Levosimendán

Levosimendán Uses, Dosage, Side Effects, Food Interaction and all others data.

Levosimendán 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. Levosimendán is used to manage acutely decompensated congestive heart failure.

Levosimendán 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 myocardial cells; they do not increase the activation energy; and they have the potential to reverse contractile dysfunction under pathophysiologic conditions, such as acidosis or myocardial stunning. Levosimendán has not been approved for use in the U.S. or Canada.

Trade Name Levosimendán
Generic Levosimendan
Levosimendan Other Names Levosimendán, Lévosimendan, Levosimendan, Levosimendanum
Type
Formula C14H12N6O
Weight Average: 280.2847
Monoisotopic: 280.107259036
Protein binding

98% bound to plasma protein.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Levosimendán
Levosimendán

Uses

Levosimendán is a calcium sensitizer indicated to treat acutely decompensated severe chronic heart failure.

For short term treatment of acutely decompensated severe chronic heart failure (CHF). Also being investigated for use/treatment in heart disease.

Levosimendán is also used to associated treatment for these conditions: Acute Decompensated Heart Failure (ADHF), Acute Decompensation of Chronic Heart Failure, Acute Heart Failure (AHF), Chronic Heart Failure (CHF), Acute Decompensated Chronic Heart Failure, Acute post-surgical heart failure, Heart failure post-myocardial infarction, Severe Decompensated Chronic Heart Failure, Positive cardiac inotropic effect, Intravenous inotropic therapy

How Levosimendán works

Levosimendán 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 consumption, (2) increasing the effects of calcium on cardiac myofilaments during systole and (3) improving contraction at low energy cost (inotropic effect). Calcium concentration and, therefore, sensitization decline during diastole, allowing normal or improved diastolic relaxation. Levosimendán also leads to vasodilation through the opening of ATP-sensitive potassium channels. By these inotropic and vasodilatory actions, levosimendan increases cardiac output without increasing myocardial oxygen demand. Levosimendán also has a selective phosphodiesterase (PDE)-III inhibitory action that may contribute to the inotropic effect of this compound under certain experimental conditions. It has been reported that levosimendan may act preferentially as a Ca2+ sensitizer at lower concentrations, whereas at higher concentrations its action as a PDE-III inhibitor becomes more prominent in experimental animals and humans.

Elimination Route

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

Half Life

Eliminination half-life is approximately 1 hour.

Innovators Monograph

You find simplified version here Levosimendán

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0000113
http://classyfire.wishartlab.com/tax_nodes/C0000113
http://classyfire.wishartlab.com/tax_nodes/C0000208
http://classyfire.wishartlab.com/tax_nodes/C0000362
http://classyfire.wishartlab.com/tax_nodes/C0000116
http://classyfire.wishartlab.com/tax_nodes/C0000265
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0003940
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0001831
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:50567
http://www.hmdb.ca/metabolites/HMDB0015058
http://www.genome.jp/dbget-bin/www_bget?drug:D04720
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3033825
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507149
https://www.chemspider.com/Chemical-Structure.2298414.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50469700
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=73107
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=50567
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL2051955
https://zinc.docking.org/substances/ZINC000003915645
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000797
http://www.pharmgkb.org/drug/PA164749138
https://en.wikipedia.org/wiki/Levosimendan
*** Taking medicines without doctor's advice can cause long-term problems.
Share