氨基糖苷类药物临床应用再评价  

Re-evaluation of Aminoglycoside Drugs in Clinical Practice

作　　者：邓万俊[1] 

机构地区：[1]南华大学附属南华医院心内科,衡阳421002

出　　处：《国外医药（抗生素分册）》2010年第5期219-223,共5页World Notes on Antibiotics

摘　　要：氨基糖苷类药物属古老抗生素之一,它们通过与细菌30S核糖体亚单位的16S核糖体RNA(rRNA)的氨酰基位置结合,直接干扰细菌蛋白合成而发挥广谱抗菌活性,但对厌氧菌无效。氨基糖苷类具有明显的抗生素后效应。由于用药后尿中浓度是血清浓度的25～100倍,99%在尿中以原形排泄,因此氨基糖苷类是治疗泌尿道感染的强有力药物。对泌尿道感染之外的其它部位革兰阴性菌脓毒血症,单用氨基糖苷类的疗效逊于β-内酰胺类。虽然许多研究者建议氨基糖苷类应与其它类型的抗生素联合应用,但临床试验并未证实氨基糖苷类与β-内酰胺类联合应用的疗效超过β-内酰胺类单药治疗。氨基糖苷类主要不良反应是剂量依赖性肾毒性及耳毒性。延长用药间隔,即每日1次给药对减少肾毒性的发生起重要作用。其耳毒性与遗传因素有关,某些患者耳聋是m.1555A>G基因变异所致。这一研究思路有望对预防耳毒性找到新方法。Aminoglycosides are one of the old classes of antimicrobials. They exhibit antimicrobial activity against a wide spectrum by binding to the aminoacyl site of 16S ribosomal RNA （rRNA） within the 30S ribosomal subunit. They display no activity against anaerobes. They have been shown to possess a significant post-antibiotic effect. Aminoglycosides reach concentrations in the urine 25-100-fold that of serum. Approximately 99% of the administered dose is eliminated unchanged in the urine, therefore, single treatment with an aminoglycoside is a very potent tool in the treatment of urinary tract infections. Single treatment with an aminoglycoside is less effective than β-lactam treatment in septic patients with Gram-negative infections from sites other than the urinary tract. Many authors recommend that aminoglycoside antibiotics should be administered in combination with other antimicrobial agents, but clinical trials attempting to compare the efficacy of β-lactam/aminoglycoside combination treatments with that of β-lactam monotherapy have failed to confirm its value. The major adverse effects of aminoglycosides are dose dependent nephrotoxicity and ototoxicity. Infrequent administration of doses （i.e., intervals of 24 h） plays a central role in minimizing the likelihood of toxicity. Ototoxicity could be associated with genetic factors .In some populations, the m.1555A〉G mutation seems to be a common cause of deafness. Novel research pathways that could lead to the development of methods that will overcome ototoxicity.

关 键 词：氨基糖苷类 肾毒性 耳毒性 

分 类 号：R978.12[医药卫生—药品]