HMG-CoA reductase inhibitors

ABSTRACT

Efforts to identify and treat individuals with elevated blood cholesterol levels have increased dramatically in recent years. The bile acid sequestrants (cholestyramine, colestipol) and nicotinic acid have been the mainstays of pharmacologic therapy for patients with phenotype(s) IIA and IIB hyperlipoproteinemia, but produce symptomatic side effects in a high percentage of patients. Clinical trials with a new class of cholesterol-lowering drugs, the HMG-CoA reductase inhibitors, have consistently demonstrated a dose-dependent reduction in total and low-density lipoprotein cholesterol levels of up to 30% and 40%, respectively. Symptomatic side effects requiring withdrawal of treatment have been uncommon, but the incidences of opacification of the ocular lens and hepatoxicity remain to be defined. Lovastatin is the first HMG-CoA reductase inhibitor commercially available in the United States. Its efficacy alone, and in combination with the bile acid sequestrants, is reviewed in this report.