Anti-Ulcer Drugs Flashcards
Two acid related disorders
Ulcer
Gastro-esophageal reflux disease (GERD)
Buffering agents
Calcium carbonate, magnesium, aluminum hydroxide
- add a base to acid to neutralize
- simple to use but not strong enough for many people
Magnesium side effects
Diarrhea
Calcium and aluminum side effects
Constipation
H2 antagonists
Cimetidine
Cimetidine
- reversible antagonists
- tolerance can develop
Cimetidine down fall
Drug interactions, it is a CYP450 inhibitor
Cimetidine side effects
- generally well tolerated
- gynecomastia: increase in the male breast
- galactorrhea: spontaneous flow of milk from the breast
Proton Pump inhibitor
Omeprazole
Omeprazole mechanism
Irreversible inhibition of the proton pump
- binds and inhibits active proton pumps
- potent acid suppression when used correctly
Omeprazole side effects
Generally well-tolerated
Concerns over long term use
- Hypergastrinemia: increased gastrin release
- Osteoporosis
Anticholinergic
Pirenzapine
Pirenzapine mechanism
- blocks muscarinic receptors
- poor efficacy
- many side effects
Mucosal defence agents
Prostaglandins - misoprostol Coating agents - sucralfate - bismuth subsalicylate (Pepto Bismol)
Misoprostol mechanism
Promotes secretion of mucous/bicarbonate
Inhibits acid secretion
Misoprostol side effects
Diarrhea
Abdominal cramping
Also induces abortion so contraindicated in pregnancy
Sucralfate mechanism
Aluminum hydroxide + sucrose sulfate
- forms paste
- stimulates mucous and bicarbonate secretion
Sucralfate side effects
Acts locally
Aluminum causeras constipation
Bismuth subsalicylate mechanism
Forms protective barrier on ulcer
Enhances mucous and bicarbonate secretion
Inhibits growth of H Pylori and adherence to mucosa
Main causes of Ulcers
H Pylori
NSAIDs
H Pylori functions
- produces inflammatory changes in mucosa
- impairs mucosal défense
- increases acid secretion
Common antibiotics used for H Pylori eradication
- Amoxicillin
- Clarithromycin
- Tetracycline
- Metronidazole
- Bismuth is often included in these regimens
How to reduce GI side effects (NSAIDs)
- take them with food
- take with misoprostol
- take with a proton pump inhibitor