Is lithium orotate safe, toxic or dangerous? Lithium orotate side-effects

 Lithium
Toxic Metal or Essential Nutrient ?

 PeterSmithUK.com © 2016 (#3)

Lithium is a not really a drug it’s an essential nutritional mineral that can be used as a drug when taken at very high doses but in tiny amounts it’s actually an essential nutrient and we need to ingest a few milligrams a day to maintain the health of our body (1).  It’s so beneficial for the health of the brain in particular that rather than wanting to avoid lithium you want more lithium in your diet.
 
It’s true that when administered at very high doses (say 170 mg) lithium can become toxic but then so could zinc, magnesium or almost any nutrient if you ingested enough of them.Lithium orotate toxic or safe
It’s a mistake to think of lithium as a highly toxic metal like say lead or mercury that you want to completely avoid, the opposite is the case when animals are fed a lithium-free diet they develop health problems in several areas of the body as we’ll see in the section lithium the new essential nutrient it is now known that lithium is an essential nutrient needed for various systems in the body to work properly; there’s also strong evidence that people living in areas with higher levels of lithium naturally occurring in their drinking water have better mental health and longer life spans.  So you don't want to avoid lithium you want more lithium in your diet and can consider supplementing safe low-doses of lithium for a wide variety of conditions including: PTSD, OCD, alcoholism, bipolar depression, unipolar depression, migraine/cluster headaches, improving low white blood cell count, juvenile convulsive disease, liver disorders, recovery from stroke, traumatic brain injury, mild cognitive impairment, Alzheimer's disease, histamine  reactions contracting the airways in the lungs, metal toxicity, inflammatory bowel disease and hyperthyroidism.
 
On this page I discus:-

  • Misunderstanding lithium’s toxicity
  • Misunderstanding high dose vs. low doses of lithium
  • Lithium- orotate vs lithium-carbonate
On other pages I discuss the role of lithium is an essential nutrient and how to use it at low doses for various health problems including bipolar syndrome:-
 

Misunderstanding Lithium’s Toxicity

It can be hard to change your mind from deeply ingrained popular thinking and there’s so much information online about lithium being a toxic metal so I’m going to go on at length in this section.Lithium orotate toxic dosage
 
We now know that at the right dosage lithium is an essential nutrient, animals fed a lithium free diet get sick, no one for sure what’s the ideal intake of lithium to maintain optimum health but diets supplying 1-2 mg of lithium a day seem to confer significant mental health benefits so let’s say the optimal daily intake for lithium should be about 2 mg, but the dosage typically used in psychiatry as 170 to 190 which is 85 to 95 mg times more than 2 mg. That which would be like swallowing 85 X 15 mg zinc supplements giving you 1275 mg of zinc, now as little as 200 mg of zinc is toxic and doses from 70-90 mg taken over a long time could cause toxicity, that means just 13 times the recommended daily allowance (RDA) of zinc is acutely toxic and continuous consumption of 4-6 times the RDA could cause toxicity. This means I routinely prescribe and take myself a dose of zinc that is closer to the toxic level of zinc than the therapeutic dose of lithium I take is to the toxic level of lithium; but just because zinc can be toxic at high doses shouldn’t put you off using 15 to 45 mg of zinc a day for therapeutic purposes. In another example the minimum RDA for magnesium varies but let’s say it’s 400 mg and I routinely prescribe 800 mg from four magnesium tablets; now 400 mg × 85 would be 34,000 mg or 170 of the tablets I use!
 
So understand that everything you have probably ever heard about lithium toxicity relates to the very high doses of lithium (in the form of lithium-carbonate) used in psychiatric medicine and as you can see they are very high doses indeed, but you can supplement lithium in the form of lithium-orotate which I’ll discuss below is better absorbed into the brain and can be used at much lower doses safely and effectively.
 
Furthermore just like zinc and magnesium know if you consume too little you become deficient and your health declines, well it’s the same with lithium, for optimum brain health I typically prescribe from as little as 1 mg all the way up to 10 mg.
 
In addition to being an essential nutrient lithium antagonises and helps detoxify toxic heavy metals including aluminium, arsenic cadmium, lead and mercury; so lithium is not a toxic metal, it combats poisonous metal toxicity.
 
Unfortunately information about lithium’s potential for toxicity has come to dominate people’s impression of this essential nutritional element and many people I meet in my practice are reluctant to take this valuable supplement, I hope with the information in this section you’ll update your understanding on this essential nutritional mineral.  For almost 2 decades I resisted taking lithium myself despite living with bipolar syndrome, even after I first heard of low-dose lithium I was still reluctant to take it because I had been led to believe that lithium was a toxic substance best avoided; eventually after learning about the tremendous health benefits to the brain (especially the brains of people with bipolar syndrome) I decided that I would like to obtain the benefits of lithium if only I could work out how to obtain the benefits without the toxic side-effects, in the section How to Use Low-Dose Lithium-Orotate I explain how to enhance the effectiveness of lithium so that you can extract a potentially powerful therapeutic effect from very low doses of lithium and avoid the toxicity risk.
 
A simplistic overview is that in terms of potential toxicity high doses of lithium can be toxic for the kidneys and may also cause unpleasant mental effects such as emotional numbness however for the brain itself lithium is a non-toxic and very healing substance even when taken at high doses.
 
When prescribed at high doses lithium can harm the kidneys, cause fluid retention and weight gain, digestive disturbance, fine muscle tremors and emotional numbness, but let’s not throw the baby out with the bathwater (I probably should stop using expressions like that because some people translate my site), lithium can be highly effective at controlling bipolar mania, some people don’t suffer very much with the side-effects and some people literally have their lives transformed in a positive way by taking lithium it literally gives them their life back, so even if they do have some unwanted side-effects these may be the lesser of two evils. I remember the story of a woman who had many good years free from bipolar syndrome by taking lithium-carbonate, she was able to work, maintain her marriage and raise a family until tragically she had to discontinue using lithium-carbonate because the dosage she needed to maintain her mental health was poisoning her kidneys and she had to make a hard trade-off between mental health versus kidney failure.
 
When prescribed at low doses lithium can exert a very protective effect on the brain, it preserves brain volume by preventing brain shrinkage which slows down brain ageing, cognitive decline/Alzheimer’s disease, it can be a remedy for cluster headaches, migraines, inflammatory bowel disease, asthma, herpes, it can be helpful for alcoholism, depression and I believe by enhancing its effectiveness of low-dose lithium can be an effective remedy for bipolar syndrome; taking supplemental lithium may also prevent health problems in a variety of systems in the body from lithium deficiency. I’ll talk about how lithium is an essential nutrient and the many potential therapeutic applications of taking lithium in another section.
 

Is Lithium Orotate Toxic?

The toxic and therapeutic levels of lithium from lithium-carbonates has been thoroughly researched and is well known because it’s so widely used in psychiatric medicine however the toxic and the therapeutic levels of lithium from lithium-orotate has hardly been researched at all so how can you be sure it’s safe to take 5 to 10 mg of lithium from lithium-orotate? Well there is a documented case of poison from lithium-orotate that gives us some useful insight: An 18-year-old girl swallowed 18 tablets of 120 mg lithium-orotate in one go which would contain 82.7 mg of lithium, she complained of nausea, vomited. She was medically examined and all her vital signs were found to be normal the only finding was a mild tremor, she was given intravenous fluids and anti-nausea medication; after three hours of observation nausea and tremor is resolved and she was transferred (returned from what I can gather) to psychiatric hospital. It would be nice to have more examples of lithium-orotate safety/toxicity but from this example it doesn’t look particularly bad, I would imagine I could produce a similar or worse effect by swallowing 18 salt spoons of table salt in one go.
 
Of course as well as the potential toxicity from single high doses we have to consider the effects of consuming a low-dose of say 5 to 10 mg on a long-term basis. Now I take my own health very seriously and endeavour to avoid toxic substances as much as possible, I’m one of that people that eats organic food, filters their tap water and uses hypoallergenic household cleaning and toiletry products. One of the main reasons I use natural dietary supplements and herbs to treat my condition as opposed to pharmaceutical drugs is to avoid the toxic side-effects of the drugs (the other main reason is because it gives me greater flexibility and control). A big part of my practice involves detoxifying the body for a healing effect, toxins in the brain can cause inflammation and interfere with healthy brain function, some toxins particularly things like toxic heavy metals can even directly interfere with our ability to metabolise neurotransmitters; I must say however that I’ve never seen detoxification on its own cure serious mental health problem.
 
Although I’m prepared to experiment on myself with new treatments I don't play Russian roulette with my health, if I thought that low-dose lithium-orotate supplements were even slightly toxic I would be reluctant to use them. I cannot find any evidence of low-dose lithium-orotate producing toxic effects and I believe it to pose no toxic risk at all. I must say for the record however that lithium-orotate has not been well researched.
 
You may have noticed earlier I said practically all the information you see about lithium toxicity relates to the high doses used in psychiatry, I have also read a few stories of people that say they were made ill by taking lithium-orotate but this does not put me off, I’m genuinely sorry they are ill but when I read their stories it sounds like there was a lot of other unknown things going on or they took the lithium on its own and didn’t combine it with at least a multivit/mineral or they had the wrong diagnosis, or they took lithium just as a study aid, or they didn’t start with a tiny dose and as a test to see what would happen.  Lithium stimulates neuroplasticity (the growth of new connections in the brain) this occurs especially in areas and circuits of the brain that are worked and stimulated and it is possible to have negative neuroplasticity whereby you grow and stimulate fear or anxious circuits, but don’t let that put you off because it’s easy to avoid this simply by starting to stimulate the brain to make desirable neuroplastic changes with appropriate brain training (therapy, meditation, relaxation brain training) and as soon as things start to shift you can increase neuroplasticity safely, like growing muscles with exercise the brain favours new growth, the newly stimulated circuits change grow faster than established circuits. Indeed some brain scans of before and after therapeutic brain training such as mindfulness show the old undesirable circuits actually shrink and lithium can help you achieve this remodelling of your brain more quickly, but don’t just drop lithium on its own into an unhealthy brain and hope for the best, use it as part of a therapeutic strategy.
 

High vs. low doses of lithium 

900 mg of lithium-carbonate = 170 mg elemental lithium
120 mg of lithium-orotate = 4.6 mg elemental lithium
 
A typical prescription in psychiatric medicine would contain:
170-225 mg of elemental lithium from 900-1200 mg of lithium-carbonate.
In my practice for general brain health to support neuroplasticity I prescribed as little as 1 mg of elemental lithium from 30 mg of lithium-orotate, this is just over a mere 0.68% or 1/148th of a standard dosage prescribed in psychiatric medicine for people with bipolar syndrome.
 
When I want a strong effect to control bipolar mania or strongly stimulate neuroplasticity I’ll prescribe approximately 9 mg of lithium from 240 mg of lithium-orotate, this is just 5.4% or 1/18th of the standard psychiatric dosage.
 
As you can see these are tiny amounts and compared to the standard doses of lithium from lithium-carbonate used in psychiatry and are minuscule compared to the higher doses used in psychiatry.
 
For a more detailed breakdown See Understanding Lithium Dosages 
 

Low lithium-orotate may be safe but does it work?

Indeed the dosages I use are so low some doctors may believe they’re too low to produce a therapeutic effect but there’s Lithium orotate the sale  UKevidence from the US and Japan that even slight elevations in the consumption of lithium in drinking water (in the order of a milligram two) reduces the rate of suicide; preventing death from suicide is powerful no? {Insert reference}. There are other human studies showing that administering as little as 0.5 mg halted Alzheimer’s progression[ii] {insert reference}; so small doses clearly can have powerful effects for some conditions but can they have an effective mood stabilising effect on bipolar syndrome including bipolar type I?
 
What I do in my practice is combine the low dose lithium with a diet and supportive supplements that assist lithium’s actions in the body and enhance its therapeutic effects thereby extracting the Lithium orotate for bipolar depressionmaximum possible effectiveness from a very low and safe dose. I explain how to do this in the section:
How to Get the Benefits of Lithium without the Side-Effects
 
In my practice I’ve used doses of lithium from 1-2 mg to as low as 0.1 mg and found them to be therapeutically useful for improving sleep, adjust sleep timing and general brain health; for people requiring a mood stabilising effect for bipolar syndrome however I used doses of between 5-10 mg.
 

Lithium-orotate versus lithium-carbonate. The difference

Lithium comes in different forms: carbonate, orotate.  

Lithium-carbonate is the form of lithium typically used in psychiatric medicine to stabilise bipolar syndrome. It is usually prescribed at very high dosages that are uncomfortably close to toxic levels and even with  frequent blood tests people can and do suffer from lithium-carbonate toxicity which damages the kidneys.   Another problem with high doses of lithium-carbonate is weight gain which probably occurs in about half of people that take it. 
 
Lithium-orotate is the alternative non-prescription form of lithium I use both personally and prescribe in my practice.  You often see it suggested online that lithium-orotate is better absorbed from the intestines than lithium-carbonate but in fact there appears to be little difference in this regard.
 
The big difference between lithium-orotate and lithium-carbonate is that lithium orotate passes the blood brain barrier more effectively than lithium-carbonate and delivers significantly more lithium to the brain where we want it. Furthermore when lithium is administered in the form of lithium-orotate it is retained in the blood and brain far longer than when delivered by lithium-carbonate versus lithium-orotate maintains far more stable levels of lithium in the system.
 
In one study 24 hours after injection of lithium-carbonate little lithium was retained in the blood compared to 2/3 of the level of lithium being retained when the same amount of lithium was injected from lithium-orotate and the level of lithium in the brain was three times greater from lithium-orotate compared to lithium-carbonate[iii].
 
I take about 10 mg of lithium a day from 240 mg of lithium-orotate, which may be delivering level of lithium to my brain equivalent to 30 mg of lithium from lithium-carbonate; this is still a very low dose but as I explain elsewhere I enhance its effectiveness with the right combination of diet and remedies to produce an useful therapeutic effect. 
 
At these low doses it does not cause weight gain, emotional flatness or require regular blood tests to monitor for toxicity.
 
There's been too little scientific research to be absolutely certain but it appears that the salt (either carbonate or orotate) that the lithium is attached to has an effect on either how well the lithium is absorbed from the blood into the cells and how quickly or slowly it is excreted by the kidneys, or put another way how long it is retained in the body.
 
People used to believe that lithium orotate was better absorbed from the intestines than lithium carbonate but it now appears that both lithium-orotate and carbonate are well absorbed from the intestines, however the lithium-carbonate is not as well absorbed from the blood into the brain where it is needed as lithium-orotate and therefore you have to take a higher dose of lithium from carbonate and maintain a higher level lithium carbonate in the blood to force it into the cells.
 
It also appears that lithium-orotate is excreted more slowly by the kidneys, this may make it easier to maintain a constant level of lithium in the system however it could also potentially make it more toxic to take too much over time.
 
There was an experiment conducted in the 1979 {ref?} in which rats were given an equal dosage of elemental lithium from lithium-carbonate and lithium-orotate and the rats given lithium-orotate suffered kidney toxicity. This experiment demonstrated what we in nutritional medicine have been saying for years and that is the format a mineral is delivered in or what it is attached to can have a profound effect on how the mineral behaves in the body and that different forms of lithium salts do indeed behave differently.
 
What the experiment doesn’t show is how does a therapeutic dosage of lithium-carbonate (say 900 mg for human) compares to the therapeutic dosage of lithium-orotate (say 240 mg for human). Unfortunately no one has performed an experiment using typical therapeutic doses of lithium-orotate gradually increasing them to reveal the upper toxic level for this lithium salt.
 
Supplementing lithium does me so much good I regret that it took me so many years to change my thinking and discover how to use it, now I love and appreciate this amazing nutritional mineral.
 
FURTHER READING
 
Lithium-orotate for bipolar syndrome
How to get the benefits out of low-dose lithium without the toxic side-effects
 
Understanding Lithium Dosages
 
Lithium the new essential nutrient, Are You Lithium Deficient?
 
Lithium isn’t only for bipolar syndrome, other health benefits of supplementing non-toxic low doses of lithium 
 
J Am Coll Nutr. 2002 Feb;21(1):14-21.
 Lithium: occurrence, dietary intakes, nutritional essentiality. Schrauzer GN1.
 
Abstract
 
Lithium is found in variable amounts in foods; primary food sources are grains and vegetables; in some areas, the drinking water also provides significant amounts of the element. Human dietary lithium intakes depend on location and the type of foods consumed and vary over a wide range. Traces of lithium were detected in human organs and fetal tissues already in the late 19th century, leading to early suggestions as to possible specific functions in the organism. However, it took another century until evidence for the essentiality of lithium became available. In studies conducted from the 1970s to the 1990s, rats and goats maintained on low-lithium rations were shown to exhibit higher mortalities as well as reproductive and behavioral abnormalities. In humans defined lithium deficiency diseases have not been characterized, but low lithium intakes from water supplies were associated with increased rates of suicides, homicides and the arrest rates for drug use and other crimes. Lithium appears to play an especially important role during the early fetal development as evidenced by the high lithium contents of the embryo during the early gestational period. The biochemical mechanisms of action of lithium appear to be multifactorial and are intercorrelated with the functions of several enzymes, hormones and vitamins, as well as with growth and transforming factors. The available experimental evidence now appears to be sufficient to accept lithium as essential; a provisional RDA for a 70 kg adult of 1,000 microg/day is suggested.
PMID: 11838882
[ii] {Curr Alzheimer Res. 2013 Jan;10(1):104-7. Microdose lithium treatment stabilized cognitive impairment in patients with Alzheimer's disease. Nunes MA, Viel TA, Buck HS.
[iii] J Pharm Pharmacol. 1978 Jun;30(6):368-70. Rat brain and serum lithium concentrations after acute injections of lithium carbonate and orotate. Kling MA, Manowitz P, Pollack IW. PMID:26768
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