High-affinity blockade of voltage-operated skeletal muscle sodium channels by 2,6-dimethyl-4-chlorophenol

Haeseler, Gertrud; Gudehus, S.; Bufler, J.; Dengler, Reinhard; Leuwer, Martin

doi:10.1017/s0265021505002176

Cited by 4 publications

(1 citation statement)

References 14 publications

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“…23,24 Although the active ingredient in Biofreeze, menthol, does not lower tissue temperature, it stimulates cold thermoreceptors [25][26][27][28] through a chemical reaction resulting in pain relief 29 through a counterirritant effect. 30 Heat packs are also commonly utilized at home when individuals seek comfort and pain relief. [31][32][33][34] Ultimately both cold and hot modalities provide an analgesic effects and successfully, albeit temporarily, reduce pain.…”

Section: Introductionmentioning

confidence: 99%

Use of a Non-Pharmacological Pain Relief Kit to Reduce Opioid Use Following Orthopedic Surgery: A Prospective Randomized Study

O’Hara

Tyler²,

McHugh

et al. 2022

International Journal of Sports Physical Therapy

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Introduction Opioid prescription to treat pain among orthopedic surgery patients remains common practice in the United States but overprescribing opioids can lead to abuse. The purpose of this study was to determine the effect of a multimodal non-pharmacological ‘pain relief kit’ on pain, function, and opioid consumption in individuals recovering from orthopedic surgery. Hypothesis Patients provided with the pain relief kit would consume less opioid medication, report lower pain levels, and have better functional outcome scores than the control group. Level of Evidence 2b Methods Fifty-three subjects (18 women, 35 men) having orthopedic surgery were randomly assigned to either receive the Pain Relief Kit (treatment) or control group. At the first postoperative physical therapy visit (within 1 week of surgery) the treatment group was provided elastic resistance bands, kinesiology tape, Biofreeze, and a hot/cold pack as part of the Pain Relief Kit. Patients completed the SF-36 and either the DASH or LEFS questionnaires consistent with their surgery at baseline and four weeks post-op. Both groups reported daily pain (Visual Analogue Scale), opioid use, and over the counter medication use. The treatment group also recorded daily kit modality use. Results There was no significant difference in total opioid use between the treatment (108±252 milligram morphine equivalents) and control groups (132±158 MME; p=0.696). Opioid use and pain declined from week one to four with no difference between groups (p<0.001). Outcome scores and SF-36 scores improved from week one to four with no difference between groups (p<0.001). Conclusion A non-pharmacological pain relief kit did not have an effect on opioid use in this patient population nor did it improve pain relief or function compared to controls.

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Section: Introductionmentioning

confidence: 99%

Use of a Non-Pharmacological Pain Relief Kit to Reduce Opioid Use Following Orthopedic Surgery: A Prospective Randomized Study

O’Hara

Tyler²,

McHugh

et al. 2022

International Journal of Sports Physical Therapy

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Topical antiseptics for the treatment of sore throat block voltage-gated neuronal sodium channels in a local anaesthetic-like manner

Buchholz

Leuwer

Ahrens

et al. 2009

Naunyn-Schmied Arch Pharmacol

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Lozenges for the treatment of sore throat provide relief of discomfort in cases of oral inflammation. This effect has not been fully explained so far. Here, we have examined the proposition that key components of pharmaceutical preparations for the treatment of sore throat which are routinely regarded antiseptics might have sodium channel-blocking, i.e. local anaesthetic-like effects. We investigated the effects of hexylresorcinol, amylmetacresol and dichloro-benzylalcohol on voltage-operated neuronal (Na(V)1.2) sodium channels heterologously expressed in HEK 293 cells in vitro. Hexylresorcinol, amylmetacresol and dichloro-benzylalcohol reversibly blocked depolarisation-induced whole-cell sodium inward currents. The half-maximum blocking concentrations (EC(50)) at -150 mV were 23.1, 53.6 and 661.6 microM, respectively. Block induced by hexylresorcinol and amylmetacresol was increased at depolarised potentials and use-dependent during trains of depolarisations applied at high frequency (100 Hz) indicating that both drugs bind more tightly to inactivated conformations of the channel. Estimates for the inactivated state affinity were 1.88 and 35 microM for hexylresorcinol and amylmetacresol, respectively. Hexylresorcinol and amylmetacresol are 10-20 fold more potent than the local anaesthetic lidocaine in blocking sodium inward current. Both drugs show an increased effect at depolarised membrane potentials or in conditions of high-frequency discharges.

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Features of the use of ClO2 in the oxidation of some alkylphenols

et al. 2023

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High-affinity blockade of voltage-operated skeletal muscle sodium channels by 2,6-dimethyl-4-chlorophenol

Cited by 4 publications

References 14 publications

Use of a Non-Pharmacological Pain Relief Kit to Reduce Opioid Use Following Orthopedic Surgery: A Prospective Randomized Study

Use of a Non-Pharmacological Pain Relief Kit to Reduce Opioid Use Following Orthopedic Surgery: A Prospective Randomized Study

Topical antiseptics for the treatment of sore throat block voltage-gated neuronal sodium channels in a local anaesthetic-like manner

Features of the use of ClO2 in the oxidation of some alkylphenols

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