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tocainide 🐶 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 | 2686 | 41708-72-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.179 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.564 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 13.677 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.176 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 88.330 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 87.940 | % | High | 1 |
| herg | hERG pIC50 | 4.199 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.426 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.811 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 87.570 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK | 27 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,CSF1R,DDR1,EPHB4,ERBB2,GRK2,MAPK7,PDK4,SIK2,SIK3,STK33 | 14 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.565 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.979 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 35.237 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 88.520 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.419 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 89.180 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.249 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 41.020 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 95.790 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 86.830 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 979.490 | uM | High | 1 |
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 |
| 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:36333 | local anaesthetic |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
| CHEBI has role | CHEBI:38633 | sodium channel blocker |
Related Drugs by ATC class:
C01BB Antiarrhythmics, class Ib 3 drugs
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 | 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 |
| DB01056 | DRUGBANK_ID |
| CHEMBL1200773 | ChEMBL_ID |
| D016677 | MESH_DESCRIPTOR_UI |
| 38945 | PUBCHEM_CID |
| 7309 | IUPHAR_LIGAND_ID |
| 4056 | INN_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