HIV Community Program, Christiana Care Health System, Wilmington, DE 19899-1668, USA.
Am J Health Syst Pharm. 2012 May 15;69(10):857-61. doi: 10.2146/ajhp110395.
The pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, dosage and administration, and place in therapy of rilpivirine are reviewed.
Rilpivirine is a human immunodeficiency virus type 1 (HIV-1)-specific nonnucleoside reverse transcriptase inhibitor (NNRTI) indicated for use in combination with other antiretroviral agents in adult patients not previously treated with antiretroviral therapy. Rilpivirine is primarily metabolized by the cytochrome P-450 (CYP)3A isoenzyme system. Therefore, providers should be cautious when administering drugs that are inhibitors or inducers of this pathway. Coadministration with CYP 3A inhibitors may lead to increased concentrations of rilpivirine, thereby increasing the risk of adverse effects. Coadministration with inducers of CYP3A isoenzymes or drugs that increase gastric pH may lead to decreased concentrations of rilpivirine, thus promoting virological failure or resistance to rilpivirine. Two Phase III, randomized, double-blind, double-dummy, active-controlled trials compared rilpivirine with efavirenz in HIV-infected adults not previously treated with an antiretroviral. The investigators concluded that rilpivirine, when combined with two nucleoside or nucleotide reverse transcriptase inhibitors, was noninferior to efavirenz for reaching the endpoint of confirmed virological response (HIV-1 RNA level of <50 copies/mL) in adults with HIV infection not previously treated with antiretroviral therapy. The most commonly reported adverse effects included depression, insomnia, headache, and rash. Rilpivirine is administered as a single 25-mg tablet given once daily in combination with other antiretroviral drugs in order to optimize efficacy and reduce resistance.
Rilpivirine is a viable NNRTI for HIV-infected patients who have not previously received antiretroviral therapy.
综述利匹韦林的药理学、药代动力学、药物相互作用、临床疗效、不良反应、剂量和给药、以及在治疗中的地位。
利匹韦林是一种人类免疫缺陷病毒 1 型（HIV-1）特异性非核苷逆转录酶抑制剂（NNRTI），与其他抗逆转录病毒药物联合用于未接受过抗逆转录病毒治疗的成年患者。利匹韦林主要通过细胞色素 P-450（CYP）3A 同工酶系统代谢。因此，在给予该途径的抑制剂或诱导剂时，提供者应谨慎。与 CYP 3A 抑制剂同时使用可能导致利匹韦林浓度升高，从而增加不良反应的风险。与 CYP3A 同工酶诱导剂或增加胃 pH 值的药物同时使用可能导致利匹韦林浓度降低，从而促进病毒学失败或对利匹韦林产生耐药性。两项 III 期、随机、双盲、双模拟、阳性对照试验比较了利匹韦林与依非韦伦在未接受过抗逆转录病毒治疗的 HIV 感染成人中的疗效。研究人员得出结论，利匹韦林与两种核苷或核苷酸逆转录酶抑制剂联合使用，在未接受过抗逆转录病毒治疗的 HIV 感染成人中，达到确认病毒学应答（HIV-1 RNA 水平<50 拷贝/ml）终点的疗效不劣于依非韦伦。最常报告的不良反应包括抑郁、失眠、头痛和皮疹。利匹韦林作为一种单一的 25mg 片剂，每日一次给药，与其他抗逆转录病毒药物联合使用，以优化疗效并降低耐药性。
利匹韦林是一种可行的 NNRTI，适用于未接受过抗逆转录病毒治疗的 HIV 感染患者。
