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Trade names | Simdax |
AHFS/Drugs.com | International Drug Names |
Routes of administration |
IV |
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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%) |
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ECHA InfoCard | 100.189.828 |
Chemical and physical data | |
Formula | C14H12N6O |
Molar mass | 280.28 g/mol |
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(what is this?) |
Levosimendan (INN) /ˌliːvoʊsaɪˈmɛndən/ 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.