Martinez Marilyn, McDermott Patrick, Walker Robert
US Food and Drug Administration, Center for Veterinary Medicine, Office of New Animal Drug Evaluation, Rockville, MD 20855, USA.
Vet J. 2006 Jul;172(1):10-28. doi: 10.1016/j.tvjl.2005.07.010. Epub 2005 Sep 9.
The fluoroquinolones are a class of compounds that comprise a large and expanding group of synthetic antimicrobial agents. Structurally, all fluoroquinolones contain a fluorine molecule at the 6-position of the basic quinolone nucleus. Despite the basic similarity in the core structure of these molecules, their physicochemical properties, pharmacokinetic characteristics and microbial activities can vary markedly across compounds. The first of the fluoroquinolones approved for use in animals, enrofloxacin, was approved in the late 1980s. Since then, five other fluoroquinolones have been marketed for use in animals in the United States, with others currently under investigation. This review focuses on the use of fluoroquinolones within veterinary medicine, providing an overview of the structure-activity relationship of the various members of the group, the clinical uses of fluoroquinolones in veterinary medicine, their pharmacokinetics and potential interspecies differences, an overview of the current understanding of the pharmacokinetic/pharmacodynamic relationships associated with fluoroquinolones, a summary of toxicities that have been associated with this class of compounds, their use in both in human and veterinary species, mechanisms associated with the development of microbial resistance to the fluoroquinolones, and a discussion of fluoroquinolone dose optimization. Although the review contains a large body of basic research information, it is intended that the contents of this review have relevance to both the research scientist and the veterinary medical practitioner.
氟喹诺酮类是一类化合物,由大量且不断扩大的合成抗菌剂组成。从结构上看,所有氟喹诺酮类在基本喹诺酮核的6位都含有一个氟分子。尽管这些分子的核心结构基本相似,但它们的物理化学性质、药代动力学特征和微生物活性在不同化合物之间可能有显著差异。第一种被批准用于动物的氟喹诺酮类药物恩诺沙星于20世纪80年代末获批。从那时起,另外五种氟喹诺酮类药物已在美国上市用于动物,还有其他一些药物目前正在研究中。本综述重点关注氟喹诺酮类在兽医学中的应用,概述该类不同成员的构效关系、氟喹诺酮类在兽医学中的临床应用、它们的药代动力学及潜在的种间差异、对目前与氟喹诺酮类相关的药代动力学/药效学关系的理解概述、与这类化合物相关的毒性总结、它们在人类和兽类物种中的使用情况、微生物对氟喹诺酮类产生耐药性的相关机制,以及对氟喹诺酮类剂量优化的讨论。尽管本综述包含大量基础研究信息,但旨在使其内容对科研人员和兽医从业者都具有相关性。