Amiodarone (HCl)

Amiodarone (HCl) is a potassium channel blocking agent. Amiodarone (HCl) is iodinated benzofuran derivative. It has been widely used as an antiarrhythmic and antianginal drug. Amiodarone (HCl) is very effective against a wide variety of arrhythmias. It has prominent adverse effects and unusual pharmakokinetic properties that have limited its use. However Amiodarone (HCl) is being increasingly used, possibly because of the recognition that other drugs may be more dangerous.


Adult Dose
Dose: 5 mg/kg
Single Dose: 5 (5)
Frequency: As recommended.
Route: IV Inf
Instructions: Initially over 20-120 min with ECG monitoring. Max. 1.2 g in 24 hrs.
Neonatal
Dose: 116 to 231 mg/square metre
Single Dose: 170 (173.5)
Frequency: 24 hourly
Route: oral
Instructions: maintenance, 5 to 7 days/week
Paedriatic
Dose: 2.5 to 5 mg/kg
Single Dose: 3.8 (3.75)
Frequency: 24 hourly
Route: Oral
Instructions: Maintenance for 5-7 Days/week
Characteristics
. It is of Synthetic origin and belongs to Benzofuran. It belongs to Adenosine uptake inhibitor pharmacological group on the basis of mechanism of action and also classified in Anti arrhythmic agents pharmacological group.The Molecular Weight of Amiodarone (HCl) is 681.80. Its pKa is 5.6.
Contraindications
Amiodarone (HCl) is contraindicated in conditions like Thyroid disease,Sinus bradycardia.
Effects
The severe or irreversible adverse effects of Amiodarone (HCl), which give rise to further complications include Neuropathy, Thyroid disorders, Alopecia.Amiodarone (HCl) produces potentially life-threatening effects which include Pulmonary Fibrosis, Pulmonary alveolitis. which are responsible for the discontinuation of Amiodarone (HCl) therapy.The signs and symptoms that are produced after the acute overdosage of Amiodarone (HCl) include ECG alterations, Sinus bradycardia, QT interval lengthening, P-R interval lengthening.The symptomatic adverse reactions produced by Amiodarone (HCl) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Skin reactions, Sleep disturbancesX, GI reactions, Visual disorders.
Indications
'Amiodarone (HCl) is primarily indicated in conditions like Angina pectoris, Atrial fibrillation, Atrial flutter, Ectopic tachycardia, Hypertrophic cardiomyopathy, Mild to moderate dementia in alzheimer''s disease, Paroxysmal re-entry av tachycardia, Paroxysmal supraventricular tachycardia, Paroxysmal ventricular tachycardia, Pituitary desensitisation, Tobacco amblyopia and leber''s optic atrophy, Ventricular fibrillation, Ventricular fibrillation, pulseless ventricular tachycardia, and can also be given in adjunctive therapy as an alternative drug of choice in Treatment of arrhythmias.'
Interactions
Amiodarone (HCl) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAcebutololAmiodarone may enhance the bradycardic effect of Acebutolol. Possibly to the point of cardiac arrest.MajorMonitor increased signs and symptoms of bradycardia with Acebutolol (possibly to the point of cardiac arrest) if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. Ophthalmic beta-blockers are likely of little concern.Afatinibmay increase the level of afatinibuse alternative or reduced doseAmprenavirAmprenavir possibly increases plasma concentration of Lignocaine; increased risk of ventricular arrhythmias. ADVICE: Avoid concomitant use.MajorArtemisininAtenololIncreased myocardial depression when beta-blockers (e.g Atenolol) given with antiarrhythmics (e.g Amiodarone).Atomoxetine HClThe effect and toxicity of atomoxetine could be increased by CYP2D6 inhibitor.Betaxolol (HCl)Amiodarone may enhance the hypotensive effect of Betaxolol. Possibly to the point of cardiac arrest.MajorMonitor increased signs and symptoms of bradycardia with Betaxolol (possibly to the point of cardiac arrest) if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. Ophthalmic beta-blockers are likely of little concern.Bisoprolol (Fumarate)Amiodarone may enhance the bradycardic effect of Bisoprolol. Possibly to the point of cardiac arrest.MajorMonitor increased signs and symptoms of bradycardia with Bisoprolol (possibly to the point of cardiac arrest) if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. Ophthalmic beta-blockers are likely of little concern.Bupivacaine (HCl)Increased myocardial depression when Bupivacaine given with anti-arrhythmics (e.g Amiodarone).Carteolol (HCl)Amiodarone may enhance the bradycardic effect of Carteolol. Possibly to the point of cardiac arrest.MajorMonitor increased signs and symptoms of bradycardia with Carteolol (possibly to the point of cardiac arrest) if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. Ophthalmic beta-blockers are likely of little concern.CarvedilolChloroquineIncreased risk of ventricular arrhythmia when amiodarone given with antimalarials (e.g Quinine). ADVICE: Avoid concomitant use or only undertaken with caution and appropriate monitoring.CisaprideClomipramine (HCl)Increased risk of ventricular arrhythmia when amiodarone given with tricyclic antidepressant (e.g clomipramine). ADVICE: Avoid concomitant use or only undertaken with caution and appropriate monitoring.MajorCyclosporin AAmiodarone may decrease the metabolism of CycloSPORINE by inhibition of CYP450 3A4 result in increase blood concentration of cyclosporin enhances the risk of nephrotoxicity and neurotoxicity. ModerateMonitor increased serum concentrations and/or toxicity of cyclosporine if amiodarone is initiated/dose increased, or decreased serum concentrations if amiodarone is discontinued/dose decreased. A reduction in cyclosporine dosage will likely be needed.Dabigatranamiodarone increases Cmax and AUC of dabigatran as well as increases its renal clearance by 65%.DextromethorphanDigoxinAmiodarone may increase the serum concentration of Digoxin,increases intestinal transit time,reduce renal clearance and volume of distribution by displacing digoxin from protein binding sites.MajorDelayed (Sequence important)Decrease digoxin dose by 50% and monitor serum digoxin levels as necessary.Diltiazem (HCl)Diltiazem may enhance the bradycardic effect of Amiodarone. Sinus arrest has been reported.MajorMonitor increased therapeutic effects, and potential signs of toxicity (eg, bradycardia, sinus arrest, and decreased cardiac output), of Diltiazem if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased.DisopyramideDisopyramide may enhance the QTc-prolonging effect of Amiodarone. Amiodarone may increase the metabolism, via CYP isoenzymes, of Disopyramide. MajorRapidIncreased risk of ventricular arrhythmias when amiodarone given with disopyramide: avoid combined administration of these two drugs (or only undertaken with caution and appropriate monitoring).ErythromycinAmiodarone increase the risk of ventricular arrhythmia by prolongation of QT interval.Erythromycin is a strong CYP450 3A4 inhibitor and increased serum concentration and inhibit metabolism of amiiodarone.ModerateDelayed (Sequence important)Coadministration of these drugs require clinical monitoring.Flecainide (Acetate)Increased plasma concentration of flecainide. Increased myocardial depression with any anti-arrhythmic. The dose of flacainide should be halved.Flunarizine (HCl)FosphenytoinHalofantrine (HCl)Haloperidolamiodarone cause prolongation of the QT interval in increased risk of ventricular arrythmia,ventricular tachycardia and torsade de pointes because of arrhythmogenic potential related to their effect on cadiac conduction.MajorFrequent use should be avoided.If the symptoms of torsades de pointes occurs patient should advised to seek medical attention.IndacaterolProlong QTc intervalmonitor closelyIodideIodineIoxaglateThe use of iodine-containing contrast media for coronary angiography in patients treated with certain antiarrhythmics such as amiodarone may result in significant prolongation of the QT interval. These contrast agents can be arrhythmogenic when injected into the coronary arteries and may have additive effects on cardiac repolarization when coadministered with antiarrhythmic agents that prolong the QT interval. ModerateCaution is advised if iodine-containing contrast media are used for coronary angiography in patients treated with class IA (e.g., disopyramide, quinidine, procainamide) or class III (e.g., amiodarone, dofetilide, ibutilide, sotalol) antiarrhythmic agents. Increased surveillance and ECG monitoring may be appropriate. Patients who receive outpatient angiographies should be advised to seek medical attention if they experience symptoms that could indicate the occurrence of arrhythmia such as dizziness, palpitations, or syncope. Levobunolol (HCl)Increased risk of bradycardia, AV block, myocardial depression and ventricular arrhythmias when amiodarone is given with beta-blocker (e.g Levobunolol).Liothyronine (Na)Lofepramine (HCl)Theoretical potential for LOFEPRAMINE increasing the ARRHYTHMOGENIC effect of AMIODARONE HYDROCHLORIDE. Major May need to avoid combinationMefloquine (HCl)This combination can prlong the QT interval may result in elevated risk of ventricular arrythmia including ventricular tachycardia and torsade depointes.MajorCautions and clinical monitoring are recommended.MetipranololInfrequent reports of METIPRANOLOL [EYE] increasing the NEGATIVE CHRONOTROPIC effect of AMIODARONE HYDROCHLORIDE. MajorMetoprolol (Tartrate)Amiodarone inhibit first pass hepatic metabolism of metoprolol leads to bradycardia,cardiac arrest and ventricular fibrillation due to additive slowing in AV conduction.ModerateCheck for patient response and hemodynamic ststus is advised.MetrizamideThe use of iodine-containing contrast media for coronary angiography in patients treated with certain antiarrhythmics such as amiodarone may result in significant prolongation of the QT interval. These contrast agents can be arrhythmogenic when injected into the coronary arteries and may have additive effects on cardiac repolarization when coadministered with antiarrhythmic agents that prolong the QT interval.Caution is advised if iodine-containing contrast media are used for coronary angiography in patients treated with class IA (e.g., disopyramide, quinidine, procainamide) or class III (e.g., amiodarone, dofetilide, ibutilide, sotalol) antiarrhythmic agents. Increased surveillance and ECG monitoring may be appropriate. Patients who receive outpatient angiographies should be advised to seek medical attention if they experience symptoms that could indicate the occurrence of arrhythmia such as dizziness, palpitations, or syncope.MexiletineIncreased risk of ventricular arrhythmia when amiodarone given with Mexiletine (HCl). ADVICE: Avoid concomitant use or only undertaken with caution and appropriate monitoring.NelfinavirNelfinavir may decrease the metabolism, via CYP isoenzymes, of Amiodarone. ADVICE:The concomitant use of Nelfinavir and amiodarone should be avoided.MajorNevirapinePentamidineRisk of ventricular arrhythmia is increased by this combination due to dose related prolongation of QT interval.MajorThis combination should be avoided.PhenelzinePhenelzine sulfate may interact with Amiodarone HCl.Phenytoin (Na)Amiodarone inhibits the hepatic metabolism of Phenytoin resulting in an increased plasma concentration of phenytoin.MajorSerum phenytoin concentration should be monitored.Potassium Iodide Prajmalium BitartarateAmiodarone may increase plasma concentration of Prajmalium bitartarate.Procainamide (HCl)Procainamide may enhance the QTc-prolonging effect of Amiodarone. Amiodarone may increase the metabolism, via CYP isoenzymes, of Procainamide. MajorRapidMonitor for decreased cardiac conduction (ie, prolonged QTc) if amiodarone and Procainamide are used concomitantly. Such would increase the risk of developing torsade de pointes. In addition, monitor for increased serum concentrations/toxicity of Procainamide if amiodarone is initiated/dose increased, or decreased serum concentrations/effects if amiodarone is discontinued/dose decreased.Propafenone (HCl)Increased myocardial depression and increased risk of ventricular arrhythmias when amiodarone given with other antiarrhythmics (e.g Propafenon). ADVICE: Avoid concomitant use or only undertaken with caution and appropriate monitoring.QuinidineQuinidine may enhance the QTc-prolonging effect of Amiodarone. Amiodarone may increase the metabolism, via CYP isoenzymes, of Quinidine. MajorRapidIncreased risk of ventricular arrhythmias when amiodarone given with quinidine: avoid combined administration of these two drugs (or only undertaken with caution and appropriate monitoring).QuinineIncreased risk of ventricular arrhythmia when amiodarone given with antimalarials (e.g Quinine). ADVICE: Avoid concomitant use or only undertaken with caution and appropriate monitoring.RitonavirRitonavir may decrease the metabolism, via CYP isoenzymes, of Amiodarone thus increase its plasma concentration resulting in prolong QT interval and ventricular arrhythmias.MajorThis combination is contraindicated.Rubidium IodideSimvastatinIncreased risk of myopathy when amiodarone is given with simvastatin. MajorAvoid doses of simvastatin above 20 mg daily.Sodium IodideSotalol (HCl)Amiodarone may enhance the bradycardic effect of Sotalol. Possibly to the point of cardiac arrest. ADVICE: Avoid concomitant use or only undertaken with caution and apprppriate monitoring.MajorTerfenadineTheophyllineamiodarone cause decrease in metabolism of theophylline leads to theophylline toxicity.Moderatepatients response and tolerance should be monitored.Thyroxine (Na)Verapamil (HCl)Verapamil may enhance the bradycardic effect of Amiodarone. Sinus arrest has been reported.MajorMonitor increased therapeutic effects, and potential signs of toxicity (eg, bradycardia, sinus arrest, and decreased cardiac output) of verapamil.VORICONAZOLEoriconazole may increase the serum concentration of amiodarone by decreasing its metabolism. alternate therpy is recommendedWarfarin (Na)Amiodarone may enhance the anticoagulant effect of Warfarin.MajorDelayedMonitor increased therapeutic effects of Warfarin if amiodarone is initiated/dose increased, or decreased effects if amiodarone is discontinued/dose decreased. An empiric warfarin dosage reduction of 30% to 50% at the initiation of amiodarone might be considered. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, Geriatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj Store at room temperature, Between 15°C-25°C. Protect from Sunlight. Tab Store in a well closed container, Below 40°C. Protect from Sunlight and Moisture.
Warnings
Monitor pulmonary, liver and thyroid function at baseline and during therapy, particularly in patients with history of goiter, thyroid nodules or other dysfunction. Appropriate baseline and periodic evaluation of thyroid function tests is recommended for all patients treated with amiodarone. It is classified as pregnancy category D. It should not be administered during pregnancy.
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