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Flumazenil (FMZ), a benzodiazepine receptor antagonist, is used to reverse the central effects of benzodiazepines (ex. sedation or intoxication with over dose). It inhibits the effects of benzodiazepine receptor agonists by competing with these drugs. The purpose of this study was to calculate the benzodiazepine receptor occupancy of FMZ using the pharmacokinetic parameters reported in the literature, and to examine the relationship between the receptor occupancy and the pharmacological effect of FMZ. Recovery of consciousness in the patients sedated with intravenous flunitrazepam was used to indicate the pharmacological effect of FMZ. In contrast with the plasma concentration of FMZ which declines rapidly after intravenous administration, the effect (recovery of consciousness) appeared relatively slowly in about 5 to 10 minutes. Therefore, there was no correlation between plasma concentration and the effect of FMZ. On the other hand, the receptor occupancy of FMZ, calculated considering the association/dissociation process at the receptor, correlated well with the effect, giving the similar pattern for various doses of FMZ. These findings indicate that the receptor occupancy is a suitable indicator of the pharmacological effects of benzodiazepine antagonists and that receptor occupancy by antagonist of more than 30% was required for all the patients to become conscious with FMZ.

Relationship between Reversal of Flunitrazepam-Induced Sedation by Flumazenil and Benzodiazepine Receptor Occupancy.