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Eszopiclone

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Summary

Summary

Lunesta, also known as eszopiclone, was approved by the FDA in December, 2004, for the short-term treatment of insomnia [1].

Moreover, Lunesta is indicated for use in patients suffering from insomnia, above the age of 18 [1].

Figure 1. Lunesta, also known as eszopiclone, is a non-benzodiazepine hypnotic agent, with a molecular weight of 388.81.

 

lunesta chemical structure

Detailed

Mechanism

The mechanism of action of Lunesta can be related to its effects on the GABA receptors [2].

Lunesta lasts around 6-8 hours in the body [1].

Lunesta is metabolised mainly in the liver by two mechanisms: oxidation and de-methylation [1].

Pharmacokinetics

Once taken, Lunesta (eszopiclone) is rapidly absorbed from the gastrointestinal (GI) tract within one hour [3].

Peak plasma concentrations of Lunesta are reached after around 1 hour of oral administration, and is binds weakly to plasma protein [4].

Lunesta & Anxiety

Lunesta (eszopiclone) has been previously investigated to determine its effects on treating insomnia comorbid with generalised anxiety disorder (GAD) [7].

Patients, aged 18-64, who fulfilled the criteria for anxiety, were administered eszopiclone and escitalopram (which is also an anti-anxiety drug).

Results of this work showed an improvement in total Hamilton Anxiety Scale scores, over 10 weeks [7].

Overall, researchers found improvements in not only sleep and daytime functioning, but also anxiety and mood in patients [7].

Dosage

Dosage

Dosing with Lunesta should be done with your health professional.

As a guide, starting dose of Lunesta is between 1-2mg at bedtime [2].

Other sources recommend an initial dose of 1mg immediately before bedtime, and, for elderly individuals, Lunesta dose should not exceed 2mg [4].

Lunesta tablets are available in 1mg, 2mg and 3mg doses. Importantly, TOTAL dose of Lunesta should not exceed 3mg, once daily [4].

It is important to note that each Lunesta tablet contains 1mg, 2mg or 3mg eszopiclone (depending on the dose), with other inactive ingredients included in each tablet [4].

Safety

Drug Interactions

Lunesta may interact with other compounds, such as olanzapine which is a drug used to treat schizophrenia, depression and bipolar disorder [5].

Alcohol is another drug that can cause drug-drug interactions with Lunesta [3]. Other interactions may occur with central nervous system (CNS) depressants, and rifampicin, which is an antibiotic [6].

Side Effects  

Side effects of Lunesta can include any one, or more of the following:

  • Dizziness
  • Dry mouth
  • Difficulty maintaining coordination [8].

In most patients, Lunesta leaves a bitter taste in the mouth [3].

Serious side effects, such as hallucinations, memory loss, along with changes in mood, should be reported to your doctor immediately [8].

Lunesta Withdrawal

Withdrawal from Lunesta can occur as a result of mental and physical dependency on Lunesta [9]. Withdrawal symptoms can occur within 12 hours of discontinuing Lunesta, and so it is highly advisable to consult your doctor before quitting [9].

Most people experiencing Lunesta withdrawal will note difficulties in sleep after quitting the drug. Common withdrawal symptoms can include:

  • Anxiety
  • Irritability
  • Tremors
  • Mood swings
  • Panic attacks [9].

Important Information

  • Avoid taking more Lunesta than already prescribed.
  • Do not take Lunesta unless you can maintain a 7-8 hour sleep cycle.
  • Administer Lunesta immediately before going to bed.
  • Contact your GP, or doctor, if insomnia has not improved within 7-10 days [10].
References

References

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1325284/

2. https://www.aafp.org/afp/2005/0615/p2359.html

3. https://www.mdedge.com/psychiatry/article/66112/eszopiclone-targeting-chronic-insomnia

4. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021476s030lbl.pdf

5. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC518985/

6. https://www.drugbank.ca/drugs/DB01045

7. https://www.ncbi.nlm.nih.gov/pubmed/18458207

8. https://www.webmd.com/drugs/2/drug-92350/lunesta-oral/details

9. https://www.addictioncenter.com/sleeping-pills/lunesta/withdrawal-detox/

10. https://www.lunesta.com/PostedApprovedLabelingText.pdf

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