Ribera Esteban, Tuset Montse, Martín Maite, del Cacho Elena
Servicio de Enfermedades Infecciosas, Hospital Universitari Vall d'Hebron, Barcelona, España.
Enferm Infecc Microbiol Clin. 2011 May;29(5):362-91. doi: 10.1016/j.eimc.2011.02.004. Epub 2011 Apr 30.
As of November 2010, a total of 22 antiretroviral agents are marketed in Spain. These agents are divided into 6 classes according to their mechanism of action: 1) nucleos(t)ide reverse transcriptase inhibitors (NRTI) (abacavir, didanosine, emtricitabine, stavudine, lamivudine, zidovudine, and tenofovir), 2) non-nucleoside reverse transcriptase inhibitors (NNRTI) (efavirenz, etravirine, and nevirapine), 3) protease inhibitors (PI) (atazanavir, darunavir, fosamprenavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, tipranavir), 4) entry inhibitors (enfuvirtide), 5) coreceptor CCR5 inhibitors (maraviroc), and 6) integrase inhibitors (raltegravir). All 22 agents are indicated for the treatment of HIV-1 infection in combination with other antiretroviral drugs. Most have also proven to be active against HIV-2 (except the NNRTIs, enfuvirtide, and maraviroc) and some are active against hepatitis B virus (lamivudine, emtricitabine, and tenofovir). The present article reviews the main characteristics of the different antiretroviral agents and classes, namely, commercial presentations, paediatric and adult dosages, dose adjustments in renal and hepatic insufficiency, pharmacokinetics and interactions, mechanism of action, treatment indications, resistance, adverse effects, and safety during pregnancy and breastfeeding. Some of the characteristics of antiretrovirals are class-specific and common to other agents of the same class, and others are individual and different from those of other drugs in the same class. Knowledge of these characteristics enables us to prepare efficacious therapeutic regimens according to the specific requirements of the patient (tolerability, simplicity, adaptability to lifestyle) and clinical setting (naive, simplification, rescue, resistance).
截至2010年11月，西班牙共有22种抗逆转录病毒药物上市。这些药物根据其作用机制分为6类：1）核苷（酸）类逆转录酶抑制剂（NRTI）（阿巴卡韦、去羟肌苷、恩曲他滨、司他夫定、拉米夫定、齐多夫定和替诺福韦），2）非核苷类逆转录酶抑制剂（NNRTI）（依非韦伦、依曲韦林和奈韦拉平），3）蛋白酶抑制剂（PI）（阿扎那韦、达芦那韦、福沙那韦、茚地那韦、洛匹那韦、奈非那韦、利托那韦、沙奎那韦、替拉那韦），4）进入抑制剂（恩夫韦肽），5）辅助受体CCR5抑制剂（马拉维罗），6）整合酶抑制剂（雷特格韦）。所有这22种药物均被指定与其他抗逆转录病毒药物联合用于治疗HIV-1感染。大多数药物也已证明对HIV-2有活性（NNRTI、恩夫韦肽和马拉维罗除外），有些药物对乙型肝炎病毒有活性（拉米夫定、恩曲他滨和替诺福韦）。本文综述了不同抗逆转录病毒药物及其类别（即商品剂型、儿童和成人剂量、肾功能和肝功能不全时的剂量调整、药代动力学和相互作用、作用机制、治疗适应证、耐药性、不良反应以及妊娠和哺乳期安全性）的主要特点。抗逆转录病毒药物的一些特点是类别特异性的，与同一类别的其他药物相同，而其他特点则是个体性的，与同一类别的其他药物不同。了解这些特点使我们能够根据患者的具体需求（耐受性、简便性、对生活方式的适应性）和临床情况（初治、简化治疗、挽救治疗、耐药）制定有效的治疗方案。
