ezetimibe

(ee zet' ah mib)

Zetia

Pregnancy Category C

Drug classes
Cholesterol-lowering agent
Cholesterol absorption inhibitor

Therapeutic actions
Localizes in the brush border of the small intestine and inhibits the absorption of
cholesterol from the small intestine; this leads to a decrease delivery of dietary
cholesterol to the liver, which will then increase the clearance of cholesterol from the
blood and lead to a decrease in serum cholesterol.

Indications
• As an adjunct to diet and exercise to lower the cholesterol, LDL and Apo-B levels
in patients with primary hypercholesterolemia as monotherapy or in combination
with HMG-CoA reductase inhibitors (statins) or bile acid sequestrants
• In combination with atorvastatin or simvastatin for the treatment of homozygous
familial hypercholesterolemia as adjuncts to other lipid-lowering treatments
• As adjunctive therapy to diet for the treatment of homozygous sitosterolemia to
reduce elevated sitosterol and campesterol levels

Contraindications and cautions

• Contraindicated with allergy to any component of the drug. If given in
combination with an HMG-CoA reductase inhibitor, contraindicated with
pregnancy, lactation, active liver disease, or unexplained persistent increases in
serum transaminase levels.
• In monotherapy, use cautiously with liver dysfunction, pregnancy, lactation,
elderly patients.

Pharmacokinetics
Route Onset Peak
Oral Moderate 4–12 hr

Metabolism: Small intestine and hepatic; T1/2: 22 hr

Distribution: May cross placenta; may enter into breast milk
Excretion: Feces and urine

Available forms
Tablets—10 mg

Dosages
ADULTS
10 mg/day PO taken without regard to food; may be taken at the same time as an HMG-
CoA reductase inhibitor; if combined with a bile acid sequestrant, should be taken > 2 hr
before or > 4 hr after the bile acid sequestrant.
PEDIATRIC PATIENTS
Safety and efficacy not established.

Adverse effects
• CNS: Headache, dizziness, fatigue
• GI: Abdominal pain, diarrhea
• Respiratory: Pharyngitis, sinusitis, upper respiratory infection, cough
• Other: Back pain, myalgia, arthralgia, viral infection

Interactions
Drug-drug
• Decreased serum levels and decreased effectiveness of ezetimibe if combined
with cholestryamine; monitor patient closely and space ezetimibe dosing > 2 hr
before or > 4 hr after the other drug
• Increased serum levels of ezetimide if combined with fenofibrate, gemfibrozil
• Risk of cholethiasis if combined with fibrates (concomitant use with fibrates not
recommended)
• Risk of increased levels and toxicity of exetimibe if combined with cyclosporine;
if this combination is used; monitor patient very carefully

Nursing considerations
Assessment
• History: Allergy to any component of the drug; pregnancy, liver dysfunction,
lactation, evidence of diet and exercise program
• Physical: Skin lesions, color, temperature; orientation, affect; liver evaluation,
bowel sounds; lipid studies, liver function tests

Interventions
• Monitor serum cholesterol, LDLs, triglycerides before starting treatment and
periodically during treatment.
• Determine that patient has been on low cholesterol diet and exercise program for
at least 2 wk before starting ezetimibe.
• If used as part of combination therapy; give drug at the same time as HMG-CoA
reductase inhibitors and > 2 hr before or > 4 hr after bile acid sequestrants.
• Encourage the use of barrier contraceptives if used with an HMG-CoA reductase
inhibitor.
• Help mother to find another method of feeding her baby if this drug is needed for
a nursing woman, it is not known if the drug enters breast milk.
• Consult with dietician regarding low cholesterol diets and provide information
about exercise programs.
• Arrange for regular follow-up during long-term therapy.
Teaching points
• Take drug once each day at a time that is easy for you to remember. Do not take
more than one tablet per day.
• Continue to take any other lipid-lowering drugs that have been prescribed for
you. If you are also taking a bile acid sequestrant, take this drug at least 2 hr
before or at least 4 hr after the bile sequestrant.
• Continue to follow your low-fat diet and participate in an exercise program.
• Plan to return for periodic blood tests, including tests of liver function and
cholesterol levels, to evaluate the effectiveness of this drug.
• These side effects may occur: Abdominal pain, diarrhea (these usually pass with
time, notify your health care provider if this becomes a problem); dizziness,
(avoid driving and operating dangerous machinery until you know how this drug
affects you); headache (analgesics may help).
• Report unusual muscle pain, weakness, or tenderness; severe diarrhea; respiratory
infections.

Adverse effects in Italic are most common; those in Bold are life-threatening.