J&P Medical Research Ltd., Vienna, Austria.
Int J Antimicrob Agents. 2010 Jul;36(1):84-6. doi: 10.1016/j.ijantimicag.2010.03.007. Epub 2010 Apr 24.
The present study aimed at assessing unbound extracellular concentrations of linezolid in inflamed soft tissue and bone of diabetic patients suffering from severe bacterial foot infections. Linezolid was administered intravenously twice daily at a dosage of 600 mg. At steady-state conditions, the microdialysis technique was utilised to sample serially interstitial space fluid from inflamed subcutaneous adipose tissue and metatarsal bone from 0-8h post dose in three representative patients. Mean peak concentrations of free linezolid in plasma, healthy subcutis, inflamed subcutis and cancellous bone were 16.6+/-3.0, 15.5+/-2.5, 15.8+/-2.8 and 15.1+/-4.1mg/L, respectively. The degree of tissue penetration as expressed by the ratio of the area under the concentration-time curve of free linezolid from 0-12h (fAUC(0-12)) in tissue to the fAUC(0-12) in plasma was 1.32+/-0.09, 1.12+/-0.22 and 1.09+/-0.11 for healthy subcutis, inflamed subcutis and bone, respectively. Based on currently available pharmacokinetic/pharmacodynamic targets, we conclude that linezolid administered at 600 mg twice daily may be considered an effective treatment in diabetic patients suffering from bacterial foot infection complicated by osteomyelitis.
本研究旨在评估患有严重细菌性足部感染的糖尿病患者炎症性软组织和骨骼中游离型利奈唑胺的细胞外浓度。利奈唑胺每天静脉注射两次，剂量为 600mg。在稳态条件下，利用微透析技术在三个代表性患者中从 0 到 8 小时，连续从炎症性皮下脂肪组织和跖骨采集间质空间液样本。游离型利奈唑胺在血浆、健康皮下组织、炎症性皮下组织和松质骨中的平均峰值浓度分别为 16.6+/-3.0、15.5+/-2.5、15.8+/-2.8 和 15.1+/-4.1mg/L。游离型利奈唑胺 0-12 小时（fAUC(0-12)）在组织中的浓度-时间曲线下面积与血浆中的 fAUC(0-12)的比值（表示组织穿透程度的比值）分别为 1.32+/-0.09、1.12+/-0.22 和 1.09+/-0.11，用于健康皮下组织、炎症性皮下组织和骨骼。根据目前可用的药代动力学/药效学目标，我们得出结论，每天两次给予 600mg 的利奈唑胺可能被认为是治疗并发骨髓炎的糖尿病细菌性足部感染患者的有效治疗方法。
