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Pharmacology, pharmacokinetics, and behavioral effects of caffeine in horses.

Abstract: Caffeine (4 mg/kg) was given by rapid IV injection to 4 horses. Plasma concentrations of the drug peaked at 10 micrograms/ml and decreased rapidly at first, and then more slowly, with an apparent beta-phase half-life of 18.2 hours. Urinary concentrations of caffeine were remarkably consistent at about 3 times plasma values of the drug. Caffeine was detectable in both plasma and urine of the horses for up to 9 days after dosing. After oral administration, caffeine was absorbed poorly with an apparent bioavailability of 39%. Although blood concentrations of caffeine peaked rapidly after oral administration, its apparent plasma half-life by this route was about 42 hours. These observations identify the possible existence of a slowly absorbed pool of caffeine in the gastrointestinal tract after oral administration. When caffeine-treated horses were given fentanyl, the locomotor response to fentanyl was enhanced. This potentiation of the fentanyl response peaked at between 0 and 4 hours after dosing and was gone by 72 hours after caffeine dosing. The data indicate that the probability of behavioral stimulation due to caffeine by 72 hours after dosing may be small.
Publication Date: 1983-01-01 PubMed ID: 6824226
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research paper studied the effects and behavior of caffeine when injected or consumed orally by horses. The findings suggest that caffeine may affect the horses’ behavioral responses to certain stimuli like fentanyl, a potent opioid.

Experiment Methodology

  • Four horses were given a caffeine dose of 4 mg/kg through a rapid intravenous (IV) injection.
  • The plasma concentrations of caffeine were noted and the changes recorded over a period of time.
  • Urine tests were conducted to evaluate the amount of caffeine present.
  • In another segment of the experiment, oral administration of caffeine was done and its bioavailability and effects were studied.
  • Additionally, the impact of caffeine on the response to fentanyl, a potent opioid, was investigated.

Key Findings

  • After the quick IV injection, the plasma concentration of the drug peaked at 10 micrograms/ml and had an apparent beta-phase half-life of 18.2 hours.
  • The presence of caffeine in urine was roughly 3 times the plasma values and could be provided consistently.
  • Caffeine was detectable in the urine and plasma of horses for up to 9 days following the initial dose.
  • When administered orally, there was poor absorption of caffeine with an apparent bioavailability of only 39%.
  • Despite experiencing a rapid peak in blood concentrations following oral administration, the plasma half-life of caffeine was about 42 hours, indicating a possibility of slow absorption of caffeine in the gastrointestinal tract.
  • Caffeine-treated horses exhibited an enhanced locomotor response to fentanyl. The effect was highest within 0-4 hours of administering caffeine and disappeared after approximately 72 hours post dosing.
  • The behavioral stimulus due to caffeine seemed to significantly reduce 72 hours following the dosage.

Implications of the Study

  • The research provides important insights into how horses metabolize caffeine, which can have wide implications in equine health and sports medicine.
  • The potentiation of the fentanyl response by caffeine could imply possible interactions between caffeine and certain opioids in horses. Further research could explore the potential impacts of such drug interactions on horse health and behavior.
  • The difference in the absorption and half-life of caffeine based on the administration route (IV injection vs. oral) provides crucial information that can affect dosage decisions in clinical or investigative settings.

Cite This Article

APA
Greene EW, Woods WE, Tobin T. (1983). Pharmacology, pharmacokinetics, and behavioral effects of caffeine in horses. Am J Vet Res, 44(1), 57-63.

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 44
Issue: 1
Pages: 57-63

Researcher Affiliations

Greene, E W
    Woods, W E
      Tobin, T

        MeSH Terms

        • Administration, Oral
        • Animals
        • Behavior, Animal / drug effects
        • Caffeine / blood
        • Caffeine / metabolism
        • Caffeine / pharmacology
        • Drug Synergism
        • Female
        • Fentanyl / pharmacology
        • Half-Life
        • Horses / metabolism
        • Horses / physiology
        • Kinetics
        • Locomotion / drug effects
        • Male

        Citations

        This article has been cited 1 times.
        1. Delfiol DJ, Oliveira-Filho JP, Casalecchi FL, Kievitsbosch T, Hussni CA, Riet-Correa F, Araujo JP Jr, Borges AS. Equine poisoning by coffee husk (Coffea arabica L.). BMC Vet Res 2012 Jan 12;8:4.
          doi: 10.1186/1746-6148-8-4pubmed: 22239973google scholar: lookup