Description

Simple

A medication used to regulate the rhythm of the heart.

Clinical

A class III antiarrhythmic indicated for the treatment of recurrent hemodynamically unstable ventricular tachycardia and recurrent ventricular fibrillation.

Overview

Amiodarone is a benzofuran derivative, anti-arrhythmic drug used commonly in a variety of settings.[4] Most known for its approved indication in life-threatening ventricular arrhythmias, it is also used off-label in the outpatient and inpatient setting for atrial fibrillation. Because of its ability to cause serious toxicity and possibly death, amiodarone use should be reserved for its approved indications, according to prescribing information.[18,19,20]

Pharmacology

Indication

The FDA approved indications for amiodarone are recurrent ventricular fibrillation (VF)
and recurrent hemodynamically unstable ventricular tachycardia (VT). The FDA emphasizes that this drug should only be given in these conditions when they are clinically documented and have not responded to norma... Read more

Pharmacodynamic

After intravenous administration, amiodarone acts to relax smooth muscles that line vascular walls, decreases peripheral vascular resistance (afterload), and increases the cardiac index by a small amount. Administration by this route also decreases cardiac conduction, preventing and treating arrhyth... Read more

Mechanism of action

Amiodarone is considered a class III anti-arrhythmic drug. It blocks potassium currents that cause repolarization of the heart muscle during the third phase of the cardiac action potential. As a result amiodarone increases the duration of the action potential as well as the effective refractory peri... Read more

Absorption

The Cmax of amiodarone in the plasma is achieved about 3 to 7 hours after administration.[18] The general time to onset of action of amiodarone after one dose given by the intr... Read more

Protein binding

The protein binding of amiodarone is about 96%.[4, Read more

Volume of distribution

In a pharmacokinetic study of 3 healthy individuals and 3 patients diagnosed with supraventricular tachycardia (SVT), the volume of distribution was found to be 9.26-17.17 L/kg in healthy volunteers and 6.88-21.05 L/kg in the SVT patients.[ Read more

Clearance

The clearance of amiodarone after intravenous administration in patients with ventricular fibrillation and ventricular tachycardia ranged from 220 to 440 ml/hr/kg in one clinically study.[ Read more

Half life

The terminal half-life of amiodarone varies according to the patient, but is long nonetheless, and ranges from about 9-100 days. The half-life duration varies according to different sources. [ Read more

Route of elimination

Amiodarone is eliminated primarily by hepatic metabolism and biliary excretion.[4... Read more

Toxicity

The LD50 of oral amiodarone in mice and rats exceeds 3,000 mg/kg.[18]
An overdose with amiodarone can have a fatal outcome due to its potential to cause arrhythmia. Signs or s... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Peripheral neuropathy US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Gait abnormalities US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Involuntary movements US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Coordination abnormal US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 20-40%
  • Clinical Trial
    Neurologic Symptoms US
  • Kind: experimental
    • Percent: 20-40
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 10-33
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 10-33
  • Clinical Trial
    Vomiting US
  • Kind: experimental
    • Percent: 25
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 25
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 25
  • Clinical Trial
    Gastrointestinal Symptoms US
  • Kind: experimental
    • Percent: 25
  • Clinical Trial
    Dermatological reaction US
  • Kind: experimental
    • Percent: 15
  • Varying Reports
    Photosensitivity US
  • Kind: experimental
    • Percent: 10
  • Varying Reports
    Paresthesias US
  • Kind: experimental
    • Percent: 4-9%
  • Clinical Trial
    Ataxia US
  • Kind: experimental
    • Percent: 4-9%
  • Unclassified
    Dizziness US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Visual Disturbance US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Pulmonary Inflammation US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Pulmonary Fibrosis US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Abnormal Liver Function Tests US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Photosensitivity US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    Solar dermatitis US
  • Kind: experimental
    • Percent: 4-9
  • Clinical Trial
    New onset ventricular fibrillation US
  • Kind: experimental
    • Percent: 2-5
  • Clinical Trial
    Polymorphic ventricular tachycardia US
  • Kind: experimental
    • Percent: 2-5
  • Clinical Trial
    Polymorphic ventricular tachycardia US
  • Kind: experimental
    • Percent: 2-5
  • Clinical Trial
    Ventricular Tachycardia (VT) US
  • Kind: experimental
    • Percent: 2-5
  • Clinical Trial
    Sinus arrest with suppression of escape foci US
  • Kind: experimental
    • Percent: 2-4
  • Clinical Trial
    Symptomatic Bradycardia US
  • Kind: experimental
    • Percent: 2-4
  • Post Marketing
    Abnormal smell US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Abnormal taste US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Flushing US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Decreased libido US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Cardiac Arrhythmias US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Congestive Heart Failure US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Hypothyroidism US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    SA node dysfunction US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Coagulation Abnormalities US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Abnormal smell US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Gastrointestinal US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Abnormal salivation US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial
    Sleep Disturbances US
  • Kind: experimental
    • Percent: 1-3
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Hypersensitivity:
      • true
      • iodine
    • Regions: US
    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US
    • Route:
      • Oral
      • Intravenous
    • Regions: US
    • Patient Conditions:
        • Name: Cardiogenic Shock
        • Drugbank Id: DBCOND0030788
    • Route:
      • Oral
      • Intravenous
    • Regions: US
    • Patient Conditions:
        • Name: Severe sinus-node dysfunction
        • Drugbank Id: DBCOND0108203
        • Modification Of:
          • Base:
            • Name: Sinus-node Dysfunction
            • Drugbank Id: DBCOND0051038
          • Severity:
            • Includes:
              • severe
    • Route:
      • Oral
      • Intravenous
    • Regions: US
    • Patient Conditions:
        • Name: Second-degree AV block
        • Drugbank Id: DBCOND0096365
    • Route:
      • Oral
      • Intravenous
    • Regions: US
    • Patient Conditions:
        • Name: Third-degree atrioventricular block
        • Drugbank Id: DBCOND0108204
    • Route:
      • Oral
      • Intravenous
    • Regions: US
    • Patient Conditions:
        • Name: Syncope caused by episodes of bradycardia
        • Drugbank Id: DBCOND0108206
        • Combination Of:
          • Caused By:
              • Name: Episodes of bradycardia
              • Drugbank Id: DBCOND0108205
          • Included Conditions:
              • Name: Syncope
              • Drugbank Id: DBCOND0007621

    Food Interactions

    Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of amiodarone.

    Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of amiodarone. Therefore it may reduce the serum concentration and effectiveness of amiodarone.

    Take with or without food. The absorption is unaffected by food.