Etomidate Mechanism Of Action

The action enhances the inhibitory effect of gaba on the central nervous system by causing chloride channel opening events which leads to membrane hyperpolarization. Etomidate is a general anesthetic without analgesic activity.

Mechanism Of Adrenal Suppression By Etomidate Etomidate

Etomidate has been shown to suppress adrenocortical function through inhibition of 11β hydroxylase which is a required enzyme to produce cortisol corticosterone and aldosterone.

Etomidate mechanism of action. Etomidate binds at a distinct binding site associated with a cl ionopore at the gaba a receptor increasing the duration of time for which the cl ionopore is open. Nci thesaurus ncit etomidate is the ethyl ester of 1 1r 1 phenylethyl 1h imidazole 5 carboxylic acid. The gabaa receptor plays a central role in the etomidate mechanism of action etomidate exerts its effects on the receptor by binding directly to a specific site or sites on the protein and allosterically enhancing the apparent affinity of gaba for its receptor.

Intravenous injection of etomidate produces anesthesia characterized by a rapid onset of action usually within one minute. Mechanism of action etomidate contains a carboxylated imidazole ring containing anesthetic compound r 1 ethyl 1 a methylbenzyl imidazole 5 carboxylate and is structurally unrelated to other anesthetic agents. Etomidate produces clinical responses such as hypnosis elevations in arterial carbon dioxide tension reduced cortisol plasma levels and similar to thiopental a transient 20 to 30 decrease in cerebral blood flow.

Mechanism of action etomidate appears to facilitate gabaminergic neurotransmission by increasing the number of available gaba receptors possibly by displacing endogenous inhibitors of gaba binding. Etomidate mechanism of action is shown here. The imidazole ring provides water solubility in acidic solutions and lipid solubility at physiological ph.

At much higher concentrations etomidate activate receptors in the absence of gaba. The mechanism underlying etomidate s well described suppression of adrenal steroid synthesis relates to the imidazole ring in its chemical structure. The post synaptic inhibitory effect of gaba in the thalamus is therefore prolonged.

Etomidate is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia and sedation for short procedures such as reduction of dislocated joints tracheal intubation cardioversion and electroconvulsive therapy. It was developed at janssen pharmaceutica in 1964 and was introduced as an intravenous agent in 1972 in europe and in 1983 in the united states. Duration of anesthesia is dose dependent but relatively brief usually three to five minutes when an average dose of 0 3 mg kg is employed.

Anesthesiology And Pain Medicine Effect Of Etomidate Versus