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Pharmacologic class: Cholesterol absorption inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category C


Inhibits cholesterol absorption in the intestine, decreasing intestinal delivery of cholesterol to the liver and increasing systemic cholesterol clearance. Net effect is decreased serum cholesterol level.


Tablets: 10 mg

Indications and dosages

Adjunct to diet to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), nonhigh-density lipoprotein cholesterol (non-HDL-C), and apolipoprotein B (Apo B) in patients with primary hyperlipidemia, alone or in combination with HMG-CoA reductase inhibitor; to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia, in combination with fenofibrate; to reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia, in combination with atorvastatin or simvastatin; to reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia

Adults: 10 mg/day P.O.


• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained, persistent transaminase elevations (when given with a statin)
• Women who are pregnant or may become pregnant (when given with a statin)
• Breastfeeding patients (when given with a statin)


Use cautiously in:
• moderate or severe hepatic impairment (use not recommended)
• skeletal muscle toxicity
• concurrent use of cyclosporine or fibrates other than fenofibrate (use not recommended)
• elderly patients
• pregnant or breastfeeding patients not receiving HMG-CoA reductase inhibitors
• children younger than age 10.


• Give with or without food.
• Be aware that drug may be given concurrently with HMG-CoA reductase inhibitor (such as atorvastatin or simvastatin).
• Give at least 2 hours before or 4 hours after bile acid sequestrant (if prescribed).

Adverse reactions

CNS: headache, dizziness, fatigue

EENT: nasopharyngitis, sinusitis

GI: diarrhea

Musculoskeletal: back pain, myalgia, joint pain, extremity pain, rhabdomyolysis

Respiratory: upper respiratory tract infection


Drug-drug.Cholestyramine: decreased ezetimibe blood level

Cyclosporine, fenofibrate, gemfibrozil: increased ezetimibe blood level

Fibrates: increased risk of cholesterol excretion into gallbladder leading to cholelithiasis

Drug-diagnostic tests.Liver function tests: increased values

Patient monitoring

• Monitor hepatic and lipid profiles.
• Monitor cyclosporine concentration in patients receiving drug concurrently with cyclosporine.
• Monitor International Normalized Ratio if patient also receiving warfarin.
• Assess for and report unexplained muscle pain.
• If cholelithiasis is suspected in patient also receiving fenofibrate, obtain gallbladder studies and consider alternative lipid-lowering therapy.

Patient teaching

• Teach patient about the role of diet, exercise, and weight loss in lowering cholesterol levels.

Instruct patient to immediately report unexplained muscle pain, tenderness, or weakness while taking this drug.
• Advise breastfeeding patient not to take this drug while taking a statin.
• Advise female patient of childbearing age to use effective contraception while taking this drug concurrently with a statin and if she becomes pregnant to stop taking ezetimibe and statin and call her prescriber.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


A drug that inhibits the absorption of cholesterol from the intestine and is used to treat primary hypercholesterolemia.


an antilipemic agent used to treat hypercholesterolemia, homozygous low-density lipoprotein receptor disorder, and homozygous sitosterolemia.


A cholesterol absorption inhibitor drug that can be used alone or, more effectively, in conjunction with a statin drug (see STATINS) to reduce blood cholesterol levels in people with hypercholesterolaemia. Such people are at risk of developing ATHEROSCLEROSIS. The drug acts specifically to inhibit cholesterol absorption and does not affect the absorption of other lipids. A brand name is Ezetrol.
References in periodicals archive ?
Ezetimibe has a long half-life that allows for once-daily dosing.
Ezetimibe reduced prostatic enlargement in aged hamsters as effectively as finasteride and combining the two drugs worked better than either one alone.
The researchers showed that ezetimibe inhibited HCV infection in cell culture and in mice transplanted with human liver cells.
In a study of aortic stenosis the patients randomised to ezetimibe + simvastatin had more cancer-related deaths than the placebo group.
The case of a 64-year-old African-American female who developed pancreatitis soon after she was started on ezetimibe is presented.
Ezetimibe (Zetia) appears to be low risk in gestation, but not in lactation.
This piece summarizes some features of this newest statin and also discusses briefly some characteristics of ezetimibe (Zetia), the other drug for dyslipidemia also introduced in the USA in 2003.
Ezetimibe can selectively inhibit cholesterol transporter in the small intestine, effectively reduce cholesterol absorption, lower plasma cholesterol level and decrease the amount of cholesterol normally available to liver cells.
In that study, the addition of 10 mg of ezetimibe to 40 mg of simvastatin in 18,144 patients followed for up to 6 years resulted in a 2% decrease in mortality associated with a 15.
A drug called ezetimibe, marketed as Zetia, lowers LDL by inhibiting activity of the same protein.
d) switch to simvastatin 20 mg/ day plus ezetimibe 10 mg/day