Prescrire Int. 2012 Nov;21(132):262-5.
In previously untreated HIV-1 infection, one first-line therapeutic option is to combine efavirenz, a non-nucleoside reverse transcriptase inhibitor, with tenofovir and emtricitabine. Rilpivirine, another non-nucleoside reverse transcriptase inhibitor, has been approved in the European Union for the treatment of antiretroviral-naive patients with low viral load. Two double-blind "non-inferiority" trials compared rilpivirine- and efavirenz-based combination therapy in a total of 1368 previously untreated patients. Efficacy was similar with respect to the primary endpoint: 80% of patients had viral load below 50 copies/ml after 48 weeks of treatment. In these trials, combinations containing rilpivirine appeared less effective than those containing efavirenz in patients with high viral load (above 100 000 copies/ml). Overall, the risk of virological failure appeared to be higher with rilpivirine than with efavirenz (20.4% versus 18% after 196 weeks). In addition, the potential for cross-resistance to other non-nucleoside reverse transcriptase inhibitors in case of virological failure appeared to be higher with rilpivirine than with efavirenz. Compared with the known adverse effect profile of efavirenz, rilpivirine was associated with less rash (17% versus 31%) and dizziness (10% versus 29%). The incidence of depression appeared similar with the two drugs. In contrast, serum creatinine elevation was more frequent with rilpivirine (5% versus < 1%). Gallstones and adrenal insufficiency are also likely to be more frequent with rilpivirine. High doses of rilpivirine prolong the QTc interval. Rilpivirine carries a risk of pharmacokinetic interactions with many other drugs, including inducers and inhibitors of cytochrome P450 isoenzyme CYP3A4, drugs that increase gastric pH, and drugs transported by P-glycoprotein. Rilpivirine also carries a high risk of pharmacodynamic interactions, notably with drugs that prolong the QTc interval. In practice, as rilpivirine has no proven therapeutic advantages, when combination therapy containing a nonnucleotide reverse transcriptase inhibitor is chosen for previously untreated patients, it is better to continue to use efavirenz, a better-known drug that creates fewer problems in case of treatment failure.
在既往未接受治疗的HIV-1感染中，一种一线治疗方案是将非核苷类逆转录酶抑制剂依非韦伦与替诺福韦和恩曲他滨联合使用。另一种非核苷类逆转录酶抑制剂利匹韦林已在欧盟获批用于治疗病毒载量低的初治抗逆转录病毒治疗患者。两项双盲“非劣效性”试验在总共1368例既往未接受治疗的患者中比较了基于利匹韦林和依非韦伦的联合治疗。在主要终点方面疗效相似：治疗48周后，80%的患者病毒载量低于50拷贝/ml。在这些试验中，对于病毒载量高（高于100000拷贝/ml）的患者，含利匹韦林的联合治疗似乎比含依非韦伦的联合治疗效果差。总体而言，利匹韦林导致病毒学失败的风险似乎高于依非韦伦（196周后分别为20.4%和18%）。此外，在病毒学失败的情况下，利匹韦林对其他非核苷类逆转录酶抑制剂产生交叉耐药的可能性似乎高于依非韦伦。与依非韦伦已知的不良反应谱相比，利匹韦林引起的皮疹（17%对31%）和头晕（10%对29%）较少。两种药物的抑郁发生率似乎相似。相比之下，利匹韦林导致血清肌酐升高更常见（5%对<1%）。利匹韦林导致胆结石和肾上腺功能不全的情况也可能更常见。高剂量的利匹韦林会延长QTc间期。利匹韦林存在与许多其他药物发生药代动力学相互作用的风险，包括细胞色素P450同工酶CYP3A4的诱导剂和抑制剂、增加胃pH值的药物以及由P-糖蛋白转运的药物。利匹韦林还存在较高的药效学相互作用风险，尤其是与延长QTc间期的药物。在实际应用中，由于利匹韦林没有已证实的治疗优势，当为既往未接受治疗的患者选择含非核苷类逆转录酶抑制剂的联合治疗时，最好继续使用依非韦伦，这是一种更知名的药物，在治疗失败时产生的问题较少。
