Indications and Dosage
Oral
Homozygous familial sitosterolaemia, Hyperlipidaemias
Adult: 10 mg once daily.
Child: ≥10 yr Same as adult dose. |
Administration
May be taken with or without food.
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Special Precautions
Exclude or treat secondary causes of dyslipidaemia prior to initiating therapy. Renal and hepatic impairment. Pregnancy and lactation.
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Adverse Reactions
Headache, abdominal pain, diarrhoea, fatigue, chest pain, arthralgia, myalgia, anaphylaxis, erythema multiforme, angioedema, rash, and urticaria. Rarely, raised liver enzymes or hepatitis, pancreatitis, thrombocytopenia, cholelithiasis, cholecystitis, raised creatine kinase, myopathy, and rhabdomyolysis.
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Monitoring Parameters
Monitor total cholesterol profile prior to therapy and periodically thereafter.
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Drug Interactions
Reduced absorption w/ colestyramine. Increased plasma concentrations w/ ciclosporin. Concomitant use w/ oral anticoagulants may result in increased INR.
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Action
Description: Ezetimibe localises at the brush border of the small intestine and inhibits absorption of cholesterol via the sterol transporter, Niemann-Pick C1-Like1 (NPC1L1). This results in decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores and increased clearance of cholesterol from the blood.
Pharmacokinetics: Absorption: Rapidly absorbed. Time to peak plasma concentration: 4-12 hr. Distribution: Plasma protein binding: >90%. Metabolism: Undergoes extensive conjugation in small intestine and liver to form an active glucuronide metabolite; may also undergo enterohepatic recycling. Excretion: Via bile in the faeces (approx 78% mainly as unchanged drug); urine (approx 11% mainly as metabolite). Elimination half-life: Approx 22 hr. |