Indication |
Used in the induction of general anesthesia. |
Pharmacodynamics |
Etomidate is a non-barbiturate hypnotic that acts at the level
of the reticular-activating system to produce anesthesia. Etomidate is
an imidazole compound that appears to depress CNS function via GABA.
Duration of action is intermediate between thiopental and methohexital,
and recovery from a single dose is rapid with little residual
depression. Like the barbiturates and propofol, etomidate is does not
induce analgesia. Etomidate induces unconsciousness within one
circulation time. Recovery is rapid as a result of extensive
redistribution and rapid metabolism. |
Mechanism of action |
Etomidate binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. |
Absorption |
Not Available |
Volume of distribution |
Not Available |
Protein binding |
76%, primarily to serum albumin. |
Metabolism |
Hepatic. Metabolized rapidly by ester hydrolysis to inactive metabolites. |
Route of elimination |
Approximately 75% of the administered dose is excreted in the urine during the first day after injection. |
Half life |
75 minutes. |
Clearance |
Not Available |
Toxicity |
Undesirable side effects of etomidate that may limit its use
include pain on injection, myoclonus and adrenocortical suppression
lasting 4-6 hours following an induction dose. |