Etomidate

Publication Title: 
European Journal of Pharmacology

Beagles, implanted with cortical and subcortical electrodes, were given etomidate i.v. (1 mg/kg) over a period of 10 sec. The effects on the EEG were compared with those obtained with 7 mg/kg of methohexital. Both compounds induced hypnosis for a duration of approximately 8 min. The EEGs showed a remarkable similarity. Visual inspection of the records as well as power spectrum analysis revealed a sustained theta-activity with underlying fast activity. The configuration of the waves was rather sharp.

Author(s): 
Wauquier, A.
van den Broeck, W. A.
Verheyen, J. L.
Janssen, P. A.
Publication Title: 
South African Medical Journal = Suid-Afrikaanse Tydskrif Vir Geneeskunde

Etomidate (Hypnomidate; Ethnor) in an alcoholic solution was used as the hypnotic component of a technique of total intravenous anaesthesia in an open pilot evaluation in 50 patients undergoing surgery. No anaesthetic gases were used. Despite cardiovascular stability, lack of respiratory depression and a short awakening time, unwanted movements by the patients made total intravenous anaesthesia with this technique unsatisfactory.

Author(s): 
Van Eeden, A. F.
Leiman, B. C.
Publication Title: 
British Journal of Anaesthesia

Etomidate was injected i.v. within 10 or 60 s at various doses. After etomidate 0.3 mg kg-1 the plasma concentration was 1.6 micrograms ml-1 at 1 min after the end of injection. For about 7 min a good hypnotic effect (stages C0-D2) was observed on the e.e.g. recording. For surgical procedures, however, a combination with analgesic drugs appeared to be necessary. When the dose of etomidate was increased (0.1-0.4 mg kg-1) a linear increase in plasma concentration and slow e.e.g. activity was observed concomitantly.

Author(s): 
Doenicke, A.
Löffler, B.
Kugler, J.
Suttmann, H.
Grote, B.
Publication Title: 
Anaesthesia

A review of the hypnotic, anticonvulsant and brain protective action of etomidate in animals shows that when given as a single injection in different animal species recovery from hypnosis is quick and that the safety margin is large. In dogs a bolus or infusion produces high amplitude theta activity on the electroencephalogram (EEG). During infusion burst suppression is seen. After high doses, behaviour and EEG changes returned to normal within 3 hours. The wide spectrum of anticonvulsant activity suggests that etomidate may be useful in the treatment of status epilepticus.

Author(s): 
Wauquier, A.
Publication Title: 
Anesthesia and Analgesia

An etomidate infusion regimen for hypnosis as part of balanced, totally intravenous anesthesia was designed to maintain plasma etomidate concentrations above the awakening concentration of 300 ng/ml while avoiding dose-related side effects. The etomidate infusion regimen of 0.1 mg/kg/min for 3 min, 0.02 mg/kg/min for 27 min, and 0.01 mg/kg/min for the remainder of the anesthesia was used together with intravenous bolus doses of fentanyl, droperidol, and pancuronium. This was evaluated in 11 patients and the kinetics of etomidate were reexamined.

Author(s): 
Fragen, R. J.
Avram, M. J.
Henthorn, T. K.
Caldwell, N. J.
Publication Title: 
South African Medical Journal = Suid-Afrikaanse Tydskrif Vir Geneeskunde

Etomidate (Hypnomidate; Janssen) 1,25% in sterile water was given rectally on 100 occasions to 50 male Long-Evans rats in doses ranging from 4 mg/kg to 12 mg/kg. The onset and duration of ataxia and hypnosis (i.e. loss of righting ability) were recorded. Ataxia was observed in all rats, even at the lowest dose levels. The lowest hypnotic dose was 6 mg/kg, when 2 out of 5 rats lost their righting ability. In all 50 rats given 8 mg/kg or more hypnosis occurred within 4 minutes (range 2-4 minutes, average 3,3 minutes), from which they recovered within an average of 10,4 minutes.

Author(s): 
Linton, D. M.
Price, S. K.
Publication Title: 
South African Medical Journal = Suid-Afrikaanse Tydskrif Vir Geneeskunde

Following the preliminary study in rats, etomidate (Hypnomidate; Janssen) 1,25% in sterile water (pH 3,5) was administered rectally to 40 children aged between 6 months and 5 years to induce general anaesthesia for scheduled minor surgical procedures. The doses given ranged from 3,0 mg/kg to 6,5 mg/kg. The time taken for hypnosis to occur and the incidence of muscle movements were recorded. Cardiovascular and respiratory parameters were monitored. Anaesthesia was maintained with nitrous oxide/oxygen and halothane as needed.

Author(s): 
Linton, D. M.
Thornington, R. E.
Publication Title: 
Pharmacotherapy

Currently available anesthetic induction agents provide adequate hypnosis but are not ideal, particularly in the high risk patient (ASA class III-V), because most cause myocardial and/or respiratory depression and some have other important side effects. Etomidate was recently marketed as an intravenous anesthetic induction agent. It is a non-barbiturate hypnotic without analgesic properties that has less cardiovascular and respiratory depressant actions than sodium thiopental, even in patients with minimal cardiovascular reserve.

Author(s): 
Giese, J. L.
Stanley, T. H.
Publication Title: 
Journal of Pharmaceutical Sciences

A sensitive and specific high-performance liquid chromatographic assay was developed for the measurement of etomidate in human plasma following extraction of the drug and the internal standard. Using 0.5-ml aliquots of plasma, the assay was linear in the concentration range of 20-2000 ng of etomidate/ml of plasma. This method was used to evaluate a preliminary clinical study of an etomidate infusion regimen for hypnosis in a total intravenous anesthesia protocol in 23 patients.

Author(s): 
Avram, M. J.
Fragen, R. J.
Linde, H. W.
Publication Title: 
Journal of Veterinary Pharmacology and Therapeutics

The pharmacokinetics and clinical effects of the short-acting hypnotic R 8110 and of the narcotic analgesic fentanyl were studied in the dog. The effects of separate intravenous (i.v.) injections of R 8110 (4 mg/kg) and fentanyl (0.015 mg/kg) and of concurrent i.v. injection of the two were studied. After administration of R 8110, induction of hypnosis occurred within 1 min, maximal depth of anaesthesia and satisfactory analgesia and muscle relaxation were obtained after 5 min. The effects had decreased within 15 min and full recovery occurred within 30 min.

Author(s): 
Monbaliu, J.
Degryse, A. D.
Ooms, L. A.
Van Dijk, P.
Lagerweij, E.
Michiels, M.
Woestenborghs, R.
Heykants, J.

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