Plasma profiles of ivermectin in horses following oral or intramuscular administration.
Abstract: A study was undertaken in order to evaluate and compare ivermectin's (IVM) plasma disposition kinetic parameters after oral or intramuscular (IM) administration in horses. Ten clinically healthy adult horses, weighing 380-496 kg body weight (BW), were allocated to two experimental groups of five horses. Group I, was treated with an oral paste formulation of IVM at the manufacturer's recommended dose of 0.2 mg/kg BW. Group II, was treated IM with an injectable 1% formulation of IVM at a dose of 0.2 mg/kg BW. Blood samples were collected by jugular puncture at different times between 0.5 h and 75 days post-treatment. After plasma extraction and derivatization, samples were analysed by high-performance liquid chromatography with fluorescence detection. A computerized kinetic analysis was performed, and data were compared using the Wilcoxon signed rank test. The parent molecule was detected in plasma between 30 min and either 20 (oral) or 40 (IM) days post-treatment. Significant differences were found for the time corresponding to peak plasma concentrations (tmax) and for absorption half-life. Peak plasma concentrations (Cmax) of 51.3 +/- 16.1 ng/ml (mean +/- SD) were obtained after oral administration and of 31.4 +/- 6.0 ng/ml for the IM route. The values for area under concentration-time curve were 137.1 +/- 35.9 ng day/ml for the group treated orally, and 303.2 +/- 4.3 ng day/ml for the IM treated group. The mean plasma residence times were 4.2 +/- 0.4 and 8.9 +/- 0.7 days for oral and IM-treated groups, respectively. The results of this study show that the route of administration considerably affects the disposition of IVM. A significant difference in bioavailabilty and half-life of elimination of IVM was observed after IM administration compared with oral administration. A close relationship between pharmacokinetic profiles and the clinical efficacy of IVM was established.
Publication Date: 2003-07-31 PubMed ID: 12887622DOI: 10.1046/j.1439-0442.2003.00531.xGoogle Scholar: Lookup
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- Clinical Trial
- Journal Article
- Randomized Controlled Trial
- Research Support
- Non-U.S. Gov't
- Adult Horses
- Analytical Methods
- Bioavailability
- Biological Half-Life
- Blood Analysis
- Body Weight
- Clinical Study
- Comparative Study
- Drug
- Equine Health
- Experimental Methods
- High-performance Liquid Chromatography (HPLC)
- Horses
- Intramuscular Administration
- Ivermectin
- Oral Administration
- Pharmacodynamics
- Pharmacokinetics
- Plasma
- Veterinary Medicine
Summary
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The study compares plasma dispositions of ivermectin in horses given either orally or via intramuscular injection. The results indicate that different administration methods have significant impacts on the absorption, bioavailability and elimination half-life of this drug.
Objective and Methodology
- The main objective was to evaluate and compare ivermectin’s plasma kinetic parameters after oral or intramuscular administration in horses.
- Two experimental groups of horses were used, each comprising five clinically healthy adult horses, weighing between 380-496 kg body weight (BW).
- Group I were treated orally with ivermectin paste at a dose of 0.2 mg/kg BW, whereas Group II were treated with an intramuscular injectable formulation of ivermectin at the same dose.
- Blood samples were taken from the subjects at different times, ranging from 0.5 hour to 75 days post-treatment, and analysed by high-performance liquid chromatography with fluorescence detection.
- A computerized kinetic analysis was performed and data was compared to identify significant differences.
Results
- Ivermectin was detected in plasma between 30 minutes and either 20 days (for oral) or 40 days (for IM) post-treatment.
- Significant differences were found between the two groups in regards to the time taken to reach peak plasma concentrations, and for absorption half-life.
- Peak plasma concentrations were 51.3 +/- 16.1 ng/ml after oral administration and 31.4 +/- 6.0 ng/ml for the IM route.
- The values for the area under the concentration-time curve were markedly higher for the horses given IM treatment (303.2 +/- 4.3 ng day/ml), compared to those who received the drug orally (137.1 +/- 35.9 ng day/ml).
- The mean plasma residence times were 4.2 +/- 0.4 days for orally treated horses and 8.9 +/- 0.7 days for IM-treated groups.
Conclusion
- The study found that the route of administration dramatically affects the disposition of ivermectin in horses. The intramuscular route showed a much higher bioavailability and elimination half-life than oral administration.
- The study also established a correlation between the pharmacokinetic profiles and the clinical efficacy of ivermectin, suggesting that the method of administration might impact the drug’s effectiveness.
Cite This Article
APA
Pérez R, Godoy C, Palma C, Cabezas I, Muñoz L, Rubilar L, Arboix M, Alvinerie M.
(2003).
Plasma profiles of ivermectin in horses following oral or intramuscular administration.
J Vet Med A Physiol Pathol Clin Med, 50(6), 297-302.
https://doi.org/10.1046/j.1439-0442.2003.00531.x Publication
Researcher Affiliations
- Facultad de Medicina Veterinaria, Universidad de Concepción, Chillán, Chile. rubperez@udec.cl
MeSH Terms
- Administration, Oral
- Animals
- Anthelmintics / administration & dosage
- Anthelmintics / blood
- Anthelmintics / pharmacokinetics
- Area Under Curve
- Female
- Horses / metabolism
- Injections, Intramuscular / veterinary
- Ivermectin / administration & dosage
- Ivermectin / blood
- Ivermectin / pharmacokinetics
- Male
Citations
This article has been cited 4 times.- Suárez G, Castells D, Imperiale F, Fagiolino P, Canton C, Lanusse C, Alvarez L. Therapeutic advantages of the combined use of closantel and moxidectin in lambs parasitized with resistant gastrointestinal nematodes. Int J Parasitol Drugs Drug Resist 2023 Aug 2;23:28-36.
- Bazzano M, Di Salvo A, Diaferia M, Veronesi F, Galarini R, Paoletti F, Tesei B, McLean A, Veneziano V, Laus F. Anthelmintic Efficacy and Pharmacokinetics of Ivermectin Paste after Oral Administration in Mules Infected by Cyathostomins. Animals (Basel) 2020 May 28;10(6).
- Kim S, Sayem SAJ, Chae H, Park SW, Gui L, Park SC, Kang J. Comparative pharmacokinetic and bioequivalence of nine oral ivermectin formulations in dogs. J Vet Sci 2025 Nov;26(6):e88.
- Buono F, Veneziano V, Veronesi F, Molento MB. Horse and donkey parasitology: differences and analogies for a correct diagnostic and management of major helminth infections. Parasitology 2023 Oct;150(12):1119-1138.
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