[Pharmacokinetics of statins].
Statins are lipid lowering agents that promote their effects on plasma lipids through the inhibition of HMG-CoA reductase, a crucial enzyme in the cascade of cholesterol synthesis, leading to reduction of tissue cholesterol pool and consequently, to an upregulation of the LDL receptor expression. There are considerable differences among statins regarding some pharmacokinetic properties, such as the coefficient of hydrophilicity, via liver metabolism (especially regarding P450 cytochrome and isoenzymes), plasma half-life and efficacy of serum lipid changes. They may also differ regarding interactions with other drugs that share the same pathway of metabolism. Recently, many pleiotropic effects have been reported with these drugs, such as anti-inflammatory properties, improvement in endothelial function and benefits on hemostasis.
Fonseca
Francisco Antonio Helfenstein
FA
Setor de Lípides, Aterosclerose e Biologia Vascular, UNIFESP-EPM.
D001189:Aryl Hydrocarbon Hydroxylases / Q000378:metabolism; D056486:Chemical and Drug Induced Liver Injury; D008078:Cholesterol, LDL / Q000378:metabolism; D004347:Drug Interactions; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics*; D009135:Muscular Diseases / Q000139:chemically induced; D012206:Rhabdomyolysis / Q000139:chemically induced
D008078:Cholesterol, LDL; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D001189:Aryl Hydrocarbon Hydroxylases; C422408:CYP3A43 protein, human