CA - Drugs for PUD Flashcards
List THREE classes of agents that reduce gastric acidity.
- Weakest: Antacids
- H2‐receptor Antagonists
- Strongest: Proton Pump Inhibitors (PPI)
List THREE examples of mucosal protective agents
Sucralfate
Misoprostol
Bismuth Compounds
Whats the MOA of antacids?
- NEUTRALISE & REDUCE gastric acidity
- DOES NOT prevent gastric acid production
Rank common antacids according to their rate of neutralization.
- NaHCO3 - Sodium Bicarb
- CaCO3 - Calcium Carb
- Mg(OH)2
- Al(OH)3
Why is simethicone often found in antacid formulations?
- Breaks up the bubbles into smaller bubbles -> easier to release gas
- reduce gastric distention & belching
Why are magnesium and aluminium compounds usually formulated together in antacids?
Magnesium causes osmotic diarrhoea
Aluminum causes constipation
Together the effects balance
List adverse effects of sodium & calcium carbonates antacids.
Sodium compounds:
Fluid retention, hypertension, caution in heart failure
Calcium compounds:
Hypercalcaemia, rebound acid secretion
BOTH:
- Metabolic alkalosis
- Milk-alkali syndrome
Carbonates and bicarbonates:
CO2 gas formation -> gastric distention, belching
List adverse effects of antacids with Mg & Al compounds.
Magnesium compounds: Osmotic diarrhoea
Aluminium compounds: Constipation
General things to take note of when taking antacids?
- Avoid long-term use in patients with renal insufficiency -> electrolytes & antacid formulations are eliminated through the kidneys
- Affects absorption of other medications
Do not take within 2 hours of other medication
Whats the MOA of H2 receptor antagonists?
Name an example.
Supresses acid secretion by parietal cells
Most potent & widely used: Famotidine
When is the best time to take H2 receptor antagonists? (DBL CHK)
- On an empty stomach before sleep at night
- Most of PUD pts have alot of nocturnal acid secretion
- Effective in controlling fasting and nocturnal acid release
What are the adverse effects of H2 receptor antagonists - famotidine & ranitidine?
- Headache, nausea, dry mouth
- Rare: Tachycardia, blood dyscrasia - imbalance in blood cell types, blurry vision, MSK pain
What are the adverse effects of H2 receptor antagonists - cimetidine?
- Headache, nausea, diarrhoea / constipation, fatigue
- Mental confusion in critically ill, or renal / hepatic dysfunction pts
- Anti-androgenic:
Men: gynaecomastia, impotence
Women: galactorrhoea
MOA of PPIs?
Name ONE.
- Irreversibly blocks Proton pumps
Omeprazole
What are the MOAs of PPIs that result in selective proton pump inhibition in the parietal cell canaliculi.
Name.
- Irreversibly blocks Proton pumps
- Enteric-coated formulation
- protects it from gastric acid
- MUST NOT be crushed/chewed bcs it will brk down enteric coating -> pro drug will be activated in stomach & never absorbed
Omeprazole
Whats the duration of action of omeprazole?
Duration of action: 24hrs
Half-life / T1/2: 1-2hrs
When is the best time to take PPIs? WHY?
- Empty stomach before breakfast
- Bioavailability decreases 50% bcs of food
- Inhibits active pumps -> Best to be present during mealtimes - 1hr before meal
Half life: 1-2hr - Once daily
- Irreversibly blocks proton pumps for 24 hrs
List adverse effects of omeprazole.
Headache, nausea, gas, diarrhoea, dizzy, rash
What are the gastric mucosal protection drugs and what do they do?
- Sucralfate
- Bismuth
- Misoprostol
- Protects cells lining walls of stomach & upper GI tract -> time for ulcer to heal
Whats the MOA of sucralfate?
- Binds to (+) charges of damaged proteins in ulcer pit -> forms gel layer which coats & protects the ulcer
- Stimulates prostaglandin -> more mucus & bicarb secretion
When is the best time to take sucralfate? WHY?
On an empty stomach at least 1hr before meals -> prevent drug-food interactions
What are the adverse effects of sucralfate?
- Constipation
- Impairs absorption of other drugs
Whats the MOA of bismuth compounds?
- Forms protective layer -> protects ulcers from acid
- Stimulates mucus and bicarbonate secretion
- Directly some anti-microbial activity against H. pylori
What are the adverse effects of bismuth compounds? Precautions to take when taking bismuth?
- Rare: Prolonged use may cause bismuth toxicity -> encephalopathy = change in brain fxns: ataxia, headaches, confusion, seizures
- Use only for short periods
- Avoid in patients with renal insufficiency - Harmless blackening of stool and reversible darkening of tongue