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Pharmacologic class: Melatonin receptor agonist

Therapeutic class: Hypnotic

Pregnancy risk category C


Promotes sleep through activity at melatonin MT1 and MT2 receptors, which are thought to be involved in maintaining circadian rhythm underlying normal sleep-wake cycle


Tablets: 8 mg

Indications and dosages

Insomnia marked by difficulty with sleep onset

Adults: 8 mg P.O. within 30 minutes of going to bed


• Hypersensitivity to drug or its components


Use cautiously in:

• sleep apnea, chronic obstructive pulmonary disease, hepatic impairment

• concurrent use of fluvoxamine

• pregnant or breastfeeding patients

• children (safety and efficacy not established).


• Give within 30 minutes of patient's bedtime.

• Don't give with or immediately after a high-fat meal.

Adverse reactions

CNS: headache, somnolence, fatigue, dizziness, exacerbated insomnia, depression

GI: nausea, diarrhea

Musculoskeletal: myalgia, arthralgia

Respiratory: upper respiratory tract infection

Other: altered taste, influenza


Drug-drug. Fluconazole, fluvoxamine, ketoconazole: increased ramelteon blood level

Rifampin: decreased ramelteon efficacy

Drug-diagnostic tests. Blood cortisol: decreased

Drug-food. High-fat meals: altered ramelteon absorption

Drug-herbs. American elder, bishop's weed, cat's claw, devil's claw, eucalyptus, feverfew, ginkgo, kava, licorice, pomegranate: increased ramelteon blood level

Valerian: additive sedation, increased ramelteon blood level

Drug-behaviors. Alcohol use: additive psychomotor impairment

Patient monitoring

• Monitor prolactin and testosterone levels, if ordered, in patient who develops unexplained amenorrhea, galactorrhea, decreased libido, or fertility problems.

• Evaluate patient for physical and psychiatric disorders before and during therapy. Worsening of insomnia or onset of new behavioral or cognitive symptoms could signal underlying psychiatric disorder.

Patient teaching

• Instruct patient to take drug within 30 minutes of going to bed.

• Advise patient not to take drug with or immediately after a high-fat meal.

• Caution patient to avoid driving and other hazardous activities until drug effects are known.

• Advise patient to contact prescriber if insomnia worsens.

• Instruct patient to report menses cessation, excessive or spontaneous lactation, decreased libido, or fertility problems.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, tests, food, herbs, and behaviors mentioned above.


(ra-mel-tee-on) ,


(trade name)


Therapeutic: sedative hypnotics
Pharmacologic: melatonin receptor agonists
Pregnancy Category: C


Treatment of insomnia characterized by difficult sleep onset.


Activates melatonin receptors, which promotes maintenance of circadian rhythm, a part of the sleep-wake cycle.

Therapeutic effects

Easier onset of sleep.


Absorption: Well absorbed (84%), but bioavailability is low (1.8%) due to extensive first pass liver metabolism. Absorption ↑ by a high fat meal.
Distribution: Widely distributed to body tissues.
Metabolism and Excretion: Extensively metabolized by the liver; mainly by CYP1A2 enzyme system. Metabolites are excreted mostly in urine (88%); 4% excreted in feces.
Half-life: 1–2.6 hr.

Time/action profile (blood levels)

POrapid30–90 minunknown


Contraindicated in: Hypersensitivity;History of angioedema with previous use;Severe hepatic impairment;Concurrent use of fluvoxamine; Lactation: Lactation; Pediatric: Safety not established.
Use Cautiously in: Depression or history of suicidal ideation;Moderate hepatic impairment;Concurrent use of CYP3A4 inhibitors, such as ketoconazole;Concurrent use of CYP2C9 inhibitors, such as fluconazole; Obstetric: Use only if maternal benefit outweighs fetal risk.

Adverse Reactions/Side Effects

Central nervous system

  • abnormal thinking
  • behavior changes
  • dizziness
  • fatigue
  • hallucinations
  • headache
  • insomnia (worsened)
  • sleep—driving


  • nausea


  • ↑ prolactin levels
  • ↓ testosterone levels


  • angioedema (life-threatening)


Drug-Drug interaction

Blood levels and effects are ↑ by fluvoxamine ; concurrent use is contraindicated.Levels and effects may be ↓ by rifampin.Concurrent use of CYP3A4 inhibitors, such as ketoconazole, may ↑ levels and effects; use cautiously.Concurrent use of CYP2C9 inhibitors, such as fluconazole, may ↑ levels and effects; use cautiously.Donepezil and doxepin may ↑ levels.↑ risk of excessive CNS depression with other CNS depressants including alcohol, benzodiazepines, opioids, and other sedative/hypnotics.


Oral (Adults) 8 mg within 30 min of going to bed.

Availability (generic available)

Tablets: 8 mg

Nursing implications

Nursing assessment

  • Assess sleep patterns before and periodically throughout therapy.

Potential Nursing Diagnoses

Risk for injury (Side Effects)


  • Do not confuse Rozerem (ramelteon) with Razadyne (galantamine).
  • Do not administer with or immediately after a high-fat meal.
    • Before administering, reduce external stimuli and provide comfort measures to increase effectiveness of medication.
  • Oral: Administer 30 min prior to going to bed.

Patient/Family Teaching

  • Instruct patient to take ramelteon as directed, within 30 min of going to bed and to confine activities to those necessary to prepare for bed. Instruct patient to read the Medication Guide before starting and with each Rx refill; changes may occur.
  • Causes drowsiness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
  • Caution patient that complex sleep-related behaviors (sleep-driving, making phone calls, preparing and eating food, having sex, sleep walking) may occur while asleep. Inform patient to notify health care professional if sleep-related behaviors (may include sleep-driving—driving while not fully awake after ingestion of a sedative-hypnotic product, with no memory of the event) occur.
  • Advise patient to notify health care professional immediately if signs of anaphylaxis (swelling of the tongue or throat, trouble breathing, and nausea and vomiting) or angioedema (severe facial swelling) occur; may occur as early as the first time the product is taken.
  • Caution patient to avoid concurrent use of alcohol or other CNS depressants.
  • Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Relief of insomnia.


a sedative-hypnotic with antianxiety properties.
indication This drug is used to treat insomnia.
contraindications Alcohol intoxication, hepatic encephalopathy, lactation, and known hypersensitivity to this drug prohibit its use. This drug should not be administered to infants or children.
adverse effects Adverse effects of this drug include dizziness, somnolence, fatigue, headache, insomnia, depression, nausea, diarrhea, dysgeusia, vomiting, myalgia, arthralgia, decreased blood cortisol, influenza, and upper respiratory infection.
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References in periodicals archive ?
Virtually nothing is known about ramelteon in the context of anxiety, and the lack of familiarity with this novel drug makes it more difficult to reassure a patient who is anxious about adverse effects than it would be if a BzRA were used, she said.
Many drugs are commonly used off-label for insomnia, but the benzodiazepine receptor agonists and the newly approved melatonin receptor agonist ramelteon (Rozerem) are the only medications with Food and Drug Administration approval for this indication.
The recently approved ramelteon is a highly selective agonist for the melatonin ML-1 receptor, which is believed to play a more important role in sleep than the ML-2 receptor.
Prescribe the selective melatonin receptor agonist ramelteon, 8 mg/d
In addition, although numerous drugs are commonly prescribed off-label for insomnia, the benzodiazepine receptor agonists and the newly approved melatonin receptor agonist ramelteon (Rozerem) are the only medications with Food and Drug Administration approval for this indication.
The NIH statement was drafted prior to FDA approval of the melatonin receptor agonist ramelteon.
DENVER -- The novel melatonin receptor agonist ramelteon was associated with significant reductions in the time it took to fall asleep in two phase III clinical trials totaling 1,234 adults with primary insomnia, investigators reported at the annual meeting of the Associated Professional Sleep Societies.
explained that ramelteon differs from the endogenous hormone melatonin in that ramelteon is highly specific for the melatonin receptors MT1 and MT2 involved in the sleep-wake cycle; indeed, ramelteon has up to a 16-fold greater affinity for those sites than melatonin itself.
In two studies of patients with chronic insomnia--one in people aged 18-64 and another in those aged 65 and older--those taking ramelteon fell asleep faster and slept longer than those on placebo.
Ramelteon is a nonsedating selective melatonin receptor agonist approved for treating insomnia characterized by sleep onset difficulty.
The newly approved drug ramelteon significantly reduced sleep latency and increased total sleep time in a phase III study of elderly patients with chronic insomnia.