Nevirapine in the treatment of HIV
Nevirapine in the treatment of HIV
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DOI：
10.1586/14787210.2.3.367
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发表时间：
2004-06
影响因子：
5.7
通讯作者：
A. Milinkovic;E. Martinez
中科院分区：
文献类型：
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作者：
A. Milinkovic;E. Martinez
奈韦拉平（Viramune®，勃林格殷格翰有限公司）是第一个上市的非核苷逆转录酶抑制剂。与任何抗逆转录病毒药物一样，奈韦拉平应始终作为完全抑制方案的一部分使用。临床研究表明，含有奈韦拉平的治疗方案可以在大约一半未接受过抗逆转录病毒治疗的患者中实现持久的病毒学和免疫学反应。它还可以成功地用作挽救疗法的组成部分，以及作为简化含蛋白酶抑制剂治疗方案的策略的一部分。奈韦拉平对未接受过治疗和接受过治疗的患者的血脂状况都有有益的影响。奈韦拉平在预防艾滋病毒母婴传播方面也发挥着重要作用。它通常具有良好的耐受性，皮疹和肝毒性是最常报告的不良事件。奈韦拉平作为底物和诱导剂与细胞色素 P450 酶相互作用。因此，每当奈韦拉平与蛋白酶抑制剂、美沙酮（Methadose®，Rosemont Pharmaceuticals Ltd）、口服避孕药、利福平（Rifadin®，Aventis Pharma）和其他潜在相互作用的药物一起使用时，应建议进行治疗药物监测。奈韦拉平耐药突变是非核苷类逆转录酶抑制剂家族常见的突变，包括 K103N、V106A、Y181C、Y188C 和 G190A。更好地了解奈韦拉平概况肯定有助于确保其临床应用变得更加有效和有益。
Nevirapine (Viramune®, Boehringer Ingelheim Ltd) is the first marketed non-nucleoside reverse transcriptase inhibitor. As with any antiretroviral drug, nevirapine should always be used as part of a fully suppressive regimen. Clinical studies have shown that nevirapine-containing regimens may accomplish durable virological and immunological responses in approximately half of all antiretroviral-naive patients. It can also be successfully used as a component of salvage therapies and as a part of a strategy to simplify protease inhibitor-containing regimens. Nevirapine has a beneficial effect on the lipid profile in both treatment-naive and -experienced patients. Nevirapine also has an important role in preventing mother-to-child transmission of HIV. It is usually well-tolerated with rash and liver toxicity being the most frequently reported adverse events. Nevirapine interacts with cytochrome P450 enzymes both as a substrate and as an inducer. For this reason, therapeutic drug monitoring should be recommended whenever nevirapine is used with protease inhibitors, methadone (Methadose®, Rosemont Pharmaceuticals Ltd), oral contraceptives, rifampicin (Rifadin®, Aventis Pharma) and other potentially interacting drugs. Nevirapine-resistant mutations are common to the non-nucleoside reverse transcriptase inhibitor family and they include K103N, V106A, Y181C, Y188C and G190A. A better understanding of the nevirapine profile will certainly contribute to ensuring that its clinical application becomes more effective and beneficial.