pinazepam

Pinazepam is a benzodiazepine derivative used primarily for the treatment of anxiety and, in some cases, severe insomnia. It acts as an anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant. Mechanistically, pinazepam enhances the inhibitory effects of gamma-aminobutyric acid (GABA) at the GABA-A receptor by binding to a specific site on the receptor complex. This increases chloride influx into neurons, reducing neuronal excitability and producing calming effects on the central nervous system[2][3][5]. Unlike many other benzodiazepines, pinazepam is noted for its limited hypnotic and motor impairment properties at therapeutic doses; it is considered more suitable for daytime use due to minimal impact on intellectual or psychomotor function[3]. After oral administration it is rapidly absorbed and metabolized mainly to N-desmethyldiazepam (nordazepam) and oxazepam[3]. Pinazepam has a longer elimination half-life in elderly patients. Pinazepam is classified as a Schedule IV controlled substance in several jurisdictions due to its potential for dependence with prolonged use[1][6]. Its unique propargyl group at the N1 position distinguishes it structurally from other benzodiazepines[3][7].

Brand names

DomarDuna

Other names

pinazepamPinazepam [INN]52463-83-9