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Huperzine A, warning?


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#1 faust

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Posted 29 October 2004 - 11:40 AM


I know, it's old. What think of that? Opinions or comments?



LE Magazine November 2000
Q & A


Huperzine A
Making the right move on when and how much you should take

Q I am seeing a lot of ads for Huperzine A, a cognitive enhancer. Several mail order companies carry products with huperzine. Have you evaluated it?

A We have extensively evaluated Huperzine A and do not recommend that healthy people take it every day. Huperzine A functions as an acetylcholinesterase inhibitor. That means that it inhibits an enzyme in your brain that is responsible for degrading the neurotransmitter acetylcholine. Alzheimer’s disease patients have elevated levels of acetylcholinesterase and can therefore benefit by taking drugs like Aricept or nutrients like Huperzine A, which inhibit acetylcholinesterase.

Healthy people, on the other hand, need acetylcholinesterase to regulate acetylcholine levels in their brains. If you wanted to impress someone with your short-term memory on any given day you could safely take the recommended dose of Huperzine A, but we would not advise that you do so daily. We have a member who is a world class chess player, and has proven he can improve his scores by taking Huperzine A the day of a chess tournament.

While it is safe to boost acetylcholine levels by inhibiting acetylcholinesterase periodically, chronic use of Huperzine A could cause over-suppression of acetylcholinesterase and subsequent acetylcholine overload with unknown consequences. Remember, you can take huge amounts of acetylcholine precursors such as choline without fear of acetylcholine overload because you have acetylcholinesterase to degrade excess acetylcholine. If you block the body’s natural regulator of acetylcholine (that regulator being acetylcholinesterease), you may have a problem. We do not recommend that people take Huperzine A more than twice a week, much less promote it for daily use like other companies do.



#2 dalessm

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Posted 29 October 2004 - 03:13 PM

Yikes!! I was taking HupA everyday (150 mg).

Please, anyone out there have any more published reviews to contribute?The scientific/scholarly-based articles are helpful, but (personally speaking) the nomenclature and jargon gets a little convoluted sometimes...

Faust, thanks for posting this review.

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#3 nootropi

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Posted 29 October 2004 - 04:00 PM

I do not agree. I have been taking an acetylcholinesterase inhibitor (and a powerful one at that) for over two years, every day continuously. The only significant difference is that I have now much more acetylcholine per synapse than before.

#4 bdnf

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Posted 29 October 2004 - 08:07 PM

"The only significant difference is that I have now much more acetylcholine per synapse than before."

True, you have more ACh in the synaptic cleft. But you have fewer ACh receptors, in order to compensate for the higher synaptic levels of ACh. The same neural changes occur when one ingests a SSRI (i.e. increased 5-HT causes a downregulation of 5-HT receptors). This is one of the many compensatory responses of the body which serves to maintain homeostasis. And suppression of acetylcholinesterase is merely another. You might not agree, but there is a wealth of studies standing contrary to your belief.

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Posted 29 October 2004 - 09:18 PM

I have not used Huperzine A recently, but I've found that even taking 1000mg of Alpha GPC I have not been getting the same effect as when using Huperzine A. I wonder whether my brain is compensating for the higher levels of acetylcholine by releasing much more acetylcholinesterase, which would defeat the purpose of taking additional choline.

Any thoughts?

#6 faust

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Posted 29 October 2004 - 09:29 PM

"The only significant difference is that I have now much more acetylcholine per synapse than before."

True, you have more ACh in the synaptic cleft. But you have fewer ACh receptors, in order to compensate for the higher synaptic levels of ACh. The same neural changes occur when one ingests a SSRI (i.e. increased 5-HT causes a downregulation of 5-HT receptors). This is one of the many compensatory responses of the body which serves to maintain homeostasis. And suppression of acetylcholinesterase is merely another. You might not agree, but there is a wealth of studies standing contrary to your belief.


Thus Aricept for a person who does not alzheimer, it is not good?

#7 bdnf

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Posted 29 October 2004 - 10:04 PM

Indeed, it is profoundly unwise.

Edited by bdnf, 29 October 2004 - 10:43 PM.


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Posted 29 October 2004 - 10:53 PM

Aricept is an AChE inhibitor, it really isn't a remarkably effect Alzheimer drug. If anything it just prolongs the inevitable, it doesn't remedy or treat the cause of Alzheimers.

#9 faust

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Posted 29 October 2004 - 11:04 PM

Aricept is an AChE inhibitor, it really isn't a remarkably effect Alzheimer drug. If anything it just prolongs the inevitable, it doesn't remedy or treat the cause of Alzheimers.


Yes, I know...

I try to find the best stack of smart drugs, the most effective, by combining medicines and supplements, at least expensive possible. Aricept is expensive, but if effective for improve my memory, I will pay, but is not very effective for non-alzheimer person, I will not buy and continue with Huperzine

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Posted 29 October 2004 - 11:42 PM

I chose Huperzine A over Aricept myself, for reasons of cost and availability.

I'm considering ordering more Huperzine A and use it concurrently with my Alpha GPC.

#11 nootropi

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Posted 30 October 2004 - 12:50 AM

But you have fewer ACh receptors, in order to compensate for the higher synaptic levels of ACh. The same neural changes occur when one ingests a SSRI (i.e. increased 5-HT causes a downregulation of 5-HT receptors). This is one of the many compensatory responses of the body which serves to maintain homeostasis. And suppression of acetylcholinesterase is merely another. You might not agree, but there is a wealth of studies standing contrary to your belief.


This is not an issue of agreeing for me. Show me the science, please.

Donepezil (aricept) is well tolerated and frequently used now to treat not only alzheimers, but also patients suffering from ADD, ADHD, depression and mania.

Proof:

Non-stimulant medications in the treatment of ADHD. Data source #1

Data source #2

[Acetylcholinesterase inhibitors--beyond Alzheimer's disease] data source #3

Drugs under investigation for attention-deficit hyperactivity disorder. Data source #4

Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder. data source #5

Non-stimulant treatments for ADHD. data source #6

Adjunctive donepezil in attention deficit hyperactivity disorder youth: case series. data source #7

Pharmacologic alternatives to psychostimulants for the treatment of attention-deficit/hyperactivity disorder. data source #8

Data source #9

Data source #10

Data source #11 (inconclusive)

I think I have proven my case is valid. Aricept is well tolerated and commonly prescribed off label for several uses.

#12 bdnf

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Posted 30 October 2004 - 12:58 AM

Most of these references are on atomoxetine, not aricept.
The studies that did mention aricept-like drugs for other conditions (e.g. ADD) are short-term investigations. Moreover, the results are weak and all warrant further research.

#13 nootropi

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Posted 30 October 2004 - 01:07 AM

Most of these references are on atomoxetine, not aricept. 
The studies that did mention aricept-like drugs for other conditions (e.g. ADD) are short-term investigations.  Moreover, the results are weak and all warrant further research.


I do not understand what you are pointing to.

We already know that donezepil improves cognitive function in healthy individuals (in processing complex tasks, the best indicator of a higher performance brain); those references were merely to further prove that donezepil is well tolerated and now frequently prescribed off label.

Donepezil and flight simulator performance: effects on retention of complex skills.

Link

However, Dr Yesavage can foresee a time when the use of memory-enhancing drugs is widespread - and controversial.

He said: "Will it worsen the gap between the haves and the have-nots when the rich are cognitively enhanced not only through better education, but also through drugs and other technologies?

"How should the use of these therapies be regulated in settings beyond aviation or normal ageing, such as chess matches or test-taking among college students?"



#14 bdnf

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Posted 30 October 2004 - 01:20 AM

True, you have more ACh in the synaptic cleft. But you have fewer ACh receptors, in order to compensate for the higher synaptic levels of ACh. The same neural changes occur when one ingests a SSRI (i.e. increased 5-HT causes a downregulation of 5-HT receptors). This is one of the many compensatory responses of the body which serves to maintain homeostasis. And suppression of acetylcholinesterase is merely another. You might not agree, but there is a wealth of studies standing contrary to your belief.


Put simply, Aricept is not effective long-term because the brain counteracts its effects. The same occurs when one takes Huperzine A (as LEF elucidated).

Is my point clear? The issue is not whether Aricept can be used off-label.

BTW, Sure aricept might be well tolerated (i.e. no side-effects), but that doesn't reveal anything about the neurophysiological changes occurring (i.e. downregulation of the cholinergic system with chronic useage). It's your brain, your game, have fun!

Edited by bdnf, 30 October 2004 - 06:29 AM.


#15 nootropi

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Posted 30 October 2004 - 01:24 AM

Once again, I have no problem with hypothesizing, it is the first step in the scientific method. I just don't necessarily believe in agreeing with anything that has not been demonstrated.

What scientific evidence do you have to present here of donezepil leading to, as you say, "downregulation of the cholinergic system with chronic useage?"

I surely have not experienced this effect. And if donezepil is truly effective at acetylcholinesesterase inhibition, that simply means that it stops the brain from releasing an enzyme that breaks acetylcholine down. If your hypothesis is true, then we would see this effect represented with enzyme inhibition agents other than Aricept.

Can you present any evidence of such an effect (that is, where enzyme inhibition leads to downregualtion of any system in the human body)?

Given we do understand very little about the human body and brain, one thing we know is that acetylcholine is the single most important identified neurotransmitter responsible for creating and storing memory in the human brain. If an enzyme breaks down acetylcholine, then its presence would definately cause there to be less acetylcholine in the brain.

I might agree that "too much acetylcholine" may be detrimental to human memory performance; however, a 5 mg daily dose of aricept appears to be safe and effective.

We do have concrete evidence that donezepil improves cognitive performance in healthy individuals. Therefore we can conclude that acetylcholinesterase inhibition is effective.

Thanks.

Edited by nootropi, 30 October 2004 - 01:44 AM.


#16 bdnf

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Posted 30 October 2004 - 01:48 AM

What scientific evidence do you have to present here of donezepil leading to, as you say, "downregulation of the cholinergic system with chronic useage?"


This is standard neuroscience textbook material. Obviously you know very little about neurophysiology, and hence pursuing this issue further with you would be a waste of my time.

You are attempting to reason on far too little information. I suggest you go away and do some reading.

#17 nootropi

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Posted 30 October 2004 - 01:52 AM

You are 100% correct! I know nothing of neuroscience.

I do not want to start with a sarcastic tone here, so please refrain from such unwarranted comments. I have based all of my arguments on scientific reasoning. If you cannot provide valid scientific data citations for your arguments (as I have for you), I cannot consider them.

Please: show me, don't tell me.

Thank you.

#18 bdnf

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Posted 30 October 2004 - 04:57 AM

I'm not going to waste my time and effort merely to please you. I am not proposing anything new. These are established facts.

You can conduct your own research.

#19 nootropi

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Posted 30 October 2004 - 05:44 AM

I'm not going to waste my time and effort merely to please you.  I am not proposing anything new.  These are established facts. 

You can conduct your own research.


Please do not clutter these forums with unsubstantiated nonsense. We already already suffer from an overdose of this thanks very much to the US Media.

You are not "wasting" your time and effort to "please" me, let me remind you that you are addressing a public forum.

You are indeed proposing your own unproven, untested hyptothetics; these are not estabilshed facts, if they were why not present them to us?

Why do you seek to argue what you do not know? Why do you want to generate animosity in this forum? I have respectfully presented you with citations to substantiate my claims.

Every other member of this forum has enough respect for the other readers to provide citatations. Please stop isolating yourself.
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#20 bdnf

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Posted 30 October 2004 - 06:16 AM

You are indeed proposing your own unproven, untested hyptothetics; these are not estabilshed facts, if they were why not present them to us?

I expect anyone who has undertaken a neuroscience major to be laughing at you right now.

Why do you seek to argue what you do not know?

Rather, what you do not know. You are out of your league.

I have respectfully presented you with citations to substantiate my claims

No you did not. I did not see a single study in which Aricept was used in healthy non-demented individuals for an extended period of time.

Please stop isolating yourself.

*sigh* As this statement exemplifies, it is unequivocal that you possess aberrant neurophysiology and thus on such basis your argument was flawed from the outset.

Edited by bdnf, 30 October 2004 - 06:33 AM.

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#21 nootropi

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Posted 30 October 2004 - 06:40 AM

I know, it's old. What think of that? Opinions or comments?



LE Magazine November 2000
Q & A


Huperzine A
Making the right move on when and how much you should take

Q I am seeing a lot of ads for Huperzine A, a cognitive enhancer. Several mail order companies carry products with huperzine. Have you evaluated it?

A We have extensively evaluated Huperzine A and do not recommend that healthy people take it every day. Huperzine A functions as an acetylcholinesterase inhibitor. That means that it inhibits an enzyme in your brain that is responsible for degrading the neurotransmitter acetylcholine. Alzheimer’s disease patients have elevated levels of acetylcholinesterase and can therefore benefit by taking drugs like Aricept or nutrients like Huperzine A, which inhibit acetylcholinesterase.

Healthy people, on the other hand, need acetylcholinesterase to regulate acetylcholine levels in their brains. If you wanted to impress someone with your short-term memory on any given day you could safely take the recommended dose of Huperzine A, but we would not advise that you do so daily. We have a member who is a world class chess player, and has proven he can improve his scores by taking Huperzine A the day of a chess tournament.

While it is safe to boost acetylcholine levels by inhibiting acetylcholinesterase periodically, chronic use of Huperzine A could cause over-suppression of acetylcholinesterase and subsequent acetylcholine overload with unknown consequences. Remember, you can take huge amounts of acetylcholine precursors such as choline without fear of acetylcholine overload because you have acetylcholinesterase to degrade excess acetylcholine. If you block the body’s natural regulator of acetylcholine (that regulator being acetylcholinesterease), you may have a problem. We do not recommend that people take Huperzine A more than twice a week, much less promote it for daily use like other companies do.


Faust:

I would beware of "reading and believing" blindly. Life Enhancement magazine is probably not the most credible source of information.

If you want to access a public library online of scientific data: Click here

Simply enter in the medicine you are interested in studying.

Take care.

#22 faust

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Posted 30 October 2004 - 12:28 PM

I don't know if Life Enhancement magazine is credible. I was found the url from rec.drugs.smart in post which talk of Huperzine.

But the answer in magazine is from doctor...

#23 nootropi

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Posted 30 October 2004 - 03:50 PM

I don't know if Life Enhancement magazine is credible. I was found the url from rec.drugs.smart  in post which talk of Huperzine.

But the answer in magazine is from doctor...


What doctor?

What makes this doctor's opinion credible?

From what sources does he base his opinion?

On the previous page I linked you directly to the publishings of several doctors and researchers regarding the use of Aricept, an acetylcholinesterase inhibitor, in non alzheimer settings. The consensus throughout the medical community is that acetylcholinesterase inhibition is not at all dangerous for healthy people as well as elderly people (suffering from Alzheimers). In fact, it is beneficial to non alzheimer subjects. Similarly, huperzine A, if indeed it is effective at inhibition of acetylcholinesterase, may be safe as well.

The point is: you need to learn how to synthesize the collective body of data/evidence and make your own decision regarding this issue.

Of course, the best way to ensure that you are not adversely affected by a negative side effect of a medicine is not to take it at all.

Take care.

#24 velocidex

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Posted 03 November 2004 - 04:56 AM

Can you present any evidence of such an effect (that is, where enzyme inhibition leads to downregualtion of any system in the human body)? 


I have to agree with bdnf. Downregulation is a well known, well-researched effect.

It is a homeostatic mechanism that eventually sets in given elevated levels of any neurotransmitter, to the best of my knowledge.

Take the MAOIs for example; monoamine receptor downregulation is apparent after chronic administration.

What on earth do you think causes tolerance to every other drug? Receptor agonists administered for a sufficient time period cause downregulation. Fact. Opiates, Benzos, direct dopamine agonists, muscarinic acetylcholine agonists, etc.

http://www.medterms....rticlekey=24471

Downregulation: An decrease in the number of receptors on the surface of target cells, making the cells less sensitive to a hormone or another agent. Some receptors can be rapidly down regulated.



#25 velocidex

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Posted 03 November 2004 - 05:10 AM

Furthermore: what do you think nerve agents (e.g. nerve gases) are? acetylcholinesterase inhibitors =\. Acetylcholine excess is not something you want to mess with. It always surprises me how scared people are of using monoamine oxidase inhibitors yet gladly take to the AChE inhibitors with glee, seeking "safe" memory improvements.

http://www.drugs.com/aricept.html

Symptoms of a Aricept overdose include severe nausea, vomiting, watering mouth, sweating, slow heartbeat, slow breathing, prolonged or severe dizziness, fainting, blurred vision, seizures, and collapse.


http://en.wikipedia....lcholinesterase

A cholinesterase inhibitor is known as an anticholinesterase. Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxins, causing excessive salivation and eye watering in low doses, followed by muscle spasms and ultimately death. Outside of biochemical warfare, anticholinesterases are used are also used in anesthesia or in the treatment of myasthenia gravis, glaucoma and Alzheimer's disease.


hmm.

#26 gulasch

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Posted 03 November 2004 - 09:28 AM

Notttropi:
How much Hyperzine A do you take - or how much would you recomend for an 21 year old. i recently ordered 300* 50mcg
I suppuse to take it twice daily, but when and with food or without
is it water or fat soutable?

here thze sup facts(nubrain-store):
Noitol contains:
Huperzine A 1% Extract 50 mcg
DMAE (Dimethylaminoaminiethanol Bitartrate) 25 mg
Choline (Dihydrogen Citrate) 250 mg
Vitamin B5 (Calcium Pantothenate) 100 mg

Is that a good mixture
what benefits does Dihydrogen Citrate have
thanks
greets
g

#27 nootropi

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Posted 03 November 2004 - 07:36 PM

velocidex: I wouldn't get too exited and emotional just because a word is defined in a medical dictionary.

"Downregulation" occurs in systems (with or) without medicine. Because the cholinergic system automatically degrades with increasing age due (explicitly) to acetylcholinesterase's increasing (among other several factors) activity; it is effective, in practice, to inhibit acetylcholinesterase.

And your point about nerve gas being toxic? I don't see where you are going with that one. Yes, nerve gas is deadly, and it inhibits acetylcholinesterease. But to an infinately exponentially higher degree than drugs such as Aricept or Hup A.

gulasch:
I have not studied the dosage efficacy of Hup A. As far as I know, it may be effective. But no conclusive data I know of indicates an effective dose. I would suggest Aricept if you can afford it. It is safe and well tolerated.

Be Well.

#28 gulasch

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Posted 03 November 2004 - 07:50 PM

thanks man
I could afford it but I already ordered it. The other issue is that I am not able to find it in europe. And a lot ofd orders from overseas get seized here in germany And all other suppliers i found in the Us do not support paypal. I do not have a credit card and my parents do not support me taking that stuff. And even if I could find one I need it quick because I have some difficult exams the next days so I need it quickly. The shipping from UK to GER does not take long.
greetings
g

#29 bdnf

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Posted 03 November 2004 - 08:13 PM

velocidex: I wouldn't get too exited and emotional just because a word is defined in a medical dictionary.


Ha! Velocidex is not emotional or excited. Why would (s)he be excited about basic facts in neuroscience that have been known for several decades and are supported by substantial scientific evidence?

"Downregulation" occurs in systems (with or) without medicine.  Because the cholinergic system automatically degrades with increasing age due (explicitly) to acetylcholinesterase's increasing (among other several factors) activity; it is effective, in practice, to inhibit acetylcholinesterase.


The key word is “age”. Since you are in your twenties, the use of an ACh inhibitor is scientifically unsupported and just plain stupid. Nootropi, you should know better. Although, given your limited understanding of neurophysiology, this would be expected from such a zealous nootropic user like yourself.

And your point about nerve gas being toxic?  I don't see where you are going with that one.  Yes, nerve gas is deadly, and it inhibits acetylcholinesterease.  But to an infinately exponentially higher degree than drugs such as Aricept or Hup A.


ACh inhibitors, such as Aricept, and like all drugs, do not exert uniform effects on the central nervous system. That is, ACh inhibition may by several times greater in, for example, the prefrontal cortex compared to the hippocampus (this effect can largely be attributed to differences in ACh receptor density and variations in ACh receptor subunit composition). And equally likely is an increase in ACh in one region of the brain and a decrease in another (n.b. this may sound contradictory, although if you were to undertake some reading you would learn the reason). It is indeed likely that ACh inhibition may be sufficiently great in one region of the brain to cause neuronal apoptosis via excessive cholinergic stimulation (akin to “nerve gas”).

Nootropi, I am not stimulating an argument here. My thoughts are in concordance with established facts. I merely want to ensure what you and others ingest is not going to have detrimental effects on the brain, particularly, since one of the primary goals in this forum is the contrary.

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#30 nootropi

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Posted 04 November 2004 - 05:36 AM

Look: if you were presenting "evidence" then show us, don't tell us. The standard practice when making a claim is to support it with evidence. Don't insult our intelligence (please) by citing "established facts" if you cannot present them to us like we do for you: in accordance with formal, concrete, and scientific standards. It is not respectful to make unsubstantiated claims here.

Be well.




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