Instructions Neoton powder for preparation of infusion solution 1 g bottle No. 4
Composition
active ingredient: phosphocreatine;
1 bottle contains 1 g of sodium phosphocreatine.
Dosage form
Powder for solution for infusion.
Main physicochemical properties: white crystalline powder.
Pharmacotherapeutic group
Cardiological drugs. Phosphocreatine. ATC code C01E B06.
Pharmacological properties
Pharmacodynamics
Phosphocreatine plays a fundamental role in the energy processes that accompany muscle contraction and is used for the resynthesis of ATP - the energy source for myocardial and skeletal muscle contraction. Insufficient energy supply, caused by a slowdown in oxidative metabolism, is the main cause of myocyte damage.
Pharmacological studies of phosphocreatine have shown that:
Prior intramuscular administration of phosphocreatine to animals in a dose-dependent manner counteracts various myocardial injuries caused by the action of chemicals (such as isoprenaline, emetine, thyroxine, p-nitrophenol); phosphocreatine has an inherent positive inotropic effect, which is manifested in the isolated heart of animals in hypodynamic conditions caused by glucose or calcium deficiency or potassium overdose; in the isolated atrium of guinea pigs, phosphocreatine counteracts the negative inotropic effect caused by anoxia; the addition of phosphocreatine to cardioplegic solutions contributes to myocardial protection in many experimental models both in isolated organs and in vivo; phosphocreatine exhibits a protective effect in experimental models of infarction and arrhythmia caused by coronary occlusion.
The cardioprotective effect of phosphocreatine is due to the phenomena of sarcolemma stabilization, preservation of the cellular pool of adenine nucleotides, which is ensured by inhibiting enzymes involved in nucleotide catabolism, inhibition of phospholipid breakdown in ischemic myocardium, and possible improvement of microcirculation in the ischemic area due to inhibition of ADP-induced platelet aggregation.
Pharmacokinetics
In humans, the mean half-life of phosphocreatine after intravenous administration is 0.09 to 0.2 hours. After intramuscular administration of 500 mg of phosphocreatine, it was detectable in the circulation after 5 minutes; maximum phosphocreatine concentrations of approximately 10 nmol/ml were reached 30 minutes after administration, after which they decreased to 4 to 5 nmol/ml after 1 hour. 2 hours after administration, concentrations remained within the measurable range of 1 to 2 nmol/ml.
40 minutes after drip infusion of 5 g of the drug, serum phosphocreatine levels fall below 5 nmol/ml, and after administration of 10 g of the drug they are approximately 10 nmol/ml.
Indication
Intraoperative myocardial ischemia; intraoperative limb ischemia; metabolic disorders of the myocardium in hypoxia: myocardial sclerosis, senile heart, cardiomyopathy due to hypertension, chronic ischemic cardiomyopathy; complex therapy: acute myocardial infarction; acute and chronic heart failure; acute cerebrovascular accident, encephalopathy, as well as hypoxic, ischemic, traumatic and toxic lesions of the central nervous system.
Contraindication
Individual hypersensitivity to the drug.
The drug in high doses (5-10 g per day) is contraindicated in patients with chronic renal failure.
Interaction with other medicinal products and other types of interactions
As part of complex therapy, the drug can increase the effectiveness of antiarrhythmic, antianginal drugs, as well as drugs that positively affect the contractile function of the myocardium.
Application features
Rapid intravenous administration of doses exceeding 1 g may lead to a temporary sharp decrease in blood pressure.
The introduction of high doses of the drug (5 - 10 g / day) leads to the absorption of a large amount of phosphate, which affects calcium metabolism and the secretion of hormones involved in the regulation of homeostasis, renal function and purine metabolism. High doses of the drug can be prescribed only to individual patients and for a short period of time.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no information available today.
Use during pregnancy or breastfeeding
There are no contraindications for using the drug during pregnancy or breastfeeding.
Method of administration and doses
In acute myocardial infarction, the drug is administered to adults in a dose of 2-4 g intravenously in a jet on the first day, followed by a 2-hour drip infusion of a solution containing 8-16 g of the drug in 200 ml of water for injection, 0.9% sodium chloride solution or 5% glucose solution. On the second day, the drug is administered in a dose of 2-4 g intravenously drip 2 times a day. On the third day, the drug is administered in a dose of 2 g intravenously drip 2 times a day. If necessary, a 6-day course of infusions is continued in a dose of 2 g of the drug 2 times a day. The best results of treatment can be obtained if it is started no later than 6-8 hours after the appearance of clinical manifestations of the disease.
Acute and chronic heart failure. In acute heart failure, the drug is administered to adults as a 2-hour intravenous infusion at a dose of 5 - 10 g per day for 3 - 5 days. The appropriate amount of the drug powder is dissolved in 200 ml of water for injection, 0.9% sodium chloride solution or 5% glucose solution. In chronic heart failure, the drug should be administered to adults as an intravenous infusion at a dose of 1 - 2 g twice a day for 10 - 14 days. Each dose of the drug should be dissolved in 50 ml of water for injection, 0.9% sodium chloride solution or 5% glucose solution and administered over 30 - 60 minutes.
In acute cerebral circulation disorders, encephalopathy, as well as in hypoxic, ischemic, traumatic and toxic lesions of the central nervous system, daily infusions of the drug are recommended for adults at a dose of 120 mg/kg of body weight for 3 days.
In case of intraoperative myocardial ischemia, the drug is administered as part of a conventional cardioplegic solution at a concentration of 10 mmol/l (2.5 g/l). NEOTON is added to the cardioplegic solution immediately before administration. It is recommended to conduct a course of infusions of the drug solution at a dose of 2 g twice a day for 3 to 5 days before the operation and for 1 to 2 days after it.
In case of intraoperative limb ischemia, before surgery, adult patients are recommended to administer a solution of 2-4 g of the drug in 50 ml of solvent intravenously over 30-60 minutes. During surgery and the reperfusion period, NEOTON should be administered as intravenous infusions in a dose of 8-10 g dissolved in at least 200 ml of solvent.
In metabolic disorders of the myocardium with hypoxia, the drug is administered to adults intravenously by jet at a dose of 1–2 g per day (the dose is dissolved in 10 ml of solvent) or drip (the dose is dissolved in 50 ml of solvent and administered over 30–60 minutes); the recommended duration of the treatment course is 2–4 weeks.
Children
There is limited information on the use of the drug in the treatment of pediatric patients.
Overdose
In case of a sharp decrease in blood pressure, including due to an overdose of the drug, symptomatic treatment is recommended, including the use of vasoconstrictor drugs. A specific antidote to phosphocreatine is unknown.
Adverse reactions
In some cases, a moderate and short-term decrease in blood pressure was observed during rapid intravenous administration of the drug in doses exceeding 1 g.
Hypersensitivity reactions, including anaphylactic reactions and angioedema, may develop.
Expiration date
3 years.
Do not use after the expiry date stated on the packaging.
Storage conditions
Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
1 g of powder in a glass vial closed with a rubber stopper and a metal crimp ring; 4 vials in a cardboard box.
Vacation category
According to the recipe.
Producer
Alfasigma S.p.A./Alfasigma SpA
Location of the manufacturer and its business address
Via Enrico Fermi 1, 65020 Alanno (Pescara), Italy.
