Ethylone

Alternative names
3,4-methylenedioxy-N-ethylcathinone; bk-MDEA; MEDEC
IUPAC Name

(RS)-1-(1,3-Benzodioxol-5-yl)-2-(ethylamino)propan-1-one

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

Recommendation (from TRS)

Substance identification
Chemically, ethylone is 1-(2H-1,3-benzodioxol-5-yl)-2-(ethylamino)propan-1- one. It is a chiral compound with isomers, and its hydrochloride salt can exist in two conformations (polymorphs) at the C–C bond linking the side chain to the aromatic ring.

Previous review
Ethylone has not previously been pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to the attention of WHO that ethylone is clandestinely manufactured, poses a serious risk to public health and society, and has no recognized therapeutic use by any Party.

Similarity to known substances and effects on the central nervous system
Ethylone can be considered a slight chemical modification of methylone (3,4-methylenedioxymethcathinone), which is included in Schedule II of the Convention on Psychotropic Substances of 1971. However, it would be likely to be inefficient to intentionally synthesize ethylone to convert it to methylone. Similar to cocaine-like drugs, ethylone has relatively nonselective monoamine uptake inhibition at dopamine, serotonin and norepinephrine transporters. It substitutes completely for the methamphetamine and cocaine discriminative stimuli in rats suggesting that it would be likely to produce their subjective effects. Reported clinical effects (often observed when accompanied by other drugs) include impaired driving, slurred speech, bloodshot watery eyes, dilated pupils, involuntary muscle movements and elevated pulse and blood pressure.

Dependence potential
No controlled studies in humans or laboratory animals regarding the potential physical dependence effects of ethylone have been reported.

Actual abuse and/or evidence of likelihood of abuse
Results of controlled laboratory studies in animals or humans characterizing the abuse potential of ethylone have not been reported. Seizures of ethylone, or its detection in biosamples, have been reported from several countries and regions. Within the first six months of 2015, ethylone had become the 12th most confiscated drug in the United States. Ethylone is aggressively marketed on the Internet and has been sold as a bath salt, plant food and cleaning product. Users report administering the drug via the oral, rectal, insufflation, sublingual and intravenous routes. Ethylone has been associated with deaths (more than eight reports). Several countries in different regions have imposed regulatory controls over ethylone.

Therapeutic usefulness
Ethylone was originally patented for its potential antidepressant and antiparkinsonian properties in 1995, but no currently approved medical applications exist for it.

Recommendation
The Committee considered that the degree of risk to public health and society associated with the abuse of ethylone (1-(2H-1,3-benzodioxol-5-yl)-2- (ethylamino)propan-1-one) is substantial. Therapeutic usefulness has not been recorded. It recognized that ethylone has similar abuse and similar ill-effects to substances in Schedule II of the Convention on Psychotropic Substances of 1971. The Committee considered that there is sufficient evidence that ethylone is being or is likely to be abused so as to constitute a public health and social problem warranting the placing of the substance under international control. As per the Guidance on the WHO review of psychoactive substances for international control (2), higher regard was accorded to the substantial public health risk than to the lack of therapeutic usefulness. The Committee recommended that ethylone be placed in Schedule II of the Convention on Psychotropic Substances of 1971.

ECDD Recommendation

Inclusion in Schedule II of the 1971 Convention on Psychotropic Substances