Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD
GENERIC NAME: ezetimibe
BRAND NAME: Zetia
DRUG CLASS AND MECHANISM: Ezetimibe is a drug that is used for the
treatment of elevated blood cholesterol. The most commonly used class of drugs
for lowering cholesterol levels, the statins, act by preventing the production
of cholesterol by the liver. Ezetimibe has a different mechanism of action and
lowers blood cholesterol by reducing the absorption of cholesterol from the
intestine. It does not affect the absorption of triglycerides or fat-soluble
vitamins. The FDA approved ezetimibe in October 2002.
PRESCRIPTION: Yes
GENERIC AVAILABLE: No
PREPARATIONS: Tablets, 10 mg
STORAGE: Ezetimibe tablets should be stored between 15°-30°C (59°-86°F).
PRESCRIBED FOR: Ezetimibe is used in combination with statins to
improve levels of total cholesterol, low-density lipoprotein cholesterol,
triglycerides, high-density lipoprotein cholesterol, and apolipoprotein B.
Combining ezetimibe with a statin is more effective than either drug alone.
Ezetimibe may be used alone or in combination with fibrates [for example,
fenofibrate
(Tricor)] to improve levels of
cholesterol, low-density lipoprotein cholesterol, and apolipoprotein B.
DOSING: The recommended dose of ezetimibe is 10 mg daily. Ezetimibe can be
taken with or without food and at the same time as statin drugs.
DRUG INTERACTIONS: Cholestyramine (Questran), colestipol (Colestid) and
colesevelam (WelChol), bile acid-binding drugs that may be used to treat
elevated levels of cholesterol, bind to ezetimibe and reduce its absorption from
the intestine by about 50%. Therefore, ezetimibe should be taken at least two
hours after or one hour before these drugs.
Cyclosporine (Gengraf, Neoral) increases the levels of
ezetimibe and could lead to greater side effects of ezetimibe.
PREGNANCY: There are no adequate studies of ezetimibe in pregnant women.
Therefore, physicians must weight the benefit of prescribing ezetimibe during
pregnancy against potential unknown risks.
NURSING MOTHERS: There are no adequate studies of ezetimibe in
nursing women.
Therefore, physicians must weight the benefit of prescribing ezetimibe to
nursing women against potential unknown risks.
SIDE EFFECTS: Ezetimibe is well-tolerated. The overall rate of side effects
with ezetimibe in clinical studies were similar to that reported with placebo
(an inactive sugar pill). Diarrhea, abdominal pain,
back pain, joint pain, and
sinusitis were the most commonly reported side effects, occurring in one in every
25 to 30 patients. 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 been reported in
post-marketing studies.
Last Editorial Review: 4/16/2008
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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