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Veterinary and animal science2023; 19; 100286; doi: 10.1016/j.vas.2023.100286

Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses.

Abstract: According to in vitro and in vivo investigations, firocoxib (FX), a second-generation coxib, is a highly selective COX-2 inhibitor in horses. With a COX-1/COX-2 IC50 ratio of 643 in horses, FX spares the COX-1 inhibitory effects. It is approved for the treatment of musculoskeletal problems and lameness in horses and dogs with osteoarthritis (OA). For the treatment of OA in horses, both an injectable formulation for IV administration at a dose of 0.09 mg/kg for five days and an oral paste formulation at a dose of 0.1 mg/kg for 14 days are licensed. Numerous analytical methods were reported in the literature to quantify FX in biological fluids, using HPLC and LC-MS. FX presents remarkable pharmacokinetics and pharmacodynamics compared to other coxibs. It has an oral bioavailability of 80% or higher and is effectively absorbed by horses. Its volume of distribution is around 2 L/kg, and it is slowly eliminated. Due to the long elimination half-life (around 2 days), which allows a once daily dosing, a single 0.3 mg/kg loading dose has been recommended. This enables the establishment of steady-state drug concentrations within 24 h, making it appropriate for acute treatment as well. Its IC80 is equal to 103 ng/mL in whole blood and, with an EC50 of 27 ng/mL, it has the highest affinity for its receptor compared to the other commonly administered NSAIDs in horses.
© 2023 The Author(s).
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Publication Date: 2023-01-11 PubMed ID: 36684818PubMed Central: PMC9852958DOI: 10.1016/j.vas.2023.100286Google Scholar: Lookup
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Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

This research article explores the effects, uses, and safety of Firocoxib in horses. Firocoxib is a selective COX-2 inhibitor drug primarily used to treat pain caused by musculoskeletal problems and osteoarthritis in horses and dogs.

Overview of Firocoxib

  • Firocoxib (FX) is a second-generation coxib, a type of drug that selectively inhibits cyclooxygenase-2 (COX-2) enzymes. These enzymes contribute to inflammation and pain in the body.
  • FX is distinguished by an IC ratio of 643 towards COX-1/COX-2 in horses. This means it mainly inhibits COX-2 enzymes, sparing COX-1 and reducing potential harmful effects on the stomach, kidney, and clotting system.
  • It is approved for use in dogs and horses to treat musculoskeletal issues and lameness specifically arising from osteoarthritis.

Usage and Administration

  • For horses, there are two licensed routes of administration: by injection and orally.
  • The injection is dosed at 0.09 mg/kg for five days, and the oral paste is dosed at 0.1 mg/kg for 14 days when treating osteoarthritis.

Pharmacokinetics and Pharmacodynamics

  • FX shows distinctive pharmacokinetics and pharmacodynamics compared to other coxibs.
  • Firocoxib’s oral bioavailability is high (above 80%), meaning the majority of the drug is absorbed into the horses’ system effectively.
  • The drug is distributed throughout the body with a volume of distribution equivalent to 2 L/kg, and it’s slowly eliminated from the body.
  • Firocoxib has a long half-life of around two days, allowing for once-daily dosing.

Other Significant Information

  • Single loading dose of 0.3 mg/kg is recommended due to its long elimination half-life. It establishes steady-state drug concentrations within 24 hours, which indicates it can be used for acute treatments as well.
  • The medicine’s IC (the concentration needed to inhibit binding by 50%) is 103 ng/mL in whole blood. Along with its effective concentration (EC) of 27 ng/mL, Firocoxib has the highest affinity for its receptor compared to other NSAIDs used in horses.

Cite This Article

APA
Fadel C, Giorgi M. (2023). Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses. Vet Anim Sci, 19, 100286. https://doi.org/10.1016/j.vas.2023.100286

Publication

Veterinary and animal science
ISSN: 2451-943X
NlmUniqueID: 101694897
Country: Netherlands
Language: English
Volume: 19
Pages: 100286

Researcher Affiliations

Fadel, Charbel
  • Department of Veterinary Medicine, University of Sassari, Sassari, Italy.
Giorgi, Mario
  • Department of Veterinary Medicine, University of Sassari, Sassari, Italy.
  • Department of Veterinary Sciences, University of Pisa, Pisa, Italy.

Conflict of Interest Statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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Citations

This article has been cited 3 times.
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