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健康老年志愿者中单独使用及联合使用环丙沙星时血清杀菌活性和药代动力学的交叉评估。

Crossover assessment of serum bactericidal activity and pharmacokinetics of ciprofloxacin alone and in combination in healthy elderly volunteers.

作者信息

Weinstein M P, Deeter R G, Swanson K A, Gross J S

机构信息

Department of Medicine, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School, New Brunswick 08901.

出版信息

Antimicrob Agents Chemother. 1991 Nov;35(11):2352-8. doi: 10.1128/AAC.35.11.2352.

Abstract

To better define the pharmacokinetics and serum bactericidal activity (SBA) of ciprofloxacin and other antimicrobial agents in the elderly, six healthy (greater than 65 years) volunteers with normal renal function were given ciprofloxacin alone orally, ciprofloxacin plus rifampin orally, ciprofloxacin plus clindamycin orally, rifampin alone orally (three volunteers), and, for comparison of SBA against gram-positive cocci, vancomycin intravenously. Mean peak ciprofloxacin concentrations and other pharmacokinetic parameters were not altered significantly by coadministration of either rifampin or clindamycin. Ciprofloxacin had somewhat greater SBA against the oxacillin-susceptible and oxacillin-resistant Staphylococcus aureus strains tested than did vancomycin, but rifampin was by far the most active single agent tested. The SBA of rifampin against S. aureus was modestly antagonized during combination therapy with ciprofloxacin, but substantial SBA still was present. The ciprofloxacin SBA against S. aureus was completely antagonized by clindamycin if the strains were susceptible to the latter agent. Ciprofloxacin had modest SBA against group A streptococci and no SBA against the three pneumococcal strains tested. All of the regimens had poor to absent SBA against Enterococcus faecalis. By contrast, ciprofloxacin had excellent SBA against Escherchia coli and Klebsiella pneumoniae and moderate SBA against Pseudomonas aeruginosa. Combination therapy with rifampin or clindamycin in general enhanced the SBA against the nonenterococcal streptococci and had no effect on the SBA against the gram-negative bacilli.

摘要

为了更好地明确环丙沙星及其他抗菌药物在老年人中的药代动力学和血清杀菌活性(SBA),对6名肾功能正常的健康(年龄大于65岁)志愿者进行了研究,分别给予单独口服环丙沙星、口服环丙沙星加利福平、口服环丙沙星加克林霉素、单独口服利福平(3名志愿者),并且,为了比较针对革兰氏阳性球菌的SBA,还静脉给予万古霉素。利福平或克林霉素与环丙沙星合用时,环丙沙星的平均峰浓度及其他药代动力学参数未发生显著改变。与万古霉素相比,环丙沙星对所检测的对苯唑西林敏感及耐药的金黄色葡萄球菌菌株具有略高的SBA,但利福平是所检测的单一药物中活性最强的。在与环丙沙星联合治疗期间,利福平对金黄色葡萄球菌的SBA受到一定程度的拮抗,但仍存在较高的SBA。如果菌株对克林霉素敏感,环丙沙星对金黄色葡萄球菌的SBA会被克林霉素完全拮抗。环丙沙星对A组链球菌的SBA较弱,对所检测的3种肺炎球菌菌株无SBA。所有治疗方案对粪肠球菌的SBA均较差或不存在。相比之下,环丙沙星对大肠杆菌和肺炎克雷伯菌具有良好的SBA,对铜绿假单胞菌具有中等SBA。利福平或克林霉素联合治疗总体上增强了对非肠球菌性链球菌的SBA,对革兰氏阴性杆菌的SBA无影响。

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本文引用的文献

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Pharmacokinetic studies of rifampicin in the elderly.
Ther Drug Monit. 1983;5(1):61-5. doi: 10.1097/00007691-198303000-00004.
2
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