What is Galantamine?
Galantamine (marketed as Lycoremine, Nivalin, Razdyne, and Reminyl) is an alkaloid originally derived from a number of plant sources (Galanthus woronowii, Narcissus, Leucojum, and Lycoris), most notably snow drops (a flower in the Amaryllis family). Now that the chemical structure is well known, it can also be produced in a lab. Virtually all galantamine produced is synthetic.
The active ingredient was isolated in the 1950s in the then USSR. Much of the early work on galantamine was done in the USSR and Japan. Scientific journal articles in English began to appear in the mid 1960s, and it was used to initially used to treat neuromuscular diseases. In 1977, the first scientific reports of its cognitive-enhancing abilities were published. However, it has been used as a folk medicine treatment against ‘old age’ in eastern European countries for much longer.
How does it work?
Classically, galantamine is known as a reversible acetylcholinesterase inhibitor. This class of drug propagates cholinergic transmission by preventing acetylcholinesterase from breaking down the acetylcholine in the synapse. Recent evidence suggests that galantamine is only a weak acetylcholinesterase inhibitor. However, it is also believed to bind to acetylcholine receptors and prevent receptor loss. Other acetylcholinesterase inhibitors don’t seem to share this property. In addition, some scientists hypothesize that galantamine has other effects on different neurotransmitter systems, including glutamate and γ-aminobutyric acid (GABA). It is thought that galantamine can modulate (increase) the effects of these neurotransmitters by interacting with their receptors. It also seems to increase the amount of dopamine in the synapse.
Most clinical research on the benefits of galantamine has been done in Alzheimer’s patients or older people with cerebrovascular insufficiency (compromised blood flow to the brain). One of the first brain regions affected in Alzheimer’ disease is called the nucleus basalis of Meynert, and it is powered by cholinergic transmission. The idea is that promoting this form of transmission with acetylcholinesterase inhibitors protects that part of the brain. In fact, several studies have demonstrated that galantamine significantly improves cognitive, functional, and behavioral symptoms of Alzheimer’s disease.
In theory, it should also promote cholinergic transmission in healthy people as well. Galantamine is reported to facilitate lucid dreaming. However, it is only available via doctor’s prescription.
Galantamine is also useful as an antidote against organophosphates and other nerve agents.
Galantamine Side Effects
Galantamine often causes upset stomach, especially when the body is acclimating to a new regimen. Other complaints associated with acetylcholinesterase inhibitors include vomiting, diarrhea, and abdominal pain. These are all due to the peripheral inhibition of acetylcholinesterase in the enteric nervous system that controls the gut. These side effects are usually mild and resolve after a few weeks. Doctors recommend that people continue to take the medication even if they experience these symptoms.
The compound is available as a tablet, an extended-release capsule, and a liquid solution that is added to water or juice. The tablets and liquid should be taken with morning and evening meals, and the extended-release capsules are typically taken once a day in the morning. Tablets are available in 4, 8, and 12 mg forms, and capsules are 8, 16, and 24 mg. When prescribed by a doctor, it is typical to be started on a low dose that is increased every four weeks, as needed.
Galantamine is rapidly absorbed and has an oral bioavailability of approximately 90%. Maximal system circulation levels are achieved in 1 hour for tablets and 4 hours for extended-release capsules. It should be taken with food and plenty of water to minimize nausea and upset stomach; having food in the stomach does not affect galantamine absorption. The elimination half-life is 7-8 hours. People with impaired kidney or liver function should be aware that they do not process galantamine as effectively, and might consider lower doses.
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Huang, Fenglei, and Yali Fu. “A Review of Clinical Pharmacokinetics and Pharmacodynamics of Galantamine, a Reversible Acetylcholinesterase Inhibitor for the Treatment of Alzheimer ‘s Disease, in Healthy Subjects and Patients.” Current Clinical Pharmacology 5.2 (2010): 115-24. Print.
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