ambenonium indications/contra

Stem definitionDrug idCAS RN
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

Drug dosage:

DoseUnitRoute
60 mg O

Approvals:

DateAgencyCompanyOrphan
May 1, 1956 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System

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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 64.09 59.62 7 27 196 3385629

Pharmacologic Action:

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SourceCodeDescription
ATC N07AA30 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
PARASYMPATHOMIMETICS
Anticholinesterases
FDA EPC N0000175723 Cholinesterase Inhibitor
MeSH PA D001337 Autonomic 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

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Myasthenia gravis indication 91637004 DOID:437
Urinary tract obstruction contraindication 7163005 DOID:5200
Parkinsonism contraindication 32798002 DOID:13548
Gastrointestinal obstruction contraindication 126765001
Asthma contraindication 195967001 DOID:2841

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Acetylcholinesterase Enzyme INHIBITOR CHEMBL CHEMBL
Acetylcholinesterase Enzyme IC50 9.92 CHEMBL
Acetylcholinesterase Enzyme Kd 4.34 CHEMBL

External reference:

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IDSource
4022236 VUID
N0000020242 NUI
C0002412 UMLSCUI
D01001 KEGG_DRUG
51FOB87G3I UNII
552 INN_ID
115-79-7 SECONDARY_CAS_RN
DB01122 DRUGBANK_ID
623 RXNORM
36537006 SNOMEDCT_US
387197009 SNOMEDCT_US
d01420 MMSL
4022236 VANDF
N0000020242 NDFRT
004686 NDDF
2131 PUBCHEM_CID
CHEMBL1652 ChEMBL_ID
CHEMBL1200541 ChEMBL_ID
D000549 MESH_DESCRIPTOR_UI
CHEBI:2627 CHEBI

Pharmaceutical products:

None