抗逆转录病毒药物之间的相互作用和药物用于代谢并发症的治疗过程中遇到的艾滋病毒感染。

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Fichtenbaum CJ, Gerber詹

抗逆转录病毒药物之间的相互作用和药物用于代谢并发症的治疗过程中遇到的艾滋病毒感染。

Pharmacokinet。2002; 41 (14): 1195 - 211。doi: 10.2165 / 00003088-200241140-00004。

PubMed ID

12405866 (在PubMed

]

文摘

抗逆转录病毒疗法治疗艾滋病病毒感染的有效结合导致了重大改进总体生存,免疫功能和机会性感染的发生率。然而,艾滋病毒感染和治疗相关的代谢并发症的发展,包括hyperlipidaemia,糖尿病,高血压,脂肪代谢障碍和骨量减少。安全药理治疗这些并发症需要了解药物之间的相互作用中使用抗逆转录病毒药物和药物代谢并发症的治疗。自正式这些交互作用的研究尚未执行,预测必须基于我们对这些药物的代谢的理解。所有艾滋病毒蛋白酶抑制剂的新陈代谢和抑制细胞色素P450 (CYP) 3 a4。例如最CYP3A4的有效抑制剂。例如和奈非那韦也引发一系列CYP亚型以及一些接合酶。非核苷逆转录酶抑制剂delavirdine强有力地抑制CYP3A4,而奈韦拉平和依法韦伦是CYP3A4的诱导物。药物相互作用的研究已经进行了HIV蛋白酶抑制剂和β-还原酶抑制剂。共同的例如加上saquinavir HIV-seronegative志愿者导致接触辛伐他汀酸增加了3059%。 Atorvastatin exposure increased by 347%, but exposure to active atorvastatin increased by only 79%. Conversely, pravastatin exposure decreased by 50%. Similar results have been obtained with combinations of simvastatin and atorvastatin with other HIV protease inhibitors. Thus, the lactone prodrugs simvastatin and lovastatin should not be used with HIV protease inhibitors. Atorvastatin may be used with caution. Although there are no formal studies available, calcium channel antagonists and repaglinide may have significant interactions and toxicity when used with HIV protease inhibitors because of their metabolism by CYP3A4. Sulfonylurea drugs utilise mainly CYP2C9 for metabolism, and this isoenzyme may be induced by ritonavir and nelfinavir with a resulting decrease in efficacy of the sulfonylurea. Losartan may have increased effect when coadministered with ritonavir and nelfinavir because of the induction of CYP2C9 and the expected increase in formation of the active metabolite, E-3174. Overall, well-designed drug-drug interaction studies at steady state are needed to determine whether antiretroviral drugs may be safely coadministered with many of the drugs used in the treatment of the metabolic complications of HIV infection.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Delavirdine	细胞色素P450 3 a4	蛋白质	人类	未知的	底物 抑制剂	细节
奈韦拉平	细胞色素P450 3 a4	蛋白质	人类	未知的	底物 诱导物	细节