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亲水性还是亲脂性他汀类药物?

Hydrophilic or Lipophilic Statins?

作者信息

Climent Elisenda, Benaiges David, Pedro-Botet Juan

机构信息

Department of Endocrinology and Nutrition, Hospital del Mar, Barcelona, Spain.

Department of Medicine, Universitat Autònoma de Barcelona, Campus Universitari Mar, Barcelona, Spain.

出版信息

Front Cardiovasc Med. 2021 May 20;8:687585. doi: 10.3389/fcvm.2021.687585. eCollection 2021.

DOI:10.3389/fcvm.2021.687585
PMID:34095267
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8172607/
Abstract

Drugs can be classified as hydrophilic or lipophilic depending on their ability to dissolve in water or in lipid-containing media. The predominantly lipophilic statins (simvastatin, fluvastatin, pitavastatin, lovastatin and atorvastatin) can easily enter cells, whereas hydrophilic statins (rosuvastatin and pravastatin) present greater hepatoselectivity. Although the beneficial role of statins in primary and secondary cardiovascular prevention has been unequivocally confirmed, the possible superiority of one statin or other regarding their solubility profile is still not well-established. In this respect, although some previously published observational studies and clinical trials observed a superiority of lipophilic statins in cardiovascular outcomes, these results could also be explained by a greater low-density lipoprotein cholesterol reduction with this statin type. On the other hand, previous studies reported conflicting results as to the possible superiority of one statin type over the other regarding heart failure outcomes. Furthermore, adverse events with statin therapy may also be related to their solubility profile. Thus, the aim of the present review was to collect clinical evidence on possible differences in cardiovascular outcomes among statins when their solubility profile is considered, and how this may also be related to the occurrence of statin-related adverse effects.

摘要

根据药物在水或含脂质介质中的溶解能力,可将其分为亲水性或亲脂性。主要为亲脂性的他汀类药物(辛伐他汀、氟伐他汀、匹伐他汀、洛伐他汀和阿托伐他汀)能够轻易进入细胞,而亲水性他汀类药物(瑞舒伐他汀和普伐他汀)则具有更高的肝选择性。尽管他汀类药物在一级和二级心血管预防中的有益作用已得到明确证实,但一种他汀类药物相对于另一种他汀类药物在溶解性方面可能存在的优势仍未完全确立。在这方面,尽管一些先前发表的观察性研究和临床试验观察到亲脂性他汀类药物在心血管结局方面具有优势,但这些结果也可能是由于该类他汀类药物能更有效地降低低密度脂蛋白胆固醇所致。另一方面,先前的研究报告了关于一种他汀类药物相对于另一种他汀类药物在心力衰竭结局方面可能存在的优势的相互矛盾的结果。此外,他汀类药物治疗的不良事件也可能与其溶解性有关。因此,本综述的目的是收集有关考虑他汀类药物溶解性时心血管结局可能存在差异的临床证据,以及这与他汀类药物相关不良反应的发生可能有何关联。

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J Control Release. 2021 May 10;333:536-559. doi: 10.1016/j.jconrel.2021.03.034. Epub 2021 Mar 29.
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The Risk of Muscular Events Among New Users of Hydrophilic and Lipophilic Statins: an Observational Cohort Study.新型亲水型和亲脂型他汀类药物使用者发生肌肉事件的风险:一项观察性队列研究。
J Gen Intern Med. 2021 Sep;36(9):2639-2647. doi: 10.1007/s11606-021-06651-6. Epub 2021 Mar 9.
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Polymers and Nanoparticles for Statin Delivery: Current Use and Future Perspectives in Cardiovascular Disease.
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Antibodies (Basel). 2025 Jul 23;14(3):63. doi: 10.3390/antib14030063.
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Medicine (Baltimore). 2025 Aug 8;104(32):e43838. doi: 10.1097/MD.0000000000043838.
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