Drug intelligence / Profile preview

midazolam + remifentanil

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Intravenous
01

Overview

Midazolam + remifentanil is a combination of two intravenous drugs commonly used for procedural sedation and analgesia, particularly during brief or painful medical procedures. Midazolam is a short-acting benzodiazepine with sedative, anxiolytic, amnesic, muscle relaxant, and anticonvulsant properties. It acts by enhancing the effect of gamma-aminobutyric acid (GABA) at the GABA-A receptor in the central nervous system, leading to CNS depression[4][8][9]. Remifentanil is an ultra-short acting synthetic opioid analgesic that acts primarily as a mu-opioid receptor agonist to provide potent pain relief[10]. The combination leverages the rapid onset and offset of both agents to achieve deep sedation and effective analgesia with quick recovery times. However, this regimen carries significant risk for respiratory depression and requires close monitoring in controlled settings[2][6].

02

Targets

GABA-A receptor α1β2γ2 (GABA_A receptor α1β2γ2 – N-methyllaurotetanine)MOR (Mu opioid receptor)

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