Instructions for Tionex 8 mg tablets No. 14
Composition
active ingredient: thiocolchicoside;
Excipients: lactose monohydrate; microcrystalline cellulose (type 101); microcrystalline cellulose (type 102); povidone (type K30); colloidal anhydrous silica; crospovidone (type A); magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: round tablets with a biconvex surface of yellow color.
Pharmacotherapeutic group
Muscle relaxants with a central mechanism of action. Thiocolchicoside. ATC code M03B X05.
Pharmacological properties
Pharmacodynamics.
Thiocolchicoside is a semi-synthetic sulfide analogue of the natural glycoside colchicine, acts as a central muscle relaxant, does not exhibit curare-like effects, since it acts through the central nervous system (CNS), and not through the neuromuscular junction. It reduces or significantly inhibits the contractile activity of spasmodic muscles, reduces passive muscle resistance during stretching, and also reduces or eliminates residual spasticity. The action of thiocolchicoside, according to studies in 2003 and 2007, is associated with a selective agonist effect on glycinergic receptors of the brainstem and spinal cord. Thiocolchicoside does not affect voluntary movements, does not cause paralysis, which eliminates the risk of respiratory function impairment, acts as an antagonist of GABA receptors in the cerebral cortex, which is associated with the risk of seizures and increased convulsive readiness. Thiocolchicoside does not affect the cardiovascular system.
Pharmacokinetics.
Absorption
After oral administration of thiocolchicoside, 2 of its metabolites are detected in the blood plasma: the pharmacologically active metabolite SL18.0740, which has the effectiveness of unchanged thiocolchicoside, and the inactive metabolite SL59.0955. The maximum concentration of these metabolites in the blood plasma (Cmax) is observed within 1 hour after administration of thiocolchicoside. After taking a single dose of 8 mg of thiocolchicoside, the Cmax and area under the pharmacokinetic curve (AUC) for SL18.0740 are 60 ng/ml and 130 ng∙g/ml, respectively. For SL59.0955, these indicators are much lower: Cmax is approximately 13 ng/ml, and AUC is in the range from 15.5 ng∙g/ml (up to 3 hours) to 39.7 ng∙g/ml (up to 24 hours).
Distribution
Data on the distribution of both metabolites are not available.
Metabolism
After oral administration, thiocolchicoside is first metabolized to the aglycone-3-demethylthiocolchicine or SL59.0955, which occurs mainly in the intestine. This is attributed to the absence of unchanged thiocolchicoside in the blood plasma after oral administration. The metabolite SL59.0955 is glucuronized to SL18.0740, which has the potency of unchanged thiocolchicoside, thus providing the pharmacological activity of oral thiocolchicoside. SL59.0955 is also demethylated to didemethylthiocolchicine.
Breeding
After oral administration, metabolites are excreted mainly in the feces (79%) and urine (20%). Thiocolchicoside is not excreted unchanged in the urine or feces. The metabolites SL18.0740 and SL59.0955 are found in the urine and feces, while didemethylthiocolchicine is excreted only in the feces.
After oral administration of thiocolchicoside, the half-life of the metabolite SL18.0740 is 3.2–7 hours, and that of the metabolite SL59.0955 is on average 0.8 hours.
Clinical characteristics.
Indication
Adjuvant therapy of painful muscle contractures in cases of acute spinal pathologies in adults and adolescents aged 16 years and older.
Contraindication
Tionex should not be used:
Interaction with other medicinal products and other types of interactions
There is no information on interactions. However, caution is recommended when taking it simultaneously with other muscle relaxants.
When used simultaneously with drugs that depress the CNS, including alcohol, antihypertensive drugs, curare-like drugs, increased muscle relaxation and CNS depression, and the development of hypotension are possible.
When used simultaneously with anticoagulants, the risk of bleeding increases.
Application features
Thiocolchicoside should be used with caution in patients with epilepsy or at risk of seizures.
The occurrence of seizures requires discontinuation of treatment.
If diarrhea occurs, the dosage should be reduced. If necessary, the tablets can be used together with antacids.
The metabolite of thiocolchicoside (SL59.0955) may cause aneuploidy (change in the number of chromosomes in dividing cells) in animal studies.
Aneuploidy is considered a risk factor for teratogenicity, embryo/fetal toxicity, miscarriage, reduced fertility and a potential risk factor for cancer. As a precaution, exceeding the recommended dose of the drug or prolonged use should be avoided (see section "Method of administration and dosage").
Patients should be well informed about the potential risks to possible pregnancy and about the effective contraceptive methods that should be used.
The medicine contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use it.
Use during pregnancy or breastfeeding
Information on the use of thiocolchicoside in pregnant women is limited, so the potential risk to the embryo and fetus is unknown.
Animal studies have shown teratogenic effects of this drug.
Tionex is contraindicated during pregnancy and in women of reproductive age not using adequate contraception (see section "Contraindications").
Breastfeeding period
The use of thiocolchicoside is contraindicated during breastfeeding as it passes into breast milk (see section "Contraindications").
Fertility
Fertility studies in animals have shown no changes in fertility at doses up to 12 mg/kg, i.e. at doses that did not cause clinical effects. Thiocolchicoside and its metabolites are aneugenic at various concentration levels, which is a risk factor for impaired fertility in humans.
Ability to influence reaction speed when driving vehicles or other mechanisms
There are no clinical study data indicating the ability of thiocolchicoside to affect driving or other mechanisms.
Despite the fact that drowsiness is considered a very rare manifestation, the possibility of its occurrence should be taken into account when planning dangerous activities.
Method of administration and doses
Method of application
Take orally with a glass of water.
Doses
The recommended dose is 8 mg every 12 hours (16 mg of thiocolchicoside is also the maximum daily dose). The duration of treatment should not exceed 7 consecutive days. Exceeding the recommended dose or prolonged use should be avoided (see section "Special instructions").
Children.
The drug is contraindicated in children and adolescents under 16 years of age.
Overdose
Symptoms
Gastrointestinal symptoms, such as diarrhea or vomiting, may occur.
Treatment
In case of overdose, close medical supervision and symptomatic treatment are recommended.
Adverse reactions
Adverse reactions are listed by organ system and by frequency: rare (≥ 1/10,000 and < 1/1,000), very rare (< 1/10,000), frequency unknown (cannot be estimated from the available information).
From the immune system.
On the skin and subcutaneous tissue.
From the gastrointestinal tract.
From the nervous system.
Expiration date
2 years.
Storage conditions
The medicine does not require any special storage conditions. Keep out of the reach of children.
Packaging
14 tablets in a blister; 1 blister in a cardboard box.
Vacation category
According to the recipe.
Producer
Biofarm Ltd. / Biofarm Sp. z oo
Address
Walbrzyska str. 13, 60-198 Poznan, Poland.
