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| Clinical data | |
|---|---|
| AHFS/Drugs.com | Monograph |
| License data | |
| Routes of administration | Intravenous |
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| Pharmacokinetic data | |
| Bioavailability | 100% (intravenous) |
| Protein binding | 54% |
| Metabolism | hepatic |
| Eliminationhalf-life | 39 and 51 minutes |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.166.378 |
| Chemical and physical data | |
| Formula | C23H36N6O5S |
| Molar mass | 508.64 g·mol−1 |
| 3D model (JSmol) | |
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Argatroban is ananticoagulant that is a small moleculedirect thrombin inhibitor.[3] In 2000, argatroban was licensed by the USFood and Drug Administration (FDA) for prophylaxis or treatment ofthrombosis in people withheparin-induced thrombocytopenia (HIT). In 2002, it was approved for use duringpercutaneous coronary interventions in people who have HIT or are at risk for developing it. In 2012, it was approved by the UKMedicines and Healthcare products Regulatory Agency for anticoagulation in people with heparin-induced thrombocytopenia Type II (HIT) who require parenteral antithrombotic therapy.[4]
Argatroban is given intravenously and drug plasma concentrations reach steady state in 1–3 hours.[5] Argatroban is metabolized in theliver and has ahalf-life of about 50 minutes. It is monitored byPTT. 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).
Argatroban is used as an anticoagulant in individuals with thrombosis and heparin-induced thrombocytopenia. Often these individuals require long-term anticoagulation. Ifwarfarin is chosen as the long-term anticoagulant, this poses particular challenges due to the falsely elevatedprothrombin time andINR 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.[6] One solution to this problem is to measure the chromogenic factor X level. A level < 40–45% typically indicates that the INR will be therapeutic (2–3) when the argatroban is discontinued.
