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加替沙星:其在细菌感染治疗中的应用综述

Gatifloxacin: a review of its use in the management of bacterial infections.

作者信息

Perry Caroline M, Ormrod Douglas, Hurst Miriam, Onrust Susan V

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2002;62(1):169-207. doi: 10.2165/00003495-200262010-00007.

Abstract

UNLABELLED

Gatifloxacin is an 8-methoxy fluoroquinolone antibacterial agent. The drug has a broader spectrum of antibacterial activity than the older fluoroquinolones (e.g. ciprofloxacin) and shows good activity against many Gram-positive and Gram-negative pathogens, atypical organisms and some anaerobes. Notably, gatifloxacin is highly active against both penicillin-susceptible and -resistant strains of Streptococcus pneumoniae, a common causative pathogen in community-acquired pneumonia (CAP), acute sinusitis and acute bacterial exacerbations of bronchitis. Gatifloxacin is absorbed well from the gastrointestinal tract (oral bioavailability is almost 100%). Therefore, patients can be switched from intravenous to oral therapy without an adjustment in dosage. High concentrations of gatifloxacin are achieved in plasma and target tissues/fluids. Gatifloxacin has a long plasma elimination half-life, thus allowing once-daily administration. Few clinically significant interactions between gatifloxacin and other drugs have been reported. In patients with CAP, clinical response rates in recipients of intravenous/oral gatifloxacin 400 mg/day ranged from 86.8 to 98.0% and rates of bacterial eradication ranged from 83.1 to 100% (up to 28 days post-treatment). Gatifloxacin showed efficacy similar to that of amoxicillin/clavulanic acid, ceftriaxone (with or without erythromycin) with or without stepdown to clarithromycin, levofloxacin or clarithromycin. Gatifloxacin was as effective as clarithromycin or amoxicillin/clavulanic acid, and was significantly more effective (in terms of clinical response; p < 0.035) than 7 to 10 days' treatment with cefuroxime axetil in the treatment of acute exacerbations of chronic bronchitis. In acute sinusitis, gatifloxacin showed clinical efficacy similar to that of clarithromycin, trovafloxacin or amoxicillin/clavulanic acid. Genitourinary infections were also successfully treated with gatifloxacin. Gatifloxacin is generally well tolerated. Its tolerability profile was broadly similar to those of comparator agents in comparative trials. The most common adverse events are gastrointestinal symptoms (oral formulation) and injection site reactions.

CONCLUSIONS

Gatifloxacin has an extended spectrum of antibacterial activity and provides better coverage of Gram-positive organisms (e.g. S. pneumoniae) than some older fluoroquinolones. The drug has favourable pharmacokinetic properties, is administered once daily and is at least as well tolerated as other fluoroquinolones. Gatifloxacin is a useful addition to the fluoroquinolones currently available for use in the clinical setting and has an important role in the management of adult patients with various bacterial infections. As with other fluoroquinolones, careful control of gatifloxacin usage in the community is important in order to prevent the emergence of bacterial resistance and thus preserve the clinical value of this agent.

摘要

未标注

加替沙星是一种8-甲氧基氟喹诺酮类抗菌药物。与较老的氟喹诺酮类药物(如环丙沙星)相比,该药具有更广泛的抗菌活性,对许多革兰氏阳性和革兰氏阴性病原体、非典型微生物及一些厌氧菌均显示出良好活性。值得注意的是,加替沙星对社区获得性肺炎(CAP)、急性鼻窦炎及急性细菌性支气管炎加重期的常见致病病原体——肺炎链球菌的青霉素敏感和耐药菌株均具有高度活性。加替沙星从胃肠道吸收良好(口服生物利用度几乎为100%)。因此,患者可从静脉给药转换为口服治疗,而无需调整剂量。加替沙星在血浆及靶组织/体液中可达到高浓度。加替沙星的血浆消除半衰期长,因此允许每日给药一次。据报道,加替沙星与其他药物之间几乎没有具有临床意义的相互作用。在CAP患者中,静脉/口服加替沙星400mg/天的患者临床有效率为86.8%至98.0%,细菌根除率为83.1%至100%(治疗后长达28天)。加替沙星显示出与阿莫西林/克拉维酸、头孢曲松(联合或不联合红霉素)相当的疗效,联合或不联合序贯至克拉霉素、左氧氟沙星或克拉霉素治疗。加替沙星与克拉霉素或阿莫西林/克拉维酸同样有效,且在治疗慢性支气管炎急性加重期方面,比7至10天的头孢呋辛酯治疗(在临床反应方面;p<0.035)显著更有效。在急性鼻窦炎中,加替沙星显示出与克拉霉素、曲伐沙星或阿莫西林/克拉维酸相似的临床疗效。加替沙星也成功用于治疗泌尿生殖系统感染。加替沙星一般耐受性良好。在比较试验中,其耐受性概况与对照药物大致相似。最常见的不良事件为胃肠道症状(口服制剂)及注射部位反应。

结论

加替沙星具有广泛的抗菌活性谱,与一些较老的氟喹诺酮类药物相比,对革兰氏阳性菌(如肺炎链球菌)的覆盖更好。该药具有良好的药代动力学特性,每日给药一次,且耐受性至少与其他氟喹诺酮类药物相当。加替沙星是目前可用于临床的氟喹诺酮类药物中的有益补充,在成年患者各种细菌感染的管理中具有重要作用。与其他氟喹诺酮类药物一样,在社区中谨慎控制加替沙星的使用对于防止细菌耐药性的出现从而保持该药物的临床价值很重要。

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