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 131.53 84.66 22 1646 764 63486590
Femoral hernia incarcerated 130.04 84.66 22 1646 819 63486535
Pancreatic steatosis 125.89 84.66 22 1646 994 63486360
Arterial haemorrhage 120.59 84.66 23 1645 1694 63485660
Wound infection pseudomonas 120.01 84.66 22 1646 1306 63486048
Seroma 109.62 84.66 22 1646 2109 63485245
Haemarthrosis 106.59 84.66 23 1645 3138 63484216
Aortic valve stenosis 105.61 84.66 23 1645 3276 63484078
Tachyarrhythmia 98.76 84.66 23 1645 4427 63482927
Wound dehiscence 91.36 84.66 22 1646 4881 63482473
Hepatic cyst 90.27 84.66 22 1646 5132 63482222
Diverticulum intestinal 89.36 84.66 23 1645 6690 63480664
Inflammatory marker increased 88.94 84.66 23 1645 6816 63480538
Aortic arteriosclerosis 86.20 84.66 22 1646 6187 63481167

FDA Adverse Event Reporting System (Male)

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
Jugular vein distension 73.39 67.69 12 506 654 34955759

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 132.35 66.76 22 1952 781 79741633
Femoral hernia incarcerated 131.30 66.76 22 1952 820 79741594
Pancreatic steatosis 124.55 66.76 22 1952 1123 79741291
Wound infection pseudomonas 116.91 66.76 22 1952 1599 79740815
Arterial haemorrhage 112.76 66.76 23 1951 2538 79739876
Seroma 109.23 66.76 22 1952 2278 79740136
Aortic valve stenosis 96.12 66.76 23 1951 5271 79737143
Haemarthrosis 93.99 66.76 23 1951 5789 79736625
Tachyarrhythmia 89.86 66.76 23 1951 6939 79735475
Hepatic cyst 87.91 66.76 22 1952 6067 79736347
Wound dehiscence 86.16 66.76 22 1952 6573 79735841
Diverticulum intestinal 85.03 66.76 23 1951 8582 79733832
Inflammatory marker increased 79.98 66.76 23 1951 10717 79731697
Eructation 79.63 66.76 23 1951 10886 79731528
Aortic arteriosclerosis 79.58 66.76 22 1952 8896 79733518
Cardiogenic shock 79.01 66.76 32 1942 41882 79700532
Mitral valve incompetence 75.90 66.76 28 1946 28537 79713877
Faecaloma 73.93 66.76 22 1952 11542 79730872
Postoperative wound infection 71.45 66.76 22 1952 12939 79729475
Groin pain 71.26 66.76 22 1952 13058 79729356
Tricuspid valve incompetence 70.12 66.76 24 1950 19688 79722726
Joint dislocation 69.66 66.76 23 1951 16916 79725498
Aplastic anaemia 68.40 66.76 23 1951 17882 79724532
Escherichia infection 68.26 66.76 23 1951 17994 79724420
Cardiovascular disorder 68.25 66.76 23 1951 18002 79724412

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
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme WOMBAT-PK
ATP-sensitive inward rectifier potassium channel 11 Ion channel WOMBAT-PK
ATP-sensitive inward rectifier potassium channel 8 Ion channel 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