Ezetrol 10-MG Tablet

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 patient should be on an appropriate lipid lowering diet and should continue on this diet during treatment with Ezetimibe.

Adult Dose: The recommended dose is Ezetimibe 10 mg tablet once daily. Ezetimibe can be administered at any time of the day, with or without food.

Use in the elderly: No dosage adjustment is required for elderly patients.

Pediatric Use–

• 10 to 17 years: No dosage adjustment is required. The clinical experience in pediatric and adolescent patients is however limited. When Ezetimibe is administered with statin, the dosage instructions for statin, in adolescents should be consulted.
• Children <10 years: Ezetimibe is not recommended for use in children below age 10 due to insufficient data on safety and efficacy.

Use in hepatic impairment: No dosage adjustment is required in patients with mild hepatic insufficiency (Child Pugh score 5 to 6). Treatment with Ezetimibe is not recommended in patients with moderate (Child Pugh score 7 to 9) or severe (Child Pugh score>9) liver dysfunction.

Use in renal impairment: No dosage adjustment is required for renally impaired patients

Fibrates may increase cholesterol excretion into the bile, leading to cholelithiasis. In a preclinical study in animals, Ezetrol increased cholesterol in the gallbladder bile. Coadministration of Ezetrol 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 Ezetrol (administered alone or with an HMG-CoA reductase inhibitor) demonstrated that Ezetrol was generally well tolerated. The overall incidence of adverse events reported with Ezetrol was similar to that reported with placebo, and the discontinuation rate due to adverse events was also similar for Ezetrol and placebo.

The following adverse reactions were observed in patients treated with Ezetrol:

• Common or very common: Fatigue, gastro-intestinal disturbances, headache, myalgia.
• Rare: Anaphylaxis, angioedema, arthralgia, hepatitis, hypersensitivity reactions, rash.
• Very rare: Cholecystitis, cholelithiasis, myopathy, pancreatitis, raised creatine kinase, rhabdomyolysis, thrombocytopenia.

Pregnancy: Ezetimibe should be given to pregnant women only if clearly necessary. No clinical data are available on the use of Ezetimibe during pregnancy. Animal studies on the use of ezetimibe in monotherapy have shown no evidence of direct or indirect harmful effects on pregnancy, embryofoetal development, birth or postnatal development.

Breast feeding: Ezetimibe should not be used during lactation. Studies on rats have shown that ezetimibe is secreted into breast milk. It is not known if ezetimibe is secreted into human breast milk.

Fertility: No clinical data are available. No effects on fertility were observed in non-clinical studies.

Concurrent administration of Ezetrol with a specific HMG-CoA reductase inhibitor should be in accordance with the product labeling for that HMG-CoA reductase inhibitor.

In clinical studies, administration of Ezetrol, 50 mg/day to 15 healthy subjects for up to 14 days, or 40 mg/day to 18 patients with primary hypercholesterolaemia for up to 56 days, was generally well tolerated. In animals, no toxicity was observed after single oral doses of 5000 mg/kg of Ezetrol in rats and mice and 3000 mg/kg in dogs. A few cases of overdosage with Ezetrol have been reported; most have not been associated with adverse experiences. Reported adverse experiences have not been serious. In the event of an overdose, symptomatic and supportive measures should be employed.

Ezetimibe

To be dispensed only by or on the prescription of registered physician. Keep out of the reach of children. Store below 30°C. Keep in a cool & dry place. in order to protect from light and moisture