Abstract |
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 MIC(90)s 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.
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Authors | J Andrews, D Honeybourne, G Jevons, M Boyce, R Wise, A Bello, D Gajjar |
Journal | The Journal of antimicrobial chemotherapy
(J Antimicrob Chemother)
Vol. 51
Issue 3
Pg. 727-30
(Mar 2003)
ISSN: 0305-7453 [Print] England |
PMID | 12615879
(Publication Type: Journal Article)
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Chemical References |
- Fluoroquinolones
- Indoles
- Quinolones
- garenoxacin
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Topics |
- Administration, Oral
- Adult
- Bronchi
(drug effects, metabolism)
- Bronchoalveolar Lavage Fluid
- Female
- Fluoroquinolones
- Humans
- Indoles
(administration & dosage, blood, pharmacokinetics)
- Macrophages, Alveolar
(drug effects, metabolism)
- Male
- Quinolones
(administration & dosage, blood, pharmacokinetics)
- Respiratory Mucosa
(drug effects, metabolism)
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