Lithium Orotate: Just a dietary supplement, not a drug at all, oh no.

This is one of the more irresponsible things I’ve seen recently:

Lithium. As a dietary supplement.

Lithium is a – perhaps the – mood stabiliser used in the treatment of bipolar disorder. It’s been used to treat mania since the 1970’s and is widely prescribed today. People who have been prescribed lithium usually have regular blood tests, because too much lithium can cause kidney damage and do bad things to the thyroid. Lithium’s useful and has saved lives, but it’s not a drug that should be treated lightly.

So how come it’s being sold like a multi-vitamin?

Oh, Dr. Nieper

For the answer we have to go back to the 1970’s and a German doctor called Hans Nieper. Nieper, who died in 1998, was known for his controversial methods of treating cancer, multiple sclerosis and heart disease. using large doses of vitamins, minerals and various extracts, he theorised that combining drugs with specific acids – which he called “mineral transporters” – could more effectively deliver the drug in the patient’s body.

Many drugs need to be in the form of a salt to be stable. Lithium, the kind that actual doctors prescribe, is usually in the form of lithium carbonate. The lithium molecule is combined with a molecule of carbonic acid, to form lithium carbonate. It would be unwise to take pure lithium as adding lithium to water results in what chemists like to call a “brisk exothermic reaction”. To put it another way, you’d end up with no tongue.

The orotate form of lithium replaces the carbonic acid with orotic acid. Nieper believed that combining a mineral like lithium with orotic acid would mean that the drug would be released only inside cells. His own description of this process can be found here.

Saying that Nieper’s approach is outside the mainstream is a little like saying that Las Vegas is on the outskirts of New York. In 1990 the US Office of Technology Assessment prepared a report for Congress on unconventional cancer treatments. Four years before, the FDA had banned the importing of drugs produced by Dr. Nieper:

More than 75 misbranded and unapproved drugs prescribed by Nieper have been detected in mail and personal baggage importations. These are directed to patients who may have been referred to the Nieper clinic by promotional groups in Wisconsin and California, including the recently established Hans A. Nieper Foundation. FDA has advised these groups that they should correct any materials they send out that suggest drugs prescribed at the Nieper clinic can be legally shipped to the United States.

The American Cancer Society reports that the Nieper cancer therapies include the discredited amygdalin (laetrile) and such other unproved substances as Iscador, fresh cell therapy and wobe-mugos enzyme. The American Heart Association says the drugs reportedly used for his cardiovascular treatments include bromelain, carnitine, selenium, magnesium orotate and potassium orotate—for which “there are no significant data indicating that any of these drugs are efficacious.” The American College of Cardiology strongly warns against any use of unapproved drugs for treatment of cardiovascular disease, adding that lithe FDA review process has done much to protect the American people from exposure to unsafe and ineffective drugs.”

And the National Multiple Sclerosis Society advises that the calcium products, including calcium aminoethyl phosphate or CaEAP, frequently prescribed as part of an expensive program of massive drug intake and special diets “has not been demonstrated to be effective in controlled experiments. II The German Multiple Sclerosis Society, according to its counterpart here, strongly advises against the treatment methods of Dr. Nieper.

In a 1981 advisory, the National Multiple Sclerosis Society emphasized that “when a physician makes a claim of producing a clinical improvement in MS, that physician has a moral and professional responsibility to prove scientifically the specificity of the treatment.” Nieper had by then been making claims about multiple sclerosis for more than a decade and had not yet—and still has not—been willing or able to demonstrate the effectiveness of his therapies to other scientists.

(from Quackwatch)

This is, incidentally, why in the USA lithium orotate is marketed as a dietary supplement rather than a drug. Since 1994, the FDA has (by law) regulated dietary supplements as foods rather than drugs. Whereas a drug has (in theory at least) to be shown to be safe and effective in order to be legal, dietary supplements are banned only if they’re shown to be unsafe. Marketing lithium orotate as a dietary supplement is clearly nonsensical and mendacious, it’s the same drug in lithium orotate as in lithium carbonate, the only possible difference is in how the drug is metabolised in the body.

Other Evidence (such as it is)

Lithium orotate is not entirely without an evidence base, although it’s a staggeringly small one. Nieper’s original study was published in 1973. Then three studies on rats were carried out by various people until the end of the 70’s. The first showed no difference between lithium in its carbonate, orotate or chloride forms. A later study involving the same author found that lithium orotate caused kidney problems (although a very large dosage of lithium was used, so it’s unclear how significant this finding is). Between these two studies, a different group of scientists found different results, concluding that “These data suggest the possibility that lower doses of lithium orotate than lithium carbonate may achieve therapeutic brain lithium concentrations and relatively stable serum concentrations.”

Later on in the 80’s, a study involving 105 alcoholic patients (63 of whom dropped out before the six month study was completed) who were treated using lithium orotate and various Nieper-influenced mineral supplements concluded that “Lithium orotate therapy was safe and the adverse side effects noted were minor, i.e., eight patients developed muscle weakness, loss of appetite or mild apathy.”

Finally, last year a case report of a young woman who had overdosed on lithium orotate supplements (which bore the embarrasingly hideous name of “Find Serenity Now”) was published in the Journal of Medical Toxicology. She developed a mild tremor. The authors conclude that “Over-the-Internet dietary supplements may contain ingredients capable of causing toxicity in overdose. Chronic lithium toxicity from ingestion of this product is also of theoretical concern.”

This is not a lot of information to go on. There’s Nieper’s odd and scientifically dubious theories about orotates, a few studies which don’t shed much light on whether lithium orotate actually behaves very differently than lithium, a limited study on alcoholics that doesn’t really prove much either way and someone who overdoses and develops mild symptoms. Frankly, anyone deriving any certainty from this tiny slice of knowledge is crazy. Or trying to sell you something.

Selling Lithium

So, we already know why lithium orotate is sold as a dietary supplement (selling it as the drug it obviously is would incur the wrath of the FDA). But look at the marketing that some of these vendors use. For example, the horribly named Find Serenity Now:

Serenity™ is an all-natural, effective mood enhancer. It promotes a natural balance to moods and emotions. Serenity™ does not lower energy levels and has no known side effects. Serenity™ changes peoples’ lives for the better every single day.

…

A key step in producing Serenity™ is our advanced ‘Micro Vortex Enteric Coating’. This is a required process of Urban Nutrition’s authentic formula, ensuring that the stomach acids are by-passed so the Orotate can carry the natural Lithium and release it within the cells where it is utilized as a trace mineral in the body.

The combination of the Orotate mineral carrier and our Micro Vortex Enteric Coating manufacturing process make Serenity™ a natural & effective product. This provides optimal absorption and there is little or NO excess lithium left in the body. Research has demonstrated that this does NOT raise the lithium levels in the blood at all or in any significant way. Therefore, toxic levels of Lithium are not an associated problem with Serenity™.

You’ve seen the total extent of research into lithium orotate. Do you think these claims reflect the facts in any way? But that’s OK, because Serenity™ can help you if you have occasional mood swings, could use a boost in your spirits, your marriage suffers from unstable emotions, you’d like a natural mood enhancer, you long to find the person you deserve to be, or even if PMS or menopause feels like a curse.

No mention of actual medical disorders there, so that’s all right then. Still, I do have one question: Who the hell takes lithium in order to find the person they “deserve to be”?

Another lithium orotate supplement Symmetry Homeopathic Spray from HBC Protocols™ seems a little more bold in its claims to:

Oh, that bit about being FDC/NDC (National Drug Code) Registered? That’s a bit of regulatory fluff. The FDA maintains a database of drug products. It publishes a database of prescription drugs and insulin products (which Symmetry, being neither, doesn’t appear on). You submit your product’s data to the FDA and they give you a number. Implying that this is some kind of mark of approval is like me saying that the UK government approves of me because hey, I have a national insurance number.

No, I’m not sure what makes it a homeopathic spray either.

They also say:

If you cannot tolerate higher doses of lithium due to side effects you might try replacing it with lithium orotate. It requires no blood tests and side effects are pretty much non-existent. It is non-prescription and even at lower doses is just as effective as much higher doses of the prescription forms of lithium.

Strong claims, especially given the incredibly limited amount of evidence for lithium orotate. And isn’t it kind of irresponsible to recommend that people who are taking lithium (who will almost certainly have been prescribed it) should switch from an approved form of the drug to a form that was last studied with any seriousness in the 1970’s?

Come back FDA, all is forgiven

These aren’t the only places selling lithium orotate while implying that it’s a great replacement for your regular lithium. There’s hundreds of alternative medicine places online that seem to be at it. It seems stunningly irresponsible to me and I’m mildly surprised that the FDA haven’t been around with their big hammer of regulation. I don’t approve of everything the FDA do (then again, it’s not like I have to care – I’m English), but isn’t this precisely what the FDA is for?

They do appear to have stopped a shipment of Chinese-produced lithium orotate from entering the USA in January on the basis that it’s an unapproved drug, but these ‘dietary supplements’ are still available.

There appears to be at least one UK company that sells the drug, too.

Lithium is a powerful drug and even if you believe the unsupported assertion that the orotate salt is miraculously side-effect free, anyone taking it probably needs to do so under the supervision of someone who knows what they’re doing, what lithium toxicity looks like and is able to evaluate whether the stuff is working or not. This is true for lithium carbonate and I’d say it was even more important for this stuff to be in place when we’re talking about a mostly untested variant with such a small evidence base.