Lithium Mineral Transporters (Lithium Orotate and Lithium Arginate)

Psychiatrists have been actively using lithium compounds for decades in psychiatric patients. The most common drug forms of lithium are lithium carbonate and lithium citrate, which are inorganic mineral salts. In these preparations the lithium is removed from the compound in the process of digestion and free lithium ions are absorbed into the blood stream. In order to establish a therapeutic dose of lithium salts, psychiatrists are trained to measure lithium levels in the blood serum. The monitoring of lithium levels and patient response to lithium combines both the science and art of medicine. With scientific testing, doctors try to establish therapeutic levels of lithium in the blood stream while attempting to avoid lithium toxicity, which is often manifested by a variety of symptoms such as diarrhea, excessive thirst, excessive urination and tremors.

Scientific studies have shown that there is a very narrow range between the blood level where lithium salts exert therapeutic effects and the level at which they exert toxic effects. Long-term, lithium salts can damage the kidneys and the thyroid so psychiatrists attempt to maintain the blood level of lithium within a very narrow therapeutic range to avoid both the acute and chronic side effects of lithium. Unfortunately, some individuals will exhibit symptoms of lithium toxicity even when they have very low lithium levels. Recognition of such a phenomenon entails the art of medicine and clinical experience where a good doctor learns to pay attention to the patient’s response and symptoms instead of just the lab report, which may show a therapeutic or even low blood level of lithium. Good doctors listen to the patient and not just little pieces of paper when making clinical decisions.

Lithium mineral transporters such as lithium arginate and lithium orotate are different types of lithium compounds than lithium carbonate or lithium citrate. When a lithium mineral transporter is used about 80% of the lithium is still bound to the transporter while the compound is in the blood stream. These compounds only release significant amounts of free lithium after the transporter carries the lithium into the cells. Free lithium is then released inside the cells when metabolic processes utilize the transport agent. With lithium mineral transporters, the clinical effects are not related to the actual amount of lithium in the blood, but rather by tissue delivery. So investigation of blood levels of lithium has little correlation with the effect of lithium mineral transporters.

These forms of nutritional lithium supplements have a high affinity for particular tissues and by maintaining control of lithium release till the transporter enter the tissues only a small amount of lithium is needed in order to achieve biological effects.

Lithium mineral transporters have a number of applications. Dr. Nieper found that low doses of Lithium orotate were useful as nutritional support in conditions ranging from alcoholism to migraines and seizures. Lithium mineral transporters need to be taken in low doses and are generally beneficial between one to sixr tablets per day. The lithium mineral transporters are absorbed with the lithium still attached to the carrier molecule (orotic acid in lithium orotate and arginine in lithium arginate). These mineral transporters are very stable in the blood stream and only release significant amounts of lithium once the cells take up the transporter. These mineral transporters contain much lower doses of elemental lithium than drug versions of lithium such as lithium citrate or lithium carbonate. It is important to recognize that even though these nutritional supplements contain only small amounts of elemental lithium some individuals may be very sensitive to any amount of lithium and may only need one per day. If an individual is sensitive they may develop temporary weakness, which is resolved by lowering the dose or using the product every other day. Lithium also plays an important role in the production of blood cells in the bone marrow and stimulates the production of new nerve cells in the brain.

Lithium orotate

Lithium orotate was used by Dr. Nieper in doses of one to two per day to help alcoholics reduce cravings to drink. Animal experiments have shown that small amounts of lithium orotate achieve higher brain concentrations of lithium than lithium given as the carbonate; however when lithium is given as the orotate form it stays in the body longer than lithium given as lithium carbonate, so a little lithium orotate goes a long way. Lithium orotate goes into the brain through the blood-brain barrier, since the orotic acid transporter is attracted to tissues, which use a specialized energy production pathway called the pentose pathway. Tissues that use this pathway are cartilage, blood vessels of the brain, the tissue that makes up the conduction system of the heart and brain glial cells. The orotate mineral transporters deliver minerals into the cell and release the minerals in the cell organelle membranes such as the membranes of mitochondria and especially of lysosomes. When lithium is released in the membranes of lysosomes it causes a displacement of sodium and stabilization of lysosomal membranes. This stabilization of lysosomal membranes reduces the release of aggressive enzymes, which is why Dr. Nieper used lithium orotate in autoimmune, inflammatory and viral diseases.

Lithium arginate with aspartate

Lithium arginate is a nutritional supplement of the trace element lithium combined with the mineral transporters arginine and aspartic acid.  When small amounts of lithium are given, it is not usually necessary to monitor the blood serum levels, which is necessary when administering the drug form of lithium such as lithium carbonate.  Lithium arginate, when taken as a nutritional supplement at low doses, does not trigger the harmful side effects that normally occur with high doses of lithium carbonate, acetate, or citrate.

Dr. Nieper reported that supplementation with either lithium arginate or lithium orotate, in recommended doses, does not significantly increase the lithium content of the blood so regular examinations of blood lithium levels are usually not necessary. When taken in recommended doses muscular tremors, diarrhea and disorderly effects on thyroid function seldom occur.

Comparison of the amount of lithium in different lithium compounds

Lithium carbonate and lithium citrate are inorganic salts. Lithium carbonate is the most commonly prescribed lithium compound. Lithium carbonate is a psychiatric drug that is frequently used by doctors to treat bipolar disorder and other psychiatric illnesses.

Lithium carbonate usually comes in 300mg and 450mg capsules. A common amount that might be prescribed would be 600-1200mg per day. When lithium drugs are ingested the digestive system will break off (disassociate) the mineral lithium from the lithium compound allowing the free mineral ion to enter the blood stream. 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 target cells. Because lithium carbonate and lithium citrate do not have mineral transport capability the only way to get adequate lithium into brain cells when these inorganic lithium salts are used is to have a substantial level of lithium in the blood stream. Unfortunately, lithium in high doses is relatively toxic so blood lithium monitoring is necessary when inorganic lithium salts are used to insure that the lithium levels in the blood stream are high enough to get enough lithium into the brain cells, but not so high as to create toxicity. The amount of lithium in the blood stream must be kept in a fairly narrow range called the therapeutic window, high enough to achieve a therapeutic effect and low enough to minimize toxicity.

Since these organic lithium salts (lithium arginate or lithium orotate) contain 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. In addition the cells rapidly take up these lithium transporters so that the amount that stays in the blood stream is relatively low. In fact it is difficult to get measurable blood lithium levels with lithium mineral transporters because of these factors. It is important to recognize that high doses of any lithium compound will be toxic so lithium mineral transporters only maintain their safety when low doses are utilized.

Lithium carbonate contains 18.8mg of elemental lithium per 100mg while lithium orotate contains 3.83mg of elemental lithium per 100mg and lithium arginate contains 3.58mg of elemental lithium per 100mg. The effective dose of lithium carbonate usually ranges from 600mg (113mg elemental lithium) to 1200mg (226mg elemental lithium). According to Dr. Nieper, an effective dose of lithium orotate or lithium arginate is between 2 to 6 120 mg tablets per day. One 120mg tablet of lithium orotate contains 4.6mg of elemental lithium and one 120mg tablet of lithium arginate contains 4.3mg of elemental lithium. So 2 tablets of lithium orotate contains 9.2 mg of elemental lithium 6 tablets contains 27.6 mg and 2 tablets of lithium arginate contains 8.6 mg of elemental lithium and 6 tablets contains 25.8 mg.

Interactions of lithium compounds may occur with: antithyroid pills, diuretics, medications for asthma, bronchitis, cystic fibrosis, emphysema, or sinusitis.

No lithium compounds are habit-forming. Long-term use of any lithium compound however may cause thyroid and kidney problems. It is wise that any individual who uses any lithium compound for prolonged periods have renal and thyroid functions monitored ever six months. Renal and thyroid problems are less likely to occur when low amounts of lithium are ingested so mineral transporters may have some advantage in this area.

It is important not to take any type of lithium drug or lithium supplement during pregnancy since lithium may increase risk of birth defects!


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