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Wiley InterScience | ||||||
  British Journal of Clinical PharmacologyVolume 42 Issue 2, Pages 157 - 162 Published Online: 2 Oct 2003 Journal compilation © 2010 The British Pharmacological Society The Journal of The British Pharmacological Society
Abstract | Full Text: PDF (Size: 355K) | Related Articles | Citation Tracking  Diazepam–omeprazole inhibition interaction: an in vitro investigation using human liver microsomes KEYWORDS omeprazole • diazepam • omeprazole sulphone • human microsomes •
in vitro metabolism • drug interactions • CYP3A • CYP2C19 ABSTRACT
1The metabolism of diazepam to its primary metabolites 3-hydroxydiazepam (3HDZ) and nordiazepam (NDZ) was evaluated in human liver microsomes. The 3HDZ pathway was the major route of metabolism representing 90% of total metabolism with a V
2Inhibition of the two metabolic pathways of diazepam by omeprazole was investigated. The NDZ pathway was not affected by omeprazole whilst a K
3Inhibitory effects of omeprazole sulphone on the 3HDZ and NDZ pathways were also investigated. Omeprazole sulphone inhibited both pathways with similar K 4These in vitro data provide direct evidence for cytochrome P450 inhibition as the mechanism for the well documented diazepam-omeprazole clinical interaction and indicate that omeprazole sulphone, as well as the parent drug, contribute to the inhibition effect.
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