CA - Drugs for PUD Flashcards

1
Q

List THREE classes of agents that reduce gastric acidity.

A
  1. Weakest: Antacids
  2. H2‐receptor Antagonists
  3. Strongest: Proton Pump Inhibitors (PPI)
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2
Q

List THREE examples of mucosal protective agents

A

Sucralfate

Misoprostol

Bismuth Compounds

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3
Q

Whats the MOA of antacids?

A
  1. NEUTRALISE & REDUCE gastric acidity
  2. DOES NOT prevent gastric acid production
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4
Q

Rank common antacids according to their rate of neutralization.

A
  1. NaHCO3 - Sodium Bicarb
  2. CaCO3 - Calcium Carb
  3. Mg(OH)2
  4. Al(OH)3
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5
Q

Why is simethicone often found in antacid formulations?

A
  • Breaks up the bubbles into smaller bubbles -> easier to release gas
  • reduce gastric distention & belching
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6
Q

Why are magnesium and aluminium compounds usually formulated together in antacids?

A

Magnesium causes osmotic diarrhoea

Aluminum causes constipation

Together the effects balance

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7
Q

List adverse effects of sodium & calcium carbonates antacids.

A

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

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8
Q

List adverse effects of antacids with Mg & Al compounds.

A

Magnesium compounds: Osmotic diarrhoea
Aluminium compounds: Constipation

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9
Q

General things to take note of when taking antacids?

A
  1. Avoid long-term use in patients with renal insufficiency -> electrolytes & antacid formulations are eliminated through the kidneys
  2. Affects absorption of other medications
    Do not take within 2 hours of other medication
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10
Q

Whats the MOA of H2 receptor antagonists?
Name an example.

A

Supresses acid secretion by parietal cells
Most potent & widely used: Famotidine

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11
Q

When is the best time to take H2 receptor antagonists? (DBL CHK)

A
  1. 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
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12
Q

What are the adverse effects of H2 receptor antagonists - famotidine & ranitidine?

A
  1. Headache, nausea, dry mouth
  2. Rare: Tachycardia, blood dyscrasia - imbalance in blood cell types, blurry vision, MSK pain
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13
Q

What are the adverse effects of H2 receptor antagonists - cimetidine?

A
  1. Headache, nausea, diarrhoea / constipation, fatigue
  2. Mental confusion in critically ill, or renal / hepatic dysfunction pts
  3. Anti-androgenic:
    Men: gynaecomastia, impotence
    Women: galactorrhoea
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14
Q

MOA of PPIs?
Name ONE.

A
  1. Irreversibly blocks Proton pumps
    Omeprazole
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15
Q

What are the MOAs of PPIs that result in selective proton pump inhibition in the parietal cell canaliculi.

Name.

A
  1. Irreversibly blocks Proton pumps
  2. 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

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16
Q

Whats the duration of action of omeprazole?

A

Duration of action: 24hrs
Half-life / T1/2: 1-2hrs

17
Q

When is the best time to take PPIs? WHY?

A
  1. Empty stomach before breakfast
    - Bioavailability decreases 50% bcs of food
    - Inhibits active pumps -> Best to be present during mealtimes
  2. 1hr before meal
    Half life: 1-2hr
  3. Once daily
    - Irreversibly blocks proton pumps for 24 hrs
18
Q

List adverse effects of omeprazole.

A

Headache, nausea, gas, diarrhoea, dizzy, rash

19
Q

What are the gastric mucosal protection drugs and what do they do?

A
  1. Sucralfate
  2. Bismuth
  3. Misoprostol
  • Protects cells lining walls of stomach & upper GI tract -> time for ulcer to heal
20
Q

Whats the MOA of sucralfate?

A
  1. Binds to (+) charges of damaged proteins in ulcer pit -> forms gel layer which coats & protects the ulcer
  2. Stimulates prostaglandin -> more mucus & bicarb secretion
21
Q

When is the best time to take sucralfate? WHY?

A

On an empty stomach at least 1hr before meals -> prevent drug-food interactions

22
Q

What are the adverse effects of sucralfate?

A
  1. Constipation
  2. Impairs absorption of other drugs
23
Q

Whats the MOA of bismuth compounds?

A
  1. Forms protective layer -> protects ulcers from acid
  2. Stimulates mucus and bicarbonate secretion
  3. Directly some anti-microbial activity against H. pylori
24
Q

What are the adverse effects of bismuth compounds? Precautions to take when taking bismuth?

A
  1. 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
  2. Harmless blackening of stool and reversible darkening of tongue
25
Whats the MOA of misoprostol?
1. Low dose: Stimulates mucus and bicarbonate secretion 2. High dose: Inhibits gastric acid secretion 3. Prevents NSAID-induced ulcers - mimics prostaglandin -> replaces their protective fxns
26
What are the adverse effects of misoprostol?
1. Abdominal pain/cramps 2. Diarrhoea 3. Abortion (uterine contraction) 4. Bone pain and hyperostosis (excessive bone growth)
27
Why is use of misoprostol limited?
1. Adverse effects 2. SHORT half life - 30mins x4 daily dosing -> non-compliance 3. Advent of COX-2 selective NSAIDs 4. Potential for abuse to abort kids
28
What is triple therapy? What isit used for?
H. Pylori eradication = Two abx + 1 PPI (7-14 days) ABX - Clarithromycin + Amoxicillin / Metronidazole (if patient allergic to penicillins) PPI - Omeprazole OR Esomeprazole
29
When to administer triple therapy drugs?
ABX: x2/daily - with/after food within 1 hr to reduce GI adverse effects PPI: x2/daily - maximise dose & ensure sustained increase in pH - before food - ensure it is present in body when proton pumps are most active aftr eating
30
What are the adverse effects of triple therapy?
Diarrhoea, nausea and vomiting
30
What is quadruple therapy? When isit used?
- In areas of high prevalence of resistance to clarithromycin or metronidazole 1 Bismuth + 2 Abx (metronidazole + tetracycline) + 1 PPI / H2 antagonist (10-14 days)
31
What are the PUD drugs that cause drug-drug interactions?
1. Antacids 2. sucralfate (Mucosal protectants - SMB)