Imaizumi M, Niimi T, Uchida Y, Asaoka M, Ozika T, Amano Y, Uchida T, Hirai K, Kazita M, Abe T
Department of Thoracic Surgery, School of Medicine, Nagoya University.
Jpn J Antibiot. 1988 Nov;41(11):1635-49.
There have been no report on concentrations in human lung tissue of aminoglycoside antibiotics which are frequently used in combination with cephem antibiotics in the treatment of severe respiratory infections. The authors examined lung tissue concentration of astromicin (ASTM) during clinical trials in thoracotomized patients using intravenous drip infusion just before operation. And the following conclusions have been obtained: 1. The average peak serum level obtained upon intravenous drip infusion of ASTM 200 mg for 1 hour just before operation was 11.2 micrograms/ml at 1 hour after starting the administration and half-life of ASTM in beta phase was 2.90 hours. 2. ASTM concentrations in the lung tissue upon 1 hour intravenous drip infusion just before operation at a dose level of 200 mg reached a maximum at 2 hours after the start of the administration averaging 7.7 micrograms/ml and were 27.7-68.8% of serum peak level. 3. Bronchiolar concentrations of ASTM 200 mg upon 1 hour intravenous drip infusion just before operation were 33.0-72.3% of peak serum level. These concentrations appear to be sufficient for the treatment of target infections. 4. The 1 hour intravenous drip infusion of ASTM 200 mg appeared to be clinically safety and useful as was the intramuscular injection of ASTM 200 mg.
在治疗严重呼吸道感染时，经常与头孢菌素类抗生素联合使用的氨基糖苷类抗生素在人体肺组织中的浓度尚无相关报道。作者在开胸手术患者的临床试验中，于手术前通过静脉滴注给药，检测了阿司米星（ASTM）在肺组织中的浓度。并得出以下结论：1. 手术前1小时静脉滴注200mg ASTM 1小时，给药开始后1小时测得的平均血清峰值水平为11.2微克/毫升，ASTM在β相的半衰期为2.90小时。2. 手术前1小时静脉滴注200mg剂量的ASTM，肺组织中的ASTM浓度在给药开始后2小时达到最高，平均为7.7微克/毫升，为血清峰值水平的27.7 - 68.8%。3. 手术前1小时静脉滴注200mg ASTM，细支气管中的浓度为血清峰值水平的33.0 - 72.3%。这些浓度似乎足以治疗目标感染。4. 静脉滴注200mg ASTM 1小时在临床上似乎是安全有效的，与肌肉注射200mg ASTM一样。
