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John W Sear
PURPOSE OF REVIEW: The current review examines the success and failures of the development of new hypnotic compounds for the human market. One of the important aspects is that one of the key present agents, propofol, is considered by many anaesthesiologists as 'the ideal'. However, all drugs have adverse or side-effects. RECENT FINDINGS: The last 30 years since the introduction of propofol has seen many new compounds evaluated; but as at the present time, only three agents may achieve a pivotal position in the market - fospropofol (a sedative agent which may have a role in endoscopic surgery); remimazolam (a short-acting benzodiazepine) whose development is also being focused on the sedation rather than anaesthesia market; and the pregnane steroid, alfaxalone (an anaesthetic agent first introduced in 1972, but withdrawn in 1984 because of adverse allergic reactions to the solvent, Cremophor EL) now solvented in a cyclodextrin...
May 29, 2018: Current Opinion in Anaesthesiology
Douglas K Rex, Raj Bhandari, Taddese Desta, Michael DeMicco, Cynthia Schaeffer, Kyle Etzkorn, Charles Barish, Ronald Pruitt, Brooks D Cash, Daniel Quirk, Felix Tiongco, Shelby Sullivan, David Bernstein
BACKGROUND: Remimazolam is an ultrashort-acting benzodiazepine. METHODS: We performed a randomized double-blind comparison of remimazolam to placebo for outpatient colonoscopy. This study design was a requirement of the U.S. Food and Drug Administration. An additional group was randomized to open-label midazolam administered according to its package insert instructions (randomization ratio for remimazolam:placebo:midazolam was 30:6:10). Study medications were administered under the supervision of the endoscopist, without any involvement of an anesthesia specialist...
April 30, 2018: Gastrointestinal Endoscopy
Narjeet Khurmi, Perene Patel, Molly Kraus, Terrence Trentman
Understanding the pharmacologic options for pediatric sedation outside the operating room will allow practitioners to formulate an ideal anesthetic plan, allaying anxiety and achieving optimal immobilization while ensuring rapid and efficient recovery. The authors identified relevant medical literature by searching PubMed, MEDLINE, Embase, Scopus, Web of Science, and Google Scholar databases for English language publications covering a period from 1984 to 2017. Search terms included pediatric anesthesia, pediatric sedation, non-operating room sedation, sedation safety, and pharmacology...
October 2017: Paediatric Drugs
Nikhil Chawla, Adjoa Boateng, Ranjit Deshpande
PURPOSE OF REVIEW: Procedures are increasingly being performed in the acute care setting, outside of the operating rooms (OR). This article aims to review the current literature on out-of-OR procedural sedation with a focus on the ICU and emergency department, highlighting the following topics: multidisciplinary team approach, choice of pharmacologic agent, sedation scales, current safety guidelines, anticipating complications, appropriate monitoring and necessary resources. RECENT FINDINGS: Subjective assessment of sedation using sedation scales is controversial...
August 2017: Current Opinion in Anaesthesiology
Tatjana Bevans, Cassandra Deering-Rice, Chris Stockmann, Joseph Rower, Derek Sakata, Christopher Reilly
BACKGROUND: Remimazolam is an ester-based short-acting benzodiazepine currently in clinical trials for IV administration. This study explored the feasibility of delivering remimazolam alone and as an adjunct to remifentanil via inhalation in rodent models. METHODS: Mice were exposed to remimazolam via inhalation; sedation was assessed using time to movement outside a set perimeter. Rats were also exposed to remimazolam aerosol alone and in combination with inhaled remifentanil, and analgesia was quantified by using a tail flick meter...
May 2017: Anesthesia and Analgesia
Ying Zhou, Pei Hu, Ji Jiang
Remimazolam is a new chemical entity belonging to the benzodiazepine class of sedative drugs, which shows faster-acting onset and recovery than currently available short-acting sedatives. In the present study, ultra high performance liquid chromatography with synapt high-definition mass spectrometry method combined with MassLynx software was established to characterize metabolites of remimazolam in human plasma and urine. In total, 5 human metabolites were detected, including 3 phase I and 2 phase II metabolites...
April 15, 2017: Journal of Pharmaceutical and Biomedical Analysis
Alexandra M Wesolowski, Michael P Zaccagnino, Raymond J Malapero, Alan D Kaye, Richard D Urman
Midazolam, fentanyl, and propofol are commonly used for sedation in modern anesthesia practice. These agents possess characteristics that have afforded various anesthetics to be delivered and produce relatively safe and effective outcomes. However, each agent has certain drawbacks in clinical practice. Remimazolam, a novel benzodiazepine created out of so-called soft drug development, is an ultrashort-acting intravenous sedative-hypnotic currently being investigated in clinical trials. In this review, we evaluate the recent literature on the use of remimazolam in clinical practice as compared with current sedative agents, and we describe its potential roles for use in sedation...
September 2016: Pharmacotherapy
Daniel J Pambianco, Keith M Borkett, Dennis S Riff, Peter J Winkle, Howard I Schwartz, Timothy I Melson, Karin Wilhelm-Ogunbiyi
BACKGROUND AND AIMS: Remimazolam is an ultra-short-acting benzodiazepine currently being developed for procedural sedation and for induction and maintenance of anesthesia. This trial was the fourth study for procedural sedation. The aim was to compare the safety and efficacy profile of remimazolam and to refine suitable doses for subsequent phase III studies in this indication. METHODS: This was a randomized, double-blind, parallel group, active controlled clinical trial with 162 male and female patients, aged 18 to 70, scheduled to undergo a routine colonoscopy...
May 2016: Gastrointestinal Endoscopy
Massimo Lamperti
PURPOSE OF REVIEW: The increasing request for procedural sedation will create in the upcoming future the need for a specific training in delivering care to patients in a continuum of sedation, whose effects and adverse events are unpredictable. The main debate in the past years has been focused on using drugs that could have few adverse effects and could be considered well tolerated when administered by a nonanaesthesiologist. Propofol remains the most used drug for procedural sedation, but given its side-effects, its administration is limited and suggested only when an anaesthesiologist is available...
December 2015: Current Opinion in Anaesthesiology
Tom G Hansen
PURPOSE OF REVIEW: There is a growing medical demand for suitable sedatives and analgesics to support the ongoing progress in diagnostic procedures and imaging techniques. This review provides an update of the pharmacology of the most commonly used drugs used for these procedures and shortly mention new drugs on the horizon. RECENT FINDINGS: There are many drugs available for procedural sedation; however, they all have drawbacks and shortcomings. Multiple adverse effects are associated with the use of these agents, hence monitoring is essential, and emergency equipment should be readily available...
August 2015: Current Opinion in Anaesthesiology
Romina G Ilic
No abstract text is available yet for this article.
2015: International Anesthesiology Clinics
Keith M Borkett, Dennis S Riff, Howard I Schwartz, Peter J Winkle, Daniel J Pambianco, James P Lees, Karin Wilhelm-Ogunbiyi
BACKGROUND: This exploratory study was the first study of remimazolam in patients to assess the safety and efficacy of different single doses for procedural sedation. METHODS: Patients scheduled to undergo a diagnostic upper gastrointestinal endoscopy were randomized to receive 1 of 3 doses of remimazolam or midazolam (25 per group) in a double-blind manner. After a single dose of study drug to achieve sedation, patients underwent gastroscopy. We assessed the success of the procedure, sedation levels, recovery from sedation, and safety...
April 2015: Anesthesia and Analgesia
Ying Zhou, Hongyun Wang, Ji Jiang, Pei Hu
A robust and validated method based on ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) has been developed for the simultaneous determination of remimazolam, which is a new chemical entity, and its major carboxylic acid metabolite (M1) in human plasma. Plasma samples were pre-purified by protein precipitation procedure and analyzed using an isocratic chromatographic separation over an Acquity UPLC CSH C18 column. The mobile phase consisted of acetonitrile-water containing 10mM ammonium formate and 0...
January 22, 2015: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Basavana Gouda Goudra, Preet Mohinder Singh
Although propofol has been the backbone for sedation in gastrointestinal endoscopy, both anesthesiologists and endoscopists are faced with situations where an alternative is needed. Recent national shortages forced many physicians to explore these options. A midazolam and fentanyl combination is the mainstay in this area. However, there are other options. The aim of this review is to explore these options. The future would be, invariably, to move away from propofol. The reason is not in any way related to the drawbacks of propofol as a sedative...
October 2014: Saudi Journal of Anaesthesia
Basavana Gouda Goudra, Preet Mohinder Singh
Remimazolam (CNS 7056) is a new drug innovation in anesthesia. It combines the properties of two unique drugs already established in anesthesia - Midazolam and remifentanil. It acts on GABA receptors like midazolam and has organ-independent metabolism like remifentanil. It is likely to be the sedative of the future, as preliminary phase II trials have shown minimal residual effects on prolonged infusions. It has potential to be used as a sedative in ICU and as a novel agent for procedural sedation. Unlike most rapidly acting intravenous sedatives available presently, the propensity to cause apnea is very low...
July 2014: Saudi Journal of Anaesthesia
P Buchwald, N Bodor
This paper summarizes recent developments in the field of soft drug development as collected and reviewed for the 9th Retrometabolism-Based Drug Design and Targeting Conference. Soft drugs are still often confused with prodrugs because they both require metabolic transformations; however, they are conceptual opposites: whereas, prodrugs are pharmacologically inactive and are converted by a predictable mechanism to the active drug, soft drugs are active therapeutic agents as such and are designed to undergo a predictable and controllable metabolic deactivation after exerting their desired therapeutic effect...
June 2014: Die Pharmazie
Mark T Worthington, Laurie J Antonik, D Ronald Goldwater, James P Lees, Karin Wilhelm-Ogunbiyi, Keith M Borkett, Mack C Mitchell
BACKGROUND: We performed the first multiple dose study of remimazolam designed to assess both the feasibility of maintaining suitable sedation during colonoscopy and reversing the sedative effects of remimazolam with flumazenil. METHODS: Healthy volunteers received fentanyl followed by remimazolam for sedation during colonoscopy. Three dose groups of 15 volunteers each received remimazolam in increasing initial doses, plus top-up doses to maintain sedation for a 30-minute period...
November 2013: Anesthesia and Analgesia
Tony Gin
PURPOSE OF REVIEW: Many studies of new intravenous sedative drugs have been published last year, including several phase I trials. This review provides a brief summary of these studies, with recommendations for selected reading. RECENT FINDINGS: Remimazolam is a rapidly metabolized benzodiazepine. Early clinical trials confirm more rapid recovery compared with midazolam. Etomidate analogues can be designed with rapid metabolism and without adrenocortical suppression, but research is only at the preclinical stage...
August 2013: Current Opinion in Anaesthesiology
Hovig V Chitilian, Roderic G Eckenhoff, Douglas E Raines
The ideal sedative-hypnotic drug would be a rapidly titratable intravenous agent with a high therapeutic index and minimal side effects. The current efforts to develop such agents are primarily focused on modifying the structures of existing drugs to improve their pharmacodynamic and pharmacokinetic properties. Drugs currently under development using this rational design approach include analogues of midazolam, propofol, and etomidate, such as remimazolam, PF0713, and cyclopropyl methoxycarbonyl-etomidate (MOC-etomidate), respectively...
2013: Surgical Neurology International
J Robert Sneyd
No abstract text is available yet for this article.
August 2012: Anesthesia and Analgesia
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