Over the Counter (OTC) Drugs

Clinical Pharmacology Seminar

Department of Pharmacology and Toxicology,

Faculty of Pharmacy
Vladimir Patras, PharmD, MBA

American College of Preventive Medicine

 OTC – What is it?

 “Over the Counter”

 Non-prescription medicines
 Medicinal products marketed as drugs - regulatory
approval (marketing authorization) is needed, which is
issued on base of proof of safety and efficacy (legal or
regulatory meaning)
 In broader sense all non-prescriptional medicines
including traditional herbal medicines or nutritional
supplements (pharmaceutical care meaning)
 Need not to be dispenced by pharmacist, in some
countries sold also outside pharmacies
 Directive 2001/83/EC
Medicinal products shall be subject to medicinal
prescription where they:
 Are likely to present danger, even when used
correctly
 Are frequently and to very wide extent used
incorrectly
 Contain substances which require further
investigation
 Are to be administered parenterally
Non-prescription medicines when none of these
criteria apply
 Criteria for OTC Designation

 Low toxicity and low risk of serious adverse reactions

 Not to mask any underlying condition or increase
resistance
 Correct self-assessment of the condition
 No known incorrect use
 Risk to public health limited in case of misuse
 Drugs are usually approved as prescription only first
and just after they prove safety in clinical use they are
recategorized as OTC
Broad Therapeutic Classes of OTC
Medications
 There are over 80 therapeutic categories of OTC
drugs which can be grouped in 12 broad
therapeutic classes
 Analgesics and antipyretics
 Cold, cough, and allergy products
 Night-time sleep-aids
 Gastrointestinal products
 Dermatologic products
 Other topical products (including dermal and
vaginal antifungals, anorectal medications, head
lice products, and otics)
Broad Therapeutic Classes of OTC
Medications
 Ophthalmic product
 Oral health care products
 Menstrual products
 Nicotine replacement products
 Weight loss aids
 Contraceptives
 Benefits of OTC availability include:
 Direct, rapid access to effective medicines
 Wide availability
 Decreased healthcare system utilization (fewer
physician visits, lower healthcare system costs)
 Allowing individuals to be in charge of their own
health
 However, there are risks associated with OTC
use:
 Incorrect self-diagnosis, delaying diagnosis, and
treatment of serious illnesses (delay in seeking
advice from a healthcare professional)
 Increased risk of drug-drug interactions
 Increased risk of adverse events when not used
appropriately
 Potential for misuse and abuse
 Clarifying Terminology
 Drugs/OTC Drugs
 Substances intended for use in the diagnosis, cure
mitigation, treatment, or prevention of disease. OTC
drugs are defined as safe and effective for use by
the general public without a doctor’ s prescription.
 Dietary supplements (including Herbal
Ingredients)
 A product taken by mouth that contains a “dietary
ingredient intended to supplement the diet.
Permitted ingredients of dietary supplements
include vitamins, minerals, herbs, and other
botanicals, and amino acids/
 Cosmetics
 “articles intended to be rubbed, poured, sprinkled,
sprayed on, introduced into, or otherwise applied to
the human body…for cleaning, beautifying,
promoting attractiveness, or altering the
appearance.”
 Another area of confusion: therapeutic error;
intentional misuse; intentional abuse
As defined by the American Association of Poison
Control Centers (AAPCC)

 Therapeutic error – an unintentional deviation

from a proper therapeutic regimen resulting in
the wrong dose, incorrect route of
administration, administration to the wrong
person, or administration of the wrong
substance
 Intentional misuse – an exposure resulting from
the unintentional improper or incorrect use of a
substance where the individual was likely
attempting to achieve a euphoric or
psychotropic effect
 Intentional abuse – resulting from the intentional
improper or incorrect use of a substance where
the individual was likely attempting to achieve a
euphoric or psychotropic effect.
 Switching

Switching = Move from prescriptional category into OTC

 Self-medication
 Treatment of common health problems with
medicines especially designed and labeled for
use without medical supervision and approved
as safe and effective for such use
 Desire of people to take responsibility for their
own health and to reduce health expenditure
 Importance of patient education,
pharmaceutical care
 Move toward self-medication has support of
governments/regulatory agencies
 Most commonly used OTC in the
US (2009)
 For oral ingestion
 Cough/cold and allergy remedies
 Analgesics
 Antacids and anti-gas products
 Laxatives
 Diarrhea remedies
 Most commonly used OTC in the
US (2009)
 For topical use
 Toothpaste
 Oral antiseptics and rinses
 First aid treatments including germicidal antiseptics
and topical hydrocortisone
 Lip remedies
 Eye care products
 Gastric Acidity and Gastroesophageal
Reflux Disease
Antacids
 Buffering gastric acid > raising acidity
 Aluminium hydroxide - MAALOX
 Calcium carbonate - TUMS

H2 antagonists
 Decrease acid production
 Ranitidine – ZANTAC, RANISAN
 Famotidine – FAMOTIDIN, QUAMATEL
 Exocrine Pancreatic Insufficiency
Takasidase
 Purified fungal (Aspergillus oryzae) enzymes
 Digestion of oligosaccharides and
polysaccharides
 ORENZYME
Purified animal pancreatin
 PANGROL, PANZYTRAT, KREON
 Constipation
Lactulose
 Disaccharide that draw water into bowel – osmotic action
 DUPHALAC

Bisacodyl
 Acts by irritating of colon
 BISAKODYL-K, FENOLAX
Sodium picosulfate
 GUTTALAX, REGULAX
 Diarrhea
Cloroxin, nifuroxazid
 Antibacterial effects - used in infectious diarrhea including traveler`s diarrhea
 ENDIARON

Loperamide
 μ opioid receptor agonist – decreasing smooth muscles motility
 IMODIUM

Intestinal Adsorbents – bind toxins in gastrointestinal tract

 Diosmectite – SMECTA
 Activated carbon - CARBOCIT, CARBOSORB
 Antimycotics (Antifungal Drugs)
Skin, nails, vaginal fungal infections
Nystatine
 Polyene antifungal used also in combinations
 FUNGICIDIN
Imidazoles
inhibition of ergosterol (component of fungal cell membrane) synthesis
 Clotrimazole – CANESTEN, CANDIBENE
 Ketoconazole – NIZORAL
 Others: Miconazole, Bifonazole, Oxiconazole
Allylamines
 Terbinafine - LAMISIL
 Disinfection, Antiseptics and
Antibiotics
Wounds/skin disinfiction
 Benzalkonium – DETTOL
 Carbethopendecinium bromide – SEPTONEX (aer deo)

Antiseptics for oral use

 Amylmetacresol, dichlorbenzyl alcohol – STREPSILS, NEO-ANGIN
 Chlorhexidine – SEPTOFORT, DRILL

Antibiotics
 Fusafungine – the only OTC antibiotic
 Used as spray for treatment of nasal and throat infection
 BIOPAROX
Nasal Preparations (Decongestants)
 Applied in nasal spray/drops to relieve nasal
congestion in rhinitis
 Vasoconstriction of blood vessels within the nasal
cavity
 Should not be taken longer than 3 days in a row

 Xylometazoline – OLYNTH
 Oxymetazoline – NASIVIN
 Tramazoline – MUCONASAL PLUS
 Nafazoline – SANORIN
 Allergies
Anihistamines
H1 antagonists
 Often used to relieve allergic rhinitis (hay fever). Neither loratadine nor
cetirizine are causing sedation
Loratadine
 CLARITINE
Cetirizine
 ZODAC, ZYRTEC, CETIRIZINE-SANDOZ

Corticosteroids
Beclometazone
 OTC products as nasal spray
 BECLOMET NASAL AQUA
 Vasoprotectives
Bioflavonoinds
 Troxerutin – CILKANOL, VENORUTON

Calcium dobesilate – DANIUM

Aescin
 Saponine isolated from the horse chesnut (Aesculus
hippocastanum)
 Induction of endothelial nitric oxide synthesis
 AESCIN, YELLON
 Analgesics (painkillers) and
antipyretics
Major classes
 Paracetamol
 Salicylates
 Non-steroidal anti-inflammatory drugs

 Most drugs of this group has both anti-inflammmatory

and antipyretic effects through inhibition of
biosynthesis of prostaglandins
 It is not recommended to use antypiretics in only
slightly elevated temperature
 Paracetamol
 Most widely used analgesic in the world, lacks anti-inflammatory properties
 Mechanism of action is disputed – COX 3 inhibition in brain (?)
 Preferred antipyretic agent in children, no side effects in gastrointestinal
tract, is not contraindicated in pregnancy (ASA is preferred in first trimester)
 Some studies suggested link between heavy paracetamol use in early
childhood and development of asthma. FDA issued Public Health Advisory
recommending use of cold and cough medicines in children under 2 years
only when necessary
 Possible liver and kidney damage in case of other liver/kidney disease or
high doses
 Combinations with caffeine, dimenhydrinate, phenylephrine,
pseudoephedrine, promethazine, guaifenesin, ascorbic acid
 PANADOL, PANADOL EXTRA, PARALEN, COLDREX, COLDREX HOT
REM, ATARALGIN, VALETOL
 Acetylsalicylic Acid (ASA)
 Most common salicylate is acetylsalicylic acid (ASA), others are
salycilamide, diflunisal
 Irreversible cycloooxygenase (COX) inhibition > suppression of
production of prostaglandins and tromboxanes (inflammation
inhibitors)
 Common side effects are gastrointestinal bleeding, ulcers and tinnitus
 Not used in children due to risk of Reye`s syndrome
 May be used in first and second trimesters of pregnancy if benefit
outweighs risk
 Often used in combinations with other drugs such as ascorbic acid,
caffeine, paracetamol, phenacetin
 ASPIRIN, ASPIRIN-C, ASPIRIN PROTECT, ACYLPYRIN,
ACYLCOFFIN, ACIFEIN, ALKA-SELTZER, ACIFEIN
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

Ibuprofen
 Indications include arthritis, dysmenorrhea, fever, migaine and other
conditions with involving inflammation. Investigational (clinical trials) use
include also Alzheimer and Parkinson diseases.
 BRUFEN, NUROFEN, IBALGIN
Naproxen
 Pain in rheumatic conditions, marketed as relieve in pain of teeth
 ALEVE, NALGESIN S
Diclofenac
 Treatment of pain of various origin – most commonly in rheumatism. It is
possible to use antipyretic effects but other substances are preferred in fever
 Beside oral administration topical use is common
 VOLTAREN ACTIGO, VOLTAREN EMULGEL, VERAL, DICLOBENE
 Joint, Connective Tissue and
Rheumatism OTC preparations
Other NSAIDs - Indometacin, Ketoprofen, Nimesulide (COX-2)
Combination of enzymes such as trypsin, bromelaine, papain has presumed
anti-inflammatory effect - WOBENZYME

Chondroitin sulfate, Glucosamine sulfate

 Often used in combination in treatment of osteoarthritis. They are
components of joint cartilage but have also anti-inflammatory effect
 CONDROSULF

Antioedema local preparations - Heparin

 Glycosaminoglycan used in ointments/gels in oedemas and bruises.
Anticoagulant effects
 LIOTON, HEPAROID
 Cough Medicines
Pharmacotherapy depends on type of cough
 Productive – mucolytics
 Non-productive – antitussics
 Opioid
 Non-opioid

 Mucolytics and antitusics shall not be used together

 FDA issued public health statement promoting
cautious use of cough medicines in children under 4
years
 Antitussics
Opioid
Dextromorphan
 Used in combinationS with other substances such as pseudoephedrine,
paracetamol
 COLDREX NITE, PARALEN PLUS
Non-opioid
Butamirate
 Used as drops or sirup, most common cough suppresant
 STOPTUSSIN, TUSSIN, SINECOD
Diphenhydramine
 Antihystamine with antitussic (sedative, anticholinergic and antiemetic)
effects, drawsiness is common side effect
 BENADRYL N
 Mucolytic Agents
Guaifenesin
 ROBITUSSIN EXPECTORANS
Acetylcysteine
 Potent mucolytic agent, antioxidative effect
 SOLMUCOL
Ambroxol
 Common mucolytic used as sirup or tablets
 MUCOSOLVAN, AMBROBENE
Bromhexine
 Metabolizes to ambroxol
 BROMHEXIN, BRONCHOSAN
 Contraception
Emergency (postcoital) contraception
Levonorgestrel in 1.5 mg dose
 Estimated effectiveness is 84 %
 ESCAPELLE

Local contraception – spremicides

Not efficient enough alone – should be complemented with other
form of contraception (barrier contraception)
 Nonoxynol – PATENTEX OVAL N
 Benzalkonium chloride – PHARMATEX
 Psychoactive OTC preparations
Sedatives
 Guaifenesin – moderate sedative effect - GUAJACURAN
 Valerian, Humulus and Lemon balm extracts

Antidepressants
 St. John wort – multiple drug interaction through cytochrome P450 induction

Nootropics
 Pirecetam – NOOTROPIL, PIRACETAM, OIKAMID
 Lecithin – phosphatidylcholine naturraly occuring in body with presumed
nootropic effects
 Vitamin and Mineral Supplements

 Many preparations are on the market, some of them

are marketed as drugs others as nutritional
supplements
 CENTRUM, GERIAVIT PHARMATON, REVALID
 Many nutritional supplements are associated with
various health claims but efficacy is not required to be
demonstrated in order to gain marketing authorization
for nutritional supplements
 Where to find information
Books

V. Foltán: Voľnopredajné lieky, 2002

Online Databases
 NobelPLUS – Slovak database of pharmaceutical products:
http://www.nobelplus.sk/
 MedlinePlus – service of U.S. National Library of Medicine and National
Institute of Health: http://www.nlm.nih.gov/medlineplus/druginformation.html

Industry Associations
 Association of the European Self-Medication Industry: http://www.aesgp.be
 Bottom Line
 OTC medications represent a diverse group of
widely available drugs. OTC use is ever
increasing and expected to continue to rise.
These drugs are safe and effective when used
as directed.
 However, physicians must be aware that some
people – with or without intention – use OTC
medications incorrectly.
 Bottom Line
 Instruct all patients on the sale and appropriate
storage and disposal of all types of medicines.
Stay abreast of trends in OTC usage,
therapeutic errors, misuse, and abuse.
 Routinely incorporate OTC conversations
during office visits. Each of these efforts will
help patients to get the maximum benefit out of
OTC use while minimizing the risks of incorrect
OTC use.
 Thank You For Your Attention !

 This presentation is published at

http://vpatras.blogspot.com

Stay
healthy….
 CHECK
1. Father of Modern Toxicology
2. The study of how a chemical causes toxic
effects by investigating its absorption,
distribution, and excretion
3. Toxicity can be defined as the relative ability of
a substance to cause ___ in living organisms.
4. Determines whether the effects of the
chemical are toxic, nontoxic or beneficial.
5. Routes of entry of a drug include ___, ___,
___, ___.
 Check
5) When are drugs needed to be prescribed? (3)
6) 5 general classifications of OTC drugs
7) 3 permitted ingredients of OTC
8)What is NSAIDs?
9) AAPCC