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

Antiarrhythmic drug 1A 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 irrespective 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 (N-APA) has a pronounced activity of antiarrhythmic drugs III class, 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 vagolytic and vasodilating properties, which causes tachycardia and lowering of arterial pressure (BP), a common peripheral vascular resistance.

Electrophysiological effects are manifested in the broadening of the complex QRS and lengthening intervals PQ and QT. Time to achieve maximum effect with oral administration 60-90 min.

Pharmacokinetics:

After ingestion, up to 95% of the dose is absorbed. Bioavailability is 85%. In plasma, it binds to blood proteins - 15-20%. The maximum concentration in the blood plasma for ingestion is reached after 1-2 hours, the maximum concentration is 10 μg / ml. Penetrates through the blood-brain and placental barrier, is secreted with breast milk.

Has the effect of "first passage", is metabolized in the liver with the formation of an active metabolite - N-APA. About 25% of the administered procainamide is converted to this metabolite, but with rapid acetylation or chronic renal failure, 40% of the dose is converted.

In chronic renal failure or chronic heart failure, the metabolite quickly accumulates in the blood to toxic concentrations, while the concentration remains within acceptable limits.

Half-life is 2.5-4.5 hours. With chronic renal failure - 11-20 hours.It is excreted by the kidneys, 50-60% in unchanged form, with bile. Procainamide and N-APA are excreted in hemodialysis, but not with peritoneal dialysis.

Indications:

Applied for various heart rhythm disorders: ventricular arrhythmias (including after myocardial infarction), atrial tachycardia, flicker and atrial flutter.

Contraindications:

Hypersensitivity to the drug, atrioventricular blockade II and III degree (in the absence of an artificial pacemaker), bundle bundle blockage, arrhythmias associated with cardiac glycoside intoxication, ventricular pirouette tachycardia, chronic heart failure, arterial hypotension, cardiogenic shock, severe atherosclerosis, systemic connective tissue diseases including systemic lupus erythematosus), bronchial asthma, leukopenia, lactation, age under 18 years (efficacy and safety not established).

Carefully:

Impaired renal and / or liver function, elderly age, myasthenia gravis, myocardial infarction, lengthening of the interval QT, pregnancy.

Dosing and Administration:

Inside, regardless of food intake.

With ventricular extrasystole - 0.25-1 g, then 0.25-0.5 g every 3-6 hours (if necessary, the daily dose can be increased to 3-4 g), with paroxysms of atrial fibrillation - 1.0- 1.5 g.

After 1 hour (in the absence of effect), another 0.5 g and then every 0.5 hours to 0.5-1.0 g (until the paroxysm has stopped, but no more than 4 hours).

The highest daily dose of 3 g (sometimes 4 g).

Side effects:

From the central nervous system: dizziness, headache, myasthenia gravis, hallucinations, convulsions, drowsiness, depression, psychotic reactions with productive symptoms, ataxia.

From the digestive system: bitter taste in the mouth, nausea, diarrhea.

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

From the sense organs: violation of taste.

From the cardiovascular system: marked decrease in LD, asystole, heart failure, decreased myocardial contractility, atrioventricular block, ventricular paroxysmal tachycardia.

Allergic reactions: skin rash, angioedema.

Other: lupus-like syndrome, fever.

Overdose:

It has a small therapeutic breadth, so heavy intoxication can easily occur (especially with the simultaneous use of other antiarrhythmics).

Symptoms: bradycardia, sinoatrial and atrioventricular blockade, asystole, lengthening of Q-T interval, paroxysms of polymorphic ventricular tachycardia, persistent decrease in blood pressure, pulmonary edema, dry mouth, mydriasis, delirium, convulsions, coma, respiratory arrest.

Treatment: if you have the above symptoms of an overdose, you need urgent medical advice. Before the doctor comes it is recommended to drink a large amount of liquid (2-3 liters) and induce vomiting. Treatment is symptomatic. Hemodialysis.

Interaction:

Concentration in the blood plasma is increased cimetidine, ranitidine, beta-blockers, amiodarone, trimethoprim, quinidine, ofloxacin.

It can not be combined with sparfloxacin.

Strengthens the effect of muscle relaxants, quinidine, lidocaine.

In combination with lidocaine, cardiodepressant effect is enhanced.

Reduces the activity of antimiasthenic drugs.

Special instructions:

In connection with the possible suppression of contractility of the myocardium and lowering of arterial pressure, it is necessary to prescribe with great care the preparation with myocardial infarction.

With the use of novocainamide during pregnancy, there is a potential risk of accumulation of the drug and the development of arterial hypotension in the mother, which can lead to uteroplacental insufficiency.

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving vehicles or performing work requiring increased attention and quick response.

Form release / dosage:

Tablets, 250 mg.

Packaging:

10 tablets per contour cell pack.

For 20 tablets in a can of lightproof glass.

A jar or 2 contour mesh packages together with an instruction for use are placed in a pack of cardboard.

Storage conditions:

In a place protected from light and inaccessible to children at a temperature of no higher than 30 ° C.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006975/08

Date of registration:01.09.2008

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp04.09.2015

Illustrated instructions

Instructions

Novokainamide (Novocainamide)