amrinone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

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

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.90 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 25 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 4.01 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 93 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.89 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 31, 1984 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CE01 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Phosphodiesterase inhibitors
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
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)

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:557
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

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:

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:

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

Pharmaceutical products:

None