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Pharmacokinetics and metabolism of orally administered firocoxib, a novel second generation coxib, in horses.
Abstract: The primary objective of this study was to determine the pharmacokinetic profile of firocoxib, a novel second generation coxib, in horses. Horses were administered either a single oral or intravenous dose of firocoxib at 0.1 mg/kg in a two-period crossover study with 12 animals. The dosage was based on previously determined pharmacodynamic parameters. Oral firocoxib was well absorbed with an average bioavailability (absolute) of 79% and a Cmax of 75 ng/mL at 3.9 h. The average elimination half-life was 30 h. Following intravenous administration the average Cmax was 210 ng/mL and the elimination half-life was 34 h. The area under the curve [AUC(0-tlast)] was 1.8 microg.h/mL for the oral dose and 2.3 microg.h/mL for the intravenous dose. Firocoxib was widely distributed with a volume of distribution value of 1.7 L/kg for the intravenous dose. Biotransformation of firocoxib was via dealkylation and glucuronidation to inactive metabolites, namely descyclopropylmethylfirocoxib and its glucuronide conjugate. Urinary excretion was the major route of elimination, and the clearance rate was 37 mL/h/kg.
Publication Date: 2007-05-03 PubMed ID: 17472652DOI: 10.1111/j.1365-2885.2007.00840.xGoogle Scholar: Lookup The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
- Randomized Controlled Trial
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 study investigates how firocoxib, a second-generation coxib medication, is absorbed and metabolized in horses. By looking at both oral and intravenous administration, the researchers found this drug to be well-absorbed and metabolized through dealkylation and glucuronidation, with the majority of it being excreted through urine.
Study Design and Objectives
- The study aimed to determine the pharmacokinetic profile of firocoxib in horses. Pharmacokinetics is the study of how an organism affects a drug. It looks at the absorption, distribution, metabolism, and excretion of the drug.
- The researchers conducted a two-period crossover study involving 12 horses. In this study design, each horse would receive two treatments – one oral and one intravenous – at different times, allowing each horse to serve as its own control.
Administration and Dosage of Firocoxib
- The horses were given a single dose of firocoxib, whether orally or intravenously, at a dosage of 0.1 mg/kg. This dosage was calculated based on previously determined pharmacodynamic parameters, which study the effects of the drug on the body.
Findings on Absorption and Distribution
- Firocoxib was found to be well-absorbed with an average bioavailability (a measure of how much and how quickly a drug reaches the body’s systemic circulation) of 79% for the oral dose.
- The maximum concentration (Cmax) of the drug reached in the blood was 75 ng/mL after 3.9 hours for the oral dose, while it was 210 ng/mL after the intravenous dose.
- The drug was shown to have a wide distribution in the body, with its volume of distribution value being 1.7 L/kg following the intravenous dose.
Metabolism and Excretion of Firocoxib
- Firocoxib was metabolized through dealkylation and glucuronidation processes to inactive metabolites, specifically descyclopropylmethylfirocoxib and its glucuronide conjugate.
- The main route of elimination for firocoxib was urinary excretion. The clearance rate, or the volume of blood from which the drug is removed per unit time, was 37 mL/h/kg.
Cite This Article
APA
Kvaternick V, Pollmeier M, Fischer J, Hanson PD.
(2007).
Pharmacokinetics and metabolism of orally administered firocoxib, a novel second generation coxib, in horses.
J Vet Pharmacol Ther, 30(3), 208-217.
https://doi.org/10.1111/j.1365-2885.2007.00840.x Publication
Researcher Affiliations
- Pharmacokinetics and Drug Metabolism, Merial Limited, North Brunswick, NJ 08902, USA. valerie.kvaternick@merial.com
MeSH Terms
- 4-Butyrolactone / administration & dosage
- 4-Butyrolactone / analogs & derivatives
- 4-Butyrolactone / blood
- 4-Butyrolactone / pharmacokinetics
- Administration, Oral
- Animals
- Area Under Curve
- Cross-Over Studies
- Cyclooxygenase 2 Inhibitors / administration & dosage
- Cyclooxygenase 2 Inhibitors / blood
- Cyclooxygenase 2 Inhibitors / pharmacokinetics
- Female
- Horses / metabolism
- Injections, Intravenous
- Male
- Sulfones / administration & dosage
- Sulfones / blood
- Sulfones / pharmacokinetics
Citations
This article has been cited 14 times.- Mercer MA, Davis JL, McKenzie HC. The Clinical Pharmacology and Therapeutic Evaluation of Non-Steroidal Anti-Inflammatory Drugs in Adult Horses. Animals (Basel) 2023 May 10;13(10).
- Fadel C, Giorgi M. Synopsis of the pharmacokinetics, pharmacodynamics, applications, and safety of firocoxib in horses. Vet Anim Sci 2023 Mar;19:100286.
- Flood J, Stewart AJ. Non-Steroidal Anti-Inflammatory Drugs and Associated Toxicities in Horses. Animals (Basel) 2022 Oct 26;12(21).
- Solà J, Menargues À, Homedes J, Salichs M, Serafini MT, Encina G. Comparative In vitro Metabolism of Enflicoxib in Dogs, Rats, and Humans: Main Metabolites and Proposed Metabolic Pathways. Drug Metab Lett 2021;14(3):206-218.
- Donnell JR, Frisbie DD. Use of firocoxib for the treatment of equine osteoarthritis. Vet Med (Auckl) 2014;5:159-168.
- Coetzee JF, Sidhu PK, Seagen J, Schieber T, Kleinhenz K, Kleinhenz MD, Wulf LW, Cooper VL, Mazloom R, Jaberi-Douraki M, Lechtenberg K. Transmammary delivery of firocoxib to piglets reduces stress and improves average daily gain after castration, tail docking, and teeth clipping1. J Anim Sci 2019 Jul 2;97(7):2750-2768.
- Mendoza FJ, Serrano-Rodriguez JM, Perez-Ecija A. Pharmacokinetics of meloxicam after oral administration of a granule formulation to healthy horses. J Vet Intern Med 2019 Mar;33(2):961-967.
- Whitfield-Cargile CM, Chamoun-Emanuelli AM, Cohen ND, Richardson LM, Ajami NJ, Dockery HJ. Differential effects of selective and non-selective cyclooxygenase inhibitors on fecal microbiota in adult horses. PLoS One 2018;13(8):e0202527.
- Serra MB, Barroso WA, da Silva NN, Silva SDN, Borges ACR, Abreu IC, Borges MODR. From Inflammation to Current and Alternative Therapies Involved in Wound Healing. Int J Inflam 2017;2017:3406215.
- Reddyjarugu B, Pavek T, Southard T, Barry J, Singh B. Analgesic Efficacy of Firocoxib, a Selective Inhibitor of Cyclooxygenase 2, in a Mouse Model of Incisional Pain. J Am Assoc Lab Anim Sci 2015 Jul;54(4):405-10.
- Barton MH, Paske E, Norton N, King D, Giguère S, Budsberg S. Efficacy of cyclo-oxygenase inhibition by two commercially available firocoxib products in horses. Equine Vet J 2014 Jan;46(1):72-5.
- Shapiro AJ, Kimble B, Hulst F, Herrin KV, Marschner C, Chen CJ, Govendir M. Pharmacokinetic profile of oral firocoxib in the koala (Phascolarctos cinereus). PLoS One 2025;20(9):e0332448.
- Buzelato Carli I, Fielding L. Long-Term Firocoxib Use in Horses. J Vet Intern Med 2025 May-Jun;39(3):e70117.
- Araújo RA, Sales NAA, Basile RC, Feringer-Junior WH, Apparício M, Ferraz GC, Queiroz-Neto A. Safety Assessment of an Oral Therapeutic Dose of Firocoxib on Healthy Horses. Vet Sci 2023 Aug 22;10(9).
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