Flumazenil

  • IUPAC: 8-fluoro -5-methyl -6-oxo -5, 6 - dihydro -4H- imidazo [ 1,5-a ] [1,4 ] benzodiazepine -3-carboxylate
  • Latin: Flumazenilum

V03AB25

White to off- white crystalline powder

Antidote benzodiazepine antagonist

Competitive antagonist at the GABA A receptor

201-203 ° C

  • Water: 128 mg · l-1 (25 ° C)
  • Slightly soluble in dichloromethane, slightly soluble in methanol

143 mg · kg -1 ( LD50, mouse, i.v.)

Template: Infobox chemical / molecular formula search available

Flumazenil is an imidazobenzodiazepine derivative and a benzodiazepine antagonist. It is used as an antidote to drugs of the benzodiazepine group, as well as other acting at the benzodiazepine binding site of non- Benzodiazepinagonisten, such as zopiclone, zolpidem and zaleplon and raises all the effects thereof on.

Pharmacodynamics

Flumazenil acts as a reversible, competitive antagonist at the benzodiazepine site of the GABAA receptor.

Pharmacokinetics

It must be given intravenously, since it is largely eliminated by the oral administration of the liver. The effect is a rapid (two minutes), but holds only relatively short ( two hours). Therefore, with longer-acting benzodiazepines the risk of recoil ( rebound ), the reinstate -setting effect after this time.

Indications

  • Lifting a Benzodiazepin-Sedierung/Überdosierung
  • Termination of a benzodiazepine anesthesia

Recent research shows that flumazenil could be effective in the treatment of primary hypersomnia

Side effects and contraindications

In addition to headaches, blurred vision, nausea and vomiting occur anxiety and restlessness. In benzodiazepine addicts can cause an acute withdrawal syndrome.

Flumazenil is contraindicated in patients known to have hypersensitivity to benzodiazepines or to treat potentially life-threatening conditions have obtained ( control of intracranial pressure after severe traumatic brain injury or status epilepticus eg ) benzodiazepines. Although there are no controlled studies in pregnant women available, but animal studies have demonstrated no teratogenic effects.

In high doses it can occur in people with a benzodiazepine to trigger withdrawal symptoms which manifest themselves about as anxiety or tremor.

Chemical and physical properties

Flumazenil is sparingly soluble in water but readily soluble in dichloromethane. Different polymorphic forms are not yet known.

64196
de