Benzodiazepine Poisoning



  • Potentiates the activity of γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter, by binding to its own specific site
  • Also facilitates GABA binding to its site
  • Results in chloride influx, membrane hyperpolarization, and inhibition of cellular excitation:
    • Benzodiazepines (BZDs) increase the frequency of chloride channel opening
    • Depresses spinal reflexes and reticular activating system
  • Rapidly absorbed from GI tract:
    • Highly protein bound
    • Large Vd
    • Most have hepatic metabolism, some have active metabolites
    • Duration of action is inversely proportional to lipophilicity with highly lipophilic drugs penetrating the CNS more rapidly
    • Duration of diazepam > lorazepam > midazolam
    • Synergistic with other sedative–hypnotic medications (e.g., ethanol, barbiturates, propofol)

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