Beta-hydroxyfentanyl

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

Recommendation (from TRS)

Substance identification
Beta-hydroxyfentanyl’ (CAS 78995-10-5), chemically N-[1-(beta-hydroxyphenethyl)-4-piperidyl]-propionanilide, is also known as NIH 10506 and MCV 4568. There is one chiral carbon atom in the molecule, so that two stereoisomers and one racemate are possible.

Similarity to known substances and effects on the CNS
Beta-hydroxyfentanyl has been classified pharmacologically 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 about 50 times that of morphine. In the rhesus monkey, beta-hydroxyfentanyl acts promptly and its duration of action (120-150 minutes) is shorter than that of morphine.

Dependence potential
Beta-hydroxyfentanyl substitutes completely for morphine in morphine-dependent withdrawn monkeys and is 50 times more potent than morphine in this regard. No human studies are available concerning the dependence potential of beta-hydroxyfentanyl.

Actual abuse and or/evidence of likelihood of abuse
Beta-hydroxyfentanyl 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-hydroxyfentanyl has no known therapeutic use.

Recommendation
The Committee found that there was sufficient evidence to indicate that beta-hydroxyfentanyl is liable to similar abuse to, and _produces ill-effects similar to those seen with, drugs in Schedule I of the Single Conventioonn. 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-hydroxyfentanyl becontrolled in Schedules I and IV of the Single Convention on Narcotic Drugs, 1961, and that Convention as amended bytht he 1972 protocol.

ECDD Recommendation

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