(2E)-N-phenyl-N-[1-(2-phenylethyl)-4-piperidinyl]-2-butenamide
Recommendation (from TRS)
Substance identification
Flualprazolam (8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3- a][1,4]benzodiazepine) is a triazolo-benzodiazepine. Flualprazolam has been detected in seized samples of tablets and, more rarely, powder, blotters and liquid. It was the subject of a patent but has never been marketed as a pharmaceutical.
WHO review history
Flualprazolam has not been reviewed previously. A direct critical review was proposed on the basis of information brought to WHO’s attention that flualprazolam poses a risk to public health and society and has no therapeutic use recognized by any Party.
Similarity to known substances and effects on the central nervous system
Flualprazolam is an agonist at the benzodiazepine site of the gamma-aminobutyric acid (GABAA) receptor. Its pharmacological effects are similar to those of other benzodiazepines, such as alprazolam, which is currently controlled under the Convention on Psychotropic Substances of 1971.
User reports have indicated that flualprazolam depresses central nervous system function, with effects such as sedation, loss of memory and disinhibition, similar to other benzodiazepines.
Dependence potential
No studies on the dependence potential of flualprazolam in humans or animals were available. In view of its mechanism of action, however, flualprazolam would be expected to produce dependence similar to other benzodiazepines, particularly the closely related alprazolam.
Actual abuse and/or evidence of likelihood of abuse
No studies on the abuse potential of flualprazolam in humans or animals were available. Flualprazolam has a fast onset of action, which would suggest that it would have a high abuse liability, similar to that of alprazolam.
Users reported that flualprazolam reduces anxiety and causes sedation, suggesting that it has significant abuse potential.
A number of countries in various regions have reported detection of flualprazolam in fatal and non-fatal intoxications and in cases of impaired driving. Over 25 deaths occurred after confirmed exposure to flualprazolam.
Therapeutic usefulness
Flualprazolam is not known to have any therapeutic uses.
Recommendation
Flualprazolam (8-chloro-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3- a][1,4]benzodiazepine) is a benzodiazepine that is chemically similar to the benzodiazepines alprazolam and triazolam, which are listed under Schedule IV of the 1971 Convention on Psychotropic Substances. In common with other benzodiazepines, flualprazolam can produce a state of dependence as well as central nervous system depression. There is sufficient evidence that it is being abused and therefore constitutes a public health and social problem. It has no therapeutic use.
■ Recommendation: The Committee recommended that flualprazolam be added to Schedule IV of the 1971 Convention on Psychotropic Substances.