Lithium

Lithium is a classic drug that is still used today as the first-choice remedy for mania and as a preventive therapy for bipolar-effective disorders (mania depression). Lithium is available as: Lithium aspartate (lithium aspartate), Quilonum (lithium acetate), Hypnorex ret, Quilonum ret. Lithium Apogepha, Leukominerase (Lithium Carbonate), Lithium Aspartate, Lithium Acetate, Lithium Carbonate, Lithium.

Fields of application

• Mania
• Bipolar-affective disorders (manic-depressive disorders)
• Preventive therapy for (unipolar) depression
• Preventive therapy for schizoaffective disorders (but no official approval)

Dosage form

Lithium is taken in the form of tablets or film tablets. After taking the tablet, it dissolves in the gastrointestinal tract and the lithium is released. The free lithium ions can now be absorbed into the cells of the intestinal mucosa.

Since lithium has a chemical structure very similar to that of sodium, which is present everywhere in the body, it enters the cell via the same transporters. While the absorption is very successful, the cells have more difficulties to release the lithium back into the bloodstream. For this reason, excessive doses can lead to the accumulation of too much lithium in the body and to symptoms of poisoning.

For this reason, it is important to stick to the prescribed quantities when taking the product. It is also essential during treatment to check the lithium level in the blood regularly so that the dose can be adjusted and an overdose cannot occur. Lithium is an active substance that enters the bloodstream of the unborn child uninhibited in pregnant women.

This is the reason why in the 1960s taking lithium during pregnancy was considered contraindicated. Over time, however, studies have shown that absolute abstinence is not necessary. Today it is recommended to reduce the dose and take smaller amounts several times a day instead of the full daily dose in the evening.

Furthermore, the pregnant woman should abstain from a low-salt diet in order to prevent an accumulation of lithium in the body. In the week before the birth the dose should be further reduced to temporarily stop taking the drug completely when the contractions start. This is because the woman’s water balance changes during childbirth, which can lead to an increase in lithium in the blood – with the above-mentioned consequences.

If the lithium therapy is to be discontinued, it is absolutely essential that the dose is slowly phased out, otherwise symptoms such as anxiety, inner restlessness or a manic phase may occur. Lithium is a very old drug and its psychological effects were first described in 1949. Lithium is always contained in the tablets as a salt in combination with another substance.

This is carbonate (in Hypnorex® from Sanofi, Lithium Apogepha® and Quilonum® retard from GlaxoSmithKline), sulfate (in Lithiofor® from Vitor Pharma) or aspartate (in Lithium-Aspartat from Köhler-Pharma). Lithium has a variety of effects on the central nervous system. To date, it has not yet been fully clarified which of the subsequent effects is ultimately responsible for its effectiveness, especially in manic-depressive illness:

• Inactivation of ion channels: In the same way that anticonvulsants (drugs against epilepsy) interfere with the cellular sodium–potassium current, lithium probably reduces the central excitability of the brain.
• Effect on second-messenger systems: All functions of life take place on the smallest cell level.

  Enzymes and proteins are among the most important executive instruments. Lithium intervenes in such enzyme chains. (inhibition of inositol monophosphatase) it leads to a decrease of certain enzyme products and their secondary products (inositol or phosphatidylinositol).

  The inhibition of these (and other) products ultimately leads to a decrease in the calcium concentration in the cells in further intricate ways. This is exactly what we want, since the so-called intracellular calcium concentration is typically elevated in manic-depressive illness. Phew… is complicated, isn’t it?

• Release of GABA: GABA is a messenger substance in the brain which, like other messenger substances, is directly related to mood. Lithium ensures an increased release of GABA
• Serotonin level Increase: Lithium leads to an increased release of the “mood transmitter” serotonin and simultaneously inhibits its breakdown.