PharmaceuticalHypnoticMelatonin receptor agonistNon-scheduled

Ramelteon

Also known as Rozerem · TAK-375

Written by enwyReviewed 5 Aug 20262 sources0 comments

Selective MT1/MT2 melatonin receptor agonist approved for sleep-onset insomnia. Non-scheduled and non-habit-forming with no meaningful abuse potential, but the hypnotic effect is modest and it does little for sleep maintenance.

01 Overview

Ramelteon (brand Rozerem) is a synthetic melatonin receptor agonist approved by the FDA in 2005 for insomnia characterised by difficulty with sleep onset. Unlike Z-drugs and benzodiazepines it does not act on GABA-A receptors, and it is the only prescription hypnotic in the US that is not a controlled substance.

In trials it modestly reduces latency to persistent sleep without producing dependence, rebound insomnia, or next-day psychomotor impairment at approved doses. Effect size is small and it has little impact on sleep maintenance or total sleep time. It is extensively metabolised by CYP1A2 and is contraindicated with the strong CYP1A2 inhibitor fluvoxamine.

02 Mechanism

High-affinity selective agonist at MT1 and MT2 melatonin receptors in the suprachiasmatic nucleus, promoting sleep onset without GABAergic sedation.

03 Dosing

Tier	Dose	Route	Notes
Approved dose	8 mg/day	Oral	Single 8 mg tablet within 30 min of bedtime; do not take with or after a high-fat meal.

04 Effects

Effect	Magnitude	Evidence
Reduced sleep onset latencyConsistent modest improvement in time to fall asleep across trials.	~9-16 min faster to persistent sleep	Clinical
No dependence or abuse liabilityNo reinforcement, tolerance, or withdrawal observed; safe for long-term nightly use.		Clinical

05 Side effects

Effect	Severity	Frequency	Evidence
Daytime somnolence / fatigueResidual drowsiness, dizziness, or fatigue reported in a minority of users.	Mild	Common	Clinical
Endocrine changes (prolactin/testosterone)Mild increases in prolactin and decreases in testosterone seen in some subjects; rarely symptomatic.	Mild	Uncommon	Clinical
Elevated levels with CYP1A2 inhibitorsFluvoxamine raises ramelteon exposure many-fold, greatly increasing sedation.	Moderate	Interaction-dependent	Clinical

06 Legal status

Marketed for insomnia. · as of Jan 2026

United States

Rx, non-controlled

FDA-approved 2005; not scheduled by the DEA. · as of Jan 2026

07 References

Efficacy and safety of ramelteon in adults with chronic insomniaSleep Medicine, 2006

Rozerem (ramelteon) FDA prescribing informationUS FDA

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.