Zhanel G G, Walkty A, Vercaigne L, Karlowsky J A, Embil J, Gin A S, Hoban D J
Departments of Clinical Microbiology.
Can J Infect Dis. 1999 May;10(3):207-38. doi: 10.1155/1999/378394.
This paper reviews the literature available on the new fluoroquinolones - clinafloxacin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, sparfloxacin and trovafloxacin - to compare these agents with each other and contrast them with ciprofloxacin, an older fluoroquinolone.
Published papers used were obtained by searching MEDLINE for articles published between 1994 and 1998, inclusive. References of published papers were also obtained and reviewed. Abstracts from scientific proceedings were reviewed.
Due to the limited data available on several of the agents, criteria for study inclusion in the in vitro, pharmacokinetics and in vivo sections were not restrictive.
The new fluoroquinolones offer excellent Gram-negative bacillary activity and improved Gram-positive activity (eg, against Streptococcus pneumoniae and Staphylococcus aureus) over ciprofloxacin. Clinafloxacin, gatifloxacin, moxifloxacin, sparfloxacin and trovafloxacin display improved activity against anaerobes (eg, Bacteriodes fragilis). All of the new fluoroquinolones have a longer serum half-life than ciprofloxacin (allowing for once daily dosing), and several are eliminated predominantly by nonrenal means. No clinical trials are available comparing the new fluoroquinolones with each other. Clinical trials comparing the new fluoroquinolones with standard therapy have demonstrated good efficacy in a variety of infections. Their adverse effect profile is similar to that of ciprofloxacin. Clinafloxacin and sparfloxacin cause a high incidence of phototoxicity (1.5% to 14% and 2% to 11.7%, respectively), grepafloxacin causes a high incidence of taste perversion (9% to 17%) and trovafloxacin causes a high incidence of dizziness (11%). They all interact with metal ion-containing drugs (eg, antacids), and clinafloxacin and grepafloxacin interact with theophylline. The new fluoroquinolones are expensive; however, their use may result in savings in situations where, because of their potent and broad spectrum of activity, they can be used orally in place of intravenous antibiotics.
The new fluoroquinolones offer advantages over ciprofloxacin in terms of improved in vitro activity and pharmacokinetics. Whether these advantages translate into improved clinical outcomes is presently unknown. The new fluoroquinolones have the potential to emerge as important therapeutic agents in the treatment of respiratory tract and genitourinary tract infections.
本文回顾了有关新型氟喹诺酮类药物——克林沙星、加替沙星、格帕沙星、左氧氟沙星、莫西沙星、司帕沙星和曲伐沙星——的现有文献，以相互比较这些药物，并与较老的氟喹诺酮类药物环丙沙星进行对比。
通过检索MEDLINE获取1994年至1998年（含）发表的文章作为已发表论文。还获取并查阅了已发表论文的参考文献。对科学会议的摘要进行了审查。
由于几种药物的可用数据有限，体外、药代动力学和体内部分纳入研究的标准并不严格。
新型氟喹诺酮类药物具有出色的革兰氏阴性杆菌活性，与环丙沙星相比，革兰氏阳性菌活性有所提高（例如，对肺炎链球菌和金黄色葡萄球菌）。克林沙星、加替沙星、莫西沙星、司帕沙星和曲伐沙星对厌氧菌（例如脆弱拟杆菌）的活性有所提高。所有新型氟喹诺酮类药物的血清半衰期均比环丙沙星长（允许每日给药一次），并且几种药物主要通过非肾脏途径消除。尚无比较新型氟喹诺酮类药物相互之间的临床试验。将新型氟喹诺酮类药物与标准疗法进行比较的临床试验已证明在多种感染中具有良好疗效。它们的不良反应谱与环丙沙星相似。克林沙星和司帕沙星引起的光毒性发生率较高（分别为1.5%至14%和2%至11.7%），格帕沙星引起味觉异常的发生率较高（9%至17%），曲伐沙星引起头晕的发生率较高（11%）。它们均与含金属离子的药物（例如抗酸剂）相互作用，并且克林沙星和格帕沙星与茶碱相互作用。新型氟喹诺酮类药物价格昂贵；然而，由于其强效和广谱活性，在可以口服使用以替代静脉用抗生素的情况下，其使用可能会节省费用。
新型氟喹诺酮类药物在体外活性和药代动力学方面比环丙沙星具有优势。这些优势是否能转化为改善的临床结果目前尚不清楚。新型氟喹诺酮类药物有潜力成为治疗呼吸道和泌尿道感染的重要治疗药物。
