Ristuccia A M, Cunha B A
Ther Drug Monit. 1985;7(1):12-25. doi: 10.1097/00007691-198503000-00003.
Amikacin, a semisynthetic analog of kanamycin, is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. The effectiveness of amikacin in the treatment of serious gram-negative bacillary infections is well documented. Due to its resistance to inactivating enzymes, it is the aminoglycoside of choice for the treatment of known or suspected serious gram-negative infections caused by organisms resistant to gentamicin or tobramycin. Amikacin should be part of an empiric antibiotic regimen for the therapy of suspected sepsis in febrile, leukopenic immunocompromised hosts since it exhibits enhanced activity against the organisms most frequently encountered in this patient population. High response rates have been reported with the use of amikacin combined with beta-lactam antibiotics in immunocompromised or granulocytopenic patients. It exhibits impressive in vitro synergy against aminoglycoside-sensitive and -resistant organisms when used in combination with the new acylureidopenicillins and third-generation cephalosporins. Amikacin has the advantage of being the aminoglycoside least inactivated by the semisynthetic penicillins. Amikacin achieves high and predictable serum concentrations and has a favorable therapeutic index. Its potential for nephrotoxicity and ototoxicity is not significantly different than that encountered with gentamicin or tobramycin. Amikacin appears to be the preferred aminoglycoside for use at the present time because of its activity against gentamicin- and tobramycin-resistant organisms, its low resistance potential, its relative low degree of inactivation by the semisynthetic penicillins, and its superior pharmacokinetic profile.
阿米卡星是卡那霉素的半合成类似物,对大多数革兰氏阴性菌具有很高的活性,包括对庆大霉素和妥布霉素耐药的菌株。阿米卡星治疗严重革兰氏阴性杆菌感染的有效性已有充分记录。由于其对灭活酶具有抗性,它是治疗由对庆大霉素或妥布霉素耐药的生物体引起的已知或疑似严重革兰氏阴性感染的首选氨基糖苷类药物。在发热、白细胞减少的免疫功能低下宿主中怀疑有败血症时,阿米卡星应作为经验性抗生素治疗方案的一部分,因为它对该患者群体中最常见的生物体具有增强的活性。据报道,在免疫功能低下或粒细胞减少的患者中,使用阿米卡星联合β-内酰胺类抗生素有很高的反应率。当与新型酰脲基青霉素和第三代头孢菌素联合使用时,它对氨基糖苷类敏感和耐药的生物体表现出令人印象深刻的体外协同作用。阿米卡星的优点是它是半合成青霉素灭活最少的氨基糖苷类药物。阿米卡星能达到高且可预测的血清浓度,并有良好的治疗指数。其肾毒性和耳毒性的可能性与庆大霉素或妥布霉素相比没有显著差异。由于其对庆大霉素和妥布霉素耐药生物体的活性、低耐药潜力、半合成青霉素对其相对较低的灭活程度以及优越的药代动力学特性,阿米卡星目前似乎是首选的氨基糖苷类药物。