Benzodiazepines (BZD) including diazepam, lorazepam, flunitrazepam and midazolam bind allosterically (binding at a site other than the ligand’s active site) to specific receptors-GABAA receptor-in the central nervous system to enhance inhibitory effect of the neurotransmitter gamma-aminobutyric acid (GABA). The various benzodiazepines differ mainly in their kinetics, however some of the differences in effects can partly be accounted for by differences in activities of benzodiazepine receptor isoforms, benzodiazepine receptor type affinity, and location of receptor within the central nervous system.
The inhibition of the CNS by benzodiazepines has a significant clinical relevance in toxicology. Diazepam and lorazepam . . .
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