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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

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:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	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
EoM (Fraction excreted unchanged in urine)	0.20 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

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FDA Adverse Event Reporting System (Female)

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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	70.28	36.98	69	611	1044696	62443646
Withdrawal syndrome	57.78	36.98	17	663	19980	63468362
Drug eruption	39.91	36.98	14	666	28680	63459662

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FDA Adverse Event Reporting System (Male)

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FDA Adverse Event Reporting System (Geriatric)

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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	98.45	40.52	88	846	1080825	78662629
Bronchial hyperreactivity	63.83	40.52	13	921	3027	79740427
Breast disorder	56.32	40.52	11	923	2070	79741384
Product use in unapproved indication	50.31	40.52	33	901	250326	79493128
Drug intolerance	46.31	40.52	32	902	264087	79479367
Withdrawal syndrome	43.40	40.52	15	919	26839	79716615

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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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)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	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

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External reference:

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ID	Source
003847	NDDF
003848	NDDF
1162382009	SNOMEDCT_US
12488	IUPHAR_LIGAND_ID
2686	INN_ID
30484-77-6	SECONDARY_CAS_RN
418221001	SNOMEDCT_US
4459	RXNORM
734509005	SNOMEDCT_US
941361	PUBCHEM_CID

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Pharmaceutical products:

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