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单次及多次口服给药后洛美沙星在支气管分泌物中的渗透情况。

Penetration of lomefloxacin into bronchial secretions following single and multiple oral administration.

作者信息

Bergogne-Bérézin E, Muller-Serieys C, Kafé H

机构信息

Department of Microbiology, Hôpital Bichat, Paris, France.

出版信息

Am J Med. 1992 Apr 6;92(4A):8S-11S. doi: 10.1016/0002-9343(92)90299-q.

Abstract

The bronchial penetration of lomefloxacin, a new difluorinated quinolone, was evaluated in 36 patients who underwent bronchoscopies for diagnostic purposes. Patients were randomized into two groups, with 18 patients (Group I) receiving a single oral dose of 400 mg lomefloxacin and 18 patients (Group II) receiving 400 mg twice daily. Samples of serum and bronchial secretions were collected simultaneously in both groups at 1, 2, or 4 hours after lomefloxacin administration. The results of this study showed that bronchial penetration of lomefloxacin was rapid and yielded high concentrations; the mean bronchial levels of the drug reached 2.78 +/- 3.64 micrograms/mL in Group I 1 hour after the dose, and 2.84 +/- 1.73 micrograms/mL in Group II at the fourth hour. The ratio between bronchial and simultaneous serum concentrations was 89% at the first and second hours after the dose for Group I, and it was 77% 4 hours after oral administration in Group II. In comparing these results to previous reports of lomefloxacin penetration into bronchial mucosa or of concentrations of other new fluoroquinolones into bronchial secretions, it is to be noted that the local concentrations of the newer quinolones are of very similar values, ranging from 2.7 micrograms/mL (ofloxacin) to 4.46 micrograms/mL (pefloxacin). This study confirms that lomefloxacin achieves high tissue concentrations in the respiratory tree; this characteristic, together with lomefloxacin's antibacterial spectrum, indicates promise in the treatment of many respiratory infections.

摘要

对36例因诊断目的接受支气管镜检查的患者,评估了新型二氟喹诺酮洛美沙星的支气管穿透性。患者被随机分为两组,18例患者(第一组)口服单剂量400mg洛美沙星,18例患者(第二组)每日两次服用400mg。在洛美沙星给药后1、2或4小时,两组同时采集血清和支气管分泌物样本。本研究结果表明,洛美沙星的支气管穿透迅速且产生高浓度;给药后1小时,第一组药物的平均支气管水平达到2.78±3.64μg/mL,第四小时第二组为2.84±1.73μg/mL。给药后第一小时和第二小时,第一组支气管与同时期血清浓度之比为89%,第二组口服给药4小时后为77%。将这些结果与先前关于洛美沙星穿透支气管黏膜或其他新型氟喹诺酮在支气管分泌物中浓度的报告进行比较时,应注意到新型喹诺酮的局部浓度值非常相似,范围从2.7μg/mL(氧氟沙星)到4.46μg/mL(培氟沙星)。本研究证实洛美沙星在呼吸道树中可达到高组织浓度;这一特性与洛美沙星的抗菌谱一起,表明其在治疗许多呼吸道感染方面具有前景。

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