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Muscle relaxant
Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It can also be administered for acute pain in general and for tension headache (muscle contraction headache). It acts on the spinal cord by depressing reflexes. It is sold under the brand names Lorzone, Paraflex and Muscol and in combination form as Parafon Forte, a combination of chlorzoxazone and acetaminophen (paracetamol). Possible side effects include dizziness, lightheadedness, malaise, nausea, vomiting. In rare cases, chlorzoxazone may cause severe liver dysfunction. On the other hand, chlorzoxazone may reduce the liver toxicity of acetaminophen by competitive inhibition.
Like metaxalone, its mechanism of action is still in question. It is believed that metaxalone works by altering serotonin levels and acting as a mild MAO inhibitor. The mechanism of action of chlorzoxazone is thought to act on GABAA and GABAB receptors and voltage-gated calcium channels to a degree. General central nervous systemdepression is the only currently accepted aspect to its medical benefits. Elucidation of the exact mechanism of action is ongoing but there is limited study due to the existence of more effective, safe muscle relaxants (e.g., diazepam, cyclobenzaprine, tizanidine), greatly limiting the potential benefit of identifying novel compounds which share chlorzoxazone's mechanism of action.
Dong DL, Luan Y, Feng TM, Fan CL, Yue P, Sun ZJ, et al. (September 2006). "Chlorzoxazone inhibits contraction of rat thoracic aorta". European Journal of Pharmacology. 545 (2–3): 161–166. doi:10.1016/j.ejphar.2006.06.063. PMID16859676.
Park JY, Kim KA, Park PW, Ha JM (January 2006). "Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe". Journal of Clinical Pharmacology. 46 (1): 109–114. doi:10.1177/0091270005282635. PMID16397290. S2CID20092326.
