Beta-hydroxy-3-methylfentanyl

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

Recommendation (from TRS)

Substance identification
Beta-hydroxy-3-methylfentanyl (CAS 78995-14-9), chemically N-[1- (beta-hydroxyphenethy])-3-methyl-4- piperidyl]propionanilide, is also known as ohmefentanyl, F-7302, NIH 10551 and OME: The molecule has three chiral centres, and eight stereoisomers and four pairs of racemates are possible.

Similarity to known substances and effects on the CNS
Beta-hydroxy-3-methylfentanyl has been classified as a relatively selective mu-type opioid-receptor agonist with a profile, similar to that of fentanyl. Its analgesic potency in rodents is estimated to be 25 000 times that of morphine. The drug has a rapid onset of action and a duration of about 90 minutes. Like other mu-opioids, beta-hydroxy-3- methylfentanyl depresses respiration but to a lesser extent than fentanyl. The respiratory depression is reversible by nalorphine.

Dependence potential
Beta- hydroxy- 3-methylfentanyl substitutes completely for morphine in morphine-dépendent withdrawn monkeys and is 25 000 times more potent than morphine. in this regard. No human studies are available concerning the dependence potential of beta-hydroxy-3- methylfentanyl.

Actual abuse and or/evidence of likelihood of abuse
Beta-hydroxy-3-methylféntany/ is one of the fentanyl analogues that have appeared in the illicit drug traffic since late 1979. It has been identified in drug seizures in the USA by a Drug Enforcement Administration laboratory, and clandestine production has been demonstrated.

Therapeutic usefulness
At present, beta-hydroxy-3-methylfentanyl has no known therapeutic use.

Recommendation
The Committee found that there was sufficient evidence to indicate that beta-hydroxy-3-methylfentanyl is liable to similar. abuse to, 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 public health and social problems associated with the substance are extremely serious and there is no known therapeutic use. Therefore, the Committee recommended that beta-hydroxy-3-methylfentanyl 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