Novocainamide solution for injection 10%, 5ml No. 10

• with ventricular rhythm disturbances (ventricular tachycardia, ventricular extra-systole);

• atrial tachycardia;

• atrial fibrillation and / or atrial flutter.

When administered intravenously, the drug is diluted in 5% dextrose (glucose) solution or 0.9% sodium chloride solution. The injection rate should not exceed 50 mg / min. In this case, it is necessary to constantly monitor the pulse rate, blood pressure (BP) and electrocardiogram (ECG).
Intravenous: 100-500 mg at a rate of 25-50 mg / min (under the control of blood pressure and ECG) until the relief of paroxysm (maximum dose - 1 g) or intravenous drip: 500-600 mg for 25-30 minutes. The maintenance dose for intravenous drip is 2-6 mg / min, if necessary, 3-4 hours after the end of the infusion, start taking the drug inside.
Intramuscularly: 50 mg per kg of body weight per day in divided doses.
The highest dose for adults with intramuscular and intravenous (drip) administration: single - 1 g (10 ml of the drug), daily - 3 g (30 ml of the drug).
When switching to oral administration of the drug, the first dose is prescribed 3-4 hours after the end of the intravenous infusion.

per 1 ml .:
active substance:
Novocainamide (in terms of 100% substance) - 100 mg
excipients :
Sodium disulfite (sodium metabisulfite) - 5 mg
Water for injection - up to 1 ml

Hypersensitivity to the drug, ventricular arrhythmia caused by intoxication with cardiac glycosides, sinoatrial and atrioventricular block II - III degree (in the absence of an implanted pacemaker), arterial hypotension, cardiogenic shock, ventricular tachycardia of the age of the 'pirouette' type, leukocyte T, prolonged interval years (efficacy and safety have not been established).
With caution
In connection with a possible decrease in myocardial contractility and a decrease in blood pressure, the drug should be prescribed with great caution in myocardial infarction. Arrhythmogenic effect is possible.
His bundle branch block, I degree atrioventricular block, chronic heart failure in the stage of decompensation, myasthenia gravis, bronchial asthma, hepatic and / or renal failure, ventricular tachycardia with coronary artery occlusion, systemic lupus erythematosus (including a history of surgery), interventions (including surgical dentistry), severe atherosclerosis, advanced age.

Trade name of the drug:

Novocainamide-FereinЃ

International non-proprietary name:

procainamide

Dosage form:

injection

Composition:

per 1 ml .:
active substance:
Novocainamide (in terms of 100% substance) - 100 mg
excipients :
Sodium disulfite (sodium metabisulfite) - 5 mg
Water for injection - up to 1 ml

Description:

clear, colorless or slightly yellowish liquid

Pharmacotherapeutic group:

antiarrhythmic agent

Pharmacological properties

Pharmacodynamics
Class 1A antiarrhythmic drug, has a membrane stabilizing effect.
It inhibits the incoming fast current of sodium ions, reduces the rate of depolarization in phase 0.
Inhibits conductivity, slows down repolarization. Reduces the excitability of the atrial and ventricular myocardium. Increases the duration of the effective refractory period of the action potential (to a greater extent in the affected myocardium). The deceleration of conduction, which is observed regardless of the magnitude of the resting potential, is more pronounced in the atria and ventricles, less in the atrioventricular node.
The indirect M-anticholinergic effect, in comparison with quinidine and disopyramide, is less pronounced, therefore, a paradoxical improvement in atrioventricular conduction is usually not observed.
Affects phase 4 depolarization, reduces the automatism of intact and affected myocardium, inhibits the function of the sinus node and ectopic pacemakers in some patients. The active metabolite, N-acetylprocainamide, has a pronounced activity of class III antiarrhythmic drugs, lengthens the duration of the action potential. Has a weak negative inotropic effect (without a significant effect on the minute volume of blood). It has an m-anticholinergic and vasodilating effect, which causes tachycardia and a decrease in blood pressure, total peripheral vascular resistance.
Electrophysiological effects are manifested in the widening of the QRS complex and the lengthening of the PQ and QT intervals. The time to reach the maximum effect with intravenous administration - immediately, with intramuscular administration - 15-60 minutes.

Pharmacokinetics
Penetrates the blood-brain barrier, is secreted in breast milk.
It is metabolized in the liver with the formation of an active metabolite - N-acegyl-procainamide, has a 'first pass' effect. About 25% of the administered procainamide is converted to the specified metabolite, however, with rapid acetylation or chronic renal failure (CRF), 40% of the dose is converted. With CRF or chronic heart failure (CHF), the metabolite rapidly accumulates in the blood to toxic concentrations, while the concentration of procainamide remains within acceptable limits.
The half-life is 2.5-4.5 hours; with chronic renal failure - 11-20 hours; N-acetylprocainamide about 6 hours.
About 25% of the administered drug is excreted by the kidneys (50-60% unchanged), and through the intestines with bile.

Indications for use

The drug is indicated:

• with ventricular rhythm disturbances (ventricular tachycardia, ventricular extra-systole);

• atrial tachycardia;

• atrial fibrillation and / or atrial flutter.

Contraindications

Hypersensitivity to the drug, ventricular arrhythmia caused by intoxication with cardiac glycosides, sinoatrial and atrioventricular block II - III degree (in the absence of an implanted pacemaker), arterial hypotension, cardiogenic shock, ventricular tachycardia of the age of the 'pirouette' type, leukocyte T, prolonged interval years (efficacy and safety have not been established).
With caution
In connection with a possible decrease in myocardial contractility and a decrease in blood pressure, the drug should be prescribed with great caution in myocardial infarction. Arrhythmogenic effect is possible.
His bundle branch block, I degree atrioventricular block, chronic heart failure in the stage of decompensation, myasthenia gravis, bronchial asthma, hepatic and / or renal failure, ventricular tachycardia with coronary artery occlusion, systemic lupus erythematosus (including a history of surgery), interventions (including surgical dentistry), severe atherosclerosis, advanced age.

Application during pregnancy and during breastfeeding

Use only when the benefit to the mother outweighs the potential risk to the fetus / child.
When administered during pregnancy, there is a potential risk of maternal arterial hypotension, which can lead to placental insufficiency.
If necessary, use during lactation, breastfeeding should be discontinued.

Method of administration and dosage

When administered intravenously, the drug is diluted in 5% dextrose (glucose) solution or 0.9% sodium chloride solution. The injection rate should not exceed 50 mg / min. In this case, it is necessary to constantly monitor the pulse rate, blood pressure (BP) and electrocardiogram (ECG).
Intravenous: 100-500 mg at a rate of 25-50 mg / min (under the control of blood pressure and ECG) until the relief of paroxysm (maximum dose - 1 g) or intravenous drip: 500-600 mg for 25-30 minutes. The maintenance dose for intravenous drip is 2-6 mg / min, if necessary, 3-4 hours after the end of the infusion, start taking the drug inside.
Intramuscularly: 50 mg per kg of body weight per day in divided doses.
The highest dose for adults with intramuscular and intravenous (drip) administration: single - 1 g (10 ml of the drug), daily - 3 g (30 ml of the drug).
When switching to oral administration of the drug, the first dose is prescribed 3-4 hours after the end of the intravenous infusion.

Side effect

Nervous system disorders : general weakness, hallucinations, headache, depression, dizziness, convulsions, agitation, insomnia; muscle weakness, psychotic reactions with productive symptoms, ataxia.
Disturbances from the gastrointestinal tract : diarrhea, nausea, vomiting, a feeling of bitterness in the mouth.
Violations of the hematopoietic and hemostatic system : with prolonged use, leukopenia, thrombocytopenia, agranulocytosis, hemolytic anemia with a positive Coombs test.
Sensory Disorders : Taste disorders.
Cardiovascular disorders: with rapid intravenous administration, it is possible to develop collapse, intracardiac blockade, asystole. Decreased blood pressure, ventricular paroxysmal tachycardia.
Others : with prolonged use - medicinal lupus erythematosus.
Allergic reactions : skin rash.

Overdose

Symptoms : confusion, severe dizziness, collapse, nausea, vomiting, cardiac depression, decreased blood pressure, atrioventricular block, asystole, ventricular fibrillation.
Treatment : symptomatic, the use of urine acidifying agents, hemodialysis, with a decrease in blood pressure - the introduction of norepinephrine or phenylephrine; magnesium salts or frequent ventricular pacing with ventricular tachycardia.

Interaction with other medicinal products

Strengthens the effect of depolarizing muscle relaxants (suxamethonium salts), antihypertensive, antiarrhythmic drugs, side effects of bregil tosylate.
When combined therapy with class III antiarrhythmic drugs, the risk of developing an arrhythmogenic effect increases.
Procainamide enhances the hypotensive effect of antihypertensive drugs, the choline-blocking effect of m-anticholinergics, antihistamines, as well as drugs that block neuromuscular transmission, weakens the effect of anticholinesterase drugs.
Reduces the activity of anti-myasthenic drugs.
With simultaneous use with drugs that cause inhibition of bone marrow hematopoiesis, leukopenia and thrombocytopenia may increase.
Cimetidine, ranitidine reduce the renal clearance of procainamide and lengthen the half-life.

special instructions

Before intravenous administration, it is necessary to dilute, inject at a rate of no more than 50 mg / min; should only be used in a hospital setting. When conducting therapy, it is necessary to constantly monitor blood pressure, ECG, peripheral blood counts (at the end of therapy). Elderly patients are more likely to develop arterial hypotension.

Influence on the ability to drive vehicles and mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

Solution for injection 10%.
5 ml in ampoules of colorless neutral glass of the 1st hydrolytic class.
5 ampoules are placed in a blister made of polyvinyl chloride film or in a blister made of polyvinyl chloride film and flexible packaging in rolls based on aluminum foil for medicines, or combined packaging material on a paper basis.
1 or 2 blister packs together with instructions for use and a knife for opening ampoules are placed in a carton box.
5 or 10 ampoules, together with instructions for use and a knife for opening ampoules, are placed in a pack with an insert with cells for ampoules in 1 or 2 rows of cardboard.
When using ampoules with notches or a break ring, the ampoule knife is not inserted.

Storage conditions

Store in a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

5 years.
Do not use the drug after the expiration date printed on the package.

Vacation conditions

Dispensed by prescription