encainide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Class I antiarrhythmics, procainamide and lidocaine derivatives | 1007 | 66778-36-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 8.11 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 27 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| CL (Clearance) | 13 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.26 % | Lombardo F, Berellini G, Obach RS |
| Vd (Volume of distribution) | 2.20 L/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.60 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 25 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1987 | YEAR INTRODUCED |
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 | C01BC08 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ic |
| 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 premature beats | indication | 17338001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.56 | acidic |
| pKa2 | 9.2 | 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 |
|---|---|
| 4019745 | VUID |
| N0000147836 | NUI |
| D07894 | KEGG_DRUG |
| 66794-74-9 | SECONDARY_CAS_RN |
| 4019356 | VANDF |
| 4019745 | VANDF |
| C0085251 | UMLSCUI |
| CHEBI:4788 | CHEBI |
| CHEMBL315838 | ChEMBL_ID |
| CHEMBL2106155 | ChEMBL_ID |
| DB01228 | DRUGBANK_ID |
| D016700 | MESH_DESCRIPTOR_UI |
| 48041 | PUBCHEM_CID |
| 4472 | INN_ID |
| SY3J0147NB | UNII |
| 281189 | RXNORM |
| 000631 | NDDF |
| 004486 | NDDF |
| 372749000 | SNOMEDCT_US |
| 46479001 | SNOMEDCT_US |
| 81017004 | SNOMEDCT_US |
Pharmaceutical products:
None