Ethmosinum

General characteristics. Structure:

Active agent: moratsizina hydrochloride of 25 or 100 mg.

Excipients: potato starch; sugar; calcium stearate; magnesium carbonate; titanium dioxide (Е 171); silicon dioxide; wheat flour; beeswax; dye quinolinic yellow (Е 104); dye solar yellow FCF (Е 110).

Pharmacological properties:

Blocks "bystry" natrium channels, stabilizes membranes of cardiomyocytes. Reduces excitability, speed of carrying out impulses and automatism owing to the slowed-down carrying out through an AV node and Gisa-Purkinye's system. Reduces action potential duration in Purkinye's fibers, reduces the effective refractory period. 0 depolarizations reduce the maximum speed of a phase, does not influence amplitude of action potential and the maximum diastolic potential. Does not exert impact on the refractory periods of auricles, an AV node and a left ventricle, in the minimum degree affects repolarization of ventricles. Does not influence carrying out in a sinuatrial node or on intra atrial carrying out, has insignificant effect on duration of a sinus cycle and for the period of recovery of activity of a sinuatrial node.
Causes small, but permanent increase in the ABP and ChSS at rest. Has the expressed mestnoanesteziruyushchy and membrane stabilizing activity. Can suppress aggregation of thrombocytes, has anticholinergic activity.

Pharmacokinetics. After intake it is well soaked up from a GIT, absorption is slowed down at reception in 30 min. after food. Cmax in blood is reached during 0,5–2 h. Linkng with blood proteins makes 90–95%. It is intensively metabolized at "the first passing" through a liver with education to 26 metabolites (two of them pharmacological are active). Induces own metabolism through system of P450 cytochrome. T1/2 makes 1,5–3 h (at a single dose – 1,5 h, at course – to 3 h). 56% of drug in the form of metabolites are removed with bile, 39% — kidneys. In small degree is exposed to repeated absorption.

Indications to use:

Supraventricular and ventricular premature ventricular contraction, paroxysm of blinking and atrial flutter, Bouveret's supraventricular disease, including syndrome Wolff-Parkinson-Whyte (WPW syndrome), Bouveret's ventricular disease (in the absence of organic lesions of heart).

Route of administration and doses:

Inside. The dose is selected individually depending on effect and portability. The Ethmosinum is accepted by each 8 h, having divided a daily dose into 3 equal parts, usually daily dose makes 600–800 mg.

At the expressed renal failures correction of the mode of dosing and careful monitoring of a condition of the patient is required.

At first select well tolerable dose, then increase it before achievement of optimum effect. Before purpose of drug and at selection of doses use control of an ECG, Holterovsky monitoring of an ECG, the test with exercises and program electric stimulation. At patients who well transfer drug long therapy is possible.

Features of use:

During therapy it is necessary to control carefully a condition of the patient and function of cardiovascular system, at long reception — to control function of a liver.

Prior to treatment by the Ethmosinum the 2 weeks break after reception of MAO inhibitors is necessary. For the period of treatment it is necessary to refrain from alcohol intake, and also from control of vehicles. It is necessary to be careful to patients at whom side effect from TsNS is shown (dizziness, fatigue, a headache).

Side effects:

- From a nervous system and sense bodys: dizziness, headache, hyperesthesia or paresthesia, uneasiness, sleep disorder, fatigue and weakness, amnesia, sonitus, dysarthtia, sight illegibility, nystagmus.
- From cardiovascular system and blood (a hemopoiesis, a hemostasis): a stethalgia, an asthma, aritmogenny effect, a ciliary arrhythmia, AV blockade, intra ventricular blockade, decrease and increase in the ABP and bradycardia (at reception of high doses).
- From respiratory system: cough, bronchospasm, apnoea.
- From bodies of a GIT: dryness in a mouth, nausea, vomiting, diarrhea; seldom — a hepatotoxic action, a gastralgia, increase in activity of hepatic transaminases.
- Other: hand and legs pain, peripheral hypostases, it is rare – fever, allergic reactions.

Interaction with other medicines:

At simultaneous use with other antiarrhytmic means the risk of aritmogenny action amplifies. It is incompatible with MAO inhibitors (risk of aritmogenny action), barbiturates.

Digoxin can strengthen the oppressing influence of the Ethmosinum on the carrying-out system of heart, propranolol strengthens effect of the Ethmosinum, Cimetidinum increases concentration of an Ethmosinum in blood (at simultaneous use it is necessary to lower the Ethmosinum dose).

The Ethmosinum increases concentration of theophylline in blood.

Contraindications:

Hypersensitivity, AV blockade of the II-III degree, cardiogenic shock, chronic heart failure of the II-III degree, the expressed arterial hypotension, an abnormal liver function and/or kidneys, pregnancy, feeding by a breast, age up to 18 years (experience of use is absent).

With extra care — a cardiomegaly (the risk of aritmogenny action increases), heavy chronic heart failure (the aggravation of symptoms and increase in risk of aritmogenny action), an ischemic heart disease and a myocardial infarction in the anamnesis is possible, the abnormal liver function (the clearance decreases and T1/2 increases, in such cases it is recommended to apply lower doses and to conduct careful monitoring of a condition of the patient), a hypopotassemia, a hyperpotassemia and/or a hypomagnesiemia (change of nature of effect of drug is possible, before an initiation of treatment it is necessary to eliminate disturbance of salt balance), a syndrome of weakness of a sinus node since time of recovery of function of a sinus node increases, are possible a sinus bradycardia, the temporary termination of activity or full "stop" of a sinus node.

With care to apply at patients with an electrocardiostimulator. Treatment is recommended to be begun in a hospital because of risk of the aritmogenny action connected using a moratsizin (development of aritmogenny action does not depend on a dose and it is the most probable within the first week of treatment).

Use at pregnancy and feeding by a breast
It is possible if the expected effect of therapy exceeds potential risk for a fruit (adequate and strictly controlled researches of safety of use for pregnant women are not conducted). For the period of treatment it is necessary to stop breastfeeding (gets into breast milk).

Overdose:

Symptoms: conductivity disturbance, the expressed decrease in the ABP, development or aggravation of symptoms of heart failure, a myocardial infarction, blockade of a sinus node, arrhythmia (including a nodal bradycardia, ventricular tachycardia, fibrillation of ventricles, an asystolia), vomiting, slackness, a coma, a syncope, диспноэ.

Treatment: symptomatic.

Storage conditions:

In the dry, protected from light place.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In bottles plastic on 50 pieces or in plastic bags on 8 kg; in capacity 1 bag.