Etatsizin (Ethacyzin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDiethylaminopropionylethoxycarbonylaminophenothiazineDiethylaminopropionylethoxycarbonylaminophenothiazine
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  • Etatsizin
    pills inwards 
    Olainfarm, AO     Latvia
    • Dosage form: & nbspCoated tablets
    Composition:
    One coated tablet contains:
    Active substance:
    ethacycin 50 mg;
    Excipients:
    potato starch, sugar, methylcellulose, calcium stearate, polyvinylpyrrolidone, quinoline yellow dye (E 104), solar yellow dye FCF (E11O), calcium carbonate, magnesium carbonate, titanium dioxide, silicon dioxide, beeswax.
    Description:The tablets covered with a cover, yellow color. The form of the tablet is round. Two layers are visible on the cross-section.
    Pharmacotherapeutic group:Antiarrhythmic agent.
    ATX: & nbsp

    C.01.B.C   Antiarrhythmic drugs Ic class

    Pharmacodynamics:
    Antiarrhythmic agent (AAP) class 1C, has a long antiarrhythmic effect. Oppresses the rate of growth of the action potential front (Minds), does not change the quiescent potential. Depending on the dose, it can reduce the duration of the action potential; does not significantly alter the effective refractory periods of the ventricles and atria. Inhibits the rapid incoming sodium current and, to a lesser extent, the slow incoming calcium current.
    Etatsizin slows down the excitation of the conduction system of the myocardium. On the ECG appears an extension of the PR interval and the QRS complex; the ST interval, reflecting the repolarization of the ventricles, tends to be shortened.
    Etatsizin has a moderate anti-ischemic effect. The arrhythmogenic effect with the use of therapeutic doses develops rarely.
    In comparison with etmosin, etatsizin is characterized by a more pronounced inhibitory effect on the fast incoming current of sodium ions into the myocardial cell and a slow incoming calcium current, which leads to suppression of spontaneous diastolic depolarization of ectopic foci of automatism to a higher degree than with the use of etmosin. On the main models of arrhythmias etatsizin exceeds ethmosin 2-3 times in intensity and 4-5 times in duration of effect. Etatsizin raises the threshold of myocardial fibrillation, as well as suppresses cardiac rhythm disturbances, which turn into fibrillation in conditions of acute myocardial ischemia.
    Unlike many antiarrhythmic drugs (propranolol, quinidine, novocainamide, amiodarone, rhythmylene) etatsizin does not cause a significant decrease in the heart rate or prolong the duration of the QT interval on the ECG. Etatsizin penetrates the placental barrier. Excreted in breast milk.Antiarrhythmic effect with ingestion usually develops on 1-2 days, the duration of treatment depends on the form of arrhythmia, efficacy and tolerability of the drug.
    Pharmacokinetics:When ingested quickly absorbed from the gastrointestinal tract and is determined in the blood after 30-60 minutes. The maximum concentration in the blood plasma is achieved after 2.5-3 hours. Bioavailability - 40%. 90% binds to blood plasma proteins. Half-life is 2.5 hours. Parameters of the pharmacokinetics of ethacyzin 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. Intensively metabolized when the "first pass" through the liver. Some of the metabolites that are formed have antiarrhythmic activity. From the body, etatsizin is excreted in the urine in the form of metabolites.
    Indications:Nadzheludochkovaya and ventricular extrasystole, paroxysms of flicker and atrial flutter, paroxysmal supraventricular tachycardia, including in the case of Wolff-Parkinson-White syndrome (WPW), paroxysmal ventricular tachycardia (in the absence of organic heart lesions).
    Contraindications:
    Increased individual sensitivity to etatsizina or excipients; pronounced conduction disorders (including sinoatrial block, atrioventricular (AV) block II and III degree in the absence of an artificial pacemaker, violation of intraventricular conduction); severe left ventricular myocardial hypertrophy, presence of postinfarction cardiosclerosis, cardiogenic shock, severe arterial hypotension; chronic heart failure of stage II and III; expressed violations of the liver and / or kidney function, pregnancy, lactation, simultaneous administration of MAO inhibitors. The appointment of ethazicin to patients with ventricular arrhythmias in combination with blockages of the Purkinje system is not contraindicated.
    Carefully:With extreme caution, with sinus node weakness, bradycardia, atrioventricular (AV) blockade of the first degree, coronary heart disease, severe peripheral circulation disorders, heart failure (compensated), closed-angle glaucoma, benign prostatic hypertrophy, cardiomegaly.increased risk of arrhythmogenic action, electrolyte imbalance (hypokalemia, hyperkalemia, hypomagnesemia), in patients with pacemaker (risk of arrhythmia), hepatic / renal failure, age - up to 18 years (efficacy and safety not established).
    Pregnancy and lactation:The use of the drug during pregnancy and lactation is contraindicated.
    Dosing and Administration:Inside, regardless of food intake, starting with 50 mg 3 times a day. In case of insufficient clinical effect, the dose is increased (under compulsory ECG monitoring) to 50 mg 4 times a day (200 mg) or 100 mg 3 times daily (300 mg). When a persistent antiarrhythmic effect is achieved, maintenance therapy is carried out in individually selected minimally effective doses.
    Side effects:
    From the cardiovascular system:
    AV blockade, violation of intraventricular conduction, decreased myocardial contractility, decreased coronary blood flow, arrhythmia. In rare cases, arrhythmogenic action develops.
    From the side of the central nervous system:
    dizziness, paresis of accommodation.
    From the gastrointestinal tract:
    nausea.
    In clinical trials, side effects after etatsizina application were recorded on average in 44% of patients, in half they were of the same type and felt subjectively: headache, dizziness, staggering when walking or turning the head, general weakness, slight drowsiness; in some cases diplopia was noted. In most patients, the side effect was manifested with its initial dose of 100-150 mg / day. Side effects were usually observed early: on the 2nd, even on the 3rd day of treatment. With long-term treatment with etatsizinom they did not increase, and with the discontinuation of the drug quickly disappeared. Other side effects of etatsizina are associated with inhibition of myocardial conductivity (28.6%).
    ECG changes:
    elongation of the PQ interval, expansion of the P wave and the QRS complex.
    Overdose:
    Symptoms, increased oppressive effect on the conductive system of the myocardium, increased risk of arrhythmogenic action.
    Treatment: gastric lavage, symptomatic therapy.
    Patients with electromechanical dissociation arising from side effects of etatsizina (or its relative overdose) should undergo urgent and prolonged resuscitation (external cardiac massage, administration of adrenomimetic drugs, calcium salts, dopamine, rheopolyglucin),treatment of ventricular tachycardia caused by etatsizin - electropulse therapy (EIT) or intravenous administration of lidocaine or trimecaine, against which the effectiveness of EIT may increase. Contraindicated for the termination of ventricular tachycardia caused by etatsizin, the use of AAP class 1A class (novokainamid, rhythmelen, aymalin, etmozin, etc.). Hemodialysis is ineffective.
    Interaction:
    The use of AAP class 1C (etmosin, enkainide, flecainide, dorkimide, propafenone) is contraindicated in combination with AAP class 1A.
    Etatsizin should not be administered simultaneously with MAO inhibitors.
    The combination of 3-adrenoblockers with AAC class 1C enhances the antiarrhythmic effect, especially in relation to arrhythmias induced by physical exertion or stress.This combination allows the use of small doses of AAP, which reduces the incidence of side effects.This combination is indicated for the treatment and prevention of paroxysmal tachycardia , including ventricular.
    With the combined use of etatsizina and digoxin, the antiarrhythmic effect of the drugs increases and the contractility of the myocardium improves.With their combined use, nausea and a decrease in appetite are possible, which is associated with an increase in the concentration of digoxin in the blood. In these cases, a decrease in the dose of digoxin is required.
    The use of glutamic acid in combination with etatsizin neutralizes the cardiodepressant effect of etatsizina in patients with initial signs of circulatory disorders.
    Special instructions:
    Patients with sinus node weakness syndrome, especially if the drug is prescribed for the first time, ECG monitoring (QRS complex) is mandatory 2-3 days after the administration of etatsizina.
    It is often clinically expedient to start treating arrhythmia by first prescribing etmosin (600-1200 mg / day), a drug that is much less likely to produce side effects, and only after the arrhythmia refractoriness has been established for this drug, is it to switch to the use of more active etatsizina. The appointment of ethazicin to patients with ventricular arrhythmias in combination with blockages of the Purkinje system is not contraindicated.
    As well as other antiarrhythmic drugs, etatsizin can act arrhythmogenically. Therefore, when etatsizina is prescribed:
    1) strictly take into account contraindications to the use of the drug;
    2) in advance to reveal and eliminate hypokalemia;
    3) avoid the use of etatsizina in combination with APP class 1A;
    4) course treatment preferably begin in the hospital (especially in the first 3-5 days of taking the drug, taking into account the dynamics of the ECG after trial and repeated doses of etatsizina or ECG monitoring data);
    5) immediately stop treatment with increased ectopic ventricular complexes, the appearance of blockades or bradycardia. Treatment with etatsizin should also immediately stop with the expansion of ventricular complexes by more than 25%, a decrease in their amplitude, the duration of the P wave on the ECG is more than 0.12 seconds.
    Risk factors for arrhythmogenic effects of ethazine are considered to be: organic heart disease (in particular, myocardial infarction suffered), reduction of ejection fraction, persistent ventricular tachycardia, maximum doses of the drug. In addition, caution should be exercised in patients with liver disease. When treating etatsizinom you should not drink alcohol. During therapy, it is necessary to carefully monitor the patient's condition and the function of the cardiovascular system (ECG, AD, ECHOCH).
    Effect on the ability to drive transp. cf. and fur:It is not recommended to drive vehicles or service complex mechanisms that require increased attention, ability to concentrate.
    Form release / dosage:
    The tablets covered with a cover, on 50 mg.
    Packaging:
    For 10 tablets in a contour mesh box made of PVC film and aluminum foil printed lacquered.
    5 contour packs together with instructions for use are placed in a pack of cardboard.
    Storage conditions:List B.
    In a dry place, protected from light, out of reach of children, at a temperature not exceeding 30 ° C.
    Shelf life:3 years.
    Do not use after the date shown on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N015386 / 01
    Date of registration:07.10.2008
    The owner of the registration certificate:Olainfarm, AOOlainfarm, AO Latvia
    Manufacturer: & nbsp
    Information update date: & nbsp10.01.2016
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