Trade Names:Zetia- Tablets 10 mgEzetrol (Canada)
Inhibits absorption of cholesterol by the small intestine.
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).
More than 90% protein bound.
Metabolized (active) in small intestine and liver to ezetimibe glucoronide.
The t ½ is approximately 22 h. Approximately 78% is excreted in feces and 11% in urine.
AUC increased approximately 1.5-fold in those with severe renal disease (CrCl up to 30 mL/min).Hepatic Function Impairment
AUC 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.Elderly
Plasma concentrations are approximately 2-fold higher.
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.
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.
PO 10 mg once daily.
Store tablets at controlled room temperature (59° to 86°F). Protect from moisture.
Aluminum- and magnesium-containing antacids decrease the peak concentration of ezetimibe but not the AUC.Cholestyramine
The AUC of ezetimibe may be decreased.Cyclosporine, fibric acid derivatives (eg, fenofibrate, gemfibrozil)
Concentrations of ezetimibe may be increased.
None well documented.
Headache (8%); dizziness (3%); fatigue (2%).
Abdominal pain, diarrhea (3%); pancreatitis (postmarketing).
Cholecystitis, cholelithiasis, hepatitis (postmarketing).
Elevated CPK, elevated liver transaminases (postmarketing).
Myalgia (5%); arthralgia, back pain (4%); myopathy/rhabdomyolysis (postmarketing).
Upper respiratory tract infection (13%); sinusitis (5%); sinusitis (4%); coughing (2%).
Chest pain (3%); viral infection (2%); hypersensitivity, including anaphylaxis, angioedema, rash, and urticaria (postmarketing).
When given with an HMG-CoA reductase inhibitor, monitor LFTs.Lipids
Ensure that lipids are measured before therapy is started and periodically during therapy.
Category C .
Safety and efficacy not established in children younger than 10 yr of age.
Use not recommended because of unknown effects on liver.
Rule out or treat secondary causes of hyperlipidemia before starting treatment with ezetimibe.
Rhabdomyolysis has been reported rarely with ezetimibe monotherapy.
Reports of overdosage have not been associated with serious adverse reactions.
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