Aritmitl

General characteristics. Structure:

International and chemical names: Amiodaron, (2-butylcoumarone-3-silt) - [4-[2-dietilamino) etoks] - 3,5-diyodofenit] a metanona a hydrochloride;
main physical and chemical properties: transparent slightly greenish liquid;
structure: 1 ml of solution contains 50 mg of Amiodaronum of a hydrochloride (in terms of 100% substance);
excipients: polysorbate 80, benzyl alcohol, water for injections.

Pharmacological properties:

Pharmacodynamics. Antiarrhytmic drug III of a class. Antiarrhytmic action is caused by increase 3 phases of action potential, generally due to blockade of potassium channels of membranes of cardiomyocytes, and also calcium channels, decrease in conductivity on an AV node, and decrease in automatism of a sinus node. In insignificant degree blocks the opened and inactivated natrium channels and slows down a bystry entrance sodium flow. Drug it is non-competitive blocks α-and β-adrenoceptors generally of a myocardium that also slows down sinuatrial, atrial and AV conductivity, without influencing intra ventricular conductivity. Amiodaronum increases the refractory period and reduces excitability of a myocardium. Slows down carrying out excitement and extends the refractory period of additional atrioventricular ways. Anti-anginal action of Amiodaronum is caused by decrease in consumption of oxygen a myocardium due to reduction of ChSS and decrease in the general peripheric resistance of vessels. Amiodaronum does not cause a considerable negative inotropic effect.

Pharmacokinetics. Amiodaronum has the large volume of distribution. In the first days of appointment drug collects practically in all fabrics, especially in fatty inclusions, a liver, a spleen, lungs. In several days removal of Amiodaronum from an organism is noted. Stable concentration is reached ranging from 1 up to several months, depending on specific features of the patient. Amiodaronum is removed with bile and a stake. Renal excretion is insignificant. The elimination half-life makes 20-100 days. After the treatment termination by Amiodaronum its removal from an organism continues within several months. Amiodaronum contains iodine therefore at metabolism in a liver there is eliminating of iodine and its allocation to urine in the form of salts. The main part of Amiodaronum and its metabolites are allocated through intestines within more than 30 days. After drug withdrawal its effective action continues within several days or even weeks.

Indications to use:

Prevention of a recurrence: the ventricular tachycardia menacing for life or fibrillation of ventricles; the ventricular tachycardia (documented) with clinical manifestations, 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. For the purpose of delay of a rhythm of reductions of ventricles or recovery of a sinoatrial rate during the blinking and an atrial flutter.

Route of administration and doses:

For intravenous administration the dose and frequency rate of use is established individually, depending on a state and needs of each patient.
Intravenous injection: The usual dose makes 5 mg/kg of body weight and has to be entered within not less than 3 minutes. The repeated intravenous injection should not be entered earlier, than in 15 min. after the first introduction even if only a part of contents of one ampoule was used. The therapeutic effect is shown within the first minutes after introduction of Amiodaronum and then gradually decreases. In this regard, intravenous infusion is necessary for maintenance of stable effect.
Intravenous infusion: The initial dose – usually makes 5 mg/kg (0,3-0,4 g) in 250 ml of 5% of solution of glucose, during the period of 20 min. to 2 h; it is possible to repeat introduction 2-3 times during 24 h. Speed of injection needs to be adjusted according to results. The therapeutic effect of drug is shown within the first minutes of introduction and disappears gradually therefore it is necessary to establish the connecting infusion. The maximum daily dose should not exceed 1200 mg/days. A maintenance dose – 10-20 mg/kg/days (on average 600-800 mg/days to 1200 mg/days) in 250 ml of 5% of solution of glucose within several days. Infusional therapy usually continues 4–5 days. From the first day of infusion it is necessary to begin gradual transition to oral administration.
For stopping of arrhythmias in urgent situations Aritmil enter to children in a dose 5 mg/kg intravenously slowly (within 1–3 min.) into 5% glucose solution, then pass to the supporting drop infusion of Aritmil in the same dose divorced in 100–250 ml   of 5% of solution of glucose and infuziruyemy during 0,5–2 h.

Features of use:

With care to apply at disturbances of electrolytic balance as there are separate messages on development or progressing of arrhythmias (up to a cardiac standstill). It is necessary to consider that at Aritmil's use changes of an ECG are possible: lengthening of an interval of QT with possible emergence of a tooth of U. It is necessary to consider that at patients of advanced age more expressed decrease in ChSS is noted. At emergence of AV blockade of II and III degrees, sinuatrial or bifastsikulyarny blockade treatment by Aritmil should be stopped. It is also necessary to consider that after drug withdrawal the pharmakodinamichesky effect remains within 10-30 days.
Aritmil contains iodine (in 200 mg of drug 75 mg of iodine contain) therefore it can exert impact on results of tests of accumulation of a radioiodine in a thyroid gland. Before an initiation of treatment, during its carrying out and for several months after the end of treatment it is necessary to conduct researches of function of a thyroid gland. In the course of treatment it is necessary to conduct an ophthalmologic research, to control function of a liver, and also to conduct X-ray inspection of lungs. In order to avoid development of a photosensitization by the patient it is necessary to avoid stay in the sun or to use effective protective equipment (protective creams). It is necessary to consider that exceptional cases of development acute respiratory a distress syndrome at adults directly after surgical interventions were celebrated. Therefore before operation the anesthesiologist has to be informed that to the patient entered Aritmil. With care appoint drug to elderly people (risk of development of bradycardia), drivers of vehicles and persons whose profession is connected with the increased concentration of attention.

Side effects:

From cardiovascular system: bradycardia (degree depends on a dose); in isolated cases – a stop of a sinus node (usually at dysfunction of a sinus node or at patients of advanced age), occasionally – sinuatrial or AV blockade. There are messages on development or progressing of arrhythmias (up to a cardiac standstill), hypotension during surgical interventions on open heart.
From an organ of sight: deposits of lipofuscin in a cornea epithelium (in this case usually subjective complaints at patients are absent); in rare instances if deposits considerable and partially fill a pupil, there are complaints to emergence of color auras or an illegibility of contours. There are data on development of neuropathies or an optic neuritis (reliable connection with reception Aritmila is not established).
Dermatological reactions: a photosensitization (at simultaneous use of radiation therapy it is shown in the form of an erythema), a lead-blue or bluish xanthopathy (at prolonged use, after the treatment termination slowly disappears), skin rash, including exfoliative dermatitis (reliable connection with reception Aritmila is not established), it is rare – an alopecia.
From the endocrine status: increase in quantity of a tetrayodtironin (T4) at normal or insignificant decrease in triiodothyronine (T3) (in the absence of clinical signs of dysfunction of a thyroid gland treatment should not be stopped). At prolonged use, in rare instances, development of a gipoterioz is possible, is much more rare – a hyperthyroidism.
From a nervous system: occasionally – neuropathy, a myopathy (reversible after drug withdrawal), an extrapyramidal tremor, a cerebellar ataxy, in isolated cases - benign intracranial hypertensia, dreadful dreams.
From a digestive tract: nausea, vomiting, taste disturbance, abnormal liver function, increase in activity of hepatic transaminases, pseudo-alcoholic hepatitis, cirrhosis.
From respiratory system: cases of development of an alveolar and/or intersticial pneumonitis, fibrosis, pleurisy, an obliterating bronchiolitis, pneumonia (with a lethal outcome), a bronchospasm (especially at patients with heavy respiratory insufficiency or bronchial asthma), an apnoea are described (at patients with heavy respiratory insufficiency).
Others: seldom – a vasculitis, renal failures, thrombocytopenia, sometimes an epididymite, impotence (reliable connection with administration of drug is not established), hemolitic or aplastic anemia. At intravenous administration feeling of heat, strengthening of a potoodeleniye, increase in intracranial pressure, locally – phlebitis.

Interaction with other medicines:

At a concomitant use with antiarrhytmic means, (including bepridit, the class drugs IA, соталол), and also Vincaminum, sultopridy, erythromycin for intravenous administration, pentamidine for parenteral administration, the risk of development of ventricular tachycardia like "pirouette" therefore these combinations are contraindicated increases. The antipsychotic drugs derivative of a fenotiazin, phenyl propyl ketone, a difenilbutilpiperidin, antimalarial drugs – derivatives of a hinolon, antihistaminic drugs II of generation increase risk of ventricular arrhythmia: астемизол, терфенадин. The combination therapy with β-adrenoblockers, some blockers of calcium channels (verapamil, diltiazem) as the automatism disturbances (which are shown bradycardia), conductivity (AV blockade) and cardiodepressive action can develop is not recommended. Aritmil together with laxative and other drugs (diuretics, system glucocorticosteroids, Amphotericinum In) which can cause a gipokalemiya as the risk of development of ventricular tachycardia like "pirouette" increases is not recommended to appoint. At simultaneous use with peroral anticoagulants danger of development of bleedings increases (control of level of a prothrombin and a correcting of doses 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. Besides, increase in concentration of digoxin in a blood plasma due to decrease in its clearance is possible (it is necessary to control concentration of digoxin in a blood plasma, to carry out monitoring of an ECG and, if necessary, to change the dosing mode). At simultaneous use with dipheninum, cyclosporine increase in concentration of the last in a blood plasma is possible. Cases of developing of bradycardia (resistant to atropine), arterial hypotension, disturbances of conductivity, decrease in cordial emission at the patients accepting Aritmil and which carried out the general anesthesia or an oxygenotherapy are described.
Under strict control it is possible to appoint drug with anapriliny for summing of effects. In combination with barbiturates Aritmil oppresses TsNS that can lead to development of a depression.

Contraindications:

Sinus bradycardia, sick sinus syndrome (in case of lack of a pacemaker), sinuatrial blockade, AV blockade, heavy disturbances of conductivity (in case of lack of a pacemaker), dysfunctions of a thyroid gland, pregnancy, a lactation, bronchial asthma, hypersensitivity to Amiodaronum and iodine.

Overdose:

Symptoms: a sinus bradycardia, AV blockade, Bouveret's ventricular disease, ventricular tachycardia like "pirouette", arterial hypotension.
Symptomatic treatment. At bradycardia it is necessary to administer the atropine drugs, antagonists of β-adrenoceptors, cardiostimulation. Aritmil and his metabolites are not removed at dialysis.

Storage conditions:

To store in the unavailable to children, protected from light place at a temperature from 15 to 25 the °sena should use drug after the termination of the period of validity specified on packaging! A period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 5 ampoules in the cartridge, on one cartridge in a pack.