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Thiocolchicoside
| File:Thiocolchicoside.png | |
| Systematic (IUPAC) name | |
|---|---|
| N-[(7S)-3-(β-D-Glucopyranosyloxy)-1,2-dimethoxy-10-(methylsulfanyl)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| |
| Oral, Topical, IM | |
| Pharmacokinetic data | |
| Bioavailability | 25%[1] |
| Half-life | 5-6 hours[1][2] |
| Identifiers | |
| 602-41-5 7px | |
| M03BX05 | |
| PubChem | CID 72067 |
| UNII | T1X8S697GT 7px |
| KEGG | D07276 7px |
| ChEMBL | CHEMBL1705373 7px |
| Chemical data | |
| Formula | C27H33NO10S |
| 563.618 g/mol | |
| |
| 14px (what is this?) (verify) | |
Thiocolchicoside (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects.[3][4][5][6] It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent.[7][8] It has powerful convulsant activity and should not be used in seizure-prone individuals.[9][10][11]
Side effects
Side effect of thiocolchicoside can include nausea, somnolence, allergy and vasovagal reactions.[12]
Although muscle relaxant have major side effect of Sedation, but Thiocholchicoside is free from sedation effect possible due to non-interference with nicotinic receptors.[citation needed]
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.[citation needed] Therefore recommended oral dose should not exceed 7 days and intramuscular dose duration should not exceed 5 days.[medical citation needed] Local skin preparations are less toxic.
References
- ^ a b Perucca E, Poitou P, Pifferi G (1995). "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. PMID 8983937. doi:10.1007/bf03190249.
- ^ Sandouk P, Bouvier d'Yvoire M, Chretien P, Tillement JP, Scherrmann JM (January 1994). "Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers". Biopharmaceutics & Drug Disposition 15 (1): 87–92. PMID 8161719. doi:10.1002/bdd.2510150108.
- ^ Tüzün F, Unalan H, Oner N et al. (September 2003). "Multicenter, randomized, double-blinded, placebo-controlled trial of thiocolchicoside in acute low back pain". Joint, Bone, Spine : Revue Du Rhumatisme 70 (5): 356–61. PMID 14563464. doi:10.1016/S1297-319X(03)00075-7.
- ^ Ketenci A, Basat H, Esmaeilzadeh S (July 2009). "The efficacy of topical thiocolchicoside (Muscoril) in the treatment of acute cervical myofascial pain syndrome: a single-blind, randomized, prospective, phase IV clinical study". Journal of the Turkish Society of Algology 21 (3): 95–103. PMID 19780000.
- ^ Soonawalla DF, Joshi N (May 2008). "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. PMID 18839644.
- ^ Ketenci A, Ozcan E, Karamursel S (July 2005). "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. PMID 15963201. doi:10.1111/j.1742-1241.2004.00454.x.
- ^ Carta M, Murru L, Botta P et al. (September 2006). "The muscle relaxant thiocolchicoside is an agonist of GABAA receptor function in the central nervous system". Neuropharmacology 51 (4): 805–15. PMID 16806306. doi:10.1016/j.neuropharm.2006.05.023.
- ^ Mascia MP, Bachis E, Obili N et al. (March 2007). "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. PMID 17234181. doi:10.1016/j.ejphar.2006.11.076.
- ^ De Riu PL, Rosati G, Sotgiu S, Sechi G (August 2001). "Epileptic seizures after treatment with thiocolchicoside". Epilepsia 42 (8): 1084–6. PMID 11554898. doi:10.1046/j.1528-1157.2001.0420081084.x.
- ^ Giavina-Bianchi P, Giavina-Bianchi M, Tanno LK, Ensina LF, Motta AA, Kalil J (June 2009). "Epileptic seizure after treatment with thiocolchicoside". Therapeutics and Clinical Risk Management 5 (3): 635–7. PMC 2731019. PMID 19707540. doi:10.2147/tcrm.s4823.
- ^ Sechi G, De Riu P, Mameli O, Deiana GA, Cocco GA, Rosati G (October 2003). "Focal and secondarily generalised convulsive status epilepticus induced by thiocolchicoside in the rat". Seizure : the Journal of the British Epilepsy Association 12 (7): 508–15. PMID 12967581. doi:10.1016/S1059-1311(03)00053-0.
- ^ "Thiocolchicoside-induced liver injury". Mar 2011. Retrieved Dec 2014.
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