Fluoroquinolones: Blessings Or Curses

莫西沙星 左氧氟沙星 医学 司帕沙星 加替沙星 喹诺酮类 诺氟沙星 环丙沙星 抗生素 氧氟沙星 DNA旋转酶 萘啶酸 药理学 重症监护医学 微生物学 生物 生物化学 大肠杆菌 基因
作者
Priyanka Majalekar,Pramodkumar J. Shirote
出处
期刊:Current Drug Targets [Bentham Science Publishers]
卷期号:21 (13): 1354-1370 被引量:88
标识
DOI:10.2174/1389450121666200621193355
摘要

Fluoroquinolones are one of the world's most valuable and popularly used categories of antimicrobial agents. This paper attempts to review the substantial progress of fluoroquinolones from their discovery to black box warning. Antibiotic drug choice will remain difficult in the presence of increasing resistance, but the introduction of fluoroquinolones has created a new and exciting era in antimicrobial treatment. These are a synthetic heterogeneous group of compounds used in both hospital and community practices to treat numerous severe infections. The era of quinolone antibiotics began with the serendipitous discovery of the quinolone prototype in 1962. The chronological development of fluoroquinolone reported that nalidixic acid was the first quinolone that gained popular choice for the treatment of urinary tract infection. The subsequent agents like levofloxacin, ofloxacin, norfloxacin, gatifloxacin, moxifloxacin, clinafloxacin, sparfloxacin, and ciprofloxacin were derived through side chain and nuclear manipulation from basic pharmacophore. The fluoroquinolone motifs have been found as a milestone, effective in certain infections that are respiratory tract infection, urinary tract infection, bone disorders, meningococcal and mycobacterial infections, sexually transmitted diseases, skin infections, etc. Fluoroquinolones are first entirely man-made antibiotics that exhibit antibacterial activity through the inhibition of topoisomerase II, topoisomerase IV and deoxyribonucleic acid gyrase, which is vital for chromosome replication and function. The post-marketing surveillance pointed out the favorable side effects associated with fluoroquinolones such as phototoxicity, QT interval prolongation and anaphylaxis. The discovery, development and clinical use of fluoroquinolone antibiotics in the last century contributed to a decline in morbidity and mortality rates.
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