Moreno Santiago, Hernández Beatriz, Dronda Fernando
Servicio de Enfermedades Infecciosas, Hospital Ramón y Cajal, Madrid, España.
Enferm Infecc Microbiol Clin. 2008 Dec;26 Suppl 17:9-13. doi: 10.1016/S0213-005X(08)76614-X.
The characteristics of atazanavir (convenient doses, good tolerance, and excellent lipid profile) makes it an attractive drug to be included in initial regimes. Clinical trials have been performed on patients with no previous antiretroviral treatment, either atazanavir without boost (400 mg once per day) or atazanavir boosted with ritonavir (400/100 mg). Although atazanavir without boost is effective, there is a tendency for a higher number of failures and a higher development of resistant mutations than in patients who fail with boosted atazanavir. Therefore, it is recommended to use boosted atazanavir in patients that start on treatment. In clinical studies, boosted atazanavir can be used with any nucleoside analogue. No pharmacokinetic or pharmacodynamic interaction problems have been detected with the two nucleoside combinations at fixed doses (tenofovir/FTC, abacavir/3TC). Randomised clinical studies have been carried out that compared atazanavir with other boosted protease inhibitors. In the comparative study with lopinavir/ritonavir administered two times a day, atazanavir/ritonavir once per day demonstrated noninferiority, with a similar efficacy regardless of the patient baseline viral load. The atazanavir/ritonavir virological efficacy did not appear to be affected by the baseline immunological status of the patients, which did influence the lopinavir/ritonavir response. Atazanavir/ritonavir is a useful drug combination in the initial treatment of HIV infected adult patients. Its increased virological and immunological efficacy, together with its ease of administration, good tolerance and excellent lipid profile makes it a PI of choice in these patients.
阿扎那韦的特性(服用剂量方便、耐受性良好且脂质谱优良)使其成为初始治疗方案中颇具吸引力的药物。已对既往未接受过抗逆转录病毒治疗的患者开展了临床试验,分别使用未联用增效剂的阿扎那韦(每日一次,400毫克)或与利托那韦联用的阿扎那韦(400/100毫克)。尽管未联用增效剂的阿扎那韦有效,但与联用增效剂的阿扎那韦治疗失败的患者相比,其治疗失败的发生率更高,耐药突变的发生率也更高。因此,建议在开始治疗的患者中使用联用增效剂的阿扎那韦。在临床研究中,联用增效剂的阿扎那韦可与任何核苷类似物合用。对于两种固定剂量的核苷组合(替诺福韦/恩曲他滨、阿巴卡韦/拉米夫定),未检测到药代动力学或药效学相互作用问题。已开展随机临床研究,将阿扎那韦与其他联用增效剂的蛋白酶抑制剂进行比较。在与每日服用两次的洛匹那韦/利托那韦的对比研究中,每日一次服用的阿扎那韦/利托那韦显示出非劣效性,无论患者基线病毒载量如何,疗效相似。阿扎那韦/利托那韦的病毒学疗效似乎不受患者基线免疫状态的影响,而基线免疫状态确实会影响洛匹那韦/利托那韦的疗效。阿扎那韦/利托那韦是成人HIV感染患者初始治疗中一种有用的药物组合。其病毒学和免疫学疗效的提高,以及给药方便、耐受性良好和脂质谱优良等特点,使其成为这些患者的首选蛋白酶抑制剂。