Bergogne-Bérézin E, Berthelot G, Kafe H
Pathol Biol (Paris). 1986 Jun;34(5 Pt 2):653-6.
Piperacillin is a ureido-penicillin characterized by the presence of a piperazine group at the position 6 of the beta-lactam ring. This group confers a broader spectrum that includes Pseudomonas. In vitro studies have shown that piperacillin is active against clinical strains recovered from intensive care unit patients with severe lower respiratory tract infections. The purpose of our study was to investigate the usefulness of piperacillin in such patients by evaluating the drug's diffusion into bronchial secretions. A single 4 g dose of piperacillin was given intravenously over three minutes to each of 6 intensive care unit patients. Serum and bronchial secretion samples (obtained through a tracheal intubation or tracheostomy tube) were taken 1/2 hour, 2 h, 4 h and 6 h after the injection to evaluate piperacillin kinetics. Serum piperacillin concentrations were maximal 30 mn after the IV (mean value: 90.6 +/- 23.8 micrograms/ml) and thereafter fell gradually (mean value after 4 hours: 40.4 +/- 27.5 micrograms/ml). Peak concentrations in bronchial secretions were recorded at 2 hours (12.2 +/- 8.5 micrograms/ml); the mean residual value at 6 hours was 4.9 +/- 8.7 micrograms/ml. The diffusion ratio (ratio of bronchial secretion concentration to simultaneous serum concentration) was 15.5% to 24.5%. Our results show that the diffusion of piperacillin into bronchial secretions is outstanding and support the use of this drug in severe respiratory tract infections.
哌拉西林是一种脲基青霉素,其特点是在β-内酰胺环的6位上有一个哌嗪基团。该基团赋予了更广泛的抗菌谱,包括假单胞菌属。体外研究表明,哌拉西林对从患有严重下呼吸道感染的重症监护病房患者中分离出的临床菌株具有活性。我们研究的目的是通过评估药物在支气管分泌物中的扩散情况,来研究哌拉西林在此类患者中的效用。给6名重症监护病房患者每人静脉注射单剂量4克哌拉西林,注射时间为3分钟。在注射后半小时、2小时、4小时和6小时采集血清和支气管分泌物样本(通过气管插管或气管造口管获取),以评估哌拉西林的动力学。静脉注射后30分钟血清哌拉西林浓度达到最大值(平均值:90.6±23.8微克/毫升),此后逐渐下降(4小时后的平均值:40.4±27.5微克/毫升)。支气管分泌物中的峰值浓度在2小时时记录(12.2±8.5微克/毫升);6小时时的平均残留值为4.9±8.7微克/毫升。扩散率(支气管分泌物浓度与同时期血清浓度的比值)为15.5%至24.5%。我们的结果表明,哌拉西林在支气管分泌物中的扩散情况良好,并支持将该药物用于严重呼吸道感染。