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

Stem definitionDrug idCAS RN
Class I antiarrhythmics, procainamide and lidocaine derivatives 1007 66778-36-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • encainide hydrochloride
  • MJ 9067
  • MJ-9067
  • encainide
One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.
  • Molecular weight: 352.48
  • Formula: C22H28N2O2
  • CLOGP: 3.52
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 41.57
  • ALOGS: -4.94
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.11 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 27 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance) 13 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.26 % Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution) 2.20 L/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.60 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 25 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AKT2,AKT3,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IRAK1,ITK,JAK1,JAK2,MAP3K21,MAP3K7,MAPK12,MAPK7,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 43
kinase-selectivity-class AXL,GRK2,PDK4,SIK2,STK33,TTK 6
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1987 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 C01BC08 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
ANTIARRHYTHMICS, CLASS I AND III
Antiarrhythmics, class Ic
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:38633 sodium channel blocker
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

Related Drugs by ATC class:

C01BC Antiarrhythmics, class Ic 4 drugs
ethacizineflecainidelorcainidepropafenone

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

DiseaseRelationSNOMED_IDDOID
Ventricular premature beats indication 17338001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.56 acidic
pKa2 9.2 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
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK
Sodium channel subunit beta-1 Ion channel WOMBAT-PK
Sodium channel subunit beta-2 Ion channel WOMBAT-PK
Sodium channel subunit beta-3 Ion channel WOMBAT-PK
Sodium channel subunit beta-4 Ion channel WOMBAT-PK

External reference:

IDSource
4019745 VUID
N0000147836 NUI
D07894 KEGG_DRUG
66794-74-9 SECONDARY_CAS_RN
4019356 VANDF
4019745 VANDF
C0085251 UMLSCUI
CHEBI:4788 CHEBI
CHEMBL315838 ChEMBL_ID
CHEMBL2106155 ChEMBL_ID
DB01228 DRUGBANK_ID
D016700 MESH_DESCRIPTOR_UI
48041 PUBCHEM_CID
4472 INN_ID
SY3J0147NB UNII
281189 RXNORM
000631 NDDF
004486 NDDF
372749000 SNOMEDCT_US
46479001 SNOMEDCT_US
81017004 SNOMEDCT_US

Pharmaceutical products:

None