All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
antihistaminics/cerebral (or peripheral) vasodilators	1200	52468-60-7

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: flunarizine sibelium flunarizine dihydrochloride flunarizine hydrochloride flunarizine HCl

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. Molecular weight: 404.51 Formula: C26H26F2N2 CLOGP: 6.34 LIPINSKI: 1 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -5.38 ROTB: 6

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.20 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.35 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

None

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 ineffective	58.49	37.44	59	550	819274	49785241
Withdrawal syndrome	49.30	37.44	15	594	17575	50586940

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 ineffective	79.00	41.26	72	741	840175	63657744
Bronchial hyperreactivity	65.36	41.26	13	800	2499	64495420
Breast disorder	57.85	41.26	11	802	1673	64496246
Product use in unapproved indication	48.12	41.26	29	784	176589	64321330
Therapy partial responder	42.59	41.26	12	801	10236	64487683
Drug intolerance	41.44	41.26	27	786	187965	64309954

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N07CA03	NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS ANTIVERTIGO PREPARATIONS Antivertigo preparations
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002121	Calcium Channel Blockers
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014665	Vasodilator 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	7.42	Basic
pKa2	3.42	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
Voltage-dependent T-type calcium channel subunit alpha-1G	Ion channel	O43497	CAC1G_HUMAN	BLOCKER	Kd	6.28		CHEMBL	SCIENTIFIC LITERATURE
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN	BLOCKER	Kd	5.44		CHEMBL	SCIENTIFIC LITERATURE
Voltage-dependent T-type calcium channel subunit alpha-1I	Ion channel	Q9P0X4	CAC1I_HUMAN	BLOCKER	Kd	6.08		CHEMBL	SCIENTIFIC LITERATURE
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	6.93		DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.66		DRUG MATRIX
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	8		DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	6.30		DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.58		DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.88		DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.61		DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.94		DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.16		DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.46		DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.06		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	7.48		DRUG MATRIX
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	7.75		DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.15		DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.50		DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.10		DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.10		DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.50		DRUG MATRIX
Sodium channel protein type 1 subunit alpha	Ion channel	P35498	SCN1A_HUMAN		IC50	6.20		WOMBAT-PK
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	6.33		DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.53		DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.36		DRUG MATRIX
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		IC50	5.02		CHEMBL
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN		IC50	5.44		CHEMBL
Voltage-dependent N-type calcium channel subunit alpha-1B	Ion channel	Q00975	CAC1B_HUMAN		IC50	5.78		CHEMBL
Cannabinoid receptor 1	GPCR	P21554	CNR1_HUMAN		Ki	5.62		DRUG MATRIX
CAAX prenyl protease 2	Enzyme	Q9Y256	FACE2_HUMAN		AC50	4.15		CHEMBL
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		IC50	5.62		CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.71		DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	6.22		DRUG MATRIX
Membrane-associated progesterone receptor component 1	Membrane receptor		PGRC1_RAT		Ki	7.42		DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	5.96		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		IC50	6.64		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	5.37		CHEMBL
Sodium channel protein type 2 subunit alpha	Ion channel		SCN2A_RAT		IC50	6.31		CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel		SCN1A_RAT SCN2A_RAT SCN3A_RAT		Ki	7.28		CHEMBL
CAAX prenyl protease 2	Enzyme		RCE1_YEAST		AC50	5.46		CHEMBL
Potassium channel subfamily K member 2	Ion channel		Q8HY88_BOVIN		IC50	5.60		CHEMBL

External reference:

ID	Source
N0000167125	NUI
D01303	KEGG_DRUG
C0016295	UMLSCUI
CHEBI:135652	CHEBI
CHEMBL30008	ChEMBL_ID
CHEMBL552659	ChEMBL_ID
D005444	MESH_DESCRIPTOR_UI
DB04841	DRUGBANK_ID
941361	PUBCHEM_CID
2686	INN_ID
30484-77-6	SECONDARY_CAS_RN
R7PLA2DM0J	UNII
4459	RXNORM
003847	NDDF
003848	NDDF
1162382009	SNOMEDCT_US
418221001	SNOMEDCT_US
734509005	SNOMEDCT_US
CHEMBL539027	ChEMBL_ID

Pharmaceutical products:

None