GBL

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

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

Summary sheet: GBL
GBL
GBL.svg
Chemical Nomenclature
Common names GBL, gamma-Butyrolactone
Substitutive name 1,4-lactone, 4-butyrolactone, 4-hydroxybutyric acid lactone, gamma-hydroxybutyric acid lactone, and oxolan-2-one
Systematic name Dihydrofuran-2(3H)-one
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 Common Heavy
0.3 - 0.3 - 0.9 - 1.5 - 3
Light Strong
Threshold 0.3 ml
Light 0.3 - 0.9 ml
Common 0.9 - 1.5 ml
Strong 1.5 - 3 ml Warning: Doses over 2 ml can induce heavy sleep.
Heavy 3 ml+
Duration
Total 1 - 2 hours
Onset 10 - 30 minutes
Peak 45 - 90 minutes
Offset 15 - 30 minutes
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.

gamma-Butyrolactone (also known as γ-butyrolactone and commonly as GBL) is a synthetic depressant substance of the GABAergic chemical class that produces powerful euphoric and disinhibiting effects similar to that of alcohol intoxication. In humans it acts as a prodrug for GHB, where 1ml is equivalent to 1.66 grams of GHB.[citation needed]

GBL is a common solvent and reagent in chemistry and is also used as a flavoring, stain remover, wheel cleaner, superglue remover, paint stripper, and as a solvent in some wet aluminum electrolytic capacitors.[citation needed] It has also been found in some wine products, which suggests it may be a naturally occurring substance (see section below).

GBL, along with 1,4-butanediol, are known to dissolve most types of plastic over time.[2] 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 recyclable 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.

GBL has reportedly been used as date rape drug (as a legal alternative to GHB), in which it is secretly put dropwise into drinks but there is little evidence to support it being widespread, especially compared to alcohol due to its strong taste. GBL and GHB are also referred to as "K.-o.-Tropfen" (K.-o.-drops) in German-speaking countries. Care should be taken when offered drinks from strangers.

Chemistry

GBL (gamma-butyrolactone) is a cyclic ester of gamma-hydroxybutanoic acid. GBL can be synthesized from GHB through dehydration of the terminal hydroxy groups, forming a saturated lactone ring. Structurally, GBL is a five-membered ring with an oxygen substituent at R1, adjacent from the oxygen atom in the ring, forming a cyclic ester called a lactone.

Physically, it is a hygroscopic colorless oily liquid with a weak characteristic odor and is soluble in water.

GBL has been found in extracts from samples of unadulterated wines.[3] This finding indicates that GBL is a naturally occurring component in some wines and may be present in similar products. The concentration detected was approximately 5 μg/mL and was easily observed using a simple extraction technique followed by GC/MS analysis.

It can also be found in cheese flavorings but typically results in a content of 0.0002% GBL in the final foodstuff.[4]

Pharmacology

Main article: GHB § Pharmacology

GBL is not active in its own right; its mechanism of action stems from its identity as a prodrug of GHB.

It is rapidly converted into GHB by lactonase enzymes found in the blood. GBL is more lipophilic (fat soluble) than GHB, and so is absorbed faster and has higher bioavailability; paradoxically this can mean that GBL has a faster onset of effects than GHB itself, even though it is a prodrug.

The levels of lactonase enzyme can vary between individuals, meaning that first-time users can show unpredictable results, even from small doses. In many this manifests as slow onset of effects, followed by headaches, semi-consciousness which is distinct from GBL sleep in normal users. If the user decides to try again at a later date, they appear to be able to enjoy the effects normally. Because of these pharmacokinetic differences, GBL tends to be more potent and faster-acting than GHB, but has a shorter duration; whereas the related compound 1,4-butanediol (1,4-B) tends to be slightly less potent, slower to take effect but longer-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 serious 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[5]

GBL 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/GBL 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. 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/GBL with alcohol or other drugs, or accidentally dosed themselves unexpectedly.[6]

One publication has investigated 226 deaths attributed to GHB.[7] 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 GBL, it is important to start with a low dose and work your way up slowly by increasing the dosage in small increments.

Accidental ingestions of GBL have also occurred due to inadequate storage methods. If GBL is put into a clear liquid, glass, or bottle, it can be easily mistaken for water. It is recommended to clearly label your GBL 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 GBL 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.[8][9][10][11] These effects are associated with decreased NMDA receptor expression in the cerebral cortex and possibly other areas as well.[12]

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/GBL, benzodiazepines, and alcohol.[13]

GHB/GBL is moderately physically and psychologically addictive. The frequent use of GHB/GBL can cause withdrawal symptoms similar to those caused by other depressants such as alcohol and benzodiazepines if abruptly discontinued.[14][15] 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.[16][13]

Although there have been reported fatalities due to GHB/GBL withdrawal, reports are inconclusive and further research is needed.[17]

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 to use on their own, they can become dangerous or even life-threatening when taken with other substances. The list below contains some potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses but still increase the possibility of injury of death. Independent research should always be conducted 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.[18] 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.[19] 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.[20][21]

  • 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 status

  • Australia: GBL is a border controlled substance and is illegal to import into Australia without a permit. The importation of a commercial quantity of a border controlled drug (over 1 kg of GBL) is punishable by up to life imprisonment and/or an $825,000 fine.[22]
  • Austria: Since January 1, 2012, GBL is illegal to possess, produce and sell under the NPSG (Neue-Psychoaktive-Substanzen-Gesetz Österreich).[citation needed]
  • Canada: GBL is a Controlled Substance under Schedule VI of the "Controlled Drugs and Substances Act" in Canada. Schedule VI of the "Controlled Drugs and Substances Act" requires vendors to collect information regarding purchases of GBL. The Act also prohibits the import and export of GBL into or out of Canada classifying it as either an indictable offence punishable with up to 10 years in prison or an offence punishable on summary conviction liable to imprisonment for up to eighteen months.[23] It is not illegal for an individual to possess GBL in Canada.
  • Germany: GBL is not listed in the narcotics law, but its distribution is controlled. Possession is not illegal, but may be punished according to the Medicines Act, when intended to be sold for human consumption or synthesis of GHB. In recent years, an increase of GBL consumption has been observed due to the prohibition of GHB.[citation needed]
  • Hong Kong: GBL is a dangerous drug controlled under Schedule 1 of the Dangerous Drugs Ordinance, Cap.134 (with exemption clause at Paragraph 16D). Any person who is found to have in his possession of it not in accordance with this Ordinance can be liable, on conviction upon indictment, a fine of HK$1,000,000 and to imprisonment for 7 years.[citation needed]
  • Israel: GBL was classified as a proscribed substance from 2007.[24]
  • Netherlands: GBL can be freely bought as a cleaning agent. Retailers do not need a licence to sell the substance.[25]
  • Poland: GBL is not classified as a drug and can be purchased in chemistry shops as a solvent.[citation needed]
  • Sweden: GBL is not classified as a drug but as a health-endangering substance. Although recently passed legislation to enter into force on 1 April 2011 will make it possible to handle narcotics for industrial purposes will enable GBL and 1,4-Butanediol to be classified as controlled substances.[26]
  • United Kingdom: Because of their legitimate uses, regulation 4B of the 2001 regulations makes it lawful to import, export, produce, supply, offer to supply or possess GBL and 1,4-BD. Except where a person does so knowing or believing that they will be used for the purpose of human ingestion.[27][28]
  • United States: GBL is regulated as a List 1 controlled chemical. As a GHB analog, it is treated as a controlled substance under Schedule I of the "Controlled Substances Act" if intended for human consumption.[29]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. 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)
  3. Detection of gamma-butyrolactone (GBL) as a natural component in wine
  4. https://www.gov.uk/government/uploads/system/uploads/attachment_data/file/100526/21-2009.pdf
  5. Development of a rational scale to assess the harm of drugs of potential misuse (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0140673607604644
  6. 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
  7. 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.
  8. 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
  9. Effects of subchronic administration of gammahydroxybutyrate (GHB) on spatial working memory in rats (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/17296081
  10. γ-Hydroxybutyric Acid–Induced Cognitive Deficits in the Female Adolescent Rat | http://onlinelibrary.wiley.com/doi/10.1196/annals.1432.044/abstract
  11. Neurotoxic effects induced by gammahydroxybutyric acid (GHB) in male rats | http://journals.cambridge.org/action/displayAbstract?fromPage=online&aid=6137924
  12. https://www.ncbi.nlm.nih.gov/pubmed/15582677 (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/15582677
  13. 13.0 13.1 GHB Withdrawal Syndrome | Texas Commission on Alcohol and Drug Abuse | https://www.erowid.org/chemicals/ghb/ghb_addiction2.pdf
  14. Systematic Assessment of Gamma Hydroxybutyrate (GHB) Effects During and After Acute Intoxication (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2759403/
  15. 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/
  16. https://www.ncbi.nlm.nih.gov/pubmed/11174231 | Gamma-hydroxybutyrate withdrawal syndrome.
  17. 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
  18. http://web.archive.org/web/20071203005230/http://www.aafs.org/pdf/Seattleabstracts06.pdf
  19. 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
  20. https://www.erowid.org/chemicals/ghb/ghb_health.shtml
  21. Suspicious death related to gamma-hydroxybutyrate (GHB) toxicity (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/15274975
  22. LAW AND JUSTICE LEGISLATION AMENDMENT (SERIOUS DRUG OFFENCES AND OTHER MEASURES) ACT 2005 NO. 129, 2005 - SCHEDULE 1 http://www.austlii.edu.au/au/legis/cth/num_act/lajladoaoma2005722/sch1.html
  23. Controlled Drugs and Substances Act (S.C. 1996, c. 19) http://laws-lois.justice.gc.ca/eng/acts/C-38.8/page-3.html
  24. section 7c of chapter B of part A of the 1st appendix of the Dangerous Drugs Act 1973 http://www.nevo.co.il/Law_word/law01/P170_001.doc
  25. "Verkopers schoonmaakmiddel verdienen fors aan partydrug GHB". Trouw (in Dutch). 11 April 2012. Retrieved 11 April 2012. 
  26. Socialutskottets betänkande 2010/11:SoU5 - Riksdagen
  27. http://www.gov.uk/government/uploads/system/uploads/attachment_data/file/100526/21-2009.pdf
  28. "UK Statutory Instrument 2011 No. 448". 2011-02-18. 
  29. Information Bulletin: GHB Analogs; GBL, BD, GHV, and GVL