Clinical Information

Diazepam, a benzodiazepine derivative, is an anxiolytic agent that reduces neuronal depolarization resulting in decreased action potentials. It enhances the action of gamma-aminobutyric acid (GABA) by tightly binding to A-type GABA receptors, thus opening the membrane channels, and allowing the entry of chloride ions. It is also used as a muscle relaxant, procedural sedation agent, and sedative-hypnotic agent to treat withdrawal states (ie, ethanol), along with other conditions (seizures).

Diazepam is metabolized to several metabolites in the liver, including temazepam, oxazepam, and nordiazepam (desmethyldiazepam), and the clearance of the drug is reduced considerably in older individuals and in patients with hepatic disease.

Therapeutic assessment typically includes measurement of both the parent drug (diazepam) and the active metabolite (nordiazepam).