Alpha-methylfentanyl

Current Scheduling Status
Schedule I and Schedule IV of the 1961 Convention on Narcotic Drugs
Year(s) and type of review / ECDD meetings
Drug Class

Recommendation (from TRS)

Substance identification
Alpha- -methylfentanyl (CAS 79704-88-4); chemical . name: (1) CAS: N-[I-(1-methyl-2-phenylethyl)-4-piperidinyl]-N-phenylpropanamide; (2) IUFA: N-(1-(α-methyl-β-phenyl)-ethyl-4 piperidyl-propionanilide; is also known as ‘China white’ or ‘synthetic heroin’.

Similarity to known substances and effects on the CNS
Alpha-methylfentanyl has been classified pharmacologically as an agonist of mu-type opioid receptors with a profile similar to that of fentanyl. As a mu-type opioid agonist it

possesses analgesic activity and produces morphine-like euphoric effects. Its analgesic potency is three times that of fentanyl and 900 times that of morphine. Its analgesic effect has a rapid onset and a short duration, but its respiratory depressant effect may last longer. The effects of alpha-methylfentanyl on the central nervous system can be reversed by narcotic antagonists such as naloxone.

Dependence potential
Alpha-methylfentanyl substitutes for morphine in the morphine-dependent monkey and produces primary physical dependence of the opiate type. The substance is self-administered by rhesus monkeys. The substance is recognized as an opiate by heroin abusers and may produce physical dependence in human subjects.

Actual abuse and or/evidence of likelihood of abuse
Street abuse of alpha-methylfentanyl has been reported in the United States of America. At least 16 overdose deaths have been associated with the drug. It has appeared frequently in illicit traffic and is clandestinely manufactured.

Therapeutic usefulness
At present alpha-methylfentanyl has no known therapeutic use.

Recommendation
The Committee found that there was sufficient evidence to indicate that alpha-methylfentanyl is liable to similar abuse as, and produces ill-effects similar to those seen with, drugs in Schedule I of the Single Convention on Narcotic Drugs, 1961 and that Convention as amended by the 1972 Protocol. The Committee rated the abuse liability of the substance as high. The

degree of seriousness of the public health and social problems associated with the substance was found to be high and there is no known therapeutic usefulness. Therefore, the Committee recommended that alphamethylfentanyl be controlled in Schedules I and IV of the Single Convention on Narcotic Drugs, 1961 and that Convention as amended by the 1972 Protocol.

ECDD Recommendation

Inclusion in Schedule I and Schedule IV of the 1961 Convention on Narcotic Drugs