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Pharmacological group Metabolic agent.
Pharmacodynamics
Phosphocreatine plays an important role in the energy mechanism of muscle contraction. It is a reserve of energy in the cells of the myocardium and skeletal muscles and is used for the re-synthesis of adenosine triphosphoric acid (ATP), the hydrolysis of which releases energy to ensure the reduction of actomyosin.
Insufficient energy supply to cardiomyocytes associated with a slowdown in oxidative processes is a key mechanism for the development and progression of myocardial damage. Lack of phosphocreatine leads to a decrease in the strength of myocardial contraction and its ability to functional recovery. In myocardial injury, there is a close correlation between the amount of energy-rich phosphorylated compounds in cells, the viability of the cells and their ability to restore contractility.
Preclinical and clinical studies have demonstrated the cardioprotective effect of phosphocreatine, which is manifested in a dose-dependent positive effect with toxic effects on the myocardium of isoprenaline, thyroxine, emetine, p-nitrophenol; in a positive inotropic effect with a deficiency of glucose, calcium ions or an overdose of potassium ions; in reducing the negative inotropic effect caused by anoxia.
In addition, the addition of phosphocreatine to cardioplegic solutions at a concentration of 10 mmol / L improves the cardioprotective effect:
- the risk of myocardial ischemia is reduced with cardiopulmonary bypass bypass grafting;
- the risk of developing reperfusion arrhythmia during infusion is reduced before the development of experimental regional ischemia as a result of ligation on the anterior descending branch of the left coronary artery for 15 minutes;
- reduces the degradation of ATP and phosphocreatine in myocardial cells, preserves the structure of mitochondria and sarcolemma, improves the process of functional recovery of the myocardium after cardiac arrest caused by the administration of a large dose of potassium, and reduces the frequency of reperfusion arrhythmia.
Phosphocreatine has a cardioprotective effect in experiments with myocardial infarction and arrhythmias caused by coronary artery occlusion: it preserves the cellular pool of adenine nucleotides by inhibiting the enzymes that cause their catabolism, inhibits the degradation of phospholipids, possibly improves microcirculation in the zone of ischemia mediated by adiphocytic acid suppression , stabilizes hemodynamic parameters, prevents a sharp decrease in the functional parameters of the heart, has an antiarrhythmic effect, reduces the frequency and duration of ventricular fibrillation and limits the zone of myocardial infarction.
Neoton (phosphocreatine) is a drug that improves myocardial and muscle tissue metabolism.
Phosphocreatine - is found in high concentration in the myocardium, skeletal muscles, smooth muscles, retina, nerve tissue cells, sperm. Plays a key role in the energy supply of muscle contraction, carrying out intracellular transport of energy from places of production to places of use. With the depletion of phosphocreatine stores, the cell loses its ability to contract even if there is a sufficient amount of ATP.
Neoton provides intracellular energy transport, slows down the decrease in the contractility of the heart muscle during ischemia. Neoton inhibits platelet aggregation and increases the plasticity of erythrocyte membranes.
After being introduced into the blood, exogenous phosphocreatine is inactivated much more slowly than ATP. In addition, this compound has the property of selectively accumulating in tissues with an increased metabolic rate.
The positive effect on myocardial metabolism and microcirculation allows Neoton to be used in sports medicine to prevent the adverse effects of physical overstrain.
In addition, Neoton can be used in neurology to treat patients with acute impairment of cerebral circulation.
Pharmacokinetics:
With a single intravenous infusion, the maximum concentration of the drug in the blood is determined for 1-3 minutes.
The half-life in the fast phase is 30-35 minutes. The half-life in the slow phase is several hours. It is excreted by the kidneys.
The greatest amount of the drug accumulates in skeletal muscles, myocardium and brain. In the tissues of the liver and lungs, the accumulation of the drug is insignificant.
Neoton Indications for use:
Drug interaction:
When used as part of complex therapy, Neoton increases the effectiveness of antiarrhythmic, antianginal and cardiotonic drugs.
INDICATIONS FOR USE of Neoton (Phosphocreatine) IN SPORT