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Zentralblatt fur Veterinarmedizin. Reihe A1990; 37(4); 253-258; doi: 10.1111/j.1439-0442.1990.tb00902.x

Plasma disposition and tolerance of aditoprim in horses after single intravenous injection.

Abstract: Aditoprim, a broad spectrum antimicrobial agent acting as a reversible dihydrofolate reductase inhibitor, was intravenously injected into four 12 to 24-year old horses at a dosage of 5 mg/kg b. w. Blood samples were collected over a 48-hour period after drug injection, and the separated plasma samples were assayed for aditoprim by high performance liquid chromatography. The body temperature, heart rate, respiration rate, and behaviour were recorded during the experiment. The bilirubin and urea concentrations were also determined in several plasma samples, and liver function tests were carried out. The concentrations of aditoprim in the plasma of horses were higher than the MIC of this drug against recently isolated pathogens for 6-13 h (Pasteurella haemolytica A 1) to 48 h (E. coli). The main pharmacokinetic characteristics of aditoprim in horses were: a large volume of distribution, reaching a mean value of 7.8 l/kg; a mean plasma clearance of 5.0 l/min; a plasma elimination half-life of 12 h. The clinical observations, blood chemistry, and liver function tests all demonstrated that the drug was well tolerated by the horses, although it was injected intravenously as a 25% solution. It was concluded that the 25% aditoprim injection solution could be used in horses without adverse effects at 5 mg/kg. Furthermore, aditoprim should demonstrate good antibacterial effects in horses when intravenously injected once a day.
Publication Date: 1990-05-01 PubMed ID: 2116704DOI: 10.1111/j.1439-0442.1990.tb00902.xGoogle Scholar: Lookup
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  • Journal Article

Summary

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The research investigated the impact of an antimicrobial agent called aditoprim on horses, which was given through an intravenous injection, and found it was well-tolerated and had beneficial antibacterial effects.

Research Methodology

  • The study was conducted on four horses aged between 12 to 24 years old.
  • An intravenous injection of aditoprim, an antimicrobial agent that acts as a reversible dihydrofolate reductase inhibitor, was administered at a dosage of 5 mg/kg of body weight.
  • Blood samples were collected over a 48-hour period to measure the drug’s concentration.
  • The researchers also recorded each horse’s body temperature, heart rate, respiration rate, and behaviour during the experiment.
  • Furthermore, the concentrations of bilirubin and urea were determined in the plasma samples, and liver function tests were carried out.

Research Results

  • The concentrations of aditoprim in the plasma of the horses were noteworthy against isolated pathogens for a duration of 6-13 hours (for Pasteurella haemolytica A 1) to 48 hours (for E. coli).
  • The drug showed a large volume of distribution (mean value of 7.8 l/kg), a mean plasma clearance of 5.0 l/minute, and a plasma elimination half-life of 12 hours.
  • Clinical observations, blood chemistry results, and liver function tests indicated that the drug had been well-tolerated by the horses, despite being injected intravenously in a 25% solution.

Conclusions

  • The researchers concluded that the 25% aditoprim injection solution could be used in horses without adverse effects at a dosage of 5 mg/kg.
  • They expected that aditoprim would show good antibacterial effects in horses when it’s intravenously injected once a day.

Cite This Article

APA
von Fellenberg RL, Jordan JC, Ludwig B, Rehm WF. (1990). Plasma disposition and tolerance of aditoprim in horses after single intravenous injection. Zentralbl Veterinarmed A, 37(4), 253-258. https://doi.org/10.1111/j.1439-0442.1990.tb00902.x

Publication

ISSN: 0514-7158
NlmUniqueID: 0331323
Country: Germany
Language: English
Volume: 37
Issue: 4
Pages: 253-258

Researcher Affiliations

von Fellenberg, R L
  • Institute of Veterinary Physiology, University of Zürich, Switzerland.
Jordan, J C
    Ludwig, B
      Rehm, W F

        MeSH Terms

        • Animals
        • Drug Tolerance
        • Female
        • Folic Acid Antagonists
        • Horses / blood
        • Horses / physiology
        • Male
        • Trimethoprim / analogs & derivatives
        • Trimethoprim / blood
        • Trimethoprim / pharmacokinetics

        Citations

        This article has been cited 4 times.
        1. Huang A, Huang X, Zhang Z, Yuan Z, Huang L, Wang Y, Tao Y, Chen D, Liu Z, Hao H. Dosing Regimen of Aditoprim and Sulfamethoxazole Combination for the Glaesserella parasuis Containing Resistance and Virulence Genes.. Pharmaceutics 2022 Sep 27;14(10).
          doi: 10.3390/pharmaceutics14102058pubmed: 36297496google scholar: lookup
        2. Cheng G, Xu Y, Zhu X, Xie S, Wang L, Huang L, Hao H, Liu Z, Pan Y, Chen D, Wang Y, Yuan Z. The antibacterial activities of aditoprim and its efficacy in the treatment of swine streptococcosis.. Sci Rep 2017 Feb 1;7:41370.
          doi: 10.1038/srep41370pubmed: 28145487google scholar: lookup
        3. Wang L, Huang L, Pan Y, Kuča K, Klímová B, Wu Q, Xie S, Ahmad I, Chen D, Tao Y, Wan D, Liu Z, Yuan Z. Metabolism and Disposition of Aditoprim in Swine, Broilers, Carp and Rats.. Sci Rep 2016 Feb 3;6:20370.
          doi: 10.1038/srep20370pubmed: 26838160google scholar: lookup
        4. Riond JL, Müller P, Wanner M. The influence of age on the pharmacokinetics of aditoprim in pigs after intravenous and oral administration.. Vet Res Commun 1992;16(5):355-64.
          doi: 10.1007/BF01839185pubmed: 1494860google scholar: lookup