Pharmacokinetics of single doses of maropitant citrate in adult horses.

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.