Description
Meldonium Pharmacodynamics
Gamma-butyrobetaine analog, inhibits gamma-butyrobetaine hydroxinase, decreases carnitine synthesis and long-chain fatty acids transport through cell membranes, prevents accumulation of activated forms of non-oxidized fatty acids in cells – acylcarnitine and acyl-enzyme A derivatives. Under ischemia, it restores the balance of oxygen delivery and consumption in the cells, prevents the disruption of adenosine triphosphate (ATP) transport; at the same time it activates glycolysis, which proceeds without additional oxygen consumption. As a result of a decrease in the concentration of carnitine, gamma-butyrobetaine, which has vasodilatory properties, is synthesized intensively. The mechanism of action determines a variety of its pharmacological effects: increase of work capacity, reduction of symptoms of mental and physical overexertion, activation of tissue and humoral immunity, cardioprotective effect. In case of acute ischemic myocardial injury it slows down the formation of necrotic zone, shortens the rehabilitation period. In heart failure (CH) increases myocardial contractility, increases exercise tolerance, reduces the frequency of angina attacks. In acute and chronic ischemic cerebral circulatory disorders it improves blood circulation in ischemic focus, promotes blood redistribution in favor of ischemic area. It is effective in case of vascular and dystrophic ocular fundus pathology. Tonic effect on the central nervous system (CNS), elimination of functional disorders of somatic and vegetative nervous systems in alcoholics during withdrawal is also characteristic.
Indications
Reduced performance, physical overexertion (including athletes).
As part of the treatment:
Coronary heart disease (CHD) (angina, myocardial infarction), chronic heart failure (CHF), cardialgia against myocardial dystrophy.
cerebral blood disorders (stroke, cerebrovascular insufficiency). hemophthalmos and retinal hemorrhages of various etiologies, central retinal vein thrombosis and its branches, retinopathies of various etiologies (including diabetic and hypertensive).
Alcohol withdrawal syndrome (in combination with specific therapy).
Contraindications
Hypersensitivity, increased intracranial pressure (with impaired venous outflow and intracranial tumors), pregnancy, lactation. Not applicable in children under 18 years of age due to lack of data.
Caution
Chronic liver and kidney diseases.
Administration during pregnancy and breast-feeding.
Safety of use during pregnancy is not proven. The drug should not be applied during pregnancy in order to avoid possible adverse effects on the fetus.
It is not known whether the drug is excreted with the breast milk. If it is necessary to use meldonium during lactation, breastfeeding should be stopped.
Dosage and administration method
- Intravenously, intramuscularly, parabulbar.
- The drug should be used in the first half of the day due to its possible excitatory effect.
- Mental and physical overload (including in athletes): intravenously, 500 mg once a day.
- The course of treatment is 10-14 days. If necessary, treatment should be repeated after 2-3 weeks.
- Unstable angina pectoris and myocardial infarction: intravenously by injection, 0.5-1 g per day. Daily dose can be administered in 1 or 2 doses. The course of treatment is 10-14 days.
- Chronic heart failure: intravenously by trickle 0.5-1 g once a day or intramuscularly by 500 mg 1-2 times a day, treatment course 10-14 days, then switch to oral administration.
- Cardialgia against myocardial dystrophy: intravenously by 0.5-1 g once daily or intramuscularly by 500 mg 1 -2 times daily, treatment course 10-14 days, then switch to oral administration. Withdrawal alcohol syndrome: 500 mg intravenously 2 times a day.
- The course of treatment is 7-10 days.
- Impaired cerebral circulation:
-acute phase of cerebrovascular pathology: intravenously, 500 mg once a day for 10 days, then switch to oral administration.
-Chronic cerebrovascular disorders: intramuscularly 500 mg 1 time per day, preferably in the morning. - The course of treatment is 10 days, then switch to oral administration.
- Vascular ocular fundus pathology and retinal dystrophy (hemophthalmos and retinal hemorrhages of various etiologies, central retinal vein thrombosis and its branches): administer 50 mg (0.5 ml) of the drug solution parabulbarically for 10 days.
