ethionamide 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 | 181.95 | 38.79 | 45 | 763 | 17323 | 46667931 |
| Tuberculosis | 79.67 | 38.79 | 21 | 787 | 10244 | 46675010 |
| Drug reaction with eosinophilia and systemic symptoms | 65.37 | 38.79 | 23 | 785 | 29525 | 46655729 |
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 | 108.81 | 41.65 | 35 | 852 | 20098 | 29931493 |
| Tuberculosis | 82.55 | 41.65 | 23 | 864 | 8054 | 29943537 |
| Electrocardiogram QT prolonged | 58.58 | 41.65 | 26 | 861 | 35809 | 29915782 |
| Tuberculoma of central nervous system | 46.60 | 41.65 | 8 | 879 | 287 | 29951304 |
| Neuropathy peripheral | 41.99 | 41.65 | 26 | 861 | 70449 | 29881142 |
| Hypothyroidism | 41.97 | 41.65 | 16 | 871 | 14947 | 29936644 |
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 |
| CHEBI has role | CHEBI:35679 | hypolipidemic agent |
| CHEBI has role | CHEBI:35816 | leprostatic |
| 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 (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 |
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 |
External reference:
| ID | Source |
|---|---|
| 4018059 | VUID |
| N0000146400 | NUI |
| D00591 | KEGG_DRUG |
| 4018059 | VANDF |
| C0015021 | UMLSCUI |
| CHEBI:4885 | CHEBI |
| CHEMBL1441 | ChEMBL_ID |
| DB00609 | DRUGBANK_ID |
| 2761171 | PUBCHEM_CID |
| D005000 | MESH_DESCRIPTOR_UI |
| 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 |