About the drug:
Antiarrhythmic agent class III, has antianginal effect.
Indications and dosage:
Treatment and prevention of paroxysmal arrhythmias: life-threatening ventricular arrhythmias (in
When ingested for adults, the initial single dose is 200 mg. For children, the dose is
For the on / in the introduction (jet or drip) single dose of 5 mg / kg daily dose – up to
Symptoms: increased or increased side effects, hypotension, bradycardia, AV conduction disorders, arrhythmia, liver dysfunction.
Treatment: gastric lavage, the appointment of activated carbon, saline laxative, with bradycardia – the introduction of atropine, beta-adrenergic receptor agonists, cardiac pacing.
Since the cardiovascular system: sinus bradycardia (refractory to m-holinoblokatoram), AV block, with prolonged use – the progression of heart failure, ventricular arrhythmia type "pirouette", enhancement of the existing arrhythmia or its occurrence, with parenteral administration, a decrease in blood pressure.
On the part of the endocrine system: the development of hypo-or hyperthyroidism.
On the part of the respiratory system: with prolonged use – cough, shortness of breath, interstitial pneumonia or alveolitis, pulmonary fibrosis, pleurisy, with parenteral administration – bronchospasm, apnea (in patients with severe respiratory failure).
On the part of the digestive system: nausea, vomiting, loss of appetite, dulling or loss of taste, feeling of heaviness in the epigastrium, abdominal pain, constipation, flatulence, diarrhea, rarely – increased activity of hepatic transaminases, with prolonged use – toxic hepatitis, cholestasis, jaundice , cirrhosis of the liver.
CNS and peripheral nervous system: headache, weakness, dizziness, depression, fatigue, paresthesia, auditory hallucinations, with prolonged use – peripheral neuropathy, tremor, impaired memory, sleep, extrapyramidal manifestations, ataxia, optic neuritis, parenteral use – intracranial hypertension.
On the part of the senses: uveitis, lipofuscin deposition in the corneal epithelium (if the deposits are significant and partially fill the pupil – complaints of luminous points or a veil in front of the eyes in bright light), microsleg of the retina.
From the hematopoietic system: thrombocytopenia, hemolytic and aplastic anemia.
Dermatological reactions: skin rash, exfoliative dermatitis, photosensitivity, alopecia, rarely – gray-blue staining of the skin.
Local reactions: thrombophlebitis.
Other: epididymitis, myopathy, reduced potency, vasculitis, with parenteral administration – fever, increased sweating.
Sinus bradycardia, SSSU, sinoatrial block, AV block II-III degree (without the use of a pacemaker), cardiogenic shock, hypokalemia, collapse, arterial hypotension, hypothyroidism, thyrotoxicosis, interstitial lung diseases, administration of MAO inhibitors, pregnancy, lactation period, stimulation. amiodarone and iodine.
Use during pregnancy and lactation is contraindicated.
Amiodarone and desmethylamiodarone penetrate the placental barrier, their concentrations in the fetal blood are 10% and 25%, respectively, of the concentration in the mother’s blood.
Interaction with other drugs and alcohol:
Drug interaction of amiodarone with other drugs is possible even several months after the end of its use due to the long half-life.
With simultaneous use of amiodarone and class I A antiarrhythmic drugs (in
The simultaneous use of amiodarone with laxatives that can cause hypokalemia increases the risk of ventricular arrhythmias.
Agents causing hypokalemia, including diuretics, corticosteroids, amphotericin B (w / w), tetracosactide, while being used with amiodarone, cause an increase in the QT interval and an increased risk of ventricular arrhythmia (in
With the simultaneous use of funds for general anesthesia, oxygen therapy, there is a risk of developing bradycardia, arterial hypotension, conduction disorders, reduction of the cardiac output, which is apparently due to additive cardiodepressant and vasodilating effects.
With the simultaneous use of tricyclic antidepressants, phenothiazines, astemizole, terfenadine cause an increase in the QT interval and an increased risk of developing ventricular arrhythmias, especially "pirouette".
With simultaneous use of warfarin, fenprocumone, acenocoumarol increases the anticoagulant effect and increases the risk of bleeding.
With the simultaneous use of vincamine, sultoprid, erythromycin (IV), pentamidine (IV / IV), the risk of developing ventricular arrhythmias increases "pirouette".
With simultaneous use, it is possible to increase the concentration of dextromethorphan in the blood plasma due to a decrease in its metabolic rate in the liver, which is caused by the inhibition of the activity of the cytochrome P450 isoenzyme CYP2D6 under the influence of amiodarone and the slowing down of dextromethorphan from the body.
With the simultaneous use of digoxin, the concentration of digoxin in the blood plasma significantly increases due to a decrease in its clearance and, as a result, the risk of developing digitalis intoxication increases.
With simultaneous use of diltiazem, verapamil increases the negative inotropic effect, bradycardia, conduction disturbance, AV-blockade.
A case of increasing the concentration of amiodarone in the blood plasma is described when it is used simultaneously with indinavir. It is believed that ritonavir, nelfinavir, saquinavir will have a similar effect.
With simultaneous use of Kolestiramin decreases the concentration of amiodarone in the blood plasma due to its binding to Kolestiramine and reducing the absorption from the gastrointestinal tract.
There are reports of increased plasma concentrations of lidocaine with simultaneous use with amiodarone and the development of convulsions, apparently due to inhibition of lidocaine metabolism under the influence of amiodarone.
It is believed that synergism is possible with regard to the inhibitory effect on the sinus node.
With the simultaneous use of lithium carbonate may develop hypothyroidism.
With simultaneous use of procainamide, the QT interval increases due to the additive effect on its size and the risk of developing ventricular tachycardia of the type "pirouette". Increased plasma concentrations of procainamide and its metabolite, N-acetylprocainamide, and increased side effects.
With the simultaneous use of propranolol, metoprolol, sotalol, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.
With the simultaneous use of trazodone described a case of arrhythmia type "pirouette".
With simultaneous use of quinidine, the QT interval increases due to the additive effect on its size and the risk of developing ventricular tachycardia of the type "pirouette". Increasing the concentration of quinidine in the blood plasma and enhancing its side effects.
With simultaneous use described case of increased side effects of clonazepam, which, apparently, due to its cumulation due to inhibition of oxidative metabolism in the liver under the influence of amiodarone.
With simultaneous use of cisapride, the QT interval significantly increases due to the additive effect, the risk of developing ventricular arrhythmias (in
With simultaneous use increases the concentration of cyclosporine in the blood plasma, the risk of nephrotoxicity.
A case of pulmonary toxicity with simultaneous use of high-dose cyclophosphamide and amiodarone is described.
The concentration of amiodarone in the blood plasma increases due to the slowing down of its metabolism under the influence of cimetidine and other inhibitors of microsomal liver enzymes.
It is believed that due to the inhibition of liver enzymes under the influence of amiodarone, with the participation of which the metabolism of phenytoin occurs, the concentration of the latter in the blood plasma may be increased and its side effects may increase.
Due to the induction of liver microsomal enzymes under the influence of phenytoin, the rate of metabolism of amiodarone in the liver increases and its concentration in the blood plasma decreases.
Composition and properties:
1 tablet contains amiodarone hydrochloride 200 mg; in a blister strip package 10 pcs., in a box of 3, 6 and 10 packs.
200 mg tablets; blister 10, pack of cardboard 3.
200 mg tablets; blister 10, pack of cardboard 6.
200 mg tablets; blister 10, carton pack 50.
200 mg tablets; blister 100, box (box) 100.
200 mg tablets; blister 10, pack of cardboard 3.
200 mg tablets; blister 10, pack of cardboard 6.
The antiarrhythmic effect is associated with the ability to increase the duration of the action potential of cardiomyocytes and the effective refractory period of the atria, ventricles of the heart, AV node, His bundle, Purkinje fibers. This is accompanied by a decrease in the automatism of the sinus node, a slowdown in AV conduction, a decrease in the excitability of cardiomyocytes. It is believed that the mechanism for increasing the duration of the action potential is associated with the blockade of potassium channels (the excretion of potassium ions from cardiomyocytes is reduced). Blocking inactivated "fast" sodium channels, has effects characteristic of class I antiarrhythmic drugs. Slows down the slow (diastolic) depolarization of the cell membrane of the sinus node, causing bradycardia, inhibits AV conduction (the effect of class IV antiarrhythmics).
The antianginal effect is due to coronary dilating and anti-adrenergic effects, a decrease in myocardial oxygen demand. It has an inhibitory effect on the α- and β-adrenoreceptors of the cardiovascular system (without their complete blockade). Reduces sensitivity to the hyperstimulation of the sympathetic nervous system, the tone of the coronary vessels; increases coronary blood flow; lowers heart rate; increases the energy reserves of the myocardium (by increasing the content of creatine sulfate, adenosine and glycogen). Reduces OPSS and systemic blood pressure (with a / in the introduction).
It is believed that amiodarone may increase the level of phospholipids in the tissues.
Contains iodine. Affects the metabolism of thyroid hormones, inhibits the conversion of T3 to T4 (blocking thyroxin-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 (T3 deficiency can lead to hyperproduction and thyrotoxicosis) .
On ingestion, the onset of action is from 2-3 days to 2-3 months, the duration of action is also variable – from several weeks to several months.
After the on / in the introduction of the maximum effect is achieved in 1-30 minutes and lasts 1-3 hours.
List B.: In the dark place at a temperature of no higher than 25 ° C.