Kardiodaron, tab. of 0,2 g, No. 10х3

General characteristics. Structure:

International and chemical names: amiodarone ([2-Butil-3-benzofuranil] - [-3,5-diyodofenit 4 (2-dietilaminoetoks)] ketone a hydrochloride);
main physical and chemical properties: tablets white or with a chartreuse shade of color, with a flat surface, from risky;
structure: 1 tablet contains Amiodaronum of a hydrochloride 0,2 g;
excipients: sugar milk, potato starch, cellulose microcrystallic, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Kardiodaron possesses antiarrhytmic and anti-anginal action.
Antiarrhytmic action is caused by lengthening of the 3rd phase of action potential due to decrease in current of potassium via channels of cellular membranes of cardiomyocytes. Increases the refractory period and reduces excitability of a myocardium. Drug it is non-competitive blocks alpha and beta adrenoceptors. Slows down sinuatrial, atrial and nodal conduction, practically does not influence intra ventricular conductivity. Slows down carrying out excitement and extends the refractory period of additional atrioventricular ways. 
Anti-anginal action is caused by decrease in consumption of oxygen a myocardium (due to reduction of ChSS and decrease in an afterload by heart), increase in a coronary blood-groove by direct impact on smooth muscles of arteries, maintenance of cordial emission by pressure decrease in an aorta and decrease in peripheric resistance.

Pharmacokinetics. After intake Kardiodaron is slowly soaked up from ЖКТ.Биодоступность makes 30-80%. Drug is found in blood through ½-4 h. The maximum concentration in blood after a single dose is observed in 3–7 h. It is brought out of an organism extremely slowly, the elimination half-life makes 20–100 days. It is metabolized in a liver with formation of an active metabolite (detsetilamiodaron), and also by deiodinating.

Indications to use:

Treatment and prevention of paroxysmal disturbances of a cordial rhythm (supraventricular tachycardia, WPW syndrome, ventricular tachycardia, atrial flutter, sinus tachycardia), and also premature ventricular contraction (supraventricular, ventricular).
Prevention of a recurrence
life-threatening ventricular tachycardia or fibrillation of ventricles;
the ventricular tachycardia (documented) with clinical manifestations and leading to disability;
the supraventricular tachycardia (documented) at patients with heart diseases;
disturbances of a rhythm at resistance or existence of contraindications to other methods of treatment;
WPW-syndrome (WPW).
Treatment of the ventricular tachycardia which is (documentary confirmed) for delay of a rhythm of reductions of ventricles or recovery of a sinoatrial rate during the blinking and an atrial flutter.
Kardiodaron patients can appoint with an ischemic heart disease and/or dysfunction of a left ventricle.

Route of administration and doses:

Optimum doses of tablets Kardiodaron need to be selected individually, taking into account possible by-effects. As a rule, drug appoint since a dose 0,2 g (1 tablet), 2–3 times a day (0,4–0,6 g a day), within 8–10 days (depending on effect), under control of an ECG. Further pass to a maintenance dose 0,1–0,4 g a day. The scheme of purpose of drug every other day is possible: it is possible to appoint a dose of 0,2 g (1 tablet) every other day, 0,1 g (0,5 tablets) – daily. For the purpose of the prevention of cumulation every 5 days it is recommended to do 2 days of a break.

Features of use:

Has to appoint Kardiodaron and to begin treatment only the doctor who has experience of therapy of disturbances of a cordial rhythm.
With care appoint drug to patients of old age as the risk of development of bradycardia increases.
Before an initiation of treatment carrying out an ECG is shown to each patient.
During treatment by Kardiodaron, and also when developing new arrhythmias or aggravations of a basic disease it is necessary to spend ECG monitoring each 3 months.
Action of Amiodaronum can cause the lengthening of an interval of QT (caused by repolarization delay) and emergence of a tooth of U on an ECG. These changes do not reflect cardiotoxicity existence.
At emergence of sinuatrial blockade, AV of blockade II and III degrees, blockade of legs of a bunch of Giss treatment should be interrupted.
At Kardiodaron's appointment can be required by patients with heart failure simultaneous treatment by cardiotonic means.
The patient should be informed that in case of development of side effects (including if ChSS makes less than 55 beats per minute) it is necessary to stop treatment and to see immediately a doctor.
The progressing asthma and unproductive cough can be symptoms of pulmonary intoxication. It is recommended to conduct X-ray inspection of a thorax and pulmonary functional trials each 6 months (including in cases of development of clinical signs of a disease of lungs).
Kardiodaron can cause dysfunctions of a thyroid gland, especially in patients with genetic and individual predisposition to diseases of a thyroid gland. It is recommended to carry out monitoring of function of a thyroid gland before an initiation of treatment, during treatment and within several months after the treatment termination. At development of dysfunctions of a thyroid gland it is necessary to interrupt treatment and to appoint the corresponding therapy.
Amiodaronum can exert impact on results of a research of function of a thyroid gland, especially on thyroxine.
During treatment by Kardiodaron it is necessary to control activity of liver enzymes (especially at patients with a liver failure).
At development of side effects from an organ of sight it is not necessary to interrupt treatment, however ophthalmologic inspection is shown to the patient.
It is necessary to be careful when performing oxygen therapy in the postoperative period at the patients accepting Kardiodaron since there is a risk of development of a respiratory distresssindrom.
The question of an opportunity to manage motor transport and to be engaged in potentially dangerous types of activity should be solved only after assessment of individual reaction of the patient to drug since at some patients reduction in the rate of psychomotor reactions against the background of treatment by Kardiodaron is noted.

Side effects:

From cardiovascular system: bradycardia (ChSS less than 55 beats per minute), development or progressing of arrhythmia, development or deterioration in a course of heart failure.
From the alimentary system: anorexia, nausea, vomiting, a lock, metal smack in a mouth; seldom – increase in activity of liver enzymes, pseudo-alcoholic hepatitis, cirrhosis, an acute liver failure.
From TsNS and peripheral nervous system: paresthesias, tremor, ataxy, headache, feeling of fatigue, retrobulbar neuritis, polyneuropathies, dizziness, auditory hallucinations.
From an organ of sight: adjournment of lipofuscin in a cornea epithelium (complaints to emergence of color auras at a look against light are in rare instances noted).
From respiratory system: cough, the progressing short wind, an intersticial pneumonitis, a pneumosclerosis, pleurisy, bronchitis.
From endocrine system: hypothyroidism, hyperthyroidism.
Dermatological reactions: photosensitization, skin rash, hair loss.
Others: myopathy, epididymite.

Interaction with other medicines:

The combination therapy with beta adrenoblockers, some blockers of calcium channels (verapamil, diltia-zy) is not recommended as the automatism disturbances (which are shown bradycardia) and conductivity can develop. For prevention of development of ventricular tachycardia like "pirouette" the combination therapy by tablets Kardiodaron with laxative drugs, diuretics, system glucocorticoids, Amphotericinum In for in/in introductions is not recommended. 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 are necessary). At simultaneous use with cardiac glycosides the automatism disturbances (which are shown the expressed bradycardia) and disturbances of atrioventricular conductivity (Kardiodaron increases concentration of digoxin in a blood plasma, it is necessary to control it, to carry out an ECG can be observed and at the need 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 a pill Kardiodaron and who were exposed to the general anesthesia or an oxygenotherapy development of bradycardia (resistant to atropine), arterial hypotension, disturbances of conductivity and decrease in cordial emission is possible.

Contraindications:

Hypersensitivity to Amiodaronum and to iodine, a sinus bradycardia, SSSU (in cases of lack of a pacemaker), sinuatrial blockade, AV blockade, a concomitant use with drugs which can cause ventricular tachycardia like "pirouette" (antiarrhytmic means, including bepridit, drugs ІА a class, соталол, and also Vincaminum, султоприд, erythromycin for in/in introductions, pentamidine for parenteral administration), a hypothyroidism, a hyperthyroidism, the expressed arterial hypotonia, a collapse, shock, a lactation, pregnancy, children's age up to 15 years.

Overdose:

Symptoms: arterial hypotension, bradycardia, disturbances of AV of conductivity, arrhythmia, abnormal liver function. 
Treatment: a gastric lavage with the subsequent purpose of absorbent carbon and salt laxative. There is no specific antidote. If necessary carry out symptomatic therapy. The patient has to be under careful observation (control of the ABP and an ECG). At bradycardia it is possible to apply atropine, adrenomimetika b1-, to establish a temporary pacemaker. Amiodaronum is not removed from an organism at a hemodialysis.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 25 °C.

Period of storage - 2 years. 

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,2 g No. 10х3 in a blister strip packaging, No. 30 - in a container plastic for medicines.