Amiodarone

Last updated: December 4, 2021

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Amiodarone is a class III antiarrhythmic agent that blocks voltage-gated potassium channels. It is used in the treatment of acute ventricular tachycardia and persisting ventricular fibrillation (VF) after unsuccessful defibrillation, as well as the long-term treatment of refractory supraventricular arrhythmia (atrial fibrillation). Since amiodarone has a very low negative inotropic effect, it can be used in patients with a reduced ejection fraction (EF). Side effects commonly involve the thyroid, liver, heart, eyes, and central nervous system. Pulmonary side effects, such as lung fibrosis and chronic interstitial pneumonitis, are rare but severe. Because amiodarone is a cytochrome P450 inhibitor, simultaneous administration of other drugs should be considered carefully to minimize the risk of interactions.

  • Primary mechanism of action: antiarrhythmic effect via blockage of voltage-gated potassium channels → prolonged repolarization of the cardiac action potential
  • Secondary mechanism of action: inhibits β-receptors and sodium and calcium channels decreases conduction through the AV and sinus node
  • Special uses: : only antiarrhythmic agent with (almost) no negative inotropic effect → use in patients with reduced EF

References:[1][2]

Although amiodarone is an extremely effective antiarrhythmic drug, its side-effect profile limits its use primarily to short-term administration. Amiodarone accumulation in tissues can cause damage to the thyroid, lungs, nerves, skin, eyes, and heart.

Organ system Side effects
Lungs
Thyroid
Liver
  • AST/ALT > 2x normal
    • If patients experience more than a two-fold elevation, drug therapy should be discontinued. LFTs should be monitored at baseline and every 6 months.
  • Hepatitis and cirrhosis
Heart
Eyes
GI tract
Skin
CNS
GU tract

"Am-IOD-arone" consists of approx. 37% iodine!

References:[3][4]

We list the most important adverse effects. The selection is not exhaustive.

Amiodarone is the drug of choice for supraventricular arrhythmias in most heart failure patients (LVEF < 40%).
References:[1][5][6][7]

References:[8][9]

We list the most important contraindications. The selection is not exhaustive.

References:[1][8]

  • Amiodarone is very lipophilic → accumulation of amiodarone in myocardium and muscles → long duration of action
  • Metabolized in the liver by CYP3A4 with biliary excretion
Oral treatment IV bolus
Onset of action 2 days to 3 weeks Within a few hours
Time to peak effect 1 week to 5 months 15 minutes
Half-life elimination 40–55 days 9–36 days

References:[8][10]

  1. UpToDate. Amiodarone: Drug Information. In: Post TW, ed. UpToDate. Waltham, MA: UpToDate. https://www.uptodate.com/contents/amiodarone-drug-information.Last updated: January 1, 2017. Accessed: April 5, 2017.
  2. Latini R, Tognoni G, Kates RE. Clinical pharmacokinetics of amiodarone. Clin Pharmacokinet. 1984; 9 (2): p.136-156. doi: 10.2165/00003088-198409020-00002 . | Open in Read by QxMD
  3. WebMD. Amiodarone (Rx). In: WebMD, Amiodarone (Rx). New York, NY: WebMD. http://reference.medscape.com/drug/pacerone-cordarone-amiodarone-342296. Updated: January 1, 2017. Accessed: April 5, 2017.
  4. Olshansky B. The Management of Atrial Fibrillation in Patients with Heart Failure. In: Post TW, ed. UpToDate. Waltham, MA: UpToDate. https://www.uptodate.com/contents/the-management-of-atrial-fibrillation-in-patients-with-heart-failure.Last updated: September 27, 2016. Accessed: April 5, 2017.
  5. Giardina EG, Zimetbaum PJ. Monitoring and Management of Amiodarone Side Effects. In: Post TW, ed. UpToDate. Waltham, MA: UpToDate. https://www.uptodate.com/contents/monitoring-and-management-of-amiodarone-side-effects.Last updated: February 13, 2017. Accessed: April 5, 2017.
  6. Wolkove N, Baltzan M. Amiodarone pulmonary toxicity. Canadian respiratory journal. 2009; 16 (2): p.43-48.
  7. Agabegi SS, Agabegi ED. Step-Up To Medicine. Lippincott Williams & Wilkins ; 2013
  8. Julian DG, Camm AJ, Frangin G, et al. Randomised trial of effect of amiodarone on mortality in patients with left-ventricular dysfunction after recent myocardial infarction: EMIAT. Lancet. 1997; 349 (9053): p.667–674. doi: 10.1016/S0140-6736(96)09145-3 . | Open in Read by QxMD
  9. Amiodarone and ACLS. https://acls-algorithms.com/acls-drugs/amiodarone-and-acls/. Updated: April 5, 2017. Accessed: April 5, 2017.
  10. Parmar MS. Thyrotoxic Atrial Fibrillation. In: n/a, Thyrotoxic Atrial Fibrillation. New York, NY: WebMD. http://www.medscape.com/viewarticle/495668_1. Updated: January 1, 2005. Accessed: October 12, 2017.

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