Atorvastatin takes effect through selectively and competitively inhibiting the hepatic enzyme HMG-CoA reductase, which is responsible for converting HMG-CoA to mevalonate in the cholesterol biosynthesis pathway. This results in a subsequent decrease in hepatic cholesterol levels. Decreased hepatic cholesterol levels stimulates upregulation of hepatic LDL-C receptors which increases hepatic uptake of LDL-C and reduces serum LDL-C concentrations.
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The primary uses of atorvastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease.