Current Scheduling Status
None
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
Methohexital . sodium’ (CAS-22151-68-4, sodium _ salt), chemically 5-allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid sodium salt, is also known as methohexitone. It is a racemic mixture.
Similarity to known substances and effects on the CNS
Methohexital sodium has been classified pharmacologically as an ultra-short-acting barbiturate used as an intravenous anaesthetic agent. Barbiturates of this type have not been scheduled. Doserelated drowsiness, vertigo, confusion, and incoordination do occur. The drug, like other barbiturates, is metabolized by hepatic microsomal enzymes and stimulates the production of these enzymes. Like other short-acting barbiturates, methohexital sodium produces a dose-related depression of the central nervous system, ranging from mild sedation to general anaesthesia and coma. Tolerance, both natural and functional can occur. Cross-tolerance may occur to other barbiturates, ethanol, and other sedative-hypnotic drugs.
Dependence potential
There are no data on the ability of methohexital to induce physical dependence. The reinforcing effect of methohexital has been demonstrated in rats and rhesus monkeys by intravenous self-administration experiments, and in baboons by oral self-administration experiments.
Actual abuse and or/evidence of likelihood of abuse
Isolated instances of abuse have been reported from Austria, Norway, and the United States of America, but the total number of these cases is very small. No government reported on any public health or social problems caused by this substance. There have been only very minor reports of illicit trafficking and no report of clandestine manufacture. It is under national control in eight countries.
Therapeutic usefulness
Methohexital is administered as sodium salt for the induction of general anaesthesia or complete anaesthesia of short duration. The drug is available in thirty-seven countries mainly for hospital use. The Committee rated the therapeutic usefulness of methohexital as an intravenous anaesthetic agent as high.
Recommendation
The Committee found that there was insufficient evidence that methohexital 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 concerning its pharmacological profile, dependence potential, and actual abuse, the Committee rated the
likelihood of abuse of methohexital sodium as moderate. The degree of the public health and social problems associated with the drug was found to be low and its therapeutic usefulness high. In the light of this assessment, the Committee recommended against scheduling of the drug.
Methohexital . sodium’ (CAS-22151-68-4, sodium _ salt), chemically 5-allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid sodium salt, is also known as methohexitone. It is a racemic mixture.
Similarity to known substances and effects on the CNS
Methohexital sodium has been classified pharmacologically as an ultra-short-acting barbiturate used as an intravenous anaesthetic agent. Barbiturates of this type have not been scheduled. Doserelated drowsiness, vertigo, confusion, and incoordination do occur. The drug, like other barbiturates, is metabolized by hepatic microsomal enzymes and stimulates the production of these enzymes. Like other short-acting barbiturates, methohexital sodium produces a dose-related depression of the central nervous system, ranging from mild sedation to general anaesthesia and coma. Tolerance, both natural and functional can occur. Cross-tolerance may occur to other barbiturates, ethanol, and other sedative-hypnotic drugs.
Dependence potential
There are no data on the ability of methohexital to induce physical dependence. The reinforcing effect of methohexital has been demonstrated in rats and rhesus monkeys by intravenous self-administration experiments, and in baboons by oral self-administration experiments.
Actual abuse and or/evidence of likelihood of abuse
Isolated instances of abuse have been reported from Austria, Norway, and the United States of America, but the total number of these cases is very small. No government reported on any public health or social problems caused by this substance. There have been only very minor reports of illicit trafficking and no report of clandestine manufacture. It is under national control in eight countries.
Therapeutic usefulness
Methohexital is administered as sodium salt for the induction of general anaesthesia or complete anaesthesia of short duration. The drug is available in thirty-seven countries mainly for hospital use. The Committee rated the therapeutic usefulness of methohexital as an intravenous anaesthetic agent as high.
Recommendation
The Committee found that there was insufficient evidence that methohexital 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 concerning its pharmacological profile, dependence potential, and actual abuse, the Committee rated the
likelihood of abuse of methohexital sodium as moderate. The degree of the public health and social problems associated with the drug was found to be low and its therapeutic usefulness 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