Peringatan Keamanan

The LD50 of oral amiodarone in mice and rats exceeds 3,000 mg/kg.L3561
An overdose with amiodarone can have a fatal outcome due to its potential to cause arrhythmia. Signs or symptoms of an overdose may include, hypotension, shock, bradycardia, AV block, and liver toxicity. In cases of an overdose, initiate supportive treatment and, if needed, use fluids, vasopressors, or positive inotropic agents. Temporary pacing may be required for heart block. Ensure to monitor liver function regularly. Amiodarone and its main metabolite, DEA, are not removable by dialysis.L8087

Amiodarone

DB01118

small molecule approved investigational

Deskripsi

Amiodarone is a benzofuran derivative, anti-arrhythmic drug used commonly in a variety of settings.A36817 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.L3561,L11265,L11286

Struktur Molekul 2D

Berat 645.3116
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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. [A1903,A189666] According to the prescribing information for amiodarone, the average apparent plasma terminal elimination half-life of amiodarone is of 58 days (ranging from 15 to 142 days). The terminal half-life range was between 14 to 75 days for the active metabolite, (DEA).[L3561] The plasma half-life of amiodarone after one dose ranges from 3.2 to 79.7 hours, according to one source.[A36817]
Volume Distribusi 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.[A183140] Prescribing information mentions that the volume of distribution of amiodarone varies greatly, with a mean distribution of approximately 60 L/kg. It accumulates throughout the body, especially in adipose tissue[A36817] and highly vascular organs including the lung, liver, and spleen. One major metabolite of amiodarone, desethylamiodarone (DEA), is found in even higher proportions in the same tissues as amiodarone.[L3561]
Klirens (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.[L3561] Another study determined that the total body clearance of amiodarone varies from 0.10 to 0.77 L/min after one intravenous dose.[A36817] Renal impairment does not appear to affect the clearance of amiodarone, but hepatic impairment may reduce clearance. Patients with liver cirrhosis exhibited significantly lower Cmax and mean amiodarone concentration for DEA, but not for amiodarone. Severe left ventricular dysfunction prolongs the half-life of DEA.[L3561] A note on monitoring No guidelines have been developed for adjusting the dose of amiodarone in renal, hepatic, or cardiac abnormalities. In patients on chronic amiodarone treatment, close clinical monitoring is advisable, especially for elderly patients and those with severe left ventricular dysfunction.[L3561]

Absorpsi

The Cmax of amiodarone in the plasma is achieved about 3 to 7 hours after administration.L3561 The general time to onset of action of amiodarone after one dose given by the intravenous route is between 1 and 30 minutes, with therapeutic effects lasting from 1-3 hours. Steady-state concentrations of amiodarone in the plasma ranges between 0.4 to 11.99 ?g/ml; it is advisable that steady-state levels are generally maintained between 1.0 and 2.5 ?g/ml in patients with arrhythmias.A36817,A183137 Interestingly, its onset of action may sometimes begin after 2 to 3 days, but frequently takes 1 to 3 weeks, despite the administration of higher loading doses.L3561 The bioavailability of amiodarone varies in clinical studies, averaging between 35 and 65%.L3561 Effect of food In healthy subjects who were given a single 600-mg dose immediately after consuming a meal high in fat, the AUC of amiodarone increased by 2.3 and the Cmax by 3.8 times.L3561 Food also enhances absorption, reducing the Tmax by about 37%.L3561

Metabolisme

This drug is metabolized to the main metabolite desethylamiodarone (DEA)A36817 by the CYP3A4 and CYP2C8 enzymes. The CYP3A4 enzyme is found in the liver and intestines.L3561 A hydroxyl metabolite of DEA has been identified in mammals, but its clinical significance is unknown.A189829

Rute Eliminasi

Amiodarone is eliminated primarily by hepatic metabolism and biliary excretion.A36817 A small amount of desethylamiodarone (DEA) is found in the urine.L3561

Farmakogenomik

1 Varian
KCNH2 (None)

The presence of polymorphisms in KCNH2 and KCNE2 may potentially be associated with increased susceptibility to long Q-T syndrome or cardiac arrhytmia when treated with amiodarone.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of amiodarone.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of amiodarone. Therefore it may reduce the serum concentration and effectiveness of amiodarone.
  • 3. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1893 Data
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Amiodarone is combined with Levodopa.
Risperidone Amiodarone may increase the hypotensive activities of Risperidone.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Amiodarone.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Amiodarone.
Armodafinil The metabolism of Amiodarone can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Amiodarone.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Amiodarone.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Amiodarone.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Amiodarone.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Amiodarone.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Amiodarone.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Amiodarone.
Silodosin The excretion of Silodosin can be decreased when combined with Amiodarone.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Amiodarone.
Agalsidase beta The therapeutic efficacy of Agalsidase beta can be decreased when used in combination with Amiodarone.
Ceritinib Amiodarone may increase the bradycardic activities of Ceritinib.
Ivabradine Amiodarone may increase the bradycardic activities of Ivabradine.
Esmolol The therapeutic efficacy of Esmolol can be increased when used in combination with Amiodarone.
Betaxolol The therapeutic efficacy of Betaxolol can be increased when used in combination with Amiodarone.
Metoprolol The therapeutic efficacy of Metoprolol can be increased when used in combination with Amiodarone.
Atenolol The therapeutic efficacy of Atenolol can be increased when used in combination with Amiodarone.
Sotalol The therapeutic efficacy of Sotalol can be increased when used in combination with Amiodarone.
Propranolol The therapeutic efficacy of Propranolol can be increased when used in combination with Amiodarone.
Labetalol The therapeutic efficacy of Labetalol can be increased when used in combination with Amiodarone.
Alprenolol The therapeutic efficacy of Alprenolol can be increased when used in combination with Amiodarone.
Pindolol The therapeutic efficacy of Pindolol can be increased when used in combination with Amiodarone.
Carvedilol The therapeutic efficacy of Carvedilol can be increased when used in combination with Amiodarone.
Acebutolol The therapeutic efficacy of Acebutolol can be increased when used in combination with Amiodarone.
Nadolol The therapeutic efficacy of Nadolol can be increased when used in combination with Amiodarone.
Bevantolol The therapeutic efficacy of Bevantolol can be increased when used in combination with Amiodarone.
Practolol The therapeutic efficacy of Practolol can be increased when used in combination with Amiodarone.
Penbutolol The therapeutic efficacy of Penbutolol can be increased when used in combination with Amiodarone.
Oxprenolol The therapeutic efficacy of Oxprenolol can be increased when used in combination with Amiodarone.
Dexpropranolol The therapeutic efficacy of Dexpropranolol can be increased when used in combination with Amiodarone.
Celiprolol The therapeutic efficacy of Celiprolol can be increased when used in combination with Amiodarone.
Nebivolol The therapeutic efficacy of Nebivolol can be increased when used in combination with Amiodarone.
Bufuralol The therapeutic efficacy of Bufuralol can be increased when used in combination with Amiodarone.
Bopindolol The therapeutic efficacy of Bopindolol can be increased when used in combination with Amiodarone.
Bupranolol The therapeutic efficacy of Bupranolol can be increased when used in combination with Amiodarone.
Indenolol The therapeutic efficacy of Indenolol can be increased when used in combination with Amiodarone.
Arotinolol The therapeutic efficacy of Arotinolol can be increased when used in combination with Amiodarone.
Levobetaxolol The therapeutic efficacy of Levobetaxolol can be increased when used in combination with Amiodarone.
Talinolol The therapeutic efficacy of Talinolol can be increased when used in combination with Amiodarone.
Anisodamine The therapeutic efficacy of Anisodamine can be increased when used in combination with Amiodarone.
Bucindolol The therapeutic efficacy of Bucindolol can be increased when used in combination with Amiodarone.
Esatenolol The therapeutic efficacy of Esatenolol can be increased when used in combination with Amiodarone.
Cloranolol The therapeutic efficacy of Cloranolol can be increased when used in combination with Amiodarone.
Mepindolol The therapeutic efficacy of Mepindolol can be increased when used in combination with Amiodarone.
Epanolol The therapeutic efficacy of Epanolol can be increased when used in combination with Amiodarone.
Tertatolol The therapeutic efficacy of Tertatolol can be increased when used in combination with Amiodarone.
Timolol The therapeutic efficacy of Timolol can be increased when used in combination with Amiodarone.
Bisoprolol The therapeutic efficacy of Bisoprolol can be increased when used in combination with Amiodarone.
Landiolol The therapeutic efficacy of Landiolol can be increased when used in combination with Amiodarone.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Amiodarone.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Amiodarone.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Amiodarone.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Amiodarone.
Fingolimod Fingolimod may increase the arrhythmogenic activities of Amiodarone.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Amiodarone.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Amiodarone.
Iloperidone The risk or severity of QTc prolongation can be increased when Amiodarone is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Amiodarone.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Amiodarone.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Amiodarone.
Pravastatin The metabolism of Pravastatin can be increased when combined with Amiodarone.
Cerivastatin The metabolism of Cerivastatin can be increased when combined with Amiodarone.
Fluvastatin The metabolism of Fluvastatin can be increased when combined with Amiodarone.
Rosuvastatin The metabolism of Rosuvastatin can be increased when combined with Amiodarone.
Mevastatin The metabolism of Mevastatin can be increased when combined with Amiodarone.
Pitavastatin The metabolism of Pitavastatin can be increased when combined with Amiodarone.
Efavirenz The serum concentration of Amiodarone can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Amiodarone can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Amiodarone can be decreased when used in combination with Nafcillin.
Nitroprusside Amiodarone may increase the hypotensive activities of Nitroprusside.
Disopyramide Amiodarone may increase the QTc-prolonging activities of Disopyramide.
Ajmaline Amiodarone may increase the QTc-prolonging activities of Ajmaline.
Sparteine Amiodarone may increase the QTc-prolonging activities of Sparteine.
Cibenzoline Amiodarone may increase the QTc-prolonging activities of Cibenzoline.
Prajmaline Amiodarone may increase the QTc-prolonging activities of Prajmaline.
Lorajmine Amiodarone may increase the QTc-prolonging activities of Lorajmine.
Hydroquinidine Amiodarone may increase the QTc-prolonging activities of Hydroquinidine.
Lidocaine The risk or severity of generalized seizure and bradycardia can be increased when Amiodarone is combined with Lidocaine.
Metreleptin The metabolism of Amiodarone can be increased when combined with Metreleptin.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Amiodarone.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Amiodarone.
Lithium citrate The risk or severity of adverse effects can be increased when Amiodarone is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Amiodarone is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Amiodarone is combined with Lithium hydroxide.
Colestipol The excretion of Amiodarone can be increased when combined with Colestipol.
Sevelamer The excretion of Amiodarone can be increased when combined with Sevelamer.
Colesevelam The excretion of Amiodarone can be increased when combined with Colesevelam.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Amiodarone.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Amiodarone.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Amiodarone.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Amiodarone.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Amiodarone.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Amiodarone.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Amiodarone.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Amiodarone.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Amiodarone.

Target Protein

HERG human cardiac K+ channel KCNH2
Beta adrenergic receptor ADRB1
Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I
Voltage gated L-type calcium channel CACNA1C
Thyroid hormone receptor THRA
Peroxisome proliferator-activated receptor gamma PPARG
Peroxisome proliferator-activated receptor alpha PPARA
Peroxisome proliferator-activated receptor gamma coactivator 1-beta PPARGC1B

Referensi & Sumber

Synthesis reference: M.J.A. Walker, P.P.S. Therapeutic Areas I: Central Nervous System, Pain, Metabolic Syndrome, Urology, Gastrointestinal and Cardiovascular: Amiodarone. Comprehensive Medicinal Chemistry II, 2007
Artikel (PubMed)
  • PMID: 5485142
    Singh BN, Vaughan Williams EM: The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br J Pharmacol. 1970 Aug;39(4):657-67.
  • PMID: 793369
    Rosenbaum MB, Chiale PA, Halpern MS, Nau GJ, Przybylski J, Levi RJ, Lazzari JO, Elizari MV: Clinical efficacy of amiodarone as an antiarrhythmic agent. Am J Cardiol. 1976 Dec;38(7):934-44.
  • PMID: 6613843
    Rosenbaum MB, Chiale PA, Haedo A, Lazzari JO, Elizari MV: Ten years of experience with amiodarone. Am Heart J. 1983 Oct;106(4 Pt 2):957-64.
  • PMID: 6370540
    Latini R, Tognoni G, Kates RE: Clinical pharmacokinetics of amiodarone. Clin Pharmacokinet. 1984 Mar-Apr;9(2):136-56. doi: 10.2165/00003088-198409020-00002.
  • PMID: 6368644
    Zipes DP, Prystowsky EN, Heger JJ: Amiodarone: electrophysiologic actions, pharmacokinetics and clinical effects. J Am Coll Cardiol. 1984 Apr;3(4):1059-71. doi: 10.1016/s0735-1097(84)80367-8.
  • PMID: 6175810
    Riva E, Gerna M, Latini R, Giani P, Volpi A, Maggioni A: Pharmacokinetics of amiodarone in man. J Cardiovasc Pharmacol. 1982 Mar-Apr;4(2):264-9. doi: 10.1097/00005344-198203000-00015.
  • PMID: 1753010
    Freedman MD, Somberg JC: Pharmacology and pharmacokinetics of amiodarone. J Clin Pharmacol. 1991 Nov;31(11):1061-9. doi: 10.1002/j.1552-4604.1991.tb03673.x.
  • PMID: 7426165
    Rowland E, Krikler DM: Electrophysiological assessment of amiodarone in treatment of resistant supraventricular arrhythmias. Br Heart J. 1980 Jul;44(1):82-90. doi: 10.1136/hrt.44.1.82.
Menampilkan 8 dari 15 artikel.

Contoh Produk & Brand

Produk: 201 • International brands: 5
Produk
  • Amiodarone
    Tablet • 200 mg • Oral • Canada • Approved
  • Amiodarone
    Tablet • 200 mg • Oral • Canada • Approved
  • Amiodarone
    Tablet • 200 mg • Oral • Canada • Approved
  • Amiodarone for Injection 50mg/ml
    Solution • 50 mg / mL • Intravenous • Canada • Approved
  • Amiodarone Hci
    Injection, solution • 50 mg/1mL • Intravenous • US • Generic • Approved
  • Amiodarone HCl
    Injection, solution • 1.8 mg/1mL • Intravenous • US
  • Amiodarone HCl
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Amiodarone HCl
    Tablet • 400 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 201 produk.
International Brands
  • Amio-Aqueous IV
  • Aratac
  • Arycor
  • Atlansil
  • Tachyra

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