Pharmacokinetics and selected pharmacodynamics of romifidine following low-dose intravenous administration in combination with exercise to quarter horses.
Abstract: Romifidine is an alpha-2 adrenergic agonist used for sedation and analgesia in horses. As it is a prohibited substance, its purported use at low doses in performance horses necessitates further study. The primary goal of the study reported here was to describe the serum concentrations and pharmacokinetics of romifidine following low-dose administration immediately prior to exercise, utilizing a highly sensitive liquid chromatography-tandem mass spectrometry assay that is currently employed in many drug testing laboratories. An additional objective was to describe changes in heart rate and rhythm following intravenous administration of romifidine followed by exercise. Eight adult Quarter Horses received a single intravenous dose of 5 mg (0.01 mg/kg) romifidine followed by 1 h of exercise. Blood samples were collected and drug concentrations measured at time 0 and at various times up to 72 h. Mean ± SD systemic clearance, steady-state volume of distribution and terminal elimination half-life were 34.1 ± 6.06 mL/min/kg and 4.89 ± 1.31 L/kg and 3.09 ± 1.18 h, respectively. Romifidine serum concentrations fell below the LOQ (0.01 ng/mL) and the LOD (0.005 ng/mL) by 24 h postadministration. Heart rate and rhythm appeared unaffected when a low dose of romifidine was administered immediately prior to exercise.
© 2017 John Wiley & Sons Ltd.
Publication Date: 2017-01-17 PubMed ID: 28097665DOI: 10.1111/jvp.12395Google Scholar: Lookup
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Summary
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The research examines the behavior and impact of a low dosage of romifidine, a drug used for sedation and pain relief in horses, when administered to them before engaging in physical activity.
Research Objectives and Methodology
- The study aimed to examine the serum concentrations and pharmacokinetics of romifidine in horses when administered at low dosage and immediately before exercise. The researchers employed a liquid chromatography-tandem mass spectrometry assay, a highly efficient method for detecting target substances, for this investigation.
- The second objective of the research was to analyze any changes in the horses’ heart rate and rhythm after the administration of the drug.
- The research involved eight adult Quarter Horses who each received a single intravenous dose of 5 mg (0.01 mg/kg) of romifidine, followed by an hour of physical activity.
- For data gathering, blood samples were collected from the horses at different times spanning up to 72 hours after the drug administration.
Results and Findings
- The study found that the systemic clearance rate of the drug, along with its steady-state volume of distribution and terminal elimination half-life, were 34.1 ± 6.06 mL/min/kg, 4.89 ± 1.31 L/kg, and 3.09 ± 1.18 hours, respectively.
- The researchers also observed that romifidine’s concentration in the horse’s serum dropped below its lower limit of quantification and detection by 24 hours after administration. This implies that the drug is metabolized and cleared out of the horse’s system relatively quickly.
- The research also found that the heart rate and rhythm of the horses appeared unaffected when a low dose of romifidine was administered immediately before physical activity. This indicates that the drug, in low doses, doesn’t impact the cardiovascular performance of performance horses.
Significance of the Study
- This study has significant implications in veterinary medicine, particularly in athletics involving horses, by demonstrating the pharmacokinetics of romifidine and its potential impact on their physical performance.
- This research also contributes to the body of knowledge in horse performance-drug interactions and informs policies regarding drug use in equine practices.
Cite This Article
APA
Knych HK, Stanley SD, McKemie DS, Steinmetz SJ.
(2017).
Pharmacokinetics and selected pharmacodynamics of romifidine following low-dose intravenous administration in combination with exercise to quarter horses.
J Vet Pharmacol Ther, 40(5), 569-574.
https://doi.org/10.1111/jvp.12395 Publication
Researcher Affiliations
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, CA, USA.
- Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, CA, USA.
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, CA, USA.
- Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, CA, USA.
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, CA, USA.
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, CA, USA.
MeSH Terms
- Administration, Intravenous / veterinary
- Adrenergic alpha-2 Receptor Agonists / pharmacokinetics
- Animals
- Dose-Response Relationship, Drug
- Heart Rate
- Horses / metabolism
- Imidazoles / pharmacokinetics
- Injections, Intravenous
- Physical Conditioning, Animal / physiology
Citations
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