GI Pharm Flashcards
cytoprotectants
- bismuth subsalicylate
- sucralfate
- misoprostol
antacids
- aluminum hydroxide
- magnesium hydroxide
- calcium carbonate
- sodium bicarbonate
H2-receptor antagonists
- cimetidine
- ranitidine
- famotidine
- nizatidine
PPIs
Omeprazole Lansoprazole Rabeprazole Pantoprazole Esomeprazole Dexlansoprazole
antacids AE
- diarrhea (Mg)
- constipation (Al)
- abd distension (Ca)
cautions: kidney insufficiency, drug interactions (chelation w/ fluoroquinolone, tetracyclines)
antacids MOA
work locally within the GI lumen to neutralize acid
quick relief of symptoms, but duration of action short (a few hours)
bismuth compounds
- bind to base of ulcers
- promote mucin and bicarb production
- antibacterial effects
bismuth subsalicylate
AE
(pepto-bismol)
- constipation
- darkening of of tongue/stool
- avoid if aspirin allergy
- drug interactions
sucralfate
sulfated polysaccharide + AlOH3
- drug (-) pref binds damaged GI mucosa (+)
- activ by acidic envio
- lasts up to 6 hr
- low bioavailability
uses: acid-peptic ulcer disease (adjunctive or alt agent), stress ulcer prophylaxis
sucralfate AE
- constipation*
- accumulation to Al3+
- drug interactions
sucralfate use in kidney insufficiency is dangerous why
accumulation of Al 3+ can occur
misoprostol
prevention of ulcers w/ NSAID use
prostaglandin E analog
- stim secretion of mucin and bicarb
- inc mucosal BF
- suppresses acid production in parietal cell by binding to EP3 receptor
misoprostol
AE
- diarrhea
- inc uterine contractility (termination/induction)
H2 antagonists
- compete w/ histamine for binding to H2 receptors on parietal cells
- more potent, longer-lasting effects than traditional antacids
H2 antagonist uses
- uncomplicated GERD
- gastric and duodenal ulcers
- stress ulcer prophylaxis
H2A should be dose adjusted for
kidney insufficiency
H2A adverse effects
- diarrhea
- constipation
- drowsiness
- fatigue
- HA
- BM suppression (rare)
- drug interactions (changes pH, interferes w/ drugs req acidic envio)
- CNS w/ high doses (confusion, delirium, hallucinations/slurred speech)
- cimetidine (gynecomastia/galactorrhea)
gynecomastia (men)
galactorrhea (women)
cimetidine (H2A)
H2A drug interactions
drugs req an acidic environment (atazanavir, itraconazole)
cimetidine (H2A) =inhibitor of CYP-450 (phenytoin, theophylline, warfarin)
PPI
MOA
IRREVERSIBLY bind to and inactivate H/K-ATPASE
- prodrugs, req activation in acidic envio
- parent cpd=unstable in acid
- enteric coated formulations usu req
PPI
pharmacokinetics
plasma half life 1-2hr
onset 2-4 days
duration of effect 24-48 hr
PPI
uses
- gastric and duodenal ulcers
- GERF
- Barret’s esophagus
- Zollinger-Ellison syndrome