Cardiosim

Cardiosim

simvastatin

Manufacturer:

Cathay YSS

Distributor:

Cathay YSS
Full Prescribing Info
Contents
Simvastatin.
Description
Each Simvastatin (Cardiosim) 20 mg Film Coated Tablet contains 20 mg simvastatin.
Each Simvastatin (Cardiosim) 40 mg Film Coated Tablet contains 40 mg simvastatin.
Action
Pharmacology: Pharmacokinetics: Simvastatin is a hypolipidemic agent; it is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase). This enzyme catalyzes the conversion of HMG-CoA to mevalonate, which is an early and rate-limiting step in the biosynthesis of cholesterol.
HMG-CoA reductase inhibitors (sometimes called "statins") reduce total cholesterol, low density lipoprotein (LDL)-cholesterol, and very-low-density cholesterol concentrations in plasma. They also tend to reduce triglycerides and to increase high-density lipoprotein (HDL)-cholesterol concentrations. They are considered to exert their hypocholesterolemic action by stimulating an increase in LDL-receptors on hepatocyte membranes thereby increasing the clearance of LDL from the circulation.
Simvastatin, an inactive lactone, is absorbed from the gastro-intestinal tract and is readily hydrolyzed to its active β-hydroxyacid form. Other active metabolites have been detected and a number of inactive metabolites are also formed. It undergoes extensive first-pass metabolism in the liver, its primary site of action. Less than 5% of the oral dose has been reported to reach the circulation as active metabolites. Both simvastatin and its β-hydroxyacid metabolites are about 95% bound to plasma proteins. It is mainly excreted in the feces via bile as metabolites. About 10 to 15% is recovered in the urine, mainly in inactive forms and 60% in the feces.
The major active metabolites of simvastatin present in human plasma are the β-hydroxyacid of simvastatin and its 6'-hydroxyl, 6'-hydroxymethyl, and 6'-exomethylene derivatives. Peak plasma concentrations of both active and total inhibitors were attained within 1.3 to 2.4 hours postdose. The half-life of the active metabolite is 1.9 hours.
Indications/Uses
Simvastatin (Cardiosim) is indicated to reduce LDL-cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in the treatment of hyperlipidaemias, including hypercholesterolaemias and combined (mixed) hyperlipidaemia (Type IIa or IIb) hyperlipoproteinaemias.
Simvastatin (Cardiosim) is also indicated as an adjunct therapy in patients with homozygous familial hypercholesterolaemia who have some LDL-receptor function.
Simvastatin (Cardiosim) is also given prophylactically to hypercholesterolaemic patients with ischaemic heart disease.
Dosage/Direction for Use
Simvastatin (Cardiosim) is given by mouth in an initial dose of 5 mg to 10 mg in the evening.
ISCHAEMIC HEART DISEASE: Simvastatin (Cardiosim) is given in an initial dose of 20 mg. The dose may be adjusted at intervals of not less than 4 weeks up to a maximum of 80 mg once daily in the evening.
HOMOZYGOUS FAMILIAL HYPERCHOLESTEROLAEMIA: Patients may be treated with Simvastatin (Cardiosim) 40 mg once daily in the evening, or 80 mg daily in three divided doses of 20 mg, 20 mg, and an evening dose of 40 mg.
A maximum of 10 mg daily is recommended in those taking ciclosporin, fibric acid derivatives, or nicotinic acid and the risk of myopathy must be considered.
Or as prescribed by the physician.
Contraindications
Hypersensitivity to any component of this medication.
Active liver disease or unexplained persistent elevations of serum transaminases.
Pregnancy and lactation.
Special Precautions
Simvastatin should not be given to patients with acute liver disease or unexplained persistently raised serum-aminotransferase concentrations.
It should be avoided during pregnancy since there is a possibility that it could interfere with fetal sterol synthesis.
It should be discontinued if marked or persistent increases in serum-aminotransferase or creatine phosphokinase concentrations occur.
It should be used with caution in patients with severe renal impairment.
Use In Pregnancy & Lactation
Contraindicated in pregnancy and lactation.
Adverse Reactions
The common adverse effects of therapy with simvastatin and other statins are gastrointestinal disturbances. Other adverse effects reported are headache, skin rashes, dizziness, blurred vision, insomnia, and dysgeusia.
May occur reversible increases in serum-aminotransferase concentrations and liver function should be assessed before treatment is initiated then monitored periodically until one year after the last elevation in dose.
Hepatitis, pancreatitis, and a hypersensitivity syndrome whose features have included angioedema has been reported.
Myopathy, characterized by myalgia and muscle weakness and associated with increased creatinine phosphokinase concentrations, has been reported, especially in patients taking simvastatin concurrently with ciclosporin, fibric acid derivatives, or nicotinic acid. Rarely, rhabdomyolysis with acute renal failure may develop.
Drug Interactions
Drugs given concurrently with statins may increase risk of myopathy.
Concomitant administration of drugs that inhibit the cytochrome P450 isoenzyme CYP3A4, such as ciclosporin, itraconazole, ketoconazole, erythromycin, clarithromycin, HIV-protease inhibitors, and nefazodone, might produce high plasma levels of simvastatin, thus increasing the risk of myopathy.
Drugs that alone can cause myopathy, such as fibric acid derivatives or nicotinic acid, can increase the risk of this reaction when given with simvastatin.
Bleeding and increases in prothrombin time have been reported in patients taking simvastatin with coumarin anticoagulants.
Raised concentrations of simvastatin have occurred in patients given with mibefradil.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
C10AA01 - simvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Presentation/Packing
FC tab 20 mg x 30's. 40 mg x 30's.
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