Cyclopropylfentanyl

IUPAC Name

1-(4-cyanobutyl)-N-(1-methyl-1-phenylethyl)-1H-indazole-3-carboxamide

Year(s) and type of review / ECDD meetings
Drug Class

Recommendation (from TRS)

Substance identification
Cyclopropylfentanyl ((N-phenyl-N-1-(2-phenylethyl)-4-piperidyl) cyclopropan- ecarboxamide) is a synthetic analogue of the opioid fentanyl. Samples obtained from seizures and from other sources suggest that cyclopropylfentanyl is availa- ble in the form of powders, liquids and tablets.

WHO review history
Cyclopropylfentanyl has not been previously pre-reviewed or critically reviewed by the WHO ECDD. A critical review was proposed based on information brought to WHO’s attention that cyclopropylfentanyl poses a serious risk to public health and has no recognized therapeutic use.

Similarity to known substances and effects on the central nervous system
Cyclopropylfentanyl has a higher affinity to the μ-opioid receptor than to the δ- and κ-opioid receptors. There is no further information on the actions and effects of cyclopropylfentanyl from controlled studies. Based on its role in numerous deaths (see below), it is reasonable to assume that cyclopropylfentanyl acts as a μ-opioid receptor agonist similar to morphine and fentanyl.

Dependence potential
No preclinical or clinical studies have been published in the scientific literature concerning dependence on cyclopropylfentanyl. However, based on its mechanism of action, cyclopropylfentanyl would be expected to produce dependence similar to other opioid drugs.

Actual abuse and/or evidence of likelihood of abuse
Numerous seizures of cyclopropylfentanyl have been reported from different regions. In some countries, this substance has been among the most common fentanyl analogues detected in postmortem samples. In almost all of these cases, cyclopropylfentanyl was determined to have either caused or contributed to death, even in the presence of other substances.

Therapeutic usefulness
Cyclopropylfentanyl is not known to have any therapeutic use.

Recommendation
The available evidence indicates that cyclopropylfentanyl has opioid actions and effects. It has been extensively trafficked and has been administered by several different routes. Its use has been associated with a large number of documented deaths, in most of which it was found to be the principal cause of death. Cyclopropylfentanyl has no known therapeutic use and has been associated with substantial harm.

■■ Recommendation: The Committee recommended that cyclopro- pylfentanyl (N-phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]cyclopro- panecarboxamide) be added to Schedule I of the 1961 Single Convention on Narcotic Drugs.

ECDD Recommendation

Inclusion in Schedule I of the 1961 Convention on Narcotic Drugs