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氟喹诺酮类抗菌药:结构、抗菌活性、药代动力学、在家畜中的临床应用及毒性

The fluoroquinolone antimicrobials: structure, antimicrobial activity, pharmacokinetics, clinical use in domestic animals and toxicity.

作者信息

Vancutsem P M, Babish J G, Schwark W S

机构信息

Department of Pharmacology, Cornell University, NYSCVM, Ithaca 14853.

出版信息

Cornell Vet. 1990 Apr;80(2):173-86.

PMID:2180631
Abstract

Fluoroquinolones form a promising family of new bactericidal antimicrobials. Enrofloxacin (Baytril) is the first antibacterial of this family to be available to veterinary medicine. They share a wide spectrum of antimicrobial activity, a large volume of distribution and are active at very low concentrations. Their target site for bactericidal action is the type II topoisomerase (E.C. 5.99.1.3.). The gastrointestinal absorption in mammals is rapid and substantial, the duration of action is long and the excretion mainly through the kidney. Their adverse effects are not severe when compared to the beneficial features fluoroquinolones exhibit. The target tissues for adverse effects are: the juvenile cartilage, central nervous system, urinary tract and digestive tract. In the USA, approved use is thus far limited to dogs; approval for use in food-animals is currently being sought for several fluoroquinolones. Published clinical trials as well as unpublished data from the author's laboratories are reviewed for dogs, cats, pigs, cattle and poultry.

摘要

氟喹诺酮类药物构成了一类很有前景的新型杀菌抗菌药物。恩诺沙星(拜有利)是该类药物中首个应用于兽医学的抗菌药。它们具有广泛的抗菌活性谱、分布容积大且在极低浓度下仍有活性。其杀菌作用的靶点是Ⅱ型拓扑异构酶(E.C. 5.99.1.3.)。在哺乳动物中,它们的胃肠道吸收迅速且充分,作用持续时间长,主要通过肾脏排泄。与氟喹诺酮类药物所展现的有益特性相比,其不良反应并不严重。不良反应的靶组织包括:幼年软骨、中枢神经系统、泌尿道和消化道。在美国,目前批准的使用范围仅限于犬类;目前正在为几种氟喹诺酮类药物寻求在食用动物中的使用批准。本文对已发表的临床试验以及作者实验室未发表的数据进行了综述,涉及犬、猫、猪、牛和家禽。

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