Active substancePhosphocreatinePhosphocreatine
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  • Neoton
    powder d / infusion 
  • Phosphocreatine
    powder d / infusion 
    ALVILS, LTD.     Russia
  • Dosage form: & nbspPowder for solution for infusion

    Composition:

      1 bottle contains: Active substance: sodium phosphosilicate tetrahydrate 1 g.


    Description:

    Powder of white color in the form of granules.


    Pharmacotherapeutic group:metabolic
    ATX: & nbsp

    C.01.E.B   Other drugs for the treatment of heart disease

    C.01.E.B.06   Phosphocreatine

    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 triphosphate (ATP), in the hydrolysis of which energy is released to provide the process of contraction of actomyosin. Insufficient energy intake into cardiomyocytes, associated with the slowing down of 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 functionally recover. With myocardial damage, there is a close correlation between the amount of energy-rich phosphorylated compounds in cells, the viability of cells and their ability to restore contractility.Preclinical and clinical studies have demonstrated the cardioprotective effect of phosphocreatine, which manifests itself in a dose-dependent positive effect with toxic effects on the myocardium of isoprenaline, thyroxine, emetin, p-nitrophenol;

    in a positive inotropic effect with a deficiency of glucose, calcium ions or overdose of potassium ions; in reducing the negative inotropic action due to 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 in cardiopulmonary by-pass bypass is reduced;

    • the risk of developing reperfusion arrhythmia is reduced by infusion until the development of experimental regional ischemia as a result of superposition of the ligature on the anterior descending branch of the left coronary artery for 15 min;

    • reduces the degradation of ATP and phosphocreatine in myocardial cells, preserves the structure of mitochondria and sarcolemma, improves the functional recovery of 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 the experiment with myocardial infarction and arrhythmia caused by occlusion of the coronary artery: it preserves the cellular pool of adenine nucleotides by inhibiting the enzymes that cause their catabolism, suppresses the degradation of phospholipids, possibly improves microcirculation in the ischemic zone, which is due to the suppression of adenosine diphosphate acid mediated platelet aggregation , stabilizes hemodynamic parameters, prevents a sharp decrease in the functional parameters of the heart, ntiaritmicheskoe effect, reduces the frequency and duration of ventricular fibrillation and myocardial infarction limits zone.

    Pharmacokinetics:

    Distribution: after a single intravenous infusion the maximum concentration of phosphocreatine in the blood plasma is determined for 1-3 min. The greatest amount of phosphocreatine is accumulated in skeletal muscle, myocardium and brain. In the tissues of the liver and lungs, the accumulation of phosphocreatine is insignificant.

    Excretion:

    The elimination of phosphocreatine is two-phase ("fast" and "slow" phases), which is due to its accumulation in tissues with subsequent excretion from the body into the second phase.The half-life in the "fast" phase is 30-35 min; The half-life in the "slow" phase is several hours. It is excreted by the kidneys.

    Indications:

    Neoton is used in combination therapy of the following diseases:

    • acute myocardial infarction;

    • chronic heart failure;

    • intraoperative myocardial ischemia;

    • intraoperative ischemia of the lower extremities,

    and also in sports medicine for the prevention of the development of the syndrome of acute and chronic physical overstrain and improving the adaptation of athletes to extreme physical stress.

    Contraindications:
    • hypersensitivity to the drug;

    • chronic renal failure (with the use of the drug in doses of 5-10 g / day);

    • age to 18 years (efficacy and safety not established).

    Pregnancy and lactation:

    There are no clinical data on the use of Neoton in pregnancy. However, animal studies did not show the toxic effect of the drug on rat fertility and embryo-fetal development of rabbits. Neoton can be used during pregnancy only when the benefit to the mother exceeds the potential risk to the fetus.

    If you need to use the drug during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    ONLY INTRAVENOUS (drip or in the form of rapid infusion)

    Acute myocardial infarction

      1 day: 2-4 g of the drug, diluted in 50 ml of water for injection, in the form of IV infusion with subsequent iv infusion of 8-16 g in 200 ml of 5% dextrose (glucose) solution for 2 hours.

      2 days: 2-4 g in 50 ml of water for injection IV drip (duration of infusion no less than 30 minutes) 2 times / day.

      3 days: 2 g in 50 ml of water for injection IV drip (duration of infusion at least 30 minutes) 2 times / day. If necessary, a course of infusions for 2 g of the drug 2 times / day. Can hold for 6 days.

    Chronic heart failure

    Depending on the patient's condition, you can start treatment with "shock" doses of 5-10 g of the drug in 200 ml of a 5% solution of dextrose (glucose) IV drip at a rate of 4-5 g / h for 3-5 days, and then go for IV infusion (duration of infusion no less than 30 minutes) 1-2 g of the drug, diluted in 50 ml of water for injection, 2 times / day. for 2-6 weeks, or immediately start iv droplet administration of maintenance doses of Neoton (1-2 g in 50 ml of water for injection 2 times / day for 2-6 weeks).

    Intraoperative myocardial ischemia

    A course of IV infusion with a duration of at least 30 minutes for 2 g of the drug in 50 ml of water for injection 2 times / day is recommended. for 3-5 days prior to surgery, and within 1-2 days after it. During surgery, Neoton is added to the usual cardioplegic solution at a concentration of 10 mmol / L or 2.5 g / L immediately before administration.

    Intraoperative ischemia of lower extremities

    2-4 g Neoton in 50 ml of water for injection in the form of IV infusion before surgery, followed by iv drip administration of 8-10 g of the drug in 200 ml of 5% dextrose (glucose) solution at a rate of 4-5 g / h during surgery and during reperfusion.

    In sports medicine, to prevent the development of the syndrome of acute and chronic physical overstrain and to improve the adaptation of athletes to extreme physical stress, Neoton should be used at a dose of 1 g / day in 50 ml of water for injection IV drip (duration of infusion of at least 30 minutes) during 3-4 weeks.

    Side effects:

    Hypersensitivity to the drug, lowering blood pressure (with a rapid intravenousadministered).

    Overdose:

    At present, cases of overdose of Neoton have not been reported.

    Interaction:

    When used as part of a combination therapy, Neoton helps to increase the effectiveness of antiarrhythmic, antianginal drugs and agents with a positive inotropic effect. Neoton maintains stability in water for injection, a solution of 5% dextrose (glucose) and cardioplegic solutions.

    Special instructions:

    The drug should be administered as soon as possible after the onset of signs of ischemia, which provides a more favorable prognosis of the disease. The use of Neoton in high doses (5-10 g / day) is accompanied by increased phosphate uptake in the kidneys, which affects calcium metabolism, secretion of hormones regulating homeostasis, renal function and purine metabolism, therefore, prolonged use of Neoton in high doses is not recommended.

    Form release / dosage:

    Powder for solution for infusion 1 g:

    Packaging:1 g of powder in a bottle of neutral colorless glass type II with a rubber stopper and an aluminum cap for running in with a detachable lid. For 1 or 4 bottles together with instructions for use in a cardboard pack.
    Storage conditions:

    Store at a temperature not exceeding 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiry date printed on the package.


    Terms of leave from pharmacies:On prescription
    Registration number:П N014030 / 01-2002
    Date of registration:24.11.2008
    The owner of the registration certificate:Alfa Wassermann SpAAlfa Wassermann SpA Italy
    Manufacturer: & nbsp
    Representation: & nbspALPHA VASSERMANN LLC ALPHA VASSERMANN LLC Italy
    Information update date: & nbsp28.10.2015
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