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LOCHOL composed of simvastatin, an inactive lactone, which is hydrolyzed to the corresponding β-hydroxy acid form which inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Inhibition of HMG-CoA reductase prevents conversion of HMG-CoA to mevalonate, an early step in cholesterol biosynthesis.
Simvastatin is effective in reducing total plasma cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), very low-density lipoprotein cholesterol (VLDL-C), plasma triglyceride (TG) and increases high-density lipoprotein cholesterol (HDL-C) in heterozygous familial/non-familial hypercholesterolemia and in mixed hyperlipidemia when elevated cholesterol was cause for concern and diet alone has been insufficient.
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