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Etomidate derivatives: Novel pharmaceutical agents in anesthesia
Etomidate is an imidazole derivative that possesses important sedative properties employed in anesthesia practice, however, etomidate has a number of well-know side effects which limit its use in certain subpopulations and over long periods of time, mostly related to dose-dependent adrenal suppressi...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Medknow Publications & Media Pvt Ltd
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5791251/ https://www.ncbi.nlm.nih.gov/pubmed/29416230 http://dx.doi.org/10.4103/0970-9185.222521 |
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author | Malapero, Raymond J. Zaccagnino, Michael P. Brovman, Ethan Y. Kaye, Alan David Urman, Richard D. |
author_facet | Malapero, Raymond J. Zaccagnino, Michael P. Brovman, Ethan Y. Kaye, Alan David Urman, Richard D. |
author_sort | Malapero, Raymond J. |
collection | PubMed |
description | Etomidate is an imidazole derivative that possesses important sedative properties employed in anesthesia practice, however, etomidate has a number of well-know side effects which limit its use in certain subpopulations and over long periods of time, mostly related to dose-dependent adrenal suppression. This review focuses on novel etomidate derivatives with an emphasis on pharmacological properties which afford improved safety profile and potentially desirable clinical effects. The pharmacology and clinical investigation of some of these etomidate derivatives, e.g. cyclopropyl-methoxycarbonyl, carboetomidate metomidate, methoxycarbonyl-etomidate, cyclopropyl-methoxycarbonyl metomidate (CPMM), and dimethyl-methoxycarbonyl metomidate, are discussed in detail. The increased potency and decreased metabolite build-up of CPMM potentially makes it a very favorable drug, particularly in the setting of prolonged infusions. Further, when compared with etomidate, CPMM produces lower plasma cytokine concentration and improved survival in lipopolysaccharide inflammatory sepsis models. |
format | Online Article Text |
id | pubmed-5791251 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | Medknow Publications & Media Pvt Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-57912512018-02-07 Etomidate derivatives: Novel pharmaceutical agents in anesthesia Malapero, Raymond J. Zaccagnino, Michael P. Brovman, Ethan Y. Kaye, Alan David Urman, Richard D. J Anaesthesiol Clin Pharmacol Review Article Etomidate is an imidazole derivative that possesses important sedative properties employed in anesthesia practice, however, etomidate has a number of well-know side effects which limit its use in certain subpopulations and over long periods of time, mostly related to dose-dependent adrenal suppression. This review focuses on novel etomidate derivatives with an emphasis on pharmacological properties which afford improved safety profile and potentially desirable clinical effects. The pharmacology and clinical investigation of some of these etomidate derivatives, e.g. cyclopropyl-methoxycarbonyl, carboetomidate metomidate, methoxycarbonyl-etomidate, cyclopropyl-methoxycarbonyl metomidate (CPMM), and dimethyl-methoxycarbonyl metomidate, are discussed in detail. The increased potency and decreased metabolite build-up of CPMM potentially makes it a very favorable drug, particularly in the setting of prolonged infusions. Further, when compared with etomidate, CPMM produces lower plasma cytokine concentration and improved survival in lipopolysaccharide inflammatory sepsis models. Medknow Publications & Media Pvt Ltd 2017 /pmc/articles/PMC5791251/ /pubmed/29416230 http://dx.doi.org/10.4103/0970-9185.222521 Text en Copyright: © 2018 Journal of Anaesthesiology Clinical Pharmacology http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms. |
spellingShingle | Review Article Malapero, Raymond J. Zaccagnino, Michael P. Brovman, Ethan Y. Kaye, Alan David Urman, Richard D. Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title | Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title_full | Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title_fullStr | Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title_full_unstemmed | Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title_short | Etomidate derivatives: Novel pharmaceutical agents in anesthesia |
title_sort | etomidate derivatives: novel pharmaceutical agents in anesthesia |
topic | Review Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5791251/ https://www.ncbi.nlm.nih.gov/pubmed/29416230 http://dx.doi.org/10.4103/0970-9185.222521 |
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