In vivo inhibition of CYP2C19 but not CYP2D6 by fluvoxamine
Open Access
- 1 October 1996
- journal article
- Published by Wiley in British Journal of Clinical Pharmacology
- Vol. 42 (4) , 518-521
- https://doi.org/10.1111/j.1365-2125.1996.tb00019.x
Abstract
Studies were performed in eight healthy extensive metabolizers of mephenytoin and debrisoquine to determine the effect of fluvoxamine on the activities of S‐mephenytoin 4′‐hydroxylase (CYP2C19) and metoprolol α‐hydroxylase (CYP2D6). Therapeutic dosing with fluvoxamine (100 mg day−1) for 2 weeks caused a significant increase in the 0–8 h urinary S/R ratio of mephenytoin from 0.16 to 0.55 (95% confidence interval for difference between means: 0.28–0.50; PP0.05) or the 0–8 h urinary recovery of α‐hydroxymetoprolol (95% confidence interval for difference between means: −0.61–0.70 mg; P >0.05). These results indicated fluvoxamine has a modest inhibitory effect on the activity of CYP2C19, but no effect on that of CYP2D6 in vivo.Keywords
This publication has 26 references indexed in Scilit:
- Effect of cigarette smoking on fluvoxamine pharmacokinetics in humansClinical Pharmacology & Therapeutics, 1995
- Evidence That CYP2C19 is the Major (S)-Mephenytoin 4'-Hydroxylase in HumansBiochemistry, 1994
- A pharmacokinetic and pharmacodynamic evaluation of the combined administration of alprazolam and fluvoxamineEuropean Journal of Clinical Pharmacology, 1994
- Effect of Fluvoxamine on the Pharmacokinetics of Imipramine and Desipramine in Healthy SubjectsTherapeutic Drug Monitoring, 1993
- Fluvoxamine is a potent inhibitor of cytochrome P4501A2Biochemical Pharmacology, 1993
- The effect of enzyme induction on the cytochrome P450-mediated bioactivation of carbamazepine by mouse liver microsomesBiochemical Pharmacology, 1992
- Inhibitors of imipramine metabolism by human liver microsomes.British Journal of Clinical Pharmacology, 1992
- Fluvoxamine-tricyclic antidepressant interactionEuropean Journal of Clinical Pharmacology, 1991
- Characterisation of theophylline metabolism by human liver microsomesBiochemical Pharmacology, 1988
- FluvoxamineDrugs, 1986