Caramiphen-induced block of sodium currents and spinal anesthesia

Leung, Yuk‐Man; Tzeng, Jann-Inn; Gong, Chi Li; Wang, Yuwen; Chen, Yu‐Wen; Wang, Jhi-Joung

doi:10.1016/j.ejphar.2014.10.035

Cited by 11 publications

(5 citation statements)

References 40 publications

(41 reference statements)

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“…Here, motor function was examined according to the extensor thrust (gram force), which resisted contacting a platform via the animal heel hit against the digital platform balance (Mettler Toledo, PB 1502‐S, Greifensee, Switzerland). A reduction in the force, representing decreased extensor muscle tone, was considered a motor deficit . A force <20 g (the weight of the ‘flaccid limb’) was recorded as the full absence of extensor postural thrust (100% motor block or 100% MPE) .…”

Section: Methodsmentioning

confidence: 99%

“…A reduction in the force, representing decreased extensor muscle tone, was considered a motor deficit. [21,22] A force <20 g (the weight of the 'flaccid limb') was recorded as the full absence of extensor postural thrust (100% motor block or 100% MPE). [23] The maximal block in the time course of spinal block was defined as the % MPE.…”

Section: Motor Proprioceptive and Nociceptive Blockmentioning

confidence: 99%

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Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats

Tzeng

Chiu

Wang

et al. 2018

Journal of Pharmacy and Pharmacology

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Objectives The aim of this experiment was mainly to examine the effects of intrathecally injected doxylamine and triprolidine, two antihistamine drugs spinal motor and sensory functions. Methods After intrathecally injecting the rats with five different doses, the dose—response curves of spinal sensory and motor block with doxylamine and triprolidine were constructed. In comparison with the local anaesthetic mepivacaine, the quality and duration of spinal anaesthesia with doxylamine or triprolidine were conducted. Key findings Doxylamine, mepivacaine and triprolidine elicited spinal motor and sensory (nociception and proprioception) blockades in a dose‐dependent fashion. On the ED50 (50% effective dose) basis, the rank order of drug potency was triprolidine > mepivacaine > doxylamine (P < 0.05) at provoking spinal motor, proprioceptive and nociceptive blockades. On the equianaesthetic doses (ED25, ED50 and ED75), the duration of spinal anaesthesia with doxylamine was longer (P < 0.01) than that with mepivacaine or triprolidine. Moreover, doxylamine or triprolidine displayed greater potency (ED50) (P < 0.05) and duration (P < 0.05) of sensory block over motor block. Conclusions Doxylamine or triprolidine produces a dose‐dependent effect of spinal motor and sensory block. Triprolidine with a better nociception‐selective action over motor block has a better potency than mepivacaine or doxylamine. Doxylamine and triprolidine produce longer durations than mepivacaine.

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Section: Methodsmentioning

confidence: 99%

Section: Motor Proprioceptive and Nociceptive Blockmentioning

confidence: 99%

Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats

Tzeng

Chiu

Wang

et al. 2018

Journal of Pharmacy and Pharmacology

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“…Nociceptive, proprioceptive, and motor functions were evaluated as previously reported . The magnitude of spinal block (nociception, proprioception, and motor function) was defined as the percent of possible effect (%PE).…”

Section: Methodsmentioning

confidence: 99%

Intrathecal amantadine for prolonged spinal blockade of sensory and motor functions in rats

Tzeng

Kan

Wang

et al. 2016

Fundamemntal Clinical Pharma

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We aimed to compare the hypothesized local anesthetic action of amantadine (1-adamantanamine) with that of the known local anesthetic mepivacaine. Motor, proprioceptive, and nociceptive functions were evaluated in rats after intrathecal administration. Amantadine elicited spinal anesthesia in a dose-related fashion and produced a better sensory-selective action over motor blockade (P < 0.01). On the 50% effective dose (ED50 ) basis, the rank of potency on spinal motor, proprioceptive, and nociceptive block was mepivacaine > amantadine (P < 0.01 for the differences). Amantadine (63.5 μmol/kg) and mepivacaine (7.1 μmol/kg) produced complete spinal block of motor function, proprioception, and nociception. On an equipotent basis (ED25 , ED50 , and ED75 ), the duration of amantadine was longer (P < 0.01) than that of mepivacaine on spinal motor, proprioceptive, and nociceptive block. Our preclinical data demonstrated that amantadine was less potent than mepivacaine at producing spinal anesthesia. The spinal block duration produced by amantadine was greater than that produced by mepivacaine. Both amantadine and mepivacaine produced a markedly nociceptive-specific blockade.

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“…Lumbar puncture was performed on conscious rats according to the previous studies . In brief, a 27‐gauge needle attached to a 50‐μL syringe (Hamilton, Reno, Nevada) was inserted into the midline of the L4–L5 intervertebral space until a tail flick test indicated entrance into the spinal space.…”

Section: Methodsmentioning

confidence: 99%

Memantine elicits spinal blockades of motor function, proprioception, and nociception in rats

Chen

Chiu

Liu

et al. 2015

Fundamemntal Clinical Pharma

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Although memantine blocks sodium currents and produces local skin anesthesia, spinal anesthesia with memantine is unknown. The purpose of the study was to evaluate the local anesthetic effect of memantine in spinal anesthesia and its comparison with a widely used local anesthetic lidocaine. After intrathecally injecting the rats with five doses of each drug, the dose-response curves of memantine and lidocaine were constructed. The potencies of the drugs and durations of spinal anesthetic effects on motor function, proprioception, and nociception were compared with those of lidocaine. We showed that memantine produced dose-dependent spinal blockades in motor function, proprioception, and nociception. On a 50% effective dose (ED50 ) basis, the rank of potency was lidocaine greater than memantine (P < 0.05 for the differences). At the equipotent doses (ED25 , ED50 , ED75 ), the block duration produced by memantine was longer than that produced by lidocaine (P < 0.05 for the differences). Memantine, but not lidocaine, displayed more sensory/nociceptive block than motor block. The preclinical data demonstrated that memantine is less potent than lidocaine, whereas memantine produces longer duration of spinal anesthesia than lidocaine. Memantine shows a more sensory-selective action over motor blockade.

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Caramiphen-induced block of sodium currents and spinal anesthesia

Cited by 11 publications

References 40 publications

Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats

Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats

Intrathecal amantadine for prolonged spinal blockade of sensory and motor functions in rats

Memantine elicits spinal blockades of motor function, proprioception, and nociception in rats

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