Thiotriazoline

Thiotriazoline Solution for Injection, 25 mg/ml, 2 ml/4 ml Ampoules

Composition

Active ingredient:

• Morpholine salt of thiazotic acid: 25 mg per ml (equivalent to 16.6 mg of thiazotic acid).
  Excipients:
• Water for injection.

Pharmaceutical Form

Solution for injection.

Appearance:
A clear, colorless liquid or with a slightly yellowish tint.

Pharmacological Group

Cardiovascular drugs. Other cardiac preparations. Thiazotic acid.

ATC Code: C01EB23.

Pharmacological Properties

Pharmacodynamics:
The therapeutic effects of thiazotic acid include anti-ischemic, membrane-stabilizing, antioxidant, and immunomodulating actions.

The drug enhances compensatory activation of anaerobic glycolysis and oxidative processes in the Krebs cycle, maintaining intracellular ATP levels. The thiol sulfur and tertiary nitrogen in its structure provide antioxidant properties by neutralizing reactive oxygen species and lipid radicals while reactivating enzymes like superoxide dismutase, catalase, and glutathione peroxidase.

Thiazotic acid reduces myocardial lipid peroxidation in ischemic zones, decreases myocardial sensitivity to catecholamines, and minimizes necrotic and ischemic areas. It also improves myocardial contractility and normalizes cardiac rhythm. Additionally, the drug enhances blood rheology by activating the fibrinolytic system.

Beyond cardiology, the drug is used for hepatic and internal organ conditions due to its hepatoprotective properties, preventing hepatocyte damage and promoting regenerative processes.

Pharmacokinetics:

• Maximum concentration:
  • Intramuscular: 0.84 hours
  • Intravenous: 0.1 hours
• Protein binding: <10%
• Accumulates primarily in kidneys (31%), heart, colon, and spleen. Minimal accumulation in small intestine and lungs (1-2%).

Indications for Use

• Ischemic heart disease: angina, myocardial infarction, post-infarction cardiosclerosis.
• Adjunct therapy for cardiac arrhythmias.
• Chronic hepatitis, alcoholic hepatitis, fibrosis, and liver cirrhosis.

Contraindications

• Hypersensitivity to thiazotic acid.
• Acute renal failure.

Drug Interactions

Can be combined with standard treatments for ischemic heart disease and hepatitis therapies.

Special Warnings and Precautions

• Pregnancy and lactation: Insufficient data for use during these periods.
• Driving or operating machinery: Exercise caution if experiencing central or peripheral nervous system side effects.

Dosage and Administration

For Ischemic Heart Disease:

• Myocardial infarction and unstable angina: 4 ml of 25 mg/ml solution (100 mg) intravenously or intramuscularly, 2-3 times daily. Course: 14 days.
• Stable angina: 4 ml intramuscularly twice daily. Course: 14 days.
• Post-infarction cardiosclerosis: 2 ml intramuscularly three times daily. Course: 20-30 days.

For Liver Diseases:

• Severe chronic hepatitis: 2 ml intramuscularly or 4 ml intravenously for the first 5 days, then switch to oral tablets for 15 days.
• Mild to moderate hepatitis: 2 ml intramuscularly three times daily. Course: 20-30 days.
• Cirrhosis: Intramuscular for 5 days, followed by tablets for 60 days.

Side Effects

• Common: Itching, skin rash, redness, urticaria, dizziness, weakness, tachycardia, dry mouth, nausea, bloating.
• Severe (rare): Angioedema, anaphylactic shock.

Overdose

• Increased sodium and potassium in urine. Discontinue use and provide symptomatic treatment.

Packaging and Storage

• Storage conditions: Keep in the original packaging, ≤25°C. Protect from children.
• Shelf life: 5 years.

Prescription Status

Prescription only.

Manufacturer:
PJSC "Galychpharm," Ukraine.

Note: Not recommended for children, pregnant, or breastfeeding women. Use cautiously in allergy-prone individuals and drivers.