Pharmacologic characteristics of statins.

Considerable effort has been devoted to improving the pharmacologic characteristics and clinical effects of statins. Desirable pharmacologic properties include potent inhibition of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase, selectivity of uptake in hepatocytes, low systemic bioavailability to reduce systemic adverse effects, prolonged elimination half-life, and no or minimal hepatic metabolism to avoid drug-drug interactions. The desirable effects on lipid variables would include increased effectiveness in reducing levels of low-density lipoprotein cholesterol and other atherogenic lipoproteins and measurable beneficial effects on high-density lipoprotein cholesterol levels. As a product of the ongoing efforts regarding statin pharmacology, the new statin rosuvastatin exhibits significant improvements in several of these characteristics.