Naber K G, Theuretzbacher U, Moneva-Koucheva G, Stass H
Department of Urology, Hospital St. Elisabeth, Straubing, Germany.
Eur J Clin Microbiol Infect Dis. 1999 Nov;18(11):783-9. doi: 10.1007/s100960050401.
Twelve healthy volunteers participated in a randomized crossover study to compare urinary concentrations, serum parameters, and urinary bactericidal activity of ciprofloxacin after single intravenous (i.v.) doses of 200 mg and 400 mg and an oral (p.o.) dose of 500 mg. The median serum concentrations at 1 h after administration were 1 microg/ml, 4.3 microg/ml, and 2.2 microg/ml, respectively. Between the first collection period (0-2 h) and the last collection period (38-48 h), the median urinary concentrations decreased from 394 microg/ml, 675 microg/ml, and 585 microg/ml, respectively, to 0.3 microg/ml, 0.6 microg/ml, and 1 microg/ml, respectively. The urinary concentrations after the 400 mg i.v. and the 500 mg p.o. doses were not statistically different but were significantly higher than those after the 200 mg i.v. dose. The urinary bactericidal titers (UBTs), defined as the highest urinary dilution bactericidal for the organism tested, were determined against Escherichia coli (ATCC 25922) and eight uropathogens up to 48 h after administration of ciprofloxacin. The UBTs after the 400 mg i.v. and the 500 mg p.o. doses were similar and were significantly higher (P < 0.05) than those following the 200 mg i.v. dose. After 400 mg i.v. and 500 mg p.o., median UBTs of > or = 1:4 were present up to 48 h for all strains for which the MIC was < or = 0.5 microg/ml, except for one nalidixic-acid resistant Escherichia coli strain for which the MIC was 0.25 microg/ml. Species for which the MIC is > or = 1 microg/ml showed median UBTs of > or = 1:4 for 8-16 h. Median UBTs of > or = 1:4 were present up to 8 and 12 h for both Pseudomonas strains tested. A once-daily dosage of 400 mg i.v. or 500 mg p.o. might be sufficient for treatment of urinary tract infections caused by highly susceptible pathogens. A twice-daily dosing scheme seems to be preferable for complicated infections caused by pathogens with intermediate susceptibilty (MIC > or = 1 microg/ml) or for empiric therapy.
12名健康志愿者参与了一项随机交叉研究，以比较单次静脉注射（i.v.）200mg和400mg以及口服（p.o.）500mg环丙沙星后的尿药浓度、血清参数和尿杀菌活性。给药后1小时的血清浓度中位数分别为1μg/ml、4.3μg/ml和2.2μg/ml。在第一个收集期（0 - 2小时）和最后一个收集期（38 - 48小时）之间，尿药浓度中位数分别从394μg/ml、675μg/ml和585μg/ml降至0.3μg/ml、0.6μg/ml和1μg/ml。400mg静脉注射剂量和500mg口服剂量后的尿药浓度无统计学差异，但显著高于200mg静脉注射剂量后的尿药浓度。尿杀菌效价（UBTs）定义为对受试菌的最高尿稀释杀菌浓度，在给予环丙沙星后长达48小时内针对大肠埃希菌（ATCC 25922）和8种尿路致病菌进行测定。400mg静脉注射剂量和500mg口服剂量后的UBTs相似，且显著高于200mg静脉注射剂量后的UBTs（P < 0.05）。静脉注射400mg和口服500mg后，对于所有最低抑菌浓度（MIC）≤0.5μg/ml的菌株，除了一株耐萘啶酸的大肠埃希菌菌株（其MIC为0.25μg/ml）外，在长达48小时内UBTs中位数≥1:4。MIC≥1μg/ml的菌株在8 - 16小时内UBTs中位数≥1:4。对于所测试的两种假单胞菌菌株，UBTs中位数≥1:4分别持续至8小时和12小时。每日一次静脉注射400mg或口服500mg的给药方案可能足以治疗由高度敏感病原体引起的尿路感染。对于由中度敏感病原体（MIC≥1μg/ml）引起的复杂感染或经验性治疗，每日两次给药方案似乎更可取。
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