benserazide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 314 | 322-35-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An inhibitor of DOPA DECARBOXYLASE that does not enter the central nervous system. It is often given with LEVODOPA in the treatment of parkinsonism to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system and reducing the required dose. It has no antiparkinson actions when given alone.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 11.10 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| S (Water solubility) | 10 mg/mL | Bocci G, Oprea TI, Benet LZ |
| fu (Fraction unbound in plasma) | 0.73 % | 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, 1990 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Drug interaction | 65.29 | 57.15 | 31 | 387 | 229100 | 63259504 |
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 |
|---|---|---|---|---|---|---|
| Product prescribing error | 53.10 | 44.55 | 18 | 620 | 44795 | 79698955 |
| General physical health deterioration | 51.17 | 44.55 | 30 | 608 | 275208 | 79468542 |
| Drug interaction | 49.16 | 44.55 | 34 | 604 | 415149 | 79328601 |
| Delirium | 45.30 | 44.55 | 19 | 619 | 84608 | 79659142 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D018726 | Anti-Dyskinesia Agents |
| MeSH PA | D000978 | Antiparkinson Agents |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:48407 | antiparkinson agent |
| CHEBI has role | CHEBI:48560 | dopaminergic agents |
| CHEBI has role | CHEBI:59321 | aromatic-L-amino-acid decarboxylase inhibitors |
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 | 3.67 | acidic |
| pKa2 | 11.55 | acidic |
| pKa3 | 12.19 | acidic |
| pKa4 | 13.97 | acidic |
| pKa5 | 6.88 | Basic |
| pKa6 | 3.1 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Aromatic-L-amino-acid decarboxylase | Enzyme | WOMBAT-PK | |||||||
| Estrogen receptor beta | Nuclear hormone receptor | IC50 | 5.52 | CHEMBL | |||||
| SUMO-activating enzyme | Enzyme | IC50 | 4.63 | CHEMBL | |||||
| Hexokinase-2 | Kinase | IC50 | 5.26 | CHEMBL | |||||
| Zinc finger protein mex-5 | Cytosolic other | EC50 | 6.95 | CHEMBL | |||||
| Cytoplasmic zinc-finger protein | Unclassified | EC50 | 4.43 | CHEMBL | |||||
| Genome polyprotein [Cleaved into: P1; Capsid protein VP0 | Unclassified | IC50 | 5.62 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01653 | KEGG_DRUG |
| 14919-77-8 | SECONDARY_CAS_RN |
| 1374 | RXNORM |
| C0005014 | UMLSCUI |
| CHEBI:64187 | CHEBI |
| CHEMBL1096979 | ChEMBL_ID |
| CHEMBL1255778 | ChEMBL_ID |
| DB12783 | DRUGBANK_ID |
| D001545 | MESH_DESCRIPTOR_UI |
| 2327 | PUBCHEM_CID |
| 5150 | IUPHAR_LIGAND_ID |
| 3026 | INN_ID |
| 762OS3ZEJU | UNII |
| 391821005 | SNOMEDCT_US |
| 391822003 | SNOMEDCT_US |
| 420240007 | SNOMEDCT_US |
| 003682 | NDDF |
| 003683 | NDDF |
Pharmaceutical products:
None