Forcad

Each film coated tablet contains: Simvastatin 10 mg, 20 mg, & 40 mg.

HMG-CoA Reductase Inhibitor.
Pharmacology: Simvastatin is a hypolipidaemic agent; it is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-determining enzyme for cholesterol synthesis. HMG-CoA reductase inhibitors (sometimes called "statins") reduce total cholesterol, low-density lipoprotein (LDL)-cholesterol, and very-low-density lipoprotein (VLDL)-cholesterol concentrations in plasma. They also tend to reduce triglyceride and to increase high-density lipoprotein (HDL)-cholesterol concentrations. They are considered to exert their hypocholesterolaemic action by stimulating an increase in LDL-receptors on hepatocyte membranes thereby increasing the clearance of LDL from the circulation.
Pharmacokinetics: Simvastatin is absorbed from the gastrointestinal tract and is hydrolyzed to its active β-hydroxyacid form. Other active metabolites have been detected and a number of inactive metabolites are also formed. Simvastatin 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 the bile as metabolites. About 10% to 15% is recovered in the urine, mainly in inactive forms. The half-life of the active metabolites is 1.9 hours.

Simvastatin is used to reduce LDL-cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in the treatment of hyperlipidaemias including hypercholesterolaemias, combined (mixed) hyperlipidaemia (type IIa or IIb hyperlipoproteinaemias), hypertriglyceridemia (type IV) and primary dysbetalipoproteinaemia (type III); as adjunct therapy in patients with homozygous familial hypercholesterolaemia who have some LDL-receptor function; used for cardiovascular risk reduction in patients with atherosclerotic cardiovascular disease or diabetes mellitus.

Primary hypercholesterolaemia, combine hyperlipidaemia, 10-20 mg daily at night, adjusted at intervals of at least 4 weeks; usual range 10-80 mg once daily at night. Homozygous familial hypercholesterolaemia, 40 mg daily at night or 80 mg daily in 3 divided doses (with largest dose at night). Prevention of cardiovascular events, initially 20-40 mg daily at night, adjusted at intervals of at least 4 weeks; maximum 80 mg once daily at night.
Note: Maximum 10 mg daily with concomitant ciclosporin, fibrate or lipid-lowering dose of nicotinic acid. Maximum 20 mg daily with concomitant amiodarone or verapamil. Maximum 40 mg daily with diltiazem.

For 10 and 20 mg film-coated tablet: This product contains FD & C yellow # 5 (Tartrazine) which may cause allergic reaction (including bronchial asthma) in certain susceptible person.

Simvastatin should not be given to patients with acute liver disease or unexplained persistent raised serum-aminotransferase concentrations. It should be avoided during pregnancy since there is a possibility that it could interfere with fetal sterol synthesis; there have been a few reports of congenital abnormalities associated with HMG-CoA reductase inhibitors. It should be discontinued if marked increase in serum-aminotransferase or creatine phosphokinase concentrations occur.

The most common adverse effects of therapy with simvastatin and other HMG-CoA reductase inhibitors are gastrointestinal disturbances. Other adverse effects reported include headache, skin rashes, dizziness, blurred vision and dysgeusia. Reversible increases in serum-aminotransferase concentrations may occur and liver function should be monitored. Myopathy, characterized by myalgia and muscle weakness and associated with increase creatine phosphokinase concentrations, has been reported, especially in patients taking simvastatin concurrently with immunosuppressive drugs, fibric acid derivatives or nicotinic acid. Rarely, rhabdomyolysis with acute renal failure may develop.

There is an increased risk of myopathy if certain drugs are given concurrently with statins. Concomitant administration of drug 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.

Store at temperatures not exceeding 30°C.

Dyslipidaemic Agents

C10AA01 - simvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

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