Cardiodarone

Cardiodarone is a medication that has coronary vasodilator, antiarrhythmic, antianginal, antihypertensive, and α- and β-adrenergic blocking activity.

Its use results in a decrease in the oxygen demand of the myocardium, a decrease in sensitivity to hyperstimulation of the sympathetic nervous system, and a decrease in coronary vascular tone. At the same time, an increase in coronary circulation, an increase in myocardial energy reserves, and a decrease in heart rate are observed. [ 1 ]

Indications Cardiodarone

It is used for the prevention and treatment of paroxysmal rhythm disorders:

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

Release form

The medicinal substance is released in tablets - 10 pieces inside a blister pack or 30 pieces inside a container.

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

Pharmacodynamics

The medication 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- and β-adrenoreceptors. At the same time, it slows down nodal, atrial and SA conduction, with almost no effect on the conduction processes inside the ventricles. It also slows down the processes of excitation impulse conduction and prolongs the refractory section of additional ducts of the ventricles and atria. [ 3 ]

The antianginal effect is achieved by reducing the volume of oxygen consumed by the myocardium (reducing the heart rate and weakening the cardiac afterload), and in addition by increasing coronary circulation through the direct influence of relatively smooth arterial muscles, maintaining cardiac ejection processes (through reducing aortic pressure) and weakening peripheral resistance.

Pharmacokinetics

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

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

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

Dosing and administration

In case of active phases of rhythm disorders, the drug is administered intravenously at 5 mg/kg; in this case, for people with CHF, the dose is reduced to 2.5 mg/kg.

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

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

In maintenance treatment, the minimum effective dosage for the patient is used. Often, its size is 100-400 mg of Cardiodarone. To avoid accumulation of the drug, it should be taken in a 5-day cycle, after which there should be a 2-day interval.

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

• Application for children

The medication is prescribed to persons under 18 years of age with extreme caution.

Use Cardiodarone during pregnancy

Because amiodarone can cross the placenta, it should not be used during pregnancy.

Contraindications

Main contraindications:

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

The medication is prescribed with extreme caution to people with liver failure or to elderly people.

Side effects Cardiodarone

Side effects include:

• potentiation of CHF, sinus bradycardia, pirouette tachycardia, AV block, decrease in blood pressure values and development of arrhythmia 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 region, as well as jaundice, toxic hepatitis, cholestasis, potentiation of intrahepatic transaminase activity and liver cirrhosis;
• dizziness, depression, memory problems, headaches and paresthesia, auditory hallucinations, weakness, tremor, polyneuropathy and sleep disorders;
• ataxia, increased ICP, neuritis affecting the optic nerve, uveitis, retinal microdetachment, extrapyramidal symptoms, myopathy and lipofuscin deposition within the corneal epithelium;
• anemia of aplastic or hemolytic nature, and thrombocytopenia;
• alopecia, exfoliative dermatitis, epidermal rashes, photosensitivity and gray-blue tint of the epidermis;
• vasculitis, thrombophlebitis, hyperhidrosis and fever, as well as epididymitis and erectile dysfunction.

Overdose

Signs of poisoning: bradycardia, arrhythmia, decreased blood pressure, AV conduction disorder and liver dysfunction.

Gastric lavage and activated charcoal are administered together with a saline laxative. There is no antidote. Symptomatic measures can be taken if necessary. The patient should be constantly monitored – ECG readings and blood pressure levels should be monitored.

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

Interactions with other drugs

It is prohibited to combine the drug with individual 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.

The drug should not be administered together with diuretics, laxatives, GCS and amphotericin B for intravenous injections, as this may provoke ventricular tachycardia (pirouette).

Use together with oral anticoagulants increases the likelihood of bleeding (it is necessary to monitor prothrombin levels and adjust the dose of anticoagulants).

Administration in combination with SG may provoke disorders of automatism (in the form of severe bradycardia) and conduction disorders within the ventricles and atria (the drug increases plasma digoxin levels, which is why they need to be constantly monitored, and in addition, an ECG should be performed and, if necessary, the dosage portion of the drug should be adjusted).

Use with cyclosporine and phenytoin may lead to an increase in their plasma levels.

In patients receiving Cardiodarone who undergo general anesthesia or oxygen therapy, bradycardia (resistant to atropine), conduction disturbances, decreased blood pressure and decreased cardiac output may occur.

Storage conditions

Cardiodarone should be stored in a dark, dry place.

Shelf life

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

Analogues

The analogs of the drug are Ritmorest, Amiodarone and Amiocordin with Cordarone, Aldarone and Concor with Anaprilin, as well as Sedacorone and Ritmiodaron.