Langtry H D, Lamb H M
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Sep;56(3):487-515. doi: 10.2165/00003495-199856030-00013.
Levofloxacin, the optically pure levorotatory isomer of ofloxacin, is a fluoroquinolone antibacterial agent. Like other fluoroquinolones, it acts on bacterial topoisomerase and has activity against a broad range of Gram-positive and Gram-negative organisms. Levofloxacin also appears to have improved activity against Streptococcus pneumoniae compared with ciprofloxacin or ofloxacin. Levofloxacin distributes well and achieves high levels in excess of plasma concentrations in many tissues (e.g., lung, skin, prostate). High oral bioavailability allows switching from intravenous to oral therapy without dosage adjustment. In patients with mild to severe community-acquired pneumonia receiving treatment for 7 to 14 days, oral levofloxacin was similar in efficacy to amoxicillin/clavulanic acid, and intravenous and/or oral levofloxacin was superior to intravenous ceftriaxone and/or oral cefuroxime axetil. With levofloxacin use, clinical success (clinical cure or improvement) rates were 87 to 96% and bacteriological eradication rates were 87 to 100%. In the 5- to 10-day treatment of acute exacerbations of chronic bronchitis, oral levofloxacin was similar in efficacy to oral cefuroxime axetil or cefaclor. Levofloxacin resulted in clinical success in 78 to 94.6% of patients and bacteriological eradication in 77 to 97%. Oral levofloxacin was also similar in efficacy to amoxicillin/clavulanic acid or oral clarithromycin in patients with acute maxillary sinusitis treated for 7 to 14 days. Equivalence between 7- to 10-day therapy with oral levofloxacin and ciprofloxacin was seen in patients with uncomplicated skin and soft tissue infections. Clinical success was seen in 97.8 and 96.1% of levofloxacin recipients and bacteriological eradication in 97.5 and 93.2%. Complicated urinary tract infections, including pyelonephritis, responded similarly well to oral levofloxacin or ciprofloxacin for 10 days or lomefloxacin for 14 days. Clinical success and bacteriological eradication rates with levofloxacin occurred in 92 to 93.3% and 93.6 to 94.7% of patients.
Levofloxacin can be administered in a once-daily regimen as an alternative to other fluoroquinolones in the treatment of infections of the urinary tract, skin and soft tissues. Its more interesting use is as an alternative to established treatments of respiratory tract infections. S. pneumoniae appears to be more susceptible to levofloxacin than to ciprofloxacin or ofloxacin. Other newer fluoroquinolone agents that also have enhanced in vitro antipneumococcal activity may not share the well established tolerability profile of levofloxacin, which also appears to improve on that of some older fluoroquinolones.
左氧氟沙星是氧氟沙星的光学纯左旋异构体，是一种氟喹诺酮类抗菌剂。与其他氟喹诺酮类药物一样，它作用于细菌拓扑异构酶，对多种革兰氏阳性和革兰氏阴性菌具有活性。与环丙沙星或氧氟沙星相比，左氧氟沙星对肺炎链球菌的活性似乎有所提高。左氧氟沙星分布良好，在许多组织（如肺、皮肤、前列腺）中可达到超过血浆浓度的高水平。高口服生物利用度允许从静脉治疗转换为口服治疗而无需调整剂量。在接受7至14天治疗的轻至重度社区获得性肺炎患者中，口服左氧氟沙星的疗效与阿莫西林/克拉维酸相似，静脉和/或口服左氧氟沙星优于静脉注射头孢曲松和/或口服头孢呋辛酯。使用左氧氟沙星时，临床成功率（临床治愈或改善）为87%至96%，细菌清除率为87%至100%。在慢性支气管炎急性加重期的5至10天治疗中，口服左氧氟沙星的疗效与口服头孢呋辛酯或头孢克洛相似。左氧氟沙星使78%至94.6%的患者获得临床成功，细菌清除率为77%至97%。在接受7至14天治疗的急性上颌窦炎患者中，口服左氧氟沙星的疗效也与阿莫西林/克拉维酸或口服克拉霉素相似。在无并发症的皮肤和软组织感染患者中，口服左氧氟沙星与环丙沙星进行7至10天治疗具有等效性。左氧氟沙星治疗组的临床成功率分别为97.8%和96.1%，细菌清除率分别为97.5%和93.2%。包括肾盂肾炎在内的复杂性尿路感染，口服左氧氟沙星10天或洛美沙星14天的反应相似。左氧氟沙星治疗患者的临床成功率和细菌清除率分别为92%至93.3%和93.6%至94.7%。
左氧氟沙星可每日一次给药，作为治疗泌尿道、皮肤和软组织感染的其他氟喹诺酮类药物的替代品。其更有趣的用途是作为呼吸道感染既定治疗方法的替代品。肺炎链球菌似乎对左氧氟沙星比对环丙沙星或氧氟沙星更敏感。其他在体外也具有增强的抗肺炎球菌活性的新型氟喹诺酮类药物可能不具有左氧氟沙星已确立的良好耐受性，而左氧氟沙星的耐受性似乎也优于一些 older fluoroquinolones。（注：这里“older fluoroquinolones”直译为“ older fluoroquinolones”，可能是文档有误，推测应为“一些老一代氟喹诺酮类药物” ）
