临床药物动力学和总结atazanavir的疗效和耐受性。
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Le Tiec C, Barrail Goujard C, Taburet
临床药物动力学和总结atazanavir的疗效和耐受性。
Pharmacokinet。2005; 44 (10): 1035 - 50。
- PubMed ID
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16176117 (在PubMed]
- 文摘
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HIV - 1蛋白酶抑制剂(pi)的疗效作为高活性抗逆转录病毒疗法的一部分,现在正在建立和许多艾滋病毒感染患者提供了好处。Atazanavir是一个新的azapeptideπ化合物,最近在美国和欧洲批准。Atazanavir建议结合其他抗逆转录病毒药物治疗的hiv - 1感染。Atazanavir迅速吸收和管理的单一剂量的Atazanavir便餐导致血浆浓度时间曲线下的面积增加了70% (AUC);因此应采取atazanavir与食物。Atazanavir 86%绑定独立人类血清蛋白的浓度。在体液浓度低于血浆浓度。像其他π,atazanavir广泛代谢由肝细胞色素P450 (CYP) 3个同功酶。意味着终端消除半衰期在健康的志愿者是大约7个小时后在稳态atazanavir管理局400毫克每日便餐。coadministered atazanavir 300毫克时,例如100毫克每日一次给药方案,atazanavir AUC从0到24小时和最小血浆浓度增加3 - 4倍,大约10倍,分别与单独atazanavir 300毫克。 Therefore, ritonavir boosted atazanavir regimen (ritonavir 100 mg and atazanavir 300 mg once daily) is increasingly favoured in some patients. Efavirenz, a potent CYP3A inducer, decreased atazanavir concentrations by 75% and, unexpectedly, tenofovir, a nucleotide reverse transcriptase inhibitor, decreased atazanavir concentrations by 25%. Average predose concentrations in HIV-infected patients who received atazanavir 400mg once daily were 273 ng/mL, which was believed to be several-fold higher than protein-binding corrected 50% inhibitory concentration of wild-type viruses. In HIV-infected patients who received once-daily ritonavir (100mg) boosted atazanavir (300 mg), mean (+/-SD) trough concentration was 862 (+/-838) ng/mL. Several clinical trials showed the efficacy of atazanavir 400 mg once daily with a nucleoside analogue backbone in antiretroviral-naive patients. The atazanavir 300/ritonavir 100 mg once-daily combination coadministered with other antiretrovirals showed the efficacy of this strategy in patients receiving efavirenz or in moderately antiretroviral-experienced HIV-infected patients. Recommended once-daily doses of atazanavir taken with food are either 400 mg or 300 mg in combination with low dose ritonavir (100 mg) in moderately antiretroviral-experienced patients. Major advantages of atazanavir to date are its simplicity of administration (once-daily administration) and its less undesirable effect on the lipid profiles in patients.
DrugBank数据引用了这篇文章
- 药物
- 药物靶点
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药物 目标 类 生物 药理作用 行动 Atazanavir 人类免疫缺陷病毒1型蛋白酶 蛋白质 人类免疫缺陷病毒1 是的抑制剂细节 - 药物酶
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药物 酶 类 生物 药理作用 行动 Atazanavir 细胞色素P450 3 a4 蛋白质 人类 未知的底物抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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药物 交互 整合药物之间
在您的软件的交互Atazanavir 依法韦伦 时可以降低血清浓度Atazanavir结合依法韦伦。
