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

Stem definitionDrug idCAS RN
2220 15574-96-6

Description:

MoleculeDescription

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:

DoseUnitRoute
1.50 mg O

ADMET properties:

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

Approvals:

None

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
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 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
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:

SourceCodeDescription
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 levelDissociation constantType (acidic/basic)
pKa1 8.8 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
D(2) dopamine receptor GPCR Ki 8.62 CHEMBL
5-hydroxytryptamine receptor 1A GPCR ANTAGONIST Ki 7.40 IUPHAR
5-hydroxytryptamine receptor 2A GPCR Ki 8.12 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 8.70 CHEMBL
5-hydroxytryptamine receptor 2C GPCR Ki 8.85 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 7.60 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8.70 CHEMBL

External reference:

IDSource
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