Pharmacokinetics research progress on statins

Abstract

Abstract: Statins are kinds of 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA)reductase inhibitors and are widely used for the treatment of hypercholesterolemia. Their efficacy in preventing cardiovascular events has been confirmed by a large number of clinical trials.However, muscular side effects, sometimes severe, including myopathy or rhabdomyolysis, are dose-dependent and associated with the pharmacokinetic alterations of statins. Based on previous studies, pharmacokinetic alterations of statins can be predicted following coadministration of other drugs or in patients with lowered activities in drug metabolism and or transport.To understand the mechanism of the pharmacokinetic alteration, we need the information about the metabolizing enzyme(s)and transporter(s)involved in the pharmacokinetics of statins.In this review, the pharmacokinetic aspects and physicochemical properties of statins are reviewed in order to understand the mechanism governing their pharmacokinetic alterations.

Key words: statins, 3-Hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, transporter, pharmacogenetics

CLC Number:

R968
R969.1

DENG Jian-wei, GUO Dong, ZHOU Hong-hao. Pharmacokinetics research progress on statins[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2007, 12(8): 850-860.

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