Extensive pharmacologic and clinical development of quinolone antimicrobial
agents has resulted in improved antimicrobial activity, pharmacokinetic fe
atures, toxicity, and drug-drug interaction profiles. Nalidixic acid and ot
her early quinolones had limited use due to poor pharmacokine tics, relativ
ely narrow antimicrobial spectrum of activity, and frequent adverse effects
. Be-ginning with the development of fluoroquinolones, such as norfloxacin
and ciprofloxacin, in the 1980s, the agents assumed a greatly expanded clin
ical role because of their broad antimicrobial spectrum of action, improved
pharmacokinetic properties, and more acceptable safety profile. Although t
he pharmaco kinetics and efficacy of the drugs have improved significantly,
a major area of continued emphasis is to further reduce the frequency and
severity of adverse events and drug-drug interactions. Older agents such as
ciprofloxacin and ofloxacin are still extensively prescribed, but the focu
s of this article is on the newer fluoroquinolones (levofloxacin and other
drugs that have been approved or have been under investigation since approx
imately 1997).