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Drug Profile

Induction and maintenance of procedural sedation in adults: focus on remimazolam injection

, &
Pages 411-426 | Received 28 Dec 2020, Accepted 08 Mar 2021, Published online: 17 Mar 2021
 

ABSTRACT

Introduction: Procedural sedation (PS) is a humane way to help patients get through painful medical procedures by the administration of sedative drugs combined with analgesics. However, each of the currently used medications has certain shortcomings, urging the search for a new drug. Remimazolam, a novel benzodiazepine, is an ultra-short-acting hypnotic agent invented out of the ‘soft drug’ development.

Areas covered: This presented review provides an overview of the drugs used in clinical practice for the induction and maintenance of procedural sedation in adults, focusing on the newly investigated benzodiazepine remimazolam. Literature search was conducted using the MEDLINE and ClinicalTrial.gov databases from January 2007 to December 2020.

Expert opinion: Based on the reported clinical trials so far, remimazolam has demonstrated its effectiveness and safety with promising properties including rapid onset, short duration of action, predictable and consistent recovery profile, metabolism almost unaffected by liver or renal function, with non or minimal cardiorespiratory depression, and availability with a reversal drug. With marketing approval received recently, remimazolam is expected to have a place in the practice for procedural sedation in the near future if its efficacy and safety are further confirmed by more clinical trials and post-market analyses.

Article highlights

  • Each of the currently used medications for procedural sedation has certain shortcomings, urging the search for a new drug.

  • Remimazolam is a novel ultra-short-acting hypnotic agent invented out of the ‘soft drug’ development.

  • The essential improvement in the chemical structure of remimazolam is the introduction of carboxylic ester side, which permits rapid hydrolysis by ubiquitous esterases to an inactive metabolite.

  • The remarkable advantages of remimazolam include its ultra-short duration of action, minimal accumulation and residual effects with prolonged infusion, low risk for cardiorespiratory depression, and the capability of fully reversal by flumazenil.

  • Remimazolam has demonstrated the effectiveness and safety as a promising sedative for procedural sedation in colonoscopy, upper gastrointestinal endoscopy, and bronchoscopy with encouraging results from existing phase I, II, & III clinical trials.

  • Remimazolam has received marketing approval for procedural sedation in the United States and in China. More data from post-market clinical investigations and cost-benefit analyses are required for further evaluation.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

One reviewer has declared being a consultant and speaker for Acacia pharma. Other peer reviewers on this manuscript have no other relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.

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