Close
New

Medscape is available in 5 Language Editions – Choose your Edition here.

 

amiodarone (Rx)Brand and Other Names:Pacerone, Cordarone, more...Nexterone

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable solution

  • 50mg/mL
  • 150mg/100mL (Nexterone)
  • 360mg/200mL (Nexterone)
  • Conventional IV preparation contains polysorbate 80 and benzyl alcohol
  • Newer IV formulation (Nexterone) does not contain polysorbate 80 or benzyl alcohol

tablet

  • 100mg
  • 200mg
  • 400mg
more...

Stable Monomorphic or Polymorphic Ventricular Tachycardia (Off-label)

150 mg IV bolus in 10 minutes; may repeat q10min as necessary, THEN

1 mg/min IV for 6 hours, THEN

0.5 mg/min IV for 18 hours; not to exceed 2.2 g/24hr

For breakthrough episodes of VF or hemodynamically unstable VT , repeat the initial Load

Dosing considerations

  • Initiate in hospital with experienced personnel

ACLS, Pulseless Ventricular Fibrillation/Ventricular Tachycardia (Off-label)

300 mg IV or intraosseous push after dose epinephrine if no initial response to defibrillation

May follow initial dose with 150 mg IV q3-5min

Dosing considerations

  • Rapid IV push if pulseless/no BP

Ventricular Arrhythmias

PO

  • Load: 800-1600 mg PO qDay for 1-3 weeks until response; once adequate arrhythmia control achieved, reduce dose to 600-800 mg/day for 1 mo; THEN reduce to maintenance dose
  • Maintenance dose: 400 mg PO qDay

IV

  • 150 mg over first 10 min (15mg/min), followed by 360 mg over next 6 hr (1 mg/min), THEN 540 mg over remaining 18 hr (0.5 mg/min), for a total of 1000 mg over 24 hr before administering maintenance infusion
  • Maintenance: 0.5 mg/min for a total 720 mg/24hr at a concentration of 1-6 mg/mL (360 mg/200mL), or 1.8 mg/mL Nexterone at rate of 278 mL/min
  • Duration of therapy: May continue to administer 0.5 mg/min for 2-3 weeks regardless of patient's age, renal function or ventricular function

Conversion to oral amiodarone after IV administration

<1 week IV infusion: 800-1600 mg/day

1-3 week IV infusion: 600-800 mg/day

>3 week IV infusion: 400 mg/day

Dosage Forms & Strengths

injectable solution

  • 50mg/mL
  • 150mg/100mL (Nexterone)
  • 360mg/200mL (Nexterone)
  • Note: Conventional IV preparation contains polysorbate 80 and benzyl alcohol
  • Newer IV formulation (Nexterone) does not contain polysorbate 80 or benzyl alcohol

tablet

  • 100mg
  • 200mg
  • 400mg
more...

Drug Resistant Refractory Cardiac Arrhythmias (Off-label)

PO

  • Age <1 year: 600-800 mg/1.73 m² q24hr or divided q12hr; continue therapy for 4-14 days and/or until adequate control achieved; if initial treatment effective, decrease dosage to 200-400 mg/1.73 m² q24hr or divided q12hr 
  • Age >1 year: Until adequate control, 10-15 mg/kg/day PO qDay or divided q12hr; if effective, reduce to 5 mg/kg/day PO qDay or divided q12hr 

IV

  • Loading dose (limited data): 5 mg/kg IV over 30-60 min
  • Maintenance dose: 0.005 mg/kg/min IV infusion; may increase to 20 mcg/kg/min per 24 hr; consider converting to oral therapy within 24-48 hr

Pulseless Ventricular Tachycardia or Ventricular Fibrillation (PALS dosing) (Off-label)

5 mg/kg IV/IO rapid bolus; not to exceed 300 mg/dose; may repeat twice to maximum 15 mg/kg during acute treatment 

Supraventricular Tachycardia (Off-label)

Infants/children/adolescents: 5 mg/kg IV over 1 hr initially; follow with 5 mg/kg/day for 47 hr 

Maintenance: 10-20 mg/kg/day for 7-10 days; follow with 3-20 mg/kg/day

Dosing Considerations

In a pediatric trial of 61 patients, aged 30 days to 15 years, hypotension (36%), bradycardia (20%), and atrioventricular block (15%) were common dose-related adverse events and were severe or life-threatening in some cases

Injection site reactions were seen in 5 (25%) of the 20 patients receiving amiodarone HCI injection through a peripheral vein, irrespective of dose regimen

Conventional IV amiodarone contains the preservative benzyl alcohol; there have been reports of fatal “gasping syndrome” in neonates (children aged less than 1 month) following the administration of IV solutions containing the preservative benzyl alcohol

Nexterone does not contain benzyl alcohol

Recommended to start dosing at the lower end of the dosing range because elderly may be predisposed to toxicity

Next

Interactions

Interaction Checker

amiodarone and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
             activity indicator 
            Previous
            Next

            Adverse Effects

            >10%

            Increased liver AST or ALT levels (3-20%; as high as 40-50% in some studies)

            Hypotension (16%)

            Dizziness (3-40%)

            Headache (3-40%)

            Malaise (3-40%)

            Abnormal gait/ataxia (3-40%)

            Fatigue (3-40%)

            Impaired memory (3-40%)

            Involuntary movement (3-40%)

            Sleep disturbances (3-40%)

            Photosensitivity (10-75%)

            Hypothyroidism (1-22%)

            Constipation (10-33%)

            Anorexia (10-33%)

            1-10%

            CHF (3%)

            Bradycardia (3-5%)

            AV block (5%)

            SA node dysfunction (1-3%)

            Hyperthyroidism (3-10%)

            Hepatitis and cirrhosis (<3%)

            Visual disturbances (2-9%)

            Optic neuritis (1%)

            Frequency Not Defined

            Corneal microdeposits

            Demyelinating polyneuropathy

            Postmarketing Reports

            Hypersensitivity: Anaphylactic/anaphylactoid reaction (including shock), angioedema, urticaria

            Pulmonary: Eosinophilic pneumonia, ARDS (in postoperative setting), bronchospasm, possibly fatal respiratory disorders (including distress, failure, arrest, and ARDS), bronchiolitis obliterans organizing pneumonia (possibly fatal), fever, dyspnea, cough, hemoptysis, wheezing, hypoxia, pulmonary infiltrates and/or mass, pulmonary alveolar hemorrhage, pleural effusion, pleuritis

            Gastrointestinal: Hepatitis, cholestatic hepatitis, cirrhosis, pancreatitis, dry mouth

            Nephrology: Renal impairment, renal insufficiency, acute renal failure

            Neurology: Pseudotumor cerebri, parkinsonian symptoms, such as akinesia and bradykinesia (sometimes reversible with discontinuation of therapy)

            Endocrine: SIADH, thyroid nodules/thyroid cancer

            Dermatology: Toxic epidermal necrolysis (sometimes fatal), erythema multiforme, Stevens-Johnson syndrome, exfoliative dermatitis, drug rash with eosinophilia and systemic symptoms (DRESS), eczema, skin cancer, vasculitis, pruritus, bullous dermatitis

            Hematology: Hemolytic anemia, aplastic anemia, pancytopenia, neutropenia, thrombocytopenia, agranulocytosis, granuloma

            Musculoskeletal: Myopathy, muscle weakness, rhabdomyolysis, demyelinating polyneuropathy

            Psychiatric: Hallucination, confusional state, disorientation, delirium

            Genitourinary: Epididymitis, impotence

            Previous
            Next

            Warnings

            Black Box Warnings

            Indicated only for life-threatening arrhythmias

            • Indicated only for life-threatening arrhythmias because of risk for substantial toxicity; poses major management problems that could be life-threatening in patients at risk of sudden death; therefore, make every effort to utilize alternative agents first
            • Difficulty of using amiodarone effectively and safely poses significant risk to patients
            • Patients must be hospitalized while IV loading dose administered; response generally requires at least 1 wk
            • Absorption and elimination variable, maintenance dosing difficult, and often requires dosage decrease or temporary discontinuation
            • Retrospective survey of 192 patients with ventricular tachyarrhythmias showed 84 patients required dose reduction and 18 required at least temporary discontinuation (because of adverse reactions); several trials have reported 15-20% overall frequencies of discontinuation because of adverse reactions
            • Time to recurrence of previously controlled life-threatening arrhythmia after discontinuation or dose adjustment is unpredictable (ranges from weeks to months); patient is at great risk during this transition and may require hospitalization
            • Fatal toxicities: Fatal toxicities may be caused by pulmonary toxicity, hepatotoxicity, and proarrhythmic effect

            Pulmonary toxicity

            • Presents as hypersensitivity pneumonitis or interstitial/alveolar pneumonitis (10-17% incidence with 400 mg/day)
            • May present without symptoms as abnormal diffusion capacity in a much higher percentage of patients
            • Fatal in ~10% of cases

            Liver injury

            • Common but usually mild and evidenced only by abnormal liver enzymes
            • Overt liver disease can occur and has been fatal in a few cases

            Proarrhythmic effect

            • Like other antiarrhythmics, can exacerbate the arrhythmia (eg, by making the arrhythmia less well tolerated or more difficult to reverse)
            • 2-5% incidence; includes significant heart block or sinus bradycardia
            • Manage arrhythmias in proper clinical setting
            • Effects are prolonged when they occur because of long drug half-life

            Contraindications

            Hypersensitivity

            Severe sinus node dysfunction, 2°/3° AV block or bradycardia causing syncope (except with functioning artificial pacemaker), cardiogenic shock

            Avoid during breastfeeding

            Cautions

            To be administered only by physicians experienced in treatment of life-threatening arrhythmias, who are thoroughly familiar with risks and benefits of amiodarone therapy, and have access to facilities adequate for monitoring effectiveness and side effects of treatment; because of long half-life of amiodarone and its metabolite desethylamiodarone, the potential for adverse reactions or interactions, as well as observed adverse effects, can persist following amiodarone withdrawal

            Adjust dosage based on adverse reaction and therapeutic response

            Avoid excessive exposure to sunlight; may cause photosensitivity

            Attempts to substitute other antiarrhythmic agents when amiodarone must be stopped is difficult due to the complex pharmacokinetics of the drug, including prolonged duration of action and half-life and difficulties predicting them, which in turn increases risk for drug interactions

            Hypothyroidism has been reported in 2 to 10% of patients receiving amiodarone and may be primary or subsequent to resolution of preceding amiodarone-induced hyperthyroidism; manage hypothyroidism by reducing the dose of or discontinuing amiodarone and considering the need for thyroid hormone supplement

            Risks of acute MI, AV block, cardiomegaly; especially with IV administration

            Bradycardia and atrio-ventricular block reported; treat bradycardia by slowing infusion rate or discontinuing therapy; in some patients, inserting a pacemaker is required; treat patients with a known predisposition to bradycardia or AV block in a setting where a temporary pacemaker is available

            Hypotension is the most common adverse reaction; in some cases, hypotension may be refractory and result in a fatal outcome; treat hypotension initially by slowing the infusion; additional standard therapy may include vasopressor drugs, positive inotropic agents, and volume expansion; monitor initial rate of infusion closely, not to exceed recommended rate

            Chronic administration of antiarrhythmic drugs may affect defibrillation or pacing thresholds in patients with implanted defibrillators, pacemakers; assess when therapy is initiated and throughout

            Correct hypokalemia, hypomagnesemia or hypocalcemia before initiating treatment as these disorders can exaggerate the degree of QTc prolongation and increase the potential for TdP; give special attention to electrolyte and acid-base balance in patients experiencing severe or prolonged diarrhea or in patients receiving concomitant diuretics and laxatives, systemic corticosteroids, amphotericin B (IV) or other drugs affecting electrolyte levels

            May increase risks of pulmonary fibrosis; liver disease; hypotension, bradycardia, hyperthyroidism; optic neuropathy; pleural effusion; pneumonitis (including eosinophilic pneumonia)

            Acute-onset (days to weeks) pulmonary injury reported in patients treated with IV amiodarone; findings have included pulmonary infiltrates and masses on X-ray, bronchospasm, wheezing, fever, dyspnea, cough, hemoptysis, and hypoxia; some cases have progressed to respiratory failure or death

            Postoperatively, occurrences of adult respiratory distress syndrome reported in patients receiving amiodarone therapy who have undergone either cardiac or noncardiac surgery; although patients usually respond well to vigorous respiratory therapy, in rare instances the outcome has been fatal; until further studies performed, monitor FiO2 and determinants of oxygen delivery to tissues (e.g., SaO2, PaO2) while taking amiodarone

            Use caution when administering concomitantly with drugs that prolong QTc interval

            Corneal microdeposits appear in majority of adults treated; usually discernible only by slit-lamp examination, but give rise to symptoms such as visual halos or blurred vision up to 10% of patients; corneal microdeposits are reversible upon reduction of dose or termination of treatment; asymptomatic microdeposits alone are not reason to reduce dose or discontinue treatment

            Causes increased INR; use caution when initiating therapy in patients treated with warfarin

            Close perioperative monitoring is recommended in patients undergoing general anesthesia who are on amiodarone therapy as they may be more sensitive to myocardial depressant and conduction effects of halogenated inhalational anesthetics

            Fatal cutaneous reactions reported, including Stevens-Johnson syndrome and toxic epidermal necrolysis; discontinue therapy if symptoms of progressive skin rash occur

            Monitor hepatic enzymes regularly in patients receiving relatively high maintenance doses

            Peripheral neuropathy reported rarely with chronic administration; may resolve upon discontinuation of therapy

            Bradycardia, some requiring pacemaker insertion reported when ledipasvir/sofosbuvir or sofosbuvir with simeprevir initiated in patients on amiodarone; bradycardia generally occurred within hours to days, but in some cases up to 2 weeks after initiating antiviral treatment; monitor heart rate in patients taking or recently discontinuing amiodarone when starting antiviral treatment

            Amiodarone can cause fetal harm when administered to a pregnant woman; fetal exposure may increase potential for adverse experiences including cardiac, thyroid, neurodevelopmental, neurological and growth effects in neonate; inform patient of potential hazard to fetus if amiodarone administered during pregnancy or if patient becomes pregnant while taking amiodarone

            Previous
            Next

            Pregnancy & Lactation

            Pregnancy category: D

            Lactation: Excreted into breast milk; not recommended

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
            Previous
            Next

            Pharmacology

            Mechanism of Action

            Class III antiarrhythmic agent, which inhibits adrenergic stimulation; affects sodium, potassium, and calcium channels; markedly prolongs action potential and repolarization; decreases AV conduction and sinus node function

            Absorption

            Bioavailability: 35-65%

            Onset (PO): Initial response 2 days to 3 wk; peak response takes 1 week to 5 months

            Duration (PO): Up to 50 days after discontinuation of therapy

            Peak serum time: 3-7 hr (PO)

            Therapeutic range: 0.8-2.8 mcg/mL

            Toxicity range: >2-2.5 mcg/mL

            Distribution

            Protein bound: 96%

            Vd: 66 L/kg

            Metabolism

            Liver with enterohepatic recirculation; hepatic CYP2C8 and CYP3A3/4 isozymes

            Metabolites: N-desethylamiodarone (DEA) (active)

            Enzymes inhibited: CYP2C9, CYP2D6, CYP3A3/4

            Elimination

            Half-life: 26-107 days (parent drug); 61 days (DEA metabolite)

            Dialyzable: Not dialyzable by hemodialysis or peritoneal dialysis

            Excretion: Feces; urine

            Previous
            Next

            Administration

            IV Incompatibilities

            Additive: Floxacillin, quinidine

            Syringe: Heparin

            Y-site: Aminophylline, ampicillin/sulbactam, bivalirudin, cefamandole, cefazolin, ceftazidime, digoxin, furosemide(?), heparin, imipenem/cilastatin, mezlocillin, piperacillin, piperacillin/tazobactam, K phosphates, Na bicarb, Na nitroprusside(?), Na phosphates

            IV Compatibilities

            Solution: D5W (incomp in 24 hr), NS (incomp in 24 hr)

            Additive: dobutamine, furosemide (incomp at high conc), lidocaine, KCl, procainamide, propafenone, verapamil

            Y-site (partial list): amphotericin B, atracurium, atropine, CaCl2, ciprofloxacin, clarithromycin, dobutamine, dopamine, epinephrine, eptifibatide, erythromycin, esmolol, fentanyl, fluconazole, gentamicin, labetalol, lorazepam, lidocaine, Mg sulfate (incomp at high conc), milrinone, morphine sulfate, nitroglycerin, norepinephrine, KCl, vancomycin

            IV Preparation

            Loading IV infusion: Dilute 150 mg (3 mL) in 100 mL to form 1.5 mg/mL concentration

            Slow/maintenance infusion: Dilute 900 mg (18 mL) of amiodarone with 500 mL to form 1.8 mg/mL concentration

            Conventional amiodarone: Dilute only with D5W

            Nexterone: May dilute with either D5W or 0.9% NaCl

            For subsequent maintenance infusion, may use 1-6 mg/mL concentrations

            IV Administration

            Concentrations >2 mg mL associated with venous irritation

            If concentration >2 mg/mL, administer via central venous catheter; in-line filter should be used during administration

            Administer IV via volumetric infusion pump

            Do not use evacuated glass containers for admixing, as incompatibility with a buffer in the container may cause precipitation

            Does not need to be protected from light during administration

            See dosing for bolus/infusion times

            Conventional amiodarone

            • Administer in glass/polyolefin bottles for infusions >2 hr

            Nexterone

            • First product to successfully overcome solubility issues of amiodarone by removing the original cosolvents polysorbate 80 and benzyl alcohol
            • As a result, Nexterone does not have many of the product administration limitations regarding compatibility and stability with plastics and ionic infusion fluids, which are included in the labeling of conventional IV amiodarone
            • May be diluted in D5W or 0.9% NaCl and administered in polyvinyl chloride (PVC), polyolefin, or glass containers

            Storage

            Store at room temp; protect from light and excessive heat

            Previous
            Next

            Images

            Previous
            Next

            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Add or Remove Plans
            Plans for
            Select State:
            Non-Medicare PlansMedicare Plans

            Select a box to add or remove a plan.

            Select a class to view formulary status for similar drugs

            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
             
             
             
            All material on this website is protected by copyright, Copyright © 1994-2016 by WebMD LLC. This website also contains material copyrighted by 3rd parties.