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18 Cards in this Set

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What are the Imidazole drugs?
Metomidate (Hypnodil)
and
Etomidate (Amidate)
What is Hypnodil used for?
Metomidate + Azeperone =

Swine Anesthetic in Europe, but taken off market.
What is Amidate used for?
Small animal anesthesia

though Off-Label in US and Europe

*Superior Induction agent in High-Risk Patients w/compromised CV fnxn.
The imidazoles are enantiomers - which form is pharmacologically active?
R is active
(though it is made as a racemic mixture)
How is Metomidate prepared?
Water Soluble
1% soln (pH 2.9)
5% soln (pH 2.4)
How is Etomidate prepared?
Water Soluble - but Unstable
2mg/mL soln in 35% propylene glycol (pH 6.9)

*HyperOsmolar -- may cause pain, phlebitis, or IV-hemolysis upon injection.
What is the mechanism for the imidazoles?
Just like barbs and phenols - Allosteric Site on GABAa

enhances benzodiazepines and GABA
The principle effect of the imidazoles is?

Are they analgesic?
Hypnosis

NO!
What is the general effect of Hypnodil?
Induces a Surgical Plane of Anesthesia in Swine for 2-3 hours

(w/minimal resp/CV effects)
What is the general effect of Amidate?
Rapid Hypnosis (less than 20 seconds)
Short Anesthesia (8-15 minutes)

Reduces Cerebral blood flow and O2 consumption.
Can Tx Epileptic Episodes and Seizures.
(odd because EEG effects mostly like barbs, but with a few spikes)
Metomidate/Etomidate

is _______ times more potent than

Metomidate/Etomidate
Etomidate is 3.5x more potent than Metomidate
What is the big advantage of Imidazoles over barbs and phenols?
ZERO to Minimal
Respiratory and CV Depressant fx

Non-Arrhythmogenic
If used alone, imidazoles may cause ______ during induction.
Coughing
Imidazoles inhibit what enzyme?

What effect does this have?
11B-hydroxylase

Can't turn Cholesterol into Cortisol
No Cortisol/Aldosterone production 2-6 hours after injection.

Thus LONG TERM admin should be avoided, and use caution in patients with Addison's Dz
Describe the PK of Etomidate
Vol-Dist is Large
Hits brain fast and rapidly redistributes.

~76% bound to Albumin.
(thus low albumin means more active drug in plasma)
Can Etomidate be used during C-section?
Yes.

Incomplete placental transfer AND fetal plasma concentrations rapidly decreased
How are Imidazoles Eliminated?
Biotransformation
Mostly Hepatic (Ester Hydrolysis)
some esterases also in Plasma
How does Etomidate clearance compare to Thio?
Way faster - so accumulation is not a huge concern, you can readminister or drip the drug.