【心血管 内科 介入 课件】093.有关比伐卢定的几个问题
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▪ Nonspecific binding to: ―Plasma proteins ―Endothelial cells (variable anticoagulation level)
▪ Inhibited by platelet factor 4 ―reduced effect in ACS
▪ Causes platelet aggregation
▪ 接触性血栓
Overcoming Limitations of Heparins
Attribute Active moieties in substance Action independent of AT Non-specific protease binding Variable PK-PD Inhibits fibrin-bound thrombin Activates/aggregates platelets T0.5 in minutes PF-4 complexing & risk of HIT
UFH Enox
Impact
30-35% 40-60% Unpredictable
No
No Unpredictable
Yes Partial Unpredictable
Yes
Less Unpredictable
No
No
Need ↑ dose
Yes
+/-
Need IIb/IIIa
60-90’ 270’
▪ Risk of HIT
Hirsh J, et al. Circulation. 2001;103:2994-3018
LMWH
Disadvantages
▪Indirect thrombin inhibitor ▪Less reversible than UFH ▪Long half-life ▪Renal clearance ▪Risk of HIT
Hirsh J, et a:. Circulation 2001;103:2994-3018
Limitations of Heparins
Attribute Active moieties in substance Action independent of AT Non-specific protease binding Variable PK-PD Inhibits fibrin-bound thrombin Activates/aggregates platelets T0.5 in minutes PF-4 complexing & risk of HIT
▪ 2005 – 2009 ▪ Elective PCI: 599,524 pts ▪ UA/NSTEMI: 836,103 pts ▪ STEMI: 267,632 pts
Subherwal S. J Am Coll Cardiol 2012;59:1861–9
UFH
Disadvantages
▪ Indirect thrombin inhibitor (does not inhibit clot-bound thrombin)
Subherwal S. J Am Coll Cardiol 2012;59:1861–9
Impact of Diabetes on the Safety and Effectiveness of Bivalirudin in Pts With AMI Undergoing
I
• PCI in STEMI and NSTE-ACS
Circulation and JACC 2005, 2007, 2009, 2011 EHJ 2010
有关比伐卢定的几个问题
▪ 为什么要用比伐卢定替代肝素？ ▪ 何时和如何使用比伐卢定？ ▪ 为什么美国心导管室比伐卢定使用率不是
100%？ ▪ 非冠脉以外介入治疗的应用
▪No HIT
Xiao Z, Theroux P: Circulation 1998;97:251-256
Changes in Utilization of Different Antithrombotic Strategies Over Time
▪ 截止2009年06月10日，全球38个国家获得上市许 可，超过 220万的患者接受了比伐卢定的治疗
有关比伐卢定的几个问题
国家心血管病中心 中国医学科学院 阜外心血管病医院
Bivalirudin Use Guidelines: ACC/AHA
I • PCI in STEMI and NSTE-ACS • Pts with HIT or HITTS
IIa
• Elective PCI
ESC/EACTS Guidelines on Myocardial Revascularization
Temporal Trends in and Factors Associated With Bleeding Complications Among Patients Undergoing PCI:
A Report From the National Cardiovascular Data Cath PCI Registry
UFH
Enox Bivalirudin
30–35% 40–60%
100%
No
No
Yes
Yes
ParFra Baidu bibliotekial
No
Yes
Less
No
No
No
Yes
Yes
+/-
Inhibits
60–90’
270’
25’
Yes Reduced
No
Bivalirudin
Advantages ▪Predictable anticoagulant response ▪ FDA在2000年12月批准上市许可 ▪Inhibits soluble and fibrin-bound thrombin ▪ 美国于2001年1月上市 ▪Inhibits thrombin-induced platelet aggregation
↑ Bleeding
Yes Reduced Very bad
普通肝素→依诺肝素→磺达肝癸钠
▪ 肝素诱导的血小板减少症 ▪ 肝素“抵抗现象” ▪ 肝素类药物依赖抗凝血酶Ⅲ发挥作用，对于抗凝血酶Ⅲ
缺乏的患者则没有抗凝效应 ▪ 出血
－最主要的副作用，低分子肝素抗凝可预测性高，不需监测，但出 血发生率，特别是在肾功能不全的患者中仍显著增高
▪ Inhibited by platelet factor 4 ―reduced effect in ACS
▪ Causes platelet aggregation
▪ 接触性血栓
Overcoming Limitations of Heparins
Attribute Active moieties in substance Action independent of AT Non-specific protease binding Variable PK-PD Inhibits fibrin-bound thrombin Activates/aggregates platelets T0.5 in minutes PF-4 complexing & risk of HIT
UFH Enox
Impact
30-35% 40-60% Unpredictable
No
No Unpredictable
Yes Partial Unpredictable
Yes
Less Unpredictable
No
No
Need ↑ dose
Yes
+/-
Need IIb/IIIa
60-90’ 270’
▪ Risk of HIT
Hirsh J, et al. Circulation. 2001;103:2994-3018
LMWH
Disadvantages
▪Indirect thrombin inhibitor ▪Less reversible than UFH ▪Long half-life ▪Renal clearance ▪Risk of HIT
Hirsh J, et a:. Circulation 2001;103:2994-3018
Limitations of Heparins
Attribute Active moieties in substance Action independent of AT Non-specific protease binding Variable PK-PD Inhibits fibrin-bound thrombin Activates/aggregates platelets T0.5 in minutes PF-4 complexing & risk of HIT
▪ 2005 – 2009 ▪ Elective PCI: 599,524 pts ▪ UA/NSTEMI: 836,103 pts ▪ STEMI: 267,632 pts
Subherwal S. J Am Coll Cardiol 2012;59:1861–9
UFH
Disadvantages
▪ Indirect thrombin inhibitor (does not inhibit clot-bound thrombin)
Subherwal S. J Am Coll Cardiol 2012;59:1861–9
Impact of Diabetes on the Safety and Effectiveness of Bivalirudin in Pts With AMI Undergoing
I
• PCI in STEMI and NSTE-ACS
Circulation and JACC 2005, 2007, 2009, 2011 EHJ 2010
有关比伐卢定的几个问题
▪ 为什么要用比伐卢定替代肝素？ ▪ 何时和如何使用比伐卢定？ ▪ 为什么美国心导管室比伐卢定使用率不是
100%？ ▪ 非冠脉以外介入治疗的应用
▪No HIT
Xiao Z, Theroux P: Circulation 1998;97:251-256
Changes in Utilization of Different Antithrombotic Strategies Over Time
▪ 截止2009年06月10日，全球38个国家获得上市许 可，超过 220万的患者接受了比伐卢定的治疗
有关比伐卢定的几个问题
国家心血管病中心 中国医学科学院 阜外心血管病医院
Bivalirudin Use Guidelines: ACC/AHA
I • PCI in STEMI and NSTE-ACS • Pts with HIT or HITTS
IIa
• Elective PCI
ESC/EACTS Guidelines on Myocardial Revascularization
Temporal Trends in and Factors Associated With Bleeding Complications Among Patients Undergoing PCI:
A Report From the National Cardiovascular Data Cath PCI Registry
UFH
Enox Bivalirudin
30–35% 40–60%
100%
No
No
Yes
Yes
ParFra Baidu bibliotekial
No
Yes
Less
No
No
No
Yes
Yes
+/-
Inhibits
60–90’
270’
25’
Yes Reduced
No
Bivalirudin
Advantages ▪Predictable anticoagulant response ▪ FDA在2000年12月批准上市许可 ▪Inhibits soluble and fibrin-bound thrombin ▪ 美国于2001年1月上市 ▪Inhibits thrombin-induced platelet aggregation
↑ Bleeding
Yes Reduced Very bad
普通肝素→依诺肝素→磺达肝癸钠
▪ 肝素诱导的血小板减少症 ▪ 肝素“抵抗现象” ▪ 肝素类药物依赖抗凝血酶Ⅲ发挥作用，对于抗凝血酶Ⅲ
缺乏的患者则没有抗凝效应 ▪ 出血
－最主要的副作用，低分子肝素抗凝可预测性高，不需监测，但出 血发生率，特别是在肾功能不全的患者中仍显著增高