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.
McKenney
James M
JM
National Clinical Research, Inc., and School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia, USA. jmckenney@ncrinc.net
D008076:Cholesterol, HDL / Q000097:blood / Q000187:drug effects; D004347:Drug Interactions; D005464:Fluorobenzenes / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D011743:Pyrimidines; D000068718:Rosuvastatin Calcium; D013329:Structure-Activity Relationship; D013449:Sulfonamides
D008076:Cholesterol, HDL; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011743:Pyrimidines; D013449:Sulfonamides; D000068718:Rosuvastatin Calcium