Reviews for amiodarone. Detailed instructions for the use of amiodarone tablets and ampoules, reviews from patients and cardiologists, amiodarone analogues acceptable for replacement description

Rest and tension (Reviews can be read at the end of the article).

Prevention of recurrence of paroxysmal rhythm disturbances is also carried out:

• ventricular fibrillation, ventricular tachycardia and other life-threatening ventricular arrhythmias;
• supraventricular arrhythmias, including organic heart diseases, with ineffectiveness and impossibility of using other therapy against arrhythmia;
• documented attacks of recurrent sustained paroxysmal supraventricular tachycardia in patients suffering from Wolff-Parkinson-White syndrome;
• atrial fibrillation and atrial flutter.

How to take the pills?

The tablets should be taken before meals with plenty of liquid. The dosage is prescribed by the doctor individually and adjusted if necessary.

Loading dose

In a hospital, the initial dosage, which is divided into several doses, is 600-800 mg per day (maximum 1200 mg). It is taken until a total dose of 10 g is reached for 5-8 days.

The outpatient dose at the beginning, which is divided into several doses, per day is 600-800 mg upon reaching total dose in 10 g for 10-14 days.

The lowest effective dose is used, based on the individual reaction of the patient, and is 100-400 mg (1-2 tablets) per day in one or two doses.

If the drug is used for a long period of time, you can take a break and take the next dose every other day or not take the drug twice a week.

The average single therapeutic dose is 200 mg.

The average daily therapeutic dose is 400 mg.

The maximum dose (single) is 400 mg.

The maximum dose (daily) is 1200 mg.

Release form, composition

Available in the form of white tablets of round, flat-cylindrical shape, having a one-sided chamfer and scoring.

Amiodarone hydrochloride - in 1 table. 200 mg.

Contains the following excipients: povidone, corn starch, Mg stearate, silicon dioxide colloid, Na starch glycolate, microcrystalline cellulose.

The tablets are packaged in blisters (10 pcs), cardboard packaging.

Useful properties

The drug has the following properties:

• antiarrhythmic;
• antianginal;
• coronary dilatant;
• alpha and beta adrenergic blocking;
• thyroid-stimulating;
• hypotensive.

The antiarrhythmic effect is characterized by its effect on the electrophysiological process in the myocardium. The drug is able to lengthen the action potential of cardiomyocytes and increase the effective refractory period of the ventricles and atria.

The antianginal effect is explained by the coronodilator effect, reducing the oxygen demand of the heart muscle. It has an inhibitory effect on receptors: alpha and beta adrenergic receptors of the heart and blood vessels. Decreased sensitivity to sympathetic stimulation nervous system and resistance of the coronary vessels, coronary blood flow increases, heart rate becomes less frequent, and the energy reserve of the myocardium increases.

Side effects

Frequency: very often (more than 10%), often (more than 1% and less than 10%), infrequently (more than 0.1% and less than 1%), rarely (more than 0.01% and less than 0.1%), very rarely (less than 0.01% + individual cases), frequency unknown.

Cardiovascular system:

• often - dose-dependent moderate bradycardia;
• infrequently - sinoatrial and AV block of varying degrees, intensification of existing arrhythmia or the occurrence of a new one, including cardiac arrest);
• very rarely - bradycardia, suspension sinus node;
• frequency unknown - worsening symptoms of chronic heart failure.

Digestive system:

• very often - vomiting and nausea, loss of appetite, impaired taste, feeling of heaviness in the stomach, increased activity of “liver” transaminases;
• often - toxic hepatitis of the acute stage (possible liver failure, including fatal);
• very rarely - chronic liver failure, including fatal.

Respiratory system:

• often - alveolar or interstitial pneumonitis, pleurisy, obliterating bronchiolitis along with pneumonia, including fatal outcomes, pulmonary fibrosis;
• very rarely - spasm in the bronchi with severe respiratory failure, acute syndrome respiratory, including death;
• frequency unknown - bleeding in the lungs.

Sense organs:

• very often - deposition of lipofuscin in the corneal epithelium;
• very rarely - optic neuritis or optic neuropathy.

Endocrine system:

• often - an increase in T4 with a decrease in T3. With long-term use, hypothyroidism may occur, and less commonly, hyperthyroidism (the drug is discontinued);
• very rarely - impaired ADH secretion.

Dermatological reaction:

• very often - photosensitivity;
• often - skin pigmentation in blue shades;
• very rarely - erythema, skin rash, exfoliative dermatitis, alopecia, vasculitis.

Nervous system:

• often - tremors, sleep disturbances, nightmares;
• rarely - peripheral neuropathy, myopathy;
• very rarely - cerebellar ataxia, benign intracranial hypertension, headache.

Very rarely, with long-term use, thrombocytopenia, hemolytic and aplastic anemia are possible.

Epididymitis, decreased potency, and vasculitis occur very rarely.

Overdose

Overdose symptoms:

• demotion blood pressure;
• sinus bradycardia;
• atrioventricular block;
• liver dysfunction;
• worsening heart failure symptoms;
• heart failure.

In case of overdose, rinse the stomach and take activated carbon if you have recently taken the drug. Otherwise, symptomatic therapy is prescribed.

In case of bradycardia, it is possible to use beta-agonists, atropine or install a pacemaker. For tachycardia, intravenous administration of Mg salts is prescribed or cardiac stimulation is performed.

Contraindications

• sick sinus syndrome;
• atrioventricular block of 2-3 degrees, two- and three-bundle blocks without a pacemaker;
• arterial hypotension;
• dysfunction thyroid gland;
• pregnancy and lactation;
• simultaneous use with drugs that increase the QT interval and cause the occurrence of paroxysmal tachycardia (quinidine, disopyramide, procainamide, dofetilide, sotalol, ibutilide, bretylium tosylate, ibutilide, sotalol and other non-antiarrhythmic drugs vincamine, bepridil, some antipsychotics, cisapride, tricyclic antidepressants ; erythromycin, spiramycin; quinine, mefloquine, halofantrine; difemanil methylsulfate, mizolastine and fluoroquinolones;
• hypokalemia and hypomagnesemia;
• congenital (acquired) prolongation of the QT interval;
• interstitial lung diseases;
• taking monoamine oxidase inhibitors in combination;
• children under 18 years of age;
• lactose intolerance, lactase deficiency (glucose-galactose malabsorption);
• high sensitivity to iodine and amiodarone, to other components of the drug.

Can be taken with caution in case of: liver failure, bronchial asthma, elderly patients, chronic heart failure, AV block of the first degree.

Drug interactions

Combinations are contraindicated:

• with antiarrhythmic drugs of classes Ia and III, sotalol;
• with other non-antiarrhythmic drugs: bepridil, vincamine, some neuroleptics: phenothiazine (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sulpiride, veraliprid, tiapride), butyrophenones (droperidol, operidol), sertindole, pimozide; tricyclic antidepressants, cisapride, macrolides (erythromycin for intravenous administration, spiramycin), azoles; antimalarial medicines(quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine (parenteral), difemanil methyl sulfate, mizolastine, astemizole, terfenadine, fluoroquinolones (including moxifloxacin).

Amiodarone is an antiarrhythmic drug. Prescribed to patients coronary disease hearts with rest and tension angina syndromes.

The antiarrhythmic effect is characterized by its effect on the electrophysiological process in the myocardium. The drug is able to lengthen the action potential of cardiomyocytes and increase the effective refractory period of the ventricles and atria. The antianginal effect is explained by the coronodilator effect, reducing the oxygen demand of the heart muscle.

On this page you will find all the information about Amiodarone: full instructions on application to this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Amiodarone. Would you like to leave your opinion? Please write in the comments.

Clinical and pharmacological group

Antiarrhythmic drug of class 3, has an antianginal effect.

Conditions for dispensing from pharmacies

Dispensed with a doctor's prescription.

Prices

How much does Amiodarone cost? Average price in pharmacies it is at the level of 80 rubles.

Release form and composition

Available in the form of white tablets of round, flat-cylindrical shape, having a one-sided chamfer and scoring.

• Amiodarone hydrochloride - in 1 table. 200 mg.
• Contains the following excipients: povidone, corn starch, Mg stearate, silicon dioxide colloid, Na starch glycolate, microcrystalline cellulose.

The tablets are packaged in blisters (10 pcs), cardboard packaging.

Pharmacological effect

Amiodarone is a class III antiarrhythmic drug. It also has alpha and beta adrenergic blocking, antianginal, antihypertensive and coronary dilation effects.

The drug blocks non-activated potassium channels in the cell membranes of cardiomyocytes. To a lesser extent, it affects sodium and calcium channels. By blocking inactivated "fast" sodium channels, it produces effects that are characteristic of class I antiarrhythmic drugs. Amiodarone causes bradycardia by inhibiting the slow depolarization of the sinus node cell membrane, and also inhibits atrioventricular conduction (the effect of class IV antiarrhythmic drugs).

The antiarrhythmic effect of the drug is due to its ability to increase the duration of the action potential of cardiomyocytes and the refractory (effective) period of the ventricles and atria of the heart, the His bundle, the AV node and Purkinje fibers, as a result of which the automaticity of the sinus node, the excitability of cardiomyocytes and the AV conduction slow down.

The antianginal effect of the drug is due to a decrease in coronary artery resistance and a decrease in myocardial oxygen demand due to a decrease in heart rate, which ultimately leads to an increase in coronary blood flow. The drug does not significantly affect systemic blood pressure.

Indications for use

According to the instructions, Amiodarone is indicated for the prevention of paroxysmal arrhythmias, namely:

• (atrial fibrillation), atrial flutter;
• Ventricular arrhythmias that threaten the patient’s life (ventricular fibrillation, ventricular tachycardia);
• Supraventricular arrhythmias (including those with organic heart disease or when it is impossible to use alternative antiarrhythmic therapy);
• Attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome.

Contraindications

This drug is contraindicated in SA and AV blockade 2-3 degrees, sinus bradycardia, collapse, hypersensitivity, cardiogenic shock, hypokalemia, pulmonary interstitial diseases, hypothyroidism, thyrotoxicosis, during pregnancy, lactation and taking MAO inhibitors.

In addition, according to the instructions, Amiodarone is prescribed with caution to people suffering from renal failure, chronic heart failure and bronchial asthma. Also, this remedy should be taken with caution by children under 18 years of age and elderly patients.

Instructions for use Amiodarone

The instructions for use indicate that Amiodarone tablets should be taken orally, before meals, with the required amount of water for swallowing. Instructions for use of Amiodarone require an individual dosage regimen, which must be established and adjusted by the attending physician.

Standard dosage regimen:

• The loading (in other words, saturating) initial dose for inpatient treatment, which is divided into several doses, is 600–800 mg per day, with the maximum allowable daily dose being up to 1200 mg. It must be taken into account that the total dose should be 10 g, usually it is achieved in 5–8 days.
• For outpatient treatment, an initial dose of 600–800 mg per day is prescribed, which is divided into several doses, also reaching a total dose of no more than 10 g, but in 10–14 days.
• To continue the course of treatment with Amiodarone, it is enough to take 100–400 mg per day. Attention! The minimum effective maintenance dose is used.
• To avoid accumulation of the drug, it is necessary to take tablets either every other day or with a break of 2 days, once a week.
• The average single dose with a therapeutic effect is 200 mg.
• The average daily dose is 400 mg.
• Maximum permissible dose– no more than 400 mg at a time, no more than 1200 mg at a time.
• For children, the dose is usually in the range of 2.5-10 mg per day.

Side effects

The use of Amiodarone may cause the following adverse reactions:

• Nervous system: extrapyramidal disorders, tremor, nightmares, sleep disorders, peripheral neuropathy, myopathy, cerebellar ataxia, headache, pseudotumor cerebri;
• Skin reactions: photosensitivity, with long-term use the drug – lead-blue or blue pigmentation of the skin, erythema, exfoliative dermatitis, skin rash, alopecia, vasculitis;
• Respiratory system: interstitial or alveolar pneumonitis, pulmonary fibrosis, pleurisy, obliterating bronchitis with pneumonia, including fatal cases, acute respiratory syndrome, pulmonary hemorrhage, bronchospasm (especially in patients with bronchial asthma);
• Sense organs: optic neuritis, lipofuscin deposition in the corneal epithelium;
• Endocrine system: an increase in the level of the hormone T4, accompanied by a slight decrease in T3 (does not require discontinuation of treatment with Amiodarone if thyroid function is not impaired). With prolonged use, hypothyroidism may develop, and less commonly, hyperthyroidism, requiring discontinuation of the drug. Very rarely, a syndrome of impaired ADH secretion may occur;
• Cardiovascular system: moderate bradycardia, sinoatrial block, proarrhythmogenic effect, AV block of varying degrees, sinus node arrest. With long-term use of the drug, progression of symptoms of chronic heart failure is possible;
• Digestive system: nausea, vomiting, taste disturbance, loss of appetite, increased activity of liver enzymes, heaviness in the epigastrium, acute toxic hepatitis, jaundice, liver failure;
• Laboratory indicators: aplastic or hemolytic anemia, thrombocytopenia;
• Other adverse reactions: decreased potency, epididymitis.

Overdose

Taking large doses of amiodarone can lead to the following conditions:

• Hypotension;
• Bradycardia;
• AV block;
• Asystole;
• Cardiogenic shock;
• Liver dysfunction;
• Heart failure.

The patient should be immediately taken to medical institution. Treatment of an overdose of amiodarone is aimed at detoxifying the body (gastric lavage, taking enterosorbents) and eliminating symptoms.

Special instructions

Taking the drug is possible only after a doctor’s prescription, who determines the treatment regimen and dosage based on the data clinical trial and ECG. It is also necessary to take into account the following special instructions:

1. Before starting to use the drug, it is recommended to conduct a study of the functional activity of the thyroid gland and the level of its hormones in the blood.
2. With long-term use, ECG monitoring of the heart and determination of the level of thyroid hormones and liver enzymes in the blood are required.
3. With increased caution and with constant ECG monitoring of heart function, Amiodarone tablets are prescribed when used in combination with beta-blockers, laxatives and diuretics that remove potassium ions from the body (potassium-sparing diuretics - furosemide), anticoagulants (warfarin), some antibiotics (rifampicin) and antiviral agents(especially drugs that inhibit viral reverse transcriptase).
4. You cannot combine the use of Amiodarone tablets with other antiarrhythmic drugs, as this will lead to an increase in its effects and the development of disturbances in the functional activity of the heart. Combinations with antimalarials, macrolide antibiotics, and fluoroquinolones are also excluded.
5. In case of cough and shortness of breath, to differentiate the inflammatory pathology of the respiratory system, X-ray examination organs chest.
6. While taking Amiodarone tablets, you must avoid activities that involve increased concentration and require a high speed of psychomotor reactions.

In pharmacies the drug is dispensed only with a doctor's prescription.

Drug interactions

• Fluoroquinolones;
• Beta blockers;
• Laxatives;
• Class 1 antiarrhythmic drugs;
• Neuroleptics;
• Tricyclic antidepressants;
• Macrolides;
• Antimalarial.

Co-administration of the listed drugs with amiodarone can lead to the appearance of pronounced side effects, often life-threatening.

The pharmacokinetics of the drug is affected by:

• Cholinesterase inhibitors;
• Orlistat;
• Cholestyramine;
• Anticoagulants;
• Cardiac glycosides;
• Antiviral drugs;
• Cimetidine.

Amiodarone itself can affect the concentrations of cyclosporine, lidocaine, statins, and sodium iodide.

Gross formula

Pharmacological group of the substance Amiodarone

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Amiodarone

Amiodarone hydrochloride is a white or cream-colored crystalline powder. Slightly soluble in water, soluble in alcohol, highly soluble in chloroform.

Pharmacology

Blocks ion channels (mainly potassium, to a lesser extent calcium and sodium) of cardiomyocyte membranes, inhibits the excitation of alpha and beta adrenergic receptors. Increases the duration of the action potential of all cardiac structures due to a pronounced decrease in its amplitude. Has a negative chronotropic effect. Sympatholytic activity and blockade of potassium and calcium channels reduce myocardial oxygen demand and lead to a negative dromotropic effect: conduction slows down and the refractory period in the sinus and AV nodes lengthens. Possessing vasodilator properties, it can reduce coronary vascular resistance.

Bioavailability after oral administration is almost 50% (varies from 35 to 65%). Cmax is achieved in plasma 3-7 hours after taking a single dose, the average concentration in plasma ranges from 1 to 2.5 mg/l. Plasma protein binding - 96%. It has the ability to express accumulation, accumulates in well-perfused organs (liver, lungs and spleen) and is deposited in adipose tissue. Crosses the placental barrier (10-50%) and passes into breast milk. The main route of excretion is through bile (minor enterohepatic recirculation may occur). Has low plasma clearance with negligible renal excretion.

Use of the substance Amiodarone

Severe arrhythmias (usually when other therapy is ineffective or impossible): atrial and ventricular extrasystole, WPW syndrome, atrial flutter and fibrillation, ventricular tachycardia, ventricular fibrillation; arrhythmias due to coronary or heart failure, ventricular arrhythmias in patients with Chagas myocarditis.

Contraindications

Hypersensitivity (including to iodine), sinus bradycardia, AV block, sinus insufficiency syndrome, severe conduction disturbances, cardiogenic shock, thyroid dysfunction.

Use during pregnancy and breastfeeding

Side effects of the substance Amiodarone

Retinal microdetachments, optic neuritis, hyper-(drug discontinuation required) or hypothyroidism, pulmonary fibrosis, pneumonitis, pleurisy, bronchiolitis, pneumonia, peripheral neuropathies and/or myopathies, extrapyramidal tremor, ataxia, cranial hypertension, nightmares, bradycardia, asystole, AV block, nausea, vomiting, liver dysfunction, alopecia, epididymitis, anemia, photosensitivity, allergic reactions.

Updating information

Complications from the organ of vision

Amiodarone can cause serious eye side effects. By April 2011, the New Zealand Adverse Reaction Database had received 51 reports of various ocular adverse reactions in patients. including optical neuropathy (3 cases), deposits in the cornea (19), visual impairment (12).

In this regard, it is recommended:
- conduct a basic examination of the visual organ before starting amiodarone therapy in patients with previous visual impairment;
- conduct periodic examinations of the organ of vision during amiodarone therapy;
- conduct an ophthalmological examination of all patients treated with amiodarone who develop new symptoms of visual impairment or experience a worsening of existing ones;
- if the presence of optic neuropathy is confirmed, the drug should be discontinued.

Sources of information
Drug safety and pharmacovigilance.- 2011.- N1.- P. 27

medsafe.goft.nz.

[Updated 27.04.2012 ]

Interaction

Beta blockers increase the risk of hypotension and bradycardia. Incompatible with CCB (increases the likelihood of developing AV block and hypotension). Cholestyramine reduces T1/2 and the level of amiodarone in plasma, cimetidine increases it. Enhances the effect of indirect anticoagulants, digitalis preparations. Increases the concentration of cyclosporine in the blood.

Updating information

A number of studies have established a clinically important interaction between amiodarone and cyclosporine. Amiodarone may increase serum levels of cyclosporine. There is no need to avoid the combined use of cyclosporine and amiodarone, but careful monitoring and, to reduce the risk of nephrotoxicity, a reduction in the dose of cyclosporine are necessary.
Source of information

Stockley's Drug Interactions/Ed. by Stockley.- 6th ed.- London - Chicago, Pharmaceutical Press.- 2002.- P. 601.

[Updated 15.08.2013 ]

Overdose

Symptoms: bradycardia, marked decrease in blood pressure, AV block, electromechanical dissociation, cardiogenic shock, asystole, cardiac arrest.

Precautions for the substance Amiodarone

ECG monitoring is required. It is not recommended to combine with beta-blockers, verapamil, diltiazem, laxatives that stimulate gastrointestinal motility. Combine with caution with drugs that cause hypokalemia (diuretics, corticosteroids, amphotericin B for intravenous administration) and are prescribed to patients with severe and prolonged diarrhea. Long-term treatment requires observation by an ophthalmologist, regular monitoring of thyroid function, and X-ray monitoring of the lungs.

Interactions with other active ingredients

Related news

Trade names

Amiodarone is an antiarrhythmic drug.

Release form and composition

Amiodarone tablets are prepared containing 200 mg of amiodarone hydrochloride.

The auxiliary components of the drug are: lactose monohydrate, magnesium stearate, colloidal silicon dioxide, microcrystalline cellulose, sodium carboxymethyl starch, corn starch, povidone.

Blisters contain 10 pieces.

Indications for use of Amiodarone

According to the instructions, Amiodarone is indicated for the prevention of paroxysmal arrhythmias, namely:

• Ventricular arrhythmias that threaten the patient’s life (ventricular fibrillation, ventricular tachycardia);
• Supraventricular arrhythmias (including those with organic heart disease or when it is impossible to use alternative antiarrhythmic therapy);
• Atrial fibrillation (atrial fibrillation), atrial flutter;
• Attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome.

Contraindications

According to the instructions, Amiodarone is contraindicated in:

• Severe arterial hypotension;
• Sick sinus syndrome (sinoatrial block, sinus bradycardia, absence of a pacemaker);
• Atrioventricular block of 2-3 degrees, two- and three-fascicle blockades (in the absence of a pacemaker);
• During pregnancy and breastfeeding;
• Thyroid gland dysfunction (hyper- or hypothyroidism);
• Hypomagnesemia, hypokalemia;
• Interstitial lung diseases;
• Hypersensitivity to amiodarone, iodine or auxiliary components of the drug;
• Congenital or acquired prolongation of the QT interval;
• Concomitant use of monoamine oxidase inhibitors;
• Lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• Under 18 years of age (the safety and effectiveness of Amiodarone have not been established);
• Concomitant use with drugs that prolong the QT interval and cause the development of paroxysmal tachycardias.

When using Amiodarone, caution should be exercised when:

• Bronchial asthma;
• Liver failure;
• Chronic heart failure;
• Old age (the likelihood of developing severe bradycardia increases);
• 1st degree AV block.

Method of administration and dosage of Amiodarone

According to the instructions, Amiodarone is intended for internal use. The tablets are taken before meals with plenty of water. The dosage of the medicine is determined individually by the attending physician.

The loading dose of Amiodarone is 60-800 mg per day (no more than 1200 mg) for 5-8 days. Once the desired effect is achieved, the dosage of the drug is reduced to 100-400 mg per day, divided into 2 doses.

Since amiodarone has a long half-life, it can be taken every other day or intermittently twice a week.

Side effects of Amiodarone

The use of Amiodarone may cause the following adverse reactions:

• Cardiovascular system: moderate bradycardia, sinoatrial block, proarrhythmogenic effect, AV block of varying degrees, sinus node arrest. With long-term use of the drug, progression of symptoms of chronic heart failure is possible;
• Digestive system: nausea, vomiting, taste disturbance, loss of appetite, increased activity of liver enzymes, heaviness in the epigastrium, acute toxic hepatitis, jaundice, liver failure;
• Respiratory system: interstitial or alveolar pneumonitis, pulmonary fibrosis, pleurisy, obliterating bronchitis with pneumonia, including fatal cases, acute respiratory syndrome, pulmonary hemorrhage, bronchospasm (especially in patients with bronchial asthma);
• Sense organs: optic neuritis, lipofuscin deposition in the corneal epithelium;
• Endocrine system: an increase in the level of the hormone T4, accompanied by a slight decrease in T3 (does not require discontinuation of treatment with Amiodarone if thyroid function is not impaired). With prolonged use, hypothyroidism may develop, and less commonly, hyperthyroidism, requiring discontinuation of the drug. Very rarely, a syndrome of impaired ADH secretion may occur;
• Nervous system: extrapyramidal disorders, tremor, nightmares, sleep disorders, peripheral neuropathy, myopathy, cerebellar ataxia, headache, pseudotumor cerebri;
• Skin reactions: photosensitivity, with long-term use of the drug - lead-blue or blue pigmentation of the skin, erythema, exfoliative dermatitis, skin rash, alopecia, vasculitis;
• Laboratory indicators: aplastic or hemolytic anemia, thrombocytopenia;
• Other adverse reactions: decreased potency, epididymitis.

Special instructions

Before starting Amiodarone therapy, and every three months during treatment, ECG monitoring, chest X-ray examination and liver function testing should be performed. It is also recommended to check the content of electrolytes in the blood plasma before starting therapy.

The frequency and severity of adverse reactions of Amiodarone directly depend on the dosage of the drug, so it should be used in the minimum permissible doses.

Withdrawal of amiodarone may cause recurrence of cardiac arrhythmias.

As a rule, pharmacological effect Amiodarone remains for another two weeks after its discontinuation.

This medicine contains iodine, which may interfere with test results for radioiodine accumulation in the thyroid gland. Before starting treatment and during drug therapy, you should regularly donate blood to check your thyroid hormone levels.

Amiodarone analogues

The following drugs are analogues of Amiodarone:

• Angoron;
• Aldaron;
• Atlansil;
• Cordarone;
• Cordinil;
• Medakoron;
• Palpitin;
• Sedakoron.

Terms and conditions of storage

Amiodarone should be stored in a dry, dark place at a cool temperature. The shelf life of the medicine is 2 years from the date of manufacture.

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Description

Transparent liquid with a yellowish or greenish tint.

Compound

One ampoule (3 ml of solution) contains: active ingredient: amiodarone hydrochloride – 150 mg; excipients: sodium acetate trihydrate, glacial acetic acid, polysorbate 80, benzyl alcohol, water for injection.

Pharmacotherapeutic group

Medicines for the treatment of heart diseases. Antiarrhythmic drugs, class III.
ATX code: C01BD01.

Pharmacological properties"type="checkbox">

Pharmacological properties

Pharmacodynamics
Antiarrhythmic properties
Extension of the 3rd phase of the action potential of cardiomyocytes without changing its height or rate of rise (class III according to the Vaughan-Williams classification). Isolated prolongation of phase 3 of the action potential occurs due to a slowdown in potassium currents, without changing sodium or calcium currents.
Bradycardic effect due to decreased automatism of the sinus node. This effect is not eliminated by the administration of atropine.
Non-competitive inhibitory effect on alpha and beta adrenergic receptors, without their complete blockade.
Slowing of sinoatrial, atrial and atrioventricular conduction, which is more pronounced against the background of tachycardia.
Does not change intraventricular conduction.
Increases the refractory period and reduces myocardial excitability at the sinoatrial, atrial and atrioventricular levels.
Slows down conduction and lengthens the refractory period of additional atrioventricular pathways.
Does not have a negative inotropic effect.
Pharmacokinetics
The amount of parenterally administered amiodarone in the blood decreases very quickly due to tissue saturation with the drug and its reaching binding sites; the effect reaches a maximum 15 minutes after administration and disappears after approximately 4 hours.
To achieve tissue saturation, intravenous or oral administration must be continued. During saturation, amiodarone accumulates, especially in adipose tissue, and a steady state is achieved over a period of one to several months.
Amiodarone hydrochloride has a long half-life, ranging from 20 to 100 days. The main route of elimination is through the liver with bile; 10% of the substance is excreted by the kidneys. Due to its low renal elimination, amiodarone can be administered to patients with renal impairment without dose adjustment.

Indications for use

Treatment with the drug should begin in a hospital setting and under the supervision of a specialist. This medicine is intended only for the treatment of severe rhythm disturbances that do not respond to other treatments, or when other treatments cannot be used.
Tachyarrhythmias associated with Wolff-Parkinson-White syndrome.
Tachyarrhythmias of all types, including supraventricular, nodal and ventricular tachycardia; atrial flutter and fibrillation, ventricular fibrillation; in cases where other drugs cannot be used.
The drug can be used when a rapid response to treatment is required or when oral administration is not possible.

Contraindications

– sick sinus syndrome (SSNS), sinus bradycardia, sinoatrial block, except in cases of correction with an artificial pacemaker;
– atrioventricular block II and III degrees, intraventricular conduction disorders (blockade of two and three legs of the His bundle); in these cases, the drug can be used in specialized departments under the guise of an artificial pacemaker (pacemaker);
– cardiogenic shock, collapse;
– severe arterial hypotension;
– simultaneous use with drugs that can cause polymorphic ventricular tachycardia of the “pirouette” type;
– thyroid dysfunction (hypothyroidism, hyperthyroidism);
– hypokalemia;
– pregnancy;
– breast-feeding;
– increased sensitivity to iodine and/or amiodarone;
– severe pulmonary dysfunction (interstitial lung disease);
– cardiomyopathy or decompensated heart failure (the patient’s condition may worsen).
Due to the presence of benzyl alcohol, Amiodarone is contraindicated in newborns, infants and children under 3 years of age.

Directions for use and doses

Method of administration: intravenous.
Do not dilute the drug with isotonic sodium chloride solution, as precipitate may form!
Do not mix with other drugs in the same infusion system.
The drug should only be used when the necessary equipment for monitoring cardiac function, defibrillation and pacing is available.
The drug can be used before direct current cardioversion.
The standard recommended dose is 5 mg/kg body weight, administered by infusion over a period of 20 minutes to 2 hours. The drug can be administered as a solution diluted in 250 ml of 5% glucose solution. After this, a repeated infusion of the drug at a dose of up to 1200 mg (approximately 15 mg/kg body weight) in a 5% glucose solution of up to 500 ml over 24 hours can be used, and the infusion rate must be adjusted depending on the patient's clinical response ( see section "Precautions").
In extremely urgent clinical situations, the drug, at the discretion of the physician, can be administered as a slow injection at a dose of 150-300 mg in 10-20 ml of 5% glucose solution over at least 3 minutes. After this, the drug can be re-administered no earlier than after 15 minutes. Patients who are administered the drug in the above manner must be closely supervised - for example, in the department intensive care(See section "Precautions").
Switching from intravenous to oral administration
Immediately after an adequate response to treatment, oral drug therapy should be started simultaneously at the usual loading dose (i.e., 200 mg three times daily). After this, the drug should be gradually withdrawn by stepwise dose reduction.
Children
The safety and effectiveness of amiodarone in children have not been evaluated, and therefore the use of this drug in children is not recommended. The medicine contains benzyl alcohol. There are reports of cases of death as a result of the development of “dyspnea syndrome” (“gasping syndrome”) in newborns after the administration of solutions containing this preservative. Symptoms of this complication include the sudden onset of shortness of breath, hypotension, bradycardia and the development of cardiovascular collapse.
Elderly patients
As with other patients, it is important to use the minimum effective dose of the drug. Although there is no evidence to support specific dosing requirements in this group of patients, these patients may be more prone to developing bradycardia and conduction disturbances when overused. high dose. Particular attention should be paid to monitoring thyroid function (see sections "Contraindications", "Precautions" and " Adverse reactions»).
Patients with renal and/or liver failure
Although no dose adjustments were required for patients with renal or hepatic impairment during long-term oral administration of amiodarone, careful clinical monitoring of these patients, especially the elderly, in the intensive care unit is necessary.
Cardiopulmonary resuscitation
The recommended dose for ventricular fibrillation/pulseless ventricular tachycardia resistant to defibrillation is 300 mg (or 5 mg/kg body weight), which is administered diluted in 20 ml of 5% glucose solution by rapid injection. If ventricular fibrillation persists, an additional 150 mg (or 2.5 mg/kg body weight) of the drug can be administered.

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Side effects

Adverse reactions classified by organ system class and frequency of occurrence according to the following criteria: very common (>1/10); often (> 1/100 to< 1/10); нечасто (>1/1000 to< 1/100); редко (>1/10000 to< 1/1000); очень редко (< 1/10000); неизвестно (не может быть оценена на основе имеющихся данных).
Disorders of the blood and lymphatic system. Granulomas have been identified in patients taking amiodarone bone marrow. The clinical significance of these findings is unknown.
Cardiac disorders. Often: bradycardia. Very rarely: the emergence of a new or worsening of an existing arrhythmia, sometimes followed by cardiac arrest. Severe bradycardia, sinus node blockade, which requires discontinuation of amiodarone, especially in patients with sinus node dysfunction and/or elderly patients, paroxysmal ventricular tachycardia of the “torsade de pointes” type. Conduction disturbances (sinoatrial block, AV block).
Endocrine disorders. Rarely: hyperthyroidism (see section "Precautions"). Very rarely: syndrome of inappropriate antidiuretic hormone secretion (SIADH). Unknown: hypothyroidism.
Violations by gastrointestinal tract. Very often: nausea. Unknown: pancreatitis (acute).
Disorders of the liver and biliary tract. Rare: moderate and isolated increase in transaminase levels (1.5–3 times higher than normal) at the beginning of treatment, which disappeared after discontinuation of the drug or even spontaneously; acute liver damage with increased serum transaminase levels and/or jaundice, including liver failure, sometimes fatal (see section "Precautions").
General disorders and reactions at the injection site. Often: an inflammatory reaction is possible, in particular phlebitis of the superficial veins, if injected directly into a peripheral vein; reactions at the injection site, in particular pain, erythema, swelling, necrosis, extravasation, infiltration, inflammation, skin induration, thrombophlebitis, cellulitis, infections and pigmentation disorders. Rarely: the excipient benzyl alcohol may cause hypersensitivity reactions.
Violations by immune system. Rarely: hypersensitivity reactions, including anaphylactic shock. Unknown: Cases of angioedema (Quincke's edema) have been reported.
Muscular, skeletal and connective tissue. Unknown: back pain.
Nervous system disorders. Often: extrapyramidal tremor. Uncommon: peripheral sensorimotor neuropathy and/or myopathy, usually reversible. Rarely: benign intracranial hypertension (pseudotumor cerebri), headache.
Violations by respiratory system, chest and mediastinal organs. Rarely: acute respiratory distress syndrome, in some cases with a fatal outcome (see section "Precautions"), bronchospasm and/or apnea in case of severe respiratory failure, especially in patients with bronchial asthma, interstitial pneumonia.
Disorders of the skin and subcutaneous tissues. Often: eczema. Redto: excessive sweating. Unknown: urticaria, skin reactions such as toxic epidermal necrolysis (TEN)/Stevens-Johnson syndrome, bullous dermatitis and drug reactions with eosinophilia and systemic symptoms.
Violations of the organ of vision. Often: microdeposits on the anterior surface of the cornea, located in the area below the pupil, are found in almost every patient. Cause colored halos in glare or blurred vision. They usually resolve within 6 to 12 months after stopping amiodarone hydrochloride. Very rarely: Optic neuropathy/neuritis, which can progress to blindness.
Vascular disorders. Often: usually a moderate and short-lived decrease in blood pressure. Cases of severe hypotension or vascular collapse have been reported, particularly in cases of overdose or after very rapid administration. Rarely: tides.

Interaction with other drugs

Precautions

Excipients
The medicinal product contains benzyl alcohol, which can cause toxic and allergic reactions in infants and children under 3 years of age (see section "Method of administration and dosage").
Since benzyl alcohol crosses the placenta, injection solutions containing benzyl alcohol are not recommended during pregnancy.
Infusion through central veins
Except in emergency situations, Amiodarone should only be used in specialized intensive care units with continuous monitoring (ECG, blood pressure).
The drug should be administered through central veins, since administration through peripheral veins may cause local reactions.
The drug should be administered only as an infusion, since even a very slow injection can increase the manifestations of arterial hypotension, heart failure or severe respiratory failure (see section "Adverse reactions").
If it is impossible to enter into central vein, the drug can be administered through peripheral veins with maximum blood flow.
Heart symptoms
There have been cases of occurrence or exacerbation of existing arrhythmia, sometimes with death (see section "Adverse reactions"). The arrhythmogenic effect of amiodarone is weak or less pronounced than the arrhythmogenic effect of most antiarrhythmic drugs, and usually occurs with the use of certain combinations of drugs (see section “Interaction with other drugs”) or with electrolyte imbalance.
Pulmonary symptoms
Several cases of interstitial pneumopathy have been reported with the use of the drug. The appearance of shortness of breath or dry cough, either alone or due to worsening general condition, indicates the possibility of pulmonary toxicity, such as interstitial pneumopathy, and requires monitoring the patient's condition (see section "Adverse reactions"). It is necessary to reconsider the advisability of using amiodarone, since interstitial pneumopathy is usually reversible if amiodarone is discontinued early.
In addition, some patients treated with amiodarone have experienced acute respiratory distress syndrome immediately after surgery, and close monitoring of these patients is recommended during mechanical ventilation.
Thyroid diseases
Amiodarone may cause hyperthyroidism, especially in patients with a history of thyroid disease or taking/previously taking amiodarone. The diagnosis is confirmed by a pronounced decrease in the level of thyroid-stimulating hormone (TSH).
Amiodarone contains iodine and may therefore interfere with radioiodine intake. However, thyroid function test results (free T3, free T4, TSH) remain interpretable. Amiodarone inhibits the peripheral conversion of thyroxine (T4) and triiodothyronine (T3) and can cause local biochemical changes in patients with normal thyroid function (increased free T4 levels with a slight decrease or even normal maintenance of free T3 levels). Such phenomena do not require discontinuation of treatment with amiodarone.
Liver symptoms
Severe and sometimes fatal hepatocellular failure may develop within 24 hours of starting the drug. At the beginning of treatment and subsequently throughout the course of treatment with amiodarone, regular monitoring of liver function is recommended (see section “Adverse reactions”). It is necessary to reduce the dose of amiodarone or discontinue this drug if transaminase levels increase more than three times compared with normal values these indicators.
Electrolyte imbalance
It is important to consider situations that may be associated with hypokalemia and may provoke proarrhythmogenic effects. Hypokalemia should be corrected before administering amiodarone.
Anesthesia
Before surgery, the anesthesiologist must be informed that the patient is receiving amiodarone. Long-term treatment with amiodarone may increase the risk of hemodynamic side effects associated with general or local anesthesia, such as bradycardia, hypotension, decreased cardiac output and conduction disturbances.
Disorders associated with interactions with other drugs
Combined use with beta-adrenergic blockers, except sotalol (contraindicated combination) and esmolol (combination requiring caution when used); verapamil and diltiazem can only be used in the case of prevention of life-threatening ventricular arrhythmias (see section “Interaction with other drugs”).