Argatroban

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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	152951
DrugBank	APRD00105
Chemical data
Formula	C23H36N6O5S
Mol. mass	508.635 g/mol
Pharmacokinetic data
Bioavailability	100% (intravenous)
Protein binding	54%
Metabolism	hepatic
Half life	39 and 51 minutes
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	intravenous

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. 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).

It is manufactured by GlaxoSmithKline.

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

Argatroban is used as an anticoagulant in individuals with thrombosis due to 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.^[2]

[edit] References

1. ^ Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288
2. ^ 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

• GlaxoSmithKline's website on argatroban

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