Amiodarone concentrate 50mg/ml 3ml ampoules, 10pcs

Composition

1 ampoule (3 ml of solution) contains: Active ingredient: amiodarone hydrochloride-150 mg; excipients: sodium acetate trihydrate, ice acetic acid, polysorbate 80, benzyl alcohol, water for injection.

Pharmacological action

Antianginal, antiarrhythmic.

Indications

Treatment with the drug should be started in a hospital setting and under the supervision of a specialist. The drug is intended only for the treatment of severe arrhythmias that do not respond to other treatments, or when other treatments cannot be used.

Tachyarrhythmias associated with Wolf-Parkinson-White syndrome.

Tachyarrhythmias of all types, including supraventricular, nodular and ventricular tachycardia; flutter and atrial fibrillation, ventricular fibrillation; in the case when other medications cannot be used.

The drug can be used when a rapid response to treatment is required or when oral use is not possible.

Contraindications

syndrome of weakness of the sinus node (SSSU), sinus bradycardia, sinoatrial block, except the correction of an artificial pacemaker;

– atrioventricular block II and III degree, violation of intraventricular conduction (blockade of two or three feet of bundle branch block); in these cases, the drug can be used in specialized departments under the guise of an artificial pacemaker (pacemaker);

– cardiogenic shock, collapse;

– severe hypotension;

– concomitant use of drugs that can cause polymorphic ventricular tachycardia type “pirouette”;

– dysfunction of the thyroid gland (hypothyroidism, hyperthyroidism);

– hypokalemia;

– pregnancy;

breast– feeding;

– hypersensitivity to iodine and/or amiodarone;

– severe dysfunction of the lungs (interstitial lung disease);

– decompensated cardiomyopathy or heart failure (possible worsening of the patient’s condition).

Due to the presence of benzyl alcohol, Amiodarone is contraindicated in newborns, infants, and children under 3 years of age.

Side effects

From the cardiovascular system: often-bradycardia (usually a moderate decrease in heart rate); decrease in blood pressure, usually moderate and transient. Cases of severe hypotension or collapse have been observed with overdose or too rapid use of the drug. Very rarely — proarrhythmogenic effect (there are reports of new arrhythmias, including polymorphic ventricular tachycardia of the “pirouette” type, or aggravation of existing ones — in some cases with subsequent cardiac arrest). These effects are observed mainly in cases of using the drug together with drugs that prolong the period of repolarization of the ventricles of the heart (QT interval) or in cases of electrolyte balance disorders (see “Interaction”). In the light of the available data, it is not possible to determine whether the occurrence of these rhythm disturbances is caused by amiodarone, or is related to the severity of cardiac pathology, or is a consequence of ineffective treatment. Severe bradycardia or, in exceptional cases, sinus node arrest, which was observed in some patients (patients with sinus node dysfunction and elderly patients), flushes of blood to the skin of the face, progression of heart failure (possibly with intravenous jet use). From the respiratory system: very rarely — cough, shortness of breath, interstitial pneumonitis; bronchospasm and/or apnea in patients with severe respiratory insufficiency, especially in patients with bronchial asthma; acute respiratory distress syndrome, sometimes fatal and sometimes immediately after surgery (it is assumed that interaction with high oxygen concentrations is possible) (see “Special Instructions”). From the digestive system: very often-nausea. Very rarely-an isolated increase in the activity of hepatic transaminases in the blood serum, usually moderate (1.5-3 times higher than normal values) and decreasing with a decrease in the dose or even spontaneously. Acute liver damage (within 24 hours after use of amiodarone) with increased transaminases and / or jaundice, including the development of liver failure, sometimes fatal (see “Special instructions”). From the skin: very rarely-a feeling of heat, increased sweating. From the central nervous system: very rarely — benign intracranial hypertension (pseudotumor of the brain), headache. Immune system disorders: very rare-anaphylactic shock. Unknown frequency-angioedema. Injection site reactions: often-inflammatory reactions, such as superficial phlebitis, when administered directly into a peripheral vein. Injection site reactions such as: pain, erythema, edema, necrosis, transudation, infiltration, inflammation, induration, thrombophlebitis, phlebitis, cellulitis, infection, pigmentation. Method of preparation or application: Amiodarone (injectable form) is intended for use in cases where rapid achievement of an antiarrhythmic effect is required or it is impossible to use the drug inside. With the exception of urgent clinical situations, the drug should only be used in a hospital in the intensive care unit under constant monitoring of ECG and blood pressure. When administered intravenously, the drug should not be mixed with other drugs or simultaneously administered other drugs through the same venous access. Use only in diluted form. Only 5% dextrose (glucose) solution should be used for dilution. Due to the peculiarities of the dosage form of the drug, it is not recommended to use concentrations of the infusion solution that are less than those obtained by diluting 2 amp. in 500 ml of 5% dextrose (glucose). To avoid reactions at the injection site, amiodarone should be administered through a central venous catheter, except in cases of cardiac resuscitation in ventricular fibrillation resistant to cardioversion, when (in the absence of central venous access) peripheral veins (the largest peripheral vein with maximum blood flow) can be used to administer the drug. Severe cardiac arrhythmias in cases where oral use is not possible (except in cases of cardiac resuscitation in cardiac arrest caused by ventricular fibrillation resistant to cardioversion)

Interaction

Drugs that can cause ventricular tachycardia of the “pirouette” type are primarily Class Ia and Class III antiarrhythmics and some neuroleptics. Hypokalemia is a predisposing factor, as is bradycardia or congenital or acquired prolongation of the QT interval.

Combinations with

– Drugs that can cause ventricular tachycardia of the “pirouette” type are contraindicated.

– Class Ia antiarrhythmic drugs (quinidine, hydroquinidine, isopyramide).

– Class III antiarrhythmic drugs (dofetilide, ibutilide, sotalol).

– Other drugs, such as bepridil, cisaprid, difemanil, IV ritromycin, mizolastine, IV vincamine, moxifloxacin, iv spiramycin.

“Sultoprid. “

The risk of ventricular arrhythmias (pirouette-type tachycardia) increases.

These contraindications do not apply to the use of amiodarone for cardiopulmonary resuscitation in the event of cardiac arrest that is resistant to electrical defibrillation.

Not recommended combinations with

Cyclosporine

It is possible to increase the level of cyclosporine in plasma, associated with a decrease in the metabolism of the drug in the liver, with possible nephrotoxic manifestations.

Determination of cyclosporine levels in the blood, testing of renal function and revision of dosage during treatment with amiodarone and after discontinuation of the drug.

Diltiazem for injection

Risk of bradycardia and atrioventricular block. If a combination is unavoidable, strict clinical and continuous ECG monitoring should be established.

Risk of bradycardia and atrioventricular block with Verapamil for injection. If a combination is unavoidable, strict clinical and continuous ECG monitoring should be established.

Antiparasitic drugs that can cause tachycardia of the “pirouette” type (halofantrine, pentamidine, lumefantrine)

If the combination is unavoidable, preliminary monitoring of the QT interval and ECG monitoring is necessary.

Neuroleptics that can cause ventricular tachycardia of the “pirouette”type:

Some phenothiazine neuroleptics (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, tiapride, veralipride), butyrophenones (droperidol, haloperidol), other neuroleptics (pimozide).

The risk of ventricular arrhythmias (pirouette-type tachycardia) increases.

Methadone

The risk of ventricular arrhythmias (pirouette-type tachycardia) increases. Recommended: ECG and clinical observation.

Combinations that require caution when using Amiodarone with:

Oral anticoagulants:

Increased anticoagulant effect and risk of bleeding due to increased plasma concentrations of anticoagulants. The need for more frequent monitoring of blood prothrombin and MHO (INR) levels, as well as adaptation of anticoagulant doses during treatment with amiodarone and after discontinuation of the drug.

Beta-blockers, with the exception of sotalol (contraindicated combination) and esmolol (combination requiring caution when used)

Disorders of contractility, automatism and conduction (suppression of compensatory sympathetic mechanisms). Clinical and ECG monitoring.

Beta-blockers prescribed for heart failure (bisoprolol, carvedilol, metoprolol)

Disorders of contractility and conduction (synergistic effect) with the risk of severe bradycardia. Increased risk of ventricular arrhythmias, especially pirouette-type tachycardia.

Regular clinical and electrocardiographic monitoring is required.

Cardiac glycosides

Violations of automatism (excessive bradycardia) and atrioventricular conduction (synergism of action). When using digoxin, an increase in its concentration in plasma (due to a decrease in the clearance of the alkaloid).

Clinical and ECG monitoring, as well as determination of plasma digoxin levels, should be performed); it may be necessary to change the dose of digoxin.

Oral diltiazem

Increases the risk of bradycardia and atrioventricular block, especially in the elderly. Clinical and ECG monitoring.

Verapamil for oral use

Risk of bradycardia and atrioventricular block, especially in the elderly. Clinical and ECG monitoring.

Esmololom

Disorders of contractility, automatism and conduction (suppression of compensatory sympathetic mechanisms). Clinical and ECG monitoring.

Hypokalemic drugs: potassium-removing diuretics (in monotherapy or combination), laxatives of a stimulating nature, amphotericin B (iv) glucocorticoids (systemic), tetracosactide.

The risk of ventricular arrhythmias increases, especially pirouette-type tachycardia (hypokalemia is a predisposing factor). Clinical and ECG monitoring, laboratory tests.

The risk of increased plasma lidocaine concentrations, with the likelihood of neurological and cardiological side effects, due to a decrease in amiodarone lidocaine metabolism in the liver. Clinical and ECG monitoring, if necessary, dose adjustment of lidocaine during treatment with amiodarone and after its withdrawal.

Orlistat

Increases the risk of reducing the concentration of amiodarone and its active metabolite in plasma. Clinical and, if necessary, ECG monitoring,

with Phenytoin (and, by extrapolation, phosphenytoin)

An increase in the level of phenytoin in plasma with symptoms of overdose, especially of a neurological nature (decreased metabolism of phenytoin in the liver). Clinical monitoring and determination of the level of phenytoin in plasma; if possible, reduce the dose of phenytoin.

Simvastatin

Increased risk of side effects (dose-dependent) such as rhabdomyolysis (decreased metabolism of simvastatin in the liver). The dose of simvastatin should not exceed 20 mg per day.

If a therapeutic effect cannot be achieved at this dose, you should switch to another statin that does not interact with this type of interaction.

Tacrolimus

Increased blood levels of tacrolimus due to inhibition of its metabolism by amiodarone. Blood tacrolimus levels should be measured, kidney function monitored, and tacrolimus levels equalized.

Drugs that cause bradycardia:

Many medications can cause bradycardia. This is especially true for Class Ia antiarrhythmic drugs, beta blockers, some Class III antiarrhythmic drugs, some calcium channel blockers, digitalis, pilocarpine and anticholinesterase agents.

Risk of excessive bradycardia (cumulative effect).

Combinations to take into account

Drugs that cause bradycardia: calcium channel blockers with a bradycardic effect (verapamil), beta-blockers (except sotalol), clonidine, guanfacine, digitalis alkaloids, mefloquine, cholinesterase inhibitors (donezepil, galantamine, rivastigmine, tacrine, ambemonium, pyridostigmine, neostigmine), pilocarpine.

Risk of excessive bradycardia (cumulative effects).

Incompatibilities

When using a material or medical equipment made of PVC plasticized with 2-diethylhexyl phthalate (DEHP) in the presence of an injectable solution of amiodarone, DEHP can be released. To minimize exposure to DEHP, it is recommended that the final dilution of the solution be carried out before infusion in equipment that does not contain DEHP.

How to take, course of use and dosage

The method of application is intravenous.

Do not dilute the drug with an isotonic sodium chloride solution, as precipitation may form!

Do not mix with other medicines in the same infusion system.

The drug should only be used when the necessary equipment is available for monitoring cardiac function, defibrillation, and pacing.

The drug can be used before performing direct current cardioversion.

The standard recommended dose is 5 mg / kg of body weight, which is administered by infusion over a period of time from 20 minutes to 2 hours. The drug can be administered as a solution diluted in 250 ml of 5% glucose solution. After that, the drug can be re-infused at a dose of up to 1200 mg (approximately 15 mg/kg body weight) in a 5% glucose solution of up to 500 ml for 24 hours, and the infusion rate should be adjusted depending on the patient’s clinical response (see the section “Precautions”).

In extremely urgent clinical situations, the drug, at the discretion of the doctor, can be administered as a slow injection at a dose of 150-300 mg in 10-20 ml of 5% glucose solution for at least 3 minutes. After that, repeated use of the drug can be carried out no earlier than in 15 minutes. Patients who are administered the drug in the manner described above should be carefully monitored – for example, in the intensive care unit (see the section “Precautions”).

Switching from intravenous to oral use

Immediately after receiving a proper response to treatment, it is necessary to simultaneously start oral therapy with the drug at the usual loading dose (i. e. 200 mg three times a day). After that, the drug should be gradually discontinued by gradually reducing the dose.

Children

The safety and efficacy of amiodarone in children have not been evaluated, so the use of this drug in children is not recommended. The drug contains benzyl alcohol. There have been reports of deaths due to the development of “dyspnea syndrome “(“gasping syndrome”). in newborns after use of solutions containing this preservative. Symptoms of this complication include sudden onset of shortness of breath, hypotension, bradycardia, and the development of cardiovascular collapse.

Elderly patients

As with other patients, it is important to use the minimum effective dose of the drug. Although there is no evidence to support specific dosage requirements in this group of patients, these patients may be more likely to develop bradycardia and conduction disturbances when using too high a dose. Special attention should be paid to monitoring thyroid function (see sections “Contraindications”, “Precautions” and “Adverse reactions”).

Patients with renal and / or hepatic insufficiency

Although no dose adjustment was required for patients with renal or hepatic impairment during long-term oral use of amiodarone, careful clinical monitoring of this category of patients, especially the elderly, in the intensive care unit is necessary.

Cardiopulmonary resuscitation

The recommended dose for ventricular fibrillation/ventricular tachycardia with no pulse, defibrillation-resistant, is 300 mg (or 5 mg/kg body weight), which is administered diluted in 20 ml of 5% glucose solution by rapid injection. If ventricular fibrillation persists, an additional 150 mg (or 2.5 mg/kg body weight) of the drug may be used.

Overdose

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

Treatment: symptomatic therapy is performed (for bradycardia – beta-adrenostimulants or pacemaker installation, for pirouette-type tachycardia-intravenous use of magnesium salts, reducing pacing). Amiodarone and its metabolites are not removed during hemodialysis and peritoneal dialysis.

Special instructions

– Disorders of electrolyte metabolism, especially hypokalemia: it is important to take into account situations that may be accompanied by hypokalemia, as predisposing to proarrhythmic phenomena. Hypokalemia should be corrected before starting the use of amiodarone

– With the exception of cases of emergency therapy, Amiodarone in the form of a solution for intravenous injection can only be used in a hospital and with constant monitoring (ECG, blood pressure).

Use with caution in patients with chronic heart failure, liver failure, bronchial asthma, and the elderly.

Form of production

Concentrate for preparing a solution for intravenous use in the form of a transparent, yellowish or greenish liquid.

Active ingredient

Amiodarone

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

For adults, For adults as prescribed by a doctor

Indications

Myocardial Infarction, Arrhythmia, Heart Failure