title: Omeprazole: pharmacokinetics and metabolism in man.
abstract: Omeprazole is acid labile and, therefore, has to be protected from exposure to the acidic gastric juice when given orally. Following a single oral dose of buffered suspension, omeprazole is rapidly absorbed with peak plasma concentrations within 0.5 hours. The volume of distribution is 0.3 litres/kg corresponding to the volume of extracellular water. In contrast to the long duration of antisecretory action, omeprazole is rapidly eliminated from plasma. The half-life is less than 1 hour, and omeprazole is almost entirely cleared from plasma within 3-4 hours. Omeprazole is completely metabolized in the liver. The two major plasma metabolites are the sulphone and hydroxyomeprazole, neither of which contributes to the antisecretory activity. About 80% of a given dose is excreted in the urine, and the remainder via the bile. The absorption of the coated granule formulation dispensed in hard gelatine capsules is slower, with peak concentrations 1-3 hours after dose. Bioavailability after a single dose is 35% and increases during repeated once-daily dosing to 60%. Omeprazole can potentially interact with the hepatic microsomal cytochrome P-450 enzymes. Studies show that the clearance of both diazepam and phenytoin are decreased and their terminal half-lives are increased during concomitant omeprazole treatment, both interactions being attributable to inhibition of hepatic metabolism. No interaction with propranolol or theophylline has been noted.
authors.affiliation: Hässle Research Laboratories, Mölndal, Sweden.
authors.forename: C
authors.initials: C
authors.lastname: Cederberg
authors.forename: T
authors.initials: T
authors.lastname: Andersson
authors.forename: I
authors.initials: I
authors.lastname: Skånberg
mesh_terms: D000284:Administration, Oral; D005744:Gastric Acid / Q000378:metabolism; D006801:Humans; D008657:Metabolic Clearance Rate; D009853:Omeprazole / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D009853:Omeprazole