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Diazepam (Valium) (Indications & side effects (Chemical safety: Acute…

- - - - Different synthesis? 2 different routes?
        
        ROUTE 2 → Nordazepam + dimethyl sulfate (methylation); 2-Amino-5-chlorobenzophenone + dimethyl sulfate + ethyl glycinate hydrochloride (methylation/condensation); p-Chloroaniline + benzyl chloride + ethyl acetoacetate + dimethyl sulfate + ammonia (Sumitomo process)
        
        ROUTE 1 → Benzoyl chloride is reacted with para-chloroaniline in the presence of a zinc chloride catalyst. The resulting 2-amino-5-chlorobenzophenone is converted to the oxime with hydroxylamine and then cyclized to the chloromethylquinazoline-3- oxide by treatment with chloroacetyl chloride. When this is treated with alkali, ring enlargement occurs, giving 7-chloro-1,3-dihydro-5-phenyl-2H-1,4- benzodiazepin-2-one-4-oxide. Raney nickel reduction of the oxide followed by methylation with dimethyl sulfate gives diazepam.
- - - - Diazepam potentiates the inhibitory activities of gamma-aminobutyric acid (GABA) by binding to the GABA receptor, located in the limbic system and the hypothalamus. This increases the frequency of chloride channel opening, allowing the flow of chloride ions into the neuron and ultimately leading to membrane hyperpolarization and a decrease in neuronal excitability.
- - - - Phase I, II and III → I Human Pharmacology, II Therapeutic Exploratory, III Therapeutic Confirmatory
- - - - 3. Clinical development : :
        
        Regulatory approval
        
        Stages: 0,1,2,3,4.