benperidol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antipsychotics, haloperidol derivatives | 312 | 2062-84-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A butyrophenone with general properties similar to those of HALOPERIDOL. It has been used in the treatment of aberrant sexual behavior. (From Martindale, The Extra Pharmacopoeia, 30th ed, p567)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.50 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 8.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5.80 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1965 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Neuroleptic malignant syndrome | 119.84 | 99.30 | 30 | 577 | 27529 | 79716252 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05AD07 | 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 | D015259 | Dopamine Agents |
| MeSH PA | D018492 | Dopamine Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D014149 | Tranquilizing Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Antisocial behavior | indication | 60814007 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.93 | acidic |
| pKa2 | 8.12 | 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 | 10.57 | WOMBAT-PK | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | EC50 | 5.94 | WOMBAT-PK | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 8.47 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 9 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | Ki | 10.18 | WOMBAT-PK | |||||
| D(4) dopamine receptor | GPCR | Ki | 8.70 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000166794 | NUI |
| D02627 | KEGG_DRUG |
| 1373 | RXNORM |
| C0005013 | UMLSCUI |
| CHEBI:93403 | CHEBI |
| CHEMBL297302 | ChEMBL_ID |
| DB12867 | DRUGBANK_ID |
| D001544 | MESH_DESCRIPTOR_UI |
| 16363 | PUBCHEM_CID |
| 9215 | IUPHAR_LIGAND_ID |
| 1577 | INN_ID |
| 97O6X78C53 | UNII |
| 321391002 | SNOMEDCT_US |
| 391820006 | SNOMEDCT_US |
| 003934 | NDDF |
Pharmaceutical products:
None