Adkins J C, Noble S
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Dec;56(6):1055-64; discussion 1065-6. doi: 10.2165/00003495-199856060-00014.
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) which shows good inhibitory activity against HIV-1. Reduced susceptibility to efavirenz has been reported with HIV-1 variants containing single and multiple mutations to the reverse transcriptase enzyme. In vitro and in vivo data suggest that the resistance profile of efavirenz overlaps with that of the NNRTIs nevirapine and delavirdine. Clinically significant drug interactions have been reported with efavirenz and indinavir and saquinavir. An increase in dosage of indinavir from 800 to 1000 mg 3 times daily is recommended during coadministration with efavirenz. Use of efavirenz in combination with saquinavir as the sole protease inhibitor is not recommended. Once-daily efavirenz in combination with zidovudine plus lamivudine or indinavir or nelfinavir increased CD4+ cell counts and reduced HIV RNA plasma levels to below quantifiable levels (< 400 copies/ml) in HIV-infected patients. A sustained reduction in viral load was maintained for at least 72 weeks in 1 study. Nervous system symptoms (including headache, dizziness, insomnia and fatigue) and dermatological effects (including maculopapular rash) appear to be the most common adverse events reported with efavirenz-containing antiretroviral regimens.
依非韦伦是一种非核苷类逆转录酶抑制剂（NNRTI），对HIV-1显示出良好的抑制活性。据报道，含有逆转录酶单突变和多突变的HIV-1变体对依非韦伦的敏感性降低。体外和体内数据表明，依非韦伦的耐药谱与NNRTIs奈韦拉平和地拉韦定的耐药谱重叠。已报道依非韦伦与茚地那韦和沙奎那韦存在具有临床意义的药物相互作用。在与依非韦伦合用时，建议将茚地那韦的剂量从每日3次、每次800毫克增加至1000毫克。不建议将依非韦伦与沙奎那韦联合使用作为唯一的蛋白酶抑制剂。在HIV感染患者中，每日一次的依非韦伦与齐多夫定加拉米夫定或茚地那韦或奈非那韦联合使用可增加CD4+细胞计数，并将HIV RNA血浆水平降低至可检测水平以下（<400拷贝/毫升）。在一项研究中，病毒载量持续下降至少维持了72周。神经系统症状（包括头痛、头晕、失眠和疲劳）和皮肤影响（包括斑丘疹）似乎是含依非韦伦的抗逆转录病毒治疗方案报告的最常见不良事件。
