Trial reportDrugs in R&D2020
Remimazolam Has Low Oral Bioavailability and No Potential for Misuse in Drug-Facilitated Sexual Assaults, with or Without Alcohol: Results from Two Randomised Clinical Trials.
Trial report in Drugs in R&D, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to 2 registered trials, which are not on this map. Cited by 17 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
A Phase 1 Study to Determine the Single-dose Pharmacodynamics, Pharmacokinetics, and Safety and Tolerability of Remimazolam Following Oral Administration With and Without Alcohol in Healthy Female Subjects
A Randomized, Open-label, Single-dose, 2-way Crossover Study to Compare the Relative Bioavailability of Orally Administered Remimazolam to an Intravenous Formulation in Healthy Volunteers
Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.
- Efficacy and Safety of Remimazolam in Endoscopic Sedation-A Systematic Review and Meta-Analysis.Frontiers in medicine · 2021Pooled it
- Pharmacokinetics and pharmacodynamics of intranasal remimazolam-a randomized controlled clinical trial.European journal of clinical pharmacology · 2020Trial
- Review of clinical advances in the procedural sedation application of remimazolam.Frontiers in pharmacology · 2026Review
- Optimal Dosing Strategies for Remimazolam Across Diverse Patient Populations: A Clinical Narrative Review.Drug design, development and therapy · 2026Review
- Clinical Pharmacokinetics and Pharmacodynamics of Remimazolam.Clinical pharmacokinetics · 2025Review
- Optimizing Pediatric Sedation: Evaluating Remimazolam and Dexmedetomidine for Safety and Efficacy in Clinical Practice.Paediatric drugs · 2025Review
- Transfer of Intravenous Remimazolam into Milk of Lactating Sheep and Uptake by Breast-fed Lambs.Current drug metabolism · 2025Article
- [Remimazolam-Update on basic pharmacologic principles and clinical potential].Die Anaesthesiologie · 2024Review
- Effective dose of intranasal remimazolam for preoperative sedation in preschool children: a dose-finding study using Dixon's up-and-down method.Frontiers in pharmacology · 2024Article
- Clinical Application and Research Progress of Remimazolam for Pediatric Patients.Drug design, development and therapy · 2024Review
- Considerations for Satisfactory Sedation during Dental Implant Surgery.Journal of personalized medicine · 2023Review
- Review
- Article
- Remimazolam: A Review in Procedural Sedation.Drugs · 2021Review
- Emerging Approaches in Intravenous Moderate and Deep Sedation.Journal of clinical medicine · 2021Review
- A comprehensive review of remimazolam for sedation.Health psychology research · 2021Review
- Remimazolam: Non-Clinical and Clinical Profile of a New Sedative/Anesthetic Agent.Frontiers in pharmacology · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesRemimazolam is a new ultra-short-acting benzodiazepine currently being developed for intravenous use in procedural sedation, general anaesthesia, and intensive care unit sedation. Benzodiazepines represent a drug class associated with drug-facilitated sexual assaults, especially in combination with alcohol. Two clinical trials were designed to evaluate the oral bioavailability and pharmacokinetics/pharmacodynamics of remimazolam and to assess the potential for remimazolam misuse in drug-facilitated sexual assaults via oral ingestion.
methodsTrial 1 was conducted in 14 healthy volunteers to evaluate the oral bioavailability of remimazolam. Part 1 of trial 2 was conducted in 21 healthy female volunteers to find the minimal biologically active dose of oral remimazolam. Part 2 of trial 2 was conducted in 11 healthy female volunteers to evaluate the pharmacokinetics/pharmacodynamics of oral remimazolam in combination with alcohol.
resultsRemimazolam undergoes rapid and extensive first-pass metabolism upon oral administration. The oral bioavailability of remimazolam was negligible (2.2% based on total systemic exposure and 1.2% based on maximum plasma concentration). Plasma clearance of both remimazolam and its metabolite was fast (elimination half-life 20‒40 min and 1.75‒2 h, respectively). Alcohol did not appear to inhibit the rapid first-pass metabolism of remimazolam. No clear sedative effects were observed for remimazolam without alcohol. Significant sedation was observed in one of ten subjects after remimazolam 360 mg (18 drug product vials) + 40% v/v alcohol.
conclusionThe oral bioavailability of remimazolam is negligible, which-together with its distinct bitter taste-suggests no meaningful potential for misuse in drug-facilitated sexual assaults via oral ingestion, with or without alcohol. CLINICAL TRIAL REGISTRATION NUMBERS: Trial 1 (NCT04113564) and trial 2 (NCT04113343) both retrospectively registered on 2 October 2019.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.