Amiodarone
BPMP
1383 Items
2019-09-19
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Clinical Pharmacology
Antianginal, antiarrhythmic.
Indications
Relief of paroxysmal tachycardia: ventricular, supraventricular, with a high frequency of ventricular contraction (especially with WPW syndrome).
Relief of paroxysmal and stable tachysystolic forms of atrial fibrillation and atrial flutter.
Cardioreanimation at cardiac arrest caused by ventricular fibrillation resistant to cardioversion.
Composition
1 amp (3 ml) - amiodarone hydrochloride 150 mg.
Excipients: sodium acetate trihydrate - 3 mg, glacial acetic acid - 0.02211 ml, acetic acid solution 10% 1M - to pH 3.5, polysorbate 80 (twin 80) - 300 mg, benzyl alcohol - 60 mg, water d / and - up to 3 ml.
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Dosage and Administration
Due to the characteristics of the medicinal form of the drug, it is impossible to use a concentration of less than 2 vials per 500 ml, only isotonic glucose solution is used. Do not add to the infusion solution other drugs.
Amiodarone should be injected into the central vein, except in cases of cardiopulmonary resuscitation with cardiac arrest, when, in the absence of central venous access, peripheral veins can be used (see “Precautions”).
It is prescribed for serious arrhythmias, in which the use of oral medications is not possible, with the exception of cardiopulmonary resuscitation for cardiac arrest caused by refractory ventricular fibrillation.
Infusion into the central vein
Initial dose: usually 5 mg / kg, in a glucose solution (if possible using an infusomat), for from 20 minutes to 2 hours; The infusion can be repeated 2-3 times within 24 hours. The short-term action of the drug requires continued administration.
Maintenance treatment: 10–20 mg / kg per day (on average, 600–800 mg / day and up to 1200 mg / day) in 250 ml of glucose solution for several days. From the first day of infusion begin a gradual transition to oral administration (3 pills per day). The dose can be increased to 4 or even 5 pills per day.
Infusion into the peripheral vein under conditions of cardiopulmonary resuscitation for cardiac arrest caused by ventricular fibrillation refractory to electrical defibrillation.
Given the mode of application and the situation in which this indication occurs, the use of a central venous catheter is recommended, if available; otherwise, the drug may be injected into the largest peripheral vein.
The initial intravenous dose is 300 mg (or 5 mg / kg), after dilution in 20 ml of 5% glucose solution. Introduced jet.
If fibrillation is not stopped, additional intravenous administration of 150 mg (or 2.5 mg / kg) is used.
You can not mix in the same syringe with other drugs!
Adverse reactions
Since 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 action (there are reports of the emergence of new arrhythmias and including polymorphic ventricular tachycardia of the "pirouette" type, or exacerbation of existing ones - in some cases with subsequent cardiac arrest). These effects are observed mainly in cases of drug use together with drugs that prolong the period of repolarization of the ventricles of the heart (QTc interval) or in case of electrolyte imbalance (see "Interaction"). In 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 disease, or is a consequence of treatment failure. Severe bradycardia or in exceptional cases, sinus node arrest, which was observed in some patients (patients with sinus dysfunction and elderly patients), blood flushes to the skin of the face, progression of heart failure (possibly with intravenous injection).
On the part of 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 surgical interventions (it is assumed the possibility of interaction with high oxygen concentrations) (see. "Special instructions").
On the part of 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 decreasing with decreasing dose or even spontaneously. Acute liver damage (within 24 hours after administration of amiodarone) with an increase in transaminases and / or jaundice, including the development of liver failure, sometimes fatal (see "Special Instructions").
On the part of the skin: very rarely - feeling hot, sweating.
From the side of the central nervous system: very rarely - benign intracranial hypertension (brain pseudotumor), headache.
Immune system disorders: very rarely - anaphylactic shock. Unknown frequency - angioedema.
Reactions at the injection site: often - inflammatory reactions, such as superficial phlebitis, when administered directly into the peripheral vein. Reactions at the injection site, such as: pain, erythema, edema, necrosis, extravasation, infiltration, inflammation, induration, thrombophlebitis, phlebitis, cellulitis, infection, pigmentation.
Method of preparation or use:
Amiodarone (injectable form) is intended for use in cases where it is necessary to quickly achieve an antiarrhythmic effect or to use the drug orally.
With the exception of urgent clinical situations, the drug should be used only in a hospital in the intensive care unit under the constant supervision of ECG and blood pressure.
With the on / in the introduction of the drug can not be mixed with other drugs or simultaneously enter other drugs through the same venous access.
Use only in diluted form. For dilution, use only 5% dextrose (glucose) solution. Due to the characteristics of the medicinal form of the drug, it is not recommended to use the concentration of the infusion solution, which is less than that obtained at a dilution of 2 amp. in 500 ml of 5% dextrose (glucose).
In order to avoid reactions at the injection site, amiodarone should be administered through the central venous catheter, except in cases of cardio-resuscitation in ventricular fibrillation resistant to cardioversion, when (in the absence of central venous access) peripheral veins can be used (the largest peripheral vein with maximum blood flow ).
Severe violations of the heart rhythm in cases where it is impossible to take the drug inside (except in cases of cardio-resuscitation with cardiac arrest caused by ventricular fibrillation resistant to cardioversion)
Contraindications
Hypersensitivity (including to iodine), SSS (sinus bradycardia, SA blockade) in the absence of a pacemaker, violation of intraventricular conduction (two-, three-beam blockade) in the absence of a pacemaker, AV blockade II-III Art. (Without pacemaker), cardiogenic shock, hypokalemia, hypomagnesemia, collapse, marked hypotension, hypothyroidism, hyperthyroidism, congenital or acquired lengthening QT interval, simultaneous reception PM prolonging QT interval and causing paroxysmal tachycardia (including type of polymorphic ventricular "pirouette"), pregnancy, lactation, age up to 18 years.
When cardioreanimation is performed when cardiac arrest caused by ventricular fibrillation resistant to cardioversion, there are no absolute contraindications.
Drug interactions
Drugs that can cause ventricular tachycardia of the "pirouette" type are primarily class Ia and class III antiarrhythmic drugs 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 such as "pirouette."
- Antiarrhythmic drugs of class Ia (quinidine, hydroquinidine, isopyramide).
- Antiarrhythmic drugs of class III (dofetilide, ibutilid, sotalol).
- Other drugs, such as bepridil, cisapride, difemanil, IV rithromycin, mizolastin, IV vincamine, moxifloxacin, IV spiramycin.
- Sultopride.
The risk of ventricular rhythm disorders (pirouette tachycardias) 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
Cyclosporin
Plasma cyclosporine may be elevated due to a decrease in drug metabolism in the liver, with possible nephrotoxic manifestations.
Determining the level of cyclosporine in the blood, checking kidney function and revising the dosage during the period of treatment with amiodarone and after drug withdrawal
Diltiazem for injection
Risk of bradycardia and atrioventricular block. If the combination is unavoidable, it is necessary to establish strict clinical and permanent ECG monitoring.
Verapamil for injection
Risk of bradycardia and atrioventricular block. If the combination is unavoidable, it is necessary to establish strict clinical and permanent ECG monitoring.
Antiparasitic drugs that can cause tachycardia such as "pirouette" (halofantrine, pentamidine, lumefantrin)
If the combination is unavoidable, preliminary monitoring of the QT interval and ECG monitoring are necessary.
Neuroleptics that can cause ventricular tachycardia such as "pirouette":
Some phenothiazine antipsychotics (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, Tiapride, veraliprid), butyrophenones (droperidol, haloperidol), other neuroprotephants, neuropropets, other neuropropets, and other neuropropets.
The risk of ventricular rhythm disorders (pirouette tachycardias) increases.
Methadone
The risk of ventricular rhythm disorders (pirouette tachycardias) increases. Recommended: ECG and clinical observation.
Combinations requiring precautions when applying Amiodarone with:
Oral anticoagulants:
Increased anticoagulant effect and the risk of bleeding, due to the increased concentration of anticoagulants in the plasma. 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 the period of treatment with amiodarone and after discontinuation of the drug.
Beta-blockers, with the exception of sotalol (a contraindicated combination) and esmolol (a combination 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 conductivity (synergistic effect) with the risk of severe bradycardia. Increased risk of ventricular arrhythmias, especially pirouette tachycardias.
Regular clinical and electrocardiographic monitoring is required.
Cardiac glycosides
Disorders 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).
It is necessary to carry out clinical and ECG monitoring, as well as determination of 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 control.
Verapamil for oral administration
Risk of bradycardia and atrioventricular block, especially in the elderly. Clinical and ECG control.
Esmolol
Violations of contractility, automatism and conduction (suppression of compensatory sympathetic mechanisms). Clinical and ECG monitoring.
Hypokalemic drugs: potassium-withdrawing diuretics (in monotherapy or combination), stimulant laxatives, amphotericin B (w / w) glucocorticoids (systemic), tetracosactide.
The risk of ventricular rhythm disturbances increases, especially pirouette tachycardias (hypokalemia is a predisposing factor). Clinical and ECG monitoring, laboratory tests.
Lidocaine
The risk of increased lidocaine concentration in plasma, with the likelihood of neurological and cardiac side effects, due to a decrease in amidarone lidocaine metabolism in the liver. Clinical and ECG control, if necessary, correction of the dose of lidocaine during treatment with amiodarone and after its withdrawal.
Orlistat
The risk of reducing the concentration of amiodarone and its active metabolite in plasma. Clinical and, if necessary, ECG control,
Phenytoin (and, by extrapolation, fosfenitoin)
Phenytoin levels increase in plasma with symptoms of overdose, especially of a neurological nature (decrease in the metabolism of phenytoin in the liver). Clinical monitoring and determination of plasma phenytoin levels; if possible, reduce the dose of phenytoin.
Simvastatin
Increased risk of side effects (dose-dependent) type of rhabdomyolysis (decrease in the 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 a therapeutic effect, one should switch to another statin that does not enter into this type of interaction.
Tacrolimus
Increased blood tacrolimus due to inhibition of its metabolism by amiodarone. Blood tacrolimus, kidney function and leveling of tacrolimus should be measured.
Drugs that cause bradycardia:
Many drugs can cause bradycardia. This is especially true of class Ia antiarrhythmic drugs, beta-blockers, some class III antiarrhythmic drugs, some calcium channel blockers, digitalis drugs, pilocarpine, and anticholinesterase agents.
Risk of excessive bradycardia (cumulative effect).
Combinations to be taken into account
Drugs that cause bradycardia: calcium channel blockers with bradycardic effect (verapamil); pilocarpine.
Risk of excessive bradycardia (cumulative effects).
Incompatibility
When using material or medical equipment made of PVC plasticized with 2-diethylhexyl phthalate (DEHP) in the presence of an amiodarone injection solution, DEHP can be released. For minimal exposure to DEHP, it is recommended to carry out the final dilution of the solution before pouring it into equipment that does not contain DEHP.
Pregnancy and Lactation
Tests on animals did not reveal the teratogenic action of Amiodarone. Consequently, one should not expect malformations in humans, since it has been shown that inducing malformations medicinal substances exhibit teratogenic effects in animals in properly conducted experiments on two different types of animals.
In clinical practice, currently available information is insufficient to assess whether amiodarone causes malformations when applied 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 in the case of earlier use is not expected. Excess iodine when using the drug after this period can lead to laboratory signs of hypothyroidism in the fetus or even clinical goiter.
The drug is contraindicated, starting from the second trimester of pregnancy.
Amiodarone, its metabolite and iodine are excreted into breast milk at concentrations higher than the level in the maternal plasma. If the mother receives treatment with this drug, breastfeeding is contraindicated due to the risk of hypothyroidism in the child.
Influence on ability to drive motor transport and control mechanisms
At present, there is 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 adjusted before the start of amiodarone
- Except in cases of emergency treatment, Amiodarone in the form of a solution for intravenous injection can be used only in the hospital and with constant monitoring (ECG, blood pressure).
With caution used in chronic heart failure, liver failure, bronchial asthma, in old age.
Overdosage
Symptoms: sinus bradycardia, cardiac arrest, paroxysmal ventricular tachycardia, ventricular tachycardia of the "pirouette" type, circulatory disorders, abnormal liver function, decreased blood pressure.
Treatment: conduct symptomatic therapy (for bradycardia - beta-adrenostimulyatory or installing a pacemaker, with tachycardia type "pirouette" - intravenous administration of magnesium salts, reducing cardiac stimulation). Amiodarone and its metabolites are not removed during hemodialysis and peritoneal dialysis.
- Brand name: Amiodarone
- Active ingredient: Amiodarone
- Dosage form: Concentrate for preparing solution for intravenous injection in the form of a transparent, yellowish or greenish shade of liquid.
- Manufacturer: Borisov plant
- Country of Origin: Belarus
Studies and clinical trials of Amiodarone (Click to expand)
- Unusual interference from primary collection tube in a high-performance liquid chromatography assay of amiodarone
- Effect of amiodarone (AMD) on the antioxidant enzymes, lipid peroxidation and mitochondrial metabolism
- Neutrality of amiodarone on the initiation and propagation of membrane lipid peroxidation
- Evaluation of reactive oxygen species involvement in amiodarone pulmonary toxicity in vivo and in vitro
- Acute alveolar hemorrhage and orthodeoxia induced by intravenous amiodarone
- Early prenatal management of a fetal ventricular tachycardia treated in utero by amiodarone with long term follow-up
- Characterization of amiodarone metabolites and impurities using liquid chromatography/atmospheric pressure chemical ionization mass spectrometry
- Synthesis of Two Metabolites of the Antiarrythmicum Amiodarone
- Acetazolamide-responsive periodic ataxia induced by amiodarone
- Unexplained bone marrow granulomas: Is amiodarone the culprit? A report of 2 cases
- Parkinsonism and amiodarone therapy
- Amiodarone and desethylamiodarone elimination kinetics following withdrawal of long-term amiodarone maintenance therapy
- Amiodarone pharmacokinetics. II. Disposition kinetics following subchronic administration in rat
- Pharmacokinetic interaction between diltiazem and amiodarone in the dog
- Pharmacokinetics of Amiodarone in hyperlipidemic and simulated high fat-meal rat models
- Pharmacokinetics of desethylamiodarone in the rat after its administration as the preformed metabolite, and after administration of amiodarone
- Amiodarone modulates pharmacokinetics of low-dose methotrexate in rats
- Effects of neferine on the pharmacokinetics of amiodarone in rats
- A liquid chromatography-mass spectrometry method for nicotine and cotinine; utility in screening tobacco exposure in patients taking amiodarone
- A liquid chromatography–mass spectrometry assay method for simultaneous determination of amiodarone and desethylamiodarone in rat specimens
- High-performance liquid chromatographic isolation and fast atom bombardment mass spectrometric identification of di-N-desethylamiodarone, a new metabolite of amiodarone in the dog
- Effect of amiodarone on Na+-, K+-ATPase and Mg2+-ATPase activities in rat brain synaptosomes
- Synthesis of Two Metabolites (Ib) and (Ic) of the Antiarrythmicum Amiodarone (Ia).
- Catalytic Adsorptive Stripping Voltammetry at a Carbon Paste Electrode for the Determination of Amiodarone
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