Effects of anti-inflammatory drugs on convulsant activity of quinolones: a comparative study of drug interaction between quinolones and anti-inflammatory drugs

Hori, Seiji; Kizu, Junko; Kawamura, Masahiro

doi:10.1007/s10156-003-0275-1

Cited by 22 publications

(26 citation statements)

References 4 publications

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“…1). The convulsant activity of LVFX (ED 50 value, 76.7 nmol/head) was the same as that previously reported, 7 and the convulsant activity of STFX was almost same as that of LVFX. Concurrent administration with BPA and fl urbiprofen markedly enhanced the convulsant activity of NFLX and ENX and did not affect the activity of LVFX.…”

supporting

confidence: 78%

“…We have also reported that various quinolones showed differing potencies to induce convulsions, and we have reported the interactions of quinolones with various anti-infl ammatory drugs. 6,7 Sitafl oxacin (STFX) is a newly developed quinolone. 8 It is noteworthy to determine whether this quinolone has convulsant activity and whether it shows interactions with anti-infl ammatory drugs.…”

mentioning

confidence: 99%

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Convulsant activity of sitafloxacin and its interactions with anti-inflammatory drugs in mice

Hori

2009

Journal of Infection and Chemotherapy

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supporting

confidence: 78%

mentioning

confidence: 99%

Convulsant activity of sitafloxacin and its interactions with anti-inflammatory drugs in mice

Hori

2009

Journal of Infection and Chemotherapy

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“…or intracerebroventricular (i.c.v.) administration induced seizures (Nozaki et al, 1991; Hori et al, 1991Hori et al, , 2003Nakamura et al, 2003). Seizure induction potential of enoxacin, ofloxacin or norfloxacin could not be detected in the present study, which might be due to the con- Vol.…”

Section: Discussioncontrasting

confidence: 44%

“…From these results, the reason why seizure induction potential of enoxacin or norfloxacin could not be detected might be related to the healthy condition in larvae and systemic exposure. Moreover, the neurotoxicity potential of quinolones used in the present study was as follows: norfloxacin > sparfloxacin > ciprofloxacin > enoxacin > ofloxacin (Lipsky and Baker, 1999;Hori et al, 2003) and the affinity of these drugs to the GABA receptor associated with seizure induction was: norfloxacin > ciprofloxacin > enoxacin > sparfloxacin > ofloxacin (Hori and Shimada, 1993). The seizure potential of ofloxacin was considered undetectable when using zebrafish since the seizure induction potential of this drug was lower than other quinolones.…”

Section: Discussionmentioning

confidence: 99%

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

et al. 2014

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-As drug-induced seizures have severe impact on drug development, evaluating seizure induction potential of candidate drugs at the early stages of drug discovery is important. A novel assay system using zebrafish has attracted interest as a high throughput toxicological in vivo assay system, and we tried to establish an experimental method for drug-induced seizure liability on the basis of locomotor activity in zebrafish. We monitored locomotor activity at high-speed movement (> 20 mm/sec) for 60 min immediately after exposure, and assessed seizure liability potential in some drugs using locomotor activity. However this experimental procedure was not sufficient for predicting seizures because the potential of several drugs with demonstrated seizure potential in mammals was not detected. We, therefore, added other parameters for locomotor activity such as extending exposure time or conducting flashlight stimulation (10 Hz) which is a known seizure induction stimulus, and these additional parameters improved seizure potential detection in some drugs. The validation study using the improved methodology was used to assess 52 commercially available drugs, and the prediction rate was approximately 70%. The experimental protocol established in this present study is considered useful for seizure potential screening during early stages of drug discovery.Key words: Zebrafish, Locomotor activity, Seizure, Extending exposure time, Flashlight stimulation Correspondence: Naoteru Koseki (E-mail: naoteru-koseki@ds-pharma.co.jp) Original ArticleThe Journal of Toxicological Sciences (J. Toxicol. Sci.) Vol.39, No.4, 579-600, 2014 Vol. 39 No. 4 579 through the blood-brain barrier (BBB). Since such assays are conducted with a focus on specific neural networks or cells associated with seizures, performing an evaluation using above alternative methods is direct and limited. On the basis of the aforementioned findings, a test system that can take pharmacokinetic effects into account and can be used to perform an evaluation under conditions closer to whole body is considered desirable. As such, an in vivo evaluation system using Caenorhabditis elegans (C. elegans), which is one of the nematodes with gamma-aminobutyratergic (GABAergic) neurons related to seizures, has been reported (Locke et al., 2006;Pandey et al., 2010), and an evaluation using behavioral assessment of such organism is expected. However, nematodes are very different from mammals in terms of the anatomical structure of central nervous system (CNS) or pharmacokinetics. Therefore, performing an assessment which approximates the evaluation of a conventional study using rodents is considered to be difficult.Zebrafish is a vertebrate and its genomic homology to humans is approximately 70% (Howe et al., 2013). In addition, zebrafish can be utilized in early stage drug screening in recent decades. For these reasons, an evaluation using zebrafish has recently been given attention as a novel in vivo evaluation system for safety assessment. Since zebrafish have tele...

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“…It has been confi rmed by animal studies that the presence of biphenyl acetate (an active metabolite of fenbufen) reduces the threshold of enoxacin for induction of convulsions several hundredfold, while that of LVX is only reduced approximately 1.3-fold [16] . As shown by subsequent nonclinical studies [17][18][19] and suggested by the above results, the extent of central nervous system excitation and interactions with NSAIDs differs markedly between the various new quinolones.…”

Section: Discussionmentioning

confidence: 61%

Post-Marketing Surveillance of the Safety of Levofloxacin in Japan

Yamaguchi

Kawai

Matsumoto³

et al. 2007

Chemotherapy

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Background: Central nervous system reactions to new quinolones, such as convulsions due to interaction with nonsteroidal anti-inflammatory drugs (NSAIDS), have attracted increased attention in Japan. Methods: The safety of levofloxacin (LVX) was investigated in Japan by post-marketing surveillance and reviewing spontaneous reports. Results: Post-marketing surveillance was performed in 16,117 patients between 1994 and 1996. The incidence of adverse reactions was 1.3% (203/16,117), being comparable with that for ofloxacin or that shown by phase II/III studies. Among 4,977 patients receiving concomitant NSAID treatment, the overall incidence of adverse reactions and the incidence of neurological reactions (including convulsions) did not significantly differ from those in patients without anti-inflammatory therapy. Review of the spontaneous reports on convulsions showed that patients with nephropathy, patients over 75 years and patients with a history of convulsive diseases were more likely to develop convulsions during LVX therapy. Conclusion: LVX should be used cautiously in patients with the above risk factors.

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Effects of anti-inflammatory drugs on convulsant activity of quinolones: a comparative study of drug interaction between quinolones and anti-inflammatory drugs

Cited by 22 publications

References 4 publications

Convulsant activity of sitafloxacin and its interactions with anti-inflammatory drugs in mice

Convulsant activity of sitafloxacin and its interactions with anti-inflammatory drugs in mice

Establishment of a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish

Post-Marketing Surveillance of the Safety of Levofloxacin in Japan

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