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

Stem definition	Drug id	CAS RN
	2220	15574-96-6

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pizotyline
pizotifen
pizotifen malate

Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.

Molecular weight: 295.44
Formula: C19H21NS
CLOGP: 4.70
LIPINSKI: 0
HAC: 1
HDO: 0
TPSA: 3.24
ALOGS: -4.62
ROTB: 0

Drug dosage:

Dose	Unit	Route
1.50	mg	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	78 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

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
Vestibular migraine	75.03	44.44	10	543	225	63488244
Clonus	74.01	44.44	15	538	4621	63483848
Hyperreflexia	70.32	44.44	15	538	5919	63482550
Therapeutic response changed	60.12	44.44	10	543	1035	63487434
Muscle twitching	52.46	44.44	15	538	19653	63468816
Serotonin syndrome	51.03	44.44	16	537	28666	63459803
Endometrial cancer	48.87	44.44	10	543	3215	63485254
Dyskinesia	45.26	44.44	15	538	31987	63456482

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
Clonus	69.65	45.89	15	614	6825	79736934
Hyperreflexia	66.61	45.89	15	614	8370	79735389
Muscle twitching	50.49	45.89	15	614	24749	79719010

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N02CX01	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Other antimigraine preparations
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D018689	Sensory System Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists
CHEBI has role	CHEBI:37956	antihistamines
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48876	muscarinic antagonists

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	8.8	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
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	8.62		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	ANTAGONIST	Ki	7.40		IUPHAR
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.12		CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	8.70		CHEMBL
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	8.85		CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.60		CHEMBL
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	8.70		CHEMBL

External reference:

ID	Source
N0000167169	NUI
D05523	KEGG_DRUG
CHEBI:50212	CHEBI
CHEMBL294951	ChEMBL_ID
93	IUPHAR_LIGAND_ID
DB06153	DRUGBANK_ID
8373	RXNORM
003497	NDDF
349963006	SNOMEDCT_US
395834002	SNOMEDCT_US
C0032036	UMLSCUI
D010918	MESH_DESCRIPTOR_UI
27400	PUBCHEM_CID
2693	INN_ID
0BY8440V3N	UNII

Pharmaceutical products:

None