The efficacy of midazolam (0.071 +/- 0.006 microgram/kg) inactivation by flumazenil, a direct antagonist of benzodiazepines, was assessed in 20 patients during local and regional anesthesia. The hemodynamic values were assessed and a complex of psychological tests used. A single intravenous injection of flumazenil in a dose of 0.2 mg (2.8 +/- 0.41 micrograms/kg) resulted in a smooth an reliable arrest of benzodiazepine effect and effective repair of the main psychomotor reactions. Reversion of benzodiazepine effect is possible after an hour, which may require repeated injection of flumazenil.