Galantamine

Summary sheet: Galantamine

Galantamine
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
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 Bioavailability 90% Threshold 1 mg Light 4 - 8 mg Common 8 - 16 mg Strong 16 - 24 mg Heavy 24 mg + Duration Total 6 - 12 hours Onset 20 - 60 minutes 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.
Interactions

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. 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. 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.

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). 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. By binding to the allosteric site of the nAChRs, a conformational change occurs which increases the receptors response to acetylcholine. This modulation of the nicotinic cholinergic receptors on cholinergic neurons in turn causes an increase in the amount of acetylcholine released. However, recent studies suggest that Galantamine does not functionally act at human nAChRs α₄β₂ or α₇ as a positive allosteric modulator. 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.

Galantamine also works as a weak competitive and reversible cholinesterase inhibitor in all areas of the body. 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

• • 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

• • Drifting
  • Colour enhancement

Cognitive effects

• • Cognitive euphoria
  • Dream potentiation
  • Memory enhancement
  • Sleepiness

Auditory effects

• • Distortions
  • Hallucinations

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:

• Erowid Experience Vaults: Galantamine

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

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.
• Switzerland: Galantamine is listed as a "Abgabekategorie B" pharmaceutical, which generally requires a prescription.

See also

• Citicoline
• Choline
• Nootropic

External links

• Galantamine (Wikipedia)
• Galantamine (Isomer Design)
• Galantamine (Drugs.com)