bromperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antipsychotics, haloperidol derivatives | 407 | 10457-90-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
bromine-substituted for chlorine in haloperidol; RN given refers to unlabeled parent cpd; structure
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | O |
| 10 | mg | P |
| 3.30 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.09 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.98 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0.50 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1973 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AD06 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Butyrophenone derivatives |
| MeSH PA | D014150 | Antipsychotic Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
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 | 8.36 | 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 | ANTAGONIST | Ki | 8.43 | WOMBAT-PK | KEGG DRUG | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | EC50 | 9.02 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7.10 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.50 | WOMBAT-PK | |||||
| Histamine H1 receptor | GPCR | Ki | 6.16 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.12 | PDSP | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 5.75 | PDSP | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 5.15 | PDSP | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 5.77 | PDSP | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 5.32 | PDSP | |||||
| D(1A) dopamine receptor | GPCR | Ki | 7 | WOMBAT-PK | |||||
| D(4) dopamine receptor | GPCR | Ki | 7.80 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| D01101 | KEGG_DRUG |
| 19777 | RXNORM |
| C1369894 | UMLSCUI |
| CHEBI:31305 | CHEBI |
| CHEMBL28218 | ChEMBL_ID |
| DB12401 | DRUGBANK_ID |
| C006820 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2448 | PUBCHEM_CID |
| 3737 | INN_ID |
| LYH6F7I22E | UNII |
| 725571009 | SNOMEDCT_US |
| 006754 | NDDF |
Pharmaceutical products:
None