ramelteon ROZEREM

Class: Selective Melatonin Receptor Agonist
FDA Indications: Sleep Onset Insomnia
Off-Label Use: Circadian Rhythm Sleep Disorders, Bipolar Disorder, Sleep Disturbances In Dementia, Lewy Body Dementia, Visual Hallucinations In Dementia With Lewy Bodies, Refractory Behavioral And Psychological Symptoms Of Dementia In Alzheimer Disease, Delirium
Prescribing
Forms: 8mg tablet
Dose Range: 8 mg/day
Starting: 8 mg QHS for most patients. Be aware that t½ is ↑'d by 45 min when given with food.
Stopping: No discontinuation symptoms ∴ should be able to discontinue w/o tapering.

NAMI drug fact sheet

Precautions
Contraindications: None, other than patients with known hypersensitivity to ramelteon
Serious Side Effects: ↑ serum prolactin in women by ~34%; can also ↓ testosterone
Side Effects: headache, sedation/somnolence, dizziness
Pharmacodynamics
1° MOA: MT1/MT2 agonist
Target: MT1, MT2
Pharmacokinetics
t½: 2 (1-2.6)° TMAX: 0.5-1.5°
Substrate of: 1A2; 2C9, 3A4
Inhibits: ∅ ; Induces:
Active Metabolites: M-II — has a 2-5° t½ but only ~10% as potent as ramelteon; M-I, M-III & M-IV are also active
DDIs
Misc
  • - not a CNS depressant, rather its melatonergic MOA enhances effect of endogenous melotonin
  • - 17x more potent at MT1/MT2 than melatonin AND has a much longer t½ (2-5° vs ~30 minutes)
  • - promotes sleep by regulating the sleep/wake cycle rather than via CNS-depression
  • - lacks strong sleep-onset induction that the benzos and nonbenzos confer
  • - no tolerance or abuse potential
  • - unusual lack of a dose-response curve
  • - ∅ next-day residual effects, i.e. no "hangover"
  • - did not get the sleep maintenance indication because it couldn't demonstrate ↓ WASO
  • - avoid in children & adolescents – reproductive development can be affected because of its impact on the endocrine system
Special Populations

Category C—There are no adequate well-controlled studies in pregnant women

It is not known whether ramelteon is secreted into human milk

No dosage adjustment necessary


No dosage adjustment necessary


With 4 active metabolites, even mild impairment can ↑ levels 4-fold

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Last updated April 20 2018 09:28:33. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.