piribedil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vasodilators 2202 3605-01-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • piribedil methanesulfonate
  • piribedil maleate
  • ET-495
  • piribedil
  • trivastal
  • trivastan
  • piribedil hydrochloride
  • piribedil HCl
  • EU 4200
  • EU-4200
A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.
  • Molecular weight: 298.35
  • Formula: C16H18N4O2
  • CLOGP: 2.13
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 0
  • TPSA: 50.72
  • ALOGS: -2.28
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dropped head syndrome 55.04 47.52 7 403 123 53348533

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Fall 65.53 43.45 35 330 196166 32316995
Gambling disorder 58.07 43.45 11 354 1858 32511303
Facial bones fracture 54.30 43.45 11 354 2625 32510536
Malaise 43.64 43.45 26 339 177112 32336049

Pharmacologic Action:

SourceCodeDescription
ATC N04BC08 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
DOPAMINERGIC AGENTS
Dopamine agonists
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018491 Dopamine Agonists
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Parkinsonism indication 32798002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.95 Basic
pKa2 2.23 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
D(2) dopamine receptor GPCR AGONIST Ki 6.90 IUPHAR SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1A GPCR AGONIST Ki 6.40 IUPHAR
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 5.90 IUPHAR
Alpha-1A adrenergic receptor GPCR ANTAGONIST Ki 6.10 IUPHAR
Alpha-2B adrenergic receptor GPCR Ki 6.54 PDSP
Alpha-2A adrenergic receptor GPCR ANTAGONIST Ki 7.10 IUPHAR
Alpha-2C adrenergic receptor GPCR ANTAGONIST Ki 7.20 IUPHAR
D(4) dopamine receptor GPCR ANTAGONIST Ki 6.50 IUPHAR
Alpha-1D adrenergic receptor GPCR Ki 6.66 PDSP
Alpha-1B adrenergic receptor GPCR Ki 5.21 PDSP
D(3) dopamine receptor GPCR AGONIST Ki 6.60 IUPHAR

External reference:

IDSource
N0000167119 NUI
D07305 KEGG_DRUG
C0031979 UMLSCUI
CHEBI:92833 CHEBI
CHEMBL1371770 ChEMBL_ID
CHEMBL1256997 ChEMBL_ID
DB12478 DRUGBANK_ID
D010891 MESH_DESCRIPTOR_UI
4850 PUBCHEM_CID
49 IUPHAR_LIGAND_ID
2569 INN_ID
DO22K1PRDJ UNII
8353 RXNORM
005711 NDDF
713435009 SNOMEDCT_US

Pharmaceutical products:

None