The penetration into sputum of garenoxacin mesilate hydrate(GRNX), a new oral des-fluoroquinolone antibiotic, was evaluated in five patients with secondary infection to chronic respiratory disease. The efficacy and safety of GRNX were evaluated. Concentrations of GRNX in sputum and plasma were measured during 400 mg once a day treatment for 10 days. The concentration reached maximum after 3-5 hours of administration, and the concentration values (average ± SD) of GRNX in sputum after 3 hours and after 24 hours were 3.50 ± 1.17 μg/g and 0.784 ± 0.199 μg/g, respectively. The trough concentration of GRNX in sputum indicated over MIC90 of major causative organisms of respiratory tract infection; i.e., quinolone-susceptive Staphylococcus aureus: 0.025 μg/mL, Streptococcus pneumoniae: 0.05 μg/mL, Haemophilus influenzae: 0.0125 μg/mL and Moraxella catarrhalis: 0.10 μg/mL. For the three cured patients in this study, whose causative organisms were eradicated, the concentration of GRNX in sputum after 24 hours of administration was greater than MIC of pathogens (Streptococcus constellatus, Pseudomonas aeruginosa and H. influenzae). No serious or significant adverse events were observed. The above results suggest that GRNX shows good penetration into sputum and GRNX treatment is useful for patients with secondary infection to chronic respiratory disease.
|Number of pages||7|
|Journal||Japanese Journal of Chemotherapy|
|Issue number||SUPPL. 1|
|Publication status||Published - 2007 Oct 1|
- Drug concentration
ASJC Scopus subject areas
- Pharmacology (medical)