Thiocolchicoside
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
Legal status
  • Prescription only
Routes Oral, Topical, IM
Pharmacokinetic data
Bioavailability 25%[1]
Half-life 5-6 hours[1][2]
Identifiers
CAS number  YesY
ATC code M03
PubChem
UNII  YesY
KEGG  YesY
ChEMBL  N
Chemical data
Formula C27H33NO10S 
Mol. mass 563.618 g/mol
 N   

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 skeletal muscle relaxants may include: sedation, drowsiness, blurred or double vision,constipation or diarrhea, dizziness and drowsiness, nervousness and confusion, dry mouth, dyspepsia (chronic or recurrent pain in the upper abdomen, upper abdominal fullness, and feeling full earlier than expected when eating), fatigue, headache, heartburn, hiccups and nausea, insomnia, stomach cramps, trembling, vomiting, and weakness; and possible dependence following long-term use. Recent updates have expressed safety concerns related to aneuploidy (an abnormal number or arrangement of chromosomes) which is a risk factor for teratogenicity, spontaneous abortion or male infertility.

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

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. ^ 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.  
  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.  
  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.  
  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.  
  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.  
  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.  
  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.  
  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.  
  9. ^ De Riu PL, Rosati G, Sotgiu S, Sechi G (August 2001). "Epileptic seizures after treatment with thiocolchicoside". Epilepsia 42 (8): 1084–6.  
  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.  
  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.