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Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Pleiotropic actions of fenofibrate on the heart
Pitchai Balakumar1, Ankur Rohilla, Nanjaian Mahadevan
1Department of Pharmacology, Institute of Pharmacy, Rajendra Institute of Technology and Sciences, Sirsa-125055, India. pbala2006@gmail.com
Insights
Fenofibrate, a lipid-lowering drug, offers direct heart protection beyond managing dyslipidemia. It demonstrates cardioprotective effects against various cardiac disorders by activating PPAR-α.
Area of Science:
- Cardiology
- Pharmacology
- Molecular Biology
Background:
- Dyslipidemia involves abnormal levels of cholesterol and triglycerides, increasing atherosclerosis risk.
- Fenofibrate is a fibric acid derivative used to manage dyslipidemia by altering lipid profiles.
- Peroxisome proliferator-activated receptor-alpha (PPAR-α) activation is the primary mechanism for fenofibrate's lipid-lowering effects.
Purpose of the Study:
- To review the recently identified pleiotropic, or multifaceted, effects of fenofibrate on the heart.
- To delineate the novel cardioprotective actions of fenofibrate against diverse cardiac disorders.
Main Methods:
- Literature review of recent studies on fenofibrate's cardiac effects.
- Critical discussion of identified pleiotropic actions and cardioprotective mechanisms.
- Analysis of fenofibrate's impact on various cardiac conditions.
Main Results:
- Fenofibrate not only lowers lipids (LDL, VLDL, triglycerides) and increases HDL but also provides direct myocardial protection.
- Fenofibrate exhibits potential in preventing hypertensive heart damage, cardiac hypertrophy, heart failure, myocarditis, and lipotoxic cardiomyopathy.
- The drug also shows promise in addressing vascular endothelial dysfunction-associated cardiovascular abnormalities.
Conclusions:
- Fenofibrate possesses significant pleiotropic effects on the heart, extending beyond its lipid-modulating capabilities.
- These novel cardioprotective effects highlight fenofibrate's potential therapeutic value in managing a range of cardiac disorders.
Abstract:
Fenofibrate is a third-generation fibric acid derivative employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. Dyslipidemia is a condition associated with elevated levels of low-density lipoproteins (LDL), very low-density lipoproteins (VLDL) and triglycerides, and reduced levels of high-density lipoproteins (HDL) in the circulation. Fenofibrate has an ability to diminish LDL, VLDL and triglycerides and pertinently augment HDL, and thus it is used to manage dyslipidemia. The lipid lowering effects of fenofibrate are classically mediated via an activation of peroxisome proliferator-activated receptor-alpha (PPAR-α). Recent studies demonstrated numerous pleiotropic effects of fenofibrate on the heart that afford direct myocardial protection besides its lipid lowering effects. Fenofibrate has an additional potential to prevent the induction and progression of hypertensive heart damage, cardiac hypertrophy, heart failure, myocarditis, lipotoxic cardiomyopathy and vascular endothelial dysfunction-associated cardiovascular abnormalities. In this review, we critically discussed recently identified pleiotropic actions of fenofibrate on the heart. Moreover, the novel cardioprotective effects of fenofibrate against various cardiac disorders have been delineated.
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