Remimazolam for anaesthesia or sedation

Sneyd, J. R.; Rigby-Jones, A. E.

doi:10.1097/aco.0000000000000877

Cited by 134 publications

(100 citation statements)

References 32 publications

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“…At present, there is a lack of data in comparison with propofol. As a benzodiazepine, remimazolam will be widely used in preoperative medication, endoscopy, induction and maintenance of general anaesthesia, and sedation of ICU patients in the future [25]. In previous studies, remimazolam was used effectively and safely in Chinese volunteers [21,26].…”

Section: Discussionmentioning

confidence: 99%

Efficacy and Safety of Remimazolam Besylate Versus Propofol during Hysteroscopy: Single‐centre Randomized Controlled Trial

Zhang¹,

Li²,

Liu³

2021

Preprint

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Background: Remimazolam besylate is a new type of benzodiazepine that has the characteristics of quick effects, short maintenance and recovery times, and no accumulation. Compound opioids can have a sedative effect in some endoscopic examinations. This trial was conducted to confirm the efficacy and safety of remimazolam besylate versus propofol during hysteroscopy.Methods: Patients undergoing hysteroscopy were randomly assigned to either the remimazolam (Group R, n=41) or the propofol group (Group P, n=41). Group R was administered an induction dosage of 0.2 mg/kg/min and a maintenance dosage of 1 mg/kg/h. Group P was started at 1.5-2.0 mg/kg propofol for up to 60-100 s and then maintained at 3.0-6.0 mg/kg/h. In both groups, remifentanil was infused using a target-controlled infusion system with a target concentration of 1.5 ng/ml and titrated during the procedure. The incidence rates of body movement and various adverse events in both groups were compared.Results: Eighty-two patients were included in this study. The incidence of adverse events in Group R (8.5%) was significantly lower than that in Group P (36.6%) (P < 0.05). Injection pain, postoperative dizziness and low SpO2 were the most common adverse events (P < 0.05). Compared with Group P patients, Group R patients recovered faster, had a shorter residence time in the PACU, and exhibited a higher quality of recovery (P < 0.05).Conclusion: Remimazolam besylate can provide safe and effective sedation for hysteroscopy. The depth of sedation is sufficient and effective, and the quality of recovery is high. Moreover, adverse events such as haemodynamic fluctuation, excessive sedation depth, low SpO2 and injection pain caused by propofol are largely avoided.Trial registrationThis study was approved by the Clinical Research Ethics Committee of Mengcheng County No.1 People's Hospital (2020MYL20003) and registered at http:// www.chictr.org.cn (15/09/2020, ChiCTR-2000038252). The study protocol is performed in the relevant guidelines.

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Section: Discussionmentioning

confidence: 99%

Efficacy and Safety of Remimazolam Besylate Versus Propofol during Hysteroscopy: Single‐centre Randomized Controlled Trial

Zhang¹,

Li²,

Liu³

2021

Preprint

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“…The major esterase responsible for remimazolam metabolism is often reported to be CES1 ( Freyer et al, 2019 ; Sneyd and Rigby-Jones, 2020 ; Zhou et al, 2020a ). However, no data appears to have been published to support this to date.…”

Section: Remimazolammentioning

confidence: 99%

“…Pharmacodynamic biomarker assessments have focused on EEG measures such as the bispectral index (BIS) score ( Bower et al, 2000 ) and scores from the Modified Observer’s Assessment of Alertness/Sedation (MOAA/S) scale ( Chernik et al, 1990 ). Some of the reasons to switch to a 3-compartment pharmacokinetic model are logical, e.g., reduced complexity and to facilitate dosing technologies such as target-controlled infusion ( Schüttler et al, 2020 ; Sneyd and Rigby-Jones, 2020 ). Other reasons for dismissing the Wiltshire model are less logical, e.g., to claim it is “discredited” ( Zhou et al, 2020a ) because it assumes lung metabolism.…”

Section: Remimazolammentioning

confidence: 99%

“…Benzodiazepines have been employed to provide anesthesia’s hypnotic component, but they are not widely used because of the variability of effect, extended duration of action, and lack of control of anesthesia depth ( Gamble et al, 1981 ; Saari et al, 2011 ). With the observation of the controllable short-acting effects of remimazolam, it became clear that it may be a useful agent in anesthesia (for comment see ( Masui, 2020 ; Sneyd and Rigby-Jones, 2020 )).…”

Section: Remimazolammentioning

confidence: 99%

“…In the anesthesia phase III studies, flumazenil was used as a reversal agent in subjects (∼5–10%) who had not awoken within 30min of the termination of remimazolam infusion ( Doi, et al, 2020b ; Doi, et al, 2020a ). The availability of a reversal agent provides a safety feature in case of overdose or adverse events that is not available for many other anesthetics, including propofol ( Sneyd and Rigby-Jones, 2020 ). An important factor to consider, however, is that flumazenil is itself an ester-based drug and has a short half-life and duration of action ( Lauven et al, 1985 ), so multiple doses may be required to avoid re-sedation events.…”

Section: Remimazolammentioning

confidence: 99%

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Remimazolam: Non-Clinical and Clinical Profile of a New Sedative/Anesthetic Agent

Kilpatrick¹

2021

Front. Pharmacol.

143

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A program to identify novel intravenous sedatives with a short and predictable duration of action was initiated in the late 1990’s by Glaxo Wellcome. The program focussed on the identification of ester-based benzodiazepine derivatives that are rapidly broken down by esterases. Remimazolam was identified as one of the lead compounds. The project at Glaxo was shelved for strategic reasons at the late lead optimization stage. Via the GSK ventures initiative, the program was acquired by the small biotechnology company, TheraSci, and, through successive acquisitions, developed as the besylate salt at CeNeS and PAION. The development of remimazolam besylate has been slow by industry standards, primarily because of the resource limitations of these small companies. It has, however, recently been approved for anesthesia in Japan and South Korea, procedural sedation in the United States, China, and Europe, and for compassionate use in intensive care unit sedation in Belgium. A second development program of remimazolam was later initiated in China, using a slightly different salt form, remimazolam tosylate. This salt form of the compound has also recently been approved for procedural sedation in China. Remimazolam has the pharmacological profile of a classical benzodiazepine, such as midazolam, but is differentiated from other intravenous benzodiazepines by its rapid conversion to an inactive metabolite resulting in a short onset/offset profile. It is differentiated from other intravenous hypnotic agents, such as propofol, by its low liability for cardiovascular depression, respiratory depression, and injection pain. The benzodiazepine antagonist flumazenil can reverse the effects of remimazolam in case of adverse events and further shorten recovery times. The aim of this review is to provide an analysis of, and perspective on, published non-clinical and clinical information on 1) the pharmacology, metabolism, pharmacokinetics, and pharmacodynamic profile of remimazolam, 2) the profile of remimazolam compared with established agents, 3) gaps in the current understanding of remimazolam, 4) the compound’s discovery and development process and 5) likely future developments in the clinical use of remimazolam.

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Oxadiazole: A highly versatile scaffold in drug discovery

Desai

Monapara

Jethawa

et al. 2022

Archiv der Pharmazie

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As a pharmacologically important heterocycle, oxadiazole paved the way to combat the problem associated with the confluence of many commercially available drugs with different pharmacological profiles. The present review focuses on the potential applications of five-membered heterocyclic oxadiazole derivatives, especially 1,2,4-oxadiazole, 1,2,5-oxadiazole, and 1,3,4-oxadiazole, as therapeutic agents. Designing new hybrid molecules containing the oxadiazole moiety is a better solution for the development of new drug molecules. The designed molecules may accumulate a biological profile better than those of the drugs currently available on the market. The present review will guide the way for researchers in the field of medicinal chemistry to design new biologically active molecules based on the oxadiazole nucleus. Antitubercular, antimalarial, anti-inflammatory, anti-HIV, antibacterial, and anticancer activities of various oxadiazoles have been reviewed extensively here.

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Remimazolam for anaesthesia or sedation

Abstract: We confirm that this paper has not been published in its current form or a substantially similar form (in print or electronically, including on a web site), that it has not been accepted for publication elsewhere, and that it is not under consideration by another publication.

Cited by 134 publications

References 32 publications

Efficacy and Safety of Remimazolam Besylate Versus Propofol during Hysteroscopy: Single‐centre Randomized Controlled Trial

Efficacy and Safety of Remimazolam Besylate Versus Propofol during Hysteroscopy: Single‐centre Randomized Controlled Trial

Remimazolam: Non-Clinical and Clinical Profile of a New Sedative/Anesthetic Agent

Oxadiazole: A highly versatile scaffold in drug discovery

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