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By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide. [2] [3]
Librium, based on the R0 6-690 compound discovered by Sternbach in 1956, was approved for use in 1960. In 1963, its improved version, Valium, was released and became astonishingly popular: between 1969 and 1982, it was the most prescribed drug in America, with over 2.3 billion doses sold in its peak year of 1978.
In ancient Greece, pills were known as katapotia ("something to be swallowed"). Pliny the Elder, who lived from 23–79 CE, first gave a name to what we now call pills, calling them pilula. [2] Pliny also wrote Naturalis Historia a collection of 38 books and the first pharmacopoea.
It was the first benzodiazepine to be synthesized and the discovery of chlordiazepoxide was by pure chance. [6] Chlordiazepoxide and other benzodiazepines were initially accepted with widespread public approval, but were followed with widespread public disapproval and recommendations for more restrictive medical guidelines for its use. [7]
Flunitrazepam, sold under the brand name Rohypnol among others, [3] is a benzodiazepine used to treat severe insomnia and assist with anesthesia. [4] As with other hypnotics, flunitrazepam has been advised to be prescribed only for short-term use or by those with chronic insomnia on an occasional basis.
Librium (chlordiazepoxide) – a benzodiazepine used to treat acute alcohol withdrawal; Lithobid, Eskalith – a mood stabilizer; Loxam (escitalopram) – an antidepressant of the SSRI class; Lunesta (eszopiclone) – a non-benzodiazepine hypnotic; Luvox (fluvoxamine) – an antidepressant of the SSRI class
Bromazepam is a "classical" benzodiazepine; other classical benzodiazepines include: diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, flurazepam, and clorazepate. [16] Its molecular structure is composed of a diazepine connected to a benzene ring and a pyridine ring, the benzene ring having a single nitrogen atom that replaces one of the ...
The structure-activity relationship of the drug class has been explored to a reasonable extent. The optimal substitution pattern is fairly tightly defined (i.e. N,N-diethyl on the amine nitrogen, 4-ethoxy on the benzyl ring and 5-nitro on the benzimidazole ring), but even derivatives incorporating only some of these features are still potent opioids.