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Pharmacokinetics of Melatonin: The Missing Link in Clinical Efficacy?


Despite widespread clinical application of melatonin, several unanswered questions remain regarding the pharmacokinetics of this drug. This lack of knowledge may contribute to the inconsistency of results in previous clinical studies. Currently, a t max value of 30–45 min and a t ½elimination of 45 min are well established. Several questions relate to what constitutes a clinically effective plasma concentration, the choice of ideal administration route, and the optimal method of analysis. Furthermore, investigations of melatonin metabolites in humans are urgently needed in order to characterize their biological functions and the metabolic fates of these derivatives. Finally, pharmacokinetics in patients should be investigated further in order to reduce the risk of potential adverse effects, such as daytime sleepiness or unintended sedation.

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Corresponding author

Correspondence to Lars Peter Holst Andersen.

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No external funding was used in the preparation of this manuscript.

Conflicts of interest

Lars P. H. Andersen, Ismail Gögenur, Jacob Rosenberg and Russel J. Reiter declare that they have no conflicts of interest that might be relevant to the contents of this article.

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Andersen, L.P.H., Gögenur, I., Rosenberg, J. et al. Pharmacokinetics of Melatonin: The Missing Link in Clinical Efficacy?. Clin Pharmacokinet 55, 1027–1030 (2016).

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