Detection and pharmacokinetics of grapiprant following oral administration to exercised Thoroughbred horses.
Abstract: Traditional therapeutic options for the treatment of lameness associated with inflammation in performance horses include administration of cyclooxygenase enzyme inhibiting non-steroidal anti-inflammatory drugs (NSAID). As long-term use of these drugs can adversely impact the health of the horse, anti-inflammatories with a more favorable safety profile are warranted. Grapiprant is a newly approved non-cyclooxygenase inhibiting NSAID that has demonstrated efficacy and safety in other species and which may be a valuable alternative to traditional NSAIDs used in the horse. The objectives of the current study were to describe drug concentrations and the pharmacokinetics of grapiprant in exercised Thoroughbred horses and to develop an analytical method that could be used to regulate its use in performance horses. To that end, grapiprant, at a dose of 2 mg/kg was administered orally to 12 exercised Thoroughbred horses. Blood and urine samples were collected prior to and for up to 96 hours post drug administration. Drug concentrations were measured using liquid chromatography-tandem mass spectrometry. Grapiprant remained above the LOQ of the assay (0.005 ng/mL) in serum for 72 hours post administration and urine concentrations were above the LOQ until 96 hours. The Cmax , Tmax and elimination half-life were 31.9 ± 13.9 ng/mL, 1.5 ± 0.5 hours and 5.86 ± 2.46 hours, respectively. The drug was well tolerated in all horses at a dose of 2 mg/kg. Results support further study of this compound in horses. Furthermore, development of a highly sensitive analytical method demonstrate that this compound can be adequately regulated in performance horses.
Copyright © 2018 John Wiley & Sons, Ltd.
Publication Date: 2018-03-25 PubMed ID: 29575649DOI: 10.1002/dta.2378Google Scholar: Lookup
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- Journal Article
Summary
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The study explored the effectiveness and safety profile of grapiprant, a new non-steroidal anti-inflammatory drug (NSAID), on exercised Thoroughbred horses. It aimed to describe drug concentrations, the pharmacokinetics of grapiprant, and develop an analytical method for its usage regulation in performance horses.
Study Objective and Method
- The main objective of the research was to investigate the use of grapiprant, a newly approved non-cyclooxygenase inhibiting NSAID, as an alternative to traditional NSAIDs used in horses, particularly for cases of inflammation-related lameness in performance horses. The study also aimed to develop an analytical method to regulate its use.
- As part of the methodology, 12 exercised Thoroughbred horses were administered with 2 mg/kg of grapiprant orally. Blood and urine samples were collected before and up to 96 hours after drug administration.
Analysis and Results
- The analysis was done using liquid chromatography-tandem mass spectrometry in order to measure the drug concentrations. In serum, the grapiprant remained detectable for up to 72 hours post-administration, while in the urine it stayed detectable up to 96 hours.
- The maximum average concentration (Cmax) of the drug was found to be 31.9 ± 13.9 ng/mL. The time taken to reach Cmax (Tmax) was 1.5 ± 0.5 hours and the half-life of the drug was calculated to be around 5.86 ± 2.46 hours.
- Every horse well-tolerated the 2 mg/kg dose of grapiprant, suggesting a favorable safety profile for the drug among the population.
Conclusion and Further Research
- The results indicated that grapiprant could be a viable alternative to traditional NSAIDs for performance horses. The study also proposed a highly sensitive analytical method for the monitoring and regulation of this drug in horses.
- However, further investigations of grapiprant in horses are needed to comprehensively understand its potential therapeutic benefits and risks. Such studies could lead to safer treatment options for inflammation-induced lameness in performance horses.
Cite This Article
APA
Knych HK, Seminoff K, McKemie DS.
(2018).
Detection and pharmacokinetics of grapiprant following oral administration to exercised Thoroughbred horses.
Drug Test Anal.
https://doi.org/10.1002/dta.2378 Publication
Researcher Affiliations
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, California.
- Department of Veterinary Molecular Biosciences, School of Veterinary Medicine, University of California, Davis, California.
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, California.
- K.L. Maddy Equine Analytical Chemistry Laboratory, School of Veterinary Medicine, University of California, Davis, California.
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