Products
Flumazenil is commercially available as a solution for injection (Anexate, generics). It was developed at Roche and has been approved in many countries since 1986.
Structure and properties
Flumazenil (C15H14FN3O3, Mr = 303.3 g/mol) exists as a white crystalline powder that is very sparingly soluble in water. It has a comparable structure to other benzodiazepines and is an imidazole derivative.
Effects
Flumazenil (ATC V03AB25) abolishes the central nervous system effects of benzodiazepines. The effects are due to competitive antagonism at the benzodiazepine receptor and occur rapidly, within minutes.
Indications
To abolish the effects of benzodiazepines in anesthesia and critical care, for example, to induce anesthesia or sedation, in cases of poisoning, overdose, and as a diagnostic measure for unconsciousness. Flumazenil is also used for Z-drugs.
Dosage
According to the SmPC. The drug is administered intravenously.
Contraindications
- Hypersensitivity
- It should not be administered if the effect of benzodiazepines is desired in life-threatening conditions.
Full precautions can be found in the drug label.
Interactions
The effects of substances related to the benzodiazepines that bind to the same receptors may also be abolished (eg, zopiclone, zaleplon). Particular caution should be exercised in cases of mixed intoxications with tri- or tetracyclic antidepressants.
Adverse effects
The most common possible adverse effects include drowsiness, injection site pain, sweating, vasodilatation, flushing, headache, visual disturbances, psychiatric disturbances, sensory disturbances, fatigue, nausea, and vomiting.
