Simvastatin; Uses, Dosage, Side Effects, Drug Interactions

Simvastatin; Uses, Dosage, Side Effects, Drug Interactions

Simvastatin is a lipid-lowering agent derived synthetically from a fermentation product of the fungus Aspergillus terreus. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells

Simvastatin is a lipid-lowering agent that is derived synthetically from the fermentation of Aspergillus terreus. It is used along with exercise, diet, and weight loss to decrease elevated lipid (fat) levels. It is also used to decrease the risk of heart problems in those at high risk. It is taken by mouth.. It is a 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 the breakdown of LDL cholesterol.

Mechanism of Action of Simvastatin

Simvastatin is a prodrug in which the 6-membered lactone ring of simvastatin is hydrolyzed in vivoto generate the beta,delta-dihydroxy acid, an active metabolite structurally similar to HMG-CoA (hydroxymethylglutaryl CoA). Once hydrolyzed, simvastatin competes with HMG-CoA for HMG-CoA reductase, a hepatic microsomal enzyme. Interference with the activity of this enzyme reduces the quantity of mevalonic acid, a precursor of cholesterol. Simvastatin is in a group of drugs called HMG CoA reductase inhibitors, or “statins.” It reduces levels of “bad” cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood while increasing levels of “good” cholesterol (high-density lipoprotein, or HDL).

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Indications of Simvastatin

  • High Cholesterol
  • High Cholesterol, Familial Homozygous
  • Hyperlipoproteinemia
  • High Cholesterol, Familial Heterozygous
  • Cardiovascular Risk Reduction
  • Hyperlipoproteinemia Type III, Elevated beta-VLDL IDL
  • Hyperlipoproteinemia Type IIa, Elevated LDL
  • Hyperlipoproteinemia Type IIb, Elevated LDL VLDL
  • Hyperlipoproteinemia Type IV, Elevated VLDL
  • Prevention of Cardiovascular Disease
  • Cardiovascular Events
  • Heterozygous Familial Hypercholesterolemia
  • High Blood Cholesterol Level
  • History of coronary heart disease cardiovascular event
  • History of stroke or another cerebrovascular disease cardiovascular event

Contra-Indications of Simvastatin

  • Alcoholism
  • Uncontrolled epilepsy
  • Hemorrhage in the brain
  • Severely low blood pressure
  • Liver problems
  • Rhabdomyolysis
  • Recent operation
  • Loss of memory
  • High blood sugar
  • Abnormal liver function tests
  • Trauma
  • Pregnancy
  • A mother who is producing milk and breastfeeding
  • Muscle pain or tenderness with increase creatine kinase
  • Metabolic syndrome X
  • Muscle damage due to autoimmunity

Dosage of Simvastatin

Strengths: 5 mg; 10 mg; 20 mg; 40 mg; 80 mg; 20 mg/5 mL; 40 mg/5 mL

Cardiovascular Disease

  • Usual dosage range: 5 to 40 mg orally once a day in the evening

Patients with CHD or at high risk of CHD

  • Initial dose: 10 to 20 mg orally once a day in the evening started simultaneously with diet and exercise

Cardiovascular Risk Reduction

  • Usual dosage range: 5 to 40 mg orally once a day in the evening

Patients with CHD or at high risk of CHD

  • Initial dose: 10 to 20 mg orally once a day in the evening started simultaneously with diet and exercise

Pediatric Hypercholesterolemia

  • Less than 10 years: Not recommended

10 years or older

  • Initial dose: 10 mg orally once a day in the evening
  • Maintenance dose: 10 to 40 mg orally once a day in the evening
  • Maximum dose: 40 mg orally once a day in the evening
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Side Effects of Simvastatin

The most common

 Common

Less common

Drug Interactions of Simvastatin

Atorvastatin may interact with following drugs, supplements & may change the efficacy of drugs

Some products that may interact with this drug include: colchicine, gemfibrozil.

Pregnancy & Lactation of Simvastatin

FDA pregnancy category X

Pregnancy

Simvastatin should not be taken during pregnancy. It may cause harm to the unborn baby. If you become pregnant, stop taking this medication and contact your doctor immediately.

Lactation

It is not known if simvastatin passes into breast milk. If you breastfeeding-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

References

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