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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.
Highlights
Specialty section: This article was submitted to Lipids in Cardiovascular Disease, a section of the journal Frontiers in Cardiovascular Medicine
As in the Cholesterol Treatment Trialists’ (CTT) meta-analysis [4], this could probably be explained by the fact that the low-density lipoprotein (LDL) cholesterol reduction was greater in the atorvastatin than the pravastatin groups (p < 0.001), and the solubility profile of each statin and the possible superiority of lipophilic statins could play a secondary role in the observed differences
Conflicting results have been observed on the superiority of hydrophilic or lipophilic statins regarding cardiovascular outcomes, including heart failure (HF) and CHD, both from primary and secondary prevention
Summary
Sulphation Hydrophilic [12, 13]. we will analyse its impact in two different clinical settings: the prevention of HF and the treatment of established HF. To the results from observational studies, the greater LDL cholesterol reduction with lipophilic atorvastatin compared to hydrophilic pravastatin could probably account for the more favourable cardiovascular results observed in subjects receiving the former, whether the solubility profile of each statin could play a role in these observed differences could be speculated. As in the CTT meta-analysis [4], this could probably be explained by the fact that the LDL cholesterol reduction was greater in the atorvastatin than the pravastatin groups (p < 0.001), and the solubility profile of each statin and the possible superiority of lipophilic statins could play a secondary role in the observed differences. Deedwania et al [54] evaluated 893 outpatients with chronic stable ischaemic heart disease
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