For the use of Registered Medical Practitioner or Hospital or Laboratory only (June-2025)

THIOSIDE*4

(Thiocolchicoside Capsules IP)

COMPOSITION:

Each hard gelatin capsule contains: Thiocolchicoside IP  4 mg

 CLINICAL PHARMACOLOGY:

Mechanism of action

Thiocolchicoside is a synthetic sulfur derivative of colchicoside, a naturally occurring glucoside contained in the Colchicum autumnale plant. Thiocolchicoside is a potent muscle relaxant with selective affinity for GABA-A receptors. It acts by activating GABAergic inhibitory pathways, helping to relieve muscular contractures.

PHARMACOKINETICS

Absorption:Oral bioavailability is ~25%. After intramuscular administration, thiocolchicoside Cmax occur in 30 min and reach values of 113 ng/mL after a 4 mg dose and 175 ng/mL after a 8 mg dose. The corresponding AUC values are 283 and 417 ng·h/mL, respectively. The active metabolite SL18.0740 appears at lower concentrations, with a Cmax of 11.7 ng/mL at 5 hours post-administration and an AUC of 83 ng·h/mL.              

Distribution:The apparent volume of distribution of thiocolchicoside is estimated to be approximately 42.7 L after an intramuscular injection of 8 mg.The binding of 3H-colchicine and its derivative 3H-thiocolchicoside to human serum, purified human proteins, as well as red blood cells was studied using equilibrium dialysis and centrifugation. Binding of colchicine and thiocolchicoside to human serum was 38.9 C +/- 4.7 and 12.8 C +/- 5.3%, respectively, to albumin.                                                                             

Metabolism: Thiocolchicoside is rapidly absorbed after oral administration and metabolized into 3 main metabolites. In the intestines, Thiocolchicoside is metabolized to 3-demethylcolchicine which is further metabolized in circulation by either conjugation to 3-O-glucurono-demethylcolchicine (active metabolite) or demethylated to didemethylcolchicine (inactive metabolite)                                                         Elimination:Thiocolchicoside is not eliminated unchanged, rather as one of three metabolites found in either faeces (~79 %) or in urine 20%. 3- demethylcolchicine (M2) and 3-O-glucurono-demethylcolchicine (M1) are found in both urine and faeces, whereas di-demethylcolchicine is found only in faeces. 

INDICATIONS AND USAGE:

Adjuvant treatment of painful muscle contractures in acute spinal pathology in adults and adolescents with age of 16 years and older.

 DOSAGE AND ADMINISTRATION:

For oral formulation of 4mg: The recommended and maximum dose is 8 mg every 12 hours (i.e. 16 mg daily). The length of treatment is limited to 7 consecutive days. Doses higher than the recommended doses or long-term use should be avoided.

 WARNINGS AND PRECAUTIONS:

In patients with epilepsy or seizure risks, as thiocolchicoside may predispose to seizures

Cytolytic or cholestatic hepatitis reported with thiocolchicoside during post-market

In case of diarrhoea, reduce the posology.

Patients with intolerance to galactose, total lactase deficiency, or glucose and galactose malabsorption syndrome (rare hereditary diseases) should not take this medicine.

ADVERSE REACTIONS:

Side effects of thiocolchicoside can include nausea, allergy and vasovagal reactions. Liver injury, pancreatitis, seizures, blood cell disorders, severe cutaneous disorders, rhabdomyolysis, and reproductive disorders have all been recorded.

 USE IN SPECIFIC POPULATIONS:

Pregnancy: Thiocolchicoside is contraindicated during pregnancy and in women of childbearing age.

OVERDOSAGE:

Digestive signs of the diarrhoea or vomiting type are possible. In case of an overdose, monitoring by a physician and symptomatic treatment are recommended. 

PRESENTATION: Carton containing 10 strips each containing 10 capsules.