Peringatan Keamanan

Some common unwanted effects include hypotension, ventricular arrhythmias, bradycardia, atrial flutter, dysgeusia, paraesthesia, dizziness and nausea.

Vernakalant

DB06217

small molecule approved investigational

Deskripsi

Vernakalant was developed by Cardiome Pharma as as an antiarrhythmic drug intended for rapid conversion of atrial fibrillation to sinus rhythm. It acts as an atypical class III antiarrhythmic drug that potentiates its effect in higher heart rates. Intravenous formulation was approved in Europe in September 2010 as Brinavess and in Canada in April 2017. It is an investigational drug under regulatory review by FDA.

Struktur Molekul 2D

Berat 349.471
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination half life in CYP2D6 extensive metabolizers is 3 hours and 5.5 hours in poor metabolizers.
Volume Distribusi Approximately 2L/kg.
Klirens (Clearance) The typical total body clearance of vernakalant was estimated to be 0.41 l/hr/kg.

Absorpsi

In patients, average peak plasma concentrations of vernakalant were 3.9 ?g/ml following a single 10 minute infusion of 3 mg/kg vernakalant hydrochloride, and 4.3 ?g/ml following a second infusion of 2 mg/kg with a 15 minute interval between doses L765.

Metabolisme

Vernakalant is mainly eliminated by CYP2D6 mediated O-demethylation in CYP2D6 extensive metabolisers. Glucuronidation is the main metabolism pathway in CYP2D6 poor metabolisers.

Rute Eliminasi

Mainly eliminated via renal excretion.

Interaksi Obat

659 Data
Fingolimod Fingolimod may increase the arrhythmogenic activities of Vernakalant.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Vernakalant.
Mirabegron The serum concentration of Vernakalant can be increased when it is combined with Mirabegron.
Nisoldipine Nisoldipine may increase the arrhythmogenic activities of Vernakalant.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Vernakalant.
Magnesium sulfate Magnesium sulfate may increase the arrhythmogenic activities of Vernakalant.
Tocainide Tocainide may increase the arrhythmogenic activities of Vernakalant.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Vernakalant.
Dexpropranolol Dexpropranolol may increase the arrhythmogenic activities of Vernakalant.
Nimesulide Nimesulide may increase the arrhythmogenic activities of Vernakalant.
Cyclandelate Cyclandelate may increase the arrhythmogenic activities of Vernakalant.
Seletracetam Seletracetam may increase the arrhythmogenic activities of Vernakalant.
Nylidrin Nylidrin may increase the arrhythmogenic activities of Vernakalant.
Carteolol Vernakalant may increase the arrhythmogenic activities of Carteolol.
Metipranolol Vernakalant may increase the arrhythmogenic activities of Metipranolol.
Dotarizine Vernakalant may increase the arrhythmogenic activities of Dotarizine.
Xylometazoline Vernakalant may increase the arrhythmogenic activities of Xylometazoline.
Tranilast Vernakalant may increase the arrhythmogenic activities of Tranilast.
Fasudil Vernakalant may increase the arrhythmogenic activities of Fasudil.
Agmatine Vernakalant may increase the arrhythmogenic activities of Agmatine.
Nicorandil Vernakalant may increase the arrhythmogenic activities of Nicorandil.
Barnidipine Vernakalant may increase the arrhythmogenic activities of Barnidipine.
Azelnidipine Vernakalant may increase the arrhythmogenic activities of Azelnidipine.
Cilnidipine Vernakalant may increase the arrhythmogenic activities of Cilnidipine.
Darodipine Vernakalant may increase the arrhythmogenic activities of Darodipine.
Niludipine Vernakalant may increase the arrhythmogenic activities of Niludipine.
Tropisetron Vernakalant may increase the arrhythmogenic activities of Tropisetron.
Carboxyamidotriazole Vernakalant may increase the arrhythmogenic activities of Carboxyamidotriazole.
Naftopidil Vernakalant may increase the arrhythmogenic activities of Naftopidil.
Vinpocetine Vernakalant may increase the arrhythmogenic activities of Vinpocetine.
Spiradoline Vernakalant may increase the arrhythmogenic activities of Spiradoline.
Cymarin Vernakalant may increase the arrhythmogenic activities of Cymarin.
Metildigoxin Vernakalant may increase the arrhythmogenic activities of Metildigoxin.
Tiracizine Vernakalant may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Vernakalant may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine Vernakalant may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Vernakalant may increase the arrhythmogenic activities of Bioallethrin.
Caroverine Vernakalant may increase the arrhythmogenic activities of Caroverine.
Fosfructose Vernakalant may increase the arrhythmogenic activities of Fosfructose.
WIN 55212-2 Vernakalant may increase the arrhythmogenic activities of WIN 55212-2.
Fish oil Vernakalant may increase the arrhythmogenic activities of Fish oil.
Emopamil Vernakalant may increase the arrhythmogenic activities of Emopamil.
Lomerizine Vernakalant may increase the arrhythmogenic activities of Lomerizine.
Tetrandrine Vernakalant may increase the arrhythmogenic activities of Tetrandrine.
Dexniguldipine Vernakalant may increase the arrhythmogenic activities of Dexniguldipine.
Fosinoprilat Vernakalant may increase the arrhythmogenic activities of Fosinoprilat.
Hydroquinidine Vernakalant may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Vernakalant may increase the arrhythmogenic activities of SOR-C13.
Betaxolol Betaxolol may increase the arrhythmogenic activities of Vernakalant.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Vernakalant.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Vernakalant.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Vernakalant.
Propranolol Propranolol may increase the arrhythmogenic activities of Vernakalant.
Atropine Atropine may increase the arrhythmogenic activities of Vernakalant.
Adenosine Adenosine may increase the arrhythmogenic activities of Vernakalant.
Loperamide Loperamide may increase the arrhythmogenic activities of Vernakalant.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Vernakalant.
Nifedipine Nifedipine may increase the arrhythmogenic activities of Vernakalant.
Acebutolol Acebutolol may increase the arrhythmogenic activities of Vernakalant.
Mibefradil Mibefradil may increase the arrhythmogenic activities of Vernakalant.
Oxprenolol Oxprenolol may increase the arrhythmogenic activities of Vernakalant.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Vernakalant.
Fluspirilene Fluspirilene may increase the arrhythmogenic activities of Vernakalant.
Azimilide Azimilide may increase the arrhythmogenic activities of Vernakalant.
Tedisamil Tedisamil may increase the arrhythmogenic activities of Vernakalant.
Nilvadipine Vernakalant may increase the arrhythmogenic activities of Nilvadipine.
Indenolol Vernakalant may increase the arrhythmogenic activities of Indenolol.
Fendiline Vernakalant may increase the arrhythmogenic activities of Fendiline.
Eperisone Vernakalant may increase the arrhythmogenic activities of Eperisone.
Melperone Vernakalant may increase the arrhythmogenic activities of Melperone.
Benidipine Vernakalant may increase the arrhythmogenic activities of Benidipine.
Simendan Vernakalant may increase the arrhythmogenic activities of Simendan.
Otilonium Vernakalant may increase the arrhythmogenic activities of Otilonium.
Nizofenone Vernakalant may increase the arrhythmogenic activities of Nizofenone.
Bunaftine Vernakalant may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Vernakalant may increase the arrhythmogenic activities of Lorcainide.
Penfluridol Vernakalant may increase the arrhythmogenic activities of Penfluridol.
Dexverapamil Vernakalant may increase the arrhythmogenic activities of Dexverapamil.
Dofetilide Dofetilide may increase the arrhythmogenic activities of Vernakalant.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Vernakalant.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Vernakalant.
Quinidine Quinidine may increase the arrhythmogenic activities of Vernakalant.
Bepridil Bepridil may increase the arrhythmogenic activities of Vernakalant.
Terodiline Vernakalant may increase the arrhythmogenic activities of Terodiline.
Isradipine Isradipine may increase the arrhythmogenic activities of Vernakalant.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Vernakalant.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Vernakalant.
Digoxin Digoxin may increase the arrhythmogenic activities of Vernakalant.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Vernakalant.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Vernakalant.
Ethosuximide Ethosuximide may increase the arrhythmogenic activities of Vernakalant.
Verapamil Verapamil may increase the arrhythmogenic activities of Vernakalant.
Losartan Losartan may increase the arrhythmogenic activities of Vernakalant.
Moricizine Moricizine may increase the arrhythmogenic activities of Vernakalant.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Vernakalant.
Zonisamide Zonisamide may increase the arrhythmogenic activities of Vernakalant.
Felodipine Felodipine may increase the arrhythmogenic activities of Vernakalant.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Vernakalant.
Bretylium Bretylium may increase the arrhythmogenic activities of Vernakalant.
Digitoxin Digitoxin may increase the arrhythmogenic activities of Vernakalant.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A
Potassium voltage-gated channel subfamily A member 5 KCNA5
A-type voltage-gated potassium channel KCND3 KCND3
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18447605
    Naccarelli GV, Wolbrette DL, Samii S, Banchs JE, Penny-Peterson E, Stevenson R, Gonzalez MD: Vernakalant--a promising therapy for conversion of recent-onset atrial fibrillation. Expert Opin Investig Drugs. 2008 May;17(5):805-10. doi: 10.1517/13543784.17.5.805 .
  • PMID: 18334607
    Cheng JW: Vernakalant in the management of atrial fibrillation. Ann Pharmacother. 2008 Apr;42(4):533-42. doi: 10.1345/aph.1K542. Epub 2008 Mar 11.
  • PMID: 17666913
    Dorian P, Pinter A, Mangat I, Korley V, Cvitkovic SS, Beatch GN: The effect of vernakalant (RSD1235), an investigational antiarrhythmic agent, on atrial electrophysiology in humans. J Cardiovasc Pharmacol. 2007 Jul;50(1):35-40.
  • PMID: 16545351
    Orth PM, Hesketh JC, Mak CK, Yang Y, Lin S, Beatch GN, Ezrin AM, Fedida D: RSD1235 blocks late INa and suppresses early afterdepolarizations and torsades de pointes induced by class III agents. Cardiovasc Res. 2006 Jun 1;70(3):486-96. Epub 2006 Feb 14.
  • PMID: 24108230
    Savelieva I, Graydon R, Camm AJ: Pharmacological cardioversion of atrial fibrillation with vernakalant: evidence in support of the ESC Guidelines. Europace. 2014 Feb;16(2):162-73. doi: 10.1093/europace/eut274. Epub 2013 Oct 9.
  • PMID: 24821654
    Camm AJ: The vernakalant story: how did it come to approval in Europe and what is the delay in the U.S.A? Curr Cardiol Rev. 2014 Nov;10(4):309-14.
  • PMID: 23637539
    Tsuji Y, Dobrev D: Safety and efficacy of vernakalant for acute cardioversion of atrial fibrillation: an update. Vasc Health Risk Manag. 2013;9:165-75. doi: 10.2147/VHRM.S43720. Epub 2013 Apr 23.
  • PMID: 20592320
    Finnin M: Vernakalant: A novel agent for the termination of atrial fibrillation. Am J Health Syst Pharm. 2010 Jul 15;67(14):1157-64. doi: 10.2146/ajhp080501.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Brinavess
    Solution • 20 mg / mL • Intravenous • Canada • Approved
  • Brinavess
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU • Approved
  • Brinavess
    Injection, solution, concentrate • 20 mg/ml • Intravenous • EU • Approved
International Brands
  • Kynapid — Cardiome Pharma Corp.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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