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Thiocolchicoside

Clinical data
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral, Topical, IM
ATC code	M03BX05 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	25%
Elimination half-life	5-6 hours
Identifiers
IUPAC name N-heptalen-7-yl]acetamide
CAS Number	602-41-5
PubChem CID	72067
UNII	T1X8S697GT
KEGG	D07276
CompTox Dashboard (EPA)	DTXSID5045330
ECHA InfoCard	100.009.107
Chemical and physical data
Formula	C27H33NO10S
Molar mass	563.618 g/mol g·mol
3D model (JSmol)	Interactive image
SMILES O=C(N4C1=C\C(=O)C(/SC)=C\C=C1c3c(cc(O2O((O)(O)2O)CO)c(OC)c3OC)CC4)C
(verify)

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABA_A receptor antagonist and also inhibits glycine receptors with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.

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.

References

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. PMID 8983937.{{cite journal}}: CS1 maint: multiple names: authors list (link)
2. Sandouk P, Bouvier d'Yvoire M, Chretien P, Tillement JP, Scherrmann JM (1994). "Single-dose bioavailability of oral and intramuscular thiocolchicoside in healthy volunteers". Biopharmaceutics & Drug Disposition. 15 (1): 87–92. PMID 8161719. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
3. Tüzün F, Unalan H, Oner N; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
4. Ketenci A, Basat H, Esmaeilzadeh S (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
5. Soonawalla DF, Joshi N (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. {{cite journal}}: Unknown parameter |month= ignored (help)
6. Ketenci A, Ozcan E, Karamursel S (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
7. Carta M, Murru L, Botta P; et al. (2006). "The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system". Neuropharmacology. 51 (4): 805–15. doi:10.1016/j.neuropharm.2006.05.023. PMID 16806306. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
8. Mascia MP, Bachis E, Obili N; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
9. De Riu PL, Rosati G, Sotgiu S, Sechi G (2001). "Epileptic seizures after treatment with thiocolchicoside". Epilepsia. 42 (8): 1084–6. doi:10.1046/j.1528-1157.2001.0420081084.x. PMID 11554898. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
10. Giavina-Bianchi P, Giavina-Bianchi M, Tanno LK, Ensina LF, Motta AA, Kalil J (2009). "Epileptic seizure after treatment with thiocolchicoside". Therapeutics and Clinical Risk Management. 5 (3): 635–7. PMC 2731019. PMID 19707540. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
11. Sechi G, De Riu P, Mameli O, Deiana GA, Cocco GA, Rosati G (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

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