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ethosuximide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1087 | 77-67-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
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 | 277.02 | 46.81 | 59 | 2290 | 7717 | 90618381 |
| Seizure | 248.76 | 46.81 | 106 | 2243 | 152523 | 90473575 |
| Drug ineffective | 145.76 | 46.81 | 177 | 2172 | 1384121 | 89241977 |
| Status epilepticus | 141.41 | 46.81 | 41 | 2308 | 18833 | 90607265 |
| Intellectual disability | 140.67 | 46.81 | 25 | 2324 | 1261 | 90624837 |
| Petit mal epilepsy | 139.39 | 46.81 | 31 | 2318 | 4927 | 90621171 |
| Generalised tonic-clonic seizure | 128.22 | 46.81 | 44 | 2305 | 34859 | 90591239 |
| Aplastic anaemia | 118.18 | 46.81 | 33 | 2316 | 13236 | 90612862 |
| Oropharyngeal oedema | 80.87 | 46.81 | 13 | 2336 | 355 | 90625743 |
| Treatment failure | 76.52 | 46.81 | 63 | 2286 | 303865 | 90322233 |
| Aggression | 72.80 | 46.81 | 27 | 2322 | 26641 | 90599457 |
| Myoclonic epilepsy | 67.36 | 46.81 | 14 | 2335 | 1613 | 90624485 |
| Lupus-like syndrome | 60.12 | 46.81 | 28 | 2321 | 48818 | 90577280 |
| Suicidal behaviour | 59.57 | 46.81 | 14 | 2335 | 2830 | 90623268 |
| Atonic seizures | 57.84 | 46.81 | 11 | 2338 | 805 | 90625293 |
| Macroglossia | 50.89 | 46.81 | 10 | 2339 | 869 | 90625229 |
| Epilepsy | 49 | 46.81 | 29 | 2320 | 82177 | 90543921 |
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 |
|---|---|---|---|---|---|---|
| Drug ineffective | 162.54 | 54.27 | 168 | 1776 | 630029 | 41989362 |
| Seizure | 152.12 | 54.27 | 84 | 1860 | 120477 | 42498914 |
| Multiple-drug resistance | 142.61 | 54.27 | 38 | 1906 | 7284 | 42612107 |
| Developmental delay | 124.99 | 54.27 | 29 | 1915 | 3153 | 42616238 |
| Petit mal epilepsy | 121.03 | 54.27 | 29 | 1915 | 3621 | 42615770 |
| Myoclonic epilepsy | 108.49 | 54.27 | 23 | 1921 | 1651 | 42617740 |
| Status epilepticus | 102.41 | 54.27 | 35 | 1909 | 15543 | 42603848 |
| Somnolence | 99.74 | 54.27 | 68 | 1876 | 141037 | 42478354 |
| Ataxia | 97.36 | 54.27 | 34 | 1910 | 16091 | 42603300 |
| Tonic convulsion | 91.72 | 54.27 | 20 | 1924 | 1639 | 42617752 |
| Generalised tonic-clonic seizure | 74.43 | 54.27 | 32 | 1912 | 26347 | 42593044 |
| Treatment failure | 60.93 | 54.27 | 37 | 1907 | 62587 | 42556804 |
| Electroencephalogram abnormal | 60.43 | 54.27 | 16 | 1928 | 2976 | 42616415 |
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 | 325.69 | 35.76 | 70 | 3576 | 7477 | 110578176 |
| Multiple-drug resistance | 296.78 | 35.76 | 72 | 3574 | 13163 | 110572490 |
| Seizure | 245.17 | 35.76 | 127 | 3519 | 221058 | 110364595 |
| Status epilepticus | 217.86 | 35.76 | 68 | 3578 | 31503 | 110554150 |
| Drug ineffective | 209.17 | 35.76 | 251 | 3395 | 1520289 | 109065364 |
| Generalised tonic-clonic seizure | 166.79 | 35.76 | 64 | 3582 | 54616 | 110531037 |
| Ataxia | 143.37 | 35.76 | 49 | 3597 | 30059 | 110555594 |
| Intellectual disability | 129.84 | 35.76 | 26 | 3620 | 1953 | 110583700 |
| Treatment failure | 123.58 | 35.76 | 89 | 3557 | 277145 | 110308508 |
| Myoclonic epilepsy | 110.58 | 35.76 | 24 | 3622 | 2667 | 110582986 |
| Somnolence | 109.16 | 35.76 | 85 | 3561 | 297364 | 110288289 |
| Developmental delay | 100.62 | 35.76 | 20 | 3626 | 1445 | 110584208 |
| Aplastic anaemia | 94.38 | 35.76 | 34 | 3612 | 24274 | 110561379 |
| Drug resistance | 84.82 | 35.76 | 40 | 3606 | 56334 | 110529319 |
| Tonic convulsion | 80.59 | 35.76 | 19 | 3627 | 3055 | 110582598 |
| Oropharyngeal oedema | 74.70 | 35.76 | 13 | 3633 | 452 | 110585201 |
| Epilepsy | 68.30 | 35.76 | 42 | 3604 | 100167 | 110485486 |
| Drug interaction | 63.39 | 35.76 | 80 | 3566 | 500103 | 110085550 |
| Suicidal behaviour | 53.33 | 35.76 | 14 | 3632 | 3483 | 110582170 |
| Benzodiazepine drug level decreased | 52.71 | 35.76 | 7 | 3639 | 35 | 110585618 |
| Psychotic disorder | 52.56 | 35.76 | 28 | 3618 | 50909 | 110534744 |
| Atonic seizures | 51.39 | 35.76 | 11 | 3635 | 1143 | 110584510 |
| Off label use | 49.00 | 35.76 | 133 | 3513 | 1500052 | 109085601 |
| Cerebellar atrophy | 48.87 | 35.76 | 11 | 3635 | 1442 | 110584211 |
| Social avoidant behaviour | 47.39 | 35.76 | 14 | 3632 | 5355 | 110580298 |
| Lupus-like syndrome | 46.58 | 35.76 | 24 | 3622 | 40768 | 110544885 |
| Aggression | 45.97 | 35.76 | 27 | 3619 | 59183 | 110526470 |
| Macroglossia | 43.42 | 35.76 | 10 | 3636 | 1451 | 110584202 |
| Behaviour disorder | 43.15 | 35.76 | 15 | 3631 | 9632 | 110576021 |
| Oliguria | 40.08 | 35.76 | 17 | 3629 | 18640 | 110567013 |
| SJS-TEN overlap | 35.91 | 35.76 | 9 | 3637 | 1865 | 110583788 |
| Hepatic adenoma | 35.86 | 35.76 | 7 | 3639 | 460 | 110585193 |
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 |
| MeSH PA | D000927 | Anticonvulsants |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
| CHEBI has role | CHEBI:53784 | antispasmodic drug |
| CHEBI has role | CHEBI:176497 | geroprotector |
| CHEBI has role | CHEBI:194338 | T-type calcium channel blocker |
| FDA EPC | N0000175753 | Anti-epileptic Agent |
Related Drugs by ATC class:
N03AD Succinimide derivatives 2 drugs
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 | 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 |
| 5SEH9X1D1D | INXIGHT DRUGS |
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 | 0071-2418 | 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 | 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 | 59762-2350 | SOLUTION | 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 | 62135-064 | SOLUTION | 250 mg | ORAL | ANDA | 12 sections |
| ETHOSUXIMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-790 | CAPSULE | 250 mg | ORAL | ANDA | 13 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 | 68382-443 | CAPSULE | 250 1 | ORAL | ANDA | 17 sections |
| Ethosuximide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68999-064 | SOLUTION | 250 mg | ORAL | ANDA | 12 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 |