Etomidate

DEA NFLIS-Drug Category -> Depressants and Tranquilizers

Pharmaceuticals -> Listed in ZINC15

Breast Feeding; Lactation; Milk, Human; Anesthetics, Intravenous; Hypnotics and Sedatives

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

142-142.8

67 °C

Warning

H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]

P261, P264, P270, P271, P273, P301+P317, P304+P340, P317, P330, P391, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 62 reports by companies from 6 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Transient inhibition of adrenal steroid synthesis is considered etomidate's most significant adverse effect. A single bolus dose causes a dose-dependent inhibition of 11-beta-hydroxylase lasting 6 to 12 hours. This enzyme is responsible for converting 11-deoxycortisol to cortisol, which results in adrenocortical suppression. Hence, it poses a theoretical risk of impairing a patient's ability to produce an adequate stress response. 80% of patients were found to have etomidate-induced adrenal inhibition at 12 hours, and most patients' suppression had resolved by 48 hours. Etomidate is no longer administered by continuous infusion because of the risks of sustained suppression of endogenous cortisol and aldosterone production.

According to manufacturer labeling, overdose can occur from too rapid and repeated injections. In addition, the administration of rapid injections is followed by a fall in blood pressure. There is no antidote for etomidate. In a suspected case of overdosage, etomidate should be discontinued, a patent airway established (intubate, if necessary) or maintained, and oxygen administered with assisted ventilation.

Drug Induced Liver Injury Rank (DILIrank 2.0)

Etomidate

vNo-DILI-concern

0

No match

DOI:10.1016/j.drudis.2016.02.015

N - Nervous system

QN - Nervous system

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.

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. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

Z22628B598

ETOMIDATE

Physiologic Effects [PE] - General Anesthesia

Established Pharmacologic Class [EPC] - General Anesthetic

Etomidate is a General Anesthetic. The physiologic effect of etomidate is by means of General Anesthesia.

AMIDATE(TM) ETOMIDATE

Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.

Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174)