Matsumoto K, Shishido H, Takahashi A
Jpn J Antibiot. 1985 Jun;38(6):1557-65.
The safety and pharmacokinetics of micronomicin (MCR) by intravenous drip infusion were evaluated and the intravenous drip infusion of MCR was carried out on several cases on which the blood levels and clinical usefulness of MCR were investigated. Five healthy adult male volunteers received by crossover method 1 hour intravenous drip infusion of MCR in doses of 60 and 120 mg and intramuscular injection in a dose of 120 mg. The mean highest serum level was 6.3 micrograms/ml by intravenous drip infusion of 60 mg, 10.7 micrograms/ml by intravenous drip infusion of 120 mg, and 10.3 micrograms/ml by intramuscular injection of 120 mg. Serum levels of MCR were similar for intravenous drip infusion and intramuscular injection of 120 mg of MCR. The biological serum half-lives of MCR were 2.15 hours by 1 hour intravenous drip infusion of 60 mg, 2.54 hours by 1 hour intravenous drip infusion of 120 mg, and 1.59 hours by intramuscular injection of 120 mg. The mean urinary recovery rates within 24 hours after administration were 74.3% by 1 hour intravenous drip infusion of 60 mg, 59.6% by 1 hour intravenous drip infusion of 120 mg, and 64.9% by intramuscular injection of 120 mg, the results being nearly consistent. In all treatment groups, MCR could be safely administered. Intravenous drip infusion of MCR in a dose of 60 or 120 mg once or twice a day was conducted on a total of 6 cases consisting of 2 cases of pneumonia and 4 cases of urinary tract infections.(ABSTRACT TRUNCATED AT 250 WORDS)
评估了小诺米星(MCR)静脉滴注的安全性和药代动力学,并对几例患者进行了MCR静脉滴注,同时研究了MCR的血药浓度和临床疗效。5名健康成年男性志愿者采用交叉法接受了剂量为60毫克和120毫克的MCR 1小时静脉滴注以及剂量为120毫克的肌肉注射。60毫克静脉滴注时的平均最高血清浓度为6.3微克/毫升,120毫克静脉滴注时为10.7微克/毫升,120毫克肌肉注射时为10.3微克/毫升。120毫克MCR静脉滴注和肌肉注射的血清浓度相似。60毫克1小时静脉滴注时MCR的生物血清半衰期为2.15小时,120毫克1小时静脉滴注时为2.54小时,120毫克肌肉注射时为1.59小时。给药后24小时内的平均尿回收率,60毫克1小时静脉滴注时为74.3%,120毫克1小时静脉滴注时为59.6%,120毫克肌肉注射时为64.9%,结果基本一致。在所有治疗组中,MCR均可安全给药。对总共6例患者进行了MCR静脉滴注治疗,剂量为60或120毫克,每日1次或2次,其中包括2例肺炎患者和4例尿路感染患者。(摘要截短于250字)