NCIt definition : A member of the benzodiazepines and a long-acting depressor of the central nervous
system (CNS) with sedative and hypnotic effects. Flurazepam binds to a specific site
on the benzodiazepine-gamma-aminobutyric acid (GABA)-A-chloride ionophore receptor
complex located on the neuronal membrane. Binding causes an allosteric modification
of the receptor thereby enhancing the affinity of GABA to the receptor leading to
an increase in the frequency of chloride-channel opening events, which leads to an
increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the
action potential, and a decrease in neuronal excitability. By modulating binding of
the GABA inhibitory neurotransmitter to GABA-A receptors in the ascending reticular
activating system, flurazepam blocks arousal of the cortical and limbic system, thereby
exerting its sedative and hypnotic effect.;