Cloxazolam

Cloxazolam (marketed under brand name Sepazon, Olcadil (Brazil, Portugal and Spain), Akton (Belgium), Lubalix (Switzerland) is a drug which is a benzodiazepine derivative. Cloxazolam is metabolised into the active metabolite chlordesmethyldiazepam (delorazepam). It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.

Indications
Cloxazolam's main use is as an anti-anxiety drug.

Side effects
An increased heart rate may occur as an adverse effect of cloxazolam.

Pharmacology
The pharmacological effects of cloxazolam are a result of mainly its active metabolites, thus cloxazolam is a prodrug. The main site of action of cloxazolam and its active metabolites are the benzodiazepine receptor.

The pharmacological actions of benzodiazepines at the GABAa receptor are similar to those of neurosteroids. Neuroactive steroids are positive allosteric modulators of the GABAa receptor, enhancing GABA function and in turn have effects on mood and other functions. Many benzodiazepines (diazepam, medazepam, estazolam, temazepam, flunitrazepam and nitrazepam) potently inhibit the enzymes involved in the metabolism of neurosteroids. The tetrahydroxazole ring that cloxazolam and oxazolam have decreases the inhibitory potency of benzodiazepines on neurosteroids. Thus there could be subtle differences between cloxazolam and other benzodiazepines. However, because the parent prodrugs of cloxazolam and oxazolam were tested rather than the active metabolites, this is purely speculative.