3-Hydroxy-3-methylglutaryl--coenzyme A reductase inhibitors in the treatment of hypercholesterolemia.

Abstract

A new class of drugs, which inhibit de novo cholesterol biosynthesis, significantly reduces the blood cholesterol concentrations in hypercholesterolemic patients. Four separate inhibitors have lowered plasma total cholesterol and low-density lipoprotein (LDL) levels in humans by 20% to 40%: mevastatin (Compactin), lovastatin (mevinolin), pravastatin (CS-514, Eptastatin, and SQ 31000), and simvastatin (Synvinolin, MK-733). In addition to lowering total and LDL cholesterol concentrations, the plasma concentration of the potentially atherogenic B apolipoprotein is also reduced by 20% to 40%. The reduction in the levels of circulating atherogenic lipoprotein particles occurs as a result of decreased synthesis and enhanced removal of LDLs by the LDL receptor pathway in hepatocytes. Moreover, the levels of high-density lipoprotein cholesterol, which are inversely related to atherosclerosis, increase in concentration with treatment by these drugs. If the short-term safety of these drugs extends to ongoing long-term studies and if cardiovascular morbidity and mortality are affected by their use, this class of hypolipidemic agent will markedly facilitate the effective treatment of hypercholesterolemia.

• Authors: J M Hoeg, H B Brewer Jr
• Journal: JAMA (JAMA) Vol. 258 Issue 24 Pg. 3532-6 (Dec 25 1987) ISSN: 0098-7484 [Print] United States
• PMID: 3316727 (Publication Type: Journal Article, Review)

Chemical References

• Anticholesteremic Agents
• Cholesterol, LDL
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Lovastatin

Topics

• Adult
• Animals
• Anticholesteremic Agents (adverse effects, therapeutic use)
• Child
• Cholesterol, LDL (blood)
• Humans
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Hypercholesterolemia (drug therapy)
• Lovastatin (therapeutic use)