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ramelteon

Melatonin Congener · Hypnotic

Melatonin CongenerHypnotic
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AlfentanilSevereDatabaseDDInter
  • BenzhydrocodoneSevereDatabaseDDInter
  • BuprenorphineSevereDatabaseDDInter
  • ButorphanolSevereDatabaseDDInter

Mechanism

Ramelteon is a synthetic tricyclic analogue of melatonin. It binds to both MT1 and MT2 receptors with high affinity. Binding to MT1 receptors promotes the onset of sleep; binding to MT2 receptors shifts the timing of the circadian system.

Indications

Insomnia (specifically difficulties of sleep onset)Transient and chronic insomniasleep onset insomnia

Dosing

Adult
An 8-mg tablet be taken about 30 min before bedtime

Pharmacokinetics

Half-life
about 2 h
Bioavailability
less than 2% (significant first-pass metabolism)
Protein binding
82%
Metabolism
largely metabolized by hepatic CYPs 1A2, 2C, and 3A4
Excretion
<0.1%

Side effects

Common
DizzinessNauseaDrowsinessHeadache
Serious
  • does not produce usual BZD-like side effects
  • free of rebound phenomena on stoppage
  • no dependence producing potential noted so far

Drug interactions

Alfentanil
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Benzhydrocodone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Buprenorphine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Butorphanol
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Codeine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Dextropropoxyphene
Severe
Database

Clinical effect not specified

Source: DDInter

Dezocine
Severe
Database

Clinical effect not specified

Source: DDInter

Dihydrocodeine
Severe
Database

Clinical effect not specified

Source: DDInter

Fentanyl
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Fluvoxamine
Severe
Database

ramelteon AUC increased 189.9-fold.

coadministration generally contraindicate[d] or at least require[s] dosage adjustment.

Source: DDInter

Hydrocodone
Severe
Database

.

Source: DDInter

Hydromorphone
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Melatonin Congener drugs

Ask House about ramelteon

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team