Thiocolchicoside

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Thiocolchicoside
Thiocolchicoside.png
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]ethanamide
Clinical data
AHFS/Drugs.com International Drug Names
Legal status
  • ℞ (Prescription only)
Routes of
administration		 Oral, Topical, IM
Pharmacokinetic data
Bioavailability 25%[1]
Biological half-life 5-6 hours[1][2]
Identifiers
CAS Number 602-41-5 YesY
ATC code M03BX05 (WHO)
PubChem CID: 72067
UNII T1X8S697GT YesY
KEGG D07276 YesY
ChEMBL CHEMBL1705373 N
Chemical data
Formula C27H33NO10S
Molecular mass 563.618 g/mol
  • 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=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
 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.[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.[medical citation needed] Local skin preparations are less toxic.

References

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