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Wikipedia - Argatroban

Argatroban
Systematic (IUPAC) name
(2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-
[[(3R)-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]
sulfonylamino]pentanoyl]-4-methyl-piperidine-2-
carboxylic acid
Identifiers
CAS number 74863-84-6
ATC code B01AE03
PubChem CID 440542
DrugBank APRD00105
ChemSpider 389444
Chemical data
Formula C23H36N6O5S 
Mol. mass 508.635 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 100% (intravenous)
Protein binding 54%
Metabolism hepatic
Half-life 39 and 51 minutes
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes intravenous
 YesY(what is this?)  (verify)

Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.[1] In 2000, argatroban was licensed by the Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). In 2002, it was approved for use during percutaneous coronary interventions in patients who have HIT or are at risk for developing it.

Argatroban is given intravenously and drug plasma concentrations reach steady state in 1-3 hours.[2] Argatroban is metabolized in the liver and has a half life of about 50 minutes. It is monitored by PTT. Because of its hepatic metabolism, it may be used in patients with renal dysfunction. (This is in contrast to lepirudin, a direct thrombin inhibitor that is primarily renally cleared).

[edit] Transitioning to warfarin in individuals with heparin induced thrombocytopenia

Argatroban is used as an anticoagulant in individuals with thrombosis and heparin induced thrombocytopenia. Often these individuals require long term anticoagulation. If warfarin is chosen as the long term anticoagulant, this poses particular challenges due to the falsely elevated prothrombin time and INR caused by argatroban. The combination of argatroban and warfarin may raise the INR to greater than 5.0 without a significant increased risk of bleeding complications.[3]

[edit] References

  1. ^ Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288
  2. ^ Dhillon S. Agratroban: A Review of its Use in the Management of Heparin-Induced Thrombocytopenia. Am J Cardiovasc Drugs 2009; 9 (4): 261-82. Link text
  3. ^ Hursting MJ, Lewis BE, Macfarlane DE. (2005). "Transitioning from argatroban to warfarin therapy in patients with heparin-induced thrombocytopenia.". Clin Appl Thromb Hemost 11 (3): 279–87. doi:10.1177/107602960501100306. PMID 16015413. 

[edit] External links

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Antithrombotics (thrombolytics, anticoagulants and antiplatelet drugs) (B01)
Antiplatelet drugs
Thromboxane inhibitors
Other
Anticoagulants
Factor Xa inhibitors
(with some II inhibition)
Other
Thrombolytic drugs/
fibrinolytics
Non-medicinal
Citrate • EDTA • Oxalate
Retrieved from "http://en.wikipedia.org/wiki/Argatroban"

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Argatroban".

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