The quinolones: decades of development and use

Abstract

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.

Detection of plasmid-mediated qnr genes among the quinolone-resistant Escherichia coli isolates in Iran

“…In this study, the resistance rates to nalidixic acid and ciprofloxacin were 82.8% and 45%, respectively, indicating a high rate of resistance to quinolone and fluoroquinolone by E. coli isolates associated with UTIs in Khorram Abad. Since the development of nalidixic acid in 1962, the drug has been used for the treatment of UTIs for more than five decades [17]. The resistance rate for nalidixic acid, therefore, is expected to be higher than for fluoroquinolones.…”

Parallel evolution and local differentiation in quinolone resistance in Pseudomonas aeruginosa

“…Quinolone antibiotics constitute a widely used class of broad spectrum antibiotics first discovered in 1962 and introduced for clinical use in 1967 as a treatment for urinary tract infections caused by enterococcal bacteria (Emmerson & Jones, 2003). Following the introduction of the first quinolone antibiotic, nalidixic acid, subsequent work led to the development of fluoroquinolones (e.g.…”

Fluoroquinolone residues in raw cow's milk

“…Compared with the classic 1 st generation quinolones that were characterised by a narrow spectrum of action and poor tissue penetration ability, fluoroquinolones feature many attributes of ideal antimicrobials (Sarkőzy 2001;Emmerson & Jones 2003). Fluoroquinolones are used for the treatment of infections caused by various bacterial agents in both human and veterinary medicine.…”