The capability of pravastatin and lovastatin, HMG-CoA reductase inhibitors likely to be taken chronically for hypercholesterolemia, to cross the blood-brain barrier was investigated in normal male volunteers. Lovastatin, which is lipophilic, was detected in cerebrospinal fluid (CSF) at concentrations that may have a pharmacologic effect. Pravastatin, which is hydrophilic, was not detected in CSF. It is concluded that pravastatin may have less potential for causing CNS-related side effects than lovastatin.
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Article Synopsis
- - Familial hypercholesterolemia is a common condition that can lead to early heart disease and stroke, with statins being the primary treatment, but they might also increase the risk of type 2 diabetes due to effects on β-cells.
- - The study used a mouse insulinoma model to analyze the effects of simvastatin and pravastatin on β-cells in the presence of fatty acids, revealing that simvastatin reduced cholesterol more effectively but was also more cytotoxic and suppressed insulin levels.
- - While simvastatin lowered insulin content significantly, this effect was reversible and not dependent on its main action, indicating that it may impact insulin secretion through mechanisms beyond just blocking HMG-CoA reductase. *
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