ramelteon ROZEREM

Class: Selective Melatonin Receptor Agonist
FDA Indications: Sleep Onset Insomnia
Off-Label Use: Circadian Rhythm Sleep Disorders
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 January 20 2018 15:32:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.