flupirtine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1215	56995-20-1

Description:

Molecule

Description

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:

Dose	Unit	Route
0.40	g	O

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	28.16 µM/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:

Date	Agency	Company	Orphan
Jan. 1, 1986	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug-induced liver injury	149.46	40.48	44	844	40178	63447956
Paranasal sinus inflammation	41.47	40.48	7	881	488	63487646

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug-induced liver injury	224.91	66.95	52	281	66065	79677990

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Potassium voltage-gated channel subfamily KQT member 2	Ion channel	O43526	KCNQ2_HUMAN	ACTIVATOR	EC50	5		IUPHAR
Potassium voltage-gated channel subfamily KQT member 3	Ion channel	O43525	KCNQ3_HUMAN					WOMBAT-PK
Serine hydroxymethyltransferase, mitochondrial	Enzyme	P34897	GLYM_HUMAN		IC50	6.03		CHEMBL

External reference:

ID	Source
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