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Levosimendan

Levosimendan
Levosimendan.svg
Levosimendan ball-and-stick.png
Clinical data
Trade names Simdax
AHFS/Drugs.com International Drug Names
Routes of
administration
IV
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 85% (oral)
Protein binding 97–98%
Metabolism Extensive hepatic
Biological half-life ~1 hour (levosimendan), 75–80 hours (metabolites)
Excretion urine (54%), feces (44%)
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.189.828
Chemical and physical data
Formula C14H12N6O
Molar mass 280.28 g/mol
3D model (Jmol)
 NYesY (what is this?)  

Levosimendan (INN) /ˌlvsˈmɛndən/ is a calcium sensitiser used in the management of acutely decompensated congestive heart failure. It is marketed under the trade name Simdax (Orion Corporation).

Levosimendan is a calcium sensitizer — it increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan exerts its positive inotropic effect by increasing calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner. It also has a vasodilatory effect, by opening adenosine triphosphate (ATP)-sensitive potassium channels in vascular smooth muscle to cause smooth muscle relaxation. The combined inotropic and vasodilatory actions result in an increased force of contraction, decreased preload and decreased afterload. Moreover, by opening also the mitochondrial (ATP)-sensitive potassium channels in cardiomyocytes, the drug exerts a cardioprotective effect.

Levosimendan is indicated for inotropic support in acutely-decompensated severe congestive heart failure.


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