Galantamine Hydrobromide is a benzazepine that is derived from the bulbs and flowers of Narcissus, Galanthus or norbelladine. It is also an oral cholinesterase inhibitor that acts as a ligand for nicotinic acetylcholine receptors and has widely been used for enhancing neurocognitive functions. It works by competitively and reversibly inhibiting acetylcholinesterase, thus elevating the concentration of acetylcholine. (1)
When taken orally, Galantamine Hydrobromide is well absorbed with a bioavailability of more than 90%. The peak effects of the supplement are achieved after one hour, and it takes about 7 hours for total elimination. When taken with food, there is some delay in absorption, although that does not affect the final total absorption of the active compounds. (2)
When absorbed in the bloodstream, Galantamine Hydrobromide is readily taken up in all areas of the body, including the brain. It binds to the nicotinic acetylcholine receptors causing conformational changes which result in an increase in the amount of acetylcholine released. It also works by competing against and reversing the actions of cholinesterase inhibitors. By inhibiting cholinesterase, it prevents the breakdown of acetylcholine, thereby increasing both the levels and duration of the effects of this powerful neurotransmitter. (3)
Basically, Galantamine Hydrobromide works on two different sides of the acetylcholine equation.
One of the most popular reasons why people use Galantamine Hydrobromide is the possibility of experiencing lucid dreaming and ease of sleep after a stressful day. When in a lucid dreaming state, one is usually aware of what they are dreaming. The dreamer may also have some control of the dream characters, the narrative, and the environment. However, it isn’t absolute that the dreamer should take control of the dream, for it to be a lucid dream, but simply conscious awareness that it is a dream. (4) Simply said, lucid dreaming is an opportunity to play around with the extraordinary abilities of the unused parts of the brain.
The primary cognitive process that makes it possible for lucid dreaming is the working memory, also known as short-term memory. It is understood that acetylcholine influences memory, the perception of one’s sense and muscle control. Moreover, acetylcholine is the primary neurotransmitter at work during rapid eye movement (REM) phase of sleep. (5) As previously mentioned, Galantamine Hydrobromide increases the level and action time of acetylcholine, thus extends REM sleep, increasing dream activity. That provides a conducive environment for lucid dreaming. (6)
Another valued effect of Galantamine Hydrobromide is its ability to enhance memory function. It increases the rate at which memories are formed and improves retention of details and facts. The aspects of memory that are improved are both for short and long-term memory. Experts believe that this long-term effect is both due to enhancing the levels of acetylcholine and modulating the effect of nicotinic receptors. (7) Nicotinic cholinergic systems are involved in learning and memory in the hippocampus and frontal cortex regions as they enhance afferent input to these areas. (8) Acetylcholine as a neurotransmitter helps in encoding new memories by acting as the messenger that increases the activity and communication of cortical neurons. (9)
Because of the benefit of improving memory, Galantamine Hydrobromide is not only used by those seeking to keep their cognition intact but also those experiencing memory loss. In fact, in the US, Galantine is licensed as a drug for treating mild to moderate dementia associated with Alzheimer’s disease. (10) One of the features of Alzheimer’s is that the affected brain has lower than normal levels of acetylcholine, due to degeneration of neurons.
Modulation of synaptic functions including the formation of new neurons is a neural aspect of the brain that is quite critical in learning and memory. Think about it this way; neurons communicate through connections (synapses). These synapses can control the strength of signals according to the number of stimuli received during a learning process. The unfortunate thing is that these synapses and neurons are prone to damage by various factors ranging from environmental factors, inflammation to oxidative damage. The good thing is that the brain can regenerate new neurons, but this ability declines as age sets in. Consequently, the ability to learn and retain new information goes down.
Galantamine Hydrobromide affects neuroplasticity both directly and indirectly. Directly, it stimulates synaptic plasticity by activating microglia and astrocytes. These cells support the blood-brain barrier, provide nutrients to neurons and repair damaged nervous tissue. Indirectly, regular use of Galantamine Hydrobromide prevents damage of neurons by acting as an anti-inflammatory agent. (11) It inhibits tumor necrosis factor a (TNF-α) which is one of the cytokines involved in early inflammatory events. Galantamine also significantly attenuates the decline in pre- and post-synaptic proteins, thus protecting dendritic branching and maintaining neuron branch length.
These mechanisms induce cognitive improvement including learning and memory, and at the same time prevent cognitive deficits.
Galantamine improves the quality of sleep by increasing the ease with which sleep occurs through provoking earlier onset of REM sleep. (12) During sleep, first comes the non-REM sleep which is characterized by light sleep, slow heartbeat, breathing, eye movements and muscle relaxation with occasional twitching. In the later stages, non-REM sleep is responsible for deep sleep that is needed for a refreshed morning.
REM sleep follows 90 minutes after falling asleep. It occurs several times during sleep and accounts for about 25% of the sleep cycle. During this phase, the brain and body are usually energized, eyes move from side to side with closed eyelids, breathing gets fast and regular, the heart rate increases and the body gets near to a waking level. However, the muscles become temporarily paralyzed to impede movement when dreaming.
Among the indicators of good sleep are a sleep latency (time it takes to fall asleep) of less than 30 minutes, awakenings per night, wake after sleep onset, and duration of REM and non-REM phases. Other than easing the onset of sleep, Galantine Hydrobromide also allows the body to relax faster, increases REM density and reduces slow-wave sleep in the non-REM cycle. (14)
The REM phase is also thought to be involved in the processes of memory formation, learning, and balancing mood. (13) Therefore, Galantamine also improves cognition by increasing REM intensity.
Galantamine Hydrobromide is available as both a prescription and an over-the-counter supplement to be taken twice or once daily. It is quite a powerful nootropic; thus, one does not have to take too much of it. The general dosage recommendation lies between 4 and 16mg, and a maximum of 24mg per day. Since everybody has different body chemistry, it is best to start with the lowest effective dose then move up. If taking in divided dosages throughout the day, it should be spaced for at least 7 to 8 hours, considering its half-life.
When used for lucid dreaming, a “wake then get back to bed” strategy is highly recommended. It involves sleeping for a few hours (4 to 6 hours), then waking up to take the supplement and getting back to sleep. At that point of sleep, there are high acetylcholine levels, and within an hour of taking the supplement, the levels are further boosted. This strategy lowers the possibility of getting nightmares or reduced sleep quality, as compared to when one takes the supplement just before bed. Most users are able to achieve lucid dreams with doses from 4 to 8mg, but one can go as high as 16mg. (15)
Although Galantamine Hydrobromide is well-tolerated by most users, some people may experience some minor side effects including loss of appetite, fatigue, nausea, headaches, and diarrhea. (16) Allergic reactions are rare, but still possible for people with flower allergies. An allergic reaction is characterized by a sudden rash, itchiness, swelling of the mouth, difficulty in breathing and redness.
Galantamine Hydrobromide is commonly stacked with cholinergic supplements such as Alpha GPC and CPD choline or Racetam nootropics like piracetam. They act synergistically to increase the levels of acetylcholine.
Studies of usage of Galantamine Hydrobromide for modern use started in the 1950s, in the Soviet Union. It was first isolated from bulbs of Galanthus nivalis, commonly known as snowdrop, by a Bulgarian chemist known as D. Paskov. When the active substance was extracted, it was widely studied in relation to its use as an acetyl-cholinesterase (AChE) inhibitor. When its effectiveness was proved, it was industrially processed in 1959. (17)
Since then, Galantamine Hydrobromide has been used in other countries other than Russia, including Eastern Europe and the United Kingdom. In the USA, Galantamine Hydrobromide was approved by the Food and Drug Administration (FDA) in 2001 as a safe and effective supplement to improve cognition, and especially memory loss.
In Greek mythology, a poet tells a story where a god Hermes, gave Odysseus a herb known as moly, which has a black root and a milk-like flower. The god claimed that the herb would make Oddyseus immune to a sorcerer’s drugs, which were an extract from Datura Stramonium, commonly referred to as jimsonweed (causes memory loss and delirium). In modern translations, the moly herb is believed to be Galanthus nivalis (acetylcholinesterase inhibitor), which formed the antidote for the sorcerer’s drug, Datura Stramomium (an anticholinergic). (18)
Finally, Galantamine Hydrobromide is a nootropic supplement that has remarkable ability to improve memory, even in individuals that have already suffered specific degenerative cognitive disorders. It increases the rate of memory formation, improves retention of facts, enhances focus, mental processing and reasoning. Here is a review of all that has been discussed in this article.
Galantamine Hydrobromide is a cholinesterase inhibitor that is obtained from bulbs of flowers of plants from the Galanthus family, hence its name. It can also be found in Narcissus flowers, red spider lily, or norbelladine.It was first isolated in the Soviet Union, by a chemist known as D. Paskov. However, it had been used for centuries by various cultures before it was officially discovered.It works by inhibiting the actions of acetylcholinesterase, an enzyme that breaks down acetylcholine into acetate and choline. By doing so, it increases the level and action time of acetylcholine, a neurotransmitter that is involved in many facets of brain activity, cognitive functions, memory, and concentration.Increases the possibility of experiencing lucid dreams by extending the duration of REM sleep cycle, expanding the state of awareness and influencing short-term memory.On sleep, it also improves quality of sleep by promoting body relaxation, shortening the REM latency, increasing REM density and reducing the slow wave phase in non-REM phase.Improves memory by stimulating nicotinic receptors and through the action of acetylcholine as a chemical messenger. For this reason, it has been licensed in the US as a drug for mild to moderate dementia.Galantamine also improves the ability of learning and memory by maintaining the integrity of neurons and synapses, preventing inflammation in the brain and sustaining high levels of neurotransmitters.Typical doses of Galantamine Hydrobromide range between 4 and 24mg. These doses are well-tolerated, but some people may experience mild gastrointestinal discomfort, headaches, and dizziness in the initial days of use.