Bromazepam
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Mechanism of action
Bromazepam binds to the GABA-A receptor producing a conformational change and potentiating its inhibitory effects. Other neurotransmitters are not influenced.
Pharmacodynamics
Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. It does not possess any antidepressant qualities. Bromazepam, like other benzodiazepines, presents a risk of abuse, misuse, and dependence. According to many psychiatric experts, Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action.
Pharmacokinetics
Half-life
10-20 hours
Absorption
Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.
Urine (69%), as metabolites
1.56 L/kg
0.82 mL/min/kg.
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.
Bromazepam has known human metabolites that include 3-Hydroxybromazepam.
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
Protein binding
70%
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.