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

Antiarrhythmic drug IA 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 (AV) node.

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

It affects the depolarization phase 4, reduces the automatism of the intact and affected myocardium, depresses 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 of the 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 P-Q and Q-T. Time to achieve the maximum effect with intravenous administration - immediately, with intramuscular injection - 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-acetyl-procainamide, has the effect of a "first pass". About 25% of the administered procainamide is converted into the specified metabolite, however, with fast acetylation or chronic renal failure (CH1H), 40% dose. In chronic renal failure or chronic heart failure, the metabolite rapidly 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 drug is excreted by the kidneys (50-60% unchanged), with bile.

Indications:

Ventricular arrhythmias: ventricular tachycardia, ventricular extrasystole.

Atrial tachycardia, flicker and / or atrial flutter.

Contraindications:Hypersensitivity to the drug components, ventricular arrhythmia caused by intoxication with cardiac glycosides, sinoatrial and atrioventricular blockade of II and III degree (in the absence of implantedpacemaker), chronic heart failure in the stage of decompensation, arterial hypotension, cardiogenic shock, systemic lupus erythematosus (including in the anamnesis), the period of breastfeeding, ventricular arrhythmias of the "pirouette" type, an extended QT interval, leukopenia, flutter or fibrillation of the ventricles, age under 18 years (efficacy and safety not established).

Carefully:

In connection with a possible reduction in myocardial contractility and a decrease in blood pressure, caution should be given to prescribing with myocardial infarction. Perhaps the arrhythmogenic effect.

Myocardial blockade of the first bundle, myasthenia gravis, bronchial asthma, hepatic and / or renal failure, chronic heart failure, ventricular tachycardia with occlusion of the coronary artery, surgical interventions (including surgical dentistry), severe atherosclerosis, elderly age .

Pregnancy and lactation:

Apply only if the benefit to the mother exceeds the potential risk to the fetus / child.

When prescribing the drug during pregnancy, there is a potential risk of developing arterial hypotension in the mother,which can lead to uteroplacental insufficiency.

Dosing and Administration:

Intravenously: 100-500 mg at a speed of 25-50 mg / min (under the control of blood pressure and electrocardiograms (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.

With heart failure of grade II, the dose is reduced (by 1/3 or more). Intramuscularly inject 5-10 ml (up to 20-30 ml per day). When administered intravenously, the drug is diluted in 5% solution of glucose or a solution of sodium chloride 0.9%. The rate of administration should not exceed 0.05 g / min. This requires a constant monitoring of heart rate. AD and ECG. The highest dose for adults with intramuscular and intravenous (drip) administration: one-time - I g (10 ml of the drug), daily - 3 g (30 ml of the drug). When switching to taking the drug inside, the first dose is prescribed 3-4 hours after the cessation of IV infusion.

Side effects:

From the central nervous system: general weakness, hallucinations, depression, myasthenia gravis, dizziness, headache, insomnia, seizures, psychotic reactions with productive symptoms, ataxia.

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

From the side of the cardiovascular system: reduction of blood pressure, ventricular paroxysmal tachycardia.

With rapid intravenous administration, the development of collapse, the violation of atrial or intraventricular conduction, asystole.

Allergic reactions: skin rash.

Overdose:

Symptoms: the drug has a small therapeutic latitude, so heavy intoxication can easily occur (especially with the simultaneous use of other antiarrhythmics): bradycardia, sinoatrial and atrioventricular blockades, asystole, lengthening of the interval Q-T, paroxysms of polymorphic ventricular tachycardia, decreased myocardial contractility, persistent arterial hypotension, pulmonary edema, convulsions, coma, respiratory arrest.

Treatment: hemodialysis. With a decrease in blood pressure - the administration of norepinephrine or phenylephrine. For the treatment of ventricular tachycardia caused by an overdose of procainamide. do not use antiarrhythmic drugs IA or 1C classes. Sodium bicarbonate can eliminate the expansion of the complex QRS or arterial hypotension.

Interaction:

Strengthens the effect of antiarrhythmic, hypotensive, anticholinergic and cytostatic agents, muscle relaxants, side effects of brethil tosylate.

With simultaneous use with antihistamines, atropine-like effects can be enhanced; with pimozide - lengthening of the interval Q-T.

Reduces the activity of antimiasthenic drugs.

Cimetidine, ranitidine reduce renal clearance of procainamide and prolong the half-life.

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

Medicines, which inhibit bone marrow hematopoiesis, increases the risk of myelosuppression.

Special instructions:

Before intravenous application, it is necessary to dilute, inject at a rate not exceeding 50 mg / min; should be taken only in a hospital.

When carrying out therapy, it is necessary to monitor blood pressure, ECG, peripheral blood formulas (at the end of therapy).

In elderly patients, the development of arterial hypotension is more likely.

Form release / dosage:Solution for intravenous and intramuscular injection, 100 mg / ml.

Packaging:

5 ml of the drug into neutral glass ampoules.

For 10 ampoules together with a knife ampoule or scarifier ampoule and instructions for use will be placed in a box of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Not Use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-000621/10

Date of registration:03.02.2010

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)