Ramelteon (brand name Rozerem® and generic) is a melatonin receptor agonist that is used as a hypnotic.
On this page, we will provide basic information about this medication. Links to other articles on this website with more advanced information and tips related to this medication and related topics are provided below—under the Related Pages section below.
FDA-approved indications
Treatment of insomnia characterized by difficulty with sleep onset.
Mechanism of Action or Pharmacodynamics
Ramelteon is a melatonin receptor agonist.
Compared to melatonin, ramelteon has (Miyamoto, 2009):
– Six times more affinity for melatonin receptors 1 (MT1), and
– Three times more affinity for melatonin receptors 2 (MT2).
Contraindications
1. Do not use with fluvoxamine.
Why not? Fluvoxamine is a strong inhibitor of the enzyme CYP1A2, When fluvoxamine and ramelteon were given together, the “area under the curve” (AUC) for ramelteon increased about 190-fold! And the Cmax increased about 70-fold.
2. Serious allergic reaction (for example, angioedema) to ramelteon
Warnings and Precautions
Patients should be advised not to consume alcohol in combination with ramelteon tablets.
Potential side effects
Please see THIS PAGE for a handout listing both the common and less common side effects of this medication, along with the percentages of patients who report them.
Potential drug interactions
1. Ramelteon should not be used along with fluvoxamine.
2. Caution is needed if ramelteon is used along with other medications that inhibit the enzyme cytochrome P4501A2
Use in special populations
Moderate hepatic impairment: Use ramelteon with caution
Severe hepatic impairment: Use of ramelteon is “not recommended”
Dosage and Administration
Adults: Rameleteon (8 mg) One tablet at bedtime Instructions 1. Do NOT take ramelteon with or after a high-fat meal 2. After taking ramelteon, make sure you get into bed within 30 minutes or less 3. Do not exceed the recommended dose of 8 mg per day
Dosage forms and strengths
Tablets: 8 mg
Important! This page does not provide all the information needed to prescribe this medication. Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Related Pages
Practical tips on using hypnotics: the Z drugs
Practical tips on using hypnotics: benzodiazepines
Relaxation Practice: A Simple and Powerful Tool for Anxiety, Tension, and Insomnia
Three important pieces of information about benzodiazepines
Sleep Hygiene worksheets-Part 1 and Part 2
Sleep log: Ten important questions about the person’s sleep
References
Ramelteon (Rozerem®) Prescribing Information
Miyamoto M. Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. Review. PubMed PMID: 19228178; PubMed Central PMCID: PMC2871175.
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