ambenonium 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
quaternary ammonium compounds 146 7648-98-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ambenonium
  • ambenonium chloride
  • ambestigmin chloride
  • mytelase chloride
  • mytelase
A quaternary ammonium compound that is an inhibitor of cholinesterase activity with actions similar to those of NEOSTIGMINE, but of longer duration. Ambenonium is given by mouth in the treatment of myasthenia gravis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1112)
  • Molecular weight: 537.57
  • Formula: C28H42Cl2N4O2
  • CLOGP: 0.18
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 58.20
  • ALOGS: -8.81
  • ROTB: 15

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 60.84 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
May 1, 1956 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07AA30 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
PARASYMPATHOMIMETICS
Anticholinesterases
FDA MoA N0000000177 Cholinesterase Inhibitors
CHEBI has role CHEBI:37733 EC 3.1.1.8 inhibitor
CHEBI has role CHEBI:35942 neurotransmitter agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D002800 Cholinesterase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010277 Parasympathomimetics
MeSH PA D018373 Peripheral Nervous System Agents
FDA EPC N0000175723 Cholinesterase Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Myasthenia gravis indication 91637004 DOID:437
Urinary tract obstruction contraindication 7163005 DOID:5200
Parkinsonism contraindication 32798002
Gastrointestinal obstruction contraindication 126765001
Asthma contraindication 195967001 DOID:2841




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.69 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 CHEMBL CHEMBL
Acetylcholinesterase Enzyme Kd 4.34 CHEMBL
Acetylcholinesterase Enzyme IC50 9.92 CHEMBL

External reference:

IDSource
4022236 VUID
N0000020242 NUI
D01001 KEGG_DRUG
115-79-7 SECONDARY_CAS_RN
468764 RXNORM
C0002412 UMLSCUI
CHEBI:2627 CHEBI
CHEMBL1652 ChEMBL_ID
DB01122 DRUGBANK_ID
L16PUN799N UNII
2131 PUBCHEM_CID
2011 MMSL
4162 MMSL
d01420 MMSL
36537006 SNOMEDCT_US
387197009 SNOMEDCT_US
46887006 SNOMEDCT_US
D000549 MESH_DESCRIPTOR_UI
CHEMBL1200541 ChEMBL_ID
4018246 VANDF
4022236 VANDF
552 INN_ID
001706 NDDF
004686 NDDF

Pharmaceutical products:

None