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

Stem definitionDrug idCAS RN
881 71-63-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • digitoxin
  • digitoxoside
  • cardidigin
  • cardigin
  • carditoxin
  • coramedan
  • cristapurat
  • crystodigin
  • digicor
  • digipural
  • digisidin
  • digitophyllin
  • digitoxigenin tridigitoxoside
  • myodigin
  • purpurid
  • tradigal
  • unidigin
A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665)
  • Molecular weight: 764.95
  • Formula: C41H64O13
  • CLOGP: 2.85
  • LIPINSKI: 2
  • HAC: 13
  • HDO: 5
  • TPSA: 182.83
  • ALOGS: -4.42
  • ROTB: 7

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
0.10 mg O
0.10 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 95 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.44 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.04 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.07 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 180 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
None FDA LILLY

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
Bradycardia 133.68 69.32 25 63 9956 2348041
Atrial fibrillation 72.33 69.32 16 72 13752 2344245

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
Therapeutic drug monitoring analysis not performed 94.49 57.34 9 63 5 1746704
Bradyarrhythmia 64.73 57.34 9 63 373 1746336
Product prescribing error 61.24 57.34 11 61 2399 1744310

Pharmacologic Action:

SourceCodeDescription
ATC C01AA04 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC GLYCOSIDES
Digitalis glycosides
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D020011 Protective Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Sodium/potassium-transporting ATPase subunit alpha-1 Transporter INHIBITOR WOMBAT-PK CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.86 WOMBAT-PK
Sodium/potassium-transporting ATPase Transporter IC50 8.10 CHEMBL
Signal transducer and activator of transcription 3 Transcription factor IC50 6.15 CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-2 Ion channel IC50 6.65 DRUG MATRIX
Sodium/potassium-transporting ATPase subunit alpha-1 Transporter IC50 8.10 CHEMBL

External reference:

IDSource
D004074 MESH_DESCRIPTOR_UI
4017429 VUID
N0000145817 NUI
C0012258 UMLSCUI
D00297 KEGG_DRUG
3403 RXNORM
373534001 SNOMEDCT_US
4596 MMSL
d00209 MMSL
81728006 SNOMEDCT_US
4017429 VANDF
000592 NDDF
CHEMBL254219 ChEMBL_ID
E90NZP2L9U UNII
1547 INN_ID
DB01396 DRUGBANK_ID
CHEBI:28544 CHEBI
6782 IUPHAR_LIGAND_ID
441207 PUBCHEM_CID

Pharmaceutical products:

None