Lipistad Mechanism of Action

Pharmacology: Pharmacodynamics: Atorvastatin as well as some of its metabolites are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. Drug dosage rather than systemic drug concentration correlates better with LDL-C reduction. Individualization of drug dosage should be based on therapeutic response.
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 metabolised by the cytochrome P450 isoenzyme CYP3A4 to a number of active metabolites. It is 98% bound to plasma proteins. The mean plasma elimination half-life of atorvastatin is about 14 hours although the half-life of inhibitory activity for HMG-CoA reductase is about 20 to 30 hours due to the contribution of the active metabolites. Atorvastatin is excreted as metabolites, primarily in the bile.