HIV蛋白酶抑制剂的药代动力学相互作用

摘要/Abstract

摘要： 艾滋病的治疗是一个长期的过程,HIV蛋白酶抑制剂是此类病人最常选用的抗病毒药物。在治疗过程中,病人很可能患其它疾病,艾滋病自身也常伴随众多并发症,使得临床上不可避免的需要联用其它药物。由于HIV蛋白酶抑制剂对药物代谢酶和转运体有广泛的作用,因此探索HIV蛋白酶抑制剂的药物相互作用问题显得十分必要。本文重点从药代相互作用机制的角度综述了HIV蛋白酶抑制剂在临床上可能出现的药物相互作用方面的研究文献,包括HIV蛋白酶抑制剂与其它药物的相互作用以及蛋白酶抑制剂之间的相互作用及机制等,期望对于临床给药方案的设计和提高临床用药的安全性和有效性提供有价值的参考和借鉴。

关键词: HIV蛋白酶抑制剂, 相互作用, CYP3A4, P-糖蛋白

Abstract: HIV protease inhibitors are the frontline drugs for the management of acquired immune deficiency syndrome during its long-term therapy. A combined medication of HIV protease inhibitors with other drugs is often used when the patients are accompanied with other diseases or complications. As is known, HIV protease inhibitors have extensive pharmacokinetic effects on cytochrome oxidase P450s and transporters so that drug interactions may take place, which are negative to clinic therapy. In this article, we review the relevant reports on drug interactions between HIV protease inhibitors and other drugs, and amongst themselves, putting more emphasis on mechanism-based pharmacokinetic interaction. Hopefully, this summary can be useful to evaluate clinic regiment designs and improve safety and efficacy of drugs in a combined medication.

Key words: HIV protease inhibitors, Interactions, CYP450, P-gp

中图分类号:

R969. 2

顾融融, 石建, 阿基业, 王广基. HIV蛋白酶抑制剂的药代动力学相互作用[J]. 中国临床药理学与治疗学, 2012, 17(4): 472-480.

GU Rong-rong, SHI Jian, A Ji-ye, WANG Guang-ji. Pharmacokinetic interactions of HIV protease inhibitors[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2012, 17(4): 472-480.

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