Pharmacological properties
Pharmacodynamics. The active substance of the drug has anti-ischemic, membrane-stabilizing, antioxidant and immunomodulatory effects.
The mechanism of action of the drug is associated with increased compensatory activation of anaerobic glycolysis and activation of oxidation processes in the Krebs cycle with preservation of the intracellular ATP pool.
The presence in the structure of the molecule of the morpholinium salt of thiazolic acid of sulfur thiol, which is characterized by redox properties, and tertiary nitrogen, which binds excess hydrogen ions, leads to the activation of the antioxidant system. The pronounced reducing properties of the thiol group cause a reaction with reactive oxygen species and lipid radicals, and the reactivation of antiradical enzymes - superoxide dismutase, catalase and glutathione peroxidase - prevents the initiation of reactive oxygen species.
Improvement of the rheological properties of blood is achieved by activating the fibrinolytic system.
The effect of the drug leads to inhibition of lipid oxidation processes in ischemic areas of the myocardium, a decrease in myocardial sensitivity to catecholamines, prevention of progressive inhibition of cardiac contractile function, stabilization and reduction of the area of necrosis and myocardial ischemia, respectively.
Improving myocardial metabolic processes, increasing its contractile ability, and promoting normalization of heart rhythm allow us to recommend the drug for the treatment of patients with various forms of coronary artery disease.
In parallel with its use in cardiology, the drug is prescribed for the treatment of diseases of the liver and other internal organs, given its high hepatoprotective properties. Morpholinium salt of thiazide acid prevents the destruction of hepatocytes, reduces the degree of fatty infiltration and the spread of centrilobular necrosis of the liver, promotes the processes of reparative regeneration of hepatocytes, normalizes protein, carbohydrate, lipid and pigment metabolism in them. It also increases the rate of synthesis and secretion of bile, normalizes its chemical composition.
Pharmacokinetics. With the / m administration of the morpholine salt of thiazide acid, C max in the blood plasma is achieved after 0.84 hours, with the / in - after 0.1 hours. Binding to blood proteins - no more than 10%. It accumulates mainly in the kidneys - 31%, as well as in large quantities in the large intestine, heart, spleen, least of all - in the small intestine and lungs (1-2%).
Indication
In the complex treatment of coronary heart disease: angina pectoris, myocardial infarction, post-infarction cardiosclerosis. as an additional agent in the therapy of cardiac arrhythmias. in the complex treatment of chronic hepatitis, alcoholic hepatitis, fibrosis and cirrhosis of the liver.
Application
In case of myocardial infarction and unstable angina, the drug is administered slowly in 4 ml of 25 mg/ml (100 mg) at a rate of 2 ml/min or intravenously drip at a rate of 20-30 drops per minute (4 ml of a 25 mg/ml solution is diluted in 150-250 ml of 0.9% sodium chloride solution) or administered intramuscularly in 4 ml of 25 mg/ml (100 mg) 2-3 times a day. The course of treatment is 14 days.
For angina pectoris of exertion and rest and post-infarction cardiosclerosis, the drug is administered intravenously at 2 ml of 25 mg/ml 3 times a day. The course of treatment is 20-30 days.
In chronic hepatitis with pronounced activity of the process, the drug is administered in the first 5 days in the form of 2 ml of 25 mg/ml (50 mg) 2-3 times a day or in the form of 4 ml of 25 mg/ml (100 mg) 1 time a day, or drip at a rate of 20-30 drops per minute (2 ampoules of 25 mg/ml solution are diluted in 150-250 ml of 0.9% sodium chloride solution). From the 5th to the 20th day of therapy, the drug is administered in the form of tablets (100 mg 3 times a day).
In chronic hepatitis of minimal and moderate activity, the drug is administered intramuscularly in a dose of 2 ml of 25 mg/ml 3 times a day. The course of treatment is 20-30 days.
In case of liver cirrhosis, treatment should begin with an intramuscular injection of 2 ml of 25 mg/ml (50 mg) 3 times a day for 5 days, and then continue treatment with tablets (100 mg 3 times a day). The course of treatment is 60 days.
Contraindication
Hypersensitivity to the active substance or other components of the drug.
Side effects
The drug is usually well tolerated. In patients with increased individual sensitivity, the following may occur:
Skin and subcutaneous tissue disorders: itching, skin hyperemia, rash, cases of urticaria;
from the immune system: cases of angioedema and anaphylactic shock have been described while taking other drugs;
others: fever, cases of chills and changes at the injection site.
In patients, mainly elderly, when taking other drugs, the following may occur:
from the central and peripheral nervous system: general weakness, dizziness, tinnitus, headache;
from the cardiovascular system: tachycardia, arterial hypertension, cases of lowering blood pressure;
from the digestive system: manifestations of dyspeptic phenomena, including dry mouth, nausea, bloating, vomiting;
Respiratory system: shortness of breath, suffocation.
Special instructions
Use during pregnancy and breastfeeding. There is no sufficient experience with the use of the drug during pregnancy and breastfeeding.
Children: There is insufficient experience with the use of the drug in children.
Ability to influence the reaction rate when driving or operating other mechanisms. In case of adverse reactions from the central and peripheral nervous system, caution should be exercised when driving or operating other mechanisms.
As a cardio- and hepatoprotective drug, it can be used in combination with basic coronary artery disease therapy and combined with traditional methods of treating hepatitis of the corresponding etiology.
Overdose
Symptoms: increased concentration of sodium and potassium in the urine.
Treatment: drug withdrawal, symptomatic therapy.
Storage conditions
In the original packaging at a temperature not exceeding 25 °C. Do not freeze.
