1,4-Butanediol

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Death may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, thienodiazepines or alcohol.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: 1,4-Butanediol
1,4-Butanediol
Molecular structure of 1,4-Butanediol
1,4-Butanediol.svg
Chemical Nomenclature
Common names 1,4-Butanediol, 1,4-B, BD, One Comma Four, One Four Bee, Butylene Glycol, or One Four B-D-O
Systematic name Butane-1,4-diol
Class Membership
Psychoactive class Depressant
Chemical class GABAergic
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold < 0.25 - 0.5 mL
Light 0.5 - 1 mL
Common 1 - 1.5 mL
Strong 1.5+ mL Warning: 2ml can induce heavy sleep.
Duration
Total 3 - 5 hours
Onset 20 minutes - 60 minutes
Peak 1 - 2 hours
Offset 1.5 - 2 hours
After effects 2 - 4 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

1,4-Butanediol (1,4-B, butylene glycol, or BD) is a thick, colourless liquid which is nearly odorless with a distinct bitter taste. 1,4-Butanediol is used industrially as a solvent and in the manufacture of some types of plastics, elastic fibers and polyurethanes. In organic chemistry, 1,4-butanediol is used for the synthesis of γ-butyrolactone (GBL).[2]

In humans, it acts as a depressant and a prodrug for GHB where 1ml is equivalent to 1g of GHB. It is used as a recreational intoxicant with effects similar to alcohol.[3]

1,4-Butanediol, as well as GBL, will dissolve most types of plastic over time.[4] For this reason, it is recommended to only transport and store the drug using a glass container, standard gelatin capsules (not vegetarian), or high-density polyethylene plastic (also known as #2 recycled plastic). To check the type of plastic used on a bottle, one can look at the bottom for a number in the triangle shaped recycling label.

Bottle of 1,4 Butanediol.

Chemistry

1,4-Butanediol is classified as a subclass of alcoholic compounds called diols. Diols are named for having two alcohol (OH-) substitutions in their structure. 1,4-Butanediol is comprised of a butane chain of four carbon groups with an alcohol group bound to each terminal carbon of this chain. 1,4-Butanediol is named for these alcohol substitutions, which are located at R1 and R4.

Pharmacology

Main article: GHB § Pharmacology

1,4-Butanediol is not active in its own right; its mechanism of action stems from its identity as a prodrug of GHB.[5]

It is converted into GHB in the liver by the enzymes alcohol dehydrogenase and aldehyde dehydrogenase, which is the same enzyme as alcohol.[6] 1,4-Butanediol is first converted into 4-hydroxybutaldehyde in the liver and is released into the bloodstream before returning to the liver to convert into GHB. This process results in a much more delayed onset than GBL or GHB.[7]

The differing levels of dehydrogenase enzymes can vary between individuals, meaning that, like alcohol, effects can differ greatly between users. In many, this manifests as a slow onset of effects and a higher rate of aldehyde collecting in the bloodstream, causing more toxic side effects. Because of these pharmacokinetic differences, 1,4-butanediol tends to be less potent and with a slower onset than GHB but has a longer duration; the related compound GBL tends to be slightly more potent and faster to take effect but more short-acting than GHB.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances and are more likely to induce a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include injury or death.

Physical effects
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Cognitive effects
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Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

Radar plot showing relative physical harm, social harm, and dependence of GHB[8]

1,4-Butanediol is not active in its own right; its mechanism of action stems from its identity as a prodrug of GHB, meaning that it is rapidly converted into GHB in the body.

GHB is considered to be a safe and non-toxic substance when used responsibly or medically. The LD50 is above the active dosage, and there is no danger of acute toxicity when this compound is taken at appropriate dosages. However, it can be dangerous when used as a recreational drug or abused. There have been many negative reports from recreational users who have overdosed, combined GHB with alcohol or other drugs, or accidentally dosed themselves unexpectedly.[9]

One publication has investigated 226 deaths attributed to GHB.[10] Seventy-one deaths (34%) were caused by GHB alone while the other deaths were from respiratory depression caused by interaction with alcohol or other drugs.

To avoid a possible overdose of GHB/1,4-Butanediol, it is important to start with a low dose and work your way up slowly by increasing the dosage in small increments as the exact toxic dosage is unknown.

Accidental ingestions of 1,4-Butanediol have also occurred due to inadequate storage methods. If 1,4-Butanediol is put into a clear liquid, glass, or bottle, it can be easily mistaken for water. It is recommended to clearly label your 1,4-Butanediol in writing and dye the liquid with blue food coloring so it no longer resembles a drinkable beverage. It is also recommended to store your 1,4-Butanediol in a container that no one would drink out of.

It is strongly recommended that one use harm reduction practices when using this drug.

Neurotoxicity

In multiple studies, GHB has been found to impair spatial memory, working memory, learning and memory in rats with chronic administration.[11][12][13][14] These effects are associated with decreased NMDA receptor expression in the cerebral cortex and possibly other areas as well.[15]

One study found that repeated administration of GHB to rats for 15 days drastically reduced the number of neurons and non-neuronal cells within the hippocampus and in the prefrontal cortex. With doses of 10 mg/kg of GHB, they were decreased by 61% in the hippocampus region and 32% in the prefrontal cortex, and with 100 mg/kg, they were decreased by 38% and 9%, respectively. This paper demonstrates contradicting effects on neuronal loss, with lower doses (10 mg/kg) producing the most neurotoxicity, and higher doses (100 mg/kg) producing less.

Tolerance and addiction potential

This table compares the withdrawal symptoms of GHB/1,4-Butanediol, benzodiazepines, and alcohol.[16]

GHB/1,4-Butanediol is moderately physically and psychologically addictive. The frequent use of GHB/1,4-Butanediol can cause withdrawal symptoms similar to those caused by other depressants such as alcohol and benzodiazepines if abruptly discontinued.[17][18] These symptoms seem to depend on the dosage and the length of time the drug was used for. Light to moderate users often experience anxiety, insomnia, sleep-related problems, and tremors whereas heavy use can cause severe withdrawal symptoms like delirium, psychosis, and hallucinations.[19][16]

Although there have been reported fatalities due to GHB/1,4-Butanediol withdrawal, reports are inconclusive and further research is needed.[20]

Tolerance will develop to the sedative-hypnotic effects within several weeks of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.

Dangerous interactions

Although many psychoactive substances are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

A review of the details of 194 deaths attributed to or related to GHB over a ten-year period found that most were from respiratory depression caused by interaction with alcohol or other drugs.[21] In humans, GHB has been shown to inhibit the elimination rate of alcohol. This may explain the respiratory arrest that has been reported after ingestion of both drugs.[22] These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation.[23][24]
  • Stimulants - It can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.

Legal issues

  • United States: While 1,4-butanediol is not currently scheduled federally in the United States, a number of states have classified it as a controlled substance. Additionally, individuals have been prosecuted for this substance under the Federal Analogue Act as being substantially similar to GHB.[25] A federal district court in Chicago ruled that 1,4-butanediol could not be considered an analogue of GHB under federal law, and the Seventh Circuit Court of Appeals upheld that ruling.[26]
  • United Kingdom: In the United Kingdom, 1,4-butanediol was scheduled in December 2009 (along with another GHB precursor, gamma-butyrolactone) as a Class C controlled substance.
  • Germany: In Germany, the drug is not explicitly illegal, but might also be treated as illegal if used as a drug.
  • Canada: It is controlled as a Schedule VI precursor in Canada.

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. http://pubs.acs.org/doi/abs/10.1021/om048983m
  3. http://www.nejm.org/doi/full/10.1056/NEJM200101113440202
  4. https://www.erowid.org/chemicals/14b/14b_storage1.shtml | 1,4-Butanediol & GBL Storage - 1,4-B & GBL May Dissolve Some Plastics by Erowid (Jul 2001)
  5. http://onlinelibrary.wiley.com/doi/10.1111/j.1460-9568.2006.05146.x/abstract;jsessionid=D1EC0DE56C54DB2E93F66DEC2CCB2EDD.f02t02
  6. http://emedicine.medscape.com/article/820531-overview | Gamma-Hydroxybutyrate Toxicity
  7. http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=8067214.PN.&OS=PN/8067214&RS=PN/8067214
  8. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  9. https://www.erowid.org/experiences/exp.php?ID=1926 | Erowid. "GHB Overdoses & Poisonings: An Experience with GHB (ID 1926)". Erowid.org. Jun 19, 2000. erowid.org/exp/1926
  10. https://www.ncbi.nlm.nih.gov/pubmed/20825811 | Zvosec DL, Smith SW, Porrata T, Strobl AQ, Dyer JE (2011). "Case series of 226 gamma-hydroxybutyrate-associated deaths: lethal toxicity and trauma". The American Journal of Emergency Medicine 29 (3): 319–32.
  11. Adolescent γ-hydroxybutyric acid exposure decreases cortical N-methyl-d-aspartate receptor and impairs spatial learning (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S009130570400320X
  12. Effects of subchronic administration of gammahydroxybutyrate (GHB) on spatial working memory in rats (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/17296081
  13. γ-Hydroxybutyric Acid–Induced Cognitive Deficits in the Female Adolescent Rat | http://onlinelibrary.wiley.com/doi/10.1196/annals.1432.044/abstract
  14. Neurotoxic effects induced by gammahydroxybutyric acid (GHB) in male rats | http://journals.cambridge.org/action/displayAbstract?fromPage=online&aid=6137924
  15. https://www.ncbi.nlm.nih.gov/pubmed/15582677 (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/15582677
  16. 16.0 16.1 GHB Withdrawal Syndrome | Texas Commission on Alcohol and Drug Abuse | https://www.erowid.org/chemicals/ghb/ghb_addiction2.pdf
  17. Systematic Assessment of Gamma Hydroxybutyrate (GHB) Effects During and After Acute Intoxication (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2759403/
  18. Illicit gamma-hydroxybutyrate (GHB) and pharmaceutical sodium oxybate (Xyrem®): differences in characteristics and misuse (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2713368/
  19. https://www.ncbi.nlm.nih.gov/pubmed/11174231 | Gamma-hydroxybutyrate withdrawal syndrome.
  20. Gamma-hydroxybutyrate: an emerging drug of abuse that causes physical dependence | http://onlinelibrary.wiley.com/doi/10.1111/j.1360-0443.1997.tb03640.x/abstract
  21. http://web.archive.org/web/20071203005230/http://www.aafs.org/pdf/Seattleabstracts06.pdf
  22. The role of gamma-hydroxybutyric acid in the treatment of alcoholism: from animal to clinical studies (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/10075397
  23. https://www.erowid.org/chemicals/ghb/ghb_health.shtml
  24. Suspicious death related to gamma-hydroxybutyrate (GHB) toxicity (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/15274975
  25. http://cases.justia.com/us-court-of-appeals/F3/312/926/608696/
  26. United States v. Turcotte, 405 F.3d 515 (7th Cir. 2005) "With specific regard to 1,4-butanediol, the jury has returned a special verdict which states that 1,4-butanediol is not a Schedule I drug analogue, because 1,4-butanediol's chemical structure is not significantly similar to the chemical structure of GHB.