Urine bactericidal activity of pefloxacin versus norfloxacin in healthy female volunteers after a single 800-mg oral dose
Urine bactericidal activity of pefloxacin versus norfloxacin in healthy female volunteers after a single 800-mg oral dose
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健康女性志愿者单次口服 800 mg 剂量后培氟沙星与诺氟沙星的尿液杀菌活性
DOI：
10.1007/bf02113592
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发表时间：
1997
期刊：
影响因子：
7.5
通讯作者：
Dr. rer. nat. M. Kresken
中科院分区：
文献类型：
--
作者：
H. Hofbauer;P. D. K. G. Naber;Dr. rer. nat. Martina Kinzig;Prof. Dr. phil. nat. F. Sörgel;Dr. rer. nat. Cornelia Rustige;Prof. Dr. rer. nat. B. Wiedemann;Andrea Reiz;Dr. rer. nat. M. Kresken
在一项开放的随机交叉研究中，14名健康女性志愿者单次口服800毫克培氟沙星和诺氟沙星后，评估了尿液中培氟沙星和诺氟沙星的抗菌活性。培氟沙星在尿中的峰值浓度低于诺氟沙星(微生物法测定，平均为217.2 mg/L和492.9 mg/L)，但足够浓度的培氟沙星存在的时间比诺氟沙星长。微生物法检测，培氟沙星给药后7天和诺氟沙星给药后2天，尿液平均浓度至少为2 mg/L。总体而言，培氟沙星和诺氟沙星的尿液回收率分别占总用药量的49.3%和25.1%。尿液对5种受试菌的平均杀菌活性如下：对奈替沙星敏感的大肠埃希菌ATCC 25922对培氟沙星作用5天，对诺氟沙星作用2天，对3株临床分离株，每株各1株。对奈利地酸(NAL-R)、肺炎克雷伯菌、腐生葡萄球菌耐药，培氟沙星作用3天，诺氟沙星作用24小时，对粪肠球菌耐药，培氟沙星作用2天，诺氟沙星作用12小时。综上所述，培氟沙星单次给药对尿路病原菌具有足够高和持久的杀菌活性。这些发现支持了对7项临床试验的荟萃分析结果，这些试验针对无并发症的下尿路感染患者，表明单次口服800毫克培氟沙星与传统的对照药物治疗一样有效[21]。
In an open randomised crossover study the antibacterial activity of pefloxacin and norfloxacin was assessed in the urine after a single 800-mg oral dose in 14 healthy female volunteers. Pefloxacin demonstrated lower peak concentrations in the urine than norfloxacin (mean, 217.2 mg/l versus 492.9 mg/l as determined by the microbiological assay) but pefloxacin was present over a longer period of time in sufficient concentrations than norfloxacin. Mean urine levels of at least 2 mg/l were present for 7 days after pefloxacin administration and 2 days after norfloxacin administration as determined by the microbiological assay. Overall, the urinary recovery of pefloxacin and norfloxacin amounted to 49.3% and 25.1%, respectively, of the total administered dose. The average urine bactericidal activity against the five test organisms was as follows: against reference strainEscherichia coliATCC 25922 susceptible to nalidixic acid (Nal-S) for 5 days with pefloxacin and 2 days with norfloxacin; against three clinical isolates, one strain each ofE. coliresistant to nalidixic acid (Nal-R),Klebsiella pneumoniaeNal-R, andStaphylococcus saprophyticus, for 3 days with pefloxacin and 24 h with norfloxacin; and against a clinical isolate ofEnterococcus faecalisfor 2 days with pefloxacin and 12 h with norfloxacin. In conclusion, pefloxacin as a single dose proved to have sufficiently high and long-lasting urine bactericidal activity against urinary pathogens. These findings support the results of a meta-analysis of seven clinical trials in patients with uncomplicated lower UTI, demonstrating a single oral dose of 800 mg pefloxacin to be as effective as a conventional treatment with comparative drugs [21].