Anti-Ulcer Drugs Flashcards
What suffix is a/w H2 receptor antagonists?
-tidine
What suffix is a/w Proton Pump Inhibitors?
-prazole
What drugs are H2 antagonists?
Cimetidine (tagamet)
Ranitidine (zantac)
Famotidine (pepcid)
Nizatidine
What is combined to make antacids?
calcium or magnesium
What is the MOA of H2 blockers?
reversibly - receptors on basolateral membrane of parietal cell
inhibits 20-50% acid production
0.5-2 hours onset, so longer than antacids but shorter than PPIs
ulcer healing 4-8 weeks
What should you consider if the drug regimen for ulcers is not working after 4-8 weeks?
think H pylori
–> ABX
Adverse effects of H2 blockers
mild, transient, infrequent
–> GI and CNS
Rare adverse effect of H2 blockers
long term, high dosing:
- Cimetidine decreases testosterone binding
- ——-> gynecomastia (M) and galactorrhea (F)
blood dyscrasias: neutropenia and thrombocytopenia
What H2 blocker is a prototypical inhibitor of several CYP450 enxzymes?
Cimetidine
–> LOTS of drug-drug interactions
What is a relative contraindication for H2 blockers?
Pregnancy
–> Ranitidine only if necessary
PPI examples
Omeprazole Esomeprasole (isoer) Lansoprazole Dexlansoprazole (isomer) Pantoprazole Rabeprazole
Can PPI completely stop acid production?
Yes with large doses since blocks H+/ K+ ATPase
PPI MOA
irreversibly bind H/K ATPase to inhibit gastric acid secretion
–>takes several days to create new steady-state pump activity
How long do PPI effects take?
full symptom effects in few-several days
How much acid do PPIs inhibit?
50-90%
Adverse effects of PPIs
*overall mild an infrequent
GI
–> C diff diarrhea
CNS
Associations with increased risk via use of PPIs
AKI
Osteoporosis/fx
MI
What PPI is prototypical inhibitor of CYP450 and has many drug-drug interactions?
omeprazole
Relative contraindications of PPIs
Pregnancy
–> use lansoprazole only if necessary
What is a sulfated polysaccharide (made of sucrose and aluminum) that is surface-acting, much like a band-aid?
Sucralfate (carafate)
MOA of Sucralfate
BAND-AID
cross-linking of damaged/ulcerated epithelial cells–> forms sticky polymer that prevents access to ulcer sites
What other effects does Sucralfate have
stimulates local prostaglandin and mucous production–> CYTOPROTECTION
does NOT affect pH