In vitro and in vivo Antibacterial Activities of Telithromycin.

摘要

BACKGROUND: Telithromycin is one of the ketolides, characterised by a 3-keto group instead of L-cladinose and a C(11)-C(12) carbamate link by an alkyl chain to a pyridinum and imidazolium ring side chain. We evaluated in vitro and in vivo antibacterial activities of telithromycin against gynaecological pathogens. METHODS: In the vitro study, the antibacterial activity of telithromycin against 180 isolates (isolated in the year 2000) of STREPTOCOCCUS AGALACTIAE (n = 33), ENTEROCOCCUS FAECALIS (n = 22), NEISSERIA GONORRHOEAE (n = 30), PEPTOSTREPTOCOCCUS ANAEROBIUS (n = 20), FINEGOLDIA MAGNA (n = 20), BACTEROIDES FRAGILIS (n = 25) and PREVOTELLA BIVIA (n = 30) was compared with that of erythromycin A, clarithromycin, azithromycin, ampicillin and levofloxacin. In the in vivo study, the efficacy of telithromycin was evaluated using experimental intra-abdominal abscesses in mice caused by B. FRAGILIS (minimum inhibitory concentration of telithromycin 0.5 mg/l). RESULTS: In the in vitro study, telithromycin inhibited more than 50% of clinical isolates of S. AGALACTIAE, E. FAECALIS, N. GONORRHOEAE, P. ANAEROBIUS, F. MAGNA, B. FRAGILIS and P. BIVIA at concentrations of 0.016, 0.063, 0.063, 0.032, 0.032, 0.5 and 0.25 mg/l, respectively. Telithromycin inhibited more than 90% of these clinical isolates at concentrations of 0.016, 4, 0.125, 0.063, 0.063, 4 and 1 mg/l, respectively. In the in vivo study, telithromycin inhibited abscess formation and significantly decreased viable cell counts in abscesses in comparison with the untreated group. CONCLUSIONS: These in vitro and in vivo antibacterial activities suggest that telithromycin could be a potential candidate for the treatment of bacterial infections complicated by chlamydial infection. Copyright 2003 S. Karger AG, Basel