Etomidate (R16659) is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia and for sedation for short procedures such as reduction of dislocated joints, tracheal intubation and cardioversion. Etomidate selectively interacts with β2- and β3-subunit containing GABAA receptors. Etomidate treatment demonstrated neuroprotective effect on the neuronal tissue against the diabetic oxidative damage. Etomidate is highly protein bound in blood plasma and is metabolised by hepatic and plasma esterases to inactive products. It exhibits a bi-exponential decline. Etomidate is a useful agent for carefully conducted procedural sedation because it provides effective, brief, deep sedation with little hemodynamic compromise.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 20 mg/mL
Ethanol 40 mg/mL
Distinct structural requirements for the direct and indirect actions of the anaesthetic etomidate at GABA(A) receptors.
Moody EJ, et al. Toxicol Lett. 1998 Nov 23;100-101:209-15. PMID: 10049144.
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