debrisoquine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quinoline derivatives | 788 | 1131-64-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An adrenergic neuron-blocking drug similar in effects to GUANETHIDINE. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 29 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 12 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 24.46 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1965 | 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 | C02CC04 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Guanidine derivatives |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D013565 | Sympatholytics |
| CHEBI has role | CHEBI:35674 | antihypertensive drugs |
| CHEBI has role | CHEBI:37962 | adrenergic agents |
| CHEBI has role | CHEBI:66991 | sympatholytic drug |
| CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
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 | 10.82 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Amine oxidase [flavin-containing] B | Enzyme | WOMBAT-PK | |||||||
| Amine oxidase [flavin-containing] A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000166976 | NUI |
| D03664 | KEGG_DRUG |
| 3118 | RXNORM |
| C0011082 | UMLSCUI |
| CHEBI:34665 | CHEBI |
| CHEMBL169901 | ChEMBL_ID |
| DB04840 | DRUGBANK_ID |
| 581-88-4 | SECONDARY_CAS_RN |
| 2966 | PUBCHEM_CID |
| 003838 | NDDF |
| 350602000 | SNOMEDCT_US |
| 396010003 | SNOMEDCT_US |
| D003647 | MESH_DESCRIPTOR_UI |
| CHEMBL1255735 | ChEMBL_ID |
| CHEMBL1593558 | ChEMBL_ID |
| 1968 | INN_ID |
| X31CDK040E | UNII |
Pharmaceutical products:
None