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Профессиональный Документы
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Classification
1. Antibiotic : Griseofulvin and antibiotic polyen (amfoterisin
B, nistatin, natamisin)
2. Derivat Imidazole : Mikonazole, Ketokonazole, Klotrimazole,
Bifonazole, Ekonazole, Isokonazole, Tiokonazole.
3. Derivat Triazole : Flukonazole, Itrakonazole, Terkonazole
4. Organic Acid : Benzoat acid, Salisilat, Propionat, Kaprilat,
Undesilinat
5. Ect, Terbinafin,Tolnaftat, Haloprogin,Naftifin,
Sikopiroks,Selensulfida, Pirition
Mechanism of action
Antibiotik
(Griseofulvin,amfoterisin B,
Nistatin, Natamisin
Permeabilitas Cell ↑↑
Fungi ↓
destroyed
O
Mechanism of action
Derivat Imidazol
(Mikonazole,Ketokonazole,Klotrimazole
,Bifonazole,Ekonazole,Isokonazole,Tio
konazol)
O
Antibiot Griseofulvin Amfoterisin B Nistatin Natamisin
ic
Source Penicillium Streptomyces Streptomyc Streptomyce
griseofulvum nodosus es noursei s nataliensis
Used Oral Oral & IV Oral,Vagin Vaginal &
al & Topical
Topical
Reabsorpt Better with Nothing Nothing Nothing
ion in Lipid
Usus
Distributi Keratin, Not diffution to Not Not
on Stratum Skin, and diffution to diffution to
(Diffution corneum mucous Skin, and skin,
) (skin),nail, membran mucous mucous
root of hair membran membran
Griseofulvin Amfoterisin Nistatin Natamisin
B
Side Efect Fotosensitisasi, Nefrotoksik Unpleasent taste Irritation on the
urtikaria,liver (vomiting) skin and
destroyed mucous
Pregnance Don’t give it Not have enough Can Give Can Give
(destroy mitosis data
of cromosom)
Side Efect Interaction with hepatic The Least effect of All the azoles
microsomal enzym (but
lesser degree than
ketokonazol)
Mild fungal
infection
Whitefield(salisilat
5% + benzoat 5%
Ec Tolnaftat Haloprogin Naftitin Siklopiroks Terbinafi
t n
Efective Efective Efective Efective Terbinafin
dermatofit Epidermofito Nail Candida Mallass
n, infection albicans and ezia furfur
Zalp + Pitirosporum, & Trichopyton (panu),
tolnaftat 2 Trichopiton.C Mallassezi rubrum candida
%+ andida a furfur dose : 2 dd dose : oral
heksaklorof Cream 1 % (panu)C cream 1% for 1-2 dd 250
en 0,5% ream 1 % 2-4 weeks mg and
topical 1-2
dd cream
10 mg
Autacoids
Autacoids are endogenous substances
with complex physiologic and
pathophysiologic functions
HISTAMIN
Released from mast cells in response to IgE-
mediated allergic reactions (rhinitis seasonal/hay
fever, urticaria, and angioneuritic edema.
Plays an important physiologic role in the control
of acid secretion in the stomach and as a
neurotransmitter
Histamin has no clinical application
Receptors anf Effects
• H1 receptor– important in smooth muscle
effects, especially those caused by IgE-
mediated responses. Effects :
bronchoconstriction, and vasodilation
• H2 receptor – mediates gastric acid secretion
by parietal cells in the stomach and also has
cardiac stimulation effects
• H3 receptor – involved mainly in presynaptic
modulation of histaminergic
neurotransmission in the CNS
Histamine H1 Antagonists
Classification and prototype :
1. First generation H1 blockers
(dyphendramine, doxylamine,
chlorphenyramine, cyclizine) highly
sedating agents with significant autonomic
receptor-blocking effects
2. Second generation H1 blockers
(fexofenadine, loratadine, cetirizine) free
of sedating and autonimic effects
Mechanism and Effects
• Competitive pharmacologic antagonists at the H1
receptor, no effect on histamine release from storage
sites. More effective if given before histamine release
occurs
• Antagonists at autonomic receptor (muscarinic
blockers and adrenoceptor blockers
• A few also blocks serotonin receptor
• No effects at H2 receptors
• Effects : sedating, antimotion sickness, potent local
anesthetics
Clinical use
• Allergies (hay fever, urticaria)
• Antimotion sickness (diphenhydramine,
dimenhydrinate, promethazine)
• Management of chemotherapy-induced
vomiting (diphenhydramine)
Toxicities
• Sedation (especially with first generation H1
blockers)
• Antimuscarinic effects (dry mouth, and
blurred vision) occur with first generation
• Alpha blocking drugs may cause orthostatic
hypotension
Histamine H2 Antagonists
• Prototype : cimetidine, ranitidine, famotidine, and nizatidine
• Mechanism of action : pharmacologic antagonists at H2
receptors
• Effects : reduction of gastric acid secretion
• Clinical use :
- acid peptic disease
- prevent recurrences of gastric peptic ulcers
- Zolinger-Ellison syndrome (acid hypersecretion, severe
recurrent peptic ulcer, GI bleeding, diarrhea)
- gastroesophageal reflux disease (GERD)
• Toxicities
- Inhibitor of hepatic drug-metabolizing enzymes and reduce
hepatic blood flow
- Antiandrogen effects
Serotonin
Serotonin plays a physiologic role as a neurotransmitter in both
the CNS and enteric nervous system
Receptor and Effects
1. 5-HT1 receptor – mediate both excitatory and
inhibitory effects in various smooth muscle
tissues
2. 5-HT2 -- mediate synaptic excitation in the
CNS and smooth muscle contraction (gut,
bronchi, vessels) or dilation (vessels)
3. 5-HT3 – found in the chemoreceptive are and
vomiting center & in peripheral sensory and
enteric nerves
Clinical use : Serotonin has no clinical application
Other Serotonin Agonists
1. 5-HT1D agonists – (sumatriptan, naratriptan).
Effective in the treatment of acute migrain and
cluster headache attacks
2. Serotonin reuptake inhibitors – Fluoxetine,
fluvoxamine, sertraline are antidepressant drugs.
Dexfenfluramine reducing appetite
Serotonin Antagonists
• Prototype :
- 5-HT2 blockers (ketanserin, phenoxybenzamine,
cyproheptadine)
- 5-HT3 blockers (ondansteron, granisetron, dolasetron,
alosetron)
Mechanism of action
• Ketanserin, cyproheptadine, and
phenoxybenzamine are poorly selective
antagonists
• Ondansetron, granisetron, and dolasetron are
selective 5-HT3 receptor and have a central
antiemetic action
Toxicities
• Ketanserin : blockade, h1 blockade
• Ondansetron : diarrhea and headache
• Dolasetron : QRS and QT prolongation ECG
• Alosetron : constipation
Clinical use
Antihypertensive (ketanserin)
Treatment carcinoid tumor (a neoplasma that
secretes large amounts of serotonin
Ketanserin, cyproheptadine, and
phenoxybenzamine
Control of vomiting associated with cancer
chemotherapy and postoperative vomiting
Irritable bowel syndrome with diarrhea
(alosetron)