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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

fever
general feeling of discomfort or illness
joint pain
loss of appetite
muscle aches and pain
runny nose
shivering
sore throat
sweating
trouble sleeping
unusual tiredness or weakness
Bladder pain
bloody or cloudy urine
cough producing mucus
dark-colored urine
difficult, burning, or painful urination
difficulty with breathing

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.

cyclosporine
desipramine
dexamethasone
haloperidol
loperamide
macrolide antibiotics (e.g., azithromycin, erythromycin, clarithromycin)
metronidazole
midazolam
ondansetron
phenobarbital
fluconazole
nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., diclofenac)
omeprazole
phenytoin
ranitidine
spironolactone
warfarin

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.