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Thiocolchicoside

Introduction

Overview

Overview

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 effects

Side effect of thiocolchicoside can include nausea, somnolence, allergy and vasovagal reactions.[12]

Although Musle relaxant have major side effect of Sedation, but Thiocholchicoside is free from sedation effect possible due to non-interference with nicotinic receptors.

Pharmacokinetics

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.Template:Medcn Local skin preparations are less toxic.

References

References

  1. ↑ 1.0 1.1 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. PMIDΒ 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. PMIDΒ 8161719.
  3. ↑ TΓΌzΓΌn 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, SpineΒ : Revue Du Rhumatisme. 70 (5): 356–61. doi:10.1016/S1297-319X(03)00075-7. PMIDΒ 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. PMIDΒ 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. PMIDΒ 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. PMIDΒ 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. PMIDΒ 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. PMIDΒ 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. PMIDΒ 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. PMCΒ 2731019. PMIDΒ 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”. SeizureΒ : the Journal of the British Epilepsy Association. 12 (7): 508–15. doi:10.1016/S1059-1311(03)00053-0. PMIDΒ 12967581.
  12. ↑ “Thiocolchicoside-induced liver injury”. Mar 2011. Retrieved Dec 2014. Check date values in: |accessdate= (help)

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