Burkhardt Olaf, Majcher-Peszynska Jolanta, Borner Klaus, Mundkowski Ralf, Drewelow Bernd, Derendorf Hartmut, Welte Tobias
Department of Pulmonary and Critical Care Medicine, University Otto-von-Guericke, Magdeburg, Germany.
J Clin Pharmacol. 2005 Jun;45(6):659-65. doi: 10.1177/0091270005276117.
Ertapenem is approved for the treatment of community-acquired pneumonia (CAP), but its in vivo penetration into lung tissue (LT), epithelial lining fluid (ELF), and alveolar cells (AC) is unknown. Fifteen patients undergoing thoracotomy were treated with 1 g intravenously for perioperative prophylaxis. Bronchoalveolar lavage was performed 1, 3, and 5 hours after ertapenem infusion. Normal LT was sampled at the time of lung extraction. Blood was collected before and at different time points up to 24 hours after infusion. Mean concentrations of ertapenem in plasma, ELF, and AC were at 1.0 hour, 63.1, 4.06, 0.004 mg/L; at 3.0 hours, 39.7, 2.59, 0.003 mg/L; and at 5.0 hours, 27.2, 2.83, 0.007 mg/L. Mean (range) concentration in LT was 7.60 (2.5-19.4) mg/kg tissue 1.5 to 4.5 hours after infusion. In plasma, ertapenem exhibited a Cmax of 94.7 +/- 23.3 mg/L and an AUC(0-last) of 501.1 +/- 266.3 mg x h/L. These results, combined with the reported (MIC)90 of most CAP bacteria, support the previously observed clinical efficacy of ertapenem in the treatment of CAP.
厄他培南已被批准用于治疗社区获得性肺炎（CAP），但其在体内对肺组织（LT）、上皮衬液（ELF）和肺泡细胞（AC）的渗透情况尚不清楚。15例接受开胸手术的患者静脉注射1g进行围手术期预防。在厄他培南输注后1、3和5小时进行支气管肺泡灌洗。在肺切除时采集正常肺组织样本。在输注前及输注后长达24小时的不同时间点采集血液。厄他培南在血浆、ELF和AC中的平均浓度在1.0小时时分别为63.1、4.06、0.004mg/L；在3.0小时时分别为39.7、2.59、0.003mg/L；在5.0小时时分别为27.2、2.83、0.007mg/L。输注后1.5至4.5小时，肺组织中的平均（范围）浓度为7.60（2.5 - 19.4）mg/kg组织。在血浆中，厄他培南的Cmax为94.7±23.3mg/L，AUC(0-last)为501.1±266.3mg·h/L。这些结果，结合大多数CAP细菌报告的（MIC）90，支持了先前观察到的厄他培南治疗CAP的临床疗效。
