aprindine indications/contra

Stem definitionDrug idCAS RN
231 37640-71-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aprindine
  • aprindin
  • aprinidine
  • aprindine hydrochloride
  • aprindine HCl
  • amidonal
  • fiboran
A class Ib anti-arrhythmia agent used to manage ventricular and supraventricular arrhythmias.
  • Molecular weight: 322.50
  • Formula: C22H30N2
  • CLOGP: 5.90
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 0
  • TPSA: 6.48
  • ALOGS: -4.62
  • ROTB: 8

Drug dosage:

DoseUnitRoute
0.10 g O
0.10 g P

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1996 YEAR INTRODUCED

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C01BB04 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class Ib
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D026941 Sodium Channel Blockers
MeSH PA D061567 Voltage-Gated Sodium Channel Blockers

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Ventricular arrhythmia indication 44103008
Supraventricular arrhythmia indication 72654001

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.56 Basic
pKa2 6.73 Basic

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
Calmodulin Cytosolic other INHIBITOR ID50 4.74 WOMBAT-PK SCIENTIFIC LITERATURE
Sodium/calcium exchanger 1 Transporter IC50 4.30 WOMBAT-PK
Proteasome subunit alpha type-1 Enzyme IC50 5.40 WOMBAT-PK
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel IC50 4.36 WOMBAT-PK
Cytochrome P450 2D6 Enzyme Ki 7.76 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel WOMBAT-PK
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK

External reference:

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IDSource
N0000167348 NUI
C0003639 UMLSCUI
D01326 KEGG_DRUG
5Y48085P9Q UNII
3179 INN_ID
N0000167348 NDFRT
1054 RXNORM
005233 NDDF
2218 PUBCHEM_CID
CHEMBL1213033 ChEMBL_ID
DB01429 DRUGBANK_ID
CHEMBL2104501 ChEMBL_ID
33237-74-0 SECONDARY_CAS_RN
D001073 MESH_DESCRIPTOR_UI
CHEBI:135370 CHEBI

Pharmaceutical products:

None