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Pharmacokinetics and disposition of flupirtine in the horse.
Abstract: Flupirtine (FLU) is a non-opioid analgesic drug, with no antipyretic or anti-inflammatory effects, used in the treatment of a wide range of pain states in human beings. It does not induce the side effects associated with the classical drugs used as pain relievers. The aim of this study was to evaluate the pharmacokinetic profiles of FLU after IV and PO administration in healthy horses. Six mixed breed adult mares were randomly assigned to two treatment groups using an open, single-dose, two-treatment, two-phase, paired, cross-over design (2 × 2 Latin-square). Group 1 (n = 3) received a single dose of 1 mg/kg of FLU injected IV into the jugular vein. Group 2 (n = 3) received FLU (5 mg/kg) via nasogastric tube. The animals then swapped groups after a 1-week wash-out period and the doses were repeated. Blood samples (5 mL) were collected at 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 24, 36 and 48 h and plasma was then analysed by a validated HPLC method. Some mild and transient adverse effects (that spontaneously resolved within 5 min) were observed in 2/6 animals after IV administration. No adverse effects were noticed in the PO administration group. After IV and PO administrations, FLU was detectable in plasma for up to 36 h. The mean elimination half-life was longer after PO (10.27 h) than after IV (3.02 h) administration. The oral bioavailability was 71.4 ± 33.1%. After compartmental simulation/modelling, an oral dose of 2.6 mg/kg was calculated to give Cmax and AUC values in horses similar to those reported in humans after a clinical dose administration with a theoretical FLU effective plasma concentration of 187 ng/mL. These findings may form the basis for further studies concerning this active ingredient in equine medicine.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication Date: 2015-08-20 PubMed ID: 26681139DOI: 10.1016/j.tvjl.2015.08.019Google 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
- Research Support
- Non-U.S. Gov't
- Adverse Effects
- Analgesia
- Animal Health
- Animal Studies
- Blood Analysis
- Clinical Study
- Drug
- Equine Health
- Equine Medicine
- High-performance Liquid Chromatography (HPLC)
- Horses
- Intravenous Administration
- Oral Administration
- Pain Management
- Pharmacodynamics
- Pharmacokinetics
- Plasma
- Veterinary Medicine
- Veterinary Practice
- Veterinary Research
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 investigates the effects and potential use of the pain-relieving drug flupirtine in horses, finding that it can adequately be administered orally or intravenously and is present in the blood up to 36 hours after administration.
Research Overview
- The study’s aim was to understand the pharmacokinetics of Flupirtine, a non-opioid painkiller, when administered either intravenously (IV) or orally (PO) in healthy horses.
- The experiment utilized a total of six adult mares, which were split into two distinct groups. Three horses formed Group 1, receiving a single dose of Flupirtine via IV, whereas the remaining three horses in Group 2 received the drug orally.
Study Design
- This research used a 2 × 2 Latin square design, which means that every treatment was tested on every subject. The two treatments involved IV and PO administration.
- The horses were subjected to a week-long “wash-out” period before swapping treatment groups. The same dosing procedure was repeated, giving each horse both treatments during two separate periods.
- Blood samples were taken at regular intervals (from 0.25h up to 48h) after administration of the drug. Each sample was then analysed using a process called High-Performance Liquid Chromatography (HPLC).
Findings
- Some mild and transient side effects were observed in 2 out of 6 horses after IV administration. However, these side effects resolved spontaneously within 5 minutes.
- There were no observable adverse effects present in the horses that received the drug orally.
- Results showed that Flupirtine was detectable in the horse’s plasma for up to 36 hours after both IV and PO administrations.
- Interestingly, the mean elimination half-life was significantly longer when the drug was administered orally rather than intravenously.
- The study also found that the bioavailability of the drug – the percentage of the drug that successfully enters the bloodstream – was approximately 71.4% ± 33.1% when administered orally.
Implications
- The results obtained from the compartmental simulation/modelling suggest, at an oral dosage of 2.6 mg/kg, the Flupirtine concentration values obtained would be similar to those reported in humans after a clinical dose.
- These findings build a foundation for potential further research into Flupirtine’s use in equine medicine.
Cite This Article
APA
Giorgi M, De Vito V, Poapolathep A, Rychshanova R, Sgorbini M, Owen H.
(2015).
Pharmacokinetics and disposition of flupirtine in the horse.
Vet J, 208, 76-80.
https://doi.org/10.1016/j.tvjl.2015.08.019 Publication
Researcher Affiliations
- Department of Veterinary Sciences, University of Pisa, Via Livornese (lato monte), San Piero a Grado, Italy. Electronic address: mgiorgi@vet.unipi.it.
- Department of Veterinary Sciences, University of Pisa, Via Livornese (lato monte), San Piero a Grado, Italy.
- Department of Veterinary Pharmacology, Faculty of Veterinary Medicine, University of Kasetsart, Bangkok, Thailand.
- Veterinary School, Kostanay State A. Baitursynov University, Kostanay, Kazakhstan.
- Department of Veterinary Sciences, University of Pisa, Via Livornese (lato monte), San Piero a Grado, Italy.
- School of Veterinary Science, The University of Queensland, Gatton Campus, Gatton, Queensland 4343, Australia.
MeSH Terms
- Aminopyridines / blood
- Aminopyridines / pharmacokinetics
- Analgesics / blood
- Analgesics / pharmacokinetics
- Analgesics, Non-Narcotic / blood
- Analgesics, Non-Narcotic / pharmacokinetics
- Animals
- Cross-Over Studies
- Dose-Response Relationship, Drug
- Female
- Horses / metabolism
- Injections, Intravenous / veterinary
- Intubation, Gastrointestinal / veterinary
- Random Allocation
Citations
This article has been cited 2 times.- Fadel C, Łebkowska-Wieruszewska B, Sartini I, Lisowski A, Poapolathep A, Giorgi M. Robenacoxib pharmacokinetics in sheep following oral, subcutaneous, and intravenous administration. J Vet Pharmacol Ther 2022 Nov;45(6):550-557.
- Patil MA, Matter BA, Raol YH, Bourne DWA, Kelley RA, Kompella UB. Brain Distribution and Metabolism of Flupirtine, a Nonopioid Analgesic Drug with Antiseizure Effects, in Neonatal Rats. Pharmaceutics 2018 Dec 16;10(4).
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