Amiodarone - instructions for use, analogs, testimonials and release forms (tablets of 200 mg, injections in ampoules for injection of 5%) of a drug for the treatment of arrhythmias and extrasystoles in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Amiodarone. There are reviews of the visitors of the site - consumers of this medication, as well as the opinions of doctors of specialists on the use of Amiodarone in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Amiodarone in the presence of existing structural analogues.Use to treat arrhythmias and extrasystoles in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Amiodarone - antiarrhythmic drug of class 3, has an antianginal effect.

Antiarrhythmic effect is associated with the ability to increase the duration of the cardiomyocyte action potential and the effective refractory period of the atria, ventricles of the heart, AV node, bundle of His, Purkinje fibers. This is accompanied by a decrease in the automatism of the sinus node, a slowing of AV conduction, a decrease in the excitability of cardiomyocytes. It is believed that the mechanism of increasing the duration of the action potential is associated with the blockade of the potassium channels (the removal of potassium ions from the cardiomyocytes decreases). Blocking inactivated "fast" sodium channels, has the effects characteristic for antiarrhythmic drugs of the 1st class. It inhibits slow (diastolic) depolarization of the membrane of the cells of the sinus node, causing bradycardia, depressing AV conduction (anti-arrhythmic effect of the 4th class).

The antianginal effect is due to coronary dilatory and antiadrenergic action, a decrease in myocardial oxygen demand.Has a retarding effect on alpha and beta-adrenergic receptors of the cardiovascular system (without complete blockade). Reduces sensitivity to hyperstimulation of the sympathetic nervous system, tone of the coronary vessels; increases coronary blood flow; reduces heart rate; increases the energy reserves of the myocardium (by increasing the content of creatine sulfate, adenosine and glycogen). Reduces OPSS and systemic blood pressure (with intravenous administration).

It is believed that amiodarone may increase the level of phospholipids in tissues.

Contains iodine. Affects the metabolism of thyroid hormones, inhibits the conversion of T3 to T4 (blockade of thyroxine-5-deiodinase) and blocks the seizure of these hormones by cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium (T3 deficiency can lead to its hyperproduction and thyrotoxicosis) .

When taken orally, the onset of action - from 2-3 days to 2-3 months, the duration of the action is also variable - from several weeks to several months.

After intravenous administration, the maximum effect is achieved after 1-30 minutes and lasts 1-3 hours.

Composition

Amiodarone hydrochloride + excipients.

Pharmacokinetics

After oral administration, it is slowly absorbed from the digestive tract, the absorption is 20-55%. It penetrates the blood-brain barrier (GEB) and the placental barrier (10-50%), excreted in breast milk (25% of the dose received by the mother). Intensively metabolized in the liver with the formation of an active metabolite of desethylamiodarone, and also, apparently, by deiodination. With prolonged treatment, Iodine concentrations can reach 60-80% of the concentration of amiodarone. It is an inhibitor of the isoenzymes CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. It is excreted mainly with bile through the intestine, there may be a small enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted in dialysis.

Indications

• life-threatening ventricular arrhythmias (including ventricular tachycardia);
• prevention of ventricular fibrillation (including after cardioversion);
• supraventricular arrhythmias (usually with ineffectiveness or impossibility of other therapies, especially those associated with WPW syndrome), incl. paroxysm of flicker and atrial flutter;
• atrial and ventricular extrasystole;
• arrhythmias on the background of coronary insufficiency or chronic heart failure;
• parasystole;
• ventricular arrhythmias in patients with Chagas myocarditis;
• angina pectoris.

Forms of release

Tablets 200 mg.

Solution for intravenous administration 5% (injections in ampoules for injection).

Instructions for use and dosage

When administered orally for adults, the initial single dose is 200 mg. For children, the dose is 2.5-10 mg per day. Scheme and duration of treatment are set individually.

For intravenous (bolus or infusion (a drip)) single dose of 5 mg / kg, daily dose - and 1.2 g (15 mg / kg).

Side effect

• sinus bradycardia (refractory to m-holinoblokatoram);
• AV blockade;
• progression of CHF;
• ventricular arrhythmia of the "pirouette" type;
• reinforcement of existing arrhythmia or its occurrence;
• a decrease in blood pressure;
• development of hypo- or hyperthyroidism;
• cough;
• dyspnea;
• interstitial pneumonia or alveolitis;
• fibrosis of the lungs;
• pleurisy;
• bronchospasm;
• apnea (in patients with severe respiratory failure);
• nausea, vomiting;
• decreased appetite;
• dullness or loss of taste;
• feeling of heaviness in epigastrium;
• abdominal pain;
• constipation, diarrhea;
• flatulence;
• toxic hepatitis;
• cholestasis;
• jaundice;
• cirrhosis of the liver;
• headache;
• weakness;
• dizziness;
• depression;
• feeling tired;
• paresthesia;
• auditory hallucinations;
• peripheral neuropathy;
• tremor;
• memory impairment, sleep;
• optic neuritis;
• intracranial hypertension;
• uveitis;
• deposition of lipofuscin in the epithelium of the cornea (if the deposits are significant and partially fill the pupil - complaints of luminous points or shroud before the eyes in bright light);
• microcellular retina;
• thrombocytopenia;
• hemolytic and aplastic anemia;
• skin rash;
• exfoliative dermatitis;
• photosensitivity;
• alopecia;
• gray-blue staining of the skin;
• thrombophlebitis;
• epididymitis;
• myopathy;
• decreased potency;
• vasculitis;
• increased sweating.

Contraindications

• sinus bradycardia;
• syndrome of weakness of the sinus node (SSSU);
• sinoatrial blockade;
• AV blockade of 2-3 degrees (without the use of a pacemaker);
• cardiogenic shock;
• hypokalemia;
• collapse;
• arterial hypotension;
• hypothyroidism;
• thyrotoxicosis;
• interstitial lung diseases;
• administration of MAO inhibitors;
• pregnancy;
• lactation period;
• increased sensitivity to amiodarone and iodine.

Application in pregnancy and lactation

Contraindicated in pregnancy and lactation.

Amiodarone and desmethylamidarone penetrate the placental barrier, their concentrations in the fetal blood are 10% and 25% of the concentration in the mother's blood, respectively.

Amiodarone and desmethylamidarone are excreted in breast milk.

Use in children

Use with caution at the age of 18 years (efficacy and safety of use not established).

Application in elderly patients

Use with caution in elderly patients (high risk of severe bradycardia).

special instructions

Do not use in patients with severe respiratory failure.

Before starting the use of amiodarone, an X-ray examination of the lungs and thyroid function should be performed, if necessary, correct electrolyte disturbances.

With long-term treatment, regular monitoring of thyroid function, consultation of the oculist and X-ray examination of the lungs are necessary.

Parenteral can be used only in specialized departments of hospitals under the constant control of blood pressure, heart rate and ECG.

Patients receiving amiodarone should avoid direct exposure to sunlight.

With the cancellation of amiodarone, recurrences of cardiac rhythm disturbances are possible.

Can influence the results of the test of accumulation of radioactive iodine in the thyroid gland.

Do not use amiodarone concomitantly with quinidine, beta-blockers, calcium channel blockers, digoxin, coumarin, doxepin.

Drug Interactions

The drug interaction of amiodarone with other drugs is possible even a few months after the end of its use due to a long half-life.

With the simultaneous use of amiodarone and antiarrhythmic drugs of class 1 A (including disopyramide), the QT interval increases due to the additive effect on its magnitude and the risk of developing a ventricular pirouette tachycardia increases.

With the simultaneous use of amiodarone with laxatives, which can cause hypokalemia, the risk of ventricular arrhythmia increases.

Means that cause hypokalemia, including diuretics, corticosteroids, amphotericin B (IV), tetracosactide with simultaneous use with amiodarone cause an increase in the QT interval and an increased risk of ventricular arrhythmia (including pirouette).

With the simultaneous use of funds for general anesthesia, oxygen therapy, there is a risk of bradycardia, arterial hypotension, conduction disorders, reduction of the shock volume of the heart, which, apparently, is due to additive cardiodepressive and vasodilating effects.

With simultaneous use of tricyclic antidepressants, phenothiazines, astemizole, terfenadine cause an increase in the QT interval and an increased risk of ventricular arrhythmia, especially of the pirouette type.

With the simultaneous use of warfarin, fenprokumona, acenocoumarol, the anticoagulant effect increases and the risk of bleeding increases.

With the simultaneous use of vinamine, sultopride, Erythromycin (intravenously), pentamidine (intravenously, intramuscularly), the risk of ventricular arrhythmia such as pirouette increases.

With simultaneous use, an increase in the concentration of dextromethorphan in the blood plasma is possible due to a decrease in the rate of its metabolism in the liver, which is due to inhibition of the activity of the CYP2D6 isoenzyme P450 system under the influence of amiodarone and delayed excretion of dextromethorphan from the body.

With the simultaneous use of digoxin, the concentration of Digoxin in the blood plasma is significantly increased due to a decrease in its clearance and, as a result, the risk of developing digitalis intoxication increases.

With the simultaneous use of diltiazem, Verapamil increased negative inotropic action, bradycardia, conduction disturbance, AV blockade.

A case of increasing the concentration of amiodarone in blood plasma is described with its simultaneous application with indinavir. It is believed that ritonavir, nelfinavir, saquinavir will have similar effects.

With simultaneous application of colestyramine, the concentration of amiodarone in the blood plasma decreases due to its binding to colestyramine and a decrease in absorption from the gastrointestinal tract.

There are reports of an increase in the concentration of Lidocaine in the blood plasma with simultaneous use with amiodarone and the development of seizures,due to inhibition of lidocaine metabolism under the influence of amiodarone.

It is not desirable to share Amiodarone with alcohol and ethanol-containing products.

It is believed that synergy is possible with respect to the oppressive effect on the sinus node.

With the simultaneous use of lithium carbonate may develop hypothyroidism.

With the simultaneous use of procainamide, the QT interval increases due to the additive effect on its magnitude and the risk of ventricular pirouette tachycardia. An increase in the concentration in the blood plasma of procainamide and its metabolite N-acetylprocainamide and the increase in side effects.

With simultaneous use of propranolol, metoprolol, sotalol possible hypotension, bradycardia, ventricular fibrillation, asystole.

With the simultaneous use of trazodone, a case of arrhythmia of the "pirouette" type is described.

With the simultaneous use of quinidine, the QT interval increases due to the additive effect on its magnitude and the risk of developing a ventricular pirouette tachycardia. An increase in the concentration of quinidine in the blood plasma and an increase in its side effects.

With simultaneous application, the case of enhancing the side effects of Clonazepam has been described, which is apparently due to its cumulation due to the inhibition of oxidative metabolism in the liver under the influence of amiodarone.

With the simultaneous use of cisapride, the QT interval is significantly increased due to the additive effect, the risk of ventricular arrhythmia (including pirouette).

With simultaneous use increases the concentration of cyclosporine in the blood plasma, the risk of developing nephrotoxicity.

A case of pulmonary toxicity is described with simultaneous application of cyclophosphamide in high doses and amiodarone.

The concentration of amiodarone in the blood plasma increases due to the slowing of its metabolism under the influence of cimetidine and other inhibitors of microsomal liver enzymes.

It is believed that due to the inhibition of liver enzymes under the influence of amiodarone, with the participation of which the metabolism of phenytoin occurs, it is possible to increase the concentration of the latter in the blood plasma and to increase its side effects.

Due to the induction of microsomal enzymes of the liver under the influence of phenytoin, the metabolic rate of amiodarone in the liver increases and its concentration in the blood plasma decreases.

Analogues of the drug Amiodarone

Structural analogs for the active substance:

• Amiodaron Belupo;
• Amiodarone Sandoz;
• Amiodarone Acry;
• Amiodarone hydrochloride;
• Amiocordin;
• Vero Amiodarone;
• Cardiodarone;
• Cordarone;
• Opakorden;
• Rhythmiodaron;
• Sedacoron.

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