Ramelton essentially mimics melatonin’s sleep-promoting properties and has high affinity for melatonin MT¹ and MT² receptors in the brain. These receptors are believed to be critical in the regulation of the body’s sleep–wake cycle.

Ramelton is rapidly absorbed and eliminated over a dose range of 4 to 64 mg. Maximum plasma concentration (C_max) is reached approximately 45 minutes after administration, and the elimination half-life is 1 to 2.6 hours. The total absorption of ramelton is at least 84%, but extensive first-pass metabolism results in a bioavailability of approximately 2%. Ramelton is primarily metabolized via the CYP 1A2 pathway and principally eliminated in urine. Repeated once-daily dosing does not appear to result in accumulation, likely because of the compound’s short half-life.

Ramelton was approved by the FDA for the treatment of insomnia characterized by difficulty with sleep onset. Potential off-label usage is centered on use in circadian rhythm disorders, predominantly jet lag, delayed sleep phase syndrome, and shift work sleep disorder.

Clinical trials and animal studies failed to find evidence of rebound insomnia of withdrawal effects.