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头孢美唑(CS-1170),一种拥有十年临床经验的“新型”头孢霉素。

Cefmetazole (CS-1170), a "new" cephamycin with a decade of clinical experience.

作者信息

Jones R N

机构信息

Clinical Microbiology Institute, Tualatin, Oregon.

出版信息

Diagn Microbiol Infect Dis. 1989 Sep-Oct;12(5):367-79. doi: 10.1016/0732-8893(89)90106-5.

Abstract

In vitro and in vivo study results were reviewed from cefmetazole, a "new" parenteral cephamycin. Cefmetazole's spectrum of activity was comparable to that of second-generation cephalosporins, which includes clinical coverage of many Enterobacteriaceae, Staphylococcus spp., streptococci, Haemophilus spp., pathogenic Neisseria, Branhamella catarrhalis, and anaerobic bacteria. Cefmetazole was generally more potent (two- to eightfold) than cefoxitin against organisms within their spectrums and was particularly active for staphylococci (MIC90, 2.0 micrograms/ml). Methicillin-resistant S. aureus strains were more susceptible to cefmetazole alone or in combination (fosfomycin) than any other cephamycin. Cefmetazole has demonstrated excellent stability to aerobic and anaerobic organism-produced beta-lactamases. It also inhibits Type I cephalosporinases and, uniquely, some other cephalosporinases produced by the Bacteroides. This superior stability, enzyme interaction, and better penetration into bacterial cells results in a sustained bactericidal effect and a capacity for more infrequent dosing. The cefmetazole serum elimination half-life was 1.5 hr, also justifying use at greater than or equal to 8-hr intervals. Clinical trials in the United States and Japan demonstrated an acceptably high cefmetazole infection cure rate (88% to 100%), especially in direct comparative studies with cefoxitin. Cefmetazole was also proven very effective in minimizing infectious wound morbidity (prophylaxis) using 2 g single- or multidose regimens. Adverse drug reactions were usually minor; in the Japanese surveillance trial (118,318 patients) the rate was only 2.2% (8.8% in United States). Cefmetazole has been extensively and safely used in Japan since 1980.

摘要

对一种“新型”胃肠外给药的头孢美唑进行了体外和体内研究结果的综述。头孢美唑的抗菌谱与第二代头孢菌素相当,包括对许多肠杆菌科细菌、葡萄球菌属、链球菌、嗜血杆菌属、致病性奈瑟菌、卡他布兰汉菌和厌氧菌的临床覆盖范围。在其抗菌谱范围内,头孢美唑通常比头孢西丁更具效力(两到八倍),对葡萄球菌特别有效(MIC90为2.0微克/毫升)。耐甲氧西林金黄色葡萄球菌菌株单独使用头孢美唑或与(磷霉素)联合使用时比任何其他头孢美唑更敏感。头孢美唑对需氧菌和厌氧菌产生的β-内酰胺酶表现出优异的稳定性。它还抑制I型头孢菌素酶,独特的是,它还能抑制拟杆菌产生的其他一些头孢菌素酶。这种卓越的稳定性、酶相互作用以及更好地渗透到细菌细胞中导致持续的杀菌作用和减少给药频率的能力。头孢美唑的血清消除半衰期为1.5小时,这也证明了每8小时或更长时间给药一次是合理的。在美国和日本进行的临床试验表明,头孢美唑的感染治愈率较高(88%至100%),在与头孢西丁的直接对比研究中尤其如此。使用2克单剂量或多剂量方案,头孢美唑在将感染性伤口发病率(预防)降至最低方面也被证明非常有效。药物不良反应通常较轻;在日本的监测试验(118318名患者)中,发生率仅为2.2%(在美国为8.8%)。自1980年以来,头孢美唑在日本已得到广泛且安全的使用。

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