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首页> 外文期刊>Pharmacology & Pharmacy >Tramadol in Japanese Population: the Relative Contribution of M1 Metabolite as Assessed by CYP2D6*10 Genotype
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Tramadol in Japanese Population: the Relative Contribution of M1 Metabolite as Assessed by CYP2D6*10 Genotype

机译：日本人群中的曲马多：CYP2D6 * 10基因型评估的M1代谢物的相对贡献

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Several preclinical and clinical studies suggested that tramadol has a multi-mechanistic analgesic action. Upon in vitro evaluation, tramadol parent drug was determined to have only very weak affinity for opioid receptors. Metabolism via CYP2D6, though, yields the O-desmethyl metabolite (M1), which has much greater opioid receptor affinity. In tests in animals and human volunteers, tramadol’s analgesic effect is only partially blocked by the opioid antagonist naloxone. Yet the contribution of parent drug to analgesia is still debated. Observance of good analgesic response to tramadol in Japanese and other Asian populations that express the CYP2D6*10 genotype suggests that parent drug accounts for the majority of tramadol’s analgesic effect in most clinical settings. Understanding of tramadol’s multi-mechanistic action continues to form the basis for understanding its clinical attributes.
机译：多项临床前和临床研究表明，曲马多具有多种机制的镇痛作用。在体外评估后，确定曲马多母体药物对阿片受体的亲和力非常弱。但是，通过CYP2D6进行的代谢会产生O-去甲基代谢物（M1），该物质具有更大的阿片受体亲和力。在对动物和人类志愿者进行的测试中，曲马多的镇痛作用仅被阿片类药物拮抗剂纳洛酮阻断。然而，母药对镇痛的作用仍存在争议。在日本和其他表达CYP2D6 * 10基因型的亚洲人群中，观察到对曲马多的良好镇痛反应表明，在大多数临床情况下，母体药物占曲马多镇痛作用的大部分。对曲马多多种作用的理解继续构成了解其临床特征的基础。

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