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

Stem definition	Drug id	CAS RN
Class I antiarrhythmics, procainamide and lidocaine derivatives	2686	41708-72-9

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tocainide hydrochloride
tocainide
(RS)-Tocainide
(+/-)-Tocainide
DL-Tocainide
tocainide HCl

An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.

Molecular weight: 192.26
Formula: C11H16N2O
CLOGP: 0.26
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 55.12
ALOGS: -2.08
ROTB: 2

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1.20	g	O
1.20	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	38 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	89 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.80 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.87 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	12 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 9, 1984	FDA

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:

Source	Code	Description
ATC	C01BB03	CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ib
CHEBI has role	CHEBI:36333	local anesthetics
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:38633	sodium channel blockers
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 | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Ventricular arrhythmia	indication	44103008

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.41	acidic
pKa2	7.53	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 alpha subunit	Ion channel	P35498 P35499 Q01118 Q14524 Q15858 Q99250 Q9NY46 Q9UI33 Q9UQD0 Q9Y5Y9	SCN1A_HUMAN SCN4A_HUMAN SCN7A_HUMAN SCN5A_HUMAN SCN9A_HUMAN SCN2A_HUMAN SCN3A_HUMAN SCNBA_HUMAN SCN8A_HUMAN SCNAA_HUMAN	BLOCKER				CHEMBL	CHEMBL

External reference:

ID	Source
4017953	VUID
N0000179720	NUI
D02088	KEGG_DRUG
71395-14-7	SECONDARY_CAS_RN
4017953	VANDF
4019950	VANDF
C0085237	UMLSCUI
CHEBI:9611	CHEBI
CHEMBL1762	ChEMBL_ID
CHEMBL222944	ChEMBL_ID
CHEMBL387108	ChEMBL_ID
DB01056	DRUGBANK_ID
CHEMBL1200773	ChEMBL_ID
D016677	MESH_DESCRIPTOR_UI
38945	PUBCHEM_CID
4056	INN_ID
7309	IUPHAR_LIGAND_ID
27DXO59SAN	UNII
142145	RXNORM
5592	MMSL
d00392	MMSL
000625	NDDF
004482	NDDF
10555000	SNOMEDCT_US
2195004	SNOMEDCT_US
372479006	SNOMEDCT_US

Pharmaceutical products:

None