Amiodarone tablets 200mg, 30
Expiration Date: 05/2027
Russian Pharmacy name:
Амиодарон таблетки 200мг, 30
When taken orally for adults, the initial single dose is 200 mg. For children, the dose is 2.5-10 mg / day. The scheme and duration of treatment are set individually.
Pills
amiodarone hydrochloride
Sinus bradycardia, SSSU, sinoatrial block, II-III degree AV block (without using a pacemaker), cardiogenic shock, hypokalemia, collapse, arterial hypotension, hypothyroidism, thyrotoxicosis, interstitial lung disease, MAO inhibitors, pregnancy, lactation, hypersensitivity to amiodarone and iodine.
pharmachologic effect
Antiarrhythmic drug of class III, has antianginal action. 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, bundle of His, Purkinje fibers. This 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. 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 decreases). By blocking inactivated 'fast' sodium channels, it has the effects characteristic of class I antiarrhythmics. Inhibits the slow (diastolic) depolarization of the sinus node cell membrane, causing bradycardia,inhibits AV conduction (the effect of class IV antiarrhythmics). The antianginal effect is due to a coronary dilator and antiadrenergic action, a decrease in myocardial oxygen demand. Has an inhibitory effect on? - and? -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; reduces 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 intravenous administration). It is believed that amiodarone can increase the level of phospholipids in tissues. Contains iodine. Affects the metabolism of thyroid hormones,inhibits the conversion of T3 to T4 (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 (T3 deficiency can lead to its overproduction and thyrotoxicosis). When taken orally, 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 intravenous administration, the maximum effect is achieved after 1-30 minutes and lasts 1-3 hours.After intravenous administration, the maximum effect is achieved after 1-30 minutes and lasts 1-3 hours.After intravenous administration, the maximum effect is achieved after 1-30 minutes and lasts 1-3 hours.
Pharmacokinetics
After oral administration, it is slowly absorbed from the gastrointestinal tract, absorption is 20-55%. Cmax in blood plasma is achieved after 3-7 hours. Due to intensive accumulation in adipose tissue and organs with a high level of blood supply (liver, lungs, spleen), it has a large and variable Vd and is characterized by a slow achievement of equilibrium and therapeutic concentrations in blood plasma and to prolonged excretion ... Amiodarone is determined in blood plasma up to 9 months after discontinuation of its use. Protein binding is high - 96% (62% - with albumin, 33.5% - with ?-lipoproteins). Penetrates the BBB and the placental barrier (10-50%), excreted in breast milk (25% of the dose received by the mother). It is extensively metabolized in the liver with the formation of an active metabolite of desethylamiodarone, and also, apparently, by deiodination.With prolonged treatment, the concentration of iodine can reach 60-80% of the concentration of amiodarone. It is an inhibitor of isoenzymes CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. Excretion is biphasic. After oral administration, T1 / 2 in the initial phase is 4-21 days, in the terminal phase - 25-110 days; desethylamiodarone - an average of 61 days. As a rule, with a course of oral administration, T1 / 2 of amiodarone is 14-59 days. After intravenous administration of amiodarone, T1 / 2 in the terminal phase is 4-10 days. It is excreted mainly in the bile through the intestines, there may be a slight enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted during dialysis.CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. Excretion is biphasic. After oral administration, T1 / 2 in the initial phase is 4-21 days, in the terminal phase - 25-110 days; desethylamiodarone - an average of 61 days. As a rule, with a course of oral administration, T1 / 2 of amiodarone is 14-59 days. After intravenous administration of amiodarone, T1 / 2 in the terminal phase is 4-10 days. It is excreted mainly in the bile through the intestines, there may be a slight enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted during dialysis.CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. Excretion is biphasic. After oral administration, T1 / 2 in the initial phase is 4-21 days, in the terminal phase - 25-110 days; desethylamiodarone - an average of 61 days. As a rule, with a course of oral administration, T1 / 2 of amiodarone is 14-59 days. After intravenous administration of amiodarone, T1 / 2 in the terminal phase is 4-10 days. It is excreted mainly in the bile through the intestines, there may be a slight enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted during dialysis.in the course of oral administration, T1 / 2 of amiodarone is 14-59 days. After intravenous administration of amiodarone, T1 / 2 in the terminal phase is 4-10 days. It is excreted mainly in the bile through the intestines, there may be a slight enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted during dialysis.in the course of oral administration, T1 / 2 of amiodarone is 14-59 days. After intravenous administration of amiodarone, T1 / 2 in the terminal phase is 4-10 days. It is excreted mainly in the bile through the intestines, there may be a slight enterohepatic recirculation. In very small amounts, amiodarone and desethylamiodarone are excreted in the urine. Amiodarone and its metabolites are not excreted during dialysis.
Indications of the active substances of the drug Amiodarone
Treatment and prevention of paroxysmal arrhythmias: life-threatening ventricular arrhythmias (including ventricular tachycardia), prevention of ventricular fibrillation (including after cardioversion), supraventricular arrhythmias (usually when other therapy is ineffective or impossible, especially associated with WPW syndrome), incl. paroxysm of atrial fibrillation and flutter; atrial and ventricular premature beats; arrhythmias against the background of coronary insufficiency or chronic heart failure, parasystole, ventricular arrhythmias in patients with Chagas myocarditis; angina pectoris. Side effect
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Contraindications for use
Sinus bradycardia, SSSU, sinoatrial block, II-III degree AV block (without using a pacemaker), cardiogenic shock, hypokalemia, collapse, arterial hypotension, hypothyroidism, thyrotoxicosis, interstitial lung disease, MAO inhibitors, pregnancy, lactation, hypersensitivity to amiodarone and iodine.
Application during pregnancy and lactation
Use during pregnancy and lactation is contraindicated. Amiodarone and desmethylamiodarone penetrate the placental barrier, their concentrations in the fetal blood are, respectively, 10% and 25% of the concentration in the mother's blood. Amiodarone and desmethylamiodarone are excreted in breast milk.
Application for violations of liver function
Use with caution in liver failure.
Application in children
Use with caution before the age of 18 (efficacy and safety have not been established).
Use in elderly patients
Use with caution in elderly patients (high risk of severe bradycardia).
special instructions
Use with caution in chronic heart failure, liver failure, bronchial asthma, in elderly patients (high risk of severe bradycardia), under the age of 18 (efficacy and safety of use have not been established). Should not be used in patients with severe respiratory failure. Before starting the use of amiodarone, an x-ray examination of the lungs and thyroid function should be performed, if necessary, correction of electrolyte disturbances should be carried out. Long-term treatment requires regular monitoring of thyroid function, consultation with an ophthalmologist and X-ray examination of the lungs. Parenterally can be used only in specialized departments of hospitals under constant monitoring of blood pressure, heart rate and ECG. Patients receiving amiodaroneshould avoid direct exposure to sunlight. With the abolition of amiodarone, recurrence of heart rhythm disturbances is possible. May interfere with the test results for the accumulation of radioactive iodine in the thyroid gland. Do not use amiodarone concomitantly with quinidine, beta-blockers, calcium channel blockers, digoxin, coumarin, doxepin.
Drug interactions
Drug interaction of amiodarone with other drugs is possible even several months after the end of its use due to prolonged T1 / 2. With the simultaneous use of amiodarone and class I A antiarrhythmics (including disopyramide), the QT interval increases due to the additive effect on its value and the risk of developing ventricular tachycardia of the 'pirouette' type increases. With the simultaneous use of amiodarone with laxatives that can cause hypokalemia, the risk of developing ventricular arrhythmia increases. Drugs that cause hypokalemia, including diuretics, corticosteroids, amphotericin B (i.v.), tetracosactide, when used simultaneously with amiodarone, cause an increase in the QT interval and an increased risk of ventricular arrhythmias (including pirouette type).With the simultaneous use of agents for general anesthesia, oxygen therapy, there is a risk of developing bradycardia, arterial hypotension, conduction disorders, a decrease in the stroke volume of the heart, which, apparently, is due to additive cardiodepressive 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 of the 'pirouette' type. With the simultaneous use of warfarin, phenprocoumon, acenocoumarol, the anticoagulant effect increases and the risk of bleeding increases. With the simultaneous use of vincamine, sultopride, erythromycin (i / v), pentamidine (i / v, i / m), the risk of developing ventricular arrhythmias of the 'pirouette' type increases.With simultaneous use, it is possible to increase the concentration of dextromethorphan in the blood plasma due to a decrease in the rate of its metabolism in the liver, which is due to inhibition of the activity of the CYP2D6 isoenzyme of the cytochrome P450 system under the influence of amiodarone and slowing down the elimination 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 the simultaneous use of diltiazem, verapamil, the negative inotropic effect, bradycardia, conduction disturbances, AV blockade are enhanced. A case of an increase in the concentration of amiodarone in blood plasma with its simultaneous use with indinavir is described. It is believed that ritonavir, nelfinavir,saquinavir will have a similar effect. With the simultaneous use of cholestyramine, the concentration of amiodarone in the blood plasma decreases due to its binding with cholestyramine and a decrease in absorption from the gastrointestinal tract. There are reports of an increase in the concentration of lidocaine in the blood plasma with simultaneous use with amiodarone and the development of seizures, apparently due to inhibition of lidocaine metabolism under the influence of amiodarone. It is believed that synergism is possible in relation to the inhibitory effect on the sinus node. With the simultaneous use of lithium carbonate, hypothyroidism may develop. With the simultaneous use of procainamide, the QT interval increases due to the additive effect on its value and the risk of developing ventricular tachycardia of the 'pirouette' type.Increased plasma concentration 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, a case of the development of arrhythmias of the 'pirouette' type has been described. With the simultaneous use of quinidine, the QT interval increases due to the additive effect on its value and the risk of developing ventricular tachycardia of the 'pirouette' type. An increase in the concentration of quinidine in blood plasma and an increase in its side effects. With simultaneous use, a case of increased side effects of clonazepam has been described, which, apparently, is due to its cumulation due to inhibition of oxidative metabolism in the liver under the influence of amiodarone.With the simultaneous use of cisapride, the QT interval is significantly increased due to the additive action, the risk of developing ventricular arrhythmias (including the 'pirouette' type). With simultaneous use, the concentration of cyclosporine in the blood plasma increases, the risk of developing nephrotoxicity. A case of pulmonary toxicity with the simultaneous use of cyclophosphamide in high doses and amiodarone is described. The concentration of amiodarone in the blood plasma increases due to a slowdown in 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 phenytoin is metabolized, it is possible to increase the concentration of the latter in the blood plasma and increase its side effects.Due to the induction of liver microsomal enzymes under the influence of phenytoin, the metabolic rate of amiodarone in the liver increases and its concentration in blood plasma decreases.
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