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

Stem definition	Drug id	CAS RN
Class I antiarrhythmics, procainamide and lidocaine derivatives	2167	88069-67-4

Description:

Molecule

Description

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:

Property	Value	Reference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,TEK	21
kinase-selectivity-class	AXL,BRAF,DDR1,EPHB4,ERBB2,GRK2,PDK4,SIK2	8
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	2.328		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
rat-kpuu-brain	Rat brain Kpuu	0.101	%	High	1

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cerebral infarction	54.56	35.54	19	543	31150	42589623
Interstitial lung disease	37.62	35.54	19	543	78443	42542330

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cerebral infarction	75.49	35.85	26	1129	51812	110536332
Cardiac failure	40.85	35.85	25	1130	187601	110400543
Cardiac tamponade	39.05	35.85	11	1144	11296	110576848
Atrial fibrillation	38.61	35.85	26	1129	229616	110358528
Renal impairment	38.20	35.85	24	1131	188421	110399723

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D026941	Sodium Channel Blockers
MeSH PA	D049990	Membrane Transport Modulators
CHEBI has role	CHEBI:38070	anti-arrhythmia drug
CHEBI has role	CHEBI:38633	sodium channel blocker

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

Disease	Relation	SNOMED_ID	DOID
Tachyarrhythmia	indication	6285003

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sodium channel protein type 4 subunit alpha	Ion channel	P35499	SCN4A_HUMAN	BLOCKER	IC50	4.38		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.69		CHEMBL

External reference:

ID	Source
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