Composition
Active ingredients:
propafenone hydrochloride 150 mg
Auxiliary substances:
microcrystalline cellulose – 100.6 mg,
croscarmellose sodium-14 mg,
hypromellose-11.2 mg,
colloidal silicon dioxide-1.4 mg,
magnesium stearate-2.8 mg.
Composition of the film shell: Â
opadray II white film coating: (polyvinyl alcohol 46.9%, macrogol 4000-23.6%, talc-17.4%, titanium dioxide-12.1%) – 10 mg
Pharmacological action
Propafenone is an Ic class antiarrhythmic drug that blocks Na+channels. It has a direct membrane-stabilizing effect on myocardiocytes.
Reduces the maximum depolarization rate of phase 0 of the action potential and its amplitude in Purkinje fibers and ventricular contractile fibers, inhibits automatism. Slows down the flow of Purkinje fibers. Lengthens the time spent on the SA node and atria. It does not affect or slightly increases the corrected recovery time of sinus node function during programmed electrical stimulation.
Increases the effective refractory period of the AV node, inhibits conduction along additional pathways in the retrograde and antegrade directions, and increases the threshold for ventricular stimulation. Electrophysiological effects are more pronounced in the ischemic than in the normal myocardium.
It has a weak beta-adrenoblocking (corresponding to approximately 1/40 of the activity of propranolol) and m-holinoblocking effect. It has a negative inotropic effect, which usually manifests itself when the LV ejection fraction decreases by less than 40%.
It has a local anaesthetic activity that approximately corresponds to the activity of procaine. The action begins 1 hour after ingestion, reaches a peak in 2-3 hours and lasts 8-12 hours.
Indications
Supraventricular and ventricular extrasystoles, paroxysmal rhythm disturbances, including atrial fibrillation and flutter, WPW-syndrome, atrioventricular re-entry tachycardia (treatment and prevention); stable monomorphic ventricular tachycardia (prevention).
Contraindications
Hypersensitivity, grade II-III AV block (without pacemaker), intraventricular bifascicular block (without pacemaker), cardiogenic shock, sinus bradycardia, CHF, SSR, lactation period.
Side effects
From the cardiovascular system:  bradycardia, AV dissociation, ventricular tachyarrhythmias, angina pectoris, worsening of heart failure (in patients with reduced left ventricular function), SA and AV block, intraventricular conduction disorders, supraventricular tachyarrhythmias; when taken in high doses —orthostatic hypotension.
From the digestive system: Â changes in taste, dry and bitter mouth, nausea, decreased appetite, heaviness in the epigastrium, constipation or diarrhea; rarely-liver function disorders, cholestasis, cholestatic jaundice.
From the central nervous system: Â headache, dizziness; rarely-blurred vision, diplopia, convulsions.
From the side of laboratory parameters: Â leukopenia, thrombocytopenia, agranulocytosis, increased bleeding time, the appearance of antinuclear antibodies.
Allergic reactions: Â skin rash, pruritus, exanthema, redness of the skin, urticaria, lupus-like syndrome.
Other services: Â weakness, bronchospasm, hemorrhagic skin rashes.
Interaction
Increases plasma concentrations of propranolol, metoprolol, digoxin (increases the risk of glycoside intoxication), indirect anticoagulants, cyclosporine.
Increases the effect of warfarin (blocks metabolism). When used concomitantly with beta-blockers and tricyclic antidepressants, the antiarrhythmic effect may increase, while local anesthetics may increase the risk of CNS damage.
Cimetidine and quinidine, slowing down the metabolism, increase the concentration of propafenone in plasma by 20%, rifampicin – reduces.
Amiodarone increases the risk of developing pirouette-type tachycardia. Drugs that depress the SA and AV nodes and have a negative inotropic effect increase the risk of side effects.
Drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.
How to take, course of use and dosage
Propafenone is taken orally, after a meal (tablets should be swallowed whole, washed down with a small amount of water).
The dosage regimen is set individually and adjusted by the doctor: 150 mg every 8 hours (450 mg per day).
The dose is increased gradually, every 3-4 days, up to 600 mg per day in 2 divided doses or up to 900 mg per day in 3 divided doses.
Special instructions
Treatment should be initiated in a hospital setting, as there is an increased risk of arrhythmogenic effects associated with propafenone use. It is recommended that previous antiarrhythmic therapy be discontinued before starting propafenone treatment in terms equal to 2-5 T1 / 2 of these drugs.
Treatment should be carried out under the control of electrolyte balance (especially K+ concentration) and ECG; periodically determine the activity of transaminases, antinuclear antibodies. In the treatment of ventricular arrhythmias, propafenone is more effective than class Ia and class Ib antiarrhythmic drugs. In case of induced rhythm disturbances, an intracardiac electrophysiological study is performed no earlier than 5-7 days after the start of use.
With ventricular extrasystole, the general rule is to reduce the number of extrasystoles by 70% from the initial one, according to daily Holter monitoring. During the treatment period, care should be taken when driving vehicles and doing other activities. potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Tablet Form of production
Storage conditions
In a dark place, at a temperature of 15-25 °C
Shelf life
3 years
Active ingredient
Propafenone
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For adults as directed by your doctor
Indications
Arrhythmia
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