levosimendan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cardiac stimulants, pimobendan derivatives 1576 141505-33-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • levosimendan
  • (R)-Simendan
  • simdax
A hydrazone and pyridazine derivative; the levo-form is a phosphodiesterase III inhibitor, calcium-sensitizing agent, and inotropic agent that is used in the treatment of HEART FAILURE.
  • Molecular weight: 280.29
  • Formula: C14H12N6O
  • CLOGP: 1.90
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 113.43
  • ALOGS: -3.50
  • ROTB: 3

Drug dosage:

DoseUnitRoute
11 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 85 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.24 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.80 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Lymphatic fistula 130.61 96.07 22 1521 764 56289760
Femoral hernia incarcerated 130.19 96.07 22 1521 779 56289745
Pancreatic steatosis 126.03 96.07 22 1521 946 56289578
Arterial haemorrhage 120.89 96.07 23 1520 1602 56288922
Wound infection pseudomonas 119.30 96.07 22 1521 1293 56289231
Seroma 111.10 96.07 22 1521 1889 56288635
Haemarthrosis 106.50 96.07 23 1520 3021 56287503
Aortic valve stenosis 105.73 96.07 23 1520 3124 56287400
Cardiogenic shock 105.41 96.07 32 1511 16293 56274231
Tachyarrhythmia 99.01 96.07 23 1520 4198 56286326

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Lymphatic fistula 130.50 76.54 22 1895 778 70925749
Femoral hernia incarcerated 130.31 76.54 22 1895 785 70925742
Pancreatic steatosis 124.32 76.54 22 1895 1038 70925489
Wound infection pseudomonas 115.49 76.54 22 1895 1562 70924965
Arterial haemorrhage 112.13 76.54 23 1894 2388 70924139
Seroma 108.95 76.54 22 1895 2112 70924415
Cardiogenic shock 98.63 76.54 37 1880 36270 70890257
Aortic valve stenosis 95.61 76.54 23 1894 4936 70921591
Haemarthrosis 93.50 76.54 23 1894 5416 70921111
Tachyarrhythmia 89.85 76.54 23 1894 6359 70920168
Hepatic cyst 87.93 76.54 22 1895 5549 70920978
Wound dehiscence 85.57 76.54 22 1895 6186 70920341
Diverticulum intestinal 84.58 76.54 23 1894 8018 70918509
Inflammatory marker increased 81.33 76.54 23 1894 9251 70917276
Aortic arteriosclerosis 80.40 76.54 22 1895 7847 70918680
Eructation 80.17 76.54 23 1894 9737 70916790

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CX08 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Other cardiac stimulants
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents
CHEBI has role CHEBI:35620 vasodilator agents
CHEBI has role CHEBI:38070 antiarrhythmic agent
CHEBI has role CHEBI:38147 cardiotonic drugs
CHEBI has role CHEBI:50568 3,5-cyclic nucleoside monophosphate phosphodiesterase inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Congestive heart failure indication 42343007 DOID:6000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.04 acidic
pKa2 11.34 acidic
pKa3 4.67 Basic
pKa4 4.04 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Troponin C, slow skeletal and cardiac muscles Cytosolic other OPENER Kd 3.16 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
ATP-sensitive inward rectifier potassium channel 11 Ion channel WOMBAT-PK
ATP-sensitive inward rectifier potassium channel 8 Ion channel WOMBAT-PK
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme WOMBAT-PK

External reference:

IDSource
D04720 KEGG_DRUG
C0246904 UMLSCUI
CHEBI:50567 CHEBI
CHEMBL2051955 ChEMBL_ID
DB00922 DRUGBANK_ID
D000077464 MESH_DESCRIPTOR_UI
3033825 PUBCHEM_CID
7020 INN_ID
C6T4514L4E UNII
73107 RXNORM
009718 NDDF
442790008 SNOMEDCT_US
442795003 SNOMEDCT_US

Pharmaceutical products:

None