Statins (HMG-CoA reductase inhibitors) are the most effective drugs available for lowering LDL cholesterol, with reductions in the range of 30 to 60 percent. They also reduce levels of VLDL and increase levels of HDL. In addition, statins are used in the primary and secondary prevention of coronary heart disease (CHD).

Statins work by inhibiting HMG-CoA reductase, a key enzyme for the synthesis of cholesterol in the liver. After blocking this rate-limiting step, hepatocytes sense sense the reduced levels of intrahepatic cholesterol and attempt to compensate by synthesizing more LDL receptors on their cell surfaces. This causes increased uptake of plasma LDL, and consequently decreases plasma LDL cholesterol concentration.

Side effects include muscle toxicity and hepatic dysfunction resulting in persistent elevations in aminotransferases. Statins carry a rating of category X by the US Food an Drug Administration and are contraindicated in women who are or may become pregnant.

Examples of statins: Atorvastatin (Lipitor), lovastatin (Mevacor), pravastatin (Pravachol), simvastatin (Zocor), and rosuvastin (Crestor).