Propafenone
Propafenone: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Propafenone
ATX code: C01BC03
Active ingredient: propafenone (propafenone)
Manufacturer: Alkaloid AD (Republic of Macedonia)
Description and photo update: 2018-24-10
Prices in pharmacies: from 260 rubles.
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Propafenone is an antiarrhythmic drug.
Release form and composition
Propafenone dosage forms:
- coated tablets: round, biconvex, with a dividing line on one side, the shell and core are white (40 pcs. in a glass bottle of dark color, in a cardboard box 1 bottle; 10 pcs. in blisters, in a cardboard box) 4 or 5 blisters);
- solution for intravenous (intravenous) administration: clear colorless liquid (10 ml in ampoules, 5 ampoules in a blister strip, 2 packs in a cardboard box).
1 tablet of Propafenone contains:
- active substance: propafenone hydrochloride - 150 mg;
- auxiliary components: sodium lauryl sulfate, lactose monohydrate, povidone, sodium carboxymethyl starch, microcrystalline cellulose, magnesium stearate, talc;
- shell composition: white opadry Y-1-7000 - hypromellose 5cP, macrogol 400, titanium dioxide (E171).
1 ampoule with Propafenone solution contains:
- active substance: propafenone hydrochloride - 35 mg;
- auxiliary components: hydrochloric acid, propylene glycol, dextrose monohydrate, water for injection.
Pharmacological properties
Pharmacodynamics
Propafenone is an antiarrhythmic drug, the membrane stabilizing property of which is aimed at treating cardiac arrhythmias. In addition, the drug has the effect of a sodium channel blocker (class IC), has a local anesthetic and weak beta-adrenergic blocking effect (class II).
The mechanism of action is aimed at reducing the maximum rate of depolarization of phase 0 of the action potential and its amplitude in the contractile fibers of the ventricles and Purkinje fibers, slowing down conduction along the Purkinje fibers. Oppresses automatism, lengthens the time of the SA (sinoatrial) node and atria.
Against the background of programmed electrical stimulation, it has practically no effect on the increase in the corrected recovery time of the sinus node function.
Increases the effective refractory period of the atrioventricular node, inhibits conduction along additional pathways in two directions (retrograde and antegrade), and increases the threshold for ventricular stimulation.
In the ischemic myocardium, the manifestation of electrophysiological effects is most pronounced in comparison with the normal myocardium. The negative inotropic effect of the drug is manifested when the left ventricular ejection fraction decreases by less than 40%. The therapeutic effect after oral administration occurs within 1 hour and lasts 8-12 hours.
Pharmacokinetics
More than 95% of the drug is absorbed. The dose-dependent bioavailability of Propafenone increases non-linearly with an increase in its dose.
When taken orally, the systemic bioavailability is 5-50%, with intensive metabolism, simultaneous food intake increases it.
When the tablets are taken, the maximum concentration in the blood plasma occurs in 1–3.5 hours. After the start of therapy, the equilibrium concentration in the blood is reached after 3-4 days.
Plasma protein binding is 85–97%.
The effect of primary passage through the liver (biotransformation by the isoenzyme CYP2D6) contributes to the absolute bioavailability of the drug, which depends on the dose and form of the drug.
Propafenone has little permeability across the blood-brain and placental barriers.
Propafenone metabolism has 2 genetically determined patterns. In more than 90% of patients, it is metabolized rapidly and to a large extent with a T 1/2 (half-life) of 2.8-11 hours. In less than 10% of patients, propafenone is metabolized more slowly, T 1/2 - about 17 hours. Since the equilibrium concentration of the drug in the blood occurs after 3-4 days of therapy, the dosage regimen is the same for all patients. Care must be taken with individual dose titration and careful monitoring of the patient's condition.
In the form of metabolites, 38% of the taken dose of the drug is excreted through the kidneys and up to 1% unchanged. With bile in the form of glucuronides, sulfates of metabolites and unchanged propafenone, 53% of the dose of the drug is excreted through the intestine.
With hepatic insufficiency, the excretion of propafenone is reduced.
Indications for use
Film-coated tablets
- prevention and treatment of ventricular arrhythmias;
- prevention and treatment of paroxysmal supraventricular tachyarrhythmias, including atrial fibrillation and atrial flutter;
- paroxysmal supraventricular tachycardia of the re-entry type with the involvement of the atrioventricular node or additional pathways, when the use of other therapy is ineffective or contraindicated.
Solution for intravenous administration
- supraventricular and ventricular premature beats;
- paroxysmal heart rhythm disturbances, including Wolff-Parkinson-White syndrome, supraventricular tachycardia, atrial fibrillation and flutter;
- atrioventricular re-entry tachycardia;
- monomorphic sustained ventricular tachycardia.
Contraindications
- uncontrolled chronic heart failure;
- stage of decompensation of severe chronic heart failure;
- atrial conduction disorders, sinoatrial block;
- cardiogenic shock (not including arrhythmic shock, arterial hypotension due to tachycardia);
- distal blockade caused by conduction disturbance at the level of the bundle branch in patients without a pacemaker;
- severe bradycardia and arterial hypotension with systolic blood pressure (BP) less than 90 mm Hg;
- severe disorders of water and electrolyte balance, including disorders of potassium metabolism;
- bradycardia-tachycardia syndrome;
- atrioventricular (AV) block II – III degree, intraventricular bifascicular block in patients without a pacemaker;
- sick sinus syndrome;
- refractory chronic heart failure with left ventricular ejection fraction less than 35%;
- myasthenia gravis;
- concomitant administration of ritonavir in a daily dose of 0.8–1.2 g;
- glucose-galactose malabsorption syndrome;
- age up to 18 years;
- breast-feeding;
- hypersensitivity to the components of the drug.
In addition, the use of Propafenone tablets is contraindicated for the treatment of patients with severe chronic obstructive pulmonary disease (COPD) or a history of bronchospasm.
Caution should be exercised when prescribing Propafenone to patients with an artificial heart rate driver, arterial hypotension, with concomitant therapy with other antiarrhythmic drugs, with impaired renal and / or liver function, myasthenia gravis, COPD, in old age, with a violation of the water-electrolyte balance.
Use during pregnancy is possible only in exceptional cases, when the expected effect of therapy for the mother is much higher than the potential threat to the fetus, especially in the first trimester of the gestation period.
Instructions for the use of Propafenone: method and dosage
Film-coated tablets
Propafenone tablets are taken orally, after a meal, swallowed whole and washed down with a small amount of water.
The dose and frequency of use is determined by the doctor based on clinical indications and adjusts it as necessary.
It is recommended to start using the drug after the preliminary cancellation of all previously taken antiarrhythmic drugs, since there is a risk of its arrhythmogenic action.
The recommended dosage for patients with a body weight of 70 kg and above: the initial dose is 150 mg 3 times a day. Treatment should be started in a hospital under the control of blood pressure, electrocardiography (ECG) and assessment of the latitude of the ventricular complex (QRS). To achieve the desired therapeutic effect, a gradual (with an interval of 3-4 days) increase in the dose to 300 mg 2 times a day is shown. The maximum daily dose is 900 mg.
With a significant expansion of the QRS complex and in patients with AV block II – III degree, it is recommended to reduce the dose.
To start the use of Propafenone in patients with a body weight of up to 70 kg and the elderly should be with a lower dose with a gradual increase only after eight days of therapy.
In case of impaired liver function, a single dose of the drug should be no more than 20-30% of the usual.
In case of impaired renal function (with creatinine clearance less than 10%), treatment should be started with ½ the usual dose.
Solution for intravenous administration
A solution of Propafenone is used by jet (within 3-5 minutes) or drip (short-term or long-term) intravenous injection.
With drip injection, the drug solution can be mixed with a 5% dextrose (glucose) solution or fructose (levulose) solution.
Cannot be mixed with 0.9% sodium chloride solution!
The doctor sets and corrects the dosage regimen individually.
Treatment should begin in a hospital, after the preliminary cancellation of all previously used antiarrhythmic drugs, under close monitoring of blood pressure, ECG, and assessment of the width of the QRS complex.
The recommended dosage for patients weighing more than 70 kg: 560 mg per day. With a body weight of up to 70 kg and in elderly patients, it is necessary to start treatment with a lower dose with a gradual increase.
The patient is injected in / in a jet dose at the rate of 0.5-1 mg per 1 kg of body weight, if necessary, after 90-120 minutes, the procedure is repeated in the same dose.
For the treatment of patients with severe arrhythmia, the use of drip IV administration of Propafenone is indicated.
When prescribing a continuous infusion, it should be started 3-5 minutes after the intravenous injection of the drug dose.
Treatment should be accompanied by regular monitoring of the patient's condition and ECG indicators. If the QT interval or QRS complex expands by more than 20% compared to baseline values, the PQ interval is lengthened by more than 50%, or the frequency and severity of arrhythmias increases, the dose of the solution should be reduced or therapy should be temporarily discontinued.
Side effects
- on the part of the cardiovascular system: angina pectoris, severe bradycardia, supraventricular tachyarrhythmias, atrioventricular dissociation, in patients with reduced left ventricular function - worsening of the course of heart failure, ventricular tachyarrhythmias, sinoatrial block, intraventricular block, proventricular atrioventricular block, videoventricular block ventricles, against the background of the use of high doses - a pronounced decrease in blood pressure, including chest pain, orthostatic and postural hypotension (more often in elderly patients);
- on the part of the hematopoietic organs: an increase in the period of bleeding, thrombocytopenia, leukopenia, granulocytopenia, manifestation of antinuclear antibodies, agranulocytosis;
- from the side of metabolism: decreased appetite;
- from the immune system: hypersensitivity reactions (cholestasis, pathological changes in the blood), allergic reactions;
- from the nervous system: anxiety, anxiety, headache, dizziness, impaired coordination of movements, fainting, sleep disturbances, confusion, nightmares in dreams, extrapyramidal symptoms, paresthesia, convulsions, vertigo;
- from the digestive system: dryness of the oral mucosa, nausea, bitter taste in the mouth, vomiting, abdominal pain, constipation, flatulence, diarrhea, taste changes, belching, liver dysfunction, including hepatocellular disorders, cholestatic jaundice, hepatitis, cholestasis;
- on the part of the organ of vision: diplopia, blurred vision in the form of blurred vision;
- dermatological reactions: urticaria, skin rash, itching, skin redness, exanthema, lupus-like syndrome, skin hemorrhagic rashes;
- from the genitourinary system: decreased potency, oligospermia;
- laboratory indicators: increased activity of liver enzymes;
- others: bronchospasm, increased sweating, weakness.
Overdose
Symptoms of intoxication may appear after 1 hour, maximum - several hours, after a single dose of a dose corresponding to a double daily dose or more.
Symptoms: persistent lowering of blood pressure, dry mouth, nausea, vomiting, drowsiness, mydriasis, confusion, extrapyramidal disorders, bradycardia, prolongation of the QT interval, conduction disturbances (intra-atrial and intraventricular), ventricular tachyarrhythmia, asystole and paroxysmal paroxysmal ventricular tachycardia, convulsions, coma, pulmonary edema, delirium.
Treatment: if taken orally - immediate gastric lavage. Dobutamine, diazepam administration, defibrillation. If necessary, artificial ventilation of the lungs, chest compressions.
The appointment of hemodialysis and hemoperfusion is ineffective, since propafenone has a high degree of binding to blood plasma proteins and has a large volume of distribution.
special instructions
The use of Propafenone should be accompanied by regular monitoring of the electrolyte composition of blood plasma, especially the level of potassium.
With significant impairment of left ventricular function (left ventricular ejection fraction less than 35%) or organic changes in the myocardium, treatment is recommended with extreme caution, including in elderly patients, starting with lower doses and gradually increasing them. Any dose increase required in the initial period of therapy and when switching to a maintenance dose should be made after 5-8 days of treatment.
Patients with an artificial pacemaker require a more careful approach when diagnosing and prescribing a dose of Propafenone.
Patients should take into account that the effect of the drug can affect the sensitivity threshold and the frequency threshold of the pacemaker. Therefore, its operation should be regularly checked and reprogrammed as necessary.
During the treatment period, the activity of hepatic transaminases should be checked periodically.
In case of insufficient liver function, the bioavailability of the drug increases by 70%, therefore, such patients are advised to reduce the dose and regularly monitor laboratory parameters of liver function.
The use of Propafenone for the treatment of ventricular arrhythmias is considered to be more effective than class IA and IB antiarrhythmics.
The onset of symptoms of the development of undesirable effects of the drug should be reported to the attending physician.
Patients who are on anticoagulant and / or hypoglycemic therapy for a long time require special attention. It is necessary to carefully monitor their clinical condition and laboratory parameters.
With the manifestation of sinoatrial blockade, atrioventricular block of the III degree or often repeated extrasystole during drug therapy, its use should be canceled.
Cancellation of Propafenone should be made by gradually reducing the dose taken.
If you skip taking the next dose, it should be taken as soon as you remember, unless this means taking a double dose of the drug at the same time.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment, it is impossible to engage in the performance of potentially hazardous types of work that require increased attention and high speed of psychomotor reactions, including driving.
Application during pregnancy and lactation
According to the instructions, Propafenone can be used during gestation only in an exceptional case, since it crosses the placental barrier (its concentration in the umbilical cord corresponds to 30% of the concentration level in the mother's blood). Therefore, during pregnancy, especially in the first trimester of the period, the drug is prescribed only if the expected benefit from therapy to the mother outweighs the potential risk to the fetus.
Use with breastfeeding is contraindicated, since the drug enters breast milk. If it is necessary to use Propafenone during lactation, breastfeeding should be stopped.
With impaired renal function
In case of impaired renal function (with creatinine clearance less than 10%), the initial dose of Propafenone in tablet form should be no more than 50% of the usual dose.
For violations of liver function
Since the accumulation of the drug is possible in case of impaired liver function, the daily dose of tablets should be used in the amount of 20-30% of the usual dose.
Use in the elderly
In elderly patients, treatment with Propafenone in tablet form is recommended to start with lower doses than in patients with a body weight of more than 70 kg. The dose can be increased only after eight days of therapy.
Drug interactions
With the simultaneous use of Propafenone:
- propranolol, metoprolol, digoxin, indirect anticoagulants, cyclosporine, theophylline, desipramine increase their level of concentration in blood plasma;
- warfarin, against the background of blocking its metabolism, enhances the effect;
- lidocaine, when combined with propafenone, when administered intravenously, increases the risk of damage to the central nervous system;
- beta-blockers can cause increased antiarrhythmic action;
- local anesthetics and cardiac depressants enhance the effect of propafenone;
- mizolastine, tricyclic antidepressants, ritonavir, antipsychotics increase the risk of arrhythmias;
- phenobarbital, rifampicin can reduce the antiarrhythmic effect of the drug;
- amiodarone increases the likelihood of developing tachycardia of the "pirouette" type, therefore, depending on the therapeutic response, a dose adjustment of each drug may be required;
- depressing sinoatrial and atrioventricular node and drugs with a negative inotropic effect increase the risk of developing adverse events;
- drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression;
- ketoconazole, cimetidine, quinidine, tropisetron, dolasetron, erythromycin, mizolastine, grapefruit juice slow down the metabolism of the drug by 20%, increasing the concentration of propafenone in the blood plasma;
- rifampicin lowers the concentration of propafenone in blood plasma;
- venflaxine may increase its plasma concentration;
- Paroxetine causes an increase in plasma levels of propafenone.
Analogs
Propafenone analogs are: Ritmonorm, Profenan, Propanorm.
Terms and conditions of storage
Keep out of the reach of children.
Store at a temperature of 15-25 ° C in a dark place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Propafenone
Reviews of Propafenone are few, to a greater extent, patients use social networks to clarify the compatibility of the drug while using it with other drugs and ethanol.
The price of Propafenone in pharmacies
The approximate price of Propafenone for a package of tablets containing 40 pcs. May be 235-288 rubles.
Propafenone: prices in online pharmacies
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Drug name Price Pharmacy |
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Propafenone 150 mg film-coated tablets 40 pcs. 260 RUB Buy |
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Propafenone 150 mg film-coated tablets 50 pcs. 325 RUB Buy |
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Propafenone tab. p / o film. 150mg No. 50 377 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
