Chemistry:Thiocolchicoside
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral, Topical, IM |
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| Bioavailability | 25%[1] |
| Elimination half-life | 5-6 hours[1][2] |
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| Formula | C27H33NO10S |
| Molar mass | 563.62 g·mol−1 |
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Thiocolchicoside (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects.[3][4][5][6] Its mechanism of action is unknown, but it is believed to be act via antagonism of nicotinic acetylcholine receptors (nAchRs). However, it also appears to be a competitive antagonist of GABAA and glycine receptors.[7][8] As such, it has powerful convulsant activity and should not be used in seizure-prone individuals.[9][10][11]
Side effects
Side effects of thiocolchicoside can include nausea, allergy and vasovagal reactions.[12] Liver injury, pancreatitis, seizures, blood cell disorders, severe cutaneous disorders, rhabdomyolysis, and reproductive disorders have all been recorded in the French and European pharmacovigilance databases and in the periodic updates that the companies concerned submit to regulatory agencies. These data do not specify the frequency of the disorders nor do they identify the most susceptible patient populations. Thiocolchicoside is teratogenic in experimental animals and also damages chromosomes. Human data are limited to a follow-up of about 30 pregnant women (no major malformations) and reports of altered spermatogenesis, including cases of azoospermia. In practice, there is no justification for exposing patients to the adverse effects of thiocolchicoside. It is better to use an effective, well-known analgesic for patients complaining of muscle pain, starting with paracetamol.[13]
Although muscle relaxants may have the major side effect of sedation, thiocolchicoside is free from sedation effects, likely due to its lack of potentiation of GABAA receptors.[7]
Pharmacokinetics
Thiocolchicoside is broken down in the body to a metabolite called 3-demethylthiocolchicine (also known as SL59.0955 or M2) that could damage dividing cells therefore inducing toxicity in the embryo, neoplastic changes and fertility reduction in males.[14] Therefore, recommended oral dose should not exceed 7 days and intramuscular dose duration should not exceed 5 days.[15] Local skin preparations are less toxic.
References
- ↑ 1.0 1.1 "Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers". European Journal of Drug Metabolism and Pharmacokinetics 20 (4): 301–5. 1995. doi:10.1007/bf03190249. PMID 8983937.
- ↑ "Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers". Biopharmaceutics & Drug Disposition 15 (1): 87–92. January 1994. doi:10.1002/bdd.2510150108. PMID 8161719.
- ↑ "Multicenter, randomized, double-blinded, placebo-controlled trial of thiocolchicoside in acute low back pain". Joint, Bone, Spine 70 (5): 356–61. September 2003. doi:10.1016/S1297-319X(03)00075-7. PMID 14563464.
- ↑ "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 21 (3): 95–103. July 2009. PMID 19780000. http://www.journalagent.com/pubmed/linkout.asp?ISSN=1300-0012&PMID=19780000.
- ↑ "Efficacy of thiocolchicoside in Indian patients suffering from low back pain associated with muscle spasm". Journal of the Indian Medical Association 106 (5): 331–5. May 2008. PMID 18839644.
- ↑ "Assessment of efficacy and psychomotor performances of thiocolchicoside and tizanidine in patients with acute low back pain". International Journal of Clinical Practice 59 (7): 764–70. July 2005. doi:10.1111/j.1742-1241.2004.00454.x. PMID 15963201.
- ↑ 7.0 7.1 "The muscle relaxant thiocolchicoside is an agonist of GABAA receptor function in the central nervous system". Neuropharmacology 51 (4): 805–15. September 2006. doi:10.1016/j.neuropharm.2006.05.023. PMID 16806306.
- ↑ "Thiocolchicoside inhibits the activity of various subtypes of recombinant GABA(A) receptors expressed in Xenopus laevis oocytes". European Journal of Pharmacology 558 (1–3): 37–42. March 2007. doi:10.1016/j.ejphar.2006.11.076. PMID 17234181.
- ↑ "Epileptic seizures after treatment with thiocolchicoside". Epilepsia 42 (8): 1084–6. August 2001. doi:10.1046/j.1528-1157.2001.0420081084.x. PMID 11554898.
- ↑ "Epileptic seizure after treatment with thiocolchicoside". Therapeutics and Clinical Risk Management 5 (3): 635–7. June 2009. doi:10.2147/tcrm.s4823. PMID 19707540.
- ↑ "Focal and secondarily generalised convulsive status epilepticus induced by thiocolchicoside in the rat". Seizure 12 (7): 508–15. October 2003. doi:10.1016/S1059-1311(03)00053-0. PMID 12967581.
- ↑ "Thiocolchicoside-induced liver injury". Clinics 66 (3): 521–2. Mar 2011. doi:10.1590/s1807-59322011000300029. PMID 21552685.
- ↑ "Thiocolchicoside: review of adverse effects". Prescrire International 25 (168): 41–3. February 2016. PMID 27042729.
- ↑ "European Medicines Agency recommends restricting use of thiocolchicoside by mouth or injection". 17 September 2018. http://www.ema.europa.eu/ema/index.jsp?curl=pages/news_and_events/news/2013/11/news_detail_001967.jsp&mid=WC0b01ac058004d5c1.
- ↑ http://www.aifa.gov.it/en/content/thiocolchicoside-containing-products-systemic-use-important-information-regarding-indication[full citation needed]
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