Document Detail

Cetirizine in horses: pharmacokinetics and effect of ivermectin pretreatment.
MedLine Citation:
PMID:  17472650     Owner:  NLM     Status:  MEDLINE    
The pharmacokinetics of the histamine H(1)-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 cetirizine 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 horses.
L Olsén; C Ingvast-Larsson; U Bondesson; H Broström; H Tjälve; P Larsson
Publication Detail:
Type:  Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of veterinary pharmacology and therapeutics     Volume:  30     ISSN:  0140-7783     ISO Abbreviation:  J. Vet. Pharmacol. Ther.     Publication Date:  2007 Jun 
Date Detail:
Created Date:  2007-05-02     Completed Date:  2007-06-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7910920     Medline TA:  J Vet Pharmacol Ther     Country:  England    
Other Details:
Languages:  eng     Pagination:  194-200     Citation Subset:  IM    
Division of Pathology, Pharmacology and Toxicology, Department of Biomedical Sciences and Veterinary Public Health, Swedish University of Agricultural Sciences, Uppsala, Sweden.
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MeSH Terms
Administration, Oral
Antiparasitic Agents / administration & dosage,  blood,  pharmacology*
Area Under Curve
Cetirizine / administration & dosage,  blood,  pharmacokinetics*
Drug Interactions
Histamine H1 Antagonists / administration & dosage,  blood,  pharmacokinetics*
Horses / metabolism*
Ivermectin / administration & dosage,  blood,  pharmacology*
Reg. No./Substance:
0/Antiparasitic Agents; 0/Histamine H1 Antagonists; 70288-86-7/Ivermectin; 83881-51-0/Cetirizine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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