What is ezetimibe (Zetia)?

Ezetimibe lowers blood cholesterol by blocking the absorption of cholesterol, including dietary cholesterol, from the intestines. It does not affect, however, the absorption of triglycerides or fat-soluble vitamins. Ezetimibe was approved by the FDA in October, 2002.

Ezetimibe can be used alone or together with a statin drug. Ezetimibe used alone is modestly effective in lowering LDL cholesterol. At a dose of 10 mg/day it can reduce LDL cholesterol by approximately 17%. When used with a statin, it can reduce LDL cholesterol level further than a statin alone. However, there is insufficient scientific data to determine whether a statin-ezetimibe combination actually further reduces heart attack or stroke risks. A new combination drug, Vytorin, is available and combines 10 mg of Zetia with 20, 40, or 80 mg of Zocor.

Ezetimibe is probably most useful in avoiding having to use high doses of a statin to achieve the 2004 NCEP LDL cholesterol targets in certain patients. Using lower doses of a statin probably reduces the risk of muscle injury. A statin-ezetimibe combination may also be helpful in treating patients with very high LDL cholesterol who cannot attain LDL cholesterol targets even with maximal doses of statins. Ezetimibe can be taken with or without food and at the same time as statin drugs.

Ezetimibe is well-tolerated. The overall rate of side effects with ezetimibe in clinical studies was similar to that reported with a placebo (an inactive sugar pill). Diarrhea, abdominal pain, back pain, joint pain, and sinusitis were the most commonly reported side effects, occurring in 1 in every 25 to 30 patients.