Amiodarone
Amiodarone: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Amiodaron
ATX code: C01BD01
Active ingredient: Amiodarone (Amiodarone)
Manufacturer: Balkanpharma-Dupnitza (Bulgaria), North Star, Organic, Biocom CJSC, AVVA-RUS, Obolenskoe FP (Russia)
Description and photo update: 2019-16-09
Prices in pharmacies: from 65 rubles.
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Amiodarone is an antiarrhythmic drug.
Release form and composition
The drug is produced in the form of tablets containing 200 mg of amiodarone hydrochloride and auxiliary substances: milk sugar, corn starch, alginic acid, low molecular weight povidone, magnesium stearic acid.
Pharmacological properties
Pharmacodynamics
Amiodarone is a class III antiarrhythmic drug. It also has alpha and beta adrenergic blocking, antianginal, antihypertensive and coronary dilating effects.
The drug blocks non-activated potassium channels in the cell membranes of cardiomyocytes. To a lesser extent, it acts on sodium and calcium channels. By blocking inactivated "fast" sodium channels, it produces the effects that are characteristic of class I antiarrhythmic drugs. Amiodarone causes bradycardia, inhibiting the slow depolarization of the sinus node cell membrane, and also inhibits atrioventricular conduction (the effect of class IV antiarrhythmic drugs).
The antiarrhythmic effect of the drug is due to its ability to increase the duration of the action potential of cardiomyocytes and the refractory (effective) period of the ventricles and atria of the heart, His bundle, AV node and Purkinje fibers, as a result of which the automatism of the sinus node, the excitability of cardiomyocytes and AV conduction slows down.
The antianginal effect of the drug is due to a decrease in the resistance of the coronary arteries and a decrease in myocardial oxygen demand due to a decrease in heart rate, which ultimately leads to an increase in coronary blood flow. The drug does not significantly affect systemic blood pressure.
Structurally, amiodarone is similar to thyroid hormones. About 37% of the molecular weight is iodine. Amiodarone affects the metabolism of thyroid hormones: it inhibits the conversion of thyroxine into triiodothyronine and blocks the capture of thyroid hormones by hepatocytes and cardiocytes, which weakens the stimulating effect of thyroid hormones on the heart muscle.
The onset of action of the drug ranges from 2-3 days to 2-3 months. The duration of action ranges from several weeks to several months or more (the active substance is found in plasma within 9 months after the last dose of the drug).
Pharmacokinetics
After oral administration, the drug is slowly absorbed from the gastrointestinal tract. Its bioavailability ranges from 35 to 65%. In the blood, amiodarone is detected in 0.5-4 hours. After 2-10 hours after taking a single dose, the maximum concentration of the drug in the blood is observed. Therapeutic plasma concentration ranges from 1 to 2.5 mg / l. It takes one to several months to reach steady-state concentration.
Amiodarone is intensively distributed in tissues (volume of distribution is 60 liters). It easily penetrates adipose tissue and organs with good blood supply. The drug passes through the placenta and the blood-brain barrier, is excreted in breast milk (up to 25% of the dose taken by a nursing woman). 95% bound to plasma proteins.
Pharmacokinetic features of the drug necessitate its use in high loading doses.
Metabolism of amiodarone is carried out in the liver. The main metabolite is desethylamiodarone, which has similar pharmacological properties and is able to enhance the antiarrhythmic effect of the main compound. According to some reports, one of the metabolic pathways is deiodination. With prolonged therapy, iodine concentrations reach 60-80% of the concentration of the active substance. Amiodarone is an inhibitor of a number of hepatic isoenzymes and P-glycoprotein, as well as a carrier of organic anions.
The half-life of the drug varies greatly, which is associated with its ability to cumulate. After oral administration, amiodarone is excreted in two phases: in the first phase, the half-life is from 4 to 21 hours, in the second - from 25 to 110 days. After prolonged treatment, the average elimination half-life is 40 days.
85–95% of the dose taken is excreted through the intestines, less than 1% - by the kidneys. Amiodarone and its metabolites are not dialyzed.
Indications for use
Treatment and prevention of paroxysmal rhythm disturbances:
- Supraventricular arrhythmias (if other therapy is impossible or ineffective);
- Life-threatening ventricular arrhythmias (including ventricular tachycardia, ventricular fibrillation);
- Arrhythmias associated with chronic heart or coronary insufficiency;
- Parasystole, ventricular arrhythmias in patients with Chagas myocarditis;
- Atrial and ventricular premature beats;
- Angina pectoris.
Contraindications
- Sick sinus syndrome;
- Interstitial lung disease;
- AV blockade II-III century (without using a pacemaker);
- SA blockades;
- Hypokalemia;
- Cardiogenic shock;
- Arterial hypotension;
- Collapse;
- Thyrotoxicosis;
- Hypothyroidism;
- Hypersensitivity to drug components, as well as to iodine.
According to the instructions, Amiodarone is contraindicated while taking MAO inhibitors; it is also not prescribed for pregnant and lactating women.
Use with caution in the elderly (due to the high risk of developing severe bradycardia), children and adolescents under 18 years of age (due to the lack of data on the effectiveness and safety of its use), as well as against the background of:
- Liver failure;
- Chronic heart failure;
- Bronchial asthma.
Instructions for the use of Amiodarone: method and dosage
The scheme and duration of treatment is set individually by the attending physician.
Tablets are taken before meals, 200 mg 2-3 times a day. Gradually, the daily dosage is reduced to 200-400 mg. To avoid cumulation, after every 5 days of taking the drug, you must take a break of 2 days. Perhaps daily use of Amiodarone for 3 weeks, followed by a break for 7 days.
Against the background of angina pectoris, the initial dosage is 0.4-0.6 g per day, divided into 2-3 doses, which after 1-2 weeks is reduced to 200 mg per day.
Side effects
- Sense organs - lipofuscin deposition in the corneal epithelium, uveitis;
- Nervous system - sleep and memory disturbances, headache, auditory hallucinations, weakness, depression, dizziness, fatigue, paresthesia;
- Cardiovascular system - sinus bradycardia, AV block;
- Respiratory system - shortness of breath, bronchospasm, cough, pleurisy;
- Metabolism - thyrotoxicosis, hypothyroidism;
- Allergic reactions - exfoliative dermatitis, skin rash;
- Digestive system - nausea, decreased appetite, flatulence, vomiting, dullness or loss of taste, diarrhea, abdominal pain, feeling of heaviness in the epigastrium, constipation.
Other side effects: myopathy, epididymitis, decreased potency, alopecia, vasculitis, photosensitivity, bluish or bluish skin pigmentation.
Overdose
In case of an overdose, the following symptoms are observed: atrioventricular block, bradycardia, worsening symptoms of existing chronic heart failure, paroxysmal and ventricular tachycardia of the "pirouette" type, cardiac arrest, abnormal liver function.
In case of an overdose, gastric lavage is performed, activated charcoal and symptomatic therapy are prescribed. With tachycardia of the "pirouette" type, cardiac stimulation is performed and magnesium salts are prescribed intravenously; with bradycardia, the introduction of atropine, beta-adrenostimulants or the installation of a pacemaker is recommended. Hemodialysis is not performed because it is ineffective.
special instructions
Before starting therapy, an x-ray of the lungs should be performed, as well as an assessment of the function of the thyroid gland and liver. With long-term therapy, X-ray examination of the lungs is recommended annually.
During treatment, to prevent the occurrence of photosensitivity, it is recommended to avoid prolonged exposure to the sun.
When the drug is discontinued, recurrence of rhythm disturbances is possible.
Application during pregnancy and lactation
Amiodarone should not be used in pregnant women, since the fetal thyroid gland begins to accumulate iodine and hypothyroidism may develop in the newborn due to the increased concentration of iodine. The use of the drug during pregnancy and breastfeeding is possible only in cases where rhythm disturbances threaten life, and other antiarrhythmic therapy is ineffective (Amiodarone causes thyroid dysfunction in the fetus).
If necessary, the use of the drug during breastfeeding, breastfeeding should be discontinued.
Drug interactions
Due to the risk of developing ventricular tachycardia of the "pirouette" type, Amiodarone is contraindicated to be used simultaneously with the following drugs:
- phenothiazines (cyamemazine, thioridazine, fluphenazine, chlorpromazine, levomepromazine, trifluoperazine);
- butyrophenones (haloperidol, droperidol);
- tricyclic antidepressants;
- macrolides (spiramycin, erythromycin intravenously);
- antimalarial drugs (chloroquine, halofantrine, quinine, mefloquine, lumefantrine);
- fluoroquinolones (including moxifloxacin);
- class IA antiarrhythmic drugs (disopyramide, quinidine, procainamide, hydroquinidine);
- class III antiarrhythmic drugs (ibutilide, dofetilide, bretilium tosylate);
- benzamides (sultopride, tiapride, amisulpride, sulpiride, veraliprid);
- azoles;
- sotalol, vincamine, pimozide, pentamidine (parenteral), mizolastine, terfenadine, bepridil, sertindole, cisapride, diphemanil methyl sulfate, astemizole.
The drug is not recommended for use in combination with beta-blockers, diltiazem and verapamil (because of the risk of conduction and automatism disturbances) and laxatives that stimulate intestinal peristalsis (because of the risk of ventricular tachycardia of the "pirouette" type in hypokalemia caused by laxatives) …
Amiodarone is used with caution in conjunction with the following drugs:
- systemic glucocorticosteroids;
- diuretics that cause hypokalemia;
- procainamide (the concentration of procainamide in plasma increases and the likelihood of developing its side effects increases);
- amphotericin B (intravenous);
- tetracosactide (increased risk of ventricular arrhythmias).
With the simultaneous use of Amiodarone with indirect anticoagulants, the risk of bleeding increases; with cardiac glycosides - atrioventricular conduction and automatism are disturbed; with phenytoin and phosphenytoin - there is a risk of neurological disorders; with esmolol - contractility, conductivity and automatism are disturbed; with flecainide - the concentration of flecainide increases.
Amiodarone increases plasma concentrations of cyclosporine, lidocaine, sildenafil, triazolam, ergotamine, fentanyl, tacrolimus, midazolam, dihydroergotamine, HMG-CoA reductase inhibitors, dabigatran.
A decrease in the plasma concentration of amiodarone is observed when it is used simultaneously with orlistat, rifampicin and St. John's wort preparations; increased concentration - when used together with cimetidine, grapefruit juice and HIV protease inhibitors.
When combined with cholinesterase inhibitors, clonidine, pilocarpine, guanfacine and inhaled drugs for general anesthesia, the likelihood of severe bradycardia increases; with radioactive iodine - a violation of the absorption of radioactive iodine and distortion of the results of radioisotope studies of the thyroid gland is possible with drugs that cause photosensitization - an additive photosensitizing effect is observed; with dextromethorphan - an increase in the concentration of dextromethorphan is possible; with clopidogrel - a decrease in the concentration of clopidogrel in plasma is possible.
Analogs
Amiodarone analogs are:
- For the active substance - Ritmorest, Cardiodarone, Amiocordin, Vero-Amiodarone, Cordaron;
- By the mechanism of action - Multak, Refralon, Nibentan, Ornid.
Terms and conditions of storage
The shelf life of the tablets is 2 years. Store in a dry place, out of the reach of children, at a temperature not exceeding 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Amiodarone
According to reviews, Amiodarone is an effective drug for normalizing blood pressure and stabilizing heart rate. The downside is a rather extensive list of side effects and a high probability of interaction with other drugs, so this drug can only be prescribed by a doctor.
Amiodarone price in pharmacies
The drug is inexpensive. The price of Amiodarone in 200 mg tablets (30 per pack) in pharmacies averages 115–140 rubles and depends on the manufacturer.
Amiodarone: prices in online pharmacies
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Drug name Price Pharmacy |
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Amiodarone tab. 5 mg 30 pcs. RUB 65 Buy |
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Amiodarone 200 mg tablets 30 pcs. 120 RUB Buy |
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Amiodarone 200mg tablets 30 pcs. 125 RUB Buy |
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Amiodarone 200 mg tablets 30 pcs. 125 RUB Buy |
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Amiodarone 200mg tablets 30 pcs. RUB 145 Buy |
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Amiodarone 200 mg tablets 30 pcs. 148 RUB Buy |
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Amiodarone tab. 200 mg 30 pcs. 194 r Buy |
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Amiodarone conc. for prig of solution for intravenous injection. 50mg / ml 3ml amp. 10 pieces. 214 r Buy |
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Amiodarone 50 mg / ml concentrate for preparation of solution for intravenous administration 3 ml 10 pcs. 244 RUB Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
