Description
Latin name
AMIODARONE
Release form
Concentrate for solution for iv administration in the form of a clear, with a yellowish or greenish tint of liquid.
Pharmacological action
Antianginal, antiarrhythmic.
Contraindications
– sinus node weakness syndrome (SSS), sinus bradycardia, sinoatrial block, with the exception of cases of correction by an artificial pacemaker
– atrioventricular block II and III degree, intraventricular conduction disturbances (these are two cases) the drug can be used in specialized departments under the cover of an artificial pacemaker (pacemaker)
– cardiogenic shock, collapse
– pronounced arterial I hypotension
– simultaneous application of drugs capable of causing polymorphic ventricular tachycardia type “pirouetteВ»
– thyroid dysfunction (hypothyroidism, hyperthyroidism)
– hypokalemia
– pregnancy
– breastfeeding
– increased sensitivity to iodine and / or amiodarone
– severe pulmonary dysfunction (interstitial lung disease)
– cardiomyopathy or decompensated heart failure (possibly heart failure).
Due to the presence of benzyl alcohol, Amiodarone is contraindicated in newborns, infants, and children under 3 years of age.
Pregnancy and lactation
Animal tests have not revealed teratogenic effects of amiodarone. Therefore, one should not expect malformations in humans, since it has been shown that drug-causing malformations exhibit teratogenic effects in animals in correctly conducted experiments on two different animal species.
In clinical practice, the currently available information is insufficient to assess whether amiodarone causes malformations when used in the first trimester of pregnancy. Since the thyroid gland of the fetus begins to bind iodine only from the 14th week of pregnancy, the effect of the drug on it is not expected in case of earlier use. An excess of iodine when using the drug after this period can lead to laboratory signs of hypothyroidism in the fetus or even to clinical goiter.
The drug is contraindicated since the second trimester of pregnancy.
Amiodarone, its metabolite and iodine are excreted in breast milk at concentrations exceeding the level in maternal plasma. If the mother receives treatment with this drug, breast-feeding is contraindicated in connection with the danger of developing hypothyroidism in the child.
Influence on the ability to drive vehicles and control mechanisms
There is currently no evidence that amiodarone affects the ability to drive vehicles and control mechanisms.
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 the start of the use of amiodarone
– Except in cases of emergency therapy, Amiodarone in the form of a solution for intravenous injection can be used only in a hospital and with constant monitoring (ECG, blood pressure).
Use with caution in chronic heart failure, liver failure, bronchial asthma, in old age.
Composition of
1 ampoule (3 ml of solution) contains:
active ingredient: amiodarone hydrochloride – 150 mg
excipients: sodium acetate trihydrate, glacial acetic acid, polysorbate 80, benzyl alcohol, water for injection.
Dosage and Administration
Dosage and Administration – Intravenous.
Do not dilute the drug with isotonic sodium chloride solution, as precipitate formation is possible!
Do not mix with other medicines in the same infusion system.
The drug should be used only when there is the necessary equipment for monitoring cardiac function, defibrillation and cardiac pacing.
The drug can be used before cardioversion with direct current.
The standard recommended dose is 5 mg / kg body weight, which is administered by infusion over a period of time from 20 minutes to 2 hours. The drug may be administered as a solution, diluted in 250 ml of 5% glucose solution. After this, repeated infusion of the drug in a dose of up to 1200 mg (approximately 15 mg / kg body weight) in a 5% glucose solution up to 500 ml in volume for 24 hours can be applied, while the infusion rate must be adjusted depending on the clinical response of the patient ( see Precautions).
In extremely urgent clinical situations, the medicine, 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 this, the repeated administration of the drug can be carried out no earlier than 15 minutes. Patients who are injected with the drug in the above manner must be carefully monitored – for example, in the intensive care unit (see section “Precautions”).
Transition from intravenous administration to oral administration of
Immediately after receiving the appropriate response to treatment, it is necessary to start oral drug therapy at the usual loading dose (i.e. 200 mg three times a day). After this, the drug should be gradually withdrawn by incremental dose reduction.
Children
The safety and effectiveness of amiodarone in children have not been evaluated, therefore the use of this medicine is not recommended for children. The drug contains benzyl alcohol. There are reports of deaths resulting from the development of “dyspnea syndrome” (“gasping syndrome”) in newborns after administration of solutions containing this preservative. Symptoms of this complication include the sudden onset of shortness of breath, arterial 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 in favor of specific drug 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. Particular attention should be paid to monitoring thyroid function (see sections “Contraindications”, “Precautions” and “Undesirable reactions”).
Patients with renal and / or liver failure
Although that dose adjustment for patients with renal or hepatic impairment during prolonged oral administration of amiodarone was not required, careful clinical monitoring of patients of this category, especially the elderly, in the intensive care unit is necessary.
Cardiopulmonary resuscitation
The recommended dose for ventricular fibrillation / ventricular tachycardia with no defibrillation-resistant pulse is 300 mg (or 5 mg / kg body weight), which is administered in 20 ml diluted 5% glucose solution by rapid injection. If ventricular fibrillation persists, an additional 150 mg (or 2.5 mg / kg body weight) of the drug can be used.
Side effects of
From the cardiovascular system: often – bradycardia (usually a moderate decrease in heart rate) decrease in blood pressure, usually moderate and transient. Cases of severe arterial hypotension or collapse were observed with an overdose or too rapid administration of the drug. Very rarely – proarrhythmogenic effect (there are reports of 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 observed mainly in cases where the drug is used in conjunction with drugs that extend the period of repolarization of the ventricles of the heart (QTc interval) or in violation of electrolyte balance (see “Interaction”). In the light of the available data, it is impossible to determine whether the occurrence of these rhythm disturbances is caused by amiodarone, or is associated with the severity of cardiac pathology, or is a consequence of treatment failure. Severe bradycardia or in exceptional cases, a stop of the sinus node, which was noted in some patients (patients with sinus node dysfunction and elderly patients), flushing of the face, progression of heart failure (possibly with intravenous jet administration).
From the respiratory system: very rarely – cough, shortness of breath, interstitial pneumonitis, bronchospasm and / or apnea in patients with severe respiratory failure, especially in patients with bronchial asthma, acute respiratory distress syndrome, sometimes fatal and sometimes immediately after surgery (it is possible to interact with high concentrations oxygen) (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-fold excess of normal values) and decreases with a decrease in dose or even spontaneously. Acute liver damage (within 24 hours after the administration of amiodarone) with an increase in 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 side of the central nervous system: very rarely – benign intracranial hypertension (pseudotumor of the brain), headache.
Disorders of the immune system: 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, induration, thrombophlebitis, phlebitis, cellulitis, infection, pigmentation.
Method of preparation or use:
Amiodarone (injection) is intended for use in cases when it is required to quickly achieve an antiarrhythmic effect 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.
In case of iv administration, the drug should not be mixed with other drugs or at the same time administered other drugs through the same venous access.
Use only in diluted form. For dilution, only 5% dextrose (glucose) solution should be used. Due to the peculiarities of the dosage form of the drug, it is not recommended to use the concentration of the infusion solution, 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 cardioreanimation in ventricular fibrillation resistant to cardioversion, when (in the absence of a central venous access) peripheral veins (the largest peripheral vein with maximum blood flow) can be used to administer the drug.
Severe heart rhythm disturbances in cases when the drug cannot be taken orally (except for cases of cardiac resuscitation with cardiac arrest caused by ventricular fibrillation resistant to cardioversion)
Drug interactions
Drugs that can cause ventricular tachycardia of the pirouette type are primarily antiarrhythmic drugs Ia and III class and some antipsychotics. Hypokalemia is a predisposing factor, as is bradycardia or congenital or acquired lengthening 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, cisapride, difemanil, iv rithromycin, misolastin, iv vincamine, moxifloxacin, iv spiramycin.
– Sultopridom.
Increased risk of ventricular rhythm disturbances (pirouette type tachycardia).
These contraindications do not apply to the use of amiodarone for cardiopulmonary resuscitation in case of cardiac arrest resistant to electrical defibrillation.
Not recommended combinations with
Cyclosporine
Possible increase in plasma cyclosporine levels associated with a decrease in the metabolism of the drug in the liver, with possible nephrotoxic manifestations.
Determination of the level of cyclosporine in the blood, check of renal function and review of dosage during treatment with amiodarone and after drug withdrawal.
Diltiazem for injection
Risk of bradycardia and atrioventricular block. If a combination is unavoidable, it is necessary to establish strict clinical and continuous ECG monitoring.
Verapamil for injection
Risk of bradycardia and atrioventricular block. If a combination is unavoidable, it is necessary to establish strict clinical and continuous ECG monitoring.
Antiparasitic drugs that can cause pirouette type tachycardia (halofantrine, pentamidine, lumefantrine)
If a combination is unavoidable, preliminary monitoring of the QT interval and ECG monitoring are necessary.
Antipsychotics capable of inducing ventricular tachycardia of the pirouette type:
Some phenothiazine antipsychotics (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, triptyride, tyripideones (droperidol, haloperidol), other antipsychotics (pimozide).
Increased risk of ventricular rhythm disturbances (pirouette type tachycardia).
Methadone
Increased risk of ventricular rhythm disturbances (pirouette type tachycardia). Recommended: ECG and clinical observation.
Combinations requiring precautions when using Amiodarone with:
Oral anticoagulants:
Enhanced anticoagulant effect and risk of bleeding due to increased plasma anticoagulant concentration. The need for more frequent monitoring of the level of prothrombin in the blood and MHO (INR), as well as the adaptation of doses of anticoagulants during treatment with amiodarone and after discontinuation of the drug.
Beta-blockers, with the exception of sotalol (a contraindicated combination) and esmolol (a combination of requiring caution when applying)
Violations of contractility, automatism and conduction (suppression of compensatory sympathetic mechanisms). Clinical and ECG monitoring.
Beta-blockers prescribed for heart failure (bisoprolol, carvedilol, metoprolol)
Violations of contractility and conduction (synergistic effect) with a risk of severe bradycardia. Increased risk of ventricular arrhythmias, especially pirouette type tachycardia.
Regular clinical and electrocardiographic monitoring is required.
Cardiac glycosides
Disorders of automatism (excessive bradycardia) and atrioventricular conduction (synergistic action). When using digoxin, an increase in its concentration in plasma (due to a decrease in alkaloid clearance).
It is necessary to carry out clinical and ECG monitoring, as well as determining the level of digoxin in plasma), 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
Violations of contractility, automatism and conduction (suppression of compensatory sympathetic mechanisms). Clinical and ECG monitoring.
Hypokalemic drugs: potassium-excreting diuretics (monotherapy or combination), stimulant laxatives, amphotericin B (iv) glucocorticoids (systemic), tetracosactide.
Increased risk of ventricular rhythm disturbances, especially pirouette type tachycardia (hypokalemia is a predisposing factor). Clinical and ECG monitoring, laboratory tests.
Lidocaine
The risk of an increase in plasma lidocaine concentration, with the likelihood of neurological and cardiological side effects, due to a decrease in amiodarone metabolism of lidocaine in the liver. Clinical and ECG control, if necessary, dose adjustment of lidocaine during treatment with amiodarone and after its cancellation.
Orlistat
Risk of decreased plasma concentrations of amiodarone and its active metabolite. Clinical and, if necessary, ECG monitoring,
Phenytoin (and, by extrapolation, phosphenytoin)
Increased plasma phenytoin levels with symptoms of an overdose, especially of a neurological nature (decreased phenytoin metabolism in the liver). Clinical monitoring and determination of the level of phenytoin in plasma, if possible – a reduction in the dose of phenytoin.
simvastatin
Increased risk of side effects (dose-related) 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 the therapeutic effect cannot be achieved, you should switch to another statin that does not enter into interactions of this type.
Tacrolimus
An increase in blood tacrolimus levels due to inhibition of its metabolism by amiodarone. It is necessary to measure the level of tacrolimus in the blood, monitor the functioning of the kidneys and level the level of tacrolimus.
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 preparations, pilocarpine, and anticholinesterase agents.
Risk of excessive bradycardia (cumulative effect).
Combinations to be taken into account
Bradycardia-causing drugs: calcium channel blockers with a bradycardic effect (verapamil), beta-blockers (except sotalol), clonidine, guanfacine, digitalis alkaloids, digitalis alkaloids, gallinamines, cholinesterans, and cholinergic drugs tacrine, ambemonium, pyridostigmine, neostigmine), pilocarpine.
Risk of excessive bradycardia (cumulative effects).
Incompatibilities
When using PVC material or medical equipment, plasticized with 2-diethylhexylphthalate (DEHP) in the presence of an injection solution of amiodarone, DEHP can be released. For minimal exposure to DEHP, it is recommended that the final dilution of the solution be performed before infusion in equipment that does not contain DEHP.
overdose
Symptoms: sinus bradycardia, cardiac arrest, paroxysmal ventricular tachycardia, pirouette ventricular tachycardia, circulatory disorders, impaired liver function, decreased blood pressure.
Treatment: carry out symptomatic therapy (for bradycardia – beta-adrenostimulators or pacemaker installation, for tachycardia type “pirouette” – intravenous administration of magnesium salts, which regulates cardiac stimulation). Amiodarone and its metabolites are not removed during hemodialysis and peritoneal dialysis.
Storage Conditions
Protected from light, at a temperature of 15 C to 25 C.
Keep out of the reach and sight of children.
Shelf life
2 years. Do not use after expiration date.
Deystvuyushtee substance
Amiodarone
Terms and conditions
For prescription
dosage form
infusion solution
Prescribing
Prescribing
For adults, For adults prescribed by a doctor
Borisov factory, Belarus
