Pharmacokinetics of single doses of maropitant citrate in adult horses

Emily H. Berryhill, Heather K Knych, Judy M. Edman, K G Magdesian

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
JournalJournal of Veterinary Pharmacology and Therapeutics
DOIs
StatePublished - Jan 1 2019

Fingerprint

citrates
pharmacokinetics
Horses
Pharmacokinetics
half life
horses
nausea
cats
dosage
intravenous injection
Half-Life
dogs
antagonists
Cats
Dogs
Nausea
receptors
vomiting
Neurokinin-1 Receptor Antagonists
bioavailability

Keywords

  • horses
  • maropitant
  • neurokinin-1
  • pharmacokinetics
  • substance P

ASJC Scopus subject areas

  • Pharmacology
  • veterinary(all)

Cite this

Pharmacokinetics of single doses of maropitant citrate in adult horses. / Berryhill, Emily H.; Knych, Heather K; Edman, Judy M.; Magdesian, K G.

In: Journal of Veterinary Pharmacology and Therapeutics, 01.01.2019.

Research output: Contribution to journalArticle

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