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用于治疗尿路感染的新型碳青霉烯类药物。

Newer carbapenems for urinary tract infections.

作者信息

Matsumoto Tetsuro, Muratani Tetsuro

机构信息

Department of Urology, School of Medicine, University of Occupational and Environmental Health, 1-1, Iseigaoka, Yahatanishi-ku, Kitakyushu 807-8555, Japan.

出版信息

Int J Antimicrob Agents. 2004 Sep;24 Suppl 1:S35-8. doi: 10.1016/j.ijantimicag.2004.03.001.

Abstract

Four carbapenems have been available clinically in Japan. These are imipenem/cilastatin (IMIP/CS) and panipenem/ betamipron (PANI/BP) of the older compounds and newer carbapenems such as biapem (BIAP) and meropenem (MERO). The latter compounds are relatively stable to dehydropeptidase-1 (DHP-1) and have been reported to have higher antimicrobial activities compared to the earlier carbapenems. The antimicrobial activity of these four carbapenems against fresh urinary isolates showed high activities against Enterobacteriacae such as Serratia marcescens, Enterobacter cloacae, Citrobacter freundii and Escherichia coli containing the class C-beta-lactamase- and extended spectrum beta-lactamase (ESBL)-producing strains compared to piperacillin (PIPC) and ceftazidime (CTAZ). Against Pseudomonas aeruginosa, the carbapenems, with the exception of panipenem showed strong antimicrobial activities compared to PIPC and CTAZ. High activities were also seen against Enterococcus faecalis, Staphylococcus aureus and Staphylococcus epidermidis, but methicillin-resistant strains were not affected. The first generation carbapenems showed better activity against E. faecalis than newer carbapenems. All four carbapenems were similar in clinical effectiveness in double blind trials for complicated urinary tract infections (UTIs). However, PANI/BP is less effective in UTIs caused by P. aeruginosa than IMIP/CS. MERO showed better eradication rate of P. aeruginosa than IMIP/CS. Retrospective analysis of treated cases using carbapenems showed a rapid defervescence in the treatment of febrile complicated UTIs, which were mainly caused by mixed infection of Gram-negative and Gram-positive bacteria, especially those involving P. aeruginosa and E. faecalis.

摘要

在日本临床上有四种碳青霉烯类药物可供使用。这些药物包括较早的化合物亚胺培南/西司他丁(IMIP/CS)和帕尼培南/倍他米隆(PANI/BP)以及较新的碳青霉烯类药物,如比阿培南(BIAP)和美罗培南(MERO)。后两种化合物对脱氢肽酶-1(DHP-1)相对稳定,据报道与早期的碳青霉烯类药物相比具有更高的抗菌活性。这四种碳青霉烯类药物对新鲜尿液分离株的抗菌活性显示,与哌拉西林(PIPC)和头孢他啶(CTAZ)相比,它们对肠杆菌科细菌如粘质沙雷氏菌、阴沟肠杆菌、弗氏柠檬酸杆菌和含有C类β-内酰胺酶及超广谱β-内酰胺酶(ESBL)的大肠埃希菌具有较高的活性。对于铜绿假单胞菌,除帕尼培南外,碳青霉烯类药物与PIPC和CTAZ相比显示出较强的抗菌活性。对粪肠球菌、金黄色葡萄球菌和表皮葡萄球菌也有较高活性,但耐甲氧西林菌株不受影响。第一代碳青霉烯类药物对粪肠球菌的活性比新型碳青霉烯类药物更好。在复杂性尿路感染(UTIs)的双盲试验中,所有四种碳青霉烯类药物的临床疗效相似。然而,PANI/BP在由铜绿假单胞菌引起的UTIs中比IMIP/CS效果差。美罗培南对铜绿假单胞菌的根除率比IMIP/CS更好。对使用碳青霉烯类药物治疗的病例进行回顾性分析显示,在治疗主要由革兰氏阴性菌和革兰氏阳性菌混合感染引起的发热性复杂性UTIs时,尤其是涉及铜绿假单胞菌和粪肠球菌的感染,体温能迅速下降。

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