title: An overview of the direct thrombin inhibitor argatroban.
abstract: Argatroban is a small molecule direct thrombin inhibitor. The main attributes of this synthetic drug are its rapid onset of anti-thrombin action, rapid reversibility of its anticoagulant effect, potent inhibition of clot-bound thrombin, absence of antibody formation and no need for initial dosage adjustment in patients with renal impairment. It is eliminated by hepatic metabolism. These properties make argatroban a predictable anticoagulant with intravenous use in a routine clinical setting. Argatroban is approved in the US and Canada for both prophylaxis and treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT); and it is approved in Japan and Korea for treatment of various thrombotic disorders. Argatroban has been shown in limited trials to provide reliable anticoagulation during percutaneous coronary interventions on HIT and non-HIT patients. Preliminary reports document the feasibility of using argatroban for anticoagulation during peripheral vascular interventions, hemodialysis and as adjunct to thrombolysis for treatment of myocardial infarction. Current recommendations for argatroban monitoring are to use the activated partial thromboplastin time for low doses and the activated clotting time for high doses. The ease of monitoring argatroban, its 'turn-on/turn-off' characteristic and its consistent safety profile provide the rationale to continue studies of argatroban as an anticoagulant in clinical settings.
authors.affiliation: Thoracic and Cardiovascular Surgery and Pathology, Loyola University Medical Center, Maywood, IL 60153 USA. jwaleng@lumc.edu
authors.forename: Jeanine M
authors.initials: JM
authors.lastname: Walenga
mesh_terms: D001120:Arginine / Q000031:analogs & derivatives; D006801:Humans; D010875:Pipecolic Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013449:Sulfonamides; D013917:Thrombin / Q000037:antagonists & inhibitors*; D013921:Thrombocytopenia / Q000139:chemically induced / Q000188:drug therapy; D013927:Thrombosis / Q000188:drug therapy; D016896:Treatment Outcome
chemical_list: D010875:Pipecolic Acids; D013449:Sulfonamides; D001120:Arginine; D013917:Thrombin; C031942:argatroban