• Q Li, R Wang, Y Guo, S Wen, L Xu, and S Wang.
• Department of Pharmacology, Tianjin Medical University, Tianjin, China.
• J Clin Pharm Ther. 2010 Apr 1; 35 (2): 239-47.

ObjectiveTo investigate the relationship between CYP2D6 genetic polymorphisms and the pharmacokinetics of tramadol in Chinese volunteers.MethodA gene chip was established for determining CYP2D6 genotype. Forty adult healthy Chinese subjects were categorized as: group 1, CYP2D6*1/*1; group 2, CYP2D6*2/*2; group 3, CYP2D6*2/*10; group 4, CYP2D6*10/*10. After oral administration of 100 mg tramadol, plasma and urine samples were collected over a 32-h period.ResultsThe main pharmacokinetic parameters of tramadol and its metabolite O-demethyltramadol (M(1)) in groups 1 and 2 were not significantly different. However, they were significantly different between groups 3 and 1, groups 4 and 1 and groups 4 and 3.ConclusionCYP2D6*2 does not alter the pharmacokinetics of tramadol, whereas CYP2D6*10 did with homozygotes showing a more pronounced reduction than heterozygotes. The 32-h metabolic ratio of tramadol to M(1) were (mean +/- SD) 2.05 +/- 1.01, 2.13 +/- 0.83, 4.24 +/- 2.75 and 6.85 +/- 2.78, respectively, in CYP2D6*1/*1, CYP2D6*2/*2, CYP2D6*2/*10 and CYP2D6*10/*10 subjects, respectively.

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