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
not affected
• Contractility not affected
• BP not affected
RS
• Depression
• No inhibition of hypoxic
pulmonary vasoconstriction
• Involuntary movements
• Contraindicated in
• ↓ Tone
porphyria
• Epileptiform activity on EEG in 25%
• Antiplatelet activity
• ↓ ICP
• ↓ CPP and↓CMRO2 • Hypersensitivity and
• ↓ IOP histamine release (rare)
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)