Agents for Peptic Ulcer Disease & GERD (Segars) Flashcards
What are the classes of Anti-ulcer drugs discussed in class?
H2 Receptor Antagonists
Proton Pump inhibitors
Surface Acting Agents
PGE1 Analogs
Bismuth Compounds
List the H2 Receptor Antagonists discussed in class
Cimetidine
Famotidine
Nizatidine
What is the MOA of Histamine H2 receptor antagonist
They reversibly inhibit H2 receptors on the baso-lateral membrane of parietal cells
What are the general adverse effects of H2 Receptor Antagonists
Primarily GI-related
Some CNS- related
What rare side effects are seen in H2 Receptor Antagonists which are more likely seen with long-term and high dosing
Gyencomastia in men
Galactorrhea in women
Blood dyscrasias such as neutropenia & thrombocytopenia
What H2 Receptor Antagonists causes gynecomastia/galactorrhea & what is it’s MOA
Cimetidine
Decreases testosterone binding to androgen receptor causing a weak anti-androgen effects
_____, an H2 Receptor Antagonist, has A LOT of drug-drug interactions and is the prototypical inhibitor of several ______
Cimetidine
CYP450
What are the relative contraindications of H2 Receptor Antagonists
Pregnancy
What proton pump inhibitors were discussed
Lansoprazole
Dexlansoprazole
Omeprazole
Esomepraazole
Pantoprazole
Rabeprazole
What is the MOA of Proton Pump Inhibitors (PPI’s)
They covalently bind to sulfhydryl groups of H+/K+ ATPase at parietal cell secretory sites, thereby inhibiting gastric acid secretion by irreversibly inhibitng functioning -ase pumps
What are the general & rare adverse effects of Proton Pump Inhibitors
General: Primary GI related & Some CNS related
Rare: Clostridioides/Clostridium difficile associated diarrhea (CDAD)
What is the prototypical PPI for CYP450 inhibition
Omeprazole
What is the relative contraindications for PPI
Pregnancy
What surface acting agents were discussed
Sucralfate
SUrface - SUcralfate
What is the MOA of Sucralfate
Undergoes cross-linking from interaction with stomach acid, creating a viscous, sticky polymer which adheres to epithelial cells around ulcer’s crater & prevents acid access to ulcer sites
Band-aid drug
What are the indications, relative contraindications and adverse effects of sucralfate
Indications - Any ulcers
Relative contraindications - Severe renal failure (avoid aluminum)
Adverse Effects - Constipation (Al(OH)3)
How are drug interactions avoided in sucralfate
Taken 4x daily (QID) for active ulcers 2 hours before meals
What are the PGE1 Analogs discussed
Misoprostol
What is the MOA of Misoprostol
Acts like a prostaglandin by binding to parietal cells and reducing acid production & also binding to superficial epithelial cells and promoting bicarbonate and mucous production
What is the indications for Misoprostol
Prevention of NSAID-induced gastric ulceration in patients at high risk of ulcerations and complications
Patients who can’t come off NSAID so you give them misprostol
What are the off label use of misoprostol
- W/ or w/o mifepristone (pregnancy termination)
- Alone for cervical ripening
- Post-partum hemorrhaging
What are the adverse effects and contraindications of Misoprostol
Adverse Effects - Primarily GI related & Some CNS related
Contraindications - Pregnancy & Inflammatory Bowel Disease
What were the Bismuth Compounds discussed
Bismuth Subsalicylate
What is the MOA of Subalicylate
Originally developed as an anti-diarrheal agent and has antimicrobial actions so it can treat H. pylori
