Alternative names
1,4-BD
IUPAC Name
1,4-butanediol
Current Scheduling Status
Recommendation not accepted
Year(s) and type of review / ECDD meetings
Drug Class
Recommendation (from TRS)
Substance identification
1,4-butanediol (butane-1,4-diol; 1,4-BDO or 1,4-BD) is a colourless, viscous liquid derived from butane by placement of alcohol groups at each end of the chain. It is one of four stable isomers of butanediol.
Previous review
During the discussion of gamma-hydroxybutyric acid (GHB) at its thirty-fourth meeting, the ECDD "noted information relating to the abuse of 1,4-BD itself (convertible to GHB in the body) and suggested this substance for pre-review." Based on the evidence presented in the pre-review of GBL during its thirty-fifth meeting, given its close association with GHB, and the recommendation made by the Committee to reschedule GHB from Schedule IV to Schedule II of the 1971 Convention, the thirty-fifth meeting of the Committee recommended that a critical review of 1,4-BD be undertaken.
Similarity to known substances and effects on the central nervous system
1,4-BD is readily converted, both chemically and in the body, to the Schedule II drug, GHB, with a Tmax of conversion following oral administration of 39.4 (± 11.2) minutes in humans. Most of 1,4-BD’s pharmacological and toxicological effects are mediated through GHB as a metabolite, as 1,4-BD itself has no binding affinity to central nervous system receptors. Nevertheless, through GHB, it produces central nervous system depressant effects which may be exacerbated by other central nervous system depressants (including ethanol). There is a steep dose–effect curve between doses producing desired and excessive effects, and there have been various published reports of adverse reactions to 1,4-BD including fatalities. Signs and symptoms include euphoria, relaxation, reduced inhibition and sedation, progressing to vomiting, urinary and faecal incontinence, agitation, convulsions, bradycardia, respiratory depression, coma and death.
Dependence potential
Some animal studies have indicated that 1,4-BD can induce physical dependence. There have been various reports that, in human users, 1,4-BD can produce a withdrawal syndrome when the substance is abruptly discontinued following regular chronic use. Withdrawal from 1,4 BD appears similar to withdrawal from other sedative–hypnotic drugs such as ethanol and benzodiazepines.
Actual abuse and/or evidence of likelihood of abuse
1,4-BD abuse and/or seized material has been reported in 18 countries. There are instances of diversion of the raw substance, and trafficking in dietary supplements containing the compound as well as discrete instances of clandestine manufacture. 1,4-BD is sold under various product and so-called street names. It is extremely difficult to accurately assess the magnitude of abuse relating specifically to 1,4- BD considering the near absence of data explicitly pertaining to 1,4-BD rather than GHB or GBL.
Therapeutic usefulness
1,4-BD has no recognized therapeutic application. However, the dimethanesulfonate form (1,4-butanediol dimethanesulfonate) is available in oral and intravenous formulations for the treatment of chronic myeloid leukaemia but does not produce any adverse effects on the central nervous system. However, 1,4-BD has industrial use as an intermediate chemical for production of tetrahydrofuran and poly(tetramethylene-ether)glycol, polybutylene terephthalate, GBL, polyurethane and other solvents.
Recommendation
1,4-Butanediol produces its effects in the body through the in vivo formation of the scheduled substance GHB. The Committee considered that the degree of risk to public health and society associated with the abuse liability of 1,4-butanediol is especially serious. While the Committee recognized its widespread and important industrial use, 1,4-butanediol has no defined therapeutic usefulness. The Committee considered that the evidence of its abuse warranted its placement under international control within Schedule I of the 1971 Convention.
1,4-butanediol (butane-1,4-diol; 1,4-BDO or 1,4-BD) is a colourless, viscous liquid derived from butane by placement of alcohol groups at each end of the chain. It is one of four stable isomers of butanediol.
Previous review
During the discussion of gamma-hydroxybutyric acid (GHB) at its thirty-fourth meeting, the ECDD "noted information relating to the abuse of 1,4-BD itself (convertible to GHB in the body) and suggested this substance for pre-review." Based on the evidence presented in the pre-review of GBL during its thirty-fifth meeting, given its close association with GHB, and the recommendation made by the Committee to reschedule GHB from Schedule IV to Schedule II of the 1971 Convention, the thirty-fifth meeting of the Committee recommended that a critical review of 1,4-BD be undertaken.
Similarity to known substances and effects on the central nervous system
1,4-BD is readily converted, both chemically and in the body, to the Schedule II drug, GHB, with a Tmax of conversion following oral administration of 39.4 (± 11.2) minutes in humans. Most of 1,4-BD’s pharmacological and toxicological effects are mediated through GHB as a metabolite, as 1,4-BD itself has no binding affinity to central nervous system receptors. Nevertheless, through GHB, it produces central nervous system depressant effects which may be exacerbated by other central nervous system depressants (including ethanol). There is a steep dose–effect curve between doses producing desired and excessive effects, and there have been various published reports of adverse reactions to 1,4-BD including fatalities. Signs and symptoms include euphoria, relaxation, reduced inhibition and sedation, progressing to vomiting, urinary and faecal incontinence, agitation, convulsions, bradycardia, respiratory depression, coma and death.
Dependence potential
Some animal studies have indicated that 1,4-BD can induce physical dependence. There have been various reports that, in human users, 1,4-BD can produce a withdrawal syndrome when the substance is abruptly discontinued following regular chronic use. Withdrawal from 1,4 BD appears similar to withdrawal from other sedative–hypnotic drugs such as ethanol and benzodiazepines.
Actual abuse and/or evidence of likelihood of abuse
1,4-BD abuse and/or seized material has been reported in 18 countries. There are instances of diversion of the raw substance, and trafficking in dietary supplements containing the compound as well as discrete instances of clandestine manufacture. 1,4-BD is sold under various product and so-called street names. It is extremely difficult to accurately assess the magnitude of abuse relating specifically to 1,4- BD considering the near absence of data explicitly pertaining to 1,4-BD rather than GHB or GBL.
Therapeutic usefulness
1,4-BD has no recognized therapeutic application. However, the dimethanesulfonate form (1,4-butanediol dimethanesulfonate) is available in oral and intravenous formulations for the treatment of chronic myeloid leukaemia but does not produce any adverse effects on the central nervous system. However, 1,4-BD has industrial use as an intermediate chemical for production of tetrahydrofuran and poly(tetramethylene-ether)glycol, polybutylene terephthalate, GBL, polyurethane and other solvents.
Recommendation
1,4-Butanediol produces its effects in the body through the in vivo formation of the scheduled substance GHB. The Committee considered that the degree of risk to public health and society associated with the abuse liability of 1,4-butanediol is especially serious. While the Committee recognized its widespread and important industrial use, 1,4-butanediol has no defined therapeutic usefulness. The Committee considered that the evidence of its abuse warranted its placement under international control within Schedule I of the 1971 Convention.
ECDD Recommendation
Schedule I of the 1971 Convention on Psychotropic Substances
Link to full TRS
who_trs_991_eng.pdf1.3 MB
MS Questionnaire Report