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The primary objective of drug therapy for people with high blood cholesterol is to lower the levels of low-density lipoprotein (LDL) or "bad" cholesterol sufficiently to reduce the risk of coronary artery disease. In general, the LDL cholesterol levels at which cholesterol-lowering medications are considered as an option are as follows:

• People with existing coronary artery disease:

  • if the LDL cholesterol level is 130 mg/dL or higher
  • goal of drug therapy is to lower the LDL cholesterol level to 100 mg/dL or lower

• People without coronary artery disease who have less than two risk factors:

  • if the LDL cholesterol level is 190 mg/dL or higher
  • goal of drug therapy is to lower the LDL cholesterol level to 160 mg/dL or lower

• People without coronary artery disease who have two or more risk factors:

  • if the LDL cholesterol level is 160 mg/dL or higher
  • goal of drug therapy is to lower the LDL cholesterol level to 130 mg/dL or lower

The initial approach to lower LDL cholesterol levels is therapeutic lifestyle changes which include a cholesterol-lowering diet, weight loss, and a regular exercise program. If this approach fails to lower LDL cholesterol levels sufficiently, cholesterol-lowering medications can be considered. A variety of cholesterol-lowering medications are available that include:

• Statins
• Bile acid sequestrants
• Nicotinic acid
• Fibrates
• Ezetimibe
• Postmenopausal hormone therapy

Statins

Statins are medications belonging to a class of drugs known as hydroxymethyl glutaryl coenzyme A reductase inhibitors. Statins are the most commonly prescribed cholesterol-lowering medications. Statins work by blocking a substance that the liver needs to produce cholesterol and they also stimulate the liver to remove excess cholesterol from the bloodstream. In general, statins are the most effective cholesterol-lowering medications and can usually decrease LDL cholesterol levels by 20% to 60%.

Studies have shown that the statins reduce the risk of second heart attack and stroke in patients with proven cardiovascular disease (secondary prevention). The role of statins, however, in the primary prevention of heart attack and stroke in people without proven cardiovascular disease is far less certain and is still under investigation.

Current guidelines of the National Cholesterol Education Program Adult Treatment Panel III recommend the use of statins for primary prevention based on an individual's risk profile and LDL cholesterol levels. For patients with an LDL cholesterol level of less than 160 mg/dL, statin therapy is only recommended for those with diabetes or those with two or more cardiac risk factors and a 10-year risk for a first coronary artery disease event of at least 10%.

A recent meta-analysis of randomized, controlled clinical trials published in the Archives of Internal Medicine (Vol. 166, pp. 2307-2313; Nov. 27, 2006) evaluated the role statin therapy for the primary prevention of cardiovascular diseases in people without proven cardiovascular disease. Based upon the analysis of the data, the authors reached the following conclusions:

• Statin therapy decreases the incidence of major coronary events (i.e., nonfatal heart attack) in people without known cardiovascular disease.