ethosuximide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1087 77-67-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ethosuximide
  • ethosuxide
  • etosuximid
  • 3-Methyl-3-ethylsuccinimide
An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.
  • Molecular weight: 141.17
  • Formula: C7H11NO2
  • CLOGP: 0.39
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 46.17
  • ALOGS: -0.15
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.25 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 39.20 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 25 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 118.30 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 93 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Nov. 2, 1960 FDA PARKE DAVIS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Aplastic anaemia 186.31 70.53 27 176 877 2357005
Seizure 92.85 70.53 26 177 24440 2333442
Intellectual disability 85.10 70.53 11 192 142 2357740
Drug ineffective 76.59 70.53 32 171 101592 2256290

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC N03AD01 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Succinimide derivatives
ATC N03AD51 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Succinimide derivatives
CHEBI has role CHEBI:35623 anticonvulsant
FDA EPC N0000175753 Anti-epileptic Agent
FDA PE N0000008486 Decreased Central Nervous System Disorganized Electrical Activity
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Absence seizure indication 79631006
Suicidal thoughts contraindication 6471006
Mood swings contraindication 18963009
Depressive disorder contraindication 35489007
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Kidney disease contraindication 90708001 DOID:557
Disease of blood AND/OR blood-forming organ contraindication 191124002 DOID:74
Acute intermittent porphyria contraindication 234422006 DOID:3890
Disease of liver contraindication 235856003 DOID:409
Neutropenic disorder contraindication 303011007 DOID:1227

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.31 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent T-type calcium channel subunit alpha-1G Ion channel BLOCKER WOMBAT-PK CHEMBL

External reference:

IDSource
D005013 MESH_DESCRIPTOR_UI
4018631 VUID
N0000146944 NUI
C0015043 UMLSCUI
D00539 KEGG_DRUG
5SEH9X1D1D UNII
1077 INN_ID
44790008 SNOMEDCT_US
4199 MMSL
4135 RXNORM
387244008 SNOMEDCT_US
4701 MMSL
d00227 MMSL
4018631 VANDF
001631 NDDF
3291 PUBCHEM_CID
CHEBI:4887 CHEBI
CHEMBL696 ChEMBL_ID
DB00593 DRUGBANK_ID
7182 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zarontin HUMAN PRESCRIPTION DRUG LABEL 1 0071-0237 CAPSULE 250 mg ORAL NDA 13 sections
Zarontin HUMAN PRESCRIPTION DRUG LABEL 1 0071-2418 SOLUTION 250 mg ORAL ANDA 13 sections
ETHOSUXIMIDE HUMAN PRESCRIPTION DRUG LABEL 1 0121-0670 SOLUTION 250 mg ORAL ANDA 13 sections
ETHOSUXIMIDE HUMAN PRESCRIPTION DRUG LABEL 1 23155-532 CAPSULE 250 mg ORAL ANDA 12 sections
ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 46672-641 SOLUTION 250 mg ORAL ANDA 12 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 59762-2250 CAPSULE 250 mg ORAL NDA AUTHORIZED GENERIC 13 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 59762-2350 SOLUTION 250 mg ORAL ANDA 13 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 61748-024 SOLUTION 250 mg ORAL ANDA 13 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 61748-025 CAPSULE 250 mg ORAL ANDA 14 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 63629-8005 CAPSULE, LIQUID FILLED 250 mg ORAL ANDA 13 sections
ETHOSUXIMIDE HUMAN PRESCRIPTION DRUG LABEL 1 64380-878 CAPSULE 250 mg ORAL ANDA 12 sections
ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 68382-443 CAPSULE 250 1 ORAL ANDA 13 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 69387-108 CAPSULE, LIQUID FILLED 250 mg ORAL ANDA 13 sections
Ethosuximide HUMAN PRESCRIPTION DRUG LABEL 1 69452-152 CAPSULE, LIQUID FILLED 250 mg ORAL ANDA 13 sections