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mephenytoin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiepileptics, hydantoin derivatives | 1695 | 50-12-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.97 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.516 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.207 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 102.802 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.228 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 64.800 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 76.680 | % | High | 1 |
| herg | hERG pIC50 | 4.063 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.045 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 2.838 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 71.760 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,STK33,TEK | 24 | |||
| kinase-selectivity-class | AXL,GRK2,SIK2,STK33,TEK | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.447 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.898 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 62.830 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.279 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 70.290 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.866 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 93.430 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 61.590 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 837.529 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 23, 1946 | FDA | NOVARTIS |
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 | N03AB04 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Hydantoin derivatives |
| ATC | N03AB54 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Hydantoin derivatives |
| FDA PE | N0000008486 | Decreased Central Nervous System Disorganized Electrical Activity |
| MeSH PA | D000927 | Anticonvulsants |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
| FDA EPC | N0000175753 | Anti-epileptic Agent |
Related Drugs by ATC class:
N03AB Hydantoin derivatives 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Epilepsy | indication | 84757009 | DOID:1826 |
| Localization-related epilepsy | indication | 230381009 | DOID:2234 |
| Motor cortex epilepsy | indication | 267592003 | |
| Epilepsy characterized by intractable complex partial seizures | indication | 442481002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.7 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel alpha subunit | Ion channel | BLOCKER | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018756 | VUID |
| N0000147059 | NUI |
| D00375 | KEGG_DRUG |
| 4018756 | VANDF |
| C0025381 | UMLSCUI |
| CHEBI:6757 | CHEBI |
| CHEMBL861 | ChEMBL_ID |
| DB00532 | DRUGBANK_ID |
| D008617 | MESH_DESCRIPTOR_UI |
| 4060 | PUBCHEM_CID |
| 7223 | IUPHAR_LIGAND_ID |
| 1463 | INN_ID |
| R420KW629U | UNII |
| 258358 | RXNORM |
| 1926 | MMSL |
| 5048 | MMSL |
| d00941 | MMSL |
| 001621 | NDDF |
| 28344001 | SNOMEDCT_US |
| 417526007 | SNOMEDCT_US |
| R420KW629U | INXIGHT DRUGS |
Pharmaceutical products:
None