Ethacizine, pills 50mg, 50pcs

Composition

Active ingredient:

Ethacizinee (diethylaminopropionylethoxycarbonylaminophenothiazine hydrochloride) 50 mg,

Auxiliary substances:

potato starch-9.57 mg;

sucrose-19.3 mg;

methylcellulose-0.33 mg;

calcium stearate-0.8 mg,

Shell:

sucrose — 37,695 mg; povidone — 0,753 mg; dye quinoline yellow (E 104) — 0.025 mg; dye “sunset” yellow (E 110) — 0,003 mg; calcium carbonate 6,308 mg; magnesium hydroxycarbonate main — 3,678 mg; titanium dioxide (E 171) — 0,665 mg; silicon dioxide — 0,827 mg; Carnauba wax — 0,046 mg

Pharmacological action

Ethacizine is an antiarrhythmic agent of the IC class, has a long-lasting antiarrhythmic effect. Inhibits the rate of rise of the front of the action potential (V_max), does not change the resting potential. Depending on the dose, it can reduce the duration of the action potential. It does not significantly alter the effective refractory periods of the ventricles and atria. Inhibits fast incoming sodium current and, to a lesser extent, slow incoming calcium current.

Ethacizinee slows down the conduction of excitation through the myocardial conduction system. The ECG shows an elongation of the PR interval and the QRS complex; the ST interval, reflecting ventricular repolarization, does not change or tends to shorten.

Ethacizinee increases the threshold of myocardial fibrillation. Unlike many antiarrhythmic drugs, Ethacizinee does not significantly reduce the heart rate or prolong the duration of the QT interval on the ECG.

The antiarrhythmic effect when taken orally usually develops on the 1st-2nd day, the duration of treatment depends on the form of arrhythmia, the effectiveness and tolerability of the drug.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract and is detected in the blood after 30-60 minutes. _Cmax in blood plasma is reached in 2.5-3 hours. Bioavailability — 40%.90% binds to plasma proteins. T_1/2 is 2.5 hours.

The pharmacokinetic parameters of Ethacizinee are subject to significant individual fluctuations and require individual study in individual patients to determine the optimal concentration of the drug in blood plasma. It is intensively metabolized during the” first pass ” through the liver. Some of the resulting metabolites have antiarrhythmic activity. Ethacizinee is excreted by the kidneys as metabolites. Ethacizine penetrates the placental barrier. It is excreted in breast milk.

Indications

• supraventricular and ventricular extrasystole;
• paroxysms of atrial fibrillation and flutter;
• ventricular and supraventricular tachycardia, including in Wolf-Parkinson-White syndrome (WPW).
• Indications for use are limited to the presence of severe organic heart damage.

Contraindications

• individual hypersensitivity to Ethacizine or auxiliary substances;
• severe conduction disorders (including sinoatrial block, AV blockade II and III degree in the absence of an artificial pacemaker), impaired intraventricular conduction;
• pronounced hypertrophy of the myocardium of the left ventricle;
• presence of postinfarction cardiosclerosis;
• cardiogenic shock;
• severe hypotension;
• chronic heart failure II and III functional class (FC);
• functional disorders of the liver and/or kidney disease;
• pregnancy;
• lactation;
• children’s age (under 18) – efficacy and safety have not been established;
• simultaneous use of MAO inhibitors;
• simultaneous use with IC-class antiarrhythmic agents (moracizine, propafenone, allapinine) and IA-class antiarrhythmics (quinidine, procainamide, disopyramide, aimalin);
• any form of cardiac arrhythmia in combination with Gis-Purkinje blockades.

With extreme caution: for sinus node weakness syndrome, bradycardia, grade I AV block, IHD, severe peripheral circulatory disorders, FC I chronic heart failure, angle-closure glaucoma, BPH, cardiomegaly (increased risk of arrhythmogenic effects), electrolyte imbalance (hypokalemia, hyperkalemia, hypomagnesemia), liver/kidney failure.

Side effects

From the cardiovascular system: sinus node arrest, AV block, violation of intraventricular conduction, decreased myocardial contractility, decreased coronary blood flow, arrhythmia (arrhythmogenic effect is most likely after a previous myocardial infarction and in other types of cardiac pathology, leading to a decrease in contractility of the heart muscle and the development of heart failure).

ECG changes: lengthening of the PQ interval, expansion of the P wave and QRS complex.

From the central nervous system: dizziness, headache, staggering when walking or turning the head, slight drowsiness; in some cases-diplopia, paresis of accommodation.

From the gastrointestinal tract: nausea.

It is possible to reduce the side effects or their disappearance after using the drug for 3-4 days. With long-term treatment with Ethacizine, they do not increase, and with discontinuation of the drug, they quickly disappear.

Side effects depend on the size of the dose and, to avoid them, do not prescribe the maximum dose of the drug.

Interaction

Contraindicated use with other antiarrhythmic agents IC (moracizine, allapinine, propafenone) and IA (quinidine, procainamide, disopyramide, aimalin) class.

Ethacizinee should not be administered concomitantly with MAO inhibitors.

The combination of beta-blockers with Ethacizinee may enhance the antiarrhythmic effect, especially in relation to arrhythmias provoked by physical exertion or stress.

How to take, course of use and dosage

Inside, regardless of food intake. The initial dose is 50 mg (1 tablet) 2-3 times a day. In case of insufficient clinical effect, the dose is increased (under mandatory ECG monitoring) to 50 mg 4 times a day (200 mg) or 100 mg 3 times a day (300 mg).

When a persistent antiarrhythmic effect is achieved, maintenance therapy is performed in individually selected minimum effective doses.

Overdose

Ethacizinee has a small therapeutic breadth, so severe intoxication can easily occur (especially with the simultaneous use of other antiarrhythmic agents).

Symptoms: prolongation of PR intervals and expansion of the QRS complex, increased T wave amplitude, bradycardia, sinoatrial and AV block, asystole, paroxysms of polymorphic and monomorphic ventricular tachycardia, decreased myocardial contractility, persistent decrease in blood pressure, dizziness, blurred vision, headache, gastrointestinal disorders.

Treatment: symptomatic; Class IA and IC antiarrhythmics should not be used to treat ventricular tachycardia; sodium bicarbonate can eliminate QRS complex expansion, bradycardia, and hypotension.

Special instructions

Just like other antiarrhythmic drugs, Ethacizinee can act arrhythmically. Therefore, when prescribing Ethacizinee, you should:

• strictly taken into account contraindications to the use of the drug;
• proactively identify and correct hypokalemia;
• avoid use in combination with antiarrhythmic means IA and IC classes;
• course of treatment is preferable to start in the hospital (especially in the first 3-5 days of taking the drug, taking into account the dynamics of the ECG after initial and repeated doses Ethacizine or data monitoring EKG)
• to immediately stop treatment with frequent ventricular ectopic complexes, the appearance of blockades or bradycardia. Treatment with Ethacizinee should also be stopped immediately if the ventricular complexes expand by more than 25%, their amplitude decreases, the duration of the P wave on the ECG is more than 0.12 s

. Risk factors for the arrhythmogenic effect of Ethacizinee are considered: organic heart damage (especially a previous myocardial infarction), a decrease in the left ventricular ejection fraction, maximum doses of the drug. In addition, caution should be exercised in patients with liver disease. When treating with Ethacizine, alcohol should not be consumed.

During therapy, it is necessary to regularly monitor the patient’s condition and cardiovascular function (ECG, blood pressure, echocardiography).

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions. Due to the risk of developing dizziness during treatment, it is not recommended to drive vehicles or maintain complex mechanisms that require increased attention and concentration.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30 °C.

Shelf

life is 3 years.

Active ingredient

Diethylaminopropionylethoxycarbonylaminophenothiazine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia