Cefquinome (HR 111V) in vitro evaluation of a broad-spectrum cephalosporin indicated for infections in animals

Murphy, Stephen P.; Erwin, Meridith E.; Jones, Ronald N.

doi:10.1016/0732-8893(94)90019-1

Cited by 43 publications

(46 citation statements)

References 7 publications

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“…Cefquinome (CFQ) is an aminothiazolyl cephalosporin developed exclusively for veterinary use (Murphy, Erwin, & Jones, ). It differs from older cephalosporins due to the addition of a quaternary ammonium side chain, which increases binding to penicillin‐binding proteins and the penetration into the periplasmatic space of gram‐negative bacilli (Bryskier, ; Murphy et al., ).…”

Section: Pharmacokinetic Parameters Of Cfq In Red‐eared Sliders (N = mentioning

confidence: 99%

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

Üney

Altan

Gül

et al. 2017

Vet Pharm & Therapeutics

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The purpose of this study was to evaluate the pharmacokinetics of cefquinome (CFQ) following single intravenous (IV) or intramuscular (IM) injections of 2 mg/kg body weight in red-eared slider turtles. Plasma concentrations of CFQ were determined by high-performance liquid chromatography and analyzed using noncompartmental methods. The pharmacokinetic parameters following IV injection were as follows: , and total body clearance (Cl T ) 12.66 ± 2.51 ml hr −1 kg −1. The pharmacokinetic parameters after IM injection were as follows: peak plasma concentration (C max ) 3.94 ± 0.84 μg/ml, time to peak concentration (T max ) 3 hr, t 1/2λz26.90 ± 4.33 hr, and AUC 0-∞ 145 ± 48 μg hr −1 ml −1. The bioavailability after IM injection was 88%. Data suggest that CFQ has a favorable pharmacokinetic profile with a long half-life and a high bioavailability in red-eared slider turtles. Further studies are needed to establish a multiple dosage regimen and evaluate clinical efficacy.

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Section: Pharmacokinetic Parameters Of Cfq In Red‐eared Sliders (N = mentioning

confidence: 99%

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

Üney

Altan

Gül

et al. 2017

Vet Pharm & Therapeutics

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“… T > MIC has been calculated for MICs of 0.06, 0.125, and 0.39 μg/ml on the basis of reported MIC 90s (0.06–0.39 μg/ml) for Escherichia coli , Pasteruella multocida, and Streptococcus agalactiae (Chin et al., ; Deshpande et al., ; Limbert et al., ; Murphy et al., ; Orden et al., ; Sheldon et al., ; Thomas et al., ; Wallmann et al., ). …”

Section: Pharmacokinetic Parameters (Mean ± Sd) Of Cefquinome In Buffmentioning

confidence: 99%

“…It is generally recommended that T > MIC should be at least 50% of the dosage interval to ensure an optimal bactericidal effect (Toutain & Lees, ). Considering the reported MIC 90s (0.06–0.39 μg/ml) for Escherichia coli , Pasteruella multocida, and Streptococcus agalactiae (Chin, Gu, Fang, & Neu, ; Deshpande, Pfaller, & Jones, ; Limbert et al., ; Murphy, Erwin, & Jones, ; Orden, Ruiz, Garcia, Cid, & Fuente, ; Sheldon, Bushnell, Montgomery, & Rycroft, ; Thomas et al., ; Wallmann et al., ), the T > MIC has been calculated for MICs of 0.06, 0.125, and 0.39 μg/ml. The experimental data presented here show that cefquinome at a dose of 2 mg/kg body weight at 24 hr interval is sufficient to maintain T > MIC above 58% following IM injection, respectively, for bacteria with MIC values ≤0.39 μg/ml.…”

Section: Pharmacokinetic Parameters (Mean ± Sd) Of Cefquinome In Buffmentioning

confidence: 99%

Pharmacokinetics of a single intramuscular injection of cefquinome in buffalo calves

Venkatachalam

Dumka

Ranjan

2017

Vet Pharm & Therapeutics

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The objective of this study was to investigate the pharmacokinetics of cefquinome following single intramuscular (IM) administration in six healthy male buffalo calves.Cefquinome was administered intramuscularly (2 mg/kg bodyweight) and blood samples were collected prior to drug administration and up to 24 hr after injection. No adverse effects or changes were observed after the IM injection of cefquinome.Plasma concentrations of cefquinome were determined by high-performance liquid chromatography. The disposition of plasma cefquinome is characterized by a monocompartmental open model. The pharmacokinetic parameters after IM administration (mean ± SE) were C max 6.93 ± 0.58 μg/ml, T max 0.5 hr, t ½kα 0.16 ± 0.05 hr, t ½β 3.73 ± 0.10 hr, and AUC 28.40 ± 1.30 μg hr/ml after IM administration. A dosage regimen of 2 mg/kg bodyweight at 24-hr interval following IM injection of cefquinome would maintain the plasma levels required to be effective against the bacterial pathogens with MIC values ≤0.39 μg/ml. The suggested dosage regimen of cefquinome has to be validated in the disease models before recommending for clinical use in buffalo calves.

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“…It shows antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative bacterial species and is stable against chromosomally and plasmid-encoded ␤-lactamases that are produced by a majority of clinically important bacteria (1,2). It has shown excellent activity against all the Enterobacteriaceae, with MIC 90 s ranging from Յ0.12 to ϳ2.0 g/ml (3).…”

mentioning

confidence: 99%

In Vivo Activity of Cefquinome against Escherichia coli in the Thighs of Neutropenic Mice

Liang

Wang

et al. 2014

Antimicrob Agents Chemother

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Cefquinome is a cephalosporin with broad-spectrum antibacterial activity, including activity against enteric Gram-negative bacilli such as Escherichia coli. We utilized a neutropenic mouse model of colibacillosis to examine the pharmacodynamic (PD) characteristics of cefquinome, as measured by organism number in homogenized thigh cultures after 24 h of therapy. Serum drug levels following 4-fold-escalating single doses of cefquinome were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The pharmacokinetic (PK) properties of cefquinome were linear over a dose range of 10 to 640 mg/kg of body weight. Serum half-lives ranged from 0.29 to 0.32 h. Dose fractionation studies over a 24-h dose range of 2.5 to 320 mg/kg were conducted every 3, 6, 12, or 24 h. Nonlinear regression analysis was used to determine which pharmacodynamic parameter best correlated with efficacy. The free percentage of the dosing interval that the serum levels exceed the MIC (fT >MIC ) was the PK-PD index that best correlated with efficacy (R 2 ‫؍‬ 73% for E. coli, compared with 13% for the maximum concentration of the free drug in serum [fC max ]/MIC and 45% for the free-drug area under the concentration-time curve from 0 to 24 h [fAUC 0-24 ]/ MIC). Subsequently, we employed a similar dosing strategy by using 4-fold-increasing total cefquinome doses administered every 4 h to treat animals infected with four additional E. coli isolates. A sigmoid maximum-effect (E max ) model was used to estimate the magnitudes of the %fT >MIC associated with net bacterial stasis, a 1-log 10 CFU reduction from baseline, and a 2-log 10 CFU reduction from baseline; the corresponding values were 28.01% ؎ 2.27%, 37.23% ؎ 4.05%, and 51.69% ؎ 9.72%. The potent bactericidal activity makes cefquinome an attractive option for the treatment of infections caused by E. coli.

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Cefquinome (HR 111V) in vitro evaluation of a broad-spectrum cephalosporin indicated for infections in animals

Cited by 43 publications

References 7 publications

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

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

Pharmacokinetics of a single intramuscular injection of cefquinome in buffalo calves

In Vivo Activity of Cefquinome against Escherichia coli in the Thighs of Neutropenic Mice

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