Metabolism and elimination of the catechol-o-methyltransferase inhibitor tolcapone in the horse

Drug Test Anal. 2019 Apr;11(4):578-585. doi: 10.1002/dta.2531. Epub 2018 Dec 3.

Abstract

The metabolism of the masking agent tolcapone in the horse has been investigated. This substance was found to have undergone various chemical transformations that produced a large variety of phase I metabolites, as well as glucuronide and sulfate conjugation. Confirmation of the presence of tolcapone and the 3-O-methylated metabolite in the blood samples collected up to 240 minutes and in urine obtained up to 24 hours, was successfully conducted using both gas chromatography- and liquid chromatography-tandem mass spectrometry techniques. The 3-O-methyl tolcapone is the better marker to use in a screening method because, in comparison to tolcapone, we have found that this substance offers superior chromatographic performance that should potentially give a lower limit of detection.

Keywords: equine drug metabolism; equine drug testing; mass spectrometry.

MeSH terms

  • Animals
  • Catechol O-Methyltransferase Inhibitors / blood*
  • Catechol O-Methyltransferase Inhibitors / metabolism
  • Catechol O-Methyltransferase Inhibitors / urine*
  • Chromatography, High Pressure Liquid
  • Drug Monitoring
  • Gas Chromatography-Mass Spectrometry
  • Horses / blood*
  • Horses / metabolism
  • Horses / urine*
  • Methylation
  • Substance Abuse Detection
  • Tolcapone / blood*
  • Tolcapone / metabolism
  • Tolcapone / urine*

Substances

  • Catechol O-Methyltransferase Inhibitors
  • Tolcapone