Indication: Rozerem is indicated for the treatment of insomnia characterized by difficulty with sleep onset.

Promotes sleep, not sedation

Rozerem has no appreciable affinity for GABAA receptors2,6

Depiction of GABAA receptors within brain

GABAA receptors are associated with sedation, amnesia, and muscle-relaxant and anxiolytic effects18-20

Rozerem does not promote sleep by generalized CNS depression2,5,6,9

  • Rozerem does not work through GABA interactions2,6
  • Patients should be advised not to consume alcohol in combination with Rozerem, as alcohol and Rozerem may have additive effects when used in conjunction2
  • Rozerem is not categorized as Schedule IV by the Drug Enforcement Administration (DEA)2,13
  • Hallucinations, as well as behavioral changes such as bizarre behavior, agitation, and mania, have been reported with Rozerem use. Amnesia, anxiety, and other neuropsychiatric symptoms may also occur unpredictably2

Rozerem promotes sleep by acting on the SCN2,6

Depiction of SCN within brain
  • The SCN is the body's master clock5
  • MT1 receptors in the SCN are associated with normal sleep induction. MT2 receptors in the SCN are associated with maintaining circadian rhythms5,9,10
  • MT1 and MT2 receptors are not exclusive to the SCN and are located throughout the brain.7 The activity of Rozerem at MT1 and MT2 receptors in the SCN is thought to promote sleep2,5-7,9,10

Rozerem works where normal sleep begins

  • Rozerem selectively binds to MT1 and MT2 receptors located throughout the brain2,6-8
  • Binding to MT1 receptors in the SCN is thought to attenuate the alerting signal from the SCN, which allows sleep load to dominate and wakefulness to subside2,5,9,10
  • Binding to MT2 receptors in the SCN is thought to maintain the circadian rhythm underlying the normal sleep-wake cycle2,5,9
  • Rozerem works with the body’s sleep-wake cycle through the melatonin receptor pathway to promote sleep2,6
  • Rozerem has been associated with decreased testosterone levels and increased prolactin levels. Patients may experience cessation of menses or galactorrhea in females, decreased libido, or fertility problems that are possibly associated with such hormone changes2

Rozerem is not a controlled substance and can be prescribed for long‑term use*

Zero evidence of abuse, dependence, or withdrawal

  • Rozerem showed no evidence of abuse potential at up to 20 times the recommended dose2,3
  • No rebound insomnia or withdrawal symptoms were observed following the abrupt discontinuation of treatment1,2,4
  • Rozerem has no appreciable affinity for receptors often associated with abuse (eg, GABA, dopamine, opiate)2,6,15-17
  • Failure of insomnia to remit after 7–10 days, worsening of insomnia, or the emergence of new cognitive or behavioral abnormalities should be medically evaluated, as this may be the result of an unrecognized underlying medical/psychiatric disorder2

*Sustained efficacy has been shown in a 6-month clinical study in adults and older patients.1

Rozerem is not a controlled substance. A clinical abuse liability study showed no differences indicative of abuse potential between Rozerem and placebo at doses up to 20 times the recommended dose (N=14). Insomnia studies up to 6 months showed no evidence of rebound insomnia or withdrawal symptoms with Rozerem compared to placebo (N=2533).2,3

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Important Safety Information for Rozerem (ramelteon)

  • In rare cases, severe anaphylactic and anaphylactoid reactions have occurred following use of Rozerem. Angioedema involving the tongue, glottis, or larynx has been reported. Some patients have had additional symptoms such as dyspnea, throat closing, or nausea and vomiting that suggest anaphylaxis. Reactions may require emergency treatment and may be fatal. Patients who develop such reactions should not be rechallenged.
  • Rozerem should not be used in patients with severe hepatic impairment or in combination with Luvox® (fluvoxamine).
  • Failure of insomnia to remit after 7–10 days, worsening of insomnia, or emergence of new cognitive or behavioral abnormalities should be medically evaluated, as this may be the result of an unrecognized underlying medical/psychiatric disorder.
  • In primarily depressed patients, worsening of depression, including suicidal ideation and completed suicides, can occur with hypnotics.
  • Hallucinations, as well as behavioral changes such as bizarre behavior, agitation, and mania, have been reported with Rozerem use. Amnesia, anxiety, and other neuropsychiatric symptoms may also occur unpredictably.
  • Complex behaviors such as “sleep-driving," making or eating food, talking on the phone, sleep-walking, or engaging in other activities while not fully awake, with amnesia for the event, may occur with use of hypnotics, including Rozerem. The use of alcohol with Rozerem may increase the risk of such behaviors. Discontinuation of Rozerem should be strongly considered for patients who report any complex sleep behavior.
  • Patients should avoid engaging in hazardous activities that require concentration (such as operating a motor vehicle or heavy machinery) after taking Rozerem.
  • Rozerem should be taken within 30 minutes before going to bed and activities confined to preparing for bed.
  • Patients should be advised not to consume alcohol in combination with Rozerem, as alcohol and Rozerem may have additive effects when used in conjunction.
  • Rozerem has been associated with decreased testosterone levels and increased prolactin levels. Patients may experience cessation of menses or galactorrhea in females, decreased libido, or fertility problems that are possibly associated with such hormone changes.
  • Rozerem has not been studied in patients with severe sleep apnea and is not recommended for use in this population.
  • Safety and effectiveness of Rozerem in pediatric patients have not been established.
  • Rozerem should not be taken with or immediately after a high-fat meal.
  • The most common adverse reactions (≥3% and more common than with placebo) are somnolence, dizziness, fatigue, nausea, and exacerbated insomnia.

Indication

Rozerem is indicated for the treatment of insomnia characterized by difficulty with sleep onset.


Please see Full Prescribing Information and Medication Guide for Rozerem.

Show references

  1. Mayer G, Wang-Weigand S, Roth-Schechter B, Lehmann R, Staner C, Partinen M. Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic, primary insomnia. Sleep. 2009;32:351-360.
  2. Rozerem package insert, Takeda Pharmaceuticals America, Inc.
  3. Johnson MW, Suess PE, Griffiths RR. Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects. Arch Gen Psychiatry. 2006;63:1149-1157.
  4. Data on file, Takeda Pharmaceuticals U.S.A., Inc.
  5. Dubocovich ML, Rivera-Bermúdez MA, Gerdin MJ, Masana MI. Molecular pharmacology, regulation and function of mammalian melatonin receptors. Front Biosci. 2003;8:d1093-d1108.
  6. Kato K, Hirai K, Nishiyama K, et al. Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology. 2005;48:301-310.
  7. Ekmekcioglu C. Melatonin receptors in humans: biological role and clinical relevance. Biomed Pharmacother. 2006;60:97-108.
  8. Dubocovich ML, Benloucif S, Masana MI. Melatonin receptors in the mammalian suprachiasmatic nucleus. Behav Brain Res. 1996;73:141-147.
  9. Liu C, Weaver DR, Jin X, et al. Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock. Neuron. 1997;19:91-102.
  10. Lavie P. Sleep-wake as a biological rhythm. Annu Rev Psychol. 2001;52:277-303.
  11. The American Geriatrics Society 2015 Beers Criteria Update Expert Panel. American Geriatrics Society 2015 updated Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2015;63:2227-2246.
  12. Roth T, Seiden D, Sainati S, et. Al. Effects of ramelteon on patient-reported sleep latency in older adults with chronic insomnia. Sleep Med. 2006;7:312-318.
  13. US Dept of Justice. Controlled Substances. Drug Enforcement Administration website. Available at:
    http://www.deadiversion.usdoj.gov/schedules/orangebook/orangebook.pdf. Accessed on September 22, 2016.
  14. Kryger M, Wang-Weigand S, Zhang J, Roth T. Effect of ramelteon, a selective MT(1)/MT(2)-receptor agonist, on respiration during sleep in mild to moderate COPD. Sleep Breath. 2008;12:243-250.
  15. Hummel M, Unterwald EM. D1 dopamine receptor: a putative neurochemical and behavioral link to cocaine action. J Cell Physiol. 2002;191:17-27.
  16. Malcolm RJ. GABA systems, benzodiazepines, and substance dependence. J Clin Psychiatry. 2003;64(suppl 3):36-40.
  17. Nestler EJ. Historical review: molecular and cellular mechanisms of opiate and cocaine addiction. Trends Pharmacol Sci. 2004;25:210-218.
  18. Rudolph U, Crestani F, Benke D, et al. Benzodiazepine actions mediated by specific g-aminobutyric acidA receptor subtypes. Nature. 1999;401:796-800.
  19. Rowlett JK, Platt DM, Lelas S, Atack JR, Dawson GR. Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates. Proc Natl Acad Sci U S A. 2005;102(suppl 3):915-920.
  20. Landolt HP, Gillin JC. GABAA1a receptors: involvement in sleep regulation and potential of selective agonists in the treatment of insomnia. CNS Drugs. 2000;13:185-199.
  21. Kryger M, Roth T, Wang-Weigand S, Zhang J. The effects of ramelteon on respiration during sleep in subjects with moderate to severe chronic obstructive pulmonary disease. Sleep Breath. 2009;13:79-84.

Important Safety Information for Rozerem (ramelteon)

Important Safety Information for Rozerem (ramelteon)

  • In rare cases, severe anaphylactic and anaphylactoid reactions have occurred following use of Rozerem. Angioedema involving the tongue, glottis, or larynx has been reported. Some patients have had additional symptoms such as dyspnea, throat closing, or nausea and vomiting that suggest anaphylaxis. Reactions may require emergency treatment and may be fatal. Patients who develop such reactions should not be rechallenged.
  • Rozerem should not be used in patients with severe hepatic impairment or in combination with Luvox® (fluvoxamine).
  • Failure of insomnia to remit after 7–10 days, worsening of insomnia, or emergence of new cognitive or behavioral abnormalities should be medically evaluated, as this may be the result of an unrecognized underlying medical/psychiatric disorder.
  • In primarily depressed patients, worsening of depression, including suicidal ideation and completed suicides, can occur with hypnotics.
  • Hallucinations, as well as behavioral changes such as bizarre behavior, agitation, and mania, have been reported with Rozerem use. Amnesia, anxiety, and other neuropsychiatric symptoms may also occur unpredictably.
  • Complex behaviors such as “sleep-driving," making or eating food, talking on the phone, sleep-walking, or engaging in other activities while not fully awake, with amnesia for the event, may occur with use of hypnotics, including Rozerem. The use of alcohol with Rozerem may increase the risk of such behaviors. Discontinuation of Rozerem should be strongly considered for patients who report any complex sleep behavior.
  • Patients should avoid engaging in hazardous activities that require concentration (such as operating a motor vehicle or heavy machinery) after taking Rozerem.
  • Rozerem should be taken within 30 minutes before going to bed and activities confined to preparing for bed.
  • Patients should be advised not to consume alcohol in combination with Rozerem, as alcohol and Rozerem may have additive effects when used in conjunction.
  • Rozerem has been associated with decreased testosterone levels and increased prolactin levels. Patients may experience cessation of menses or galactorrhea in females, decreased libido, or fertility problems that are possibly associated with such hormone changes.
  • Rozerem has not been studied in patients with severe sleep apnea and is not recommended for use in this population.
  • Safety and effectiveness of Rozerem in pediatric patients have not been established.
  • Rozerem should not be taken with or immediately after a high-fat meal.
  • The most common adverse reactions (≥3% and more common than with placebo) are somnolence, dizziness, fatigue, nausea, and exacerbated insomnia.

Indication

Rozerem is indicated for the treatment of insomnia characterized by difficulty with sleep onset.


Please see Full Prescribing Information and Medication Guide for Rozerem.