Thiocolchicoside

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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-[(7S)-3-(β-D-Glucopyranosyloxy)-1,2-dimethoxy-10-(methylsulfanyl)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide;
CAS Number	602-41-5 ;
PubChem CID	72067;
UNII	T1X8S697GT;
KEGG	D07276 ;
ChEMBL	ChEMBL1705373 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C27H33NO10S
Molar mass	563.618 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C(N[C@@H]4C1=C\C(=O)C(/SC)=C\C=C1c3c(cc(O[C@@H]2O[C@@H]([C@@H](O)[C@H](O)[C@H]2O)CO)c(OC)c3OC)CC4)C;
	InChI InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16?,19-,22-,23+,24-,27-/m1/s1 ; Key:LEQAKWQJCITZNK-MSQQGMGVSA-N ;
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Thiocolchicoside
Clinical data
ATC code	M03BX05 (WHO) ;
Identifiers
	IUPAC name N-[1,2-dimethoxy-10-methylsulfanyl-9-oxo-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6,7-dihydro-5H-benzo[d]heptalen-7-yl]acetamide;
PubChem CID	72067;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C27H33NO10S
Molar mass	563.618 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects.^[3]^[4]^[5]^[6] It acts as a competitive GABA_A 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, 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.^{[citation needed]}

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.^{[citation needed]} 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

↑ ^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. PMID 8983937.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ "Thiocolchicoside-induced liver injury". Mar 2011. Retrieved Dec 2014. Check date values in: |accessdate= (help)

[pmid8983937-1] 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. PMID 8983937.

[pmid8161719-2] 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.

[pmid14563464-3] 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.

[pmid19780000-4] 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.

[pmid18839644-5] 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.

[pmid15963201-6] 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.

[pmid16806306-7] 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.

[pmid17234181-8] 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.

[pmid11554898-9] 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.

[pmid19707540-10] 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.

[pmid12967581-11] 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: |accessdate= (help)

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v t e Skeletal Muscle relaxants (M03)
Peripherally acting (primarily antinicotinic, neuromuscular-blocking drugs)	Template:Navbox subgroup
Centrally Acting	Template:Navbox subgroup
Directly acting	Dantrolene

v t e Analgesic products (N02A, N02B)
Opioids See also: Opioids template	Alphaprodine · Anileridine · Buprenorphine · Butorphanol · Codeine · Dextromoramide · Dextropropoxyphene · Dezocine · Desomorphine · Diamorphine · Dihydrocodeine · Dihydromorphine · Fentanyl · Hydrocodone · Hydromorphone · Ketobemidone · Levorphanol · Meptazinol · Methadone · Morphine · Nalbuphine · Nicomorphine · Opium · Oxycodone · Oxymorphone · Pethidine · Pentazocine · Pethidine · Piminodine · Piritramide · Tilidine · Tramadol · Tapentadol
Salicylic acid and derivatives	Aspirin (Acetylsalicylic Acid) · Benorylate · Diflunisal · Ethenzamide · Magnesium Salicylate · Salicin · Salicylamide · Salsalate · See also: NSAIDs
Pyrazolones	Ampyrone/Aminophenazone · Metamizole · Phenazone
Cannabinoids	Cannabis · Tetrahydrocannabinol · AM404
Anilides	Paracetamol (acetaminophen) · Phenacetin · Propacetamol
Non-Salicylate Non-Steroidal Anti-Inflammatories See also: NSAIDs template	Template:Navbox subgroup
Atypical, Adjunct & Miscellaneous	Bicifadine · Clonidine · Cyclobenzaprine · Duloxetine · Flupirtine · Gabapentin · Nefopam · Orphenadrine · Trazadone · Ziconotide

Clinical data
ATC code	M03BX05 (WHO)
Identifiers
IUPAC name N-[1,2-dimethoxy-10-methylsulfanyl-9-oxo-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6,7-dihydro-5H-benzo[d]heptalen-7-yl]acetamide
PubChem CID	72067
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C₂₇H₃₃NO₁₀S
Molar mass	563.618 g/mol

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%^[1]
Elimination half-life	5-6 hours^[1]^[2]
Identifiers
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
CAS Number	602-41-5^Y
PubChem CID	72067
UNII	T1X8S697GT
KEGG	D07276^Y
ChEMBL	ChEMBL1705373^N
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C₂₇H₃₃NO₁₀S
Molar mass	563.618 g/mol
3D model (JSmol)	Interactive image
SMILES O=C(N[C@@H]4C1=C\C(=O)C(/SC)=C\C=C1c3c(cc(O[C@@H]2O[C@@H]([C@@H](O)[C@H](O)[C@H]2O)CO)c(OC)c3OC)CC4)C
InChI InChI=1S/C27H33NO10S/c1-12(30)28-16-7-5-13-9-18(37-27-24(34)23(33)22(32)19(11-29)38-27)25(35-2)26(36-3)21(13)14-6-8-20(39-4)17(31)10-15(14)16/h6,8-10,16,19,22-24,27,29,32-34H,5,7,11H2,1-4H3,(H,28,30)/t16?,19-,22-,23+,24-,27-/m1/s1^N Key:LEQAKWQJCITZNK-MSQQGMGVSA-N^N
^NY (what is this?) (verify)

Thiocolchicoside

Overview

Side effects

Pharmacokinetics

References

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