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Pharmacology of 3‐Hydroxy‐3‐Methylglutaryl‐Coenzyme A Reductase Inhibitors (Statins), Including Rosuvastatin and Pitavastatin
Author(s) -
Igel Michael,
Sudhop Thomas,
Bergmann Klaus
Publication year - 2002
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/009127002401102731
Subject(s) - pitavastatin , pravastatin , rosuvastatin , cerivastatin , atorvastatin , lovastatin , pharmacology , medicine , simvastatin , fluvastatin , hmg coa reductase , reductase , statin , cholesterol , hydroxymethylglutaryl coa reductase , chemistry , enzyme , biochemistry
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 drugs for the treatment of hypercholesterolemia. They lower plasma cholesterol due to the inhibition of endogenous cholesterol synthesis in the liver and 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.