Rozerem [ramelteon]
updated on October 31, 2006
Rozerem [ramelteon]

Rozerem is chemically related to the natural hormone melatonin, which may help
regulate the body's sleep-wake cycle, and is thought to work by stimulating melatonin
receptors in the brain.

Rozerem is another option for people with the main form of insomnia. It is the first
prescription sleep aid not designated as a controlled substance, as researchers didnÂ’
t find dependence in the study. ROZEREM has a unique action mechanism because
ROZEREM selectively targets two receptors in the brain's suprachiasmatic nucleus
(SCN). The SCN is the body's "master clock" because it regulates 24-hour or
"circadian" rhythms, including the sleep-wake cycle.

HOW ROZEREM WORKS EXACTLY?

Ramelteon (TAK-375) showed very high affinity for human MT1 and MT2 receptors,
and chick forebrain melatonin receptors, making the affinities of ramelteon for these
receptors 3-16 times higher than those of melatonin.

The affinity of ramelteon for hamster brain MT3 binding sites was extremely weak
compared to melatonin's affinity for the MT3 binding site. In addition, ramelteon
showed no measurable affinity for a large number of ligand binding sites and no effect
on the activity of various enzymes. Ramelteon inhibited forskolin-stimulated cAMP
production in the CHO cells that express the human MT1 or MT2 receptors.

Taken together, these results indicate that ramelteon is a potent and highly selective
agonist of MT1/MT2 melatonin receptors.

HOW SAFE IS ROZEREM? What are the risks?
The major potential risks and side effects of Rozerem therapy include worsening of
insommia, mental, or behavior changes. Rozerem causes drowsiness, may affecting
your ability to drive or do other dangeroius activities. It may also affect your
reproductive hormones by increasing prolactin and decreasing testosterone levels,
leading to missed monthly periods, nipple drainage, decreased sex drive, or problems
getting pregnant.

WHAT ARE ITS SIDE EFFECTS FOR SHORT TERM USE?
Common side effects of Rozerem include headache, daytime sleepiness, dizziness,
tiredness, nausea, worsening insomnia and colds.

LONG-TERM USE?
Not sure. This drug is too new.

HOW BIG IS THE MARKET?
Almost a third of adults have trouble sleeping, and about 10 percent have symptoms
of daytime impairment that signal true insomnia.

SUMMARY
Takeda discovered ramelteon in 1996, and they filed the New Drug Application (NDA)
for ROZEREM in September 2004. The approval is based on a clinical research
program of 4,200 patients. In the study, ROZEREM has been shown to decrease the
time to sleep onset in controlled clinical trials with the wide range of patients including
older adults. Rozerem will be available in late September, 2005.

ALL RIGHTS RESERVED ZHION 2006
References
FDA approves Rozerem (ramelteon) for insomnia Medical Newstoday.com, 26 Jul 2005  
FDA approves new insomnia treatment, CNN.com, Monday, July 25, 2005
Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist. Neuropharmacology.
2005 Feb;48(2):301-10. Patient Information Sheet Ramelteon Tablets (marked as Rozerem) August 30, 2005
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