Current Scheduling Status
None
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
Febarbamate (INN, CAS-13246-02-1), chemically 1-(3’-butoxy-2’-hydroxypropyl)-5-ethyl-5-phenylbarbituric acid carbamate, is also known as phebarbamate, and phenobamate. It is a racemic mixture.
Similarity to known substances and effects on the CNS
Febarbamate is a derivative of phenobarbital in which one nitrogen is substituted with a butoxylcarbamoylpropyl group. It has been reported that the drug is extensively metabolized in the body, but not to phenobarbital. The manufacturer claims that because of this bulky substitution, phenobarbital loses its typical pharmacological profile and febarbamate is completely devoid of sedative-hypnotic effects. Most of the reported pharmacological data concern tetrabamate, which is a stable complex containing two molecules of febarbamate. The drug is not similar to any of the already scheduled substances. Pharmacological data from animal studies concerning febarbamate have been provided by the manufacturer. The drug is
reported to be devoid of sedative-hypnotic and toxic effects after oral administration. However, an intraperitoneal LD, of 277 mg/kg of body weight was reported for mice. Unfortunately, no report of observed signs and symptoms was given. It is possible that the drug is poorly absorbed in the gastrointestinal tract and/or rapidly metabolized.
Dependence potential
There is no information available on the ability of febarbamate to induce physical or psychic dependence, in either animals or man in controlled laboratory studies.
Actual abuse and or/evidence of likelihood of abuse
Isolated cases of abuse in France have been reported but it is not clear whether these involved the substance itself or the complex tetrabamate. In the Congo, the drug was reported to be found in illicit trafficking. It is under national control in five countries.
Therapeutic usefulness
Febarbamate has been reported to be a thymoanaleptic and to be of use in the treatment of agitation in the elderly. The Committee felt that there was insufficient information to judge the usefulness of febarbamate. Large quantities of the drug are used either as a pure drug or as a constituent of the complex tetrabamate, particularly in France.
Recommendation
The Committee found that there was insufficient evidence that febarbamate 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. On the basis of the very limited data concerning its pharmacological profile, dependence potential, and actual abuse, the Committee rated the likelihood of abuse of febarbamate as indeterminate. The degree of the public health and social problems associated with the drug was found to be low and its therapeutic
usefulness remains to be established. In the light of this assessment, the Committee recommended against scheduling of the drug. However, owing to the large consumption of the drug, it was felt that continued surveillance was warranted.
Febarbamate (INN, CAS-13246-02-1), chemically 1-(3’-butoxy-2’-hydroxypropyl)-5-ethyl-5-phenylbarbituric acid carbamate, is also known as phebarbamate, and phenobamate. It is a racemic mixture.
Similarity to known substances and effects on the CNS
Febarbamate is a derivative of phenobarbital in which one nitrogen is substituted with a butoxylcarbamoylpropyl group. It has been reported that the drug is extensively metabolized in the body, but not to phenobarbital. The manufacturer claims that because of this bulky substitution, phenobarbital loses its typical pharmacological profile and febarbamate is completely devoid of sedative-hypnotic effects. Most of the reported pharmacological data concern tetrabamate, which is a stable complex containing two molecules of febarbamate. The drug is not similar to any of the already scheduled substances. Pharmacological data from animal studies concerning febarbamate have been provided by the manufacturer. The drug is
reported to be devoid of sedative-hypnotic and toxic effects after oral administration. However, an intraperitoneal LD, of 277 mg/kg of body weight was reported for mice. Unfortunately, no report of observed signs and symptoms was given. It is possible that the drug is poorly absorbed in the gastrointestinal tract and/or rapidly metabolized.
Dependence potential
There is no information available on the ability of febarbamate to induce physical or psychic dependence, in either animals or man in controlled laboratory studies.
Actual abuse and or/evidence of likelihood of abuse
Isolated cases of abuse in France have been reported but it is not clear whether these involved the substance itself or the complex tetrabamate. In the Congo, the drug was reported to be found in illicit trafficking. It is under national control in five countries.
Therapeutic usefulness
Febarbamate has been reported to be a thymoanaleptic and to be of use in the treatment of agitation in the elderly. The Committee felt that there was insufficient information to judge the usefulness of febarbamate. Large quantities of the drug are used either as a pure drug or as a constituent of the complex tetrabamate, particularly in France.
Recommendation
The Committee found that there was insufficient evidence that febarbamate 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. On the basis of the very limited data concerning its pharmacological profile, dependence potential, and actual abuse, the Committee rated the likelihood of abuse of febarbamate as indeterminate. The degree of the public health and social problems associated with the drug was found to be low and its therapeutic
usefulness remains to be established. In the light of this assessment, the Committee recommended against scheduling of the drug. However, owing to the large consumption of the drug, it was felt that continued surveillance was warranted.
ECDD Recommendation
Placed under surveillance
Link to full TRS
who_trs_741.pdf2.21 MB