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Talk:Baclofen
Revision as of 18:11, 20 June 2019 by >Tracer(Question)
I have doubts that baclofen is a gabapentinoid. Although it blocks α2δ subunits, unlike other gabapentinoids (phenibut, gabapentin and pregabalin), the actions of baclofen on α2δ subunit-containing VGCCs are likely not clinically-relevant. What do you think about it? --Tracer (talk) 20 June 2019 (UTC)
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
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.
Baclofen was synthesized in 1962 at Ciba-Geigy, a Swiss pharmaceutical company.[3] Today, it is used clinically to treat muscle spasticity, and holds promise as a treatment for alcoholism.[4]
Baclofen was synthesized in 1962 by Heinrich Keberle at Ciba (pharmaceutical company) in Basel, Switzerland, based on the idea of enhancing the lipophilicity of GABA in order to achieve penetration of the blood-brain barrier.[3] It was marketed as Lioresal in 1972.[3]
In his 2008 book, Le Dernier Verre (translated literally as "The Last Glass" and published in English as "The End of my Addiction"), French-American cardiologist Olivier Ameisen described how he treated his alcoholism with baclofen. Inspired by this book, an anonymous donor gave $750,000 to the University of Amsterdam to initiate a clinical trial of high-dose baclofen, which Ameisen had called for since 2004.[5]
Chemistry
As with phenibut, baclofen is a derivative of γ-aminobutyric acid (GABA), except with a chlorine-substituted phenyl group in the β-position of the molecule. It is a chiral molecule and thus has two potential configurations as (R)- and (S)-enantiomers. It has an almost identical chemical structure to F-phenibut (only replacing a fluorine with a chlorine atom in the para-position of the phenyl group).
Pharmacology
Baclofen produces its effects by activating the GABABreceptor, similar to the drug phenibut which also activates this receptor and shares some of its effects. Baclofen is postulated to block mono-and-polysynaptic reflexes by acting as an inhibitory ligand, inhibiting the release of excitatory neurotransmitters.
Similarly to phenibut (β-phenyl-GABA), as well as pregabalin (β-isobutyl-GABA), which are close analogues of baclofen, baclofen (β-(4-chlorophenyl)-GABA) has been found to block α2δ subunit-containing voltage-gated calcium channels (VGCCs). However, it is weaker relative to phenibut in this action (Ki = 23 and 39 μM for R- and S-phenibut and 156 μM for baclofen). Moreover, baclofen is in the range of 100-fold more potent by weight as an agonist of the GABAB receptor in comparison to phenibut, and in accordance, is used at far lower relative dosages. As such, the actions of baclofen on α2δ subunit-containing VGCCs are likely not clinically-relevant.[6]
Subjective effects
In comparison to other commonly used GABAergic depressants such as alcohol or benzodiazepines, baclofen is reported to be longer lasting, more euphoric and more recreational at higher doses.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWikicontributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects
Stimulation and Sedation - Baclofen has different effects on physical energy levels depending on the dosage used. At lower doses, baclofen has a mild physical and mental stimulation effect, encouraging movement, wakefulness, and productivity. At common doses and higher, phenibut is physically sedating, encouraging sleep and lethargy.
There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
This toxicity and harm potential section is a stub.
As a result, it may contain incomplete or even dangerously wrong information! You can help by expanding upon or correcting it. Note: Always conduct independent research and use harm reduction practices if using this substance.
Baclofen is moderately physically and psychologically addictive. Discontinuation of baclofen can be associated with a withdrawal syndrome which resembles benzodiazepinewithdrawal and alcohol withdrawal. Withdrawal symptoms are more likely if baclofen is used for long periods of time (more than a couple of months) and can occur from low or high doses. The severity of baclofen withdrawal depends on the rate at which it is discontinued. Abrupt withdrawal is more likely to result in severe withdrawal symptoms. Acute withdrawal symptoms can be stopped by recommencing baclofen.[8]
Baclofen produces cross-tolerance with [[Cross-tolerance::all GABAgenic depressants]], meaning that after its consumption, depressants will have a reduced effect.
Dangerous interactions
Warning:Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).
Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.
Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and dying from the resulting suffocation. If a sudden loss of consciousness occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
Stimulants - It is dangerous to combine baclofen with stimulants due to the risk of excessive intoxication. Stimulants mask the sedative effect of phenibut, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of baclofen will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of baclofen per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.
↑Agarwal, S. K., Kriel, R. L., Cloyd, J. C., Coles, L. D., Scherkenbach, L. A., Tobin, M. H., Krach, L. E. (January 2015). "A pilot study assessing pharmacokinetics and tolerability of oral and intravenous baclofen in healthy adult volunteers". Journal of Child Neurology. 30 (1): 37–41. doi:10.1177/0883073814535504. ISSN1708-8283.
↑ 3.03.13.2Froestl, Wolfgang (2010). "Chemistry and Pharmacology of GABAb Receptor Ligands". In Blackburn, Thomas P. (ed.). GABAb Receptor Pharmacology – A Tribute to Norman Bowery. Advances in Pharmacology. 58. pp. 19–62. doi:10.1016/S1054-3589(10)58002-5. ISBN 978-0-12-378647-0. PMID 20655477.
↑Enserink, M. (2011). "Anonymous Alcoholic Bankrolls Trial of Controversial Therapy". Science. 332 (6030): 653. doi:10.1126/science.332.6030.653. PMID 21551041.
↑R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26234470
↑A pilot study assessing pharmacokinetics and tolerability of oral and intravenous baclofen in healthy adult volunteers. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/25028414
↑Koski, A., Ojanperä, I., & Vuori, E. (2002). Alcohol and benzodiazepines in fatal poisonings. Alcoholism: Clinical and Experimental Research, 26(7), 956-959.
