Novokainamid bufus (Novocainamide bufus)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceProcainamideProcainamide
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    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ml of the solution contains:

    active substance: procainamide hydrochloride 100 mg;

    Excipients: sodium disulfite (sodium metabisulphite) 5 mg, water for injection up to 1 ml.

    Description:Transparent colorless or slightly colored liquid.
    Pharmacotherapeutic group:antiarrhythmic drug
    ATX: & nbsp

    C.01.B.A   Antiarrhythmic drugs Ia class

    C.01.B.A.02   Procainamide

    Pharmacodynamics:

    Antiarrhythmic drug IA class. Inhibits incoming high current Na+, 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 AV node.

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

    Affects the depolarization phase 4, reduces the automatism of the intact and affected myocardium, depresses the functionthe 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 (IOC)). Has m-anticholinergic and vasodilating effect. It has vagolytic and vasodilating properties, which causes tachycardia and lowering of arterial pressure (BP), total peripheral vascular resistance (OPSS).

    Electrophysiological effects are manifested in the broadening of the complex QRS and lengthening intervals PQ and QT. 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-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.

    The half-life is 2.5-4.5 h; 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 rhythm disturbances: atrial tachycardia, atrial fibrillation and flutter.

    Contraindications:

    Hypersensitivity to the drug; ventricular arrhythmia caused by intoxication with cardiac glycosides, sinoatrial and atrioventricular blockade II-III (in the absence of an implanted pacemaker), chronic heart failure in the stage of decompensation, arterial hypotension, cardiogenic shock, systemic lupus erythematosus (including in the anamnesis), the period of breastfeeding, ventricular pirouette tachycardia, an extended interval QT, leukopenia, age under 18 years (efficacy and safety not established).

    Carefully:

    In connection with the possible decrease in myocardial contractility and loweringmanagement of blood pressure should be with great care to prescribe the drug for 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 during pregnancy, there is a potential risk of developing arterial hypotension inmother, which can lead to fetoplacental insufficiency.

    Dosing and Administration:

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

    With intravenous administration, the drug is diluted in a 5% solution of glucose or 0.9% solution of sodium chloride. The rate of administration should not exceed 50 mg / min. In this case, a constant monitoring of heart rate (heart rate), blood pressure and electrocardiogram (ECG) is necessary.

    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 you switch to taking the drug inside, the first dose is prescribed 3-4 hours after stopping the intravenous infusion.

    Side effects:

    From the central nervous system: general weakness, hallucinations, depression,muscle weakness, dizziness, headache, insomnia, convulsions, 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: decreased blood pressure, ventricular paroxysmal tachycardia.

    With rapid on / in the introduction of possible collapse, violation of atrial or intraventricular conduction, asystole.

    Allergic reactions: skin rash.

    Overdose:

    Symptoms: the drug has a small therapeutic, breadth, 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 lowering of arterial pressure, pulmonary edema, convulsions, coma, respiratory arrest.

    Treatment: symptomatic. To treat ventricular tachycardia, 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 depolarizing muscle relaxants (salts of suxamethonium), side effects of brethil tosylate.

    With simultaneous use with antihistamines, m-cholinoblocking effects may 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.

    Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

    Special instructions:

    Before intravenous application, it is necessary to dilute, inject at a rate of not more than 50 mg / min.

    It should be used only in a hospital.

    When carrying out therapy, it is necessary to carry out constant monitoring of 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 per ampoule polymer from high-density polyethylene or from low-pressure polyethylene, or from polyethylene for medical purposes, or from polyethylene or polypropylene for infusion solutions and injections.

    For polymer ampoules, labels from label paper, writing or label text are applied directly to the ampoule by a polymer method of drop-jet printing.

    For 10, 100 ampoules of polymer 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 lem.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003624/10
    Date of registration:30.04.2010
    The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC
    Information update date: & nbsp04.09.2015
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