Pharmacokinetics of difloxacin and its concentration in body fluids and endometrial tissues of mares after repeated intragastric administration.
Abstract: Pharmacokinetics of difloxacin and its distribution within the body fluids and endometrium of 6 mares were studied after intragastric (IG) administration of 5 individual doses. Difloxacin concentrations were serially measured in serum, urine, peritoneal fluid, synovial fluid, cerebrospinal fluid, and endometrium over 120 h. Bacterial susceptibility to difloxacin was determined for 174 equine pathogens over a 7-month period. Maximum serum concentration (Cmax) was 2.25 +/- 0.70 microg/mL at 3.12 +/- 2.63 h and Cmax after the 5th dose was 2.41 +/- 0.86 microg/mL at 97.86 +/- 1.45 h. The mean elimination half-life (t(1/2)) was 8.75 +/- 2.77 h and area under the serum concentration versus time curve (AUC) was 25.13 +/- 8.79 microg h/mL. Highest mean synovial fluid concentration was 1.26 +/- 0.49 microg/mL at 100 h. Highest mean peritoneal fluid concentration was 1.50 +/- 0.56 microg/mL at 98 h. Highest mean endometrial concentration was 0.78 +/- 0.48 microg/g at 97.5 h. Mean cerebrospinal fluid concentration was 0.87 +/- 0.52 microg/mL at 99 h. Highest mean urine concentration was 92.05 +/- 30.35 microg/mL at 104 h. All isolates of Salmonella spp. and Pasteurella spp. were susceptible. In general, gram-negative organisms were more susceptible than gram-positives. Difloxacin appears to be safe, adequately absorbed, and well distributed to body fluids and endometrial tissues of mares and may be useful in the treatment of susceptible bacterial infections in adult horses. μ μ μ μ μ μ μ μ Salmonella Pasteurella
Publication Date: 2005-09-29 PubMed ID: 16187554PubMed Central: PMC1176303
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Summary
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The researchers conducted a study on the pharmacokinetics of difloxacin, tracking its distribution in the body fluids and endometrial tissues of six horses after repeated doses administered orally. The tests noted difloxacin’s efficacy in treating bacterial infections in horses, particularly against Salmonella and Pasteurella strains.
Study Objectives and Methodology
- The main objective of this research was to study the behaviour of difloxacin, an antibiotic, in horses. This involved determining how long the drug takes to get absorbed in the body, its distribution in various body fluids and endometrial tissues, and how effectively and quickly it gets eliminated from the body. Moreover, the study also aimed to observe the drug’s effectiveness on different equine pathogens.
- The study was conducted using six horses to which difloxacin was repeatedly administered orally. The difloxacin concentrations were then serially examined over a period of 120 hours in various body fluids including serum, urine, peritoneal fluid, synovial fluid, cerebrospinal fluid, and endometrium.
- Additionally, the susceptibility of 174 equine pathogens to difloxacin was assessed over seven months.
Results and Observations
- The study recorded the maximum serum concentration of difloxacin to be 2.25 +/- 0.70 micrograms/mL at around 3.12 +/- 2.63 hours, and after the fifth dose, the concentration was found to be 2.41 +/- 0.86 micrograms/mL at approximately 97.86 +/- 1.45 hours.
- The average elimination half-life of the drug was observed to be around 8.75 +/- 2.77 hours. The area under the serum concentration versus time curve, a key metric in pharmacology that helps in determining the drug’s bioavailability, was found to be 25.13 +/- 8.79 microgram hours/mL.
- Furthermore, the researchers found that gram-negative organisms were more susceptible to difloxacin than gram-positive ones. All the tested strains of Salmonella and Pasteurella were susceptible to the antibiotic, proving its potential effectiveness in treating these infections in adult horses.
Conclusion
- Based on the data gathered, the researchers concluded that difloxacin appears to be a safe drug that is adequately absorbed and well-distributed across body fluids and endometrial tissues in horses.
- However, while difloxacin might prove to be an effective treatment for bacterial infections susceptible to this drug, the specifics of its use, such as the correct dosage and treatment duration, should be further investigated for optimal results.
Cite This Article
APA
Adams AR, Haines GR, Brown MP, Gronwall R, Merritt K.
(2005).
Pharmacokinetics of difloxacin and its concentration in body fluids and endometrial tissues of mares after repeated intragastric administration.
Can J Vet Res, 69(3), 229-235.
Publication
Researcher Affiliations
- Department of Large Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville, Florida 32610-0136, USA.
MeSH Terms
- Animals
- Anti-Bacterial Agents / pharmacokinetics
- Area Under Curve
- Ascitic Fluid / chemistry
- Ascitic Fluid / metabolism
- Bacteria / drug effects
- Body Fluids / chemistry
- Body Fluids / metabolism
- Ciprofloxacin / analogs & derivatives
- Ciprofloxacin / pharmacokinetics
- Endometrium / chemistry
- Endometrium / metabolism
- Female
- Fluoroquinolones / pharmacokinetics
- Half-Life
- Horses / metabolism
- Intestinal Absorption / drug effects
- Microbial Sensitivity Tests
- Synovial Fluid / chemistry
- Synovial Fluid / metabolism
- Tissue Distribution
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