preview

Simvastatin

Decent Essays

Simvastatin
Introduction
Simvastatin is used to lower the cholesterol level in the blood such as the low-density lipoprotein (LDL) and triglycerides and to raise the high-density lipoprotein (HDL), It decreases the risk of heart diseases and helps to prevent the heart attacks and strokes by reducing the amount of cholesterol that is made by the liver (Raleys.com, 2015). Chemical structure and functional groups
Simvastatin is one of the statins derivatives that is synthesised from a fermentation product of Aspergillus terreus. The simvastatin is an inactive lactone which is hydrolysed to the β-hydroxyacid form when it is taken orally. β-hydroxyacid form is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A(HMG-CoA) reductase. This enzyme …show more content…

The mode of action
Statins are competitive inhibitors HMG-CoA reductase, it has been considered as a first line for the treatment of hypercholesterolemia. Their mode of action is by mimicking the substrate molecule HMG-CoA and competes for binding to the HMGCR enzyme. It works by slowing the production rate of mevalonate which responsible for the production of cholesterol molecule.
Most of the cholesterol synthesis in the body is done by internal mechanism through the liver cells particularly at night during fasting; it is taken at night to inhibit the cholesterol production. It maximizes its inhibitory effect and the data shows a significant fall in the LDL and a fall in the total cholesterol level in the blood.
Simvastatin can have different pharmacological effects from other statins groups due to different ring structures and chemical side groups such as different affinity toward the receptors, different rates of connection to liver cells from non-liver cells, different bioavailability and biochemical metabolism and execration. All these factors affect its half-life which is short (Anon, 2015).
Statins are selective towards the hepatic cells because of their lipophilic properties. It passes through the membrane towards the cell

Get Access