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Atorvastatin
Systematic (IUPAC) name
[R-(R, R)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5- (1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H- pyrrole-1-heptanoic acid
Identifiers
CAS number	134523-00-5
ATC code	C10AA05
PubChem	60823
DrugBank	APRD00055
Chemical data
Formula	C₃₃H₃₄FN₂O₅
Mol. weight	558.64
Pharmacokinetic data
Bioavailability	12%
Metabolism	Liver
Half life	14 hours
Excretion	Bile
Therapeutic considerations
Pregnancy cat.	D(AU) X(US)
Legal status	S4(AU) POM(UK) ℞-only(US)
Routes	oral

Atorvastatin (INN) (IPA: [əˈtɔvəˌstætn]) is a member of the drug class known as statins, used for lowering cholesterol and thereby reducing 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.

With 2005 sales of US$12.2 billion under the brand name Lipitor, it is the largest selling drug in the world.

1 Pharmacology
2 Clinical use
3 References
4 External links
5 Further reading

Pharmacology

Main article: Statin

As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis. Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases the LDL uptake by the hepatocytes, decreasing the amount of LDL in the blood.

Clinical use

Indications

Atorvastatin is indicated as an adjunct to diet for the treatment of dyslipidaemia, specifically hypercholesterolaemia. It has also been used in the treatment of combined hyperlipidemia.^[1]

Available forms

Atorvastatin calcium tablets are currently marketed by Pfizer under the trade name Lipitor, in tablets (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated. In some countries it may also be known as: Sortis, Torvast, Totalip, Tulip, Xarator or Liprimar.

Adverse effects

For additional information see: Statin#Safety

Common adverse drug reactions (≥1% of patients) associated with atorvastatin therapy include: myalgia, mild transient gastrointestinal symptoms, elevated hepatic transaminase concentrations, headache, insomnia, and/or dizziness.^[1]

Myopathy and rhabdomyolysis occur in <0.1% of patients. Risk is increased in patients with renal impairment, serious concurrent illness; and/or concomitant use of drugs which inhibit CYP3A4.^[1]

References

^ ^a ^b ^c Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3

External links

Lipitor.com – manufacturer's site
MedlinePlus Drug information: Atorvastatin (Systemic) – information from USP DI Advice for the Patient

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Drugs & Medication

Atorvastatin (Lipitor)

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