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[依曲韦林用于一线治疗]

[Etravirine in first-line therapy].

作者信息

Garcés Piedad Arazo, Tena Esther Valero

机构信息

Hospital Universitario Miguel Servet, Zaragoza, España.

出版信息

Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:12-20. doi: 10.1016/S0213-005X(09)73214-8.

Abstract

Etravirine (ETR) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with a potent and broad in vitro spectrum of activity against HIV-1 and viruses with NNRTI resistances, allowing sequential use of drugs of this family. The potency, efficacy and safety of etravirine have been demonstrated in multi-treated patients, but few data are available on first-line antiretroviral therapy (ART) and the role of this drug in initial treatment phases has not been defined. The presence of primary NNRTI resistances and those acquired during first-line therapy is increasingly frequent. Due to its genetic barrier and efficacy, ETR can form part of a second-line ART regimen in patients with failure to a first-line regimen. In the initial phases, adverse effects continue to be the main reason for modifying ART. ETR has demonstrated safety and tolerability, with no central nervous system adverse effects and a good liver, lipid and gastrointestinal safety profile. As with the other NNRTIs, the most common adverse effect is rash. Because of ETR good tolerability profile, this drug can be considered when a new treatment is required due to adverse effects. Because of the characteristics of ETR the possibility of once-daily administration and dissolution in water, as well as the absence of drug-drug interactions with methadone this drug is especially attractive as a firstline therapy and in patients with poor adherence, such as intravenous drug users receiving methadone treatment.

摘要

依曲韦林(ETR)是一种非核苷类逆转录酶抑制剂(NNRTI),在体外对HIV-1及具有NNRTI耐药性的病毒具有强大且广泛的活性谱,使得该类药物可序贯使用。依曲韦林的效力、疗效及安全性已在接受多种治疗的患者中得到证实,但关于一线抗逆转录病毒治疗(ART)的数据较少,且该药物在初始治疗阶段的作用尚未明确。原发性NNRTI耐药以及在一线治疗期间获得的耐药情况日益常见。由于其基因屏障和疗效,依曲韦林可成为一线治疗方案失败患者二线ART方案的一部分。在初始阶段,不良反应仍是调整ART的主要原因。依曲韦林已证明具有安全性和耐受性,无中枢神经系统不良反应,肝脏、脂质及胃肠道安全性良好。与其他NNRTIs一样,最常见的不良反应是皮疹。由于依曲韦林耐受性良好,当因不良反应需要新的治疗时可考虑使用该药物。鉴于依曲韦林具有一日一次给药、可溶于水的特点,以及与美沙酮不存在药物相互作用,该药物作为一线治疗药物以及对于依从性差的患者(如接受美沙酮治疗的静脉吸毒者)尤其具有吸引力。

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