Mazzei T, Paradiso M, Nicoletti I, Periti P
J Infect Dis. 1976 Nov;134 SUPPL:S374-9. doi: 10.1093/infdis/135.supplement_2.s374.
Based on the proportion of resistant, moderately sensitive, and sensitive strains, the descending order of activity of amikacin against clinical isolates of urinary pathogens was Salmonella, Klebsiella, Enterobacter, Escherichia coli, Staphylococcus aureus, Citrobacter, Proteus species, and Pseudomonas aeruginosa. However, amikacin was the most active of the antibiotics tested (including gentamicin and tobramycin) against 100 strains of P. aeruginosa. The calculated half-life of amikacin was substantially longer in patients with compromised renal function than in normal subjects. Immaturity of renal function, characteristic of the newborn, similarly slowed the rate of excretion of amikacin. The cure rate (complete clinical remission and eradication of the pathogen) was 91% in 22 patients with urinary tract infection (including 16 with chronic pyelonephritis) treated with 500 mg of amikacin every 8 or 12 hr for eight to 17 days. After single injections of 7.5 mg/kg 2-3 hr before delivery, appreciable amounts of the drug were recovered from the cord blood. No local or systemic intolerance or laboratory abnormalities were observed in a total of 42 patients (including eight infants) treated for a maximum of two weeks. No ototoxicity was demonstrable in any of the 12 patients subjected to audiometry; nystagmography revealed slight vestibular dysfunction in two elderly patients.
根据耐药、中度敏感和敏感菌株的比例,阿米卡星对泌尿系统病原菌临床分离株的活性由高到低依次为沙门氏菌、克雷伯菌、肠杆菌、大肠杆菌、金黄色葡萄球菌、柠檬酸杆菌、变形杆菌属和铜绿假单胞菌。然而,在针对100株铜绿假单胞菌进行测试的抗生素(包括庆大霉素和妥布霉素)中,阿米卡星的活性最高。肾功能受损患者体内阿米卡星的计算半衰期明显长于正常受试者。新生儿特有的肾功能不成熟同样减缓了阿米卡星的排泄速度。在22例尿路感染患者(包括16例慢性肾盂肾炎患者)中,每8或12小时给予500毫克阿米卡星,持续8至17天,治愈率(临床完全缓解并清除病原体)为91%。在分娩前2至3小时单次注射7.5毫克/千克后,脐血中可检测到相当数量的药物。在总共42例患者(包括8例婴儿)中,最长治疗两周,未观察到局部或全身不耐受或实验室异常情况。在接受听力测试的12例患者中,未发现任何耳毒性;眼震图显示两名老年患者有轻微前庭功能障碍。