Cross-resistance analysis for DU-6859a, a new fluoroquinolone, compared to six structurally similar compounds (ciprofloxacin, clinafloxacin, fleroxacin, levofloxacin, ofloxacin, and sparfloxacin)

Cormican, Martin; Marshall, Steven A.; Jones, Ronald N.

doi:10.1016/0732-8893(94)00116-e

Cited by 12 publications

(11 citation statements)

References 19 publications

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“…The MIC 90 s for oxacillin-resistant strains ranged from 0.25 to 1 g/ml and were considerably higher than those for oxacillin-susceptible strains (MIC 90 , 0.03 to 0.12 g/ml), as shown for other quinolones (1,3). Sitafloxacin was the most active agent against oxacillin-resistant strains, being two times more active than clinafloxacin and at least eight times more active than the other quinolones.…”

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confidence: 83%

“…Sitafloxacin was the most active agent against gram-positive cocci and anaerobes. Against Enterobacteriaceae and nonfermenters, its activity was either equivalent to or better than that of clinafloxacin.Sitafloxacin (DU-6859a) is a new fluoroquinolone active against gram-positive and gram-negative bacteria, including anaerobes (3,7,13). In the present study, the in vitro activities of sitafloxacin against a large number of contemporary and clinically relevant bacterial isolates were determined and compared with those of ciprofloxacin, clinafloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin.…”

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In Vitro Activities of Sitafloxacin (DU-6859a) and Six Other Fluoroquinolones against 8,796 Clinical Bacterial Isolates

Milatovic

Schmitz

Brisse

et al. 2000

Antimicrob Agents Chemother

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The in vitro activities of sitafloxacin, ciprofloxacin, trovafloxacin, levofloxacin, clinafloxacin, gatifloxacin, and moxifloxacin against 5,046 gram-negative bacteria, 3,344 gram-positive cocci, and 406 anaerobes were determined. Sitafloxacin was the most active agent against gram-positive cocci and anaerobes. Against Enterobacteriaceae and nonfermenters, its activity was either equivalent to or better than that of clinafloxacin.Sitafloxacin (DU-6859a) is a new fluoroquinolone active against gram-positive and gram-negative bacteria, including anaerobes (3,7,13). In the present study, the in vitro activities of sitafloxacin against a large number of contemporary and clinically relevant bacterial isolates were determined and compared with those of ciprofloxacin, clinafloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin.A total of 8,796 bacterial strains were tested which had been isolated between April 1997 and February 1999 from patients in 24 university hospitals in 14 European countries, 1 in Israel, and 3 in South Africa. Only one isolate per patient was permitted. Strains were reidentified in our laboratory using a combination of standard methods and either the VITEK or the API system (BioMerieux, s'Hertogenbosch, The Netherlands). MICs were determined by a microdilution method described by the National Committee for Clinical Laboratory Standards (15), using cation-adjusted Mueller-Hinton broth. For testing Streptococcus spp. and Neisseria spp., 5% lysed horse blood was added. Haemophilus spp. were tested using Haemophilus test medium. The inoculum was adjusted to 5 ϫ 10 5 CFU/ml. Plates were read after 20 to 24 h of incubation at 35°C in ambient air. Anaerobic bacteria were tested with WilkinsChalgren broth and a final inoculum of 10 6 CFU/ml. Plates were read after 48 h of incubation at 35°C in an anaerobic environment (16).The results of susceptibility testing are presented as the MICs at which 50 and 90% of the isolates tested are inhibited (MIC 50 and MIC 90 ) and the ranges of MICs (Table 1). Sitafloxacin was very active against enterobacterial species, inhibiting 96.9% of the 3,129 strains at a concentration of 1 g/ml. The MIC 50 s ranged from Յ0.008 to 1 g/ml, and the MIC 90 s ranged from 0.015 to 2 g/ml. The MIC 90 for Providencia spp. was the highest (2 g/ml), followed by those for Enterobacter aerogenes and Escherichia coli (1 g/ml for each). These three species also exhibited the highest rates of ciprofloxacin resistance (51.6, 38.5, and 14.6%, respectively). The MIC 90 s of sitafloxacin for Citrobacter koseri, Klebsiella oxytoca, Pantoea agglomerans, Proteus vulgaris, salmonellae, Serratia liquefaciens, Shigella spp., and Yersinia enterocolitica ranged from 0.015 to 0.12 g/ml and were similar to those of ciprofloxacin. However, sitafloxacin was four times more active than ciprofloxacin against Citrobacter freundii, Klebsiella pneumoniae, Morganella morganii, and Serratia marcescens and at least eight times more active against E. aerogenes, Enterobacter cloacae, E. coli, and Prot...

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In Vitro Activities of Sitafloxacin (DU-6859a) and Six Other Fluoroquinolones against 8,796 Clinical Bacterial Isolates

Milatovic

Schmitz

Brisse

et al. 2000

Antimicrob Agents Chemother

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“…Em algumas espécies, como Serratia sp., a DU 6859-a foi quatro vezes mais potente que a ciprofloxacina (MIC50 de 0,06µg/mL e 0,25µg/mL, respectivamente). Embora a DU 6859-a tenha mecanismo de ação semelhante a outras fluoroquinolonas (inibição da DNA girase bacteriana) 5 e o principal mecanismo de resistência bacteriana às fluoroquinolonas seja alteração do sítio de ação por meio de mutações cromossômicas, esse estudo demonstrou que essa fluoroquinolona mantém potente ação mesmo contra bactérias resistentes à ciprofloxacina e outras fluoroquinolonas. Cem por cento das amostras testadas foram suscetíveis à DU 6859-a.…”

Section: Resultsunclassified

“…Atualmente, com o aumento da importância das infecções por cocos gram-positivos como os enterococos e estreptococos, para os quais as fluoroquinolonas têm potência limitada 5 , e com a emergência de bactérias gram-negativas resistentes a essa classe de antimicrobianos 6,7 , tem sido incentivada a pesquisa por novos compostos dessa classe.…”

Section: Introductionunclassified

“…Como essa droga parece apresentar excelente penetração tecidual, principalmente pulmonar, e possuir melhor atividade bactericida contra Staphylococcus aureus, Streptococcus pneumoniae e Haemophilus influenzae, ela poderá representar uma opção para o tratamento de infecções pulmonares 3,8 . Uma das mais recentes fluoroquinolonas, a DU 6859-a, possui estrutura similar à ciprofloxacina, administração oral, e tem demonstrado excelente atividade in vitro contra bactérias gram-negativas, cocos grampositivos e anaeróbios 5,9 . O sucesso das cefalosporinas de 3 a geração tem sido limitado pela rápida evolução das β-lactamases.…”

Section: Introductionunclassified

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Avaliação da atividade in vitro dos novos antimicrobianos da classe das fluoroquinolonas, cefalosporinas e carbapenens contra 569 amostras clínicas de bactérias gram-negativas

Gales¹,

Pignatari²,

Jones³

et al. 1997

Rev. Assoc. Med. Bras.

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RESUMO -OBJETIVO. A proposta deste estudo foi a avaliação da atividade in vitro INTRODUÇÃOA resistência bacteriana tem emergido como um problema mundialmente importante, fazendo com que muitas classes de antimicrobianos tenham se tornado menos efetiva nos últimos anos. Algumas vezes, parte da emergência de resistência está relacionada ao uso intensivo ou inadequado desses compostos, ocasionando a seleção de patógenos resistentes 1 . Pacientes infectados por bactérias resistentes necessitam de maior tempo de hospitalização, apresentam risco aumentado de mortalidade e utilizam antimicrobianos mais potentes, que normalmente são mais caros e/ou mais tóxicos 2 . Esses fatores têm motivado a busca por drogas cada vez mais potentes e estáveis aos mecanismos de resistência bacteriana. Muitas vezes, modificações estruturais são realizadas nas moléculas de antimicrobianos já utilizados na prática clínica para que esse objetivo seja alcançado.No final dos anos 80, as fluoroquinolonas tornaram-se uma excelente opção para o tratamento de infecções causadas por bactérias aeróbias gram-negativas, pois, além de potentes, essas drogas permitiam a continuação do tratamento por via oral 3,4 . Atualmente, com o aumento da importância das infecções por cocos gram-positivos como os enterococos e estreptococos, para os quais as fluoroquinolonas têm potência limitada 5 , e com a emergência de bactérias gram-negativas resistentes a essa classe de antimicrobianos 6,7 , tem sido incentivada a pesquisa por novos compostos dessa classe.A grepafloxacina (anteriormente designada OPC 17116) é uma fluoroquinolona que mantém potente ação contra gram-negativos e maior potência contra gram-positivos, quando comparada com as fluoroquinolonas já disponíveis comercialmente no Brasil. Como essa droga parece apresentar excelente penetração tecidual, principalmente pulmonar, e possuir melhor atividade bactericida contra Staphylococcus

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Determination of quinolones and fluoroquinolones in hospital sewage water by off-line and on-line solid-phase extraction procedures coupled to HPLC-UV

Turiel¹,

Bordin

Rodríguez

2005

J. Sep. Science

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In this work, the development of two solid-phase extraction procedures (off-line and on-line formats) for the identification and quantification of several (fluoro)quinolones in hospital sewage water by HPLC-UV is described. Both procedures are based on the use of C18 and anion exchange (SAX) sorbents for the preconcentration and clean-up steps, respectively, and all variables influencing both steps were optimised. In the off-line format, after its pH was adjusted to 2.5, sample was preconcentrated on a C18 cartridge and eluted with 4 mL of methanol/ammonia (94/6). The methanolic extract must be diluted up to 10 mL with water to allow quantitative retention of the analytes on the SAX cartridge. In the on-line format, the addition of 2.5% of NH4Cl to the sewage water sample (pH = 2.5) was necessary to increase the breakthrough volumes of the analytes in the C18 precolumn. Quantitative transfer of the (fluoro)quinolones from the C18 precolumn to the SAX precolumn was accomplished by pumping 2 mL of a mixture methanol/water (40/60, pH = 9.2) at 2 mL min(-1). Elution of the analytes from the SAX precolumn by means of the chromatographic mobile phase required the inclusion of an additional isocratic step at the beginning of the gradient program. Both off-line and on-line solid phase extraction procedures coupled to HPLC-UV were applied to the analysis of a sewage water sample collected in the sewer system at the output of the St Dimphna Hospital (Geel, Belgium). The fluoroquinolone ciprofloxacin was found in this sample and quantified at 5.8 +/- 0.4 microg L(-1) (off-line method) and 5.6 +/- 0.5 microg L(-1) (on-line method). The analysis of spiked samples containing the seven (fluoro)quinolones studied provided quantitative recoveries in all cases with low RSD values (from 6 to 12%), and all the analytes could be identified by means of their UV spectra with match factors varying from 950 to 985 depending on the (fluoro)quinolone.

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Cross-resistance analysis for DU-6859a, a new fluoroquinolone, compared to six structurally similar compounds (ciprofloxacin, clinafloxacin, fleroxacin, levofloxacin, ofloxacin, and sparfloxacin)

Cited by 12 publications

References 19 publications

In Vitro Activities of Sitafloxacin (DU-6859a) and Six Other Fluoroquinolones against 8,796 Clinical Bacterial Isolates

In Vitro Activities of Sitafloxacin (DU-6859a) and Six Other Fluoroquinolones against 8,796 Clinical Bacterial Isolates

Avaliação da atividade in vitro dos novos antimicrobianos da classe das fluoroquinolonas, cefalosporinas e carbapenens contra 569 amostras clínicas de bactérias gram-negativas

Determination of quinolones and fluoroquinolones in hospital sewage water by off-line and on-line solid-phase extraction procedures coupled to HPLC-UV

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