Atorvastatin

Clinical data
Pregnancy category	X (USA) D (Aust)
Routes of administration	oral
ATC code	C10AA05 (WHO)
Legal status
Legal status	Schedule 4 (Aust)
Pharmacokinetic data
Bioavailability	12%
Metabolism	Liver
Elimination half-life	14 hours
Excretion	Bile
Identifiers
IUPAC name [R-(R*, R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5- (1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H- pyrrole-1-heptanoic acid
CAS Number	134523-00-5
PubChem CID	60823
DrugBank	APRD00055
CompTox Dashboard (EPA)	DTXSID8029868
ECHA InfoCard	100.125.464
Chemical and physical data
Formula	(C33H34FN2O5)2Ca•3H2O
Molar mass	1209.42

In medicine and pharmacology, atorvastatin is a member of the drug class of statins, used for lowering cholesterol and thereby preventing cardiovascular disease. Atorvastatin inhibits a rate-determining enzyme located in hepatic tissue used in cholesterol synthesis, which lowers the amount of cholesterol produced. This also has the effect of lowering the total amount of LDL cholesterol.

Unlike simvastatin and pravastatin, atorvastatin is a completely synthetic compound.

Atorvastatin is currently marketed by the pharmaceutical company Pfizer as Lipitor®. With 2004 sales of US$10.9 billion, it is the best selling drug in the world.

Available forms

Atorvastatin is available as Lipitor in tablet form (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated.

Mechanism of action

Atorvastatin is a competitive inhibitor of HMG-CoA reductase. This enzyme catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, which is the rate limiting step in hepatic cholesterol synthesis.

Because cholesterol synthesis decreases, hepatic cells increase the number of LDL receptors on the surface of the cells, which increase the amount of LDL uptake by the hepatic cells, and decreases the amount of LDL in the blood.