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

Frequently asked questions

About Rozerem

How does Rozerem promote sleep?

Rozerem is thought to promote sleep by acting on MT1 and MT2 receptors within the SCN.6 The SCN is the body's master clock.5 Rozerem selectively binds to MT1 and MT2 receptors located throughout the brain.2,6-8 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 subside.2,5,9,10 Binding to MT2 receptors in the SCN is thought to maintain the circadian rhythm underlying the normal sleep-wake cycle.2,5,9 Rozerem has been associated with decreased testosterone levels and increased prolactin levels.2

Rozerem promotes sleep, not sedation. Rozerem works with the body's sleep-wake cycle.6 Rozerem does not promote sleep by generalized CNS depression.2,5,6,9 Patients should avoid engaging in activities requiring complete mental alertness such as operating machinery or driving a motor vehicle after ingesting the drug.2

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.

Has Rozerem shown evidence of abuse potential in clinical studies?

No. Rozerem showed zero evidence of abuse potential at up to 20 times the recommended dose.2,3 Rozerem has no appreciable affinity for receptors often associated with abuse (eg, GABA, dopamine, opiate).2,6,15-17

What were the results of the 6-month sleep study?

In a randomized, double-blind, placebo-controlled, 6-month study, sleep latency was evaluated by PSG in adults (aged 18 to 79 years) with chronic insomnia on the first 2 consecutive nights of Week 1, the last 2 nights of Months 1, 3, 5, and 6, and on the first 2 nights of the 2-week, single-blind, placebo run-out.1

Rozerem is effective for long-term use, as demonstrated in a 6-month sleep study. The 6-month sleep study found that Rozerem significantly reduced sleep latency through 6 months. In adults and older patients with chronic insomnia, Rozerem reduced latency to persistent sleep (LPS) by 40 minutes (56%) from baseline at Month 6 compared with 30 minutes (43%) in patients receiving placebo.1,4 No rebound insomnia or withdrawal symptoms were observed following the abrupt discontinuation of treatment.1,2

In addition, sleep recordings showed significant reductions in time to fall asleep as early as Night 1. Sleep recordings showed that patients receiving Rozerem experienced a 39-minute (55%) reduction in LPS from baseline on Nights 1 and 2 compared with 23 minutes (33%) in patients receiving placebo.1,4

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 disorder.2

How does Rozerem address patients’ concerns about waking up "hungover” the next day?

Across several studies, no clinically relevant next-day residual effects were seen with respect to memory, mood and feelings, or alertness and concentration when compared to placebo.1,2

  • Patients should avoid engaging in hazardous activities that require concentration (such as operating a motor vehicle or heavy machinery) after taking Rozerem2
  • 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 behavior2
  • 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
Can Rozerem be used in older patients?

A total of 654 subjects in double-blind, placebo-controlled, efficacy trials who received Rozerem were at least 65 years of age; of these, 199 were 75 years of age or older. No overall differences in safety or efficacy were observed between elderly and younger adult subjects.2

A double-blind, randomized, placebo-controlled study in elderly subjects with insomnia (n=33) evaluated the effect of a single dose of Rozerem on balance, mobility, and memory functions after middle of the night awakening. There is no information on the effect of multiple dosing. Night time dosing of Rozerem 8 mg did not impair middle-of-the-night balance, mobility, or memory functions relative to placebo. The effects on night balance in the elderly cannot be definitively known from this study.2

Can Rozerem be used in patients with mild-to-severe COPD?

Studies showed that mean oxygen saturation (SaO2) did not worsen throughout the night in patients with moderate-to-severe COPD. In a study of 25 patients with moderate-to-severe COPD, no overall statistically significant difference in mean percent SaO2 was observed in patients receiving Rozerem 8 mg compared with placebo over the 8 hours postdose.21 Similarly, in a separate study of 26 patients with mild-to-moderate COPD, Rozerem 16 mg (twice the recommended dose) and placebo had similar effects on mean percent SaO2 over the 8 hours postdose.14 The percentage of the night that SaO2 was <90% was similar for Rozerem and placebo in patients with mild, moderate, and severe COPD.14,21 There is no available information on the respiratory effects of multiple doses of Rozerem in patients with COPD. The respiratory depressant effects in patients with COPD cannot be definitively known from this study.

Can Rozerem be used in patients for whom substance abuse is a concern?

Yes. Rozerem provides insomnia treatment with no evidence of potential abuse. In a study of adult subjects with histories of poly-drug abuse, Rozerem showed no significant difference in abuse liability or cognitive (memory)/psychomotor performance vs placebo at any dose tested (even at up to 20 times the recommended dose).3 By contrast, triazolam, used as a reference treatment, at the 2 highest doses showed significant differences compared with placebo, demonstrating a dose-dependent effect.3 Patients should be advised not to consume alcohol in combination with Rozerem, as alcohol and Rozerem may have additive effects when used in conjunction.

About the Rozerem HCP member program

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Once signed in, you can update your account at any time by visiting My account at the top of any page. Select “Request change to DEA number” and fill out and submit the support request. Your DEA number will be updated after verification.

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.