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Drugs Acting On Git
Drugs Acting On Git
, SpKK
Dr.dr. Asep Sukohar, M.Kes
Department of Pharmacology and Therapy
Medical School Lampung University
I. Drugs used to treat peptic ulcer disease
Phatogenesis :
3 major factors :
- Infection Helicobacter pylori
- HCl secretion
- Inadequate mucosal defense against gastric
acid
Treatment :
- Eradicating H. pylori infection
- Reducing secretion of gastric acid /
neutralization
- Providing agents to protect gastric mucosa
Drugs used to treat peptic ulcer disease
(continued)
V. Antimuscarinic agents
-Hyoscyamine - Pirenzepine
-Mepenzolate
VI. Antacids
-Aluminum hydroxide -Magnesium hydroxide
-Calcium carbonate -Sodium bicarbonate
Second-line regimen
• Two AM :
• Metronidazole- amoxicillin
orclarithromycin+antisecretoryagent (omeprazole)
Single AM :
• Less effective
Secretion of acid by gastric parietal cells
regulated by
- Histamine
- Acetylcholine
- Gastrin
- Prostaglandin E2 & I2
Drugs :
• Cimetidine(prototype) -Famotidine
• Ranitidine-Nizatidine
Therapeutic uses :
• Peptic ulcers
• Zollinger-Ellison syndrome
• Acute stress ulcers
• Gastroesophagealreflux disease (heartburn)
Cimetidine& other DOA > , Potency 5-
Ranitidine
Cimetidine
H2-antagonist : 10 x >
Given orally thancimetidine
distributed widely in Minimal SE ,≠
the body ( breast milk, produceantiandrogenic
placenta) E : Urine orprolactin-stimulating
Short serum half-life effects ofcimetidine
increased in renal ≠ inhibit the mixed
failure function oxygenase
Slowly inactivated by system liver
the ≠ affect the
liver’smicrosomalmixed concentration of other
functionoxygenasesyst drugs
em
• Similar ranitidine in its pharmacologic
action
Famotidine • 20-160 x > potent thancimetidine
• 3-20 x > potent than ranitidine
Pirenzepine
Relatively specific muscarinic M1-receptor
antagonist
SE <
Weak bases that react with gastric acid Water + salt
Reduction H.pylori colonization & stimulation PG
synthesis
E.g. -Aluminum hydroxide -Magnesium hydroxide
-Calcium carbonate -Sodium bicarbonate
MOA :
Pepsin is inactive in solution above pH 4.0
Once antacids administered, they will chemically reduce/neutralize
gastric acidity
peptic activity
Relieve symptoms of peptic ulcer disease
Sodium Bicarbonat systemic antacid
NaHCO3 + HCl NaCl + H2O + CO2
- Active ingredient in backing soda
- Highly soluble
absorbed rapidly from the gut
promote systemic alkalosis and fluid retention
Not recommended for long-term use
Therapeutic uses :
effective against traveler's diarrhea, used either alone or in
combination with antimicrobial agents (trimethoprim,
cotrimoxazole , fluoroquinolone).
If clinical improvement in acute diarrhea does not occur
within 48 hours, loperamide should be discontinued.
adjunct treatment in almost all forms of chronic diarrheal
disease.
should not be used in children younger than 2 years of age
lacks significant abuse potential
overdosage → CNS depression and paralytic ileus
children > sensitive than adults to the CNS-
depressants effects of loperamide
in patients with active inflammatory disease of the
colon, loperamide should be used with great caution
to prevent development of toxic megacolon.
structurally related to meperidine
difenoxin is the active metabolite of diphenoxylate and also
is used as such to treat diarrhea
as antidiarrheal agents, diphenoxylate and difenoxin >
potent than morphine
Pharmacokinetic :
- extensively absorbed after oral administration, Tmax = 1-2 hours
deesterified
diphenoxylate -----------------> difenoxin , t1/2=12 hours
- higher doses (40-60 mg per day) → CNS effects →
potential for abuse and/or addiction
- available in preparations containing small doses of
atropine to discourage abuse and deliberate overdosage
Adsorbent agents such as kaolin, pectin,
methylcellulose and activatedattapulgite, magnesium
aluminum silicatewidely used to control diarrhea.
Catharsis :
• Evacuation of unformed, usually watery fecal
material from the entire colon