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Re: Larry what do you think about lithium orotate? » Ron Hill

Posted by Larry Hoover on June 2, 2003, at 8:51:48

In reply to Re: Larry what do you think about lithium orotate?, posted by Ron Hill on June 1, 2003, at 23:37:58

> Larry,
> If the sales pitch is true and the lithium orotate does indeed cross the cell membrane more readily than the inorganic Li ion, then an equivalent pharmacological effect might be accomplished with reduced Li blood levels. This in turn would reduce the side effects including possible thyroid damage from long-term use of lithium.

I think that claims such as that require some evidence. I can't find any.

The best theory I've yet seen is that lithium ions interfere with calcium-dependent gene regulation within the cell, effectively down-regulating a number of processes. Yes, that happens inside the cell, but there is so much ion movement in and out of the cell, lithium doesn't just stay there.

> Since I am self-insured, the cost of prescription lithium carbonate is comparable to the cost of the lithium orotate supplement product.

If you want to give it a try, I'd consider it to be an experimental treatment. Lithium orotate was considered for use about 25 years ago, and it was dropped from consideration, for whatever reason.

> Larry, I highly value your opinion and I have learned much from your writings (we are fortunate to have you here). If you have time, could you please read this link and give me your opinion?

Thanks, Ron. My pleasure.

> Specifically, does Li orotate enter the cells more efficiently than inorganic Li, thereby, facilitating a marked reduction in the dosage required when using the Li orotate product?

Not that I can find evidence for.

> Also, although the web page does not specifically say this, I get the impression that the lithium orotate crosses the cell membrane prior to dissociation (i.e.; the Li ion is still bound to the transporter molecule).

That's what they want you to believe.

>If this is true, when and where does the Li ion break free from the transporter molecule so that the Li ion can start doing whatever it does as a moodstabilizer?

Good question. Does the molecule magically know when it has arrived at its destination? I don't know. There are orotic acid transporters, as orotic acid is a precursor to RNA, but why that would be better than the pre-existing Na+/Li+ transporter is beyond me.

> And finally, Lithobid is a slow-release product. I doubt that the lithium orotate product has a slow-release feature.

They're suggesting it's inherent, I think.

> Here's the link.
>
> http://www.findserenitynow.com/product_info_4.html
>
> Thank you sooooooooo much.
>
> -- Ron
>

Like I said, my pleasure. I like questions, and ones like this one, even more than many others.

I looked at the web-link before I went to Pubmed, etc., and my gut-reaction was a bullshit-detector activation. Here are my thoughts, relevant to quotes from the site.

"Lithium carbonate and lithium citrate are both inorganic salts."

Pardon me? Organic means carbon-based. We have carbonate (CO3--), and citrate (C6H5O7---). Nothing inorganic about those ions.

"Lithium carbonate usually comes in 300mg and 450mg capsules. A common amount that might be prescribed would be 600-1200mg per day. Once ingested; the digestive system will break off the mineral lithium from the lithium compound, allowing the free mineral ion to enter the blood stream."

It doesn't break the lithium off, it dissolves it. Why the semantic twisting? Moreover, we know that lithium readily enters the blood from the gut, so what's the issue?

"In order to have a physiological effect, the lithium mineral ion will have to pass from the blood stream through cell membranes in order to enter the necessary cells."

No shit! They use the Na+/Li+ transporter.

"Lithium carbonate and lithium citrate do not have mineral transport capability..."

At this point, the lithium salts have ceased to exist, so this is a distraction or deception.

"Inorganic lithium compounds are used to insure that the lithium levels in the blood stream are high enough so that enough lithium enters the brain cells to be effective. Unfortunately, lithium in high doses is relatively toxic and blood lithium monitoring is necessary when these inorganic lithium salts are used."

Lithium flux goes both ways. Even if the lithium orotate efficiently transports lithium into neurons, and dissociates in a timely manner, the lithium will then both leak out, and be pumped out. The "high blood concentrations" mentioned are a necessary component of ionic equilibrium. Uptake has to equal release (from a whole cell vs. blood concentration perspective, across the cell membrane) at some point in time, and if there's none in the blood, there will soon be none in the neuron.

"Dr. Nieper developed the organic lithium salt in Serenity."

Ohh? And Dole invented the Internet.

"Serenity has mineral transport capability. Dr. Nieper developed the organic lithium salt in Serenity - which is a lithium mineral transporter. This means that the organic lithium salt in Serenity remains intact through the digestive system so that the entire compound enters the blood stream with most of the lithium still bound to the transporter molecule. Since the mineral transporter in Serenity enables the entire compound to enter the blood stream - the amount of Lithium used can be drastically reduced."

So, how does the orotic acid preferentially target brain neurons? Little maps? Kidney and liver have very high affinities (uptake capacity) for orotic acid. Moreover, calling orotic acid a lithium mineral transporter is deceptive. If it is a mineral transporter, it's not specific to lithium.

"In fact: the organic lithium in Serenity contains about 5 times less elemental lithium per 100mg than lithium carbonate. The amount of lithium that enters the blood stream is significantly lower when lithium mineral transporters are used."

...because you take less in.

"In addition our human cells rapidly absorb the lithium transporters in Serenity, so that the amount that stays in the blood stream is relatively low."

As I said, but most are not in the brain.

"In fact: because of these factors: It is difficult to obtain measurable lithium levels in the blood with the lithium mineral transporter in Serenity."

Equilibrium lies to which side? Brain loses this one.

"It is important to recognize that high doses of any lithium compound will be toxic -- so the lithium mineral transporter in Serenity provides a safety from this toxicity as only low doses of lithium are used."

Proof of efficacy?

"Lithium carbonate contains 18.8mg of elemental lithium per 100mg. With the mineral transporter, it is only necessary for Serenity to contain 3.83mg of elemental lithium per 100mg."

What a distorted way to present the mass ratios of the two salts.

"The effective dose of lithium carbonate usually ranges from 600mg (113mg elemental lithium) to 1200mg (226mg elemental lithium). Dr. Nieper reports: an effective dose of Serenity is between 2-6 120 mg tablets per day. One 120mg tablet of Serenity contains 4.6mg of elemental lithium.

2 tablets of Serenity contains 9.2 mg of elemental lithium.
6 tablets contain 27.6 mg."

Nothing in the literature to suggest those are effective doses for lithium orotate.

"Interactions of the inorganic lithium compounds, lithium carbonate & citrate, may occur with: antithyroid pills, diuretics. medications for asthma, bronchitis, cystic fibrosis, emphysema, or sinusitis. Serenity helps to avoid these interactions by keeping the lithium levels in the body very low."

Proof it doesn't work?

"No lithium compounds are habit-forming, however, long-term use of inorganic lithium carbonate and lithium citrate may cause thyroid and kidney problems. Again -- Serenity strongly helps to avoid these problems by keeping the lithium levels low."

Maybe rats aren't representative mammals, but maybe they are.

J Pharm Pharmacol 1979 Mar;31(3):161-3

Kidney function and lithium concentrations of rats given an injection of lithium orotate or lithium carbonate.

Smith DF, Schou M.

A recent study by Kling et al (1978) noted the finding of higher lithium concentrations in serum and brain of rats after an intraperitoneal injection (2 mmol lithium kg-1) of lithium orotate as a slurry than of lithium carbonate in solution. The authors suggested that lithium orotate might offer advantages in the treatment of patients. We repeated the experiments of Kling et al but in addition examined the kidney function of the rats. Glomerular filtration rate and urine flow were markedly lower in rats given lithium orotate than in rats given lithium carbonate, sodium chloride or a sham injection. The renal lithium clearance was significantly lower, the kidney weight and the lithium concentrations in serum, kidney and heart significantly higher after injection of lithium orotate than after injection of lithium carbonate. The higher lithium concentrations could be accounted for by the lower kidney function. It seems inadvisable to use lithium orotate for the treatment of patients.

"It is important not to take any type of lithium (organic or inorganic) during pregnancy as lithium can be counterproductive during these 9 months."

Evidence? Huh?

Ron, I'm biased. Read between my words. I don't like my gut reaction. Are my arguments rational?

Lar

 

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poster:Larry Hoover thread:230335
URL: http://www.dr-bob.org/babble/20030530/msgs/230745.html