Hypocholesterolemic

Simvastatin 20 mg, n30

International Nonproprietary Name (INN): Simvastatin

Pharmaceutic group: Hypocholesterolemic

Presentation:

  • Film-coated tablets 10 mg n30;
  • Film-coated tablets 20 mg n30.

Available with prescription

Question?

THERE ARE CONTRAINDICATIONS. CAREFULLY READ THE INSTRUCTIONS FOR USE, OR OBTAIN A SPECIALIST ADVICE

Simvastatin is a hypolipidemic drug used to control elevated cholesterol, or hypercholesterolemia. It is a member of the statin class of pharmaceuticals.

Simvastatin is a synthetic derivate of a fermentation product of Aspergillus terreus.

MEDICAL USES. The primary uses of simvastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels sufficiently.

Since its introduction, there has been a large debate surrounding the price for lipid-lowering treatment and its benefits with regard to atherosclerosis. Although this has affected the other statins, simvastatin was the first statin drug to be used extensively in clinical practice.

A number of large epidemiological studies were conducted to discover which patients would benefit most from statin drugs; most studies involve simvastatin as the study drug. The most influential studies were the Scandinavian Simvastatin Survival Study (4S) and the Heart protection study (HPS).

It has been suggested that patients with one or more risk factors for cardiovascular disease (such as diabetes mellitus, hypertension or a positive family history) can benefit from statins even if they do not have substantially elevated cholesterol levels.

Simvastatin was introduced in the late 1980s, and in many countries it is now available as a generic preparation. This has led to a decrease of the price of most statin drugs, and a reappraisal of the health economics of preventive statin treatment. In the UK in 2008 the typical per patient cost to the NHS of simvastatin was approx £1.50 per month.

DOSE. Simvastatin is a powerful lipid-lowering drug that can decrease low density lipoprotein (LDL) levels by up to 50%. It is used in doses of 5 mg up to 80 mg. Higher doses (160 mg) have been found to be too toxic, while giving only minimal benefit in terms of lipid lowering.

In secondary prevention, 80 mg per day reduced major cardiovascular events by an absolute rate of 1.2% compared to 20 mg per day in a randomized controlled trial.

The drug is in the form of an inactive lactone that is hydrolyzed after ingestion to produce the active agent. It is a white, nonhygroscopic, crystalline powder that is practically insoluble in water, and freely soluble in chloroform, methanol and ethanol.

Grapefruit contains furanocoumarins, notably bergamottin and 6',7'-dihydroxybergamottin, which inhibit the intestinal cytochrome P450 3A4 isoform. This in turn slows metabolization of simvastatin and a large number of other drugs resulting in higher plasma levels of the drug. Due to the risk of toxicity patients taking simvastatin should avoid intake of grapefruit and grapefruit-containing products.