Sader HS, Ferreira AT, Tosin I, Gales AC, Keim LS, Carbadillo JM, Mello SJ, Tavares W
Special Laboratory of Clinical Microbiology, Federal University of São Paulo.
Braz J Infect Dis. 1998 Oct;2(5):241-255.
Piperacillin/tazobactam is a highly active antibiotic against most clinically important species of Gram-negative and positive bacteria, including anaerobes. It has never been used or tested against bacteria isolated in Brazil. In this article we report the in vitro activity of piperacillin/tazobactam against clinical isolates from two tertiary hospitals in São Paulo and Rio de Janeiro and review the evolving clinical literature. The study was performed before its commercialization in Brazil. Its activity was compared to that of several broad-spectrum antimicrobial agents commercially available in Brazil. Piperacillin/tazobactam was active against 83% of the isolates tested, while imipenem was active against 91%, cefepime 77%, and ciprofloxacin 73%. Against Enterobacteriaceae (n=398), cefepime was more active than piperacillin/tazobactam (92% versus 88%). Klebsiella pneumoniae strains (n=95) presented low susceptibility to piperacillin/tazobactam (79%), ceftazidime (67%), and to cefepime (82%) indicating a high percentage of ESBL-producing strains. The most active compounds against this species were imipenem (100%) and ciprofloxacin (93%). Piperacillin/tazobactam was the most active compound against Gram-positive cocci (n=238; percentage of susceptibility rank order: piperacillin/tazobactam = imipenem > ciprofloxacin > cefepime) and the second most active against nonenteric Gram-negative bacilli (n=250, rank order: imipenem [72%] > piperacillin/tazobactam [60%] > cefepime [56%] > ceftazidime [52%] > gentamicin [45%] > ciprofloxacin = aztreonam [42%]). Cefepime was the most active compound against P. aeruginosa (n=128, only 67%), followed by ceftazidime (64%), piperacillin/tazobactam (63%) and imipenem (59%). Only imipenem (91%) was active against more than 50% of the A. baumannii isolates (n=79) tested. Piperacillin/tazobactam was the second most active compound against A. baumannii (49%) and the most active against B. cepacia (91%). Our results demonstrated a high level of antimicrobial resistance in the hospitals evaluated, especially among nonenteric Gram-negative bacilli; and clonal dissemination of multiresistant strains. Piperacillin/tazobactam may contribute to the treatment of nosocomial infections in Brazil, however, some degree of resistance was detected in some species in the instance of frequent multiresistant bacteria in the tertiary level hospitals where the drug was evaluated.
哌拉西林/他唑巴坦是一种对大多数临床上重要的革兰氏阴性菌和阳性菌（包括厌氧菌）具有高活性的抗生素。它从未在巴西分离出的细菌上使用过或进行过测试。在本文中，我们报告了哌拉西林/他唑巴坦对圣保罗和里约热内卢两家三级医院临床分离株的体外活性，并回顾了不断发展的临床文献。该研究在其于巴西商业化之前进行。将其活性与巴西市场上几种广谱抗菌药物的活性进行了比较。哌拉西林/他唑巴坦对83%的测试分离株有活性，而亚胺培南对91%的分离株有活性，头孢吡肟为77%，环丙沙星为73%。针对肠杆菌科细菌（n = 398），头孢吡肟比哌拉西林/他唑巴坦更具活性（92%对88%）。肺炎克雷伯菌菌株（n = 95）对哌拉西林/他唑巴坦（79%）、头孢他啶（67%）和头孢吡肟（82%）的敏感性较低，表明产超广谱β-内酰胺酶（ESBL）菌株的比例较高。针对该菌属最具活性的化合物是亚胺培南（100%）和环丙沙星（93%）。哌拉西林/他唑巴坦是对革兰氏阳性球菌（n = 238；敏感性百分比排序：哌拉西林/他唑巴坦 = 亚胺培南 > 环丙沙星 > 头孢吡肟）最具活性的化合物，对非肠道革兰氏阴性杆菌（n = 250，排序：亚胺培南[72%] > 哌拉西林/他唑巴坦[60%] > 头孢吡肟[56%] > 头孢他啶[52%] > 庆大霉素[45%] > 环丙沙星 = 氨曲南[42%]）是第二具活性的化合物。头孢吡肟是对铜绿假单胞菌（n = 128，仅67%）最具活性的化合物，其次是头孢他啶（64%）、哌拉西林/他唑巴坦（63%）和亚胺培南（59%）。仅亚胺培南（91%）对超过50%的鲍曼不动杆菌分离株（n = 79）有活性。哌拉西林/他唑巴坦是对鲍曼不动杆菌第二具活性的化合物（49%），对洋葱伯克霍尔德菌最具活性（91%）。我们的结果表明，在所评估的医院中存在高水平的抗菌药物耐药性，尤其是在非肠道革兰氏阴性杆菌中；以及多重耐药菌株的克隆传播。哌拉西林/他唑巴坦可能有助于巴西医院感染的治疗，然而，在评估该药物的三级医院中，在一些常见的多重耐药细菌种类中检测到了一定程度的耐药性。
