Amikacin disulfate

Amikacin is an aminoglycoside antibiotic^[1]. Amikacin is used to treat a variety of infections caused by Gram-negative bacteria^[2]. Amikacin can enter bacterial cells and bind to their ribosomes. By interfering with bacterial protein synthesis, it prevents normal bacterial growth and reproduction, thereby exerting its antibacterial effects ^[3]. Amikacin is widely used in the treatment of complex urinary tract infections, respiratory infections, and sepsis^[4].

In vitro, Amikacin (0.003 - 25mg/mL) treatment of equine joint cells (including chondrocytes, synovial cells, adipose-derived and bone marrow-derived mesenchymal stem cells) induces rapid cell death within 1 hour in a dose-dependent manner. Moreover, the cytotoxicity of Amikacin is not mitigated by the presence of synovial fluid^[5]. Amikacin (32mg/L) alone or in combination with 2mg/L Colistin can effectively kill bacteria within biofilms of mature Pseudomonas aeruginosa (PAO1 and CRPAO1) treatment for 24 hours^[6].

In vivo, Amikacin (15mg/kg) combined with Imipenem (40mg/kg) administered intraperitoneally every 8 hours is used to treat mice infected with drug-resistant Escherichia coli. The combination of Amikacin and Imipenem significantly reduces the bacterial count in the blood of mice^[7]. Amikacin (7.5mg/kg; every 12 hours) combined with Meropenem (200mg/kg; every 8 hours) administered intraperitoneally to mice infected with carbapenem-resistant Enterobacteriaceae (CRE). Compared to Meropenem monotherapy, the combination therapy significantly reduces bacterial density in the thigh muscles of mice and increases survival rates^[8].

References:
[1] Ramirez MS, Tolmasky ME. Amikacin: Uses, Resistance, and Prospects for Inhibition. Molecules. 2017 Dec 19;22(12):2267.
[2] Meyer RD. Amikacin. Ann Intern Med. 1981 Sep;95(3):328-32.
[3] Jenkins A, Thomson AH, Brown NM, et al. Amikacin use and therapeutic drug monitoring in adults: do dose regimens and drug exposures affect either outcome or adverse events? A systematic review. J Antimicrob Chemother. 2016 Oct;71(10):2754-9.
[4] Kato H, Hamada Y. Amikacin Therapy in Japanese Pediatric Patients: Narrative Review. Int J Environ Res Public Health. 2022 Feb 10;19(4):1972.
[5] Pezzanite L, Chow L, Soontararak S, et al. Amikacin induces rapid dose-dependent apoptotic cell death in equine chondrocytes and synovial cells in vitro. Equine Vet J. 2020 Sep;52(5):715-724.
[6] Wang Y, Li C, Wang J, et al. The Efficacy of Colistin Combined with Amikacin or Levofloxacin against Pseudomonas aeruginosa Biofilm Infection. Microbiol Spectr. 2022 Oct 26;10(5):e0146822.
[7] Farhan SM, El-Baky RMA, Abdalla S, et al. In Vitro and In Vivo Effect of Amikacin and Imipenem Combinations against Multidrug-Resistant E. coli. Trop Med Infect Dis. 2022 Oct 2;7(10):281.
[8] Hagihara M, Kato H, Yamashita R, et al. In vivo study assessed meropenem and amikacin combination therapy against carbapenem-resistant and carbapenemase-producing Enterobacteriaceae strains. J Infect Chemother. 2020 Jan;26(1):1-7.

Amikacin是一种氨基糖苷类抗生素^[1]。Amikacin被应用于治疗多种由革兰氏阴性菌引起的感染^[2]。Amikacin能够进入细菌细胞内，与细菌的核糖体结合。通过干扰细菌的蛋白质合成过程，阻止细菌正常生长和繁殖，从而发挥抗菌作用^[3]。Amikacin常被用于治疗复杂性尿路感染、呼吸道感染以及败血症等疾病^[4]。

在体外，Amikacin（0.003 - 25mg/mL）处理马的关节细胞（包括软骨细胞、滑膜细胞、脂肪源性和骨髓源性间充质干细胞）1小时内，Amikacin快速诱导细胞死亡，且这种细胞毒性作用以Amikacin剂量依赖的方式发生。此外，Amikacin的细胞毒性作用不会因滑膜液的存在而减轻^[5]。Amikacin（32mg/L）单独或与2mg/L的Colistin联合处理铜绿假单胞菌（PAO1和CRPAO1）生物膜24小时，能够有效杀灭生物膜内的细菌^[6]。

在体内，Amikacin（15mg/kg）联合Imipenem（40mg/kg）每8小时腹腔注射一次，用于处理感染耐药大肠杆菌的小鼠。Amikacin联合Imipenem显著减少了小鼠血液中的细菌数量^[7]。Amikacin（7.5mg/kg；每12小时一次）联合Meropenem（200mg/kg；每8小时一次）腹腔注射处理感染了碳青霉烯类耐药肠杆菌科细菌（CRE）的小鼠。与单独使用Meropenem相比，联合治疗显著降低了小鼠大腿肌肉中的细菌密度，并提高了生存率^[8]。