Cazzola M, Matera M G, Tufano M A, Polverino M, Catalanotti P, Varanese L, Rossi F
Istituto di Farmacologia e Tossicologia, Facoltà di Medicina e Chirurgia, Seconda Università Napoletana, Napoli, Italy.
Pulm Pharmacol. 1994 Dec;7(6):377-81. doi: 10.1006/pulp.1994.1044.
The aim of this study was to evaluate the concentrations of dirithromycin, a new macrolide antibiotic, in bronchial secretions (BS), bronchial mucosa (BM), epithelial lining fluid (ELF) and serum in 25 patients with acute exacerbation of chronic bronchitis after a 5-day, once-daily, dirithromycin regimen. All patients received dirithromycin, 500 mg (two 250 mg tablets) given orally once daily at 08.00 fasted, for 5 consecutive days. They were divided into five groups (n = 5 in each group) according to sampling time (24, 48, 72, 96 and 120 h, after the last dose). Mean serum concentrations remained low throughout the study (0.44 microgram/ml at 24 h, 0.31 microgram/ml at 48 h, 0.33 microgram/ml at 72 h, 0.12 microgram/ml at 96 h and 0.11 microgram/ml at 120 h, respectively), although they were higher than the MICs for Moraxella catarrhalis for up to 72 h and than that for Streptococcus pneumoniae for up to 120 h after the last dose. By contrast, in all other samples, mean concentrations were higher than the MICs for many relevant respiratory pathogens for at least 3 days, and higher than that for S. pneumonia and M. catarrhalis for up to 120 h (mean concentrations measured 2.67, 2.15, 1.74, 0.27 and 0.17 micrograms/ml, respectively, in BS; 2.59, 2.59, 1.96, 0.41 and 0.27 micrograms/g, respectively, in BM; 2.21, 2.25, 1.57, 0.22 and 0.15 micrograms/ml, respectively, in ELF). These findings demonstrate that dirithromycin is concentrated in each of these potential sites of infection for up to 3 days after a 5-day course of therapy. Therefore, short-term therapy with dirithromycin may be useful for many respiratory infections.
本研究旨在评估25例慢性支气管炎急性加重患者在接受为期5天、每日一次的地红霉素治疗方案后，支气管分泌物（BS）、支气管黏膜（BM）、上皮衬液（ELF）和血清中新型大环内酯类抗生素地红霉素的浓度。所有患者均接受地红霉素，500mg（两片250mg片剂），于禁食状态下每天08:00口服一次，连续服用5天。根据采样时间（最后一剂后24、48、72、96和120小时）将他们分为五组（每组n = 5）。在整个研究过程中，血清平均浓度一直较低（24小时时为0.44微克/毫升，48小时时为0.31微克/毫升，72小时时为0.33微克/毫升，96小时时为0.12微克/毫升，120小时时为0.11微克/毫升），尽管在最后一剂后长达72小时内高于卡他莫拉菌的最低抑菌浓度（MIC），长达120小时内高于肺炎链球菌的MIC。相比之下，在所有其他样本中，平均浓度至少在3天内高于许多相关呼吸道病原体的MIC，长达120小时内高于肺炎链球菌和卡他莫拉菌的MIC（在BS中的平均浓度分别为2.67、2.15、1.74、0.27和0.17微克/毫升；在BM中分别为2.59、2.59、1.96、0.41和0.27微克/克；在ELF中分别为2.21、2.25、1.57、0.22和0.15微克/毫升）。这些发现表明，在为期5天的治疗疗程后，地红霉素在这些潜在感染部位中的每一个部位均可浓缩长达3天。因此，地红霉素短期治疗可能对许多呼吸道感染有用。
