Ramelteon

Category: sleep

Aliases: Rozerem

Pharmacological Mechanism

Selective MT1 + MT2 melatonin-receptor agonist with ~16× greater MT1 affinity than melatonin. No GABAergic activity → no dependence potential, no scheduling. Modest efficacy on sleep-onset latency (~10 min improvement). CYP1A2 substrate — fluvoxamine contraindicated (>200× AUC rise).

Half-Life (t½)

PO: 1.5h

Dosing Guidelines

• PO: Typical 8 mg (Range: 8–8 mg)

Target Organ Systems

• endocrine
• digestive

Pathways It Modulates

• Circadian clock (activator) — MT1 / MT2 selective agonist
• Orexin / wakefulness arousal axis (activator) — MT1 + MT2 (melatonin agonist)
• Tryptophan → serotonin → melatonin (activator) — MT1 + MT2

Chemical Identifiers

• PubChem CID: 208902
• Formula: C16H21NO2
• Molecular weight: 259.34 g/mol
• InChIKey: YLXDSYKOBKBWJQ-LBPRGKRZSA-N
• SMILES: CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3

References

• PMID 16432265
• PMID 15695169