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依折麦布+辛伐他汀治疗高胆固醇血症的药代动力学药物评价

Pharmacokinetic drug evaluation of ezetimibe + simvastatin for the treatment of hypercholesterolemia.

作者信息

Bove Marilisa, Fogacci Federica, Cicero Arrigo F G

机构信息

a Internal and Surgical Medicine Sciences Department , University of Bologna , Bologna , Italy.

出版信息

Expert Opin Drug Metab Toxicol. 2017 Oct;13(10):1099-1104. doi: 10.1080/17425255.2017.1381085. Epub 2017 Sep 26.

Abstract

Cholesterol lowering treatment is mainly based on statins eventually associated to adjunctive drugs of different class such as ezetimibe. In the present review, we analysed the pharmacokinetics, efficacy and safety of ezetimibe + simvastatin drug association. Areas covered: The bio-equivalence of ezetimibe and simvastatin when co-administrated in separate tablets or combined in a single pill is well documented. Ezetimibe is absorbed in small intestine, reaching peak plasma concentrations in 4-12 h, with a plasma half-life of 22 h. Simvastatin, ingested as a prodrug, is hydrolyzed in liver to its active beta-hydroxyacid metabolite, reaching peak plasma concentrations in 2-4 h, with a plasma half-life of approximately 5 h. The available evidence support the clinical efficacy of this drug combination, both in term of LDL-cholesterol reduction and cardiovascular risk decrease. Expert opinion: The synergistic action of these two drugs and the efficacy and safety extensively demonstrated of their association (in particular in the large IMProved Reduction of Outcomes: Vytorin Efficacy International Trial -IMPROVE-IT-) promote its clinical use, especially in subjects with high cardiovascular risk who need to optimize their LDL-Cholesterolemia, but also in patients who cannot tolerate high-dose of more powerful statins.

摘要

降胆固醇治疗主要基于他汀类药物,最终可能会联合使用不同类型的辅助药物,如依折麦布。在本综述中,我们分析了依折麦布+辛伐他汀联合用药的药代动力学、疗效和安全性。涵盖领域:依折麦布和辛伐他汀分别制成片剂共同给药或制成单片复方制剂时的生物等效性已有充分记录。依折麦布在小肠吸收,4-12小时达到血浆峰浓度,血浆半衰期为22小时。辛伐他汀作为前体药物摄入后,在肝脏水解为其活性β-羟基酸代谢物,2-4小时达到血浆峰浓度,血浆半衰期约为5小时。现有证据支持这种药物组合在降低低密度脂蛋白胆固醇和降低心血管风险方面的临床疗效。专家意见:这两种药物的协同作用以及它们联合使用时广泛证明的疗效和安全性(特别是在大型改善预后:Vytorin疗效国际试验-IMPROVE-IT-中)促进了其临床应用,尤其适用于需要优化低密度脂蛋白血症的高心血管风险患者,也适用于不能耐受高剂量更强效他汀类药物的患者。

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