Metabolite-inactive etomidate analogues alleviating suppression on adrenal function in Beagle dogs

Owing to rapid generation in body, the metabolites of etomidate softdrug are able to accumulate in either the brain or periphery and subsequently affect the recovery from anaesthesia or cause corticosteroid suppression. This study was designed to investigate the ability of two etomidate analogues (E...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2017-03, Vol.99, p.343-349
Main Authors: Yang, Jun, Kang, Yi, Wang, Bin, Yang, Linghui, Liu, Jin, Zhang, Wensheng
Format: Article
Language:English
Subjects:
Adrenal Glands - drug effects
Adrenocorticotropic Hormone
Animals
Corticosterone - blood
Dogs
Etomidate - administration & dosage
Etomidate - analogs & derivatives
Etomidate analogues
Female
Hydrocortisone - blood
Hypnotics and Sedatives - administration & dosage
Inactive metabolite
Intravenous anaesthetic drug
Male
Reduced corticosteroid suppression
Slow metabolism
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Summary:Owing to rapid generation in body, the metabolites of etomidate softdrug are able to accumulate in either the brain or periphery and subsequently affect the recovery from anaesthesia or cause corticosteroid suppression. This study was designed to investigate the ability of two etomidate analogues (ET-26, ET-42) with inactive metabolites to provide anaesthesia with lesser corticosteroid suppression. The 50% effective dose (ED50) of ET-26, ET-42, Etomidate, MOC-ET (an etomidate softdrug) and CPMM (an improved etomidate softdrug) required to induce anaesthesia intravenously in Beagle dogs were 1.44mg/kg, 0.72mg/kg, 0.43mg/kg 23.12mg/kg and 0.59mg/kg, respectively. After adrenocorticotropic hormone (ACTH) stimulation, the serum concentrations of cortisol and corticosterone in the ET-26, ET-42 and CPMM groups were similar to those of controls, and significantly higher than those of the etomidate and MOC-etomidate groups (P
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2016.12.041