Levosimendan

DB00922

small molecule approved investigational

Deskripsi

Levosimendan increases calcium sensitivity to myocytes by binding to troponin C in a calcium dependent manner. This increases contractility without raising calcium levels. It also relaxes vascular smooth muscle by opening adenosine triphosphate sensitive potassium channels. Levosimendan is used to manage acutely decompensated congestive heart failure.

Struktur Molekul 2D

Berat 280.2847
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Eliminination half-life is approximately 1 hour.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The bioavailability of oral levosimendan is 85 ± 6% in healthy volunteers and 84 ± 4% in patients.

Metabolisme

Complete metabolism, with some active metabolites (OR-1855 and OR-1896) possibly extending the drug's haemodynamic effects.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

668 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Levosimendan.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Levosimendan is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Levosimendan is combined with Levodopa.
Risperidone Levosimendan may increase the hypotensive activities of Risperidone.
Nicorandil Nicorandil may increase the hypotensive activities of Levosimendan.
Lidocaine Lidocaine may increase the arrhythmogenic activities of Levosimendan.
Mexiletine Mexiletine may increase the arrhythmogenic activities of Levosimendan.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Levosimendan.
Magnesium sulfate Magnesium sulfate may increase the arrhythmogenic activities of Levosimendan.
Carteolol Levosimendan may increase the arrhythmogenic activities of Carteolol.
Tocainide Levosimendan may increase the arrhythmogenic activities of Tocainide.
Deslanoside Levosimendan may increase the arrhythmogenic activities of Deslanoside.
Metipranolol Levosimendan may increase the arrhythmogenic activities of Metipranolol.
Aprindine Levosimendan may increase the arrhythmogenic activities of Aprindine.
Nimesulide Levosimendan may increase the arrhythmogenic activities of Nimesulide.
Cyclandelate Levosimendan may increase the arrhythmogenic activities of Cyclandelate.
Flunarizine Levosimendan may increase the arrhythmogenic activities of Flunarizine.
Seletracetam Levosimendan may increase the arrhythmogenic activities of Seletracetam.
Nylidrin Levosimendan may increase the arrhythmogenic activities of Nylidrin.
Dotarizine Levosimendan may increase the arrhythmogenic activities of Dotarizine.
Xylometazoline Levosimendan may increase the arrhythmogenic activities of Xylometazoline.
Sparteine Levosimendan may increase the arrhythmogenic activities of Sparteine.
Tranilast Levosimendan may increase the arrhythmogenic activities of Tranilast.
Fasudil Levosimendan may increase the arrhythmogenic activities of Fasudil.
Agmatine Levosimendan may increase the arrhythmogenic activities of Agmatine.
Azelnidipine Levosimendan may increase the arrhythmogenic activities of Azelnidipine.
Darodipine Levosimendan may increase the arrhythmogenic activities of Darodipine.
Niludipine Levosimendan may increase the arrhythmogenic activities of Niludipine.
Tropisetron Levosimendan may increase the arrhythmogenic activities of Tropisetron.
Carboxyamidotriazole Levosimendan may increase the arrhythmogenic activities of Carboxyamidotriazole.
Vinpocetine Levosimendan may increase the arrhythmogenic activities of Vinpocetine.
Spiradoline Levosimendan may increase the arrhythmogenic activities of Spiradoline.
Cymarin Levosimendan may increase the arrhythmogenic activities of Cymarin.
Metildigoxin Levosimendan may increase the arrhythmogenic activities of Metildigoxin.
Tiracizine Levosimendan may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Levosimendan may increase the arrhythmogenic activities of Ethacizine.
Hydroquinine Levosimendan may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Levosimendan may increase the arrhythmogenic activities of Bioallethrin.
Tertatolol Levosimendan may increase the arrhythmogenic activities of Tertatolol.
Caroverine Levosimendan may increase the arrhythmogenic activities of Caroverine.
Fosfructose Levosimendan may increase the arrhythmogenic activities of Fosfructose.
WIN 55212-2 Levosimendan may increase the arrhythmogenic activities of WIN 55212-2.
Fish oil Levosimendan may increase the arrhythmogenic activities of Fish oil.
Emopamil Levosimendan may increase the arrhythmogenic activities of Emopamil.
Lomerizine Levosimendan may increase the arrhythmogenic activities of Lomerizine.
Tetrandrine Levosimendan may increase the arrhythmogenic activities of Tetrandrine.
Hydroquinidine Levosimendan may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Levosimendan may increase the arrhythmogenic activities of SOR-C13.
Dofetilide Dofetilide may increase the arrhythmogenic activities of Levosimendan.
Disopyramide Disopyramide may increase the arrhythmogenic activities of Levosimendan.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Levosimendan.
Sotalol Sotalol may increase the arrhythmogenic activities of Levosimendan.
Quinidine Quinidine may increase the arrhythmogenic activities of Levosimendan.
Procainamide Levosimendan may increase the arrhythmogenic activities of Procainamide.
Bepridil Levosimendan may increase the arrhythmogenic activities of Bepridil.
Dronedarone Levosimendan may increase the arrhythmogenic activities of Dronedarone.
Terodiline Levosimendan may increase the arrhythmogenic activities of Terodiline.
Betaxolol Betaxolol may increase the arrhythmogenic activities of Levosimendan.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Levosimendan.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Levosimendan.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Levosimendan.
Propranolol Propranolol may increase the arrhythmogenic activities of Levosimendan.
Atropine Atropine may increase the arrhythmogenic activities of Levosimendan.
Adenosine Adenosine may increase the arrhythmogenic activities of Levosimendan.
Loperamide Loperamide may increase the arrhythmogenic activities of Levosimendan.
Nifedipine Levosimendan may increase the arrhythmogenic activities of Nifedipine.
Propafenone Levosimendan may increase the arrhythmogenic activities of Propafenone.
Acebutolol Levosimendan may increase the arrhythmogenic activities of Acebutolol.
Flecainide Levosimendan may increase the arrhythmogenic activities of Flecainide.
Mibefradil Levosimendan may increase the arrhythmogenic activities of Mibefradil.
Oxprenolol Levosimendan may increase the arrhythmogenic activities of Oxprenolol.
Prenylamine Levosimendan may increase the arrhythmogenic activities of Prenylamine.
Fluspirilene Levosimendan may increase the arrhythmogenic activities of Fluspirilene.
Azimilide Levosimendan may increase the arrhythmogenic activities of Azimilide.
Tedisamil Levosimendan may increase the arrhythmogenic activities of Tedisamil.
Nilvadipine Levosimendan may increase the arrhythmogenic activities of Nilvadipine.
Fendiline Levosimendan may increase the arrhythmogenic activities of Fendiline.
Eperisone Levosimendan may increase the arrhythmogenic activities of Eperisone.
Melperone Levosimendan may increase the arrhythmogenic activities of Melperone.
Benidipine Levosimendan may increase the arrhythmogenic activities of Benidipine.
Otilonium Levosimendan may increase the arrhythmogenic activities of Otilonium.
Nizofenone Levosimendan may increase the arrhythmogenic activities of Nizofenone.
Bunaftine Levosimendan may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Levosimendan may increase the arrhythmogenic activities of Lorcainide.
Penfluridol Levosimendan may increase the arrhythmogenic activities of Penfluridol.
Dexverapamil Levosimendan may increase the arrhythmogenic activities of Dexverapamil.
Esmolol Esmolol may increase the arrhythmogenic activities of Levosimendan.
Isradipine Isradipine may increase the arrhythmogenic activities of Levosimendan.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Levosimendan.
Timolol Timolol may increase the arrhythmogenic activities of Levosimendan.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Levosimendan.
Digoxin Digoxin may increase the arrhythmogenic activities of Levosimendan.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Levosimendan.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Levosimendan.
Ethosuximide Ethosuximide may increase the arrhythmogenic activities of Levosimendan.
Nicardipine Nicardipine may increase the arrhythmogenic activities of Levosimendan.
Verapamil Verapamil may increase the arrhythmogenic activities of Levosimendan.
Losartan Losartan may increase the arrhythmogenic activities of Levosimendan.
Moricizine Moricizine may increase the arrhythmogenic activities of Levosimendan.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Levosimendan.

Target Protein

Troponin C, slow skeletal and cardiac muscles TNNC1
ATP-sensitive inward rectifier potassium channel 11 KCNJ11
ATP-sensitive inward rectifier potassium channel 8 KCNJ8
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A

Referensi & Sumber

Synthesis reference: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Ashwini Amol Sawant, "Process for Preparing Levosimendan and Intermediates for Use in the Process." U.S. Patent US20120165524, issued June 28, 2012.
Artikel (PubMed)
  • PMID: 17473298
    Mebazaa A, Nieminen MS, Packer M, Cohen-Solal A, Kleber FX, Pocock SJ, Thakkar R, Padley RJ, Poder P, Kivikko M: Levosimendan vs dobutamine for patients with acute decompensated heart failure: the SURVIVE Randomized Trial. JAMA. 2007 May 2;297(17):1883-91.
  • PMID: 17323593
    Kasikcioglu HA, Cam N: A review of levosimendan in the treatment of heart failure. Vasc Health Risk Manag. 2006;2(4):389-400.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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