The New Fluoroquinolones: A Critical Review

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Zhanel, George G
Walkty, Andrew
Vercaigne, Lavern
Karlowsky, James A
Embil, John
Gin, Alfred S
Hoban, Daryl J
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OBJECTIVE: This paper reviews the literature available on the new fluoroquinolones – clinafloxacin, gatifloxacin, grepafloxacin, levofloxacin, moxifloxacin, sparfloxacin and trovafloxacin – to compare these agents with each other and contrast them with ciprofloxacin, an older fluoroquinolone.DATA SELECTION: Published papers used were obtained by searching MEDLINE for articles published between 1994 and 1998, inclusive. References of published papers were also obtained and reviewed. Abstracts from scientific proceedings were reviewed.DATA EXTRACTION: Due to the limited data available on several of the agents, criteria for study inclusion in the in vitro, pharmacokinetics and in vivo sections were not restrictive.DATA SYNTHESIS: The new fluoroquinolones offer excellent Gram-negative bacillary activity and improved Gram-positive activity (eg, against Streptococcus pneumoniae and Staphylococcus aureus) over ciprofloxacin. Clinafloxacin, gatifloxacin, moxifloxacin, sparfloxacin and trovafloxacin display improved activity against anaerobes (eg, Bacteriodes fragilis). All of the new fluoroquinolones have a longer serum half-life than ciprofloxacin (allowing for once daily dosing), and several are eliminated predominantly by nonrenal means. No clinical trials are available comparing the new fluoroquinolones with each other. Clinical trials comparing the new fluoroquinolones with standard therapy have demonstrated good efficacy in a variety of infections. Their adverse effect profile is similar to that of ciprofloxacin. Clinafloxacin and sparfloxacin cause a high incidence of phototoxicity (1.5% to 14% and 2% to 11.7%, respectively), grepafloxacin causes a high incidence of taste perversion (9% to 17%) and trovafloxacin causes a high incidence of dizziness (11%). They all interact with metal ion-containing drugs (eg, antacids), and clinafloxacin and grepafloxacin interact with theophylline. The new fluoroquinolones are expensive; however, their use may result in savings in situations where, because of their potent and broad spectrum of activity, they can be used orally in place of intravenous antibiotics.CONCLUSIONS: The new fluoroquinolones offer advantages over ciprofloxacin in terms of improved in vitro activity and pharmacokinetics. Whether these advantages translate into improved clinical outcomes is presently unknown. The new fluoroquinolones have the potential to emerge as important therapeutic agents in the treatment of respiratory tract and genitourinary tract infections.
George G Zhanel, Andrew Walkty, Lavern Vercaigne, et al., “The New Fluoroquinolones: A Critical Review,” Canadian Journal of Infectious Diseases, vol. 10, no. 3, pp. 207-238, 1999. doi:10.1155/1999/378394