Melatonin Receptor Agonists (Rozerem) for Falling Asleep

Rozerem (ramelteon) is a prescription insomnia medication that was approved by the FDA in July 2005 and began to be marketed to consumers in 2006.1 Rozerem has a unique mechanism of action - melatonin receptor agonist - that selectively targets specific receptors in the brain that are responsible for controlling the body's sleep-wake cycle. It works by mimicking melatonin, a naturally occurring hormone that is produced during the sleep period.

Rozerem may have an advantage over the other benzodiazepine and non-benzodiazepine classes for the following reasons:

  • It specifically targets brain structures responsible for the sleep-wake cycle.
  • It is the first prescription sleep medication that has shown no evidence of abuse, dependence, or withdrawal (as such it has not been designated as a controlled substance by the U.S. DEA).
  • Rozerem is approved by the FDA to be prescribed for long-term use in adults.1
  • Rozerem has been shown to be safe in older adults, as well as those with mild-to-moderate chronic obstructive pulmonary disease (COPD) and mild-to-moderate sleep apnea.

Some of the primary warnings, side-effects, and contraindications for the use of Rozerem include the following (there are many others but these are the most significant):1

  • It is not recommend for use in patient with severe COPD or sleep apnea
  • It should not be used in patients with severe hepatic impairment or sensitivity to the medication
  • It is not recommended to used in conjunction with alcohol consumption
  • More common side-effects (greater than 2% in the study groups compared to placebo) include daytime sleepiness, dizziness, and fatigue.
  • In primarily depressed patients, the medication may cause worsening of depression or suicidal ideation (this issue has not been directly studied with Rozerem but is seen with other sleeping medications)

Some of the issues that should be taken into account when using Rozerem for insomnia associated with chronic pain include the following:1

  • As with the other sleeping medications (aside from the antidepressants), the use of Rozerem has not been directly studied in a chronic pain patient population.
  • Rozerem has no analgesic (pain relieving) properties as has been shown with some of the antidepressants medications when used for sleep.
  • Most chronic pain patients have difficulty initiating and maintaining sleep. While Rozerem has been shown to improve sleep-onset, its effects on sleep-maintenance are unknown.

As with the other sleeping medications, Rozerem will not address any underlying medical problems causing the insomnia. It should be used in conjunction with other treatments that are focused on the primary medical problem (e.g. chronic pain).