Ranitidine
Mechanism of Action:
- Ranitidine competitively
blocks histamine H₂ receptors on gastric parietal cells, leading to:
- ↓ Histamine-induced gastric
acid secretion
- ↓ Gastrin and
acetylcholine-induced acid secretion (indirectly)
- ↓ Pepsin secretion (due to
reduced volume of gastric juice)
It
reduces basal, nocturnal, and food-stimulated acid secretion.
Pharmacokinetics:
- Route: Oral, IV, IM
- Absorption: Rapid and well-absorbed
orally (~50% bioavailability)
- Onset: Within 1 hour, peak at 2–3
hours
- Duration: 8–12 hours
- Plasma half-life: 2–3 hours
- Metabolism: Partially in the liver
- Excretion: Mainly unchanged in urine
Therapeutic Uses:
Peptic ulcer disease (gastric and duodenal ulcers)
Gastroesophageal reflux disease (GERD)
Stress ulcer prophylaxis in ICU patients
Zollinger-Ellison syndrome (less preferred than PPIs)
Dyspepsia and non-ulcer dyspepsia
Pre-anesthetic medication to reduce acidity and volume of gastric
contents (aspiration prophylaxis)
Adverse Effects:
Generally well-tolerated, but may cause:
- Headache, dizziness
- Nausea, vomiting, diarrhea
or constipation
- Rash
- Rarely:
- Hepatitis (transient rise
in liver enzymes)
- Thrombocytopenia
- Bradycardia (when given IV
rapidly)
- Confusion in elderly (rare,
less than cimetidine)
Drug
Interactions:
- Minimal CYP450 inhibition → minimal drug
interactions.
- May reduce absorption of
drugs requiring acidic pH (e.g., ketoconazole).
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