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

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Leung YM, Tzeng JI, Kuo CS, Chen YW, Chu CC, Wang JJ

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

Eur J Pharmacol. 2013 Aug 15;714(1-3):366-72. doi: 10.1016/j.ejphar.2013.07.013. Epub 2013 Jul 16.

PubMed ID

23872380 [ View in PubMed

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Abstract

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<0.05). Carbetapentane was more potent than lidocaine (P<0.05) in spinal anesthesia. Intrathecal 5% dextrose (vehicle) elicited no spinal anesthesia. Lidocaine, used as a positive control, demonstrated concentration- and state-dependent effects on tonic block of voltage-gated Na(+) currents (IC(5)(0) of 49.6 and 194.6 microM at holding potentials of -70 and -100 mV, respectively). Carbetapentane was more potent (IC(5)(0) of 36.3 and 62.2 microM at holding potentials of -70 and -100 mV, respectively). Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33 Hz), 50 microM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block. These results revealed carbetapentane had a more potent and prolonged spinal blockade with a more sensory/nociceptive-selective action over motor blockade in comparison with lidocaine. Spinal anesthesia with carbetapentane could be through inhibition of voltage-gated Na(+) currents.

DrugBank Data that Cites this Article

Drugs

Pentoxyverine

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pentoxyverine	Voltage-gated sodium channel alpha subunit (Protein Group)	Protein group	Humans	Unknown	Inhibitor	Details