Brand Name
Amidate
Broad category
Intravenous anesthetic/ ultrashort-acting nonbarbiturate hypnotic
Pharmacological class
carboxylated imidazole derivative
- Single enantiomer formulation (R)
MOA (primary)
Binds directly as GABA-A agonists mimicking inhibitory effects of GABA and increases the receptors affinity for endogenous GABA
Secondary effects
disinhibitory effects on parts of the nervous system that control extrapyrimidal motor activity (high incidence of myoclonus)
Indications
Induction, procedural sedation:
- Cardiac (stable hemodynamic profile)
- Trauma
- Elderly
- Low EF patients
- ECT (proconvulsant)
CV effects?
Minimal
- if sudden hypotension patient is likely acutely hypovolemic
Respiratory effects
less ventilatory depression than propofol or barbs
CNS
Decreased CBF
Decreased ICP
Decreased CMRO2
myoclonus, may reduce seizure threshold (proconvulsant)
GI
N/V
Burn on injection
Yes significant due to propylene glycol formulation
- pretreat with lidocaine
Histamine release?
No
Other significant effects
Yes, adrenal corticosuppression through 11-Beta-Hydroxylase inhibition. Decreases ability to turn LDL into cortisol (and aldosterone).
- lasts up to 48hrs
Absolute Contraindications
Adrenocortical suppression
Relative contraindications (precautions)
cautious in epilepsy and profound hypovolemia
Induction Dosing
0.2-0.3 mg/kg
Onset
30-60 seconds
Duration
3-5 mins
up to
5-15 mins (dose dependent)
Concentration
2 mg/mL
Metabolism
Hepatic enzymes and plasma esterase hydrolysis
Active metabolites
no
Elimination
85% renal
10-13% bile/feces
Protein binding
76%
Elimination Half-life
2-5 hours