文档介绍：有关比伐卢定的几个问题
ESC/EACTS Guidelines on Myocardial Revascularization
PCI in STEMI and NSTE-ACS
I
Bivalirudin Use Guidelines: ACC/AHA
PCI in STEMI and NSTE-ACS
Pts with HIT or HITTS
I
EHJ 2010
Circulation and JACC 2005, 2007, 2009, 2011
Elective PCI
IIa
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
Temporal Trends in and Factors Associated With Bleeding Complications Among Patients Undergoing PCI: A Report From the National Cardiovascular Data Cath PCI Registry
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
Indirect thrombin inhibitor (does not inhibit clot-bound thrombin)
Nonspecific binding to:
Plasma proteins
Endothelial cells
(variable anticoagulation level)
Inhibited by platelet factor 4
reduced effect in ACS
Causes platelet aggregation
Risk of HIT
Disadvantages
Hirsh J, et al. Circulation. 2001;103:2994-3018
LMWH
Indirect thrombin inhibitor
Less reversible than UFH
Long half-life
Renal clearance
Risk of HIT
Disadvantages
Hirsh J, et a:. Circulation 2001;103:2994-3018
Limitations of Heparins
Attribute
UFH
Enox
Impact
Active moieties in substance
30-35%
40-60%
Unpredictable
Action independent of AT
No
No
Unpredictable
Non-specific protease binding
Yes
Partial
Unpredictable
Variable PK-PD
Yes
Less
Unpredictable
Inhibits fibrin-bound thrombin
No
No
Need ↑ dose
Activates/aggregates platelets
Yes
+/-
Need IIb/IIIa
in minutes
60-90’
270’
↑ Bleeding
PF-4 complexing & risk of HIT
Yes
Reduced
Very bad
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
接触性血栓
普通肝素→依诺肝素→磺达肝癸钠
Overcoming Limitations of Heparins
Attribute
UFH
Enox
Bivalirudin
Active moieties in substance
30–35%
40–60%
100%
Action independent of AT
No
No
Yes
Non-specific protease binding
Yes
Partial
No
Variable PK-PD