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Review
. 2021 Aug 17:69:102733.
doi: 10.1016/j.amsu.2021.102733. eCollection 2021 Sep.

Molecular mechanisms of lidocaine

Resiana Karnina  1   2 , Syafri Kamsul Arif  3 , Mochammad Hatta  4 , Agussalim Bukhari  5
Affiliations
Review

Molecular mechanisms of lidocaine

Resiana Karnina et al. Ann Med Surg (Lond). .

Abstract

Lidocaine is an amide-class local anesthetic used clinically to inhibit pain sensations. Systemic administration of lidocaine has antinociceptive, antiarrhythmic, anti-inflammatory, and antithrombotic effects. Lidocaine exerts these effects under both acute and chronic pain conditions and acute respiratory distress syndrome through mechanisms that can be independent of its primary mechanism of action, sodium channel inhibition. Here we review the pathophysiological underpinnings of lidocaine's role as an anti-nociceptive, anti-inflammatory mediated by toll-like receptor (TLR) and nuclear factor kappa-β (NF-kβ) signalling pathways and downstream cytokine effectors high mobility group box 1 (HMGB1) and tumour necrosis factor-α (TNF-α).

Keywords: Analgesia; Inflammation; Lidocaine; Local anesthesia; Neurotransmitter; Pain.

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Figures

Fig. 1
Fig. 1
Chemical structure of lidocaine [21].
Fig. 2
Fig. 2
The mechanism of action of local anesthetics on inflammation [21].
Fig. 3
Fig. 3
The relationship between HMGB1, TLR4, and RAGE. TLR4 binding induces cytokine secretion from macrophages and monocytes (left), meanwhile, RAGE modulates endothelial and tumor cell function (right) [3].
See this image and copyright information in PMC

References

    1. Hsing C.H., Wang J.J. Clinical implication of perioperative inflammatory cytokine alteration. Acta Anaesthesiol. Taiwanica. 2015;53:23–28. doi: 10.1016/j.aat.2015.03.002. - DOI - PubMed
    1. Cicchese J.M., Evans S., Hult C., Joslyn L.R., Wessler T., Millar J.A., Marino S., Cilfone N.A., Mattila J.T., Linderman J.J., Kirschner D.E. Dynamic balance of pro- and anti-inflammatory signals controls disease and limits pathology. Immunol. Rev. 2018;285:147–167. doi: 10.1111/imr.12671. - DOI - PMC - PubMed
    1. Alhayyan A., McSorley S., Roxburgh C., Kearns R., Horgan P., McMillan D. The effect of anesthesia on the postoperative systemic inflammatory response in patients undergoing surgery: a systematic review and meta-analysis. Surg. Open Sci. 2020;2:1–21. doi: 10.1016/j.sopen.2019.06.001. - DOI - PMC - PubMed
    1. Andersson U., Tracey K.J. HMGB1 is a therapeutic target for sterile inflammation and infection. Annu. Rev. Immunol. 2011;29:139–162. doi: 10.1146/annurev-immunol-030409-101323. - DOI - PMC - PubMed
    1. Josh F., Soekamto T.H., Adriani J.R., Jonatan B., Mizuno H., Faruk M. The combination of stromal vascular fraction cells and platelet-rich plasma reduces malondialdehyde and nitric oxide levels in deep dermal burn injury. J. Inflamm. Res. 2021;14:3049–3061. doi: 10.2147/JIR.S318055. - DOI - PMC - PubMed