| Description | Amikacin disulfate (BAY-416651 sulfate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A. |
| In vitro | Amikacin disulfate对细菌30S核糖体的16S rRNA具有高亲和力,导致mRNA读码错误,使得细菌无法合成对其生长至关重要的蛋白质。[1] Amikacin在体外对铜绿假单胞菌属、[2]大肠杆菌[3]、产碱克雷伯菌属(吲哚阳性及吲哚阴性)、普罗维登斯菌属、克雷伯-肠杆菌-沙雷菌群、鲍曼不动杆菌(以前称为Mima-Herellea)种和柠檬酸克雷伯菌[4] [5]具有活性。体外研究显示,Amikacin disulfate与β-内酰胺类抗生素(包括莫西拉克坦或哌拉西林)联用,对许多临床重要的革兰阴性菌有协同作用。[6] |
| In vivo | Amikacin(80 mg/kg 静脉注射)在实验性兔子心内膜炎模型中显著降低了主动脉瓣膜内假单胞菌密度,与对照组相比有显著差异。此外,每天一次给药的Amikacin比每天两次给药方案更为有效。[7] 单独使用Amikacin,剂量为50 mg/kg,无论是分一次、两次还是三次给药,均在米氏分枝杆菌复合体感染的米色小鼠模型中显示出显著疗效。加入克洛法西明可以显著增加其活性。[8] |
| Synonyms | 硫酸阿米卡星, Pierami, 阿米卡星硫酸盐, BAY-416651 sulfate, BB-K8, Amikacin sulfate |
| molecular weight | 781.76 |
| Molecular formula | C22H43N5O13·2H2O4S |
| CAS | 39831-55-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 10 mM DMSO: Insoluble |
| References | 1. Umezawa H. Jpn J Antibiot, 1979, 32 Suppl, S1-S14. 2. Kluge RM, et al. Antimicrob Agents Chemother, 1974, 6(4), 442-446. 3. Price KE, et al. Antimicrob Agents Chemother, 1974, 5(2), 143-152. 4. Sharp PM, et al. Antimicrob Agents Chemother, 1974, 5(5), 435-438. 5. Falagas ME, et al. Expert Rev Anti Infect Ther, 2012, 10(2), 207-218. |