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)

        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 in the elderly and with liver dysfunction, pregnancy, lactation.

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.

 

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

 

Adverse effects

        CNS: Headache, dizziness, fatigue

        GI: Abdominal pain, diarrhea

        Respiratory: Pharyngitis, sinusitis, URI, 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.

        You may experience these side effects: 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.