[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Other hypnotics (melatonin agonists and orexin antagonists)](https://durgical.com/en/pharmacology/classes/other-hypnotics/) › Ramelteon

[Pharmacology](https://durgical.com/en/pharmacology/) · [Other hypnotics (melatonin agonists and orexin antagonists)](https://durgical.com/en/pharmacology/classes/other-hypnotics/)

# Ramelteon

A melatonin receptor agonist for trouble falling asleep. It does not act on GABA, is not a controlled substance and shows no abuse potential.

Updated 2026-11-01

- Class: [Other hypnotics (melatonin agonists and orexin antagonists)](https://durgical.com/en/pharmacology/classes/other-hypnotics/)
- Receptor: Melatonin receptor MT1
- ATC code: N05CH02

◎**Melatonin receptor MT1**Ramelteon

ⓘ The figure shows ramelteon itself bound to the human MT1 melatonin receptor.

**Target in 3D:** Melatonin receptor MT1. PDB structure 6ME2 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6ME2) · Drag to rotate · pinch to zoom

## Mechanism of action

Ramelteon binds MT1 and MT2 melatonin receptors with high affinity and stimulates them, imitating the night signal of melatonin in the brain's clock. It has no appreciable affinity for the GABA receptor complex.

- Binds MT1 and MT2 melatonin receptors
- Imitates melatonin's night signal
- Sleep onset comes sooner

## Pharmacokinetics

**Absorption**
Not taken with or right after a high-fat meal

**Metabolism**
Mainly by CYP1A2, with minor CYP2C and CYP3A4

**Half-life**
About 1 to 2.6 hours

## Indications

- Insomnia with difficulty falling asleep [Insomnia disorder →](https://durgical.com/en/conditions/insomnia-disorder/)

## Adverse effects

### Common

- Drowsiness and tiredness
- Dizziness
- Nausea and worsened insomnia

### Serious (rare, important)

- Angioedema and other allergic reactions
- Complex sleep behaviours such as sleep-driving
- Lower testosterone and higher prolactin

## Contraindications

- Previous angioedema with ramelteon
- Use with fluvoxamine

## Key interactions

**Fluvoxamine (strong CYP1A2 inhibitor)**
Much higher ramelteon levels: contraindicated

**Alcohol**
Added sedation

## What is monitored

- Sleep onset
- Unexplained missed periods, milk discharge, low libido or fertility problems: prolactin and testosterone may be checked

## Administration and safety

- Given by mouth shortly before bed
- Not with or right after a high-fat meal

## Nursing care

- Check how the person slept, next-morning alertness and falls
- Ask about alcohol and other sedatives
- Teach to take it only when a full night in bed is possible and not to drive the next morning if drowsy
- Teach to report sleepwalking, sleep-driving or other actions done while not fully awake

## Pregnancy and breastfeeding

Post-marketing reports have not shown a clear risk of major birth defects; animal studies showed harm at high exposures.

## Memory aid

Ramelteon: «RAM the MElaTonin receptor» – MT1/MT2 agonist, no GABA, no abuse; never with fluvoxamine.

## Test yourself

Think of the answer, then tap the question to see it.

## Is ramelteon a controlled substance?

No; it shows no abuse potential or physical dependence.

## Which enzyme mainly breaks down ramelteon?

CYP1A2, which is why fluvoxamine is contraindicated.

## Which hormonal changes are linked to ramelteon?

Lower testosterone and higher prolactin.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/ramelteon/)

## Related drugs

- [Melatonin](https://durgical.com/en/pharmacology/melatonin/)
- [Suvorexant](https://durgical.com/en/pharmacology/suvorexant/)

## Related conditions

- [Insomnia disorder](https://durgical.com/en/conditions/insomnia-disorder/)

[← Back to the class: Other hypnotics (melatonin agonists and orexin antagonists)](https://durgical.com/en/pharmacology/classes/other-hypnotics/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - RAMELTEON tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5c1ba52a-8e7a-844a-6c48-d1c9bf9fff0e) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N05CH02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [6ME2: XFEL crystal structure of human melatonin receptor MT1 in complex with ramelteon](https://www.rcsb.org/structure/6ME2) (RCSB Protein Data Bank, 2019).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/ramelteon/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/ramelteon/