Cardiodarone

Cardiodarone is a drug that has coronary dilator, antiarrhythmic, antianginal, antihypertensive, as well as α- and β-adrenergic blocking activity.

Thanks to its use, the oxygen demand of the myocardium decreases, the sensitivity to hyperstimulation concerning the sympathetic NA decreases, and the coronary vascular tone decreases. Along with this, there is an increase in coronary circulation, an increase in energy reserves of the myocardium, as well as a decrease in heart rate indicators. [1]

Indications Cardiodarone

It is used to prevent and treat with paroxysmal rhythm disorders:

• life-threatening ventricular arrhythmias;
• ventricular tachycardia ;
• angina pectoris;
• arrhythmias of the supraventricular type;
• prevention of the development of ventricular fibrillation ;
• paroxysm with atrial flutter and atrial fibrillation;
• arrhythmia that occurs with CHF;
• parasystole.

Release form

The release of the drug substance is made in tablets - 10 pieces inside the contour packs or 30 pieces inside the container.

In addition, it is realized in the form of a liquid for making intravenous injections.

Pharmacodynamics

The drug demonstrates antianginal and antiarrhythmic effects.

Antiarrhythmic activity develops with prolongation of the 3rd stage of the influence potential - by weakening the potassium passage through the channels inside the cell walls of cardiomyocytes. In addition, there is an extension of the refractory segment and a decrease in myocardial excitability. [2]

The drug has a non-competitive blocking effect on α- as well as β-adrenergic receptors. At the same time, it slows down the nodal, atrial and CA-conduction, almost without affecting the conduction processes inside the ventricles. It also slows down the processes of conduction of excitation impulses and prolongs the refractory segment of the additional ducts of the ventricles and atria. [3]

The antianginal effect is provided by a decrease in the volume of oxygen consumed by the myocardium (a decrease in the heart rate and a weakening of cardiac afterload), and in addition, an increase in coronary circulation through the direct influence of relatively smooth arterial muscles, maintenance of heart ejection processes (through a decrease in aortic pressure) and a weakening of peripheral resistance.

Pharmacokinetics

When administered orally, the drug is absorbed at a low rate inside the gastrointestinal tract. Bioavailability values range from 30-80%. The medication is determined inside the blood after 0.5-4 hours. The indicator of blood Cmax with a single administration of Cardiodarone is recorded after 3-7 hours.

Intrahepatic metabolic processes are realized with the formation of a metabolic element with a therapeutic effect (decetylamiodarone), and in addition, with deiodination.

Excretion occurs at an extremely low rate; half-life term - within 20-100 days.

Dosing and administration

In the case of active phases of rhythm disorders, the drug is used in / in the way - at 5 mg / kg; while for people with CHF, the portion is reduced to 2.5 mg / kg.

The tablets must be taken with or after food, swallowed whole and washed down with plain water. The portion size is selected by the doctor personally - taking into account the patient's condition. The initial dosage per day is often in the range of 600-800 mg (must be divided into 2-3 uses). If required, the portion can be increased to 1200 mg per day.

Such dosages are used in the period of 8-15 days, and then the patient is transferred to supportive treatment.

With maintenance treatment, the minimum effective dosage for the patient is used. Often, its size is 100-400 mg of Cardiodarone. To avoid drug accumulation, it should be consumed in a 5-day cycle followed by a 2-day interval.

In addition, the tablets can be used for a period of 3 weeks, after which take a 7-day break.

• Application for children

For persons under the age of 18, the medication is prescribed with extreme caution.

Use Cardiodarone during pregnancy

Because amiodarone is able to cross the placenta, it should not be used during pregnancy.

Contraindications

The main contraindications:

• sinus bradycardia;
• cardiogenic shock;
• severe intolerance to the elements of the drug;
• SA blockade;
• hypokalemia;
• Stage 2-3 AV block;
• hypothyroidism or hyperthyroidism;
• SSSU;
• collapse;
• pulmonary lesions of the interstitial type;
• decrease in blood pressure;
• use of MAOI drugs;
• breast-feeding.

People with insufficient liver function or the elderly are prescribed medication with extreme caution.

Side effects Cardiodarone

Among the side effects:

• potentiation of CHF, sinus-type bradycardia, tachycardia "pirouette", AV blockade, a decrease in blood pressure values and the development of arrhythmias or potentiation of an existing one;
• pleurisy, apnea, pulmonary fibrosis, cough and dyspnea, pneumonia, bronchial spasm, alveolitis and the appearance of hyper- or hypothyroidism;
• vomiting or nausea, bloating, constipation, loss of appetite, diarrhea, pain and heaviness in the epigastric zone, and in addition, jaundice, hepatitis of a toxic nature, cholestasis, potentiation of the activity of intrahepatic transaminases and hepatic cirrhosis;
• dizziness, depression, memory problems, headaches and paresthesias, auditory hallucinations, weakness, tremors, polyneuropathy and sleep disturbances;
• ataxia, increased ICP values, neuritis affecting the optic nerve, uveitis, retinal microdetachment, extrapyramidal symptoms, myopathy and lipofuscin deposition inside the corneal epithelium;
• anemia of aplastic or hemolytic nature and thrombocytopenia;
• alopecia, exfoliative dermatitis, epidermal rashes, photosensitivity and blue-gray tinge of the epidermis;
• vasculitis, thrombophlebitis, hyperhidrosis and fever; and epididymitis and erectile dysfunction.

Overdose

Signs of poisoning: bradycardia, arrhythmias, decreased blood pressure, AV conduction disorder and hepatic dysfunction.

Gastric lavage is performed and activated charcoal is applied along with a saline-type laxative. There is no antidote. If necessary, symptomatic measures can be performed. The patient needs to be constantly monitored - to monitor the ECG readings and the blood pressure level.

In the case of bradycardia, atropine with β1-adrenergic agonists is used, and a temporary pacemaker is installed. Hemodialysis does not lead to the excretion of amiodarone.

Interactions with other drugs

It is forbidden to combine the drug with separate Ca channel blockers (diltiazem or verapamil) and β-blockers, because this can lead to disorders of automatism (in the form of bradycardia), as well as conduction.

You can not enter the medication together with diuretics, laxatives, GCS and amphotericin B for intravenous injections, as this can provoke ventricular tachycardia ("pirouette").

Use together with oral anticoagulants increases the likelihood of bleeding (it is required to monitor prothrombin parameters and adjust the amount of anticoagulants).

Administration in combination with FH can provoke automatism disorders (in the form of severe bradycardia) and conduction disturbances inside the ventricles and atria (the drug increases the plasma values of digoxin, which is why they need to be constantly monitored, and in addition, an ECG should be performed and, if necessary, corrected dosage portion of drugs).

The use together with cyclosporine and phenytoin can lead to an increase in their plasma parameters.

People using Cardiodarone who are undergoing general anesthesia or oxygen therapy may develop bradycardia (resistant to atropine), conduction disturbances, decreased blood pressure, and decreased cardiac output.

Storage conditions

Cardiodarone should be stored in a dark and dry place.

Shelf life

Cardiodarone can be used within 24 months from the date of manufacture of the drug substance.

Analogs

Analogues of drugs are Ritmorest, Amiodarone and Amiocordin with Cordarone, Aldaron and Concor with Anaprilin, as well as Sedacoron and Ritmiodarone.