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

Stem definitionDrug idCAS RN
acetylcholinesterase inhibitors 927 17299-00-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BC-51
  • hexamarium
  • distigmine
  • distigmine bromide
  • ubretid
  • Molecular weight: 416.52
  • Formula: C22H32N4O4
  • CLOGP: -7.11
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 0
  • TPSA: 66.84
  • ALOGS: -6.02
  • ROTB: 11

Drug dosage:

DoseUnitRoute
5 mg O
0.25 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 8 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.20 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 59.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 5, 1967 PMDA Torii Pharmaceuticals

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
Cholinergic syndrome 61.05 35.22 9 453 374 46685226
Neurogenic bladder 37.11 35.22 8 454 2902 46682698

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
Appendicolith 48.64 31.07 10 923 909 29950636
Urinary retention 37.67 31.07 19 914 32898 29918647

Pharmacologic Action:

SourceCodeDescription
ATC N07AA03 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
PARASYMPATHOMIMETICS
Anticholinesterases
MeSH PA D018678 Cholinergic Agents
MeSH PA D002800 Cholinesterase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:37733 bche inhibitor
CHEBI has role CHEBI:38325 muscarinic agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute cystitis indication 68226007 DOID:13148
Myasthenia gravis indication 91637004 DOID:437
Difficulty passing urine indication 102835006

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
Acetylcholinesterase Enzyme INHIBITOR KEGG DRUG KEGG DRUG

External reference:

IDSource
D01228 KEGG_DRUG
15876-67-2 SECONDARY_CAS_RN
C2987626 UMLSCUI
CHEBI:31512 CHEBI
CHEMBL1199307 ChEMBL_ID
CHEMBL1098285 ChEMBL_ID
DB13694 DRUGBANK_ID
C084645 MESH_SUPPLEMENTAL_RECORD_UI
27522 PUBCHEM_CID
764 INN_ID
T940307O7B UNII
154982 RXNORM
003959 NDDF
349943004 SNOMEDCT_US
395966008 SNOMEDCT_US
396033002 SNOMEDCT_US

Pharmaceutical products:

None