Thiotriazolin®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT TIIOTRIAZOLIN® (THIOTRIAZOLIN)

Composition:

Active substance(s): tiazotic acid;

One tablet contains morpholine salt of tiazotic acid, equivalent to 100% substance – 200 mg, corresponding to 133 mg of tiazotic acid;

Excipients: potato starch, povidone, powdered sugar, microcrystalline cellulose, calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white or almost white, round-shaped tablets with a flat surface, beveled edges and a score line.

Pharmacotherapeutic group.

Cardiological preparations. Other cardiological preparations. Tiazotic acid.

ATC code C01EB23.

Pharmacological Properties.

Pharmacodynamics.

The pharmacological effect of thiotropic acid is due to its anti-ischemic, membrane-stabilizing, antioxidant, and immunomodulatory actions.

The drug's effect is achieved by enhancing compensatory activation of anaerobic glycolysis and stimulating oxidation processes in the Krebs cycle, thereby preserving intracellular ATP levels. The presence of a thiol sulfur group in the molecular structure of thiotropic acid, which exhibits redox properties, and a tertiary nitrogen atom capable of binding excess hydrogen ions, contributes to the activation of the antioxidant system. The strong reducing properties of the thiol group lead to reactions with active oxygen species and lipid radicals. Reactivation of antiradical enzymes—superoxide dismutase, catalase, and glutathione peroxidase—prevents the initiation of active oxygen species.

Thiotropic acid inhibits lipid peroxidation in ischemic areas of the myocardium, reduces myocardial sensitivity to catecholamines, prevents progressive depression of cardiac contractile function, and stabilizes and reduces the extent of myocardial necrosis and ischemia. Improvement in blood rheological properties is achieved through activation of the fibrinolytic system. Enhanced myocardial metabolism, increased myocardial contractility, and support for normalization of cardiac rhythm allow thiotropic acid to be recommended for the treatment of patients with various forms of ischemic heart disease.

In addition to its use in cardiology, thiotropic acid is also used in the treatment of liver and other internal organ diseases due to its pronounced hepatoprotective properties. The drug prevents hepatocyte destruction, reduces fatty infiltration and the spread of centrilobular liver necroses, promotes reparative regeneration of hepatocytes, and normalizes protein, carbohydrate, lipid, and pigment metabolism within them. It increases the rate of bile synthesis and excretion and normalizes its chemical composition.

Pharmacokinetics.

After oral administration, the drug is rapidly absorbed, with an absolute bioavailability of 53%. Maximum plasma concentration is reached 1.6 hours after a single 200 mg dose. The elimination half-life is approximately 8 hours.

Clinical characteristics.

Indications.

In complex treatment of ischemic heart disease: angina pectoris, myocardial infarction, postinfarction cardiosclerosis; cardiac arrhythmias.

In complex treatment of chronic hepatitis of various etiologies, including alcoholic hepatitis; liver cirrhosis.

Contraindications.

Hypersensitivity to thiotropic acid and to other components of the drug;

acute renal failure.

Interaction with other medicinal products and other forms of interactions.

Thiotriazolin® as a cardioprotective agent can be used in combination with basic therapeutic agents for ischemic heart disease.

As a hepatoprotective agent, it may be combined with conventional treatments for hepatitis.

Special precautions.

None.

Use during pregnancy or breastfeeding.

The efficacy and safety of the medicinal product during pregnancy or breastfeeding have not been studied.

Ability to affect reaction rate while driving or operating machinery.

Currently there are no reports, however, the possibility of developing dizziness should be taken into account.

Dosage and Administration.

For stable exertional angina, prescribe Thiotriazolin® 200 mg orally three times daily. Treatment course: 8 weeks.

For angina at rest, myocardial infarction, and post-infarction cardiosclerosis, prescribe Thiotriazolin® 200 mg orally three times daily for 20–30 days.

For cardiac arrhythmias, prescribe Thiotriazolin® 200 mg orally or sublingually three times daily.

For liver diseases, prescribe Thiotriazolin® 200 mg orally three times daily for 20–30 days.

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

Children. Experience with the use of the drug in children is insufficient.

Overdose.

In case of overdose, the concentration of sodium and potassium in urine increases. In such cases, the drug should be discontinued.

Treatment is symptomatic.

Adverse reactions.

The drug is usually well tolerated.

In patients with increased individual sensitivity, the following may occur:

Skin and subcutaneous tissue disorders: pruritus, skin hyperemia, rash, urticaria, angioneurotic edema.

When used as part of combination therapy, mainly in elderly patients, the following may occur:

Immune system disorders: anaphylactic shock;

Nervous system disorders: dizziness, tinnitus;

Gastrointestinal disorders: dyspeptic symptoms including dry mouth, nausea, vomiting; abdominal distension;

Respiratory, thoracic and mediastinal disorders: dyspnea, asthma;

General disorders: general weakness, fever.

During the post-marketing surveillance period, the following reactions were also observed, for which the relationship to the use of Thiotriazoline® has not been established:

Cardiovascular system disorders: arterial hypertension, tachycardia.

Shelf life. 2 years.

Storage conditions.

In the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. Tablets 200 mg, 10 tablets per blister, 3 or 9 blisters per carton; 15 tablets per blister, 6 blisters per carton.

Prescription category. Prescription only.

Manufacturer.

JSC "Kyivmedpreparat".

LLC "MARIFARM".

Manufacturer's address and place of business.

139 Saksaganskogo Street, Kyiv, 01032, Ukraine.

8 Minarikova Street, Maribor, 2000, Slovenia.