Bivalirudin Trifluoroacetate role

Bivalirudin Trifluoroacetate role with heparin, it does not rely on antithrombin 1V (NI1_ Ⅳ), heparin cofactor Ⅱ and so on. Thrombin plays a central role in the coagulation serine protease: it is the hydrolysis of fibrinogen to generate fibrin monomers; activation of coagulation factor X Ⅲ; promote crosslinking of fibrin clots to form a stable covalent structure. Meanwhile, thrombin activates factor V, Ⅷ; activates platelets promote platelet aggregation and granule release. This product can be hydrolyzed due to thrombin peptide sequence Arg3 and Pro4 peptide bond between, so that the product inactivation, so the product of thrombin inhibition is reversible and transient. In in vitro experiments, the product concentration-dependent manner to extend the healthy human plasma activated partial thromboplastin time (activated partial thromboplastin time, af T), thrombin time (thrombin time, 1vr), prothrombin time (prothrombin time, PT ). The goods and the free thrombin or thrombus thrombin binding without affecting platelet release substances. Trial in healthy volunteers show: This product dose and concentration-dependent manner activated clotting time extension (activated clotting time, ACT), af Ding, Prr and 1vr. Due to vascular occlusion ≥ 70% while receiving percutaneous transluminal coronary angioplasty (PTCA) in patients with coronary heart disease treatment given after the product is also available with the same anticoagulant effect of healthy people. In the generation after intravenous anticoagulant effect of this product, the patient's coagulation in about 1 h after discontinuation tended to be normal. 291 cases due to vascular occlusion greater than 70% while receiving PTCA in patients treated with the dose increased, the majority of patients with ACI, time to reach the 300 or 350S. iv 1 mg'kg this product, combined 2.5 mg · kg · h infusion for 4h, and then 0.2 mg · kg · h dose to maintain 14 to 20h, all patients A (vr values ​​exceed 300S.

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