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培氟沙星与环丙沙星治疗慢性呼吸道感染的对比活性

Comparative activities of pefloxacin and ciprofloxacin in the treatment of chronic respiratory tract infections.

作者信息

Scaglione F, Scamazzo F, Arcidiacono M M, Cogo R, Monzani G P, Fraschini F

机构信息

Department of Pharmacology, University of Milan, Italy.

出版信息

J Chemother. 1995 Apr;7(2):140-5. doi: 10.1179/joc.1995.7.2.140.

DOI:10.1179/joc.1995.7.2.140
PMID:7666121
Abstract

To determine the efficacy in vivo of pefloxacin and ciprofloxacin in the treatment of acute infectious bronchopneumopathies, 90 patients, suffering from acute exacerbation of chronic bronchitis and with no known allergies to quinolones, were admitted to the study. Patients were randomly divided into three groups of 30; the first group was dosed with pefloxacin 800 mg i.v. every 24 hours; the second group with pefloxacin 800 mg per os every 24 hours and the third with 500 mg per os of ciprofloxacin every 12 hours. Blood and bronchial secretion samples were simultaneously collected 2, 4, 8, 12, 14 and 24 hours after the first daily dose of antibiotic. Serum and bronchial secretion concentrations of pefloxacin and ciprofloxacin were determined by using a microbiological agar disk diffusion assay, employing Escherichia coli Kp 712 as test organism. Eradication of responsible microorganisms (Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis) were achieved in 98% of patients around 72 hours post treatment. Generally, both antibiotics expressed similar bactericidal properties when orally administered, while intravenous administration of pefloxacin displays a more rapid antibacterial action in comparison with the oral administration schedules. Maximal concentrations of both drugs in bronchial secretion were recorded at the same time after treatment (4 hours), with concentrations of about 2.5 micrograms/ml. Pefloxacin, having a longer half-life, was found 24 hours post-treatment with plasma concentrations of 1.5 micrograms/ml following a single oral dose of 800 mg. Ciprofloxacin, having a shorter half-life, showed a peak of about 1 microgram/ml, 12 hours after administration (500 mg/12 hours/os).

摘要

为确定培氟沙星和环丙沙星治疗急性感染性支气管肺炎的体内疗效,90例慢性支气管炎急性加重且对喹诺酮类药物无已知过敏史的患者被纳入研究。患者被随机分为三组,每组30人;第一组每24小时静脉注射800毫克培氟沙星;第二组每24小时口服800毫克培氟沙星,第三组每12小时口服500毫克环丙沙星。在每日首次给予抗生素后的2、4、8、12、14和24小时同时采集血液和支气管分泌物样本。采用微生物琼脂平板扩散法,以大肠杆菌Kp 712作为测试菌,测定培氟沙星和环丙沙星的血清及支气管分泌物浓度。治疗后约72小时,98%的患者体内的致病微生物(金黄色葡萄球菌、流感嗜血杆菌、卡他莫拉菌)被清除。一般来说,两种抗生素口服时表现出相似的杀菌特性,而培氟沙星静脉给药相比口服给药方案显示出更快的抗菌作用。治疗后同一时间(4小时)记录到两种药物在支气管分泌物中的最大浓度,约为2.5微克/毫升。培氟沙星半衰期较长,单次口服800毫克后,治疗24小时后血浆浓度为1.5微克/毫升。环丙沙星半衰期较短,给药后12小时(500毫克/12小时/口服)达到约1微克/毫升的峰值。

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