This study included 24 healthy volunteers who received a single 37.5 mg oral dose of tramadol. We analyzed 18 polymorphisms within CYP2D6, CYP2B6, CYP3A, COMT, ABCB1, SLC22A1 and OPRM1 genes by quantitative PCR, to study whether these polymorphisms affect its pharmacokinetics, pharmacodynamics and safety. CYP2D6 intermediate metabolizers (n = 6) showed higher tramadol plasma concentrations and lower clearance compared with normal and ultrarapid metabolizers. CYP2B6 G516T T/T (n = 2) genotype was also associated to higher tramadol plasma levels. No other polymorphism affected tramadol pharmacokinetics. Three volunteers experienced a prolonged QTc not associated with the genetic variants studied or altered phamacokinetic parameters. The correlation of CYP2B6 genotype with higher tramadol concentrations is remarkable since its influence on its elimination is also relevant and has been less studied to date. However, given our small sample size, it is important to interpret our results with caution.

译文

这项研究包括24名健康志愿者,他们接受了单次37.5毫克的曲马多口服剂量。我们通过定量PCR分析了CYP2D6,CYP2B6,CYP3A,COMT,ABCB1,SLC22A1和OPRM1基因内的18个多态性,以研究这些多态性是否影响其药代动力学,药效学和安全性。CYP2D6中间代谢者 (n = 6) 显示出较高的曲马多血浆浓度和较低的清除率与正常和超类代谢者相比。CYP2B6 G516T T/T (n = 2) 基因型也与较高的曲马多血浆水平相关。没有其他多态性影响曲马多的药代动力学。三名志愿者经历了长时间的QTc,与所研究的遗传变异或遗传动力学参数的改变无关。CYP2B6基因型与较高曲马多浓度的相关性是显着的,因为它对其消除的影响也是相关的,迄今为止研究较少。但是,鉴于我们的样本量较小,因此谨慎解释我们的结果很重要。

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