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Journal of veterinary pharmacology and therapeutics2002; 24(6); 405-414; doi: 10.1046/j.1365-2885.2001.00364.x

Continuous measurement of caffeine and two metabolites in blood and skeletal muscle of unrestrained adult horses by semi-automated in vivo microdialysis.

Abstract: Concentrations of caffeine (CA) and two metabolites were measured simultaneously in venous blood and splenius muscle of adult horses using a semi-automated in vivo microdialysis sampling technique. Dialysates from muscle and jugular vein were collected continuously for 48 h and drug levels were determined by high performance liquid chromatography (HPLC). Following i.v. injection, CA (3 mg/kg) attained a peak blood level of nearly 5400 +/- 600 ng/mL and decreased with a half-life of 15.3 +/- 0.7 h. Pharmacokinetic and statistical comparisons between CA concentrations in jugular dialysates and plasma samples revealed no significant differences between these sampling techniques. However, measurements in muscle and blood revealed unexpected pharmacokinetic differences, including significantly elevated concentrations of CA in muscle for 4 h following drug administration. In contrast, the CA metabolites theophylline (TP) and theobromine (TB) exhibited delayed appearances in muscle and blood with peak concentrations of 300 +/- 60 ng/mL (TP) and 150 +/- 50 ng/mL (TB) detected in both tissues 1 day following CA administration. This study demonstrates that our novel semi-automated microdialysis procedure for continuous monitoring of drug and metabolite levels may be useful for related studies in other domesticated large animal species.
Publication Date: 2002-03-21 PubMed ID: 11903871DOI: 10.1046/j.1365-2885.2001.00364.xGoogle Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't
  • Validation Study

Summary

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The research studies the levels of caffeine and its two metabolites in the blood and muscles of adult horses using a semi-automatic microdialysis technique. It sheds light on the different pharmacokinetic behavior of caffeine and its metabolites in various tissues which can have implications for drug testing in large domesticated animals.

Objective and Methodology:

  • The research aimed to measure the concentrations of caffeine, and its two metabolites, in the blood and muscle of adult horses.
  • The study made use of a semi-automated in vivo microdialysis process to continuously sample from muscle tissues and the jugular vein for 48 hours.
  • Levels of the substances were then determined using high-performance liquid chromatography (HPLC).

Findings:

  • Following an intravenous injection of caffeine, a peak blood level averaging 5400 +/- 600 ng/mL was reached.
  • The caffeine level then decreased with a half-life of roughly 15.3 +/- 0.7 hours.
  • Contrary to expectations, noticeable pharmacokinetic differences were noticed between the muscle and blood samplings.
  • The muscle tissues showed substantially higher concentrations of caffeine for 4 hours after drug administration.
  • However, the measured levels of the caffeine metabolites, theophylline and theobromine, appeared delayed in both muscle and blood samples, reaching peak concentrations 1 day after caffeine administration.

Significance:

  • The findings from the study highlight the dynamic and varied pharmacokinetic behavior of caffeine and its metabolites in different tissues within the body.
  • The novel semi-automated microdialysis procedure used presents potential applications in continuous drug and metabolite level monitoring for large domesticated animals.

Cite This Article

APA
Chou CC, Webb AI, Brown MP, Gronwall RR, Vickroy TW. (2002). Continuous measurement of caffeine and two metabolites in blood and skeletal muscle of unrestrained adult horses by semi-automated in vivo microdialysis. J Vet Pharmacol Ther, 24(6), 405-414. https://doi.org/10.1046/j.1365-2885.2001.00364.x

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 24
Issue: 6
Pages: 405-414

Researcher Affiliations

Chou, C C
  • Department of Physiological Sciences, College of Veterinary Medicine, University of Florida, Gainesville, FL 32610-0144, USA.
Webb, A I
    Brown, M P
      Gronwall, R R
        Vickroy, T W

          MeSH Terms

          • Animals
          • Area Under Curve
          • Caffeine / blood
          • Caffeine / pharmacokinetics
          • Central Nervous System Stimulants / blood
          • Central Nervous System Stimulants / pharmacokinetics
          • Chromatography, High Pressure Liquid / veterinary
          • Female
          • Horses / metabolism
          • Injections, Intravenous / veterinary
          • Microdialysis / instrumentation
          • Microdialysis / standards
          • Microdialysis / veterinary
          • Muscle, Skeletal / metabolism
          • Reproducibility of Results
          • Theobromine / metabolism
          • Theophylline / metabolism

          Citations

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