Pharmacokinetic profile and behavioral effects of gabapentin in the horse

Terry, R. L., McDonnell, S. M., van Eps, A. W., Soma, L. R., Liu, Y., Uboh, C. E., Moate, P. J. and Driessen, B. (2010) Pharmacokinetic profile and behavioral effects of gabapentin in the horse. Journal of Veterinary Pharmacology and Therapeutics, 33 5: 485-494. doi:10.1111/j.1365-2885.2010.01161.x

Author Terry, R. L.
McDonnell, S. M.
van Eps, A. W.
Soma, L. R.
Liu, Y.
Uboh, C. E.
Moate, P. J.
Driessen, B.
Title Pharmacokinetic profile and behavioral effects of gabapentin in the horse
Journal name Journal of Veterinary Pharmacology and Therapeutics   Check publisher's open access policy
ISSN 0140-7783
Publication date 2010-10
Sub-type Article (original research)
DOI 10.1111/j.1365-2885.2010.01161.x
Volume 33
Issue 5
Start page 485
End page 494
Total pages 10
Editor Jim E. Riviere
Johanna Fink-Gremmels
Place of publication Oxford, U.K.
Publisher Wiley-Blackwell Publishing
Collection year 2011
Language eng
Formatted abstract
Gabapentin is being used in horses although its pharmacokinetic (PK) profile, pharmacodynamic (PD) effects and safety in the equine are not fully investigated. Therefore, we characterized PKs and cardiovascular and behavioral effects of gabapentin in horses. Gabapentin (20 mg/kg) was administered i.v. or p.o. to six horses using a randomized crossover design. Plasma gabapentin concentrations were measured in samples collected 0–48 h postadministration employing liquid chromatography-tandem mass spectrometry. Blood pressures, ECG, and sedation scores were recorded before and for 12 h after gabapentin dosage. Nineteen quantitative measures of behaviors were evaluated. After i.v. gabapentin, the decline in plasma drug concentration over time was best described by a 3-compartment mammillary model. Terminal elimination half-life (t1/2γ) was 8.5 (7.1–13.3) h. After p.o. gabapentin terminal elimination half-life (t1/2e) was 7.7 (6.7–11.9) h. The mean oral bioavailability of gabapentin (±SD) was 16.2 ± 2.8% indicating relatively poor absorption of gabapentin following oral administration in horses. Gabapentin caused a significant increase in sedation scores for 1 h after i.v. dose only (< 0.05). Among behaviors, drinking frequency was greater and standing rest duration was lower with i.v. gabapentin (< 0.05). Horses tolerated both i.v. and p.o. gabapentin doses well. There were no significant differences in t1/2γ and t1/2e. Oral administration yielded much lower plasma concentrations because of low bioavailability.
© 2010 Blackwell Publishing Ltd
Keyword Neuropathic pain
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Non HERDC
School of Veterinary Science Publications
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Citation counts: TR Web of Science Citation Count  Cited 15 times in Thomson Reuters Web of Science Article | Citations
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Created: Fri, 04 Mar 2011, 14:48:23 EST by Dr Andrew Van Eps on behalf of !NON-HERDC