Department of Therapy and Medical Diagnostics, Lviv National Medical University, Lviv, Ukraine.
Department of Clinical and Molecular Medicine, Faculty of Medicine and Psychology, University of Rome Sapienza, Sant'Andrea Hospital, Rome, Italy.
Expert Opin Pharmacother. 2020 Apr;21(5):531-539. doi: 10.1080/14656566.2020.1714028. Epub 2020 Feb 8.
: Although statin therapy is a powerful lipid-lowering strategy, only one-fifth of statin users currently reach their lipid goals. In addition, statin treatment alone has relatively low efficacy in reducing other lipid fractions than low-density lipoprotein-cholesterol (LDL-C). In such cases, most guidelines recommend adding the cholesterol absorption inhibitor ezetimibe.: This paper summarizes the main pharmacological characteristics of rosuvastatin and ezetimibe (mechanism of action, metabolism), their lipid-lowering and pleiotropic effects, with particular attention to the clinical effects of the combined drugs in hypercholesterolemia and mixed dyslipidemia patients (such as the ones affected by diabetes mellitus and Acquired Immune Deficiency Syndrome (AIDS)).: The additive effect of rosuvastatin and ezetimibe helps to reach lipid goals in a large number of high-risk patients, while avoiding some safety issues related to high dosages of intensive statin therapy. Patients with diabetes receive additional benefits from ezetimibe as they seem to absorb cholesterol more effectively than non-diabetic ones, because of increased NPC1L1 gene expression. Ezetimibe augments rosuvastatin triglyceride-lowering and anti-inflammatory effects, as well. Taking into account its excellent safety profile and lack of clinically relevant drug-drug interactions, the rosuvastatin/ezetimibe association is a valuable alternative to statin dose uptitration.
: 尽管他汀类药物治疗是一种强大的降脂策略，但目前只有五分之一的他汀类药物使用者达到了他们的血脂目标。此外，他汀类药物单独治疗在降低除低密度脂蛋白胆固醇（LDL-C）以外的其他血脂成分方面的疗效相对较低。在这种情况下，大多数指南建议添加胆固醇吸收抑制剂依折麦布。
: 本文总结了瑞舒伐他汀和依折麦布的主要药理学特性（作用机制、代谢）、降脂和多效作用，特别关注联合药物在高胆固醇血症和混合血脂异常患者（如受糖尿病和艾滋病（AIDS）影响的患者）中的临床效果。
: 瑞舒伐他汀和依折麦布的联合作用有助于使大量高危患者达到血脂目标，同时避免与高强度他汀类药物治疗相关的一些安全问题。由于 NPC1L1 基因表达增加，糖尿病患者对依折麦布的吸收胆固醇能力似乎比非糖尿病患者更强，因此能从中获得额外益处。依折麦布还增强了瑞舒伐他汀降低甘油三酯和抗炎的作用。考虑到其出色的安全性和缺乏临床相关的药物相互作用，瑞舒伐他汀/依折麦布联合治疗是他汀类药物剂量递增的有价值替代方案。
