Approved For Treatment of Alzheimer’s Disease
Synthetic galantamine was first registered for the treatment of Alzheimer's disease in Sweden in 2000. After that, approval came swiftly in the European Union, the United States, Canada, Japan, and many other countries around the world. The principal purpose in using it for Alzheimer’s disease is because it acts as a cholinesterase inhibitor.The Memory-Saving Strength of Cholinesterase Inhibitors
A key neurotransmitter in the brain is acetylcholine. It has many important roles including the retention of memory, attention, and concentration. In Alzheimer's, acetylcholine is in short supply. The principal enzyme that breaks down acetylcholine in the brain is called acetylcholinesterase. By limiting the activity of this enzyme, more acetylcholine is available for communication between brain cells. This can stabilize or improve symptoms of dementia, at least for a time. Drugs that do this are called cholinesterase inhibitors (ChEIs), of which galantamine is one. Few studies have ever examined whether ChEIs are helpful for Alzheimer’s patients beyond one year, so a longer trial was conducted by scientists at the Karolinska Institute in Sweden.Galantamine Is The Top Performer
The researchers compared 11,652 mild to moderate Alzheimer’s patients taking any one of three ChEIs - donepezil, rivastigmine, and galantamine - with a carefully matched group of 5,826 Alzheimer’s patients that were not prescribed any of these drugs. Scores were available for each participant for a widely used test of cognitive function, the Mini-Mental State Exam (MMSE). This was carried out within three months of the first drug prescription and repeated annually. After five years, 255 patients developed severe Alzheimer’s disease, and 6,055 died. The findings of the study were that those taking ChEIs had higher (better) MMSE scores at each visit compared to non-users, as well as a 27 percent lower risk of death. Galantamine was the only ChEI that demonstrated a significant reduction in the risk of developing severe dementia. It also had the strongest effect on cognition and provided the biggest mortality risk reduction.Nicotine Plays a Role
The scientists believe the reason it outperformed the other ChEIs is because it’s the only one of the three that acts on nicotinic receptors. These work with acetylcholine to trigger more rapid nerve transmission. While this may sound strange, research over the last decade has shown that targeting nicotinic receptors is beneficial for memory loss and, if these receptors are blocked, this prevents the memory loss associated with Alzheimer’s disease. Neurobiologist Maria Eriksdotter, who led the study, said, "Our results provide strong support for current recommendations to treat people with Alzheimer's disease with cholinesterase inhibitors, but also shows that the therapeutic effect lasts for a long time.” More than 90 clinical trials have evaluated galantamine's effect on Alzheimer's and other conditions. Overall, they find a consistent symptomatic benefit on cognition and clinical measures in patients with Alzheimer’s disease following several years of treatment; however, as with all cholinesterase inhibitors, researchers believe that, on average, galantamine's effect is small. But that may be about to change…Synthetically Modified vs. Natural Galantamine
Kevin Stephens, a former sheep farmer and owner of Agroceutical Products which grows the daffodils, claims the galantamine drugs have nasty side effects. For example, there are studies linking synthetically modified galantamine to heart health complications. On the other hand, naturally derived galantamine, as well as being less toxic, is also thought to have a wider range of activities. Some researchers believe it is a stronger cholinesterase inhibitor than synthetic galantamine. Currently, Agroceutical Products can only produce enough of the daffodil-derived version to treat 9,000 patients a year, but hopes this will rise to 450,000 patients as they ramp up production. Of course, it will take a future study to see whether the naturally derived version of galantamine really is safer and more effective than the synthetic version used in the research. Meanwhile, synthetically-modifed Galantamine is available as a tablet, as solution, and, since 2005, as a once-daily extended-release capsule with the trade name RazadyneTM. Since then, several generic equivalents have been approved by the FDA.