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Query: UMLS:C0023241 (Legionella)
 6,990 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The activity of trovafloxacin against 22 clinical Legionella isolates was determined by broth microdilution susceptibility testing. The trovafloxacin concentration required to inhibit 90% of strains tested was < or = 0.004 micrograms/ml, in contrast to 0.032 micrograms/ml for ofloxacin. In guinea pig alveolar macrophages, trovafloxacin achieved intracellular levels up to 28-fold over the extracellular concentration, which was similar to the levels obtained with erythromycin. Trovafloxacin (0.25 micrograms/ml) reduced bacterial counts of two L. pneumophila strains grown in guinea pig alveolar macrophages by > 2 log10 CFU/ml, without regrowth, under drug-free conditions over a 3-day period; trovafloxacin was significantly more active than ofloxacin or erythromycin (0.25 to 1 microgram/ml) in this assay. Single-dose (10 mg of prodrug CP-116,517-27 per kg of body weight given intraperitoneally [i.p.], equivalent to 7.5 mg of trovafloxacin per kg) pharmacokinetic studies performed in guinea pigs with L. pneumophila pneumonia revealed peak serum and lung trovafloxacin levels to be 3.8 micrograms/ml and 5.0 micrograms/g, respectively, at 0.5 h and 4.2 micrograms/ml and 2.9 micrograms/g, respectively, at 1 h. Administration of a lower prodrug dose (1.4 mg of trovafloxacin equivalent per kg i.p.) gave levels in lung and serum of 0.4 microgram/g and 0.4 microgram/ml, respectively, 1 h after drug administration. The terminal half-lives of elimination from serum and lung were 0.8 and 1.1 h, respectively. All 15 infected guinea pigs treated for 5 days with CP-116,517-27 once daily (10 mg/kg/day i.p., equivalent to 7.5 mg of trovafloxacin per kg/day) survived for 10 days after antimicrobial therapy, as did all 15 guinea pigs treated with ofloxacin once daily (10 mg/kg/day i.p.) for 5 days. None of 13 animals treated with saline survived. In a second experiment with animals, trovafloxacin (1.4 mg/kg/day i.p. for 5 days) protected all 16 guinea pigs from death, whereas all 15 animals treated with saline died. Trovafloxacin is an effective antimicrobial agent against Legionella in vitro and in vivo, with the ability to concentrate in macrophages and kill intracellular organisms.
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PMID:Activity of trovafloxacin (CP-99,219) against Legionella isolates: in vitro activity, intracellular accumulation and killing in macrophages, and pharmacokinetics and treatment of guinea pigs with L. pneumophila pneumonia. 883 72

Trovafloxacin (CP-99,219) was very active against Gram-negative species examined including Haemophilus influenzae, Moraxella catarrhalis, Legionella spp., Neisseria spp. and Escherichia coli (MIC90s < or = 0.03 mg/L). In general trovafloxacin was twice as active as ofloxacin but only half as active as ciprofloxacin against Gram-negative species. Trovafloxacin was active against Gram-positive organisms, including Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes and Enterococcus faecalis (MIC90s < or = 0.25 mg/L). Against these organisms activity was eight to 16 times greater for trovafloxacin than for either ofloxacin or ciprofloxacin. In addition, Chlamydia spp., Mycoplasma spp. and Ureaplasma urealyticum were eight to 16 times more susceptible to trovafloxacin than to either ofloxacin or ciprofloxacin. These in-vitro data show that trovafloxacin is a broad-spectrum fluoroquinolone with greater activity against clinically important Gram-positive species compared with ofloxacin or ciprofloxacin.
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PMID:In-vitro activity of trovafloxacin, a new fluoroquinolone, against recent clinical isolates. 922 69

Trovafloxacin, sparfloxacin, ciprofloxacin and levofloxacin were equally active against Moraxella catarrhalis, Haemophilus influenzae, Legionella pneumophila, Klebsiella pneumoniae, Enterobacter cloacae and Serratia marcescens. Ciprofloxacin was the most active compound against Pseudomonas aeruginosa (MIC90 = 1 mg/L), followed by trovafloxacin (MIC90 = 4 mg/L). Trovafloxacin was twice as active as sparfloxacin against Streptococcus pyogenes (MIC90 = 0.12 mg/L), Streptococcus pneumoniae (MIC90 = 0.12 mg/L) and Staphylococcus aureus (MIC90 = 0.06 mg/L) (except quinolone-resistant, methicillin-resistant S. aureus, for which the MIC90 was 8 mg/L). Trovafloxacin was the most active compound against Enterococcus faecalis: 80% of strains were susceptible to 0.25 mg/L. There was complete cross-resistance between all fluoroquinolones.
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PMID:In-vitro activities of ciprofloxacin, levofloxacin, lomefloxacin, ofloxacin, pefloxacin, sparfloxacin and trovafloxacin against gram-positive and gram-negative pathogens from respiratory tract infections. 933 98

The activity of trovafloxacin, a new fluorinated naphtheridone, was tested against 61 Legionella spp. isolates and compared with that of 4 fluoroquinolones, 2 macrolides, and rifampin. Trovafloxacin MICs were determined by a reference agar dilution method and E-test (Solna, Sweden) strips on buffered charcoal yeast extract agar. Among the fluoroquinolone compounds, the rank order of activity (on the basis of MIC90 results) determined with E-test strips was as follows: levofloxacin (MIC90, 0.094 microgram/ml) > trovafloxacin = sparfloxacin = ofloxacin (MIC90, 0.19 microgram/ml). Rifampin (MIC90, 0.008 microgram/ ml) and clarithromycin (MIC90, 0.032 microgram/ml) were the most potent of all drugs tested, and erythromycin and ciprofloxacin were the least active. In this study, the E-test strips with trovafloxacin were validated (100% of results +/- one log2 dilution compared to the reference value) for susceptibility testing with Legionella isolates.
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PMID:Anti-Legionella activity of trovafloxacin compared with seven other antimicrobial agents including an intermethod evaluation. 935 Apr 17

Quinolones are broad-spectrum antibiotics active primarily against aerobic gram-negative organisms. All quinolones have activity against oral anaerobes, but only trovafloxacin provides coverage against Bacteroides fragilis, the primary anaerobe of the abdomen/pelvis. In addition, quinolones are very active against atypical pulmonary pathogens, e.g., Legionella, but trovafloxacin is the least active against Chlamydia. As with other antibiotics, the selection of quinolones depends not simply on the degree of microbiologic activity but also on safety profile and cost. Ciprofloxacin and trovafloxacin are associated with central nervous system side effects. Photosensitivity reactions may occur with sparfloxacin. Trovafloxacin is associated with more adverse reactions than any other quinolone, and its gastrointestinal side effects are most frequent among the quinolones. Resistance potential is highest with ciprofloxacin and lowest with levofloxacin. Sparfloxacin and grepafloxacin are available only as oral formulations. Among the parenteral quinolones, ciprofloxacin and trovafloxacin are the most expensive, levofloxacin, the least expensive. Levofloxacin is preferred for general use alone or in combination because it has virtually no side effects, induces no resistance, and is the least expensive and most versatile quinolone currently available.
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PMID:Quinolones: clinical use and formulary considerations. 1034 49

The comparative in vitro potency and post-antibiotic effect (PAE) of gemifloxacin (SB-265805), moxifloxacin, trovafloxacin, grepafloxacin, levofloxacin, ofloxacin, ciprofloxacin, azithromycin, clarithromycin, erythromycin and rifampicin were evaluated against Legionella pneumophila serogroups 1-9 and 12 (n = 204) and other Legionella spp. (n = 34). MICs were determined by standard two-fold agar dilution. PAE was determined by exposing the isolates to the test agents at 4 x MIC for 1 h. Trovafloxacin was the most potent agent overall (MIC range < or =0.004-0.016 mg/L, MIC(90) < or =0.008 mg/L). Of the other quinolones tested, gemifloxacin, moxifloxacin, grepafloxacin and levofloxacin were more potent (MIC(90) 0.016 mg/L) against L. pneumophila than ciprofloxacin and ofloxacin (MIC(90) 0. 03 mg/L). Against Legionella spp., the test quinolones were more potent (MIC range < or =0.004-0.06 mg/L) than either erythromycin or azithromycin (MIC(90) 0.5 and 0.25 mg/L, respectively). Gemifloxacin had the longest PAE (4.65 h) of the agents tested against erythromycin-resistant L. pneumophila. Of the quinolones, only gemifloxacin, grepafloxacin, levofloxacin and ofloxacin had PAEs of >3 h against erythromycin-resistant Legionella spp. Azithromycin, erythromycin and clarithromycin had PAEs of <3 h against all erythromycin-resistant strains. Against erythromycin-susceptible L. pneumophila, only gemifloxacin, moxifloxacin, ofloxacin and ciprofloxacin had PAEs of >3 h, and only rifampicin, ofloxacin, gemifloxacin and erythromycin had PAEs of >2 h against erythromycin-susceptible Legionella spp. The superior potency of gemifloxacin compared with erythromycin indicates that it may be of use in the treatment of legionellosis. The significant PAE described here, combined with favourable pharmacokinetics, supports once-daily dosing for gemifloxacin in the treatment of legionella infections.
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PMID:Comparative in vitro activity and post-antibiotic effect of gemifloxacin against Legionella spp. 1082 31