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Countering the effects of anticholinergic drugs

acetylcholine neurotransmitters cognition

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#1 OFFLINE   chloliz

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Posted 16 April 2012 - 12:00 PM


Hello all!

As a relative newbie to the field, I’m still trying to get my head around how neurotransmitters actually work, so as to understand how they are being manipulated when we take nootropic drugs/antidepressants, etc.

For example, I have a lot of minor allergies and suffer from motion sickness, so when necessary I take Benadryl to relieve these symptoms. I read that diphenhydramine is an anticholinergic agent as well as an antihistamine, and so, with my rudimentary knowledge, I took this to mean that this drug physically reduces the amount of acetylcholine in the nervous system. However, after further reading, it seems like anticholinergics work by binding to acetylcholine receptors, thus blocking the transmission of acetylcholine, leaving an abundance of ACh floating around in the synapses.

Will this process therefore result in a build-up of ACh until the half-life of the Benadryl elapses?

Or will all of the excess ACh be hydrolyzed by acetylcholinesterase, hence confirming my initial assumption that global levels of ACh will be depleted?

I ask because, while a welcome relief to the allergic symptoms and/or motion-induced nausea, Benadryl leaves me in a state of malaise for about 24-48 hours after I take it. That hypnotic drowsiness characteristic of drugs (as opposed to fatigue) leaves me absent-minded, apathetic and unable to concentrate, and I was wondering whether I could alleviate these after-effects by taking a choline supplement such as Alpha GPC? I’m in this zombie-like state of being right now; it’s extremely frustrating. I begin writing a sentence and half way through lose my train of thought, which leads to incessant deleting and retyping. I feel my writing style also becomes very clinical/robotic when I’m feeling this way, whereas normally my language is full of analogies, imagery and metaphors. This is bad news given that I study English Literature with Creative Writing at university and have several major deadlines looming.

I want to start a wider discussion on some of the seemingly paradoxical properties of acetylcholine when it comes to creativity and cognition, but I feel that’s one for another thread :D

Incidentally, if someone took a choline supplement alongside diphenhydramine, would it have any effect? My guess would be no, as I imagine it would simply be added to the heap of ‘locked out’ acetylcholine precipitated by the Benadryl, but correct me if I am wrong.

Thanks for reading, your thoughts are much appreciated :)

Chloe xxx

#2 OFFLINE   hippocampus Re: Countering the effects of anticholinergic drugs

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Posted 16 April 2012 - 02:02 PM

nicotine is cholinergic, although I would advise against it, since it's strongly (!) addictive.
maybe racetams, like piracetam would help - I don't know, just speculating.

#3 OFFLINE   jadamgo Re: Countering the effects of anticholinergic drugs

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Posted 16 April 2012 - 11:53 PM

You could try taking an antihistamine with no anticholinergic properties. The non-drowsy ones like Allegra, Zyrtec, Claritin, and Alavert should help with the allergies, and perhaps the motion sickness.

If they don't help with motion sickness, you could get a prescription anti-nausea drug from a doctor, and specifically ask for one without anticholinergic or sedating properties.

#4 OFFLINE   Billybear185 Re: Countering the effects of anticholinergic drugs

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Posted 20 April 2012 - 03:41 AM

View Postchloliz, on 16 April 2012 - 12:00 PM, said:

Hello all!

As a relative newbie to the field, I’m still trying to get my head around how neurotransmitters actually work, so as to understand how they are being manipulated when we take nootropic drugs/antidepressants, etc.

For example, I have a lot of minor allergies and suffer from motion sickness, so when necessary I take Benadryl to relieve these symptoms. I read that diphenhydramine is an anticholinergic agent as well as an antihistamine, and so, with my rudimentary knowledge, I took this to mean that this drug physically reduces the amount of acetylcholine in the nervous system. However, after further reading, it seems like anticholinergics work by binding to acetylcholine receptors, thus blocking the transmission of acetylcholine, leaving an abundance of ACh floating around in the synapses.

Will this process therefore result in a build-up of ACh until the half-life of the Benadryl elapses?

Or will all of the excess ACh be hydrolyzed by acetylcholinesterase, hence confirming my initial assumption that global levels of ACh will be depleted?

I ask because, while a welcome relief to the allergic symptoms and/or motion-induced nausea, Benadryl leaves me in a state of malaise for about 24-48 hours after I take it. That hypnotic drowsiness characteristic of drugs (as opposed to fatigue) leaves me absent-minded, apathetic and unable to concentrate, and I was wondering whether I could alleviate these after-effects by taking a choline supplement such as Alpha GPC? I’m in this zombie-like state of being right now; it’s extremely frustrating. I begin writing a sentence and half way through lose my train of thought, which leads to incessant deleting and retyping. I feel my writing style also becomes very clinical/robotic when I’m feeling this way, whereas normally my language is full of analogies, imagery and metaphors. This is bad news given that I study English Literature with Creative Writing at university and have several major deadlines looming.

I want to start a wider discussion on some of the seemingly paradoxical properties of acetylcholine when it comes to creativity and cognition, but I feel that’s one for another thread :D

Incidentally, if someone took a choline supplement alongside diphenhydramine, would it have any effect? My guess would be no, as I imagine it would simply be added to the heap of ‘locked out’ acetylcholine precipitated by the Benadryl, but correct me if I am wrong.

Thanks for reading, your thoughts are much appreciated :)

Chloe xxx

To answer your question acetyl-choline does build up when you take anticholinergics drugs. After the anticholinergic drug wares off, the acetyl choline floods through the post synaptic receptors. A good example of this would be galantamine, which is commonly used for lucid dreaming. In order to counteract the effect of anticholinergic drugs take piracetam. I know that this works because I use piracetam for this very reason and I have read that piracetam does have this effect. I would not spend too much money on choline supplements, for the most part they are not necessary.

#5 OFFLINE   chloliz Re: Countering the effects of anticholinergic drugs

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Posted 22 April 2012 - 11:30 AM

Quote

To answer your question acetyl-choline does build up when you take anticholinergics drugs. After the anticholinergic drug wares off, the acetyl choline floods through the post synaptic receptors.

This was the answer I was looking for. I was basically trying to establish whether this sort of brain fog is caused by a sudden overload of acetylcholine or a deficiency in it, as this would be helpful with my forays into the world of nootropic drugs :)

My current hypothesis is that I have always been a very high ACh person. I spend large amounts of time in 'the land of Chloe' as my dad used to call it - to the untrained observer I would appear to be on 'standby', expression glazed, perhaps playing with my hair or wandering around aimlessly (my parents were very worried) - but in my head I'd be traversing the Pacific on a Spanish galleon, or designing my own militia of warrior princess robots, or turning all of my enemies into ladybirds.

In accordance with this conjecture, I have tried a few ACh-enhancing drugs, (Alpha GPC, Galantamine, Piracetam) and the effect is always the same - my brain feels like it's been replaced with cotton wool, and everything around me seems vaguely surreal, as if viewed through a TV screen. Even piracetam on its own makes me feel like a helium balloon, a state in which all I want to think about is the universe and spacetime and what I would do in the event of an apocalypse, which is very annoying when I have a 3000 word essay to write on the pitfalls of editing short fiction (lion yawn).

So I'm increasingly beginning to wonder whether this avenue of noots is worth pursuing at all, and whether I ought to be looking into ways of nudging the catecholamines into action. I am the ultimate sloth, physically and mentally, but every now and then I get a rush of energy and inspiration, start a major project (casting aside all of my mundane and unimportant university assignments), feel super optimistic about life and the world, and then have a massive crash afterwards. The crash consists of every muscle in my body aching and knotting itself up, intense salt cravings (to the point of eating whole oxo cubes and pesto sauce with a spoon) time speeding up tenfold so that it takes me two hours to shower and dress, a pervasive sense of apathy, usually an existential crisis coupled with a steaming slice of thanatophobia, and all vestiges of creativity leaking out through my ears. Oh, and the despair isn't helped with the sudden mountain of work I'm faced with that has accumulated during my week/month/day of blissful ignorance.

The crash always lasts an amount of time corresponding with the high. E.g. at the beginning of every new academic year (September/October) I experience this surge of academic fervour - reading ahead, rambling on in seminars speeding through tangent after tangent, 8 hour stints in the library... you get the picture. I then spend the rest of the winter in my pjs, barely leaving the house, eating mainly toast, feeling like a failure. Occasional bursts of optimism punctuate this hibernatory state of being, for example, this February I spent four days in London, seeing plays and visiting art galleries with my mum. I was so astronomically happy for those four days. Four days after I returned, I was breaking down in  hysterical tears before my GP, telling him I felt like dying, who promptly handed me a prescription for citalopram.

Didn't expect that to turn into a minor life story. Rambling is something of a speciality of mine. But basically, you can see why I might want to change my ways a bit and become more of a functioning human. I'm sick of selling myself short. I get mediocre marks at uni because I get a combination of firsts and thirds in my modules. I'm also dyspraxic, which doesn't help matters.

Anyhow I'll stop wasting your life now; you're free to go and ponder all of the more productive and useful things you could have spent the last five minutes doing :D

Chloe xxx

#6 OFFLINE   Billybear185 Re: Countering the effects of anticholinergic drugs

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Posted 22 April 2012 - 11:49 AM

View Postchloliz, on 22 April 2012 - 11:30 AM, said:

Quote

To answer your question acetyl-choline does build up when you take anticholinergics drugs. After the anticholinergic drug wares off, the acetyl choline floods through the post synaptic receptors.

This was the answer I was looking for. I was basically trying to establish whether this sort of brain fog is caused by a sudden overload of acetylcholine or a deficiency in it, as this would be helpful with my forays into the world of nootropic drugs :)

My current hypothesis is that I have always been a very high ACh person. I spend large amounts of time in 'the land of Chloe' as my dad used to call it - to the untrained observer I would appear to be on 'standby', expression glazed, perhaps playing with my hair or wandering around aimlessly (my parents were very worried) - but in my head I'd be traversing the Pacific on a Spanish galleon, or designing my own militia of warrior princess robots, or turning all of my enemies into ladybirds.

In accordance with this conjecture, I have tried a few ACh-enhancing drugs, (Alpha GPC, Galantamine, Piracetam) and the effect is always the same - my brain feels like it's been replaced with cotton wool, and everything around me seems vaguely surreal, as if viewed through a TV screen. Even piracetam on its own makes me feel like a helium balloon, a state in which all I want to think about is the universe and spacetime and what I would do in the event of an apocalypse, which is very annoying when I have a 3000 word essay to write on the pitfalls of editing short fiction (lion yawn).

So I'm increasingly beginning to wonder whether this avenue of noots is worth pursuing at all, and whether I ought to be looking into ways of nudging the catecholamines into action. I am the ultimate sloth, physically and mentally, but every now and then I get a rush of energy and inspiration, start a major project (casting aside all of my mundane and unimportant university assignments), feel super optimistic about life and the world, and then have a massive crash afterwards. The crash consists of every muscle in my body aching and knotting itself up, intense salt cravings (to the point of eating whole oxo cubes and pesto sauce with a spoon) time speeding up tenfold so that it takes me two hours to shower and dress, a pervasive sense of apathy, usually an existential crisis coupled with a steaming slice of thanatophobia, and all vestiges of creativity leaking out through my ears. Oh, and the despair isn't helped with the sudden mountain of work I'm faced with that has accumulated during my week/month/day of blissful ignorance.

The crash always lasts an amount of time corresponding with the high. E.g. at the beginning of every new academic year (September/October) I experience this surge of academic fervour - reading ahead, rambling on in seminars speeding through tangent after tangent, 8 hour stints in the library... you get the picture. I then spend the rest of the winter in my pjs, barely leaving the house, eating mainly toast, feeling like a failure. Occasional bursts of optimism punctuate this hibernatory state of being, for example, this February I spent four days in London, seeing plays and visiting art galleries with my mum. I was so astronomically happy for those four days. Four days after I returned, I was breaking down in  hysterical tears before my GP, telling him I felt like dying, who promptly handed me a prescription for citalopram.

Didn't expect that to turn into a minor life story. Rambling is something of a speciality of mine. But basically, you can see why I might want to change my ways a bit and become more of a functioning human. I'm sick of selling myself short. I get mediocre marks at uni because I get a combination of firsts and thirds in my modules. I'm also dyspraxic, which doesn't help matters.

Anyhow I'll stop wasting your life now; you're free to go and ponder all of the more productive and useful things you could have spent the last five minutes doing :D

Chloe xxx

First, you are very good at writing. In regard to your problem I suggest who make a life altering decision, in order for you to get over this never ending cycle you seem to be on. I don't know you, so I have no idea what that might be, however from what I have read it looks to be absolutely necessary. On a side note you may want to take omega 3 fish oil for depression, as it seems, from what you told me, you are depressed. 4 grams of quality fish oil containing EPA and DHA is essential.

I wish you the best for your troubles ahead, and hope that you fix your problem.





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