Okada K, Kawamura N, Ohkoshi M, Nemoto S, Oda T, Ikeda N
Jpn J Antibiot. 1983 Nov;36(11):3302-11.
In recent years, aminoglycoside agents as well as beta-lactam antibiotics have been increasingly used with increased incidence of opportunistic infection caused mainly by Gram-negative bacteria. Therefore, we administered micronomicin sulfate (MCR), reportedly lower in nephrotoxicity, at doses of 60 and 120 mg by intravenous drip infusion for 1 and 2 hours to healthy male volunteers and determined the blood level and the urinary recovery rate. The peak of blood level after 1 hour infusion of MCR was 7.3 micrograms/ml in the 60 mg group and 9.5 micrograms/ml in the 120 mg group. T 1/2 (beta) was 3.34 and 2.48 hours respectively. The peak of blood level after 2 hours infusion of MCR was 5.7 micrograms/ml in the 60 mg group and 8.7 micrograms/ml in the 120 mg group. T 1/2 (beta) was 3.36 and 3.71 hours respectively. In the 120 mg group, the urinary recovery rate for the first 24 hours was 53.5% after 1 hour infusion and 60.9% after 2 hours infusion. In the 60 mg group, the rate was higher, 90.1 and 98.6% respectively. It was suggested that intravenous drip infusion of 120 mg of MCR for 1 hour is comparable to intramuscular injection of the same dose. Further, safety and effectiveness of this drug were studied in 7 clinical cases of urological infection. Good results were obtained in 7 clinical cases given 60 or 120 mg of MCR by intravenous drip infusion. Neither side effects nor abnormal laboratory findings were observed in clinical cases.
近年来,随着主要由革兰氏阴性菌引起的机会性感染发病率的增加,氨基糖苷类药物以及β-内酰胺类抗生素的使用越来越频繁。因此,我们对健康男性志愿者静脉滴注剂量为60毫克和120毫克的硫酸小诺米星(MCR),据说其肾毒性较低,滴注时间为1小时和2小时,并测定了血药浓度和尿回收率。在60毫克组中,MCR滴注1小时后的血药浓度峰值为7.3微克/毫升,120毫克组为9.5微克/毫升。T 1/2(β)分别为3.34小时和2.48小时。MCR滴注2小时后的血药浓度峰值在60毫克组为5.7微克/毫升,120毫克组为8.7微克/毫升。T 1/2(β)分别为3.36小时和3.71小时。在120毫克组中,滴注1小时后前24小时的尿回收率为53.5%,滴注2小时后为60.9%。在60毫克组中,该回收率更高,分别为90.1%和98.6%。提示静脉滴注120毫克MCR 1小时与肌肉注射相同剂量相当。此外,我们在7例泌尿系统感染临床病例中研究了该药物的安全性和有效性。静脉滴注60毫克或120毫克MCR的7例临床病例均取得了良好效果。临床病例中未观察到副作用或实验室检查异常。