1. Effects of CYP2C9*1/*13 on the pharmacokinetics and pharmacodynamics of meloxicam.
- Author
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Bae JW, Choi CI, Jang CG, and Lee SY
- Subjects
- Adult, Aryl Hydrocarbon Hydroxylases genetics, Asian People, Cytochrome P-450 CYP2C9, Humans, Male, Meloxicam, Metabolic Clearance Rate, Polymorphism, Genetic, Republic of Korea, Young Adult, Anti-Inflammatory Agents, Non-Steroidal pharmacokinetics, Aryl Hydrocarbon Hydroxylases drug effects, Cyclooxygenase Inhibitors pharmacokinetics, Thiazines pharmacokinetics, Thiazoles pharmacokinetics
- Abstract
Aims: To determine the effects of the CYP2C9*1/*13 genotype on the pharmacokinetics and pharmacodynamics of meloxicam in Korean subjects., Methods: Meloxicam (15 mg) was orally administered to 21 healthy Korean volunteers with either the CYP2C9*1/*1 or the CYP2C9*1/*13 genotype. Plasma meloxicam concentrations were analysed by HPLC-UV for 72 h after drug administration. The pharmacodynamic effects of meloxicam were determined by measuring TXB(2) generated in blood., Results: The AUC(0,∞) and C(max) of meloxicam were 2.43- and 1.46-fold higher in the CYP2C9*1/*13 group than in the CYP2C9*1/*1 group, respectively. The oral clearance of meloxicam was significantly lower in the CYP2C9*1/*13 group (37.9% of wild type) than in the CYP2C9*1/*1 group. The t(1/2) of meloxicam was 1.84-fold longer in the CYP2C9*1/*13 group than in the CYP2C9*1/*1 group. The rate of TXB(2) production was significantly lower in the CYP2C9*1/*13 group than in the CYP2C9*1/*1 group., Conclusions: The CYP2C9*1/*13 genotype is associated with decreased metabolism and increased pharmacodynamic effects of meloxicam., (© 2011 The Authors. British Journal of Clinical Pharmacology © 2011 The British Pharmacological Society.)
- Published
- 2011
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