JAC Advance Access published online on November 12, 2003
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkh001
© 2003 by The British Society for Antimicrobial Chemotherapy
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Original article
1 First Department of Internal Medicine, Faculty of Medicine,
University of the Ryukyus, 207 Uehara,
Nishihara, Okinawa 903-0215, Japan
* Corresponding author. E-mail: fhiga{at}med.u-ryukyu.ac.jp.
Received 6 May 2003
; revised 24 September 2003
; accepted 1 October 2003
The activity of the fluoroquinolone olamufloxacin (HSR-903)
against Legionella spp. was studied in
vitro and in vivo. The olamufloxacin MIC at
which 50% of isolates are inhibited (MIC50)
for 81 different Legionella spp. strains (59 type
strains and 22 clinical isolates) was 0.008 mg/L, which was identical
to sparfloxacin, whereas the MIC50s for erythromycin,
levofloxacin and ciprofloxacin were 0.25, 0.032 and 0.032 mg/L,
respectively. Olamufloxacin and sparfloxacin (at 0.008 mg/L) inhibited
intracellular growth and subsequent cytotoxicity of L.
pneumophila 80-045 in J774.1 macrophages, whereas levofloxacin
and ciprofloxacin did not, at the same concentration. When olamufloxacin
was given to the infected guinea pigs orally (5 mg/kg of body weight), peak
levels in the lung were 3.02 mg/kg at 2 h post-administration, with
a half-life of 3.41 h and an AUC0-12 of 12.31
mg·h/kg. The 2 day post-infection bacterial burden of the
lung in the animals treated with olamufloxacin (5 and 1.25 mg/kg
given orally twice a day) was much lower than in those treated with
levofloxacin (same dose as olamufloxacin) or erythromycin (10 mg/kg
given orally twice a day). When treated with olamufloxacin (5 mg/kg
given orally twice a day) for 7 days, 11 of 12 L. pneumophila-infected
guinea pigs survived for 14 days post-infection, as did all 12 guinea
pigs treated with levofloxacin (5 mg/kg given orally twice a day)
for 7 days. In contrast, only two of 12 animals treated with erythromycin
survived and 10 of 11 died in the physiological saline group. Olamufloxacin
was as effective as levofloxacin in a guinea pig model of Legionnaires’ disease.
These data warrant further study of whether olamufloxacin is an
option for the treatment of Legionella infections.
Keywords: fluoroquinolones, Legionnaires’ disease, Legionella pneumophila
In vitro and in vivo activity
of olamufloxacin (HSR-903) against Legionella spp
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