Research article - Peer-reviewed, 2007
Cetirizine in horses: pharmacokinetics and effect of ivermectin pretreatment
Olsen L, Ingvast-Larsson C, Bondesson U, Brostrom H, Tjalve H, Larsson PAbstract
The pharmacokinetics of the histamine Hl-antagonist cetirizine and the effects of pretreatment with the antiparasitic macrocyclic lactone ivermectin on the pharmacokinetics of cetirizine were studied in horses. After oral administration of cetirizine at 0.2 mg/kg bw, the mean terminal half-life was 3.4 h (range 2.9-3.7 h) and the maximal plasma concentration 132 ng/mL (101-196 ng/mL). The time to reach maximal plasma concentration was 0.7 h (0.5-0.8 h). Ivermectin (0.2 mg/kg bw) given orally 1.5 h before cetirizine did not affect its pharmacokinetics. However, ivermectin pretreatment 12 h before cetirizinc increased the area under the plasma concentration-time curve by 60%. The maximal plasma concentration, terminal half-life and mean residence time also increased significantly following the 12 h pretreatment. Ivermectin is an inhibitor of P-glycoprotein, which is a major drug efflux transporter in cellular membranes at various sites. The elevated plasma levels of cetirizine following the pretreatment with ivermectin may mainly be due to decreased renal secretion, related to inhibition of the P-glycoprotein in the proximal tubular cells of the kidney. The pharmacokinetic properties of cetirizine have characteristics which are suitable for an antihistamine, and this substance may be a useful drug in horsesPublished in
Journal of Veterinary Pharmacology and Therapeutics2007, volume: 30, number: 3, pages: 194-200
Publisher: BLACKWELL PUBLISHING
Authors' information
Swedish University of Agricultural Sciences, Department of Biomedical Science and Veterinary Public Health
Ingvast Larsson, Carina
Swedish University of Agricultural Sciences, Department of Biomedical Science and Veterinary Public Health
Broström, Hans
Swedish University of Agricultural Sciences, Department of Clinical Sciences
Tjälve, Hans
Swedish University of Agricultural Sciences, Department of Biomedical Science and Veterinary Public Health
Bondesson, Ulf
Larsson, Pia
Swedish University of Agricultural Sciences, Department of Biomedical Science and Veterinary Public Health
UKÄ Subject classification
Animal and Dairy Science
Veterinary Science
Publication Identifiers
DOI: https://doi.org/10.1111/j.1365-2885.2007.00850.x
URI (permanent link to this page)
https://res.slu.se/id/publ/14812