Pharmacokinetics and disposition of flupirtine in the horse

Giorgi, M., De Vito, V., Poapolathep, A., Rychshanova R., Sgorbini, M. and Owen, H. (2015) Pharmacokinetics and disposition of flupirtine in the horse. Veterinary Journal, 208 76-80. doi:10.1016/j.tvjl.2015.08.019

Author Giorgi, M.
De Vito, V.
Poapolathep, A.
Rychshanova R.
Sgorbini, M.
Owen, H.
Title Pharmacokinetics and disposition of flupirtine in the horse
Journal name Veterinary Journal   Check publisher's open access policy
ISSN 1532-2971
Publication date 2015
Year available 2015
Sub-type Article (original research)
DOI 10.1016/j.tvjl.2015.08.019
Open Access Status Not Open Access
Volume 208
Start page 76
End page 80
Total pages 5
Place of publication London, United Kingdom
Publisher Elsevier
Language eng
Formatted 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.
Keyword Flupirtine
Pain reliever
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
School of Veterinary Science Publications
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