Complete or partial reversal of sedative effects of benzodiazepines where general anesthesia induced or maintained with benzodiazepines, where sedation produced with benzodiazepines for diagnostic or therapeutic procedures, and for the management of benzodiazepine overdose.
Reversal of Conscious Sedation or in General Anesthesia
Adults:IV 0.2 mg over 15 sec. If desired level of consciousness is not achieved in 45 sec, additional 0.2 mg doses can be administered at 60 sec intervals (max, 1 mg). In event of resedation, repeat doses (0.2 mg/min to max 1 mg) at 20 min intervals as needed (max, 3 mg/h).
Management of Suspected Benzodiazepine Overdose
Adults:IV 0.2 mg over 30 sec. If desired level of consciousness is not achieved in 30 sec, an additional dose of 0.3 mg over 30 sec can be administered. Further doses of 0.5 mg over 30 sec can be administered at 1 min intervals as needed (max, 3 mg).
Hypersensitivity to flumazenil or benzodiazepines; in patients given benzodiazepines for control of a potentially life-threatening condition (eg, status epilepticus); in patients showing signs of serious cyclic antidepressant overdose.
Absorption: Mean Cmax is 24 ng/mL (range, 11 to 43 ng/mL); mean AUC was 15 ng•h/mL (range, 10 to 22 ng•h/mL).
Distribution: Initial distribution t ½ is 7 to 15 min. VDinitial is 0.5 L/kg; Vdss is 0.l77 to 1.60 L/kg. Protein binding is about 50%.
Metabolism: Primarily hepatically metabolized and dependent on hepatic blood flow (highly extracted).
Excretion: Terminal t ½ is 41 to 79 min. Total Cl is 0.7 to 1.3 L/h/kg (increases by 50% during ingestion of food). Less than 1% is excreted unchanged in the urine; 90% to 95% is excreted in urine and 5% to 10% in feces.