With the ongoing advancement of comfort-oriented healthcare, procedural sedation is increasingly applied in clinical practice. As a novel benzodiazepine derivative, remimazolam offers distinct advantages in procedural sedation. This paper aims to thoroughly examine its pharmacological properties and key clinical applications, providing systematic guidance for rational clinical use while promoting further adoption and development of this medication in relevant fields.
Conduct a systematic analysis and summary by examining the pharmacological characteristics of remimazolam, including its mechanism of action and pharmacokinetic properties, and integrating its application scenarios, dosing regimens, and comparative efficacy data across various clinical sedation procedures.
Remimazolam, with its unique pharmacological advantages—such as rapid onset, short duration of action, inactive metabolites, and high safety profile—demonstrated excellent sedative efficacy and tolerability in clinical procedural sedation. It effectively meets sedation requirements across diverse procedural settings while exhibiting a low incidence of adverse reactions, thereby offering significant clinical value.
As a novel benzodiazepine derivative, remimazolam overcomes the limitations of traditional sedatives, offering a new option for procedural sedation in palliative care. Its unique pharmacologic properties ensure rapid onset, controllable duration of action, and high safety, thereby enhancing clinical procedural efficiency and patient experience. This systematic review of its clinical applications provides scientific evidence for the rational and standardized use of remimazolam in clinical practice. Future research should focus on expanding its application in more complex clinical scenarios and conducting long-term safety and efficacy studies to further promote the widespread use of remimazolam in procedural sedation.
With the advancement of comfort-oriented healthcare, procedural sedation has gained widespread clinical application due to its controllable administration and minimal impact on vital signs. As a novel ester-type benzodiazepine, remimazolam has demonstrated significant potential across multiple clinical scenarios. This review explores the pharmacologic properties of remimazolam and its clinical applications in procedural sedation.
Remimazolam, as a short-acting benzodiazepine, primarily exerts its effects by binding to GABAA receptors containing the α1 subunit within the central nervous system. Upon binding to GABAA receptors, remimazolam enhances the permeability of nerve cells to chloride ions. Chloride ions enter the nerve cells via concentration gradients, inducing hyperpolarization and reducing excitability. This ultimately results in sedative, hypnotic, and anxiolytic effects (
Remimazolam is completely absorbed by the gastrointestinal tract after oral administration. However, due to its rapid and extensive first-pass elimination, its oral bioavailability is virtually negligible. Furthermore, the clearance rate of remimazolam and its metabolites from plasma is relatively fast after oral administration, making it difficult to produce significant sedative effects. Combined with its characteristic bitter taste, remimazolam is unsuitable for direct oral use (
Intravenous infusion of remimazolam is a commonly used clinical approach. Following injection, the drug concentration in the blood reaches its peak almost immediately and rapidly distributes to the target sites. Its average half-life ranges between 0.5 and 2 min, and the cumulative dose exhibits a dose-dependent relationship with the area under the plasma concentration-time curve (
Current research indicates that remimazolam can also be administered via the nasal route. The absorption rate of this drug through the nasal mucosa is approximately 1/50th that of intravenous administration. To achieve the same blood concentration as intravenous administration, a dose 5 to 10 times higher than the intravenous dose is required (
Remimazolam has a relatively small volume of distribution, approximately 50–70 L. After entering the body, it is primarily distributed in bodily fluids such as blood and interstitial fluid, with relatively little accumulation in tissues like adipose tissue. Remimazolam exhibits a high serum protein binding rate of 92%, primarily binding to site II of albumin (
Remimazolam is primarily and rapidly hydrolyzed
Remimazolam, as a novel benzodiazepine sedative, has demonstrated favorable performance in the clinical application of regional anesthesia sedation. In the field of combined spinal-epidural anesthesia (CSEA) sedation, Song et al. determined the median effective dose (ED50) of remimazolam for sedation in elderly patients undergoing CSEA for hip replacement surgery to be 0.212 mg/kg, with a 95% effective dose (ED95) of 0.288 mg/kg (
In recent years, remimazolam has gained widespread adoption in procedural sedation for gynecological hysteroscopic surgery due to its unique advantages. In comparison with the traditional sedative propofol, multiple studies have demonstrated that remimazolam exhibits a more pronounced sedative effect. Zhang et al. found in a single-center randomized controlled trial that the remimazolam group exhibited significantly lower incidence of hypotension (5% vs. 43.3%, P < 0.001) and hypoxemia (3.3% vs. 20.0%, P = 0.006) during sedation compared to the propofol group. Additionally, the remimazolam group exhibited shorter recovery times (7.0 ± 1.5 min vs. 10.0 ± 2.0 min, P < 0.001) and higher anesthetic satisfaction scores from surgeons. These findings suggest that remimazolam provides a safer and more comfortable surgical environment while maintaining adequate anesthetic efficacy (
Dental procedures often cause anxiety, stress, and fear in patients. In recent years, the use of remimazolam in dentistry has garnered significant attention and research. A prospective exploratory study demonstrated that remimazolam monotherapy achieved a 100% success rate in sedation during outpatient third molar extraction, with no significant respiratory or circulatory effects observed during sedation and no need for additional pharmacological intervention (
Endoscopic retrograde cholangiopancreatography (ERCP) urgently requires an ideal sedative to enhance patient comfort, and remimazolam, as a novel sedative, demonstrates significant application potential in this field. Lee et al. compared the efficacy and safety of remimazolam versus propofol in a study of ERCP patients. Results demonstrated a 100% sedation success rate for remimazolam, along with predictable duration of action and high sedation safety. This study suggests that remimazolam may serve as a safe and effective procedural sedation regimen, offering clinicians a broader range of sedation options. This confirms remimazolam as a safe and effective sedation option capable of replacing propofol, offering clinicians a broader range of sedation choices (
To date, numerous scholars have explored the efficacy of using remimazolam for sedation during bronchoscopy. Zhou et al. conducted a meta-analysis to evaluate the safety and efficacy of remimazolam for patient sedation during flexible bronchoscopy. The results indicated that remimazolam demonstrated comparable sedation success rates to conventional agents (e.g., propofol, dexmedetomidine, midazolam) while exhibiting weaker respiratory and circulatory depressant effects, thereby offering superior safety (
With the growing demand for comfortable medical care, endoscopic procedures are increasingly becoming the mainstream choice. In the field of painless gastroscopy, Zhu et al. compared the sedative effects of different doses of remimazolam versus propofol during gastroscopy. found that the high-dose remimazolam group (0.2 mg/kg) demonstrated not only a higher sedation success rate but also superior safety compared to both the propofol group (1.5 mg/kg) and the low-dose remimazolam group (0.15 mg/kg) (P < 0.001) (
Remimazolam is not only widely used in the aforementioned common procedural sedation operations but also demonstrates new exploration and application potential in other fields. In facial plastic surgery, Huang et al. found that during intubation-free anesthesia for facial procedures, remimazolam demonstrated comparable sedative effects to propofol, but with a significantly lower incidence of respiratory depression (P < 0.05). This finding strongly supports remimazolam as a safer sedative agent (
In existing research and trials, the superiority of remimazolam has been preliminarily demonstrated. However, during the study period, certain adverse drug reactions were observed, including symptoms such as hypotension, respiratory depression, dizziness, and nausea. Additionally, reports of other related adverse events have emerged during clinical application. For example, multiple reports indicate that mixing remimazolam with Ringer’s solution may cause precipitation, with higher remimazolam concentrations and greater pH values increasing the likelihood of precipitation formation. Therefore, when combining the two, a low concentration of remimazolam should be used while increasing the infusion rate of Ringer’s solution to prevent precipitation (
Based on current research findings, as a novel benzodiazepine sedative, remimazolam has gained limited application in routine procedural sedation due to its rapid onset, swift metabolism, and lower risk of respiratory and circulatory depression. Its safety and efficacy in specific scenarios have been supported by some studies. However, unresolved issues and potential risks must also be acknowledged. First, the lack of long-term safety data represents a critical gap that cannot be overlooked. Existing clinical evidence primarily stems from studies involving short-to-medium-term use. There remains an insufficient body of evidence-based medical data regarding the safety of continuous administration beyond several weeks, potential dependence associated with long-term use, withdrawal symptoms, and effects on neurocognitive function. This uncertainty complicates its application in chronic disease sedation or scenarios requiring repeated sedation. Second, debates over its cost-effectiveness remain inadequately explored. For instance, compared to established, low-cost sedatives like propofol, whether remimazolam’s higher pricing can offset costs through reduced adverse reactions and shorter recovery times—thereby lowering overall healthcare expenditures—lacks robust support from large-scale, multicenter health economics studies. Additionally, regional disparities in accessibility may limit equitable realization of its clinical value. Currently, remimazolam remains unapproved in some countries and regions. Even in approved areas, variations in drug supply across different healthcare levels and health insurance reimbursement policies may limit its availability to only a small number of patients, hindering its adoption as a universally accessible sedation option. Finally, concerns regarding its use in specific populations and the associated learning curve require attention. For special populations such as elderly patients, those with hepatic or renal impairment, and obese patients, current dosage recommendations are largely derived from small-sample studies, resulting in significant individual variability. Clinicians must gradually optimize treatment regimens through accumulated experience, presenting a learning curve. Furthermore, safety data for populations like pregnant women and children remain severely inadequate, limiting the expansion of its applicable scope.
Overall, as a novel sedative, remimazolam demonstrates certain application potential in clinical sedation practices. However, current research evidence remains significantly limited. Overemphasizing its advantages while overlooking potential risks and unresolved issues may misguide clinical decision-making. Future efforts should include more high-quality long-term follow-up studies, health economics research, and population-specific drug studies to clarify its appropriate indications and risk-benefit ratio. Concurrently, optimizing drug supply policies and improving medical insurance reimbursement mechanisms are essential to narrow accessibility gaps. Only by adopting a more critical and neutral perspective on its clinical value can we promote the rational use of remimazolam, ultimately benefiting patients.
QW: Writing – original draft, Writing – review and editing. SB: Writing – review and editing.
The author(s) declared that this work was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
The author(s) declared that generative AI was not used in the creation of this manuscript.
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