Argatroban

drugbox
IUPAC_name = (2"R",4"R")-1- [(2"S")-5-(diaminomethylideneamino)-2-
[ [(3"R")-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]
sulfonylamino] pentanoyl] -4-methyl-piperidine-2-
carboxylic acid

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CAS_number = 74863-84-6
ATC_prefix = B01
ATC_suffix = AE03
ATC_supplemental =
PubChem = 152951
DrugBank = APRD00105
C=23 | H=36 | N=6 | O=5 | S=1
molecular_weight = 508.635 g/mol
bioavailability = 100% (intravenous)
protein_bound = 54%
metabolism = hepatic
elimination_half-life = 39 and 51 minutes
pregnancy_category =
legal_status =
routes_of_administration = intravenous

Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor. [Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. "N Engl J Med" 2005;353:1028-40. PMID 16148288] 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. 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.cite journal | author=Hursting MJ, Lewis BE, Macfarlane DE. | title=Transitioning from argatroban to warfarin therapy in patients with heparin-induced thrombocytopenia. | journal=Clin Appl Thromb Hemost | year=2005 | volume=11 | issue=3 | pages=279–87 | pmid=16015413 | doi=10.1177/107602960501100306]

References

External links

* [http://www.argatroban.com GlaxoSmithKline's website on argatroban]