Propanorm tabs 150mg #50

User manual for Propanorm pills

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Composition

1 tablet may include 150 mg or 300 mg of propafenone hydrochloride.
In addition: sodium lauryl sulfate, microcrystalline granular cellulose, copovidone, corn starch, croscarmellose sodium, hypromellose 5, magnesium stearate, macrogol 6000, dimethicone emulsion with silicon dioxide, titanium dioxide.

Form of issue

The medicine Propanorm is made in the form of tablets of 10 pieces in a blister № 5 in a cardboard package (50 tablets).

pharmachologic effect

Antiarrhythmic.

Pharmacodynamics and pharmacokinetics

Medication Propanorm refers to a group of antiarrhythmic drugs class Ic, which are blockers of fast sodium channels. It is characterized by m-cholinoblocking activity and weak β-adrenergic blocking efficiency, approximately corresponding to 1/40 of the effects of propranolol. The antiarrhythmic efficacy of the drug is based on direct membrane-stabilizing and local anesthetic action against myocarditis, as well as calcium channel blocking and adrenergic β-adrenergic receptors. The local anesthetic effect is approximately equal to the action of procaine.
The mechanism of action of propafenone is based on its ability to block fast sodium channels, resulting in the inhibition of automatism, a dose-dependent reduction in the rate of depolarization, suppression of the 0 phase of the action potential and its amplitude in the contractile ventricular fibers and Purkinje fibers. The drug inhibits the impulse on the Purkinje fibers and increases the time of the impulse to the atria and the sinoatrial node. When taking propaphenone on the ECG, the PQ interval is extended and the QRS complex is enlarged (from 15 to 25), and the histogram shows an increase in the HV and AN intervals. The inhibition of the processes of impulse conduction leads to an elongation of the effective refractory period in the AV node, atria, additional beams, and also to a lesser extent in the ventricles. The drug did not reveal any significant effect of propafenone on the QT-interval. Electrophysiological effects are more pronounced in ischemic myocardium. This preparation also has a negative inotropic effect, usually manifested when the fraction of ejection of blood from the left ventricle is reduced to 40% and lower.
Effects of the drug are observed after 60 minutes after its oral administration, reach a maximum after 2-3 hours and last for 8-12 hours.
The absorption of the orally ingested propafenone passes by more than 95%. The degree of bioavailability of the drug increases non-linearly with an increase in a single dose, from 5% with 150 mg to 12% with 300 mg and 40-50% with 450 mg. Plasma Cmax is 500-1500 μg / l and is observed after 1-3.5 hours.
Binding to plasma proteins and proteins of internal organs is at the level of 85-97%. Vd is 3-4 l / kg. Permeability through blood-brain and placental barriers is rather low.
Metabolic transformations of propafenone occur almost in full. There are 11 products of drug metabolism, of which only 2 are pharmacologically active and have antiarrhythmic efficacy comparable with propafenone (N-depropylpropaphenone and 5-hydroxypropaphenone). Oxidative metabolism is determined by specific cytochrome, the activity of which is determined genetically. The therapeutic range of plasma content of propafenone is 0.5-2 mg / l.
In patients with a characteristic intensive metabolism T1 / 2 of the drug takes 2-10 hours, in patients with delayed metabolism - 10-32 hours. Excretion in the form of metabolic products is carried out with urine by 38% (less than 1% of propafenone is excreted in its original form), and also with bile by 53% (in the form of sulfates and glucuronides).
If liver function is insufficient, there is a decrease in the time of excretion of the drug.

Indications for use

Appointment Propanorm is indicated for the purpose of prophylaxis and therapy of the following painful conditions associated with the functioning of the heart muscle:
    ventricular and supraventricular extrasystoles;
    atrial-ventricular tachycardia re-entry;
    paroxysmal heart rhythm disorders (WPW syndrome, flutter and atrial fibrillation - supraventricular);
    monomorphic stable ventricular tachycardia.

Contraindications

It is absolutely counter-indicative to appoint Propanorm with:
    decompensated heart failure;
    myocardial infarction;
    chronic uncontrolled heart failure;
    blockade of the legs of the bundle;
    cardiogenic shock (with the exception of antiarrhythmic shock and arterial hypotension, which developed as a result of tachycardia);
    syndrome of "tachycardia-bradycardia";
    personal hypersensitivity;
    severe bradycardia;
    SSSU;
    AV-blockade of II and III severity (without the use of pacemaker);
    severe arterial hypotension;
    breastfeeding;
    sinoatrial blockade;
    intoxication with digoxin;
    impaired atrial foci;
    bifascicular intraventricular blockade (without using an electrocardiostimulator);
    up to 18 years (due to an undefined degree of safety and efficiency).
Relative contraindications to the reception of Propanorm are:
    COPD;
    hepatic cholestasis;
    myasthenia gravis (including myasthenia gravis);
    presence of an electrocardiostimulator;
    heart failure (with less than 30% of the ejection fraction);
    liver / kidney pathology;
    cardiomyopathy;
    elderly age (70 years and older);
    arterial hypotension;
    electrolyte disorders (require mandatory correction before treatment);
    parallel therapy with the use of other antiarrhythmic drugs with similar effects aimed at the electrophysiology of the heart.

Side effects

Digestive system:
    bitter taste in the mouth;
    change in taste;
    heaviness in epigastrium;
    dry mouth;
    decreased appetite;
    nausea;
    constipation / diarrhea;
    impaired hepatic function;
    cholestasis;
    cholestatic jaundice.
The cardiovascular system:
    worsening of diagnosed heart failure (for patients with reduced functionality of the left ventricle);
    AV blockade;
    bradycardia;
    supraventricular tachyarrhythmias;
    AV dissociation;
    sinoatrial blockade;
    ventricular tachyarrhythmias;
    disorders of intraventricular conduction;
    angina pectoris;
    Orthostatic hypotension (when taking large doses).
Nervous system:
    diplopia;
    headache;
    blurred vision;
    dizziness;
    convulsions.
Hemopoietic system:
    agranulocytosis;
    leukopenia;
    prolonged bleeding time;
    the emergence of antinuclear antibodies;
    thrombocytopenia.
Sexual system:
    deterioration of potency;
    oligospermia.
Allergic manifestations:
    lupus-like syndrome;
    skin rash / itching;
    redness of the skin;
    exanthema;
    hives.
Other:
    cutaneous hemorrhagic eruptions;
    bronchospasm;
    feeling of weakness.

Propanorm, instructions for use (Method and dosage)

Before you buy Propanorm, you should reed the instruction.
Instruction for use Propanorm involves the setting of a dosage regimen of therapy on an individual basis and its adjustment by a physician at the entire stage of treatment. Tablets of the drug should be taken after meals in a general form (without chewing and not crushing) and wash down with a small amount of water.
Originally prescribed Propanorm in a daily dose of 450 mg. Tablets take three times a day for 150 mg every 8 hours. Then follows a gradual (3-4 days) increase in daily dosage to 600 mg in two divided doses (morning and evening). Maximum of 24 hours allowed to take 900 mg of propafenone in 3 divided doses.
Extension of the QRS complex or QT interval by more than 20% compared to the baseline, an increase in the PQ interval by more than 50%, a QT interval of more than 500 msec, and an increase in the severity and frequency of the arrhythmia, require reduced dosage or temporary discontinuation of therapy.
Elderly patients (over 70 years of age) and patients weighing less than 70 kg need the initial appointment of smaller dosages of Propanorm, with mandatory first-dose administration in a hospital under the control of blood pressure and ECG.
If there is a violation of the hepatic function, due to the possible accumulation of propafenone, Propanorm dosages equal to 20-30% of the usually recommended doses are used.
If there is a violation of renal function (CC less than 10 ml / min), reduce the initial dose by 50%.

Overdose

In the case of a single dose of propafenone twice the recommended daily dosage, negative symptoms of intoxication may appear after 60 minutes, maximum for several hours.
For the state of intoxication with an overdose of propafenone, the following conditions are characteristic: stable decrease in blood pressure, extrapyramidal disorders, nausea / vomiting, mydriasis, dry mouth, drowsiness, bradycardia, confusion, AV blockade, QT interval prolongation, ventricular tachyarrhythmia, intraventricular and atrial conduction, paroxysm of ventricular polymorphic tachycardia, asystole, sinoatrial block, coma, delirium, convulsions, pulmonary edema.
Treatment of overdose, depending on their severity, may require the purification of the digestive tract, the introduction of Diazepam and Dobutamine, the conduct of indirect heart massage and defibrillation, the transfer of the patient to the ventilator.

Interaction

Because of the intensification of cardiodepressive action, the combination of propafenone with lidocaine should be avoided.
Parallel reception of propafenone and Warfarin enhances the effect of the latter (due to the blocking of metabolism).
At the same time, propafenone taken is able to increase plasma concentrations of metoprolol, propranolol and digoxin (thereby increasing the possibility of glycosidic intoxication), as well as Cyclosporine and indirect anticoagulants.
A combination of appointment with tricyclic antidepressants or beta-blockers can lead to an increase in antiarrhythmic action.
Rifampicin lowers the plasma concentration of propafenone.
Quinidine and cimetidine slow the metabolism and increase the serum content of propafenone by 20%.
Simultaneous use of local anesthetics increases the possibility of CNS damage.
In parallel, Amiodarone therapy increases the risk of tachycardia such as pirouette.
The joint administration of propafenone with therapeutic agents that suppress bone marrow hematopoiesis can cause myelosuppression.
The possibility of formation of side effects associated with propafenone increases with combined intake of drugs of the oppressive AV node and sinoatrial node and characterized by a negative inotropic effect.

Storage conditions

Propanorm tablets should be stored in a temperature range of 15-25 ° C.
Shelf life - 3 years from the date of issue.

special instructions

Throughout the therapeutic course of taking Propanorm, especially at the beginning of treatment, ECG monitoring should be performed.
In connection with the increased risk of arrhythmogenic effects associated with the action of propafenone, therapy is recommended to begin in the hospital.
Therapy with reception of Propanorm should be performed under the control of electrolyte blood balance (especially the level of potassium) and periodic studies of hepatic transaminase activity.
The presence of the pacemaker in the patient requires a particularly cautious approach to determining the indications for the use of Propanorm and the choice of its dosage regimen.
Regarding the treatment of cardiac rhythm disorders of ventricular etiology, propafenone is more effective than antiarrhythmic drugs of classes IA and IB.
Bioavailability of propafenone in patients with hepatic function deficiency increases by 70%, which requires lowering the doses of the drug and conducting regular monitoring of laboratory parameters.
Patients undergoing prolonged therapy using Propanorm and concurrently taking hypoglycemic drugs or anticoagulants need to be clinically and laboratory monitored.
Frequent extrasystole, AV-blockade III degree or sinoatrial blockade, observed in the patient during the treatment, is the reason for discontinuing therapy.
Given the likelihood of proaritmogenic exposure to propafenone, the drug Propanorm is recommended for use solely for its intended use and under medical supervision.
During the period of taking Propanorm, the patient is advised to refrain from potentially life-threatening activities, including driving motor vehicles.

Children

Patients in the age group under 18 years of age are not allowed to take Propanorm.

With alcohol

The combination of Propanorm and alcohol, taking into account the effects of the drug and the painful conditions in which its purpose is indicated, can lead to serious negative consequences, therefore, during the treatment, alcohol must be excluded.

In pregnancy and lactation

Appointment Propanorm for pregnant women, especially in the I trimester, is allowed only if the benefit of such therapy is significantly exceeded in comparison with the possible negative consequences for the fetus.
Nursing women Propanorm prescribed contraindicated.

Reviews about Propanorm

Reviews about Propanorm position it as a fairly effective and relatively safe remedy, most often completely coping with its purpose in case of application strictly according to indications. Naturally, you can not prescribe this drug yourself. Therapy with its use should be carried out exclusively under the supervision of a physician with an individual selection of the dosage regimen and taking into account all the features of the patient's state of health.