In Vitro and In Vivo Activities of Sparfloxacin in Legionella Infections

Saito, Atsushi; Gaja, Michihiro

doi:10.2165/00003495-199500492-00058

Cited by 7 publications

(5 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…All fluoroquinolones examined in this study had good intracellular activity against Legionella, a finding consistent with the results of previous studies (13,30). Sparfloxacin was most potent among the fluoroquinolones tested in this study, in agreement with our previous study (29) and that of Edelstein et al (6). Thus, the results obtained with the cytopathic effect assay system used in the present study are consistent with those of previous in vitro and in vivo studies.…”

Section: Discussionsupporting

confidence: 93%

Simplified Quantitative Assay System for Measuring Activities of Drugs against IntracellularLegionella pneumophila

et al. 1998

Self Cite

View full text Add to dashboard Cite

We developed a new simple assay for the quantitation of the activities of drugs against intracellular Legionella pneumophila. The cells of a murine macrophage-like cell line (J774.1 cells) allowed the intracellular growth and replication of the bacteria, which ultimately resulted in cell death. The infected J774.1 cell monolayers in 96-well microplates were first treated with antibiotics and were further cultured for 72 h. The number of viable J774.1 cells in each well was quantified by a colorimetric assay with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and an enzyme-linked immunosorbent assay reader. The number of growing bacteria in each well was also determined by counting the numbers of CFU on buffered charcoal yeast extract-α agar plates. Viable J774.1 cell counts, determined by the colorimetric assay, were inversely proportional to the number of intracellular replicating bacteria. The minimum extracellular concentrations (MIECs) of 24 antibiotics causing inhibition of intracellular growth of L. pneumophila were determined by the colorimetric assay system. The MIECs of beta-lactams and aminoglycosides were markedly higher than the MICs in buffered yeast extract-α broth. The MIECs of macrolides, fluoroquinolones, rifampin, and minocycline were similar to the respective MICs. According to their intracellular activities, clarithromycin and sparfloxacin were the most potent among the macrolides or fluoroquinolones tested in this study. Our results indicated that the MTT assay system allows comparative and quantitative evaluations of the intracellular activities of antibiotics and efficient processing of a large number of samples.

show abstract

Section: Discussionsupporting

confidence: 93%

Simplified Quantitative Assay System for Measuring Activities of Drugs against IntracellularLegionella pneumophila

et al. 1998

Self Cite

View full text Add to dashboard Cite

show abstract

“…Grepafloxacin's activity against L. pneumophila was found to be superior to that of the two macrolides evaluated, erythromycin and clarithromycin. This activity of fluoroquinolones compared to erythromycin has been noted in other studies [20,21].…”

Section: Discussionsupporting

confidence: 83%

“…This but slightly less active than sparfloxacin, against L. activity of fluoroquinolones compared to erythromycin pneurnophila. The clinical efficacy of grepafloxacin has been noted in other studies [20,21].…”

Section: Discussionmentioning

confidence: 58%

In vitro activity, postantibiotic effect and human monocyte activity of grepafloxacin against Legionella species

Dubois

St-Pierre

1999

Clinical Microbiology and Infection

View full text Add to dashboard Cite

OBJECTIVE: To determine the in vitro antimicrobial activity, postantibiotic effect (PAE) and human monocyte activity of grepafloxacin compared with sparfloxacin, ciprofloxacin, clarithromycin, erythromycin and rifampicin against 181 strains of Legionella pneumophila, nine strains of L. micdadei, 10 strains of L. dumoffii, seven strains of L. longbeachae and seven other Legionella strains. METHODS: MICs were determined by standard agar dilution using buffered yeast extract (BYE) agar. PAE and human monocyte activity were determined by standard culture techniques. RESULTS: Grepafloxacin, sparfloxacin and rifampicin were the most active agents against L. pneumophila (MIC90

show abstract

“…Olamufloxacin and sparfloxacin inhibited the cytopathic effect of intracellularly multiplying L. pneumophila at a concentration four times lower than levofloxacin. The efficacy of erythromycin, levofloxacin, 8 ciprofloxacin 9 and sparfloxacin 11,12 in the pulmonary infection model has been evaluated elsewhere, and all these drugs are effective. In this study, olamufloxacin was almost as effective as levofloxacin and more effective than erythromycin (20 mg/kg/day) in the pulmonary infection model.…”

Section: Discussionmentioning

confidence: 99%

“…in vitro and in vivo. 11,12 In this study, the in vitro and in vivo activity of olamufloxacin against Legionella spp. was evaluated, and compared with those of erythromycin, levofloxacin, ciprofloxacin and sparfloxacin.…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo activity of olamufloxacin (HSR-903) against Legionella spp.

Higa

Arakaki

Tateyama

et al. 2003

Journal of Antimicrobial Chemotherapy

View full text Add to dashboard Cite

The activity of the fluoroquinolone olamufloxacin (HSR-903) against Legionella spp. was studied in vitro and in vivo. The olamufloxacin MIC at which 50% of isolates are inhibited (MIC50) for 81 different Legionella spp. strains (59 type strains and 22 clinical isolates) was 0.008 mg/L, which was identical to sparfloxacin, whereas the MIC50s for erythromycin, levofloxacin and ciprofloxacin were 0.25, 0.032 and 0.032 mg/L, respectively. Olamufloxacin and sparfloxacin (at 0.008 mg/L) inhibited intracellular growth and subsequent cytotoxicity of L. pneumophila 80-045 in J774.1 macrophages, whereas levofloxacin and ciprofloxacin did not, at the same concentration. When olamufloxacin was given to the infected guinea pigs orally (5 mg/kg of body weight), peak levels in the lung were 3.02 mg/kg at 2 h post-administration, with a half-life of 3.41 h and an AUC0-12 of 12.31 mg.h/kg. The 2 day post-infection bacterial burden of the lung in the animals treated with olamufloxacin (5 and 1.25 mg/kg given orally twice a day) was much lower than in those treated with levofloxacin (same dose as olamufloxacin) or erythromycin (10 mg/kg given orally twice a day). When treated with olamufloxacin (5 mg/kg given orally twice a day) for 7 days, 11 of 12 L. pneumophila-infected guinea pigs survived for 14 days post-infection, as did all 12 guinea pigs treated with levofloxacin (5 mg/kg given orally twice a day) for 7 days. In contrast, only two of 12 animals treated with erythromycin survived and 10 of 11 died in the physiological saline group. Olamufloxacin was as effective as levofloxacin in a guinea pig model of Legionnaires' disease. These data warrant further study of whether olamufloxacin is an option for the treatment of Legionella infections.

show abstract

In Vitro and In Vivo Activities of Sparfloxacin in Legionella Infections

Cited by 7 publications

References 1 publication

Simplified Quantitative Assay System for Measuring Activities of Drugs against IntracellularLegionella pneumophila

Simplified Quantitative Assay System for Measuring Activities of Drugs against IntracellularLegionella pneumophila

In vitro activity, postantibiotic effect and human monocyte activity of grepafloxacin against Legionella species

In vitro and in vivo activity of olamufloxacin (HSR-903) against Legionella spp.

Contact Info

Product

Resources

About