Exembol
Exembol Uses, Dosage, Side Effects, Food Interaction and all others data.
Exembol 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. Exembol 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.
Exembol 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. Exembol is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Exembol does not require the co-factor antithrombin III for antithrombotic activity. Exembol 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. Exembol is highly selective for thrombin with an inhibitory constant (Ki) of 0.04 µM. At therapeutic concentrations, Exembol has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein).Exembol is capable of inhibiting the action of both free and clot-associated thrombin.
Trade Name | Exembol |
Availability | Prescription only |
Generic | Argatroban |
Argatroban Other Names | Argatroban |
Related Drugs | warfarin, Coumadin, heparin, alteplase, Jantoven, streptokinase |
Type | infusion |
Formula | C23H36N6O5S |
Weight | Average: 508.64 Monoisotopic: 508.246789457 |
Protein binding | 54% |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | Mitsubishi Tanabe Pharma Europe Ltd, |
Available Country | United Kingdom |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Exembol is a synthetic direct thrombin inhibitor used for the prevention and treatment of thrombosis related to heparin use.
Exembol 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.
Exembol is also used to associated treatment for these conditions: Thrombotic events
How Exembol works
Exembol 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.
Exembol 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
Exembol 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
Exembol is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.
Innovators Monograph
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