Thiocolchicoside

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Thiocolchicoside
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
Legal status
  • (Prescription only)
Routes of
administration
Oral, Topical, IM
Pharmacokinetic data
Bioavailability 25%[1]
Biological half-life 5-6 hours[1][2]
Identifiers
CAS Registry Number 602-41-5 YesY
ATC code M03BX05
PubChem CID: 72067
UNII T1X8S697GT YesY
KEGG D07276 YesY
ChEMBL CHEMBL1705373 N
Chemical data
Formula C27H33NO10S
Molecular mass 563.618 g/mol
 N (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[edit]

Side effect of thiocolchicoside can include nausea, 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[edit]

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[edit]

  1. ^ 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. doi:10.1007/bf03190249. PMID 8983937. 
  2. ^ 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. doi:10.1002/bdd.2510150108. PMID 8161719. 
  3. ^ 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. doi:10.1016/S1297-319X(03)00075-7. PMID 14563464. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. doi:10.1111/j.1742-1241.2004.00454.x. PMID 15963201. 
  7. ^ 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. doi:10.1016/j.neuropharm.2006.05.023. PMID 16806306. 
  8. ^ 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. doi:10.1016/j.ejphar.2006.11.076. PMID 17234181. 
  9. ^ De Riu PL, Rosati G, Sotgiu S, Sechi G (August 2001). "Epileptic seizures after treatment with thiocolchicoside". Epilepsia 42 (8): 1084–6. doi:10.1046/j.1528-1157.2001.0420081084.x. PMID 11554898. 
  10. ^ 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. doi:10.2147/tcrm.s4823. PMC 2731019. PMID 19707540. 
  11. ^ 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. doi:10.1016/S1059-1311(03)00053-0. PMID 12967581. 
  12. ^ "Thiocolchicoside-induced liver injury". Mar 2011. Retrieved Dec 2014.