Etatsizin

Active material: 2-karʙetoksiamino-10-(3-diethylaminopropionyl)-phenothiazine hydrochloride
When ATH: C01BC
CCF: Antiarrhythmic drugs. Класс I C
ICD-10 codes (testimony): I45.6, I47.1, I47.2, I48, I49.4
When CSF: 01.11.01.01.03
Manufacturer: OLAINFARM AS (Latvia)

Pharmaceutical form, composition and packaging

Pills, coated yellow color, round, in cross section showed two layers.

1 tab.
2-karʙetoksiamino-10-(3-diethylaminopropionyl)-phenothiazine hydrochloride50 mg

Excipients: potato starch, sucrose, methyl cellulose, calcium stearate.

The composition of the shell: sucrose, povidone, quinoline yellow dye (E104), colorant sunset yellow (E110), calcium carbonate, magnesium gidroksicarbonat main, Titanium dioxide (E171), silicon dioxide, carnauba wax.

10 PC. – packings Valium planimetric (5) – packs cardboard.

 

Pharmacological action

Antiaritmicski product class I, C. It has long antiaritmicski effect. Depresses the rate of rise of the front of the building (Vmax), does not change the resting potential.

Depending on the dose may reduce the duration of the building. It does not change significantly effective refrakternae periods of the ventricles and Atria. Oppressing Quick incoming sodium current and, less, slow incoming calzievy current.

Ethacyzin slows down the holding institution to meet the myocardium. On the ECG appears lengthening of the interval PR and QRS complex; ST interval, reflecting the slowed repoliarizatia fibrillation, does not change or tends to decreases.

Ethacyzin increases the threshold of ventricular myocardium. Unlike many complications drugs Ethacyzin causes no reliable reduce HEART RATE or lengthening the duration of the QT interval on the ECG.

The ingestion antiaritmicski effect usually develops on 1-2 day, duration of treatment depends on the type of arrhythmia, efficacy and tolerability.

 

Pharmacokinetics

Absorption

The ingestion drug is rapidly absorbed from the digestive tract and is determined in the blood through 30-60 m. Cmax plasma levels achieved after 2.5-3 no. Bioavailability – 40%.

Distribution

Binding to plasma proteins is approximately 90%. Ethacyzin penetrates through the placental barrier. Provided with breast milk.

Metabolism

Intensive metabolised in “first pass” through the liver. Some of the formed metabolites have antiaritmicescoy activity.

Deduction

The body of the active substance presented with urine in the form of metabolites. T1/2 is 2.5 no.

Pharmacokinetics in special clinical situations

Pharmacokinetics Etazizina subject to large individual variations and require case-by-case examination of individual patients to determine the optimal concentrations of the drug in plasma.

 

Testimony

— najeludochkovaya and ventricular arrythmia;

is a frequent flicker and atrial flutter;

-Ventricular and najeludochkovaya tachycardia (in t. no. and the syndrome WPW).

Indications for use are limited to the presence of heavy organic lesion of the heart.

 

Dosage regimen

The drug is taken orally with or without food for 50 mg 3 times / day.

With little clinical effect dose (under the mandatory supervision of ECG) to 50 mg 4 times / day (200 mg) or 100 mg 3 times / day (300 mg).

On reaching the strong protivoaritmicheskogo effect conducting supportive therapy in individually selected minimum effective dose.

 

Side effect

Cardio-vascular system: Stop sinus, AV блокада, violation of intraventricular conduction, reducing sokratimosti attack, reduced coronary blood flow, arrhythmia, ECG changes (extension PQ interval, expansion of r-wave and QRS complex). Aritmogennoe action, probability is greatest after suffering a myocardial infarction and other kinds of heart diseases, leading to a decline in heart muscle contractility and heart failure development.

CNS: dizziness, headache, unsteady when walking or turns of a head, slight drowsiness; in some cases there was diplopia, Parez akkomodacii.

From the digestive system: nausea.

May reduce side effects or their disappearance after applying medication for 3-4 days. In long-term care Jetacizinom these side effects are not amplified, but with the cessation of the drug quickly disappear.

Side effects depend on the magnitude of the dose and, to avoid, nor should appoint maximum dose.

 

Contraindications

— expressed violations conductivity (incl. sinoatrialynaya blockade, AV-блокада II и III степени) in the absence of artificial pacemaker, violation of intraventricular conduction;

-cardiac arrhythmias in conjunction with blockades of GISA – Purkinje fibers;

is pronounced myocardial hypertrophy of left ventricle;

— availability of postmyocardial infarction cardiosclerosis;

- Cardiogenic shock;

- Severe hypotension;

-chronic heart failure functional class II and III;

-expressed human liver and/or kidney disease;

- Simultaneous MAO inhibitors;

-simultaneous reception antiaritmicakimi class I tools with (moracizin/atmozin/, propafenone, allapinin) and class I and (quinidine, prokaynamyd, disopyramide, aimalin);

- Up to 18 years (efficacy and safety have not been established);

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

FROM caution the preparation is used when SSSU, ʙradikardii, AV-блокаде I степени, CHD, heavy human peripheral blood circulation, chronic heart failure functional class I, angle closure glaucoma, benign prostatic hyperplasia, kardiomegalii (increases the risk of aritmogennogo actions), renal failure, hepatic insufficiency, violation of elektrolitnogo balance (hypokalemia, hyperkalemia, gipomagniemii).

 

Pregnancy and lactation

Do not use this drug during pregnancy and lactation (breast-feeding).

Ethacyzin penetrates through the placental barrier. Provided with breast milk.

 

Cautions

Also like other antiarrhythmic drugs, Ethacyzin can act aritmogenno. Therefore, in appointing Etazizina should:

— strictly take into account contraindications to the medication;

-identify and resolve in advance hypokaliemia;

— avoid Etazizina in combination with drugs antiaritmicakimi class I a and class I with;

-course treatment, preferably starting in the hospital (particularly in the first 3-5 day dosing, given the dynamics of ECG after trial and repeated doses Etazizina or ECG monitoring data);

-to immediately cease treatment of frequent ventricular ectopic complexes, the emergence of blockades or bradycardia;

-stop treatment when extending ventricular complexes of more than 25%, reduce their amplitude, duration of ECG r-wave more 0.12 sec.

Risk factors aritmogennogo Etazizina actions: organic lesion of the heart (especially myocardial infarction), decrease in left ventricular ejection fraction, maximum dosage. Besides, You should use caution in patients with liver diseases.

When treating Jetacizinom not to consume alcohol.

During therapy should regularly monitor the patient's condition and function of the cardiovascular system (FROM, ECG, Echocardiography).

Effects on ability to drive vehicles and management mechanisms

Due to the risk of dizziness is not recommended driving or maintain complex mechanisms, requiring special attention, ability to concentrate.

 

Overdose

Symptoms: PR interval extension and expansion of micro, increased amplitude t wave inversion, bradycardia, sinoatrialnaya and AV-blokada, asistolija, frequent and detect polymorphic ventricular tachycardia, reducing sokratimosti attack, stable lowering ad, dizziness, blurred vision, headache, gastrointestinal disorders.

Treatment: symptomatic therapy. For the treatment of ventricular tachycardia should not use antiarrhythmic classes I, a and I,. Sodium bicarbonate is capable of removing the expansion of micro, bradycardia and hypertension hypotension.

 

Drug Interactions

Contraindicated use Etazizina with other antiaritmicakimi drugs class I with (moracizin/atmozin/, propafenone, allapinin) and class I and (quinidine, prokaynamyd, disopyramide, aimalin).

Ethacyzin should not be administered concomitantly with MAO inhibitors.

The combination of beta-adrenoblokatorov with Jetacizinom enhances protiwaritmicescoe action, especially in relation to arrhythmias, provociruemym physical activity or stress.

 

Conditions of supply of pharmacies

The drug is released under the prescription.

 

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 30 ° C. Shelf life – 3 year.

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