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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.