Description
Mechanism of Action
Atorvastatin competitively inhibits HMG-CoA reductase, the enzyme that catalyses the conversion of HMG-CoA to mevalonate. This results in the induction of the LDL receptors and stimulation of LDL catabolism, leading to lowered LDL-cholesterol levels.
Absorption: Readily absorbed from the GI tract. Bioavailability: Approx 12%.
Distribution: Volume of distribution: Approx 381 L. Plasma protein binding: 98%.
Metabolism: Metabolised by CYP3A4 isoenzyme to active ortho- and parahydroxylated derivates and an inactive β-oxidation product.
Excretion: Via faeces (as metabolites); urine (<2% as unchanged drug). Elimination half-life: Approx 14 hr.
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AA05 – atorvastatin; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia
