Lithium as a mood stabilizer has been used as the standard pharmacological treatment for
Bipolar Disorder (BD) for more than 60 years. Recent studies have also shown that it has the potential
for the treatment of many other neurodegenerative disorders, including Alzheimer’s, Parkinson’s and
Huntington’s disease, through its neurotrophic, neuroprotective, antioxidant and anti-inflammatory actions.
Therefore, exploring its pharmacokinetic features and designing better lithium preparations are
becoming important research topics. We reviewed many studies on the pharmacokinetics, drug design
and toxicity of lithium based on recent relevant research from PubMed, Web of Science, Elsevier and
Springer databases. Keywords used for searching references were lithium, pharmacology, pharmacokinetics,
drug design and toxicity. Lithium is rapidly and completely absorbed from the gastrointestinal
tract after oral administration. Its level is initially highest in serum and then is evidently redistributed
to various tissue compartments. It is not metabolized and over 95% of lithium is excreted unchanged
through the kidney, but different lithium preparations may have different pharmacokinetic
features. Lithium has a narrow therapeutic window limited by various adverse effects, but some novel
drugs of lithium may overcome these problems. Various formulations of lithium have the potential for
treating neurodegenerative brain diseases but further study on their pharmacokinetics will be required
in order to determine the optimal formulation, dosage and route of administration.