Hydrophilic or Lipophilic Statins?
Hydrophilic or Lipophilic Statins?
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亲水性或亲脂性他汀类药物？
DOI：
10.3389/fcvm.2021.687585
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发表时间：
2021
影响因子：
3.6
通讯作者：
Pedro-Botet J
中科院分区：
文献类型：
--
作者：
Climent E;Benaiges D;Pedro-Botet J
药物可根据其在水或含脂质介质中的溶解能力分为亲水性或亲脂性。主要是亲脂性他汀类药物（辛伐他汀、氟伐他汀、匹伐他汀、洛伐他汀和阿托伐他汀）可以容易地进入细胞，而亲水性他汀类药物（瑞舒伐他汀和普伐他汀）具有更大的肝选择性。虽然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，但一种他汀类药物或其他药物在溶解度方面的可能优效性仍未得到充分证实。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的优效性，但这些结果也可以通过这种他汀类药物降低低密度脂蛋白胆固醇的作用更大来解释。另一方面，先前的研究报告了关于一种他汀类药物在心力衰竭结局方面可能优于另一种他汀类药物的相互矛盾的结果。此外，他汀类药物治疗的不良事件也可能与其溶解度特征有关。因此，本综述的目的是收集关于他汀类药物在溶解度方面可能存在的心血管结局差异的临床证据，以及这可能与他汀类药物相关不良反应的发生有关。
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.