Etacizin tablets p / o 50mg, No. 50

• supraventricular and ventricular premature beats;

• paroxysms of atrial fibrillation and atrial flutter;

• ventricular and supraventricular tachycardia (including with WPW syndrome).

Indications for use are limited by the presence of severe organic heart damage.

The drug should be taken orally, regardless of food intake, 50 mg 2-3 times / day.

With insufficient clinical effect, the dose is increased (under mandatory ECG control) to 50 mg 4 times / day (200 mg) or 100 mg 3 times / day (300 mg).

Upon reaching a persistent antiarrhythmic effect, maintenance therapy is carried out in individually selected minimum effective doses.

Active ingredient: etacizin (diethylaminopropionylethoxycarbonylaminophenothiazine hydrochloride) - 50 mg

Excipients : potato starch - 9.57 mg, sucrose - 19.3 mg, methylcellulose - 0.33 mg, calcium stearate - 0.8 mg.

Shell composition: sucrose - 37.695 mg, povidone K25 - 0.753 mg, quinoline yellow dye (E104) - 0.025 mg, sunset yellow dye (E110) - 0.003 mg, calcium carbonate - 6.308 mg, magnesium hydroxycarbonate - 3.678 mg, titanium dioxide ( E171) - 0.665 mg, silicon dioxide - 0.827 mg, carnauba wax - 0.046 mg.

• severe conduction disturbances (including sinoatrial blockade, AV block II and III degrees in the absence of an artificial pacemaker), impaired intraventricular conduction;

• heart rhythm disturbances in combination with blockages of conduction along the His system - Purkinje fibers;

• severe hypertrophy of the left ventricular myocardium;

• the presence of postinfarction cardiosclerosis;

• cardiogenic shock;

• severe arterial hypotension;

• chronic heart failure II and III FC according to NYHA classification;

• severe violations of the liver and / or kidneys;

• simultaneous administration of MAO inhibitors;

• concomitant use with class IC antiarrhythmics (propafenone, allapinin) and class IA (quinidine, procainamide, disopyramide, aymalin);

• age up to 18 years (efficacy and safety have not been established);

• pregnancy;

• lactation period (breastfeeding);

• hypersensitivity to the components of the drug.

The drug is used with extreme caution in SSS, bradycardia, AV blockade of the 1st degree, coronary artery disease, severe peripheral circulatory disorders, chronic heart failure FC I, angle-closure glaucoma, benign prostatic hyperplasia, cardiomegaly (the risk of arrhythmogenic action increases), renal failure, hepatic insufficiency, electrolyte imbalance (hypokalemia, hyperkalemia, hypomagnesemia).

Clinical and pharmacological group: Antiarrhythmic drug. IC class

Pharmaco-therapeutic group: Antiarrhythmic agent

pharmachologic effect

It has a long-term antiarrhythmic effect. Oppresses the rate of rise of the action potential front (Vmax), does not change the rest potential.

Depending on the dose, it can reduce the duration of the action potential. Does not significantly change the effective refractory periods of the ventricles and atria. Inhibits fast incoming sodium current and, to a lesser extent, slow incoming calcium current.

EtacizinЃ slows down the conduction of excitation along the myocardial conduction system. On the ECG, an extension of the PR interval and the QRS complex appears; the ST interval, reflecting the repolarization of the ventricles, does not change or tends to be shortened.

EtacizinЃ increases the myocardial fibrillation threshold. Unlike many antiarrhythmic drugs, EtacizinЃ does not cause a significant decrease in heart rate or prolongation of the QT interval on the ECG.

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

Pharmacokinetics

Suction

When taken orally, the drug is rapidly absorbed from the gastrointestinal tract and is determined in the blood after 30-60 minutes. Cmax in blood plasma is achieved after 2.5-3 hours. Bioavailability is 40%.

Distribution

Plasma protein binding is about 90%. Etacizin crosses the placental barrier. Excreted in breast milk.

Metabolism

It is extensively metabolized during the 'first pass' through the liver. Some of the resulting metabolites have antiarrhythmic activity.

Withdrawal

The active substance is excreted from the body in the urine in the form of metabolites. T1 / 2 is 2.5 hours.

Pharmacokinetics in special clinical situations

The pharmacokinetic parameters of etacizin are subject to significant individual fluctuations and require individual study in individual patients to determine the optimal concentration of the drug in the blood plasma.

Indications of the drug EtacizinЃ

• supraventricular and ventricular premature beats;

• paroxysms of atrial fibrillation and atrial flutter;

• ventricular and supraventricular tachycardia (including with WPW syndrome).

Indications for use are limited by the presence of severe organic heart damage.

Dosage regimen

The drug should be taken orally, regardless of food intake, 50 mg 2-3 times / day.

With insufficient clinical effect, the dose is increased (under mandatory ECG control) to 50 mg 4 times / day (200 mg) or 100 mg 3 times / day (300 mg).

Upon reaching a persistent antiarrhythmic effect, maintenance therapy is carried out in individually selected minimum effective doses.

Side effect

From the side of the cardiovascular system: stopping the sinus node, AV block, impaired intraventricular conduction, decreased myocardial contractility, decreased coronary blood flow, arrhythmia, ECG changes (lengthening of the PQ interval, expansion of the P wave and QRS complex). Arrhythmogenic effect, the likelihood of which is greatest after a myocardial infarction and in other types of cardiac pathology, leading to a decrease in the contractility of the heart muscle and the development of heart failure.

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

From the digestive system: nausea.

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

Side effects depend on the size of the dose and, in order to avoid them, the maximum doses of the drug should not be prescribed.

Contraindications for use

• severe conduction disturbances (including sinoatrial blockade, AV block II and III degrees in the absence of an artificial pacemaker), impaired intraventricular conduction;

• heart rhythm disturbances in combination with blockages of conduction along the His system - Purkinje fibers;

• severe hypertrophy of the left ventricular myocardium;

• the presence of postinfarction cardiosclerosis;

• cardiogenic shock;

• severe arterial hypotension;

• chronic heart failure II and III FC according to NYHA classification;

• severe violations of the liver and / or kidneys;

• simultaneous administration of MAO inhibitors;

• concomitant use with class IC antiarrhythmics (propafenone, allapinin) and class IA (quinidine, procainamide, disopyramide, aymalin);

• age up to 18 years (efficacy and safety have not been established);

• pregnancy;

• lactation period (breastfeeding);

• hypersensitivity to the components of the drug.

The drug is used with extreme caution in SSS, bradycardia, AV blockade of the 1st degree, coronary artery disease, severe peripheral circulatory disorders, chronic heart failure FC I, angle-closure glaucoma, benign prostatic hyperplasia, cardiomegaly (the risk of arrhythmogenic action increases), renal failure, hepatic insufficiency, electrolyte imbalance (hypokalemia, hyperkalemia, hypomagnesemia).

Application during pregnancy and lactation

The use of the drug during pregnancy and lactation (breastfeeding) is contraindicated.

Etacizin crosses the placental barrier. Excreted in breast milk.

Application for violations of liver function

The use of the drug is contraindicated for severe liver dysfunctions.

With caution in liver failure.

Application for impaired renal function

The use of the drug is contraindicated in case of severe renal impairment.

With caution in renal failure.

Application in children

Contraindicated in children and adolescents under 18 years of age.

special instructions

As well as other antiarrhythmic drugs, EtacizinЃ can act arrhythmogenic. Therefore, when prescribing the drug, you should:

• strictly take into account the contraindications to the use of the drug;

• to identify and eliminate hypokalemia in advance;

• avoid the use of EtacizinЃ in combination with class IA and class IC antiarrhythmic drugs;

• it is preferable to start the course treatment in a hospital (especially in the first 3-5 days of taking the drug, taking into account the dynamics of the ECG after the trial and repeated doses of EtatsizinЃ or ECG monitoring data);

• stop treatment with an increase in ectopic ventricular complexes, the appearance of blockages or bradycardia;

• stop treatment when 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 seconds.

Risk factors for the arrhythmogenic effect of EtatsizinЃ: organic heart damage (especially suffered myocardial infarction), decreased left ventricular ejection fraction, maximum doses of the drug. In addition, caution should be exercised in patients with liver disease.

Alcohol should not be consumed during treatment with etacizine.

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

Influence on the ability to drive vehicles and mechanisms

Due to the risk of dizziness, it is not recommended to drive vehicles or operate complex mechanisms that require increased attention, the ability to concentrate.

Overdose

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

Treatment: symptomatic therapy is performed. Class IA and IC antiarrhythmic drugs should not be used to treat ventricular tachycardia. Sodium bicarbonate is able to eliminate the expansion of the QRS complex, bradycardia and arterial hypotension.

Drug interactions

The use of EtacizinЃ with other class IC antiarrhythmic drugs (propafenone, allapinin) and class IA (quinidine, procainamide, disopyramide, aymalin) is contraindicated.

EtacizinЃ should not be administered concurrently with MAO inhibitors.

The combination of beta-blockers with etacizin enhances the antiarrhythmic effect, especially in relation to arrhythmias provoked by exercise or stress.

Storage conditions

The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25 ? C.

Shelf life

Shelf life is 3 years.

Terms of sale

The drug is available with a prescription.

Contacts for inquiries

OLINEFARM RUS LLC (Russia)