Amiodarone is an anti-anginal and a class 3 antiarrhythmic medication which should be used under monitored cardio-physician or specialist supervision.
This drug is also known as Amiobeta, Aratac, SKF 33134 A, Amiodarone, Amiodarex, Amiodarone, Amiohexal, Amiodarone Hydrochloride, Braxan, Corbionax, Rytmarone, L3428, Ortacrone, Cordarex, Cordarone Hydrochloride, and Amiodarone Kordaron.
Amiodarone falls under the class antiarrhythmics or antidysrhythmics class 3.
Mode Of Action
The mode of action of drugs in the class, including amiodarone hydrochloride, is to curb stimulation of the adrenergic receptors, to prolong the repolarization and the action potential, to reduce the functions of the sinus node and Atrioventricular conduction and lastly to affect the calcium, sodium and potassium channels. By performing all these actions, Amiodarone hydrochloride injection or the tablets helps save the heart from life-threatening arrhythmias.
The drug is available in different formulations. There is the amiodarone hydrochloride injection and the amiodarone tablets among others. The drug has a 35%-65% bioavailability once it is taken. When taken orally, the first response is from 48 hrs to 3 weeks. The drug's peak response starts from 7 days to 5 months. The drug continues showing its pharmacological effects for up to 50 days after it is discontinued. When taken orally, the drug reaches peak levels in blood in 2-8 hrs. The therapeutic index of amiodarone hydrochloride is 0.8 to 2.8 mcg/ ml. In case the drug is circulating above 2.5 mcg/ml, there will be toxicity symptoms or signs of amiodarone hydrochloride overdose. The drug is protein bound up to 96% to albumin hence caution is required when it comes to drug interactions. Its volume of distribution is 66 liters per kg. When it comes to metabolization, the drug undergoes first-pass metabolism in the hepatic system where it is metabolized by the CYP enzymes releasing an active metabolite such as N-desethylamiodarone (DEA). The active metabolite is eliminated from the body in 2 months time while the parent drug's elimination half-life is one month - four months. The drug is secreted in the enterohepatic circulation while a small portion is excreted in urine.
NB: This drug is not affected by dialysis, whether peritoneal or hemodialysis. This is a bonus!
Dosage and Usage
As discussed above, amiodarone is used to manage serious tachycardias and ventricular fibrillation. When used effectively, this drug restores the sinus rhythm of the heart. Despite this drug is very important, precautions must be taken when using it.
After receiving or purchasing the drug, read the instructions on the Amiodarone Hydrochloride manual provided in the product box. If you feel you need answers, kindly consult with your pharmacist or doctor. The medication guide is always the best guide before taking any medication.
This drug can be taken with meals or without. Usually, the oral formulation is the most common. It is mostly recommended to take it once or twice daily at a certain time. It is always good when you take a drug at specified times of the day every single day to enhance effectiveness.
Some fruits such as grapefruit elevate the levels of Amiodarone in your system. This among other drug interactions have been discussed on a sub-topic below.
Mostly, the dosage your doctor gives you is grounded on how the disease is acting with your body and the response to the disease from your body. Once you feel you are okay or feeling better, do not discontinue taking this drug rather keep taking it as prescribed. If your condition worsens, always seek your doctor for increased dosage or change of drug.
Amiodarone Side Effects
Some minor side effects might be noted when taking this drug. Not all though and still, they are not supposed to be worse to an extent that they affect your activities daily living. In case they reach to such a point, consult your doctor/ pharmacist.
You might experience slight hypotension, your liver function tests might show elevated levels of AST and ALT as higher as 45%, feelings of drowsiness, headaches, general body aches, and fatigue, abnormal walking styles, and postures, confusion, lack of remembrance, disturbances during sleep, fecal impaction among many others.
Just as any other prescribed drug, some meds affect the distribution of other drugs in the system. It is important to know these drugs so that by no chance will you take them concomitantly. These drug interactions are as follows:
- If Amiodarone Hydrochloride is used concomitantly with Phenytoin, the levels of phenytoin rise steadily in blood and a patient could easily develop phenytoin overdose symptoms. These symptoms include extreme fatigue, involuntary eye movement among other signs.
- There is an increased rate of a patient on anticoagulants such as warfarin or coumarins, developing an increased risk of bleeding due to the effect of amiodarone hydrochloride on concomitant usage. When used together, the prothrombin time (PT) is increased/ prolonged.
- Amiodarone hydrochloride should not be used with procainamide. This is due to procainamide increased blood concentrations which might lead to its toxicity.
- Concomitant administration of quinidine with amiodarone hydrochloride has seen the former drug increasing in serum plasma which may lead to quinidine toxicity. You should seek your doctor when using the two drugs altogether.
- Cyclosporine, an immunosuppressant drug, increases in serum plasma when used concomitantly with amiodarone hydrochloride. This leads to increased levels of creatinine which fail to subside despite a decrease in cyclosporine dosage.
- These are not the only drugs that interact with Amiodarone hydrochloride. Therefore, it is very important to be cautious with any drug that you will be taking concomitantly with. Always consult your doctor or pharmacist when mixing or taking drugs together.
This drug is marked as a category D drug in pregnancy. During pregnancy, this drug should be used as the last result in the management of life-threatening maternal/fetal tachyarrhythmias which have become resistant to other drugs. Studies have shown that Amiodarone Hydrochloride may cause hypothyroidism in neonates or goiter. Nevertheless, this drug should be used only if the benefits are much better than the risks.
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