Amiodaron-LH tab.200 mg No. 30

General characteristics. Structure:

International and chemical names: Amiodaronum ([2-butyl-3-benzofuranil] - [4 (2-dietilaminoetoks) - 3,5-diyodofenit] ketone a hydrochloride); main physical and chemical properties: tablets of a ploskotsilindrichesky form with a facet and risky, white or almost white color; structure: 1 tablet contains Amiodaronum of a hydrochloride 200 mg;
excipients: starch corn, lactoses monohydrate, sodium of a kroskarmelloz, magnesium stearate, aerosil.

Pharmacological properties:

Pharmacodynamics. Amiodaronum belongs to antiarrhytmic drugs III of a class (on classification Voganum Williams) though also I has some properties of antiarrhytmic means, the II that the IV classes. It blocks preferential potassium, and also natrium and calcium channels and is non-competitive the effect of stimulation alpha and beta adrenoceptors oppresses. Antiarrhytmic action of Amiodaronum is connected with ability to increase duration of action potential of cells of a myocardium, the effective refractory period of peredserdiya and ventricles, an atrioventricular node and the carrying-out system of heart accompanying with decrease in automatism of a sinus node, delay of atrioventricular conductivity, decrease in excitability of cardiomyocytes. Anti-anginal action is implemented due to decrease in need of a myocardium for oxygen (decrease in frequency of reductions and reduction of an afterload).
The clinical antiarrhytmic effect of Amiodaronum develops approximately through
7 days after an initiation of treatment also reach a maximum in 15 - 30 days. After the treatment termination the effect remains on an extent of 10 - 30 days.

Pharmacokinetics. Amiodaronum is slowly soaked up at oral administration. Its bioavailability makes about 40%. The peak of concentration in plasma is reached in 2 - 10 h after single use. At prolonged treatment the maximum concentration in a blood plasma is reached gradually for several weeks or months. Amiodaronum is metabolized, generally in a liver with education dezetilamiodaro-on which has similar pharmacological properties. Also only an insignificant part - with urine is removed preferential with bile and a stake. After single use of Amiodaronum the elimination half-life makes from 3,2 to 20,7 hours; at long use the elimination half-life of Amiodaronum increases and makes from 13 to 103 days (on average - 53 ± 24 days). Drug contacts receptors of fabrics owing to what its cumulation is observed.

Indications to use:

Prevention of a recurrence:
- the ventricular tachycardia menacing to fibrillation of ventricles;
- symptomatic ventricular tachycardia which results in disability;
- supraventricular tachycardia at patients with a heart disease if other drugs have no such effect or contraindications;
- fibrillation of ventricles;
- treatment and prevention of trembling and atrial fibrillation;
- treatment of ventricular premature ventricular contraction.

Route of administration and doses:

The usual dose makes from 600 to 1000 mg a day and can be applied for 8 - 10 days: on 2 tablets 2-3 times a day.
The supporting treatment. Apply a minimal effective dose, depending on individual reaction. A usual dose - from ½ tablets a day (1 tablet of times in 2 days) to 2 tablets a day.
Patients have to swallow of a tablet without chewing, washing down with a small amount of water. A pill is taken in time or after food. A pill is recommended to be taken regularly at the same time days. If the patient missed reception of a tablet, it has to accept it as soon as possible. But if time of use of the following dose came, it is necessary to take only this planned pill (without doubling of a dose).

Features of use:

Amiodaron-LH causes changes on an ECG: lengthening of a QT interval (in connection with the prolonged repolarization) with possible emergence of a tooth of U; these changes are result of therapeutic saturation, but not toxicity of drug.
Patients of advanced age can show hypersensitivity to action of the tablets Amiodaron-LH even at purpose of usual doses of drug.
Drug should be cancelled at emergence of an atrioventricular block of IІ and ІІ the I degree, sinuatrial blockade or blockade of legs of a ventriculonector. At atrioventricular the I-degrees block it is necessary to double the watch of the patient.
Amiodaron-LH contains iodine and therefore can influence absorption of a radioiodine. However functional researches of a thyroid gland (T3, T4, thyritropic hormone (TTG)) give in to assessment.
Cases диспноэ or unproductive cough can be connected with pulmonary toxicity of drug and demand carrying out a X-ray analysis (see. "Side effect").
Precautionary measures. Before an initiation of treatment the tablets Amiodaron-LH recommend to conduct an ECG research, definition of TTG and level of potassium in serum.
The hypopotassemia should be modified before use of the tablets Amiodaron-LH.
Side effects of drug (see. "Side effect") usually depend on a dose therefore it is necessary to adhere to care when determining minimum effective maintenance dose to avoid or reduce undesirable effects to a minimum.
Patients should be warned that they during treatment avoided impact of a sunlight or used means of protection.
Amiodaron-LH can cause dysfunction of a thyroid gland (see. "Side effect"), in particular at patients with dysfunction of a thyroid gland in the anamnesis or at relatives. Therefore before an initiation of treatment, during treatment and in several months after the end of treatment it is necessary to carry out careful clinical and biological monitoring. At suspicion of dysfunction of a thyroid gland it is necessary to take measurement of the TTG level in serum.
During treatment regular carrying out analyses of function of a liver (transaminase) for identification of the possible disturbances caused by the tablets Amiodaron-LH is recommended.
Children. Safety and efficiency of use of the tablets Amiodaron-LH for children were not studied therefore drug is not appointed to children.
Anesthesia: before operation it is necessary to report to the anesthesiologist that the patient accepts Amiodaron-LH (see. "Interaction with other medicines").

Influence on ability to drive the car or to work with difficult mechanisms. There are no data on influence of the tablets Amiodaron-LH on ability to drive the car or to work with difficult mechanisms.
Pregnancy. A research in an experiment on animals did not find teratogenic effect of drug. However nowadays there is no sufficient information to estimate whether leads Amiodaron-LH to malformations at a fruit at use it by women in the I trimester of pregnancy. Because of influence of drug on a thyroid gland of a fruit use of the tablets Amiodaron-LH is contraindicated, since the II trimester of pregnancy.
Feeding period breast. Amiodaron-LH it is excreted in breast milk in a significant amount therefore it is contraindicated to the women nursing.

Side effects:

Amiodaronum reduces heart rate and can cause bradycardia in some patients (heart rate - lower than 55 beats per minute).
Amiodaronum can strengthen the existing arrhythmia or cause new attacks of arrhythmia.
If heart rate is lower than 55 beats per minute, it is necessary to reduce a dose or to temporarily stop treatment. Conductivity disturbance (a sinoauricular block, an atrioventricular block of different degree), arterial hypotension is possible.
Amiodaronum can cause development of heart failure or strengthen manifestations of existing.
Nausea, vomiting, lock or loss of appetite belongs to side effects from digestive tract; sometimes there is a reversible deterioration in functional activity of a liver (increase in activity of enzymes of a liver). Side effects can
also to be shown in the form of an acute liver failure (with the high level of transaminases and/or jaundice) and chronic diseases of a liver (pseudo-alcoholic hepatitis, cirrhosis). Therefore it is necessary to control a condition of patients with a liver failure and if necessary to stop treatment. After the treatment termination symptoms of a liver failure, as a rule, disappear.
In time or after the treatment termination the hypothyroidism or a hyperthyroidism can be observed by Amiodaronum. In this case treatment by Amiodaronum should be stopped. A hypothyroidism it is necessary to treat by means of replacement therapy, and at a hyperthyroidism it is necessary to begin temporary thyreostatic therapy.
Cough and the progressing short wind testify to direct or indirect pulmonary toxicity of Amiodaronum. Such states as intersticial pneumonia, a pneumosclerosis, pleurisy, obstructive bronchitis can develop.
These side effects usually have temporality. At hypersensitivity to Amiodaronum it is necessary to stop treatment and to appoint corticosteroid therapy.
During treatment by Amiodaronum and in several weeks after the termination of its reception the photosensitization therefore it is necessary to use sun-protection creams on open body parts in the summer can develop.
Treatment by Amiodaronum can be followed by emergence of microdeposits on an uchatka of a cornea which at adults arise almost constantly and are most often localized in a zone under a century. In exclusively isolated cases they can cause a vision disorder in the form of emergence of a color aura at bright light or sight mistings. Microdeposits in a cornea zone which are formed by a complex of lipids always disappear after the end of treatment. In such cases it is not necessary to stop treatment, but the patient is recommended to be directed to ophthalmologic inspection.
Neurologic disturbances during therapy by Amiodaronum can be shown in the form of paresthesia, trembling, an ataxy, a headache, an optic neuritis, a polyneuropathy, dizziness and auditory hallucinations.
Other possible side effects include a myopathy, an epididymite, metal smack in a mouth, a hair loss and fatigue.

Interaction with other medicines:

Contraindicated simultaneous use of the tablets Amiodaron-LH with drugs which can cause Bouveret's ventricular disease like "torsade de pointes".
Antiarrhytmic drugs I of a class (quinidine, hydroquinidine, Disopyramidum).
Antiarrhytmic drugs ІІІ class (соталол, дофетилид, ибутилид).
Bepridil, цисаприд, difemanit, erythromycin for intravenous administration, мизоластин, спарфлоксацин, Vincaminum for intravenous administration.
Sultoprid.
The increased risk of development of ventricular arrhythmias, in particular a Bouveret's disease like "torsade de pointes".
Sparfloksatsin.
Danger of development of a Bouveret's disease like "torsade de pointes" in connection with prolongation of a QT interval (the additive electrophysiologic action).
The combination therapy with following drugs is not recommended.
Neuroleptics which can cause a Bouveret's disease like "torsade de pointes": some fenotiazinovy neuroleptics (Chlorpromazinum, циамемазин, levomepromazinum, thioridazine, трифлуоперазин), benzamides (амисульприд, Sulpiridum, тиаприд), phenyl propyl ketones (Droperidolum, haloperidol), Pimozidum.
The increased risk of development of ventricular arrhythmias, in particular paroxysmal tachycardia like "torsade de pointes".
Galofantrin, moxifloxacin, pentamidine.
The increased risk of development of ventricular arrhythmias, in particular paroxysmal tachycardia like "torsade de pointes". If such combination is not passed, the previous control of a QT interval and constant electrocardiographic control is necessary.
Injection form of diltiazem.
Risk of development of bradycardia and atrioventricular block. If such combination is not passed, careful control of a condition of the patient and constant electric car-diografichesky control is necessary.
Blockers of beta receptors, except a sotalol and an esmolol.
Risk of disturbance of automatism, conductivity and sokratitelny ability of heart (oppression of sympathetic compensatory mechanisms).
 With care it is necessary to appoint in a combination with the tablets Amiodaron-LH the drugs given below.
Peroral anticoagulants. Due to strengthening of effect of peroral anticoagulants and increase in risk of bleeding it is necessary to control more often prothrombin level in blood and to adjust a dose of peroral anticoagulants during treatment by the tablets Amiodaron-LH and after drug withdrawal.
Cyclosporine. The increase in level of cyclosporine in plasma connected with decrease in his metabolism in a liver, increasing nephrotoxicity of drug is possible. In this case necessary dose adjustment.
Diltiazem. Risk of development of bradycardia and an atrioventricular block, especially at patients of advanced age. Clinical and cardiographic control of a condition of the patient is necessary.
Foxglove drugs. Automatism disturbance (the expressed bradycardia) and atrioventricular conductivity is possible. Increase in concentration of digoxin in plasma is possible (because of decrease in its clearance).
It is necessary to conduct an ECG research, clinical and biological control (if necessary determination of level of digoxin in plasma); there can be a need for change of doses of cardiac glycosides.
Esmolol. Disturbance of automatism, conductivity and sokratitelny ability of heart (oppression of sympathetic compensatory mechanisms) is possible. Clinical and cardiographic control of a condition of the patient is necessary.
Means which can cause a hypopotassemia:
the diuretics causing a hypopotassemia in itself or in a combination with other drugs;
laxatives of a promoting effect;
 - system corticosteroids (glyuko-, mineralo-), тетракозактид;
 - Amphotericinum In (intravenous use).
The risk of development of ventricular disturbances of a rhythm, in particular a Bouveret's disease like "torsade de pointes" amplifies (the hypopotassemia is a favorable factor). Clinical and cardiographic control of a condition of the patient is recommended,
control of level of potassium in blood.
Phenytoinum. Increase in level of Phenytoinum in plasma with overdose symptoms is possible (in particular neurologic character). Clinical control and a dose decline of Phenytoinum with the advent of overdose signs is necessary; whenever possible - determination of level of Phenytoinum in plasma.
The means causing bradycardia: blockers of calcium channels (diltiazem, verapamil), blockers of beta adrenoceptors (except a sotalol), a clonidine, гуанфацин, foxglove drugs, мефлохин, cholinesterase inhibitors (donezepit, Galantaminum, ривастигман, такрин, амбемониум, pyridostigmine, неостигмин). Strengthening of risk of development of ventricular disturbances of a rhythm, in particular a Bouveret's disease like "torsade de pointes". Clinical and cardiographic control of a condition of the patient is recommended.
Simvastin. The risk of development of side effects (depending on a dose), such as рабдомиолиз amplifies (because of reduction of metabolism of drug in a liver). The dose of a simvastin should not exceed 20 mg a day. If at such dose it is impossible to reach therapeutic effect, it is necessary to apply other statine which is not interacting with the tablets Amiodaron-LH.
Anesthesia. Potentially heavy complications at patients to whom the general anesthesia is carried out can be observed: the bradycardia which is not adjusted atropine, arterial hypotension, conductivity disturbance, decrease in cordial emission.
Very seldom - the heavy respiratory complications which sometimes are coming to an end with a lethal outcome (acute respiratory distresssindry adults). As a rule, they are observed in the period of directly after surgical intervention owing to incompatibility with high concentration of oxygen.
The combination therapy with beta adrenoblockers, some blockers of calcium channels (verapamil, diltiazem) since the automatism disturbances (which are shown bradycardia) and conductivity can develop is not recommended. For prevention of development of ventricular tachycardia like "pirouette" it is not recommended combined
therapy of the drug Amiodaron-LH, tablet with diuretics, system glucocorticoids, Amphotericinum In for intravenous administration, laxative drugs. At simultaneous use with anticoagulants for intake the risk of development of bleedings increases (control of level of a prothrombin and dose adjustment of anticoagulants is necessary). At simultaneous use with cardiac glycosides the automatism disturbances (which are shown the expressed bradycardia) and disturbances of atrioventricular conductivity can be observed (Amiodaron-LH increases concentration of digoxin in a blood plasma therefore it is necessary to control it, to carry out an ECG, if necessary to change the drug dosing mode). At simultaneous use with Phenytoinum, cyclosporine increase in concentration of the last in a blood plasma is possible. At the patients taking the pill Amiodaron-LH and who were exposed to the general anesthesia or an oxygenotherapy it is possible, development of bradycardia (resistant to atropine), arterial hypotension, disturbances of conductivity and decrease in cordial emission.

Contraindications:

Sinus bradycardia and sinuatrial heart block in the absence of pacemakers.
Sick sinus syndrome, except for correction cases a rhythm pacemaker (risk of a stop of a sinus node).
Heavy disturbances of conductivity in the absence of correction by a rhythm pacemaker.
The combined use with the drugs capable to cause Bouveret's gastric disease like "torsade de pointes":
- antiarrhytmic drugs of the class Ia (quinidine, hydroquinidine, Disopyramidum);
- antiarrhytmic drugs of a class III (соталол, дофетилид, ибутилид);
- other medicines, such as bepridit, цизаприд, difemanit, erythromycin, мизоластин, moxifloxacin, Spheromycinum (intravenously), Vincaminum (intravenously);
- sultopridy.
Hyperthyroidism.
Hypersensitivity reaction to iodine or to the drug Amiodaron-LH is known.
I and II trimesters of pregnancy, feeding period breast.

Overdose:

Information concerning overdose of the tablets Amiodaron-LH is limited. The sinus bradycardia, gastric arrhythmia, in particular tachycardia like "torsade de po_ntes", and damage of a liver were in some cases observed. Considering a pharmacokinetic profile of drug, control of a condition of the patient throughout the long period, in especially control of cardiac performance is recommended.
Symptomatic treatment. Neither Amiodaron-LH, nor its metabolites are removed by dialysis.

Storage conditions:

To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.
Period of validity –2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister, on 3 blisters in a pack cardboard.