Peringatan Keamanan

The oral LD50 in rats is 1346mg/kg and in mice is 170mg/kg.L8923 The subcutaneous LD50 in rats is 215mg/kg and in mice is 188mg/kg.L8923 The oral TDLO in women is 20mg/kg and in men is 40mg/kg/2W.L8923

Patients experiencing an overdose may present with ECG abnormalities such as a lengthened PR interval, increased QRS duration, prolonged QT interval, increased amplitude of the T wave, reduced myocardial rate and contractility, hypotension, or death.L8878,L5056 Treat patients with symptomatic and supportive treatment which may involve administration of inotropic agents, assisted respiration, circulatory assistance, and acidification of the urine.L8878,L5056 Hemodialysis is not expected to be useful in the removal of flecainide from serum.A186853,L5056

Flecainide

DB01195

small molecule approved withdrawn

Deskripsi

Flecainide is a Class I anti-arrhythmic agent like encainide and propafenone.A186880 Flecainide’s development began in 1966 and was first synthesized in 1972 as an attempt to generate new anesthetics.A186931 It is used to prevent supraventricular and ventricular arrhythmias, as well as paroxysmal atrial fibrillation and flutter.L8878,L5056

Flecainide was granted FDA approval on 31 October 1985.L8875

Struktur Molekul 2D

Berat 414.3427
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy subjects, intravenous flecainide has an average half life of 13 hours for a single dose and 16 hours for multiple oral doses.[A186853,L8878,L5056] In patients with a ventricular premature complex, flecainide has a half life of 20 hours.[A186853,L5056] The half life of meta-O-dealkylated flecainide, a major metabolite of flecainide, is 12.6h.[A186853]
Volume Distribusi The average volume of distribution in 8 male subjects is 5.0-13.4L/kg.[A186853]
Klirens (Clearance) The average clearance of intravenous flecainide is 4.6-12.1mL/min/kg in 8 male subjects.[A186853] For oral flecainide, the clearance was 4-20mL/min/kg.[A186853]

Absorpsi

Oral flecainide has a Tmax of 3-4h and a bioavialability of 90%.A186853,A186931 Taking flecainide with food or aluminum hydroxide antacids do not significantly affect the absorption of flecainide.A186853,L8878,L5056

Metabolisme

Flecainide is mainly metabolized to meta-O-dealkylated flecainide or the meta-O-dealkylated lactam of flecainide.A186853 Meta-O-dealkylated flecainide has 20% the activity of flecainide.A186853 Both of these metabolites are generally detected as glucuronide or sulfate conjugates.A186853 Flecainide’s metabolism involves the action of CYP2D6 and CYP1A2.L5056,A186931

Rute Eliminasi

Approximately 86% of a single oral dose is eliminated in the urine, with 42% as unchanged flecainide and 14% as meta-O-dealkylated flecainide, a similar amount of the meta-O-dealkylated lactam of flecainide, approximately 3% as an unidentified acid metabolite, and <1% as 2 other unknown metabolites.A186853,L8878,L5056 5% is eliminated in the feces.A186853,L5056

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

952 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Flecainide.
Deferasirox The serum concentration of Flecainide can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Flecainide can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Flecainide can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Flecainide can be decreased when it is combined with Teriflunomide.
Ethoxzolamide The excretion of Flecainide can be decreased when combined with Ethoxzolamide.
Methazolamide The excretion of Flecainide can be decreased when combined with Methazolamide.
Acetazolamide The excretion of Flecainide can be decreased when combined with Acetazolamide.
Zonisamide The excretion of Flecainide can be decreased when combined with Zonisamide.
Diclofenamide The excretion of Flecainide can be decreased when combined with Diclofenamide.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Flecainide.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Flecainide.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Flecainide.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Flecainide.
Verapamil The risk or severity of adverse effects can be increased when Verapamil is combined with Flecainide.
Tipranavir The serum concentration of Flecainide can be increased when it is combined with Tipranavir.
Amiodarone The metabolism of Flecainide can be decreased when combined with Amiodarone.
Boceprevir The serum concentration of Flecainide can be increased when it is combined with Boceprevir.
Amprenavir The serum concentration of Flecainide can be increased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Flecainide can be increased when it is combined with Fosamprenavir.
Mirabegron The serum concentration of Flecainide can be increased when it is combined with Mirabegron.
Sodium bicarbonate Sodium bicarbonate may decrease the arrhythmogenic activities of Flecainide.
Abiraterone The metabolism of Flecainide can be decreased when combined with Abiraterone.
Cyproterone acetate The metabolism of Flecainide can be increased when combined with Cyproterone acetate.
Nisoldipine Nisoldipine may increase the arrhythmogenic activities of Flecainide.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Flecainide.
Magnesium sulfate Magnesium sulfate may increase the arrhythmogenic activities of Flecainide.
Tocainide Tocainide may increase the arrhythmogenic activities of Flecainide.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Flecainide.
Carteolol Flecainide may increase the arrhythmogenic activities of Carteolol.
Metipranolol Flecainide may increase the arrhythmogenic activities of Metipranolol.
Dexpropranolol Flecainide may increase the arrhythmogenic activities of Dexpropranolol.
Nimesulide Flecainide may increase the arrhythmogenic activities of Nimesulide.
Cyclandelate Flecainide may increase the arrhythmogenic activities of Cyclandelate.
Seletracetam Flecainide may increase the arrhythmogenic activities of Seletracetam.
Nylidrin Flecainide may increase the arrhythmogenic activities of Nylidrin.
Dotarizine Flecainide may increase the arrhythmogenic activities of Dotarizine.
Xylometazoline Flecainide may increase the arrhythmogenic activities of Xylometazoline.
Fasudil Flecainide may increase the arrhythmogenic activities of Fasudil.
Agmatine Flecainide may increase the arrhythmogenic activities of Agmatine.
Nicorandil Flecainide may increase the arrhythmogenic activities of Nicorandil.
Barnidipine Flecainide may increase the arrhythmogenic activities of Barnidipine.
Azelnidipine Flecainide may increase the arrhythmogenic activities of Azelnidipine.
Cilnidipine Flecainide may increase the arrhythmogenic activities of Cilnidipine.
Darodipine Flecainide may increase the arrhythmogenic activities of Darodipine.
Niludipine Flecainide may increase the arrhythmogenic activities of Niludipine.
Tropisetron Flecainide may increase the arrhythmogenic activities of Tropisetron.
Carboxyamidotriazole Flecainide may increase the arrhythmogenic activities of Carboxyamidotriazole.
Naftopidil Flecainide may increase the arrhythmogenic activities of Naftopidil.
Vinpocetine Flecainide may increase the arrhythmogenic activities of Vinpocetine.
Spiradoline Flecainide may increase the arrhythmogenic activities of Spiradoline.
Cymarin Flecainide may increase the arrhythmogenic activities of Cymarin.
Tiracizine Flecainide may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Flecainide may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine Flecainide may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Flecainide may increase the arrhythmogenic activities of Bioallethrin.
Caroverine Flecainide may increase the arrhythmogenic activities of Caroverine.
Fosfructose Flecainide may increase the arrhythmogenic activities of Fosfructose.
WIN 55212-2 Flecainide may increase the arrhythmogenic activities of WIN 55212-2.
Fish oil Flecainide may increase the arrhythmogenic activities of Fish oil.
Emopamil Flecainide may increase the arrhythmogenic activities of Emopamil.
Lomerizine Flecainide may increase the arrhythmogenic activities of Lomerizine.
Tetrandrine Flecainide may increase the arrhythmogenic activities of Tetrandrine.
Dexniguldipine Flecainide may increase the arrhythmogenic activities of Dexniguldipine.
Fosinoprilat Flecainide may increase the arrhythmogenic activities of Fosinoprilat.
Hydroquinidine Flecainide may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Flecainide may increase the arrhythmogenic activities of SOR-C13.
Dofetilide Dofetilide may increase the arrhythmogenic activities of Flecainide.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Flecainide.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Flecainide.
Terodiline Flecainide may increase the arrhythmogenic activities of Terodiline.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Flecainide.
Atropine Atropine may increase the arrhythmogenic activities of Flecainide.
Adenosine Adenosine may increase the arrhythmogenic activities of Flecainide.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Flecainide.
Prenylamine Flecainide may increase the arrhythmogenic activities of Prenylamine.
Fluspirilene Flecainide may increase the arrhythmogenic activities of Fluspirilene.
Azimilide Flecainide may increase the arrhythmogenic activities of Azimilide.
Tedisamil Flecainide may increase the arrhythmogenic activities of Tedisamil.
Nilvadipine Flecainide may increase the arrhythmogenic activities of Nilvadipine.
Fendiline Flecainide may increase the arrhythmogenic activities of Fendiline.
Eperisone Flecainide may increase the arrhythmogenic activities of Eperisone.
Benidipine Flecainide may increase the arrhythmogenic activities of Benidipine.
Simendan Flecainide may increase the arrhythmogenic activities of Simendan.
Otilonium Flecainide may increase the arrhythmogenic activities of Otilonium.
Nizofenone Flecainide may increase the arrhythmogenic activities of Nizofenone.
Bunaftine Flecainide may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Flecainide may increase the arrhythmogenic activities of Lorcainide.
Penfluridol Flecainide may increase the arrhythmogenic activities of Penfluridol.
Dexverapamil Flecainide may increase the arrhythmogenic activities of Dexverapamil.
Isradipine Isradipine may increase the arrhythmogenic activities of Flecainide.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Flecainide.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Flecainide.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Flecainide.
Ethosuximide Ethosuximide may increase the arrhythmogenic activities of Flecainide.
Losartan Losartan may increase the arrhythmogenic activities of Flecainide.
Moricizine Moricizine may increase the arrhythmogenic activities of Flecainide.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Flecainide.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Flecainide.
Bretylium Bretylium may increase the arrhythmogenic activities of Flecainide.

Target Protein

Sodium channel protein type 4 subunit alpha SCN4A
Sodium channel protein type 5 subunit alpha SCN5A
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
Ryanodine receptor 2 RYR2

Referensi & Sumber

Synthesis reference: Bmitt, E.H. and Brown, W.R.; U.S. Patent 3,900,481; August 19,1975; assigned to Riker Laboratories, Inc.
Artikel (PubMed)
  • PMID: 1449923
    Gill JS, Mehta D, Ward DE, Camm AJ: Efficacy of flecainide, sotalol, and verapamil in the treatment of right ventricular tachycardia in patients without overt cardiac abnormality. Br Heart J. 1992 Oct;68(4):392-7.
  • PMID: 2115193
    Sakurada H, Hiyoshi Y, Tejima T, Yanase O, Tokuyasu Y, Watanabe K, Motomiya T, Sugiura M, Hiraoka M: Effects of oral flecainide treatment of refractory tachyarrhythmias. Kokyu To Junkan. 1990 May;38(5):471-6.
  • PMID: 1900101
    Echt DS, Liebson PR, Mitchell LB, Peters RW, Obias-Manno D, Barker AH, Arensberg D, Baker A, Friedman L, Greene HL, et al.: Mortality and morbidity in patients receiving encainide, flecainide, or placebo. The Cardiac Arrhythmia Suppression Trial. N Engl J Med. 1991 Mar 21;324(12):781-8.
  • PMID: 8541168
    Greenberg HM, Dwyer EM Jr, Hochman JS, Steinberg JS, Echt DS, Peters RW: Interaction of ischaemia and encainide/flecainide treatment: a proposed mechanism for the increased mortality in CAST I. Br Heart J. 1995 Dec;74(6):631-5.
  • PMID: 12687841
    Gasparini M, Priori SG, Mantica M, Napolitano C, Galimberti P, Ceriotti C, Simonini S: Flecainide test in Brugada syndrome: a reproducible but risky tool. Pacing Clin Electrophysiol. 2003 Jan;26(1 Pt 2):338-41.
  • PMID: 6364769
    Conard GJ, Ober RE: Metabolism of flecainide. Am J Cardiol. 1984 Feb 27;53(5):41B-51B. doi: 10.1016/0002-9149(84)90501-0.
  • PMID: 2499646
    Abi Samra F: The clinical use of class IC antiarrhythmic drugs. J La State Med Soc. 1989 May;141(5):27-31.
  • PMID: 25870032
    Tamargo J, Le Heuzey JY, Mabo P: Narrow therapeutic index drugs: a clinical pharmacological consideration to flecainide. Eur J Clin Pharmacol. 2015 May;71(5):549-67. doi: 10.1007/s00228-015-1832-0. Epub 2015 Apr 15.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 114 • International brands: 2
Produk
  • Ag-flecainide
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Ag-flecainide
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Apo-flecainide
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Apo-flecainide
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Auro-flecainide
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Auro-flecainide
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Flecainide
    Tablet • 50 mg • Oral • Canada • Approved
  • Flecainide
    Tablet • 100 mg • Oral • Canada • Approved
Menampilkan 8 dari 114 produk.
International Brands
  • Almarytm
  • Apocard

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