Ezetimibe
Pronouncation: (Ez-ET-i-mibe)Class: Antihyperlipidemic agent
Trade Names:
Zetia
- Tablets 10 mg
Pharmacology
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Inhibits absorption of cholesterol by the small intestine.
Pharmacokinetics
Absorption
C max is 3.4 to 5.5 ng/mL (ezetimibe) and 45 to 71 ng/mL (metabolite). T max is 4 to 12 h (ezetimibe) and 1 to 2 h (metabolite).
Distribution
More than 90% protein bound.
Metabolism
Metabolized (active) in small intestine and liver to ezetimibe glucoronide.
Elimination
The t ½ is approximately 22 h. Approximately 78% is excreted in feces and 11% in urine.
Special Populations
Renal Function ImpairmentAUC increased approximately 1.5-fold in those with severe renal disease (Ccr up to 30 mL/min).
Hepatic Function ImpairmentAUC increased approximately 1.7-fold in those with mild impairment, 3- to 4-fold in moderate impairment, and 5- to 6-fold in severe impairment.
ElderlyPlasma concentrations are approximately 2-fold higher.
Indications and Usage
Administration alone or with HMG-CoA reductase inhibitors as adjunctive therapy to diet for reduction of elevated total cholesterol, LDL cholesterol, and apolipoprotein (apo) in patients with primary hypercholesterolemia; with atorvastatin or simvastatin for the reduction of elevated total cholesterol and LDL levels in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments or if such treatments are unavailable; as adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia; with fenofibrate as an adjunct to diet for reduction of elevated total cholesterol, LDL cholesterol, apo, and non-HDL cholesterol in patients with mixed hyperlipidemia.
Contraindications
Ezetimibe is contraindicated in combination with HMG-CoA reductase inhibitors in patients with active liver disease or unexplained persistent elevations in serum transaminases; hypersensitivity to any component of the product.
Dosage and Administration
Adults and children older than 10 yr of agePO 10 mg once daily.
General Advice
- Administer with or without food. Administer alone or in combination with other lipid-lowering therapy.
- Administer 2 h before or 4 h after a bile acid sequestrant.
Storage/Stability
Store tablets at controlled room temperature (59° to 86°F). Protect from moisture.
Drug Interactions
AntacidsAluminum- and magnesium-containing antacids decrease the peak concentration of ezetimibe but not the AUC.
CholestyramineThe AUC of ezetimibe may be decreased.
Cyclosporine, fibric acid derivatives (eg, fenofibrate, gemfibrozil)Concentrations of ezetimibe may be increased.
Laboratory Test Interactions
None well documented.
Adverse Reactions
CNS
Headache (8%); dizziness (3%); fatigue (2%).
EENT
Pharyngitis (3%).
GI
Abdominal pain, diarrhea (3%); pancreatitis (postmarketing).
Hepatic
Cholecystitis, cholelithiasis, hepatitis (postmarketing).
Lab Tests
Elevated CPK, elevated liver transaminases (postmarketing).
Metabolic-Nutritional
Thrombocytopenia (postmarketing).
Musculoskeletal
Myalgia (5%); arthralgia, back pain (4%); myopathy/rhabdomyolysis (postmarketing).
Respiratory
Upper respiratory tract infection (13%); sinusitis (5%); sinusitis (4%); coughing (2%).
Miscellaneous
Chest pain (3%); viral infection (2%); hypersensitivity, including anaphylaxis, angioedema, rash, and urticaria (postmarketing).
Precautions
MonitorWhen given with an HMG-CoA reductase inhibitor, monitor LFTs. LipidsEnsure that lipids are measured before therapy is started and periodically during therapy. |
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established in children younger than 10 yr of age.
Hepatic Function
Use not recommended because of unknown effects on liver.
Secondary causes of hyperlipidemia
Rule out or treat secondary causes of hyperlipidemia before starting treatment with ezetimibe.
Skeletal muscle effects
Rhabdomyolysis has been reported rarely with ezetimibe monotherapy.
Overdosage
Symptoms
Reports of overdosage have not been associated with serious adverse reactions.
Patient Information
- Advise patient to review the patient information leaflet before starting the medication and each time the medication is refilled.
- Advise patient to take once daily as prescribed, without regard to meals.
- Advise patient to try to take each dose at about the same time each day.
- Inform patient that drug helps control, but not does cure, cholesterol abnormality and to continue taking drug as prescribed if cholesterol levels are lowered.
- Caution patient not to change or stop taking the dose unless advised by health care provider.
- Advise patient that if a dose is missed, to take as soon as possible, but to never take more than 1 dose of medicine a day.
- Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
- Emphasize to patient the importance of the following other modalities on cholesterol control: dietary changes (eg, increase soluble fiber intake, reduced saturated fat intake), regular exercise, smoking cessation, and weight control.
- Instruct patient to promptly notify health care provider of any unexplained muscle pain, tenderness, weakness, or any other unusual feelings.
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More Ezetimibe resources:
Ezetimibe - Includes detailed dosage instructions.
Sitosterolemia, High Cholesterol, High Cholesterol - Familial Heterozygous
