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头孢吡肟:抗菌活性、药代动力学特性及治疗用途综述

Cefepime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

作者信息

Barradell L B, Bryson H M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1994 Mar;47(3):471-505. doi: 10.2165/00003495-199447030-00007.

Abstract

Cefepime is a 'fourth' generation cephalosporin that has a broader spectrum of antibacterial activity than the third generation cephalosporins and is more active in vitro against Gram-positive aerobic bacteria. The fact that cefepime is stable to hydrolysis by many of the common plasmid- and chromosomally-mediated beta-lactamases, and that it is a poor inducer of type I beta-lactamases, indicates that cefepime may be useful for treatment of infections resistant to earlier cephalosporins. In comparative trials, cefepime 1 to 2 g, usually administered intravenously twice daily, was as effective as ceftazidime 1 to 2 g, usually administered 3 times daily, for treatment of bacteraemia and infections of the lower respiratory tract, urinary tract, pelvis and skin and skin structures. Furthermore, cefepime was as effective as ceftazidime and piperacillin or mezlocillin in combination with gentamicin when administered as empirical treatment for fever in patients with neutropenia. A limited number of trials have found cefepime to be as effective as cefotaxime for the treatment of gynaecological and lower respiratory tract infections. Similarly, cefepime 2 g twice daily intravenously (alone or in combination with metronidazole) was as effective as gentamicin in combination with mezlocillin or clindamycin, respectively, for the treatment of intra-abdominal infection. Cefepime has a linear pharmacokinetic profile, an elimination half-life of approximately 2 hours and is primarily excreted by renal mechanisms as unchanged drug. Cefepime has a tolerability profile similar to that of other parenteral cephalosporins; adverse events are primarily gastrointestinal in nature. A total of 1.4 and 2.9% of patients receiving cefepime < or = 2 g/day and > 2 g/day, respectively, required treatment withdrawal as a result of any adverse event. Thus, cefepime has the advantage of an improved spectrum of antibacterial activity, and is less susceptible to hydrolysis by some beta-lactamases, compared with third generation cephalosporins. Despite these advantages, cefepime has not been found to be more effective than ceftazidime and cefotaxime in clinical trials, although most trials selected patients with organisms sensitive in vitro to both comparator agents. Further trials, particularly in areas of widespread bacterial resistance, are required to confirm the positioning of cefepime for treatment of serious infection, and in particular to further explore whether its potential advantages result in clinical benefits.

摘要

头孢吡肟是一种“第四代”头孢菌素,其抗菌活性谱比第三代头孢菌素更广,并且在体外对革兰氏阳性需氧菌更具活性。头孢吡肟对许多常见的质粒介导和染色体介导的β-内酰胺酶的水解作用稳定,且它是I型β-内酰胺酶的弱诱导剂,这表明头孢吡肟可能对治疗耐早期头孢菌素的感染有用。在比较试验中,头孢吡肟1至2克,通常每日静脉注射两次,与头孢他啶1至2克(通常每日给药3次)在治疗菌血症以及下呼吸道、泌尿道、盆腔、皮肤和皮肤结构感染方面效果相当。此外,当作为经验性治疗用于中性粒细胞减少症患者的发热时,头孢吡肟与头孢他啶以及哌拉西林或美洛西林联合庆大霉素的效果相当。有限数量的试验发现头孢吡肟在治疗妇科和下呼吸道感染方面与头孢噻肟效果相当。同样,静脉注射头孢吡肟2克每日两次(单独或与甲硝唑联合)在治疗腹腔内感染方面分别与庆大霉素联合美洛西林或克林霉素效果相当。头孢吡肟具有线性药代动力学特征,消除半衰期约为2小时,主要通过肾脏机制以原形药物排泄。头孢吡肟的耐受性与其他胃肠外头孢菌素相似;不良事件主要为胃肠道性质。接受头孢吡肟≤2克/天和>2克/天的患者中,分别有1.4%和2.9%因任何不良事件而需要停药。因此,与第三代头孢菌素相比,头孢吡肟具有抗菌活性谱改善的优势,并且对某些β-内酰胺酶的水解作用更不敏感。尽管有这些优势,但在临床试验中尚未发现头孢吡肟比头孢他啶和头孢噻肟更有效,尽管大多数试验选择的患者其病原体在体外对两种对照药物均敏感。需要进一步的试验,特别是在细菌耐药广泛的地区,以确认头孢吡肟在治疗严重感染中的定位,尤其是进一步探索其潜在优势是否能带来临床益处。

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