Drug therapy of hypercholesterolemia.

The rationale for drug treatment of patients with hypercholesterolemia is that sustained reductions in the plasma concentrations of atherogenic lipoproteins will retard the development of atherosclerosis. Drug therapy should be initiated only after the exclusion of secondary factors and after an adequate trial of dietary therapy has failed to lower plasma cholesterol to a satisfactory level. The bile-acid sequestrants (cholestyramine and colestipol), nicotinic acid, and lovastatin are the most effective drugs for use in patients with primary hypercholesterolemia; these agents reduce total and LDL cholesterol concentrations by 15-35%. For patients with high concentrations of LDL cholesterol who concurrently have hypertriglyceridemia, nicotinic acid is the drug of choice, and bile-acid sequestrants are contraindicated. Combined therapy with drugs that have different mechanisms of action can be effectively utilized in the treatment of patients with severe hypercholesterolemia; combinations involving lovastatin, nicotinic acid, and bile-acid sequestrants are the most effective.