IUPAC Name
N-phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]furan-2-carboxamide
Current Scheduling Status
Schedule I of the 1961 Convention on Narcotic Drugs
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
Chemically, ocfentanil is N-(2-Fluorophenyl)-2-methoxy-N-[1-(2-phenylethyl) piperidin-4-yl]acetamide. It has no stereoisomers.
Previous review
Ocfentanil has not been previously pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to the attention of WHO that ocfentanil is clandestinely manufactured, poses a risk to public health and society, and has no recognized therapeutic use by any Party. Preliminary information collected from various sources indicated that this substance may cause substantial harm and that it has no medical use.
Similarity to known substances and effects on the central nervous system
Chemically, ocfentanil comprises two modifications to fentanyl: replacement of the propionamide group with a methoxyacetamide and the addition of ortho- fluorine to the N-phenyl ring. The pharmacodynamic effects of ocfentanil appear to be similar to those of fentanyl, a potent agonist at the μ subtype of opioid receptors and a Schedule I drug under the 1961 Convention. In rodents, ocfentanil was 2.3 times more potent as an analgesic than fentanyl, and its duration of action was shorter. In human subjects, ocfentanil produces a dose-related increase in analgesia and a decrease in respiration. Clinical research conducted on its use as a supplement to general anaesthesia describes a similar potency of ocfentanil and fentanyl and it had no clear advantage over the latter in terms of safety. Ocfentanil has also been reported to produce other typical opioid effects such as itching, nausea and sedation. Ocfentanil-related deaths have been reported in some European and North American countries.
Dependence potential
No data regarding the dependence and abuse potential of ocfentanil from controlled, human or laboratory animal studies are available.
Actual abuse and/or evidence of likelihood of abuse
Ocfentanil is sold online as heroin. Users of material containing analytically confirmed ocfentanil have reported effects similar to those of heroin including euphoria with stimulation. Epidemiological estimates of use are not available. Ocfentanil is a regulated substance in a number of countries.
Therapeutic usefulness
Ocfentanil is not used therapeutically. It was investigated for therapeutic purposes but found to have a similar clinical profile to fentanyl so further development was discontinued.
Recommendation
Ocfentanil is an opioid that is structurally related to fentanyl, which is regulated under Schedule I of the 1961 Single Convention on Narcotic Drugs. It produces opioid effects including analgesia, euphoria, sedation and potentially serious respiratory depression. Ocfentanil-related deaths have been reported, and it has been brought under national control in several countries in various regions of the world.
Ocfentanil is a compound liable to similar abuse and with similar ill effects to controlled opioids such as fentanyl, which are included in Schedule I of the Single Convention on Narcotic Drugs of 1961. It has no recorded therapeutic use, and its use has been associated with fatalities. There is sufficient evidence that it 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. Thus, because it meets the required condition of similarity, it is recommended that ocfentanil (N-(2-Fluorophenyl)-2-methoxy-N-[1-(2-phenylethyl)piperidin- 4-yl]acetamide) be placed in Schedule I of the Single Convention on Narcotic Drugs, 1961, as consistent with Article 3, paragraph 3 (iii) of that Convention in that the substance is liable to similar abuse and productive of similar ill effects to drugs in Schedule I.
Chemically, ocfentanil is N-(2-Fluorophenyl)-2-methoxy-N-[1-(2-phenylethyl) piperidin-4-yl]acetamide. It has no stereoisomers.
Previous review
Ocfentanil has not been previously pre-reviewed or critically reviewed. A direct critical review was proposed based on information brought to the attention of WHO that ocfentanil is clandestinely manufactured, poses a risk to public health and society, and has no recognized therapeutic use by any Party. Preliminary information collected from various sources indicated that this substance may cause substantial harm and that it has no medical use.
Similarity to known substances and effects on the central nervous system
Chemically, ocfentanil comprises two modifications to fentanyl: replacement of the propionamide group with a methoxyacetamide and the addition of ortho- fluorine to the N-phenyl ring. The pharmacodynamic effects of ocfentanil appear to be similar to those of fentanyl, a potent agonist at the μ subtype of opioid receptors and a Schedule I drug under the 1961 Convention. In rodents, ocfentanil was 2.3 times more potent as an analgesic than fentanyl, and its duration of action was shorter. In human subjects, ocfentanil produces a dose-related increase in analgesia and a decrease in respiration. Clinical research conducted on its use as a supplement to general anaesthesia describes a similar potency of ocfentanil and fentanyl and it had no clear advantage over the latter in terms of safety. Ocfentanil has also been reported to produce other typical opioid effects such as itching, nausea and sedation. Ocfentanil-related deaths have been reported in some European and North American countries.
Dependence potential
No data regarding the dependence and abuse potential of ocfentanil from controlled, human or laboratory animal studies are available.
Actual abuse and/or evidence of likelihood of abuse
Ocfentanil is sold online as heroin. Users of material containing analytically confirmed ocfentanil have reported effects similar to those of heroin including euphoria with stimulation. Epidemiological estimates of use are not available. Ocfentanil is a regulated substance in a number of countries.
Therapeutic usefulness
Ocfentanil is not used therapeutically. It was investigated for therapeutic purposes but found to have a similar clinical profile to fentanyl so further development was discontinued.
Recommendation
Ocfentanil is an opioid that is structurally related to fentanyl, which is regulated under Schedule I of the 1961 Single Convention on Narcotic Drugs. It produces opioid effects including analgesia, euphoria, sedation and potentially serious respiratory depression. Ocfentanil-related deaths have been reported, and it has been brought under national control in several countries in various regions of the world.
Ocfentanil is a compound liable to similar abuse and with similar ill effects to controlled opioids such as fentanyl, which are included in Schedule I of the Single Convention on Narcotic Drugs of 1961. It has no recorded therapeutic use, and its use has been associated with fatalities. There is sufficient evidence that it 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. Thus, because it meets the required condition of similarity, it is recommended that ocfentanil (N-(2-Fluorophenyl)-2-methoxy-N-[1-(2-phenylethyl)piperidin- 4-yl]acetamide) be placed in Schedule I of the Single Convention on Narcotic Drugs, 1961, as consistent with Article 3, paragraph 3 (iii) of that Convention in that the substance is liable to similar abuse and productive of similar ill effects to drugs in Schedule I.
ECDD Recommendation
Inclusion in Schedule I of the 1961 Convention on Narcotic Drugs
Link to full TRS
9789241210188-eng.pdf417.9 KB
MS Questionnaire Report
4.5_ocfentanil_annex1.pdf402.25 KB