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头孢丙烯。对其抗菌活性、药代动力学特性及治疗潜力的综述。

Cefprozil. A review of its antibacterial activity, pharmacokinetic properties, and therapeutic potential.

作者信息

Wiseman L R, Benfield P

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1993 Feb;45(2):295-317. doi: 10.2165/00003495-199345020-00008.

Abstract

Cefprozil is an orally active cephalosporin which has demonstrated activity against a wide range of organisms in vitro. It is particularly active against the Gram-positive organisms Streptococcus pyogenes, pneumoniae and agalactiae and against methicillin-susceptible Staphylococcus aureus. Strains of methicillin-resistant S. aureus are not susceptible to cefprozil. Cefprozil is also moderately active against Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, many Enterobacteriaceae and certain anaerobic organisms, and is relatively stable to hydrolysis by a number of beta-lactamases. In comparative trials, the clinical and bacteriological efficacy of cefprozil 500mg or 20 mg/kg administered once or twice daily has been comparable with multiple daily dosage regimens of erythromycin in patients with tonsillitis or pharyngitis, with cefaclor and amoxicillin/clavulanate in lower respiratory tract infections, with amoxicillin/clavulanate and erythromycin in skin and skin-structure infections and with cefaclor in acute uncomplicated urinary tract infections. The clinical efficacy of cefprozil is similar to that of cefaclor in patients with tonsillitis or pharyngitis but the bacteriological efficacy of cefprozil is significantly greater than that of cefaclor. Cefprozil is clinically more effective than cefuroxime axetil in the treatment of lower respiratory tract infections and demonstrated greater efficacy than cefaclor in one of 2 comparative studies when administered twice daily in patients with skin and skin-structure infections. In children with acute otitis media, cefprozil 15 mg/kg twice daily was as effective as cefaclor or amoxicillin/clavulanate 13.3 mg/kg 3 times daily and was as effective as cefixime 8 mg/kg once daily. The most frequently reported adverse effects associated with cefprozil, diarrhoea and nausea, are usually mild to moderate in severity and discontinuation of treatment is rarely necessary. Thus, cefprozil with its convenient administration regimen appears to be a suitable alternative to cefaclor, cefixime, amoxicillin/clavulanate or erythromycin for the treatment of upper and lower respiratory tract infections, skin and skin-structure infections, and otitis media in children. While cefprozil has shown similar efficacy to cefaclor in the treatment of uncomplicated urinary tract infections, well-controlled clinical trials comparing its efficacy with that of cotrimoxazole (trimethoprim+sulfamethoxazole) in this indication are required.

摘要

头孢丙烯是一种口服活性头孢菌素,已在体外显示出对多种微生物的活性。它对革兰氏阳性菌化脓性链球菌、肺炎链球菌和无乳链球菌以及对甲氧西林敏感的金黄色葡萄球菌具有特别活性。耐甲氧西林金黄色葡萄球菌菌株对头孢丙烯不敏感。头孢丙烯对流感嗜血杆菌、卡他莫拉菌、淋病奈瑟菌、许多肠杆菌科细菌和某些厌氧菌也有中度活性,并且对多种β-内酰胺酶的水解相对稳定。在比较试验中,对于扁桃体炎或咽炎患者,每日一次或两次给予500mg或20mg/kg头孢丙烯的临床和细菌学疗效与红霉素的多次每日给药方案相当;对于下呼吸道感染患者,与头孢克洛和阿莫西林/克拉维酸相当;对于皮肤及皮肤结构感染患者,与阿莫西林/克拉维酸和红霉素相当;对于急性单纯性尿路感染患者,与头孢克洛相当。在扁桃体炎或咽炎患者中,头孢丙烯的临床疗效与头孢克洛相似,但头孢丙烯的细菌学疗效明显优于头孢克洛。在治疗下呼吸道感染时,头孢丙烯在临床上比头孢呋辛酯更有效,并且在一项比较研究中,对于皮肤及皮肤结构感染患者每日两次给药时,其疗效优于头孢克洛。在患有急性中耳炎的儿童中,每日两次给予15mg/kg头孢丙烯与每日三次给予13.3mg/kg头孢克洛或阿莫西林/克拉维酸效果相同,并且与每日一次给予8mg/kg头孢克肟效果相同。与头孢丙烯相关的最常报告的不良反应腹泻和恶心,严重程度通常为轻度至中度,很少需要停药。因此,对于治疗儿童的上、下呼吸道感染、皮肤及皮肤结构感染和中耳炎,头孢丙烯因其方便的给药方案似乎是头孢克洛、头孢克肟、阿莫西林/克拉维酸或红霉素的合适替代药物。虽然头孢丙烯在治疗单纯性尿路感染方面已显示出与头孢克洛相似的疗效,但需要进行对照良好的临床试验来比较其在该适应症中与复方新诺明(甲氧苄啶+磺胺甲恶唑)的疗效。

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