ezetimibe

e·zet·i·mibe (-zt-mb)

n.

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

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ezetimibe,

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

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ezetimibe

Ezetrol (UK), Zetia

Pharmacologic class: Cholesterol absorption inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category C

Action

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

Availability

Tablets: 10 mg

⊘Indications and dosages

➣ Adjunct to diet and exercise in primary hypercholesterolemia; adjunct to other lipid-lowering drugs in homozygous familial hypercholesterolemia; adjunct to diet in homozygous sitosterolemia

Adults: 10 mg/day P.O.

Contraindications

• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained, persistent transaminase elevations (when given with HMG-CoA reductase inhibitors)
• Pregnancy (when given with HMG-CoA reductase inhibitors)

Precautions

Use cautiously in:
• renal or hepatic impairment
• elderly patients
• pregnant patients not receiving HMG-CoA reductase inhibitors
• breastfeeding patients
• children younger than age 10.

Administration

• 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).

Route	Onset	Peak	Duration
P.O.	Moderate	4-12 hr	Unknown

Adverse reactions

CNS: headache, dizziness, fatigue

EENT: pharyngitis, sinusitis

GI: nausea, vomiting, diarrhea, abdominal pain, flatulence, dyspepsia, dry mouth, anorexia

Musculoskeletal: back pain, myalgia, joint pain

Respiratory: pneumonia, upper respiratory tract infection

Other: viral infection

Interactions

Drug-drug. Cholestyramine: decreased ezetimibe blood level

Cyclosporine, fenofibrate, gemfibrozil: increased ezetimibe blood level

Fibrates: increased risk of cholesterol excretion into gallbladder

Immunosuppressants: increased immunosuppression and bone marrow depression

Drug-diagnostic tests. Liver function tests: increased values

Patient monitoring

• Monitor hepatic and lipid profiles.
• Assess for and report unexplained muscle pain.

Patient teaching

• Teach patient about role of diet, exercise, and weight loss in lowering cholesterol levels.
• Instruct patient to report GI upset.
• Caution female patient to avoid pregnancy during therapy.
• Advise patient to use hard candy or gum to relieve dry mouth.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.