Effects of CYP2C9*1/*13 on the pharmacokinetics and pharmacodynamics of meloxicam

Jung Woo Bae, Chang Ik Choi, Choon Gon Jang, Seok Yong Lee

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51 Scopus citations

Abstract

To determine the effects of the CYP2C9*1/*13 genotype on the pharmacokinetics and pharmacodynamics of meloxicam in Korean subjects. METHODS Meloxicam (15mg) 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 72h after drug administration. The pharmacodynamic effects of meloxicam were determined by measuring TXB2 generated in blood. RESULTS The AUC(0,∞) and Cmax 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 t1/2 of meloxicam was 1.84-fold longer in the CYP2C9*1/*13 group than in the CYP2C9*1/*1 group. The rate of TXB2 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.

Original languageEnglish
Pages (from-to)550-555
Number of pages6
JournalBritish Journal of Clinical Pharmacology
Volume71
Issue number4
DOIs
StatePublished - Apr 2011

Keywords

  • CYP2C9
  • Genetic polymorphism
  • Meloxicam
  • Pharmacodynamics
  • Pharmacokinetics

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