Ethionamide
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Chetan Lokhande, M.B.B.S [2]
Overview
Ethionamide (2-ethylthioisonicotinamide, Trecator SC) is an antibiotic used in the treatment of tuberculosis. It was discovered in 1956.[1]
Ethionamide is activated by EthA, a mono-oxygenase in Mycobacterium tuberculosis, and binds NAD to form an adduct which inhibits InhA in the same way as isoniazid. Expression of the ethA gene is controlled by EthR, a transcriptional repressor. It is understood that improving ethA expression will increase the efficacy of ethionamide and so EthR inhibitors are of great interest to co-drug developers.
It is a prodrug[2] and as a thioamide, it is used in regimens to treat multi-drug-resistant and extensively drug-resistant tuberculosis.[1] It has been proposed for use in combination with gatifloxacin.[3]
Category
Antimycobacterial
US Brand Names
TRECATOR®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
The action may be through disruption of mycolic acid.[1][4]
References
- ↑ 1.0 1.1 1.2 "Ethionamide". TB Online. Global Tuberculosis Community Advisory Board.
Ethionamide is part of a group of drugs used in the treatment of drug resistant TB called thioamides. It is used as part of treatment regimens, generally involving 5 medicines, to treat MDR and XDR TB. It was discovered in 1956. Ethionamide is used as part of a South Africa’s standard regimen to treat MDR TB.
Text " accessdate" ignored (help) - ↑ Vannelli TA, Dykman A, Ortiz de Montellano PR (2002). "The anti-tuberculosis drug ethionamide is activated by a flavoprotein monooxygenase". J. Biol. Chem. 277 (15): 12824–9. doi:10.1074/jbc.M110751200. PMID 11823459. Unknown parameter
|month=ignored (help) - ↑ Cynamon MH, Sklaney M (2003). "Gatifloxacin and ethionamide as the foundation for therapy of tuberculosis". Antimicrob. Agents Chemother. 47 (8): 2442–4. doi:10.1128/AAC.47.8.2442-2444.2003. PMC 166105. PMID 12878502. Unknown parameter
|month=ignored (help) - ↑ Quémard A, Lanéelle G, Lacave C (1992). "Mycolic acid synthesis: a target for ethionamide in mycobacteria?". Antimicrob. Agents Chemother. 36 (6): 1316–21. PMC 190338. PMID 1416831. Unknown parameter
|month=ignored (help)