Neoton (Phosphocreatine). Powder for parental use
4 bottles of powder + 1 solvent bottle + kit for single use
Neoton (4gr)- the preparation of a solution of phosphocreatine (Alfa Schiapparelli Wassermann). The desire to increase the efficiency of recovery of energy resources in the myocardium led to the creation of another product containing macroergic compounds — phosphocreatine (CP). Neoton available in bottles containing 200, 500, 1000, 2000 and 5000 mg FC administered intravenously.
Pharmacokinetics. After a single intravenous infusion there is a rapid dose-dependent increase in the content of FC in blood to a maximum level within 1-5 min., the Process of excretion of FC is divided into two phases: the first, fastest, characterized by the half-time of FC, constituting 30 to 35 minutes, the duration of the second slow phase of excretion, — a few hours. The contents of FC in the urine begins to increases after 30 min and reached a maximum after 60 min after injection. A significant portion of the administered phosphocreatine is captured by different bodies. Analysis of the distribution of exogenous PCR in blood and other tissues suggests that this compound specifically accumulates in skeletal muscle, myocardium and brain tissues in which intracellular FC plays a functionally important role. The removal of FC from the tissues is slow, which determines the duration of the second phase of elimination from the body.
Pharmacodynamics. Neoton improves myocardial metabolism and muscle tissue, slows down the process of destruction of the sarcolemma of ischemic cardiomyocytes and myocytes, provides intracellular transport of energy. By improving microcirculation drug reduces the size of the zone of necrosis and ischemia. During ischemia and postischemic reperfusion causes antiarrhythmic effect, which is associated with a decrease in ectopic activity of the ventricles and preservation of physiological functions of the cells of the Purkinje fibers.
Phosphocreatine is a key substrate in the transport system makroergov to their disposal. In conditions of hypoxia or ischemia, muscle contraction is terminated at the moment when almost completely exhausted cellular reserves of FC, even while maintaining about 90% of ATP. The reduction of the concentration of FC in the cell below the critical level coincides with the destruction of the membrane and the beginning of irreversible changes in the cell, it triggers phospholipases and lipid peroxidation. Although the cell membrane is considered impermeable to polar compounds, such as FC, there is experimental evidence from enrolling him in a cell under certain physiological and pathological conditions.
Creatine and phosphocreatine are involved in the transfer of energy from the mitochondria to the places of its utilization, increase the energy potential and Poole adenilovoj by nucleotide-induced activation of phosphoribosylpyrophosphate (a key enzyme in the synthesis of nucleotides) in two ways: indirectly through increasing the level of ATP and directly by eliminating the inhibitory effect on the enzyme ADP.
The drug reduces the damaging effects of ischemia on the cell membrane limits the size of the zone of necrosis after experimental myocardial infarction. This effect is accomplished by stimulation adenilatziklaznuu complex of the sarcolemma, regulating the flow of Ca2+ ions through the slow channels of the nodal cells, without the participation of creatine kinase. Under the action of FC there is a change in the hormonal regulation of metabolism, which is based on activation of the pituitary-adrenal system, stimulation of adaptive protein synthesis, changes in the ionic composition of the internal environment of the body and other reactions, which leads to increase the body's resistance to hypoxia.
It is established that FC is present in the cardioplegic solutions in the optimum concentration, significantly improves protection to the ischemic heart by maintaining its functionality, structural integrity and postischemic antiarrhythmic action.
The mechanisms of the biochemical effects of phosphocreatine diverse:
inhibition of platelet aggregation by removal of ADP in the extracellular creatinkinase the course of the reaction;
the penetration of a certain amount of FC into cells and its participation in the system of energy transmission by maintaining high local concentrations of ATP;
slowing the degradation of adenindinucleotide at 5-nucleotidase reactions occurring in sarcolemmal the membrane of cardiomyocytes;
inhibition of the accumulation of lysophospholipids ishemizirovanna in the myocardium and preservation of the structure of the sarcolemma of miocardiotita;
translation of the cell membrane in a more ordered state as a result of electrostatic interactions between drug molecule and the phospholipids in the presence of calcium ions.
Due to the fact that the charged phospholipids are located on both sides of the sarcolemma, exogenous and endogenous phosphocreatine can be equally important for its stability. Rapid depletion of cellular phosphocreatine during ischemia period can be one of the factors of destabilization of membrane and increase the speed of its destruction. Exogenous phosphocreatine can stabilize the membrane after attaching to its outer surface without penetrating into the cells.
In the experiment in hypoxia and heart failure introduction phosphocreatine is accompanied by inhibition of processes of lipid peroxidation, reduction of organic damage to cell membranes caused by hypoxia and stress.
Indications: acute myocardial infarction; congestive heart failure; intraoperative myocardial ischemia, intraoperative ischemia of the extremities; acute ischemic stroke; neurology for the treatment of patients with acute violation of cerebral circulation. Positive effects on myocardial metabolism and microcirculation allows the use of Neoton in sports medicine to prevent development of the syndrome of physical stress and improving adaptation to extreme physical stress, i.e. the drug is effective as a post-workout reductant (rower, runner, swimmer, of international level can start 1 time in a few days with good performance, and the use of Neoton — every day). The efficiency of organizers and players. The use of the drug before a competition reduces the severity of acidosis but does not increase the result.
The dosage: in acute myocardial infarction in the first day is administered 2-4 g intravenously, followed by drip infusion of 8 to 16 g in 200 ml 5% glucose solution for 2 h On the second day appoint 2-4 g intravenously 2 times a day, on the third day, 2 g intravenously 2 times a day. If necessary, infusion of the drug at 2 g, 2 times a day can be carried out within 6 days. In cases of chronic heart failure administered intravenously at 1-2 g 2 times a day for 10-14 days. Intraoperative myocardial ischemia, the drug is administered as part of regular cardioplegia solution in an amount of 3 g per 1 l of Neoton added to the composition of the solution immediately before administration. Recommended rate of infusion of the drug at 2 g, 2 times a day for 3-5 days prior to surgery and for 1-2 days after surgery. If possible, the development of intraoperative ischemia of the extremities is recommended intravenously to enter 2-4 g of the drug before surgery, followed by infusion of 8-10 g in 5 % glucose solution during the operation and the period of reperfusion. In applying the drug in sports medicine his daily dose of 5-10 g.
Sports activities Neoton often injected intravenously for a few days before competitions in sports, aimed at priority development of endurance in a daily dose of 2-4 g (morning or evening) and dose of 15-24 g. it should be noted that not a single scientific work on laboratory or field trials with this drug
in the conditions of intensive muscular activity of different energetic orientation, we have not met. I.e., evidence regarding the extent of its influence on the results in exercises of different energetic orientation, effective dosages, timing of administration, etc. do not exist.
Contraindications: hypersensitivity to the drug. Data on the safety and efficacy of Neoton during pregnancy and breastfeeding are not available.
Side effects: when applying on the testimony at the recommended doses side effects are not detected.
The drug should be administered in the shortest possible time from the time of onset of ischemia, providing a more favorable prognosis. Neoton is not used for emergency correction of disorders of the heart.
Overdose: currently, the cases of drug overdose of Neoton was not reported.
Drug interactions: when used in the complex therapy Neoton enhances the effectiveness of antiarrhythmic, antianginal tools and also drugs that have a positive effect on the inotropic function of the myocardium.