Anderson Vanessa R, Perry Caroline M
Wolters Kluwer Health Adis, Auckland, New Zealand.
Drugs. 2008;68(4):535-65. doi: 10.2165/00003495-200868040-00011.
Levofloxacin (Levaquin) is a fluoroquinolone antibacterial that is the L-isomer of ofloxacin. A high-dose (750 mg) short-course (5 days) of once-daily levofloxacin is approved for use in the US in the treatment of community-acquired pneumonia (CAP), acute bacterial sinusitis (ABS), complicated urinary tract infections (UTI) and acute pyelonephritis (AP). The broad spectrum antibacterial profile of levofloxacin means that monotherapy is often a possibility in patients with CAP at times when other agents may require combination therapy, although levofloxacin can be used in combination therapy when necessary. The high-dose, short-course levofloxacin regimen maximizes its concentration-dependent bactericidal activity and may reduce the potential for resistance to emerge. In addition, this regimen lends itself to better compliance because of the shorter duration of treatment and the convenient once-daily administration schedule. Oral levofloxacin is rapidly absorbed and is bioequivalent to the intravenous formulation; importantly, patients can transition between the formulations, which results in more options in regards to the treatment regimen and the potential for patients with varying degrees of illness to be treated. Levofloxacin has good tissue penetration and an adequate concentration can be maintained in the urinary tract to treat uropathogens. Levofloxacin is generally well tolerated and has good efficacy in the treatment of patients with CAP, ABS, complicated UTI and AP. The efficacy and tolerability of levofloxacin 500 mg once daily for 10 days in patients with CAP, ABS and UTIs is well established, and the high-dose, short-course levofloxacin regimen has been shown to be noninferior to the 10-day regimen in CAP and ABS, and to have a similar tolerability profile. Similarly, the high-dose, short-course levofloxacin regimen is noninferior to ciprofloxacin in patients with complicated UTI or AP. Thus, levofloxacin is a valuable antimicrobial agent that has activity against a wide range of bacterial pathogens; however, its use should be considered carefully so that the potential for resistance selection can be minimized and its usefulness in severe infections and against a range of penicillin- and macrolide-resistant pathogens can be maintained.
左氧氟沙星（可乐必妥）是一种氟喹诺酮类抗菌药物，是氧氟沙星的L-异构体。在美国，高剂量（750毫克）短疗程（5天）每日一次的左氧氟沙星被批准用于治疗社区获得性肺炎（CAP）、急性细菌性鼻窦炎（ABS）、复杂性尿路感染（UTI）和急性肾盂肾炎（AP）。左氧氟沙星的广谱抗菌谱意味着在其他药物可能需要联合治疗时，CAP患者有时可以采用单一疗法，不过必要时左氧氟沙星也可用于联合治疗。高剂量、短疗程的左氧氟沙星方案可最大化其浓度依赖性杀菌活性，并可能降低耐药性出现的可能性。此外，由于治疗疗程较短且给药方案方便，每日一次，该方案更易于患者依从。口服左氧氟沙星吸收迅速，与静脉制剂具有生物等效性；重要的是，患者可以在不同剂型之间转换，这为治疗方案提供了更多选择，也为不同病情程度的患者提供了治疗可能性。左氧氟沙星具有良好的组织穿透力，可在尿路中维持足够浓度以治疗尿路病原体。左氧氟沙星一般耐受性良好，在治疗CAP、ABS、复杂性UTI和AP患者方面疗效显著。每日一次服用500毫克左氧氟沙星，连续服用10天，治疗CAP、ABS和UTI患者的疗效已得到充分证实，高剂量、短疗程的左氧氟沙星方案在CAP和ABS治疗中已被证明不劣于10天疗程，且耐受性相似。同样，在复杂性UTI或AP患者中，高剂量、短疗程的左氧氟沙星方案不劣于环丙沙星。因此，左氧氟沙星是一种有价值的抗菌药物，对多种细菌病原体具有活性；然而，应谨慎使用，以尽量减少耐药性选择的可能性，并维持其在严重感染以及针对一系列耐青霉素和耐大环内酯类病原体方面的有效性。
