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.
Mechanisms of lipid-lowering agents / C. R. Sirtori, C. Manzoni, M. R. Lovati. - In: CARDIOLOGY. - ISSN 0008-6312. - 78:3(1991), pp. 226-235.
|Titolo:||Mechanisms of lipid-lowering agents|
SIRTORI, CESARE (Primo)
MANZONI, CRISTINA MARIA TERESA (Secondo)
LOVATI, MARIA ROSA (Ultimo)
|Parole Chiave:||β-sitosterol; cholestyramine; colestipol; dextrothyroxine; fibric acid derivatives; HMG-CoA reductase inhibitors; metformin; neomycin; nicotinic acid; panthetine; probucol; tiadenol|
|Settore Scientifico Disciplinare:||Settore BIO/14 - Farmacologia|
|Data di pubblicazione:||1991|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1159/000174789|
|Appare nelle tipologie:||01 - Articolo su periodico|