Galantamine
| Summary sheet: Galantamine |
| Galantamine | |||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||
| Common names | Galantamine | ||||||||||||||||||||||||||
| Systematic name | (4aS,6R,8aS)-5,6,9,10,11,12-Hexahydro-3-methoxy-11-methyl-4aH-[1]benzofuro[3a,3,2-ef][2]benzazepin-6-ol | ||||||||||||||||||||||||||
| Class Membership | |||||||||||||||||||||||||||
| Psychoactive class | Nootropic / Oneirogen | ||||||||||||||||||||||||||
| Chemical class | Benzazepine | ||||||||||||||||||||||||||
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Galantamine (also known as Nivalin, Razadyne, Razadyne ER, Reminyl, and Lycoremine) is a water soluble, reversible, competitive acetylcholinesterase inhibitor that functions as a nootropic, oneirogen, and mild dissociative substance. It is well known and used widely as a dream potentiator. Along with its oneirogenic effects, it has stimulant and nootropic effects in low doses, and has mild dissociative effects in higher doses. It is an alkaloid that is obtained either synthetically, or from the bulbs and flowers of Galanthus caucasicus, Galanthus woronowii and related genera.[2] It is also available in both a prescription form and as an over-the-counter supplement.
Studies of usage in modern medicine began in the Soviet Union in the 1950s by Soviet pharmacologists M. D. Mashkovsky and R. P. Kruglikova–Lvova.[3] The active ingredient was extracted, identified, and studied, particularly in relation to its mechanism of action. Galantamine has been used for decades in Eastern Europe and Russia for the treatment of various conditions such as myasthenia, myopathy, and sensory and motor dysfunction associated with disorders of the central nervous system. In the United States, it is FDA approved for the treatment of Alzheimer's disease.[4]
More recently, galantamine has been popularized in supplement groups for its ability to improve dream recall and facilitate lucid dreaming. It is commonly recommended to be taken 30 minutes to one hour before bed.
Chemistry
Galantamine's chemical structure contains a tertiary amine. It is a complex alkaloid that is found endogenously in certain plants or is synthesized for medical use. It is comprised of a fusion between a methoxy substituted benzene ring to a hydrogenated and methylated azepine ring along with a hydroxylated benzofuran group.
The alkaloid has been isolated from the bulbs and flowers of Galanthus nivalis (Common snowdrop), Galanthus caucasicus (Caucasian snowdrop), Galanthus woronowii (Voronov's snowdrop), and some other members of the family Amaryllidaceae, such as Narcissus (daffodil), Leucojum aestivum (snowflake), and Lycoris including Lycoris radiata (red spider lily).[2] It can also be produced synthetically.
Pharmacology
Galantamine, a tertiary alkaloid, is a competitive and reversible inhibitor of acetylcholinesterase. Is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through inhibiting acetylcholinesterase, a neurochemical responsible for breaking down acetylcholine. Higher concentrations of acetylcholine have also been linked to higher levels of cognition and focus.
Galantamine is a potent allosteric potentiating ligand of human nicotinic acetylcholine receptors (nAChRs) α4β2, α3β4, and α6β4, and chicken/mouse nAChRs α7/5-HT3 in certain areas of the brain.[5] By binding to the allosteric site of the nAChRs, a conformational change occurs which increases the receptors response to acetylcholine.[6] This modulation of the nicotinic cholinergic receptors on cholinergic neurons in turn causes an increase in the amount of acetylcholine released.[7] However, recent studies suggest that Galantamine does not functionally act at human nAChRs α4β2 or α7 as a positive allosteric modulator.[8] Galantamine also provides potentiation of NMDA-receptor antagonists such as Memantine and Ketamine, and may directly antagonize these receptors in high doses, which is responsible for galantamine's mild dissociative effects.[9]
Galantamine also works as a weak competitive and reversible cholinesterase inhibitor in all areas of the body.[5] By inhibiting acetylcholinesterase, it increases the concentration and thereby action of acetylcholine in certain parts of the brain. Galantamine's effects on nAChRs and complementary acetylcholinesterase inhibition make up a dual mechanism of action. It is hypothesized that this action might relieve some of the symptoms of Alzheimer's.
Subjective effects
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 PsychonautWiki contributors. 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 
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- Stimulation - Galantamine is primarily stimulating and provides nootropic effects.
- Physical fatigue
- Dizziness
- Headaches
- Nausea - When taken by itself on an empty stomach, Galantamine has a wide range of unpleasant side effects related to digestion. These effects are less pronounced when taken sublingually or with food.
- Dehydration
- Dizziness
- Sleep paralysis
Visual effects 
Cognitive effects 
Auditory effects 
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
Galantamine is non-addictive, is not known to cause harm in reasonable doses, and has an extremely low toxicity relative to dose. Various studies have shown that in reasonable doses in a careful context, it presents few negative cognitive, psychiatric or toxic physical consequences, though some exist.
It is strongly recommended that one be familiar with harm reduction practices when using this drug.
Tolerance and addiction potential
Galantamine is not known to be not habit-forming and the desire to use it can actually decrease with use. It is most often self-regulating.
Galantamine does not seem to build up an immediate tolerance, and, due to its long half life, becomes stronger with prolonged use. Caution should be heeded when taking galantamine for extended periods longer than two weeks. Galantamine presents cross-tolerance with no other known compounds, meaning that after the consumption of Galantamine all other psychoactive compounds will not have a reduced effect.
Legal status
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This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
- Germany: Galantamine is a prescription medicine, according to Anlage 1 AMVV.[10]
- Switzerland: Galantamine is listed as a "Abgabekategorie B" pharmaceutical, which generally requires a prescription.[citation needed]
See also
External links
References
- ↑ Farlow, M. R. (2003). "Clinical pharmacokinetics of galantamine". Clinical Pharmacokinetics. 42 (15): 1383–1392. doi:10.2165/00003088-200342150-00005. ISSN 0312-5963.
- ↑ 2.0 2.1 NNFCC Project Factsheet: Sustainable Production of the Natural Product Galanthamine (Defra), NF0612 — NNFCC, 2016
- ↑ PJ Online, Christmas 2004 (Snowdrops: the heralds of spring and a modern drug for Alzheimer’s disease), News, Pharmaceutical Journal, 2016
- ↑ Galantamine: MedlinePlus Drug Information
- ↑ 5.0 5.1 "Galantamine". Drugs.com. https://www.drugs.com/mtm/galantamine.html
- ↑ Raskind, M. A., Peskind, E. R., Wessel, T., Yuan, W., the Galantamine USA Study Group (27 June 2000). "Galantamine in AD: A 6-month randomized, placebo-controlled trial with a 6-month extension". Neurology. 54 (12): 2261–2268. doi:10.1212/WNL.54.12.2261. ISSN 0028-3878.
- ↑ Woodruff-Pak, D. S., Vogel, R. W., Wenk, G. L. (13 February 2001). "Galantamine: Effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning". Proceedings of the National Academy of Sciences. 98 (4): 2089–2094. doi:10.1073/pnas.98.4.2089. ISSN 0027-8424.
- ↑ Moerke, M. J., McMahon, L. R., Wilkerson, J. L. (April 2020). "More than Smoke and Patches: The Quest for Pharmacotherapies to Treat Tobacco Use Disorder". Pharmacological Reviews. 72 (2): 527–557. doi:10.1124/pr.119.018028. ISSN 1521-0081.
- ↑ Lopes, J. P., Tarozzo, G., Reggiani, A., Piomelli, D., Cavalli, A. (March 2013). "Galantamine potentiates the neuroprotective effect of memantine against NMDA-induced excitotoxicity". Brain and Behavior. 3 (2): 67–74. doi:10.1002/brb3.118. ISSN 2162-3279.
- ↑ Anlage 1 AMVV - Einzelnorm