Flumazenil (Ro 15-1788) proved to be a very efficacious competitive antagonist 
of benzodiazepines that reliably counteracts their pharmacological actions 
within 1-2 min as could be demonstrated in clinical and EEG studies. In general, 
a total dose of 0.3-0.8 mg will be sufficient in clinical practice, avoiding 
side effects like nausea, tremor, sweating, or transient anxiety that could be 
observed when higher dosages were administered. Its therapeutic range is very 
high as could be demonstrated in experimental animal in which up to 8.000-fold 
the clinical dose was administered. The total volume of distribution (Vdes) 
amounts to nearly 1.000 ml/kg BW and the total clearance exceeds 1.200 ml/min, 
resulting in a biological half-life of less than 60 min. According to the 
benzodiazepine dosage and the rapid plasma concentration decline of flumazenil, 
in some cases a resedation could be observed. Hence, a careful observation of 
the antagonised patient on the ward is mandatory for 1.5-2 h, even if at first 
sight the antagonization seemed successful and the patient fully awake and 
cooperative. In anaesthesia, indications to administer flumazenil are adverse 
drug reactions and prolonged recovery after adequate benzodiazepine dosage. In 
intensive care medicine, the antagonist may be used in the treatment of 
benzodiazepine overdose as well as in the differential diagnosis of a coma of 
unknown origin. Additionally, the antagonist may be administered to interrupt 
benzodiazepine sedation e.g. for neurological examination.