(ee zet' ah mib)
Pregnancy Category C
Cholesterol absorption inhibitor
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.
· 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.
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.
Safety and efficacy not established.
Metabolism: Small intestine and hepatic; T1/2: 22 hr
Distribution: May cross placenta; may enter into breast milk
Excretion: Feces and urine
· CNS: Headache, dizziness, fatigue
· GI: Abdominal pain, diarrhea
· Respiratory: Pharyngitis, sinusitis, URI, cough
· Other: Back pain, myalgia, arthralgia, viral infection
· 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
· 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
· 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.
· 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.