Research Progress of Pharmacokinetic Interactions between Lopinavir/Ritonavir and Statins

F. Bu, J. Chen, N. Ding, Z. Jiao, X. Xiang
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Abstract

OBJECTIVE: To provide references for the selection of an appropriate statin and its dose adjustment in clinical practice when combined lopinavir/ritonavir (LPV/r) and statins. METHODS: Pharmacokinetic interactions between LPV/r and seven commonly used statins were reviewed by searching relevant domestic and foreign literatures. RESULTS AND CONCLUSIONS: Ritonavir is a potent time dependent inhibitor of cytochrome P450 3A4 (CYP3A4) and will greatly increase the plasma exposure of simvastatin and lovastatin, leading to the increasing risk of liver damage and rhabdomyolysis. Therefore, it is forbidden to use LPV/r together with these two statins. Whereas atorvastatin and rosuvastatin need to be used with caution and started at the lowest dose. No clinical data has been reported to support the relationship and extent of fluvastatin and LPV/r interactions, nor is there a dose recommendation for the combination. Moreover, LPV/r almost have no effect on the pharmacokinetic profiles of pravastatin and pitavastatin, so it is recommended to use pravastatin/pitavastatin with LPV/r in clinical practice.
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洛匹那韦/利托那韦与他汀类药物相互作用的研究进展
目的:为临床应用洛匹那韦/利托那韦(LPV/r)联合他汀类药物时选择合适的他汀类药物及剂量调整提供参考。方法:检索国内外相关文献,回顾LPV/r与7种常用他汀类药物的药动学相互作用。结果与结论:利托那韦是一种有效的时间依赖性细胞色素P450 3A4 (CYP3A4)抑制剂,会大大增加辛伐他汀和洛伐他汀的血浆暴露,导致肝损伤和横纹肌溶解的风险增加。因此,禁止LPV/r与这两种他汀类药物同时使用。而阿托伐他汀和瑞舒伐他汀需要谨慎使用,并以最低剂量开始。没有临床数据报道支持氟伐他汀和LPV/r相互作用的关系和程度,也没有联合使用的剂量推荐。此外,LPV/r对普伐他汀和匹伐他汀的药代动力学特征几乎没有影响,因此在临床实践中推荐使用LPV/r的普伐他汀/匹伐他汀。
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