Propanorm tablets p / o 150mg, No. 50

- Prevention and treatment of supraventricular and ventricular extrasystoles,

paroxysmal rhythm disturbances (supraventricular - atrial fibrillation and flutter, Wolff-Parkinson-White syndrome), atrioventricular re-entry tachycardia;

- Prevention of persistent monomorphic ventricular tachycardia.

Inside. The tablets should be swallowed whole after meals with a little water.
The dosage regimen is set individually and adjusted by the doctor.
The daily dose is 450 mg (3 times a day, 150 mg every 8 hours). The dose is increased gradually (every 3-4 days) up to 600 mg / day for 2 doses per day or up to a maximum of 900 mg / day for 3 doses.
If during treatment there is an expansion of the QRS complex or the QT interval by more than 20% compared to baseline values, or an extension of the PQ interval by more than 50%, an extension of the QT interval by more than 500 ms, an increase in the frequency and severity of arrhythmias, the dose should be reduced or temporarily interrupt the use of Propanorm.
In patients over 70 years of age, as well as in patients weighing less than 70 kg, smaller doses are used (the first dose is given in a hospital under the control of ECG and blood pressure).
In case of impaired liver function (cumulation is possible), Propanorm is used in doses of 20-30% of the usual, in case of impaired renal function (creatinine clearance less than 10%), the initial dose is 50% of the original.

Each coated tablet contains:

active substance: propafenone hydrochloride 150 mg (corresponds to propafenone 135.7 mg).

excipients : microcrystalline granular cellulose, corn starch, copovidone, croscarmellose sodium, magnesium stearate, sodium lauryl sulfate, hypromellose 5, macrogol 6000, titanium dioxide, emulsion of dimethicone with silicon dioxide.

- Hypersensitivity to the drug and drug components, intoxication with digoxin;

- Severe forms of chronic heart failure (in the stage of decompensation), uncontrolled chronic heart failure;

- Cardiogenic shock (except for arterial hypotension due to tachycardia and antiarrhythmic shock);

- Severe bradycardia and severe arterial hypotension;

- SA blockade, violation of intra-atrial conduction;

- Blockade of the legs of the bundle of His;

- Intraventricular bifascicular blockade and AV block II-III degree (without pacemaker);

- Sick sinus syndrome;

- Syndrome 'tachycardia-bradycardia';

- Myocardial infarction;

- Lactation period;

- Age up to 18 years (efficacy and safety have not been established).

With care : chronic obstructive pulmonary disease (COPD), myasthenia gravis (including myasthenia gravis), heart failure (ejection fraction less than 30%), cardiomyopathy, arterial hypotension, patients with a permanent or temporary pacemaker; hepatic cholestasis, hepatic and / or renal failure, a combination with other antiarrhythmic drugs similar in their effect on the electrophysiology of the heart, electrolyte disturbances (must be corrected before the appointment of propafenone), age over 70 years.

Trade name : PropanormЃ

International non-proprietary name : propafenone

Dosage form : coated tablets

Composition .

Each coated tablet contains:

active substance: propafenone hydrochloride 150 mg or 300 mg (corresponds to propafenone 135.7 mg and 271.05 mg).
excipients : microcrystalline granular cellulose, corn starch, copovidone, croscarmellose sodium, magnesium stearate, sodium lauryl sulfate, hypromellose 5, macrogol 6000, titanium dioxide, emulsion of dimethicone with silicon dioxide.

Description . Round, biconvex coated tablets of white or almost white color.

Pharmacotherapeutic group : antiarrhythmic agent.

Pharmacological properties
Pharmacodynamics
Class I C antiarrhythmic drug, blocks fast sodium channels. It has a weak ?-adrenergic blocking activity (corresponds to about 1/40 of the activity of propranolol) and an M-anticholinergic effect. The antiarrhythmic effect is based on a local anesthetic and direct membrane stabilizing effect on myocardiocytes, as well as on the blockade of adrenergic beta receptors and calcium channels.
The local anesthetic effect roughly corresponds to the activity of procaine. Propafenone, blocking fast sodium channels, causes a dose-dependent decrease in the rate of depolarization and inhibits phase 0 of the action potential and its amplitude in Purkinje fibers and ventricular contractile fibers, inhibits automatism. Slows down the conduction along the Purkinje fibers. Extends the time of conduction in the sinoatrial (SA) node and atria. With the use of propafenone, the PQ interval lengthens and the QRS complex expands (from 15 to 25), as well as the A-H and HV intervals. By slowing down the conduction, the drug lengthens the effective refractory period in the atria, in the atrioventricular (AV) node, in additional bundles, and, to a lesser extent, in the ventricles. There are no significant changes in the QT interval.Electrophysiological effects are more pronounced in ischemic than in normal myocardium. It has a negative inotropic effect, which is usually manifested when the left ventricular ejection fraction decreases below 40%. The action begins 1 hour after ingestion, reaches a maximum after 2-3 hours and lasts 8-12 hours.

Pharmacokinetics
More than 95% of the drug is absorbed. Propafenone exhibits dose-dependent bioavailability, which increases non-linearly with increasing dose: it increases from 5% to 12% with an increase in a single dose from 150 mg to 300 mg, and at 450 mg - up to 40-50%. The maximum concentration in blood plasma after oral administration is reached within 1-3.5 hours and its concentration ranges from 500 to 1500 ?g / l. Permeability through the blood-brain and placental barrier is low. The volume of distribution is 3-4 t / kg. Communication with proteins of blood plasma and internal organs (liver, lungs, etc.) - 85-97%. 11 metabolites of the drug are described, pharmacologically active - 5-hydroxypropafenone and N-depropylpropafenone, which have antiarrhythmic activity comparable to propafenone. Oxidative metabolism depends on a specific cytochrome, whose activity is genetically determined.
The therapeutic range of concentration of propafenone in blood plasma is 0.5-2.0 mg / l. Propafenone is almost completely metabolized. The half-life (T?) In 'fast' metabolizers is 2-10 h, in 'slow' ones - 10-32 h, biological T? is about 6.2 hours. It is excreted by the kidneys - 38% in the form of metabolites (less than 1% unchanged), with bile - 53% (in the form of glucuronides and sulfates of metabolites and the active substance). With hepatic insufficiency, excretion is reduced.

Indications for use
- Prevention and treatment of supraventricular and ventricular extrasystoles,

paroxysmal rhythm disturbances (supraventricular - atrial fibrillation and flutter, Wolff-Parkinson-White syndrome), atrioventricular re-entry tachycardia;

- Prevention of persistent monomorphic ventricular tachycardia.

Contraindications

- Hypersensitivity to the drug and drug components, intoxication with digoxin;

- Severe forms of chronic heart failure (in the stage of decompensation), uncontrolled chronic heart failure;

- Cardiogenic shock (except for arterial hypotension due to tachycardia and antiarrhythmic shock);

- Severe bradycardia and severe arterial hypotension;

- SA blockade, violation of intra-atrial conduction;

- Blockade of the legs of the bundle of His;

- Intraventricular bifascicular blockade and AV block II-III degree (without pacemaker);

- Sick sinus syndrome;

- Syndrome 'tachycardia-bradycardia';

- Myocardial infarction;

- Lactation period;

- Age up to 18 years (efficacy and safety have not been established).

With care : chronic obstructive pulmonary disease (COPD), myasthenia gravis (including myasthenia gravis), heart failure (ejection fraction less than 30%), cardiomyopathy, arterial hypotension, patients with a permanent or temporary pacemaker; hepatic cholestasis, hepatic and / or renal failure, a combination with other antiarrhythmic drugs similar in their effect on the electrophysiology of the heart, electrolyte disturbances (must be corrected before the appointment of propafenone), age over 70 years.

Pregnancy and lactation
The use of propafenone during pregnancy, especially in the first trimester, is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.

Dosing and Administration
Inside. The tablets should be swallowed whole after meals with a little water.
The dosage regimen is set individually and adjusted by the doctor.
The daily dose is 450 mg (3 times a day, 150 mg every 8 hours). The dose is increased gradually (every 3-4 days) up to 600 mg / day for 2 doses per day or up to a maximum of 900 mg / day for 3 doses.
If during treatment there is an expansion of the QRS complex or the QT interval by more than 20% compared to baseline values, or an extension of the PQ interval by more than 50%, an extension of the QT interval by more than 500 ms, an increase in the frequency and severity of arrhythmias, the dose should be reduced or temporarily interrupt the use of Propanorm.
In patients over 70 years of age, as well as in patients weighing less than 70 kg, smaller doses are used (the first dose is given in a hospital under the control of ECG and blood pressure).
In case of impaired liver function (cumulation is possible), Propanorm is used in doses of 20-30% of the usual, in case of impaired renal function (creatinine clearance less than 10%), the initial dose is 50% of the original.

Side effect
From the side of the cardiovascular system: bradycardia, AV dissociation, ventricular tachyarrhythmias, angina pectoris, worsening of the course of heart failure (in patients with reduced left ventricular function), SA blockade, AV blockade, intraventricular conduction disorders, supraventricular tachyarrhythmias, when taken in high doses - orthostatic hypotension.
From the digestive system: a change in taste, dry mouth, bitterness in the mouth, nausea, decreased appetite, a feeling of heaviness in the epigastrium, constipation or diarrhea, rarely - liver dysfunction, cholestatic jaundice, cholestasis.
From the side of the central nervous system: headache, dizziness, rarely - blurred vision, diplopia, convulsions.
Laboratory indicators:leukopenia, agranulocytosis, increased bleeding time, thrombocytopenia, the appearance of antinuclear antibodies.
From the genitourinary system: oligospermia, decreased potency.
Allergic reactions: skin rash, itching, exanthema, skin redness, urticaria, lupus-like syndrome.
Others: weakness, bronchospasm, hemorrhagic skin rashes.

Overdose
Intoxication can occur with a single dose of 2 times the daily dose; symptoms of intoxication appear after 1 hour, maximum - after a few hours.
Symptoms: persistent decrease in blood pressure, nausea, dry mouth, vomiting, mydriasis, drowsiness, extrapyramidal disorders, confusion, bradycardia, prolongation of the QT interval, disturbances in intra-atrial and intraventricular conduction, ventricular tachyarrhythmias, paroxysms of tachycardia and polymorphic ventricular block, SA asystole, coma, convulsions, delirium, pulmonary edema.
Treatment: gastric lavage, defibrillation, administration of dobutamine, diazepam; if necessary, artificial ventilation of the lungs and chest compressions. Hemodialysis is not effective.

Interaction with other medicinal products
Cannot be combined with lidocaine (cardiodepressant effect is enhanced).
Increases the plasma concentration of propranolol, metoprolol, digoxin (the risk of glycoside intoxication increases), indirect anticoagulants, cyclosporine. Enhances the effect of warfarin (blocks metabolism).
With simultaneous use with beta-blockers, tricyclic antidepressants, an increase in the antiarrhythmic effect is possible, with local anesthetics - an increase in the risk of damage to the central nervous system.
Cimetidine and quinidine, slowing down metabolism, increase the concentration of propafenone in plasma by 20%, rifampicin - reduces.
Amiodarone increases the risk of pirouette-type tachycardia.
Drugs that inhibit SA and AV nodes and have a negative inotropic effect increase the risk of side effects.
Medicines that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

Special instructions
During the course of treatment, especially at the beginning of therapy, ECG monitoring is necessary.
It is recommended to start treatment in a hospital setting, since the risk of arrhythmogenic effects associated with the use of propafenone is increased. The use of Propanorm should be carried out under the control of the electrolyte balance of the blood (especially the concentration of potassium) and ECG; periodically it is necessary to determine the activity of 'hepatic' transaminases.
In the treatment of ventricular arrhythmias, propafenone is more effective than class IA and IB antiarrhythmic drugs.
In patients with insufficient liver function, the bioavailability of propafenone increases by 70%, in such patients it is recommended to reduce the dose and conduct regular monitoring of laboratory parameters.
The indications and dose should be especially carefully determined for patients with an inserted pacemaker.
For patients undergoing long-term treatment with anticoagulants and hypoglycemic drugs, it is necessary to conduct careful clinical and laboratory monitoring.
If SA blockade or AV block of the III degree, or often repeated extrasystole, appear during therapy, then the treatment must be interrupted.
Given the possibility of proarrhythmogenic effects, the drug is recommended to be used only as directed and under the supervision of a physician.
During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form
Film-coated tablets, 150 mg and 300 mg each.
There are 10 tablets in a blister, 5 blisters together with instructions for use in a cardboard box.

Storage conditions
List B. In a dry, dark place, out of reach of children, at a temperature of 15-25 ? C.

Shelf life is
3 years.
Do not use after the date indicated on the package.

Terms of dispensing from pharmacies
Prescription.