What types of drugs affect gastric secretion?
What types of drugs increase GI motility?
What types of drugs reduce GI motility?
Describe the events that lead to gastric acid secretion starting with the intake of dietary peptides
What type of cell produces histamine in the GI tract?
ECL (enterochromaffin-like) cells
Which antacids have high neutralizing capacity?
NaHCO3
Al(OH)3
Mg(OH)2
Which antacid has moderate neutralizing capacity?
CaCO3
What is one adverse effect of CaCO3?
milk-alkali syndrome
What is one adverse effect of NaHCO3?
systemic alkalosis
What is one adverse effect of Al(OH)3?
constipation
What is one adverse effect of Mg(OH)2?
diarrhea
Why don’t histamine receptor antagonists cause complete deactivation of parietal cells?
Parietal cells are activated through other mechanisms aside from histamine, including CNS activation from acetylcholine and from gastrin
What are the 2nd generation H2 receptor antagonists?
Ranitidine (Zantac)
Nizatidine (Axid)
Famotidine (Pepcid)
What are the characteristics of 2nd generation H2 receptors antagonists?
-longer half-life (HS vs. BID dosing)
-fewer effects on CYP450 system
-greater potency
-absorbed quickly to reduce parietal cell function
What is the mechanism of action of proton pump inhibitors?
They irreversibly bind to the H+/K+ ATPase pump
What is the difference between omeprazole and esomeprazole?
Omeprazole: racemic mixture, less potent
Esomeprazole: S-enantiomer, more potent
Proton pump inhibitors are substituted ______________
Benzimidazoles
Why do proton pump inhibitors have slow onset?
They must be absorbed in the small intestine, circulate, and then be taken up by the parietal cells
What activates the prodrug form of a PPI?
The acidic pH in the parietal cell
PPIs have a ______ plasma life but _____ duration action
short, long
What are the 5 risk factors for GERD?
What are the 5 characteristics of GERD pathophysiology?
What medications are a direct irritant to esophageal mucosa?
What is the mechanism of action of H2RAs?
Reversible inhibition of histamine receptors on parietal cells