Propanorm, 300 mg 50 pcs

A class IC antiarrhythmic drug, blocks fast sodium channels.

It has weak ?-adrenoblocking activity (corresponds to about 1/40 part of the activity of propranololol) and m-cholinoblocking effect. Antiarrhythmic effect is based on local anesthetic and direct membrane stabilizing effect on myocardiocytes as well as on blockade of adrenergic ?-adrenoreceptors and calcium channels.

The local anesthetic action corresponds approximately to the activity of procaine.

Propafenone, by blocking fast sodium channels, causes a dose-dependent decrease in the rate of depolarization and inhibits phase 0 action potential and its amplitude in Purkinje and ventricular contractile fibers, inhibits automatism. Slows conduction along Purkinje fibers.

Longens conduction time in the sinoatrial node and atria. The use of propafenone results in prolongation of the PQ interval and extension of the QRS complex (15 to 25) on the ECG, as well as the NA and HV intervals on the histogram.

Inhibiting conduction, the drug prolongs the effective refractory period in the atria, AV node, accessory bundles, and, to a lesser extent, the ventricles. No significant changes in the QT interval are observed.

The electrophysiological effects are more pronounced in ischemic than in normal myocardium. It has a negative inotropic effect, which is usually seen when left ventricular ejection fraction decreases below 40%.

The action of the drug starts 1 hour after oral administration, reaches a maximum of 2-3 hours and lasts for 8-12 hours.

Indications

Active ingredient

Composition

1 coated tablet contains:

Propafenone hydrochloride 300 mg, which corresponds to the content of propafenone 271.05 mg.

Auxiliary substances:

Microcrystalline granulated cellulose,

Corn starch,

copovidone,

sodium croscarmellose,

magnesium stearate,

sodium lauryl sulfate,

hypromellose 5,

macrogol 6000,

titanium dioxide,

emulsion of dimethicone with silicon dioxide.

How to take, the dosage

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

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

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

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

If during treatment, extension of QRS complex or QT interval by more than 20% compared to baseline values, or prolongation of PQ interval by more than 50%, prolongation of QT interval by more than 500 msec, increase in arrhythmia frequency and severity, the dose should be reduced or Propanorm should be temporarily stopped.

Propanorm use in hepatic dysfunction: If liver function is impaired (cumulation is possible), Propanorm is used in doses that are 20-30% of the usual dose.

Application in impaired renal function: In impaired renal function (creatinine clearance < 10 ml/min) the starting dose is 50% of the starting dose.

– Use in elderly patients and patients with a body weight less than 70 kg In patients over 70 years of age and in patients with a body weight of < 70 kg a smaller dose is used (the first dose is given in the hospital under control of ECG and BP).

Interaction

Propanorm should not be combined with lidocaine because the cardiodepressant effect is increased.

In concomitant use propafenone increases plasma concentrations of propranololol, metoprolol, digoxin (increased risk of glycoside intoxication), indirect anticoagulants, cyclosporine.

In concomitant use propafenone increases the effect of warfarin (by blocking the metabolism).

Concomitant use with beta-adrenoblockers, tricyclic antidepressants and may increase the antiarrhythmic effect.

Concomitant use with local anesthetics increases the risk of CNS damage.

Cimetidine and quinidine, by slowing down the metabolism, increase the plasma concentration of propafenone by 20%, rifampicin decreases it.

In concomitant use with propafenone, amiodarone increases the risk of pirouette tachycardia.

The drugs depressing sinoatrial node and AV node and having negative inotropic effect increase the risk of side effects when used concomitantly with propafenone.

Drugs that inhibit medullary hematopoiesis increase the risk of myelosuppression when used concomitantly with propafenone.

Special Instructions

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

The treatment is recommended to start in a hospital setting because of the increased risk of arrhythmogenic effects associated with the use of propafenone.

Propanorm should be used under monitoring of blood electrolyte balance (especially potassium concentration) and ECG; hepatic transaminase activity should be determined periodically.

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

The indication and dose should be particularly carefully determined for patients with a pacemaker.

Clinical and laboratory monitoring should be performed in patients undergoing long-term treatment with anticoagulants and hypoglycemic agents when Propanorm is used concomitantly.

If sinoatrial blockade or AV blockade of degree III, or recurrent extrasystole are noted during treatment, treatment must be discontinued.

Contraindications

The drug should be prescribed with caution in the following cases:

Side effects

Cardiovascular system disorders: bradycardia, AV dissociation, ventricular tachyarrhythmias, angina pectoris, worsening of heart failure (in patients with reduced left ventricular function), sinoatrial blockade, AV blockade, intraventricular conduction disorders, supraventricular tachyarrhythmias, in high doses – orthostatic hypotension.

Digestive system disorders: change in taste, dry mouth, bitter mouth, nausea, decreased appetite, feeling of heaviness in epigastrium, constipation or diarrhea; rarely – liver function disorders, cholestatic jaundice, cholestasis.

CNS disorders: headache, dizziness; rarely – blurred vision, diplopia, seizures.

Hematopoietic system disorders: leukopenia, agranulocytosis, increased bleeding time, thrombocytopenia, appearance of antinuclear antibodies.

In the sexual system: oligospermia, decreased potency.

Allergic reactions: skin rash, itching, exanthema, skin redness, urticaria, lupus-like syndrome.

Others: weakness, bronchospasm, hemorrhagic rashes on the skin.

Overdose

If a single dose of twice the daily dose is taken, symptoms of intoxication may appear in 1 hour, maximum in a few hours.

Symptoms: Persistent BP decrease, nausea, dry mouth, vomiting, mydriasis, somnolence, extrapyramidal disorders, confusion, bradycardia, QT interval prolongation, intraatrial and intraventricular conduction disorders, ventricular tachyarrhythmias, polymorphic ventricular tachycardia paroxysms, sinoatrial block, AV blockade, asystole, coma, seizures, delirium, pulmonary edema.

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

Pregnancy use

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