| Item |
Information |
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Drug Groups
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approved |
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Description
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A derivative of lovastatin and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (hydroxymethylglutaryl COA reductases), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL receptors, it increases breakdown of LDL cholesterol. [PubChem] |
| Indication |
For the treatment of hypercholesterolemia. |
| Pharmacology |
Simvastatin, the methylated form of lovastatin, is an oral antilipemic agent which inhibits HMG-CoA reductase. simvastatin is used in the treatment of primary hypercholesterolemia and is effective in reducing total and LDL-cholesterol as well as plasma triglycerides and apolipoprotein B. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Hepatic, simvastatin is a substrate for CYP3A4. |
| Absorption |
Absorption of simvastatin, estimated relative to an intravenous reference dose, in each of two animal species tested, averaged about 85% of an oral dose. In animal studies, after oral dosing, simvastatin achieved substantially higher concentrations in the liver than in non-target tissues. |
| Half Life |
3 hours |
| Protein Binding |
Both simvastatin and its b-hydroxyacid metabolite are highly bound (approximately 95%) to human plasma proteins. |
| Elimination |
Following an oral dose of 14C-labeled simvastatin in man, 13% of the dose was excreted in urine and 60% in feces. |
| References |
| • |
Wolozin B, Wang SW, Li NC, Lee A, Lee TA, Kazis LE: Simvastatin is associated with a reduced incidence of dementia and Parkinson's disease. BMC Med. 2007 Jul 19;5:20.
[Pubmed]
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| External Links |
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