Etomidate MOA: Etomidate has a unique mechanism of action as a GABA-a modulator that requires:
Etomidate binds at an ___ site on the GABA-A receptor.
Etomidate enhances the effect of GABA by increasing ___ conductance and prolonging channel ___. Without GABA present, there is little to no channel opening → ___ effect.
GABA to be present for activation.
Etomidate binds at an allosteric site on the GABA-A receptor.
Etomidate enhances the effect of GABA by increasing chloride conductance and prolonging channel opening. Without GABA present, there is little to no channel opening → minimal effect.
Slide 14
Etomidate’s Carboxylated Imidazole ring is similar to the ring in __________, allowing it to be water-soluble in solution and lipid-soluble in the body.
Midazolam
When the ring is open, it is water soluble in solution. The ring closes in the body and becomes very lipid soluble.
Slide 14
Etomidate is typically prepared as a __________% solution for induction purposes.
How many mg per mL?
0.2%
2 mg per mL
Tex Wes Ref and PP: Etomidate’s dose for induction in adults is typically ____.
0.3 mg/kg
Tex Wes Ref: The onset on action of etomidate is about __ minute.
1 minute
The duration of action of etomidate is __ to _ minutes.
10 to 20 minutes.
True or False
There is no pain on injection with Etomidate
False
Pain on injection and it DOES NOT provide analgesia –> need to add something for pain.
True or false
The induction dose of Etomidate is the only dose. There is no change for elderly or sick.
True!
A rare but significant adverse effect of prolonged Etomidate use is ____ _____.
Adrenocortical Suppression
Etomidate can cause adrenocortical suppression due to inhibition of which enzyme?
11-Beta-Hydroxylase
11-B-Hydroxylase converts cholesterol to cortisol
What is the significance of 11β-Hydroxylase?
11β-Hydroxylase converts cholesterol directly into cortisol.
The duration of adrenocortical suppression caused by a single dose of Etomidate is ___ hours?
4-8 hours
Lowers post operative cortisol levels in healthy patients
In addition to adrenocortical suppression, Etomidate is also associated with a high incidence of ____:
Postoperative nausea and vomiting (PONV)
Corn: sometimes called VOMIDATE
Etomidate is considered worst for PONV of all induction drugs, up to ________% of patients.
PONV in 30% of patients (worst of all induction drugs)