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Simvastatin is synthesized from the glycolysis of Aspergillus terreus. It is an inactive lactone. Its active structure is an inhibitor of 3-hydroxy3-methylglutaryl-Coenzyme A(HMG-CoA) reductase. It was first sold in the UK in 1988. Clinical results have confirmed that it can reduce the levels of total cholesterol, low density lipoprotein cholesterol (LDL-C) and very low density lipoprotein white cholesterol (VLDL-C). In addition, it can also raise high-density lipoprotein cholesterol (HDL-C) and reduce triglycerides. It is suitable for primary hypercholesterolemia and low density lipoprotein cholesterol, while raising the cholesterol of high density fat eggs and reducing the level of high triglycerides in serum.
Simvastatin can catalyze the conversion of β-methyl-β-hydroxyglutarate coenzyme A(HMG-CoA) to β-methyl-P-α dihydroxyvalerate, which is a specific inhibitor of HMG-CoA reductase. After oral administration, it is hydrolyzed into the corresponding β-hydroxy acid, which is one of the effective and safe drugs in lipid-lowering drugs at present, and can reduce the content of serum total cholesterol, low density lipoprotein, very low density lipoprotein, triglyceride, and moderately increase high density lipoprotein cholesterol.
Indications
1. Hyperlipidemia :(1) In patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia, or mixed hypercholesterolemia, simvastatin may be used to lower elevated total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B, and triglycerides when dietary control and other non-pharmacological treatments are not ideal. And simvastatin increases HDL cholesterol, thereby reducing the LDL/HDL and total cholesterol/HDL ratios.
(2) In patients with homozygous familial hypercholesterolemia, simvastatin can be used to lower elevated total cholesterol, low-density lipoprotein cholesterol, and apolipoprotein B when dietary control and non-dietary therapies are not ideal.
2. Coronary heart disease: In patients with coronary heart disease, simvastatin can be used to:
(1) reduce the risk of death.
(2) Reduce the risk of coronary heart disease death and non-fatal myocardial infarction.
(3) Reduce the risk of stroke and transient cerebral ischemia.
(4) Reduce the risk of myocardial revascularization (coronary artery bypass grafting and percutaneous balloon coronary angioplasty).
(5) Delay the progression of atherosclerosis, including the occurrence of new lesions and total blockage.
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