Influence of the Injection Site on the Pharmacokinetics of Cefquinome Following Intramuscular Injection in Piglets

Song, In Bae; Kim, Tae Won; Lee, Hong Gee; Kim, Myoung Seok; Hwang, Youn–Hwan; Park, Byung Kwon; Lim, Jong Hwan; Yun, Hyo In

doi:10.1292/jvms.12-0201

Cited by 8 publications

(8 citation statements)

References 15 publications

(32 reference statements)

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“…The diffusion of cefquinome in the body tissues of different animal species is very small. In this study, barely 0.32 L ⁄kg of V ss was obtained in black swans similar to 0.25 L/kg in piglets and 0.19 L/kg in pigs [ 21 , 22 ]. According to the CVMP report, an attenuated distribution of cefquinome to intracellular spaces was due to low fat solubility and that it acts as an organic acid with a low pKa of 2.51 or 2.91 [ 5 ].…”

Section: Discussionmentioning

confidence: 82%

Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans (Cygnus atratus)

Wang

Zhao

2017

BMC Vet Res

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BackgroundThe objective of this study is to investigate pharmacokinetics and dose regimens of cefquinome in black swans following intravenous (IV) and intramuscular (IM) administration at a single dose of 2 mg/kg. The MICs of cefquinome against 49 Escherichia coli isolates from black swans were determined. Monte Carlo simulation was applied to conduct the dose regimen assessment and optimization of cefquinome against E. coli in black swans, and a pharmacokinetic/pharmacodynamic (PK/PD) cutoff was established for E. coli isolates obtained in this study.ResultsThe PK parameters of T1/2α (0.31 h), T1/2β (1.69 h) and ClB (0.13 L/kg·h) indicated a rapid distribution and elimination of cefquinome in black swans after IV administration. After IM injection, the corresponding PK parameters of T1/2Ka, T1/2Ke, Tmax, Cmax, and F were 0.12 h, 1.62 h, 0.39 h, 5.71 μg/mL and 74.2%, respectively. The MICs of cefquinome against black swans E. coli ranged from 0.03 to 8 μg/mL, with MIC50 and MIC90 of 0.06 and 0.5 μg/mL, respectively. The PK/PD cutoff of cefquinome against E. coli was determined to be 0.2 μg/mL. Monte Carlo simulation showed that the nominal dose regimen (2 mg/kg/24 h) could not achieve a satisfactory probability of target attainment (PTA) for %TMIC ≥ 50%, indicating a risk of treatment failure and the development of potential drug resistance.ConclusionsThe current daily dosage of cefquinome when divided into 12-h interval (1 mg/kg/12 h) may be effective for the treatment of E. coli infections with an MIC ≤0.5 μg/mL.Electronic supplementary materialThe online version of this article (doi:10.1186/s12917-017-1148-7) contains supplementary material, which is available to authorized users.

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Section: Discussionmentioning

confidence: 82%

Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans (Cygnus atratus)

Wang

Zhao

2017

BMC Vet Res

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“…The bioavailability ( F ) and time to peak concentration ( t max ) of cefquinome following IM administration were 97.8% and 0.43 h, respectively, reflecting its almost complete and relatively rapid absorption. These values were compatible with the results previously reported ranging from 93.3% to 103% and 0.38 to 0.45 h in mice, piglets and ducks, respectively (Limbert et al ., ; Yuan et al ., ; Song et al ., ). Compared to IM administration bioavailability of 98%, similar full bioavailability (107%) following SC injection was obtained.…”

Section: Discussionmentioning

confidence: 97%

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

Zhou

Zhao

et al. 2015

Vet Pharm & Therapeutics

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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.

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“…Generally, the V ss from various species animals existed at low values, which indicated that cefquinome probably distributed mainly in the plasma compartment. The clearance rate (Cl) of cefquinome in dog (0.49 L·kg/h) in this study was higher than 0.18–0.34 L·kg/h in piglets, sows, wild boars, sheep, goats, rabbits, ducks and chicken (Song et al ., ; Block et al ., ; Uney et al ., ; Errecalde et al ., ; Hwang et al ., ; Yuan et al ., ; Xie et al ., ). These limited distributions and low clearance rate of cefquinome in the various species could be attributed to low fat solubility, protein binding activity and its pKa values of 2.51–2.91 (Hwang et al ., ; Zhang et al ., ).…”

Section: Discussionmentioning

confidence: 99%

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

Zhang

et al. 2013

Vet Pharm & Therapeutics

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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.

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Influence of the Injection Site on the Pharmacokinetics of Cefquinome Following Intramuscular Injection in Piglets

Cited by 8 publications

References 15 publications

Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans (Cygnus atratus)

Pharmacokinetics, bioavailability and dose assessment of Cefquinome against Escherichia coli in black swans (Cygnus atratus)

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

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

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