Etmozine (Tablets) Instructions for Use

Marketing Authorization Holder

Onlinepharm, JSC (Latvia)

ATC Code

C01BG01 (Moracizine)

Active Substance

Moracizine (Rec.INN registered by WHO)

Dosage Form

Etmozine

Film-coated tablets, 100 mg: 10, 20, 30, 40, or 50 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.
10 pcs. – blister packs (5) – cardboard packs.

Clinical-Pharmacological Group

Antiarrhythmic drug. Class I C

Pharmacotherapeutic Group

Antiarrhythmic agent

Pharmacological Action

Antiarrhythmic agent. According to the Vaughan-Williams classification of antiarrhythmics, Moracizine belongs to drugs of classes IA, IB, and IC, but does not fully belong to any of them. It suppresses the fast, inward-directed transport of sodium ions through the membranes of cardiomyocytes. It has pronounced local anesthetic and membrane-stabilizing activity.

It reduces excitability, conduction velocity, and automaticity due to slowed conduction in the atrioventricular node and the His-Purkinje system. It reduces the action potential duration (APD) in Purkinje fibers, also reduces the effective refractory period (ERP), but to a lesser extent than the APD, thus the ERP/APD ratio increases.

It reduces the maximum rate of phase 0 depolarization (V_max), but does not affect the action potential amplitude or the maximum diastolic potential.

It does not affect the refractory periods of the atria, AV node, or left ventricle and has a minimal effect on ventricular repolarization. It does not affect conduction in the sinoatrial node or intra-atrial conduction and only slightly affects the sinus cycle length and sinoatrial node recovery time. It has a less pronounced effect on the slope of phase 0 and a stronger influence on APD and ERP than class IC drugs.

It causes a slight but persistent increase in blood pressure and heart rate at rest. It may suppress platelet aggregation and has anticholinergic activity.

Pharmacokinetics

After oral administration, it is completely absorbed, with C_max in plasma reached within 0.5-2 hours. Plasma protein binding is about 95%. It undergoes intensive first-pass metabolism in the liver. During metabolism, at least 26 metabolites are formed, only two of which may be pharmacologically active. Moracizine induces its own metabolism via the CYP system in the liver.

T_1/2 is 1.5-3.5 hours. It is excreted as metabolites in bile – 56%, by the kidneys – 39%; less than 1% is excreted unchanged. Some enterohepatic recirculation is noted.

Indications

Atrial and ventricular extrasystole, paroxysmal atrial tachycardia, paroxysmal ventricular tachycardia, paroxysmal atrial tachyarrhythmia; arrhythmias due to cardiac glycoside overdose.

ICD codes

Dosage Regimen

Initiate treatment in a hospital setting due to the risk of proarrhythmic effects, which are most likely during the first week of therapy.

The recommended daily dose for adults is 600 mg to 900 mg, administered orally in three divided doses.

For severe renal impairment, adjust the dosage regimen and implement careful monitoring of the patient’s clinical status.

Do not use in patients with severe hepatic insufficiency.

Exercise caution in patients under 18 years of age, as safety and efficacy have not been established in this population.

Maintain an interval of at least 14 days between discontinuation of MAO inhibitors and initiation of Etmozine therapy.

Adverse Reactions

From the cardiovascular system proarrhythmic effect (ventricular arrhythmias), atrial fibrillation, bradycardia, increased blood pressure, decreased blood pressure (especially with IV administration), chest pain, AV block, intraventricular block, development or worsening of heart failure (dyspnea, peripheral edema).

From the central and peripheral nervous system blurred vision, headache, dizziness, tremor, ataxia, tinnitus, dysarthria, nystagmus, hyperesthesia, paresthesia, nervousness, anxiety, sleep disorders, increased fatigue, weakness, hallucinations, amnesia.

From the digestive system diarrhea, dry mouth, nausea, vomiting, gastralgia; rarely – increased activity of liver transaminases, hepatotoxicity.

Local reactions with IM administration – pain at the injection site.

Other allergic reactions, myalgia; rarely – fever.

Contraindications

Hypersensitivity to moracizine; second-degree sinoatrial block, second and third-degree AV block (without a pacemaker), right bundle branch block combined with block of one of the branches of the left bundle branch, intraventricular conduction block, chronic heart failure stage II-III, severe arterial hypotension, cardiogenic shock, severe renal/hepatic insufficiency; pregnancy, lactation (breastfeeding).

Use in Pregnancy and Lactation

Adequate and strictly controlled studies on the safety of moracizine use during pregnancy have not been conducted.

Contraindicated for use during pregnancy.

There are reports that Moracizine may be excreted in breast milk, so if use during lactation is necessary, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

Contraindicated for use in severe hepatic insufficiency.

Use in Renal Impairment

Contraindicated for use in severe renal insufficiency. When used in patients with severe renal impairment, dosage regimen adjustment and careful monitoring are required.

Pediatric Use

Should be used with caution in patients under 18 years of age (efficacy and safety have not been studied).

Special Precautions

Should be used with caution in cardiogenic shock, myocardial infarction (subacute period), post-infarction cardiosclerosis, coronary cardiosclerosis, sick sinus syndrome (sinus node recovery time increases, sinus bradycardia, temporary cessation of activity or complete block of the sinus node are possible), first-degree AV block, bradycardia, arterial hypotension, electrolyte imbalance – hypokalemia, hyperkalemia, hypomagnesemia (the nature of moracizine’s action may change), during cardiac pacing (increased risk of arrhythmia development), in hepatic and/or renal insufficiency, cardiomegaly, severe myocardial hypertrophy, in patients under 18 years of age (efficacy and safety have not been studied).

In severe renal impairment, dosage regimen adjustment and careful monitoring are required.

Use with caution in patients with a pacemaker, as the risk of moracizine-induced arrhythmias may increase. Treatment is recommended to be initiated in a hospital due to the risk of arrhythmogenic action associated with the use of moracizine. The development of arrhythmogenic action does not depend on the dose and is most likely during the first week of treatment.

The interval after taking MAO inhibitors and before starting moracizine should be at least 14 days.

Influence on the ability to drive vehicles and operate machinery

Caution is required when driving vehicles or performing other work requiring increased attention during the period of use due to possible dizziness.

Drug Interactions

With simultaneous use with antiarrhythmic agents, the risk of developing arrhythmogenic action increases; with MAO inhibitors – the risk of developing arrhythmogenic action increases significantly.

A case of bleeding development has been described with simultaneous use with warfarin.

It is believed that with simultaneous use with digoxin, a significant increase in the QT interval is possible, which can lead to AV block.

With simultaneous use with cimetidine, the plasma concentration of moracizine increases; with theophylline – the plasma concentration of theophylline increases.

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.