Pharmacodynamics effects were observed shortly after administration and returned to baseline generally within 4 hours. Pharmacodynamics assessments included Standardford Sleepiness Scale (SSS) and Observer’s Assessment of Alertness/Sedation Scale sum score to assess sedation, and Digit-Symbol Substitution Test (DSST) percent correct and trial completion rate to assess psychomotor performance. Following a single 2.5 or 5 mg dose of intranasal midazolam, pharmacodynamic effects were observed shortly after administration and returned to baseline generally within 4 hours. The pharmacodynamics effects of intranasal midazolam was assessed in a single dose (2.5 mg and 5 mg), phase-1, randomized, double-blind, 2-way crossover study (≥4 day washout period) in generally healthy geriatric (≥65 years n=18) and non-geriatric (18-40 years n=12) participants. Midazolam dissolves in water at a low pH, but at physiologic pH it becomes lipophilic, allowing the medication to cross the blood-brain-barrier. Midazolam is a small molecular weight of 325.8 Da allows for easy permeation of nasal mucosa. Increased chloride influx leads to hyperpolarization of neurons, which results in an inhibitory effect. This binding increases the permeability of the central pore of the receptor to chloride ion into the neuron. Midazolam acts as an agonist at the benzodiazepine receptors by forming a component of the midazolam-GABA receptor-chloride ionophore complex. Benzodiazepines appear to intensify the physiological inhibitory mechanisms mediated by gamma-aminobutyric acid (GABA), the most common inhibitory neurotransmitter in the brain. The mechanism of action of the benzodiazepines is under continuous investigation. It has anxiolytic, hypnotic, anticonvulsant, muscle relaxant, and anterograde amnestic effects, which are characteristic of benzodiazepines. Midazolam is a short-acting, benzodiazepine, central nervous system (CNS) depressant. Benzalkonium Chloride IP (as preservative)……….0.01% w/vĪqueous intranasal spray Pharmacology Pharmacodynamics
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