Serrano-Rodríguez J M, Cárceles-García C, Cárceles-Rodríguez C M, Gabarda M L, Serrano-Caballero J M, Fernández-Varón E
Department of Pharmacology, Toxicology and Legal and Forensic Medicine, Faculty of Veterinary Medicine, University of Cordoba, Campus de Rabanales, Córdoba 14.071, Spain.
Department of Pharmacology. Faculty of Veterinary Medicine, University of Murcia, Campus de Espinardo, Murcia 30.071, Spain.
Vet Rec. 2017 Apr 15;180(15):376. doi: 10.1136/vr.103964. Epub 2017 Feb 17.
Minimum inhibitory concentration (MIC) and mutant prevention concentration (MPC) of veterinary fluoroquinolones as enrofloxacin, its metabolite ciprofloxacin, danofloxacin, difloxacin and marbofloxacin against strains (n=24) isolated from milk of sheep and goats affected by clinical mastitis were evaluated. The authors have used the MIC and MPC, as well as the pharmacokinetic-pharmacodynamic relationships in plasma and milk. MIC values were significantly different between drugs, unlike MPC values. Lower MIC values were obtained for danofloxacin and difloxacin, middle and higher values for enrofloxacin, ciprofloxacin and marbofloxacin. However, differences in MPC values were not found between drugs. At conventional doses, the AUC/MIC and AUC/MPC ratios were close to 30-80 hours and 5-30 hours, with exception of danofloxacin, in plasma and milk. The time inside the mutant selection window (T) was close to 3-6 hours for enrofloxacin, ciprofloxacin and marbofloxacin, near to 8 hours for danofloxacin and 12-22 hours for difloxacin. From these data, the mutant selection window could be higher for danofloxacin and difloxacin compared with the other fluoroquinolones tested. The authors concluded that enrofloxacin and marbofloxacin, at conventional doses, could prevent the selection of bacterial subpopulations of , unlike danofloxacin and difloxacin, where higher doses could be used.
评估了恩诺沙星、其代谢产物环丙沙星、达氟沙星、二氟沙星和马波沙星等兽用氟喹诺酮类药物对从患有临床乳腺炎的绵羊和山羊乳汁中分离出的菌株(n = 24)的最低抑菌浓度(MIC)和突变预防浓度(MPC)。作者使用了MIC和MPC以及血浆和乳汁中的药代动力学-药效学关系。药物之间的MIC值存在显著差异,而MPC值则不同。达氟沙星和二氟沙星的MIC值较低,恩诺沙星、环丙沙星和马波沙星的MIC值中等和较高。然而,各药物之间的MPC值未发现差异。在常规剂量下,除达氟沙星外,血浆和乳汁中的AUC/MIC和AUC/MPC比值分别接近30 - 80小时和5 - 30小时。恩诺沙星、环丙沙星和马波沙星在突变选择窗内的时间(T)接近3 - 6小时,达氟沙星接近8小时,二氟沙星为12 - 22小时。根据这些数据,与其他测试的氟喹诺酮类药物相比,达氟沙星和二氟沙星的突变选择窗可能更高。作者得出结论,在常规剂量下,恩诺沙星和马波沙星可以防止细菌亚群的选择,而达氟沙星和二氟沙星则不同,可能需要使用更高剂量。