Propanorm

General characteristics. Structure:

Active agent: propafenona hydrochloride of 150 mg / 300 mg

Other ingredients: the cellulose microcrystallic granulated starch corn, коповидон, sodium of a kroskarmelloz, magnesium stearate, sodium lauryl sulfate, a gipromelloza 5, polyethyleneglycol 6000, titanium dioxide, an emulsion of a simetikon from silicon dioxide.

Pharmacological properties:

Propafenona a hydrochloride (1-[2-[2-hydroxy-3-propilamino) propoks] phenyl] - 3-phenyl-1-пропанон a hydrochloride) — the antiarrhytmic drug Ic of a class with moderately expressed β-adrenoceptor blocking effect. Has direct membranostabilizuyushchy effect on cardiomyocytes, oppresses bystry natrium channels, reduces the maximum speed of depolarization of cardiomyocytes and their excitability. Slows down carrying out an impulse in auricles, an AV node, especially in system of a ventriculonector and Purkinye's fibers. Propafenon increases an interval of PR and QRS is insignificant. In the presence of additional ways of carrying out increases their refractory period and completely blocks carrying out excitement as in the antegrade, and retrograde direction. Drug increases the effective refractory period of an AV node and ventricles.
Absorption at intake almost full (95%). Cmax in a blood plasma is reached in 2–3 h Propanorm shows dozozavisimy bioavailability. Almost completely (85–97%) contacts proteins of a blood plasma and internals (a liver, lungs, etc.). Is exposed to biotransformation in a liver by means of system of P450 cytochrome which activity is determined genetically. There are 2 main phenotypes — at most (90%) of people biotransformation happens quickly to formation of active metabolites (5-gidroksipropafenon, N-depropilpropafenon, etc.). T½ at such patients makes 2–10 h (on average — 5,5 h). At a phenotype of slow metabolism the effect of primary passing through a liver is considerably less expressed, T½ makes 10–32 h (on average — 17,2 h). The effect develops approximately in 1 h after intake, reaches the maximum expressiveness in 2–3 h and lasts 8–12 h. Range of therapeutic concentration of a propafenon in a blood plasma makes 0,5–2 mg/l.
With urine in the form of metabolites about 10% of drug are excreted, бóльшая a part (87%) of a dose is removed with bile (in a look пропафенон glucuronides and sulfates).

Indications to use:

The prevention and elimination of arrhythmias — all types of supraventricular and ventricular premature ventricular contraction, fibrillation of auricles, a supraventricular tachyarrhythmia, including at patients with additional ways are carrying out excitement (WPW of cm, Klerk's syndrome — Levi — Kristesko).

Route of administration and doses:

To adults the dose and frequency rate of reception are established individually and korrigirut under control of the ABP and ECG level. At increase in duration of the QRS complex and interval of Q-t by more than 20% of a reference value it is necessary to lower a dose or to temporarily cancel drug before normalization of indicators. The therapeutic dose for patients with the body weight of 70 kg makes 450–600 mg/days (on 150 mg 3 times a day or on 300 mg 2 times a day). The maximum daily dose — 900 mg. To patients with smaller body weight respectively reduce a dose.
Drug is taken after food, a pill is swallowed without chewing, washing down with enough water.

Features of use:

With extra care apply at patients with the implanted electrocardiostimulator. In an initiation of treatment Propanormom is necessary constant ECG control.
The ratio advantage/risk should be weighed at patients with AV blockade of the I degree, severe forms of an obstructive bronchopulmonary disease, OH, of an electrolytic imbalance, a hepatic unsufficiency, a myasthenia гравис. At patients with a hepatic unsufficiency biological availability of a propafenon increases by 70% therefore such patients should lower a dose and to constantly carry out monitoring of laboratory parameters. At patients who it is long are treated by anticoagulants and antidiabetic means, carrying out clinical and laboratory control is required. It is necessary to apply with care at patients with a myocardial infarction in the anamnesis and not to appoint in the first 3 months after an acute myocardial infarction. If during therapy there is a sinoauricular block or AV blockade of heavy degree, or premature ventricular contraction (frequent or polymorphic), treatment by Propanorm needs to be stopped.
There is no clinical experience of use of drug for children.
During treatment by drug it is necessary to avoid control of vehicles and the performance of work requiring special attention and speed of psychomotor reactions. In need of surgical intervention it is necessary to take into account that administration of local anesthetics can strengthen action of a propafenon. It is not recommended to use drug during feeding by a breast. Also it is not recommended to children to accept aged up to 15 years.

Side effects:

At Propanorm's reception in a high dose there can be anorexia, feeling of overflow of a stomach, nausea, vomiting, taste disturbance, dryness in a mouth, in isolated cases — dizziness, a headache, weakness, decrease in visual acuity, a sleep disorder, extrapyramidal disturbances, a coma, confusion of consciousness, memory loss. Sometimes note allergic reactions.
Patients of advanced age can have orthostatic reactions, sometimes — bradycardia, disturbance of conductivity of an AV node (AV blockade, increase in the QRS complex), ventricular premature ventricular contraction and tachycardia, an atrial flutter, AV dissociation, weakness of a sinus node, a cardiac standstill; stenocardia attacks, can arise or amplify symptoms of heart failure. Extremely seldom note a cholestasia, decrease in a potentiality, anemia, hemorrhagic rash, a neutropenia, increase in a bleeding time, a leukopenia, thrombocytopenia. The composition of peripheral blood is normalized after drug withdrawal.

Interaction with other medicines:

At simultaneous use of local anesthetics, and also the drugs reducing ChSS and contractility of a myocardium (blockers of β-adrenoceptors, tricyclic antidepressants), it is necessary to consider a possibility of mutual strengthening of cardiodepressive action.
The concomitant use of a ritonavir increases the frequency of by-effects of Propanorm. The combined use with other antiarrhytmic means is undesirable.
Cases of increase in concentration of propranolol, metoprolol in a blood plasma at simultaneous use of a propafenon are described. Quinidine promotes increase in plasma level of a propafenon at decrease in level of its main metabolite of a 5-gidroksipropafenon.
There are messages on increase in level of a propafenon in a blood plasma at its simultaneous use with Cimetidinum, increase in a prothrombin time at the combined use with indirect anticoagulants. Propanorm increases concentration in a blood plasma of cyclosporine, digoxin (the risk of development of glikozidny intoxication increases), and also theophylline and diltiazem. Exponentiates effect of warfarin, braking its biotransformation. Rifampicin reduces Propanorm's action.

Contraindications:

Hypersensitivity to a propafenon, cardiogenic shock (except the shock caused by arrhythmia), heart failure, a sinus bradycardia (ChSS <50 уд. / mines), weakness of a sinus node, arterial hypotension (the ABP <100/70 mm of mercury.), conductivity disturbance (sinuatrial, AV blockade of the II-III degree, blockade of legs of a ventriculonector), a myasthenia, the expressed electrolytic imbalance, a bronchospasm, a serious obstructive illness of lungs, an abnormal liver function and kidneys, the period of pregnancy and feeding by a breast (пропафенон gets into breast milk), in the first 3 months after an acute myocardial infarction, and also to patients with reduced cordial emission (except patients with atrial arrhythmia, life-threatening).

Overdose:

It can be shown by anorexia, feeling of overflow of a stomach, nausea, vomiting, disturbance of flavoring sensitivity, a headache, decrease in visual acuity, extrapyramidal disturbances, a coma, confusion of consciousness, amnesia. There can be orthostatic reactions, bradycardia, disturbance of conductivity of an AV node (AV blockade, increase in the QRS complex), ventricular tachycardia, an atrial flutter, AV dissociation, weakness of a sinus node, a cardiac standstill; symptoms of heart failure can arise and amplify, develop spasms. At emergence of symptoms of overdose reduce a dose or cancel drug.
Treatment: in/in enter sodium a lactate and potassium chloride. Sometimes there is a need for introduction of a glucagon, Epinephrinum and cardiostimulation use.

Storage conditions:

In internal packaging and a box at a temperature of 15-25 °C.

Issue conditions:

According to the recipe

Packaging:

The tab. п / about 150 mg, No. 50.
The tab. п / about 300 mg, No. 50.