Zhanel George G, Fontaine Sonya, Adam Heather, Schurek Kristen, Mayer Matt, Noreddin Ayman M, Gin Alfred S, Rubinstein Ethan, Hoban Daryl J
Department of Medical Microbiology, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, CanadaDepartment of Clinical Microbiology, Health Sciences Centre, Winnipeg, Manitoba, CanadaDepartment of Medicine, Health Sciences Centre, Winnipeg, Manitoba, Canada.
Treat Respir Med. 2006;5(6):437-65. doi: 10.2165/00151829-200605060-00009.
The new respiratory fluoroquinolones (gatifloxacin, gemifloxacin, levofloxacin, moxifloxacin, and on the horizon, garenoxacin) offer many improved qualities over older agents such as ciprofloxacin. These include retaining excellent activity against Gram-negative bacilli, with improved Gram-positive activity (including Streptococcus pneumoniae and Staphylococcus aureus). In addition, gatifloxacin, moxifloxacin and garenoxacin all demonstrate increased anaerobic activity (including activity against Bacteroides fragilis). The new fluoroquinolones possess greater bioavailability and longer serum half-lives compared with ciprofloxacin. The new fluoroquinolones allow for once-daily administration, which may improve patient adherence. The high bioavailability allows for rapid step down from intravenous administration to oral therapy, minimizing unnecessary hospitalization, which may decrease costs and improve quality of life of patients. Clinical trials involving the treatment of community-acquired respiratory infections (acute exacerbations of chronic bronchitis, acute sinusitis, and community-acquired pneumonia) demonstrate high bacterial eradication rates and clinical cure rates. In the treatment of community-acquired respiratory tract infections, the various new fluoroquinolones appear to be comparable to each other, but may be more effective than macrolide or cephalosporin-based regimens. However, additional data are required before it can be emphatically stated that the new fluoroquinolones as a class are responsible for better outcomes than comparators in community-acquired respiratory infections. Gemifloxacin (except for higher rates of hypersensitivity), levofloxacin, and moxifloxacin have relatively mild adverse effects that are more or less comparable to ciprofloxacin. In our opinion, gatifloxacin should not be used, due to glucose alterations which may be serious. Although all new fluoroquinolones react with metal ion-containing drugs (antacids), other drug interactions are relatively mild compared with ciprofloxacin. The new fluoroquinolones gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin have much to offer in terms of bacterial eradication, including activity against resistant respiratory pathogens such as penicillin-resistant, macrolide-resistant, and multidrug-resistant S. pneumoniae. However, ciprofloxacin-resistant organisms, including ciprofloxacin-resistant S. pneumoniae, are becoming more prevalent, thus prudent use must be exercised when prescribing these valuable agents.
新型呼吸喹诺酮类药物（加替沙星、吉米沙星、左氧氟沙星、莫西沙星，即将上市的加雷沙星）与环丙沙星等旧药相比有许多改进之处。这些改进包括对革兰氏阴性杆菌保持优异活性，同时增强了对革兰氏阳性菌的活性（包括肺炎链球菌和金黄色葡萄球菌）。此外，加替沙星、莫西沙星和加雷沙星均表现出增强的抗厌氧活性（包括对脆弱拟杆菌的活性）。与环丙沙星相比，新型喹诺酮类药物具有更高的生物利用度和更长的血清半衰期。新型喹诺酮类药物允许每日一次给药，这可能提高患者的依从性。高生物利用度使得能够从静脉给药迅速过渡到口服治疗，最大限度地减少不必要的住院，这可能降低成本并改善患者的生活质量。涉及社区获得性呼吸道感染（慢性支气管炎急性加重、急性鼻窦炎和社区获得性肺炎）治疗的临床试验显示细菌根除率和临床治愈率很高。在社区获得性呼吸道感染的治疗中，各种新型喹诺酮类药物似乎彼此相当，但可能比基于大环内酯类或头孢菌素的治疗方案更有效。然而，在能够明确指出新型喹诺酮类药物作为一个类别在社区获得性呼吸道感染中比对照药物能带来更好的治疗效果之前，还需要更多数据。吉米沙星（除过敏率较高外）、左氧氟沙星和莫西沙星的不良反应相对较轻，与环丙沙星或多或少相当。我们认为，由于可能出现严重的血糖改变，不应使用加替沙星。虽然所有新型喹诺酮类药物都与含金属离子的药物（抗酸剂）发生反应，但与环丙沙星相比，其他药物相互作用相对较轻。新型喹诺酮类药物加替沙星、吉米沙星、左氧氟沙星和莫西沙星在细菌根除方面有很大优势，包括对耐药呼吸道病原体如耐青霉素、耐大环内酯和多重耐药肺炎链球菌的活性。然而，耐环丙沙星的微生物，包括耐环丙沙星的肺炎链球菌，正变得越来越普遍，因此在开具这些有价值的药物时必须谨慎使用。
