Flumazenil

WHAT IS IT?

Flumazenil is a GABA antagonist/benzodiazepine antagonist. It is a competitive inhibitor of the benzodiazepine binding site on the GABA receptor.

Flumazenil binds the GABA receptor at the same location as benzodiazepines and Zolipedem (source)
Flumazenil binds the GABA receptor at the same location as benzodiazepines and Zolpidem (source)
WHEN DO WE USE IT?

Benzodiazepine overdose: given its activity this medication can help reverse the symptoms of benzodiazepine overdose.

Reversal of Zolpidem: given the binding site of Zolpidem, Flumazenil can be used to reverse its signaling effects.

WHEN DO WE AVOID USING IT?

Barbiturate overdose: barbiturates bind at a different site on the GABA receptor, so Flumazenil will not help with barbiturate overdose.

HOW IS IT ADMINISTERED?

IV administration

Source
Source
WHAT ARE THE SIDE EFFECTS/TOXICITY?

Seizures: blocking GABA receptors can lead to over-excitation and seizures in some patients.

FURTHER READING

DynaMed

UpToDate

 

Page Updated: 08.14.2016