Mephenesin (INN), also called myanesin,[1][2] is a centrally acting muscle relaxant. It can be used as an antidote for strychnine poisoning. Mephenesin however presents with the major drawbacks of having a short duration of action and a much greater effect on the spinal cord than the brain, resulting in pronounced respiratory depression at clinical doses and therefore a very low therapeutic index. It is especially dangerous and potentially fatal in combination with alcohol and other depressants.[3] Mephenesin was the inspiration for the synthesis of a derivative of 1,3-propanediol, meprobamate, by Bernard Ludwig and Frank Berger,[4] the first tranquilizer to see widespread clinical use. Mephenesin is no longer available in North America but is used in Italy and a few other countries.[5] Its use has largely been replaced by the related drug methocarbamol, which is better absorbed.[6]
Mephenesin may be an NMDA receptor antagonist.[7] Mephenesin was previously used in France as an OTC muscle relaxant called Décontractyl but was taken out of production by Sanofi Aventis and due to a French Health Ministry decree in July 2019. Mephenesin is, however, still available in Italy.
^Berger FM (December 1947). "The mode of action of myanesin". British Journal of Pharmacology and Chemotherapy. 2 (4): 241–50. doi:10.1111/j.1476-5381.1947.tb00341.x. PMC 1509790. PMID 19108125.
^"Mephenesin". MIMS.
^Ban TA (2006). "The role of serendipity in drug discovery". Dialogues in Clinical Neuroscience. 8 (3): 335–44. doi:10.31887/DCNS.2006.8.3/tban. PMC 3181823. PMID 17117615.
^"Mephenesin". Drugs.com.
^Huf, Ernst; et al. (1959). "Comparative Plasma Levels of Mephenesin, Mephenesin Carbamate and Methocarbamol". Proceedings of the Society for Experimental Biology and Medicine. 102 (2). Experimental Biology & Medicine: 276–7. doi:10.3181/00379727-102-25218. PMID 14403806. S2CID 37483102. Retrieved 8 January 2014.
^Keshavarz M, Showraki A, Emamghoreishi M (2013). "Anticonvulsant Effect of Guaifenesin against Pentylenetetrazol-Induced Seizure in Mice". Iran J Med Sci. 38 (2): 116–21. PMC 3700057. PMID 23825891.
Mephenesin (INN), also called myanesin, is a centrally acting muscle relaxant. It can be used as an antidote for strychnine poisoning. Mephenesin however...
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Wallace Laboratories. He also discovered the 'tranquilising' effects of mephenesin in rodents while working at a laboratory in the United Kingdom, and campaigned...
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