ARGATROBAN

12.1 Mechanism of Action 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; activation of protein C; and platelet aggregation. Argatroban inhibits thrombin with an inhibition 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.

Contraindications

• • 4 CONTRAINDICATIONS Argatroban is contraindicated in: Patients with major bleeding
• • [see Warnings and Precautions (5.1) ] Patients with a history of hypersensitivity to argatroban. Airway
• • skin
• • and generalized hypersensitivity reactions have been reported [see Adverse Reactions (6.1) ] Major bleeding (4) History of hypersensitivity to this product (4)