Ezetim : Each tablet contains Ezetimibe INN 10 mg.
Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe reduces total-C, LDL-C, Apo B, and TG, and increases HDL-C in patients with hypercholesterolemia. Administration of Ezetimibe with an HMG-CoA reductase inhibitor is effective in improving serum total-C, LDL-C, Apo B, TG, and HDL-C beyond either treatment alone. Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. In a 2-week clinical study in 18 hypercholesterolemic patients, Ezetimibe inhibited intestinal cholesterol absorption by 54%, compared with placebo. Ezetimibe had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E, and did not impair adrenocortical steroid hormone production. The cholesterol content of the liver is derived predominantly from three sources. The liver can synthesize cholesterol, take up cholesterol from the blood from circulating lipoproteins, or take up cholesterol absorbed by the small intestine. Intestinal cholesterol is derived primarily from cholesterol secreted in the bile and from dietary cholesterol. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants [resins], fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion. Instead, Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors.
Ezetimibe can be administered with or without food.
Ezetimibe administered alone, is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.
Combination therapy with HMG-CoA reductase inhibitors
Ezetimibe, administered in combination with an HMG-CoA reductase inhibitor, is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.
Homozygous Familial Hypercholesterolemia (HoFH)
The combination of Ezetimibe and Atorvastatin or Simvastatin, is indicated for the reduction of elevated total-C and LDL-C levels in patients with HoFH, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are unavailable.
Ezetimibe is indicated as adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia. Therapy with lipid-altering agents should be a component of multiple risk-factor intervention in individuals at increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Lipidaltering agents should be used in addition to an appropriate diet (including restriction of saturated fat and cholesterol) and when the response to diet and other non-pharmacological measures has been inadequate.
Dosage & Administration
The patient should be placed on a standard cholesterol-lowering diet before receiving Ezetimibe and should continue on this diet during treatment with Ezetimibe. The recommended dose of Ezetimibe is 10 mg once daily. Ezetimibe can be administered with or without food. Ezetimibe may be administered with an HMG-CoA reductase inhibitor for incremental effect. For convenience, the daily dose of Ezetimibe may be taken at the same time as the HMG-CoA reductase inhibitor, according to the dosing recommendations for the HMG-CoA reductase inhibitor.
Patients with Hepatic Insufficiency
No dosage adjustment is necessary in patients with mild hepatic insufficiency.
Patients with Renal Insufficiency
No dosage adjustment is necessary in patients with renal insufficiency.
No dosage adjustment is necessary in geriatric patients.
Co-administration with Bile Acid Sequestrants
Dosing of Ezetimibe should occur either 2 hours before or 4 hours after administration of a bile acid sequestrant.
Ezetimibe has been evaluated for safety in more than 4700 patients in clinical trials. 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. The rare side effects include fatigue, abdominal pain, diarrhea, infection viral, pharyngitis, sinusitis, arthralgia, back pain, coughing.
Concurrent administration Ezetimibe with a specific HMG-CoA reductase inhibitor should be in accordance with the product labeling for that HMG-CoA reductase inhibitor. 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.
Hepatic Insufficiency : 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.
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.
The pharmacokinetics of Ezetimibe in adolescents (10 to 18 years) has been shown to be similar to that in adults. Treatment with Ezetimibe in children (<10 years) is not recommended.
Use in Pregnancy & Lactation
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.
Ezetim : Each box contains 3 Alu-Alu blister strips of 10 tablets