Etomidate (etomidate)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Etomidate is a sedative and hypnotic agent used for general anesthesia.

Etomidate, a carboxylated imidazole, is a sedative and hypnotic agent used for general anesthesia. The drug is structurally unrelated to other currently available IV anesthetics.

Following IV injection, etomidate has a rapid onset of action and will produce loss of consciousness within 1 arm-brain circulation time (i.e., usually within about 60 seconds). Etomidate produces its anesthetic activity by enhancing the activity of gamma-aminobutyric acid (GABA), the principal inhibitory neurotransmitter in the CNS, through modulation and direct activation of the GABAA receptor complex.

Etomidate is capable of producing all levels of CNS depression--from light sleep to deep coma--depending on the dosage; however, the drug has no analgesic activity. The degree of depression and duration of action depend on dosage, rate and route of administration, and pharmacokinetics of the drug. Substantial changes on the EEG appear to occur following induction doses of etomidate.

The EEG changes are indicative of the various stages of anesthesia and appear to be similar to those occurring following induction of anesthesia with barbiturates. Etomidate may decrease cerebral blood flow and intracranial pressure, while cerebral perfusion pressure is increased or maintained during induction of anesthesia.

Etomidate causes minimal hemodynamic changes and is associated with a decreased incidence and severity of cardiovascular effects compared with other IV anesthetic agents. Minor increases in cardiac index and slight decreases in heart rate, systemic vascular resistance, and arterial blood pressure have been reported with use of etomidate. In addition, equivalent induction doses of etomidate cause less respiratory depression than propofol or barbiturates.

Increases in carbon dioxide tension (PCO2) have been reported with administration of etomidate.

Some data suggest that etomidate usually reduces intraocular pressure (IOP).

The pharmacokinetic profile of etomidate is characterized by a rapid distribution from blood into CNS, rapid clearance from the brain, and substantial tissue uptake. Following the usual induction dose (0.3 mg/kg) of etomidate, duration of hypnosis is short (about 3-10 minutes) and dose dependent. The elimination half-life of etomidate is about 1.25-5 hours.

The drug is rapidly metabolized in the liver, principally by hydrolysis, to form etomidate carboxylic acid, which appears to be pharmacologically inactive. About 75% of an administered dose is excreted in urine within 24 hours, mainly (about 80%) as the carboxylic acid metabolite, while 13 and 10% of a dose are excreted in feces and bile, respectively.

Generic name: etomidate

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Etomidate:

  • Administration Of General Anesthesia
  • General Anesthesia Adjunct

Also known as: Adjunct General Anesthesia.

Dosing

Dosage of etomidate should be adjusted according to individual requirements and response, age, physical and clinical status, underlying pathologic conditions (e.g., shock, intestinal obstruction, malnutrition, anemia, burns, advanced malignancy, ulcerative colitis, uremia, alcoholism), and the type and amount of premedication or concomitant medication(s). In addition, dosage of the drug should be titrated to clinical effect.

Drug interactions

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Contraindications

Known hypersensitivity to etomidate.

Adverse reactions

The most frequent adverse effects associated with IV use of etomidate are transient venous pain at the injection site and transient skeletal muscle movements (i.e., myoclonus), which occur in about 20% (range: 1-42%) and 32% (range: 23-63%) of patients, respectively. Although generally mild to moderate in severity, such adverse effects can occasionally be severe.

Most (74%) cases of transient skeletal muscle movements have been classified as myoclonic, but tonic movements (10%), ocular movements (9%), and averting movements (7%) also have been noted. Such movements are usually bilateral (of the arms, legs, shoulders, neck, chest wall, trunk, and/or all 4 extremities, with one or more muscle groups predominating), with an electroencephalogram (EEG) suggesting that they are manifestations of cortical disinhibition in the absence of evidence of seizure activity. Alternatively, muscle movements may be unilateral or predominate on one side (e.g., predominance of movement of the arm in which the IV was started), or a mixture of bilateral and unilateral types may occur. The incidence of skeletal muscle movements, particularly those considered disturbing, has been minimized with IV administration of fentanyl immediately before induction of anesthesia with etomidate.

Other adverse effects reported in patients receiving etomidate include hyperventilation, hypoventilation, apnea (duration: 5-90 seconds), laryngospasm, hiccups and snoring (may be associated with partial upper airway obstruction), hypertension, hypotension, arrhythmias (e.g., tachycardia, bradycardia), and postoperative nausea and vomiting.

Precautions

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ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data