2006
DOI: 10.1016/j.pain.2006.07.003
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Tramadol, fentanyl and sufentanil but not morphine block voltage-operated sodium channels

Abstract: Lidocaine-like sodium channel blocking drugs provide pain relief either by interrupting impulse conduction in neurons when applied locally in high concentrations or, when given systemically, by suppressing high-frequency ectopic discharges due to preferential drug binding to inactivated channel states. Lidocaine-like actions of opioids have frequently been demonstrated clinically. However, drug binding to resting and inactivated channel conformations has been studied systematically only in the case of meperidi… Show more

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Cited by 95 publications
(68 citation statements)
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“…Abnormal activity expressed by these afferents is suppressed by pregabalin, duloxetine, and tramadol (Haeseler et al. 2006; Wang et al. 2010; Chen et al.…”
Section: Discussionmentioning
confidence: 99%
“…Abnormal activity expressed by these afferents is suppressed by pregabalin, duloxetine, and tramadol (Haeseler et al. 2006; Wang et al. 2010; Chen et al.…”
Section: Discussionmentioning
confidence: 99%
“…It is conceivable that peripherally administered tramadol might inhibit peripheral 5-HT reuptake (Raffa et al, 1992) leading to increased extracellular 5-HT, 5-HT 7 receptor activation on sensory afferents, generation of intracellular cyclic AMP, extracellular efflux of adenosine with a subsequent activation of extracellular A 1 receptors, but this possibility needs to be explored experimentally. Additional peripheral effects of tramadol such as local anesthetic properties and NMDA and TRPV1 receptor interactions may also contribute to local antinociception (Haeseler et al, 2006;Hara et al, 2005;Marincsák et al, 2008), but it is not clear how such actions would involve A 1 receptors.…”
Section: Adenosine a 1 Receptors And Systemic Spinal And Peripheral mentioning
confidence: 99%
“…Furthermore, tramadol is now recognized to interact with additional cellular targets, such as Na + channels (Haeseler et al, 2006), N-methyl-D-aspartate (NMDA) receptors (Hara et al, 2005), and transient receptor potential vanilloid-1 (TRPV1) receptors (Marincsák et al, 2008), and such actions also may contribute to antinociception, particularly when tramadol is given locally and higher local tissue concentrations occur.…”
Section: Introductionmentioning
confidence: 99%
“…[4][5][6]29,30 Os mecanismos envolvidos nessa ação periférica ainda não são bem compreendidos. Há relatos de efeito anti-inflamatório fraco e efeito dependente de cálcio para tramadol.…”
Section: Análise Estatísticaunclassified
“…3 Além disso, apresenta efeito analgésico nos nervos periféricos que, em parte, é semelhante ao de anestésico local. [4][5][6] O efeito analgésico periférico de tramadol também foi identificado em humanos após infiltração para extração de terceiro molar, procedimentos cirúrgicos menores em crianças e como adjuvante aos anestésicos locais para reduzir a dor no pós-operatório. [7][8][9][10][11][12] Os receptores opioides periféricos há muito foram descritos e seu papel na analgesia em animais e humanos já foi demonstrado, 13---20 …”
Section: Introductionunclassified