Moyle G J
Chelsea and Westminster Hospital, 369 Fulham Rd, London, SW10 9NH, UK.
Expert Opin Investig Drugs. 1999 Apr;8(4):473-86. doi: 10.1517/13543784.8.4.473.
Efavirenz (DMP-266, Sustiva, Stocrin) is a member of the non-nucleoside class of HIV-1 reverse transcriptase inhibitors. It has demonstrated potent antiretroviral activity in treatment-naïve patients in combination with two nucleoside analogues or with a protease inhibitor. In nucleoside analogue-experienced patients, best activity has been seen with two nucleosides plus a protease inhibitor. An open-label comparison versus indinavir plus two nucleoside analogues in predominantly treatment-naïve patients, demonstrated that the efavirenz-based triple therapy provides at least similar antiviral effects, and possibly stronger effects, over 48 weeks. Furthermore, fewer patients discontinued efavirenz-based triple therapy than indinavir-based therapy because of adverse events. Side-effects associated with efavirenz include a maculopapular rash and central nervous system (CNS) disturbances (dizziness, vivid dreams, poor concentration, sleep disturbances) which generally occur, and resolve, within the first weeks of therapy. Efavirenz will be used as a combination agent with other antiretrovirals where therapy for HIV infection is indicated.
依非韦伦(DMP - 266,施多宁,Stocrin)是HIV - 1逆转录酶抑制剂非核苷类药物中的一员。在初治患者中,它与两种核苷类似物或一种蛋白酶抑制剂联合使用时,已显示出强大的抗逆转录病毒活性。在有核苷类似物治疗史的患者中,使用两种核苷加上一种蛋白酶抑制剂时疗效最佳。在主要为初治患者中进行的一项与茚地那韦加两种核苷类似物的开放标签对照试验表明,基于依非韦伦的三联疗法在48周内至少能提供相似的抗病毒效果,甚至可能效果更强。此外,因不良事件而停用基于依非韦伦的三联疗法的患者比停用基于茚地那韦疗法的患者更少。与依非韦伦相关的副作用包括斑丘疹和中枢神经系统(CNS)紊乱(头晕、生动梦境、注意力不集中、睡眠障碍),这些副作用通常在治疗的头几周出现并消退。在有指征进行HIV感染治疗时,依非韦伦将与其他抗逆转录病毒药物联合使用。