Pharmacokinetic drug evaluation of bucindolol for the treatment of atrial fibrillation in heart failure patients. (3rd April 2017)

• Record Type: Journal Article
• Authors: Rosa, Gian Marco; Meliota, Giovanni; Brunelli, Claudio; Ferrero, Simone
• Is Part Of: Expert opinion on drug metabolism and toxicology. Volume 13:Number 4(2017:Apr.)
• Page Start: 473
• Page End: 481
• Publication Date: 2017-04-03
• Subjects: Bucindolol -- β-blocker drugs -- atrial fibrillation -- heart failure; Drugs -- Toxicology -- Periodicals; Drugs -- Metabolism -- Periodicals; 615.7
• DOI: 10.1080/17425255.2017.1291631
• Languages: English
• ISSNs: 1742-5255

Abstract

ABSTRACT: Introduction : 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.