Choline Information by Ray Sahelian, M.D. Health benefit and side effects of choline supplement

What you will find on this page:
Choline research
Choline bitartrate supplement
Mind Power Rx with choline for mind, memory, and mood support.
Passion Rx - a sexual enhancement product for men and women
Diet Rx with choline to help you eat less

Choline is an essential nutrient required by the body to make several important compounds necessary for healthy cell membranes. Choline helps form phosphatidylcholine, the primary phospholipid of cell membranes. Choline is also the precursor to acetylcholine, one of the crucial brain chemicals involved in memory. A major use of choline in the body is the formation of betaine, an important methyl donor. Furthermore, choline helps transport of lipids from the liver.

Choline Bitartrate, 500 mg, 60 Capsules
Physician Formulated by Dr. Ray Sahelian, M.D.

Get a FREE Diet Rx bottle, see below
Choline is an essential precursor of acetylcholine, a stimulatory neurotransmitter. It also helps in the production of lipotropic agents which converts fats into useful products and aids in the production of HDL (good) cholesterol.*This choline supplement is 100 % natural choline bound to tartaric acid, making it easier to absorb.

Choline Supplement Facts
Choline - 500 mg * (as Choline bitartrate)

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Subscribe to a FREE Supplement Research Update newsletter. Twice a month you will receive a review of several studies on various supplements and natural medicine topics - including the role of choline in health and disease - and their practical interpretation by Ray Sahelian, M.D.

Usage: Take half or 1 choline capsule a few minutes before breakfast or lunch or as directed by your health care provider.
* Choline daily value not established

Choline availability
Choline is sold in dosages ranging from 250 to 500 mg and in a number of forms including choline bitartrate, choline chloride, and choline citrate. Many brand names are available.
Choline is also found in Diet Rx, a natural diet pill that helps you eat less.

Mind Power Rx with Choline and Inositol - Formulated by Ray Sahelian, M.D.

Mind Power Rx with Choline is a sophisticated cognitive formula. It combines a delicate balance of brain circulation agents and neurotransmitter precursors with powerful natural brain chemicals that support:

Memory and Mood
Mental clarity
Concentration 
Alertness & Focus

Why buy choline and all the individual herbs and nutrients separately -- at great expense -- when you can buy this excellent combination? The herbs in Mind Power Rx include: Ashwagandha, Bacopa, Fo-Ti, Ginkgo biloba, Ginseng, Mucuna pruriens, and Reishi.  The nutrients and vitamins in Mind Power Rx include Acetyl-l-Carnitine, Carnitine, Carnosine, Choline, Inositol, DMAE, Methylcobalamin, Pantothenic acid, Trimethylglycine, Tyrosine, and Vinpocetine.
Click Choline above in blue for more information

Libido effects of choline
Choline is discussed in the book Natural Sex Boosters by Ray Sahelian, M.D.  For consistent libido and sexual enhancement, read on....

Passion Rx -- for Men and Women with Choline bitartrate -- Formulated by Ray Sahelian, M.D.

How quickly does Passion Rx work?
Passion Rx provides results that are sometimes seen within hours, but continue to improve the next day, and over several days of use. Our feedback thus far indicates more than 85% user satisfaction by the first week.
Dr. Sahelian and his research staff have tested various doses and extracts of exotic herbs from a number or raw material suppliers to determine the ideal dose and combination for optimal libido enhancement with fewest side effects. After years of trial and error, a UNIQUE proprietary blend with 15 herbal extracts, has been created which works within hours with the fewest side effects. This unique blend is a close kept secret known only to Dr. Sahelian and his research staff. You will only find this exact combination in Passion Rx.

Passion Rx supports:

The potent herbal extracts in Passion Rx include Ashwagandha, Catuaba, Choline bitartrate, Cnidium, Coleus forskohlii, Damiana, Horny goat weed, Maca, Mucuna pruriens, Muira puama, Passion flower, Pfaffia paniculata, Rehmannia, Rhodiola, Tribulus, and Tongkat Ali.

Click the link above for Choline for more information about Passion Rx

Choline in our diet
Choline, usually as part of phosphatidylcholine, is widely available in a number of foods, particularly eggs, fish, legumes, nuts, and meats and vegetables, as well as in human breast milk. Dietary intake of choline ranges from 300 to 900 mg a day. Most individuals who have a normal diet are not deficient in choline. The importance of choline was emphasized in 1998 when the National Academy of Sciences classified it as an essential nutrient. In the past, it was thought that the human body made adequate amounts when needed. However, a study by Dr. Steven Zeisel, from the Department of Nutrition at the University of North Carolina at Chapel Hill, demonstrated that volunteers on a choline deficient diet were not able to produce enough of this nutrient.        

Choline studies
Several studies have been done administering choline to humans in order to evaluate memory function. The results have been mixed with some showing positive results (Sitaran 1978) while others indicating no improvement (Mohs 1980). Choline has also been tested in bipolar disorder, also known as manic-depression. When six patients already on lithium were given choline bitartrate, five of them had a reduction in manic symptoms (see study at bottom of page).

Phosphatidylcholine and Homocysteine
A report in the July 2005 issue of the American Journal of Clinical Nutrition, indicates that a daily dose of choline, supplemented as phosphatidyl choline, lowers fasting as well as postmethionine-loading plasma homocysteine concentrations in healthy men with mildly elevated homocysteine concentrations. If high homocysteine concentrations indeed cause cardiovascular disease, choline intake may reduce cardiovascular disease risk in humans. The mechanism may be the ability of choline to be transformed into betaine, also known as trimethylglycine.
Higher intakes of dietary choline and betaine are related to lower homocysteine concentrations independent of other determinants, including folate and other B vitamins.

Choline Side effects
A common side effect of choline ingestion is increased body temperature and sweating. Nausea and loss of appetite can result from very high doses. Most people notice having more focus and being more alert. A positive side effect is that choline helps with erections.

Dr. Sahelian’s Experience
Within a few hours of taking choline, I notice an improvement in mental focus that lasts most of the day. I have not experienced side effects with dosages smaller than 500 mg. On a dosage of 750 mg, I experience increased body warmth and slight nausea.

Choline and Pregnancy
Pregnancy may deplete the amount of choline found in the liver resulting in reduced methylation of homocysteine. The demand of choline during pregnancy is very high due to the transport of choline from mother to the fetus. High intake of choline in pregnant women is important to lower the risk of neural tube defects.
   According to the results of several studies in rats, providing choline during pregnancy enhances memory and learning capacity in the fetus (Williams 1998). Dr. Christina Williams, a behavioral neuroscientist at Duke University in Durham, North Carolina, says her study findings demonstrate, "That supplementation with choline during the last third of pregnancy has fairly dramatic and long-lasting effects on the memory of offspring." A 1997 study published in Advances in Pediatrics by Dr. Zeisel showed that choline reserves are depleted during pregnancy and lactation (Zeisel 1997). This depletion may affect normal brain development and memory in the offspring. The National Academy of Sciences suggests that pregnant women consume at least 450 milligrams of choline per day.


Choline
Recommendations
Individuals whose diet includes a wide variety of foods are not likely to suffer from choline deficiency. Growing infants, pregnant or lactating women, and individuals with liver cirrhosis may potentially be deficient in choline (Zeisel 1994). Whether choline supplements benefit older individuals with age related memory decline has not yet been adequately determined. Because of its relative safety, and potential benefits, I recommend small amounts of choline in the elderly who have age related cognitive decline. See chapter 18 for specific recommendations. Choline can be taken occasionally by younger individuals on days when better concentration and focus would be helpful.

Various forms of choline
You can find choline as part of phosphatidyl choline (lecithin), choline chloride, cdp choline, choline bitartrate, choline inositol combination, etc.

Choline deficiency
In many mammals, including baboons, long term (weeks to months) ingestion of a diet deficient in choline but adequate, though limited, in methionine and folate leads to hepatic, renal, pancreatic, memory, and growth disorders. Muscle damage also occurs from choline deficiency.
     A choline -deficient diet increased DNA damage in humans. Subjects in whom these diets induced liver or muscle dysfunction also had higher rates of apoptosis in their peripheral lymphocytes than did subjects who did not develop organ dysfunction. Assessment of DNA damage and apoptosis in lymphocytes appears to be a clinically useful measure in humans (such as those receiving parenteral nutrition) in whom choline deficiency is suspected.

THE MEMORY NUTRIENTS—CHOLINE AND PHOSPHOLIPIDS
from the book Mind Boosters by
Ray Sahelian, M.D.

Like omega-3 fatty acids, phospholipids are also important for optimal brain health. As the name implies, phospholipids are made of the combination of lipids (fats) and the mineral phosphorus. Phospholipids are found in high concentrations in the lining of practically every cell of the body, including brain cells. They help brain cells communicate and influence how well receptors function. Although present in many foods, phospholipids are found in higher concentrations in soy, eggs and the brain tissue of animals. There may actually be a biochemical rational for the folk wisdom that says eating brain makes one smarter. The two most common phospholipid supplements sold over the counter are phosphatidylcholine and phosphatidylserine. Phosphatidylcholine is also known as lecithin. This chapter explains the role and function of phospholipids, their clinical effects, and practical recommendations for or against supplementation.

In addition to these phospholipids, I will also discuss choline, a nutrient that helps form phosphatidylcholine. Choline is the precursor to acetylcholine, the brain chemical involved with memory. Choline has been sold over the counter for many years. A new and more activated form of choline, called CDP-choline, became available in the US in 1998.

What Benefits Do Choline and Phospholipids Provide?
Individuals who don’t have a good dietary intake of phospholipids may find that taking these nutrients leads to an improvement in learning and memory. Most young and healthy people who take phosphatidylcholine or phosphatidylserine are not likely to notice any significant changes, although supplements could help some seniors. The effects from choline, and its cousin CDP-choline, are more noticeable.

Which Conditions Can Choline and Phospholipids Benefit?
The clinical application of these nutrients has not yet been fully evaluated, but scientists have studied their role in age related cognitive decline (ARCD), Alzheimer’s disease, and Parkinson’s disease. No firm conclusions are yet available as to whether phosphatidylserine and phosphatidylcholine help these conditions. Choline and CDP-choline could potentially be beneficial in ARCD and Alzheimer’s disease.

The Making of Phospholipids
In order to better understand how the nutrients in this chapter work, it helps to know how they are related to each other. As you can see from figure 8.1, PS can be converted into phosphatidylcholine. Choline converts into CDP-choline and then phosphatidylcholine. All of the nutrients listed in this figure, except for acetylcholine, are available over the counter as supplements. Acetylcholine is a brain chemical, among various other functions, involved in memory and learning.

                                      Choline ß à Acetylcholine
           â
 
                                    CDP-Choline
           â
Phosphatidylserine à Phosphatidylcholine

Figure 8.1 Relation of Choline to Acetylcholine and Phospholipids: from Mind Boosters book
 

Choline Research Update
Synaptic proteins and phospholipids are increased in gerbil brain by administering uridine plus docosahexaenoic acid orally.
Brain Res. 2006 Apr 19; Wurtman RJ, Ulus IH, Cansev M, Watkins CJ, Wang L, Marzloff G.
Department of Brain and Cognitive Sciences, Massachusetts Institute of Technology, MIT, Cambridge, MA
The synthesis of brain phosphatidyl choline may utilize three circulating precursors: choline; a pyrimidine (e.g., uridine, converted via UTP to brain CTP); and a PUFA (e.g., docosahexaenoic acid); phosphatidylethanolamine may utilize two of these, a pyrimidine and a PUFA. We observe that consuming these precursors can substantially increase membrane phosphatide and synaptic protein levels in gerbil brains. Alzheimer's disease brains contain fewer and smaller synapses and reduced levels of synaptic proteins, membrane phosphatides, choline and DHA. The three phosphatide precursors might thus be useful in treating this disease.

Choline deficiency in mice and humans is associated with increased plasma homocysteine concentration after a methionine load.
American Journal of Clinical Nutrition, Vol. 81, No. 2, 440-444, February 2005
Background: Elevated concentrations of homocysteine in blood may be an independent risk factor for the development of atherosclerosis. Elevated homocysteine concentrations can be caused by decreased methylation of homocysteine to form methionine, as occurs in folate deficiency. A parallel pathway exists for methylation of homocysteine, in which choline, by way of betaine, is the methyl donor. Objective: Our goal was to determine whether choline deficiency results in a decreased capacity to methylate homocysteine. Design: C57BL/6J mice were fed diets containing 0, 10, or 35 mmol choline/kg diet for 3 wk. We then administered an oral methionine load to the animals and measured plasma homocysteine concentrations. Also, in a pilot study, we examined 8 men who were fed a diet providing 550 mg choline/d per 70 kg body weight for 10 d, followed by a diet providing almost no choline, until the subjects were clinically judged to be choline deficient or for 42 d. A methionine load was administered at the end of each dietary phase. Results: Two hours after the methionine load, choline-deficient mice had plasma homocysteine concentrations twice those of choline-fed mice. Four hours after the methionine load, clinically choline-depleted men had plasma homocysteine concentrations that were 35% greater than those in men not choline depleted. Conclusion: These results suggest that choline, like folate, plays an important role in the metabolism of homocysteine in humans and that response to a methionine load may be useful when assessing choline nutriture.

Oral choline decreases brain purine levels in lithium-treated subjects with rapid-cycling bipolar disorder: a double-blind trial using proton and lithium magnetic resonance spectroscopy.
Lyoo IK. Brain Imaging Center, McLean Hospital, Belmont, MA, .
Bipolar Disord. 2003 Aug;5(4):300-6.
Oral choline administration has been reported to increase brain phosphatidylcholine levels. As phospholipid synthesis for maintaining membrane integrity in mammalian brain cells consumes approximately 10-15% of the total adenosine triphosphate (ATP) pool, an increased availability of brain choline may lead to an increase in ATP consumption. Given reports of genetic studies, which suggest mitochondrial dysfunction, and phosphorus (31P) magnetic resonance spectroscopy (MRS) studies, which report dysfunction in high-energy phosphate metabolism in patients with bipolar disorder, the current study is designed to evaluate the role of oral choline supplementation in modifying high-energy phosphate metabolism in subjects with bipolar disorder. Eight lithium-treated patients with DSM-IV bipolar disorder, rapid cycling type were randomly assigned to 50 mg/kg/day of choline bitartrate or placebo for 12 weeks. Brain purine, choline and lithium levels were assessed. Patients received four to six MRS scans, at baseline and weeks 2, 3, 5, 8, 10 and 12 of treatment . Patients were assessed using the Clinical Global Impression Scale (CGIS), the Young Mania Rating Scale (YRMS) and the Hamilton Depression Rating Scale (HDRS) at each MRS scan. RESULTS: There were no significant differences in change-from-baseline measures of CGIS, YMRS, and HDRS, brain choline/creatine ratios, and brain lithium levels over a 12-week assessment period between the choline and placebo groups or within each group. However, the choline treatment group showed a significant decrease in purine metabolite ratios from baseline compared to the placebo group, controlling for brain lithium level changes. Brain lithium level change was not a significant predictor of purine ratios.  The current study reports that oral choline supplementation resulted in a significant decrease in brain purine levels over a 12-week treatment period in lithium-treated patients with DSM-IV bipolar disorder, rapid-cycling type, which may be related to the anti-manic effects of adjuvant choline. This result is consistent with mitochondrial dysfunction in bipolar disorder inadequately meeting the demand for increased ATP production as exogenous oral choline administration increases membrane phospholipid synthesis.

CDP-choline increases plasma ACTH and potentiates the stimulated release of GH, TSH and LH: the cholinergic involvement.
Fundam Clin Pharmacol. 2004 Oct;18(5):513-523.
Abstract In the present study, we investigated the effect of intracerebroventricular (i.c.v.) administration of cytidine-5'-diphosphate (CDP) choline on plasma adrenocorticotropin (ACTH), serum growth hormone (GH), thyroid stimulating hormone (TSH), follicle stimulating hormone (FSH) and luteinizing hormone (LH) levels in conscious rats. The involvement of cholinergic mechanisms in these effects was also determined. In basal conditions, CDP-choline increased plasma ACTH levels dose- and time-dependently, but it did not affect the TSH, GH, FSH and LH levels. In stimulated conditions, i.c.v. administration of CDP-choline produced an increase in clonidine-stimulated GH, thyrotyropin-releasing hormone (TRH)-stimulated TSH, LH-releasing hormone (LHRH)-stimulated LH, but not FSH levels. Injection of equimolar dose of choline produced similar effects on hormone levels, but cytidine (1 μmol, i.c.v.) failed to alter plasma levels of these hormones. Pretreatment with hemicholinium-3, a neuronal high affinity choline uptake inhibitor, (20 μg, i.c.v.) completely blocked the observed hormone responses to CDP-choline. The increase in plasma ACTH levels induced by CDP-choline was abolished by pretreatment with mecamylamine, a nicotinic receptor antagonist, (but not atropine, a muscarinic receptor antagonist. The increase in stimulated levels of serum TSH by CDP-choline was blocked by atropine but not by mecamylamine pretreatment. However, CDP-choline induced increases in serum GH and LH levels were greatly attenuated by both atropine and mecamylamine pretreatments. The results show that CDP-choline can increase plasma ACTH and produce additional increases in serum levels of TSH, GH and LH stimulated by TRH, clonidine and LHRH, respectively. The activation of central cholinergic system, mainly through the presynaptic mechanisms, was involved in these effects. Central nicotinic receptors solely mediated the increase in plasma ACTH levels while the activation of central muscarinic receptors was involved in the increase in TSH levels. Both muscarinic and nicotinic receptor activations, separately, mediated the increases in serum GH and LH levels after CDP choline.

Choline Emails
Q. Dear Dr Sahelian, I noticed your Mind Power RX formula does not contain CDP Choline. Does this suggest that CDP choline should not be taken with choline, or is it safe to do so simultaneously?
     A. There are countless supplements and herbs that have an influence on the mind, and we had to limit the number we could place in Mind Power Rx. CDP-choline is an excellent mind nutrient, and it can be taken with choline, just that the dose of CDP-choline and choline need to be reduced in order not to get overstimulated.

Q. I enjoy reading your book "Mind Boosters" in that book  you talked about your experienced with Choline.  I am wondering is there any long term side affects if one were to take it regularly with the minimum dosage?
    
A. No one knows for sure. Our daily intake of choline ranges between 200 to 500 mg through food. It would appear to be safe to take 100 to 200 mg of choline a day as a supplement. Since most capsules contain more than this amount of cholien, you may need to open a capsule and take part of it.

Q. I have heard that taking choline can help some people with liver problems. My problem is my local DR's and I have been unable to locate someone or some place that can conduct a blood test that will measure a serum choline level to identify if there is a deficiency. I have been told that one should find out if there is a deficiency before starting to take a Choline supplement.
     A. Choline deficiency is extremely rare and may occur in those who have malnutrition or are eating a very restrictive diet. Testing for choline in the blood is unlikely to reveal any information that would be clinically helpful. Anyone with suspected liver problems should have blood liver function tests and if abnormal, further studies can be done to determine the problem and course of action.

Q. Is it best to take choline on an empty stomach or with food? At what time of the day is most effective?
     A. Choline is best taken early in the day since it can interfere with sleep if taken in the evening. Taking choline right before a meal is fine although it works well when taken with a meal.

Q. I found the following information on a web site on choline interesting: Choline and sleep -- One of the lesser-known functions of acetylcholine is helping to maintain sleep. Acetylcholine controls the amount of sensory input. It strengthens the so-called stimulus barrier, making it possible to sleep through minor noises and other disturbances. As we age, we tend to become "light sleepers," easily roused from sleep. Menopausal women, who experience a sudden drop in acetylcholine levels due to estrogen withdrawal, often complain about having suddenly become "light sleepers." The same stimulus barrier also helps us concentrate and solve problems. Too little acetylcholine makes us distracted and irritable as too many unimportant stimuli bombard us, in essence preventing us from thinking. I have tried it, but it didn't seem to help, so perhaps I wasn't using enough. I plan on experimenting with higher doses by taking choline chloride.
    A. Based on my understanding of choline, it actually causes alertness rather than help with sleep.

I've had a libido problem for a long time. I stumbled across your website and it occurred to me that my problem might not be solely hormone related, but may be due to the inability of my brain to adequately handle stimulus. I purchased a bottle of Choline Bitartrate, and after almost a week of taking 1 pill per day I have noticed a difference in my sexual response. So far, it seems as if my body has become slightly more responsive to stimulus and I am actually able to become somewhat aroused.

Q. Are the benefits of choline and cdp- choline same other than the faster response of cdp- choline.
     A. It's a good question. Since choline and cdp- choline have not been tested head to head in a human study, it's hard to say.

Q. Can you tell me the difference of choline bitrate and choline chloride? on the web site it only mention:
Various forms of choline: you can find choline as part of phosphatidyl choline (lecithin), choline chloride, cdp choline, choline bitartrate, choline inositol combination, etc.
     A. Practically speaking there is not too much difference between choline bitartrate and choline chloride, but no human studies have been done comparing these two forms to see whether in the long run one form is better than the other.

Q. Since reading about information on choline on your website, I find it very interesting and informative. I've decided to try choline bitartrate of 250 mg. Can I take this choline together with a regular multivitamin pill? Will this help a lot with my studies which involves a lot of memorization? Can I take Vitamin B6 together with choline? What about Taurine, does it functions like choline?
     A.  It is best to learn how each supplement works for you by itself before combining. We don't have as much experience with taurine to know for sure how well it works for memory or mental enhancement.

This choline page was last updated March 2008.