Clinical Pharmacology of Omeprazole

Research output: Contribution to journalArticle

122 Citations (Scopus)

Abstract

Omeprazole is a specific inhibitor of H+, K+-ATPase or ‘proton pump’ in parietal cells. This enzyme is responsible for the final step in the process of acid secretion; omeprazole blocks acid secretion in response to all stimuli. Single doses produce dose-dependent inhibition with increasing effect over the first few days, reaching a maximum after about 5 days. Doses of omeprazole 20mg daily or greater are able to virtually abolish intragastric acidity in most individuals, although lower doses have a much more variable effect. Omeprazole causes a dose-dependent increase in gastrin levels. Omeprazole must be protected from intragastric acid when given orally, and is therefore administered as encapsulated enteric-coated granules. Absorption can be erratic but is generally rapid, and initially the drug is widely distributed. It is highly protein-bound and extensively metabolised. Its elimination half-life is about 1h but its pharmacological efTecl lasts much longer, since it is preferentially concentrated in parietal cells where it forms a covalent linkage with H+, K+-ATPase, which it irreversibly inhibits. Omeprazole binds to hepatic cytochrome P450 and inhibits oxidative metabolism of some drugs, the most important being Phenytoin. Omeprazole has produced short term healing rates superior to the histamine H2-receptor antagonists in duodenal ulcer, gastric ulcer and reflux oesophagitis. It has also been shown to be highly effective in healing ulcers which have failed to respond to H2-receptor antagonists, and has been extremely valuable in treating patients with Zollinger-Ellison syndrome.

Original languageEnglish (US)
Pages (from-to)38-49
Number of pages12
JournalClinical Pharmacokinetics
Volume20
Issue number1
DOIs
StatePublished - Jan 1 1991

Fingerprint

Omeprazole
Clinical Pharmacology
Proton-Translocating ATPases
Histamine H2 Antagonists
Zollinger-Ellison Syndrome
Proton Pumps
Peptic Esophagitis
Histamine H2 Receptors
Acids
Secretory Pathway
Gastrins
Phenytoin
Stomach Ulcer
Duodenal Ulcer
Pharmaceutical Preparations
Cytochrome P-450 Enzyme System
Ulcer
Half-Life
Pharmacology
Liver

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

Cite this

Clinical Pharmacology of Omeprazole. / Howden, Colin.

In: Clinical Pharmacokinetics, Vol. 20, No. 1, 01.01.1991, p. 38-49.

Research output: Contribution to journalArticle

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