Pharmacokinetics of intramuscular maropitant in pigs (Sus scrofa domesticus)

Abstract

Pigs are at risk of vomiting from medical conditions as well as the emetic side effects of drugs administered for peri‐operative manipulations, but there is a lack of pharmacokinetic data for potential anti‐emetic therapies, such as maropitant, in this species. The main objective of this study was to estimate plasma pharmacokinetic parameters for maropitant in pigs after a single intramuscular (IM) administration dosed at 1.0 mg/kg. A secondary objective was to estimate pilot pharmacokinetic parameters in pigs after oral (PO) administration at 2.0 mg/kg. Maropitant was administered to six commercial pigs at a dose of 1.0 mg/kg IM. Plasma samples were collected over 72 h. After a 7‐day washout period, two pigs were administered maropitant at a dose of 2.0 mg/kg PO. Maropitant concentrations were measured via liquid chromatography/mass spectrometry (LC–MS/MS). A non‐compartmental analysis was used to derive pharmacokinetics parameters. No adverse events were noted in any of the study pigs after administration. Following single IM administration, maximum plasma concentration was estimated at 412.7 ± 132.0 ng/mL and time to maximum concentration ranged from 0.083 to 1.0 h. Elimination half‐life was estimated at 6.7 ± 1.28 h, and mean residence time was 6.1 ± 1.2 h. Volume of distribution after IM administration was 15.9 L/kg. Area under the curve was 1336 ± 132.0 h*ng/mL. The relative bioavailability of PO administration was noted to be 15.5% and 27.2% in the two pilot pigs. The maximum systemic concentration observed in the study pigs after IM administration was higher than what was observed after subcutaneous administration in dogs, cats, or rabbits. The achieved maximum concentration exceeded the concentrations for anti‐emetic purposes in dogs and cats; however, a specific anti‐emetic concentration is currently not known for pigs. Further research is needed into the pharmacodynamics of maropitant in pigs to determine specific therapeutic strategies for this drug.

Pig Sedation and Anesthesia for Medical Research

“…Maropitant is primarily administered before anesthetic premedication and used as antiemetic medication but also for visceral analgesia. The minimum alveolar concentration of sevoflurane is decreased by maropitant, indicating a potential role as an adjunct visceral analgesic [55].…”

Pig Sedation and Anesthesia for Medical Research

“…Maropitant is a potent, selective neurokinin (NK-1) receptor antagonist primarily administered before anesthetic premedication (1 mg/kg q 24 h, IM) as an antiemetic medication [64]. The MAC of sevoflurane is decreased by maropitant, indicating a potential role as an adjunct visceral analgesic, as demonstrated in other animals [65].…”