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7 Cards in this Set
The most important side effect of cimetidine is inhibition of P450 -
mediated (CYP1A2, CYP2C9, CYP3A4) metabolism of drugs such as
warfarin, phenytoin, theophylline, phenobarbital, diazepam, propranolol, and
imipramine. Hence, if coadministered with cimetidine, the doses of these
drugs may have to be decreased.
Cimetidine blocks androgen receptors and when taken in high doses
for long periods, e.g., for treatment of Zollinger-Ellison Syndrome, can lead to
gynecomastia and impotence in men and galactorrhea in women.
These are rare but slurred speech, delirium, confusional states have
been reported especially in elderly patients.
PROTON PUMP INHIBITOR
irreversibly blocks the H+/K+ proton pump.
Gastrin levels rise due to increase in gastric pH. This leads to hyperplasia of
ECL cells and ECL tumors in rats treated with the drug for long periods (2
High pH allows bacterial growth in stomach -- it has been suggested that
nitroso-compounds synthesized from nitrites may lead to gastric cancer.
Interactions due to INCREASED GASTRIC pH
e.g. Decreased bioavailability of
analog of prostaglandin E1
Inhibits acid secretion
- and mucus secretion
Promotes gastric blood flow
Diarrhea due to increased intestinal motility and secretion
Uterine contraction can cause abortion of pregnancy
Pregnancy termination in combination with mifepristone (RU486, Mifeprex®)
If pH < 4, sucralfate polymerizes to form a thick, sticky gel which adheres to
proteins in the ulcer crater.
SE some drug interactions, e.g., decreases absorption of cimetidine.
Act much like sucralfate, but may also kill H. pylori
Often used in conjunction with antibiotics and H2-blockers or proton pump inhibitors.
Mg2+ increases motor activity, accelerates gastric emptying diarrhea.
Al3+ decreases motor activity, slows gastric emptying constipation.
3. Systemic antacids alkalinize blood/urine
4. Drug Interactions Al3+ and Mg2+ e.g., tetracycline
The main advantage of eradicating H. pylori is the very low rate of
recurrence of the ulcer after cessation of treatment,
H. pylori rapidly becomes resistant to the antibiotics metronidazole and
clarithromycin, therefore, these drugs are not used alone, but in combination with