Dihydrolevobunolol is a potent ocular beta-adrenoceptor antagonist

J Ocul Pharmacol. Spring 1987;3(1):11-5. doi: 10.1089/jop.1987.3.11.

Abstract

The ocular beta-adrenoceptor antagonist activity of dihydrolevobunolol (DHLB), the major ocular and systemic metabolite of levobunolol was investigated by determining its ability to block isoproterenol-induced ocular hypotension in normotensive rabbits. Topically-applied 0.001% and 0.01% DHLB virtually abolished the response to isoproterenol, indicating a beta-blocking potency similar to that of timolol. Thus, the ocular metabolism of levobunolol leads to the formation of a highly potent beta-adrenoceptor antagonist that may contribute to its clinical efficacy.

MeSH terms

  • Adrenergic beta-Antagonists / pharmacology*
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Eye / drug effects*
  • Female
  • Intraocular Pressure / drug effects
  • Isoproterenol / antagonists & inhibitors
  • Isoproterenol / pharmacology
  • Levobunolol / analogs & derivatives*
  • Levobunolol / pharmacology
  • Male
  • Rabbits

Substances

  • Adrenergic beta-Antagonists
  • dihydrobunolol
  • Levobunolol
  • Isoproterenol