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PubMed1980

Methohexitone or etomidate for induction of dental anaesthesia.

Ninety-two patients who presented for outpatient dental extractions received methohexitone (1.5 mg . kg-1, 46 patients) or etomidate (0.3 mg . kg-1, 23 patients and 0.2 mg . kg-1, 23 patients). The induction characteristics of both drugs such as pain on injection, involuntary muscle movements and respiratory difficulties were comparable and the theoretical disadvantages of etomidate for dental anaesthetics did not prove troublesome in practice. Muscle movements did not interfere with the dentists' manipulations and pain on injection into veins of the antecubital fossa did not occur. The duration of operation for up to four extractions was three minutes and, following induction, anaesthesia was maintained with nitrous oxide, oxygen and halothane. Recovery was assessed by grading consciousness, airway control and motor activity. All the patients could maintain their airways one minute after the end of operation. The incidence of nausea and vomiting was significantly greater in the etomidate group.

Adolescent↗

PubMed1999

Propofol, but not etomidate, reduces desflurane-mediated sympathetic activation in humans.

PURPOSE: The administration of desflurane to humans can lead to substantial activation of the neurohumoral axis. Propofol can inhibit the sympathetic response to stress. This study compared the neurocirculatory effects of induction of anesthesia with propofol with those of etomidate on desflurane-mediated sympathetic activation. METHODS: After informed consent, awake baseline recordings of heart rate (HR), mean arterial blood pressure (MAP), and efferent sympathetic nerve activity (SNA, peroneal nerve) were obtained from healthy volunteers randomly assigned to receive either 2.5 mg x kg(-1) propofol (n=8) or 0.3 mg x kg(-1) etomidate (n=7). Two minutes after i.v. induction, desflurane 3.6% was added to the inspired gas, and increased in consecutive minutes to 7% and 10.9%. Ventilation via mask was continued for an additional seven minutes. Normocarbia was maintained while neurocirculatory parameters were continuously recorded. RESULTS: There were no differences between groups at baseline. The administration of desflurane via mask after etomidate led to increases in HR, MAP and SNA. Propofol significantly reduced the MAP response and delayed and attenuated the sympatho-excitation. CONCLUSION: Propofol induction reduced the sympathetic activation and hypertension associated with desflurane.

Adult↗

PubMed1984

Effects of etomidate on steroid biosynthesis in subcellular fractions of bovine adrenals.

The imidazole derivative, etomidate, inhibits the 11 beta-hydroxylase in cell-free systems and mitochondria isolated from bovine adrenal cortex. Fifty per cent inhibition is achieved at 3.10(-7) M. The less active hypnotic L-enantiomer is also a less potent inhibitor of the 11-hydroxylation. At a 2 times higher concentration, etomidate affects the cholesterol side chain cleavage. The inhibition of both steroidogenic enzyme systems may be due to binding of the unhindered nitrogen of the imidazole ring of etomidate to the heme iron atom of the adrenal cortex mitochondrial cytochrome P-450 species.

Adrenal Cortex↗

PubMed1983

Etomidate inhibits prolactin release but not through a dopaminergic mechanism.

A short-acting non-barbiturate intravenous general anaesthetic, etomidate, when administered i.v. lowered serum prolactin levels in the rat. The effect was evident at rest, after surgical stress or after injection of 5-hydroxytryptophan. Haloperidol-induced hyperprolactinaemia was not modified. Administered via the intracerebroventricular route, etomidate strongly reduced serum prolactin levels in unanesthetized rats. Studies performed on superfused synaptosomes from brain areas rich in dopaminergic nerve endings did not show any influence of the etomidate, 10(-7) M-10(-6) M, on [3H]dopamine release. A peculiar GABA-like mechanism and/or possible interplay with serotonergic control of the prolactin release may be postulated in order to explain the suppressive effects of the drug on secretion of lactotrophs.

5-Hydroxytryptophan↗

PubMed1985

Clinical assessment of etomidate for outpatient general anesthesia: a preliminary evaluation.

Etomidate, a nonnarcotic, nonbarbiturate hypnotic agent, was assessed in a group of 20 patients requiring general anesthesia for outpatient oral surgical procedures. Changes in mean blood pressure, heart rate, and transcutaneous oxygen tension (PtcO2) were examined following the intravenous administration of etomidate for the induction and maintenance of general anesthesia. Clinical evidence of pain on injection, myoclonic muscle activity, apnea, nausea, and emesis were documented. A postoperative questionnaire evaluated levels of amnesia and acceptance of the drug by the patient and surgeon. No significant (P less than 0.05) change in PtcO2 occurred during etomidate infusion; however, a statistically significant but clinically insignificant change did occur in mean blood pressure and heart rate. Although myoclonic muscle activity, pain on injection, and nausea and vomiting were documented, the subjective evaluation of this agent by patient and surgeon was favorable.

Adolescent↗

PubMed1986

The enhancement of diazepam and muscimol binding by pentobarbital and (+)-etomidate: size of the molecular arrangement estimated by electron irradiation inactivation of rat cortex.

Synaptosomal membranes were prepared from frozen rat cortices irradiated by 10 MeV electrons and the enhancement of [3H]diazepam and [3H]muscimol binding by pentobarbital (PB) and (+)-etomidate was studied. The target sizes of the corresponding parts of the receptor complex were estimated from the decrease in the enhancement as a function of irradiation dose. Different radiation inactivation constants suggest different regulatory units for the enhancement by PB and (+)-etomidate. Target sizes for PB and (+)-etomidate enhancement of [3H]diazepam binding were 127 +/- 14 and 360 + 124 kDa, respectively.

Animals↗

PubMed1995

Etomidate potentiation of GABAA receptor gated current depends on the subunit composition.

The role of the gamma 2 subunit in etomidate potentiation of GABAA receptor-gated chloride current was studied by whole cell patch clamp experiments on H293 cells expressing GABAA receptors. The GABAA receptor subunits alpha 1 beta 1 with or without the gamma 2 subunit expressed well, with an overall peak current of 157 +/- 42 pA/pF. At a clinically relevant concentration, etomidate potentiates the peak current induced by GABA equally well in receptors with or without the gamma 2 subunit. In contrast, the time course of current decay was prolonged only in receptors with the gamma 2 subunit. This gamma 2 subunit-dependent prolongation of the current time course was not blocked by the benzodiazepine receptor antagonist flumazenil. These results show that etomidate, an imidazole general anesthetic, interacts with the GABAA receptor in a gamma 2 subunit-dependent manner.

Action Potentials↗

PubMed1991

Effects of the hypnotic drug etomidate in a model nervous system (Buccal ganglia, Helix pomatia).

1. Effects of the hypnotic drug etomidate were studied with intracellular recordings of the identified neurons B1 to B4 of the buccal ganglia of Helix pomatia. 2. At threshold doses of 10 mumol/l, etomidate mainly affected interneuronal networks. 3. In concentrations above 200 mumol/l, the drug induced typical epileptic activities (paroxysmal depolarization shifts, PDS). Neurons B1 to B4 generated epileptic activities in differential concentration ranges. PDS were synchronized via electrical contacts. PDS could be blocked by the "calcium antagonist" verapamil but not by a block of chemical synaptic transmission. 4. In comparison with the epileptogenic drug pentylenetrazol, effective doses of etomidate to induce PDS were about 100 times lower.

Action Potentials↗

PubMed2003

Myoclonus associated with etomidate for ED procedural sedation and analgesia.

We report 3 cases of myoclonus associated with etomidate during ED procedural sedation and analgesia (PSA). EPs should be familiar with myoclonus associated with etomidate. Clinicians using this drug for PSA should be prepared to offer the brief period of support, and occasionally, respiratory assistance, required when etomidate-associated myoclonus is encountered.

Aged↗

PubMed2003

Effects of etomidate, ketamine or propofol, and their combinations with conventional antiepileptic drugs on amygdala-kindled convulsions in rats.

Ketamine, etomidate and propofol modified behavioral and electrographic correlates of kindled seizures in rats. In detail, ketamine (5 mg/kg) and propofol (15 mg/kg) significantly increased afterdischarge threshold, reduced seizure severity and shortened seizure and afterdischarge durations. Etomidate (7.5 mg/kg) was effective in terms of seizure and afterdischarge durations. Moreover, the combinations of ketamine (2.5 mg/kg) with carbamazepine (15 mg/kg) or valproate (50 mg/kg; all drugs at their subeffective doses), reduced the severity and duration of kindled seizures. The antiseizure potency of the ketamine/carbamazepine combination was comparable to that of carbamazepine alone administered at 20 mg/kg, while the effect of ketamine/valproate was comparable to the efficacy of valproate alone at 100 mg/kg. However, the combinations of ketamine with phenobarbital or diphenylhydantoin did not exert any protective action. Propofol and etomidate entirely failed to interact with conventional antiepileptics. The combinations of ketamine with carbamazepine or valproate did not induce any significant motor impairment in the chimney test or memory deficit in the passive avoidance task. A pharmacokinetic interaction, at least in plasma, can be excluded, because ketamine (2.5 mg/kg) did not affect the free plasma concentrations of carbamazepine or valproate. Results of the present study may suggest that there may be no risk of negative interactions between injectable anesthetics and antiepileptics in cases of partial epilepsy.

Amygdala↗

PubMed1998

Blocking effects of the anaesthetic etomidate on human brain sodium channels.

Sodium channels from human brain tissue were incorporated into voltage-clamped planar lipid bilayers in presence of batrachotoxin and exposed to increasing concentrations of the intravenous anaesthetic drug etomidate (0.03-1.02 mM). Etomidate interacted with the sodium-conducting pathway of the channel causing a concentration-dependent block of the time-averaged sodium conductance (computer fit of the concentration-response curve: half-maximal blocking concentration, EC50, 0.19 mM; maximal block, block(max), 38%). This block of sodium-conductance resulted from two distinct effects (I) major effect: reduction of the sodium-channel amplitude and (II) minor effect: reduction of the fractional channel open-time. These results were observed at concentrations above clinically-relevant serum concentrations (up to 0.01 mM), suggesting only a limited role for human brain sodium channels in the mechanism of action of etomidate during clinical anaesthesia.

Batrachotoxins↗

PubMed2000

Etomidate-facilitated hip reduction in the emergency department.

Joint dislocations are common presenting complaints in emergency departments (EDs). Dislocations of major joints, such as the shoulder, elbow, and hip, are often difficult to gently reduce because of the challenge in obtaining sufficient relaxation of large muscle groups. This is the first reported use of etomidate to assist in the reduction of a major joint in an outpatient setting. We discuss the case of an elderly woman with total hip arthroplasty who experienced four spontaneous posterior hip dislocations in a 5-month period. Narcotics and benzodiazepines failed to facilitate reduction at every encounter, whereas etomidate made the procedure easy the two times it was used in the ED. This article reviews the administration of etomidate for conscious sedation and discusses potential complications.

Aged↗

PubMed1990

[Pharmacokinetics of etomidate].

Etomidate is the ester of a carboxylated imidazole. This lipophilic (octanol/water partition coefficient: 1000) and weak base (pKa = 4.5) is a potent short-acting hypnotic agent, which can be used for anaesthetic induction or maintenance. The plasma concentration curve fits an open three compartment pharmacokinetic model, with distribution half-lives of 2.6 and 20 min, and terminal elimination half-life of about 4-5 h. Hypnotic plasma concentrations (greater than 0.2 microgram.ml-1) are observed during the intermediate distribution phase (t1/2 approximately 20 min); they reflect the short lasting pharmacodynamic effect. The slow elimination phase is of importance for intravenous infusions lasting more than 2 h; it is recommended to decrease by half the maintenance dose (0.005 mg.kg-1.min-1) so as to prevent a cumulative effect. Etomidate is hydrolysed by hepatic esterases to the corresponding carboxylic acid, which is inactive. The pharmacokinetics of etomidate are altered in the elderly, with a decrease initial distribution volume and clearance (a decreased of 2 ml.min-1.kg-1 every decade) as well as in cirrhotic patients (a 100% increase in terminal half-life).

Adult↗

PubMed1992

[Propofol versus etomidate in short-time urologic surgery].

Thirty patients, scheduled for short urological surgical procedures and ranked ASA 1 or 2, were randomly assigned to two homogenous groups. In group P, they were given a 2 mg.kg-1 bolus of propofol and 10 micrograms.kg-1 of alfentanil, followed by a continuous infusion of propofol (5 mg.kg-1.h-1) and 5 micrograms.kg-1 doses of alfentanil. In group E, they were given a 0.3 mg.kg-1 bolus of etomidate, followed by an infusion (1.5 mg.kg-1.h-1). The doses of alfentanil were the same as in group P. Further doses of either propofol (0.5 mg.kg-1) or etomidate (0.2 mg.kg-1) were used should anaesthesia prove not to be deep enough. The patients were not intubated, and breathed spontaneously. Surgery lasted a mean of 18.3 +/- 11.8 min (group P) and 18.8 +/- 9.4 min (group E). The following parameters were studied: the amount of each agent required for maintenance of anaesthesia, the duration of apnoea at induction, the quality of anaesthesia and of muscle relaxation, adverse effects (coughing, trismus, restlessness, nausea, vomiting), the time required for recovery, and its quality. In group P, there was a 27% decrease in arterial pressure, without any tachycardia or hypoxia, together with a quick recovery of excellent quality. On the other hand, in group E, there was little or no haemodynamic alteration, but there often was a trismus at induction. Hypoxia also occurred during induction with etomidate, being severe enough in one case to require tracheal intubation and artificial ventilation. The reasons for this hypoxia seemed to be the apnoea and the trismus, which tends to hinder assisted ventilation.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

PubMed1988

[Comparison of etomidate and thiopental for the anesthesia in cardioversion].

A controlled study was carried out, comparing etomidate and thiopentone used for anaesthesia for cardioversion. Eighty patients presenting with supraventricular tachyarrhythmias were randomly allocated to two groups with stratification for duration of supraventricular tachyarrhythmias and cardiothoracic ratio. After premedication with 10 mg of diazepam, anaesthesia was induced and maintained if necessary with etomidate (0.3 and 0.15 mg.kg-1 respectively) or thiopentone (3 and 1.5 mg.kg-1 respectively). The following observations were made by an independent observer: energy of the electric discharge, systolic and diastolic arterial pressures, heart rate, apnoea with duration, quality of anaesthesia, side-effects if present, and induction, anaesthesia and recovery times. A drawing test and an ambulation test were carried out after recovery. Data were analysed using one-way analysis of variance (continuous variables) and chi-squared test with Yates correction for small numbers (categorical variables) with p less than 0.05 considered significant. The thiopentone (THIO) and etomidate (ETO) groups were similar, except for premedication and number of NYHA class III and IV patients, being more common in ETO (p = 0.04; p = 0.05). Anaesthesia time was 4.6 +/- 2.3 min in THIO and 9.9 +/- 3.5 min in ETO (p less than 10(-9)) with more reinjections in THIO (p = 0.003). Awakening time was shorter in THIO (p less than 10(-6)) and graphic test was carried out better at 15 min in THIO. No difference was found later for graphic test and ambulation. Apnoea was more frequent in THIO (p = 0.002).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

PubMed2001

Anaphylactoid reaction to etomidate: report of a case.

We report an anaphylactoid reaction to etomidate twice in a 60-year-old male with coronary artery disease and peripheral vascular disease. Following the first anaphylactoid reaction, the patient developed myocardial infarction. In addition, the patient's blood was moderately positive for latex antibodies, which made the differential diagnosis difficult. We concluded that the patient had anaphylactoid reaction to etomidate due to the temporal relationship to induction with the drug. The patient did not manifest similar reaction to other induction drugs used for other surgeries. The patient recovered from both incidents of anaphylactoid reaction to etomidate following intravenous administration of epinephrine and fluids.

Anaphylaxis↗

PubMed2003

Ambulatory electrical external cardioversion with propofol or etomidate.

STUDY OBJECTIVE: To compare, in pairwise fashion, the effects of propofol and etomidate during ambulatory cardioversion and early recovery. DESIGN: Clinical, prospective, randomized, blinded, monocenter, pairwise, comparative study SETTING: OR and recovery area of the electrophysiological department, University Hospital Ghent, Belgium. PATIENTS: 34 patients with atrial arrhythmia who were scheduled for repetitive electrical cardioversion, of whom 25 patients completed the study. INTERVENTIONS: Nonpremedicated patients received during the first cardioversion either propofol (1 mg/kg) or etomidate (0.2 mg/kg) until loss of consciousness, followed by electrical external cardioversion. If after restoration of sinus rhythm for at least 1 day, atrial arrhythmia reoccurred, a second session was performed a week later, using the other induction drug. MEASUREMENTS: Systolic and diastolic blood pressure values taken before drug administration, at loss of consciousness, 60 seconds after cardioversion, and awake; the number of shocks, the total amount of energy, the number of patients in which we failed to restore sinus rhythm, the time before opening eyes, answering simple questions and be able to sit, were all noted. Aldrete scores and the Steward postanesthetic recovery scores were noted every minute until 10 minutes after the external cardioversion. Recovery tests were performed and evaluated 5, 10, 15, and 20 minutes after energy delivery. MAIN RESULTS: Number of shocks, amount of energy, and blood pressure values were comparable in both groups. Recovery times and Aldrete and Steward postanesthetic recovery scores showed a faster awakening in patients who were induced with propofol. Overall performance of the psychomotor test was better in the propofol group, and most pronounced at 10 and 15 minutes. CONCLUSIONS: Etomidate and propofol are both useful during ambulatory external electrical cardioversion. The described doses maintain stable hemodynamic conditions in nonpremedicated patients. Recovery scores and psychomotor test indicate a faster recovery in the propofol group. However, no intergroup differences were noted at 20 minutes after the cardioversion. A safe discharge of all patients from the critical care unit or postanesthesia care unit to the ward can be considered after 30 minutes.

Ambulatory Care↗

PubMed1997

Bolus administration of eltanolone, thiopental, or etomidate does not affect systemic vascular resistance during cardiopulmonary bypass.

OBJECTIVE: To discover possible effects on systemic vascular resistance of the anesthetic induction agent eltanolone in comparison with thiopental and etomidate. The measurements were performed during cardiopulmonary bypass to maintain a constant cardiac output (approximately pump flow). DESIGN: The patients were prospectively randomized in three groups to receive either eltanolone, thiopental, or etomidate. SETTING: University hospital as a single center. PARTICIPANTS: Seventy-five patients scheduled for elective coronary artery bypass grafting. INTERVENTIONS: The anesthetic induction agents were repeated at the same dosage when cardiopulmonary bypass was instituted. The respective mean dosages were eltanolone, 0.41 +/- 0.1 mg/kg; thiopental, 2.88 +/- 0.62 mg/kg; etomidate, 0.26 +/- 0.06 mg/kg. MEASUREMENTS AND MAIN RESULTS: Systemic vascular resistance was calculated from the mean of a triple measurement (normal pump flow and +/- 20%). Points of measurement were before, and 2 and 5 minutes after injection of the hypnotic agent. None of the injected drugs made a significant change in the systemic vascular resistance. A small (not significant) decrease from 1,295 +/- 296 dyne/s/cm-5 to 1,196 +/- 323 dyne/s/cm-5 (mean +/- SD) was seen in the eltanolone group, whereas the other patients did not show any change during the study period. CONCLUSIONS: The reason for the significant reduction of the arterial pressure attributed to anesthetic induction by eltanolone may be more a cardiodepressive effect than a direct vasodilation.

Anesthetics, Intravenous↗