Safety, pharmacokinetics and use of the novel NK-1 receptor antagonist maropitant (Cerenia) for the prevention of emesis and motion sickness in cats.
The present study characterizes the safety, pharmacokinetics, and anti-emetic effects of the selective NK-1 receptor antagonist maropitant in the cat. Safety of maropitant was determined following 15 days of subcutaneous (SC) administration at 0.5-5 mg/kg. Maropitant was well tolerated in cats at doses that exceeded the efficacious anti-emetic dose range of the drug by at least a factor of 10 and adverse clinical signs or pathological safety findings were not noted at any dose.The pharmacokinetics of maropitant in cats were determined following single dose oral (PO), intravenous (IV) and SC administration. Maropitant had a terminal half-life of 13-17 h and a bioavailability of 50 and 117% when administered PO and SC, respectively. Efficacy was determined against emesis induced either by xylazine or by motion. A dosage of 1 mg/kg maropitant administered IV, SC or PO prevented emesis elicited by xylazine. The compound had good oral antiemetic activity and a long (24 h) duration of action. Maropitant (1.0 mg/kg) was highly effective in preventing motion-induced emesis in cats. These studies indicate that the NK-1 receptor antagonist maropitant is well tolerated, safe and has excellent anti-emetic properties in cats.
Hickman
M A
MA
Pfizer Animal Health, Discovery Research, Pfizer Inc, Kalamazoo, MI 49001, USA.
Cox
S R
SR
Mahabir
S
S
Miskell
C
C
Lin
J
J
Bunger
A
A
McCall
R B
RB
D000818:Animals; D002415:Cats; D005260:Female; D008297:Male; D008657:Metabolic Clearance Rate; D009041:Motion Sickness / Q000209:etiology / Q000517:prevention & control / Q000662:veterinary*; D064729:Neurokinin-1 Receptor Antagonists; D011812:Quinuclidines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control / Q000662:veterinary*
D064729:Neurokinin-1 Receptor Antagonists; D011812:Quinuclidines; C518176:maropitant