Sezstad

Sezstad

ezetimibe

Nhà sản xuất:

Stellapharm J.V.

Nhà phân phối:

Khuong Duy
Thông tin kê toa chi tiết tiếng Anh
Contents
Ezetimibe.
Description
Excipients/Inactive Ingredients: Lactose monohydrate, sodium lauryl sulphate, povidone K30, croscarmellose sodium, magnesium stearate.
Action
Pharmacotherapeutic Group: Other lipid modifying agents. ATC Code: C10AX09.
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.
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 >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 hrs.
Indications/Uses
Primary Hypercholesterolaemia: Monotherapy: As adjunctive therapy to diet for use in patients with primary (heterozygous familial and nonfamilial) hypercholesterolaemia in whom a statin is considered inappropriate or is not tolerated.
Co-Administered with an HMG-CoA Reductase Inhibitor (Statin): As adjunctive therapy to diet for use in patients with primary (heterozygous familial and nonfamilial) hypercholesterolaemia who are not appropriately controlled with a statin alone.
Homozygous Familial Hypercholesterolaemia (HoFH): Co-Administered with a Statin: As adjunctive therapy to diet for use in patients with HoFH.
Homozygous Sitosterolaemia (Phytosterolaemia): As adjunctive therapy to diet for use in patients with homozygous familial sitosterolaemia.
Dosage/Direction for Use
The patient should be on an appropriate lipid-lowering diet and should continue on this diet during treatment.
Concomitant Lipid-Lowering Therapy: Ezetimibe may be administered with a statin (in patients with primary hyperlipidemia) or with fenofibrate (in patients with mixed hyperlipidemia) for incremental effect.
The daily dose of ezetimibe may be taken at the same time as the statin or fenofibrate, according to the dosing recommendations for the respective medications.
Co-Administration with Bile Acid Sequestrants: Dosing of ezetimibe should occur either at least 2 hrs before or 4 hrs after administration of a bile acid sequestrant.
Recommended Dose: 1 tab daily.
Children and Adolescents ≥10 years: No dosage adjustment is required.
Children <10 years: Ezetimibe is not recommended for use in children <10 years due to insufficient data on safety and efficacy.
Hepatic or Renal Impairment: No dosage adjustment is necessary in patients with mild hepatic impairment or renal impairment.
Elderly: No dosage adjustment is required for elderly patients.
Administration: Take orally at any time of the day, with or without food.
Overdosage
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.
Contraindications
Hypersensitivity to ezetimibe or to any of the excipients of Sezstad 10.
Therapy with ezetimibe co-administered with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in serum transaminases, and in pregnancy and lactation.
Special Precautions
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. If myopathy is suspected based on muscle symptoms or is confirmed by a creatine phosphokinase level >10 times the ULN, ezetimibe, any statin, and any of these other agents that patient is taking concomitantly should be immediately discontinued.
Excipient: Sezstad 10 contains lactose. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Effects on the Ability to Drive or Operate Machinery: 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.
Use in Pregnancy & Lactation: 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, embryofetal development, birth or postnatal development.
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.
Use In Pregnancy & Lactation
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, embryofetal development, birth or postnatal development.
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.
Adverse Reactions
Common (1/100 ≤ ADR < 1/10): Headache, abdominal pain, diarrhea, rash, angioedema, fatigue, chest pain and arthralgia.
Rare (1/10,000 ≤ ADR < 1/1000): Raised liver enzymes or hepatitis, pancreatitis, thrombocytopenia, cholelithiasis and cholecystitis.
Drug Interactions
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.
Ciclosporin: Ciclosporin 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 INR should be appropriately monitored.
Storage
Store in well closed container, in a dry place. Do not store above 30°C.
Shelf-Life: 24 months.
ATC Classification
C10AX09 - ezetimibe ; Belongs to the class of other lipid modifying agents.
Presentation/Packing
Tab (white to off-white, oval-shaped, biconvex and plain on both sides) 10 mg x 1 x 10's, 3 x 10's, 6 x 10's.
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in