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[依曲韦林的安全性与耐受性]

[Safety and tolerability of etravirine].

作者信息

Portilla Joaquín

机构信息

Hospital General Universitario de Alicante, España.

出版信息

Enferm Infecc Microbiol Clin. 2009 Dec;27 Suppl 2:21-6. doi: 10.1016/S0213-005X(09)73215-X.

Abstract

Etravirine (ETR) is the first representative of a new generation of non-nucleoside reverse transcriptase inhibitors (NNRTI) and is indicated in patients with HIV infection and virological failure. The recommended dose is 200 mg (two tablets) every 12 hours after a meal. ETR has good tolerability and the tablets can be dissolved in water, which can aid swallowing in some patients. This drug has a plasma half-life of 30-40 hours and consequently is a candidate for once-daily regimens. The most frequent adverse effect is rash (affecting 19% of patients), which is usually mild (grades 1 or 2) and does not lead to drug withdrawal. The DUET 1 and 2 studies, which compared ETR versus placebo, with both groups receiving boosted darunavir and an optimized background regimen, did not demonstrate a higher incidence of liver toxicity, neuropsychiatric symptoms, gastrointestinal disturbances or atherogenic dyslipidemia in patients receiving ETR. The safety profile of ETR suggests that it could be used as a substitute drug in patients with toxicity induced by first-generation NNRTIs or other antiretroviral drugs.

摘要

依曲韦林(ETR)是新一代非核苷类逆转录酶抑制剂(NNRTI)的首个代表药物,适用于感染人类免疫缺陷病毒(HIV)且出现病毒学治疗失败的患者。推荐剂量为餐后每12小时服用200毫克(两片)。依曲韦林耐受性良好,其片剂可溶于水,有助于某些患者吞咽。该药物的血浆半衰期为30 - 40小时,因此是每日一次给药方案的候选药物。最常见的不良反应是皮疹(19%的患者出现),通常为轻度(1级或2级),不会导致停药。DUET 1和2研究比较了依曲韦林与安慰剂,两组均接受增强型达芦那韦和优化的背景治疗方案,结果显示接受依曲韦林治疗的患者在肝毒性、神经精神症状、胃肠道紊乱或致动脉粥样硬化血脂异常方面的发生率并未更高。依曲韦林的安全性表明,它可作为第一代非核苷类逆转录酶抑制剂或其他抗逆转录病毒药物所致毒性患者的替代药物。

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