GI Meds Flashcards
Proton Pump Inhibitors
Omeprazole
Administration of omeprazole
administered as inactive acid-liable pro-drugs that have an enteric coating to protect against rapid destruction in the stomach. Dissolved and absorbed in the intestines.
Mechanism of Omeprazole
Absorbed in intestine where it is acid activated and blocks H-K-ATPase irreversibly by forming a covalent bond with SH-groups of H-K_ATPase. ATLEAST 18 HOURS ARE REQUIRED FOR FORMATION OF A NEW ATPASE
How often is Omeprazole given?
Once daily, twice is severe GERD, should be given 30 min before meal for peak plasma levels.
By what percent does food decrease the bioavailability of Omeprazole?
50%
Why does ir take 3-4 days of daily medication for full acid inhibition?
Not all H-pumps are inactivated with the first dose
Uses of omeprazole
gastric ulcers, alone or in combo with H. pylori; also used in GERD
DRUG OF CHOICE WITH ZOLLINGER ELLISON SYNDROME
T/F: Proton pump inhibitors are superior to H2 receptor antagonists and to mucosal protectants in the healing of NSAID Peptic Ulcers
True
WHy should you avoid omeprazole and plavix?
Omeprazole is a moderate CYP2C19 inhibitor, that reduces the pharmacological activity of plavix(clopidogrel). Avoid using concomitantly or 12 hrs apart.
Histamine H2-receptor antagonist
Cimetidine
Main role of cimetidine
Inhibits fasting secretion of gastric acid with a smaller effect on food stimulated gastric acid secretion. Competetive inhibitor at the parietal cell H2-receptor. ALSO BLUNTS RESPONSES TO GASTRIN AND ACH
Uses of cimetidine
gastric ulcers, GERD, and heartburn
How safe is cimetidine?
Very safe its is available over the counter
Drug interactions of cimetidine
interferes with metabolism of other drugs due to inhibition of cytochrome p450
Mucosal Protective agents
Misoprostol, Sucralfate, Bismuth subsalicylate
Misoprostol
A stable analog of PGE that bings to the PG receptro and causes a modest inhibition of acid secretion. Cytoprotective.
PROMOTES SECRETION OF MUCUS AND BICARB
Uses of misoprostol
prevention of gastric damage due to chronic use of NSAIDs