bretylium 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quaternary ammonium compounds | 394 | 61-75-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 77 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 12.07 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 23 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 6, 1986 | FDA | INTL MEDICATION |
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 | C01BD02 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY ANTIARRHYTHMICS, CLASS I AND III Antiarrhythmics, class III |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ventricular arrhythmia | indication | 44103008 | |
| Ventricular fibrillation | indication | 71908006 | |
| Life-Threatening Ventricular Tachycardia | indication | ||
| Prevention of Ventricular Fibrillation | indication | ||
| Cardiac arrest | off-label use | 410429000 | DOID:0060319 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Low cardiac output syndrome | contraindication | 44088000 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Aortic valve stenosis | contraindication | 60573004 | DOID:1712 |
| Pulmonary hypertension | contraindication | 70995007 | DOID:6432 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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-dependent noradrenaline transporter | Transporter | SUBSTRATE | CHEMBL | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| Beta-2 adrenergic receptor | GPCR | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019638 | VUID |
| N0000171583 | NUI |
| D00645 | KEGG_DRUG |
| 151447 | RXNORM |
| C0006168 | UMLSCUI |
| CHEMBL1199080 | ChEMBL_ID |
| DB01158 | DRUGBANK_ID |
| CHEMBL1095292 | ChEMBL_ID |
| C045166 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2431 | PUBCHEM_CID |
| 7130 | IUPHAR_LIGAND_ID |
| RZR75EQ2KJ | UNII |
| 3352 | MMSL |
| 4296 | MMSL |
| d00005 | MMSL |
| 372774002 | SNOMEDCT_US |
| 56230001 | SNOMEDCT_US |
| 56613007 | SNOMEDCT_US |
| D001950 | MESH_DESCRIPTOR_UI |
| 927 | INN_ID |
| 4018742 | VANDF |
| 4019638 | VANDF |
| 59-41-6 | SECONDARY_CAS_RN |
| 001840 | NDDF |
| 004448 | NDDF |
Pharmaceutical products:
None