Posts tagged ‘drugs’

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.

May 16, 2008 at 4:56 pm 154 comments


This morning at 8am I found myself sitting on my sofa, with my headphones on, listening to music. I had no memory of what had occured during the previous 24 hours. I was feeling fine, if a little hungry. But I was very confused.

It’s now 10am. It’s taken me a couple of hours to piece together what happened yesterday. I took quite a lot of temazepam during the afternoon, which was dumb and kind of screwed with my memory. But the really interesting part took place later on.

You probably haven’t heard of Ayahuasca. It’s a psychedelic drink used as a sacrament in some South American religions, especially in shamanistic practices. The plants used in it vary dramatically, but generally there’s a plant that contains DMT (N,N-dimethyltryptamine) and a plant that contains harmaline, which is a natural mono-amine oxidase inhibitor. Without harmaline or another MAOI, the DMT is quickly metabolised into inactive compounds by the liver. With it, the DMT hangs around for a few hours and produces all kinds of visions and hallucinations.

I’ve had the ingredients for my own ayahuasca recipe hanging around for the last year or so. Last night I finally brewed some up. This took a while, but turned out to be pleasingly simple. I took some harmaline that I’d previously extracted from some Syrian Rue seeds. And half an hour later, I chugged down half a mug full of DMT laden tea.

I began to feel the first effects about half an hour later. Another half an hour and I was experiencing the most intense visual hallucinations I can imagine. Beautiful crystalline visions. Like nothing I’ve ever seen before.

Let me put it this way: DMT. Is. Fucking. Insane. But there was also something very spiritual about it. As utterly alien and transformed as the drug made my consciousness, it also kept me safe through the whole thing. It’s going to take me a while to integrate the experience back into my everyday mind. Reality was completely shattered.

There’s still some subtle visual effects going on. Everything seems slightly strange. But in a good way. It sounds dumb, especially since I’m an atheist, but somehow I feel blessed.

April 6, 2008 at 9:28 am 3 comments


There was a suggestion earlier in the week that some kind of night out, drinks and rock-club extravaganza might be going on tonight. It’s 8pm now, so my suspicion is that this isn’t now happening. I don’t know whether to be disappointed or relieved. When it was originally suggested my response was that I’d have to see how I felt on the night. Sometimes going to a club is the last thing I want to do. Other times, once I get past the nightmare of hundreds of people in close proximity, it can be quite fun. Doing things like that makes me feel normal; it’s a statement that yes, I can go out and enjoy myself and not turn into some kind of dumb, depressed fool.

I don’t know how I’m feeling. I suspect that if one of my friends were to call, it wouldn’t take much to persuade me to join them. On the other hand, it’s not like I’ve called anyone to enquire if it were still happening. Also, given my recent handling of syrian rue extracts (which as well as being a potent drug also work as a dye), my fingers would probably fluoresce under blacklight, which would look quite cool.

Since it looks like this evening will be spent alone, I may end up using the alkaloids as a drug rather than an unintentional fashion statement.

I don’t know whether to classify this particular kind of drug use as self-destructive or not. I think it’s more that life was a lot better when I was in my experimenting-with-weird-drugs phase and maybe I want to go back there for a while. Another escapist plot, yes, but I’m a fuckin’ expert when it comes to the theory of these substances and there’s about as much physical risk to me as from drinking a pint in a pub. So, fuck it.

My other choice of recreation consists of developing a search engine for my pornography collection. (Actually, I’ve been quietly developing this over the last week or two. It’s quite impressive in a deeply pathetic, way-too-much-time-on-my-hands way. Still, it’s taught me the basic principles of database design and a smattering of SQL; who knew porn could be so educational?) Anyway, the point is, doing drugs isn’t exactly going to distract me from important work.

I don’t know. I’ve been feeling fucked-up in so many ways lately. Is another way going to make much difference?

[2.5 hours pass]

I’ve now smoked a small quantity of the harmala alkaloids, mostly to make sure that my extract is reasonably pure. It was a very smooth smoke actually. The most noticable effect is that the bass-line of the music I’m listening to is much heavier than it usually sounds. Who knew my head had its own graphic equaliser? I feel more relaxed than I have done in a while, which could be placebo, derive from a sense of comfort in reliving my jaded past, or could be a genuine pharmacological effect (it apparently has some benzodiazepine-like anxiolytic effects).

September 22, 2007 at 9:37 pm Leave a comment

A Little Kitchen Chemistry

Boredom is a terrible thing. Especially when one of your hobbies is getting out of your skull. For the last month I’ve been staring longingly at the bottles of spirits behind the counter of the shop I buy cigarettes at. Drinking alone seems likely to lead to potential death, so I haven’t purchased any. About a year ago I bought some entirely legal plant-materials. Said plant materials are interesting because they contain significant percentages of certain chemicals, most of which are also entirely legal. This box of interestingly made-up plant-matter has been sitting around my room doing nothing for the best part of a year.

One of the little packets of plant-material that the box contained was filled with the seeds of a plant called Syrian Rue. Planted and suitably nurtured they’d have grown into pretty five-petalled flowers. That, however, was not the destiny of these particular seeds. Instead they were subjected to a fairly rough extraction process, designed to separate the interesting chemicals they contained from the dull cellulose and fibre.

The chemicals in question aren’t ones you’ll have heard of unless you’re a drugs geek. The plant’s latin name is Peganum Harmala and the chemicals it contains are named after it. Harmaline, harmine and a little tetrahydroharmine; all variations on beta-carboline. The chemistry is fascinating even from my uneducated perspective (break open the nitrogen-containing benzene-ring and lose the methyl and you end up with tryptamine, the chemical backbone of neurotransmitters like serotonin) but to go into this too much would bore you and show me up as ignorant. Besides, nobody cares what drugs are made from, only what they do. So what do these harmala alkaloids do?

Beta-carbolines are MAOIs. They inhibit the enzyme monoamine oxidase. They stop it doing what it does best, which is to replace the nitrogen atoms of molecules called monoamines with oxygen atoms. Three monoamines that it does this to: Serotonin, norepinephrine and dopamine. You may have heard of MAOIs – they’re the least-favoured class of antidepressants. Older ones can cause hypertensive crises if you eat or drink the wrong thing: Like cheese. Or wine. Or soy sauce. The newer ones are reversible and are much less likely to do this. Beta-carbolines are in this latter category.

Eating seeds is one way to get this effect from Syrian Rue, but it’s not particularly pleasant. Far better to spend a little time in the kitchen, boiling and adding salt and chilling and crystallising and evaporating until you have a few grams of sparkly orange-brown powder. I’m not going to go into the details of the process, but it’s not the kind of kitchen chemistry that ends up with explosions and hazmat teams. The worst disaster that could have occurred would have been scalding myself with hot water. A complete lack of flammability is something I value in a chemical process.

If you’re in Canada: Don’t do this. While it’s absolutely, 100% legal here in the UK, the authorities in Canada have made possessing this rather obscure drug illegal where you are.

The main value of the beta-carbolines is to potentiate other drugs. Dimethyltryptamine is the best example. If you smoke it, you trip. If you eat it, nothing happens: Monoamine oxidase strips off the nitrogen before it gets to the brain. If you take a beta-carboline ahead of time, the monoamine oxidase fails to work, the DMT reaches the brain and you see tiny space-elves hopping around. Maybe. This combination has been used traditionally in South America for centuries. And by hippies and drug-geeks for the last fifty years or so.

If you’re in most places – don’t do this. DMT is illegal pretty much everywhere.

Harmaline and Harmine are active by themselves, in ways that the synthetic MAOI’s don’t seem to be. I know this, because I’ve tried Syrian Rue before. It’s an interesting few hours. It doesn’t lead to enlightenment or deep knowledge of the universe or anything else of much value. But it’s interesting, rather than boring, which is the point really.

If I’m going to use this substance then it’s better to do it now than when I’m prescribed other drugs. MAOIs tend to have hideous interactions with other drugs, leading to the fun of hypertensive crises and serotonin syndrome. Of course, this is a false dichotomy: I don’t have to use it now or later, I can also choose not to use it at all. And really, I’m not sure if I will or not. It’s reasonably safe (though eating cheese and drinking wine at the same time would be a bad idea, I’m sure), but then again, I’m currently mad and, though I haven’t sought medical advice, it would be to not do any substances. At all. Ever. You junkie.

So my newly-extracted harmala alkaloids are currently sitting in the box of various plant-materials. (Ah, Experimental Chimp: Where drugs and mental illness mix badly…)

September 22, 2007 at 1:30 pm Leave a comment

Hi, I'm James. I'm a 26 year old guy from England with bipolar disorder (currently well controlled). I also have a circadian rhythm sleep disorder (not so well controlled). This blog has charted my journey from mental illness, through diagnosis and, recently, into recovery. It's not always easy, but then, what is?


Self-righteous note about smoking

As of 12th September 2008 it has been forty five weeks since I quit smoking. So in another seven weeks it'll have been a whole year.