Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties.
藥理
Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing inhibitory effects of GABA.
藥動學
Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration. Protein binding: 70%. Metabolism: Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes). One of the main metabolites is 3-hydroxybromazepam. It is pharmacologically active and the half life is similar to that of the parent compound. Route of elimination: Urine (69%), as metabolites. Half life:
10-20 hours.