Walker R D, Stein G E, Hauptman J G, MacDonald K H
Animal Health Diagnostic Laboratory, College of Veterinary Medicine, Michigan State University, East Lansing 48824.
Am J Vet Res. 1992 Dec;53(12):2315-9.
Enrofloxacin was administered orally to 6 healthy dogs at dosages of approximately 2.75, 5.5, and 11 mg/kg of body weight, every 12 hours for 4 days, with a 4-week interval between dosage regimens. Serum and tissue cage fluid (TCF) concentrations of enrofloxacin were measured after the first and seventh treatments. The mean peak serum concentration occurred between 1 and 2.5 hours after dosing. Peak serum concentrations increased with increases in dosage. For each dosage regimen, there was an accumulation of enrofloxacin between the first and seventh treatment, as demonstrated by a significant (P = 0.001) increase in peak serum concentrations. The serum elimination half-life increased from 3.39 hours for the 2.75 mg/kg dosage to 4.94 hours for the 11 mg/kg dosage. Enrofloxacin accumulated slowly into TCF, with peak concentrations being approximately 58% of those of serum. The time of peak TCF concentrations occurred between 3.8 hours and 5.9 hours after drug administration, depending on the dosage and whether it was after single or multiple administrations. Compared with serum concentrations (area under the curve TCF/area under the curve serum), the percentage of enrofloxacin penetration into TCF was 85% at a dosage of 2.75 mg/kg, 83% at a dosage of 5.5 mg/kg, and 88% at a dosage of 11 mg/kg. All 3 dosage regimens of enrofloxacin induced continuous serum and TCF concentrations greater than the minimal concentration required to inhibit 90% (MIC90) of the aerobic and facultative anaerobic clinical isolates tested, except Pseudomonas aeruginosa.(ABSTRACT TRUNCATED AT 250 WORDS)
恩诺沙星以大约2.75、5.5和11毫克/千克体重的剂量口服给予6只健康犬,每12小时给药一次,持续4天,给药方案之间间隔4周。在首次和第七次治疗后测量恩诺沙星的血清和组织笼液(TCF)浓度。给药后1至2.5小时出现平均血清峰值浓度。血清峰值浓度随剂量增加而升高。对于每种给药方案,首次和第七次治疗之间恩诺沙星有蓄积,血清峰值浓度显著升高(P = 0.001)证明了这一点。血清消除半衰期从2.75毫克/千克剂量的3.39小时增加到11毫克/千克剂量的4.94小时。恩诺沙星缓慢蓄积到TCF中,峰值浓度约为血清峰值浓度的58%。TCF峰值浓度出现时间在给药后3.8小时至5.9小时之间,具体取决于剂量以及是单次还是多次给药。与血清浓度相比(TCF曲线下面积/血清曲线下面积),恩诺沙星在2.75毫克/千克剂量时进入TCF的渗透率为85%,在5.5毫克/千克剂量时为83%,在11毫克/千克剂量时为88%。除铜绿假单胞菌外,恩诺沙星的所有3种给药方案诱导的血清和TCF浓度持续高于抑制所测试的需氧和兼性厌氧临床分离株90%(MIC90)所需的最低浓度。(摘要截断于250字)