替格瑞洛讲座.ppt

替格瑞洛（倍林达）在抗血小板聚集中的作用 Ticagrelor for the role of anti-platelet aggregation,昌平区中医医院：张碎虎,content,Changping chineses medicine hospital,噻吩吡啶类药物发展史,Anti-platelet aggregation,卜晓斐.现代药物与临床,27(1).,血小板血栓形成过程,Adhesion,1,Activation,2,Thrombin,ADP,5 HT,PAF,Handin RI. Harrisons Principles of Internal Medicine.Vol 1. 14th ed. NY, NY: McGraw-Hill; 1998:339-345. Schafer AI. Am J Med. 1996;101:199-209.,3,Aggregation,替格瑞洛,P2Y12,替格瑞洛（倍林达）作用机制,替格瑞洛药物特点,氯吡格雷：肝脏CYP450酶两步代谢（CYP2C19, CYP3A4等）,普拉格雷：肝脏CYP450一步代谢,替格瑞洛：2/3以原型化合物起效，1/3可经肝脏CYP3A4代谢，代谢产物仍有活性,Yousuf, O. & Bhatt, D. L. Nat. Rev. Cardiol. advance online publication 12 July 2011,P2Y12受体抑制剂的药理特性比较,Clark MG, et al.Heart 12:30-47.,替格瑞洛的临床作用,PLATO,HOUYI-STUDY,SPEGASUS-TIMI 54,第一PPT模板网：,PLATO,HR 95%CI 0.79 0.69-0.91,倍林达与氯吡格雷相比，显著降低心血管死亡率达21%,倍林达与氯吡格雷相比，总体主要出血发生率无显著差异,*PLATO主要出血的定义:致命性或颅内出血、伴有心包填塞的心包内出血、由出血导致的低血容量休克或严重低血压需要升压药或手术、Hb下降(50g/L)、因出血而输血4u(全血或浓集红细胞PRBC)；其他主要出血：显著的功能丧失(如眼内出血伴永久性失明)、Hb下降(30-50g/L)、因出血而输血2-3u(全血或PRBC),Wallentin L, et al. N Engl J Med 2009; 361:10451057.,6.10%,5.11%,11.60%,9.63%,PEGASUS-TIMI 54,Result:Ticagrelor 90mg,60mg vs placebo Reduced the rate of the primary end point 15%, 16%,Bonaca MP. N Engl J Med. 2015 May 7;372(19):1791-800.,Efficacy End Points as 3 year Kaplan-Meier Estimates(%),Efficacy End Points as 3 year Kaplan-Meier Estimates(%),HOUYI Study,Percentage of patients with a PRU value of 240. PRU=P2Y12 reaction unit,替格瑞洛（倍林达）指南类推荐,Europe,Canada,United States,Chinese,1. Roffi M, et al. European Heart Journal. 2015doi:10.1093/eurheartj/ehv320 2. Windecker S, et al. Eur Heart J. 2014;35(37):2541-2619 3. Perk J, et al. European Heart Journal . 2012;33:16351701 4. Steg G, et al. European Heart Journal.2012;33:25692619,1. Amsterdam EA, et al. Circulation. 2014;130:e344-e426. 2. OGara PT, et al. Circulation. 2013;127:e362-e425 3. Guyatt GH, et al. CHEST. 2012;141:7S-47S 4. Smith SC Jr, et al. Circulation. 2011;124(22):2458-2473 5. Levine GL, et al. J Am Coll Cardiol. 2011;58:2550-2583；,Bell AD, et al. Can J Cardiol. 2011 May-Jun;27 Suppl A:S1-S59,1.中华医学会心血管病学分会.中华心血管病杂志,2015;43(5):380-393 2.中华医学会心血管病学分会介入心脏病学组.中华心血管病杂志.2012;40(4):271-277 3.中华医学会心血管病分会 中华心血管病杂志. 2012;40(5):353-367,Thank you! for taking the time to listen t