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(RS)-thiocolchicoside

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Also known as N-[1,2-dimethoxy-10-(methylthio)-9-oxo-3-{[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy}-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide, thiocolchicoside

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a semi-synthetic derivative of colchicine, used as muscle relaxant with anti-inflammatory and analgesic effects. Its mechanism of action is unknown, but it is believed to act via antagonism of nicotinic acetylcholine receptors (nAchRs). However, it also appears to be a competitive antagonist of GABAA and glycine receptors. As such, it has powerful convulsant activity and should not be used in seizure-prone individuals.

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Encyclopedic overview

5 sections
Contents
  • Medical uses
  • Low back pain
  • Side effects
  • Pharmacokinetics
  • References

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a semi-synthetic derivative of colchicine, used as muscle relaxant with anti-inflammatory and analgesic effects. Its mechanism of action is unknown, but it is believed to act via antagonism of nicotinic acetylcholine receptors (nAchRs). However, it also appears to be a competitive antagonist of GABAA and glycine receptors. As such, it has powerful convulsant activity and should not be used in seizure-prone individuals.

== Medical uses == === Low back pain === In low back pain, thiocolchicoside is efficacious in reducing pain intensity, improving physical flexibility as seen in decreasing the distance from the hands to the floor when leaning forward without bending the knees (finger-floor distance), and reducing the total consumption of paracetamol. Thiocolchicoside administration also leads to a reduction in muscle spasm during palpation, an improvement in the overall assessment of patients with low back pain, and an enhancement in their ability to perform daily activities.

Excerpted from Wikipedia’s “(RS)-thiocolchicoside” article, available under the CC BY-SA 4.0 licence.