ajmaline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiarrhythmics, ajmaline derivatives | 100 | 4360-12-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An alkaloid found in the root of RAUWOLFIA SERPENTINA, among other plant sources. It is a class Ia antiarrhythmic agent that apparently acts by changing the shape and threshold of cardiac action potentials.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 4 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.24 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 7.30 hours | Lombardo F, Berellini G, Obach RS |
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 | C01BA05 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class Ia |
| 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 | |
| Supraventricular arrhythmia | indication | 72654001 | |
| Cardiac arrhythmia | indication | 698247007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.52 | acidic |
| pKa2 | 7.56 | Basic |
| pKa3 | 6.62 | 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 | INHIBITOR | DRUGBANK | DRUGBANK | |||||
| Potassium voltage-gated channel subfamily D member 3 | Ion channel | INHIBITOR | IC50 | 7.58 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Potassium voltage-gated channel subfamily A member 5 | Ion channel | INHIBITOR | IC50 | 7.77 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| N0000166953 | NUI |
| D00199 | KEGG_DRUG |
| 4410-48-4 | SECONDARY_CAS_RN |
| 423 | RXNORM |
| C0001888 | UMLSCUI |
| CHEBI:28462 | CHEBI |
| AJM | PDB_CHEM_ID |
| CHEMBL2105617 | ChEMBL_ID |
| DB01426 | DRUGBANK_ID |
| D000404 | MESH_DESCRIPTOR_UI |
| 6100671 | PUBCHEM_CID |
| 1PON08459R | UNII |
| 1156230005 | SNOMEDCT_US |
| 003818 | NDDF |
Pharmaceutical products:
None