CLINICAL PHARMACOKINETICS OF PARENTERALLY ADMINISTERED DANOFLOXACIN IN CATTLE
CLINICAL PHARMACOKINETICS OF PARENTERALLY ADMINISTERED DANOFLOXACIN IN CATTLE
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DOI：
10.1111/j.1365-2885.1991.tb00854.x
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发表时间：
1991-12-01
影响因子：
1.3
通讯作者：
RICE, JR
中科院分区：
文献类型：
--
作者：
GILES, CJ;MAGONIGLE, RA;RICE, JR
达诺沙星是一种新的氟喹诺酮类抗菌药物，专门为兽医开发。对其体外活性和药代动力学性质进行了研究，以评估其在治疗牛呼吸道疾病方面的潜力。丹诺沙星对牛呼吸道主要致病菌--溶血性巴氏杆菌、多杀性巴氏杆菌和睡眠嗜血杆菌的最低抑菌浓度为0.125-mU·g/ml。丹诺沙星在肌肉内和皮下注射后迅速吸收，生物利用度几乎完全(分别为101%和94%)。达诺沙星在肌内和皮下给药的血药浓度曲线相似，连续给药1、3或5天后的血药浓度-时间曲线下面积(AUC)无显著差异，但肌内给药的血药浓度峰值略高。肌肉给药后，达诺沙星在肺内的平均峰值浓度是血浆浓度的4.1倍。同样，肺组织的AUC是血浆的3.7倍。这些数据表明，达诺沙星特别适合于治疗牛细菌性呼吸道疾病。
Danofloxacin is a new fluoroquinolone antibacterial, developed specifically for veterinary use. Its in vitro activity and pharmacokinetic properties have been investigated to assess its potential for use in the therapy of respiratory disease in cattle. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, was 0.125-mu-g/ml. The plasma and lung kinetics of danofloxacin following parenteral administration of 1.25 mg/kg were evaluated in two studies. Danofloxacin was rapidly absorbed following intramuscular and subcutaneous injection and bioavailability was virtually complete (101% and 94% respectively). Plasma concentration profiles of danofloxacin were similar for intramuscular and subcutaneous routes with no significant differences in the area under the plasma concentration-time curves (AUC) following one, three or five consecutive daily doses, although slightly higher peak plasma concentrations were achieved by the intramuscular route. Following intramuscular administration, the mean peak lung concentration of danofloxacin was 4.1 times greater than that of plasma. Similarly, the AUC for lung tissue was 3.7 times greater than that for plasma. These data indicate that danofloxacin should be particularly appropriate for the therapy of bacterial respiratory disease in cattle.