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恩曲他滨:关于其在HIV感染管理中应用的综述。

Emtricitabine: a review of its use in the management of HIV infection.

作者信息

Frampton James E, Perry Caroline M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2005;65(10):1427-48. doi: 10.2165/00003495-200565100-00008.

DOI:10.2165/00003495-200565100-00008
PMID:15977972
Abstract

Emtricitabine (Emtriva) is an orally administered nucleoside reverse transcriptase inhibitor (NRTI) that is indicated in combination with other antiretroviral agents in the treatment of HIV infection in adults. As a component of antiretroviral therapy (ART), emtricitabine effectively reduces and/or maintains suppression of viral load in ART-naive adults or ART-experienced adults switching from stable combination regimens, and is generally well tolerated. Emtricitabine is a component of preferred initial HIV combination therapy regimens; it can be used in place of lamivudine as part of the dual NRTI backbone in non-nucleoside reverse transcriptase inhibitor (NNRTI)- and protease inhibitor (PI)-based regimens. Moreover, preliminary data from a randomised, open-label study suggest that emtricitabine plus tenofovir DF, a preferred dual-NRTI combination, is better tolerated than co-formulated lamivudine/zidovudine, another preferred dual-NRTI combination, resulting in a higher persistent virological response rate, as analysed using the US FDA time to loss of virological response (TLOVR) algorithm. With the convenience of once-daily (single pill) administration, no dietary restrictions and a favourable drug interaction and tolerability profile, emtricitabine should facilitate patient adherence to treatment, which, in turn, is central to the success of antiretroviral therapy. Similarly, emtricitabine is attractive as an option for ART-experienced stable adults requiring regimen simplification.

摘要

恩曲他滨(Emtriva)是一种口服核苷类逆转录酶抑制剂(NRTI),适用于与其他抗逆转录病毒药物联合使用,治疗成人HIV感染。作为抗逆转录病毒疗法(ART)的一个组成部分,恩曲他滨能有效降低和/或维持初治成人或从稳定联合治疗方案转换过来的经治成人的病毒载量抑制,并且耐受性通常良好。恩曲他滨是首选的初始HIV联合治疗方案的组成部分;在基于非核苷类逆转录酶抑制剂(NNRTI)和蛋白酶抑制剂(PI)的方案中,它可作为双NRTI主干的一部分替代拉米夫定使用。此外,一项随机、开放标签研究的初步数据表明,恩曲他滨加替诺福韦酯(一种首选的双NRTI组合)的耐受性优于另一种首选双NRTI组合——复方拉米夫定/齐多夫定,按照美国食品药品监督管理局(US FDA)的病毒学应答丧失时间(TLOVR)算法分析,其病毒学持续应答率更高。由于每日一次(单一片剂)给药方便、无饮食限制且具有良好的药物相互作用和耐受性,恩曲他滨应有助于患者坚持治疗,而这对于抗逆转录病毒疗法的成功至关重要。同样,对于需要简化治疗方案的经治稳定成人来说,恩曲他滨作为一种选择很有吸引力。

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