Thiotriazoline
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Pharmacological properties
the pharmacological effect of thiazoic acid is due to anti-ischemic, membrane-stabilizing, antioxidant and immunomodulatory effects.
The effect of the drug is realized by enhancing the compensatory activation of anaerobic glycolysis and the activation of oxidation processes in the Krebs cycle while maintaining the intracellular ATP pool. The presence of sulfur thiol in the structure of a thiazoic acid molecule, which is characterized by redox properties, and tertiary nitrogen, which binds the excess of hydrogen ions, causes the activation of the antioxidant system. The strong reducing properties of the thiol group cause a reaction with reactive oxygen species and lipid radicals. Reactivation of antiradical enzymes - superoxide dismutase, catalase and glutathione peroxidase - prevents the initiation of reactive oxygen species.
Thiazoic acid inhibits the processes of lipid oxidation in ischemic areas of the myocardium, reduces the sensitivity of the myocardium to catecholamines, prevents progressive inhibition of the contractile function of the heart, stabilizes and, accordingly, reduces the area of necrosis and myocardial ischemia. Improving the rheological properties of blood is due to the activation of the fibrinolytic system. Improving the processes of myocardial metabolism, increasing its contractile ability, contributing to the normalization of the heart rhythm, allows recommending thiazoic acid for the treatment of patients with various forms of IHD.
Pharmacokinetics Cmax thiazitic acid in blood plasma is achieved with i / m administration after 0.84 hours, with iv after 0.1 hours. Binding to blood proteins does not exceed 10%. Thiazoic acid accumulates mainly in the kidneys - 31%. In a significant amount, it accumulates in the colon, heart, spleen, least of all - in the small intestine and lungs (1-2%).
Indications
In the complex treatment of coronary heart disease: angina pectoris, myocardial infarction.
Application
In case of myocardial infarction and unstable angina, the antares drug is administered iv slowly 2 ml 50 mg / ml solution (100 mg) at a rate of 2 ml / min or iv drip at a rate of 20-30 drops per minute (2 ml p 50 mg / ml is diluted in 150–250 ml of 0.9% sodium chloride solution), or 2 ml of 50 mg / ml solution (100 mg) is administered 2–3 times a day. the course of treatment is 14 days.
With angina pectoris, Antares is administered IM 4 ml of 50 mg / ml solution 2 times a day (daily dose - 400 mg). The course of treatment is 14 days.
Contraindications
Hypersensitivity to thiazoic acid; rel.
During pregnancy and breastfeeding.
Childrens age (up to 18 years).
Side effects
The drug is generally well tolerated. in patients with increased individual sensitivity, the following may occur:
on the part of the skin and subcutaneous tissue: itching, flushing of the skin, rash, urticaria;
from the immune system: while taking other drugs, cases of angioedema, anaphylactic shock are described;
others: fever, chills, and changes at the injection site.
In patients, mainly the elderly, when taking other drugs, you may experience:
from the central and peripheral nervous system: general weakness, dizziness, tinnitus, headache;
from the cardiovascular system: tachycardia, hypertension, decreased blood pressure;
from the gastrointestinal tract: manifestations of dyspeptic phenomena, including dry mouth, nausea, bloating, vomiting;
from the respiratory system: shortness of breath and suffocation.
special instructions
Use during pregnancy and lactation. experience with the drug during pregnancy or lactation is insufficient.
Children. The experience of using the drug in children is insufficient.
The ability to influence the reaction rate when driving vehicles and working with other mechanisms.In case of adverse reactions from the central and peripheral nervous system, care must be taken when driving vehicles and working with other complex mechanisms.
Interactions
The drug Antares can be used in combination with basic treatment for coronary artery disease.
Overdose
With an overdose in the urine, the concentration of sodium and potassium increases. in such cases, the drug must be discontinued. symptomatic treatment.
Storage conditions
At a temperature not exceeding 25 ° C.