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Stereospecific analysis of omeprazole supports artemisinin as a potent inducer of CYP2C19
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
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1999 (English)In: Fundamental & Clinical Pharmacology, ISSN 0767-3981, E-ISSN 1472-8206, Vol. 13, no 6, 671-675 p.Article in journal (Refereed) Published
Abstract [en]

The purpose of the study was to determine the enantiomer pharmacokinetics of omeprazole and 5-hydroxy-omeprazole before and after administration of the antimalarial artemisinin to confirm artemisinin's ability to induce CYP2C19. Nine healthy male Vietnamese subjects were given a single 20 mg dose of omeprazole orally 1 week before (day -7) artemisinin administration. Artemisinin was then given orally (500 mg) for 7 days (days 1-7). On days 1 and 7, a single 20 mg dose of omeprazole was coadministered with artemisinin. After a washout period of 6 days, a single 20 mg dose of omeprazole was again administered together with a single 500 mg of artemisinin (day 14). Stereoselective pharmacokinetics of omeprazole and 5-hydroxyomeprazole was determined on days of omeprazole administration. Seven days of artemisinin administration significantly decreased the AUC of both omeprazole enantiomers (day 7), compared with day 1 (P < 0.001). All values were normalized after the washout period. Artemisinin increased the AUC ratio of R-5-hydroxyomeprazole/R-omeprazole significantly (P < 0.01) on day 7. The AUC ratio of omeprazole sulphone/S-omeprazole did not differ between study days. Artemisinin decreased the AUC of S-omeprazole to the same extent as that of R-omeprazole in extensive CYP2C19 metabolizers, suggesting that artemisinin induces a different enzyme in addition to CYP2C19. These results support and strengthen earlier findings that artemisinin induces CYP2C19 as well as at least one enzyme other than CYP3A4. 

Place, publisher, year, edition, pages
1999. Vol. 13, no 6, 671-675 p.
Keyword [en]
artemisinin, CYP2C19, metabolism, induction, omeprazole, enantiomers
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-208925ISI: 000084628400008OAI: oai:DiVA.org:uu-208925DiVA: diva2:655486
Available from: 2013-10-11 Created: 2013-10-11 Last updated: 2013-10-14Bibliographically approved

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Svensson, Ulrika S H
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