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Understanding Cholesterol-Lowering Medications (cont.)

Cholesterol Absorption Inhibitors

Ezetimibe (Zetia) is a commonly prescribed cholesterol absorption inhibitor.

How does ezetimibe work?

Ezetimibe was approved by the US Food and Drug Administration (FDA) in late 2002. Ezetimibe by itself reduces LDL cholesterol by 18%-20% by selectively decreasing cholesterol absorption. It mildly reduces triglycerides. Ezetimibe is most useful in people who cannot take statins or as an additional drug for people who take statins but notice side effects when the statin dose is increased. Adding ezetimibe to a statin increases the cholesterol-lowering effect by a 2- to 3-fold factor.

Who should not use these medications?

Individuals who are allergic to ezetimibe (Zetia) should not take it.

Use: Ezetimibe is taken once daily, with or without food. It is often combined with statins to increase effectiveness.

Drug or food interactions: Bile acid sequestrants bind to ezetimibe and reduce its absorption from the intestine by about 50%. Take ezetimibe at least 2 hours before or 4 hours after bile acid sequestrants. Fenofibrate (Tricor), gemfibrozil (Lopid), and cyclosporine increase the blood levels of ezetimibe.

Side effects: Diarrhea, abdominal pain, back pain, joint pain, and sinusitis are the most commonly reported side effects. Hypersensitivity reactions, including angioedema (swelling of the skin and underlying tissues of the head and neck that can be life-threatening) and skin rash rarely occur. Nausea, pancreatitis, muscle damage (myopathy or rhabdomyolysis) and hepatitis have also been reported.