Antares

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT ANTAres® (ANTARES®)

Composition:

Active substance: morpholine salt of thiatic acid;

1 ml of solution contains 50 mg of morpholine salt of thiatic acid, calculated as 100% substance, equivalent to 33.3 mg of thiatic acid;

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physico-chemical properties: clear, colorless liquid or with a slight yellowish tint.

Pharmacotherapeutic group. Cardiological agents. Other cardiological agents. Thiatic 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 realized through enhanced compensatory activation of anaerobic glycolysis and stimulation of oxidation processes in the Krebs cycle, preserving the intracellular adenosine triphosphate (ATP) pool. 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 its reaction with reactive oxygen species and lipid radicals. Reactivation of radical-scavenging enzymes—superoxide dismutase, catalase, and glutathione peroxidase—prevents the formation of reactive oxygen species.

Thiotropic acid inhibits lipid peroxidation in ischemic areas of the myocardium, reduces myocardial sensitivity to catecholamines, prevents progressive suppression of cardiac contractile function, and stabilizes and subsequently reduces the area of myocardial necrosis and ischemia. Improvement of blood rheological properties occurs via activation of the fibrinolytic system. Enhanced myocardial metabolism, increased contractile function, and support in normalizing cardiac rhythm allow thiotropic acid to be recommended for the treatment of patients with various forms of ischemic heart disease.

Pharmacokinetics.

Maximum plasma concentration of thiotropic acid is achieved within 0.84 hours after intramuscular administration and within 0.1 hours after intravenous administration. Plasma protein binding does not exceed 10%. Thiotropic acid accumulates predominantly in the kidneys—31%. Significant accumulation also occurs in the colon, heart, and spleen; the lowest levels are found in the small intestine and lungs (1–2%).

Clinical characteristics.

Indications.

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

Contraindications.

Hypersensitivity to thiotropic acid, acute renal failure.

Pregnancy and lactation period.

Pediatric age (under 18 years).

Interaction with other medicinal products and other types of interactions.

The medicinal product Antares® can be used in combination with basic therapeutic agents for ischemic heart disease.

Special precautions for use.

Use during pregnancy or breastfeeding. Experience with the use of the drug during pregnancy or breastfeeding is insufficient.

Ability to affect reaction rate when driving or operating machinery. Caution should be exercised when driving or operating other complex machinery in case of adverse reactions affecting the central or peripheral nervous system.

Method of administration and dosage.

For myocardial infarction and unstable angina, the medicinal product Antares® should be administered intravenously slowly at a rate of 2 ml/min, injecting 2 ml of the 50 mg/ml solution (100 mg); or administered intravenously by infusion at a rate of 20–30 drops per minute (2 ml of the 50 mg/ml solution is diluted in 150–250 ml of 0.9% sodium chloride solution); or administered intramuscularly with 2 ml of the 50 mg/ml solution (100 mg) 2–3 times daily. The treatment course is 14 days.

For exertional angina, the medicinal product Antares® should be administered intramuscularly twice daily with 4 ml of the 50 mg/ml solution (daily dose — 400 mg). The treatment course is 14 days.

Children.

Experience with the use of the medicinal product in children is insufficient.

Overdose. In case of overdose, concentration of sodium and potassium in urine increases. In such cases, the medicinal product should be discontinued. Symptomatic treatment is recommended.

Adverse Reactions

The medicinal product is generally well tolerated. In patients with increased individual sensitivity, the following may occur:

Skin and subcutaneous tissue disorders: pruritus, skin hyperemia, rash, urticaria;

Immune system disorders: angioneurotic edema and anaphylactic shock have been reported in association with the use of other drugs;

Other: fever, chills, and local reactions at the injection site.

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

Central and peripheral nervous system disorders: general weakness, dizziness, tinnitus, headache;

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

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

Respiratory system disorders: dyspnea, wheezing.

Reporting of adverse reactions after medicinal product registration is of great importance. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

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 a vial, 10 vials in a blister pack, 1 blister pack per carton.
4 ml in a vial, 5 vials in a film-coated blister pack, 2 film-coated blister packs per carton.

Prescription category: Prescription only.

Manufacturer: JSC "Galichfarm".

Manufacturer's location and address of business activity:
6/8 Opryshkivska Street, Lviv, 79024, Ukraine.