Antacid Pharm Flashcards
Regarding Parietal cell acid secretion, Ach and Gastrin action occurs through raising the levels of what>
IP3 and Calcium
Histamine stimulates acid production through?
Adenylyl cyclate (raising cAMP levels)
Somatostatin and Prostaglandins lower acid secretion via?
Lowering cAMP levels….cut off the histamine pathway
pH goal of antacid tx is?
pH greater than 4
Antacids can significantly impact the absorption of other drugs!!! worth knowing….do not have pts take antacids within hrs of other meds.
ok
H2 blockers mechanism
Block the binding of histamine to the histamine receptor.
H2 blockers inhibit the basal, cephalic, and nocturnal Gastric Acid Secretion!!!!
Reduce volume and acidity of GA secretions.
Potency of Cimetidine?
1x
Potency of Ranitodine and Nizatidine?
4-10x
Famotidine potency?
20-50
Cimetidine has what effect on CYPs?
inhibits them
Famotidine leads to low clearance of ?
Theophylline
Proton Pump Inhibitors mechanism>
Inhibit the proton pump (Hydrogen Potassium ATPase) at the apical membrane of the parietal cells. Most effective form of gastric acid relief/
PPI’s are absorbed into the bloodstream in the small intestine as lipid soluble prodrugs. Carried in teh blood to parietal cells and diffuse to canaliculi where the acid pH ionizes them. The ionized form of the drug then binds irreversibly to H/K ATPase and achlorhydria results. Because the binding is irreversible, the parietal cell must make new PP.
KNOW this mech
All PPIs are CYP— substrates?
CYP219
Which of the PPIs is the weakest of the CYP219 substrates?
Pantoprazole….rabeprozole is also right there with it