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
3-Methylfentanyl (CAS 42045-86-3); chemical name: (1) CAS: N-[3-methyl-1-(2-phenylethyl)-4-piperidinyl]-N-phenylpropanamide; 5 TUFA. N-(3- Methyl-1-(2-phenylethyl)-4-piperidyl)propionanilide. The drug is also known as F7209. Two racemates and four stereoisomers are possible for 3-methylfentanyl.
Similarity to known substances and effects on the CNS
3-Methylfentanyl has been classified pharmacologically as an agonist of mu-type opioid receptors with a profile similar to that of fentanyl. It possesses analgesic activity and
produces morphine-like euphoric effects. Its analgesic potency is about four times that of fentanyl and 1100 times that of morphine. Like other mu-type opioids, 3-methylfentanyl depresses respiration, and its effects on the central nervous system can be reversed by narcotic antagonists such as naloxone. Cis-3-methylfentanyl has a rapid onset of activity and duration of activity of at least 2% hours. Its potency is estimated to be 1000 times that of morphine. Trans-3-methylfentanyl also has a rapid onset of activity but a shorter duration of action than the cis-isomer. Its potency is about 600 times that of morphine. The analgesic activity was greatest for the (+) cis-isomer (ED50 = 0 0058 mg/kg of body weight in mice).
Dependence potential
3-Methylfentanyl (both cis- and trans-isomers) substitutes for morphine in the morphine-dependent monkey and produces physical dependence of the morphine 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 subjects.
Actual abuse and or/evidence of likelihood of abuse
Street abuse of 3-methylfentanyl has been reported in the United States of America. Over 60 cases of death due to an overdose have been reported to be associated with the substance. It has appeared frequently in illicit traffic and is clandestinely manufactured. On the basis of urine analysis, it was suspected that the substance was being abused by approximately 10% of 500 individuals enrolled in drug treatment programmes in California, USA.
Therapeutic usefulness
At present, 3-m ethylfentanyl has no known therapeutic use.
Recommendation
The Committee found that there was sufficient evidence to indicate that 3-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 drug as high. The degree of seriousness of the public health and social problems associated with the drug was also found to be high, and there is no known therapeutic use. Therefore, the Committee recommended that 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.
3-Methylfentanyl (CAS 42045-86-3); chemical name: (1) CAS: N-[3-methyl-1-(2-phenylethyl)-4-piperidinyl]-N-phenylpropanamide; 5 TUFA. N-(3- Methyl-1-(2-phenylethyl)-4-piperidyl)propionanilide. The drug is also known as F7209. Two racemates and four stereoisomers are possible for 3-methylfentanyl.
Similarity to known substances and effects on the CNS
3-Methylfentanyl has been classified pharmacologically as an agonist of mu-type opioid receptors with a profile similar to that of fentanyl. It possesses analgesic activity and
produces morphine-like euphoric effects. Its analgesic potency is about four times that of fentanyl and 1100 times that of morphine. Like other mu-type opioids, 3-methylfentanyl depresses respiration, and its effects on the central nervous system can be reversed by narcotic antagonists such as naloxone. Cis-3-methylfentanyl has a rapid onset of activity and duration of activity of at least 2% hours. Its potency is estimated to be 1000 times that of morphine. Trans-3-methylfentanyl also has a rapid onset of activity but a shorter duration of action than the cis-isomer. Its potency is about 600 times that of morphine. The analgesic activity was greatest for the (+) cis-isomer (ED50 = 0 0058 mg/kg of body weight in mice).
Dependence potential
3-Methylfentanyl (both cis- and trans-isomers) substitutes for morphine in the morphine-dependent monkey and produces physical dependence of the morphine 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 subjects.
Actual abuse and or/evidence of likelihood of abuse
Street abuse of 3-methylfentanyl has been reported in the United States of America. Over 60 cases of death due to an overdose have been reported to be associated with the substance. It has appeared frequently in illicit traffic and is clandestinely manufactured. On the basis of urine analysis, it was suspected that the substance was being abused by approximately 10% of 500 individuals enrolled in drug treatment programmes in California, USA.
Therapeutic usefulness
At present, 3-m ethylfentanyl has no known therapeutic use.
Recommendation
The Committee found that there was sufficient evidence to indicate that 3-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 drug as high. The degree of seriousness of the public health and social problems associated with the drug was also found to be high, and there is no known therapeutic use. Therefore, the Committee recommended that 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
Link to full TRS
who_trs_761.pdf1.41 MB