amrinone indications/contra

Stem definitionDrug idCAS RN
cardiac stimulants, amrinone derivatives 201 60719-84-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • inamrinone lactate
  • amrinone
  • cartonic
  • cordemcura
  • inamrinone
  • vesistol
  • wincoram
A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.
  • Molecular weight: 187.20
  • Formula: C10H9N3O
  • CLOGP: -0.69
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 68.01
  • ALOGS: -1.52
  • ROTB: 1

Drug dosage:

DoseUnitRoute
0.50 g P

Approvals:

DateAgencyCompanyOrphan
July 31, 1984 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C01CE01 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Phosphodiesterase inhibitors
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D058987 Phosphodiesterase 3 Inhibitors
MeSH PA D010726 Phosphodiesterase Inhibitors
MeSH PA D020011 Protective Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Decompensated cardiac failure indication 195111005
Myocardial infarction contraindication 22298006 DOID:5844
Hypovolemia contraindication 28560003
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Pulmonic valve stenosis contraindication 56786000 DOID:6420
Aortic valve stenosis contraindication 60573004 DOID:1712
Kidney disease contraindication 90708001 DOID:2527
Hypertrophic cardiomyopathy contraindication 233873004 DOID:11984
Disease of liver contraindication 235856003 DOID:409
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Idiopathic hypertrophic subaortic stenosis contraindication 360465008
Myocardial infarction in recovery phase contraindication 418044006

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.6 acidic
pKa2 6.6 Basic
pKa3 2.8 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Enzyme INHIBITOR IC50 4.78 WOMBAT-PK CHEMBL
Phosphodiesterase 4 Enzyme IC50 4.39 CHEMBL
cGMP-inhibited 3',5'-cyclic phosphodiesterase B Enzyme INHIBITOR IC50 4.51 IUPHAR

External reference:

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IDSource
CHEBI:2686 CHEBI
4021234 VUID
N0000148678 NUI
C0304521 UMLSCUI
7202 IUPHAR_LIGAND_ID
D00231 KEGG_DRUG
CHEMBL12856 ChEMBL_ID
3698 PUBCHEM_CID
4021233 VANDF
d00172 MMSL
412412006 SNOMEDCT_US
412411004 SNOMEDCT_US
4019612 VANDF
738 RXNORM
N0000005907 NDFRT
N0000147706 NDFRT
N0000148677 NDFRT
006203 NDDF
DB01427 DRUGBANK_ID
CHEMBL2096642 ChEMBL_ID
I229274Y5B UNII
75898-90-7 SECONDARY_CAS_RN
4310 INN_ID
D000676 MESH_DESCRIPTOR_UI

Pharmaceutical products:

None