Impact of the β1-adrenoceptor Arg389Gly polymorphism on heart-rate responses to bisoprolol and carvedilol in heart-failure patients

Clin Pharmacol Ther. 2012 Jul;92(1):21-8. doi: 10.1038/clpt.2012.18. Epub 2012 May 23.

Abstract

This pharmacogenetic substudy of the prospective, double-blind, randomized CIBIS-ELD trial determined the impact of the β1-adrenoceptor Arg189Gly polymorphism on heart-rate responses to bisoprolol or carvedilol in elderly patients with heart failure (421 with sinus rhythm, 107 with atrial fibrillation). Patients were randomized 1:1 to bisoprolol or carvedilol with a fortnightly dose-doubling scheme and guideline target doses. Patients with sinus rhythm responded essentially identically to bisoprolol and carvedilol, independent of genotype. Atrial fibrillation patients homozygous for Arg389 had a much smaller response to carvedilol than carriers of at least one Gly389 allele (mean difference 12 bpm, P < 0.00001). Carvedilol up to 2 × 12.5 mg did not reduce heart rate in Arg389Arg homozygotes at all. Interestingly, the immediate response to carvedilol did not differ between genotypes. The Arg389Gly polymorphism has a major impact on the heart-rate response to carvedilol (but not bisoprolol) in patients with heart failure plus atrial fibrillation.

Publication types

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

MeSH terms

  • Adrenergic beta-1 Receptor Antagonists / administration & dosage
  • Adrenergic beta-1 Receptor Antagonists / pharmacokinetics
  • Aged
  • Atrial Fibrillation* / complications
  • Atrial Fibrillation* / drug therapy
  • Atrial Fibrillation* / genetics
  • Bisoprolol* / administration & dosage
  • Bisoprolol* / pharmacokinetics
  • Carbazoles* / administration & dosage
  • Carbazoles* / pharmacokinetics
  • Carvedilol
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Female
  • Heart Failure* / complications
  • Heart Failure* / drug therapy
  • Heart Failure* / genetics
  • Heart Rate* / drug effects
  • Heart Rate* / genetics
  • Humans
  • Male
  • Polymorphism, Single Nucleotide
  • Propanolamines* / administration & dosage
  • Propanolamines* / pharmacokinetics
  • Receptors, Adrenergic, beta-1 / genetics*
  • Treatment Outcome

Substances

  • Adrenergic beta-1 Receptor Antagonists
  • Carbazoles
  • Propanolamines
  • Receptors, Adrenergic, beta-1
  • Carvedilol
  • Bisoprolol