Atorvastatin Calcium CAS No. 134523-03-8
CAS No.134523-03-8
Chemical Name:Atorvastatin calcium
SynonymsTahor;ci-981;YM-548;Sortis;LIPITOR;pd134298-38a;Atorvastatin c;ATORVASTATIN CA;Atorvastatin 3S,5S-Atorvastatin
CBNumber:CB4260130
Molecular Formula:C66H68CaF2N4O10
Formula Weight:1155.36
Atorvastatin calcium Properties
Melting point:176-178°C
storage temp. Store at +4°C
solubility DMSO: ≥10mg/mL
Indications and Usage
Atorvastatin is a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Atorvastatin can lower the serum low-density lipoprotein cholesterol of some homozygous familial hypercholesterolemia patients, which is a population that rarely responds to other lipid-lowering drugs. It is clinically used to treat primary hypercholesterolemia, mixed hyperlipidemia, and hypertriglyceridemia, homozygous familial hypercholesterolemia, and it is used to prevent and treat atherosclerosis. Atorvastatin can also regulate blood lipids and combat atherosclerosis.
Mechanisms of Action
Atorvastatin mainly inhibits HMGCoA reductase synthesis to inhibit cholesterol synthesis, reducing the amount of serum low-density lipoprotein cholesterol and triglycerides. Atorvastatin inhibits cells from synthesizing cholesterol, thus interrupting lipoprotein production, which causes serum total cholesterol levels to decrease, effectively lowers serum triglyceride levels, and increases serum high-density lipoprotein cholesterol levels.
Pharmacokinetics
Rapidly absorbed after oral intake, reaches maximum blood concentration in 1-2 hours, and is not affected when taken with food. Its absolute bioavailability is about 12%, and its usage in inhibiting HMG-CoA reductase is about 30%. This low percentage is due to cleansing by gastrointestinal mucosa and the first round of metabolism in the liver. Its serum protein binding rate is above 98%. It is mainly metabolized in the liver by cytochrome P450 3A4, its metabolites are O-hydroxylate, its derivatives and various beta oxidants, and these o-hydroxylates are active against o-hydroxylate metabolites. This drug and its metabolites are metabolized in and/or out of the liver and excreted mainly in bile, and small amounts (less than 2% of dosage amount) is excreted through urine. This drug's average serum clearing half-life is 14 hours, and its active metabolites' half-life is 20-30 hours.
Chemical Properties
White Crystalline Powder
Uses
A selective, competitive HMG-CoA reductase inhibitor. The only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia