SIMVASTIN 10 Tablet

In the treatment of Type 2a and 2b

Dosage

Initial dose: 5-10mg in the evening. 20mg may be used in patients with ischaemic heart disease.

The dose may be adjusted at intervals of not less than 4 weeks up to a maximum of 80mg once daily in the evening or as directed by the physician.

Simvastatin should not be given to patients with acute liver disease or unexplained persistent raised serum- aminotransferase concentrations or to those with porphyria.

The side effects include gastro-intestinal disturbances, headache, skin rashes, dizziness, blurred vision, and insomnia.

Concomitant administration of drugs that inhibit the CYP450 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. Concurrent administration with coumaria anticoagulants causes bleeding and increases in prothrombin.

Raised concentration of simvastatin when administered with mibefradil.

It should be avoided during pregnancy since there is a possibility that it could interfere with fetal sterol synthesis and may cause congential abnormalities.

It is not known whether simvastatin is excreted in milk. Because the risk of adverse effects to the developing infants. Simvastatin should not be administered to nursing mother.

Simvastatin is less effective in patients with hypercholesterolemia. It should not be given to patients with acute liver disease or persistent raised serum-aminotransferase concentrations or to those with porphyria. It should be avoided during pregnancy and lactation. It should be used with caution in patients with severe renal impairment.

Simvastatin is a lipid regulating drug and is a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate determining enzyme for cholesterol synthesis. Simvastatin is absorbed from the gastrointestinal tract and is hydrolysed to its active β-hydroxyacid form. It undergoes extensive first-pass metabolism in the liver. Simvastatin and its metabolite is about 95% bound to plasma proteins. It is mainly excreted in the faeces via the bile as metabolites.