BENZODIAZEPINE ANTAGONISTS: FLUMAZENIL

Question 1

What is Flumazenil?

Answer 1

is one of** several 1,4-benzodiazepine derivatives** with a
**high affinity for the benzodiazepine **binding site on the GABA A receptor that act as competitive antagonists.

It blocks many of the actions of benzodiazepines, zolpidem, zaleplon, and eszopiclone.

Question 2

Flumazenil does not antagonize the central nervous system effects of other sedative-hypnotics,______________

Flumazenil is approved for use in reversing the central nervous
system depressant effects of benzodiazepine overdose and to hasten recovery following use of these drugs in anesthetic and diagnostic procedures.

Answer 2

ethanol, opioids, or general anesthetics.

Question 3

Although the drug reverses the sedative effects
of benzodiazepines, antagonism of benzodiazepine-induced respiratory depression is less predictable.

When given intravenously,
flumazenil** __________________**

Answer 3

acts rapidly but has a short half-life (0.7–1.3 hours) due to** rapid hepatic clearance.**

Question 4

Because all ___________have a
longer duration of action than flumazenil, sedation commonly
recurs, requiring repeated administration of the antagonist.

Answer 4

benzodiazepines

Question 5

Adverse effects of flumazenil include _____________.

Answer 5

• agitation,
• confusion,
• dizziness,
• and nausea

Question 6

Flumazenil may cause a severe precipitated
abstinence syndrome in patients __________

Answer 6

developed marked
benzodiazepine dependence

Question 7

In patients who have ingested benzodiazepines
with tricyclic antidepressants, seizures and cardiac
arrhythmiasmay followflumazenil administration.