Smart Neil A, Kwok Nigel, Holland David J, Jayasighe Rohan, Giallauria Francesco
School of Science and Technology, University of New England, Armidale, NSW 2351, Australia.
Clin Med Insights Cardiol. 2011;5:55-66. doi: 10.4137/CMC.S4309. Epub 2011 Jun 28.
Bucindolol is a non-selective β-adrenergic receptor blocker with α-1 blocker properties and mild intrinsic sympatholytic activity. The Beta-Blocker Evaluation of Survival Trial (BEST), which is the largest clinical trial of bucindolol in patients with heart failure, was terminated prematurely and failed to show an overall mortality benefit. However, benefits on cardiac mortality and re-hospitalization rates were observed in the BEST trial. Bucindolol has not shown benefits in African Americans, those with significantly low ejection fraction and those in NYHA class IV heart failure. These observations could be due to the exaggerated sympatholytic response to bucindolol in these sub-groups that may be mediated by genetic polymorphisms or changes in gene regulation due to advanced heart failure. This paper provides a timely clinical update on the use of bucindolol in chronic heart failure.
布辛多洛尔是一种具有α-1受体阻滞特性和轻度内在拟交感活性的非选择性β-肾上腺素能受体阻滞剂。β受体阻滞剂生存评估试验（BEST）是布辛多洛尔在心力衰竭患者中进行的最大规模临床试验，该试验提前终止，未显示出总体死亡率获益。然而，在BEST试验中观察到了对心脏死亡率和再住院率的益处。布辛多洛尔在非裔美国人、射血分数显著降低的患者以及纽约心脏协会（NYHA）IV级心力衰竭患者中未显示出益处。这些观察结果可能是由于这些亚组中对布辛多洛尔的拟交感反应过度，这可能由基因多态性或晚期心力衰竭导致的基因调控变化介导。本文及时提供了布辛多洛尔在慢性心力衰竭中应用的临床最新情况。
