Novokainamide (Novocainamide)

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 (novocainamide) in terms of 100% of the substance - 100 mg,

    Excipients: sodium Disulfite (sodium pyrosulfite technical, sodium metabisulphite) - 5 mg, water for injection - up to 1 ml.

    Description:

    Transparent, colorless or slightly yellowish 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, 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, 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 class III, lengthens the duration of the action potential.

    Has a weak negative inotropic effect (without significant influence on the IOC). 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. The time to achieve the maximum effect when administered / administered - 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 into the specified metabolite, but with rapid acetylation or chronic renal failure (CRF), 40% dose. 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-acetylprocainamide - 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 / or atrial 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), flutter or fibrillation of the ventricles.

    Carefully:

    In connection with a possible decrease in myocardial contractility and a decrease in blood pressure from great caution in prescribing the drug for myocardial infarction. Perhaps the arrhythmogenic effect.

    Myocardial blockade of the first degree, myasthenia gravis, bronchial asthma, hepatic and / or honorable 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.

    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.

    Dosing and Administration:

    Intravenously: 100-500 mg at a rate of 25-50 mg / min (under control of BP and ECG) to paroxysm (maximum dose g -1) or intravenously: 500-600 mg per 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% glucose solution or 0.9% sodium chloride solution. The rate of administration should not exceed 0.05 g / min. In this case, constant monitoring of heart rate, blood pressure and ECG is necessary.

    Higher dose for adults with intramuscular and intravenous (infusion) administration: single - 1 g (10 ml preparation) daily - 3 g (30 ml preparation).

    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 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 latitude, so heavy intoxication can easily occur (especially when using 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: symptomatic. To treat ventricular tachycardia, do not use antiarrhythmic drugs IA or IC classes. Sodium bicarbonate can eliminate the expansion of the complex QRS or arterial hypotension.

    Interaction:

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

    With simultaneous use with antihistamine drugs, 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 / in the application must be diluted, injected at a rate of not more than 50 mg / min; 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 intramuscular and intravenous administration, 100 mg / ml.
    Packaging:

    5 ml into neutral glass ampoules.

    For 10 ampoules together with the instruction for use and scarifier ampoule ceramic in a box of cardboard.

    5 ampoules per contour cell pack.

    2 contour mesh packages together with instructions for use and a ceramic ampoule scarifier in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of 0 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N000789 / 01
    Date of registration:22.01.2008
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspMOSHIMFARM PREPARATES them. NA Semashko OJSC MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia
    Information update date: & nbsp04.09.2015
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