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Etomidate: Induction Agent Overview

Etomidate is an induction agent used for patients with poor cardiovascular states. It is formulated as a lipid emulsion or solution to improve solubility and stability. Etomidate works by prolonging the opening of GABA chloride channels, causing hyperpolarization. It is metabolized primarily in the liver by esterases and has a short distribution phase. Potential side effects include adrenal suppression, pain on injection, myoclonus, and nausea.
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0% found this document useful (0 votes)
101 views4 pages

Etomidate: Induction Agent Overview

Etomidate is an induction agent used for patients with poor cardiovascular states. It is formulated as a lipid emulsion or solution to improve solubility and stability. Etomidate works by prolonging the opening of GABA chloride channels, causing hyperpolarization. It is metabolized primarily in the liver by esterases and has a short distribution phase. Potential side effects include adrenal suppression, pain on injection, myoclonus, and nausea.
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© © All Rights Reserved
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Etomidate

Imidazole derivative and an ester


Indications : induction agent in poor cardiovascular state eg dilated
cardiomyopathy, poor ejection fraction

Preparation :
• To increase solubility, it is formulated as a 0.2% solution at pH of 4.1 and
contain 35% propylene glycol OR in lipid emulsion 2mg/ml (20mg in 10ml)
• To improve stability and reduce its irritant properties of injection.

Dose- 0.3 mg/kg


MOA- increase duration of opening GABA chloride channels that cause
hyperpolarization
Pharmacokinetics
pH 8.1, pKa 4.24
^ Etomidate is 75% bound to albumin
^ actions are terminated by rapid distribution into tissues
(volume distribution 3L/kg)
^ elimination depends on hepatic metabolism and renal
excretion (excreted 90% in urine and bile 10%)
-Non-specific hepatic esterases, and possibly plasma cholinesterase,
hydrolyse etomidate to ethyl alcohol and its carboxylic acid metabolite.
-may also inhibit plasma cholinesterase.
EFFECTS

side effects
CVS CNS • Inhibits steroid synthesis- by inhibition of 11β and 17α-hydroxylase, for
• Most stable induction agent • Hypnosis 24 hourly after only 1 dose.

• Slight ↓ SVR • Tremor • Pain on injection in 25%


• Myocardial O2 consumption • Involuntary movements
not affected • Contraindicated in
• ↓ Tone
• Contractility not affected porphyria
• Epileptiform activity on EEG in 25%
• BP not affected • Antiplatelet activity
• ↓ ICP
RS
• ↓ CPP and↓CMRO2 • Hypersensitivity and
• Depression
• ↓ IOP histamine release (rare)
• No inhibition of hypoxic
pulmonary vasoconstriction GI
• Nausea and vomiting (especially in
conjunction with opioid)
side effects
• Inhibits steroid synthesis- by inhibition of 11β and 17α-
hydroxylase, for 24 hourly after only 1 dose.
---resulting in inhibition of cortisol and aldosterone synthesis

• Pain on injection in 25%

• Contraindicated in
porphyria

• Antiplatelet activity

• Hypersensitivity and
histamine release (rare)

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