Faecal excretion profile of moxidectin and ivermectin after oral administration in horses.
Abstract: A study was undertaken to evaluate and compare faecal excretion of moxidectin and ivermectin in horses after oral administration of commercially available preparations. Ten clinically healthy adult horses, weighing 390-446 kg body weight (b.w.), were allocated to two experimental groups. Group I was treated with an oral gel formulation of moxidectin at the manufacturer's recommended therapeutic dose of 0.4 mg/kg b.w. Group II was treated with an oral paste formulation of ivermectin at the recommended dose of 0.2 mg/kg b.w. Faecal samples were collected at different times between 1 and 75 days post-treatment. After faecal drug extraction and derivatization, samples were analysed by High Performance Liquid Chromatography using fluorescence detection and computerized kinetic analysis. For both drugs the maximum concentration level was reached at 2.5 days post administration. The ivermectin treatment groups' faecal concentrations remained above the detectable level for 40 days (0.6 +/- 0.3 ng/g), whereas the moxidectin treatment group remained above the detectable level for 75 days (4.3 +/- 2.8 ng/g). Ivermectin presented a faster elimination rate than moxidectin, reaching 90% of the total drug excreted in faeces at four days post-treatment, whereas moxidectin reached similar levels at eight days post-treatment. No significant differences were observed for the values of maximum faecal concentration (C(max)) and time of C(max)(T(max)) between both groups of horses, demonstrating similar patterns of drug transference from plasma to the gastrointestinal tract. The values of the area under the faecal concentration time curve were slightly higher in the moxidectin treatment group (7104 +/- 2277 ng.day/g) but were not significantly different from those obtained in the ivermectin treatment group (5642 +/- 1122 ng.day/g). The results demonstrate that although a 100% higher dose level of moxidectin was used, attaining higher plasma concentration levels and more prolonged excretion and gut secretion than ivermectin, the concentration in faeces only represented 44.3+/- 18.0% of the total parental drug administered compared to 74.3 +/- 20.2% for ivermectin. This suggests a higher level of metabolization for moxidectin in the horse.
Copyright 2001 Harcourt Publishers Ltd.
Publication Date: 2001-01-09 PubMed ID: 11145833DOI: 10.1053/tvjl.2000.0521Google Scholar: Lookup
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- Journal Article
- Research Support
- Non-U.S. Gov't
- Animal Health
- Animal Studies
- Clinical Study
- Comparative Study
- Disease Treatment
- Drug
- Equine Diseases
- Equine Health
- Experimental Methods
- Feces
- High-performance Liquid Chromatography (HPLC)
- Horses
- Ivermectin
- Metabolism
- Oral Administration
- Pharmacodynamics
- Pharmacokinetics
- Physiology
- Veterinary Medicine
- Veterinary Research
Summary
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This study evaluates how horses excrete two types of orally administered drugs, moxidectin and ivermectin, by comparing how long these drugs remain detectable in faeces. The findings show that even though moxidectin was administered at a higher dose and had greater plasma levels, ivermectin was represented as a larger portion of the total drug administered in faeces, which suggests moxidectin is more quickly metabolized in the horse.
Methodology
- The researchers used ten clinically healthy adult horses of weights ranging from 390-446 kg for the study. These horses were divided into two experimental groups.
- Group I was treated with an oral gel formulation of moxidectin at a dose recommended by the manufacturer, 0.4 mg/kg body weight.
- Group II was treated with an oral paste formulation of ivermectin at a dose of 0.2 mg/kg body weight.
- Faecal samples were collected at varying times between 1 and 75 days after the treatment was administered.
- Horse faecal drug extractions were performed and samples were analysed using a high-performance liquid chromatography method that uses fluorescence detection and computerized kinetic analysis.
Findings
- Both the moxidectin and ivermectin achieved their highest concentrations in faeces at 2.5 days after administration.
- The faecal concentrations of ivermectin remained above detectable levels for 40 days after treatment. Moxidectin’s faecal concentrations remained above a detectable level for 75 days.
- Ivermectin was eliminated from the system faster than moxidectin, with 90% of the total drug excreted in faeces four days after treatment. By comparison, moxidectin took eight days to reach this level.
- Both drugs showed similar patterns of drug transfer from blood plasma to the gastrointestinal tract, with no significant difference in the times and quantities that they were found in faecal matter.
- Though administered at a 100% higher dosage than ivermectin, the concentration of moxidectin in faeces only represented 44.3% of the total drug administered, compared to 74.3% for ivermectin. This indicates that moxidectin is metabolized at a higher rate in horses.
Conclusion
- This research suggests a higher metabolization rate for moxidectin in horses compared to ivermectin, despite the dose of moxidectin being twice as high.
- The findings of this study could provide valuable insight into drug metabolization in horses, which could aid in the proper administration of these drugs in clinical settings.
Cite This Article
APA
Pérez R, Cabezas I, Sutra JF, Galtier P, Alvinerie M.
(2001).
Faecal excretion profile of moxidectin and ivermectin after oral administration in horses.
Vet J, 161(1), 85-92.
https://doi.org/10.1053/tvjl.2000.0521 Publication
Researcher Affiliations
- Laboratorio de Farmacologia, Facultad Medicina Veterinaria, Universidad de Conception, Chile. rubperez@udec.cl
MeSH Terms
- Administration, Oral
- Animals
- Anthelmintics / administration & dosage
- Anthelmintics / pharmacokinetics
- Anti-Bacterial Agents / administration & dosage
- Anti-Bacterial Agents / pharmacokinetics
- Chromatography, High Pressure Liquid
- Feces / chemistry
- Gels
- Horses / metabolism
- Ivermectin / administration & dosage
- Ivermectin / pharmacokinetics
- Macrolides
- Ointments
Citations
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