About Chlordiazepoxide Benzodiazepine derivative, Sedative /hypnotic, Antianxiety and skeletal muscle relaxant. Mechanism of Action of Chlordiazepoxide Chlordiazepoxide mainly acts on Limbic system and ascending reticular formation in the CNS. It binds to the BZD receptor. The binding will facilitates GABA mediated chloride channel opening and produce hyperpolarisation. This will increase the concentration of inhibitory neurotransmitter GABA and chloride ions in the CNS and decreases firing rate of neurons. This in turn alters normal excitatory functions of the body.