Pharmacokinetics and endometrial tissue concentrations of enrofloxacin and the metabolite ciprofloxacin after i.v. administration of enrofloxacin to mares.
Abstract: Enrofloxacin was administered i.v. to five adult mares at a dose of 5 mg/kg. After administration, blood and endometrial biopsy samples were collected at regular intervals for 24 h. The plasma and tissue samples were analyzed for enrofloxacin and the metabolite ciprofloxacin by high-pressure liquid chromatography. In plasma, enrofloxacin had a terminal half-life (t(1/2)), volume of distribution (area method), and systemic clearance of 6.7 +/- 2.9 h, 1.9 +/- 0.4 L/kg, and 3.7 +/- 1.4 mL/kg/min, respectively. Ciprofloxacin had a maximum plasma concentration (Cmax) of 0.28 +/- 0.09 microg/mL. In endometrial tissue, the enrofloxacin Cmax was 1.7 +/- 0.5 microg/g, and the t(1/2) was 7.8 +/- 3.7 h. Ciprofloxacin Cmax in tissues was 0.15 +/- 0.04 microg/g and the t(1/2) was 5.2 +/- 2.0 h. The tissue:plasma enrofloxacin concentration ratios (w/w:w/v) were 0.175 +/- 0.08 and 0.47 +/- 0.06 for Cmax and AUC, respectively. For ciprofloxacin, these values were 0.55 +/- 0.13 and 0.58 +/- 0.31, respectively. We concluded that plasma concentrations achieved after 5 mg/kg i.v. are high enough to meet surrogate markers for antibacterial activity (Cmax:MIC ratio, and AUC:MIC ratio) considered effective for most susceptible gram-negative bacteria. Endometrial tissue concentrations taken from the mares after dosing showed that enrofloxacin and ciprofloxacin both penetrate this tissue adequately after systemic administration and would attain concentrations high enough in the tissue fluids to treat infections of the endometrium caused by susceptible bacteria.
Publication Date: 2002-11-09 PubMed ID: 12423224DOI: 10.1046/j.1365-2885.2002.00434.xGoogle Scholar: Lookup
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- Journal Article
Summary
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This research study investigates the behavior of the drug Enrofloxacin and its metabolite Ciprofloxacin in the bodies of mares following intravenous injection. Results revealed that this drug and its metabolite are effectively distributed in the blood and can penetrate the endometrial tissue, where they remain at sufficient concentrations to fight against bacterial infections.
Research Methodology
- The experiment was carried out on five adult mares. Each animal was given an intravenous dose of Enrofloxacin at a concentration of 5mg/kg.
- After administering the drug, blood and endometrial biopsy samples were taken from each animal at regular intervals for a period of 24 hours. These samples were used to monitor the presence and behavior of Enrofloxacin and its metabolite, Ciprofloxacin, in the blood plasma and endometrial tissue.
- The samples were analyzed using high-pressure liquid chromatography, a reliable method for isolating and quantifying compounds.
Key Findings
- In the plasma, the half-life of Enrofloxacin was around 6.7 hours, signifying that it took this time for half of the drug to be eliminated from the body.
- The volume of distribution for Enrofloxacin in the blood was approximately 1.9 L/kg, indicating the apparent space in the body available to contain the drug.
- In contrast, the maximum plasma concentration (Cmax) of Ciprofloxacin, the metabolite that Enrofloxacin breaks down into, was 0.28 micrograms/mL.
- In the endometrial tissue, Enrofloxacin was present at a maximum concentration of around 1.7 micrograms/g, and had a longer half-life of approximately 7.8 hours. Its metabolite Ciprofloxacin had a Cmax of 0.15 micrograms/g and a shorter half-life of about 5.2 hours.
Conclusions
- The study concluded that the plasma concentrations achieved after a 5 mg/kg intravenous dosage of Enrofloxacin are high enough to effectively combat most susceptible gram-negative bacteria.
- The results also showed that both Enrofloxacin and Ciprofloxacin adequately penetrate the endometrial tissue after systemic administration. Therefore, they would reach high enough concentrations in the tissue fluids to treat infections of the endometrium caused by susceptible bacteria.
- Thus, the study sheds light on the effective use of Enrofloxacin for treating endometrial infections in mares.
Cite This Article
APA
Papich MG, Van Camp SD, Cole JA, Whitacre MD.
(2002).
Pharmacokinetics and endometrial tissue concentrations of enrofloxacin and the metabolite ciprofloxacin after i.v. administration of enrofloxacin to mares.
J Vet Pharmacol Ther, 25(5), 343-350.
https://doi.org/10.1046/j.1365-2885.2002.00434.x Publication
Researcher Affiliations
- Department of Molecular Biomedical Sciences, College of Veterinary Medicine, North Carolina State University, 4700 Hillsborough Street, Raleigh, NC 27606, USA. mark_papich@ncsu.edu
MeSH Terms
- Animals
- Anti-Infective Agents / administration & dosage
- Anti-Infective Agents / blood
- Anti-Infective Agents / pharmacokinetics
- Area Under Curve
- Chromatography, High Pressure Liquid / veterinary
- Ciprofloxacin / administration & dosage
- Ciprofloxacin / blood
- Ciprofloxacin / pharmacokinetics
- Endometrium / metabolism
- Enrofloxacin
- Female
- Fluoroquinolones
- Horses / metabolism
- Infusions, Intravenous / veterinary
- Quinolones / administration & dosage
- Quinolones / blood
- Quinolones / pharmacokinetics
Citations
This article has been cited 3 times.- Kang J, Hossain MA, Park HC, Kim Y, Lee KJ, Park SW. Pharmacokinetic and pharmacodynamic integration of enrofloxacin against Salmonella Enteritidis after administering to broiler chicken by per-oral and intravenous routes.. J Vet Sci 2019 Mar;20(2):e15.
- Slate AR, Bandyopadhyay S, Francis KP, Papich MG, Karolewski B, Hod EA, Prestia KA. Efficacy of enrofloxacin in a mouse model of sepsis.. J Am Assoc Lab Anim Sci 2014 Jul;53(4):381-6.
- Hwang YH, Kim MS, Song IB, Lim JH, Park BK, Yun HI. Altered pharmacokinetics of enrofloxacin in experimental models of hepatic and renal impairment.. Vet Res Commun 2009 Jun;33(5):481-7.
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