- 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
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 = intravenousArgatroban is an
anticoagulant that is a small moleculedirect 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 theFood and Drug Administration (FDA) for prophylaxis or treatment ofthrombosis in patients withheparin-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 tolepirudin , 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]
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