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cinnarizine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics/cerebral (or peripheral) vasodilators | 654 | 298-57-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 90 | mg | O |
| 90 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 83 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK | 43 | |||
| kinase-selectivity-class | AXL,ERBB2,GRK2,PDK4,SIK2 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 |
|---|---|---|---|---|---|---|
| Medication overuse headache | 83.25 | 29.78 | 15 | 1290 | 1486 | 90625656 |
| Vestibular migraine | 69.26 | 29.78 | 10 | 1295 | 242 | 90626900 |
| Therapeutic response changed | 52.74 | 29.78 | 10 | 1295 | 1307 | 90625835 |
| Endometrial cancer | 42.68 | 29.78 | 10 | 1295 | 3602 | 90623540 |
| Bipolar disorder | 33.64 | 29.78 | 10 | 1295 | 8975 | 90618167 |
| Basal ganglia haemorrhage | 31.86 | 29.78 | 6 | 1299 | 755 | 90626387 |
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 |
|---|---|---|---|---|---|---|
| Medication overuse headache | 103.43 | 30.36 | 18 | 1490 | 1545 | 110586246 |
| Vestibular migraine | 40.86 | 30.36 | 6 | 1502 | 173 | 110587618 |
| Portal tract inflammation | 31.53 | 30.36 | 5 | 1503 | 242 | 110587549 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06BX53 | NERVOUS SYSTEM PSYCHOANALEPTICS PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS Other psychostimulants and nootropics |
| ATC | N07CA02 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS ANTIVERTIGO PREPARATIONS Antivertigo preparations |
| ATC | N07CA52 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS ANTIVERTIGO PREPARATIONS Antivertigo preparations |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
| CHEBI has role | CHEBI:37956 | histamine antagonist |
| CHEBI has role | CHEBI:38215 | calcium channel blocker |
| CHEBI has role | CHEBI:48876 | muscarinic antagonist |
| CHEBI has role | CHEBI:50857 | anti-allergic agent |
| CHEBI has role | CHEBI:50919 | antiemetic |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
N06BX Other psychostimulants and nootropics 19 drugs
N07CA Antivertigo preparations 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Motion sickness | indication | 37031009 | DOID:2951 |
| Vertigo | indication | 399153001 | |
| Nausea | indication | 422587007 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | Ki | 6.04 | DRUG MATRIX | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.59 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.78 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.77 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.24 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.55 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.21 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.99 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.33 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 5.99 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.07 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 8.06 | DRUG MATRIX | |||||
| Histamine H4 receptor | GPCR | Ki | 6.85 | PDSP | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.22 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.79 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.29 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.02 | DRUG MATRIX | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.89 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 6.24 | DRUG MATRIX | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 6.36 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 5.72 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | ANTAGONIST | Ki | 7.88 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.97 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.30 | DRUG MATRIX | |||||
| Membrane-associated progesterone receptor component 1 | Membrane receptor | IC50 | 6.79 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| N0000167127 | NUI |
| D01295 | KEGG_DRUG |
| 2549 | RXNORM |
| C0008803 | UMLSCUI |
| CHEBI:31403 | CHEBI |
| N90 | PDB_CHEM_ID |
| CHEMBL43064 | ChEMBL_ID |
| DB00568 | DRUGBANK_ID |
| D002936 | MESH_DESCRIPTOR_UI |
| 1547484 | PUBCHEM_CID |
| 9072 | IUPHAR_LIGAND_ID |
| 1021 | INN_ID |
| 3DI2E1X18L | UNII |
| 003951 | NDDF |
| 349958007 | SNOMEDCT_US |
| 395955001 | SNOMEDCT_US |
| 3DI2E1X18L | INXIGHT DRUGS |
Pharmaceutical products:
None