Flumazenil or Anexate is an imidazo benzodiazepine that binds competitively to BDZ receptors and antagonizes many of the actions of benzodiazepines.
Flumazenil is a benzodiazepine antagonist.
It does not block the pharmacologic effects of GABA or all GABA mimetic but it specifically antagonizes the actions of benzodiazepines. Given alone, it has minimal effect on the CNS.
The drug can cause withdrawal syndrome in patients dependent on BDZ. Clinically, it can rapidly reverse the effects of benzodiazepines.
Flumazenil infusion can facilitate the return of consciousness within 5-15 minutes in patients with benzodiazepine poisoning.
Given orally, it is rapidly absorbed and has a high hepatic clearance. It is metabolized in the liver and little is excreted unchanged.
It is given IV initially in the dose of 0.2 mg over 15 seconds, and then repeated in the dose of 0.1mg every minute to a total dose of not more than 1 mg. It is also given by IV infusion. The duration of action of a single dose is 30-60 minutes.
Flumazenil Therapeutics uses
- In benzodiazepine poisoning, and
- For reversal of sedative effect of a benzodiazepine administered during general anesthesia, a diagnostic or therapeutic procedure.
- It is contraindicated in patient with raised intracranial pressure as after severe head injury.