房颤的药物治疗及进展.pptVIP

* 体外实验结果证明利伐沙班是一个特异性、竞争性、直接Xa因子抑制剂1。在健康人体的试验显示它对凝血酶没有直接作用，不需要辅助因子2。 利伐沙班可以抑制人血浆中内源性和外源性凝血途径生成的的Xa因子3，包括游离的以及与纤维蛋白结合的Xa因子，同时还可抑制凝血酶原复合物中的Xa因子 1,4 利伐沙班是一个疗效卓越的抗凝药物，因为它的作用已经被所有的凝血试验（凝血酶原时间、活化部分凝血活酶时间）所证实2,5 利伐沙班抑制凝血酶生成6 利伐沙班不会直接影响血小板聚集3,7,8 发生出血后使用重组因子VIIa, 能部分逆转大剂量利伐沙班的抗凝作用9 Perzborn E et al. In vitro and in vivo studies of the novel antithrombotic agent BAY?59-7939—an oral, direct Factor Xa inhibitor. J Thromb Haemost 2005;3:514–521 Kubitza D et al. Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY?59-7939, an oral, direct Factor Xa inhibitor. Clin Pharmacol Ther 2005;78:412–421 Fareed J et al. Antithrombotic mechanism of action of BAY?59-7939 – a novel, oral, direct Factor Xa inhibitor. J Thromb Haemost 2005;3(S1):Abstract P0518 Depasse F et al. Effect of BAY 59-7939 – a novel, oral, direct Factor Xa inhibitor – on clot-bound Factor Xa activity in vitro. J Thromb Haemost 2005;3 (Suppl. 1):Abstract P1104 Kubitza D et al. Safety, pharmacodynamics and pharmacokinetics of BAY?59-7939 – an oral, direct Factor Xa inhibitor – after multiple dosing in healthy male subjects. Eur J Clin Pharmacol 2005;61:873–880 Graff J et al. Effects of the oral, direct Factor Xa-inhibitor rivaroxaban (BAY 59-7939) on platelet-induced thrombin generation and prothrombinase activity. J Clin Pharmacol 2007; doi: 10.1177/0091270007302952 Perzborn E et al. Biochemical and pharmacologic properties of BAY 59-7939, an oral, direct Factor Xa inhibitor. Pathophysiol Haemost Thromb 2004;33(S2):Abstract PO079 Kubitza D et al. Rivaroxaban (BAY?59?7939) – an oral, direct Factor Xa inhibitor – has no clinically relevant interaction with naproxen. Br J Clin Pharmacol 2007;63:469–474 Tinel H, Huetter J, Perzborn E. Partial reversal of the anticoagulant effect of high-dose rivaroxaban – an oral, direct Factor Xa inhibitor – by recombinant Factor VIIa in rats. Blood 2006;108:Abstract 915 * * * The following slides summarize the ROCKET AF clinical trial, investigating the use of rivaroxa