Each tablet contains ezetimibe 10 mg.
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, 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. Ezetimibe does not appear to inhibit hepatic cholesterol synthesis or increase bile acid excretion.
Pharmacokinetics: Ezetimibe is rapidly absorbed when given orally and undergoes extensive conjugation in the small intestine and liver to an active glucuronide metabolite. Both ezetimibe and the glucuronide are more than 90% bound to plasma proteins. Ezetimibe is excreted primarily in the faeces via bile and undergoes enterohepatic recycling. After an oral dose, about 78% is excreted in the faeces, mainly as ezetimibe, and about 11% is excreted in the urine, mainly as the glucuronide. The elimination half-life for both ezetimibe and the glucuronide is about 22 hours.
Primary hypercholesterolaemia: Monotherapy is indicated as adjunctive therapy to diet for use in patients with primary (heterozygous familial and non-familial) hypercholesterolaemia in whom a statin is considered inappropriate or is not tolerated.
Co-administered with an HMG-CoA reductase inhibitor (statin) is indicated as adjunctive therapy to diet for use in patients with primary (heterozygous familial and non-familial) hypercholesterolaemia who are not appropriately controlled with a statin alone.
Homozygous familial hypercholesterolaemia (HoFH): Co-administered with a statin is indicated as adjunctive therapy to diet for use in patients with HoFH.
Homozygous sitosterolaemia (phytosterolaemia): Ezetimibe is indicated as adjunctive therapy to diet for use in patients with homozygous familial sitosterolaemia.
Administration: Sezstad 10 is administered orally at any time of the day, with or without food.
The patient should be on an appropriate lipid-lowering diet and should continue on this diet during treatment.
Concomitant lipid-lowering therapy: When Sezstad 10 is added to a statin, either the indicated usual initial dose of that particular statin or the already established higher statin dose should be continued. In this setting, the dosage instructions for that particular statin should be consulted.
Co-administration with bile acid sequestrants: Dosing of ezetimibe should occur either at least 2 hours before or 4 hours after administration of a bile acid sequestrant.
Dosage: The recommended dose is one tablet daily.
Children and adolescents ≥10 years: No dosage adjustment is required.
Children <10 years: Ezetimibe is not recommended for use in children below age 10 due to insufficient data on safety and efficacy.
Use in the elderly: No dosage adjustment is required for elderly patients.
Patients with hepatic impairment or renal impairment: No dosage adjustment is necessary in patients with mild hepatic impairment or renal impairment.
Symptoms: A few cases of overdosage with ezetimibe have been reported; most have not been associated with adverse experiences. Reported adverse experiences have not been serious.
Treatment: In the event of an overdose, symptomatic and supportive measures should be employed.
Hypersensitivity to the active substance or any of the excipients.
Therapy with ezetimibe co-administered with a statin is contraindicated during pregnancy and lactation.
Ezetimibe co-administered with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in serum transaminases.
Liver enzymes: In controlled co-administration trials in patients receiving ezetimibe with a statin, consecutive transaminase elevations (≥3 the upper limit of normal (ULN)) have been observed. When ezetimibe is co-administered with a statin, liver function test should be performed at initiation of therapy and according to the recommendation of the statin.
Skeletal muscle: In post-marketing experience with ezetimibe, cases of myopathy and rhabdomyolysis have been reported. Most patients who developed rhabdomyolysis were taking a statin concomitantly with ezetimibe. All patients starting therapy with ezetimibe should be advised of the risk of myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness.
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.
Excipients: Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on ability to drive and use machines: No studies on the effects on the ability to drive and use machines have been performed. However, when driving vehicles or operating machines, it should be taken into account that dizziness has been reported.
Ezetimibe co-administered with a statin is contraindicated during pregnancy and lactation.
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, embryo fetal development, birth or postnatal development.
Lactation: 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.
Myalgia has occurred in patients taking ezetimibe either alone or when added to a statin.
Common: Headache, abdominal pain, diarrhea, rash, angioedema, fatigue, chest pain, and arthralgia.
Rare: Raised liver enzymes or hepatitis, pancreatitis, thrombocytopenia, cholelithiasis, and cholecystitis.
Cholestyramine: Concomitant cholestyramine administration decreased the mean area under the curve (AUC) of total ezetimibe (ezetimibe + ezetimibe glucuronide) approximately 55%. The incremental low-density lipoprotein cholesterol (LDL-C) reduction due to adding ezetimibe to cholestyramine may be lessened by this interaction.
Fibrates: In patients receiving fenofibrate and ezetimibe, physicians should be aware of the possible risk of cholelithiasis and gallbladder disease. If cholelithiasis is suspected in a patient receiving ezetimibe and fenofibrate, gallbladder investigations are indicated and this therapy should be discontinued.
Statins: No clinically significant pharmacokinetic interactions were seen when ezetimibe was co-administered with atorvastatin, simvastatin, pravastatin, lovastatin, fluvastatin or rosuvastatin.
Cyclosporine: Cyclosporine has been reported to increase the plasma concentration of ezetimibe and patients receiving both drugs should be carefully monitored; the effect may be greater in patients with severe renal impairment.
Anticoagulants: Concomitant administration of ezetimibe (10 mg once daily) had no significant effect on bioavailability of warfarin and prothrombin time in a study of twelve healthy adult males. However, there have been post-marketing reports of increased International Normalised Ratio (INR) in patients who had ezetimibe added to warfarin or fluindione. If ezetimibe is added to warfarin, another coumarin anticoagulant, or fluindione, the International Normalised Ratio (INR) should be appropriately monitored.
Store in a well-closed container, in a dry place. Do not store above 30°C.
C10AX09 - ezetimibe ; Belongs to the class of other lipid modifying agents.
Sezstad 10 tab 10 mg
3 × 10's
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