Martin S J, Jung R, Garvin C G
The University of Toledo, College of Pharmacy, Ohio 43606, USA.
Drug Saf. 2001;24(3):199-222. doi: 10.2165/00002018-200124030-00004.
As a class, the quinolone antibacterials can no longer be assumed to be both effective and relatively free of significant adverse effects. Recent safety issues with newer generation fluoroquinolones, and concerns regarding drug-use associated bacterial resistance have made all drugs in this class subject to intense scrutiny and further study. Levofloxacin is a second generation fluoroquinolone with a post marketing history of well tolerated and successful use in a variety of clinical situations. Quinolones as a class cause a variety of adverse effects, including phototoxicity, seizures and other CNS disturbances, tendonitis and arthropathies, gastrointestinal effects, nephrotoxicity, prolonged QTc interval and torsade de pointes, hypo- or hyperglycaemia, and hypersensitivity reactions. Levofloxacin has been involved in only a few case reports of adverse events, which include QTc prolongation, seizures, glucose disturbances, and tendonitis. Levofloxacin has been shown to be effective at dosages of 250mg to 500mg once-daily in clinical trials in the management of acute maxillary sinusitis, acute bacterial exacerbations of chronic bronchitis, community-acquired pneumonia, skin and skin structure infections, and urinary tract infections. There are data suggesting that levofloxacin may promote fluoroquinolone resistance among the Streptococcus pneumoniae, and that clinical failures may result from this therapy. Other data suggest that fluoroquinolones with lower potency against Pseudomonas aeruginosa than ciprofloxacin, such as levofloxacin, may drive class-wide resistance to this pathogen. Levofloxacin is an effective drug in many clinical situations, but its cost is significantly higher than amoxicillin, erythromycin, or first and second generation cefalosporins. Because of the propensity to select for fluoroquinolone resistance in the pneumococcus and potentially other pathogens, levofloxacin should be an alternative agent rather than a drug-of-choice in routine community-acquired respiratory tract, urinary tract, and skin or skin structure infections. In areas with increasing pneumococcal beta-lactam resistance, levofloxacin may be a reasonable empiric therapy in community-acquired respiratory tract infections. Similarly, in patients with risk factors for infectious complications or poor outcome, levofloxacin may be an excellent empiric choice in severe community-acquired respiratory tract infections, urinary tract infections, complicated skin or skin structure infections, and nosocomial respiratory and urinary tract infections. Better clinical data are needed to identify the true place in therapy of the newer fluoroquinolones in common community-acquired and nosocomial infections. Until then, these agents, including levofloxacin, might best be reserved for complicated infections, infection recurrence, and infections caused by beta-lactam or macrolide-resistant pathogens.
作为一类药物,不能再认为喹诺酮类抗菌药既有效又相对没有明显的不良反应。新一代氟喹诺酮类药物最近出现的安全问题,以及对与药物使用相关的细菌耐药性的担忧,使得该类所有药物都受到了严格审查和进一步研究。左氧氟沙星是第二代氟喹诺酮类药物,上市后在各种临床情况下都有耐受性良好且使用成功的历史。喹诺酮类药物作为一个类别会引起多种不良反应,包括光毒性、癫痫发作和其他中枢神经系统紊乱、肌腱炎和关节病、胃肠道反应、肾毒性、QTc间期延长和尖端扭转型室速、低血糖或高血糖以及过敏反应。左氧氟沙星仅涉及少数不良事件的病例报告,其中包括QTc延长、癫痫发作、血糖紊乱和肌腱炎。在治疗急性上颌窦炎、慢性支气管炎急性细菌加重、社区获得性肺炎、皮肤及皮肤结构感染和尿路感染的临床试验中,已证明左氧氟沙星每日一次剂量为250mg至500mg时有效。有数据表明,左氧氟沙星可能会促使肺炎链球菌产生氟喹诺酮耐药性,并且这种治疗可能会导致临床治疗失败。其他数据表明,对铜绿假单胞菌的效力低于环丙沙星的氟喹诺酮类药物,如左氧氟沙星,可能会导致对该病原体产生全类别耐药性。左氧氟沙星在许多临床情况下是一种有效的药物,但其成本明显高于阿莫西林、红霉素或第一代和第二代头孢菌素。由于在肺炎球菌以及可能的其他病原体中容易产生氟喹诺酮耐药性,在常规社区获得性呼吸道、泌尿道以及皮肤或皮肤结构感染中,左氧氟沙星应作为替代药物而非首选药物。在肺炎球菌对β-内酰胺耐药性增加的地区,左氧氟沙星在社区获得性呼吸道感染中可能是一种合理的经验性治疗药物。同样,对于有感染并发症风险或预后不良的患者,在严重社区获得性呼吸道感染、泌尿道感染、复杂性皮肤或皮肤结构感染以及医院获得性呼吸道和泌尿道感染中,左氧氟沙星可能是一个很好的经验性选择。需要更好的临床数据来确定新型氟喹诺酮类药物在常见社区获得性和医院获得性感染治疗中的真正地位。在此之前,包括左氧氟沙星在内的这些药物最好保留用于复杂性感染、感染复发以及由β-内酰胺或大环内酯耐药病原体引起的感染。