Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: iPharma (Pty) Ltd., 124 Elevation Avenue, Randjesfontein, MIDRAND, 1683, SOUTH AFRICA
A 7.5 Serum-cholesterol reducers
ATC-Code: C10AA01
Simvastatin is a cholesterol-lowering agent derived synthetically from a fermentation product of Aspergillus terreus. After oral ingestion simvastatin, an inactive lactone, is hydrolysed to the corresponding beta-hydroxyacid, the active form. This is a principal metabolite and an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyses the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in the biosynthesis of cholesterol. As a result, simvastatin, reduces total plasma cholesterol, low-density lipoprotein (LDL) and very lowdensity lipoprotein (VLDL)-cholesterol concentrations. Apolipoprotein B is also decreased. In addition, simvastatin moderately increases high-density lipoprotein (HDL)-cholesterol and variably reduces plasma triglycerides.
There is extensive first-pass extraction by the liver, with oral bioavailability of the active medicine or metabolites being less than 5%. More than 95% of simvastatin and its beta-hydroxy metabolite are bound to plasma proteins. Following an oral dose, peak plasma concentrations of simvastatin are seen in 1 to 2 hours. Simvastatin is excreted primarily via the liver, and less than 13% of its metabolites are excreted in the urine.
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