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

Stem definition	Drug id	CAS RN
cardiac stimulants, pimobendan derivatives	1576	141505-33-1

Description:

Molecule

Description

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:

Dose	Unit	Route
11	mg	P

ADMET properties:

Property	Value	Reference
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Congestive heart failure	indication	42343007	DOID:6000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Troponin C, slow skeletal and cardiac muscles	Cytosolic other	P63316	TNNC1_HUMAN	OPENER	Kd	3.16		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
ATP-sensitive inward rectifier potassium channel 11	Ion channel	Q14654	KCJ11_HUMAN					WOMBAT-PK
ATP-sensitive inward rectifier potassium channel 8	Ion channel	Q15842	KCNJ8_HUMAN					WOMBAT-PK
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Enzyme	Q14432	PDE3A_HUMAN					WOMBAT-PK

External reference:

ID	Source
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