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

Stem definition	Drug id	CAS RN
	1087	77-67-8

Description:

Molecule	Description
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: 0.40 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

Molecule

Description

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: 0.40
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:

Dose	Unit	Route
1.25	g	O

ADMET properties:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	93 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Nov. 2, 1960	FDA	PARKE DAVIS

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
Multiple-drug resistance	200.08	45.75	42	1603	5128	63482249
Seizure	164.38	45.75	76	1569	132558	63354819
Aplastic anaemia	104.83	45.75	28	1617	9541	63477836
Drug ineffective	104.40	45.75	130	1515	1044635	62442742
Status epilepticus	100.59	45.75	30	1615	15203	63472174
Petit mal epilepsy	97.28	45.75	22	1623	3772	63483605
Intellectual disability	91.98	45.75	17	1628	1069	63486308
Generalised tonic-clonic seizure	85.33	45.75	31	1614	28985	63458392
Oropharyngeal oedema	81.58	45.75	13	1632	336	63487041
Epilepsy	65.23	45.75	25	1620	27040	63460337
Suicidal behaviour	60.63	45.75	14	1631	2625	63484752
Myoclonic epilepsy	53.14	45.75	11	1634	1243	63486134
Macroglossia	53.10	45.75	10	1635	695	63486682
Aggression	50.56	45.75	20	1625	23478	63463899

FDA Adverse Event Reporting System (Male)

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
Multiple-drug resistance	122.59	52.82	30	1230	5209	34950462
Petit mal epilepsy	121.75	52.82	27	1233	3051	34952620
Drug ineffective	105.41	52.82	103	1157	456648	34499023
Seizure	89.04	52.82	52	1208	104805	34850866
Myoclonic epilepsy	79.34	52.82	16	1244	1141	34954530
Tonic convulsion	78.74	52.82	16	1244	1185	34954486
Developmental delay	75.70	52.82	18	1242	2757	34952914
Ataxia	58.19	52.82	21	1239	13832	34941839
Status epilepticus	56.29	52.82	20	1240	12594	34943077

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
Petit mal epilepsy	276.51	41.65	58	2505	5669	79736156
Multiple-drug resistance	235.68	41.65	55	2508	8753	79733072
Seizure	165.64	41.65	92	2471	188742	79553083
Drug ineffective	131.85	41.65	166	2397	1080747	78661078
Generalised tonic-clonic seizure	130.25	41.65	50	2513	43860	79697965
Status epilepticus	129.22	41.65	43	2520	24998	79716827
Aplastic anaemia	85.41	41.65	29	2534	17876	79723949
Oropharyngeal oedema	75.58	41.65	13	2550	433	79741392
Myoclonic epilepsy	72.63	41.65	16	2547	1954	79739871
Tonic convulsion	70.73	41.65	16	2547	2204	79739621
Epilepsy	65.34	41.65	30	2533	40830	79700995
Intellectual disability	55.81	41.65	12	2551	1308	79740517
Drug resistance	55.24	41.65	27	2536	42186	79699639
Suicidal behaviour	54.73	41.65	14	2549	3233	79738592
Benzodiazepine drug level decreased	52.89	41.65	7	2556	35	79741790
Ataxia	51.67	41.65	22	2541	25017	79716808
Cerebellar atrophy	51.61	41.65	11	2552	1150	79740675
Developmental delay	50.97	41.65	11	2552	1220	79740605
Macroglossia	45.80	41.65	10	2553	1171	79740654
Drug interaction	45.50	41.65	61	2502	415122	79326703
Somnolence	44.31	41.65	46	2517	238935	79502890

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N03AD01	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Succinimide derivatives
ATC	N03AD51	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Succinimide derivatives
FDA PE	N0000008486	Decreased Central Nervous System Disorganized Electrical Activity
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:176497	geroprotectors
CHEBI has role	CHEBI:194338	T-type calcium channel blockers
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents
FDA EPC	N0000175753	Anti-epileptic Agent

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.31	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
Voltage-dependent T-type calcium channel subunit alpha-1G	Ion channel	O43497	CAC1G_HUMAN	BLOCKER				WOMBAT-PK	CHEMBL

External reference:

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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zarontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0237	CAPSULE	250 mg	ORAL	NDA	19 sections
Zarontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0237	CAPSULE	250 mg	ORAL	NDA	19 sections
Zarontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-2418	SOLUTION	250 mg	ORAL	ANDA	19 sections
Zarontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-2418	SOLUTION	250 mg	ORAL	ANDA	19 sections
Zarontin	HUMAN PRESCRIPTION DRUG LABEL	1	0071-2418	SOLUTION	250 mg	ORAL	ANDA	19 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0670	SOLUTION	250 mg	ORAL	ANDA	19 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0670	SOLUTION	250 mg	ORAL	ANDA	19 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0670	SOLUTION	250 mg	ORAL	ANDA	19 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	23155-532	CAPSULE	250 mg	ORAL	ANDA	17 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	42806-708	CAPSULE	250 mg	ORAL	ANDA	18 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	42806-711	CAPSULE	250 mg	ORAL	ANDA	18 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	59762-2250	CAPSULE	250 mg	ORAL	NDA AUTHORIZED GENERIC	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	59762-2350	SOLUTION	250 mg	ORAL	ANDA	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	59762-2350	SOLUTION	250 mg	ORAL	ANDA	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	61748-024	SOLUTION	250 mg	ORAL	ANDA	17 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	61748-025	CAPSULE	250 mg	ORAL	ANDA	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	61748-025	CAPSULE	250 mg	ORAL	ANDA	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	63629-8005	CAPSULE, LIQUID FILLED	250 mg	ORAL	ANDA	18 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	64380-878	CAPSULE	250 mg	ORAL	ANDA	12 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	64380-878	CAPSULE	250 mg	ORAL	ANDA	12 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	17 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	69387-108	CAPSULE, LIQUID FILLED	250 mg	ORAL	ANDA	19 sections
Ethosuximide	HUMAN PRESCRIPTION DRUG LABEL	1	69452-152	CAPSULE, LIQUID FILLED	250 mg	ORAL	ANDA	19 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	71335-1763	CAPSULE	250 mg	ORAL	ANDA	12 sections
ETHOSUXIMIDE	HUMAN PRESCRIPTION DRUG LABEL	1	71335-1763	CAPSULE	250 mg	ORAL	ANDA	12 sections