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Amidate

Amidate - General Information

Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.

 

Pharmacology of Amidate

Amidate is a non-barbiturate hypnotic that acts at the level of the reticular-activating system to produce anesthesia. Amidate is an imidazole compound that appears to depress CNS function via GABA. Duration of action is intermediate between thiopental and methohexital, and recovery from a single dose is rapid with little residual depression. Like the barbiturates and propofol, etomidate is does not induce analgesia. Amidate induces unconsciousness within one circulation time. Recovery is rapid as a result of extensive redistribution and rapid metabolism.

 

Amidate for patients

When appropriate, patients should be instructed as to the hazards of drowsiness that may follow use of barbiturates. Outpatients should be released in the company of another individual, and no skilled activities, such as operating machinery or driving a motor vehicle, should be engaged in for 8 to 12 hours.

 

Amidate Interactions

The following drug interactions have been reported with etomidate.

Drug Effect
   Probenecid    Prolonged action of etomidate 
   Diazoxide    Hypotension
   Zimelidine    etomidate antagonism 
   Opioid analgesics    Decreased antinociceptive action
   Aminophylline     Etomidate antagonism
   Midazolam    Synergism

 

Amidate Contraindications

Contraindicated in pregnancy (labor/delivery).

 

Additional information about Amidate

Amidate Indication: Used in the induction of general anesthesia.
Mechanism Of Action: Amidate binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Etomidate
Synonyms: Etomidic acid
Drug Category: Anesthetics, Intravenous; Hypnotics and Sedatives
Drug Type: Small Molecule; Approved
Other Brand Names containing Etomidate: Amidate; Hypnomidate;
Absorption: Not Available
Toxicity (Overdose): Undesirable side effects of etomidate that may limit its use include pain on injection, myoclonus and adrenocortical suppression lasting 4-6 hours following an induction dose.
Protein Binding: 76%, primarily to serum albumin.
Biotransformation: Hepatic. Metabolized rapidly by ester hydrolysis to inactive metabolites.
Half Life: 75 minutes.
Dosage Forms of Amidate: Solution Intravenous
Chemical IUPAC Name: ethyl 3-(1-phenylethyl)imidazole-4-carboxylate
Chemical Formula: C14H16N2O2
Etomidate on Wikipedia: http://en.wikipedia.org/wiki/Etomidate
Organisms Affected: Humans and other mammals