Primary Hypercholesterolemia: Ezetimibe co-administered with statin is indicated as adjunctive therapy to diet for use in patients with primary (heterozygous familial and non-familial) hypercholesterolemia who are not appropriately controlled with a statin alone. Ezetimibe monotherapy is indicated as adjunctive therapy to diet for use in patients with primary (heterozygous familial and non-familial) hypercholesterolemia in whom a statin is considered inappropriate or is not tolerated. Prevention of Cardiovascular Events: Ezetimibe is indicated to reduce the risk of cardiovascular events in patients with coronary heart disease (CHD) and a history of acute coronary syndrome (ACS) when added to ongoing statin therapy or initiated concomitantly with a statin. Homozygous Familial Hypercholesterolaemia (HoFH): Ezetimibe co-administered with a statin, is indicated as adjunctive therapy to diet for use in patients with HoFH. Patients may also receive adjunctive treatments (e.g., LDL apheresis). Homozygous Sitosterolemia (Phytosterolemia): Ezetimibe is indicated as adjunctive therapy to diet for use in patients with homozygous familial sitosterolemia
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.
The recommended dose of Ezetimibe is 10 mg once daily. Ezetimibe can be administered with or without food.
Fibrates may increase cholesterol excretion into the bile, leading to cholelithiasis. In a preclinical study in animals, Ezetimibe increased cholesterol in the gallbladder bile. Coadministration of Ezetimibe with fibrates is not therefore recommended until use in patients is studied.
Hypersensitivity to any component of this medication. The combination of Ezetimibe with an HMG-CoA reductase inhibitor is contraindicated in patients with active liver disease or unexplained persistent elevations in serum transaminases.
Clinical studies of Ezetimibe (administered alone or with an HMG-CoA reductase inhibitor) demonstrated that Ezetimibe was generally well tolerated. The overall incidence of adverse events reported with Ezetimibe was similar to that reported with placebo, and the discontinuation rate due to adverse events was also similar for Ezetimibe and placebo.
There are no adequate and well-controlled studies of Ezetimibe in pregnant women. Ezetimibe should be used during pregnancy only if the potential benefit justifies the risk to the fetus
No cases of overdosage with Ezetimibe have been reported. Administration of Ezetimibe, 50 mg/day, to 15 subjects for up to 14 days was generally well tolerated. In the event of an overdose, symptomatic and supportive measures should be employed.
Exclude or treat secondary causes of dyslipidaemia prior to initiating therapy. Renal and hepatic impairment. Pregnancy and lactation.
Store in a cool & dry place protected from light and moisture. Keep out of reach of children.