Clinical pharmacokinetics of melatonin: a systematic review

Abstract

Despite methodological differences between the included studies, Tmax was approximately 50 min following oral immediate-release formulations of melatonin. T1/2 was 45 min in both administration routes. Cmax, AUC, Cl, and VD varied extensively between studies. Bioavailability of oral melatonin was approximately 15%.

Melatonin inhibits TPA-induced oral cancer cell migration by suppressing matrix metalloproteinase-9 activation through the histone acetylation

“…It is achievable for 20 mM melatonin clinically [58]. Moreover, a systematic review article also concluded that time to maximal plasma/serum concentration (Tmax) was approximately 50 min following oral immediate-release formulations of melatonin and the bioavailability of oral melatonin was approximately 15% [59]. Thus, the experimental concentrations of Melatonin used in this study (0–1 mM) could become clinically achievable.…”

Melatonin for the management of sleep problems in children with neurodevelopmental disorders: a systematic review and meta-analysis

“…Some authors believed that there could be a carry-on effect of melatonin on sleep parameters and circadian rhythm 15 28 30. A recent systematic review on the pharmacokinetics of melatonin showed that the maximum concentration of melatonin after supplementation would be reached after approximately 50 min with oral immediate-release formulations 30. The elimination half-life of both oral and intravenous melatonin was about 45 min.…”

A novel LC–MS/MS assay for the simultaneous determination of melatonin and its two major metabolites, 6-hydroxymelatonin and 6-sulfatoxymelatonin in dog plasma: Application to a pharmacokinetic study

“…The dogs adopted by Wang et al [25] were younger and lighter. It has been known that the clinical pharmacokinetics of exogenous MEL was affected by age [17]; therefore, we speculated that the difference in the dog pharmacokinetics of MEL might be caused by the same reason.…”

“…The pharmacokinetics of exogenous MEL in rat, dog and human have been investigated [13][14][15][16][17]. Nevertheless, there is little information about the pharmacokinetics of its major metabolites 6-O-MEL and S-O-MEL, which is partly due to lack of convenient analysis methods for simultaneous quantification of MEL and its metabolites in bio-matrices.…”