Dayer P, Collart L, Desmeules J
Division of Clinical Pharmacology and Pain Clinic, University Hospital, Geneva, Switzerland.
Drugs. 1994;47 Suppl 1:3-7. doi: 10.2165/00003495-199400471-00003.
(+/-)-Tramadol is a central analgesic with low affinity for opioid receptors. The rate of production of its M1 metabolite (O-demethyl tramadol) is influenced by debrisoquine-type polymorphism, and this metabolite shows a higher affinity for opioid receptors than the parent drug. Experimental and clinical data suggest that tramadol may also exert its analgesic effect through direct modulation of central monaminergic pathways. Indeed, after a single oral dose, the role of the mu-receptor agonist component of the antinociceptive effect of tramadol appears to be minor, with most of the analgesic effect being attributable to nonopioid properties of the parent compound. Approximately 2-fold accumulation of the parent compound and the M1 metabolite may be expected during multiple dose treatment. The duration of analgesic effect after a single oral dose of tramadol 100 mg is about 6 hours. Clinical experience has confirmed that tramadol is an effective and relatively safe analgesic that may be of value in several pain conditions not requiring treatment with strong opioids.
（±）-曲马多是一种对阿片受体亲和力较低的中枢性镇痛药。其M1代谢产物（O-去甲基曲马多）的生成速率受异喹胍型多态性影响，且该代谢产物对阿片受体的亲和力高于母体药物。实验和临床数据表明，曲马多也可能通过直接调节中枢单胺能途径发挥其镇痛作用。实际上，单次口服给药后，曲马多镇痛作用中μ受体激动剂成分的作用似乎较小，其大部分镇痛作用归因于母体化合物的非阿片类特性。在多剂量治疗期间，母体化合物和M1代谢产物可能会有大约2倍的蓄积。单次口服100mg曲马多后的镇痛作用持续时间约为6小时。临床经验证实，曲马多是一种有效且相对安全的镇痛药，在几种不需要用强效阿片类药物治疗的疼痛状况中可能具有价值。
