Galantamine
Galantamine is a type of acetylcholinesterase inhibitor. It is an alkaloid extracted from the bulbs and flowers of Galanthus nivalis (common snowdrop), Galanthus caucasicus (Caucasian snowdrop), Galanthus woronowii (Voronov's snowdrop), and 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.
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| Trade names | Razadyne, Reminyl, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a699058 |
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| Routes of administration | By mouth |
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| Bioavailability | 80–100% |
| Protein binding | 18% |
| Metabolism | Liver partially CYP450:CYP2D6/3A4 substrate |
| Elimination half-life | 7 hours |
| Excretion | Kidney (95%, of which 32% unchanged), fecal (5%) |
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| ECHA InfoCard | 100.118.289 |
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| Formula | C17H21NO3 |
| Molar mass | 287.359 g·mol−1 |
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| Melting point | 126.5 °C (259.7 °F) |
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Galantamine is primarily known for its potential to slow cognitive decline. It is used clinically for treating early-stage Alzheimer's disease and memory impairments, although it has had limited success with the more advanced condition of dementia.
It works by increasing the amount of a type of neurotransmitter named acetylcholine by the inhibiting activity of enzyme called acetylcholinesterase known for breaking down acetylcholine. This elevates and prolongs acetylcholine levels boosting acetylcholine's neuromodulatory functionality, subsequently enhancing functionality of the various cognitions that acetylcholine is involved in, such as memory processing, reasoning, and thinking. It is a prescription drug taken orally and is also available over the counter. Galantamine may cause serious adverse effects, such as stomach bleeding, liver injury or chest pain.
Galantamine was isolated for the first time from bulbs of Galanthus nivalis (common snowdrop) in the Soviet Union in the 1940s. The active ingredient was extracted, identified, and studied, in particular in relation to acetylcholinesterase (AChE)-inhibiting properties. The first industrial process was developed in 1959. However, it was not until the 1990s when full-scale synthesis was upscaled and optimized.