Instructions Thiozide tablets 8 mg No. 20
Composition
active ingredient: thiocolchicoside;
1 tablet contains thiocolchicoside 8 mg;
Excipients: copovidone, lactose monohydrate, pregelatinized starch, microcrystalline cellulose, colloidal anhydrous silicon dioxide, sodium stearyl fumarate.
Dosage form
Pills.
Main physicochemical properties: round, biconvex, yellow tablets with a break line on one side and engraved with "8" on the other side.
Pharmacotherapeutic group
Muscle relaxants with a central mechanism of action. ATC code M0ZV X05.
Pharmacological properties
Pharmacodynamics
Thiocolchicoside is a semisynthetic muscle relaxant derived from the glycoside colchicoside. It exhibits selective affinity for gamma-aminobutyric acid (GABA) and glycine receptors.
The muscle relaxant effect is manifested mainly at the supraspinal level, due to complex regulatory mechanisms; a glycinergic mechanism of action is also not excluded.
The binding of thiocolchicoside to GABA is qualitatively and quantitatively separated from its active metabolite, the glucuronidated derivative.
Thiocolchicoside and its derivatives do not have a sedative effect.
Pharmacokinetics
Absorption.
After taking a single dose of 8 mg of thiocolchicoside, the maximum concentration (Cmax) is reached within 30 minutes and reaches a value of 175 ng/ml. The area under the concentration-time curve (AUC) is 417 ng.hour/ml.
The pharmacologically active metabolite SL18.0740 is also detected at lower concentrations with a Cmax of 11.7 ng/ml, achieved 5 hours after dosing, and an AUC of 83 ng.hour/ml. No data are available for the inactive metabolite SL59.0955.
After oral administration of thiocolchicoside, only two metabolites are detected in the blood plasma: the pharmacologically active metabolite SL18.0740 and the inactive metabolite SL59.0955. The maximum plasma concentration of both metabolites of thiocolchicoside is reached after approximately 60 minutes. After a single oral dose of 8 mg, the Cmax and AUC values of the metabolite SL18.0740 are approximately 60 ng/ml and 130 ng.h/ml, respectively. For the metabolite SL59.0955, the values are much lower: Cmax is approximately 13 ng/ml and AUC ranges from 15.5 ng.h/ml (up to 3 hours) to 39.7 ng.h/ml (up to 24 hours).
Distribution.
The volume of distribution of thiocolchicoside is approximately 42.7 L after administration of 8 mg. Data on the volume of distribution of metabolites are not available.
Metabolism.
After oral administration, thiocolchicoside is rapidly metabolized to the aglycone-3-dimethylthiocolchicoside or SL59.0955. This is mainly due to intestinal metabolism, which explains the absence of unchanged thiocolchicoside after oral administration. The metabolite SL59.0955 is glucuronidated to SL18.0740, which has equivalent pharmacological activity to thiocolchicoside and thus provides the pharmacological activity after oral administration of thiocolchicoside. SL59.0955 is also demethylated to dimethylthiocolchicine.
Breeding.
After oral administration, 14C-thiocolchicoside is mainly excreted in the feces (79%), with only 20% in the urine. Thiocolchicoside is 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.
Indication
Symptomatic treatment of painful muscle contractures in spinal cord pathologies.
Contraindication
Hypersensitivity to the active substance or to other components of the drug;
pregnancy and breastfeeding;
use in women of childbearing age who are not using contraception.
Interaction with other medicinal products and other types of interactions
There is no data on drug interactions. However, caution is recommended when taking it simultaneously with other muscle relaxants.
When used simultaneously with drugs that depress the central nervous system, including alcohol, antihypertensive drugs, and 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 is not recommended for use in children under 16 years of age.
If nausea occurs, the dose of the drug should be reduced.
Thiocolchicoside may cause seizures in patients with a predisposition to seizures or with epilepsy.
One of the metabolites of thiocolchicoside (SL59.0955) is known to induce aneuploidy (i.e. an unequal number of chromosomes in dividing cells) at concentrations close to those found in human plasma at a dose of 8 mg twice daily orally. Aneuploidy is a risk factor for teratogenicity, embryo-/fetotoxicity, spontaneous abortion, impaired male fertility, and cancer. Therefore, use of the drug in doses exceeding the recommended dose and for prolonged periods should be avoided.
The drug contains lactose monohydrate, therefore patients with rare hereditary forms of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.
Use during pregnancy or breastfeeding
The drug is contraindicated during pregnancy and breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
During the treatment period, caution should be exercised when driving vehicles or engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions, due to the possibility of drowsiness.
Method of administration and doses
The recommended dose is 8 mg every 12 hours (daily dose 16 mg). The duration of therapy should be up to 7 consecutive days.
Children
The drug should not be used in children under 16 years of age.
Overdose
There are no data on overdose.
Treatment: symptomatic, supportive therapy.
Adverse reactions
On the part of the immune system: anaphylactic reactions, urticaria, hypotension, anaphylactic shock after intramuscular injection, angioedema.
Skin and subcutaneous tissue disorders: allergic skin reactions (after intramuscular administration).
From the nervous system: drowsiness, lethargy, vasovagal syncope, occurring within a few minutes after application.
From the digestive tract: diarrhea, stomach pain, vomiting, nausea.
Expiration date
2 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging.
Keep out of reach of children.
Packaging
10 tablets in a blister, 1 or 2 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
Nobel Ilach Sanai ve Tijaret A.Sh.
Location of the manufacturer and address of its place of business.
Sankaklar Quarter, Eski Akcakoca Ave., No. 299, 81100 Duzce, Turkey.
Address
Sankaklar Quarter, Eski Akcakoca Ave., No. 299, 81100 Duzce, Turkey.
