Pagani L, Migliavacca R, Luzzaro F, Giacobone E, Perilli M, Micheletti P, Amicosante G
Section of Microbiology, Department of Morphological and Clinical Sciences, University of Pavia, Varese, Italy.
Chemotherapy. 1998 Nov-Dec;44(6):377-84. doi: 10.1159/000007147.
beta-Lactam resistance on the part of the Enterobacteriaceae causes serious therapeutic problems in our institutions due to their production of extended-spectrum beta-lactamases (ESbetaLs). We studied the in vitro activity of beta-lactam/beta-lactamase inhibitor combinations and third-generation cephalosporins and monobactams against 71 clinically relevant Enterobacteriaceae which produced TEM- and SHV-derivative ESbetaLs. Of the single drugs and combinations tested, piperacillin/tazobactam proved to be the most effective. Piperacillin/tazobactam was highly active against Proteus mirabilis, with minimum inhibitory concentrations (MICs) ranging from 0.125 to 16 microg/ml; Escherichia coli (MICs from 2 to 16 microg/ml) and Serratia marcescens (MICs from 4 to 8 microg/ml), while its activity against Klebsiella pneumoniae ESbetaL producers turned out to be closely related to the type and the amount of enzyme produced, the MIC ranging from 1 to 128 microg/ml. The antibacterial activity of piperacillin/tazobactam was stronger than that of ticarcillin/clavulanate, ceftriaxone, cefotaxime, ceftazidime and aztreonam, and the combination shared favorable in vitro activity properties against the ESbetaL producers with imipenem which, however, should be kept as reserve product.
肠杆菌科细菌对β-内酰胺类抗生素产生耐药性，由于其产生超广谱β-内酰胺酶（ESβLs），给我们机构带来了严重的治疗问题。我们研究了β-内酰胺/β-内酰胺酶抑制剂联合用药、第三代头孢菌素和单环β-内酰胺类抗生素对71株产生TEM和SHV衍生ESβLs的临床相关肠杆菌科细菌的体外活性。在所测试的单一药物和联合用药中，哌拉西林/他唑巴坦被证明是最有效的。哌拉西林/他唑巴坦对奇异变形杆菌具有高度活性，最低抑菌浓度（MICs）范围为0.125至16μg/ml；对大肠杆菌（MICs为2至16μg/ml）和粘质沙雷氏菌（MICs为4至8μg/ml）也有活性，而其对产ESβL的肺炎克雷伯菌的活性结果与所产生酶的类型和数量密切相关，MIC范围为1至128μg/ml。哌拉西林/他唑巴坦的抗菌活性强于替卡西林/克拉维酸、头孢曲松、头孢噻肟、头孢他啶和氨曲南，并且该联合用药与亚胺培南对产ESβL细菌具有相似的良好体外活性特性，不过亚胺培南应作为储备药物。
