 20 mg, lumefantrine 120 mg aquine. given with water to the younger children.
Pack: 6’s; 12’s; 24’s
Pack: 6’s (in sachets) POM ACT-A® (Elbe)
POM OGAMAL® (Lifeback) Oral suspension, Artemether 240 mg, lumefantrine POM AROFEN® (Vixa)
Tablets, Artesunate 200 mg + Amodiaquine 600 mg Tablets, Artesunate 200 mg + Amodiaquine 600 mg
Tablet, Artemether 20 mg, lumefantrine 120 mg; 1440 mg; granule for reconstitution. Combipack: 6’s (3 Amodiaquine tablets + 3 Artesu-
f-c yellow tab. Combipack: 6’s.
POM TERMAX® (Placeware) nate tablets). Tablets, Artesunate 50 mg + Amodiaquine 150 mg.
Tablet, QS, Artemether 80 mg, lumefantrine 480 mg;
Tablet, Artemether 20 mg, lumefantrine 120 mg POM AMONATE® FDC (Dafra) Combipack: 2 x 12’s.
f-c yellow tab.
Pack: 3 x 8’s Tablet, (Adult), Artesunate 100 mg, Amodiaquine
Suspension, Artemether 180 mg, lumefantrine 1080 POM ARSUGIN® (Beta Drugs)
mg per mL POM UPLUFA® Plus (Award Global) 306.2 mg. Tablet, Artesunate 200 mg, Amodiaquine 600 mg
Pack: 60 mL Capsule, Artemether 40 mg, lumefantrine 240 mg; Pack: 6’s Pack: 3 x 3’s.
soft gelatin cap. Tablet, (Junior), Artesunate 50 mg, Amodiaquine
POM PEMAMETRE® (Pemason) 153.1 mg. POM ARTEMODIAQUINE® (Adpharm)
Pack:1 x 12’s
Tablet, Artemether 20mg, lumefantrine 120mg Pack: 6’s Tablet, Amodiaquine 600 mg + Artesunate 200 mg
Syrup, Artemether 180 mg, lumefantrine 1080 mg POM V-MARTEM® (Vitahealth) Combipack : 1 x 6’s
per 60 mL Tablet, Artemether 20 mg, lumefantrine 120 mg POM ANATE® (Astra) Granules, Amodiaquine base 75 mg + Artesunate
; f-c tab Tablets, (Adult), Amodiaquine 600 mg + Artesunate powder 25 mg
POM PESRIDON® (Pharmabase) 200 mg.
Pack: 6’s; 12’s;18’s; 24’s (in blisters) Combipack: 1 x 6’s
Tablet, Artemether 20 mg, lumefantrine 120 mg Combipack: 6’s (3 Artesunate tablets + 3 Amodi-
Tablet, (DS), Artemether 80 mg, lumefantrine 480
Pack: 3 x 8’s (in blister) aquine tablets). POM ARTEPLUS® Combi (Eutrix)
mg; f-c tab
Suspension, Artemether 180 mg, lumefantrine 1080 Dose: Adult (>14 years), 1 Amodiaquine tablet + 1 Tablets, (Adult), Artesunate 100 mg + Amodiaquine
mg per 60 mL; dry pineapple flavoured powder Artesunate tablet to be taken together once base 300 mg.
Suspension, Artemether 180 mg, lumefantrine 1080
which turns yellow on reconstitution with water. daily for 3 consecutive days. Combipack: 12’s (6 Artesunate tablets + 6 Amodi-
mg per 60 mL
Pack: 60 mL. Note: For patients having difficulties in swallowing, aquine tablets).
Pack: 60 mL
POM PRO-FANTRINE® (Korlyns) the tablets can be crushed and dissolved in water. Dose: Artesunate 4 mg/kg b. wt + Amodiaquine 10
POM VOATHER® (Visko) Tablets, (Junior), Amodiaquine 300 mg + Artesunate mg/kg b. wt.:
Tablet, Artemether 20 mg, lumefantrine 120 mg
Tablet, (Forte), Artemether 80 mg, lumefantrine 100 mg. Adult (>14 years), 2 Artesunate tablets + 2
Tablet, Artemether 40mg, lumefantrine 240 mg
480 mg Combipack: 6’s (3 Artesunate tablets + 3 Amodi- Amodiaquine tablets to be taken simulta-
POM ROBAMAL® (Onifam) Pack: 1 x 6’s aquine tablets). neously with water after meal once daily for
Tablets, Artemether 80 mg, lumefantrine 480 mg; Dose: Child (7-13 years), 1 Amodiaquine tablet + 1 3 consecutive days.
POM VOATHER® Powder (Visko)
yellow f-c tab. Artesunate tablet to be taken together once Note: For adults (especially ages between 14 and
Suspension, Artemether 180mg, lumefantrine
Pack: 1 x 6’s (in alu alu blister) daily for 3 consecutive days. 18) having small body weight, the drug can be
1080mg per 60 mL
POM ROLOTHER® (Rohi) Pack:1x10 Powder, Amodiaquine 150 mg + Artesunate 50 mg; taken in daily divided doses of 12 hours for the 3
days treatment period. For patients having difficul- Tablets, Artesunate 50 mg + Amodiaquine 200 mg ≥ 9 – <18 kg 50mgAS 50mgAS 50mgAS POM DLANATE-C® (Pharmabase)
ties in swallowing, the tablets can be crushed and Combipack: 6’s (3 Artesunate tablets + 3 Amodi- (1-5years)* 135mgAQ 135mgAQ 135mgAQ Tablets, Amodiaquine 150 mg + Artesunate 50 mg
dissolved in water. aquine tablets). ≥ 18 – <36 kg 100mgAS 100mgAS 100mgAS Combipack: 6’s (3 Artesunate tablets + 3 Amodi-
Tablets, (Junior), Artesunate 100 mg + Amodiaquine (6-13years)* 270mgAQ 270mgAQ 270mgAQ aquine tablets).
POM CAMOSUNATE® (Geneith)
base 300 mg. ≥ 36 kg 200mgAS 200gAS 200mgAS Dose: Child (1-6 years), 1 Amodiaquine tablet + 1
Tablets, (Adult), Amodiaquine 600 mg (yellow tab.)
Combipack: 6’s (3 Artesunate tablets + 3 Amodi- (≥14 years)* 540mgAQ 540mgAQ 540mgAQ Artesunate tablet to be taken together 6
+ Artesunate 200 mg (white tab.).
aquine tablets) * if a weight-age mismatch occurs, dosing should be for 3 consecutive days.
Combipack: 6’s (3 white Artesunate tablets + 3
Dose: Child (7-13 years), 1 Artesunate tablet + 1 weight-based. Note: The two tablets which constitute the daily Dla-
yellow Amodiaquine tablets).
Amodiaquine tablet to be taken simulta- AS: artesunate // AQ: amodiaquine nate-C dose must be taken simultaneously without
Dose: Adult (above 14 years), 1 white tablet + 1
neously with water after meal once daily Administration: Not to be taken with a high-fat chewing them with large amount of drinking water.
yellow tablet to be taken together once
for 3 consecutive days. meal (may lower Cmax of artesunate). Swallow For patients having difficulties to swallow the tablets
daily for 3 consecutive days.
Powder, Artesunate 50 mg + Amodiaquine base 150 tablet with water. For patients unable to swallow can be crushed and dispersed in some water.
Tablets ,(Junior), Amodiaquine 300 mg (yellow tab.)
mg; powder for reconstitution in sachets. the tablets whole, the tablets can be dissolved in
+ Artesunate 100 mg (white tab.) POM EFONREX® (Bond)
Combipack: 6’s (3 Artesunate sachets + 3 Amodi- water before administration. The tablets can also be
Combipack: 6’s (3 white Artesunate tablets + 3 Tablet, Artesunate 50 mg (white) + Amodiaquine (as
aquine sachets). crushed and administered with water. Should vom-
yellow Amodiaquine tablets). HCI) 153.8 mg (yellow).
Dose: Child (1-6 years), 1 Artesunate sachet + 1 iting occur within half an hour after dosing, repeat
Dose: Child (7-13 years), 1 white tablet + 1 yellow Pack: (12 white Artesunate + 12 yellow Amodiaquine
Amodiaquine sachet to be dissolved in the dose. In case of further vomiting, treatment for
tablet to be taken together once daily for 3 tablets)
30 mL water and taken once daily for 3 severe malaria should be considered.
consecutive days.
consecutive days. POM FALCIMOD® (Neimeth)
Powder, Amodiaquine 150 mg + Artesunate 50 mg; POM COTEMAL® (Chanmedi)
Note: The sachets can be dissolved in water, mul- Tablet, Artesunate 200 mg, amodiaquine 300 mg
powder for reconstitution in sachets. Tablet, Artesunate 50 mg, Amodiaquine 153.33 mg
tivitamin syrup or fruit drinks and taken once daily Combipack: 9’s
Combipack: 6’s (3 white labelled Artesunate sachets Pack: 12 x 12’s.
after meal.
+ 3 black labelled Amodiaquine sachets) POM FEVACOMB® (Crystal)
Paediatric powder, Artesunate 25 mg + Amodiaquine POM DART® (Swipha)
Dose: Child (1-6 years), 1 white labelled sachet + Tablets, Artesunate 50 mg + Amodiaquine 153.1 mg
EMDEX
base 75 mg; powder for reconstitution in sachets. Caplets, (Adult), Amodiaquine 600 mg (yellow scored
1 black labelled sachet to be dissolved in Combipack: 12 + 12’s; 6 + 6’s; 3 + 3’s.
Combipack: 6’s (3 Artesunate sachets + 3 Amodi- caplet) + Artesunate 200 mg (white scored caplet).
30 mL water and taken once daily for 3
aquine sachets) Combipack: 6’s (3 white Artesunate caplets + 3 POM GLUMET® (Jubilee)
consecutive days.
Dose: Child (<1 year), 1 Artesunate sachet + 1 yellow Amodiaquine caplets). Tablets, Amodiaquine 600 mg + Artesunate 200 mg
Paediatric Powder, Amodiaquine 75 mg + Artesunate
Amodiaquine sachet to be dissolved in Dose: Adult (above 14 years), 1 white Artesunate Combipack: 6’s (3 Artesunate tablets + 3 Amodi-
25 mg; powder for reconstitution in sachets.
30 mL water and taken once daily for 3 caplet + 1 yellow Amodiaquine caplet to aquine tablets).
Combipack: 6’s (3 white labelled Artesunate sachets
consecutive days. be taken together once daily for 3 consec- Dose: Adult, one Amodiaquine tablet + one Artesu-
+ 3 black labelled Amodiaquine sachets)
Note: The sachets can be dissolved in water, mul- utive days. nate tablet to be taken together once daily
Dose: Child (<1 year), 1 white labelled sachet + 1
tivitamin syrup or fruit drinks and taken once daily Tablets, (Child), Amodiaquine 200 mg (yellow scored for 3 consecutive days.
black labelled sachet to be dissolved in
after meal. tablet) + Artesunate 50 mg (white scored tablet).
30 mL water and taken once daily for 3 POM GSUNATE Kit® (Greenlife)
POM ARTESMODIA® (Maydon) consecutive days. Combipack: 6’s (3 white Artesunate tablets + 3 Tablets, Amodiaquine 600 mg + Artesunate 200 mg
Powder, Amodiaquine 150 mg + Artesunate 50 mg; yellow Amodiaquine tablets). Combipack: 6’s (3 Artesunate tablets + 3 Amodi-
POM COARSUCAM® (Sanofi-Aventis) Dose: Child (1-6 years), 1 white Artesunate tablet +
powder for reconstitution in sachets. aquine tablets).
Tablet (25 mg/67.5 mg), Artesunate 25 mg, Amodi- 1 yellow Amodiaquine tablet to be taken
Dose: Child (7-12 years): 1 sachet 2 times daily for 3 Dose: Adult, 1 Artesunate tablet + 1 Amodiaquine
aquine (as HCl) 67.5 mg; bilayer, yellow/white to together once daily for 3 consecutive days.
consecutive days. tablet to be taken together once daily for 3
light yellow, scored tab. marked “AS” on one side Tablet to be crushed in water and taken
Powder, Amodiaquine 75 mg + Aretsunate 25 mg consecutive days.
and “25” on the reverse. immediately.
Dose: Child (<1 year): 1 sachet daily for 3 consecutive
Combipack: 1 x 3’s; 25 x 3’s. POM IBASUNATE® (Elbe)
days; 1-6 years, 1 sachet 2 times daily for 3 POM DIASUNATE® (Emzor)
Tablet, (50 mg/135 mg), Artesunate 50 mg, Amo- Tablet, Artesunate + Amodiaquine.
consecutive days. Caplet, Amodiaquine (as HCl) 300 mg, artesunate
diaquine (as HCl) 135 mg; bilayer, yellow/white to Combipack: 12’s (6 Amodiaquine tablets + 6 Ar-
POM ARTESUNAT®-Plus (Neros) light yellow, scored tab. marked “AS” on one side 100 mg. tesunate tablets).
Tablet, Artesunate 50 mg, Amodiaquine 200 mg and “50” on the reverse. Combipack: 6’s.
Pack: 2 x 12’s (in blisters) Combipack: 1 x 3’s; 25 x 3’s. Dose: By mouth, Adult, 2 caplets once every 24 POM JOARTIN® (JB Pharma)
Tablet, (100 mg/270 mg), Artesunate 100 mg, Amo- hours for 3 days; to be taken after meals or Tablet, Amodiaquine 300 mg + Artesunate 100 mg;
POM ARZEMAL® (Diamond Remedies) at bed time. both uncoated tabs.
diaquine (as HCl) 270 mg; bilayer, yellow/white to
Tablets, Artesunate 200 mg (film-coated) + Amodi- Child (above 6 months old and 5 kg b. wt): Combipack: 4’s (2 Artesunate tablets + 2 Amodi-
light yellow, scored tab. marked “AS” on one side
aquine 600 mg (sunset yellow). Artesunate, 4 mg/kg b. wt and Amodi- aquine tablets).
and “100” on the reverse.
Combipack: 6’s (3 Artesunate tablets + 3 Amodi- aquine, 10 mg/kg b. wt.; to be given for 3
Combipack: 1 x 3’s; 25 x 3’s; 1 x 6’s; 25 x 6’s. POM JUSUNATE® (Juhel)
aquine tablets). consecutive days.
Note: Mottled appearance does not alter the safety Caplets, Artesunate 100 mg + Amodiaquine 300 mg
POM ASAQ® (Sanofi-Aventis) nor the efficay of the tablet. The scoreline only POM DLANATE-A® (Pharmabase) Combipack: 12’s (6 Amodiaquine caplets + 6 Ar-
Tablet, (25 mg/67.5 mg), Artesunate 25 mg, Amodi- facilitates breaking for ease of swallowing and not Tablets, Amodiaquine 600 mg + Artesunate 200 mg tesunate caplets)
aquine 67.5 mg (as HCI). to divide into equal doses. Combipack: 6’s (3 Artesunate tablets + 3 Amodi-
Pack: 3’s (in blisters); 1 x 25’s Dose: Based on body weight, 4 mg/kg (range 2-10 POM LARIMAL® (IPCA)
aquine tablets).
Tablet, (50 mg/135 mg), Artesunate 50 mg, Amodi- mg/kg) Artesunate + 10 mg/kg (range 7.5- Tablets, Amodiaquine base 153.1 mg, yellow tablet
Dose: Adult, 1 Amodiaquine tablet + 1 Artesunate
aquine 135 mg (as HCI). 15 mg/kg) Amodiaquine base to be taken + Artesunate 50 mg, white tablet; in a combination
tablet to be taken together once daily for 3
Pack: 3’s (in blisters); 1 x 25’s simultaneously once daily for 3 days kit containing co-packaged blister packs of Amodi-
consecutive days.
Tablet, (100 mg/270 mg), Artesunate 100 mg, Amo- aquine tablets and Artesunate tablets.
Weight (approx
1st day 2nd day 3rd day Note: A dose must be taken simultaneously without
diaquine 270 mg (as HCI) age range) Pack (Adult): 12 + 12 (in blisters).
chewing them with large amount of drinking water.
Pack: 3’s; 6’s (in blisters); 1 x 25’s 25mgAS 25mgAS 25mgAS Pack (Junior): 6 + 6 (in blisters).
≥ 4.5 – <9 kg For patients having difficulties to swallow the tablets
(2 – 11 months)* 67.5mgAQ 67.5mgAQ 67.5mgAQ
Pack (Child): 3 + 3 (in blisters).
POM ASKASUNATE-AM-C® (Diamond Remedies) can be crushed and dispersed in some water.
Dose: Adult, by mouth, 2 Amodiaquine tablets and
2 Artesunate tablets twice daily for 3 days. Combipack: 24’s (12 Artesunate tablets + 12 Amo- Lactabs (600/750), Artesunate 200 mg + Mefloquine 250 mg.
Child (above 6 months and 5 kg b. wt.), by diaquine tablets). (as HCl) 250 mg. Combipack: 6’s (3 Artesunate tablets + 3 Mefloquine
mouth, 10 mg/kg b.wt of Amodiaquine Dose: Adults: 2 Artesunate tablets + 2 Amodiquine Combipack: 6’s (3 Artesunate lactabs + 3 Mefloquine tablets).
and 4 mg/kg b.wt of Artesunate for 3 days. tablets twice daily for 3 consecutive days. lactabs).
POM MEFLONATE® (Geneith)
Children: For children above 6 months of
POM MALACT® (May & Baker) POM ARFLOQUIN® (Neros) Tablet (600/750), Artesunate 200 mg, mefloquine
age and above 5 kg b.wt, the dosage of
Tablets, Amodiaquine 300 mg + Artesunate 100 mg Caplet/Tablet, (600/750), Artesunate 200 mg (caplet) 250 mg
Artesunate is 4 mg/kg b.wt per day and of
Combipack: 6 Artesunate tablets + 6 Amodiaquine + Mefloquine HCl 250 mg (film-coated tablet)
Amodiaquine is 10 mg/kg b.wt per day in POM THYDOP® (Pharmabase)
caplets). Combipack: 6’s (3 Artesunate caplets + 3 Mefloquine
two divided does daily. Tablets ,(600/750), Artesunate 200 mg + Mefloquine
Dose: Adult (12 years and above), 2 Artesunate tablets).
(as HCl) 250 mg.
tablets + 2 Amodiaquine caplets once daily POM ROMOQUIN® (Rohi)
POM ARSUGIN-M® (Beta Drugs) Combipack: 6’s (3 Artesunate tablets + 3 Mefloquine
for 3 consecutive days. Tablet, Artesunate 100 mg, amodiaquine 300 mg
Tablet, Artesunate 200 mg, Mefloquine 250 mg tablets).
Child (above 6 months of age and above 5 Pack: 12’s
Pack: 3 x 3’s
kg b.wt), the dosage of Artesunate is 4 mg/
POM SUNAD® (Estate drugs) ARTESUNATE plus SULFADOXINE/
kg b.wt and of Amodiaquine is 10 mg/kg POM ARTEQUIN® (Oculus) PYRIMETHAMINE
Tablet, Artesunate 50 mg, Amodiaquine 150 mg.
b.wt for 3 consecutive days. Lactabs ,(600/750), Artesunate 200 mg + Mefloquine
Pack: 1 x 12’s; 2 x 6’s. Note: Available as separate scored tablets
(as HCl) 250 mg.
POM MALMED® Jr (Fidson) Dose: Adult & Child (>13 years): 2 tablets twice a day containing 50 mg of artesunate and tablets
Combipack: 6’s (3 Artesunate lactabs + 3 Mefloquine
Tablets, Artesunate 100 mg + Amodiaquine 300 mg for 3 consecutive days. containing 500 mg of sulfadoxine and 25 mg
lactabs).
Combipack: 6’s (3 Artesunate tablets + 3 Amodi- Child (7-13 years): 1 tablet twice a day for 3
Dose: Adult and child (30-55 kg b. wt), one Artesu- of pyrimethamine. According to WHO, the
aquine tablets). consecutive days; 1 to 6 years, 1 tablet once
nate lactab + one Mefloquine lactab to be combination is effective only where 28-day
Dose: 1 tablet of Artesunate + 1 tablet Amodiaquine a day for 3 consecutive days.
taken together once daily for 3 consecutive cure rates with sulfadoxine-pyrimethamine
to be taken once a day for 3 consecutive
days. alone exceeded 80%. Continued availability
days. ARTESUNATE plus MEFLOQUINE Dosage may be increased for non-immune
EMDEX
widespread use of sulfadoxine-pyrimethamine,
POM MEDNOVAS® Kit (Evans) Therapeutic category: Antimalarial; Artemis- patients and patients with a b. wt >55 kg.
sulfalene plus pyrimethamine and cotrimox-
Tablet, Amodiaquine base153 mg (f-c tab) + Artesu- inin-based combination therapy (ACT). Not recommended for use in patient <30
nate 50 mg (uncoated tab). kg b. wt. azole (trimethoprim plus sulfamethoxazole)
Indications: Treatment of acute uncompli-
Combipack: Children Kit: 6’s (3 white Artesunate Note: The 2 tablets must be taken simultaneously may worsen resistance and reduce efficacy of
cated malaria infection caused by Plasmodium
tablets + 3 yellow Amodiaquine tablets) without chewing them, with a large amount of liquid the combination.
falciparum.
Adolescent Kit: 12’s (6 white Artesunate tablets + 6 and if possible with a meal. For patients having diffi- Dose: WHO recommends a target dose of 4
Contra-indications: Hypersensitivity to ar-
yellow Amodiaquine tablets) culties with swallowing, the tablets can be crushed mg/kg/day artesunate given once a
Adult Kit: 24’s (12 white Artesunate tablets + 12 tesunate or mefloquine, to their chemically and dissolved in some water. day for 3 days and a single adminis-
yellow Amodiaquine tablets). related compounds like other artesunate Lactabs (600/1500), Artesunate 200 mg + Mefloquine tration of 25/1.25 mg/kg sulfadox-
Dose: To be administered every 24 hours for 3 days derivatives, quinine or quinidine or any other (as HCl) 250 mg.
ine-pyrimethamine on day 1.
for the treatment of acute malaria attack ingredient of the tablets. Patients <30 kg b.wt. Combipack: 9’s (3 Artesunate lactabs + 6 Mefloquine
Therapeutic dose range is between
Child (<1 year): Not appropriate for prophylactic use against lactabs).
Dose: Adult and child (>40 kg b. wt), one Artesunate 2–10 mg/kg/day artesunate and
Day 1 ½ tablet Amodiaquine + ½ tablet Artesunate malaria infections.
lactab + two Mefloquine lactabs to be taken 25–70/1.25–3.5 mg/kg sulfadox-
Day 2 ½ tablet Amodiaquine + ½ tablet Artesunate Precautions: Coadministration of halofantrine
Day 3 ½ tablet Amodiaquine + ½ tablet Artesunate together once daily for 3 consecutive days. ine-pyrimethamine.
and mefloquine may increase risk of heart
Child (<6 years): Lactabs ,(300/375), Artesunate 100 mg + Mefloquine
attack. May cause dizziness; ability to drive POM AMALAR® Plus (Elbe)
Day 1 1 tablet Amodiaquine + 1 tablet Artesunate (as HCl) 125 mg.
or operate machinery may be impaired. Preg- Tablets, Artesunate 100 mg + Sulfadoxine 500 mg/
Day 2 1 tablet Amodiaquine + 1 tablet Artesunate Combipack: 6’s (3 Artesunate lactabs + 3 Mefloquine
nancy, lactation Pyrimethamine 25 mg.
Day 3 1 tablet Amodiaquine + 1 tablet Artesunate lactabs).
Adverse effects: Abdominal pain, nausea, Combipack: 9’s (3 Sulfadoxine/Pyrimethamine
Adolescent: Dose: Child (15-30 kg b. wt), one Artesunate lactab +
tablets + 6 Artesunate tablets).
Day 1 2 tablets Amodiaquine + 2 tablets Artesunate vomiting, diarrhoea or loss of appetite, dizzi- one Mefloquine lactab to be taken together
Day 2 2 tablets Amodiaquine + 2 tablets Artesunate ness, headache, trouble in sleeping, fatigue and once daily for 3 consecutive days. POM ARSUGIN-SP® (Beta Drugs)
Day 3 2 tablets Amodiaquine + 2 tablets Artesunate general weakness. Rarely, rash and itching of Tablet, Artesunate 200 mg, Sulfadoxine 500 mg,
POM ARTEQUIN® Paediatric (Oculus)
Adult: the skin may also occur. Pyrimethamine 25 mg.
Pellets, Artesunate 50 mg, Mefloquine (as HCl) 125
Day 1 4 tablets Amodiaquine + 4 tablets Artesunate Pack: 3 x 3’s.
Advice to patients: Complete the full course mg; white to off-white pellets and a fine white to
Day 2 4 tablets Amodiaquine + 4 tablets Artesunate
Day 3 4 tablets Amodiaquine + 4 tablets Artesunate
of therapy. off-white powder in stickpack foil. POM FARENAX® (Swipha)
Dose: WHO recmmends a target dose of 4 Pack: 3 stickpacks Tablets, (Adult), Artesunate 200 mg (white oblong
POM METAMOQUINE® (Drugfield) mg/kg/day artesunate given once Dose: Child (10-20 kg), by mouth, one stickpack as scored tab.) + Sulfadoxine 500 mg/Pyrimethamine
Tablet, Artesunate 100 mg, amodiaquine 306.2 mg a day for 3 days and 25 mg/kg of a single daily dose, for 3 consecutive days. 25 mg (red round tab.).
Pack:1 x 6’s (in blisters) Children weighing >20 kg should use high- Combipack: 6’s (3 oblong Artesunate tablets + 3
mefloquine either split over 2 days
er-dosed preparation. round Sulfadoxine/Pyrimethamine tablets).
POM ODIESHIMATE® (Pharmgate) as 15mg/kg and 10mg/kg or over 3 Not recommended for children <10 kg. Dose: Adult (above 12 years), 3 round tablets of Sul-
Tablet, Artesunate 200 mg, amodiaquine 600 mg days as 8.3 mg/kg/day once a day for Administrations: Open stickpack following the fadoxine + Pyrimethamine and one oblong
Pack: 6’s (3 Artesunate tabs + 3 Amodiaquine tabs) 3 days. dotted line and administer its content directly onto caplet of Artesunate to be taken at once
POM PENATE® (Pemason) The therapeutic dose range is the child's tongue; wash down with some liquid e.g. on the first day, then one oblong caplet of
Tablet, Artesunate 100 mg, amodiaquine 300 mg between 2–10 mg/kg/dose/day of milk or water. Encourage child to resume normal Artesunate on the 2nd and 3rd days.
artesunate and 7–11 mg/kg/dose/day food intake as soon as possible. Tablets, (Child), Artesunate 50 mg (white scored tab.)
POM QUINSUNAT® (Neros) + Sulfadoxine 500 mg/Pyrimethamine 25 mg (blue
of mefloquine. POM LEVERPLUS® (Geneith)
Tablets, Amodiaquine 150 mg (f-c tab.) + Artesunate double scored tab.)
50 mg. POM AMDIN® (Vixa) Tablets ,(600/750), Artesunate 200 mg, mefloquine
Combipack: 4’s (3 white Artesunate tablets + 1 blue
Sulfadoxine/Pyrimethamine tablet). Combipack: 6’s (3 Artesunate tabs + 3 Sulfameth- Tablet, Dihydroartemisinin 40 mg, Piperaquine POM FALCIDIN® (Neros)
Dose: Child (2-6 years), 1 blue tablet of Sulfadoxine oxy-pyrazine/Pyrimethamine tabs). phosphate 320 mg; green. Caplet, Dihydroartemisinin 40 mg, piperaquine
+ Pyrimethamine and one white tablet of Dose: Adults (40-80 kg): phosphate 320 mg; f-c caplet.
POM ARTECXIN® (O’Nell)
Artesunate to be taken at once on the first Day 1: 1 tablet (200 mg) Artesunate together with Pack: 1 x 8’s.
Tablet, Dihydroartemisinin 32 mg, Piperaquine 320
day, then one white tablet of Artesunate on the 1 Sulfamethoxypyrazine/Pyrimeth- Suspension, Dihydroartemisinin 80 mg, piperaquine
mg, Trimethoprim 90 mg; green tab.
the 2nd and 3rd days. amine tablet. phosphate 640 mg.
Pack: 8’s.
Tablet to be crushed in water and taken Day 2: 1 tablet (200 mg) Artesunate together with Pack: 1’s.
Dose: Adult (>40 kg), by mouth, initially 2 tablets;
immediately. the 1 Sulfamethoxypyrazine/Pyrimeth-
then, 2 tablets repeated at 8th, 24th and POM GENAQUINE® (Next Generation)
amine tablet.
POM MALOSUNATE® (Astra) 32nd hour. Tablet, Dihydroartemisinin 32 mg, piperaquine
Day 3: 1 tablet (200 mg) Artesunate together with
Tablets (Adult), Artesunate 100 mg + Sulfadoxine 500 Child (10-19 kg), initially ½ tablet; 20-29 phosphate 320 mg, trimethoprim 90 mg.
the 1 Sulfamethoxypyrazine/Pyrimeth-
mg, Pyrimethamine 25 mg. kg, 1 tablet; 30-39 kg, 1½ tablet. Same Pack: 8’s (in blisters)
amine tablet.
Pack: 9’s (6 Artesunate tablets + 3 Sulfadoxine/ initial doses according to the weight to be Powder for suspension, Dihydroartemisinin 10.7 mg,
Tablets Junior, Artesunate 100 mg (small scored tab.)
Pyrimethamine tablets). repeated at 8th, 24th and 32nd hour. piperaquine phosphate 107 mg, trimethoprim 30
+ Sulfamethoxypyrazine 250 mg/Pyrimethamine
Dose: Malosunate adult 100 mg mg per 5 mL; granules for oral suspension.
12.5 mg (large pink tab.); both marked “DAFRA POM ARTERAKINE® (Neros)
Weight Age Day 1 Day 2 Day 3 Pack: 60 mL
PHARMA”. Caplet, Dihydroartemisinin 40 mg, Piperaquine
Sulfadoxine/
Pyrimethamine
Dose: Adolescents and children (20-39 kg): phosphate 320 mg; film-coated caplet. POM P-ALAXIN® (Greenlife)
Artesunate Artesunate 2 Day 1: Artesunate 4 mg/kg body weight as a single Tablet, Dihydroartemisinin 40 mg, Piperaquine
45 kg Adults 3 tablets +
2 tablets tablets
Pack: 8’s.
Artesunate 2 dose (1 tablet) together with 1 Sulfameth- Dose phosphate 320 mg; f-c tab.
tablets oxypyrazine/Pyrimethamine tablet. Pack: 8’s (in blister).
Sulfadoxine / 1st day 2nd day 3rd day
Day 2: Artesunate 4 mg/kg body weight as a single Age Dose
Pyrimethamine (caplet) (caplet) (caplet)
Artesunate Artesunate 1 dose (1 tablet) together with 1 Sulfameth-
31-45 kg 9-14 2 tablets + Adult (>15 years) 4 2 2 Age (years) <6 6 – 11 11-16 >16
1 tablet tablet
Artesunate 1 oxypyrazine/Pyrimethamine tablet. Child (3-6 years) 1 0.5 0.5 Day 1 1 1½ 2 3
EMDEX
tablet Day 3: Artesunate 4 mg/kg body weight as a single Child (7-10 years) 2 1 1 Day 2 1 1½ 2 3
Sulfadoxine/ dose (1 tablet) together with 1 Sulfameth- Child (11-14 years) 3 1.5 1.5 Day 3 1 1 2 2
Pyrimethamine
21-30 kg 4-8 2 tablets +
Artesunate Artesunate oxypyrazine/Pyrimethamine tablet. Child (6 mths-3 years) Use under the doctor’s advise Total (tablets) 3 4 6 8
½ tablet ½ tablet Note: Tablets may be broken or crushed for con-
Artesunate ½ Administration: First day, divide the dosage into Powder for oral suspension, Dihydroartemisinin 80
tablet venience. Do not exceed the recommended dose two – give the 2nd dose 8 hours after the first. mg, piperaquine phosphate 640 mg.
Sulfadoxine/ without seeking medical advice. In order to ensure
Pyrimethamine The following days: administer once daily. For best Pack: 80 mL
11-20 kg <4 ½ tablet +
Artesunate Artesunate complete recovery, the entire course of treatment result, the drug should be administered at 24 hourly
¼ tablet ¼ tablet must be taken. POM PIPART® (Digitall)
Artesunate ¼ intervals from the first dosage.
tablet Tablet, Dihydroartemisinin 40 mg, piperaquine
Tablets (Child), Artesunate 50 mg + Sulfadoxine 500 DIHYDROARTEMISININ POM AXCIN® (Vixa) phosphate 320 mg.
mg/Pyrimethamine 25 mg. plus PIPERAQUINE Tablet, Dihydroartemisinin 32 mg, Piperaquine 320 Pack: 8’s (in blister)
Pack: 8’s (6 Artesunate tablets + 2 Sulfadoxine/ mg, Trimethoprim 90 mg; green coated tab.
POM AMNOQUINE® (E-Globa) Pack: 8’s (in blister). POM PYMAL® (Pinnacle)
Pyrimethamine tablets). Capsule, Dihydroartemisinin 40 mg, piperaquine
Caplet, Dihydroartemisinin 40 mg, piperaquine Dose: Adult (>40 kg), by mouth, 2 tablets; followed
Dose: Malosunate children 50 mg phosphate 320 mg.
phosphate 320 mg; green f-c caplet marked “DP” by 2 tablets at the 8th, 24th and 32nd hour.
Weight Age Day 1 Day 2 Day 3 Pack: 1 x 8’s Pack: 9’s.
The total dose is 8 tablets.
Sulfadoxine
/Pyrimethamine 1st day 2nd day 3rd day Child (10-19 kg), ½ tablet; 20-29 kg, 1 tab- POM SOLARTEP® (Solution Pharma)
Artesunate Artesunate Age
31-45 kg 9-14 2 tablets +
2 tablets 2 tablets
(1st dose/8h later) (24h later) (48h later) let; 30-39 kg, 1½ tablet. Same doses to be Tablet, Dihydroartemisinin 40 mg, piperaquine
Artesunate 2 repeated at the 8th, 24th and 32nd hour. To
tablets
3-6 ½ ½ ½ ½ phosphate 320 mg
7-10 1 1 1 1 be taken after meals. Pack: 8’s (in blisters)
Sulfadoxine
/Pyrimethamine 11-14 1½ 1½ 1½ 1½ Dose:
Artesunate Artesunate POM CODISON® Plus (Geneith)
21-30 kg 4-8 1 tablet + ≥15 2 2 2 2
Artesunate 1
1 tablet 1 tablet Tablet, Dihydroartemisinin 40 mg, piperaquine Age 7-10 yrs 11-15 yrs ≥16 yrs
tablet POM AMOSININ® (Astra) 320 mg Initial dose 1 tab 1½ tabs 2 tabs
Sulfadoxine
Tablets, (Adult), Amodiaquine base 600 mg + Dihy- Pack: 8’s 8 hrs after 1 tab 1½ tabs 2 tab
/Pyrimethamine 24 hrs after 1 tab 1½ tabs 2 tab
Artesunate Artesunate droartemisinin 120 mg.
11-20 kg <4 ½ tablet + POM DIPRITRIM® (Jubilee) 48 hrs after 1 tab 1½ tabs 2 tabs
½ tablet ½ tablet
Artesunate ½ Pack: 6’s (3 Amodiaquine tablets + 3 Dihydroarte- Tablet, Dihydroartemisinin 32 mg, Piperaquine 320
tablet
Complete dose 4 tabs 6 tabs 8 tabs
misinin tablets). mg, Trimethoprim 90 mg; green coated tab. which
Tablets, (Junior), Amodiaquine base 300 mg + Dihy- Suspension, Dihydroartemisinin 90 mg, piperaquine
appears off-white or light yellow on removing the
POM MALTARKA® (Lifeback) droartemisinin 60 mg. phosphate 720 mg per 60 mL.
coating.
Tablet, Sulfadoxine 500 mg, Pyrimethamine 25 mg Pack: 6’s (3 Amodiaquine tablets + 3 Dihydroarte- Pack: 60 mL.
Pack: 8’s (in blister).
(caplet) + Artesunate 200 mg (tablet). misinin tablets). Dose: Adult (>40 kg), by mouth, initially 2 tablets; POM TriACT®(Tiopharms)
Combipack: 6’s (3 tablets of Artesunate + 3 caplets Powder, Amodiaquine base 150 mg + Dihydroarte- then, 2 tablets repeated at 8th, 24th and Caplet, Dihydroartemisinin 32 mg, Piperaquine 320
of Sulfadoxne/Pyrimethamine) misinin 30 mg. 32nd hour for a total of 8 tablets. mg, Trimethoprim 90 mg; olive green tab marked
Pack: 6’s (3 Amodiaquine sachets + 3 Dihydro-arte- Children: Based on b. wt. as below 'TriACT'.
ARTESUNATE plus misinin sachets).
SULFAMETHOXYPYRAZINE/ Day 1 Day 2 550 mg – 8's
PYRIMETHAMINE Paediatric powder, Amodiaquine base 75 mg + Weight (kg) Powder for suspension (Paediatric), Dihydroartemis-
0h 8h 24h 32h
Dihydroartemisinin 15 mg. inin 8 mg, Piperaquine 80 mg, Trimethoprim 22.5
10-19 1/2 1/2 1/2 1/2
POM CO-ARINATE® (Dafra) Pack: 6’s (3 Amodiaquine sachets + 3 Dihydro-arte- mg per 5 mL; light pinkish, sweetened powder with
20-29 1 1 1 1
Tablets, Artesunate 200 mg (small scored tab.) + misinin sachets). strawberry flavour which turns outright pinkish after
Sulfamethoxypyrazine 500 mg/Pyrimethamine 25 3-39 11/2 11/2 11/2 11/2
POM ARTCOP® (Watson) reconstitution.
mg (large pink tab.); both marked “DAFRA PHARMA”. ≥40 2 2 2 2
440 | 9.3.1.2 Drugs for the treatment of severe malaria 9.3.1.2 Drugs for the treatment of severe malaria | 441
Pack: 8 g shown in the schedule below. May 2.4 mg/kg at 0 h, 12 h and 24 h. Then once 50 mg – 12’s.
break and crush tablet before admin- daily for max. 6 days.
POM VISKART-P® (Visko) POM ASKASUNATE® (Diamond Remedies)
Tablet, Dihydroartemisinin + Piperaquine phosphate istration. Continue for minimum of 24 hours Tablet, Artesunate 50 mg; uncoated tab.
Pack: 8 x 10’s Dosage schedule by age groups as follows: and then switch to oral therapy as 50 mg – 12’s (in blister).
Age 0 hr 24 hrs soon as patient can tolerate it. Give a
full course of ACT for total of 3 days. POM GSUNATE® (Greenlife)
ARTEMISININ plus PIPERAQUINE ≥16 years 2 tablets 2 tablets Tablet, Artesunate 100 mg; coated tab.
Reconstitution: Artesunic acid should be dissolved
Therapeutic category: Antimalarial; Artemis- 11 to 15 years 1½ tablets 1½ tablets
in sodium bicarbonate 5% solution for injection (to 100 mg – 6’s.
inin-based combination therapy. 7 to 10 years 1 tablet 1 tablet
form sodium artesunate), and then further diluted POM LEVER® (Geneith)
Pharmacology: Song et al (Malaria Journal in 5 mL of glucose 5% solution for injection before Tablet, Artesunate 50 mg; white scored tab. marked
POM ARTEQUICK® (Artepharm)
2011, 10:231) compared the efficacy and tol- administration; solutions should be freshly prepared “AS” and “50 mg” on one side and “Lever” on the
Tablet, Artemisinin 62.5 mg, Piperaquine 375 mg.
erability of 2-day regimen of Artemisinin-Piper- Pack: 4’s (in blisters) prior to administration; consult manufacturer’s reverse.
aquine (AP) against the standard 3-day courses literature. Pack: 20 x 12’s.
of Dihydroartemisinin-Piperaquine phosphate ARTESUNATE plus TETRACYCLINE OR See also under the proprietary preparations below. POM MALMETER® (Evans)
(DHP) and Artemether-Lumefantrine (AL), for DOXYCYCLINE OR CLINDAMYCIN Tablet, Artesunate 50 mg.
the treatment of uncomplicated Falciparum Indications: Reserved for very rare occasions POM Artesunate (WMF 6.5.3) 50 mg – 12’s.
malaria. After 28-day follow-up, the cure rate of treatment failures to the recommended Tablet, Artesunate 50 mg.
Injection, ampoules, containing 60 mg anhydrous POM REKMAL® (Emzor)
was 95.1% (AP), 98.2% (DHP) and 82.4% (AL); ACTs and in some special groups, e.g. pregnant
Artesunic acid with a separate ampoule of 5% Injection, Artesunate 60 mg.
both parasite and fever clearance times were women failing ACT treatment. Pack: 1 vial Artesunate + 1 amp Sodium bicarbonate
Sodium bicarbonate solution.
similar in all three groups. In an earlier study Dose: Available as individual dosage forms 5% w/v 1 mL + Sodium chloride 0.9% w/v 5 mL.
however, Krusood et al (Southeast Asian J Trop and should be dosed separately for POM ARSUMAX® (Sanofi)
Med Public Health. Nov 2007; 38(6): 971–978), Tablet, Artesunate 50 mg; white scored tab. POM TEKMAL® (Onifam)
hospital use only.
EMDEX
50 mg – 12. Tablet, Artesunate 100 mg
found that 2-day courses of Artemisinin Artesunate (2 mg/kg once a day) plus 100 mg – 1 x 6’s.
with Piperaquine were associated with late Tetracycline (4 mg/kg four times a POM ARTESUN® (Phillips)
recrudescence within the 28 days of hospital day or Doxycycline (3.5 mg/kg once a Injection, Artesunate 60 mg ARTEMETHER
observation in about one quarter of the pa- day) or Clindamycin (10 mg/kg twice POM ARTESUNAT® (Neros) Indications: Treatment of severe P. falciparum
tients treated. In contrast, the 3-day regimens a day). Tablet, Artesunate 50 mg. malaria in areas where quinine is ineffective
of both Artemisinin-Piperaquine (AP) and Any of these combinations should be 50 mg – 1 x 12’s; 10 x 12’s (in blisters). (see also notes in EMDEX Vol. 3).
Dihydroartemisinin-Piperaquine (DHP), gave given for 7 days. Powder for oral suspension, Artesunate 160 mg; in
Contra-indications: First trimester of preg-
cure rates >98%. Current WHO recommenda- Source: World Health Organization (WHO). Guidelines for the 80 mL bottle.
nancy.
tion is that ACTs should include at least 3 days treatment of malaria. 2nd edition, 2010. Pack: 80 mL bottle.
Powder for injection, Artesunate 60 mg per mL; in Precautions: SKILLED TASKS: Dizziness may im-
of treatment with an artemisinin derivative.
vial plus 1 mL of 5% Sodium bicarbonate as solvent. pair ability to perform skilled tasks, for example
Artemisinin has potent and rapid parasiticidal
effect on those parasites in intra-erythrocyte
9.3.1.2 Drugs for the treatment Pack: 1’s (in vial) + 1 mL solvent (in amp.). operating machinery, driving.
of severe malaria Administration: By deep IM injection or slow IV Adverse effects: Headache, nausea, vomiting,
stage. Moreover, its efficacy is much quicker injection.
See detailed notes in EMDEX Vol. 3. abdominal pain, diarrhoea; dizziness, tinnitus,
than that of quinine, chloroquine and all Deep IM Injection: Dissolve 60 mg of Artesunate neutropenia, elevated liver enzyme values; car-
other non-artemisinin antimalarial drugs. Pip- with 1 mI of 5% sodium bicarbonate solution for diotoxicity (after high doses); neurotoxicity—in
eraquine is a 4-aminoquinolone compound. ARTESUNATE injection before use.
animal studies.
Studies showed that the efficacy and curative Indications: Artesunate injection is for use in Slow IV Injection: Dissolve 60 mg of Artesunate with
1 mI of 5% sodium bicarbonate solution for injection Dose: Treatment of severe P. falciparum ma-
index of piperaquine were 2.6 and 6.6 times the management of severe malaria. Artesunate
and add 5 mI of 0.9% sodium chloride solution for laria (in areas of quinine resistance), by
higher than those of chloroquine. Following tablets should be used in combination with injection before use to make 1 mI containing 10 mg IM injection, ADULT and CHILD over
oral administration, peak plasma concentration either amodiaquine, mefloquine, or sulfa- of Artesunate. Injection must follow immediately 6 months, loading dose of 3.2 mg/kg,
occurs about 3 hours. Artemisinin is converted doxine /pyrimethamine for the treatment of soon after dissolution; if the solution appears cloudy then 1.6 mg/kg daily until patient can
to inactive metabolites via the CYP2B6 and uncomplicated malaria caused by P. falciparum. or sediment occurs, it should be rejected. tolerate oral medication or to maxi-
other enzymes; it is a potent inducer of its Contra-indications: First trimester of preg- POM Artesunate (Jawa) mum of 7 days; this is followed by a
own metabolism. The elimination half-life is nancy. Injection, Artesunate 60 mg. single dose of mefloquine 15 mg/kg
approx. 1 hour. Precautions: Risk of recurrence if used alone Pack: 1 x 3’s. (or occasionally, if necessary 25 mg/
Indications: Treatment of falciparum and in non-immune patients.
POM Artesunate (Zolon)
kg) to effect a radical cure.
vivax malaria. Adverse effects: Headache, nausea, vomiting, Administration: Since small volumes are required
Precautions: Hepatic or renal dysfunction; Injection, Artesunate 60 mg per mL
abdominal pain, diarrhoea, dizziness, tinnitus, Pack: vial along with one ampoule of 1 mL sodium
for children, a 1-mL syringe should be used to ensure
Pregnancy, Breastfeeding, Elderly. neutropenia, elevated liver enzyme values; ECG correct dosage.
Adverse effects: Mainly GI symptoms namely bicarbonate injection 5% and one ampoule of 5 mL
abnormalities, including prolongation of QT Note: For IM use only; administer aseptically in the
sodium chloride injection 0.9%
nausea, vomiting, abdominal pain, diarrhea; interval; temporary suppression of reticulocyte upper-outer quadrant of the buttock. Do not mix
Dizziness observed occasionally. POM ARTHLON-50® (GoldMoore) with other drugs in the same syringe.
response and induction of blackwater fever,
Dose: Adult, by mouth, 2 tablets at 0 hour Tablet, Artesunate 50 mg; uncoated tab.
reported; neurotoxicity—in animal studies. See also under the proprietary preparations below.
and 2 tablets at 24 hours (total = 4 Pack: 12’s.
Dose: See detailed notes in EMDEX Vol. 3.
tablets). Treatment of severe malaria, Adult or POM ARTICIN® (Embassy) POM Artemether (WMF 6.5.3)
Children: a two-dose regimen as child, by slow IV injection or IM injection, Tablet, Artesunate 50 mg. Oily injection, Artemether 80 mg/mL; in 1-mL
442 | 9.3.1.2 Drugs for the treatment of severe malaria 9.3.1.2 Drugs for the treatment of severe malaria | 443
ampoule. POM GENMETHER® (Next Generation) POM ZARTHER® (Shrezar) 10 mg/kg (quinine sulfate) every 8
Injections, Artemether 20 mg, 40 mg, 80 mg per 1 mL Injection, Artemether 80 mg per mL hours for 3, 7, or 10 days; duration of
POM Artemether (EDL 5.7)
Pack: 6 amp x 1 mL treatment depends on local suscep-
Injection, Artemether 80 mg per mL; in 1-mL amp. POM GLOATHER® (Global Healthcare)
Injections, Artemether 20 mg, 40 mg, 80 mg per mL. tibility of P. falciparum and whether
POM ARMEETHER® (Bakangizo)
Pack: 1 mL x 6’s; 1 mL x 10’s. QUININE or not additional antimalarials also
Injection, Artemether 80 mg per mL Indications: Multiple-drug-resistant P. falci-
Pack: 1 x 6 amps POM GVITHER® (Greenlife)
used. Treatment of multiple-drug
parum malaria. resistant P. falciparum malaria (in
Injection, Artemether 20 mg per mL Injection, Artemether 80 mg per mL; sterile and
Pack: 1 x 10 amps colourless solution in 1 mL colourless glass amp. Contra-indications: Haemoglobinuria; optic patients unable to take quinine by
with disposable 2 mL syringe & needle. neuritis; tinnitus; myasthenia gravis. mouth), by slow IV infusion (over 4
POM Artemether (BG Pharma) Precautions: Atrial fibrillation, conduction de-
Pack: 6’s. hours), ADULT 20 mg/kg (quinine
Injection, Artemether 80 mg per mL fects, heart block; monitor for signs of cardiac
Oral Suspension, Artemether 15 mg per 5 mL. dihydrochloride) followed by 10 mg/
Pack: 6 x 1 mL ampoules
Pack: 100 mL. toxicity and blood-glucose and electrolyte kg (quinine dihydrochloride) every
POM ARMEETHER® (Eutrix) concentration during IV use; pregnancy (but 8 hours; CHILD 20 mg/kg (quinine
POM HILACT® (CG Biostadt)
Injection, Artemether 80 mg per mL; clear, colourless appropriate for treatment of malaria, Ap- dihydrochloride) followed by 10 mg/
Injection, Artemether 80 mg; in amps
or yellow oily solution in amp. pendix 2); breastfeeding (Appendix 3); renal
Pack: 6’s kg (quinine dihydrochloride) every 12
Pack: 1 mL x 6’s.
impairment (Appendix 4); G6PD deficiency; hours; initial dose should be halved in
POM LABNAT® (Embassy)
POM Artemether (N.C.I)
Injection, Arthemeter 80 mg. interactions: Appendix 1. patients who have received quinine,
Injection, Artemether 80 mg per mL. Adverse effects: Cinchonism (tinnitus, head- quinidine or mefloquine during the
Pack: 6’s.
Pack: 1 mL x 6’s. ache, blurred vision, temporary blindness, previous 12–24 hours.
POM LARITHER® (IPCA) altered auditory acuity, nausea, diarrhoea, hot
POM Artemether (Solution Pharma) Dilution and Administration: intravenous injection
Capsule, Artemether 40 mg.
Injection, Artemether 80 mg per mL; in amp. and flushed skin, rashes, confusion); hypersen- of quinine is so hazardous that it has been super-
40 mg – 6’s.
EMDEX
Pack: 1 mL x 6’s. sitivity reactions including angioedema; rarely seded by infusion; where facilities for IV infusion
Injection (,40 mg), Artemether 40 mg per mL
haemorrhage and asthma; hypoglycaemia (es- are unavailable, an appropriate dilution may be
POM ARTEMETIN-BETA® (Beta Drugs) Pack: 1 mL x 6’s.
pecially after parenteral administration); renal administered by IM injection.
Injection, Artemether 80 mg per mL. Injection ,(80 mg), Artemether 80 mg per mL
Pack: 1 x 6’s. Pack: 1 mL x 6’s. damage (culminating in acute renal failure and See also under the proprietary preparations below.
POM MALETHER® (Geneith)
anuria); blood disorders; cardiovascular, GI and
POM ARTEJECT® (Crystal) POM Quinine (WMF 6.5.3)
Injection, Artemether 40 mg, 80 mg. Injection ,(40 mg), Artemether 40 mg per mL CNS effects; very toxic in overdosage—imme-
diate medical attention required. Tablet, Quinine sulfate 300 mg or Quinine bisulfate
Pack: 1 mL x 6’s (in amps) Injection ,(80 mg), Artemether 80 mg per mL 300 mg.
Advice to patients: Swallow dose whole
POM Artemether (Hochiez) POM NANCIMAL® (Teta) Injection, Quinine hydrochloride 300 mg/mL; in
to avoid bitter taste and irritation to gastric 2-mL ampoule.
Injection, Artemether 80 mg per mL; in 1 mL amp. Injection, Artemether 80 mg per mL
Pack: 5’s amp (in blisters); 12’s (in carton)
mucosa; avoid use of aluminium-containing
Pack: 1 mL POM Quinine (EDL 5.7)
antacids because of drug absorption problems;
POM Artemether (Vixa) POM NEXTHER® (Next Generation) may cause night blindness. Patients should Injection, Quinine (as dihydrochloride) 300 mg per
Tablets, Artemether 50 mg, 100 mg; white tabs. Injection, α-β Artemether 75 mg; in arachis oil. mL; in 2-mL amp.
notify their physician if rash, fever, unusual
Pack: 2 mL x 3’s POM CINKONA® (Hochiez)
POM ARTESIANE® (Dafra) bleeding or bruising, ringing in the ears, visual
Injection, Artemether 80 mg per mL; sterile, colour- POM NOFALSI-H® (Mark) disturbances, or syncope occur. If all or part of Tablet, Quinine (as sulfate) 300 mg; f-c tab.
less oily solutn in 1 mL clear glass amp. Injection, Artemether 80 mg; in 1-mL amp. a dose is vomited within one hour, the same 300 mg – 6’s.
Pack: 1 mL x 5’s. Injection, Quinine (as dihydrochloride) 300 mg per
POM PALUTHER® (Sanofi-Aventis) amount must be readministered immediately.
Suppogel, Artemether 40 mg. mL; in 2 mL amp.
Injection, Artemether 80 mg per mL; arachis oil based Nursing action: Administer before or after 20 mg – 10 x 10’s.
Pack: 6 suppositories.
solution in 1 mL colourless glass amp meals at the same time to minimise GI distress
Dose: Child, by rectum, 4 mg/kg b. wt as follows: POM LIZOQUIN® (Standard Generics)
Pack: 1 mL x 6. and maintain drug level; do not crush tablets
5-9 kg, 1 suppogel on Day 1 and 1 suppogel Injection, Quinine dihydrochloride 600 mg per 2 mL.
daily on Days 2 to 5; 10-19 kg, 2 suppogels POM RARTEL® (Chanmedi) as drug is irritating to gastric mucosa.
on Day 1 and 1 suppogel daily on days 2 Injection, Artemether 80 mg per mL • Give slowly by IV infusion over at least 1 hour. POM MALAGOLD® (Medreich)
to 5; 20-29 kg, 3 suppogels on Day 1 and 2 Pack: 2 mL x 10 x 10’s • Observe closely for cinchonism viz nausea, blurred Tablet, Quinine sulfate 300mg (equiv. to Quinine 248
suppogels daily on Days 2 to 5. vision, tinnitus, headache, difficulty in focusing. mg); white s-c tab.
POM SANARTEME® (Vixa) • Teach patient to avoid POM preparations (unless
Paediatric injection, Artemether 20 mg per mL in POM Moko Liquid Quinine (New Healthway)
Tablets, Artemether 50 mg, 100 mg. on prescription) and tonic water.
fractionated coconut oil; sterile colourless solution. Solution, Quinine (as HCl) 100 mg per 5 mL
Pack: 6’s. Dose: NOTE: Quinine (anhydrous base) 100
Pack: 1 mL x 10’s (in amps). Pack: 200 mL.
Injections, Artemether 40 mg/0.5ml, 80 mg/mL mg Ξ Quinine bisulfate 169 mg Ξ
POM ARTHEC® (Geneith) Pack: 6 amps. POM PENINE® (Pemason)
Quinine dihydrochloride 122 mg Ξ
Injection, Artemether 80 mg per mL. Injection, Quinine dihydrochloride 600 mg per 2 mL;
POM SUMETHER® (Superior) Quinine sulfate 121 mg.
POM ERITHER® (Onifam) Injection, Artemether 80 mg per mL; oily base. Quinine bisulfate 300 mg tablets in amber coloured amp. marked “Penine”
Injection ,(40 mg/mL), Artemether 40 mg per mL. Pack: 2 mL x 10 x 10’s.
POM THERAMETHER® (Therapeutic) provide less quinine than 300 mg of
Pack: 1 mL x 6’s (in amp) the sulfate or dihydrochloride. POM Q-300® (Strides Vital)
Oral Suspension, Artemether 15 mg per 5 mL.
Injection, (80 mg/mL), Artemether 80 mg per mL. Tablet, Quinine sulfate 300 mg.
Pack: 100 mL. Treatment of multiple-drug resistant
Pack: 1 mL x 6’s (in amp) 300 mg – 3 x 10’s.
POM VISKOTHER® (Visko)
P. falciparum malaria, by mouth,
POM FASTHAR® (Hochiez) ADULT 600 mg (quinine sulfate) every POM QUINAC® (Goldmoore)
Injection, Artemether 80 mg
Injection, Artemether 80 mg per mL. 8 hours for 3, 7, or 10 days; CHILD Injection, Quinine dihydrochloride 300 mg per 2 mL.
Pack: 6 x 1 mL
Pack: 80 mg per mL.
444 | 9.3.1.3 Agents for chemoprophylaxis 9.3.1.3 Agents for chemoprophylaxis | 445
POM QUINIMAX® (Sanofi) Contra-indications: History of neuropsychiat- These may be signs of impending toxicity. 100 mg.
Tablets, Quinine 125 mg, 500 mg; scored f-c tabs. ric disorders including depression or convul- Dose: NOTE: All doses are in terms of the base
125 mg – 18’s sions; hypersensitivity to quinine. Prophylaxis of malaria, by mouth, PROGUANIL
500 mg – 9’s. Precautions: Pregnancy (use only if other an- ADULT 250 mg once a week; CHILD Indications: Prophylaxis of malaria in areas
Dose: By mouth, Adult, 500 mg every 8 hours.
timalarials inappropriate; Appendix 2), avoid over 5 kg, 5 mg/kg once a week; of low resistance; see notes in EMDEX Vol. 3.
Child (15 kg), 125 mg every 8 hours.
Child (30 kg), 250 mg every 8 hours pregnancy during and for 3 months after use; prophylaxis should start 1–3 weeks Contra-indications: Use in areas of known re-
Note: The duration of treatment is 5-7 days. cardiac conduction disorders; avoid for proph- before departure and continue for 4 sistance to either proguanil or pyrimethamine.
Injection, Quinine 125 mg per mL; solution for ylaxis in severe hepatic impairment (Appendix weeks after last exposure, see notes Precautions: Renal impairment (Appendix
injection in 1 mL, 2 mL and 4 mL amber glass amps. 5) and in epilepsy; breastfeeding (Appendix 3); in EMDEX Vol. 3. 4); pregnancy (folate supplements required,
Pack: 3’s; 25’s. not recommended for infants under 3 months Appendix 2); breastfeeding (Appendix 3);
POM Mefoquine (WMF 6.5.3)
Dose: By IV infusion or slow deep IM injection, 8 (5 kg); interactions: Appendix 1. interactions: Appendix 1.
Tablet, Mefloquine (as HCl) 250 mg.
mg/kg 2-3 times daily; not exceeding 25 NOTE: Patients should be informed about ad- Adverse effects: Mild gastric intolerance,
mg/kg daily. POM Mefloquine (EDL 5.7)
verse effects associated with mefloquine and diarrhoea, constipation; occasional mouth
Tablet, Mefloquine (as HCl) 250 mg.
POM Quinine (E-Globa) if they occur advised to seek medical advice on ulcers and stomatitis; rarely skin reactions and
Tablet, Quinine sulphate 300 mg. alternative antimalarials. POM LARIAM® (Swipha) hair loss, cholestasis, vasculitis, hypersensitivity
300 mg – 10 x 10’s (in blisters). Adverse effects: Nausea, vomiting, diarrhoea, Tablet, Mefloquine 250 mg. reactions such as urticaria and angioedema.
abdominal pain, anorexia, headache, dizziness 250 mg – 4; 50.
POM Quinine (Embassy) Dose: Prophylaxis of malaria, by mouth,
Tablet, Quinine sulfate 300 mg; s-c tab. (can be severe), loss of balance, somnolence, ADULT 200 mg daily, after food;
300 mh – 10’s. insomnia and abnormal dreams; neurological DOXYCYCLINE
CHILD under 1 year, 25 mg daily;
Injection, Quinine dihydrochloride 300 mg per mL; and psychiatric disturbances including sensory Indications: Supplement to quinine or artesu- CHILD 1–4 years, 50 mg daily; CHILD
in 2 mL amp. and motor neuropathies, tremor, ataxia, visual nate treatment for multiple-drug-resistant P. 5–8 years, 100 mg daily; CHILD 9– 14
EMDEX
Pack: 2 mL x 10’s. disturbances, tinnitus, vestibular disorders; falciparum malaria; short-term prophylaxis of years, 150 mg daily.
POM Quinine (Nomagbon) convulsions, anxiety, depression, suicidal ide- multiple-drugresistant P. falciparum malaria; Note: The daily dose is best taken with water, after
Liquid, Quinine sulhpate 150 mg per 5 mL; colouration, confusion, hallucinations, panic attacks, see also notes above; bacterial infections food, at the same time each day. For a young child,
less liquid. emotional instability, aggression, agitation and (section 9.1.2.3). the dose may be administered crushed and mixed
Pack: 100 mL glass bottle. psychoses; circulatory disorders, tachycardia, Contra-indications: Pregnancy (Appendix 2); with milk, honey or jam. Non-immune subjects
children under 8 years; porphyria; systemic entering a malarious region are advised to begin
POM Quinine B (Beta Drugs) bradycardia, cardiac conduction disorders;
lupus erythematosus. treatment with proguanil at least 24 hours before
Injection, Quinine dihydrochloride 300 mg. muscle weakness, myalgia, arthralgia; rash, arrival. The daily dose of proguanil should be contin-
Pack: 10 x 10’s. urticaria, pruritus, alopecia; disturbances in Precautions: Avoid exposure to sunlight or
ued throughout exposure to risk and for four weeks
liver function tests, leukopenia, leucocytosis, sunlamps—photosensitivity reported; renal after leaving the area.
POM Quinine Sulphate (E-Globa)
Tablet, Quinine sulphate 300 mg; sugar coated tab. thrombocytopenia; rarely, Stevens-Johnson impairment (Appendix 4); hepatic impairment
(Appendix 5); breastfeeding (Appendix 3); POM Proguanil (WMF 6.5.3)
300 mg – 10 x 10’s (in blisters) syndrome, atrioventricular block and enceph- Tablet, Proguanil (as HCl) 100 mg.
alopathy. interactions: Appendix 1.
POM Quinine Sulphate (Kakaki) Adverse effects: GI disturbances; anorexia; POM Proguanil (EDL 5.7)
Tablet, Quinine sulphate 300 mg Advice to patients: Warn travellers about
the importance of avoiding mosquito bites, flushing, tinnitus; photosensitivity; hyper- Tablet, Proguanil (as HCl) 100 mg.
300 mg – 28’s; 500’s
importance of taking prophylaxis regularly, sensitivity reactions; headache and visual POM PALUDRINE® (Reals)
POM QUININJECT® (Medreich) disturbances; hepatotoxicity, blood disorders,
and importance of immediate visit to doctor if Tablet, Proguanil HCl 100 mg; white scored tab.
Injection, Quinine (as dihydrochloride) 300 mg per pancreatitis and antibiotic-associated colitis marked ‘P/P’ and ‘ICI’.
mL; in 2 mL amp.
ill within 1 year and especially within 3 months
of potential exposure. reported; staining of growing teeth and occa-
Pack: 10’s; 100’s. POM PILAN® (Evans)
Nursing action: Tell patient not to take the sional dental hypoplasia. Tablet, Proguanil (as HCl) 100 mg; uncoated tab.
POM QUINLON® (Shrezar) drug on an empty stomach and always to take Dose: Supplement to malaria treatment (see 100 mg – 10’s (in blister)
Injection, Quinine dihydrochloride 300 mg per mL; notes above), by mouth, ADULT and
it with a full glass of water. POM RELUDRINE® (Reals)
in 2 mL amp CHILD over 8 years, 100 mg twice
• Avoid coadministration with quinine or quinidine.
Pack: 10 amp x 2 mL Tablet, Proguanil HCl 100 mg.
There should be at least 12 hours between the daily for 7–10 days.
POM QUINYN® (E-Globa) commencement of mefloquine therapy and last Short-term prophylaxis of malaria, by
Injection, Quinine (as dihydrochloride) 600 mg dose of quinine or quinidine. mouth, ADULT 100 mg daily for up to
• Advise patient to exercise caution when perform- SULFADOXINE plus PYRIMETHAMINE
per 2 mL. 8 weeks; CHILD over 8 years, 1.5 mg/
Pack: 2 mL x 10’s. ing hazardous activities that require alertness and Indications: Intermittent preventive treatment
kg daily for up to 8 weeks; doxycy-
good coordination because dizziness, disturbed (IPT) of malaria in pregnant women during the
POM WHYTEQUIN® (Al-Tinez) sense of balance, and neuropsychiatric reactions
cline should be started on the day
2nd and 3rd trimesters of pregnancy
Tablet, Quinine sulphate 300 mg; sugar coated tab. have been reported. before exposure and continued for 4
300 mg – 10 x 10’s Contra-indications: Hypersensitivity to sulfo-
• Periodic eye examinations are recommended for weeks after last risk of exposure.
Administration: Capsules should be swallowed namides or pyrimethamine; severe hepatic or
patients on long-term therapy.
9.3.1.3 Agents for chemoprophylaxis whole with plenty of fluid while sitting or standing renal impairment (except where no alternative
• Induce vomiting and seek medical advice imme-
diately if overdose is suspected as it can cause to prevent oesophageal irritation. May be given with treatment available).
MEFLOQUINE cardiotoxicity. food or milk, to counter gastric irritation. Precautions: Avoid in blood disorders—
• Patients on mefloquine prophylaxis should discon- unless specialist supervision; discontinue
Indications: Prophylaxis of malaria for travel- POM Doxycycline (WMF 6.5.3)
tinue the drug if they notice signs of unexplained Capsule, Doxycycline (as HCl) 100 mg. immediately if blood disorder occurs; rash,
lers to areas with high risk of multiple-resistant
anxiety, depression, confusion, or restlessness. Dispersible tablet, Doxycycline (as monohydrate) sore throat, mouth ulcers, or shortness of
P. falciparum (see notes in EMDEX Vol. 3).
446 | 9.3.1.3 Agents for chemoprophylaxis 9.3.1.4 Other antimalarial drugs | 447
breath—withdraw treatment; G6PD deficiency; white doubly scored tab. marked with maker’s name must be taken not later than 30 days before antagonises the enzyme dihydrofolic–re-
predisposition to folate deficiency; pregnancy and symbol. the expected date of delivery. ductase, which converts dihydrofolic acid to
(Appendix 2); breastfeeding (Appendix 3); 525 mg – 3’s; 500’s. tetrahydrofolic acid.
POM MALCIDAL® (Juhel)
interactions: Appendix 1. Syrup, Sulfadoxine 500 mg, pyrimethamine Indications: Intermittent preventive treatment
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg.
25 mg per 5 mL.
Adverse effects: Rashes, pruritus, slight 525 mg – 50 x 3’s; 500’s. of malaria during the 2nd and 3rd trimesters of
Pack: 10 mL.
hair loss; rarely erythema multiforme (Ste- Injection, Sulfadoxine 500 mg, pyrimethamine 25 POM MALDOX® (Emzor)
pregnancy (IPTp). Also used for the treatment
vens-Johnson syndrome) and toxic epidermal mg; clear colourless solution in transparent 2.5 Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg of acute malaria attacks in combination with
necrolysis; GI disturbances including nausea, mL amp. 525 mg – 3 x 50. Artesunate.
vomiting, stomatitis; rarely, hepatitis, leu- Pack: 2.5 mL x 15’s. Contra-indications: Hypersensitivity to sul-
POM MALWIN® (Fidson)
kopenia, thrombocytopenia, megaloblastic POM FRALOMIN® (Embassy)
fonamides or pyrimethamine or other com-
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg
anaemia and purpura—withdraw treatment; Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. 525 mg – 3. ponents of preparation. Marked liver damage,
fatigue, headache, fever, polyneuritis, also renal insufficiency, blood dyscrasias, infants
reported; pulmonary infiltrates such as eo- POM GARYDOX® (Agary) POM NOVAXINE® (SKG) during the first two weeks of life, pregnancy
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg.
sinophilic or allergic alveolitis—if symptoms (during the last 2 weeks).
525 mg – 3’s.
of cough or shortness of breath—withdraw POM GILANOX® (Geneith) Precautions: Pregnancy, infants, patients
treatment. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. POM PYRAMIN® (Dana) predisposed to folic acid deficiency; reduce
Advice to patients: Drink plenty of fluids; 525 mg – 50 x 3’s. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg dose in renal disorders; regular blood controls
avoid prolonged exposure to the sun; notify Pack: 3’s (in blisters); 1000’s (in jar) during long therapy.
POM GOMAXINE® (GoldMoore)
physician if rash, sore throat, pallor, shortness Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. POM RIDMAL® (Diamond Remedies) Adverse effects: Seldomly nausea, vomiting
of breath, or glossitis occurs. Pack: 3’s. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg and cutaneous erythema; blood dyscrasias.
Dose: Intermittent preventive treatment 525 mg – 3 x 50; 10 x 50. Dose: See under the preparations below.
POM LARIDOX® (IPCA)
EMDEX
of malaria during pregnancy (IPTp), Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. POM SURAMEX® (May & Baker) POM MALAFIN® (Medreich)
by mouth, One full treatment dose 525 mg – 3’s; 500’s. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg; Tablet, Sulfamethoxypyrazine 500 mg, pyrimeth-
given twice, during the 2nd and 3rd Syrup, Sulfadoxine 500 mg, pyrimethamine white tab. amine 25 mg.
trimesters. Last dose to be given 25 mg per 5 mL. 525 mg – 3’s. 525 mg – 2’s.
not later than one month before the Pack: 10 mL. Dose: 2 tablets taken as a single dose not more than
Injection, Sulfadoxine 500 mg, pyrimethamine 25 POM SWIDAR® (Swipha)
expected date of delivery. Avoid use Tablet, Sulfadoxine 500 mg, pyrimethmine 25 mg. twice during the 2nd and 3rd trimesters of
mg; in 2.5 mL amp. pregnancy; the second and last dose must
in first trimester. Pack: 3,500.
Pack: 2.5 mL x 5’s. be taken not later than 30 days before the
POM Sulfadoxine plus Pyrimethamine (WMF 6.5.3) POM USIDAR® (Adler) expected date of delivery.
POM MALADAR® (Bond).
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg.
Tablet, Sulphadoxine 500 mg, pyrimethamine 25 mg POM METAFIZIN®(Drugfield)
POM Sulfadoxine plus Pyrimethamine (EDL 5.7) Pack: 3’s x 10's Pack: 3’s.
Tablet, Sulphamethoxypyrazine 500 mg, pyrimeth-
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. POM VITADAR® (Strides Vital) amine 25 mg
POM MALAGON® (Therapeutic)
POM AMALAR® (Elbe) Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg; Pack: 2’s
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg; 525 mg – 3’s scored tab. marked with the company’s logo.
525 mg – 3’s. POM METALENE® (Korlyns)
white scored tab. marked ‘AMALAR’ Suspension, Sulfadoxine 500 mg, pyrimethamine Tablet, Sulphamethoxypyrazine 500 mg, pyrimeth-
Pack: 3’s 25 mg per 5 mL. POM WIN MALAR® (Mecure) amine 25 mg.
Pack: 15 mL. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg; Pack: 5 x 6’s
POM ANTIMAL® (Neimeth)
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. POM MALAKARE® (Dizpharm) white tab. marked ‘MECURE’. Dose: Intermittent Preventive Therapy (IPT) in
525 mg – 3’s; 30’s; 250’s; 1000’s. Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg 525 mg – 50 x 3’s. pregnancy. To be administered in the 2nd
Syrup, Sulfadoxine 500 mg, pyrimethamine 25 g 525 mg – 3; 500. and 3rd trimesters of pregnancy during
POM ZIMALDAR® (Gauze)
per 5 mL. antenatal care. 3 tablets as a single dose
POM MALAREICH® (Medreich) Oral Liquid, Sulphadoxine 500 mg, pyrimethamine
Pack: 15 mL. at the 2nd trimester of pregnancy (after
Capsule/Tablet, (525 mg), Sulfadoxine 500 mg, py- 25 mg per 5 mL
quickening) 3 tablets as a single dose at the
POM CELOXINE® (Hochiez) rimethamine 25 mg. Pack: 10 mL
3rd trimester of pregnancy (at least 4 weeks
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg. 525 mg – 3’s. after the first dose) 3 doses in HIV + patients.
Pack: 50 x 3’s; 50 x 10’s. Tablet, (1575 mg), Sulfadoxine 1500 mg, pyrimeth- SULFAMETHOXYPYRAZINE plus
PYRIMETHAMINE
amine 75 mg. 9.3.1.4 Other antimalarial drugs
POM DUPRIDOX® (Drugfield) Therapeutic category: Antimalarial
1575 mg – 1’s.
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg Pharmacology: The combination has anti-
Suspension, Sulfadoxine 500 mg, pyrimethamine
Pack: 3’s AMODIAQUINE
25 mg per 5 mL. plasmodial activity and is effective in malaria
POM EFRODAR® (FAB) Pack: 10 mL. caused by P. falciparum, P. vivax, P. malariae and Indications: Treatment of uncomplicated
Tablet, Sulphadoxine 500 mg, pyrimethamine 25 mg Suspension, Sulfadoxine 500 mg, pyrimethamine 25 P. ovale. It provides a double attack at different malaria caused by P. falciparum in combination
525 mg – 3’s (in blister) mg per 2.5 mL; in amp. points of the same metabolic pathway of the with Artesunate only (see notes in EMDEX Vol. 3).
Pack: 2.5 mL x 3’s (in ampoules). Contra-indications: Hepatic impairment (Ap-
POM EVAMAL® (Evans) pathogen. While sulfamethopyrazine antago-
Dose: 2-3 tablets or capsules (SP500/25 mg) or 1 pendix 5); blood disorders, retinopathy.
Tablet, Sulphadoxine 500 mg, pyrimethamine 25 mg tablet (SP 1500/75 mg), or 10 mL 525/5ml nises the plasmodial enzyme dihydro-pteroate
Pack: 3’s synthetase, thus preventing the synthesis Precautions: Pregnancy (Appendix 2) and
suspension taken as single dose not more
than twice during the 2nd and 3rd trimes- of dihydropteroate, an intermediate in the breastfeeding (Appendix 3); G6PD deficiency;
POM FANSIDAR® (Swipha)
ters of pregnancy; the second and last dose formation of dihydrofolate, pyrimethamine avoid concurrent therapy with hepatotoxic
Tablet, Sulfadoxine 500 mg, pyrimethamine 25 mg;
drugs; interactions: Appendix 1.
448 | 9.3.1.4 Other antimalarial drugs 9.3.1.4 Other antimalarial drugs | 449
Adverse effects: Blood disorders including same syringe. individuals. mg per 5 mL.
leukopenia and agranulocytosis, hepatitis, GI Advice to patients: May take with meals; Pack: 30 mL
POM FONTETHER® (Mark)
disturbances, visual disturbances (retinopathy report any visual disturbances or difficulty in Suspension, (1-3 years), Chloroquine sulfate 102
Injection, α-β arteether 75 mg; in arachis oil
associated with long-term, high-dose ther- hearing or ringing in the ears; tablets are bitter mg per 5 mL.
Pack: 3 x 2 mL
Pack: 30 mL
apy); rarely rash, pruritus, skin pigmentation, tasting; may cause diarrhoea, loss of appetite,
POM GLOMETHER® (PharmacyPlus) Suspension ,(4-11 months), Chloroquine sulfate 51
neuromyopathy. Injection, α−βArteether 150 mg per 2 mL; in ara-
nausea, stomach pain; notify physician if these mg per 5 mL.
Advice to patients: Patients and their carers chis oil become severe. Oral chloroquine should be Pack: 30 mL
should be told how to recognize the signs of Pack: 2 mL x 3’s. taken after meals to minimize nausea and vom-
POM CAPQUIN® (Evans)
blood disorders and advised to seek medical iting; if part or all a dose is vomited, the same
POM IBAJECT® (Crystal) Capsule, Chloroquine phosphate 250 mg; yellow cap.
attention as soon as possible if symptoms amount must be immediately readministered. marked ‘CG’ and ‘FEV’.
Injection, alpha-beta Arteether 150 mg per 2 mL; in
such as fever, sore throat, rash, mouth ulcers, amber coloured amp. Nursing action: Administer oral dose before 250 mg – 10’s.
purpura, bruising or bleeding develop. They Pack: 2 mL x 3’s. or after meals as prescribed; advise patient to
should also be told how to recognize signs of take at the same time each day to maintain POM CHLOMAL® (Medreich)
POM TERETINE® (Dabak) Tablet, Chloroquine phosphate 250 mg; white
hepatitis and advised to seek medical attention blood level.
Injection, Arteether 150 mg per 2 mL; in arachis oil. plain tab.
if symptoms such as anorexia, abnormal weight • Aspirate to avoid injecting drug into the blood
Pack: 2 mL x 3’s. 250 mg – 1 x 10’s; 100’s.
loss, asthenia, abdominal pains, fever, nausea system, prior to IM therapy (IV dose causes hy-
Dose: Adult, by deep IM injection, 150 mg (one amp.) Syrup, Chloroquine base 50 mg per 5 mL; orange
or vomiting develop. potension, asystole, heart block); rotate inj sites.
once daily for 3 consecutive days. coloured liquid.
• Avoid use in retinal or visual field changes or
Dose: See under Artesunate plus Amodi- Child: 3 mg/kg per day for 3 days. Pack: 60 mL amber bottle.
porphyria; children are extremely susceptible to
aquine. toxicity.
POM VOATHERM® (Visko) POM CHLOROCAP® (Rajrab)
POM Amodiaquine (WMF 6.5.3) Injection, α-β Arteether 150 mg per 2mL. Dose: NOTE: All doses are in terms of the Capsule, Chloroquine phosphate 250 mg; capsule
Tablets, Amodiaquine (as HCl) 153 mg, 200 mg. Pack: 3 x 2 mL. base. marked “CHLOROCAP 250”.
EMDEX
Treatment of malaria, by mouth, 250 mg – 10’s
POM CAMOQUIN® (Pfizer) POM ZIMMETAR® (Pharmgate)
Tablet, Amodiaquine HCl 200 mg; yellow scored tab. Injection, α−β Arteether 150 mg per 2 mL; in ADULT and CHILD 10 mg/kg followed POM CHLOROJECT® (Medreich)
200 mg – 25 x 3’s (in blister). arachis oil by 5 mg/kg 6–8 hours later; then 5 Injection, Chloroquine base 200 mg per 5 mL; in
Suspension, Amodiaquine (as HCl) 50 mg per 5 mL. Pack: 2 mL x 3’s mg/kg daily on next 2 days (or 10 mg/ amps.
Pack: 60 mL. kg for 2 days, followed by 5 mg/kg POM Chloroquine (Embassy)
POM LOQUIN® (Medreich) CHLOROQUINE daily on day 3); total dose, 25 mg/kg Injection, Chloroquine 40 mg per mL; in 5 mL amp.
Tablet, Amodiaquine (as HCl) 200 mg. Indications: Treatment of acute malaria caused over 3 days.
Dilution and Administration: According to POM Chloroquine (Emzor)
200 mg – 9’s. by P. malariae,P. vivax, and P. ovale (followed by Tablet, Chloroquine phosphate 250 mg; white plain
Paediatric suspension, Amodiaquine (as HCl) 50 mg primaquine to eliminate intrahepatic forms); manufacturer’s directions. Avoid rapid parenteral
administration (risk of toxic plasma concentrations biconvex tab.
per 5 mL. prophylaxis of malaria for pregnant women
and fatal cardiovascular collapse). 250 mg – 1000.
Pack: 60 mL. and non-immune individuals at risk; see notes Note: Parenteral Chloroquine – If a patient is Syrup, Chloroquine phosphate 80 mg per 5 mL
in EMDEX Vol. 3; rheumatic disorders (section unable to take chloroquine by mouth, e.g. due to Pack: 60 mL; 2 L.
α−β ARTEETHER
2.1.2). vomiting, adequate hydration should first be en- POM Chloroquine (Evans)
POM ALBETHER® (Pharma Ethics) Precautions: If patient continues to deteri- sured e.g. by admitting the patient and giving intra- Tablet, Chloroquine phosphate 250 mg; yellow
Injection, α−β Arteether 75 mg per mL; in 2 mL amp. orate after chloroquine—suspect resistance venous fluids or food and drink. The blood pressure plain tab.
Pack: 2 mL x 3’s (in amps) and administer quinine intravenously as emer- should be checked. Reducing fever before parenteral 250 mg – 10; 1000.
gency measure; hepatic impairment; renal therapy with chloroquine helps to minimise the risk Syrup, Chloroquine phosphate 80 mg per 5 mL; clear
POM ARTEBETA® (Jawa)
impairment (Appendix 4); pregnancy (but in of hypotension by minimising the peripheral vaso- colourless sweentened syrup.
Injection, α−β Arteether 75 mg, 150 mg; in amps.
dilation caused by fever. Chloroquine hydrochloride Pack: 60 mL.
75 mg – 1 mL x 3’s. malaria, benefit considered to outweigh risk;
should be given I.M. or, in the case of shock, I.V. every
150 mg – 2 mL x 3’s. Appendix 2); breastfeeding (Appendix 3); may 6 to 8 hours up to a maximum 900 mg base per day. POM Chloroquine (Fidson)
POM CIDAREX® (Teta) exacerbate psoriasis; neurological disorders Usually after 2 injections, the patient should feel Tablet, Chloroquine phosphate 250 mg.
Injection, α-β Arteether 150 mg per 2 mL (avoid for prophylaxis if history of epilepsy); better and therapy can be continued by the use of POM Chloroquine (Fil Pharma)
Pack: 2 mL x 3’s (in amps) may aggravate myasthenia gravis; severe GI tablets or syrup to complete the 10 mg base/kg/2nd Tablet, Chloroquine phosphate 250 mg.
disorders; G6PD deficiency; avoid concurrent day and 5 mg/kg/3rd day. 250 mg – 1000’s.
POM E MAL® (Fidson)
therapy with hepatotoxic drugs; interactions: POM Chloroquine (WMF 6.5.3)
Injection, α−β Arteether 150 mg per 2 mL; oily solu- POM Chloroquine (Gauze)
tion in 2 mL amp. Appendix 1. Tablets, Chloroquine (as phosphate or sulfate) 100 Liquid, Chloroquine phosphate 80 mg per 5 mL
Pack: 2 mL x 3’s. Adverse effects: Headache, GI disturbances; mg, 150 mg. Pack: 60 mL; 2 L
Indications: α−β Arteether is a synthetic derivative also convulsions; visual disturbances (retin- Oral liquid, Chloroquine (as phosphate or sulfate)
of artemisinin which is metabolized in the body opathy associated with long-term, high dose 50 mg/5 mL. POM Chloroquine (Goz)
Syrup, Chloroquine phosphate 80 mg (equiv. to 50
to dihydroartemisinin. It is a blood schizonticide therapy or inappropriate self-medication); POM Chloroquine (EDL 5.7/Restricted List)
specifically indicated for the treatment of chloro- mg Chloroquine base) per 5 mL.
depigmentation or loss of hair; rashes; pruri- Tablet, Chloroquine (as phosphate or sulfate) 200
quine resistant P. falciparum malaria and cerebral Pack: 60 mL; 2 L
tus—may become intolerable; bone-marrow mg.
malaria cases. POM Chloroquine (Jawa)
suppression; hypersensitivity reactions such
Dose: By IM injection only, Adult, 150 mg once daily POM 2-2-1 Forte (May & Baker) Injection, Chloroquine phosphate
as urticaria and angioedema; atrioventricular Capsule, Chloroquine sulfate 400 mg.
for 3 consecutive days. Pack: 4 x 50’s (in vials)
Child: 3 mg/kg per day for 3 consecutive block (may be result of inappropriate self-med- 400 mg – 5’s
days. Do not mix with other drugs in the ication); porphyria and psoriasis in susceptible Suspension, (4-6 years),Chloroquine sulfate 136 POM Chloroquine (Juhel)
450 | 9.3.1.4 Other antimalarial drugs 9.3.1.4 Other antimalarial drugs | 451
Tablet, Chloroquine phosphate 250 mg. 500 mg – 5; 100; 250. Tablet, Chloroquine phosphate 250 mg. Pack: 60 mL in glass bottle.
250 mg – 1000’s. 250 mg – 10’s (in blister); 1000’s
POM FAPCHLOR® (Food & Pharma) POM MAXIQUINE® (Vitabiotics)
Syrup, Chloroquine phosphate 80 mg per 5 mL Injection, Chloroquine phosphate 322 mg per 5 mL.
Tablet, Chloroquine phosphate 250 mg. Syrup, Chloroquine phosphate 81 mg, promethazine
Pack: 60 mL.
250 mg – 10 x 10; 1000. POM NOROLON® (GSK) HCl 3 mg, Paracetamol 100 mg per 5 mL
POM Chloroquine (Neimeth) Syrup, Chloroquine phosphate 80 mg per 5 mL Tablet, Chloroquine phosphate 250 mg; white bicon- Pack: 60 mL.
Tablet, Chloroquine phosphate 250 mg. Pack: 60 mL. vex tab. marked ‘NOROLON’.
500 mg – 5’s; 1000’s. 250 mg – 10. DIHYDROARTEMISININ
POM FEVOKINE® (GSK)
Capsule ,(Double-strength), Chloroquine phosphate
Tablet, Chloroquine phosphate 250 mg; white POM NOVALOR® (SKG) Pharmacology: Dihydroartemisinin belongs
500 mg (equiv. to 300 mg Chloroquine base).
500 mg – 5’s; 1000’s.
biconvex tab. marked ‘F’. Caplet, Chloroquine phosphate 250 mg; yellow to the sesquiterpene lactone group of antima-
250 mg – 10; 1000. caplet marked ‘CQ 250’ on one side and ‘SKG’ on larials; effective against P. falciparum, P. vivax,
Syrup, Chloroquine phosphate 80 mg per 5 mL
the reverse. P. malariae and P. ovale. It is a blood schizon-
Pack: 60 mL. POM FRAQUIN® (Embassy)
250 mg – 50 x 10’s; 1000’s. ticide and acts on the erythrocytic stages of
Tablet, Chloroquine phosphate 250 mg.
POM Chloroquine (N.C.I.) Syrup, Chloroquine phosphate 80 mg per 5 mL
250 mg – 10’s; 1000’s. the parasite which are directly responsible
Injection, Chloroquine phosphate 64.5 mg per mL. Pack: 60 mL in amber bottle.
Pack: 30 mL x 25’s. POM HIGHQUINE® (E-Globa)
for the clinical symptoms of the disease. It
POM QUINCAN® (Canopus) elicits its action on the plasmodium parasite
Injection, Chloroquine phosphate 64.5 mg per mL;
POM Chloroquine (Nomagbon) Injection, Chloroquine phosphate 40 mg per mL through inhibition of protein synthesis via
clear solution in glass vial.
Syrup, Chloroquine Phosphate 80 mg per 5 mL; Pack: 30 mL
Pack: 200’s vials. DNA replication. It is rapidly absorbed after oral
yellow syrup.
Pack: 60 mL (in glass bottle).
POM ROBAQUINE® (Swipha) administration (2.2mg/kg) and rectal insertion
POM HOCHIQUINE® (Hochiez)
Caplet, (forte) Chloroquine phosphate 500 mg (8mg/kg); Tmax in the serum are 1.33hrs and
Injection, Chloroquine phosphate 64.5 mg equiv.
POM Chloroquine (Rajrab) (equiv. to 300 mg Chloroquine base). 4.4hrs respectively. It is rapidly excreted from
to Chloroquine base 40 mg per mL; clear solution
Tablet, Chloroquine phosphate 250 mg; company 500 mg – 5. the body; the elimination half-life is 1.57hrs for
in amber vial.
EMDEX
logo marked on both sides of the tab.
Pack: 30 mL amber coloured glass vial. POM ROXYTEX® (Vixa) the tablet and 4.8hrs for the suppository. About
250 mg – 1000’s
Syrup, Chloroquine 80 mg per 5 mL; 60-mL pack has
Tablet, Chloroquine (as Phosphate) 250 mg; f-c tab. 0.15% of the drug is excreted unchanged in the
POM IBASTOP® (Afrab-Chem)
250 mg – 1 x 10’s. urine. Excretion is via glomerular filtration and
company logo on the cap. Oral drops, Chloroquine phosphate 60 mg (equiv. to
Pack: 60 mL; 2 L 37.5 mg Chloroquine base) per mL. POM SILAQUINE® (GoldMoore) tubular secretion.
Pack: 10 mL in amber bottle. Tablet, Chloroquine phosphate 128.8 mg per 2 mL Indications: In combination with Piperaquine
POM Chloroquine (Strides Vital)
(equiv. to 80 mg Chloroquine base). only, for the treatment of uncomplicated Fal-
Tablet, Chloroquine phosphate 250 mg; white tab. POM KLOQUIN® (Ranbaxy)
marked ‘CQ/250’. Tablet, Chloroquine phosphate 250 mg.
Pack: 10’s; 50’s. ciparum malaria.
250 mg – 1 x 10’s; 1000’s. 250 mg – 10; 1000. POM SIVOQUINE® (Adpharm) Precautions: Pregnancy (first trimester); use
Syrup, Chloroquine phosphate 80 mg per 5 mL Injection, Chloroquine phosphate 322.5 mg per 5 mL. in pregnancy during the second and third
POM CLOTIN® (Beta Drugs)
Pack: 60 mL; 2 L. Pack: 1 x 100’s trimesters has been proven to be safe but the
Injection, Chloroquine phosphate 128.8 mg per 2
benefit should be seen to outweigh the risk
mL equiv. to 80 mg chloroquine base; clear sterile POM LABQUIN® (Embassy) POM TAVQUINE® (Justeen)
solution in 2-mL ampoule. Injection, Chloroquine phosphate 40 mg per mL; Injection, Chloroquine phosphate 322 mg per 5 mL.
before administration.
Pack: 2-mL x 10’s; 2-mL x 50’s in 5 mL amp. Pack: 1 x 100’s. Adverse effects: Transient slight lowering of
Injection, Chloroquine phosphate 250 mg per 5 mL Pack: 30’s. reticulocyte count which normalizes during
equiv. to 155 mg chloroquine base; clear sterile POM ULTIQUINE® (Dizpharm) or after completion of therapy; dizziness, nau-
solution in 5-mL ampoule. POM LARIAGO® (IPCA) Syrup, Chloroquine phosphate 80 mg per 5 mL
sea, headache and abdominal pain may occur
Pack: 5-mL x 5’s; 5-mL x 100’s Tablet, Chloroquine phosphate 250 mg. Pack: 60 mL.
250 mg – 1000’s. within the first 2 days of treatment and may be
Injection, Chloroquine phosphate 322 mg per 5 mL POM VINAQUINE® (May & Baker) due to malaria itself.
equiv. to 200 mg chloroquine base; clear sterile POM MALADRIN® (P.Z.) Tablet, (Adult), Chloroquine sulfate 200 mg; white Dose: See under Dihydroartemisinin plus
solution in 5-mL ampoule. Tablet, Chloroquine phosphate 250 mg. tab. marked ‘VINAQUINE 200’
Pack: 5-mL x 5’s; 5-mL x 100’s.
Piperaquine.
Syrup, Chloroquine phosphate 80 mg per 5 mL 200 mg – 10’s
Note: Add freshly boiled and cooled water to marked
POM CQP-500® (GoldMoore) Tablet ,(Minor), Chloroquine sulfate 68 mg; white tab.
POM MATHEWQUINE® (Daily Need) level. Shake well before use. The suspending liquid
Tablet, Chloroquine phosphate 500 mg; f-c tab. marked ‘VINAQUINE 68 mg’
Syrup, Chloroquine phosphate 80 mg per 5 mL can be stored for 14 days in refrigerator, and 7 days
Pack: 5’s. 68 mg – 10’s
Pack: 60 mL. in room temperature.
Syrup, Chloroquine sulfate 68 mg per 5 mL
POM ELANQUINE® (Jopan) POM MEQUIN® (Fil Pharma) Pack: 60 mL POM ALAXIN® (Greenlife)
Tablet, Chloroquine (as phosphate) 250 mg; white Injection, Chloroquine (as phosphate) 40 mg per mL; Tablet, Dihydroartemisinin 60 mg; white coated tab.
scored tab. marked ‘JOPAN’ on one side and ‘ELAN- POM ZARQUINE® (Shrezar)
in 5 mL amp. and 30 mL vial. 60 mg – 8.
QUINE/250’ on the reverse. Injection, Chloroquine phosphate per 30 mL
Oral Suspension, Dihydroartemisinin 10 mg per 5 mL;
250 mg – 10 x 10’s (in blisters). POM Moko Chloroquine® (New Healthway) Pack: 1 x 50
white powder for reconstitution.
Syrup, Chloroquine phosphate 80 mg per 5 mL Compound preparations Pack: 80 mL.
POM EMZOQUINE® (Emzor) Pack: 60 mL. Suppository, Dihydroartemisinin 40 mg.
Tablet , Chloroquine phosphate 250 mg. POM COMBIQUNINE® (Adler)
POM NASMOQUIN® (NASDMU) 40 mg – 8’s.
250 mg – 10; 1000. Tablet, Chloroquine phosphate 250 mg, paracetamol
Syrup, Chloroquine phosphate 80 mg per 5 mL Tablet, Chloroquine phosphate 250 mg; white tab. 250 mg. POM CODISIN® (Geneith)
Pack: 60 mL; 2 L. marked “NASMOQUIN” on one side and “NASDMU” Pack: 30’s. Tablet, Dihydroartemisinin 60 mg; white divisible tab.
Capsule ,(forte), Chloroquine phosphate 500 mg on the reverse. 60 mg – 8’s.
(equiv. to 300mg Chloroquine base); yellow/green 250 mg – 1000. POM CONVULSAN® (Nomagbon) Suspension, Dihydroartemisinin 10 mg per 5 mL;
cap. Syrup, Chloroquine phosphate 80 mg, paracetamol powder for reconstitution in amber bottle.
POM NORMAQUINE® (Geneith) 120 mg per 5 mL; colourless liquid
452 | 9.3.2 Antiamoebic, antigiardial and antitrichomonal drugs 9.3.2 Antiamoebic, antigiardial and antitrichomonal drugs | 453
Pack: 80 mL. PRIMAQUINE widely used, but other compounds, including DILOXANIDE FUROATE
POM SANTECXIN® (Vixa) Indications: Elimination of intrahepatic forms clefamide, etofamide, and teclozan, are also Indications: Amoebiasis (asymptomatic
Tablet, Dihydroartemisinin 60 mg; white coated tab. of P. vivax and P. ovale (after standard chloro- effective. Treatment with diloxanide furoate is carriers in non-endemic areas; eradication of
60 mg – 8. quine therapy); elimination of gametocytes regarded as successful if stools are free of E. residual luminal amoebae after treatment of
Oral Suspension, Dihydroartemisinin 10 mg per 5 mL; of P. falciparum (after routine therapy with histolytica for one month. Several specimens invasive disease with other drugs)
white powder for reconstitution. a blood schizontocide); see notes in EMDEX should be examined in evaluating response Precautions: Pregnancy (defer treatment until
Pack: 80 mL. to treatment.
Vol. 3. after first trimester, Appendix 2); breastfeeding
POM TEMECXIN® (Bond) Contra-indications: Pregnancy (treatment Symptomatic (invasive) amoebiasis may be (Appendix 3).
Tablet, Dihydroartemisinin 60 mg with primaquine should be delayed until after classified as intestinal or extraintestinal. Intes- Adverse effects: Flatulence; occasionally,
delivery; Appendix 2); breastfeeding (Appendix tinal amoebiasis is either amoebic dysentery or vomiting, pruritus and urticaria.
HALOFANTRINE 3); conditions that predispose to granulocyto- non-dysenteric amoebic colitis. Extra-intestinal Dose: Amoebiasis (see above), by mouth,
Therapeutic category: Antimalarial penia (including active rheumatoid arthritis amoebiasis most commonly involves the liver, ADULT 500 mg 3 times daily for 10
Pharmacology: Halofantrine is a phenanthren- and lupus erythematosus). but may involve the skin, genito-urinary tract, days; CHILD over 25 kg, 20 mg/kg
emethanol antimalarial which is schizonticidal Precautions: Monitor blood count; if methae- lung and brain. Invasive amoebiasis is more daily in 3 divided doses for 10 days;
with a high degree of activity against the moglobinaemia or haemolysis occurs, with- likely in malnutrition, immunosuppression course may be repeated if necessary.
asexual erythrocytic stage of malaria parasites. draw treatment and consult physician; G6PD and pregnancy. Amoebic dysentery may take POM Diloxanide furoate (WMF 6.5.1)
It is devoid of significant activity against exo- deficiency (exclude before radical treatment for a fulminating course in late pregnancy and the Tablet, Diloxanide (as furoate) 500 mg.
erythrocytic or gametocyte stages of malaria P. vivax and P. ovale, but not before single dose puerperium; treatment with metronidazole
parasites. It is used for the treatment of single gametocytocidal treatment); interactions: POM CYSTOGYL® (Help Pharmacy)
may be life saving. In less severe infection,
Tablet, Diloxanide furoate 500 mg
or mixed infections of Plasmodium falciparum Appendix 1. metronidazole should, if possible, be avoided 500 mg – 10’s (in blister)
or Plasmodium vivax. It has been shown to be Adverse effects: Anorexia, N & V, abdominal in the first trimester. All patients with invasive
EMDEX
effective against P. falciparum in areas where pain; acute haemolytic anaemia (frequently amoebiasis require treatment with a systemi- METRONIDAZOLE
chloroquine or multi-drug resistant strains are in G6PD deficiency); rarely, methaemoglobi- cally active compound such as metronidazole,
Therapeutic category: Amoebicide; Anti-
common. Limited data indicates favourable naemia, haemoglobinuria, agranulocytosis, ornidazole and tinidazole followed by a
protozoal
results with P. Ovale and P. Malariae. It should granulocytopenia and leukopenia. luminal amoebicide in order to eliminate any
Indications: Invasive amoebiasis and giardia-
not be used as either a casual or suppressive Dose: NOTE. All doses are in terms of the base surviving organisms in the colon. Combined
sis; trichomoniasis; tissue nematode infections
prophylactic. Radical treatment of P. vivax and P. preparations are useful.
(section 9.4.1.3); bacterial infections (section
Indications: Consult manufacturer's literature. ovale malaria (after standard chlo-
In severe cases of amoebic dysentery, tetra- 9.1.2.6); Helicobacter pylori eradication (sec-
Contra-indications: Pregnancy and breast roquine therapy), by mouth, ADULT
cycline given in combination with a systemic tion 4.1).
feeding (avoid during treatment); cardiac 250 µg/kg daily (or 15 mg daily) for
amoebicide lessens the risk of superinfection, Contra-indications: Chronic alcohol depend-
disorders. 14 days; CHILD 250 µg/kg daily for
intestinal perforation and peritonitis. Hepatic ence.
Interactions: Avoid co-administration with 14 days; in G6PD deficiency, ADULT
abscesses should be lanced by needle aspi- Precautions: Disulfiram-like reaction with
other drugs which may induce arrhythmias 750 µg/kg once a week for 8 weeks;
ration. alcohol; hepatic impairment and hepatic
viz chloroquine, mefloquine, quinine, TCAs, CHILD 500–750 µg/kg once a week
GIARDIASIS encephalopathy (Appendix 5); pregnancy
antipsychotics, certain antiarrhythmics, and for 8 weeks.
(Appendix 2; see also notes above); breast-
antihistamines such as astemizole. Gametocytocidal treatment of P. falci- Giardiasis is caused by Giardia intestinalis and
feeding (Appendix 3); clinical and laboratory
Adverse effects: Abdominal pain, diarrhoea, parum (after routine blood schizonto- is acquired by oral ingestion of Giardia cysts.
monitoring in courses lasting longer than 10
pruritus and skin rash. cide therapy), by mouth, ADULT and Giardiasis can be treated with tinidazole in a
days; interactions: Appendix 1.
Advice to patients: Food, especially high fat CHILD 500–750 µg/kg as a single single dose or with another 5-nitroimidazole
Adverse effects: Nausea, vomiting, unpleas-
food, enhances absorption of halofantrine and dose. such as metronidazole; both are highly effec-
ant metallic taste, furred tongue and GI
may increase the incidence of adverse effects. POM Primaquine (WMF 6.5.3) tive and should be offered when practicable to
disturbances; rarely headache, drowsiness,
Dose: Consult manufacturer's literature. Tablets, Primaquine (as diphosphate) 7.5 mg, 15 mg. all infected patients. Family and institutional
dizziness, ataxia, darkening of urine, erythema
POM ADFANTRIN® (Astra) contacts should also be treated. Larger epi-
multiforme, pruritus, urticaria, angioedema,
Tablet, Halofantrine 250 mg. 9.3.2 Antiamoebic, antigiardial and demics are difficult to eradicate because of the
and anaphylaxis; abnormal liver function tests,
250 mg – 6’s (in blister) antitrichomonal drugs high proportion of symptomless carriers and
hepatitis, jaundice, thrombocytopenia, aplastic
Oral solution, Halofantrine 100 mg per 5 mL because excreted cysts can survive for long
Pack: 30 mL in bottle.
AMOEBIASIS anaemia, myalgia, arthralgia; peripheral neu-
periods outside the human host.
Amoebic dysentery is caused by Entamoeba ropathy, epileptiform seizures, leukopenia, on
POM HALFAN® (GSK) TRICHOMONIASIS prolonged or high dosage regimens.
Tablets, Halofantrine HCl 250 mg; white, scored, histolytica. It is transmitted by the faeco-oral
route and infection is usually caused by in- Trichomoniasis is an infection of the genito-uri- Advice to patients: Urine may be discoloured
capsule-shaped tab.
gestion of cysts from contaminated food and nary tract caused by Trichomonas vaginalis to a dark or reddish-brown; avoid alcohol dur-
250 mg – 6.
Suspension, Halofantrine HCl 100 mg per 5 mL; drink. Asymptomatic carriers are common and transmission is usually sexual. In women ing and for at least 48 hours after treatment;
white suspension. in endemic areas. In non-endemic areas, it causes vaginitis although some are asymp- may cause metallic taste; may be taken with
Pack: 30 mL. symptomless carriers should be treated with a tomatic. It is usually asymptomatic in men but food to minimise stomach upset; notify phy-
luminal amoebicide which will reduce the risk may cause urethritis. Patients and their sexual sician if numbness or tingling in extremities
POM VISHANTRIN® (Visko)
of transmission and protect the patient from in- partners should be treated with metronida- occurs.
Tablet, Halofantrine 250 mg
Pack size: 1 x 6’s vasive amoebiasis. Diloxanide furoate is most zole or other nitroimidazole. Nursing action: Administer after meals to
minimise GI distress and its metallic taste.
• The IV form should be administered by slow infu- POM AMBIGYL® (Ranbaxy) POM FLAGYL® (Sanofi-Aventis) Injection (IV), Metronidazole 500 mg per 100 mL.
sion only. Don’t give by IV push. Tablet, Metronidazole 200 mg. Tablet, Metronidazole 200 mg; white scored tab. Pack: 100 mL.
• Advise patient’s partner to use condom for coitus, if 200 mg – 1000. marked ‘FLAGYL 200’.
POM METROGEM® (Gemini)
receiving treatment for trichomoniasis, to prevent Suspension, Metronidazole benzoyloxylate 200 mg 200 mg – 21; 250.
Tablets, Metronidazole (as benzoate) 200 mg, 400
cross transmission. per 5 mL. Suspension, Metronidazole (as benzoate) 200 mg per
mg.
• Emphasize good personal hygiene after bowel Pack: 60 mL. 5 mL; clear and colourless solution.
Pediatric Suspension, Metronidazole 200 mg per 5
movement viz handwashing and care of perineum. Pack: 60 mL.
POM AMEBANIL® (Dana) mL; banana and raspberry flavoured susp.
• If indicated during pregnancy for trichomoniasis, Infusion, Metronidazole 0.5%; in 100 mL viaflex
Tablet, Metronidazole 200 mg; uncoated tab
the 7-day regimen is preferred to the 2-g single IV bag. POM METROGYL® (Hochiez)
200 mg – 10 x 10’s (in blisters); 1000’s; 100’s (in jar)
dose regimen. Pessary, See under section 11.2.2. Tablet, Metronidazole 200 mg, 400 mg; f-c tab.
Suspension, Metronidazole (as Benzoate) 200 mg
• Use cautiously in patients with a history of blood 200 mg – 10’s
per 5 mL POM GARYMET® (Agary)
dyscrasia or CNS disorder, and in patients with 400 mg – 10’s
Pack: 60 mL Tablet, Metronidazole 200 mg.
retinal or visual field changes.
200 mg – 1000’s (n carton); 10 x 10’s (in blisters) POM METROJECT® (Crystal)
• Use with caution in hepatic disease or alcoholism POM AMIBAGYL® (Afrab-chem)
and in conjunction with known hepatotoxic drugs. Infusion, Metronidazole 500 mg/100 mL.
Tablet, Metronidazole 200 mg; off-white scored tab. POM GG Metronidazole (Geneith)
Pack: 100 mL bottle.
Dose: Invasive amoebiasis, by mouth, ADULT marked afrab. Injection, Metronidazole 500 mg per 100 mL.
and CHILD 30 mg/kg daily in 3 200 mg – 1000. Pack: 100 mL. POM METROLEX® (Med Impex)
divided doses for 8–10 days; subse- Suspension, Metronidazole 200 mg per 5 mL Infusion, Metronidazole 0.5% w/v.
POM IVEMETRO® (Zoomota)
quent course of luminal amoebicide Pack: 60 mL; 100 mL. Pack: 100 mL bottle.
Infusion, Metronidazole 5mg/mL; colourless solution
(see notes above). POM AVROGYL® (Avro) in 100 mL flexi bottle. POM METROMAX® (GoldMoore)
Invasive amoebiasis (if oral adminis- Tablet, Metronidazole 200 mg; white uncoated tab. Pack: 100 mL. Tablet, Metronidazole 200 mg.
tration not possible), by IV infusion, 200 mg – 10 x 10’s (in blisters). Pack: 1 x 10’s; 1 x 1000’s.
POM JAWAGYL® (Jawa)
ADULT and CHILD 30 mg/kg daily in Tablet, Metronidazole 400 mg; yellow tab.
EMDEX
Suspension, Metronidazole 200 mg per 5 mL. POM METROMED® (Embassy)
Suspension, Metronidazole (as benzoate) 200 mg per
3 divided doses (until patient able Pack: 60 mL (in pilfer proof bottle). Tablet, Metronidazole 200 mg.
5 mL; pleasantly flavoured.
to complete course with oral drugs); 200 mg – 100’s; 1000’s.
Pack: 60 mL. POM JUGYL® (Juhel)
subsequent course of luminal amoe- Tablets, Metronidazole 200 mg, 400 mg; white,
POM BONAGYL® (Bond) POM METRONE® (Fidson)
bicide (see notes above). scored tabs. Suspension, Metronidazole (as benzoate) 200 mg
Giardiasis, by mouth, ADULT 2 g once Tablet, Metronidazole 200 mg
Pack: 10 x 10’s; 100 x 10’s; 1000’s. per 5 mL.
daily for 3 days; CHILD 15 mg/kg daily POM CANOGYL® (Canopus) Suspension, Metronidazole (as benzoate) 200 mg
POM Metronidazole (Ceenek)
in divided doses for 5–10 days. Injection, Metronidazole 500 mg per 100 mL. per 5 mL.
Pack: 100 mL Pack: 60 mL. Tablet, Metronidazole 200 mg.
Urogenital trichomoniasis, by mouth, 200 mg – 1000’s; 10 x 100’s (in blisters).
ADULT 2 g as a single dose or Infusion (i.v.), Metronidazole 0.5%.
POM CAREGYL® (Dizpharm) Oral suspension, Metronidazole 200 mg per 5 mL;
400–500 mg twice daily for 7 days; Pack: 100 mL.
Tablet, Metronidazole 200 mg; white scored tab. yellowish suspension
sexual partners should be treated marked “m/200”. POM LAMETRO® (Mecure) Pack: 60 mL
concomitantly 200 mg – 10 x 10; 1000. Tablet, Metronidazole 200 mg; yellow tab. marked
‘LAMETRO’ and ‘200’. POM Metronidazole (Dana)
Note: In amoebiasis and giardiasis, various dosage
POM CIKAGYL® (Michelle Lab) Infusion, Metronidazole 500 mg, sodium chloride 0.9
regimens are used and definitive recommendations 200 mg – 10 x 10’s; 1 x 1000’s.
Tablet, Metronidazole 200 mg g, water for injection q.s per 100 mL.
should be based on local experience.
200 mg – 10 x 10’s (in blisters); 1000’s (in jars) POM LOXAGYL® (May & Baker) Pack: PVC Pouches of 100 mL overwrapped & packed
Administration: Metronidazole tablets should Tablet, Metronidazole 200 mg; white scored tab. in mono carton.
be swallowed whole with water, during or after POM Dr. Meyer’s Metrocide® (Farmex)
marked ‘LOXAGYL 200’
a meal; metronidazole suspension should be Suspension, Metronidazole (as benzoate) 200 mg POM Metronidazole (Evans)
200 mg – 10 x 10’s.
per 5 mL. Suspension, Metronidazole 200 mg per 5 mL.
taken one hour before a meal. Avoid alcoholic Tablet, Metronidazole 400 mg; yellow scored tab.
Pack: 60 mL. 200 mg – 60 mL
beverages. marked ‘LOXAGYL 200’
POM ELAGYL® (Jopan) 400 mg – 10 x 10’s POM Metronidazole (Goz)
POM Metronidazole (WMF 6.5.1) Suspension, Metronidazole (as benzoate) 200 mg per
Tablet, Metronidazole 200 mg; yellow scored tab. Suspension, Metronidazole BP 200 mg per 5 mL.
Tablets, Metronidazole 200-500 mg. 5 mL; cream coloured susp.
marked ‘JOPAN’ on one side and ‘ELAGYL/200’ on Pack: 60 mL
Oral liquid, Metronidazole (as benzoate) 200 mg/5 Pack: 60 mL
the reverse.
mL. POM Metronidazole (Mopson)
Injection, Metronidazole 500 mg; in 100-mL vial. POM METROZOLE® (Vitabiotics) Tablet, Metronidazole 200 mg
POM EMGYL® (Emzor) Suspension, Metronidazole 200 mg 200 mg – 1000’s
POM Metronidazole (EDL 5.1 & 5.5) Pack: 60 mL
Tablet, (200 mg), Metronidazole 200 mg; white tab. Suspension, Metronidazole (as benzoyl) 200 mg
Tablets, Metronidazole 200 mg, 400 mg.
200 mg – 1000. per 5 mL
Oral liquid, Metronidazole 200 mg per 5 mL POM METRODINE® (Drugfield)
Tablet, Metronidazole 400 mg; yellow tab. Pack: 60 mL; 2 L
Tablet, Metronidazole 200 mg
POM ALPHAGYL® (Alpha) Suspension, Metronidazole (as benzoate) 200 mg
200 mg – 10 x 10’s (in blisters) POM Metronidazole (Pemason)
Tablet, Metronidazole 200 mg, 400 mg; scored, white, per 5 mL.
Suspension, Metronidazole 200 mg per 5 mL IV Infusion, Metronidazole 500 mg per 100 mL
biconvex tab Pack: 60 mL.
Pack: 60 mL
Pack: 100 x 10’s(in blisters) POM METROPAED® (SKG)
POM FAPOGYL® (Food & Pharma)
Suspension, Metronidazole 200 mg per 5 mL POM METROFUSION® (Hochiez) Suspension, Metronidazole (as benzoate) 200 mg per
Tablet, Metronidazole 200 mg.
Pack: 60 mL Injection, Metronidazole 0.5% w/v. 5 mL; yellow, flavoured susp.
200 mg – 1000.
Infusion, Metronidazole 0.5 g per 100 mL Pack: 100 mL. Pack: 60 mL in amber bottle.
Suspension, Metronidazole 200 mg per 5 mL
Pack:100 mL
Pack: 60 mL. POM METROGATE® (Pharmgate) POM METROTAB® (SKG)
Tablet, (200 mg), Metronidazole 200 mg; white, 200 mg – 10 x 10’s. Precautions: Renal and hepatic impairment. infections, trichomonal vaginosis/infections,
round, biconvex, uncoated tab. Suspension, Metronidazole 125 mg per 5 mL; yellow Pregnancy and lactation. Child <1 yr. and in malodorous tumours and ulcers due to
200 mg – 10 x 10’s (in blisters); 1000’s. susp. with mixed fruit flavour. Interactions: May possibly interact with highly anaerobic infections.
Tablet, (400 mg), Metronidazole 400 mg; yellow tab. Pack: 60 mL. protein-bound drugs e.g. warfarin. Increased Contra-indications: Hypersensitivity to
400 mg – 10 x 10’s (in blisters); 1000’s. Injection, Metronidazole 500 mg per 100 mL;
AUC with food. quinolones and 5-nitroimidazoles.
colourless solution in a 100-mL plastic wrapped
POM METROZALE® (Adler) Adverse effects: Asthenia, fever, pain, allergic Precautions: Children and adolescents. Epi-
transparent infusion bottle with a blue cap.
Infusion, Metronidazole 0.5%. reactions, pelvic pain, chills, dizziness, somno- lepsy, CNS damage, and severe cerebrovascular
Pack: 100 mL.
Pack: 100 mL. lence, insomnia, tremor, hypesthesia, vomiting, disease. Renal and hepatic impairment. Preg-
POM SOFAGYL® (Sofak)
POM METROZOL® (Vitabiotics) dyspepsia, anorexia, flatulence, constipation, nancy, lactation.
Tablet, Metronidazole 200 mg
200 mg – 100’s; 1000’s
dry mouth, thirst, discoloured urine, dysuria, Interactions: Ornidazole with alcohol pro-
200 mg – 1000’s. amenorrhea, kidney pain, skin rash, eye dis- vokes a disulfiram like reaction. Acute confu-
Suspension, Metronidazole 200 mg per 5 mL
POM MIRA-METRO® (Miraflash) Pack: 60 mL colouration. Ear ache, tachycardia, syncope, sion and psychosis have been associated with
Injection, Metronidazole 500 mg per 100 mL; in hypertension, leg cramps, spontaneous bone ornidazole and disulfiram. Ornidazole impairs
POM TAVZOLE® (Justeen)
water for injection. fracture. the metabolism or excretion of drugs such as
Pack: 100 mL
Pack: 10 x 10’s. Dose: Administer with food for enhanced warfarin, phenytoin, lithium and fluorouracil.
POM MOKOGYL® (New Healthway) absorption Mineral supplements, vitamins with iron or
POM TRICOGYN® (Bentos) By mouth, Amoebiasis, giardiasis, cryp- minerals, or antacids containing aluminium or
Tablets, Metronidazole 200 mg (white); 400 mg
Tablet, Metronidazole 200 mg. tosporidiosis and helminthic infections, magnesium should not be taken within 2 hours
(yellow).
200 mg – 10 x 20’s; 1000’s.
Suspension, Metronidazole 200 mg per 5 mL Adult & Child (>12 years), 500 mg every before or after a dose of Ofloxacin.
Suspension, Metronidazole 200 mg per 5 mL.
POM MYDAZOLE® (Topway) Pack: 60 mL 12 hours for 3 days. Adverse effects: Nausea, insomnia, dizzi-
Tablet, Metronidazole 200 mg; yellow scored tab. Child (1-3 years): 100 mg every 12 ness, furry tongue, glossitis, stomatitis and
EMDEX
POM TRIMETRO (Phillips) hours; 4-11 years, 200 mg every 12 diarrhoea, fleeting joint pains, sometimes
marked “TOPWAY’ on one side and ‘METRO-200’
Injection (IV), Metronidazole 500 mg per 100 mL.
on the reverse. hours. All doses to be taken for 3 days. resembling serum sickness.
Pack: 100 mL.
200 mg – 100’s; 1000’s (in blisters). Fasciolasis, Adult, 1250 mg every 12 Ornidazole: Convulsive seizures, peripheral
POM TROMET® (Elbe) hours for 7 days. neuropathy; dizziness, vertigo, ataxia, con-
POM NADAZOLE® (NASDMU)
Infusion, Metronidazole. fusion, irritability, depression, weakness,
Tablet, Metronidazole 200 mg; marked “200 NADA- POM NETAZOX® (Zoomota)
Pack: 100 mL. insomnia, headache, cystitis, polyuria, sense
ZOLE” on one side and “NASDMU” on reverse side. Tablet, Nitazoxanide 500 mg; f-c yellow tab.
200 mg – 1000; 10 x 10’s POM TRONID® (Neimeth) 500 mg – 10 x 6’s. of pelvic pressure.
Tablet, Metronidazole 200 mg. Ofloxacin: Flatulence, pruritus vulvae, vaginitis,
POM NEMEGYL® (Nemel) POM NETAZOX® (Zoomota)
200 mg – 100’s. fatigue, rash, drowsiness, dry mouth, altered
Tablet, Metronidazole 200 mg; yellow uncoated tab. Tablet, Nitazoxanide 500 mg; f-c tab.
Suspension, Metronidazole (as benzoate) 200 mg taste, visual disturbances, decreased appetite,
200 mg – 10 x 10’s (in blisters); 1000’s (in tin). 500 mg – 6’s (in blisters).
per 5 mL. nervousness and pain in the chest and trunk.
POM NIRMET® (Jawa) Pack: 60 mL. Tablet, (Dispersable), Nitazoxanide 200 mg.
200 mg – 6’s (in blisters). Dose: Adult, by mouth, Susceptible protozoal
Infusion, (IV), Metronidazole 500 mg per 100 mL.
POM TROZ® (Global Organics) Oral suspension, Nitazoxanide 100 mg per 5 mL; and polymicrobial aerobic and anaero-
Pack: 100 mL.
Injection, Metronidazole 500 mg, sodium chloride powder for reconstitution. bic infections, dysentery ofmixed origin
POM NIZOLE® (Hovid) 800 mg, water for injection per 100 mL Pack: 30 mL. and intra-abdominal infections, 1
Tablet, Metronidazole 200 mg. Pack: 100 mL
tablet every 12 hours for 5-10 days.
200 mg – 10; 100. ORNIDAOLE plus OFLOXACIN
POM ULTRAGYL® (Strides Vital) Trichomonal infections, 3 tablets as a
POM PILGYL® (Pharchem) Tablet, Metronidazole 200 mg; yellow tab. marked Therapeutic category: Antiprotozoal; Anti- single dose; alternatively, BID dosing
Tablet, (200 mg), Metronidazole 200 mg; yellow ‘MTZ/200’ on one side and doubly scored on the bacterial for a 5-day course.
tab. marked ‘PIL’ on one side and ‘METRO 200’ on reverse. Pharmacology: Ornidazole, a synthetic anti- Malodourous tumours and ulcers due
the reverse. 200 mg – 10 x 10’s; 1000’s. bacterial compound, interfers with susceptible to anaerobic infections, 1 tabet every
200 mg – 10’s (in blister); 1000’s (in securitainer).
POM VINCOGYL® (Vinco) microbial DNA. It possesses direct tricho- 12 hours for 5-10 days.
Tablet, (400 mg), Metronidazole 400 mg
Tablets, Metronidazole 200 mg, 400 mg. monacidal and amoebicidal activity against Note: Limit the use of the combination to failed
400 mg – 1000’s (in securitainer).
Balantidium coli, Blastocystis Hominis, Tricho- treatment with individual drugs or recurrent infec-
Suspension, Metronidazole 200 mg per 5 mL; yellow POM ZIMAGIL® (Gauze)
monas vaginalis, Entamoeba histolytica, Giardia tion due to microbial resistance.
flavoured susp. Oral Liquid, Metronidazole 200 mg per 5 mL
Pack: 60 mL (in amber bottle). 200 mg – 60 mL; 2 L lamblia, and obligate anaerobic bacteria. POM ECOFLOCIN® Plus (Pinnacle)
Gram-negative anaerobic Bacilli and Clostridia Tablet, Ofloxacin 200 mg, ornidazole 500 mg; f-c tab.
POM RABGYL® (Rajrab) POM ZOLATROL® (Watson)
are also susceptible. Ofloxacin like other Pack: 10’s
Tablet, Metronidazole 200 mg; white scored tab. Caplet, Metronidazole 400 mg; yellow tab.
marked with company logo. 400 mg – 10 x 10’s; 1000’s. quinolones exerts its antimicrobial action by POM NIDOF® (Tamar & Pharez)
200 mg – 100’s; 1000’s (in blisters). inhibiting bacterial topoisomerase IV and DNA Tablet, Ornidazole 500 mg, ofloxacin 200 mg; f-c tab
NITAZOXANIDE gyrase enzymes required for DNA replication, Pack: 10 x 1 x 10’s (in blisters)
POM RAPHAGYL® (Rapha)
Therapeutic category: Antiamoebic, antipro- transcription, repair and recombination. It has
Tablet, Metronidazole 400 mg POM ORNILOX® (Micronova)
400 mg – 1 x 10 x 10's tozoal agent. activity against a wide range of gram-negative Tablet, Ornidazole 500 mg, ofloxacin 200 mg; f-c tab.
Indications: Diarrhoea caused by Giardia and gram-positive microorganisms. Pack: 10’s
POM SHALMET® (Shalina) Indications: Susceptible protozoal and pol-
Tablet, Metronidazole 200 mg; green tab. marked lamblia or Crytosporidium parvum.
Contra-indications: Hypersensitivity. ymicrobial aerobic and anaerobic infections.
‘Shalmet’
Dysentery of mixed origin, intra-abdominal
458 | 9.3.3 Antileishmanial drugs 9.3.3 Antileishmanial drugs | 459
SECNIDAZOLE Pharmacology: As for Metronidazole but has ment or disseminated progressive disease in serious disfigurement or disability, antimonials
Therapeutic category: Antimicrobial agent of longer duration of action. the cutaneous form and to a fatal diseases should be administered systemically.
nitro-imidazole group Indications: As for metronidazole. without treatment for the visceral form. With Infections due to L. braziliensis and the less
Indications: Trichomonas vaginalis, urethritis Contra-indications, Precautions, Adverse ef- some exceptions (visceral leishmaniasis in common L. panamensis should be treated
and vaginitis, intestinal amoebiasis; hepatic fects, Nursing action and Advice to patients: South Asia and in Eastern Africa and cutaneous with systemic antimonials because of the risk
amoebiasis. See under Metronidazole. leishmaniasis caused by Leishmania tropica), of mucosal involvement. L. aethiopica is less
Contra-indications: Hypersensitivity to Dose: Anaerobic infections, by mouth, 2 g human beings incidental hosts of infection, responsive at conventional doses and the sores
imidazole derivatives; first three months of initially as a single dose, followed by 1 and mammals such as rodents and canids are should be left to heal spontaneously if there is
pregnancy; breast-feeding. g daily or 500 mg twice daily, usually reservoir hots. The parasites are transmitted no evidence of diffuse cutaneous involvement.
Precautions: Disulfiram-like reaction with for 5-6 days. by sandflies. L. guyanensis infections should be treated with
alcohol Non-specific vaginitis, trichomoniasis, VISCERAL LEISHMANIASIS pentamidine.
Interactions: Alcohol, oral anticoagulants giardiasis, and acute ulcerative gingivi-
tis, by mouth, 2 g as a single dose. Visceral leishmaniasis (kala-azar) is caused MUCOCUTANEOUS LEISHMANIASIS
Adverse effects: Metallic taste in the mouth,
Intestinal amoebiasis, by mouth, 2 g by Leishmania donovani and L. infantum (Old Mucocutaneous leishmaniasis is caused by L.
gastralgia, nausea, abdominal pain, vomiting,
daily for 3 days. World) and by L. chagasi (New World), and it is braziliensis and L. panamensis. In this form of
stomatitis; rarely, vertigo, moderate neurolog-
See lit. for details. usually responsive initially to the pentavalent the disease the primary lesions do not heal
ical troubles.
antimony compounds, meglumine antimo- and spread to the mucosa may occur. It usually
Advice to patients, Nursing action: See under POM Tinidazole (EDL 5.5) niate or sodium stibogluconate at a dosage responds to antimonials and, when relapses
Metronidazole. Tablet, Tinidazole 500 mg. of 20mg/kg/daily for 28 days. Patients are occur, more extended courses of treatment
Dose: Trichomonas vaginalis infections, by
POM AMTIBA® (Interpharma) considered to be parasitologically cured when are often successful. Patients who still fail to
mouth, 2 g (4 tabs) as a single dose. Tablet, Tinidazole 500 mg no parasites are detected in splenic or bone respond should receive amphotericin B or
Intestinal amoebiasis (acute, asympto- 500 mg – 25 x 4’s
EMDEX
marrow aspirates. Amphotericin B, miltefos- pentamidine isetionate, although neither
matic), by mouth, Adult, 2 g (4 tabs)
POM BATINA® (Bakangizo) ine or combinations of antimonials miltefosine, treatment is highly satisfactory. Because of re-
as a single dose.
Tablet, Tinidazole 500 mg; yellow oblong tab. amphotericin, paromomycin (aminosidine), sistance to antimonials, L. aethiopica infections
Child: 30 mg/kg b.wt. as a single dose.
500 mg – 2 x 10’s or pentamidine isetionate have been used should be treated with pentamidine from the
Hepatic amoebiasis, by mouth, Adult, Injection, Tinidazole 400 mg per 10 mL with success in patients in relapse who have outset until complete healing occurs.
1.5 g (3 tabs) once daily or in divided 400 mg – 100 mL become unresponsive to antimonials alone. In
doses for 5 days. Emergency use of corticosteroids may be
POM FASIGYN® (Pfizer) some areas, resistance to antimonials is wide-
Child: 30 mg/kg b.wt. once daily or in needed to control pharyngeal or tracheal
Tablet, Tinidazole 500 mg; white f-c tab. spread (India). In these areas, amphotericin B
divided doses for 5 days. oedema produced by severe inflammation
500 mg – 4; 100. , parenteral paromomycin (aminosidine), or
Note: To be administered with meals to avoid GI resulting from antigens liberated from dead
symptoms and metallic taste in the mouth. POM TINDEX®-500 (Embassy) oral miltefosine [not included on WHO Model
List], can be used for the treatment of visceral parasites during the early phase of treatment.
Tablet, Tinadazole 500 mg; f-c tab
POM BACTROSEC®(Help Pharmacy) leishmaniasis. Antibiotics may also be needed to treat sec-
Tablet, Secnidazole 500 mg ondary infections, and plastic surgery offers the
Dose: Anaerobic infections, by mouth, 2 g initially as CUTANEOUS LEISHMANIASIS
a single dose, followed by 1 g daily or 500 only means of ameliorating disfiguring scars.
POM FLAGENTYL® (Sanofi-Aventis) mg twice daily, usually for 5-6 days. Cutaneous leishmaniasis comprises two con-
ditions. The Old World variety is caused by L. DIFFUSE CUTANEOUS LEISHMANIASIS
Tablet, Secnidazole 500 mg; yellowish white scored Non specific vaginitis, trichomoniasis, gi-
f-c tab. ardiasis and acute ulcerative gingivitis, by tropica, L. major, L. infantum and L. aethiopica. Diffuse cutaneous leishmaniasis usually occurs
500 mg – 4’s mouth, 2 g as a single dose. The New World variety is caused by L. amazon- following infection with L. amazonensis, L.
Intestinal amoebiasis, by mouth, 2 g daily ensis, L. mexicana, L. peruviana, L. guyanensis, L. aethiopica or L. mexicana and is usually treated
POM SECDYL® (Solidum) for 3 days.
Tablet, Secnidazole 500 mg; f-c tab. panamensis and L. braziliensis. These conditions with antimonial compounds, but relapses
500 mg – 4’s POM TINEXDA® (Vixa) are characterized by a cell-mediated reaction must be expected and repeated courses of
Capsule, Tinidazole 500 mg of varying intensity at the site of inoculation. pentamidine isetionate may be needed until
POM SECTAB® (Digitall) 500 mg – 1 x 10’s The New World variety tends to be more severe clinical immunity is established.
Tablet, Secnidazole 500 mg; f-c tab.
500 mg – 1 x 4’s POM TINIMARK® (Mark) and slower to heal. Infections caused by L.
Infusion, Tinidazole 0.2%, sodium chloride 0.79% per major, L. mexicana, L. tropica and L. peruviana, AMPHOTERICIN B
POM SECWID® (May & Baker) are responsive to intralesional injections of
100 mL; water for injection. Indications: Visceral and mucocutaneous
Caplet, Secnidazole 500 mg; scored caplet. Pack: 400 mL antimonial compounds. leishmaniasis unresponsive to pentavalent
500 mg – 4’s.
POM TINIZOL® (Shalina) Mild lesions can often be left to heal spontane- antimony compounds; fungal infections
POM TAGERA® Forte (Phillips) Tablet, Tinidazole 500 mg f-c tab; yellow tab. (section 9.2).
ously. However, it is preferable to treat L. tropica
Tablet, Secnidazole 1 g; f-c tab. 500 mg – 4’s (in blisters). Precautions: Close medical supervision
1 g – 2’s (in blisters). infections with a view to reducing transmission
since humans seem to be the only host. When throughout treatment and initial test dose
POM ZARYL® (Alvid) 9.3.3 Antileishmanial drugs the lesion is inflamed or ulcerated, larger than required (see note below); renal impairment
Tablet, Secnidazole 500 mg; tab. marked ‘ZRL’ (Appendix 4); hepatic and renal function tests;
Leishmaniasis is caused by the parasitic 3 cm of diameter, the lesion is in the face close
500 mg – 4’s blood counts and plasma electrolyte monitor-
protozoa Leishmania. It can be categorized to the eyes, there are 3 or more lesions, or when
as visceral, cutaneous or mucocutaneous. It there is obstruction of lymphatic drainage, ing; corticosteroids (avoid except to control
TINIDAZOLE reactions); pregnancy (Appendix 2); breast-
may be a self-limiting localized skin lesion sporotricoid form, next to joints, superinfected
Therapeutic category: Antimicrobial agent. or destruction of cartilage creates a risk of feeding (Appendix 3); avoid rapid infusion
but may range from this to mucosal involve-
460 | 9.3.3 Antileishmanial drugs 9.3.3 Antileishmanial drugs | 461
(risk of arrhythmias); interactions: Appendix 1. involvement)—may require corticosteroids. amphotericin B (see below). PENTAMIDINE
ANAPHYLAXIS: Anaphylaxis occurs rarely with Adverse effects: Anorexia, nausea, vomiting, Diffuse cutaneous leishmaniasis (L. Indications: Leishmaniasis (see notes, above);
intravenous amphotericin B and a test dose is abdominal pain, ECG changes (possibly requir- amazonensis), by IM injection, ADULT African trypanosomiasis (section 9.3.4.1);
advisable before the first infusion. The patient ing dose reduction or withdrawal), cough (see and CHILD 20 mg/kg daily for several Pneumocystis carinii (Pneumocystis jiroveci)
should be observed for about 30 minutes after Precautions); headache, lethargy, arthralgia, months after clinical improvement pneumonia (section 9.3.5).
the test dose. myalgia; raised liver enzymes; renal function occurs; relapse must be expected Contra-indications: Severe renal impairment
Adverse effects: Fever, headache, anorexia, impairment; rarely anaphylaxis, fever, sweating, until immunity develops. Precautions: Risk of severe hypotension
flushing, substernal pain (see Precautions), Administration: Meglumine antimoniate and following administration (establish baseline
weight loss, N & V, malaise, diarrhoea, muscle
vertigo, bleeding from nose or gum, jaun- sodium stibogluconate may be given by deep IM
and joint pain, dyspepsia, and epigastric pain; blood pressure and administer with patient
dice, biochemical (frequent) or clinical (rare) injection (if the volume of injection exceeds 10 mL,
renal function disturbances including hypokal- it should be divided in 2 doses: one in each buttock
lying down); monitor blood pressure during
aemia, hypomagnesaemia and renal toxicity; pancreatitis, rash; pain and thrombosis on IV administration and treatment period; hypo-
or thigh) and/or by slow IV injection (over at least 5
blood disorders; cardiovascular toxicity (in- administration; pain on IM injection. minutes). Both may be administered intralesionally. tension or hypertension; hypoglycaemia or
cluding arrhythmias); neurological disorders Dose: NOTE: Doses are expressed in terms of hyperglycaemia; hepatic impairment; leuko-
pentavalent antimony. POM Meglumine antimoniate (WMF 6.5.2)
(including peripheral neuropathy); abnormal penia, thrombocytopenia, anaemia; immu-
Visceral leishmaniasis, by IM injection, Injection, Meglumine antimoniate 30% (equiv. to
liver function (discontinue treatment); rash; approx. 8.1% antimony); in 5-mL ampoule. nodeficiency—if acute deterioration in bone
anaphylactoid reactions (see above); pain and ADULT and CHILD 20 mg/kg daily for marrow, renal or pancreatic function, interrupt
28 days. The minimum dose is 2 mL POM Meglumine antimonate (EDL 5.9) or discontinue treatment; renal impairment
thrombophlebitis at injection site.
(200 mg) for children weighing less Injection, Meglumine antimonate 30% equiv. to (Appendix 4); pregnancy—in potentially fatal
Dose: Visceral and mucocutaneous leishma- Antimony 8.5%; in 5-mL amp.
niasis (unresponsive to pentavalent than 10 kg.; if relapse, retreat immedi- visceral leishmaniasis, treat without delay
antimony compounds), by IV infusion, ately with same daily dosage. POM Sodium stibogluconate (EDL 5.9) (Appendix 2); breastfeeding (Appendix 3); carry
ADULT initial test dose of 1 mg over Cutaneous leishmaniasis, by intrale- Injection, Sodium stibogluconate equiv. to Anti- out laboratory monitoring according to manu-
EMDEX
sional injection, ADULT and CHILD mony 10%. facturer’s literature; interactions: Appendix 1.
20–30 minutes, then, 5–10 mg,
increased by 5–10 mg daily up to 1–3 mL into base of lesion; if no Adverse effects: Nephrotoxicity; acute hypo-
apparent response, may be repeated PAROMOMYCIN tension—with dizziness, headache, breathless-
maximum of 0.5–1 mg/kg, which
is then administered on alternate once or twice at intervals of 1–2 days; Indications: Visceral leishmaniasis. ness, tachycardia and syncope following rapid
days (total cumulative dose of 1–3 g relapse is unusual. Contra-indications: Hypersensitivity to IV injection; hypoglycaemia—may be followed
Contra-indications of local therapy: aminoglycosides, previous course of paro- by hyperglycaemia and type 1 diabetes melli-
usually required).
• Lesion in the face close to the eyes momycin treatment in preceding 3 months,
Reconstitution and Administration: According to tus; pancreatitis; also hypocalcaemia, GI distur-
• 3 lesions or more concurrent administration with nephrotoxic
manufacturer’s directions.
• Large lesion more than 3 cm of diameter
bances, confusion, hallucinations, arrhythmias;
or ototoxic drugs including aminoglycosides, thrombocytopenia, leukopenia, abnormal liver
POM Amphotericin B (WMF 6.5.2) • Sporotricoid forms
Powder for injection, Amphotericin B 50 mg; in vial. • Lesion on the joint renal impairment. function tests; anaemia; hyperkalaemia; rash,
See under section 9.2 for proprietary prepara- • Super-infected lesions Precautions: Pregnancy (Appendix 2); interac- Stevens-Johnson syndrome, reported; pain,
tions • Lesions produced by L. brazilensis, L. guyanensis tions: Appendix 1. local induration, sterile abscess and muscle
and L. tropica Adverse effects: Injection site reactions necrosis at injection site.
MEGLUMINE ANTIMONIATE When systemic treatment is required for including pain and swelling, raised aspartate Dose: Visceral leishmaniasis (unresponsive to
cutaneous leishmaniasis( except for lesions aminotransferase and alanine aminotrans- or intolerant of pentavalent antimony
Indications: Leishmaniasis (see notes above).
produced by L. brazilensis, L. guyanensis and ferase, pyrexia; ototoxicity (reversible at recom- compounds), by deep IM injection or
Contra-indications: Severe cardiac, liver and
L. tropica), pentavalent antimonials by IM mended dosage), vomiting, proteinuria, raised by IV infusion, ADULT and CHILD 4
kidney disorders; breastfeeding.
injection could be used with the following alkaline phosphatase and blood bilirubin; mg/kg 3 times a week for 5–25 weeks
Precautions: The risk of serious, even fatal, tox-
doses: ADULT and CHILD 10–20 mg/kg daily nephrotoxicity and neurotoxicity including or longer, until two consecutive
icitiy of pentavalent antimonials is increased
until a few days after clinical cure and negative numbness, skin tingling, muscle twitching, splenic aspirates taken 14 days apart
in patients who concomitantly present with:
slit-skin smear. The treatment of cutaneous convulsions reported with aminoglycosides; are negative.
cardiac disease, in particular arrhythmia; renal
leishmaniasis by L. braziliensis requires 20 mg/ neuromuscular blockage and respiratory Cutaneous leishmaniasis (L. aethiopica,
failure, liver disease, evere malnutrition/se-
kg daily, until lesion has healed and for at least paralysis reported following high doses of L. guyanensis), by deep IM injection or
verely impaired general condition; advanced
4 weeks; relapse may occur due to inadequate aminoglycosides. by IV infusion, ADULT and CHILD 3–4
HIV infection; pregnancy. If one of these
dosage or interrupted treatment; relapse after Dose: NOTE: All doses are in terms of paromo- mg/kg once or twice a week until the
conoditions are present, provide protein-rich
full course of treatment requires treatment mycin base. lesion is no longer visible; relapse is
diet throughout treatment and, if possible,
with pentamidine (see below). Visceral leishmaniasis, by IM injection, unusual.
correct iron and other nutritional deficiencies;
Mucocutaneous leishmaniasis (L. ADULT and CHILD over 5 kg, 11 mg/ Diffuse cutaneous leishmaniasis (L.
renal and hepatic impairment (Appendices 4
braziliensis), by IM injection, ADULT kg daily for 21 days. aethiopica), by deep IM injection or
and 5); monitor cardiac, renal and hepatic func-
tion; treat intercurrent infection (for example and CHILD 20 mg/kg daily until slit- POM Paromomycin (WMF 6.5.2) by IV infusion, ADULT and CHILD 3–4
pneumonia), and if possible an alternative drug skin smears are negative and for at Solution for IM injection, Paromomycin base (as mg/kg once a week, continued for
should be used. least 4 weeks; if inadequate response, sulfate) 750 mg per 2 mL. at least 4 months after parasites no
10–15 mg/kg every 12 hours for Note: Paromomycin base 11 mg is approx. equiv. to longer detectable in slit-skin smears;
MUCOCUTANEOUS DISEASE: Successful treat- paromomycin sulfate 15 mg. relapse frequent during first few
same period; if relapse, retreat for at
ment of mucocutaneous leishmaniasis may in- months until immunity established.
least twice as long; if unresponsive to
duce severe inflammation around lesions (may Mucocutaneous leishmanisais (L.
treatment, treat with pentamidine or
be lifethreatening if pharyngeal or tracheal
462 | 9.3.4 Antitrypanosomal drugs 9.3.4.1 African trypanosomiasis | 463
braziliensis, L. aethiopica), by deep IM b. gambiense patients with meningoencepha- bottle. Contra-indications: Severe renal impairment;
injection or by IV infusion, ADULT and litic involvement when eflornithine treatment T. b. rhodesiense infection (since primary resist-
CHILD 4 mg/kg 3 times a week for has failed or is unavailable. Several treatment MELARSOPROL ance observed).
5–25 weeks or longer, until lesion no regimens for adults and children are currently Indications: Treatment of meningoencepha- Precautions: CSF examination before treat-
longer visible. used in the absence of clear evidence that one litic stage of T. b. rhodesiense or T. b. gambiense ment (pentamidine not likely to be effective if
Reconstitution and Administration: According is better than another. Most treatment regi- infections. leukocyte count greater then 5 cells/mm3, total
to manufacturer’s directions. Deep IM injection is mens have low starting doses, which might be Contraindications: Pregnancy; avoid use protein greater then 37 mg/100 mL, or trypano-
the preferred route of administration. Pentamidine preferred for children and debilitated patients; during influenza epidemics (increased somes detected in centrifuge deposits); risk of
isetionate is toxic; care required to protect personnel
these regimens increase to a maximum of 3.6 risk of reactive encephalopathy in febrile severe hypotension following administration
during handling and administration.
mg/kg daily and are given in short courses of patients). (establish baseline blood pressure and admin-
POM Pentamidine (WMF 6.5.2) 3–4 days with an interval of 7–10 days. The Precautions: Hospitalization and close medical ister with patient lying down); monitor blood
Powder for injection, Pentamidine (as isetionate) 200 effectiveness of 2.2 mg/kg daily for 10 days supervision required throughout treatment; pressure during administration and treatment
mg, 300 mg; in vials. has been demonstrated for T. b. gambiense period; hypotension or hypertension; hepatic
episodes of reactive encephalopathy require
POM Pentamidine (EDL 5.9) and might be preferred for its conciseness, treatment suspension; treat intercurrent infec- impairment; hypoglycaemia or hyperglycae-
Injection, Pentamidine (as isetionate) 300 mg; particularly in epidemic situations with limited tions such as pneumonia and malaria before mia; leukopenia; thrombocytopenia; anaemia;
powder in vial. resources. melarsoprol administration; malnutrition (if immunodeficiency—if acute deterioration in
An increasing number of melarsoprol treat- possible, correct with protein-rich diet); G6PD bone marrow, renal or pancreatic function,
SODIUM STILBOGLUCONATE deficiency; leprosy—may precipitate erythema interrupt or discontinue treatment; renal im-
ment failures due to drug resistance have been
See under Meglumine antimoniate above reported in the last years in several countries. nodosum. pairment (Appendix 4); pregnancy—should
Adverse effects: Fatal reactive encephalopa- not be withheld, even if evidence of menin-
Following treatment of African trypanosomia- thy characterized by headache, tremor, slurred goencephalitic involvement, as melarsoprol
EMDEX
9.3.4 Antitrypanosomal drugs sis, patients should be followed up at six month speech, convulsions and ultimately coma contraindicated (Appendix 2); breastfeeding
intervals over 24 months for leukocytes, total (in 3–8% of patients, usually at end of first (Appendix 3); interactions: Appendix 1.
9.3.4.1 African trypanosomiasis
9.3.4.2 American trypanosomiasis protein content and trypanosome presence in 3–4 days of treatment); myocardial damage; Adverse effects: Nephrotoxicity; acute hypo-
CSF, to evaluate treatment efficacy. albuminuria; hypertension; hypersensitivity tension, hypoglycaemia—may be followed by
9.3.4.1 African trypanosomiasis reactions; agranulocytosis; doserelated renal hyperglycaemia and type I diabetes mellitus;
EFLORNITHINE
African trypanosomiasis, or sleeping sick- and hepatic impairment; hyperthermia, urti- pancreatitis; also hypocalcaemia, GI distur-
Indications: Treatment of meningoencepha- caria, headache, diarrhoea and vomiting—in bances, confusion, hallucinations, arrhythmias;
ness, is a protozoan infection transmitted by litic stages of T. b. gambiense infection.
Glossina spp. (tsetse flies). Two subspecies of late stage of treatment. thrombocytopenia, leukopenia, abnormal liver
Contra-indications: Pregnancy; breast-feed- Dose: Treatment of T. b. rhodesiense and T. b. function tests; anaemia; hyperkalaemia; rash,
Trypanosoma brucei—T. brucei gambiense and ing.
T. brucei rhodesiense—produce distinctive gambiense with meningoencephalitic Stevens-Johnson syndrome reported; pain,
Precautions: Hospitalization and close su- involvement (see notes above), by slow local induration, sterile abscess and muscle
clinical forms of the disease. The early stage of pervision throughout treatment; monitor
African trypanosomiasis results from infection IV injection, ADULT and CHILD dose necrosis at injection site.
complete blood and platelet counts for bone gradually increased from 1.2 mg/kg Dose: Treatment of haemolymphatic stage
of the blood stream and lymph nodes. The marrow suppression—severe anaemia, leu-
late meningoencephalitic stage results from to maximum of 3.6 mg/kg daily in of T. b. gambiense infection, by IM
kopenia or thrombocytopenia requires an in- courses of 3–4 days with intervals of injection, ADULT and CHILD 4 mg/kg
infection of the central nervous system. Signs terruption in treatment until there is evidence
of the later stage develop within a few weeks in 7–10 days between courses; alterna- daily or on alternate days for a total of
of bone marrow recovery; renal impairment tively for T. b. gambiense infection, 2.2 7–10 doses.
T. b. rhodesiense infection but only after several (Appendix 4).
months or years in T. b. gambiense infection. mg/kg daily for 10 days. Treatment of meningoencephalitic
Adverse effects: Diarrhoea, anaemia, leuko- ADMINISTRATION: Injection very irritant— stage of T. b. gambiense (prior to
Treatment of early-stage infections of T. b. penia, thrombocytopenia and convulsions; avoid extravasation. Patients should remain melarsoprol), by IM injection, ADULT
rhodesiense with suramin sodium and T. b. impaired hearing reported; vomiting, anorexia, supine and fasting for at least 5 hours after and CHILD 4 mg/kg daily on days one
gambiense with pentamidine isetionate can alopecia, abdominal pain, headache, facial injection. and two.
be curative if started before the central nervous oedema, eosinophilia and dizziness—less com- Reconstitution and Administration: According to
system has become involved. In areas where mon and reversible on treatment withdrawal. POM Melarsoprol (WMF 6.5.5.1) manufacturer’s directions. Pentamidine isetionate is
pentamidine resistance occurs, suramin so- Injection, Melarsoprol 3.6% solution; in 5-mL am-
Dose: Treatment of meningoencephalitic T. b. toxic; care is required to protect personnel during
poule (180 mg of active compound). handling and administration.
dium may be used for T. b. gambiense infection. gambiense infections, by IV infusion,
ADULT 100 mg/kg over 45 minutes, POM Melarsoprol (EDL 5.9)
Eflornithine is used for the treatment of T. POM Pentamidine (WMF 6.5.5.1)
every 6 hours for 14 days. Injection, Melarsoprol 3.6%; solution for injection Powder for injection, Pentamidine isetionate 200
b. gambiense with meningoencephalitic inin 5-mL amp.
volvement. Eflornithine is considerably less CHILDREN: A higher dose may be required in mg; in vial.
neurotoxic than melarsoprol, but requires a children. For children less than 12 years old or PENTAMIDINE POM Pentamidine (EDL 5.9)
more intensive administration schedule. If re- under 35 kg, 150 mg/kg over 45 minutes every Injection, Pentamidine (as isetionate) 300 mg;
Indications: Treatment of haemolymphatic
lapse occurs after treatment with eflornithine, 6 hours for 14 days has been used and has pro- powder in vial.
stage of T. b. gambiense infection; adjunct to
a course of melarsoprol treatment should be vided an adequate response. This dose is based
melarsoprol in meningoencephalitic stage of SURAMIN SODIUM
considered. on clinical experience and limited evidence.
T. b. gambiense infection; leishmaniasis (section
Melarsoprol is used in T. b. rhodesiense patients POM Eflornithine (WMF 6.5.5.1)
Indications: Treatment of haemolymphatic
9.3.3); Pneumocystis carinii (Pneumocystis
with meningoencephalitic involvement or in T. Injection, Eflornithine HCl 200 mg/mL; in 100-mL stage of T. b. rhodesiense infections; onchocer-
jiroveci) pneumonia (section 9.3.5).
ciasis (section 9.4.2.3).
464 | 9.3.4.2 American trypanosomiasis 9.3.5 Antipneumocystosis and antitoxoplasmosis drugs | 465
Contra-indications: Previous anaphylaxis or enlargement and less, frequently, oesopha- rashes and other allergic reactions. pyrimethamine with sulfadiazine; a folate
suramin sensitivity; severe liver or renal func- geal and colonic dilatation. At this stage, only Dose: Acute American trypanosomiasis (Cha- supplement is also given to counteract the
tion impairment; elderly or debilitated. symptomatic treatment is of benefit. gas disease), by mouth, ADULT 8–10 megaloblastic anaemia associated with these
Precautions: Administer only under close At present the only therapeutic agents of value mg/kg daily in 3 divided doses for 90 drugs.
medical supervision in hospital and with are benznidazole and nifurtimox. Both sup- days; CHILD 15–20 mg/kg daily in 4
general condition improved as far as possible press parasitaemia and are efficacious during divided doses for 90 days. PENTAMIDINE
before treatment; first dose—possible loss the early stages of infection. POM Nifurtimox (WMF 6.5.5.2) Indications: Pneumocystis carinii (Pneumocys-
of consciousness (see under Dosage, below); Tablets, Nifurtimox 30 mg, 120 mg, 250 mg tis jiroveci) pneumonia; leishmaniasis (section
maintain satisfactory food and fluid intake Safe use of both drugs in pregnancy has not
9.3.3); African trypanosomiasis (section 9.3.4.1).
during treatment; urine tests before and been established and treatment should be
9.3.5 Antipneumocystosis and Contra-indications: Severe renal impairment
weekly during treatment—reduce dose if deferred until after the first trimester. They
antitoxoplasmosis drugs Precautions: Risk of severe hypotension
moderate albuminuria, discontinue immedi- should be instituted immediately to avoid the
following administration (establish baseline
ately if severe albuminuria or casts in urine; risk of congenital transmission. PNEUMOCYSTOSIS
blood pressure and administer with patient
pregnancy—should not be withheld, even if Studies are in progress to determine whether Pneumocystis carinii (Pneumocystis jiroveci) lying down); monitor blood pressure during
evidence of meningoencephalitic involvement, benznidazole and nifurtimox have any influence is classified as a protozoan although there administration and treatment period; hypo-
as melarsoprol contraindicated. on the later manifestations of the disease. is evidence to suggest that it is probably a tension or hypertension; hypoglycaemia or
Adverse effects: Rarely, immediate and po- Symptomatic treatment may be necessary in fungus. Pneumocystis carinii (Pneumocystis hyperglycaemia; hepatic impairment; renal
tentially fatal reaction with nausea, vomiting, advanced cases. jiroveci) pneumonia is probably acquired by the impairment (Appendix 4); leukopenia, throm-
shock and loss of consciousness during first airborne route. In otherwise healthy persons it bocytopenia, anaemia; immuno-deficiency—if
dose—see First (Test) Dose, above; albu- BENZNIDAZOLE rarely produces signs of infection. However, it acute deterioration in bone marrow, renal or
minuria; abdominal pain; severe diarrhoea; Indications: Acute American trypanosomiasis is a frequent cause of opportunistic infection pancreatic function, interrupt or discontinue
EMDEX
stomal ulceration; exfoliative dermatitis; fever; (Chagas disease). in immunosuppressed, debilitated or mal- treatment; pregnancy—in potentially fatal P.
tiredness; anorexia; malaise; polyuria; thirst; Contra-indications: Early pregnancy. nourished patients; it is the commonest cause carinii (P. jiroveci) pneumonia, treat without
raised liver enzyme values; paraesthesia and Precautions: Hepatic, renal or haemato- of pneumonia in AIDS and the most frequent delay (Appendix 2); breastfeeding (Appendix
hyperaesthesia of palms and soles. logical insufficiency—require close medical immediate cause of death in these patients. 3); carry out laboratory monitoring according
Dose: Treatment of haemolymphatic T. b. supervision; monitor blood count, especially Sulfamethoxazole with trimethoprim is the to manufacturer’s literature; interactions:
rhodesiense and T. b. gambiense leukocytes, throughout treatment. treatment of choice for Pneumocystis carinii Appendix 1.
infections, by slow IV injection, ADULT Adverse effects: Rashes—if severe and ac- (Pneumocystis jiroveci) pneumonia and is Adverse effects: Nephrotoxicity; acute hypo-
and CHILD 5 mg/kg on day 1, 10 mg/ companied by fever and purpura, discontinue also used for prophylaxis in highrisk patients; tension—with dizziness, headache, breathless-
kg on day 3 and 20 mg/kg on days 5, treatment; nausea, vomiting and abdominal pentamidine isetionate is used in patients un- ness, tachycardia and syncope following rapid
11, 17, 23 and 30. pain; dose-related paraesthesia and peripheral responsive to or intolerant of sulfamethoxazole intravenous injection; hypoglycaemia—may
Reconstitution of injection: Reconstitute in wa- neuritis—discontinue treatment; leukopenia with trimethoprim. be followed by hyperglycaemia and type I di-
ter for injections to produce a final concentration and rarely, agranulocytosis. abetes mellitus; pancreatitis; also hypocalcae-
of 10%. The treatment of Pneumocystis carinii (Pneu-
Dose: Acute American trypanosomiasis mia, GI disturbances, confusion, hallucinations,
FIRST (TEST) DOSE: Administer first dose with mocystis jiroveci) infections must only be
(Chagas disease), by mouth, ADULT arrhythmias; thrombocytopenia, leukopenia,
particular caution; wait at least 1 minute after undertaken with specialist supervision where
5–7 mg/kg daily in two divided doses abnormal liver function tests; anaemia; hy-
injecting the first few microlitres; inject next 0.5 there are appropriate monitoring facilities.
for 60 days; CHILD up to 12 years 10 perkalaemia; rash, Stevens-Johnson syndrome
mL over 30 seconds and wait one minute; inject mg/kg daily in two divided doses for TOXOPLASMOSIS reported; pain, local induration, sterile abscess
the remainder over several minutes. 60 days. Toxoplasmosis is caused by infection with the and muscle necrosis at injection site.
POM Suramin (WMF 6.5.5.1)
POM Benznidazole (WMF 6.5.5.2) protozoan parasite Toxoplasma gondii. Most Dose: Treatment of P. carinii (P. jiroveci)
Powder for injection, Suramin sodium 1 g; in vial. infections are self-limiting and do not require pneumonia (see notes above), by slow
Tablet, Benznidazole 100 mg.
POM Suramin (EDL 5.9) treatment. However, in immunodeficiency, IV infusion or by deep IM injection,
Injection, Suramin 1 g; powder in vial. NIFURTIMOX primary infection may result in encephalitis, ADULT and CHILD 4 mg/kg daily for at
Indications: Acute American trypanosomiasis myocarditis or pneumonitis; impairment of im- least 14 days.
9.3.4.2 American trypanosomiasis (Chagas disease). munity (such as occurs in AIDS) in a previously Prophylaxis of P.carinii (P. jiroveci) pneu-
Contra-indications: Early pregnancy. infected person, may result in encephalitis or monia (see notes above), by slow IV
American trypanosomiasis (Chagas disease)
Precautions: History of convulsions or psy- meningoencephalitis. Congenital transmission infusion, ADULT and CHILD 4 mg/kg
is caused by the protozoan parasite Trypa-
chiatric disease—requires close medical su- may occur if there is a primary infection in early once every 4 weeks or by inhalation
nosoma cruzi which are carried by reduviid
pervision; avoid alcohol—to reduce incidence pregnancy or if the mother is immunodeficient. of nebulized solution, ADULT 300 mg
or triatomine bugs which feed on human
and severity of adverse effects; co-administer Such cases often result in spontaneous abor- as a single dose once every 4 weeks;
blood. The acute febrile phase of the disease
aluminium hydroxide to reduce gastrointesti- tion, fetal death or severe congenital disease. CHILD 4 mg/kg as a single dose once
frequently passes unrecognized. Occasionally,
nal irritation. Spiramycin [not included on WHO Model List] every 4 weeks.
however, infection follows a fulminating course
can reduce transmission of maternal infection Reconstitution and Administration: According to
terminating in a fatal myocarditis and menin- Adverse effects: Anorexia, loss of weight,
to the fetus. Ocular toxoplasmosis causes chori- manufacturer’s directions. Pentamidine isetionate is
goencephalitis. In about half of the surviving nausea, vomiting, gastric pain, insomnia, head- toxic; care is required to protect personnel during
cases, and after a latent interval ranging from ache, vertigo, excitability, myalgia, arthralgia, oretinitis and is often the result of a childhood
handling and administration.
10 to more than 20 years, chronic myopathy convulsions—dose-related, reduce dose; pe- infection that becomes apparent in adulthood.
POM Pentamidine (WMF 6.5.4)
degeneration results in arrhythmias, cardiac ripheral neuritis—may require discontinuation; The treatment of choice for toxoplasmosis is
Powder for injection, Pentamidine (as isetionate) 200
466 | 9.3.5 Antipneumocystosis and antitoxoplasmosis drugs 9.4 Anthelmintics | 467
mg, 300 mg; in vials. continue immediately; predisposition to folate intake (to avoid crystalluria; avoid in blood 9.4 Anthelmintics
deficiency; elderly; asthma; G6PD deficiency; disorders (unless under specialist supervision);
9.4.1 Intestinal anthelmintics
PYRIMETHAMINE pregnancy—avoid in first trimester, but may be monitor blood counts and discontinue imme- 9.4.2 Antifilarials
Indications: Toxoplasmosis (with sulfadiazine); given thereafter if danger of congenital trans- diately if blood disorder develops; rash—dis- 9.4.3 Trematode infections
malaria (with sulfadoxine) (section 6.4.3). mission (Appendix 2); breastfeeding (Appendix continue immediately; predisposition to folate
Contra-indications: Hepatic and renal im- 3); interactions: Appendix 1. deficiency; elderly; asthma; G6PD deficiency; 9.4.1 Intestinal anthelmintics
pairment. Adverse effects: Nausea, vomiting, diarrhoea, pregnancy (Appendix 2); breastfeeding (Ap-
headache; hypersensitivity reactions including pendix 3); interactions: Appendix 1. 9.4.1.1 Cestode infections
Precautions: Pregnancy (avoid in first tri-
9.4.1.2 Intestinal nematode infections
mester but give in later pregnancy if danger rashes, pruritus, photosensitivity reactions, Adverse effects: Nausea, vomiting, diarrhoea,
9.4.1.3 Tissue nematode infections
of congenital transmission; Appendix 2); exfoliative dermatitis, and erythema nodosum; headache; hypersensitivity reactions including
breastfeeding (Appendix 3); blood counts rarely, erythema multiforme (Stevens-Johnson rashes, pruritus, photosensitivity reactions,
9.4.1.1 Cestode infections
required with prolonged treatment; folate syndrome) and toxic epidermal necrolysis; sys- exfoliative dermatitis and erythema nodosum;
supplements throughout treatment; interac- temic lupus erythematosus, myocarditis, serum rarely, erythema multiforme (Stevens-Johnson Cestode infections (tapeworms) include intesti-
tions: Appendix 1. sickness; crystalluria—resulting in haematuria, syndrome) and toxic epidermal necrolysis; sys- nal taeniasis and cysticercosis, hymenolepiasis
Adverse effects: Depression of haematopoie- oliguria, anuria; blood disorders including temic lupus erythematosus, myocarditis, serum (dwarf tapeworm), diphyllobothriasis and
sis with high doses; megaloblastic anaemia; granulocytopenia, agranulocytosis, aplastic sickness; crystalluria—resulting in haematuria, echinococcosis (hydatid disease). Cysticercosis
rashes; insomnia; GI disturbances. anaemia, purpura—discontinue immediately; oliguria, anuria; blood disorders including is a systemic infection caused by the larval form
Dose: Toxoplasmosis (in second and third also reported, liver damage, pancreatitis, anti- granulocytopenia, agranulocytosis, aplastic (cysticercus) of Taenia solium.
trimesters of pregnancy), by mouth, biotic-associated colitis, eosinophilia, cough anaemia, purpura—discontinue immediately; Neurocysticercosis occurs when the infection
ADULT 25 mg daily for 3–4 weeks. and shortness of breath, pulmonary infiltrates, also reported, liver damage, pancreatitis, anti- involves the brain. In man, echinococcosis is
Toxoplasmosis in neonates, by mouth, aseptic meningitis, depression, convulsions, biotic-associated colitis, eosinophilia, cough due to the larval stage of Echinococcus granulo-
EMDEX
NEONATE 1 mg/kg daily; duration ataxia, tinnitus, vertigo, dizziness, hallucina- and shortness of breath, pulmonary infiltrates, sus or E. multilocularis. The larvae (oncospheres)
of treatment depends on whether tions, and electrolyte disturbances. aseptic meningitis, depression, convulsions, develop by expansion (cystic echinococcosis)
neonate has overt disease—continue Dose: Toxoplasmosis (in second and third ataxia, tinnitus, vertigo, dizziness, hallucina- or tumour-like infiltration (alveolar echino-
for 6 months, or is without overt trimesters of pregnancy), by mouth, tions, and electrolyte disturbances; megalo- coccosis), respectively, in the liver, lungs, or
disease but, born to mother infected ADULT 3 g daily in 4 divided doses. blastic anaemia due to trimethoprim. other organs.
during pregnancy—treat for 4 weeks, Toxoplasmosis in neonates, by mouth, Dose: Treatment of P. carinii (P. jiroveci) pneu-
DIPHYLLOBOTHRIASIS
followed by further courses if infec- neonate 85 mg/kg daily in 2 divided monia (see notes above), by mouth
tion confirmed. doses; duration of treatment depends or by IV infusion, ADULT and CHILD In diphyllobothriasis, niclosamide or prazi-
Toxoplasmosis in immunodeficiency, on whether the neonate has overt sulfamethoxazole up to 100 mg/ quantel in a single dose is highly effective.
by mouth, ADULT 200 mg in divided disease—continue for 6 months, or kg daily with trimethoprim up to 20 Hydroxocobalamin and folic acid supplements
doses on first day, then 75–100 mg is without overt disease but born to mg/kg daily in 2–4 divided doses for may also be required.
daily for at least 6 weeks, followed by mother infected during pregnancy— 14–21 days. ECHINOCOCCOSIS
a suppressive dose of 25–50 mg daily. treat for 4 weeks, followed by further Prophylaxis of P. carinii(P. jiroveci) pneu-
In echinococcosis, surgery (or, if this is not
Chorioretinitis, by mouth, ADULT 75 courses, if infection confirmed. monia (see notes above), by mouth,
possible, a technique such as ‘puncture-aspi-
mg daily for 3 days then 25 mg daily Toxoplasmosis in immunodeficiency, ADULT and CHILD sulfamethoxazole
ration-injection-reaspiration’) is the treatment
for 4 weeks; in unresponsive patients, by mouth, ADULT 4–6 g daily in 4 25 mg/kg with trimethoprim 5 mg/kg
of choice for operable cystic disease due to
50 mg daily for a further 4 weeks. divided doses for at least 6 weeks, in 2 divided doses on alternate days
Echinococcus granulosus but chemotherapy
Note: For the treatment of toxoplasmosis, pyrimeth- followed by a suppressive dose of 2–4 (3 times a week).
with benzimidazoles, such as mebendazole
amine must always be taken with sulfadiazine (see g daily.
below). POM Sulfamethoxazole plus Trimethoprim and albendazole, may be of value as adjunc-
Chorioretinitis, by mouth, ADULT 2 g (WMF 6.5.4) tive therapy. Alveolar echinococcosis due to E.
POM Pyrimethamine (WMF 6.5.4) daily in 4 divided doses. Tablets, Sulfamethoxazole 400 mg with trimeth- multilocularis requires both surgery and long-
Tablet, Pyrimethamine 25 mg. Note: For the treatment of toxoplasmosis, sulfadi- oprim 80 mg; Sulfamethoxazole 800 mg with
azine must always be taken with pyrimethamine term treatment with either mebendazole or
trimethoprim 160 mg.
(see above). albendazole to inhibit spread of the infection.
SULFADIAZINE Oral suspension, Sulfamethoxazole 200 mg with
POM Sulfadiazine (WMF 6.5.4) trimethoprim 40 mg/5 mL. In animal studies, albendazole and meben-
Deleted from the current WHO Model Formulary Injection, Sulfamethoxazole 80 mg with trimethop- dazole have been found to be teratogenic.
Tablets, Sulfadiazine 500 mg.
Indications: Toxoplasmosis (with pyrimeth- rim 16 mg/mL; in 5-mL and 10-mL ampoules. They are contraindicated for the treatment of
amine); rheumatic fever (section 9.1.2.9). SULFAMETHOXAZOLE plus POM Sulfamethoxazole plus Trimethoprim cestode infections in pregnancy; pregnancy
Contra-indications: Hypersensitivity to sulfo- TRIMETHOPRIM (EDL 5.3) should be excluded before treatment with
namides; porphyria. Indications: Pneumocystis carinii (Pneumo- Tablet, Sulfamethoxazole 400 mg, Trimethoprim albendazole (non-hormonal contraception
Precautions: Hepatic impairment (avoid if cystis jiroveci) pneumonia; bacterial infections 80 mg during and for 1 month after treatment). For
severe; Appendix 5); renal impairment (avoid (section 9.1.2.9). Oral suspension, Sulfamethoxazole 200 mg, Trimeth- single-dose or short-term use in pregnancy,
Contra-indications: Hypersensitivity to sulfo- oprim 40 mg per 5 mL. see section 9.4.1.2.
if severe; Appendix 4); maintain adequate fluid
intake (to avoid crystalluria); avoid in blood namides or trimethoprim; porphyria. See section 9.1.2.9 for the proprietary prepara- HYMENOLEPIASIS
disorders (unless under specialist supervision); Precautions: Renal impairment (avoid if se- tions of Co-trimoxazole.
vere; Appendix 4); hepatic impairment (avoid In hymenolepiasis, praziquantel is more ef-
monitor blood counts and discontinue imme-
if severe; Appendix 5); maintain adequate fluid fective than niclosamide, although resistance
diately if blood disorder develops; rashes—dis-
468 | 9.4.1.1 Cestode infections 9.4.1.1 Cestode infections | 469
to praziquantel has been reported. Repeated Alveolar echinococcosis, by mouth, OTC JAWADAZOLE® (Jawa) OTC XTAL® (Vixa)
treatment may be necessary to cure intense ADULT as for cystic echinococcosis, Suspension, Albendazole 100 mg per 5 mL Tablet, Albendazole 200 mg.
infections or to eliminate the parasite within but treatment cycles may need to be Pack: 20 mL 200 mg – 2’s.
a family group or institution. continued for months or years. Neu- OTC LEXZEN® (Med Impex) OTC ZEBEN® (Medreich)
TAENIASIS rocysticercosis, by mouth, ADULT over Chewable tablet, Albendazole 200 mg. Tablets, Albendazole 200 mg, 400 mg; vanilla fla-
60 kg, 800 mg daily in 2 divided doses 200 mg – 2’s (in blister). voured orange chewable tabs.
In taeniasis, praziquantel is well tolerated and for 8–30 days; ADULT less than 60 kg, Suspension, Albendazole 100 mg per 5 mL. Suspension, Albendazole 2% w/v; orange flavoured
extensively absorbed and kills adult intestinal 15 mg/kg daily in two divided doses Pack: 10 mL in bottle. susp.
taenia worms in a single dose. Praziquantel (to a maximum daily dose of 800 mg) Pack: 20 mL bottle.
OTC NEMOZOLE® (IPCA)
also kills T. solium cysticerci when taken for 14 for 8–30 days. Tablets, Albendazole 200 mg, 400 mg; f-c tabs. OTC ZENTEL® (GSK)
days in high doses and it can therefore be used Note: No fasting or purging is required. To be 200 mg – 2’s. Tablet, Albendazole 200 mg; off-white, circular ‘Tiltab’
to treat neurocysticercosis. However, because chewed, swallowed or crushed and mixed with food. 400 mg – 1’s. tab. with pentagonal projection on both sides.
dying and disintegrating cysts may induce Suspension, Albendazole 100 mg per 5 mL. 200 mg – 2.
See also under the proprietary preparations below.
localized cerebral oedema, treatment with Pack: 20 mL. Suspension, Albendazole 100 mg per 5 mL; pleasant
praziquantel must always be undertaken in a tasting, fruit flavoured susp.
OTC Albendazole (WMF 6.1.1.) OTC PACDAZOLE® (Pacmai)
hospital setting. In addition, a corticosteroid Pack: 20 mL.
Chewable tablet, Albendazole 400 mg. Tablet, Albendazole 400 mg
Dose: Adult and Child (>2 years), 2 tabs or 20 mL
is usually given to reduce the inflammatory 400 mg – 1’s (in blister)
OTC Albendazole (EDL 5.2) susp. (400 mg) as single dose.
response. Albendazole also kills neuro- Strongyloidiasis or Taeniasis, 2 tabs or 20
Tablet, Albendazole 200 mg. OTC PANZOLE® (Jopan)
cysticerci when given daily for one month; Oral liquid, Albendazole 100 mg per 5 mL. Tablet, Albendazole 400 mg mL susp. (400 mg) as single dose for 3 con-
a corticosteroid or an antihistamine is also 400 mg – secutive days; second course may be given
given to reduce any inflammatory reaction. OTC Albendazole (Gauze) after 3 weeks if necessary.
Tablet, Albendazole 500 mg OTC RALBEN® (Seagreen)
EMDEX
Surgery may be the preferred treatment for Child (<2 years), 10 mL susp. or ½ tab. (200
400 mg – 20 x 1 Tablet, Albendazole 200 mg; f-c tab. mg) as single dose for common hehminth
neurocysticerosis in some cases. The longer-es-
200 mg – 2’s (in blisters) infections. Hymenolepis nana infection,
tablished niclosamide acts only against the OTC ALBEN-G® (Geneith)
Chewable tablet, Albendazole 400 mg; uncoated tab 2 tabs or 20 mL susp. (400 mg) for 3 con-
adult intestinal worms. Cestode infections, Tablet, Albendazole 200 mg; off-white f-c tab.
400 mg – 1’s (in blisters) secutive days.
due to T. solium, occurring during pregnancy 200 mg – 2’s (in blisters).
Tablet, Albendazole 400 mg OTC SHANU-ZOLE® (Jawa)
should always be treated immediately (with OTC ZOLAT® (Emzor)
400 mg – 1’s (in blisters) Suspension, Albendazole 25 mg Caplet, Albendazole 200 mg.
praziquantel or niclosamide, but not with al- Pack: 1 L
bendazole) because of the risk of cysticercosis. OTC ALBONZ® (Shrezar) 200 mg – 2.
Tablet, Albendazole 400 mg OTC TANZOL® (Shalina) Suspension, Albendazole 100 mg per 5 mL; pleasant
ALBENDAZOLE 400 mg – 1 x 1 x 20’s Tablet, (Chewable), Albendazole 400 mg; yellow tasting, fruit flavoured susp.
orange-flavoured tab. Pack: 20 mL.
Indications: Echinococcus multilocularis and E. OTC AVIS® (Al-Tinez)
400 mg – 1’s.
granulosus infections prior to or not amenable Tablet, Albendazole 400 mg; orange f-c tab.
Suspension, Albendazole 400 mg per 10 mL. MEBENDAZOLE
to surgery; neurocysticercosis; nematode in- 400 mg – 1’s.
Pack: 10 mL. Indications: Echinococcus granulosus and E.
fections (sections 9.4.1.2 and 9.4.1.3); filariasis OTC BAIZEN® (Embassy)
OTC UNABEN® (Neimeth) multilocularis infections before surgery or not
(section 9.4.2.2). Tablet, Albendazole 200 mg.
Tablet, Albendazole 400 mg. amenable to surgery; nematode infections
Contra-indications: Pregnancy (Appendix 2; 200 mg – 2’s.
400 mg – 1’s; 500’s. (sections 9.4.1.2 and 9.4.1.3).
see notes above and Precautions). OTC CIKAZOLE® (Michelle Lab) (429) Suspension, Albendazole 100 mg per 5 mL. Contra-indications: Pregnancy (Appendix 2;
Precautions: Liver function tests and blood Tablet, Albendazole 400 mg Pack: 10 mL in bottle. see also notes above).
counts before treatment and twice during each 400 mg – 1’s (in blister)
OTC WORMEXP® (Juhel) Precautions: Blood counts and liver function
cycle; exclude pregnancy before starting treat-
OTC CYSTAZOLE® (Afrab-Chem) Caplet, Albendazole 200 mg. tests (with high-dose regimens); breastfeeding
ment (non-hormonal contraception during 200 mg – 2’s (in blister).
Tablet, Albendazole 200 mg. (Appendix 3); interactions: Appendix 1.
and for 1 month after treatment); breastfeed- Pack: 2’s (in blisters). Suspension, Albendazole 100 mg per 5 mL. Adverse effects: GI disturbances, headache,
ing; interactions: Appendix 1. Suspension, Albendazole 200 mg per 5 mL. Pack: 20 mL. dizziness; with high doses, allergic reactions,
Adverse effects: GI disturbances, headache, Pack: 10 ml (in bottle).
OTC WORMIDAN® (Dana) raised liver enzymes, alopecia, bone marrow
dizziness; increases in liver enzymes; reversible Chewable tablet, Albendazole 400 mg
OTC FLUSH OFF (Mecure) depression.
alopecia; rash; fever; leukopenia and rarely, Tablet, Albendazole 400 mg. 400 mg – 1’s (in blisters) Advice to patients: Tablets may be chewed,
pancytopenia; allergic shock if cyst leakage; 400 mg – 1 x 1’s. Suspension, Albendazole 100 mg per 5 mL swallowed whole, or crushed and mixed with
convulsions and meningism in cerebral Pack: 20 mL.
OTC GLOWORM® (Hochiez) food to minimise GI upset; hygienic precau-
disease.
Chewable tablet, Albendazole 400 mg OTC WORMOFF® (Gauze) tions should be taken to prevent reinfection
Dose: Cystic echinococcosis, by mouth, ADULT Oral Liquid, Albendazole 200 mg per 10 mL
400 mg – 1’s such as wearing shoes and washing hands;
over 60 kg, 800 mg daily in 2 divided Suspension, Albendazole 400 mg per 10 mL Pack: 10 mL wash all fruits and vegetables before eating; a
doses for 28 days followed by 14 tab- Pack: 10 mL
OTC WORMTAC® (Maydon) second course of therapy may be needed after
let-free days; ADULT less than 60 kg,
OTC IHIE® (Carrot-Top) Tablet, Albendazole 400 mg. 3 weeks if necessary; deworm all family mem-
15 mg/kg daily in two divided doses
Chewable tablets, Albendazole 200 mg, 400 mg 400 mg – 1’s bers; dietary restrictions, enamas or laxatives
(to a maximum daily dose of 800 mg) 200 mg – 1 x 2’s (in blisters) Oral suspension, Albendazole 200 mg per 5 mL. are not necessary.
for 28 days followed by 14 tablet-free 400 mg – 1 x 2’s (in blisters) 200 mg – 10 mL Nursing action: No dietary restrictions, laxa-
days; up to 3 courses may be given.
470 | 9.4.1.1 Cestode infections 9.4.1.2 Intestinal nematode infections | 471
tives, or enemas are necessary. Treat all family NICLOSAMIDE during and for 72 hours after treatment); inter- anthelminthics, albendazole or mebendazole
members. Indications: Taenia saginata, T. solium, Hy- actions: Appendix 1. are also effective.
• Teach patient about the need for good personal menolepis nana, and Diphyllobothrium latum Adverse effects: Abdominal discomfort, nau- CAPILLARIASIS
hygiene, especially good handwashing technique. sea, vomiting, diarrhoea, malaise; headache,
infections.
To avoid reinfection, teach him to wash perianal dizziness, drowsiness; rarely hypersensitivity Capillariasis is caused by infection of the intes-
Precautions: Chronic constipation (restore
area daily. Change undergarments and bedclothes
reactions including fever, urticaria, pruritus, tine with Capillaria philippinensis. Prolonged
daily. Wash hands and clean fingernails before regular bowel movement before treatment);
eosinophilia (may be due to dead and dying treatment with mebendazole or albendazole
meals and after bowl movements. give antiemetic before treatment; not effective
parasites); in neuro-cysticercosis, headache, offers the only prospect of cure.
• Advise patient to avoid preparing food during against larval worms; pregnancy (Appendix 2).
infestation. Adverse effects: Nausea, retching, abdominal hyperthermia, seizures, intracranial hyperten- ENTEROBIASIS
Dose: Cystic echinococcosis, alveolar echino- pain; lightheadedness; pruritus. sion (inflammatory response to dead and dying Enterobiasis is an infection of the large intes-
coccosis, by mouth, ADULT 4.5 g daily Nursing action: Administer a laxative 2-3 parasites in CNS). tine caused by Enterobius vermicularis (pin-
in 3 divided doses for 6 months; in hours after the niclosamide dose if treating Advice to patients: Do not chew tablets due worm, threadworm). All household members
alveolar echinococcosis, treatment Taenia solium infections to prevent the devel- to bitter taste; take with food; caution should should be treated concurrently with a single
may be required for up to 2 years opment of cysticercosis. be used when performing tasks requiring dose of mebendazole, albendazole or py-
after radical surgery, or indefinitely in • Fruit juice can aid the expulsion of dwarf tape- mental alertness, may impair judgement and rantel. Since reinfection readily occurs, at least
inoperable cases. worms lodged in the intestinal mucous. Patient co-ordination. one further dose should be given 2–4 weeks
Administration: Doses should be taken between is regarded cured when 3 negative stool results Dose: Taenia saginata and T. solium infections, later. Piperazine is also effective but must be
meals. have been received. by mouth, ADULT and CHILD over 4
• Teach patient proper hygiene methods.
taken regularly for at least 7 consecutive days.
POM Mebendazole (WMF 6.1.1.) years 5–10 mg/kg as a single dose
Dose: Taenia solium infection, by mouth, Hymenolepis nana infection, by HOOKWORM INFECTIONS
Chewable tablets, Mebendazole 100 mg, 500 mg
ADULT and CHILD over 6 years 2 g as mouth, ADULT and CHILD over 4 Hookworm infections are caused by Ancylos-
EMDEX
POM Mebendazole (EDL 5.2) a single dose after a light breakfast, years, 15–25 mg/kg as a single dose. toma duodenale (ancylostomiasis) and Necator
Tablets, Mebendazole 100 mg, 500 mg. followed by a purgative after 2 hours; Diphyllobothrium latum infection, americanus (necatoriasis); they are a major
Suspension, Mebendazole 100 mg per 5 mL. CHILD under 2 years 500 mg, 2–6 by mouth, ADULT and CHILD over 4 cause of iron-deficiency anaemia in the tropics
POM CIKAMEB® (Michelle Lab) years 1 g. years, 10–25 mg/kg as a single dose. and sub-tropics. Ideally all cases of hookworm
Tablet, Mebendazole 100 mg T. saginata and Diphyllobothrium Cysticercosis, by mouth, ADULT and infection should be treated. However, when
100 mg – 6’s (in blisters) latum infections, by mouth, as for T. this is impracticable, priority should be given
CHILD over 4 years, 50 mg/kg daily in
POM ERIZOLE® (FAB) solium but half the dose may be taken 3 divided doses for 14 days with pred- to women in 2nd– and 3rd-trimester of preg-
Tablet, Mebendazole 100 mg after breakfast and the remainder 1 nisolone (or similar corticosteroid) nancy, children and debilitated patients. In
100 mg – 6’s hour later followed by a purgative 2 given 2–3 days before and through- hookworm, broadspectrum anthelminthics are
hours after last dose. out treatment period. preferred wherever other nematode infections
POM EXPELL® (Ranbaxy)
Suspension, Mebendazole 100 mg per 5 mL. Hymenolepis nana infection, by Dermal cysticercosis, by mouth, ADULT are endemic. Both mebendazole and alben-
Pack: 30 mL. mouth, ADULT and CHILD over 6 and CHILD over 4 years, 60 mg/kg dazole are effective.
years 2 g as a single dose on first day daily in 3 divided doses for 6 days.
POM MEBEZOLE® (Greenlife) In animal studies, albendazole and mebenda-
then 1 g daily for 6 days; CHILD under Note: The tablets should be taken unchewed with
Tablet, Mebendazole 100 mg; uncoated tab. zole have been found to be teratogenic. There
2 years 500 mg on the first day then some liquid during meals. Keeping the tablets or its
100 mg – 6. is some evidence to suggest that the use of
250 mg daily for 6 days; 2–6 years, 1 segments in the mouth can give a bitter taste which
POM MEBOK® (GoldMoore) can promote gagging or vomiting. mebendazole in pregnancy is not associated
g on first day then 500 mg daily for
Tablet, Mebendazole 100 mg; uncoated tab. with an increased incidence of adverse effects
6 days. POM Praziquantel (WMF 6.1.1.)
100 mg – 25 x 6’s. Administration: Tablets should be chewed thor- on the fetus. However, neither mebendazole
Tablets, Praziquantel 150 mg, 600 mg.
oughly (or crushed) before washing down with nor albendazole should be used during the
POM MEBOX® (Richygold)
Suspension, Mebendazole 100 mg per 5 mL. water. POM Praziquantel (EDL 5.2) first trimester of pregnancy to treat nematode
Tablet, Praziquantel 600 mg. infections. Both drugs are contraindicated for
POM VERMOX® (Janssen-Cilag) POM Niclosamide (WMF 6.1.1.)
Chewable tablet, Niclosamide 500 mg. POM PIQUET® (Richygold) the treatment of cestode infections in preg-
Tablet, Mebendazole 100 mg (light-brown scored
Caplet, Praziquantel 600 mg; white scored caplet nancy (see section 9.4.1.1).
tab), 500 mg (biconvex tab. marked ‘VERMOX 500’) POM YOMESAN® (Gemini)
100 mg – 6; 240. marked ‘RGT’ on one side and ‘600’ on the reverse. Levamisole is effective in the treatment of
Tablet, Niclosamide 500 mg; yellow, chewable tab.
500 mg – 1 marked ‘BAYER’ and ‘FE’. mixed Ascaris and hookworm infections and
Suspension, Mebendazole 100 mg per 5 mL. 500 mg – 4.
9.4.1.2 Intestinal nematode infections pyrantel has been highly effective in some
Pack: 30 mL. Intestinal nematode infections include asca- community-based control programmes,
POM WORMIN® (Interpharma) PRAZIQUANTEL riasis, capillariasis, enterobiasis, hookworm although several doses are often needed
Tablet, Mebendazole 100 mg Indications: Taenia saginata, T. solium, Hy- infection, strongyloidiasis, trichostrongyliasis to eliminate Necator americanus infection.
100 mg – 6’s menolepis nana and Diphyllobothrium latum and trichuriasis. Patients with iron-deficiency anaemia caused
Suspension, Mebendazole 100 mg per 5 mL by hookworm infection require supplementary
infections; trematode infections (sections ASCARIASIS
Pack: 30 mL iron salts and should receive ferrous sulfate
9.4.3.1 and 9.4.3.2).
POM X-PELL® (Jawa) Ascariasis is an infection, usually of the small (200 mg daily for adults) for at least 3 months
Contra-indications: Ocular cysticercosis.
Suspension, Mebendazole 100 mg per 5 mL intestine, caused by Ascaris lumbricoides after the haemoglobin concentration of 12
Precautions: Neurocysticercosis (corticos-
Pack: 30 mL. (roundworm). Single doses of levamisole or g/100 mL is obtained.
teroid cover with monitoring, in hospital);
pyrantel are effective; the broad-spectrum
pregnancy (Appendix 2); breastfeeding (avoid STRONGYLOIDIASIS
472 | 9.4.1.2 Intestinal nematode infections 9.4.1.2 Intestinal nematode infections | 473
Strongyloidiasis is an infection of the small or 200 mg initially then 100 mg twice 40 mg – 3’s (in blisters). Administration: Doses should be taken between
intestine caused by Strongyloides stercoralis. daily for 3 days (severe infections). Syrup, Levamisole HCl Ph. Eur. 47.2 mg (equiv. to 40 meals.
All infected patients should be treated. Iver- Strongyloidiasis, by mouth, ADULT mg Levamisole) per 5 mL.
POM Mebendazole (WMF 6.1.1)
mectin (section 9.4.2.3) in a single dose of 200 and CHILD over 2 years, 400 mg once Dose: The following doses of Retrax are given as a
Chewable tablets, Mebendazole 100 mg, 500 mg
single dose, preferably after a light meal.
µg/kg or 200 µg/kg/day on two consecutive or twice daily for 3 days.
Patient’s age in years Dose POM Mebendazole (EDL 5.2)
days is the treatment of choice for chronic Capillariasis, by mouth, ADULT and Tablets, Mebendazole 100 mg, 500 mg.
1-4 5 mL
strongyloidiasis but it may not be available CHILD over 2 years, 400 mg daily for Oral liquid, Mebendazole 100 mg per 5 mL.
5-15 10 mL
in all countries. Albendazole 400 mg once or 10 days. 16 and over 15 mL See section 9.4.1.1 for the proprietary preparations of
twice daily for 3 days is well tolerated by both OTC Albendazole (WMF 6.1.1) In cases of severe hookworm infection it is suggested Mebendazole.
adults and children aged over 2 years and it Chewable tablets, Albendazole 400 mg. that a second standard dose be given one or seven
may eradicate up to 80% of infections. Meben- days after the first, whichever timing is feasible.
dazole has also been used but, to be effective, OTC Albendazole (EDL 5.2) PIPERAZINE
Tablet, Albendazole 200 mg.
it must be administered for longer periods as MEBENDAZOLE Therapeutic category: Anthelmintic
Oral liquid, Albendazole 100 mg per 5 mL.
it has a limited effect on larvae and hence the Indications: Ascariasis, hookworm infections, Pharmacology: Piperazine is effective against
prevention of autoinfection. See section 9.4.1.1 for the proprietary preparations of round-worms (ascaris) and threadworms
Albendazole. enterobiasis, trichuriasis, and capillariasis;
TRICHOSTRONGYLIASIS cestode infections (section 9.4.1.1); tissue (enterobius). It produces reversible muscle
nematode infections (section 9.4.1.3). paralysis in roundworms which takes at least
Trichostrongyliasis is an infection of the small LEVAMISOLE 5 hours to develop; the worms are then easily
intestine caused by Trichostrongylus spp. In Precautions: Pregnancy (Appendix 2; see also
Indications: Ascariasis, hookworm, and mixed notes above and section 9.4.1.1); breastfeeding dislodged by gut movement.
symptomatic trichostrongyliasis, a single dose Indications: Treatment of enterobiasis and
ascariasis with hookworm infections; malig- (Appendix 3); interactions: Appendix 1.
of pyrantel (10 mg/kg) or albendazole (400 ascariasis.
nant disease (section 12.1). Adverse effects: GI disturbances, headache,
EMDEX
mg) is effective. Contra-indications: Liver disease, epilepsy,
Contra-indications: Breastfeeding (Appendix and dizziness; adverse effects associated with
TRICHURIASIS 3). use in cestode infections (section 9.4.1.1). renal failure.
Trichuriasis is an infection of the large intes- Precautions: Pregnancy (Appendix 2); interac- Advice to patients: Tablets may be chewed, Precautions: Impaired renal function, latent
tine caused by Trichuris trichiura (whipworm). tions: Appendix 1. swallowed whole, or crushed and mixed with epilepsy, chronic disorders of CNS.
Chemotherapy is required whenever symp- Adverse effects: Abdominal pain, nausea, food to minimise GI upset; hygienic precau- Adverse effects: Nausea, vomiting; colic,
toms develop or when faecal samples are vomiting, dizziness, and headache tions should be taken to prevent reinfection diarrhoea; headache, dizziness, convulsion,
found to be heavily contaminated (up to 10 000 Dose: Ascariasis, hookworm, and mixed as- such as wearing shoes and washing hands; muscular incoordination and weakness.
eggs per gram). A single dose of albendazole cariasis with hookworm infections, by wash all fruits and vegetables before eating; a Advice to patients: Take on an empty stom-
(400 mg) or mebendazole (500 mg) can be ef- mouth, ADULT and CHILD 2.5 mg/kg second course of therapy may be needed after ach for best absorption; if severe or persistent
fective in mild to moderate infections; heavier as a single dose; in severe hookworm 3 weeks if necessary; deworm all family mem- headache, loss of balance or co-ordination,
infections require a 3-day course. infection, a second dose may be bers; dietary restrictions, enamas or laxatives dizziness, vomiting, diarrhoea, or rash occurs,
given after 7 days. are not necessary. contact physician. If used for pinworm infec-
ALBENDAZOLE Dose: Ascariasis, by mouth, ADULT and tions, all members of family should be treated.
OTC Levamisole (WMF 6.1.1.2)
Indications: Ascariasis, hookworm infections, CHILD over 1 year, 500 mg as a single Nursing action: Administer drug crushed or
Tablets, Levamisole (as HCl), 50 mg, 150 mg
strongyloidiasis, enterobiasis, trichuriasis, dose or 100 mg twice daily for 3 days. chewed if patient is unable to swallow it whole;
OTC Levamisole (EDL 5.2) may be given with food, but for best absorption
trichostrongyliasis, and capillariasis; cestode Hookworm infections, trichuriasis,
Tablet, Levamisole 40 mg. give on an empty stomach.
infections (section 9.4.1.1); tissue nematode Oral liquid, Levamisole 40 mg per 5 mL. by mouth, ADULT and CHILD over 1
year, 100 mg twice daily for 3 days; • Give laxative if patient is constipated.
infections (section 9.4.1.3); filariasis (9.4.2.2).
OTC DUTRAX®(Drugfield) • Teach patient proper hygiene after bowel move-
Precautions: Pregnancy (see notes above and if eggs persist in the faeces, second
Tablet, Levamisole HCI 40 mg ment, to avoid reinfection.
Appendix 2; also section 9.4.1.1); interactions: course after 3–4 weeks; alternatively • Discontinue if CNS or significant GI reactions occur.
40 mg – 3’s
Appendix 1. (especially for mass treatment control • Because of potential for neurotoxicity, avoid
Adverse effects: GI discomfort, headache; OTC EVIKT® (Mecure) programmes), by mouth, ADULT and prolonged or repeated treatment, especially in
adverse effects associated with use in cestode Tablet, Levamisole 40 mg; red tab. CHILD over 1 year, 500 mg as a single children.
40 mg – 1 x 500’s. dose. Dose: Ascariasis, Adult and child >10 years,
infections (section 9.4.1.1).
Dose: Ascariasis, hookworm infections, OTC LEVATAB® (Laider) Enterobiasis, by mouth, ADULT and 30 mL elixir; 6-10 years, 20 mL; under
enterobiasis,and trichostrongyliasis, Tablet, Levamisole (as HCl) 40 mg CHILD over 2 years, 100 mg as a 2 years, 120 mg piperazine hydrate
by mouth, ADULT and CHILD over 2 40 mg – 3 x10’s. single dose, repeated after interval of per kg. b.wt. To be taken as a single
years, 400 mg as a single dose; child OTC MAXTEX® (Richygold) 2–3 weeks; all household members dose.
12 months–2 years, 200 mg as a Tablet, Levamisole 40 mg. over 2 years should be treated at the Enterobiasis, Adult and child >12
single dose. 40 mg – 500’s. same time. years, 15 mL elixir; 5-12 years, 10 mL;
Trichuriasis, by mouth, ADULT and Capillariasis, by mouth, ADULT and 2-4 years, 5 mL; <2 years 50-75 mg
OTC MEDTAX® (Embassy)
CHILD over 2 years, 400 mg as a single Tablet, Levamisole 40 mg. CHILD over 2 years, 200 mg daily for piperazine hydrate per kg b.wt. To be
dose (for moderate infections) or 400 40 mg – 500’s. 20–30 days; for mass treatment con- taken once daily for 7 days.
mg daily for 3 days (severe infections); trol programmes, by mouth, ADULT See lit. for dose equivalents of tablets
OTC RETRAX® (Reals)
child 12 months–2 years, 200 mg as a and CHILD over 2 years, 500 mg as a and granules.
Tablet, Levamisole HCI 47.2 mg equiv. to Levamisole
single dose (for moderate infections) 40 mg; dark red f-c tab.
single dose 4 times a year. OTC ANTEPAR® (SKG)
474 | 9.4.1.3 Tissue nematode infections 9.4.2 Antifilarials | 475
Elixir, Piperazine hydrate 750 mg per 5 mL (as hydrate a second dose after 2–4 weeks. prepared salt-water fish; and early evisceration be administered concurrently, either topically
and citrate). of fish after capture and freezing of seafood at or systemically.
Pack: 30 mL OTC Pyrantel (WMF 6.1.1.2)
Chewable tablet, Pyrantel (as embonate) 250 mg –20°C for at least 60 hours before sale.
OTC ANTEZIN® (SKG) Oral liquid, Pyrantel (as embonate) 50 mg/mL CUTANEOUS LARVA MIGRANS 9.4.2 Antifilarials
Elixir, Piperazine citrate; clear, orange coloured
OTC Pyrantel (EDL 5.2) Cutaneous larva migrans (creeping eruption) 9.4.2.1 Loiasis
solution.
Tablets, Pyrantel 125 mg. is caused by infection with larvae of animal 9.4.2.2 Lymphatic filariasis
Oral liquid, Pyrantel 125 mg per 5 mL. 9.4.2.3 Onchocerciasis
hookworms, usually Ancylostoma braziliense
OTC MATHEWWORM® (Daily Need)
OTC COMBANTRIN® (Neimeth) and A. caninum which infect cats and dogs.
Elixir, Piperazine (as citrate) 937.5 mg per 5 mL.
Tablet, Pyrantel pamoate 125 mg; orange tab. Albendazole (section 9.4.1) in a single dose 9.4.2.1 Loiasis
Pack: 30 mL.
125 mg – 6; 1000. of 400 mg is effective. Loiasis is an infection with the filarial nematode
OTC Moko Worm Elixir® (New Healthway) Caplet, Pyrantel pamoate 250 mg; orange caplet. Loa loa and is transmitted by the biting tabanid
Elixir, Piperazine (as citrate) 0.9375%. 250 mg – 3; 75. DRACUNCULIASIS
fly Chrysops. Diethylcarbamazine is effective
Pack: 30 mL. Suspension, Pyrantel pamoate 250 mg per 5 mL; Dracunculiasis (dracontiasis, guinea-worm against both adult worms and larvae; a single
yellow caramel flavoured susp. infection) is caused by infection with Dracun-
OTC PADRAX® (GSK) weekly dose is normally effective as prophy-
Pack: 15 mL. culus medinensis, acquired through drinking
Oral powder, Piperazine citrate 5 g per sachet. laxis. During individual treatment, particularly
Pack: 10 OTC COMBIWORM® (Vitabiotics) water containing larvae that develop in small of persons with heavy microfilaraemia (>50 000
OTC Piperazine (Emzor)
Tablet, Pyrantel pamoate 125 mg. freshwater crustaceans. Metronidazole microfilariae/mL blood), a condition simulating
Tablet, Piperazine (as citrate) 500 mg
125 mg – 12 x 6’s. (section 9.3.2) (25 mg/kg daily for 10 days, meningoencephalitis occasionally occurs. This
500 mg – 3; 100; 500; 1000. OTC Dr. Meyer’s D-Worm P® (Farmex) with a daily maximum of 750 mg for children) probably results from sludging of moribund
Suspension, Pyrantel pamoate 250 mg. provides rapid symptomatic relief. It also microfilariae within cerebral capillaries. The
OTC UVILON® (Gemini)
Pack: 15 mL. weakens the anchorage of the worms in the frequency of meningoen-cephalitis associated
EMDEX
Syrup, Piperazine hydrate 750 mg per 5 mL
Pack: 30 mL.
subcutaneous tissues, and they can then be with diethylcarbamazine therapy of loiasis
OTC PYRANTRIN® (Neimeth)
Tablet, Pyrantel pamoate 125 mg; orange flavoured. removed by traction. However, since it has no is reported as 1.25%, with a mortality rate of
OTC ZIMPERAZINE® (Gauze) effect on the larvae of pre-emergent worms,
Oral Liquid, Piperazine citrate 937.5 mg per 5 mL
Pack: 6’s; 1000’s. about 50% in affected patients; treatment with
Caplet, Pyrantel pamoate 250 mg; orange coloured. it does not immediately prevent transmission. diethylcarbamazine should be stopped at the
Pack: 30 mL; 2 L
Pack: 3’s; 75’s (in blisters) TRICHINELLOSIS first sign of cerebral involvement (and specialist
Oral suspension, Pyrantel pamoate 250 mg per 5 mL; advice sought). Permanent cerebral damage is
PYRANTEL yellow, caramel flavoured. Trichinellosis (trichinosis) is caused by infection
Indications: Ascariasis, hookworm infections, with the larvae of Trichinella spiralis. Each case common among patients who survive and this
Pack: 15 mL.
enterobiasis, and trichostrongyliasis; tissue of confirmed or even suspected trichinellosis possibility should be considered when decid-
OTC THELMIN® (Hovid) ing on treatment. Treatment of heavily infected
nematode infections (section 9.4.1.3). Tablet, Pyrantel pamoate 125 mg; f-c tab. infection should be treated in order to prevent
Precautions: Pregnancy; breastfeeding (Ap- the continued production of larvae. In both patients should thus begin at low dosage and
125 mg – 100. corticosteroid and antihistamine cover should
pendix 3); liver disease (reduce dose). adults and children, mebendazole (section
Adverse effects: Mild GI disturbances, head- OTC WORMRAX® (Embassy) 9.4.1) (200 mg daily for 5 days), albendazole be provided for the first 2 to 3 days.
Tablet, Pyrantel pamoate 125 mg.
ache, dizziness, drowsiness, insomnia, rash, and (section 9.4.1) (400 mg daily for 3 days), and
125 mg – 6’s. DIETHYLCARBAMAZINE
elevated liver enzymes. Suspension, Pyrantel pamoate 250 mg per 5 mL. pyrantel (section 9.4.1) (10 mg/kg daily for 5
Advice to patients: May mix drug with food, days) are all effective. Prednisolone (40–60 mg Indications: Treatment of loiasis; prophylaxis
Pack: 15 mL.
milk or fruit juice; strict hygiene is essential to daily) may be needed to alleviate the allergic of loiasis in temporary residents in endemic
prevent reinfection. and inflammatory symptoms. areas; tissue nematode infections (section
9.4.1.3 Tissue nematode infections
Nursing action: Shake well before pouring to 9.4.1.3); lymphatic filariasis (section 9.4.2.2).
Tissue nematode infections include angi- VISCERAL LARVA MIGRANS
assure acurate dosage; treat other members Contra-indications: Pregnancy (delay treat-
ostrongyliasis, anisakiasis, cutaneous larva Visceral larva migrans (toxocariasis) is caused ment until after delivery); infants, elderly, de-
of the family.
• Teach patient proper hygiene after bowel move- migrans, dracunculiasis, trichinellosis, and by infection with the larval forms of Toxocara bilitated (usually excluded from mass treatment
ment especially handwashing, scrubbing of finger visceral larva migrans. canis and less commonly, T. cati (which infect programmes; see also Precautions).
nails before and after eating, washing of the per- ANGIOSTRONGYLIASIS dogs and cats). Treatment should be reserved Precautions: Renal impairment (reduce dose;
ineal area and change of under pant. for symptomatic infections. A 3-week oral Appendix 4); cardiac disorders; other severe
• Instruct patient to wash all fruits and vegetables Angiostrongyliasis is caused by infection with
course of diethylcarbamazine (section 9.4.2) acute diseases—delay diethylcarbamazine
well before eating. the larvae of the rat lungworm, Parastrongylus
kills the larvae and arrests the disease, but treatment until after recovery; risk of menin-
• No dietary restrictions, laxatives, or enemas are cantonensis (Angiostrongylus cantonensis).
established lesions are irreversible. To reduce goencephalitis in severe infection (see notes
necessary. Symptomatic treatment pending spontaneous
the intensity of allergic reactions induced by above).
Dose: Ascariasis, trichostrongyliasis, by recovery is often all that is required.
dying larvae, dosage is commonly commenced Adverse effects: Headache, dizziness, drows-
mouth, ADULT and CHILD 10 mg/kg ANISAKIASIS at 1 mg/kg twice daily and raised progressively iness, N & V; immunological reactions, within
as a single dose.
Anisakiasis is caused by infection with seafood to 3 mg/kg twice daily (adults and children). a few hours of the first dose, subsiding by fifth
Hookworm infections, by mouth,
containing larvae of Anisakis, Contracaecum, or Ocular larva migrans occurs when larvae day of treatment, and including fever, head-
ADULT and CHILD 10 mg/kg as a
Pseudoterranova spp. In anisakiasis, anthelmin- invade the eye, causing a granuloma which ache, joint pain, dizziness, anorexia, malaise,
single dose.
thic treatment is rarely necessary. Prevention may result in blindness. In order to suppress nausea and vomiting, urticaria, and asthma in
Enterobiasis, by mouth, ADULT and
is dependent upon informing communities allergic inflammatory responses in patients asthmatics (similar to Mazzotti reaction—see
CHILD 10 mg/kg as a single dose with
of the hazards of eating raw or inadequately with ophthalmic lesions, prednisolone should section 9.4.2.3), induced by disintegrating
476 | 9.4.2.2 Lymphatic filariasis 9.4.2.3 Onchocerciasis | 477
microfilariae; microencephalitis (with heavy carbamazine 0.1% can eliminate W. bancrofti; a See section 9.4.2.1 for the proprietary preparations of IVERMECTIN
microfilaraemia, see notes above); reversible concentration of 0.3% for 3–4 months may be Diethylcarbamazine.
Indications: Suppressive treatment of oncho-
proteinuria. required where B. malayi is endemic. cerciasis; filariasis (section 9.4.2.2); strongyloid-
Advice to patients: Do not skip doses; take 9.4.2.3 Onchocerciasis iasis (section 9.4.1.2)
till gone. Complete the prescribed course DIETHYLCARBAMAZINE Contra-indications: Pregnancy (delay treat-
as directed to minimize allergic reactions to Onchocerciasis (river blindness) is caused by
Indications: Systemic lymphatic filariasis and ment until after delivery).
dying parasites. infection with the filarial nematode Oncho-
occult filariasis; loiasis (section 9.4.2.1); tissue Precautions: Breastfeeding (avoid treating
Dose: Loiasis, treatment, by mouth, ADULT cerca volvulus. The vector is the blackfly which
nematode infections (section 9.4.1.3). mother until infant is 1 week old).
1 mg/kg as a single dose on the first breeds near fastflowing rivers. Ivermectin
Contra-indications: Pregnancy (delay treat- Adverse effects: Mild ocular irritation; som-
day, doubled on 2 successive days, has transformed suppressive treatment of
ment until after delivery). nolence; raised liver enzymes; rarely postural
then adjusted to 2–3 mg/kg 3 times onchocerciasis and is now used extensively
Precautions: Renal impairment (reduce dose; hypotension; mild Mazzotti reaction within
daily for a further 18 days. in control programmes in many countries. It
Appendix 4); cardiac disorders; other severe 3 days of treatment, resulting from death of
Loiasis, prophylaxis, by mouth, ADULT rapidly eliminates microfilariae from the skin
acute disease—delay diethylcarbamazine microfilariae—fever, headache, sore throat,
300 mg weekly for as long as expo- and more gradually from the eye. Its microfilari-
treatment until after recovery. cough, pruritus, rash, conjunctivitis, arthralgia,
sure occurs. cidal action is more persistent and less liable to
Adverse effects: Headache, dizziness, drows- myalgia, lymphadenopathy, lymphadenitis,
provoke adverse reactions than that of diethyl-
POM Diethylcarbamazine (WMF 6.1.2) iness, N & V; immunological reactions, within oedema, weakness, tachycardia, N & V, diar-
carbamazine. A single oral dose of ivermectin
Tablets, Diethylcarbamazine (as dihydrogen citrate) a few hours of the first dose, subsiding by fifth rhoea.
reduces the microfilarial count to low levels
50 mg, 100 mg. day of treatment, including fever, headache, Advice to patients: To be taken with water on
for up to a year. It appears both to kill micro-
POM Diethylcarbamazine (EDL 5.4)
joint pain, dizziness, anorexia, malaise, tran- empty stomach. No food must be taken for at
filariae and to inhibit their expulsion from the
Tablet, Diethylcarbamazine (as citrate) 50 mg sient haematuria, urticaria, vomiting, asthma in least 2 hours before or after the dose.
uterus of female worms. A single annual dose
asthmatics (similar to Mazzotti reaction—see Dose: Suppression of microfilariae, by mouth,
EMDEX
POM BANOCIDE® (SKG) may suppress the microfilaraemia to a degree
section 6.1.2.3) induced by disintegrating mi- ADULT and CHILD over 5 years (and
Tablet, Diethylcarbamazine citrate 50 mg; white that prevents development of clinical disease.
crofilariae; nodules (palpable subcutaneously weighing over 15 kg), 150 µg/kg as a
scored tab. marked ‘WELLCOME S2A’ Although the drug is generally well tolerated, it
50 mg – 100. and along spermatic cord—formed by recently single dose once a year.
is advisable to have medical support available
killed worms); transient lymphangitis and exac-
POM CENOCIDE® (SKG) during treatment programmes. Patients with POM Ivermectin (WMF 6.1.2)
erbation of lymphoedema. Tablets ,(scored), Ivermectin 3 mg, 6 mg.
Tablet, Diethylcarbamazine 50 mg; off white, scored a heavy microfilarial load occasionally react
Dose: Lymphatic filariasis (bancroftian), by
tab. marked ‘S2A’ and ‘WELLCOME’. adversely and, rarely, transient severe postural POM Ivermectin (EDL 5.4)
mouth, ADULT and CHILD over 10
50 mg – 100’s; 1000’s in securitainers. hypotension has occurred within 12–24 hours Tablet, Ivermectin 6 mg.
years, 6 mg/kg daily, preferably in
of treatment.
divided doses after meals, for 12 days; POM IVACTIN® (Alpha)
9.4.2.2 Lymphatic filariasis Treatment of pregnant women with ivermectin Tablet, Ivermectin 6 mg; white to off-white scored
CHILD under 10 years, half the adult
Lymphatic filariasis is caused by infection with dose; mass treatment control pro- should be limited to those situations where the tab.
Wuchereria bancrofti (bancroftian filariasis), grammes, ADULT and CHILD over 10 risk of complications from untreated oncho- 6 mg – 6’s.
Brugia malayi or B. timori (brugian filariasis). years, 6 mg/kg in divided doses over cerciasis exceeds the potential risk to the fetus
Occult filariasis (tropical pulmonary eosin- 24 hours, once a year; CHILD under 10 from treatment. Mass treatment programmes SURAMIN
ophilia) is a clinical variant of W. bancrofti years, half the adult dose. should not include children under 15 kg, Indications: Curative treatment of onchocerci-
infection. Individual treatment with diethyl- Lymphatic filariasis (brugian), by pregnant patients or those with severe illness. asis; trypanosomiasis (section 9.3.4.1).
carbamazine which has both microfilaricidal mouth, ADULT and CHILD over Diethylcarbamazine is now largely super- Contra-indications: Previous anaphylaxis or
and macrofilaricidal activity is effective. Total 10 years, 3–6 mg/kg, preferably in seded as a microfilaricide in onchocerciasis suramin sensitivity; pregnancy (delay treat-
cumulative dosages of 72 mg/kg are generally divided doses after meals, for 6–12 because of the frequency with which it induces ment until after delivery); severe liver or renal
recommended for Wuchereria bancrofti infec- days; CHILD under 10 years, half the severe host (Mazzotti) reactions characterized function impairment; elderly or debilitated;
tions with half this dose used for Brugia malayi adult dose; mass treatment control by itching, rash, oedema, pain and swelling of total blindness (unless required for relief from
and B. timori infections. In all cases treatment is programmes, ADULT and CHILD over the lymph nodes, fever and severe eye lesions. intensely itchy lesions).
best initiated with smaller doses for 2–3 days to 10 years, 3–6 mg/kg in divided doses Precautions: Administer only under close
avoid the danger of immunological reactions. Suramin is the only macrofilaricide that is medical supervision in hospital and with gen-
over 24 hours, 6 times at weekly or
Rigorous hygiene to the affected limbs with currently available for use against Onchocerca eral condition of patient improved as far as
monthly intervals; CHILD under 10
adjunctive measures to minimize infection and volvulus. Administered intravenously over a possible before treatment (see notes above);
years, half the adult dose.
promote lymph flow are important for reduc- period of several weeks suramin also kills mi- first dose—possible loss of consciousness
Occult filariasis, by mouth, ADULT 8
ing acute episodes of inflammation. crofilariae. It is, however, one of the most toxic (see under Dosage, below); maintain satisfac-
mg/kg daily for 14 days, repeated as
substances used in clinical medicine and should tory food and fluid intake during treatment;
In communities where filariasis is endemic, an- necessary if symptoms return.
always be given under medical supervision in a urine tests before and weekly during treat-
nual administration of single doses of albenda- Note: The above dose regimens are intended only
as a guide, since many countries have developed hospital. A careful assessment must always be ment—reduce dose if moderate albuminuria,
zole 400 mg with either diethylcarbamazine made of the patient’s capacity to withstand the
specific treatment regimens. discontinue immediately if severe albuminuria
(6 mg/kg) or ivermectin (200 µg/kg) is effective effects of suramin treatment both before and
for interrupting transmission; this treatment is POM Diethylcarbamazine (WMF 6.1.2) or casts in urine.
during administration. Adverse effects: Rarely, immediate and po-
continued for at least 5 years. Trials in India and Tablets, Diethylcarbamazine citrate 50 mg, 100 mg
China have shown that the consistent use for tentially fatal reaction with nausea, vomiting,
POM Diethylcarbamazine (EDL 5.4)
6–12 months of table salt containing diethyl- shock and loss of consciousness during first
Tablet, Diethylcarbamazine (as citrate) 50 mg.
dose—see First (Test) Dose, above; albu-
478 | 9.4.3 Trematode infections 9.4.3.2 Fluke infections | 479
minuria; abdominal pain; severe diarrhoea; nor has mutagenic or carcinogenic activity mansoni (Egypt and southern Africa), See under section 9.4.1.1 for proprietary preparations
stomal ulceration; exfoliative dermatitis; fever; been shown in experimental animals. ADULT and CHILD 60 mg/kg in di-
tiredness; anorexia; malaise; polyuria; thirst; Drugs still widely used in the treatment of vided doses over 2–3 days (maximum 9.4.3.2 Fluke infections
raised liver enzyme values; paraesthesia and schistosomiasis include oxamniquine, which single dose 20 mg/kg).
hyperaesthesia of palms and soles; swelling, The intestinal flukes include Fasciolopsis buski,
is effective against S. mansoni. Strains resistant POM Oxamniquine (WMF 6.1.3) Metagonimus yokogawai, Heterophyes heter-
tenderness and abscess formation around to oxamniquine, which have been reported Capsule, Oxamniquine 250 mg.
adult worms; urtico-papular rash, painful hip, ophyes, Echinostoma spp. and Gastrodiscoides
in South America, have been effectively Oral liquid, Oxamniquine 250 mg/5 mL.
hand and foot joints, inflammatory and degen- hominis. The liver flukes include Clonorchis
treated with praziquantel. It is preferable to sinensis, Opisthorchis viverrini, O. felineus and
erative changes in optic nerve and retina—due delay treatment with oxamniquine in pregnant PRAZIQUANTEL
to dying microfilariae. Fasciola hepatica. In some areas C. sinensis
women until after delivery unless immediate Therapeutic category: Schistosomicide. and Opisthorchis spp. infections are strongly
Dose: Curative treatment of onchocerciasis, by intervention is essential. Due to lack of infor- Pharmacology: Praziquantel increases cell
slow IV injection, ADULT 3.3 mg/kg associated with cholangiocarcinoma (cancer
mation on whether oxamniquine is excreted in membrane permeability in susceptible worms, of the bile ducts). The lung flukes are of the
as a single dose (see First (Test) Dose breast milk, it is preferable not to administer it resulting in a loss of intracellular calcium,
administration, below), followed at genus Paragonimus.
to nursing mothers. massive contractions and paralysis of their
weekly intervals by incremental doses musculature. There is further vacuolization and Praziquantel has transformed the therapy
of 6.7 mg/kg, 10.0 mg/kg, 13.3 mg/ OXAMNIQUINE disintegration of the schistosome tegument of most fluke infections. Parasitological cure
kg, 16.7 mg/kg, and 16.7 mg/kg on followed by attachment of phagocytes to the has been obtained in virtually all cases (with
Therapeutic category: Schistosomicide
weeks 2 to 6 respectively (total dose parasite and death. the exception of Fasciola infections) without
Pharmacology: It is a quinoline compound
66.7 mg/kg over 6 weeks). Indications: Intestinal schistosomiasis; urinary significant adverse effect but it needs to be
active against Schistosoma mansoni. It causes
Reconstitution of Injection: Reconstitute in water taken for several days in the treatment of
the worms to shift from the mesenteric veins schistosomiasis; cestode infections (section
for injections to produce a final concentration of Paragonimus infections.
to the liver where they are destroyed. It has no 9.4.1.1); fluke infections (section 9.4.3.2).
EMDEX
10%.
significant activity against S. haematobium. Contraindications: Ocular cysticercosis (see Triclabendazole, a benzimidazole compound
FIRST (TEST) DOSE: Administer first dose with section 9.4.1.1). is highly effective and well tolerated, as a single
Indications: Intestinal schistosomiasis due to
particular caution; wait at least 1 minute after Precautions: Pregnancy (Appendix 2); breast- dose or two divided doses, for both Fasciola
Schistosoma mansoni (acute stage and chronic
injecting the first few microlitres; inject the feeding (Appendix 3); areas endemic for and Paragonimus infections.
hepatosplenic disease).
next 0.5 mL over 30 seconds and wait 1 minute; cysticercosis—possible oedematous reaction;
Precautions: Epilepsy—close observation,
inject the remainder over several minutes. interactions: Appendix 1. PRAZIQUANTEL
may precipitate seizures; pregnancy and
POM Suramin (WMF 6.1.2) breastfeeding (see notes above). Adverse effects: Abdominal discomfort, nau- Indications: Intestinal flukes, liver flukes, and
Powder for injection, Suramin sodium 1 g; in vial. sea, vomiting, malaise, headache, dizziness, lung flukes; cestode infections (section 9.4.1.1);
Adverse effects: Commonly, dizziness and
drowsiness, rectal bleeding; rarely hypersen- schistosomiasis (section 9.4.3.1).
drowsiness; headache, nausea, vomiting,
9.4.3 Trematode infections diarrhoea; intense reddish discoloration of
sitivity reactions, including fever, pruritus, Contra-indications: Ocular cysticercosis (see
eosinophilia (may be due to dead and dying section 9.4.1.1).
9.4.3.1 Schistosomiasis urine; rarely, urticaria, hallucinations, epilepti-
9.4.3.2 Fluke infections parasites). Precautions: Paragonimus infections—treat-
form convulsions; raised liver enzyme values;
Advice to patients: Do not chew tablets due ment in hospital as may be central nervous
transient fever, eosinophilia, scattered pul-
9.4.3.1 Schistosomiasis to bitter taste; take with food; caution should system involvement; pregnancy (unless im-
monary infiltrates (Loeffler syndrome)—after
be used when performing tasks requiring mediate treatment required, delay treatment
Schistosomiasis, a waterborne parasitic infec- 3-day course in patients in Egypt and eastern
mental alertness, may impair judgement and until after delivery; Appendix 2); breastfeeding
tion, is caused by several species of trematode Mediterranean.
co-ordination. (avoid during and for 72 hours after treatment);
worms (blood flukes). Its socioeconomic im- Nursing action: Give orally, after meals for
Nursing action: Tablets can be halved or quar- areas endemic for cysticercosis—possible
pact as a parasitic disease is outstripped only improved GI tolerance.
• Teach patient to avoid driving and other hazardous tered; laxatives may be given before treatment oedematous reaction; interactions: Appen-
by that of malaria. Intestinal schistosomiasis to cleanse bowel.
activities if he feels drowsy. dix 1.
is caused principally by Schistosoma mansoni • Teach patient proper hygiene techniques.
• Teach patient proper personal hygiene; tell patient Adverse effects: Abdominal discomfort, nau-
as well as S. japonicum, S. mekongi, and S. in- that urine may turn orange or red. • Patient should not breast-feed on the day of treat- sea, vomiting, malaise, headache, dizziness,
tercalatum. Urinary schistosomiasis is caused • Use cautiously in patients with a history of seizure ment and 72 hours after.
drowsiness, rectal bleeding; rarely hypersensi-
by S. haematobium. The latter is an important disorders. Epileptiform seizure have rarely been Dose: Schistosomiasis, by mouth, ADULT and
tivity reactions, including fever, pruritus.
predisposing cause of squamous cell cancer observed within the first few hours after ingestion. CHILD over 4 years 40–60 mg/kg as a
Advice to patients: Do not chew tablets due
of the bladder. Dose: Intestinal schistosomiasis due to S. single dose; alternatively 3 doses of
to bitter taste; take with food; caution should
Praziquantel has transformed the treatment of mansoni (West Africa, South America, 20 mg/kg on one day at intervals of
be used when performing tasks requiring
schistosomiasis and is often effective in a single Caribbean islands), by mouth, ADULT 4–6 hours.
mental alertness, may impair judgement and
15 mg/kg as a single dose; CHILD Note: The tablets should be taken unchewed with
dose, against all species of the parasite. It can co-ordination.
under 30 kg, 20 mg/kg in 2 divided some liquid during meals. Keeping the tablets or its
be of particular value in patients with mixed segments in the mouth can give a bitter taste which Dose: Intestinal fluke infections, by mouth,
infections and those who do not respond doses. ADULT and CHILD over 4 years, 25
can promote gagging or vomiting.
adequately to other drugs. It is also extremely Intestinal schistosomiasis due to S. mg/kg as a single dose.
well tolerated and well suited for mass treat- mansoni (East and central Africa, POM Praziquantel (WMF 6.1.3)
Tablet, Praziquantel 600 mg.
Liver and lung fluke infections, by
ment control programmes. Extensive use over Arabian peninsula), by mouth, ADULT mouth, ADULT and CHILD over 4
several years has provided no evidence of and CHILD 30 mg/kg in 2 divided POM Praziquantel (EDL 5.8) years, 25 mg/kg 3 times daily for 2
serious adverse effects or long-term toxicity, doses. Tablet, Praziquantel 600 mg. consecutive days; alternatively 40
Intestinal schistosomiasis due to S.
480 | 9.5 Antiviral drugs 9.5.1 Herpes and cytomegalovirus infections | 481
mg/kg as a single dose; treatment is generally not required except for immuno- test results. 3 months (with disseminated herpes
may need to be extended for several compromised patients and those at special risk • Administer tablet with or without food with a full simplex), 20 mg/kg every 8 hours for
days in paragonimiasis. (for example because of severe cardiovascular glass of water. Shake suspension before use. 10–14 days (21 days if CNS involve-
Note: The tablets should be taken unchewed with or respiratory disease or chronic skin disorder); • Avoid giving by bolus IV injection; infusion must ment); CHILD 3 months–12 years,
some liquid during meals. Keeping the tablets or its be administered over at least 1 hour to prevent
aciclovir should be given for 10 days with at 250 mg/m2 every 8 hours usually for
segments in the mouth can give a bitter taste which renal tubular damage.
least 7 days of parenteral treatment. Specialist • Maintain adequate fluid intake to prevent deposit
5 days.
can promote gagging or vomiting.
advice should be sought for the treatment of in kidneys. Treatment of herpes simplex encephali-
POM Praziquantel (WMF 6.1.3) chickenpox during pregnancy. • Discontinue drug therapy and inform the physician tis, varicella-zoster in the immunocom-
Tablet, Praziquantel 600 mg. if severe abdominal pain and bleeding occur. promised, by IV infusion, ADULT and
While most HIV positive patients with herpes
POM Praziquantel (EDL 5.8) zoster (shingles) experience only one self-lim- • Teach patient that drug does not cure infection but CHILD over 12 years 10 mg/kg every 8
Tablet, Praziquantel 600 mg. symptoms will be controlled. hours; CHILD 3 months–12 years, 500
iting course, some will experience repeated
Dose: Treatment of herpes simplex (including mg/m2 every 8 hours; usually given
See section 9.4.3.1 for the proprietary preparations of episodes. Treatment should be reserved for
genital herpes), by mouth, ADULT for at least 10 days in encephalitis,
Praziquantel. debilitating disease and when there is high
and CHILD over 2 years, 200 mg (400 possibly for 14–21 days.
risk of serious complications, such as in ad-
mg in the immunocompromised Reconstitution and Administration: According
TRICLABENDAZOLE vanced HIV disease. Aciclovir is the treatment
or if absorption impaired) 5 times to manufacturer’s directions. In obese patients,
of choice and it can be administered in high parenteral dose should be calculated on the basis of
Indications: Fascioliasis; paragonimiasis daily, usually for 5 days (longer if new
oral dose or in the case of lack of response to ideal weight for height (to avoid excessive dosage).
Precautions: Paragonimus infections—treat- lesions appear during treatment or if
oral therapy or CNS involvement, it should be
ment in hospital as may be central nervous healing incomplete); CHILD under 2 POM Aciclovir (WMF 6.5.1)
given intravenously.
system involvement; severe fascioliasis—bil- years, half adult dose. Tablet, Aciclovir 200 mg.
iary colic, due to obstruction by dying worms. CYTOMEGALOVIRUS (CMV) Prevention of recurrent herpes simplex, Powder for injection, Aciclovir (as sodium salt) 250
EMDEX
Adverse effects: GI discomfort; headache. Parenteral antiviral ganciclovir arrests retino- by mouth, ADULT 200 mg 4 times mg; in vial.
Dose: Fascioliasis, by mouth, ADULT and choroiditis and enteritis caused by CMV in HIV daily or 400 mg twice daily possibly POM Aciclovir (EDL 5.11)
CHILD over 4 years, 10 mg/kg as a infected patients. Maintenance therapy with reduced to 200 mg 2–3 times daily Tablets, Aciclovir 200 mg, 400 mg.
single dose. oral ganciclovir should be given to prevent and interrupted every 6–12 months Oral liquid, Aciclovir 200 mg per 5 mL.
Paragonimiasis, by mouth, ADULT and relapse of retinitis. Alternative therapy with infor reassessment. Injection, Aciclovir (as Sodium salt) 250 mg; powder
CHILD over 4 years, 20 mg/kg given in travenous foscarnet can be used if necessary. Prophylaxis of herpes simplex in the im- for injection in vial.
munocompromised, by mouth, ADULT Cream, See under section 15.1.4
2 divided doses.
POM Triclabendazole (WMF 6.1.3)
ACICLOVIR and CHILD over 2 years, 200–400 mg POM Aciclovir (Evans)
Tablet, Triclabendazole 250 mg. Synonym: Acyclovir 4 times daily; CHILD under 2 years, Tablet, Aciclovir 200 mg; round white uncoated tab.
half adult dose. 200 mg – 10’s (in strips)
Indications: Treatment of primary genital
9.5 Antiviral drugs herpes; disseminated varicella–zoster in im- Treatment of chickenpox, by mouth, POM Aciclovir (Neros)
munocompromised patients; herpes simplex ADULT 800 mg 4–5 times daily for Tablet, Aciclovir 200 mg
9.5.1 Herpes and cytomegalovirus infections 5–7 days; CHILD under 2 years 200 200 mg – 10 x 10’s (in blister)
9.5.2 Antiretroviral drugs
encephalitis; eye (section 13.1).
Precautions: Maintain adequate hydration; mg 4 times daily, 2–5 years 400 mg POM Acyclovir (Solution Pharma)
9.5.3 Other antivirals
renal impairment (Appendix 4); pregnancy 4 times daily, over 6 years 800 mg 4 Tablet, Aciclovir 200 mg; white scored tab. marked
(Appendix 2); breastfeeding (Appendix 3); times daily. ‘TRL’
9.5.1 Herpes and cytomegalovirus Treatment of herpes zoster, by mouth,
infections interactions: Appendix 1. POM ACYLEX® (Biostadt)
Adverse effects: Nausea, vomiting, abdom- ADULT 800 mg 5 times daily for 7–10
Tablet, Aciclovir 200 mg, 400 mg, 800 mg; f-c tab
HERPES SIMPLEX VIRUS (HSV) INFECTIONS inal pain, diarrhoea, headache, fatigue, rash, days. 200 mg – 5 x 5’s (in blisters)
Aciclovir is active against herpes viruses but urticaria, pruritus, photosensitivity; very rarely Treatment of herpes simplex in the 400 mg – 2 x 10’s (in blisters)
does not eradicate them. It is only effective if hepatitis, jaundice, dyspnoea, neurological immunocompromised, severe initial Suspension, Aciclovir 200 mg per 5 mL
started at onset of infection; it is also used for reactions (including dizziness, confusion, genital herpes, by IV infusion, ADULT Pack: 60 mL
prevention of recurrence in the immunocom- hallucinations, convulsions, drowsiness), acute and CHILD over 12 years 5 mg/kg Ointment, Aciclovir 50 mg per gram
promised. Genital lesions, oesophagitis and renal failure, anaemia, thrombocytopenia, every 8 hours usually for 5 days. Pack: 5 gm tube
proctitis may be treated with oral aciclovir. HSV leukopenia; on intravenous infusion, severe Treatment of varicella–zoster, by IV POM Apo-Acyclovir® (Lahams)
encephalitis or pneumonitis should be treated local inflammation (sometimes resulting in infusion, ADULT and CHILD over 12 Tablet, Aciclovir 200 mg; blue, bevel-edged tab.
with intravenous aciclovir. ulceration), and very rarely fever, agitation, years 5 mg/kg every 8 hours usually marked ‘APO 200’.
tremor, psychosis. for 5–7 days (dose doubled in the 200 mg – 100.
Valaciclovir [not included on WHO Model List],
Advice to patients: .Patients are contagious immunocompromised); NEONATE POM HEPIRAX® (Goben)
a prodrug of aciclovir, can be given by mouth
only when viral shedding is occurring; recur- and INFANT up to 3 months, 10–20 Dispersible tablet, Aciclovir 200 mg; blue, shield-
as an alternative treatment for herpes simplex
rences tend to appear within 3 months of mg/kg every 8 hours for at least 7 shaped dispersible tab. marked ‘CCM’ and ‘200’.
infections of the skin and mucous membranes
original infection; Aciclovir is NOT a cure; avoid days; CHILD 3 months–12 years, 250 200 mg – 3 x 10’s; 5 x 10’s.
(including initial and recurrent genital herpes). Dispersible tablet, Aciclovir 400 mg; pink, shield-
sexual intercourse when lesions are present; mg/m2 every 8 hours usually for 5
VARICELLA–ZOSTER INFECTIONS days (dose doubled in the immuno- shaped dispersible tab. marked ‘CCM’ and ‘400’.
may take with food.
compromised). 400 mg – 7 x 10’s.
Chickenpox in neonates should be treated Nursing action: Obtain specimen for C&S test Administration: To be swallowed whole with a little
with parenteral aciclovir to reduce the risk of before first dose; therapy may begin pending Treatment of herpes simplex, by IV
water or dispersed in a minimum of 50 mL of water.
severe disease. Otherwise, antiviral treatment infusion, NEONATE and INFANT up to
482 | 9.5.2 Antiretroviral drugs 9.5.2 Antiretroviral drugs | 483
POM LOVIR® (Ranbaxy) who.int/hiv/pub/guidelines/adult/en/index.html). is reduced by using a combination of 3 or 4 Recommended initial treatment with a potent
Tablets, Aciclovir 200 mg, 400 mg. • Antiretroviral therapy of HIV infection in infants and drugs; such combinations should have additive combination of antiretroviral drugs (‘highly
200 mg – 5 x 5 (in blisters) children: Towards universal access: Recommenda- or synergistic activity while ensuring that their active antiretroviral therapy’, HAART) includes:
400 mg – 5 x 5 (in blisters). tions for a public health approach, 2006 (available toxicity is not additive. • 2 nucleoside reverse transcriptase inhibitors (sec-
at: http://www.who.int/hiv/pub/guidelines/art/ tion 9.5.2.1), plus
POM VIREST® (Hovid) Women of childbearing age receiving antiret-
en/index.html). • a non-nucleoside reverse transcriptase inhibitor
Tablets, Aciclovir 200 mg, hexagon-shaped, blue
• Antiretroviral drugs for treating pregnant women roviral therapy must have available effective (section 9.5.2.2), or
uncoated tab.; 400 mg, hexagon-shaped, pink
and preventing HIV Infection in infants: Towards contraceptive methods to prevent unintended • a third nucleoside reverse transcriptase inhibitor
uncoated tab.
universal access: Recommendations for a public pregnancy. Women who are taking non-nu- (section 9.5.2.1), or
200 mg – 100; blisters of 5 x 5
health approach, 2006 (available at: http://www. cleoside reverse transcriptase inhibitors or • a protease inhibitor which may be combined with
400 mg – 150, blisters of 5 x 5.
who.int/hiv/pub/guidelines/pmtct/en/index.html). ritonavir as booster (section 9.5.2.3).
protease inhibitors which can lower blood
POM VIVORAX® (Interpharma) • Other current WHO guidelines on HIV and AIDS
are available at: http://www.who.int/hiv/pub/
concentration of hormonal oral contraceptives, MONITORING
Tablet, Aciclovir 200 mg.
200 mg – 10’s. guidelines/en/ should be advised to use additional or alterna-
In resource-limited settings the basic clinical
tive contraceptives.
POM WATCLOV® (Watson) Antiretroviral drugs do not cure HIV (human assessment before initiating antiretroviral
Tablet, Aciclovir 200 mg; white tab. immunodeficiency virus) infection; they only DRUGS USED TO TREAT HIV INFECTION therapy includes documentation of past med-
temporarily suppress viral replication and Zidovudine, a nucleoside reverse transcriptase ical history, identification of current and past
POM ZOVIRAX® (GSK)
Tablet, Aciclovir 200 mg improve symptoms. Patients receiving these inhibitor (or ‘nucleoside analogue’), was the HIV-related illnesses, identification of co-exist-
200 mg – 25. drugs require careful monitoring by appropri- first anti-HIV drug to be introduced. Other ing medical conditions that may influence the
Suspension, Aciclovir 200 mg per 5 mL. ately trained health professionals in an ade- nucleoside reverse transcriptase inhibitors choice of therapy (for example, pregnancy or
Injection, Aciclovir (as sodium salt) 250 mg; powder quately resourced setting. Rigorous promotion include abacavir, didanosine, emtricitabine, tuberculosis) as well as current symptoms and
in vial. of measures to prevent new infections remains lamivudine, and stavudine. Nucleotide re- physical signs.
EMDEX
POM ZOYLEX® (Pharmabox) essential and its need is not diminished by the verse transcriptase inhibitors act in a similar The absolute minimum laboratory tests before
Tablet, Aciclovir 200 mg; pale blue, hexagonal tab. availability of antiretroviral drugs. Effective way and include tenofovir. initiating antiretroviral therapy are an HIV
200 mg – 25’s; 50’s; 100’s; 300’s therapy requires the simultaneous use of 3 or The protease inhibitors include indinavir, antibody test (in patients over 18 months
4 drugs; alternative regimens are necessary lopinavir, nelfinavir, ritonavir and saquina- of age) and a haemoglobin or haematocrit
IDOXURIDINE to meet specific requirements at start-up, to vir. Ritonavir in low doses is used in combi- measurement.
substitute for first-line regimens in cases of nation with indinavir, lopinavir or saquinavir
POM Idoxuridine (EDL 5.11) Additional basic testing should include:
intolerance, or to replace failing regimens. The as a booster. The small amount of ritonavir in
Topical solution, See under Section 15.1.4 • white blood cell count;
use of a 3– or 4-drug combination as specified such combinations has no intrinsic antiviral • differential cell count (to identify a decline in
LAMIVUDINE in the WHO treatment guidelines is recom- activity but it increases the antiviral activity of neutrophils and the possibility of neutropenia);
mended. Fixed-dose preparations for some the other protease inhibitors by reducing their • total lymphocyte count;
Indications: Treatment of chronic hepatitis B
drug combinations are available; their use is metabolism. Indinavir, nelfinavir, ritonavir and • serum alanine or aspartate aminotransferase
virus infection in adult and children over 16
recommended if the pharmaceutical quality is possibly saquinavir inhibit the cytochrome
concentration to assess the possibility of hepatitis
years of age. co-infection and to monitor for hepatotoxicity;
assured and interchangeability with the single P450 enzyme system and therefore have a
Contra-indications, Precautions, etc: See • serum creatinine and/or blood urea nitrogen to
products is demonstrated as specified by the potential for significant drug interactions.
Lamivudine under HIV below. assess baseline renal function;
relevant drug regulatory authority. Protease inhibitors are associated with lipodys-
Dose: By mouth, Adult (>12 years) 100 mg • serum glucose;
once daily. To be swallowed whole Selection of 2 or 3 protease inhibitors from the trophy and other metabolic effects (see below). • pregnancy tests for women.
with water and with or without food. Model List will need to be determined by each The non-nucleoside reverse transcriptase Desirable supplemental tests include measure-
See lit. for details. country after consideration of local treatment inhibitors include efavirenz and nevirapine. ment of liver enzymes, creatinine, glucose and
guidelines and experience, as well as compar- They interact with a number of drugs metab- serum lipids. CD4-cell determinations are, of
POM Lamivudine (Jopan)
ative costs of available products. Low-dose olized in the liver; the doses of protease inhib- course, very desirable and efforts should be
Tablet, Lamivudine 150 mg
150 mg – 60’s (in jar)
ritonavir is used in combination with indinavir, itors may need to be increased when they are made to make these widely available. Viral
lopinavir or saquinavir as a ‘booster’; ritonavir given with efavirenz or nevirapine. Nevirapine load testing is currently considered optional
POM ZEFFIX® (GSK) is not recommended as a drug in its own right.
Tablet, Lamivudine 100 mg; capsule shaped and is associated with a high incidence of rash because the exact threshold to be used for
butterscotch coloured f-c tab. PRINCIPLES OF TREATMENT (including Stevens-Johnson syndrome) and oc- switching therapy is still not clearly defined;
Treatment is aimed at reducing the plasma viral casionally fatal hepatitis. Rash is also associated its role in long-term therapy, particularly in set-
9.5.2 Antiretroviral drugs load as much as possible and for as long as with efavirenz but it is usually milder. Efavirenz tings with a limited formulary and healthcare
possible; it should be started preferably before treatment has also been associated with an infrastructure, is not well established.
9.5.2.1 Nucleoside reverse transcriptase inhibitors increased plasma cholesterolconcentration
9.5.2.2 Non-nucleoside reverse transcriptase the immune system is irreversibly damaged CHANGING THERAPY
and before the onset of clinical immunode- and neuropsychiatric symptoms (including
inhibitors Deterioration of the condition (including clin-
9.5.2.3 Protease inhibitors ficiency. The need for early drug treatment sleep disorders and depression).
ical, immunological, and virological changes)
9.5.2.4 Fixed-dose combinations should, however, be balanced against the INITIATION OF TREATMENT usually calls for replacement of the failing
WHO has published the following guidelines development of toxicity. Commitment to The time for initiating antiviral treatment is drugs. Intolerance to adverse effects and
on antiretroviral therapy for HIV. treatment and strict adherence over many determined by the clinical stage of the HIV drug-induced organ dysfunction usually re-
• Antiretroviral therapy for HIV infection in adults years are required; the regimen chosen should infection as indicated by signs and symptoms, quire change in therapy.
and adolescents: Recommendations for a Public take into account convenience and the patient’s and where available, by the CD4-cell count.
Health Approach, 2006 (available at: http://www. tolerance of it. The development of resistance The choice of an alternative regimen depends
484 | 9.5.2 Antiretroviral drugs 9.5.2.1 Nucleoside reverse transcriptase inhibitors | 485
on factors such as the response to previous Various regimens have been used to specif- resistance and dyslipidaemia; collectively out, even when other diagnoses possible—if
treatment, tolerance and the possibility of ically prevent the transmission of HIV from these effects have been termed lipodystrophy rechallenge necessary it must be carried out in
cross-resistance. If treatment fails, a new sec- mother to the neonate at term. Women not syndrome. Regimens containing protease hospital setting; if abacavir is stopped for any
ond-line regimen will be needed. If toxicity already taking antiretrovirals should receive inhibitors and some nucleoside reverse tran- reason other than hypersensitivity, exclude
occurs, and it is related to an identifiable drug zidovudine from the 28th week of pregnancy scriptase inhibitors (particularly stavudine) hypersensitivity reaction as the cause and
in the regimen, the offending drug can be sub- (or as soon as possible thereafter); they should are associated with redistribution of body rechallenge only if medical assistance is readily
stituted with another drug that does not have also receive a single dose of nevirapine during fat in some patients (for example, decreased available; care needed with concomitant use of
the same adverse effect profile. However, if it labour. Zidovudine and lamivudine should also fat under the skin, increased abdominal fat, drugs which cause skin toxicity.
is not possible to identify the offending drug, be given to the mother during labour and for ‘buffalo humps’ and breast enlargement). HEPATIC DISEASE: Potentially life-threatening
an entirely new regimen should be considered. 1 week after birth. Antiretrovirals, particularly protease inhibitors, lactic acidosis and severe hepatomegaly with
PREGNANCY New born infants should receive a single dose are associated with dyslipidaemia. Protease steatosis reported—caution in patients (par-
of nevirapine, as well as zidovudine for 1 week. inhibitors are also associated with metabolic ticularly obese women) with hepatomegaly,
Treatment of HIV infection in pregnancy abnormalities such as insulin resistance and
aims to: Longer courses of zidovudine, usually up to 4 hepatitis, liver enzyme abnormalities, or risk
weeks, may be necessary depending on the an- hyperglycaemia. Clinical examination should factors for liver disease and hepatic steatosis
• minimize the viral load and disease progression
tiretroviral drug regimen given to the mother. include an evaluation of fat distribution; (including alcohol abuse); discontinue if
in the mother;
• reduce the risk of toxicity to the fetus (although Alternative regimens can be used. monitoring of serum lipids and blood glucose rapid deterioration in liver function tests,
the teratogenic potential of most antiretroviral should be considered. symptomatic hyperlactataemia, progressive
More information is available in Antiretroviral drugs for
drugs is unknown); hepatomegaly or lactic acidosis.
treating pregnant women and preventing HIV Infection
• prevent transmission of infection to the neonate.
in infants: Towards universal access: Recommendations
9.5.2.1 Nucleoside reverse Adverse effects: Hypersensitivity reactions
In pregnant women, it may be desirable to for a public health approach, 2006 (available at: http:// transcriptase inhibitors (see above), nausea, vomiting, diarrhoea,
initiate antiretroviral therapy after the first www.who.int/hiv/pub/guidelines/pmtct/en/index.html). In some settings it may not be possible to carry anorexia, lethargy, fatigue, fever, headache,
EMDEX
trimester, although for pregnant women who out full monitoring described under each drug insomnia, dizziness; blood disorders; lipo-
are severely ill, the benefit of early therapy BREASTFEEDING entry; in such cases the level of monitoring dystrophy (see notes above); pancreatitis,
outweighs the potential risk to the fetus. All Antiretroviral drugs may be present in breast- should be determined by local guidelines (see liver damage and lactic acidosis (see hepatic
treatment options require careful assessment milk, and may reduce viral load in breastmilk also notes above). disease, above); very rarely Stevens-Johnson
by a specialist. and reduce the risk of transmission through syndrome and toxic epidermal necrolysis; rash
breastfeeding. However, the concentration ABACAVIR and GI disturbances more common in children.
A combination of zidovudine, lamivudine and
nevirapine is the recommended treatment for of antiretroviral drugs in breastmilk may not Synonym: ABC Advice to patients: Patients should be told
women who are pregnant and are eligible for be adequate to prevent viral replication and Indications: HIV infection in combination with the importance of regular dosing (intermittent
antiviral treatment. Alternative regimens can there is therefore the possibility of promoting at least two other antiretroviral drugs. therapy may increase sensitization), how to rec-
be used. Monotherapy with either zidovudine the development of drug-resistant virus which Precautions: Chronic hepatitis B or C, hepatic ognize signs of hypersensitivity, and advised to
or with nevirapine reduces transmission of could be transmitted to the infant. impairment (see below and Appendix 5); renal seek immediate medical attention if symptoms
infection to the neonate (see also below), but Women with HIV infection should be coun- impairment (Appendix 4); pregnancy (see develop or before re-starting treatment.
combination antiretroviral therapy maximizes selled about the risks of breastfeeding and, notes above and Appendix 2); breastfeeding Dose: HIV infection (in combination with
the chance of preventing transmission and where possible, they should avoid breastfeed- (see notes above); interactions: Appendix 1. other antiretroviral drugs), by mouth,
represents optimal therapy for the mother’s ing. When replacement feeding is acceptable, HYPERSENSITIVITY REACTIONS: Life-threat- ADULT 300 mg twice daily; CHILD 3
own health. Low-dose ritonavir is required if feasible, affordable, sustainable and safe, ening hypersensitivity reactions reported— months–16 years, 8 mg/kg twice daily
either indinavir or saquinavir is used in preg- breastfeeding should be avoided. Otherwise, characterized by fever or rash and possibly (maximum 600 mg daily).
nancy because adequate drug concentration is exclusive breast-feeding is recommended dur- nausea, vomiting, diarrhoea, abdominal pain, POM Abacavir (WMF 6.4.2.1)
achieved only with ritonavir boosting. ing the first months of life and should then be dyspnoea, cough, lethargy, malaise, headache, Tablet, Abacavir (as sulfate) 300 mg.
discontinued as soon as feasible. HIV-infected and myalgia; less frequently mouth ulceration, Oral liquid, Abacavir (as sulfate) 100 mg/5 mL.
Lactic acidosis and hepatic steatosis associated
women should be counselled on infant feed- oedema, hypotension, sore throat, adult
with didanosine and stavudine may be more POM Abacavir (EDL 5.11.1.2)
ing options and they should be supported in respiratory distress syndrome, paraesthesia, Tablet, Abacavir (as sulfate) 300 mg.
frequent in pregnant women, particularly
their choice. arthralgia, conjunctivitis, lymphadenopathy, Oral liquid, Abacavir (as sulfate) 100 mg/5 mL.
when both drugs are used concomitantly.
lymphocytopenia, renal failure, and anaphy-
Tenofovir, is associated with potential fetal POST-EXPOSURE PROPHYLAXIS POM ABAVIR® (Evans)
laxis (hypersensitivity reactions presenting as
bone toxicity. Emtricitabine is believed to Treatment with antiretroviral drugs may be ap- Tablet, Abacavir (as sulfate) 300 mg; f-c tab.
sore throat, influenza-like illness, cough and 300 mg – 60’s
be non-teratogenic in humans, however, propriate following occupational exposure to breathlessness identified); rarely myolysis; Oral solution, Abacavir (as sulfate) 20 mg per mL
experience of its use in pregnancy is still HIV-contaminated material and sexual assault. laboratory abnormalities may include raised Pack: 100 mL; 240 mL.
limited. Therefore, emtricitabine, didanosine, Immediate expert advice should be sought in liver enzymes (see below) and creatine kinase;
stavudine, and tenofovir should be used in such cases; national guidelines on post-expo- symptoms usually appear in the first 6 weeks, DIDANOSINE
pregnancy only when no alternatives are avail- sure prophylaxis for healthcare workers and but may occur at any time; monitor for symp- Synonym: ddI, DDI
able. Protease inhibitors have been associated victims of sexual assault have been developed toms every 2 weeks for 2 months; discontinue Indications: HIV infection in combination with
with glucose intolerance and pregnant women and local ones may also be available. immediately if any symptom of hypersensi- at least two other antiretroviral drugs.
should be instructed to recognize symptoms of
LIPODYSTROPHY AND METABOLIC EFFECTS tivity develops and do not rechallenge (risk Precautions: History of pancreatitis (preferably
hyperglycaemia and to seek health care advice
of more severe hypersensitivity reaction); avoid, otherwise extreme caution, see also
if they occur. Metabolic effects associated with antiretrovi-
discontinue if hypersensitivity cannot be ruled below); peripheral neuropathy or hyperuri-
ral therapy include fat redistribution, insulin
486 | 9.5.2.1 Nucleoside reverse transcriptase inhibitors 9.5.2.1 Nucleoside reverse transcriptase inhibitors | 487
caemia (see under Adverse effects); chronic 60 kg 400 mg daily in 1–2 divided Dose: HIV infection (in combination with other Nursing action: Administer twice daily with
hepatitis B or C; renal impairment (Appendix doses; CHILD under 3 months, 50 mg/ antiretroviral drugs), by mouth, ADULT or without food; usually given with other
4); hepatic impairment (see below and Ap- m2 twice daily; 3 months–13 years, and CHILD, bodyweight over 33 kg, antiretrovirals.
pendix 5); pregnancy and breastfeeding (see 90–120 mg/m2 twice daily or 240 1 capsule (200 mg) or 24 mL (240 • Monitor children for pancreatitis viz abdominal
notes above); dilated retinal examinations mg/m2 once daily. mg) oral solution once daily; CHILD 4 pain, nausea, vomiting.
recommended (especially in children) every months–18 years, bodyweight under • Evaluate frequently for opportunistic infection and
POM Didanosine (WMF 6.4.2.1) other complications of HIV.
6 months, or if visual changes occur; interac- Tablets, (buffered chewable, dispersible), Didanosine 33 kg, 6 mg/kg (oral solution) once
• Teach patient that drug does not cure infection but
tions: Appendix 1. (with calcium and magnesium antacids) 25 mg, 50 daily. symptoms will be controlled.
PANCREATITIS: If symptoms of pancreatitis mg; 100 mg, 150 mg, 200 mg. POM Emtricitabine (WMF 6.4.2.1) Dose: HIV infection (in combination with other
develop or if serum amylase or lipase is raised Buffered powder for oral liquid, Didanosine (with Capsule, Emtricitabine 200 mg. antiretroviral drugs), by mouth, ADULT
(even if asymptomatic) suspend treatment un- calcium and magnesium antacids) 100 mg/sachet, Oral liquid, Emtricitabine 10 mg/mL.
167 mg/sachet, 250 mg/sachet.
150 mg twice daily or 300 mg once
til diagnosis of pancreatitis excluded; on return Note: 240 mg oral solution ≡ 200 mg capsule; where daily; INFANT under 1 month, 2 mg/
to normal values re-initiate treatment only if Capsules, (unbuffered enteric-coated), Didanosine appropriate capsules may be used instead of oral
125 mg, 200 mg, 250 mg, 400 mg. kg twice daily; CHILD 1 month or
essential (using low dose increased gradually solution; oral solution contains propylene glycol
Note: Antacids in the formulation may affect ab- as an excipient.
over, 4 mg/kg twice daily (maximum
if appropriate). Whenever possible avoid con- sorption of other drugs—see interactions: Appendix 300 mg daily).
comitant treatment with other drugs known 1 (antacids). Prevention of mother-to-child trans-
to cause pancreatic toxicity (for example LAMIVUDINE
POM Didanosine (EDL 5.11.1.2) mission of HIV (see also notes above
intravenous pentamidine isetionate); monitor Synonym: 3TC
Tablets, (buffered chewable, dispersible), Didanosine under Pregnancy), by mouth, ADULT
closely if concomitant therapy unavoidable. Therapeutic category: Antiviral Agent; Re-
25 mg, 50 mg, 100 mg, 150 mg, 200 mg. 150 mg at onset of labour followed by
Since significant elevations of triglycerides verse Transcriptase Inhibitor.
Capsules, (unbuffered enteric-coated), Didanosine 150 mg every 12 hours until delivery;
cause pancreatitis monitor closely if elevated. 125 mg, 200 mg, 250 mg, 400 mg. Indications: HIV infection in combination with
after delivery 150 mg twice a day for
EMDEX
Buffered powder for oral liquid, Didanosine 100 mg/ at least two other antiretroviral drugs; preven-
HEPATIC DISEASE: Potentially life-threatening 7 days.
sachet, 167 mg/sachet, 250 mg/sachet. tion of mother-to-child transmission of HIV (see
lactic acidosis and severe hepatomegaly with
also notes above under Pregnancy). POM Lamivudine (WMF 6.4.2.1)
steatosis reported—caution in patients (par- Tablet, Lamivudine 150 mg.
EMTRICITABINE Precautions: Renal impairment (Appendix 4),
ticularly obese women) with hepatomegaly, Oral liquid, Lamivudine 50 mg/5 mL.
Indications: HIV infection in combination with chronic hepatitis B or C, hepatic disease (see
hepatitis, liver enzyme abnormalities, or risk
other antiretroviral drugs. below); pregnancy and breastfeeding (see POM Lamivudine (EDL 5.11.1.2)
factors for liver disease and hepatic steatosis
Precautions: Renal impairment (Appendix 4), notes above); interactions: Appendix 1. Tablet, Lamivudine 150 mg.
(including alcohol abuse); discontinue if Oral solution, Lamivudine 5 mg/mL.
rapid deterioration in liver function tests, hepatic disease (see below); pregnancy (see HEPATIC DISEASE: Potentially life-threatening
symptomatic hyperlactataemia, progressive notes above and Appendix 2); breastfeeding lactic acidosis and severe hepatomegaly with POM AVOLAM® (Ranbaxy)
hepatomegaly or lactic acidosis. (see notes above). steatosis reported—caution in patients (par- Tablet, Lamivudine 150 mg.
ticularly obese women) with hepatomegaly, 150 mg – 60.
Adverse effects: Pancreatitis (see also under HEPATIC DISEASE: Potentially life-threatening
Precautions); peripheral neuropathy especially lactic acidosis and severe hepatomegaly with hepatitis (especially hepatitis C treated with POM EPIVIR® (GSK)
in advanced HIV infection–suspend (reduced steatosis reported—caution in patients (par- interferon alfa and ribavirin), liver enzyme Tablet, Lamivudine 150 mg; white diamond-shaped
dose may be tolerated when symptoms re- ticularly obese women) with hepatomegaly, abnormalities, or risk factors for liver disease f-c tab. marked “150” on one side and “GXCJ7” on
solve); hyperuricaemia (suspend treatment if and hepatic steatosis (including alcohol the reverse side.
hepatitis (especially hepatitis C treated with
abuse); discontinue if rapid deterioration in 150 mg – 60.
significant elevation); diarrhoea (occasionally interferon alfa and ribavirin), liver enzyme Oral Solution, Lamivudine 10 mg per mL; clear,
serious); also reported, nausea, vomiting, dry abnormalities, or risk factors for liver disease liver function tests, symptomatic hyperlacta-
colourless to pale yellow, strawberry-banana fla-
mouth, parotid gland enlargement, sialad- and hepatic steatosis (including alcohol abuse); taemia, progressive hepatomegaly or lactic voured liquid.
enitis, headache, hypersensitivity reactions, discontinue if rapid deterioration in liver acidosis. Exacerbation of hepatitis in patients Pack: 240 mL.
dry eyes, retinal and optic nerve changes function tests, symptomatic hyperlactataemia, with chronic hepatitis B may occur on discon-
tinuation of lamivudine. POM Lamivudine (Strides Vital)
(especially in children), diabetes mellitus, progressive hepatomegaly or lactic acidosis. Tablet, Lamivudine 150 mg.
hypoglycaemia, raised liver enzymes (see also Exacerbation of hepatitis in patients with Adverse effects: Nausea, vomiting, diarrhoea,
150 mg – 60’s.
under Precautions), liver failure, acute renal chronic hepatitis B may occur on discontinu- abdominal pain; cough; headache, fatigue,
failure, rhabdomyolysis; alopecia, insomnia, insomnia; malaise, fever, rash, alopecia, muscle POM LAVIR® (Fil Pharma)
ation of emtricitabine—monitoring required.
disorders; nasal symptoms; peripheral neurop- Tablets, Lamivudine 100 mg, 150 mg; f-c tabs.
dizziness, blood disorders, lipodystrophy (see Adverse effects: Nausea, vomiting, abdom- 100 mg – 60’s.
notes above). inal pain, dyspepsia, diarrhoea; headache, athy reported; rarely pancreatitis (discontinue);
150 mg – 60’s.
Advice to patients: To ensure sufficient ant- dizziness, peripheral neuropathy, asthenia, neutropenia, anaemia, thrombocytopenia and
acid from tablets containing antacid, each dose insomnia, abnormal dreams, depression; anae- red-cell aplasia; lactic acidosis; raised liver en- POM LAVUDINE® (Evans)
to be taken as 2 tablets (CHILD under 1 year zymes and serum amylase reported. Tablet, Lamivudine 150 mg.
mia, neutropenia; arthralgia, myalgia, bone ne-
Advice to patients: Lamivudine is not a cure 150 mg – 60’s.
1 tablet) chewed thoroughly, crushed or dis- crosis; elevated serum lipase, amylase, creatine
persed in water; tablets should be taken at least kinase, and liver enzyme concentrations (see for HIV infection and does not reduce risk of POM VIREX-L® (Fidson)
1 hour before food or on an empty stomach. also under Precautions), hyperbilirubinaemia, transmission to others; patient may still ex- Tablet, Lamivudine 150 mg; f-c tab.
Dose: HIV infection (in combination with perience illness associated with HIV infection; 150 mg – 3 x 10’s; 60’s.
hyper-triglyceridaemia, hyperglycaemia; rash,
other antiretroviral drugs), by mouth, to be taken exactly as prescribed and on an Syrup, Lamivudine 50 mg per 5 mL.
pruritus, urticaria, hyperpigmentation; lipodys- Pack: 100 mL.
ADULT under 60 kg 250 mg daily in trophy and metabolic effects (see also hepatic empty stomach if possible; children should
1–2 divided doses, body weight over disease above). be monitored for symptoms of pancreatitis.
488 | 9.5.2.1 Nucleoside reverse transcriptase inhibitors 9.5.2.1 Nucleoside reverse transcriptase inhibitors | 489
STAVUDINE POM Stavudine (WMF 6.4.2.1) neutropenia; nephritis, nephrogenic diabetes of selected patients with advanced AIDS in
Synonym: d4T Capsules, Stavudine 15 mg, 20 mg, 30 mg, 40 mg insipidus, renal impairment, effects on renal combination with Zidovudine.
Powder for oral liquid, Stavudine 5 mg/5 mL proximal tubules including Fanconi syndrome, Contra-indications: Hypersensitivity to Zalcit-
Therapeutic category: Antiviral agent; Nucle-
oside reverse transcriptase inhibitor. POM Stavudine (EDL 5.11.1.2) proteinuria, polyuria; reduced bone density; abine; avoid in pregnancy.
Indications: HIV infection in combination with Tablet, Stavudine 40 mg. pancreatitis, hepatitis, lactic acidosis (see Precautions: Monitor pancreatic enzymes and
at least two other antiretroviral drugs. POM AVOSTAV® (Ranbaxy)
hepatic disease above); raised liver enzymes, liver function tests in patients with history of
Precautions: History of peripheral neuropathy Capsule, Stavudine 40 mg. creatinine, and serum-amylase reported; see pancreatitis, increased amylase, those on par-
(see below); history of pancreatitis or concom- 40 mg – 60. also notes above. enteral nutrition or with a history of alcohol
itant use with other drugs associated with Dose: HIV infection (in combination with other abuse; discontinue immediately if pancreatitis
POM MELXICAP® (Evans)
pancreatitis; chronic hepatitis B or C, hepatic antiretroviral drugs), by mouth, ADULT is suspected; hepatic impairment (may exac-
Tablets, Stavudine 30 mg, 40 mg.
disease (see below); renal impairment (Appen- 30 mg – 60’s. 245 mg once daily. erbate existing liver dysfunction); peripheral
dix 4); pregnancy and breastfeeding (see notes 40 mg – 60’s. Administration: Tablets can be dispersed in at least neuropathy (avoid use if possible); safety and
100 mL water, orange juice or grape juice for patients efficacy not yet established in children less
above); interactions: Appendix 1.
POM STADINE® (Fil Pharma) with difficulty swallowing. than 13 years of age.
PERIPHERAL NEUROPATHY: Suspend if periph- Capsule, Stavudine 40 mg.
POM Tenofovir (WMF 6.4.2.1) Interactions: Increased risk of peripheral neu-
eral neuropathy develops characterized by 40 mg – 60’s.
Tablet, Tenofovir disoproxil fumarate 300 mg (equiv. ropathy or other toxicities with amphotericin,
persistent numbness, tingling or pain in feet POM Stavudine (Strides Vital) to 245 mg tenofovir disoproxil). aminoglycosides, chloramphenicol, cisplatin,
or hands; if symptoms resolve satisfactorily on Tablets, Stavudine 30 mg, 40 mg.
POM INFEX® (Evans) dapsone, ethionamide, isoniazid, metronida-
withdrawal, and if stavudine needs to be con- 30 mg – 60’s.
Tablet, Tenofovir disoproxil fumarate 300 mg (equiv. zole, vincristine, phenytoin, nitrofurantoin.
tinued, resume treatment at half previous dose. 40 mg – 60’s.
to Tenofovir disproxil 245 mg); f-c tab. Adverse effects: Oral ulcers, chest pain,
HEPATIC DISEASE: Potentially life-threatening POM VIREX-S30® (Fidson) 300 mg – 30’s headache, dizziness, myalgia, anaemia, gran-
EMDEX
lactic acidosis and severe hepatomegaly with Tablet, Stavudine 30 mg. ulocytopenia,skin rash, pruritus, nausea, dys-
steatosis reported—caution in patients (par- Pack: 3 x 10’s; 60’s. ZALCITABINE phagia, abdominal pain, vomiting, diarrhoea,
ticularly obese women) with hepatomegaly, Dose: For treatment of HIV infections: Adult (weigh-
Synonym.: Dideoxycytidine; ddc. body weight reduction, oedema, palpitations,
hepatitis, liver enzyme abnormalities, or risk ing <60 kg), one tablet twice daily.
Therapeutic category: Antiviral Agent; Re- increased heart rate, pancreatitis, hepatic
factors for liver disease and hepatic steatosis POM VIREX-S40® (Fidson) verse Transcriptase Inhibitor. disorders, peripheral neuropathy, tremors,
(including alcohol abuse); discontinue if Tablet, Stavudine 40 mg. Indications: Treatment as monotherapy in confusion, increased micturition frequency.
rapid deterioration in liver function tests, Pack: 3 x 10’s; 60’s. Advice to patients: Zalcitabine is not a cure
HIV-infected adults with advanced disease who
symptomatic hyperlactataemia, progressive Dose: For treatment of HIV infections: Adult (weigh-
cannot tolerate Zidovudine or whose disease for AIDS; if numbness or tingling occurs, or if
ing >60 kg), one tablet twice daily.
hepatomegaly or lactic acidosis. has progressed despite it; for the treatment persistent, severe abdominal pain, nausea, or
Adverse effects: Peripheral neuropathy
TENOFOVIR ABBRE VIATIONS: The following abbreviations are sometimes used for antiretroviral drugs
(dose-related, see above); pancreatitis; nausea,
vomiting, diarrhoea, constipation, anorexia, Indications: HIV infection in combination with Generic name Most common and preferred abbreviation Alternative abbreviation
abdominal discomfort; chest pain; dyspnoea; other antiretroviral drugs. Abacavir ABC ABV
headache, dizziness, insomnia, mood changes; Precautions: Renal impairment (Appendix 4), Atazanavir ATV ATZ
abnormal dreams, cognitive dysfunction, hepatic disease (see below); pregnancy (see
Darunavir DRV TMC-114, DAR
drowsiness, depression, anxiety; gynaeco- notes above and Appendix 2); breastfeeding
(see notes above). Didanosine ddI DDI, DID
mastia; asthenia, musculoskeletal pain; influ-
Efavifenz EFV EFZ
enza-like symptoms, rash and other allergic HEPATIC DISEASE: Potentially life-threatening
reactions; lymphadenopathy; neoplasms; lactic acidosis and severe hepatomegaly with Emtricitabine FTC ETC, ETB
elevated liver enzymes (see hepatic disease, steatosis reported—caution in patients (par- Enfuvirtide ENF T-20, ENV, EFT
above) and serum amylase; neutropenia, ticularly obese women) with hepatomegaly, Fosamprenavir FPV f-APV, FOS
thrombocytopenia. hepatitis (especially hepatitis C treated with
Indinavir IDV IND
Nursing action: Obtain specimen for C&S test interferon alfa and ribavirin), liver enzyme
Lamivudine 3TC LMV, LAM
before first dose; therapy may begin pending abnormalities, or risk factors for liver disease
test results. and hepatic steatosis (including alcohol abuse); Lopinavir LPV LOP
• Administer 12 hrly around-the-clock preferably 1 discontinue if rapid deterioration in liver func- Maraviroc MVC UK-427, 857, MRV, MAR
hr before meals. tion tests, symptomatic hyper-lactataemia, Nevirapine NVP NEV
• Teach patient that drug does not cure infection progressive hepatomegaly or lactic acidosis.
but symptoms will be controlled; to avoid OTC Raltegravir RAL MK-0518, RTG, RGV, RALT
Exacerbation of hepatitis in patients with
medications unless prescribed. Ritonavir RTV, r✳ RIT
chronic hepatitis B may occur on discontinua-
Dose: HIV infection (in combination with other
tion of tenofovir. Saquinavir SQV SAQ
antiretroviral drugs), by mouth, ADULT
Adverse effects: Nausea, vomiting, abdom- Stavudine d4T STV, D4t
under 60 kg, 30 mg twice daily prefer-
inal pain, flatulence, diarrhoea, anorexia; Tenofovir TDF TNV, TNF
ably at least 1 hour before food; over
hypophosphataemia; dizziness, peripheral
60 kg, 40 mg twice daily; CHILD over Tipranavir TPV PNU-140, 690, TPN
neuropathy, headache, dyspnoea, insomnia,
3 months, under 30 kg, 1 mg/kg twice Zidovudine AZT ZDV
depression, asthenia, sweating, myalgia,
daily; over 30 kg, 30 mg twice daily.
rash, hypertriglyceridaemia, hyperglycaemia, ✳ Preferred option if used at low dose as a pharmacological booster.
490 | 9.5.2.1 Nucleoside reverse transcriptase inhibitors 9.5.2.2 Non-nucleoside reverse transcriptase inhibitors | 491
vomiting occur, notify your doctor. Women of symptomatic hyperlactataemia, progressive hours starting within 12 hours after for efavirenz in pregnant women or women
childbearing age should use effective contra- hepatomegaly or lactic acidosis. birth for up to 1–6 weeks depending for whom effective contraception cannot be
ceptive while on Zalcitabine; take on an empty Adverse effects: Anaemia (may require on national recommendations; by IV assured).
stomach, if possible. transfusion), neutropenia, and leukopenia (all infusion, NEONATE 1.5 mg/kg every 6 Precautions: Chronic hepatitis B or C, hepatic
Nursing action: Recommend the use of wig if more frequent with high dose and advanced hours until oral dosing possible. impairment (avoid if severe; Appendix 5);
hair is lost during treatment. disease); also nausea and vomiting, abdominal POM Zidovudine (WMF 6.4.2.1)
severe renal impairment (Appendix 4); breast-
Dose: Monotherapy, by mouth, Adult, 0.75 pain, dyspepsia, diarrhoea, flatulence, taste Capsules, Zidovudine 100 mg, 250 mg. feeding (see notes above); elderly; history
mg every 8 hours, given together disturbance, pancreatitis, liver disorders in- Tablet, Zidovudine 300 mg. of mental illness or seizures; interactions:
with 200 mg Zidovudine (Total daily cluding fatty change and raised bilirubin and Oral liquid, Zidovudine 50 mg/5 mL. Appendix 1.
dose is 2.25 mg Zalcitabine and 600 liver enzymes (see hepatic disease, above); Solution for IV infusion, Zidovudine 10 mg/mL; in RASH: Rash, usually in the first 2 weeks, is the
mg Zidovudine); if Zalcitabine is dis- chest pain, dyspnoea, cough; influenza-like 20-mL vial.
most common adverse effect; discontinue if
continued due to toxicities decrease symptoms, headache, fever, paraesthesia, neu- POM Zidovudine (EDL 5.11.1.2) severe rash with blistering, desquamation,
Zidovudine dose to 100 mg every 4 ropathy, convulsions, dizziness, somnolence, Capsules, Zidovudine 100 mg, 250 mg. mucosal involvement or fever; if rash mild or
hours. insomnia, anxiety, depression, loss of mental Oral liquid, Zidovudine 50 mg/5 mL. moderate, may continue without interrup-
Note: Safety and efficacy in children less than 13 acuity, malaise, anorexia, asthenia, myopathy,
POM Apo-Zidovudine (Lahams) tion—rash usually resolves within 1 month.
years of age have not been established. Dosage myalgia; pancytopenia, thrombocytopenia; gy- Capsule, Zidovudine 100 mg; white no.3 capsule PSYCHIATRIC DISORDERS: Patients should be
should be adjusted in renal and hepatic impairment. naecomastia; urinary frequency; rash, pruritus, marked ‘APO 100’.
pigmentation of nail, skin and oral mucosa. advised to seek medical attention if severe, de-
POM Zalcitabine (EDL 5.11.1.2) 100 mg – 100.
Tablet, Zalcitabine 750 mcg. Advice to patients: Take 30 minutes before or pression, psychosis or suicidal ideation occur.
POM AVIRO-Z® (Ranbaxy) Adverse effects: Rash including Stevens-John-
POM HIVID® (Swipha) 1 hour after a meal with a glass of water; limit Tablet, Zidovudine 300 mg.
paracetamol containing analgesics; maternal/ son syndrome (see also above); abdominal
Tablets, Zalcitabine 0.375 mg, 0.75 mg; f-c tabs. 300 mg – 60.
EMDEX
foetal transmission may appear in some cases pain, diarrhoea, nausea, vomiting; anxiety,
0.375 mg – 100
0.750 mg – 100 despite therapy. POM RETROVIR® (GSK) depression, dizziness, headache, insomnia,
Capsules, Zidovudine 100 mg, white cap with a somnolence, abnormal dreams, fatigue, im-
Nursing action: Ensure that patient adheres
central dark-blue band marked “Wellcome” “100” paired concentration (administration at bed-
ZIDOVUDINE to the 4 hourly dosage schedule; suggest the and “Y9C”; 250 mg, white/blue cap with a central
use of alarm clock if necessary. time especially in the first 2–4 weeks reduces
Note: The abbreviation AZT which has sometimes been dark-blue band marked “Wellcome”“250” and “H2F.”
• Advise patient that blood transfusion, dosage CNS effects); pruritis; less frequently hepatitis,
used for zidovudine has also been used for another drug. Tablet, Zidovudine 300 mg; white scored f-c tab.
modifications and even drug discontinuation marked “Wellcome X4F”
psychosis, mania, suicidal ideation, amne-
Synonym: Azidothymidine; AZT, ZDV may be needed if blood disorders such as anae- Oral Solution, Zidovudine 50 mg per 5 mL; pale sia, ataxia, convulsions, blurred vision; also
Indications: HIV infection in combination with mia occur. yellow strawberry-flavoured sugar-free solution reported raised serum cholesterol, elevated
at least two other antiretroviral drugs; preven- • Zidovudine is neither a cure for HIV infection nor containing 10 mL oral-dosing syringe. liver enzymes (especially if seropositive for
does it prevent the risk of transmission of HIV to hepatitis B or C), pancreatitis, gynaecomastia,
tion of mother-to-child HIV transmission (see POM VIRAZID® (Swipha)
others. photosensitivity.
also notes above under Pregnancy). Tablet, Zidovudine 100 mg.
Dose: HIV infection (in combination with other Dose: HIV infection (in combination with other
Contra-indications: Abnormally low neutro- Pack: 90’s.
antiretroviral drugs), by mouth, ADULT antiretroviral drugs), by mouth (as tab-
phil counts or haemoglobin (consult product
500–600 mg daily in 2–3 divided POM VIREX-Z® (Fidson) lets or capsules), ADULT and CHILD
literature); neonates either with hyperbili- Tablet, Zidovudine 100 mg; f-c tab.
doses; INFANT under 4 weeks, 4 mg/ 40 kg and over, 600 mg once daily;
rubinaemia requiring treatment other than 100 mg – 3 x 10’s; 60’s.
kg twice daily; CHILD 4 weeks–13 CHILD over 3 years, 10–14 kg, 200 mg
phototherapy or with raised transaminase Syrup, Zidovudine 50 mg per 5 mL.
years 180 mg/m2 twice daily. once daily; 15–19 kg, 250 mg once
(consult product literature). Pack: 100 mL.
Patients temporarily unable to take daily; 20–24 kg, 300 mg once daily;
Precautions: Haematological toxicity; vitamin
zidovudine by mouth, by IV infusion POM XILEX® (Evans)
25–32 kg, 350 mg once daily; 33–39
B12 deficiency (increased risk of neutropenia); Tablet, Zidovudine 300 mg.
over 1 hour, ADULT 1–2 mg/kg every kg, 400 mg once daily; by mouth
reduce dose or interrupt treatment according 300 mg – 60’s.
4 hours (approximating to 1.5–3 mg/ (as oral solution), ADULT and CHILD
to product literature if anaemia or myelo-
kg every 4 hours by mouth) usually 40 kg and over, 720 mg once daily;
suppression; renal impairment (Appendix 4); 9.5.2.2 Non-nucleoside reverse
for not more than 2 weeks; CHILD CHILD over 3 years, 10–15 kg, 270 mg
chronic hepatitis B or C, hepatic impairment transcriptase inhibitors
3 months–12 years, 80–160 mg/m2 once daily; 15–20 kg, 300 mg once
(see below and Appendix 5); risk of lactic
every 6 hours (120 mg/m2 every 6 In some settings it may not be possible to carry daily; 20–24 kg, 360 mg once daily;
acidosis, (see below); elderly; pregnancy and
hours intravenously approximates to out full monitoring described under each drug 25–32 kg, 450 mg once daily; 33–39
breastfeeding (see notes above); interactions:
180 mg/m2 every 6 hours by mouth). entry; in such cases the level of monitoring kg, 510 mg once daily.
Appendix 1.
Prevention of mother-to-child trans- should be determined by local guidelines (see
HEPATIC DISEASE: Potentially life-threatening mission of HIV (see also notes above also notes above). POM Efavirenz (WMF 6.4.2.2)
lactic acidosis and severe hepatomegaly with under Pregnancy), by mouth, ADULT Tablet, Efavirenz 600 mg.
steatosis reported—caution in patients (pat- Capsules, Efavirenz 50 mg, 100 mg, 200 mg
300 mg twice daily from week 28 of EFAVIRENZ
Oral liquid, Efavirenz 150 mg/5 mL.
icularly obese women) with hepatomegaly, pregnancy; at onset of labour 600 Synonym : EFV, EFZ Note: The bioavailability of efavirenz oral solution is
hepatitis, liver enzyme abnormalities, or risk mg (or 300 mg at onset followed by Indications: HIV infection in combination with lower than that of the capsules and tablets; the oral
factors for liver disease and hepatic steatosis 300 mg every 3 hours until delivery); at least two other antiretroviral drugs. solution is not interchangeable with either capsules
(including alcohol abuse); discontinue if after delivery 300 mg twice daily for Contra-indications: Pregnancy (see notes or tablets on a milligram-for-milligram basis.
rapid deterioration in liver function tests, 7 days; NEONATE 4 mg/kg every 12 above and Appendix 2; substitute nevirapine POM Efavirenz (EDL 5.11.1.1)
492 | 9.5.2.2 Non-nucleoside reverse transcriptase inhibitors 9.5.2.3 Protease inhibitors | 493
Tablet, Efavirenz 600 mg. dose cautiously. increase dose cautiously. headache, dizziness, insomnia; myalgia, my-
Capsules, Efavirenz 50 mg, 100 mg, 200 mg. RASH: Rash, usually in first 6 weeks, is most ositis, rhabdomyolysis, fatigue, hypoaesthesia,
POM Nevirapine (WMF 6.4.2.2)
Oral liquid, Efavirenz 150 mg per 5 mL. common side-effect; incidence reduced if paraesthesia; hyperglycaemia; hypersensitivity
Tablet, Nevirapine 200 mg.
POM Efavirenz (Strides Vital) introduced at low dose and dose increased Oral liquid, Nevirapine 50 mg/5 mL. reactions, rash (including Stevens-Johnson
Tablets, Efavirenz 200 mg, 600 mg. gradually, monitor closely for skin reactions syndrome), pruritus, dry skin, hyperpigmenta-
POM Nevirapine (EDL 5.11.1.1)
Pack: 60’s. during first 18 weeks; discontinue permanently tion, alopecia, paronychia; interstital nephritis,
POM EFAZ® (Adler) if severe rash or if rash accompanied by blister- Oral liquid, Nevirapine 50 mg/5 mL. nephrolithiasis (may require interruption or
Tablet, Efavirenz 200 mg ing, oral lesions, conjunctivitis, facial oedema, discontinuation; more frequent in children),
general malaise or hypersensitivity reactions; POM EVADINE® (Evans) dysuria, haematuria, crystalluria, proteinuria,
200 mg – 10 x 10`s.
if rash mild or moderate may continue without pyuria (in children); hepatitis, transient hy-
POM EFCURE® (Fil) 200 mg – 60’s.
Tablet, (200 mg), Efavirenz 200 mg; f-c tab. interruption but dose should not be increased perbilirubinaemia; blood disorders including
until rash resolves. POM NEVIPAN® (Ranbaxy) neutropenia, haemolytic anaemia; lipodystro-
200 mg – 30’s.
Adverse effects: Rash including Stevens-John- Tablet ,Nevirapine 200 mg. phy and metabolic effects, see notes above.
Tablet, (600 mg), Efavirenz 600 mg; f-c tab.
son syndrome and rarely, toxic epidermal necrol- 200 mg – 60. Dose: HIV infection (in combination with nu-
600 mg – 30’s.
ysis (see also above); nausea, hepatitis (see also POM NEVIR® (Fil Pharma) cleoside reverse transcriptase inhibitors
POM POLODIPIN® (Evans)
Hepatic Disease above), headache, less com- Tablet, Nevirapine 200 mg; uncoated tab. and low-dose ritonavir booster), by
Tablet, Efavirenz 600 mg.
monly vomiting, abdominal pain, fatigue, fever, 200 mg – 60’s. mouth, ADULT indinavir 800 mg and
600 mg – 60’s.
and myalgia; rarely diarrhoea, angioedema, POM Nevirapine (Solution Pharma) ritonavir 100 mg both twice daily.
NEVIRAPINE anaphylaxis, hypersensitivity reactions (may Tablet, Nevirapine 200 mg; white to off-white HIV infection (in combination with
Synonym: NVP involve hepatic reactions and rash, see Hepatic scored tab. nucleoside reverse transcriptase inhib-
Disease above); arthralgia, anaemia, and gran- 200 mg – 10`s (in blisters). itors but without ritonavir booster), by
Therapeutic category: Antiviral agent; Nucle-
EMDEX
oside reverse transcriptase inhibitor. ulocytopenia (more frequent in children); very POM Nevirapine (Strides Vital) mouth, ADULT 800 mg every 8 hours;
Indications: HIV infection, in combination rarely neuropsychiatric reactions. Tablet, Nevirapine 200 mg. CHILD and ADOLESCENT 4–17 years,
with at least two other antiretroviral drugs; Nursing action: Obtain specimen for C&S test 200 mg – 60’s. 500 mg/m2 every 8 hours (maxi-
prevention of mother-to-child transmission before first dose; therapy may begin pending mum 800 mg every 8 hours); CHILD
POM VIREX-N® (Fidson)
in HIV-infected patients (see also notes above test results. Tablet, Nevirapine 200 mg; f-c tab. under 4 years, safety and efficacy not
• Administer around-the-clock in equal intervals 200 mg – 3 x 10’s; 60’s. established.
under Pregnancy).
to promote less variation in peak and trough Syrup, Nevirapine 50 mg per 5 mL. Administration: Administer 1 hour before or 2
Contra-indications: Severe hepatic impair- serum levels.
ment; post-exposure prophylaxis. Pack: 100 mL. hours after a meal; may be administered with
• Administer tablet with or without food.
Precautions: Hepatic impairment (see below low-fat, light meal; when given with didano-
• Teach patient that drug does not cure infection
and Appendix 5; chronic hepatitis B or C, high but symptoms will be controlled; to avoid OTC 9.5.2.3 Protease inhibitors sine tablets, allow 1 hour between the drugs
CD4 cell count, and women (all at greater medications unless prescribed. In some settings it may not be possible to carry (antacids in didanosine reduce absorption of
risk of hepatic sideeffects—preferably avoid • Monitor patient for allergic reactions. out full monitoring described under each drug indinavir).
in women with CD4 cell count greater then Dose: HIV infection (in combination with other entry; in such cases the level of monitoring POM Indinavir (WMF 6.4.2.3)
250 cells/mm3 or in men with CD4 cell count antiretroviral drugs), by mouth, ADULT should be determined by local guidelines (see Capsules, Indinavir (as sulfate) 200 mg, 333 mg,
greater than 400 cells/mm3; pregnancy and 200 mg once daily for first 14 days also notes above) 400 mg.
breastfeeding (see notes above); interactions: then (if no rash present) 200 mg twice POM Indinavir (EDL 5.11.1.3)
Appendix 1. daily; INFANT 15–30 days old, 5 mg/ INDINAVIR Capsules, Indinavir (as sulfate) 200 mg, 400 mg
HEPATIC DISEASE: Potentially life-threatening kg once daily for 14 days, then (if no Synonym: IDV
rash present) 120 mg/m2 twice daily POM DENAVIR® (Evans)
hepatotoxicity including fatal fulminant hepa- Indications: HIV infection in combination with Capsule, Indinavir 400 mg.
titis reported usually in the first 6 weeks; close for 14 days, then 200 mg/m2 twice two nucleoside reverse transcriptase inhibitors 400 mg – 60’s.
monitoring required during first 18 weeks; daily; CHILD 1 month–13 years, 120 and usually with low-dose ritonavir booster.
assess liver function before treatment then mg/m2 once daily for first 14 days, POM Indinavir (Strides Vital)
Contra-indications: Porphyria.
then (if no rash present) 120–200 mg/ Capsule, Indinavir sulfate 400 mg.
every 2 weeks for 2 months then after 1 month Precautions: Chronic hepatitis B or C (in- 400 mg – 60’s.
and then regularly; discontinue permanently if m2 twice daily. creased risk of hepatotoxicity), hepatic impair-
liver abnormalities accompanied by hypersen- Prevention of mother-to-child transmis- ment (Appendix 5); ensure adequate hydration LOPINAVIR plus RITONAVIR
sitivity reaction (rash, fever, arthralgia, myalgia, sion of HIV (see also notes above under to reduce risk of nephrolithiasis; patients at risk
Pregnancy), by mouth, ADULT 200 mg Synonym: LPV/r; RTV-LPV
lymphadenopathy, hepatitis, renal impairment, of nephrolithiasis (monitor for nephrolithiasis);
as a single dose at onset of labour; Indications: HIV infection in combination with
eosinophilia, granulocytopenia); suspend if diabetes mellitus (see also Lipodystrophy and
NEONATE 2 mg/kg as a single dose two other antiretroviral drugs.
severe liver abnormalities but no hypersen- Metabolic Effects in notes above); haemophilia;
within 72 hours of birth; if maternal NOTE: Ritonavir increases effect of lopinavir
sitivity reaction—discontinue permanently if pregnancy (see notes above and Appendix 2);
dose given less than 2 hours before (see notes above); low dose in combination
significant liver function abnormalities recur, breastfeeding (see notes above); metabolism
delivery, 2 mg/kg immediately after does not have intrinsic antiviral activity.
monitor patient closely if mild to moderate of many drugs inhibited if administered con-
birth followed by a further dose Precautions: Chronic hepatitis B or C (in-
liver abnormalities with no hypersensitivity comitantly; interactions: Appendix 1.
within 24–72 hours. creased risk of hepatotoxicity), hepatic im-
reaction. Adverse effects: Nausea, vomiting, diarrhoea,
Note: If treatment interrupted for more than 7 days pairment—avoid if severe (Appendix 5);
Note: If treatment interrupted for more than 7 abdominal discomfort, dyspepsia, flatulence,
reintroduce with 200 mg daily (INFANT 15–30 days renal impairment (Appendix 4); haemophilia;
days reintroduce with lowest dose and increase pancreatitis, dry mouth, taste disturbances;
old, 5 mg/kg; CHILD over 1 month, 120 mg/m2) and pregnancy (see notes above and Appendix 2);
494 | 9.5.2.3 Protease inhibitors 9.5.2.3 Protease inhibitors | 495
breastfeeding (see notes above and Appendix appropriate capsules may be used instead of oral Tablet, Nelfinavir 250 mg. SAQUINAVIR
3); diabetes mellitus; oral solution contains solution; oral solution excipients include propylene Synonym: SQV
POM VIRACEPT® (Swipha)
propylene glycol—avoid in hepatic and renal glycol and alcohol 42%.
Tablet, Nelfinavir (as mesylate) 250 mg. Therapeutic category: Antiviral agent; Pro-
impairment, and in pregnancy, increased sus- POM Lopinavir plus Ritonavir (EDL 5.11.1.3) 250 mg – 270. tease Inhibitor.
ceptibility to propylene glycol toxicity in slow Tablet (heat stable), Lopinavir 100 mg, Ritonavir 25 Indications: HIV infection in combination with
metabolizers; concomitant use with drugs that mg; Lopinavir 200 mg, Ritonavir 50 mg. RITONAVIR two other antiretroviral drugs and usually with
prolong QT interval; interactions: Appendix 1. Capsule, Lopinavir 133.3 mg, Ritonavir 33.3 mg.
Synonym: r, RTV low-dose ritonavir booster.
Oral liquid, Lopinavir 400 mg, Ritonavir 100 mg
PANCREATITIS: Signs and symptoms suggestive per 5 mL. Indications: HIV infection, as a booster Contra-indications: Severe hepatic impair-
of pancreatitis (including raised serum amylase to increase effect of indinavir, lopinavir or ment (Appendix 5).
and lipase) should be evaluated—discontinue POM MEDAVIR-LR® (Evans) saquinavir and in combination with two other Precautions: Chronic hepatitis B or C, hepatic
Tablet, Lopinavir 200 mg, ritonavir 50 mg; f-c tabs antiretroviral drugs. impairment (Appendix 5); renal impairment
if pancreatitis diagnosed.
Pack: 120’s
Adverse effects: GI disturbances, anorexia; he- Contra-indications: Severe hepatic impair- (Appendix 4); diabetes mellitus; haemophilia;
patic dysfunction, pancreatitis (see Precautions ment; porphyria pregnancy and breastfeeding (see notes
NELFINAVIR
above); blood disorders (including anaemia, Precautions: Chronic hepatitis B or C (in- above); concomittant use of garlic (reduces
Synonym: NFV creased risk of hepatotoxicity), hepatic im- plasma saquinavir concentration); interac-
neutropenia, and thrombocytopenia), sleep
Therapeutic category: Antiviral agent; Pro- pairment; diabetes mellitus; haemophilia; tions: Appendix 1.
disturbances, fatigue, headache, dizziness,
tease Inhibitor pregnancy and breastfeeding (see notes Adverse effects: Diarrhoea, buccal and
paraesthesia; myalgia, myositis, rhabdo-
Indications: HIV infection in combination with above); interactions: Appendix 1. mucosal ulceration, abdominal discomfort,
myolosis; taste disturbances; rash, pruritis,
two other antiretroviral drugs. nausea, vomiting, taste disturbances; head-
Stevens-Johnson syndrome, hypersensitivity PANCREATITIS: Signs and symptoms suggestive
Precautions: Renal impairment, hepatic im- ache, chest pain, peripheral neuropathy, par-
reactions; lipo-dystophy and metabolic effects of pancreatitis (including raised serum amylase
pairment, chronic hepatitis B or C (increased aesthesia, dizziness, insomnia, mood changes,
(see notes above); electrolyte disturbances and lipase) should be evaluated—discontinue
EMDEX
risk of hepatotoxicity); diabetes mellitus; changes in libido, ataxia, musculoskeletal
in children; less commonly dysphagia, appe- if pancreatitis diagnosed.
haemophilia; pregnancy and breastfeeding disorders, fatigue; hypersensitivity reactions,
tite changes, weight changes, cholecystitis, Adverse effects: Nausea, vomiting, diarrhoea
(see notes above); interactions: Appendix 1. fever, pruritus, rash and other skin eruptions,
hypertension, myocardial infarction, palpita- (may impair absorption—close monitoring
Adverse effects: Diarrhoea, nausea, vomiting, rarely Stevens-Johnson syndrome; other rare
tion, thrombophlebitis, vasculitis, chest pain, required), abdominal pain, taste disturbances,
flatulence, abdominal pain; rash (very rarely adverse effects include thrombocytopenia
oedema, dyspnoea, cough, agitation, anxiety, dyspepsia, anorexia, throat irritation; vasodil-
erythema multiforme); reports of elevated and other blood disorders, liver damage,
amnesia, ataxia, hypertonia, confusion, depres- atation, hypotension, syncope; headache,
creatine kinase, hepatitis, pancreatitis, neu- pancreatitis and nephrolithiasis; reports of
sion, abnormal dreams, extrapyramidal effects, drowsiness; circumoral and peripheral par-
tropenia, hypersensitivity reactions including elevated creatine kinase, raised liver enzymes
neuropathy, influenza-like syndrome, Cushing’s aesthesia, hyperaesthesia, dizziness, sleep
bronchospasm, fever, pruritus and facial and neutropenia when used in combination
syndrome, hypothyroidism, menorrhagia, disturbances, fatigue, rash, hypersensitivity
oedema; myalgia, myositis and rhabdomyol- therapy; lipodystrophy and metabolic effects
sexual dysfunction, breast enlargement, reactions, leukopenia; seizures; raised liver
ysis; lipodystrophy and metabolic effects, see (see notes above).
dehydration, hypercalciuria, lactic acidosis, enzymes, bilirubin, and uric acid; occasionally
notes above.. Advice to patients: Saquinavir is not a cure for
arthralgia, hyperuricaemia, abnormal vision, flatulence, eructation, dry mouth and ulcera-
Nursing action: Obtain specimen for C&S test HIV infection nor does it reduce the transmis-
otitis media, tinnitus, dry mouth, sialadenitis, tion, cough, anxiety, fever, pain, menorrhagia,
before first dose; therapy may begin pending sion of HIV; opportunistic infections and other
mouth ulceration, periodontitis, acne, alopecia, myalgia, myositis, rhabdomyolysis, weight loss,
test results. illnesses associated with AIDS may still occur;
dry skin, sweating, skin discoloration, nail dis- decreased thyroxine, sweating, pruritus, elec-
• Administer tablet with food.
orders, rarely prolonged PR interval. trolyte disturbances, anaemia, neutropenia, take saquinavir within 2 hours after a full meal;
• Discontinue drug therapy and inform the physician
Dose: HIV infection (in combination with other if severe abdominal pain and bleeding occur. increased prothrombin time; pancreatitis (see avoid direct sunlight when taking saquinavir.
antiretroviral drugs), by mouth, ADULT • Teach patient that drug does not cure infection also Pancreatitis, above); lipodystrophy and Nursing action: See under Nelfinavir.
and ADOLESCENT with body surface but symptoms will be controlled; to avoid other metabolic effects, see notes above. Dose: HIV infection (in combination with nu-
area of 1.3 m2 or greater, 3 capsules medications unless prescribed. Dose: HIV infection (as a booster with other cleoside reverse transcriptase inhibitors
or 5 mL twice daily (lopinavir 400 mg • Monitor patient for allergic reactions.
antiretroviral drugs), by mouth, and low-dose ritonavir booster), by
and ritonavir 100 mg twice daily); Dose: HIV infection (in combination with other ADULT 100 mg twice daily; CHILD 6 mouth, ADULT saquinavir 1 g and
CHILD 6 months–13 years, lopinavir antiretroviral drugs), by mouth, ADULT months–13 years 57.5 mg/m2 twice ritonavir 100 mg twice daily.
225 mg/m2 and ritonavir 56.25 mg/ 1.25 g twice daily or 750 mg 3 times daily (or 3–5 mg/kg twice daily) (max- HIV infection (in combination with
m2 twice daily (or body weight 7–15 daily; CHILD under 1 year, 40–50 mg/ imum 100 mg twice daily). other antiretroviral drugs but without
kg lopinavir 12 mg/kg and ritonavir kg 3 times daily or 65–75 mg/kg twice ritonavir booster), by mouth, ADULT
daily; 1–13 years, 55–65 mg/kg twice POM Ritonavir (WMF 6.4.2.3) 1.2 g every 8 hours after a meal;
3 mg/kg twice daily, body weight
daily. Capsule, Ritonavir 100 mg. CHILD under 16 years, safety and
15–40 kg lopinavir 10 mg/kg and Oral solution, Ritonavir 400 mg/5 mL.
ritonavir 2.5 mg/kg twice daily). Administration: Administer with or after food; pow- efficacy not established.
Note: Increase dose by 33% if used with efavirenz der may be mixed with water, milk, formula feeds or POM Ritonavir (EDL 5.11.1.3) Administration: Administer with or after food.
or with nevirapine. pudding; it should not be mixed with acidic foods Solid oral dosage form, Ritonavir 100 mg. Note: To avoid confusion between the different
Administration: Each dose to be taken with food. or juices owing to its taste. Oral liquid, Ritonavir 400 mg/5 mL. formulations of saquinavir, prescribers should
POM Nelfinavir (WMF 6.4.2.3) Note: Limit use to patients weighing >25 kg specify the brand to be dispensed; absorption from
POM Lopinavir plus Ritonavir (WMF 6.4.2.3) gelfilled capsules containing saquinavir is much
Capsules, Lopinavir 133.3 mg and ritonavir 33.3 mg. Tablet, Nelfinavir (as mesilate) 250 mg. POM NORVIR® (Unique)
Oral powder, Nelfinavir 50 mg/g. greater than from capsules containing saquinavir
Oral liquid, Lopinavir 400 mg and ritonavir 100 Capsule, Ritonavir 100 mg; soft elastic cap.
mesilate. Treatment should generally be initiated
mg/5 mL. POM Nelfinavir (EDL 5.11.1.3) 100 mg – 84’s
with gel-filled capsules.
Note: 5 mL oral solution equiv. to 3 capsules; where
496 | 9.5.2.4 Fixed-dose combinations 9.5.2.4 Fixed-dose combinations | 497
POM Squinavir (WMF 6.4.2.3) and Stavudine. POM Stavudine + Lamivudine (Strides Vital) Pack: 60’s.
Capsule, Saquinavir 200 mg. Dose: HIV infection (alone as a complete Tablet, Stavudine 30 mg, Lamivudine 150 mg.
POM COMBIVIR®(GSK)
regimen or in combination with other Pack: 60’s.
POM Squinavir (EDL 5.11.1.3) Tablet, Lamivudine 150 mg, Zidovudine 300 mg;
antiretroviral drugs), by mouth, ADULT Tablet, Stavudine 40 mg, Lamivudine 150 mg.
Capsule, Saquinavir 200 mg. white to off-white f-c tab.
Pack: 60’s.
lamivudine 150 mg and nevirapine
POM FORTOVASE® (Swipha) POM Lamivudine + Zidovudine (Strides Vital)
200 mg and stavudine 30 mg, 1 tablet POM Stavudine + Lamivudine + Nevirapine
Capsule, Saquinavir 200 mg; soft gel capsule. Tablet, Lamivudine 150 mg, Zidovudine 300 mg.
twice daily. (Strides Vital)
200 mg – 180. Pack: 60’s.
Note: A lead-in dose of nevirapine 200 mg once Tablet, Stavudine 30 mg, Lamivudine 150 mg, Nev-
POM INVIRASE® (Swipha) daily for 14 days is recommended for those who irapine 200 mg. POM LAZID® (Fil Pharma)
Capsule, Saquinavir mesylate 200 mg; hard gel cap. have just initiated therapy with nevirapine; the other Pack: 60’s. Tablet, Lamivudine 150 mg, zidovudine 300 mg;
200 mg – 270. drugs should be taken separately during this time. Tablet, Stavudine 40 mg, Lamivudine 150 mg, Nev- f-c tab.
This twice daily fixed-dose tablet can be started if irapine 200 mg. Pack: 60’s.
9.5.2.4 Fixed-dose combinations no rash or liver function test abnormalities present Pack: 60’s.
POM VIREX-LZ® (Fidson)
(see Precautions for nevirapine). If treatment of the POM VIREX-LS30® (Fidson) Tablet, Lamivudine 150 mg, zidovudine 300 mg.
EFAVIRENZ plus EMTRICITABINE fixed-dose tablet is interrupted for more than 7 days Tablet, Lamivudine 150 mg, stavudine 30 mg; Pack: 3 x 10’s; 60’s.
plus TENOFOVIR reintroduce using a lead-in dose of nevirapine 200 lilac-coloured coated tab.
Indications: HIV infection (alone as a complete mg daily and separate tablets for the other drugs. Pack: 3 x 10’s; 60’s. LAMIVUDINE plus NEVIRAPINE
regimen, or in combination with other antiret- POM Lamivudine plus Nevirapine plus Stavudine Dose: For treatment of HIV infections: Adult (weigh- plus ZIDOVUDINE
roviral drugs). (WMF 6.4.2) ing <60 kg), one tablet twice daily.
NOTE: The abbreviation AZT which has sometimes
Contra-indications: Pregnancy (see notes Tablet, Lamivudine 150 mg, Nevirapine 200 mg, POM VIREX-LS40® (Fidson) been used for zidovudine has also been used for an-
above and Efavirenz, Appendix 2). Stavudine 30 mg. Tablet, Lamivudine 150 mg, stavudine 40 mg; cream- other drug.
Precautions: see Efavirenz, Emtricitabine, and POM Lamivudine plus Nevirapine plus Stavudine coloured coated tab.
EMDEX
Tenofovir. Pack: 3 x 10’s; 60’s. Indications: HIV infection (alone as a complete
(EDL 5.11.1.4)
Adverse effects: see Efavirenz, Emtricitabine, Tablet, Lamivudine 30 mg, Nevirapine 50 mg, Dose: For treatment of HIV infections: Adult (weigh- regimen, or in combination with other antiret-
and Tenofovir. Stavudine 6 mg. ing >60 kg), one tablet twice daily. roviral drugs).
Dose: HIV infection (alone as a complete Tablets, (dispersible), Lamivudine 150 mg, Nevi- Precautions: see Lamivudine, Nevirapine, and
POM VIREX-LS30N® (Fidson)
regimen or in combination with rapine 200 mg, Stavudine 30 mg; 60 mg + 100 mg Tablet, Lamivudine 150 mg, stavudine 30 mg, nev- Zidovudine.
other antiretroviral drugs), by mouth,
+ 12 mg. irapine 200 mg. Adverse effects: see Lamivudine, Nevirapine,
ADULT over 18 years, 1 tablet once POM EMTRAL® (Fil) Pack: 3 x 10’s; 60’s. and Zidovudine.
daily. Tablet, (30), Stavudine 30 mg, lamivudine 150 mg, Dose: For treatment of HIV infections: Adult (weigh- Dose: HIV infection (alone as a complete
nevirapine 200 mg; uncoated tab. ing <60 kg), one tablet twice daily. regimen or in combination with
POM Efavirenz plus Emtricitabine plus Tenofovir Pack: 60’s. other antiretroviral drugs), by mouth,
(WMF 6.4.2) POM VIREX-LS40N® (Fidson)
Dose: Adult (<60 kg), 1 tab. twice daily. Tablet, Lamivudine 150 mg, stavudine 40 mg, nev- ADULT 1 tablet twice daily.
Tablet, Efavirenz 600 mg, emtricitabine 200 mg, Tablet, (40), Stavudine 40 mg, lamivudine 150 mg, Note: A lead-in dose of nevirapine 200 mg once
tenofovir 300 mg. irapine 200 mg.
nevirapine 200 mg; uncoated tab. Pack: 3 x 10’s; 60’s. daily for 14 days is recommended for those who
Pack: 60’s. Dose: For treatment of HIV infections: Adult (weigh- have just initiated therapy with nevirapine; the other
EMTRICITABINE plus TENOFOVIR Dose: Adult (>60 kg), 1 tab. twice daily. ing >60 kg), one tablet twice daily. drugs should be taken separately during this time.
Precautions: see Emtricitabine, and Tenofovir. Suspension, Nevirapine 70 mg, lamivudine 40 mg, This twice daily fixed-dose tablet can be started if
Adverse effects: see Emtricitabine, and stavudine 10 mg per 5 mL; 6 g powder for reconsti- no rash or liver function test abnormalities present
LAMIVUDINE plus ZIDOVUDINE
Tenofovir. tution to make 60 mL oral susp. (see Precautions for nevirapine). If treatment of the
Pack: 6g/60 mL. NOTE: The abbreviation AZT which has sometimes fixed-dose tablet is interrupted for more than 7 days
Dose: HIV infection (in combination with
Dose: By mouth, Child (3 months to <8 years), been used for zidovudine has also been used for an- reintroduce using a lead-in dose of nevirapine 200
other antiretroviral drugs), by mouth, according to weight: 7.5-12.5 kg, 5 mL; mg daily and separate tablets for the other drugs.
other drug.
ADULT over 18 years, 1 tablet once 12.5-17.5 kg, 7.5 mL; 17.5-22.5 kg, 10 mL;
daily. 22.5-27.5 kg, 12.5 mL. To be taken twice Indications: HIV infection in combination with POM Lamivudine plus Nevirapine plus Zidovudine
Administration: Tablets can be dispersed in at least daily; shake well before each use. at least one other antiretroviral drug. (WMF 6.4.2)
100 mL water, orange juice or grape juice for patients Precautions: see Lamivudine, and Zidovudine. Tablet, Lamivudine 150 mg, nevirapine 200 mg,
with difficulty swallowing. Directions for reconstitution: Slowly add boiled zidovudine 300 mg.
Adverse effects: see Lamivudine, and Zi-
and cooled water up to the mark on the bottle.
POM Emtricitabine plus Tenofovir (WMF 6.4.2) dovudine. POM Lamivudine plus Nevirapine plus Zidovudine
Shake vigorously. Adjust the volume up to the (EDL 5.11.1.4)
Tablet, Emtricitabine 200 mg, tenofovir 300 mg Dose: HIV infection (in combination with at
mark by adding more water, if necessary. This Tablet, Lamivudine 30 mg, nevirapine 50 mg, zidovu-
least one other antiretroviral drug), by
makes 60ml suspension. The reconstituted dine 60 mg; 150 mg + 200 mg + 300 mg.
LAMIVUDINE plus NEVIRAPINE mouth, ADULT and CHILD over 12
plus STAVUDINE suspension should be used within 15 days of
years, 1 tablet twice daily. POM ARVED-N® (Evans)
Indications: HIV infection (alone as a complete preparation.
Tablet, Lamivudine 150 mg, zidovudine 300 mg,
POM Lamivudine plus Zidovudine (WMF 6.4.2)
regimen, or in combination with other antiret- POM LAVUDINE-S® (Evans) nevirapine 200 mg.
Tablet, Lamivudine 150 mg, zidovudine 300 mg.
roviral drugs). Tablet, Lamivudine 150 mg, stavudine 30/40 mg. Pack: 60’s.
Precautions: see Lamivudine, Nevirapine, and Pack: 60’s. POM Lamivudine plus Zidovudine (EDL 5.11.1.4)
POM VIREX-LZN® (Fidson)
Stavudine; combined preparation not suitable Tablets, Lamivudine 30 mg, zidovudine 60 mg; 150
POM LAVUDINE-SNP® (Evans) Tablet, Lamivudine 150 mg, zidovudine 300 mg,
mg + 300 mg.
for use in children. Tablet, Lamivudine 150 mg, zidovudine 300 mg, nevirapine 200 mg.
Adverse effects: see Lamivudine, Nevirapine, stavudine 30/40 mg. POM ARVED® (Evans) Pack: 3 x 10’s; 60’s.
Pack: 60’s. Tablet, Lamivudine 150 mg, zidovudine 300 mg.
498 | 9.5.3 Other antivirals 9.5.3 Other antivirals | 499
9.5.3 Other antivirals lactation, infants <1 year. sidered. Lassa fever is especially severe late in 10–15 minutes), ADULT initially 33
Haemorrhagic fever virus infection Interactions: Coadministration of probenecid pregnancy, with maternal death or fetal loss mg/kg (maximum 1 g) then 16 mg/
results in an approximate two fold increase in occurring in more than 80% of cases during kg (maximum 1 g) every 6 hours for
Ribavirin (tribavirin) inhibits a variety of exposure to oseltamivir carboxylate due to a the third trimester. 4 days, then 8 mg/kg (maximum 500
DNA and RNA viruses. It is active against viral decrease in active anionic tubular secretion in Precautions: For woman or man, contracep- mg) every 8 hours for 6 days
haemorrhagic fevers caused by the Arenavir- the kidney. However, due to the safety margin tion during and for at least 7 months after
idae and Bunyaviridae family viruses, which POM Ribavirin (WMF 6.4.3)
of oseltamivir carboxylate, no dose adjust- treatment; renal impairment (Appendix 4); Oral solid dosage forms, Ribavirin 200 mg, 400 mg,
include Lassa fever, Argentine haemorrhagic ments are required when coadministering monitor blood counts at least weekly; inter- 600 mg.
fever, Crimean-Congo haemorrhagic fever with probenecid. actions: Appendix 1. Injection for IV administration, Ribavirin 1000 mg and
and haemorrhagic fever with renal syndrome. Adverse effects: Nausea & vomiting; diar- Adverse effects: Haemolytic anaemia, neu- 800 mg in 10-mL phosphate buffer solution.
Treatment of Lassa fever is most effective if rhoea, bronchitis, abdominal pain, dizziness tropenia, thrombocytopenia, aplastic anaemia;
started within 6 days of the onset of fever. and headache. Rarely hypersensitivity reac- myocardial infarction, arrhythmias; infections; SECURININE
Other indications for ribavirin include the tions mainly allergic skin reactions such as nausea, vomiting, diarrhoea, colitis, anorexia, Indications: Inhibitor of viral replication in
treatment of respiratory syncytial virus infec- rash, dermitis, urticaria, eczema, face edema fever, rigors, dyspnoea, cough, dizziness, in- hepatitis A, B, C, D, E. Treatment of acute viral
tion, and with peginterferon alfa or interferon and erythma. somnia, myalgia, arthalgia, fatigue, headache, hepatitis (A, B, C, D, E) or chronic viral hepatitis
alfa for the treatment of chronic hepatitis C Dose: See under preparations below. impaired concentration, irritability, anxiety, (B, C, D) with or without jaundice.
infection (consult manufacturer’s literature for depression, suicidal ideation (more frequent Contra-indications: Absolute: Cirrhosis with
treatment details). POM Oseltamivir (WMF 6.4.3)
Capsules, Oseltamivir 30 mg, 45 mg, 75 mg. in children), autoimmune disorders, pulmonary retention of peritoneal liquid; primitive liver
Oral powder, Oseltamivir 12 mg/mL. toxicity, pancreatitis, diabetes, hypothyroidism, cancer. Relative: do not give toxic liver medi-
OSELTAMIVIR hyperthyroidism, retinal haemorrhage, retinal cine to viral hepatitis patient, notably certain
Pharmacology: Oseltamivir phosphate is a POM TAMOVAN® (Evans)
thrombosis, alopecia, pruritus, rash, rarely antituberculosis drugs and anti-inflammatory
Capsule, Oseltamivir (as phosphate) 75 mg
EMDEX
pro-drug of the active metabolite (oseltamivir hypersensitivity reactions. steroids. The patient must abstain from alco-
carboxylate). The active metabolite inhibits Dose: Treatment of Influenza, Adult and Child (>13 Advice to patients: Oral ribavirin should be holic drinks as well as fatty foods.
influenza A and B neuraminidases in vitro; neu- years), 75 mg twice daily for 5 days. Treat- taken with food. Warnings: Pregnancy and nursing: although
raminidase enzyme is important both for viral ment should begin within 2 days of onset Dose: Haemorrhagic fevers, by mouth, ADULT not toxic to the foetus and the child, there is
entry into uninfected cells and for the release of symptoms of influenza. initially 2 g then 1 g every 6 hours for placenta and maternal milk passage respec-
of recently formed virus particles from infected Prophylaxis of Influenza, Adult and Child 4 days, then 500 mg every 6 hours tively.
cells, and for the further spread of infectious vi- (>13 years), 75 mg once daily for at least 7 for 6 days; CHILD initially 30 mg/kg Adverse effects: May cause gastric pains
rus in the body. Oseltamivir is readily absorbed days. Therapy should begin within 2 days then 15 mg/kg every 6 hours for 4 especially if taken on an empty stomach. The
from the GI tract after oral administration of of exposure.
days, then 7 mg/kg every 6 hours for medicine must be taken after food.
Note: The recommended dose for prophylaxis dur-
oseltamivir phosphate (pro-drug) and is ex- 6 days. Dose: By mouth, Adults and adolescents,
ing a community outbreak of influenza is 75 mg once
tensively converted by predominantly hepatic daily. Safety and efficacy have been demonstrated By slow IV infusion (over 10–15 Acute phase, 3 capsules together
esterases to the active metabolite (oseltamivir for up to 6 weeks. The duration of protection lasts minutes), ADULT initially 17 mg/kg thrice daily for a month.
carboxylate). At least 75 % of an oral dose for as long as dosing is continued. (maximum 1 g) then every 6 hours for Chronic phase: 3 capsules together
reaches the systemic circulation as the active 4 days, then 8 mg/kg (maximum 500 thrice daily for 6 months.
metabolite. Approx. 3% is bound to human RIBAVIRIN mg) every 8 hours for 6 days; CHILD
OTC HEPANTIVIR® (Bolar)
plasma protein. It is eliminated primarily via Synonym: Tribavirin. initially 17 mg/kg then every 6 hours Capsule, Securinine 200 mg
the kidneys and <20% in the faeces. Indications: Treatment of haemorrhagic fever, for 4 days, then 7 mg/kg every 8 200 mg – 60’s (in box)
Indications: Oseltamivir should be used including Lassa fever, Argentine haemorrhagic hours for 6 days Syrup, Securinine 2.5 g per 100 mL.
only in compliance with the WHO treatment fever, and Crimean-Congo haemorrhagic fever; Haemorrhagic fever with renal Pack: 100 mL
guidelines, i.e. (1) for treatment of patients haemorrhagic fever with renal syndrome. syndrome, by slow IV infusion (over
with severe or progressive clinical illness with Contra-indications: Pregnancy (teratogenic
confirmed or suspected influenza pandemic risk; see note below and Precautions); breast-
(H1N1) 2009, (2) for the treatment of patients feeding; severe cardiac disease, including
with confirmed or suspected but uncompli- unstable or uncontrolled cardiac disease in
cated illness due to pandemic influenza virus previous 6 months; haemoglobinopathies
infection who were in higher risk groups, most (including thalassemia or sickle-cell anaemia),
notably for pregnant women and children haemoglobin levels less than 8 g/dl; severe
under 2 years of age. debilitating medical conditions; severe hepatic
Contra-indications: Hypersensitivity to the dysfunction or decompensated cirrhosis of the
oseltamivir. liver; autoimmune disease (including autoim-
Precautions: Initiate treatment not later than mune hepatitis).
40 hours after the appearance of symptoms.
Chronic cardiac disease and/or respiratory PREGNANCY: Risk of serious fetal abnormalities
disease Immunocompromised patients. Im- exists when ribavirin is used during pregnancy,
portant to rule out serious bacterial infections but because of the high risk of mortality from
which may begin with influenza-like symp- haemorrhagic fevers for both pregnant women
toms. Hepatic or renal impairment. Pregnancy, and the fetus, maternal benefit should be con-
10.1 Antidiabetic drugs | 501
10. Endocrine system 10.1 Antidiabetic drugs

10.1.1 Insulins
10.1.2 Oral antidiabetic drugs
10.1.1 Insulins
Appropriate insulin regimens should be
worked out for each patient. Insulin require-
drugs See EMDEX Vol. 3 for the detailed coverage on Man- ments may be affected by variations in lifestyle
agement of Type 2 Diabetes Mellitus in Adults. (diet and exercise)—drugs such as corticoster-
oids, infections, stress, accidental or surgical
See EMDEX Paediatric Drug Guide for the Manage- trauma, puberty and pregnancy (second and
10.1 Antidiabetic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 501 ment of Diabetes in Children & Adolescents, third trimesters) may increase insulin require-
10.1.1 Insulins. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 501 ments; renal or hepatic impairment and some
Diabetes mellitus is characterized by hyperg-
endocrine disorders (for example Addison
10.1.2 Oral antidiabetic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 506 lycaemia and disturbances of carbohydrate, fat
disease, hypopituitarism) or coelic disease
and protein metabolism. There are 2 principal
10.1.2.1 Sulfonylureas. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 507 may reduce requirements. In pregnancy insulin
types of diabetes.
requirements should be monitored frequently.
10.1.2.2 Biguanides. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 510 Type 1 diabetes or insulin-dependent diabetes
Insulin must be given by injection because
10.1.2.3 Thiazolidinediones . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 513 mellitus is due to a defiency of insulin caused
it is inactivated by gastrointestinal enzymes.
by autoimmune destruction of pancreatic beta
10.1.2.4 Dipeptidyl peptidase-4 (DPP-4) inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . 516 Generally, insulin is given by subcutaneous in-
cells. Patients require administration of insulin.
jection into the upper arms, thighs, buttocks, or
10.1.2.5 Alpha glucosidase inhibitors. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 517 Type 2 diabetes or non-insulin dependent abdomen. There may be increased absorption
10.1.2.6 Weight-loss agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 518 diabetes mellitus is due to reduced secretion of from a limb site, if the limb is used in strenuous
insulin or to peripheral resistance to the action exercise following the injection. It is essential to
10.1.3 Diabetes supplies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519
EMDEX
of insulin. Patients may be controlled by diet use only syringes calibrated for the particular
10.2 Thyroid hormones and antithyroid drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519 alone, but often require administration of oral concentration of insulin administered.
antidiabetic drugs or insulin. The energy and
10.2.1 Thyroid hormones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 519 Insulin preparations can be classified accord-
carbohydrate intake must be adequate but
ing to duration of action after subcutaneous
10.2.2 Antithyroid drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 520 obesity should be avoided. In type 2 diabetes,
injection as follows:
obesity is one of the factors associated with • those of short duration which have a relatively
10.3 Corticosteroids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 522 insulin resistance. Diets high in complex carbo- rapid onset of action, for example soluble or
10.4 Sex hormones. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 530 hydrate and fibre and low in fat are beneficial. neutral insulin;
Emphasis should be placed on exercise and • those with an intermediate action, for example
10.4.1 Estrogens (Female sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 530 increased activity. isophane insulin;
10.4.2 Progestogens (Female sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 533 • those with a relatively slow onset and long duration
The aim of treatment is to achieve the best of action, for example protamine zinc insulin.
10.4.3 Androgens (Male sex hormones). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 536 possible control of blood-glucose concentra-
tion and prevent or minimize complications Soluble insulin, when injected subcutane-
10.5 Drugs acting on pituitary ovarian axis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 537 including microvascular complications (retin- ously, has a rapid onset of action (after 30–60
opathy, albuminuria, neuropathy). Diabetes minutes), a peak action between 2 and 4 hours,
10.5.1 Anti-estrogens (Ovulation inducers). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 537
mellitus is a strong risk factor for cardiovascular and a duration of action up to 8 hours. Soluble
10.5.2 Anterior pituitary hormones (Gonadotrophins). . . . . . . . . . . . . . . . . . . . . . . . . 538 disease; other risk factors such as smoking, insulin by the IV route is reserved for urgent
10.5.3 Posterior pituitary hormones . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 541 hypertension, obesity and hyperlipidaemia treatment and fine control in serious illness and
should also be addressed. perioperatively. When injected intravenously,
10.6 Other Endocrine Drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 543 soluble insulin has a very short half-life of
Nursing action: – Antidiabetic medications only about 5 minutes and its effect disappears
• Give insulin after warming to room temp by
rotating in palms to prevent lipodystrophy from
within 30 minutes.
injecting cold insulin. Change to human insulin if When injected subcutaneously, intermedi-
patient is allergic to beef or pork. ate-acting insulins have an onset of action of
• Rotate injection sites when giving insulin within approximately 1–2 hours, a maximal effect at
anyone of these regions: abdomen, upper back, 4–12 hours and a duration of action of 16–24
thighs, upper arm, buttocks. Keep a record of sites.
hours. They can be given twice daily together
• Give oral antidiabetics 30 min before meals.
• Monitor blood and urine glucose levels, fasting with short-acting insulin or once daily, par-
blood sugar, 2 hr PP. ticularly in elderly patients. Most can be mixed
• Advise patient to avoid alcohol and salicylates with soluble insulin in the syringe, essentially
except on doctor’s prescription; to maintain weight retaining properties of each component.
control, dietary restrictions, exercise, hygiene; to go Long-acting insulins have an onset of action
for eye check yearly.
approximately 4 hours after SC injection; peak
• Ensure patient understands symptoms of hypo-
glycaemia namely headache, tremors, fatigue, activity is between 10 and 20 hours, and du-
weakness; and to carry candy or sugar to treat ration of action up to 36 hours. Mixed insulin
hypoglycaemia. zinc suspension can be classified as either
502 | 10.1.1 Insulins 10.1.1 Insulins | 503
intermediate or long-acting. rious hazard especially for drivers and those in be required. Patients whose hypoglycaemia is surgery (oral hypoglycaemic drugs having
The duration of action of different insulin dangerous occupations. Very tight control low- caused by a sulfonylurea should be transferred been omitted).
preparations varies considerably from one pa- ers the blood-glucose concentration needed to to hospital because the hypoglycaemic effects Further information on Insulin
tient to another and this needs to be assessed trigger hypoglycaemic symptoms; increase in of these drugs may persist for many hours.
the frequency of hypoglycaemic episodes re- Insulin is an anabolic hormone in man pro-
for every individual. The type of insulin used DRIVING duced exclusively by the beta-cells of the
and its dose and frequency of administration duces the warning symptoms experienced by
patients. Beta-blockers can also blunt hypogly- Drivers need to be particularly careful to avoid islets of Langerhans in the Pancrease. The
depend on the needs of each patient. For hypoglycaemia. Drivers treated with insulin major effects of insulin are on carbohydrate,
patients with acute onset diabetes mellitus, caemic awareness (and delay recovery). Some
patients report loss of hypoglycaemic warning should normally check their blood-glucose fat and protein metabolism. Insulin reduces
treatment should be started with soluble in- concentration before driving and, on long blood sugar concentration by (a) increasing
sulin given 3 times daily with medium-acting after transfer to human insulin. Clinical studies
do not confirm that human insulin decreases journeys, at intervals of approximately two glucose uptake by peripheral tissues namely
insulin at bedtime. For those less seriously ill, hours; they should ensure that a supply of muscle and fat cells, and (b) reducing hepatic
treatment is usually started with a mixture of hypoglycaemic awareness. If a patient believes
that human insulin is responsible for loss of sugar is always readily available and avoid glucose release through inhibiting glycogen
pre-mixed short– and medium-acting insulins driving if their meal has been delayed. If hy- breakdown (glycogenolysis) and suppressing
(for example 30% soluble insulin with 70% warning it is reasonable to revert to animal
insulin. To restore warning signs, episodes of poglycaemia occurs or warning signs appear, gluconeogenesis, a process in which pyruvate,
isophane insulin) given twice daily. The pro- the driver should stop the vehicle in a safe lactate and amino acids such as alanine are
portions of soluble insulin can be increased hypoglycaemia must be reduced to a mini-
mum; this involves appropriate adjustment of place, ingest a suitable sugar supply and wait converted into glucose.
in patients with excessive post-prandial hy- until recovery is complete (may be 15 minutes
perglycaemia. insulin dose and frequency, and suitable timing Sources of insulin include Pork, beef and
and quantity of meals and snacks. or longer). Driving is particularly hazardous human. Beef insulins are now rarely used. All
Regimens should be developed by each when hypoglycaemic awareness is impaired. insulin preparations are to a greater or lesser
country. For sporadic physical activity, extra carbohy-
drate may need to be taken to avert hypogly- DIABETIC KETOACIDOSIS extent immunogenic in man.
EMDEX
MONITORING caemia. Blood glucose should be monitored Diabetic ketoacidosis is a potentially lethal Insulin is needed by all patients, regardless of
If possible patients should monitor their own before, during and after exercise. condition caused by an absolute or relative lack age, presenting with ketoacidosis, and most of
blood-glucose concentration using blood glu- Initial treatment of mild to moderate hypo- of insulin; it commonly occurs when adjust- those with rapid onset of symptoms: weight
cose strips. Since blood-glucose concentration glycaemia involves glucose 10–20 g given by ments to insulin dosage fail to compensate for loss, weakness and sometimes vomiting often
varies throughout the day, patients should aim mouth either in liquid form or as granulated increases in insulin requirements, for example associated with ketonuria.
to maintain blood-glucose concentration be- sugar (2 teaspoons) or sugar lumps (3 lumps). during severe infection or major intercurrent Almost all children with diabetes require
tween 4 and 9 mmol/litre for most of the time If necessary this may be repeated after 10–15 illness. Diabetes ketoacidosis occurs mostly in insulin therapy. The latter is also needed for
(4–7 mmol/litre before meals and less than 9 minutes. patients with Type 1 diabetes mellitus. It also type 2 diabetes when other methods have
mmol/litre after meals) while accepting that occurs in Type 2 diabetics who have a tempo- failed to achieve good control, and tempo-
on occasions it will be higher; strenuous efforts Hypoglycaemia which causes unconsciousness rary need for insulin. Diabetic ketoacidosis is
is a medical emergency. Glucagon [not in- rarily in the presence of intercurrent illness or
should be made to prevent blood-glucose con- characterized by hyperglycaemia, hyperke- preoperatively. Pregnant women with type 2
centration falling below 4 mmol/litre because cluded on the WHO Model List], a polypeptide tonaemia and acidaemia with dehydration
hormone produced by the alpha cells of the diabetes should be treated with insulin when
of the risk of hypoglycaemia. Patients should and electrolyte disturbances. It is essential diet alone fails.
be advised to look for troughs and peaks of islets of Langerhans, increases plasma-glucose that soluble insulin (and intravenous fluids) is
blood glucose and to adjust their insulin dos- concentration by mobilising glycogen stored readily available for its treatment. Insulin Kinetics: Insulin is destroyed by gas-
age only once or twice a week. Insulin doses are in the liver. In hypogylcaemia, if sugar cannot tro-intestinal enzymes and therefore always
be given by mouth, glucagon can be given INFECTIONS given parenterally. The absorption of Insulin
determined on an individual basis, by gradually
increasing the dose to optimise blood-glucose by injection. Carbohydrates should be given Infections are more likely to develop in patients into the blood stream and, consequently, the
concentration while avoiding hypoglycaemia. as soon as possible to restore liver glycogen; with poorly controlled diabetes mellitus. These onset of hypoglycaemic effect are among other
glucagon is not appropriate for chronic hypo- should be treated promptly and effectively to factors influenced by route of administration
In the absence of blood-glucose monitoring glycaemia. If glucagon is not effective in 10 avoid diabetic ketoacidosis. (IV, IM, SC), site of injection (abdomen, thighs,
strips, urine-glucose monitoring strips can minutes, intravenous glucose should be given. buttocks), ambient temperature, injection
be used; in fact this is the method of personal SURGERY
Alternatively, 50 mL of glucose IV infusion 20% volume (dose), strength of insulin, and indi-
choice for many patients with Type 2 diabetes Particular attention should be paid to insulin vidual patient factors such as reactions at the
mellitus. It is less reliable than blood glucose [not included on WHO Model List] may be requirements when a patient with diabetes
given intravenously into a large vein through injection site.
but is easier and costs much less. All patients undergoes surgery that is likely to need an IV
should monitor either blood– or urine-glucose a large gauge needle; care is required since this infusion of insulin for longer than 12 hours. Method of Administration: Insulin is usually
concentration daily. concentration is irritant especially if extrava- Soluble insulin should be given in IV infusion administered subcutaneously (SC), however, IM
sation occurs. Alternatively, 25 mL of glucose of glucose and potassium chloride (provided or IV administration is possible, e.g. in diabetic
HYPOGLYCAEMIA solution 50% (section 26.2) may be given, but emergencies such as Ketoacidosis or surgery if
the patient is not hyperkalaemic), and adjusted
Hypoglycaemia is a potential complication this higher concentration is more irritant and to provide a blood-glucose concentration of a more rapid effect is wanted.
in all patients treated with insulin or less fre- viscous, which makes administration difficult. between 7 and 12 mmol/litre. The duration of Subcutaneous injection into the abdominal
quently with sulfonylureas. The consequences Glucose intravenous infusion 10% (section action of IV insulin is only a few minutes there- wall ensures a faster absorption than from
of hypoglycaemia include confusion, seizures, 26.2) may also be used but a larger volume fore the infusion must not be stopped unless other regions of the body. Injection into a lifted
coma and cerebral infarction. is needed. Close monitoring is necessary in the patient becomes frankly hypoglycaemic. skin fold minimizes the risk of IM injection.
Loss of warning of hypoglycaemia is common the case of an overdose with a long-acting For non-insulin dependent diabetics, insulin
insulin because further administration may An injection should be followed by a meal
among insulin-treated patients and can be a se- treatment is almost always required during or snack containing carbohydrate within 30
504 | 10.1.1 Insulins 10.1.1 Insulins | 505
minutes. tions used depend on numerous factors which The ability to drive or operate machinery can tions: Appendix 1.
Injection Technique: A volume of air correspond- vary greatly between individuals. Concomitant be impaired during the initial period of insulin Adverse effects: Transient oedema; hypogly-
ing to the prescribed dose of insulin is injected disease, especially if the patient is febrile, usu- therapy, as well as upon change of product, or caemia in overdose; rarely hypersensitivity re-
into the vial. Turn vial and syringe upside down ally increases the patient’s requirement. Blood if the patient is under exceptional physical or actions including urticaria, rash; local reactions
and draw up the prescribed dose of insulin. glucose monitoring is recommended. mental stress and/or unaware of symptoms of and lipoatrophy at injection site.
Remove syringe from vial and expel any air Total daily dose of insulin is 0.6-1 mcg/kg hypoglycaemia. Nursing action: Administer after warming vial
from syringe. Lift up a skin fold and inject the body-weight. 2/3 of total insulin dose is usually Drivers need to be particularly careful to avoid by rotating in palms to prevent lipodystrophy
insulin under the skin. Keep the needle under given in the morning before breakfast and the hypoglycaemia and should be warned of the from injecting cold insulin.
• Use SC route for administration because absorp-
the skin for a few seconds to make sure that all remaining 1/3 in the evening before supper. problems. They should normally check their
tion rate and pain are less than with IM injections.
insulin has been injected. If blood appears after The overall dose is usually adjusted according blood-glucose concentration before driving Press but do not rub site after injection; rotate
withdrawing the needle, press the injected site to response. When short and medium acting and, on long journeys, at intervals of approx- injection site to avoid overuse of one area.
lightly with a finger. insulins are mixed, the ratio of the short to the imately 2 hours. If hypoglycaemia occurs, • Do not interchange insulin sources (human or
Insulin Types/Duration of Action: Insulin prepa- medium is normally 1:3. a driver should switch off the ignition until beef or pork) or insulin brands without physicians
rations are of three types: Most patients are best started on insulin of recovery is complete. approval.
• Short-acting, soluble, regular or neutral insulin. • Teach patient to be able differentiate between
intermediate action twice daily and a short-act- Interactions with other drugs: The following
The effect begins after approximately ½ hour, is symptoms of hypoglycaemia and hyperglycaemia.
ing insulin can be added later to cover any substances may enhance the hypoglycaemic • Advise patient to carry a lump of sugar, crackers
maximal between 1 and 3 hours and terminates hyperglycaemia which may follow breakfast effect of insulin: Non-selective beta-blocking
after approximately 8 hours. biscuit or sweetened chewing gum on hand for
or evening meal. agents, ACE-inhibitors, alcohol, anabolic ster- emergency.
• Intermediate-acting insulin. The effect begins after
approximately 1½-2 ½ hours, is maximal between Insulin requirements may be increased by oids, salicylate, MAOIs. The following drugs • Cigarette smoking decreases insulin absorption;
4 and 5 hours and terminates after approximately infection, stress, accidental or surgical trauma, may increase insulin requirements: Oral con- advise patient not to smoke at least 30 minutes
after taking insulin injection.
EMDEX
24 hours. Examples are Insulin Zinc suspension, puberty and, during the second and third traceptives, thiazides, corticosteroids, thyroid
Isophane insulin. hormones and sympathomimetics. • Insulin requirement increases drastically in preg-
trimesters of pregnancy. nancy and declines during postpartum.
• Long-acting insulin. The effect begins after ap- Storage Conditions: Insulin preparations not in
proximately 4 hours,is maximal between 8 and Requirements may be decreased in patients • Ensure that patient knows that insulin relieves
with renal or hepatic impairment and in those use should be stored in a refrigerator, between symptoms but does not cure disease.
30 hours and terminates after 36 hours. Examples
include Protamine Zinc Insulin (PZI) – rarely used with some endocrine disorders (e.g. Addison’s 2°C and 8°C, at which temperature they will • Instruct patient on how to monitor urine glucose
retain the biological and antimicrobial effect and use of equipment for performing self-moni-
today as they do not offer good control of the disease, hypopituitrism) or coeliac disease.
blood glucose. until the date of expiry printed on the pack. toring of blood glucose.
For intensive insulin regimens, multiple • Store insulin in a cool area; refrigeration is desirable
The duration of action of a particular type of injections (3 to 4 times daily) are usually rec- Insulin stored in a refrigerator must not be but not essential.
insulin varies considerably from one patient to ommended; soluble insulin can also be given stored in or near the freezing compartment. In- • Check expiration date on the vial before using
another and needs to be assessed individually. by continuous subcutaneous infusion using sulin which has been frozen must not be used. the contents.
an infusion pump. Insulin vials may be stored at room tempera- • Instruct patient about the nature of disease; the
Short-acting Insulin is a crystalline zinc-Insulin importance of adhering to therapeutic regimen,
complex dispensed as a clear solution at neu- Warnings and Precautions for use: Insulin is ture (up to 25°C) for up to six weeks after first
adhering to recommended diet, weight reduction,
tral pH. All other commercial insulins have been contra-indicated in hypoglycaemia and in the use but should be protected from excessive exercise and personal hygiene to prevent infection,
modified to provide prolonged action and are presence of insulinoma. Patients should be heat or direct sunlight. Never keep insulin in and timing of injection and eating (meals must
dispensed as turbid suspensions at neutral able to differentiate the warning symptoms an unventilated vehicle that is parked in the not be omitted).
pH with either protamine in phosphate buffer of too low blood glucose (hypoglycaemia) sunlight. Do not place insulin in the same room Dose: Diabetes mellitus, by SC injection, by
(Protamine Zinc and NPH insulin) or varying from those indicating too high blood glucose with dry ice (carbon dioxide). IM injection, by IV injection or by IV
concentrations of Zinc in acetate buffer (ul- (hyperglycaemia). Significant deficiency of Insulin vials in use may be stored in the refrig- infusion, ADULT and CHILD according
tralente, lente, and semilente insulins). insulin may lead to diabetic Ketoacidosis, a fatal erator for three months after first use. to individual requirements.
complication of hyper-glycaemia. An overdose Note: Injection should be followed by a meal within
Colour: Short-acting, soluble, regular or neutral Positioning of Insulin Preparations: Insulin vials 30 minutes of administration.
insulin must be as clear as water, while others of insulin can cause hypoglycaemia with early should be stored horizontally. This is because
are milky and cloudy when properly shaken. symptoms such as cold sweat, fatigue, nausea, the insulin in certain preparations, e.g. suspen- POM Soluble insulin (WMF 18.5)
When drawing, the vial should be gently trembling of hands, hunger and rapid heart Injection, (Solution for injection), Soluble insulin 40
sions, can settle during storage. If this should
beat. Sugar or food rich in carbohydrate can IU/mL in 10-mL vial; 100 IU/mL in 10-mL vial.
shaken or turned upside down ten times to occur while the bottles are stored in an upright
ensure the even dispersal of the active ingre- ameliorate the symptoms at this stage. Severe position, it can be difficult to redisperse the POM Soluble Insulin (EDL 21.2.1)
dients. If particles or undissolved substances hypoglycaemia can result in temporary or insulin uniformly in the liquid. Injection, Short-acting insulin 100 units per mL; in
are formed in the vial, it should not be used. permanent impairment of brain function and 10-mL vial.
death. Diabetics should be advised always to SOLUBLE INSULIN POM BIOSULIN-R® (Fidson)
Mixing of Insulin: When mixing insulin is re-
carry some sugar lumps or biscuits with them. Injection, Soluble human insulin EP 40 units, 100
quired, the soluble portion should be drawn Synonym: Regular insulin; Short-acting insulin.
first into the syringe before the intermedi- Insulin does not pass the placental barrier (safe Indications: Diabetes mellitus; diabetic emer- units per mL; in 10 mL vials.
ate-acting insulin is drawn. The mixture should in pregnancy) and it does not pose any risk to gencies and at surgery; diabetic ketoacidosis POM HUMULIN R® (CHI/Eli Lilly)
be administered immediately most especially the breast-fed baby. Diabetes may become or coma. Injection, Soluble human insulin 100 units per mL;
the Zinc suspensions. more difficult to manage during pregnancy Precautions: see notes above; reduce dose in in 10 mL vial.
and lactation, and hence, closer supervision renal impairment (Appendix 4); pregnancy and POM INSUGEN® R (Zoomota)
Insulin Dosing: The dose, frequency or admin-
is necessary. breastfeeding (Appendices 2 and 3); interac- Injection, (40 IU), Human soluble insulin 40 IU per
istration and combination of insulin formula-
506 | 10.1.2 Oral antidiabetic drugs 10.1.2.1 Sulfonylureas | 507
mL; cloudy white aqueous suspension in 10-mL vial vidual requirements. 10.1.2.3 Thiazolidinediones reactions (disulfiram-like reaction with alco-
with orange cap. Important: IV injection contraindicated. 10.1.2.4 Dipeptidyl peptidase-4 inhibitors hol), endocrine reactions, headache.
Pack: 10 mL vial. 10.1.2.5 Alpha glucosidase inhibitors Nursing action: Administer 30 minutes before
Injection, (100 IU), Human soluble insulin 100 IU per POM Isophane insulin (WMF 18.5) 10.1.2.6 Weight-loss agents
Injection, Isophane insulin 40 IU/mL in 10-mL vial;
meal.
mL; cloudy white aqueous suspension in 10-mL vial Oral antidiabetic (hypoglycaemic) drugs are • Ensure patient understands nature of the disease
with yellow cap. 100 IU/mL in 10-mL vial.
used for non-insulin-dependent diabetes and the importance of following therapeutic reg-
Pack: 10 mL vial. Biosynthetic Human Insulin imen, adhering to specific diet, weight reduction,
mellitus in patients who do not respond to
dietary adjustment and an increase in physical exercise and personal hygiene to prevent infection.
POM BIOSULIN-N® (Fidson)
INSULIN ZINC SUSPENSION • Explain how and when to monitor urinary and
Injection, Human isophane insulin EP 40 units, 100 exercise. They are used to supplement the ef-
Synonym: Insulin zinc suspension (mixed); blood sugar levels.
units per mL; in 10-mL vials. fects of diet and exercise, not to replace them. • Teach patient to differentiate between symptoms
I.Z.S. There are various types of oral antidiabetic
POM HUMULIN N® (CHI/Eli Lilly) of hypoglycaemia and hyperglycaemia.
Indications: Diabetes mellitus. Injection, Human isophane insulin 100 units per mL; agents. The most commonly used are the • Ensure that patient understands that therapy
Contra-indications: IV administration. in 10-mL vial. sulfonylureas and the biguanide, metformin. relieves symptoms but does not cure disease.
Precautions: see notes above; reduce dose in • Evaluate therapeutic response viz decrease in
renal impairment (Appendix 4); pregnancy and POM INSUGEN® N (Zoomota)
Injection, (40 IU), Human isophane insulin 40 IU per 10.1.2.1 Sulfonylureas polyuria, polydipsia, polyphagia.
breastfeeding (Appendices 2 and 3); interac- • Patient needs no transition period should there
mL; cloudy white aqueous suspension in 10-mL vial Sulfonylureas act mainly by augmenting insu-
tions: Appendix 1. with dark green cap.
be need to change to another sulfonylurea anti-
Adverse effects: Hypoglycaemia in overdose; lin secretion and are therefore only effective diabetic agent.
Pack: 10-mL vial. if there is some residual pancreatic beta-cell
rarely hypersensitivity reactions, including • Patient may require hospitalization during transi-
Injection, (100 IU), Human isophane insulin 100 IU
urticaria, rash; local reactions and lipoatrophy activity. They may occasionally lead to hypogly- tion from insulin to oral antidiabetic agent; monitor
per mL; cloudy white aqueous suspension in 10-mL
caemia 4 hours or more after food. This usually patient’s blood sugar.
at injection site. vial with light green cap.
• Tell patient to avoid ingesting alcohol, since
indicates excessive dose and it occurs more
EMDEX
Nursing action: See under Soluble Insulin. Pack: 10-mL vial.
frequently in the elderly and with long-acting headache, light-headedness, and occasional
Dose: Diabetes mellitus, by SC injection, breathlessness may occur.
ADULT and CHILD according to indi- BIPHASIC ISOPHANE INSULIN sulfonylureas such as glibenclamide. The
• Observe for signs of impending renal insufficiency
vidual requirements. Synonym: Biphasic isophane insulin injection. sulfonylureas have the disadvantage that they such as dysuria, anuria, haematuria, and report to
Important: IV injection contraindicated. Indications: Diabetes mellitus (intermediate may encourage weight gain. They should not doctor immediately.
acting). be used during breastfeeding and caution is • Advise patient to avoid taking other drugs without
POM Insulin zinc suspension (WMF 18.5) required in the elderly and those with renal
Contra-indications, Precautions, etc: See clearance from the doctor.
Injection, Insulin zinc (mixed) 40 IU/mL in 10-mL vial;
Isophane insulin above. or hepatic insufficiency because of the risk of • Advise patient to carry sweets to treat mild hy-
100 IU/mL in 10-mL vial.
hypoglycaemia. Insulin therapy is generally re- poglycaemia.
Dose: By SC injection, according to patient’s • Patient on oral antidiabetic therapy may require
POM Insulin Zinc Suspension (EDL 21.2.1) quired during intercurrent illness such as myo-
Injections, Insulin zinc suspension 100 units per mL; requirements. insulin during periods of increased stress, such as
cardial infarction, coma, infection, and trauma,
in 10-mL vial. POM Biphasic Isophane Insulin (EDL 21.2.1) infection, fever, surgery, or trauma.
during surgery and also during pregnancy.
Injection, Mixture of Soluble insulin 30% and Iso- • Elderly patients are particularly prone to the
POM BIOSULIN-L® (Fidson) dangers of hypoglycaemia when long-acting
phane insulin 70% 100 units per mL
Injection, Human insulin zinc suspension EP 40 units, CHLORPROPAMIDE sulfonylureas are used namely Chlorpropamide
100 units per mL; in 10-mL vials. POM BIOSULIN 30/70® (Fidson) Note: Not recommended for use in Nigeria by and Glibenclamide.
POM HUMULIN L® (CHI/Eli Lilly) Injection, Mixture of human soluble insulin (30%) and Diabetes Association of Nigeria. Dose: Initial therapy, 250 mg daily; 100-
human isophane insulin (70%), 40 units, 100 units
Injection, Human insulin zinc suspension 100 units Therapeutic category: Oral hypoglycaemic; 125 mg daily for elderly patients;
per mL; in 10-mL vial. per mL; in 10-mL vials.
Sulfonylurea. increased or decreased according to
POM VINSULIN® L (Fidson) POM HUMULIN 70/30® (CHI/Eli Lilly) Indications: Diabetes mellitus. patient’s response. See lit. for details.
Injection, Insulin Zinc suspension EP 40 IU/mL & Injection, A mixture of highly purified 70% inter- Contra-indications: Hypersensitivity to the
mediate-acting human isophane insulin and 30% POM Apo-Chlorpropamide (Lahams)
100 IU/mL. drug, diabetic ketoacidosis (with or without Tablet, Chlorpropamide 250 mg; white, scored, oval
Pack: 10-mL vial. rapid-acting human soluble insulin, 100 units per
coma), insulin-dependent (juvenile) diabetes f-c tab. marked ‘AP0 250’.
mL; in 10-mL vial.
mellitus. 250 mg – 1000’s.
ISOPHANE INSULIN POM INSUGEN® 30/70 (Zoomota) Precautions: Hypoglycaemia, loss of control
Injection, (40 IU), Mixture of human soluble insulin POM CHLORBINESE® (Neimeth)
Indications: Diabetes mellitus. of blood glucose, pregnancy, breast feeding, Tablet, Chlorpropamide 250 mg
(30%) and human isophane insulin (70%) 40 IU per
Contra-indications: IV administration. elderly, obesity. 250 mg – 20’s; 100’s
mL; cloudy white aqueous suspension in 10-mL
Precautions: see notes above; reduce dose in vial with red cap.
Interactions: NSAIDs such as phenylbuta-
POM DIABINESE® (Pfizer)
renal impairment (Appendix 4); pregnancy and Pack: 10-mL vial. zone; drugs that are highly protein bound
Tablet, Chlorpropamide 250 mg
breastfeeding (Appendices 2 and 3); interac- Injection, (100 IU), Mixture of human soluble insulin like sulphonamides, probenecid, chloram- 250 mg – 20’s; 100’s.
tions: Appendix 1. (30%) and human isophane insulin (70%) 100 IU per phenicol, beta-blockers; drugs that cause
Adverse effects: Hypoglycaemia in overdose; mL; cloudy white aqueous suspension in 10-mL vial hyperglycaemia like diuretics, corticosteroids, POM DIPROMID® (Hovid)
rarely hypersensitivity reactions, including with brown cap. phenothiazines, oral contraceptives, isoniazid, Tablet, Chlorpropamide 250 mg.
Pack: 10-mL vial. 250 mg – 1000’s.
urticaria, rash; local reactions and lipoatrophy sympathomimetics, calcium channel blockers;
at injection site. alcohol.
10.1.2 Oral antidiabetic drugs GLIBENCLAMIDE
Nursing action: See under Soluble Insulin. Adverse effects: Hypoglycaemia, Gl reactions,
Dose: Diabetes mellitus, by SC injection, (e.g cholestatic jaundice rarely, dermatological Synonym: Glyburide
10.1.2.1 Sulphonylureas
ADULT and CHILD according to indi- 10.1.2.2 Biguanides reactions, haematological reactions, metabolic Therapeutic category: Oral hypoglycaemic;
508 | 10.1.2.1 Sulfonylureas 10.1.2.1 Sulfonylureas | 509
Sulfonylurea. 5 mg – 100’s (in blister). GLICLAZIDE only in a minority of patients. A
Indications: Diabetes mellitus. POM DIABETA® (Greenlife) Therapeutic category: Oral Hypoglycaemic maximum of 8 mg per day may not
Contra-indications: Ketoacidosis; porphyria; Tablet, Glibenclamide BP 5 mg. Indications: Type 2 diabetes. be exceeded.
breastfeeding (Appendix 3). 5 mg – 10 x 10’s (in blisters). Contra-indications, Precautions, etc: See To be taken before or with breakfast
Precautions: Pregnancy (Appendix 2); renal under glibenclamide and notes above. or first main meal.
POM DIABETANIL® (Beta Drugs)
impairment (Appendix 4); hepatic impairment Tablet, Glibenclamide 5 mg. Dose: By mouth, 40-320 mg daily depending POM AMARYL® (Sanofi-Aventis)
(Appendix 5); elderly; substitute insulin during 5 mg – 10 x 10’s. on blood glucose response. Tablets, Glimepiride 1 mg, 2 mg, 3 mg, 4 mg
severe infection, trauma, surgery (see notes Doses ≥ 160 mg daily should be taken Pack: 30’s (in blisters)
above); interactions: Appendix 1. POM DIABIFAR® (Neros)
Tablet, Glibenclamide 5 mg. in 2 divided doses and according to POM AZULIX® (Zolon)
Adverse effects: Mild and infrequent, in- the main meals of the day.
5 mg – 10 x 20’s. Tablets, Glimepiride 1 mg, 2 mg; uncoated tabs
cluding GI disturbances and headache; liver 1 mg – 10’s
POM DIATAB® (May & Baker) POM Gliclazide (EDL 21.2.2)
disorders; hypersensitivity reactions usually in 2 mg – 10’s
Tablet, Glibenclamide 5 mg. Tablet, Gliclazide 80 mg
first 6–8 weeks; rarely, erythema multiforme,
5 mg – 3 x 10’s. POM DIAMICRON® MR (Servier Int’l) POM DIAPRIDE® (Micronova)
exfoliative dermatitis, fever and jaundice; hy-
Tablet, Gliclazide 30 mg; modified-release tab. Tablet, Glimepiride 1 mg, 2 mg; uncoated tablet.
poglycaemia, particularly in the elderly; rarely POM GILEMAL® (Sanofi)
Pack: 30’s; 60’s. Pack: 30’s.
blood disorders including leukopenia, throm- Tablet, Glibenclamide 5 mg.
5 mg – 28; 500; 1000. Dose: By mouth, usually 30-120 mg once daily prefer- POM GETRYL® (Zoomota)
bocytopenia, agranulocytosis, pancytopenia,
ably at breakfast time; adjust dose based on Tablet, Glimepiride 1 mg, 2 mg, 3 mg, 4 mg.
haemolytic anaemia, and aplastic anaemia. POM GLABETIX® (Lifeback) response (blood glucose, HbA1c). Pack: 20’s (in blisters).
Advice to patients: Eat regularly, do not skip Tablet, Glibenclamide 5 mg; uncoated tab. Note: To be swallowed whole with half glass of
meals; carry a quick source of sugar. 5 mg – 10 x 10’s water. Administration must always be followed by POM GLEMAX® (Joswe/Afrab)
Nursing action: Patients who are anorexic or a meal. Same dose in elderly patients or those with Tablets, Glimepiride 2 mg, 3 mg, 4 mg, 6 mg.
POM GLEMID®-5 (Reals)
EMDEX
NPO, may need to have their dose held to avoid mild-to-moderate renal failure. Pack: Box of 30 tablets.
Tablet, Glibenclamide BP 5 mg.
hypoglycaemia. 5 mg – 10 x 10’s (in blisters). POM GLEZIDEX® (Vixa) POM GLIMAR® (Taylek)
See also under Chlorpropamide. Tablet, Gliclazide 80 mg. Tablet, (1 mg), Glimepiride 1 mg; pink, scored tab.
POM GLIBEN-J® (Juhel)
Dose: Diabetes mellitus, by mouth, ADULT 80 mg – 60’s. Tablet, (2 mg), Glimepiride 2 mg; green, scored tab.
Caplet, Glibenclamide 5 mg; white scored caplet
initially 5 mg once daily with or Tablet, (3 mg), Glimepiride 3 mg; light yellow,
marked ‘GLI/5’ on one side and ‘Juhel’ on the reverse. POM GLIMICRON® (Hovid)
immediately after breakfast (ELDERLY scored tab.
5 mg – 10 x 10’s (in blister); 500’s (in jars). Tablet, Gliclazide 80 mg; white, uncoated tab. cross
2.5 mg, but avoid—see notes above), Tablet, (4 mg), Glimepiride 4 mg; blue, scored tab.
POM Glibenclamide (Crystal) scored on one side. Pack: 7’s; 10’s; 14’s; 15’s; 28’s; 30’s; 56’s; 60’s; 98’s;
adjusted according to response (max- 80 mg – 10 x 10 (in blister pack); 500’s.
Tablet, Glibenclamide 5 mg; white scored tab. 100’s; 120’s.
imum 15 mg daily). 5 mg – 10 x 10’s POM GLYCINORM® (IPCA) POM GLIMESTAR® (Phillips)
POM Glibenclamide (EDL 21.2.2) Tablets, Gliclazide BP 40 mg, 80 mg. Tablets, Glimepiride 1 mg, 2 mg, 3 mg, 4 mg; un-
POM GLIBENOL® (Afrab-Chem)
Tablet, Glibenclamide 5 mg. 40 mg – 10’s (in blister) coated tabs.
Tablet, Glibenclamide 5 mg; white scored tab.
marked “af”. 80 mg – 10’s (in blister). Pack: 3 x 10’s (in blisters)
POM Glibenclamide (WMF 18.5)
Tablets, Glibenclamide 2.5 mg, 5 mg. POM RECLIDE® (Phillips/Dr. Reddy’s) POM GUPERIDE® (Kayhelt)
POM GLIBEX® (Fidson)
Tablet, Glibenclamide 5 mg; uncoated yellow tab. Tablet, Gliclazide BP 80 mg; uncoated tab. Tablet, Glimepiride 2 mg; uncoated tab
POM Apo-Glyburide (Lahams)
80 mg – 10’s. 2 mg – 10 x 10’s
Tablet, Glibenclamide 5 mg; white, capsule-shaped
POM GLICHIK® (Canopus)
bevel-edged tab. marked ‘APO 5’. POM ZELTINE-MR® (PharmacyPlus) POM HOBETIC® (Hovid)
Tablet, Glibenclamide 5 mg
5 mg – 500’s. Tablet, Gliclazide 30 mg, 60 mg; uncoated modified Tablet, Glimepiride 2 mg; uncoated tab
5 mg – 3 x 10’s
release tab. 2 mg – 3 x 10’s (in blisters)
POM BG NIL® (BG Pharmacy)
POM GLIDANIL® (Salem Gates) Pack: 2 x 14’s (in blisters)
Tablet, Glibenclamide 5 mg. POM MEPIRYL® (May & Baker)
Tablet, Glibenclamide 5 mg; white scored tab.
5 mg – 30’s; 100’s. Tablets, Glimepiride 2 mg, 4 mg.
5 mg – 10 x 10’s; 3 x 10’s GLIMEPIRIDE
POM CIKANIL® (Michelle Lab) 2 mg – 30’s.
POM GLUBEN® (Pemason) Therapeutic category: Oral hypoglycaemic; 4 mg – 30’s.
Caplet, Glibenclamide 5 mg
Tablet, Glibenclamide 5 mg; white tab. Sulfonylurea.
5 mg – 100’s; 10 x 10’s (in blisters) POM MEPRID® (Zolon)
POM GLYBORAL® (Synergy) Indications: Diabetes mellitus.
POM CLADYL® (Chanmedi)) Tablet, Glimepiride 2 mg; uncoated tab
Tablet, Glibenclamide 5 mg. Contra-indications, Precautions, etc.: See
Tablet, Glibenclamide 5 mg. 2 mg – 3 x 10’s
5 mg – 10 x 10’s (in blisters). under Glibenclamide.
5 mg – 10 x 10’s. POM PERGLIM® (Mega Lifesciences)
Dose: By mouth, Adult, initially 1 mg once
POM GLYBETIS® (Diamond Remedies) Tablets, Glimepiride 1 mg, 2 mg; uncoated tabs.
POM CLAMIDE® (Hovid) daily. If necessary, the daily dose can
Tablet, Glibenclamide 5 mg 1 mg – 3 x 10’s; 10 x 10’s.
Tablet, Glibenclamide 5 mg. be raised. It is recommended that the
5 mg – 10’s; 10 x 10’s. 2 mg – 3 x 10’s; 10 x 10’s.
5 mg – 1000’s. increase be guided by regular blood
POM LIBENCLOM® (JB Pharma) POM PERGLIM® (Mega Lifesciences)
POM CLEZIDE® (Vixa) glucose monitoring, and that the
Tablet, Glibenclamide 5 mg Capsule, Glimepiride 3 mg, 4 mg; uncoated tabs.
Tablet, Glibenclamide 5 mg
dose be increased gradually, i.e. at
5 mg – 10 x 10’s intervals of 1-2 weeks and according 3 mg – 3 x 10’s; 10 x 10’s
POM SOLIMIDE® (Solidum) to the following dose steps: 1 mg – 2 4 mg – 3 x 10’s; 10 x 10’s.
POM DAONIL® (Sanofi-Aventis)
Tablet, Glibenclamide 5 mg; scored tab. mg – 3 mg – 4 mg – 6 mg. Daily doses POM ZORYL® (Phillips)
Tablet, Glibenclamide 5 mg; almost white scored
5 mg – 30’s; 100’s Tablets, Glimepiride 1 mg, 2 mg, 4 mg; uncoated tabs.
oblong tab. of more than 6 mg are more effective
510 | 10.1.2.2 Biguanides 10.1.2.2 Biguanides | 511
Pack:10’s (in blisters) Adverse effects: Anorexia, nausea and vom- POM DIABETMIN® (Hovid) Tablet, Metformin (as HCl) 500 mg; white f-c tab.
iting, diarrhoea (usually transient), abdominal Tablet, Metformin (as HCl) 500 mg; f-c tab. 500 mg – 5 x 10’s.
10.1.2.2 Biguanides pain, metallic taste; rarely lactic acidosis (most 500 mg – 1000.
POM GLUMIN® (Seagreen)
likely in patients with renal impairment)—dis- Retard tablet, Metformin HCl 850mg; s-r tab.
Metformin exerts its effect by decreasing Tablet, Metformin 500 mg, 850 mg
850 mg – 10 x 10; 100.
gluconeogenesis and by increasing peripheral continue; decreased vitamin B12 absorption, 500 mg – 6 x 14’s
erythema, pruritus and urticaria; hepatitis POM DIABEX® (Solidum) 850 mg – 4 14’s
utilization of glucose. Metformin can only act
also reported. Tablet, Metformin (as HCI) 500 mg; f-c tab.
in the presence of endogenous insulin there- 500 mg – 30’s; 100’s
POM GLYCOMET® (Synergy)
fore is effective only in diabetics with some Nursing action: Ensure patient understands Tablets, Metformin HCl BP 500 mg, 850 mg.
residual functioning pancreatic islet cells. It the disease and its treatment. POM DIABEX® XL (Solidum) Pack: 10 x 10’s (in blisters).
• Administer with food to decrease GI irritation. Tablet, Metformin HCI 1000 mg; f-c extended-re-
is used as a first-line treatment in overweight POM GUAMET® (Medreich)
• Warn patient to avoid excessive alcohol consump- lease tab.
non-insulin-dependent diabetic patients and tion to prevent excessive elevation of blood lactate. Tablet, Metformin (as HCl) 500 mg; white f-c tab.
1000 mg – 30’s, 100’s
in others when strict dieting and sulfonylureas • Discontinue therapy and report to doctor imme- 500 mg – 30’s; 100’s; 500’s.
have failed to control the disease. GI adverse diately if vomiting occurs; may be due to lactic POM DIAMET® (May & Baker)
POM JUFORMIN® (Juhel)
effects are common on initial treatment and acidosis potentially fatal complication of biguanide Tablet, Metformin (as HCl) 500 mg.
Tablet, Metformin 500 mg.
may persist, particularly when very high doses therapy. 500 mg – 84’s.
500 mg – 100’s.
(such as 3 g daily) are given. In order to reduce Dose: Diabetes mellitus, by mouth, ADULT POM DIAMIN® (Korlyns)
POM LIZOPHAGE® (Standard Generics)
GI effects, treatment should be initiated with and CHILD over 10 years initially Tablet, Metformin (as HCl) 500 mg; f-c tab.
Tablet, Metformin (as HCl) 500 mg
a low dose which may be gradually increased. 500 mg with breakfast for at least 1 500 mg – 10 x 10’s (in blisters)
500 mg – 5 x10’s (in blister)
Metformin may provoke lactic acidosis which week then 500 mg with breakfast POM DEGLUCO® (Kayhelt)
is most likely to occur in patients with renal and evening meal for at least 1 week, POM LOFIN® (Fidson)
Tablet, Metformin HCI 500 mg; f-c tab
Tablets, Metformin (as HCl) 500 mg, 850 mg; f-c tabs.
impairment; it should not be used in patients then 500 mg with breakfast, lunch 500 mg – 3 x 10’s; 10 x 10’s (in blisters)
EMDEX
with even mild renal impairment. One major and evening meal or 850 mg every 12 POM FORBETIC® (Swipha)
POM MEFOXIMIN® (Salem Gates)
advantage of metformin is that it does not usu- hours with or after food; usual maxi- Tablet, Metformin 500 mg; f-c tab.
Tablet, Metformin HCl 500 mg; f-c tab.
ally cause hypoglycaemia. It may be used with mum 2 g daily in divided doses. 500 mg – 10’s (in blisters); 5 x 10’s; 500’s (in jar)
500 mg – 30’s.
insulin (but weight gain and hypoglycaemia POM Metformin (WMF 18.5) POM MEPHAGE® (Pharmabase)
POM FORMET® (Strides Vital)
can be problems—weight gain minimised if Tablet, Metformin HCl 500 mg. Tablet, Metformin (as HCI) 500 mg; uncoated tab.
Tablet, Metformin 500 mg.
insulin given at night) or sulfonylureas ( pos- Pack: 3 x 10’s.
500 mg – 6 x 10’s; 500’s.
sibility of increased adverse effects with such POM Metformin (EDL 21.2.2)
Tablet, Metformin HCl 500 mg. POM MEPHAGE® SR (Adler)
combinations remains unconfirmed). During POM FORMINEC® (JB Pharma)
Tablet, Metformin 1000 mg
POM ASKAPHAGE® (Diamond Remedies) Tablet, Metformin (as HCI) 500 mg; f-c tabs
medical and surgical emergencies insulin 1000 mg – 30’s
Tablet, Metformin 500 mg 500 mg – 10 x 10’s (in blister)
treatment is almost always required; insulin
500 mg – 14’s (in blister); 500’s (in jar) POM METFORCAP® (Laider)
should be substituted for metformin before POM GAUZOPHAGE® (Gauze)
Tablet, Metformin (as HCl) 500 mg; oblong off-
elective surgery and in pregnancy. POM AUROMET® (Rohi) Tablet, Metformin HCI 500 mg
white tab.
Tablet, Metformin HCI 500 mg 500 mg – 5 x 10’s
METFORMIN 500 mg – 100’s POM GLAVAMET® SR (Evans)
POM Metformin (Afrab-Chem)
Therapeutic category: Oral hypoglycaemic; POM BETAFORM® (Greenlife) Tablets, Metformin (as HCl) 500 mg, 1000 mg; un-
Tablet, Metformin HCl 500 mg
Biguanide. Tablet, Metformin (as HCI) 500 mg; f-c tab. coated extended-release tabs.
500 mg – 30’s
Indications: Diabetes mellitus (see notes 500 mg – 10 x 10’s. 500 mg – 10’s (in blister)
1000 mg – 10’s (in blister) POM Metformin (Crystal)
above). POM BETAPHAGE® (Beta Drugs) Tablet, Metformin HCI 500 mg; uncoated tab.
Contra-indications: Renal impairment (Ap- Tablet, Metformin HCl 500 mg. POM GLUCOPAC® (Pacmai)
pendix 4); ketoacidosis; withdraw if tissue 500 mg – 10 x 10’s. Tablet, Metformin HCI 500 mg
hypoxia likely (for example sepsis, respiratory 500 mg – 5 x 10’s (in blisters) POM Metformin (Kakaki)
POM BG LOPHAGE® (BG Pharmacy) Tablet, Metformin 500 mg
failure, recent myocardial infarction, hepatic Tablet, Metformin (as HCl) 500 mg; white f-c tab. POM GLUCONROM® SR (Zolon)
500 mg – 28’s; 500’s
impairment), use of iodine-containing X-ray 500 mg – 14’s (in blister) Tablet, Metformin HCI 500 mg, 1000 mg; uncoated
contrast media (do not restart metformin until s-r tab POM Metformin (Lifeback)
renal function returns to normal) and use of POM CIKAFORMIN® (Michelle Lab) Tablet, Metformin HCI 500 mg
Tablet, Metformin HCI 500 mg POM GLUCOPHAGE® (Biofem)
general anaesthesia (suspend on the morning 500 mg – 14’s
500 mg – 100’s; 10 x 10’s (in blisters) Tablets, Metformin HCl 500 mg, 850 mg; white f-c
of surgery and restart when renal function tabs. POM Metformin (Miraflash)
returns to normal); alcohol dependence; preg- POM CLAMET® (Pharmgate) 500 mg – 84’s Tablets, Metformin HCl 500 mg, 850 mg.
nancy (Appendix 2). Tablet, Metformin 500 mg. 850 mg – 30’s.
500 mg – 3 x 10’s. POM Metformin (Novartis)
Precautions: Determine renal function before POM GLUDIAB® (Al-Tinez) Tablet, Metformin HCl 500 mg; round, white, double
treatment and once or twice annually (more POM CHANFORMIN® (Chanmedi) Tablet, Metformin HCI 500 mg; f-c tab radius f-c tab.
frequently in the elderly or if deterioration Tablet, Metformin 500 mg. 500 mg – 5 x 10’s (in blisters) 500 mg – 28’s; 30’s; 50’s; 56’s; 60’s; 84’s; 90’s; 100’s;
suspected); substitute insulin during severe 500 mg – 1 x 500’s. 120’s; 180’s; 250’s; 270’s (in blisters)
POM GLUFORMIN® (NGC)
infection, trauma, surgery (see notes above and POM DIABETESE® (Therapeutic) Tablet, Metformin HCl 850 mg; white, oval f-c tab.
Tablet, Metformin HCl 500 mg
contraindications); breast-feeding (Appendix Tablet, Metformin HCI 500 mg. 850 mg – 20’s; 28’s; 30’s; 40’s; 50’s; 56’s; 60’s; 84’s; 90’s;
500 mg – 10 x 10’s
3); interactions: Appendix 1. 500 mg – 10 x 10’s (in blisters). 100’s; 120’s; 180’s; 250’s; 300’s (in blisters)
POM GLUFORT® (E-Globa)
512 | 10.1.2.2 Biguanides 10.1.2.3 Thiazolidinediones | 513
POM Metformin (Phillips) Tablet, Metformin HCI 500 mg, glibenclamide 5.0 POM AMARYL M® (Sanofi-Aventis) POM ZORYL-M® (Phillips)
Tablet (500 mg), Metformin HCI 500 mg; white f-c mg; f-c tab Tablet, (1/250 mg), Glimepiride 1 mg, Metformin Tablet, Glimepiride 1 mg, Metformin HCI 500 mg; f-c
tab. marked ‘A’ on one side and ‘60 on the reverse. Pack:15’s (in blisters) 250 mg; f-c tab. extended-release tab.
500 mg – 14’s (in blisters). Pack: 3 x 10’s (in blister) Pack: 10’s (in blisters).
POM METCON® SR (Barata)
Tablet (850 mg), Metformin HCI 850 mg; white f-c TabletTablet (2/500 mg), Glimepiride 2 mg, Metformin Tablet, Glimepiride 2 mg, Metformin HCI 500 mg; f-c
Tablet, Metformin HCI 500 mg, glibenclamide 2.5
tab. marked ‘A’ on one side and ‘61’ on the reverse. 500 mg; f-c tab. extended-release tab.
mg; f-c tab
850 mg – 14’s (in blisters) Pack: 3 x 10’s (in blister) Pack: 10’s (in blisters).
Pack:14’s (in blisters)
Tablet (1000 mg), Metformin HCI 500 mg; white
POM AQUAFORMIN® (Pinnacle)
oval, scored f-c tab. marked ‘62’ on one side and ‘A’ POM MET-GLIM® (Hovid) 10.1.2.3 Thiazolidinediones
Tablet, Glimepiride 1 mg, Metformin 500 mg; f-c
on the reverse. Tablet, Glibenclamide 5 mg, metformin HCI 500
sustained release tab. Rosiglitazone and Pioglitazone belong to the
1000 mg – 10’s (in blisters). mg; f-c tab
Pack: 30’s thiazolidinedione (or glitazone) class of anti-
POM METCON-G® (Barata) Tablet, Glimepiride 2 mg, Metformin 500 mg; f-c
diabetic agents. They reduce blood-glucose
Tablet, Metformin HCI 500 mg; uncoated extended POM METKEN® (Canopus) sustained release tab.
release tab Pack: 30’s
concentration by increasing insulin sensitivity
Tablet, Metformin 500 mg
500 mg – 15’s (in blisters) 500 mg – 10 x 10’s
in muscle and adipose tissue, and inhibiting
POM AZULIX MF® (Zolon) hepatic gluconeogenesis. By increasing the
POM MIFORMIN® (Didachons) POM QVEXYL® 2.5 (Salem Gates) Tablet , (1 mg/500 mg), Metformin HCl [in s-r form] insulin sensitivity in the periphery, they en-
Tablet, Metformin HCI 500 mg. Tablet, Metformin HCI 500 mg; Glibenclamide 2.5 500 mg, Glimepiride 1 mg.
hance glucose uptake in muscle. They improve
mg. Tablet, (2 mg/500 mg), Metformin HCl [in s-r form]
POM PANFOR SR® (Mega Lifesciences)
500 mg, Glimepiride 2 mg.
glycaemic control while reducing circulating
Tablets, Metformin (as HCl) 500 mg, 1000 mg; un- insulin levels; pioglitazone may have more
Dose: To be taken once daily with full meal pref-
coated s-r tabs. POM QVEXYL® 5 (Salem Gates) +ve lipid effect.
erably in the evening. Tablet should be
500 mg – 10 x 10’s. Tablet, Metformin HCI 500 mg; Glibenclamide 5 mg. swallowed whole. Do not crush or chew.
1000 mg – 10 x 10’s. Pack: 3 x 10’s (in blisters)
EMDEX
By mouth, Adult, start one tablet (1 mg/500 PIOGLITAZONE
POM RANOPHAGE OD® (Ranbaxy) mg) daily; may increase dose depending Pharmacology: Pioglitazone is an insulin
Tablet, Metformin HCl 500 mg; extended-release tab. METFORMIN plus GLIMEPIRIDE upon the glycemic control to 2 tablets sensitizer; it improves insulin sensitivity in
500 mg – Box of 30’s. Pharmacoloy: Glimepiride lowers blood once daily. Alternatively, may start with one
insulin-resistant patients without stimulating
glucose primarily by stimulating the release tablet (2 mg/500 mg) daily; may increase to
POM VPL Metformin (Vixa) 2 tablets once daily depending on response insulin release from pancreatic beta cells, thus
Tablet, Metformin 500 mg of insulin from functioning pancreatic beta avoiding the risk of hypoglycemia. It appears to
and blood sugar level.
500 mg – 10 x 10’s cells. Metformin is an antihyperglycemic agent act via activation of specific nuclear receptors
Patient Information: Counsel patient that they may
which improves sugar tolerance in patients (PPAR-gamma or peroxisome proliferator ac-
POM WATFORM® (Watson) pass empty matrix “ghost” (tablets) in the stool. It
with type 2 diabetes by lowering both basal should be of no concern as the active medication tivated receptor gamma) leading to increased
Tablet, Metformin 500 mg; white tab.
and post-prandial plasma glucose. It decreases has already been absorbed. insulin sensitivity of liver, fat and skeletal
POM ZOOMETF® (Zoomota) hepatic glucose production, decreases intesti-
Tablet, Metformin (as HCl) 500 mg; f-c tab. POM CO-MEPIRYL® (May & Baker) muscle cells in animals. Treatment with pio-
nal absorption of glucose, and improves insulin glitazone has been shown to reduce hepatic
500 mg – 6 x 14’s (in blister) Tablet, Glimepiride 2 mg, Metformin HCI 500 mg;
sensitivity by increasing the peripheral glucose uncoated bilayered tablet. output of glucose and to increase peripheral
uptake and utilization. Unlike sulfonylureas, Pack: 3 x 10’s (in blisters) insulin uptake. Improved glycaemic control is
METFORMIN plus GLIBENCLAMIDE
Metformin does not cause hypoglycemia. The Dose:Adult, by mouth, initially 1 tablet once daily; associated with a reduction in both fasting and
POM BENIMET® (Solidum) combination of sulphonylurea and biguanide adjust based on response and tolerance. postprandial plasma insulin concentrations in
Tablet, Metformin HCI 500 mg, glibenclamide 5 has additive action. Max. 4 tablets/day.
type 2 diabetes.
mg; f-c tab. Glimepiride is completely absorbed from the POM DIAPRIDE® Plus (Micronova) Following oral administration, pioglitazone
Pack: 30’s GI tract after oral administration reaching Tablet, Glimepiride 1 mg, Metformin HCl 500 mg; is rapidly absorbed with C max of 2 hours.
POM CLABETIC® (Swipha) maximum plasma concentration after about s-r tab. Absorption is not influenced by food intake.
Tablet, Glibenclamide 5 mg, Metformin HCl 500 mg. 2-3 hours. The oral bioavailability of Metformin Pack: 30’s. Absolute bioavailability is greater than 80%.
Pack: 30’s. is about 50-60% and 30% of it is excreted via Tablet, Glimepiride 2 mg, Metformin HCl 500 mg;
It undergoes extensive hepatic metabolism
feces. Decrease in oral administration could s-r tab.
POM GLUCOVANCE® (Biofem)
Pack: 30’s. predominantly via CYP 2C8. It is eliminated
Tablet, Metformin HCl 500 mg, glibenclamide 2.5 be due to first pass metabolism. Concomitant mainly in the feces and lesser amounts in urine.
mg; white f-c tab marked ‘2.5 mg’. food intake may slightly impair the absorption. POM RANOPHAGE G® (Ranbaxy) Indications: As an adjunct to diet and exercise
Pack: 30’s. Following a single oral dose of Metformin HCl Tablet ,(1 mg/500 mg) Glimepiride 1 mg, metformin to improve glycemic control in type 2 diabetes
Tablet, Metformin HCl 500 mg, Glibenclamide 5 mg; SR, Cmax is achieved within 4 to 6 hours. HCI (in s-r form) 500 mg; bilayered tab.
inadequately controlled with metformin or
white f-c tab marked ‘5 mg’. Indications: Type 2 diabetes mellitus when Pack: 10’s (in blisters)
Pack: 30’s. Tablet , (2 mg/500 mg) Glimepiride 1 mg, metformin sulfonylurea; may be used as monotherapy or
diet, exercise and single agent do not result in in combination with metformin, sulfonylurea,
HCI (in s-r form) 500 mg; bilayered tab.
POM METCLAMIDE® (Mark) adequate glycemic control. or insulin.
Tablet, Meformin HCI 500 mg, glibenclamide 5 Contra-indications, Precautions, etc: see Contra-indications: Hypersensitivity to
mg; f-c tab under Glibenclamide and Metformin. POM PERGLIM-M® (Mega Lifesciences)
Table, Glimepiride 1 mg, Metformin HCl 500 mg;
pioglitazone; cardiac failure or history of
Pack: 10 x 3’s; 10 x 10’s Dose: According to individual patient’s need,
s-r tab. cardiac failure (NYHA stages I to IV); hepatic
POM METAGLOMIDE® (Vixa) usually once or twice daily. impairment or ALT levels >2.5 times the ULN;
Pack: 20’s (in blister)
Tablet, Metformin 500 mg, glibenclamide 5 mg Administer with food (either imme- diabetic ketoacidosis.
Table, Glimepiride 2 mg, Metformin HCl 500 mg;
500 mg – 3 x 10’s. diately before or together with food). s-r tab. Precautions: Fluid retention which may exac-
POM METCON-G®-5 (Barata) See below. Pack: 20’s (in blister) erbate or precipitate heart failure; co-admin-
514 | 10.1.2.3 Thiazolidinediones 10.1.2.3 Thiazolidinediones | 515
istration with insulin (increased risk of edema Tablets, Pioglitazone (as HCl) 15 mg, 30 mg, 45 mg Starting dose should be based on pregnancy may be increased (ensure adequate
& HF); elderly >75 years; perform LFT before 15 mg – 14’s patient’s current dosage regimen of contraception is used); thiazolidinediones
initiating treatment & periodically afterwards 30 mg – 15’s pioglitazone and/or metformin. can cause fluid retention/oedema which can
(avoid if ALT levels >2.5 X ULN or any evidence 45 mg – 14’s For patients who are inadequately exacerbate or lead to CHF; may cause weight
of liver disease); weight gain; macular edema POM TARGLIT® (Zolon) controlled on metformin monotherapy, gain which probably involves a combination
with decreased visual acuity; increased risk Tablet, Pioglitazone (as HCI) 15 mg, 30 mg; un- may be started on pioglitazone/met- of fluid retention and fat accumulation; avoid
of fractures in women; hypoglycemia (in coated tab. formin 15 mg/500 mg or 15 mg/850 use if patient shows clinical evidence of active
combination therapy with sulfonylurea or in- 15 mg – 3 x 10’s mg 1-2 times daily; adjust dose grad- liver disease or increased serum transaminase
30 mg – 3 x 10’s
sulin); resumption of ovulation in anovulatory ually based on therapeutic response. levels; pregnancy and lactation.
premenopausal women with PCOS (due to en- POM ZOLITAL® (PharmacyPlus) For patients who are on pioglitazone Interactions: Rosiglitazone is predominantly
hanced insulin action); anemia (small reduction Tablets, Pioglitazone 15 mg, 30 mg. monotherapy and needs additional metabolized by CYP2C8, and to a lesser extent,
in Hgb & Hct) consistent with hemodilution; 15 mg – 2 x 14’s (in blisters) glycaemic control, may be started on 2C9. Co-administration with CYP2C8 inhibitors
pregnancy, lactation. 30 mg – 2 x 14’s (in blisters). pioglitazone/metformin 15 mg/500 may cause inceased rosiglitazone plasma
Interactions: CYP 2C8 inhibitors e.g. Gemfibro- mg twice daily or 15 mg/850 mg once concentration while the inducers may produce
zil increase blood levels of pioglitazone while PIOGLITAZONE plus GLIMEPIRIDE daily; adjust dose gradually based on opposite effect (close monitoring of glycaemic
the inducers e.g. Rifampicin cause decreased Indications: Type 2 diabetes mellitus. therapeutic response. control and rosiglitazone dose adjustment may
blood levels. Cholestyramine decrease absorp- Contra-indications, Precautions, etc.: See be needed).
POM NILGAR M® (Megalife sciences)
tion of pioglitazone. under Pioglitazone and Glimepiride. Adverse effects: Oedema, anaemia, hy-
Tablet, Pioglitazone (as HCl) 15 mg, metformin
Adverse effects: Visual disturbance; upper Dose: Dosage should be individualised (as HCl) 500 mg; white & orange coloured ob- per-cholesterolaemia, weight gain, hypogly-
respiratory tract infection; weight gain; hypo- based on patient’s response and long-shaped tab. caemia, CHF/pulmonary oedema, cardiac
aesthesia; anaemia; edema. tolerance. Starting dose should be Pack: 5 x 20’s (in blister) ischaemia; hepatic dysfunction evidenced
EMDEX
Dose: To be taken orally once daily with or based on patient’s current dosage Tablet, Pioglitazone HCl 30 mg, metformin HCl 500 primarily by elevated hepatic enzymes.
without food. regimen of pioglitazone and/or mg; white & blue coloured oblong-shaped tab. Advice to patients: May be taken with or with-
Adult (>18 years), initially 15-30 mg sulfonylurea. Inappropriate dose may Pack: 5 x 20’s (in blister) out meals. Inform patient that management of
once daily; may increase up to a max. cause hypoglycemia. A single dose POM PIONORM-M® (Micronova) of type 2 diabetes should include diet control.
45 mg once daily. should be taken once daily with the Tablet, Pioglitazone (as HCI) 15 mg, Metformin (as Caloric restriction, weight loss, and exercise
Combination therapy with Met- first main meal. HCI) 500 mg; sustained release tab. are essential for the proper treatment of the
formin, Sulfonylurea or Insulin: 15-30 For patients who are inadequately Pack: 30’s. diabetic patient becauses they help improve
mg once daily. controlled on glimepiride monother- Tablet, Pioglitazone (as HCI) 30 mg, Metformin (as insulin sensitivity. This is important not only
apy, may be started on pioglitazone/ HCI) 500 mg; sustained relesease tab.
Elderly: No dosage adjustment is in the primary treatment of type 2 diabetes,
glimepiride 15 mg/2 mg, 30 mg/2 Pack: 30’s.
necessary. but also in maintaining the efficacy of drug
Child (<18 years): not recommended. mg or 30 mg/4 mg once daily; adjust POM PIOZER® Plus (CG Biostadt) therapy. Instruct patient to adhere to the diet
dose gradually to desired response. Tablet, (15/500), Pioglitazone (as HCl) 15 mg, Met- and to regularly check blood glucose and
(Additional information sourced from Actos monograph: http://
For patients who are inadequately formin (as HCl) 500 mg; f-c tab.
www.medicines.org.uk/) Hgb levels; it can take up to 2 weeks to see a
controlled on pioglitazone monother- Pack: 14’s
Tablet, (15/850), Pioglitazone (as HCl) 15 mg, Met-
reduction in blood glucose and 2-3 months to
POM ACTOVISTA® (Vatican Bells) apy, may be started on pioglitazone/ see full effect. Advise patient to report imme-
formin (as HCl) 850 mg; f-c tab.
Tablet, Pioglitazone 30 mg glimepiride 15 mg/2 mg or 30 mg/2 diately any unexplained symptoms of nausea,
Pack: 14’s
30 mg – 20’s mg once daily; adjust dose gradually vomiting, abdominal pain, fatigue, anorexia, or
to desired response. POM TARGLIT-M® (Zolon)
POM DIAVISTA® (Phillips/Dr. Reddy’s) dark urine. Patient should also be told to report
Tablet, Pioglitazone HCI 15 mg, metformin HCI (in s-r
Tablets, Pioglitazone (as HCl) 15 mg, 30 mg; un- POM PIOZER-G® (CG Biostadt) unusually rapid increase in weight or oedema,
form) 500 mg; uncoated bilayered tab.
coated tabs. Tablet (15/2), Pioglitazone 15 mg, glimepiride 2 mg or shortness of breath or other symptoms of
Pack: 3 x 10’s
15 mg – 10’s (in blister). Pack: 10’s heart failure. Explain to patient that rosigli-
30 mg – 10’s (in blister). Tablet (30/2), Pioglitazone 30 mg, glimepiride 2 mg ROSIGLITAZONE tazone when used alone or in combination
POM GLITTER® (Zoomota) Pack: 14’s with other hypoglycaemic agents can cause
Tablets, Pioglitazone 15 mg, 30 mg; white tabs. Tablet (30/4), Pioglitazone 30 mg, glimepiride 4 mg Note: Diabetes Association of Nigeria recommends hypoglycaemia; teach patient the symptoms,
15 mg – 10 x 10’s (in blisters) Pack: 14’s discontinuation of the clinical use of Rosiglitazone
treatment and predisposing factors. Ensure
30 mg – 10 x 10’s (in blisters) especially in patients with underlying cardiac problems.
adequate contraception is used as therapy
PIOGLITAZONE plus METFORMIN
POM PIONORM® (Micronova) Indications: Type 2 diabetes mellitus. may result in ovulation in some premenopausal
Tablet,s Pioglitazone (as HCI) 15 mg, 30 mg; un- Indications: Type 2 diabetes mellitus. Contra-indications: History of hypersensitivity anovulatory women with increased risk for
coated tab. Contra-indications, Precautions, etc.: See to rosiglitazone or any other ingredient of the pregnancy.
15 mg – 30’s. under Pioglitazone and Metformin. preparation. Dose: The management of antidiabetic
30 mg – 30’s. Dose: Dosage should be individualised Precautions: Rosiglitazone is active only in therapy should be individualised.
POM PIOTAZONE® (Evans) based on patient’s response and the presence of endogenous insulin (avoid Periodic fasting blood glucose meas-
Tablets, Pioglitazone (as HCl) 15 mg, 30 mg; un- tolerance but not exceeding max. use in patients with type 1 diabetes for the urements should be performed to
coated tabs. daily dose of Pioglitazone 45 mg and treatment of diabetic ketoacidosis); may cause monitor therapeutic response prior to
15 mg – 10’s (in blister) Metformin 2550 mg. To be given in resumption of ovulation in premenopausal up-titrating dose. To be given with or
30 mg – 10’s (blister) divided daily doses with meals to anovulatory women with insulin resistance and without food.
POM PIOZER® (CG Biostadt) reduce GI upset. as a result of improved insulin sensitivity, risk of Monotherapy: Start 4 mg as a single
516 | 10.1.2.4 Dipeptidyl peptidase-4 (DPP-4) inhibitors 10.1.2.5 Alpha glucosidase inhibitors | 517
dose once daily or in divided doses formin 1000 mg; f-c tab. vildagliptin enhances the sensitivity of β cells Note: The 50 mg dose should be administered
twice daily; may be increased to 8 Dose: May be taken with or without food. Food to glucose, resulting in more glucose-appro- once daily in the morning. The 100 mg dose
mg as a single dose once daily or may reduce GI symptoms associated with priate glucagon secretion. The reduction in should be administered as two divided doses
in divided doses twice daily if FPG metformin. Starting with low dose and inappropriate glucagon during meals in turn of 50 mg given in the morning and evening.
slowly increasing the dose may reduce GI
(fasting plasma glucose) shows inad- attenuates insulin resistance. The enhanced Patients with hepatic or renal impairment: Not
side effects due to Metformin (Start low
equate response following 12 weeks & go slow). increase in the insulin/glucagon ratio during recommended in patients with hepatic impair-
of treatment. As Initial Therapy: Start 2 mg/500 mg 1-2 hyperglycaemia due to increased incretin ment including patients with a pre-treatment
Combination therapy with Metformin: times daily; may use upper range particu- hormone levels results in a decrease in fasting ALT or AST >2.5X ULN. No dosage adjustment
Start 4 mg as a single dose once daily larly for patients with HbA1c >11% or FPG and postprandial hepatic glucose production, in patients with mild renal impairment. Not
or in divided doses twice daily; may >270 mg/dL. leading to reduced glycaemia. recommended in patients with moderate or
be increased to 8 mg/day following As Second-Line Therapy: 1) For patients The known effect of increased GLP-1 levels to severe renal impairment or End stage renal
12 weeks of therapy if there is insuffi- inadequately controlled on Metformin delay gastric emptying is not observed with disease (ESRD) on haemodialysis.
monotherapy: Initially, 4 mg Rosiglitazone
cient reduction in FPG. vildagliptin treatment. In addition, a reduction Elderly: No dosage adjustments required. Pae-
(total daily dose) plus the dose of Metformin
Combination therapy with Sulfony- already being taken.
in postprandial lipaemia that is not associated diatric patients: Not recommended for use in
lurea: Start 4 mg as a single dose once 2) For patients inadequately controlled with vildagliptin’s incretin mediated effect to patients under 18 years of age.
daily or in divided doses twice daily; on Rosiglitazone monotherapy: Initially, improve islet function has been observed. POM GALVUS® (Novartis)
may be increased to 8 mg/day 8 to 1000 mg Metformin (total daily dose) plus Vildagliptin is weight neutral. Tablet, Vildagliptin 50 mg; white to light yellow tab.
12 weeks after initiation of therapy if the dose of Rosiglitazone already being Vildagliptin has an absolute bioavailability of marked ‘NVR’ on one side and ‘FB’ on reverse.
there is insufficient reduction in FPG. taken. 85%. Food slightly delays absorption but the 50 mg – 28’s
Combination therapy with Insulin: Start Child: Not recommended for child <18 effect is clinically insignificant. About 69%
4 mg as a single dose once daily or in years of age. of oral dose is metabolized by hydrolysis to VILDAGLIPTIN plus METFORMIN
EMDEX
Elderly: May reduce dose due to the poten-
divided doses twice daily; may reduce inactive products; DPP-4 contributes partially
tial for decreased renal function. POM GALVUS Met® (Novartis)
insulin dose by 10-25% if patient Hepatic impairment: In mild hepatic im- to the hydrolysis. Cytochrome P-450 enzymes
Tablet, (50/500 mg), Vildagliptin 50 mg, Metformin
reports hypoglycaemia or if FPG con- pairment (Child-Pugh A, scores <6) no dose play no significant role in the metabolism. Ap- (as HCl) 500 mg; light yellow f-c tab marked ‘NVR’ on
cns decreased to <100 mg/dl. Futher adjustment of rosiglitazone is required. prox. 85% (23% unchnaged drug) of the dose one side and ‘LLO’ on reverse.
adjustments should be individualised However, as hepatic impairment is a risk is excreted in urine and 15% in faeces. Half-life Pack: 56’s
based on glucose-lowering response. factor for lactic acidosis with metformin, is approx. 3 hours. Tablet, (50/850 mg), Vildagliptin 50 mg, Metformin
Oral triple combination therapy with avoid use in patients with functional hepatic Indications: As an adjunct to diet and exercise (as HCl) 850 mg; yellow f-c tab. marked ‘NVR’ on one
Meformin and a Sulfonylurea: Start 4 impairment. to improve glycaemic control in adults with side and ‘SEH’ on reverse.
mg as a single dose once daily or in type 2 diabetes mellitus; as monotherapy Pack: 56’s
divided doses twice daily; may cau- 10.1.2.4 Dipeptidyl peptidase-4 and in dual combination with metformin, a Tablet, (50/1000 mg), Vildagliptin 50 mg, Metformin
tiously adjust dose up to 8 mg/day 8 (DPP-4) inhibitors sulphonyurea (SU), a thiazolidinedione (TZD)
(as HCl) 1000 mg; dark yellow f-c tab. marked ‘NVR’
on one side and ‘FLO’ on reverse.
to 12 weeks after initiation of therapy or insulin when diet, exercise and a single Pack: 56’s
if FPG is inadequately controlled. VILDAGLIPTIN antidiabetic agent do not result in adequate Indications: As an adjunct to diet and exercise to
Maximum recommended dose: 8 mg as Therapeutic category: Oral hypoglycaemic glycaemic control. improve glycaemic control in patients with type 2
a single dose once daily or in divided agent; Dipeptidyl peptidase-4 (DPP-4) inhibitor Contra-indications: Hypersensitivity to diabetes mellitus whose diabetes is not adequately
doses twice daily. (aka Incretin enhancer or Gliptin). vildagliptin or to any of the excipients. controlled on Metformin or Vildagliptin alone or
Note: No dosage adjustments are required in Pharmacology: Vildagliptin, a member of the Precautions: Not a substitute for insulin in who are already treated with the combination of
erderly, renal impairment (avoid combination with islet enhancer class, is a potent and selective insulin-requiring patients. Not recommended Vildagliptin and Metformin, as separate tablets.
Metformin). Not recommended for children under dipeptidyl-peptidase-4 (DPP-4) inhibitor that Dose: To be individualized based on response and
for patients with type 1 diabetes or for the
18 years. improves glycaemic control. In patients with tolerance as well as on the patient’s current
treatment of diabetic ketoacidosis. Renal and regimen of Vildagliptin and/or Metformin.
POM AVANDIA® (GSK) type 2 diabetes, administration of vildagliptin hepatic impairment. Monitor liver enzymes. Do not exceed the maximum daily dose of
Tablet, Rosiglitazone 4 mg. led to inhibition of DPP-4 enzyme activity for a Discontinue therapy if jaundice or other signs Vildagiptin (100 mg). Administer with meals
24-hr period resulting in increased fasting and of hepatic dysfunction occur. Contains lactose. to reduce the GI side effects associated with
ROSIGLITAZONE plus METFORMIN postprandial endogenous levels of the incretin Interactions: Vildagliptin is not a substrate nor Metformin.
Therapeutic category: Oral antidiabetic hormones namely glucagon-like peptide 1 does it inhibit nor induce CYP450 enzymes,
agent; Thiazolidinedione; Biguanide. (GLP-1) and glucose-dependent insulinotropic and is therefore not likely to interact with 10.1.2.5 Alpha glucosidase inhibitors
Indications: Type 2 diabetes mellitus. polypeptide (GIP). co-medications that are substrates, inhibitors
Contra-indications, Precautions, etc: see By increasing the endogenous levels of these or inducers of these enzymes. ACARBOSE
under Rosiglitazone and Metformin above. incretin hormones, vildagliptin enhances the Adverse effects: As monotherapy, these side Therapeutic category: Antidiabetic agent,
Dose: see under the proprietary preparations sensitivity of β cells to glucose resulting in im- effects are usually mild and transient and most alpha glucosidase inhibitor.
below. proved glucose-dependent insulin secretion. are uncommon namely dizziness, headache, Pharmacology: Acarbose is a competitive
The degree of improvement in β-cell function is constipation, hypoglycaemia, arthralgia. Rarely inhibitor of intestinal alpha-glucosidases with
POM AVANDAMET® (GSK)
Tablet,(2 mg/500 mg) Rosiglitazone 2 mg, metformin
dependent on the initial degree of impairment; hepatic dysfunction including hepatitis (mon- maximum specific inhibitory activity against
500 mg; f-c tab. in nondiabetic (normal glycaemic) individuals, itor liver function). sucrase. The digestion of starch and sucrose
Tablet, (2 mg/1000 mg) Rosiglitazone 2 mg, met- vildagliptin does not stimulate insulin secre- Dose: Adult, by mouth, 50-100 mg daily for into absorbable monosaccharides in the
formin 1000 mg; f-c tab. tion or reduce glucose levels. monotherapy and in dual combina- small intestine is delayed and this results in
Tablet, (4 mg/1000 mg), Rosiglitazone 2 mg, met- By increasing endogenous GLP-1 levels, tion with metformin, a TZD or insulin.
518 | 10.1.2.6 Weight-loss agents 10.1.3 Diabetes supplies | 519
a lowering of postprandial hyperglycaemia 10.1.2.6 Weight-loss agents Capsule, Orlistat 120 mg. may create a state of hyperinsulinism.
and a smoothing effect on fluctuations in the 120 mg – 84 (in blisters). Dose: Suck or chew 1 – 2 tablets several
daily blood glucose profile. Unlike sulphon- ORLISTAT times daily. To be administered orally.
ylureas acarbose has no stimulatory action Therapeutic category: Anti-obesity agent. 10.1.3 Diabetes supplies OTC GLUCOTAB® (Goldmoore)
on the pancreas. It also reduces fasting blood Pharmacology: Orlistat is the hydrated form OTC DISPOVAN® U100 (Zoomota) Chewable tablet, D-glucose 3.4 g, excipients q.s.
glucose and has a modest effect on the HA1c. of a naturally occuring molecule (lipstatin). The Insulin syringe/needle, Disposable syringe with 30G Flavour: Orange.
Following oral administration, only 1-2% of hydration leads to an improved stability profile. needle. Indication: Hypoglycemia.
acarbose is absorbed; the bulk of it is elimi- It is a potent reversible inhibitor of gastric and Pack: 10 x 10’s Dose: Suck or chew 1-2 tablets several times daily.
nated in the faeces. pancreatic lipases, which acts locally in the OTC GlucoDr® (Zoomota) OTC IDIL® (E-Globa)
Indications: Treatment of non-insulin de- GIT lumen and inhibits the cleavage of triglyc- Blood glucose test strips, Each strip contains Glucose Powder, Glucose anhydrous 20 g, Sodium chloride
pendent diabetes mellitus (NIDDM) in patients erides. It therefore prevents the absorption dehydrogenase, potassium ferricyanide, immobi- 3.5 g, Sodium citrate 2.9 g, Potassium chloride 1.5 g.
inadequately controlled on diet alone, or on of up to 30% of ingested dietary fat. The fat is lized & sterile. Pack: 3 x 27.9 g
diet and oral hypoglycaemic agents. excreted in the faeces, producing hypocaloric Pack: 2 x 25’s
OTC IMPULSE® (Crowther)
Contra-indications: Hypersensitivity to Disposable lancet, Contain 3 beveled sterile lancets
state and weight loss almost exclusively by the Energy boost drink
acarbose, pregnancy, lactation; Inflammatory 28 G for single use only.
reduction of visceral and subcutaneous fat. The Pack: 200’s
bowel disease, colonic ulceration, partial intes- OTC Victor Super (Crowther)
efficacy of orlistat depends on the presence of Tablet, Glucose
tinal obstruction or predisposition to intestinal dietary fat, which is why it should be taken with Storage and Handling of Test Strips
Pack: 25 x 6’s
obstruction; Chronic intestinal diseases asso- • Store the package at temperatures between 1oC
meals. Cessation of treatment leads rapidly to
ciated with marked disorders of digestion or – 32oC (34oF – 90oF). Avoid direct sunlight and OTC Vita Glucose D (Vitahealth)
a normalization of fat absorption. excessive humidity.
absorption; Conditions which may deteriorate Energy drink, Glucose (Dextrose monohydrate)
Indications: For long term weight control • Always close the vial with the cap immediately 99.4%, minerals (TCP & DCP) vitamin D
as a result of increased gas formation in the in- (Weight loss, Weight maintenance, Prevention after removing a test strip. If the test strip vial is
EMDEX
Pack: 50 g
testine, e.g. larger hernias. Hepatic impairment; of weight regain) when used in conjunction left open for a long period of time, test strips will
Severe renal impairment. Children (<18 years). with a moderately hypocaloric diet in obese become unusable. OTC VITERGIN® (Taylek)
Precautions: May potentiate the hypoglycae- • Use the test strip immediately after removing it Tablet, Glucose.
patients with a body mass index (BMI, pa-
mic effects of insulin and sulphonylurea drugs. from the vial. Pack: 50 x 6’s.
tient’s body-weight divided by the square of
Acarbose delays digestion and absorption of patient’s height) greater or equal to 30 kg/m2 • Use all the strips within 4 months after the first
disaccharides e.g. sucrose (patients should opening. 10.2 Thyroid hormones and
or over weight patients (BMI >28 kg/m2) with
use glucose for hypoglycaemia). Monitor liver • Store your test strips only in their original vial; do antithyroid drugs
associated risk such as diabetes, hypertension not transfer them to a new bottle or any other
enzymes during the first 6-12 months of ther- and dislipidaemia. 10.2.1 Thyroid hormones
container.
apy; discontinue if transaminases are elevated. In type 2 diabetic patients who are overweight • Do not handle the strip with wet hands.
10.2.2 Antithyroid drugs
Interactions: Intestinal adsorbents (e.g. (BMI >28 kg/m2) or obese BMI >30 kg/m2, Orl- • Do not bend, cut or alter a test strip in any way
charcoal) and digestive enzymes preps (e.g. istat in conjuction with a mildly hypocaloric 10.2.1 Thyroid hormones
amylase, pancreeatin) may reduce its effect. diet provides additional glycaemic control ORAL GLUCOSE Thyroid agents are natural or synthetic agents
Cholestyramine may enhance its postprandial when used in combination with other antidi- containing levothyroxine (thyroxine) or lio-
insulin reducing effect. Sucrose containing OTC ALLENBURYS’ GLUCOSE D® (Evans)
abetic agents. thyronine (tri-iodothyronine). The principal
foods may increase abdominal discomfort. Powder, Calcium Glycerophosphate 7mg, Vitamin D
Contra-indications: Chronic malasoption 19 IU, Dextrose Monohydrate 15g per 15 g. effect is to increase the metabolic rate. They
Adverse effects: Flatulence, diarrhoea, ab- syndromes, cholestasis and in patients with also exert a cardiostimulatory effect which may
Pack: 15 g; 50 g (in sachet) 175 g; 400 g (in tin)
dominal pains, N & V, dyspepsia, increase in known hypersensitivity to orlistat or any of the be the result of a direct action on the heart.
liver enzymes. other components of the capsule. OTC ENERGIN® (Fidson)
Dose: By mouth, Adult, initially 50 mg 1-2 Tablet, (Chewable), Dextrose Monohydrate, Starch, Thyroid hormones are used in hypothyroid-
Adverse effects: Abdominal pain/discomfort, ism (myxoedema) and also in diffuse non-toxic
times daily; increased to 3 times Citric acid, Pineapple, Flavour, Orange flavour,
flatulence, liquid stools, soft stools, rectal pain/ Magnesium stearate. goitre, Hashimoto thyroiditis (lymphadenoid
daily depending on response and discomfort. The incidence of these side effects Indications: In hypoglycemic state, for fast relief goitre) and thyroid carcinoma. Neonatal hy-
tolerance. If no response after 6-8 inceases the higher the fat content of the diet from low blood glucose level. Energin is an easily
weeks, may increase further to a max. pothyroidism requires prompt treatment for
and thus faeces. assimilable source of instant energy. Glucose, a
normal development.
100-200 mg 3 times daily. Dose: By mouth, 120 mg capsule with each monosaccharide, is administered by mouth or by IV
Administration: Should be chewed with the first meal; to be taken immediately before, infusion in the treatment of carbohydrate and fluid Levothyroxine sodium (thyroxine sodium) is
mouthful of food, or swallowed whole with a little depletion. It is administered orally in Glucose Toler- the treatment of choice for maintenance ther-
during or up to one hour after the
liquid directly before the meal. Owing to the great ance Test as a diagnostic aid for diabetes mellitus. apy. It is almost completely absorbed from the
individual variation of glucosidase activity in the
meal.
Contra-indications: Glucose-galactose malabsorption GI tract but the full effects are not seen for up
Note: The patient should be on nutritionally bal-
intestinal mucosa, there is no fixed dosage regimen, syndrome. Diabetic coma while blood glucose levels are
anced, mildly hypocaloric diet. to 1 to 3 weeks after beginning therapy; there
and patients should be treated according to clinical excessively high.
response and tolerance of intestinal side-effects. A is a slow response to dose change and effects
POM ECOSLIM® (Micronova) Adverse effects: A high dose of dextrose given by
gradual dose escalation is favoured to minimise GI Capsule, Orlistat 120 mg. mouth may cause nausea and vomiting. Hyper-
may persist for several weeks after withdrawal.
side effects. Pack: 30’s. phosphatemia may follow after prolonged use. Oral Dosage of levothyroxine in infants and children
contraceptive may compound the effect of well- for congenital hypothyroidism and juvenile
POM GLUCOBAY® (Bayer Schering) POM ORLIS® (Biostadt)
known risk factors, such as hypertension, diabetes, myxoedema should be titrated according
Tablets, Acarbose 50 mg, 100 mg. Capsule, Orlistat 120 mg.
50 mg – 5 x 15’s hyperlipidemias, age and obesity. In particular some to clinical response, growth assessment and
100 mg – 5 x 15’s progestogens are known to decrease HDL choles- measurement of plasma thyroxine and thy-
POM XENICAL® (Swipha) terol and cause glucose intolerance, while estrogen roid-stimulating hormone.
520 | 10.2.2 Antithyroid drugs 10.2.2 Antithyroid drugs | 521
LEVOTHYROXINE SODIUM Tablets, Levothyroxine (as Sodium salt) 0.05 mg, breast-feeding. nausea and vomiting occur.
Synonym: Thyroxine sodium. 0.1 mg. Precautions: Pregnancy; signs of blood disor- Nursing action: Improve taste of drug (has
Indications: Hypothyroidism. POM EUTHROX® (Biofem) der such as sore throat, fever or rashes. very salty taste) by diluting with water, milk or
Contra-indications: Thyrotoxicosis. Tablets, Levothyroxine sodium 25 ug, 50 ug, 150 Adverse effects: Rashes, nausea, headache, juice; give with meals to minimize GI distress;
Precautions: Cardiovascular disorders (myo- ug; tabs marked ‘EM/25’, ‘EM/50’, ‘EM/150’ on one GI upset, blood disorders, arthralgia, alopecia, give with a straw to prevent tooth discol-
cardial insufficiency or MI); hypopituitarism or side respectively. hepatitis, psychotic reactions. ouration; give at the same time each day to
Pack: 100’s. Advice to patients: Notify physician immedi- maintain blood level.
predisposition to adrenal insufficiency (must
be corrected by corticosteroid prior to initial ately of symptoms of blood disorders viz sore • Encourage patient to take adequate fluids.
levothyroxine); elderly; longstanding hypothy- 10.2.2 Antithyroid drugs throat, mouth ulcers, bruising, fever, malaise, • Advise patient not to discontinue drug abruptly to
or non-specific illness. prevent thyroid crisis.
roidism, diabetes insipidus, diabetes mellitus Antithyroid drugs such as propylthiouracil
Dose: By mouth, usually 20-60 mg daily for Dose: By mouth, 0.1-0.3 mL 3 times daily well
(may need to increase dose of insulin or oral and carbimazole are used in the management
4-8 weeks; then reduced gradually to diluted with water or milk.
antidiabetic drug); pregnancy (Appendix 2), of thyrotoxicosis. They are also used to pre-
breastfeeding (Appendix 3); interactions: pare the patient for thyroidectomy. They are 5-15 mg daily for about 18 months. POM Iodine plus Potassium Iodide (EDL 21.6.1)
Appendix 1. usually well-tolerated, with mild leukopenia Child: initially 15 mg daily, adjusted Oral liquid, Iodine 5%, potassium iodide 10% in
Adverse effects: (usually with excessive dose) or rashes developing in a few percent of cases, according to response. purified water.
anginal pain, arrhythmias, palpitations, tach- usually during the first 6–8 weeks of therapy. POM Carbimazole (EDL 21.6.1)
ycardia, skeletal muscle cramps, diarrhoea, During this time the blood count should be PROPYLTHIOURACIL
Tablet, Carbimazole 5 mg.
vomiting, tremors, restlessness, excitability, checked every 2 weeks or if a sore throat or Synonym: PTU.
POM CARBIROID® (Hovid) Indications: Hyperthyroidism.
insomnia, headache, flushing, sweating, ex- other signs of infection develop. The drugs Tablet, Carbimazole 5 mg.
cessive loss of weight and muscular weakness. are generally given in a high dose in the first Precautions: Large goitre; pregnancy and
5 mg – 1000.
Advice to patients: Do not change brands instance until the patient becomes euthyroid, breastfeeding (see also notes; Appendices
EMDEX
without physicians knowledge; report imme- the dose may then be gradually reduced to POTASSIUM IODIDE 2 and 3); hepatic impairment (Appendix
diately to physician any chest pain, increased a maintenance dose which is continued for 5)—withdraw treatment if hepatic function
Indications: Thyrotoxicosis (pre-operative
pulse, palpitations, heat intolerance, excessive 12–18 months, followed by monitoring to deteriorates (fatal reactions reported); renal
treatment); sporotrichosis, subcutaneous
sweating; do not discontinue without notifying identify relapse. There is a lag time of some 2 impairment—reduce dosage (Appendix 4).
phycomycosis (section 9.2). Adverse effects: Nausea, rashes, pruritus,
your physician. weeks between the achievement of biochem- Contra-indications: Breastfeeding (Appendix
Nursing action: Administer drug in the morn- ical euthyroidism and clinical euthyroidism. arthralgia, headache; rarely, alopecia, cuta-
3); long-term treatment. neous vasculitis, thrombocytopenia, aplastic
ing on an empty stomach, as a single dose to Beta-adrenoceptor antagonists (beta-block- Precautions: Pregnancy (Appendix 2), children.
reduce sleeplessness, and at the same time ers) (usually propranolol) may be used as a anaemia, lupus erythematosus-like syndrome,
Adverse effects: Hypersensitivity reactions jaundice, hepatitis, hepatic necrosis, encepha-
each day to maintain drug level in the blood. short-term adjunct to antithyroid drugs to including coryza-like symptoms, headache, lac-
• Assess vital signs of BP and pulse rate before giving control symptoms but their use in heart failure lopathy, nephritis.
rimation, conjunctivitis, pain in salivary glands, Advice to patients: Do not exceed prescribed
each dose of drug. associated with thyrotoxicosis is controversial.
• Tell patient to report immediately if chest pain, laryngitis, bronchitis, rashes; on prolonged dosage; take at regular intervals around-the-
palpitations, sweating, nervousness, shortness of Treatment can be given, if necessary, in preg- treatment, depression, insomnia, impotence, clock; notify physician or pharmacist of symp-
breath, or other signs of overdosage or aggravated nancy but antithyroid drugs cross the placenta goitre in infants of mothers taking iodides.
toms of blood dyscrasias viz fever, sore throat,
cardiovascular disease occur. and in high doses may cause fetal goitre and Dose: Pre-operative management of thyro- unusual bleeding or bruising, headache, or
Dose: Hypothyroidism, by mouth, ADULT hypothyroidism. The lowest dose that will toxicosis, by mouth, ADULT 60–180 general malaise.
initially 50–100 µg daily (25–50 µg for control the hyperthyroid state should be used mg daily. Nursing action: Give drug with meals to re-
those over 50 years) before break- (requirements in Graves disease tend to fall
POM Potassium iodide (WMF 18.8) duce GI distress, and at the same time each day
fast, increased by 25–50 µg every during pregnancy). Propylthiouracil appears Tablet, Potassium iodide 60 mg. to maintain drug level in the blood.
3–4 weeks until normal metabolism in breast milk but does not preclude breast- • Advise patient to consult physician before taking
maintained (usual maintenance dose, feeding as long as neonatal development is IODINE plus POTASSIUM IODIDE OTC products for cough or any iodine containing
100–200 µg daily); where there is closely monitored and the lowest effective products or iodized salt or sea foods such as
Synonym: Lugol’s Solution; Aqueous Iodine
cardiac disease, initially 25 µg daily or dose is used. shell fish.
Oral Solution.
50 µg on alternate days, adjusted in If surgery (partial thyroidectomy) is contem- • Instruct patient not to discontinue drug abruptly
Indications: Pre-operative treatment of thy- to prevent thyroid crisis.
steps of 25 µg every 4 weeks. plated, it may be necessary to give iodine for rotoxicosis.
Congenital hypothyroidism and juve- • Stop drug if severe rash or cervical lymph nodes
10 to 14 days in addition to antithyroid drugs Precautions: Pregnancy, breast-feeding, in- develop.
nile myxoedema (see notes above), by to assist control and reduce vascularity of the fants; not for long-term treatment. • Monitor CBC periodically to detect impending leu-
mouth, NEONATE up to 1 month, in- thyroid. Iodine should not be used for long- Adverse effects: Mental depression, nerv- kopenia, thrombocytopenia, and agranulocytodsis.
itially 5–10 µg/kg daily, CHILD over 1 term treatment since its antithyroid action ousness, insomnia, sexual impotence, myx- Dose: Hyperthyroidism, by mouth, ADULT
month, initally 5 µg/kg daily, adjusted tends to diminish. In patients in whom drug oedema, headache, pain and swelling in 300–600 mg daily until patient be-
in steps of 25 µg every 2–4 weeks, therapy fails to achieve long-term remissions the salivary glands, weakness, conjuctivitis, comes euthyroid; dose may then be
until mild toxic symptoms appear, definitive treatment with surgery or (increas- bronchitis, skin reactions. gradually reduced to a maintenance
then reduce dose slightly. ingly) radioactive iodine is preferable. Advice to patients: Take after meals with food dose of 50–150 mg daily.
POM Levothyroxine sodium (WMF 18.8) or milk or dilute with a large quantity of water, POM Propylthiouracil (WMF 18.8)
Tablets, Levothyroxine (as sodium salt) 50 µg, 100 µg. CARBIMAZOLE fruit juice, milk, or both; take with a straw to Tablet, Propylthiouracil 50 mg.
POM Levothyroxine sodium (EDL 21.6.2) Indications: Thyrotoxicosis. prevent tooth discolouration; discontinue use
Contra-indications: Tracheal obstruction, if stomach pain, skin rash, metallic taste, or POM Propylthiouracil (EDL 21.6.1)
522 | 10.3 Corticosteroids 10.3 Corticosteroids | 523
Tablet, Propylthiouracil 50 mg. long-term disease control. a prolonged period may lead to acute adrenal immunoglobulin [not included on WHO Model
Dexamethasone has very high gluco-corticoid insufficiency, hypotension or death (see With- List] is needed for exposed non-immune pa-
10.3 Corticosteroids activity and insignificant mineralo-corticoid drawal of Systemic Corticosteroids, below). tients receiving systemic cortico-steroids or for
Corticosteroids (section 8.3) include hormones activity, making it particularly suitable for Withdrawal may also be associated with fever, those who have used them within the previous
secreted by the adrenal cortex and synthetic conditions where water retention would be myalgia, arthralgia, rhinitis, conjunctivitis, 3 months; varicella–zoster immunoglobulin
analogues of these hormones. The adrenal a disadvantage. It also has a long duration painful itchy skin nodules and weight loss. should preferably be given within 3 days of
cortex normally secretes hydrocortisone of action and this, together with its lack of CORTICOSTEROID COVER DURING STRESS exposure and no later than 10 days. Confirmed
which has glucocorticoid activity and weak mineralocorticoid activity makes it particularly chickenpox warrants specialist care and urgent
To compensate for a diminished adrenocortical treatment. Corticosteroids should not be
mineralocorticoid activity. It also secretes the suitable for conditions requiring suppression response caused by prolonged corticosteroid
mineralocorticoid aldosterone. Synthetic gluco- of corticotrophin secretion such as congenital stopped and dosage may need to be increased.
treatment, any significant intercurrent illness,
corticoids include betamethasone, dexameth- adrenal hyperplasia. trauma, or surgery requires a temporary Topical, inhaled or rectal corticosteroids are
asone and prednisolone. Fludrocortisone [not Disadvantages of corticosteroids increase in corticosteroid dose, or if already less likely to be associated with an increased
included on WHO Model List] has glucocorticoid stopped, a temporary re-introduction of risk of severe chickenpox.
properties but it is used for its potent mineralo- Overdosage or prolonged use may exaggerate
some of the normal physiological actions of corticosteroid treatment. Anaesthetists must MEASLES
corticoid effects. therefore know whether a patient is taking
corticosteroids leading to mineralocorticoid Patients taking corticosteroids should be ad-
In physiological (low) doses, corticosteroids and glucocorticoid adverse effects. or has been taking a corticosteroid, to avoid vised to take particular care to avoid exposure
replace deficient endogenous hormones. In a precipitous fall in blood pressure during to measles and to seek immediate medical
pharmacological (high) doses, glucocor-ticoids Mineralocorticoid adverse effects include hy- anaesthesia or in the immediate postoperative
pertension, sodium and water retention and advice if exposure occurs. Prophylaxis with
decrease inflammation and suppress the im- period. A suitable regimen for corticosteroid intramuscular normal immunoglobulin [not
mune response. potassium loss. These effects are most marked replacement, in patients who have taken more
with fludrocortisone but are significant with included on WHO Model List] may be needed.
EMDEX
In therapeutic doses glucocorticoids suppress than 10 mg prednisolone daily (or equivalent)
hydrocortisone, occur slightly with predniso- within 3 months of surgery, is: Dosage and administration
release of corticotrophin (adrenocorticotrophic lone and are negligible with dexamethasone.
hormone, ACTH) from the pituitary thus the • Minor surgery under general anaesthesia – usual Adverse effects of systemic gluco-corticoids,
Glucocorticoid adverse effects include diabetes oral corticosteroid dose on the morning of sur- including suppression of the HPA (hypo-thala-
adrenal cortex ceases secretion of endogenous gery or hydrocortisone 25–50 mg intravenously
corticosteroids. If suppressive doses are given mellitus and osteoporosis which is of particular mo-pituitary-adrenal) axis, are dose – and dura-
at induction; the usual oral corticosteroid dose is
for prolonged periods, the adrenal cortex may importance in the elderly since it may result tion-dependent; thus patients should be given
recommenced after surgery
atrophy; this leads to a deficiency on sudden in osteoporotic fractures of the hip or verte- treatment for the shortest period at the lowest
• Moderate or major surgery – usual oral corticosteroid
withdrawal or dosage reduction of the cor- brae. High doses may also be associated with dose on the morning of surgery and hydrocortisone dose that is clinically necessary. In life-threat-
ticosteroid in or situations such as stress or avascular necrosis of the femoral neck. Muscle 25–50 mg intravenously at induction, followed ening diseases, high doses are needed because
trauma when corticosteroid requirements are wasting may also occur and there is a weak link by hydrocortisone 25–50 mg 3 times a day by the complications of therapy are likely to be less
increased. After high dosage or prolonged with peptic ulceration. Mental disturbances intravenous injection for 24 hours after moderate serious than the disease. In long-term therapy
can occur, including serious paranoid state or surgery or for 48–72 hours after major surgery; the in relatively benign chronic conditions such
therapy, withdrawal of the corticosteroid
depression with risk of suicide, particularly in usual preoperative oral corticosteroid dose is re- as rheumatoid arthritis, adverse effects often
should be gradual, see Withdrawal of Systemic commenced on stopping hydrocortisone injections
Corticosteroids. The suppressive effect of a patients with a history of mental disorders; eu- outweigh the advantages. In order to minimize
corticosteroid on cortisol secretion is least phoria is also common. High doses may cause Infections the adverse effects, the maintenance dose
when it is given as a single dose in the morning. Cushing syndrome with moon face, striae and Prolonged courses of corticosteroids increase should be as low as possible and if possible,
Because the therapeutic effects of corticoster- acne; it is usually reversible on withdrawal of susceptibility to infections and increase their single morning doses or alternate-day therapy
oids are of longer duration than the metabolic treatment, but this should always be tapered severity; clinical presentation of infections should be used. Glucocorticoids can improve
effects, intermittent therapy may allow the gradually to avoid symptoms of acute adrenal may also be atypical. Serious infections, for the prognosis of serious conditions such as
therapeutic effects to be maintained while insufficiency (see also Withdrawal of Systemic example septicaemia and tuberculosis, may systemic lupus erythematosus, temporal
reducing metabolic effects. Alternate-day Corticosteroids). In children, corticosteroids reach an advanced stage before being recog- arteritis and polyarteritis nodosa; in such dis-
dosing is, however, suitable only in certain may result in suppression of growth and nised, and amoebiasis or strongyloidiasis may orders the effects of the disease process may
disease states and for corticosteroids with corticosteroids administered during preg- be activated or exacerbated (exclude before be suppressed and symptoms relieved but the
small mineralocorticoid effects and a relatively nancy can affect adrenal development in the initiating a corticosteroid in those at risk or with underlying condition is not cured.
short duration of action. fetus. Any adrenal suppression in the neonate suggestive symptoms). Fungal or viral ocular A corticosteroid may be used in the manage-
following prenatal exposure usually resolves infections may also be exacerbated. ment of raised intracranial pressure or cerebral
Hydrocortisone is used in adrenal replace- spontaneously after birth and is rarely clinically
ment therapy and on a short-term basis by CHICKENPOX oedema that occurs as a result of malignancy;
important. Healing of wounds may be impaired high doses of dexamethasone are generally
intravenous injection for the emergency man- and infections and thinning of the skin may Unless they have had chickenpox, patients
agement of some conditions. Its mineralocor- used. However, a corticosteroid should not
occur; spread of infections may result from receiving oral or parenteral corticosteroids for be used for the management of head injury
ticoid activity is too high for it to be used on modification of tissue reactions. purposes other than replacement should be
a longterm basis for disease control. The high or stroke because it is unlikely to be of benefit
Adrenal suppression regarded as being at risk of severe chickenpox. and may even be harmful.
mineralocorticoid activity of fludrocortisone is Manifestations of fulminant illness include
used together with glucocorticoids in adrenal Adrenal suppression occurs during prolonged pneumonia, hepatitis and disseminated intra- Glucocorticoids are used both topically
insufficiency. therapy with corticosteroids, with develop- vascular coagulation; rash is not necessarily a and systemically. In emergency situations,
Prednisolone has predominantly gluco-corti- ment of adrenal atrophy which may persist for prominent feature. hydrocortisone may be given intravenously.
coid activity and is the corticosteroid used for years after stopping. Abrupt withdrawal after Whenever possible, local treatment with
Passive immunization with varicella–zoster
creams (section 15.2), intra-articular injections, described above. masked until advanced stage; clinical presenta- rotate sites; use 21G needle. SC injection may cause
inhalations (section 7.1.2), eye-drops (section tion may be atypical; risk of chickenpox and atrophy and sterile abscess and should be avoided.
During corticosteroid withdrawal the dose may • Not for alternate day therapy; once daily doses
13.2) or enemas (section 4.8) should be used be reduced rapidly down to the physiological measles increased (see notes above); quiescent
in preference to systemic therapy. tuberculosis—chemoprophylactic therapy should be given in the morning for better results
dosage (equivalent to 7.5 mg prednisolone and less toxicity.
Withdrawal of systemic corticosteroids daily) and then reduced more slowly. Assess- during prolonged corticosteroid treatment;
• Provide assistance with ambulation for the patient
ment of the disease may be needed during elderly; children and adolescents (growth with bone tissue disease to prevent fractures.
The rate of withdrawal of systemic gluco-cor- retardation possibly irreversible); hyperten-
withdrawal to ensure that relapse does not • Patient should avoid abrupt withdrawal of medi-
ticoids is dependent upon several factors sion, recent myocardial infarction (rupture
occur. cation to prevent adrenal crisis.
including size of dose, duration of treatment, reported), congestive heart failure, liver failure, • May mask or exacerbate infections.
individual response, and the likelihood of renal impairment, diabetes mellitus including • Insulin dosage may need to be adjusted in diabet-
relapse of the underlying disease. If there is DEXAMETHASONE
family history, osteoporosis (may be mani- ics; monitor blood glucose.
uncertainty about suppression of the HPA Therapeutic category: Corticosteroid; Glu- • Teach patient to report early signs of adrenal insuf-
fested as back pain, postmenopausal women
axis, withdrawal should be gradual to enable cocorticoid. ficiency namely fatigue, muscular weakness, joint
at special risk), glaucoma including family
the adrenal gland to recover. Patients should Indications: Suppression of inflammatory and pain, fever, anorexia, nausea, dyspnoea, dizziness
history, severe affective disorder (particularly if
be advised not to stop taking glucocorticoids allergic disorders (see also allergy and allergic and fainting.
history of steroid-induced psychosis), epilepsy, Dose: Suppression of inflammatory and aller-
abruptly unless permitted by their doctor. disorders, section 8.3); shock; diagnosis of
psoriasis, peptic ulcer, hypothyroidism, history gic disorders, by mouth, ADULT usual
Cushing syndrome; congenital adrenal hyper-
Gradual withdrawal should be considered in of steroid myopathy; pregnancy (Appendix
plasia; cerebral oedema. range 0.5–10 mg daily; by IM injection
those whose disease is unlikely to relapse and 2); breastfeeding (Appendix 3); interactions:
Contra-indications: See notes above; systemic or slow IV injection or IV infusion (as
who have: Appendix 1.
infection (unless life-threatening or specific an- dexamethasone phosphate), ADULT
• recently received repeated courses (particularly if Adverse effects: GI effects including dys-
taken for longer than 3 weeks) timicrobial therapy given); avoid live virus vac- initially 0.5–20 mg daily; CHILD
pepsia, peptic ulceration (with perforation), 200–500 µg/kg daily
cines in those receiving immunosuppressive
EMDEX
• taken a short course within 1 year of stopping abdominal distension, acute pancreatitis,
long-term therapy doses (serum antibody response diminished). Cerebral oedema, by IV injection (as
oesophageal ulceration and candidosis; dexamethasone phosphate), ADULT
• other possible causes of adrenal suppression Precautions: Adrenal suppression during pro-
• received more than 40 mg daily prednisolone (or musculoskeletal effects including proximal 10 mg initially, then 4 mg by IM injec-
longed treatment which persists for years after
equivalent) myopathy, osteoporosis, vertebral and long tion (as dexamethasone phosphate)
stopping treatment (see notes above); ensure
• been given repeat doses in the evening bone fractures, avascular osteonecrosis, every 6 hours, as required for 2–10
patients understand importance of compliance
• received more than 3 weeks’ treatment tendon rupture; endocrine effects including days
with dosage and have guidance on precautions
Abrupt withdrawal may be considered in those adrenal suppression, menstrual irregularities Diagnosis of Cushing syndrome, see
to reduce risks; monitor weight, blood pressure,
whose disease is unlikely to relapse and who and amenorrhoea, Cushing syndrome (with manufacturer’s literature.
fluid and electrolyte balance and blood glucose
have received treatment for 3 weeks or less high doses, usually reversible on withdrawal), Note: Dexamethasone 1 mg ≡ dexamethasone
levels throughout prolonged treatment; infec-
and who are not included in the patient groups hirsutism, weight gain, negative nitrogen and phosphate 1.2 mg ≡ dexamethasone sodium phos-
tions (greater susceptibility, symptoms may be
calcium balance, increased appetite, increased phate 1.3 mg.
Table-1: Equivalent doses of systemic corticosteroids susceptibility to and severity of infection;
POM Dexamethasone (WMF 18.1)
Drug Equivalent Dose (mg)† Relative Mineralocorticoid Potency neuropsychiatric effects including euphoria, Tablet, Dexamethasone 500 µg.
Glucocorticoids
psychological dependence, depression, insom- Injection, Dexamethasone phosphate (as dexa-
nia, increased intracranial pressure with papil- methasone sodium phosphate) 4 mg/mL; in 1-mL
Short-acting (T½ = 8 – 12 hours)
loedema in children (usually after withdrawal), ampoule.
Cortisone 25 2 psychosis and aggravation of schizophrenia,
POM Dexamethasone (EDL 21.1)
Hydrocorticone 20 2 aggravation of epilepsy; ophthalmic effects Tablets, Dexamethasone. 0.5 mg, 4 mg.
including glaucoma, papilloedema, posterior Injection, Dexamethasone 2 mg, 4 mg per mL; in
Intermediate-acting (T½ = 12 – 36 hours)
subcapsular cataracts, corneal or scleral thin- 2-mL amps.
Methylprednisolone 4 0 ning and exacerbation of ophthalmic viral or
POM DEMESONE® (Adler)
Prednisolone 5 1 fungal disease; also impaired healing, skin at- Tablet, Dexamethasone 0.5 mg.
Prednisone 5 1
rophy, bruising, striae, telangiectasia, acne, my- 0.5 mg – 1000’s.
ocardial rupture following recent myocardial
Triamcinolone 4 0 POM DEXADON® (Standard Generics)
infarction, fluid and electrolyte disturbances,
Long-acting (T½ = 36 – 54 hours) Tablet, Dexamethasone 0.5 mg.
leukocytosis, hypersensitivity reactions (includ-
0.5 mg – 10 x 10’s; 1000’s.
Betamethasone 0.6 0 ing anaphylaxis), thromboembolism, nausea,
malaise and hiccups; perineal irritation may POM DEXALAB® (Embassy)
Dexamethasone 0.75 0
follow IV administration of phosphate ester. Tablet, Dexamethasone 500 mcg.
Mineralocorticoid 500 mcg – 100’s.
Advice to patients: Take with food to minimize
Fludrocortisone (T½ = 12 – 24 hours) Not used for glucocorticoid effect 125 GI upset; do not use longer than prescribed; re- POM Dexamethasone (Alpha)
†
Equivalent doses are approximations and may not apply to all diseases or routes of administration. Duration of port signs of infection or injury during therapy; Injection, Dexamethasone phosphate 5 mg per mL;
hypothalamic-pituitary-adrenal (HPA) axis suppression and degree of mineralocorticoid activity must be considered let the physician or dentist know that you are 1-mL amp.
separately.
Source: Compendium of Pharmaceuticals and Specialties. Canadian Pharmacists Association. [updated
on steroid before any surgery. POM Dexamethasone (Alpha)
2011 Oct; cited 2013 Aug 25]. Available from: http://www.univadis.ca/medical_and_more/eCPS_ Nursing action: Give with meals or milk to Injection, Dexamethasone sodium phosphate 4
search?language=en&documentid=m139800&product=Corticosteroids%3a+Systemic# reduce GI upset. mg per mL
• Give IM injection deep into the gluteal muscle;
POM Dexamethasone (Jopan) ness, severe or continuing headache, swelling Adverse effects: GI effects including dys- evening); CHILD 10–30 mg.
Tablet, Dexamethasone 1 mg of feet or lower legs or unusual weight gain pepsia, peptic ulceration (with perforation), Acute adrenocortical insufficiency, by
Pack: 100’s occur. abdominal distension, acute pancreatitis, slow IV injection or by IV infusion,
POM Dexamethasone (Mecure) Nursing action: Administer drug with food or oesophageal ulceration and candidosis; ADULT 100–500 mg, 3–4 times in 24
Tablet, Dexamethasone USP 0.5 mg. milk to minimise GI upset. musculoskeletal effects including proximal hours or as required; by slow IV injec-
0.5 mg – 1 x 100’s. • Provide assistance with ambulation for the patient myopathy, osteoporosis, vertebral and long tion, CHILD up to 1 year 25 mg, 1–5
with bone tissue disease to prevent fractures. bone fractures, avascular osteonecrosis, years 50 mg, 6–12 years 100 mg.
POM Dexamethasone (Vixa)
• Diet low in sodium and high in potassium may be tendon rupture; endocrine effects including
Injection, Dexamethasone 4 mg per mL; in 1-mL amp. POM Hydrocortisone (WMF 18.1)
recommended.
Pack: 1 mL x 25’s; 1 mL x 100’s. adrenal suppression, menstrual irregularities Injection, Hydrocortisone (as sodium succinate)
• Advise patient to avoid discontinuing drug
abruptly and to report signs of infection.
and amenorrhoea, Cushing syndrome (with 100-mg vial.
POM Dexamethasone (Zolon)
Tablet, Dexamethasone 0.5 mg; uncoated tab Dose: By mouth, Adrenocortical insufficiency, high doses, usually reversible on withdrawal),
POM Hydrocortisone (EDL 21.1 & 18.1)
Adult, 50-300 mcg daily. hirsutism, weight gain, negative nitrogen and
POM DEXAREL® (Embassy) Injection, Hydrocortisone (as sodium succinate) 100
Child: 5 mcg/kg daily. calcium balance, increased appetite, increased mg; powder for reconstitution in vial.
Tablet, Dexamethasone 0.5 mg. susceptibility to and severity of infection;
0.5 mg – 100’s. POM Fludrocortisone (EDL 21.1/Restricted List) POM ALFACORT® (Alpha)
neuropsychiatric effects including euphoria,
POM DEXATOP® (Neros) Tablet, Fludrocortisone 0.1 mg. Injection, Hydrocortisone (as sodium succinate) 100
psychological dependence, depression, insom-
Tablet, Dexamethasone acetate 0.5 mg. mg; powder for injection.
nia, increased intracranial pressure with papil-
0.5 mg – 10 x 10’s (in blisters). HYDROCORTISONE POM CLOSONE® (Chanmedi)
loedema in children (usually after withdrawal),
POM GG Dexamethasone (Geneith) Therapeutic category: Corticosteroid; Miner- psychosis and aggravation of schizophrenia, Injection, Hydrocortisone 100 mg.
Tablet, Dexamethasone 1 mg. alocorticoid; Anti-iflammatory Agent. aggravation of epilepsy; ophthalmic effects 100 mg – 5 mL x 50’s.
1 mg – 10 x 10’s Indications: Adrenocortical insufficiency; including glaucoma, papilloedema, posterior POM DROCORT® (Elbe)
EMDEX
hypersensitivity reactions including anaphy- subcapsular cataracts, corneal or scleral thin- Injection, Hydrocortisone 500 mg.
POM MESLON® (Beta Drugs)
Injection, Dexamethasone 4 mg per mL; in 1-mL amp. lactic shock (section 8.3); inflammatory bowel ning and exacerbation of ophthalmic viral or POM EMBALUT® Depot (Embassy)
Pack: 25’s x 1 mL; 10’s x 1 mL. disease (section 4.8); skin (section 15.2); asthma fungal disease; also impaired healing, skin Injection, Hydroxyprogesterone (as caproate) 250
(section 7.1.2). atrophy, bruising, striae, telangiectasia, acne, mg, benzyl alcohol 1% (as preservative), arachis oil
POM NOVAMAK® (Mark) Contra-indications: See notes above; systemic
Tablet, Dexamethasone 0.5 mg. myocardial rupture following recent myocar- q.s; in 1-mL amp.
infection (unless life-threatening or specific an- dial infarction, fluid and electrolyte distur- Pack: 1 mL x 1’s (in amp)
POM NOZET® (Geneith) timicrobial therapy given); avoid live virus vac- bances, leukocytosis, hypersensitivity reactions
Injection, Dexamethasone 4 mg per mL POM HYDROCORT®(Hochiez)
cines in those receiving immunosuppressive (including anaphylaxis), thromboembolism, Injection, Hydrocortisone (as sodium succinate)
POM PACSONE® (Pacmai) doses (serum antibody response diminished). nausea, malaise and hiccups. 100 mg.
Tablet, Dexamethasone 0.5 mg; uncoated tab. Precautions: Adrenal suppression during pro- Advice to patients: See also under Predni- Pack: 10’s
0.5 mg – 10 x 10’s (in blisters). longed treatment which persists for years after solone.
Injection, Dexamethasone phosphate 4 mg per mL POM Hydrocortisone (Alpha)
stopping treatment (see notes above); ensure Nursing action: Oral dose may be given with
4 mg – 1 x 10’s amp Injection, Hydrocortisone succinate 100 mg; white
patients understand importance of compliance meals or milk to reduce GI upset. to almost white powder in a vial.
POM PEMADEX® (Pemason) with dosage and have guidance on precautions • Give IM injection deep in large muscle mass; rotate Pack: 1 x 50’s.
Tablets, Dexamethasone 0.5 mg, 1 mg to reduce risks; monitor weight, blood pressure, sites; avoid deltoid; use 21 G needle; SC injection
0.5 mg – 10 x 10’s; 1000’s fluid and electrolyte balance and blood glucose may damage tissue, and should be avoided. POM HYDROZAR® (Shrezar)
1 mg – 10 x 10’s • Give once daily doses in the morning for better Injection, Hydrocortisone sodium succinate 100 mg
levels throughout prolonged treatment; infec-
Injection, Dexamethasone 4 mg per mL;in 1-mL amp. results and to prevent adrenal suppression. Pack: 1 x 10’s
tions (greater susceptibility, symptoms may be
marked “Pemadex”. • Provide assistance with ambulation in patients POM LABOHYDRO® (Embassy)
masked until advanced stage; clinical presenta-
Pack: 1 mL x 10 x 10’s. who have bone tissue disease to prevent fractures. Injection, Hydrocortisone 100 mg.
tion may be atypical; risks of chickenpox and • Teach patient to report early signs of adrenal insuf-
POM SIVOMETHASONE® (Adpharm) measles increased (see notes above); quiescent Pack: 50’s.
ficiency viz fatigue, muscular weakness, joint pain,
Injection, Dexamethasone 4 mg per mL. tuberculosis—chemoprophylactic therapy fever, nausea, dyspnoea, dizziness and fainting. POM NATOXAL® (Vixa)
POM TADI® (Pharmgate) during prolonged corticosteroid treatment; • May mask or exacerbate infections. Injection, Hydrocortisone sodium succinate 100
Tablet, Dexamethasone 0.5 mg elderly; children and adolescents (growth • Note that diabetics may require increased insulin; mg/vial.
0.5 mg – 1 x 10’s; 1 x 1000’s retardation possibly irreversible); hyperten- monitor blood sugar. Pack: 10’s (in vials).
sion, recent myocardial infarction (rupture • Diet low in sodium and high in potassium and POM RYCORT® (Reals)
POM XASTEN® (Vixa) protein may be recommended.
Tablet, Dexamethasone 0.5 mg. reported), congestive heart failure, liver failure, Injection, (100 mg) Hydrocortisone sodium succinate
• Tell patient to avoid OTC medications viz salicy- 134 mg equiv. to Hydrocortisone 100 mg; in vial.
Injection, Dexamethasone 4 mg per mL; in 1-mL amp. renal impairment, diabetes mellitus including
lates, alcohol in cough mixtures, and cold remedies Injection, (500 mg) Hydrocortisone sodium succinate
family history, osteoporosis (may be mani- unless otherwise instructed by doctor.
fested as back pain, postmenopausal women 670 mg equiv. to Hydrocortisone 500 mg; in vial.
FLUDROCORTISONE • Inspect patient’s skin for petechiae; warn him that
Therapeutic category: Corticosteroid; Min- at special risk), glaucoma including family he may bruise easily. POM SOLU-CORTEF® (Pfizer)
eralocorticoid. history, severe affective disorder (particularly if • Observe for depression or psychotic episodes, Injection, (100 mg), Hydrocortisone 100 mg; in 2
history of steroid-induced psychosis), epilepsy, especially when treatment involves high-dose. compartment vial containing sterile powder for
Indications: Mineralocorticoid replacement in
psoriasis, peptic ulcer, hypothyroidism, history Dose: Replacement therapy in adrenocortical reconstitution + water for injection as diluent.
adrenocortical insufficiency. Pack: 2-mL Act-O-Vial.
Contra-indications, Precautions, etc.: See of steroid myopathy; pregnancy (Appendix insufficiency, by mouth, ADULT 20–30
Injection, (250 mg) Hydrocortisone 250 mg; in 2
under Dexamethasone. 2); breastfeeding (Appendix 3); interactions: mg daily in divided doses (usually 20
compartment vial containing sterile powder for
Advice to patients: Notify physician if dizzi- Appendix 1. mg in the morning and 10 mg in early
reconstitution + water for injection as diluent. POM Methylprednisolone (EDL 21.1/Restricted List) longed treatment which persists for years after Advice to patients: Notify surgeon or dentist
Pack: 2-mL Act-O-Vial. Injection, Methylprednisolone acetate 40 mg per mL; stopping treatment (see notes above); ensure before surgical repairs; may cause GI upset;
in 1-mL, 2-mL vials. patients understand importance of compliance take oral formulation with food or milk to
POM STRICORT® (Strides Vital)
Injection, Hydrocortisone 100 mg; in vials. POM METHYSOL® (Korlyns) with dosage and have guidance on precau- decrease GI effects.
Pack: 100’s. Tablet, Methylprednisolone 4 mg; white and round tions to reduce risks; monitor weight, blood Nursing action: Oral dose may be given with
tablet. pressure, fluid and electrolyte balance and meals to minimize GI upset.
POM SYNERCORT® (Synergy) • Tell patient not to discontinue drug abruptly or
4 mg – 100’s; 500’s (in bottle) blood glucose levels throughout prolonged
Injection, Injection, Hydrocortisone (as sodium without doctor’s consent.
succinate) 100 mg.
Injection, (125 mg), Methylprednisolone (as Sodium treatment; infections (greater susceptibility,
succinate) 125 mg; white crystalline powder in a symptoms may be masked until advanced • This drug may mask or exacerbate infections,
Pack: 100 mg per vial. instruct patient to report slow healing of wound.
10-mL glass vial stage; clinical presentation may be atypical;
125 mg – 10 vials + 10 diluent Amps (2-mL). • Teach patient the early signs of adrenal insuf-
METHYLPREDNISOLONE risk of chickenpox and measles increased (see ficiency which may include fatigue, muscular
Dose: Acute allergic reactions, status asthmaticus,
notes above); quiescent tuberculosis—chem- weakness, joint pain, fever, anorexia, nausea,
Therapeutic category: Corticosteroid; Gluco- cerebral oedema, Adult, initially 10-40 mg
depending on the condition being treated; oprophylactic therapy during prolonged dizziness and fainting.
corticoid; Anti-inflammatory Agent.
may be repeated 2-3 times in 24 hours. corticosteroid treatment; elderly; children • Watch for depression or psychotic episodes; dia-
Pharmacology: Methylprednisolone is a
Child: By IV injection (over a period of one and adolescents (growth retardation possibly betic patient may require increased insulin, ensure
synthetic glucocorticoid with potent anti-in-
to several minutes), not less than 0.5 mg per irreversible); hypertension, recent myocardial blood glucose is monitored.
flammatory effects in disorders of many organ • Don’t confuse with prednisone.
kg every 24 hours; to be reduced gradually infarction (rupture reported), congestive heart
systems; it has little mineralocorticoid effect. once the patient’s condition is under con- • May be used for alternate-day therapy
failure, renal impairment, hepatic impairment
Indications: Suppression of inflammatory and trol. Dosage should depend more on the • Diet low in sodium and high in potassium and
(Appendix 5); diabetes mellitus including
allergic disorders; cerebral oedema; rheumatic severity of the condition and response of protein may be recommended.
family history, osteoporosis (may be mani-
and dermatologic diseases. the patient than on the age and size. Dose: Suppression of inflammatory and
fested as back pain, postmenopausal women
Contra-indications, Precautions, etc: See Injection, (500 mg), Methylprednisolone (as Sodium allergic disorders, by mouth, ADULT
EMDEX
succinate) 500 mg; white crystalline powder in a at special risk), glaucoma including family
under Prednisolone. initially up to 10–20 mg daily (severe
20-mL glass vial history, severe affective disorder (particularly if
Advice to patients: See also under Predni- disease, up to 60 mg daily), preferably
500 mg – 5 vials + 5 diluent Vials (7.8-mL). history of steroid-induced psychosis), epilepsy,
solone. taken in the morning after breakfast;
Dose: Suppression of graft injection reaction, by IV in- psoriasis, peptic ulcer, hypothyroidism, history
Nursing action: Oral dose may be given with dose can often be reduced within a
jection, 0.5-2.0 g every 24-48 hours (30 mg/ of steroid myopathy; pregnancy (Appendix
meals to reduce GI upset. kg/day). Because of the risk of arrhythmias, few days, but may need to be con-
• Give IM injection deep in large muscle mass; rotate 2); breast-feeding (Appendix 3); interactions:
it should be given by infusion in cases of tinued for several weeks or months;
sites; avoid deltoid; use 21G needle; after shaking Appendix 1.
myocardial damage. CHILD fractions of adult dose may be
parenteral suspension; SC injectin may damage Adverse effects: GI effects including dys-
used (for example, at 1 year 25% of
tissue, and should be avoided. POM SOLU-MEDROL® (Pfizer) pepsia, peptic ulceration (with perforation),
Injection, Methylprednisolone (as Sodium succinate)
adult dose, at 7 years 50%, and at 12
• Give I.V. dose slowly over 1 minute. Acetate salt abdominal distension, acute pancreatitis,
is not for I.V. use; it should not be used when fast 40 mg; sterile powder for reconstitution. years 75%) but clinical factors must
oesophageal ulceration and candidosis;
onset of action is needed. Pack: 1-mL Act-O-Vial. be given due weight.
musculoskeletal effects including proximal
• Give once daily doses in the morning for better Dose: By IM, slow IV injection or infusion, initially 10- Maintenance, by mouth, ADULT
myopathy, osteoporosis, vertebral and long
results and to prevent adrenal suppression. 500 mg; may need larger doses for severe, 2.5–15 mg daily or higher; cushingoid
acute conditions. bone fractures, avascular osteonecrosis,
• Teach patient to report early signs of adrenal insuf- features are increasingly likely with
ficiency viz fatigue, muscular weakness, joint pain, As adjunctive therapy in life-threatening tendon rupture; endocrine effects including
doses above 7.5 mg daily; CHILD frac-
fever, nausea, dyspnoea, dizziness and fainting. conditions, by IV injection (over a period of adrenal suppression, menstrual irregularities
tions of adult dose may be used (for
• Monitor body weight, serum electrolytes, vital at least 30 mins), 30 mg/kg b. wt.; may be and amenorrhoea, Cushing syndrome (with
example, at 1 year 25% of adult dose,
signs, and report abnormal weight gain or any repeated every 4-6 hours for up to 48 hours. high doses, usually reversible on withdrawal),
at 7 years 50%, and at 12 years 75%)
chest pain to the doctor. hirsutism, weight gain, negative nitrogen and
POM SOLUPRED® (Strides Vital) but clinical factors must be given due
• Monitor intake and urinary output, noting espe- calcium balance, increased appetite, increased
Injection, Methylprednisolone 500 mg, 1000 mg. weight.
cially decrease in output. susceptibility to and severity of infection;
Pack: 1’s. Myasthenia gravis, initially 10 mg on
• May mask or exacerbate infections.
neuropsychiatric effects including euphoria,
• Note that diabetics may require increased insulin; alternate days, increased in steps of
monitor blood sugar. PREDNISOLONE psychological dependence, depression, insom-
10 mg on alternate days to 1–1.5 mg/
• Provide assistance with ambulation in patients Therapeutic category: Adrenal corticosteroid; nia, increased intracranial pressure with papil-
kg (maximum 100 mg) on alternate
who have bone tissue disease to prevent fractures. Glucocorticoid; Anti-inflammatory Agent. loedema in children (usually after withdrawal),
days or initially 5 mg daily increased
• Monitor sleep pattern of the patient since euphoria Indications: Suppression of inflammatory and psychosis and aggravation of schizophrenia,
in steps of 5 mg daily to usual dose of
may interfere with sleep initially. Reassure patient allergic reactions (see also section 8.3); with aggravation of epilepsy; ophthalmic effects
that he will adjust within 1-3 weeks.
60–80 mg daily (0.75–1 mg/kg daily).
antineoplastic drugs for acute leukaemias and including glaucoma, papilloedema, posterior Note: Alternate-Day Therapy (ADT) should be
• Diet low in sodium and high in potassuim and subcapsular cataracts, corneal or scleral thin-
lymphomas (section 12.2.2); eye (section 13.2); considered for long-term therapy; ADT is a corti-
protein may be recommended. ning and exacerbation of ophthalmic viral or
• May be used for alternate-day therapy. asthma (section 7.1.2). costeroid dosing regimen in which twice the usual
Contra-indications: See notes above; systemic fungal disease; also impaired healing, skin daily dose of corticoid is administered every other
• Observe patient for depression or psychotic
symptoms, especially when high doses are used. infection (unless life-threatening or specific an- atrophy, bruising, striae, telangiectasia, acne, morning. The purpose of this mode of therapy is to
timicrobial therapy given); avoid live virus vac- myocardial rupture following recent myocar- provide the patient requiring long-term, pharma-
Dose: By IM injection or slow IV injection or cologic-dose treatment with the beneficial effects
infusion, initially 10–500 mg; graft cines in those receiving immunosuppressive dial infarction, fluid and electrolyte distur-
bances, leukocytosis, hypersensitivity reactions of corticoids while minimising certain undesirable
rejection, up to 1 g daily by IV infusion doses (serum antibody response diminished). effects, including pituitary-adrenal suppression, the
for up to 3 days. Precautions: Adrenal suppression during pro- (including anaphylaxis), thromboembolism,
cushingoid state, corticoid withdrawal symptoms,
nausea, malaise and hiccups.
530 | 10.4 Sex hormones 10.4.1 Estrogens (Female sex hormones) | 531
and growth suppression in children. The rationale Pack: 2 mL x 10’s. bone by increasing calcium deposition. They (until age 50 years).
for this treatment schedule is based on two major are secreted at varying rates during the men-
premises: (a) the anti-inflammatory or therapeutic
POM PROLONE® (Chanmedi) RISKS OF HRT
Tablet, Prednisolone 5 mg. strual cycle throughout the period of activity
effect of corticoids persists longer than their physical of the ovaries. During pregnancy, the placenta When prescribing HRT, women must be made
5 mg – 1000’s.
presence and metabolic effects, and (b) admin- aware of the increased incidence of venous
becomes the main source of estrogens. Ovarian
istration of corticosteroid every other morning POM RGI Prednisolone® (Richygold) thromboembolism, of stroke and, after some
allows for reestablishment of more nearly normal Tablet, Prednisolone 5 mg.
secretion declines at the menopause.
years of use, endometrial cancer (reduced by a
hypothalamic-pituitary-adrenal (HPA) activity on 5 mg – 10 x 10’s. Estrogen therapy is given cyclically or contin- progestogen) and breast cancer. Each decision
the off-steroid day. uously principally for contraception and for
POM ZYCORT®(Nalis) to start HRT should be made on an individual
POM Prednisolone (WMF 18.1) Tablet, Prednisolone 5 mg the alleviation of menopausal symptoms. If basis, and treatment should be regularly reap-
Tablet, Prednisolone 5 mg, 25 mg. 5 mg – 10 x 10’s (in blisters) long-term therapy is required for menopausal praised. Factors such as corticosteroid therapy,
hormone therapy a progestogen should nor- family history of osteoporosis, thinness, lack of
POM Prednisolone (EDL 21.1)
Tablets, Prednisolone 1 mg, 5 mg. PREDNISONE mally be added to prevent cystic hyperplasia exercise, alcoholism or smoking, early meno-
Therapeutic category: Corticosteroid; Gluco- of the endometrium (or of endometrial foci in pause, fractures to the hip or forearm before
POM DELTACORTRIL® (Neimeth) women who have had a hysterectomy) and
Tablet, Prednisolone 5 mg. corticoid; Anti-inflammatory Agent. age 65 years should be taken into account
Pharmacology: Prednisone is inactive and possible transformation to cancer. when considering the use of HRT; women of
5 mg – 100’s; 1000’s.
must be metabolised to prednisolone which The palliative care of advanced inoperable, African origin appear to be less susceptible
POM PERILON® (Hovid) may be impaired in patients with impaired liver metastatic carcinoma of the breast in both to osteoporosis than those who are white or
Tablet, Prednisolone 5 mg.
function. See under prednisolone. men and postmenopausal women is another of Asian origin.
5 mg – 10 x 10’s (blister)
Indications, Contra-indications, etc: see indication for estrogen therapy. There is an increased risk of deep-vein throm-
POM PETREP® (Pemason) under Prednisolone.
Tablet, Prednisolone acetate 5 mg Hormone replacement therapy (HRT) bosis and of pulmonary embolism in women
Dose: By mouth, initially 5-60 mg/day de-
EMDEX
Pack: 10 x 10’s Estrogens are used for replacement therapy taking HRT especially in the first year of use.
pending on the nature and severity of About 10 in every 1000 women aged 50–59
POM PEXALONE® (BG Pharmacy) the disease, and patient’s response. in perimenopausal and menopausal women
who are unduly affected by symptoms such years develop venous thromboembolism over
Tablet, Prednisolone 5 mg; uncoated tab. See also under prednisolone and the
5 mg – 10 x 10’s (in blister) as vasomotor instability and vulval and 5 years; this figure rises by about 1 extra case
proprietary preparations below. in 1000 in those using estrogen-only HRT and
vaginal atrophy. Estrogens can also prevent
POM PREDILAB-5® (Embassy) POM Apo-Prednisone® (Lahams) about 4 extra cases in 1000 in those using an
Tablet, Prednisolone 5 mg. postmenopausal osteoporosis but drugs that
Tablet, Prednisone 5mg; white scored tab marked estrogen and a progestogen for 5 years. About
5 mg – 10 x 10’s. have a specific effect on bone metabolism are
‘APO 5’. 20 in every 1000 women aged 60–69 years not
5 mg – 1000’s. now preferred.
POM PREDILIN® (Geneith) using HRT develop venous thromboembolism
Tablet, Prednisolone 5 mg. POM Prednisone (Neros)
HRT does not prevent coronary heart disease over 5 years; this figure rises by about 4 extra
Tablet, Prednisone 5 mg. nor does it protect against a decline in cogni- cases in 1000 in those using estrogen-only HRT
POM PREDINGA® (Crowther)
5 mg – 10 x 20’s (in blisters). tive function and it should not be prescribed and about 9 extra cases in 1000 in those using
5 mg – 10 x10’s Dose: Short-term treatment, Adult, 6-16 tablets daily for these reasons. The minimum effective dose an estrogen and a progestogen for 5 years. In
Long-term treatment, Adult, 1-3 tablets daily of HRT should be used for the shortest duration women who have predisposing factors such
POM PREDNICORTEX® (Korlyns) Children: ¼ to ½ tablet/5 kg of b.wt daily. possible, and treatment should be reviewed at
Tablet, Prednisolone 5 mg; white tab. marked ‘PDC-5’ as a personal or family history of deep venous
least annually. thrombosis or pulmonary embolism, severe
5 mg – 10 x 10’s (in blisters). TRIAMCINOLONE
Whilst a short course of a topical vaginal estro- varicose veins, obesity, surgery, trauma or
POM PREDNI-J® (Juhel)
POM EMBALON® (Embassy) gen preparation can relieve symptoms of vulval prolonged bed-rest, the overall risk may out-
Tablet, Prednisolone 5 mg; white scored tab
5 mg – 10 x 10’s (in blisters); 1000’s (in tins).
Injection, Triamcinolone acetonide 40 mg per mL; and vaginal atrophy, systemic HRT is required weigh the benefit. Travel involving prolonged
in 1-mL amp. to alleviate vasomotor symptoms. immobility also increases the risk of venous
POM Prednisolone (Hochiez) thromboembolism.
POM TRAMLOG® (Mark) In women with an intact uterus (or endometrial
Injection, Triamcinolone acetate 40 mg per mL foci), the addition of a progesterone to the Using HRT increases the risk of breast cancer
POM Prednisolone (Onifam) estrogen therapy reduces the risk of endo- slightly. The increased risk is related to the
See lit. for more information.
Tablet, Prednisolone 5 mg. metrial cancer (but can slightly increase the duration of HRT use and this excess risk dis-
5 mg – 10 x 10’s
risk of breast cancer). Medroxyproges-terone appears within about 5 years of stopping. The
POM Prednisolone (Pharmabox) 10.4 Sex hormones acetate (see also section 10.4.2) may be given risk of breast cancer is greater with combined
Tablet, Prednisolone 5 mg; white scored f-c tab. 10.4.1 Estrogens (Female sex hormones) in a dose of 10 mg daily for the last 12–14 days HRT (an estrogen and a progestogen) than
marked ‘Pred’. 10.4.2 Progestogens (Female sex hormones) of each cycle of estrogen therapy. Alternatively, with estrogen-only HRT (but estrogen alone
5 mg – 10 x 10’s (in blisters). 10.4.3 Androgens (Male sex hormones) norethisterone 1 mg daily may be given on the may not be suitable for women with intact
POM PREDNITAB® (Adler) last 12–14 days of each 28-day estrogen cycle. uterus, see above).
Tablet, Prednisolone 5 mg. 10.4.1 Estrogens (Female
HRT may be considered for women with early In women aged between 50 and 64 years not
5 mg – 1000’s. sex hormones)
natural or surgical menopause (before age 45 using HRT, a breast cancer will be diagnosed
POM PREDNOL® (Shrezar) Estrogens are necessary for the development years); however, alternatives to HRT should be in about 14 out of every 1000 women over
Tablet, Prednisolone 5 mg; uncoated tab. of female secondary sexual characteristics; considered if osteoporosis is the main concern. 5 years. In women using an estrogen and a
5 mg – 10 x 10’s (in blisters) they also stimulate myometrial hypertrophy For early menopause, HRT can be given until progestogen for 5 years, there will be about
Injection, Prednisolone sodium phosphate 15 mg with endometrial hyperplasia. They affect the approximate age of natural menopause 6 additional cases in 1000; in women using
per mL; in 2-mL amp
532 | 10.4.1 Estrogens (Female sex hormones) 10.4.2 Progestogens (Female sex hormones) | 533
estrogen-only HRT for 5 years, there will be 11.3.1). progestogen if necessary, see notes Note: Give injection very slowly to avoid transient
about 1.5 additional cases in 1000. Contra-indications: Pregnancy; estrogen-de- above). urge to cough, coughing fits, respiratory distress that
pendent cancer; active thrombophlebitis or Palliation in prostate cancer, by mouth, may occur during or immediately after the injection
In women aged between 50 and 79 years not of oily solutions
using HRT, breast cancer will be diagnosed thromboembolic disorders or history of recent ADULT 0.15–1.5 mg daily.
in about 31 out of every 1000 women over venous thromboembolism (unless already on POM Ethinylestradiol (WMF 18.4) POM PRIMOGYN Depot® (CHI/Schering)
anticoagulant therapy); undiagnosed vaginal Injection, (Depot), Estradiol valerate 10 mg per mL;
5 years. In women using an estrogen and a Tablets, Ethinylestradiol 10 µg, 50 µg.
bleeding; breastfeeding (Appendix 3); liver oily injection.
progestogen for 5 years there will be about POM Ethinylestradiol (EDL 21.4) Pack: 1 x 1-mL amp.
4 additional cases in 1000; in women using disease (where liver function tests have failed
Tablets, Ethinylestradiol 0.01 mg, 0.05 mg.
estrogen only HRT for 5 years there will be no to return to normal), Dubin-Johnson and Rotor POM Oestradiol (Mark)
additional cases of breast cancer diagnosed. syndromes (or monitor closely). Oily injection, Estradiol (dipropionate) 10 mg per
ESTRADIOL mL; clear, colourless to green-yellow oily solution
Precautions: Progestogen may need to be
HRT slightly increases the risk of stroke. About added to regimen to reduce risk of endo- Indications: Intramuscular estrogen indicated in ampoule.
3 in every 1000 women aged 50–59 years not metrial cancer due to unopposed estrogen in primary and secondary amenorrhoea, Pack: 1-mL x 5’s.
using HRT have a stroke over 5 years; this figure (see notes above); migraine (or migraine-like deficiency symptoms in young women after
rises by about 2 additional cases in 1000 in headache); diabetes (increased risk of heart oophorectomy or radiological castration for ESTROGENS, CONJUGATED
those using estrogen-only HRT and by about disease); history of breast nodules of fibrocystic non-carcinomatosis disease, gynaeoclogical Oral Hormonal Replacement Therapy (HRT)
1 additional case in those using an estrogen disease—closely monitor breast status (risk of operations, dysfunctional bleeding. Indications: Menopausal and postmenopausal
and a progestogen for 5 years. About 26 in breast cancer, see notes above); uterine fibroids Contra-indications: Pregnancy; existing or estrogen replacement therapy for vasomotor
every 1000 women aged 60–69 years not using may increase in size; symptoms of endome- suspected hormone dependent tumours of symptoms and allied disorders such as oesteo-
HRT have a stroke over 5 years; this figure rises triosis may be exacerbated; predisposition to the uterus or mammae; previous or existing porosis, atrophic vaginitis, kraurosis vulvae, and
by about 6 additional cases in 1000 in those thromboembolism (see notes above); presence liver tumours; endometriosis; thromboembolic postmenopausal atrophic urethritis.
EMDEX
using an estrogen-only HRT and by about 4 of antiphospholipid antibodies; increased risk processes. Contra-indications: Cancer of the breast
additional cases in those using an estrogen of gallbladder disease; hypophyseal tumours; Precautions: Regular general medical and and other estrogen-dependent neoplasia;
and a progestogen for 5 years. porphyria; interactions: Appendix 1. gynaecological examination before starting undiagnosed abnormal genital bleeding;
HRT possibly increases the risk of coronary Adverse effects: Nausea and vomiting, treatment and at 6-monthly intervals.; exclude thrombophlebitis, thrombosis or thromboem-
heart disease in the first year. About 3 in every abdominal cramps and bloating, weight in- pregnancy. Risk of thromboembolic diseases bolic disorders; acute or chronic liver disease;
1000 women aged 50–69 not using HRT have crease; breast enlargement and tenderness; appears to increase especially in patients with severe cardiac or renal disease; pregnancy
endometrial cancer diagnosed over 5 years; premenstrual-like syndrome; sodium and history of thromboembolic diseases or in the (for estrogen-progestogen combination only).
in those using estrogen-only HRT for 5 years fluid retention; thromboembolism (see notes presence of severe diabetes with vascular Precautions: Not recommended for use as
endometrial cancer is diagnosed in about 5 above); altered blood lipids (may lead to pan- changes or sickle-cell anaemia. Rarely, ma- oral contraceptive. The estrogen-progestogen
additional cases in 1000. The risk of endome- creatitis); cholestatic jaundice, glucose intoler- lignant liver tumours leading to threatening preparation is unsuitable for use with oral con-
trial cancer cannot be reliably estimated in ance; rashes and chloasma; changes in libido; intraabdominal haemorrhage may occur; traceptive and is not necessary for women who
those using an estrogen and a progestogen depression, headache, migraine, dizziness, leg patient should report any unusual upper have had a hysterectomy (for whom oestrogen
because the addition of a progestogen for at cramps (rule out venous thrombosis); vaginal abdominal complaints. Monitor patient with alone is recommended). The estrogen-only
least 12 days per month greatly reduces the candidiasis; contact lenses may irritate. diabetes (need for oral antidiabetics or insulin preparation is unsuitable for long-term use
additional risk. Advice to patients: Photosensitivity may can change). alone in women with an intact uterus (for
occur. Women should inform their physicians Adverse effects: Rarely, feeling of tension in whom estrogen-progestogen combination is
About 3 in every 1000 women aged 50–69 the breasts; liver tumours.
if signs or symptoms of any of the following recommended).
years not using HRT have ovarian cancer Dose: By slow I.M. injection only, Primary
occur: Thromboembolic or thrombotic dis- Adverse effects: Nausea, vomiting, anorexia,
diagnosed over 5 years; this figure rises by and secondary amenorrhoea, initially
orders including sudden severe headache bloating, breast enlargement and tenderness,
about 1 additional case in 1000 in those using 20 mg on 1st day; 10 mg on 14th
or vomiting, disturbance of vision or speech, peripheral oedema, headache, increased libido,
estrogen-only HRT for 5 years; the risks in day with 5 mg Oral Norethisterone
loss of vision, numbness or weakness in an migraine, dizziness, cholestatic jaundice, rash,
women using an estrogen and a progestogen 2-3 times daily from the 19th to the
extremity, sharp or crushing chest pain, calf depression.
are unknown. 26th day of treatment (withdrawal
pain, shortness of breath, severe abdominal Advice to patients: See under Ethinylestradiol
HRT does not provide contraception. If a pain or mass, mental depression or unusual bleeding starts about 28th day). In Nursing action: See under Ethinyloestradiol.
potentially fertile woman needs to use HRT, bleeding. Women should discontinue taking place of Norethisterone, 250 mg IM Dose: See under preparations below.
non-hormonal contraceptive measures are the medication if they suspect they are preg- Hydroxyprogesterone may be given
POM PREMARIN®
necessary. nant or become pregnant. on the 14th day. Tablets, Conjugated estrogen 0.625 mg (maroon),
Precautions for patients on HRT undergoing Nursing action: Give at bedtime to minimise Continuation of therapy (over min- 1.25 mg (yellow), 2.4 mg (purple); all ‘s-c’ tabs.
surgery and reasons to stop HRT are the same occurrence of adverse effects; teach patient imum 2-3 cycles), 10 mg on the 6th
as those for hormonal contraceptives (see self-examination of the breasts. and 16th day of the artificial cycle; 10.4.2 Progestogens (Female
notes in section 11.3.1). • Explain to patient on cyclic therapy for postmen- then, by mouth, 5 mg Norethister- sex hormones)
opausal symptoms that, although withdrawal one 2 times daily from the 19th to
the 26th day of the cycle. In place of Progesterone is a hormone secreted by
ETHINYLESTRADIOL bleeding may occur during week off drug, fertility
has not been restored. Pregnancy cannot occur Norethisterone, 250 mg IM Hydroxy- the corpus luteum whose actions include
Indications: Hormone replacement for men- induction of secretory changes in the endo-
since she has not ovulated. progesterone may be given on the
opausal symptoms; osteoporosis prophylaxis; metrium, relaxation of uterine smooth muscle
Dose: Hormone replacement, by mouth, 16th day together with the 10 mg
palliation in prostate cancer; contraception and production of changes in the vaginal
ADULT (female) 10–20 µg daily (with Estradiol.
in combination with a progestogen (section
534 | 10.4.2 Progestogens (Female sex hormones) 10.4.2 Progestogens (Female sex hormones) | 535
epithelium. Progesterone is relatively inactive culinisation of the female foetus. to 10 days beginning on day 16 to 21 POM NORISTERAT® (SFH)
following oral administration and produces • Instruct patient to report breast pain or tenderness, of cycle for 2 cycles. Injection, Norethisterone enanthate 200 mg; oily
local reactions at site of injection. This has led vaginal discharge or bleeding, swelling of hand or Secondary amenorrhoea, by mouth, solution in 1-mL amp.
to the development of synthetic progestogens feet, visual disturbances or migraine. ADULT 2.5–10 mg daily for 5–10 days POM PRIMOLUT N® (Bayer Schering)
• Teach patient self-examination of the breasts.
including levonorgestrel, norethisterone beginning on day 16 to 21 of cycle for Tablet, Norethisterone 5 mg, white tab. marked ‘AN’
• Inform patient that normal menstruation may not
and medroxyprogesterone. resume for 2-3 months after drug therapy. 3 cycles. in a hexagon.
Endometrial cancer, by mouth, ADULT 5 mg – 30.
Where endometriosis requires drug treatment, Dose: By I.M. injection, Habitual abortion, as
it may respond to a synthetic progestogen soon as pregnancy is diagnosed 250- 200–400 mg daily.
PROGESTERONE
given on a continuous basis. A progestogen 500 mg at weekly intervals during the POM Medroxyprogesterone (WMF 18.5)
may also be used for the treatment of severe initial months or as needed. Tablet, Medroxyprogesterone acetate 5 mg POM CYCLOGEST® (Alpha)
dysmenorrhoea but where contraception is Threatened abortion, initially 500 mg Pessaries, Progesterone 200 mg, 400 mg.
also required the best choice is a combined 2-3 times weekly until the bleeding NORETHISTERONE 200 mg – 15’s
oral contraceptive. In postmenopausal women ceases; then 250 mg twice weekly 400 mg – 15’s
Therapeutic category: Oral progestogen
Indications: Premenstrual syndrome; postnatal
receiving long-term estrogen therapy for until patient remains free from Indications: Endometriosis; menorrhagia; depression. Establishment & maintenance of
hormone replacement, a progestogen needs complaints. severe dysmenorrhoea; contraception (section pregnancy in women undergoing IVF or Embryo
to be added for women with an intact uterus Infertility due to corpus luteum insuffi- 11.3.1); HRT (section 10.4.1). transfer process.
to prevent hyperplasia of the endometrium ciency, 250 mg about 3 days after the Contra-indications: Pregnancy (Appendix
(section 10.4.1). Progestogens have been rise in basal body temperature; then, POM DEXPORIN® (Vixa)
2); undiagnosed vaginal bleeding; hepatic
Injection, Progesterone 25 mg per mL; in 1-mL amp.
used for the treatment of menorrhagia, but 5-10 mg I.M. Estradiol may be added impairment or active liver disease (Appendix Indications: Imminent and habitual abortion of
they are not as effective as tranexamic acid due to a likely coexisting oestrogen 5); severe arterial disease; breast or genital hormonal origin, prolonged menorrhoea and
[not included on WHO Model List]; mefenamic deficiency. tract cancer; porphyria; history in pregnancy
EMDEX
hypermenorrhoea due to defective corpus luteum
acid [not included on WHO Model List] is par- Primary and secondary amenorrhoea, of idiopathic jaundice, severe pruritus or pem- formation, irregular menstruation or polymenor-
ticularly useful where dysmenorrhoea is also a See under Estradiol in Section 10.4.1. phigoid gestationis. rhoea. Generally, in uterine bleeding due to defi-
problem. Medroxyprogesterone is also used in Precautions: Epilepsy; migraine; diabetes ciency of corpus luteum hormone (haemorrhagic
POM PRIMOLUT Depot® (Bayer Schering)
the treatment of endometrial cancer. mellitus; hypertension; cardiac or renal disease metropathy).
Injection, (Depot), Hydroxyprogesterone hexanoate
and those susceptible to thromboembolism; Dose: See lit for details.
Progestogens are also used in combined oral 250 mg per mL.
contraceptives and progestogen-only contra- Pack: 250 mg/mL amp. depression; breastfeeding (Appendix 3); in- POM Progesterone (Mark)
ceptives (section 11.3.1). teractions: Appendix 1. Injection, Progesterone 25 mg per mL
MEDROXYPROGESTERONE Adverse effects: Acne, urticaria, fluid retention, Pack: 10’s (in ampoules)
weight increase, GI disturbances, changes in Indications: In amenorrhea and abnormal uterine
HYDROXYPROGESTERONE Indications: Endometriosis; dysfunctional
bleeding due to hormonal imbalance in the absence
Therapeutic category: Parenteral proges- uterine bleeding; secondary amenorrhoea; libido, breast discomfort, premenstrual symp-
of organic pathology, such as sub-mucous fibroids
togen. endometrial cancer; contraception (section toms, irregular menstrual cycles, depression, or uterine cancer.
Indications: Habitual and threatened abortion, 11.3.1); adjunct in HRT (section 10.4.1). insomnia, somnolence, headache, dizziness, Dose: By IM injection, Amenorrhea, 5-10 mg daily
infertility due to corpus-luteum insufficiency, Contra-indications: Pregnancy (Appendix 2); alopecia, hirsutism, anaphylactoid-like reac- for 6-8 consecutive days. If there has been
primary and secondary amenorrhoea, uterine hormone-dependent breast or genital neo- tions; exacerbation of epilepsy and migraine; sufficient ovarian activity to produce a
hypoplasia. plasms; undiagnosed vaginal bleeding; hepatic rarely jaundice. prolliferative endometrium, one can expect
Contra-indications: A history of herpes of impairment or active liver disease (Appendix 5); Dose: Endometriosis, by mouth, ADULT withdrawal bleeding 48-72 hours after the
severe arterial disease; porphyria. (female) 10 mg daily starting on fifth last injection. This may be followed by
pregnancy, history of or existing liver tumours. spontaneous normal cycles.
Precautions: General medical and gynaeco- Precautions: Small increase in possible risk of day of cycle (increased if spotting
Functional uterine bleeding, 5-10 mg daily
logical examination (including the breasts) to breast cancer; migraine; depression; thrombo- occurs to 20–25 mg daily, reduced
for 6 doses. Bleeding may be expected to
exclude herpes of pregnancy, liver tumours, embolic or coronary vascular disease; diabetes once bleeding has stopped). cease within 6 days. When estrogen is given
diabetic women. mellitus; trophoblastic disease; hypertension; Menorrhagia, by mouth, ADULT as well, the administration of Progesterone
Interactions: Insulin and antidiabetic require- renal disease; breastfeeding (Appendix 3); (female) 5 mg three times daily for is begun after two weeks of estrogen ther-
ments may change. interactions: Appendix 1. 10 days to stop bleeding; to prevent apy. If menstrual flow begins during the
Advice to patients: Take this medicine only Adverse effects: Acne, urticaria, fluid reten- bleeding 5 mg twice daily from day course of injections of progesterone, they
tion, weight gain, GI disturbances, changes 19 to 26 of cycle. are discontinued.
as directed; do not exceed recommended May be irritating at the site of injection.
dosage nor take it for a longer period of time; in libido, breast discomfort, premenstrual Dysmenorrhoea, by mouth, ADULT
if you suspect you may have become pregnant, symptoms, irregular menstrual cycles; de- (female) 5 mg 2–3 times daily from POM MECPRO® (Bakangizo)
stop taking this medicine; take with food; no- pression, insomnia, somnolence, headache, day 5 to 24 for 3 to 4 cycles. Capsules, Progesterone (micronised) 100 mg, 200
alopecia, hirsutism; anaphylactoid reactions; mg, 400 mg; soft gelatin cap.
tify physician of pain in the calves along with POM Norethisterone (WMF 18.5)
rarely jaundice. 100 mg – 1 x 10’s (in blisters)
swelling and warmth, severe headache, visual Tablet, Norethisterone 5 mg.
disturbance. Dose: Mild to moderate endometriosis, by
POM Norethisterone (EDL 21.3.2) 400 mg – 1 x 10’s (in blisters)
Nursing action: Administer oily solution deep mouth, ADULT 10 mg 3 times daily for
Injection, Norethisterone enantate 200 mg per mL;
into the gluteal muscle; rotate the sites. 90 consecutive days, beginning on in 1-mL amp.
• Advise patient never to use drug to induce with- day 1 of cycle.
drawal bleeding or test for pregnancy, because Dysfunctional uterine bleeding, by POM NORELUT® (Hovid)
Tablet, Norethisterone 5 mg.
drug may cause defects in the newborn or mas- mouth, ADULT 2.5–10 mg daily for 5
5 mg – 500; 1000.
536 | 10.4.3 Androgens (Male sex hormones) 10.5 Drugs acting on pituitary ovarian axis | 537
10.4.3 Androgens (Male prostate cancer, headache, depression, gas- every 2-3 weeks.Aplastic anaemia, 250 mg this treatment. Most patients who are going to
every 2-3 weeks. respond will do so to the first course; 3 courses
sex hormones) trointestinal bleeding, nausea, polycythaemia,
cholestatic jaundice, changes in libido, gy- POM RICOSTRONE® (GoldMoore) should be adequate; long-term cyclical therapy
Androgens are secreted by the testes and less (more than 6 cycles) is not recommended as it
naecomastia, anxiety, asthenia, paraesthesia; Injection, Testosterone propionate 25 mg; in 1-mL
potent androgens by the adrenal cortex and amp. may increase risk of ovarian cancer.
ovaries. In the male, they are responsible for the electrolyte disturbances including sodium
retention with oedema and hypercalcaemia, Pack: 100 x 1-mL.
development and maintenance of the sex or- CLOMIFENE
gans and the secondary sexual characteristics, hypertension, weight gain; increased bone POM Testosterone (Alpha)
normal reproductive function, and sexual per- growth; androgenic effects such as hirsutism, Injection, Testosterone enantate 250 mg per mL; oily Clomifene citrate is a complementary drug for fertility
male-pattern baldness, seborrhoea, acne, pru- solution in 1-mL amp. treatment.
formance ability in addition to stimulating the
growth and development of the skeleton and ritus, priapism, precocious sexual development
MESTEROLONE Synonym: Clomiphene
skeletal muscle during puberty. At high doses and premature closure of epiphyses in prepu-
Indications: Anovulatory infertility.
in the normal male androgens inhibit pituitary bertal males, virilism in females, and suppression Therapeutic category: Oral Androgen.
Contra-indications: Hepatic disease; ovarian
gonadotrophin secretion and depress spermat- of spermatogenesis in men; rarely liver tumours; Indications: Orally active androgen indicated
cysts; hormone dependent tumours or uterine
ogenesis. Testosterone is used as replacement sleep apnoea also reported. in hypogonadism, infertility, potency dis-
bleeding of undetermined cause; pregnancy
therapy in those who are hypogonadal due to Nursing action: Store IM preparation at room turbance, reduced efficiency in middle and
(exclude before treatment, Appendix 2).
either pituitary (secondary hypogonadism) or temperature; warming injection to room tem- advanced age.
Precautions: Visual disturbances (discontinue
testicular disease (primary hypogonadism). perature and shaking vial will help redissolve Contra-indications, Precautions: See under
and initiate eye examination) and ovarian
Androgens are useless as a treatment of im- crystals that may have formed after storage. Testosterone.
hyperstimulation syndrome (discontinue treat-
potence and impaired spermatogenesis unless
• Administer by deep IM injection into the upper Adverse effects: Rarely benign and malignant
outer quadrant of the gluteus maximus; report ment immediately); polycystic ovary syndrome
there is associated hypogonadism; they should liver tumours. Frequent or persistent erections
soreness at injection site. (cysts may enlarge during treatment); uterine
may occur (reduce dose or discontinue).
EMDEX
not be given until the hypogonadism has been • Monitor for signs of hypoglycaemia; advise patient fibroids, ectopic pregnancy, incidence of
properly investigated and treatment should al- Dose: By mouth, Adult, Androgen deficiency
to report such signs immediately they occur. multiple births increased (consider ultrasound
ways be under expert supervision. When given and male infertility associated with
• Provide diet with increased calories and protein; monitoring); breastfeeding (Appendix 3).
to patients with hypopituitarism they can lead reduce sodium if oedema occurs. hypogonadism, 25 mg 3-4 times daily
Adverse effects: Visual disturbances, ovarian
to normal sexual development and potency • For therapeutic response in breast cancer, 1 to 3 for several months.
hyperstimulation, hot flushes, abdominal
but not fertility. If fertility is desired, the usual months course is necessary; report if the disease Maintenance: 50-75 mg daily in
discomfort, occasional nausea and vomiting,
treatment is with gonadotrophins or pulsatile progresses. divided doses
• Periodic liver function tests should be performed. depression, insomnia, breast tenderness,
gonadotrophin-releasing hormone which will Potency disturbances and diminishing
Dose: Hypogonadism, by slow IM injection, headache, intermenstrual spotting, menorrha-
stimulate spermatogenesis as well as androgen efficiency, initially 25 mg 3 times
ADULT (males), initially 200–250 gia, endometriosis, convulsions, weight gain,
production. Androgens cannot induce fertility daily; may be reduced according to
mg every 2–3 weeks; maintenance rashes, dizziness and hair loss.
in men with primary hypogonadism. Caution patient’s need. Maintenance: 25 mg
200–250 mg every 3–6 weeks. Advice to patients: May cause visual distur-
should be used in treating boys with delayed 1-2 times daily for several months.
Breast cancer, by slow IM injection, bances, dizziness, lightheadedness; if possi-
puberty with excessive doses of testosterone Not recommended for children.
ADULT (females) 250 mg every 2–3 bility of pregnancy, stop the drug and consult
since the fusion of epiphyses is hastened POM Mesterolone (EDL 21.7/Restricted List) your physician.
weeks. Tablet, Mesterolone 25 mg.
and may result in short stature. Androgens, Nursing action: Ovulation is assessed by basal
including testosterone have also been used POM Testosterone (WMF 18.2) POM PROVIRON® (Bayer Schering) body temperature or serum progesterone 2
in postmenopausal women for the palliative Injection, Testosterone (as enantate) 200 mg/mL; in Tablet, Mesterolone 25 mg. weeks after last clomifene dose; teach patient
treatment of androgen-responsive, advanced, 1-mL ampoule. 25 mg – 20. how ovulation can be determined (there is a
metastatic breast cancer; care is required to POM Testosterone (EDL 21.7/Restricted List) slight decrease in temperature, then a sharp
prevent masculinizing effects. Injection, Testosterone 200 mg per mL; oily in 1-mL 10.5 Drugs acting on pituitary increase for ovulation); reassure patient that
amp. ovarian axis generally ovulation occurs after first course
TESTOSTERONE POM PRIMOTESTON® (CHI/Schering) of therapy but if pregnancy does not occur,
10.5.1 Anti-estrogens (Ovulation inducers)
Indications: Hypogonadism; palliative treat- Injection, Testosterone propionate 25 mg per mL; 10.5.2 Anterior pituitary hormones (Gonadotro- course of therapy may be repeated twice.
ment of advanced breast cancer in women. oily in 1-mL amp. phins) • Advise patient to attempt coitus 3 days before and
Contra-indications: Breast cancer in men, Dose: By IM injection, Androgen deficiency, 50 mg 10.5.3 Posterior pituitary hormones every other day after ovulation.
prostate cancer, hypercalcaemia, pregnancy 2-3 times weekly. Delayed puberty, 50 mg • Caution patient not to perform hazardous task
weekly. Breast cancer, 100 mg 2-3 times because drug may cause dizziness or visual dis-
(Appendix 2), breastfeeding (Appendix 3),
weekly.
10.5.1 Anti-estrogens
turbances.
nephrotic syndrome, history of primary liver (Ovulation inducers) • Advise patient to stop drug and inform physician
tumours. POM PRIMOTESTON Depot®(CHI/Schering)
The anti-estrogen, clomifene is used in the if pregnancy is suspected.
Precautions: Cardiac, renal or hepatic impair- Injection, (Depot), Testosterone enanthate 250 mg
per mL. treatment of female infertility due to distur- • Tell patient that multiple births are common and
ment (Appendix 5), elderly, ischaemic heart bances in ovulation. It induces gonadotrophin that risk increases with high doses of drug.
Pack: 250 mg/mL amp.
disease, hypertension, epilepsy, migraine, release by occupying estrogen receptors in the • Advise patient to stop drug and report immediately
Dose: By slow IM injection, Male hypogonadism,
diabetes mellitus, skeletal metastases (risk of if abdominal symptoms or pain occurs; may indi-
initially 250 mg every 2-3 weeks; mainte- hypothalamus, thereby interfering with feed-
hypercalcaemia); regular examination of pros- cate ovarian enlargement or ovarian cyst.
nance, 250 mg every 3-6 weeks. Potency back mechanisms. Patients should be carefully
tate and breast during treatment; prepubertal disorders, initially 100 mg, followed by Dose: Anovulatory infertility, by mouth,
counselled and should be fully aware of the
boys; interactions: Appendix 1. another 100 mg after 1 week; then 100 mg ADULT (female) 50 mg daily for 5
potential adverse effects, including a risk of
Adverse effects: Prostate abnormalities and every 2-4 weeks. Male climacteric, 100 mg days, starting within 5 days of onset
multiple pregnancy (rarely more than twins), of
538 | 10.5.2 Anterior pituitary hormones (Gonadotrophins) 10.5.2 Anterior pituitary hormones (Gonadotrophins) | 539
of menstruation, preferably on the in the treatment of oligospermia associated POM DICLAIR®-HP-HCG (Mark) gonadotrophin levels indicating primary
second day, or at any time if cycles with hypopituitarism. Their use in primary Injection, Human Chorionic Gonadotrophin 2,000 IU, testicular failure.
have ceased; a second course of 100 gonadal failure is not justified. HCG has also 5,000 IU, 10,000 IU; freeze dried, sterile powder for Precautions: Ovarian enlargement (use the
mg daily for 5 days may be given in been used in delayed puberty in the male to reconstitution in amp. lowest possible dose); multiple pregnancy
Pack: 1’s (in amp.) + Solvent.
the absence of ovulation. stimulate endogenous testosterone produc- (advise patient on the frequency and potential
Indications & Dose: The freeze dried powder should
POM Clomifene (WMF 18.6)
tion, but has little advantage over testosterone. be reconstituted with the solvent provided hazards).
Tablet, Clomifene citrate 50 mg HCG is well absorbed after I.M. administration and the solution injected immediately. By Adverse effects: Gynaecomastia, ovarian en-
and has a biologic half-life of 8 hours, com- SC or IM injection, In females: Anovulatory largement, abdominal distension, pain/rash at
POM Clomifene (EDL 21.5) infertility, 5,000-10,000 IU given 3 days after injection site, multiple pregnancy.
Tablet, Clomifene (as citrate) 50 mg. pared to 30 minutes for LH.
completion of a recommended course of Advice to patients: Multiple ovulations result-
POM CLIFEN® (Pharmabox) Menotrophin or Clomiphene (given to cre- ing in plural gestations have been reported.
HUMAN CHORIONIC GONADOTROPHIN
Tablet, Clomifene citrate 50 mg; light-yellow f-c ate prior stimulation of follicular maturation Nursing action: Administer by deep I.M. after
oval tab. Synonym: Chorionic Gonadotrophin, CG; HCG. and endometrial proliferation). Up to three
reconstituting with 1-2 mL of normal saline
50 mg – 10’s. Indications: In women, primary amenorrhoea, repeat injections of 5,000 IU may be given
injection, use immediately; rotate injection site
secondary amenorrhoea over about 6 months, within 9 days following the first injection to
POM CLOPINAX® (Pharmabase) prevent insufficiency of the corpus luteum. to prevent muscle atrophy.
post partum amenorrhoea, infertility due to a
Tablet, Clomiphene citrate 50 mg Habitual abortion, once pregnancy is con- • Inform patient of the frequency and potential
50 mg – 10’s (in blister) shortened corpus luteum phase. hazards of multiple pregnancy; in the treatment
In boys and men, cryptorchidism in boys firmed, inject 5,000 IU per day on three alter-
nate days. From the 9th day of the first injec- of infertility, encourage patient to have daily in-
POM IKACLOMIN® (Dizpharm) of six years and older, secondary hypo-
tion, inject 2,000 IU twice a week till the 14th tercourse from the day before drug is given until
Tablet, Clomifene citrate 50 mg gonadism, delayed puberty, impotentia week of pregnancy. By SC or IM injection, In ovulation occurs (pregnancy usually occurs 4-6
50 mg – 10’s.
coeundi. males: Hypogonadotrophic hypogonadism, weeks after therapy).
POM OVUMINE® 50 (Carrot-Top) Contra-indications: Carcinoma of the prostate. • Instruct patient to report severe abdominal
EMDEX
500-1,000 IU 2-3 times a week. Sterility due
Tablet, Clomifene citrate 50 mg Precautions: In male, latent or overt cardiac to deficient spermatogenesis, 2,000 IU 2-3 pain, bloating, swelling of hands or feet, nausea,
failure, renal dysfunction, hypertension, times a week in combination with meno- vomiting, diarrhoea, substantial weight gain or
10.5.2 Anterior pituitary hormones trophin. Menotrophin may be given daily shortness of breath.
epilepsy or migraine (or a history of these
(Gonadotrophins) or 2-3 times a week. The combined therapy Dose: By deep IM injection, according to
conditions). In female, pregnancies occuring
should continue for at least 4 months. patient’s response.
The Gonadotrophins, Luteinizing hormone after ovulation induction may increase the risk
Cryptorchidism (not due to anatomical ob-
(LH) and Follicle-stimulating hormone of miscariage and multiplets. POM Follicle-stimulating Hormone (FSH) plus
struction), 500-1,000 IU on alternate days
(FSH), are secreted by the anterior pituitary in Adverse effects: Oedema, headache, tired- Luteinising Hormone (LH) (EDL 21.5/Restricted List)
for several weeks.
ness, mood changes, local reactions; sexual Injection, Human FSH 75 units, human LH 75 units;
response to hypothalamic gonadotrophin-re-
POM IVF-C® (Alpha) powder for reconstitution.
leasing hormone (GNRH). precocity.
Injection, HCG 5000 IU; white to almost white
Advice to patients: Discontinue immediately POM DICLAIR®-HP-HMG (Mark)
Human gonadotrophins are available as: lyophilized powder in a colourless transparent
if pregnancy is suspected. Injection, Highly Purified Human Follicle Stimulating
• Human menopausal gonadotrophin (HMG), green vial.
Nursing action: Administer I.M., and rotate Hormone (FSH) 75 or 150 I.U. plus Highly Purified
or menotrophin which is an extract of the urine Pack: 1 x 3’s
injection site to prevent muscle atrophy. Human Luteinising Hormone (LH) 75 or 150 I.U.;
of postmenopausal women containing primarily
• Administer usually after failure of clomifene in ano- Gonadorelin releasing Hormone freeze dried, sterile and pyrogen free powder for
follicle-stimulating hormone (with luteinising
vulatory patients; in infertility, encourage patients analogue (GnRH-analogue) reconstitution in amp.
hormone), and Human chorionic gonadotrophin
to have sexual intercourse from the day before HCG Pack: 1’s (in amp.) + 1 mL isotonic Sodium Chloride
(HCG) or chorionic gonadotrophin which is a Leuprorelin
therapy until ovulation occurs; inform patient that (as solvent in amp.).
preparation of a glycol-protein fraction secreted
when used with menotrophins to induce ovulation, POM LUPHERE® (Alpha) Indications: Follicle stimulation in females with ano-
by the placenta and obtained from the urine of
multiple pregnancy/births are possible; Injection (deopt), Leuprorelin acetate 3.75 mg; vulatory infertility; Stimulation of spermatogenesis
pregnant women having the action of the pituitary
• Instruct patient to report facial, axillary and pubic powder for injection with solvent presyringed with in males with oligospermia.
luteinizing hormone.
hair changes, change in voice, penile enlarge- 23-G needle. Dose: The powder in the ampoule should be recon-
In both male and female, HMG or menotrophin ment, acne, abdominal pain, distension and vag- stituted with the solvent provided just prior
See lit. for more information.
(i.e., FSH plus LH) must be used in conjunction inal bleeding in female patient, bloating, nausea, to use. By SC or IM injection, In Females:
with a LH, i.e., HCG, to permit ovulation and vomiting and diarrhoea; be alert for symptoms of Two dosage schedules may be employed.
implantation in women and testosterone ectopic pregnancy. FOLLICLE-STIMULATING HORMONE Schedule 1. Alternate day therapy: Three equal
plus LUTEINISING HORMONE doses of Diclair-HP-HMG are given on alternate
production and full masculinisation in men. Dose: By IM or SC injection, according to
Synonym: Human Menopausal Gonadotro- days, in the first half (proliferative phase) of the
HMG or menotrophin is given to stimulate patient’s response. menstrual cycle. This is followed by a single dose
follicular growth and maturation and bring phin; Menotropin (i.e., the 1:1 ratio)
POM Human Chorionic Gonadotrophin (EDL 21.5/ of 5,000 I.U. Diclair-HP-HCG given one week after
oestrogen levels into the optimum range Indications: Sequentially with HCG to induce
Restricted List) the first injection of Diclair-HP-HMG provided the
for ovulation. HCG is then given to stimulate ovulation and pregnancy in the infertile
Injection, Chorionic gonadotrophin 500 units, 1000 clinical and biochemical responses are adequate
ovulation. There is a risk of multiple pregnancy woman with functional anovulation; used and not excessive.
units; powder for injection in amps.
and the abortion rate may be higher than with with HCG in men to stimulate spermatogene- Schedule 2. Daily therapy: Daily injection of Di-
POM CHORAGON® (Alpha) sis in those with primary hypogonadotrophic clair-HP-HMG is given until an adequate response
pregnancy following spontaneous ovulation. Injection, HCG 5000 I.U.; in amp.
Hyperstimulation of the ovaries causes ovarian hypogonadism. is achieved. This is judged on the basis of daily
enlargement and if severe, ascites, pleural effu- POM CHORIGON® (Dizpharm) Contra-indications: Primary ovarian failure, oestrogen determinations or Sonography. In the
Injection, Chorionic gonadotrophin 2500 I.U., 5000 overt thyroid and adrenal dysfunction, abnor- absence of a response the dose of Diclair-HP-HMG
sion, electrolyte imbalance and hypovolaemia. may be increased or the course may have to be
I.U. mal bleeding, pregnancy, men with normal
The gonadotrophins are also occasionally used urine gonadotrophin concentrations, elevated abandoned. A single injection of 5,000 to 10,000
540 | 10.5.2 Anterior pituitary hormones (Gonadotrophins) 10.5.3 Posterior pituitary hormones | 541
I.U. Diclair-HP-HCG is administered 24 to 48 hours days 2 to 5 of the cycle. Max. 450 IU with pregnancy; fibroid tumours of the uterus is obtained, stop treatment and with-
after the last dose of Diclair-HP-HMG. daily. incompartible with pregnancy. hold hCG; treatment should recom-
By SC or IM injection, In males: In the Treatment is continued until ade- Precautions: Adhere to the recommended mence in the next cycle at a dosage
treatment of oligospermia, 1 ampoule of quate follicular development has dosage and monitor patient closely to avoid lower than that of the previous cycle.
Diclair-HP-HMG is given 3 times a week been achieved. A single injection ovarian hyperstimulation syndrome which oc- Women undergoing superovulation for
in combination with Diclair-HP-HCG 2000 upto 10,000IU hCG (Human Chorionic curs usually 1 to 2 weeks following hCG admin- in-vitro fertilisation and other assisted
I.U., 2-3 times a week. The combined therapy Gondadotropin) is administered istration and ovulation. In case of symptoms conception techniques,usually 150-225
should continue for at least 4 months. In 48 hours after the last Follitropin such as pelvic pain, abdominal distension or IU daily (commencing on day 2 or 3
men, elevated androgenous/FSH levels are injection. ovarian enlargement or if oestrogen assays or of the cycle); doage may be adjusted
indicative of primary testicular failure. Such ultrasound examination suggest an excessive according to the patient’s response
POM FOLLITROPE® (Alpha)
patients are usually unresponsive to Diclair- oestrogen response, urofollitropin administra- up to a maximum of 450 IU daily.
Injections, Recombitant follicle stimulating hormone
HP-HMG/Diclair-HP-HCG therapy. (FSH) 75 IU, 150 IU; white lyophilized powder in vials. tion should be discontinued and hCG should Treatment should be continued until
POM IVF-M® (Alpha) 75 IU – 1’s + Solvent (in vials) not be administered and intercourse avoided adequate follicular development is
Injection, FSH 75 IU, LH 75 IU; white to almost white 150 IU – 1’s + Solvent (in vials) in order to prevent ovarian hyperstimulation. achieved. A single injection of up to
powder. Symptoms such as ascites, pericardial effusion, 10,000 IU hCG is given 24-48 hours
Pack: 75 IU x 1’s + Solvent (in vials) EPIMESTROL hydrothorax, haemo-concentration, secondary after the last urofollitropin injection
POM MENOGON® (Alpha) hyperaldosteronism or hypercoagulability to induce follicular maturation.
POM Epimestrol (EDL 21.5/Restricted List)
Injection, Menotropin (equiv. to human FSH 75 I.U. should be controlled through appropriate Note: The powder should be reconstituted imme-
Tablet, Epimestrol 5 mg.
plus human LH 75 I.U.); powder for injection in vial measures, including avoidance of unnecessary diately prior to use with the solvent provided. In
plus 1 mL solvent. pelvic examination. order to avoid the injection of large volumes, up to
UROFOLLITROPIN (FSH) 5 ampoules of urofollitropin may be dissolved in 1
POM MENOPUR® (Alpha) Interactions: Co-administration with clomi-
Synonym: Urofollitrophin.
EMDEX
mL of solvent. An unused reconstituted material
Injection, Highly purified human FSH 75 I.U. plus LH phene citrate may potentiate the follicular
Pharmacology: Urofollitropin is obtained should be discarded.
75 I.U.; powder for injection in vials plus solvent. response, whereas concurrent use of GnRH
from human menopausal urine, with only FSH POM DICLAIR-HP-FSH® (Mark)
agonist-induced pituitary desensitisation may
POM PERGONAL® (Dizpharm) activity. Human menopausal gonadotrophin Injection, Urofollitrophin 75 IU, 150 IU; powder for
increase the dosage of urofollitropin needed
Injection, Menotropin (equiv. to human FSH 75 I.U. (HMG) exerts FSH and LH activities. For this reconstitution in amps. plus 1 mL solvent.
plus human LH 75 I.U.); powder in amp. plus 1 mL to elicit an adequate ovarian response. Avoid
reason, HMG is indicated in hypogonatropic Pack: 1 amp (freeze dried, sterile powder) + 1 amp.
solvent. mixing with other drugs in the same syringe. solvent (0.9% NaCl).
hypopituitarism (WHO Group I patients), where
Pack: 5. Adverse effects: Local reactions at the injec-
both gonadotrophin secretions are needed. POM METRODIN HP ®(Dizpharm)
tion site, fever and arthralgias; GI symptoms,
In patients showing normal or high LH levels Injection, Urofollitropin 75 IU, 150 IU; powder for
HUMAN FOLLICLE STIMULATING bloating of the stomach, pelvic pain or sore
HORMONE (FSH) (WHO Group II), selective FSH deficiencies reconstitution in amps. plus 1 mL solvent.
breasts; mild to moderate ovarian enlarge-
Synonyms: Follitropin beta; hFSH require availability of preparations without LH Pack: 1’s; 10’s.
ment, ovarian cysts; rarely severe hyperstimu-
Indications: Treatment of female infertility in activity; this characteristic belongs to FSH. FSH
lation syndrome, arterial thrombo-embolisms;
controlled ovarian hyperstimulation to induce stimulates both the growth and maturation of 10.5.3 Posterior pituitary hormones
few incidence of multiple births; pregnancy
the development of multiple follicles in med- follicles; it induces the secretion of oestrogens The hormones secreted by the posterior pitu-
wastage by miscarriage or abortion especially
ically assisted reproduction program (e.g. in and a proliferation of the endometrium. itary are vasopressin (antidiuretic hormone,
in women with other fertility problems; ectopic
vitro fertilization/embryo transfer). Indications: Stimulation of follicular growth ADH) and Oxytocin. Oxytocin is used in ob-
pregnancy especially in women with history of
Contra-indications: Tumors of the ovary, in infertile women. A course of Urofollitropin stetrics (see section 11.1).
prior tubal disease.
breast, uterus, hypothalamus or pituitary gland; is usually followed by human chorionic gon-
Dose: By SC or IM injection, Adult, Women Diabetes Insipidus: Underproduction of ADH
Pregnancy and lactation; Undiagnosed vaginal adotrophin (hCG) to induce ovulation. It is
with hypothalamic-pituitary dysfunc- causes pituitary (cranial) diabetes insipidus,
bleeding; Primary ovarian failure; Ovarian cysts used: (a) For single follicular development in
tion who present with either oligom- which is characterized by the passage of
or enlarged ovaries, not related to polycystic cases such as hypothalamic pituitary dysfunc-
enorrhoea or amenorrhoea (WHO large volumes of urine of low osmolality, and
ovarian disease (PCOD); Malformations of the tion (WHO Group II classification), including
Group II), usually 75-150 IU daily polydipsia. Treatment is by hormone replace-
sexual organs incompatible with pregnancy; patients with polycystic ovarian disease; (b)
(commencing within the first 7 days ment, although mild cases of cranial diabetes
Fibroid tumors of the uterus incompatible For multiple follicular development (assisted
of the menstrual cycle for menstruat- insipidus may respond to chlorpropamide 250
with pregnancy; Uncontrolled non-gonadol conception techniques); incases such as tubal
ing patients); increased or decreased mg daily or carbamazepine 200-400 mg daily.
endocrinopathies (e.g. thyroid, adrenal or occlusion, unexplained infertility and male
by up to 75 IU/day at 7 or 14 day These drugs sensitize the renal tubule to the
pituitary disorders) factor infertility.
intervals if necessary to obtain an ad- action of remaining endogenous vasopressin.
Precautions: Ovarian hyperstimulation (dis- Contra-indications: For safety reasons, avoid
equate, but not excessive, response. If In nephrogenic diabetes insipidus the symp-
continue); higher rate of abortion than normal; in cases of prior hypersensitivity to menotro-
no adequate response after 4 weeks toms of polyuria and polydipsia are due to
ectopic pregnancy. phins; pregnancy; ovarian enlargement or cyst
of treatment, that cycle should be a refractoriness of the kidney to respond to
Adverse effects: Injection site reactions such not due to polycystic ovarian syndrome; gynae-
abandoned. An optimal response the action of vasopressin. In the absence of
as bruising, pain, swelling and itching, which cological haemorrhages of unknown aetiology;
is followed by a single IM injection a correctable cause such as hypokalaemia or
are usually mild and transient. Increased risk of ovarian, uterine or mammary carcinoma. Also
of up to 10,000 IU hCG 24-48 hours hypercalcaemia, patient may benefit from the
ectopic pregnancy and multiple pregnancies. avoid use when an effective response cannot
after the last urofollitropin injection. paradoxical antidiuretic effect of thiazides, e.g.,
Rarely, thromboembolism. be obtained such as in primary ovarian failure
Patient is encouraged to have coitus bendrofluazide 5-10 mg daily; chlorthalidone
Dose: By SC/IM injection, Hyperovulation, (ovarian dysgenesis, premature menopause);
on the day of and that following hCG 100 mg twice daily reduced to maintenance
150-300 IU daily, commencing on malformations of sexual organs incompartible
administration. If excessive response
542 | 10.5.3 Posterior pituitary hormones 10.6 Other Endocrine Drugs | 543
dose of 50 mg daily. ischaemia and infarction. • Teach patient using S.C. desmopression to rotate in stable circulating levels when the drug is
Advice to patients: Side effects such as ab- injection sites to prevent tissue damage. administered twice daily. It is highly concen-
Vasopressin, an octapeptide hormone, has a
dominal cramps and nausea may be reduced Dose: Intranasally, Diagnosis of Diabetes Insip- trated in the liver, adrenals, and kidneys and is
direct anti-diuretic action on the kidneys. It is
by drinking a glass of water with each dose. idus, Adult and child, 20 mcg; limit excreted in both faeces and urine.
the treatment of choice for pituitary diabetes
Nursing action: Assess patient’s B.P. and pulse fluid intake to 500 mL from 1 hour
insipidus. It also constricts peripheral vessels
when giving IM; weigh patient daily. before to 8 hours after administration. BROMOCRIPTINE
and causes contraction of the intestine,
• Observe for signs of IV infiltration and gangrene. Treatment of Diabetes Insipidus, Adult, Therapeutic category: Prolactin inhibitor
gall-bladder, and urinary bladder. It is devoid
• Warn elderly patients not to increase their nor- 10-40 mcg daily in 1-2 divided doses; Indications: Prolactin-dependent menstrual
of oxytocic activity and is ineffective in nephro- mal fluid intake to avoid water intoxication and Child: 5-20 mcg; infants may require cycle disorders such as amenorrhoea, female
genic diabetes insipidus. When other methods hyponatraemia; watch patient for signs of water lower doses. infertility, premenstrual symptoms, hyper-prol-
of treatment fail, bleeding oesophageal varices intoxication viz lethargy, behavioural changes, Primary Nocturnal Enuresis Adult (<65 actinaemia in men, prolactinomas, acromegaly,
may respond to ADH. Here vasopressin (20 disorientation, and neuromuscular excitability.
years) and child (over 5 years), initially inhibition of lactation such as after abortion,
units) is infused over about 5 minutes i.v. and • Check for oedema in extremeties. If water reten-
tion is severe, a diuretic may be prescribed by 20 mcg at bedtime; may be increased benign breast disease; Parkinson’s disease.
may stop the bleeding by causing constriction
the doctor. to 40 mcg if lower dose is not effec- Contra-indications: Hypersensitivity to bro-
of splanchnic arterioles and a reduction in
Dose: By SC or IM injection, Diabetes insipi- tive. Withdraw for at least 1 week for mocriptine or other ergot alkaloids, toxaemia
portal venous pressure.
dus, 5-20 units 4 hourly. reassessment after 3 months. of pregnancy, hypertension postpartum and
Vasopressin is well absorbed from buccal and By SC or IM injection, Diagnosis of
POM Vasopressin (EDL 21.8.1/Restricted List) in the puerperium.
nasal mucosa and may also be given s.c., i.m., Diabetes Insipidus, Adult and Child,
Injection, Vasopressin 20 units per mL; in 1-mL amp. Precautions: Pregnancy; history of psychic or
or i.v. Its plasma half-life is about 15 minutes 2 mcg. severe cardiovascular disorders, patients on
and it is rapidly inactivated by the liver and Treatment of Diabetes Insipidus, Adult,
DESMOPRESSIN drugs that can alter BP should be monitored;
kidneys. Circulating ADH is largely unbound. 1-4 mcg daily; Child: 400 nanograms.
Therapeutic category: Synthetic Vasopressin acromegalic patients with history or evidence
EMDEX
Desmopressin is a synthetic Vasopressin ana- POM Desmopressin (EDL 21.8.1/Restricted List) of peptic ulceration.
Analogue; Antihaemophilic Agent; Haemo-
logue with greater antidiuretic activity, a more Injection, Desmopressin 4 mcg per mL Interactions: Alcohol, erythromycin, CNS
static Agent.
prolonged action and no significant pressor Nasal spray, Desmopressin 10 mcg per metered depressants.
Indications: Treatment of diabetes insipidus
activity. It is given intranasally for maintenance spray. Adverse effects: Orthostatic hypotension, na-
and controlling bleeding in mild to moderate Intranasal solution, Desmopressin 100 mcg per mL
therapy, and by injection in the postoperative sal congestion, nausea, vomiting, somnolence;
haemophilia; also in nocturnal enuresis.
period or in unconscious patients; the injec- POM Desmopressin (Alpha) very rarely constipation, dyspepsia, psych-
Contra-indications: Hypersensitivity to des-
tion is also used for the diagnosis of diabetes Injection,Desmopressin omotor agitation, cold-induced vasospasm;
mopressin or any component; cardiac insuffi-
insipidus. Nasal spray, Desmopressin at high doses, psychic disturbances, fatigue,
ciency and related conditions. Intranasal solution, Desmopressin
Interactions: Drugs known to potentiate the Precautions: Avoid overhydration; renal bladder trouble.
effects of Vasopressin include chlorpropamide, impairment, Cardiovascular disease, hyperten- Advice to patients: See Label 21 in Appendix
clofibrate, and carbamazepine. Inhalation of 10.6 Other Endocrine Drugs A. Take with food or milk; drowsiness com-
sion, elderly, cystic fibrosis.
vasopressin may be ineffective when nasal Interactions: Demeclocycline, lithium (de- Bromocriptine monly occurs upon initiation of therapy; limit
congestion is present. creased ADH effects). Chlorpropamide, flud- use of alcohol; avoid exposure to cold; inci-
Bromocriptine acts as a partial dopamine re-
rocortisone (increased ADH effects). dence of side effects is high with nausea the
ceptor agonist. It inhibits the secretion of the
VASOPRESSIN Adverse effects: Nausea, abdominal cramps, most common; hypotension occurs commonly
anterior pituitary hormone prolactin without
Synonym: Antidiuretic hormone (ADH). headache, dizziness, pain at injection site, with initiation of therapy, usually upon rising
affecting normal levels of other pituitary hor-
Therapeutic category: Anti-diuretic. increase in BP, water intoxication and hypon- after prolonged sitting or lying; discontinue
mones. However, bromocriptine can reduce
Indications: Diabetes insipidus due to a defi- atraemia. immediately if pregnant; may restore fertility;
elevated levels of growth hormone (GH) in
ciency in antidiuretic hormone; bleeding from Advice to patients: Avoid overhydration; women desiring not to become pregnant
patients with acromegaly. It does not have the
oesophageal varices. notify physician if headache, shortness of should use mechanical contraceptive means.
undesirable effects of oestrogens. It normalises
Contra-indications: Vascular disease, chronic breath, heartburn, nausea, abdominal cramps, Nursing action: Give with meals to minimize
the ovarian function, and can be used to pre-
nephritis with nitrogen retention. or vulval pain occur. GI upset.
vent or inhibit physiological lactation and to
• Raise bed rails and institute safety measures; aid
Precautions: Asthma, epilepsy, migraine, heart Nursing action: Advise patient to drink only treat pathological prolactin-related conditions. patient with ambulation, may cause postural
failure; adjust fluid intake to avoid hyponatrae- enough water to satisfy thirst; if water retention Danazol hypotension and drowsiness.
mia and water intoxication; children, elderly, is severe, diuretic may be prescribed. • Advise patient to avoid dizziness and fainting by
pregnancy. • Adjust fluid intake to reduce risk of water intoxication Danazol is a synthetic derivative of ethisterone.
getting up slowly.
Interactions: Drugs known to potentiate the and sodium depletion especially in children and It suppresses the pituitary-gonadal axis by • Since early postpartumm pregnancy can occur, test
effects of Vasopressin include chlorpropamide, elderly, shown by lethargy, behavioural change, inhibiting the output of pituitary gonadotro- for pregnancy every 4 weeks.
clofibrate, and carbamazepine. Inhalation of disorientation, neuromuscular excitability. phins in both male and female. It has neither • Inform patient that it may take between 6-8 weeks
• Nasal congestion, allergic rhinitis, or upper respira- oestrogenic nor progestational activity but for menstruation to be reinstated and galactor-
vasopressin may be ineffective when nasal
tory tract infections may impair drug absorption, possesses mild androgenic activity. The action rhoea to be suppressed.
congestion is present. therefore, advise patient to report such conditions
is reversible; ovulation and cyclic bleeding • In parkinsonism, bromocriptine is usually given
Adverse effects: Hypersensitivity reactions to the physician.
usually return within 60 to 90 days of discon- together with either levodopa alone or levodo-
including bronchial constriction; in large doses • Advise patient not to take OTC products for cough pa-carbidopa combination.
pallor, nausea, eructation, desire to defaecate, since these preparations may contain epinephrine tinuation of therapy.
Dose: By mouth, Menstrual Cycle disorder and
uterine cramps; constriction of coronary arter- which can decrease drug response; do not use Danazol is slowly metabolised in human, female infertility, 1.25 mg 2-3 times
ies, which may cause chest pain, myocardial with alcohol. having a half-life of over 15 hours. This results daily; increased to 2.5 mg 2-3 times
544 | 10.6 Other Endocrine Drugs 10.6 Other Endocrine Drugs | 545
daily, if necessary. DANAZOL to minimise GI symptoms. to ascertain that the patient is not pregnant while
Premenstrual symptoms, 1-2.5 mg Therapeutic category: Gonadotrophin release • Avoid use in women of child-bearing age until on danazol therapy.
daily starting on the 14th day of the inhibitor; Androgen. pregnancy is ruled out. Young girls: Precocious puberty, 100-
cycle; increased in steps of 1.25 mg • Advise patient to have a wash after sexual inter- 400 mg daily, according to patient’s
Indications: Endometriosis, associated infer- course to decrease the signs of vaginitis, and to
daily up to 2.5 mg twice daily until tility; benign breast disease (chronic cystic age and weight.
wear cotton pants. Gynaecomastia, 400 mg daily in up
menstruation sets in. mastitis, virginal breast hyperplasia, mazoplasia, • Advise patient to have routine self-examination
Hyperprolactinaemia in men, 1.25 mg mastodynia); severe cyclical mastalgia with or to 4 divided doses for 6 months
of the breasts.
2-3 times daily; increased gradually to without nodularity unresponsive to counseling • Evaluate signs of virilisation, deepening of voice, (adolescents 200 mg daily, increased
5-10 mg per day or simple analgesics to reduce pain, tenderness decreased libido, facial hair (may not be reversible); to 400 mg daily if no response after 2
Prolactinomas, 1.25 mg 2-3 times and nodularity; dysfunctional uterine bleeding advise patient not to discontinue drug abruptly. months).
daily; increased gradually as required presenting as menorrhagia and associated Dose: Adult females: Endometriosis, 200-800 For pre-operative thinning of endo-
to keep plasma prolactin adequately dysmenorrhoea; preparation for hysteroscopic mg daily in ‘4’ divided doses. Dura- metrium, 400-800 mg daily in up to 4
suppressed (occasionally up to 30 endometrial ablation to thin the endometrium tion: 3-6 months uninterrupted but divided doses for 3-6 weeks.
mg daily). and facilitate surgery; severe symptomatic gy- may be extended to 9 months. POM Danazol (EDL 21.5/Restricted List)
Acromegaly, 1.25 mg 2-3times daily; naecomastia, both idiopathic and drug induced, Benign breast disese, 300 mg daily in Capsules, Danazol 100 mg, 200 mg.
increased gradually to 10-20 mg daily to reduce the size of the breast and to control divided doses. Duration: 3-6 months.
POM DANOL® (Sanofi)
depending on response and side associated pain and tenderness. Menorrhagia, usually 200 mg daily for Capsules, Danazol 200 mg; white opaque cap.
effects. Contra-indications: Pregnancy, breast-feed- 12 weeks. 200 mg – 50.
Inhibition of lactation, 1.25 mg with ing; markedly impaired hepatic, renal or cardiac Severe cyclical mastalgia, 100-400 mg
food in the morning and evening on daily usually for 3-6 months. POM DANOCIN® (Alpha)
function; porphyria; androgen-dependent Capsules, Danazol 200 mg; orange cap. filled with
the 1st day; followed by 2.5 mg twice tumour; undiagnosed abnormal genital bleed- Note: For the above conditions, treatment should
white to light yellow powder.
EMDEX
daily for 14 days. To prevent the onset start during menstruation preferably on day 1
ing; thromboembolic disease. 200 mg – 10 x 10’s
of lactation, treatment should be otherwise appropriate tests should be performed
Precautions: Discontinue therapy if virilisa-
instituted within a few hours of partu- tion (may be irreversible on continued use),
rition or abortion, but not before vital papilledema, headache, visual disturbances
signs have stabilized or raised intracranial pressure, jaundice or
Puerperal breast engorgement, 2.5 mg significant hepatic disturbance, thrombosis
as a single dose; may be repeated or thromboembolism occurs; hepatic, renal or
after 6-12 hours. cardiovascular disease (avoid if severe); diabetes
Incipient puerperal mastitis, as for inhi- mellitus, polycythemia, epilepsy, lipoprotein
bition of lactation plus an antibiotic. disorder, migraine; exclude carcinoma before
Benign breast disease, 1.25 mg 2-3 initiation of therapy; nonhormonal method of
times daily; increased gradually to contraception should be used.
5-7.5 mg per day. Interactions: May increase plasma level of
Parkinsons disease, see Bromocriptine carbamazepine, phenytoin, phenobarbitone,
in section 1.6.1. cyclosporin. Can potentiate the action of
POM Bromocriptine (EDL 21.5) warfarin (inhibits metabolism). Can reduce the
Tablets or Capsules, Bromocriptine (as mesylate) 1 effectiveness of antihypertensive agents.
mg, 2.5 mg. Adverse effects: Acne, oedema, mild hirsuit-
POM Apo-Bromocriptine (Lahams) ism, decrease in breast size, deepening of the
Tablet, Bromocriptine mesylate 2.5 mg; white, scored voice, oily skin or hair, weight gain and rarely
oval tab. marked ‘APO 2.5’. clitorial hypertrophy are androgenic effects as-
2.5 mg – 100’s. sociated with danazol. Also hyperoestrogenic
effects such as sweating vaginitis including
POM BROMERGON® (Taylek)
Tablet, Bromocriptine(as methanesulphonate) itching, dryness, burning and vaginal bleeding,
2.5 mg. nervousness, and emotional liability have been
2.5 mg – 30’s. reported. Allergic effects such as skin rashes
and CNS effects such as dizziness, headache,
POM PARILAC® (Dizpharm)
Tablet, Bromocriptine (as mesylate) 2.5 mg
nervousness and nausea have also been re-
2.5 mg – 30’s ported. Others include back-ache and hair loss.
Advice to patients: Notify physician if mas-
POM PARLODEL® (Novartis) culinity effects occur; virilisation may occur in
Tablets, Bromocriptine (as mesylate) 1 mg, 2.5 mg;
female patients; report menstrual irregularities;
white scored tab. marked tab. name and strength.
1 mg – 100’s male patients report persistent penile erec-
2.5 mg – 30’s. tions; all patients should report persistent GI
distress, diarrhoea or jaundice.
Nursing action: Administer with food or milk
11.1 Drugs used in obstetricts | 547
11. Drugs used 11.1 Drugs used in obstetricts PREMATURE LABOUR

11.1.1 Oxytocics Nifedipine a dihydropyridine calcium-chan-
11.1.2 Antioxytocics (tocolytics) nel blocker, relaxes the uterus and it can be
in obstetrics, Drugs may be used to modify uterine con- used to postpone labour in uncomplicated
tractions. These include oxytocic drugs used cases of premature labour. It can permit a
to stimulate uterine contractions both in delay in delivery of at least 48 hours. The
greatest benefit is obtained by using this de-
gynaecology and
induction of labour and to control postpar-
tum haemorrhage and beta2-adrenoceptor lay to administer corticosteroid therapy or to
agonists used to relax the uterus and prevent implement other measures known to improve
premature labour. perinatal health.
urinary-tract TERMINATION OF PREGNANCY ECLAMPSIA AND PRE-ECLAMPSIA
Termination of pregnancy must be carried out Magnesium sulfate has a major role in
only where facilities for the management of eclampsia for the prevention of recurrent
disorders
complications are readily available and where seizures. Monitoring of blood pressure, respira-
the procedure is permitted under national law tory rate and urinary output is carried out, as
and is culturally acceptable. Medical abortion is monitoring for clinical signs of overdosage
may be induced by the sequential use of (loss of patellar reflexes, weakness, nausea, sen-
11.1 Drugs used in obstetricts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 547
mifepristone and misoprostol. Misoprostol sation of warmth, flushing, double vision and
11.1.1 Oxytocics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 547 on its own is only a weak abortifacient and slurred speech—calcium gluconate injection
is often ineffective when used alone for the (section 6.8) is used for the management of
11.1.2 Antioxytocics (tocolytics). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 551
EMDEX
termination of pregnancy. magnesium toxicity).
11.1.3 Nausea and vomiting in pregnancy . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 551 Magnesium sulfate is also used in women with
Mifepristone, an antiprogestogenic steroid, pre-eclampsia who are at risk of developing
11.2 Genital anti-infectives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 552 facilitates medical termination of pregnancy eclampsia; careful monitoring of the patient
11.2.1 Antifungal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 552 by sensitising the myometrium to prostaglan- (as described above) is necessary.
din-induced contractions and, therefore, abor-
11.2.2 Other anti-infective drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 554 tion occurs in a shorter time and with a lower 11.1.1 Oxytocics
11.3 Contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 554 dose of prostaglandin. For the termination of
pregnancy, a single oral dose of mifepristone ERGOMETRINE
11.3.1 Oral hormonal contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 555 is followed by vaginal administration of the
Synonym: Ergonovine
11.3.2 Injectable hormonal contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 561 prostaglandin misoprostol.
Therapeutic category: Oxytocic
11.3.3 Intrauterine devices. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 563 INDUCTION AND AUGMENTATION OF LABOUR Indications: Prevention and treatment of
Prostaglandins, including misoprostol, are ef- postpartum and post-abortion haemorrhage
11.3.4 Barrier methods & lubricants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 565 in emergency situations and where oxytocin
fective for the induction of labour. Misoprostol
11.3.5 Implantable contraceptives. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 566 is usually administered as a low-dose vaginal not available.
tablet; it can alternatively be given by mouth Contra-indications: Induction of labour, first
11.3.6 Natural methods & pregnancy test kits. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 567
but this route is less effective and requires a and second stages of labour; vascular disease,
11.4 Drugs for genito-urinary disorders. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 567 larger dose. Misoprostol is associated with severe cardiac disease especially angina pec-
uterine hyperstimulation—it can increase the toris; severe hypertension; severe renal and
11.4.1 Drugs used in benign prostatic hypertrophy (BPH). . . . . . . . . . . . . . . . . . . . . . 567
risk of rupture and associated complications hepatic impairment; sepsis; eclampsia.
11.4.2 Drugs used in urological pain. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 570 in women who have undergone multiple Precautions: Cardiac disease, hypertension,
pregnancies or who have uterine scarring from hepatic impairment (Appendix 5), renal im-
11.4.3 Drugs used in erectile dysfunction (ED). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 570
surgery or caesarean section. pairment (Appendix 4), multiple pregnancy,
11.4.4 Drugs used for overactive bladder (OAB) . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 572 porphyria; interactions: Appendix 1.
POSTPARTUM HAEMORRHAGE
Adverse effects: Nausea, vomiting, headache,
Ergometrine and oxytocin differ in their dizziness, tinnitus, abdominal pain, chest pain,
actions on the uterus. In moderate doses oxy- palpitations, dyspnoea, bradycardia, transient
tocin produces slow generalized contractions hypertension, vasoconstriction; stroke, my-
with full relaxation in between; ergometrine ocardial infarction and pulmonary oedema
produces faster contractions superimposed also reported.
on a tonic contraction. High doses of both sub- Advice to patients: May cause nausea, vomit-
stances produce sustained tonic contractions. ing, dizziness, increased BP, headache, ringing
Oxytocin is now recommended for routine in the ears, chest pain, or shortness of breath.
use in postpartum and post-abortion haemor- Nursing action:
rhage since it is more stable than ergometrine. • Administer IM deep into large muscle mass and
However, ergometrine may be used if oxytocin rotate site of injection if repeat doses are required;
is not available or in emergency situations. IV use should be limited to patients with severe
548 | 11.1.1 Oxytocics 11.1.1 Oxytocics | 549
uterine bleeding or other life threatening emer- MAGNESIUM SULFATE POM Magnesium sulfate (Mark) MISOPROSTOL
gency situations. Indications: Prevention of recurrent seizures Injection, Magnesium sulfate heptahydrate 500 Indications: Induction of labour; with mife-
• Monitor BP, pulse rate and uterine response; mg per mL
in eclampsia; prevention of seizures in pre-ec- pristone, medical termination of intrauterine
report sudden changes in vital signs and uterine Pack: 5 mL x 5's (in ampoules)
hypotonia as well as the type and amount of lampsia. pregnancy of up to 63 days gestation.
Precautions: see notes above; myasthenia POM MAGPHATE® (Zolon) Contra-indications: INDUCTION OF LABOUR:
vaginal blood loss.
gravis; hepatic impairment (Appendix 5); renal Injection,Magnesium Sulphate 50 %; water for Placenta praevia or unexplained vaginal
• Contractions begin 5-15 minutes after oral dose;
injection.
2-5 minutes after IM dose; immediately after IV impairment (Appendix 4); pregnancy (Appen- bleeding during pregnancy, ruptured mem-
Pack size: 10-mL ampoule pack
dose. The uterine effects persists for 3 hours or dix 2); interactions: Appendix 1. branes, major cephalopelvic disproportion
more with oral or IM administration; 45 minutes Adverse effects: Generally associated with or fetal malpresentation, history of caesarean
after IV injection. MIFEPRISTONE
hypermagnesaemia (see also notes above), section or major uterine surgery, untreated
Dose: Prevention and treatment of postpar- nausea, vomiting, thirst, flushing of skin, Indications: with misoprostol, medical termi- pelvic infection, fetal distress, grand multiparas
tum haemorrhage, when oxytocin is hypotension, arrhythmias, coma, respiratory nation of intra-uterine pregnancy of up to 63 and multiple pregnancy, history of difficult or
not available, by IM injection, ADULT depression, drowsiness, confusion, loss of days gestation. traumatic delivery.
and ADOLESCENT 200 µg when the tendon reflexes, muscle weakness. Contra-indications: Uncontrolled severe MEDICAL TERMINATION OF PREGNANCY: See
anterior shoulder is delivered or Dose: Prevention of recurrent seizures in asthma; suspected ectopic pregnancy (use under Mifepristone.
immediately after birth. eclampsia, by IV injection, ADULT other specific means of termination); chronic Precautions: Conditions where hypotension
Excessive uterine bleeding, by slow and ADOLESCENT initially 4 g over adrenal failure, porphyria. might precipitate severe complications (for
IV injection, ADULT and ADOLES- 5–15 minutes followed either by Precautions: If treatment fails, essential that example cerebrovascular disease, cardiovas-
CENT 250–500 µg when the anterior IV infusion, 1 g/hour for at least 24 pregnancy terminated by another method; cular disease).
shoulder is delivered or immediately hours after the last seizure or delivery asthma (avoid if severe); haemorrhagic dis- MEDICAL TERMINATION OF PREGNANCY:
after birth. (whichever occurs later) or by deep orders and anticoagulant therapy; prosthetic History of caesarean section or major uterine
EMDEX
IM injection 5 g into each buttock heart valve or history of endocarditis (antibacte- surgery, grand multiparas (risk of rupture).
POM Ergometrine (WMF 22.1)
Injection, Ergometrine (as hydrogen maleate 200 µg/ then 5 g every 4 hours into alternate rial prophylaxis recommended); smokers aged IMPORTANT: For warnings relating to use of
mL; in 1-mL ampoule. buttocks for at least 24 hours after over 35 years (increased risk of cardiovascular mifepristone in a patient undergoing induc-
Note: Injection requires transport by ‘cold chain’ and the last seizure or delivery (whichever events); adrenal suppression (may require tion of abortion with misoprostol, see under
refrigerated storage. occurs later); recurrence of seizures corticosteroid); not recommended in hepatic Mifepristone.
may require additional IV injection of or renal impairment; breast-feeding (Appendix Adverse effects: Uterine hyperstimulation,
POM Ergometrine (EDL 25)
Tablet, Ergometrine maleate 0.5 mg 2 g (4 g if bodyweight over 70 kg). 3); avoid aspirin and NSAIDs for analgesia; uterine rupture, fetal distress; less commonly
Injection, Ergometrine maleate 0.5 mg per mL Prevention of seizures in pre-eclampsia, interactions: Appendix 1. in obstetric setting diarrhoea, abdominal pain,
by IV infusion, ADULT and ADOLES- IMPORTANT: For warnings relating to misopros- dyspepsia, flatulence, nausea and vomiting,
POM Elfa Ergot (Mark)
CENT initially 4 g over 5–15 minutes tol in a patient undergoing induction of abor- rashes, dizziness.
Injection, Ergometrine malaete 0.5 mg per mL; in
1 mL amp. followed either by IV infusion, 1 g/ tion with mifepristone, see under Misoprostol. Dose: Induction of labour, by vagina, ADULT
Pack: 1 x 10’s hour for 24 hours or by deep IM in- Adverse effects: Nausea, vomiting, gastroin- and ADOLESCENT initially 25 µg
jection 5 g into each buttock then 5 g testinal cramps; uterine contractions, vaginal repeated after 6 hours if necessary,
POM ERGOTRIM® (Embassy) bleeding (sometimes severe); less commonly
Injection, Ergometrine 0.5 mg per mL. every 4 hours into alternate buttocks if still no response increase to 50 µg
for 24 hours; if seizure occurs, addi- hypersensitivity reactions including rash, every 6 hours for up to 4 doses.
Pack: 100’s.
tional dose by IV injection of 2 g. urticaria, and facial oedema; rarely malaise, Note: Should it be necessary to continue induction
POM ERGOZAR® (Shrezar) headache, fever, hot flushes, dizziness, chills. of labour with oxytocin, administration of oxytocin
Dilution and Administration: For IV injection, con-
Tablet, Ergometrine 0.5 mg Dose: Medical termination of intra-uterine should be avoided within 8 hours of using miso-
centration of magnesium sulfate should not exceed
Pack: 1 x 10 x 10’s pregnancy of up to 63 days gestation, prostol.
20% (dilute 1 part of magnesium sulfate injection
Injection, Ergometrine 0.5 mg per mL
50% with at least 1.5 parts of water for injection); under close medical supervision, by Medical termination of intra-uterine
Pack: 1 x 10 x 10’s
for intramuscular injection, mix magnesium sulfate mouth, ADULT and ADOLESCENT pregnancy of up to 63 days gestation,
POM GLOMETRINE® (Hochiez) injection 50% with 1 mL lidocaine injection 2%. mifepristone 200 mg as a single under close medical supervision, by
Injection, Ergometrine maleate 0.5 mg per mL; in dose, followed 36–48 hours later vagina, ADULT and ADOLESCENT
POM Magnesium sulfate (WMF 5)
1 mL amp. misoprostol 800 µg 36–48 hours after
Injection, Magnesium sulfate 500 mg/mL; in 2-mL (unless abortion already complete)
ampoule, 10-mL ampoule. by misoprostol 800 µg by vagina mifepristone 200 mg as a single dose
POM LEKERGIN® (Taylek) and individual observed for at least by mouth (unless abortion already
POM Magnesium sulfate (EDL 3)
Tablet, Ergometrine maleate 0.5 mg; capsule 6 hours (or until bleeding or pain at complete), and individual observed
Injection, Magnesium sulfate 50% (500 mg/mL); in
shaped tab. acceptable level) with follow-up visit for at least 6 hours (or until bleeding
2-mL amp.
0.5 mg – 20; 100; 500.
10–15 days later to verify complete or pain at acceptable level) with fol-
Injection, Ergometrine maleate 0.5 mg per mL; in POM CLAMPEX® (Fidson)
expulsion (if treatment fails essen- low-up visit 10–15 days later to verify
1 mL amp. Injection, Magnesium sulfate 50%; in 5 mL amp.
Pack: 50. Pack: 5 mL x 1’s. tial that pregnancy terminated by complete expulsion (if treatment fails
another method). essential that pregnancy terminated
POM Methylergometrine (Alpha) POM MAGFIN® (Crystal) Note: Careful monitoring essential for 6 hours after by another method).
Injection, Methylergometrine maleate 0.2 mg; in 1 Injection, Magnesium Sulfate 50%; in 10 mL amp. administration of misoprostol (risk of hypotension). Administration: For medical termination of preg-
mL amber coloured amp. Pack: 1 x 5’s. nancy oral tablets may be administered vaginally
POM Mifepristone (WMF 22.1)
POM Magnesium sulfate (Alpha) if a suitable vaginal preparation is not available; for
Tablet, Mifepristone 200 mg.
Injection, Magnesium sulfate 50%; in 10 mL amp. induction of labour, low-dose vaginal tablets should
550 | 11.1.1 Oxytocics 11.1.2 Antioxytocics (tocolytics) | 551
be used, but if these are not available, 100-µg oral • Monitor and record uterine contractions, heart monitor fluid and electrolytes. visual disturbances; gum hyperplasia; aesthe-
tablets can be divided to the required dose and rate, fetal heart rate and character of vaginal blood nia, paraesthesia, myalgia, tremor, gynaeco-
POM Oxytocin (WMF 22.1)
administered vaginally. loss ¼-hourly. mastia; depression, telangiectasis, cholestasis,
Injection, Oxytocin 10 IU/mL; 1-mL ampoule.
• Observe for fetal distress indicated by deceleration, jaundice reported.
POM Misoprostol (WMF 22.1)
bradycardia, tachycardia and notify the physician. POM Oxytocin (EDL 25)
Tablet, Misoprostol 200 µg. Dose: Premature labour, sublingually (im-
• Larges doses may cause excessive fluid retention Injection, Oxytocin 5 units, 10 units per mL; in amps.
Vaginal tablet, Misoprostol 25 µg. mediate-release capsules), ADULT
which can lead to seizures and coma; monitor
fluid I&O. POM ALFATOCIN®-10 (Alpha) initially 10 mg every 15 minutes if
POM MISOCLEAR® (Apple Pharma)
• Not recommended for routine IM use; it may be Injection, Oxytocin 10 IU; clear colourless soln in necessary, maximum of 40 mg in
Tablet, Misoprostol 200 mcg.
given IM after delivery of placenta to prevent colourless amp. the first hour then by mouth (sus-
200 mcg – 10’s.
postpartum haemorrhage. Pack: 10 x 10’s
tained-release tablets), 60–160 mg
POM Misoprostol (Crystal)
Dose: Induction of labour, by IV infusion, POM LABTOCIN® (Embassy) daily in 3–4 divided doses adjusted to
Tablet, Misoprostol 200 mcg
ADULT and ADOLESCENT, initially Injection, Oxytocin 10 i.u. uterine activity.
POM Misoprostol (Zolon) 0.001–0.002 units/minute increased Pack: 100’s.
Tablet, Misoprostol 200 mcg; white tab. POM Nifedipine (WMF 22.2)
in 0.001–0.002 units/minute incre- POM Oxytocin (Alpha) Immediate release capsule, Nifedipine 10 mg
200 mcg – 3’s (in blister).
ments at intervals of 30 minutes until Injections, Oxytocin 3 IU, 5 IU, 10 IU per mL
a maximum of 3–4 contractions occur 11.1.3 Nausea and vomiting
OXYTOCIN POM Oxytocin (Crystal)
every 10 minutes; maximum rate 0.02 in pregnancy
Therapeutic category: Oxytocic Injection, Oxytocin 10 IU per 1 mL
units/minute. Pack: 100's (in ampoules)
Indications: Routine prevention and treatment Note: The dose shown above is suitable for use in See detailed information on Managing Nausea & Vom-
of postpartum and post-abortion haemor- hospital where equipment to control the infusion POM Oxytocin (Mark) iting during Pregnancy in EMDEX Vol. 3.
rhage; induction of labour. rate is available; alternative recommendations may Injection, Oxytocin 10 IU per mL
EMDEX
Contra-indications: Hypertonic uterine con- be suitable for other settings (consult Managing Pack:10 amps DOXYLAMINE plus PYRIDOXINE
tractions, mechanical obstruction to delivery, Complications in Pregnancy and Childbirth: A guide for
POM Oxytocin (Pemason) Pharmacology: The combination, doxylamine
fetal distress; any condition where sponta- midwives and doctors 2000. Geneva: WHO).
Injection, Oxytocin 10 IU per mL; in 1-mL amp. plus pyridoxine, is indicated for the treatment
IMPORTANT: Careful monitoring of fetal heart rate
neous labour or vaginal delivery inadvisable; marked “Pemason Oxytocin”.
of pregnancy-induced nausea and vomiting in
and uterine motility essential for dose titration
avoid prolonged administration in oxytocin-re- Pack: 1 mL x 10 x 10’s.
(avoid bolus intravenous injection during labour); women who do not respond to diet and life-
sistant uterine inertia, in severe pre-eclamptic discontinue immediately in uterine hyperactivity POM SYNTOCINON® (Novartis) style modifications. The mechanism of action is
toxaemia or in severe cardiovascular disease. or fetal distress. Injections, Synthetic Oxytocin 5 units, 10 units per mL unknown. Doxylamine is a first generation an-
Precautions: Induction or enhancement of Prevention of postpartum haemor- tihistamine of the ethanolamine class; it binds
POM SYNTOSTAN® (Standard Generics)
labour in presence of borderline cephalopelvic rhage, by IM injection, ADULT and AD- non-selectively to H1-receptors both centrally
Injection, Oxytocin 10 IU per mL; in 1-mL amp.
disproportion (avoid if significant); mild to OLESCENT 10 units when the anterior Pack: 1 mL x 10’s. and peripherally. Ethanolamines derivatives
moderate pregnancy-associated hypertension shoulder is delivered or immediately have greater anticholinergic activity than other
or cardiac disease; age over 35 years; history of after birth. 11.1.2 Antioxytocics (tocolytics) antihistamines and are commonly associated
low-uterine segment caesarean section; avoid Prevention of postpartum haemor- with dry mouth, blurred vision, constipation
tumultuous labour if fetal death or meconi- rhage, by slow IV injection, ADULT NIFEDIPINE and urinary retention; they are also more likely
um-stained amniotic fluid (risk of amniotic and ADOLESCENT 5 units when the to cause sedation.
Indications: Uncomplicated premature labour
fluid embolism); water intoxication and hy- anterior shoulder is delivered or Vitamin B6 is composed of three forms namely
between 24–33 weeks gestation.
ponatraemia (avoid large volume infusions and immediately after birth. pyridoxine, pyridoxal, and pyridoxamine.
Contra-indications: Cardiogenic shock;
restrict fluid intake); caudal block anaesthesia Treatment of postpartum haemor- Pyridoxine is converted in erythrocytes to the
advanced aortic stenosis; within 1 month of
(risk of severe hypertension due to enhanced rhage, by slow IV injection, ADULT active moiety, pyridoxal phosphate (requiring
myocardial infarction; unstable or acute attacks
vasopressor effect of sympathomimetics); and ADOLESCENT 5–10 units or by riboflavin for the conversion), while pyridoxam-
of angina; porphyria.
interactions: Appendix 1. IM injection, 10 units, followed in ine is converted into pyridoxamine phosphate.
Precautions: Stop if ischaemic pain occurs
Adverse effects: Uterine spasm, uterine hy- severe cases by IV infusion, a total Pyridoxine has modest antiemetic effects.
shortly after starting treatment; poor cardiac
perstimulation (usually with excessive doses— of 40 units should be infused at a Indications: Nausea and vomiting during
reserve; heart failure or significantly impaired
may cause fetal distress, asphyxia and death, or rate of 0.02–0.04 units/minute; this pregnancy.
left ventricular function; severe hypotension;
may lead to hypertonicity, tetanic contractions, should be started after the placenta Contra-indications: Hypersensitivity to any of
reduce dose in hepatic impairment (Appendix
soft-tissue damage or uterine rupture); water is delivered. its ingredients; MAOI therapy.
5); diabetes mellitus; breastfeeding (Appendix
intoxication and hyponatraemia associated Note: For further details on management of postpar- Precautions: May cause drowsiness (caution
3); avoid grapefruit juice (may affect nifedipine
with high doses and large volume infusions; tum haemorrhage consult Managing Complications
about activities that require mental alertness);
in Pregnancy and Childbirth: A guide for midwives and metabolism); interactions: Appendix 1.
nausea, vomiting, arrhythmias, rashes and Asthma; Glaucoma; Peptic ulcer; Epilepsy;
doctors 2000. Geneva. WHO. Adverse effects: Headache, flushing, dizziness,
anaphylactoid reactions also reported. other CNS depressants e.g. alcohol. Pregnancy
Dilution and Administration: According to manu- lethargy; tachycardia, palpitation; exaggerated
Nursing action: (clinical experience limited to within 14 weeks);
• Administer by IV infusion and in hospital where facturer’s directions. Prolonged IV administration at fall in blood pressure and reflex tachycardia
critical care facilities and doctor are available. high doses with large volume of fluid (for example which may lead to myocardial or cerebrovas- Breastfeeding.
• Do not give by bolus IV injection; rapid IV injection in inevitable or missed abortion or postpartum cular ischaemia; gravitational oedema; rash Interactions: MAOIs (contraindicated). Other
may cause short-lasting drop in BP. haemorrhage) may cause water intoxication with (erythema multiforme reported), pruritis, agents with anticholinergic effects e.g. phe-
hyponatraemia. To avoid: use electrolyte-containing nothiazines, some antipsychotics, tricyclic
• Used for induction and enhancement of labour urticaria; nausea, constipation ordiarrhoea;
diluent (not glucose), increase oxytocin concentra-
only when pelvis is adequate, and fetal maturity increased frequency of micturition; eye pain, antidepressants, etc. CNS depressants e.g. al-
and position are assured and favourable. tion to reduce fluid, restrict fluid intake by mouth;
cohol, narcotic analgesics, etc. SSRIs (enhanced
552 | 11.2 Genital anti-infectives 11.2.1 Antifungal drugs | 553
sedation). Pyridoxine may antagonize effect CLOTRIMAZOLE Pack: 6's in strips phytes and candida species but also a bacte-
of Levodopa. Indications: Anogenital candidosis. OTC GOGYNAX® (Shalina) ricidal activity against gram-positive bacteria.
Adverse effects: Drowsiness, dizziness, nerv- Precautions: Damages latex condoms and Vaginal tablet, Clotrimazole 100 mg It has a soothing effect on the symptoms that
ousness, epigastric pain, fatigue, headache, diaphragms – alternative contraceptive pre- 100 mg – 6’s frequently accompany candida infections, e.g.
asthenia, constipation, dry mouth, anorexia, cautions must be used. pruritis, leukorrhoea and burning sensation.
OTC GYNOTAB® (Embassy)
dry mucous membranes, disorientation, irri- Adverse effects: Local irritation. Vaginal tablet, Clotrimazole 200 mg.
Indications: Vulvovaginitis caused by candida
tability, confusion, urinary retention, dysuria, Advice to patients: May cause irritation to the 200 mg – 6’s. and/or grampositive bacteria; leukorrhoea;
insomnia, blurred vision, tachycardia, palpita- skin; avoid contact with eyes. itching, burning sensation of the vulva.
tions, hypersensitivity, pruritus, rash. OTC IMAZOLE-V® (Greenlife) Advice to patients: Avoid contact with the
Nursing action: Vaginal tablet, Clotrimazole 100 mg.
Dose: Delayed-release tablets: Adult, by • Clean area with soap and water before applying. eyes; for vaginal product, insert high into
100 mg – 7’s.
mouth, Nausea and vomiting of preg- • Advise patient to use nonstop for the prescribed Vaginal pessaries, Clotrimazole 500 mg. vagina and complete full course of therapy;
nancy, Delayed-release tablet: Take 2 period; if condition persists or worsens, or if irrita- 500 mg – 1’s notify physician if itching or burning occur;
tablets (a total of doxylamine 20 mg tion, burning, itching, redness or stinging occur, refrain from intercourse to prevent reinfection.
and pyridoxine 20 mg) at bedtime. discontinue use and report to physician. OTC MYCORON® (Justeen) Nursing action: See under Clotrimazole.
• Advise patient to abstain from sexual intercourse Cream, Clotrimazole 1% w/w.
May take 1 additional tablet in the Dose: Cream, 1 applicatorful (5 g) once daily
during vaginal or vulval treatment. Pack: 30 g.
morning and 1 tablet midafternoon; • Advise patient to continue using during menstru- for 7 days, even after the pruritus
adjust dose based on individual OTC MYCOTEN® (Drugfield) leukorrhoea have disappeared.
ation and to wash hands before and after each
response, up to a max. 4 tablets daily. Vaginal tablet, Clotrimazole 100 mg. Ovules, 200 mg every night for 7 days
application.
Note: Tablets are taken on a daily basis not on an “as Vaginal cream, Clotrimazole 1%.
Dose: Anogenital candidosis, ADULT, apply or 400 mg every night for 3 consecu-
needed” basis; reassess continued need for therapy 1% cream to anogenital area 2–3 OTC PENOTRIN® (Nalis) tive days.
as pregnancy progresses. Clinical experience is Vaginal tablet, Clotrimazole 200 mg
times daily. OTC (EDL 12.2)
EMDEX
limited to within 14 weeks of gestation. 200 mg – 1 6 x 6’s
Administration: To be taken on an empty stomach Vaginal candidosis, ADULT, vaginal Ovules, Miconazole nitrate 200 mg, 400 mg.
with a glass of water. Delayed-release tablets should administration, 5 g of 10% vaginal OTC SABRESTEN® (Gemini)
OTC FUNGUR® (Taylek)
be swallowed whole without chewing or breaking. cream as a single dose at night, Vaginal cream, Clotrimazole 0.35 g per 35 g
Vaginal cream, Miconazole nitrate 20 mg per g.
repeated once if necessary. Pack: 35 g with applicator.
(Additional information sourced from Doxylamine and Pyri- Pack: 40 g plus 7 applicators; 80 g plus 14 applicators
Vaginal candidosis, ADULT, vaginal Dose: 1 filled applicator (approx. 5 g) should be
doxine monograph [1] http://www.uptodate.com/ [2] https://
inserted daily into the vagina as deeply as OTC GYNO-DAKTARIN® (Janssen-Cilag)
www.clinicalkey.com/) administration of pessary, 100 mg at
possible, preferably at night, for 6 consec- Cream, Miconazole nitrate 2%
night for 6 nights or 200 mg at night utive days. A six day treatment is generally
POM MURNISIK® (Zeenat) Pack: 40 g plus applicator
for 3 nights or 500 mg at night as a sufficient for vaginitis caused by fungi. Ovules, Miconazole nitrate 200 mg, 400 mg.
Tablet, Doxylamine succinate 10 mg, Pyridoxine HCl
single dose. Note: Best result is achieved when lying back with 200 mg – 7
10 mg, Folic acid 2.5 mg; yellow tab.
Pack: 10’s (in blisters). OTC Clotrimazole (WMF 6.3) the legs slightly drawn up. If necessary, a second six- 400 mg – 3.
Vaginal tablets, Clotrimazole 100 mg, 500 mg day treatment may be carried out. Treatment should
be timed so as to avoid the menstrual period and be MICONAZOLE plus METRONIDAZOLE
11.2 Genital anti-infectives Vaginal cream, Clotrimazole 1%, 10%.
finished before the onset of menstruation. In cases
OTC Clotrimazole (EDL 12.2) of concomitant vulvitis or Candida balanitis of the
Indications: Treatment of vaginal candidiasis,
11.2.1 Antifungal drugs
11.2.2 Other anti-infective drugs Pessaries, Clotrimazole 100 mg, 200 mg. sexual partner and in order to prevent reinfection, bacterial and trichomonal vaginitis, or mixed
both partners should also undergo local treatment forms of vaginitis.
OTC BG TRIVAG® (BG Pharmacy)
with Sabresten cream. Sabresten vaginal cream is Contra-indications: Hypersensitivity to any
11.2.1 Antifungal drugs Vaginal tablet, Clotrimazole 100 mg.
Pack: 1 x 6’s.
odourless and can be washed off. component of the preparation; severe hepatic
Imidazole drugs (Clotrimazole, Tioconazole, dysfunction; alcohol; first trimester of preg-
OTC YTACAN-C® (Strides Vital)
Econazole, Fenticonazole, Isoconazole and OTC CANDID-V6® (Glenmark) nancy, lactation.
Vaginal tablet, Clotrimazole 100 mg.
Miconazole) are effective in short courses of Vaginal tablet, Clotrimazole 100 mg; uncoated tab.
100 mg – 6’s. Precautions: Avoid alcohol during treatment
3 to 14 days according to the preparation used; 100 mg – 6’s (in aluminum foil with applicator).
and at least 48 hours after. Treat sexual partner
single dose preparations offer an advantage OTC CANDID V-1® (Glenmark) ISOCONAZOLE of trichomoniasis patient. Renal and hepatic
when compliance is a problem. Vaginal tablet, Clotrimazole 500 mg; uncoated tab. insufficiency.
Indications: One shot antimycotic for fungal
Nystatin is a well established treatment (but 500 mg – 1’s (in aluminum foil with applicator). Interactions: Concomitant use with alcohol
infections of the vagina including mixed infec-
stains clothing yellow). Recurrence is common OTC CANDID®-V Gel (Glenmark) tions with gram-positive bacteria. (disulfiram-like reaction ).
if the full course of treatment is not completed Gel, Clotrimazole 2% Dose: Insert 1 ovule as single dose deep into Adverse effects: Vaginal irritation, rash,
and is also particularly likely if there are pre- Pack: 30 g with applicator abdominal pain or cramps, metallic taste,
vagina at bedtime.
disposing factors such as antibiotic therapy, OTC CLOMAZ® (L.B.S.) Not to be used during menstruation. diarrhea, lack of appetite, nausea, headache.
oral contraceptive use, pregnancy, or diabetes Vaginal tablet, Clotrimazole 100 mg; white oblong Dose: See under preparations below.
OTC GYNO-TRAVOGEN® (Bayer Schering)
mellitus. Possible reservoirs of infection may tab. marked with marker’s name. POM NEO-PENOTRAN® Forte (Bayer Schering)
Vaginal Ovule, Isoconazole nitrate 600 mg.
also lead to recontamination and should be 100 mg – 6 with applicator. Vaginal pessary, Metronidazole 750 mg, miconazole
Pack: 1 Ovule plus applicator.
treated. These include other skin sites such as OTC CLOTIVAL® (Al-Tinez) nitrate 200 mg.
the digits, nail beds, and umbilicus as well as Vaginal tablet, Clotrimazole 100 mg MICONAZOLE Pack: 7 pessaries with 7 disposable fingerstalls
the GIT, and the bladder. The partner may also Pack: 1 x 6’s Dose: Insert 1 pessary into vagina at bedtime for
Therapeutic category: Imidazole antifungal. 7 days.
be the source of the re-infection and should be
OTC Clotrimazole (Zolon) Pharmacology: Miconazole possesses not only
treated with cream at the same time. Vaginal tablet, Clotrimazole 100 mg; f-c tab a potent fungicidal action against dermato-
554 | 11.2.2 Other anti-infective drugs 11.3.1 Oral hormonal contraceptives | 555
NYSTATIN may be effective in patients who are improved but 11.3.5 Implantable contraceptives 11.3.1 Oral hormonal contraceptives
Therapeutic category: Antifungal antibiotic. not cured by the first course.
WHO publishes guidelines on the use of contraceptives, Women who use hormonal contraceptives
Vaginal ovule, Tioconazole 300 mg.
Indications: Vaginal candidiasis including the Medical Eligibility Criteria for Contracep- should receive the following information:
300 mg – 1’s + applicator.
Adverse effects: Transient local discomfort tive Use, available at www.who.int/reproductivehealth/ Serious Warnings & Precautions
Dose: 300 mg applied at night upon retiring as a one
may be experienced. publications/mec, and the Selected Practice Recommen- Cigarette smoking increases the risk of
day single dose therapy; may be repeated
Advice to patients: See under Miconazole. dations for Contraceptive Use, available at www.who.
one week later if necessary. serious cardiovascular events from com-
int/reproductive-health/publications/spr.
Nursing action: See under Clotrimazole. bined oral contraceptive (COC) use. This risk
Dose: Adult, 1 or 2 pessaries intravaginally 11.2.2 Other anti-infective drugs Parenteral hormonal contraception increases with age and becomes significant
for at least 14 days; not to be inter- in hormonal contraceptive users older than
rupted during menstrual period. Medroxyprogesterone acetate and norethister-
CLINDAMYCIN plus CLOTRIMAZOLE 35 years of age. Women over 35 years old
Vaginal cream, 1 or 2 applications one enantate are long-acting progestogens
Indications: Treatment of infective leucor- who smoke should not use COC.
(of 4 g each) high into the vagina for given by IM injection every three months
rhoea, mixed infections and non-specific vag- Birth control pills Do Not Protect against
14 consecutive nights, or longer, re- and every two months respectively. Women
initis, vaginal candidiasis, bacterial vaginosis sexually transmitted infections (STIs), in-
gardless of any intervening menstrual should be counselled about the likelihood of
and trichomoniasis. cluding HIV/AIDS. For protection against
period. Reinfection from the candidal menstrual disturbance and the potential for a
Contraindications: History of hypersensitivity STIs, it is advisable to use latex or polyure-
content of the intestinal tract may be delay in return to full fertility; delayed return
to clindamycin or clotrimazole or any of the thane condoms in combination with birth
prevented by concomitant therapy of fertility and irregular cycles may occur after
components of the preparation; history of control pills.
with oral nystatin. Nystatin cream, discontinuation of treatment but there is
regional enteritis, ulcerative colitis, or antibi- no evidence of permanent infertility. Heavy Advise all users to report potential signs of
gel or ointment should be applied to otic-associated colitis. bleeding has been reported in patients given cardiovascular trouble namely ACHES, acro-
the perineal region 2-4 times daily, if Precautions: Pregnancy and lactation; co-ad- parenteral progestogen-only contraceptives nym for severe Abdominal pain, Chest pain,
necessary. ministration with neuromuscular blocking
EMDEX
in the immediate puerperium (the first dose Headache, Eye problem and Severe leg pain.
Note: To prevent reinfection with Candida, the male
agents. is best delayed until 6 weeks after birth). If the
consort should be treated concurrently with nystatin Hormonal contraception is one of the most
Adverse effects: Genital itching or burning; woman is not breast-feeding, the first injection
cream or gel applied to the external genital area 2-4 effective methods of reversible fertility control.
times daily during the treatment period. irritation, vaginal pain, an increased need to may be given within 5 days after birth (she
urinate, lower abdominal cramps may occur. COMBINED ORAL CONTRACEPTIVES
POM Nystatin (EDL 5.11.2) should be warned that the risk of heavy or
Dose: Insert 1 suppository intravaginally prolonged bleeding may be increased). Paren- Estrogen plus progestogen combinations are
Pessary, Nystatin 100,000 units.
once a day, preferably at bedtime, for teral progestogen-only contraceptives reliably the most widely used hormonal contracep-
3 consecutive days. inhibit ovulation, and protect against ectopic tives. They produce a contraceptive effect
TIOCONAZOLE
POM CLOLIND® (Canopus) pregnancy and functional ovarian cysts. mainly by suppressing the hypothala-micpitu-
Therapeutic category: Imidazole antifungal.
Vaginal suppositories, Clindamycin (as phosphate) Reduction in bone mineral density and rare itary system resulting in prevention of ovula-
Pharmacology: A broad spectrum antifungal
100 mg, Clotrimazole 100 mg cases of osteoporosis and osteoporotic fraction; in addition, changes in the endometrium
agent which also has antibacterial activity Pack: 1 x 6’s tures have been reported with medroxy-pro- make it unreceptive to implantation.
against certain Gram-positive organisms.
gesterone acetate; the reduction in bone Endometrial proliferation is usually followed
Indications: Local treatment of vaginal yeast METRONIDAZOLE mineral density occurs in the first 2–3 years of by thinning or regression of the endometrium
infections.
Indications: Trichomonas vaginalis vaginitis; use and then stablises. resulting in reduced menstrual flow. Ovulation
Contra-indications: Hypersensitivity to imida-
non-specific vaginitis. Medroxyprogesterone acetate with estradiol usually resumes within three menstrual cycles
zole antifungal agents.
Dose: 1 pessary in the vagina daily for 7-10 cipionate is a combined progestogen plus after oral contraception has been discontinued;
Precautions: Pregnancy
days; may be combined with oral estrogen preparation given monthly by IM anovulation and amenorrhoea persisting for six
Adverse effects: Local irritation.
treatment. injection. Medroxyprogesterone with estradiol months or longer requires investigation and
Dose: 300 mg intravaginally at night as
See under section 9.3.2 for more information. cipionate is associated with fewer menstrual appropriate treatment if necessary.
a one-day single dose treatment;
disturbances and a faster return to fertility Potential non-contraceptive benefits of com-
may be repeated one week later if
POM FLAGYL® (Sanofi-Aventis) after discontinuation than progestogen-only bined oral contraceptives include improved
necessary.
Pessary, Metronidazole 500 mg. contraceptives. regularity of the menstrual cycle, decreased
Note: To be inserted deep in the vagina preferably
before retiring for the night; avoid use during
500 mg – 10’s. Levonorgestrel is another progestogen, which blood loss, less irondeficiency anaemia and
menstruation. Compound preparations is available as a subdermal implant. It provides significant decrease in dysmenorrhoea. Long-
long-term contraception, which is rapidly term use is associated with reduced risk of
POM GYNO-TROSYD® (Pfizer) POM KLOVINAL® (Seagreen) endometrial and ovarian cancer and of some
Vaginal ovule, Tioconazole 300 mg. Vaginal pessary, Metronidazole 500 mg, Clotrimazole reversed upon removal. Levo-norgestrel im-
plants are an alternative for women in whom pelvic infections.
300 mg – 1 100 mg, Lactobacillus spores 150 millions cfu.
Pack: 6’s copper-containing intra-uterine devices (IUDs) There may be an association between the
POM GYNO-TIOCOSID® (Neimeth) amount of estrogen and progestogen in
Indications: Vaginal infections like trichomoniasis, are unsuitable because of pelvic inflammatory
Vaginal tablet, Tioconazole 100 mg. oral contraceptives and the increased risk
100 mg – 6’s + applicator.
bacterial vaginosis and vulvovaginal candidiasis. disease, dysmenorrhoea, or heavy menstrual
bleeding. Levonorgestrel implant insertion and of adverse cardiovascular effects. The use of
Dose: 100 mg applied once nightly on retiring for
the specific duration of treatment using the 11.3 Contraceptives removal requires training. oral contraceptive combinations containing
applicator supplied. the progestogens, desogestrel or gestodene
11.3.1 Oral hormonal contraceptives
Note: Gyno-Tiocosid is effective when applied for is associated with a slightly increased risk of
11.3.2 Injectable hormonal contraceptives
3,6 or 14 days. Three days treatment effects a cure in 11.3.3 Intrauterine devices venous thromboembolism compared with oral
most patients. A repeat course of 3 days treatment 11.3.4 Barrier methods contraceptives containing the progestogens
556 | 11.3.1 Oral hormonal contraceptives 11.3.1 Oral hormonal contraceptives | 557
levonorgestrel or norethisterone. • Hepatitis, jaundice, liver enlargement; contraceptives (courtesy: Wyeth). 4. How To Continue:
• Blood pressure above systolic 160 mmHg and
RISK FACTORS FOR VENOUS THROMBOEMBO- diastolic100 mmHg;
1. Selection Of An Oral Contraceptive: When you finish your first pack, take no tablets
LISM OR ARTERIAL DISEASE • Detection of 2 or more risk factors for venous Combined oestrogen and progestogen oral for 7 days (your period usually begins about 3
Risk factors venous thromboembolism include thromboembolism or arterial disease, see notes contraceptives are most effective and generally days after the last tablets). Start the next pack 8
family history of venous thromboembolism above used. Higher concentrations of the oestrogen days after the tablet, even if you are still bleed-
in first-degree relative aged under 45 years, and progestogen provide increased protection ing. A new pack is always started on the same
PROGESTOGEN-ONLY CONTRACEPTIVES
obesity, long-term immobilization and vari- but with possibility of increased side-effects. day of the week as the day you started taking
Progestogen-only contraceptives, such as oral your present pack. As stated above, everyday
cose veins. Generally, a preparation with the lowest oes-
levonorgestrel may offer a suitable alternative (ED) pills contain seven inactive pills corre-
Risk factors for arterial disease include family trogen and progestogen content which gives
when estrogens are contra-indicated but the sponding with the 7-day interval and hence, no
history of arterial disease in firstdegree relative good cycle control and minimal side-effects in
oral progestogen-only preparations do not interval is necessary in between packs.
aged under 45 years, diabetes mellitus, hyper- the individual patient is chosen. The oestrogen
prevent ovulation in all cycles and have a higher
tension, smoking, age over 35 years (avoid if content usually ranges from 20 to 50 µg; the 5. Missed Pills:
failure rate than combined estrogen-containing
over 50 years), obesity and migraine. upper range may be suitable in conditions of If you forget to take 1 or more pills; or if you
preparations. Progestogen-only contraceptives
If any one of the factors is present, combined reduced bioavailability such as in those using start a package late, your body may not have
carry less risk of thromboembolic and CVD
oral contraceptives should be used with antiepileptics. enough of the substances needed to prevent
than combined oral contraceptives and are
caution; if 2 or more factors for either venous Progestogen-only pills are less effective than pregnancy. In such cases, use a supplementary
preferable for women at increased risk of such
thromboembolism or arterial disease are the combined pills and may be recommended birth control method (other than oral contra-
complications, for example smokers over 35
present, combined oral contraceptives should only when oestrogen are contraindicated and ceptive tablets, for example, mechanical) until
years. They can be used as an alternative to
be avoided. Combined oral contraceptives are in heavy smokers. you have taken a tablet daily for 7 days or until
estrogen-containing combined preparations
contraindicated in migraine with aura, in severe When changing from combined to proges- you finish the package if less than 7 days tablets
prior to major surgery. Oral progestogen-only
EMDEX
migraine without aura regularly lasting over togen-only pill treatment should start on the daily remain.
contraceptives may be started 3 weeks after
72 hours despite treatment and in migraine day following completion of the combined Suppose you forget to take a day’s pill, take the
birth; breastfeeding women should preferably
treated with ergot derivatives. contraceptives course; there is no break in missed pill when you remember, and the pill
start at least 6 weeks after birth. Menstrual
SURGERY tablet taking. for that day at the regular time.
irregularities (oligomenorrhoea, menorrhagia,
Estrogen-containing oral contraceptives amenorrhoea) are common. 2. Before Starting Oral Contraceptive: In this case, you take 2 pills for the day you
should preferably be discontinued (and ade- Tell your doctor or pharmacist if you are taking remember. Continue your schedule until
EMERGENCY CONTRACEPTION
quate alternative contraceptive arrangements any drug or medication and if you have had a the package is finished. Remember to use
Levonorgestrel is used for emergency con- a supplementary contraceptive method as
made) 4 weeks before major elective surgery serious health problem. After starting, if you
traception. Levonorgestrel 1.5 mg should described above.
and all surgery to the legs or surgery which need any kind of medicine (whether prescribed
be taken as a single dose within 120 hours Suppose you forget 2 tablets in a row. Take
involves prolonged immobilization of a lower by a doctor or obtained without a prescription)
of unprotected intercourse; alternatively, the 2 missed pills when you remember, and
limb. They should normally be restarted at the be sure to tell your doctor or pharmacist.
levonorgestrel 750 µg can be taken within 72 the pill for that day at regular time. In this case
first menses occuring at least 2 weeks after full This is important because some drugs may
hours of unprotected intercourse followed 12 you take 3 pills on the day you remember.
mobilization. When discontinuation is not pos- interfere with the action of the contraceptive.
hours later by another 750 µg. Adverse effects Continue your schedule until the package is
sible thromboprophylaxis (with heparin and Also whenever you visit a doctor or health clinic
include nausea, vomiting, headache, dizziness, finished. Remember to use a supplementary
graduated compression hosiery) is advised. for any reason, mention that you are taking oral
breast discomfort, and menstrual irregularities. contraceptive method as described above. If
REASONS TO STOP COMBINED ORAL CONTRA- contraceptive.
If vomiting occurs within 2–3 hours of taking you forget 3 tablets in row do not take them
CEPTIVES IMMEDIATELY If while taking oral contraceptive you develop
the tablets, replacement tablets can be given when you remember and do not finish the
an illness with vomiting and diarrhoea that
Combined estrogen-containing oral contra- with an antiemetic. package. Wait 4 more days. This makes 1 week
lasts over 24 hours, your protection may be
ceptives should be stopped immediately if It should be explained to the woman that her without tablets.
reduced. In such a case, continue taking your
any of the following symptoms occur and next period may be early or late; that she needs Then, begin a new package 8 days after the last
pills, and also use a supplementary birth con-
resumed only after consultation with a health to use a barrier contraceptive method until tablet you took even if you are still bleeding.
trol method such as the barrier method until
care provider: her next period, and that she should return During the 7 days without tablet and until
the end of that cycle.
• Sudden severe chest pain (even if not radiating promptly if she has any lower abdominal pain you have taken a tablet daily for 7 days from
to left arm); (because this could signify an ectopic preg- 3. Your First Package: the new package use a supplementary birth
• Sudden breathlessness (or cough with blood- nancy) or if the subsequent menstrual bleed is COCs are most effective if started on Day 1 of control method for example, mechanical.
stained sputum); abnormally light, heavy, brief or absent. There cycle; may be started any day up to Day 6. May 6. If You Miss A Period:
• Severe pain in calf of one leg; is no evidence of harmful effects to the fetus
• Severe stomach pain;
start on first Sunday after the period begins if
if pregnancy should occur. desiring to avoid weekend periods. A missed period rarely means pregnancy
• Serious neurological effects including unusual,
Take your tablets at the same time each day, provided you have followed the schedule.
severe, prolonged headache especially if first time Advice To Oral Contraceptive Users
or getting progressively worse or sudden partial preferably at the evening meal or at bedtime. Failure to menstruate occurs occasionally
Users of oral contraceptives should be guided with all oral contraceptives. Even if you have
or complete loss of vision or sudden disturbance For Sunday starters and/or if started after Day
on the selection of a suitable product and taken your tablets regularly, should you miss
of hearing or other perceptual disorders or dys- 5, ovulation may not be inhibited during that
phagia or bad fainting attack or collapse or first should also be advised before and while taking a period, consult your doctor before starting
cycle and additional contraceptive precaution
unexplained epileptic seizure or weakness, motor such product. The following is a guide to the your next package.
should therefore be taken during the first 7-10
disturbances, very marked numbness suddenly health care personnel and some of them are If you omitted any pill or started a package
days. This also applies when changing from a
affecting one side or one part of body; excerpts from the literature on Wyeth’s oral later, and do not menstruate during the tab-
high to low oestrogen preparation.
558 | 11.3.1 Oral hormonal contraceptives 11.3.1 Oral hormonal contraceptives | 559
let-free days, see your doctor. Take no more ease, including disorders of hepatic secretion breast cancer should be weighed against the Ethinylestradiol 0.03 mg.
tablets until he says you can resume. Use an such as Dubin-Johnson or Rotor syndromes, protective effect against cancers of the ovary POM LOGYNON® (CHI/Schering)
alternative method of contraceptive, not oral infectious hepatitis (until liver function nor- and endometrium). Tablets, Levonorgestrel 0.05 mg, ethinyl-estradiol
contraceptive tablets, for example, mechanical mal); porphyria; systemic lupus erythematosus; Dose: Contraception, by mouth, 1 tablet daily 0.03 mg (6 tabs);
until pregnancy is ruled out. liver adenoma; history of haemolytic uraemic for 21 days; subsequent courses re- Levonorgestrel 0.075 mg, ethinylestradiol 0.04 mg
syndrome; gallstones; estrogen-dependent ne- peated after a 7-day interval (during (5 tabs);
7. Adjusting To Oral Contraceptives:
oplasms; neoplasms of breast or genital tract; which withdrawal bleeding occurs); Levonorgestrel 0.125 mg, ethinylestradiol 0.03 mg
Most side effects of the pill are serious and undiagnosed vaginal bleeding; history during everyday (ED) preparations, 1 active (10 tabs).
usually occur during the first few months pregnancy of pruritus, chorea, deteriorating tablet daily started on day 1 of the Pack: 21.
while your body adjusts. The most common otosclerosis, cholestatic jaundice, pemphigoid cycle, subsequent courses repeated POM MICROGYNON® (Bayer/Schering)
side effects are nausea, vomiting, bleeding gestationis; after evacuation of hydatidiform without interval; withdrawal bleeding Tablet, Levonorgestrel 0.15 mg, ethinyl-estradiol
between menstrual periods, weight gain and mole (until return to normal of urine and occurs when inactive tablets are 0.03 mg.
breast tenderness. plasma gonadotrophin values). being taken. Pack: 21’s.
8. When To Consult Your Doctor: Precautions: Risk factors for venous throm- Administration: Each tablet (‘pill’) should be taken POM NEOGYNON® (Bayer/Schering)
boembolism and arterial disease (see notes at approximately the same time each day; if delayed Tablet, Levonorgestrel 0.15 mg, ethinyl-estradiol
Stop taking tablets and see your doctor im- by longer than 24 hours contraceptive protection
above); migraine (see below); hyper-prolacti- 0.05 mg.
mediately if you have persistent leg, chest or may be lost (see Missed Pill below).
naemia (seek specialist advice); some types of Pack: 21.
abdominal pain, breathing difficulties, severe
headache or vomiting, dizziness or fainting, hyperlipidaemia; gallbladder disease; history of MISSED PILL: The critical time for loss of con- With ferrous fumarate
difficulty in seeing or talking, numb or weak severe depression especially if induced by hor- traception protection is when a pill is omitted
POM COMBINATION® 3 (SFH)
feeling in an arm or leg, if you cough up blood, monal contraception; long-term immobiliza- at the beginning or end of a cycle (which
Tablet, Ethinylestradiol 0.03 mg, Levonorgestrel 0.15
if you notice unexpected vaginal bleeding tion (see also Travel below); sickle-cell disease; lengthens the pill free interval). mg, Ferrous fumerate 75 mg; in a pack containing 21
EMDEX
or changes in your menstrual period, if you inflammatory bowel disease including Crohn If a woman forgets to take a pill, she should take yellow active tabs & 7 brown iron tabs.
become very sad or irritable, or have other disease; interactions: Appendix 1. MIGRAINE: it as soon as she remembers, and take the next Pack: 28’s.
unusual symptoms. Patients should report any increase in head- one at the normal time. If the delay is 24 hours POM DUOFEM® (SFH)
ache frequency or onset of focal symptoms or longer with any pill (especially the first in the Tablet, Norgestrel 0.3 mg, ethinylestradiol 0.03 mg
9. Cigarette Smoking: (discontinue immediately and refer urgently packet) the pill may not work. As soon as she (white tab.) PLUS Ferrous fumarate 75 mg (brown
Cigarette smoking increases the risk of serious to neurology expert if focal neurological remembers, she should continue taking the pill tab.) in a 28 day pack containing 21 “active” white
side effects on the heart and blood vessels from symptoms not typical of aura persist for more normally but she will not be protected for the pills (with hormones) and 7 brown “reminder” pills
oral contraceptive use. This risk increases with than one hour); contraindications: migraine next 7 days and she must either not have sex (with iron).
age and with heavy smoking (15 or more cig- with typical focal aura; migraine without aura Dose: 1 tab. daily for 28 consecutive days starting
or she should use another method of contra-
arette per day) and is quite marked in women regularly lasting over 72 hours duration despite from 1st day of cycle and continuing non-
ception such as a condom. If these 7 days run stop until the pack is empty.
over 35 years of age. Women who use oral treatment; migraine treated with ergot deriva- beyond the end of the packet, the next packet Advice to patients: Take each pill at the same time
contraceptives should not smoke. tives; precautions: migraine without focal aura should be started at once, omitting the pill-free every day. Do not skip pills even if you are spotting
10. Childbirth: or controlled with 5-HT1 agonist. interval (or, in the case of everyday (ED) pills, or bleeding between monthly periods or feel sick
TRAVEL: Women taking oral contraceptives omitting the 7 inactive tablets). to your stomach (nausea). Do not skip pills even if
Following childbirth oral contraceptives can be
may be at increased risk of deep vein throm- you do not have sex very often. Start the next pack
started at any time after 3 to 4 weeks postpar- Emergency contraception is recommended
bosis during travel involving long periods of on the day after your last “reminder” (brown) pill. Do
tum (not earlier because of the increased risk if more than 2 combined oral contraceptive not wait any day between the packs.
immobility (over 5 hours). The risk may be re-
of thrombosis in relation to the combined pill, tablets are missed from the first 7 tablets in
duced by appropriate exercise during the jour- POM LOCON-F® (SFH)
and of breakthrough bleeding in relation to the a packet.
ney and possibly by wearing elastic hosiery. Tablets, Levonorgestrel 0.1 mg, Ethinylestradiol 0.02
progestogen-only pill). If they are started later DIARRHOEA AND VOMITING: Vomiting up to
Adverse effects: Nausea, vomiting, headache, mg (orange tab.) + Ferrous fumarate 75 mg equiv. to
than 4 weeks postpartum extra contraceptive 2 hours after taking an oral contraceptive or
breast tenderness, increase in body weight, 24.375 mg iron (brown tab.); both s-c tabs.
precautions should be taken for 7 days. very severe diarrhoea can interfere with the Pack: 28’s (Everyday pill pack with 21 active (hormo-
thrombosis, changes in libido, depression,
chorea, skin reactions, chloasma, hyperten- absorption of the pill. Additional precautions nal) orange pills + 7 brown pills with iron).
ETHINYLESTRADIOL plus should be used during and for 7 days after re-
LEVONORGESTREL sion, impairment of liver function, ‘spotting’ in
early cycles, absence of withdrawal bleeding, covery (see also Missed Pill above). If vomiting ETHINYLESTRADIOL plus DROSPIRENONE
Indications: Contraception; menstrual symp-
irritation of contact lenses; rarely, photosen- and diarrhoea occur during the last 7 pills, the Warnings: COCs containing Drospirenone (DRSP)
toms; endometriosis (see also progestogens,
sitivity and hepatic tumours; breast cancer next pill-free period should be omitted (in the may be associated with a higher risk of venous
section 10.4.2).
(small increase in risk of having breast cancer case of everyday (ED) tablets, the inactive ones thromboembolism (VTE) than COCs containing
Contra-indications: Use within 3 weeks of
diagnosed in women taking the combined oral should be omitted). Levonorgestrel or some other progestins. Before
birth; breastfeeding until weaning or for first
contraceptive; this relative risk may be due to initiating Yaz in a new COC user or a woman who
6 months after birth (Appendix 3); personal POM Ethinylestradiol plus levonorgestrel (WMF
earlier diagnosis; cancers diagnosed are more is switching from a contraceptive that does not
history of or 2 or more risk factors for venous 18.3.1)
contain DRSP, consider the risks and benefits of a
or arterial thrombosis (see notes above); heart likely to be localised to the breast; risk appears Tablet, Ethinylestradiol 30 µg, levonorgestrel 150 µg.
DRSP-containing COC in light of her risk of a VTE.
disease associated with pulmonary hyperten- to relate to age at which the contraceptive is
POM Levonorgestrel plus Ethinylestradiol (EDL
stopped rather than total duration of use; any Indications: Oral contraception. Moderate
sion or risk of embolism; migraine (see below); 21.3.4)
increased risk disappears gradually during Tablet, Levonorgestrel 0.15 mg, Ethinylestradiol acne vulgaris in women ≥14 years of age
history of sub-acute bacterial endocarditis;
the 10 years after stopping and there is no 0.03 mg who have no known contraindications to oral
ischaemic cerebrovascular disease; liver dis-
excess risk by 10 years; small increase in risk of Tablet (Triphasic), Levonorgestrel 0.05 – 0.15 mg, contraceptive therapy, desire contraception,
560 | 11.3.1 Oral hormonal contraceptives 11.3.2 Injectable hormonal contraceptives | 561
and have achieved menarche. Premenstrual mg; in a blister pack containing 24 active light pink Missed Pill: If a pill is not taken on time, it should be 11.3.2 Injectable hormonal
dysphoric disorder (PMDD) for women who and 4 inactive white, both f-c tabs. taken as soon as possible, and the next one taken at contraceptives
choose to use an oral contraceptive for con- Pack: 28’s. the usual time. If administration is delayed by more
than 3 hours, the woman should resume taking the Medroxyprogesterone acetate and nore-
traception. thisterone enantate are long-acting pro-
ETHINYLESTRADIOL plus pill at the usual time as soon as possible; further-
Contra-indications: History of or current NORETHISTERONE gestogens given by intramuscular injection.
more, because contraceptive efficacy is reduced, an
thrombophlebitis or thromboembolic disor- additional method of contraception such as the con- Women should be counselled about the
Indications, Contra-indications, etc: See un-
ders, cerebrovascular disorders, myocardial dom is required for 2 days. Emergency contraception likelihood of menstrual disturbance and the
der Ethinylestradiol plus levonorgestrel above.
infarction or coronary artery disease, valvular may be considered if 1 or more progestogen-only potential for a delay in return to full fertility;
heart disease, thrombosis (e.g., transient POM Ethinylestradiol plus norethisterone (WMF contraceptive pills are missed or taken more than
18.3.1)
delayed return of fertility and irregular cycles
ischemic attack, angina pectoris). Presence of 3 hours late and intercourse has occurred before 2
Tablet, Ethinylestradiol 35 µg, norethisterone 1 mg. may occur after discontinuation of treatment
risk factor(s) for arterial or venous thrombosis further tablets have been taken correctly.
Diarrhoea and vomiting: Vomiting up to 2 hours but there is no evidence of permanent infer-
(e.g., severe hypertension ≥160/100 mmHg, POM Norethisterone plus ethinylestradiol (EDL tility. Heavy bleeding has been reported in
after taking an oral contraceptive or very severe di-
severe dyslipoproteinemia, heavy smoking 21.3.4)
patients given parenteral progestogen-only
Tablet, Norethisterone 1 mg, Ethinyloestradiol arrhoea can interfere with the absorption of the pill.
(>15 cigarettes per day) and over age 35, Additional precautions should be used during and contraceptives in the immediate puerperium
diabetes mellitus with vascular involvement, 0.035 mg
for 2 days after recovery (see also Missed Pill above). (the first dose is best delayed until 6 weeks
major surgery with prolonged immobilization). Emergency (post-coital) contracep- after birth). If the woman is not breast-feed-
Breast cancer or other estrogen– or proges- LEVONORGESTREL
tion, by mouth, ADULT (female), 1.5 ing, the first injection may be given within 5
tin-dependent cancer, Undiagnosed vaginal Indications: Contraception (particularly when
mg as a single dose (taken within 120 days after birth (she should be warned that
bleeding, Jaundice, Migraine with focal aura, estrogens are contraindicated); emergency
hours (5 days) of unprotected inter- the risk of heavy or prolonged bleeding may
Pancreatitis. Renal impairment, Adrenal insuffi- hormonal contraception.
course); alternatively 750 µg (taken be increased). Parenteral progestogen-only
ciency, Liver tumors or liver disease. Pregnancy. Contra-indications: Progestogen-only oral
within 72 hours of unprotected inter- contraceptives reliably inhibit ovulation, and
EMDEX
Avoid use within 3 weeks postpartum. contraceptives: severe arterial disease; liver
course) followed by a second dose of protect against ectopic pregnancy and func-
Precautions: See also the notes under hormonal tumours; history of breast cancer but may be
750 µg 12 hours later. tional ovarian cysts.
contraceptives. COCs containing drospirenone used after 5 years if no evidence of current Administration: Taking as soon as possible after
(DRSP) may be associated with a higher risk of disease; thromboembolic disorders; porphyria; unprotected intercourse increases efficacy; should
Medroxyprogesterone acetate may be used
venous thromboembolism (VTE) than COCs Progestogen-only emergency hormonal contra- not be administered if menstrual bleeding overdue. as a short-term or long-term contraceptive.
containing levonorgestrel or some other ceptives: porphyria. Reduction in bone mineral density and rare
POM Levonorgestrel (WMF 18.3.1) cases of osteoporosis and osteoporotic frac-
progestins Hyperkalemia: DRSP has antimin- Precautions: Undiagnosed vaginal bleeding; Tablets, Levonorgestrel 30 µg; 750 µg (pack of two);
eralocorticoid activity. Do not use in patients cardiac disease; past ectopic pregnancy; active tures have been reported; the reduction in
1.5 mg.
predisposed to hyperkalemia. Monitor serum liver disease, recurrent cholestatic jaundice; bone mineral density occurs in the first 2–3
migraine; diabetes mellitus; breastfeeding POM GLOSTINOR® (Global) years of use and then stablises.
potassium esp. in women on medications that
Tablet, Levonorgestrel 0.75 mg; f-c tab.
may increase serum potassium concentration (Appendix 3); interactions: Appendix 1. Norethisterone enantate is usually used as a
e.g., ACE inhibitors. Obese & older women Adverse effects: Menstrual irregularities short-term interim contraception e.g. before
(increased risk of DVT). Epilepsy (some anti- but tend to resolve on long-term treatment POM I-PILL®(Vitahealth) vasectomy becomes effective.
(including oligomenorrhoea and menorrha- Tablet, Levonorgestrel 1.5 mg; f-c tab.
convulsants may decrease efficacy of COCs).
gia); nausea, vomiting, headache, dizziness, Pack: 1’s (in blisters)
Inflammatory bowel disease (diarrhoea may MEDROXYPROGESTERONE
decrease absorption of COCs). Liver disease breast discomfort, depression, skin disorders, POM PREGNON® (SFH) Indications: Parenteral progestogen-only con-
(discontinue if jaundice occurs); Hypertension; disturbances of appetite, weight increase, Tablet, Levonorgestrel BP 0.75 mg; f-c tab. traception (short-term or long-term); menstrual
Diabetes; Dyslipidemia; Headache; Uterine change in libido; breast cancer (small increase Pack: 2’s.
symptoms and endometriosis (section 10.4.2).
bleeding; Smokers. Not recommended for in the risk of having breast cancer diagnosed Contra-indications: Pregnancy (Appendix
nursing mothers as it can decrease milk pro- in women using, or who have recently used, METHYLOESTRADIOL plus
METHYLOESTRENOLONE 2); history of breast cancer but may be used
duction. a progestogen-only contraceptive pill; this after 5 years if no evidence of current disease;
relative risk may be due to an earlier diagnosis; Therapeutic category: Female sex hormones
Interactions: Co-administration with inducers undiagnosed vaginal bleeding; history of
risk factor appears to be related to the age at Indications: For the treatment of non-occur-
of hepatic enzymes (e.g., CYP3A4) may de- pruritus during pregnancy, active liver disease
which the contraceptive is stopped rather than rence of menstrual periods in certain cases
crease the effectiveness of COCs or increase (Appendix 5); severe arterial disease; multiple
the total duration of use; increased risk reduces (secondary amenorrhea). Delay use for at least
breakthrough bleeding. Antibiotics e.g., risk factors for venous thromboembolism and
gradually during the 10 years after stopping 8weeks after the last menstruation to rule out
penicillins, tetracyclines, griseofulvin may also arterial disease (see section 11.3.1); porphyria.
and there is no excess risk by 10 years; small pregnancy.
decrease effectiveness. Precautions: Small increase in possible risk
increase in the risk of breast cancer should be Contra-indications: Pregnancy.
Adverse effects: Headache or migraine, men- of breast cancer, see also adverse effects of
weighed against the benefits). Dose: By mouth, 1 tablet to be taken with a
strual irregularities, nausea & vomiting, breast levonorgestrel, section 11.3.1; migraine; liver
Dose: Contraception, by mouth, ADULT little fluid on two consecutive days.
pain or tenderness, mood changes, decreased disease; thromboembolic or coronary vascular
(female), 1 tablet (‘pill’) (30 µg) daily, Mentrual bleeding should occur after
libido, increased weight. disease; diabetes mellitus; hypertension; renal
starting on the first day of the cycle 3-6 days but may take up to 15 days.
Dose: 24/4-regimen: 1 tablet every day for 28 disease; interactions: Appendix 1.
consecutive days starting on day 1 of and then continuously. POM GYNAECOSID® (FAB) Adverse effects: Menstrual irregularities;
menstrual cycle. Administration: Each tablet (‘pill’) should be taken Tablet, Methyloestrenolone 5mg, methyloestradiol
delayed return to fertility; reduction in bone
at approximately the same time each day. If delayed 0.3 mg.
POM YAZ® (Bayer Healthcare) for longer than 3 hours contraceptive protection Pack: 2’s mineral density; weight gain; depression;
Tablet, Ethinylestradiol 0.020 mg, Drospirenone 3 may be lost. rarely, anaphylaxis; injection-site reactions.
562 | 11.3.2 Injectable hormonal contraceptives 11.3.3 Intrauterine devices | 563
Dose: Contraception (short-term), by deep Dose: Contraception, by deep IM injec- NORETHISTERONE plus ESTRADIOL Adverse effects: Rarely, headache, gastric
IM injection, ADULT (female) 150 mg tion, ADULT (female) a single dose Pharmacology: The progesterone-estrogen upsets, nausea, a feeling of tension in the
within first 7 days of cycle or within (medroxyprogesterone acetate 25 mg combination acts primarily by inhibiting ovu- breasts, changes in body weight and libido or
first 5 days after parturition (delay with 5 mg estradiol cipionate 5 mg) lation and altering the cervical mucus. In ad- depressive moods; Break-through bleeding
until 6 weeks after parturition if within first 7 days of cycle, repeated dition, it causes morphological and enzymatic and amenorrhea.
breastfeeding). monthly. changes in the endometrium which have the Dose: Contraception, by deep slow IM
Contraception (long-term), by deep IM Administration: If interval between injections is effect of rendering nidation difficult. injection (preferably intragluteal,
injection, ADULT (female) as for short- greater than 35 days, exclude pregnancy before alternatively into the upper arm), 1
Indications: Hormonal contraception.
term, repeated every 3 months. next injection and advise patient to use additional mL on 1st day of a cycle; repeat doses
contraceptive measures (for example barrier) for 7
Contra-indications: Pregnancy; severe dis-
Administration: If interval between injections is turbances of liver function; jaundice or per- are given regardless of the cycle
greater than 3 months and 14 days, exclude preg- days after the injection.
sistent itching during a previous pregnancy; pattern at intervals of 30 ± 3 days (i.e.
nancy before next injection and advise patient to POM Medroxyprogesterone plus estradiol (WMF minimum 27, maximum 33 days).
use additional contraceptive measures (for example
Dubin-Johnson syndrome; Rotor syndrome;
18.3.2) Note: Administer the IM injection slowly to avoid
barrier) for 7 days after the injection. past or present liver tumours; past or present
Injection, Medroxyprogesterone acetate 25 mg, short lasting reactions (urge to cough, coughing
Patient advice: It is recommended that women estradiol cypionate 5 mg. thromboembolic processes in arteries or
fits, respiratory distress) which may occur during or
receive full counselling (backed by manufacturer’s veins and conditions which predispose to immediately after the injection of oily solutions. Place
approved leaflet if possible) before treatment, NORETHISTERONE ENANTATE such diseases (e.g. disturbances of the clotting a plaster over the injection site after the injection to
concerning menstrual irregularities and because of system with a tendency towards thrombosis, prevent any reflux of the solution. If the injection is
prolonged activity and the potential for a delay in Indications: Parenteral progestogen-only
certain heart diseases); sickle-cell anaemia; extended beyound the maximum of 33 days, no ade-
return to full fertility. contraception (short-term).
present or treated cancer of the breast or the quate contraceptive cover will be available from that
Note: Injection vial should be vigorously shaken just Contra-indications: see Medroxyprogester- time onwards. If no withdrawal bleeding occurs within
endometrium; severe diabetes with vascular
before use to ensure that the dose being adminis- one acetate above. 30 days after an injection, pregnancy must be ruled out
changes; disturbances of lipometabolism; a
EMDEX
tered represents a uniform suspension. I.M. injection Precautions: see Medroxyprogesterone ace- by means of a suitable test.A vaginal bleeding episode
is in the gluteal or deltoid muscle. To increase history of herpes of pregnancy; otosclerosis
tate; interactions: Appendix 1. will occur 1-2 weeks after the first injection. This is
assurance that the patient is not pregnant at the with deterioration during pregnancy.
Adverse effects: Bloating, breast discomfort, normal and if the treatment is continued, bleeding
time of the first administration, it is recommended Precautions: Regular general medical and episodes will usually occur at 30 day intervals. The
headache, dizziness, depression, nausea,
that this injection be given only during the first 5 gynaecological examination (including the time of the monthly injection will normally be during
days after the onset of a normal menstrual period;
menstrual irregularities; delayed return to
breasts and a cytological smear of the cervix) the bleeding free interval. Ability to conceive is usually
within 5-days postpartum if not breast-feeding; or if fertility; rarely, weight gain; injection-site
before starting treatment and at 6-monthly resumed within 60 days after the last injection, oth-
breast-feeding, at 6-weeks postpartum. If the period reactions.
intervals; rule out disturbances of the clotting erwise appropriate treatment is indicated in women
between injections is greater than 14-weeks, patient Dose: Short-term contraception, by deep IM who wish to become pregnant.
system; exclude pregnancy. Risk of venous and
should be examined to rule out pregnancy before injection into gluteal muscle, ADULT
administering the drug. arterial thromboembolic diseases (e.g. stroke, POM NORIGYNON® (SFH)
(female) 200 mg within first 7 days of
myocardial infarction) appears to increase Injection, Norethisterone enanthate 50 mg, estra-
POM Medroxyprogesterone (WMF 18.3.2) cycle or immediately after parturition;
further when heavy smoking, increasing age diol valerate 5 mg; oily solution in 1 mL amp.
Depot injection, Medroxyprogesterone acetate 150 repeated after 2 months.
Administration: If interval between injections is
and the use of combined hormonal contracep-
mg/mL; in 1-mL vial.
greater than 2 months and 14 days, exclude preg- tives coincide. Rarely, malignant liver tumours 11.3.3 Intrauterine devices
POM Medroxyprogesterone (EDL 21.3.2) nancy before next injection and advise patient to leading to threatening intraabdominal haem-
Injection (Depot), Medroxyprogesterone acetate 150
Copper-bearing intrauterine contraceptive
use additional contraceptive measures (for example orrhage may occur; patient should report any devices consist of a plastic carrier wound with
mg per mL; in 3-mL vial. barrier) for 7 days after the injection. unusual upper abdominal complaints. Monitor copper wire or fitted with copper bands; some
POM DEPO-PROVERA® (SFH) Patient advice: It is recommended that women patient closely for diabetes mellitus, hyperten-
receive full counselling (backed by manufacturer’s
also have a central core of silver to prevent
Injection (Depot), Medroxyprogesterone acetate 150 sion, varicose veins, a history of phlebitis, oto- fragmentation of copper. Smaller devices have
mg per mL; sterile aqueous suspension in 1-mL vial. approved leaflet if possible) before treatment, sclerosis, multiple sclerosis, epilepsy, porphyria,
Pack: 1 mL x 5’s; 1 mL x 25’s. concerning possible menstrual irregularities and been introduced to minimize adverse effects
tetany, chorea minor. Breast-feeding must be and the replacement time for these devices
because of prolonged activity.
Note: It should be administered as a deep IM stopped if the newborn is suffering from severe is normally between 3 and 8 years. Fertility
MEDROXYPROGESTERONE or persistent jaundice.
plus ESTRADIOL injection (preferably intragluteal, alternatively into declines with age and therefore a copper
the upper arm). It is advised to place a plaster over Discontinue medication if:
Indications: Parenteral progestogen-estrogen • Risk factors for thrombolism are present namely
intrauterine device fitted in a woman over 40
the injection site to prevent any reflux of the drug years of age, may remain in the uterus until
contraception (short-term). first time migrainous headache or frequent and
solution. The short-lasting reactions (urge to cough,
Contra-indications: see under Combined Oral unusually severe headache; sudden perceptual the menopause.
coughing fits, respiratory distress) which occur in
Contraceptives (section 11.3.1). rare cases during or immediately after the injection disorders (e.g. disturbances of vision or hearing); The intrauterine device is appropriate for
Precautions: see Combined Oral Contra-cep- of oil solutions can be avoided by injecting the solu- first signs of thrombophlebitis or thromboem- women who expect to use it for continuous
tives (section 11.3.1); interactions: Appendix tion extremely slowly. Following discontinuation, bolic symptoms (e.g. unusual pain in or swelling long-term contraception. It is suitable for older
1 (see Contraceptives, Oral). normal ability to conceive usually returns about 4-5 of the legs, stabbing pain on breathing or cough- parous women; intrauterine devices should be
months after the last injection. ing for no apparent reason); pain and tightness used with caution in young nulliparous women
Adverse effects: Menstrual irregularities (usu-
in the chest; impending operations (six weeks
ally stabilizes after initial months of use); less POM Norethisterone enantate (WMF 18.3.2) because of the increased risk of expulsion.
before hand); immobilization (for instance, after
commonly weight gain, headache, dizziness; Oily injection, Norethisterone enantate 200 mg/mL; accidents).
Young women at risk of sexually transmitted
abdominal pain, acne, alopecia, asthenia, 1-mL ampoule. • Onset of jaundice, hepatitis, itching over the whole infections are also at risk of pelvic inflamma-
breast tenderness, decreased libido, depres- body, increase in frequency of epileptic seizures, tory disease.
POM Norethisterone enantate (EDL 21.3.2)
sion, enlarged abdomen, nausea, nervousness Injection, Norethisterone enantate 200 mg per mL; significant rise in blood pressure, pregnancy. The timing and technique of fitting an IUD are
and vulvovaginal disorder reported. in 1-mL amp. Interactions: See Appendix 1. critical for its performance and call for proper
564 | 11.3.3 Intrauterine devices 11.3.4 Barrier methods & lubricants | 565
training and experience. Women should unfold. After the inserter is removed, the COPPER-CONTAINING DEVICE copper containing devices.
receive full counselling backed by the manu- threads attached to the end of the copper T Indications: Contraception; emergency con- POM Lippe’s Loop (EDL 21.3.3)
facturer’s approved leaflet. For routine contra- will be clipped. The threads will extend into the traception. Intra-uterine contraceptive device (IUCD), various
ception the device can be inserted between 4 vaginal from the cervical opening. The tenac- Contra-indications: Pregnancy; severe anae- sizes, A, B, C and D with insertion tubes.
and 12 days after the start of menstruation (see ulum and speculum will then be removed. At mia; 48 hours–4 weeks post partum; puer-
below for emergency contraception). There is various stages during this procedure, you may peral sepsis; postseptic abortion; cervical LEVONORGESTREL
an increased risk of infection for 20 days after feel some pain, cramping, nauseated, weak or or endometrial cancer; pelvic inflammatory Therapeutic category: Contraceptive, intrau-
insertion and this may be related to existing faint. At the end, you should remain lying down disease; recent sexually transmitted disease terine system (IUS).
lower genital tract infection. Pre-screening (at for a while and rise slowly to prevent fainting. (if not fully investigated and treated); pelvic Indications: Contraception; Idiopathic menor-
least for chlamydia and gonorrhoea) should When it is time to remove the copper T, your tuberculosis; unexplained uterine bleeding; rhagia; Protection from endometrial hyperplasia
be performed if feasible and appropriate. If doctor must remove it. Its removal may cause active trophoblastic disease; distorted or small during estrogen replacement therapy.
sustained pelvic or lower abdominal pain occur pain or cramping. The arms of the copper T uterine cavity; copper allergy; Wilson disease; Contra-indications, Precautions, etc: See
during the following 20 days after insertion of should fold upwards as it is withdrawn from medical diathermy. under Levonorgestrel-releasing implant.
the device, the woman should be treated as the uterus. Precautions: Anaemia; heavy menstrual bleed- Administration: Vaginal insertion, Adult
having acute pelvic inflammatory disease. An 2.Checking Your Copper T ing, endometriosis, severe primary dysmenor- women (>18 years), Contraception,
intrauterine device should not be removed in rhoea, history of pelvic inflammatory disease, Insert into the uterine cavity within
midcycle unless an additional contraceptive The Copper T can come out of the uterus
ovarian cancer, fertility problems, nulliparity 7 days of the onset of menstruation,
was used for the previous 7 days. If removal (womb) without your knowing it, especially
and young age, severely scarred uterus or or immediately after 1st trimester
is essential (for example to treat severe pelvic during or right after menstrual period. There-
severe cervical stenosis, valvular heart disease abortion by curettage or 6 weeks
infection) post-coital contraception should fore, at least after each menstrual period, you
or history of endocarditis (antibacterial cover postpartum.
be considered. If the woman becomes preg- should check to make sure the threads can be
needed at insertion); HIV infection or immuno- Idiopathic menorrhagia, Insert into
EMDEX
nant, the device should be removed in the felt at the cervix as follows:
• Wash your hands suppressive therapy (risk of infection—avoid if the uterine cavity within 7 days of the
first trimester and the possibility of ectopic marked immunosuppression); increased risk of onset of menstruation. Replace a new
• Squat down or seat yourself on the toilet
pregnancy considered; if the threads of the • Insert the index or middle finger into your vagina expulsion if inserted before uterine involution; system at any time of the cycle.
intrauterine device are already missing on and locate your cervix. The cervix is the mouth of gynaecological examination before insertion Endometrial protection during estrogen
presentation, the pregnancy is at risk of second the uterus. It feels firm, like the tip of your nose. and 4–6 weeks afterwards—counsel women replacement therapy, Insert at any
trimester abortion, haemorrhage, pre-term • Feel for the threads of the copper T. The threads to see doctor promptly if significant symptoms time in an amenorrhoeic woman, or
delivery and infection. should extend from the cervix and be high in your such as pain; anticoagulant therapy; remove during the last days of menstruation
vagina. The threads may be difficult to feel. if pregnancy occurs (consider possibility of
EMERGENCY CONTRACEPTION or withdrawal bleeding.
• If you can feel the threads, the copper T is probably,
ectopic pregnancy). Note: The initial release of levonorgestrel is about
Insertion of a copper intrauterine contracep- but not always, in place. You should not pull on
20 µg/24 hours. It is effective for five years in the
the threads. Doing so many displace the copper T. Adverse effects: Uterine or cervical perfora-
tive device is more effective than hormonal indications for contraception and idiopathic men-
• If you cannot feel the copper T itself, it has probably tion, displacement, expulsion; pelvic infection
methods of emergency contraception; the orrhagia; 4 years for protection from endometrial
been displaced from the uterus. Also if you or your exacerbated; heavy menstrual bleeding;
device can be inserted at any time in the men- hyperplasia. Recommended for women (≥18 years).
partner can feel the copper T during intercourse, dysmenorrhoea; pain and bleeding and occa-
strual cycle within 5 days of unprotected inter- Before insertion, a gynaecological examination,
it is displaced. And until you can be examined by sionally epileptic seizure or vasovagal attack
course. Sexually transmitted diseases should including examination of the breasts and exclusion
a doctor, use an alternative birth control method. on insertion.
be tested for and insertion of the device should of a pregnancy, should be performed. Cervical in-
3.When To Consult Your Doctor Administration: Contraception (see also fection and sexually transmitted diseases should be
usually be covered by antibacterial prophylaxis.
Advice To Users Of Copper T notes above), the device can be in- excluded. The position of the uterus and the size of
Copper T is intended to prevent pregnancy.
serted at any time between day 4 and the uterine cavity should be determined. The patient
1.How The Copper T Is Inserted And Removed It does not protect against transmission of should be re-examined six weeks after insertion
day 12 after the start of menstrual
HIV (AIDS) and other sexually transmitted and once a year thereafter, or more frequently if
Before insertion, your doctor will examine your bleeding; not to be fitted during
diseases such as chlamydia, genital herpes, clinically indicated.
pelvis to determine the size, shape and position heavy menstrual bleeding.
genital warts, gonorrhoea, hepatitis B and
of the uterus. An instrument called a speculum Emergency contraception (see also POM MIRENA® (Bayer Schering)
symphillis. If you have the copper T inserted,
will hold your vagina open so that the cervix notes above), the device may be Intrauterine system, Levonorgestrel 52 mg with initial
contact your doctor immediately for any of the release rate of 20 mcg/24 hours
(the entrance to the uterus) can be seen. inserted up to 120 hours (5 days) after
following reasons: 52 mg – 1’s.
The cervix is then cleaned with an antiseptic • A missed period may indicate pregnancy and unprotected intercourse, at any time
solution and an instrument call a tenaculum is copper T should be removed. of menstrual cycle; if intercourse has
attached to it. This instrument assists in holding • Abnormal vaginal bleeding or discharge; a delayed occurred more than 5 days previously, 11.3.4 Barrier methods & lubricants
the uterus steady during insertion. The doctor period followed by scanty or irregular bleeding; device can still be inserted up to 5
will then guide a narrow instrument called a pelvic or lower abdominal pain or cramps or unex- days after the earliest likely calculated BARRIER METHODS
sound through the opening of the cervix into plained fever; genital sores or lesion, or fever with day of ovulation; device can be re- Note: Barrier methods are not as effective in preventing
the uterus. The sound measures the depth and vaginal discharge. These are symptoms of infection moved at the beginning of menstrua- conception as hormonal contraception and copper
position of the uterus. or ectopic pregnancy (i.e. pregnancy outside of the tion if no longer required. intrauterine devices. Spermicidal methods when used
uterus) and require immediate treatment. Note: Copper T must be replaced every 5 to 8 years, alone are generally considered relatively ineffective and
Then your doctor will guide the copper T (with
• Tail or thread disappearance or pain during sex to maintain its contraceptive effectiveness. such use is not recommended.
the cross arms of the T folded down) through indicate that the copper T may have expelled or
the vagina and the cervix into the uterus. As displaced, or may have perforated the uterus. POM Copper (EDL 21.3.3) Indications: Contraception; for condoms, also
the copper T. is inserted, the arm of the T will Intra-uterine contraceptive device (IUCD), various to decrease risk of transmission of HIV and
566 | 11.3.5 Implantable contraceptives 11.3.6 Natural methods & pregnancy test kits | 567
other sexually transmitted diseases. 11.3.5 Implantable contraceptives 11.3.6 Natural methods & accurately your most fertile days to conceive, thus
Precautions: Oil-based products including pregnancy test kits its very useful in timing intercourse. It also increases
baby oil, massage oil, lipstick, petroleum jelly, LEVONORGESTREL-RELEASING IMPLANT the chances of selecting the desired sex of baby.
OTC CYCLEBEADS® (SFH) Predicte® acts by detecting the sharp increase in
sun-tan oil can damage latex condoms and Therapeutic category: Contraceptive, im- Description: CycleBeads are a string of coloured beads luteinizing hormone (LH) in your urine. This hor-
render them less effective as barrier method plant. that represents each day of a woman’s menstrual mone is responsible for ovulation. The sharp increase
of contraception and as a protection from Indications: Parenteral progestogen-only cycle. White beads represent the fertile window (i.e., occurs 24-36 hours before your ovulation.
sexually transmitted infections (including contraception (long term). days 8 through 19 of the cycle) while brown beads
HIV); if a lubricant required, use one that is represent the low-fertility period. Based on a natural OTC PREDICTE® Pregnancy Test (Carrot-Top)
Contra-indications: Pregnancy (Appendix 2);
water-based; male condom must be put on method of family planning called the standard days Test kit
ischaemic heart disease, stroke, migraine with Indications: Predicte® Pregnancy Test is a simple
before the penis touches the vaginal area and method. Works best for women who have menstrual
aura, thromboembolic disorders, unexplained cycles between 26 and 32 days long. and easy test kit that confirms your pregnancy even
the penis must not touch the vaginal area after vaginal bleeding, breast cancer, active viral before you miss your period.
the condom has been taken off; spermicides or hepatitis, severe liver disease (Appendix 5), OTC PREDICTE®-Plus (Carrot-Top)
diaphragm not suitable for women at high risk liver tumours. Predicte-Plus is an ovulation prediction mi-
11.4 Drugs for genito-urinary
of HIV infection or with HIV infection. Precautions: Hypertension, heart disease, his- croscope that uses saliva or cervical mucus as disorders
Adverse effects: Vaginal and cervical irri- tory of thromboembolism, epilepsy, migraine test sample. It is a very useful tool in natural
tation (spermicides), toxic shock syndrome family planning. It has been shown that the 11.4.1 Drugs used in benign prostatic hypertrophy
without aura, depression, gallbladder disease,
(diaphragm, cap). egg is most fertilizable within 12 hours after (BPH)
diabetes, elevated cholesterol or triglycerides, 11.4.2 Drugs used in urological pain
OTC Barrier methods (WMF 18.3.4) breast nodules, breastfeeding and less than 6 ovulation. After about 24 hours, it cannot be
11.4.3 Drugs used in erectile dysfunction
Barriers, Male latex condoms, male non-latex con- months after birth (Appendix 3); interactions: fertilized anymore. From the point of view of 11.4.4 Drugs used for overactive bladder (OAB)
doms or female non-latex condoms; diaphragm or Appendix 1. family planning, this post-ovulation period is
cervical caps. Adverse effects: Menstrual irregularties, 48 hours comprising the 24 hours of egg life 11.4.1 Drugs used in benign prostatic
EMDEX
headache, dizziness, lower abdominal pain, and a second day for safety. hypertrophy (BPH)
OTC Barrier methods (EDL Primary Care List)
weight gain, acne; nausea, mood changes, Pack: Reusable kit for unlimited tests
Barriers, Condoms with or without Spermicide (Non-
Direction for use:
oxynol); Diaphragms with Spermicide (Nonoxynol). breast tenderness, loss of libido also reported. • Use the Predicte®-Plus microscope for checking your ALFUZOSIN
OTC Delight Condoms (Hugo)
Administration: Contraception (long-term), menstrual cycle quickly and simply, anytime, anywhere. Therapeutic category: Alpha1 antagonist.
Pack: 3 x 1 x 24 ADULT (female) 150 mg implant; • Open the microscope by turning the upper part in any
Indications: Treatment of the functional
direction
insert subdermally in non-dominant symptoms of benign prostatic hypertrophy
OTC Moods Condoms (Sequoia) • Place saliva or uterine cervical mucus on the small round
upper arm 6–8 cm above the elbow side with your finger (BPH); adjuvant treatment to a catheter in acute
Pack: 3’s
within first 7 days of cycle; remove • Let the specimen dry for 6-8 minutes then return the upper urinary retention (AUR) related to BPH.
OTC VIVA® Condoms (Korlyns) and replace after 4 to 5 years depend- part into starting position.
• Hold the microscope so that your thumb is on the small Contra-indications: History of orthostatic
Male latex condoms. ing on preparation. point in the centre of the upper part. hypotension. Combination with other al-
Note: Implant insertion and removal requires spe- • Look through the lens, holding it near to your eye. Press pha-blockers. Hepatic insufficiency.
LUBRICANTS cialist training (consult manufacturer’s literature). both parts gently to focus your microscope until you see
clear picture. By turning the upper part slightly in both
Precautions: Patients on antihypertensive
For further details on the use of contraceptives consult Med- medications may experience more postural
OTC PRE-SEED® (Carrot-Top) directions, you can observe all details of the specimen.
ical Eligibility Criteria for Contraceptive Use, third edition,
Vaginal lubricant, Hydroxyethylcellulose, pluronic, 2004 (www.who.int/reproductive-health/publications/mec) and Interpreting results: hypotension – monitor BP more regularly; Re-
sodium chloride, arabinogalactan, sodium phosphate, the Selected Practice Recommendations for Contraceptive Use, Fertile (A): Strong ferning – or crystal – pattern nal impairment; coronary insufficiency; elderly.
potassium phosphate, carbomer, methylparaben, available at www.who.int/reproductive-health/publications/spr. dominate the sample. Ovulation is about to occur Interactions: Antihypertensive agents; ni-
sodium hydroxide, purified water. or already occurring. At this time conception is likely. trates; potent CYP3A4 inhibitors e.g. ketocona-
Pack: 40 g in a tube POM Levonorgestrel-releasing implant (WMF This is the most fertile time of the month.
zole, itraconazole, ritonavir, clarithromycin,
Indications: To relieve vaginal dryness prior to 18.3.5) Transitional (B): Small ferning patterns – or crystal
intercourse. Does not harm the sperm or embryos forms – appear among the spots and lines. Ovulation
erythromycin.
Implant, Two-rod Levonorgestrel-releasing implant,
and can be used while trying to conceive. each rod containing 75 mg of Levonorgestrel (150 may occur in 3-4 days. At this time, conception is Adverse Effects: Faintness/dizziness, head-
Administration: It should be placed deep within mg total). possible, though not yet likely. ache; vision problem; rhinitis; nausea, abdom-
the vagina, to allow the product to coat Infertile (C): Simple dot patterns and lines. Not fertile inal pain; asthenia
POM Levonorgestrel-releasing implant (EDL
the vagina and external cervix, providing at this time. Dose: See below.
21.3.1)
moisture where it is most needed. Apply For natural family planning, advise patient to
Implant, Two-rod Levonorgestrel-releasing implant, POM XATRAL XL® (Sanofi-Aventis)
about 15 minutes prior to intercourse. abstain from intercourse from the time the small
each rod containing 75 mg of Levonorgestrel (150 Tablet, Alfuzosin 10 mg; prolonged-release tab.
ferning patterns begin to appear (transitional) till
mg total). 10 mg – 30’s
SPERMICIDES 24 hours after the pattern dusaapears completely.
Dose: BPH, Adult male, 10 mg once daily after a meal.
POM Levonorgestrel (EDL 21.3.2) The Predicte®-Plus Ovulation Microscope is a useful
Recommended for use together with barrier AUR, Adult (65 years and older), 10 mg daily
Implant, Levonorgestrel 36 mg; subdermal. tool for natural family planning and contraception.
methods such as condoms and IUDs. They do after a meal; to be taken from the 1st day of
Although the reliability of this test if carried out
POM JADELLE® (Bayer Schering) catheterisation. The treatment should be
not give adequate security when used alone. properly exceeds 98%, as other fully natural methods
Implant, The set contains two flexible rod-like im- administered for 3-4 days, 2-3 days during
it cannot provide 100% safety.
Nonoxynol is a non-ionic surfactant with plants. Each implant contains 75 mg Levonorgestrel. catheterisation and 1 day after its removal.
spermicidal properties. Pack: Sine inserter 2 x 75 mg implants. OTC PREDICTE® Ovulation Prediction Test (Carrot- Note: For AUR, no benefit has been established in
Top) patients <65 years of age or if treatment is extended
Test strips >4 days.
Pack: 5’s Administration: To be taken with food (preferably
Indications: Predicte® Ovulation Test determines immediately after supper). Swallow whole. Do not
568 | 11.4.1 Drugs used in benign prostatic hypertrophy (BPH) 11.4.1 Drugs used in benign prostatic hypertrophy (BPH) | 569
divide, crush or chew. is converted to DHT by the enzyme 5α-reduc- sia, Adult male (including elderly), without food. Not recommended for
tase, which exists as 2 isoforms: type 1 (active in 0.5 mg once a day. Treatment for at children.
DOXAZOSIN the reproductive organs) and type 2 (in the skin least 6 months may be necessary to POM PROSCAR®
Therapeutic category: Alpha1A antagonist. and liver). Dutasteride competitively inhibits achieve a satisfactory response. Ad- Tablet, Finasteride 5 mg.
Pharmacology: Benign prostatic hyperplasia both isoenzymes. It has no affinity for the hu- ministered alone or in combination
man androgen receptor. The maximum effect with the alpha-blocker tamsulosin POM FINSTAL-5® (PharmacyPlus)
(BPH) is a common cause of urinary outflow
Tablet, Finasteride 5 mg; f-c tab.
obstruction in aging males, and in severe of daily doses of dutasteride on the reduction (0.4 mg).
5 mg – 2 x 14’s
cases may lead to urinary retention and renal of DHT is dose dependent and is observed Prostate Cancer Risk reduction, 0.5 mg
damage. The obstructive symptoms and re- within 1 to 2 weeks Tmax is 1-3 hours and absolute once a day. TAMSULOSIN
duced urinary flow rate are associated with an bioavailability is approx. 60%, not affected by Note: Capsules should be swallowed whole and
not chewed or opened, as contact with the capsule Therapeutic category: Alpha1A antagonist,
increase in smooth muscle tone in the prostate food. Has a large volume of distribution and
contents may result in irritation of the oropharyn- selective
and bladder neck, mediated by the alpha1 is highly bound to plasma proteins (>99.5%).
geal mucosa. May be taken with or without food. Indications: Lower urinary tract symptoms asso-
adrenoceptor. The selective alpha-blockers Metabolism is by CYP3A4 and the unchanged
ciated with Benign Prostatic Hyperplasia (BPH).
such as doxazosin and prazosin decrease ure- drug is excreted in the faeces. POM AVODART® (GSK)
Capsule, Dutasteride 0.5 mg; yellow oblong cap. Contra-indications, Precautions, etc: see
thral resistance and may relieve the obstruction Indications: As monotherapy, treatment and
marked ‘GX CE2’. under Doxazosin above.
and BPH symptoms. Doxazosin acts within 1-2 prevention of progression of benign prostatic
0.5 mg – 30’s; 90’s. Dose: For Benign prostate hyperplasia, Usually
weeks to decrease the severity of BPH symp- hyperplasia (BPH) through alleviating symptoms,
0.4 mg once daily; may incerease to
toms and improve urinary flow rate. reducing prostate size (volume), improving
urinary flow rate and reducing the risk of acute FINASTERIDE 0.8 mg once daily if no response after
Indications: Treatment of both the urinary out-
Therapeutic category: Antiandrogen; Testos- 2-4 weeks.
flow obstruction and obstructive and irritative urinary retention (AUR) and the need for BPH
terone 5α-reductase inhibitor. Administer approx. 30 mins follow-
symptoms associated with BPH. Obstructive related surgery. In combination with the alpha
EMDEX
Pharmacology: The development of the ing the same meal each day. To be
symptoms such as hesitation, intermittency, blocker tamsulosin, for the treatment of sympto-
prostate gland and subsequent benign pros- swallowed whole and not crushed or
dribbling. weak urinary stream, incomplete matic BPH in men with enlarged prostate. Also for
tatic hyperplasia (BPH) is dependent upon chewed.
emptying of the bladder. Irritative symptoms reduction in the risk of prostate cancer in men
conversion of testosterone to dihydrotestos- If administration is discontinued or
include nocturia, daytime frequency, urgency, at increased risk of developing the disease.
terone (DHT) within the prostrate. Finasteride interrupted for several days at either
burning. Contraindications: Hypersensitivity to
belongs to a class of specific inhibitors of the 0.4 mg or 0.8 mg dose, therapy
Contra-indications, Precautions, etc: see dutasteride, other 5α-reductase inhibitors, or
5α−reductase, an intracellular enzyme which should be started again with 0.4 mg
Doxazosin in Section 5.3.3. any component of the preparation; Preganancy,
metabolises testosterone into the more potent once daily dose.
Dose: Benign prostatic hyperplasia, initially women of child bearing potential, and children.
androgen, DHT. Finasteride has no affinity for No dosage adjustment in renal
1 mg once daily in the a.m. or p.m.; Precautions: Women and children must avoid
the androgen receptor. impairment and in mild to moderate
increased if necessary at intervals of contact with capsules (wash immediately with
Indications: Treatment and control of benign hepatic insufficiency.
1-2 weeks to 2 mg, 4 mg and max. 8 soap and water if contact is made) – can be
mg once daily. absorbed thru the skin. Hepatic impairment. prostatic hyperplasia (BPH) to cause regression POM CONTIFLO OD® (Ranbaxy)
Maintenance, usually 2-4 mg daily. Perform digital rectal exam to rule out prostate of the enlarged prostate, improve urinary Capsule, Tamsulosin HCl 0.4 mg; cap. containing
Note: Routine check on BP is recommended. cancer before initiating therapy & periodically flow, and improve the symptoms associated controlled-release beads.
afterwards. Determine baseline serum PSA with BPH. POM FLOSURE® (Biostadt)
POM CARDURA® (Pfizer)
(prostate-specific antigen) level before ther- Contra-indications: Hypersensitivity to Capsule, Tamsulosin (as HCI) 0.4 mg
Tablets, Doxazosin mesylate 2 mg, 4 mg.
2 mg – 10 (blister) apy and monitor values regularly afterwards. finasteride; women who are or may become 0.4 mg – 2 x 10’s (in blisters)
4 mg – 10 (blister) Approx. 50% decrease in mean serum PSA pregnant; children.
POM TAMSULON-XL® (PharmacyPlus)
levels after 6 months of treatment. Evaluate Precautions: Monitor for obstructive uropathy Capsule, Tamsulosin (as HCl) 400 mcg; sustained-re-
POM Doxazosin (Alpha)
sustained increases from lowest PSA level while in patients with large residual urine volume lease granules in capsule.
Tablets, Doxazosin mesylate 2 mg, 4 mg.
on treatment as that may be sign of prostate and/or severely diminished urinary flow. 400 mcg – 4 x 7’s
2 mg – 28’s.
4 mg – 28’s. cancer or non-compliance to therapy. Advise Perform digital rectal examination and other
POM URIFLOW® (Bond)
not to donate blood for at least 6 months evaluations for prostate cancer on patients
POM PENCOR® (Mark) Capsule, Tamsulosin HCI 0.4 mg
following the last dose of the drug. with BPH before initiating therapy and peri-
Tablet, Doxazosin mesylate equiv. to Doxazosin
Interactions: Co-administration with CYP3A4 odically thereafter. PROSTATE SPECIFIC ANTIGEN
2 mg, 4 mg.
2 mg – 10 x 10’s (in blisters) inhibitors may lead to increased dutasteride Adverse effects: Impotence, decreased (PSA) SELF-TEST
4 mg – 10 x 10’s (in blisters). exposure though further inhibition of 5α-re- lipido, decreased volume of ejaculate, breast
OTC PROSTA-Check® (PharmacyPlus)
ductase in unlikely. tenderness and enlargement, hypersensitivity
PSA test kit: Prosta-Check test allows determining a
DUTASTERIDE Adverse effects: Most commonly impotence, reactions including lip swelling and skin rash. high blood level, above 4 ng/ mL, of prostate specific
Therapeutic category: Antiandrogen; Testos- decreased libido, breast disorders (including Nursing action: antigen likely to show benign or malignant prostate
breast enlargement and tenderness), and • Administer with or without meals. hypertrophy.
terone 5α-reductase inhibitor. • Drug may have adverse effect on developing
Pharmacology: Dutasteride inhibits the con- ejaculation disorders. Rarely allergic reactions Pack: 1’s
male foetus; advise pregnant women to avoid NRN: 03-1620
version of testosterone to dihydrotestosterone including rash, pruritus, urticaria, localised contact with drug or semen of a patient taking
(DHT). DHT is the androgen primarily responsi- oedema, and angioedema; skin and subcu- this medication. Procedure: Available inside the kit
ble for the initial development and subsequent taneous tissue disorders; alopecia (primarily • Therapeutic response may take 3-6 months includ-
enlargement of the prostate gland. Testosterone body hair loss), hypertrichosis. ing increased urinary flow, hair growth.
Dose: By mouth, Benign Prostatic Hyperpla- Dose: By mouth, Adult, 5 mg daily with or
570 | 11.4.2 Drugs used in urological pain 11.4.3 Drugs used in erectile dysfunction (ED) | 571
11.4.2 Drugs used in urological pain the treatment of ED. Anatomical deformation of ide (NO) from nerve terminals and endothelial mended dosing frequency is once per
the penis, sickle cell anaemia, multiple myeloma, cells, which stimulates the synthesis of cGMP day. Not recommended for individu-
POTASSIUM CITRATE leukaemia (monitor closely). Lower doses are in smooth muscle cells. Cyclic GMP causes als <18 years.
Indications: Relief of discomfort in mild uri- recommended in hepatic impairment, elderly, smooth muscle relaxation and increased (Additional information sourced from Cialis monograph available
nary-tract infections; alkalinisation of urine. severe renal impairment and during concomi- blood flow into the corpus cavernosum. The from: http://www.medicines.org.uk)
Precautions: Renal impairment, cardiac dis- tant use of potent CYP3A4 inhibitors. inhibition of phosphodiesterase type 5 (PDE5)
Interactions: Sildenafil metabolism is prin- enhances erectile function by increasing the POM DABAFORT® (Dabak)
ease, elderly.
cipally mediated by the CYP3A4. Inhibitors amount of cGMP. Tadalafil inhibits PDE5. Be- Tablet, Tadalafil 20 mg; light brown heart-shaped tab.
Interactions: See Potassium salts in Appendix 1 20 mg – 4’s.
of these isoenzymes (such as Ketoconazole, cause sexual stimulation is required to initiate
POM Mist. Potassium Citrate (Gauze) POM SONAGRA® (Bond)
erythromycin or cimetidine) may reduce silde- the local release of nitric oxide, the inhibition of
Oral Liquid, Potassium citrate 1.5 g, citric acid 0.25 Capsule, Tadalafil 10 mg
g per 10 mL
nafil clearance while inducers of the enzymes, PDE5 by tadalafil has no effect in the absence
Pack: 200 mL; 2 L such as rifampicin, will decrease plasma levels of sexual stimulation. Tadalafil is more potent POM SUPALIS® (Crystal)
of sildenafil. on PDE 5 than on other phospodiesterases. Tablet, Tadalafil 20 mg; green round tab.
POM Moko Mist Potassium Citrate (New Healthway) Adverse effects: Headaches, flusing, dyspepsia, Tadalafil is readily absorbed after oral admin- 20 mg – 1 x 4’s (in satchets).
Solution, Potassium citrate 3 g, citric acid 0.5 g per
nasal congestion, UTI, abnormal vision, diarrhoea, istration and Cmax is about 2 hours after dosing. POM TADALIS® (Evans)
10 mL.
Pack: 200 mL dizziness, rash. Other less common adverse Food has no effect on the rate and extent of Tablets, Tadalafil 10 mg, 20 mg; f-c tabs.
events include chest pain, abdominal pain, absorption. It is 94% bound to plasma proteins. 10 mg – 4’s
11.4.3 Drugs used in erectile asthenia, cardiovascular disturbances, GI dis- Metabolism is predominantly by the CYP3A4 20 mg – 4’s
dysfunction (ED) turbances, metabolic and nutritional disorders; isoform and excretion is mainly in the faeces,
POM WELFIL® (Barata)
others are disturbances of the musculoskeletal, as inactive metabolites. Tablet, Tadalafil 20 mg; f-c tab
SILDENAFIL CNS, respiratory tract, skin, special senses and Indications: Treatment of erectile dysfunction. 20 mg – 4’s (in blisters)
EMDEX
urogenital tract. Contra-indications: Hypersensitivity to
Pharmacology: Sexual stimulation produces POM WINFORCE® (Megalife sciences)
Advice to patients: Sildenafil offers no protec- tadalafil; avoid coadministration with nitrates;
erection of the penis via the release of nitric oxide Tablet, Tadalafil 20 mg; f-c tab
tion against sexually transmitted diseases and avoid use with alpha-blockers other than 0.4
(NO) in the corpus cavernosum. NO then activates 20 mg – 1 x 4’s
protective measures are necessary to guard mg once-daily tamsulosin.
the enzyme guanylate cyclase, which results in POM XTENDA® (Lifeback)
against such including HIV. Precautions: Not recommended for patients
increased levels of cyclic guanosine monophos- Tablet, Tadalafil 20 mg; f-c tabs.
Dose: By mouth, usually 50 mg once daily to with CVD such as MI within the last 90 days;
phate (cGMP), producing smooth muscle relax-
be taken approx. 1 hour before sexua unstable angina or angina occurring during
ation in the corpus cavernosum and allowing VARDENAFIL
activity; may be increased to 100 sexual intercourse; CHF in the last 6 months;
inflow of blood. Sildenafil enhances the effect of Therapeuticcategory: PDE-5 inhibitor (Phos-
mg or reduced to 25 mg once daily uncontrolled arrhythmias; hypotension
nitric oxide (NO) by inhibiting phosphodiesterase phodiesterase-5 enzyme inhibitor).
depending on effectiveness and tol- (<90/50 mm Hg), or uncontrolled hypertension
type 5 (PDE5), which is responsible for degradation Indications: Treatment of erectile dysfunction.
erance. In conditions associated with (>170/100 mm Hg); stroke within the last 6
of cGMP in the corpus cavernosum. Sildenafil Contra-indications: Hypersensitivity to varde-
increased plasma levels of sildenafil months. Patients at risk of priapism (such as
has no direct relaxant effect on isolated human nafil; avoid co-administration with nitrates or
such as elderly, hepatic impair- sickle cell anaemia, multiple myeloma, or leu-
corpus cavernosum. It has no effect also in the nitric oxide donors (may potentiate the hypo-
ment, severe renal impairment and kaemia), or those with anatomical deformation
absence of sexual stimulation. Sildenafil is rapidly tensive effects of nitrates); avoid co-adminis-
concomitant use of potent CYP3A4 of the penis. Renal or hepatic impairment.
absorbed after oral administration, with absolute tration with potent inhibitors of CYP3A4 such
inhibitors, a starting dose of 25 mg Interactions: CYP3A4 inhibitors (ketocona-
bioavailability of about 40%. Tmax is about 30-120 as protease inhibitors e.g. indinavir or ritonavir.
once daily is recommended. Sildenafil zole, ritonavir, erythromycin, itraconazole,
minutes following oral dosing in the fasted state. Precautions: Assess the cardiovascular status
may be taken anywhere from 4 hours and grapefruit juice) may increase tadalafil
High fat meal will reduce the rate of absorption. of patients prior to therapy (has vasodilator
to 0.5 hour before sexual activity. exposure. CYP3A4 inducers (rifampin, carba-
Elimination is mainly by hepatic metabolism, effects which may result in mild and transient
POM VIAGRA® (Pfizer)
mazepine, phenytoin, and phenobarbitol)
with an active metabolite similar in properties decreases in blood pressure); patients with
Tablet, Sildenafil citrate 50 mg; blue, f-c, rounded-di- may decrease tadalafil exposure. Tadalafil can
to the parent compound. Sildenafil and its major anatomical deformation of the penis (such as
amond-shaped tab. potentiate the hypotensive effect of nitrates
metabolite are both approximately 96% bound to angulation, cavernosal fibrosis or Peyronie’s
50 mg – 4 (blister pack). leading to unsafe drop in BP. Use with alcohol
plasma proteins. Metabolites are excreted mainly disease) or in patients who have conditions
may increase blood-pressure-lowering effects
in the faeces and to a lesser extent in the urine. POM VIVERA® (Shrezar)
which may predispose them to priapism (such
Tablet, Sildenafil citrate) 100 mg; f-c tab of both drugs leading to increase in heart rate,
Indications: Treatment of erectile dysfunction. as sickle cell anaemia, multiple myeloma or
100 mg – 1 x 4’s; 10 x 1 x 4’s (in blisters) decrease in standing blood pressure, dizziness,
Contra-indications: Hypersensitivity to silde- leukaemia); avoid co-administration with other
and headache. Alpha-blockers.
nafil. Avoid coadministration with nitrates; treatments for erectile dysfunction. Avoid use
TADALAFIL Adverse effects: Dizziness, headache, dys-
children, women. in severe hepatic impairment, endstage renal
Pharmacology: Tadalafil is a selective, revers- pepsia, abdominal pain, hypotension, myalgia,
Precautions: Thorough medical history and disease requiring dialysis, hypotension (resting
ible inhibitor of cyclic guanosine monophos- back pain, nasal congestion, flushing, palpi-
physical examination are needed for proper systolic blood pressure of <90 mmHg), recent
phate (cGMP)-specific phosphodiesterase type tation. Rarely allergic reaction, rash, urticaria,
diagnosis of erectile dysfunction (ED), determi- history of stroke or myocardial infarction
5 (PDE5). Penile erection during sexual stimu- prolonged erection, visual disturbances.
nation of underlying causes and selection of (within 6 months), unstable angina, and known
lation is caused by increased penile blood flow Dose: Adult men, initially 10mg, taken prior
appropriate treatment. Establishment of cardi- hereditary degenerative retinal disorders such
resulting from the relaxation of penile arteries to anticipated sexual activity; may be
ovascular status of the patient is recommended as retinitis pigmentosa. Patients with bleeding
and corpus cavernosal smooth muscle. This increased to 20 mg or decreased to 5
before initiating any treatment for ED. Avoid disorders or significant active peptic ulceration.
response is mediated by the release of nitric ox- mg, based on individual efficacy and
co-administration with other agents used for Not indicated for use in newborns, children
tolerability. The maximum recom-
572 | 11.4.4 Drugs used for overactive bladder (OAB)
or women. rivative (in extensive metabolisers accounting
Interactions: Vardenafil is metabolized predom- for majority of population). In poor CYP2D6
inantly by CYP3A4, with some contribution from metabolisers, accounting for 7% of popula-
CYP3A5 and CYP2C isoforms; clearance may be tion, metabolism is via CYP3A4 to inactive
reduced inhibitors of these enzymes. Max. dose N-dealkylated metabolites. Clinical use not
of 5 mg Vardenafil should not be exceeded when affected by metabolism differences as toltero-
used in combination with potent CYP3A4 inhibi- dine and its CYP2D6-dependent metabolite,
tors viz ketoconazole, itraconazole, erythromycin, 5-hydroxymethyl tolterodine are equipotent.
indinavir, or ritonavir. Avoid use with dosages of ke- Renally excreted (77%) mainly as metabolites
toconazole and itraconazole higher than 200 mg. and some as unchanged drug (<1%), and via
Adverse reactions: Headache, dizziness, faeces (17%).
flushing, erythema, nasal congestion, oedema Indications: Treatment of overactive bladder
mucosal, rhinitis, dyspepsia, nausea. with symptoms of urinary frequency and
Advice to patients: May take with or without urgency with or without urge incontinence.
food; do not drive or operate machinery until Contra-indications: Hypersensitivity to toltero-
the effect of drug is established; efficacious dine or its ingredients; urinary retention, gastric
when taken up to 4-5 hours before sexual retention, uncontrolled narrow-angle glaucoma,
activity. myasthenia gravis, severe ulcerative colitis, or
Dose: By mouth, Usually 5-10 mg once daily toxic megacolon.
approximately 25-60 minutes before Precautions: Patients with clinically significant
sexual activity; may be increased up bladder outflow obstruction because of the risk
to a max. 20 mg once daily. of urinary retention. Antimuscarinics decrease
Elderly (above 65 years): Start 5 mg GI motility and should be avoided in patients
once daily; may be increased up to with gastrointestinal obstructive disorders,
max. 20 mg once daily based on effi- such as pyloric stenosis because of the risk of
EMDEX
cacy and tolerability. Renal clearance gastric retention. Renal & hepatic impairment;
may be reduced in elderly. QT prolongation. Pregnancy, lactation.
Children (from birth to 16 years): Not Interactions: Co-administration with potent
recommended. CYP3A4 inhibitors may cause increased
Hepatic impairment: Use normal dose serum concentrations of tolterodine in poor
in mild hepatic impairment and start CYP2D6 metabolisers with (subsequent) risk
5 mg once daily in moderate hepatic of overdosage (see under Pharmacology).
impairment; may be increased to a Co-administration with potent CYP2D6 inhib-
max. 10 mg based on tolerability and itors (e.g., Fluoxetine) does not cause clinically
efficacy. Not recommended in severe significant interaction since tolterodine and its
hepatic impairment. CYP2D6-dependent metabolite, 5-hydroxym-
Renal impairment: No dosage adjust- ethyl tolterodine are equipotent.Tolterodine
ment is needed. is not an inhibitor of the following hepatic
POM LEVITRA® (GSK)
enzymes: CYP2D6, 2C19, 2C9, 3A4 or 1A2.
Tablets, Vardenafil (as monohydrochloride trihy- Adverse effects: Dry mouth, dyspepsia,
drate) 5 mg, 10 mg, 20 mg. constipation, abdominal pain; dry eyes, abnor-
5 mg – 1’s; 2’s; 4’s; 8’s; 12’s. mal vision, dry skin; urinary retention, dysuria;
10 mg – 1’s; 2’s; 4’s; 8’s; 12’s. headache, somnolence, nervousness.
20 mg – 1’s; 2’s; 4’s; 8’s; 12’s. Dose: Adult (including Elderly), by mouth,
1-2 mg twice daily; depending on
11.4.4 Drugs used for overactive response and tolerance. Evaluate
bladder (OAB) treatment after 2-3 months Co-ad-
ministration with potent CYP2D6 in-
TOLTERODINE hibitors, hepatic or renal impairment,
Pharmacology: Tolterodine is a competitive 1 mg twice daily.
muscarinic receptor antagonist. Both urinary Child: Not recommended.
bladder contraction and salivation are me- POM ROLITEN® (Ranbaxy)
diated via cholinergic muscarnic receptors. Tablet, Tolterodine tartrate 2 mg; white f-c tab.
Undergoes extensive hepatic metabolism via marked “2”
CYP2D6 to form active 5-hydroxymethyl de- 2 mg – 10’s
12. Antineoplastic and
immunosuppressive
drugs, and drugs used
in palliative care
12.1 Cytotoxic (antineoplastic) drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 574
12.1.1 Alkylating drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 575
12.1.2 Cytotoxic antibiotics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 577
12.1.3 Antimetabolites and related therapy. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 580
12.1.4 Vinca alkaloids and etoposide. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 583
12.1.5 Other antineoplastic drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 585
12.2 Immunosuppressive drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 590
EMDEX
12.2.1 Cytotoxic immunosuppressants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 590
12.2.2 Corticosteroids and other immunosuppressants. . . . . . . . . . . . . . . . . . . . . . . . 591
12.2.3 Interferons. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 595
12.3 Sex hormones and antagonists used in malignant diseases. . . . . . . . . . . . . . . . 596
12.4 Drugs used in palliative care. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 601
574 | 12.1 Cytotoxic (antineoplastic) drugs 12.1.1 Alkylating drugs | 575
Management of Cancer involves three lines consulted. compresses until the inflammation subsides; Good symptom control is the best way to
of attack: Surgery; Radiation therapy and Cytotoxic drugs are often combined with in severe cases, hydrocortisone cream may be prevent anticipatory symptoms and the ad-
Chemotherapy. other classes of drugs (section 12.3) in the applied topically to the site of inflammation. dition of diazepam to antiemetic therapy is
Chemotherapy is used as palliative measure treatment of malignant conditions. Such drugs The manufacturer’s literature should also be helpful because of its sedative, anxiolytic and
and to prolong life. It involves the use of include hormone agonists and antagonists, consulted for more specific information. amnesic effects.
1. Cytotoxic drugs corticosteroids and immunostimulant drugs. ADVERSE EFFECTS Hyperuricaemia. Hyperuricaemia may com-
2. Steroid hormones, and Combinations are, however, more toxic than Cytotoxic drugs have a considerable potential plicate treatment of conditions such as
3. Immunotherapy. single drugs. to damage normal tissue. Specific adverse non-Hodgkin lymphomas and leukaemia.
The study of the cell-cycle provides a rational The following information covers drugs that effects apply, but a number of effects are Renal damage may result from the formation
basis for the design of cancer treatment pro- have specific anti-tumour activity. However, common to all cytotoxics such as bone-marrow of uric acid crystals. Patients should be ade-
tocols. There are cell-cycle specific (CCS) and they are toxic drugs which should be used and immunological suppression. Furthermore, quately hydrated and hyperuricaemia may
cell-cycle non-specific (CCNS) drugs. with great care and close monitoring. The the concomitant use of immunosuppressive be managed with allopurinol (section 2.2.2)
specific doses and details of contra-indications, drugs will enhance susceptibility to infections. initiated 24 hours before cytotoxic treatment
CCS drugs: Asparaginase, Azathioprine, and continued for 7 to 10 days afterwards.
Bleomycin, MTX, Vinblastine, Vinscritine, precautions and adverse effects for cytotoxic Fever associated with neutropenia or immu-
Cytarabine. drugs have been omitted from this section nosuppression requires immediate treatment Alopecia. Alopecia is common during treat-
since treatment should be undertaken by with antibiotics. ment with cytotoxic drugs. There is no drug
CCNS drugs: Actinomycin D, Bleomycin, specialists using agreed regimens. treatment, but the condition often reverses
Busulfan, Carmustin, Chlorambucil, Cyclophos- Nausea and vomiting. Nausea and vomiting
PRECAUTIONS AND CONTRA-INDICATIONS following administration of cytotoxic drugs spontaneously once treatment has stopped.
phamide, Daunorubicin.
Treatment with cytotoxic drugs should be and abdominal radiotherapy are often distress- Oral mucositis. Oral mucositis is common dur-
Agents may be selected which exert their ef- ing and may compromise further treatment. ing cancer chemotherapy, particularly with
initiated only after baseline tests of liver and
EMDEX
fects primarily in different phases of the cycle. Symptoms may be acute (occurring within 24 fluorouracil, methotrexate and the anthracy-
Sequencing of drug combinations can be done kidney function have been performed and
baseline blood counts established. It may be hours of treatment), delayed (first occurring clines. Prevention of a sore mouth is important,
to provide maximal benefits. Drug combina- more than 24 hours after treatment), or antic- because once it has developed treatment is
tions provide maximal cell kill within the range necessary to modify or delay treatment in cer-
tain circumstances. The patient should also be ipatory (occurring before subsequent doses). much less effective. Brushing teeth with a soft
of toxicity tolerated by the host for each drug Delayed and anticipatory symptoms are more brush 2–3 times daily and rinsing the mouth
and prevent or slow the development of new monitored regularly during chemotherapy and
cytotoxic drugs withheld if there is significant difficult to control than acute symptoms and frequently are probably effective preventative
resistant cells. Essentially, all classes of anti- require different management. measures. Sucking icechips during short infu-
cancer drugs select and allow overgrowth of deterioration in bone-marrow, liver or kidney
function. Susceptibility to drug-induced nausea and sions of fluorouracil is also helpful. Treatment
specifically drug–resistant neoplastic cells. This involves regular use of saline mouthwashes.
is a major cause of chemotherapeutic failure. Most cytotoxic drugs are teratogenic and vomiting varies amongst patients; those af-
fected more include women, patients under Generally mucositis is self-limiting, but it can
should not be administered during pregnancy be a focus for blood-borne infection in the
12.1 Cytotoxic (antineoplastic) drugs especially in the first trimester. Contraceptive 50 years, anxious patients and those who
suffer from motion sickness. Repeated expo- absence of good oral hygiene. Any pain caused
12.1.1 Alkylating drugs
measures are required during therapy and by mucositis should be dealt with effectively.
possibly for a period after therapy has ended. sure to the cytotoxic therapy also increases
12.1.2 Cytotoxic antibiotics
Cytotoxic drugs are also contraindicated during susceptibility.
12.1.3 Antimetabolites and related therapy 12.1.1 Alkylating drugs
12.1.4 Vinca alkaloids and etoposide breastfeeding. The risk of venous thromboem- Cytotoxic drugs associated with a low risk of
12.1.5 Other antineoplastic drugs bolism in cancer is increased by chemotherapy; emesis include etoposide, fluorouracil, low- Alkylating drugs are among the most widely
prophylaxis against thromboembolism may dose methotrexate, and the vinca alkaloids; used drugs in cancer chemotherapy. They act
NOTE: WHO advises that adequate resources and spe-
be appropriate for patients receiving chemo- those with an intermediate risk include lower by damaging DNA and therefore interfering
cialist supervision are a prerequisite for the introduction
of this class of drugs. Specific expertise, diagnostic preci- therapy. doses of cyclophosphamide, doxorubicin, and with cell replication. However, there are two
sion, individualization of dosage or special equipment high-dose methotrexate; and the highest risk complications. Firstly, they affect gametogen-
Cytotoxic drugs should be administered with esis and may cause permanent male sterility; in
are required for their proper use. is with cisplatin, high-dose cyclophosphamide,
care to avoid undue toxicity to the patient or women, the reproductive span may be short-
exposure during handling by the health care and dacarbazine.
The treatment of cancer with drugs, radiother- ened by the onset of a premature menopause.
apy and surgery is complex and should only be provider. Local policies for the handling and For patients at a low risk of emesis, pretreat- Secondly, they are associated with a marked
undertaken by an oncologist. For this reason, reconstitution of cytotoxic drugs should be ment with an oral phenothiazine (for example increase in the incidence of acute non-lympho-
the following information is provided merely strictly adhered to; also all waste, including chlorpromazine, section 1.2), continued for cytic leukaemia, in particular when combined
as a guide. Chemotherapy may be curative patient’s body fluids and excreta (and any up to 24 hours after chemotherapy, is often with extensive radiation therapy.
or used to alleviate symptoms or to prolong material contaminated by them) should be helpful. For patients at a higher risk dexameth-
treated as hazardous. asone 6–10 mg by mouth (section 10.3) may Cyclophosphamide requires hepatic activa-
life. Where the condition can no longer be tion; it can therefore be given orally and is
managed with cytotoxic therapy, alternative Extravasation of intravenously administered be added before chemotherapy. For patients
at a high risk of emesis or when other thera- not vesicant when given intravenously. Like
palliative treatment (section 12.4) should be cytotoxic drugs can result in severe pain and all alkylating drugs its major toxic effects are
considered. necrosis of surrounding tissue. If extravasation pies are ineffective, high doses of intravenous
metoclopramide (section 4.6) may be used. myelosuppression, alopecia, nausea and vom-
For some tumours, single-drug chemotherapy occurs, aspiration of the drug should first be at- iting. It can also cause haemorrhagic cystitis;
may be adequate, but for most malignancies tempted, then the affected limb is elevated and Dexamethasone is the drug of choice for the an increased fluid intake for 24 to 48 hours will
a combination of drugs provides the best warm compresses applied to speed and dilute prevention of delayed symptoms; it is used help to avoid this complication. Cyclophospha-
response; specialist literature should be the infusion or it is localized by applying cold alone or with metoclopramide. mide is used either as part of treatment or as an
576 | 12.1.1 Alkylating drugs 12.1.2 Cytotoxic antibiotics | 577
adjuvant in non-Hodgkin lymphomas, breast POM Busulfan (EDL 7) voiding is too infrequent in the night to prevent and hand-foot syndrome may occur.Dactin-
cancer, childhood leukaemia, and ovarian can- Tablet, Busulfan 2 mg. cystitis.. omycin is used to treat paediatric cancers. Its
cer. It is also used in several palliative regimens. • Avoid all IM injections when platelets are below toxicity is similar to that of doxorubicin, but
POM MYLERAN® (SKG)
100,000/mm3. it is not cardiotoxic.Daunorubicin is used in
Chlorambucil is used to treat chronic lympho- Tablets, Busulfan 0.5 mg, 2 mg.
• Encourage adequate fluid intake and frequent
cytic leukaemia, non-Hodgkin lymphomas, 0.5 mg – 25 acute leukaemias. Its toxicity is similar to that
voiding to help prevent haemorrhagic cystitis.
2 mg – 25. of doxorubicin.
Hodgkin disease, ovarian cancer and Walden- • Advise both male and female patients to use
strom (primary) macroglobulinaemia. Adverse contraceptive measures during treatment and for
CHLORAMBUCIL 12 weeks after end of therapy; drug is potentially BLEOMYCIN
effects, apart from bone marrow suppression,
are uncommon. However, severe widespread Indications: Chronic lymphocytic leukaemia; teratogenic. Indications: Adjunct to surgery and radio-
some non-Hodgkin lymphomas; Hodgkin • Monitor serum uric acid; allopurinol may be therapy in palliative treatment of Hodgkin
rash can develop and may progress to Ste-
disease, and Waldenstrom (primary) mac- given with adequate hydration to prevent hype- and non-Hodgkin lymphomas; reticulum
vens-Johnson syndrome or toxic epidermal ruricaemia.
necrolysis. If a rash occurs, further treatment roglobulinaemia. cell sarcoma and lymphoma; carcinomas of
• Warn patient that alopecia, which is reversible,
with chlorambucil is contraindicated. Contra-indications: see notes above and con- the head, neck, larynx, cervix, penis, skin,
may occur; a wig or hairpiece may make him/her
sult specialist literature; pregnancy (Appendix feel better. vulva, testicles and including embryonal cell
Chlormethine (mustine) forms part of the 2) and breastfeeding (Appendix 3). Dose: Consult specialist literature. carcinoma, choriocarcinoma and teratoma;
regimen for treatment of advanced Hodgkin Precautions: see notes above and consult malignant effusions.
disease and malignant lymphomas. Its toxicity specialist literature; severe hepatic impairment POM Cyclophosphamide (WMF 8.2) Contra-indications: see notes above and con-
includes myelosuppression, severe nausea and (Appendix 5); renal impairment (Appendix 4); Tablet, Cyclophosphamide 25 mg.
sult specialist literature; pregnancy (Appendix
vomiting, alopecia and thrombophlebitis due interactions: Appendix 1.
Powder for injection, Cyclophosphamide 500-mg
in vial. 2) and breastfeeding (Appendix 3).
to vesicant effect. Adverse effects: see notes above and consult Precautions: see notes above and consult spe-
specialist literature. POM Cyclophosphamide (EDL 7) cialist literature; renal impairment (Appendix
BUSULFAN
EMDEX
Advice to patients: Notify physician immedi- Tablets, Cyclophosphamide 25 mg, 50 mg. 4); interactions: Appendix 1.
Pharmacology: Acts by inhibition of DNA Injections, Cyclophosphamide 100 mg, 500 mg, 1 g;
ately if sore throat or bleeding occurs; contra- Adverse effects: see notes above and consult
replication like other alkylating drugs. See powder in vials.
ceptive measures are recommended during specialist literature.
notes above. therapy (Drug is potentially teratogenic). POM ALKYLOXAN® (Alpha) Note: Irritant to tissues.
Indications: Chronic myeloid leukaemia Nursing action: See under Busulfan. Tablet, Cyclophosphamide 50 mg (anhydrous); white Advice to patients: Hair will reappear after
Contra-indications: Porphyria, pregnancy, Dose: Consult specialist literature. tab. marked ‘CWP’ ‘A’ discontinuance of medication; maintain excel-
lactation. 50 mg – 50’s
POM Chlorambucil (WMF 8.2)
lent oral hygiene habits; report any coughing,
Precautions: May induce severe bone marrow POM CYCLOCEL® (L’Pacemaker) shortness of breath, or wheezing; skin rashes,
Tablet, Chlorambucil 2 mg.
hypoplasia (frequent blood count required); if Injection, Cyclophosphamide (anhydrous) 500 mg shaking, chills, or transient fever may occur
WBC is high, give hydration and allopurinol to POM Chlorambucil (EDL 7) per vial. following administration.
prevent hyperuricaemia. Tablets, Chlorambucil 2 mg, 5 mg. Pack: One single vial in a carton. Nursing action:
Adverse effects: Bone marrow suppression POM LEUKERAN® (SKG) POM CYCRAM® (Alpha) • Check injection site for signs of irritation.
and blood disorders; endocardial fibrosis; Tablet, Chlorambucil 2 mg, 5 mg; both yellow tabs. Injection, Cyclophosphamide 500 mg; powder for • Give anti-emetic 30-60 min before giving drug to
hyperpigmentation of skin, urticaria, alopecia; 2 mg – 25 injection in vials. reduce nausea.
nausea, vomiting, diarrhoea; muscle weakness. 5 mg – 25. • Encourage deep breathing exercises; raise HOB to
Advice to patients: Watch for signs of bleed- facilitate breathing.
12.1.2 Cytotoxic antibiotics
ing; excellent oral hygiene is needed to mini- CYCLOPHOSPHAMIDE • Patients should be monitored for signs of pul-
Bleomycin is used in regimens for the treat- monary toxicity; check body weight at regular
mize oral discomfort. Indications: Malignant lymphomas includ-
ment of Hodgkin disease and testicular cancer. intervals.
Nursing action: ing non-Hodgkin lymphomas, lymphocytic • Monitor for signs of anaphylaxis; allergic reactions
It has several antineoplastic drug toxicities; it is
• Give at the same time each day, on empty stomach. lymphoma, Burkitt lymphoma; multiple may be delayed for several hours, especially in
• Avoid all I.M injections when platelets are below known to cause dose-related pneumonitis and
myeloma; leukaemias, mycosis fungoides; patients with lymphoma.
100,000/mm3. fibrosis which can be fatal, and is associated
neuroblastoma; adenocarcinoma of the ovary; • Inform patient that alopecia may occur, but is
• Observe for signs of infection (fever, sore-throat, with rare acute hypersensitivity reactions.
retinoblastoma; breast cancer. reversible.
fatigue), bleeding from gum or nose, and report Cutaneous toxicity has also been reported. • Check temperature and pulse for bleomycin-in-
to physician.
Contra-indications: see notes above and con-
sult specialist literature; pregnancy (Appendix Doxorubicin is a widely used anthracycline duced fever; may treat with antipyretic.
• Educate patient on good oral hygiene; maintain • More stable in glass bottles than in plastic IV bags.
strict medical asepsis. 2) and breastfeeding (Appendix 3). antibiotic used to treat acute leukaemias,
Precautions: see notes above and consult lymphomas, and a variety of solid tumours. Dose: Consult specialist literature
• Instruct patient to report cough and progressive
Doxorubicin also plays a palliative role in the Note: Doses of bleomycin are expressed in interna-
dyspnoea with alveolar exudate which may be due specialist literature; renal impairment (Appen- tional units. 1 Bleomycin Unit in the USP is equivalent
to drug toxicity and not pneumonia; dosage may dix 4) and hepatic impairment (Appendix 5); treatment of other malignancies. The primary
to 1000 international units.
need to be adjusted. interactions: Appendix 1. toxic effects are myelosuppression, alopecia,
• Encourage deep breathing exercises. Adverse effects: see notes above and consult nausea, vomiting, and dose-related cardiomy- POM Bleomycin (WMF 8.2)
• Anticoagulants and aspirin products including opathy. It is also vesicant and can cause severe Powder for injection, Bleomycin (as sulfate) 15 mg
specialist literature.
ibuprofen should be used cautiously; instruct skin ulceration on extravasation. Liposomal in vial.
patient to avoid aspirin-containing OTC products. Advice to patients: Drink plenty of fluids be-
fore and after doses; report any blood in urine. formulations of doxorubicin [not included on POM Bleomycin (EDL 7)
• Monitor serum uric acid; allopurinol may be
given with adequate hydration to prevent hype- Nursing action: WHO Model List] are now available. They may Injection, Bleomycin sulfate 15,000 units; powder
• Give in the morning so that drug can be eliminated reduce the incidence of cardiotoxicity and for injection in vial.
ruricaemia.
Dose: See lit. before bedtime; do not give at bedtime because local necrosis, but severe infusion reactions POM BLEOCIN® (Alpha)
578 | 12.1.2 Cytotoxic antibiotics 12.1.2 Cytotoxic antibiotics | 579
Injection, Bleomycin sulfate 15,000 units; powder in vial. POM CELONDOXILYD 50® (L’Pacemaker) alkalinization, and prophylaxis with allopurinol
for injection in vials. Injection, Doxorubicin HCI 50 mg, mannitol 300 mg, to prevent hyperuricemia may minimize poten-
DOXORUBICIN lactose(anhydrous) 250 mg, methylparaben 10 mg tial complications of tumour-lysis syndrome.
DACTINOMYCIN per sterile lyophilized vial. Renal and hepatic dysfunction. May impart
Synonym: ADR; Hydroxydaunomycin.
Pack: Single dose vial.
Synonym: Actinomycin D; ACT. Indications: Acute leukaemias; carcinomas of a red color to the urine for 1-2 days after
Indications: Trophoblastic tumours, Wilm the breast, bladder, ovary and thyroid; neu- POM RUBIDOX® (Reals) administration.
tumour, Ewing sarcoma, rhabdo-myosarcoma roblastoma; Wilm tumour; non-Hodgkin and Injection, Doxorubicin HCI 50 mg; powder in vial Adverse effects: GI disturbances such as nau-
Contra-indications: See notes above and con- Hodgkin lymphomas; soft tissue sarcomas, Pack: 50 mg (in vial). sea, vomiting and diarrhoea; Myelosuppres-
sult specialist literature; pregnancy (Appendix osteosarcoma. sion; Cardiotoxicity; Alopecia, accompanied
2) and breastfeeding (Appendix 3) EPIRUBICIN by lack of beard growth in males. Mucositis,
Contra-indications: See notes above and con-
Precautions: See notes above and consult sult specialist literature; pregnancy (Appendix Pharmacology: Epirubicin, an anthracycline usually involving stomatitis; Red coloration of
specialist literature; interactions: Appendix 1 2) and breastfeeding (Appendix 3) derivative, is a cytotoxic antibiotic whose ac- urine for 1-2 days after administration; Extrava-
Adverse effects: See notes above and consult Precautions: See notes above and consult spe- tivity is related to its ability to bind to DNA. It is sation, injection site reactions; Hot flushes;
specialist literature. cialist literature; hepatic impairment (Appendix structurally related to doxorubicin. Cell culture Anorexia, dehydration.
NOTE: Irritant to tissues. 5); interactions: Appendix 1. studies have shown rapid cell penetration, Dose: Consult product literature.
Advice to patients: Notify physician of symp- Adverse effects: See notes above and consult localisation in the nucleus and inhibition of Administration: Epirubicin should be administered
toms of infection viz fever, persistent sore specialist literature. nucleic acid synthesis and mitosis. Epirubicin by intravenous injection. It is not active when given
throat, bleeding, bruising, fatigue or malaise. Note: Irritant to tissues. has proved to be active on a wide spectrum orally and should not be injected intramuscularly or
Nursing action: Advice to patients: Discolours urine red/ of experimental tumors including L 1210 and intrathecally. It is advisable to give the drug via the
• Administer by slow IV push over 10-15 minutes; do P 388 leukemias, sarcomas SA 180 (solid and tubing of a freely-running IV saline infusion after
orange; immediately report any change in
checking that the needle is well placed in the vein.
not give I.M or S.C.; avoid extravasation (extremely sensation (e.g., stinging) at injection site during ascetic forms), melanoma B 16, mammary
This method minimizes the risk of drug extravasation
EMDEX
damaging to soft tissue and can lead to tissue infusion (may be an early sign of infiltration). carcinoma, Lewis lung carcinoma and colon
necrosis, pain and ulceration). and makes sure that the vein is flushed with saline
Nursing action: carcinoma 38. It has also shown activity against after the administration of the drug. Extravasation
• Give anti-emetic 30-60 min before giving drug to
• Administer by slow I.V. push into tubing of freely human tumors transplanted into athymic nude from the vein during injection may give risk to severe
reduce nausea; increase fluid intake.
• Observe for signs of infection and bleeding, and
flowing I.V.; never give I.M. or S.C.; avoid extravasa- mice (melanoma, mammary lung, prostatic tissue lesions even necrosis. Venous necrosis may
tion. Local erythematous streaking along the vein and ovarian carcinomas). Toxicity studies in result from injection into small vessels or repeated
report to physician.
and/or facial flushing may indicate too rapid a rate animals have indicated that Epirubicin has injections into the same vein.
• Inform patient that alopecia may occur, but is
of administration. Epirubicin should not be mixed with heparin
reversible; recommend wig to patient. a better therapeutic index and less systemic
• Give anti-emetic before giving drug to reduce due to chemical incompatibility which may
Management of extravasation: Stop infusion; nausea.
and cardiac toxicity than doxorubicin. In pa-
apply ice immediately for 30-60 minutes; then tients with-normal hepatic and renal function, lead to precipitation. When the drugs are in
• Inform patient that alopecia may occur, but is
alternate off/on every 15 minutes for one day. reversible. plasma levels after IV injection of 75-90 mg/m2 certain proportions, Epirubicin can be used in
Dose: Consult specialist literature. • Advise patient that orange or red urine for 1-2 of the drug follow a tri-exponential decreasing combination with other antitumour agents,
days is normal and does not indicate the presence pattern with a very fast first phase and a slow but it is not recommended that it be mixed
POM Dactinomycin (WMF 8.2) with these drugs in the same syringe
of blood. terminal phase with a mean half-life of about
Powder for injection, Dactinomycin 500-microgram
• Monitor serum uric acid; allopurinol may be 40 hours. Undergoes hepatic metabolism and
in vial. POM EPIZIN® (Alpha)
given with adequate hydration to prevent hype- excretion is mainly in the bile. Injection, Epirubicin HCl 50 mg; red freeze-dried cake
POM Dactinomycin (EDL 7) ruricaemia.
Indications: A wide spectrum of neoplastic in a colourless transparent vial with red cap.
Injection, Dactinomycin 0.5 mg; powder in vial. • Observe for signs of infection and bleeding, and
diseases including breast carcinoma, malig- Pack: 1 vial.
POM DACTICIN® (Alpha) nant lymphomas, soft tissue sarcoma; gastric, POM RUBILON® 50 (L’Pacemaker)
Management of extravasation: Apply ice
Injection, Dactinomycin 0.5 mg; yellow to light red, hepatic, pancreatic, colorectal, lung, ovarian Injection, Epirubicin HCl 50 mg; sterile lyophilized
freeze dried cake in a blue capped amber vial. immediately for 30-60 minutes; then alternate
off/on every 15 minutes for one day. carcinoma and leukemias. powder for injection.
0.5 mg – 1’s. Contra-indications: Myelosuppression in- Pack: single dose vial.
Dose: Consult specialist literature.
duced by previous treatments with other Preparation of the Solution: Epirubicin should
DAUNORUBICIN POM Doxorubicin (WMF 8.2) be dissolved in sterile water for injection or normal
antitumor agents or by radiotherapy; Previous
Indications: Acute leukaemias. Powder for injection, Doxorubicin HCl 10-mg vial, treatment with maximal cumulative doses saline as indicated in the table below:
Contra-indications: See notes above and con- 50-mg vial.
of other anthracyclines such as doxorubicin Freeze-dried vial Diluent added Final concentration
sult specialist literature; pregnancy (Appendix POM Doxorubicin (EDL 7) or daunorubicin; Current or previous history 50 mg 25 mL 2 mg/mL
2) and breastfeeding (Appendix 3). Injections, Doxorubicin (as HCl) 10 mg, 50 mg; of cardiac impairment; Hypersensitivity to
Precautions: See notes above and consult powder in vials.
After adding the diluent, shake the vial until
hydroxybenzoates; Pregnancy, breastfeeding. the drug has completely dissolved. The recon-
specialist literature; renal and hepatic impair- POM ADRICIN® (Alpha) Precautions: Monitor cardiac and haemato-
ment (Appendices 4 and 5); interactions: stituted solution is stable for 24 hours at room
Injection, Doxorubicin 50 mg; powder for injection logical functions regularly. Total cumulative temperature, and for 48 hours in a refrigerator
Appendix 1. in vials. dose should not exceed 0.9–1 g/m2 to avoid
Adverse effects: See notes above and consult (2-8°C). However, it is recommended that in line
POM CELONDOXILYD 10® (L’Pacemaker) cardiotoxicity. Extravasation during IV injection with good pharmaceutical practice, the solution
specialist literature. may produce local pain, severe tissue lesions
Injection, Doxorubicin HCI 10 mg, mannitol 60 mg, should not normally be stored for longer than
Note: Irritant to tissues. (vesication, severe cellulitis) and necrosis.
lactose(anhydrous) 50 mg, methylparaben 2 mg per 24 hours at 2° to 8°C. It should be protected
Dose: Consult specialist literature sterile lyophilized vial. Avoid IM & SC routes. May induce hyperu- from light.
POM Daunorubicin (WMF 8.2) Pack: Single dose vial. ricemia as a result of rapid lysis of neoplastic
Powder for injection, Daunorubicin (as HCl) 50-mg cells (tumour-lysis syndrome); hydration, urine
580 | 12.1.3 Antimetabolites and related therapy 12.1.3 Antimetabolites and related therapy | 581
12.1.3 Antimetabolites and Nursing action: may be given orally mixed in water, grape juice, or dFdCDP reduces the concentration of deox-
related therapy • Give anti-emetic before giving drug to reduce carbonated beverage. ynucleosides in general and, in particular,
nausea. • Do not refrigerate and avoid using cloudy solu- dCTP. Second, dFdCTP competes with dCTP for
Cytarabine is used in the treatment of acute • Reconstituted solution is stable for 48 hours; dis- tions; if crystals form, redissolve by warming.
leukaemia; children may tolerate high doses incorporation into DNA (self-potentiation). The
card cloudy reconstituted solution. Solution is more stable in plastic I.V. bags than in
better than adults. Its effects are highly de- reduced intracellular concentration of dCTP
• Avoid IM injections in patients with thrombocyto- glass bottles.
pendent upon the schedule of administration. penia to prevent bleeding. • Avoid IM injection in patients with thrombocyto- potentiates the incorporation of dFdCTP into
It causes myelosuppression, mucositis, and in • Observe for signs of infection and bleeding and penia to prevent bleeding. DNA resulting in a complete inhibition in fur-
high doses, central neurotoxicity. report to physician. • Anti-emetic may be given before giving drug to ther DNA synthesis and cell death or apoptosis.
• Educate patient on good oral hygiene which prevent nausea. Peak plasma concn is obtained within 5 mins
Fluorouracil is primarily used in the adjuvant prevent stomatitis. • Educate patient on good and frequent oral of the end of the infusion. Half-life ranged from
treatment of colorectal and breast cancer. It • Nausea and vomiting are more frequent in large hygiene. 42-94 mins depending on age & gender. Protein
is also employed in the palliative treatment doses; anti-emetic may be given before giving • Instruct patient to avoid aspirin products or binding is negligible. Gemcitabine is rapidly
of other malignancies. It causes myelosup- drug. NSAIDs.
metabolised by cytidine deaminase in the liver,
pression and the palmar-plantar syndrome • Monitor serum uric acid; allpurinol may be given • Inform patient that alopecia may occur; recom-
mend use of wig.
kidney, blood and other tissues. The intracel-
(erythema and painful desquamation of the with increased fluid intake to prevent urate ne-
phropathy. • Stomatitis and diarrhoea are signs of toxicity; lular metabolites e.g. dFdCDP and dFdCTP are
hands and feet). When its action is modified active and have not been detected in plasma or
Dose: Consult specialist literature. discontinue therapy.
by other drugs (such as calcium folinate), its • Warn patient that alopecia, which is reversible, urine. The primary metabolite (dFdU) is not ac-
toxicity profile can change; mucositis and POM Cytarabine (WMF 8.2) may occur. tive and is found in plasma and urine. Less than
diarrhoea may be significant problems. Central Powder for injection, Cytarabine 100-mg in vial. Dose: Consult specialist literature. 10% is excreted as unchanged drug in the urine.
neurotoxicity can also occur. POM Cytarabine (EDL 7) During the week following administration, 92 to
POM Fluorouracil (WMF 8.2)
Mercaptopurine is frequently used in the Injection, Cytarabine 100 mg; powder in vial. Injection, Fluorouracil 50 mg/mL; in 5-mL ampoule. 98% of the dose of gemcitabine administered is
EMDEX
therapy of childhood leukaemia. It is admin- POM CYTABINE® (Alpha) recovered, 99% in the urine, mainly in the form
POM Fluorouracil (EDL 7) of dFdU and 1% of the dose is excreted in faeces.
istered orally and toxic effects include myelo- Injection, Cytarabine 100 mg per 5 mL; clear colour- Injection, Fluorouracil (as sodium salt) 50 mg per
suppression, nausea, hepatotoxicity and rarely less soln in a colourless 5-mL amp. Mild to moderate renal insufficiency (GFR from
mL; in 5 mL amp.
pancreatitis. 100 mg/5 mL x 10’s 30 mL/min to 80 mL/min) has no consistent,
POM 5 FLUCEL® (L’Pacemaker) significant effect on gemcitabine pharma-
Methotrexate is used to treat a variety of Injection, Fluorouracil 250 mg per 5 mL
FLUOROURACIL cokinetics.
malignancies and it plays a major role as an Pack: 5 amp
adjuvant for the treatment of breast cancer. Synonym: 5-Fluorouracil; 5FU. Indications: Alone or in combination with
Injection, Fluorouracil 500 mg per 10 mL
Like fluorouracil, methotrexate is myelotoxic, Therapeutic category: Cytostatic antineo- Pack: 5 amp.
other agents in the treatment of various can-
but nausea and vomiting are minimal. It also plastic. cers e.g. non-small cell lung cancer (NSCLC),
Indications: Carcinomas of the colorectum, POM Fluoro-Uracil (Swipha) pancreatic cancer, breast cancer, ovarian
causes mucositis. Renal impairment reduces Injection, Fluorouracil 250 mg per 5 mL; colourless
methotrexate excretion and can exacerbate breast, stomach, pancreas, cervix, prostate, cancer, bladder cancer.
liquid in transparent glass amp.
toxicity. ovary and endometrium; liver tumours; head Contra-indications: Hypersensitivity to the
and neck tumours; actinic keratosis (section POM 5 F.U-ABC® (Dizpharm) drug; preegnancy, lactation.
Calcium folinate is used to counteract the Injection, Fluorouacil 50 mg per mL; in 5 mL amp Precautions: Prolonged infusion time and
15.6).
folate-antagonist action of methotrexate Pack: 10. increased dosing frequency may increase
and thus speed recovery from methotrex- toxicity. Bone marrow suppression (monitor
sult specialist literature; pregnancy (Appendix POM UTORAL® (Alpha)
ate-induced mucositis or myelosuppression. platelet, leucocyte and granulocyte counts
2) and breastfeeding (Appendix 3) Injection, Fluorouracil 500 mg; in 10 mL amber
Calcium folinate also enhances the effects of coloured glass vial. prior to each dose). Discontinue at the first
Precautions: See notes above and consult spe-
fluorouracil when the two are used together signs of microangiopathic haemolytic anaemia
cialist literature; hepatic impairment (Appendix
for metastatic colorectal cancer. GEMCITABINE (may lead to irreversible renal failure). Hepatic
Adverse effects: See notes above and consult Therapeutic category: Antineoplastic agent, insufficiency. Radiotherapy (concurrent &
CYTARABINE non-concurrent) may increase risk of radiation
specialist literature. antimetabolite.
Indications: Acute lymphoblastic leukae- Advice to patients: Avoid unnecessary expo- Pharmacology: Gemcitabine (dFdC), which is injury. Avoid yellow fever vaccine and other live
mia; chronic myeloid leukaemia; meningeal sure to sunlight; any signs of infection, easy a pyrimidine antimetabolite, exhibits cell phase attenuated vaccines. History of cardiovascular
leukaemia; erythroleukaemia; non-Hodgkin bruising or bleeding, shortness of breath, or specificity, primarily killing cells undergoing events. Children (<18 years).
lymphomas. painful or burning urination should be brought DNA synthesis (S-phase) and also blocking the Interactions: Radiotherapy; live attenuated
Contra-indications: See notes above and con- to the attention of the physician. Nausea, progression of cells through the G1/S phase vaccines.
sult specialist literature; pregnancy (Appendix vomiting, or hair loss sometimes occur. The boundary. It is metabolised intracellularly by Adverse effects: Bone marrow suppression
2) and breastfeeding (Appendix 3) drug may cause permanent sterility and may nucleoside kinase to the active diphosphate especially leucopenia; N & V, diarrhea, stomati-
Precautions: See notes above and consult spe- cause birth defects. The drug may be excreted (dFdCDP) and triphosphate (dFdCTP) nucle- tis & mouth ulceration, constipation; anorexia;
cialist literature; hepatic impairment (Appendix in breast milk, therefore, an alternative form of osides. The cytotoxic effect of gemcitabine headache, insomnia, somnolence; dyspnea,
5); interactions: Appendix 1. feeding your baby should be used. is due to inhibition of DNA synthesis by two cough, rhinitis; Elevation of liver transaminases
Adverse effects: See notes above and consult Nursing action: mechanisms of action by dFdCDP and dF- (AST and ALT ) and alkaline phosphatase;
specialist literature. • Cool to body temperature before using; after vial dCTP. First, dFdCDP inhibits ribonucleotide allergic skin rash frequently associated with
Advice to patients: Notify physician of signs has been entered, any unused portion should be reductase, which catalyses the production pruritus; alopecia, itching, sweating; back pain,
of infection viz fever, sore throat, bleeding, discarded within 1 hour. of deoxynucleoside triphosphates (dCTP) for myalgia; haematuria, mild proteinuria; flu-like
or bruising. • IV administration is unpredictable; IV formulation DNA synthesis. Inhibition of this enzyme by symptoms; edema, fever, asthenia, chills. Rarely
582 | 12.1.3 Antimetabolites and related therapy 12.1.4 Vinca alkaloids and etoposide | 583
MI, hypotension, interstitial pneumonitis, bron- 3.Inspect visually for particulate with increased fluid intake to prevent hyperuri- Injection, Methotrexate (as sodium salt) 50 mg;
chospasm, injection site reaction. matter and discolouration prior to caemia. powder in vial.
Dose: By IV Infusion over 30 mins, Bladder administration. If particulate matter is • Instruct patient to avoid aspirin products or
POM ABITREXATE® (Dizpharm)
cancer, Combination with Cisplatin, observed, do not administer. NSAIDs.
Injection, Methotrexate 50 mg per 2 mL; in 2 mL vial.
• Observe for signs of bleeding and infection and
1,000 mg/m2 on days 1, 8 and 15 of Any unused product or waste mate-
report to physician. POM UNITREXATE® (Alpha)
each 28-day cycle. May repeat this rial should be disposed of in accord- • Watch for signs of hepatic dysfunction; discontinue Tablet, Methotrexate 2.5 mg.
4-week cycle. Adjust dose based on ance with local requirements. if liver tenderness occurs. 2.5 mg – 100’s
toxicity. (Additional information sourced from Gemzar monograph: Dose: Consult specialist literature. Injection, Methotrexate (as sodium salt) 25 mg per
Pancreatic cancer, 1,000 mg/m2 once http://www.medicines.org.uk/) mL; in 2 mL vials.
POM Mercaptopurine (WMF 8.2)
weekly for up to 7 weeks followed
POM CELZAR® (L’Pacemaker) Tablet, Mercaptopurine 50 mg.
by a week of rest. May continue once CALCIUM FOLINATE
weekly injections for 3 consecutive Injections, Gemcitabine HCI 200 mg, 1000 mg per POM Mercaptopurine (EDL 7)
sterile lyophilized vial. Synonyms: Folinic acid; Leucovorin.
weeks out of every 4 weeks. Adjust Tablet, Mecaptopurine 50 mg.
200 mg – lyophilized powder in a single use vial. Indications: High-dose methotrexate ther-
dose based on toxicity. 1000 mg – lyophilized powder in a single use vial. apy (‘folate rescue’); inadvertent overdose of
Non-small cell lung cancer, Monother- METHOTREXATE
methotrexate; with fluorouracil in the palliative
apy, 1,000 mg/m2 once weekly for POM GEMBIN® (Reals) Synonyms: MTX; Amethopterin. treatment of advanced colorectal cancer.
3 weeks, followed by a 1-week rest Injection, Gemcitabine HCI 200 mg. Therapeutic category: Antineoplastic agent,
Pack: 200 mg (in vial). Precautions: Not for pernicious anaemia or
period. This 4-week cycle is then re- Antimetabolite; Immunosuppressant. other megaloblastic anaemias due to vitamin
peated. Adjust dose based on toxicity. POM GEMTAZ® (Synergy) Indications: Carcinoma of the breast, head and B12 deficiency; pregnancy (Appendix 2); breast-
Combination with Cisplatin, 1,250 IV Infusion, Gemcitabine (as HCl) 200 mg, 1 g; ly- neck, and lung; trophoblastic tumours; acute feeding; interactions: Appendix 1.
mg/m2 on days 1 and 8 of the 21-day ophilized powder for solution for infusion. lymphoblastic leukaemia, meningeal leukae- Adverse effects: Allergic reactions; pyrexia
EMDEX
200 mg – 1’s (in vial) mia; non-Hodgkin lymphomas; advanced
cycle. Adjust dose based on toxicity. after parenteral administration.
1 g – 1’s (in vial)
Breast cancer, Combination with Pa- cases of mycosis fungoides; non-metastatic Dose: Antidote to methotrexate (usually
clitaxel, 1,250 mg/m2 on days 1 and osteosarcoma; severe rheumatoid arthritis started 24 hours after methotrexate),
MERCAPTOPURINE
8 of each 21-day cycle. Adjust dose (section 2.1.2). by IM or IV injection or by IV infusion,
based on toxicity. Mercaptopurine is a complementary cytotoxic drug. Contra-indications: See notes above and con- ADULT and CHILD up to 120 mg in
Ovarian cancer, Combination with sult specialist literature; pregnancy (Appendix divided doses over 12–24 hours, then
Synonym: 6-Mercaptopurine; 6-MP.
Carboplatin, 1,000 mg/m2 on days 2) and breastfeeding (Appendix 3). 12–15 mg by IM injection or 15 mg by
Therapeutic category: Antineoplastic Agent,
1 and 8 of each 21-day cycle. Adjust Precautions: See notes above and consult mouth every 6 hours for 48–72 hours.
Antimetabolite (Purine).
dose based on toxicity. specialist literature; renal and hepatic impair- Methotrexate overdosage (started as
Indications: Acute leukaemias; inflammatory
Administration: All infusions are given over ment (Appendices 4 and 5); interactions: soon as possible, preferably within 1
bowel disease (section 4.8).
30-minute period. If extravasation occurs, infusion Appendix 1.
Contra-indications: See notes above and con- hour of methotrexate), by IV injection
must be stopped immediately and started again in Adverse effects: See notes above and consult
another blood vessel. The only approved diluent for sult specialist literature; pregnancy (Appendix or infusion, ADULT and CHILD, dose
specialist literature. equal to or higher than that of
reconstitution of gemcitabine sterile powder is so- 2) and breastfeeding (Appendix 3).
Nursing action: methotrexate, at rate not exceeding
dium chloride 9 mg/mL (0.9%) solution for injection Precautions: See notes above and consult spe- • Give after evening meal before bedtime; encour-
(without preservative). Due to solubility considera- cialist literature; renal impairment (Appendix 160 mg/minute.With fluorouracil in
age patient to drink 10-12 glasses of fluid daily.
tions, the maximum concentration for gemcitabine 4); monitor liver function – hepatic impairment • Avoid IM injection in patients with thrombocy-
colorectal cancer, consult specialist
upon reconstitution is 40 mg/mL. Reconstitution at (Appendix 5); interactions: Appendix 1. literature.
topenia.
concentrations greater than 40 mg/mL may result Note: Intrathecal injection of calcium folinate is
Adverse effects: See notes above and consult • Anti-emetic may be given before giving drug to
in incomplete dissolution and should be avoided. contraindicated.
specialist literature. prevent nausea.
1.Use aseptic technique during the • Give iron, vitamin supplements as ordered.
Advice to patients: Should not be taken POM Calcium folinate (WMF 8.2)
reconstitution and any further dilu- • Advise patient to avoid prolonged exposure to Tablets, Folinic acid (as calcium folinate) 15 mg
with meals; notify physician of any signs of
tion of gemcitabine for IV infusion. sunlight; to avoid conception during and imme- Injection, Folinic acid (as calcium folinate) 3 mg/mL;
infection, easy bruising or bleeding, shortness
2.To reconstitute, add 5 mL of sterile diately after therapy due to possible abortion or in 10-mL ampoule.
of breath or painful or burning urination; nau- congenital anomalies.
NaCl 0.9 % solution for injection,
sea, vomiting, or hair loss sometimes occurs. • May discontinue drug if GI or pulmonary adverse POM NYRIN® (Alpha)
without preservative, to the 200 mg
The drug may cause permanent sterility and reactions occur. Tablet, Leucovorin calcium 19 mg equiv. to Leucov-
vial or 25 mL to the 1,000 mg vial. orin 15 mg; pale yellow tab. marked ‘FN’ ‘UT’
may cause birth defects. The drug may be ex- • Observe for bleeding (especially GI) and infection.
The total volume after reconstitution 15 mg – 3 x 10’s
creted in breast milk, therefore, an alternative • Monitor serum uric acid; allopurinol may be given
is 5.26 mL (200 mg vial) or 26.3 mL with increased fluid intake to prevent hyperuri- Injection, Leucovorin calcium 55 mg equiv. to Leu-
form of feeding your baby should be used.
(1,000 mg vial) respectively. This caemia. covorin 50 mg per 5 mL; clear, pale yellow soln in
Contraceptive measures are recommended
yields a gemcitabine concentration of Dose: Consult specialist literature. 5-mL amber amp.
during therapy. 50 mg/5 mL x 1’s
38 mg/mL, which includes account-
Nursing action: POM Methotrexate (WMF 8.2)
ing for the displacement volume of • Give after evening meal before bedtime; encour- Tablet, Methotrexate (as sodium salt) 2.5 mg 12.1.4 Vinca alkaloids and etoposide
the lyophilised powder. Shake to dis- age patient to drink 10-12 glasses of fluid daily. Powder for injection, Methotrexate (as sodium salt)
solve. Further dilution with the same • Give iron, vitamin supplements as ordered. 50 mg in vial. The vinca alkaloids, vinblastine and vincris-
diluent can be done. Reconstituted • Avoid IM injection in patients with thrombocyto- tine, are primarily used in the treatment of
solution is a clear, colourless to light penia to prevent bleeding. POM Methotrexate (EDL 7)
acute leukaemias. Vinblastine is also used for
• Monitor serum uric acid; allopurinol may be given Tablet, Methotrexate (as sodium salt) 2.5 mg
straw-coloured solution.
584 | 12.1.4 Vinca alkaloids and etoposide 12.1.5 Other antineoplastic drugs | 585
Hodgkin disease and some solid tumours. specialist literature. Adverse effects: see notes above and consult Cisplatin is a platinum compound used alone
Vincristine is also used in the management Note: Irritant to tissues. specialist literature. or in combination with other cytotoxic drugs
of non-Hodgkin lymphomas. Both can cause Advice to patients: Hair may be lost during Note: Irritant to tissues. for the treatment of testicular, lung, cervical,
neurotoxicity, but this is more of a problem with treatment but will regrow to its pretreatment Advice to patients: Maintain adequate fluid bladder, head and neck, and ovarian cancer.
vincristine. Myelosuppression is more common extent even with continued treatment; report intake; rinse mouth with water 3-4 times Cisplatin is myelosuppressive and also pro-
with vinblastine. Vinblastine and vincristine are any bleeding; examine mouth daily and report daily, brush teeth with soft brush and floss duces slight alopecia; it also causes severe
for intravenous injection only. Inadvertent soreness to a physician; avoid constipation, use with waxed floss; nausea, vomiting or hair loss dose-related nausea and vomiting, and is
intrathecal administration causes severe neuro- softener for prophylaxis; notify physician of any sometimes occur; report any nerve effects to nephrotoxic and neurotoxic. Nephrotoxicity
toxicity which is usually fatal. signs of infection, easy bruising or bleeding, physician; stool softener should be used for can be reduced by maintaining high urine
shortness of breath, or painful or burning constipation prophylaxis; report to physician output during cisplatin administration and
Etoposide is an important component of the
urination; nausea, vomiting may occur. The any persistent or severe fever, sore throat, immediately afterwards, but neurotoxicity is
treatment of testicular carcinoma, and is also
drug may cause permanent sterility and may bleeding or bruising, shortness of breath. often dose-limiting.
used in several regimens for lung cancers and
cause birth defects. The drug may be excreted Nursing action:
lymphomas. It causes myelosuppression and Dacarbazine, thought to act as an alkylating
in breast milk, therefore, an alternative form of • Administer by I.V. only; draw up the solution into a
alopecia and it can cause hypotension during syringe and inject either directly into a vein or into drug, is a component of a regimen for Hodgkin
feeding your baby should be used.
infusion. It does not produce significant nausea the tubing of a running I.V. infusion, whichever is disease. It is also used in the palliative therapy
Nursing action:
and vomiting. more suitable for the patient; injection may be of metastatic malignant melanoma. Its major
• Administered by IV only, avoid extravasation; fatal
if given intrathecally. completed in about 1 minute; avoid infiltration toxic effects are myelosuppression, and severe
ETOPOSIDE • Anti-emetic may be given before giving drug to of subcutaneous tissues and if it occurs, stop the nausea and vomiting.
Indications: Refractory testicular tumours; prevent nausea. injection immediately and any remaining dose
Procarbazine is used in the treatment of ad-
lung cancer. • Encourage deep breathing exercises; raise HOB to should be introduced into another vein.
• Avoid contamination of the eyes which may cause vanced Hodgkin disease. Toxic effects include
Contra-indications: see notes above and facilitate breathing.
EMDEX
severe irritation and even corneal ulceration myelosuppression, N & V, CNS symptoms and
consult specialist literature; severe hepatic im- • Give iron, vitamin supplements as ordered.
(accidental contamination should be washed depression. Procarbazine possesses a weak
pairment (Appendix 5); pregnancy (Appendix • Inform patient that alopecia may occur; recom-
mend use of wig. thoroughly and immediately). monoamine oxidase inhibitory effect but
2) and breastfeeding (Appendix 3) • Calculate and administer the dose carefully to dietary restriction is not necessary.
• Educate patient on good and frequent oral
Precautions: see notes above and consult spe- hygiene. avoid overdosage which may have serious or
cialist literature; renal impairment (Appendix • Maintain adequate hydration; allopurinol may be fatal outcome. ASPARAGINASE
4); interactions: Appendix 1. given to prevent uric acid nephropathy; may cause • See also under Vinblastine.
Synonym: Crisantaspase
Adverse effects: see notes above and consult sloughing upon extravasation. Dose: Consult specialist literature.
Note: Vincristine is for IV administration only.
Indications: Acute lymphoblastic leukaemia.
specialist literature. • Management of extravasation: Mix 150 units
hyaluronidase with 1 mL NS. Inject the hyaluroni- Intrathecal injection causes severe neurotoxicity
NOTE: Irritant to tissues. sult specialist literature; pregnancy (Appendix
dase solution S.C. through 6 clockwise injections which is usually fatal.
Dose: Consult specialist literature. 2) and breastfeeding (Appendix 3)
into the infiltrated area using a 25-gauge needle; POM Vincristine (WMF 8.2)
POM Etoposide (WMF 8.2) change the needle with each new injection. Apply Precautions: See notes above and consult
Powder for injection, Vincristine (as sulfate) 1 mg, 5
Capsule, Etoposide 100 mg. warm compress immediately for 1 hour; repeat mg; in vials. specialist literature; interactions: Appendix 1
Injection, Etoposide 20 mg/mL; in 5-mL vial. 4 times daily for 3-5 days. Application of cold or Adverse effects: See notes above and consult
hydrocortisone is contraindicated. POM Vincristine (EDL 7) specialist literature.
POM ETOPUL® (Alpha)
Dose: Consult specialist literature Injections, Vincristine (as sulfate) 1 mg, 2 mg, 5 mg; Dose: Consult specialist literature.
Injection, Etoposide 100 mg per 5 mL; clear colour-
Note: Vinblastine is for IV administration only. powder in vials.
less to pale yellow soln in 5-mL amber amp. POM Asparaginase (WMF 8.2)
100 mg/5 mL x 10’s. Intrathecal injection causes severe neurotoxicity POM CRISTOVIN® (Dizpharm)
which is usually fatal. Powder for injection, Asparaginase 10 000 IU in vial.
Injection, Vincristine sulfate 1 mg; powder in vial
VINBLASTINE POM Vinblastine (WMF 8.2) with diluent.
CISPLATIN
Powder for injection, Vinblastine (as sulfate) 10 mg; POM Vincristine (Dizpharm)
Vinblastine is a complementary cytotoxic drug.
in vial. Therapeutic category: Antineoplastic Agent,
Injection (Solution), Vincristine sulfate 1 mg per mL;
Synonym: VLB. Alkylating Agent.
in multidose vials of 1 mL, 2 mL and 5 mL
Indications: Disseminated Hodgkin and VINCRISTINE Injection (Lyophilised powder), Vincristine sulfate 1
Indications: Metastatic testicular tumours,
non-Hodgkin lymphomas; advanced testic- mg; in 1 mg vial plus solvent. metastatic ovarian tumours, advanced bladder
Synonym: VCR.
ular carcinoma, breast carcinoma; palliative carcinoma and other solid tumours.
Indications: Acute lymphoblastic leukaemia; POM VINRACINE® (Alpha)
treatment of Kaposi sarcoma; trophoblastic Contra-indications: See notes above and con-
neuroblastoma, Wilm tumour, Hodgkin and Injection, Vincristin sulfate 1 mg per mL; in multi
tumours; Letterer-Siwe disease. sult specialist literature; pregnancy (Appendix
non-Hodgkin lymphomas; rhabdomyosar- dose vials of 1 mL.
Contra-indications: see notes above and con- 2) and breastfeeding (Appendix 3)
coma, Ewing sarcoma; mycosis fungoides.
Precautions: See notes above and consult spe-
sult specialist literature; pregnancy (Appendix Contra-indications: see notes above and con- 12.1.5 Other antineoplastic drugs
2); breastfeeding (Appendix 3). cialist literature; renal impairment (Appendix
sult specialist literature; pregnancy (Appendix The enzyme asparaginase is an important
IMPORTANT: Intrathecal injection is contrain- 4); interactions: Appendix 1.
2); breastfeeding (Appendix 3). component in the management of childhood
dicated. Adverse effects: See notes above and consult
IMPORTANT: Intrathecal injection is contrain- leukaemia, but is not used in any other malig-
Precautions: see notes above and consult spe- specialist literature.
dicated. nancy. Its toxicity profile is broad and the drug
cialist literature; hepatic impairment (Appendix Advice to patients: Drink plenty of fluids to
Precautions: see notes above and consult spe- must be carefully administered because of the
5); interactions: Appendix 1. maintain urine output; be prepared for severe
cialist literature; hepatic impairment (Appendix risk of anaphylaxis.
Adverse effects: see notes above and consult nausea and vomiting following drug admin-
586 | 12.1.5 Other antineoplastic drugs 12.1.5 Other antineoplastic drugs | 587
istration which can be delayed for up to 48 specialist literature. 1. Remove the drug and the diluent vials from POM TAXTAS® (Phillips)
hours; notify physician of numbness or tingling Note: Irritant to tissues. the refrigerator and keep at room temperature Injection, Docetaxel 20 mg per mL
in extremities or hearing loss. Dose: Consult specialist literature. for about 5 minutes. Pack: 20 mg/1 mL; 160 mg/8 mL
Nursing action: POM Dacarbazine (WMF 8.2) 2. Aseptically withdraw the diluent from its vial
• Pretreatment hydration with 1-2 L of fluid is into a syringe and transfer to the vial contain- HYDROXYUREA
Powder for injection, Dacarbazine 100 mg; in vial.
recommended prior to cisplatin administration; ing the drug concentrate. Hydroxycarbamide (aka Hydroxyurea) is an
adequate hydration and urinary output (more POM DTI® (Alpha)
3. Gently rotate for about 15 seconds to ensure antineoplastic drug used in hematological
than 100 mL per hour) should be maintained for 4 Injection, Dacarbazine 200 mg; white to pale yellow
freeze dried cake in amber vial with red cap. full mixture of the concentrate and diluent. malignancies, specifically polycythemia vera
consecutive hours before therapy and for 24 hours
after administration. Pack: 10’s 4. The resultant premix solution (10 mg and essential thrombocytosis. It is also used to
• Nausea and vomiting may be severe and prolonged docetaxel/mL) should be clear; allow to stand reduce the rate of painful attacks in sickle-cell
(up to 24 hours); an anti-emetic e.g metoclopr- DOCETAXEL for a few minutes to allow any foam formed disease and has antiretroviral properties in
amide can be started 24 hours before therapy. Indications: Treatment of patients with locally (due to the polysorbate 80) to dissipate. diseases such as AIDS
• Increase fluid intake to prevent urate deposits and
advanced or metastatic breast cancer after 5. Aseptically withdraw the required amount (Source: http://en.wikipedia.org/wiki/Hydroxyurea)
calculi formation. of premix solution into a syringe and inject
• Instruct patient to avoid aspirin products, NSAIDs,
failure of prior chemotherapy.
Contra-indications: Histor y of severe into a 250 mL infusion bag or bottle of either POM HYDRINE® (Alpha)
alcohol. 0.9% NaCl solution or D5W to produce a final
hypersensitivity reactions to docetaxel or Capsule, Hydroxyurea 500 mg.
• Educate patient on good oral hygiene.
polysorbate 80. Avoid use in patients with concentration of 0.3-0.9 mg/mL. Pack: 100’s.
• Instruct patient to report tinnitus immediately to
prevent permanent hearing loss; and to also report neutrophil counts below 1500 cells/mm3. 6. Thoroughly mix the infusion by manual POM OXYUREA® (Bond)
signs of infection and bleeding. Precautions: To be administered under the su- rotation. Capsules, Hydroxyurea 100 mg, 250 mg, 500 mg.
• Withhold drug when platelets are below 100,000/ pervision of a qualified physician experienced 7. Inspect the resultant infusion solution for 100 mg – 30’s
mm3 or CBC is below 4000/mm3. in the use of antineoplastic agents; all patients particulate matter or discolouration prior to 250 mg – 30’s
EMDEX
• Do not allow drug to come in contact with skin
should be premedicated with oral corticos- administration. 500 mg – 2 x 10’s
or mucous membrane; use soap and water if • Discard the premix solution or infusion solution if it
teroids such as dexamethasone to reduce the
contact occurs. is not clear or appears to have precipitate. IRINOTECAN
• Observe for signs of infection and bleeding, and severity of fluid retention and hypersensitivity • Avoid contact of the drug concentrate with plasti-
reactions; observe closely for hypersensitivity Pharmacology: Irinotecan is an antineplastic
report to physician. cised PVC equipment or devices.
• Monitor for possible anaphylactoid reaction; reactions especially during the first and second agent which acts as a specific inhibitor of DNA
• Store drug in a refrigerator at 2° to 8°C, and protect
monitor renal, haematologic, otic, and neurologic infusions; monitor blood counts frequently from bright light. Freezing does not adversely affect topoisomerase I. It is metabolised by carboxy-
functions frequently. and adjust dose accordingly (discontinue if the product. lesterase in most tissues to SN-38, which was
Dose: Consult specialist literature. neutrophil count falls below 1500 cells/mm3); Dose: By I.V. infusion (over 1 hour), 60-100 found to be more active than irinotecan in
avoid use in pregnancy, lactation; not recom- mg/m2 every 3 weeks. purified topoisomerase I and more cytotoxic
POM Cisplatin (WMF 8.2)
mended for use in children below 16 years ; Note: Premedication Regimen – Dexamethasone than irinocetan against several murine and
Powder for injection, Cisplatin 10 mg, 50 mg; in vials.
hepatic impairment. 16 mg per day (e.g., 8 mg b.i.d) for 3 days, starting on human tumour cell lines. The inhibition of
POM Cisplatin (EDL 7) the day before each course of docetaxel. DNA topoisomerase I by irinocetan or SN-38
Interactions: Metabolism of docetaxel may
Injection, Cisplatin 10 mg, 50 mg; powder in vials. induces single-strand DNA lesions which block
be modified by the concomitant administra- POM BELOTAXEL® (Alpha)
POM ABIPLATIN® (Dizpharm) tion of compounds that induce, inhibit, or are Injection, Docetaxel trihydrate 42.68 mg (as 40 mg the DNA replication fork and are responsible
Injection, Cisplatin 500 mcg per mL; in 20 mL vial. metabolized by cytochrome P450 3A4, such of Docetaxel anhydride)per mL. for the cytotoxicity. This cytoxic activity was
POM CELPLAT 10® (L’Pacemaker) as ciclosporin, terfenadine, ketoconazole, Pack: 1 vial + 1 diluent found time-dependent and was specific to
Injection, Cisplatin 1 mg per mL erythromycin. POM CELON CELTERE® (L’Pacemaker)
the S phase. In addition to hydrolysis by car-
Pack: Sterile single dose vial Adverse effects: Neutropenia, leukopenia, Injection (concentrate), Docetaxel 20 mg/0.5 mL; boxylesterase, irinotecan undergoes CYP3A4
thrombocytopenia, anaemia, toxic deaths, fe- with solvent. enzyme-dependent oxidations. Its clearance
POM CELPLAT 50® (L’Pacemaker)
ver, infections,hypersensitivity reactions, fluid Combipacks: 2 mL (80 mg) x 1’s; 3 mL (120 mg) x 1’s is decreased by about 40% in patients with
Injection, Cisplatin 1 mg per mL
Pack: Sterile single dose vial retention, neurotoxicity, cutaneous reactions, (in vials) + 13% ethanol in WFI as diluent bilirubinemia. Irinotecan is also an inhibitor of
GI effects, alopecia, stomatitis, asthenia, my- POM DOCETERE® (Phillips/Dr. Reddy’s) acetylcholinesterase.
POM UNISTIN® (Alpha) Indication: Treatment of patients with ad-
Injection, Cisplatin 50 mg; in 50 mL amber coloured algia, athralgia, local reaction at infusion site. Concentrate for injection, Docetaxel trihydrate equiv.
Nursing action: to anhydrous Docetaxel 20 mg, Polysorbate 80 USP vanced colorectal cancer in combination with
glass vial.
• Administer by IV infusion over hour under ambient q.s. to 0.5 mL + 1.5 mL solvent containing 13% 5-fluorouracil and folinic acid in patients with-
room temperature and lighting conditions; put Alcohol USP 95% v/v (absolute Alcohol content = out prior chemotherapy for advanced disease,
DACARBAZINE 15.25% v/v).
on gloves. OR as a single agent in patients who have
Indications: Metastatic malignant melanoma; • Avoid contact of the drug concentrate, premix solu- Pack: 0.5 mL x 1’s (in single-dose vial) + 1.5 mL failed an established 5-fluorouracil containing
Hodgkin disease. tion, or infusion solution with the skin or mucous solvent. treatment regimen.
Contra-indications: See notes above and con- membrane; wash off immediately and thoroughly POM MANOTERE® (Manola) Contra-indications: Chronic inflammatory
sult specialist literature; pregnancy (Appendix with water if contact occurs. Injection, Docetaxel (anhydrous) 20 mg, per mL; clear, bowel disease and/or bowel obstruction;
2) and breastfeeding (Appendix 3) • Both the drug concentrate and the diluent vial colourless to pale yellow solution.
contain an overfill, for example Docetaxel 80 mg
history of severe hypersensitivity reaction to
Precautions: See notes above and consult Pack: 20 mg/1 mL; 80 mg/4 mL; 160 mg/8 mL (in irinocetan or to any of the excipients; preg-
specialist literature; renal impairment (Ap- contains 94.4 mg/2.36ml in the vial while the vials).
diluent vial has 7.33 mL of diluent (to give a final nancy and lactation; bilirubin >3 times the
pendix 4); hepatic impairment (Appendix 5); POM TAXOTERE® (Sanofi-Aventis) upper limit of the normal range; severe bone
premix concentration of 10 mg docetaxel per mL).
interactions: Appendix 1. • Preparation of the Premix Solution and Infusion Concentrate for IV infusion, Docetaxel 40 mg per mL; marrow failure; WHO performance status >2;
Adverse effects: See notes above and consult Solution from the Concentrate: in 2 mL vial + 13% ethanol in WFI as diluent. Concomitant use with St. John’s Wort.
588 | 12.1.5 Other antineoplastic drugs 12.1.5 Other antineoplastic drugs | 589
Precautions: Inform patient of the risk of de- regimen on days 1, 2, 15, 16, 29, and 30, with Dose: See under preparations below. 5% Dextrose injection, and then administered
layed diarrhea occurring more than 24 hours the next cycle beginning on day 43. POM ELOXATIN® Concentrate (Sanofi-Aventis)
by IV infusion over 2-6 hours.
after treatment and at any time before the After initiation of chemotherapy patients IV infusion, Oxaliplatin 5 mg per mL; concentrate for POM MANOLATIN® (Manola)
next cycle. Incidence of diarrhea is more pro- should be carefully monitored for toxicity solution for infusion. Injection, Oxaliplatin 5 mg per mL; in 10-mL and
nounced in the elderly, women and those who and doses for irinotecan, LV and 5-FU should 5 mg/1 mL x 10 mL; 20-mL vials.
received a weekly dose of 125 mg/m2 vs. 100 be modified as necessary to accommodate 5 mg/1 mL x 20 mL Pack: 50 mg/10 mL ; 100 mg/20 mL (in vials)
mg/m2. As soon as the first liquid stool occurs, individual patient’s tolerance to the treatment. Dose: Adjuvant treatment: 85 mg/m2 IV in
the patient should start drinking large volumes Preparation of infusion solution: Irinotecan combination with 5-FU & Folinic acid, PACLITAXEL
of beverage containing electrolytes and an injection must be diluted prior to infusion. repeated every 2 weeks for 12 cycles Indications: Metastatic carcinoma of the ovary
appropriate antidiarrhoeal therapy must be Irinotecan should be diluted in 5% dextrose (6 months). or breast, after failure of standard therapy.
initiated immediately. Weekly monitoring of injection (preferred) or 0.9% sodium chloride Treatment of metastatic colorectal Precautions: Monitor blood count frequently.
complete blood cell counts (inform patient of injection to a final concentration range of 0.12 cancer: 85 mg/m2 IV repeated every Continuous cardiac monitoring needed in
the risk of neutropenia and the significance of to 2.8 mg/mL. In most clinical trials, irinotecan 2 weeks. patients with previous significant conduction
fever). Perform liver function tests at baseline was administered in 250-500 mL of 5% dex- POM CELDACH® (L’Pacemaker) abnormalities. Dose-limiting bone marrow
and before each cycle. Give antiemetics before trose injection. Injections, Oxaliplatin 50 mg, 100 mg; sterile ly- depression, WBC count usually lowest 11
each treatment. Avoid co-administration with The solution is physically and chemically ophilized powder for reconstitution in vials. days after use and recovery usually 15-21 days
CYP3A4 inhibitors or inducers. Patients with stable for up to 24 hours at room temperature after the dose (3-hour infusion may cause less
POM PLATINOX® (Alpha)
bowel obstruction. Avoid pregnancy (contra- (approx. 25°C). When refrigerated, dextrose problem). Severe hepatic impairment. Avoid in
Injection, Oxaliplatin 50 mg; white freeze-dried cake
ceptive measures during & for at least 3 months solutions may be stable for 48 hours; NaCl in a red capped colourless vial. those hypersensitive to polyoxyl castor oil, an
after cessation of therapy). May impair ability to solutions should not be refrigerated due to 50 mg – 1’s. ingredient in the formulation. Contains alcohol.
drive or operate machinery. Elderly. incidence of particulates. Freezing may result Dose: Treatment of metastatic cancer of the Adverse effects: Myelosuppression; Peripheral
EMDEX
Adverse effects: GI disorders including de- in precipitation of the drug and should be colon or rectum as first line therapy, by neuropathy. Hypersensitivity reactions, with
layed diarrhea, nausea and vomiting, dehydra- avoided. Other drugs should not be added to IV infusion, 85 mg/m2 on day 1 as part flushing, rash, dyspnoea, hypotension, chest
tion. Neutropenia is a dose-limiting toxic effect; the infusion solution. of a 2-day combination regimen that pain, and angioedema may occur (premedi-
Acute cholinergic syndrome, asthenia, fever, includes fluorouracil & leucovorin. cation with corticosteroids, antihistamines,
mild infusion site reactions, dyspnea, alopecia, POM CAMPTO® (Pfizer)
Infusion, Irinotecan HCl trihydrate 20 mg per mL;
May be repeated at 2-week intervals. and histamine H2-antagonists recommended).
mild allergic reactions, muscular contraction or Adjuvant treatment of stage III colon Other adverse effects include alopecia, arthral-
concentrate for solution for infusion in 2 mL vial.
cramps, paresthesia. Pack: 2 mL x 1’s (in vials). cancer patients who have undergone gia and myalgia, GI disturbances, mucositis,
Dose: Combination therapy: Irinotecan can be complete resection of the primary bradycardia and ECG changes, nail dystrophies,
administered in 2 different regimens POM IRNOCAM® (Phillips/Dr. Reddy’s)
tumor, 2-day regimen given every and elevation of liver enzyme values. Infections
in combination with 5-flurouracil Infusion, Irinotecan HCl trihydrate 20 mg per mL; in
2 mL and 5 mL vials. 2 weeks for 12 cycles (6 months) as are common, as are injection site reactions;
(5-FU) and leucovorin (LV) for the follows: Day 1: 85 mg/m2 IV infusion extravasation may result in tissue damage.
Pack: 2 mL x 1’s; 5 mL x 1’s (in single-dose vials).
treatment of colorectal cancer. in 250-500 mL D5W and leucovorin Rarely hypertension, severe thrombotic events,
In regimen 1, the initial dose of irinotecan is 125 OXALIPLATIN 200 mg/m2 IV infusion in D5W both MI, heart failure, severe cardiac conduction
mg/m2 infused IV over a period of 90 minutes Indications: In combination with 5-fluorouracil given over 120 minutes at the same abnormalities, seizures, neuroencephalopathy,
followed by LV 20 mg/m2 given by rapid IV and leucovorin in the treatment of metastatic time in separate bags using a Y-line, paralytic ileus, optic nerve disturbances, severe
injection and then 5-FU 500 mg/m2 given by cancer of the colon or rectum as first line followed by 5-FU 400 mg/m2 IV bolus skin reactions, hepatic necrosis, and hepatic
rapid IV injection (“bolus”). Treatment is given therapy; adjuvant treatment of stage III colon given over 2-4 minutes, followed by encephalopathy; interstitial pneumonia and
weekly for 4 weeks on days 1, 8, 15, and 22 cancer patients who have undergone complete 5-FU 600 mg/m2 IV infusion in 500 mL other lung disorders.
during a 6-week cycle; the next cycle begins resection of the primary tumor; Progressive or D5W (recommended) as a 22-hour Dose: By IV injection, 175 mg/m2 over 3
on day 43 (four weeks on therapy and 2 weeks metastatic gastric carcinoma where operation continuous infusion. hours every 3 weeks.
off therapy). Day 2: Leucovorin 200 mg/m2 IV Note: Myelosuppression may be less frequent and
is not possible. less severe with 3-hour vs. 24-hour infusion regimen
After initiation of chemotherapy, patients Contra-indications: Hypersensitivity to infusion over 120 minutes, followed
should be carefully monitored for toxicity and oxaliplatin or other platinum compounds; by 5-FU 400 mg/m2 IV bolus given POM CELTAX® (L’Pacemaker)
doses for irinotecan, LV and 5-FU should be myelosuppression; peripheral sensitive neu- over 2-4 minutes, followed by 5-FU Injection, Paclitaxel 6 mg per mL; clear colourless to
modified as necessary to accomodate indi- ropathy; severe renal impairment; pregnancy 600 mg/m2 IV infusion in 500 mL D5W slightly yellow viscous solution in 16.7 mL and 50
vidual’s patient’s tolerance to the treatment. (recommended) as a 22-hour continu- mL multidose vials.
& lactation. Pack: 100 mg/16.7 mL; 300 mg/50 mL (in vials).
Precautions: Heart disease, infection, chicken- ous infusion.
In regimen 2, the initial dose of irinotecan
pox, elderly; extravasation, renal impairment; Therapy in progressive or metastatic POM MANOXEL® (Manola).
is 180 mg/m2 infused IV over a period of 90
neurological, GI and hematological toxicities; gastric carcinoma which is impossible Injection, Paclitaxel 6 mg per mL; clear colourless
minutes followed by LV 200 mg/m2 infused IV
to have operation, 100 mg/m2; may to slightly yellow viscous solution in 16.7-mL and
over 2 hours, then 5-FU 400 mg/m2 by rapid IV abnormal LFT results, portal hypertension.
repeat every 2 weeks in combination 50-mL vials.
injection (“bolus”), and then 5-FU 600 mg/m2 Adverse effects: Nausea, vomiting, and/or Pack: 100 mg/16.7 mL; 300 mg/50 mL (in vials).
diarrhea; myelosuppression, neutropenia; with 5-FU and leucovorin as continu-
infused IV over 22 hours. Treatment is given
tingling, numbness, and sometimes burning of ous infusion if tolerated. POM UNITAXEL® (Alpha)
during a 6-week cycle with administration of
the fingers and toes; anaphylaxis. Less common Preparation: Always administer oxaliplatin Injection, Paclitaxel 100 mg per 16.67ml; colourless
irinotecan on days 1, 15, and 29, and adminis-
before 5-FU. The lyophilized powder must be to pink yellow viscous liquid in a yellow capped
tration of the LV and 5-FU (rapid IV injection are alopecia, fever, rash, fatigue and rarely, amber vial.
kidney damage. diluted in an infusion solution of 250-500 mL of
[“bolus”] and infusional) component of the Pack: 1’s
590 | 12.2 Immunosuppressive drugs 12.2.2 Corticosteroids and other immunosuppressants | 591
PROCARBAZINE individualization of dosage or special equipment are corticoste-roids; nausea; rarely pancreatitis, weeks may necessitate dose reduction.
required for their proper use pneumonitis, hepatic veno-occlusive disease. Corticosteroids have significant immuno-
Indications: Part of MOPP regimen in Hodgkin
and non-Hodgkin lymphomas. Advice to patients: Take with meals; response suppressant activity and can also be used to
Immunosuppressive drugs are used in organ
Contra-indications: see notes above and in rheumatoid arthritis may not occur for up to prevent rejection of organ transplants.
transplant recipients to suppress rejection;
consult specialist literature; severe renal 3 months; do not stop taking without the phy- The corticosteroids prednisolone, dexa-
they are also used as second-line drugs in
impairment (Appendix 4); severe hepatic im- sician’s approval, do not have any vaccinations methasone and hydrocortisone are synthetic
chronic inflammatory conditions. Treatment
pairment (Appendix 5); pregnancy (Appendix before checking with your physician; notify hormones given at pharmacological doses
should only be initiated by a specialist. Careful
2) and breastfeeding (Appendix 3). your physician if you have a persistent sore particularly for haematological malignancies.
monitoring of blood counts is required in pa-
Precautions: see notes above and consult throat, unusual bleeding or bruising, or fatigue. Although there is no evidence for therapeutic
tients receiving immunosuppressive drugs and
specialist literature; interactions: Appendix 1 Nursing action: Give with meals to reduce superiority, prednisolone is used more com-
the dose should be adjusted to prevent bone-
Adverse effects: See notes above and consult GI upset. monly than dexamethasone or hydrocortisone
marrow toxicity. Immunosuppressed patients • Give IV only if oral route is not possible; IM inj may
specialist literature. (section 10.3); prednisolone is an important
are particularly prone to atypical infections. cause bleeding and should be avoided.
Advice to patients: Avoid food with high component of curative regimens for lympho-
• Advise patient to use soft toothbrush to prevent mas and childhood leukaemias and elsewhere
tyramine content; do not take any new pre- 12.2.1 Cytotoxic immunosuppressants bleeding.
scription or OTC drug without consulting it has a palliative role. However, chronic use
• Monitor blood tests; discontinue drug if leukocytes
your physician or pharmacist; avoid alcohol Azathioprine is widely used in transplant leads to the development of a cushingoid
<3000/mm3 or platelets <100,000/mm3.
and alcohol containing products including recipients. It is useful when corticosteroid • Observe for signs of infection and report to syndrome.
topicals; notify physician of persistent fever, therapy alone has proven inadequate or for physician.
sore throat, bleeding or bruising; may impair other conditions when a reduction in the dose Dose: Transplant rejection, by mouth or by IV CICLOSPORIN
judgement and coordination; avoid prolonged of concurrently administered corticosteroids is injection (over at least 1 minute and Synonym: Cyclosporin
exposure to sunlight. required. It is metabolized to mercaptopurine followed by 50 mL sodium chloride IV Indications: Rejection in kidney, liver, heart
EMDEX
Nursing action: and, as with mercaptopurine, doses need infusion) or by IV infusion, ADULT up or bone-marrow transplantation; graftver-
• Administer in divided doses and at bedtime to min- to be reduced when given with allopurinol. to 5 mg/kg on day of surgery, then re- sus-host disease; nephrotic syndrome.
imize nausea and vomiting; give nonphenothiazine Toxic effects include myelosuppression and duced to 1–4 mg/kg daily according Precautions: Monitor kidney function (dose
antiemetic before and after treatment as ordered hepatic toxicity. to response for maintenance. dependent increase in serum creatinine and
to prevent vomiting. Note: Intravenous injection is alkaline and very urea during first few weeks may necessitate
• Warn patient not to drink alcoholic beverages while AZATHIOPRINE irritant; the IV route should therefore only be used dose reduction, exclude rejection if kidney
taking this drug. if oral administration is not possible.
Therapeutic category: Immunosuppressant transplant); monitor liver function (adjust
• Instruct patient to stop medication and report
to doctor immediately if disulfiram-like reaction antimetabolite POM Azathioprine (WMF 8.1) dosage according to bilirubin and liver en-
occurs namely chest pains, rapid or irregular heart- Indications: To prevent rejection in transplant Tablet, Azathioprine 50 mg. zymes, also Appendix 5); monitor blood
beat, severe headache and stiff neck. recipients; rheumatoid arthritis (section 2.1.2); Powder for injection, Azathioprine (as sodium salt) pressure (discontinue if hypertension cannot
• Avoid co-administration with other MAOIs, TCAs, inflammatory bowel disease (section 4.7). 100 mg; in vial. be controlled by antihypertensives); monitor
or foods with high tyramine content; procarbazine Contra-indications: Hypersensitivity to aza- POM Azathioprine (EDL 7) serum potassium, particularly if marked renal
inhibits MAO and can cause disulfiram-like reaction thioprine and mercaptopurine; breast-feeding Tablet, Azathioprine 50 mg impairment (risk of hyperkalaemia); monitor
if given with these drugs. (Appendix 3). Injection, Azathioprine (as sodium salt) 50 mg; serum magnesium; hyperuricaemia; measure
• Avoid all IM injections in patients with thrombo-
Precautions: Monitor for toxicity throughout powder in vial. blood lipids before and during treatment;
cytopenia
treatment; full blood counts necessary every POM Azathioprine (Alpha) avoid in porphyria; pregnancy (Appendix 2);
• Warn patient to avoid hazardous activities that
require alertness until the CNS effects of drug week (or more frequently with higher doses Tablet, Azathioprine 50 mg. breastfeeding (Appendix 3); interactions:
are known. and in renal or hepatic impairment) for first 50 mg – 56’s. Appendix 1.
• Inform patient that alopecia may occur; recom- 4 weeks of treatment, and at least every 3 ADDITIONAL CAUTIONS IN NEPHROTIC SYN-
POM IMURAN® (GSK)
mend use of wig. months thereafter; reduce dose in elderly; DROME: Reduce dose by 25–50% if serum
Tablets, Azathioprine 25 mg, orange f-c scored tab
• Observe for signs of infection and bleeding, and pregnancy (Appendix 2); renal impairment
marked ‘L3C’; 50 mg, yellow f-c scored tab marked creatinine more than 30% above baseline at
(Appendix 4); liver disease (Appendix 5); in- ‘WELLCOME K7A’. more than one measurement; perform renal
Dose: Consult specialist literature. teractions: Appendix 1. Injection, Azathioprine (as sodium salt) 50 mg; yellow biopsies at yearly-intervals; contraindicated
POM Procarbazine (WMF 8.2) BONE MARROW SUPPRESSION: Patients should to amber coloured powder in clear glass vial.
in uncontrolled infections and malignancy.
Capsule, Procarbazine (as HCl) 50 mg. be warned to report immediately any signs or Adverse effects: Dose-related and reversible
POM Procarbazine (EDL 7)
symptoms of bone marrow suppression, for 12.2.2 Corticosteroids and other increases in serum creatinine and urea unre-
Capsule, Procarbazine (as HCl) 50 mg. example unexplained bruising or bleeding, immunosuppressants lated to tissue rejection; burning sensation in
infection. Ciclosporin is a potent immunosuppressant hands and feet during initial therapy; electrolyte
12.2 Immunosuppressive drugs Adverse effects: Hypersensitivity reactions which is virtually free of myelotoxic effects, disturbances including hyperkalaemia,
including malaise, dizziness, vomiting, fever, but is markedly nephrotoxic. It is particularly hypomagnesaemia; hepatic dysfunction;
12.2.1 Cytotoxic immunosuppressants muscular pains, arthralgia, rash, hypotension
12.2.2 C orticosteroids and other immunosup- useful for the prevention of graft rejection and hyperuricaemia; hypercholesterolaemia;
or interstitial nephritis call for immediate for the prophylaxis of graft-versus-host disease. hyperglycaemia, hypertension (especially in
pressants
withdrawal; haematological toxicity includes The dose is adjusted according to plasma-ciclo- heart transplant patients); increased incidence
12.2.3 Interferons
leukopenia and thrombocytopenia (reversible sporin concentrations and renal function. of malignancies and lymphoproliferative dis-
NOTE: WHO advises that this class of drugs is for upon withdrawal); liver impairment, cholestatic
use only when adequate resources and specialist care Dose-related increases in serum creatinine and orders; increased susceptibility to infections
jaundice; hair loss; increased susceptibility to blood urea nitrogen (BUN) during the first few due to immunosuppression; GI disturbances;
are available. Specific expertise, diagnostic precision,
infections and colitis in patients also receiving
592 | 12.2.2 Corticosteroids and other immunosuppressants 12.2.2 Corticosteroids and other immunosuppressants | 593
gingival hyperplasia; hirsutism; fatigue; allergic over 2–6 hours, ADULT and CHILD Tablets, Dexamethasone 0.5 mg, 4 mg. and third months of treatment, then monthly
reactions; thrombocytopenia (sometimes with over 3 months 3–5 mg/kg daily for 2 Injection, Dexamethasone (as sodium phosphate) 4 through the first year. Discontinue if absolute
haemolytic uraemic syndrome); also mild weeks, starting on day before surgery, mg per mL; in amp. neutrophil count <1.3 x 103/µl. Avoid the use
anaemia, tremors, convulsions, neuropathy; followed by maintenance by mouth. See section 10.3 for the proprietory preparations of live attenuated vaccines. Active GI disease.
dysmenorrhoea or amenorrhoea; pancreatitis, Nephrotic syndrome, by mouth, ADULT As an IMPDH (inosine monophosphate dehy-
myopathy or muscle weakness; cramp; gout; 5 mg/kg daily in 2 divided doses; HYDROCORTISONE drogenase) inhibitor, avoid in patients with rare
oedema; headache. CHILD 6 mg/kg daily in 2 divided hereditary deficiency of hypoxanthine-guanine
Advice to patients: To mask taste, mix oral doses; in renal impairment initial See under section 10.3 phosphoribosyl-transferase (HGPRT) such as
solution with milk, chocolate drink, cola, or dose should not exceed 2.5 mg/kg Lesch-Nyhan and Kelley-Seegmiller syndrome.
orange juice immediately before taking (and daily; for maintenance treatment POM Hydrocortisone (WMF 8.3) Interactions: Coadministration with aciclovir,
rinse with more to ensure total dose); stir well Powder for injection, Hydrocortisone (as sodium
slowly reduce to lowest effective dose or its prodrugs, e.g. valaciclovir, ganciclovir,
succinate) 100 mg; in vial.
and drink at once; take dose at the same time according to proteinuria and serum may lead to competition for tubular secre-
each day. Do no mix with grapefruit juice. Do creatinine measurements; discon- tion and increases in concentrations of both
MYCOPHENOLATE
not use plastic cup. Keep medicine measure tinue after 3 months if no improve- drugs. Reduced absorption with antacids with
away from other liquids (including water). ment (after 6 months in membranous Therapeutic category: Immunosuppressant magnesium and aluminium hydroxides, and
Nursing action: glomerulonephritis). Pharmacology: Mycophenolate mofetil (MMF) cholestyramine. Reduced plasma levels when
• Give dosage once daily in the morning and encour- Conversion: Any conversion between brands should is a prodrug of Mycophenolic acid (MPA) – in- combined with ciclosporin, rifampicin, quinolo-
age patient to do so at the same time, each day. be undertaken very carefully, and the manufacturer tended to improve the oral bioavailability of nes. Increased plasma levels with probenecid,
• Do not administer from plastic cup; use a glass consulted for further information. MPA; also available as Mycophenolate sodium. other drugs that undergo renal tubular secre-
container instead to minimize adherence to Note: Concentrate for infusion may contain poly- Following oral administration, mycophenolate tion. Avoid use with live vaccines. May reduce
container walls. ethoxylated castor oil, which has been associated mofetil undergoes rapid and extensive absorp-
• Mixing with milk, chocolate drink, cola, or orange with anaphylaxis; observe patient for 30 minutes
antibody response to other vaccines.
EMDEX
tion and complete presystemic metabolism to Adverse effects: Vomiting, abdominal pain,
juice preferably at room temperature, improves after starting infusion and then at frequent intervals. the active metabolite, MPA. MPA is a reversible
palatability; stir well; do not allow to stand before diarrhoea, nausea; Sepsis, gastrointestinal can-
POM Ciclosporin (WMF 8.1) inhibitor of inosine monophosphate dehydro- didiasis, urinary tract infection, herpes simplex,
drinking; rinse with more diluent to ensure that the
Capsule, Ciclosporin 25 mg genase in purine biosynthesis; it selectively
total dose is taken; after use, dry outside of pipette; herpes zoster; Leucopenia, thrombocytopenia,
Concentrate for injection, Ciclosporin 50 mg/mL; in inhibits the de novo pathway which is critical
do not rinse mouth with water or other cleaning anaemia; Less commonly GI perforation or
1-mL ampoule for organ transplantation. for the proliferation of T– and B-lymphocytes.
agents; may cause inflamed gums. haemorrhage, dyspepsia; pneumonia, other
• Advise patient to take drug with meals if nausea POM Ciclosporin (EDL 7) Other cell types can make purines via separate RTIs; skin cancer; electrolyte imbalance; agita-
occurs; anorexia, nausea and vomiting are tran- Oral liquid, Ciclosporin 100 mg per mL scavenger pathways and thus less affected tion, insomnia, confusion; tremor, somnolence,
sient, occuring frequently at the start of therapy. Injection, Ciclosporin 50 mg per mL; in amp. by the cytostatic effects of MPA. Mean bio-
• Stress that drug should not be withdrawn without dizziness, headache; BP changes; dyspnoea,
POM CIPOL-N® (Alpha) availability of mycophenolate mofetil (oral vs. cough; hepatitis, jaundice; rash, acne, alopecia;
doctor’s knowledge.
Capsules, Cyclosporine 25 mg, 100 mg; gray coloured IV), based on MPA AUC, is 94 %. Food had no arthralgia; renal impairment; oedema, pyrexia,
• To prevent thrush, patient should swish and swal-
low nystatin 4 times daily as ordered. soft caps containing yellowish viscous liquid. effect on the extent of absorption (MPA AUC) chills, pain, malaise, asthenia.
Dose: NOTE: Lower doses are required when
25 mg – 5 x 10’s of mycophenolate mofetil but MPA Cmax was Dose: See eBOC for detailed information.
100 mg – 5 x 10’s decreased by 40 % in the presence of food.
ciclosporin is used with other immu- (Additional information sourced from Cellcept monograph:
nosuppressants. POM PANIMUN BIORAL® (Zoomota) Mycophenolate mofetil is not measurable http://www.medicines.org.uk/)
Organ transplantation, by mouth, Capsules, Cyclosporine 25 mg, 50 mg, 100 mg. systemically in plasma following oral adminis-
ADULT and CHILD over 3 months 25 mg – 5 x 6’s tration. MPA is 97 % bound to plasma albumin. POM IMMUCEPT® (Alpha)
10–15 mg/kg 4–12 hours before
50 mg – 5 x 6’s MPA is metabolised principally by glucuronyl Capsule, Mycophenolate mofetil 250 mg; light blue/
100 mg – 5 x 6’s transferase to its inactive form. It is mostly light brown cap. containing white to pale white pdr.
surgery, then 10–15 mg/kg daily for 250 mg – 10 x 10’s (blister)
1–2 weeks, reducing to 2–6 mg/kg POM PROMUNE® (Megalife sciences) excreted in the urine.
daily for maintenance (adjust dose Capsule, (25 mg), Ciclosporin (microemulsion) 25 mg; Indications: In combination with ciclosporin POM MYCEPT® (Zoomota)
according to blood-ciclosporin con- grey coloured oval-shaped softgel cap. and corticosteroids for the prophylaxis of Capsule, Mycophenolate mofetil 250 mg; blue/
25 mg – 10 x 5’s acute transplant rejection in patients receiving brown cap.
centration and kidney function). Capsule, (50 mg), Ciclosporin (microemulsion) 50 allogeneic renal, cardiac or hepatic transplants. 250 mg – 3 x 10’s
Organ transplantation, by IV infusion mg; off white oval-shaped softgel cap. Tablet, Mycophenolate mofetil 500 mg; f-c pastel
over 2–6 hours, ADULT and CHILD Contra-indications: Hypersensitivity to my-
50 mg – 10 x 5’s pink tab
one-third of the corresponding dose cophenolate mofetil or mycophenolic acid;
Capsule, (100 mg), Ciclosporin (microemulsion) 500 mg – 3 x 10’s
by mouth. 100 mg; grey coloured oblong-shaped softgel cap.
Pregnancy, lactation.
Bone marrow transplantation, graft- 100 mg – 10 x 5’s Precautions: Advice to limit exposure to
PREDNISOLONE
versus-host disease, by mouth, ADULT sunlight/UV light to minimise the risk for skin
and CHILD over 3 months 12.5–15 DEXAMETHASONE cancer; recommend wearing protective cloth- Prednisolone is a representative corticosteroid. Various
ing and using a sunscreen with a high SPF. drugs can serve as alternatives. Prednisolone is a comple-
mg/kg daily for 2 weeks, starting on See under section 10.3 mentary drug for the treatment of malignant neoplasms.
day before surgery, followed by 12.5 Instruct to report immediately any evidence
mg/ kg daily for 3–6 months, then of infection, unexpected bruising, bleeding Indications: With antineoplastic drugs for
POM Dexamethasone (WMF 8.3)
gradually tailed off (may take up to 1 or any other manifestation of bone marrow acute lymphoblastic and chronic lymphocytic
Injection, Dexamethasone phosphate (as disodium
year after transplant). salt) 4 mg; in 1-mL ampoule. depression. Monitor for neutropenia; perform leukaemias, Hodgkin disease, and non-Hodg-
Bone marrow transplantation, graft- complete blood counts weekly during the kin lymphomas; inflammatory and allergic
POM Dexamethasone (EDL 7) first month, twice monthly for the second
versus-host disease, by IV infusion reactions (sections 8.3 and 10.3); eye (section
594 | 12.2.2 Corticosteroids and other immunosuppressants 12.2.3 Interferons | 595
13.2). Injections, Prednisolone (as sodium phosphate or levels. Tacrolimus is a CYP3A4 inhibitor may cells which include gene activation, modula-
Contra-indications: Untreated bacterial, viral, sodium succinate) 20 mg, 25 mg per mL; in vials. affect the metabolism of the substrates of this tion of cell growth and division and modulation
and fungal infections; avoid live virus vaccines. See Proprietary Preparations in section 10.3 enzyme e.g. Ciclosporin, phenytoin, statins. of the cells of the immune system.
Precautions: Monitor body weight, blood May increase the nephrotoxic or neurotoxic
pressure, fluid and electrolyte balance, and effects of aminoglycosides, gyrase inhibitors, INTERFERON ALFA–2A
TACROLIMUS
blood glucose concentration throughout treat- vancomycin, sulfamethoxazole+trimethoprim, Indications: Hairy cell leukaemia (HCl),
ment; adrenal suppression during and for some Therapeutic category: Immunosuppressant; NSAIDs, ganciclovir or aciclovir. May increase cutaneous T-cell lymphoma (CTCL), chronic
months after withdrawal—intercurrent infec- Calcineurin inhibitor. hyperkalaemia due to high potassium intake, myelogenous leukaemia (CML), multiple mye-
tion or surgery may require increased dose of Pharmacology: Tacrolimus is a highly po- or potassium-sparing diuretics (e.g., amiloride, loma, thrombocytosis in CML, thrombocytosis
corticosteroid (or temporary reintroduction tent immunosuppressive agent. It inhibits the triamterene, or spironolactone). Avoid con- in myeloproliferative diseases other than CML,
if already withdrawn); quiescent amoebiasis, formation of cytotoxic lymphocytes, which are comitant use of live attenuated vaccines. May low-grade non-Hodgkin’s lymphoma (NHL),
strongyloidiasis, or tuberculosis possibly re- mainly responsible for graft rejection. Tacrolimus displace drugs with high affinity for plasma AIDS-related kaposis’s sarcoma (KS), renal cell
activated; increased severity of viral infections, suppresses T-cell activation and T-helper-cell proteins (e.g., NSAIDs, oral anticoagulants, or carcinoma, malignant melanoma, chronic
particularly chickenpox and measles—pas- dependent B-cell proliferation, as well as the oral antidiabetics). active hepatitis-B, chronic hepatitis-C, condy-
sive immunization with immunoglobulin formation of lymphokines and the expression Adverse effects: Diarrhoea, nausea, abdomi- lomata acuminata.
required; hypertension, recent myocardial of the interleukin-2 receptor. It is absorbed nal pains, dyspepsia, constipation, flatulence, Contra-indications: Hypersensitivity to
infarction, congestive heart failure; eldery; throughout the GI tract. Cmax is approx. 1–3 bloating and distension; tremor, headache, recombinant interferon alfa-2a or any com-
children and adolescents (growth retardation hours following oral admin with a mean oral insomnia, anxiety, mood disorders, seizures, ponent of the preparation; severe cardiac
possibly reversible); renal impairment; hepatic bioavailability of 20–25%. Food esp. high-fat neuropathies, dizziness, other CNS disorders; disease or any history of cardiac illness;
impairment (Appendix 5); diabetes mellitus; meal decreases both the rate and extent of renal & hepatic impairment; vision blurred, severe renal, hepatic or myeloid dysfunction;
osteoporosis; glaucoma, corneal perforation; absorption. Highly bound (>98.8%) to plasma photophobia, eye disorders; tinnitus; dysp- seizure disorders and/or compromised CNS
EMDEX
severe psychosis, epilepsy; psoriasis; peptic proteins, mainly to serum albumin and alpha- noea, haryngitis, cough, nasal congestion; function; chronic hepatitis with advanced,
ulcer; hypothyroidism; history of steroid myo- 1-acid glycoprotein. Has a low clearance rate hyperglycaemia, diabetes mellitus, hyper- decompensated hepatic disease or cirrhosis
pathy; pregnancy (Appendix 2); breastfeeding and T1/2 is long and variable. Metabolism is kalaemia, electrolyte & lipid abnormalities, of the liver; chronic hepatitis in patients who
(Appendix 3); interactions: Appendix 1. mediated primarily by the CYP3A4 only one hyperuricaemia, appetite decreased, anorexia, are being or have recently been treated with
Adverse effects: GI effects including dyspep- of the metabolites has immunosuppressive metabolic acidoses; hypertension, tachycardia, immunosuppressive agents, excluding short-
sia, oesophageal ulceration, development of activity. Excretion is mainly in the faeces. blood disorders; pruritus, rash, alopecias, acne, term “steroid withdrawal”; CML patients who
or aggravation of peptic ulcers, abdominal Indications: Prophylaxis of transplant rejection sweating increased; arthralgia, muscle cramps, have an HLA-identical relative and for whom
distension, acute pancreatitis; increased appe- in liver, kidney or heart allograft recipients. pain in limb, back pain ; increased risk for in- allogeneic bone marrow transplantation is
tite and weight gain; adrenal suppression with Treatment of allograft rejection resistant to fections; primary graft dysfunction; asthenia, planned or possible in the immediate future.
high doses, leading to cushingoid symptoms treatment with other immunosuppressive febrile disorders, oedema, pain and discomfort, Precautions: Administration should be under
(moon face, acne, bruising, abdominal striae, medicinal products. blood alkaline phosphatase increased, weight the supervision of a qualified physician expe-
truncal obesity, muscle wasting); menstrual Contra-indications: Hypersensitivity to tac- increased; allergic and anaphylactoid reactions rienced in the management of the respective
irregularities and amenorrhoea; hypertension; rolimus or other macrolides; lactation. Dose: See eBOC for detailed information. indications. Mild to moderate renal, hepatic
osteoporosis, with resultant vertebral collapse Precautions: Routinely monitor the following or myeloid dysfunction (close monitoring of
(Additional information sourced from Prograf monograph: http://
and long-bone fractures; avascular osteone- during the initial post-transplant period: blood www.medicines.org.uk/) these functions is required); careful periodic
crosis; ophthalmic effects including glaucoma, pressure, ECG, neurological and visual status, neuropsychiatric monitoring of all patients
subcapsular cataracts, exacerbation of viral fasting blood glucose levels, electrolytes (par- POM PANGRAF® (Zoomota) is recommended; suppressive effect on bone
or fungal eye infections; diabetes mellitus; ticularly potassium), liver and renal function Capsules, Tacrolimus 0.5 mg (light yellow), 1 mg
marrow in patients with severe myelosuppres-
tests, haematology parameters, coagulation (white), 5 mg (pink).
thromboembolism; delayed tissue healing; sion; therapeutic immunosuppression may
values, and plasma protein determinations. 0.5 mg – 6 x 10’s
myopathy, muscle weakness of arms and legs; 1 mg – 6 x 10’s be weakened in transplant patients; children
depression, psychosis, epilepsy; raised intracra- Herbal preparations e.g. St. John’s wort (Hyperi- (safety and effectiveness not yet established);
5 mg – 10 x 10’s
nial pressure; hypersensitivity reactions. cum perforatum) may reduce blood concentra- neurotoxicity, haematotoxicity or cardiotoxic
Nursing action: See Prednisolone in Section tions of tacrolimus. Diarrhoea episodes (moni- effects of previously or concurrently adminis-
tor for changes in plasma concn of tacrolimus). 12.2.3 Interferons
10.3. tered centrally-acting drugs may be increased;
Dose: Leukaemias and lymphomas, by mouth, Avoid co-administration of ciclosporin and Interferons are naturally occurring proteins
pregnancy (to be used only if the benefit to the
ADULT initially up to 100 mg daily, tacrolimus. QT interval elongation. Monitor which affect the immune response as well
woman justifies the potential risk to the foetus);
then gradually reduced if possible to for increased risk of opportunistic infections as the cell function. There are alfa, beta and
breast-feeding (not yet established whether it
20–40 mg daily; CHILD up to 1 year, (bacterial, fungal, viral and protozoal). Limit gamma interferons.
is excreted in human milk).
initially up to 25 mg, then 5–10 mg; exposure to sunlight and UV light (wearing pro- Interferon alfa-2a (Roferon-A®) is a highly Interactions: Theophylline (its metabolism is
2–7 years, initially up to 50 mg, then tective clothing and using a sunscreen with a purified sterile protein consisting of 165 ami- inhibited leading to enhanced effect).
10–20 mg; 8–12 years, up to 75 mg, high SPF). May visual disturbances. Pregnancy. noacids. It is produced by DNA recombinant Adverse effects: Flu-like symptoms; reactiva-
then 15–30 mg. Interactions: CYP3A4 inhibitors (e.g. ke- technology. Following binding to specific cell tion of peptic ulcer and non-life-threatening GI
to-conazole, fluconazole, erythromycin, membrane receptor, transcytoplasmic signals bleeding; rarely, hepatitis, pulmonary oedema,
POM Prednisolone (WMF 8.3) ritonavir may increase while the inducers
Tablets, Prednisolone 5 mg, 25 mg. initiate the appearance of up to 15 major new CHF, cardiorespiratory arrest and myocardial
(e.g. rifampicin, phenytoin or St. John’s Wort) protein species in the cytoplasm, the products infarction; severe somnolence, coma, cerebro-
POM Prednisolone (EDL 7) may decrease plasma levels of tacrolimus. of interferon inducible genes. These lead to vascular adverse events, transient impotence
Tablet, Prednisolone 5 mg. Corticosteroids may reduce tacrolimus blood morphological and behavioural changes in
596 | 12.3 Sex hormones and antagonists used in malignant diseases 12.3 Sex hormones and antagonists used in malignant diseases | 597
and ischaemic retinopathy are rare compli- 1-3 m.i.u. 1-3 times daily. Low grade is produced primarily from the conversion effects include: vaginal bleeding, anorexia,
cations; rarely, cardiovascular problems in NHL, concomitantly with chemother- of androstenedione to estrone through the hypercholesterolaemia, vomiting, somnolence;
patients with hepatitis-B; transient leukopaenia apy, 6 m.i.u./sq. m from day 22-26 of aromatase enzyme complex in peripheral increases in gamma-GT and bilirubin, hepatitis-
in about one third to over one half of cancer each 28-day cycle; or as maintenance tissues. Estrone is subsequently converted to erythema multiforme. Rarely, Stevens-Johnson
patients; thrombocytopenia and decrease of after chemotherapy (usually after 4-6 estradiol. Reducing circulating estradiol levels syndrome; allergic reactions including an-
haemoglobin in non-myelosuppressed pa- weeks), 3 m.i.u. thrice weekly for at has been shown to produce a beneficial effect gioedema, urticaria and anaphylaxis. It lowers
tients. Recovery of severe haematological de- least 12 months. in women with breast cancer. Anastrozole does circulating oestrogen levels and may cause
viations to pretreatment levels usually occurs AIDS-related KS, initially, 18-36 m.i.u. not possess any progestogenic, androgenic or a reduction in bone mineral density placing
within 7-10 days after discontinuing treatment. for 12 weeks; maintenance, thrice oestrogenic activity. some patients at a higher risk of fracture.
Nursing action: weekly injections at dose acceptable Absorption of anastrozole is rapid and maxi- Dose: Adults including the elderly: 1 mg to
• Administer at bedtime to minimize daytime to patient, but not exceeding 36 m.i.u. mum plasma concentrations typically occur be taken orally once a day.
drowsiness. for 12 weeks – optimum duration yet within two hours of dosing (under fasted Child: Not recommended for use in
• Use S.C. route in patients with platelets count to be determined. conditions). Anastrozole is eliminated slowly children Renal impairment: No dose
below 50,000/mm3; inspect injection site and skin
Renal cell carcinoma, initially, when with a plasma elimination half-life of 40 to 50 change in mild or moderate renal
for signs of bruising.
• Ensure patient is properly hydrated especially
used with Vinblastine, 18 m.i.u. thrice hours. Food slightly decreases the rate but not impairment
during the early stage of therapy. weekly for 8-12 weeks; maintenance the extent of absorption. Anastrozole is only Hepatic impairment: No dose change
• Paracetamol may be given to minimize flu-like with Vinblastine, 18 m.i.u. (max.) 40% bound to plasma proteins. It is extensively in mild hepatic disease. For early
symptoms experienced by almost all patients. thrice weekly. metabolised by postmenopausal women with disease, the recommended duration
• Instruct patient on proper oral hygiene during Malignant melanoma, initially, 18 less than 10% of the dose excreted in the urine of treatment should be 5 years.
treatment, because the suppressive effect of m.i.u. thrice weekly for 8-12 weeks; unchanged within 72 hours of dosing. The me- POM ARIMIDEX® (Reals)
the drug on bone marrow may cause microbial maintenance, 18 m.i.u. thrice weekly tabolites are excreted primarily via the urine. Tablet, Anastrozole 1 mg; whitefilm-coated tab.
EMDEX
infection, delayed healing, and gingival bleeding. or at max. dose acceptable to pa- Indications: Adjuvant treatment of post- marked with logo on one side and strength on
Interferon may also decrease salivary flow.
tient – optimum duration yet to be menopausal women with hormone receptor the reverse.
• Co-administration with a live vaccine may potenti-
ate replication of vaccine virus, increase adverse re- determined. positive early invasive breast cancer. Adjuvant
actions, and decrease patient’s antibody response; Chronic active Hepatitis-B, 2.5-5 m.i.u./ treatment of early breast cancer in hormone BICALUTAMIDE
advise patient to inform the doctor before having sq. m thrice weekly for 4-6 months. receptor positive postmenopausal women Therapeutic category: Antineoplastic agent,
any immunization. Chronic Hepatitis-C, initially 6 m.i.u. who have received 2 to 3 years of adjuvant Antiandrogen.
• Reassure patient that loss of hair is temporary thrice weekly for 3 months; mainte- tamoxifen. Treatment of advanced breast Pharmacology: Bicalutamide is a non-steroi-
and normal growth of hair will resume when drug nance, patients whose ALT has nor- cancer in postmenopausal women. Efficacy has dal antiandrogen, devoid of other endocrine
is stopped. malised should then receive 3 m.i.u. not been demonstrated in oestrogen receptor activity. It binds to androgen receptors without
• Monitor for CNS adverse reactions such as de- thrice weekly for another 3 months. negative patients unless they had a previous
creased mental status and dizziness; careful pe- activating gene expression, and thus inhibits
Condylomata acuminata, 1-3 m.i.u. positive clinical response to tamoxifen. the androgen stimulus. Regression of prostatic
riodic neuropsychiatric monitoring of all patients
is recommended. thrice weekly for 1-2 months. Contra-indications: Premenopausal women; tumours results from this inhibition. Clinically,
• Store drug in a refrigerator; use reconstituted POM ROFERON–A® (Swipha)
pregnant or lactating women; patients with discontinuation of bicalutamide can result
solution within 30 days. Injections, Interferon alfa-2a (rbe) 4.5, 9 million i.u.; severe renal impairment (creatinine clearance in antiandrogen withdrawal syndrome in a
Dose: By SC or IM injection, HCl, initially, 3 powder for reconstitution in vials. All with syringes, <20 mL/min); patients with moderate or severe subset of patients. Bicalutamide is a racemate
m.i.u. daily for 16-24 weeks; mainte- needles and ampoules containing 1 mL sterile water hepatic disease; hypersensitivity to anastrozole with its antiandrogenic activity being almost
nance, 3 m.i.u. thrice weekly. for injection. or to any of the excipients. exclusively in the (R)-enantiomer. Bicalutamide
CTCL, initially, 18 m.i.u. daily for 12 Pack: 1 x 5. Precautions: Children, moderate or severe is well absorbed following oral administration.
weeks; maintenance, thrice weekly hepatic impairment, severe renal impairment Food does not affect the bioavailability. The
injections at doses acceptable to 12.3 Sex hormones and antagonists (creatinine clearance less than 20 mL/min); pharmacokinetics of the (R)-enantiomer are
patient, but not exceeding 18 m.i.u. used in malignant diseases Osteoporosis (lowers circulating oestrogen unaffected by age, renal impairment or mild
CML, initially, 9 m.i.u. daily for 8-12 Tamoxifen is an estrogen-receptor antagonist. levels and may cause a reduction in bone to moderate hepatic impairment. There is
weeks or for a max. of 18 months; It is the adjuvant hormonal treatment of choice mineral density); LHRH analogues; contains evidence that for subjects with severe hepatic
for patients with complete haema- for all women with estrogen-receptor positive lactose. Unlikely to impair the ability to drive impairment, the (R)-enantiomer is more slowly
tological response, continue with 9 breast cancer and for palliative management and operate machinery but may cause asthenia eliminated from plasma. Bicalutamide is highly
m.i.u. daily or thrice weekly (mini- in patients with advanced disease. When given and somnolence. protein bound (racemate 96%, R-bicalutamide
mum) – optimum duration yet to be at recommended doses, it has few adverse Interactions: Avoid co-administration with 99.6%) and extensively metabolised (via oxi-
determined. effects, although, it can induce uterine endo- oestrogen-containing therapies as they would dation and glucuronidation): Its metabolites
Multiple Myeloma, 3 m.i.u. thrice metrial malignancies. negate its pharmacological action. Concurrent are eliminated via the kidneys and bile in
weekly indefinitely unless rapid tamoxifen therapy may diminish its pharmaco- approximately equal proportions.
progression or severe intolerance ANASTROZOLE logical action. Indications: Treatment of advanced prostate
develops. Therapeutic category: Antineoplastic agent, Adverse effects: Hot flushes, asthenia, joint cancer in combination with LHRH analogue
Thrombocytosis in CML, initially as Enzyme inhibitor. pain/stiffness, vaginal dryness, hair thinning, therapy or surgical castration.
for CML,Thrombocytosis in other Pharmacology: Anastrozole is a potent and rash, nausea, diarrhoea, headache, Car- Contra-indications: Females and children.
myeloproliferative diseases, 6 m.i.u. highly selective non-steroidal aromatase in- pal Tunnel Syndrome; increases in alkaline Hypersensitivity to bicalutamide. Avoid co-ad-
daily for up to 30 days; maintenance, hibitor. In postmenopausal women, estradiol phosphatase, alanine aminotransferase and ministration with terfenadine, astemizole or
aspartate aminotransferase. Uncommon side
598 | 12.3 Sex hormones and antagonists used in malignant diseases 12.3 Sex hormones and antagonists used in malignant diseases | 599
cisapride. therapy. Treatment of advanced breast cancer by flutamide administration. Flutamide is 250 mg – 4 x 21’s
Precautions: Moderate to severe hepatic im- in women with natural or induced postmen- rapidly and completely absorbed, and food POM LUTAMIDE® (PharmacyPlus)
pairment; periodic liver function testing should opausal status whose disease has progressed has no effect on bioavailability. Undergoes Tablet, Flutamide 250 mg; uncoated tab.
be considered due to the possibility of hepatic following anti-oestrogen therapy. hepatic metabolism via CYP1A2 to the active 250 mg – 4 x 21’s (in blisters)
changes within the first 6 months of therapy. Contra-indications: Hypersensitivity; pre-meno- metabolite, 2-hydroxyflutamide. Excreted
Avoid use in females and must not be given to pausal women; Pregnancy and lactation. mainly in urine and half-life of hydroxyfluta- TAMOXIFEN
pregnant women or nursing mothers. Unlikely Precautions: Determine postmenopausal mide is 6 hours.
Tamoxifen is a complementary drug for the treatment
to impair the ability to drive or operate ma- status of the patient prior to treatment where Indications: Treatment of advanced prostatic
of breast cancer.
chinery but occasional somnolence may occur. appropriate. Hepatic or renal impairment. cancer (D2) as initial treatment in combination
Adverse effects: Breast tenderness, gynaeco- Osteoporosis or at risk patients (assess bone with a luteinizing hormone-releasing hormone Therapeutic category: Estrogen antagonist.
mastia, hot flushes; diarrhoea, nausea; hepatic mineral density prior to treatment & monitor (LHRH) agonist, as adjunctive therapy in pa- Indications: Adjuvant treatment of estro-
changes (elevated levels of transaminases, regularly afterwards). Co-administration with tients already on LHRH agonist, in surgically gen-receptor-positive breast cancer; meta-
cholestasis and jaundice); asthenia, Pruritus; drugs metabolised via CYP3A4 esp. those with castrated patients and in patients who have static breast cancer.
rarely vomiting, dry skin, hepatic failure. narrow therapeutic window. not responded or have become refractory Contra-indications: Pregnancy (exclude be-
Dose: Adult males including the elderly: 50 Interactions: CYP3A4 inducers (such as ri- to or who cannot tolerate other hormonal fore treatment and advise nonhormonal con-
mg once a day. Treatment should be fampicin, phenytoin, carbamazepine, St John’s manipulation. Also indicated in combination traception if appropriate, see also Appendix 2).
started at the same time as treat- Wort) may reduce efficacy of exemestane. with LHRH agonists for the management of Precautions: Monitor for endometrial changes
ment with an LHRH analogue or Oestrogen-containing drugs may antagonis locally confined stage B2-C prostate carcinoma. (increased incidence of hyperplasia, polyps,
surgical castration.Child: Avoid use in its action. Contra-indications: Hypersensitivity to fluta- cancer, and uterine sarcoma); cystic ovarian
children. Adverse effects: Most commonly hot flushes, mide or any components of this preparation; swellings in premenopausal women; increased
Renal impairment: No dosage adjust- arthralgia, fatigue, nausea, insomnia, head- severe hepatic dysfunction; pregnancy. risk of thromboembolism when used with anti-
EMDEX
ment. ache; increased sweating; joint & musculoskel- Precautions: Inform patient of the possibility neoplastic drugs; breastfeeding (Appendix 3);
Hepatic impairment: No dosage adjustment is etal pain. Less common: Depression, Dizziness, of hepatic dysfunction and to report immedi- avoid in porphyria; interactions: Appendix 1.
necessary for patients with mild hepatic impairment. Abdominal pain, vomiting, constipation, dys- ately if symptoms of hepatic dysfunction occur Adverse effects: Hot flushes; endometrial
Increased accumulation may occur in patients with pepsia, diarrhoea, Rash, alopecia, Osteoporosis, namely itching of the skin, dark urine(amber or changes (symptoms such as vaginal bleeding
moderate to severe hepatic impairment. and other menstrual irregularities, vaginal
fracture, Pain, peripheral oedema. yellow-green urine is not a cause for concern),
POM CASODEX® (Reals) Dose: By mouth, Adult & Elderly, 25 mg once nausea, vomiting, persistent lack of appetite, discharge, pelvic pain require immediate inves-
Tablet, Bicalutamide 50 mg; white f-c tab. daily, preferably after a meal. yellow eyes or skin, tenderness in the right tigation); increased pain and hypercalcaemia
POM BICALUT® (Alpha) Patients with early breast cancer, upper abdomen or “flu like” symptoms. Monitor with bony metastases; tumour flare; nausea
Tablet, Bicalutamide 50 mg; white f-c tab. marked Continue treatment until completion liver function. Indicated for men only. and vomiting; liver enzyme changes (rarely
‘K.D’ ‘50’. of 5 years of combined sequential ad- Interactions: Flutamide is an antiandrogen cholestasis, hepatitis, hepatic necrosis); hyper-
50 mg – 2 x 14’s. juvant hormonal therapy (tamoxifen and may interact pharmacologically with triglyceridaemia (sometimes with pancreatitis);
followed by exemestane), or earlier if androgens, oestrogens or other forms of hor- thromboembolic events; decreased platelet
EXEMESTANE tumour relapse occurs. monal therapy. count; oedema; alopecia; rash; headache;
Therapeutic category: Antineoplastic agent, Patients with advanced breast cancer, Adverse effects: Most frequently gynaeco- visual disturbances including corneal changes,
Enzyme inhibitor. Continue treatment until tumour mastia, impotence, breast tenderness, some cataracts, retinopathy; rarely interstitial pneu-
Pharmacology: Exemestane is an irreversible, progression is evident. times galactorrhoea. Less frequent, diarrhoea, monitis, hypersensitivity reactions including
steroidal aromatase inhibitor, structurally Child: Not recommended. nausea, vomiting, insomnia, tiredness, tran- angioedema, Stevens-Johnson syndrome,
related to the natural substrate androstenedi- Hepatic or Renal Insufficiency: No sient abnormal liver function and hepatitis. bullous pemphigoid.
one. In postmenopausal women, oestrogens dose adjustment. Decreased libido, upset stomach, anorexia, Advice to patients: Report any vomiting that
are produced primarily from the conversion ulcer-like pain, heartburn, constipation, occurs after taking dose; patient should be ad-
POM AROMASIN® (Pfizer)
of androgens into oestrogens through the Tablet, Exemestane 25 mg; coated tab. oedema, ecchymosis, pruritus, lupus-like syn- ivsed to notify their physician of vaginal bleed-
aromatase enzymes in peripheral tissues. 25 mg – 30’s (in blister). drome, headache, dizziness, weakness, malaise, ing, weakness, mental confusion; increased
Oestrogen deprivation through aromatase blurred vision and reduced sperm counts bone and tumour pain and local disease flare
inhibition is an effective and selective treat- FLUTAMIDE have been reported rarely. Rarely anaemia, may occur with start of therapy.
ment for hormone dependent breast cancer in Therapeutic category: Antiandrogen; Antineo- leukopenia, anorexia, jaundice, hypertension, Nursing action:
postmenopausal women. It does not possess central nervous system adverse events and • Give after evening meal before bedtime; increase
plastic agent fluid intake to prevent dehydration.
any progestogenic or oestrogenic activity. It is Pharmacology: Flutamide, an acetanilide is thrombocytopenia may be observed. Very
• Anti-emetic may be given before giving drug to
rapidly absorbed following oral administration; a non-steroidal, orally active antiandrogen. It rarely, haemolytic anaemia, methaemoglobi-
prevent nausea.
food increases the bioavailability by 40%. exerts its antiandrogenic action by inhibiting naemia, photosensitivity reactions, cholestatic • Give iron, vitamin supplements as ordered.
Terminal elimination half-life is 24h and bind- androgen uptake and/or by inhibiting nuclear jaundice, hepatic encephalopathy and hepatic • Reassure patient that increased bone pain during
ing to plasma proteins is 90%. It undergoes binding of androgen in target tissues or both. necrosis. The hepatic conditions were usually tamoxifen therapy usually indicates a good ther-
hepatic metabolism and the amount excreted When flutamide is given in combination with reversible after stopping treatment. apeutic response; give analgesic to relieve pain.
unchanged in urine is 1% of the dose. surgical or medical castration, suppression of Dose: By mouth, 250 mg 3 times daily at • Inform patient that alopecia may occur but it is
Indications: Adjuvant treatment of postmen- 8-hour intervals. Max. 750 mg/day temporary; recommend use of wig.
both testicular and adrenal androgen activity
opausal women with oestrogen receptor Dose: Breast cancer, by mouth, ADULT 20
is achieved. Elevations of plasma testosterone POM G-FLUTA® (Global Healthcare)
positive invasive early breast cancer, follow- mg daily.
and estradiol levels have been noted followed Tablet, Flutamide 250 mg.
ing 2-3 years of initial adjuvant tamoxifen
600 | 12.3 Sex hormones and antagonists used in malignant diseases 12.4 Drugs used in palliative care | 601
POM Tamoxifen (WMF 8.3) drug or other LHRH analogues; pregnancy or trophin. At the appropriate stage of and non-drug measures. Some types of pain
Tablets, Tamoxifen (as citrate) 10 mg, 20 mg lactation; Children. follicular development, gonadotro- respond well to a combination of a non-opioid
POM Tamoxifen (EDL 7) Precautions: Worsening of signs and symp- phin is stopped and human chorionic and an opioid analgesic. Other types of pain
Tablets, Tamoxifen (as citrate) 10 mg, 20 mg toms especially cancer-related pain during the gonadotrophin (hCG) is administered are relieved by combining a corticosteroid
first few weeks of treatment (usually controlled to induce ovulation. Treatment and an opioid. Neuropathic pains often show
POM APO-TAMOX® (Lahams) monitoring, oocyte retrieval and little response to non-opioids and opioids, but
Tablet, Tamoxifen citrate 20 mg; off-white tab.
by analgesics); ureteral obstruction and spinal
cord compression in men (monitor carefully fertilisation techniques are performed may be eased by tricyclic antidepressants and
marked ‘APO T20’.
20 mg-100. during the first month of therapy); women according to the normal practice of anticonvulsants (see below). Cancer patients
with metabolic bone disease (may cause loss the individual clinic. often have many fears and anxieties, and may
POM NOLVADEX® (Reals) Not recommended for children. become depressed. Very anxious or deeply
of bone mineral density in women); children
Tablet, Tamoxifen (as citrate)10 mg; white round, Note: Administration: Do not remove the sterile
(not recommended). depressed patients may need an appropriate
bionvex tab marked ‘NOLVADEX 10 and ICI’. syringe until immediately before use. After cleaning
Adverse effects: Rarely anaphylaxis; wors- psychotropic drug in addition to an analgesic.
POM NOLVADEX-D® (Reals) with an alcohol swab, a local anaesthetic may be If this fact is not appreciated, the pain may
ening of the signs and symptoms early in
Tablet, Tamoxifen (as citrate) 20 mg; white, octagonal used on an area of skin on the upper abdominal
the treatment manifested by an increase in remain intractable.
biconvex tab marked ‘NOLVADEX–D AND ICI’. wall. Stretch the patient’s skin with one hand, and
bone pain, increased difficulty in urinating, grip the needle into the SC fat.
In the majority of patients, cancer pain can be
POM Tamoxifen (Alpha) hot flashes, injection site irritation, weakness; Do not aspirate: If the hypodermic needle penetrates relieved with analgesics:
Tablet, Tamoxifen citrate 20 mg. sexual dysfunction, impotence, postmeno- a large vessel, blood will be seen instantly in the • by mouth: if possible analgesics should be given
pausal symptoms, gynaecomastia, oedema, syringe chamber. Change the direction of the needle by mouth. Rectal suppositories are useful in pa-
POM Tamoxifen (Dizpharm) tients with dysphagia, uncontrolled vomiting or
Tablets, Tamoxifen (as citrate) 10 mg, 20 mg headache, lethargy, dizziness, insomnia, skin so it parallels the abdominal wall. Push the needle
in until the barrel hub touches the patient’s skin. gastrointestinal obstruction. Continuous subcuta-
10 mg – 30 rash, breast tenderness/enlargement, sweat- neous infusion offers an alternative route.
20 mg – 30. Withdraw the needle 1cm to create a space to
ing, increased bone pain, bone loss, diarrhoea, • by the clock: analgesics are more effective in
EMDEX
discharge the drug; fully depress the plunger to
POM Tamoxifen (Kakaki) nausea, vomiting. discharge. preventing pain than in the relief of established
Tablets, Tamoxifen 10 mg, 20 mg Advice to patients: Females must use reliable Withdraw needle and bandage the site. Confirm pain, therefore doses should be given at fixed time
10 mg – 30’s contraceptive during therapy; symptoms discharge by ensuring tip of the plunger is visible intervals and titrated against the patient’s pain; if
20 mg – 30’s may worsen temporarily during first week of within the tip of the needle. pain occurs between doses, a rescue dose should
therapy. be given, and the next dose increased.
POM ZOLADEX® (Reals) • by the ladder: the first step is to give a non-opioid
GOSERELIN ACETATE Dose: By SC injection (into the upper Implant, Goserelin acetate (equiv. to 3.6 mg Gos- analgesic such as acetylsalicylic acid, paraceta-
Therapeutic category: Antineoplastic agent; abdomen), 3.6 mg every 28 days. No erelin); Sterile, white to cream coloured cylindrical mol or ibuprofen, if necessary with an adjuvant
Luteinizing Hormone-Releasing Hormone dosage adjustment for patients with depot in which goserelin acetate (equiv. to 3.6 mg drug. If this does not relieve the pain, an opioid
(LHRH) Analogue. renal or hepatic impairment, or for of goserelin) is dispersed in a biodegradable matrix for mild to moderate pain such as codeine should
Pharmacology: Goserelin is a synthetic ana- the elderly. of lactide-glycolide co-polymer. It is supplied as a be added. When this combination fails to relieve
logue of naturally occurring LHRH also known Prostate carcinoma: intended for long- single dose SafeSystemTM syringe applicator with a pain, an opioid for moderate to severe pain such
as gonadotropin-releasing hormone (GnRH) term administration. protective sleeve in a sealed pouch which contains as morphine should be substituted.
Endometriosis: recommended a desiccant. • for the individual: there are no standard doses for
incorporated into a biodegradable depot ma-
Pack: Implant, in pre-filled syringe. opioid drugs. The range for oral morphine is from as
terial which allows for continuous slow release duration is 6 months (safety data is
little as 5 mg to more than 100 mg every 4 hours.
over 28 days. Continuous daily administration not available for longer treatment
results in suppression of ovarian and testicular periods). 12.4 Drugs used in palliative care Sustained-release morphine tablets are available
to enable oral dosing every 12 hours.
steroidogenesis due to decreased levels of LH Endometrial thinning: Two depots to NOTE: The Expert Committee on the Selection and • with attention to detail: the first and last doses of
and FSH with subsequent decrease in testos- be administered 4 weeks apart, with Use of Essential Medicines recommends that all the the day should be linked to the patient’s waking
terone (male) and oestrogen (female) levels. surgery timed for between zero and drugs mentioned in Cancer Pain Relief: with a Guide time and bedtime. Ideally the drug regimen should
to Opioid Availability, 2nd edition. Geneva: WHO 1996
This suppression leads to prostate tumour two weeks after the second depot. be written out in full for the patient and his or
be considered essential. These drugs are included in the her family. The patient should be warned about
regression and symptomatic improvement in Uterine fibroid: 3.6 mg depot with relevant sections of the Model List according to their
the majority of patients.Goserelin is inactive supplementary iron may be given for possible adverse effects.
therapeutic use, for example analgesics.
when administered orally. Absorption is rapid up to three months before surgery. Drugs for neuropathic pain
when administered subcutaneously and it can Assisted reproduction: 3.6 mg given Palliative care includes both pain relief and Neuropathic pain often responds to a tricyclic
be detected in the serum in 10 minutes. Time to to downregulate the pituitary gland, the symptomatic relief of conditions includ- antidepressant, such as amitriptyline (section
peak serum concentration is about 12-15 days. as defined by serum estradiol levels ing dyspnoea, restlessness and confusion, 1.4), or to an anticonvulsant such as carba-
Indications: Management of prostate cancer, similar to those observed in the early anorexia, constipation, pruritus, nausea and mazepine or sodium valproate (both section
breast cancer in premenopausal and peri- follicular phase (approx. 150 pmol/l). vomiting, and insomnia. Health organizations 1.7.1); ketamine (section 3.1.1) or lidocaine
menopausal women, endometriosis; uterine This will usually take between 7 and should be encouraged to develop their own (section 5.4) by intravenous infusion may be
fibroids (in conjunction with iron therapy in 21 days.When downregulation is palliative care services. useful in some situations. Neuropathic pain
the haematological improvement of anaemia achieved, superovulation (controlled Pain relief can be achieved with drugs and responds only partially to opioids, but they
patients with fibroids prior to surgery); prethin- ovarian stimulation) with gonado- neurosurgical, psychological and behavioural my be considered when other options fail. A
ning of the endometrium prior to endometrial trophin is commenced. The down- approaches adapted to individual patient corticosteroid may be required, particularly to
ablation or resection. regulation achieved with a depot needs. If carried out correctly, most patients relieve pressure and therefore pain in patients
Assisted reproduction: Pituitary down regula- agonist is more consistent suggesting with cancer pain can obtain effective relief. with nerve compression.
tion in preparation for superovulation. that, in some cases, there may be an Pain is best treated with a combination of drug
Contra-indications: Hypersensitivity to the increased requirement for gonado-
13.1 Anti–infective drugs | 603
13. Ophthalmological
Administration of eye preparations atitis requires immediate specialist treatment.
Preparations for the eye should be sterile when Aciclovir is an antiviral used in the treatment
issued. Use of single application containers is of keratitis due to herpes simplex virus. Lesions
preparations
preferable; multiple-application preparations usually heal after 5–9 days of treatment. For
include antimicrobial preservatives and when systemic treatment with antivirals, such as
used particular care should be taken to prevent aciclovir, see section 9.5.1.
contamination of the contents, including the Gentamicin is a broad-spectrum bactericidal
13.1 Anti–infective drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 603 avoidance of contact between the applicator aminoglycoside antibiotic with particular activ-
13.2 Anti-Inflammatory/Anti-allergic/Anti-infective drugs. . . . . . . . . . . . . . . . . . . . . . 608 and the eye or other surfaces. ity against Pseudomonas aeruginosa, Neisseria
Eye drops are generally instilled into the lower gonorrhoea and other bacteria that may be im-
13.3 Mydriatics and cycloplegics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 614 conjunctival sac which is accessed by gently plicated in blepharitis or conjunctivitis. Topical
13.3.1 Antimuscarinics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 614 pulling down the lower eyelid to form a pocket application may lead to systemic absorption
into which one drop is instilled. The eye should and possible adverse effects.
13.3.2 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 615 be kept closed for as long as possible after
application, preferably 1–2 minutes. A small Idoxuridine is an antiviral used in the treat-
13.4 Drugs used in glaucoma. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 616 ment of keratitis due to herpes simplex virus.
amount of eye ointment is applied similarly;
13.4.1 Miotics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 617 the ointment melts rapidly and blinking helps Idoxuridine is effective against epithelial
to spread it. infections of recent origin. These may re-
13.4.2 Beta-blockers . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 617 spond to treatment within a week and resolve
When two different eye drops are required
13.4.3 Sympathomimetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 618 at the same time, dilution and overflow may completely in 1–2 weeks. Eye drops must be
occur if one immediately follows the other; an applied frequently to maintain a high concen-
13.4.4 Carbonic anhydrase inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 619
EMDEX
interval of at least 5 minutes should be allowed tration and achieve a successful therapeutic
13.4.5 Prostaglandin analogue . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 619 between the two applications. outcome; however, if there is no relief within
Systemic absorption, which may occur after 7 days, treatment should be discontinued and
13.5 Local anaesthetics. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 620
topical application of eye drops, can be min- alternative treatment is indicated. For systemic
13.6 Miscellaneous eye preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 620 imized by using the finger to compress the treatment with antivirals such as aciclovir, see
lacrimal sac at the medial canthus for at least section 9.5.1.
one minute after instillation of the drops. This Silver nitrate is a topical anti-infective. Its
helps block the passage of the drops through antibacterial activity is attributed to precipi-
the naso-lacrimal duct. tation of bacterial proteins by silver ions. It is
PERFORMANCE OF SKILLED TASKS available in 1% ophthalmic solutions and is
used for prophylaxis of gonococcal ophthalmia
Application of eye preparations may cause neonatorum.
blurring of vision which is generally transient;
patients should be advised not to carry out Tetracycline is a broad spectrum antibiotic
skilled tasks such as operating machinery or with activity against many Grampositive
driving until their vision has cleared. and Gram-negative bacteria including N.
gonorrhoea, and most chlamydia, rickettsia,
13.1 Anti–infective drugs mycoplasma and spirochetes. Ophthalmic tet-
racycline is used in blepharitis, conjunctivitis,
Blepharitis, conjunctivitis, keratitis and en- and keratitis produced by susceptible bacteria.
dophthalmitis are common acute infections of Tetracycline is also used in the treatment of
the eye and can be treated topically. However, trachoma caused by Chlamydia trachomatis
in some cases, for example, in gonococcal and in the prophylaxis of neonatal conjunc-
conjunctivitis, both topical and systemic tivitis (ophthalmia neonatorum) caused by N.
anti-infective treatment may be necessary. gonorrhoea and C. trachomatis.
Blepharitis and conjunctivitis are often caused
by staphylococcus, while keratitis and endoph- ACICLOVIR
thalmitis may be bacterial, viral or fungal. Bac- Indications: Keratitis caused by herpes sim-
terial blepharitis is treated with an antibacterial plex; systemic infections (section 9.5.1).
eye ointment or drops. Although most cases Adverse effects: Local irritation including
of acute bacterial conjunctivitis may resolve transient mild stinging, inflammation; super-
spontaneously, anti-infective treatment ficial punctuate keratopathy reported; very
shortens the infectious process and prevents rarely hypersensitivity reactions including
complications. Acute infective conjunctivitis is angioedema.
treated with antibacterial eye drops by day and Dose: Herpes simplex keratitis, by application
eye ointment applied at night. A poor response to the eye, ADULT and CHILD 1 cm
may indicate viral or allergic conjunctivitis. Ker- of ointment 5 times daily; continue
604 | 13.1 Anti–infective drugs 13.1 Anti–infective drugs | 605
for at least 3 days after healing is POM Chloramphenicol (NCI) Eye/Ear drop, Ciprofloxacin 3 mg per mL GENTAMICIN
complete. Eye/Ear drops, Chloramphenicol 0.5% w/v; colour- Pack: 5 mL
less soln. Gentamicin is a representative ophthalmic antibacterial.
POM Aciclovir (WMF 21.1) POM CIPRO-J® (Juhel) Various drugs can serve as alternatives.
Pack: 10 mL x 1’s
Ointment, Aciclovir 3% w/w. Eye/Ear drops, Ciprofloxacin base 0.3%w/v, Benza-
POM CHLOROPHENICOL® (Richygold) lkonium chloride 0.01% w/v; clear liquid. Therapeutic category: Topical antibiotic,
POM Acyclovir (EDL 24.1) Eye ointment, Chloramphenicol. Pack: 10 mL (in polyethylene bottle). aminoglycoside
Eye ointment, Acyclovir 3%. Indications: Blepharitis; bacterial conjunctivi-
POM CHLOZAR® (Shrezar) POM CIPROEYE® (Kayhelt)
POM ZOVIRAX® (SKG) Ear drop, Chloramphenicol 5% Solution, Ciprofloxacin HCI 0.3%, benzalkonium tis; systemic infections (section 9.1.2.5).
Eye ointment, Aciclovir 3%. Pack: 10 mL chloride 0.01% per mL Contra-indications: Hypersensitivity to
Eye drop, Chloramphenicol 0.5% Pack: 5 mL; 10 mL aminoglycoside group of antibiotics.
CHLORAMPHENICOL Pack: 10 mL Indications: Treatment of corneal ulcer and con- Precautions: Prolonged use may lead to
Indications: Ocular infections POM CRISTAPHENICOL® (Crystal)
junctivitis caused by susceptible strains of bacteria. skin sensitization and emergence of resistant
Adverse effects: Blood dyscrasias Eye/Ear drops, Chloramphenicol 0.5% w/v POM CIPROZAR® (Shrezar) organisms including fungi; discontinue if
Advice to patients: Wash hands, clean crusts Pack: 10-mL bottle with dropper. Eye/Ear drop, Ciprofloxacin HCl 0.3%, benzalkonium purulent discharge, inflammation or exacer-
or discharge from eye, instil eye drops and chloride solution 0.01% (as preservative) bation of pain.
POM IVYPHENICOL® (Dortemag)
apply pressure to lacrimal sac for 1 minute Pack:10 mL Adverse effects: Burning, stinging, itching,
Eye drop, Chloramphenicol 0.5%.
to prevent systemic absorption; do not share Pack: 10-mL bottle with dropper
dermatitis.
POM EYE-CIPRO® (Al-Tinez)
make-up and towel with family members dur- Eye drop, Ciprofloxacin HCI 0.3%, benzalkonium
Advice to patients: Wash hands, clean crusts
ing infection; do not allow the container tip to POM MCA Chloramphenicol (Embassy) or discharge from eye, instil eye drops and
chloride (as preservative) 0.5%
Eye drop, Chloramphenicol 5 mg per mL. apply pressure to lacrimal sac for 1 minute
touch the eye; discontinue therapy and notify Pack: 10 mL
Pack: Bottle of 10 mL with dropper.
physician immediately of any signs of sensitiv- to prevent systemic absorption; do not share
Ear drop, Chloramphenicol 50 mg per mL. POM IVYZOXAN® (Dortemag)
EMDEX
ity viz itching, increased redness, burning or make-up and towel with family members dur-
Eye/ear drops, Ciprofloxacin (as HCl) 3 mg per mL
stinging sensation; ointment may temporarily POM OPTACHLOR® (Standard Generics) ing infection; do not allow the container tip to
Pack: 5 mL.
Eye drops, Chloramphenicol 0.5% touch the eye; discontinue therapy and notify
blur vision, apply in the night. Indications: Bacterial infections of the eye and the
Pack: 10 mL
Dose: 1-2 drops 4 times daily; up to hourly in ear and for corneal ulcers. physician immediately of any signs of sensitiv-
severe cases. Apply ointment in the POM RICHPHENICOL® (Goldmoore) Adverse effects: Burning, discomfort, itching, foreign ity viz itching, increased redness, burning or
night in conjuction with daily drops. Eye drop, Chloramphenicol 0.5%. body (gritty) sensation, redness of the eye or inside stinging sensation; ointment may temporarily
Pack: 10-mL bottle. the eyelid, crust formation on the eyelid, swelling of blur vision, apply in the night.
POM Chloramphenicol (EDL 24.1) the eyelid, decreased vision, increased tear produc-
Eye-drops, Chloramphenicol 0.5% POM VISTAPHENICOL® (Alpha) Dose: Mild to moderate infection, by instilla-
tion, sensitivity to light and particles in the cornea; tion into the eye, ADULT and CHILD
Eye Ointment, Chloramphenicol 1% Eye drops, Chloramphenicol 0.5%
nausea, bad taste in the mouth and allergic reactions
Compound preparations
1 drop every 2 hours, reducing fre-
POM CAFON Eye Drop (Beta Drugs) e.g. itching, swelling or breathing difficulties.
Dose: Eye infections, Adult and child, Instil 2 drops quency as infection is controlled, then
Eye drop, Chloramphenicol 0.5%. POM CANDIBIOTIC® (Glenmark)
in the affected eye every 3 hours. continue for 48 hours after healing is
Pack: 20-mL dropper bottle. Ear drop, Chloramphenicol 5%, beclometasone
Corneal ulcers, Instil 2 drops every 15 min- complete.
POM CHLOMACOL® (Geneith) dipropionate 0.025%, clotrimazole 1%, lidocaine 2%.
utes for the first 6 hours and then 2 drops Severe infection, by instillation into
Eye drops, Chloramphenicol 0.5% Pack: 5 mL.
every 30 minutes during the first day; On the eye, ADULT and CHILD 1 drop
Pack: 10 mL Indications: Allergic and inflammatory conditions
the second day, 2 drops every hour; from every hour, reducing frequency as
of the ear. Otorrhoea, wax, middle/external ear’s
POM CHLORACETIN® (Hochiez) 3rd to 14th day, 2 drops every 4 hours. infection is controlled, then continue
fulminating bacterial infections. Mastoid surgery.
Eye drop, Chloramphenicol 0.5 w/v. Duration is usually 14 days.
Dose: Instil 4-5 drops in the ear 3-4 times a day. for 48 hours after healing is complete.
Pack: 10 mL. Ear infection, 2-3 drops in affected ear 3-4
POM MEDICLOPHENCID-H® (Neros) times a day and at night. POM Gentamicin (WMF 21.1)
POM Chloramphenicol (Alpha) Ointment, Chloramphenicol 40 mg, hydrocortisone Eye drops,Gentamicin (as sulfate) 0.3%; solution.
Eye drop, Chloramphenicol 0.5%. acetate 30 mg. CIPROFLOXACIN plus DEXAMETHASONE
Pack: 10 mL. POM Gentamicin (EDL 24.1)
Indications: Eye: keratoconjuctivitis, chronic
See under the preparations below. Eye drops or ointment, Gentamicin sulfate 0.3%.
POM Chloramphenicol (Drugfield) conjunctivitis, keratitis, blepharitis, dacryocystitis
Eye drop, Chloramphenicol 5 mg per mL and traumatic conditions caused by burn, caustic POM ALCOMICIN® (CHI )
or eyelid eczema. Skin: ulcer, folliculitis, eczema, POM DEXCIPRO® (Kayhelt) Eye-drops, Gentamicin sulfate 3 mg per mL.
Pack: 10 mL
dermatitis, lichen, erythema, lupus. Eye drop, Ciprofloxacin HCI 0.3%, dexamethasone
Ear drop, Chloramphenicol 50 mg per mL POM BACLEXIN® (Evans)
Dose: Eye: Apply a small amount of the ointment 0.1%, benzalkonium chloride 0.01% per mL
Pack: 10 mL Eye drop, Gentamicin.
to the affected eye 3-4 times a day, for Pack: 5 mL; 10 mL
Eye ointment, Chloramphenicol 10 mg per 1 g Pack: 5 mL.
5-12 days. Indications: Treatment of corneal ulcer and conjunc-
Pack: 5 g
Skin: Apply a thin layer of the ointment tivitis caused by susceptible strains of bacteria. Dexa- POM DRUGENT® (Drugfield)
POM Chloramphenicol (Hovid) to the affected skin 3-4 times a day, for methasone is used to treat eye inflammation caused Eye/Ear drop, Gentamicin (as sulphate) 3 mg per mL
Eye-drops, Chloramphenicol 0.5% 5-12 days. by infections, injury, surgery, or other conditions. Pack: 10 mL
POM ZIPRONAT® Plus (Zeenat) POM EVRIL® (Medreich)
POM Chloramphenicol (Juhel) CIPROFLOXACIN Eye drop, Ciprofloxacin 0.3% w/v, Dexamethasone Eye/Ear drops, Gentamicin sulfate BP equiv. to 0.3%
Eye drop, Chloramphenicol 0.5% 0.1% w/v. w/v Gentamicin base; clear colourless & sterile soln
See under the preparations below.
Pack: 10 mL Pack: 5 mL Pack: 10-mL plastic bottle.
Ear drop, Chloramphenicol 5% POM CIFLAXIN® (Drugfield).
Pack: 10 mL POM GARMICIN® (Standard Generics)
606 | 13.1 Anti–infective drugs 13.1 Anti–infective drugs | 607
Eye & Ear drops, Gentamicin (as sulfate) 0.3% Pack: 5 mL. POM Idoxuridine (EDL 24.1) components and also after uncomplicated removal
Eye-drops, Idoxuridine 0.1% of a cornea foreign body in eye. Otic use is not recom-
POM GENTA® (Nosak) POM IVYDEXGENT® (Dortemag)
Eye Ointment, Idoxuridine 0.5% mended where there is perforation of the ear drum.
Eye drops, Gentamicin (as sulfate) 0.3%. Eye/Ear drops, Dexamethasone (as sodium phos-
Adverse effects: Elevation of intraocular pressure
Pack: 15 mL phate) 1 mg, gentamicin (as sulfate) 3 mg per mL POM DENDRID® (CHI )
with possible development of glaucoma and infre-
Dose: Eye: Instil 1-2 drops in the affected eye up to Eye-drops, Idoxuridine 0.1%
POM GENTAGLOB® (Hochiez) quent optic nerve damage; posterior subcapsular
6 times a day. Pack: 15 mL
Eye/Ear drop, Gentamicin (as sulfate) 0.3%. cataract formation; and delayed wound healing.
Ear: Instil 2 or 3 drops in the ear 3-4 times a Eye Ointment, Idoxuridine 0.5%
Pack: 10 mL. Secondary development of bacterial or fungal infec-
day and at night. Pack: 3.5 g.
tions. Cornea is prone to fungal infections especially
POM GENTALAB® (Embassy) with prolonged use of steroids.
Eye/Ear drops, Gentamicin. IDOXURIDINE MICONAZOLE Dose: Ophthalmic: Instil 1-2 drops into the affected
Pack: 10 mL. eye 3 times daily.
Deleted from the current WHO Model Formulary POM Miconazole (EDL 24.2)
POM GENTALEK®(Taylek) Otic: Instil 2-4 drops into the external ear ca-
Eye drop, Miconazole 1%.
Eye/Ear drops, Gentamicin (as sulfate) 0.3%. Indications: Keratitis or keratoconjunctivitis nal for treatment of infections 3 times daily.
Pack: 5 mL. caused by herpes simplex. Shake well before use.
OFLOXACIN
Eye/Ear ointment, Gentamicin (as sulfate) 0.3% Contra-indications: Pregnancy; concurrent POM Oxytetracycline plus Polymyxin B (EDL 24.1)
Pack: 3 g (in tubes). use of an eye preparation containing boric acid. See under the preparations below. Eye ointment, Oxytetracycline HCl 5 mg, Polymyxin
POM Gentamicin (Al-Tinez) Precautions: Existing deep ulceration of cor- B sulfate 10,000 units per g; in 3.5 g tube
Eye drop, Gentamicin (as sulphate) 3000 IU, benza- nea; prolonged or excessive use may damage POM Ofloxacin (Zeenat)
lkonium chloride (as preservative) 0.01% per mL the cornea; do not exceed frequency or dura- Eye/Ear drop, Ofloxacin 0.3% mg w/v, Benzalkonium SULFACETAMIDE plus
Pack: 10 mL tion of treatment, discontinue if no relief within
chloride (as preservative). CHLORAMPHENICOL
Pack: 5 mL
7 days; concurrent use of a corticosteroid Pharmacology: Both chloramphenicol and
POM Gentamicin (GoldMoore)
Adverse effects: Occasionally burning, itch- POM Ofloxacin Eye Drop (Neros) sulfacetamide act bacteriostatically due to
EMDEX
Eye/Ear drops, Gentamicin (as sulfate) 0.3%.
Pack: 5 mL; 10 mL. ing, irritation, pain, conjunctivitis, oedema, Eye drop, Ofloxacin 0.3%. their interference with the metabolism of the
inflammation, photophobia, pruritus; rarely Pack: 5 mI bottle. bacteria cell. Chloramphenicol is a lipophilic,
POM Gentamicin (Juhel) Indications: Infections of the external segment of
allergic reactions. low molecular weight antibiotic which acts
Eye/Ear drops, Gentamicin base 0.3% w/v, Benzalko- the eye: conjunctivitis, corneal ulcer, dacryocysitis,
nium chloride 0.01% w/v; clear liquid. Advice to patients: Patient should understand by inhibiting the protein synthesis due to a
blepharitis, tarsitis, sty.
Pack: 10 mL (in polyethylene bottles). how to instil the drug. May cause sensitivity to Contra-indications: Hypersensitivity to ofloxacin supression of the transfer of activated amino
bright light; minimize by wearing sunglasses; or any derivatives of quinolones. Children under acids. Sulfacetamide, an antagonist of P-ami-
POM GENTAZET® (Geneith) nobenzoic acid (PABA) inhibits the synthesis
notify physician if improvement is not seen 1 year old, pregnant woman and nursing mothers.
Eye/Ear drops, Gentamicin 0.3%.
in 7-8 days, if condition worsens, or if pain, Precautions: Do not wear contact lenses when of folic acid inside the bacterial cell. The com-
Pack: 5 mL x 1’s
decreased vision, itching, or swelling of the using the drug. bination of both drugs results in an increased
POM GENTINEX® (Neros) eye occur; do not exceed recommended dose. Adverse Reactions: A short-term warm sensation in antibacterial spectrum.
Eye drop, Gentamicin (as sulfate) 0.3%. the eye may occur. Indications: Bacterial infections of the eyelids,
Nursing action:
Pack: 5 mI bottle. Dose: Instil 2 drops into the affected eye (s), 4 times the conjunctiva, the cornea (corneal ulcer),
• Teach patient how to instill drops.
daily. May use longer than 15 days if needed.
POM IVYGENTACIN® (Dortemag) • Idoxuridine solution should not be mixed with the anterior uvea as well as of the lacrimal
Eye/Ear drop, Gentamicin (as sulfate) 3 mg per mL. other topical eye medications. POM OFLOXALAB® (Embassy) system. Trachoma and other infections caused
Pack: 10 mL • Store Idoxuridine 0.1% solution in a refrigerator. Eye/Ear drop, Ofloxacin 3 mg per mL. by chlamydozoa, benign lymphoreticulosis
• Idoxuridine may cause sensitivity to bright Pack: 10 mL.
POM KAYMICIN® (Kayhelt) (cat-scratch fever) and Parinaud’s conjunctiva.
light; advise patient to minimize this by wearing
Eye/Ear drop, Gentamicin sulphate 0.3%, phenyl- Prophylaxis of infection before and after rinsing
sunglasses, and to avoid prolonged exposure to OXYTETRACYCLINE plus POLYMYXIN B
mercuric nitrate 0.002% (as preservative) per mL. sunlight. of the lacrimal duct, before and after eye sur-
Pack: 5 mL Indications: Prophylaxis and treatment of gery as well as after cauterizations and burns.
Dose: Herpes simplex keratitis, by instillation
superficial ocular infection due to susceptible Contra-indications: Hypersensitivity to the
POM TAMAN® (Beta Drugs) (522) into the eye, ADULT and CHILD 1
Eye/Ear drops, Gentamycin 0.3%. organisms. ingredients.
drop every hour during daytime and
Pack: 20-mL dropper bottle. Dose: Apply the Ointment 3-6 times daily Interactions: Avoid co-administration with
every 2 hours at night-time, reducing
usually for 10-15 days in acute and up other topical preparations containing heavy
POM ZARCIN® (Shrezar) frequency as infection is controlled to
to 3 months in chronic cases. metals particularly copper, zinc and silver due
Eye/Ear drop, Gentamicin (as sulphate) 0.3%, phenyl- 1 drop every 2 hours during daytime
mercuric nitrate (as preservative) 0.002% . and every 4 hours at night-time, then POM OXYCORTRIL-B® (Drugfield) to chemical incompatibilities. Avoid co-ad-
Pack: 10 mL continue for 3–5 days after healing Eye/Ear suspension, Oxytetracycline 10 mg (as HCI) ministration with bactericidal substances such
is complete; maximum length of hydrocortisone 5 mg (as acetate) polymyxin 10,000 as penicillins, cephalosporins (antagonism is
GENTAMICIN plus DEXAMETHASONE (as sulphate) per 1 mL. possible).
treatment 21 days.
Pack: 5 mL Adverse effects: Rarely allergic reactions
See under the preparations below. Herpes simplex keratitis, by applica- Indications: Treatment of blepharitis of the eyelid,
tion to the eye, ADULT and CHILD 1 which manifest as eczema of the eyelid mar-
conjunctivitis, scleritis, epideritis of sclera; non-spe-
POM GENTACORT-D® (Embassy) application of ointment every 4 hours gin. Prolonged topical therapy (2-3 months)
cific inflammatory conditions involving the cornea,
Eye/Ear drops, Gentamicin 0.3%, dexamethasone during daytime and once at night- particularly where neo-vascularization is a problem;
with chloramphenicol may cause aplastic
0.05%. time (5 applications), then continue infection of the external ear canal caused by sus- anaemia.
Pack: 10 mL. for 3–5 days after healing is complete; ceptible organisms; in infections of undetermined Dose: Instil 1 drop 2-4 times daily; up to 1
maximum length of treatment 21 etiology accompanied by inflammatory reactions. drop hourly in acute cases.
POM BACLEXIN-D® (Evans)
days. Contra-indications: Hypersensitivity to any of the
Eye drop, Gentamicin, dexamethasone. POM SPERSACET C®
608 | 13.2 Anti-Inflammatory/Anti-allergic/Anti-infective drugs 13.2 Anti-Inflammatory/Anti-allergic/Anti-infective drugs | 609
Eye-drops, Sulfacetamide sodium 100 mg, chloram- sive corneal ulcer and subsequent permanent ANTAZOLINE plus TETRAHYDROZOLINE Ears: 2-3 drops, 2-3 hourly.
phenicol 5 mg per mL. corneal scarring, with possible damage to Therapeutic category: Antiallergic/Vaso-
Pack: 10 mL. POM BETNESOL® (GSK)
vision and even loss of the eye. constrictor Drops, (Ear or Eye), Betamethasone sodium
Corticosteroids such as prednisolone are Pharmacology: The antihistamine antazoline phosphate 0.1%
TETRACYCLINE Pack: 5 mL; 10 mL
useful in the treatment of inflammatory con- blocks the histamine receptors and in this way
Tetracycline is a representative ophthalmic antibacterial. ditions including uveitis and scleritis. They are protects the cell membrane from the effects of Eye Ointment, Betamethasone sodium phosphate
Various drugs can serve as alternatives. liberated histamine and prevents the patho- 0.1%
also used for reducing postoperative ocular
Pack: 3 g.
Indications: Superficial bacterial infection of inflammation. Before administration of an logical changes that would otherwise occur.
the eye; mass treatment of trachoma in en- ophthalmic corticosteroid, the possibility of The vasoconstrictor tetrahydrozoline rapidly POM VISTAMETHASONE® (Alpha)
bacterial, viral or fungal infection should be relieves irritation of the conjunctiva and brings Eye/Ear drops, Bethamethasone sodium phosphate
demic areas; prophylaxis of neonatal conjuncti-
a subjective improvement. Lacrymal secretion 1%.
vitis (ophthalmia neonatorum) due to Neisseria excluded. Treatment should be the lowest
is slightly reduced but the preparation has no Pack: 10 mL
gonorrhoea or Chlamydia trachomatis. effective dose for the shortest possible time;
Contra-indications: Hypersensitivity to tetra- if long-term therapy (more than 6 weeks) is effect on pupillary diameter, accommodation
BETAMETHASONE plus NEOMYCIN
cycline group of antibiotics. unavoidable, withdrawal of an ophthalmic cor- or intraocular pressure.
ticosteroid should be gradual to avoid relapse. Indications: Inflammatory conditions of Therapeutic category: Corticosteroid/anti-
Precautions: Prolonged use may lead to over-
the conjunctiva of allergic origin, especially bacterial.
growth of non-susceptible organisms.
ANTAZOLINE plus NAPHAZOLINE hay-fever and vernal conjuctivitis, and in drug Pharmacology: Betamethasone has topical
Adverse effects: Rash; rarely stinging, burning.
hypersensitivity reactions, excessive lacrymal corticosteroid activity. The presence of ne-
Dose: Superficial bacterial infection, by appli- Therapeutic category: Mucosal decongestant
secretion and stenosis of the lacrymal canal. omycin should prevent the development of
cation to the eye, ADULT and CHILD with antihistaminic effect.
Nursing action: See under Antazoline plus bacterial infection.
aged over 8 years 1 application of Pharmacology: Naphazoline is a vasocon-
Naphazoline. Indications: For short-term treatment of
ointment 3–4 times daily. Prophy- strictor which has both a rapid and prolonged
EMDEX
Dose: In acute cases, one drop 3 hourly. steroid responsive inflammatory conditions
laxis of neonatal conjunctivitis, by action in suppressing conjunctival hyperaemia.
In protracted treatment, one drop 2-3 of the eye after clinical exclusion of bacterial,
application to the eye, NEWBORN at Antazoline is an antihistamine with an antialler-
times daily. viral and fungal infections but where proph-
birth after cleansing eyes with sterile gic action which reduces vascular permeability.
In severe cases, can be applied hourly. ylaxis against secondary bacterial infection
gauze, 1 application of ointment into Indications: Irritative conjunctivitis, allergic
Child: 1-2 drops daily is required, such as allergic conjunctivitis,
each eye; close eyelids and massage disorder of the conjunctiva (vernal catarrh).
blepharitis, uveitis, etc.
gently to aid spread of ointment. Precautions: Some sensitive patients might POM Antazoline plus Tetrahydrozoline (EDL 24.2)
Trachoma, intermittent treatment, by have a passing prickling feeling during instilla- Eye-drops, Antazoline HCl 0.5%, Tetrahydrozoline
under betamethasone.
application to the eye, ADULT and tion which, however, does not affect the treat- HCl 0.05%.
Dose: 1-2 drops, 1-2 hourly or the ointment
CHILD 1 application of ointment into ment’s efficacy. Close the bottle immediately POM ANTALLERGE® (Drugfield) 3-4 times daily and/or at night.
each eye either twice daily for 5 days after use and discard any remaining product Eye drop, Antazoline HCI 0.5 mg, tetrahydrozoline
or once daily for 10 days, every month at the end of treatment. HCI 0.4 mg per mL. POM BETADRONE-N® (Drugfield)
for 6 consecutive months each year, Advice to patients: Discontinue eye drops if Pack: 10 mL Eye ointment, Neomycin sulphate 5 mg, betamethasone
repeated as necessary. Trachoma, con- visual changes or ocular pain occurs. Notify sodium phosphate 1 mg per g.
POM SPERSALLERG® (Novartis) Pack: 5 g
tinuous intensive treatment, by appli- physician of insomnia, tremor, or irregular Eye-drops, Antazoline HCl 0.5 mg, tetrahydrozoline Eye/Ear drop, Betamethasone sodium phosphate 1
cation to the eye, ADULT and CHILD 1 heartbeat; do not use for more than 72 hours HCl 0.4 mg per mL. mg, neomycin sulphate 5 mg.
application of ointment into each eye unless directed to do so; remove contact lenses Pack: 10 mL. Pack: 10 mL (in lupolen bottle)
twice daily for at least 6 weeks. before using in eye.
Nursing action: BETAMETHASONE POM BETNACIN-EEN® (Korlyns)
POM Tetracycline (WMF 21.1) Eye/Ear Nasal drop, Betamethasone sodium phosphate
• Teach patient how to instill the drug: wash hands Therapeutic category: Corticosteroid
Eye ointment, Tetracycline (as HCl) 1%. 0.1%, neomycin 0.5%.
before and after instillation, avoid touching drop-
Indications: Short-term treatment of steroid Pack: 10 mL
POM LIF-EYE® (Jubilee) per tip to eye or sorrounding tissue, tilt head back,
place medication in conjunctival sac, and close
responsive inflammatory conditions of the eye
Eye ointment, Tetracycline HCl USP 1%. POM BET-N® (Juhel)
Pack: 3.5 g collapsible tube. eyes. Apply light finger-pressure on lacrimal sac after clinical exclusion of bacterial, viral and
Eye/Ear drops, Bethamethasone sodium phosphate
for 1minute following instillation. fungal infections. Non-infected inflammatory 0.1% w/v, Neomycin sulfate 0.5% w/v; clear liquid
POM Tetracycline (GoldMoore) conditions of the ear.
• Instruct patient to report changes in vision, blur- Pack: 10 mL (in polyethylene bottle).
Eye Ointment, Tetracycline (as HCl) 1% w/w.
ring or loss of sight, headache, respiratory dys- Contra-indications: Bacterial, viral and fungal
Pack: 3.5 g tube. POM BETNESOL-N® (GSK)
function, sweating, anxiety, weakness, lid oedema. infections, tuberculosis or purulent conditions
• Reassure patient that the blurring of vision will Eye-drops, Betamethasone sodium sulfate 0.1%,
of the eye; glaucoma, herpetic keratitis (e.g.
13.2 Anti-Inflammatory/Anti-allergic/ decrease with repeated use of drugs; he should dendritic ulcer); patients who wear soft lenses.
Neomycin sulfate 0.5%.
Anti-infective drugs avoid hazardous tasks until he can see properly. Pack: 5 mL, 10 mL
Precautions: Should not be administered to Eye Ointment, Betamethasone sodium phosphate
Ophthalmic corticosteroids should only be • Inform patient that rebound congestion and
conjunctivitis may occur with frequent and pro-
“red eyes” until definitive diagnosis is made; 0.1%, neomycin sulfate 0.5%
used under supervision of an ophthalmologist prolonged use without regular check to ex- Pack: 3 g.
longed use.
as inappropriate use is potentially blinding. clude raised intra-ocular pressure.
Dose: Instil 1-2 drops into the conjunctival POM EYEBETSOL-N® (Al-Tinez)
Dangers include the development of open-an- Adverse effects: Rise in intra-ocular pressure,
sac 3-4 times daily. Eye/Ear drop, Betamethasone sodium phosphate
gle glaucoma (chronic simple glaucoma) and corneal perforation, cataract. 0.1%, neomycin (as sulfate) 0.5%, thiomersal 0.005%
Child: 1-2 drops daily.
cataracts, and the aggravation of a simple Dose: Eyes: 1-2 drops, 1-2 hourly or the oint- (as preservative)
herpes simplex epithelial lesion into an exten- ment 2-3 times daily and/or at night Pack: 10 mL
POM IVYBETANEOCIN® (Dortemag) mg per mL. Pack: 5 mL enzyme phospholipase A2. It also inhibits the
Eye/Ear drop, Betamethasone (as sodium phosphate) 1 Pack: 5 mL. Indications:Acute and chronic keratitis and con- chemostatic infiltration of neutrophils into
mg, neomycin (as sulfate) 3.5 mg per mL. junctivitis of an allergic nature with severe swelling the focus of inflammation. In contrast to other
Dose: Instil 1 drop in the affected eye 4-6 times a day DEXAMETHASONE plus and increased vascular injection. Inflammation topical glucocorticoids, fluorometholone does
CHLORAMPHENICOL of the anterior uvea (iritis, iridocyclitis), scleritis,
POM NEKESOL-N® (Lifeback) not significantly raise the intraocular pressure
Therapeutic category: Corticosteroid/anti- episcleritis, myositis. Sympathetic ophthalmia.
Eye/Ear Drops, Betamethasone (as Na+ phosphate) as it is more rapidly degraded in ocular tissue.
biotic. Dose: Instill 1 drop 1-4 times daily into the conjunc-
0.1%, neomycin (as sulfate) 0.5%. Its anti-inflammatory action is at least 40 times
Indications: Non-purulent forms of infectious tival sac; may increase to 1 drop hourly in
Pack: 10 mL (with dropper) stronger than that of hydrocortisone. Tetrahy-
acute cases.
conjunctivitis and blepharitis of allergic origin; drozoline (Tetryzoline) is a sympathomimetic,
POM VISTAMETHASONE-N® (Alpha) Note: To keep systemic resorption as low as pos-
Eye/Ear drops, Bethamethasone sodium phosphate
Kerato-conjunctivitis, non-viral keratitis, acne sible, the tear flow should be blocked by pressing which causes local vasoconstriction due to
0.1%, neomycin sulfate 0.5%. rosacea keratitis, iritis, post operative anti-exu- with the finger on the side of the nose, near the its alpha-adrenergic receptor agonist activity.
Pack: 10 mL dative treatment after eye surgery. cornea, for 1-2 mins after instillation. The vasoconstrictive action of tetryzoline sets
Contra-indications: Injuries and ulcerating in rapidly and alleviates swelling, hyperaemia
+ Clotrimazole
conditions of the cornea, particularly those DEXAMETHASONE plus NEOMYCIN and irritation of the conjunctiva.
POM DERMABACT® (Xcel) of viral origin, purulent infections of the con- Therapeuticcategory:Anti-inflammatory/Antialler-
Cream, Betamethasone dipropionate 0.05%, neo- Indications: Acute allergic non-infectious
junctiva and eyelids, tuberculous infections, gic/Antibiotic. conjunctivitis and keratitis; non-infectious
mycin sulfate 0.35%, clotrimazole 1%. mycosis, glaucoma.
Pack30 gm Indications: Eye infection and inflammation inflammation of the anterior segment of the
Precautions: Primary infection of the eye such as keratits, conjunctivitis, iritis; ulcers, eye (including anterior uveitis, episcleritis and
may be masked by corticosteroid; children, burns and injuries of the cornea. scleritis); postoperative inflammation following
DEXAMETHASONE
prolonged use. Contra-indications: Ophthalmic herpes sim- squint, cataract and glaucoma operations.
Therapeutic category: Corticosteroid Adverse effects: Rise in intraocular pressure. plex, fungal infections of the eye and ear, acute Contra-indications: Hypersensitivity to any
Indications: Vernal catarrh, allergic nonin- Advice to patients: Ensure patient under-
EMDEX
phase of most viral infections of the cornea component of the preparation; infectious
fectious blepharitis and conjunctivitis, nonin- stands instillation method; shake suspension and conjunctiva. conjunctivitis or keratitis; injuries and ulcerous
fectious keratitis; iritis, myositis, sympathetic well before use; notify physician of exacerba- Precautions: Raised I.O.P.; prolonged ap- processes of the cornea, especially infections
ophthalmia. tion of cornea or ulceration; do not discontinue plication of steroids to the eyes may cause caused by virus, bacteria and fungi; glaucoma;
Contra-indications, Precautions, etc: See drug abruptly. Discard after 28 days of opening subcapsular cataracts. diseases associated with stromal damage to
under Betamethasone. the bottle. Adverse effects: Rarely hypersensitivity reac- the cornea or sclera; dry eyes, especially kera-
Advice to patients: Ensure patient under- Dose: Instil 1 drop 3-5 times daily; up to 1 tions; secondary bacterial or fungal infections. toconjunctivitis sicca; children under 2 years.
stands instillation method; shake suspension drop hourly in severe cases. Dose: Instil 1-2 drops hourly during the day Not recommended for use during pregnancy
well before use; notify physician of exacerba-
POM DEXCHOL® (Al-Tinez) and every 2 hours at night; when con- and lactation.
tion of cornea or ulceration; do not discontinue
Eye/Ear drop, Dexamethasone sodium phosphate trolled, reduce to 1drop 4 hourly or Precautions: May temporarily affect visual
drug abruptly.
0.1%, chloramphenicol 1.0%, phenylmercuric nitrate even less frequently. Ointment, apply acuity; if affected do not drive or operate ma-
Nursing action: (as preservative) 0.002%.
• Teach patient how to instill the drug: wash hands as a thin layer 3-4 times daily until chinery. Administer after careful risk/benefits
Pack: 10 mL controlled then reduce frequeuency.
before and after instillation, avoid touching evaluation in the following cases: (1) Severe
dropper tip to eye or sorrounding tissue, shake POM SPERSADEX COMP.® (Novartis) POM BIVACYN-N®(Taylek) circulation disorders e.g. hypertension; (2)
suspension well before use, tilt head back, place Eye-drops, Dexamethasone phosphate 1mg, Chlo- Eye/Ear-drops, Dexamethasone 1 mg, neomycin Metabolic disturbances e.g. diabetes; (3) His-
medication in conjunctival sac, and close eyes. ramphenicol 5 mg per mL; opalescent colourless to sulfate 3500 I.U. (5 mg) per mL; in 5 mL vials. tory of ocular herpes simplex infection. Avoid
Apply light finger-pressure on lacrimal sac for 1 slightly yellow soln. Pack: 5 mL prolonged use. Reactive hyperaemia may occur
minute following instillation to prevent systemic Pack: 5 mL. Eyes/Ear Ointment, Dexamethasone 0.5 mg, neomy- after discontinuation of therapy. Regularly
absorption. cin sulfate 3500 I.U. per g.
POM STADEX® Plus (Drugfield) examine patients on long-term treatment
• Advise patient to stop medication and inform Pack: 3 g; 5 g (in tubes).
Eye drop, Dexamethasone sodium phosphate 1 mg, for intraocular pressure, systemic adverse re-
doctor immediately if visual acuity is affected or
chloramphenicol 5 mg per mL. POM NECODEX® (Mark) actions and secondary infections. May mask,
visual field diminishes.
Pack: 5 mL. Eye drops, Dexamethasone phosphate 0.1%, Neomy-
• Watch for corneal ulceration; may require stopping activate or aggravate an infection in the eye.
medication. + Tetrahydrozoline cin 0.35%, Benzalkonium chloride 0.01%. Use with caution in children and elderly due to
• Instruct patient not to share medication with other Pack: 5 mL. possibility of systemic adverse effects
POM EYESAXOLINE® (Al-Tinez)
family members. POM IVYDEXNEOCIN® (Dortemag) Interactions: Avoid co-administration with
Eye drop, Chloramphenicol 5 mg, dexamethasone
Dose: One drop 3-5 times daily; up to one disodium phosphate 1 mg, tetrahydrozoline HCI Eye/Ear drops, Dexamethasone (as sodium phos- TCAs or with MAOIs (for the latter there must
drop hourly in severe cases. 0.25 mg per mL phate) 1 mg, neomycin (as sulfate) 3.5 mg per mL. be an interval of at least 10 days since last
Indications: Acute and chronic keratitis and Dose: Instil one drop in the affected eye 4-6 times treatment).
POM IVYDEXONE® (Dortemag)
conjunctivitis with heavy swelling and superficial daily.
Eye drops, Dexamethasone (as sodium phosphate) Adverse effects: Slight and transient burning
1 mg per mL. congestion by allergy and inflammation; iritis, irid- sensation. Prolonged use may cause reactive
Pack: 5 mL ocyclitis, scleritis, episcleritis bullosa. FLUOROMETHOLONE plus
TETRAHYDROZOLINE hyperaemia. Rarely, allergic reactions. Local
Dose: Instil 1 drop in the affected eye(s) up to 4
POM OPTIDEX® (Standard Generics) times daily. Therapeutic category: Anti-inflammatory and application of steroids may cause: increased
Eye drops (0.1%), Dexamethasone (as sodium phos- decongestant combination. susceptibility to infections (especially mycosis/
phate) 5 mg; colourless solution POM STADEXOLENE® (Drugfield) herpes simplex), delayed wound healing and
Eye drop, Dexamethasone sodium phosphate 1 Pharmacology: Like all anti-inflammatory
POM STADEX® (Drugfield) glucocorticoids, fluorometholone reduces very rarely mydriasis, ptosis and exophthalmos.
mg, chloramphenicol 5 mg, tetrahydrozoline HCI
Eye drops, Dexamethasone sodium phosphate 1 prostaglandin synthesis by inhibiting the Long-term application of steroids may cause:
0.25 mg per mL.
increase in intraocular pressure, posterior
subcapsular cataracts, corneal melting and Dose: Instil 2-3 drops into the affected eye, patient’s reaction and therefore his ability to Pack: 5 mL
perforation of the globe and systemic adverse nostril or ear every 1-4 hours accord- drive, operate machinery or perform other POM IVYSOLONE® (Dortemag)
reactions (especially with children and geriatric ing to the severity of the case; after hazardous tasks. Ophthalmic suspension, Prednisolone (as acetate)
patients). Tetryzoline may cause irritation of the inflammation has subsided, the Dose: Adult, elderly and children above 12 10 mg per mL.
the conjunctiva and in rare cases mydriasis. In dosage may be gradually reduced to years, instil 1 drop twice daily into the Pack: 5 mL
spite of the low doses for topical application, 1-2 drops 3-4 times daily. conjuctival sac of each eye.
systemic sympathomimetic adverse reactions Child <12 years: Efficacy has not been SODIUM CROMOGLICATE
POM HYCOMYCIN®(Dizpharm)
are possible: palpitations, arrhythmia, angina, Drops,(Eye Nose or Ear), Hydrocortisone acetate tested but it has beeb shown to be
See under preparations below for information.
hypertension, occipital headaches, pallor, cen- 1.5%, neomycin sulfate 0.5%; as an isotonic buffered safe in children as young as 3 years.
tral excitation, tremor and sweating. suspension. Note: Maximum duration for treatment is 6 weeks. POM IVYCROM® (Dortemag)
Dose: Adult, instil 1 drop 2-3 times daily into Pack: 5 mL. May be used up to 1 month after first opening the Eye drops, Sodium cromoglycate 20 mg per mL.
the conjunctival sac. In the first 24-48 bottle (taking into account the expiring date). Indications: Relief and treatment of acute allergic
hours, the dose may be increased to 1 KETOTIFEN POM EYEDITEN® (Al-Tinez) conjunctivitis such as hay fever, chronic allergic
drop hourly for adults. Not recom- Therapeutic category: Anti-allergic. Ophthalmic solution, Ketotifen fumarate 0.69 mg, conjunctivitis and vernal kerato-conjunctivitis.
mended for child <2 years. Pharmacology: Ketotifen is a histamine H1-re- chlorobutanol 3 mg per 1 mL; colourless to pale Adverse effects: Transient stinging and burning.
yellow solution in a semi-transparent container. Dose: Adult and child, 1-2 drops in each eye, 4
POM EFEMOLINE® (Novartis) ceptor antagonist; it also inhibits the release of
Pack: 5 mL times a day
Eye-drops, Fluorometholone 1 mg, Tetrahydrozoline mediators (such as histamines, prostaglandins,
HCl 0.25 mg per mL. leukotrienes) from cells involved in type 1 POM KAYTIFEN® (Kayhelt) POM CRISTACROM® (Crystal)
Pack: 5 mL. or immediate allergic reactions (mast cells, Eye drop, Ketotifen fumarate 0.345 mg equiv. to keto- Drops, Sodium cromoglycate 2% w/v
tifen 0.25 mg, benzalkonium chloride 0.01% per mL. Pack: 10 mL
eosinophils, basophils and neutrophils). Keto-
HYDROCORTISONE plus NEOMYCIN tifen also reduces the chemotaxis, activation Pack: 5 mL. POM EYEGLYCATE® (Kayhelt)
EMDEX
Indications: EYE – Steroid-responsive allergic and degranulation of eosinophils. cAMP levels POM ZADITEN® (Oculus) Eye drop, Sodium cromoglicate 2%, benzalkonium
and inflammatory disorders of the anterior seg- increased by phosphodiesterase inhibition Eye drops, Ketotifen (as fumarate) 0.25 mg per mL. chloride 0.01%.
can contribute to the cell-stabilising action of Pack: Dropper bottle of 5 mL. Pack:5 mL; 10 mL
ment of the eye (conjunctival, corneal or uveal
tract inflammation) or mechanical, chemical or ketotifen. The antihistamine effect of ketotifen
eye drops has a rapid onset following instilla- PREDNISOLONE TETRAHYDROZOLINE
thermal trauma, where bacterial infection or a
risk of bacterial ocular infection exists. tion into the eye and persists for 8-12 hours. Indications: Short-term local treatment of Therapeutic category: Ophthalmic decon-
NOSE – Allergic and vasomotor rhinitis and Ketotifen eye drops alleviate the symptoms inflammation of the eye; malignant disease gestant
as an adjuvant treatment in affections of the of allergic conjunctivitis such as pruritus and (section 12.2.2); inflammatory and allergic Pharmacology: Tetrahydrozoline is a sympath-
sinus. hyperaemia. reactions (section 10.3, also section 8.3). omimetic agent which brings about deconges-
EAR – Inflammation and infection of the ex- Indications: Treatment and prevention of signs Contra-indications: Undiagnosed ‘red eye’ tion by vasoconstriction. It whitens reddened
ternal auditory canal, seborrheic dermatitis, and symptoms of allergic conjunctivitis. caused by herpetic keratitis; glaucoma. eyes by constricting the small blood vessels.
infected eczematoid dermatitis. Contra-indications: Hypersensitivity to keto- Precautions: Cataract; corneal thinning, It does not produce a dilation of the pupil or
Contra-indications: Hypersensitivity to either tifen or any of the excipients. corneal or conjunctival infection; discontinue cause rebound hyperaemia.
component of the preparation; topical corti- Precautions: In principle, contact lenses treatment if no improvement within 7 days; Indications: Symptomatic relief of conjunctival
costeroids should be avoided in tuberculosis of should not be worn if the eyes are red and/ risk of adrenal suppression after prolonged oedema and hyperaemia secondary to ocular
the skin, herpes simplex, vaccinia, varicella and or inflammed. The eye drops in bottles of 5ml use in infants. allergies, minor irritations, nonspecific or ca-
untreated fungal or viral ear infections; avoid contain benzalkonium chloride as preserva- Adverse effects: Secondary ocular infection; tarrhal conjunctivitis.
application to the external auditory canal of tive, which can permeate into soft hydrophilic impaired corneal healing (due to corneal thin- Precautions: Glaucoma.
patients with perforated eardrum. contact lenses. For this reason, soft hydrophilic ning), optic nerve damage, cataract; glaucoma, Adverse effects: Ocular stinging, burning,
Precautions: Pregnancy, breastfeeding; oto- contact lenses must be taken out before apply- mydriasis, ptosis, epithelial punctate keratitis, reactive hyperaemia
toxicity and nephrotoxicity may occur with ing ketotifen eye drops, and not replaced for at delayed hypersensitivity reactions including Advice to patients: See under Antazoline plus
topical neomycin in patients with aural or renal least 15 minutes (this does not apply to single burning, stinging. Tetrahydrozoline.
disease especially when co-administered with dose units which do not contain preservative). Dose: Note: Use only under the supervision Nursing action: See under Antazoline plus
aminogly-coside antibiotic; discontinue ther- Avoid use in irritation caused by contact lenses. of an ophthalmologist. Inflammation Naphazoline.
apy if sensitisation or irritation occurs; intraoc- Pregnancy. of the eye, by instillation into the eye, Dose: Instil 1-2 drops in each eye 2-3 times
ular pressure should be routinely monitored if Interactions: If several medicines are to be ADULT and CHILD 1 drop every 1–2 daily
used in the eye for 10 days or longer; advise administered into the eye, there should be an hours, reducing frequency as inflam- OTC IVYSINE® (Dortemag)
patients to refrain from tasks requiring visual interval of at least 5 minutes between each mation is controlled. Eye drops, Tetrahydrozoline (as HCl) 0.5 mg per mL.
acuity until they feel able to do so. application. POM Prednisolone (WMF 21.2) OTC PHARSINE® (Pharmabox)
Adverse effects: Rarely irritation or burning Adverse effects: Occasionally changes in Eye drops, Prednisolone (as sodium phosphate) Eye drops, Tetrahydrozoline (as HCl) 0.05%; colourless
may occur; prolonged ophthalmological use visual acuity, dry eyes, headaches, fatigue, 0.5%; solution. or yellowish transparent solution.
may cause elevated intraocular pressure and/ skin rash. Isolated cases of burning/stinging, Pack: 15 mL.
POM Prednisolone (EDL 24.2)
or glaucoma, posterior subcapsular cataract conjunctivitis, subconjunctival haemorrhage, Eye drops, Prednisolone (as acetate) 1%, or (as so- OTC SIRSINE® (Embassy)
formation and an increased possibility of sec- ophthalmalgia, sensitivity to light, allergic dium phosphate) 0.5%. Eye drops, Tetrahydrozoline HCl 0.05%, Benzalko-
ondary ocular infections due to host-response reaction, dry mouth, eczema. nium chloride 0.02%; in sterile aqueous base.
Advice to patients: Ketotifen can impair the POM Prednisolone (Zeenat)
suppression. Pack: 15 mL (in plastic vial).
Eye drop, Prednisolone acetate 1% w/v
614 | 13.3 Mydriatics and cycloplegics 13.3.2 Sympathomimetics | 615
OTC VISINE® (Bolar) 13.3.1 Antimuscarinics 3 months–1 year (0.1%), 1–5 years instil 1-2 drops (2% or 5%); repeat in
Eye drops, Tetrahydrozoline HCl 0.05%; clear colour- (0.1–0.5%), over 5 years (0.5–1%), 1 5-10 minutes if necessary for 2 or 3
less solution in a dropper container. Short-acting, relatively weak mydriatics, such
as Tropicamide 0.5%, facilitate the examina- drop twice daily for 1–3 days before doses.
Pack: 15 mL. procedure with a further dose given Uveitis, Adult and Child, instil 1-2
tion of the fundus of the eye. Cyclopentolate
1 hour before procedure. Iritis, uveitis, drops (2% or 5%) up to 3-4 hourly.
13.3 Mydriatics and cycloplegics 1% or Atropine are preferable for producing
cycloplegia for refraction in young children. At- by instillation into the eye, ADULT 1 POM Homatropine (EDL 24.5)
13.3.1 Antimuscarinics drop (0.5 or 1%) up to 4 times daily; Eye drops, Homatropine hydrobromide 1%, 2%
ropine 1% as ointment is preferred for children
13.3.2 Sympathomimetics
under 5 years of age. Atropine is also used for CHILD 1 drop (0.5 or 1%) up to 3
Antimuscarinics, by blocking the cholinergic the treatment of iridocyclitis mainly to prevent times daily. TROPICAMIDE
effects of acetylcholine, paralyse the pupillary posterior synechiae, often with phenylephrine POM Atropine (WMF 21.5) Indications: Mydriatic and cycloplegic (with
constrictor muscles causing dilation of the 10% eye-drops. Eye drops, Atropine (as sulfate) 0.1%, 0.5%, 1%. a rapid recovery of accommodation) for
pupil (mydriasis) and paralyse the ciliary mus- POM Atropine (EDL 24.4.2) refraction.
cles resulting in paralysis of accommodation ATROPINE Eye drops, Atropine (as sulfate) 0.1%, 0.5%, 1%. Contra-indications: Narrow angle glaucoma;
(cycloplegia). Mydriasis may precipitate acute Therapeutic category: Mydriatic soft lenses.
angle-closure glaucoma particularly in elderly POM ATROP® (Goben)
Indications: Iritis, uveitis; cycloplegic refrac- Precautions: Unknown I.O.P; in infants put
Eye drops, Atropine sulfate 1%; benzalkonium chlo-
or long-sighted patients. In patients with dark tion procedures; premedication (section 3.2); pressure over lachrymal sac for 1 minute.
ride 0.01% as preservative.
iridic pigmentation, higher concentrations of organophosphate poisoning (section 19.2.3). Pack: 10-mL dropper bottle. Adverse effects: Transient stinging, dry mouth,
mydriatic drugs are usually required and care Contra-indications: Angle-closure glaucoma Note: Discard 4 weeks after opening. blurred vision, photophobia, tachycardia,
should be taken to avoid overdosing. Precautions: May precipitate acute attack of headache, psychotic reactions, behavioural
POM Atropine (Alpha)
Atropine is a long-acting antimuscarinic angle-closure glaucoma, particularly in the Eye drop, Atropine sulfate 1%.
changes.
elderly or long-sighted; risk of systemic effects Advice to patients: See under Homatropine.
EMDEX
used for cycloplegic refraction procedures, Pack: 10 mL
particularly in children. It is also used to with eye drops in infants under 3 months—eye Eye ointment, Atropine 1%. Nursing action:
immobilize the ciliary muscle and iris and to ointment preferred. Pack: 3 g tube. • Teach patient correct method of instillation: wash
SKILLED TASKS: May cause sensitivity to light hands before and after instillation, avoid touching
prevent formation of posterior synechiae in POM Atropine (Embassy) dropper tip to eye, tilt head back, place medication
the treatment of inflammatory eye disorders and blurred vision. Do not carry out skilled Eye drop, Atropine (as sulfate) 1%, benzalkonium in conjunctival sac, and close eyes. Apply light
such as iritis and uveitis. tasks, for example operating machinery or chloride (preservative) 0.02%. finger-pressure on lacrimal sac for 1 minute after
Further clinical notes driving, until vision is clear. Pack: 10 mL instillation.
Antimuscarinics are used to dilate the pupil Adverse effects: Transient stinging and POM Atropine (Rohi) • Reassure patient that blurred vision will decrease
and to paralyse the ciliary muscles in order raised intra-ocular pressure; on prolonged Eye drop, Atropine (as sulfate) 1%. with repeated use of drug; advise him not to
to facilitate surgical procedures. Atropine is administration, local irritation, hyperaemia, Pack: 10 mL x 1’s engage in hazardous tasks such as driving until
the most potent whilst Tropicamide is least oedema and conjunctivitis may occur; contact he can see clearly.
potent. They also vary in their duration of ac- dermatitis; systemic toxicity may occur in the • Advise patient to wear dark sunglasses if photo-
HOMATROPINE
very young and the elderly. phobia occurs.
tion. Whilst tropicamide effects may last for 3 Indications: Mydriatic and cycloplegic for • Wait for 5 minutes before applying other eye drops.
hours, the effect of atropine is seen up to 7 days Advice to patients: Ensure patient knows how refraction, uveitis. Dose: 1-2 drops (1%) at 1-5 minute intervals.
or longer. Cyclopentolate and Homatropine to instil drug; do not allow dropper bottle or Contra-indications: Glaucoma If patient not examined within 30
have intermediate potencies and their effects tube to touch eye or surrounding tissue dur- Adverse effects: Loss of accommodation; minutes, an additional drop shoud
last for up to 24 hours. Sympathomimetics like ing administration; may cause blurred vision, raised intraocular pressure; local irritation on be used.
Phenylephrine are also used as mydiatrics and increased sensitivity to light or eye pain, notify prolonged use.
decongestants. physician if it becomes severe or persists. POM Tropicamide (EDL 24.5)
Advice to patients: Ensure patient knows how
Contact dermatitis is common with the Nursing action: Eye-drops, Tropicamide 0.5%, 1%.
to instil drug; do not allow dropper bottle or
antimuscarinic mydriatic drugs, especially • Finger pressure should be applied to lacrimal sac
tube to touch eye or surrounding tissue dur-
atropine. In addition, toxic systemic reactions for 1-2 minutes after instillation to decrease risk of 13.3.2 Sympathomimetics
absorption and systemic reactions.
ing administration; may cause blurred vision,
to atropine may occur in the very young and increased sensitivity to light or eye pain, notify Phenylephrine is used as a mydriatic/decon-
• Advise patient to use chewing gum if dry mouth
the very old. physician if it becomes severe or persist. gestant in combination with atropine. It is
becomes a problem.
Mydriasis may precipitate acute closed-angle • Advise patient to avoid hazardous activities until Nursing action: contraindicated in glaucoma and may induce
(‘congestive’) glaucoma in a few patients, usu- the visual impairment caused by this drug wears • Teach patient how to instil the drug: wash hands loss of accommodation.
ally aged over 60 years, who are predisposed to off; sunglasses can relieve the discomfort of before and after instillation, avoid touching drop-
the condition because of a small eyeball with photophobia. per tip to eye or sorrounding tissue, tilt head back, PHENYLEPHRINE
a shallow anterior chamber and small diame- • Observe for signs of glaucoma namely increased place medication in conjunctival sac, and close Indications: Mydriatic, decongestant and
ter cornea. A family history is significant and I.O.P., eye pain, headache, progressive blurring of eyes. Apply light finger-pressure on lacrimal sac for
vasoconstrictor.
mydriatics should be avoided in such patients. vision; report to physician. 1-2 minutes following instillation to decrease risk
of absorption and systemic reactions. Contra-indications: Glaucoma, soft contact
Phenylephrine may interact with systematically Dose: Cycloplegic refraction, by instillation
• Advise patient to avoid hazardous tasks such as lense use.
administered monoamine-oxidase inhibitors. into the eye, ADULT 1 drop (1%) twice
driving, until he can see clearly; sunglasses can Adverse effects: Occular effects include
Patients should be warned not to drive for 1 to daily for 1–2 days before procedure
relieve the discomfort of photophobia. transient burning or stinging on instillation,
2 hours after mydriasis. or a single application of 1 drop (1%) • Advise patient to use chewing gum if dry mouth blurred vision, allergic conjunctivitis, photo-
1 hour before procedure; CHILD becomes a problem. phobia; systemic effects include hypertension,
under 3 months (see Precautions), Dose: Cycloplegic refraction, Adult and child, palpitations, tchycardia, trembling, sweating.
616 | 13.4 Drugs used in glaucoma 13.4.1 Miotics | 617
Advice to patients: Ensure patient knows ho condition is chronic open-angle glaucoma miotic, a beta-blocker or a systemic carbonic ing, diarrhoea.
to instil drug; do not touch dropper tip to the (chronic simple glaucoma) in which the in- anhydrase inhibitor in the treatment of chronic Advice to patients: May sting on instillation;
eye; may cause blurred vision, do not drive; tra-ocular pressure increases gradually and the open-angle glaucoma; however, because notify physician of sweating, urinary retention;
may cause photophobia, use sunglasses. condition is usually asymptomatic until well epinephrine is also a mydriatic, it is contrain- usually causes difficulty in dark adaptation;
Nursing action: advanced. In contrast, angle-closure glaucoma dicated for angle-closure glaucoma unless an advice patients to use caution while night
• Teach patient how to instil drug: wash hands before (closed-angle glaucoma) usually occurs as an iridectomy has been carried out. driving or performing hazardous tasks in poor
and after instillation, avoid touching dropper tip to acute emergency resulting from a rapid rise in Acetazolamide, by reducing carbonic anhy- illumination; after topical instillation, finger
eye, tilt head back, place medication in conjunctival intra-ocular pressure; if treatment is delayed, drase in the eye, reduces the production of pressure should be applied to lacrimal sac for
sac, and close eyes Apply light finger-pressure on
chronic angle-closure glaucoma may develop. aqueous humour and so reduces intra-ocular 1-2 minutes to decrease drainage into the nose
lacrimal sac for 1-2 minutes following instillation
to prevent systemic absorption.
In ocular hypertension intra-ocular pressure is pressure. It is used systemically as an adjunct in and throat and minimize possible systemic
• Monitor patient’s B.P. and pulse. raised without signs of optic nerve damage. chronic open-angle glaucoma unresponsive to absorption and reactions.
• Avoid in patients with idiopathic orthostatic hypo- Drugs used in the treatment of glaucoma treatment with topically applied antiglaucoma Dose: Chronic open-angle glaucoma, by
tension; may cause high blood pressure. lower the intra-ocular pressure by a variety of drugs. Prolonged therapy with acetazolamide instillation into the eye, ADULT 1 drop
• Advise patient not to exceed recommended dose mechanisms including reduction in secretion is not normally recommended, but if treatment (2% or 4%) up to 4 times daily. Acute
because systemic effects are common. of aqueous humour by the ciliary body, or is unavoidable blood count and plasma elec- angle-closure glaucoma before surgery,
• May cause blurred vision; warn patient against increasing the outflow of the aqueous hu- trolyte concentration should be monitored. Ac- by instillation into the eye, ADULT 1
driving or operating a machinery until this effect mour by opening of the trabecular network. etazolamide is also used as part of emergency drop (2%) every 10 minutes for 30–60
wears off.
Antiglaucoma drugs used include topical ap- treatment for an acute attack of angle-closure minutes, then 1 drop every 1–3 hours
• May cause photophobia; advise patient to wear
dark sunglasses and to contact physician if con- plication of a beta-blocker (beta-adrenoceptor glaucoma; however it should not be used in until intra-ocular pressure subsides.
dition persists for over 12 hours afer stopping antagonist), a miotic, or a sympathomimetic chronic angleclosure glaucoma as it may mask POM Pilocarpine (WMF 21.4)
the drug. such as epinephrine; systemic administration deterioration of the condition. Eye drops, Pilocarpine (as HCl or nitrate) 2%, 4%.
EMDEX
• Wait for 5 minutes before applying other eye drops. of a carbonic anhydrase inhibitor may be used
POM Pilocarpine (EDL 24.4.2)
Dose: Mydriasis and Vasoconstruction, Adult, as an adjunct. 13.4.1 Miotics
Eye drops, Pilocarpine HCl 1%, 2%, 3%, 4%
instil 1 drop (2.5% or 10%); may Timolol is a non-selective beta-blocker that
repeat in 1 hour if necessary. reduces the secretion of aqueous humour. A PILOCARPINE POM PILO® (Goben)
Child: instil 1 drop (2.5%) as above. beta-blocker is usually the drug of choice for Eye drops, Pilocarpine HCl 1%, 2%, 4%; benzalkonium
Pilocarpine is a representative miotic. Various drugs can chloride 0.02% as preservative.
To relieve eye redness, Adult, instil 1-2 initial and maintenance treatment of chronic serve as alternatives. Pack: 10-mL dropper bottle.
drops (0.12%) up to 4 times daily. open-angle glaucoma. If further reduction
Indications: Chronic open-angle glaucoma, Note: Discard 4 weeks after opening.
Chronic mydriasis, Adult, instil 1 drop in intra-ocular pressure is required a miotic,
(2.5% or 10%) 2-3 times daily. a sympathomimetic or a systemic carbonic ocular hypertension; emergency treatment of POM Pilocarpine (Alpha)
Child: instil 1 drop (2.5%) 2-3 times anhydrase inhibitor may be used with timolol. acute angle-closure glaucoma; to antagonize Eye drops, Pilocarpine HCl 2%, 4%.
daily. In angle-closure glaucoma, timolol should effects of mydriasis and cycloplegia following POM Pilocarpine (Drugfield)
Posterior synechia (adhesion of iris), be used with a miotic and not alone. Since surgery or ophthalmoscopic examination. Eye drops, Pilocarpine HCI 2%, 4% per mL
Adult and child, instil 1 drop (10%) systemic absorption can occur, an ophthalmic Contra-indications: Acute iritis, acute uveitis, Pack: 10 mL (in sterile lupolen bottles)
Mydriasis (without cycloplegia), Adult beta-blocker should not be used in patients anterior uveitis, some forms of secondary glau-
and Child, instil 1 drop (2.5% or 10%) with asthma or a history of obstructive airways coma; acute inflammation of anterior segment; 13.4.2 Beta-blockers
before examination. disease, unless no alternative is available; in not advisable after angle-closure surgery (risk
Note:10% solution should not be used in infants; such cases precautions should be taken to of posterior synechiae). BETAXOLOL
use cautiously in the elderly. guard against bronchospasm. Precautions: Retinal disease, conjunctival or
corneal damage; monitor intraocular pressure See under preparations below for information.
POM Phenylephrine (EDL 24.5) A miotic such as pilocarpine, through its
Eye-drops, Phenylephrine HCl 0.25%, 0.5%, 2.5%, parasympathomimetic action, contracts the in chronic open-angle glaucoma and in long-
POM Betaxolol (Zeenat)
10%. iris sphincter muscle and the ciliary muscle, term treatment; cardiac disease, hypertension, Eye drop, Betaxolol 0.25% w/v
and opens the trabecular network. It is used in asthma, peptic ulceration, urinary-tract ob- Pack: 5 mL
POM Phenylephrine (Alpha)
chronic open-angle glaucoma either alone or, struction, Parkinson disease; stop treatment if
Eye drop, Phenylephrine 10%. POM IVYXOLOL® (Dortemag)
Pack: 10 mL if required, with a beta-blocker, epinephrine symptoms of systemic toxicity develop.
Eye drops, Betaxolol (as HCl) 5 mg per mL.
or a systemic carbonic anhydrase inhibitor. Pi- SKILLED TASKS: Causes difficulty with dark Indications: Ocular hypertension.
locarpine is used with systemic acetazolamide adaptation; may cause accommodation spasm.
13.4 Drugs used in glaucoma Adverse effects: Discomfort, itching, gritty sen-
in an acute attack of angle-closure glaucoma Do not carry out skilled tasks, for example oper- sation, redness of the eye or inside the eyelid,
13.4.1 Miotics ating machinery or driving until vision is clear. inflammation of the cornea, increased tear produc-
prior to surgery; however, it is not advisable
13.4.2 Beta-blockers Adverse effects: Eye pain, blurred vision, tion, sensitivity to light, changes in pupil size and
13.4.3 Sympathomimetics
to use pilocarpine after surgery because of a
risk of posterior synechiae forming. Systemic ciliary spasm, lacrimation, myopia, browache; decreased sensitivity.
13.4.4 Carbonic anhydrase inhibitors Dose: Adult, Instil 1 drop in the affected eye twice
absorption of topically applied pilocarpine can conjunctival vascular congestion, superficial
Glaucoma is normally associated with raised daily.
occur producing muscarinic adverse effects. keratitis, vitreous haemorrhage and increased
intra-ocular pressure and eventual damage to
The sympathomimetic drug epinephrine pupillary block have been reported; lens
the optic nerve which may result in blindness. TIMOLOL
(adrenaline) probably acts by reducing the opacities have occurred following prolonged
The rise in pressure is almost always due to Therapeutic category: Anti-glaucoma (Ocular
rate of production of aqueous humour and use; rarely systemic effects including hyperten-
reduced outflow of aqueous humour, the hypotensive)
increasing the outflow through the trabecular sion, tachycardia, bronchial spasm, pulmonary
inflow remaining constant. The most common Indications: Ocular hypertension; chronic
network. Epinephrine is usually used with a oedema, salivation, sweating, nausea, vomit-
618 | 13.4.3 Sympathomimetics 13.4.4 Carbonic anhydrase inhibitors | 619
open-angle glaucoma, aphakic glaucoma, Eye drop, Timolol (as maleate) 0.5%, benzalkonium Adverse effects: Stinging, blurred vision, pho- Nursing action:
some secondary glaucomas. chloride 0.01% (as preservative). tophobia, eye pain, conjunctival hyperaemia, • Administer orally with food to reduce nausea;
Contra-indications: Uncontrolled heart Pack:10 mL headache or browache; occasionally, conjunc- absorption may be reduced slightly.
failure, bradycardia, heart block; asthma or tival sensitization and local skin reactions; after • Patient may be placed on high potassuim diet.
POM GLAUMOL® (Mark)
• Advise patient to rise slowly from lying down or
history of obstructive airways disease (see Eye drops, Timolol (as maleate) 0.5%. prolonged use conjunctival pigmentation and
sitting position; to avoid hazardous activities if
notes above). Pack: 5 mL x 1’s (in glass bottle). macular oedema in aphakia; systemic adverse drowsiness occurs.
Precautions: Older people (risk of keratitis); if POM IVYTIMOL® (Dortemag) reactions are rare following topical use at • Weigh patient daily as elderly patient is susceptible
used in angle-closure glaucoma, use with a mi- Eye drop, Timolol (as maleate) 5 mg per mL. normal dosage but tachycardia, hypertension, to excess diuresis; weight loss and hypotension
otic, and not alone; interactions: Appendix 1. arrhythmia, dizziness, sweating may occur. should be assessed.
POM JAMOL® (Jubilee)
Adverse effects: Stinging, burning, pain, Dose: Chronic open-angle glaucoma, by • Monitor fluid I&O, electrolytes viz sodium, bicar-
Eye drop, Timolol (as maleate) 0.5% w/v, benzalkonium
itching, erythema, transient dryness, allergic instillation into the eye, ADULT 1 drop bonate and chloride.
chloride 0.01% w/v (as preservative).
blepharitis, transient conjunctivitis, keratitis, Pack: 10-mL plastic vial. (0.5% or 1%) 1–2 times daily. Dose: Chronic open-angle glaucoma, sec-
decreased corneal sensitivity, diplopia, ptosis; ondary glaucoma, by mouth, ADULT
POM LITHIMOLE® (Rohi) POM Epinephrine (WMF 21.4)
systemic effects, particularly on the pulmonary, Eye drops, Epinephrine (as HCl) 2%.
0.25–1 g daily in divided doses.
Eye drop,Timolol maleate 5 mL
cardiovascular and central nervous systems, POM Acetazolamide (WMF 21.4)
Pack: 1 x 5 mL
may follow absorption. 13.4.4 Carbonic anhydrase inhibitors Tablet, Acetazolamide 250 mg.
Advice to patients: Apply gentle pressure to POM NYOLOL®(Novartis)
Eye-drop, Timolol (as maleate) 0.5%. POM Acetazolamide (EDL 24.4.1)
lacrimal sac during and immediately following ACETAZOLAMIDE
Pack: 5 mL (in a dropper bottle). Tablet, Acetazolamide 250 mg.
instillation (1 minute) to avoid systemic absorp-
Gel, Timolol (as maleate) 0.1%; for once daily ap- Therapeutic category: Diuretic; Carbonic Injection, Acetazolamide 500 mg/vial.
tion; stop drug if breathing difficulty occurs. plication. anhydrase inhibitor. POM Apo-Acetazolamide (Lahams)
Nursing action:
Indications: As an adjunct in the treatment
EMDEX
• Teach patient how to instil drug: wash hands before POM TIMITOL® (Standard Generics) Tablet, Acetazolamide 250 mg; white, double scored
and after instillation, avoid touching dropper tip to Eye drop,(0.25%), Timolol (as maleate) 2.5 mg, Ben- of chronic open-angle glaucoma; secondary tab. marked ‘APO 250’.
eye, tilt head back, place medication in conjunctival zalkonium chloride 0.01%; clear colourless soln. glaucoma; as part of pre-operative treatment 250 mg – 100; 500.
sac, and close eyes. Apply light finger-pressure on Pack: 5 mL (in plastic bottle). of acute angleclosure glaucoma. POM ACETOMID® (Hovid)
lacrimal sac for 1 minute following instillation to Eye drop, (0.5%), Timolol (as maleate) 5.0 mg, Benza- Contra-indications: Hypersensitivity to sul- Tablet, Acetazolamide 250 mg
prevent systemic absorption. lkonium 0.01%; clear colourless soln. fonamides; chronic angle-closure glaucoma 250 mg – 500.
• Monitor for systemic effect of beta-blockade even Pack: 5 mL (in plastic bottle). (may mask deterioration); hypokalaemia,
when administering ophthalmic product. POM OCCUMOX® (Salem Gates)
POM TIMODROP® (Onifam) hyponatraemia, hyperchloraemic acidosis;
Dose: Ocular hypertension, chronic open-an- Tablet, Acetazolamide 250 mg; uncoated tab.
Eye drop, Timolol maleate 0.5%. renal impairment (Appendix 4), severe hepatic 250 mg – 10’s (in blisters); 3 x 10’s; 500’s (in jar).
gle glaucoma, aphakic glaucoma, Pack: 5 mL x 25’s impairment.
some secondary glaucomas, by Precautions: Elderly; pregnancy (Appendix 2);
instillation into the eye, ADULT 1 drop
POM TIMOEYE® (Kayhelt) 13.4.5 Prostaglandin analogue
Eye drop, Timolol maleate 0.5%, benzalkonium breastfeeding (Appendix 3); diabetes mellitus;
(0.25% or 0.5%) twice daily. chloride 0.01% per mL pulmonary obstruction; monitor blood count LATANOPROST
POM Timolol (WMF 21.4) Pack:5 mL; 10 mL and electrolytes if used for long periods; inter-
Indications: Reduction of elevated IOP in
Eye drops, Timolol (as maleate) 0.25%, 0.5%; solution. POM Timolol (Alpha) actions: Appendix 1.
patient with open angle glaucoma and ocular
Eye drop, Timolol maleate 0.5%. SKILLED TASKS: May impair ability to perform
POM Timolol (EDL 24.4.2) hypertension.
Eye-drops, Timolol maleate 0.25%, 0.5%. Pack: 5 mL skilled tasks, for example operating machinery,
Contra-indications: Known hypersensitivity to
driving.
POM Apo-Timop (Lahams) POM Timolol (Hovid) latanoprost or benzalkonium chloride.
Adverse effects: Nausea, vomiting, diarrhoea,
Eye drop, Timolol maleate 0.25%; clear, colourless Eye-drops, Timolol maleate 0.25%, 0.5%; clear, Precautions: Prostanglandin analogues may
colourless liquid. taste disturbance; loss of appetite, paraes-
to light yellow, sterile isotonic buffered aqueous gradually change eye colour by increasing the
Pack: 5 mL. thesia, flushing, headache, dizziness, fatigue,
opthlamic solution. amount of brown pigment in the iris; monitor
Pack: 5 mL. irritability, depression; thirst, polyuria; reduced
patient. Pregnancy and breastfeeding.
13.4.3 Sympathomimetics libido; metabolic acidosis and electrolyte dis-
POM DRUMOPTOL® (Drugfield) Adverse effects: Major side effects include
turbances on long-term therapy; occasionally
Eye drops, Timolol maleate 0.5%; clear, colourless blurred vision, increased pigmentation of iris,
EPINEPHRINE drowsiness, confusion, hearing disturbances,
to light yellow conjunctival hyperaemia & punctuate epithe-
Pack: 5 mL (in white plastic bottle with lip and
urticaria, melaena, glycosuria, haematuria,
Epinephrine is a complementary drug for use when lial erosions. Mild to moderate conjunctival or
white cap) abnormal liver function, renal calculi, blood
drugs in the main list cannot be made available. episcleral hyperaemia may occur during topical
disorders including agranulocytosis and throm-
POM EMBAROL® (Embassy) treatment and photophobia. Rarely (<1%)
Synonym: Adrenaline bocytopenia, rashes including Stevens-John-
Eye drops, Timolol maleate 0.25%, 0.5%. conjunctivitis, diplopia & eye discharge have
Indications: Chronic open-angle glaucoma, son syndrome and toxic epidermal necrolysis;
0.25% – 5 mL. been reported. Most common systemic events
0.5% – 5 mL. ocular hypertension; anaphylaxis (section 8.3); transient myopia reported.
include upper respiratory tract infections,
cardiac arrest (section 5.4). Advice to patients: May take with food; report
POM EMOPTOL® (Zolon) cold & flu, pain in muscle, joints, back, chest &
Contra-indications: Angle-closure glaucoma, numbness or tingling of extremities to physi-
Eye drops, Timolol (as maleate) 0.25%, 0.5%, benza- angina pectoris.
unless an iridectomy has been carried out. cian; ability to perform tasks requiring mental
lkonium chloride (as preservative) 0.01% Dose: Instil 1 drop (1.5 µg) once daily pref-
Precautions: Hypertension, heart disease, aneu- alertness and/or physical co-ordination may be
Pack: 5 mL erably in the evening, which should
rysm, arrhythmia, tachycardia, hyperthyroidism, impaired; drug may cause substantial increase
POM EYEMOLOL® (Al-Tinez) not be exceeded. Reduction of IOP
cerebral arteriosclerosis, diabetes mellitus. in blood glucose in some diabetic patients.
starts 3-4 hours after administration;
620 | 13.5 Local anaesthetics 13.6 Miscellaneous eye preparations | 621
pressure reduction is maintained for rarely, allergic reactions may occur. Adverse effects: Occasionally, mild or mod- Also for prophylaxis and reduction of post-op-
at least 24 hours. Advice to patients: May cause transient burn- erate, transient stinging and /or blurred erative ocular inflammation.
Note: Can be used concomitantly with other ing or stinging of eyes upon instillation; do not vision directly after application of eye drops. Contra-indications: Hypersensitivity to any of
products to be used 5 minutes apart. Store in the touch or rub eye until anaesthesia has worn off. Rarely, hypersensitivity reaction in the form the ingredients in the formulation.
fridge. Vial in use should be discarded 6 weeks Dose: Local anaesthesia, by instillation into the of itching, reddening, and photosensitivity; Adverse effects: Transient stinging and burn-
after opening.
eye, ADULT and CHILD 1 drop. Kertitis punctata. ing on instillation, corneal edema, iritis, ocular
POM DRULATAN® (Drugfield)
POM Tetracaine (WMF 21.3)
Dose: Adults, Preoperative, up to 5 x 1 drop in irritation, allergic reactions, superficial ocular
Eye drop, Latanoprost 50 µg per mL; clear, isotonic, the 3 hours preceding surgery. infections and superficial keratitis.
Eye drops, Tetracaine (as HCl) 0.5%; solution.
buffered, preserved solution. Postoperative, 3 x 1 drop immediately Dose: Adult, Ocular itching due to seasonal
Pack: 2.5 mL POM Tetracaine (EDL 24.3) after surgery, thereafter 3-5 x 1 drop allergic conjunctivitis, Instil 1 drop into
Eye drops, Tetracaine HCl 0.5%.
POM LAXAT® (A-tinez). daily for as long as required. the affected eye(s) 4 times daily.
Note: Not for use in preterm neonates.
Eye drop, Latanoprost 0.05 mg, 10% benzalkonium Other indications, 4-5 x 1 drop daily, Post-operative ocular inflammation,
chloride solution 2 mg as preservative. depending on the severity of the Instil 1 drop into the affected eye(s) 4
Pack:2.5 mL 13.6 Miscellaneous eye preparations
condition. times daily beginning 24 hours after
POM Latanoprost (Alpha) A variety of other agents are applied for local the surgery and continuing through
POM DICLOEYE® (Kayhelt)
Eye drops, Latanoprost 2.5 mL per 5 mL or systemic effects. the first 2 weeks of the post-operative
Eye drop, Diclofenac sodium 0.1%, phenylmercuric
Pack: 1 x 2.5 mL; 3 x 2.5 mL Chymotrypsin is a zonulolytic which is useful nitrate (as preservative) 0.001% period.
POM PROSTAN® (Korlyns) in intracapsular cataract extraction. Pack: 5 mL POM TOROLAC® (Micronova)
Eye drops, Latanoprost 50 µg per mL, with 50 µg Hyaluronidase is used to promote resorption POM Diclofenac (Zeenat) Eye drop, Ketorolac tromethamine 0.5% w/v, Benza-
benzalkonium chloride as preservative. of excess fluids and extravasated blood in the Eye drop, Diclofenac sodium 0.1% w/v. lkonium chloride 0.02% w/v.
Pack: 5-mL bottle. Pack: 5 mL Pack: 5 mL.
tissue during ocular surgery.
EMDEX
POM XALATAN® POM DICLOLAB® (Embassy)
Methylcellulose, an emollient, is used for tear FLURBIPROFEN
Drops, Latanoprost 50 µg per mL, with 50 µg benza- Eye/Ear drops, Diclofenac sodium 0.1% w/v, Sorbic
lkonium chloride as preservative.
deficiencies.
acid 0.2% w/v. See under the preparations below for information.
Pack: 5-mL bottle. Zinc Sulfate, a traditional astringent, is used Pack: 10 mL.
+ Timolol in eye–drops for treatment of excessive POM IVYFLUR® (Dortemag)
POM EYETAREN® (Al-Tinez)
lachrymation. It should not be combined with Eye drops, Flurbiprofen sodium 0.3 mg per mL.
POM LAXAT® Plus (Al-Tinez) Ophthalmic solution, Diclofenac sodium 1 mg per mL
epinephrine eye drops because of the risk in Pack: 5 mL
Indications: Inhibition of intra-operative miosis
Eye drop, Latanoprost 50 µg, timolol maleate 6.83
using epinephrine in patients predisposed to during eye surgery and to control post-operative
mg, benzalkonium chloride 0.2 mg as preservative. POM I-GESIC® (Al-Tinez) inflammation of the anterior segment of the eye.
Pack: 2.5 mL closed–angle glaucoma.
Eye drop, Diclofenac sodium 0.1%, sorbic acid 0.2% Adverse effects: Mild irritation or grittiness of the
DICLOFENAC (as preservative) eye or visual disturbances; increased bleeding from
13.5 Local anaesthetics Pack: 5 mL ocular surgery; wound healing may be delayed.
Therapeutic category: Non-steroidal anti-in- Dose: Intraoperative miosis, Instil 1 drop beginning
Topical local anaesthetics are employed for flammatory drug (NSAID). POM VOLTAREN OPHTHA® (Oculus)
2 hours prior to surgery and repeated at
simple ophthalmological procedures and Pharmacology: Diclofenac sodium is a Eye-drops, Diclofenac sodium 1 mg per mL
30 minute intervals for a total of 4 drops
for short operative procedures involving the non-steroidal drug with anti-inflammatory
Pack: 5 mL (in a dropper bottle).
per eye.
cornea and conjunctiva. Tetracaine, available and analgestic effects. It acts by inhibitions of POM MEDICLEYE® (Neros) To control post-operative inflammation, the
in 0.5% ophthalmic solution, provides a rapid prostaglandin synthesis. It has an anti-inflam- Eye drops, Diclofenac sodium 0.1%. same dosage regimen as above is used prior
local anaesthesia which lasts for 15 minutes matory effect when given after surgery or Pack: 5 mI bottle. to ocular surgery followed 24 hours after
or more. Prolonged or unsupervized use of trauma to the eye and in other non-infectious
surgery by the instillation of 1 drop 4 times
+ Gentamicin
tetracaine is not recommended. a day for 1-3 weeks.
inflammatory conditions. Prophylactic admin- POM DICLOGENTA® (Al-Tinez)
istration of diclofenac in patients undergoing Eye drop, Diclofenac sodium 1 mg, gentamicin sul- METHYLCELLULOSE
TETRACAINE
cataract removal and intraocular lens implan- phate 3 mg, benzalkonium chloride 0.01% per mL
tation reduces the frequency and severity Indications: An emolient used for tear defi-
Tetracaine is a representative ophthalmic local anaes- Pack: 5 mL
thetic. Various drugs can serve as alternatives. of intra-operative miosis and post-operative ciencies.
Contra-indications: Soft lenses.
Synonym: Amethocaine cystoid macular oedema. KETOROLAC
Indications: Inhibition of miosis during cat- Dose: See lit.
Indications: Short-acting local anaesthesia of Therapeutic category: Non-steroidal anti-in-
cornea and conjunctiva. aract surgery. Postoperative inflammation flammatory drug (NSAID). POM Methylcellulose (EDL 24.7)
after cataract surgery and other surgical Pharamacology: Ketorolac tromethamine is a Eye-drops, Methylcellulose 1%, 2%.
Contra-indications: Hypersensitivity to es-
ter-type local anaesthetics; eye inflammation procedures. Prevention of cystoid macular NSAID with analgesic, antipyretic and anti-in-
oedema associated with lens extraction and POTASSIUM IODIDE plus SODIUM IODIDE
or infection. flammatory activity. It inhibits the cyclo-oxy-
Precautions: Avoid prolonged use (cause of se- intraocular lens implantation. Non-infectious genase enzyme essential for the biosynthesis Therapeutic category: Anti-cataractogenic.
vere keratitis, permanent corneal opacification, inflammatory conditions affecting the anterior of prostaglandins. It has been shown to reduce Pharmacology: Iodides can activate the me-
scarring, delayed corneal healing); protect eye segment of the eye (e.g. chronic non-infectious prostaglandin levels in the aqueous humour tabolism and occasionally counteract cloud-
from dust and bacterial contamination until conjunctivitis). Post-traumatic inflammation after topical ophthalmic administration. iness of the vitreous body. Potassium iodide
sensation fully restored. in penetrating and non-penetrating wounds Indications: For the temporary relief of ocular diffuses rapidly into the vitreous humour after
Adverse effects: Burning, stinging, redness; (as an adjuvant to local anti-infective therapy). itching due to seasonal allergic conjunctivitis. local administration.
622 | 13.6 Miscellaneous eye preparations
Indications: Opacity of and bleeding in the vit- POM VITREOLENT® (Oculus)
reous body of any cause ( age, myopia, hyper- Eye-drops, Potassium iodide 3 mg, sodium iodide
tension, diabetes, periphlebitis etc.). Clouding 3 mg per mL.
of the lens as the first sign of senile cataract. Pack: 10 mL (in a dropper bottle).
Contra-indications: Known hypersensitivity
ZINC SULFATE
to iodine (iodism) or other components of
the formulation. Functional disturbances of See under the preparations below for information.
the thyroid.
Precautions: Gently compress the lacrimal POM IVYZINC® (Dortemag)
sac with the index finger for 1-2 mins after Eye drops, Zinc sulfate 2.5 mg per mL.
instillation to minimize systemic absoprtion. Therapeutic category: Astringent; Antiseptic.
Indications: Minor eye irritations. It works by re-
Pregnancy and lactation.
ducing the production of secretions in the eye and
Adverse effects: Slight and transient burning helping to prevent infections.
or pricking sensation. Occasionally, increased Adverse effects: Mild stinging sensation in the eyes.
tear flow. Hyperthyroidism and acne-type Dose: Adult and Child, Instil 1-2 drops in each af-
effects may occur. fected eye up to 3 or 4 times a day.
Dose: Instil one drop into the conjunctival
sac 1-3 times a day. ARTIFICIAL TEARS
Note: Gently compress the lacrimal sac with the
index finger for 1-2 mins after instillation to minimize OTC HypoTears® (Occulus)
systemic absorption. Eye drop, Polyvinyl alcohol 1%, Polyethylene glycol
400 1%.
POM CATAREST® (Al-Tinez) Pack: 5 mL.
Eye drop, Potassium iodide 3.3%, sodium chloride Indications: For temporary relief of burning and
0.83%, calcium chloride 1.0%, phenylmercuric irritation due to dryness of the eye or to exposure
nitrate 0.001% (as preservative) to wind or sun; also help to protect against further
Pack: 10 mL
EMDEX
eye irritation.
POM EYETREOLENT® (Al-Tinez) Dose: Instill 1-2 drops into the affected eye(s) as
Eye drop, Potassium iodide (2.29 mg as iodide) 3 needed. Patients who wear contact lenses
mg, sodium iodide (2.54 mg as iodide) 3 mg per mL; should be advised to remove them before
colourless and transparent solution. administration. After 15 minutes, the lenses
Pack: 10 mL can be reinserted.
POM PHARMALENT® (Pharmabox) POM Hypromellose (Alpha)

Eye drops, Potassium iodide (2.29 mg as iodide) 3 mg, Eye drop, Hypromellose 0.3%.
sodium iodide (2.54 mg as iodide) 3 mg; colourless Pack: 10 mL
and transparent solution. POM IVYMOICELL® (Dortemag)
Pack: 10 mL. Eye drops, Hydroxypropyl methylcellulose 7 mg
POM VISTULENT® (Drugfield) per mL
Eye drops, Potassium iodide 3 mg, sodium iodide Indications: To replace natural tears and help
3 mg per mL lubricate dry eyes.
Pack: 10 mL in white sterile lupolen bottles. Dose: Adult and child, Instil 2 drops in the affected
eye every 3 hours.
14. Ear, nose and throat
(ENT) drugs
14.1 Ear drugs . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 624
14.1.1 Anti-infective and/or Anti-inflammatory drugs. . . . . . . . . . . . . . . . . . . . . . . . . . 624
14.1.2 Preparations for the removal of ear wax . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 626
14.2 Nasal drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 626
14.2.1 Intranasal corticosteroids (INCS). . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 626
14.2.2 Intranasal decongestants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 627
14.2.3 Systemic nasal decongestants . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 628
14.2.4 Preparations for the cauterisation of nose . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 632
14.3 Throat drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 632
EMDEX
624 | 14.1 Ear drugs 14.1.1 Anti-infective and/or Anti-inflammatory drugs | 625
14.1 Ear drugs the affected ear uppermost for 5 to 10 minutes Pack: 10 mL reduce frequency. The drops can be
after a generous amount of the solution has POM ELISCA® (Medreich) applied by placing a napkin soaked
14.1.1 Anti-infective and/or Anti-inflammatory drugs
14.1.2 Preparations for the removal of ear wax been introduced into the ear. Ear drop, Chloramphenicol 5%. in the solution to the ear for 12-24
Pack: 10 mL bottle hours; reduce dose when controlled.
Drugs are applied locally as drops or ointment, 14.1.1 Anti-infective and/or Anti- Dose: Adult (including the elderly) and Child, 1-2
into the ear for the treatment of ear infections POM BIVACYN-N® (Taylek)
inflammatory drugs drops applied topically to each affected Eye / Ear drops, Dexamethasone 1 mg, neomycin
and to remove excess ear wax. The major disor- ear up to 6 times daily or more frequently
Chloramphenicol ear drugs contain propylene sulfate 3500 I.U. per mL.; in 5 mL vials
ders of the ear are otitis externa, an eczematous if required. Pack: 5 mL.
reaction of the meatal skin, and otitis media glycol and cause sensitivity in about 10% of
patients. An eye ointment of chloramphenicol POM RICHPHENICOL® (GoldMoore) Eye/Ear ointment, Dexamethasone 0.5 mg, neomycin
which is the commonest cause of severe pain in Ear drop, Chloramphenicol BP 5% w/v, Phenylmer- sulfate 3500 I.U. per g.
small children and recurrent attacks especially may be used. It is primarily indicated for bacte-
curic Nitrate BP 0.002% (as preservative). Pack: 3 g; 5 g (in tubes).
in infants, are particularly distressing. rial infection of the external ear. Framycetin and
Pack: 10 mL bottle.
Gentamicin are the other widely-used anti-in- HYDROCORTISONE plus NEOMYCIN
For otitis externa, one must exclude an under- fectives for bacterial infections of the external + Dexamethasone
lying chronic otitis media before treatment is Indications: Inflammation and infection of the
ear. However, when otitis externa is treated POM OTIFAR® (Neros)
started. Many cases recover after thorough external auditory canal, seborrheic dermatitis,
topically with preparations containing amino- Ear drop, Chloramphenicol 80 mg, Dexame-thasone
cleansing of the meatus by suction, dry mop- infected eczematoid dermatitis.
glycosides or polymyxins in patients who have acetate 4 mg; in 8 mL bottle.
ping or gentle syringing. For resistant cases, it is Pack: 8 mL x 1’s (in bottle). Contra-indications: Perforated ear drum,
a perforation of the tympanic membrane, there
effective to introduce a ribbon gauze dressing Indications: Otitis externa, purulent otitis exterma, fungal or viral infections, tuberculosis.
is an increased risk of drug-induced deafness.
soaked in an astringent such as aluminum otorrhea, tinnitus, ear eczema. Precautions: Extensive or prolonged use in
acetate, or anti-inflammatory corticosteroid Solutions containing an anti-infective and a Dose: Adult: Instill 1-5 drops into the affected ear, 2 pregnancy or infants.
solution. When this is not possible, the ear corticosteroid (such as Gentisone HC) are used times daily for 6 to 10 days. Adverse effects: Superinfection, sensitisation.
EMDEX
should be gently cleared with a probe covered for treating cases where infection is present Child: Instill 1-2 drops into the affected Nursing action: See under Chloramphenicol.
with inflammation and eczema. ear, 2 times daily according to age, for 6 Dose: Instil 2-3 drops into the affected ear
in cotton wool and the patient encouraged
to 10 days.
to lie with the affected ear uppermost for ten every 1-4 hours according to the
CHLORAMPHENICOL severity of the case; after the inflam-
minutes after the canal has been filled with a GENTAMICIN
liberal quantity of the appropriate solution. Indications: Bacterial infection of the external mation has subsided, the dosage may
ear Indications: Bacterial infection of the external be gradually reduced to 1-2 drops 3-4
If infection is present, a topical anti-infective
Precautions: Avoid prolonged use as it may in- ear times daily.
which is not used systemically (such as framy-
crease chances of sensitisation and emergence Adverse effects: Hypersensitivity.
cetin, neomycin or clioquinol) may be used for POM Hydrocortisone plus Neomycin (EDL 19.1.3)
of resistant organisms Nursing action: See under Chloramphenicol.
only about a week as excessive use may result Ear drops, Hydrocortisone acetate 1.5%, neomycin
Adverse effects: Sensitivity reactions such as Dose: Apply 2–3 drops, 2–3 times daily.
in fungal infections. Sensitivity to the anti-in- sulfate 0.5%.
fective or solvent may occur and resistance to transient irritation, burning, stinging, itching POM Gentamicin (EDL 19.1.1)
and dermatitis, may occur. See section 13.2 for the proprietory preparations
antibacterial is a possibility with prolonged use. Ear drops, Gentamicin sulfate 0.3%
Nursing action: See section 13.1 for the proprietory preparations
For acute otitis media local treatment is ineffec- • Teach patient how to instil ear drops correctly HYDROCORTISONE plus
tive and there is no place for drops containing without touching dropper to the ear. NEOMYCIN plus POLYMYXIN B
a local anaesthetic. Many attacks are viral in • Remove impacted cerumen by irrigation; clean BETAMETHASONE Indications: Bacterial infection with inflamma-
origin and require only treatment with simple stopper with methylated spirit; restrain child if Indications: Atopic/eczematous inflammation tion of the ear, e.g. otitis externa.
analgesics for pain. Severe attacks of bacterial necessary; warm solution to body temperature; Nursing action: See under Chloramphenicol.
of the external ear.
origin should be treated with systemic antibi- drop drug into the ears.
Contra-indications: Perforated ear drum Dose: Apply 2-3 drops every 8 hours.
otics. Identification of the infecting organism • Inform patient that dizziness may occur after
instilling drug. Dose: Apply 2-3 drops, every 2-3 hours. POM OTOSPORIN® (SKG)
by bacterial examination of the discharge, if
• Monitor the ears for pain, redness, swelling and POM Betamethasone (EDL 19.1.2) Ear drops, Hydrocortisone acetate 10 mg, neomycin
present, is helpful in selecting the appropriate fever. sulfate 3,400 units, polymyxin B sulfate 10,000 units
treatment. In recurrent acute otitis media a Ear drops, Betamethasone sodium phosphate 0.1%.
Dose: Apply 2-3 drops, 2-3 times daily. per 10 mL.
daily dose of a prophylactic antibiotic (co-tri- See section 13.2 for the proprietory preparations
POM Chloramphenicol (EDL 19.1.1) + Fludrocortisone
moxazole or erythromycin) during the cold
season can be tried. Ear drops, Chloramphenicol 5%. POM OTO-MED® (Afrab-Chem)
DEXAMETHASONE plus NEOMYCIN
POM AURICHLOR® (Standard Generics) Ear drops, Fludrocortisone acetate 0.1%, Neomycin
For chronic otitis media, thorough cleansing Therapeutic category: Anti-inflammatory/
Ear drops, Chloramphenicol 1%, 5%. sulfate 0.44%, Polymyxin B sulfate 0.12%, Lidocaine
with an aural suction tube may completely Antiallergic/Antibiotic. HCl 4.0%.
Pack: 10 mL.
control infection. However, acute exacerba- Indications: Diseases of the external ear such Pack: 8 mL.
tions of chronic infection may require systemic POM CHLOMACOL® (Geneith) as seborrhoeic dermatitis, eczema. Dose: Apply 4-5 drops 2-4 times daily depending
antibiotics. Ear drops, Chloramphenicol 5%. on the seriousness and patient’s response.
Contra-indications: Perforated ear drum,
Pack: 10 mL.
Ear wax may be readily removed by syringing untreated infection.
with warm water. If necessary, wax can be sof- POM CHLORAF® (Afrab-Chem) Precautions: Avoid prolonged use OFLOXACIN
tened before syringing with topical solutions, Eardrops, Chloramphenicol 5%; in a bottle of 10 mL Adverse effects: Local sensitivity reactions.
solution with dropper. See under the preparations below.
the most effective of which is sodium bicarbo- Dose: Clean and dry the ear canal carefully.
nate ear-drops. Other simple remedies are olive POM Chloramphenicol (Al-Tinez) Apply the ointment as a thin layer POM EMPROFLOX® (Zolon)
oil and almond oil. The patient should lie with Ear drop, Chloramphenicol 5.0% per mL 2-3 times daily until controlled then Eye/Ear drops, Ofloxacin 0.3%, benzalkonium (as
626 | 14.1.2 Preparations for the removal of ear wax 14.2.2 Intranasal decongestants | 627
preservative) 0.01% used for this purpose are oxymetazoline, xylo- puffs (100 mcg) into each nostril the intranasal route only.
Pack: 5 mL; 10 mL (in FFS plastic vial) metazoline, tetrahydrozoline, antazoline and twice daily or 1 puff (50 mcg) 3-4 For the prophylaxis and treatment of
POM Ofloxacin Ear Drop (Neros) phenylephrine. They cause vasoconstriction times daily; max. 8 puffs daily. seasonal allergic rhinitis and perennial
Ear drop, Ofloxacin 0.3%. of the mucosal blood vessels which in turn POM Beclometasone (EDL 19.2.1.3)
rhinitis: Adults and children (>12
Pack: 5 mI bottle. reduces the thickness of the nasal mucosa. Nasal spray, Beclometasone dipropionate 50 mcg years): 2 sprays into each nostril once
Indications: Otitis externa, acute otitis media, The major problem with their use is that they per metered spray. a day, preferably in the morning; may
purulent otitis media due to several different mi- often give rise to a rebound phenomena as increase upto max. 2 sprays into each
croorganisms. POM BECONASE® (GSK)
their effects wear off due to a secondary vas- nostril twice daily if required.
Contra-indications: Hypersensitivity to ofloxacin Nasal spray, Beclometasone dipropionate 50
odilation with a subsequent increase in nasal mcg per dose; metered-dose aerosol with nasal Children (4-11 years): 1 spray into
or any derivative quinolones. Children under 1 year
old, pregnant women and nursing mothers. Do not
congestion. Ephedrine nasal drops is perhaps applicator. each nostril once a day, preferably in
instil into the eye. the safest, giving relief for several hours. Oxym- Pack: 200 dose unit. the morning; may incerease to max.
Dose: Instil 2-3 drops into the affected ear, 2 to 3 etazoline, phenylephrine and xylometazoline 1 spray into each nostril twice daily if
times daily. are more potent and more likely to cause a FLUTICASONE required.
rebound effect. All of these preparations may Therapeutic category: Corticosteroid. Elderly: normal adult dose.
POM OFLOXALAB® (Embassy)
Eye/Ear drop, Ofloxacin 3 mg per mL. cause a hypertensive crisis if used during treat- Indications: Prophylaxis and treatment of POM FLIXONASE® (GSK)
Pack: 10 mL. ment with a monoamine-oxidase inhibitor. seasonal allergic rhinitis including hay fever, Nasal spray, Fluticasone proprionate; aqueous
and perennial rhinitis. nasal spray.
14.1.2 Preparations for the 14.2.1 Intranasal corticosteroids (INCS) Contra-indications: Hypersensitivity to any
removal of ear wax of its ingredients. 14.2.2 Intranasal decongestants
BECLOMETASONE Precautions: Local infection of the nasal air-
Various formulations contain organic solvents
Therapeutic category: Corticosteroid. ways; patient on systemic steroid particularly if XYLOMETAZOLINE
EMDEX
and these can cause irritation of the meatal
Pharmacology: Beclometasone dipropionate there is impaired adrenal function; full benefit Therapeutic category: Vasoconstrictor for
skin. Glycerol plus sodium bicarbonate ear
has a potent anti-inflammatory effect within may take several days of regular use. nasal decongestion.
drops does not cause this kind of irritation
the respiratory tract at doses which are not Interactions: Ritonavir (a highly potent cy- Pharmacology: It acts by stimulatindg the
and is as effective for the removal of ear wax.
systemically active. tochrome P450 3A4 inhibitor) can interact with alpha-adrenergic receptors in the arterioles
GLYCEROL plus SODIUM BICARBONATE Indications: Prophylaxis and treatment of per- intranasal or inhaled fluticasone propionate, of the nasal mucosa causing vasoconstriction.
ennial and seasonal allergic rhinitis including resulting in increased systemic corticosteroid Onset of action is about 5-10 minutes and lasts
Indications: To soften ear wax before removal.
hay fever and vasomotor rhinitis. effects including Cushing’s syndrome and for about 5-6 hours.
Dose: Apply sufficient drops into the affected
Precautions: Nasal infections should be appro- adrenal suppression; concomitant use should Indications: Colds of various types; to aid
ear for 3 consecutive nights.
priately treated, patients on systemic steroid be avoided, unless the potential benefit to drainage of secretions in affections of the para-
POM Glycerol plus Sodium Bicarbonate (EDL treatment, pregnancy. the patient outweighs the risk of systemic nasal sinuses; as an adjuvant in otitis media; to
19.1.4) Adverse effects: Sneezing and very rarely, corticosteroid side-effects. Other inhibitors facilitate rhinoscopy.
Ear drops, Glycerol 30 mL, Sodium bicarbonate 5 g septal perforation. of cytochrome P450 3A4 produce negligible Contra-indications: Status post hypophysec-
in 100 mL solution.
Nursing action: (erythromycin) and minor (ketoconazole) tomy or after surgical interventions in which
• Ensure patient understands how to use medica- increases in systemic exposure to fluticasone the dura mater has been exposed. Narrow-an-
14.2 Nasal drugs tion: shake container and invert; blow the nose to propionate but care is advised when co-ad- gle glaucoma.
14.2.1 Intranasal corticosteroids (INCS) clear nasal passages.
ministering potent cytochrome P450 3A4 Precautions: Hypersensitivity to sympatho-
14.2.2 Intranasal decongestants • Tilt head slightly forward (to prevent the spray
running down the back of the throat) and insert
inhibitors and fluticasone. mimetics, prolonged use e.g. in chronic colds.
14.2.3 Systemic nasal decongestants Adverse effects: Immune system disorders: Very Advice to patients: Do not exceed recom-
14.2.4 Preparations for the cauterisation of nose the nozzle into nostril, pointing it away from the
septum – use right hand to spray the left nostril rarely, Hypersensitivity reactions, anaphylaxis/ mended dose; do not use for more than 3
Nasal drugs are formulated as drops or sprays and left hand to spray the right nostril. Close the anaphylactic reactions, bronchospasm, skin consecutive days as it may cause rebound
for the treatment of inflammatory nasal disor- other nostril with finger. rash, oedema of the face or tongue. congestion.
ders. Nasal allergy is controlled by oral antihis- • Press down on the nozzle once while breathing in Nervous system disorders: Commonly Head- Adverse effects: Occasionally burning sen-
tamines and systemic nasal decongestants. gently through the nose and keeping the mouth ache, unpleasant taste, unpleasant smell. As sation in the nose and throat; local irritation,
Severe attacks are relieved by topical prepa- closed. Breath out through the mouth. with other nasal sprays, unpleasant taste and nausea, headache, dryness of the nasal mu-
rations of corticosteroids with no significant • Shake container again and repeat in the other
smell and headache have been reported. cosa. Overuse may cause rebound congestion.
nostril.
side-effects. Very disabling symptoms may Eye disorders: Very rarely Glaucoma, raised Dose: Adult and children over 7 years of age,
• Advise patient to continue with the drug even in
justify the use of systemic corticosteroids for the presence of mild nasal bleeding (this is only intraocular pressure, cataract. 2-3 drops of 0.1% solution into each
short periods. They may also be used at the transient). Respiratory, thoracic and mediastinal disorders: nostril every 8-10 hours; not exceed-
beginning of a course of treatment with a • Explain to patient that therapeutic effect is not Very commonly epistaxis. Common is Nasal ing 3 doses per day.
corticosteroid spray to relieve severe mucosal immediate unlike nasal decongestants. dryness, nasal irritation, throat dryness, throat Infants and children up to 6 years of
oedema and allow the spray to penetrate the • Instruct patient to notify the doctor if there is no irritation. As with other intranasal products, age, 1-2 drops of 0.05% solution into
nasal cavity. Decongestant nasal drops and improvement in symptoms within 3 weeks or if dryness and irritation of the nose and throat, each nostril every 8-10 hours, up to a
sprays are used for the symptomatic relief of nasal irritation persists. and epistaxis have been reported. Very rarely, max. 3 doses/day.
• Observe for fungal infections.
nasal congestion which may accompany vas- nasal septal perforation. Note: Blow the nostrils. Tilt head slightly forward
• Do not refrigerate. Discard the spray after 3 months
omotor rhinitis, nasal polypi and the common of first opening. Dose: Advice patient full benefit may take (to prevent the spray running down the back of the
cold. The commonest sympathomimetic drugs 3-4 days of regular use. To be used by throat); spray 1 or 2 times into each nostril. Breath
Dose: Adult and Children over 6 years, 2 deeply. Repeat as needed q8-10 hrs.
628 | 14.2.3 Systemic nasal decongestants 14.2.3 Systemic nasal decongestants | 629
OTC CLARINEZ® (Shalina) Oily solution, Levomenth 4.1%, Juniperberry oil 2.7%, function impairment; pregnancy. allergic rhinitis. Also used for urticaria and emer-
Nasal drops (Paediatric), Xylometazoline HCI 0.05%, Wintergreen oil 3.7%, Eucalyptus oil 35.45%, Cajuput Interactions: TCAs and other CNS depressants, gency treatment of anaphylactic reactions.
Domiphen bromide 0.011%, Thiomersal 0.0024%. oil 18.5%, Clove oil 0.1%, Dementholised mint oil MAOIs, general anaesthetics, other sympa- Dose: Doses to be taken 3 times daily.
Pack: 10 mL. 35.45%; liquid in amber bottle. thominetics and hepatic enzyme– inducing Child (1-2 yrs): 2.5 mL; 2-5 yrs, 5 mL; 6-12
Nasal drops (Adult), Xylometazoline HCI 0.1%, Domi- yrs, 10 mL.
OTC PENETROL® (BCN) agents.
phen bromide 0.011%, Thiomersal 0.0024%.
Inhalant, Menthol 17.5%, cajuput oil 2.5%, lavender Adverse effects: Drowsiness; dryness of OTC OFF-COLD® (Sofak)
Pack: 10 mL.
oil 8%, eucalyptus oil 7.5%, peppermint oil 0.2%. mouth, nose and throat; GI disturbances. Syrup, Paracetamol 120 mg, ascorbic acid 25 mg,
OTC ENAPHRIN® (Afrab-Chem) Pack: 20 mL. Dose: By mouth, Adult, 2 tabs 3-4 times daily. chlorpheniramine maleate 2 mg per 5 mL
Nasal drops, Xylometazoline HCl 0.05%, 0.1%; almost Indications: For the relief of catarrh, hay fever, nasal Pack: 100 mL
Child (>6 years), 1 tab 3-4 times daily;
odourless, slight menthol odour. congestion. Dose: 1 – 2 years: 2-5 mL; 2-5 years: 5mL,6-12 years:
Pack: 10 mL. Precautions: Asphyxiation in young children, spasm
do not exceed 50 mg Phenylpropan- 10 mL (three times daily).
Pack: 10 mL. of the glottis. olamine daily.
Paracetamol + Chlorpheniramine
Adverse effects: Hypersensitivity reactions includ- OTC PARCLORPHEN® (Hovid)
OTC OTRIVIN® (Novartis) + Phenylephrine
ing contact dermatitis. Tablet, Phenypropanolamine HCl 12.5 mg, chlorphe-
Nasal drops, Xylometazoline HCI 0.1%.
Dose: Sprinkle a few drops on your handkerchief niramine maleate 2 mg, paracetamol 300 mg; f-c tab. OTC ANTYCOLD® (Hochiez)
Pack: 10 mL
and inhale the vapour. Pack: 100; 1000. Tablet, Paracetamol 500 mg, caffeine 30 mg, phenyle-
Paediatric nasal drops, Xylometazoline HCI 0.05%.
phrine 2.5 mg, chlorpheniramine 4 mg.
Nasal gel, Xylometazoline HCI 1% OTC ROBB® (P.Z.) OTC KATA® (Jawa) Pack: 4’s.
Pack: 10 mL Inhalant, Menthol 42.5%, camphor 40%, eucalyptus Tablet, Paracetamol 500 mg, phenylpropanolamine Dose: Adult: 1 tablet 3 times daily. Child (2-6 years):
oil 5%, methyl salipcylate 12.5%. HCl 25 mg, chlorpheniramine maleate 2 mg.
OTC XYLO-MEPHA® (Oculus) ¼ tablet 3 times daily. Max. 3 tablets daily.
Indications: Relief of nasal congestion.
Nasal spray, Xylomethazoline HCl 0.05%, 0.1% Paracetamol + Chlorpheniramine
Dose: Insert tip of inhaler into end of nostril and OTC AVROCOLD® (Avro)
Pack: 10 mL
breathe in deeply. OTC COL-COL® (Justeen) Tablet, Paracetamol 500 mg, Phenylephrine HCl 5
EMDEX
Tablet, Paracetamol 500 mg, chlorpheniramine mg, Chlorpheniramine 2 mg.
XYLOMETAZOLINE plus ANTAZOLINE OTC SEFSIL® (Reals)
maleate 2 mg. Pack: 25 x 4’s.
Vaporizing ointment, Kapur (camphor) 5.5%, Terpin
Indications: Nasal congestion of allergic origin. Pack: 4 x 25’s. Dose: Adult & Child (>12 years), 2 tablets q6hrs.
tel (Pinus longifolia) 4.53%, Menthol 3.0%, Euca-
Dose: 2-3 drops or 1 spray into each nostril, lyptus oil 1.15%, Nutmeg oil 0.54%, Ajwain Phool OTC BUCOLD® (JB Pharma)
OTC SAKOLD® (Geneith)
3-4 times daily (Carum copticum) 0.11%. Tablet, Paracetamol 500 mg, phenylephrine HCl 10
Tablet, Paracetamol 500 mg, phenylephrine HCI 2.5
OTC OTRIVIN-ANTISTIN® (Novartis) Pack: 10 g; 25 g mg, chlorpheniramine maleate 2 mg, caffeine 30 mg, chlorpheniramine maleate 2 mg, caffeine (anhy-
Nasal drops and spray, Xylometazoline HCI 0.05%, Indications: For relief of cough & cold, etc. Apply in mg; uncoated tab. drous) 30 mg; double layer uncoated tab.
antazoline sulphate 0.5%. the nostrils in children. Pack: 48 x 1 x 4’s Pack: 4’s (in blisters)
Pack: 10 mL. Indications: Relief of nasal and sinus congestion.
Paracetamol + Diphenhydramine Relief of allergic symptoms of the nose or throat
14.2.3 Systemic nasal decongestants
MISCELLANEOUS PREPARATIONS OTC SILAPEN® Night (RichyGold) due to upper respiratory tract allergies.Relief of sinus
Safety of Phenylpropanolamine (PPA) pain and headache. Adjunct with antibacterials in
Tablet, Paracetamol, diphenhydramine HCl.
OTC Medicated Oil (Neros) The Food and Drug Administration (FDA) sinusitis, tonsilitis and otitis media.
Oily solution, Peppermint oil 58 g, Menthol 8 g, Paracetamol + Chlorpheniramine Dose: Adults: 1 tablet 3-4 times daily
issued a public health advisory in November + Ascorbic acid
Methylsalicylate 2 g per 100 mL; paraffin oil. Child (6-12 years): ½ tablet 3-4 times daily.
2000 concerning phenylpropanolamine
Pack: 2 mL x 1’s; 10 mL x 1’s (in bottles). OTC CIKAFLU® (Michelle Lab)
hydrochloride. OTC products containing phe- OTC COLDAFLU® Plus (Adler)
Indications: Cold and flu; Rhinorrhea, stuffy nose; Tablet, Paracetamol 500 mg, chlorpheniramine
nylpropanolamine are no longer marketed in Tablet, Paracetamol, phenylephrine, chlorphe-
Muscles pains and strains; Mild skin antiseptic maleate 2 mg, ascrobic acid 25 mg.
US and also in Canada. niramine maleate.
(insect bites). Pack: 50 x 4’s
The drug is associated with increased risk of Pack: 4’s
Contra-indications: Do not use in newborns.
Precautions: Avoid applying on the mucosa, eyes, hemorrhagic stroke (bleeding into the brain OTC FLU-J® (Juhel) OTC COLDROP®(Hocheiz)
open and infected wound, serious skin diseases. Do or into tissue surrounding the brain) and FDA Tablet, Paracetamol 500 mg, chlorpheniramine Tablet, Paracetamol 500 mg, Caffeine (anhydrous) 30
not apply on the breast of nursing mother. maleate 2 mg, ascorbic acid 25 mg. mg, Chlorpheniramine maleate 2 mg, Phenylephrine
recommends that consumers not use any
Dose: Nasa congestion, Apply one drop of pure oil Pack: 200; 500. HCI 2.5 mg.
products that contain phenylpropanolamine. Indications: For symptomatic relief of fever, head-
into the nostrils or add a few drops in a Pack: 4’s
bowl of hot water and inhale the vapor with ache and nasal congestion associated with influenza Indications: Fast relief from symptoms of common
PHENYLPROPANOLAMINE plus and common cold, including allergic rhinitis.
decongestant effect. CHLORPHENIRAMINE plus PARACETAMOL cold, headache, influenza, Rhinitis, Nasal congestion
Muscle pain, Apply on the skin and massage. Dose: Adult: 2 tabs. 2-3 times daily; up to a max. and fever.
Indications: Symptomatic relief of pain, fever 6 tabs. daily. Child (2-6 years): ½ tab. 3
OTC MEKO® (Neros) and nasal congestion associated with allergic times daily. OTC GG Cold (Geneith)
Inhaler, Menthol 504 mg, Camphor 119 mg, Methyl- rhinitis, hay fever, sensitivity reactions, urticaria Syrup, Paracetamol 120 mg, Chlorpheniramine Capsule, Chlorpheniramine maleate 4 mg, Phenyle-
salicylate 19 mg, Turpentine oil 50 mg, Lemon oil and common cold. maleate 2 mg, Ascorbic acid 25 mg per 5 mL. phrine HCl 5 mg.
0.75µ1, Liquid paraffin 76 mg. Contra-indications: Hypersensitivity to any Pack: 100 mL. Pack: 10’s.
Pack: 6’s (in blisters). Dose: Adult (≥12 years), 1-3 capsules daily in di-
of the components; nursing mothers, children OTC AVROLIN® for Children (Avro)
Indications: For fast relief of nasal congestion in cold vided doses.
and catarrh. Insert into each nostril, holding other
below 6 years, hypertensive patients. Syrup, Paracetamol 120.0 mg, Chlorpheniramine
Precautions: May cause drowsiness thereby af- maleate 1 mg, Ascorbic acid 25 mg per 5 mL. OTC Mecure’s Cold Free (Mecure)
nostril closed, inhale deeply.
fecting mental alertness and ability to perform Pack: 100 mL Tablets, Flu tablet (Paracetamol 500 mg, Phenyle-
OTC OLBAS® (Kensington) hazardous tasks; avoid alcoholic beverages; Indications: For symptomatic relief of fever, head- phrine HCl 5 mg, Chlorpheniramine maleate 4 mg,
Inhaler, Menthol 40% w/w; in a plastic tube with a ache, running nose and nasal congestion associated Caffeine 30 mg) + Vitamin C tablet (Vitamin C 50 mg).
cardiovascular disorder, diabetes mellitus, hy-
screw-on cover. with influenza and common cold, catarrh, including Pack: 4 Flu tablets + 4 Vit C tablets (in a blister).
pertension, hyperthyroidism, renal and hepatic
630 | 14.2.3 Systemic nasal decongestants 14.2.3 Systemic nasal decongestants | 631
OTC STALCOLD® (GoldMoore) do not crush sustained release product; consult maleate 1 mg, Pseudoephedrine HCl 15 mg per 5 mL. PSEUDOEPHEDRINE plus TRIPROLIDINE
Tablet, Paracetamol, Caffeine, Phenylephrine. pharmacist or physician before using. Pack: 60 mL Therapeutic category: Nasal decongestant
Nursing action: Drops, Paracetamol 100 mg, Chlorpheniramine
Indications: Non-specific nasal congestions;
PARACETAMOL plus CETIRIZINE • Do not crush extended release drug product. maleate 1 mg, Pseudoephedrine HCl 9.38 mg per mL.
Pack: 15 mL with dropper. nasal allergic conditions, common cold, Hay
• Give chewing gum or sips of water to relieve dry
See under the preparations below fever, allergic and vasomotor rhinitis, aerotitis
mouth. OTC PROCOLD® (Orange Drugs)
• Elderly patients should be counseled about the
(otitis barotrauma).
OTC FLU-J Non Drowzy® (Juhel) Tablet, Paracetamol 500 mg, pseudoephedrine HCl
proper use of OTC cough and cold preparations. Contra-indications: Hypersensitivity to
Tablet, Paracetamol 500 mg, cetirizine 25 mg. 30 mg, chlorpheniramine maleate 2 mg
• Advise patient to avoid activities requiring mental Pack: Strips of 4’s.
Pseudoephedrine or Triprolidine or other sym-
Pack: 10’s; 100’s. pathomimetic amines; Severe hypertension
alertness as drowsiness or dizziness may occur. Dose: Adult, 1 tablet 3-4 times daily; Child (6-12
Indications: For daytime symptomatic relief of fever,
Dose: Adult and children over 12 years of years): ½ tablet 3-4 times daily and prostatic enlargement; MAOIs; Bronchial
headache and nasal congestion associated with in-
fluenza and common cold, including allergic rhinitis. age, One cap. 12 hourly preferably asthma, glaucoma, hyperthyroidism, hyper-
OTC SHECKOLD® (Embassy)
Dose: Adult: 2 tabs. 2-3 times daily; up to a max. 6 morning and evening. tension, diabetes mellitus.
Tablet, Paracetamol 500 mg, caffeine 30 mg, pseu-
tabs. daily. Not for long-term treatment. doephedrine 30 mg, chlorpheniramine 2 mg. Precautions: May affect ability to drive or
Child (6-12 years), 1 tab. 3 times daily; 2-6 Pack: 48 x 4’s. operate machinery. Pregnancy and lactation;
OTC Pseudoephedrine (EDL 19.2.1.2)
years, ½ tab. 3 times daily.
Tablet, Pseudoephedrine HCl 60 mg. Hepatic or renal dysfunction; Children under
Pseudoephedrine + Dextromethorphan
Oral liquid, Pseudoephedrine HCl 30 mg per 5 mL 2 years. Discontinue therapy if insomnia, pal-
+ Chlorpheniramine
PHENYLPROPANOLAMINEplus pitation or dizziness occurs. Alcohol or other
CHLORPHENIRAMINE plus OTC OTRINOL® (Novartis) POM FLUCOR DAY® (Hovid)
CAFFEINE plus PARACETAMOL centrally acting sedatives.
Capsule, Pseudoephedrine HCl 120 mg; s-r cap. Capsule, Paracetamol 250 mg, dextromethorphan
Indications: For symptomatic relief of fever, Interactions: Alcohol and other sedative-hyp-
120 mg – 10. HBr 10 mg, pseudoephedrine HCI 30 mg
headache, nasal congestion and rhinitis asso- notics may enhance sedative and CNS depres-
OTC Pseudoephedrine (Afrab-Chem) Pack: 10 x 10’s; 1 x 8’s; 1 x 2’s (in blisters); 100’s (in
ciated with influenza and common cold. sant effects of Triprolidine.
EMDEX
Tablet, Pseudoephedrine HCl bottle)
Precautions: Avoid driving a motor vehicle or Adverse effects: Drowsiness, dizziness, GI dis-
Pseudoephedrine + Chlorpheniramine OTC NOCOF® (Afra-Chem) turbances, dry mouth has occurred in some pa-
operating machinery while taking this drug. Drops, Pseudoephedrine HCl 9.38 mg, Dextrometho-
Dose: By mouth, Adult, 1 tab. 3-4 times daily; OTC KOLMED® (Embassy)
tients; Coordination disorder, tremor, fatigue.
rphan HBr 3.12 mg, Chlorpheniramine maleate 1.00 Advice to patients: Do not take drug within
Child (6-12 years), ½ tab. 3-4 times Capsule, Chlorpheniramine maleate 4 mg, pseu- mg.
daily; 2-6 years, ¼ tab. 3-4 times daily. doephedrine 30 mg. 2 hours of bedtime; because it can cause
Pack: 15 mL with dropper (in bottle).
Pack: 100’s. insomnia; take hard chewing gum or frequent
OTC CAEPRAMIN® (Vital) + Ammonium chloride sips of water to relieve dry mouth; do not crush
Tablet, Paracetamol 500 mg, caffeine 30 mg, phe- Pseudoephedrine + Paracetamol
+ Chlorpheniramine OTC COLZA® (Orange Drugs) extended-release dosage forms; avoid concur-
nylpropanolamine HCl 25 mg, chlor-pheniramine
Sachet, Paracetamol 500 mg, pseudoephedrine HCI rent use of alcohol and other CNS depressants;
maleate 2 mg; pink scored tab. marked ‘CAEPRAMIN’. OTC KOLD TIME® (Embassy)
Pack: 50 x 4.
30 mg, chlorpheniramine maleate 1 mg, ammonium notify physician if confusion, restlessness or
Tablet, Paracetamol 500 mg, caffeine (anhydrous) chloride 87.5 mg per 7 mL. hypotension occurs.
25 mg, pseudoephedrine (as HCI) 30 mg, chlorphe- Pack: Sachet of 7 mL.
PSEUDOEPHEDRINE niramine (as maleate) 2 mg.
Dose: Adult and children over 12 years, 1 tab.
Indications: For symptomatic relief of common
Pack: 48 x 4’s. or 10 mL 3 times daily; 6-12 years, 5
Therapeutic category: Oral vasoconstrictor cold/influenza such as fever, headache, stuffy and
Dose: Adult, 1 tablet 3-4 times daily. mL 3 times daily; 2-5 years, 2.5 mL 3
for nasal decongestion. runny nose, sneezing, sorethroat and cough
Child (6-12 years): ½ tablet 3-4 times daily. Dose: Adult, 1 sachet 3 times daily times daily.
Indications: Symptomatic relief from nasal
stuffiness due to colds, from irritation and OTC KOLDWIN® (Crowther) OTC ACTID® (Ranbaxy)
inflammation of the nose and throat due to Tablet, Paracetamol 500 mg, caffeine (anhydrous) 25 PSEUDOEPHEDRINE plus BROMHEXINE Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine
hay fever and other conditions of allergic origin mg, pseudoephedrine HCl 30 mg, chlorpheniramine Indications: As decongestant for respiratory HCl 30 mg.
(as maleate) 2 mg. conditions complicated by tenacious mucus Pack: 100 mL.
and from nasal catarrh due to irritation of the
Pack: 30 x 4’s. and congestion e.g. Asthma, Common cold,
vasomotor nerves. OTC ACTIFED® (GSK)
Dose: Adult, 1 tablet 3-4 times daily. Child (6-12
Contra-indications: Severe hypertension years): ½ tablet 3-4 times daily.
Tonsilitis, laryngitis, Sinusitis, Bronchitis, Tablet, Triprolidine HCl 2.5 mg, pseudoephedrine HCl
or severe coronary artery disease; diabetes; Pharyngitis. 60 mg; white scored tab. marked ‘WELLCOME M2A’.
patients receiving MAOIs. OTC MIXAGRIP® (Orange Drugs) Contra-indications, Precautions, etc: see Pack: 20; 100.
Caplet, Paracetamol 500 mg, pseudoephedrine HCl Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine
Precautions: Hypertension; hyperthyroidism; under Pseudoephedrine.
30 mg, chlorpheniramine maleate 2 mg HCl 30 mg per 5 mL.
enlargement of the prostate; persons over 65 Dose: Adult & Children (>12 years), 10 mL or Pack: 100 mL
Pack: Strips of 4’s.
years of age; pregnancy, breast-feeding. Dose: Adult, 1 caplet 3-4 times daily; Child (6-12
1 tablet 3 times daily.
Interactions: MAOIs (avoid co-administration), Child (2-5 years): 2.5 mL 3 times daily; OTC ACTIHIST® (Hovid)
years): ½ caplet 3-4 times daily
antihypertensives, digitalis, tricyclic anti-de- 6-12 years, 5 mL 3-4 times daily. Tablet, Triprolidine HCl 2.5 mg, pseudoephedrine
OTC NOCOLD® (Fil Pharma) HCl 60 mg.
pressants, aluminium hydroxide. POM SOLVIN® Plus (IPCA)
Tablet, Paracetamol 500 mg, pseudoephedrine 60 Pack: 1000.
Adverse effects: Occasionally dryness of Tablet, Bromhexine 8 mg, Pseudoephedrine 60 mg.
mg, chlorpheniramine 2 mg; uncoated tab.
mouth, loss of appetite, restlessness, insomnia, Pack: 10’s. OTC G-FED® (Greenlife)
Pack: 50 x 4’s.
acceleration of the pulse, palpitation. Oral liquid, Bromhexine 4 mg, Pseudoephedrine 30 Tablet, Triprolidine HCl BP 2.5 mg, Pseudoephedrine
Dose: Adult: 1 tablet 3-4 times daily; Child (6-12
Advice to patients: Do not exceed recom- mg per 5 mL. HCl BP 60 mg.
years): ½ tablet 3-4 times daily; 2-6 years),
Pack: 60 mL; 120 mL. Pack: 25 x 4’s.
mended dosage and do not use for more than ¼ tablet 3-4 times daily.
Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine
3-5 days; may cause wakefulness or nervous- HCl 30 mg per 5 mL.
OTC PANDA® Cold Drops (Afrab-Chem)
ness; take last dose 4-6 hours before bedtime; Syrup, Paracetamol 120 mg, Chlorpheniramine Pack: 60 mL.
632 | 14.2.4 Preparations for the cauterisation of nose 14.3 Throat drugs | 633
OTC PROFED® (Reals) the treatment of infections and inflammatory OTC Moko Glycerine Borax (New Healthway) Pastille, Menthol 1.07%, peppermint oil 0.54%, myrrh
Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine conditions of the respiratory tract include Mouth wash, Glycerine 88%, Borax decahydrate 12%. tincture 1.39%
HCl 30 mg per 5 mL. fusafungine which is used as spray in sinusitis, Pack: 50 mL. Pack: 24’s (in blisters)
Pack: 60 mL. rhinitis, coryza, pharyngitis, tonsillitis and other Indications: Sooth and help to reduce inflammation.
HEXETIDINE Recommended to help relieve throat irritation or
OTC SINUFED® (SKG) related conditions for oral hygiene. Glycerine,
dryness which may occur if you have been talking,
Tablet, Triprolidine HCl 2.5 mg, pseudoephedrine HCl thymol, menthol, camphor and eucalyptus are Indications: Oral hygiene
singing or smoking excessively of if you have a cold.
60 mg; white scored tab. marked ‘SKG C3A’. used in different formulations either as mouth- Dose: Use 15 mL undiluted 2-3 times daily Dose: Adults, Elderly & Children >12 years, dissolve
Pack: 20’s; 100’s. washes or as tablets or lozenges. OTC Hexetidine (EDL / Patent Medicines List) one pastille in the mouth and breath deeply.
Syrup, Triprolidine HCl 1.25 mg, pseudoephedrine
Mouth wash or gargle, Hexetidine 0.1% Repeat every 2 hours if required.
HCl 30 mg per 5 mL; clear orange syrup.
DEQUALINIUM Do not give to children <12 years.
Pack: 50 mL in amber bottle. OTC HEXEDENE® (Pharma-Deko)
Description: Dequadin is used locally for oral Mouth-wash, Hexetidine 0.1%; clear red solution.
OTC TRIFED® (Reals) antisepsis and to relieve pain and inflamma- NEOMYCIN plus BACITRACIN plus
Tablet, Pseudoephedrine (as HCl) 60 mg, triprolidine AMYLOCAINE plus MENTHOL
tion. MENTHOL plus ASCORBIC
(as HCl) 2.5 mg.
ACID plus CITRIC ACID Indications: Sore throat, tonsillitis, gingivitis,
Indications: For rapid relief of pain, soreness
+ Paracetamol seasonal mouth and throat infections, treat-
and inflammation associated with common Indications: Oral hygiene.
ment of germ carriers.
OTC ALTACOLD® (Evans) mouth infections such as Vincent’s angina, Dose: Dissolve one solution tablet or lozenge
Contra-indication: Hypersensitivity to any
Tablet, Paracetamol 500 mg, Pseudoephedrine HCl tonsillitis, sore throat, stomatitis, pharyngitis, under the tongue 3 times daily.
component of the preparation.
30 mg, Triprolidine HCl 2.5 mg. aphthous ulcer, thrush, glossitis; also for pre- OTC Menthol plus Ascorbic Acid plus Citric Acid
Pack: 50 x 4’s. Precautions: Not recommended for children
vention and treatment of infections following (EDL / Patent Medicines List)
Syrup, Paracetamol 125 mg, Pseudoephedrine HCl under 3 years of age, pregnant women, dia-
tooth extractions. Lozenges, Menthol 0.0900%, Ascorbic acid 2.9412%,
15 mg, Triprolidine HCl 0.625 mg per 5 mL. betic patients; avoid long-term use since it may
Dose: Initially, one Lozenge to be sucked Citric acid 0.8332%
EMDEX
Pack: 60 mL. result in growth of non-susceptible organism.
slowly 2-3 hourly; decrease the time
Indications: Symptomatic relief of fever, headaches, If itching, burning, inflammation or other signs
and nasal congestion associated with influenza and interval between doses when infec- MENTHOL plus EUCALYPTUS OIL
plus CAMPHOR plus THYMOL of sensitivity occur, patients should be advised
common cold, including allergic rhinitis. tion subsides.
Indications: Nasal obstruction in acute rhinitis to discontinue this preparation and consult a
Dose: Syrup/Tablet: Children (6 months – 2 years), OTC Dequalinium (EDL / Patent Medicines List)
or sinusitis physician.
2.5 mL; 2 – 6 years, 5mL; 6 – 12 years, Lozenges, Dequalinium HCl 0.25 mg.
5 – 10 mL. Precautions: Infants less than one month Adverse effects: Because of local anesthetic
Adult: One tab. 3-4 times a day OTC DEQUADIN® (Evans) of age. effect, taste of food may be disturbed.
Lozenge, Dequalinium Chloride 250 mcg; mottled Dose: Dissolve one lozenge under the Dose: Allow one lozenge to be dissolved
orange coloured pleasantly tasting flat/plain tab. slowly in the mouth; 8-10 lozenges
14.2.4 Preparations for the 250 mcg – 250’s.
tongue 3 times daily.
cauterisation of nose (or more if necessary) daily.
Dose: One lozenge to be sucked slowly every 2-3 OTC Menthol plus Eucalyptus Oil plus Camphor
hours. plus Thymol (EDL / Patent Medicines List) OTC MYBACIN® (Didachons)
SILVER NITRATE Paint, Dequalinium Chloride 0.5% w/v; clear bright Lozenges, Menthol 0.207%, Eucalyptus oil 0.069%, Lozenge, Neomycin sulfate equiv. to Neomycin base
Indications: Cauterisation of the nose. hygroscopic solution. Camphor 0.0007%, thymol 0.007%. 2.5 mg, Bacitracin zinc 100.0 units, Amylocaine
Pack: 10 mL. HCI 0.5 mg. Excipients – Sodium cyclamate, PVP
Nursing action: Avoid contact with clothing
Dose: Apply by means of a cotton wool or cotton MENTHOL plus PEPPERMINT K-90 (povidone), Menthol, Peppermint oil, Calcium
and unaffected areas, since discolouration
bud to the sites of infection every 3 hours; OIL plus MYRRH TINCTURE Stearate, Sucrose qs. to 1.0 g.
may occur. Pack: 10’s (in aluminium satchets); 40’s and 140’s
do not swallow saliva for a few moments
POM Silver Nitrate (EDL 19.2.1.1) after each application and for young child, OTC VOCALZONE® (Barata) (in boxes).
Aqueous solution, Silver nitrate 0.5%; freshly pre- hold its mouth open for a few moments.
pared
Sticks or crystals, Silver nitrate. DOMIPHEN BROMIDE
Therapeutic category: Antiseptic lozenge
14.3 Throat drugs Indications: Prevention and treatment of
Drug preparations are used locally for oral sore throats and husky voice (laryngitis); oral
antisepsis and to relieve pain and inflammation hygiene.
in such conditions as tonsillitis, mouth ulcers Dose: One lozenge to be sucked every 2-3
and infections, pharyngitis, glossitis and other hours
related inflammatory conditions. Corticoster- OTC Domiphen Bromide (EDL / Patent Medicines List)
oids in lozenges or paste are most effective Lozenges, Domiphen bromide 1.5 mg.
particularly if used in the prodromal phase of
aphthous ulcers. GLYCERINE plus THYMOL
Oral antiseptic lozenges like dequalinium, Indications: Oral hygiene,
domiphen bromide and amylmetacresol plus
OTC Glycerine plus Thymol (Afrab-chem)
dichlorobenzyl alcohol do have beneficial ac- Mouth-wash, Glycerol 10%, thymol 0.05%; clear
tions in mouth and throat infections but may red solution.
sometimes irritate and cause sore tongue and Pack: 200 mL.
sore lips. Topical antibiotic formulations for
15.1 Anti-infective skin preparations | 635
15. Dermatological drugs

The skin is frequently exposed to hazards from Topical formulations containing 2% mupirocin
the environment which explains the varieties or 2% fusidic acid [neither included on WHO
of skin infections and disorders that plague Model List] can be used to treat bacterial
man. However, the skin is highly amenable infections of the skin such as impetigo and
15.1 Anti-infective skin preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 635 to treatment by local application as there is folliculitis. To prevent the development of
intimate contact between the drug and target resistance, mupirocin and fusidic acid should
15.1.1 Antibacterial preparations. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 635 tissue with minimal systemic effects. In burns not be used for more than 10 days. Topical
15.1.2 Antifungal preparations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 638 and excoriated skin surfaces, systemic effects preparations containing neomycin and bac-
may create some problems due to enhanced itracin are also widely used but these carry a
15.1.3 Scabicides and pediculicides. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 647 absorption. Similarly, it may be difficult to risk of sensitization particularly with continued
15.1.4 Antiviral preparations . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 648 control the quantity of drug applied to the area or repeated use.
concerned and lack of patient compliance may Topical use of preparations containing anti-
15.2 Anti-inflammatory and antipruritic drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 649
be a problem. microbials which are widely used systemically
15.3 Astringents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 655 For topical application, dermatological drugs should be avoided. These include penicillins,
15.4 Preparations for acne. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 655 are usually formulated as ointments, creams, sulfonamides, streptomycin and gentamicin,
lotions or sprays. In these formulations, the which should be reserved for the systemic
15.4.1 Topical preparations for acne . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 656 vehicle and the active ingredients are both im- treatment of infections because of the pos-
15.4.2 Oral preparations for acne. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 657 portant to the success of treatment. The vehicle sibility of inducing sensitivity and favouring
may affect the degree of skin hydration, have the emergence of resistant organisms. Only
15.5 Preparations for psoriasis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 658 mild anti-inflammatory effect and the penetra- widespread superficial or deep-seated infec-
15.6 Preparations for actinic keratosis. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 659 tion of active drug in the preparation. The other tions associated with fever require treatment
EMDEX
additives may be a source of skin sensitization with a systemic antibiotic (sections 9.1.1 and
15.7 Preparations for warts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 659
particularly of eczamatous skin. This should 9.1.2). Whenever possible, the choice of an
15.8 Ultraviolet blocking agents. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 660 be considered during treatment. The serious antimicrobial should be based on the results
skin disorders encountered include bacterial of sensitivity tests.
15.9 Hair growth stimulants. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 661
and fungal infections for which appropriate
15.10 Other dermatologicals . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 661 formulations are used. Serious inflammatory BENZYLPENICILLIN
conditions are also encountered. Synonym: Penicillin G; Crystalline Penicillin
Therapeutic category: Penicillin antibiotic
15.1 Anti-infective skin preparations Indications: Local treatment of topical infec-
15.1.1 Antibacterial preparations tions of the skin including infected wounds, im-
15.1.2 Antifungal preparations petigo, abscess, intertrigo, secondary infected
15.1.3 Scabicides and pediculicides eczema, burns, furunculi.
15.1.4 Antiviral preparations Contra-indications: Hypersensitivity to
penicillin
15.1.1 Antibacterial preparations Adverse effects: Allergic reactions such as
Staphylococcal infections of the skin such exanthema, rash or urticaria may occur at
as impetigo, folliculitis, and furunculi and the site of application (usually disappear on
streptococcal infections such as cellulitis and cessation of therapy).
erysipelas are very common where the climate Dose: Apply in a thin layer to the affected
is hot and humid, where standards of hygiene area 2-3 times daily. Cover with a ster-
are compromised, and in immunodeficient ile dressing to avoid contamination of
patients. the affected area.
In all skin infections, an important part of OTC Penicillin (Daily Need)
Ointment, Penicillin potassium BP 10,000 IU per g.
treatment is cleansing and thorough drying.
Pack: 20 g.
Washing with soap and water will often help to
prevent infection. Light localized infections can OTC Penicillin (Drugfield)
often be treated effectively with an antiseptic Ointment, Benzylpenicillin.
solution such as chlorhexidine (section 16.3). Pack: 20 g.
Superficial crusts should be gently washed
with soap and water or a weak solution of GENTAMICIN
aluminium diacetate (section 15.3) or a Therapeutic category: Aminoglycoside, broad
0.01% solution of potassium permanganate. spectrum bactericidal antibiotic.
Infected burns should be treated with silver Indications: Primary skin infections; infected
sulfadiazine, which is bactericidal against both burns and wounds and other secondary skin
Grampositive and Gram-negative organisms. infections.
Contra-indications: Hypersensitivity to
636 | 15.1.1 Antibacterial preparations 15.1.1 Antibacterial preparations | 637
gentamicin Dose: Skin infections, apply 2 or 3 times daily OTC BANEDIF® (Afrab-Chem) if sensitisation reaction or severe local irritation
Precautions: Prolonged treatment may cause for 3 days. Powder, Neomycin sulfate 5 mg, bacitracin zinc 250 occurs; pregnancy, breast-feeding.
overgrowth of nonsusceptible micro-organ- units per g. Adverse effects: Localised itching, a burning
OTC Methylrosanilinium chloride (WMF 13.2) Spray, Neomycin sulfate 165,000 units, bacitracin
isms including fungi; if irritation, hypersensitiv- Aqueous solution, Methylrosanilinium chloride 0.5% sensation, erythema, stinging and dryness;
12, 500 units.
ity or significant infection occurs, discontinue Tincture, Methylrosanilinium chloride 0.5% rarely cutaneous sensitisation reactions.
Ointment, Neomycin sulphate 5 mg, bacitracin
therapy. zinc 500 I.U Advice to patients: For topical use only; do not
OTC Methylrosanilinium chloride (EDL 12.3)
Adverse effects: Irritation of skin, erythema, Pack: 20 g (in collapsible tube) apply into the eye; discontinue if rash, itching,
Aqueous solution, Methylrosanilinium chloride 0.5%.
itching, smarting; allergic sensitization (dis- or irritation occurs; improvement should be
OTC MOKO GENTIAN VIOLET® (New Healthway) OTC BANEOCIN® (Novartis)
continue treatment). seen in 5 days; do not use for treatment of
Solution, Gentian violet 5 mg per mL. Ointment, Bacitracin zinc 250 IU, neomycin (as sul-
Nursing action: phate) 5000 IU per 1 g
pressure sores in elderly.
Pack: 60 mL.
• Cleanse affected area with soap and water before
Pack: 20 g Dose: Apply three times a day for up to ten
application; apply enough medication to com- OTC Gentian Violet Paint (Nomagbon) days. Duration of treatment should
Powder, Bacitracin zinc 250 IU, neomycin (as sul-
pletely cover lesions, after drying. Liquid, Gentian violet 0.5% ; dark blue liquid. not be extended beyond ten days.
phate) 5000 IU per 1 g
• Teach patient to aply carefully under asepsis to Pack: 60 mL (in PET bottle). Pack:10 g (in sprinklers) Discard the remaining ointment after
avoid further infection.
• Avoid use on large skin lesions or over a wide area OTC Gentian Violet Solution (Gauze) OTC BIVACYN® (Taylek) treatment
because of possible systemic toxic effects. Liquid, Crystal violet 0.5% Powder, Neomycin sulfate 3,500 l.U. (5 mg), bacitracin POM BACTROBAN® (GSK)
• Prolonged use may result in overgrowth of non- Pack: 60 mL 250 I.U. per g. Ointment, Mupirocin 2%; sterile ointment in a
susceptible organisms. Pack: 5 g. white, transluscent, water soluble, polyethylene
• Instruct patient not to use in eyes or external ear, NEOMYCIN plus BACITRACIN Spray, (Aerosol Powder), Neomycin sulfate 165,000 glycol base.
if ear drum is perforated. Therapeutic category: Topical antibiotic. l.U., bacitracin 12,500 l.U. per 150 mL
• Advise patient to avoid the use of OTC creams, Pack: 150 mL. POM SUPIROCIN® (Glenmark)
Indications: Superficial bacterial infections of Ointment, Mupirocin 2% w/w.
EMDEX
ointment or lotions unless on doctor’s prescription
the skin due to staphylococci and streptococci. OTC CATRIN® (Embassy) Pack: 5 g; 15 g (in tubes).
• Observe for allergic reactions e.g. burning, stinging,
swelling, redness, rash.
Contra-indications: Neonates. Powder, Neomycin sulfate 3400 I.U, polymyxin B
Precautions: Avoid application to substantial sulfate 5000 IU, bacitracin zinc 400 IU per g. POLYVIDONE-IODINE
Dose: Cream or Ointment, apply a thin layer Pack:10 g; 100 g
to the affected skin area 3-4 times areas of skin or to broken skin (risk of significant
See under section 16.7.
daily. systemic absorption); overgrowth of resistant OTC CICATRIN® (SKG)
organisms on prolonged use. Powder, Neomycin sulfate 3,300 units, bacitracin
POM Gentamicin (EDL 12.3) Adverse effects: Sensitization, especially to zinc 250 units, L-cysteine 2 mg, dl-threonine 1 mg, POTASSIUM PERMANGANATE
Cream, Gentamicin (as sulfate) 0.3% neomycin, causing reddening and scaling; glycine 10 mg per g. Indications: Wet dressings to assist healing of
POM GENTADERM® (Fill Pharma) anaphylaxis reported rarely; systemic ab- Pack: 5 g.
suppurating superficial wounds, tropical ulcers,
Cream, Gentamicin (as Sulfate) 1 mg per g. sorption leading to irreversible ototoxicity, OTC NEOBACIN® (Drugfield) tinea pedis, pemphigus, impetigo.
Pack: 20 g. particularly in children, the elderly, and in renal Powder, Neomycin (as sulfate) 5 mg, bacitracin (as Contra-indications: Avoid occlusive dressings.
POM GENTALEK® (Taylek) impairment. zinc) 0 250 I.U per gram. Precautions: Irritant to mucous membranes.
Cream or Ointment, Gentamicin sulfate 1 mg per g. Nursing action: Pack: 5 g Adverse effects: Local irritation; skin and
Pack: 15 g. • Cleanse lesion with soap and water before appli- fabrics stained brown.
cation; cover lesion completely with medication. MUPIROCIN
POM Gentamicin (Drugfield) Dose: Suppurating superficial wounds and
• Teach patient to wash hands before and after each Therapeutic category: Topical antibiotic
Ointment, Gentamicin 0.% tropical ulcers, wet dressings of 1:10
application. Pharmacology: Mupirocin is a topical broad
Pack: 15 g • Observe skin for redness, burning, stinging or 000 (0.01%) solution, changed 2 or
spectrum antibiotic for the treatment of bac- 3 times daily; tropical ulcers also
swelling.
METHYLROSANILINIUM CHLORIDE • Do not use for more than 1 week unless directed
teria skin infections. It is active against staph- require treatment for 2–4 weeks with
Synonym: Gentian violet; Crystal violet. by physician. ylococci, including methicillin-resistant strains. procaine benzylpenicillin (section
Indications: Superficial fungal and bacterial Dose: Bacterial skin infections, ADULT and It is also active against many Gram-negative 9.1.1.1). Tinea pedis, soak severe
infections. CHILD over 2 years apply thin layer 3 bacteria as a result of the high concentrations weeping lesions in 1:10 000 (0.01%)
Contra-indications: Excoriated or ulcerated times daily (short term use). achieved after topical administration. Mupiro- solution every 8 hours. Impetigo,
lesions, broken skin, mucous membranes; Note: Aerosol powder – Prior to use, shake the aer- cin penetrates intact human skin but the rate superficial crusts should be gently
porphyria. osol container vigorously and spray the powder to of absorption is low and the absorbed drug is separated with a 1:10 000 (0.01%)
Adverse effects: Severe irritation (discontinue
the affected area from a distance of 20-25 cm. After rapidly metabolised and excreted as inactive solution.
use clean the valve by turning the aerosol container metabolite, monic acid.
treatment); temporary staining of skin, perma- upside down and blow the valve by short pressing. POM Potassium permanganate (WMF 13.2)
nent staining of fabrics; animal carcinogenicity Indications: Topical treatment of skin infec-
Aqueous solution, Potassium permanganate 1:10
(restricted use in some countries). OTC Neomycin plus Bacitracin (WMF 13.2) tions such as impetigo, folliculitis, infected
000 (0.01% solution)
Advice to patients: Drug stains skin and cloth- Ointment, Neomycin sulfate 5 mg, bacitracin zinc dermatosis e.g infected eczema, infected Note: Potassium permanganate is sometimes
ing purple; do not apply to ulcerative lesion;
500 IU/g. traumatic lesions e.g insect bites and minor supplied as an aqueous stock solution of 1 in 1000
keep affected area clean, dry and expose to OTC Bacitracin plus Neomycin (EDL 12.3) wounds and burns; to prevent bacterial in- (0.1%) for dilution before use.
air to prevent spread of infection. Ointment, Neomycin sulfate 5 mg, bacitracin zinc fection of small wounds, cuts and abrasions.
Nursing action: 500 units per g. Contra-indications: Not recommended for SILVER SULFADIAZINE
• Apply carefully to the lesion only; avoid undue Dusting powder, Neomycin sulfate 5 mg, bacitracin ophthalmic or intra-nasal use. Therapeutic category: Topical antibacterial.
staining of the skin. zinc 250 units per g. Precautions: When used on the face, avoid Pharmacology: Silver sulfadiazine has anti-
• Do not use occlusive dressings. contact with the eyes. Discontinue treatment
638 | 15.1.2 Antifungal preparations 15.1.2 Antifungal preparations | 639
microbial activity similar to the sulfonamides. Compound preparations fluconazole may be required if the foot is exten- because much of the infected area may appear
It possesses additional activity against Ps. POM HILDERM-CH® (Greenlife) sively infected. Tinea pedis commonly recurs normal and be left untreated. Better results
aeruginosa and some fungi due to the silver Cream, Silver sulfadiazine 1%, chitosan hydrochlo- and may be treated with miconazole cream. have been reported with topical applications
component. It is used topically, mainly for ride 2%; cream base. Severe weeping lesions respond to frequent of miconazole or selenium sulfide.
burns, pressure sores and leg ulcers. soaking in solutions of 1:10 000 potassium
POM Silver Sulfadiazine plus Chlorhexidine
Indications: Prophylaxis and treatment of permanganate, and systemic antifungals may BENZOIC ACID plus SALICYLIC ACID
(Crystal)
infection in burns. Cream,Silver sulfadiazine 1%, chlorhexidine (as also be needed. Indications: Mild dermatophyte infections,
Contra-indications: Hypersensitivity to sulfo- gluconate) 0.20% Nail infections (onychomycosis, tinea un- particularly tinea pedis and tinea corporis.
namides; pregnancy (Appendix 2); neonates pack: 30 g guium) are difficult to treat; fingernails may Adverse effects: Occasionally localized, mild
Precautions: Renal or hepatic impairment; require 6 months treatment with oral griseof- inflammatory reaction.
OTC SOS BURNS® (Bond)
G6PD deficiency; breastfeeding (Appendix 3) Cream, Silver sulfadiazine 1 g, chlorhexidine gluco- ulvin and toenails may require 12 months or Dose: Fungal skin infections, apply twice daily
Adverse effects: Allergic reactions include nate 0.2 g per 100 g. more of this treatment. Approximately 60% of until the infected skin is shed (usually
rashes, burning and itching; argyria and sulfo- Pack: 20 g nail infections either do not respond or relapse at least 4 weeks).
namide-induced systemic toxicity, including after treatment with griseofulvin.
POM SULPHADERM® (Miraflash) OTC Benzoic acid plus Salicylic acid (WMF 13.1)
blood disorders following application to large Cream or ointment, Benzoic acid 6%, salicylic acid 3%.
Cream, Silver sulphadiazine 1%, Chlorhexidine Ringworm of the groin (tinea cruris) is usually
areas or prolonged use; transient leukopenia gluconate 0.2%; cream base.
reported. limited to the skin of the inner thigh in contact OTC Benzoic acid plus Salicylic acid (EDL 12.2)
Advice to patients: For external use only; with the scrotum. Flexural eczema, often super- Ointment or Cream, Salicylic acid 3%, Benzoic acid 6%
bathe daily to aid in debridement (if not infected with candida or bacteria, occurs in the OTC DERMOL® (Jawa)
15.1.2 Antifungal preparations same site. The latter is frequently treated with
contraindicated); apply liberally to burned Ointment, Benzoic acid 6%, salicylic acid 3%, precip-
RINGWORM combined antifungal/corticosteroid prepara- itated sulphur 5%, menthol crystals 1.5%, titanium
areas; notify physician if condition persists
EMDEX
or worsens. Benzoic acid and methylrosanilinium chlo- tions, but must not be treated with a corticos- dioxide 8%.
Nursing action: ride (gentian violet) solutions are inexpensive teroid alone, which will worsen the condition. Pack: 15 g tube.
• Cleanse the affected area with soap & water to and effective fungistatic compounds for the An imidazole cream such as miconazole Indications: Athlete’s foot, skin itch, prickly
remove debris before each application if necessary. treatment of dermatophyte infections such as applied daily for 2 weeks is usually effective. heat, ringworm, eczema, skin rash, burning
• Completely cover burns with enough medication ringworm. Minor skin lesions due to ringworm Lesions unresponsive to topical preparations skin, acne, etc.
at all times, using aseptic technique. If needed, give can be cleared with repeated applications of can usually be cleared with a 4-week course Dose: Wash the affected parts of the skin
an analgesic before application. of griseofulvin. gently with warm water and soap
compound benzoic acid ointment (Whitfield
• Inspect patient’s skin daily and notify doctor if and dry. Apply the ointment on the
there is excessive pain or burning.
ointment), which combines the fungistatic CANDIDOSIS
action of benzoic acid with the keratolytic affected parts twice daily, in the
• Evaluate therapeutic response viz development of Candida can infect the oral cavity, the vagina
action of salicylic acid. However, the most morning and evening.
granulation tissue. or the skin. Cutaneous lesions tend to occur
• Encourage patient to bathe daily, if possible. effective topical treatment for dermatophyte in patients with diabetes mellitus and some OTC MAXADERM® (Therapeutics)
Dose: Infection in burns, apply using aseptic infections is a cream containing an imidazole chronic debilitating conditions, including Ointment, Benzoic acid 6%, salicylic acid 3%.
technique daily (more frequently if such as miconazole or clotrimazole, which hypoparathyroidism and various congenital
Pack: 15 g tube; 30 g; 60 g.
volume of exudate is large) whilst is effective for long-established lesions but is disorders of the immune system. The most OTC VITADERM® (Strides Vital)
there is a possibility of infection, or more expensive than compound benzoic acid severe infections of candida are now seen in Ointment, Benzoic acid 6%, salicylic acid 3%, sulphur
until healing is complete. ointment. Extensive and generalized infections patients with HIV infection. 4.5%; white coloured cream.
of the skin, nails and scalp should be treated Pack: 30 g.
POM Silver sulfadiazine (WMF 13.2) Cutaneous candidosis usually responds to
Cream, Silver sulfadiazine 1%; in 500-g container. systemically for several weeks with griseoful- OTC Whitfield’s Ointment (Drugfield)
vin or fluconazole (see section 9.2). miconazole or clotrimazole cream as a twice
Ointment, Salicylic acid, benzoic acid
POM Silver Sulfadiazine (EDL 12.3) daily application. Chronic candida paronychia,
Scalp ringworm (tinea capitis) typically appears Pack: 20 g.
Cream, Silver sulfadiazine 1% which can result ultimately in nail dystrophy,
as a patch of scaling alopecia, or a swollen is more difficult to treat. Treatment should be
POM DERMAZIN® (Taylek) inflammatory area (tinea kerion). Mild forms MESULPHEN plus SULPHUR
Cream, Silver sulfadiazine 1% in a hydrophilic base. based on determination of the underlying
may remit spontaneously at puberty. Inflamed Therapeutic category: Antifungal/keratolytic
Pack: 25 g; 50 g; 250 g. cause and its reduction or elimination; hands
lesions should be treated systemically with Indications: Parasitic skin infections such as
Dose: Cleanse the burn and apply with a and folds of the nail must be kept dry and daily
griseofulvin. Application of miconazole scabies, ringworm. Also pyoderma, seborrhoid
sterile spatula or a gloved hand to application of an imidazole cream for several
cream may accelerate healing of scaly lesions. eczema, secondary infections of acne vulgaris,
cover the burnt area once daily; may months may be required, ensuring penetration
Ringworm on the body (tinea corporis) can pruritus.
be reapplied daily in severe burn of the cleft between the nail plate and the
also be cleared with compound benzoic acid Contra-indications: Hypersensitivity to any of
wounds. Before each reapplication, swollen skin around the nail.
ointment or a topical imidazole such as mi- the ingredients.
wash the burn in shower or with an PITYRIASIS VERSICOLOR
antiseptic solution. Duration of treat- conazole. In resistant cases a 4-week course of OTC Bliss’s Sulphur Ointment® (Greenlife)
oral griseofulvin is required. Pityriasis (tinea) versicolor is caused by a com- Ointment, Precipitated sulfur 10%, mineral oil 10%,
ment depends on the injury ranging
mensal yeast. Application of sodium thiosul- white ointment 80%
from several days to one month at Foot ringworm (tinea pedis or athlete’s foot) is fate twice daily for 4 weeks is usually effective Pack: 30 g
most. usually treated topically. Compound benzoic although areas of depigmentation on darker OTC MEDSULF® (Embassy)
POM SILVEROL® (Dizpharm) acid ointment should be applied twice daily to skins remain after completion of treatment.
all infected areas and all toe clefts for at least Ointment, Precipitated sulfur 10%.
Cream, Silver sulfadiazine 1% Relapses can be frequent, however, probably Pack: 30 g.
Pack: 400 g. 4 weeks. Systemic therapy with griseofulvin or
OTC MITIGAL® (Gemini) skin folds, 2-3 weeks; Pack: 20 g (in tube). POM BAFAMA® (Seagreen)
Ointment, Sulphur 20%, mesulphen 64%. Pityriasis versicolor, erythrasma, 2 Dose: Apply thinly to the affected parts and gently Cream, Clotrimazole 1.0%, betamethasone dipropi-
Pack: 15 g. weeks; massage 2-3 times daily. Duration of treat- onate 0.05%, neomycin sulphate 0.5%
Superficial candidosis of the skin, 2 ment could be up to 2-4 weeks depending Pack: 15 g; 30 g
OTC Moko Sulphur (New Healthway)
on the extent and site of the disease. Indications: Topical use in treatment of a wide
Ointment, Precipitated sulphur 25 g. weeks.
range of eczemas and other inflammatory and al-
OTC CLOTRIMAX® (SKG)
OTC SULPHOREC® (GoldMoore) POM MYCOGEM® (Gemini) lergic infections of skin caused by various bacteria/
Cream, Clotrimazole 1%, in a water-miscible base.
Ointment, Precipitated Sulfur 10% w/w, mineral oil Cream, Bifonazole 0.15 g per 15 g. fungi. These conditions include contact dermatitis,
Pack: 20 g.
10% w/w, white ointment 80% w/w Pack: 15 g (tube). follicular dermatitis, impetigo, intertrigo, eczematoid
Pack: 30 g tube. OTC Clotrimazole (Miraflash) dermatitis, non specific pruritus.
CLOTRIMAZOLE Cream, Clotrimazole 1.0% w/w
OTC Sulphur (Daily Need) OTC BETA Forte (Crystal)
Pack: 30 g
Ointment, Sulphur. Therapeutic category: Imidazole antifungal Cream, Clotrimazole 1%, Betamethasone dipro-pion-
Indications: Dermatomycoses due to derma- OTC MEDYSTEN® (Embassy) ate 0.025%, Neomycin sulphate 0.5%; white creamy
OTC Sulphur (Drugfield) substance in tube.
tophytes and candida species; other fungal Cream, Clotrimazole 1%.
Ointment, Sulphur. Pack: 30 g.
skin diseases showing secondary infection Pack: 20 g.
Pack: 25 g.
with these fungi. Cream (forte), Clotrimazole 1%, betamethasone
POM CANDID-B® (Glenmark)
0.05%, neomycin 0.5%.
BIFONAZOLE Advice to patients: May cause irritation to the Lotion, Clotrimazole 1%, beclomethasone dipro-pi-
Pack: 20 g.
skin; avoid contact with eyes; notify physician onate 0.025%.
Therapeutic category: Broad spectrum anti- Pack: 15 mL.
if condition worsens or persists, or itching or OTC MYCOTEN® (Drugfield)
fungal with fungicidal activity. Cream, Clotrimazole 1% Indications: Fungal infections of the skin, particu-
Pharmacology: Bifonazole is a broad spectrum burning occurs.
Pack: 20 g. larly when accompanied by eczematous features:
antifungal reliably active against dermato- Nursing action:
Solution, Clotrimazole 2% Tinea capitis, Tinea pedis, Tinea corporis, Tinea
• Cleanse affected area with soap and water, dry well
EMDEX
phytes, yeasts, moulds and other fungi such as Pack: 25 mL. versicolor, Tinea barbae, Erythrasma, Tinea cruris,
before each application (dry the spaces between
Malassezia furfur; further, it is effective against Powder, Clotrimazole 1% Vulvo-vaginal candidiasis, Tinea manum, Candidal
the toes well if affected); completely cover lesions
Corynebacterium minutissimum. Its in vitro Pack: 20 g. nappy rash, Tinea unguium, Candidal paronychia.
with enough medication; do not use occlusive
activity against dermatophytes (e.g Trichophy- Dose: Wash & dry the affected area and then rub
dressings; teach patient to wash hands before and OTC NESTIN® (Bond) in the lotion. In hairly sites, the hair should
ton spp) is primarily fungicidal where as, that after each application. Cream, Clotrimazole 20 mg per g be parted before application to allow
against yeasts is primarily fungistatic. • Tell patient to continue using drug until full treat- Pack: 20 g tube direct contact with the lesions. Apply 2 to
Indications: Mycoses of the skin caused by ment period even if symptoms may have improved.
OTC SABRESTEN® (Gemini) 3 times daily
dermatophytes, yeasts, moulds and other fungi • Instruct patient to avoid OTC creams, lotions and
ointments unless on prescription. Cream, Clotrimazole 1%, in a water-miscible base. POM CANDIDERM® (Glenmark)
such as Malassezia furfur and infections due to Pack: 10 g; 20 g.
• Evaluate signs of allergy viz burning, swelling, Cream, Clotrimazole 1%, Beclometasone dipropion-
Corynebacterium minutissimum. stinging, redness; advise patient to notify physician Dose: Apply thinly 2-3 times daily to the diseases ate 0.025%, gentamicin 0.1%.
Infections of this type may be e.g. mycoses if no improvement is observed. sites and rubb in. Duration of treatment Pack: 5 g tube; 250 g (in jar)
affecting feet and hands (athlete’s foot, tinea depends on the extent and localisation of
Dose: See under the preparations below. Indications: Eczemas and other inflammatory and
manuum), mycoses involving skin and skin the disease: allergic dermatoses where secondary bacterial and/
folds (tinea corporis, tinea cruris). Pityriasis OTC Clotrimazole (EDL 12.2) Dermatomycoses, 3-4 weeks; or fungal infection is present or suspected: inguinal
Cream or Ointment, Clotrimazole 1%. Candida vulvitis and candida balanitis, 1-2
versicolor; Candida balanitis; Erythrasma. dermatoses, chronic dermatitis, erythrasma, eczem-
Dusting powder, Clotrimazole 1%. weeks; atoid dermatitis, dyshidrosis, contact dermatitis,
Contra-indications: Hypersensitivity to Pessaries, see section 11.2 Erythrasma and pityriasis versicolor, approx.
bifonazole seborrhoeic dermatitis, neurodermatitis, pustular
3 weeks. acne, follicular dermatitis, intertigo, impetigo, etc.
Dose: Unless otherwise prescribed, Micogem OTC CANDID® Dusting Powder (Glenmark)
Note: In fungi infection of the feet, to prevent Also useful in Tinea infections, particularly Tinea
cream is used once daily, at best Dusting powder, Clotrimazole 1%; in a purified
relapses, treatment should be continued for about pedis, Tinea cruris and Tinea corporis where sec-
Talc base.
before retiring. It is applied thinly to 2 weeks beyond the disapperance of all signs of dis- ondary bacterial infection is often seen along with
Pack: 30 g; 100 g (in bottles).
the skin areas affected and rubbed ease. After washing, the feet should be thoroughly pronounced eczema.
Dose: Wash & dry the affected area. Sprinkle dried (spaces between the toes). Sabresten cream
into the skin. Usually only a small Contra-indications: Skin tuberculosis, chicken pox,
the powder onto the affected area(s) is odourless, can be washed off and does not stain.
amount of cream (line of about ½ herpes simplex, measles, vaccinia, syphilitic skin
twice daily, morning and evening,
cm) will suffice for the treatment of OTC VISITA® (Elbe) lesions and in patients with hypersensitivity to any
in both adults and children (2-12 of its components. Avoid use of large amounts or for
an area of the size of the palm. For Cream, Clotrimazole 1%.
years of age); may also be dusted prolonged periods during pregnancy.
hygenic support of treatment it is OTC YTACAN® (Strides Vital)
into clothes or shoes in contact with Dose: Apply a thin layer to cover completely the
advisable to wash and thoroughly dry Cream, Clotrimazole 1%.
affected area. Duration of therapy affected area 2-3 times daily.
the skin area affected before applying Pack: 30 g.
usually 3 to 4 weeks.
the cream. POM DANBACT-3® (Dabak)
Compound preparations Cream, Clotrimazole 1%, bethamethasone dipropi-
Note: To achieve a lasting cure, treatment with mico- OTC CANEXCREAM® (Orange Drugs)
gem cream should not be stopped when the acute Cream, Clotrimazole 1% POM 3K Cream® (Kayhelt) onate 0.05%, gentamicin 0.1%
inflammatory symptoms and signs have subsided Pack: 20 g tube Cream, Clotrimazole 1.0%, betamethasone dipropi- Pack: 1 x 30 g
but, depending on the type of disease, be continued onate 0.05%, neomycin sulphate 0.5%. POM FUNZERO® (Mark)
OTC CLOTICAN® (Solution Pharma)
for the periods listed below: Pack: 15 g; 20 g Cream, Clotrimazole 1%, Betamethasone (as dipro-
Cream, Clotrimazole 1%
Mycoses of the foot, body, interdigital Pack: 30 g OTC ABF-3 (Bond) pionate) 0.05%, Neomycin sulfate 0.5%.
mycoses (be tween the toes), 3 weeks; Cream, Beclomethasone dipropionate 0.025%, Pack: 30 g tube
Mycoses affecting body, hands and OTC CLOTRIDERM® (Fill Pharma) Indications: Treatment of local fungal infections
Cream, Clotrimazole 1% clotrimazole 1.0%, gentamicin (as sulphate) 0.1%.
such as tinea pedis (athlete s foot), tinea cruris (jock for ophthalmic use. POM 3G® (Eutrix) versicolor, Paronychia candidimycetica.
itch), or tinea corporis (fungal infections elsewhere Adverse effects: Erythema, stinging, blistering, Cream, Econazole nitrate 10 mg, Triamcinolone Precautions: Avoid contact with eyes.
on the body). peeling, edema, burning and general irritation of acetonide 1 mg, Gentamicin sulfate 1 mg per g; Adverse effects: Skin irritation; allergic re-
Dose: Apply twice daily to affected areas the skin could be reported in connection with the white cream. actions.
use of Tribotan. Pack: 20 g (tube).
POM GENTAPROX® (Crystal) Dose: Superficial dermatomycoses, apply once
Advice to patients: Use the medication for full treat- Indications: Allergic and inflammatory skin dis-
Cream, Clotrimazole 1%, Betamethasone dipro-pi- daily for 2-3 weeks or longer.
ment time even when symptoms have improved. eases (eczema, dermatitis, diaper rash, intertrigo).
onate 0.05%, Gentamycin 0.10%; white creamy Vulvo-vaginal mycoses, apply twice
Inform the physician if the area of application Dermatophytosis (tinea): tinea pedis (athlete’s foot,
substance in tube. daily for 1 week. Treat sexual partner
shows signs of increased irritation (redness, itching, dyshidrotic tinea), tinea corporis (ringworm, vesic-
Pack: 20 g.
burning, blistering, swelling or oozing) indicative ular macular tinea), facial tinea (ringworm), tinea concurrently.
POM KEMI® (Jawa) of possible sensitization. Avoid sources of infection capitis, tinea cruris, tinea barbae, tinea versicolor;
POM TRAVOGEN® (Bayer Schering)
Cream, Clotrimazole 0.15 g (1%), Beclomethasone or re-infection. dermal candidiasis; secondary bacterial infection.
Cream/Ointment, Isoconazole nitrate 1%.
dipropionate 0.00375 g (0.025%) Dose: Gently massage sufficient Tribotan into the Dose: Apply to the affected skin area several times
Pack: 20 g tube.
Pack: 15 g affected and surrounding skin areas twice a day.
a day Relief usually occurs within 1st week
POM MIRACUTE® (Miraflash) POM DEMAPLUS® (Crystal) KETOCONAZOLE
of treatment
Cream, Clotrimazole BP 1%, Beclomethasone dipro- Cream, Econazole 10 mg, Triamcinolone 10 mg,
Therapeutic category: Synthetic broad-spec-
pionate BP 0.025%, Gentamicin sulphate BP 0.1%. OTC BABY TRIBOTAN® (Fidson) Gentamicin 1 mg.
Cream, Clotrimazole, Boric acid, Ichthammol Pack: 20 g tube.
trum antifungal agent.
Dose: Adult and child >12 years, Apply into the Pack: 20 g (in tube). Indications: Dermatophyte infections of the
POM DRUNALOG®(Drugfield) skin, cutaneous candidosis, tinea(ptyriasis)
affected and surrounding skin areas twice Indications: Prevention and treatment of baby
Cream, Econazole nitrate 10 mg, triamcinolone versicolor, seborrheic dermatitis, dandruff.
daily, in the morning and evening. nappy rashes and superficial inflammation occurring
acetonide 1 mg, gentamicin sulphate 1 mg per 1 g.
as a result of moisture and humidity in body areas; Precautions: Avoid contact with eyes; irrita-
POM NUFORCE-G® (Phillips) Pack: 20 g
Heat rashes on baby’s skin; Itching, discoloration, tion may occur when used after a prolonged
EMDEX
Cream, Betamethasone dipropionate 0.643 mg, blemishes, eczema and other skin disorders peculiar POM ENDIX-G® (Al-Tinez) therapy with topical corticosteroids(gradually
clotrimazole 10 mg, gentamicin sulphate 1 mg. to babies and young children. Cream, Econazole nitrate 10 mg, Triamcinolone withdraw the steroid therapy).
Pack: 20 g Dose: Apply sufficient cream unto buttocks area acetonide 1 mg, Gentamicin sulfate 1 mg per g. Adverse effects: Irritation, burning sensation.
OTC TRIBOTAN® (Fill Pharma) during every nappy change. For other Indications: For topical treatment of inflammatory
affected areas, apply sufficient cream unto Nursing action: See under Clotrimazole.
Ointment, Clotrimazole, Zinc oxide, Ichthammol, dermatomycoses and inflammatory skin conditions
Menthol. area 2-3 times daily or as often as you bathe complicated by bacteria or fungal skin infection: al- Dose: Cream, Dermatophyte skin infections
Pack: 20 g (in tube). the baby. lergic inflammatory dermatoses (eczema, dermatitis, and tinea versicolor, apply once daily
Pharmacology: Tribotan is useful for the treat- See also under Tribotan® for Adult above. diaper dermatitis, intertrigo, etc) Trychophytosis: to the affected areas for at least until
ment of skin infections caused by various species tinea pedis, tinea corporis, tinea face, tinea capitis, a few days after disappearance of all
POM VISITA® Plus (Elbe)
of pathogenic dermatophyte, yeasts, and other tinea cruris, tinea sycosis,Tinea versicolor,Skin symptoms; Serborrhoeic dermatitis,
Cream, Clotrimazole 1%, beclomethasone 0.02%,
isolates. Clotrimazole exhibits fungistatic activity candidiasis,Bacterial skin infections caused by apply 1-2 times daily depending on
gentamicin 0.1%.
against isolates of Trichophyton mentagrophytes. susceptible strains to gentamicin. severity of infection as above.
Pack: 20 g (in white tube with red stripes)
Epidermophyton floccusum and Candida spp. in- Dose: Apply to the affected area once to several
Shampoo, wash the affected areas of
cluding Candida albicans. Strains of fungi having times daily.
ECONAZOLE the skin with the shampoo:
resistance to clotrimazole are rare. Only a single
POM ENERVA® (Mark) Treatment, Seborrhoeic dermatitis and
isolate of Candida guilliermondi has been reported Therapeutic category: Imidazole antifungal
Cream, Econazole nitrate 10 mg, Triamcinolone dandruff, twice weekly for 2-4 weeks;
to have primary resistance to clotrimazole. Zinc Pharmacology: Econazole is an imidazole acetonide 1 mg, Gentamicin sulphate 1 mg.
Oxide and ichthamol are used in combination to antifungal agent closely related to miconazole Pityriasis versicolor, once daily for 5
Pack: 20 g tube.
treat other skin infections such as chronic eczema. and with similar antifungal and antibacterial days.
The bacteriostatic property of Ichthamol makes it
properties POM HD Cream (Next Generation) Prophylaxis, Seborrhoeic dermatitis
useful in treating other varieties of skin disorders. Cream, Econazole nitrate 10 g, triamcinolone ace- and dandruff, once every 1-2 weeks.
Menthol when applied to the skin has a soothing
Indications: Fungal infections of the skin such tonide 1.0 mg, gentamicin sulphate 1.0 mg per 1 g.
as candidiasis, pityriasis versicolor and tinea. The shampoo should be left on the
effect, which helps in relieving the discomfort of Pack:20 g skin for 3-5 minutes before rinsing.
itching and skin irritation. Advice to patients: See under clotrimazole.
Nursing action: See under Clotrimazole. POM TRI-ECO-G® (Solution Pharma) POM Ketoconazole (Nosak)
Indications: Treatment of superficial inflamma-
Cream, Econazole nitrate 1%, Triamcinolone aceton-
tion occurring in moist skin-folds of inner thighs, Dose: Apply 1-2 times daily up to a minimum Cream, Ketoconazole 2% w/w
ide 0.1%, Gentamicin 1%; cream base.
waist, buttocks, underside of breasts and armpits; of 10 days after symptoms subside. Pack: 30 g POM KETAZOL® (Shalina)
all dermatomycoses due to fungal species such
POM MITEKOL® (Taylek) Cream, Ketoconazole 2%
as Trichophyton species, yeast (Candida species), POM UPWELL® (Award Global)
Cream, Econazole nitrate 1% Pack: 30 g.
mould and other fungi; skin rashes; eczema and Cream, Econazole 10 mg, triamcinolone acetonide
Pack: 30 g (in tube). Shampoo, Ketoconazole 2%.
slight excoriation; pruritus and urticaria of the skin; 1.0 mg, gentamicin sulphate 1.0 mg per gram
Powder, Econazole nitrate 1% Pack: 100 mL (in bottle).
other skin disorders. Pack: 20 g
Contra-indications: Hypersensitivity to any of the Pack: 30 g (in box). POM KETOGATE® (Pharmgate)
constituents. ISOCONAZOLE Shampoo, Ketoconazole 2%, Salicylic acid 2%
Precautions: Discontinue if irritation occurs; use ECONAZOLE plus TRIAMCINOLONE Pack: 100 mL X 1’s.
plus GENTAMICIN Indications: Broad spectrum antimycotic
the medication for full duration of treatment even Cream, Ketoconazole 2%.
when symptoms have improved. Avoid sources of for the following skin conditions: superficial Pack: 20 g x 1’s.
POM ACNEAWAY® (Elbe)
infection, or re-infection. Even when symptoms mycoses caused by dermatophytes; yeast and
Cream, Econazole nitrate 10 mg, triamcinolone POM MEKOZORAL® (Neros)
have improved, do not discontinue the use of the acetate 1 mg, gentamicin sulfate 1 mg. yeast-like fungi particularly Candida albicans;
Cream, Ketoconazole 2%.
medication before full duration of treatment. Not Pack: 20 g (in green tube) moulds e.g. Tinea species, Candidosis, Pityriasis
Pack: 15g in tube.
POM NIZORAL® (Janssen-Cilag) least 10 days after the condition has base. OTC Nystatin (EDL 12.2)
Cream, Ketoconazole 2%; in a water-miscible base. cleared. Nail infections, apply 1–2 Pack: 15 g (in tube) Ointment or Cream, Nystatin 100,000 units per g.
Pack: 15 g (in tubes). times daily.
Shampoo, Ketoconazole 2% MICONAZOLE plus DEXAMETHASONE SELENIUM SULFIDE
Pack: 60 mL (in plastic containers). OTC Miconazole (WMF 13.1) plus NEOMYCIN
Cream or ointment, Miconazole (as nitrate) 2%. Selenium sulfide is a complementary drug for use in rare
POM NITOZOL® (Pharmabox) POM FUNGUSOL® Plus (Afrab-chem) disorders or in exceptional circumstances.
Cream, Ketoconazole 20 mg per g; milky white OTC Miconazole (EDL 12.2) Cream, Miconazole nitrate 2%, dexamethasone so-
topical cream. Cream, Miconazole nitrate 2% dium phosphate 0.056%, neomycin sulphate 0.665% Indications: Pityriasis versicolor (lotion),
Pack: 20 g. Lotion, Miconazole nitrate 2%; tincture. Pack: 20 g seborrhoeic dermatitis (detergent-based
Oral gel, Miconazole nitrate 2-2.5% Lotion, Miconazole nitrate 2%, dexamethasone so- suspension).
Compound Ketoconazole preparations Dusting powder, Miconazole nitrate 2% dium phosphate 0.056%, neomycin sulphate 0.665% Contra-indications: Children <5 years.
POM HAICNEAL® (Vixa) Vaginal ovule, See under section 11.2 Pack: 50 mL Precautions: Do not apply to damaged skin
Lotion, Ketoconazole 0.015 g, Clobetasol propionate OTC DAKTANOL® (Mark) (risk of systemic toxicity); avoid contact with
0.00025 g per. Cream, Miconazole nitrate 20 mg per g. MICONAZOLE plus HYDROCORTISONE
Pack: 50 mL (in tube).
eyes; do not use within 48 hours of applying
Pack: 30 g. Therapeutic category: Antimycotic, antibac- preparations for hair colouring, straightening,
Indications: For treatment of dandruff, seborrheic
dermatitis and pruritus on the scalp caused by OTC DAKTARIN® (Janssen-Cilag) terial, anti-inflammatory agent. or permanent waving.
Pityrosporum. Cream, Miconazole nitrate 2%; in a water-miscible Indications: Mycotic infections of the skin Adverse effects: Local irritation, hair discolor-
Dose: Apply about 5 mL to moist hair; massage it base. associated with inflammation, pruritus and al- ation or loss; absorption may result in systemic
gently to let the lotion contact with the Pack: 15 g (in tube). lergy; bacterial infections due to staphylococci toxicity including tremors, weakness, lethargy,
scalp thoroughly. After 3-5 minutes, rinse Powder, Miconazole nitrate 2% and streptococci; eczematous skin diseases pain in lower abdomen, occasional vomiting
cleanly with water. For treatment purpose, Pack: 20 g (in a shaker) that require “protective” treatment. (symptoms usually resolve within 10 days).
use twice a week and continuously for 2-4 Tincture, Miconazole 2%; alcoholic solution.
Contra-indications: Tuberculous skin affec-
EMDEX
Pack: 30 mL (in a bottle with brush)
Advice to patients: For external use only;
weeks. For prevention purpose, use once
Dose: Apply 2 times daily, to the lesion and spread it
tion, herpes simplex, vaccinia, all forms of notify physician if condition persists or wors-
every 1-2 weeks.
out with the brush. For feet infections, pow- varicella. ens; avoid contact with eyes; thoroughly rinse
POM SKINEAL® (Vixa) der the feet with Daktarin powder during Precautions: Pregnancy and infants especially after application; discontinue use and notify
Cream, Ketoconazole 10 mg, Clobetasol propionate and after treatment especially between the if the medication is to be applied to extensive physician if rash or irritation occurs.
0.25 mg, Neomycin (as Sulfate) 5000 IU per g; white toes and also possibly the socks and shoes. surface areas or under occlusive dressing. Dose: Pityriasis versicolor, apply lotion with a
or off-white cream with an emulsive base. Note: Hygienic measures such as washing the Dose: Apply 1-2 times daily; rub into the small amount of water to the entire
Pack: 50 mL (in tube). lesions or infected areas daily, changing and disin-
Indications: Topical treatment of fungal infection affected areas gently until completely affected area and rinse off after 10
fecting socks and shoes are recommended. Clean absorbed. Continue treatment until
of skin such as tinea manus, tinea pedis, tinea cor- minutes, repeat once daily for 7–14
the treated nail once weekly with a piece of cotton
poris, tinea cruris and tinea versicolor; also effective lesion has disappeared. days; or apply undiluted lotion at
with pure acetone (no nail remover) since dust and
for many kinds of dermatitis, eczema and pruritus. fibres of clothes may colour the nail black. Do not POM Miconazole plus Hydrocortisone (EDL 12.2) bedtime and rinse off the following
Dose: Apply externally to affected area twice daily; apply to open lesions. Cream, Miconazole 2%, Hydrocortisone 1%. morning, apply 2–7 times over 2
use for 2 weeks on ordinary tinea corporis weeks; repeat course if necessary.
and tinea cruris, and for 4 weeks on tinea OTC FUNGUR® (Taylek) POM DAKTACORT® (Janssen-Cilag)
Seborrhoeic dermatitis, massage 5–10
pedis and tinea manus. Cream, Miconazole nitrate 20 mg per g Cream, Miconazole nitrate 2%, hydrocortisone 1%.
Pack: 25 g; 50 g (in tubes) Pack: 15 g (in tube). mL of shampoo into wet hair and
POM SKIPERM® (Pemason) leave for 2–3 minutes before rinsing
Cream, Ketoconazole 10 mg, clobetasol 0.25 mg, OTC FUNGUSOL® (Afrab-chem) thoroughly; repeat twice weekly for 2
Lotion, Miconazole nitrate 2%. NYSTATIN
neomycin 5000 I.U. weeks, then once weekly for 2 weeks,
Pack: 15 gm Pack: 50 mL. Therapeutic category: Antifungal Agent,
thereafter only when needed.
Indications: Topical treatment of fungal infections Powder, Miconazole nitrate 2%. topical
Note: To minimize absorption, rinse hair thoroughly
of the skin including, tinea manus, tinea pedis, tinea Pack: 20 g. Indications: Localized forms of candidiasis, after use and remove all traces from skin (including
corporis, tinea cruris, tinea versicolor, dermatitis, Ointment, Miconazole nitrate 2%. infant eczema, pruritus and vulvae. nails).
allergic reactions such as eczema, pruritus. Pack: 20 g. Adverse effects: Contact dermatitis.
Dose: Candida infections, tinea cruris and corporis, OTC Selenium sulfide (WMF 13.1)
Advice to patients: Discontinue and report
MICONAZOLE apply twice daily (morning and evening) Detergent-based suspension, Selenium sulfide 2%.
to the affected areas for 2 weeks. to physician if irritation occurs; do not stop
Therapeutic category: Imidazole antifungal. Tinea pedis, apply twice daily as above for treatment even if you are feeling better; use OTC Selenium Sulfide (EDL Patent Medicines List)
Indications: Superficial fungal infections due one month. only on the skin. Shampoo, Selenium sulfide 2.5%.
to dermatophytes and yeasts, and secondary Tinea versicolor, apply once daily. Nursing action:
infections caused by Gram-positive cocci, in- • Cleanse affected area with soap and water, and dry SODIUM THIOSULFATE
OTC MICOZOL® (Drugfield)
cluding ringworm, intertrigo, candida napkin well before application. Indications: Pityriasis versicolor; cyanide poi-
Cream, Miconazole nitrate 2%
rash, paronychia, and pityriasis versicolor. • Do not use occlusive dressings. soning (section 19.2.7).
Pack: 20 g
Adverse effects: Occasional local irritation and • Cream is recommended for intertrigous areas; Dose: Pityriasis versicolor, apply twice daily
Lotion, Miconazole nitrate 2%
burning, also contact dermatitis; discontinue if powder for very moist areas; ointment for dry areas.
Pack: 50 mL. for 4 weeks.
• Tell patient to continue using drug until full treat-
sensitization occurs.
OTC MINAK® (Nosak) ment period. POM Sodium thiosulfate (WMF 13.1)
Advice to patients: See under clotrimazole.
Cream, Miconazole (as nitrate) 2% w/w. Dose: Apply 2-4 times daily; continue treat- Solution, Sodium thiosulfate 15%.
Nursing action: See under Clotrimazole.
OTC TINAZOL® (Hovid) ment for 7 days after lesions have
Dose: Skin infections, apply twice daily to
Cream, Miconazole nitrate 2%; in a water-miscible healed.
clean dry lesions, continuing for at
646 | 15.1.2 Antifungal preparations 15.1.3 Scabicides and pediculicides | 647
TERBINAFINE skin area 1-2 times daily. Prevention of athlete’s foot, apply once daily. Precautions: Do not use on inflamed or bro-
Therapeutic category: Allylamine antifungal Spray application, Undecenoic acid 2.5%, di- ken skin; avoid contact with eyes and mucous
POM BETROSIL® (Drugfield) chlorophen 0.25%; pressurised aerosol pack.
Pharmacology: A broad spectrum antifungal Cream, Tioconazole 1%. membranes; not recommended for children;
Pack: 100 mL. breastfeeding (withhold during treatment).
which at low concentrations is fungicidal Pack: 20 g. Dose: Treatment of athlete’s foot, apply twice daily
against dermatophytes, moulds and certain Adverse effects: Local irritation, particularly
POM TIOCOSID® (Neimeth) continuing for 7 days after lesions have
dimorphic fungi. The activity agianst yeasts healed. in children.
Cream, Tioconazole 1%.
is fungicidal or fungistatic, depending on the Pack: 20 g tube Prevention of athlete’s foot, apply once daily. Nursing action:
species. Less than 5% of terbinafine is absorbed • For topical use only; do not apply to raw or in-
POM TROSYD® (Neimeth) flamed skin, or face; avoid contact with eyes. Flush
after topical application to humans; systemic
Cream, Tioconazole 1%.
15.1.3 Scabicides and pediculicides with water if there is accidental contact with eyes.
exposure is thus very slight. Pack: 20 g tube SCABIES • Instruct patient to discontinue and report to phy-
Indications: Fungal infections of the skin and sician if skin irritation or hypersensitivity occurs.
nails caused by dermatophytes; yeast infec- Scabies is caused by a mite, Sarcoptes scabiei,
TOLNAFTATE • Clothing and bedding should be washed off
tions of the skin caused by the genus candida; that burrows into the skin. It is readily transmit- drug and then sterilized by boiling, dry cleaning
Therapeutic category: Antifungal Agent, ted from person to person, therefore the entire
pityriasis (tinea) versicolor. or applying very hot iron to kill the scabies mite.
Topical. household must be treated at the same time to
Precautions: Avoid contact with eyes; children. • Reassure patient that itching may take several
Indications: Treatment of tinea pedis, tinea cru- prevent reinfection. It is not necessary to take weeks to stop.
Adverse effects: Occasionally redness, itching
ris ,tinea manuum, tinea versicolor infections. a bath before treatment with an acaricide, but • Topical corticosteroids may be prescribed if der-
or stinging at the site of application.
Contra-indications: Hypersensitivity to tolnaf- all clothing and bedding should be washed to matitis develops from scratching.
Advice to patients: For external use only;
tate ;nail and scalp infections. prevent reinfection. • Avoid application to children’s hands as they will
not for oral, ophthalmic, or intravaginal use; if
Precautions: Keep from eyes; if no improve- put hands in their mouths.
irritation or sensitivity occurs, discontinue use Benzyl benzoate is an inexpensive scabicide. • Benzyl benzoate is preferred to lindane in treating
ment within 4 weeks,discontinue treatment.
and notify physician. It must be applied to all skin surfaces, from children and pregnant or nursing mothers.
EMDEX
Usually not effective alone for the treatment
Dose: Apply once or twice daily to the the scalp to the soles of the feet, avoiding Dose: Scabies, ADULT, apply over whole
of infections involving hair follicles or nails.
affected skin and sorrounding area contact with the eyes; it is too irritant for use on body; repeat without bathing on
Adverse effects: Pruritus, contact dermatitis,
in a thin layer and rub in lightly; for children. Permethrin is less irritant and more the following day and wash off 24
irritation, stinging.
1-2 weeks in tinea corporis or cruris, effective than benzyl benzoate, but also more hours later; a third application may
Advice to patients: Avoid contact with eyes;
2-4 weeks in tinea pedis, 1-2 weeks expensive; it may be used on children. Young be needed in some cases. Pedicu-
apply to clean dry area; consult the physician if
in cutaneous candidiasis, 2 weeks in infants can be treated with a cream containing losis, ADULT, apply to affected area
a skin irritation develops or if the skin infection
pityriasis versicolor. precipitated sulfur 6–10% applied once daily and wash off 24 hours later; further
worsens or does not improve after 10 days of
Note: Cleanse and dry the affected areas thoroughly for one week. applications possibly needed after 7
prior to application. therapy; does not stain skin or clothing.
Nursing action: Ivermectin (section 9.4.2.3) in a single oral and 14 days.
POM LAMISIL® (Novartis) • Wash and dry the affected area before each appli- dose of 200 µg/kg may be used in combina- OTC Benzyl benzoate (WMF 13.6)
Cream, Terbinafine HCI 10 mg per g cation; apply only a small quantity of medication tion with topical drugs for the treatment of Lotion, Benzyl benzoate 25%.
Pack: 7.5 g; 15 g as directed; ensure the area is not wet with the hyperkeratotic scabies that does not respond
Solution, Terbinafine HCI 10 mg per mL solution after the application. OTC Benzyl Benzoate (EDL 12.7)
to topical treatment alone. Emulsion, Benzyl benzoate 25%.
Pack: 30 mL vial • Tell patient to continue using medication until full
Spray, Terbinafine HCI 10 mg per mL treatment period. PEDICULOSIS
OTC Moko Benzyl Benzoate (New Healthway)
Pack: 15 mL; 30 mL vial • Itching, burning, and soreness are usually relieved Pediculosis of the head and body is caused Emulsion, Benzyl benzoate 28%.
DermGel, Terbinafine HCI 10 mg per mL within 24-72 hours. by Pediculus humanus capitis and Pediculus Pack: 100 mL
Pack: 5 g; 15 g; 30 g • Discontinue medication and report to doctor if
humanus corporis respectively; pubic lice (crab OTC Benzyl Benzoate (Nomagbon)
POM TERBIMAX® (Evans) condition worsens.
lice) infestations are caused by Pthirus pubis, Liquid, Benzyl Benzoate 25% ; white emulsion.
Cream, Terbinafine 10 mg. Dose: Wash and dry the affected area; apply
which may also affect the eye lashes and brows. Pack: 60 mL (in glass bottle).
1-3 drops of solution and rub into the
All are transmitted by person to person contact,
TIOCONAZOLE affected areas 2-3 times per day for OTC Benzyl Benzoate (Rajrab)
and may also contaminate clothing and bed-
Therapeutic category: Antifungal 2-4 weeks. Topical solution, Benzyl benzoate 25% w/v; 100-mL
ding. All members of the affected household pack marked “RAJRAB” on the cap.
Pharmacology: Tioconazole is a broad spec- (and sexual contacts) must be treated at the Pack: 100 mL; 2 L
trum antifungal agent which also has antibac- ZINC UNDECENOATE plus
UNDECENOIC ACID PREPARATIONS same time, and clothing and bedding should
terial activity against several Gram-positive OTC SCABCARE® (Vitabiotics)
be washed or exposed to the air; in head lice
organisms including staphylococcus and OTC MYCOTA® (Olpharm) Cream, Benzyl Benzoate
infestations, hair brushes and combs should Pack: 100 mL.
streptococcus spp. Cream, Zinc undecenoate 20%, undecenoic acid 5%.
Pack: 25 g. also be disinfected.
Indications: Topical treatment of dermal OTC SCABISTOP® (Gauze)
Dose: Treatment of athlete’s foot, apply twice daily Head and body lice are readily treated with Lotion, Benzyl benzoate 25% v/v
infections due to susceptible fungi (derma- continuing for 7 days after lesions have permethrin; malathion is effective against Pack: 100 mL
tophytes and yeasts) and in those conditions healed. pubic lice. Benzyl benzoate may be used for
complicated by infection with susceptible Prevention of athlete’s foot, apply once daily. all lice infestations. CROTAMITON
gram-positive bacteria. Powder, Zinc undecenoate 20%, undecenoic acid 2%.
Precautions: 1st trimester of pregnancy. Pack: 70 g. Indications: Treatment of scabies. For the
Dose: Treatment of athlete’s foot, apply twice daily
BENZYL BENZOATE relief of itching and skin irritation caused
Advice to patients: See under clotrimazole.
Nursing action: See under Clotrimazole. continuing for 7 days after lesions have Indications: Scabies; head, body and pubic by, for example, sunburn, dry eczema, itchy
Dose: Apply to the affected and surrounding healed. lice. dermatitis, allergic rashes, hives, nettle rash,
648 | 15.1.4 Antiviral preparations 15.2 Anti-inflammatory and antipruritic drugs | 649
chickenpox, insect bites and stings, heat rashes Idoxuridine is used less frequently for herpetic 15.2 Anti-inflammatory and may be responsible for exacerbations; in such
and personal itching. infections of the skin since aciclovir is more antipruritic drugs cases, an oral antibiotic such as erythromycin
Contra-indications: Hypersensitivity; Acute effective. Herpes simplex seems to respond See EMDEX Vol. 3 for the detailed information on
can be given for 7–10 days (section 9.1.2.4).
exudative dermatitis; Avoid contact with the to frequent applications if started early and Topical Corticosteroids SEBORRHOEIC DERMATITIS
eyes as may cause conjunctival inflammation. continued for 3 to 4 days.
Precaution: For external use only. Avoid ap- CONTACT DERMATITIS Use of a keratolytic shampoo and exposure to
plication near the eyes, broken skin or mucous ACICLOVIR ultraviolet light reduce both the inflammation
Contact dermatitis can result from an allergic and the scaling resulting from seborrhoeic der-
membrane. Pregnancy; nursing mother should Indications: Herpes viral infections of the skin. or irritant skin reaction. Removal of the sub-
not apply the cream to the nipple area; Children matitis of the scalp (dandruff ). The shampoo
Adverse effects: Transient burning and sting- stance provoking the reaction is the first step
(<3 years). should be massaged into the scalp, immedi-
ing, rash, pruritus. in treating this condition. Mild cases of contact
Adverse effects: Occasionally irritation of the ately rinsed off and then reapplied until a foam
Nursing action: dermatitis can be treated with topical hydro-
skin or contact allergy may occur (discontinue). • Wear finger cot or rubber gloves when applying is produced, leaving the second application in
cortisone which suppresses inflammation. A contact with the scalp for at least 5 minutes.
Dose: Scabies, Apply to the whole body from cream or ointment for self-protection.
short course of oral prednisolone or a topical
chin down, after a hot bath and dry- • For use on skin only; don’t apply to the eye. Selenium sulfide, which has both antifungal
• Ensure ointment covers all the lesions. corticosteroid such as betamethasone should and keratolytic properties, is widely used in
ing including body folds and creases. be considered for more severe cases and for
May repeat once daily for 3-5 days. • Inform patient that he may transmit the virus many proprietary shampoos. A combination of
even during treatment; he should avoid sexual suppression of severe acute reactions associ- sulfur and salicylic acid, which has an additional
Clothings and bed linens should be intercourse when lesions are present. ated with blistering, exudation and oedema.
changed the next morning to avoid antimicrobial action, is also effective.
• Explain to patient that aciclovir is not a cure. Soaking in clean water or mild saline solution
re-infection. Dose: Adult and child: apply to all lesions is recommended in the acute stages of severe ICHTHYOSIS
Pruritus, Apply to the affected area every 3 hours while awake, 6 times dermatitis. In ichthyosis, emollients such as aqueous
2-3 times daily; usually provides daily for one week. creams and emulsifying creams should be ap-
EMDEX
relief from irritation for 6-10 hours PRURITUS
POM Aciclovir (EDL 5.11)
plied daily (or more frequently in severe cases)
after each application. May repeat Pruritus or itching is a common symptom of to affected skin. The addition of a keratolytic,
Cream, Aciclovir 5%.
as needed. A cleaning bath should many skin diseases. However, systemic disease, such as salicylic acid 5% can be helpful.
be taken 48 hours after the last POM Aciclovir (Neros) contact with certain substances, conditions
application. Cream, Acilovir 5%. that dry the skin, stress, and extremes of LICHEN PLANUS
Pack: 5 g tube. temperature may also be a cause. Thus, an Lichen planus is a chronic, papular, pruritic skin
OTC MITIGEM® (Gemini)
Cream, Crotamiton 10% w/w. POM ACRON® (Pharmabox) important part of treatment is to eliminate or eruption that occurs typically in middle age
Cream, Aciclovir 50 mg per g; milky white cream. minimize the reason for the irritation. and later life; the condition is often mild and
PERMETHRIN Pack: 10 g tube.
Emollients are of value in pruritus associated may need no treatment. In generalized mild
POM LOVIR® (Ranbaxy) with dry skin or in pruritus occurring in an cases, a topical corticosteroid may relieve pru-
Indications: Scabies; head and body lice.
Cream, Aciclovir 5%. otherwise healthy elderly individual; the ritus. In severe forms systemic treatment may
Precautions: Do not use on inflamed or broken
Pack: 5 g; 10 g (in tubes). value of calamine lotion is uncertain. Systemic be necessary; oral corticosteroids, ciclosporin
skin; avoid contact with eyes; breastfeeding
antihistamines, such as oral chlorphenamine and retinoids have been used.
(withhold during treatment). POM VACRAX® (Alpha)
Adverse effects: Local irritation; rarely rashes Cream, Aciclovir 5%; in a white soluble cream base. (section 8.1), may relieve generalized pruritus. PITYRIASIS ROSEA
and oedema. Pack: Tubes of 5 g and 10 g. Topical corticosteroids, such as hydrocortisone In pityriasis rosea, a common self-limiting
Dose: Scabies and body lice, apply cream over POM VIREST® (Hovid) or betamethasone applied topically, are appro- dermatosis that is probably of infective origin,
whole body and wash off after 8–12 Cream, Aciclovir 5%; white opaque cream. priate for treating insect stings. calamine lotion helps to relieve pruritus in
hours; if hands washed with soap Pack: 5 g; 10 g (in tubes). ATOPIC DERMATITIS most cases. If it does not, topical application
within 8 hours of application, treat of hydrocortisone in a concentration not
POM ZOVIRAX® (GSK) Atopic dermatitis (or eczema) is a common skin
again; repeat application after 7 days. Cream, Aciclovir 5%. exceeding 1% may be tried.
disorder, which mainly occurs in infants and
Head lice, apply lotion to clean damp
children; it is associated with intense itching,
hair and rinse off after 10 minutes. IDOXURIDINE BETAMETASONE.
with areas of red skin. Pruritus may be partially
OTC Permethrin (WMF 13.6) Indications: Severe herpetic infections of relieved by applying astringent aluminium Indications: Severe inflammatory skin condi-
Cream, Permethrin 5%. the skin. diacetate (section 15.3) lotion to exudative tions inluding contact dermatitis, atopic der-
Lotion, Permethrin 1%. Precautions: Pregnancy, breast-feeding; matitis (eczema), seborrhoeic dermatitis, lichen
lesions and emollients to lichenified plaques.
OTC Permethrin (EDL 12.7) solution in DMS should not be used close to Topical hydrocortisone should be applied planus, psoriasis (under specialist supervision),
Cream, Permethrin 5%. the eyes. in short courses of 1–2 weeks to treat even intractable pruritus.
Lotion, Permethrin 1%. Adverse effects: Stinging on application. mild areas of involvement. The use of topical Contra-indications: Untreated skin infections,
Dose: Apply to the affected area 4 times daily betamethasone should be considered in the broken skin, rosacea, acne, perioral dermatitis.
15.1.4 Antiviral preparations for 3-4 days. treatment of persistent localized dermatitis in Precautions: Children (avoid prolonged use
Aciclovir cream is indicated for the treatment POM Idoxuridine (EDL 5.11) adults. Topical antihistamines are not effective and use under specialist supervision); psoriasis
of initial and recurrent labial and genital Solution, Idoxuridine 5% in dimethylsulphoxide; for and should be avoided because of the risk of (may precipitate severe pustular psoriasis on
herpes simplex infections. However, systemic external application. sensitization. However, a sedative antihista- withdrawal; avoid in widespread plaque psoria-
treatment is necessary for buccal or vaginal mine can be given at night to calm pruritus and sis); adrenal suppression if used on a large area
infection and herpes zoster (shingles) infection. facilitate sleep (section 8.1). A secondary infec- of the body or for a long time, particularly with
tion, often involving Staphylococcus aureus, an occlusive dressing; avoid use on the face for
650 | 15.2 Anti-inflammatory and antipruritic drugs 15.2 Anti-inflammatory and antipruritic drugs | 651
more than 7 days; secondary infection requires POM BETATOP® (Embassy) BETAMETASONE plus CLIOQUINOL Cream, Betametasone, Neomycin.
treatment with an appropriate antimicrobial. Cream, Betametasone 0.05%. Therapeutic category: Corticosteroid/anti- Pack: 15 g.
Adverse effects: Exacerbation of local infec- Pack: 30 g.
bacterial POM BETNOVATE-N® (GSK)
tion; local atrophic changes particularly on the POM BETNOVATE® (GSK) Pharmacology: Betamethasone valerate is an Cream, Betametasone (as valerate ester) 0.1%,
face and in skinfolds, characterized by thinning Cream, Betametasone (as valerate ester) 0.1%; white active topical corticosteroid which produces a neomycin sulfate 0.5%; smooth white water mis-
of the dermis, depigmentation, dilatation of water-miscible cream in tubes, rapid response in those inflammatory derma- cible cream.
superficial blood vessels and formation of Pack: 15 g; 30 g; 100 g. Pack: 15 g; 30 g (in tubes).
toses that are normally responsive to topical
striae; contact dermatitis; perioral dermatitis; Ointment, Betametasone (as valerate ester) 0.1%, Ointment, Betametasone (as valerate ester) 0.1%, ne-
white, paraffin-based ointment.
corticosteroid therapy, and is often effective in omycin sulfate 0.5%; white paraffin-based ointment
acne at site of application; suppression of the the less responsive conditions such as psoriasis.
Lotion, Betametasone (as valerate ester) 0.1%; white Pack:15 g; 30 g (in tubes)
hypothalamic-pituitary-adrenal axis with pro- translucent aqueous fluid in bottles. Clioquinol is an anti–infective agent which has Lotion, Betametasone (as valerate ester) 0.1%, neo-
longed or widespread use (particularly under Pack: 20 mL. both antibacterial and anticandidal activity. mycin sulfate 0.5%; white aqueous translucent fluid.
occlusion); hypertrichosis reported. Indications: Inflammatory skin conditions Pack: 20 mL (in bottle).
Advice to patients: Apply sparingly to affected POM BMN® (Jubilee)
Cream, Betametasone (as valerate) 0.1% w/w, Ne- where secondary bacterial and/or fungal in- POM DERZID-N® (Mark)
areas and gently rub in until it disappears; not fection is present, suspected, or likely to occur
omycin sulfate 0.5% w/w, Chlorocresol 0.1% w/w Cream, Betamethasone 0.1 g, neomycin 0.30 g
for use on broken skin; do not apply to wet skin (as preservative). such as in eczema, psoriasis, neurodermatoses, Pack: 15 g
unless directed; do not apply to face or inguinal Pack: 20 g tube. seborrheic dermatitis, contact sensitivity reac-
areas; discontinue use and notify physician if POM METAZONE-N® (Fidson)
tions; also in secondarily infected insect bites
skin irritation or ulceration occurs. POM TEMPROSONE® (Orange Drugs) Cream, Betametasone 1.0 mg, neomycin 5.0 mg.
Cream, Betamethasone (as dipropionate) 0.05%; in and anal and genital intertrigo. Pack: 20 g tube.
Nursing action: Contra-indications, Precautions, etc: see
a water-washable cream base.
• Wash the skin gently; rub medication in gently under Betamethasone. POM NEO-BETASONE® (Hovid)
Pack: 30 g (in tube).
to prevent damage to skin, leaving a thin coat. If Cream, Betametasone (as 17-valerate) 0.1%, neo-
Advice to patients: See under Betamethasone.
EMDEX
the area is hairy, part the hair and apply directly Compound preparations mycin sulfate 0.5%.
to lesion.
Dose: Small quantity applied to the affected Pack:15 g.
POM BEGECIN® (JB Pharma) area 2-3 times daily until improve-
• Avoid application near eyes, mucous membranes
Cream, Beclomethasone dipropionate 0.025%, ment occurs; then, once daily or less POM TRIDERMIX-G® (Miraflash)
or in ear canal; do not apply on broken skin or in
gentamicin sulphate 0.2%, clotrimazole 1.0%, for maintenance. Cream, Betamethasone valerate BP 0.05%, Neomycin
areas of infection.
iodochlorohydroxyquinoline 2.0%; white thick sulphate BP 0.5%, Tolnaftate USP 1.0, Iodochlor-hy-
• Inform patient that the gel may cause mild,
soft mass. POM BETNOVATE-C® (GSK) droxyquinoline (Clioquinol) BP 1.0%.
transient stinging especially if used on or near
Pack: 1 x 30 g Cream, Betametasone (as the valerate ester) 0.1%, Pack: 30 g (in tube).
excoriated skin due to alcohol content of vehicle.
clioquinol 3%; smooth, straw-coloured water-mis-
• Prolonged or excessive use as well as occlusive POM DEMA® (Pharmabox) cible cream. + Clotrimazole
dressings can enhance systemic absorption. Cream, Clotrimazole 10 mg, betamethasone Ointment, Betametasone (as the valerate ester) 0.1%, POM BAFAMA® (Seagreen)
• Teach patient to stop drug and inform physician if dipro-pionate 0.64 mg, gentamicin sulfate 1 mg per clioquinol 3%; white or pale, straw-coloured paraffin Cream, Clotrimazole 1.0%, betamethasone (as dipro-
he develops signs of systemic absorption, skin ir- g; milky white topical cream. based ointment. pionate) 0.05%, Neomycin sulfate 0.5%.
ritation or ulceration, hypersensitivity, or infection. Pack: 15 g; 20 g; 450 g.
Pack: 15 g; 30 g (in tubes).
• Avoid use of plastic pants or diapers that are
tight-fitting on treated areas in young children to
POM DERZID-C® (Mark) BETAMETASONE plus NEOMYCIN
POM FUNBACT-A® (Greenlife)
Cream, Betamethasone valerate 0.1 g, clotrimazole Therapeutic category: Corticosteroid/anti-
minimize systemic absorption. Cream, Clotrimazole 1.0%, betamethasone (as
1g
• It is important not to put occlusive dressing for bacterial dipropionate) 0.05%, neomycin (as sulfate) 0.5%.
Pack: 15 g
a long time; it should be avoided in infections or Pharmacology: Betametasone valerate is an Pack: 15 g; 30 g.
with weeping or exudative lesions. Guaze dressings POM DIGICLOGE® (Digitall) active topical corticosteroid used in inflamma- Dose: Apply thinly and evenly to the affected
are preferable. Cream, Betamethasone (as dipropionate) 0.10%, tory dermatoses. Neomycin sulfate is a broad area 2-3 times a day with a gentle rub.
• Treatment should be continued for a few days after clotrimazole 1.0%, gentamicin (as sulfate) 0.10%; spectrum bactericidal antibiotic effective POM NEOSKIN® (Elbe)
clearing of lesions to prevent recurrence. cream base.
against the majority of bacteria commonly Cream, Clotrimazole 1.0%, betamethasone (as
Dose: Inflammatory skin conditions, ADULT Pack: 15 g; 20 g.
associated with skin infections. dipropionate) 0.5%, neomycin (as sulfate) 0.5%; in
and CHILD over 2 years of age, apply POM EPIDERM® (Shalina) Indications: Severe inflammatory skin disorders cream base.
small quantity to the affected area Cream, Betamethasone dipropionate 0.643 mg, as for betamethasone but where prophylaxis Pack: 15 g; 30 g
1–2 times daily until improvement Gentamicin s(as sulphate) 1 mg, Tolnaftate 10 mg, against secondary bacterial infection is re- POM TRIBACT® (Geneith)
occurs, then less frequently. Iodochlorhydroxyquinoline 10 mg, chlorocresol
quired. Cream, Clotrimazole 1%, betamethasone, neomycin.
(preservative) 1 mg.
POM Betametasone (WMF 13.3) Contra-indications, Precautions, etc: See Pack: 30 g.
Pack: 15 g; 30 g.
Cream or ointment, Betametasone (as valerate) 0.1% under Betamethasone.
Lotion, Betamethasone dipropionate 0.643 mg,
POM Betametasone (EDL 12.4) Gentamicin sulphate equiv. to Gentamicin base 1 Advice to patients: See under Betamethasone. CALAMINE
Cream or Ointment, Betametasone (as valerate) 0.1%. mg, Tolnaftate 10 mg, Iodochlorhydroxyquinoline Dose: Small quantity applied to the affected Indications: Mild pruritus.
10 mg, chlorocresol (preservative) 1 mg. area 2-3 times daily until improve- Dose: Mild pruritus, apply liberally 3–4 times
POM BETACYLIC® (Neros)
Pack: 30 mL. ment occurs; then, once daily or less
Ointment, Betametasone dipropionate 0.0075 g, daily.
Salicylic acid 0.45 g per 15 g. POM GENTAMESON® (Neros) for maintenance.
OTC Calamine (WMF 13.3)
Pack: 15 g (in tube). Cream, Betamethasone dipropionate 0.64 mg, POM Betamethasone plus Neomycin (Drugfield) Lotion, Calamine.
Clotrimazole 10 mg, Gentamicin 1 mg. Cream, Betametasone, neomycin.
POM Betamethasone (Drugfield)
Pack: 20 g Pack: 20 g. OTC Calamine (EDL 12.4)
Cream, Betamethasone (as valerate ester) 0.1%
Lotion, Calamine
Pack: 20 g POM BETAVEL-N® (Strides Vital)
652 | 15.2 Anti-inflammatory and antipruritic drugs 15.2 Anti-inflammatory and antipruritic drugs | 653
See also section 15.3 (Astringents) for Calamine plus Gel, Clobetasol propionate 50 mg. herpes simplex. Cream, Diflucortolone valerate 0.1%, Chlorquin-
Zinc oxide preparations. Pack: 30 g. Precautions: Pregnancy, infants, long term adol 1%.
and extensive use; avoid occlusive dressing. Pack: 15 g tube.
Clobetasol + Gentamicin + Miconazole
Adverse effects: Skin irritation, dryness of skin. Indications: Steroid-responsive dermatoses compli-
CLOBETASOL POM 3-BETA Cream® (Beta Drugs) cated by bacteria or monilial infection.
Therapeutic category: Corticosteroid See also under Betamethasone.
Cream, Clobetasol propionate 0.05%, miconazole
Pharmacology: Clobetasol propionate is a nitrate 2.0%, neomycin sulphate 0.5% per gm. Advice to patients: See under Betamethasone
DIFLUCORTOLONE plus ISOCONAZOLE
very active topical corticosteroid which is of Pack: 30 gm Dose: Apply sparingly twice daily, continuing
several days after the disappearance Indications: Combination of corticosteroid
particular value when used in short courses Indications: Dermatoses where secondary bac-
terial infection and/or fungal infection is present, of symptoms. and antimycotic topical preparation indicated
for the treatment of more resistant dermatoses. in initial or interim treatment of dermato-
suspected or likely to occur. e,g psoriasis(excluding
Indications: Short-course treatment of more POM BEYTUCEN® (Orange Drugs) mycoses accompanied by inflammatory or
wide spread plaque psoriasis), recalcitrant eczema.
resistant dermatoses e.g. psoriasis, recalcitrant Cream, Dexamethasone 0.04 g, Clotrimazole 1 g eczematous skin conditions.
Dose: Apply sparingly to the affected area once
eczemas, lichen planus, discoid lupus erythe- per 100 g.
or twice daily until improvemente occurs. Contra-indications, Precautions, etc: See
matosus, and other conditions which do not Pack: 20 g tube
POM BG Cream (BG Pharma) under Betamethasone.
respond satisfactorily to less potent steroids. POM BIOCOTEN® (Drugfield) Dose: Apply thinly 1-2 times daily; not
Cream, Clobetasol propionate 0.05%, gentamicin
Contra-indications, Precautions, etc: See Cream, Dexamethasone, gentamicin, clotrimazole exceeding 15 days, then change over
sulphate 0.1%, miconazole nitrate 2%, chlorocresol
under Betamethasone. Pack: 20 g.
0.10%. to isoconazole cream alone.
Advice to patients: Apply sparingly in light Pack: 15 g POM KEMI®(Jawa)
film; rub in lightly; do not use tight-fitting dia- POM TRAVOCORT® (Bayer Schering)
Cream, Clotrimazole 0.15%, beclomethasone
POM NOSACORT® (Nosak) Cream, Diflucortolone valerate 1 mg, isoconazole
pers or plastic pants on children being treated dipro-pionate 0.00375%.
Cream, Clobetasol propionate 0.05% w/w, Micona- nitrate 10 mg per g.
in the diapper area; use only as prescribed and zole nitrate 2.0% w/w, Gentamicin sulfate 0.1%
Pack: 15 g tube.
Pack: 15 g tube.
for no longer than the period prescribed; avoid
EMDEX
w/w; in tube. POM TRICUTEN® (SKG)
contact with eye; notify physician if condition Indications: Dermatosis where secondary bacterial Cream, Clotrimazole 10 mg, Gentamicin 1 mg, Dex- FLUOCINOLONE
being treated persists or worsens; do not use and/or candidal infection is present, suspected or amethazone 0.4 mg per g.Pack: 20 g. Therapeutic category: Corticosteroid.
on open wounds. likely to occur, as when using occlusive dressing
such as psoriasis.
POM VECUTEN® (Gemini) Pharmacology: Fluocinolone is a synthetic
Nursing action:
Dose: Apply to the affected areas 1-2 times daily.
Cream, Dexamethasone 6 mg, clotrimazole 150 mg, glucocorticoid used topically in the treatment
• Warn patient not to use for longer than 14 con-
neomycin sulfate 96.8 mg per 15 g. of various skin disorders.
secutive days because drug is a very potent and
Pack: 15 g in tube. Indications: Local inflammatory, pruritic and
fluoridated corticosteroid. CLOBETASONE
• Not recommended for children under 12 years. allergic conditions of the skin and mucosa such
Therapeutic category: Topical corticosteroid DEXAMETHASONE plus NEOMYCIN
• Avoid use of occlusive dressings; do not bandage, as atopic dermatoses (e.g. eczema), contact
Indications: Eczema and dermatitis of all types
cover or wrap the treated area of skin. Therapeutic category: Anti-inflammatory/ dermatitis, psoriasis in all its forms; intertrigo,
including atopic eczema, photodermatitis,
• See also under Betamethasone. antiallergic/antibiotic otitis externa.
Dose: Apply sparingly 1-2 times daily until otitis externa, primary irritant and allergic
Indications: Primary inflammation of the Precautions: Infants and adolescent girls when
improvement occurs; up to 4 weeks. dermatitis(including napkin rash), intertrigo,
skin including pyoderma; allergic dermatoses extensive or prolonged treatment is envisaged.
prurigo nodularis, seborrhoeic dermatitis and
POM Clobetasol (EDL 12.4/Restricted List) including dermatitis, eczema, pruritus. Advice to patients: See under Clobetasol.
insect bite reactions.
Cream or Ointment, Clobetasol (as propionate) Contra-indications: Skin turberculosis, vacci- Dose: Apply a small quantity to the affected
0.05%. nation, varicella; see also under Betamethasone. area 2-3 times daily.
under Betamethasone.
Dose: Apply as a thin layer to the affected
POM DERMOVATE® (GSK) Advice to patients: See under Clobetasol. POM Fluocinolone (EDL 12.4/Restricted List)
Ointment, Clobetasol propionate 0.05%; white
area 1-3 times daily.
Dose: Apply sparingly to the affected area Cream or Ointment, Fluocinolone (as acetonide)
paraffin-based ointment. up to 4 times daily until improve- POM BIVACYN-N® (Taylek) 0.025%.
Pack:25 g; 100 g. ment occurs, reducing according to Cream or Ointment, Dexamethasone 0.1%, Neomycin
POM SYNALAR® (Reals)
Scalp application, Clobetasol propionate 0.05%, sulfate 0.5%.
response. Cream and Ointment, Fluocinolone acetonide
isopropyl alcohol 50%; transparent, slightly gelled Pack: 20 g (in tube).
0.025% w/w; both white.
solution. POM EUMOVATE® (GSK)
Pack: 15 g tube
Cream, Clobetasone butyrate 2.05%; white emolient DIFLUCORTOLONE
POM HYPROGEL® (Orange Drugs)
water-miscible cream. With Clioquinol
Gel, Clobetasol propionate 0.05%. Indications: All dermatoses in which corti-
Ointment, Clobetasone butyrate 2.05%; white par-
coids are indicated; Psoriasis vulgaris; first POM SYNALAR C® (Reals)
POM NEUTROTONE® (Orange Drugs) affin-based ointment.
degree burn; insect bite; dyshidrosis; contact Cream and Ointment, Fluocinolone acetonide
Cream, Clobetasol propionate 0.050 g, glyceryl
dermatitis. 0.025%, clioquinol 3%
monostearate q.s. CLOTRIMAZOLE plus DEXAMETHASONE Pack: 15 g (in tube).
Pack: 100 g Contra-indications, Precautions, etc: See
Therapeutic category: Anti-eczematous
under Betamethasone.
POM TEMPOVATE® (Orange Drugs) Indications: Inflammation and infection of the HYDROCORTISONE
Cream, Clobetasol propionate 0.05%; white wa- Dose: Apply thinly 1-2 times daily for up to
skin particularly those caused by fungi and/or Indications: Contact dermatitis, atopic der-
ter-miscible cream. 4 weeks.
bacteria such as various forms of eczema, in- matitis (eczema), lichen planus; intractable
Pack: 25 g (in tube). tertrigo, non-specific pruritus, neurodermatitis POM NERISONE® (CHI/Schering)
Gel, Clobetasol propionate 0.05%; slight pink in pruritus and phototoxic reactions, including
,pyodermia, pustular dermatitis. Cream or Ointment, Diflucortolone valerate 0.1%.
appearance. polymorphic light eruptions and actinic pru-
Contra-indications: Tuberculosis of the skin, Pack: 15 g tube.
Pack: 25 g (in tube) rigo; short-term treatment of psoriasis of the
viral infections of the skin e.g. chickenpox, POM NERISONE C® (CHI/Schering) face and flexures.
POM TENOVATE® (Embassy)
654 | 15.2 Anti-inflammatory and antipruritic drugs 15.3 Astringents | 655
Contra-indications: Untreated skin infections, HYDROCORTISONE plus daily. Not exceeding 12 weeks in Solution, Aluminium diacetate 13%; to be diluted
broken skin, rosacea, acne, perioral dermatitis. OXYTETRACYCLINE adults and 4 weeks in children.
Precautions: Children (avoid prolonged use); Therapeutic category: Anti-inflammatory/ CALAMINE plus ZINC OXIDE
POM ADVANTAN® (Bayer Schering)
occlusive dressings increase penetration anti-infective. Indications: Relieves the discomfort due to
Cream, Methylprednisolone aceponate 0.1%
into keratinized lesions; secondary infection Pharmacology: Oxytetracycline is a potent Pack: 15 g (tube). rashes, stings, insect bites, and other similar
requires treatment with an appropriate anti- broad spectrum antibiotic whereas hydrocor- Recommended for acute and weeping stages of skin conditions such as measles; pruritus.
microbial. tisone has anti-inflammatory, antipruritic and eczema, for very greasy skin and for use on exposed Dose: Apply to the to the affected parts
Adverse effects: Exacerbation of local infec- vasoconstrictive actions. or hairy parts of the body. with the help of cotton wool or any
tion; atrophic changes (see under Betametha- Indications: Cutaneous infections; atopic der- Ointment, Methylprednisolone aceponate 0.1%. suitable applicator
sone) less likely with mild corticosteroids, but matitis; contact dermatitis; nonspecific pruritus Pack: 15 g (tube).
Recommended for skin conditions which are neither OTC Calamine plus Zinc Oxide (EDL 12.5)
infants and children particularly susceptible; of the anus, vulva, and scrotum.
weeping nor very dry; it makes the skin slightly Lotion or Plaster, Calamine, Zinc oxide.
contact dermatitis; perioral dermatitis; hyper- Contra-indications: Acute herpes simplex,
greasy without retaining warmth and fluid. OTC Calamine Lotion (BCN)
trichosis reported. tuberculosis of the skin, fungal diseases of the
skin, hypersensitivity to the drug. Lotion, Calamine 15.0 g, zinc oxide 5.0 g phenol 0.42
Advice to patients: See under Betamethasone. METHYL SALICYLATE
Precautions: Discontinue if irritation occurs; g, bentonite 3.0 g, sodium citrate 0.5 g, glycerol 6.3
Dose: Inflammatory skin conditions, apply a g; thick pink coloured suspension.
small quantity to the affected area over-growth of nonsusceptible organisms; See under section 2.5
Pack: 100 mL.
1–2 times daily until improvement pregnancy.
occurs, then less frequently. Adverse effects: Local irritations such as OTC Calamine Lotion (Evans)
PANTHENOL
burning, itching, dryness, allergic contact Lotion, Calamine 15.0 g, zinc oxide 5.0 g, phenol 0.43
POM Hydrocortisone (WMF 13.3) Indications: To support wound healing and g, bentonite 3.0 g, sodium citrate 0.5 g, glycerol 6.3
dermatitis.
Cream or ointment, Hydrocortisone (as acetate) 1%. epithelization. g; thick pink coloured suspension.
Advice to patients: See under Betametasone.
Dose: Apply thinly to the affected area 1-3 Pack: 100 mL.
EMDEX
POM Hydrocortisone (EDL 12.4) Dose: Apply a small amount to the affected
Cream, Ointment, Hydrocortisone acetate 1%. times daily. OTC Galways Calamine Lotion (SKG)
skin areas 2-4 times daily.
OTC BEPANTHEN® (Swipha) Lotion, Calamine 15 g, zinc oxide 5 g, liquified phenol
POM CORTISONE® (Hovid) POM TERRA-CORTRIL® (Pfizer)
Cream, Panthenol 5%; white non-sticky odourless 0.5 mL, bentonite 3 g, sodium citrate 0.5 g, glycerol
Ointment, Hydrocortisone 1%. Ointment, Oxytetracycline (as HCl) 30 mg, Hydrocor-
cream. 5 mL per 100 mL; thick pink coloured suspension.
Pack: 15 g. tisone 10 mg per g.
Pack: 30 g. Pack: 100 mL.
POM Hydrocortisone (Al-Tinez) Pack: 5 g.
OTC Moko Calamine (New Healthway)
Cream, Hydrocortisone acetate 200 mg
Pack 20 g METHYLPREDNISOLONE 15.3 Astringents Lotion, Calamine 15 g, zinc oxide 5 g, bentonite 3
Aluminum acetate is a topical astringent used g, phenol 0.5 mL per 100 mL; thick pink coloured
POM Hydrocortisone (Drugfield) Pharmacology: Topical methylprednisolone suspension.
is effective in suppressing inflammatory and as an antiseptic for various skin conditions
Cream, Hydrocortisone.
allergic skin reactions as well as reactions as- including suppurating superficial wounds and OTC Calamine Lotion (Gauze)
Pack: 15 g.
tropical ulcers, and the lesions produced by Lotion, Calamine powder 15 gm, zinc oxide 5 gm, liq-
sociated with increased cellular regeneration,
POM LABOHYDRO® (Embassy) pemphigus and impetigo. uid phenol 0.5 mL, sodium citrate 0.5 gm, bentonite
Cream, Hydrocortisone acetate 1%, chlorocresol (as leading to regression of the objective symp- 3.0 gm, glyerine 5.0 mL per 100 mL.
preservative) 0.1%. toms (erythemia, oedema, thickening of the Pack: 100 mL
skin, coarseness of the skin surface) and the ALUMINIUM DIACETATE
Pack: 20 g
subjective complaints (itching, burning, pain). Indications: Wet dressings to assist healing OTC Calamine Lotion (Nomagbon)
of suppurating superficial wounds, tropical Lotion, Calamine 15 g, zinc oxide 5 g, bentonite 3
HYDROCORTISONE plus GENTAMICIN Indications: Endogenous eczema (atopic
g, sodium citrate 500 mg, liquid phenol 0.50 mL,
dermatitis, neurodermatitis); contact eczema; ulcers and eczematous skin lesions; removal
See under preparations below sorbitol 5 mL; pink liquid.
degenerative, dyshidrotic, or vulgar eczema; of adherent crusts. Pack: 100 mL (in PET bottle).
eczema in children. Precautions: Avoid use of plastic or rubber
POM DRUGENT HC®(Drugfield) OTC Calamine Lotion (Topway)
Cream, Gentamicin (as sulphate) 3.5 mg, hydrocor- Contra-indications: Tuberculous or syphilitic occlusive dressings.
Dose: Suppurating superficial wounds and Lotion, Calamine 15 g, zinc oxide 5 g, phenol crys-
tisone (as acetate) 10 mg. processes in the affected area; viral diseases tals 0.42 g, bentonite 3 g, sodium citrate 0.50 g,
Pack: 20 g (e.g. vaccinia, chicken-pox, shingles); rosacea. tropical ulcers, apply dressings soaked
glycerol 6.30 g.
Precautions: Pregnant and lactating women; in 0.65% solution for 30–120 minutes Pack: 100 mL.
HYDROCORTISONE plus NEOMYCIN avoid large area or prolonged use; skin diseases daily, changing dressings every 5–15
Indications: Inflammatory dermatoses with involving bacterial and/or fungal infection minutes; tropical ulcers also require 15.4 Preparations for acne
secondary bacterial infection. may require additional therapy; avoid contact treatment with procaine benzylpen-
icillin for 2–4 weeks (section 9.1.1.1). 15.4.1 Topical preparations for acne
Advice to patients: See under Betamethasone. with eyes when applying to the face; ointment
Impetigo, apply dressings soaked in 15.4.2 Oral preparations for acne
Dose: Apply sparingly 2-3 times daily should be used instead of cream if excessive
skin drying occurs during prolonged use. 0.65% solution until superficial crusts Acne vulgaris
POM Hydrocortisone plus Neomycin (EDL 12.4) can be separated.
Adverse effects: Local skin reactions such as Acne is a disorder of the pilosebaceous follicles
Ointment or Cream, Hydrocortisone 0.5-1%, Neo- Dilution of Aluminium Diacetate Solution 5%:
mycin 0.25-0.5%. itching, burning, erythema or vesiculation. and typically first appears during puberty when
Rarely folliculitis, increased growth of body hair Dilute 1 in 7.7 with water for 0.65% solution.
androgenic stimulation triggers excessive pro-
(hypertrichosis), perioral dermatitis, allergic OTC Aluminium diacetate (WMF 13.4) duction of sebum. Mild acne is characterized
skin reactions. Solution, Aluminium acetate 5%. by comedones and a few pustules which heal
Advice to patients: See under Betamethasone. OTC Aluminium Diacetate (EDL 12.5) without scarring, and usually responds to
Dose: Apply thinly to the affected area once
656 | 15.4.1 Topical preparations for acne 15.4.2 Oral preparations for acne | 657
topical therapy alone. In moderate acne, where if excessive dryness or peeling occurs, reduce cin sulfate exerts an antibacterial effect and Thoroughly wash hands after applying; avoid
there are more extensive pustules causing mild dose, frequency or concentration; if excessive avoids the development of cutaneous superin- hydration of skin immediately before applying;
scarring, oral antibiotics such as a tetracycline stinging or burning occurs, remove with mild fections. Aluminium chlorohydroxide hydrate minimize exposure to sunlight; avoid washing
or erythromycin (section 9.1.2.4) are commonly soap and water; resume use the next day; if causes lesions to dry. Sulfur has keratolytic and face more frequently than 2-3 times daily; if se-
used. In severe acne, widespread pustules are excessive redness or irritation occurs, discon- antifungal properties. vere irritation occurs, discontinue medication
accompanied by nodular abscesses and cysts, tinue use. Avoid excessive sunlight, sun lamps, Indications: Treatment of acne vulgaris, acne temporarily and adjust dose when irritation
requiring systemic treatment with estrogens, or other topical medications unless directed rosacea and seborrhoeic dermatitis; control of subsides; avoid using topical preparations
antiandrogens, or retinoids [not included on by a physician. skin irritation and eruptions that often occur with high alcoholic content during treatment
WHO Model List]. Since scarring of the skin Nursing action: after shaving. period such as shaving lotion; do not exceed
resulting from severe nodular acne causes • Observe for signs of systemic infection; granulation Contra-indications: Hypersensitivity; tuber- prescribed dose.
major distress, acne should always be treated may indicate effectiveness. culosis of the skin, herpes simplex, vaccinia, Nursing action:
as soon as possible. Exposure to substances Dose: Acne, initially apply to clean skin on al- varicella. • Cleanse area thoroughly before application. Advise
suspected of causing or aggravating the con- ternate days, increasing frequency to Precautions: Due to potential for nephrotox- patient to wash face with a mild soap no more than
dition should be avoided. Systemic treatment 1–2 times daily as tolerance to irritant icity, ototoxicity and super-infection, avoid 2-3 times daily; avoid strong or medicated cosmet-

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Table of Contents

Quick & Easy to Navigate

Copyright © EMDEX Limited

Jointly published by:

Web address: www.EmdexOnline.com

Y o utn!ers EMDEX Vols 1 & 2

Dear EMDEX User,

Assistant Editor (Trainee) Drug Information Representative 1.6 Antiparkinson drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51

Nigeria’s National Drug Essential drugs

Rational use of drugs

1. Central nervous system 1.1 Drugs used in anxiety and insomnia.

POM PLACOMP® Retard (Visko)

10. Endocrine system 10.1 Antidiabetic drugs

11. Drugs used 11.1 Drugs used in obstetricts PREMATURE LABOUR

urinary-tract TERMINATION OF PREGNANCY ECLAMPSIA AND PRE-ECLAMPSIA

POM PHARMALENT® (Pharmabox) POM Hypromellose (Alpha)

15. Dermatological drugs

Вам также может понравиться

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eEMDEX 2014-2015b

Загружено:

Авторское право:

Доступные форматы

Table of Contents

Quick & Easy to Navigate

Copyright © EMDEX Limited

Jointly published by:

Web address: www.EmdexOnline.com

Y o utn!ers EMDEX Vols 1 & 2

Dear EMDEX User,

Assistant Editor (Trainee) Drug Information Representative 1.6 Antiparkinson drugs. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 51

Nigeria’s National Drug Essential drugs

Rational use of drugs

1. Central nervous system 1.1 Drugs used in anxiety and insomnia.

POM PLACOMP® Retard (Visko)

10. Endocrine system 10.1 Antidiabetic drugs

11. Drugs used 11.1 Drugs used in obstetricts PREMATURE LABOUR

urinary-tract TERMINATION OF PREGNANCY ECLAMPSIA AND PRE-ECLAMPSIA

POM PHARMALENT® (Pharmabox) POM Hypromellose (Alpha)

15. Dermatological drugs

Вам также может понравиться

1. Central nervous system 1.1 Drugs used in anxiety and insomnia.

10. Endocrine system 10.1 Antidiabetic drugs

11. Drugs used 11.1 Drugs used in obstetricts PREMATURE LABOUR

15. Dermatological drugs