丁丙诺啡:临床药物动力学在阿片类药物依赖的治疗。

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Elkader, Sproule B

丁丙诺啡:临床药物动力学在阿片类药物依赖的治疗。

Pharmacokinet。2005; 44 (7): 661 - 80。

PubMed ID

15966752 (在PubMed

]

文摘

丁丙诺啡是一种半合成的阿片类药物来源于二甲基吗啡,罂粟的一种天然生物碱,果实。丁丙诺啡的药理学的独特之处在于,它是一个在μ阿片受体部分激动剂。丁丙诺啡经历广泛的初步的新陈代谢,因此口服生物利用度很低;然而,其生物利用度舌下广泛足以让这一个可行的给药途径为阿片类药物依赖的治疗。舌下后的平均最大血浆浓度时间管理是可变的,从40分钟到3.5小时。丁丙诺啡的大量分布和高度蛋白结合的(96%)。它被N-dealkylation广泛代谢norbuprenorphine主要通过细胞色素P450 (CYP) 3 a4。丁丙诺啡的终端消除半衰期长,有相当大的变化,报道值(平均值从3 - 44小时)。大多数的剂量丁丙诺啡是消除粪便,尿液中大约10 - 30%。纳洛酮已被添加到舌下制定丁丙诺啡来减少产品的滥用倾向。 The presence of naloxone does not appear to influence the pharmacokinetics of buprenorphine. Buprenorphine crosses the placenta during pregnancy and also crosses into breast milk. Buprenorphine dosage does not need to be significantly adjusted in patients with renal impairment; however, since CYP3A activity may be decreased in patients with severe chronic liver disease, it is possible that the metabolism of buprenorphine will be altered in these patients. Although there is limited evidence in the literature to date, drugs that are known to inhibit or induce CYP3A4 have the potential to diminish or enhance buprenorphine N-dealkylation. It appears that the interaction between buprenorphine and benzodiazepines is more likely to be a pharmacodynamic (additive or synergistic) than a pharmacokinetic interaction. The relationship between buprenorphine plasma concentration and response in the treatment of opioid dependence has not been well studied. The pharmacokinetic and pharmacodynamic properties of buprenorphine allow it to be a feasible option for substitution therapy in the treatment of opioid dependence.

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药物

丁丙诺啡