Current Scheduling Status
None
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
Hexobarbital (INN, CAS 56-29-1), chemically 5-(1-cyclohexen-1-yl)-1,5-dimethylbarbituric acid, is also known as ciclobarbital, enhexymal, enhexymalum, enimal, esobarbital, hexabarbital,
hexobarbitalum, hexobarbitone, methexenyl, methyl-cyclohexenylmethyl- barbitusaure, methylhexabarbital, methylhexabital. The substance is a racemic mixture.
Similarity to known substances and effects on the CNS
Hexobarbital has been classified as a short-acting intravenous anaesthetic agent. As such it is not similar to any of the already scheduled barbiturates. The drug has also been used orally as a sedative and a hypnotic. It produces dose-related drowsiness, vertigo, confusion, and incoordination. It is metabolized by hepatic microsomal enzymes and stimulates the production of these enzymes. Thus, hexobarbital is similar to other barbiturates in this regard. The drug produces typical barbiturate-like effects on the central nervous system. Tolerance, both natural and functional, does occur. Cross-tolerance occurs to other barbiturates, ethanol, and to other sedative-hypnotic drugs.
Dependence potential
It has been demonstrated in animal experiments that rats seek intravenous self administration of hexobarbital, indicating that it has dependence potential.
Actual abuse and or/evidence of likelihood of abuse
Isolated cases of abuse have been reported by four countries. The drug is under national control in four countries. Several reports of illicit trafficking andor seizures have been reported from six countries. There were no reports of clandestine manufacture.
Therapeutic usefulness
Hexobarbital is used orally as a hypnotic and a sedative. It was formerly used as an induction anaesthetic with similar effects and toxicity to those of thiopental sodium. It is also widely used as a laboratory agent for measuring the potentiation of sleeping time. Hexobarbital is produced and/or marketed in seven countries. In most countries where it is marketed, hexobarbital is available on prescription only, with no refill. The Committee rated its therapeutic usefulness as a sedative-hypnotic as relatively low. Its usefulness as an intravenous anaesthetic agent and as a laboratory agent for measuring the potentiation of sleeping time, was rated as relatively high.
Recommendation
The Committee found that there was insufficient evidence that hexobarbital 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 data concerninigt s pharmacological profile, dependence potential, and actual abuse, the Committee rated the
likelihood of abuse of hexobarbital as moderate. The degree of the public health and social problems associated with the drug was found to be low .as was its therapeutic usefulness as a
sedative-hypnotic. As an intravenous anaesthetic agent and laboratory standard its usefulness was rated as relatively high. In the light of this assessment, the Committee recommended
against scheduling of the drug.
Hexobarbital (INN, CAS 56-29-1), chemically 5-(1-cyclohexen-1-yl)-1,5-dimethylbarbituric acid, is also known as ciclobarbital, enhexymal, enhexymalum, enimal, esobarbital, hexabarbital,
hexobarbitalum, hexobarbitone, methexenyl, methyl-cyclohexenylmethyl- barbitusaure, methylhexabarbital, methylhexabital. The substance is a racemic mixture.
Similarity to known substances and effects on the CNS
Hexobarbital has been classified as a short-acting intravenous anaesthetic agent. As such it is not similar to any of the already scheduled barbiturates. The drug has also been used orally as a sedative and a hypnotic. It produces dose-related drowsiness, vertigo, confusion, and incoordination. It is metabolized by hepatic microsomal enzymes and stimulates the production of these enzymes. Thus, hexobarbital is similar to other barbiturates in this regard. The drug produces typical barbiturate-like effects on the central nervous system. Tolerance, both natural and functional, does occur. Cross-tolerance occurs to other barbiturates, ethanol, and to other sedative-hypnotic drugs.
Dependence potential
It has been demonstrated in animal experiments that rats seek intravenous self administration of hexobarbital, indicating that it has dependence potential.
Actual abuse and or/evidence of likelihood of abuse
Isolated cases of abuse have been reported by four countries. The drug is under national control in four countries. Several reports of illicit trafficking andor seizures have been reported from six countries. There were no reports of clandestine manufacture.
Therapeutic usefulness
Hexobarbital is used orally as a hypnotic and a sedative. It was formerly used as an induction anaesthetic with similar effects and toxicity to those of thiopental sodium. It is also widely used as a laboratory agent for measuring the potentiation of sleeping time. Hexobarbital is produced and/or marketed in seven countries. In most countries where it is marketed, hexobarbital is available on prescription only, with no refill. The Committee rated its therapeutic usefulness as a sedative-hypnotic as relatively low. Its usefulness as an intravenous anaesthetic agent and as a laboratory agent for measuring the potentiation of sleeping time, was rated as relatively high.
Recommendation
The Committee found that there was insufficient evidence that hexobarbital 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 data concerninigt s pharmacological profile, dependence potential, and actual abuse, the Committee rated the
likelihood of abuse of hexobarbital as moderate. The degree of the public health and social problems associated with the drug was found to be low .as was its therapeutic usefulness as a
sedative-hypnotic. As an intravenous anaesthetic agent and laboratory standard its usefulness was rated as relatively high. In the light of this assessment, the Committee recommended
against scheduling of the drug.
ECDD Recommendation
Scheduling/control not currently recommended
Link to full TRS
who_trs_741.pdf2.21 MB