Thiotriasoline^® (Tablets, Solution) Instructions for Use

ATC Code

A05BA (Drugs for the treatment of liver diseases)

Active Substance

Thiotriazoline (BP British Pharmacopoeia)

Clinical-Pharmacological Group

Metabolic drug with cardio- and hepatoprotective action

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

Antioxidant agent with hepatoprotective action and cardioprotective properties. Possesses anti-ischemic, membrane-stabilizing, and antioxidant activity.

The antioxidant properties are manifested due to the presence of thiol sulfur in the molecular structure of thiotriazoline, which has redox properties, and tertiary nitrogen, which binds excess hydrogen ions. Thiotriazoline reacts with reactive oxygen species and lipid radicals due to the pronounced reducing properties of the thiol group and prevents the initiation of reactive oxygen species by reactivating antiradical enzymes – superoxide dismutase, catalase, and glutathione peroxidase.

It prevents damage and death of hepatocytes, reduces the degree of fatty infiltration and the prevalence of centrilobular liver necrosis, activates the processes of reparative regeneration of hepatocytes, and normalizes protein, carbohydrate, lipid, and pigment metabolism in them. It accelerates the synthesis and secretion of bile and normalizes its chemical composition.

Thiotriazoline increases the compensatory activation of anaerobic glycolysis, reduces the inhibition of oxidation processes in the Krebs cycle while preserving ATP reserves. It activates the antioxidant system and inhibits lipid oxidation processes in ischemic areas of the myocardium, reduces the sensitivity of the heart muscle to catecholamines, prevents the progression of suppression of cardiac contractile activity, stabilizes and reduces the size of the myocardial necrosis and ischemia zone. It improves the rheological properties of blood by activating the fibrinolytic system.

Pharmacokinetics

When taken orally, the relative bioavailability is 64.5%, the half-absorption period is 0.28 h, T_1/2 is 1.3 h, C_max in blood plasma is noted after 1.18 h, binding to plasma proteins does not exceed 10%. After IV administration, C_max in blood plasma is noted after 0.1 h, after IM – after 0.84 h. It accumulates in significant amounts in the myocardium, liver, spleen, kidney, and rectal tissues, and in small amounts – in the lungs and small intestine. It is excreted mainly by the kidneys.

With IM administration, C_max in blood plasma is 399 µg/ml and is achieved after 0.84 h. With IV administration, C_max in blood plasma is achieved after 0.1 h. Absolute bioavailability is 34.6%.

Indications

For oral and parenteral administration: toxic liver lesions, including those of alcoholic, viral, and drug origin; chronic alcoholic hepatitis of minimal and moderate activity; chronic viral hepatitis, fatty liver disease, liver cirrhosis.

For oral administration: prevention of attacks in stable angina pectoris (as part of combination therapy).

ICD codes

Dosage Regimen

Solution

For chronic hepatitis, in the first 5 days of the disease, Thiotriazoline^® is administered IM at 2 ml of a 2.5% solution 2-3 times/day (2-3 times 50 mg), or IV at 4 ml of a 2.5% solution (100 mg) slowly at a rate of 2 ml/min or by drip at a rate of 20-30 drops/min (2 ampoules of 2.5% solution are dissolved in 150-250 ml of saline).

From day 5 to day 20 of treatment, Thiotriazoline^® is prescribed in tablets (100 mg 3 times/day). The course of treatment is 20-30 days.

Tablets

Orally. Thiotriazoline^® is prescribed 1 – 2 tablets 3-4 times/day for 20-30 days.

The duration of the treatment course is determined by the doctor individually depending on the severity and characteristics of the disease.

Adverse Reactions

From the digestive system very rarely – nausea, dryness of the oral mucosa, abdominal bloating.

From the cardiovascular system very rarely – tachycardia, increased blood pressure, arrhythmia, pain in the heart area.

From the nervous system very rarely – dizziness, tinnitus.

From the respiratory system very rarely – shortness of breath, bronchospasm.

From the skin very rarely – skin itching, skin hyperemia.

Allergic reactions very rarely – urticaria, hypersensitivity reactions, angioedema.

General reactions very rarely – general weakness, fever.

Contraindications

Renal failure, pregnancy, breastfeeding, children and adolescents under 18 years of age, hypersensitivity to thiotriazoline.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

Used for liver diseases as indicated.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Contraindication: children and adolescents under 18 years of age.

Geriatric Use

Used in elderly patients as indicated, taking into account the state of renal function.

Special Precautions

When used in elderly patients over 65 years of age, due to possible age-related deterioration of renal function, the concentration of creatinine and urea in the blood should be monitored.

Drug Interactions

Thiotriazoline as a cardioprotective agent can be combined with basic agents used for the therapy of coronary artery disease; as a hepatoprotective agent – it can be combined with traditional methods of hepatitis treatment.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.