Pharmacokinetic drug evaluation of bucindolol for the treatment of atrial fibrillation in heart failure patients.
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.
a Department of Internal Medicine, Cardiology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
Gian Marco
GM
Rosa
a Department of Internal Medicine, Cardiology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
Giovanni
G
Meliota
a Department of Internal Medicine, Cardiology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
Claudio
C
Brunelli
b Department of Obstetrics and Gynaecology, IRCCS AOU San Martino - IST , University of Genoa , Genova , Italy.
Simone
S
Ferrero
D000319:Adrenergic beta-Antagonists / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D001281:Atrial Fibrillation / Q000188:drug therapy* / Q000503:physiopathology; D006333:Heart Failure / Q000188:drug therapy* / Q000235:genetics / Q000503:physiopathology; D006760:Hospitalization; D006801:Humans; D011412:Propanolamines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D018341:Receptors, Adrenergic, alpha-2 / Q000235:genetics; D018342:Receptors, Adrenergic, beta-1 / Q000235:genetics
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D018341:Receptors, Adrenergic, alpha-2; D018342:Receptors, Adrenergic, beta-1; C024307:bucindolol
Bucindolol; atrial fibrillation; heart failure; β-blocker drugs