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18 Cards in this Set
- Front
- Back
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What are the Imidazole drugs?
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Metomidate (Hypnodil)
and Etomidate (Amidate) |
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What is Hypnodil used for?
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Metomidate + Azeperone =
Swine Anesthetic in Europe, but taken off market. |
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What is Amidate used for?
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Small animal anesthesia
though Off-Label in US and Europe *Superior Induction agent in High-Risk Patients w/compromised CV fnxn. |
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The imidazoles are enantiomers - which form is pharmacologically active?
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R is active
(though it is made as a racemic mixture) |
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How is Metomidate prepared?
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Water Soluble
1% soln (pH 2.9) 5% soln (pH 2.4) |
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How is Etomidate prepared?
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Water Soluble - but Unstable
2mg/mL soln in 35% propylene glycol (pH 6.9) *HyperOsmolar -- may cause pain, phlebitis, or IV-hemolysis upon injection. |
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What is the mechanism for the imidazoles?
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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! |
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What is the general effect of Hypnodil?
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Induces a Surgical Plane of Anesthesia in Swine for 2-3 hours
(w/minimal resp/CV effects) |
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What is the general effect of Amidate?
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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) |
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Metomidate/Etomidate
is _______ times more potent than Metomidate/Etomidate |
Etomidate is 3.5x more potent than Metomidate
|
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What is the big advantage of Imidazoles over barbs and phenols?
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ZERO to Minimal
Respiratory and CV Depressant fx Non-Arrhythmogenic |
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If used alone, imidazoles may cause ______ during induction.
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Coughing
|
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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 |
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Describe the PK of Etomidate
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Vol-Dist is Large
Hits brain fast and rapidly redistributes. ~76% bound to Albumin. (thus low albumin means more active drug in plasma) |
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Can Etomidate be used during C-section?
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Yes.
Incomplete placental transfer AND fetal plasma concentrations rapidly decreased |
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How are Imidazoles Eliminated?
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Biotransformation
Mostly Hepatic (Ester Hydrolysis) some esterases also in Plasma |
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How does Etomidate clearance compare to Thio?
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Way faster - so accumulation is not a huge concern, you can readminister or drip the drug.
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