Dosing and uses of Ramelteon (Rozerem)
Adult dosage forms and strengths
tablet
- 8mg
Insomnia
8 mg PO qHs
Administration
Take within 30 min of going to bed
Do not take with or immediately after high fat meaL
Pediatric dosage forms and strengths
Safety & efficacy not established
Ramelteon (Rozerem) adverse (side) effects
1-10%
Dizziness
Somnolence (similar to placebo)
Fatigue
Headache
Dysgeusia
Nausea
Frequency not defined
Depression
Worsening of insomnia
Hallucinations
Mania
Angioedema (rare )
Warnings
Contraindications
Hypersensitivity
Severe hepatic impairment
Concomitant fluvoxamine
Cautions
Moderate hepatic impairment
Concomitant CYP1A2 inhibitors
Potential for cognitive & behavioral changes
May impair ability to drive/perform hazardous tasks
Pregnancy and lactation
Pregnancy category: C
Lactation: no clinical studies, not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Ramelteon (Rozerem)
Absorption: 84%
Bioavailability: 1.8%
Protein Bound: 82%
Metabolism: extensive first-pass metabolism; mostly by hepatic CYP1A2
Excretion
Urine: 84%
Feces: 4%
Mechanism of action
Melatonin receptor agonist with high affinity for MT1 & MT2 receptors
