Abstract |
The neurokinin-1 (NK) receptor antagonist, maropitant citrate, mitigates nausea and vomiting in dogs and cats. Nausea is poorly understood and likely under-recognized in horses. Use of NK-1 receptor antagonists in horses has not been reported. The purpose of this study was to determine the pharmacokinetic profile of maropitant in seven adult horses after single intravenous (IV; 1 mg/kg) and intragastric (IG; 2 mg/kg) doses. A randomized, crossover design was performed. Serial blood samples were collected after dosing; maropitant concentrations were measured using LC-MS/MS. Pharmacokinetic parameters were determined using noncompartmental analysis. The mean plasma maropitant concentration 3 min after IV administration was 800 ± 140 ng/ml, elimination half-life was 10.37 ± 2.07 h, and volume of distribution was 6.54 ± 1.84 L/kg. The maximum concentration following IG administration was 80 ± 40 ng/ml, and elimination half-life was 9.64 ± 1.27 hr. Oral bioavailability was variable at 13.3 ± 5.3%. Maropitant concentrations achieved after IG administration were comparable to those in small animals. Concentrations after IV administration were lower than in dogs and cats. Elimination half-life was longer than in dogs and shorter than in cats. This study is the basis for further investigations into using maropitant in horses.
|
Authors | Emily H Berryhill, Heather Knych, Judy M Edman, K Gary Magdesian |
Journal | Journal of veterinary pharmacology and therapeutics
(J Vet Pharmacol Ther)
Vol. 42
Issue 4
Pg. 487-491
(Jul 2019)
ISSN: 1365-2885 [Electronic] England |
PMID | 31190332
(Publication Type: Journal Article, Randomized Controlled Trial, Veterinary)
|
Copyright | © 2019 John Wiley & Sons Ltd. |
Chemical References |
- Antiemetics
- Quinuclidines
- maropitant
|
Topics |
- Animals
- Antiemetics
(pharmacokinetics)
- Area Under Curve
- Cross-Over Studies
- Female
- Half-Life
- Horses
(blood, metabolism)
- Male
- Quinuclidines
(blood, pharmacokinetics)
|