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Acepromazine pharmacokinetics: a forensic perspective.

Fiona I Schneiders1, Glenys K Noble, Raymond C Boston

  • 1School of Animal and Veterinary Sciences, Charles Sturt University, Locked Bag 588, Wagga Wagga, NSW 2678, Australia.

Veterinary Journal (London, England : 1997)
|April 27, 2012
PubMed
Summary

Acepromazine (ACP) is hard to detect in horses due to rapid metabolism. Its metabolite, 2-(1-hydroxyethyl)promazine sulphoxide (HEPS), is a reliable forensic marker, detectable for longer periods in blood and urine.

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Area of Science:

  • Veterinary Pharmacology
  • Forensic Toxicology
  • Analytical Chemistry

Background:

  • Acepromazine (ACP) is a widely used therapeutic agent in horses.
  • Its use is prohibited in competition animals due to doping concerns.
  • Rapid metabolism of ACP makes its detection challenging in equine samples.

Purpose of the Study:

  • To investigate the metabolite 2-(1-hydroxyethyl)promazine sulphoxide (HEPS) as a potential forensic marker for Acepromazine (ACP) use in horses.
  • To determine the pharmacokinetic profile of HEPS following intravenous administration of ACP.
  • To assess the feasibility of using HEPS for estimating ACP dosage in forensic cases.

Main Methods:

  • Intravenous administration of Acepromazine maleate to 12 racing-bred geldings.
  • Collection of blood and urine samples for 7 days post-administration.
  • Analysis of ACP and HEPS using liquid chromatography-mass spectrometry (LC-MS).

Main Results:

  • Acepromazine (ACP) was quantifiable in plasma for only up to 3 hours, with minimal excretion in urine.
  • The metabolite HEPS was detected in plasma for up to 24 hours and in urine for up to 144 hours.
  • A strong correlation was observed between peak plasma HEPS and its formation pharmacokinetics, enabling accurate modeling.

Conclusions:

  • Direct testing for Acepromazine (ACP) in forensic samples is ineffective for intravenous administration due to rapid metabolism.
  • HEPS is a valuable indicator of ACP use owing to its longer detection window in plasma and urine.
  • Urine-to-plasma concentration ratios of HEPS can potentially estimate the administered ACP dose.