Procainamide (Procainamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antiarrhythmics

Included in the formulation
  • Novokainamide
    solution w / m in / in 
    BINNOFARM, CJSC     Russia
  • Novokainamide
    solution w / m in / in 
    ORGANICS, JSC     Russia
  • Novokainamide
    pills inwards 
    ORGANICS, JSC     Russia
  • Novokainamide
    solution w / m in / in 
    MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC     Russia
  • Novokainamid bufus
    solution w / m in / in 
    UPDATE OF PFC, CJSC     Russia
  • Novokainamid-Ferein
    solution for injections 
    BRYNTSALOV-A, CJSC     Russia
  • Prokainamid-Eskom
    solution w / m in / in 
    ESKOM NPK, OAO     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    C.01.B.A   Antiarrhythmic drugs Ia class

    C.01.B.A.02   Procainamide

    Pharmacodynamics:

    Refers to antiarrhythmic drugs IA class. It blocks sodium channels, inhibits the incoming fast current of sodium ions, reduces the rate of depolarization into phase 0. Reduces the conductivity and excitability of Purkinje fibers, inhibits impulses from the atria, AV (atrioventricular) node. It blocks potassium channels and thereby prolongs phases 3, lengthens the effective refractory period of the Purkinje fiber. It blocks sodium channels in phase 4, prolongs it, thereby suppressing the automatism of Purkinje fiber, sinus node and ectopic rhythm drivers, increases the threshold of ventricular myocardial fibrillation.

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

    Has a weak negative inotropic effect. Has vasodilating properties, which causes a decrease in blood pressure and reflex tachycardia. Electrophysiological effects are manifested in the broadening of the QRS complex and in the elongation of the PQ and QT intervals.

    The active metabolite N-acetylprocainamide has a pronounced activity of antiarrhythmic drugs of the III class, prolongs the duration of the action potential.

    Pharmacokinetics:

    Time to achieve maximum effect with oral administration of 60-90 minutes, with intravenous administration - immediately, with intramuscular - 15-60 minutes.

    After oral administration, up to 95% of the dose is absorbed. Plasma binds to proteins 15-25%. Biotransformiruetsya in the liver with the formation of an active metabolite - N-acetylprokainamide. Half-life is 2.5-4.5 hours Excreted by the kidneys, with 50-60% unchanged; the rate of excretion of the active metabolite is lower in comparison with the initial compound. Passes through the placenta and penetrates into breast milk.

    Indications:

    Atrial flutter, paroxysmal atrial fibrillation, supraventricular tachycardia (including WPW syndrome), ventricular extrasystole, ventricular tachycardia.

    Ventricular arrhythmias: extrasystole, paroxysmal ventricular tachycardia. Nadzheludochkovye arrhythmia: paroxysmal atrial fibrillation or atrial flutter, supraventricular tachycardia (including WPW syndrome).

    ICD-10

    IX.I30-I52.I47.2   Ventricular tachycardia

    IX.I30-I52.I47.1   Nadzheludochkovaya tachycardia

    IX.I30-I52.I45.6   Syndrome of premature agitation

    IX.I30-I52.I48   Atrial fibrillation and flutter

    IX.I30-I52.I49.3   Premature depolarization of the ventricles

    IX.I30-I52.I49.8   Other specified disorders of heart rhythm

    Contraindications:Hypersensitivity(in the absence of an artificial pacemaker), flutter or fibrillation of the ventricles, ventricular arrhythmia against the background of cardiac glycoside intoxication, leukopenia, arterial hypotension, cardiogenic shock, ventricular pirouette tachycardia, an elongated interval QT, age to 18 years
    Carefully:

    Myocardial infarction, bundle branch blockade, myasthenia gravis, systemic lupus erythematosus (incl.a history of asthma), bronchial asthma, decompensated chronic heart failure, ventricular tachycardia with coronary artery occlusion, surgical interventions (including surgical dentistry), severe atherosclerosis, atrioventricular block I degree, myasthenia gravis, hepatic and / or renal failure, ventricular tachycardia with occlusion of the coronary artery, systemic lupus erythematosus, elderly age.

    In connection with the possible inhibition of myocardial contractility and lowering blood pressure should be used with great caution in myocardial infarction. It is not recommended for severe heart failure and severe atherosclerosis. When using procainamide in pregnant women, there is a potential risk of cumulation and development of hypotension in the mother, which can lead to uteroplacental insufficiency. Care should be taken when driving vehicles or performing work that requires special attention.

    Pregnancy and lactation:

    Recommendations FDA category C. Adequate and well-controlled studies in humans have not been conducted. Procainamide and N-acetylprocainamide penetrate the placental barrier, are found in the fetal serum. There is a potential risk of accumulation of procainamide and utero-placental insufficiency and ventricular arrhythmias due to maternal hypotension.

    The drug should be used when the benefits for pregnant women and mothers exceed the potential risk to the fetus and newborn.

    Procainamide and N-acetylprocainamide penetrate into breast milk.

    If it is necessary to use during lactation, breastfeeding should be discontinued.

    Dosing and Administration:Inside, intravenously, intramuscularly. Dosing regimen is individual. When administered orally, the initial dose is usually 0.25-1 g, then 0.25-0.5 g every 3-6 hours. The maximum daily dose is 3-4 g. W / m: 50 mg / kg / day in divided doses every 3-6 hours. In / in (previously diluted in 0.9% solution of sodium chloride or 5% solution of dextrose) at a rate of not more than 50 mg / min; IV infusion is performed under the control of ECG and blood pressure. Higher doses for adults with / m and / in (drip) introduction: one-time - 1 g, daily - 3 g.
    Side effects:

    From the nervous system and sensory organs: hallucinations, depression, myasthenia gravis, dizziness, headache, convulsions, psychotic reactions with productive symptoms, ataxia, taste disorder.

    On the part of the digestive system: nausea, diarrhea, bitterness in the mouth.

    From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): lowering blood pressure, reducing myocardial contractility, ventricular paroxysmal tachycardia, heart failure. With rapid on / in the introduction of a possible collapse, violation of atrial or intraventricular conduction, asystole. With long-term use - oppression of bone marrow hematopoiesis (leukopenia, thrombocytopenia, neutropenia, agranulocytosis, hypoplastic anemia), hemolytic anemia with a positive breakdown of Coombs.

    Other: fever, allergic reactions (skin rash); with prolonged use - drug lupus erythematosus (in 30% of patients with a duration of therapy more than 6 months). Probable microbial infections, slowing healing processes and bleeding gums.

    Overdose:

    Symptoms: confusion, decreased urination, severe dizziness or fainting, rapid or irregular heartbeat, sinoatrial and atrioventricular blockade, asystole, decreased myocardial contractility, persistent lowering of blood pressure, pulmonary edema, convulsions, paroxysms of polymorphic ventricular tachycardia, nausea, or vomiting.

    Treatment: gastric lavage, induction of vomiting, hemodialysis, vasoconstrictors and maintenance of airway patency, sodium hydrogen carbonate can eliminate the expansion of the QRS complex or arterial hypotension.

    Interaction:

    Antihypertensive drugs - increased antihypertensive effect, especially with IV introduction.

    Anti-asthma means - decreased effectiveness.

    Anticholinergic, antihistamines, prokinetics - potentiation of cholinoblocking effects.

    Ofloxacin, levofloxacin, ciprofloxacin - increased plasma concentration of procainamide due to inhibition of its secretion by the kidneys.

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

    Sparfloxacin, gatifloxacin, moxifloxacin, pimozode - prolongation of the QT interval.

    Other antiarrhythmic drugs - increased cardiodepressive action.

    Means that inhibit neuromuscular transmission - lengthening and strengthening the action.

    The drugs that depress the bone marrow are aggravation of cytopenias.

    Means that extend the QT interval: amiodarone, amitriptyline, bepridil, disopyramid, erythromycin, haloperidol, imipramine, pimozide, sotalol, quinidine, thioridazine - Strengthening the antiarimic / toxic effect of procainamide.

    Trimethoprim, amiodarone - increased plasma concentration of procainamide.

    Special instructions:

    With iv introduction is better tolerated than quinidine, and with prolonged ingestion - worse.

    The routine use of procainamide to prevent sudden cardiac death increases the risk of death in high-risk patients.

    Antiarrhythmic therapy with procainamide for 24 ± 15 months does not affect the likelihood of fatal outcome (total, cardiovascular, sudden cardiac mortality) in elderly patients with heart disease and asymptomatic ventricular complex arrhythmia compared with patients without antiarrhythmic therapy.

    Procainamide IV is less quickly and less efficiently restores sinus rhythm in patients with acute atrial fibrillation after heart surgery compared with propafenone and with more pronounced arterial hypotension.

    Antiarrhythmic effect (30-month reception) of procainamide in patients with coronary atherosclerosis is accompanied by a decrease in the level of total cholesterol, triglycerides, apo-AII, apo-B.

    In elderly patients, hypotension is most likely.

    Impact on the ability to drive vehicles and manage mechanisms

    Care should be taken when driving vehicles or performing work that requires special attention.

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