Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Traditional IUPAC Name
pKa (strongest acidic)
pKa (Strongest Basic)
Dược Lực Học :
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.
Cơ Chế Tác Dụng :
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 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.
Dược Động Học :
▧ Absorption :
Bioavailability is 100% (intravenous).
▧ Volume of Distribution :
* 174 mL/kg
* 12.18 L [70-kg adult]
▧ Protein binding :
▧ Metabolism :
Liver via hydroxylation and aromatization of the 3-methyltetrahydroquinoline ring. Age and gender do not substantially affect the pharmacodynamic or pharmacokinetic profile of argatroban.
▧ Route of Elimination :
Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.
▧ Half Life :
39 and 51 minutes
▧ Clearance :
* 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min]
Độc Tính :
Chỉ Định :
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.
Tương Tác Thuốc :
Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Argatroban. Monitor for increased bleeding during concomitant thearpy.
Liều Lượng & Cách Dùng :
Solution - Intravenous - 100mg/mL
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