新型氟喹诺酮类药物的研究进展:重点关注其在呼吸道感染中的应用。

George G Zhanel, Sonya Fontaine, Heather Adam, Kristen Schurek, Matt Mayer, Ayman M Noreddin, Alfred S Gin, Ethan Rubinstein, Daryl J Hoban
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引用次数: 48

摘要

新的呼吸用氟喹诺酮类药物(加替沙星、吉氟沙星、左氧氟沙星、莫西沙星,以及即将推出的加诺沙星)比环丙沙星等老药有许多改进。这些包括对革兰氏阴性杆菌保持良好的活性,并提高革兰氏阳性活性(包括肺炎链球菌和金黄色葡萄球菌)。此外,加替沙星、莫西沙星和加诺沙星均表现出增加的厌氧活性(包括对脆弱拟杆菌的活性)。与环丙沙星相比,新型氟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。新的氟喹诺酮类药物允许每天一次给药,这可能会提高患者的依从性。高生物利用度允许快速从静脉给药到口服治疗,最大限度地减少不必要的住院治疗,这可能会降低成本并提高患者的生活质量。涉及治疗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)的临床试验表明,细菌根除率和临床治愈率很高。在治疗社区获得性呼吸道感染方面,各种新型氟喹诺酮类药物似乎彼此具有可比性,但可能比大环内酯类药物或头孢菌素类药物更有效。然而,在强调新型氟喹诺酮类药物在社区获得性呼吸道感染方面的疗效优于比较药物之前,还需要更多的数据。吉氟沙星(除了高过敏率)、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。我们认为不应该使用加替沙星,因为葡萄糖改变可能很严重。虽然所有新的氟喹诺酮类药物都与含金属离子的药物(抗酸药)发生反应,但与环丙沙星相比,其他药物的相互作用相对较轻。新的氟喹诺酮类药物加替沙星、吉氟沙星、左氧氟沙星和莫西沙星在根除细菌方面有很大作用,包括对耐药呼吸道病原体的活性,如耐青霉素、耐大环内酯和耐多药肺炎链球菌。然而,耐环丙沙星生物,包括耐环丙沙星肺炎链球菌,正变得越来越普遍,因此在开处方时必须谨慎使用这些有价值的药物。
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A Review of New Fluoroquinolones : Focus on their Use in Respiratory Tract Infections.

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.

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