Binds reversibly to thrombin active sites with anticoagulant effects by inhibiting thrombin catalyzed or induced reactions, including activation of coagulation factors V, VIII and XIII, protein C, and platelet aggregation.
Distributed mainly in the extracellular fluid space.
Approximately 50% protein bound.
Approximately 5% excreted in the feces and 22% excreted in the urine.
No dosage adjustment needed for renal disease but is recommended for the presence of hepatic disease.
Used for prophylaxis and treatment of thrombosis in heparin induced thrombocytopenia.
Utilized as an anticoagulant in patients at risk for heparin induced thrombocytopenia undergoing percutaneous coronary intervention.
With moderate hepatic impairment the initial dose is 0.5 mcg/kg/min with monitoring by the activated partial thromboplastin time.
Usual recommended starting dose 2.0 microgram/kg/min infusion.
For HIT or HIT with thrombosis the dose can be titrated as clinically indicated up to 10 mcg/kg, until a steady state of aPTT 1.5-3 times the initial baseline value.
With percutaneous coronary intervention in HIT or HIT and thrombosis an initial dose of 25 mcg as a continuous infusion and a bolus of 350 mcg/kg over 3-5 minutes: activated clotting time is checked in 5-10 minutes after bolus and additional bolus are administered to reach a activated clotting time between 300 and 450 sec.
Adverse reactions include: hypotension 1%, cardiac arrest 6%, bradycardia and ventricular tachycardia 5%, myocardial infarction 4%, atrial fibrillation 3%, headache 5%, intracranial hemorrhage 4%, allergic reactions les than 0%, minor gastrointestinal bleeding 14%, diarrhea and vomiting 6%, abdominal pain 4%, major gastrointestinal bleeding 2% and gastro esophageal reflux disease 1%, minor genitourinary bleeding 12%, abnormal renal function 3%, major genitourinary bleeding 1% overall bleeding 5% retroperitoneal hemorrhage 1%, hemoptysis 3% cough and dyspnea 10%.
Argatroban a selective thrombin inhibitor, directly inhibits freeand clot associated thrombin, as well as thrombin induced events, and is widely used to treat acute ischemic stroke, particularly in Asian countries.
Among patients with acute ischemic stroke treatment with argatroban plus intravenous alteplase compared with alteplase alone did not result in a significant grade likelihood of excellent functional outcome at 90 days.