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Argatroban

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Argatroban
File:Argatroban.svg
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
Clinical data
Trade names Argatroban
AHFS/Drugs.com monograph
intravenous
Pharmacokinetic data
Bioavailability 100% (intravenous)
Protein binding 54%
Metabolism hepatic
Half-life 39 and 51 minutes
Identifiers
74863-84-6 7pxY
B01AE03
PubChem CID 440542
DrugBank DB00278 7pxY
ChemSpider 389444 7pxY
UNII OCY3U280Y3 7pxY
KEGG C04931 7pxY
ChEMBL CHEMBL1166 7pxN
Chemical data
Formula C23H36N6O5S
508.635 g/mol
 14pxN (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. In 2012, it was approved by the MHRA in the UK for anticoagulation in patients with Heparin-Induced Thrombocytopenia Type II (HIT) who require parenteral antithrombotic therapy.[2]

Argatroban is given intravenously and drug plasma concentrations reach steady state in 1-3 hours.[3] 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).

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.[4] One solution to this problem is to measure the chromogenic factor X level. A level < 40-45% typically indicates that the INR will be therapeutic (2-3) when the argatroban is discontinued.

References

  1. ^ Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288
  2. ^ http://www.pharmatimes.com/Article/12-07-03/UK_launch_for_Mitsubishi_s_blood_thinner_Exembol.aspx
  3. ^ Dhillon S. Argatroban: A Review of its Use in the Management of Heparin-Induced Thrombocytopenia. Am J Cardiovasc Drugs 2009; 9 (4): 261-82. Link text
  4. ^ 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. PMID 16015413. doi:10.1177/107602960501100306. 

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