Classifications: melatonin agonist; psychotropic agent; sedative-hypnotic; Therapeutic: sedative-hypnotic
Pregnancy Category: C
8 mg tablets
Ramelteon is a melatonin receptor agonist with high affinity for melatonin MT1 and MT2 receptors and selectivity affinity for the MT3 receptor in the brain. The activity of ramelteon at MT1 and MT2 receptors is believed to promote sleep, as these receptors, in response to endogenous melatonin, are thought to be involved
in maintaining the circadian rhythm underlying the normal sleep-wake cycle.
Effective in promoting onset of sleep.
Treatment of insomnia characterized by difficulty with sleep onset.
Hypersensitivity to ramelteon; severe hepatic function impairment (Child-Pugh C class); severe sleep apnea or severe COPD;
concurrent use of alcohol, sedative, or CNS depressant drugs; concurrent use of fluvoxamine; severe depression; suicidal
ideation; pregnancy (category C); lactation.
Moderate hepatic function impairment (Child-Pugh b class); depression with suicidal tendencies; elderly.
Route & Dosage
Adult: PO 8 mg within 30 min of h.s.
- Give within 30 min of bedtime.
- Do not administer to anyone on concurrent fluvoxamine therapy without alerting physician. This combination causes a dramatic
increase in ramelteon blood level.
- Store at 15°30° C (59° 86° F).
Adverse Effects (≥1%)CNS: Depression
, dizziness, fatigue
, headache, insomnia
, somnolence. GI: Diarrhea
, unpleasant taste, nausea. Musculoskeletal: Arthralgia
, myalgia. Respiratory:
Upper respiratory tract infection
Concurrent use with ethanol
produces additive CNS
depressant effects; ketoconazole, itraconazole,
increase ramelteon levels; other CYP1A2 inhibitors (e.g., ciprofloxacin, enoxacin, mexiletine, norfloxacin, tacrine
) may also increase ramelteon levels; rifampin
decreases ramelteon levels. Food:
High fat meal, grapefruit
or grapefruit juice
increase ramelteon level.
45 min. Distribution:
82% protein bound. Metabolism:
Rapid and extensive first pass hepatic metabolism
; one metabolite
, M-II, is active. Elimination:
Assessment & Drug Effects
- Monitor for and report worsening insomnia and cognitive or behavioral changes.
- Monitor for S&S of decreased testosterone levels (e.g., loss of libido) or increased prolactin levels (galactorrhea).
- Lab test: Baseline LFTs.
Patient & Family Education
- Follow directions for taking the drug (see Administration).
- Do not take with or immediately after a high fat meal.
- Do not drive or engage in potentially hazardous activities until response to drug is known.
- Do not consume alcohol while taking this drug.
- Report any of the following to physician: worsening insomnia, cognitive or behavioral changes, problem with reproductive