15 replies to this topic

[focus83]

Hi guys!I just received 28x 5mg Aricept tablets for which I paid an outrageous price. Now I am about to swallow the first pill. If I tolerate it I will take one 5mg pill every morning for one month.Right now I do not have an extensive regimen, but here is what I take:Pentoxifylline (Trental) 3x daily 400 mgVenlafaxine 150mgoccasionally L-Dopa with green teasometimes Memantine, but not on a daily basisClenbuterol twice daily 20mcgI would like to keep you updated about the effects it has on me. Is there interest in such a mini-blog? Or is Aricept not endorsed among the nootropics community?Btw, I didn't get any positive nor negative effects from Huperzine-A so I am very excited about what Aricept will do for me.If anyone else is using Aricept please share your experiences!I will try to post the effects of the first pill today.cheersfocus

[Guacamolium]

How well does pentoxifylline affect you?

[yowza]

Dude, just to warn ya...

Aricept has a half life of 70 hours (or roughly 3 days), which means that an additional half life after this would take another 3 days. Therefore, if you have a bad effect from the aricept it could take about 2 weeks roughly to wear off to a certain extent.
The effects of aricept, on first time usage, seem to creep on ya. After the first dosage one may not feel much but after the 2nd or the 3rd day in a row, bad effects can hit suddenly out of nowhere.

I also ordered this medication online about a year ago. I took 5 mg up to 4 days until I couldn't take it anymore. About 3 weeks later I tried 2.5 mg each day and this built up after 3 days. One month after this I took 1 5mg and was miserable for 2-3 weeks afterwards (it seems you can become more sensitive to the effects after just a short while). Just to warn you, it is pretty easy to snap in anger while under this stuff if everything doesn't go just so... This also had some mental effects that took a while to wear off for me. So my advice...

BE CAREFUL.

Especially with any drug that inhibits acetylcholinesterase (the enzyme that breaks down acetylcholine).
Unfortunately drugs are still in the early phase in regards to acetylcholine. Personally, I'd try Galantamine over aricept since that may yield some benefit but shouldn't be used long term every day I'm sorry to say.

Edited by yowza, 18 March 2009 - 12:34 AM.

[focus83]

Ok, day 1:

Took 1 5mg in the afternoon and felt sick about half an hour later. This completely disappeared after some minutes.

So far there is not much to tell. No effects that I could definitely attribute to Aricept although I had the impression I needed less effort to remember things, but this could be placebo anyway.
I also had a very restful sleep, but again this can be due to a number of things.

I will keep you updated.

[focus83]

Dude, just to warn ya...

Aricept has a half life of 70 hours (or roughly 3 days), which means that an additional half life after this would take another 3 days. Therefore, if you have a bad effect from the aricept it could take about 2 weeks roughly to wear off to a certain extent.
The effects of aricept, on first time usage, seem to creep on ya. After the first dosage one may not feel much but after the 2nd or the 3rd day in a row, bad effects can hit suddenly out of nowhere.

I also ordered this medication online about a year ago. I took 5 mg up to 4 days until I couldn't take it anymore. About 3 weeks later I tried 2.5 mg each day and this built up after 3 days. One month after this I took 1 5mg and was miserable for 2-3 weeks afterwards (it seems you can become more sensitive to the effects after just a short while). Just to warn you, it is pretty easy to snap in anger while under this stuff if everything doesn't go just so... This also had some mental effects that took a while to wear off for me. So my advice...

BE CAREFUL.

Especially with any drug that inhibits acetylcholinesterase (the enzyme that breaks down acetylcholine).
Unfortunately drugs are still in the early phase in regards to acetylcholine. Personally, I'd try Galantamine over aricept since that may yield some benefit but shouldn't be used long term every day I'm sorry to say.

Thanks yowza! I am aware of the long half life, but I will be careful if I notice any of the unpleasant effects you described. Galantamine would be my next candidate in case Aricept doesn't live up to my excpectations. Unfortunately it is also extremely expensive. Or do you know a cheap source? Pls. PM me if you know one.

[focus83]

How well does pentoxifylline affect you?

It's good for increasing blood flow. Can't say I feel any nootropic effects, but it definetly helps with my cold hands and feet and it makes me feel warmer (meaning body temperature). However, I do not plan to order it again since the benefits are too few compared to the price.

[focus83]

Day 2: Took 5mg in the morning

Much improved focus and mood elevation. Less anxiety and I was more social and talkative. No side effects to speak of.
It's too early to say something about improved memory. I guess I will wait a couple more days before I make any conclusions. But I have the impression that information is flowing easier into the brain.

Will keep you updated around day 5.

Cu

[yowza]

Bump

I'd like to hear how the 3rd/4th days go for ya.

Once your done with your initial trial; I'd read the following study... It's pretty interesting.

Mol Pharmacol. 2004 Sep;66(3):538-44.

Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release.

Zhang L, Zhou FM, Dani JA.

Division of Neuroscience, Baylor College of Medicine, Houston, TX 77030-3498, USA.

Alzheimer's disease is a neurodegenerative disorder associated with a decline in cognitive abilities. Patients also frequently have noncognitive symptoms, such as anxiety, depression, apathy, and psychosis, that impair daily living. The most commonly prescribed treatments for Alzheimer's disease are acetylcholinesterase inhibitors, such as donepezil and galantamine. Enhanced cholinergic functions caused by these compounds are believed to underlie improvements in learning, memory, and attention. The noncognitive aspects of dementia, however, are usually linked to serotonin and dopamine rather than acetylcholine because those neurotransmitter systems most directly influence mood, emotional balance, and psychosis. Fast-scan cyclic voltammetry applied to mouse striatal brain slices was used to measure the real-time release of dopamine arising from spontaneous activity or from single electrical stimulations. At concentrations that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) increase action potential-dependent dopamine release. Consistent with previous literature, the data support slightly different modes of action for donepezil and galantamine. The ability of these commonly prescribed drugs to alter catecholamine release may underlie their influence over noncognitive symptoms of dementia. Furthermore, these results suggest that acting via nicotinic receptors, these drugs may serve presently untapped therapeutic roles by altering dopamine release in other disorders involving dopaminergic systems.

There have been users that have stated cholinergic compounds have potentiated the response of dopamergic drugs at times. From this study, it appears that this is primarily due to cholinergic compounds stimulating the nicotine receptors.




Fuck, I'm officially pissed off...

My message above got cut off and it was very interesting... (I took breif notes on what it was and will try and post it later in abbreviated less grammatically correct fashion)

Ah well... It also double posted on me. If someone could delete the one below that would be great.

Edited by yowza, 20 March 2009 - 02:35 AM.

[yowza]

Bump

I'd like to hear how the 3rd/4th days go for ya.

Once your done with your initial trial; I'd read the following study... It's pretty interesting.

Mol Pharmacol. 2004 Sep;66(3):538-44.

Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release.

Zhang L, Zhou FM, Dani JA.

Division of Neuroscience, Baylor College of Medicine, Houston, TX 77030-3498, USA.

Alzheimer's disease is a neurodegenerative disorder associated with a decline in cognitive abilities. Patients also frequently have noncognitive symptoms, such as anxiety, depression, apathy, and psychosis, that impair daily living. The most commonly prescribed treatments for Alzheimer's disease are acetylcholinesterase inhibitors, such as donepezil and galantamine. Enhanced cholinergic functions caused by these compounds are believed to underlie improvements in learning, memory, and attention. The noncognitive aspects of dementia, however, are usually linked to serotonin and dopamine rather than acetylcholine because those neurotransmitter systems most directly influence mood, emotional balance, and psychosis. Fast-scan cyclic voltammetry applied to mouse striatal brain slices was used to measure the real-time release of dopamine arising from spontaneous activity or from single electrical stimulations. At concentrations that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) increase action potential-dependent dopamine release. Consistent with previous literature, the data support slightly different modes of action for donepezil and galantamine. The ability of these commonly prescribed drugs to alter catecholamine release may underlie their influence over noncognitive symptoms of dementia. Furthermore, these results suggest that acting via nicotinic receptors, these drugs may serve presently untapped therapeutic roles by altering dopamine release in other disorders involving dopaminergic systems.

There have been users that have stated cholinergic compounds have potentiated the response of dopamergic drugs at times. From this study, it appears that this is primarily due to cholinergic compounds stimulating the nicotine receptors.

[yowza]

Ok. Here's what I intened to follow up my comment under the quote above with in less grammatically correct fashion:

It's my opinion that the cholinesterase medications out now are not selective enough to potentiate more benefits vs. side effects. This is both in regards to the nootropic effect of acetylcholine itself and to correlatory responses like the stimulatory action with nicotine receptors (backdoor route to potentiate dopamine).

However, these class of drugs do hold potential for the future as long as they can become more selective. Right now, there are a number of different drugs being developed that may combine the best of both worlds (acetylcholine benefits with less side effects and dopamergic benefits with less side effects). For instance, one of the most popular being developed now seems to be Ispronicline (http://en.wikipedia....ki/Ispronicline) that's also known as TC-1734 (by targacept whose a lab subsidiary of rjr tobacco) or AZD-3480 (astra zeneca calls it this; they are the company targacept is trying to market ispronicline thru once the FDA approves it).

Unfortunately, the only partial nicotine agonist out now seems to be chantix, which makes you sick from nicotine, which is for smoking cessation.


Here's some additional info. I've managed to dig up about the cholinesterase medications out now:
Enzymes that inhibit cholinesterase:
AChE and BChE molecules
1) can be globular (G1, G2, and G4) or
G molecules can show amphiphilic (detergent-interacting, GA) or hydrophilic (GH) behavior. [2006]
2) asymmetric forms (A4, A8, and A12) (Massouli??, 2002),


Unlike some older cholinergic drugs, aricept doesn't seem to effect butylcholinesterase. This can inhibit detox thru the liver and cause all sorts of nasty peripheral side effects thru the Autonomic Nervous System as one would become overly parasympathetic dominant and be quite miserable unless they were using the drug for a chronic condition. In terms of Acetylcholinesterase inhibition, it seems to mainly act in the Central Nervous System on g1 and g4 mainly (any more?). It's also said to be not neurotoxic like Tacrine but still quite dangerous and can throw one's body out of wack.

One interesting observation about aricept (based off the study above and a number of experiences) though is that it may potentiate dopminergic inhibitor like ritaline if taken in a very small amount like 1 mg over the course of a week possibly (in a way ritalin may kind of feel like an amphetamine to a certain point only without the direct agonistic action that amphetamines can have). However, this combination probably I wouldn't be comfortable with for a prolonged period of time.

If looking for a stimulating feel, Galantamine may be better since it's agonistic towards nicotine receptors and may inhibit less acetylcholinesterase isoforms? (not sure on this) This is the best medication based option at the moment it seems. Hopefully, there'll be something better in the near future...

[focus83]

Ok. Here's what I intened to follow up my comment under the quote above with in less grammatically correct fashion:

It's my opinion that the cholinesterase medications out now are not selective enough to potentiate more benefits vs. side effects. This is both in regards to the nootropic effect of acetylcholine itself and to correlatory responses like the stimulatory action with nicotine receptors (backdoor route to potentiate dopamine).

However, these class of drugs do hold potential for the future as long as they can become more selective. Right now, there are a number of different drugs being developed that may combine the best of both worlds (acetylcholine benefits with less side effects and dopamergic benefits with less side effects). For instance, one of the most popular being developed now seems to be Ispronicline (http://en.wikipedia....ki/Ispronicline) that's also known as TC-1734 (by targacept whose a lab subsidiary of rjr tobacco) or AZD-3480 (astra zeneca calls it this; they are the company targacept is trying to market ispronicline thru once the FDA approves it).

Unfortunately, the only partial nicotine agonist out now seems to be chantix, which makes you sick from nicotine, which is for smoking cessation.


Here's some additional info. I've managed to dig up about the cholinesterase medications out now:
Enzymes that inhibit cholinesterase:
AChE and BChE molecules
1) can be globular (G1, G2, and G4) or
G molecules can show amphiphilic (detergent-interacting, GA) or hydrophilic (GH) behavior. [2006]
2) asymmetric forms (A4, A8, and A12) (Massouli??, 2002),


Unlike some older cholinergic drugs, aricept doesn't seem to effect butylcholinesterase. This can inhibit detox thru the liver and cause all sorts of nasty peripheral side effects thru the Autonomic Nervous System as one would become overly parasympathetic dominant and be quite miserable unless they were using the drug for a chronic condition. In terms of Acetylcholinesterase inhibition, it seems to mainly act in the Central Nervous System on g1 and g4 mainly (any more?). It's also said to be not neurotoxic like Tacrine but still quite dangerous and can throw one's body out of wack.

One interesting observation about aricept (based off the study above and a number of experiences) though is that it may potentiate dopminergic inhibitor like ritaline if taken in a very small amount like 1 mg over the course of a week possibly (in a way ritalin may kind of feel like an amphetamine to a certain point only without the direct agonistic action that amphetamines can have). However, this combination probably I wouldn't be comfortable with for a prolonged period of time.

If looking for a stimulating feel, Galantamine may be better since it's agonistic towards nicotine receptors and may inhibit less acetylcholinesterase isoforms? (not sure on this) This is the best medication based option at the moment it seems. Hopefully, there'll be something better in the near future...

Hi yowza!

I just glanced over your postings, because I am short on time (currently at work). Seems to be very interesthing though. I will read it more closely when I have the time this evening.

Day 3 and 4:
I tolerate Aricept pretty well and it gives me a nice boost in focus, talkativity and I worry less about social interaction (I do suffer from social phobia also). I am also more coordinated in what I do. Less confusion and brain fog.
I still can't notice any memory improvements, but still I'm pretty satisified with how things go.

I do have to mention that I took 2mg Klonipin each night which could very well be the reason why I didn't notive any significant memory improvements from Aricept so far. I will, however, stop using Klonipin now for at least a period of 2 weeks.

Also, next week I will receive a package of 20 tablets Pramiracetam. I'm curious about what this will do in combination with Aricept. Unfortunately, this stuff is too expensive to buy more of it.

cheers

[yowza]

Ok. Here's what I intened to follow up my comment under the quote above with in less grammatically correct fashion:

It's my opinion that the cholinesterase medications out now are not selective enough to potentiate more benefits vs. side effects. This is both in regards to the nootropic effect of acetylcholine itself and to correlatory responses like the stimulatory action with nicotine receptors (backdoor route to potentiate dopamine).

However, these class of drugs do hold potential for the future as long as they can become more selective. Right now, there are a number of different drugs being developed that may combine the best of both worlds (acetylcholine benefits with less side effects and dopamergic benefits with less side effects). For instance, one of the most popular being developed now seems to be Ispronicline (http://en.wikipedia....ki/Ispronicline) that's also known as TC-1734 (by targacept whose a lab subsidiary of rjr tobacco) or AZD-3480 (astra zeneca calls it this; they are the company targacept is trying to market ispronicline thru once the FDA approves it).

Unfortunately, the only partial nicotine agonist out now seems to be chantix, which makes you sick from nicotine, which is for smoking cessation.


Here's some additional info. I've managed to dig up about the cholinesterase medications out now:
Enzymes that inhibit cholinesterase:
AChE and BChE molecules
1) can be globular (G1, G2, and G4) or
G molecules can show amphiphilic (detergent-interacting, GA) or hydrophilic (GH) behavior. [2006]
2) asymmetric forms (A4, A8, and A12) (Massouli??, 2002),


Unlike some older cholinergic drugs, aricept doesn't seem to effect butylcholinesterase. This can inhibit detox thru the liver and cause all sorts of nasty peripheral side effects thru the Autonomic Nervous System as one would become overly parasympathetic dominant and be quite miserable unless they were using the drug for a chronic condition. In terms of Acetylcholinesterase inhibition, it seems to mainly act in the Central Nervous System on g1 and g4 mainly (any more?). It's also said to be not neurotoxic like Tacrine but still quite dangerous and can throw one's body out of wack.

One interesting observation about aricept (based off the study above and a number of experiences) though is that it may potentiate dopminergic inhibitor like ritaline if taken in a very small amount like 1 mg over the course of a week possibly (in a way ritalin may kind of feel like an amphetamine to a certain point only without the direct agonistic action that amphetamines can have). However, this combination probably I wouldn't be comfortable with for a prolonged period of time.

If looking for a stimulating feel, Galantamine may be better since it's agonistic towards nicotine receptors and may inhibit less acetylcholinesterase isoforms? (not sure on this) This is the best medication based option at the moment it seems. Hopefully, there'll be something better in the near future...

Hi yowza!

I just glanced over your postings, because I am short on time (currently at work). Seems to be very interesthing though. I will read it more closely when I have the time this evening.

Day 3 and 4:
I tolerate Aricept pretty well and it gives me a nice boost in focus, talkativity and I worry less about social interaction (I do suffer from social phobia also). I am also more coordinated in what I do. Less confusion and brain fog.
I still can't notice any memory improvements, but still I'm pretty satisified with how things go.

I do have to mention that I took 2mg Klonipin each night which could very well be the reason why I didn't notive any significant memory improvements from Aricept so far. I will, however, stop using Klonipin now for at least a period of 2 weeks.

Also, next week I will receive a package of 20 tablets Pramiracetam. I'm curious about what this will do in combination with Aricept. Unfortunately, this stuff is too expensive to buy more of it.

cheers

In my opinion, it's not worth buying Pramiracetam unless you can figure out how to get in bulk.

Sounds like your responding to the Aricept pretty well so far with it being the 4th day. The 5th and 6th day will be interesting are without the Klonopin.

[bgwithadd]

Oh, never mind.

Edited by bgwithadd, 21 March 2009 - 02:03 AM.

[yowza]

Any updates on the Aricept trial?


I recently found Galantamine can be purchased by pill (for a much cheaper price) at the following site...

http://www.libertyme...Browse.aspx?l=G

I don't want to encourage anyone to order anything but just making note of the fact that certain medications (that someone may be trialing for whatever hopefully good reason) are available in reduced amounts.

[Guacamolium]

In my opinion, it's not worth buying Pramiracetam unless you can figure out how to get in bulk.

I agree. It isn't worth the retail price. I had such high expectations for it, and it really didn't outperform oxiracetam at all. It is one of the medium-expensive racetams, so perhaps one of us can offer it at a more alluring price. Some racetams are more than double in price than Pram - imagine that.

[focus83]

Any updates on the Aricept trial?


I recently found Galantamine can be purchased by pill (for a much cheaper price) at the following site...

http://www.libertyme...Browse.aspx?l=G

I don't want to encourage anyone to order anything but just making note of the fact that certain medications (that someone may be trialing for whatever hopefully good reason) are available in reduced amounts.

Sorry for not updating my thread :-(

There is really nothing new to report. I still have the same benefits I mentioned earlier with virtually zero side effects. I rarely tolerate a drug that well.

What I should add is that my essential tremor is reduced (for whatever reason) and hence my movements are more coordinated. I still can't say that my memory has improved beyond placebo, but it feels like I can slightly better recall things.

I did experiment with 1 x 10mg as well, but didn't have the impression that the effects were much stronger. I only noticed a very slight tension headache a few hours after intake.

Anyway, if my budget allows it I will definetly reorder Aricept even though this time from a cheap Indian source.
But before ordering again I will buy some Galantamine!

Btw, I cancelled my Pramiracetam order because of issues with the bank transfer. So please do not wait for a report :-(