How does Circadin® work compared to other melatonin formulations?

Circadin.com December 8, 2014
Circadin® is a prolonged-release formulation of melatonin, which circumvents the fast clearance of the hormone by releasing the melatonin over an extended period of time12, thereby mimicking physiological patterns of melatonin secretion. Administration of exogenous melatonin does not affect the endogenous secretion of melatonin14. Other melatonin formulations are immediate-release – meaning that they are rapidly absorbed and metabolised with an elimination half-life of ~60 minutes15. Following oral administration of immediate-release melatonin, peak plasma levels that are 5-10 fold higher than those of Circadin®, are reached after ~50 minutes15, rapidly falling off again due to the first-pass hepatic metabolism. Immediate-release melatonin is quickly cleared from the circulation. The differences in the effects of fast vs slow release formulations is best exemplified by their effects on the blood pressure rhythm. Whereas Circadin improves blood pressure control in nocturnal hypertension fast release formulations are not efficacious16. Despite common beliefs, the effect of Circadin® on sleep latency is no less than that of fast release melatonin because the brain is very sensitive to low doses of melatonin in the beginning of the night17 11.
In a study that was performed in the UK in order to assess the efficacy and safety of melatonin in treating patients with REM sleep behaviour disorder it was found out that Circadin® is more effective than standard melatonin preparations (Freeman A, Muza R, Leschziner G, et al. Sustained Release and Standard Preparation Melatonin for the Treatment of REM Sleep Behavioural Disorder. Sleep 2011; 34: A197-A198).

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