About Midazolam An ultra short-acting benzodiazepine derivative, Anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant,Sedative. Mechanism of Action of Midazolam Midazolam mainly acts on Limbic system and ascending reticular formation in the CNS and binds to the BZD receptor. The binding will facilitates GABA mediated chloride channel opening and produce hyperpolarisation. This will produce an increase in the concentration of the inhibitory neurotransmitter GABA and chloride ions and decreases firing rate of neuron. This in turn alters normal functions of the body. Midazolam is used as adjuncts in anaesthesia for anxiolysis, amnesia and sedation prior to induction of anaesthesia