Новокаинамид-Ферейн®

General characteristics. Structure:

Active ingredient: 100 mg of a novokainomid in 1 ml of solution.

Excipients: sodium pyrosulphite, water for injections.

Pharmacological properties:

Pharmacodynamics. Antiarrhytmic drug I of the Class A, has membrane stabilizing effect.

Brakes the entering bystry current of ions of sodium, reduces depolarization speed in a phase 0. Conductivity oppresses, slows down repolarization. Reduces excitability of a myocardium of auricles and ventricles. Increases duration of the effective refractory period of action potential (in the affected myocardium - more). Conductivity delay which is observed irrespective of rest potential size is more expressed in auricles and ventricles, it is less in an atrioventricular node.

Indirect M-holinoblokiruyushchy the effect, in comparison with quinidine and Disopyramidum, is expressed less therefore paradoxical improvement of atrioventricular conductivity usually is not noted.

4 depolarizations influence a phase, reduces automatism of the intact and affected myocardium, oppresses function of a sinus node and ectopic pacemakers at some patients.

The active metabolite - N-atsetilprokainamid has the expressed activity of antiarrhytmic means of the III class, extends action potential duration.

Possesses a weak negative inotropic effect (without significant effect on cordial emission). Has vagolytic and vazodilatiruyushchy properties that causes tachycardia and a lowering of arterial pressure, the general peripheric vascular resistance.

Electrophysiologic effects are shown in broadening of the QRS complex and lengthening of intervals of PQ and QT. Time of achievement of the maximum effect at in introduction - immediately, at in oil - 15-60 min.

Pharmacokinetics. Gets through a blood-brain barrier, cosecretes with breast milk. It is metabolized in a liver with formation of an active metabolite – N-acetyl-prokainamida, has effect of "the first passing". About 25% of the entered procaineamide turn into the specified metabolite, however at bystry acetylation or the chronic renal failure (CRF) 40% of a dose are exposed to transformation. At HPN or chronic heart failure the metabolite quickly collects in blood to toxic concentration, at the same time concentration of procaineamide remains in acceptance limits.

Elimination half-life - 2,5-4,5 hours; at HPN - 11-20 h; N-atsetilprokainamida about 6 h. About 25% of entered are removed by kidneys (50-60% in not changed look), with bile.

Indications to use:

Ventricular disturbances of a rhythm (ventricular tachycardia, ventricular premature ventricular contraction), atrial tachycardia, blinking and atrial flutter.

Route of administration and doses:

Intravenously: 100-500 mg with a speed of 25 - 50 mg/min. (under control of the ABP and an ECG) before stopping of a paroxysm (the maximum dose - 1 g) or intravenously kapelno: 500-600 mg in 25 - 30 min. The maintenance dose at intravenous drop administration - 2-6 mg/min., if necessary in 3-4 hours after the termination of infusion to begin administration of drug inside.

Intramusculary: 50 mg on body weight kg a day in the divided doses.

At intravenous administration drug is dissolved in 5% solution of a dextrose (glucose) or solution of sodium of chloride of 0,9%. Rate of administering should not exceed 0,05 g/min. At the same time it is necessary to watch pulse rate, arterial pressure and an ECG constantly.

The highest dose for adults at introduction intramuscular and intravenous (kapelno): one-time - 1 g (10 ml of drug), daily - 3 g (30 ml of drug).

Upon transition to oral administration of drug, the first dose is appointed in 3-4 hours after the termination in/in infusion.

Features of use:

When performing therapy it is necessary to carry out monitoring of arterial pressure, control of an ECG, indicators of peripheral blood, especially leukocytes (each 2 weeks within the first three months of therapy, further with longer intervals).

During long treatment or at manifestation of the symptoms similar to a system lupus erythematosus, it is necessary to define a caption of antinuclear antibodies periodically.

At appointment during pregnancy there is a potential risk of development of arterial hypotension in mother that can result in uteroplacental insufficiency.

Side effects:

From a nervous system: general weakness, headache, depression, dizziness, spasms, excitement, sleeplessness; muscular weakness, psychotic reactions with productive symptomatology, an ataxy.

From the alimentary system: diarrhea, nausea, vomiting, feeling of bitterness in a mouth.

From bodies of a hemopoiesis and system of a hemostasis: at prolonged use - a leukopenia, thrombocytopenia, an agranulocytosis, hemolitic anemia with positive test of Koombs.

Co of the party of sense bodys: taste disturbances.

From cardiovascular system: at bystry intravenous administration development of a collapse, endocardiac blockade, an asystolia is possible. Lowering of arterial pressure, ventricular Bouveret's disease.

Others: at prolonged use - a medicinal lupus erythematosus.

Allergic reactions: skin rash.

Interaction with other medicines:

At simultaneous use of procaineamide with other antiarrhytmic drugs strengthening of antiarrhytmic effect is possible.

Procaineamide strengthens hypotensive effect of anti-hypertensive drugs, holinoblokiruyushchy action of m-holinoblokatorov, antihistaminic drugs, and also the means blocking neuromuscular transmission weakens action of antikholinesterazny means.

At simultaneous use with the drugs causing oppression of a marrowy hemopoiesis strengthening of a leukopenia and thrombocytopenia is possible.

Strengthens effect of cytostatic means, side effects of a bretylium of tosylate. Cimetidinum reduces renal clearance of procaineamide and extends an elimination half-life.

At a combination therapy with antiarrhytmic means of the III class, the risk of development of aritmogenny effect increases.

Contraindications:

Hypersensitivity to drug; the ventricular arrhythmia caused by intoxication cardiac glycosides, sinuatrial and atrioventricular blockade of the II-III degree (in the absence of the implanted electrocardiostimulator), chronic heart failure, arterial hypotension, cardiogenic shock, a renal and liver failure, a system lupus erythematosus, pregnancy and the period of breastfeeding, ventricular tachycardias like "pirouette", the extended QT interval, a myasthenia, bronchial asthma, the expressed atherosclerosis, a leukopenia, age up to 18 years (efficiency and safety are not established).

Due to the possible decrease in contractility of a myocardium and a lowering of arterial pressure it is necessary to appoint carefully drug at a myocardial infarction.

Overdose:

Symptoms: confusion of consciousness, severe dizziness, collapse, nausea, vomiting, oppression of cordial activity, lowering of arterial pressure, atrioventricular block, asystolia, fibrillation of ventricles.

Treatment - symptomatic, use of the cure acidifying urine, a hemodialysis for a lowering of arterial pressure - introduction of Norepinephrinum or Phenylephrinum; salts of magnesium or frequent stimulation of ventricles at ventricular tachycardia.

Storage conditions:

List B. In the place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 5 years. Not to use upon termination of the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

10% solution for injections in ampoules of 5 ml. 5 ampoules in a blister strip packaging. 1 or 2 blister strip packagings with the application instruction place in a pack from a cardboard.