Drug intelligence / Profile preview

thiocolchicoside

Development stage
Phase 4
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intramuscular
01

Overview

Thiocolchicoside is a semisynthetic derivative of colchicoside, itself a glucoside from the Colchicum autumnale plant. It is classified as a muscle relaxant with anti-inflammatory and analgesic properties. Thiocolchicoside is primarily used for the symptomatic treatment of painful muscle spasms associated with musculoskeletal conditions such as acute or chronic back pain, neck pain, postoperative pain, ankylosing spondylitis, rheumatoid arthritis, joint disease, vertebral damage, traumatic injuries, nerve conditions (e.g., persistent torticollis), and other orthopedic or rheumatic disorders[1][2][3][5]. Its mechanism of action involves interaction with gamma-aminobutyric acid type A (GABA-A) receptor and strychnine-sensitive glycine receptor in the central nervous system; it acts mainly as an antagonist at Gamma-aminobutyric acid type A receptor but also exhibits partial agonist-like effects on inhibitory neurotransmission[2][6]. This leads to reduced muscle tone and spasticity. Due to safety concerns including potential genotoxicity and epileptogenic risk (convulsant activity), regulatory agencies have restricted its use to short-term adjuvant therapy for adults[5].

Brand names
MuscorilMyorilNeoflax
Other names
thiocolchicosidethiocolchicine 2-glucoside analogthiocolchicine2-glucoside analogthiocolchicine-2-glucoside analog
02

Targets

GLRA1 (Glycine receptor subunit Alpha-1)GABRR (GABA-A receptor subunit rho)

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