aprindine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

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

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.86 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 85 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK 49
kinase-selectivity-class AKT3,AXL,CAMK2D,CDK4,EIF2AK3,EPHB4,GRK2,PDK4,PRKCD,SIK2,STK33,TEK 12
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.490 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
rat-kpuu-brain Rat brain Kpuu 1.199 % High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1996 YEAR INTRODUCED

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 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 D026941 Sodium Channel Blockers
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D061567 Voltage-Gated Sodium Channel Blockers
CHEBI has role CHEBI:38070 anti-arrhythmia drug

Related Drugs by ATC class:

C01BB Antiarrhythmics, class Ib 3 drugs
lidocainemexiletinetocainide

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

DiseaseRelationSNOMED_IDDOID
Ventricular arrhythmia indication 44103008
Supraventricular arrhythmia indication 72654001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Calmodulin Cytosolic other INHIBITOR ID50 4.75 WOMBAT-PK SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2 Ion channel WOMBAT-PK
Cytochrome P450 2D6 Enzyme Ki 7.76 WOMBAT-PK
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK
Sodium/calcium exchanger 1 Transporter IC50 4.30 WOMBAT-PK
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 Ion channel IC50 4.36 WOMBAT-PK
Proteasome subunit alpha type-1 Enzyme IC50 5.40 WOMBAT-PK

External reference:

IDSource
N0000167348 NUI
D01326 KEGG_DRUG
1054 RXNORM
C0003639 UMLSCUI
CHEBI:135370 CHEBI
CHEMBL1213033 ChEMBL_ID
DB01429 DRUGBANK_ID
CHEMBL2104501 ChEMBL_ID
D001073 MESH_DESCRIPTOR_UI
2218 PUBCHEM_CID
3179 INN_ID
33237-74-0 SECONDARY_CAS_RN
5Y48085P9Q UNII
005233 NDDF
005247 NDDF
5Y48085P9Q INXIGHT DRUGS

Pharmaceutical products:

None