Cordarone
Cordarone
Cordarone (Amiodarone)Pharmacological action
Antiarrhytmic preparation of III class. Antiarrhytmic and antianginal an effect has.
Antiarrhytmic action is caused by augmentation of 3 phases of an action potential, basically at the expense of depression of a current of a potassium through channels of cellular membranes of cardiomyocytes. Slows down sinuatrial, atrial and nodal conductivity, not rendering influence on intraventricular conductivity. Cordarone enlarges the refractory period and reduces excitability of a myocardium. Slows down carrying out of excitation and extends the refractory period of additional atrioventricular ways.
Antianginal Cordarone action is caused by depression of consumption of oxygen by a myocardium, not competitive blockade a - and b-adrenoretseptorov, augmentation of a coronary blood flow by direct influence on a smooth musculation of arteries, maintenance of warm emission by pressure decrease in an aorta and depression of peripheric resistance.
Cordarone does not render significant negative inotropic effect, reduces contractility of a myocardium in the basic ambassador i.v. introductions.
It is defined in a blood plasma throughout 9 months after the termination of its reception.
Therapeutic effects are observed in 1 week (from several days till 2 weeks) after the beginning of reception of a preparation inside.
At i.v. Cordarone introduction its activity reaches a maximum through 15 mines and disappears approximately through 4 h after introduction. In spite of the fact that the quantity Cordarone entered in blood quickly decreases, reached saturation of tissues by a preparation. In the absence of repeated injections the preparation is gradually deduced. At renewal of its introduction or at appointment of a preparation for intake it is formed it fabric has reserved.
Indications
Cupping of attacks of a Bouveret's disease
- Cupping of attacks of a ventricular Bouveret's disease;
- Ventricular arrhythmias menacing to a life and fibrillation of ventricles of heart;
- A ciliary arrhythmia (fibrillation of auricles) and an atrial flutter.
- After recently transferred myocardial infarction, 10 ventricular extrasystoles having more at 1 o'clock, clinical implications of a chronic heart failure and the lowered fraction of emission of a left ventricle.
Cordarone especially it is recommended to patients with organic diseases of heart (including from an ischemic heart disease), accompanied by left ventricle dysfunction.
Cordarone for i.v. introduction it is intended for only for application in a hospital when fast achievement of antiarrhytmic effect or when preparation reception inside is impossible is required.
Dosage regimen
For intake
At preparation appointment in a loading dose various schemes can be used. At application in a hospital the initial dose parted on some receptions, makes from 600-800 mg/sut to the maximum 1200 mg/sut before achievement of a total dose 10 g (usually within 5-8 days).
At out-patient appointment the initial dose parted on some receptions, makes from 600 mg to 800 mg/sut before achievement of a total dose 10 g (usually within 10-14 days).
The maintenance dose is defined from calculation of mass of a body of 3 mg/kg a day and can be in limits from 100 mg/sut to 400 mg/sut at reception of 1 times/days it is necessary to apply the minimum effective dose. Since Amiodaronum has very big period of semideducing, the preparation can be accepted every day (200 mg it is possible to give every day, and 100 mg are recommended to be accepted daily) or to do breaks (2 days in a week).
For a solution for i.v. introduction
Loading Cordarone dose makes originally 5-7 mg/kg of mass of a body in 250 ml 5 %-s solutions Dextrosums (glucoses) within 30-60 minutes Therapeutic Cordarone effect is shown within the first minutes of introduction and disappears gradually, that demands correction of rate of its introduction according to results of treatment.
For a maintenance therapy a preparation prescribe in the form of constant or intermittent (2-3 times/sut) i.v. infusions in 5 % a solution Dextrosums (glucoses) within several days in a dose to 1200 mg/sut before achievement of a total dose of 10 After i.v. introduction in a loading dose instead of continuation i.v. infusions it is possible transition to Cordarone reception inside in a dose from 600-800 mg to 1200 mg/24h before achievement of a total dose of 10 From first day i.v. Cordarone introductions expediently to begin gradual transition to preparation reception inside.
At carrying out i.v. injections in a dose of 5 mg/kg enter a preparation within at least 3 minutes Cordarone it is impossible to type in one syringe with other medical products!
It is not necessary to apply concentration to i.v. infusion below 600 mg/l. For preparation of solutions for i.v. introduction to use only 5 % a solution Dextrosums (glucoses).
Side effect
Solution for injections
System reactions: sensation of the fever, the raised diaphoresis, BP depression (usually moderated and transient); cases of a serious arterial hypotension or a collapse (have been registered at an overdosage or too fast introduction), a moderate bradycardia; on occasion - the aggravation of an arrhythmia sometimes accompanied by a cardiac standstill (on available data it is impossible to establish connection with preparation application, with gravity of a lesion of heart or with a treatment inefficiency). In the therapy beginning rising of activity of hepatic transaminases in blood serum which usually remains moderated (in 1 time above the top border of norm/VGN/) becomes perceptible and, as a rule, is normalised at a dose decline or even is spontaneous. At substantial increase of level of transaminases treatment should be stopped. There are separate reports on cases of acute hepatic insufficiency with high level of hepatic transaminases in blood serum and-or an icterus (some with a lethal outcome). In individual (exclusively rare) cases became perceptible - an anaphylactic shock, a good-quality intracranial hypertensia (a brain pseudoneoplasm), in particular at sick of a bronchial asthma.
Local reactions: a phlebitis (it is possible to avoid at use of the central venous catheter).
From a sight organ: lipofuscin microadjournment in an eye cornea (almost always present) are usually limited by pupil area, are reversible after preparation cancellation, sometimes lead to disturbance of sight in the form of occurrence of the painted aura at bright illumination or sensations of a fog; on occasion - an optic nerve neuropathy/NEURITIS (communication with reception by Amiodaronum by present time accurately is not established).
Dermatological reactions: a photosensitization; an erythema (at radiotheraphy carrying out); on occasion - an eruption (usually nonspecific), an exfoliative dermatitis (communication with preparation reception formally is not established); at long application in high doses - a grayish or bluish xanthopathy (after the treatment termination slowly disappears).
From endocrine system: rising of level T3 in blood serum (T4 remains normal or slightly lowered); hypothyrosis development (masses of the body weakly expressed augmentation, the lowered activity more expressed/in comparison with expected / bradycardia) is possible; a hyperthyroidism. The suspicion on a hyperthyroidism can arise at the following weakly expressed clinical symptoms: loss of mass of a body, arrhythmia development, a stenocardia, a heart failure.
From the alimentary system: a nausea, vomiting, taste disturbances (usually meet in the therapy beginning at application in loading doses and decrease at a dose decline); in the treatment beginning - the isolated rising activity of hepatic transaminases (decrease at a dose decline of a preparation or even it is spontaneous); on occasion - acute disturbances of function of a liver and-or an icterus (preparation cancellation demand), a fatty hepatosis, a cirrhosis. Clinical symptoms and laboratory changes can be minimum; therefore during treatment the regular control of function of a liver is recommended.
From respiratory system: on occasion - a pneumonitis, a fibrosis, a pleuritis, an obliterating bronchiolitis with a pneumonia (sometimes coming to an end with a lethal outcome), a bronchospasm at patients with serious respiratory diseases (especially with a bronchial asthma), an acute respiratory distress-syndrome at adults.
Allergic reactions: seldom - a vasculitis, a lesion of kidneys with rising of level of a creatinine, a thrombocytopenia; on occasion - a hemolitic anaemia, aplastic anemias.
The other: an alopecia; on occasion - an epididymitis, an impotency.
Contraindications
For tablets
- Disturbances AV - and intraventricular conductivity (AV-blockade II and III degrees, blockade of legs of a ventriculonector) in the absence of the artificial driver of a rhythm (cardiostimulator);
- Simultaneous application of the preparations, capable to cause a polymorphic ventricular tachycardia of type "pirouette";
- Thyroid gland dysfunction (a hypothyrosis);
- A hypopotassemia;
- A heart failure (in a decompensation stage);
- Simultaneous reception of inhibitors MAO;
- Intersticial illnesses of lungs;
- Age till 18 years (efficiency and safety are not established);
- Pregnancy;
- A lactemia;
- A hypersensibility to iodine and-or Amiodaronum.
For a solution for i.v. introduction
- AV-blockade II and III degrees, disturbance of intraventricular conductivity (blockade of two and three legs of a ventriculonector); in these cases Amiodaronum can be i.v. used in specialised units under cover of the artificial driver of a rhythm (cardiostimulator);
- Acute cardiovascular insufficiency (a shock, a collapse);
- The expressed arterial hypotension;
- Simultaneous application with the preparations, capable to cause a polymorphic ventricular tachycardia of type "pirouette";
- Thyroid gland dysfunctions (a hypothyrosis, a hyperthyroidism);
- Pregnancy;
- A lactemia;
- Age till 18 years (efficiency and safety are not established);
With care apply at a chronic heart failure, hepatic insufficiency, a bronchial asthma, in advanced age.
Pregnancy and lactemia
At Cordarone pregnancy prescribe only under vital indications since the preparation has an effect on a foetus thyroid gland.
Amiodaronum is allocated with thoracal milk in significant amounts, therefore the preparation is contraindicative to application in a lactemia.
Special indicatings
With care prescribe Cordarone at disturbances of electrolytic balance since there are separate reports on development or advance of arrhythmias (up to a cardiac standstill). Before the beginning and in the course of treatment treatment it is recommended to spend definition of level of a potassium in blood serum. However now it is not obviously possible to differentiate the changes bound to reception of a preparation, and the changes which are bound to available diseases of heart or growing out of insufficient efficiency of treatment.
Before the beginning and in the course of treatment it is recommended to spend an electrocardiogram-research.
It is necessary to consider, that at patients of advanced age more expressed depression of the CARDIAC CONTRACTIONS RATE becomes perceptible.
Occurrence of a dyspnea or unproductive tussis can be bound to toxic Cordarone action on lungs. At patients with an accruing dyspnea at exercise stresses, without dependence from deterioration of their general condition (the raised weariness, loss of mass of a body, a fervescence), before the therapy beginning it is necessary to spend thorax roentgenography. Disturbances from respiratory system basically are reversible at early cancellation of Amiodaronum. Clinical symptoms usually pass within 3-4 weeks, and then there is slower restoration of a X-ray pattern and function easy (some months).
Influence on ability to driving of motor transport and to management of mechanisms
Now there are no data that Cordarone influences ability to driving of motor transport and management of mechanisms.
Overdosage
Symptoms: a sinus bradycardia, a cardiac standstill, a ventricular tachycardia of type "pirouette", disturbances of a circulation, disturbance of function of a liver, BP depression.
Treatment: spend symptomatic therapy. Amiodaronum and its metabolites do not leave at a dialysis.
Medicinal interaction
At simultaneous Cordarone reception with antiarrhytmic agents, and also with Vincaminum, erythromycin for i.v. introduction, a pentamidine for parenteral introduction enlarges risk of development of a ventricular tachycardia of type "pirouette". Therefore the given combinations are contraindicative.
The combined therapy with the beta adrenoblockers, some blockers of calcium channels (verapamil) is not recommended, since automatism disturbances (shown by a bradycardia) and conductions can develop.
It is not recommended to apply Cordarone simultaneously with purgative preparations which can cause a hypopotassemia since the risk of development of a ventricular tachycardia of type "pirouette" is enlarged.
At simultaneous Cordarone application with anticoagulants for intake the risk of development of bleedings (therefore it is necessary to supervise level of a prothrombin and to correct a dose of anticoagulants) is enlarged.
At simultaneous Cordarone application with warm glycosides automatism disturbances (shown by the expressed bradycardia) and disturbances of atrioventricular conductivity can be observed. The augmentation of concentration of digoxin in a blood plasma at the expense of depression of its clearance (therefore it is necessary to supervise concentration of digoxin in a blood plasma to spend an electrocardiogram and if necessary to change a dosage regimen) is besides, possible.
Cases of occurrence of a bradycardia (refractory to atropine), an arterial hypotension, disturbances of conductivity, depression of warm emission at the patients who were accepting Cordarone and exposed to the general anaesthesia are described.
At oxygenotherapy application in the postoperative period at the patients receiving Cordarone, rare cases of development of the serious respiratory complications which sometimes were coming to an end with a lethal outcome are described.
Conditions and periods of storage
The preparation should be stored in the place protected from light at a room temperature (not above 25 C). The Period of validity of tablets - 3 years. A period of validity of a solution for injections - 2 years.
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