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By Medicover Hospitals / 27 Jan 2021
Home | Medicine | Ramelteon

What is Ramelteon?

  • Ramelteon, marketed among others under the brand name Rozerem, is a sleep agent medicine that binds exclusively to the suprachiasmatic nucleus of the MT1 and MT2 receptors instead of binding to GABAA receptors, such as with drugs such as zolpidem.
    1. Ramelteon Uses
    2. Ramelteon Side effects
    3. Precautions
    4. Overdose
    5. Ramelteon Storage
    6. Ramelteon vs Melatonin
    7. Frequently Asked Questions
    8. Citations

    Ramelteon Uses:

  • Ramelteon is used to help patients fall asleep more rapidly who have sleep-onset insomnia (difficulty falling asleep). Ramelteon is in a class of medicines called agonists of the melatonin receptor. Melatonin, a natural substance in the brain that is required for sleep, functions similarly.
  • How to take

    • As a tablet to take by mouth, Ramelteon comes. It is usually taken once a day, 30 minutes before bedtime at the latest. Do not take ramelteon with a meal or soon after. Carefully follow all the instructions given on the prescription label and ask your doctor or pharmacist to clarify any aspect that you do not understand or not clear. Just take Ramelteon as directed. Do take more or less of it more often than what is recommended by your physician.
    • Swallow whole tablets; do not divide, chew, or crush them.
    • Soon after you take Ramelteon, you can become sleepy. You should finish any required bedtime preparations and go to bed after you take ramelteon. For this time, don't schedule any other things.
    • If you are unable to stay asleep for 7 to 8 hours after taking the drug, do not use ramelteon
    • After you begin treatment with ramelteon, your insomnia should improve within 7 to 10 days. If your insomnia does not improve during this period or gets worse at some time during your care, call your doctor.
    • When you begin treatment with Ramelteon and each time you refill your prescription, your doctor or pharmacist will send you the manufacturer's patient information sheet (Medication Guide). Read the details carefully and, if you have any questions, ask your doctor or pharmacist.

    How does it work

  • Ramelteon is a melatonin receptor with both a high affinity for melatonin MT1 and MT2 receptors and very low selectivity for the MT3 receptor. The development of melatonin is simultaneous with nocturnal sleep, which means that a rise in melatonin levels is associated with the onset of self-reported sleepiness and an increase in the tendency to sleep. MT1 receptors are believed to be responsible for controlling sleepiness and promoting sleep onset, and the phase-shifting effects of melatonin on the circadian rhythm are believed to be mediated by MT2 receptors. Although the sleep-wake cycle is correlated with MT1 and MT2 receptors, MT3 has a totally different profile and is therefore not likely to be involved in the sleep-wake cycle. Ramelteon has no important affinity for neuropeptides, cytokines, serotonin, dopamine, norepinephrine, acetylcholine, or opiates that bind to the gamma-aminobutyric acid (GABA) receptor complex or receptors.
  • Dosage and administration:

  • Adult Dose For Adults
  • ROZEREM's prescribed dosage is 8 mg taken within 30 minutes of bedtime. It is best not to take ROZEREM with or directly after a high-fat meal
  • The dosage of ROZEREM in total does not exceed 8 mg daily.
  • Dosing In Patients With Hepatic Deficiency
  • In patients with serious liver disease, ROZEREM is not recommended. In patients with mild liver disease, ROZEREM should be used with caution.
  • Management Of Other Drugs
  • In conjunction with fluvoxamine, ROZEREM should not be used. In patients taking other CYP1A2 inhibiting medications, ROZEREM should be used with caution.
  • Ramelteon Side Effects:

    • Swelling of the tongue or throat
    • Difficulty swallowing or breathing
    • Feeling that the throat is closing
    • Nausea
    • Vomiting
    • Irregular or missed menstrual periods
    • Milky discharge from the nipples
    • Decreased sexual desire
    • Fertility problems
    • Drowsiness or tiredness
    • Dizziness


    • If you are allergic to Ramelteon, any other drugs, or any of the ingredients in Ramelteon tablets, notify your doctor and pharmacist. For a list of the ingredients, ask your pharmacist or consult the Drug Guide.
    • If you are taking fluvoxamine, tell your doctor if you have (Luvox). Your doctor may tell you not to take Ramelteon while you are taking this medication.
    • Tell your doctor whether you have ever thought or intended or attempted to kill yourself and whether you have or have ever had the chronic obstructive pulmonary disease (COPD, lung damage that makes it hard to breathe) or any other lung disease, sleep apnea (a condition in which you suddenly stop breathing several times during your period of time).
    • If you are pregnant, or expecting to become pregnant, or breast-feeding, tell your doctor. Give your doctor a call if you get pregnant while taking Ramelteon.
    • If you are pregnant, or expecting to become pregnant, or breast-feeding, tell your doctor. Give your doctor a call if you get pregnant while taking Ramelteon.
    • During your care with Ramelteon, do not drink alcohol. Alcohol can make Ramelteon's side effects worse.
    • Endocrine effects include reduced testosterone and increased levels of prolactin; unexplained effects on the reproductive axis in human development.
    • In patients with respiratory disability, including sleep apnea or COPD, use caution; not recommended in patients with serious sleep apnea
    • Caution should be used in patients with hepatic impairment; extreme hepatic impairment is not recommended.
    • Database analysis of drug interactions with substantial drug interactions.

    Missed Dose:

  • If you have forgotten to take any doses, take it as soon as you recall. If the time for the next dose has already come, skip the forgotten dose.
  • Overdose:

  • Do not overdose. If someone takes too much something serious can happen, immediately go to the doctor.
  • Storage:

  • Store it away from excess heat/direct heat and moisture at room temperature and (not in the bathroom). Throw the expired medicine.
  • Ramelteon vs Melatonin:

    Formula: C16H21NO2 Formula: C13H16N2O2
    Is a sleep agent medication Associated with control of the sleep-wake cycle.
    Ramelteon is used to help patients fall asleep more rapidly who have sleep-onset insomnia Used for the short-term treatment of insomnia
    Brand Name: Rozerem Brand Name: N-acetyl-5-methoxytryptamine

    Frequently Asked Questions:

    Ramelteon (Rozerem) is a type 1 and type 2 agonist of the highly selective melatonin receptor 1,2, unlike non-prescription melatonin, which is not selective for all three melatonin receptors.
    It acts by stimulating the brain's receptors for melatonin. Melatonin and its receptors regulate the body's circadian rhythm, which regulates the sleep/wake cycle. Ramelteon is not addictive, and it is not a controlled substance, unlike many drugs used for treating insomnia.
    Some common side effects are swelling of the tongue, difficulty in swallowing or breathing, feeling discomfort in the throat, Nausea, Vomiting, irregular or missed menstrual periods, milky discharge from the nipples, decreased sexual desire, fertility problems, drowsiness or tiredness, dizziness
    It may or may not cause you to weight gain, depends on your body
    In the elderly, nonbenzodiazepines are safer and better tolerated than tricyclic antidepressants, antihistamines, and benzodiazepines, such as zolpidem, eszopiclone, zaleplon, and ramelteon. Only after sleep hygiene is discussed, however, should pharmacotherapy be recommended.
    Even though GABA is not mediated by melatonin agonists, it is suggested that melatonin and ramelteon should not be mixed with alcohol. Alcohol may decrease the sleep effectiveness of melatonin and, when combined with ramelteon, may have additive CNS effects and increase the risk of sleep-related complex behaviors.


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