when to take choline bitartrate

Advanced Guide to Choline in Nootropic Stacks

David Tomen
Author:
David Tomen
11 minute read

best form of choline supplement

Choline is often the center of a great nootropic stack. Because without adequate levels of choline in your brain, the rest of your stack is unlikely to work very well.

Choline is neither a vitamin or mineral.  It is a water-soluble “nutrient” related to the B-Vitamin group. Choline was recognized as an “essential” nutrient by the US Institute of Medicine in 1998.[i]  “Essential” because your body cannot make enough choline on its own. You need to get it from food, or a supplement.

Choline is found naturally in eggs, liver, beef, salmon, cauliflower, Brussels sprouts and breast milk. Eggs are often considered “brain food” because they supply high amounts of choline.

Choline is needed by your body for liver function, normal brain function and development, nerve function, muscle movement, cellular energy and metabolism.

Choline assists in methylation involved in genetic expression and the repair of DNA, nerve signaling, and detoxification.

Your brain has a huge appetite for choline. It is critical for the synthesis of the key neurotransmitter acetylcholine. Which your brain uses to maintain clear communication between its billions of neurons.

In fact, choline is so vital to cognition and nerve function that, without it, we couldn’t move, think, sleep or remember anything.

Choline and acetylcholine are needed for the basics of attention, focus, memory, mood, thinking, and sleep.

Not enough choline and you deal with poor recall, memory loss, fatigue, brain fog, inability to learn, feeling irritable or distracted, and difficulty walking or staying balanced.

Stacking Racetams with Choline

If you use any of the racetam-family of nootropics in your stack, you likely should add a choline supplement. Because the racetams all affect choline and/or acetylcholine use in your brain in some way.

  • Aniracetam – releases more acetylcholine (ACh)
  • Coluracetam – increases choline – ACh conversion through the High Affinity Choline Uptake (HACU) process
  • Noopept – modulates ACh transmission
  • Oxiracetam – enhances choline-acetyltransferase (ChAT) which is used to synthesize acetylcholine
  • Piracetam – potentiates the flow of, and increases the effect of ACh
  • Phenylpiracetam – increases the density of ACh receptors
  • Pramiracetam – increases choline – ACh conversion through the High Affinity Choline Uptake (HACU) process
  • Nefiracetam – potentiates nicotinic acetylcholine receptors

I’ll dive into more detail on how each of the racetams affect acetylcholine in your brain in the post on acetylcholine. For now, you should know that when a racetam affects ACh in some way, it usually means you need to make sure more ACh is available. Or the racetam will not be as effective.choline bitartrate vs phosphatidylcholine

The other primary issue facing neurohackers are racetam-headaches. These headaches are unique because they usually only happen in a part of your brain. You’ll get to recognize them for what they are with more experience.

Racetam-headaches are caused by using a racetam without enough supplemental choline. Your brain is telling you it’s starved for choline.

Who Needs Choline

Even if you’re not interested in nootropics or brain optimization, anyone over 45 years can benefit from a good choline supplement. You’ll experience more alertness, energy, faster recall and better memory.

We all need choline for clarity and mental energy. And we have several nootropic supplements to choose from to boost choline in the brain. And increase the synthesis of acetylcholine.

We’ll review the best nootropics for boosting choline in your brain next.

CDP Choline and Alpha GPC together

Best Forms of Choline Supplements

Alpha GPC

Alpha GPC (L-Alpha Glycerylphosphorylcholine) is a choline source derived from soy or sunflower lecithin. This highly bioavailable form of choline quickly enters your brain.

As a nootropic supplement, Alpha GPC is about 40% choline by weight.

Alpha GPC naturally occurs in your brain as a byproduct of phosphatidylcholine (PC). When your brain needs more choline, and choline floating around in your brain is running low, it breaks down PC from cell membranes. And turns it into Alpha GPC.

The combination of the omega-3 fatty acid DHAAlpha GPC, and phosphatidylserine (PS) is used to form brain cell membranes.[ii]

And like other choline supplements, Alpha GPC provides the choline needed to synthesize acetylcholine.

But Alpha GPC is unique from other forms of choline. It helps increase human growth hormone.[iii] It restores and boosts nerve growth factor receptors in the brain.[iv] And stimulates the release of dopamine.[v]

One study in particular demonstrated why Alpha GPC is a favorite among neurohackers. 32 healthy volunteers received either Alpha GPC or a placebo.  Ten days later they were injected with scopolamine to induce amnesia. The researchers found Alpha GPC was able to prevent the impairment of attention and memory normally caused by scopolamine.[vi]

The researchers showed that memory function in healthy young people could be boosted simply by taking Alpha GPC as a nootropic supplement.

But a very recent study published in 2021 conducted with more than 12 million individuals aged 50 years or older who used Alpha GPC for at least 10 years had a 46% increased chance of stroke. So for short-term use Alpha GPC is safe. But if you need a choline supplement for long-term use you may want to consider switching to CDP-Choline (Citicoline) like I did once I read that study.

Choline Bitartrate

Choline Bitartrate is choline combined with tartaric acid to increase bioavailability. One of the least expensive forms of choline, it’s about 40% choline by weight.

Like other choline supplements, Choline Bitartrate provides the choline needed for acetylcholine synthesis. But neurohackers have found this form is not nearly as effective as other forms of choline.

However, if Choline Bitartrate is the only choline supplement you have available, we do have the science to prove it works as a nootropic.

A research team in the Netherlands gave 28 volunteers 2 grams of Choline Bitartrate or a placebo. An hour and 10 minutes after taking the supplements, they had participants attempt to hit the center of a target.

The volunteers who used the choline supplement were not only more accurate at hitting the target center than the placebo group. The also did it faster.

The researchers concluded there was a “choline-induced bias” towards precision, speed and accuracy.[vii] Now logic tells us that you’d have this positive outcome with any choline supplement. So if all you have to take is Choline Bitartrate – you’ll be OK.

Choline Citrate

Choline Citrate is choline combined with citrate which is an ester of citric acid. Citrate is involved in the transport mechanism of acetyl units from its site of synthesis in mitochondria to the site of acetylcholine synthesis.[viii]

And citrate plays another important role in the brain. Citrate is an intermediate in the Krebs cycle (also known as the TCA cycle or Tricarboxylic Acid cycle, or Citric acid cycle).

Citrate synthase catalyzes the condensation of oxaloacetate with acetyl CoA to form citrate. Citrate then acts as the substrate for aconitase and is converted in aconitic acid. This cycle ends with the regeneration of oxaloacetate.

This series of chemical reactions is the source of 2/3’s of the energy we get from food. Most of the energy made available by these steps is transferred to form NADH. Which then drives adenosine triphosphate (ATP) synthesis that fuels mitochondria and provides the energy needed for brain cells.[ix]

One of the less expensive versions of choline, Choline Citrate is about 50% choline by weight. And like other sources of choline, provides the raw material needed to synthesize acetylcholine.

Acetylcholine is the neurotransmitter needed to signal muscle movement.[x] But Choline Citrate is unique because it helps prevent fatigue, muscle aches and pain following a workout.best choline source reddit

I have personal experience with the benefits of Choline Citrate. For years, I saw a rheumatologist who injected cortisone into my shoulder muscles to relieve excruciating pain. Once I began supplementing with 3 – 4 grams of Choline Citrate per day, the severe muscle pain in my shoulders was gone.

So Choline Citrate provides the double benefit of improving concentration, energy levels, focus and memory. Along with less muscle pain and faster recovery after a workout.

CDP-Choline (Citicoline)

CDP-Choline (Cytidine Diphosphate Choline or cytidine 5′-diphosphocholine) is also known as Citicoline. This naturally occurring choline source is present in every cell in your body.

The CDP-Choline supplement is unique as a choline source. Once it’s digested it separates into cytidine and choline. When it gets to your brain it converts back to CDP-Choline.

Choline is needed for the synthesis of acetylcholine. And cytidine is a component of Ribonucleic acid (RNA). This molecule is involved in coding, decoding, regulation and the expression of genes. And once it gets into the brain, it converts to uridine.

When choline is in short supply, neuronal signaling resorts to grabbing choline molecules from phosphatidylcholine (PC) in cell membranes. This is where uridine steps in. Uridine is used to synthesize phosphatidylcholine (PC). Supplemental CDP-Choline provides the uridine needed for this synthesis. Which means that CDP-Choline helps repair those same cell membranes. To maintain neuron integrity.[xi]

CDP-Choline is only about 18% choline by weight. But it packs a punch when it comes to brain optimization. And is a favorite nootropic stack addition with many experienced neurohackers.

CDP-Choline vs Alpha GPC

When it comes to choosing between CDP-Choline or Alpha GPC for your nootropic stack. There really is no contest. These two choline supplements work well together.

The synthesis of acetylcholine (ACh) is largely dependent on the choline provided by phosphatidylcholine (PC).

Alpha GPC is a byproduct of phosphatidylcholine (PC). And supplemental CDP-Choline provides the uridine needed for PC synthesis.

So taken together, you provide your brain with the type of choline it needs right down at the cellular level.

Combining CDP-Choline together with Alpha GPC
 is a winning combination for any nootropic stack.

when to take choline bitartrate

Side Effects of Choline

Choline is considered safe and non-toxic. Small amounts are made in your body. And it is an “essential” nutrient.

But too much choline, like all nutrients and supplements, can become toxic if too much is taken. Or your body does not need supplemental choline.

My wife is a classic example. This stunningly beautiful, charming, intelligent women turns into the Wicked Witch From the West if she takes a choline supplement.

Like any nootropic used for brain optimization, neurotransmitter balance is key. Excess acetylcholine will depress levels of dopamine, norepinephrine and serotonin.

Serotonin and acetylcholine have an inverse relationship in your brain. In other words, as one goes up, the other goes down. So taking too much of a choline supplement can boost ACh too much. And force serotonin levels to drop.

Symptoms of too much choline or acetylcholine can include:

  • Irritability or anger
  • Anxiety and/or depression
  • Fatigue or feeling overly sleepy
  • Trouble concentrating, brain fog, lack of focus
  • Mental confusion or fatigue
  • Decreased motivation
  • Negativity, pessimism, rumination
  • Poor memory
  • Problems understanding or performing tasks
  • Feelings of helplessness or hopelessness
  • Diarrhea, constipation, gas, bloating, nausea, vomiting, dizziness
  • Muscle weakness
  • Tingling or numbness in the arms or legs
  • Joint pain, discomfort or swelling[xii]

Nootropics Expert Recommendation

Every one of us needs choline to function. Choline is an essential nootropic supplement for anyone whose goal is brain optimization.

Choline is needed to synthesize acetylcholine (ACh). We need choline for cell-membrane signaling (phospholipids), lipid transport (lipoproteins), and methyl-group metabolism (homocysteine reduction).[xiii]

We need choline to provide the acetylcholine affected by any of the racetam-family of nootropics.

Your brain will start to literally consume itself to get the building blocks it needs to make acetylcholine. If you don’t provide it with enough choline.

My favorite choline supplements after years of trial and error are CDP-Choline (Citicoline) and Alpha GPC. If I’ve got muscle pain, I’ll take Choline Citrate for a few days. Until the pain goes away.

I use 500 mg of Cognizin™ (branded form of citicoline) per day in my nootropic stack. Cognizin is included in the double-dose of Mind Lab Pro I use every day.

Whenever I feel a racetam-headache coming on I’ll take 500 mg of Alpha GPC. And the headache is gone within 15 minutes.

Your Mileage May Vary. Each of us has a unique body and brain. So what works for me may not work as well for you. Listen to your body and give your brain the choline it needs.

As an Amazon Associate I earn from qualifying purchases. This post may also contain other affiliate links and I will be compensated if you make a purchase after clicking on my links.

[i] Zeisel S.H., da Costa K.A. “Choline: an essential nutrient for public health.” Nutrition Reviews. 2009 Nov;67(11):615-23. (source)

[ii] Kidd P.M. “Neurodegeneration from mitochondrial insufficiency: nutrients, stem cells, growth factors, and prospects for brain rebuilding using integrative management.” Alternative Medicine Revue. 2005 Dec;10(4):268-93. (source)

[iii] Ceda G.P., Ceresini G., Denti L., Magnani D., Marchini L, Valenti G., Hoffman A.R. “Effects of cytidine 5′-diphosphocholine administration on basal and growth hormone-releasing hormone-induced growth hormone secretion in elderly subjects.” Acta Endocrinologica (Copenhagen).1991;124(5):516-20. (source)

[iv] Vega J.A., Cavallotti C., del Valle M.E., Mancini M., Amenta F. “Nerve growth factor receptor immunoreactivity in the cerebellar cortex of aged rats: effect of choline alfoscerate treatment.” Mechanisms of Ageing and Development 1993 Jun;69(1-2):119-27. (source)

[v] Trabucchi M., Govoni S., Battaini F.  “Changes in the interaction between CNS cholinergic and dopaminergic neurons induced by L-alpha-glycerylphosphorylcholine, a cholinomimetic drug.” Farmaco Sci.1986 Apr;41(4):325-34. (source)

[vi] Canal N., Franceschi M., Alberoni M., Castiglioni C., De Moliner P., Longoni A. “Effect of L-alpha-glyceryl-phosphorylcholine on amnesia caused by scopolamine.” International Journal of Clinical Pharmacology, Therapy, Toxicology. 1991 Mar;29(3):103-7. (source)

[vii] Naber M., Hommel B., Colzato L.S. “Improved human visuomotor performance and pupil constriction after choline supplementation in a placebo-controlled double-blind study.” Scientific Reports 2015 Aug 14;5:13188. (source)

[viii] Sterling G.H., O’Neill J.J. “Citrate as the precursor of acetyl moiety of acetylcholine” Journal of Neurochemistry 31(2):525-30 · September 1978 (source)

[ix] Ebenhöh O., Heinrich R. “Evolutionary optimization of metabolic pathways. Theoretical reconstruction of the stoichiometry of ATP and NADH producing systems.” Bulletin of Mathematical Biology. 2001 Jan;63(1):21-55. (source)

[x] Sanders L.M., Zeisel S.H. Choline – Dietary Requirements and Role in Brain Development Nutrition Today 2007; 42(4): 181–186. (source)

[xi] Wang L., Pooler A.M., Albrecht M.A., Wurtman R.J. “Dietary uridine-5′-monophosphate supplementation increases potassium-evoked dopamine release and promotes neurite outgrowth in aged rats.” Journal of Molecular Neuroscience 2005;27(1):137-45. (source)

[xii] Overstreet D.H., Janowsky D.S. “The Role of Acetylcholine Mechanisms in Affective Disorders” American College of Neuropsychopharmacology (source)

[xiii] Penry J, Manore M. ‘Choline: an important micronutirent for maximal endurance-exercise performance?’  International Journal of Sports Nutrition, Exercise and Metabolism. 2008;18:191–203. (source)

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Join The Discussion - 107 comments

Jenna
July 22, 2024

Hi David,
I’m really hoping you can help me figure out why when my Son who is 16 takes PC his thoughts become scrambled. He’s confused about what’s going on around him, can’t keep things straight. He can’t remember things, his mouth movements become “off” like he’s talking with a mouthful of marbles. This has happened 4-5 times over the past few years when I’ve tried giving him PC and a couple other forms of choline but I can’t recall which ones they were. The last time I tried giving it to him it was sunflower lecithin and the same things happened! The reason why I have tried giving him forms of choline over the years is to help his speech and language comprehension and expressive language, working memory and overall cognition. Meanwhile, choline does the complete opposite. This is such a mystery and I think it must be a hint as to what is behind is cognitive issues. Perhaps his receptors are malfunctioning and can’t handle choline? Maybe it’s a severe drop in serotonin? Have you ever heard of this? I bet his body isn’t using choline properly. I wonder what your insight might be on this.

    David Tomen
    July 23, 2024

    Jenna, some people simply cannot use a choline supplement. I first discovered this with my wife who went nuts on one dose of CDP-Choline. Keep in mind the human brain continues to develop until somewhere between 21 – 25 years old. That could be a factor as well.

    Has you son ever been diagnosed with ADHD or autism? If you haven’t had that looked at I suggest you do. Better to catch this while he’s young. I didn’t find out I was Adult ADD until I was 45 years old. I sometimes wonder how different my life would have been esp. relationship and career-wise if I had known much sooner.

Michel
June 16, 2024

Hi. Can I take noopept and choline during the day and 650mg of GABA before sleep?
Thanks

    David Tomen
    June 17, 2024

    Yes

Nadrecnadh
May 15, 2024

Hmm, interesting about citrate, what other natural sources can be used every day, if you do not consume citrus fruits)) or citrate precursors in the body.

I’m also wondering what supplements/nutrition help better convert NAD to NADH?

    David Tomen
    May 19, 2024

    IF you are trying to increase acetylcholine your best option is CDP-Choline or Alpha GPC.

    And your body naturally converts NAD to NADH.

Travis S Gingerich
May 8, 2024

I’m considering combining Alpha GPC and Citicoline. Wondering what’s the best ratio between the two. Considering taking 300 mg of Citicolene, twice daily, alongside 150 mg of alpha GPC choline, twice daily. Or possibly 300 citicolene twice daily with 300 Alpha babyGPC twice daily. What’s your advice please? Thanks!

    David Tomen
    May 9, 2024

    Travis, use either Alpha GPC or CDP-Choline but not both. 300 mg of either twice per day.

Oliver Engholm
May 3, 2024

Hey David, I have another quick question;

Does Huperzine A and Piperine have immediate effects or are they saturational? Would I need to take them every single day for them to benefit cognitive performance? Would 5mg of Piperine and 200mcg of Huperzine A be very beneficial when taken together within my nootropic stack?

Thanks again!

    David Tomen
    May 3, 2024

    Oliver, Huperzine-A must be used only every 2nd or 3rd day. NOT every day or it will build up to a toxic level. Piperine will not have any effect on its mechanism of action.

Oliver Engholm
May 2, 2024

P.S.

What nootropics have immediate benefits upon consumption? I would want something that has immediate benefits 30-60 minutes after consumption. Do you have any recommendations?

Thanks again!

    David Tomen
    May 2, 2024

    Oliver, most amino acids including things like L-Tyrosine, L-Tryptophan, PharmaGABA, and choline supplements like CDP-Choline and ALCAR provide their benefit within 20 – 30 minutes. And they have a short half-life so need to used twice per day.

    There is no reason to use both Alpha GPC and CDP-Choline. And I recommend CDP-Choline for long-term use because Alpha GPC has been shown to increase your chance of stroke.

    And CDP-Choline need to be taken with ALCAR, Vitamins B1 & B5, magnesium and Vitamin D to produce acetylcholine.

      Oliver Engholm
      May 2, 2024

      Thank you so much for your response!

      I see, so would you recommend Alpha-GPC for short-term use to gain the cognitive benefits from it? If so, would you say that a single daily dosage of 600mg would be optimal for good cognitive benefits? I only know that the dosage stems between 300-1200mg.

      Thank you again!

        David Tomen
        May 3, 2024

        Oliver, you don’ need any more than 300 mg Alpha GPC per dose and use it up to 30-times per day. Used short term should not be a problem. It’s long=term use that increases your chance of stroke. But you need to use it with 500 mg ALCAR to produce acetylcholine.

        Oliver Engholm
        May 3, 2024

        I see, would it be beneficial for me to add in Piperine (5mg) into my ‘immediate’ nootropic stack? I’m thinking of combining it with; N-Acetyl L-Tyrosine (1000mg), Alpha-GPC (400mg), Caffeine (130mg) and L-Theanine (130mg). Would it be necessary in your opinion? Would it interfere with my other nootropics when I consume all at once?

        Thanks again!

        David Tomen
        May 8, 2024

        Piperine will not potentiate the effects of the other supplements in your stack. But it is a great nootropic on its own.

        Oliver Engholm
        May 5, 2024

        Would any of these listed ingredients interfere with Cognizin?

        – N-Acetyl L-Tyrosine
        – BioPerine
        – L-Theanine
        – Caffeine

        Thanks!

        David Tomen
        May 7, 2024

        They work together.

Oliver Engholm
May 2, 2024

Hey David! How are you doing?

When it comes to using Alpha-GPC with CDP-Choline, in what ratio do they work the best in when taken together? Can I take both of them at the same time? Would 600mg of Alpha-GPC work well witth 250-500mg of Cognizin?

Thanks!

Elon
April 20, 2024

Hi David,
I get a headache after taking an acetylcholinesterase inhibitor, do you have an idea why that could happen and how I can avoid it? Is it too little choline maybe ??

    David Tomen
    April 22, 2024

    Elon, when you use an acetylcholinesterase inhibitor you are forcing your brain to reuse the acetylcholine that is already present in your brain. If that causes you a head ache it may be you already have too much acetylcholine. There are some (including my wife) who cannot use any type of choline supplement because it’ll cause some crazy type behavior.

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