Document Detail

Pharmacology of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors (statins), including rosuvastatin and pitavastatin.
MedLine Citation:
PMID:  12162466     Owner:  NLM     Status:  MEDLINE    
Coronary heart disease (CHD) is the leading cause of morbidity and mortality in the Western world, with hypercholesterolemia as the major risk factor. The 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors represent the most efficient drugsfor the treatment of hypercholesterolemia. They lower plasma cholesterol due to the inhibition of endogenous cholesterol synthesis in the liverand subsequent increased expression of low-density lipoprotein (LDL) receptors, resulting in an up-regulated catabolic rate for plasma LDL. The beneficial effect of statins on the incidence of CHD was clearly demonstrated in several large-scale clinical trials. Currently, five statins (atorvastatin, fluvastatin, lovastatin, pravastatin, and simvastatin) are available, and two novel compounds (pitavastatin, rosuvastatin) are undergoing clinical investigation. To point out potential mechanisms leading to increased toxicity and to compare the novel statins with the established ones, this article summarizes their pharmacological data since the prevalence of adverse events can be explained at least in part by their pharmacokinetic differences.
Michael Igel; Thomas Sudhop; Klaus von Bergmann
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review    
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  42     ISSN:  0091-2700     ISO Abbreviation:  J Clin Pharmacol     Publication Date:  2002 Aug 
Date Detail:
Created Date:  2002-08-06     Completed Date:  2003-02-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  835-45     Citation Subset:  IM    
Department of Clinical Pharmacology, University of Bonn, Germany.
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MeSH Terms
Acyl Coenzyme A / antagonists & inhibitors*,  metabolism
Antilipemic Agents / adverse effects,  pharmacokinetics,  pharmacology,  therapeutic use
Coronary Disease / drug therapy
Enzyme Inhibitors / adverse effects,  pharmacokinetics,  pharmacology*,  therapeutic use
Fluorobenzenes / adverse effects,  pharmacokinetics,  pharmacology*,  therapeutic use
Quinolines / adverse effects,  pharmacokinetics,  pharmacology*,  therapeutic use
Reg. No./Substance:
0/Acyl Coenzyme A; 0/Antilipemic Agents; 0/Enzyme Inhibitors; 0/Fluorobenzenes; 0/Pyrimidines; 0/Quinolines; 0/Sulfonamides; 147526-32-7/NK 104; 1553-55-5/3-hydroxy-3-methylglutaryl-coenzyme A; 287714-41-4/rosuvastatin
Erratum In:
J Clin Pharmacol. 2003 Sep;43(9):1015

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