debrisoquine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
quinoline derivatives 788 1131-64-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • debrisoquin
  • debrisoquine
  • isocaramidine
  • debrisoquin sulfate
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.
  • Molecular weight: 175.24
  • Formula: C10H13N3
  • CLOGP: 0.74
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 2
  • TPSA: 53.11
  • ALOGS: -2.32
  • ROTB: 0

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

PropertyValueReference
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 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.82 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Amine oxidase [flavin-containing] B Enzyme WOMBAT-PK
Amine oxidase [flavin-containing] A Enzyme WOMBAT-PK

External reference:

IDSource
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