Ethionamide: Difference between revisions
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{{Ethionamide}} | {{Ethionamide}} | ||
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==Overview== | ==Overview== | ||
Ethionamide (2-ethylthioisonicotinamide, Trecator SC) is an [[antibiotic]] used in the treatment of [[tuberculosis]]. It was [[1956 in science#Medicine|discovered in 1956]].<ref name="GTCABoard">{{cite web| publisher= Global Tuberculosis Community Advisory Board | url= http://www.tbonline.info/posts/2011/8/24/ethionamide/ | title= Ethionamide | work= TB Online | quote= 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 [[Multi-drug-resistant tuberculosis|MDR]] and [[Extensively drug-resistant tuberculosis|XDR TB]]. It was discovered in 1956. Ethionamide is used as part of a South Africa’s standard regimen to treat MDR TB.| accessdate}}</ref> | |||
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. | 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. | ||
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It is a [[prodrug]]<ref name="pmid11823459">{{cite journal |author=Vannelli TA, Dykman A, Ortiz de Montellano PR |title=The anti-tuberculosis drug ethionamide is activated by a flavoprotein monooxygenase |journal=J. Biol. Chem. |volume=277 |issue=15 |pages=12824–9 |year=2002 |month=April |pmid=11823459 |doi=10.1074/jbc.M110751200 |url=http://www.jbc.org/cgi/pmidlookup?view=long&pmid=11823459}}</ref> and as a [[thioamide]], it is used in [[regimen]]s to treat [[multi-drug-resistant tuberculosis|multi-drug-resistant]] and [[extensively drug-resistant tuberculosis|extensively drug-resistant]] tuberculosis.<ref name="GTCABoard"/> | It is a [[prodrug]]<ref name="pmid11823459">{{cite journal |author=Vannelli TA, Dykman A, Ortiz de Montellano PR |title=The anti-tuberculosis drug ethionamide is activated by a flavoprotein monooxygenase |journal=J. Biol. Chem. |volume=277 |issue=15 |pages=12824–9 |year=2002 |month=April |pmid=11823459 |doi=10.1074/jbc.M110751200 |url=http://www.jbc.org/cgi/pmidlookup?view=long&pmid=11823459}}</ref> and as a [[thioamide]], it is used in [[regimen]]s to treat [[multi-drug-resistant tuberculosis|multi-drug-resistant]] and [[extensively drug-resistant tuberculosis|extensively drug-resistant]] tuberculosis.<ref name="GTCABoard"/> | ||
It has been proposed for use in combination with [[gatifloxacin]].<ref name="pmid12878502">{{cite journal |author=Cynamon MH, Sklaney M |title=Gatifloxacin and ethionamide as the foundation for therapy of tuberculosis |journal=Antimicrob. Agents Chemother. |volume=47 |issue=8 |pages=2442–4 |year=2003 |month=August |pmid=12878502 |pmc=166105 |doi= 10.1128/AAC.47.8.2442-2444.2003|url=http://aac.asm.org/cgi/pmidlookup?view=long&pmid=12878502}}</ref> | It has been proposed for use in combination with [[gatifloxacin]].<ref name="pmid12878502">{{cite journal |author=Cynamon MH, Sklaney M |title=Gatifloxacin and ethionamide as the foundation for therapy of tuberculosis |journal=Antimicrob. Agents Chemother. |volume=47 |issue=8 |pages=2442–4 |year=2003 |month=August |pmid=12878502 |pmc=166105 |doi= 10.1128/AAC.47.8.2442-2444.2003|url=http://aac.asm.org/cgi/pmidlookup?view=long&pmid=12878502}}</ref> | ||
==Category== | ==Category== | ||
Antimycobacterial | Antimycobacterial | ||
==US Brand Names== | ==US Brand Names== | ||
TRECATOR<sup>®</sup> | |||
==FDA Package Insert== | ==FDA Package Insert== | ||
'''[[Ethionamide description|Description]]''' | '''[[Ethionamide description|Description]]''' | ||
Revision as of 02:52, 31 December 2013
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 | Compatibility, Reconstitution, and Stability | Directions For Use | How Supplied | Labels and Packages
Mechanisms 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)