丁丙诺啡：一种在阿片类药物成瘾治疗中作用不断扩大的镇痛药。
Buprenorphine: an analgesic with an expanding role in the treatment of opioid addiction.
作者信息
Robinson Susan E
机构信息
Department of Pharmacology and Toxicology, P O Box 980613, Virginia Commonwealth University, Richmond, VA 23298-0613, USA.
出版信息
CNS Drug Rev. 2002 Winter;8(4):377-90. doi: 10.1111/j.1527-3458.2002.tb00235.x.
Buprenorphine, a long-acting opioid with both agonist and antagonist properties, binds to mu-opioid (OP(3)), kappa-opioid (OP(2)), delta-opioid (OP(1)), and nociceptin (ORL-1) receptors. Its actions at these receptors have not been completely characterized, although buprenorphine is generally regarded as a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist. Its pharmacology is further complicated by an active metabolite, norbuprenorphine. Although buprenorphine can be used as an analgesic agent, it is of greater importance in the treatment of opioid abuse. Because of its partial agonist activity at mu-opioid receptors and its long half-life, buprenorphine has proven to be an excellent alternative to methadone for either maintenance therapy or detoxification of the opioid addict. Although buprenorphine may ultimately prove to be superior to methadone in the maintenance of the pregnant addict, its effects on the developing fetus must be carefully evaluated.
丁丙诺啡是一种具有激动剂和拮抗剂特性的长效阿片类药物，可与μ阿片受体（OP(3)）、κ阿片受体（OP(2)）、δ阿片受体（OP(1)）和孤啡肽（ORL-1）受体结合。尽管丁丙诺啡通常被视为μ阿片受体部分激动剂和κ阿片受体拮抗剂，但其在这些受体上的作用尚未完全明确。其活性代谢产物去甲丁丙诺啡使丁丙诺啡的药理学特性更为复杂。尽管丁丙诺啡可用作镇痛药，但它在阿片类药物滥用治疗中更为重要。由于丁丙诺啡在μ阿片受体上具有部分激动剂活性且半衰期长，已证明它是美沙酮用于阿片类成瘾者维持治疗或脱毒的极佳替代品。尽管丁丙诺啡最终可能被证明在维持妊娠成瘾者方面优于美沙酮，但必须仔细评估其对发育中胎儿的影响。
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