Raw material Simvastatin

Simvastatin More Info

1. General Information

Product Name: Simvastatin

Common Names: Simvastatin, Simvastatin Hydrochloride (when in salt form), also known as Xinfatatin in Chinese markets.

Chemical Name: (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthyl 2,2-dimethylbutyrate.

Molecular Formula: C25H38O5

Molecular Weight: Approximately 418.57 g/mol

CAS Number: 79902-63-9

Physical Appearance: White or nearly white crystalline powder. When formulated as tablets, they are typically white or nearly white, round, biconvex with a film coating.

Solubility: Highly soluble in ethanol, methanol, and acetonitrile; slightly soluble in propylene glycol; practically insoluble in water.

Purity: Typically >99% for pharmaceutical-grade material.

2. Pharmacological Classification

Drug Class: HMG-CoA Reductase Inhibitor (Statin)

Mechanism of Action: Simvastatin is a prodrug that is hydrolyzed in vivo to its active β-hydroxy acid form. It competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to reduced intracellular cholesterol levels and upregulation of LDL receptors, thereby increasing the clearance of LDL cholesterol from the bloodstream.

3. Indications (Therapeutic Uses)

Simvastatin is primarily used for:

Hypercholesterolemia: Primary hypercholesterolemia, mixed hyperlipidemia, and heterozygous familial hypercholesterolemia.

Cardiovascular Risk Reduction: To reduce the risk of cardiovascular events (such as heart attack and stroke) in patients with coronary heart disease (CHD), diabetes, or other risk factors.

Atherosclerosis: To slow the progression of atherosclerosis.

4. Dosage Forms and Strengths

Simvastatin is available in various dosage forms, including:

Oral Tablets: Common strengths include 5 mg, 10 mg, 20 mg, 40 mg, and 80 mg.

Pharmaceutical Grade Powder: For research and formulation purposes, typically supplied in bulk (e.g., 250 mg, 1 g).

5. Storage Conditions

General Storage: Should be stored in a tightly sealed container, in a dry place, protected from light and moisture.

Temperature: Usually stable at room temperature (20-25°C); some formulations recommend storage at 2-8°C for stability.

6. Safety and Contraindications

Contraindications: Active liver disease, persistent elevation of liver transaminases, pregnancy, and lactation. It is also contraindicated in patients with known hypersensitivity to any component of the formulation.

Warnings: Patients should be monitored for signs of myopathy or rhabdomyolysis, especially when used in combination with certain other medications (e.g., some antibiotics, antifungals, or other lipid-lowering agents). Regular monitoring of liver function tests is recommended.

Drug Interactions: Notable interactions include those with certain antibiotics (e.g., erythromycin, clarithromycin), antifungal agents (e.g., itraconazole, ketoconazole), protease inhibitors, and grapefruit juice, which can increase the risk of muscle toxicity.