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Exelon Patch


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#1 johnblaze

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Posted 23 April 2008 - 08:52 PM


About two months ago I was in a car accident in which both of my ankles/feet fractured/dislocated. My memory of the accident is quite interesting. I have had false memories of it, and my initial recollection of events turns out to be completely inaccurate (different area of town, different circumstances, etc). I don't remember going unconsious specifically, or blacking out for any significant length of time, and the medics didn't indicate anywhere that I suffered from a concussion. The only opportunity would have been right at the point of impact when the airbags deployed, for maybe a second or two at most, because I immediatly checked to see if the other passenger was ok while I was still catching my breath from the impact. At any rate I have a hard time remembering the accident and the hours preceeding the accident. Some details come back but I don't fully trust that they are not imagined or false.

Moving on, since the accident I have experienced lack of concentration and mental vigilance. I would drift in and out of a conversation, tho I could pull one off fine it wasn't optimal. I couldnt read anything for more than a few seconds. I had insomnia as well. Most of this I attributed to the opiate therapy from the surgeries/trauma treatment. I am now off painkillers and the insomnia has worsened. I can concentrate better but it is still a battle, I have barely gotten a dozen pages into Kurzweils latest book after weeks hah. Converations arent a problem, but word and memory recall are.

I saw an old friend who is a psychiatrist today and told her what had happened and my symptoms and she mentioned after two concusions Aricept is a standard treatment given to people. She said she preffered Exelon and then said it may help me out right now. She mentioned it is a acetylcholinesterase and butryrlcholinesterase inhibitor, and that sounded right on track for me. I have had experience with alpha-gpc, piracetam, and aniracetam in the past, and was even thinking about taking piracetam but my surgeon recomended waiting till after my course of lovenox(blood thinner) to do so.

This Exelon looks pretty damn cool actually, from my viewpoint of researching the racetams in the past. It is a reversable AcCh and ButCH inhibitor and the transdermal system keeps a low and constant plasma concentration. It easily crosses the BBB and does totally bypasses hepatic isoenzymes (CYP450). It has a low side effect profile as well.

My questions to you all are what are your experiences with the *esterase inhibitors (opposed to agonists/racetams); do any of you have direct expereience of Exelon? Also as a general FYI because I have not heard this substance mentioned in the forums and it seems to be a real gem! This is my first day and I'm on the 4.6mg/day patch, I will update with my reactions to it as I encounter them.

Some further info
http://en.wikipedia....ki/Rivastigmine
http://www.rxlist.co...xelon-patch.htm

#2 johnblaze

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Posted 24 April 2008 - 06:49 PM

So far I have spent 24 hours on the patch and my experience is as follows:
  • Slight dizzyness in the evening, most prominent with dinner
  • Reduced appetite to the point of feeling like I overate
  • Similar stimulation as felt from piracetam - clean, non-jittery, and slightly amphetemine like
  • Inreased conversation/talkative
  • Slept better than I have in weeks (surprised)
This has been my initial anecdotal experience so far and I still have yet to take the first patch off.

One slight symptom I have experienced is both dysphoria and euphoria simultaneously accompanied with rapid mood swings and hyperemotions, but I have been experiencing this before starting the patch so I won't rule it as part of the Exelon experience.

As always looking forward to feedback.
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#3 johnblaze

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Posted 26 April 2008 - 04:42 AM

Well it's been a couple days now. The sleep the first night might have been placebo or who knows what because last night I couldn't sleep for hours upon hours :(

Side effects that have been consistant now are GI related mostly:
  • Reduced Appetite
  • Intestinal Cramps
  • Periodic nausea/dizzyness
  • Constant Heartburn
The slight speediness has faded (into the backround perhaps), and at this point I don't notice much.

As for the head trauma symptom management I dont feel a definate effect that I could say it's working or not.

Will continue to update the thread as the experience unfolds.

Edit: I did read >80 pages of Kurzweils Fantastic Voyage, I don't know if it's because it's of interest to me or it's the Exelon, but it's a marked improvement.

Edited by johnblaze, 26 April 2008 - 04:52 AM.

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#4 graatch

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Posted 27 April 2008 - 01:22 PM

Do you remember why she preferred Exelon to Aricept?

To my mind, inhibiting butylcholinesterase (which is mostly peripheral) is not really a good thing -- galantamine and aricept are known to be more selective for acetylcholinesterase.

Peripheral butylcholinesterase inhibition ----> the peripheral cholinergic side effects you describe.

Insomnia is not surprising. You might try taking the patch off at night.

Finally, you might think about methylphenidate, which is really more accepted than ACHe inhibitors for ADD secondary to head trauma, and has been shown to promote recovery. I'm not sure the same is true for the ACHe inhibitors, and it may even pose a problem in this respect (theoretically, I am worried about possibly enhancing excitotoxicity from NMDA, the transmission of which ACHe inhibitors significantly enhance), especially if sleep is significantly impaired.

Edited by graatch, 27 April 2008 - 01:23 PM.


#5 johnblaze

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Posted 29 April 2008 - 09:21 PM

Do you remember why she preferred Exelon to Aricept?

To my mind, inhibiting butylcholinesterase (which is mostly peripheral) is not really a good thing -- galantamine and aricept are known to be more selective for acetylcholinesterase.

Peripheral butylcholinesterase inhibition ----> the peripheral cholinergic side effects you describe.

Insomnia is not surprising. You might try taking the patch off at night.

Finally, you might think about methylphenidate, which is really more accepted than ACHe inhibitors for ADD secondary to head trauma, and has been shown to promote recovery. I'm not sure the same is true for the ACHe inhibitors, and it may even pose a problem in this respect (theoretically, I am worried about possibly enhancing excitotoxicity from NMDA, the transmission of which ACHe inhibitors significantly enhance), especially if sleep is significantly impaired.


I will look into methylphenidate and discuss it with her, do you have any studies or literature to point me towards?

Also when it comes to the GI problems, I did experience these with piracetam as well but it is a AcCh agonist which hits both the central and peripheral neverous so I didnt even think to look at the ButCh pathway, thanks for the info.

As for why she recomends it, again I'll ask her to go into more depth, but a safe asumption would be she likes the lack of drug-drug interaction (in the hepatic and renal pathways) and the consistant plasma levels/convenient dosing afforded by the transdermal patch; also, sleep might be affected at a greater level by methylphinidate than exelon.

Now almost a week into dosing I find my sleep has normalized and I require less of it every night. Also the GI symptoms have receeded a bit into the background as well. I still am getting a lot of reading done and my mental vigilance/concentration remain improved. I do feel a bit edgey and agitated at times, but thats a grey area in terms of exelon being the sole culprit.

All-in-all a positive experience thus far.

#6 graatch

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Posted 01 May 2008 - 09:30 AM

http://www.google.co...ate head trauma

I note a lot of summarized research pieces you can pull up.

Methylphenidate improves sleep quality in ADD/ADHD -- probably due to enhanced daytime activity coupled with the short half-life. This is probably valid unless one is taking stupid doses.

Aricept's long half-life also would point in the direction of consistent blood levels.

I do very much like galantamine, but it seems to affect me much longer than it should, based simply on the half-life.

Good to hear that the GI and sleep problems are receding a bit -- that's usually what seems to be the course, from reading other accounts of non-elderly people taking ACHe inhibitors for one reason or another.

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#7 johnblaze

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Posted 23 May 2008 - 10:12 PM

I saw the dr again ecently and have few updates.

As to her preference of the Exelon patch over Aricept it is in fact the clinical effects of constant plasma levels, easy dosing, and lack of drug interactions that she preffered. She also felt that bypasing the GI tract for administration reduced GI symptoms, albeit I'm hypersensitive to most medications and this is not true for me. As for butyrylcholinsterase being peripheral she thought the jury was still out on that, that it may be both central and peripheral.

As for methylphenidate, I have had diagnoses in the past for major depression, anxiety, and dysthmia and allthough I do not take pharmacueticals anymore for these conditions. She felt this coupled with my hypersensitivity, sleeping issues, that methyphinidate would not be a good match.

Last month she had given me a sample pack of the low-dose pack, and today I'm moving up to the mainteneance dosage. I have noticed that it hasn't completly helped with my mild cognitivie impairment. Also, I just found it'll be $160/mo which is way too expesnive for me(as an art student!). I will finish out this months dosage and then discuss alternatives with her for the future. I'm leaning toward Huperzine-A coupled with piracetam & cdp-choline. I will also look into galantamine. Does anyone have any other suggestions?

Current daily supps are:
9g Fishoil (1.7g EPA, 1.1g DHA)
Orthocore
Glucosamine & Chondroitin + MSM
NOW D-Flame (Holy Basil, Tree Turmeric, Turmeric, Boswellin, GTE, Ginger)
ZMA




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