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Lunesta (Zopiclone)

Lunesta (eszopiclone formerly referred to as Estorra) is a nonbenzodiazepine hypnotic agent approved for the long term treatment of insomnia and sleep maintenance.
 
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General Information

Lunesta

Eszopiclone, also known as Estorra, is a nonbenzodiazepine hypnotic medication that has been licenced for the long-term treatment of insomnia and sleep maintenance.

Lunesta is used to treat individuals who have trouble getting asleep as well as those who have trouble staying asleep all night long (sleep maintenance difficulties).

The Federal Register classified ezopiclone as a Schedule IV restricted drug in April 2005. It shouldn’t be taken by pregnant women, those with known psychiatric conditions, or anyone who are using other prescription or over-the-counter sleep aids concurrently without a doctor’s supervision. Patients taking eszopiclone or any other hypnotic medication run the risk of developing dependent and going through withdrawal upon stopping use.

The medicine comes in tablets with strengths of 1 mg, 2 mg, and 3 mg. Most non-elderly adults should start taking Lunesta at a dose of 2 mg right before bed. If clinically necessary, the dose can be increased to 3 mg because it is more effective at promoting sleep maintenance at this level.

Use 1 mg right before night for elderly people whose main complaint is trouble falling asleep. If clinically necessary, the dose for these patients may be increased to 2 mg. The recommended dose is 2 mg right before bedtime for older people whose main complaint is trouble sleeping.

Clinical Results

The outcomes of six research trials involving 2100 people with both chronic and sporadic insomnia served as the foundation for the FDA’s approval of Lunesta. Based on the results of a six-month, double-blind, placebo-controlled experiment with 788 participants, the FDA decided to approve Lunesta for the long-term treatment of insomnia. A total of 24 clinical trials were represented in the Lunesta NDA.

Transient Insomnia

  • In a double-blind, parallel-group, single-night trial 436 healthy adults were evaluated in a model of transient insomnia sleep laboratory in a comparing two doses of eszopiclone and placebo. Results showed that Lunesta 3 mg was superior to placebo on measures of sleep latency and sleep maintenance, including polysomnographic (PSG) parameters of latency to persistent sleep (LPS) and WASO.

Chronic Insomnia

The treatment of chronic insomnia was established in five controlled studies. Three controlled studies were in adult subjects, and two controlled studies were in elderly subjects with chronic insomnia.

  • In the first study, 308 adults were evaluated in a double-blind, parallel-group trial of 6 weeks? duration comparing Lunesta 2 mg and 3 mg with placebo. Objective endpoints were measured for 4 weeks. Clinical results showed that both 2 mg and 3 mg were superior to placebo on LPS at 4 weeks. In addition, data showed that the 3 mg dose was superior to placebo on WASO.
  • In the second study, 788 adults were evaluated using subjective measures in a double-blind, parallel-group trial comparing the safety and efficacy of Lunesta 3 mg with placebo administered nightly for 6 months. Clinical results showed that Lunesta was superior to placebo on subjective measures of sleep latency, total sleep time, and WASO.
  • A 6-period cross-over PSG study evaluated eszopiclone doses of 1 to 3 mg, each given over a 2-day period, demonstrated effectiveness of all doses on LPS, and of 3 mg on WASO. A dose-related response was observed in the study.

Elderly

  • Elderly subjects (ages 65-86) with chronic insomnia were evaluated in two double-blind, parallel-group trials of 2 weeks? duration. One study (n=231) compared the effects of Lunesta with placebo on subjective outcome measures, and the other (n=292) on objective and subjective outcome measures. The first study compared 1 mg and 2 mg of Lunesta with placebo, while the second study compared 2 mg of Lunesta with placebo. Results showed that all doses were superior to placebo on measures of sleep latency. In both studies, 2 mg of Lunesta was superior to placebo on measures of sleep maintenance.

Side Effects

  • Adverse events associated with the use of Lunesta may include (but are not limited to) the following:

    • Drowsiness
    • Viral Infection
    • Dry Mouth
    • Dizziness
    • Hallucinations
    • Infection
    • Rash
    • Unpleasant Taste

Mechanism Of Action

Lunesta is a nonbenzodiazepine hypnotic agent that is a pyrrolopyrazine derivative of the cyclopyrrolone class. It is the S-isomer of the marketed non-benzodiazepine rapid-acting hypnotic zopiclone. Lunesta raises levels of an amino acid called Gamma-Aminobutyric Acid (GABA). GABA slows down brain activity so that your mind and body can relax, enabling you to fall asleep and stay sleep.

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