Dosage Forms
- 10 mg tablet
Drug Group
Anti-hypercholesterolemia
Packaging
- 10 tablets in one blister. 3 blisters in a box.
Primary hypercholesterolemia. Ezetimibe is indicated as adjunctive therapy to diet for the reduction of elevated total-cholesterol, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia and reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.
Ezetimibe is an inhibitor of intestinal cholesterol absorption. Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to decrease in the delivery of intestinal cholesterol to the liver.
When ezetimibe is co-administered with an HMG-CoA reductase inhibitor, liver function tests should be performed at initiation of therapy and according to the recommendations of the HMG-CoA reductase inhibitor. Due to the unknown effects of the increased exposure to ezetimibe in patients with moderate or severe hepatic insufficiency, ezetimibe is not recommended in these patients.
The most common adverse effects include headache, abdominal pain, and diarrhea; other gastro-intestinal disorders, myalgia, upper respiratory tract infection, back pain, coughing, dizziness, pharyngitis, sinusitis and urinal infection, hypersensitivity reactions including rash and angioedema, fatigue, chest pain, and arthralgia.
Pregnancy category C. It is not known whether ezetimibe is distributed into human breast milk. Therefore, ezetimibe should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant.
Colestyramine: reduces the absorption of ezetimibe and should not be given at the same time of day. Cyclosporine: has been reported to increase the plasma concentration of ezetimibe and patients receiving both drugs should be carefully monitored. Fenofibrate: Concomitant administration increases total ezetimibe concentrations. Fibrates: Concomitant administration increases cholesterol excretion leading to cholelithiasis.