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Detection and Pharmacokinetics of Etoricoxib in Thoroughbred Horses
Affiliation:1. Equine Forensic Unit, Central Veterinary Research Laboratory, Dubai, United Arab Emirates;2. School of Forensic and Applied Sciences, College of Science and Technology, University of Central Lancashire, Preston, UK;1. Faculty of Veterinary Medicine, Department of Anatomy and Embryology, Alexandria University, Alexandria, Egypt;2. Faculty of Medicine, School of Veterinary Medicine and Science, University of Nottingham, Nottingham, UK;3. Faculty of Veterinary Medicine, Department of Surgery, Damanhur University, Damanhur, Egypt;4. Faculty of Veterinary Medicine, Department of Surgery, Alexandria University, Alexandria, Egypt;1. Department of Anatomy and Embryology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt;2. Department of Surgery, Anesthesiology and Radiology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt;3. Department of Theriogenology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt;1. Faculty of Veterinary Medicine, Sub-Department of Pathophysiology, Department of Preclinical Veterinary Sciences, University of Life Sciences, Lublin, Poland;2. Faculty of Veterinary Medicine, Department and Clinic of Animal Surgery, University of Life Sciences, Lublin, Poland;1. Department of Veterinary Sciences, Biochemistry Unit, University of Messina, Polo Universitario dell’Annunziata, Messina, Italy;2. Department of Clinical and Experimental Medicine, University of Messina, Policlinico Universitario, Messina, Italy;3. Department of Veterinary Sciences, Physiology Unit, University of Messina, Polo Universitario dell’Annunziata, Messina, Italy;1. Department of Animal Science, Berry College, Mount Berry, GA;2. Department of Animal Science, University of Tennessee, Knoxville, TN;3. Department of Large Animal Clinical Sciences, University of Tennessee, Knoxville, TN;1. Instituto de Virología e Innovaciones Tecnológicas (IVIT), Instituto Nacional de Tecnología Agropecuaria (INTA), Buenos Aires, Argentina;2. Cátedra de Enfermedades Infecciosas, Escuela de Veterinaria, Universidad del Salvador, Buenos Aires, Argentina;3. Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) scientific career, Buenos Aires, Argentina;4. Dirección de Remonta y Veterinaria, Ejército Argentino, Buenos Aires, Argentina;5. Department of Infectious and Parasitic Diseases, Veterinary Virology and Animal Viral Diseases, FARAH Center, Faculty of Veterinary Medicine, University of Liege (B-4000), Liege, Belgium
Abstract:Etoricoxib, a selective inhibitor of cyclooxygenase-2, is used in the treatment of many inflammatory diseases and dental pain in humans. The aim of this study was to determine the pharmacokinetics and metabolism of etoricoxib in horses. Six horses weighing an average of 475 ± 25 kg were administered a single oral dose of etoricoxib at 1 mg/kg body weight. The results show that the drug reached a maximum concentration of 505.2 ± 67.8 ng/mL in 48 minutes after administration. The elimination half-life was calculated to be 10.20 ± 1.30 hours. Mass spectrometric analysis confirmed that etoricoxib is metabolized in horses via the oxidation of its 6′-methyl group to form a hydroxyl methyl etoricoxib which can further be oxidized to form either an acid or be glucuronidated. In addition, the 1′-N terminal of 6′-hydroxymethyl metabolite is oxidized to form the corresponding 1′-N oxide metabolite. The present results have clearly demonstrated that etoricoxib is mainly excreted in urine as metabolites. From these data, it is also possible to postulate a detection time for the metabolites which in turn can assist in the control of illegal use of the drug in horse racing.
Keywords:Elimination  Etoricoxib  Horses  Metabolism  Pharmacokinetics
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