Loading Pathway...
Error: Pathway image not found.
Hide
Pathway Description
Lidocaine NMDA Anesthetic Action Pathway
Homo sapiens
Drug Action Pathway
Created: 2023-06-09
Last Updated: 2023-10-25
Lidocaine is a local anesthetic used in a wide variety of superficial and invasive procedures. It can be found under the brand names Agoneaze, Akten, Alivio, Anestacon, Anodyne Lpt, Astero, Band-aid Hurt-free, Cathejell, Curacaine, Depo-medrol With Lidocaine, Dermacinrx Lido V Pak, Dermacinrx Phn Pak, Dermacinrx Prikaan, Diphen, Emla, Fortacin, Glydo, Instillagel, Kenalog, Lido Bdk, Lido-prilo Caine Pack, Lidodan, Lidoderm, Lidopac, Lidopril, Lidopro, Lidothol, Lidotral, Lignospan, Marcaine, Max-freeze, Medi-derm With Lidocaine, Neo-bex, Octocaine, Octocaine With Epinephrine, Oraqix, P-care, P-care X, Pliaglis, Prilolid, Prizotral, Procomycin, Readysharp Anesthetics Plus Ketorolac, Readysharp-A, Readysharp-p40, Readysharp-p80, Relador, Synera, Triple Antibiotic, Venipuncture Px1, Viadur, Xylocaine, Xylocaine With Epinephrine, Xylocard, Xylonor, Zingo, and Ztlido. Ever since its discovery and availability for sale and use in the late 1940s, lidocaine has become an exceptionally commonly used medication. In particular, lidocaine's principal mode of action in acting as a local anesthetic that numbs the sensations of tissues means the agent is indicated for facilitating local anesthesia for a large variety of surgical procedures. Nevertheless, lidocaine's local anesthetic action sees its use in many medical situations or circumstances that may benefit from its action, including the treatment of premature ejaculation. Lidocaine is a local anesthetic of the amide type. It is used to provide local anesthesia by nerve blockade at various sites in the body. It does so by stabilizing the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. In particular, the lidocaine agent acts on sodium ion channels located on the internal surface of nerve cell membranes. At these channels, neutral uncharged lidocaine molecules diffuse through neural sheaths into the axoplasm where they are subsequently ionized by joining with hydrogen ions. The resultant lidocaine cations are then capable of reversibly binding the sodium channels from the inside, keeping them locked in an open state that prevents nerve depolarization. As a result, with sufficient blockage, the membrane of the postsynaptic neuron will ultimately not depolarize and will thus fail to transmit an action potential. This facilitates an anesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their generation in the first place. In addition to blocking conduction in nerve axons in the peripheral nervous system, lidocaine has important effects on the central nervous system and cardiovascular system. Some side effects of using lidocaine may include chest pain, difficulty breathing, and lightheadedness.
References
Lidocaine NMDA Anesthetic Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Khaliq W, Alam S, Puri N: Topical lidocaine for the treatment of postherpetic neuralgia. Cochrane Database Syst Rev. 2007 Apr 18;(2):CD004846. doi: 10.1002/14651858.CD004846.pub2.
Pubmed: 17443559
Geha PY, Baliki MN, Chialvo DR, Harden RN, Paice JA, Apkarian AV: Brain activity for spontaneous pain of postherpetic neuralgia and its modulation by lidocaine patch therapy. Pain. 2007 Mar;128(1-2):88-100. doi: 10.1016/j.pain.2006.09.014. Epub 2006 Oct 25.
Pubmed: 17067740
Thomson PD, Melmon KL, Richardson JA, Cohn K, Steinbrunn W, Cudihee R, Rowland M: Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973 Apr;78(4):499-508. doi: 10.7326/0003-4819-78-4-499.
Pubmed: 4694036
StatPearls Internet: Lidocaine Profile
Kong W, Po S, Yamagishi T, Ashen MD, Stetten G, Tomaselli GF: Isolation and characterization of the human gene encoding Ito: further diversity by alternative mRNA splicing. Am J Physiol. 1998 Dec;275(6):H1963-70. doi: 10.1152/ajpheart.1998.275.6.H1963.
Pubmed: 9843794
Kikuno R, Nagase T, Ishikawa K, Hirosawa M, Miyajima N, Tanaka A, Kotani H, Nomura N, Ohara O: Prediction of the coding sequences of unidentified human genes. XIV. The complete sequences of 100 new cDNA clones from brain which code for large proteins in vitro. DNA Res. 1999 Jun 30;6(3):197-205. doi: 10.1093/dnares/6.3.197.
Pubmed: 10470851
Zhu XR, Wulf A, Schwarz M, Isbrandt D, Pongs O: Characterization of human Kv4.2 mediating a rapidly-inactivating transient voltage-sensitive K+ current. Receptors Channels. 1999;6(5):387-400.
Pubmed: 10551270
Bahring R, Dannenberg J, Peters HC, Leicher T, Pongs O, Isbrandt D: Conserved Kv4 N-terminal domain critical for effects of Kv channel-interacting protein 2.2 on channel expression and gating. J Biol Chem. 2001 Jun 29;276(26):23888-94. doi: 10.1074/jbc.M101320200. Epub 2001 Apr 3.
Pubmed: 11287421
An WF, Bowlby MR, Betty M, Cao J, Ling HP, Mendoza G, Hinson JW, Mattsson KI, Strassle BW, Trimmer JS, Rhodes KJ: Modulation of A-type potassium channels by a family of calcium sensors. Nature. 2000 Feb 3;403(6769):553-6. doi: 10.1038/35000592.
Pubmed: 10676964
Ohya S, Morohashi Y, Muraki K, Tomita T, Watanabe M, Iwatsubo T, Imaizumi Y: Molecular cloning and expression of the novel splice variants of K(+) channel-interacting protein 2. Biochem Biophys Res Commun. 2001 Mar 23;282(1):96-102. doi: 10.1006/bbrc.2001.4558.
Pubmed: 11263977
Rabert DK, Koch BD, Ilnicka M, Obernolte RA, Naylor SL, Herman RC, Eglen RM, Hunter JC, Sangameswaran L: A tetrodotoxin-resistant voltage-gated sodium channel from human dorsal root ganglia, hPN3/SCN10A. Pain. 1998 Nov;78(2):107-14. doi: 10.1016/s0304-3959(98)00120-1.
Pubmed: 9839820
Muzny DM, Scherer SE, Kaul R, Wang J, Yu J, Sudbrak R, Buhay CJ, Chen R, Cree A, Ding Y, Dugan-Rocha S, Gill R, Gunaratne P, Harris RA, Hawes AC, Hernandez J, Hodgson AV, Hume J, Jackson A, Khan ZM, Kovar-Smith C, Lewis LR, Lozado RJ, Metzker ML, Milosavljevic A, Miner GR, Morgan MB, Nazareth LV, Scott G, Sodergren E, Song XZ, Steffen D, Wei S, Wheeler DA, Wright MW, Worley KC, Yuan Y, Zhang Z, Adams CQ, Ansari-Lari MA, Ayele M, Brown MJ, Chen G, Chen Z, Clendenning J, Clerc-Blankenburg KP, Chen R, Chen Z, Davis C, Delgado O