Differential effects of nonselective versus selective β-blockers on cardiac sympathetic activity and hemostasis in patients with heart failure

J Nucl Med. 2013 Oct;54(10):1733-9. doi: 10.2967/jnumed.113.120477. Epub 2013 Aug 22.

Abstract

Carvedilol, a nonselective β-blocker, may be more effective than the selective β-blocker metoprolol in reducing the risk of thromboembolic events in heart failure. The aim of this study was, first, to assess whether there is a differential response in cardiac sympathetic activity by (123)I-meta-iodobenzylguanidine ((123)I-MIBG) imaging when either β-blocker is used. Second, we assessed whether that response correlates with levels of various serum factors that serve as markers for coagulability.

Methods: In this prospective, randomized, open-label crossover study with masked outcome assessments, stable heart failure patients (left ventricular ejection fraction < 40%) homozygous for the Arg16/Gln27 (n = 13) or Gly16/Glu27 haplotype (n = 8) of the β2-receptor were randomized to equipotent dosages of carvedilol or metoprolol for two 6-wk periods. Primary outcome was sympathetic activity as measured by (123)I-MIBG myocardial washout. Secondary outcomes included markers of hemostasis.

Results: (123)I-MIBG cardiac washout was lower during carvedilol than metoprolol treatment (12.9% ± 3.9% vs. 22.1% ± 2.8%, respectively, P = 0.003), irrespective of β2-adrenergic receptor haplotype. In addition, treatment with carvedilol resulted in a lower von Willebrand factor than did metoprolol (149% ± 13% vs. 157% ± 13%, respectively, P = 0.01), irrespective of β2-adrenergic receptor haplotype.

Conclusion: Compared with metoprolol, carvedilol resulted in greater reduction of sympathetic activity after 6 wk of treatment and lower von Willebrand factor concentrations in both Arg16/Gln27 and Gly16/Glu27 individuals. Therefore, carvedilol may reduce the risk of thromboembolic events in patients with heart failure, irrespective of β2-receptor haplotype status.

Keywords: genetics, coagulation; heart failure; sympathetic nervous system; β-blockers.

Publication types

  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Iodobenzylguanidine
  • Adrenergic beta-Antagonists / pharmacology*
  • Adrenergic beta-Antagonists / therapeutic use
  • Aged
  • Carbazoles / pharmacology
  • Carbazoles / therapeutic use
  • Carvedilol
  • Female
  • Haplotypes
  • Heart / drug effects
  • Heart / innervation*
  • Heart / physiopathology*
  • Heart Failure / diagnostic imaging
  • Heart Failure / drug therapy*
  • Heart Failure / physiopathology*
  • Hemostasis / drug effects*
  • Humans
  • Male
  • Metoprolol / pharmacology
  • Metoprolol / therapeutic use
  • Middle Aged
  • Patient Selection
  • Propanolamines / pharmacology
  • Propanolamines / therapeutic use
  • Radionuclide Imaging
  • Receptors, Adrenergic, beta-2 / genetics
  • Receptors, Adrenergic, beta-2 / metabolism
  • Sympathetic Nervous System / diagnostic imaging
  • Sympathetic Nervous System / drug effects*
  • Treatment Outcome

Substances

  • Adrenergic beta-Antagonists
  • Carbazoles
  • Propanolamines
  • Receptors, Adrenergic, beta-2
  • Carvedilol
  • 3-Iodobenzylguanidine
  • Metoprolol