Anti-Ulcer Pharm Flashcards
What are the main classes of anti-ulcer agents?
- H2 receptor antagonists
- PPIs
- surface acting agents (sucralfate)
- PGE1 analogs (misoprostol)
- bismuth compounds
- antacids
What is a good example of why it is important to ask about OTC medications that is exemplified by anti-ulcer medications?
some OTC medications have CYP450 inhibition
- cimetidine
- omeprazole
*both are prototypical examples of CYP inhibitors used in questions
What anti-ulcer classes are used in an acute settings to decrease acid?
What is their relative order of effective onset of action/symptom relief?
antacids > H2 antagonists > PPIs
rapid/instant > 0.5-2 hours > 1-2 days
What anti-ulcer medications are used primarily in prophylactic settings?
-PGE1 analogs (misoprostol)
*prophylactic for NSAID related ulcers
What anti-ulcer class does not affect amount of acid produced/present?
-surface acting agents (sucralfate)
What is the common suffix of H2 receptor antagonists?
What are the main drugs in the class?
“-tidine”
- cimetidine
- famaotidine
- nizatidine
- ranitidine (zantac)
Where do H2 receptor antagonists act and what is their mechanism of action?
How does this relate to its effectiveness in reducing acid production?
indirect inhibition of acid production
- reverisbly inhibits H2 receptor on basolateral membrane of parietal cells
- decreases cAMP -> decreased acid production
Because there are multiple pathways of stimulating acid production and this is only indirectly blocks acid production via one pathway, other pathways can still stimulate acid production (20-50% reduction in acid)
What are the general adverse effects of H2 receptor antagonists?
relatively uncommon and mild -> most are OTC for this reason
Adverse effects:
-GI s/x (diarrhea/constipation)
-CNS s/x (HA/dizziness)
What adverse effects are associated with cimetidine specifically?
Rare (assoc. w/ long-term use and high does)
- weak anti-androgen effect (most prominent in cimetidine) -> gynecomastia in men/galactorrhea in women
- even more rare, impotency in men
What drug interactions occur with H2 receptor antagonists?
- cimetidine is a CYP450 inhibitor -> many interactions
- ranitidine also but 10%
- no interacitons in others
What are contraindications for H2 receptor antagonist use?
-pregnancy (relative contraindication) - if necessary, use ranitidine
What is the common suffix of PPIs?
What are the main drugs in the class?
“-prazole”
- omeprazole**
- esomeprazole
- lansoprazole/dexlansoprazole
- pantoprazole
- rabeprazole
Where do PPIs act and what is their mechanism of action?
How does this relate to its effectiveness in reducing acid production?
direct inhibition of acid production:
- irreverisbly inhibit H+/K+ ATPase on apical surface of parietal cells
- covalently binds sulfhydryl group preventing function
Directly inhibits acid secretion 50-90+% reduction in acid depending on dose/frequency
What are the adverse effects of PPIs?
relatively uncommon and mild -> some are OTC for this reason
Adverse effects:
- risk of CDAD (C. difficile-associated diarrhea)
- GI s/x (diarrhea/constipation)
- CNS s/x (HA/dizziness)
- decreased Mg2+/Mg2+
What drug interactions occur with PPI use?
-omeprazole is a CYP450 inhibitor -> many interactions