Mechanisms of Lipid-Lowering Agents

Vol. 78, No. 3, 1991

Free Abstract Article (PDF 3267 KB)

Clinical Pharmacology

Mechanisms of Lipid-Lowering Agents
Cesare R. Sirtori, Cristina Manzoni, Maria R. Lovati

Institute of Pharmacological Sciences, University of Milan, Italy

Address of Corresponding Author

Cardiology 1991;78:226-235 (DOI: 10.1159/000174789)

Key Words

Cholestyramine
Colestipol
Neomycin
Fibric acid derivatives
Nicotinic acid
Probucol
HMG-CoA reductase inhibitors
Dextrothyroxine
-Sitosterol
Metformin
Tiadenol
Panthetine

Abstract

Lipid-lowering agents are used with the purpose of ameliorating hyperlipoproteinemias, in order to prevent arterial disease. Lipid-lowering drugs can be classified into absorbable agents and into nonabsorbable compounds, acting within the gastrointestinal lumen. Absorbable drugs (fibric acids, nicotinic acid, probucol, HMG-CoA reductase inhibitors) reduce plasma very-low-density lipoproteins (VLDL) and/or low-density lipoproteins (LDL) by a variety of mechanisms. Fibric acids, in particular, act by stimulating the catabolism of VLDL and also, as a consequence, improving LDL delipidation, thus favoring receptor uptake. Nicotinic acid and acipimox interfere with the biosynthesis of LDL and can also improve the clearance of VLDL/LDL. Probucol acts by a newly described mechanism, i.e. accelerating reverse transport of cholesteryl esters from high-density lipoproteins to lower-density lipoproteins. Finally, HMG-CoA reductase inhibitors, interfering with the biosynthesis of cholesterol, can induce an increased expression of liver high-affinity lipoprotein receptors. Nonabsorbable agents (anion-exchange resins, neomycin, beta -sitosterol) interrupt the recirculation of bile acids and/or reduce the absorption of cholesterol with the gut. They display a selective activity on hypercholesterolemia, again by increasing LDL receptor expression. The choice of one or more lipid-lowering agents will depend upon the patient's phenotype, determining responsiveness to the pharmacological treatment.

Author Contacts

Prof. Cesare R. Sirtori, Chair of Clinical Pharmacology, Institute of Pharmacological Sciences, Via Balzaretti, 9, I-20133 Milano (Italy)

Article Information

Published online: November 12, 2008
Number of Print Pages : 10

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