This therapeutic review discusses the pharmacology, pharmacokinetics, in vi
tro activity, drug interactions, and adverse effects of levofloxacin, a flu
oroquinolone antibiotic. Particular emphasis is placed on the clinical effi
cacy of levofloxacin and its place in therapy. Compared with ciprofloxacin
and the earlier quinolone agents, levofloxacin has an improved pharmacokine
tic profile that allows convenient once-daily dosing in either an oral or p
arenteral formulation. Levofloxacin has enhanced activity against gram-posi
tive aerobic organisms, including penicillin-resistant pneumococci. In publ
ished comparative trials involving commonly used treatment regimens, levofl
oxacin had equivalent if not greater activity in the treatment of community
-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, a
cute bacterial sinusitis, acute pyelonephritis, and complicated urinary tra
ct infection. Levofloxacin is well tolerated and induces minimal adverse dr
ug reactions. Based on the above attributes, it may be reasonable to includ
e levofloxacin on the hospital formulary in place of older quinolones. More
recently released quinolones such as trovafloxacin exhibit similar advanta
ges; however, until direct comparative trials between levofloxacin and thes
e newer agents are conducted, it is difficult to advocate one agent over an
other. Regardless of which quinolone is the primary agent on the formulary,
it is imperative that this class of antimicrobial drugs be used with discr
etion to minimize the development of resistance.