Marlin G E, Burgess K R, Burgoyne J, Funnell G R, Guinness M D
Thorax. 1981 Oct;36(10):774-80. doi: 10.1136/thx.36.10.774.
Bronchial mucosal biopsies were obtained during fibreoptic bronchoscopy in 12 patients receiving a new semisynthetic penicillin, piperacillin. The piperacillin levels estimated in bronchial mucosa exceeded those required to eradicate organisms associated with acute bronchitis, Haemophilus influenzae and Streptococcus pneumoniae, and compared favourably with those required for activity against a wide variety of anaerobic and Gram-negative organisms including Pseudomonas aeruginosa. Sputum and serum piperacillin levels were obtained from eight patients with bronchial disease receiving a five to seven day course (8 to 16 g/day). Sputum/serum level ratios were constant for the two dosages (10.7% for 8 g/day; 14.3% for 16 g/day) suggesting a diffusion transfer process, although the presence of pus in the sputum appeared to facilitate penetration. Seven patients achieved sputum levels exceeding those required for activity against Haemophilus influenzae and Streptococcus influenzae, and four for Pseudomonas aeruginosa. This study provides pharmacolinetic support of the use of piperacillin in bronchopulmonary infection.
在12例接受新型半合成青霉素哌拉西林治疗的患者进行纤维支气管镜检查时获取了支气管黏膜活检样本。在支气管黏膜中测得的哌拉西林水平超过了根除与急性支气管炎相关的病原体(流感嗜血杆菌和肺炎链球菌)所需的水平,并且与针对包括铜绿假单胞菌在内的多种厌氧菌和革兰氏阴性菌产生活性所需的水平相比具有优势。从8例接受5至7天疗程(8至16克/天)的支气管疾病患者中获取了痰液和血清中的哌拉西林水平。两种剂量的痰液/血清水平比值恒定(8克/天为10.7%;16克/天为14.3%),提示存在扩散转运过程,尽管痰液中存在脓液似乎有助于药物渗透。7例患者的痰液水平超过了针对流感嗜血杆菌和肺炎链球菌产生活性所需的水平,4例超过了针对铜绿假单胞菌产生活性所需的水平。本研究为哌拉西林在支气管肺部感染中的应用提供了药代动力学支持。