Effect of the CYP2C19 oxidation polymorphism on fluoxetine metabolism in Chinese healthy subjects

Aims The study was designed to investigate whether genetically determined CYP2C19 activity affects the metabolism of fluoxetine in healthy subjects. Methods A single oral dose of fluoxetine (40 mg) was administrated successively to 14 healthy young men with high (extensive metabolizers, n=8) and l...

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Veröffentlicht in:	British journal of clinical pharmacology 2001-07, Vol.52 (1), p.96-99
Hauptverfasser:	Liu, Zhao‐Qian, Cheng, Ze‐Neng, Huang, Song‐Lin, Chen, Xiao‐Ping, Ou‐Yang, Dong‐Sheng, Jiang, Chang‐Hong, Zhou, Hong‐Hao
Format:	Artikel
Sprache:	eng
Schlagworte:	Adolescent Adult Aryl Hydrocarbon Hydroxylases Biotransformation China - epidemiology Chromatography, High Pressure Liquid CYP2C19 Cytochrome P-450 CYP2C19 Cytochrome P-450 Enzyme System - genetics Cytochrome P-450 Enzyme System - metabolism fluoxetine Fluoxetine - analogs & derivatives Fluoxetine - pharmacokinetics Gene Dosage gene dose Genotype Humans Liver - metabolism Male Mixed Function Oxygenases - genetics Mixed Function Oxygenases - metabolism Mutation norfluoxetine Oxidation-Reduction pharmacokinetics Polymorphism, Genetic Serotonin Uptake Inhibitors - pharmacokinetics Short Reports
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Zusammenfassung:	Aims The study was designed to investigate whether genetically determined CYP2C19 activity affects the metabolism of fluoxetine in healthy subjects. Methods A single oral dose of fluoxetine (40 mg) was administrated successively to 14 healthy young men with high (extensive metabolizers, n=8) and low (poor metabolizers, n = 6) CYP2C19 activity. Blood samples were collected for 5–7 half‐lives and fluoxetine, and norfluoxetine were determined by reversed‐phase high performance liquid chromatography. Results Poor metabolizers (PMs) showed a mean 46% increase in fluoxetine peak plasma concentrations (Cmax, P
ISSN:	0306-5251 1365-2125
DOI:	10.1046/j.0306-5251.2001.01402.x