How to administer remimazolam for anesthesia induction

Hirata, Naoyuki; Hayamizu, Kengo; Yamakage, Michiaki

doi:10.1007/s00540-020-02864-x

Cited by 14 publications

(11 citation statements)

References 2 publications

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“…To date, there have been no published clinical trials of bolus administration of remimazolam to induce anesthesia; thus, bolus administration is not currently recommended for general anesthesia. Therefore, future trials on bolus remimazolam injection for induction of general anesthesia are warranted to establish more practical administration methods [ 44 ].…”

Section: Clinical Applications Of Remimazolammentioning

confidence: 99%

Remimazolam: pharmacological characteristics and clinical applications in anesthesiology

Kim

2022

Anesth Pain Med

122

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A novel ultra-short-acting benzodiazepine (BDZ), remimazolam (CNS 7056), has been designed by ‘soft drug’ development to achieve a better sedative profile than that of the current drugs. Notably, the esterase linkage in remimazolam permits rapid hydrolysis to inactivate metabolites by non-specific tissue esterase and induces a unique and favorable pharmacological profile, including rapid onset and offset of sedation and a predictable duration of action. Similar to other BDZs, its sedative effects can be reversed using flumazenil, a BDZ antagonist. The pharmacokinetics and pharmacodynamics of remimazolam are characterized by relatively high clearance, small steady-state volume of distribution, short elimination half-life, short context-sensitive half-life, and fast onset and recovery, indicating rapid elimination, minimal tissue accumulation, and good control. In addition, remimazolam possesses a superior safety profile, including low liability for cardiorespiratory depression and injection pain, making it a preferred hypnotic agent in various clinical settings. Early clinical investigations suggest that remimazolam is well tolerated and effective for procedural sedation and for induction and maintenance of general anesthesia. To date, however, the clinical use of remimazolam has been confined to a few volunteer studies and a limited number of clinical investigations. Therefore, further studies regarding its recovery issues or postoperative complications, characteristics of electroencephalogram changes, and cost-benefit analyses are required to facilitate its widespread use.

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Section: Clinical Applications Of Remimazolammentioning

confidence: 99%

Remimazolam: pharmacological characteristics and clinical applications in anesthesiology

Kim

2022

Anesth Pain Med

122

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“…Remimazolam besylate is formulated as a lyophilized product for reconstitution ( FDA, 2020a ) but has sparing aqueous solubility, meaning that relatively large administration volumes need to be employed to accommodate the doses required in the anesthesia setting ( Hirata et al, 2020 ).…”

Section: Remimazolammentioning

confidence: 99%

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

Kilpatrick¹

2021

Front. Pharmacol.

129

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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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“…The manufacturer proposes continuous intravenous infusion for administering remimazolam (1-mg remimazolam per 1-mL normal saline), starting at a rate of 6 mg/kg/h (0.1 mg/kg/min) or 12 mg/kg/h (0.2 mg/kg/min) until loss of consciousness (LoC) is achieved for anesthesia induction in adults (Table 1) [15][16][17][18][19]. Subsequently, this infusion rate should be decreased at a rate of 1 mg/kg/h as appropriate to maintain proper anesthetic depth (maximum allowable rate, 2 mg/kg/h) [17][18][19][20]. The infusion rates can be adjusted according to the patient's condition.…”

Section: Clinical Doses Of Remimazolammentioning

confidence: 99%

Clinical profile of a new anesthetic: remimazolam

Lee

Kim

2023

Med Biol Sci Eng

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Remimazolam is a novel ultrashort-acting benzodiazepine that acts on g-aminobutyric acid A receptor. It has been approved for use as a general anesthetic and sedative. This medication is recommended for inducing and maintaining anesthesia using continuous intravenous infusion; however, bolus dosing of remimazolam can also be adopted. Continuous intravenous infusion should be started at a rate of 6 or 12 mg/kg/h until loss of consciousness is achieved. Subsequently, this infusion rate should be decreased at a rate of 1 mg/kg/h as appropriate to maintain proper anesthetic depth (maximum allowable rate, 2 mg/kg/h). These recommended doses show more stable hemodynamics than those of propofol. The clinical profiles of anesthesia induction and maintenance are comparable between remimazolam and propofol. Although remimazolam has a slightly longer anesthetic induction time than propofol, the results are not inferior to each other. Recovery profiles show somewhat contradictory results, but the effects of remimazolam and propofol are comparable. Whether the bispectral index or other anesthetic depth indices are suitable for monitoring the sedative effect of remimazolam remains controversial. The appropriate ranges of electroencephalography (EEG) indices for remimazolam are unclear, but it has higher EEG indices than propofol. Thus, co-administration of opioids with a low dose of remimazolam is recommended to maintain the appropriate ranges for patients. Despite the favorable effects of remimazolam, the risk of re-sedation should always be considered after remimazolam reversal, especially when using flumazenil. Thus, remimazolam is considered comparable with propofol for inducing general anesthesia.

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How to administer remimazolam for anesthesia induction

Cited by 14 publications

References 2 publications

Remimazolam: pharmacological characteristics and clinical applications in anesthesiology

Remimazolam: pharmacological characteristics and clinical applications in anesthesiology

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

Clinical profile of a new anesthetic: remimazolam

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