Simvastatin

Also known as: Synvinolin

Drug #659

Simvastatin is antihyperlipidic agent. Simvastatin is structural analog of HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme). Like other agents, it inhibits the enzyme hydroxymethylglutaryl-CoA (HMG-CoA) reductase. It has an extremely high affinity for this enzyme and was considered the most potent agent of the HMG-CoA class until atorvastatin was approved. Simvastatin is inactive lactone prodrug and hydrolyzed in the gastrointestinal tract to the active ß hydroxy derivative. It was approved by the FDA in December 1991. It decreases total cholesterol, LDL cholesterol, triglycerides, and apolipoprotein B, while increasing HDL.

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Primary Characteristics

Simvastatin is also known as Synvinolin.

It is of Synthetic origin and belongs to Lactone.

It belongs to HMGCoA reductase inhibitor pharmacological group on the basis of mechanism of action and also classified in Antilipemic Agent pharmacological group.

Molecular Weight: 418.6 · Solubility in Water: almost Insoluble · Solubility in Alcohol: freely soluble · Non-proprietary name: Simvastatin.

Pharmacokinetics

Absorption: Simvastatin has an oral bioavailability is 42.5% (±42.5%), pre-systemic (first-pass) metabolism accounts for 83% (±7%).

Distribution: Simvastatin has a volume of distribution is 98%. plasma protein binding is ~95%.

Elimination: it is metabolised via Hepatic, plasma half-life is 1.9 hr, renal excretion is 13%.

Indications

Simvastatin is primarily indicated in conditions like Atherosclerosis, Combined hyperlipidaemia, Coronary heart disease, Elevated plasma cholesterol levels, Homozygous familial hypercholesterolemia, Hypercholesterolaemia, Induction and maintenance of anaesthesia, Myocardial infarction prophylaxis, NSAID-associated gastric and duodenal ulcers (prophylaxis).

Contraindications

Simvastatin is contraindicated in conditions like Hyperlipidemia, Porphyria, Familial hypercholesterolaemia, Hypersensitivity, Acute liver disease.

Dosage

Simvastatin's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
42.5 mg	42.5 mg	Every 24h	PO	In evening, maintenance dose ranges 5-40 mg.
Paediatric Dosage (20kg)
0 – 0	—	—		Not recommended in this age group
Neonatal Dosage (3kg)
0 – 0	—	—		Not recommended in this age group

Drug Interactions

Unknown5 interactions

10 interactions

Major3 interactions

Moderate (Sequence important)1 interaction

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Simvastatin in overdosage may give rise to further complications which include Acute renal failure .

Simvastatin is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Constipation , Diarrhea, Elevation of liver enzymes, Fatigue, Flatulence, Headache, Hepatitis, Increased intracranial pressure, Muscle tenderness, Myopathy, Nausea, Pancreatitis, Rhabdomyolysis.

Warnings / Precautions

Use simvastatin with caution in patients with liver disease, severe infection, kidney disease, heart disease, hypothyroidism, history of alcoholism or any allergy, especially drug allergies. Limit alcohol intake as it may aggravate side effects. Simvastatin should not be used during pregnancy or lactation.

Interference in Pathology

Simvastatin may interfere in the diagnosis of Increased Alkaline Phosphatase Levels, Elevaions in creatinine phosphokinase levels.

Available Brands

Click on a strength to view available brands.

Single Ingredient

Tabs

10 mg 20 mg 40 mg 80 mg

Multi-Ingredient Combinations

Tabs

10 mg 20 mg 40 mg 5 mg 80 mg

Storage Conditions

Simvastatin should be stored Tab.

Drug Classification

1.12.6 — Lipid-regulating drugs /Anti-atheromas