Clorazepic acid

Clorazepic acid (clorazepate) is a water-soluble benzodiazepine with muscle-relaxant and anticonvulsant actions effective in the treatment of anxiety. Following administration, clorazepate is rapidly converted to nordiazepam (N-desmethyldiazepam), its active metabolite, before entering systemic circulation. Similar to other benzodiazepines, the active metabolite of clorazepate enhances the binding of gamma-aminobutyric acid (GABA) to the GABA type A (GABA-A) receptor, which promotes channel opening and neuronal hyperpolarization. The concomitant use of clorazepate and opioids may result in profound sedation, respiratory depression, coma, and death. Also, the use of clorazepate exposes users to users to the risks of abuse, misuse, and addiction, and its continued use may lead to significant physical dependence. In September 2020, a black box warning describing these risks was included on the product label of benzodiazepines as per FDA regulation. Clorazepate and its active metabolite, nordiazepam, are present in breast milk.