The Effects of the Local Anesthetics Lidocaine and Procaine on Glycine and γ-Aminobutyric Acid Receptors Expressed in Xenopus Oocytes

Hara, Koji; Sata, Takeyoshi

doi:10.1213/01.ane.0000261509.72234.a6

Cited by 41 publications

(35 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Indeed, tramadol has been demonstrated to be ineffective in injured peripheral nerves. 7 However, in the aforementioned study, nerves were damaged by constriction for a long periodthere was no evidence of chronic nerve damage in our experiment, as the allodynia reversed with time.…”

contrasting

confidence: 52%

“…4 Furthermore, after outpatient arthroscopic partial meniscectomy, intra-articular tramadol plus pericapsular incisional bupivacaine provides better analgesia than intraarticular plus pericapsular incisional bupivacaine. 5,6 Evidence in the literature suggests that tramadol antagonizes glutamate N-methyl-D-aspartic acid (NMDA) receptors 7,8 that are known to be involved in the pathophysiology of chronic pain. 9 Tramadol, fentanyl, sufentanil, but not morphine, block voltage-gated sodium channels.…”

Section: Résumémentioning

confidence: 99%

“…20 Other possible mechanisms of local anesthetic action distinct from sodium channel blockade are unlikely, since tramadol has no effects on inhibitory glycine or gammaaminobutyric acid (GABA) receptors at clinically relevant concentrations. 7 Primary activity through opioid action is unlikely, since direct application of peripheral intraplantar naloxone does not reverse tramadol's effect on reducing heat-induced nociception, 10 and naloxone does not reverse tramadol's ability to block the licking response to formalin in the paw. 20 Thus, it is likely that tramadol produces its analgesic effects in the tail-flick test by blockade of sodium channels.…”

mentioning

confidence: 99%

See 2 more Smart Citations

Effects of local tramadol administration on peripheral glutamate-induced nociceptive behaviour in mice

Wang

Chung

Whitehead

et al. 2010

Can J Anesth/J Can Anesth

View full text Add to dashboard Cite

Purpose The use of peripheral tramadol to block pain has been advocated. However, since its actions in the periphery have not been elucidated fully, we tested the hypothesis that peripheral tramadol blocks peripheral glutamate-induced nociceptive behaviour in mice. Methods First, we compared the duration of paw licking after intraplantar (ipl.) glutamate administration, with and without tramadol, using a randomized blinded controlled design. Next, we established the half maximal effective concentrations (EC 50s ) for local tramadol and reference compound lidocaine in the hot water tail-flick latency test and the glutamate-induced paw allodynia assay. Results Tramadol reduced glutamate-induced paw licking from 33 ± 12 sec to 4 ± 4 sec (mean ± SD; t test, P \ 0.05; n = 6 per group). The tramadol and lidocaine EC 50 nerve conduction blocks in the tail did not differ significantly (84 ± 24 mM vs 69 ± 5 mM, respectively).Although tramadol reduced glutamate-induced allodynia (EC 50 , 46 ± 13 mM), lidocaine was more potent (EC 50 , 13 ± 5 mM; Dixon's up-and-down method; P \ 0.05). Tramadol was 2.5 times as effective at blocking nerve conduction in the tail compared with allodynia in the paw. Conclusions Local tramadol administration blocked nociceptive behaviour in mice induced by peripheral glutamate. Compared with lidocaine, the relative potency of tramadol was lower for blocking glutamate-induced allodynia than for sensory nerve conduction blockade, suggesting the activation of a pronociceptive receptor system in the periphery. RésuméObjectif L'utilisation de tramadol pe´riphe´rique a e´teṕ ropose´e pour bloquer la douleur. Cependant, comme nous ne connaissons pas pleinement ses actions sur les nerfs pe´riphe´riques, nous avons e´mis l'hypothe`se que le tramadol pe´riphe´rique bloquait les comportements nociceptifs provoque´s par le glutamate pe´riphe´rique chez la souris. Méthode Nous avons d'abord compare´la dure´e du le´chage de la patte apre`s une administration intraplantaire (ipl.) de glutamate, avec ou sans tramadol, en utilisant une me´thode contrôle´e randomise´e en aveugle. Ensuite, nous avons de´termine´les concentrations efficaces moyennes (CE 50 ) pour le tramadol administre´localement et un compose´de lidocaı¨ne comme re´fe´rence a`l'aide du test de latence du retrait de la queue et du test d'allodynie de la patte provoque´e par le glutamate. Résultats Le tramadol a re´duit le le´chage de patte provoque´par le glutamate de 33 ± 12 sec a`4 ± 4 sec (moyenne ± ET; test t, P \ 0,05; n = 6 par groupe). Les CE 50 pour le bloc de conduction nerveuse re´alise´avec le

show abstract

contrasting

confidence: 52%

Section: Résumémentioning

confidence: 99%

mentioning

confidence: 99%

See 1 more Smart Citation

Effects of local tramadol administration on peripheral glutamate-induced nociceptive behaviour in mice

Wang

Chung

Whitehead

et al. 2010

Can J Anesth/J Can Anesth

View full text Add to dashboard Cite

show abstract

“…ii) The effects evoked by lidocaine on nAChRs in either SCG neurons or muscle fibres have some similarities to those described for other members of 12 the Cys-loop family of receptors. So, lidocaine inhibits, though at higher concentrations, glycine and GABA A receptors expressed in oocytes (Hara and Sata, 2007), although its mechanisms of blockade remain to be elucidated.…”

Section: Discussionmentioning

confidence: 99%

Lidocaine effects on acetylcholine-elicited currents from mouse superior cervical ganglion neurons

Alberola-Die

Reboreda

Lamas

et al. 2013

Neuroscience Research

View full text Add to dashboard Cite

show abstract

“…Low dose lidocaine (10 μM) enhances and high dose (1 mM) inhibits glycinergic signalling [174]. The lidocaine metabolite, N-ethylglycine (NEG) is a substrate of the glycine reuptake transporter so it competes with endogenous and synaptically released glycine for reuptake leading to increased extracellular and synaptic glycine levels [172].…”

Section: The Rationale For Ivlt In the Management Of Painmentioning

confidence: 99%

A Review of Intravenous Lidocaine Infusion Therapy for Paediatric Acute and Chronic Pain Management

Lauder¹

2017

Pain Relief - From Analgesics to Alternative Therapies

View full text Add to dashboard Cite

Pediatric acute and chronic pain experiences involve the interaction of physiological, psychological, behavioural, developmental, pharmacological and situational factors. In the acute perioperative pain setting preventative multimodal analgesia is required to provide comfort and minimise the potential for "wind-up" and central sensitisation. When pain is recurrent, ongoing or chronic some children embark on a downward spiral of decreased physical, psychological and social functioning. The multidisciplinary team management approach is a well-established standard of care for children with complex chronic pain. Intravenous lidocaine has peripheral and central mediated analgesic, anti-inflammatory and anti-hyperalgesic properties. Intravenous lidocaine infusion therapy (IVLT) has been shown to be effective in the management of acute and chronic pain in adults. This chapter will present the rational for IVLT in pediatric pain management with emphasis on preventative multimodal therapy in acute pain and the multidisciplinary treatment approach in chronic pain. Large multi-centre randomised controlled trials are required to provide the evidence-base to confirm that IVLT is indeed an effective and safe treatment option in acute preventative multimodal analgesia and as an adjunct in the multidisciplinary care of chronic pain in the pediatric population. Keywords

show abstract

The Effects of the Local Anesthetics Lidocaine and Procaine on Glycine and γ-Aminobutyric Acid Receptors Expressed in Xenopus Oocytes

Cited by 41 publications

References 20 publications

Effects of local tramadol administration on peripheral glutamate-induced nociceptive behaviour in mice

Effects of local tramadol administration on peripheral glutamate-induced nociceptive behaviour in mice

Lidocaine effects on acetylcholine-elicited currents from mouse superior cervical ganglion neurons

A Review of Intravenous Lidocaine Infusion Therapy for Paediatric Acute and Chronic Pain Management

Contact Info

Product

Resources

About