Klastersky J, Odio W, Hensgens C
Clin Pharmacol Ther. 1975 Mar;17(3):348-54. doi: 10.1002/cpt1975173348.
The sensitivity to gentamicin (G) and to amikacin (A) of 25 strains of Escherichia coli (EC), 25 Klebsiella sp. (K), 25 Proteus and Providence sp. (PP), and 25 Ps. aeruginosa (PA) were tested in vitro by the disc method, by the inocula-replicating method, and by a tube dilution technique using 10-5 microorganisms/ml. Bactericidal concentrations active on 50% and 90% of the strains were 1.5 and 4.5 mug/ml for EC, 3 and mug/ml for K, 1.5 and 3 mug/ml for PP, and 3 and 3 mug/ml for PA. Resistance to killing by 12 mug/ml of G was found for 16 strains (1 EC, 9 K, 4 PP, and 2 PA) but only 5 strains were also resistant to 12 mug/ml of A. Conversely, 4 strains (1 EC, 1 PP, and 2 PA) were resistant to 12 mug/ml of A but were killed by 6 mug/ml of G or even less. G (1.5 MG/KG) AND A (5 mg/kg) were administered to 5 bolunteers in a crossover fashion. The mean bactericidal activity of the sera obtained at 1 hr after the injection of G and A was, respectively, 1/4 and 1/4 for ED, 1/4 and 1/8 for K, 1/2 and 1/2 for PP, and 1/2 and 1/2 for PA. Sera obtained in A-treated patients killed at a dilution of 1/8, 8 strains of ED, 17 K, 1 PP, and O PA; at that dilution sera from G-treated patients killed 5 ED, 9 K, O P, and O PA. The main advantage of A over G might be the absence of cross-resistance between A and G for particular pathogens.
采用纸片法、接种物复制法以及使用每毫升含10⁻⁵个微生物的试管稀释技术,对25株大肠杆菌(EC)、25株克雷伯菌属(K)、25株变形杆菌和普罗威登斯菌属(PP)以及25株铜绿假单胞菌(PA)进行庆大霉素(G)和阿米卡星(A)的体外敏感性测试。对50%和90%菌株有活性的杀菌浓度,对于大肠杆菌分别为1.5和4.5微克/毫升,对于克雷伯菌属为3和未知微克/毫升,对于变形杆菌和普罗威登斯菌属为1.5和3微克/毫升,对于铜绿假单胞菌为3和3微克/毫升。发现16株菌株(1株大肠杆菌、9株克雷伯菌属、4株变形杆菌和普罗威登斯菌属以及2株铜绿假单胞菌)对12微克/毫升的庆大霉素有耐药性,但只有5株菌株对12微克/毫升的阿米卡星也耐药。相反,4株菌株(1株大肠杆菌、1株变形杆菌和普罗威登斯菌属以及2株铜绿假单胞菌)对12微克/毫升的阿米卡星耐药,但被6微克/毫升甚至更低浓度的庆大霉素杀死。以交叉方式给5名志愿者分别注射庆大霉素(1.5毫克/千克)和阿米卡星(5毫克/千克)。注射庆大霉素和阿米卡星后1小时获得的血清的平均杀菌活性,对于大肠杆菌分别为1/4和1/4,对于克雷伯菌属为1/4和1/8,对于变形杆菌和普罗威登斯菌属为1/2和1/2,对于铜绿假单胞菌为1/2和1/2。在接受阿米卡星治疗的患者中获得的血清在1/8稀释度时杀死了8株大肠杆菌、17株克雷伯菌属、1株变形杆菌和普罗威登斯菌属以及0株铜绿假单胞菌;在该稀释度时,来自接受庆大霉素治疗患者的血清杀死了5株大肠杆菌、9株克雷伯菌属、0株变形杆菌和0株铜绿假单胞菌。与庆大霉素相比,阿米卡星的主要优势可能在于对于特定病原体,它与庆大霉素之间不存在交叉耐药性。