ezetimibe
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ezetimibe
Pharmacologic class: Cholesterol absorption inhibitor
Therapeutic class: Antihyperlipidemic
Pregnancy risk category C
Action
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.
Availability
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.
Contraindications
• 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)
Precautions
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.
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).

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
Interactions
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.