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Etomidate

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https://www.readbyqxmd.com/read/28514325/an-etomidate-analogue-with-less-adrenocortical-suppression-stable-hemodynamics-and-improved-behavioral-recovery-in-rats
#1
Bin Wang, Jun Yang, Jun Chen, Yi Kang, Ling-Hui Yang, Jin Liu, Wen-Sheng Zhang
BACKGROUND: ET-26 hydrochloride (ET-26HCl) is a novel etomidate analogue designed to alleviate the adrenocortical suppression caused by etomidate while retaining the rapid sedative-hypnotic onset and stable hemodynamic features of etomidate. This study compared the anesthetic effect, hemodynamic stability, and recovery profiles of ET-26HCl, etomidate, and the sedative-hypnotic drug propofol in rats. METHODS: The metabolic half-life of ET-26HCl was determined in vitro using high performance liquid chromatography analysis of samples of rat plasma and liver homogenates taken from 3 animals...
May 12, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28505538/synthesis-and-pharmacological-evaluation-of-neurosteroid-photoaffinity-ligands
#2
Pavel Y Savechenkov, David C Chiara, Rooma Desai, Alexander T Stern, Xiaojuan Zhou, Alexis M Ziemba, Andrea L Szabo, Yinghui Zhang, Jonathan B Cohen, Stuart A Forman, Keith W Miller, Karol S Bruzik
Neuroactive steroids are potent positive allosteric modulators of GABAA receptors (GABAAR), but the locations of their GABAAR binding sites remain poorly defined. To discover these sites, we synthesized two photoreactive analogs of alphaxalone, an anesthetic neurosteroid targeting GABAAR, 11β-(4-azido-2,3,5,6-tetrafluorobenzoyloxy)allopregnanolone, (F4N3Bzoxy-AP) and 11-aziallopregnanolone (11-AziAP). Both photoprobes acted with equal or higher potency than alphaxalone as general anesthetics and potentiators of GABAAR responses, left-shifting the GABA concentration - response curve for human α1β3γ2 GABAARs expressed in Xenopus oocytes, and enhancing [(3)H]muscimol binding to α1β3γ2 GABAARs expressed in HEK293 cells...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28484025/common-general-anesthetic-propofol-impairs-kinesin-processivity
#3
Brandon M Bensel, Stephanie Guzik-Lendrum, Erin M Masucci, Kellie A Woll, Roderic G Eckenhoff, Susan P Gilbert
Propofol is the most widely used i.v. general anesthetic to induce and maintain anesthesia. It is now recognized that this small molecule influences ligand-gated channels, including the GABAA receptor and others. Specific propofol binding sites have been mapped using photoaffinity ligands and mutagenesis; however, their precise target interaction profiles fail to provide complete mechanistic underpinnings for the anesthetic state. These results suggest that propofol and other common anesthetics, such as etomidate and ketamine, may target additional protein networks of the CNS to contribute to the desired and undesired anesthesia end points...
May 8, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28462732/anaesthesia-for-electroconvulsive-therapy-new-tricks-for-old-drugs-a-systematic-review
#4
Tobias Kvist Stripp, Martin Balslev Jorgensen, Niels Vidiendal Olsen
OBJECTIVE: The objective of this review is to investigate existing literature in order to delineate whether the use of anaesthesia and timing of seizure induction in a new and optimised way may improve the efficacy of electroconvulsive therapy (ECT). METHODS: PubMed/MEDLINE was searched for existing literature, last search on 24 June 2015. Relevant clinical studies on human subjects involving choice of anaesthetic, ventilation and bispectral index (BIS) monitoring in the ECT setting were considered...
May 2, 2017: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/28459733/a-phase-1-single-center-double-blind-placebo-controlled-study-in-healthy-subjects-to-assess-the-safety-tolerability-clinical-effects-and-pharmacokinetics-pharmacodynamics-of-intravenous-cyclopropyl-methoxycarbonylmetomidate-abp-700-after-a-single-ascending
#5
Michel M R F Struys, Beatrijs I Valk, Douglas J Eleveld, Anthony R Absalom, Peter Meyer, Sascha Meier, Izaak den Daas, Thomas Chou, Kai van Amsterdam, Jason A Campagna, Steven P Sweeney
BACKGROUND: Cyclopropyl-methoxycarbonylmetomidate (ABP-700) is a new "soft" etomidate analog. The primary objectives of this first-in-human study were to describe the safety and efficacy of ABP-700 and to determine its maximum tolerated dose. Secondary objectives were to characterize the pharmacokinetics of ABP-700 and its primary metabolite (cyclopropyl-methoxycarbonyl acid), to assess the clinical effects of ABP-700, and to investigate the dose-response and pharmacokinetic/pharmacodynamic relationships...
May 1, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28450928/effect-of-etomidate-on-the-oxidative-stress-response-and-levels-of-inflammatory-factors-from-ischemia-reperfusion-injury-after-tibial-fracture-surgery
#6
Renke Li, Lei Fan, Fenglei Ma, Yongyan Cao, Junwei Gao, Huawen Liu, Yan Li
The effect of etomidate on the oxidative stress response and levels of inflammatory factors resulting from ischemia-reperfusion injury of the lower extremities during tibial fracture surgery were investigated. From December 2013 to June 2015, 60 tibial fracture patients with surgical indications for open reduction and internal fixation were selected. Patients were randomly divided into the observation group and the control group. All patients were stanched by tourniquet hemostasis. Patients in the observation group were anesthetized with etomidate (3-6 mg/kg·h) + remifentanil (0...
March 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28433802/role-of-environmental-stressors-in-determining-the-developmental-outcome-of-neonatal-anesthesia
#7
Ling-Sha Ju, Jiao-Jiao Yang, Nikolaus Gravenstein, Christoph N Seubert, Timothy E Morey, Colin Sumners, Terrie Vasilopoulos, Jian-Jun Yang, Anatoly E Martynyuk
BACKGROUND: The majority of studies evaluating neurocognition in humans who had procedures under anesthesia early in life found long-term deficits even though the typical anesthesia duration normalized to the human life span is much shorter than that shown to induce developmental abnormalities in rodents. Therefore, we studied whether subsequent environmental stressors contribute to deficiencies programmed by a brief neonatal etomidate exposure. METHODS: Postnatal days (P) 4, 5, or 6, Sprague-Dawley rats, pretreated with vehicle or the Na(+)-K(+)-2Cl(-) (NKCC1) inhibitor, bumetanide, received two injections of etomidate resulting in anesthesia for 2h...
April 7, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28431430/contrasting-effects-of-the-%C3%AE-aminobutyric-acid-type-a-receptor-%C3%AE-3-subunit-n265m-mutation-on-loss-of-righting-reflexes-induced-by-etomidate-and-the-novel-anesthetic-barbiturate-r-mtfd-mpab-erratum
#8
https://www.readbyqxmd.com/read/28424861/s-ketamine-compared-to-etomidate-during-electroconvulsive-therapy-in-major-depression
#9
Maxim Zavorotnyy, Ina Kluge, Kathrin Ahrens, Thomas Wohltmann, Benjamin Köhnlein, Patricia Dietsche, Udo Dannlowski, Tilo Kircher, Carsten Konrad
Objective of the study was to compare two commonly used anesthetic drugs, S-ketamine and etomidate, regarding their influence on seizure characteristics, safety aspects, and outcome of electroconvulsive therapy (ECT) in major depression. Treatment data of 60 patients who underwent a total number of 13 ECTs (median) because of the severe or treatment-resistant major depressive disorder (DSM-IV) were analyzed. Etomidate, mean dosage (SD) = 0.25 (0.04) mg/kg, was used for anesthesia in 29 participants; 31 patients received S-ketamine, mean dosage (SD) = 0...
April 19, 2017: European Archives of Psychiatry and Clinical Neuroscience
https://www.readbyqxmd.com/read/28416372/effects-of-bilobalide-ginkgolide-b-and-picrotoxinin-on-gabaa-receptor-modulation-by-structurally-diverse-positive-modulators
#10
Chiu Chin Ng, Rujee K Duke, Tina Hinton, Graham A R Johnston
Anxiolytics and anticonvulsants generally positively modulate the action of GABA, whereas many convulsants (including the chloride channel blocker picrotoxinin) negatively modulate the action of GABA on GABAA receptors. Like picrotoxinin, bilobalide and ginkgolide B, active constituents of Ginkgo biloba, have been shown to negatively modulate the action of GABA at α1β2γ2L GABAA receptors. However, unlike picrotoxinin, bilobalide and ginkgolide B are not known to cause convulsions. We have assessed the action of bilobalide, ginkgolide B and picrotoxinin on a range of GABAA modulators (etomidate, loreclezole, propofol, thiopentone sodium, diazepam, and allopregnanolone), using two-electrode voltage clamp electrophysiology at recombinant α1β2γ2L GABAA receptors expressed in Xenopus oocytes...
April 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28415947/effect-of-pretreatment-with-midazolam-on-etomidate-induced-myoclonus-a-meta-analysis
#11
Chengmao Zhou, Yu Zhu, Zhen Liu, Lin Ruan
Objective To investigate the effect of pretreatment with midazolam on myoclonus induced by etomidate injection. Methods A meta-analysis was performed using Review Manager software, version 5.2. Two researchers independently searched PubMed, Cochrane Library, and Embase® databases for randomized controlled trials involving patients who underwent etomidate induced general anaesthesia with or without midazolam pretreatment, published between 1990 and 2016. Outcome measures comprised overall myoclonus incidence rate and incidence rate classified by degree of myoclonus following etomidate injection...
April 2017: Journal of International Medical Research
https://www.readbyqxmd.com/read/28406323/the-inhibiting-effect-of-intravenous-anesthesia-on-adrenal-gland-functions-under-the-sepsis-condition
#12
Te Wang, Changdong Liu, Pihong Wei, Lili Lv, Zaiqi Yang
This study aims to explore the effect of intravenous anesthesia on the adrenal gland functions of rats with sepsis as well as on their lungs and adrenal gland tissues in order to provide a theoretical reference for the cure of sepsis. Female Sprague Dawley (SD) rats were taken as the research objects in this study. Venous channels of rats were constructed by catheterization through the external jugular vein, and the cecal ligation and puncture technique was adopted to duplicate the sepsis rat models. The level of tumor necrosis factor-α (TNF-α) in serum was detected using enzyme-linked immunosorbent assay (ELISA), and necrocytosis was observed by the fluorescent staining method...
April 1, 2017: International Journal of Immunopathology and Pharmacology
https://www.readbyqxmd.com/read/28404686/propofol-anesthesia-is-reduced-in-phospholipase-c-related-inactive-protein-type-1-knockout-mice
#13
Yoshikazu Nikaido, Tomonori Furukawa, Shuji Shimoyama, Junko Yamada, Keisuke Migita, Kohei Koga, Tetsuya Kushikata, Kazuyoshi Hirota, Takashi Kanematsu, Masato Hirata, Shinya Ueno
The GABA type A receptor (GABAA-R) is a major target of intravenous anesthetics. Phospholipase C-related inactive protein type-1 (PRIP-1) is important in GABAA-R phosphorylation and membrane trafficking. In this study, we investigated the role of PRIP-1 in general anesthetic action. The anesthetic effects of propofol, etomidate, and pentobarbital were evaluated in wild-type and PRIP-1 knockout (PRIP-1 KO) mice by measuring the latency and duration of loss of righting reflex (LORR) and loss of tail-pinch withdrawal response (LTWR)...
June 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28389811/general-anesthetic-actions-on-gabaa-receptors-in-vivo-are-reduced-in-phospholipase-c-related-catalytically-inactive-protein-knockout-mice
#14
Masaki Hayashiuchi, Tomoya Kitayama, Katsuya Morita, Yosuke Yamawaki, Kana Oue, Taiga Yoshinaka, Satoshi Asano, Kae Harada, Youngnam Kang, Masato Hirata, Masahiro Irifune, Mitsugi Okada, Takashi Kanematsu
PURPOSE: The aim of this study was to investigate the action of general anesthetics in phospholipase C-related catalytically inactive protein (PRIP)-knockout (KO) mice that alter GABA receptor signaling. METHODS: PRIP regulates the intracellular trafficking of β subunit-containing GABAA receptors in vitro. In this study, we examined the effects of intravenous anesthetics, propofol and etomidate that act via β subunit-containing GABAA receptors, in wild-type and Prip-KO mice...
April 7, 2017: Journal of Anesthesia
https://www.readbyqxmd.com/read/28337880/effects-of-anesthesia-using-propofol-and-etomidate-on-t-lymphocyte-subpopulation-of-infectious-shock-patients-in-perioperative-period
#15
Y Wang, J Zhang, S J Zhang
Infectious or septic shock is induced when a toxic microorganism invades blood circulation in the human body. Emergency operation is an effective method for treating infectious shock in the early stages although the use of anesthesia is more complex due to the internal disorders caused by the disease. This study explored the effects of propofol and etomidate anesthesia on the cellular immune function (T lymphocyte subpopulation) of infectious shock patients, aiming to provide a basis for the selection of the proper anesthetic method...
January 2017: Journal of Biological Regulators and Homeostatic Agents
https://www.readbyqxmd.com/read/28337083/continuous-infusion-etomidate-in-a-patient-receiving-extracorporeal-membrane-oxygenation
#16
Joseph M LaRochelle, Bonnie Desselle, Janet L Rossi
We describe a 16-year-old, 65-kg male deployed on extracorporeal membrane oxygenation (ECMO) for refractory respiratory failure secondary to ingestion of multiple substances. During his ECMO course, standard sedative and analgesic strategies failed and alternative medications were used. The patient received various dosages of fentanyl, morphine, hydromorphone, clonidine patches, dexmedetomidine, lorazepam, methadone, pentobarbital, olanzapine, and propofol. Despite administration of multiple agents, on day 29 of ECMO the patient experienced elevated blood pressures due to agitation, and continuous infusion etomidate was started...
January 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/28291508/parecoxib-sodium-pretreatment-reduces-myoclonus-after-etomidate-a-prospective-double-blind-randomized-clinical-trial%C3%A2
#17
Xiuze Li, Jun Liu, Mengjun Zhou, Chaojing Zhou
OBJECTIVE: Myoclonus induced by etomidate during induction of general anesthesia is a common phenomenon. This prospective, randomized, saline-controlled clinical study was performed to evaluate the effect of parecoxib sodium pretreatment on the incidence and severity of etomidate-induced myoclonus. METHODS: 60 patients, American Society of Anesthesiologists (ASA) physical status I or II, aged 20 to 60 years, who were scheduled to undergo elective laparoscopic cholecystectomy under general anesthesia, were allocated randomly into one of two groups to receive parecoxib sodium 40 mg intravenous (group P, n = 30) or the same volume of saline (group S, n = 30) 30 minutes before administration of etomidate (0...
March 14, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28284883/etomidate-versus-propofol-sedation-for-complex-upper-endoscopic-procedures-a-prospective-double-blinded-randomized-controlled-trial
#18
Mi Gang Kim, Se Woo Park, Jae Hyun Kim, Jin Lee, Sea Hyub Kae, Hyun Joo Jang, Dong Hee Koh, Min Ho Choi
BACKGROUND AND AIMS: Although a growing body of evidence demonstrates that propofol-induced deep sedation can be effective and performed safely, cardiopulmonary adverse events have been observed frequently. Etomidate is a new emerging drug that provides hemodynamic and respiratory stability, even in high-risk patient groups. The objective of this study was to compare safety and efficacy profiles of etomidate and propofol for endoscopic sedation. METHODS: A total of 128 patients undergoing EUS were randomized to receive either etomidate or propofol blinded administered by a registered nurse...
March 8, 2017: Gastrointestinal Endoscopy
https://www.readbyqxmd.com/read/28223779/effect-of-dexmedetomidine-in-preventing-etomidate-induced-myoclonus-a-meta-analysis
#19
REVIEW
Xueke Du, Chengmao Zhou, Linghui Pan, Changlong Li
OBJECTIVE: To investigate the effect of dexmedetomidine in the prevention of etomidate-induced myoclonus. METHODS: We searched for randomized controlled trials (RCTs) regarding the use of dexmedetomidine in preventing etomidate-induced myoclonus in the databases PubMed, EMBASE, the Cochrane Library, and CNKI. We extracted data and assessed the quality of the literature and adopted RevMan 5.2 to conduct meta-analysis on each effective index and employed funnel plot to test publication bias...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28217049/effectiveness-of-sodium-thiopentone-propofol-and-etomidate-as-an-ideal-intravenous-anesthetic-agent-for-modified-electroconvulsive-therapy
#20
Altaf Hussain Mir, Nida Farooq Shah, Mehraj Ud Din, Shabir Ahmad Langoo, Fayaz Ahmad Reshi
INTRODUCTION: Electroconvulsive therapy (ECT) is a well-established psychiatric treatment in which seizures are electrically induced in patients for therapeutic effects. ECT can produce severe disturbances in the cardiovascular system and a marked increase in cerebral blood flow and intracranial pressure. These cardiovascular changes may be altered using various anesthetic drugs. AIM AND OBJECTIVES: This study was undertaken to compare the effects of intravenous (IV) sodium thiopentone, propofol, and etomidate, used as IV anesthetic agents in modified ECT as regards, induction time and quality of anesthesia, alteration of hemodynamics, seizure duration, and recovery time...
January 2017: Saudi Journal of Anaesthesia
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