Cinazepam (BD-798, sold under brand name Levana) is an atypical benzodiazepine derivative.[1] It produces pronounced hypnotic, sedative, and anxiolytic effects with minimal myorelaxantside effects.[2][3][4] In addition, unlike many other benzodiazepine and nonbenzodiazepine hypnotics such as diazepam, flunitrazepam, and zopiclone, cinazepam does not violate sleep architecture, and the continuity of slow-wave sleep and REM sleep are proportionally increased.[2][3][4] As such, cinazepam produces a sleep state close to physiological, and for that reason, may be advantageous compared to other, related drugs in the treatment of insomnia and other sleep disorders.[2]
Cinazepam has an order of magnitude lower affinity for the benzodiazepine receptor of the GABAA complex relative to other well-known hypnotic benzodiazepines such as nitrazepam and phenazepam.[2] Moreover, in mice, it is rapidly metabolized, with only 5% of the base compound remaining within 30 minutes of administration.[2] As such, cinazepam is considered to be a benzodiazepine prodrug; specifically, to 3-hydroxyphenazepam, as the main active metabolite.[2]
See also[]
Gidazepam
Cloxazolam
References[]
^Sleep Research. Brain Information Service/Brain Research Institute, University of California. 1997.
^ abMakan, S. Yu.; Boiko, I. A.; Smul’skii, S. P.; Andronati, S. A. (2007). "Effect of cinazepam administration on the ligand affinity of neuromediator system receptors in rat brain". Pharmaceutical Chemistry Journal. 41 (5): 249–252. doi:10.1007/s11094-007-0055-9. ISSN0091-150X. S2CID24532012.
^ abAndronati, S. A.; Makan, S. Yu.; Neshchadin, D. P.; Yakubovskaya, L. N.; Sava, V. M.; Andronati, K. S. (1998). "Bioaccessibility of cinazepam introduced as inclusion complex with β-cyclodextrin". Pharmaceutical Chemistry Journal. 32 (10): 513–515. doi:10.1007/BF02465736. ISSN0091-150X. S2CID26513288.