The biotransformation and urinary excretion of dexamethasone in equine male castrates.
Abstract: The pro-drugs of dexamethasone, a potent glucocorticoid, are frequently used as anti-inflammatory steroids in equine veterinary practice. In the present study the biotransformation and urinary excretion of tritium labelled dexamethasone were investigated in cross-bred castrated male horses after therapeutic doses. Between 40-50% of the administered radioactivity was excreted in the urine within 24 h; a further 10% being excreted over the next 3 days. The urinary radioactivity was largely excreted in the unconjugated steroid fraction. In the first 24 h urine sample, 26-36% of the total dose was recovered in the unconjugated fraction, 8-13% in the conjugated fraction and about 5% was unextractable from the urine. The metabolites identified by microchemical transformations and thin-layer chromatography were unchanged dexamethasone, 17-oxodexamethasone, 11-dehydrodexamethasone, 20-dihydrodexamethasone, 6-hydroxydexamethasone and 6-hydroxy-17-oxodexamethasone together accounting for approx 60% of the urinary activity. About 25% of the urinary radioactivity associated with polar metabolites still remains unidentified.
Publication Date: 1986-10-01 PubMed ID: 3773525DOI: 10.1016/0022-4731(86)90401-2Google Scholar: Lookup
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- Journal Article
Summary
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This study examines how dexamethasone, a steroid used in equine veterinary care, is metabolized and expelled from the bodies of male castrated horses. Researchers discovered that within 24 hours of administration, 40-50% of the administered dexamethasone was expelled in the urine. Additionally, a number of metabolites were identified, accounting for roughly 60% of the urinary activity.
Objective of the Research
- The main aim of this research was to study the biotransformation and urinary excretion of a potent glucocorticoid, dexamethasone, in castrated male horses.
Methodology
- The study involved the administration of therapeutic doses of tritium-labelled dexamethasone to the horses.
- Researchers then monitored and analyzed the urinary excretion of the administered dexamethasone over a span of several days.
- The metabolites of dexamethasone excreted in the urine were identified through microchemical transformations and thin-layer chromatography.
Findings
- Researchers found that between 40-50% of the administered dexamethasone was excreted in the urine within the first 24 hours of administration, with an additional 10% excreted over the following three days.
- Significantly, the majority of the urinary radioactivity was excreted in the form of the unconjugated steroid fraction.
- Six metabolites of dexamethasone were identified, which accounted for approximately 60% of the urinary activity.
- The metabolites identified were unchanged dexamethasone, 17-oxodexamethasone, 11-dehydrodexamethasone, 20-dihydrodexamethasone, 6-hydroxydexamethasone and 6-hydroxy-17-oxodexamethasone.
- About 25% of the urinary radioactivity was associated with polar metabolites that remain unidentified.
Conclusion
- The findings of this research provide crucial insights into the biotransformation and urinary excretion of dexamethasone in horses, which can potentially contribute to more effective therapeutic use of this drug within equine veterinary practice.
Cite This Article
APA
Dumasia MC, Houghton E, Moss MS, Chakraborty J, Marks V.
(1986).
The biotransformation and urinary excretion of dexamethasone in equine male castrates.
J Steroid Biochem, 25(4), 547-553.
https://doi.org/10.1016/0022-4731(86)90401-2 Publication
Researcher Affiliations
MeSH Terms
- Acetylation
- Animals
- Biotransformation
- Chromatography, Thin Layer
- Dexamethasone / metabolism
- Dexamethasone / urine
- Gas Chromatography-Mass Spectrometry
- Horses / metabolism
- Injections, Intramuscular
- Male
- Orchiectomy
- Oxidation-Reduction
Citations
This article has been cited 1 times.- Musee N, Kebaabetswe LP, Tichapondwa S, Tubatsi G, Mahaye N, Leareng SK, Nomngongo PN. Occurrence, Fate, Effects, and Risks of Dexamethasone: Ecological Implications Post-COVID-19.. Int J Environ Res Public Health 2021 Oct 27;18(21).
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