Ramelteon
ROZEREM
What it isMT1 and MT2 melatonin-receptor agonist; sleep-onset insomnia.
Why this oneIt is unscheduled and has no meaningful abuse or withdrawal liability, unlike benzodiazepine-site hypnotics.
What limits itEffect on sleep onset is modest. Strong CYP1A2 inhibition, especially fluvoxamine, can raise exposure markedly.
FDA-approved for
- insomnia (2005)
Off-label
- delirium prevention (limited evidence)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Insomnia (sleep-onset) | Adults | 8 mg QHS | 8 mg QHS | 8 mg/day |
Renal No adjustment needed
Hepatic Caution in moderate impairment; not recommended in severe
Instructions
- Take within 30 min of bedtime
- Do not take with or immediately after a high-fat meal
- Do not use with fluvoxamine; caution with other CYP1A2 inhibitors
- Reevaluate if insomnia persists after 7-10 days
Contraindications
- History of angioedema with prior ramelteon; do not rechallenge
Cautions
- Angioedema/anaphylaxis (do not rechallenge)
- Abnormal thinking, complex sleep behaviors (sleep-driving, hallucinations)
- Worsening depression / suicidal ideation
- CNS impairment (driving, machinery)
- Decreased testosterone, increased prolactin
- Not recommended in severe sleep apnea
Adverse reactions
- Somnolence
- Dizziness
- Fatigue
- Nausea
- Exacerbated insomnia
Pregnancy No drug-associated risk identified in postmarketing data; teratogenic in rats at high multiples
Lactation Undefined
NO BOXED WARNINGS
Principal riskModest effect; contraindicated with fluvoxamine
Cost, est. cash$5–$150/month
Generic entry2013
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySomnolence and dizziness; overdose is generally less dangerous than sedative-hypnotics.
Mechanism of action: Ramelteon ballicule
Open Ramelteon in the interactive console ↗
Memory aids: mascots and interaction avatars
