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Galanthamine HBr

From: Peter Lau
Category: ÉÌƷתÈÃ
Date: 8/13/2003
Time: 8:13:26 AM
Remote Name: 220.168.13.187

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Galanthamine HBr manufacturer

Peter Lau

sales@organic-herb.com

Galanthamine HBr manufacturer

Peter Lau

sales@organic-herb.com

Galanthamine Hydrobromide OHI

Product Name: Galanthamine Hydrobromide

Plant Origin: Lycorts radiate

Plant Part Used: Rhizoma

Molecular formula: C17H21NO3HBr

Molecular weight: 368.27

Structure formula:

Appearance: Fine white powder

Solubility: Soluble in water slight soluble in alcohol, insoluble in acetone chloroform ether and benzene.

Melt Point: 126¡æ-127¡æ

Plant Picture:

Review of the acetylcholinesterase inhibitor galanthamine.

Sramek JJ, Frackiewicz EJ, Cutler NR

California Clinical Trials, 8501 Wilshire Boulevard, 2nd Floor Beverly Hills, CA 90211, USA. Expert Opin Investig Drugs 2000 Oct;9(10):2393-402

ABSTRACT

Galanthamine (or galantamine, Reminyl) is a tertiary alkaloid acetylcholinesterase inhibitor (AChEI) which has been approved in several countries for the symptomatic treatment of senile dementia of the Alzheimer's type. Derived from bulbs of the common snowdrop and several Amaryllidaceae plants, (-)-galanthamine (GAL) has long been used in anaesthetics to reverse neuromuscular paralysis induced by turbocurarine-like muscle relaxants and more recently, has been shown to attenuate drug- and lesion-induced cognitive deficits in animal models of learning and memory. Galanthamine directly inhibits acetylcholinesterase activity, while demonstrating much weaker activity on butyrylcholinesterase (BuChE). Galanthamine also stimulates pre- and postsynaptic nicotinic receptors, although the clinical significance of this finding is yet unclear. Numerous variants and analogues of galanthamine have also been developed, with varying potency in inhibiting AChE activity. Galanthamine is readily absorbed after oral administration, with a t(max) of 52 min and a plasma elimination t(1/2) of 5.7 h. The efficacy of galanthamine administered to Alzheimer's disease (AD) patients has been well demonstrated by large-scale clinical trials. Typical of AChEIs, the most common adverse events associated with galanthamine are nausea and vomiting. In conclusion, evidence to date suggests galanthamine to be similar to other AChEIs in improving cognitive function in Alzheimer's disease patients.

Galantamine is a Safe, Effective, and Natural Plant Product Galantamine Rescues Brain Cells

Now the news! Another drug has been found to be safe and effective. Big deal. That's not news. But why do we never hear this pronouncement applied to anything else? Such as . . .

A food is safe and effective A nutrient supplement is safe and effective A sexual practice is safe and effective If studies were published finding that these statements were scientifically tenable, would you then believe that it's safe to eat or take a vitamin or have sex? Do we need the FDA to set recommended daily allowances for our dinner, our vitamins, and our acts of love? Do we want them in our kitchens, our bathrooms, and our bedrooms? Where do we draw the line? For certain, if the FDA had its way, everything would be a drug, and "everything not permitted would be forbidden."

IS LIFE SAFE AND EFFECTIVE? Consider another headline: Life has been found to be safe and effective. We certainly know that this is not true. Life is conditional. It is not guaranteed. And until some undetermined time in the future, life will end for each and every one of us. So how can it be safe and effective? Can food - the staff of life - be safe and effective? Can nutrients - essential to life - be safe and effective? And again, what about sex? The safety of food or supplements or sex must be judged on its own merit. Also, who should be the judge?

Yet we are led to believe and not question that drugs, especially when approved by a federal agency, can be pronounced as "safe and effective." There are certainly things that are safe and certainly things that are effective, but there are a great many circumstances surrounding every issue, and a governmental body, subject as it is to political persuasion and consideration, is not an appropriate judge.

Obviously, drug standards are not the same as those we use to judge whether food, for example, is safe and effective. If we fail to distinguish the difference between the drug standard and the food standard, we are pulling the wool over our eyes, or giving others permission to do just that.

GALANTAMINE IS SAFE AND EFFECTIVE According to a recent paper in the British Medical Journal (BMJ) reporting on a study of 653 Alzheimer's disease patients, galantamine "appears to slow the progression of the neurodegenerative condition" and is "safe and effective."1 Now this isn't the FDA speaking, but the authors of the latest double-blind, placebo-controlled research on galantamine, including a British professor, a director of research at a pharmaceutical company, and a statistician (also with a pharmaceutical company), all in league with the Galantamine International-1 Study Group.

The BMJ study lasted for 6 months, at the end of which the patients receiving the phytonutrient (plant-derived nutrient) galantamine were found to be better off than those receiving placebo. Galantamine (taken at either 24 or 32 mg/day) resulted in significantly higher cognitive scores. There was little difference between the two doses in this regard. In the same study, an additional measure of the efficacy of galantamine was evaluated through interviews by clinicians who confirmed the perception of its effectiveness.

GALANTAMINE IS AN HERB, NOT A DRUG There have been several other large-scale, multicenter studies of galantamine in the last few years that have found similar results.2 So the BMJ research is not the first study to arrive at the clear finding that galantamine is effective. However, to the study's discredit, its authors make the following statement:

Galantamine is a new drug that reversibly and competitively inhibits acetylcholinesterase and enhances the response of nicotinic receptors to acetylcholine.

While presumably valid as a conclusion about the mechanism of galantamine, this statement is misleading because galantamine is a plant extract and not a synthetic drug. The Merck Index indicates that galantamine is an unaltered extract from the Caucasian snowdrop plant, Galanthus wornorii. In the earliest reference to galantamine in Medline's Index Medicus, it is referred to as a "medical plant."3 Even further back in Old Medline, galantamine is referred to as an herb and a plant4,5 with many references to its sources as extracts from a wide variety of plants.6,7,8

The Bulgarian Pharmaceutical Industry, where the modern use of galantamine originated back in the 1950s, refers to it on its Web site as a "natural substance,"13 in a column that distinguishes it from pharmaceuticals and phytochemicals. If it's natural and it's not a chemical or a pharmaceutical, how can it be a drug?

MEDICAL ESTABLISHMENT TRYING TO PASS OFF GALANTAMINE AS A DRUG Strangely, there is not one word in the text of the BMJ paper that gives a clue that the "drug" galantamine is extracted unchanged from plants and thus is a natural substance. Only a very studious reader can grasp that it is a plant extract and not a drug. That is, there are no clues in the titles of the references and only 3 out of 35 references have any keywords that suggest or mention plants, extracts, herbs, or indeed any origin or source for galantamine. Moreover, the text of the entire BMJ article does not mention the words extract, plant, herbs, herbal, phytonutrient, natural, or any of the common or Latin names of the plants from which galantamine has been extracted - not once. Yet the word drug is used again and again. Why?

DRUGS ARE MORE PROFITABLE THAN HERBS AND MORE EXPENSIVE TOO A tool found valuable for understanding questions of motives is Cui bono (whose interest is served?). The projected estimate for galantamine sales in the United States for the first year - if made available and marketed as a drug rather than as a dietary supplement - could approach $1.5 billion. This doesn't suggest that there is a conspiracy to defraud the public or the doctors and other professionals who read the BMJ, but merely it provides drug companies with the opportunity to presell the idea of galantamine as a drug that can be obtained only by prescription. Thus, the establishment of an exclusive franchise on galantamine, in effect a monopoly, can dictate price structure.

The medical establishment recognizes the importance of establishing the effectiveness of galantamine. They want it so bad because it is so good. But they can't have it unless it is declared "safe and effective," a phrase necessary to assure successful marketing and use of a drug, and the phrase "safe and effective" has been coopted and monopolized by the FDA, an agency highly subject to political correctness.

If, on the other hand, galantamine is classified as a phytonutrient - and thus grandfathered in by the Dietary Supplement Health and Education Act (DSHEA) of 1994 because it was sold as a dietary supplement before that law's date of enactment - then its fate will be very different. Galantamine would be widely available and far less expensive.

Galantamine may still become a blockbuster, but instead of one pharmaceutical company having a monopoly on it, it is highly probable that it will be sold by many nutrient companies. Furthermore, through broad-spectrum marketing, galantamine is likely to be not only less expensive, but more accessible, better explained, and of higher potential standards - believe it or not. Who loses by restricting availability and driving prices higher for a naturally safe and effective product? Many of those who need it most.

GALANTAMINE TARGETS ACETYLCHOLINE DEFICIENCY Alzheimer's disease is a devastating disorder with progressive dementia as its hallmark. The disease is characterized by protein plaques and nerve tangles that gradually distort the architecture of the brain. A naturally occurring protein, amyloid, has been implicated as a key player in the destructive process, but the primary dysfunctionality is attributed to the loss of availability and activity of the neurotransmitter acetylcholine (ACh).

If the studies about galantamine are what they appear to be, galantamine is one of the best - if not the best - treatments yet discovered for age-related memory impairment, decline, and dementia progressing to Alzheimer's disease. But the connection is not new, and its effect as a acetylcholinesterase (AChE) inhibitor and for treatment of the central nervous system was suggested at least as far back as 1960,10-11 and for memory loss back in 1972.12

Galantamine takes the ACh deficiency head-on by inhibiting the production of AChE that breaks down ACh. It also enhances the brain's response to ACh, which is directly linked to memory maintenance. In the study, out of 653 patients diagnosed with mild to moderate Alzheimer's disease, approximately half received galantamine while the other half received a placebo. Galantamine was found to be well tolerated and effective, slowing the decline of functional ability as well as cognition.

According to the study's lead author, Dr. Wilcock, "To halt the disease, you have to stop the brain cells from being killed." What galantamine does to improve the symptoms is the functional equivalent of that, making up for the loss of brain cells in other ways. In other words, galantamine rescues brain cells from death.

ALZHEIMER'S THREATENS TO DOMINATE COGNITIVE DEGENERATION One in ten people over the age of 65, and nearly half of those over 85, have Alzheimer's disease, according to the Alzheimer's Association in Chicago - and the situation is getting worse as people live longer. Over 4 million Americans have Alzheimer's disease, and, unless a cure or prevention is found, that number will leap to 14 million by the year 2050. On a global scale, it is estimated that by the year 2025, 22 million individuals will develop this debilitating disease.

TO AGE OR NOT TO AGE As serious as Alzheimer's is, it is not the only reason to consider the use of galantamine. As we age, a slow but sure mental degeneration takes place. Ultimately, aging is the thief that steals our memory, consciousness, and personality away. But that thief, specifically, is the age-related decline of the cholinergic system.

Galantamine offers a means to do something about age-related memory impairment right now, a syndrome now viewed as a precursor to advanced degenerative diseases such as Alzheimer's. It can help to prevent the decline and deterioration of our vital mental functions by enhancing our supply of the essential neurotransmitter acetylcholine. There is probably no better way to ensure the preservation of memory and its myriad of precious functions than through a well-designed cognitive supplement program, in which galantamine plays a fundamental role.

Galantamine is a natural plant-derived product that has been used throughout Eastern Europe for more than 40 years. It is reassuring to know that galantamine is currently available and affordable, not because it has achieved "drug status," but because of its track record for the treatment of a wide variety of age-related deficiencies and age-related decline


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