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Amiodarone is an “old friend” that cardiologists often deal with, especially for arrhythmia patients. As an anti-arrhythmic star, what are the right and wrong of amiodarone?

History of amiodarone

(1) Synthesis, popularity and silence

Amiodarone has been used as an antiarrhythmic drug for more than 40 years. Amiodarone was not first used as an antiarrhythmic, but was synthesized in 1961 by scientists in the Labze laboratory in order to find a marketable coronary dilator, which was launched in France in 1968. Then a doctor in Argentina accidentally discovered its antiarrhythmic efficacy, and began to use it for antiarrhythmic treatment in 1976. In 1985, amiodarone was approved by the US FDA for antiarrhythmic treatment. At first, in order to shorten the onset time and enhance the effect of the drug, the dose of amiodarone was relatively large, so there were many toxic side effects and adverse reactions. As more arrhythmia drugs are developed, amiodarone is gradually being replaced by sodium channel blockers (also known as class I antiarrhythmic drugs).

(2) Become the first-line drug again

Before the 1990s, people judged the main efficacy of antiarrhythmic drugs to reduce the occurrence of arrhythmia. Until the CAST test in 1989, it was confirmed that antiarrhythmic drugs such as sodium channel blockers such as incarnib, flecainide, and moricizine could control arrhythmia, but they would make the prognosis of patients with structural heart disease worse. . The original quinidine and other drugs also have serious side effects, which shakes the status of class I antiarrhythmic drugs. Scientists have turned their research direction to the research and development of class III drugs, and amiodarone, a representative drug of class III antiarrhythmic drugs, has been proved to have good antiarrhythmic effects in a number of large-scale multicenter clinical trials. favored by clinicians.

Wide indications

Amiodarone is mainly used for the treatment of patients with structural heart disease, including heart failure, or arrhythmia that is ineffective with other drugs It is one of the alternatives when the corresponding drug treatment cannot be used.

At the same time of anti-arrhythmia, it also takes into account the etiological treatment, improves cardiac ischemia, and has a stronger effect than other drugs. According to the latest guidelines, it can be known that in acute In the treatment of patients with atrial fibrillation, amiodarone can be used to control ventricular rate in critically ill patients with heart failure or ischemia, but long-term use is not recommended unless other drugs are ineffective or unavailable.

As for the cardioversion of atrial fibrillation, amiodarone can be used for patients with stable hemodynamics, obvious symptoms, structural heart disease complicated with heart failure or acute coronary atherosclerotic syndrome. For patients with pre-excitation syndrome, amiodarone is listed as a contraindication abroad; but in China, for patients with pre-excitation syndrome and atrial fibrillation, amiodarone can be used as an alternative treatment for incapable of electrical cardioversion. With the defibrillator in place, it should be closely observed to prevent hemodynamic instability due to increased ventricular rate.

Amiodarone can be used intraoperatively and postoperatively to prevent and treat atrial fibrillation when left atrial ablation is performed concurrently with surgery. In CPR patients, amiodarone can also be used in patients with unsuccessful defibrillation and epinephrine, and in patients with structural heart disease using an implantable pacemaker-defibrillator (ICD), amiodarone can also be used to reduce ICD discharge.

Many adverse reactions and drug interactions

Although amiodarone is widely used, its adverse reactions are also worthy of attention. Intravenous amiodarone containing polysorbate 80 may cause liver damage and interstitial pneumonia, especially when used in large doses, the incidence of amiodarone pulmonary toxicity is 17%. Thyroid dysfunction may occur whether intravenous or oral amiodarone is used, and the incidence can be as high as 10.9% when used in high doses. At the same time, solar dermatitis and non-inflammatory keratopathy may occur during the use of amiodarone. Most of the adverse reactions of amiodarone are related to the time and concentration of administration.

Amiodarone may have some adverse reactions in combination with other drugs. If amiodarone is taken together with stimulant laxatives, hypokalemia can occur; when combined with propranolol, bradycardia and sinus arrest can occur; when combined with levofloxacin and erythromycin, it can lead to prolongation of QTc; Combined use of farin can easily cause cerebral hemorrhage.

Conclusion

Amiodarone, as an antiarrhythmic “panacea”, has some adverse reactions, but its therapeutic effect is undeniable. In the process of medication, we can use it correctly, monitor it at any time, detect it early and deal with it in a timely manner, we can still ensure the efficacy and safety of the medication.

Liu Longzhen, deputy director of the Pharmacy Department of Zhuzhou Second Hospital

References:

1. Li Gengshan. The history and current situation of clinical application of amiodarone[J]. Chinese Journal of Cardiac Pacing and Electrophysiology, 2001,15(05):8-11.

2. Expert Advice on Amiodarone Standard Application Expert Writing Group. Expert Suggestion on Amiodarone Standard Application[J ].Chinese Journal of Internal Medicine,2019,58(04):258-264.

3.Zhang Yuechen,Wang Qian.Adverse reactions of amiodarone[J].Chinese Journal of Hospital Pharmacy,1992,12( 06): 36-37.