Propanorm

Пропанорм Drug photo

The description is actual on 13.05.2016

  • Latin name: Propanorm
  • ATH code: C01BC03
  • Active ingredient: Propafenon (Propafenone)
  • Producer: HBM Pharma s.r.o. (Slovak Republic), PRO.MED.CS Praha a.s. (Czech Republic)

Structure

1 tablet can include 150 mg or 300 mg of a propafenon of a hydrochloride.

In addition: sodium lauryl sulfate, the microcrystallic granulated cellulose, kopovidon, corn starch, croscarmellose sodium, a gipromelloza 5, magnesium stearate, a macrogoal 6000, an emulsion of a dimetikon with silicon dioxide, titanium dioxide.

Release form

Medicine Propanorm is made in the form of tablets on 10 pieces in the blister No. 5 in cardboard packaging (50 tablets).

Pharmacological action

Antiarrhythmic.

Pharmacodynamics and pharmacokinetics

Medicine Propanorm belongs to group of the antiarrhytmic drugs of the class IC which are locks of fast natrium channels. The m-holinoblokiruyushchey by the activity and weak β-adrenoceptor blocking efficiency approximately corresponding 1/40 from effects of propranolol is characterized. Antiarrhythmic efficiency of drug is based on direct membranostabiliziruyushchy and mestnoanesteziruyushchy action concerning cardiomyocytes, and also on blocking of calcium channels and adrenergic β-adrenoceptors.......... The Mestnoanesteziruyushchy effect is approximately equal to action of Procainum.

The mechanism of action of a propafenon is based on its ability to blocking of fast natrium channels owing to what there is an automatism oppression, dozozavisimy reduction of speed of depolarization, suppression 0 phases of action potential and its amplitude in sokratitelny ventricular fibers and Purkinye's fibers. Drug slows down carrying out an impulse on Purkinye's fibers and increases time of carrying out an impulse on auricles and a sinuatrial node. At reception of a propafenon on an ECG lengthening of a PQ interval and expansion of a QRS complex (from 15 to 25) is observed, and on the histogram increase in intervals of HV and AN is noted. Braking of processes of carrying out an impulse leads to lengthening of the effective refractory period in an AV node, auricles, additional bunches, and also in a smaller measure in ventricles. Administration of drug did not reveal any significant influence of a propafenon on a QT interval. Electrophysiologic effects are to a large extent shown in an ischemic myocardium. Negative inotropic impact, as a rule, shown at reduction of fraction of emission of blood from a left ventricle to 40% and below is also characteristic of this drug.

Effects of drug are observed in 60 minutes after its oral administration, reach a maximum after 2-3 hours and last for 8-12 hours.

Absorption of orally accepted propafenon takes place more than for 95%. Degree of bioavailability of drug increases not linearly with increase of a one-time dosage, from 5% at reception of 150 mg to 12% at reception of 300 mg and to 40-50% at reception of 450 mg. Plasma Cmax equals 500-1500 mkg/l and is noted in 1-3,5 hours.

Linkng with plasma proteins and proteins of internals is at the level of 85-97%. Vd makes 3-4 l/kg. Permeability through hematoencephalic and placental barriers quite low.

Metabolic transformations of a propafenon happen almost in full. There are 11 products of a metabolism of drug from which only 2 pharmacological are active and possess comparable with propafenony antiarrhythmic efficiency (N-depropilpropafenon and 5-gidroksipropafenon). The oxidizing metabolism is defined by specific cytochrome which activity is determined genetically. Therapeutic range of plasma maintenance of a propafenon makes 0,5-2 mg/l.

With a characteristic intensive metabolism of T1/2 of drug takes 2-10 hours patients, patients with the slowed-down metabolism have 10-32 hours. Excretion in the form of products of a metabolism is carried out with urine for 38% (less than 1% of a propafenon are brought in an initial look), and also with bile to 53% (in the form of sulfates and glucuronides).

At insufficiency of hepatic function decrease in time of removal of drug is observed.

Indications to use

Propanorm's appointment is shown for the purpose of carrying out prevention and therapy of the following painful states, work-related a cardiac muscle:

  • ventricular and supraventricular ekstrasistoliya;
  • atrioventricular tachycardia of re-entry;
  • paroxysmal frustration of a cordial rhythm (WPW syndrome, trembling and fibrillation of auricles – supraventricular);
  • monomorphic steady ventricular tachycardia.

Contraindications

It is absolutely contraindicated to appoint Propanorm at:

  • dekompensirovanny heart failure;
  • myocardial infarction;
  • chronic uncontrollable heart failure;
  • to blockade of legs of a ventriculonector;
  • cardiogenic shock (except for antiarrhytmic shock and the arterial hypotension which developed owing to tachycardia);
  • syndrome of "tachycardia bradycardia";
  • personal hypersensitivity;
  • the expressed bradycardia;
  • SSSU;
  • To AV blockade II and III severity (without use of an electrocardiostimulator);
  • the expressed arterial hypotonia;
  • feeding by a breast;
  • to sinuatrial blockade;
  • intoxications digoxin;
  • the broken intra atrial carrying out;
  • to bifastsikulyarny intra ventricular blockade (without use of an electrocardiostimulator);
  • till 18 years (because of unspecified degree of safety and efficiency).

Relative contraindications to Propanorm's reception are:

  • HOBL;
  • hepatic cholestasia;
  • myasthenia (including gravis myasthenia);
  • existence of an electrocardiostimulator;
  • heart failure (at less than 30% of fraction of emission);
  • pathologies of livers/kidneys;
  • cardiomyopathy;
  • advanced age (70 years are also more senior);
  • arterial hypotension;
  • electrolytic disturbances (demand obligatory adjustment prior to treatment);
  • parallel therapy using other antiarrhytmic remedies with the similar effects directed to a heart electrophysiology.

Side effects

Alimentary system:

  • bitterness in a mouth;
  • taste change;
  • weight in epigastriums;
  • dryness in a mouth;
  • loss of appetite;
  • nausea;
  • lock/diarrhea;
  • disturbance of hepatic function;
  • cholestasia;
  • cholestatic jaundice.

Cardiovascular system:

  • deterioration in the diagnosed heart failure (concerning patients with reduced functionality of a left ventricle);
  • AV blockade;
  • bradycardia;
  • supraventricular tachyarrhythmias;
  • AV dissociation;
  • sinuatrial blockade;
  • ventricular tachyarrhythmias;
  • disorders of intra ventricular conductivity;
  • stenocardia;
  • orthostatic hypotension (at reception of big dosages).

Nervous system:

Hemopoietic system:

Reproductive system:

Allergic manifestations:

  • volchanochnopodobny syndrome;
  • skin rash / itch;
  • reddening of integuments;
  • dieback;
  • small tortoiseshell.

Others:

  • skin hemorrhagic rashes;
  • bronchospasm;
  • feeling of weakness.

Propanorm, application instruction (Way and dosage)

The application instruction of Propanorm assumes installation of the dosing mode of therapy in an individual order and its adjustment by the doctor at all stage of carrying out treatment. A pill of drug needs to be taken after food in the whole look (without chewing and without making small) and to wash down with the small volume of water.

Initially appoint Propanorm in a daily dose 450 mg. A pill is taken three times a day on 150 mg by each 8 hours. Then increase of a daily dosage to 600 mg in two steps follows gradual (3-4 days) (in the morning and in the evening). As much as possible in 24 hours allow reception of 900 mg of a propafenon in 3 receptions.

Expansion against the carried-out treatment of a QRS complex or a QT interval is more than for 20% in comparison with basic data, increase in a PQ interval is more than for 50%, it is more QT interval than on 500 ms, and also increase of weight and frequency of arrhythmia, demand decrease in dosages or the temporary termination of therapy.

Elderly patients (is more senior than 70 years) and patients weighing less than 70 kilograms need initial purpose of smaller dosages of Propanorm, with obligatory reception of the first dose in a hospital under control of the ABP and an ECG.

At disturbance of hepatic function, because of possible cumulation of a propafenon, equal 20-30% of usually recommended doses apply Propanorm's dosages.

At disturbance of renal function (KK less than 10 ml/min.) lower an initial dose by 50%.

Overdose

In case of one-time reception of a dose of a propafenon twice exceeding the recommended daily dosages, the negative symptomatology of intoxication can appear in 60 minutes, at most for several hours.

For a condition of intoxication at overdose propafenony the following states are characteristic: steady decrease in the ABP, extrapyramidal frustration, nausea/vomiting, a mydriasis, dryness in a mouth, drowsiness, bradycardia, confusion of consciousness, AV blockade, lengthening of a QT interval, a ventricular tachyarrhythmia, disturbance intra ventricular and intra-atrial conduction, a paroxysm of ventricular polymorphic tachycardia, an asystolia, sinuatrial blockade, a coma, a delirium, spasms, a fluid lungs.

Treatment of the phenomena of overdose, depending on their expressiveness, can demand cleaning of a gastrointestinal tract, administration of Diazepam and Dobutaminum, carrying out an indirect cardiac massage and defibrillation, transfer of the patient into IVL.

Interaction

Because of strengthening of cardiodepressive action it is necessary to avoid a combination of a propafenon with Lidocaine.

Parallel reception of a propafenon and Warfarin strengthens action of the last (due to blocking of a metabolism).

At the same time accepted propafenon it is capable to increase plasma concentration of Metoprolol, Propranolol and Digoxin (thereby strengthening a possibility of glikozidny intoxication), and also Cyclosporine and indirect anticoagulants.

The combined appointment with tricyclic antidepressants or beta adrenoblockers can lead to increase in antiarrhytmic action.

Rifampicin reduces plasma concentration of a propafenon.

Quinidine and Cimetidinum slow down a metabolism and increase the serumal maintenance of a propafenon by 20%.

Simultaneous use of local anesthetics strengthens a possibility of defeat of TsNS.

In parallel the carried-out therapy by Amiodaronum increases risk of forming of tachycardia like "pirouette".

Joint reception of a propafenon with the remedies suppressing a marrowy hemopoiesis can become the miyelosupressiya reason.

The possibility of forming of the side effects inherent in a propafenon increases at the combined administration of drugs oppressing an AV node and a sinuatrial node and characterized by negative inotropic effect.

Terms of sale

Propanorm is released from drugstores at presentation of the recipe.

Storage conditions

Propanorm's tablets should be stored in range of temperatures of 15-25 °C.

Period of validity

3 years from the moment of release.

Special instructions

Throughout a therapeutic course of reception of Propanorm, especially in an initiation of treatment, it is necessary to carry out ECG monitoring.

Due to the increased risk of the aritmogenny effects connected by action of a propafenon, therapy is recommended to begin in a hospital.

Therapy with Propanorm's reception needs to be carried out under control of electrolytic blood balance (in particular potassium level) and periodic researches of activity of hepatic transaminases.

Presence demands especially careful approach to definition of indications to Propanorm's use and the choice of its dosing mode from the patient of an electrocardiostimulator.

Concerning treatment of disturbances of a cordial rhythm of a ventricular etiology propafenon is more effective, than antiarrhytmic medicines of the classes IA and IB.

Bioavailability of a propafenon at patients with insufficiency of hepatic function increases for 70% that demands decrease in doses of drug and carrying out regular monitoring of laboratory parameters.

The patients passing long therapy using Propanorm and in parallel the accepting hypoglycemic drugs or anticoagulants, need clinical and laboratory supervision.

The frequent ekstrasistoliya, AV blockade of the III degree or sinuatrial blockade observed at the patient during the carried-out treatment is a reason for the therapy termination.

Considering probability of proaritmogenny influence of a propafenon, drug Propanorm recommend to use exclusively to destination and under medical control.

During Propanorm's reception to the patient recommend to abstain from potentially life-threatening types of activity, including driving of motor transport.

Propanorm's analogs

Coincidence on the ATH code of the 4th level:

Propanorm's analogs including identical active ingredient are provided by drugs: Propafenon, Ritmokard and Ritmonorm.

Zdravzona

  • Propanorm of 150 mg No. 50 tabletkipro.med.cs Praha
  • Propanorm of 300 mg No. 50 tabletkipro.med.cs Praha
  • Propanorm 3,5mg/ml solution for injections of 10 ml No. 10 ampulypro.med.cs Praha

Drugstore of IFC

  • Propanorm tbl p/pl/o 150 mg No. 50, Pro.Med.CS Prahachekhiya
  • Propanorm tbl 300 mg No. 50, Pro.Med.CS Prahachekhiya
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Apteka24

  • Propanormpro.Med.Cs Praha (Czech Republic)
  • Propanorm of a tablet 150 of mg No. 50promed of Farm (Czech Republic)
  • Propanormka)

Paniapteka

  • Propanorm of the tab. of 150 mg No. 50promed of Farm
  • Propanorm of the tab. of 150 mg No. 50promed of Farm

BIOSPHERE

  • Propanorm of 300 mg No. 50 tabl.p.o.pro.med.cs Praha a.s. (Czech Republic)
  • Propanorm of 150 mg No. 50 tabl.p.o.pro.med.cs Praha a.s. (Czech Republic)
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Section: Cardiological Cardiovascular
in more detail

Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Propanorm surely consult with the attending physician.