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普卢利沙星的药理学特性

Pharmacologic characteristics of prulifloxacin.

作者信息

Matera Maria Gabriella

机构信息

Unit of Pharmacology Leonardo Donatelli, Department of Experimental Medicine, School of Medicine, Second University, Via del Parco Margherita 24, 80121 Naples, Italy.

出版信息

Pulm Pharmacol Ther. 2006;19 Suppl 1:20-9. doi: 10.1016/j.pupt.2005.09.009. Epub 2005 Dec 19.

Abstract

Prulifloxacin, the prodrug of ulifloxacin, is a broad-spectrum oral fluoroquinolone antibacterial agent. After absorption, prulifloxacin is metabolized by esterases to ulifloxacin. The drug has a long elimination half-life, allowing once-daily administration. In vitro, ulifloxacin is generally more active than other fluoroquinolones against a variety of clinical isolates of Gram-negative bacteria, including community and nosocomial isolates of Escherichia coli, Klebsiella spp., Proteus, Providencia and Morganella spp., Moraxella catarrhalis, Haemophilus spp., and Pseudomonas aeruginosa. Gram-positive organisms, including methicillin- or oxacillin-susceptible Staphylococcus aureus, Enterococcus spp. and Streptococcus pneumoniae, are susceptible to ulifloxacin. In well-designed clinical trials, prulifloxacin showed good clinical and bacteriological efficacy (similar to that of ciprofloxacin) and was generally well tolerated, demonstrating a similar tolerability profile to that of ciprofloxacin. In conclusion, the in vitro inhibitory and bactericidal activities exhibited by ulifloxacin and the favorable characteristics shown by its prodrug (prulifloxacin) in clinical trials, particularly indicate this drug for the treatment of lung and urinary infections.

摘要

普卢利沙星是乌利沙星的前体药物,是一种广谱口服氟喹诺酮类抗菌剂。吸收后,普卢利沙星被酯酶代谢为乌利沙星。该药物消除半衰期长,允许每日给药一次。在体外,乌利沙星对多种革兰氏阴性菌临床分离株(包括社区和医院获得性大肠杆菌、克雷伯菌属、变形杆菌、普罗威登斯菌属和摩根菌属、卡他莫拉菌、嗜血杆菌属和铜绿假单胞菌)的活性通常比其他氟喹诺酮类药物更强。革兰氏阳性菌,包括对甲氧西林或苯唑西林敏感的金黄色葡萄球菌、肠球菌属和肺炎链球菌,对乌利沙星敏感。在精心设计的临床试验中,普卢利沙星显示出良好的临床和细菌学疗效(与环丙沙星相似),并且总体耐受性良好,显示出与环丙沙星相似的耐受性特征。总之,乌利沙星表现出的体外抑制和杀菌活性以及其前体药物(普卢利沙星)在临床试验中显示出的有利特性,特别表明该药物可用于治疗肺部和泌尿系统感染。

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