Effects of established hypolipidemic drugs on HDL concentration, subclass distribution, and function
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Published on: November 10, 2017
Monica Gomaraschi1, Maria Pia Adorni, Maciej Banach
1Center E. Grossi Paoletti, Department of Pharmacological and Biomolecular Sciences, University of Milano, Via Balzaretti 9, 20133, Milan, Italy, monica.gomaraschi@unimi.it.
Insights
Increasing high-density lipoprotein cholesterol (HDL-C) may protect against cardiovascular disease. This review examines how statins, fibrates, and niacin affect HDL-C levels and function.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
- Lipid Metabolism
Background:
- An inverse relationship exists between high-density lipoprotein cholesterol (HDL-C) and cardiovascular disease (CVD) risk.
- Increasing HDL-C is hypothesized to be protective against cardiovascular events.
- Current lipid-lowering therapies have limited, non-specific effects on HDL-C.
Purpose of the Study:
- To review the impact of established hypolipidemic drugs on HDL-C.
- To examine effects on HDL subclass distribution and function.
- To assess HDL functions like cholesterol efflux, endothelial protection, and antioxidant properties.
Main Methods:
- Review of established hypolipidemic drugs: statins, fibrates, and niacin.
- Analysis of their effects on plasma HDL-C concentrations.
- Evaluation of impacts on HDL subclass distribution and functional assays.
Main Results:
- Statins yield modest HDL-C increases (2-10%).
- Fibrates offer moderate HDL-C elevation (5-15%).
- Niacin is most potent (up to 30%) but has side effects.
Conclusions:
- Established hypolipidemic drugs have varying effects on HDL-C levels.
- Further research is needed to understand their impact on HDL function.
- Optimizing HDL-C and function remains a target for CVD prevention.
Abstract:
The knowledge of an inverse relationship between plasma high-density lipoprotein cholesterol (HDL-C) concentrations and rates of cardiovascular disease has led to the concept that increasing plasma HDL-C levels would be protective against cardiovascular events. Therapeutic interventions presently available to correct the plasma lipid profile have not been designed to specifically act on HDL, but have modest to moderate effects on plasma HDL-C concentrations. Statins, the first-line lipid-lowering drug therapy in primary and secondary cardiovascular prevention, have quite modest effects on plasma HDL-C concentrations (2-10%). Fibrates, primarily used to reduce plasma triglyceride levels, also moderately increase HDL-C levels (5-15%). Niacin is the most potent available drug in increasing HDL-C levels (up to 30%), but its use is limited by side effects, especially flushing.The present chapter reviews the effects of established hypolipidemic drugs (statins, fibrates, and niacin) on plasma HDL-C levels and HDL subclass distribution, and on HDL functions, including cholesterol efflux capacity, endothelial protection, and antioxidant properties.
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