Phosphocreatine (Phosphocreatinum)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePhosphocreatinePhosphocreatine
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  • Phosphocreatine
    powder d / infusion 
    ALVILS, LTD.     Russia
    • Dosage form: & nbspPowder for solution for infusion
    Composition:

    Composition per 1 bottle 0.5 g:

    Active substance: phosphocreatine sodium tetrahydrate - 0.64 g, in terms of sodium phosphocreatine - 0.5 g.

    Composition per 1 bottle 1.0 g:

    Active substance: phosphocreatine sodium tetrahydrate - 1.28 grams, in terms of sodium phosphocreatine - 1.0 g.

    Description:Ba white or almost white crystalline powder.
    Pharmacotherapeutic group:Metabolic means
    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 functional recovery.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 made it possible to demonstrate 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 enzymes that cause their catabolism, suppresses phospholipid degradation, possibly improves microcirculation in the ischemic zone, which is due to suppression of adenosinediphosphoric acid mediated platelet aggregation , stabilizes hemodynamic parameters, prevents a sharp decline in the functional parameters of the heart a, has antiarrhythmic effect, reduces the frequency and duration of ventricular fibrillation and limits the area of ​​myocardial infarction.

    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 accumulates in skeletal muscles, 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:

    Phosphocreatine 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:

    - Dhypersensitivity to the drug;

    - chronic renal failure (with 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 phosphocreatine in pregnancy.However, animal studies did not show the toxic effect of the drug on rat fertility and embryo-fetal development of rabbits. Phosphocreatine can be used in pregnancy only when the benefit to the mother exceeds the potential risk to the fetus.

    During the period of application of the drug, breastfeeding should be stopped.

    Dosing and Administration:

    Only intravenously (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, as an IV fast infusion followed by 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 in / in the drip (infusion duration of at least 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 of 2 g of the drug 2 times / day can be carried out for 6 days.

    Chronic heart failure

    Depending on the patient's condition, it is possible to 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 to / in the drip (duration of infusion of at least 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 / in the drip of supporting doses of the drug (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 a day for 3-5 days preceding the surgical procedure and 1-2 days after it is recommended. During surgery, the drug 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 of the drug in 50 ml of water for injection in the form of IV infusion prior to surgery followed by iv injection of 8-10 g of the drug in 200 ml of a 5% solution of dextrose (glucose) at a rate of 4-5 g / h during surgery and during reperfusion.

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

    Side effects:

    Hypersensitivity to the drug, lowering blood pressure (when rapid intravenous administration).

    Overdose:

    At present, no cases of drug overdose have been reported.

    Interaction:

    When used in combination therapy, the drug Phosphocreatine contributes to an increase in the effectiveness of antiarrhythmic, antianginal agents and agents with a positive inotropic effect.

    Phosphocreatine remains stable 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.

    Application of the drug Phosphocreatine in high doses (5-10 g / day) is accompanied by increased phosphate uptake in the kidneys, which affects calcium metabolism, the secretion of hormones regulating homeostasis, kidney function and purine metabolism,so long-term use of the drug in high doses is not recommended.

    Effect on the ability to drive transp. cf. and fur:

    When using the drug should be careful when working with mechanisms and driving vehicles.

    Form release / dosage:

    Powder for solution for infusion, 0.5 g and 1.0 g.

    Packaging:

    0.5 g or 1.0 g, in terms of sodium phosphocreatine, in bottles of colorless transparent glass (neutral glass, class II), sealed with a rubber stopper made of halogenated butyl rubber, crimped with an aluminum cap with a plastic lining. Each bottle is labeled or labeled with a quick-fixing paint.

    On 1 bottle together with the instruction on application place in a pack a cardboard.

    Storage conditions:

    At a temperature not exceeding 20 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004179
    Date of registration:15.03.2017
    Expiration Date:15.03.2022
    The owner of the registration certificate:ALVILS, LTD. ALVILS, LTD. Russia
    Manufacturer: & nbsp
    Representation: & nbspAlvils, OOOAlvils, OOO
    Information update date: & nbsp05.04.2017
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