Influence of ABCB1 gene polymorphisms on the pharmacokinetics of azithromycin among healthy Chinese Han ethnic subjects |
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| Authors: | Xiao-Jing He Li-Mei Zhao Feng Qiu Ya-Xin Sun Jesse Li-Ling |
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| Institution: | 1. Department of Pharmacy, Shengjing Hospital of China Medical University, Shenyang 110004, China;2. Department of Medical Genetics, China Medical University, Shenyang 110001, China;3. Sino-Dutch Biomedical and Information Engineering School, Northeastern University, Shenyang 110003, China |
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| Abstract: | The aim of this study was to evaluate the effects of ABCB1 gene polymorphisms on azithromycin pharmacokinetics in Chinese Han ethnic subjects. In total, 20 healthy volunteers with various ABCB1 genotypes (6 with 2677GG/3435CC, 8 with 2677GT/3435CT, 6 with 2677TT/3435TT) were enrolled. Each was given a single oral dose of 500 mg azithromycin. Plasma concentration was measured for up to 96 h by LC/MS/MS. As shown, Cmax was significantly lower among individuals with 2677TT/3435TT genotype (468.0 ± 173.4 ng ? h/ml) than those with 2677GG/3435CC (911.2 ± 396.4 ng ? h/ml, p = 0.013). However, the tmax value was higher among subjects with 2677TT/3435TT (2.0 ± 0.5 h) than those with 2677GT/3435CT (1.6 ± 0.3 h) or 2677GG/3435CC (1.4 ± 0.4 h) genotypes (p = 0.068 and p = 0.026, respectively). Furthermore, the AUC last tended to be higher among subjects with 2677GG/3435CC than those with 2677GT/3435CT or 2677TT/3435TT genotypes (5000.2 ± 1610.0 vs. 4558.0 ± 805.0 vs. 4131.0 ± 995.1 ng/ml). Our results showed for the first time that azithromycin pharmacokinetics may be influenced by particular polymorphisms of the ABCB1 gene. Individualized dosage regimen design incorporating such information may improve the efficacy of the drug while reducing adverse reactions. |
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| Keywords: | azithromycin pharmacokinetics single nucleotide polymorphism (SNP) |
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