remimazolam + alcohol

Remimazolam + alcohol refers to the combination of the ultra-short-acting benzodiazepine **remimazolam** with **ethanol (alcohol)**. Remimazolam acts as a positive allosteric modulator at the gamma-aminobutyric acid type A receptor (**GABA_A receptor**), enhancing inhibitory neurotransmission, and is primarily used for procedural sedation and anesthesia. Alcohol is a central nervous system depressant that also potentiates GABA_A receptor activity. When co-administered, both substances may produce additive or synergistic CNS depressant effects. Unlike other benzodiazepines, remimazolam is metabolized by liver carboxylesterases (CES-1) rather than cytochrome P450 enzymes, but alcohol can inhibit CES-1 and potentially increase remimazolam plasma exposure. However, clinical evidence indicates that oral remimazolam has negligible bioavailability, and alcohol-induced increases in systemic exposure are minor. The combination can theoretically increase risk of sedation, amnesia, impaired motor function, and respiratory depression, as is the case with all benzodiazepine-alcohol combinations, but in trials with oral remimazolam such potentiation was minimal. Nonetheless, the combination has been investigated due to concerns over misuse in drug-facilitated assault.[1][3]