Anti-Ulcer Agents Flashcards
H2 receptor antagonist suffix
-tidine
Proton pump inhibitor suffix
-prazole
Four most common Histamine Type-2 Blockers
Cimetidine, ranitidine, famotidine, nizatidine
H2 Receptor antagonist MOA
inhibit H2 receptors on baso-lateral membrane of parietal cell
H2 antagonist onset of relief/ulcer healing
0.5-2 hours, healing in 4-8+ weeks
How much acid production is inhibited by H2 receptor antagonists?
20-50+% , but dependent on dose and duration
AE of H2 receptor antagonist
mild and infrequent, but may include primarily GI-related and some CNS-related, rarely may include blood dyscrasias (neutropenia and thrombocytopenia)
AE cimetidine
decrease testosterone binding to androgen receptor, may cause gynecomastia in men and galactorrhea in women
Cimetidine drug interactions
inhibitor of several CYP450 isoenzymes, so will have many interactions
Ranitidine drug interactions
~10% of CYP450 inhibition compared to cimetidine
Relative contraindications of H2 blockers
pregnancy (ranitidine if necessary)
MOA PPIs
covalently bind to sulfhydryl groups of H/K ATPase at parietal cell secretory sites, inhibiting gastric acid secretion by irreversibly inhibiting functioning of -ase pumps
Onset of relief with PPI
several days to create new steady-state
Acid inhibition of PPIs
50%-90+% depending on dose, frequency, duration
AE PPi
GI related - C. diff-associated diarrhea, CNS
PPI drug interactions
Omeprazole is a prototypical CYP450 inhibitor
Relative contraindication of PPI
pregnancy (may use lansoprazole)
Sucralfate MOA
cross-linking from interaction with stomach acid, creates a viscous, sticky polymer that adheres to epithelial cells around the ulcer; prevents acid access to ulcer sites, may also stimulate local prostaglandin and mucous production and EDGF