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Amiodarone is used in the treatment of cardiac arrhythmias. The drug was developed in 1961 and is now included in many medications. He is widely regarded as very effective, but can cause serious side effects. For this reason Amiodarone is used only as a means second choice in the treatment of cardiac arrhythmias. Here you can read everything about Amiodarone.
Mechanism of action
In order for the heart muscle regularly can pump blood through the body, its cells must be excited uniformly. This excitation formed between back repeatedly. These processes called ion channels are involved: Through them flow when energized and when the repolarization certain charged particles (ions) into the cells or out of the cells
At the heart rhythm (arrhythmia) is disturbed this uniform alternation between arousal and regression of excitement: a result, the heart muscle can no longer contract rhythmically – an irregular heart rate is the result. If there is more common to such irregularities, an adequate blood flow to the body is no longer guaranteed. Then may be necessary, treatment with so-called antiarrhythmics (medicines for heart rhythm disturbances).
A representative of antiarrhythmics is the active ingredient Amiodarone. It blocks several ion channels (potassium, sodium and calcium channels) and thus inhibits an excessive excitation of the heart muscle. So the beat rate of the heart is normalized.
Amiodarone Hydrochloride is taken up in varying amounts from the intestine into the blood (25-80 percent). Thereupon, the degradation in the liver and excretion primarily in the faeces.
Because the drug accumulates in fatty tissue, it can after discontinuation of the drug still take up to 100 days until Amiodarone is completely removed from the body.
When will Amiodarone used?
The active ingredient is Amiodarone in cardiac arrhythmias (such as atrial fibrillation) used when other antiarrhythmic drugs were ineffective or not allowed to be used.
How Amiodarone is used
Amiodarone can be injected in acute cases, but usually a treatment is carried out in the form of tablets.
The dosage is in the first eight to ten days 600-1000 milligrams daily. Thereafter, the daily dose will be gradually reduced to 100 to 200 milligrams.
reason for this procedure: Amiodarone accumulates in the fatty tissue. But effect is only part of the active compound which is present in the blood, which is why at the beginning of the treatment a “Amiodarone saturation” of adipose tissue is needed. The effect is also for this reason, after about two weeks.
In particular, in elderly patients requires this particular drug “distribution” in the body a regular dose monitoring by the treating physician.
What are the side effects of Amiodarone?
Very often, that is, more than ten percent of those treated, can cause by deposits on the cornea Amiodarone side effects such as rashes and blurred vision.
Often (at one to ten percent of patients), there is black violet, reversible skin discoloration, thyroid disorders, tremors, insomnia, slowed heartbeat (bradycardia), low blood pressure (hypotension), muscle weakness and lung changes with unproductive and breathing difficulties.
Occasionally (ie less than one percent of patients), the Amiodarone intake to reduced sexual desire (libido), arousal disorders of forwarding on the heart, fatigue and gastrointestinal symptoms. Even more rarely can cause renal dysfunction.
What should be considered when taking Amiodarone?
In some cases, Amiodarone should not be used:
- to low pulse (less than 55 beats per minute, so-called “Brady”)
- all forms of delaying the excitation forwarding the heart (eg, atrioventricular block), unless a pacemaker is used
- thyroid diseases
- iodine allergies
- certain changes in the electrocardiogram (QT prolongation)
- to low potassium levels
- Simultaneous treatment with so-called MAO inhibitors such as tranylcypromine, moclobemide, selegiline and rasagiline (depression and)
- Co-administration of (at excessively high cholesterol levels), if the daily dose exceeds 20 milligrams
- Pregnancy and lactation
Pregnancy and lactation
Amiodarone should be used by pregnant only in emergencies, as there is evidence that the drug can cause the unborn damage. There are, however, very few data on the use during pregnancy.
In a planned pregnancy Amiodarone should be discontinued already six months’ advance, so that no Amiodarone remains longer in the body at the time of fertilization.
Is a revenue during lactation unavoidable or Amiodarone was taken during pregnancy, the baby should not be breastfed, as the drug is excreted in human breast milk.
To use the drug in children and adolescents are to date is insufficient experience. Treatment should only be done after a strict risk-benefit assessment by the doctor.
While you are taking Amiodarone the skin is particularly sensitive to light (“photosensitizing”). Therefore, it should be omitted Sunbake.
Because Amiodarone is very slowly eliminated from the body, still has up to six months after stopping the drug with interactions when other drugs are expected.
Amiodarone enhances the effects and side effects of the following agents:
- warfarin (blood-thinning drug)
- Phenytoin (medicines)
- Diltiazem, Verapamil (for cardiac arrhythmias,)
- cyclosporin, Tacrolimus (suppress the immune system, such as after transplants or in autoimmune diseases)
- fentanyl (strong painkiller)
- cholesterol-lowering drug (statin)
- Sildenafil (for impotence)
- midazolam (for anesthesia)
- triazolam (sleeping pills)
- dihydroergotamine, ergotamine (for migraine)
- flecainide (for arrhythmia)
The following substances strengthen Amiodaronwirkung:
- digitalis (for heart disorders)
- medicines for HIV
- Grapefruit Juice
When co-administered the following drugs and Amiodarone can cause a potentially life threatening cardiac arrhythmia (“torsades de pointes tachycardia”) are:
- other antiarrhythmics
- certain active substances against bacterial, parasitic and fungal infections (Erythromycin, cotrimoxazole, pentamidine, moxifloxacin)
- drugs to treat mental illness (lithium, tricyclic antidepressants, chlorpromazine, thioridazine, fluphenazine, pimozide, haloperidol, amisulpride)
- antimalarial (quinine, mefloquine, Chloroquine)
- cisapride (for stomach ulcers)
laxatives, diuretics (diuretics), glucocorticoids (“cortisone”) or amphotericin B (antifungals) lead to low potassium levels in the blood. When co-administered with Amiodarone, it may also lead to a “torsade de pointes tachycardia” or other heart rhythm disorders.
Driving and using machines
Even with proper dosage can Amiodarone affect the reactivity strong. Experts therefore recommend that, during the treatment to the active participation in the road traffic and using heavy machinery to dispense.
How to obtain medication with Amiodarone
medication with Amiodarone are highly effective drugs, in which the treatment success should be regularly checked by the doctor. Therefore, these drugs are available only with a doctor’s prescription in the pharmacy.
Since when Amiodarone is known?
Amiodarone was developed in the year 1961st Meanwhile chemically optimized active ingredients are available in which fewer side effects occur. Amiodarone is therefore only used as a means second choice to control heart rhythm.