Diazepam is a benzodiazepine derivative identified chemically as 7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. It is a colorless crystalline compound, insoluble in water and has a molecular weight of 284.75. Diazepam is a benzodiazepine with CNS depressant properties and a somewhat flatter dose-response slope than the sedative-hypnotic drugs. In laboratory animals, it produces, in varying doses, taming, disinhibitory, sedative, anticonvulsant, muscle relaxant, ataxic and hypnotic effects.
Diazepam is a 1,4-benzodiazepine, which binds with high affinity to the GABA A receptor in the brain to reduce arousal and to affect emotions. Diazepam’s action causes an increase in affinity of the major inhibitory neurotransmitter, GABA. GABA binds mainly to the a subunit while diazepam binds to the b subunit. The g subunit is also essential for modulation of chloride transport by benzodiazepines. Diazepam increases chloride transport through ion-channels and ultimately reduces the arousal of the cortical and limbic systems in the CNS. Diazepam depresses the electrical after-discharge in the amygdala and hippocampus regions of the limbic system that affect emotions.
Diazepam is used for the short-term relief of symptoms related to anxiety disorders. Diazepam is also used for the treatment of agitation, tremors, delirium, seizures, and hallucinations as a result of alcohol withdrawal. Diazepam is also used for relief of muscle spasms in certain neurological diseases. Diazepam is used to abort active seizures and can be combined with other drugs in treating severe recurrent seizures.