Influence of ABCB1 gene polymorphisms on the pharmacokinetics of azithromycin among healthy Chinese Han ethnic subjects.

Journal Title: Pharmacological Reports - Year 2009, Vol 61, Issue 5

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, C(max) was significantly lower among individuals with 2677TT/3435TT genotype (468.0 +/- 173.4 ng x h/ml) than those with 2677GG/3435CC (911.2 +/- 396.4 ng x h/ml, p = 0.013). However, the t(max) 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.

Authors and Affiliations

Xiao-Jing He, Li-Mei Zhao, Feng Qiu, Ya-Xin Sun, Jesse Li-Ling

Keywords

Related Articles

Effects of diphenhydramine and famotidine on lipid peroxidation and activities of antioxidant enzymes in different rat tissues.

The potential antioxidant activity of diphenhydramine (histamine H(1)-receptor antagonist) and famotidine (histamine H(2) receptor antagonist) was studied. Diphenhydramine inhibited the spontaneous, Fe(II)-induced and Fe...

Acute and repeated treatment with the 5-HT(7) receptor antagonist SB 269970 induces functional desensitization of 5-HT(7) receptors in rat hippocampus.

Background: SB 269970, a 5-HT(7) receptor antagonist may produce a faster antidepressant-like effect in animal models, than do antidepressant drugs, e.g., imipramine. The present work was aimed at examining the effect of...

Blocking angiogenesis with peptides that inhibit the activity of procollagen C-endopeptidase.

Procollagen C-endopeptidase (BMP-1) is one of two key enzymes crucial for conversion of fibrillar procollagens to self-assembling collagen monomers. Recently, we have reported inhibition of the largest variant of BMP-1,...

Association between remote organ injury and tissue polyamine homeostasis in acute experimental pancreatitis - treatment with a polyamine analogue bismethylspermine.

Experimental pancreatitis is associated with activation of polyamine catabolism. The polyamine analog bismethylspermine (Me(2)Spm) can ameliorate pancreatic injury. We investigated the roles of polyamine catabolism in re...

Raloxifene similarly affects the skeletal system of male and ovariectomized female rats.

Raloxifene, a selective estrogen receptor modulator, is used for prevention and treatment of osteoporosis in postmenopausal women. Raloxifene use in male subjects is increasingly considered and a few clinical studies of...

Download PDF file
  • EP ID EP83332
  • DOI -
  • Views 116
  • Downloads 0

How To Cite

Xiao-Jing He, Li-Mei Zhao, Feng Qiu, Ya-Xin Sun, Jesse Li-Ling (2009). Influence of ABCB1 gene polymorphisms on the pharmacokinetics of azithromycin among healthy Chinese Han ethnic subjects.. Pharmacological Reports, 61(5), 843-850. https://europub.co.uk/articles/-A-83332