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

Stem definitionDrug idCAS RN
1215 56995-20-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flupirtin maleate
  • flupirtine maleate
  • flupirtine
  • katadolon
  • Molecular weight: 304.33
  • Formula: C15H17FN4O2
  • CLOGP: 3.05
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 89.27
  • ALOGS: -3.62
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 28.16 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.60 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.15 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 8.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1986 YEAR INTRODUCED

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
Drug-induced liver injury 155.20 41.20 44 844 28051 50576185

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Drug-induced liver injury 230.89 65.55 52 281 47591 64450808

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02BG07 NERVOUS SYSTEM
ANALGESICS
OTHER ANALGESICS AND ANTIPYRETICS
Other analgesics and antipyretics
MeSH PA D000700 Analgesics
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents

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 8.83 acidic
pKa2 7.26 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
Potassium voltage-gated channel subfamily KQT member 2 Ion channel ACTIVATOR EC50 5 IUPHAR
Potassium voltage-gated channel subfamily KQT member 3 Ion channel WOMBAT-PK
Serine hydroxymethyltransferase, mitochondrial Enzyme IC50 6.03 CHEMBL

External reference:

IDSource
4025785 VUID
N0000179138 NUI
D07978 KEGG_DRUG
75507-68-5 SECONDARY_CAS_RN
4025785 VANDF
4025786 VANDF
C0060583 UMLSCUI
CHEBI:94646 CHEBI
CHEMBL255044 ChEMBL_ID
CHEMBL1256752 ChEMBL_ID
DB06623 DRUGBANK_ID
C034161 MESH_SUPPLEMENTAL_RECORD_UI
53276 PUBCHEM_CID
2598 IUPHAR_LIGAND_ID
3976 INN_ID
MOH3ET196H UNII
236774 RXNORM
006784 NDDF
006785 NDDF

Pharmaceutical products:

None