Phosphocreatine
Phosphocreatine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Phosphocreatine
ATX code: C01EB06
Active ingredient: phosphocreatine (Phosphocreatine)
Manufacturer: Hebei Tiancheng Pharmaceutical Co., Ltd. (Hebei Tiancheng Pharmaceutical Co., Ltd.) (China)
Description and photo updated: 2020-19-03
Phosphocreatine - a drug that improves myocardial and muscle tissue metabolism; cardioprotector.
Release form and composition
The preparation is produced in the form of a powder for the preparation of a solution for infusion: crystalline, almost white or white [0.5 or 1 g each (in terms of sodium phosphocreatine) in a transparent colorless glass bottle, sealed with a rubber stopper with a crimped aluminum cap; in a cardboard box 1 bottle and instructions for the use of Phosphocreatine].
Composition for 1 bottle: active substance - sodium phosphocreatine tetrahydrate - 0.64 or 1.28 g, which is equivalent to sodium phosphocreatine in an amount of 0.5 and 1 g, respectively.
Pharmacological properties
Pharmacodynamics
Phosphocreatine plays an important role in the energy mechanism of muscle contraction. This substance is a reserve of energy in the cells of the heart and skeletal muscles and is used to re-produce adenosine triphosphoric acid (ATP), in the process of hydrolysis of which energy is released for the contractile movement of muscle fibers, provided by the protein actomyosin.
The lack of energy received by cardiomyocytes due to a slowdown in oxidative processes is a key mechanism for the onset and progression of damage to the heart muscle. Deficiency of phosphorocreatine leads to a weakening of the force of contraction of the myocardium and a decrease in its ability to restore functions. In cases of damage to the heart muscle, there is a close correlation between the viability of cells, the number of energy-rich phosphorylated compounds they contain, and the ability to restore cell contractility.
The cardioprotective effect of Phosphocreatine, established in the course of preclinical and clinical studies, is manifested in the form of a dose-dependent positive effect against the background of toxic effects on the heart muscle of emetine, isoprenaline, thyroxine, p-nitrophenol; positive inotropic action with a lack of glucose, calcium ions, or with an overdose of the latter; weakening the negative inotropic effect associated with anoxia.
In addition, the inclusion of a drug in cardioplegic solutions at a concentration of 10 mmol / L increases the cardioprotective effect, including providing:
- reducing the risk of myocardial ischemia on the background of cardiopulmonary bypass grafting;
- weakening the threat of the development of reperfusion arrhythmia during infusion before the onset of experimental regional ischemia caused by the imposition of a ligature for 15 minutes on the anterior descending branch of the left coronary artery;
- reducing the degradation of phosphocreatine and ATP in the cells of the heart muscle, preserving the structure of the sarcolemma and mitochondria, improving the process of functional recovery of the myocardium after cardiac arrest as a result of high-dose potassium administration, and reducing the incidence of reperfusion arrhythmia.
In an experiment with arrhythmia and myocardial infarction (MI), arising from occlusion of the coronary artery, the agent demonstrates a cardioprotective effect: it preserves the cellular pool of adenine nucleotides as a result of suppression of the enzymes that cause them catabolism, blocks the degradation of phospholipids, presumably contributes to the improvement of microcirculation in the area of ischemia mediated inhibition. platelets. Phosphocreatine also normalizes hemodynamic parameters, does not allow a sharp decrease in the functional parameters of the heart, exhibits antiarrhythmic action, helps to limit the MI zone, and reduces the frequency and duration of ventricular fibrillation.
Pharmacokinetics
After a single intravenous (IV) infusion of the drug, its maximum concentration (C max) in the blood plasma is fixed for 1-3 minutes. The greatest amount of phosphocreatine accumulates in the brain, skeletal and cardiac muscles, in a small dose - in the tissues of the lungs and liver.
Elimination of the agent is two-phase (fast and slow phases), which is associated with its accumulation in tissues and with further excretion from the body in the second phase. In the fast phase, the half-life (T 1/2) of the drug is 30–35 minutes, in the slow phase - several hours. The agent is excreted by the kidneys.
Indications for use
The metabolic drug is recommended for use in the combined treatment of the following diseases:
- acute MI;
- intraoperative myocardial ischemia;
- chronic heart failure (CHF);
- intraoperative ischemia of the lower extremities.
Phosphocreatine is also used in sports medicine in order to prevent the occurrence of acute / chronic physical overstrain syndrome and to improve the adaptation process to extreme physical exertion.
Contraindications
Absolute:
- age up to 18 years;
- breast-feeding;
- chronic renal failure (CRF) when the drug is prescribed in daily doses of 5–10 g;
- hypersensitivity to phosphocreatine.
With caution and only under the supervision of a specialist, it is allowed to use the drug in pregnant women, provided that the expected benefit to the mother outweighs the possible threat to the fetus.
Phosphocreatine, instructions for use: method and dosage
Solution for infusion Phosphocreatine should be administered only by intravenous drip or as a rapid infusion.
Recommended dosage regimen:
- acute MI: I day - as a rapid infusion at a dose of 2-4 g, dissolved in 50 ml of water for injection (d / s), then infused over 2 hours at a dose of 8-16 g, diluted in 200 ml of dextrose solution (glucose) 5%; II day - drip for at least 30 minutes, 2 times / day at a dose of 2-4 g in 50 ml of water d / i; III day - drip 2 times / day, 2 g in 50 ml of water d / i, duration of infusion - at least 30 minutes, if necessary, infusion in a given daily dose can be carried out within 6 days;
- intraoperative myocardial ischemia: drip 2 times / day for at least 30 minutes at a dose of 2 g in 50 ml of water for 3–5 days before and 1–2 days after surgery; during the operation, the agent is added immediately before the introduction into the usual cardioplegic solution at a concentration of 2.5 g / l or 10 mmol / l;
- CHF: taking into account the patient's condition, treatment can be started in shock doses - drip at a rate of 4-5 g / h, 5-10 g in 200 ml of 5% dextrose (glucose) solution for 3-5 days, and then drip lasting at least 30 minutes 2 times / day at a dose of 1-2 g in 50 ml of water d / and for 14-42 days, or immediately start therapy with drip infusion in maintenance doses - 1-2 g in 50 ml of water d / and 2 times / day, course - 14–42 days;
- intraoperative ischemia of the lower extremities: in the form of a rapid infusion at a dose of 2-4 g in 50 ml of water d / and before surgery with further drip infusion at a rate of 4-5 g / h at a dose of 8-10 g in 200 ml of dextrose (glucose) 5% during surgery and during reperfusion;
- prevention of the syndrome of acute / chronic physical overstrain and in order to improve adaptation to excessive physical exertion (in sports medicine): drip in a daily dose of 1 g in 50 ml of water d / and with an infusion duration of at least 30 minutes, course - 21-28 days …
Side effects
Against the background of treatment with Phosphocreatine, undesirable phenomena such as a decrease in blood pressure (with rapid intravenous infusion) and hypersensitivity reactions to the agent may occur.
Overdose
Cases of drug overdose have not been registered so far.
special instructions
The drug must be administered as soon as possible after the onset of ischemic signs to ensure the most favorable prognosis of the disease.
The introduction of a cardioprotective agent in high daily doses (5–10 g) leads to an increased uptake of phosphates in the kidneys, thereby affecting calcium metabolism, the production of hormones regulating homeostasis, purine metabolism and renal function. As a result, long-term use of Phosphocreatine in high doses is not recommended.
Influence on the ability to drive vehicles and complex mechanisms
During therapy, it is recommended to drive vehicles and other mechanisms with caution.
Application during pregnancy and lactation
There are no clinical data on the use of the drug during pregnancy. According to the results obtained in the course of animal studies, the metabolic agent did not have a toxic effect on the embryofetal development of rabbits and the fertility of rats. The use of Phosphocreatine in pregnant women is allowed only if the expected benefit to the woman outweighs the possible threat to the fetus.
For women who are breastfeeding, Phosphocreatine is contraindicated. Breastfeeding should be discontinued during the treatment period.
Pediatric use
Since the safety and efficacy of phosphocreatine therapy in persons under 18 years of age have not been established, the drug is contraindicated in patients of this age group.
With impaired renal function
For patients with chronic renal failure, the use of the drug in daily doses of 5-10 g is contraindicated.
Drug interactions
When used as part of a complex treatment, Phosphocreatine contributes to an increase in the effectiveness of antianginal, antiarrhythmic drugs, as well as drugs with a positive inotropic effect.
Phosphocreatine remains stable in cardioplegic solutions, water d / i, dextrose (glucose) solution 5%.
Analogs
The analogue of Phosphocreatine is Neoton.
Terms and conditions of storage
Store out of reach of children at a temperature not exceeding 20 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Phosphocreatine
Currently, there are no reviews on Phosphocreatine on specialized sites, therefore it is not possible to make an objective assessment of the shortcomings and effectiveness of the cardioprotector.
Phosphocreatine price in pharmacies
There is no reliable information about the price of Phosphocreatine, since the metabolic agent is not currently sold in the pharmacy network. The cost of an analogue of the drug, Neoton, in the form of a powder for the preparation of a solution for infusion (1 g in a vial) can be 4850-5050 rubles. for 4 bottles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
