The quinolones: decades of development and use

The quinolones: decades of development and use
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DOI:
10.1093/jac/dkg208
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发表时间:
2003-05-01
影响因子:
5.2
通讯作者:
Jones, AM
Jones, AM
中科院分区:
医学2区
文献类型:
--
作者:
Emmerson, AM;Jones, AM

文献摘要

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1962年发现萘啶酸,并于1967年将其引入临床使用,标志着喹诺酮开发和使用五十年的开始。直到20世纪70年代和80年代氟喹诺酮类药物的发现和许可,这些药物才开始在临床有用的抗菌药物中建立自己的位置。在世纪初,在它们发现和使用的第五个十年中,我们对结构-功能关系的理解有所提高,并且在抗菌覆盖谱和药代动力学方面开发了更好的化合物。在不断变化的治疗环境中,需要不断监测这类不断扩大的抗菌药物的临床效用以及对“更新”氟喹诺酮类药物产生耐药性的较低倾向。在耐药性增加的情况下,抗生素药物的选择仍然很困难,但新的氟喹诺酮类药物的引入开创了抗菌治疗的新时代。这些药物的作用已经在一些临床指南中得到认可,适当使用这些药物可能有助于保持其临床效用,使其能够充分发挥其治疗潜力。
The discovery of nalidixic acid in 1962, and its introduction for clinical use in 1967, marks the beginning of five decades of quinolone development and use. It was not until the discovery and licensing of the fluoroquinolones in the 1970s and 1980s that these drugs began to establish their place in the armamentarium of clinically useful antimicrobials. At the beginning of the 21st century, in their fifth decade of discovery and use, our understanding of structure-function relationships has improved, and better compounds, in terms of both spectrum of antimicrobial cover and pharmacokinetics, have been developed. The clinical utility of this expanding class of antimicrobial agents, and the lower propensity for the development of resistance with the 'newer' fluoroquinolones will need to be continually monitored in the changing therapeutic environment. Antibiotic drug choice will remain difficult in the presence of increasing resistance, but the introduction of the new fluoroquinolones has created a new and exciting era in antimicrobial treatment. The role of these agents has already been acknowledged in a number of clinical guidelines, and appropriate use of these agents may help to preserve their clinical utility, enabling them to realize their full therapeutic potential.