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达芦那韦:特性、用途和药物相互作用的关键性评价。

Darunavir: a critical review of its properties, use and drug interactions.

机构信息

Drugs and Medicines Quality Control Laboratory, School of Pharmaceutical Sciences University Estadual Paulista, Araraquara, Brazil.

出版信息

Pharmacology. 2012;90(1-2):102-9. doi: 10.1159/000339862. Epub 2012 Jul 12.

Abstract

Darunavir is a synthetic nonpeptidic protease inhibitor which has been shown to be extremely potent against wild-type HIV as well as a large panel of PI-resistant clinical isolates and shows a high genetic barrier to the development of antiretroviral resistance. The treatment of HIV/AIDS requires combinations of multiple antiretroviral drugs. In addition, patients frequently need to coadminister other medications for reasons including the prevention or treatment of opportunistic infections, treatment of concomitant illnesses and management of antiretroviral side effects. Drug interactions have been observed between darunavir and other drugs. New and more comprehensive drug interaction studies will be required since the increase in life expectancy of patients often brings new comorbidities and the concomitant use of different drugs. This paper discusses the impact of the use of darunavir in the treatment of HIV-infected patients, its pharmacological and physical-chemical properties, its drug interactions, and challenges that remain in order to ensure safety and compliance of treatment.

摘要

达芦那韦是一种合成的非肽类蛋白酶抑制剂,对野生型 HIV 以及大量抗蛋白酶抑制剂耐药的临床分离株均具有极强的抑制作用,且具有较高的遗传屏障,不易产生抗药性。治疗 HIV/AIDS 需要多种抗逆转录病毒药物联合治疗。此外,患者经常需要同时使用其他药物,包括预防或治疗机会性感染、治疗合并疾病以及处理抗逆转录病毒药物的副作用等。已经观察到达芦那韦与其他药物之间存在药物相互作用。由于患者的预期寿命延长,往往会带来新的合并症,同时使用不同的药物,因此需要进行新的、更全面的药物相互作用研究。本文讨论了达芦那韦在治疗 HIV 感染患者中的应用、其药理学和理化性质、药物相互作用以及为确保治疗的安全性和依从性而仍然存在的挑战。

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