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At least 379 records · Page 21Linked to original sources
PubMed2006

Comparison of antimicrobial effects of dexmedetomidine and etomidate-lipuro with those of propofol and midazolam.

BACKGROUND AND OBJECTIVES: The aim of our study was to investigate the antimicrobial effects of dexmedetomidine and etomidate-lipuro, and to compare these effects with those of midazolam and propofol on Staphylococcus aureus, Escherichia coli, Pseudomonas aeroginosa, Acinetobacter baumannii and extended-spectrum beta-lactamase Escherichia coli ( E. coli ESBL). METHODS: All hypnotic dilutions were exposed to micro-organisms for 0, 30, 60, 120 and 240 min at room temperature in vitro. The inoculums taken from diluted suspensions were re-inoculated on blood agar and incubated for 18-24 h at 35 degrees C after which a count of the colonies was compared. RESULTS: Midazolam reduced the viable cells of S. aureus at 30, 60, 120 and 240 min, and also completely inhibited the growth of E. coli, P. aeroginosa, A. baumannii and E. coli ESBL. Dexmedetomidine, etomidate-lipuro and propofol, however, did not inhibit any of the micro-organisms tested. CONCLUSION: In vitro, midazolam had an antimicrobial effect on E. coli, P. aeroginosa, A. baumannii and E. coli ESBL. Like propofol and dexmedetomidine, etomidate-lipuro had no antimicrobial effect on any of the micro-organisms tested.

Acinetobacter baumannii↗
PubMed2003

2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.

To locate general anesthetic binding sites on ligand-gated ion channels, a diazirine derivative of the potent intravenous anesthetic, R-(+)-etomidate (2-ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate), has been synthesized and characterized. R-(+)-Azietomidate [2-(3-methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate] anesthetizes tadpoles with an EC(50) of 2.2 microM, identical to that of R-(+)-etomidate. At this concentration both agents equally enhanced GABA-induced currents and decreased binding of the caged-convulsant [(35)S]TBPS to GABA(A) receptors. In all of the above actions R-(+)-azietomidate is about an order of magnitude more potent than S-(-)-azietomidate, an enantioselectivity comparable to etomidate's. R-(+)-Azietomidate also inhibits acetylcholine-induced currents in nicotinic acetylcholine receptors, with about twice the potency of the parent compound. [(3)H]Azietomidate photoincorporated into Torpedo nicotinic acetylcholine receptor-rich membranes. Desensitization decreased photoincorporation into the delta-subunit and increased that into the alpha-subunit. The latter increase was confined to a proteolytic fragment containing the first three transmembrane segments. Thus, R-(+)-azietomidate is a potent stereoselective general anesthetic and an effective photolabel.

Allosteric Regulation↗
PubMed2001

Perioperative response of leptin and the tumor necrosis factor alpha system in morbidly obese patients. Influence of cortisol inhibition by etomidate.

BACKGROUND: Leptin, tumor necrosis factor alpha (TNFalpha) and soluble TNFalpha receptors are secreted by the adipose tissue. Surgery induces a complex cytokine and neurohormonal response. The aim of our study was to investigate the perioperative response of leptin and the TNFalpha system in morbidly obese patients submitted to gastroplasty, and the possible involvement of cortisol in their responses. METHODS: Serum cortisol, adrenocorticotropic hormone (ACTH), leptin, TNFalpha and soluble TNFalpha receptor I were measured in 22 morbidly obese women (11 anesthetized with thiopental and 11 with etomidate, a well known inhibitor of cortisol synthesis). Samples were collected before anesthesia induction, just before surgical incision, and 2, 4, 6, 12, 24 and 48 h after the start of surgery. RESULTS: Baseline serum leptin correlated with body mass index (r=0.567, P=0.007). Baseline serum leptin and TNFalpha were higher than normal. Cortisol release was inhibited in the etomidate group with a subsequent higher stimulation of ACTH release. A statistically significant decrease in serum leptin levels was observed in both groups at 2, 4, 6 and 48 h, compared with basal values. A similar decrease in serum TNFalpha levels was observed in both groups, but the decrease reached significance only in the etomidate group. Serum soluble TNFalpha receptor I did not decrease. No differences were found between the two groups in leptin, TNFalpha or soluble TNFalpha receptor I concentrations at any time. CONCLUSION: Serum leptin and TNFalpha levels decrease in obese patients during gastroplasty. Transitory inhibition of cortisol release does not alter this response.

Adrenocorticotropic Hormone↗
PubMed1999

Adrenocortical function in critically ill patients 24 h after a single dose of etomidate.

We compared the effects of single doses of etomidate and thiopentone on adrenocortical function in a randomised controlled clinical trial involving 35 critically ill patients who needed a general anaesthetic. Just before induction of anaesthesia, a baseline blood cortisol sample was taken. Twenty-four hours later we performed a short adrenocorticotrophic hormone stimulation test. No patient had a low cortisol level (< 160 nmol.l-1) at any time during the study. Baseline, pre-ACTH and post-ACTH cortisol levels were similar in the two groups. However, significantly more patients in the etomidate group had an ACTH-stimulated cortisol increment < 200 nmol.l-1. The clinical significance of these findings is not clear, but we conclude that single doses of etomidate may interfere with cortisol synthesis for at least 24 h in the critically ill.

Adolescent↗
PubMed1997

Distinct loci mediate the direct and indirect actions of the anesthetic etomidate at GABA(A) receptors.

Most general anesthetics produce two distinct actions at GABA(A) receptors. Thus, these drugs augment GABA-gated chloride currents (referred to as an indirect action) and, at higher concentrations, elicit chloride currents in the absence of GABA (referred to as a direct action). Because a beta subunit appears to be required for the direct action of intravenous anesthetics in recombinant GABA(A) receptors, site-directed mutagenesis of the beta3 subunit was performed to identify amino acid residues that are critical for this action. In HEK293 cells expressing a prototypical GABA(A) receptor composed of alpha1beta3gamma2 subunits, mutation of amino acid 290 from Asn to Ser dramatically reduced both etomidate-induced chloride currents and its ability to stimulate [3H]flunitrazepam binding. By contrast, the ability of etomidate to augment GABA-gated chloride currents and GABA-enhanced [3H]flunitrazepam binding was retained. The demonstration that the direct, but not the indirect, actions of etomidate are dependent on beta3(Asn290) indicates that the dual actions of this intravenous anesthetic at GABA(A) receptors are mediated via distinct loci.

Anesthetics, Intravenous↗
PubMed1986

The effects of etomidate in the cat middle cerebral artery occlusion model of brain ischaemia. An experimental study.

The effects of etomidate on focal cerebral ischaemia following transorbital occlusion of the cat middle cerebral artery were investigated. Etomidate had no effect on CBF before or after onset of ischaemia by comparison with controls, but caused a greater fall in CBF in cats with high preocclusion or initial ischaemic CBF than in those in which CBF was lower. There were more sustained rises in Kp on SG. The established flow threshold for water accumulation was lost; more gyri with CBF above and fewer gyri with CBF below the flow threshold accumulated water. The relationship between mean occlusion CBF and in vitro GABA uptake was lost; uptakes from MG were lower and from SG and EG higher than expected. In the ischaemic penumbra there was a trend towards reduction in CBF, disruption of ion homeostasis and cerebral oedema formation, whilst in areas of lower flow there was some recovery of GABA uptake and less cerebral oedema following administration of etomidate.

Animals↗
PubMed1999

Etomidate dose-response on somatosensory and transcranial magnetic induced spinal motor evoked potentials in primates.

There is growing interest and need to monitor reliably both motor (MEP) and somatosensory (SEP) evoked potentials under anesthesia. On a pre-established primate model, the present study examined the effect of incremental etomidate (ET) dosages on spinal neural MEPs to transcranial magnetic stimulation (TMS) and posterior tibial rate (PTN) SEPs. Through a small thoracic T11-T12 laminotomy, an insulated double bipolar electrode was inserted epidurally in seven cynomolgus monkeys. Spinal TMS-MEPs, PTN-SEPs, and frontal EEG were tested against graded increase of ET doses. Etomidate 0.5 mg kg-1 i.v. was initially given and followed by 30 min continuous infusion of 0.01 mg kg-1 min-1, 0.018, 0.032, 0.056, 0.1, and 0.18 mg kg-1 min-1 in that order. Measurable spinal MEPs and SEPs were recorded under deep ET anesthesia (total 12.38 mg kg-1 cumulative dose over 180 min). The EEG showed marked slow wave and graded burst suppression at cumulative dose of > or = 3.14 mg kg-1. The direct (D) and subsequent initial indirect (I) waves (I1, I2, I3) were reproducible at doses < 0.18 mg kg-1 min-1 infusion. The latter I-waves (I4 and I5) showed graded loss at infusion dosage 0.056 mg kg-1 min-1. Etomidate remains an anesthetic of attractive features in neuroanesthesia. In the primate model, neural MEPs-SEPs were reproducible despite the exceedingly high dose of ET and markedly depressed EEG. Moreover, MEP-SEP can be monitored during ET burst-suppressive neuroprotective state. The study may set a model in humans for intra-operative multi-modality neurophysiologic recording under ET-based anesthesia.

Animals↗
PubMedDate not supplied

A comparison of rapid-sequence intubation and etomidate-only intubation in the prehospital air medical setting.

OBJECTIVES: To compare laryngoscopy conditions produced by etomidate-only intubation (EOI) with those produced by rapid-sequence intubation (RSI) in the prehospital air medical setting. METHODS: A prospective crossover trial design used two helicopters staffed by the same flight paramedics and nurses. Each aircraft used an EOI protocol (0.3 mg/kg) for six months. An RSI protocol using the same dose of etomidate plus succinylcholine (1.5 mg/kg) was used for the alternate six months. Laryngoscopy conditions were graded by three scales: 1) a formal Laryngoscopy Grading Scale (LGS), 2) the Percentage of Glottic Opening (POGO) score, and 3) subjective overall intubation difficulty using a Likert scale of 1 (very easy) to 5 (very difficult). Orotracheal intubation success was also recorded. RESULTS: Forty-nine patients were intubated using the EOI (n = 24) and RSI (n = 25) protocols. Mean age was 38 years, 76% were male, and 90% were intubated for trauma. Fifteen (63%) of the 24 EOI patients required additional etomidate (n = 3) or RSI (n = 12) to allow intubation, while one (4%) of the 25 RSI patients required additional medication dosing (p < 0.0001). Laryngoscopy conditions were assessed for all patients. Good or acceptable conditions as assessed by the LGS were seen in 79% of RSI patients and 13% of EOI patients (p < 0.0001). Mean rates of POGO visualization were 60% with RSI and 12% with EOI (p < 0.0001). Mean global intubation difficulty scores were 3.0 (moderate) with RSI and 4.7 (difficult to very difficult) with EOI (p < 0.0001). Ninety-two percent of the patients undergoing RSI and 25% of the EOI patients were successfully orotracheally intubated (p < 0.0001). CONCLUSIONS: Patients receiving RSI had better laryngoscopy conditions and were easier to intubate than patients receiving EOI. Intubation success rate was higher with RSI.

Adolescent↗
PubMed1979

Etomidate for induction of anaesthesia at caesarean section: comparison with thiopentone.

Thirty mothers undergoing elective Caesarean section received thiopentone 3.5 mg kg-1 and 30 received etomidate 0.3 mg kg-1 for induction of anaesthesia. Subsequent management of anaesthesia was identical in both groups. Maternal to fetal base excess differences and the degree of biochemical correlation between mother and infant were more favourable following etomidate than following thiopentone. The clinical status of the newborn was considered superior with etomidate.

Adult↗
PubMed1979

Effect of etomidate on intracranial pressure and cerebral perfusion pressure.

Ten patients with intracranial lesions, anaesthetized with thiopentone and nitrous oxide (70%) in oxygen (30%) received etomidate 0.2 mg kg-1 i.v. Ventilation was controlled in each patient. Intracranial pressure (i.c.p.) and mean arterial pressure (m.a.p.) were recorded. I.c.p. decreased significantly in all patients (0.01 greater than P greater than 0.001). Although PaCO2 decreased during the period of measurement, the extent and time-course of this change suggested that it was not mainly responsible for changes in i.c.p. M.a.p. decreased in most patients, but the decrease was statistically significant only at 3 and 4 min after the administration of etomidate (0.05 greater than P greater than 0.02). The changes in cerebral perfusion pressure (c.p.p.) and heart rate were not clinically or statistically significant. We conclude that etomidate can be used for the induction of anaesthesia in patients with intracranial space-occupying lesions without increasing i.c.p. or seriously reducing c.p.p.

Adult↗
PubMed1979

Cardiorespiratory changes following induction of anaesthesia with etomidate in patients with cardiac disease.

The cardiorespiratory effects of etomidate were measured in two groups of six patients with aortic or mitral valve disease. The induction of anaesthesia with etomidate 0.3 mg kg-1 was followed by a second dose 10 min later. After the first dose, a 19% decrease in systemic arterial pressure was associated with a decrease in systemic vascular resistance and left ventricular heart work. Cardiac index, pulmonary artery pressure and wedge pressure all decreased slightly. Central venous pressure and heart rate did not change. A slight increase in respiratory frequency failed to prevent an increase in PACO2. Changes after the second dose were similar. The two groups of patients did not differ significantly in their response to etomidate. No patient complained of pain during injection, nor did myoclonic movements occur.

Aged↗
PubMed1982

Efferent vagal discharge and heart rate in response to methohexitone, althesin, ketamine and etomidate in cats.

The effects of methohexitone, Althesin, ketamine and etomidate on single fibre discharge of cardiac vagal efferents and on heart rate were studied in cats. Cardiac vagal efferents were inhibited markedly and regularly for equihypnotic doses of methohexitone (2.0 mg kg-1), Althesin (0.1 ml kg-1) and ketamine (5.0 mg kg-1), but not of etomidate (0.8 mg kg-1). These inhibitory effects were independent of arterial pressure and mirrored the increases of heart rate elicited by the first three agents. Etomidate did not consistently affect cardiac vagal discharge or heart rate. Thus methohexitone. Althesin and ketamine inhibit efferent cardiac vagal drive by their central action independently of baroreflex function. This central vagolysis is probably the cause of their positive chronotropic effects.

Action Potentials↗
PubMed1982

Recovery from day-case anaesthesia. Comparison between methohexitone, Althesin and etomidate.

One hundred unpremedicated patients, undergoing short gynaecological procedures, were randomly allocated to receive one of three i.v. hypnotic agents (methohexitone, Althesin and etomidate) alone or in combination with fentanyl, to supplement 66% nitrous oxide in oxygen. Recovery was assessed by the time patients took to open the eyes, to give correct date of birth, to achieve a certain level of manipulative skill with a children's post-box toy, and to perform a paper and pencil test. Satisfactory operating conditions were not obtained using etomidate alone. Administration of methohexitone alone resulted in a more rapid initial awakening than Althesin alone (P less than 0.05) and the administration of fentanyl with methohexitone reduced the total dose given of the latter (P less than 0.01). Administration of fentanyl with Althesin or methohexitone did not significantly prolong the "post-box" recovery time. Side-effects were less common with Althesin, with or without fentanyl and etomidate with fentanyl was associated with the greatest frequency of complications.

Adolescent↗
PubMed1984

Venous sequelae following the injection of etomidate or thiopentone i.v.

The frequency of local venous reactions after the injection i.v. of etomidate or thiopentone was studied in 61 patients undergoing surgery for prolapsed lumbar disc. Of the patients who received etomidate, 24% developed thrombophlebitis in the period after operation (up to 14 days). Of the patients who received thiopentone, 4% developed thrombophlebitis in the period after operation. Pain on injection occurred in 24% of the patients receiving etomidate, but there was no correlation between pain on injection and the subsequent thrombophlebitis.

Adult↗
PubMed1985

Effect of induction of anaesthesia with etomidate on corticosteroid synthesis in man.

The effects of a single bolus dose of etomidate 0.3 mg kg-1 or thiopentone 5 mg kg-1, on the synthesis of corticosteroid hormones and adrenocorticotrophic hormone (ACTH), were compared for 24 h in 12 patients, undergoing minor surgery under general anaesthesia. Following opioid premedication i.m. and general anaesthesia, plasma cortisol concentrations decreased transiently within the first hour of anaesthesia in all 12 patients. The six patients who received etomidate had statistically higher plasma 11-deoxycorticosterone concentrations at 4 and 24 h than those who had received thiopentone (P less than 0.01). Throughout the study, no difference in plasma cortisol, corticosterone or ACTH concentrations were found between the two groups. We have demonstrated a biochemical effect of a single bolus dose of etomidate consistent with incomplete inhibition of adrenocortical mitochondrial 11 beta-hydroxylase activity, but no clinically significant adrenocortical suppression.

Adrenal Cortex Hormones↗
PubMed1985

Comparison of etomidate and althesin in the reduction of increased intracranial pressure after head injury.

The increasing use of shorter-acting hypnotic agents to control intracranial pressure (ICP) following severe head injury has prompted a prospective double-blind controlled trial comparing the efficacy of etomidate and Althesin, given by i.v. infusion. Over the dose ranges used, the two drugs appeared equipotent in decreasing ICP whilst preserving cerebral perfusion pressure. However, in two patients (one in each group) ICP did not respond to hypnotic infusion, a feature noted in other studies to occur in a minority of patients. With the cessation of Althesin manufacture and the discussion about the use of etomidate infusions, it is timely to document the effectiveness of etomidate in decreasing ICP.

Adolescent↗
PubMed1985

Porphyrinogenicity of etomidate and ketamine as continuous infusions. Screening in the DDC-primed rat model.

The porphyrinogenicity of etomidate and ketamine administered as continuous i.v. infusions was screened in the DDC-primed rat model of latent variegate porphyria. Ketamine produced no change from control in 5-aminolaevulinate synthase (ALAs) activity and haem intermediate production in either untreated or DDC-primed rats, and would appear to be safe for use in the patient with genetic porphyria. Etomidate, while producing no significant changes in these parameters in untreated rats, caused a statistically significant 47% increase in hepatic ALAs activity with a corroborative 85% increase in coproporphyrin and a 40% increase in protoporphyrin content, in DDC-primed rats. On these grounds, etomidate must be regarded as potentially porphyrinogenic when administered as a continuous infusion for total i.v. anaesthesia.

5-Aminolevulinate Synthetase↗
PubMed1985

Effect of propofol, thiopentone and etomidate on adrenal steroidogenesis in vitro.

The i.v. anaesthetic agents propofol, thiopentone and etomidate inhibited ACTH-stimulated production of cortisol by guineapig dispersed adrenal cells in a dose-related manner. For two of the drugs, propofol and thiopentone, inhibition occurred over a similar concentration range: 2 X 10(-5) - 5 X 10(-4) mol litre-1. With etomidate, inhibition occurred over a much lower concentration range (5 X 10(-8) - 5 X 10(-6) mol litre-1). The concentrations of anaesthetic which induced 50% inhibition of cortisol secretion were propofol 1.7 X 10(-4), thiopentone 1.6 X 10(-4), and etomidate 1.0 X 10(-7) mol litre-1.

Adrenal Glands↗