Jha K, Roy B K, Singh R C
Department of Pharmacology and Toxicology, Ranchi Veterinary College, India.
Vet Res Commun. 1996;20(5):473-9. doi: 10.1007/BF00419185.
The kinetic profiles of norfloxacin were evaluated in afebrile, febrile and probenecid pre-treated (70 mg/kg orally) febrile goats after a single intravenous (i.v.) dose (5 mg/kg). Fever was induced and maintained for 12 h by injecting Escherichia coli endotoxin (0.2 microgram/kg, i.v.) and repeating it in half the dose (0.1 microgram/kg) 5 h later. The plasma pharmacokinetic values for norfloxacin were best represented using a two-compartment open model. The peak norfloxacin plasma level of 90.52 +/- 3.18 micrograms/ml attained in the probenecid pre-treated febrile goats was higher than that in the febrile (75.46 +/- 0.72 micrograms/ml) or afebrile goats (62.25 +/- 1.23 micrograms/ml). ClB and Kel values were significantly (p < 0.01) decreased in febrile compared with afebrile goats. These values were further reduced in febrile goats after probenecid pre-treatment. However, t1/2 beta was not affected by the fever-probenecid interaction. Norfloxacin may be used as an infusion with probenecid in caprine diseases where very high plasma levels are required to combat resistant organisms such as Bacteroides.
在单次静脉注射（5毫克/千克）诺氟沙星后，对无热、发热以及经丙磺舒预处理（口服70毫克/千克）的发热山羊的诺氟沙星动力学特征进行了评估。通过静脉注射大肠杆菌内毒素（0.2微克/千克）诱导并维持发热12小时，并在5小时后以半量（0.1微克/千克）重复注射。诺氟沙星的血浆药代动力学值最适合用二室开放模型表示。经丙磺舒预处理的发热山羊中诺氟沙星的血浆峰值水平为90.52±3.18微克/毫升，高于发热山羊（75.46±0.72微克/毫升）或无热山羊（62.25±1.23微克/毫升）。与无热山羊相比，发热山羊的清除率（ClB）和消除速率常数（Kel）值显著降低（p<0.01）。在经丙磺舒预处理的发热山羊中，这些值进一步降低。然而，消除半衰期（t1/2β）不受发热-丙磺舒相互作用的影响。在山羊疾病中，当需要非常高的血浆水平来对抗如拟杆菌等耐药菌时，诺氟沙星可与丙磺舒一起用作静脉输注药物。
