Mechanism of Action

As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis. Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, atorvastatin also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.

Indication
 

LIPITOR is anHMG-CoA reductase inhibitorindicatedas an adjunct therapy to diet to:

• Reduce the risk of MI, stroke, revascularization procedures, and angina in adult patients without CHD, but with multiple risk factors.
• Reduce the risk of MI and stroke in adult patients with type 2 diabetes without CHD, but with multiple risk factors .
• Reduce the risk of non-fatal MI, fatal and non-fatal stroke, revascularization procedures, hospitalization for CHF, and angina in adult patients with CHD .
• Reduce elevated total-C, LDL-C, apo B, and TG levels and increase HDLC in adult patients with primary hyperlipidemia (heterozygous familial and nonfamilial) and mixed dyslipidemia .
• Reduce elevated TG inadultpatientswith hypertriglyceridemiaand primary dysbetalipoproteinemia.
• Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH)
• Reduce elevated total-C, LDL-C, and apo B levels in pediatric patients, 10 years to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) after failing an adequate trial of diet therapy