Propanorm coated pills 150mg N50
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Active ingredients
Propafenone
Release form
Pills
Composition
Propafenone hydrochloride 150 mg; which corresponds to the content of propafenone 135.7 mg; excipients: microcrystalline granulated cellulose, corn starch, copovidone, croscarmellose sodium, magnesium stearate, sodium lauryl sulfate, hypromellose 5, macrogol 6000, titanium dioxide, emulsion of dimethicone with silicon dioxide.
Pharmacological effect
Antiarrhythmic drug class IC, blocking fast sodium channels .; It has a weak β-adrenergic blocking activity (corresponds to approximately 1/40 of the activity of propranolol) and m-anticholinergic blocking effect. Antiarrhythmic effect is based on local anesthetic and direct membrane-stabilizing effect on myocardiocytes, as well as on the blockade of adrenergic β-adrenergic receptors and calcium channels .; Local anesthetic effect approximately corresponds to the activity of procaine. Propafenone, blocking fast sodium channels, causes a dose-dependent decrease in the depolarization rate and inhibits the action potential phase 0 and its amplitude in Purkinje fibers and contractile fibers of the ventricles, inhibits automatism. Slows down the purkinje fibers. Lengthens the time of the sinoatrial node and atria. With the use of propafenone, the PQ interval is extended and the QRS complex is expanded (from 15 to 25) on the ECG, as well as the AH and HV intervals on the histogram. By slowing down, the drug lengthens the effective refractory period in the atria, AV node, additional bundles, and, to a lesser extent, ventricles. No significant changes in the QT interval are observed. Electrophysiological effects are more pronounced in ischemic than in normal myocardium. It has a negative inotropic effect, which usually occurs when the left ventricular ejection fraction decreases below 40%; The effect of the drug begins 1 hour after ingestion, reaches a maximum after 2-3 hours and lasts 8-12 hours.
Pharmacokinetics
Absorption More than 95% of propafenone is absorbed after taking the drug inside. The bioavailability of the drug increases nonlinearly with increasing dose (from 5% to 12% with an increase in a single dose from 150 mg to 300 mg, and when taken at a dose of 450 mg to 40-50%).C max is reached in 1-3.5 hours and is 500-1500 μg / l .; ; Distribution; Binding to plasma proteins and internal organs is 85-97%; Permeability through the BBB and placental barrier is low. V d - 3-4 l / kg .; ; Metabolism; Propafenone is almost completely metabolized. Described 11 drug metabolites, pharmacologically active are 5-hydroxypropanone and N-depropylpropanone, which have antiarrhythmic activity comparable to propafenone. Oxidative metabolism depends on a specific cytochrome, the activity of which is genetically determined .; The therapeutic concentration of propafenone in the blood plasma is 0.5-2 mg / l .; ; Removal; T 1/2 in patients with intensive metabolism ranges from 2 to 10 hours, in patients with delayed metabolism - from 10 to 32 hours; Excreted in the urine - 38% in the form of metabolites (<1% in unchanged form), with bile - 53% (in the form of glucuronides and sulfates) .; ; Pharmacokinetics in special clinical situations; In liver failure, excretion is reduced.
Indications
Prevention and treatment of paroxysmal rhythm disturbances (supraventricular - atrial fibrillation and atrial flutter, Wolff-Parkinson-White syndrome); Prevention and treatment of atrioventricular re-tachycardia;);
Contraindications
Severe forms of chronic heart failure (decompensated), uncontrolled chronic heart failure.; Cardiogenic shock (with the exception of arterial hypotension due to tachycardia and antiarrhythmic shock); Severe bradycardia.; Severe arterial hypotension.; Sinoatrial blockade, in the treatment of heart failure,; ; The blockade of the bundle of his. His.; Intraventricular bifascicular block and AV block II and III degree (without installing a pacemaker) .; SSS.; Tachycardia syndrome-b Radicardia ".; Myocardial infarction.; Lactation period (breastfeeding); Children and adolescents under 18 years of age (efficacy and safety have not been established); Digoxin intoxication.; Hypersensitivity to the components of the drug.; You should prescribe the drug in the following cases: COPD; Myasthenia gravis (including myasthenia gravis); Cardiacfailure (ejection fraction less than 30%); Cardiomyopathy; Arterial hypotension; Hepatic cholestasis; Hepatic and / or renal insufficiency. Electrolyte disturbances (must be corrected before the appointment of propafenone); Patients over the age of 70 years .; Patients with permanent or temporary pacemaker.; Simultaneous administration with other antiarrhythmic drugs of similar effect.
Use during pregnancy and lactation
The use of propafenone during pregnancy, especially in the first trimester, is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.
Side effects
Cardiovascular; Bradycardia, AV-dissociation, ventricular tachyarrhythmias, angina, worsening of heart failure (in patients with reduced left ventricular function), sinoatrial blockade, AV-blockade, impaired intraventricular conduction, supraventricular tachyarrhythmias, at admission doses - Orthostatic hypotension; ; On the part of the digestive system; A change in taste, dry mouth, bitter taste in the mouth, nausea, loss of appetite, a feeling of heaviness in the epigastrium, constipation or diarrhea; rarely, liver dysfunction, cholestatic jaundice, cholestasis .; ; CNS; headache, dizziness; rarely blurred vision, diplopia, convulsions .; ; From the hemopoietic system; Leukopenia, agranulocytosis, increased bleeding time, thrombocytopenia, the appearance of antinuclear antibodies .; ; On the part of the reproductive system; Oligospermia, reduced potency .; ; Allergic reactions; Skin rash, itching, rash, redness of the skin, urticaria, lupus-like syndrome .; ; Other; Weakness, bronchospasm, hemorrhagic rash on the skin.
Overdose
At a single dose of 2 times the daily dose, symptoms of intoxication may appear after 1 h, and a maximum after a few hours. Symptoms: persistent lowering of blood pressure, nausea, vomiting, dry mouth, dysphagia, emergency cerebral patients, cerebs , asystole, coma, convulsions, delirium, pulmonary edema.; Treatment: gastric lavage, defibrillation, administration of dobutamine, diazepam; if necessary, mechanical ventilation and indirect heart massage. Hemodialysis is ineffective.
Interaction with other drugs
You can not combine propanorm with lidocaine, because enhanced cardiodepressive effect .; With the simultaneous use of propafenone increases the concentration of propranolol, metoprolol, digoxin (increases the risk of glycoside intoxication), indirect anticoagulants, cyclosporine in the blood plasma .; With the simultaneous use of propafenone enhances the effect of warfarin (by blocking the metabolism) .; With simultaneous use with beta-blockers, tricyclic antidepressants and may increase antiarrhythmic action .; With simultaneous use with local anesthetics increases the risk of damage to the central nervous system .; Cimetidine and quinidine, slowing down the metabolism, increase the concentration of propafenone in the plasma by 20%, rifampicin - reduces .; When used concomitantly with propafenone, amiodarone increases the risk of developing pirouette tachycardia .; Drugs that inhibit the sinoatrial node and AV node and have a negative inotropic effect, while used with propafenone increase the risk of side effects .; Drugs that inhibit bone marrow hematopoiesis, while used with propafenone, increase the risk of myelosuppression.