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 | 201.66 | 56.12 | 32 | 125 | 2592 | 2355336 |
| Vomiting | 92.27 | 56.12 | 31 | 126 | 71571 | 2286357 |
| Anaemia | 90.93 | 56.12 | 26 | 131 | 34766 | 2323162 |
| Tuberculosis | 73.31 | 56.12 | 13 | 144 | 1922 | 2356006 |
| Electrocardiogram QT prolonged | 60.54 | 56.12 | 14 | 143 | 7800 | 2350128 |
| Neuropathy peripheral | 60.27 | 56.12 | 15 | 142 | 11417 | 2346511 |
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 |
|---|---|---|---|---|---|---|
| Tuberculosis | 95.56 | 48.44 | 18 | 173 | 1848 | 1744742 |
| Drug resistance | 91.54 | 48.44 | 19 | 172 | 3211 | 1743379 |
| Anaemia | 76.87 | 48.44 | 26 | 165 | 29431 | 1717159 |
| Vomiting | 73.94 | 48.44 | 27 | 164 | 38288 | 1708302 |
| Neuropathy peripheral | 62.14 | 48.44 | 17 | 174 | 9236 | 1737354 |
| Electrocardiogram QT prolonged | 60.50 | 48.44 | 15 | 176 | 5530 | 1741060 |
| Hypothyroidism | 54.87 | 48.44 | 12 | 179 | 2548 | 1744042 |
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 agent |
| CHEBI has role | CHEBI:35679 | antilipemic drug |
| CHEBI has role | CHEBI:35816 | leprostatic drug |
| CHEBI has role | CHEBI:50266 | prodrug |
| 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 |
|---|---|
| D005000 | MESH_DESCRIPTOR_UI |
| 4018059 | VUID |
| N0000146400 | NUI |
| C0015021 | UMLSCUI |
| D00591 | KEGG_DRUG |
| 414148003 | SNOMEDCT_US |
| 4127 | RXNORM |
| 32800009 | SNOMEDCT_US |
| 4700 | MMSL |
| d01100 | MMSL |
| 4018059 | VANDF |
| 002851 | NDDF |
| 2761171 | PUBCHEM_CID |
| CHEBI:4885 | CHEBI |
| CHEMBL1441 | ChEMBL_ID |
| DB00609 | DRUGBANK_ID |
| OAY8ORS3CQ | UNII |
| 867 | INN_ID |
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 | 13 sections |