Amiodarone


Full Generic Medicine Info
Dosage/Direction for Use

Oral
Supraventricular arrhythmias
Adult: Initially, 200 mg tid for 1 week then reduced to 200 mg bid for another week. Maintenance: ≤200 mg daily based on patient response.
Elderly: Use minimum effective dose.

Oral
Ventricular arrhythmias
Adult: Initially, 200 mg tid for 1 week then reduced to 200 mg bid for another week. Maintenance: ≤200 mg daily based on patient response.
Elderly: Use minimum effective dose.

Intravenous
Ventricular arrhythmias
Adult: Initially, 5 mg/kg via infusion over a period of 20-120 minutes, may repeat infusion up to 1,200 mg (approx 15 mg/kg) per 24 hours, with a rate of infusion adjusted based on clinical response. For emergency cases: 150-300 mg via slow inj over ≥3 minutes, may be repeated at least 15 minutes after the first dose.
Elderly: Use the minimum effective dose.
Reconstitution: For initial infusion, dilute the required dose with 250 mL dextrose 5% solution, then 500 mL dextrose 5% solution for the succeeding infusion.
Incompatibility: Incompatible with 0.9% NaCl solutions. Y-site admin: Incompatible with aminophylline, cefamandole nafate, cefazolin, mezlocillin, heparin, Na bicarbonate.

Intravenous
Supraventricular arrhythmias
Adult: Initially, 5 mg/kg via infusion over a period of 20-120 minutes, may repeat infusion up to 1,200 mg (approx 15 mg/kg) per 24 hours, with a rate of infusion adjusted based on clinical response. For emergency cases: 150-300 mg via slow inj over ≥3 minutes, may be repeated at least 15 minutes after the first dose.
Elderly: Use the minimum effective dose.
Reconstitution: For initial infusion, dilute the required dose with 250 mL dextrose 5% solution, then 500 mL dextrose 5% solution for the succeeding infusion.
Incompatibility: Incompatible with 0.9% NaCl solutions. Y-site admin: Incompatible with aminophylline, cefamandole nafate, cefazolin, mezlocillin, heparin, Na bicarbonate.

Intravenous
Pulseless ventricular tachycardia
Adult: For cardiopulmonary resuscitation in cases that are resistant to defibrillation: Initially, 300 mg (or 5 mg/kg) via rapid inj. Additional 150 mg (or 2.5 mg/kg) may be given if ventricular fibrillation or pulseless ventricular tachycardia persists.
Reconstitution: Dilute required dose with 20 mL dextrose 5% solution.
Incompatibility: Incompatible with 0.9% NaCl solutions. Y-site admin: Incompatible with aminophylline, cefamandole nafate, cefazolin, mezlocillin, heparin, Na bicarbonate.

Intravenous
Ventricular fibrillation
Adult: For cardiopulmonary resuscitation in cases that are resistant to defibrillation: Initially, 300 mg (or 5 mg/kg) via rapid inj. Additional 150 mg (or 2.5 mg/kg) may be given if ventricular fibrillation or pulseless ventricular tachycardia persists.
Reconstitution: Dilute required dose with 20 mL dextrose 5% solution.
Incompatibility: Incompatible with 0.9% NaCl solutions. Y-site admin: Incompatible with aminophylline, cefamandole nafate, cefazolin, mezlocillin, heparin, Na bicarbonate.
Administration
May be taken with or without food. Take consistently w/ or w/o meals. Take w/ meals if high dose or to reduce GI discomfort.
Contraindications
Sinus bradycardia, sino-atrial heart block, severe conduction disturbances (e.g. high-grade AV block, bifascicular or trifascicular block) without a presence of pacemaker, cardiogenic shock, severe hypotension, severe respiratory failure, known or history of thyroid dysfunction, known hypersensitivity to iodine, corneal refractive laser surgery. IV (bolus inj): Hypotension, heart failure, cardiomyopathy. Lactation. Concomitant use with drugs which may induce QT prolongation or torsades de pointes.
Special Precautions
Patient with latent or manifest heart failure, implantable cardioverter defibrillator or pacemaker, decompensated cardiomyopathy, hypotension. Patient undergoing surgery. Elderly. Pregnancy. Patient Counselling This drug may cause eye disorders, if affected, do not drive or operate machinery. Avoid excessive exposure to sunlight and use proper protective measures during treatment. Monitoring Parameters Monitor blood pressure, heart rate and rhythm (ECG), LFT, serum electrolytes (particularly K and Mg); pacing or defibrillation thresholds prior to and during treatment (in patients with implantable cardiac devices). Evaluate thyroid function tests prior to therapy and periodically (every 3-6 months) thereafter. Perform regular ophthalmologic examination, chest X-ray, and pulmonary function tests.
Adverse Reactions
Significant: Bradycardia, QT prolongation, hypotension, peripheral neuropathy, photosensitivity, optic neuropathy and/or optic neuritis. Eye disorders: Corneal microdeposits. Gastrointestinal disorders: Nausea, vomiting, dysgeusia, constipation. General disorders and administration site conditions: Inj site reactions (e.g. pain, erythema, oedema, extravasation, infiltration, inflammation, induration, necrosis, infection, thrombophlebitis, phlebitis, cellulitis). Investigations: Increased serum transaminases, elevated bilirubin levels. Nervous system disorders: Extrapyramidal tremor. Psychiatric disorders: Nightmares, sleep disorders. Skin and subcutaneous tissue disorders: Blue-grey skin discolouration (prolonged use), eczema.
Potentially Fatal: Onset or worsening of arrhythmia, hepatotoxicity (e.g. cirrhosis, hepatitis, jaundice, hepatic failure), pulmonary toxicity (e.g. hypersensitivity pneumonitis, alveolar/interstitial pneumonitis, fibrosis, pleural effusion), Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), hyperthyroidism.
Overdosage
Symptoms: Sinus bradycardia, heart block, ventricular tachycardia attacks, torsades de pointes, circulatory failure, hepatic injury. Management: Symptomatic and supportive treatment. Perform gastric lavage to reduce absorption. Administer β-adrenergic agonists or glucagon if bradycardia occurs. Monitor cardiac status.
Drug Interactions
Increased concentration with inhibitors of CYP3A4 (e.g. HIV-protease inhibitors, cimetidine). Reduced concentration with inducers of CYP3A4 (e.g. rifampicin, phenytoin). May induce bradycardia with β-blockers, Ca channel blockers, and other antiarrhythmic drugs. May increase risk of arrhythmia with stimulant laxatives, diuretics, systemic corticosteroids. May increase concentration of ciclosporin, clonazepam, digoxin, flecainide, procainamide, quinidine, simvastatin, warfarin. May affect drugs that are P-glycoprotein substrates.
Potentially Fatal: May cause prolongation of QT interval with fluoroquinolones, antipsychotics (e.g. chlorpromazine, thioridazine, fluphenazine), lithium, TCAs (e.g. doxepin, maprotiline, amitriptyline), halofantrine, and terfenadine.
Food Interaction
Increased plasma concentrations with grapefruit juice.
Action
Amiodarone is a class III antiarrhythmic agent but exhibits characteristics of all Vaughn-Williams classes. Its main effect is to lengthen the action potential and refractory period in the myocardial tissue. It blocks the Na, K, and Ca channels resulting in slowing of the conduction and prolongation of refractoriness. It produces negative chronotropic effect in nodal tissues similar to class IV.
Onset: Oral: 2 days to 3 weeks. IV: Within hours (electrophysiologic); 2-3 days to 1-3 weeks (antiarrhythmic).
Absorption: Variably and slowly absorbed from the gastrointestinal tract. Bioavailability: Oral: Approx 50% (range: 35-65%). Time to peak plasma concentration: 3-7 hours (oral).
Distribution: Extensively distributed and accumulates in fat, skeletal muscles, and highly perfused tissues (e.g. liver, lung, spleen). Crosses the placenta and enters breast milk. Volume of distribution: Oral: 66 L/kg (range: 18-148 L/kg); IV: 40-84 L/kg. Plasma protein binding: >96%.
Metabolism: Metabolised in the liver primarily by CYP3A4 and CYP2C8 to N-desethylamiodarone (active metabolite), may undergo enterohepatic recirculation.
Excretion: Mainly via faeces, urine (<1% as unchanged drug). Elimination half-life: Amiodarone: 58 days (range: 15-142 days); N-desethylamiodarone: 36 days (range: 14-75 days).
Storage
Intravenous: Store between 20-25°C. Protect from light and moisture. Oral: Store between 20-25°C. Protect from light and moisture.
CIMS Class
ATC Classification
C01BD01 - amiodarone ; Belongs to class III antiarrhythmics.
Disclaimer: This information is independently developed by CIMS based on amiodarone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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