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pizotifen 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2220 | 15574-96-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.
|
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.044 | Moderate | 0.65 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.524 | Moderate | 0.65 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 29.107 | 10^-6 cm/s | Moderate | 0.65 |
| dh-clint | Dog hepatocyte intrinsic clearance | 88.105 | uL/min/10^6 cells | Moderate | 0.65 |
| dppb | Dog plasma protein binding (% unbound) | 5.050 | % | Moderate | 0.65 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 11.840 | % | Moderate | 0.65 |
| herg | hERG pIC50 | 5.457 | pIC50 | Moderate | 0.65 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.936 | uL/min/10^6 cells | Moderate | 0.65 |
| hlm-clint | Human liver microsomal intrinsic clearance | 10.093 | uL/min/mg protein | Moderate | 0.65 |
| hppb | Human plasma protein binding (% unbound) | 6.440 | % | Moderate | 0.65 |
| kinase-safety-class | ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK4,PDPK1,PIM2,PRKDC,STK33,TEK,TGFBR1,TTK | 30 | |||
| kinase-selectivity-class | AXL,TTK | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.311 | Moderate | 0.65 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 193.642 | Moderate | 0.65 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.860 | Moderate | 0.65 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.102 | Moderate | 0.65 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.65 | |
| pppb | Pig plasma protein binding (% unbound) | 12.890 | % | Moderate | 0.65 |
| rh-clint | Rat hepatocyte intrinsic clearance | 353.997 | uL/min/10^6 cells | Moderate | 0.65 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 28.100 | % | Moderate | 0.65 |
| rppb | Rat plasma protein binding (% unbound) | 7.840 | % | Moderate | 0.65 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 668.344 | uM | Moderate | 0.65 |
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 | 73.77 | 53.89 | 10 | 823 | 242 | 90627372 |
| Clonus | 69.91 | 53.89 | 15 | 818 | 5735 | 90621879 |
| Neovascularisation | 68.33 | 53.89 | 12 | 821 | 1618 | 90625996 |
| Hyperreflexia | 67.72 | 53.89 | 15 | 818 | 6642 | 90620972 |
| Therapeutic response changed | 57.24 | 53.89 | 10 | 823 | 1307 | 90626307 |
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 |
|---|---|---|---|---|---|---|
| Neovascularisation | 68.59 | 46.63 | 12 | 921 | 1725 | 110586641 |
| Clonus | 64.97 | 46.63 | 15 | 918 | 8701 | 110579665 |
| Hyperreflexia | 63.70 | 46.63 | 15 | 918 | 9470 | 110578896 |
| Paradoxical drug reaction | 47.87 | 46.63 | 12 | 921 | 9805 | 110578561 |
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 | D000928 | Antidepressive Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:37956 | histamine antagonist |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:48876 | muscarinic antagonist |
Related Drugs by ATC class:
N02CX Other antimigraine preparations 4 drugs
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 | 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:
| ID | Source |
|---|---|
| N0000167169 | NUI |
| D05523 | KEGG_DRUG |
| CHEBI:50212 | CHEBI |
| CHEMBL294951 | ChEMBL_ID |
| 93 | IUPHAR_LIGAND_ID |
| DB06153 | DRUGBANK_ID |
| 235747 | RXNORM |
| 003497 | NDDF |
| 003498 | NDDF |
| 1371019001 | SNOMEDCT_US |
| 322845001 | SNOMEDCT_US |
| 349963006 | SNOMEDCT_US |
| 395834002 | SNOMEDCT_US |
| C0032036 | UMLSCUI |
| D010918 | MESH_DESCRIPTOR_UI |
| 27400 | PUBCHEM_CID |
| 2693 | INN_ID |
| 0BY8440V3N | UNII |
| 0BY8440V3N | INXIGHT DRUGS |
Pharmaceutical products:
None