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

Stem definitionDrug idCAS RN
988 312-48-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • edrophonium
  • edrophonium chloride
A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.
  • Molecular weight: 166.24
  • Formula: C10H16NO
  • CLOGP: -2.44
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 20.23
  • ALOGS: -3.62
  • ROTB: 2

  • Status: OFM

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.60 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 3, 1951 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC V04CX07 VARIOUS
DIAGNOSTIC AGENTS
OTHER DIAGNOSTIC AGENTS
Other diagnostic agents
FDA EPC N0000175723 Cholinesterase Inhibitor
CHEBI has role CHEBI:33295 diagnostic agent
CHEBI has role CHEBI:50247 antidote
MeSH PA D000931 Antidotes
MeSH PA D018678 Cholinergic Agents
MeSH PA D002800 Cholinesterase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D020011 Protective Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Reversal of neuromuscular blockade indication 241703000
Curare Overdose indication
Neuromuscular Block due to Nondepolarizing Drug indication
Diagnostic Test for Myasthenia Gravis indication
Brain damage contraindication 2470005
Tachyarrhythmia contraindication 6285003
Urinary tract obstruction contraindication 7163005 DOID:5200
Severe chronic ulcerative colitis contraindication 14311001
Toxic megacolon contraindication 28536002 DOID:1770
Atony of colon contraindication 29479008
Hyperthyroidism contraindication 34486009 DOID:7998
Hypertensive disorder contraindication 38341003 DOID:10763
Complete trisomy 21 syndrome contraindication 41040004 DOID:14250
Conduction disorder of the heart contraindication 44808001
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Paralytic ileus contraindication 55525008 DOID:8442
Peptic reflux disease contraindication 57643001
Ulcerative colitis contraindication 64766004 DOID:8577
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Spastic paralysis contraindication 78403003
Disturbance of salivary secretion contraindication 78948009
Hiatal hernia contraindication 84089009 DOID:12642
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Gastrointestinal obstruction contraindication 126765001
Autonomic dysreflexia contraindication 129618003
Bleeding contraindication 131148009
Asthma contraindication 195967001 DOID:2841
Myocardial dysfunction contraindication 233928007
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Pyloric obstruction contraindication 244815007
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Drowsy contraindication 271782001
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastric ulcer contraindication 397825006 DOID:10808
Chronic lung disease contraindication 413839001
Disorder of coronary artery contraindication 414024009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.87 acidic

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 Ki 8.79 CHEMBL CHEMBL
Acetylcholinesterase Enzyme Ki 6.70 CHEMBL

External reference:

IDSource
D004491 MESH_DESCRIPTOR_UI
4019741 VUID
N0000147833 NUI
C0013615 UMLSCUI
D00994 KEGG_DRUG
46913003 SNOMEDCT_US
3752 RXNORM
373342004 SNOMEDCT_US
d00220 MMSL
4019741 VANDF
004688 NDDF
3202 PUBCHEM_CID
CHEBI:251408 CHEBI
CHEMBL60745 ChEMBL_ID
CHEMBL1104 ChEMBL_ID
CHEMBL1128 ChEMBL_ID
DB01010 DRUGBANK_ID
QO611KSM5P UNII
187 INN_ID
116-38-1 SECONDARY_CAS_RN
9073 IUPHAR_LIGAND_ID

Pharmaceutical products:

None