2023年6月5日 · Identify the mechanism of action of simvastatin. Review the indications for using simvastatin in lipid control. Explain the adverse event profile of simvastatin and how it compares with other statin medications.

Mechanism of action Simvastatin is a prodrug in which the 6-membered lactone ring of simvastatin is hydrolyzed in vivo to generate the beta,delta-dihydroxy acid, an active metabolite structurally similar to HMG-CoA (hydroxymethylglutaryl CoA).

2020年2月10日 · Mechanism of Action. Simvastatin is a methylated derivative of lovastatin that acts by competitively inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis.

2024年2月29日 · Mechanism of Action. Statins are a selective, competitive inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase, the enzyme responsible for converting HMG-CoA to mevalonate in the cholesterol synthesis pathway.

Statins’ primary mechanism of action is through the competitive, reversible inhibition of HMG-CoA reductase, the rate-limiting step in cholesterol biosynthesis. HMG-CoA reductase catalyses the conversion of HMG-CoA to l -mevalonate and coenzyme A via a four-electron reductive deacetylation (Figure 1).

The beneficial effects of statins are the result of their capacity to reduce cholesterol biosyntesis, mainly in the liver, where they are selectively distributed, as well as to the modulation of lipid metabolism, derived from their effect of inhibition upon HMG‐CoA reductase.

Simvastatin is a prodrug that is administered in its inactive lactone form and converted in the body to an active beta-hydroxy acid metabolite Endo and Hasumi (1989). The mechanism of action for simvastatin is competitive, reversible inhibition of HMG CoA reductase (EC 1.1.1.34), the rate-limiting enzyme in cholesterol synthesis Alberts (1980).

2024年10月17日 · 12.1 Mechanism of Action. Simvastatin is a prodrug and is hydrolyzed to its active β-hydroxyacid form, simvastatin acid, after administration. Simvastatin acid and its metabolites are inhibitors of HMG-CoA reductase, the rate-limiting enzyme that converts HMG-CoA to mevalonate, a precursor of cholesterol.

2023年6月5日 · This activity outlines the indications, mechanism of action, methods of administration, significant adverse effects, contraindications, and monitoring, of simvastatin, so providers can direct patient therapy in treating hyperlipidemia …

Some of the statins are obtained after fungal fermentation: lovastatin (Mevacor), pravastatin (Lipostat, Pravachol) and simvastatin (Zocor), others by synthesis: fluvastatin (Lescol), atorvastatin (Sortis, Lipitor), and cerivastatin (Baycol, Lipobay).