Propanorm, pills 150mg, 50pcs

Composition

Active ingredient:

propafenone hydrochloride 150 mg;

Auxiliary substances:

Microcrystalline granulated cellulose,

corn starch,

copovidone,

sodium croscarmellose,

magnesium stearate,

sodium lauryl sulfate,

hypromellose 5,

macrogol 6000,

titanium dioxide,

dimethicone emulsion with silicon dioxide.

Pharmacological action

Propanorm is an antiarrhythmic drug.

Pharmacodynamics

An IC-class antiarrhythmic drug that blocks fast sodium channels. It has a weak beta-adrenoblocking activity and m-holinoblocking effect. The antiarrhythmic effect is based on a local anesthetic and direct membrane-stabilizing effect on myocardiocytes, as well as on the blockade of beta-adrenergic receptors and calcium channels.

It causes a dose-dependent decrease in the depolarization rate, inhibits phase 0 of the action potential and its amplitude in Purkinje fibers and ventricular contractile fibers, and inhibits automatism. Slows down the flow of Purkinje fibers. Lengthens the time of sinoatrial (SA) node and atrial conduction. When propafenone is used, the PQ interval is lengthened and the QRS complex is expanded (from 15 to 25), as well as the AH and HV intervals. The drug prolongs the effective refractory period in the atria, in the internode, 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 usually manifests itself when the left ventricular ejection fraction decreases below 40%.

The action begins 1 hour after ingestion, reaches a maximum in 2-3 hours and lasts 8-12 hours

. Pharmacokinetics

More than 95% of the drug is absorbed. Propafenon showed a dose-dependent bioavailability, which increases nonlinearly with the increase of dose increases from 5% to 12% with increasing dose from 150 to 300 mg and 450 mg in up to 40-50%. C_max in blood plasma after an oral dose is achieved within 1 to 3,5 h and ranges from 500 to 1500 µg/L. Permeability through the BBB and placental barrier is low. The volume of distribution is 3-4 l / kg. The relationship with plasma proteins and internal organs (liver, lungs, etc. ) is 85-97%.

The therapeutic range of propafenone concentration in blood plasma is 0.5–2.0 mg/l. Propafenone is almost completely metabolized. 11 metabolites of the drug are described: 5-hydroxypropaphenone and N-depropropaphenone are pharmacologically active and have antiarrhythmic activity comparable to propafenone. T_1/2 “fast metabolizers” — 2-10 hours, “slow” – 10-32 hours, biological_{T 1/2} 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). With hepatic insufficiency, excretion decreases.

Indications

Prevention and treatment of supraventricular and ventricular extrasystoles, paroxysmal rhythm disorders (supraventricular-atrial fibrillation and flutter, WPW-syndrome), atrioventricular re-entry tachycardia;

prevention of persistent monomorphic ventricular tachycardia.

Use during pregnancy and lactation

The use of propafenone during pregnancy, especially in the first trimester, is possible only if the expected benefit to the mother exceeds the potential risk to the fetus.

Contraindications

• hypersensitivity to the components of the drug;
• digoxin intoxication;
• severe forms of chronic heart failure (decompensation), uncontrolled congestive heart failure;
• cardiogenic shock (with the exception of hypotension due to tachycardia, antiarrhythmic and shock);
• bradycardia and severe hypotension;
• SA blockade, a violation of vnutriepreserdna conduct; blockade of the legs of bundle branch block, intraventricular bifascicular blockade and AV blockade of II–III degree (without pacemaker);
• the syndrome of weakness of the sinus node syndrome “tachycardia-bradycardia”;
• myocardial infarction;
• lactation,
• age under 18 years (effectiveness and safety not established).

With caution:

• chronic obstructive pulmonary disease (COPD);
• myasthenia gravis (including myasthenia gravis);
• heart failure (ejection fraction less than 30%), cardiomyopathy, hypotension, presence of a permanent or temporary pacemaker;
• hepatic cholestasis, hepatic and/or renal failure;
• combination with other antiarrhythmic means, a similar influence on the electrophysiology of the heart;
• electrolyte disturbances (must necessarily be adjusted prior to the appointment of propafenon);
• age over 70 years.

Side effects

From the cardiovascular system: bradycardia, AV dissociation, ventricular tachyarrhythmias, angina pectoris, worsening of the course of heart failure (in patients with reduced left ventricular function), sinoatrial block, AV block, intraventricular conduction disorders, supraventricular tachyarrhythmias, when taken in high doses – orthostatic hypotension.

From the digestive system: changes in taste, dry mouth, bitterness in the mouth, nausea, decreased appetite, a feeling of heaviness in the epigastrium, constipation or diarrhea; rarely-liver function disorders, cholestatic jaundice, cholestasis.

From the central nervous system: headache, dizziness; rarely-blurred vision, diplopia, convulsions.

From the hematopoietic system: leukopenia, agranulocytosis, increased bleeding time, thrombocytopenia, the appearance of antinuclear antibodies.

On the part of the reproductive system: oligospermia, decreased potency.

Allergic reactions: skin rash, pruritus, exanthema, redness of the skin, urticaria, lupus-like syndrome.

Others: weakness, bronchospasm, hemorrhagic skin rashes.

Interaction

Do not combine Propanorm with lidocaine, because the cardiodepressive effect increases.

When used concomitantly, propafenone increases the concentration of propranolol, metoprolol, digoxin (increases the risk of glycoside intoxication), indirect anticoagulants, cyclosporine in blood plasma.

When used concomitantly, propafenone enhances the effect of warfarin (by blocking metabolism).

When used concomitantly with beta-blockers, tricyclic antidepressants, it is possible to increase the antiarrhythmic effect.

When used concomitantly with local anesthetics, the risk of CNS damage increases.

Cimetidine and quinidine, slowing down the metabolism, increase the concentration of propafenone in plasma by 20%, rifampicin-reduces.

When used concomitantly with propafenone, amiodarone increases the risk of developing pirouette-type tachycardia.

Drugs that depress the sinoatrial node and AV node and have a negative inotropic effect, when used simultaneously with propafenone, increase the risk of side effects.

Drugs that inhibit bone marrow hematopoiesis, when used simultaneously with propafenone, increase the risk of myelosuppression.

How to take, course of use and dosage

The dosage regimen is set individually and adjusted by the doctor.

The drug is taken after a meal. Tablets should be swallowed whole, without chewing, with a small amount of water.

The drug is prescribed 150 mg 3 times a day (every 8 hours). The daily dose is 450 mg.

The dose is increased gradually (every 3-4 days) to 600 mg/day (divided into 2 doses) or up to a maximum of 900 mg/day (divided into 3 doses).

If during treatment there is an extension of the QRS complex or 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 msec, an increase in the frequency and severity of arrhythmia, the dose should be reduced or the use of Propanorm should be temporarily interrupted.

Application in case of impaired liver function: In case of impaired liver function (accumulation is possible), Propanorm is used in doses of 20-30% of the usual.

Use in patients with impaired renal function: In patients with impaired renal function ( creatinine clearance

Use in elderly patients and in patients weighing less than 70 kg: In patients over 70 years of age, as well as in patients with a body weight of

Overdose

With a single dose of 2 times the daily dose, symptoms of intoxication may appear in 1 hour, maximum-in a few hours.

Symptoms: persistent decrease in blood pressure, nausea, dry mouth, vomiting, mydriasis, drowsiness, extrapyramidal disorders, confusion, bradycardia, prolongation of the QT interval, atrial and intraventricular conduction disorders, ventricular tachyarrhythmias, paroxysms of polymorphic ventricular tachycardia, sinoatrial block, AV block, asystole, coma, convulsions, delirium, pulmonary edema.

Treatment: gastric lavage, defibrillation, use of dobutamine, diazepam; if necessary – mechanical ventilation and indirect heart massage. Hemodialysis is ineffective.

Special instructions

ECG monitoring is necessary during the course of treatment, especially at the beginning of therapy.

Treatment is recommended to start in a hospital setting, as the risk of arrhythmogenic effects associated with the use of propafenone is increased.

Propanorm should be used under the control of blood electrolyte balance (especially potassium concentration) and ECG; periodically, the activity of hepatic transaminases should be determined.

In the treatment of ventricular arrhythmias, propafenone is more effective than Class IA and class IB antiarrhythmic drugs.

Indications and dosage should be determined especially carefully for patients with an installed pacemaker.

It is necessary to conduct clinical and laboratory monitoring of patients undergoing long-term treatment with anticoagulants and hypoglycemic drugs, while simultaneously using Propanorm.

If treatment involves sinoatrial block or grade III AV block, or frequently recurring extrasystole, then treatment should be interrupted.

Given the possibility of proarrhythmogenic effects, the drug is recommended to be used only as prescribed and under the supervision of a doctor.

– Use in patients with impaired liver function: In patients with hepatic insufficiency, the bioavailability of propafenone increases by 70%, in such patients it is recommended to reduce the dose and conduct regular monitoring of laboratory parameters. When liver function is impaired (accumulation is possible), Propanorm is used in doses of 20-30% of the usual dose.

– Use in patients with impaired renal function: In patients with impaired renal function ( creatinine clearance

Influence on the ability to drive motor vehicles or manage mechanisms: During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-25 °C

Shelf life

3 years

Active ingredient

Propafenone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Arrhythmia