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

Stem definitionDrug idCAS RN
Class I antiarrhythmics, procainamide and lidocaine derivatives 2167 88069-67-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pilsicainide
  • pilzicainide
  • pilsicainide hydrochloride
  • SUN 1165
  • pilsicainide HCl
  • pilsicainide hydrochloride hemihydrate
  • pilsicainide hydrochloride hydrate
  • Molecular weight: 272.39
  • Formula: C17H24N2O
  • CLOGP: 2.05
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 32.34
  • ALOGS: -2.84
  • ROTB: 3

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 5 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Cerebral infarction 57.24 37.44 19 436 27436 34929040

FDA Adverse Event Reporting System (Geriatric)

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
Cerebral infarction 66.38 33.76 24 981 45652 79697731
Cardiac tamponade 39.16 33.76 11 994 9265 79734118
Cardiac failure 35.91 33.76 23 982 154819 79588564
Cerebral haemorrhage 34.31 33.76 16 989 57657 79685726

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D026941 Sodium Channel Blockers
CHEBI has role CHEBI:38070 antiarrhythmic agent
CHEBI has role CHEBI:38633 sodium channel blockers

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

DiseaseRelationSNOMED_IDDOID
Tachyarrhythmia indication 6285003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.97 acidic
pKa2 9.08 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 4 subunit alpha Ion channel BLOCKER IC50 4.38 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.69 CHEMBL

External reference:

IDSource
D01554 KEGG_DRUG
C0164155 UMLSCUI
CHEBI:135127 CHEBI
CHEMBL163238 ChEMBL_ID
DB12712 DRUGBANK_ID
C042288 MESH_SUPPLEMENTAL_RECORD_UI
4820 PUBCHEM_CID
6554 INN_ID
88069-49-2 SECONDARY_CAS_RN
AV0X7V6CSE UNII

Pharmaceutical products:

None