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Omeprazole

Pharmacology

Clinical Particulars

Regulatory Class

Omeprazole is a substituted benzimidazole

Pharmacodynamics

Pharmacokinetics

Mechanism of Action

  • Proton Pump Inhibitor: Omeprazole is a selective and irreversible proton pump inhibitor. In an acidic environment, activated omeprazole becomes a sulfenamide derivative that binds irreversibly at the secretory surface of parietal cells to the enzyme H+/K+ ATPase. This binding inhibits the transport of hydrogen ions into the stomach by 90% to 99%. Omeprazole blocks/prevents histamine, acetylcholine and gastrin-induced acid secretion. Omeprazole blocks gastric acid secretion irrespective of the stimulus. Omeprazole is inactive at physiological pH and has a limited effect on systemic ATP-ase.

Applications

  • Antacid & Gastroprotection

  • GERD Reflux Oesophagitis

  • Helicobacteriosis

  • Gastrinoma

  • CSF Reduction

Pharmacodynamics

Metabolism

  • Hepatic: Omeprazole is metabolised extensively in the liver to multiple metabolites (typically Hydroxyomeprazole and Omeprazole sulfone). Significant hepatic dysfunction can reduce the first-pass effect of Omeprazole, increasing the systemically available drug and prolonging its duration of action.

Elimination

  • Mixed Urine and Faeco-Biliary Excretion: Mainly as metabolites. Metabolites are mainly excreted in urine, but some are excreted via the biliary route in faeces.

Pharmacokinetics

Precautions

Precautions

Availability

Availability

Identifiers

Systematic [IUPAC] Name:  6-methoxy-2-[ (4-methoxy-3,5-dimethylpyridin-2-yl) methylsulfinyl]-1H-benzimidazole]. Omeprazole is a substituted benzimidazole.

  • Formula: C17-H19-N3-O3-S

  • Pharmacotherapeutic group: Proton Pump Inhibitor and Cytochrome P450 2C19 Inhibitor.

  • ATC Vet Code: QA02BC01

  • ATC Code: A02BC01

Identifiers

Evidence Base

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  7. Banisaeed, N., Truding, R.M., Chang, C., 2003. Tetracycline-induced spongiotic esophagitis: a new endoscopic and histopathologic finding. Gastrointestinal Endoscopy, Review Article: Dieulafoy’s Lession 58, 292–294. https://doi.org/10.1067/mge.2003.364

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