论文部分内容阅读
（±）－曲马多（Ｔｒａｍａｄｏｌ）是一种与阿片受体的亲和力很低的中枢性镇痛剂。其Ｍ_１代谢物Ｏ－去甲曲马多）的生成率可以受ｄｅｂｒｉｓｏｑｕｉｎｅ型多形性的影响，此代谢物对阿片受体比其母体（曲马多）有更高的亲和力。临床观察和实验室研究的结果表明曲马多也可能直接作用于中枢单胺能通路发挥镇痛效应。事实上，一次口服剂量的曲马多所发挥的抗伤害性感受效应中μ受体激动剂的成分很小，大部分的镇痛效应来自其非阿片性质。在多次给药治疗中药物本身及其Ｍ_１代谢物的累积浓度大约可达２倍。一次口服１００毫克曲马多的镇痛效应大约可维持６小时。临床实践证实曲马多是一种相对完全的镇痛药，可能适合于不需要强阿片样物质治疗的疼痛患者。
(±) - Tramadol is a central analgesic with a low affinity for opioid receptors. Its M 1 metabolite O-desmethyltramadol) can be affected by the debrisoquine polymorphism, which has a higher affinity for opioid receptors than its parent (tramadol). Clinical observations and laboratory studies have shown that tramadol may also act directly on the central monoamine pathway to exert analgesic effects. In fact, a single dose of tramadol exerts a very small fraction of μ-agonist in the antinociceptive response and most of the analgesic effect comes from its non-opiate properties. In multiple administrations, the cumulative concentration of the drug itself and its M 1 metabolite can be up to 2-fold. The analgesic effect of 100 mg of tramadol once orally can last about 6 hours. Clinical practice has confirmed that tramadol is a relatively complete analgesic and may be suitable for painful patients who do not require strong opioid therapy.