In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species

Higa, Futoshi; Akamine, Morikazu; Haranaga, Shusaku; Tohyama, Masato; Shinzato, Takashi; Tateyama, Masao; Koide, Michio; Saitô, Atsushi; Fujita, Jiro

doi:10.1093/jac/dki391

Cited by 23 publications

(15 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…pneumophila is very susceptible to several antibiotics, such as the fluoroquinolones, ketolides and macrolides [14]. Pazufloxacin, a fluoroquinolone antibiotic available in Japan, is also effective against Legionella [19,23]. In this study, pazufloxacin showed slight decrease of the number of viable bacteria, however, the combination therapy showed more effective for decreasing of bacteria with a significant difference in spite of the short duration of treatment.…”

Section: Discussionmentioning

confidence: 58%

See 1 more Smart Citation

In vivo efficacy of sivelestat in combination with pazufloxacin againstLegionellapneumonia

Morinaga¹,

Yanagihara²,

Araki³

et al. 2010

Experimental Lung Research

View full text Add to dashboard Cite

It is important to regulate excessive inflammation when we treat patients with severe infectious disease. Sivelestat sodium hydrate (sivelestat), a neutrophil elastase inhibitor, is used in the treatment of lung injury but its effect on pneumonia is unknown. We examined the efficacy of sivelestat in combination with a fluoroquinolone, in a Legionella pneumophila pneumonia mouse model. The combination therapy did not show a significant survival improvement compared to the treatment with fluoroquinolone alone, but reduced bacteria number and inflammatory cells in the early phase. The combination therapy can contribute to treatment of L. pneumophila pneumonia with protecting lungs.

show abstract

Section: Discussionmentioning

confidence: 58%

“…Pazufloxacin is a parenteral fluoroquinolone antibiotic available in Japan that has potent activity against Legionella species [19]. However, treating patients with severe pneumonia using antibiotics alone is difficult and thus additional therapies aimed at the various aspects of Legionella pathology are required.…”

Section: Introductionmentioning

confidence: 99%

In vivo efficacy of sivelestat in combination with pazufloxacin againstLegionellapneumonia

Morinaga¹,

Yanagihara²,

Araki³

et al. 2010

Experimental Lung Research

View full text Add to dashboard Cite

show abstract

“…Recently, to assess the intracellular anti-Legionella activity of antimicrobial agents, infection models using various kinds of cells derived from humans, mice, and guinea pigs have been developed (2,10,11,14,22). In this study, we used the A/J mouse strain for determination of both in vitro intracellular antibacterial activity and in vivo efficacy in pulmonary infection models, because it has been reported that this strain permits growth of Legionella as a feature of its genetic background (8,27).…”

Section: Discussionmentioning

confidence: 99%

In Vitro Intracellular Activity and In Vivo Efficacy of Modithromycin, a Novel Bicyclolide, against Legionella pneumophila

Sato

Tateda

Kimura

et al. 2011

Antimicrob Agents Chemother

View full text Add to dashboard Cite

The in vitro and in vivo activities of modithromycin, a novel bicyclolide, against Legionella pneumophila were compared with those of telithromycin, clarithromycin, azithromycin, and levofloxacin. All the test agents decreased the intracellular growth of viable L. pneumophila bacteria over 96 h of incubation in both types of cells used, A/J mouse-derived macrophages and A549 human alveolar epithelial cells, at extracellular concentrations of 4؋ and 16؋ MIC, respectively. However, when the agents were removed from the medium after exposure for 2 h, regrowth of intracellular bacteria occurred in both cell systems when they were exposed to telithromycin, clarithromycin, and levofloxacin but not when they were exposed to modithromycin and azithromycin. Once-daily administration of modithromycin at a dose of 10 mg/kg of body weight for 5 days led to a significant decrease of intrapulmonary viable L. pneumophila bacteria in immunosuppressed A/J mice. The efficacy of modithromycin was superior to the efficacies of telithromycin and clarithromycin and comparable to the efficacies of azithromycin and levofloxacin. In addition, modithromycin and azithromycin inhibited the intrapulmonary regrowth of bacteria even at 72 h after the last treatment, but telithromycin and levofloxacin did not. These results suggested that modithromycin has longer-lasting cellular pharmacokinetic features like azithromycin. In conclusion, modithromycin, as well as azithromycin, has excellent in vitro and in vivo bactericidal activities and persistent efficacy against intracellular L. pneumophila. Modithromycin should be a useful agent for treatment of pulmonary infections caused by this pathogen.

show abstract

“…This drug has good in vitro and in vivo activity against a broad range of bacteria, especially Gram-negative bacteria [1,2]. Clinical trials showed its intravenous injection formula was effective in treating respiratory infections and the drug has been approved and is available in Japan [3]. The literature survey revealed that analytical methods reported for the estimation of pazufloxacin mesylate in human plasma include chemiluminescence flow injection [4] and HPLC methods [5][6][7].…”

Section: Introductionmentioning

confidence: 99%

HPLC and Densitometric TLC Methods for Simultaneous Determination of Pazufloxacin with Some Co-Administered Drugs in Human Plasma

Abdallah¹

2012

J Chromat Separation Techniq

View full text Add to dashboard Cite

Two chromatographic methods have been developed for determination of pazufloxacin in human plasma with two co-administered drugs, cefoperazone and sulbactam sodium. First method depends on reverse phase high performance liquid chromatography. The plasma sample was extracted using mixture of ethyl acetate and 15% perchloric acid. The method was linear over the concentration range 0.5 to 20 µg/ml, 1 to 30 µg/ml and 1 to 25 µg/ ml of pazufloxacin mesylate, cefoperazone and sulbactam sodium, respectively.The mobile phase used consist of methanol, 0.01 M sodium acetate buffer (pH adjusted to 3 using trifluoroacetic acid) in a ratio 20:80 and 0.5% TEA and flow rate 1 ml/min in isocratic mode and UV-detection at wavelength 240 nm. Second method depends on densitometric thin layer chromatography. The method was linear over concentration range 1 to 20 µg/ml, 6 to 24 µg/ml and 4 to 20 µg/ml of pazufloxacin mesylate, cefoperazone and sulbactam sodium, respectively. The mobile phase used consists of chloroform, methanol and ammonia in the ratio of (11:6:2, v/v/v). Densitometric analysis was carried out at wavelength 240 nm. The stability of pazufloxacin mesylate and the coadministered drugs in plasma was confirmed during three freeze-thaw cycles (−20°C).

show abstract

In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species

Abstract: Pazufloxacin and tosufloxacin, as well as other quinolones, were more potent than macrolides and an azalide. Present data warrant further study on the efficacy of these drugs in the treatment of Legionella infections.

Cited by 23 publications

References 22 publications

In vivo efficacy of sivelestat in combination with pazufloxacin againstLegionellapneumonia

In vivo efficacy of sivelestat in combination with pazufloxacin againstLegionellapneumonia

In Vitro Intracellular Activity and In Vivo Efficacy of Modithromycin, a Novel Bicyclolide, against Legionella pneumophila

HPLC and Densitometric TLC Methods for Simultaneous Determination of Pazufloxacin with Some Co-Administered Drugs in Human Plasma

Contact Info

Product

Resources

About