Argatroban
Argatroban Uses, Dosage, Side Effects, Food Interaction and all others data.
Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban.
Argatroban is a synthetic direct thrombin inhibitor derived from L-arginine indicated as an anticoagulant for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia. Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation. Argatroban is highly selective for thrombin with an inhibitory constant (Ki) of 0.04 µM. At therapeutic concentrations, Argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein).Argatroban is capable of inhibiting the action of both free and clot-associated thrombin.
Trade Name | Argatroban |
Availability | Prescription only |
Generic | Argatroban |
Argatroban Other Names | Argatroban |
Related Drugs | warfarin, Coumadin, heparin, alteplase, Jantoven, streptokinase |
Weight | 1mg/ml, 100mg/ml, |
Type | Infusion, Intravenous Solution, Intravenous |
Formula | C23H36N6O5S |
Weight | Average: 508.64 Monoisotopic: 508.246789457 |
Protein binding | 54% |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | Accord Healthcare Limited |
Available Country | United Kingdom, United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Argatroban is a synthetic direct thrombin inhibitor used for the prevention and treatment of thrombosis related to heparin use.
Argatroban is indicated for prevention and treatment of thrombosis caused by heparin-induced thrombocytopenia (HIT). It is also indicated for use in patients with, or at risk for, HIT who are undergoing percutaneous coronary intervention.
Argatroban is also used to associated treatment for these conditions: Thrombotic events
How Argatroban works
Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; protein C; and platelet aggregation.
Toxicity
Excessive bleeding
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of argatroban; however, the evidence is conflicting.
- Exercise caution with St. John's Wort.
Argatroban Drug Interaction
Major: enoxaparin, enoxaparin, clopidogrel, clopidogrelUnknown: lorazepam, lorazepam, amoxicillin / clavulanate, amoxicillin / clavulanate, bumetanide, bumetanide, diltiazem, diltiazem, propofol, propofol, furosemide, furosemide, levofloxacin, levofloxacin, octreotide, octreotide
Argatroban Disease Interaction
Volume of Distribution
- 174 mL/kg
- 12.18 L [70-kg adult]
Elimination Route
Bioavailability is 100% (intravenous).
Half Life
39 and 51 minutes
Clearance
- 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min]
Elimination Route
Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.
Innovators Monograph
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