Pharmacokinetics and ex‐vivo pharmacodynamics of cefquinome against Klebsiella pneumonia in healthy dogs

Abstract

A two-period cross-over study was carried to investigate the pharmacokinetics (PK) and ex-vivo pharmacodynamics (PD) of cefquinome when administrated intravenously (IV) and intramuscularly (IM) in seven healthy dogs at a dose of 2 mg/kg of body weight. Serum concentrations were determined by HPLC-MS/MS assay and cefquinome concentration vs. time data after IV and IM were best fit to a two-compartment open model. Cefquinome mean values of area under concentration-time curve (AUC) were 5.15 μg · h/mL for IV dose and 4.59 μg · h/mL for IM dose. Distribution half-lives and elimination half-lives after IV dose and IM dose were 0.27 and 0.44 h, 1.53 and 1.94 h, respectively. Values of total body clearance (ClB ) and volume of distribution at steady-state (Vss ) were 0.49 L · kg/h and 0.81 L/kg, respectively. After IM dose, Cmax was 2.53 μg/mL and the bioavailability was 89.13%. For PD profile, the determined MIC and MBC values against K. pneumonia were 0.030 and 0.060 μg/mL in MHB and 0.032 and 0.064 μg/mL in serum. The ex vivo time-kill curves also were established in serum. In conjunction with the data on MIC, MBC values and the ex vivo bactericidal activity in serum, the present results allowed prediction that a single cefquinome dosage of 2 mg/kg may be effective in dogs against K. pneumonia infection.

Pharmacokinetic and Pharmacodynamic Evaluation of Marbofloxacin in Pig against Korean Local Isolates ofActinobacillus pleuropneumoniae

“…PK/PD indices, such as C max /MIC and AUC 0–24 h /MIC values of the target organism, have been used to predict the clinical efficacy of antibacterial agents. Another important PK/PD parameter to describe drug efficacy is the time during which the drug concentration exceeds the MIC ( T > MIC) [42]. It is generally recommended that T > MIC should be at least 50% of the dosage interval to ensure an optimal bactericidal effect [42, 43].…”

“…Another important PK/PD parameter to describe drug efficacy is the time during which the drug concentration exceeds the MIC ( T > MIC) [42]. It is generally recommended that T > MIC should be at least 50% of the dosage interval to ensure an optimal bactericidal effect [42, 43]. During the present study, to optimize the marbofloxacin dosage regimen, we also calculated the T > MIC at a dose of 2.50 mg/kg of body weight in pigs after i.v., i.m., and p.o.…”

Pharmacokinetics of cefquinome in red‐eared slider turtles (Trachemys scripta elegans) after single intravenous and intramuscular injections

“…CFQ could potentially be used for the treatment of many turtle diseases. Pharmacokinetic studies of CFQ have been investigated in salmon (San Martín, Bataglia, Hernández, Quiroz, & Cañon, ), camels (Al‐Taher, ), rabbits (Hwang et al., ), sheep (Tohamy, ; Uney, Altan, & Elmas, ), ducks (Yuan et al., ), ponies (Smiet, Haritova, Heil, Fink‐Gremmels, & Wijnberg, ), cross‐bred wild boars (Liu et al., ), chickens (Xie, Zhang, Wang, & Du, ), pigs (Zhao et al., ), cattle (Shan et al., ), tilapia (Shan et al., ), dogs (Zhang et al., ), buffalo calves (Venkatachalam & Dumka, ), and horses (Uney et al., ). These studies have reported favorable pharmacokinetic features of CFQ, such as good absorption, high bioavailability, and primary elimination via the kidney.…”

Investigation of kinetic and tissue residues of cefquinome after its intramuscular administration in experimentally infected rabbits with Klebsiella pneumoniae

“…In certain cases, the use of some antibiotics resulted in a significant decrease in the K. pneumoniaenumbers; nevertheless, treatment may be re-stricted if the bacterium produces an extendedspectrum ꞵ-lactamase (ESBL). ESBLproducing K. pneumoniae, which is reluctant to different antibacterial therapies (Lautenbach et al, 2001;Zhang et al, 2014), should be medicated by an extra-lactamase-stable antibacterial.…”