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HMG-CoA Reductase Inhibitor.
Pharmacology: Pharmacodynamics: Atorvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor (as statin), is a lipid regulating drug with actions on plasma lipids.
Pharmacokinetics: Atorvastatin is rapidly absorbed from the gastrointestinal tract. It has low absolute bioavailability of about 12% due to presystemic clearance in the gastrointestinal mucosa and/or first-pass metabolism in the liver, its primary site of action. Atorvastatin is metabolized by the cytochrome P450 isoenzyme CYP3A4 to a number of compounds which are also active inhibitors of HMG-CoA reductase. The mean plasma elimination half-life of atorvastatin is about 14 hours although the half-life of inhibitory activity for HMG-CoA reductase is approximately 20 to 30 hours due to the contribution of the active metabolites. It is 98% bound to plasma proteins. Atorvastatin is excreted as metabolites, primarily in the bile.
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