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Pharmacokinetics and bioavailability of cefazolin in horses.

Abstract: The pharmacokinetics and bioavailability of cefazolin given (IV, IM) to horses at the dosage of 11 mg/kg were investigated. The disposition of cefazolin given by IV route was characterized by a rapid disposition phase with a half-life of 5 to 10 minutes and a subsequent slower elimination phase with a half-life of 35 to 46 minutes. The total plasma clearance of cefazolin averaged 5.51 ml/min/kg and was due mainly to renal clearance (5.39 ml/min/kg) of unchanged drug. The volume of distribution at steady-state averaged 188 ml/kg. Plasma protein binding of cefazolin at a concentration of 10 micrograms/ml averaged 8.1 +/- 1.9%. Given by the IM route, cefazolin was rapidly absorbed; the extent of bioavailability was 78.4 +/- 18.8%, and the terminal half-life ranged from 49 to 99 minutes. Thus, cefazolin was extensively absorbed, but was eliminated more slowly than after IV administration.
Publication Date: 1985-02-01 PubMed ID: 3994100
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  • Comparative Study
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research article explores the pharmacokinetics and bioavailability (how effectively a drug is absorbed and used by the body) of cefazolin, an antibiotic, in horses. The findings showcase that when administered either intravenously (IV) or intramuscularly (IM), cefazolin is quickly absorbed by the horse’s body, undergoes rapid initial disposal followed by slower elimination, and is mostly cleared from the system through the kidneys.

Methodology and Administration

  • The study aimed to investigate the pharmacokinetics and bioavailability of cefazolin given through IV and IM routes to horses at a dosage of 11 mg/kg.
  • Pharmacokinetics refers to the movements of drugs within the body, and these may include how the drug is absorbed, distributed, metabolized, and ultimately eliminated from the body.

Disposition Phase and Half-life of Cefazolin

  • The disposition of cefazolin administered through the IV route went through a rapid disposition phase with a half-life of 5 to 10 minutes, followed by a slower elimination phase with a half-life of 35 to 46 minutes.
  • The half-life of a drug refers to the time taken for the concentration of the drug in the body to decrease by half. This measure helps to determine the dosage amount and frequency.

Clearance and Volume of Distribution

  • The total plasma clearance of cefazolin was around 5.51 ml/min/kg, indicating the volume of plasma from which the drug would completely be removed per minute. The majority of this clearance was due to renal (kidney) clearance (5.39 ml/min/kg) of unchanged drug.
  • The volume of distribution at steady-state averaged 188 ml/kg. The volume of distribution indicates the extent to which the drug spreads throughout the body’s tissues.

Protein Binding and Bioavailability

  • The plasma protein binding of cefazolin at a concentration of 10 micrograms/ml averaged 8.1 +/- 1.9%. This indicates the proportion of the drug that binds to proteins in the blood, which can affect the drug’s distribution and elimination.
  • When given through the IM route, cefazolin was quickly absorbed; the degree of bioavailability was 78.4 +/- 18.8%, and the terminal half-life fluctuated between 49 to 99 minutes, meaning the drug was extensively absorbed with slightly slower elimination times after IM administration compared to IV administration.

Cite This Article

APA
Sams RA, Ruoff WW. (1985). Pharmacokinetics and bioavailability of cefazolin in horses. Am J Vet Res, 46(2), 348-352.

Publication

ISSN: 0002-9645
NlmUniqueID: 0375011
Country: United States
Language: English
Volume: 46
Issue: 2
Pages: 348-352

Researcher Affiliations

Sams, R A
    Ruoff, W W

      MeSH Terms

      • Animals
      • Biological Availability
      • Cefazolin / administration & dosage
      • Cefazolin / blood
      • Cefazolin / metabolism
      • Chromatography, High Pressure Liquid
      • Female
      • Half-Life
      • Horses / metabolism
      • Injections, Intramuscular / veterinary
      • Injections, Intravenous / veterinary
      • Protein Binding

      Citations

      This article has been cited 3 times.
      1. Kuroda T, Minamijima Y, Niwa H, Tamura N, Mita H, Fukuda K, Kaimachi M, Suzuki Y, Enoki Y, Taguchi K, Matsumoto K, Toutain PL, Bousquet-Melou A, Kasashima Y. Rational dosage regimens for cephalothin and cefazolin using pharmacokinetics and pharmacodynamics analysis in healthy horses.. Equine Vet J 2021 Nov;53(6):1239-1249.
        doi: 10.1111/evj.13406pubmed: 33341979google scholar: lookup
      2. Lee DH, Birhanu BT, Lee EB, Lee SJ, Boby N, Park YS, Park SC. Pharmacokinetic and pharmacodynamic integration for optimal dosage of cefquinome against Streptococcus equi subsp. equi in foals.. Vet Res 2020 Oct 15;51(1):131.
        doi: 10.1186/s13567-020-00853-2pubmed: 33059768google scholar: lookup
      3. Yáñez JA, Remsberg CM, Sayre CL, Forrest ML, Davies NM. Flip-flop pharmacokinetics--delivering a reversal of disposition: challenges and opportunities during drug development.. Ther Deliv 2011 May;2(5):643-72.
        doi: 10.4155/tde.11.19pubmed: 21837267google scholar: lookup