1. Strongly increased exposure of meloxicam in CYP2C9∗3/∗3 individuals.
- Author
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Lee, Hye-In, Bae, Jung-Woo, Choi, Chang-Ik, Lee, Yun-Jeong, Byeon, Ji-Yeong, Jang, Choon-Gon, and Lee, Seok-Yong
- Abstract
The effects of CYP2C9∗1/∗3 and ∗3/∗3 genotypes on the pharmacokinetics and pharmacodynamics of meloxicam were evaluated in healthy Korean subjects.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.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.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. [ABSTRACT FROM AUTHOR]
- Published
- 2014
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