Pharmacokinetics, bioavailability and PK/PD relationship of cefquinome for Escherichia coli in Beagle dogs.

Abstract

The pharmacokinetics and bioavailability of cefquinome in Beagle dogs were determined by intravenous (IV), intramuscular (IM) or subcutaneous (SC) injection at a single dose of 2 mg/kg body weight (BW). The minimum inhibitory concentrations (MIC) of cefquinome against 217 Escherichia coli isolated from dogs were also investigated. After IV injection, the plasma concentration-time curve of cefquinome was analyzed using a two-compartmental model, and the mean values of t1/2α (h), t1/2β (h), Vss (L/kg), ClB (L/kg/h) and AUC (μg·h/mL) were 0.12, 0.98, 0.30, 0.24 and 8.51, respectively. After IM and SC administration, the PK data were best described by a one-compartmental model with first-order absorption. The mean values of t1/2Kel , t1/2Ka , tmax (h), Cmax (μg/mL) and AUC (μg·h/mL) were corresponding 0.85, 0.14, 0.43, 4.83 and 8.24 for IM administration, 0.99, 0.29, 0.72, 3.88 and 9.13 for SC injection. The duration of time that drug levels exceed the MIC (%T > MIC) were calculated using the determined MIC90 (0.125 μg/mL) and the PK data obtained in this study. The results indicated that the dosage regimen of cefquinome at 2 mg/kg BW with 12-h intervals could achieve %T > MIC above 50% that generally produced a satisfactory bactericidal effect against E. coli isolated from dogs in this study.

• Authors: Y F Zhou, D H Zhao, Y Yu, X Yang, W Shi, Y B Peng, Y H Liu
• Journal: Journal of veterinary pharmacology and therapeutics (J Vet Pharmacol Ther) Vol. 38 Issue 6 Pg. 543-8 (Dec 2015) ISSN: 1365-2885 [Electronic] England
• PMID: 25776615 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2015 John Wiley & Sons Ltd.

Chemical References

• Anti-Bacterial Agents
• Cephalosporins
• cefquinome

Topics

• Animals
• Anti-Bacterial Agents (administration & dosage, blood, pharmacology, therapeutic use)
• Biological Availability
• Cephalosporins (administration & dosage, blood, pharmacokinetics, therapeutic use)
• Dog Diseases (drug therapy, metabolism, microbiology)
• Dogs
• Escherichia coli (drug effects)
• Escherichia coli Infections (drug therapy, veterinary)
• Female
• Injections, Intramuscular (veterinary)
• Injections, Intravenous (veterinary)
• Injections, Subcutaneous (veterinary)
• Male
• Microbial Sensitivity Tests (veterinary)