ethionamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1083 | 536-33-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A second-line antitubercular agent that inhibits mycolic acid synthesis.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.75 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 100.45 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 30, 1965 | FDA | WYETH PHARMS INC |
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 resistance | 205.57 | 43.86 | 50 | 783 | 18939 | 50585352 |
| Drug reaction with eosinophilia and systemic symptoms | 75.29 | 43.86 | 25 | 808 | 28399 | 50575892 |
| Electrocardiogram QT prolonged | 44.15 | 43.86 | 20 | 813 | 51866 | 50552425 |
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 resistance | 120.22 | 38.17 | 39 | 899 | 21501 | 29552088 |
| Electrocardiogram QT prolonged | 56.64 | 38.17 | 26 | 912 | 36111 | 29537478 |
| Tuberculoma of central nervous system | 40.57 | 38.17 | 7 | 931 | 241 | 29573348 |
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 |
|---|---|---|---|---|---|---|
| Drug resistance | 284.88 | 37.88 | 83 | 1793 | 35019 | 64461837 |
| Electrocardiogram QT prolonged | 88.43 | 37.88 | 44 | 1832 | 79404 | 64417452 |
| Drug reaction with eosinophilia and systemic symptoms | 84.85 | 37.88 | 38 | 1838 | 54179 | 64442677 |
| Neuropathy peripheral | 69.72 | 37.88 | 43 | 1833 | 117482 | 64379374 |
| Tuberculoma of central nervous system | 67.41 | 37.88 | 12 | 1864 | 542 | 64496314 |
| Anaemia | 56.85 | 37.88 | 62 | 1814 | 378618 | 64118238 |
| Vomiting | 48.51 | 37.88 | 69 | 1807 | 551048 | 63945808 |
| Hypothyroidism | 46.68 | 37.88 | 23 | 1853 | 40434 | 64456422 |
| Drug-induced liver injury | 43.12 | 37.88 | 23 | 1853 | 47620 | 64449236 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J04AD03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF TUBERCULOSIS Thiocarbamide derivatives |
| FDA EPC | N0000175483 | Antimycobacterial |
| CHEBI has role | CHEBI:33231 | antitubercular agents |
| CHEBI has role | CHEBI:35679 | antilipemic drugs |
| CHEBI has role | CHEBI:35816 | leprostatic drugs |
| CHEBI has role | CHEBI:50185 | fatty acid synthesis inhibitors |
| CHEBI has role | CHEBI:50266 | Prodrugs |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000963 | Antimetabolites |
| MeSH PA | D000995 | Antitubercular Agents |
| MeSH PA | D054872 | Fatty Acid Synthesis Inhibitors |
| MeSH PA | D000960 | Hypolipidemic Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute tuberculosis | indication | 25629007 | |
| Pulmonary tuberculosis | indication | 154283005 | DOID:2957 |
| Pulmonary Mycobacterium avium complex infection | indication | 186342000 | |
| Tuberculosis of meninges | off-label use | 58437007 | |
| Leprosy | off-label use | 81004002 | DOID:1024 |
| Atypical mycobacterial infection | off-label use | 111812000 | |
| Alcoholism | contraindication | 7200002 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Hepatic failure | contraindication | 59927004 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.43 | acidic |
| pKa2 | 5.85 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Enzyme | INHIBITOR | DRUGBANK | CHEMBL | |||||
| Catalase-peroxidase | Enzyme | WOMBAT-PK | |||||||
| Polyphenol oxidase 2 | Enzyme | IC50 | 5.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018059 | VUID |
| N0000146400 | NUI |
| D00591 | KEGG_DRUG |
| 4018059 | VANDF |
| C0015021 | UMLSCUI |
| CHEBI:4885 | CHEBI |
| CHEMBL1441 | ChEMBL_ID |
| DB00609 | DRUGBANK_ID |
| D005000 | MESH_DESCRIPTOR_UI |
| 2761171 | PUBCHEM_CID |
| 867 | INN_ID |
| OAY8ORS3CQ | UNII |
| 4127 | RXNORM |
| 4700 | MMSL |
| d01100 | MMSL |
| 002851 | NDDF |
| 32800009 | SNOMEDCT_US |
| 414148003 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Trecator | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0008-4117 | TABLET, FILM COATED | 250 mg | ORAL | NDA | 25 sections |