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氟罗沙星对引起复杂性尿路感染的分离菌株的体外活性及其在精液、前列腺液和前列腺腺瘤组织中的浓度

In-vitro activity of fleroxacin against isolates causing complicated urinary tract infections and concentrations in seminal and prostatic fluid and in prostatic adenoma tissue.

作者信息

Naber K G, Sörgel F, Kees F, Schumacher H, Metz R, Grobecker H

机构信息

Urologic Clinic, Elisabeth Krankenhaus, Straubing, Federal Republic of Germany.

出版信息

J Antimicrob Chemother. 1988 Oct;22 Suppl D:199-207. doi: 10.1093/jac/22.supplement_d.199.

Abstract

Fleroxacin is a new fluoroquinolone with a broad antibacterial spectrum and a serum half-life of about 8-12 h. Eighty percent of 400 isolates from complicated or hospital-acquired urinary tract infections were inhibited by a concentration of 1 mg/l and 95% by 4 mg/l. As with other quinolones, fleroxacin is less active in acid urine (pH 5.4) than in Mueller-Hinton broth (pH 7.4). In 12 healthy volunteers the concentrations of fleroxacin were measured in plasma and seminal and prostatic fluid 2, 4 and 12 h after an oral dose of 400 mg. The mean plasma concentrations of three or four volunteers at each time were 4.2, 3.6 and 1.2 mg/l, respectively. The corresponding prostatic fluid/plasma ratios were 0.30, 0.27 and 1.96, respectively. By concomittant administration of ioxitalamic acid it could be demonstrated that in samples obtained 12 h after administration urinary contamination must be considered. Fleroxacin is concentrated in seminal fluid by a median ratio of 1.7. In 13 elderly patients the prostatic fluid and prostatic adenoma tissue concentrations were determined one to four hours following oral administration of 400 mg. The concentrations in prostatic fluid were similar to those of volunteers. The tissue concentrations exceeded plasma concentrations by only about 10% (median). Fleroxacin is very active against isolates causing complicated UTI. Concentrations in seminal and prostatic fluid and prostatic adenoma tissue are sufficiently high to treat bacterial prostatitis or vesiculitis caused by susceptible bacterial strains.

摘要

氟罗沙星是一种新型氟喹诺酮类药物,抗菌谱广,血清半衰期约为8 - 12小时。来自复杂性或医院获得性尿路感染的400株分离菌中,80%被1 mg/l的浓度所抑制,95%被4 mg/l的浓度所抑制。与其他喹诺酮类药物一样,氟罗沙星在酸性尿液(pH 5.4)中的活性低于在穆勒-欣顿肉汤(pH 7.4)中的活性。在12名健康志愿者口服400 mg剂量后2、4和12小时,测定了血浆、精液和前列腺液中氟罗沙星的浓度。每次三或四名志愿者的平均血浆浓度分别为4.2、3.6和1.2 mg/l。相应的前列腺液/血浆比值分别为0.30、0.27和1.96。通过同时给予碘他拉酸可以证明,在给药12小时后采集的样本中必须考虑尿液污染。氟罗沙星在精液中的浓缩中位比值为1.7。在13名老年患者中,口服400 mg后1至4小时测定了前列腺液和前列腺腺瘤组织中的浓度。前列腺液中的浓度与志愿者的相似。组织浓度仅比血浆浓度高约10%(中位数)。氟罗沙星对引起复杂性尿路感染的分离菌非常有效。精液、前列腺液和前列腺腺瘤组织中的浓度足够高,可治疗由易感菌株引起的细菌性前列腺炎或精囊炎。

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