Tioactiv

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT TIOACTIV

Composition:

Active substance: thiocyanate morpholinium;

1 ml of solution contains thiocyanate morpholinium, recalculated to 100 % substance – 25 mg.

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear colorless or slightly yellowish liquid.

Pharmacotherapeutic group. Cardiological agents. Other cardiological agents. Thiocyanic acid. ATC code C01EB23.

Pharmacological Properties.

Pharmacodynamics.

The active ingredient of the medicinal product exerts anti-ischemic, membrane-stabilizing, antioxidant, and immunomodulatory effects.

The mechanism of action of the medicinal product is associated with enhanced compensatory activation of anaerobic glycolysis and activation of oxidation processes in the Krebs cycle, thereby preserving the intracellular ATP pool.

The presence in the molecular structure of the morpholine salt of thiotropic acid of a thiol sulfur, which exhibits redox properties, and a tertiary nitrogen capable of binding excess hydrogen ions, promotes activation of the antioxidant system. The strong reducing properties of the thiol group lead to reactions with reactive oxygen species and lipid radicals, while reactivation of anti-radical enzymes—superoxide dismutase, catalase, and glutathione peroxidase—prevents the initiation of reactive oxygen species.

Improvement of blood rheological properties occurs due to activation of the fibrinolytic system.

The effect of the medicinal product leads to inhibition of lipid peroxidation in ischemic areas of the myocardium, reduced myocardial sensitivity to catecholamines, prevention of progressive suppression of cardiac contractile function, stabilization, and consequently reduction of myocardial necrosis and ischemia zones.

Improved myocardial metabolism, increased contractile capacity, and support of cardiac rhythm normalization allow recommending the medicinal product for the treatment of patients with various forms of ischemic heart disease.

In addition to its use in cardiology, the medicinal product can be used in the treatment of liver and other internal organ diseases, taking into account its pronounced hepatoprotective properties. The morpholine salt of thiotropic acid prevents hepatocyte destruction, reduces the extent of fatty infiltration and the spread of centrilobular liver necrosis, promotes reparative regeneration of hepatocytes, and normalizes protein, carbohydrate, lipid, and pigment metabolism within them. It also increases the rate of bile synthesis and excretion and normalizes its chemical composition.

Pharmacokinetics.

After intramuscular administration, the maximum plasma concentration of the morpholine salt of thiotropic acid is reached within 0.84 hours; after intravenous administration, it is achieved within 0.1 hours. Plasma protein binding does not exceed 10%. The compound accumulates predominantly in the kidneys (31%), as well as in significant amounts in the colon, heart, and spleen, and to the least extent in the small intestine and lungs (1–2%).

Clinical characteristics.

Indications.

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

As an additional agent in the therapy of cardiac arrhythmias.

In the complex treatment of chronic hepatitis, alcoholic hepatitis, liver fibrosis, and cirrhosis of the liver.

Contraindications.

Hypersensitivity to the active substance or to other components of the medicinal product.

Acute renal failure.

Pregnancy or breastfeeding period.

Children under 18 years of age.

Interaction with other medicinal products and other types of interactions.

As a cardio- and hepatoprotective medicinal agent, it can be used in combination with basic therapy for ischemic heart disease and combined with conventional treatment methods for hepatitis of corresponding etiology.

Special precautions for use.

Use during pregnancy or breastfeeding.

There is insufficient experience with the use of the medicinal product during pregnancy or breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

Caution should be exercised when driving or operating complex machinery in case of adverse reactions affecting the central or peripheral nervous system.

Administration and Dosage.

For myocardial infarction and unstable angina: administer the drug intravenously slowly at a rate of 2 ml/min, giving 4 ml of 25 mg/ml solution (100 mg); or administer intravenously by drip at a rate of 20–30 drops per minute (dilute 4 ml of 25 mg/ml solution in 150–250 ml of 0.9% sodium chloride solution); or administer intramuscularly, 4 ml of 25 mg/ml solution (100 mg) 2–3 times daily. Treatment duration: 14 days.

For angina at rest and post-infarction cardiosclerosis: administer the drug intramuscularly, 2 ml of 25 mg/ml solution 3 times daily. Treatment duration: 20–30 days.

For exertional angina: administer the drug intramuscularly, 4 ml of 25 mg/ml solution 2 times daily (daily dose: 200 mg). Treatment duration: 14 days.

For chronic hepatitis with marked disease activity: during the first 5 days, administer the drug intramuscularly, 2 ml of 25 mg/ml solution (50 mg) 2–3 times daily; or intravenously slowly at a rate of 2 ml/minute, 4 ml of 25 mg/ml solution (100 mg) once daily; or by drip infusion at a rate of 20–30 drops per minute (dilute 2 ampoules of 25 mg/ml solution in 150–250 ml of 0.9% sodium chloride solution). From day 5 to day 20 of therapy, administer the drug in tablet form (100 mg 3 times daily).

For chronic hepatitis of minimal or moderate activity: administer the drug intramuscularly, 2 ml of 25 mg/ml solution 3 times daily. Treatment duration: 20–30 days.

For liver cirrhosis: initiate treatment with intramuscular administration of 2 ml of 25 mg/ml solution (50 mg) 3 times daily for 5 days, followed by continuation of treatment with tablets (100 mg 3 times daily). Treatment duration: 60 days.

Children.

There is insufficient experience with the use of the drug in children.

Overdose.

Symptoms: increased urinary concentration of sodium and potassium.

Treatment: discontinue the drug, symptomatic therapy.

Adverse Reactions

The medicinal product is generally well tolerated.

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

Skin and subcutaneous tissue disorders: itching, skin hyperemia, rash, cases of urticaria;

Immune system disorders: in association with the use of other medicinal products, hypersensitivity reactions have been reported, including angioneurotic edema and anaphylactic shock;

General disorders and administration site conditions: feeling of warmth, chills, and injection site reactions.

In predominantly elderly patients receiving other medicinal products, the following may occur:

Nervous system disorders: general weakness, dizziness, tinnitus, headache;

Cardiovascular system disorders: tachycardia, arterial hypertension, cases of decreased arterial pressure;

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

Respiratory, thoracic and mediastinal disorders: dyspnea, suffocation.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

2 ml in vials, 5 vials in a blister pack, 2 blisters per carton.

Prescription status. Prescription only.

Manufacturer.

Subsidiary enterprise «FARMATREYD», Ukraine.

Manufacturer's address and place of business.

82100, Drohobych, Lviv region, Sambirska St., 85.