Ezetimibe

Hypolipidaemic/Anti-atheroma · Cholesterol absorption inhibitor

Indications

Adjunct to diet in primary hypercholesterolaemia either co-administered with a statin for patients not appropriately controlled with a statin alone, or as monotherapy when a statin is inappropriate or not tolerated. Adjunct to diet in homozygous familial hypercholesterolaemia in combination with a statin and, if necessary, other adjunctive treatments. Adjunct to diet in homozygous familial sitosterolaemia.

Dosage

Adults: 1 tab daily. Children: Under 10 yr, not recommended. Adjunct to statin treatment in primary hypercholesterolaemia and homozygous familial hypercholesterolaemia, ezetimibe alone in primary hypercholesterolaemia if statin inappropriate or not tolerated; adjunct to dietary measures in homozygous sitosterolaemia: 10-18 yr, 10 mg once daily.

Adverse Effects

Headache, abdominal pain, diarrhoea, GI upset, fatigue, abnormal LFTs.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Risk cannot be ruled out. Lactation: Contraindicated or not recommended. Contraindications: Moderate to severe hepatic impairment, concomitant use with a statin in active liver disease. Precautions: Monitor liver function if giving with a statin. Unexplained muscle weakness or pain; monitor creatine kinase levels if myopathy suspected.

Interactions

Fibrates, cyclosporin, cholestyramine, colestipol, anticoagulants.

Advice to Patient

Take with or without meals. Take medication at the same time each day. Take 2 hours before or 4 hours after bile acid binding agents. Contact prescriber if there is chest pain, palpitations, muscle pain, weakness, skeletal pain, joint pain or increased sweating. Take low-cholesterol diet. Exercise regularly. Try to lose weight.

Pharmacokinetics

Onset of action: Within 1 wk. Max effect: 2-4 wks. Metabolism: Small intestine and liver. Bioavailability: Variable. Hepatic impairment: Moderate hepatic impairment (Child-Pugh score 7-9): AUC increased 3-4 times. Severe hepatic impairment (Child-Pugh 10-15): AUC increased 5-6 times. Renal impairment: Severe renal dysfunction (CrCl <30 mL/min/1.73 m2): AUC increased 1.5 times. Half-life elimination: 22 hrs (ezetimibe and metabolite).

Brands with this active ingredient

• Bemdo EZ
• Bemletol-EZ
• Bempeget-EZ
• Bempex-Z
• Bempion EZ
• Bmp-E
• Crescor-Eze
• Crestat EZ
• Eglocard S
• Ezita
• Ezkan
• Gauge
• Gelita
• Kestore-EZ
• Loster EZ

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.