Brand and Other Names:Amidate
- Classes: General Anesthetics, Systemic
Dosing & Uses
Dosage Forms & Strengths
Cushing Syndrome (Off-label)
Inhibition of steroidogenesis in patients with Cushing syndrome
ICU continuous infusion: 0.04-0.05 mg/kg/hr IV; continuous monitoring required
- Used rarely; often toxic at doses required to reduce cortisol secretion
- Long-term use limited by the requirement for repeated IV administration
Dosage Forms & Strengths
General Anesthesia Induction
<10 years: Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Transient injection site pain (30-80%)
Skeletal muscle movements, mainly myoclonic (32%)
Apnea (duration: 5-90 seconds)
Snoring (may be associated with partial upper airway obstruction)
Controversial: Sepsis, septic shock
Lack of ventilatory support
Adrenal suppression (and prolonged therapy)
Prolonged IV infusion not recommended
Safety during labor and delivery not elucidated; not recommended
Pregnancy & Lactation
Pregnancy category: C
Lactation: Not known if excreted in breast milk; use caution
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Nonbarbiturate hypnotic used for the induction of anesthesia; lacks analgesic activity; has minimal cardiovascular effects
Cushing syndrome (off-label): Blocks 11-beta-hydroxylase
Blocks steroidogenesis; 0.3 mg/kg will reduce plasma cortisol for up to 24 hr
Does not affect cardiac metabolism; no depression of cardiac output or of peripheral or pulmonary circulation
Onset: Within 60 sec
Duration: 3-5 min due to redistribution from CNS
Protein bound: 76%
Vd: 2-4.5 L/kg
Hepatic and plasma esterases
Excretion: Urine, as inactive agent
Y-site: Ascorbic acid, vecuronium
Y-site: Alfentanil, atracurium, atropine, ephedrine, fentanyl, lidocaine, lorazepam, midazolam, mivacurium, morphine sulfate, pancuronium, phenylephrine, succinylcholine, sufentanil
Inject undiluted by direct IV injection over 30-60 sec; do not administer by prolonged IV infusion
Inject into large forearm vein
Consider lidocaine preadministration to minimize injection-site pain
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