The pharmacokinetics of some aminoglycoside antibiotics in the horse.
Abstract: The disposition kinetics and bioavailability of streptomycin, kanamycin and neomycin were determined following their administration as parenteral preparations to horses. Single doses (10 mg/kg) of each aminoglycoside were given by the intravenous (i.v.) and intramuscular (i.m.) routes and, at a later time, seven intramuscular doses were injected at 12-h intervals. The pharmacokinetic behaviour of the three aminoglycosides was similar, in that a rapid distribution phase was followed by a relatively short half-life. The half-life (mean +/- SD, n = 6) of kanamycin (1.80 +/- 0.17 h) was significantly (P less than 0.01; t test, 10 d.f.) shorter than that of streptomycin (3.40 +/- 0.42 h), while neomycin half-life (2.10 +/- 0.97 h) was of an intermediate length. The apparent volume of distribution of neither kanamycin nor neomycin varied significantly (P greater than 0.05) from that of streptomycin and numerically (V1 d congruent to 230 ml/kg) was the same as the extracellular fluid volume. The body clearance of kanamycin (88.5 +/- 11.3 ml/kg.h) was significantly (P less than 0.01) larger than that of streptomycin (47.5 +/- 7.9 ml/kg.h), while a significant difference in this parameter did not exist (P greater than 0.05) between neomycin and streptomycin. Following intramuscular injection, each aminoglycoside was rapidly and completely absorbed from the injection site, although neomycin showed wide individual variation in the fraction absorbed. The administration of multiple doses did not change either the bioavailability or the apparent half-life from the values obtained after a single dose. The only pharmacokinetic difference between these aminoglycosides that is of clinical importance lies in the rate of their elimination. A dosage interval of 8 h would be appropriate for kanamycin compared with a 12-h interval for streptomycin. The dosage interval for neomycin based on half-life should be 8 h but, due to the relatively greater toxicity of this aminoglycoside, an interval of 12 h might be recommended. The height of the peak serum concentration is determined by the size of the dose.
Publication Date: 1981-12-01 PubMed ID: 7349342DOI: 10.1111/j.1365-2885.1981.tb00863.xGoogle Scholar: Lookup
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- Journal Article
Summary
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This study investigates how the bodies of horses handle and process three different aminoglycoside antibiotics: streptomycin, kanamycin, and neomycin. The research shows these antibiotics have similar behavior in the body, but their speed of elimination and possible dosage intervals could differ.
Methodology
- The researchers examined the kinetics (the rates of reactions) and bioavailability (how much and how soon the drug reaches the circulatory system) of the three antibiotics given intravenously and intramuscularly.
- Each horse was given single 10 mg/kg doses of streptomycin, kanamycin, and neomycin via both methods. This was followed by seven intramuscular doses delivered every 12 hours.
Findings
- All three antibiotics showed similar pharmacokinetic behavior, with a quick distribution phase followed by a relatively short half-life. The “half-life” of a drug is the duration it takes for its concentration in the body to decrease by half.
- Between the three antibiotics, kanamycin has the shortest half-life (1.80 hours), followed by neomycin (2.10 hours), and streptomycin (3.40 hours).
- On average, the volume of distribution of kanamycin and neomycin didn’t differ significantly from streptomycin. This means they occupy similar spaces within the body proportionate to their doses.
- The body clears kanamycin more rapidly (88.5 ml/kg.h) than streptomycin (47.5 ml/kg.h). The clearance rate of neomycin was not significantly different from streptomycin.
- After intramuscular injection, all three antibiotics were absorbed rapidly and entirely. However, the amount of neomycin absorbed varied more widely between individual horses.
- Multiple doses did not change the bioavailability or apparent half-life from those obtained after a single dose.
Implications
- One significant difference among these antibiotics lies in their elimination rate. As kanamycin is eliminated faster, the dosage interval should be 8 hours, compared with a 12-hour interval for streptomycin.
- Due to its relative toxicity compared to the other two, a 12-hour dosage interval for neomycin is suggested, despite its half-life suggesting an 8-hour interval.
- The size of the dose determines the maximum serum concentration. This information is important as it guides veterinarians on the effective dosage and frequency for using these antibiotics on horses.
Cite This Article
APA
Baggot JD, Love DN, Rose RJ, Raus J.
(1981).
The pharmacokinetics of some aminoglycoside antibiotics in the horse.
J Vet Pharmacol Ther, 4(4), 277-284.
https://doi.org/10.1111/j.1365-2885.1981.tb00863.x Publication
Researcher Affiliations
MeSH Terms
- Aminoglycosides / metabolism
- Animals
- Anti-Bacterial Agents / metabolism
- Biological Availability
- Half-Life
- Horses / metabolism
- Injections, Intramuscular
- Kanamycin / metabolism
- Kinetics
- Models, Biological
- Neomycin / metabolism
- Streptomycin / metabolism
Citations
This article has been cited 5 times.- Rampal S, Srivastava AK, Chaudhary RK. Disposition kinetics, urinary excretion and dosage regimen of kanamycin in buffalo calves following single intravenous administration. Vet Res Commun 1993;17(3):219-25.
- Baggot JD, Love DN, Rose RJ, Raus R. Selection of an aminoglycoside antibiotic for administration to horses. Equine Vet J 1985 Jan;17(1):30-4.
- Jayachandran C, Singh MK, Singh SD, Banerjee NC. Pharmacokinetics of streptomycin with particular reference to its distribution in plasma, milk and uterine fluid of she-buffaloes. Vet Res Commun 1987;11(4):353-8.
- Errecalde JO, Mariño EL. A discriminatory study of a pharmacokinetic model for intramuscular gentamicin in sheep. Vet Res Commun 1990;14(1):53-8.
- Lashev LD, Pashov DA, Marinkov TN. Interspecies differences in the pharmacokinetics of kanamycin and apramycin. Vet Res Commun 1992;16(4):293-300.
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