Etatsizin

General characteristics. Structure:

Active agent: диэтиламинопропионилэтоксикарбонил-аминофенотиазина hydrochloride of 50 mg

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

Structure of a cover: sucrose - 37.695 mg, povidone - 0.753 mg, dye quinolinic yellow (E104) - 0.025 mg, dye a sunset yellow (E110) - 0.003 mg, calcium a carbonate - 6.308 mg, magnesium a hydroxycarbonate the main - 3.678 mg, titanium dioxide (E171) - 0.665 mg, silicon dioxide - 0.827 mg, wax of karnaubskiya - 0.046 mg.

Pharmacological properties:

Antiarrhytmic drug of a class I C. Possesses long antiarrhytmic action. Speed of increase of the front of the action potential (Vmax) oppresses, does not change rest potential.
Depending on a dose can reduce action potential duration. Significantly does not change the effective refractory periods of ventricles and auricles. The bystry entering sodium current and, to a lesser extent, the slow entering calcic current oppresses.
Etatsizin slows down carrying out excitement on the carrying-out system of a myocardium. On an ECG lengthening of an interval of PR and the QRS complex appears; ST interval reflecting repolarization of ventricles does not change or tends to shortening.
Etatsizin raises a threshold of fibrillation of a myocardium. Unlike many antiarrhytmic drugs Etatsizin does not cause reliable decrease in ChSS or lengthening of duration of an interval of QT on an ECG.
The antiarrhytmic effect at intake develops usually for 1-2 day, duration of a course of treatment depends on a form of arrhythmia, efficiency and portability of drug.

Pharmacokinetics.
Absorption
At intake drug is quickly soaked up from a GIT and is defined in blood in 30-60 min. Cmax in a blood plasma is reached in 2.5-3 h. Bioavailability - 40%.

Distribution
Linkng with proteins of a blood plasma makes about 90%. Etatsizin gets through a placental barrier. It is allocated with breast milk.

Metabolism
It is intensively metabolized at "the first passing" through a liver. Some of the formed metabolites have antiarrhytmic activity.

Removal
Active agent is removed from an organism with urine in the form of metabolites. T1/2 makes 2.5 h.

Pharmacokinetics in special clinical cases
Parameters of pharmacokinetics of Etatsizin are subject to considerable individual fluctuations and demand individual studying from certain patients for definition of optimum concentration of drug in a blood plasma.

Indications to use:

— supraventricular and ventricular premature ventricular contraction;
— paroxysms of blinking and atrial flutter;
— ventricular and supraventricular tachycardia (including and at WPW syndrome).

Indications to use are limited to existence of crushing organic lesion of heart.

Route of administration and doses:

It is necessary to accept drug inside irrespective of meal on 50 mg 2-3
At insufficient clinical effect the dose is increased (under obligatory control of an ECG) to 50 mg 4 (200 mg) or 100 mg 3 (300 mg).
On reaching lasting antiarrhythmic effect carry out a maintenance therapy in individually picked up minimum effective doses.

Features of use:

Also as well as other antiarrhytmic drugs, Etatsizin can act aritmogenno. Therefore at Etatsizin's appointment follows:

— to strictly consider contraindications to drug use;
— in advance to reveal and eliminate a hypopotassemia;
— to avoid Etatsizin's use in combination with antiarrhytmic drugs of a class I A and class I C;
— it is preferable to begin course treatment in a hospital (especially in the first 3-5 days of administration of drug, taking into account the ECG loudspeakers after trial and repeated doses of Etatsizin or data of monitoring of an ECG);
— to immediately stop treatment at increase of ectopic ventricular complexes, emergence of blockade or bradycardia;
— to stop treatment at expansion of ventricular complexes more than for 25%, reduction of their amplitude, duration of a tooth P on an ECG more than 0.12 sec.

Risk factors of aritmogenny action of Etatsizin: organic lesion of heart (especially postponed myocardial infarction), decrease in fraction of emission of a left ventricle, the maximum doses of drug. Besides, it is necessary to be careful at patients with liver diseases.
At treatment by Etatsizin it is impossible to take alcohol.
During therapy it is regularly necessary to control a condition of the patient and function of cardiovascular system (the ABP, an ECG, EhoKG).

Influence on ability to driving of motor transport and to control of mechanisms
Because of risk of development of dizziness it is not recommended to manage vehicles or to service the difficult mechanisms requiring special attention, ability to concentration.

Side effects:

- From cardiovascular system: a stop of a sinus node, AV blockade, disturbance of intra ventricular conductivity, decrease in contractility of a myocardium, reduction of a coronary blood-groove, arrhythmia, changes on an ECG (lengthening of an interval of PQ, expansion of a tooth P and the QRS complex). Aritmogenny action which probability is most high after the postponed myocardial infarction and at other types of the cardiac pathology leading to decrease in contractility of a muscle of heart and development of heart failure.
- From TsNS: dizziness, a headache, a poshatyvaniye during the walking or turns of the head, small drowsiness; the diplopia, accommodation paresis was in some cases noted.
- From the alimentary system: nausea.
Reduction of side effects or their disappearance after use of drug within 3-4 days is possible. At prolonged treatment by Etatsizin these side effects amplify, and with the termination of administration of drug quickly disappear.
Side effects depend on the size of a dose and to avoid them, it is not necessary to appoint the maximum doses of drug.

Interaction with other medicines:

Etatsizin's use with other antiarrhytmic drugs of the class IC (пропафенон, аллапинин) and the class IA (quinidine, procaineamide, Disopyramidum, Ajmalinum) is contraindicated.
Etatsizin it is not necessary to appoint along with MAO inhibitors.
The combination of beta adrenoblockers with Etatsizin strengthens antiarrhythmic effect, in particular in relation to the arrhythmias provoked by an exercise stress or a stress.

Contraindications:

— the expressed conductivity disturbances (including sinuatrial blockade, AV blockade of II and III degrees in the absence of an artificial pacemaker), disturbance of intra ventricular conductivity;

— disturbances of a heart rhythm in combination with blockade of carrying out on Gis's system - to Purkinye's fibers;

— the expressed hypertrophy of a myocardium of a left ventricle;
— existence of a postinfarction cardiosclerosis;
— cardiogenic shock;
— the expressed arterial hypotension;
— chronic heart failure of II and III functional classes on NYHA classification;
— the expressed disturbances of functions of a liver and/or kidneys;
— concomitant use of MAO inhibitors;
— a concomitant use with antiarrhytmic means of a class I C (пропафенон, аллапинин) and a class I A (quinidine, procaineamide, Disopyramidum, Ajmalinum);
— age up to 18 years (efficiency and safety are not established);
— pregnancy;
— period of a lactation (breastfeeding);
— hypersensitivity to drug components.

With extra care use drug at SSSU, bradycardia, AV blockade of the I degree, ischemic heart disease, heavy disturbances of peripheric circulation, chronic heart failure of the I functional class, closed-angle glaucoma, a benign hyperplasia of a prostate, a cardiomegaly (the risk of development of aritmogenny action), a renal failure, a liver failure, disturbance of electrolytic balance (a hypopotassemia, a hyperpotassemia, a hypomagnesiemia increases).

Use of drug ETATsIZIN at pregnancy and feeding by a breast
Use of drug at pregnancy and in the period of a lactation (breastfeeding) is contraindicated.
Etatsizin gets through a placental barrier. It is allocated with breast milk.

Use at abnormal liver functions
Use of drug at the expressed disturbances of functions of a liver is contraindicated.

Use at renal failures
Use of drug at the expressed disturbances of functions of kidneys is contraindicated.

Overdose:

Symptoms: lengthening of an interval of PR and expansion of the QRS complex, increase in amplitude of a tooth of T, bradycardia, sinuatrial and AV blockade, asystolia, paroxysms of polymorphic and monomorphic ventricular tachycardia, decrease in contractility of a myocardium, permanent decrease in the ABP, dizziness, sight zatumanennost, headache, disorders of a GIT.

Treatment: carry out symptomatic therapy. For treatment of ventricular tachycardia it is not necessary to use antiarrhytmic drugs of classes of IA and IC. Natrii hydrocarbonas is capable to eliminate expansion of the QRS complex, bradycardia and arterial hypotension.

Storage conditions:

List B. Drug should be stored in the unavailable to children, dry, protected from light place at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 50 mg. According to 10 tab. in a blister strip packaging from the film of PVC and printing aluminum foil varnished. On 5 blister strip packagings in a pack from a cardboard.