Etomidate: Difference between revisions

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{{drugbox |
| IUPAC_name = ethyl&nbsp;3-[(1''R'')-1-phenylethyl]imidazole-<br>4-carboxylate
| image = Etomidate skeletal.svg
| image2 = Etomidate3d.png
| CAS_number = 33125-97-2
| ATC_prefix = N01
| ATC_suffix = AX07
| PubChem = 667484
| DrugBank = APRD00965
| C = 14 |H = 16 |N = 2 |O = 2
| molecular_weight = 244.289 [[Gram|g]]/[[Mole (unit)|mol]]
| protein_bound = 75%
| metabolism = [[Ester]] [[hydrolysis]]
| elimination_half-life = 75 [[Minutes|min]]
| excretion = [[Kidney|Renal]] (85%) and biliary (15%)
| pregnancy_category = D <small>([[United States|U.S.]])</small>
| legal_UK = POM
| routes_of_administration = [[Intravenous therapy|Intravenous]]
}}
'''Etomidate''' is a short acting [[intravenous]] anaesthetic agent used for the induction of [[general anaesthesia]] and for [[sedation]] for short procedures such as reduction of dislocated joints and [[cardioversion]]. It was discovered at [[Janssen Pharmaceutica]] in [[1964]].
==Drug class==
Etomidate, a hypnotic is a carboxylated [[imidazole]] derivative. Etomidate has [[anesthesia|anesthetic]] and [[amnesia|amnestic]] properties, but has no [[analgesia|analgesic]] properties.
==Uses==
Etomidate is commonly used in the emergency setting as part of a [[rapid sequence induction]] to induce anesthesia or for [[conscious sedation]]. It is often used in this setting since it has a rapid onset of action and a low cardiovascular risk profile, and therefore is less likely to cause a significant drop in blood pressure than other induction agents. 
In the operating room with a stable patient, anesthesiologists may choose an alternative induction agent, such as [[propofol]], [[thiopental]] or [[methohexital]]. (see Side effects below).
At the typical dose, anesthesia is induced for about 5–10 minutes even though the half-life of drug metabolism is approximately 75 minutes.  This is because etomidate is redistributed from the plasma to other tissues.
==Dosage==
The anaesthetic induction dose for adult humans is 0.3&nbsp;mg/kg intravenously, with a typical dose ranging from 20-40 mg. In common with all induction agents, etomidate causes loss of consciousness after one '''arm-brain circulation time'''. In very brief procedures such as cardioversion, a 10 mg dose may be used which may be repeated for effect.
==Metabolism==
Etomidate is highly protein bound in [[blood plasma]] and is metabolised by hepatic and plasma [[esterase]]s to inactive products. It exhibits a [[Exponential decay|bi-exponential decline]], with a redistribution [[half-life]] of 2–5 minutes and an elimination half-life of 68–75 minutes.
==Side effects==
The use of etomidate infusions for [[sedation]] of critically ill patients in [[intensive care unit]]s has been associated with increased mortality, which is due to suppression of [[steroid]] synthesis (both [[glucocorticoid]]s and [[mineralocorticoid]]s) in the [[adrenal cortex]]. This effect has been demonstrated after a single dose, and lasts about 24 hours. There is no evidence that a single induction dose of etomidate has any effect on morbidity or mortality. However, some sources advise giving a prophylactic dose of steroids (e.g. [[hydrocortisone]]) if etomidate is used.
Seizure-like activity is occasionally seen with anesthetic induction.  In the absence of concurrent EEG monitoring, it is difficult to ascribe this to cortical activity.  [[Myoclonic]] movement originating at the spinal cord level is often a likely mechanism.  Excitatory phenomena, and epileptiform movements and [[EEG]] activity may be observed during induction. Etomidate consistently increases the amplitude of somatosensory [[evoked potentials]] (in contrast to most anaesthetic agents).
Etomidate in the propylene glycol formulation may produce [[Pain and nociception|pain]] on injection, a side effect which is less likely with the lipid formulation.
There is a 30-fold difference between the [[effective dose]] and the [[lethal dose]] of etomidate, making it an extremely safe agent.
==Formulation==
Etomidate is usually presented as a clear colourless solution for injection containing 2&nbsp;mg/ml of etomidate in an aqueous solution of 35% [[propylene glycol]], although a [[lipid]] [[emulsion]] preparation (of equivalent strength) has also been introduced. Etomidate is presented as a [[racemic]] mixture, but only the D-[[isomer]] has pharmacological activity.
{{General anesthetics}}
[[Category:Anesthetics]]
[[Category:Imidazoles]]
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[[ru:Этомидат]]

Revision as of 00:42, 18 June 2014