Concentration of ceftiofur metabolites in the plasma and lungs of horses following intramuscular treatment.
Abstract: Ceftiofur sodium, a broad spectrum cephalosporin antibiotic approved for veterinary use, is metabolized to desfuroylceftiofur which is conjugated to micro as well as macromolecules. Twelve horses, weighting 442-618 kg, were injected intramuscularly with a single dose of 2.2 mg ceftiofur/kg (1.0 mg/lb) body weight. Blood was collected at various intervals over 24 h after treatment. Three groups of four horses each were euthanized and lungs were collected at 1, 12, and 24 h after treatment. The concentration of desfuroylceftiofur and desfuroylceftiofur conjugates in the plasma and lungs was determined by converting them to desfuroylceftiofur acetamide (DCA) and measured DCA by high performance liquid chromatography with UV detection. The average maximum concentration (Cmax) of desfuroylceftiofur and related metabolites in plasma expressed as ceftiofur equivalents was 4.46 +/- 0.93 micrograms/ml occurred at 1.25 +/- 0.46 h after treatment. These concentrations declined to 0.99 +/- 0.16, 0.47 +/- 0.15 and 0.17 +/- 0.02 microgram/ml at 8, 12, and 24 h, respectively. The mean residence time of ceftiofur metabolites was 6.10 +/- 1.27 h. Concentrations of desfuroylceftiofur and desfuroylceftiofur conjugates in the lungs of horses expressed as ceftiofur equivalents were 1.40 +/- 0.36, 0.27 +/- 0.07, and 0.15 +/- 0.08 micrograms/ml at 1, 12, and 24 h, respectively. These concentrations of the drug at 12 and 24 h in lung homogenate were similar but slightly lower than plasma concentrations in the same horses, and the plasma pharmacokinetic values including half-life were similar to those observed at the approved dose of 1.1-2.2 mg ceftiofur/kg body weight administered intramuscularly once daily for 3-5 days in cattle.
Publication Date: 1994-02-01 PubMed ID: 8196090DOI: 10.1111/j.1365-2885.1994.tb00517.xGoogle Scholar: Lookup
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- Journal Article
- Antibiotics
- Biological Half-Life
- Clinical Pathology
- Clinical Study
- Disease Treatment
- Equine Diseases
- Equine Health
- High-performance Liquid Chromatography (HPLC)
- Horses
- Intramuscular Administration
- Lung Health
- Metabolism
- Metabolites
- Pharmacodynamics
- Pharmacokinetics
- Physiology
- Plasma
- Veterinary Medicine
- Veterinary Procedure
- Veterinary Research
Summary
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The study investigates how ceftiofur sodium, a veterinary antibiotic, is metabolized in horses and how its concentration changes in plasma and lungs over time after intramuscular injection.
Research Design
- The researchers studied twelve horses, each weighing between 442-618 kg.
- A single dose of ceftiofur sodium (2.2 mg/kg body weight) was administered intramuscularly.
- Blood samples were collected from each horse at various time intervals up to 24 hours post-treatment.
- The animals were divided into three groups of four horses each, and these groups were euthanized at three different points in time – 1 hour, 12 hours, and 24 hours post-treatment – at which point their lungs were collected for further testing.
Data Collection and Analysis
- The desfuroylceftiofur and its conjugates in the plasma and lung samples were measured by converting them into a derivative (desfuroylceftiofur acetamide or DCA) and using high-performance liquid chromatography with UV detection to identify the concentration of DCA.
Key Findings
- The peak (or maximum) concentration of desfuroylceftiofur and its related metabolites in plasma was found to be 4.46 micrograms/ml, approximately 1.25 hours post-treatment.
- These concentrations decreased gradually to 0.99 micrograms/ml at 8 hours, 0.47 micrograms/ml at 12 hours, and 0.17 micrograms/ml at 24 hours post-treatment.
- The average time the metabolites of ceftiofur sodium stayed in the body (mean residence time) was around 6.10 hours.
- In the lung tissue, concentrations of the drug and its metabolites measured 1.40 micrograms/ml at 1 hour, 0.27 micrograms/ml at 12 hours, and 0.15 micrograms/ml at 24 hours post-treatment.
- The drug concentrations in the lungs were similar to but slightly lower than those in the blood plasma of the same horses.
- The plasma half-life and other pharmacokinetic values observed in this study were found to match those seen when administering the approved dose of ceftiofur sodium (1.1-2.2 mg/kg body weight) to cattle through intramuscular injection for a 3-5 day period.
Conclusion
- This research provided insightful data on the behaviour of ceftiofur sodium in the body of horses, its metabolization, and how its concentrations change over time in both blood plasma and lungs after intramuscular administration.
Cite This Article
APA
Jaglan PS, Roof RD, Yein FS, Arnold TS, Brown SA, Gilbertson TJ.
(1994).
Concentration of ceftiofur metabolites in the plasma and lungs of horses following intramuscular treatment.
J Vet Pharmacol Ther, 17(1), 24-30.
https://doi.org/10.1111/j.1365-2885.1994.tb00517.x Publication
Researcher Affiliations
- Upjohn Company, Kalamazoo, MI 49001.
MeSH Terms
- Animals
- Cephalosporins / administration & dosage
- Cephalosporins / blood
- Cephalosporins / pharmacokinetics
- Chromatography, High Pressure Liquid / veterinary
- Female
- Half-Life
- Horses / blood
- Injections, Intramuscular / veterinary
- Lung / metabolism
- Male
- Tissue Distribution
Citations
This article has been cited 4 times.- Lee DH, Birhanu BT, Lee EB, Lee SJ, Boby N, Park YS, Park SC. Pharmacokinetic and pharmacodynamic integration for optimal dosage of cefquinome against Streptococcus equi subsp. equi in foals.. Vet Res 2020 Oct 15;51(1):131.
- Wang J, Schneider BK, Xue J, Sun P, Qiu J, Mochel JP, Cao X. Pharmacokinetic Modeling of Ceftiofur Sodium Using Non-linear Mixed-Effects in Healthy Beagle Dogs.. Front Vet Sci 2019;6:363.
- Hooper SE, Korte SW, Giguère S, Fales WH, Davis JL, Dixon LW. Pharmacokinetics of Ceftiofur Crystalline-Free Acid in Clinically Healthy Dogs (Canis lupus familiaris).. J Am Assoc Lab Anim Sci 2016 Mar;55(2):224-9.
- Vilos C, Velasquez LA, Rodas PI, Zepeda K, Bong SJ, Herrera N, Cantin M, Simon F, Constandil L. Preclinical Development and In Vivo Efficacy of Ceftiofur-PLGA Microparticles.. PLoS One 2015;10(4):e0123335.
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