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metabolic agent
A drug: MELDONIUM (MELDONIUM)
Active ingredient: meldonium
ATX code: C01EB
KFG: A drug that improves metabolism and energy supply of tissues
Reg. number: LSR-000797/09
Date of registration: 06.02.09
The owner of the reg. acc.: PHARMSTANDART-LEKSREDSTVA (Russia)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - cellular contour packings (6) - packs of cardboard.
PHARMACHOLOGIC EFFECT
Means that improves metabolism, an analogue of gamma-butyrobetaine. Suppresses gamma-butyrobetaine hydroxynase, inhibits the synthesis of carnitine and the transport of long-chain fatty acids through cell membranes, prevents the accumulation in cells of activated forms of unoxidized fatty acids - derivatives of acylcarnitine and acylcoenzyme A.
Under conditions of ischemia, it restores the balance of the processes of oxygen delivery and its consumption in cells, prevents the violation of 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 vasodilating properties, is intensively synthesized. The mechanism of action determines the variety of its pharmacological effects: increased efficiency, reduced symptoms of mental and physical overstrain, activation of tissue and humoral immunity, cardioprotective effect.
In the case of acute ischemic myocardial damage, it slows down the formation of a necrotic zone, shortens the rehabilitation period. In heart failure, it increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation, it improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area. Effective in vascular and dystrophic pathology of the fundus. It has a tonic effect on the central nervous system, eliminates functional disorders from nervous system in patients with chronic alcoholism with withdrawal syndrome.
PHARMACOKINETICS
After oral administration, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 78%. C max in plasma is achieved 1-2 hours after administration. Biotransformed in the body with the formation of two main metabolites, which are excreted by the kidneys. T 1/2 is 3-6 hours and depends on the dose.
INDICATIONS
For oral or intravenous administration: as part of complex therapy for coronary artery disease (angina pectoris, myocardial infarction), chronic heart failure, dyshormonal cardiomyopathy; as part of the complex therapy of acute and chronic disorders of cerebral circulation (strokes and cerebrovascular insufficiency); decreased performance, physical overstrain (including in athletes), postoperative period to speed up rehabilitation; withdrawal syndrome in chronic alcoholism (in combination with specific alcoholism therapy).
For parabulbar administration: acute circulatory disorders in the retina, hemophthalmos and retinal hemorrhages of various etiologies, thrombosis of the central retinal vein and its branches, retinopathy of various etiologies (including diabetic and hypertensive) - only for parabulbar administration.
DOSING MODE
In connection with the possibility of developing an exciting effect, it is recommended to use it in the morning. The dose is set individually depending on the indications and route of administration.
When taken orally, a single dose is 0.25-1 g, the frequency of administration and the duration of treatment depend on the indications.
When administered intravenously, the dose is 0.5-1 g 1 time / day, the duration of treatment depends on the indications.
Parabulbarno enter 0.5 ml of injection with a concentration of 500 mg / 5 ml for 10 days.
SIDE EFFECT
From the side of the cardiovascular system: rarely - tachycardia, changes in blood pressure.
From the side of the central nervous system: rarely - psychomotor agitation.
From the digestive system: rarely - dyspeptic symptoms.
Allergic reactions: rarely - itching, redness, rash, swelling.
CONTRAINDICATIONS
Increased intracranial pressure (including in violation of venous outflow, intracranial tumors), pregnancy, lactation (breastfeeding), hypersensitivity to meldonium.
PREGNANCY AND LACTATION
During pregnancy and lactation (breastfeeding), the use of the drug is contraindicated.
SPECIAL INSTRUCTIONS
Use with caution in diseases of the liver and / or kidneys, especially for a long time.
Many years of experience in the treatment of acute myocardial infarction and unstable angina in cardiology departments shows that meldonium is not a first-line drug in acute coronary syndrome.
Pediatric use
In children and adolescents under the age of 18, the efficacy and safety of meldonium has not been established.
Meldonium in the form of capsules is contraindicated for use in children and adolescents under the age of 18; in the form of syrup - in children under the age of 12 years.
DRUG INTERACTIONS
When used together, meldonium enhances the effect of antianginal drugs, some antihypertensive drugs, and cardiac glycosides.
With the simultaneous use of meldonium with nitroglycerin, nifedipine, alpha-blockers, antihypertensive agents and peripheral vasodilators, moderate tachycardia, arterial hypotension may develop (with these combinations, caution is required).
When using the drug "Mildronate" a powerful tonic effect is observed. People's memory improves, thought processes accelerate, the level of dexterity of movements increases, the body's resistance to various aggressive and negative factors improves. You can use the drug "Mildronate" intramuscularly or take it in tablets.
Mildronate is an artificial analogue of gamma-butyrobetaine. This substance is found in every tissue cell human body. The mechanism of action of this drug is based on its beneficial effect on the processes of energy metabolism, as well as some tonic effect it has on the central nervous system. Under conditions of high stress on the body, the drug provides a balance in the processes of delivery and use of oxygen in cells. It optimizes metabolic processes in such a way that the level of oxygen demand is reduced for energy production. As a rule, long-term heavy loads lead to increased fatigue. In the case of using the medication "Mildronate" intramuscularly or in tablets, the body tolerates stress more easily, consumes oxygen economically and quickly restores energy reserves in order to withstand new trials. This tool performs the function of gamma-butyrobetaine, which is able to increase the speed of transmission of nerve impulses. As a result, all reactions are accelerated, and the quality of the overall metabolism improves. Therefore, when using the drug "Mildronate" intramuscularly or in tablets, the body's capabilities increase.
With significant mental and physical stress (including in sports), the following doses of the drug are recommended: for adults, the optimal regimen is 1 tablet of 250 mg four times a day. The course is two weeks. If necessary, therapy can be repeated after three weeks. The medication "Mildronate" is injected intramuscularly at a dose of 500 mg once a day. This is the optimal scheme and dosage. Where to get injections? "Mildronate" can be injected into the gluteal muscles. For athletes, dosages are somewhat different. The drug in tablets is recommended to be taken before training at 500-1000 mg twice a day. In preparation for the competition, the duration of the course is 2-3 weeks. During their period - no more than 14 days. Care must be taken when co-administered with nifedipine, antihypertensives, nitroglycerin, alpha-blockers and peripheral vasodilators.
Means "Carnitine" (L-carnitine) is similar in its action to the drug "Mildronate". Both of them during ischemia reduce the level of fatty acids in mitochondria, which remained underoxidized. Both agents are stimulators of alternative energy synthesis. In fact, the Mildronate medication does not allow harmful fatty acids into the mitochondria, and the Carnitine removes them from there by increasing the concentration of the substance of the same name. The mechanisms of action of these funds are somewhat different, but their tasks are similar. Medication "Carnitine" stimulates metabolic processes, affects different stages of energy metabolism, takes part in lipid metabolism, restores alkaline blood reserves, helps to reduce the formation of keto acids.
This agent does not affect the blood coagulation system in any way, increases the protection of tissues from toxic compounds, has an antihypoxic effect, promotes the inhibition of anaerobic glycolysis, stimulates aerobic processes, and accelerates wound healing. The medication can be used intravenously and orally. It is undesirable to use this remedy together with glucocorticoid drugs. They contribute to the accumulation of the active substance in the body. The drug "Carnitine" enhances the effect of anabolic agents.
pharmachologic effect
Means that improves metabolism, an analogue of gamma-butyrobetaine. Suppresses gamma-butyrobetaine hydroxynase, inhibits the synthesis of carnitine and the transport of long-chain fatty acids through cell membranes, prevents the accumulation in cells of activated forms of unoxidized fatty acids - derivatives of acylcarnitine and acylcoenzyme A.
Under conditions of ischemia, it restores the balance of the processes of oxygen delivery and its consumption in cells, prevents the violation of 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 vasodilating properties, is intensively synthesized. The mechanism of action determines the variety of its pharmacological effects: increased efficiency, reduced symptoms of mental and physical overstrain, activation of tissue and humoral immunity, cardioprotective effect.
In the case of acute ischemic myocardial damage, it slows down the formation of a necrotic zone, shortens the rehabilitation period. In heart failure, it increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation, it improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area. Effective in vascular and dystrophic pathology of the fundus. It has a tonic effect on the central nervous system, eliminates functional disorders of the nervous system in patients with chronic alcoholism with withdrawal syndrome.
Pharmacokinetics
After oral administration, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 78%. C max in plasma is achieved 1-2 hours after administration. Biotransformed in the body with the formation of two main metabolites, which are excreted by the kidneys. T 1/2 is 3-6 hours and depends on the dose.
Indications
For oral or intravenous administration: as part of complex therapy for coronary artery disease (angina pectoris, myocardial infarction), chronic heart failure, dyshormonal cardiomyopathy; as part of the complex therapy of acute and chronic disorders of cerebral circulation (strokes and cerebrovascular insufficiency); decreased performance, physical overstrain (including in athletes), postoperative period to speed up rehabilitation; withdrawal syndrome in chronic alcoholism (in combination with specific alcoholism therapy).
For parabulbar administration: acute circulatory disorders in the retina, hemophthalmos and retinal hemorrhages of various etiologies, thrombosis of the central retinal vein and its branches, retinopathy of various etiologies (including diabetic and hypertensive) - only for parabulbar administration.
Dosing regimen
In connection with the possibility of developing an exciting effect, it is recommended to use it in the morning. The dose is set individually depending on the indications and route of administration.
When taken orally, a single dose is 0.25-1 g, the frequency of administration and the duration of treatment depend on the indications.
When administered intravenously, the dose is 0.5-1 g 1 time / day, the duration of treatment depends on the indications.
Parabulbarno enter 0.5 ml of injection with a concentration of 500 mg / 5 ml for 10 days.
Side effect
From the side of the cardiovascular system: rarely - tachycardia, changes in blood pressure.
From the side of the central nervous system: rarely - psychomotor agitation.
From the digestive system: rarely - dyspeptic symptoms.
Allergic reactions: rarely - itching, redness, rash, swelling.
Contraindications for use
Increased intracranial pressure (including in violation of venous outflow, intracranial tumors), pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to meldonium.
Use during pregnancy and lactation
During pregnancy and lactation (breastfeeding), the use of the drug is contraindicated.
Use in children
In children and adolescents under the age of 18, the efficacy and safety of meldonium has not been established.
Meldonium in the form of capsules is contraindicated for use in children and adolescents under the age of 18; in the form of syrup - in children under the age of 12 years.
drug interaction
When used together, meldonium enhances the effect of antianginal drugs, some antihypertensive drugs, and cardiac glycosides.
With the simultaneous use of meldonium with nitroglycerin, nifedipine, alpha-blockers, antihypertensive agents and peripheral vasodilators, moderate tachycardia, arterial hypotension may develop (with these combinations, caution is required).
Application for violations of liver function
Use with caution in liver diseases, especially for a long time.
Application for violations of kidney function
Use with caution in kidney disease, especially for a long time.
special instructions
Use with caution in diseases of the liver and / or kidneys, especially for a long time.
Many years of experience in the treatment of acute myocardial infarction and unstable angina in cardiology departments shows that meldonium is not a first-line drug in acute coronary syndrome.
The page presents analogues Meldonium, in accordance with medical terminology, called "synonyms" - drugs that are interchangeable in terms of effects on the body, containing one or more identical active substances. When choosing synonyms, consider not only their cost, but also the country of origin and the reputation of the manufacturer.
Under conditions of ischemia, it restores the balance of the processes of oxygen delivery and its consumption in cells, prevents the violation of 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 vasodilating properties, is intensively synthesized. The mechanism of action determines the variety of its pharmacological effects: increased efficiency, reduced symptoms of mental and physical overstrain, activation of tissue and humoral immunity, cardioprotective effect.
In the case of acute ischemic myocardial damage, it slows down the formation of a necrotic zone, shortens the rehabilitation period. In heart failure, it increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation, it improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area. Effective in vascular and dystrophic pathology of the fundus. It has a tonic effect on the central nervous system, eliminates functional disorders of the nervous system in patients with chronic alcoholism with withdrawal syndrome.
Note! The list contains Meldonium analogues that have the same composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by the doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from of Eastern Europe: Krka, Gedeon Richter, Actavis, Egis, Lek, Geksal, Teva, Zentiva.
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