Amiodarone structural formula. Amiodarone tablets: instructions for use

concentrate for preparing a solution for intravenous administration

One ampoule contains:

Active substance: amiodarone hydrochloride in terms of 100% substance - 150.0 mg;Excipients: sodium acetate trihydrate - 3.0 mg; glacial acetic acid - 0.02211 ml; 1 M acetic acid solution - up to pH 3.5; Polysorbate 80 (Tween-80) - 300.0 mg; gasoline alcohol - 60.0 mg; water for injection - up to 3.0 ml.

Amiodarone belongs to the III class of antiarrhythmic drugs (repolarization inhibitors) and has a unique mechanism of antiarrhythmic action: in addition to the properties of class III antiarrhythmics (potassium channel blockade), it has the effects of class I antiarrhythmics (sodium channel blockade), class IV antiarrhythmics (calcium channel blockade) and non-competitive beta-adrenergic blocking action.

In addition to the antiarrhythmic action, it has antianginal, coronary dilating, alpha and beta adrenergic blocking effects. The severity of the action of amiodarone reaches a maximum 15 minutes after its intravenous administration and stops after approximately 4 hours.

Antiarrhythmic properties are due to:

-an increase in the duration of the 3rd phase of the action potential of cardiomyocytes (mainly due to blocking the ion current in potassium channels - the effect antiarrhythmic agent III class according to Williams classification);

-a decrease in the automatism of the sinus node, leading to a decrease in the heart rate (HR);

-non-competitive blockade of alpha and beta adrenergic receptors;

-deceleration of intracardiac (sinoatrial, atrial and atrioventricular - AV) conduction. This action is more pronounced with tachycardia. It has no significant effect on intraventricular conduction;

-an increase in the duration of the refractory period and a decrease in the excitability of myocardiocytes of the atria and ventricles, as well as an increase in the duration of the refractory period of the AV node;

-slowing down the speed of conduction and increasing the duration of the refractory period in additional bundles of atrioventricular conduction.

Other effects of amiodarone:

-a decrease in oxygen consumption by the myocardium due to a moderate decrease in total peripheral vascular resistance (OPSS) and heart rate, as well as myocardial contractility;

-an increase in coronary blood flow due to a direct effect on the tone of the coronary arteries;

-preservation of the value of cardiac output despite a slight decrease in myocardial contractility (due to a decrease in OPSS and afterload);

-influence on the metabolism of thyroid hormones: inhibition of the transformationT 3 in T 4 (blockade of thyroxine-5-deiodinase) and blocking the capture of these hormones by myocardiocytes and hepatocytes, leading to a weakening of the stimulating effect of thyroid hormones;

The remedy was created in 1960. Has been clinically tested in laboratories and time. Despite the danger of side effects, experts appreciate the drug for its high efficiency. And today we will consider in more detail the indications for use and instructions for the drug Amiodarone, its reviews, prices and analogues.

Features of the drug

The remedy among antiarrhythmic drugs has established itself as one of the best. The use of the drug must be prescribed with caution, given side effects... For a long time, the medicine was considered by cardiologists as a "last resort".

A number of studies have shown that the drug not only has the characteristics of the most effective, but also in comparison with drugs of this direction is the safest. Observations and study of statistical data have revealed that the use of amiodarone leads to a decrease in mortality rates, including sudden death.

Arrhythmogenic effects while taking the drug were seen in one percent of patients, which is the minimum number compared to other drugs. Specialists prescribe amiodarone, if indicated, to patients, including those with organic heart lesions.

In the following English-language video with useful schemes, the drug Amiodarone is discussed in great detail:

Amiodarone composition

The main active substance - amiodarone hydrochloride. Each tablet contains 200 mg of it.

Additional substances:

• sodium carboxymethyl starch,
• povidone,
• lactose monohydrate,
• silica,
• magnesium stearate,
• corn starch,
• microcrystalline cellulose.

Dosage forms

The drug is available in the form of round tablets. They are flat-cylindrical. On one side of the tablet, a risk is applied and a bevel is selected. The color of the drug is white, it may look rough white.

The package contains three blisters of 10 tablets each. average price packaging 135 p.

Now is the time to talk about the mechanism of action of Amiodarone.

pharmachologic effect

The drug has an effect on the body:

• antianginal - removal of the prerequisites for myocardial ischemia,
• antiarrhythmic - normalization of the state at.

Pharmacodynamics

• The action of the drug is aimed at reducing the oxygen demand of the heart muscles. This effect occurs due to the blocking of channels that allow ions to pass to a greater extent of potassium. Channels associated with the passage of calcium ions are less blocked.
• As a result of such changes in the work of the channels, conduction slows down, while the period when the atrioventricular and sinus nodes return to normal operation is lengthened.
• The drug has a relaxing effect on the smooth muscles of the coronary vessels. Thus, the action of the drug helps to increase the lumen of the coronary vessels, which reduces the resistance in them.

Pharmacokinetics

Half of the taken dose of the drug is absorbed in the body. Ninety-six percent of the bioavailable substance binds to plasma proteins.

The active substance accumulates in the organs:

• spleen,
• liver,
• lungs.

Also, the main component is deposited in the tissues of the fat layer. The drug is excreted through the bile.

Indications

The remedy is prescribed for such conditions:

• atrial flutter and,
• ventricular arrhythmias, which can be life-threatening;
• patients with a diagnosis who have had attacks of supraventricular tachycardia ();
• - even in cases where other similar drugs cannot be used or they do not help, as well as if there is an organic lesion of the heart.

During the gestation of a child and breastfeeding, the drug is not prescribed.

Instructions for use

The dose of taking the medicine at a time is determined individually by the doctor. On average, the following norms are accepted:

• maximum single dose - 400 mg,
• the same average therapeutic dose - 200 mg,
• maximum daily dose – 1200 mg,
• the same average therapeutic dose is 400 mg.

The tablets are taken before meals. The drug is washed down with water.

Contraindications

The drug is not used if the patient has:

• dysfunction of the thyroid gland,
• hypersensitivity to drug components, including iodine;
• severe conductivity disorders,
• AV blockade.

About what side effects has the action of amiodarone, read below.

Side effects

Taking the drug can cause undesirable effects:

• asystole,
• bronchiolitis,
• micro retinal detachment,
• nightmares,
• epididymitis,
• neuritis optic nerve,
• photosensitivity,
• pneumonia,
• disorders in the liver,
• hyperthyroidism,
• hypothyroidism,
• allergies,
• alopecia,
• extrapyramidal tremor,
• peripheral neuropathies,
• anemia
• nausea
• peripheral myopathies,
• fibrosis of the lungs
• AV blockade,
• vomiting
• pneumonitis,
• bradycardia,
• ataxia,
• pleurisy.

special instructions

The drug can cause side effects. It has been noticed that this happens more often with prolonged use of the medication. According to statistics, uncomfortable conditions occur in half of the patients taking the drug.

At the same time, negative manifestations of side effects force 5-25% of users to stop taking the drug. Particular attention should be paid to the state of vision.

• On the eve of the treatment course and with an interval of three months, the patient should be examined, which must necessarily include.
• To avoid if possible negative effects from the use of the drug, a dose should be prescribed for taking in the minimum amount of a substance that can give a therapeutic effect.
• A patient taking amiodarone is advised to avoid activities requiring precision and increased attention. And also it is necessary to give up activities associated with danger, including driving a car.
• If the patient develops shortness of breath or cough, it is necessary to check the condition of the lungs. For symptoms of lung damage, it is recommended to take a chest x-ray every six months.
• To avoid the effect of photosensitization, it is necessary to avoid direct rays of the sun. If you have to be in open places, protective measures should be taken.
• During treatment with the drug, regular examination of the cornea of \u200b\u200bthe eye is indicated. Observation of the patient by an ophthalmologist can provide information about whether it is possible to continue the course of treatment with amiodarone.
• The drug contains iodine in its composition. Therefore, an endocrinologist is involved in deciding whether it can be applied to a specific patient, and whether the course does harm the state of the thyroid gland.

INN: Amiodarone

Manufacturer: Open Joint Stock Company "Borisov Plant medical supplies"(JSC" BZMP ")

Anatomical-therapeutic-chemical classification: Amiodarone

Registration number in the RK: No. RK-LS-5 No. 016246

Registration period: 12.11.2015 - 12.11.2020

Instructions

Tradename

Amiodarone

International non-proprietary name

Amiodarone

Dosage form

Tablets 200 mg

Composition

One tablet contains:

active substance - amiodarone hydrochloride (in terms of 100% substance) 200 mg,

excipients: lactose monohydrate, potato starch, povidone, calcium stearate.

Description

Tablets are white or almost white, flat-cylindrical, with a score and a bevel.

Farmakotherapeutic group

Drugs for the treatment of heart disease. Class III antiarrhythmic drugs. Amiodarone.

ATX code C01BD01.

Pharmacological properties

Pharmacokinetics

Absorption is slow and variable - 30-50%, bioavailability - 30-50%. The maximum concentration in blood plasma is observed in 3-7 hours.The therapeutic plasma concentration range is 1-2.5 mg / l (but when determining the dose, it is necessary to keep in mind clinical picture). The volume of distribution is 60 liters, which indicates an intensive distribution in the tissue. It has a high fat solubility, in high concentrations it is found in adipose tissue and organs with good blood supply (the concentration in adipose tissue, liver, kidneys, myocardium is higher than in plasma, respectively, by 300, 200, 50 and 34 times). The features of the pharmacokinetics of amiodarone necessitate the use of the drug in high loading doses. Penetrates the blood-brain barrier and the placenta (10-50%), is secreted in breast milk (25% of the dose received by the mother). Communication with plasma proteins - 95% (62% - with albumin, 33.5% - with beta-lipoproteins).

Metabolized in the liver. The main metabolite, desethylamiodarone, is pharmacologically active and can enhance the antiarrhythmic effect of the main compound. Possibly, it is also metabolized by deiodination (at a dose of 300 mg, approximately 9 mg of elemental iodine is released). With prolonged treatment, iodine concentrations can reach 60-80% of the concentration of amiodarone. It is an inhibitor of the enzyme system CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver.

Given the ability to cumulate and the associated large variability of pharmacokinetic parameters, the data on the half-life are contradictory. Withdrawal of amiodarone after oral administration it is carried out in 2 phases: the initial period is 4-21 hours, in the second phase the half-life is 25-110 days. After prolonged oral administration, the average elimination half-life is 40 days (this is important when choosing a dose, since it may take at least 1 month to stabilize the new plasma concentration, while complete elimination can last 61 days (more 4 months).

It is excreted in the bile (85-95%), less than 1% of the dose taken orally is excreted by the kidneys (therefore, in case of impaired renal function, there is no need to change the dosage). Amiodarone and its metabolites are not dialyzed.

Pharmacodynamics

Class III antiarrhythmic drug (repolarization inhibitor). It also has antianginal, coronary dilating, alpha and beta adrenergic blocking and hypotensive effects.

The antianginal effect is due to a coronary dilator and antiadrenergic action, a decrease in myocardial oxygen demand.

Has an inhibitory effect on the alpha and beta adrenergic receptors of the cardiovascular system (without their complete blockade). Reduces sensitivity to hyperstimulation of the sympathetic nervous system, the tone of the coronary vessels; increases coronary blood flow; slows down the heart rate; increases the energy reserves of the myocardium (by increasing the content of creatine sulfate, adenosine and glycogen).

The antiarrhythmic effect is due to the effect on the electrophysiological processes in the myocardium; lengthens the action potential of cardiomyocytes, increasing the effective refractory period of the atria, ventricles, atrioventricular node, bundle of His and Purkinje fibers, additional pathways of excitation.

By blocking inactivated "fast" sodium channels, it has the effects characteristic of class I antiarrhythmic drugs.

It inhibits the slow (diastolic) depolarization of the sinus node cell membrane, causing bradycardia, and inhibits atrioventricular conduction (the effect of class IV antiarrhythmics).

Its structure is similar to thyroid hormones. The iodine content is about 37% of its mol. masses. Affects the exchange of thyroid hormones, inhibits the conversion of T4 to T3 (blockade of thyroxine-5-deiodinase) and blocks the capture of these hormones by cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium.

The onset of action (even when using "loading" doses) is from 2-3 days to 2-3 months, the duration of action varies from several weeks to months (determined in plasma for 9 months after stopping it).

Indications for use

Amiodarone therapy can be carried out only in hospitals or on an outpatient basis under the supervision of a cardiologist.

For the treatment of severe arrhythmias that cannot be treated with other drugs, or when other drugs cannot be prescribed.

Tachyarrhythmias associated with Wolff-Parkinson-White syndrome.

Atrial fibrillation and atrial flutter, if other medications cannot be prescribed.

Tachyarrhythmias of a paroxysmal nature, including atrial, atrioventricular and ventricular tachycardias, ventricular fibrillation, when other drugs cannot be prescribed.

Method of administration and dosage

Initial treatment

The usual dosage regimen is 600 mg / day - 3 tablets per day, divided into 2-3 doses, for 8-10 days.

In some cases, at the beginning of treatment, higher doses may be used (4 or 5 tablets per day), but only for a short time and with electrocardiographic control.

Supportive care

The minimum effective dose should be determined, in accordance with the individual response, it can range from ½ tablet per day (1 tablet every other day) to 2 tablets per day.

The average single therapeutic dose is 200 mg, the average therapeutic daily dose is 400 mg, the maximum single dose is 400 mg, and the maximum daily dose is 1200 mg.

Side effects

Frequency: very often (10% or more), often (1% or more; less than 10%), infrequently (0.1% or more; less than 1%), rarely (0.01% or more; less than 0.1 %), very rarely (less than 0.01%, including individual cases), the frequency is unknown (the frequency cannot be determined from the available data).

Very often (10% or more)

Nausea, vomiting, decreased appetite, dullness or loss of taste, a feeling of heaviness in the epigastrium, an isolated increase in the activity of "liver" transaminases (1.5 - 3 times higher than normal)

Microdeposits in the cornea are almost always present in adults, and are usually localized in the area under the pupil and are not a contraindication to continuing treatment. In exceptional cases, they may be accompanied by the perception of colored and dazzling light or blurred vision. Micro-deposits in the cornea, which are formed by a complex of lipids, always disappear after stopping treatment.

In the absence of any clinical symptoms of distyroidism, the level of "dissociated" thyroid hormone (an increase in the level of T4 with a normal or slightly reduced level of T3) is not a reason to interrupt treatment.

Often (1% or more; less than 10%)

Moderate bradycardia (dose dependent);

Acute toxic hepatitis with an increase in the activity of "hepatic" transaminases and / or jaundice, including the development of liver failure, incl. fatal;

Interstitial or alveolar pneumonitis, obliterating bronchiolitis with pneumonia, incl. fatal, pleurisy, pulmonary fibrosis;

With prolonged use, hypothyroidism, hyperthyroidism may develop (possibly fatal, drug withdrawal is required);

Grayish or bluish skin pigmentation (with prolonged use; disappears after stopping the drug);

Tremor and other extrapyramidal symptoms, sleep disorders, incl. "Nightmarish" dreams

Infrequently (0.1% or more; less than 1%)

SA and AV blockade of various degrees, proarrhythmogenic effect (the emergence of new or worsening of existing arrhythmias, including with cardiac arrest);

Conduction disturbances (sinoauricular block of varying degrees)

Seldom:

Peripheral neuropathy (sensory, motor, mixed) and / or myopathy

Very rare (less than 0.01%, including isolated cases)

Severe bradycardia, sinus node arrest (in patients with sinus node dysfunction and elderly patients);

Chronic liver failure (pseudo-alcoholic hepatitis, cirrhosis), incl. fatal;

Bronchospasm in patients with severe respiratory failure (especially in patients with bronchial asthma), acute respiratory syndrome, incl. fatal;

Optic neuritis / optic neuropathy.

Syndrome of inappropriate secretion of ADH CHCAD / RSIADH (hyponatremia)

Erythema (with simultaneous radiation therapy), skin rash, exfoliative dermatitis (no connection with the drug has been established), alopecia.

Cerebellar ataxia, benign intracranial hypertension (pseudotumor of the brain), headache, vertigo;

Vasculitis

Epididymitis;

Violation of potency (the connection with taking the drug has not been established);

With prolonged use, thrombocytopenia, hemolytic and aplastic anemia;

Renal failure with a moderate increase in creatinine;

Frequency unknown (frequency cannot be determined from available data)

Pulmonary bleeding;

Bone marrow granulomas;

Cases of angioedema.

Contraindications

Hypersensitivity (including to iodine);

Sick sinus syndrome;

Sinus bradycardia;

Sinoatrial blockade;

Atrioventricular block II-III st. (without using a pacemaker);

Cardiogenic shock;

Hypokalemia;

Collapse;

Arterial hypotension;

Hypothyroidism;

Thyrotoxicosis;

Interstitial lung disease;

Children and adolescents up to 18 years old;

Taking monoamine oxidase inhibitors.

Two- and three-beam blockade (without using a pacemaker);

Hypomagnesemia;

Hypothyroidism;

Hyperthyroidism;

Congenital or acquired lengthening of the Q-T interval;

Simultaneous intake of drugs that lengthen q-T interval and causing paroxysmal tachycardia (including polymorphic ventricular type "pirouette");

Pregnancy and lactation.

Carefully: chronic insufficiency III and IV degrees, stage I AV block, liver failure, bronchial asthma, old age (high risk of developing severe bradycardia)

Drug interactions

Contraindicated combinations (risk of developing polymorphic ventricular tachycardia of the "pirouette" type): class 1a antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide, procainamide), class III (dofetilide, ibutilide, bretilium tosylate), sotalol; bepridil, vincamine, phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultoprid, sulpiride, tiapride, veraliprid), butyrophenones (seryperidol, p. tricyclic antidepressants, cisapride, macrolides (iv erythromycin, spiramycin), azoles, antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine (parenteral), diphemanil methyl sulfate, mizolastine, astemizole, terfenadine, fluoroquinolones (including moxifloxacin).

Combinations not recommended: beta-blockers, blockers of slow calcium channels (verapamil, diltiazem) - risk of disruption of automatism (severe bradycardia) and conduction; laxative drugs that stimulate intestinal motility - the risk of developing ventricular tachycardia of the "pirouette" type against the background of hypokalemia caused by laxative drugs, cardiac glycosides - a violation of automatism (severe bradycardia) and AV conduction (increased concentration of digoxin);

Combinations requiring caution:

Diuretics that cause hypokalemia, amphotericin B (i.v.), systemic glucocorticosteroids, tetracosactide - the risk of developing ventricular arrhythmias, incl. ventricular tachycardia of the "pirouette" type;

Procainamide - the risk of side effects of procainamide (amiodarone increases the plasma concentration of procainamide and its metabolite N-acetylprocainamide);

Anticoagulants indirect action (warfarin) - amiodarone increases the concentration of warfarin (risk of bleeding) by inhibiting the isoenzyme CYP2C9;

Esmolol - violation of contractility, automatism and conduction (suppression of compensatory reactions of the sympathetic nervous system);

Phenytoin, phosphenytoin - risk of development neurological disorders (amiodarone increases the concentration of phenytoin by inhibiting the isoenzyme CYP2C9);

Flecainide - amiodarone increases its concentration (by inhibiting the isoenzyme CYP2D6);

Medicines metabolized with the participation of the CYP3A4 isoenzyme (cyclosporine, fentanyl, lidocaine, tacrolimus, sildenafil, midazolam, triazolam, dihydroergotamine, ergotamine, statins, including simvastatin - amiodarone increases their concentration and / or the risk of their pharmacological effects);

Orlistat reduces the concentration of amiodarone and its active metabolite; clonidine, guanfacine, cholinesterase inhibitors (donepezil, galantamine, rivastigmine, tacrine, ambenonium chloride, pyridostigmine, neostigmine), pilocarpine - the risk of severe bradycardia;

Cimetidine, grapefruit juice slow down the metabolism of amiodarone and increase its plasma concentration;

Medicines for inhalation anesthesia - the risk of developing bradycardia (resistant to the administration of atropine), lowering blood pressure, conduction disturbances, decreased cardiac output, acute respiratory distress syndrome, incl. fatal, the development of which is associated with high oxygen concentrations;

Radioactive iodine - amiodarone (contains iodine) may interfere with absorption radioactive iodinethat can distort the results of radioisotope studies of the thyroid gland;

Rifampicin and St. John's wort preparations (powerful inducers of the CYP3A4 isoenzyme) reduce the concentration of amiodarone in plasma; HIV protease inhibitors (inhibitors of the isoenzyme CYP3A4) can increase plasma concentrations of amiodarone;

Clopidogrel - a decrease in its plasma concentration is possible;

Dextromethorphan (substrate of CYP3A4 and CYP2D6 isoenzymes) - its concentration may be increased (amiodarone inhibits the CYP2D6 isoenzyme).

special instructions

Chronic heart failure (FC III-IV according to NYHA classification), grade I AV block, liver failure, bronchial asthma, old age (high risk of severe bradycardia).

Before starting therapy, it is necessary to conduct an ECG, an X-ray examination of the lungs, to assess the function of the thyroid gland (hormone concentration), liver (transaminase activity) and the concentration of plasma electrolytes (potassium).

During the period of treatment, transaminases are periodically analyzed (with an increase of 3 times or doubling in the case of their initially increased activity, the dose is reduced, until the complete cessation of therapy) and an ECG (width complex QRS and the duration of the QT interval). An increase in the QTc interval of no more than 450 ms or no more than 25% of the initial value is acceptable. These changes are not a manifestation of the toxic effect of the drug, however, they require monitoring to adjust the dose and assess the possible proarrhythmogenic effect of amiodarone.

Recommended annual lung x-ray, function test external respiration Once every six months, testing for thyroid-stimulating hormone before starting treatment and then on a regular basis during treatment and several months after stopping treatment. With absence clinical signs dysfunction of the thyroid gland, treatment should not be stopped. Shortness of breath or unproductive cough may be associated with the toxic effect of amiodarone on the lungs. Respiratory system disorders are generally reversible with early withdrawal of amiodarone. Early withdrawal of amiodarone associated with glucocorticosteroid therapy or not associated with it leads to regression of disorders. Clinical symptoms usually disappear within 3-4 weeks, and then there is a slower recovery of the radiological picture and lung function (several months).

To prevent the development of photosensitization, it is recommended to avoid sun exposure or use special sunscreens.

If blurred vision or decreased visual acuity occurs while taking amiodarone, it is recommended to conduct a complete ophthalmological examination, including fundoscopy. Cases of neuropathy and / or optic neuritis require a decision on the advisability of using amiodarone.

If canceled, recurrence of rhythm disturbances is possible.

Due to the presence of lactose in the preparation, it is not recommended for patients with congenital galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption.

After cancellation, the pharmacodynamic effect persists for 10-30 days.

Contains iodine (in 200 mg - 75 mg of iodine), therefore it may affect the results of tests for the accumulation of radioactive iodine in thyroid gland.

When carrying out surgical interventions, the anesthesiologist should be informed about the drug intake (the possibility of acute respiratory distress syndrome in adults immediately after surgery).

In the case of the simultaneous use of amiodarone and simvastatin, the dose of simvastatin should not exceed 10 mg per day due to the potential risk of rhabdomyolysis in such patients. In the case of the simultaneous use of amiodarone and lovastatin, the dose of the latter should not exceed 40 mg per day. The patient should also be informed of the need for immediate medical attention in the event of any unexpected muscle pain, muscle weakness.

Pregnancy and lactation

Application during pregnancy and lactation is possible only with life-threatening rhythm disturbances with the ineffectiveness of other antiarrhythmic therapy (causes dysfunction of the fetal thyroid gland). Safety and efficacy in children has not been determined.

Features of influence drug on the ability to manage vehicle or potentially dangerous mechanisms

During the treatment period, it is necessary to refrain from driving and practicing potentially dangerous species activities requiring increased concentration of attention and speed of psychomotor reactions.

Overdose

Symptoms: bradycardia, atrioventricular block, lowering blood pressure, paroxysmal tachycardia of the "pirouette" type, aggravation of existing CHF, impaired liver function, cardiac arrest.

Amiodarone: instructions for use and reviews

Latin name: Amiodaron

ATX code: C01BD01

Active substance: Amiodarone (Amiodarone)

Manufacturer: Balkanpharma-Dupnitza (Bulgaria), North Star, Organic, Biocom CJSC, AVVA-RUS, Obolenskoe FP (Russia)

Description and photo update: 16.09.2019

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.

In blisters of 10 pieces.

Indications for the use of Amiodarone

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

• Life-threatening ventricular arrhythmias (ventricular fibrillation, ventricular tachycardia);
• Supraventricular arrhythmias (including in organic heart disease or in the impossibility of using alternative antiarrhythmic therapy);
• Atrial fibrillation (atrial fibrillation), atrial flutter;
• Seizures of recurrent persistent supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome.

Contraindications

According to the instructions, Amiodarone is contraindicated for:

• Severe arterial hypotension;
• Sick sinus syndrome (sinus blockade, sinus bradycardia, absence of a pacemaker);
• Atrioventricular blockade 2-3 degrees, two- and three-beam blockade (in the absence of a pacemaker);
• The period of pregnancy and breastfeeding;
• Thyroid dysfunction (hyper- or hypothyroidism);
• Hypomagnesemia, hypokalemia;
• Interstitial lung disease;
• Hypersensitivity to amiodarone, iodine or auxiliary components of the drug;
• Congenital or acquired lengthening of the QT interval;
• Concomitant use of monoamine oxidase inhibitors;
• Lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• Under the age of 18 (safety and effectiveness of amiodarone have not been established);
• Simultaneous administration with drugs that lengthen the QT interval and cause the development of paroxysmal tachycardia.

Caution should be exercised in the use of Amiodarone when:

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

Method of administration and dosage of Amiodarone

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

The loading dose of Amiodarone is 60-800 mg per day (not more than 1200 mg) for 5-8 days. Upon reaching the desired effect, 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 twice a week with breaks.

Side effects of Amiodarone

The use of Amiodarone can cause the following adverse reactions:

• Cardiovascular system: moderate bradycardia, sinoatrial block, proarrhythmogenic action, AV block of varying degrees, stopping the sinus node. With prolonged use of the drug, progression of symptoms of chronic heart failure is possible;
• Digestive system: nausea, vomiting, taste disturbances, 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 ones, acute respiratory syndrome, pulmonary hemorrhage, bronchospasm (especially in patients with bronchial asthma);
• Sensory organs: optic neuritis, lipofuscin deposition in the corneal epithelium;
• Endocrine system: an increase in the level of the T4 hormone, accompanied by a slight decrease in T3 (does not require the termination of treatment with Amiodarone if the thyroid function is not impaired). With prolonged use, hypothyroidism may develop, less often - hyperthyroidism, requiring drug withdrawal. Very rarely, a syndrome of impaired ADH secretion may occur;
• Nervous system: extrapyramidal disorders, tremors, nightmares, sleep disturbances, peripheral neuropathy, myopathy, cerebellar ataxia, headache, pseudotumor of the brain;
• Skin reactions: photosensitivity, with prolonged use of the drug - lead-blue or blue skin pigmentation, erythema, exfoliative dermatitis, skin rash, alopecia, vasculitis;
• Laboratory indicators: aplastic or hemolytic anemia, thrombocytopenia;
• Other side reactions: decreased potency, epididymitis.

special instructions

Before starting therapy with Amiodarone, as well as every three months during treatment, ECG control, X-ray examination of the lungs and liver function tests should be performed. Also, before starting therapy, it is recommended to check the content of electrolytes in the blood plasma.

Frequency and severity adverse reactions Amiodarone is directly dependent on the dosage of the drug, so it should be used in the minimum acceptable doses.

Withdrawal of amiodarone can cause recurrence of cardiac arrhythmias.

As a rule, the pharmacological effect of Amiodarone persists for another two weeks after its withdrawal.

The medicine contains iodine, which can interfere with the results of tests for the accumulation of radioactive iodine in the thyroid gland. Before starting treatment and during therapy with the drug, blood should be regularly donated to the level of thyroid hormones.

Amiodarone analogs

Amiodarone analogs are the following drugs:

• Angoron;
• Aldaron;
• Atlansil;
• Kordaron;
• Cordinil;
• Medacoron;
• 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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