Capoten daily dose. At what pressure is Capoten prescribed: instructions for use

How to take Cordarone for arrhythmia?

To normalize the heart rate, it is important to choose the most effective drug– in accordance with the spectrum of its effects and the nature of the arrhythmia. At the same time, it must be as safe as possible. At atrial fibrillation(MA) “Cordarone” occupies a wide niche of applicability.

Composition and release form

"Cordarone" is a drug called amiodarone hydrochloride. The product is produced in tablets (200 mg of amiodarone hydrochloride with a dividing line) and in solution for injection (3 ml ampoules containing 150 mg of amiodarone hydrochloride). The medicine is produced by Sanofi Winthrop Industry (France), Quinoin (Hungary).

Cordarone is a unique product of its kind

Cordarone is administered intravenously in emergency situations (with life-threatening attacks of arrhythmia, in a hospital), with monitoring of ECG and blood pressure (BP), since there is a high risk of a critical drop in blood pressure and terminal heart failure. "Cordarone" is administered slowly, diluted with 5% glucose solution.

Pharmacological effects

"Cordarone" affects a number of factors affecting the reactivity and electrical conductivity of the sinoatrial and atrioventricular nerve nodes:

"Cordarone" is able to partially block potassium, sodium and calcium channels cell membranes, He:

slows down the passage of potassium and sodium ions through the myocardial membranes, lengthening the action potential and the effective refractory period, that is, the heartbeat becomes measured and calm;
due to partial blockade of calcium transport, it expands peripheral vessels, reducing total peripheral resistance.

Reduces the sensitivity of heart adrenergic receptors to stress hormones.
Reduces the stimulating influence of hormones thyroid gland on the myocardium, inhibiting one of the links in their synthesis.

Since “Cordarone” affects many factors and little by little, it is relatively safe, as far as, in general, we can talk about the safety of use in relation to regulators heart rate.

In addition, Cordaron expands coronary vessels and reduces blood pressure

Who is Cordaron indicated for?

The choice is made in favor of “Cordaron” if:

in a patient with arrhythmia, normal or decreased arterial pressure, and it cannot be further reduced;
CHF is present and cannot be reduced contractility hearts;
the patient does not have serious structural heart damage;
The production of thyroid hormones is approximately within normal limits.

"Cordarone" is used for:

stopping episodes paroxysmal tachycardia, paroxysms and permanent form of MA.
prevention of repeated episodes of ventricular arrhythmias and fibrillations, AF attacks, sudden, possibly fatal arrhythmia in post-infarction patients.

Contraindications

Cordarone is contraindicated for:

sinus node dysfunction and atrioventricular (AV) block II and III degree(without pacemaker);
hypokalemia, hypomagnesemia;
diseases connective tissue lungs, non-cardiogenic pulmonary edema;
the production of thyroid hormones is less than normal or above normal;
prolongation of electrical systole on the ECG;

There are no medications without contraindications for their use. For “Kordaron” this is: periods of pregnancy and breastfeeding

taking substances that prolong the electrical systole and can provoke paroxysmal tachycardia, including pirouette-type tachycardia;
childhood;
pregnancy and breastfeeding;
intolerance to iodine or amiodarone itself.

"Cordarone" is undesirable:

with severe CHF;
weakened liver function;
insufficiency respiratory function and bronchial asthma;
V old age;
with AV block of the first degree.

Side effects

Side effects(pills):

moderate bradycardia (in 1–10% of cases);
sinotrial or atrioventricular block (0.1–1%);
provoking new arrhythmias or complication of existing ones, both as a result of the action of the drug and due to its inefficiency - 0.1–1%;
nausea, vomiting, unwillingness to eat, heaviness in the stomach - 10% or more when taking saturating doses;
increased liver transaminases and bile pigments, development of liver failure (1-10%);
development chronic diseases liver – less than 0.01% of cases;
pneumonitis and bronchiolitis obliterans (1–10%);
bronchospasm, pulmonary edema (less than 0.01%);

Common adverse reactions to Cordarone: nausea and vomiting

blurred vision caused by lipid deposits in the cornea (common), neuritis optic nerve(very rarely). With neuritis, the drug is urgently canceled;
hypothyroidism, hyperthyroidism (quite often);
increased sensitivity of the skin to solar radiation (almost always);
trembling limbs, sleep disturbances.

Side effects of the injection solution:

heat (" hot prick”), decreased blood pressure, bradycardia varying degrees expressiveness;
provoking arrhythmias (rarely);
increased levels of liver transaminases;
anaphylactic shock, increase intracranial pressure, bronchospasm (extremely rare);
phlebitis at the injection site.

Dosage of Cordarone for arrhythmia

At the beginning of taking Cordarone tablets in the hospital, the total (distributed) daily dose is prescribed from 600 to 1200 mg. The patient takes the drug in this amount for approximately a week until he consumes the “satiating” amount – 10 grams. Next, a maintenance dose of 100–400 mg per day is prescribed. The lowest dose possible to maintain the antiarrhythmic effect should be selected to avoid side effects.

Take Cordarone exactly as prescribed

At home, for safety reasons, the saturation period is extended to approximately 2 weeks, prescribing from 600 to 800 mg per day (in several doses). Upon reaching a saturating amount of 10 g, a maintenance dose is selected for the patient.

Maximum possible single dose 400 mg. "Kordaron" is slowly excreted from the body, so schemes with a maintenance dose every other day are possible. The duration of maintenance therapy with "Kordaron" is from several months to 2 years.

Overdose

Acute overdose, symptoms:

a sharp slowdown in heart rate;
tachycardia, including the “pirouette” type;
increased CHF;
heart failure.

There is no specific antidote to Cordarone. If the drug has just been taken, it is necessary to rinse the stomach, give Activated carbon and call an ambulance; to stop the effects of an overdose, it may be necessary to administer adrenaline or magnesium salts, or pacing.

How to take Cordarone during an attack of arrhythmia?

"Cordarone" is used to relieve an attack in cardiology department or at least in the presence of an emergency doctor. It is dangerous to drink it on your own during an arrhythmia attack.

Cordarone in tablet form should be swallowed with water.

Interaction with other drugs

Cordarone should not be taken in parallel with:

β-blockers, other antiarrhythmic drugs and blockers calcium channels(“Verapamil”, “Diltiazem”);
antipsychotic drugs (including Sultopride) and antidepressants (MAO inhibitors);
"Pentamidine", "Vincamine", "Erythromycin".

It is undesirable to take Kordaron with laxatives and diuretics (potassium deficiency is possible). If it is necessary to take anticoagulants, the level of prothrombin is controlled ( increased risk bleeding); cardiac glycosides – digoxin level (digoxin excretion decreases). List drug interactions incomplete, you must carefully study the instructions for the drug.

special instructions

During the Cordarona course:

alcohol is contraindicated;
exposure to the sun should be avoided. In addition to the possibility of burns, pigmentation acquires unnatural grayish shades;
you need to refrain from driving a car and requiring high speed class reactions.

Analogues of Kordaron - Amiodaron, Amiocordin, Aritmil, Cardiodaron, Rotaritmil. "Cordarone" is sold by prescription. The price of tablets No. 30 is from 300 rubles or 200 hryvnia.

Reviews about Cordarone indicate its effectiveness in arrhythmias and a real statistical increase in patient survival, but, unfortunately, also the presence side effects. Thyroid dysfunction is the most commonly reported disorder.

sosudoff.ru

CORDARON

DOSAGE FORM, COMPOSITION AND PACKAGING

Tablets are round, divided, white or white with a creamy tint, engraved with a symbol in the form of a middle and the number "200" on one side; tablets can be easily separated along the break line when normal conditions applications.

1 tab. amiodarone hydrochloride 200 mg

Excipients: lactose monohydrate, corn starch, polyvidone K90F, colloidal anhydrous silicon dioxide, magnesium stearate.

10 pieces. - blisters (3) - packs of cardboard.

PHARMACHOLOGIC EFFECT

Class III antiarrhythmic drug. Has antiarrhythmic and antianginal effects.

The antiarrhythmic effect is due to an increase in the 3rd phase of the action potential, mainly due to a decrease in the potassium current through the channels of the cell membranes of cardiomyocytes and a decrease in the automatism of the sinus node. The drug non-competitively blocks α- and β-adrenergic receptors. Slows down sinoatrial, atrial and nodal conduction without affecting intraventricular conduction. Cordarone increases the refractory period and reduces myocardial excitability. Slows down the conduction of excitation and lengthens the refractory period of additional atrioventricular pathways.

The antianginal effect of Kordaron is due to a decrease in myocardial oxygen consumption (due to a decrease in heart rate and a decrease in OPSS), non-competitive blockade of α- and β-adrenergic receptors, an increase in coronary blood flow by direct influence on smooth muscles arteries, maintaining cardiac output by reducing aortic pressure and reducing peripheral resistance.

Cordarone has no significant negative effect inotropic effect, reduces myocardial contractility mainly after intravenous administration.

It affects the exchange of thyroid hormones, inhibits the conversion of T3 to T4 (blockade of thyroxine-5-deiodinase) and blocks the uptake of these hormones by cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium. Determined in blood plasma for 9 months after stopping its use.

Therapeutic effects are observed 1 week (from several days to 2 weeks) after starting to take the drug orally.

With intravenous administration of Cordarone, its activity reaches a maximum after 15 minutes and disappears approximately 4 hours after administration. Despite the fact that the amount of administered Cordarone in the blood quickly decreases, tissue saturation with the drug is achieved. In the absence of repeated injections, the drug is gradually eliminated. When its administration is resumed or when the drug is prescribed for oral administration, its tissue reserve is formed.

PHARMACOKINETICS

Suction

After oral administration, amiodarone is absorbed slowly (absorption is 30-50%), the rate of absorption is subject to significant fluctuations. Bioavailability after oral administration ranges from 30 to 80% in different patients (on average about 50%). After a single dose of the drug orally, Cmax in blood plasma is achieved within 3-7 hours.

Distribution

Amiodarone has a large Vd. Amiodarone accumulates most in adipose tissue, liver, lungs, spleen and cornea. After a few days, amiodarone is eliminated from the body. Css is achieved within 1 to several months, depending on individual characteristics patient. Binding to blood plasma proteins is 95% (62% to albumin, 33.5% to beta-lipoproteins).

Metabolism

Metabolized in the liver. The main metabolite, desethylamiodarone, is pharmacologically active and can enhance the antiarrhythmic effect of the main compound. Each dose of Cordarone (200 mg) contains 75 mg of iodine; 6 mg of this was determined to be released as free iodine. With prolonged treatment, its concentrations can reach 60-80% of amiodarone concentrations.

breeding

Elimination when taken orally occurs in 2 phases: T1/2 in the α-phase - 4-21 hours, T1/2 in the β-phase - 25-110 days. After prolonged oral administration, the average T1/2 is 40 days (this has important when choosing a dose, because At least 1 month is required for plasma concentrations to stabilize, and complete elimination may take more than 4 months).

After discontinuation of the drug, its complete elimination from the body continues for several months. The presence of pharmacodynamic effects of Cordarone should be taken into account for 10 days and up to 1 month after its discontinuation. Amiodarone is excreted in bile and feces. Renal excretion is negligible.

Pharmacokinetics in special clinical cases

Insignificant excretion of the drug in the urine allows the drug to be prescribed in moderate doses for renal failure. Amiodarone and its metabolites are not dialyzable.

INDICATIONS

Relief of attacks of ventricular paroxysmal tachycardia;

Relief of attacks of supraventricular paroxysmal tachycardia with a high frequency of ventricular contractions (especially against the background of WPW syndrome);

Relief of paroxysmal and stable form atrial fibrillation (atrial fibrillation) and atrial flutter.

Relapse Prevention

Life-threatening ventricular arrhythmias and ventricular fibrillation (treatment should be started in a hospital with careful cardiac monitoring);

Supraventricular paroxysmal tachycardias, incl. documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with organic diseases hearts; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients without organic heart disease, when antiarrhythmic drugs other classes are not effective or there are contraindications to their use; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with WPW syndrome;

Atrial fibrillation (atrial fibrillation) and atrial flutter.

Prevention of sudden arrhythmic death in patients from the group high risk after recently suffered a heart attack myocardium having more than 10 ventricular extrasystoles at 1 o'clock, clinical manifestations chronic heart failure and reduced left ventricular ejection fraction (Cordarone is especially recommended for patients with organic heart disease (including coronary heart disease) accompanied by left ventricular dysfunction.

Cordarone for intravenous administration is intended only for use in a hospital in cases where rapid achievement of an antiarrhythmic effect is required or when it is impossible to take the drug orally.

DOSING REGIME

For oral administration

When prescribing the drug in a loading dose, various schemes can be used. When used in a hospital, the initial dose, divided into several doses, ranges from 600-800 mg/day to a maximum of 1200 mg/day (usually for 5-8 days).

For outpatient use, the initial dose, divided into several doses, ranges from 600 mg to 800 mg / day (usually for 10-14 days).

The maintenance dose is determined at the rate of 3 mg/kg body weight per day and can range from 100 mg/day to 400 mg/day when taken once a day. The minimum effective dose should be used. Because Amiodarone has a very long half-life, the drug can be taken every second day (200 mg can be given every second day, and 100 mg is recommended to be taken daily) or taken in breaks (2 days a week).

For solution for intravenous administration

The loading dose of Cordarone is initially 5-7 mg/kg body weight in 250 ml of a 5% dextrose (glucose) solution for 30-60 minutes. Therapeutic effect Cordarone appears during the first minutes of administration and disappears gradually, which requires adjustment of the rate of its administration in accordance with the results of treatment.

For maintenance therapy, the drug is prescribed as a continuous or intermittent (2-3 times/day) intravenous infusion in a 5% dextrose (glucose) solution for several days at a dose of up to 1200 mg/day. After intravenous administration at a loading dose, instead of continuing intravenous infusion, it is possible to switch to taking Kordarone orally at a dose of 600-800 mg to 1200 mg / day. From the first day of intravenous administration of Kordaron, it is advisable to start a gradual transition to taking the drug orally.

When conducting intravenous injections, the drug at a dose of 5 mg / kg is administered for at least 3 minutes. Cordarone cannot be put into the same syringe with others. medicines!

For intravenous infusion, concentrations below 600 mg/l should not be used. For the preparation of solutions for intravenous administration, use only 5% dextrose (glucose) solution.

SIDE EFFECT

Solution for intravenous administration

Systemic reactions: feeling of heat, increased sweating, decreased blood pressure (usually moderate and transient); cases of severe arterial hypotension or collapse (have been reported with overdose or too rapid administration), moderate bradycardia (in some cases, especially in elderly patients, severe bradycardia and, in exceptional cases, sinus node arrest, requiring discontinuation of therapy); rarely - proarrhythmic effect. At the beginning of therapy, there is an increase in the activity of liver transaminases in the blood serum, which usually remains moderate (1.5-3 times higher upper limit norms /ULN/) and, as a rule, normalizes when the dose is reduced or even spontaneously. If transaminase levels increase significantly, treatment should be discontinued. There are isolated reports of cases of acute liver failure with high level serum liver transaminases and/or jaundice (some with fatal). In isolated (exceptionally rare) cases, anaphylactic shock, benign intracranial hypertension(pseudotumor cerebri), bronchospasm and/or apnea in patients with severe respiratory failure, especially in patients bronchial asthma. Several cases of acute respiratory distress, mostly associated with interstitial pneumonitis, have been observed.

Local reactions: phlebitis (can be avoided by using central venous catheter).

For oral administration

From the outside of cardio-vascular system: bradycardia (mostly moderate and dose-dependent); in some cases (with sinus node dysfunction, in the elderly) - severe bradycardia; in exceptional cases - sinus block; rarely - conduction disturbances (sinoatrial block, AV block various degrees, intraventricular block); in some cases - the emergence of new arrhythmias or aggravation of existing ones, in some cases - with subsequent cardiac arrest (according to available data, it is impossible to establish a connection with the use of the drug, with the severity of heart damage or with the ineffectiveness of treatment). These effects are observed mainly in cases of combined use of Cordarone with drugs that prolong the period of repolarization of the ventricles of the heart (QTc interval) or in cases of disorders electrolyte balance.

On the part of the organ of vision: microdeposits of lipofuscin in the cornea of the eye (almost always present) are usually limited to the pupil area, are reversible after discontinuation of the drug, sometimes lead to visual impairment in the form of the appearance of a colored halo in bright light or a feeling of fog; in some cases - neuropathy/optic neuritis (the connection with amiodarone has not been clearly established to date).

Dermatological reactions: photosensitivity; erythema (during radiotherapy); in some cases - rash (usually nonspecific), exfoliative dermatitis(the connection with taking the drug has not been formally established); with prolonged use in high doses- grayish or bluish pigmentation of the skin (slowly disappears after stopping treatment).

From the outside endocrine system: increase in serum T3 level (T4 remains normal or slightly reduced) in such cases in the absence clinical signs thyroid dysfunction does not require discontinuation of the drug); hypothyroidism may develop (mild weight gain, decreased activity, more pronounced /compared to expected/ bradycardia); hyperthyroidism (both during therapy and for several months after stopping the drug). Suspicion of hyperthyroidism may arise from the following mild clinical symptoms: weight loss, development of arrhythmia, angina pectoris, heart failure. The diagnosis is confirmed by a clear decrease in serum TSH. Amiodarone should be discontinued.

From the outside digestive system: nausea, vomiting, taste disturbances (usually found at the beginning of therapy when used in loading doses and decrease when the dose is reduced); at the beginning of treatment - an isolated increase (1.5-3 times higher than ULN) in the activity of liver transaminases (they decrease with a decrease in the dose of the drug or even spontaneously); in some cases - acute disorders liver function and/or jaundice (require discontinuation of the drug), fatty hepatosis, cirrhosis. Clinical symptoms And laboratory changes may be minimal (hepatomegaly is possible, increased activity of liver transaminases is increased up to 1.5-5 times compared to ULN); Therefore, regular monitoring of liver function is recommended during treatment.

From the respiratory system: in some cases - pneumonitis, fibrosis, pleurisy, bronchiolitis obliterans with pneumonia (sometimes resulting in death), bronchospasm in patients with severe respiratory diseases(especially with bronchial asthma), acute respiratory distress syndrome in adults.

From the central nervous system and peripheral nervous system: rarely - sensorimotor peripheral neuropathies and / or myopathies (usually reversible after discontinuation of the drug), extrapyramidal tremor, cerebellar ataxia; in rare cases - benign intracranial hypertension, nightmares.

Allergic reactions: rarely - vasculitis, kidney damage with increased creatinine levels, thrombocytopenia; in some cases - hemolytic anemia, aplastic anemia.

Other: alopecia; in some cases - epididymitis, impotence (the connection with the use of the drug has not been established).

CONTRAINDICATIONS

For oral administration

SSSU (sinus bradycardia, sinoatrial blockade) except for cases of correction by an artificial pacemaker;

Violations of AV and intraventricular conduction (AV blockade II and III degree, blockade of the legs of the bundle of His) in the absence of an artificial pacemaker (pacemaker);

Thyroid dysfunction (hypothyroidism, hyperthyroidism);

Hypokalemia;

Heart failure (in the stage of decompensation);

Concomitant use of MAO inhibitors;

Interstitial lung diseases;

Pregnancy;

Lactation;

For solution for intravenous administration

SSSU (sinus bradycardia, sinoatrial blockade) with the exception of patients with an artificial pacemaker (danger of stopping the sinus node);

AV block II and III degree, violations of intraventricular conduction (blockade of two and three legs of the bundle of His); in these cases, intravenous amiodarone can be used in specialized departments under the cover of an artificial pacemaker (pacemaker);

Acute cardiovascular failure(shock, collapse);

Severe arterial hypotension;

Simultaneous use with drugs that can cause polymorphic ventricular tachycardia of the "pirouette" type;

Thyroid dysfunction (hypothyroidism, hyperthyroidism);

Pregnancy;

Lactation;

Age up to 18 years (efficacy and safety have not been established);

Hypersensitivity to iodine and/or amiodarone.

IV administration is contraindicated in severe violations lung function (interstitial lung disease), cardiomyopathy or decompensated heart failure (the patient's condition may worsen).

Use with caution in chronic heart failure, liver failure, bronchial asthma, in old age (due to the high risk of developing severe bradycardia).

PREGNANCY AND LACTATION

During pregnancy, Cordarone is prescribed only for health reasons, because the drug has an effect on the fetal thyroid gland.

Amiodarone is released from breast milk V significant quantities, therefore the drug is contraindicated for use during lactation.

SPECIAL INSTRUCTIONS

Before starting and during treatment, it is recommended to conduct an ECG study. Due to the prolongation of the period of repolarization of the ventricles of the heart, pharmachologic effect Cordarone causes certain ECG changes: prolongation of the QT interval, QTc, possible appearance of U waves. An increase in the QTc interval by no more than 450 ms or by no more than 25% of the original value is acceptable. These changes are not a manifestation of the toxic effect of the drug, but require monitoring to adjust the dose and assess the possible proarrhythmogenic effect of Cordarone.

It should be taken into account that in elderly patients there is a more pronounced decrease in heart rate.

If second or third degree AV block, sinoatrial or bifascicular block develops, treatment with Cordarone should be discontinued.

The appearance of shortness of breath or nonproductive cough may be related to toxic effect Cordarone for the lungs. In patients with increasing shortness of breath with physical activity, regardless of their deterioration general condition(increased fatigue, weight loss, increased body temperature), an x-ray should be taken before starting therapy chest. Respiratory problems are mostly reversible with early discontinuation of amiodarone. Clinical symptoms usually resolve within 3-4 weeks, followed by a slower recovery X-ray picture and lung function (several months). Therefore, the possibility of re-evaluating amiodarone therapy and prescribing corticosteroids should be considered.

If blurred vision or decreased visual acuity occurs while taking Cordarone, it is recommended to conduct a full ophthalmological examination, including fundoscopy. Cases optic neuropathy and/or optic neuritis require a decision on the advisability of using Cordarone.

Cordarone contains iodine (200 mg contains 75 mg iodine), so may interfere with accumulation test results radioactive iodine V thyroid gland, but does not affect the reliability of the determination of T3, T4 and TSH. Amiodarone may cause thyroid dysfunction, especially in patients with a history of thyroid dysfunction (including a family history). Therefore, before starting treatment, during treatment and several months after the end of treatment, careful clinical and laboratory monitoring should be carried out. If thyroid dysfunction is suspected, serum TSH levels should be measured. When signs of hypothyroidism appear, normalization of thyroid function is usually observed within 1-3 months after cessation of treatment. In life-threatening situations, treatment with amiodarone can be continued, with simultaneous additional administration of levothyroxine. Serum TSH levels serve as a guide for levothyroxine dosage. If signs of hyperthyroidism appear, amiodarone should be discontinued. Normalization of thyroid function usually occurs within several months after discontinuation of the drug. Wherein clinical symptoms normalizes before normalization of the level of hormones that reflect the function of the thyroid gland occurs. In severe cases, immediate medical intervention is required. Treatment in each individual case is selected individually and includes antithyroid drugs (which may not always be effective), corticosteroids, and beta-blockers.

Cordarone for intravenous administration is used only in a specialized hospital department under constant monitoring of ECG and blood pressure. In this case, Cordarone should be administered by infusion rather than by injection due to the risk of hemodynamic disturbances (hypotension, acute cardiovascular failure).

IV injections of Cordarone should be carried out only in emergency situations when there are no other therapeutic options and only in cardiac intensive care units with continuous ECG monitoring.

When administering Cordarone by injection, a dose of approximately 5 mg/kg should be administered over at least 3 minutes. The injection should not be repeated earlier than 15 minutes after the first injection, even if the last one consisted of only one ampoule (irreversible collapse is possible).

Particular caution is required when infusing the drug in cases of arterial hypotension, severe respiratory failure, decompensated cardiomyopathy or severe heart failure.

Patients should avoid prolonged exposure to the sun and UV radiation (or use sunscreen).

Impact on the ability to drive vehicles and operate machinery

Currently, there is no evidence that Cordarone affects the ability to drive vehicles and operate machinery.

OVERDOSE

Symptoms: sinus bradycardia, cardiac arrest, ventricular tachycardia, paroxysmal ventricular tachyarrhythmias of the “pirouette” type, circulatory disorders, liver dysfunction, decreased blood pressure.

Treatment: carried out symptomatic therapy(gastric lavage, administration of cholestyramine, for bradycardia - beta-adrenergic stimulants or installation of a pacemaker, for tachycardia of the “pirouette” type - intravenous administration of magnesium salts, reducing cardiac pacing). Amiodarone and its metabolites are not removed by dialysis.

There is no information about overdose with intravenous administration of Cordarone.

DRUG INTERACTIONS

At simultaneous reception Cordarone with antiarrhythmic drugs (including bepridil, class I A drugs, sotalol), as well as with vincamine, sultopride, erythromycin for intravenous administration, pentamidine for parenteral administration the risk of developing polymorphic paroxysmal disease increases ventricular tachycardia"pirouette" type. Therefore, these combinations are contraindicated.

Not recommended combination therapy with beta-blockers, some calcium channel blockers (verapamil, diltiazem), because Automaticity disorders (manifested by bradycardia) and conduction may develop.

It is not recommended to use Cordarone simultaneously with laxatives (stimulating intestinal motility), which can cause hypokalemia, because the risk of developing ventricular tachycardia of the “pirouette” type increases.

Cordarone should be used with caution simultaneously with drugs that cause hypokalemia (diuretics, systemic GCS and mineralocorticoids, tetracosactide, amphotericin B /for intravenous administration/), because the development of ventricular tachycardia of the “pirouette” type is possible.

At simultaneous use Cordarone with anticoagulants for oral administration increases the risk of bleeding (therefore it is necessary to monitor the level of prothrombin and adjust the dose of anticoagulants).

With the simultaneous use of Cordarone with cardiac glycosides, disturbances in automaticity (manifested by severe bradycardia) and disturbances in atrioventricular conduction may be observed. In addition, it is possible to increase the concentration of digoxin in the blood plasma due to a decrease in its clearance (therefore, it is necessary to monitor the concentration of digoxin in the blood plasma, conduct an ECG and laboratory monitoring, and, if necessary, change the dosage regimen of cardiac glycosides).

With the simultaneous use of Cordarone with phenytoin, cyclosporine, flecainide, it is possible to increase the concentration of the latter in the blood plasma (therefore, the concentration of phenytoin, cyclosporine, flecainide in the blood plasma should be monitored and their dose adjusted if necessary).

Cases of bradycardia (resistant to atropine), arterial hypotension, conduction disturbances, and decreased cardiac output have been described in patients taking Cordarone and exposed to general anesthesia.

When using oxygen therapy in postoperative period in patients treated with Cordarone, rare cases development of severe respiratory complications, sometimes resulting in death (acute adult respiratory distress syndrome).

At joint use with simvastatin, it is possible to increase the risk of side effects (primarily rhabdomyolysis) due to impaired metabolism of simvastatin (if it is necessary to use such a combination, the dose of simvastatin should not exceed 20 mg/day; if the therapeutic effect is not achieved at this dose, you should switch to taking another lipid-lowering drug) .

CONDITIONS OF DISCHARGE FROM PHARMACIES The drug is dispensed with a prescription. The drug in the form of a solution for intravenous administration is intended for use only in a hospital setting.

TERMS AND CONDITIONS OF STORAGE

The drug in tablet form should be stored at room temperature (not higher than 30°C). The shelf life of the tablets is 3 years. The drug in the form of a solution for intravenous administration should be stored in a dry place at a temperature not exceeding 25°C. The shelf life of the solution for intravenous administration is 2 years.

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Cordaron

Cordarone is an antiarrhythmic drug that can be used to eliminate any arrhythmias. Cordarone is also used as a remedy emergency assistance for life-threatening arrhythmias, and as ongoing maintenance treatment.

My review will be devoted to Cordarone, a drug for the treatment of arrhythmias. This is a drug for long-term treatment, and for “first aid”, and for prevention... In any case, it is really very, very strong medicine. Therefore, I’ll probably break “traditions” a little pharmacological reviews, talking about Cordaron. But I hope that this is forgivable, at least due to what I will describe here important drug, and, moreover, the drug is interesting!

Cordarone is a unique remedy of its kind. Due to the fact that it combines the properties of antiarrhythmics of all classes (that is, it has a multifaceted and complex effect), it can be used to treat absolutely any type of arrhythmias. As a rule, if other medications do not work, Cordarone will definitely help.

In addition, Cordarone dilates coronary vessels and reduces blood pressure. These are not its main effects (the main one is antiarrhythmic), but they are also quite pronounced.

At its core, Cordarone is an “analogue” of thyroid hormones. It blocks the activation of thyroxine, and this effect is often a problem in long-term treatment. In most cases, Cordarone is not prescribed as a drug for continuous use, so its benefits, even against the background of this feature, outweigh the harm from it.

It turned out a little differently for me: I took a variety of antiarrhythmics, but the effect of the treatment was still not satisfactory. For almost two years I consistently drank half a tablet of Etatsizin a day, and felt quite good. When even Etatsizin stopped working, my doctor had to prescribe me Cordarone (daily!), since it was guaranteed to eliminate the arrhythmia.

After 8 months of taking it, I began to experience all the symptoms of hypothyroidism: my weight began to steadily increase, terrible weakness appeared, constant drowsiness. It became difficult for me to do any business - I immediately felt tired. TSH in tests increased several times (last time it was almost 16.5, instead of 3-4!). All this was also aggravated by the fact that about ten years ago I had a lobe of my thyroid gland removed.

In addition to hypothyroidism, I experienced other side effects:

blurred vision;
bradycardia;
sleep disturbance;
change in skin color - it has become bluish;
tremor;
photosensitivity - being in the sun can sometimes be downright painful.

My doctor warned me about these consequences. In addition, he mentioned other common adverse reactions to taking Cordarone:

nausea and vomiting;
change taste sensations;
decreased appetite;
heaviness and pain in the abdomen;
emergence acute hepatitis;
pneumonia, pulmonary fibrosis.

Separately, it is worth mentioning how Cordarone is combined with other drugs. Surely, a whole book could be written about this, but, fortunately, I don’t have much experience in this. I had to stop taking Nebivolol because it... joint reception With these medications, the pulse constantly dropped to 50-55/minute, which is not enough for me. Now I don't take anything for treatment at all arterial hypertension, pressure up to normal level reduces Cordarone.

Another drug is Plavix. I do not have a diagnosis of coronary heart disease (and even atherosclerosis, supposedly), but the blood is “thick”, and Plavix was needed as a preventive measure. I didn’t stop taking it, but I had to reduce the dose: in combination with Cordarone, all the side effects of Plavix and similar drugs appear much more often.

Interesting property Cordarone: indications for the use of tablets and injections are different.

Tablet forms are indicated for the treatment of any types of arrhythmias and their prevention:

atrial fibrillation and flutter;
sudden “arrhythmic death”;
paroxysmal tachycardias;
atrial fibrillation.

Injections (droppers) with Cordarone are used as an “ambulance” if cardiac resuscitation is necessary, for example, to eliminate ventricular fibrillation (this condition can lead to death in 40-50 seconds!).

There are no contraindications for drugs such as Cordarone. If a medicine is used “for life-saving indications”, that is, in the absence of treatment the patient may die, only the relationship between the benefits and harms of the drug is considered.

Nevertheless, here are the conditions in which Cordarone is prescribed especially carefully:

thyroid diseases are the most important condition;
sick sinus syndrome;
inadequate response organism for iodine;
severe forms intracardiac blockades;
deficiency of potassium and magnesium;
pregnancy.

As I already indicated, these are NOT contraindications. Cordarone can be used in these conditions, but only if it is a matter of preserving the patient’s life.

This is the review of Cordaron that I wanted to present to you. Many people encounter this drug, and most of the information about it is difficult to understand. I analyzed everything that my attending physician told me: this resulted in this review.

Thank you for your attention, and may arrhythmias bypass you. Do not be ill!

otzivilekarstv.ru

Cordarone - use and contraindications

The drug Cordarone, with all its indications and contraindications for use, belongs to the group of third class antiarrhythmic drugs. That is, its action is based on the blockade of potassium channels. The medicine also has the properties of antiarrhythmics of the first and fourth classes. And accordingly, it can simultaneously block sodium and calcium channels. Among other things, the drug has beta-adrenergic blocking, antianginal and coronary dilatatory effects.

Indications for use of Cordarone tablets

The drug is based on amiodarone hydrochloride. Standard dosage active substance– 200 mg. In addition to this, the drug contains the following: auxiliary components:

anhydrous colloidal silica;
lactose monohydrate;
magnesium stearate;
corn starch;
povidone.

The drug Cordarone is indicated for use both for treatment and for preventive purposes. It is usually prescribed for:

supraventricular paroxysmal tachycardias;
ventricular arrhythmias;
Wolff-Parkinson-White syndrome;
supraventricular and ventricular extrasystole;
atrial flutter;
sinus tachycardia;
recovery after myocardial infarction;
acute phase myocardial infarction;
atrial fibrillation;
ventricular dysfunction;
coronary heart disease;
attacks of angina.

How exactly to use Cordarone tablets is determined by your attending physician. Can be used in therapy different schemes. For example, in a hospital setting, the optimal initial dose is 600-800 mg of amiodarone hydrochloride, divided into several doses. The maximum permissible total daily dose is 10 g. And such treatment lasts from five to eight days.

Scheme outpatient treatment similar, but it should last a little longer - from ten days to two weeks. It is important to remember that the half-life of Cordarone is rather long, so it is recommended to use it every other day. You can also take tablets with short breaks - up to a couple of days.

Contraindications to the use of Cordarone

Almost any medication has contraindications. And Cordaron was no exception. It is not recommended to be treated with this antiarrhythmic if:

hypersensitivity to the components of the composition;
prolongation of the QT interval (both congenital and acquired);
sinus bradycardia;
sinoatrial block;
pregnancy;
breastfeeding;
interstitial lung disease;
hypokalemia;
hypomagnesemia;
thyroid dysfunction (such as hyper- or hypothyroidism);
atrioventricular block from the first to the third degree.

Children under eighteen should not take the pills. Patients with:

arterial hypotension;
decompensated or severe chronic heart failure;
cardiogenic shock;
bronchial asthma;
cardiomyopathy;
liver failure.

Elderly patients whose bodies are weakened should also take the medicine under the supervision of a specialist. age-related changes and exposed to risks.

It is very undesirable to combine Cordarone with the following medications:

Quinidine;
Mefeloquine;
Quinine;
Pimozide;
Fluphenazine;
Spiramycin;
Mizolastine;
Sultopride;
Terfenadine;
Haloperidol;
Bretylia;
Sotalol;
Spiramycin;
Chlorpromazine;
Cyamemazine.

Articles

Cordarone is an antiarrhythmic drug that can be used to eliminate any arrhythmias. Cordarone is used both as an emergency treatment for life-threatening arrhythmias and as ongoing maintenance treatment.

My review will be devoted to Cordarone, a drug for the treatment of arrhythmias. This is a drug for long-term treatment, and for “first aid”, and for prevention... In any case, this is really a very, very strong medicine. Therefore, I’ll probably break the “traditions” of pharmacological reviews a little by talking about Cordarone. But I hope that this is forgivable, if only because I will describe here an important drug, and, moreover, an interesting drug!

In addition, Cordarone dilates coronary vessels and reduces blood pressure. These are not its main effects (the main one is antiarrhythmic), but they are also quite pronounced.

At its core, Cordarone is an “analogue” of thyroid hormones. It blocks the activation of thyroxine, and this effect is often a problem with long-term treatment. In most cases, Cordarone is not prescribed as a drug for continuous use, so its benefits, even against the background of this feature, outweigh the harm from it.

After 8 months of taking it, I began to experience all the symptoms of hypothyroidism: my weight began to steadily increase, terrible weakness and constant drowsiness appeared. It became difficult for me to do any business - I immediately felt tired. TSH in tests increased several times (last time it was almost 16.5, instead of 3-4!). All this was also aggravated by the fact that about ten years ago I had a lobe of my thyroid gland removed.

In addition to hypothyroidism, I experienced other side effects:

blurred vision;
bradycardia;
sleep disturbance;
change in skin color - it has become bluish;
tremor;
photosensitivity - being in the sun can sometimes be downright painful.

My doctor warned me about these consequences. In addition, he mentioned other common adverse reactions to taking Cordarone:

nausea and vomiting;
change in taste sensations;
decreased appetite;
heaviness and pain in the abdomen;
the occurrence of acute hepatitis;
pneumonia, pulmonary fibrosis.

Separately, it is worth mentioning how Cordarone is combined with other drugs. Surely, a whole book could be written about this, but, fortunately, I don’t have much experience in this. I had to stop taking Nebivolol, because taking these drugs together, the pulse constantly dropped to 50-55/minute, which is not enough for me. Now I don’t take anything at all to treat arterial hypertension; Cordarone lowers my blood pressure to normal levels.

An interesting property of Cordarone: the indications for the use of tablets and injections are different.

Tablet forms are indicated for the treatment of any types of arrhythmias and their prevention:

atrial fibrillation and flutter;
sudden “arrhythmic death”;
paroxysmal tachycardias;
atrial fibrillation.

Nevertheless, here are the conditions in which Cordarone is prescribed especially carefully:

thyroid disease is the most important condition;
sick sinus syndrome;
inadequate response of the body to iodine;
severe forms of intracardiac blockade;
deficiency of potassium and magnesium;
pregnancy.

As I already indicated, these are NOT contraindications. Cordarone can be used in these conditions, but only if it is a matter of preserving the patient’s life.

Thank you for your attention, and may arrhythmias bypass you. Do not be ill!

otzivilekarstv.ru

CORDARON

DOSAGE FORM, COMPOSITION AND PACKAGING

1 tab. amiodarone hydrochloride 200 mg

Excipients: lactose monohydrate, corn starch, polyvidone K90F, colloidal anhydrous silicon dioxide, magnesium stearate.

10 pieces. - blisters (3) - packs of cardboard.

PHARMACHOLOGIC EFFECT

Class III antiarrhythmic drug. Has antiarrhythmic and antianginal effects.

The antianginal effect of Cordarone is due to a decrease in oxygen consumption by the myocardium (due to a decrease in heart rate and a decrease in peripheral resistance), non-competitive blockade of α- and β-adrenergic receptors, an increase in coronary blood flow through a direct effect on the smooth muscles of the arteries, maintaining cardiac output by reducing pressure in the aorta and reducing peripheral resistance .

Cordarone does not have a significant negative inotropic effect and reduces myocardial contractility mainly after intravenous administration.

Therapeutic effects are observed 1 week (from several days to 2 weeks) after starting to take the drug orally.

PHARMACOKINETICS

Suction

Distribution

Amiodarone has a large Vd. Amiodarone accumulates most in adipose tissue, liver, lungs, spleen and cornea. After a few days, amiodarone is eliminated from the body. Css is achieved within 1 to several months, depending on the individual characteristics of the patient. Binding to blood plasma proteins is 95% (62% to albumin, 33.5% to beta-lipoproteins).

Metabolism

breeding

Elimination when taken orally occurs in 2 phases: T1/2 in the α-phase - 4-21 hours, T1/2 in the β-phase - 25-110 days. After prolonged oral administration, the average T1/2 is 40 days (this is important when choosing a dose, since at least 1 month is required to stabilize the plasma concentration, and complete elimination can last more than 4 months).

Pharmacokinetics in special clinical situations

Insignificant excretion of the drug in the urine allows the drug to be prescribed in moderate doses for renal failure. Amiodarone and its metabolites are not dialyzable.

INDICATIONS

Relief of attacks of ventricular paroxysmal tachycardia;

Relief of attacks of supraventricular paroxysmal tachycardia with a high frequency of ventricular contractions (especially against the background of WPW syndrome);

Relief of paroxysmal and persistent forms of atrial fibrillation (atrial fibrillation) and atrial flutter.

Relapse Prevention

Life-threatening ventricular arrhythmias and ventricular fibrillation (treatment should be started in a hospital with careful cardiac monitoring);

Supraventricular paroxysmal tachycardias, incl. documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with organic heart diseases; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients without organic heart disease, when antiarrhythmic drugs of other classes are not effective or there are contraindications to their use; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with WPW syndrome;

Atrial fibrillation (atrial fibrillation) and atrial flutter.

Prevention of sudden arrhythmic death in high-risk patients after a recent myocardial infarction, with more than 10 ventricular extrasystoles per hour, clinical manifestations of chronic heart failure and reduced left ventricular ejection fraction (Cordarone is especially recommended for patients with organic heart disease (including . with ischemic heart disease), accompanied by left ventricular dysfunction.

DOSING REGIME

For oral administration

For outpatient use, the initial dose, divided into several doses, ranges from 600 mg to 800 mg / day (usually for 10-14 days).

For solution for intravenous administration

The loading dose of Cordarone is initially 5-7 mg/kg body weight in 250 ml of a 5% dextrose (glucose) solution for 30-60 minutes. The therapeutic effect of Cordarone appears during the first minutes of administration and disappears gradually, which requires adjustment of the rate of its administration in accordance with the results of treatment.

When conducting intravenous injections, the drug at a dose of 5 mg / kg is administered for at least 3 minutes. Cordarone cannot be taken into the same syringe with other medications!

For intravenous infusion, concentrations below 600 mg/l should not be used. For the preparation of solutions for intravenous administration, use only 5% dextrose (glucose) solution.

SIDE EFFECT

Solution for intravenous administration

Systemic reactions: feeling of heat, increased sweating, decreased blood pressure (usually moderate and transient); cases of severe arterial hypotension or collapse (have been reported with overdose or too rapid administration), moderate bradycardia (in some cases, especially in elderly patients, severe bradycardia and, in exceptional cases, sinus node arrest, requiring discontinuation of therapy); rarely - proarrhythmic effect. At the beginning of therapy, there is an increase in the activity of hepatic transaminases in the blood serum, which usually remains moderate (1.5-3 times higher than the upper limit of normal (ULN)) and, as a rule, normalizes when the dose is reduced or even spontaneously. If transaminase levels increase significantly, treatment should be discontinued. There are isolated case reports of acute liver failure with high serum levels of liver transaminases and/or jaundice (some with fatal outcome). In isolated (exceptionally rare) cases, anaphylactic shock, benign intracranial hypertension (pseudotumor of the brain), bronchospasm and/or apnea were observed in patients with severe respiratory failure, especially in patients with bronchial asthma. Several cases of acute respiratory distress, mostly associated with interstitial pneumonitis, have been observed.

Local reactions: phlebitis (can be avoided by using a central venous catheter).

For oral administration

From the cardiovascular system: bradycardia (mostly moderate and dose-dependent); in some cases (with sinus node dysfunction, in the elderly) - severe bradycardia; in exceptional cases - sinus block; rarely - conduction disorders (sinoatrial block, AV block of various degrees, intraventricular block); in some cases - the emergence of new arrhythmias or aggravation of existing ones, in some cases - with subsequent cardiac arrest (according to available data, it is impossible to establish a connection with the use of the drug, with the severity of heart damage or with the ineffectiveness of treatment). These effects are observed mainly in cases of combined use of Cordarone with drugs that prolong the period of repolarization of the ventricles of the heart (QTc interval) or in case of electrolyte imbalance.

Dermatological reactions: photosensitivity; erythema (during radiotherapy); in some cases - rash (usually nonspecific), exfoliative dermatitis (the connection with taking the drug has not been formally established); with prolonged use in high doses - grayish or bluish pigmentation of the skin (slowly disappears after stopping treatment).

From the endocrine system: an increase in the level of T3 in the blood serum (T4 remains normal or slightly reduced) in such cases, in the absence of clinical signs of thyroid dysfunction, discontinuation of the drug is not required); possible development of hypothyroidism (mild weight gain, decreased activity, more pronounced (compared to expected) bradycardia); hyperthyroidism (both during therapy and for several months after stopping the drug). Suspicion of hyperthyroidism may arise from the following mild clinical symptoms: weight loss, development of arrhythmia, angina pectoris, heart failure. The diagnosis is confirmed by a clear decrease in serum TSH. Amiodarone should be discontinued.

From the digestive system: nausea, vomiting, taste disturbances (usually found at the beginning of therapy when used in loading doses and decrease when the dose is reduced); at the beginning of treatment - an isolated increase (1.5-3 times higher than ULN) in the activity of liver transaminases (they decrease with a decrease in the dose of the drug or even spontaneously); in some cases - acute liver dysfunction and/or jaundice (require discontinuation of the drug), fatty hepatosis, cirrhosis. Clinical symptoms and laboratory changes may be minimal (hepatomegaly is possible, increased activity of liver transaminases is increased to 1.5-5 times compared to ULN); Therefore, regular monitoring of liver function is recommended during treatment.

From the respiratory system: in some cases - pneumonitis, fibrosis, pleurisy, bronchiolitis obliterans with pneumonia (sometimes resulting in death), bronchospasm in patients with severe respiratory diseases (especially bronchial asthma), acute respiratory distress syndrome in adults.

From the central nervous system and peripheral nervous system: rarely - sensorimotor peripheral neuropathies and/or myopathies (usually reversible after discontinuation of the drug), extrapyramidal tremor, cerebellar ataxia; in rare cases - benign intracranial hypertension, nightmares.

Allergic reactions: rarely - vasculitis, kidney damage with increased creatinine levels, thrombocytopenia; in some cases - hemolytic anemia, aplastic anemia.

Other: alopecia; in some cases - epididymitis, impotence (the connection with the use of the drug has not been established).

CONTRAINDICATIONS

For oral administration

SSSU (sinus bradycardia, sinoatrial blockade) except for cases of correction by an artificial pacemaker;

Violations of AV and intraventricular conduction (AV blockade II and III degree, blockade of the legs of the bundle of His) in the absence of an artificial pacemaker (pacemaker);

Thyroid dysfunction (hypothyroidism, hyperthyroidism);

Hypokalemia;

Heart failure (in the stage of decompensation);

Concomitant use of MAO inhibitors;

Interstitial lung diseases;

Pregnancy;

Lactation;

For solution for intravenous administration

SSSU (sinus bradycardia, sinoatrial blockade) with the exception of patients with an artificial pacemaker (danger of stopping the sinus node);

Acute cardiovascular failure (shock, collapse);

Severe arterial hypotension;

Simultaneous use with drugs that can cause polymorphic ventricular tachycardia of the "pirouette" type;

Thyroid dysfunction (hypothyroidism, hyperthyroidism);

Pregnancy;

Lactation;

Age up to 18 years (efficacy and safety have not been established);

Hypersensitivity to iodine and/or amiodarone.

IV administration is contraindicated in severe pulmonary dysfunction (interstitial lung disease), cardiomyopathy or decompensated heart failure (possible deterioration of the patient's condition).

Use with caution in chronic heart failure, liver failure, bronchial asthma, in old age (due to the high risk of developing severe bradycardia).

PREGNANCY AND LACTATION

During pregnancy, Cordarone is prescribed only for health reasons, because the drug has an effect on the fetal thyroid gland.

Amiodarone is excreted in breast milk in significant quantities, so the drug is contraindicated for use during lactation.

SPECIAL INSTRUCTIONS

Before starting and during treatment, it is recommended to conduct an ECG study. Due to the prolongation of the period of repolarization of the ventricles of the heart, the pharmacological action of Cordarone causes certain changes in the ECG: prolongation of the QT interval, QTc, the appearance of U waves is possible. An increase in the QTc interval is permissible by no more than 450 ms or by no more than 25% of the original value. These changes are not a manifestation of the toxic effect of the drug, but require monitoring to adjust the dose and assess the possible proarrhythmogenic effect of Cordarone.

It should be taken into account that in elderly patients there is a more pronounced decrease in heart rate.

If second or third degree AV block, sinoatrial or bifascicular block develops, treatment with Cordarone should be discontinued.

The appearance of shortness of breath or nonproductive cough may be associated with the toxic effect of Cordarone on the lungs. In patients with increasing shortness of breath during exercise, regardless of the deterioration of their general condition (increased fatigue, weight loss, increased body temperature), a chest x-ray should be performed before starting therapy. Respiratory problems are mostly reversible with early discontinuation of amiodarone. Clinical symptoms usually resolve within 3-4 weeks, followed by a slower recovery of radiographic appearance and pulmonary function (several months). Therefore, the possibility of re-evaluating amiodarone therapy and prescribing corticosteroids should be considered.

If blurred vision or decreased visual acuity occurs while taking Cordarone, it is recommended to conduct a full ophthalmological examination, including fundoscopy. Cases of optic neuropathy and/or optic neuritis require a decision on the advisability of using Cordarone.

Cordarone contains iodine (200 mg contains 75 mg of iodine), so it may affect the results of tests for the accumulation of radioactive iodine in the thyroid gland, but does not affect the reliability of the determination of T3, T4 and TSH. Amiodarone may cause thyroid dysfunction, especially in patients with a history of thyroid dysfunction (including a family history). Therefore, before starting treatment, during treatment and several months after the end of treatment, careful clinical and laboratory monitoring should be carried out. If thyroid dysfunction is suspected, serum TSH levels should be measured. When signs of hypothyroidism appear, normalization of thyroid function is usually observed within 1-3 months after cessation of treatment. In life-threatening situations, treatment with amiodarone can be continued, with simultaneous additional administration of levothyroxine. Serum TSH levels serve as a guide for levothyroxine dosage. If signs of hyperthyroidism appear, amiodarone should be discontinued. Normalization of thyroid function usually occurs within several months after discontinuation of the drug. In this case, clinical symptoms normalize before normalization of the level of hormones that reflect the function of the thyroid gland occurs. In severe cases, immediate medical intervention is required. Treatment in each individual case is selected individually and includes antithyroid drugs (which may not always be effective), corticosteroids, and beta-blockers.

IV injections of Cordarone should be performed only in emergency situations, when there are no other therapeutic options, and only in cardiac intensive care units with continuous ECG monitoring.

Particular caution is required when infusing the drug in cases of arterial hypotension, severe respiratory failure, decompensated cardiomyopathy or severe heart failure.

Patients should avoid prolonged exposure to the sun and UV radiation (or use sunscreen).

Impact on the ability to drive vehicles and operate machinery

Currently, there is no evidence that Cordarone affects the ability to drive vehicles and operate machinery.

OVERDOSE

Treatment: symptomatic therapy is carried out (gastric lavage, administration of cholestyramine, for bradycardia - beta-adrenergic stimulants or installation of a pacemaker, for tachycardia of the “pirouette” type - intravenous administration of magnesium salts, reducing pacemaker). Amiodarone and its metabolites are not removed by dialysis.

There is no information about overdose with intravenous administration of Cordarone.

DRUG INTERACTIONS

When taking Cordarone simultaneously with antiarrhythmic drugs (including bepridil, class I A drugs, sotalol), as well as with vincamine, sultopride, erythromycin for intravenous administration, pentamidine for parenteral administration, the risk of developing polymorphic paroxysmal ventricular tachycardia of the “pirouette” type increases. Therefore, these combinations are contraindicated.

Combination therapy with beta-blockers, some calcium channel blockers (verapamil, diltiazem) is not recommended. Automaticity disorders (manifested by bradycardia) and conduction may develop.

With caution, Kordaron should be used simultaneously with drugs that cause hypokalemia (diuretics, systemic corticosteroids and mineralocorticoids, tetracosactide, amphotericin B / for intravenous administration /), because the development of ventricular tachycardia of the “pirouette” type is possible.

With the simultaneous use of Kordaron with oral anticoagulants, the risk of bleeding increases (therefore, it is necessary to control the level of prothrombin and adjust the dose of anticoagulants).

Cases of bradycardia (resistant to atropine), arterial hypotension, conduction disturbances, and a decrease in cardiac output in patients taking Kordaron and undergoing general anesthesia are described.

When using oxygen therapy in the postoperative period in patients treated with Kordaron, rare cases of the development of severe respiratory complications, sometimes ending in death (acute respiratory distress syndrome in adults), are described.

When used together with simvastatin, it is possible to increase the risk of side effects (primarily rhabdomyolysis) due to impaired metabolism of simvastatin (if such a combination is necessary, the dose of simvastatin should not exceed 20 mg / day, if the therapeutic effect is not achieved at this dose, you should switch to taking another lipid-lowering drug).

CONDITIONS OF DISCHARGE FROM PHARMACIES The drug is dispensed with a prescription. The drug in the form of a solution for intravenous administration is intended for use only in a hospital setting.

TERMS AND CONDITIONS OF STORAGE

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Cordarone - use and contraindications

Indications for use of Cordarone tablets

The drug is based on amiodarone hydrochloride. The standard dosage of the active substance is 200 mg. In addition to this, the drug contains the following auxiliary components:

anhydrous colloidal silica;
lactose monohydrate;
magnesium stearate;
corn starch;
povidone.

The drug Cordarone is indicated for use both for treatment and for preventive purposes. It is usually prescribed for:

supraventricular paroxysmal tachycardias;
ventricular arrhythmias;
Wolff-Parkinson-White syndrome;
supraventricular and ventricular extrasystole;
atrial flutter;
sinus tachycardia;
recovery after myocardial infarction;
acute phase of myocardial infarction;
atrial fibrillation;
ventricular dysfunction;
coronary heart disease;
attacks of angina.

How exactly to use Cordarone tablets is determined by your attending physician. Different regimens can be used in therapy. For example, in a hospital setting, the optimal initial dose is 600-800 mg of amiodarone hydrochloride, divided into several doses. The maximum permissible total daily dose is 10 g. And such treatment lasts from five to eight days.

The scheme of outpatient treatment is similar, but it should last a little longer - from ten days to two weeks. It is important to remember that the half-life of Cordarone is rather long, so it is recommended to use it every other day. You can also take tablets with short breaks - up to a couple of days.

Contraindications to the use of Cordarone

Almost any medication has contraindications. And Cordaron was no exception. It is not recommended to be treated with this antiarrhythmic if:

hypersensitivity to the components of the composition;
prolongation of the QT interval (both congenital and acquired);
sinus bradycardia;
sinoatrial block;
pregnancy;
breastfeeding;
interstitial lung disease;
hypokalemia;
hypomagnesemia;
thyroid dysfunction (such as hyper- or hypothyroidism);
atrioventricular block from the first to the third degree.

Children under eighteen should not take the pills. Patients with:

arterial hypotension;
decompensated or severe chronic heart failure;
cardiogenic shock;
bronchial asthma;
cardiomyopathy;
liver failure.

Elderly patients whose bodies are weakened by age-related changes and are at risk should also take the medicine under the supervision of a specialist.

It is very undesirable to combine Cordarone with the following medications:

Quinidine;
Mefeloquine;
Quinine;
Pimozide;
Fluphenazine;
Spiramycin;
Mizolastine;
Sultopride;
Terfenadine;
Haloperidol;
Bretylia;
Sotalol;
Spiramycin;
Chlorpromazine;
Cyamemazine.

Articles

Name:

Cordarone (Amiodarone)

Pharmacological
action:

Antiarrhythmic drug. Amiodarone belongs to class III (class of repolarization inhibitors) and has a unique mechanism of antiarrhythmic action, because in addition to the properties of class III antiarrhythmics (potassium channel blockade), it has the effects of class I antiarrhythmics (sodium channel blockade), class IV antiarrhythmics (calcium channel blockade) and a non-competitive beta-blocker effect.
In addition to the antiarrhythmic effect, the drug has antianginal, coronary dilation, alpha and beta adrenergic blocking effects.
Antiarrhythmic effect:
- an increase in the duration of phase 3 of the action potential of cardiomyocytes, mainly due to blocking the ion current in potassium channels (the effect of class III antiarrhythmics according to the Williams classification);
- decrease in the automaticity of the sinus node, leading to a decrease in heart rate;
- non-competitive blockade of α- and β-adrenergic receptors;
- slowing of sinoatrial, atrial and AV conduction, more pronounced with tachycardia;
- no changes in ventricular conductivity;
- an increase in refractory periods and a decrease in the excitability of the myocardium of the atria and ventricles, as well as an increase in the refractory period of the AV node;
- slowing down conduction and increasing the duration of the refractory period in additional AV conduction bundles.

Other effects:
- absence of negative inotropic effect when taken orally;
- reduction of oxygen consumption by the myocardium due to a moderate decrease in peripheral vascular resistance and heart rate;
- increase coronary blood flow due to direct effects on the smooth muscles of the coronary arteries;
- maintaining cardiac output by reducing pressure in the aorta and reducing peripheral vascular resistance;
- influence on the exchange of thyroid hormones: inhibition of the conversion of T3 to T4 (blockade of thyroxine-5-deiodinase) and blocking the uptake of these hormones by cardiocytes and hepatocytes, leading to a weakening of the stimulating effect of thyroid hormones on the myocardium.
After starting to take the drug orally, the therapeutic effects develop on average within a week (from several days to 2 weeks).
After stopping its use, amiodarone is detected in the blood plasma for 9 months. The possibility of maintaining the pharmacodynamic effect of amiodarone for 10-30 days after its discontinuation should be taken into account.

Pharmacokinetics
Suction
Bioavailability after oral administration in different patients ranges from 30% to 80% (average value is about 50%). After a single dose of the drug inside, Cmax in blood plasma is reached after 3-7 hours. However therapeutic effect usually develops a week after the start of the drug (from several days to 2 weeks).
Distribution
Plasma protein binding is 95% (62% with albumin, 33.5% with beta-lipoproteins).
Amiodarone has a large Vd. Amiodarone is characterized by slow entry into tissues and high affinity for them.
During the first days of treatment, the drug accumulates in almost all tissues, especially in adipose tissue and, in addition, in the liver, lungs, spleen and cornea.
Metabolism
Amiodarone is metabolized in the liver via isoenzymes CYP3A4 and CYP2C8. Its main metabolite, desethylamiodarone, is pharmacologically active and can enhance the antiarrhythmic effect of the main compound.
Amiodarone and its active metabolite desethylamiodarone in vitro have the ability to inhibit the isoenzymes CYP2C9, CYP2C19, CYP2D6, CYP3A4, CYP2A6, CYP2B6 and CYP2C8. Amiodarone and desethylamiodarone have also demonstrated the ability to inhibit certain transporters, such as P-glycoprotein (P-gp) and organic cation transporter (POK2). In vivo, interactions of amiodarone with substrates of the isoenzymes CYP3A4, CYP2C9, CYP2D6 and P-gp were observed.

breeding
Elimination of amiodarone begins after a few days, and the achievement of equilibrium between the intake and elimination of the drug (achieving equilibrium state) occurs after one to several months, depending on the individual characteristics of the patient. The main route of elimination of amiodarone is the intestine.
Amiodarone and its metabolites are not eliminated by hemodialysis.
Amiodarone has a long T1/2 with great individual variability (therefore, when selecting a dose, for example, increasing or decreasing it, it should be remembered that at least 1 month is needed to stabilize the new plasma concentration of amiodarone).
Elimination when taken orally occurs in 2 phases: initial T1/2 (first phase) - 4-21 hours, T1/2 in the 2nd phase - 25-110 days. After prolonged oral administration, the average T1/2 is 40 days. After discontinuation of the drug, complete elimination of amiodarone from the body may continue for several months.
Each dose of amiodarone (200 mg) contains 75 mg of iodine. Part of the iodine is released from the drug and is found in the urine in the form of iodide (6 mg per 24 hours at daily dose amiodarone 200 mg).
Most of the iodine remaining in the drug is excreted through the intestines after passing through the liver, however, with prolonged use of amiodarone, iodine concentrations in the blood can reach 60-80% of the concentrations of amiodarone in the blood.
The peculiarities of the pharmacokinetics of the drug explain the use of loading doses, which is aimed at quickly achieving the required level of tissue impregnation, at which its therapeutic effect is manifested.
Pharmacokinetics in special clinical situations
Due to the insignificant excretion of the drug by the kidneys in patients with renal failure no dose adjustment of amiodarone is required.

Indications for
application:

Relief of attacks of paroxysmal tachycardia;
- relief of attacks of ventricular paroxysmal tachycardia;
- relief of attacks of supraventricular paroxysmal tachycardia with a high frequency of ventricular contractions, especially against the background of Wolff-Parkinson-White syndrome;
- relief of paroxysmal and stable forms of atrial fibrillation (atrial fibrillation) and atrial flutter.

Relapse Prevention:
– life-threatening ventricular arrhythmias and ventricular fibrillation (treatment should be started in the hospital with careful cardiac monitoring);
– supraventricular paroxysmal tachycardia, including documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with organic heart diseases; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients without organic heart disease, when antiarrhythmic drugs of other classes are not effective or there are contraindications to their use; documented attacks of recurrent sustained supraventricular paroxysmal tachycardia in patients with WPW syndrome;
– atrial fibrillation (atrial fibrillation) and atrial flutter.

Prevention of sudden arrhythmic death in patients at high risk, after a recent myocardial infarction, with more than 10 ventricular extrasystoles per 1 hour, clinical manifestations of chronic heart failure and reduced left ventricular ejection fraction (< 40%):
- Cordarone is especially recommended for patients with organic heart diseases (including coronary disease heart), accompanied by left ventricular dysfunction.
Injectable form of Cordarone intended for use in cases where rapid achievement of an antiarrhythmic effect is required or if it is impossible oral administration. For hospital use only.

Mode of application:

Pills.
Loading dose: Various regimens can be used.
In the hospital: the initial dose, divided into several doses, ranges from 600-800 mg to (up to a maximum of 1200 mg) per day until a total dose of 10 g is reached (usually within 5-8 days).
Outpatient: the initial dose, divided into several doses, is from 600 mg to 800 mg per day until a total dose of 10 g is reached (usually within 10-14 days). Maintenance dose: 3 mg/kg body weight per day and can range from 100 mg/day to 400 mg/day as a single dose.
The minimum effective dose should be used according to the individual therapeutic outcome.
Since Cordarone has a very long half-life, it can be taken every second day (200 mg can be given every second day, and 100 mg is recommended to be taken daily); you can also take breaks (2 days a week).
The drug should be taken only as prescribed by a doctor.

Injection.
Intravenous infusion.
The recommended loading dose for adults is 5 mg/kg of the patient's body weight, which should be administered in 250 ml of a 5% glucose solution over 20 minutes to 2 hours.
Administration can be repeated 2-3 times within 24 hours.
The infusion rate should be adjusted according to the results.
The therapeutic effect of the drug appears during the first minutes of administration and then gradually decreases, so a maintenance infusion is necessary.
Recommended maintenance dose for adults: 10-20 mg/kg/day (average 600 to 800 mg/day, maximum dose- 1200 mg/day) in 250 ml of 5% glucose solution for several days.
From the first day of infusion it is necessary to begin the transition to oral administration drug.
Intravenous injection.
The recommended dose for adults is 5 mg/kg and should be administered over at least 3 minutes.
The second injection should be performed no earlier than 15 minutes after the first injection.
If further treatment is necessary, use intravenous infusion.
For children over 3 years of age, the recommended dose is 5 mg/kg.
The pediatrician is responsible for the use of the drug in children. Cordarone should not be mixed in the same syringe with other drugs.

Side effects:

Frequency determination adverse reactions: very often (≥ 10%), often (≥ 1%,<10); нечасто (≥ 0.1%, < 1%); редко (≥ 0.01%, < 0.1%), очень редко, включая отдельные сообщения (< 0.01%), частота неизвестна (по имеющимся данным частоту определить нельзя).
From the cardiovascular system: often – usually moderate, the severity of which depends on the dose of the drug; infrequently - conduction disturbances (sinoatrial block, AV block of various degrees), arrhythmogenic effect (/there are reports of the emergence of new arrhythmias or aggravation of existing ones, in some cases with subsequent cardiac arrest/; in the light of available data it is impossible to determine whether this is caused by the use of drug, or is associated with the severity of heart damage, or is a consequence of treatment failure.
These effects are observed mainly in cases of using the drug Cordarone in conjunction with drugs that prolong the period of repolarization of the ventricles of the heart (QTc interval) or in case of disturbances in the content of electrolytes in the blood).
Very rarely - severe bradycardia or, in exceptional cases, sinus node arrest, which were observed in some patients (patients with sinus node dysfunction and elderly patients); frequency unknown - progression of chronic heart failure (with long-term use), ventricular "pirouette" tachycardia.

From the digestive system: very often - nausea, vomiting, dysgeusia (dullness or loss of taste), usually occurring when taking a loading dose and disappearing after its reduction.
From the liver and biliary tract: very often - an isolated increase in transaminase activity in the blood serum, usually moderate (exceeding normal values by 1.5-3 times; decreases with decreasing dose or spontaneously); often - acute liver damage with increased transaminase activity and/or jaundice, including the development of liver failure, sometimes fatal; very rarely - chronic liver diseases (pseudoalcoholic hepatitis, cirrhosis), sometimes fatal.
Even with a moderate increase in transaminase activity in the blood, observed after treatment lasting more than 6 months, chronic liver damage should be suspected.

From the respiratory system: often - pulmonary toxicity, sometimes fatal (alveolar/interstitial pneumonitis or fibrosis, pleurisy, bronchiolitis obliterans with pneumonia). Although these changes can lead to the development of pulmonary fibrosis, they are largely reversible with early discontinuation of amiodarone and with or without the use of corticosteroids.
Clinical manifestations usually disappear within 3-4 weeks.
Recovery of the X-ray picture and lung function occurs more slowly (several months).
The appearance of severe shortness of breath or a dry cough in a patient taking amiodarone, either accompanied or not accompanied by a deterioration in the general condition (increased fatigue, loss of body weight, increase in body temperature), requires a chest x-ray and, if necessary, discontinuation of the drug.
Very rarely - bronchospasm (in patients with severe respiratory failure, especially in patients with bronchial asthma), acute respiratory distress syndrome (sometimes fatal and sometimes immediately after surgery; possible interaction with high oxygen concentrations is expected).
Frequency unknown - pulmonary hemorrhage.

From the side of the organ of vision: very common - microdeposits in the corneal epithelium, consisting of complex lipids, including lipofuscin, they are usually limited to the pupil area and do not require cessation of treatment and disappear after discontinuation of the drug, sometimes they can cause visual impairment in the form of a colored halo or blurred contours in bright light ; very rarely - optic neuritis/optic neuropathy (no relationship with amiodarone has been established to date; however, since optic neuritis can lead to blindness, if blurred vision or decreased visual acuity occurs while taking Cordarone, a full ophthalmological examination is recommended, including fundoscopy, and if optic neuritis is detected, stop taking the drug).
From the endocrine system: often - hypothyroidism (weight gain, chilliness, apathy, decreased activity, drowsiness, excessive bradycardia compared to the expected effect of amiodarone).
The diagnosis is confirmed by identifying an elevated serum TSH level (using an ultrasensitive TSH test); normalization of thyroid function is usually observed within 1-3 months after cessation of treatment; in life-threatening situations, treatment with amiodarone can be continued with simultaneous additional administration of L-thyroxine under the control of serum TSH levels.

Hyperthyroidism is also common, sometimes fatal, and may occur during and after treatment (cases of hyperthyroidism developing several months after discontinuation of amiodarone have been described).
Hyperthyroidism occurs more silently with a small number of symptoms: minor unexplained weight loss, decreased antiarrhythmic and/or antianginal effectiveness; mental disorders in elderly patients or even the phenomenon of thyrotoxicosis. The diagnosis is confirmed by identifying a reduced serum TSH level (using an ultrasensitive TSH test).
If hyperthyroidism is detected, amiodarone should be discontinued.
Normalization of thyroid function usually occurs within several months after discontinuation of the drug.
In this case, clinical symptoms normalize earlier (after 3-4 weeks) than normalization of thyroid hormone levels occurs. Severe cases can be fatal, so urgent medical intervention is required in such cases. Treatment in each individual case is selected individually.

If the patient's condition worsens both due to thyrotoxicosis itself and due to a dangerous imbalance between the myocardial oxygen demand and its delivery, it is recommended to immediately begin treatment: the use of antithyroid drugs (which may not always be effective in this case), treatment with corticosteroids ( 1 mg/kg), which lasts quite a long time (3 months), beta-blockers.
Very rarely - syndrome of impaired secretion of ADH.
From the skin and subcutaneous tissues: very often - photosensitivity; often (in case of prolonged use of the drug in high daily doses) - grayish or bluish pigmentation of the skin (after stopping treatment, this pigmentation slowly disappears); very rarely - erythema (during radiation therapy), skin rash (usually unspecific), alopecia, exfoliative dermatitis; frequency unknown - urticaria.

From the nervous system: often - tremor or other extrapyramidal symptoms, sleep disturbances, nightmares; uncommon - sensorimotor peripheral neuropathies and/or myopathy (usually reversible after discontinuation of the drug); very rarely - cerebellar ataxia, benign intracranial hypertension (pseudotumor cerebri), headache.
From the side of blood vessels: very rarely - vasculitis.
From the genital organs and breast: very rarely - epididymitis, impotence.
From the blood and lymphatic system: very rarely - thrombocytopenia, hemolytic anemia, aplastic anemia.
From the immune system: frequency unknown - angioedema (Quincke's edema).
Laboratory and instrumental data: very rarely - increased serum creatinine concentration.

Contraindications:

Pills:
- hypersensitivity to iodine and/or amiodarone;
- sick sinus syndrome (sinus bradycardia, sinoatrial block), except in cases of correction with an artificial pacemaker (danger of “stopping” the sinus node);
- disorders of atrioventricular and intraventricular conduction
(atrioventricular block (P-III stage), bundle branch block) in the absence of an artificial pacemaker (pacemaker);
- combination with drugs that can cause polymorphic ventricular tachycardia of the “pirouette” type;
- thyroid dysfunction (hypothyroidism, hyperthyroidism);
- hypokalemia, heart failure (in the stage of decompensation);
- pregnancy;
- lactation period;
- children's age (up to 18 years) (efficacy and safety have not been established);
- simultaneous use of MAO inhibitors;
- interstitial lung diseases.

Injection
Cordarone for intravenous administration is not recommended for use in the following cases:
- allergy to iodine or amiodarone;
- sinus bradycardia, sinoatrial heart block;
- sick sinus syndrome, except in cases of correction by a pacemaker;
- severe conduction disturbances in the absence of an artificial pacemaker,
- in combination with drugs that can cause paroxysmal ventricular tachycardia;
- thyroid dysfunction;
- pregnancy, except in exceptional cases;
- lactation;
- children under 3 years old.

Carefully should be used for decompensated or severe chronic (III-IV functional class according to the NYHA classification) heart failure, liver failure, bronchial asthma, severe respiratory failure, in elderly patients (high risk of developing severe bradycardia), with AV blockade of the first degree.

Since the side effects of amiodarone are dose-related, patients should be treated with the lowest effective doses to minimize the possibility of their occurrence.
Patients should be warned to Avoid exposure to direct sunlight during treatment or took protective measures (eg, applying sunscreen, wearing appropriate clothing).
Treatment monitoring
Before starting amiodarone, it is recommended to conduct an ECG study and determine the potassium level in the blood.
Hypokalemia should be corrected before starting amiodarone.
During treatment ECG must be monitored regularly(every 3 months) and transaminase activity and other indicators of liver function.
In addition, due to the fact that amiodarone can cause hypothyroidism or hyperthyroidism, especially in patients with a history of thyroid disease, before taking amiodarone, clinical and laboratory (serum TSH concentration determined using an ultrasensitive TSH test) examination should be performed for the subject of identifying dysfunctions and diseases of the thyroid gland.

During treatment with amiodarone and for several months after its cessation, the patient should be regularly monitored for clinical or laboratory signs of changes in thyroid function.
If you suspect thyroid dysfunction it is necessary to determine the concentration of TSH in the blood serum (using an ultrasensitive TSH test).
In patients receiving long-term treatment for arrhythmias, an increase in the frequency of ventricular defibrillation and/or an increase in the threshold of the pacemaker or implanted defibrillator has been reported, which may reduce the effectiveness of these devices.
Therefore, before starting or during treatment with amiodarone, their correct functioning should be checked regularly.
Regardless of the presence or absence of pulmonary symptoms during treatment with amiodarone, it is recommended to conduct an X-ray examination of the lungs and pulmonary function tests every 6 months.

The appearance of shortness of breath or dry cough, either isolated or accompanied by deterioration of general condition (fatigue, weight loss, fever), may indicate pulmonary toxicity, such as interstitial pneumonitis, the suspicion of which requires X-ray examination of the lungs and pulmonary function tests.
Due to the prolongation of the period of repolarization of the ventricles of the heart, the pharmacological effect of the drug Cordarone causes certain ECG changes: prolongation of the QT interval, QTc (corrected), the appearance of U waves is possible. An increase in the QTc interval is permissible by no more than 450 ms or by no more than 25% of the original value.
These changes are not a manifestation of the toxic effect of the drug, but require monitoring to adjust the dose and assess the possible proarrhythmogenic effect of the drug Cordarone.
If II and III degree AV block, sinoatrial block or double-bundle intraventricular block develops, treatment should be discontinued. If 1st degree AV block occurs, monitoring should be intensified.

Although arrhythmia was noted or worsening of existing arrhythmias, sometimes fatal, the proarrhythmogenic effect of amiodarone is mild, less than that of most antiarrhythmic drugs, and usually occurs in the context of factors prolonging the QT interval, such as interactions with other drugs and/or electrolyte abnormalities blood.
Despite the ability of amiodarone to prolong the QT interval, it has shown little activity in producing torsade de pointes (TdP).
If vision is blurred or visual acuity is reduced, an immediate ophthalmological examination, including fundus examination, is necessary.
With the development of neuropathy or optic neuritis caused by amiodarone, the drug must be discontinued due to the risk of blindness.
Since Cordarone contains iodine, taking it Maybe interfere with the absorption of radioactive iodine and distort the results of a radioisotope study of the thyroid gland, however, taking the drug does not affect the reliability of determining the content of T3, T4 and TSH in the blood plasma.

Amiodarone inhibits the peripheral conversion of thyroxine (T4) to triiodothyronine (T3) and may cause isolated biochemical changes (increased serum free T4 concentrations, with slightly reduced or even normal serum free T3 concentrations) in clinically euthyroid patients, which is not the cause to discontinue amiodarone.
Development of hypothyroidism can be suspected when the following clinical signs, usually mild, appear: weight gain, cold intolerance, decreased activity, excessive bradycardia.
Before surgery, the anesthesiologist should be informed that the patient is taking Cordarone.
Long-term treatment with Cordarone may increase the hemodynamic risk inherent in local or general anesthesia. This particularly applies to its bradycardic and hypotensive effects, decreased cardiac output and conduction disturbances.

In addition, in rare cases, acute respiratory distress syndrome was observed in patients taking Cordarone immediately after surgery.
These patients require careful monitoring during mechanical ventilation.
Close monitoring of liver function tests is recommended(determination of transaminase activity) before starting to take the drug Cordarone and regularly during treatment with the drug. Acute liver dysfunction (including hepatocellular failure or liver failure, sometimes fatal) and chronic liver damage may occur when taking Cordarone.
Therefore, treatment with amiodarone should be discontinued when transaminase activity increases to 3 times the ULN.
Clinical and laboratory signs of chronic liver failure when taking amiodarone orally can be minimally expressed (hepatomegaly, increased transaminase activity 5 times the ULN) and reversible after discontinuation of the drug, but cases of death with liver damage have been reported.

Impact on the ability to drive vehicles and operate machinery
Based on safety data, there is no evidence that amiodarone impairs the ability to drive or engage in other potentially hazardous activities.
However, as a precautionary measure, it is advisable for patients with paroxysms of severe rhythm disturbances during treatment with Cordarone to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction
other medicinal
by other means:

Drugs that can cause torsade de pointes (TdP) or prolong the QT interval
Drugs that can cause torsade de pointes (TdP)
Combination therapy with drugs that can cause ventricular torsades de pointes is contraindicated, because the risk of developing potentially fatal ventricular torsade de pointes (TdP) increases.
- antiarrhythmic drugs: class I A (quinidine, hydroquinidine, disopyramide, procainamide), sotalol, bepridil;
- other (non-antiarrhythmic) drugs such as; vincamine; some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sulpride, tiapride, veralipride), butyrophenones (droperidol, haloperidol), sertindole, pimozide; tricyclic antidepressants; cisapride; macrolide antibiotics (erythromycin with intravenous administration, spiramycin); azoles; antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine for parenteral administration; difemanil methyl sulfate; mizolastine; astemizole; terfenadine

Drugs that can prolong the QT interval
Co-administration of amiodarone with drugs that can increase the duration of the QT interval should be based on a careful assessment for each patient of the ratio of expected benefits and potential risks (the possibility of an increased risk of developing ventricular "torsade de pointes"); when using such combinations, it is necessary to constantly monitor the ECG of patients (to identify prolongation of the QT interval), the content of potassium and magnesium in the blood.
Fluoroquinolones, including moxifloxacin, should be avoided in patients taking amiodarone.
Drugs that reduce heart rate or cause automaticity or conduction disorders
Combination therapy with these drugs is not recommended.
Beta-blockers, slow calcium channel blockers that reduce heart rate (verapamil, diltiazem) can cause disturbances in automaticity (development of excessive bradycardia) and conduction.

Drugs that can cause hypokalemia
Not Recommended Combinations
- with laxatives that stimulate intestinal motility, which can cause hypokalemia, which increases the risk of developing torsade de pointes. When combined with amiodarone, laxatives from other groups should be used.
Combinations requiring caution when using
- with diuretics that cause hypokalemia (in monotherapy or in combination with other drugs);
- with systemic corticosteroids (glucocorticoids, mineralocorticoids), tetracosactide;
- with amphotericin B (in / in the introduction).
It is necessary to prevent the development of hypoglycemia, and in case of its occurrence, restore the potassium content in the blood to normal levels, monitor the concentration of electrolytes in the blood and ECG (for possible prolongation of the QT interval), and in the event of ventricular “torsade de pointes” tachycardia, antiarrhythmic drugs should not be used (ventricular pacing should be started; intravenous administration of magnesium salts is possible).

Preparations for inhalation anesthesia
The possibility of developing the following severe complications in patients taking amiodarone while receiving general anesthesia has been reported: bradycardia (resistant to atropine), arterial hypotension, conduction disturbances, and decreased cardiac output.
Very rare cases of severe complications from the respiratory system, sometimes fatal (acute adult respiratory distress syndrome), which developed immediately after surgery, the occurrence of which is associated with high oxygen concentrations, have been observed.
Drugs that reduce heart rate (clonidine, guanfacine, cholinesterase inhibitors (donepezil, galantamine, rivastigmine, tacrine, ambenonium chloride, pyridostigmine bromide, neostigmine bromide), pilocarpine
Risk of developing excessive bradycardia (cumulative effects).
Effect of amiodarone on other drugs
Amiodarone and/or its metabolite desethylamiodarone inhibit the isoenzymes CYP3A4, CYP2C9, CYP2D6 and P-gp and may increase the systemic exposure of drugs that are their substrates. Due to the long half-life of amiodarone, this interaction may occur even several months after discontinuation of amiodarone.

Drugs that are P-gp substrates
Amiodarone is a P-gp inhibitor. It is expected that its combined use with drugs that are P-gp substrates will lead to increased systemic exposure of the latter.
Cardiac glycosides (digitalis preparations)
Possibility of disturbances in automaticity (severe bradycardia) and atrioventricular conduction. In addition, when combining digoxin with amiodarone, an increase in the concentration of digoxin in the blood plasma is possible (due to a decrease in its clearance). Therefore, when combining digoxin with amiodarone, it is necessary to determine the concentration of digoxin in the blood and monitor possible clinical and electrocardiographic manifestations of digitalis intoxication. Digoxin dosages may need to be reduced.
Dabigatran
Caution should be exercised when amiodarone is used concomitantly with dabigatran due to the risk of bleeding. The dose of dabigatran may need to be adjusted in accordance with the instructions in its instructions for use.

Medicines that are substrates of the CYP2C9 isoenzyme
Amiodarone increases the blood concentration of drugs that are substrates of the CYP2C9 isoenzyme, such as warfarin or phenytoin due to inhibition of cytochrome P450 2C9.
Warfarin
When warfarin is combined with amiodarone, the effects of the indirect anticoagulant may be enhanced, which increases the risk of bleeding. Prothrombin time (MHO) should be monitored more frequently and anticoagulant doses adjusted, both during treatment with amiodarone and after discontinuation of its use.
Phenytoin
When combining phenytoin with amiodarone, an overdose of phenytoin may develop, which can lead to the appearance of neurological symptoms; clinical monitoring is necessary and, at the first signs of overdose, a reduction in the dose of phenytoin; it is advisable to determine the concentration of phenytoin in the blood plasma.

Medicines that are substrates of the CYP2D6 isoenzyme
Flecainide
Amiodarone increases plasma concentrations of flecainide due to inhibition of the CYP2D6 isoenzyme. Therefore, dose adjustment of flecainide is required.
Medicines that are substrates of the CYP3A4 isoenzyme
When amiodarone, an inhibitor of the CYP3A4 isoenzyme, is combined with these drugs, their plasma concentrations may increase, which may lead to increased toxicity and/or increased pharmacodynamic effects and may require a reduction in their doses. Such drugs are listed below.
Cyclosporine
The combination of cyclosporine with amiodarone may increase plasma concentrations of cyclosporine; dose adjustment is necessary.

Fentanyl
Combination with amiodarone may increase the pharmacodynamic effects of fentanyl and increase the risk of developing its toxic effects.
HMG-CoA reductase inhibitors (statins) (simvastatin, atorvastatin and lovastatin)
Increased risk of statin muscle toxicity when used concomitantly with amiodarone. The use of statins that are not metabolized by the CYP3A4 isoenzyme is recommended.
Other drugs metabolized by CYP3A4: lidocaine (risk of sinus bradycardia and neurological symptoms), tacrolimus (risk of nephrotoxicity), sildenafil (risk of increased side effects), midazolam (risk of psychomotor effects), triazolam, dihydroergotamine, ergotamine, colchicine ).
A drug that is a substrate of CYP2D6 and CYP3A4 isoenzymes - dextromethorphan
Amiodarone inhibits CYP2D6 and CYP3A4 and may theoretically increase plasma concentrations of dextromethorphan.

Clopidogrel
Clopidogrel, which is an inactive thienopyrimidine drug, is metabolized in the liver to form active metabolites. There is a possible interaction between clopidogrel and amiodarone, which may lead to a decrease in the effectiveness of clopidogrel.
Effect of other drugs on amiodarone
Inhibitors of CYP3A4 and CYP2C8 isoenzymes may have the potential to inhibit the metabolism of amiodarone and increase its concentration in the blood and, accordingly, its pharmacodynamic and side effects.
It is recommended to avoid CYP3A4 inhibitors (eg, grapefruit juice and certain drugs such as cimetidine and HIV protease inhibitors (including indinavir) during therapy with amiodarone. HIV protease inhibitors, when used concomitantly with amiodarone, may increase amiodarone concentrations in blood.

CYP3A4 isoenzyme inducers
Rifampicin
Rifampicin is a potent inducer of the CYP3A4 isoenzyme; when used in combination with amiodarone, it can reduce plasma concentrations of amiodarone and desethylamiodarone.
Preparations of St. John's wort
St. John's wort is a potent inducer of the CYP3A4 isoenzyme. In this regard, it is theoretically possible to reduce the plasma concentration of amiodarone and reduce its effect (clinical data are not available).

Pregnancy:

Pregnancy
Currently available clinical information is insufficient to determine the possibility or impossibility of developmental defects in the embryo when using amiodarone in the first trimester of pregnancy.
Since the fetal thyroid gland begins to bind iodine only from the 14th week of pregnancy (amenorrhea), amiodarone is not expected to affect it if it is used earlier.
Excess iodine when using the drug after this period can lead to the appearance of laboratory symptoms of hypothyroidism in the newborn or even to the formation of a clinically significant goiter.
Due to the effect of the drug on the fetal thyroid gland, amiodarone is contraindicated during pregnancy, except in special cases when the expected benefit outweighs the risks (in case of life-threatening ventricular arrhythmias).
Breastfeeding period
Amiodarone is excreted into breast milk in significant quantities, so it is contraindicated during breastfeeding (during this period the drug should be discontinued or breastfeeding should be stopped).

Overdose:

Symptoms: When ingesting very large doses, several cases of sinus bradycardia, cardiac arrest, attacks of ventricular tachycardia, paroxysmal ventricular “torsade de pointes” and liver damage have been described. Possible slowdown of AV conduction, worsening of existing heart failure.
Treatment: gastric lavage, use of activated charcoal, if the drug has been taken recently, in other cases, symptomatic therapy is carried out: for bradycardia - beta-adrenergic stimulants or installation of a pacemaker, for ventricular "pirouette" tachycardia - intravenous administration of magnesium salts or cardiac stimulation.
Neither amiodarone nor its metabolites are removed by hemodialysis. There is no specific antidote.

1 ampoule of Cordarone solution for intravenous administration contains:
- active ingredient: amiodarone hydrochloride - 150 mg;
- excipients: benzyl alcohol - 60 mg, polysorbate 80 - 300 mg, water for injection - up to 3 ml.

Kordaron refers to cardiovascular drugs. Released only by prescription.

Pharmacological action of Kordaron

Cordarone is an antiarrhythmic drug of the third class. Eliminates angina pectoris and arrhythmia, helps block adrenergic receptors, slow down sinoatrial, atrial and nodal conduction, without affecting intraventricular conduction.

The drug also reduces myocardial excitability and lengthens the refractory period. Cordarone also has an antianginal effect due to a decrease in myocardial oxygen consumption. This occurs due to a decrease in heart rate and a decrease in total vascular peripheral resistance. Due to its direct effect on the muscles of the arteries, Cordarone increases coronary blood flow; in addition, the drug supports cardiac output and reduces myocardial contractility.

According to reviews, Cordarone reaches maximum activity 15 minutes after intravenous administration, and the medicinal effect on the body continues for four hours. Gradually, the amount of the drug in the blood decreases, but this does not prevent it from saturating the tissues. If the patient does not receive repeated injections, the drug is eliminated from the body within several months.

Release form

Kordaron is issued in the form of solution and tablets.

Indications for Kordaron's use

Cordarone is used to relieve attacks of paroxysmal tachycardia, to relieve paroxysmal ventricular and supraventricular tachycardia, accompanied by a high frequency of ventricular contractions, to remove paroxysmal and stable forms of atrial fibrillation, as well as atrial flutter.

According to reviews of Cordarone, the drug is effective in the treatment of patients suffering from heart diseases of organic origin (including coronary heart disease), which are accompanied by changes in left ventricular function.

Application instruction of Kordaron

According to the instructions Kordaron tablets are taken according to several schemes.

Outpatient treatment begins with taking 600 to 800 milligrams of the drug per day, divided into several times. After a period of 10 to 14 days, when the total amount of the drug taken reaches 10 grams, the patient is recommended to take a maintenance dose, which is prescribed at the rate of 3 milligrams per kilogram of weight (on average, from 100 to 400 milligrams per day).

During inpatient treatment, the patient is first prescribed to take the drug from 600 to 800 grams per day (the maximum dose is 1200 milligrams). Within 5-8 days, bring up to 10 grams.

Since Cordarone has a long half-life, the drug can be taken daily in the amount of 100 milligrams and every second day in the amount of 200 milligrams. Breaks in taking the drug are allowed two days a week.

Cordarone solution is used for intravenous injections and infusions. When performing an infusion, the loading dose for an adult is 5 milligrams per kilogram of body weight. Cordarone is dissolved in 250 milliliters of 5% glucose. The infusion lasts from 20 minutes to 2 hours. During the day, the administration is repeated 2-3 times.

Over time, the effect of the drug gradually decreases, so a maintenance infusion is recommended, for which adults are prescribed the drug at a rate of 10 to 20 milligrams per 1 kilogram of weight (an average of 600 to 800 milligrams per day, the maximum dose is no more than 1200 milligrams) . This dose is also diluted in 250 milliliters of 5% glucose before administration.

The dose recommended for adult patients is 5 milligrams per 1 kilogram of weight. The procedure is carried out within three minutes, the next injection is no earlier than 15 minutes after the previous one. If it is necessary to continue treatment, it is recommended to switch to infusion administration.

Cordarone can also be used by children after they reach the age of three. Dosage – 5 milligrams per 1 kilogram of weight. The syringe should not contain any other drug except Cordarone; mixing it with other drugs is not allowed.

In case of an overdose of the drug, the following are possible: sinus bradycardia, paroxysmal ventricular tachycardia, cardiac arrest, ventricular tachycardia of the “pirouette” type, impaired liver and circulatory function, decreased blood pressure.

To eliminate the symptoms of overdose, symptomatic treatment is prescribed, including gastric lavage, taking cholestyramine; for pirouette-type tachycardia, intravenous administration of magnesium salts, as well as reducing cardiac pacing; for bradycardia, beta stimulators or the installation of a pacemaker are prescribed.

Side effects of Cordarone

The use of the drug can lead to: deposition of lipofuscin in the corneal epithelium, photosensitivity, hypothyroidism, hyperthyroidism, bradycardia, hypotension, decreased AV conductivity, alveolitis, nausea, impaired liver function, heaviness in the epigastrium.

There are reviews of Cordarone as a drug that provokes tremor and the development of peripheral neuropathy.

With parenteral administration, fever, sweating, apnea, bronchospasm, phlebitis, and increased intracranial pressure may occur.

Contraindications to the use of Cordarone

According to the instructions, it is not recommended to prescribe Cordarone in tablets if the patient is intolerant to amiodarone or iodine, with weakness of the sinus node, changes in intraventricular and atrioventricular conduction, dysfunction of the thyroid gland, hypokalemia, heart failure, interstitial pulmonary disease.

In addition, the drug in tablets is contraindicated in children under 18 years of age, as well as in nursing and pregnant women.

It is not allowed to administer Kordaron intravenously to children under the age of three years and to lactating women. The drug is prescribed to pregnant women only in exceptional cases.

The simultaneous use of Kordaron with antiarrhythmic drugs, as well as with sultopride, vincamine, pentamidine for parenteral administration, erythromycin for intravenous administration, is not recommended, since the development of ventricular tachycardia of the "pirouette" type is possible.

It is forbidden to carry out combination therapy with beta-blockers, as well as individual calcium channel blockers (these include: verapamil, diltiazem). The consequences of the simultaneous administration of Kordaron with these drugs may be a violation of automatism (in the form of bradycardia) and conduction.

It is forbidden to take Kordaron together with laxative drugs, drugs that provoke the occurrence of hypokalemia, with anticoagulants, with cardiac glycosides, with cyclosporine, phenytoin, flecainide, simvastatin. In addition, according to the instructions, Kordaron is not recommended for patients who have undergone general anesthesia.

Storage conditions and periods

The drug in the form of tablets is recommended to be stored in a dark place at a positive temperature not exceeding 30 ° C. Shelf life - three years. Cordarone solution for intravenous administration is stored in a dry place where the temperature does not exceed 25°C. Shelf life is two years.

My review will be devoted to Cordarone, a drug for the treatment of arrhythmias. This is a drug for long-term treatment, and for "ambulance", and for prevention.... In any case, this is indeed a very, very strong medicine. Therefore, I’ll probably break the “traditions” of pharmacological reviews a little by talking about Cordarone. But I hope that this is forgivable, if only because I will describe here an important drug, and, moreover, an interesting drug!

Besides, Cordarone dilates coronary vessels and reduces blood pressure. These are not its main effects (the main one is antiarrhythmic), but they are also quite pronounced.

At its core, Cordarone is “ analogue of thyroid hormones. It blocks the activation of thyroxine, and this effect is often a problem with long-term treatment. In most cases, Kordaron is not prescribed as a drug for continuous use, therefore its benefit, even against the backdrop of this feature, exceeds the harm from it.

It turned out a little differently for me: I took a variety of antiarrhythmics, but the effect of the treatment was still not satisfactory. For almost two years I consistently drank half a tablet of Etatsizin a day, and felt quite good. When even stopped working, my doctor had to prescribe me Cordaron (daily!), because he guaranteed to eliminate the arrhythmia.

After 8 months of admission, I had all symptoms of hypothyroidism: weight began to grow steadily, terrifying weakness appeared, constant drowsiness. It became difficult for me to do any business - I immediately felt tired. TSH in tests increased several times (last time it was almost 16.5, instead of 3-4!). All this was also aggravated by the fact that about ten years ago I had a lobe of my thyroid gland removed.

In addition to hypothyroidism, I experienced other side effects:

blurred vision;
bradycardia;
sleep disturbance;
change in skin color - it became bluish;
tremor;
photosensitivity - being in the sun is sometimes frankly painful.

My doctor warned me about these consequences. He also mentioned other frequent adverse reactions to take Cordarone:

nausea and vomiting;
change in taste sensations;
decreased appetite;
heaviness and pain in the abdomen;
the occurrence of acute hepatitis;
pneumonia, pulmonary fibrosis.

It is worth mentioning separately that how Kordaron is combined with other drugs. Surely, a whole book could be written about this, but, fortunately, I don’t have much experience in this. I had to stop taking it, because from the joint use of these drugs, the pulse constantly dropped to 50-55 / minute, which is not enough for me. Now I don’t take anything at all to treat arterial hypertension; Cordarone lowers my blood pressure to normal levels.

Another drug is . I do not have a diagnosis of coronary heart disease (and even atherosclerosis, supposedly), but the blood is “thick”, and Plavix was needed as a preventive measure. I didn’t stop taking it, but I had to reduce the dose: in combination with Cordarone, all the side effects of Plavix and similar drugs appear much more often.

An interesting property of Cordarone: the indications for the use of tablets and injections are different.

Tablet forms shown for the treatment of all types of arrhythmias and their prevention:

atrial fibrillation and flutter;
sudden “arrhythmic death”;
paroxysmal tachycardias;
atrial fibrillation.

Injections (droppers) with Kordaron are used as "Ambulance" if cardioresuscitation is necessary, for example, to eliminate ventricular fibrillation (this condition can lead to death in 40-50 seconds!).

For drugs such as Cordarone, there are no contraindications. If the medicine is used "for health reasons", that is, in the absence of treatment, the patient may die, only the relationship between benefits and harms of the drug.

Nevertheless, here are the conditions in which Cordarone is prescribed especially carefully:

thyroid disease is the most important condition;
sick sinus syndrome;
inadequate response of the body to iodine;
severe forms of intracardiac blockade;
deficiency of potassium and magnesium;
pregnancy.

As I already indicated, these are NOT contraindications. Cordarone can be used for these conditions, but only if it is a matter of preserving the patient’s life.

Thank you for your attention, and may arrhythmias bypass you. Do not be ill!