Last Updated on February 19, 2017 by Dr.Derek Fhisher
Most popular brand: Cardarone
Active ingredient: Amiodarone
Available dosage forms: 200 mg
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Amiodarone general information
Ask your wellbeing care provider any questions which may have regarding just how to utilize Cordarone. Call your physician for medical advice regarding side effects. Don’t utilize amiodarone without telling your doctor should you be pregnant. Use Cordarone as instructed by your doctor.
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Amiodarone – instructions for use, analogs, reviews and release form (tablets 200 mg injections in vials for injection 5%) of the drug for the treatment of arrhythmias and extrasystoles in adults, children and in pregnancy. Composition and alcohol
In this article, you can read the instructions for use of the drug Amiodarone. Presents reviews of visitors – users of the drug, as well as opinions of doctors skilled in the use of amiodarone in their practice. Most requested actively add their own reviews of the preparation: helped or did not help to get rid of the medicine from the disease, which were observed complications and side effects may not be claimed by the manufacturer in the summary. Analogs of amiodarone in the presence of the available structural analogues. Use for the treatment of arrhythmias and extrasystoles in adults, children, and during pregnancy and breastfeeding. The composition and interaction of the drug with alcohol.
Amiodarone – Class 3 antiarrhythmic drug, has anti-anginal activity.
The antiarrhythmic effect is associated with the ability to increase the duration of action potential of cardiomyocytes and effective refractory period of atrial, ventricular, the AV node, the bundle of His, Purkinje fibers. This is accompanied by a decrease in sinus automatism, slowing AV – conduction, decreased excitability of cardiomyocytes. It is believed that the mechanism of prolonging the action potential is associated with the blockade of potassium channels (reduced excretion of potassium ions from the cardiomyocytes). By blocking the inactivated “fast” sodium channels, it has effects that are typical of class 1 antiarrhythmic agents. Hinders slow (diastolic) depolarization of the membrane of the sinus node cells, causing bradycardia, depresses AV conducting (4 antiarrhythmics class effect).
Antianginal effect is due koronarorasshiryayuschee and antiadrenergicheskim action, decrease myocardial oxygen demand. It has an inhibitory effect on alpha – and beta – adrenergic receptors of the cardio – vascular system (without their complete blockade). It reduces sensitivity to hyperstimulation of the sympathetic nervous system, the tone of the coronary vessels; increase coronary blood flow; slows heart rate; It increases the energy reserves of the myocardium (by increasing the content kreatinsulfata, adenosine and glycogen). It reduces peripheral vascular resistance and systemic blood pressure (when administered intravenously).
is believed to amiodarone may increase the level of phospholipids in tissues.
It contains iodine. It influences the metabolism of thyroid hormone, inhibits the conversion of T3 to T4 (thyroxine blockade – 5 – deiodinase) and blocks the capture of these hormones cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium (T3 deficiency may lead to overproduction and thyrotoxicosis) .
When administered onset of action – from 2 – 3 days to 2 – 3 months, the duration of action and is variable – from a few weeks to several months.
After intravenous administration of the maximum effect is achieved within 1 – 30 minutes and lasts for 1 – 3 hours.
Amiodarone hydrochloride + auxiliaries.
Once inside slowly absorbed from the gastrointestinal tract, absorption is 20 – 55%. Penetrates through the blood-brain barrier (BBB) and the placenta (10 – 50%) is excreted in breast milk (25% of the dose received by the mother). Intensively metabolized in the liver to the active metabolite desetilamiodarona, as well as on – apparently, by deiodination. In long-term treatment of iodine concentrations may reach 60 – 80% concentration of amiodarone. It is an inhibitor of isoenzymes CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver. Write mainly in the bile through the intestines, small enterohepatic recirculation may occur. In very small amounts of amiodarone and desetilamiodaron excreted in the urine. Amiodarone and its metabolites are not displayed during dialysis.
- life-threatening ventricular arrhythmia (including ventricular tachycardia);
- prevention of ventricular fibrillation (including after cardioversion);
- supraventricular arrhythmias (usually with inefficiency or inability to other therapies, especially those associated with WPW syndrome), including: paroxysm of atrial fibrillation and atrial flutter;
- atrial and ventricular premature beats;
- fibrillation on a background of coronary artery disease or congestive heart failure;
- ventricular arrhythmias in patients with Chagas myocarditis;
Tablets 200 mg.
A solution for intravenous administration of 5% (injections in vials for injection).
Instructions for use and dosage
When administered to adult initial single dose of 200 mg. For children, the dose is 2.5 – 10 mg per day. The scheme and the duration of treatment is determined individually.
For intravenous (bolus or infusion (a drip)) single dose of 5 mg / kg, daily dose – and 1.2 g (15 mg / kg).
- sinus bradycardia (refractory to m – holinoblokatoram);
- AV blockade;
- the progression of heart failure;
- ventricular arrhythmias such as “pirouette”;
- strengthening of existing arrhythmias or its origin;
- BP reduction;
- the development of hypo – or hyperthyroidism;
- shortness of breath;
- interstitial pneumonitis or alveolitis;
- pulmonary fibrosis;
- apnea (in patients with severe respiratory failure);
- nausea, vomiting;
- loss of appetite;
- dulling or loss of taste;
- a feeling of heaviness in the epigastric;
- abdominal pain;
- constipation, diarrhea;
- toxic hepatitis;
- a sense of fatigue;
- auditory hallucinations;
- peripheral neuropathy;
- memory impairment, sleep;
- optic neuritis;
- intracranial hypertension;
- deposition of lipofuscin in the corneal epithelium (if the deposits are large and partially fill the pupil – a complaint at the luminous point or a veil before the eyes in bright light);
- mikrootsloyka retina;
- hemolytic and aplastic anemia;
- skin rash;
- exfoliative dermatitis;
- gray – blue color of the skin;
- reduced potency;
- sinus bradycardia;
- sick sinus syndrome (SSS);
- sinoatrial block;
- AV block 2 – 3 degrees (without pacemaker);
- cardiogenic shock;
- interstitial lung disease;
- MAO inhibitors;
- Hypersensitivity to amiodarone and iodine.
Application of pregnancy and breastfeeding
Do not use this during pregnancy and lactation.
Amiodarone and desmetilamiodaron cross the placental barrier, their concentration in the blood of the fetus, are respectively 10% and 25% of the concentration in maternal blood.
Amiodarone and desmetilamiodaron excreted in breast milk.
Use in children
C care to apply at the age of 18 years (effectiveness and safety have not been established).
Use in elderly patients
C caution in elderly patients (high risk of severe bradycardia).
It should not be used in patients with severe respiratory failure.
Before starting amiodarone should conduct X-ray examination of the lungs and thyroid function, if necessary, to carry out the correction of electrolyte abnormalities.
With long-term treatment requires regular monitoring of thyroid function, consult an ophthalmologist and X-ray light.
Parenteral can only be used in specialized departments of hospitals under the constant control of blood pressure, heart rate and ECG.
Patients receiving amiodarone, should avoid direct exposure to sunlight.
When the abolition of amiodarone possible recurrences of heart rhythm disorders.
It may affect the test results of accumulation of radioactive iodine in the thyroid gland.
It should not be used concurrently with amiodarone, quinidine, beta – blockers, calcium channel blockers, digoxin, coumarin, doxepin.
Drug interactions with other drugs amiodarone maybe even a few months after the end of its application due to a long half-life.
With the simultaneous use of amiodarone and antiarrhythmic agents of class 1A (including disopyramide) increases the QT interval due to the additive effect on its value and increases the risk of ventricular tachycardia type “pirouette”.
With the simultaneous use of amiodarone with laxatives, which can cause hypokalemia, increased risk of ventricular arrhythmias.
The means cause hypokalemia, including diuretics, corticosteroids, amphotericin B (w / w), tetrakozaktid while the use of amiodarone cause an increase in the QT interval and increased risk of ventricular arrhythmia (including type “pirouette”).
With simultaneous use of funds for general anesthesia, oxygen therapy the risk of bradycardia, hypotension, conduction disturbances, reducing the stroke volume of the heart, which, in – apparently due to additive cardiodepressive and vasodilating effects.
With simultaneous use of tricyclic antidepressants, phenothiazines, astemizole, terfenadine cause an increase in the QT interval and increased risk of ventricular arrhythmias, especially type “pirouette”.
With the simultaneous use of warfarin, fenprokumona, atsenokumarola enhanced anticoagulant effect and increased risk of bleeding.
In an application vincamine, sultopride, erythromycin (iv), pentamidine (intravenous, intramuscular) increases the risk of ventricular arrhythmias such as “pirouette”.
In an application may increase the concentration of dextromethorphan in the plasma due to the reduction of its rate of metabolism in the liver that is caused by inhibition of the CYP2D6 isoenzyme of cytochrome P450 under the influence of amiodarone and slower elimination of dextromethorphan from the body.
With the simultaneous use of digoxin significantly increased digoxin plasma concentration by reducing its clearance and, consequently, increases the risk of digitalis intoxication.
With the simultaneous use of diltiazem, verapamil amplified negative inotropic effect, bradycardia, conduction disturbances, AV – blockade.
A case of amiodarone increase plasma concentrations when an application with indinavir. It is believed that ritonavir, nelfinavir, saquinavir will have a similar effect.
In an application kolestiramina amiodarone reduced plasma concentration due to its binding to kolestiraminom and reduce absorption from the digestive tract.
There are reports of increased lidocaine plasma concentrations while the use of amiodarone and the development of seizures, in – apparently due to inhibition of metabolism of lidocaine under the influence of amiodarone.
It is undesirable joint use of amiodarone with alcohol and ethanol-containing products.
It is believed that the possible synergies with the inhibitory action on the sinus node.
With the simultaneous application of lithium carbonate may develop hypothyroidism.
In an application procainamide increases the QT interval due to the additive effect on its value and the risk of ventricular tachycardia type “pirouette”. Increased plasma concentrations of procainamide and its metabolite N – acetylprocainamide and increased side effects.
With the simultaneous use of propranolol, metoprolol, sotalol possible hypotension, bradycardia, ventricular fibrillation, asystole.
With the simultaneous use of trazodone, a case of arrhythmias such as “pirouette”.
With the simultaneous use of quinidine increases the QT interval due to the additive effect on its value and the risk of ventricular tachycardia type “pirouette”. Quinidine Increased plasma concentrations increased and its side effects.
In an application described a gain side effects of clonazepam, which, in – apparently due to its cumulation due to inhibition of oxidative metabolism in the liver under the influence of amiodarone.
With the simultaneous use of cisapride significantly increase the QT interval due to the additive effect, the risk of ventricular arrhythmia (including type “pirouette”).
With the simultaneous application of cyclosporine increased the concentration in the blood plasma, the risk of nephrotoxicity.
A case of pulmonary toxicity, while the use of cyclophosphamide at high doses and amiodarone.
Increased amiodarone concentration in blood plasma owing to retardation of its metabolism under the influence of cimetidine and other inhibitors of microsomal liver enzymes.
It is believed that by inhibiting amiodarone influenced by liver enzymes, which occurs with the participation of phenytoin metabolism may increase the last plasma concentration and amplification of its side effects.
Because of induction of microsomal liver enzymes under the influence of phenytoin increases the rate of metabolism in the liver and amiodarone is a decrease in blood plasma concentration.
Analogues drug Amiodarone
The structural analogs of active material:
- Amiodarone Belupo;
- Amiodarone Sandoz;
- Amiodarone Acre;
- Amiodarone hydrochloride;
- Vero Amiodarone;
In the absence of drug analogs of active material, it is possible to follow the links below on the disease, which makes it an appropriate drug and see the existing analogues for therapeutic impact.