Propafenone hydrochloride (1- [2- [2-hydroxy-3-propylamino) propoxy] phenyl] -3-phenyl-1-propanone hydrochloride) is a class ic antiarrhythmic preparation with a moderate β-adrenergic blocking effect. has a direct membrane-stabilizing effect on myocardiocytes, inhibits fast sodium channels, reduces the maximum rate of depolarization of myocardiocytes and their excitability. slows down the conduction of the impulse in the atria, av-node, especially in the system of the bundle of his and Purkinje fibers. propafenone increases the p – r interval and slightly qrs. in the presence of additional conduction pathways, it increases their refractory period and completely blocks the conduction of excitation both in the antegrade and retrograde directions. the preparation increases the effective refractory period of the av-node and ventricles.
Oral absorption is almost complete (95%). Cmax in blood plasma is reached after 2-3 hours. Propanorm exhibits dose-dependent bioavailability. Almost completely (85–97%) binds to proteins of blood plasma and internal organs (liver, lungs, etc.). It undergoes biotransformation in the liver using the cytochrome P450 system, the activity of which is genetically determined. There are 2 main phenotypes - in most (90%) people, biotransformation occurs rapidly with the formation of active metabolites (5-hydroxypropafenone, N-depropylpropafenone, etc.). T½ in such patients is 2-10 hours (on average - 5.5 hours). In the phenotype of slow metabolism, the effect of primary passage through the liver is much less pronounced, T½ is 10–32 hours (on average, 17.2 hours). The effect develops approximately 1 hour after oral administration, reaches its maximum in 2-3 hours and lasts 8-12 hours. The range of therapeutic concentrations of propafenone in blood plasma is 0.5-2 mg / l.
About 10% of the preparation is excreted in the urine in the form of metabolites, the greater part (87%) of the dose is excreted in the bile (in the form of propafenone glucuronides and sulfates).
Prevention and elimination of arrhythmias - all types of supraventricular and ventricular extrasystoles, atrial fibrillation, supraventricular tachyarrhythmias, including in patients with additional pathways of excitation (wpw c-m, clerk's syndrome - levi - cristesco).
For adults, the dose and frequency of administration are set individually and corrected under the control of the level of blood pressure and ecg. with an increase in the duration of the qrs complex and the q – t interval by more than 20% of the initial value, it is necessary to reduce the dose or temporarily cancel the preparation until the indicators normalize. the therapeutic dose for patients weighing 70 kg is 450-600 mg / day (150 mg 3 times a day or 300 mg 2 times a day). the maximum daily dose is 900 mg. for patients with less body weight, the dose is reduced accordingly.
The preparation is taken after meals, the tablets are swallowed without chewing, drinking plenty of water.
Hypersensitivity to propafenone, cardiogenic shock (except shock caused by arrhythmia), heart failure, sinus bradycardia (heart rate 50 beats / min), weakness of the sinus node, arterial hypotension (blood pressure 100/70 mm Hg), conduction disturbance ( sinoatrial, av-blockade II-III degree, bundle branch block), myasthenia gravis, severe electrolyte imbalance, bronchospasm, severe obstructive pulmonary disease, impaired liver and kidney function, pregnancy and lactation (propafenone enters breast milk), in the first 3 months after acute myocardial infarction, as well as in patients with reduced cardiac output (except for patients with life-threatening atrial arrhythmia).
When taking propanorm in a high dose, anorexia, a feeling of stomach fullness, nausea, vomiting, taste disturbances, dry mouth, in rare cases - dizziness, headache, weakness, decreased visual acuity, sleep disturbances, extrapyramidal disturbances, coma, confusion may occur , memory loss. sometimes allergic reactions are noted.
Elderly patients may experience orthostatic reactions, sometimes bradycardia, abnormal conduction of the AV node (AV block, increase in the QRS complex), ventricular premature beats and tachycardia, atrial flutter, AV dissociation, weakness of the sinus node, cardiac arrest; attacks of angina pectoris, symptoms of heart failure may occur or worsen. Cholestasis, decreased potency, anemia, hemorrhagic rash, neutropenia, increased bleeding time, leukopenia, thrombocytopenia are extremely rare. The composition of peripheral blood is normalized after preparation withdrawal.
Use with extreme caution in patients with an implanted pacemaker. at the beginning of treatment with propanorm, constant ECG control is required.
The benefit / risk ratio should be weighed in patients with grade I AV block, severe obstructive bronchopulmonary disease, asthma, electrolyte imbalance, liver failure, myasthenia gravis. In patients with liver failure, the bioavailability of propafenone is increased by 70%, therefore, such patients should reduce the dose and constantly monitor laboratory parameters. In patients who are treated for a long time with anticoagulants and antidiabetic agents, clinical and laboratory control is required. It should be used with caution in patients with a history of myocardial infarction and should not be prescribed in the first 3 months after acute myocardial infarction. If during therapy there is a sinoauricular block or severe AV block, or extrasystole (frequent or polymorphic), treatment with Propanorm should be discontinued.
There is no clinical experience of using the preparation in children.
During treatment with the preparation, you should avoid driving and performing work that requires increased attention and speed of psychomotor reactions. If surgical intervention is necessary, it must be taken into account that the administration of local anesthetics can enhance the effect of propafenone. It is not recommended to use the preparation during breastfeeding. Also not recommended for children under 15 years of age.
With the simultaneous use of local anesthetics, as well as preparations that reduce heart rate and myocardial contractility (β-adrenoreceptor blockers, tricyclic antidepressants), it is necessary to take into account the possibility of mutual enhancement of the cardiodepressant effect.
Concomitant use of ritonavir increases the incidence of side effects of Propanorm. Combined use with other antiarrhythmic preparations is undesirable.
Cases of an increase in the concentration of propranolol, metoprolol in blood plasma with the simultaneous use of propafenone have been described. Quinidine increases the plasma level of propafenone while decreasing the level of its main metabolite, 5-hydroxypropafenone.
There are reports of an increase in the level of propafenone in the blood plasma with its simultaneous use with cimetidine, an increase in prothrombin time when used in combination with indirect anticoagulants. Propanorm increases the plasma concentration of cyclosporine, digoxin (the risk of glycoside intoxication increases), as well as theophylline and diltiazem. Potentiates the effect of warfarin, inhibiting its biotransformation. Rifampicin reduces the action of Propanorm.
It can manifest itself as anorexia, a feeling of fullness in the stomach, nausea, vomiting, impaired taste sensitivity, headache, decreased visual acuity, extrapyramidal disturbances, coma, confusion, amnesia. orthostatic reactions, bradycardia, abnormal conduction of the av-node (av-blockade, increase in the qrs complex), ventricular tachycardia, atrial flutter, av-dissociation, weakness of the sinus node, cardiac arrest may occur; symptoms of heart failure may occur and intensify, convulsions may develop. if symptoms of an overdose appear, reduce the dose or discontinue the preparation.
Treatment: sodium lactate and potassium chloride are injected intravenously. Sometimes there is a need for the introduction of glucagon, epinephrine and the use of pacing.
In an inner package and a box at a temperature of 15-25 ° C.
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