重度抑郁症的安非他酮:药代动力学和配方方面的考虑。

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杰弗逊JW, Pradko摩根富林明,缪尔KT次方

重度抑郁症的安非他酮:药代动力学和配方方面的考虑。

其他。2005年11月,27 (11):1685 - 95。

PubMed ID

16368442 (在PubMed

]

文摘

背景:重度抑郁症(MDD)是一种常见的精神状态,在美国有6.6%的成年人在任何一年经历严重抑郁发作。抑郁症患者必须接受适当治疗临床成功的可能性最大化。盐酸安非他酮、去甲/多巴胺的抗抑郁药,可在3口服剂型:立即释放(IR) (TID),持续释放(SR)(招标),和扩展释放(XL) (QD)。理解安非他酮的药代动力学(PK)属性和配方可以帮助优化临床使用。目的:本文的目的是提供一个审查的PK安非他酮的性质和识别它的各种剂型和临床应用,帮助优化治疗MDD。方法:综述、数据/报告收集的文章关于PK试验确认使用PubMed搜索。必威国际app搜索是没必威国际app有日期限制和使用搜索词安非他酮,老安非他酮,安非他酮XL,安非他酮药物动力学,安非他酮代谢和安非他酮药物的相互作用。额外的报告从引用被选中,出现在文章中确定原来的搜索。必威国际app此外,研究了产品信息和标签的数据。所有可用的信息,关注人类的研究,相关的安非他酮PK属性和/或配方是包括在内。 RESULTS: : Bupropion is extensively metabolized by the liver (t(1/2), approximately 21 hours). Hydroxybupropion, the primary active metabolite (t(1/2), approximately 20 hours), is formed by cytochrome P450 (CYP) 2B6. At steady state, C(max) of hydroxybupropion is 4- to 7-fold higher, and the AUC is approximately 10-fold greater, compared with those of the parent drug. Threohydrobupropion and erythrohydrobupropion (mean [SD] t(1/2) values, approximately 37 [13] and approximately 33 [10] hours, respectively), the other active metabolites of bupropion, are formed via nonmicrosomal pathways. Relative to bupropion, the C(max) values are approximately 5-fold greater for threohydrobupropion and similar for erythrohydrobupropion. Based on a mouse antitetrabenazine model, hydroxybupropion is approximately 50% as active as bupropion, and threohydrobupropion and erythrohydrobupropion are approximately 20% as active as bupropion. Bupropion lowers the seizure threshold and, therefore, concurrent administration with other agents that lower the seizure threshold should be undertaken cautiously. Potential interactions with other agents that are metabolized by CYP2B6 should be considered. In addition, bupropion inhibits CYP2D6 and may reduce clearance of agents metabolized by this enzyme. Absorption of the XL formulation is prolonged compared with the IR and SR formulations (T(max), approximately 5 hours vs approximately 1.5 and approximately 3 hours, respectively). Bupropion is dosed without regard to food. CONCLUSIONS: : Understanding the PK profile and formulations of bupropion can help optimize clinical use. Bupropion is metabolized extensively, resulting in 3 active metabolites. This metabolic profile, various patient factors (eg, age, medical illnesses), and potential drug interactions should be considered when prescribing bupropion. The 3 formulations-bupropion, bupropion SR, and bupropion XL-are bioequivalent and offer options to optimize treatment for patients with MDD.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
安非他酮	细胞色素P450 2 b6	蛋白质	人类	未知的	底物	细节