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QuickView for levosimendan (compound)

Name: Levosimendan
Name (isomeric): DB00922
Drug Type: small molecule
Brand: Simdax, Simendan
Category: Vasodilator Agents, Phosphodiesterase Inhibitors, Cardiotonic Agents, Anti-Arrhythmia Agents
CAS number: 141505-33-1
Indication: For short term treatment of acutely decompensated severe chronic heart failure (CHF). Also being investigated for use/treatment in heart disease.
Levosimendan is a new Ca2+-sensitizing inotropic agent. Ca2+ sensitizers represent a new class of inotropic agents, which overcome the disadvantages associated with currently available inotropic agents in as they are not associated with an increased risk of arrhythmias, cell injury and death due to Ca2+ overload in ...
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Mechanism of Action:
Levosimendan appears to increase myofilament calcium sensitivity by binding to cardiac troponin C in a calcium-dependent manner. This stabilizes the calcium-induced conformational change of troponin C, thereby (1) changing actin-myosin cross-bridge kinetics apparently without increasing the cycling rate of the cross-bridges or myocardial ATP consum...
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Absorption: The bioavailability of oral levosimendan is 85 ± 6% in healthy volunteers and 84 ± 4% in patients.
Protein binding: 98% bound to plasma protein.
Biotransformation: Complete metabolism, with some active metabolites (OR-1855 and OR-1896) possibly extending the drug's haemodynamic effects.
Half Life: Eliminination half-life is approximately 1 hour.
Affected organisms: Humans and other mammals