Kardiodaron-Zdorovye, 5% solution for infection. 3 ml No. 10

General characteristics. Structure:

International and chemical names: amiodarone, { 2-butyl-3-benzofuranil 4 (2-diethyl-aminoetoksi) - 3,5-diyodofenit ketone a hydrochloride };
main physical and chemical properties: transparent solution from yellowish till greenish-yellowish color;
structure: 1 ampoule (3 ml) contains 150 mg of Amiodaronum of a hydrochloride (in recalculation for 100% substance); 
excipients: polysorbate – 80 (the twin - 80), benzyl alcohol, 0,1 M acid solution hydrochloric, water for injections.

Pharmacological properties:

Pharmacodynamics. Antiarrhytmic and anti-anginal means. Blocks ion channels of cellular membranes of cardiomyocytes, more – potassium and to a lesser extent – calcic and sodium, slows down excitement alpha and beta adrenoceptors. Increases the 3rd phase of action potential, reduces automatism of a sinus node, slows down sinuatrial, atrial and nodal conduction, does not exert impact on intra ventricular conductivity, 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 is also caused by decrease in consumption of oxygen a myocardium due to reduction of heart rate and the general peripheric vascular resistance, increase in a coronary blood-groove by direct impact on smooth muscles of arteries, maintenance of cordial emission due to pressure decrease in an aorta. Does not render a significant negative inotropic effect.
Amiodaronum contains 37% of iodine, can exert impact on metabolism of hormones of a thyroid gland with development of the phenomena hypo - or a hyperthyroidism. 

Pharmacokinetics. After intravenous administration concentration of Amiodaronum in blood quickly decreases, at the same time its distribution and accumulation almost in all tissues, especially fatty and muscular tissues of a myocardium is observed. Elimination from an organism begins in several days. The elimination half-life makes 20 - 100 days. Amiodaronum is removed with bile and a stake, renal excretion is insignificant. Removal of drug continues within several months.

Indications to use:

Paroxysmal arrhythmias; Wolf's syndrome – Parkinson – Whyte; trembling and atrial fibrillation; ventricular tachycardia; atrial and ventricular premature ventricular contraction.

Route of administration and doses:

Appoint in the form of intravenous infusions. The initial dose makes usually 5 mg/kg in 250 ml of 5% of solution of glucose within 20 - 120 min. Speed of injection should be adjusted according to results. The therapeutic effect of drug is shown within the first minutes of introduction and disappears gradually. It is possible to repeat introduction 2 - 3 times within 24 hours. The supporting infusion: 10 - 20 mg/kg/days (on average 600 - 800 mg/days) in 250 ml of 5% of solution of glucose within several days. The maximum daily dose – 1200 mg. From the first day of infusions it is necessary to begin gradual transition to oral administration.

Features of use:

Kardiodaron-Zdorovye it has to be applied only in specialized departments of hospitals under constant control of arterial pressure, heart rate and indicators of an ECG. Possible changes of an ECG (are especially visible in assignments of V1 and V5): moderate lengthening of an interval of Q-T (at not changed QRS complex duration), expansion of a tooth of T, decrease in its amplitude, flattening of top or a dvugorbost, emergence of a tooth of U. The specified phenomena appear approximately for the 4th day from an initiation of treatment at 75% of patients, remain within a week after its termination and are considered as saturation signs by drug. With care appoint drug at disturbances of electrolytic balance.
Due to the high content of iodine in drug the patients having genetic predisposition to diseases of a thyroid gland should be careful at purpose of Kardiodarona-Zdorovye. In order to avoid development of a photosensitization patients should avoid stay in the sun.
At reduction of a dose and drug withdrawal regression of manifestations of side effects is possible. To pregnant women and the feeding women appoint only according to vital indications. Safety and efficiency of use of Amiodaronum for treatment of children is not studied. People of advanced age, especially with dysfunction of a thyroid gland, can have a hypersensitivity to Amiodaronum. 

Side effects:

Bradycardia, in rare instances – an asystolia; atrioventricular block; aritmogenny action; lowering of arterial pressure (usually moderate and passing); a bronchospasm, an apnoea (at patients with heavy respiratory insufficiency); abnormal liver function; allergic skin reactions; muscular weakness, tremor, sleeplessness; feeling of heat, nausea, perspiration; locally - phlebitis. At jet intravenous administration the acute anaphylaxis and increase in intracranial pressure are possible.

Interaction with other medicines:

Kardiodaron-Zdorovye it is incompatible with antiarrhytmic drugs (including bepredit, class drugs I, сотолол), and also with lidoflazinum, sultopridy, Prenylaminum, Vincaminum and erythromycin for intravenous administration. Combined use of Kardiodarona-Zdorovye with the verapamil, diltiazem, MAO inhibitors, beta adrenoblockers increasing risk of developing of hypotension and bradycardia and also with laxatives of the stimulating type is not recommended.
Kardiodaron-Zdorovye strengthens effect of Phenytoinum, indirect anticoagulants, glycosides, considerably increasing their concentration in blood. Holestiramin reduces an elimination half-life and level of Amiodaronum in plasma, Cimetidinum – increases. 
Extra care is demanded by combined use of Kardiodarona-Zdorovye and drugs possessing gipokaliyemichesky action (diuretics, glyuko-and mineralokortikoida, тетракосактид, Amphotericinum In at intravenous administration), and also its appointment as the patient with heavy diarrhea. Joint purpose of the specified drugs demands control of an ECG and optimization of dosages of drugs. Cases of developing of bradycardia, arterial hypotension, disturbance of conductivity and decrease in cordial emission at the patients who underwent the general anesthesia or an oxygenotherapy are described.

Contraindications:

Atrioventricular block, the expressed conductivity disturbances, sinus bradycardia, sick sinus syndrome, cardiogenic shock, collapse, the expressed arterial hypotension, dysfunction of a thyroid gland, hypersensitivity to iodine, pregnancy, the lactation period.

Overdose:

Symptoms: bradycardia, hypotension, atrioventricular block, cardiogenic shock, asystolia, Bouveret's ventricular disease, including pirouette type, disturbance of blood circulation, abnormal liver function. Treatment: dialysis is inefficient. Precautionary measures: slow administration, use of minimum effective doses of drug and careful choice of a combination therapy.

Storage conditions:

To store in the place protected from light at a temperature from 15 °C to 25 °C. To store the place, unavailable to children. 
Period of validity – 2 years. 

Issue conditions:

According to the recipe

Packaging:

On 10 ampoules in a pack.