Bioavailability of oral penicillins in the horse: a comparison of pivampicillin and amoxicillin.
Abstract: The pharmacokinetics of ampicillin and amoxicillin following intravenous administration at a dose rate of 15 and 10 mg/kg respectively were studied in four healthy adult horses. Pharmacokinetics of pivampicillin and amoxicillin were studied after oral administration to four healthy adult horses. Pivampicillin, a prodrug of ampicillin, was administered orally to starved and fed horses at a dose rate of 19.9 mg/kg, which is equivalent on a molecular basis to 15 mg/kg ampicillin. Amoxicillin was administered orally to starved horses only, at a dose rate of 20 mg/kg. Ampicillin and amoxicillin concentrations in plasma, synovial fluid and urine were determined. Mean biological half-life of intravenously administered ampicillin and amoxicillin was 1.72 and 1.43 h respectively, whilst the distribution volume (Vss) appeared to be 0.180 and 0.192 1/kg. Orally administered pivampicillin and amoxicillin were rapidly absorbed. A maximum concentration in plasma of 3.80 micrograms/ml was reached 2 h after administration of pivampicillin to starved horses; in fed horses a maximum concentration of 5.12 micrograms/ml was reached 1 h after administration. After oral administration of amoxicillin a maximum concentration of 2.03 micrograms/ml was reached after 1 h. The (absolute) bioavailability of pivampicillin administered orally was 30.9% in starved horses and 35.9% in fed horses. The bioavailability of amoxicillin administered orally was 5.3% in starved horses.
Publication Date: 1992-09-01 PubMed ID: 1433484DOI: 10.1111/j.1365-2885.1992.tb01010.xGoogle Scholar: Lookup
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- Comparative Study
- Journal Article
Summary
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This research study investigates the pharmacokinetics and bioavailability of two oral penicillins, pivampicillin and amoxicillin, in horses, providing valuable insights into their absorption rates, biological half-lives, and distribution volumes.
Overview of the Study
- The pharmacokinetics of ampicillin and amoxicillin were studied in four healthy adult horses following intravenous administration.
- Pivampicillin and amoxicillin were also administered orally to these horses, and their pharmacokinetics were analyzed.
- Pivampicillin, a prodrug of ampicillin, was given to both starved and fed horses, while amoxicillin was only administered to starved horses.
- The concentrations of both drugs in plasma, synovial fluid, and urine were determined to assess absorption and distribution.
Findings of the Research
- The mean biological half-life for intravenously administered ampicillin and amoxicillin was found to be 1.72 hours and 1.43 hours respectively, indicating the time these drugs take to reduce to half their original concentration in the body.
- The distribution volume (Vss), which represents the extent of drug distribution in the body, appeared to be 0.180 l/kg for ampicillin and 0.192 l/kg for amoxicillin.
- Both orally administered pivampicillin and amoxicillin were rapidly absorbed in the horse’s body. The maximum concentration in plasma was reached at different times for different drugs and conditions (starved or fed).
Bioavailability of the Drugs
- Bioavailability of a drug is a measure of the rate and extent to which the active ingredient is absorbed and becomes available in the body. This study found that orally administered pivampicillin had a bioavailability of 30.9% in starved horses and 35.9% in fed horses.
- The bioavailability of orally administered amoxicillin was significantly lower at 5.3% in starved horses.
This study provides crucial insights into the pharmacokinetics and bioavailability of pivampicillin and amoxicillin in horses, which could guide their use in veterinary practice.
Cite This Article
APA
Ensink JM, Klein WR, Mevius DJ, Klarenbeek A, Vulto AG.
(1992).
Bioavailability of oral penicillins in the horse: a comparison of pivampicillin and amoxicillin.
J Vet Pharmacol Ther, 15(3), 221-230.
https://doi.org/10.1111/j.1365-2885.1992.tb01010.x Publication
Researcher Affiliations
- Department of General and Large Animal Surgery, State University of Utrecht, The Netherlands.
MeSH Terms
- Administration, Oral
- Amoxicillin / administration & dosage
- Amoxicillin / pharmacokinetics
- Ampicillin / administration & dosage
- Ampicillin / pharmacokinetics
- Animals
- Biological Availability
- Fasting
- Female
- Half-Life
- Horses / metabolism
- Injections, Intravenous / veterinary
- Male
- Pivampicillin / administration & dosage
- Pivampicillin / pharmacokinetics
Citations
This article has been cited 9 times.- Koutsoumanis K, Allende A, Alvarez-Ordóñez A, Bolton D, Bover-Cid S, Chemaly M, Davies R, De Cesare A, Herman L, Hilbert F, Lindqvist R, Nauta M, Ru G, Simmons M, Skandamis P, Suffredini E, Andersson DI, Bampidis V, Bengtsson-Palme J, Bouchard D, Ferran A, Kouba M, López Puente S, López-Alonso M, Nielsen SS, Pechová A, Petkova M, Girault S, Broglia A, Guerra B, Innocenti ML, Liébana E, López-Gálvez G, Manini P, Stella P, Peixe L. Maximum levels of cross-contamination for 24 antimicrobial active substances in non-target feed.u2028Part 4: β-Lactams: amoxicillin and penicillin V. EFSA J 2021 Oct;19(10):e06855.
- Zhou Q, Xiao Q, Zhang Y, Wang X, Xiao Y, Shi D. Pig liver esterases PLE1 and PLE6: heterologous expression, hydrolysis of common antibiotics and pharmacological consequences. Sci Rep 2019 Oct 29;9(1):15564.
- Caol S, Divers T, Crisman M, Chang YF. In vitro susceptibility of Borrelia burgdorferi isolates to three antibiotics commonly used for treating equine Lyme disease. BMC Vet Res 2017 Sep 29;13(1):293.
- Elsheikh HA, Taha AA, Khalafalla AE, Osman IA, Wasfi IA. Pharmacokinetics of amoxicillin trihydrate in Desert sheep and Nubian goats. Vet Res Commun 1999 Dec;23(8):507-14.
- Sabnis S. Factors influencing the bioavailability of peroral formulations of drugs for dogs. Vet Res Commun 1999 Nov;23(7):425-47.
- Escudero E, Espuny A, Vicente S, Cárceles CM. Pharmacokinetics of an ampicillin-sulbactam combination after intravenous and intramuscular administration to sheep. Can J Vet Res 1999 Jan;63(1):25-30.
- Dubbelboer IR, Olsén L, Pelander L, Lacroix MZ, Claustre L, Roques B, Ekstrand C. Pharmacokinetics of Amoxicillin in the Cat. J Vet Pharmacol Ther 2025 Sep;48(5):380-388.
- Guzelaydin K, Gunes Y, Anlas C, Yildirim M. Pharmacokinetics and oral bioavailability of ampicillin and its prodrug bacampicillin in chickens and turkeys. J Vet Sci 2025 Mar;26(2):e21.
- Guardabassi L, Apley M, Olsen JE, Toutain PL, Weese S. Optimization of Antimicrobial Treatment to Minimize Resistance Selection. Microbiol Spectr 2018 May;6(3).
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