Sörgel F, Kinzig M
IBMP, Institute for Biomedical and Pharmaceutical Research, Nürnberg-Heroldsberg, Germany.
Intensive Care Med. 1994 Jul;20 Suppl 3:S14-20. doi: 10.1007/BF01745246.
Piperacillin/tazobactam is a new combination of a broad-spectrum penicillin and a beta-lactamase inhibitor. In studies in healthy volunteers, the pharmacokinetics of piperacillin combined with tazobactam were similar to those of piperacillin alone. In contrast, tazobactam administered with piperacillin achieved higher plasma concentrations and had a longer half-life than tazobactam administered alone. Intravenous infusion of 4.0 g piperacillin with 0.5 g tazobactam over 5 min resulted in mean maximum plasma concentrations of 380 micrograms piperacillin/ml and 35.3 micrograms tazobactam/ml; half-lives were 1.14 h for piperacillin and 0.92 h for tazobactam. Within 30 min of infusion, piperacillin/tazobactam achieves 16-85% of plasma concentrations in skin, muscle, lung, gallbladder, and intestinal mucosa. Plasma and tissue levels remain above the MIC90s of major pathogens for 2 h post administration. These findings show that piperacillin/tazobactam is truly synergistic combination which can be expected to be effective in treating a wide variety of infections in the clinical setting.
哌拉西林/他唑巴坦是一种广谱青霉素与β-内酰胺酶抑制剂的新型组合。在健康志愿者的研究中，哌拉西林与他唑巴坦联合使用时的药代动力学与单独使用哌拉西林时相似。相比之下，与哌拉西林一起给药的他唑巴坦比单独给药的他唑巴坦达到更高的血浆浓度且半衰期更长。在5分钟内静脉输注4.0克哌拉西林与0.5克他唑巴坦，导致哌拉西林的平均最大血浆浓度为380微克/毫升，他唑巴坦为35.3微克/毫升；哌拉西林的半衰期为1.14小时，他唑巴坦为0.92小时。在输注30分钟内，哌拉西林/他唑巴坦在皮肤、肌肉、肺、胆囊和肠黏膜中的血浆浓度达到16% - 85%。给药后2小时，血浆和组织水平仍高于主要病原体的MIC90。这些发现表明哌拉西林/他唑巴坦是一种真正具有协同作用的组合，有望在临床环境中有效治疗多种感染。
