Names and pronunciation
(ehz-eh-tim′bee) Ezetrol , Zetia
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Drug reference
(ehz-eh-tim′bee) Ezetrol , Zetia
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Func. class.: Antilipemic; cholesterol absorption inhibitor
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ACTION: Inhibits absorption of cho- lesterol by the small intestine, causes reduced hepatic cholesterol stores
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USES: Hypercholesterolemia, homo- zygous familial hypercholesterolemia (HoFH), homozygous sitosterolemia
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CONTRAINDICATIONS: Hyper- sensitivity, severe hepatic disease Precautions: Pregnancy, breastfeeding, children, hepatic disease
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SIDE EFFECTS CNS: Fatigue, dizziness, headache GI: Diarrhea, abdominal pain MISC: Chest pain MS: Myalgias, arthralgias, back pain, myopathy, rhabdomyolysis RESP: Pharyngitis, sinusitis, cough, URI EENT: Sinusitis, nasopharyngitis SYST: Angioedema
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INTERACTIONS Increase: action of ezetimibe—fibric acid derivatives, cycloSPORINE E Decrease: action of ezetimibe—antac- ids, bile acid sequestrants Drug/Lab Test Increase: LFTs
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DOSAGE AND ROUTES • Adult/adolescent/child >10 yr: PO 10 mg/day
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Available forms: Tablets 10 mg
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Administer: Without regard to meals • Separate by ≥2 hr prior to or ≥4 hr after bile acid sequestrant, may use with HMG-CoA reductase inhibitors
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Assess: • Hypercholestrolemia: diet history: fat content, lipid levels (triglycerides, LDL, HDL, cholesterol); LFTs at baseline, peri- odically during treatment • Myopathy/rhabdomyolysis: increased CPK, myalgia, muscle cramps, musculo- skeletal pain, lethargy, fatigue, fever; more common when combined with statins • Pregnancy/breastfeeding: do not use in pregnancy, breastfeeding
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Evaluate: • Therapeutic response: decreased cho- lesterol, LDL; increased HDL
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That compliance is needed • That risk factors should be decreased: high-fat diet, smoking, alcohol consump- tion, absence of exercise • To notify prescriber if pregnancy sus- pected, planned, or if breastfeeding • To notify prescriber if unexplained weakness, muscle pain present • To notify prescriber of dietary/herbal supplements
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PHARMACOKINETICS Absorption variable, metabolized in small intestine, liver; excreted in feces 78%, urine 11%; peak 4-12 hr; half- life 22 hr
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• Adult/adolescent/child >10 yr: PO 10 mg/day
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