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Atorvastatin (Lipitor)

Drugs & Medication

Atorvastatin (Lipitor)

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Atorvastatin chemical structure
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.

Contents

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

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

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

External links

{{ChemicalSources

Further reading


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