Literature DB >> 26302692

Effectiveness of retigabine against levobupivacaine-induced central nervous system toxicity: a prospective, randomized animal study.

Yanxin Cheng1, Hong Li2, Jun Li3, Yongxue Chen4, Ran Duan1, Jinge Yuan4, Senming Zhao5.   

Abstract

PURPOSE: KCNQ2/3 channels play an important role in controlling neuronal excitability. Agents that decrease KCNQ2/3 current amplitudes are proconvulsant, whereas KCNQ2/3 current enhancers are anticonvulsant. Levobupivacaine is able to block the KCNQ2/3 channels and enhance neuronal excitation, whereas retigabine is able to reopen the channels and thus reduce overexcitation of neurons. In this study, we aimed to determine if retigabine is able to abolish local-anesthetic-induced seizures.
METHODS: Twenty New Zealand rabbits were randomly divided into two groups of ten. Levobupivacaine (0.5 %) was infused into conscious rabbits via the marginal ear vein at 8 ml/kg/h until the rabbits seized, and 5 mg/kg of retigabine were injected intravenously to terminate the seizure. The corresponding volume of saline was used as a control. The behavior of and the electroencephalogram (EEG) for each rabbit were continually monitored. Before levobupivacaine infusion, the rabbits were placed in a prostrate position calmly on the experimental platform, and the EEG pattern exhibited β waves. Intravenous levobupivacaine induced a typical EEG seizure characterized by multiple spike and slow wave complexes. The EEG changes were accompanied by behavioral convulsions which were characterized by clonic activity and opisthotonus.
RESULTS: Retigabine effectively terminated the electrographic and behavioral seizures. After receiving 5 mg/kg of retigabine, the animals became drowsy, and the EEG changed to δ waves.
CONCLUSIONS: We propose that KCNQ2/3 channels play an important role in levobupivacaine-induced central nervous system toxicity, and a KCNQ2/3 channel activator may be used to treat levobupivacaine-induced convulsions.

Entities:  

Keywords:  KCNQ2/3 channels; Local anesthetic toxicity; Retigabine; Seizure

Mesh:

Substances:

Year:  2015        PMID: 26302692     DOI: 10.1007/s00540-015-2069-x

Source DB:  PubMed          Journal:  J Anesth        ISSN: 0913-8668            Impact factor:   2.078


  13 in total

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Review 2.  Stereoselective interactions between local anesthetics and ion channels.

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Journal:  Can J Anaesth       Date:  2010-02-12       Impact factor: 5.063

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Journal:  Nature       Date:  1966-01-08       Impact factor: 49.962

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Authors:  Martin J Gunthorpe; Charles H Large; Raman Sankar
Journal:  Epilepsia       Date:  2012-01-05       Impact factor: 5.864

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Journal:  Anesthesiology       Date:  1995-03       Impact factor: 7.892

9.  Retigabine stimulates human KCNQ2/Q3 channels in the presence of bupivacaine.

Authors:  Mark A Punke; Patrick Friederich
Journal:  Anesthesiology       Date:  2004-08       Impact factor: 7.892

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  1 in total

1.  Activation of KCNQ channels located on the skeletal muscle membrane by retigabine and its influence on the maximal muscle force in rat muscle strips.

Authors:  P Zagorchev; E Apostolova; V Kokova; L Peychev
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  1 in total

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