COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: an in vitro analysis

Pharmacol Res. 2005 Oct;52(4):302-6. doi: 10.1016/j.phrs.2005.04.004.

Abstract

We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays. As expected, comparison of IC50 indicated that meloxicam and carprofen are more selective inhibitors of COX-2 than phenylbutazone and flunixin; meloxicam was the most advantageous for horses of four NSAIDs examined. However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50. We therefore propose that the selectivity of NSAIDs should be assessed at the 80% as well as 50% inhibition level.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Carbazoles / pharmacology
  • Clonixin / analogs & derivatives
  • Clonixin / pharmacology
  • Cyclooxygenase Inhibitors / pharmacology*
  • Dinoprostone / blood
  • Female
  • Horses*
  • In Vitro Techniques
  • Male
  • Meloxicam
  • Phenylbutazone / pharmacology
  • Thiazines / pharmacology
  • Thiazoles / pharmacology
  • Thromboxane B2 / blood

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Carbazoles
  • Cyclooxygenase Inhibitors
  • Thiazines
  • Thiazoles
  • flunixin
  • Thromboxane B2
  • carprofen
  • Phenylbutazone
  • Dinoprostone
  • Clonixin
  • Meloxicam