Ramelteon

Ramelteon is a prescription medication used to help adults fall asleep. It acts like melatonin, which is produced in the brain to control the sleep-wake cycle. The Food and Drug Administration (FDA) approved ramelteon on July 22, 2005, and it became the first drug of its kind.

Other Names

Takeda Pharmaceuticals markets ramelteon under the name Rozerem.

Uses

Ramelteon is used to treat adults with insomnia. It is used to help people fall asleep and can be used long-term.

How Ramelteon Is Taken

Ramelteon is available in 8 mg tablets. It is taken 30 minutes before bedtime. The action of ramelteon may be delayed if it is taken with a high-fat meal. Taking the dose on an empty stomach or 30 minutes after a meal helps to avoid this problem.

How Ramelteon Works

Melatonin is a chemical that helps control the sleep-wake cycle. It is released in the brain in response to darkness and promotes sleep. The action of melatonin is mediated by melatonin receptors located in specific brain regions. Ramelteon induces sleep by activating these melatonin receptors.

How the Body Affects Ramelteon

Enzymes in the liver metabolize, or chemically-alter, ramelteon. This process helps the body excrete the drug. The amount of time needed for the concentration of ramelteon in the blood to be reduced by half, the half-life, is approximately 1–3 hours. Most of a dose of ramelteon is excreted in the urine. High-fat meals increase the absorption of ramelteon into the body, but they also increase the time to reach maximum concentrations of the drug in the body. Ramelteon should not be taken with meals because of this delay.

The concentration of Ramelteon in the elderly is much higher than that seen in younger adults. To date however, this has not translated into an increased risk of developing side effects.

Side Effects

Below are some common side effects associated with the use of ramelteon:

• headache
• daytime sleepiness
• dizziness
• tiredness
• nausea
• worsening insomnia
• colds

Benefits

Ramelteon, unlike many other sleep medications, is not a controlled substance. It activates melatonin receptors, which means that development of addiction and withdrawal symptoms is unlikely. The use of many other sleep aid medicines is associated with addictive behaviors and withdrawal symptoms. But the action of these drugs is different than that of ramelteon.

The chemical that ramelteon acts like, melatonin, is also available as a sleep aid without a prescription and at a lower cost. Whether ramelteon is more effective than melatonin is not known. However, ramelteon may have an advantage over melatonin because its dose and purity are standardized by the FDA.

Risks and Precautions

Ramelteon is normally not used in people with the following conditions:

• an allergy to ramelteon or to any of the ingredients in Rozerem
• severe liver disease
• breathing problems when sleeping (sleep apnea)
• severe chronic obstructive pulmonary disorder, which is a lung disease that hinders breathing

Because of the risk of an interaction, ramelteon is normally not taken with fluvoxamine (Luvox).

People with psychological problems, or whose insomnia is caused by an underlying medical condition, may experience worsening of insomnia, mental, or behavior changes. These symptoms are not normal and may necessitate changing medications or discontinuing ramelteon.

Ramelteon may cause excessive drowsiness and interfere with driving or other activities. It is best taken before going to bed and after daily activities are complete.

Melatonin helps regulate the levels of some hormones in the body. Accordingly, ramelteon may increase prolactin and decrease testosterone levels. The consequences of these changes include the following:

• missed monthly periods
• nipple drainage
• decreased sex drive
• problems getting pregnant

Doctors can monitor levels of prolactin and testosterone with simple blood tests.

Drug Interactions

Ramelteon has the potential to interact with many medications because it is metabolized by enzymes in the liver. Other drugs that either inhibit or increase the activity of these enzymes could influence the effectiveness or safety of ramelteon. A list of drugs that could interact with ramelteon is below:

• fluvoxamine
• rifampin (Rifadin)
• ketoconazole (Nizoral)
• fluconazole (Diflucan)

Melatonin supplements may increase the risk of side effects because they have a similar mechanism of action as ramelteon. Similarly, alcohol could increase the risk of side effects because it causes drowsiness.

Alternatives

Many other medications are available to treat insomnia:

• zolpidem(Ambien)
• eszopiclone (Lunesta)
• temazepam (Restoril)
• zaleplon (Sonata)
• triazolam (Halcion)
• flurazepam (Dalmane)

None of these medications work like ramelteon.

Clinical Trials

The effectiveness of ramelteon was determined in 405 adults with chronic insomnia.^[1] The average time to fall asleep was 32 minutes and 48 minutes in patients treated with ramelteon (8 mg) and placebo, respectively. Ramelteon improved sleep for over five weeks, and did not significantly effect daily activities.

References

1. ↑ Zammit G, Erman M, Wang-Weigand S, Sainati S, Zhang J, Roth T. Evaluation of the efficacy and safety of ramelteon in subjects with chronic insomnia. J Clin Sleep Med. 2007 Aug 15;3(5):495-504. Abstract | Full Text

External Links

Rozerem Website