(3S,5S)-Atorvastatin Sodium Salt (Atorvastatin EP Impurity E) is a selective, competitive HMG-CoA reductase inhibitor. The only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.
atorvastatin exists in four optical forms. the (3r, 5r)-atorvastatin enantiomer displays the greatest activity against hmg-coa reductase. (3s,5s)-atorvastatin is an enantiomer of atorvastatin with little or no inhibitory activity against hmg-coa reductase [1]. atorvastatin is a synthetic hmg-coa reductase inhibitor implicated in lowering plasma cholesterol levels by inhibiting endogenous cholesterol synthesis. atorvastatin also reduces triglyceride levels through an as yet unproven mechanism [2]. in various trials in patients with hypercholesterolaemia, atorvastatin produced greater reductions in total cholesterol, apolipoprotein b, ldl-cholesterol and triglyceride levels. in patients with primary hypercholesterolaemia, atorvastatin in combination with colestipol produced significant reductions in ldl-cholesterol levels and smaller reductions in triglyceride levels than atorvastatin monotherapy [2].
[1] kocarek t a, dahn m s, cai h, et al. regulation of cyp2b6 and cyp3a expression by hydroxymethylglutaryl coenzyme a inhibitors in primary cultured human hepatocytes[j]. drug metabolism and disposition, 2002, 30(12): 1400-1405.
[2] lea a p, mctavish d. atorvastatin[j]. drugs, 1997, 53(5): 828-847.
