Novokainamid-Ferein - instructions for use, dose, side effects, contraindications

Antiarrhythmic drug I A class, has a membrane-stabilizing effect. It inhibits the incoming fast current of sodium ions, reduces the rate of depolarization into phase 0. Depresses the conductivity, slows repolarization. Reduces the excitability of the myocardium of the atria and ventricles. Increases the duration of the effective refractory period of the action potential (in the affected myocardium - to a greater extent).The conduction slowdown, which is observed regardless of the magnitude of the resting potential, is more pronounced in the atria and ventricles, less in the atrioventricular node.

Indirect M-holinoblokiruyuschy effect, compared with quinidine and disopyramide, expressed less, so the paradoxical improvement of atrioventricular conductivity is usually not noted.

It affects the depolarization phase 4, reduces the automatism of the intact and affected myocardium, inhibits the function of the sinus node and ectopic rhythm drivers in some patients.

Active metabolite - N-acetylprocainamide has a pronounced activity of antiarrhythmic drugs of the III class, lengthens the duration of the action potential.

Has a weak negative inotropic effect (without a significant effect on cardiac output). It has a vagolytic and vasodilating properties, which causes tachycardia and a reduction in blood pressure, a common peripheral vascular resistance.

Electrophysiological effects are manifested in the broadening of the complex QRS and lengthening intervals PQ and QT. The time to achieve the maximum effect with / in the introduction - immediately, with a / m - 15-60 minutes.

Pharmacokinetics:

Penetrates through the blood-brain barrier, it is secreted with breast milk. Metabolized in the liver with the formation of an active metabolite - N-acetylprocainamide, has the effect of a "first pass". About 25% of the administered procainamide is converted to this metabolite, but with rapid acetylation or chronic renal failure (CRF), 40% of the dose is converted. With CRF or chronic heart failure, the metabolite quickly accumulates in the blood to toxic concentrations, while the concentration of procainamide remains within acceptable limits.

Half-life is 2.5-4.5 hours; with CRF - 11-20 hours; N-Acetylprokainamide - about 6 hours. About 25% of the injected is excreted by the kidneys (50-60% unchanged), with bile.

Indications:

Ventricular arrhythmias (ventricular tachycardia, ventricular extrasystole), atrial tachycardia, flicker and atrial flutter.

Contraindications:

Hypersensitivity to the drug, ventricular arrhythmia caused by intoxication with cardiac glycosides, sinoatrial and atrioventricular blockades of II-III degree (in the absence of an implanted pacemaker),chronic heart failure, arterial hypotension, cardiogenic shock, renal and hepatic insufficiency, systemic lupus erythematosus, pregnancy and the period of breastfeeding, ventricular pirouette tachycardia, an elongated interval QT, myasthenia gravis, bronchial asthma, severe atherosclerosis, leukopenia, age under 18 years (efficacy and safety not established).

Carefully:In connection with the possible reduction in myocardial contractility and lowering of arterial pressure, it is necessary to prescribe with great care the drug with myocardial infarction.

Dosing and Administration:

Intravenously: 100-500 mg at a speed of 25-50 mg / min (under the control of blood pressure and ECG) to arrest paroxysm (maximum dose - 1 g) or intravenously drip: 500-600 mg for 25 -30 minutes. The maintenance dose for intravenous drip introduction is 2-6 mg / min, if necessary, 3-4 hours after stopping the infusion, start taking the drug inside.

Intramuscularly: 50 mg per kg of body weight per day in divided doses.

With intravenous administration, the drug is diluted in a 5% solution of dextrose (glucose) or 0.9% sodium chloride solution. The rate of administration should not exceed 0.05 g / min.In this case, it is necessary to constantly monitor the pulse rate, arterial pressure and ECG.

The highest dose for adults with intramuscular and intravenous (drip) introduction: single-dose - 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 cessation of IV infusion.

Side effects:

From the nervous system: general weakness, headache, depression, dizziness, convulsions, agitation, insomnia; muscle weakness, psychotic reactions with productive symptoms, ataxia.

From the digestive system: diarrhea, nausea, vomiting, bitterness in the mouth,

On the part of the organs of hematopoiesis and the system of hemostasis: with long-term use - leukopenia, thrombocytopenia, agranulocytosis, hemolytic anemia with a positive breakdown Coombs.

From the sense organs: violation of taste.

From the side of the cardiovascular system: with rapid intravenous injection, the development of collapse, intracardiac blockade, asystole. Reduction of arterial pressure, ventricular paroxysmal tachycardia.

Other: with prolonged use - drug lupus erythematosus.

Allergic reactions: skin rash.

Overdose:

Symptoms: confusion, severe dizziness, collapse, nausea, vomiting, oppression of cardiac activity, lowering of arterial pressure, atrioventricular blockade, asystole, ventricular fibrillation.

Treatment: symptomatic, the use of drugs that acidify urine, hemodialysis with a decrease in blood pressure - the introduction of norepinephrine or phenylephrine; magnesium salts or frequent stimulation of the ventricles with ventricular tachycardia.

Interaction:

With the simultaneous use of procainamide with other antiarrhythmic drugs, an antiarrhythmic effect may increase.

Procainamide enhances the antihypertensive effect of antihypertensive drugs, the anticholinergic anticholinergic action of cholinoblockers, antihistamines, and neuromuscular blocking agents, weaken the action of anticholinesterase drugs.

With simultaneous use with drugs that cause oppression of bone marrow hematopoiesis, it is possible to increase leukopenia and thrombocytopenia.

Enhances the effect of cytostatic agents, side effects of brethil tosylate.

Cimetidine reduces the renal clearance of procainamide and prolongs the half-life.

With combined therapy with antiarrhythmic drugs of III class, the risk of arrhythmogenic effect increases.

Special instructions:

When carrying out therapy, it is necessary to monitor blood pressure, monitor ECG, peripheral blood, especially leukocytes (every 2 weeks for the first three months of therapy, then at longer intervals).

During prolonged treatment or with symptoms similar to systemic lupus erythematosus, it is necessary to periodically determine the titer of antinuclear antibodies.

At appointment during pregnancy there is a potential risk of development of an arterial hypotension at mother that can lead to a utero-placental insufficiency.

Form release / dosage:Solution for injection, 10%.

Packaging:

In ampoules of 5 ml.

5 ampoules into the contour cell package.

1 or 2 contour packagings with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use at the end of the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002646 / 01-2003

Date of registration:08.07.2008

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Representation: & nbspBRYNTSALOV-A, CJSCBRYNTSALOV-A, CJSC

Information update date: & nbsp04.09.2015

Illustrated instructions

Instructions

Novokainamid-Ferein (Novocainamide-Ferein)