The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents

Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) an...

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Bibliographic Details
Published in:European journal of pharmacology 2013-08, Vol.714 (1-3), p.366-372
Main Authors: Leung, Yuk-Man, Tzeng, Jann-Inn, Kuo, Chang-Shin, Chen, Yu-Wen, Chu, Chin-Chen, Wang, Jhi-Joung
Format: Article
Language:English
Subjects:
analgesia
anesthesia
Anesthesia, Spinal
Animals
Behavior, Animal - drug effects
Behavior, Animal - physiology
Carbetapentane
Cell Line
Cyclopentanes - pharmacology
Electrophysiological Phenomena - drug effects
glucose
inhibitory concentration 50
Intrathecal
Lidocaine
Male
Motor Activity - drug effects
Motor Activity - physiology
pain
pharmacology
Rats
Rats, Sprague-Dawley
sodium
Sodium - metabolism
sodium channels
Sodium currents
Spinal anesthesia
Voltage-Gated Sodium Channels - metabolism
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Summary:Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) anesthesia. We evaluated the effects of carbetapentane on rat motor and pain behavior (when administered intrathecally) and on voltage-gated sodium channels in differentiated neuronal NG108-15 cells. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade (P
ISSN:0014-2999
1879-0712
DOI:10.1016/j.ejphar.2013.07.013