Ohkoshi M, Okada K, Kawamura N
Jpn J Antibiot. 1982 Mar;35(3):691-703.
Micronomicin is a new aminoglycosidic antibiotic discovered and developed by Kyowa Hakko Kogyo Co., Ltd. It is produced by Micromonospora sagamiensis var. nonreducans. Investigation of micronomicin performed in 134 research facilities in Japan led to the following results. 1) Micronomicin showed a broad antibacterial spectrum against Gram positive and Gram negative bacteria. 2) In susceptibility tests of clinical isolates, micronomicin was almost similarly active to GM. 3) Bactericidal activity of micronomicin against Pseudomonas aeruginosa and E. coli was higher than those of TOB and DKB. 4) Micronomicin showed a synergistic antibacterial activity against Pseudomonas aeruginosa and E. coli with CBPC and SBPC. 5) The therapeutic activity of micronomicin in mice infected with Pseudomonas aeruginosa and Serratia sp. was in high correlation with in vitro antibacterial activity similarly to that of GM. 6) Micronomicin was confirmed to be stable against aminoglycoside 6'-acetyltransferase of Pseudomonas aeruginosa and to be not inactivated. 7) Pharmacokinetics of micronomicin was almost similar to those of GM with respect to the concentrations in the serum, urine and tissues. 8) Ototoxicity of micronomicin in guinea pigs was found to be approximately four times less than that of GM. 9) Nephrotoxicity of micronomicin in rabbits was estimated to be less than those of GM and DKB. In rats, nephrotoxicity of micronomicin was approximately 4 times less than that of GM. 10) Micronomicin was effective on 964 cases out of 1,469 cases from 127 research facilities in Japan (65.6%), suggesting its favorable activity against respiratory tract infections and against urinary tract infections. 11) Side effects with the drug were observed in 43 cases out of 1,532 cases (2.81%). Abnormalities in laboratory findings were also recognized, but transient without severe cases. 12) In conclusion, micronomicin is a favorable drug having lesser ototoxicity and nephrotoxicity as well as antibacterial and bactericidal activity of aminoglycosidic antibiotics usually used.
小诺米星是日本协和发酵工业株式会社发现并研制的一种新型氨基糖苷类抗生素。它由相模小单孢菌无还原变种产生。在日本134个研究机构对小诺米星进行的研究得出了以下结果。1）小诺米星对革兰氏阳性菌和革兰氏阴性菌均显示出广谱抗菌活性。2）在临床分离株的药敏试验中，小诺米星的活性与庆大霉素几乎相似。3）小诺米星对铜绿假单胞菌和大肠杆菌的杀菌活性高于妥布霉素和双去氧卡那霉素。4）小诺米星与羧苄青霉素和磺苄青霉素联合使用时，对铜绿假单胞菌和大肠杆菌显示出协同抗菌活性。5）小诺米星对感染铜绿假单胞菌和沙雷氏菌属的小鼠的治疗活性与体外抗菌活性高度相关，与庆大霉素相似。6）已证实小诺米星对铜绿假单胞菌的氨基糖苷6'-乙酰转移酶稳定，不会被灭活。7）小诺米星的药代动力学在血清、尿液和组织中的浓度方面与庆大霉素几乎相似。8）发现小诺米星对豚鼠的耳毒性约为庆大霉素的四分之一。9）据估计，小诺米星对家兔的肾毒性低于庆大霉素和双去氧卡那霉素。在大鼠中，小诺米星的肾毒性约为庆大霉素的四分之一。10）在日本127个研究机构的1469例病例中，小诺米星对964例有效（65.6%），表明其对呼吸道感染和尿路感染具有良好的活性。11）在1532例病例中有43例（2.81%）观察到药物的副作用。实验室检查结果也有异常，但均为一过性，无严重病例。12）总之，小诺米星是一种良好的药物，耳毒性和肾毒性较小，同时具有常用氨基糖苷类抗生素的抗菌和杀菌活性。
