Short detailed note on Omeprazole

Omeprazole

 Mechanism of Action:

  • Omeprazole irreversibly inhibits the H⁺/K⁺ ATPase (proton pump) present on the luminal surface of gastric parietal cells.
  • This blocks the final step of gastric acid secretion, reducing both basal and stimulated acid secretion.
  • Since it binds covalently, new proton pumps need to be synthesized for acid secretion to resume.

 Pharmacokinetics:

  • Route: Oral
  • Form: Enteric-coated capsules/tablets (acid-labile, destroyed by gastric acid)
  • Absorption: In small intestine, bioavailability ~35-40% (increased on repeated dosing).
  • Plasma half-life: 1–2 hours, but duration of action lasts ~24 hours due to irreversible binding.
  • Metabolism: Extensively in the liver (CYP2C19, CYP3A4).
  • Excretion: Urine and feces.

Therapeutic Uses:

    Peptic ulcer disease (gastric and duodenal ulcers)
    Gastroesophageal reflux disease (GERD)
    Zollinger-Ellison syndrome (hypersecretory conditions)
    Prevention and treatment of NSAID-induced ulcers
    Part of H. pylori eradication regimens (triple therapy: Omeprazole + Clarithromycin + Amoxicillin/Metronidazole)

 Adverse Effects:

  • Common:
    • Headache
    • Nausea, vomiting
    • Diarrhea or constipation
    • Abdominal pain
  • Long-term use:
    • Vitamin B₁₂ deficiency (↓ acid → ↓ B₁₂ release)
    • Hypomagnesemia
    • Increased risk of fractures (hip, spine, wrist)
    • Increased risk of enteric infections (e.g., Clostridium difficile)
    • Hypergastrinemia (rebound acid hypersecretion on sudden withdrawal)

Drug Interactions:

  • Omeprazole inhibits CYP2C19, which can:
    • Decrease activation of Clopidogrel (↓ antiplatelet effect).
    • Increase levels of Phenytoin, Diazepam, Warfarin.
  • Decreased absorption of drugs requiring acidic pH:
    • Ketoconazole, Itraconazole, Iron, Vitamin B₁₂.

Contraindications:

  • Known hypersensitivity
  • Caution in severe hepatic impairment.

Dose:

  • 20–40 mg once daily, before meals, preferably in the morning.
                                                                     END OF THE DOCUMENT

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