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Veterinary journal (London, England : 1997)2007; 177(2); 242-249; doi: 10.1016/j.tvjl.2007.03.026

Cetirizine in horses: pharmacokinetics and pharmacodynamics following repeated oral administration.

Abstract: The pharmacokinetics of the histamine H(1)-antagonist cetirizine and its effect on histamine-induced cutaneous wheal formation were studied in six healthy horses following repeated oral administration. After three consecutive administrations of cetirizine (0.2 mg/kg body weight, bw) every 12h, the trough plasma concentration of cetirizine was 16+/-4 ng/mL (mean+/-SD) and the wheal formation was inhibited by 45+/-23%. After four additional administrations of cetirizine (0.4 mg/kg bw) every 12 h, the trough plasma concentration was 48+/-15 ng/mL and the wheal formation was inhibited by 68+/-11%. The terminal half-life was about 5.8 h. A pharmacokinetic/pharmacodynamic link model showed that the maximal inhibition of wheal formation was about 95% and the EC(50) about 18 ng/mL. It is concluded that cetirizine in doses of 0.2-0.4 mg/kg bw administered at 12 h intervals exhibits favourable pharmacokinetic and pharmacodynamic properties without causing visible side effects, and the drug may therefore be a useful antihistamine in equine medicine.
Publication Date: 2007-06-19 PubMed ID: 17581764DOI: 10.1016/j.tvjl.2007.03.026Google Scholar: Lookup
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The study examined how cetirizine, an antihistamine, behaves in the body of horses and its impact on their allergic reactions. The research found that regular doses of 0.2 to 0.4 mg/kg body weight every 12 hours can inhibit the formation of allergy-induced skin welts by up to 95% without noticeable side effects, making it a potentially useful treatment in equine medicine.

Understanding the Study

In order to provide a comprehensive explanation of the research paper, the content is divided into several key insights:

  • Objective: The purpose of the study was to understand the pharmacokinetics (how the drug moves in the body) and pharmacodynamics (the effect of the drug on the body) of cetirizine in horses. Researchers specifically looked at how this antihistamine affected the formation of skin welts caused by histamine, a substance that the body produces during allergic reactions.
  • Methodology: The study involved administering cetirizine orally to six healthy horses. Initially, doses of 0.2 mg/kg body weight were given every 12 hours for three cycles. After that, the dosage was increased to 0.4 mg/kg body weight for four cycles. Plasma concentrations were measured after each cycle, and the effectiveness of cetirizine in suppressing skin welts was evaluated.
  • Results: After three cycles of 0.2mg/kg dosage, the study found a plasma concentration of cetirizine of 16 ng/mL and a 45% inhibition of welt formation. When the dosage was increased, the plasma concentration rose to 48 ng/mL, and welt formation inhibition rose to 68%. The elimination half-life of cetirizine from the body was about 5.8 hours.
  • Pharmacokinetic/Pharmacodynamic Link: The researchers developed a model based on the results and found that the maximal inhibition of welt formation was roughly 95% and the concentration of cetirizine needed to achieve 50% of this maximum effect (EC50) was about 18 ng/mL.
  • Conclusion: The study concluded that cetirizine in doses of 0.2-0.4 mg/kg body weight given at 12-hour intervals exhibited promising pharmacokinetic and pharmacodynamic properties. With no visible side effects, the drug could be useful as an antihistamine in equine medicine.

Implications of the Study

  • This study provides notable information on the impact of cetirizine in horses and its potential viability as a histamine antagonist in equine medicine. The ability to reduce histamine-induced welts by up to 95% could significantly enhance the treatment and management of allergic conditions in horses.
  • The research also gives a base dosage and administration frequency, providing a useful starting point for veterinarians prescribing cetirizine.
  • Nevertheless, larger-scale studies with a broader range of horses would be beneficial to confirm these findings and to uncover any less common or long-term side effects.

Cite This Article

APA
Olsén L, Bondesson U, Broström H, Tjälve H, Ingvast-Larsson C. (2007). Cetirizine in horses: pharmacokinetics and pharmacodynamics following repeated oral administration. Vet J, 177(2), 242-249. https://doi.org/10.1016/j.tvjl.2007.03.026

Publication

ISSN: 1090-0233
NlmUniqueID: 9706281
Country: England
Language: English
Volume: 177
Issue: 2
Pages: 242-249

Researcher Affiliations

Olsén, Lena
  • Division of Pathology, Pharmacology and Toxicology, Department of Biomedical Sciences and Veterinary Public Health, Swedish University of Agricultural Sciences, Uppsala, Sweden. Lena.Olsen@bvf.slu.se
Bondesson, Ulf
    Broström, Hans
      Tjälve, Hans
        Ingvast-Larsson, Carina

          MeSH Terms

          • Administration, Oral
          • Animals
          • Anti-Allergic Agents / administration & dosage
          • Anti-Allergic Agents / pharmacokinetics
          • Area Under Curve
          • Cetirizine / administration & dosage
          • Cetirizine / blood
          • Cetirizine / pharmacokinetics
          • Female
          • Half-Life
          • Horses / blood
          • Horses / metabolism

          Citations

          This article has been cited 1 times.
          1. Ikeda Y, Kuroda T, Mita H, Tamura N, Ohta M. Comparing the effectiveness of four antihistamines with olopatadine in healthy Thoroughbred horses. J Vet Med Sci 2025 Feb 4;87(2):171-174.
            doi: 10.1292/jvms.24-0412pubmed: 39805609google scholar: lookup