Amiodarone - official instructions for use. The drug Amiodarone - reviews

Date: 28.10.2020

Catad_pgroup Antiarrhythmic drugs

Amiodarone - official instructions for use

Read this leaflet carefully before using this medication.
Save the instructions as you may need them again.
If you have any questions, see your doctor.
This medicine has been prescribed for you personally and should not be passed on to others as it may harm them even if they have the same symptoms as you.

Registration number:

LP 003074-060715

Tradename

Amiodarone

International non-proprietary name

Amiodarone

Dosage form

Pills

Composition for one tablet

Active substance:
Amiodarone hydrochloride - 200.0 mg
Excipients:
Lactose monohydrate - 100.0 mg, potato starch - 60.6 mg, microcrystalline cellulose - 24.0 mg, talc - 7.0 mg, povidone (polyvinylpyrrolidone) - 4.8 mg, calcium stearate - 3.6 mg.

Description

Tablets, white or white with a creamy shade, flat-cylindrical with a scored and beveled.

Pharmacotherapeutic group

Antiarrhythmic agent

ATX code

Pharmacological properties

Pharmacodynamics
Class III antiarrhythmic drug (repolarization inhibitor). It also has antianginal, coronary dilating, alpha and beta adrenergic blocking and antihypertensive effects.
Blocks non-activated potassium (to a lesser extent - calcium and sodium) channels of cell membranes of cardiomyocytes. 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, inhibits atrioventricular (AV) conduction (the effect of class IV antiarrhythmics).
Has the properties of a non-competitive blocker of alpha and beta-adrenergic receptors.
The antiarrhythmic effect of amiodarone is associated with its ability to cause an increase in the duration of the action potential of cardiomyocytes and the effective refractory period of the atria and ventricles of the heart, AV node, His bundle, Purkinje fibers, which is accompanied by a decrease in the automatism of the sinus node, a slowdown in AV conduction, and a decrease in the excitability of cardiomyocytes.
The antianginal effect is due to a decrease in myocardial oxygen demand due to a decrease in the heart rate (HR) and a decrease in the resistance of the coronary arteries, which leads to an increase in coronary blood flow. Does not significantly affect systemic blood pressure (BP).
Its structure is similar to thyroid hormones. The iodine content is about 37% of its molecular weight. It affects the exchange of thyroid hormones, inhibits the conversion of thyroxine (T4) into triiodothyronine (TZ) (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 with the use of "loading" doses) is from 2-3 days to 2-3 months, the duration of action varies from several weeks to months (determined in blood plasma for 9 months after stopping its intake).

Pharmacokinetics
Suction
After oral administration, it is slowly absorbed from the gastrointestinal tract, bioavailability is 35-65%. It is found in the blood after 1 / 2-4 hours. The maximum concentration in the blood after taking a single dose is observed after 2-10 hours. The therapeutic plasma concentration range is 1-2.5 mg / l (but when determining the dose, it is necessary to keep in mind the clinical picture) ... Time to reach steady-state concentration (TCss) - from one to several months (depending on individual characteristics).
Distribution
The volume of distribution is 60 liters, which indicates an intensive distribution in the tissues. 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 blood plasma by 300, 200, 50 and 34 times, respectively).
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%), secreted in breast milk (25% of the dose received by the mother). Communication with blood plasma proteins - 95% (62% - with albumin, 33.5% - with beta-lipoproteins).
Metabolism
Metabolized in the liver; the main metabolite, desethylamiodarone, which has similar pharmacological properties, 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, the concentration of iodine can reach 60-80% of the concentration of amiodarone. It is a carrier of organic anions, an inhibitor of P-glycoprotein and isoenzymes CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7, CYP1AI, CYP1A2. CYP2C19, CYP2A6, CYP2B6, CYP2C8 in the liver.
Withdrawal
Given the ability to cumulate and the associated large variability of pharmacokinetic parameters, the data on the half-life (T1 / 2) are contradictory. Excretion of amiodarone after oral administration is carried out in 2 phases: the initial period - 4-21 hours, in the second phase T1 / 2 - 25-110 days (on average 20-100 days). After prolonged oral administration, the average T1 / 2 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 more than 4 months) ...
It is excreted through the intestines - 85-95%, by the kidneys - less than 1% of the dose taken orally (therefore, in case of impaired renal function, there is no need to change the dosage). Amiodarone and its metabolites are not dialyzed.

Indications for use

Prevention of recurrence of paroxysmal rhythm disturbances: life-threatening ventricular arrhythmias (including ventricular tachycardia and ventricular fibrillation); supraventricular arrhythmias (including with organic heart diseases, as well as with ineffectiveness or impossibility of using other antiarrhythmic therapy); documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome; atrial fibrillation (atrial fibrillation) and atrial flutter.
Prevention of sudden death due to arrhythmia in high-risk patients: patients after a recent myocardial infarction with the number of ventricular extrasystoles more than 10 / h, with clinical signs of chronic heart failure (CHF) and left ventricular ejection (LV) fraction less than 40%.

Contraindications

Hypersensitivity to any of the components of the drug or iodine; sick sinus syndrome (sinus bradycardia and sinoatrial blockade in the absence of a pacemaker (risk of stopping the sinus node); atrioventricular block TI-III degree, two- and three-beam blockade (in the absence of a pacemaker); hypothyroidism, hyperthyroidism; severe arterial hypotension, lactose intolerance lactase, glucose-galactose malabsorption syndrome; hypokalemia, hypomagnesemia; interstitial lung disease; pregnancy, breastfeeding; concomitant use of monoamine oxidase inhibitors, drugs that prolong the QT interval, congenital or acquired lengthening of the QT interval; age up to 18 years. with other drugs ".

Carefully

Chronic heart failure (CHF) (III-IV functional class according to the classification of chronic heart failure of the New York Heart Association - NYHA), atrioventricular block I degree, liver failure, bronchial asthma, old age (high risk of developing severe bradycardia).

If you have one of the listed diseases, be sure to consult your doctor before using the drug.

Application during pregnancy and during breastfeeding

You should not use Amiodarone during pregnancy, because during this period the thyroid gland of the newborn begins to accumulate iodine, and the use of Amiodarone during this period can provoke the development of hypothyroidism due to an increase in the concentration of iodine. Application during pregnancy and lactation is possible only with life-threatening rhythm disturbances with the ineffectiveness of other antiarrhythmic therapy, since the drug causes dysfunction of the fetal thyroid gland.
Amiodarone crosses the placenta (10-50%), is secreted in breast milk (25% of the dose received by the mother), therefore, the drug is contraindicated for use during lactation. If it is necessary to use it during lactation, then breastfeeding should be canceled.

Method of administration and dosage

Use Amiodarone only as directed by your doctor!
The tablets are taken orally with a sufficient amount of liquid.
The drug can be taken during or after meals. The dosage regimen is set individually in accordance with the condition and needs of the patient and is adjusted by the doctor.
Loading (saturating) dose
In the hospital: the initial dose (divided into several (2-3) doses) is 600-800 mg / day (up to a maximum dose of 1200 mg / day), until a total dose of 10 g is reached (usually within 5-8 days).
Outpatient: the initial dose, divided into several doses, is 600-800 mg / day until a total dose of 10 g is reached (usually within 10-14 days).
Maintenance dose
For maintenance treatment, the lowest effective dose is used, depending on the individual patient's response and usually ranges from 100-400 mg / day. (1 / 2-2 tablets) in 1-2 doses.
Due to the long half-life, the drug can be used every other day or take a break in taking 2 days a week (taking a therapeutic dose of the drug for 5 days a week, with a break for 2 days at the end of the week). When treating the elderly, it is recommended to use the smallest loading and maintenance doses of Amiodarone.
The average therapeutic single dose is 200 mg, the average therapeutic daily dose is 400 mg. The maximum single dose is 400 mg, the maximum daily dose is 1200 mg.

Side effect

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 (according to the available data, it is not possible to determine the frequency).
On the part of the cardiovascular system: often - moderate bradycardia (dose-dependent); infrequently - sinoatrial and atrioventricular blockade of various degrees, proarrhythmogenic effect; very rarely - severe bradycardia, sinus node arrest (in patients with sinus node dysfunction and elderly patients); frequency unknown - ventricular tachycardia of the "pirouette" type, progression of symptoms of chronic heart failure (with prolonged use).
From the digestive system: very often - nausea, vomiting, decreased appetite, dullness or loss of taste, metallic taste in the mouth, a feeling of heaviness in the epigastrium, an isolated increase in the activity of "hepatic" transaminases; often - acute toxic hepatitis with an increase in the activity of "hepatic" transaminases and / or jaundice, including the development of liver failure; very rarely - chronic liver failure.
From the respiratory system: often - interstitial or alveolar pneumonitis, bronchiolitis obliterans with pneumonia, pleurisy, pulmonary fibrosis; very rarely - bronchospasm in patients with severe respiratory failure (especially in patients with bronchial asthma), acute respiratory syndrome; frequency unknown - pulmonary hemorrhage.
On the part of the organ of vision: very often - microdeposits in the corneal epithelium, consisting of complex lipids, including lipofuscin (complaints about the appearance of a colored halo or blurred contours of objects in bright light); very rare - optic neuritis / optic neuropathy.
From the side of metabolism: often - hypothyroidism, hyperthyroidism; very rarely - syndrome of impaired secretion of antidiuretic hormone.
From the side of the skin: very often - photosensitivity; often - grayish or bluish skin pigmentation (with prolonged use), disappears after stopping the drug; very rarely - erythema (with simultaneous radiation therapy), skin rash, exfoliative dermatitis (the relationship with the drug has not been established), alopecia; frequency unknown - urticaria.
From the nervous system: often - tremor and other extrapyramidal disorders, sleep disturbance; infrequently - peripheral neuropathy and / or myopathy; very rarely - cerebellar ataxia, benign intracranial hypertension, headache.
Others: frequency unknown - angioedema, formation of granulomas, including bone marrow granulomas; very rarely - vasculitis, epididymitis, impotence (the connection with taking the drug has not been established), thrombocytopenia, hemolytic and aplastic anemia.

In case of adverse reactions, it is necessary to discontinue the use of the drug and consult a doctor.
If any of the side effects indicated in the instructions are aggravated or you notice any other side effects that are not listed in the instructions, inform your doctor.

Overdose

Symptoms: bradycardia, AV block, ventricular tachycardia of the "pirouette" type, paroxysmal tachycardia of the "pirouette" type, aggravation of symptoms of existing CHF, impaired liver function, cardiac arrest.
Treatment: gastric lavage, intake of activated charcoal, symptomatic therapy (for bradycardia - beta-adrenostimulants, atropine or installation of a pacemaker; for tachycardia of the "pirouette" type - intravenous administration of magnesium salts, cardiac stimulation). Hemodialysis is ineffective.

Interaction with other medicinal products

Contraindicated combinations: the risk of developing polymorphic ventricular tachycardia of the "pirouette" type (arrhythmia characterized by polymorphic complexes that change the amplitude and direction of excitation through the ventricles relative to the isoline (electric systole of the heart): class IA antiarrhythmics (quinidine, hydroquinidine, disopyramide, procainamide), class III (dofetilide , ibutilide, bretilium tosylate), sotalol; bepridil, vincamine, phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazii, fluphenazii), benzamides (amisulpride, sultoprid, sulpirofen, seropridone), buroperidinol pimozide; tricyclic antidepressants, cisapride, macrolides (erythromycin IV, spiramycin), azoles, antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine (parenteral), diphemanilone, methylastinol including moxifloxacin).
Combinations not recommended: beta-blockers, blockers of "slow" calcium channels (verapamil, diltiazem) - the risk of impaired automatism (pronounced bradycardia) and conduction; laxatives that stimulate intestinal motility - the risk of developing ventricular tachycardia of the "pirouette" type against the background of hypokalemia caused by laxatives.
Combinations requiring caution: diuretics that cause hypokalemia, amphotericin B (intravenously), systemic glucorticosteroids, tetracosactide - the risk of ventricular arrhythmias, incl. ventricular tachycardia of the "pirouette" type; procainamide - the risk of developing side effects of procainamide (amiodarone increases the plasma concentration of procainamide and its metabolite -N-acetylprocainamide).
Indirect anticoagulants (warfarin) - amiodarone increases the concentration of warfarin (the risk of bleeding) by inhibiting the isoenzyme CYP2C9; cardiac glycosides - violation of automatism (severe bradycardia) and AV conduction (increased concentration of digoxin).
Esmolol - violation of contractility, automatism and conduction (suppression of compensatory reactions of the sympathetic nervous system). Phenytoin, phosphenytoin - the risk of developing neurological disorders (amiodarone increases the concentration of phenytoin due to inhibition of the CYP2C9 isoenzyme).
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, HMG-CoA reductase inhibitors) - amiodarone increases their concentration and / or the risk of developing their pharmacodynamic effects in case of toxicity co-administration of amiodarone with high doses of simvastatin increases the likelihood of developing myopathy).
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.
Inhaled drugs for general anesthesia - the risk of developing bradycardia (resistant to the administration of atropine), acute respiratory distress syndrome, incl. fatal, the development of which is associated with high oxygen concentrations, the risk of lowering blood pressure, cardiac output, conduction disturbances.
Radioactive iodine - amiodarone (contains iodine in its composition) can interfere with the absorption of radioactive iodine, which can distort the results of a radioisotope study of the thyroid gland.
Rifampicin and St. John's wort preparations (strong inducers of the isoenzyme CYP3A4) reduce the concentration of amiodarone in the blood plasma. Inhibitors of HIV - protease (inhibitors of the isoenzyme CYP3A4) - can increase plasma concentrations of amiodarone.
Photosensitizing drugs have an additive photosensitizing effect.
Clopidogrel - a decrease in its plasma concentration is possible; dextromethorphan (a substrate of CYP3A4 and CYP2D6 isoenzymes) - its concentration may be increased (amiodarone inhibits the CYP2D6 isoenzyme). Dabigatran - an increase in its concentration in blood plasma when used simultaneously with amiodarone.

special instructions

Care should be taken when prescribing the drug to patients with heart failure, liver disease, hypokalemia, porphyria, and elderly patients.
Before starting treatment and every 6 months during therapy, it is recommended to check the function of the thyroid gland, the activity of "hepatic" transaminases and conduct an X-ray examination of the lungs and consult an ophthalmologist. Control ECGs should be taken every 3 months.
It should be borne in mind that against the background of the use of Amiodarone, the results of determining the concentration of thyroid hormones (triiodothyronine, thyroxine, thyroid-stimulating hormone) may be distorted.
With a heart rate below 55 beats / min, the drug must be temporarily canceled.
When using the drug Amiodarone, changes in the ECG are possible: lengthening of the QT interval with the possible appearance of a U wave. When atrioventricular block II and III degree, sinoatrial blockade, and also blockade of the bundle of His bundle appear, treatment with Amiodarone should be stopped immediately. If canceled, recurrence of heart rhythm disturbances is possible. After discontinuation of the drug, the pharmacodynamic effect persists for 10-30 days. Before carrying out surgical interventions, as well as oxygen therapy, it is necessary to warn the doctor about the use of Amiodarone, since there have been rare cases of acute respiratory distress syndrome in adult patients in the postoperative period.
To avoid the development of photosensitivity, patients should avoid exposure to the sun. The deposition of lipofuscin in the corneal epithelium diminishes on its own when the dose is reduced or amiodarone is withdrawn. Skin pigmentation decreases after discontinuation of the drug and gradually (within 1-4 years) completely disappears. After stopping treatment, spontaneous normalization of thyroid function is usually observed.

Information about the possible impact on the ability to drive vehicles, mechanisms

During the period of treatment, one should refrain from driving and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

200 mg tablets.
10 tablets in a blister strip packaging.
2, 3 blisters together with instructions for use are placed in a carton box.

Storage conditions

In a dark place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Shelf life

2 years.
Do not use after the expiration date printed on the package.

Vacation conditions

Dispensed by prescription.

Marketing Authorization Holder / Manufacturer

CJSC Altayvitamins, 659325,
Russia, Altai Territory, Biysk, st. Factory, 69

Peace 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 disease, with ineffectiveness and inability to use other therapy against arrhythmias;
documented attacks of recurrent persistent paroxysmal supraventricular tachycardia in patients with Wolff-Parkinson-White syndrome;
atrial fibrillation and atrial flutter.

How do I take the pills?

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

Loading dose

In the hospital, the initial dosage, which is divided into several times of admission, 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, is 600-800 mg per day upon reaching a total dose of 10 g for 10-14 days.

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

If the drug is used for a long period of time, you can take a break and drink 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

It is produced in the form of white tablets of a round, flat-cylindrical shape, with a one-sided bevel and a risk.

Amiodarone hydrochloride - 1 tab. 200 mg.

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

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

Beneficial features

The drug has the following properties:

antiarrhythmic;
antianginal;
coronary dilating;
alpha and beta adrenergic blocking;
thyrotropic;
hypotensive.

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

The antianginal effect is explained by the coronary expansion effect, a decrease in 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. The sensitivity to stimulation of the sympathetic nervous system and the resistance of the coronary vessels decrease, the coronary blood flow increases, the 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% + isolated cases), the frequency is unknown.

The cardiovascular system:

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

Digestive system:

very often - vomiting and nausea, impaired appetite, impaired taste, a feeling of heaviness in the stomach, an increase in the activity of "hepatic" transaminases;
often - toxic hepatitis of the acute stage (liver failure is possible, including fatal);
very rarely - chronic liver failure, including fatal.

Respiratory system:

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

Senses:

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

Endocrine system:

often - an increase in T4 with a decrease in T3. With prolonged use, hypothyroidism may occur, less often - hyperthyroidism (the drug is canceled);
very rarely - impaired secretion of ADH.

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.

Very rarely there is epididymitis, decreased potency, vasculitis.

Overdose

Overdose symptoms:

lowering blood pressure;
sinus bradycardia;
atrioventricular block;
disruption of the liver;
worsening symptoms of heart failure;
heart failure.

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

In the case of bradycardia, it is possible to use beta-adrenostimulants, atropine, or the installation of a pacemaker. In pritachycardia, 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-beam blockade without a pacemaker;
arterial hypotension;
dysfunction of the thyroid gland;
pregnancy and lactation;
simultaneous administration with medications that increase the QT interval and cause the occurrence of paroxysmal tachycardia (quinidine, disopyramide, procainamide, dofetilide, sotalol, ibutilide, bretilium tosylate, ibutilide, sotalol and other non-antiarrhythmic agents vincamine, bepridil, some neuroleptics, antipsychotics, antipsychotics ; erythromycin, spiramycin; azoles; quinine, mefloquine, chloroquine, halofantrine; pentamidine; diphemanil methyl sulfate; astemizole, mizolastine, terfenadine and fluoroquinolones;
hypokalemia and hypomagnesemia;
congenital (acquired) lengthening of the QT interval;
interstitial lung disease;
taking monoamine oxidase inhibitors in the complex;
children under 18;
lactose intolerance, lack of lactase (glucose-galactose malabsorption);
high sensitivity to iodine and amiodarone, to other components of the drug.

It can be taken with caution in case of: liver failure, bronchial asthma, elderly patients, chronic heart failure, AV blockade of the 1st 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 (amisulprid, galoprid, sulpiridom, seroferidinol) pimozide; tricyclic antidepressants, cisapride, macrolides (intravenous erythromycin, spiramycin), azoles; antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine (parenteral), diphemanil methyl sulfate, mizolastine, astemizole, terfenadine, fluoroquinolones (including moxifloxacin).

Dosage Form: & nbsp

pills

Composition:

Active substance:

Amiodarone hydrochloride - 200.0 mg

Excipients:

Lactose monohydrate - 100.0 mg, potato starch - 60.6 mg, microcrystalline cellulose - 24.0 mg, talc - 7.0 mg, povidone (polyvinylpyrrolidone) - 4.8 mg, calcium stearate - 3.6 mg.

Description:

Tablets, white or white with a creamy shade, flat-cylindrical with a scored and beveled.

Pharmacotherapeutic group:Antiarrhythmic agent ATX: & nbsp

C.01.B.D.01 Amiodarone

Pharmacodynamics:

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

Blocksnon-activated potassium (to a lesser extent - calcium and sodium) channels of cell membranes of cardiomyocytes. 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, inhibits the atrioventricular(AV) carrying out (effect of class IV antiarrhythmics).

Has the properties of a non-competitive blocker of alpha and beta adrenergic receptors.

The antiarrhythmic effect of amiodarone is associated with its ability to pull out an increase in the duration of the action potential of cardiomyocytes and the effective refractory period of the atria and ventricles of the heart, AV node, His bundle, Purkinje fibers, which is accompanied by a decrease automatism of the sinus node, slowing down AV-conduction, reducing the excitability of cardiomyocytes.

Antiangianalth effect is due to a decrease in myocardial oxygen demand due to a decrease in the heart rate (HR) and a decrease in the resistance of the coronary arteries, which leads to an increase in coronary blood flow. Does not significantly affect systemic blood pressure (BP).

Its structure is similar to thyroid hormones. The iodine content is about 37% of its molecular weight. Influences the exchange of thyroid hormones, inhibits the conversion of thyroxine (T4) to triiodothyronine (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 blood plasma for 9 months after stopping it).

Pharmacokinetics:

Suction

After oral administration, it is slowly absorbed from the gastrointestinal tract, bioavailability is 35-65%. It is detected in the blood after 1 / 2-4 hours. The maximum concentration in the blood after taking a single dose is observed after 2-10 hours. The therapeutic plasma concentration range is 1-2.5 mg / l (but when determining the dose, it is necessary to have a clinical picture in the vein) ... Time to reach steady-state concentration(TCss) - from one to several months (depending on individual characteristics).

Distribution

The volume of distribution is 60 liters, which indicates an intensive distribution in the tissues. It has a high fat solubility, in high concentrations it is found in adipose tissue and organs with good blood supply (concentration in adipose tissue, liver, kidneys, myocardium is higher than in blood plasma by 300, 200, 50 and 34 times, respectively). 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%), secreted in breast milk (25% of the dose received by the mother). Communication with blood plasma proteins - 95% (62% - with albumin, 33.5% - with beta-lipoproteins).

Metabolism

Metabolized in the liver; the main metabolite, desethylamiodarone, which has similar pharmacological properties, 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, the concentration of iodine can reach 60-80% of the concentration of amiodarone. It is a carrier of organic anions, an inhibitor of P-glycoprotein and isoenzymesCYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7, CYP1A1, CYP1A2, CYP2C19, CYP2A6, CYP2B6, CYP2C8 in the liver.

Withdrawal

Given the ability to cumulate and the associated large variability of pharmacokinetic parameters, the data on the half-life (T1 / 2) are contradictory. Excretion of amiodarone after oral administration is carried out in 2 phases: the initial period - 4-21 hours, in the second phase T1 / 2 - 25-110 days (on average 20-100 days). After prolonged oral administration, the average T1 / 2 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 more than 4 months) ...

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

Indications:

Prevention of sudden death due to arrhythmia in high-risk patients: patients after a recent myocardial infarction with the number of ventricular extrasystoles more than 10 / h, with clinical signs of chronic heart failure (CHF) and left ventricular ejection (LV) fraction less than 40%.

Contraindications:

Hypersensitivity to any of the components of the drug or iodine; sick sinus syndrome (sinus bradycardia and sinoatrial blockade in the absence of a pacemaker (risk of stopping the sinus node); atrioventricular block II-III degree, two- and three-beam blockade (in the absence of a pacemaker); hypothyroidism, hyperthyroidism; severe arterial hypotension; lactic insufficiency lactase, glucose-galactose mapabsorption syndrome; hypokalemia, hypomagnesemia; interstitial lung disease; pregnancy, breastfeeding; concomitant use of monoamine oxidase inhibitors, drugs that prolong the QT interval, congenital or acquired lengthening of the QT interval; age up to 18 years. Interaction with other medicinal products ".

Carefully:

If you have one of the listed diseases, be sure to consult your doctor before using the drug.

Pregnancy and lactation:It should not be used during pregnancy, since during this period the thyroid gland of the newborn begins to accumulate, and the use of Amiodarone during this period can provoke the development of hypothyroidism due to an increase in the concentration of iodine. Application during pregnancy and lactation is possible only with life-threatening rhythm disturbances with the ineffectiveness of other antiarrhythmic therapy, since the drug causes dysfunction of the fetal thyroid gland. crosses the placenta (10-50%), is secreted in breast milk (25% of the dose received by the mother), therefore the drug is contraindicated for use during lactation. If it is necessary to use it during lactation, then breastfeeding should be canceled. Method of administration and dosage:

The average therapeutic single dose is 200 mg, the average therapeutic daily dose is 400 mg. The maximum single dose is 400 mg, 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 (according to the available data, it is not possible to determine the frequency).

With side of the cardiovascular system : often - moderate bradycardia (dose-dependent); infrequently - sinoatrial and atrioventricular blockade of various degrees, proarrhythmogenic effect; very rarely - severe bradycardia, sinus node arrest (in patients with sinus node dysfunction and elderly patients); frequency unknown - ventricular tachycardia of the "pirouette" type, progression of symptoms of chronic heart failure (with prolonged use).

From the digestive system: very often - nausea, vomiting, decreased appetite, dullness or loss of taste, metallic taste in the mouth, a feeling of heaviness in the epigastrium, an isolated increase in the activity of "hepatic" transaminases; often - acute toxic hepatitis with increased activity of "hepatic" transaminases and / or jaundice, including the development of liver failure; very rarely - chronic liver failure.

From the respiratory system: often interstitial or alveolar pneumonitis, bronchiolitis obliterans with pneumonia, pleurisy, pulmonary fibrosis; very rarely - bronchospasm in patients with severe respiratory failure (especially in patients with bronchial asthma), acute respiratory syndrome; frequency unknown - pulmonary hemorrhage.

On the part of the organ of vision: very often - microdeposits in the corneal epithelium, consisting of complex lipids, including lipofuscin (complaints about the appearance of a colored halo or blurred contours of objects in bright light); very rare - optic neuritis / optic neuropathy.From the side of metabolism:often - hypothyroidism, hyperthyroidism; very rarely - syndrome of impaired secretion of antidiuretic hormone.

From the side of the skin: very often - photosensitivity; often - grayish or bluish skin pigmentation (with prolonged use), disappears after stopping the drug; very rarely - erythema (with simultaneous radiation therapy), skin rash, exfoliative dermatitis (no connection with the drug has been established), alopecia; frequency unknown - urticaria.

From the nervous system: often - tremor and other extrapyramidal disorders, sleep disturbance; infrequently - peripheral neuropathy and / or myopathy; very rarely - cerebellar ataxia, benign intracranial hypertension, headache.

Others: frequency unknown - angioedema, education granulomas, including bone marrow granulomas; very rarely - vasculitis, epididymitis, impotence (the connection with the drug intake has not been established), trambocytopepia, hemolytic and aplastic anemia.

If adverse reactions occur, it is necessary to discontinue the use of the drug and consult a doctor.

If any of the side effects indicated in the instructions are aggravated or you notice any other side effects not listed in instructions, tell your doctor.

Overdose:

Symptoms: bradycardia, AV- blockade, ventricular tachycardia of the "pirouette" type, paroxysmal tachycardia of the "pirouette" type, aggravation of the symptoms of theXCH, impaired liver function, cardiac arrest.

Treatment: gastric lavage, intake of activated charcoal, symptomatic therapy (for bradycardia - beta-adrenostimulants, or installation of a pacemaker; for tachycardia of the "pirouette" type - intravenous administration of magnesium salts, cardiac stimulation). Hemodialysis is ineffective.

Interaction:

Contraindicated combinations: the risk of developing polymorphic ventricular tachycardia of the "pirouette" type (arrhythmia characterized by polymorphic complexes that change the amplitude and direction of excitation through the ventricles relative to the isoline (cardiac electrical systole): class IA antiarrhythmics (, hydroquinidine, disopyramide,), class III (dofetilide, ibutilide ,),; bepridil, phenothiazines (, shamemazin,), benzamides (, sultopride, veraliirid), butyrophenones (,), pimozide; tricyclic antidepressants, cisapride, macrolides (i / v,), azoles, antimalarial drugs (quinine, halofantrine , lumefantrine); pentamidine (parenteral), diphemanil methyl sulfate, mizolastine, teefenadine, fluoroquinolones (including).

Combinations not recommended: beta-blockers, blockers"slow" calcium channels (,) - the risk of violation of automatism (pronounced bradycardia) and conduction; laxatives that stimulate intestinal motility - the risk of developing ventricular tachycardia of the "pirouette" type against the background of hypokalemia caused by laxatives.

Combinations requiring caution: diuretics that cause hypokalemia, amphotericin B (intravenously), systemic glucocorticosteroids, - the risk of developing ventricular rhythm disturbances, incl. pirouette-type ventricular tachycardia; - the risk of developing side effects of procainamide (increases the plasma concentration of procainamide and its metabolite - N-acetyl procainamide).

Indirect anticoagulants () - increases the concentration of warfarin (the risk of bleeding) by inhibiting the isoenzyme CYP2C9; cardiac glycosides - a violation of automatism (pronounced bradycardia) and AV-conduction (an increase in the concentration of digoxin).

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

Phenytoin, phosphenytoin - the risk of developing neurological disorders (increases the concentration of phenytoin due to inhibition of the CYP2C9 enzyme).

Flecainide - increases its concentration (by inhibiting the enzyme CYP2D6).

Medicines metabolized with the participation of the CYP3A4 isoenzyme (eg, miidazolam, triazolam, dihydroergotamine, ergotamine, HMG-CoA reductase inhibitors) - increases their concentration (the risk of developing their toxicity and / or increasing pharmacodynamic effects when taking simivodarone with high doses development of myopathy).

Orlistat reduces the concentration of amiodarone and its active metabolite; onidine, cholinesterase inhibitors (eg, tacrine, ambenonium chloride, pyridoshygmin, neoshygmin), - the risk of developing severe bradycardia.

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

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

Radioactive - (contains in its composition) can disrupt the absorption of radioactive iodine, which can distort the results of a radioisotope study of the thyroid gland.

Rifampicin and St. John's wort preparations (strong inducers and: CYP2A4 enzyme) reduce the concentration of amiodarone in the blood plasma.

Inhibitors of HIV - protease (inhibitors of the isoenzyme CYP3A4) - can increase plasma concentrations of amiodarone.

Photosensitizing drugs have an additive photosensitizing effect.

Clopidogrel - a decrease in its plasma concentration is possible; dextromethorphan (substrate of CYP3A4 and CYP2D6 isoenzymes) - its concentration may increase (inhibits the CYP2D6 isoenzyme). Dabigagran - an increase in its concentration in blood plasma when used simultaneously with amiodarone.

Special instructions:

Care should be taken when prescribing the drug to patients with heart failure, liver disease, hypokalemia, porphyria, and elderly patients.

Before starting treatment and every 6 months during therapy, it is recommended to check the function of the thyroid gland, the activity of "hepatic" transaminases and conduct an X-ray examination of the lungs and consult an ophthalmologist. Control ECGs should be taken every 3 months. It should be borne in mind that against the background of the use of Amiodarone, the results of determining the concentration of thyroid hormones (triiodothyronine, thyroxine, thyroid-stimulating hormone) may be distorted.

With a heart rate below 55 in d / m, the drug must be temporarily canceled.

When using the drug, changes in the ECG are possible: lengthening of the intervalQTwith the possible appearance of a toothU. When atrioventricular block of II and III degrees, sinoatrial blockade, and also blockade of the bundle of His, treatment with the drug should be stopped immediately. If canceled, recurrence of heart rhythm disturbances is possible. After discontinuation of the drug, the pharmacodynamic effect persists for 10-30 days. Before carrying out surgical interventions, as well as oxygen therapy, it is necessary to warn the doctor about the use of the drug, since there have been rare cases of acute respiratory distress syndrome in adult patients in the postoperative period.

InTo avoid the development of photosensitivity, patients should avoid exposure to the sun. The deposition of lipofuscin in the corneal epithelium decreases on its own when the dose is reduced or amiodarone is withdrawn. Skin pigmentation decreases after discontinuation of the drug and gradually (within 1-4 years) completely disappears. After stopping treatment, spontaneous normalization of thyroid function is usually observed.

Impact on the ability to drive vehicles Wed and fur .:

During the period of treatment, one should refrain from driving and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form / dosage:200 mg tablets. Package:

10 tablets in a blister strip packaging.

2, 3 blisters together with instructions for use are placed in a carton box.

Storage conditions:

In a dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Tradename: Amiodarone.

International non-proprietary name: Amiodarone / Amiodarone.

Release form: tablets 200 mg.

Description: tablets of white or almost white color, flat-cylindrical, with a score and a chamfer.

Composition: one tablet contains: active substance- amiodarone hydrochloride 200 mg; Excipients: lactose monohydrate, potato starch, povidone, calcium stearate.

Pharmacotherapeutic group: class III antiarrhythmic agent. Amiodarone.

ATX code - С01BD01.

Relapse prevention
Life-threatening ventricular arrhythmias, including ventricular tachycardia and ventricular fibrillation (treatment should be started in hospital with close cardiac monitoring).
Supraventricular paroxysmal tachycardia:
- documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients with organic heart diseases;
- documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients without organic heart disease, when antiarrhythmic drugs of other classes are ineffective or there are contraindications to their use;
- documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome.
Atrial fibrillation (atrial fibrillation) and atrial flutter.
Prevention of sudden arrhythmic death in high-risk patients
Patients after a recent myocardial infarction with more than 10 ventricular extrasystoles in 1 hour, clinical manifestations of chronic heart failure and a reduced left ventricular ejection fraction (less than 40%).
Amiodarone can be used to treat rhythm disturbances in patients with coronary artery disease and / or impaired left ventricular function.

Hypersensitivity to iodine, amiodarone or excipients of the drug.
Lactose intolerance (lactase deficiency), glucose-galactose malabsorption syndrome (the drug contains lactose).
Syndrome of weakness of the sinus node (sinus bradycardia, sinoatrial blockade), except for the cases of their correction by an artificial pacemaker (danger of "stopping" the sinus node).
Atrioventricular block II-III degree, in the absence of an artificial pacemaker (pacemaker).
Hypokalemia, hypomagnesemia.
The combination with drugs that can lengthen the QT interval and cause the development of paroxysmal tachycardia, including ventricular "pirouette" tachycardia (see section "Interaction with other medicinal products"):
- antiarrhythmic drugs: class IA (quinidine, hydroquinidine, di-zopyramide, procainamide); class III antiarrhythmics (dofetilide, ibutilide, bretilium tosylate); sotalol;
- other (non-antiarrhythmic) drugs such as bepridil; vincamine; some antipsychotics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sulpride, tiapride, veraliprid), butyrophenones (droperidol), sertinimazine; cisapride; tricyclic antidepressants; macrolide antibiotics (in particular, intravenous erythromycin, spiramycin); azoles; antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine); pentamidine for parenteral administration; diphemanil methyl sulfate; mizolastine; astemizole, terfenadine; fluoroquinolones.
Congenital or acquired lengthening of the QT interval.
Thyroid dysfunction (hypothyroidism, hyperthyroidism).
Interstitial lung disease.
Pregnancy (see "Use during pregnancy and lactation").
Lactation period (see "Use during pregnancy and lactation").
Age up to 18 years (efficacy and safety have not been established).

The drug should only be taken as directed by a doctor!
Amiodarone tablets are taken orally, before meals and washed down
enough water.
Loading ("saturating") dose
Various saturation schemes can be used.
In a hospital, the initial dose, divided into several doses, ranges from 600-800 mg (up to a maximum of 1200 mg) per day until a total dose of 10 g is reached (usually within 5-8 days).
On an outpatient basis, the initial dose, divided into several doses, is from 600 to 800 mg per day until a total dose of 10 g is reached (usually within 10-14 days).
The maintenance dose can vary in different patients from 100 to 400 mg / day. The minimum effective dose should be used in accordance with the individual therapeutic effect.
Since Amiodarone has a very long half-life, it can be taken every other day or interrupted 2 days a week.
The average therapeutic single dose is 200 mg.
The average therapeutic daily dose is 400 mg.
The maximum single dose is 400 mg.
The maximum daily dose is 1200 mg.

Diseases of the cardiovascular system rank first in terms of prevalence among the pathologies of all systems of the human body. From this article you can find out what Amiodarone consists of, how the drug works, whether it can help with heart rhythm disturbances, the features of its use, and what is the cost of the drug.

Composition and form of release

Amiodarone is a class 3 antiarrhythmic drug (potassium channel blockers) characterized by an increase in the duration of the repolarization process and an increase in the action potential.

The preparation contains an active substance - amiodarone hydrochloride, as well as additional elements:

magnesium stearate;
lactose monohydrate;
corn starch;
croscarmellose sodium;
anhydrous colloidal silicon dioxide.

The drug is produced in the form of white flat-cylindrical tablets with a risk, weighing 200 mg.

In addition, you can find Amiodarone in ampoules of 3 ml of a 5% solution.

Mechanism of action

Amiodarone is characterized by a decrease in the increased contractility of the myocardium. In addition, the drug reduces resistance in the coronary vessels, thereby increasing coronary blood flow. Due to the vasodilating effect on peripheral arterial and venous vessels, it leads to a decrease in heart rate, a decrease in blood pressure.

The amount of creatine phosphate and glycogen increases as a result of taking the drug, which proves the positive effect of Amiodarone on energy metabolism.

In addition to the block of potassium channels, amiodarone is also characterized by a blocking effect on:

sodium channels;
beta-adrenergic receptors;
calcium channels (least expressed).

In general, the drug is characterized by a mechanism of action that combines the properties of antiarrhythmic drugs of the first, second and fourth groups, but still the basis of the action of Amiodarone is to reduce the automatism, conductivity and excitability of the sinus-atrial and atrioventricular nodes.

The antiarrhythmic effect of the drug develops slowly. Long-term use of the drug is accompanied by an increase in the duration of the action potential, the effective refractory period of the atria, atrioventricular node and ventricles. The mechanism for increasing the duration of the action potential is associated with a block of potassium channels, which leads to a decrease in the release of the corresponding ions from cardiomyocytes. At the same time, repolarization will slow down. On the electrocardiogram, the QT interval is lengthened.

Pharmacokinetics

After oral administration, the drug is absorbed in the organs of the gastrointestinal tract by 50%. It is usually administered once a day. The effect occurs several weeks after taking the pills. When it enters the liver, it is metabolized.

For Amiodarone, material accumulation is pronounced, which is the reason for the slow elimination of the drug through the intestines, into which it enters along with bile. The active substance of the drug accumulates in the liver itself unchanged or as metabolites, as well as in the lungs and spleen and is deposited in adipose tissue. The drug has a high level of affinity for blood plasma proteins - 96%.

When using Amiodarone in the form of a solution for slow (drip) intravenous administration, it is possible to reduce the time for the effects of the drug to occur to 1-2 hours after administration.

Indications for use

The drug is used to treat:

Supraventricular tachycardia - leads to a decrease or slowdown.
Coronary heart disease.
Pathologies that lead to impaired functioning of the left ventricle - as a complex therapy, since it has little effect on other diseases and helps to normalize the conduction and contractility of the myocardium.

The effectiveness of the drug (as a clinical form of coronary heart disease) is to reduce myocardial oxygen demand.

Amiodarone is used as a prophylactic agent for relapses:

, which threatens the patient's life. In this case, treatment should be started in stationary conditions or if there is a possibility of constant monitoring of the patient's condition.
Symptomatic ventricular tachycardia, which leads to a person's disability.
that requires treatment. It is most often used when other antiarrhythmic drugs are ineffective.
Ventricular fibrillation.

Terms of use

Initial therapy is to take 1 tablet 200 mg 3 times a day. It is recommended to use Amiodarone before meals without chewing.

In some cases, the patient needs to prescribe a higher dose, which can be 4-5 tablets per day. Moreover, such therapy is short-term, accompanied by regular electrocardiographic monitoring (the method of daily ECG monitoring according to Holter can be used).

When switching to supportive therapy, the patient is prescribed the minimum dose at which the desired effect will be observed. Depending on the severity of the case, the patient's reaction to the drug, the dosage can be from half a tablet to 2 tablets per day.

Considering that amiodarone is characterized by a pronounced material cumulation, the agent is taken 5 days a week with a break of 2 days.

Prescribing the drug for children, pregnant and breastfeeding women

The active substance of the drug penetrates the histohematogenous barriers, including the transplacental, blood-brain. In this regard, Amiodarone is prohibited from prescribing to pregnant women. The drug has a negative effect on the thyroid gland of the fetus. The drug can be used during pregnancy only in cases where the positive effect for the mother significantly outweighs the risk of complications in the child.

If a woman took Amiodarone before the fact of pregnancy is established, the drug is canceled and the patient is notified of the possible consequences.

The drug is strictly contraindicated during breastfeeding, since the active substance penetrates the baby along with milk and causes irreversible disorders. If a woman suffers from tachycardia, which threatens her health and life, Amiodarone can be prescribed only if the child is transferred to artificial feeding.

The drug is not prescribed for children under the age of 18.

Contraindications

In addition to being under age, during pregnancy and breastfeeding in women, contraindications to the use of Amiodarone include:

hypersensitivity to the drug, its components, iodine;
sinoatrial heart block in the absence of an endocardial pacemaker as an artificial heart rate driver;
sick sinus syndrome without a pacemaker in a patient - associated with a high risk of stopping the sinus node;
violation of atrioventricular conduction of severe development without a pacemaker in a patient;
dysfunction of the thyroid gland.

Side effects

Among the most common effects in patients are possible:

dyspeptic symptoms;
excessive decrease in heart rate;
atrioventricular block;
reversible deposition of microcrystals in the cornea;
skin pigmentation, in which the human cover will take on a gray-blue color;
photodermatitis (the patient has an increased sensitivity to ultraviolet radiation, therefore, prolonged exposure to the sun should be avoided during therapy with Amiodarone);
dysfunction of the thyroid gland;
fibrosis of the lungs;
neuropathy of the optic nerve, which can progress to complete blindness;
syndrome of inadequate secretion of antidiuretic hormone - observed in rare cases, most often when used together with drugs that cause a significant decrease in the level of sodium ions in the blood (hyponatremia);
bronchospasm is the most common complaint of patients who suffer from acute respiratory failure and bronchial asthma;
epididymitis or inflammatory lesion of the epididymis - a side effect of the drug, the connection with which is not clear enough at the moment; can lead to impotence;
kidney damage, accompanied by an increase in creatinine clearance;
angioedema;
hemolytic or aplastic anemia, thrombocytopenia.

The use of the drug in doses exceeding therapeutic ones often leads to the occurrence of neurological disorders, among which paresthesias and tremors are most common in patients.

When treating with the use of Amiodarone, it should also be borne in mind that side effects, even after discontinuation of the drug, can persist for quite a long time. Pigmentation caused by taking the drug disappears only after 1-2 years after long-term use.

Compatibility with other drugs and alcohol

When amiodarone is used together with other antiarrhythmic drugs, a better therapeutic effect can be provided, especially in cases where drugs belong to different classes or groups. But the treatment process requires more careful monitoring of the patient's response and cardiac activity indicators.

It is contraindicated to use Amiodarone with drugs of the same group, such as Ornid, Sotalol and Dofetilide, as this can cause an increase in the frequency and increase in the manifestation of side effects.

It should also be remembered that the use as a combination therapy of several drugs that can cause torsades de pointes is prohibited. These drugs include Amiodarone, Sotalol, quinidine compounds, Disopyramide. Also, the risk of pathology increases with a decrease in the level of potassium in the blood, which is typical for many diuretics, with bradycardia, congenital or acquired prolonged QT interval.

Among the strict contraindications for joint use with Amiodarone are:

class Ia antiarrhythmics (Quinidine, Hydroquinidine);
class III antiarrhythmic drugs;
arsenic compounds, Cisapride, Vincamycin, Toremifen, Spiramycin, Erythromycin (especially with enteral administration of drugs).

All of the above combinations lead to an increase and increase in side effects from the heart, while heart rhythm disturbances are more common.

The concurrent use of Amiodarone with the following agents should be strictly controlled by the attending physician:

Cyclosporine- a drug that belongs to cyclic polypeptide antibiotics and immunosuppressants. The drugs in this group are characterized by significant nephrotoxicity, which, when used together with Amiodarone, is more frequent.
Diltiazem in the form of a solution for injection. The patient has an increased risk of developing bradycardia and atrioventricular block.
Antipsychotics that can cause pirouette tachycardia. These funds include: Amisulpride, Chlorpromazine, Tsiamemazin, Droperidol, Haloperidol. In addition, such combinations can lead to other ventricular arrhythmias.
Methadone The risk of heart rhythm disturbances is increased.
Verapamil in the form of a solution for injection. Increases the manifestation of side effects of drugs, especially from the heart - the occurrence of an atrioventricular block in the patient, a decrease in heart rate.

When amiodarone is used together with Pilocarpine, the patient needs to monitor the electrocardiogram, since the combined effect of both drugs often leads to a slowdown in the heart rate.

It is not recommended to consume alcoholic beverages during treatment. This is due to the effect of ethanol on the tone of peripheral vessels and the effect of alcohol on the level of blood pressure.

Where can you buy the drug?

Amiodarone can be purchased at these pharmacies:

Planet Health;
Neopharm;
Cosmoteque;
Lighthouse;
Melody of health;
Samson-Pharma;
Pharmacy IFC.

Price the drug fluctuates in the region of 89-208 rubles.

The drug Amiodarone has a rather wide range of contraindications and side effects, but with strict adherence to the rules of admission, ECG monitoring, hemodynamic parameters and general health, the patient gets an excellent chance to cope with severe pathologies and cardiac arrhythmias.