The information highlighted (if any) are the most recent updates for this brand.
Each tablet contains Ezetimibe 10 mg.
The score line is only to facilitate breaking for ease of swallowing and not for dividing dose.
Pharmacology: Pharmacodynamics: Ezetimibe, a cholesterol absorption inhibitor, is an antilipemic agent that differs chemically and pharmacologically from other currently available antilipemic agents. Following absorption, the drug localizes at the brush border of the small intestine and inhibits absorption of cholesterol through the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), resulting in decreased delivery of intestinal cholesterol to the liver. This causes a reduction in hepatic cholesterol stores, a compensatory increase in hepatic uptake of cholesterol from systemic circulation, and consequently, an increase in systemic clearance of cholesterol. Moreover, this decreases total cholesterol, LDL-cholesterol, apolipoprotein B (apo B), and triglyceride while increasing HDL-cholesterol.
Pharmacokinetics: Peak plasma concentrations of ezetimibe occur within 4 to 12 hours after an oral dose of ezetimibe. The effect of ezetimibe will present in approximately 2 weeks after therapy initiation. Its oral bioavailability is variable. It was found that food does not appear to affect the extent of absorption of ezetimibe. However, concomitant administration of the drug with a high-fat meal resulted in a 38% increase in peak plasma concentrations of the drug. Ezetimibe is rapidly absorbed when given orally and undergoes extensive conjugation in the small intestine and liver to ezetimibe glucuronide. Ezetimibe and its glucuronide metabolites constitutes 10-20% and 80-90% respectively, of the total absorbed drug in plasma. Both ezetimibe and ezetimibe glucuronide are more than 90% bound to plasma proteins. Ezetimibe and ezetimibe glucuronide are each slowly eliminated from plasma with a half-life of approximately 22 hours. After an oral dose, about 78% is excreted in the feces, mainly as ezetimibe, and about 11% is excreted in the urine, mainly as the glucuronide.
Primary Hypercholesterolemia: Ezetimibe administered with HMG-CoA reductase inhibitor (statin) or alone is indicated as adjunctive therapy to diet for the reduction of elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apo B), triglycerides (TG), non-high-density lipoprotein cholesterol (non-HDL-C) and to increase high-density lipoprotein cholesterol (HDL-C) in adult and adolescent (10-17 years of age) patients with primary (heterozygous familial and nonfamilial) hypercholesterolemia.
Ezetimibe administered in combination with fenofibrate, is indicated as adjunctive therapy to diet for the reduction of evaluated total-C, LDL-C, apo B, and non-HDL-C in adult patients with mixed hyperlipidemia.
Prevention of cardiovascular disease: Ezetimibe with a statin, is indicated to reduce the risk of cardiovascular events (cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, hospitalization for unstable angina, or need for revascularization), in patients with coronary heart disease (CHD).
Prevention of major cardiovascular events in chronic kidney disease: Ezetimibe, administered with simvastatin, is indicated to reduce the risk of major cardiovascular events in patient with chronic kidney disease.
Homozygous familial hypercholesterolemia (HoFH): Ezetimibe, administered with a statin, is indicated for the reduction of elevated total-C and LDL-C levels in adult and adolescent (10 to 17 years of age) patients with HoFH. Patient may also receive adjunctive treatments (e.g. LDL apheresis).
Homozygous familial sitosterolemia (Phytosterolemia): Ezetimibe with diet is indicated for the reduction of elevated serum sitosterol and campesterol levels in patients with homozygous familial sitosterolemia.
Use in patients with primary hypercholesterolemia, homozygous familial hypercholesterolemia, homozygous sitosterolemia in adults and children 10 years of age and older, the recommended dosage of ezetimibe is 10 mg once daily.
For prevention of cardiovascular disease, ezetimibe 10 mg may be administered with a statin with proven cardiovascular benefit.
Ezetimibe may be used alone or in combination with a statin or fenofibrate and may be administered at the same time as a statin or fenofibrate.
In combination with bile acid sequestrants, ezetimibe should be administered at least 2 hours before or 4 hours after the drug. Ezetimibe can be administered with or without food.
The recommended dosage of ezetimibe in fixed combination with simvastatin for the management of homozygous familial hypercholesterolemia in adults is 10 mg of ezetimibe and 40 mg of simvastatin once daily in the evening.
Use in Patients with Renal Impairment/Chronic Kidney Disease: Ezetimibe monotherapy: No dosage adjustment is necessary in patients with renal impairment.
Ezetimibe combination therapy with simvastatin: In patients receiving ezetimibe in fixed combination with simvastatin, no dosage adjustment is necessary in patients with mild renal impairment (estimated GFR of 60 mL/min/ 1.73 m2 or greater). In patients with chronic kidney disease and an estimated GFR of less than 60 mL/min/1.73 m2, the dosage of the fixed combination preparation is 10 mg of ezetimibe and 20 mg simvastatin once daily in the evening. In such patients, higher dosage should be used with caution and close monitoring.
Use in the Elderly: No dosage adjustment is necessary in geriatric patients.
Use in Pediatric patients: Children and adolescents ≥ 6 years may be given ezetimibe at the same doses as in adults. There are no differences in the pharmacokinetics of ezetimibe between children and adolescents ≥ 6 years and adults and pharmacokinetic data are not available for pediatric patients younger than 6 years of age.
Use in Hepatic Impairment: No dosage adjustment is required in patients with mild hepatic insufficiency (Child-Pugh score 5 to 6, class A). Because the effects of increased exposure to ezetimibe in patients with moderate (Child-Pugh score 7 to 9, class B) or severe (Child-Pugh score >9, class C) hepatic impairment currently is not known, ezetimibe is not recommended in such patients.
Overdose and treatment: Overdose data are limited. The signs and symptoms of an acute overdose are expected to be similar to excessive pharmacologic effects such as diarrhea, abdominal pain and fatigue. In the event of an overdose, symptomatic and supportive measures should be employed.
Known hypersensitivity to ezetimibe or any ingredient in the formulation.
Ezetimibe, in combination with a HMG-CoA reductase inhibitor (statin), is contraindicated in patients with active liver disease or unexplained, persistent increases in serum aminotransferase (transaminase) concentrations.
Concomitant use of the fixed combination of ezetimibe and simvastatin with potent inhibitors of cytochrome P-450 (CYP) isoenzyme 3A4, cyclosporine, danazol, or gemfibrozil is contraindicated.
Elevated hepatic transaminase: A higher incidence of elevated transaminases (3 or more times the upper limit of normal [ULN]) has been observed with concomitant use of ezetimibe and statins compared to statin monotherapy. Consider discontinuation of ezetimibe and/or the statin for persistently evaluated transaminase (ALT or AST 3 or more times the ULN).
Myopathy and rhabdomyolysis: Myopathy, including rhabdomyolysis, has been reported (rarely) with ezetimibe monotherapy. Risk may be increased with concomitant use of a statin or fibrate. Moreover, risk may be increased with patients older than 65 years of age, patients with hypothyroidism, higher dosage of statin. Discontinue ezetimibe and statins or fibrate immediately if myopathy is suspected or confirmed (symptomatic patient with creatinine phosphokinase more than 10 times the ULN).
Renal function impairment: Use with caution in patients with severe renal impairment (CrCl 30 mL/min/ 1.73 m2 or less). If using concurrent simvastatin in patients with moderate to severe renal impairment (CrCl less than 60 mL/min/1.73 m2) simvastatin dose exceeding 20 mg may be used with caution and close monitoring for adverse events (e.g. myopathy).
Hepatic function impairment: Use with caution in patients with mild hepatic impairment (Child-Pugh score 5 to 6, class A). Use is not recommended in patients with moderate or severe hepatic impairment (Child-Pugh score 7 to 9, class B or Child-Pugh score >9, class C).
Ezetimibe is rated as category C.
Use is contraindicated in pregnant women who require combination of ezetimibe and HMG-CoA reductase inhibitor.
The drug should not be used in nursing women unless the potential benefits justify the possible risks to the infant.
Central nervous system: Fatigue.
Gastrointestinal: Diarrhea.
Hepatic: Increase serum transaminases (with HMG-CoA reductase inhibitors; ≥ 3 x ULN).
Infection: Influenza.
Neuromuscular & skeletal: Arthralgia, pain in extremity.
Respiratory: Sinusitis, upper respiratory tract infection.
Rare but important or life-threatening: Abdominal pain, anaphylaxis, angioedema, cholecystitis, cholelithiasis, depression, dizziness, headache, hepatitis, hypersensitivity reaction, myalgia, nausea, pancreatitis, paresthesia, rhabdomyolysis, skin rash, thrombocytopenia, urticaria.
Bezafibrate: Bezafibrate may enhance the adverse/toxic effect of ezetimibe. Avoid combination.
Bile acid sequestrants: Bile acid sequestrants may decrease the absorption of ezetimibe. Ezetimibe should be administered at least 2 hours before or at least 4 hours after administration of the bile acid sequestrant.
Cyclosporine (systemic): Ezetimibe may increase the serum concentration of cyclosporine (systemic). Cyclosporine (systemic) may increase the serum concentration of ezetimibe. Patient receiving both drugs should be carefully monitored.
Fenofibrate and derivatives: Fenofibrate and derivatives increased ezetimibe concentrations and may enhance the adverse/toxic effect of ezetimibe. Specially, the risk of myopathy and cholelithiasis may be increased. When used in combination with fenofibrate, monitor liver function tests and signs and symptoms of cholelithiasis.
Gemfibrozil: Gemfibrozil may enhance the adverse/toxic effect of ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Gemfibrozil may increase the serum concentration of ezetimibe. Avoid concomitant use of ezetimibe with gemfibrozil.
Antacids: Concomitant use of ezetimibe and an aluminum and magnesium hydroxide containing antacids decrease AUC and peak plasma concentration of total ezetimibe.
Hydroxymethylglutaryl-Coenzyme A (HMG-CoA) reductase inhibitors (statins): Concomitant use of ezetimibe and statins (atorvastatin, fluvastatin, lovastatin, pravastatin or rosuvastatin) decrease AUC of total ezetimibe and increase peak plasma concentration of total ezetimibe.
Warfarin: Increase international normalized ratio (INR) with concomitant use of ezetimibe and warfarin. If ezetimibe is initiated in a patient receiving warfarin, the INR should be monitored.
C10AX09 - ezetimibe ; Belongs to the class of other lipid modifying agents.
Mibeaz tab 10 mg
3 × 10's
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