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洛匹那韦利托那韦:在治疗人类免疫缺陷病毒 1 型感染中的应用评价。

Lopinavir/Ritonavir: a review of its use in the management of HIV-1 infection.

机构信息

Adis, Auckland, New Zealand.

出版信息

Drugs. 2010 Oct 1;70(14):1885-915. doi: 10.2165/11204950-000000000-00000.

Abstract

Lopinavir/ritonavir (Kaletra®) is an orally administered coformulated ritonavir-boosted protease inhibitor (PI) comprising lopinavir and low-dose ritonavir. It is indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in adults, adolescents and children. Lopinavir/ritonavir is available as a tablet, soft-gel capsule and an oral solution for patients with difficulty swallowing. In well designed, randomized clinical trials, lopinavir/ritonavir, in combination with other antiretroviral therapies (ART), provided durable virological suppression and improved immunological outcomes in both ART-naive and -experienced adult patients with virological failure. Furthermore, lopinavir/ritonavir demonstrated a high barrier to the development of resistance in ART-naive patients. More limited data indicate that it is effective in reducing plasma HIV-1 RNA levels in paediatric patients. Lopinavir/ritonavir has served as a well established benchmark comparator for the noninferiority of other ritonavir-boosted PI regimens. Although generally well tolerated, lopinavir/ritonavir is associated with generally manageable adverse gastrointestinal side effects and hypertriglyceridaemia and hypercholesterolaemia, which may require coadministration of lipid-lowering agents to reduce the risk of coronary heart disease. Lopinavir/ritonavir, in combination with other ART agents, is a well established and cost-effective treatment for both ART-naive and -experienced patients with HIV-1 infection and, with successful management of adverse events, continues to have a role as an effective component of ART regimens for the control of HIV-1 infection.

摘要

洛匹那韦利托那韦(克力芝®)是一种口服的利托那韦增强的蛋白酶抑制剂(PI)复方制剂,包含洛匹那韦和低剂量利托那韦。它与其他抗逆转录病毒药物联合用于治疗成人、青少年和儿童的 HIV-1 感染。洛匹那韦利托那韦有片剂、软胶囊和口服液供吞咽困难的患者使用。在精心设计的随机临床试验中,洛匹那韦利托那韦与其他抗逆转录病毒疗法(ART)联合使用,为病毒学失败的初治和经验丰富的成年患者提供了持久的病毒学抑制和改善的免疫结果。此外,洛匹那韦利托那韦在初治患者中显示出对耐药性发展的高屏障。更有限的数据表明,它在降低儿科患者的血浆 HIV-1 RNA 水平方面是有效的。洛匹那韦利托那韦一直是其他利托那韦增强的 PI 方案非劣效性的良好基准比较剂。尽管通常耐受良好,但洛匹那韦利托那韦与一般可管理的胃肠道不良副作用以及高甘油三酯血症和高胆固醇血症相关,可能需要联合使用降脂药物来降低冠心病的风险。洛匹那韦利托那韦与其他 ART 药物联合使用,是 HIV-1 感染的初治和经验丰富患者的一种成熟且具有成本效益的治疗方法,通过成功管理不良反应,它继续作为控制 HIV-1 感染的 ART 方案的有效组成部分发挥作用。

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