Pharm - Anti-ulcers Flashcards
list the H2- receptor antagonists
1) cimetidine
2) famotidine
3) nizatidine
4) ranitidine
list the proton-pump inhibitors
1) lansoprazole
2) dexlansoprazole
3) omeprazole
4) esomeprazole
5) pantoprazole
6) rabeprazole
list the surface acting agents
sucralfate
list the PGE1 analogs
misoprostol
list the bismuth compounds
bismuth subsalicylate
- tidine ending indicates a ______
H2 receptor antagonist
-prazole ending indicates a ______
proton pump inhibitor
MOA of histamine type 2 (H2) blockers
reversibly inhibit H2 receptors on basolateral membrane of parietal cells
- inhibits 20%-50% of acid production depending on dose
onset of action for H2 receptor blockers
rapid (0.5-2 hours)
compare onset of H2 receptor blockers, antacids, and PPIs
most rapid onset: antacids
middle: H2 receptor blocker
slowest onset: PPIs
how long does ulcer healing take w/ H2 receptor blockers
4-8+ weeks
normal adverse effects H2 receptor blockers
(all relatively mild, transient, and infrequent)
- nausea/diarrhea/constipation
- headaches
rare adverse effects of H2 receptor blockers, particularly cimetidine
- decreases testosterone binding to androgen receptors –> gynecomastia in men and galactorrhea in women
- neutropenia, thrombocytopenia
drug interactions of cimetidine (H2 receptor blocker)
cimetidine is the prototypical inhibitor of several CYP450 isoenzymes –> LOTS of drug-drug interactions
drug interactions of ranitidine (H2 receptor blocker)
inhibits CYP450 (but only 10% compared to cimetidine)
relative contraindications of H2 receptor blockers
pregnancy
- famotidine can be used
- only use ranitidine if necessary
MOA of proton pump inhibitors
covalently bind to sulfhydryl groups of H+/K+ ATPase at parietal cell secretory sites –> inhibits gastric acid secretion by irreversibly inhibiting functioning “-ase” pumps
- inhibits 50%-90% acid secretion
how long does ulcer healing take w/ PPIs
4-8+ weeks
how long does it take to see full symptom effects of PPIs and how long do their effects last
several days
- effects last 24 hours
adverse effects of PPIs
- diarrhea/dyspepsia/nausea
- CDAD** (c. diff associated diarrhea)
- headaches/dizziness
- myalgia/fatigue/myopathy
drug interactions of PPIs
omeprazole is the prototypical PPI that inhibits CYP450 –> lots of drug interactions