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lorcainide 🐶 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 | 1607 | 59729-31-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 2.40 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 17.98 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 6.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 16 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.15 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 6.50 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 30 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 39 | |||
| kinase-selectivity-class | AKT3,AXL,EIF2AK3,GRK2,PDK4,PRKCD | 6 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
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 | C01BC07 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ic |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| CHEBI has role | CHEBI:38070 | anti-arrhythmia drug |
Related Drugs by ATC class:
C01BC Antiarrhythmics, class Ic 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.18 | 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 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:
| ID | Source |
|---|---|
| D04778 | KEGG_DRUG |
| 58934-46-6 | SECONDARY_CAS_RN |
| C0065183 | UMLSCUI |
| CHEBI:135568 | CHEBI |
| CHEMBL87543 | ChEMBL_ID |
| CHEMBL3085477 | ChEMBL_ID |
| DB13653 | DRUGBANK_ID |
| C015970 | MESH_SUPPLEMENTAL_RECORD_UI |
| 42884 | PUBCHEM_CID |
| 4143 | INN_ID |
| KGJ2T0N7IQ | UNII |
| 008142 | NDDF |
| 008143 | NDDF |
Pharmaceutical products:
None