Amiodarone, 50 mg/ml concentrate 3 ml 10 pcs

Myocardial infarction, Heart failure, Arrhythmia, Rapid heartbeat

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

Tachyarrhythmias associated with Wolff-Parkinson-White syndrome.

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

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

Active ingredient

How to take, the dosage

The method of administration is intravenous.

Do not dilute the drug with isotonic sodium chloride solution as precipitate formation is possible!

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

The medication should only be used when the necessary equipment is available to monitor cardiac function, defibrillation and pacing.

The drug can be used before direct current cardioversion.

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

In extremely urgent clinical situations, the drug, at the discretion of the physician, may be administered as a slow injection in a dose of 150-300 mg in 10-20 ml of 5% glucose solution for at least 3 minutes. Thereafter, the drug may be administered again not earlier than 15 minutes later. Patients who are administered the drug in the above manner should be closely monitored – for example, in the intensive care unit (see section “Precautions”).

Transition from intravenous to oral administration

After an appropriate response to treatment, oral therapy with the medication at the usual loading dose (i.e., 200 mg three times daily) should be started at the same time. Thereafter, the medication should be withdrawn gradually by stepwise dose reduction.

In children

The safety and effectiveness of amiodarone in children has not been evaluated, so the use of this drug in children is not recommended. The drug contains benzyl alcohol. There have been reports of cases of death due to the development of “dyspnea syndrome” (“Gasping Syndrome”) in infants after administration of solutions containing this preservative. Symptoms of this complication include sudden onset of dyspnea, arterial hypotension, bradycardia and development of cardiovascular collapse.

Elderly patients

As with other patients, it is important to use the lowest effective dose of the drug. Although there is no evidence to support specific dosing requirements in this group of patients, these patients may be more prone to develop bradycardia and conduction abnormalities if too high a dose is used. Particular attention should be paid to monitoring thyroid function (see Contraindications, Precautions, and Adverse Reactions).

Patients with renal and/or hepatic impairment

While no dose adjustments were required for patients with renal or hepatic impairment during long-term oral use of amiodarone, close clinical monitoring of this patient category, especially the elderly, in the intensive care unit is necessary.

Cardiopulmonary resuscitation

The recommended dose for ventricular fibrillation/ventricular tachycardia with no pulse that is resistant to defibrillation is 300 mg (or 5 mg/kg body weight), which is given 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 administered.

Interaction

Drugs capable of causing pirouette-type ventricular tachycardia are primarily class Ia and III antiarrhythmic drugs 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 pirouette-type ventricular tachycardia are contraindicated.

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

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

– Other drugs such as bepridil, cisapride, difeminil, IV ritromycin, misolastin, IV vincamine, moxifloxacin, IV spiramycin.

– Sultopride.

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

These contraindications do not apply to the use of amiodarone for cardiopulmonary resuscitation in cases of cardiac arrest resistant to electric defibrillation.

Not recommended combinations with

Cyclosporine

Possible increased plasma levels of cyclosporine associated with decreased metabolism of the drug in the liver, with possible nephrotoxic manifestations.

Determine cyclosporine blood levels, check renal function, and revise dosage during amiodarone treatment and after drug withdrawal.

Diltiazem for injection

The risk of bradycardia and atrioventricular block. If the combination is unavoidable, strict clinical and continuous ECG monitoring should be established.

Verapamil for injection

The risk of bradycardia and atrioventricular block. If the combination is unavoidable, strict clinical and continuous ECG monitoring should be established.

Antiparasitic drugs that can cause pirouette-type tachycardia (halofantrine, pentamidine, lumefantrine)

If the combination is unavoidable, prior QT interval control and ECG monitoring is necessary.

Neuroleptics capable of causing pirouette-type ventricular tachycardia:

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

The risk of ventricular rhythm abnormalities (pirouette tachycardia) increases.

Methadone

The risk of ventricular rhythm abnormalities (pirouette tachycardia) is increased. Recommended: ECG and clinical monitoring.

Combinations requiring precautions when using Amiodarone with:

Oral anticoagulants:

Enhancement of anticoagulant effects 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 adjusting anticoagulant doses during amiodarone treatment and after drug withdrawal.

Beta-blockers, except sotalol (contraindicated combination) and esmolol (combination requiring caution in use)

Disorders of contractility, automaticity 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 risk of severe bradycardia. Increased risk of ventricular arrhythmias, especially pirouette tachycardia.

He needs regular clinical and electrocardiographic monitoring.

Cardiac glycosides

Disorders of automatism (excessive bradycardia) and atrial-ventricular conduction (synergism). When using digoxin, increased plasma concentrations (due to decreased clearance of the alkaloid).

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

Diltiazem for oral administration

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

Verapamil for oral administration

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

Esmolol

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

Hypokalemic drugs: potassium-eluting diuretics (in monotherapy or combination), stimulant laxatives, amphotericin B (IV) glucocorticoids (systemic), tetracosactide.

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

Lidocaine

The risk of increased plasma concentrations of lidocaine, with the possibility of neurological and cardiac side effects, due to the reduction of lidocaine metabolism in the liver by amiodarone. Clinical and ECG monitoring and, if necessary, adjustment of lidocaine dose during amiodarone treatment and after discontinuation.

Orlistat

The risk of decreased plasma concentrations of amiodarone and its active metabolite. Clinical and, if necessary, ECG monitoring,

Phenytoin (and, by extrapolation, fosphenytoin)

An increase in plasma phenytoin levels with symptoms of overdose, particularly neurological symptoms (decreased metabolism of phenytoin in the liver). Clinical monitoring and determination of plasma phenytoin levels; if possible, phenytoin dose reduction.

Simvastatin

An 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 at this dose it is not possible to achieve therapeutic effect, you should switch to another statin that does not interact with this type.

Tacrolimus

An increase in tacrolimus levels in blood due to inhibition of its metabolism by amiodarone. Blood tacrolimus levels should be measured, renal function should be monitored, and tacrolimus levels should be equalized.

Drugs that cause bradycardia:

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

The risk of excessive bradycardia (cumulative effect).

Combinations to consider

Drugs that cause bradycardia: Calcium channel blockers with bradycardic effects (verapamil), beta-blockers (except sotalol), clonidine, guanfacine, foxglove alkaloids, mefloquine, cholinesterase inhibitors (donepil, galantamine, rivastigmine, tacrine, ambemonium, pyridostigmine, neostigmine), pilocarpine.

The risk of excessive bradycardia (cumulative effects).

Incompatibilities

The use of PVC material or medical devices plasticized with 2-diethylhexyl phthalate (DEHP) in the presence of amiodarone injection solution may release DEHP. To minimize exposure to DEGF, it is recommended that the solution be final diluted before infusion in equipment that does not contain DEGF.

Special Instructions

– Electrolyte metabolism disorders, especially hypokalemia: it is important to take into account situations that may be accompanied by hypokalemia as predisposing to proarrhythmic phenomena. Hypokalemia must be corrected before starting amiodarone

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

With caution is used in chronic heart failure, liver failure, bronchial asthma, the elderly.

Contraindications

– sinus node weakness syndrome (SBNS), sinus bradycardia, sinoatrial block, except when corrected by an artificial pacemaker;

– atrioventricular block of II and III degree, intraventricular conduction disorders (two and three-legged Gis block); In these cases the drug may be used in specialized departments under cover of an artificial pacemaker;

– cardiogenic shock, collapse;

– severe arterial hypotension;

– concomitant use with medications capable of causing pirouette-type polymorphic ventricular tachycardia;

– Thyroid dysfunction (hypothyroidism, hyperthyroidism);

– hypokalemia;

– pregnancy;

– breastfeeding;

– hypersensitivity to iodine and/or amiodarone;

– severe pulmonary function disorders (interstitial lung disease);

– cardiomyopathy or decompensated heart failure (possible deterioration of the patient).

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

Side effects

Cardiovascular system: often – bradycardia (usually moderate heart rate slowing); BP decrease, usually moderate and transient. Cases of severe arterial hypotension or collapse have been observed in overdose or too rapid administration of the drug. Very rarely – proarrhythmogenic effect (there are reports about the occurrence 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 mainly observed when using the drug together with drugs prolonging the period of ventricular repolarization (QTc interval) or with electrolyte balance disorders (see “Interaction”). In light of the available data, it is impossible to determine whether the occurrence of these rhythm abnormalities 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 have been noted in some patients (patients with sinus node dysfunction and elderly patients), flushes of blood to the skin of the face, progression of heart failure (possible with intravenous jet injection).

Respiratory system: very rarely – cough, dyspnea, interstitial pneumonitis; bronchospasm and/or apnea in patients with severe respiratory failure, especially in patients with bronchial asthma; acute respiratory distress syndrome, sometimes with fatal outcome and sometimes immediately after surgical interventions (possible interaction with high concentrations of oxygen is assumed) (see “Special Precautions. “

Digestive system: very common – nausea. Very rarely – an isolated increase of liver transaminase activity in serum, usually moderate (1.5-3-fold excess of normal values) and reduced with dose reduction or even spontaneously. Acute liver damage (within 24 hours after administration of amiodarone) with increased transaminases and/or jaundice, including the development of liver failure, sometimes fatal (see “Cautions”).

Skin disorders: very rare – fever, increased sweating.

CNS: very rarely – benign intracranial hypertension (pseudotumor of brain), headache.

Immune system disorders: very rarely – anaphylactic shock. Unknown frequency – angioedema.

Reactions at the injection site: often – inflammatory reactions, such as superficial phlebitis, when injected directly into the peripheral vein. Reactions at the injection site, such as: pain, erythema, edema, necrosis, transudation, infiltration, inflammation, thickening, thrombophlebitis, phlebitis, cellulitis, infection, pigmentation.
Method of preparation or use:

Amiodarone (injectable form) is intended for use in cases where rapid achievement of antiarrhythmic effect is required or when oral administration of the drug is not possible.
Except for urgent clinical situations, the drug should be used only in hospital in the intensive care unit under constant ECG and BP monitoring.

When administered intravenously, the drug should not be mixed with other drugs or simultaneously administered through the same venous access.

Use only in diluted form. For dilution use only 5% dextrose (glucose) solution. Due to the peculiarities of the drug form it is not recommended to use infusion solution concentrations less than those obtained by dilution of 2 ampoules in 500 ml of 5% dextrose (glucose).

To avoid reactions at the site of administration, amiodarone should be administered through the central venous catheter, except in cardiac resuscitation in ventricular fibrillation resistant to cardioversion, when (in the absence of central venous access) the peripheral veins (the largest peripheral vein with maximum blood flow) can be used to administer the drug.
Severe cardiac rhythm disturbances when oral administration is not possible (except for cardiac resuscitation in cardiac arrest caused by ventricular fibrillation resistant to cardioversion)

Overdose

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

Treatment: symptomatic therapy (in bradycardia – beta-adrenergic pacemakers or pacemaker placement, in “pirouette” tachycardia – intravenous administration of magnesium salts, pacing pacing). Amiodarone and its metabolites are not eliminated by hemodialysis and peritoneal dialysis.

Similarities