Strongly increased exposure of meloxicam in CYP2C9*3/*3 individuals.

Abstract:

OBJECTIVE:The effects of CYP2C9*1/*3 and *3/*3 genotypes on the pharmacokinetics and pharmacodynamics of meloxicam were evaluated in healthy Korean subjects. METHODS:After oral administration of 15 mg meloxicam, the plasma concentrations of meloxicam were assessed in 11 CYP2C9*1/*1 individuals, eight CYP2C9*1/*3 individuals, and three CYP2C9*3/*3 individuals. The pharmacodynamic effects were determined by measuring thromboxane B2 generated in blood. RESULTS:A nine-fold lower apparent oral clearance and an eight-fold higher AUC0-∞ of single-dose meloxicam were observed in CYP2C9*3/*3 individuals when compared with CYP2C9*1/*1 individuals. CYP2C9*3/*3 individuals also showed markedly increased inhibition of thromboxane B2 generation by meloxicam. CONCLUSION:These results indicate that CYP2C9*3/*3 individuals may be at a higher risk for concentration-dependent adverse effects during long-term treatment with standard doses of meloxicam.

journal_name

Pharmacogenet Genomics

authors

Lee HI,Bae JW,Choi CI,Lee YJ,Byeon JY,Jang CG,Lee SY

doi

10.1097/FPC.0000000000000025

subject

Has Abstract

pub_date

2014-02-01 00:00:00

pages

113-7

issue

2

eissn

1744-6872

issn

1744-6880

journal_volume

24

pub_type

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