Thiocolchicoside

Thiocolchicoside
Clinical data
AHFS/Drugs.com International Drug Names
Routes of
administration		 Oral, Topical, IM
ATC code M03BX05 (WHO)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 25%[1]
Biological half-life 5-6 hours[1][2]
Identifiers
CAS Number 602-41-5 YesY
PubChem (CID) 72067
UNII T1X8S697GT YesY
KEGG D07276 YesY
ChEMBL CHEMBL1705373 N
ECHA InfoCard 100.009.107
Chemical and physical data
Formula C27H33NO10S
Molar mass 563.618 g/mol
3D model (Jmol) Interactive image
 NYesY (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, allergy and vasovagal reactions.[12]

Although muscle relaxants may have the major side effect of sedation, thiocholchicoside is free from sedation effects possible due to non-interference with nicotinic receptors.

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. Therefore, recommended oral dose should not exceed 7 days and intramuscular dose duration should not exceed 5 days. Local skin preparations are less toxic.

References

  1. 1 2 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 2731019Freely accessible. 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. Check date values in: |access-date= (help)
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