Aminoglycosides
Aminoglycosides
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DOI：
10.1007/978-1-4614-1400-1_7
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发表时间：
2012-01-01
期刊：
影响因子：
--
通讯作者：
Miller, George H.
中科院分区：
文献类型：
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作者：
Armstrong, Eliana S.;Kostrub, Corwin F.;Miller, George H.
氨基糖苷类始于天然产物的发现，它彻底改变了结核病和其他严重感染的治疗。氨基糖苷具有广谱的活性、广泛的应用于许多适应症、快速的杀菌性、有价值的溶解度、稳定性和药代动力学特性，这使得氨基糖苷成为临床常用的一类药物，尽管对肾毒性和耳毒性的担忧限制了该类药物的使用。通过全球研究人员的勤奋努力，半合成衍生物随后被确定，扩大了用途，并避免了抗性机制，这些机制已经开始侵蚀其前身的功效。随着对氨基糖苷的药代动力学和药效学的理解的发展，出现了指导原则，允许以最大化功效同时最小化毒性的方式最佳使用氨基糖苷。这些方面将在本章中描述，以及对新出现的耐药病原体的潜在活性，这些病原体激发了氨基糖苷类的持续创新。
The aminoglycoside class began with the discovery of natural products that revolutionized the treatment of tuberculosis and other serious infections. Their broad spectrum of activity, broad utility across many indications, rapid bactericidality, and valuable solubility, stability, and pharmacokinetic properties made aminoglycosides a popular and clinically useful class of drugs, though concerns about nephrotoxicity and ototoxicity have limited the usage of older members of the class. Through the diligent efforts of researchers worldwide, semisynthetic derivatives were subsequently identified that broadened the utility and evaded the resistance mechanisms that had begun to erode the efficacy of their predecessors. As the understanding of the pharmacokinetics and pharmacodynamics of the aminoglycosides has developed, guiding principles have emerged that allow for the optimal use of aminoglycosides in ways that maximize efficacy while minimizing toxicity. These aspects will be described in this chapter along with the potential for activity against emerging resistant pathogens which motivate continued innovation in the aminoglycoside class.