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Finally, note that the benzodiazepine core is a privileged scaffold, which has been used to derive drugs with diverse activity that is not limited to the GABA A modulatory action of the classical benzodiazepines, [60] such as devazepide and tifluadom, however these have not been included in the list below. 2,3-benzodiazepines such as tofisopam ...
Benzodiazepines such as nitrazepam are lipid-soluble and have a high cerebral uptake. [89] The time for nitrazepam to reach peak plasma concentrations following oral administration is about 2 hours (0.5 to 5 hours). The half-life of nitrazepam is between 16.5 and 48.3 hours. In young people, nitrazepam has a half-life of about 29 hours and a ...
Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with comorbid psychiatric disorders. [80] Because of their muscle relaxant action, benzodiazepines may cause respiratory depression in susceptible individuals.
Midazolam is a short-acting benzodiazepine in adults with an elimination half-life of 1.5–2.5 hours. [13] In the elderly, as well as young children and adolescents, the elimination half-life is longer. [44] [66] Midazolam is metabolised into an active metabolite alpha-hydroxymidazolam.
Flurazepam is a "classical" benzodiazepine; some other classical benzodiazepines include diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, bromazepam, and clorazepate. [16] Flurazepam generates an active metabolite, N-desalkylflurazepam, with a very long elimination half-life. [3]
Clonazepam, sold under the brand name Klonopin among others, is a benzodiazepine medication used to prevent and treat anxiety disorders, seizures, bipolar mania, agitation associated with psychosis, obsessive–compulsive disorder (OCD), and akathisia. [11]
Different benzodiazepines have different abuse potential; the more rapid the increase in the plasma level following ingestion, the greater the intoxicating effect and the more open to abuse the drug becomes. The speed of onset of action of a particular benzodiazepine correlates well with the 'popularity' of that drug for abuse.
[5] [4] [28] It has been shown to suppress cortisol levels. [29] Oxazepam is the most slowly absorbed and has the slowest onset of action of all the common benzodiazepines according to one British study. [30] Oxazepam is an active metabolite formed during the breakdown of diazepam, nordazepam, and certain similar drugs.