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左氧氟沙星:美国治疗细菌感染用药综述

Levofloxacin: a review of its use in the treatment of bacterial infections in the United States.

作者信息

Croom Katherine F, Goa Karen L

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2003;63(24):2769-802. doi: 10.2165/00003495-200363240-00008.

Abstract

UNLABELLED

Levofloxacin (Levaquin) is a fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and Gram-negative bacteria and atypical respiratory pathogens. It is active against both penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae. The prevalence of S. pneumoniae resistance to levofloxacin is <1% overall in the US.A number of randomised comparative trials in the US have demonstrated the efficacy of levofloxacin in the treatment of infections of the respiratory tract, genitourinary tract, skin and skin structures. Sequential intravenous to oral levofloxacin 750mg once daily for 7-14 days was as effective in the treatment of nosocomial pneumonia as intravenous imipenem/cilastatin 500-1000mg every 6-8 hours followed by oral ciprofloxacin 750mg twice daily in one study. In patients with mild to severe community-acquired pneumonia (CAP), intravenous and/or oral levofloxacin 500mg once daily for 7-14 days achieved clinical and bacteriological response rates similar to those with comparator agents, including amoxicillin/clavulanic acid, clarithromycin, azithromycin, ceftriaxone and/or cefuroxime axetil and gatifloxacin. A recent study indicates that intravenous or oral levofloxacin 750mg once daily for 5 days is as effective as 500mg once daily for 10 days, in the treatment of mild to severe CAP. Exacerbations of chronic bronchitis and acute maxillary sinusitis respond well to treatment with oral levofloxacin 500mg once daily for 7 and 10-14 days, respectively. Oral levofloxacin was as effective as ofloxacin in uncomplicated urinary tract infections and ciprofloxacin or lomefloxacin in complicated urinary tract infections. In men with chronic bacterial prostatitis treated for 28 days, oral levofloxacin 500mg once daily achieved similar clinical and bacteriological response rates to oral ciprofloxacin 500mg twice daily. Uncomplicated skin infections responded well to oral levofloxacin 500mg once daily for 7-10 days, while in complicated skin infections intravenous and/or oral levofloxacin 750mg for 7-14 days was at least as effective as intravenous ticarcillin/clavulanic acid (+/- switch to oral amoxicillin/clavulanic acid) administered for the same duration. Levofloxacin is generally well tolerated, with the most frequently reported adverse events being nausea and diarrhoea; in comparison with some other quinolones it has a low photosensitising potential and clinically significant cardiac and hepatic adverse events are rare.

CONCLUSION

Levofloxacin is a broad-spectrum antibacterial agent with activity against a range of Gram-positive and Gram-negative bacteria and atypical organisms. It provides clinical and bacteriological efficacy in a range of infections, including those caused by both penicillin-susceptible and -resistant strains of S. pneumoniae. Levofloxacin is well tolerated, and is associated with few of the phototoxic, cardiac or hepatic adverse events seen with some other quinolones. It also has a pharmacokinetic profile that is compatible with once-daily administration and allows for sequential intravenous to oral therapy. The recent approvals in the US for use in the treatment of nosocomial pneumonia and chronic bacterial prostatitis, and the introduction of a short-course, high-dose regimen for use in CAP, further extend the role of levofloxacin in treating bacterial infections.

摘要

未标注

左氧氟沙星(可乐必妥)是一种氟喹诺酮类抗菌药物,对革兰氏阳性菌、革兰氏阴性菌及非典型呼吸道病原体具有广泛的抗菌活性。它对青霉素敏感和耐药的肺炎链球菌均有活性。在美国,肺炎链球菌对左氧氟沙星的总体耐药率<1%。美国的多项随机对照试验已证实左氧氟沙星在治疗呼吸道、泌尿生殖道、皮肤及皮肤结构感染方面的疗效。在一项研究中,每日一次静脉滴注750mg左氧氟沙星序贯口服,疗程7 - 14天,治疗医院获得性肺炎的疗效与每6 - 8小时静脉滴注500 - 1000mg亚胺培南/西司他丁,随后每日两次口服750mg环丙沙星相当。对于轻至重度社区获得性肺炎(CAP)患者,每日一次静脉滴注和/或口服500mg左氧氟沙星,疗程7 - 14天,其临床和细菌学反应率与对照药物(包括阿莫西林/克拉维酸、克拉霉素、阿奇霉素、头孢曲松和/或头孢呋辛酯及加替沙星)相似。最近一项研究表明,每日一次静脉滴注或口服750mg左氧氟沙星,疗程5天,在治疗轻至重度CAP方面与每日一次口服500mg、疗程10天的疗效相当。慢性支气管炎急性加重和急性上颌窦炎分别口服500mg左氧氟沙星,疗程7天和10 - 14天,治疗效果良好。在单纯性尿路感染中,口服左氧氟沙星与氧氟沙星疗效相当,在复杂性尿路感染中与环丙沙星或洛美沙星疗效相当。在接受28天治疗的慢性细菌性前列腺炎男性患者中,每日一次口服500mg左氧氟沙星与每日两次口服500mg环丙沙星的临床和细菌学反应率相似。单纯性皮肤感染口服500mg左氧氟沙星,疗程7 - 10天,疗效良好;而在复杂性皮肤感染中,静脉滴注和/或口服750mg左氧氟沙星,疗程7 - 14天,至少与静脉滴注替卡西林/克拉维酸(±换用口服阿莫西林/克拉维酸)、疗程相同的疗效相当。左氧氟沙星一般耐受性良好,最常报告的不良事件为恶心和腹泻;与其他一些喹诺酮类药物相比,其光敏性较低,临床上显著的心脏和肝脏不良事件罕见。

结论

左氧氟沙星是一种广谱抗菌药物,对多种革兰氏阳性菌、革兰氏阴性菌及非典型病原体均有活性。它在一系列感染中均具有临床和细菌学疗效,包括由青霉素敏感和耐药肺炎链球菌菌株引起的感染。左氧氟沙星耐受性良好,与其他一些喹诺酮类药物相比,光毒性、心脏或肝脏不良事件较少。它还具有与每日一次给药相适应的药代动力学特征,并允许序贯静脉滴注至口服治疗。美国最近批准其用于治疗医院获得性肺炎和慢性细菌性前列腺炎,并引入了用于CAP的短疗程、高剂量方案,进一步扩大了左氧氟沙星在治疗细菌感染方面的作用。

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