Procainamide-Eskom (Solution) Instructions for Use

Marketing Authorization Holder

Mir Chemical and Pharmaceutical Concern, LLC (Russia)

ATC Code

C01BA02 (Procainamide)

Active Substance

Procainamide (Rec.INN registered by WHO)

Dosage Form

Procainamide-Eskom

Solution for intravenous and intramuscular injection 500 mg/5 ml: amp. 5, 10 or 20 pcs.

Dosage Form, Packaging, and Composition

5 ml – ampoules (5) – plastic contour packs (1) – cardboard boxes.
5 ml – ampoules (5) – plastic contour packs (2) – cardboard boxes.
5 ml – ampoules (10) – plastic contour packs (1) – cardboard boxes.
5 ml – ampoules (10) – plastic contour packs (2) – cardboard boxes.

Clinical-Pharmacological Group

Antiarrhythmic drug. Class I A

Pharmacotherapeutic Group

Antiarrhythmic agent

Pharmacological Action

An antiarrhythmic agent of class IA, it has membrane-stabilizing activity. It inhibits the incoming fast sodium ion current and reduces the depolarization rate in phase 0. It suppresses conduction and slows repolarization. It reduces the excitability of the atrial and ventricular myocardium. It increases the duration of the effective refractory period of the action potential (to a greater extent in the affected myocardium). The slowing of conduction, which is observed regardless of the resting potential magnitude, is more pronounced in the atria and ventricles and less so in the AV node.

The indirect m-cholinoblocking effect, compared to quinidine and disopyramide, is less pronounced, so paradoxical improvement of AV conduction is usually not observed. It affects phase 4 of depolarization, reduces the automaticity of the intact and affected myocardium, and suppresses the function of the sinus node and ectopic pacemakers in some patients.

The active metabolite, N-acetylprocainamide, has pronounced activity of class III antiarrhythmic agents and prolongs the action potential duration. It has a weak negative inotropic effect (without significant effect on cardiac output), vagolytic and vasodilating properties, which causes tachycardia and a decrease in blood pressure and systemic vascular resistance.

The electrophysiological effects are manifested in the widening of the QRS complex and prolongation of the PQ and QT intervals. The time to reach the maximum effect when taken orally is 60-90 minutes, with intravenous administration – immediately, with intramuscular administration – 15-60 minutes.

Pharmacokinetics

Absorption is rapid after oral and intramuscular administration. Protein binding is 15-20%. It is metabolized in the liver to form the active metabolite N-acetylprocainamide. Usually, about 25% of the administered procainamide is converted into this metabolite; however, with rapid acetylation or impaired renal function, up to 40% of the dose is converted.

The T_1/2 of procainamide is 2.5-4.5 hours, and in case of impaired renal function – 11-20 hours; that of N-acetylprocainamide is about 6 hours. It is excreted by the kidneys, 50-60% unchanged, the rest as the metabolite. In case of impaired renal function or chronic heart failure, the metabolite rapidly accumulates in the blood to toxic concentrations, while the concentration of procainamide remains within acceptable limits.

Indications

Ventricular arrhythmias: extrasystole, paroxysmal ventricular tachycardia. Supraventricular arrhythmias. Paroxysm of atrial fibrillation or atrial flutter. Supraventricular tachycardia (including WPW syndrome).

ICD codes

Dosage Regimen

Individual. When taken orally, the initial dose is from 250 mg to 1 g, then, if necessary and taking into account tolerance, 250-500 mg every 3-6 hours.

With intramuscular injection – 50 mg/kg/day in divided doses every 3-6 hours.

With intravenous bolus injection, a single dose is 100 mg; if necessary, repeated administrations are possible until the arrhythmia stops. With intravenous infusion, the dose is 500-600 mg.

Maximum doses for adults when taken orally – 4 g/day; with intravenous bolus injection with repeated administrations, the total dose is 1 g.

Adverse Reactions

From the cardiovascular system: arterial hypotension (up to the development of collapse), intraventricular blocks, ventricular tachycardia, tachyarrhythmia; with rapid intravenous administration – collapse, intraventricular block, asystole.

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

From the hematopoietic system: with long-term use – inhibition of bone marrow hematopoiesis (leukopenia, thrombocytopenia, neutropenia, agranulocytosis, hypoplastic anemia), hemolytic anemia with a positive Coombs test.

Allergic reactions: skin rash, itching.

Other: bitterness in the mouth, with long-term use – drug-induced lupus erythematosus (in 30% of patients with therapy duration of more than 6 months); microbial infections, slowing of healing processes, and bleeding gums are possible due to the risk of leukopenia and thrombocytopenia.

Contraindications

AV block of II and III degree (except in cases with a pacemaker), ventricular flutter or fibrillation, arrhythmias due to cardiac glycoside intoxication, leukopenia, hypersensitivity to procainamide.

Use in Pregnancy and Lactation

If it is necessary to use procainamide during pregnancy and lactation (breastfeeding), it should be taken into account that the active substance crosses the placental barrier and is excreted in breast milk.

Therefore, the use of procainamide is possible only if the potential benefit to the mother outweighs the possible risk to the fetus or infant.

Use in Hepatic Impairment

Use with caution in hepatic insufficiency.

Use in Renal Impairment

Use with caution in renal insufficiency.

Geriatric Use

Use with caution in elderly patients.

Special Precautions

The arrhythmogenic effect of procainamide was noted in 5-9% of cases. Due to the possible suppression of myocardial contractility and decrease in blood pressure, it should be used with great caution in myocardial infarction. In severe atherosclerosis, Procainamide is not recommended.

Use with caution in bundle branch block, arrhythmia due to cardiac glycoside intoxication, myasthenia gravis, hepatic and/or renal insufficiency, SLE (including history), bronchial asthma, chronic heart failure in the stage of decompensation, ventricular tachycardia with coronary artery occlusion, surgical interventions (including in surgical dentistry), with prolonged QT interval, arterial hypotension, atherosclerosis, in myasthenia gravis, in elderly patients.

Drug Interactions

With simultaneous use with antiarrhythmic agents, an additive cardiodepressant effect is possible; with antihypertensive agents – the antihypertensive effect is enhanced; with anticholinesterase agents – the effectiveness of anticholinesterase agents is reduced.

With simultaneous use with m-cholinoblockers, antihistamines, their anticholinergic effect is enhanced.

With simultaneous use, the effect of agents blocking neuromuscular transmission is enhanced; with simultaneous use of agents causing inhibition of bone marrow hematopoiesis, leukopenia and thrombocytopenia may be enhanced.

With simultaneous use with amiodarone, the QT interval increases due to an additive effect on its duration and the risk of developing torsades de pointes ventricular arrhythmia. The plasma concentration of procainamide and its metabolite N-acetylprocainamide increases, and side effects may be enhanced.

With simultaneous use with captopril, the risk of developing leukopenia may increase.

With simultaneous use with ofloxacin, an increase in the plasma concentration of procainamide is possible; with prenylamine – the negative inotropic effect and the risk of developing torsades de pointes ventricular arrhythmia are enhanced.

With simultaneous use with sotalol, quinidine, an additive increase in the QT interval is possible.

With simultaneous use with trimethoprim, the plasma concentration of procainamide and its active metabolite N-acetylprocainamide increases, and there is a risk of developing toxic reactions.

With simultaneous use with cisapride, the duration of the QT interval significantly increases due to an additive effect, and there is a risk of developing ventricular arrhythmia (including torsades de pointes).

With simultaneous use with cimetidine, the plasma concentration of procainamide and the risk of increased side effects increase, especially in elderly patients and in cases of impaired renal function, which is due to a reduction in the renal excretion of procainamide by almost 1/3 or more under the influence of cimetidine.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.