Ligand bias prevents class equality among beta-blockers

Curr Opin Pharmacol. 2014 Jun;16:50-7. doi: 10.1016/j.coph.2014.03.002. Epub 2014 Mar 27.

Abstract

β-Blockers are used for a wide range of diseases from hypertension to glaucoma. In some diseases/conditions all β-blockers are effective, while in others only certain subgroups are therapeutically beneficial. The best-documented example for only a subset of β-blockers showing clinical efficacy is in heart failure, where members of the class have ranged from completely ineffective, to drugs of choice for treating the disease. Similarly, β-blockers were tested in murine asthma models and two pilot clinical studies. A different subset was found to be effective for this clinical indication. These findings call into question the current system of classifying these drugs. To consider 'β-blockers', as a single class is misleading when considering their rigorous pharmacological definition and their appropriate clinical application.

Publication types

  • Review

MeSH terms

  • Adrenergic beta-Antagonists* / classification
  • Adrenergic beta-Antagonists* / pharmacology
  • Adrenergic beta-Antagonists* / therapeutic use
  • Animals
  • Asthma / drug therapy
  • Asthma / metabolism
  • Humans
  • Ligands
  • Receptors, Adrenergic, beta-2 / metabolism*
  • Signal Transduction

Substances

  • Adrenergic beta-Antagonists
  • Ligands
  • Receptors, Adrenergic, beta-2