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flunarizine 🐶 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 | 1200 | 52468-60-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.02 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.20 % | 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 |
| BA (Bioavailability) | 80 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 35 | |||
| kinase-selectivity-class | AKT3,AXL,ERBB2 | 3 | |||
| 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 |
|---|---|---|---|---|---|---|
| Serotonin syndrome | 124.13 | 38.11 | 37 | 1133 | 37850 | 90589427 |
| Drug ineffective | 85.97 | 38.11 | 96 | 1074 | 1384202 | 89243075 |
| Off label use | 77.87 | 38.11 | 82 | 1088 | 1102170 | 89525107 |
| Drug ineffective for unapproved indication | 77.77 | 38.11 | 30 | 1140 | 66614 | 90560663 |
| Withdrawal syndrome | 73.67 | 38.11 | 22 | 1148 | 22502 | 90604775 |
| Medication overuse headache | 71.70 | 38.11 | 13 | 1157 | 1488 | 90625789 |
| Drug eruption | 45.05 | 38.11 | 17 | 1153 | 35390 | 90591887 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Therapy partial responder | 93.80 | 78.22 | 25 | 451 | 19996 | 42600863 |
| Product use in unapproved indication | 82.27 | 78.22 | 40 | 436 | 184416 | 42436443 |
| Paraesthesia | 79.71 | 78.22 | 30 | 446 | 73429 | 42547430 |
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 |
|---|---|---|---|---|---|---|
| Off label use | 123.03 | 41.57 | 125 | 1417 | 1500060 | 109087697 |
| Product use in unapproved indication | 106.83 | 41.57 | 70 | 1472 | 447307 | 110140450 |
| Drug ineffective | 101.85 | 41.57 | 114 | 1428 | 1520426 | 109067331 |
| Therapy partial responder | 72.69 | 41.57 | 25 | 1517 | 37036 | 110550721 |
| Drug intolerance | 65.17 | 41.57 | 50 | 1492 | 406462 | 110181295 |
| Withdrawal syndrome | 60.87 | 41.57 | 21 | 1521 | 31359 | 110556398 |
| Bronchial hyperreactivity | 59.55 | 41.57 | 13 | 1529 | 3531 | 110584226 |
| Drug abuse | 57.90 | 41.57 | 34 | 1508 | 177377 | 110410380 |
| Treatment failure | 55.42 | 41.57 | 39 | 1503 | 277195 | 110310562 |
| Breast disorder | 53.22 | 41.57 | 11 | 1531 | 2303 | 110585454 |
| Paraesthesia | 50.89 | 41.57 | 37 | 1505 | 276484 | 110311273 |
| Medication overuse headache | 45.26 | 41.57 | 9 | 1533 | 1554 | 110586203 |
| Insomnia | 44.24 | 41.57 | 38 | 1504 | 360552 | 110227205 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07CA03 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS ANTIVERTIGO PREPARATIONS Antivertigo preparations |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
Related Drugs by ATC class:
N07CA Antivertigo preparations 3 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 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Voltage-dependent T-type calcium channel subunit alpha-1G | Ion channel | BLOCKER | Kd | 6.28 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | BLOCKER | Kd | 5.44 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Voltage-dependent T-type calcium channel subunit alpha-1I | Ion channel | BLOCKER | Kd | 6.08 | CHEMBL | SCIENTIFIC LITERATURE | |||
| D(1A) dopamine receptor | GPCR | Ki | 5.71 | DRUG MATRIX | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.93 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 8 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | Ki | 6.30 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.58 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.88 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.61 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.94 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.16 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.46 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.06 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.48 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 7.75 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.15 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.50 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.10 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.10 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.50 | DRUG MATRIX | |||||
| Sodium channel protein type 1 subunit alpha | Ion channel | IC50 | 6.20 | WOMBAT-PK | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 6.33 | DRUG MATRIX | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.53 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 6.36 | DRUG MATRIX | |||||
| Kappa-type opioid receptor | GPCR | IC50 | 5.02 | CHEMBL | |||||
| Delta-type opioid receptor | GPCR | IC50 | 5.44 | CHEMBL | |||||
| Voltage-dependent N-type calcium channel subunit alpha-1B | Ion channel | IC50 | 5.78 | CHEMBL | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.66 | DRUG MATRIX | |||||
| CAAX prenyl protease 2 | Enzyme | AC50 | 4.15 | CHEMBL | |||||
| Cannabinoid receptor 1 | GPCR | Ki | 5.62 | DRUG MATRIX | |||||
| Mu-type opioid receptor | GPCR | IC50 | 5.62 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.22 | DRUG MATRIX | |||||
| Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 7.42 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 5.96 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | IC50 | 6.64 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.37 | CHEMBL | |||||
| Sodium channel protein type 2 subunit alpha | Ion channel | IC50 | 6.31 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | Ki | 7.28 | CHEMBL | |||||
| CAAX prenyl protease 2 | Enzyme | AC50 | 5.46 | CHEMBL | |||||
| Potassium channel subfamily K member 2 | Ion channel | IC50 | 5.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167125 | NUI |
| D01303 | KEGG_DRUG |
| C0016295 | UMLSCUI |
| CHEBI:135652 | CHEBI |
| CHEMBL30008 | ChEMBL_ID |
| CHEMBL552659 | ChEMBL_ID |
| CHEMBL539027 | ChEMBL_ID |
| D005444 | MESH_DESCRIPTOR_UI |
| DB04841 | DRUGBANK_ID |
| 941361 | PUBCHEM_CID |
| 12488 | IUPHAR_LIGAND_ID |
| 2686 | INN_ID |
| 30484-77-6 | SECONDARY_CAS_RN |
| R7PLA2DM0J | UNII |
| 4459 | RXNORM |
| 003847 | NDDF |
| 003848 | NDDF |
| 1162382009 | SNOMEDCT_US |
| 418221001 | SNOMEDCT_US |
| 734509005 | SNOMEDCT_US |
| R7PLA2DM0J | INXIGHT DRUGS |
Pharmaceutical products:
None