Department of Anesthesiology and Pain Medicine, Nationwide Children's Hospital and The Ohio State University, 700 Children's Drive, Columbus, OH , 43205, USA.
J Anesth. 2021 Feb;35(1):130-141. doi: 10.1007/s00540-020-02887-4. Epub 2021 Jan 12.
Like morphine, methadone is a pure agonist at the µ opioid receptor. However, in distinction to morphine which has an elimination half-life of 2-3 h, methadone has an elimination half-life of 24-36 h. In addition to its effects at the µ opioid receptor, methadone is an antagonist at the N-methyl-D-aspartate (NMDA) receptor and also inhibits the reuptake of the neurotransmitters, serotonin and norepinephrine, in the central nervous system. Given its long half-life and high oral bioavailability, methadone has had a primary role in the outpatient treatment of patients with a history of opioid abuse or addiction. However, its unique pharmacology and cellular effects make it a valuable agent in the treatment of both acute and chronic pain of various etiologies. The following manuscript reviews the pharmacologic properties of methadone and discusses its clinical applications in the practice of pediatric anesthesiology and pediatric critical care medicine.
就像吗啡一样，美沙酮也是μ阿片受体的纯激动剂。然而，与半衰期为 2-3 小时的吗啡不同，美沙酮的半衰期为 24-36 小时。除了在μ阿片受体上的作用外，美沙酮还是 N-甲基-D-天冬氨酸（NMDA）受体的拮抗剂，并且还抑制中枢神经系统中神经递质 5-羟色胺和去甲肾上腺素的再摄取。由于其半衰期长且口服生物利用度高，美沙酮在门诊治疗有阿片类药物滥用或成瘾史的患者方面发挥了主要作用。然而，其独特的药理学和细胞效应使其成为治疗各种病因的急性和慢性疼痛的有价值的药物。以下手稿综述了美沙酮的药理学特性，并讨论了其在小儿麻醉学和小儿危重病医学实践中的临床应用。
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