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Review
. 2003 Apr;26(4 Suppl 3):III32-8.
doi: 10.1002/clc.4960261507.

Pharmacologic characteristics of statins

James M McKenney  1
Affiliations
Review

Pharmacologic characteristics of statins

James M McKenney. Clin Cardiol. 2003 Apr.

Abstract

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.

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References

    1. Istvan ES, Deisenhofer J: Structural mechanism for statin inhibition of HMG‐CoA reductase. Science 2001; 292: 1160–1164 - PubMed
    1. McTaggart F, Buckett L, Davidson R, Holdgate G, McCormick A, Schneck D, Smith G, Warwick M: Preclinical and clinical pharmacology of rosuvastatin, a new 3‐hydroxy‐3‐methylglutaryl coenzyme A reductase inhibitor. Am J Cardiol 2001; 87 (suppl): 28B–32B - PubMed
    1. Chapman MJ, McTaggart F: Optimizing the pharmacology of statins: Characteristics of rosuvastatin. Atheroscler Suppl 2002; 2: 33–37 - PubMed
    1. Buckett L, Ballard P, Davidson R, Dunkley C, Martin L, Stafford J, McTaggart F: Selectivity of ZD4522 for inhibition of cholesterol synthesis in hepatic versus nonhepatic cells (abstr). Atherosclerosis 2000; 151: 41
    1. Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults : Executive summary of the third report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III). J Am Med Assoc 2001; 285: 2486–2497 - PubMed

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