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The Journal of veterinary medical science2010; 72(8); 1023-1026; doi: 10.1292/jvms.09-0321

Pharmacokinetics of the gastroprokinetic agent mosapride citrate after single oral administration in horses.

Abstract: The purpose of this study was to determine the pharmacokinetics and dose proportionality of mosapride citrate, a selective 5-HT4 agonist, after oral administration in horses. Seven healthy Thoroughbreds were dosed with distilled water and 0.5, 1.0, or 1.5 mg/kg mosapride citrate through a nasogastric tube. Serum mosapride concentrations were measured by a liquid chromatography/tandem mass spectrometry (LC/MS/MS) method. Mosapride showed the Cmaxs of 31, 60, and 104 ng/g and AUCs of 178, 357, and 566 ng.hr/g at doses of 0.5, 1.0, 1.5 mg/kg, respectively. The Cmaxs and AUCs increased in proportion to the dose, indicating linear pharmacokinetics of mosapride up to 1.5 mg/kg. The pharmacokinetic profiles of mosapride in horses are quite different from that in humans. The average t1/2 in horses was almost 2 fold longer than that reported in healthy adult humans. Therefore, it is thought that it is suitable to reduce the number of doses a day in horses compared to humans.
Publication Date: 2010-05-12 PubMed ID: 20467210DOI: 10.1292/jvms.09-0321Google Scholar: Lookup
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  • Journal Article

Summary

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The research article investigates the pharmacokinetics, or the way the drug mosapride citrate moves within the body, of a single orally administered dose in horses. It was found that the drug behaved differently in horses compared to humans, suggesting the need for different dosing schedules between the species.

Objective of the Research

  • The study primarily sought to understand the pharmacokinetics of mosapride citrate in horses. Pharmacokinetics is the scientific study of how an organism affects a drug, including the processes of absorption, distribution, metabolism, and excretion.
  • The researchers also wanted to determine whether the effects of the drug were dose-proportional; in other words, if increasing the dosage of the drug proportionally increases its effects on the body.

Method of the Research

  • The team administered doses of mosapride citrate to seven healthy Thoroughbred horses at three different dose levels.
  • The doses were administered with distilled water through a nasogastric tube, which is a tube inserted through the nose into the stomach.
  • The serum concentration of mosapride (or the amount of the drug present in the horse’s bloodstream) was then measured using a method known as liquid chromatography/tandem mass spectrometry.

Findings of the Research

  • The study found that the Cmaxs (the maximum or peak serum concentration that a drug achieves in a tested population after administration) and AUCs (the area under the curve, a measure of the drug exposure over time) of mosapride increased in proportion to the dose. This indicated a linear pharmacokinetic profile for mosapride in horses.
  • A salient finding was that mosapride behaved quite differently in horses versus humans. In horses, the t1/2, or half-life (the time required for a quantity to reduce to half its initial value), was almost two times longer than in humans. This means that the drug is eliminated from a horse’s system slower than it is from a human’s system.

Implications of the Findings

  • Given the longer half-life of mosapride in horses versus humans, the researchers suggest that the frequency of dosing in horses could possibly be reduced compared with humans.
  • Note that actual adjustments in dosage would require further studies, taking into account clinical efficacy and safety aspects, before any changes in recommended dosage can be implemented.

Cite This Article

APA
Okamura K, Sasaki N, Fukunaka M, Yamada H, Inokuma H. (2010). Pharmacokinetics of the gastroprokinetic agent mosapride citrate after single oral administration in horses. J Vet Med Sci, 72(8), 1023-1026. https://doi.org/10.1292/jvms.09-0321

Publication

ISSN: 0916-7250
NlmUniqueID: 9105360
Country: Japan
Language: English
Volume: 72
Issue: 8
Pages: 1023-1026

Researcher Affiliations

Okamura, Koichi
  • The United Graduate School of Veterinary Sciences, Gifu University, Gifu, Japan.
Sasaki, Naoki
    Fukunaka, Morito
      Yamada, Haruo
        Inokuma, Hisashi

          MeSH Terms

          • Administration, Oral
          • Animals
          • Area Under Curve
          • Benzamides / administration & dosage
          • Benzamides / blood
          • Benzamides / pharmacokinetics
          • Dose-Response Relationship, Drug
          • Female
          • Gastrointestinal Agents / administration & dosage
          • Gastrointestinal Agents / blood
          • Gastrointestinal Agents / pharmacokinetics
          • Half-Life
          • Horses
          • Kinetics
          • Male
          • Morpholines / administration & dosage
          • Morpholines / blood
          • Morpholines / pharmacokinetics
          • Orchiectomy / veterinary

          Citations

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