Pharmacokinetics of cefquinome after single and repeated subcutaneous administrations in sheep.

The purpose of this study was to determine the pharmacokinetics of cefquinome (CFQ) following single and repeated subcutaneous (SC) administrations in sheep. Six clinically healthy, 1.5 ± 0.2 years sheep were used for the study. In pharmacokinetic study, the crossover design in three periods was performed. The withdrawal interval between the study periods was 15 days. In first period, CFQ (Cobactan, 2.5%) was administered by an intravenous (IV) bolus (3 sheep) and SC (3 sheep) injections at 2.5 mg/kg dose. In second period, the treatment administration was repeated via the opposite administration route. In third period, CFQ was administrated subcutaneously to each sheep (n = 6) at a dose of 2.5 mg/kg q. 24 hr for 5 days. Plasma concentrations of CFQ were measured using the HPLC-UV method. Pharmacokinetic parameters were calculated using non-compartmental methods. The elimination half-life and mean residence time of CFQ after the single SC administration were longer than IV administration (p < 0.05). Bioavailability (F%) of CFQ following the single SC administration was 123.51 ± 11.54%. The area under the curve (AUC0-∞ ) and peak concentration following repeated doses (last dose) were higher than those observed after the first dose (p < 0.05). CFQ accumulated after repeated SC doses. CFQ can be given via SC at a dose of 2.5 mg/kg every 24 hr for the treatment of infections caused by susceptible pathogens, which minimum inhibitory concentration is ≤1.0 μg/ml in sheep.

[1]  Y. Lu,et al.  In vivo activity of cefquinome against Riemerella anatipestifer using the pericarditis model in the duck. , 2016, Journal of veterinary pharmacology and therapeutics.

[2]  F. Mahmoud,et al.  Pharmacokinetics of cefquinome following multiple doses intramuscular administration in goats using HPLC , 2016 .

[3]  Yahong Liu,et al.  In Vivo Pharmacodynamics of Cefquinome in a Neutropenic Mouse Thigh Model of Streptococcus suis Serotype 2 at Varied Initial Inoculum Sizes , 2015, Antimicrobial Agents and Chemotherapy.

[4]  N. Zhang,et al.  Response of a clinical Escherichia coli strain to repeated cefquinome exposure in a piglet tissue-cage model , 2015, BMC Veterinary Research.

[5]  Shuyu Xie,et al.  Integration of PK/PD for dose optimization of Cefquinome against Staphylococcus aureus causing septicemia in cattle , 2015, Front. Microbiol..

[6]  K. A. Sadariya,et al.  Blood parameters on concurrent administration of cefquinome and tolfenamic acid in sheep , 2015 .

[7]  N. Zhang,et al.  In vivo evaluation of mutant selection window of cefquinome against Escherichia coli in piglet tissue-cage model , 2014, BMC Veterinary Research.

[8]  Z. Zeng,et al.  In Vivo Activity of Cefquinome against Escherichia coli in the Thighs of Neutropenic Mice , 2014, Antimicrobial Agents and Chemotherapy.

[9]  M. Aboubakr,et al.  Comparative Pharmacokinetics of Cefquinome (Cobactan 2.5%) following Repeated Intramuscular Administrations in Sheep and Goats , 2014, Journal of veterinary medicine.

[10]  Z. Zeng,et al.  Pharmacodynamics of Cefquinome in a Neutropenic Mouse Thigh Model of Staphylococcus aureus Infection , 2014, Antimicrobial Agents and Chemotherapy.

[11]  I. Wijnberg,et al.  Comparing the pharmacokinetics of a fourth generation cephalosporin in three different age groups of New Forest ponies. , 2012, Equine veterinary journal. Supplement.

[12]  K. Eltom,et al.  Prevalence of Staphylococcus aureus subsp. anaerobius in sub-clinical abscess cases of sheep. , 2012 .

[13]  M. A. Tohamy Age-related intramuscular pharmacokinetics of cefquinome in sheep , 2011 .

[14]  F. Altan,et al.  Development and Validation of a High-Performance Liquid Chromatography Method for Determination of Cefquinome Concentrations in Sheep Plasma and Its Application to Pharmacokinetic Studies , 2010, Antimicrobial Agents and Chemotherapy.

[15]  D. Paterson,et al.  Therapeutic drug monitoring of beta-lactams in critically ill patients: proof of concept. , 2010, International journal of antimicrobial agents.

[16]  A. Widmer,et al.  Comparison of the clinical efficacy of cefquinome with the combination of penicillin G and gentamicin in equine patients , 2009 .

[17]  D. Su,et al.  Pharmacokinetics and bioavailability of cefquinome in healthy piglets. , 2008, Journal of veterinary pharmacology and therapeutics.

[18]  S. Bell Respiratory disease in sheep , 2008, In Practice.

[19]  Jiang Chun-mao Pharmacokinetics of cefquinome sulfate suspension in pigs , 2007 .

[20]  M. Kietzmann,et al.  Tissue distribution of cefquinome after intramammary and "systemic" administration in the isolated perfused bovine udder. , 2006, Veterinary journal.

[21]  C. Wilhelm,et al.  Antibacterial activity of cefquinome against equine bacterial pathogens. , 2006, Veterinary microbiology.

[22]  D. Maes,et al.  Determination of cefquinome concentrations in bronchoalveolar lavage fluid , 2006 .

[23]  P. Toutain,et al.  Bioavailability and its assessment. , 2004, Journal of veterinary pharmacology and therapeutics.

[24]  P. Toutain,et al.  Volumes of distribution. , 2004, Journal of veterinary pharmacology and therapeutics.

[25]  K. Waldmann,et al.  Vorschläge der Arbeitsgruppe "Antibiotikaresistenz" für die Belegung von Mikrotiterplatten zur Empfindlichkeitsprüfung von Bakterien gegenüber antimikrobiellen Wirkstoffen in der Routinediagnostik: Mastitis- und Großtierlayouts , 2004 .

[26]  A. Böttner,et al.  Comparative field efficacy study between cefquinome and gentamicin in neonatal calves with clinical signs of septicaemia , 2004 .

[27]  P. Toutain,et al.  The pharmacokinetic-pharmacodynamic approach to a rational dosage regimen for antibiotics. , 2002, Research in veterinary science.

[28]  E. Zschiesche,et al.  A field study of cefquinome for the treatment of pigs with respiratory disease , 2002 .

[29]  J. Turnidge The Pharmacodynamics of β-Lactams , 1998 .

[30]  N. Shpigel,et al.  Efficacy of cefquinome for treatment of cows with mastitis experimentally induced using Escherichia coli. , 1997, Journal of dairy science.

[31]  R. Jones,et al.  Cefquinome (HR 111V). In vitro evaluation of a broad-spectrum cephalosporin indicated for infections in animals. , 1994, Diagnostic microbiology and infectious disease.

[32]  H. Neu,et al.  In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibiotics. , 1992, Diagnostic microbiology and infectious disease.

[33]  G. Seibert,et al.  Antibacterial activities in vitro and in vivo and pharmacokinetics of cefquinome (HR 111V), a new broad-spectrum cephalosporin , 1991, Antimicrobial Agents and Chemotherapy.

[34]  G. Fischer,et al.  Recent Developments in the Field of Cephem Antibiotics , 1989 .

[35]  W. Colburn Estimating the accumulation of drugs. , 1983, Journal of pharmaceutical sciences.

[36]  J. Rossum Pharmacokinetics of accumulation , 1968 .