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In humans, 90% of orally administered exogenous melatonin is cleared in a single passage through the liver, a small amount is excreted in urine, and a small amount is found in saliva. [13] Melatonin is excreted in the urine 2 to 5% as the unchanged drug. [6] [8] Melatonin has an elimination half-life of about 20 to 60 minutes.
The popular sleep aid can have side effects.
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In humans, ~30 μg of melatonin is produced daily and 80% of the total amount is produced in the night (W). The plasma maximum concentration of melatonin at night are 80–120 pg/mL and the concentrations during the day are between 10–20 pg/mL. [76] [77]
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Consuming caffeine to stay awake at night may lead to sleeplessness, anxiety, frequent nighttime awakenings, and overall poorer sleep quality. [139] The main metabolite of melatonin (6-sulfatoxymelatonin) gets reduced with consumption of caffeine in the day, which is one of the mechanisms by which sleep is interrupted. [137]
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Large doses of melatonin can even be counterproductive: Lewy et al. [48] provide support to "the idea that too much melatonin may spill over onto the wrong zone of the melatonin phase-response curve." The long-term effects of melatonin administration have not been examined. In some countries, the hormone is available only by prescription or not ...