Sedation outcomes for remimazolam, a new benzodiazepine

Abstract

Remimazolam is a new ultrashort-acting benzodiazepine with fast onset, quick recovery, and few side effects, such as hypotension and respiratory depression. It is expected to be safe and effective for a wide range of patients undergoing intravenous sedation for dental procedures. The aim of this literature review was to evaluate clinical and sedation outcomes for remimazolam, including method of administration, level of sedation at the dose required, and clinical adverse events. An electronic literature search of databases was conducted, and eight articles were selected for inclusion in this review. Onset time from drug administration to optimal sedation level was faster for remimazolam (around 1.5-6.4 min) than for midazolam. Recovery time was significantly shorter for remimazolam than for midazolam and propofol. A study comparing various doses of remimazolam with midazolam found no significant difference in safety. Comparison of a remimazolam group with a propofol group showed that incidences of hypotension (13.0% vs 42.9%, respectively) and respiratory depression (1.1% vs 6.9%, respectively) were significantly lower for remimazolam. Remimazolam appears to be an ideal sedative.

Remimazolam: pharmacological characteristics and clinical applications in anesthesiology

“…Although it has a rapid onset of action and a very short half-life, it precipitates more adverse events, notably possible hypotension, respiratory depression, bradycardia, and pain upon injection. Therefore, there is a need for safer sedatives while ensuring their efficacy [ 35 ]. Clinical studies comparing efficacy and safety of remimazolam vs. propofol for procedural sedation suggested that remimazolam was non-inferior in terms of sedative efficacy and exhibited better safety profile than that of propofol [ 32 , 34 , 36 ].…”

Efficacy of Remimazolam for Procedural Sedation in American Society of Anesthesiologists (ASA) I to IV Patients Undergoing Colonoscopy: A Systematic Review and Meta-Analysis

“…It has a high affinity and selectivity for the benzodiazepine site on the GABA receptors [ 21 - 22 ]. Furthermore, the metabolite of remimazolam has a lower affinity for the benzodiazepine receptors than the metabolite of midazolam, α-hydromidazolam [ 23 ]. The addition of a carboxylic ester in the benzodiazepines makes it receptive to tissue esterases (CES), resulting in a pharmacologically inactive metabolite, CNS-7054.…”

Retrospective audit of midazolam dose and intravenous sedation record keeping in a primary care oral surgery service

“…8 Remimazolam is a new benzodiazepine that has recently been found to provide good outcomes in conscious sedation in dentistry due to its ultrashort-acting properties. 9 Remimazolam, as its name suggests, combines the properties of midazolam and remifentanil and it acts on the gamma aminobutyric acid (GABA) receptors, but its ester-linked side chain to the diazepine ring makes it an ultrashort-acting sedation drug that is metabolised rapidly to inactive metabolites by liver tissue esterases. 9 Also, the hepatic drug-metabolising enzyme cytochrome P450 (CYP) is not involved in the metabolism, similar to that of remifentanil.…”

“…9 Remimazolam, as its name suggests, combines the properties of midazolam and remifentanil and it acts on the gamma aminobutyric acid (GABA) receptors, but its ester-linked side chain to the diazepine ring makes it an ultrashort-acting sedation drug that is metabolised rapidly to inactive metabolites by liver tissue esterases. 9 Also, the hepatic drug-metabolising enzyme cytochrome P450 (CYP) is not involved in the metabolism, similar to that of remifentanil. 10 These combined properties therefore make remimazolam a drug of fast onset, high clearance, short half-life, and few side-effects.…”

“…10 These combined properties therefore make remimazolam a drug of fast onset, high clearance, short half-life, and few side-effects. 9 Due to remimazolam’s novelty, more studies are warranted to further evaluate and establish its safety in dental sedation.…”