An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.
An antianginal and antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting Na,K-activated myocardial adenosine triphosphatase. There is a resulting decrease in heart rate and in vascular resistance.
Top Gene Interactions
- Metabolism: Amiodarone is extensively metabolized in the liver via CYP2C8 (under 1% unchanged in urine), and can effect the metabolism of numerous other drugs. The major metabolite of amiodarone is desethylamiodarone (DEA), which also has antiarrhythmic properties. The metabolism of amiodarone is inhibited by grapefruit juice, leading to elevated serum levels of amiodarone. Route of Elimination: Amiodarone is eliminated primarily by hepatic metabolism and biliary excretion and there is negligible excretion of amiodarone or DEA in urine. Half Life: 58 days (range 15-142 days)
- Uses/Sources: Intravenously, for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Orally, for the treatment of life-threatening recurrent ventricular arrhythmias such as recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia.
- Health Effects: Some side effects have a significant mortality rate: specifically, hepatitis, exacerbation of asthma and congestive failure, and pneumonitis.
- Route of Exposure: Slow and variable (about 20 to 55% of an oral dose is absorbed).
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: Intravenous, mouse: LD<sub>50</sub> = 178 mg/kg.
Mechanism of Action
|Target Name||Mechanism of Action||References|
Potassium voltage-gated channel subfamily H member 2
Voltage-dependent calcium channel subunit alpha-2/delta-2
Voltage-dependent T-type calcium channel subunit alpha-1H
Beta-1 adrenergic receptor