Rozerem (Ramelteon)

• Generic name: Ramelteon
• Brand name: Rozerem
• Class: Non-benzodiazepine hypnotic, Melatonin receptor agonist

Rozerem is specifically indicated for the treatment of chronic or transient (temporary) insomnia characterized by difficulty in falling asleep. It is suitable for long-term use.

Because ramelteon did not show evidence of abuse potential or dependence in clinical studies, Rozerem is the first and only non-scheduled hypnotic. It is a non-controlled substance by the U.S. DEA.

Rozerem Advantages

• Specifically targets brain structures responsible for the sleep-wake cycle.
• Non habit forming, no development of tolerance or rebound insomnia after discontinuing.
• No morning residual side effects. It does not cause significant deficits of alertness, short term learning and memory performance, and ability to concentrate on the day following treatment.
• May be used in older adults, as well as those with mild-to-moderate chronic obstructive pulmonary disease (COPD) and mild-to-moderate sleep apnea.
• Lack of abuse potential: Rozerem may be considered for sleep disturbances in persons with a history of alcohol or substance abuse.

Rozerem Disadvantages

• Because of its different mechanism of action, Rozerem is not helpful for someone who needs sleep immediately because it takes time for ramelteon to begin working.
• Probably won't be helpful for severe insomnia or insomnia associated with mood disorders.
• Not suitable for people with severe liver impairment and should be used with caution in those with mild or moderate liver disease.
• The most common side effects are somnolence, dizziness, fatigue, nausea, and insomnia.

How does Rozerem work?

Ramelteon is a melatonin MT1 and MT2 receptor agonist. It has a unique mechanism of action that selectively targets two receptors located in the brain's suprachiasmatic nucleus (SCN). The SCN is known as the body's "master clock" because it regulates 24-hour, or circadian, rhythms including the sleep-wake cycle. By binding selectively at these receptors, ramelteon mimics and enhances the action of melatonin, which maintains the circadian sleep rhythm through the inhibitory activity of MT1 and MT2 systems on excitatory wakefulness-promoting circuits in the suprachiasmic nucleus.

Ramelteon does not affect other systems, such as benzodiazepine receptors, dopamine receptors, and opiate receptors. It has no effect on the activity of various enzymes.

Chronic Insomnia

Rozerem is an effective hypnotic for chronic insomnia.

Ramelteon was investigated in a pair of randomized, double-blind studies designed to determine its efficacy for chronic insomnia via polysomnography. This first study enrolled adults ages 18-64, who received one of two doses of Ramelteon (8 mg or 16 mg) or placebo nightly before bed for 35 days. Sleep analysis via polysomnography was performed on days 1, 2 of weeks 1, 3 and 5.

The second study enrolled elderly patients age 65 and older in a three-period crossover study. Participants received one of two doses of Ramelteon (4 mg or 8 mg) or placebo in each study period, with polysomnography analysis performed for 2 consecutive nights in each period. In both studies, each dose of Rozerem produced significant reductions in average latency to persistent sleep onset, compared to placebo.

Transient Insomnia

Rozerem is an effective for transient insomnia.

A randomized, double-blind study investigated the efficacy of Rozerem in treating transient insomnia. The study enrolled healthy adults, who received ramelteon (8 mg or 16 mg) or placebo before a night of polysomnography analysis. The 8 mg dose significantly reduced mean latency to persistent sleep, vs. placebo.

Abuse Potential

Unlike many other hypnotics, clinical and animal trials of Rozerem did not revealed potential for physical dependence or abuse.