Introduction: Overuse of muscles, stress and dehydration are some of the reasons for muscle spasms. Muscle cramps often resolve on their own but in some cases medical intervention is required.
Aim: The aim of this article is to study the modulating muscle activity using GABA inhibitors.
Materials and Methods: Treatment plans for bruxism include different ways for modulating muscle activity, which should be studied.
Results: A spasm is an involuntary, unexpected contraction of one or more muscles.Muscle spasms can happen in any muscle of the human body. The most common reasons for the occurrence of spasms are overuse of a muscle, dehydration or stress.
Discussion: Gamma-aminobutyric acid (GABA) serves as the main inhibitory neurotransmitter in the developed, mature central nervous system of mammals. GABAA receptors are ligand-activated chloride channels. GABA receptors are the main focus of this study because of their wide spread throughout the mammalian nervous system. In a recent study from 2017, Gervasi, Sisti and team from Baltimore discovered that the regular application of thiocolchicoside-based foam topically on m. rectus et biceps femoris reduced the risk of muscle cramps, muscle pain and improved the overall performance of the athletes in the study group.
Conclusion: This discovery, along with the known properties of thiocolchicoside and its structure, present an interesting perspective when considering new ways to treat muscle spasms. Dermal patches ensure the gradual release of a substance in a certain area through the skin. The idea is to develop a dermal patch for application on m. masseter et temporalis when treating patients with bruxism.
Barrell A. Why do muscle spasms happen? 2020. Available at: https://sfchiro.org/why-do-muscle-spasms-happen/
Ffrench-Constant RH, Rocheleau TA, Steichen JC, Chalmers AE. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature. 1993;363(6428):449-51. doi: 10.1038/363449a0.
Szabadics J, Varga C, Molnár G, Oláh S, Barzó P, Tamás G. Excitatory effect of GABAergic axo-axonic cells in cortical microcircuits. Science. 2006;311(5758):233-5. doi: 10.1126/science.1121325.
Phulera S, Zhu H, Yu J, Claxton DP, Yoder N, Yoshioka C, et al. Cryo-EM structure of the benzodiazepine-sensitive α1β1γ2S tri-heteromeric GABAA receptor in complex with GABA. Elife. 2018;7:e39383. doi: 10.7554/eLife.39383.
Li K, Xu E. The role and the mechanism of gamma-aminobutyric acid during central nervous system development. Neurosci Bull. 2008;24(3):195-200. doi: 10.1007/s12264-008-0109-3.
Folkman S. The Oxford handbook of stress, health, and coping. Oxford: Oxford University Press; 2011.
Kaila K, Voipio J. Postsynaptic fall in intracellular pH induced by GABA-activated bicarbonate conductance. Nature. 1987;330(6144):163-5. doi: 10.1038/330163a0.
Kandel ER, Schwartz JH, Jessell TM, Siegelbaum SA, Hudspeth AJ, editors. Principles of neural science. 5th ed. McGraw-Hill Education/Medical; 2012.
Wei W, Zhang N, Peng Z, Houser CR, Mody I. Perisynaptic localization of delta subunit-containing GABA(A) receptors and their activation by GABA spillover in the mouse dentate gyrus. J Neurosci. 2003 Nov 19;23(33):10650-61. doi: 10.1523/JNEUROSCI.23-33-10650.2003.
Farrant M, Nusser Z. Variations on an inhibitory theme: phasic and tonic activation of GABA(A) receptors. Nat Rev Neurosci. 2005;6(3):215-29. doi: 10.1038/nrn1625.
Tüzün F, Unalan H, Oner N, Ozgüzel H, Kirazli Y, Içağasioğlu A, et al. Multicenter, randomized, double-blinded, placebo-controlled trial of thiocolchicoside in acute low back pain. Joint Bone Spine. 2003;70(5):356-61. doi: 10.1016/s1297-319x(03)00075-7.
Ketenci A, Basat H, Esmaeilzadeh S. The efficacy of topical thiocolchicoside (Muscoril) in the treatment of acute cervical myofascial pain syndrome: a single-blind, randomized, prospective, phase IV clinical study. Agri. 2009;21(3):95-103.
Soonawalla DF, Joshi N. Efficacy of thiocolchicoside in Indian patients suffering from low back pain associated with muscle spasm. J Indian Med Assoc. 2008;106(5):331-5.
Ketenci A, Ozcan E, Karamursel S. Assessment of efficacy and psychomotor performances of thiocolchicoside and tizanidine in patients with acute low back pain. Int J Clin Pract. 2005;59(7):764-70. doi: 10.1111/j.1742-1241.2004.00454.x
Carta M, Murru L, Botta P, Talani G, Sechi G, De Riu P, et al. The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system. Neuropharmacology. 2006;51(4):805-15. doi: 10.1016/j.neuropharm.2006.05.023.
Mascia MP, Bachis E, Obili N, Maciocco E, Cocco GA, Sechi GP, et al. Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes. Eur J Pharmacol. 2007;558(1-3):37-42. doi: 10.1016/j.ejphar.2006.11.076.
De Riu PL, Rosati G, Sotgiu S, Sechi G. Epileptic seizures after treatment with thiocolchicoside. Epilepsia. 2001;42(8):1084-6. doi: 10.1046/j.1528-1157.2001.0420081084.x.
Giavina-Bianchi P, Giavina-Bianchi M, Tanno LK, Ensina LF, Motta AA, Kalil J. Epileptic seizure after treatment with thiocolchicoside. Ther Clin Risk Manag. 2009;5(3):635-7. doi: 10.2147/tcrm.s4823.
Sechi G, De Riu P, Mameli O, Deiana GA, Cocco GA, Rosati G. Focal and secondarily generalised convulsive status epilepticus induced by thiocolchicoside in the rat. Seizure. 2003;12(7):508-15. doi: 10.1016/s1059-1311(03)00053-0.
Gervasi M, Sisti D, Benelli P, Fernández-Peña E, Calcabrini C, Rocchi MBL, et al. The effect of topical thiocolchicoside in preventing and reducing the increase of muscle tone, stiffness, and soreness: A real-life study on top-level road cyclists during stage competition. Medicine (Baltimore). 2017;96(30):e7659. doi: 10.1097/MD.0000000000007659.
Email this article (Login required) 
