Rosa Gian Marco, Meliota Giovanni, Brunelli Claudio, Ferrero Simone
a Department of Internal Medicine, Cardiology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
b Department of Obstetrics and Gynaecology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
Expert Opin Drug Metab Toxicol. 2017 Apr;13(4):473-481. doi: 10.1080/17425255.2017.1291631. Epub 2017 Feb 15.
Atrial fibrillation (AF) and heart failure (HF) often coexist. When AF and HF are both present, they are associated with negative outcomes, increased hospitalizations and mortality. As β-blockade is effective inF and may be useful in presence of AF, bucindolol, a non-selective β-blocker with α-1 vasodilatory effect, may be used. Area covered: This review evaluates the efficacy and safety of bucindolol in HF patients with AF. The largest amount of data comes from BEST trial which evaluated the efficacy of bucindolol in HF patients. Since bucindolol's effects are genetically modulated by β1 and α2c-adrenergic receptor polymorphisms BEST genetic substudy arose. Expert opinion: In the BEST Trial, bucindolol demonstrated efficacy in HF patients showing a 74% reduction in new-onset atrial fibrillation events particularly in β1 389 Arg/Arg homozygous. GENETIC-AF study was designed to determine whether bucindolol therapy is superior to metoprolol in preventing recurrent AF in a genetically targeted population of HF patients. Furthermore, this drug is safe, but presents the same side effects as all β-blockers and has showed no clear benefits in African-Americans and in class IV NYHA patients. Further studies are needed to confirm and validate the role of bucindolol and its economic implications.
心房颤动（AF）与心力衰竭（HF）常并存。当AF和HF同时存在时，它们与不良后果、住院率增加及死亡率升高相关。由于β受体阻滞剂对HF有效且在AF存在时可能有用，布新洛尔，一种具有α-1血管舒张作用的非选择性β受体阻滞剂，可能会被使用。涵盖领域：本综述评估布新洛尔在合并AF的HF患者中的疗效和安全性。最大量的数据来自评估布新洛尔在HF患者中疗效的BEST试验。由于布新洛尔的作用受β1和α2c肾上腺素能受体多态性的基因调控，因此出现了BEST基因亚研究。专家观点：在BEST试验中，布新洛尔在HF患者中显示出疗效，新发房颤事件减少了74%，尤其是在β1 389 Arg/Arg纯合子患者中。GENETIC-AF研究旨在确定在基因靶向的HF患者群体中，布新洛尔治疗在预防房颤复发方面是否优于美托洛尔。此外，这种药物是安全的，但具有所有β受体阻滞剂相同的副作用，并且在非裔美国人及纽约心脏协会（NYHA）IV级患者中未显示出明显益处。需要进一步研究来证实和验证布新洛尔的作用及其经济影响。
