JAC Advance Access published online on January 28, 2003
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkg110
© 2003 by The British Society for Antimicrobial Chemotherapy
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Original article
1 Department of Medical
Microbiology, City Hospital NHS Trust, Birmingham
* Corresponding author. E-mail: jenny.Andrews{at}cityhospbham.wmids.nhs.uk.
Received 27 August 2002
; revised 7 November 2002
; accepted 3 December 2002
A microbiological assay was used to measure concentrations
of garenoxacin (BMS-284756) in plasma, bronchial mucosa
(BM), alveolar macrophages (AM) and epithelial lining fluid (ELF), following
a single 600 mg oral dose. Twenty-four healthy subjects were allocated
into four nominal time intervals after the dose, 2.5-3.5,
4.5-5.5, 10.5-11.5 and 23.5-24.5 h. Mean
concentrations in plasma, BM, AM and ELF, respectively, for the
four nominal time windows were for 2.5-3.5
h 10.0 mg/L (S.D. 2.8), 7.0 mg/kg (S.D. 1.3),
106.1 mg/L (S.D. 60.3) and 9.2 mg/L (S.D. 3.6); 4.5-5.5
h 8.7 mg/L (S.D. 2.2), 6.0 mg/kg (S.D. 1.9),
158.6 mg/L (S.D. 137.4) and 14.3 mg/L (S.D. 8.2); 10.5-11.5
h 6.1 mg/L (S.D. 1.9), 4.0 mg/kg (S.D. 1.4),
76.0 mg/L (S.D. 47.7) and 7.9 mg/L (S.D. 4.6);
and 23.5-24.5 h 2.1 mg/L (S.D. 0.5), 1.7
mg/kg (S.D. 0.7), 30.7 mg/L (S.D. 12.9)
and 3.3 mg/L (S.D. 2.3). Concentrations at all
sites exceeded MIC90s for the common respiratory pathogens Haemophilus influenzae (0.03 mg/L), Moraxella
catarrhalis (0.015 mg/L) and Streptococcus pneumoniae (0.06
mg/L). These data suggest that garenoxacin should be effective in
the treatment of community-acquired pneumonia and chronic obstructive
pulmonary disease.
Keywords: garenoxacin, concentrations, respiratory tree
Concentrations of garenoxacin in plasma, bronchial
mucosa, alveolar macrophages and epithelial lining fluid following
a single oral 600 mg dose in healthy adult subjects
2 Department of Respiratory Medicine,
Heartlands NHS Trust, Birmingham
3 Hammersmith Medicines Research Ltd, Central Middlesex Hospital,
London, UK
4 Bristol-Myers
Squibb, USA
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