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Zopiclone: A Comprehensive Review of its Development and Use in Treating Insomnia

Insomnia is a common sleep disorder that affects millions of people worldwide. Among the most commonly prescribed medicines to treat insomnia are benzodiazepines and Z-drugs, including zopiclone. Zopiclone has been in use for over three decades and has been proven effective in treating insomnia. This article provides a comprehensive review of the development and use of zopiclone in treating insomnia.


What is Insomnia?

Insomnia is a sleep disorder that affects a person's ability to fall asleep or stay asleep. It is a condition of overactive brain activity during sleep, and studies have shown that areas of the brain associated with wakefulness remain more active during sleep in patients with insomnia. Insomnia impacts approximately 25 million American adults and is associated with numerous serious health conditions, such as psychiatric disorders, cardiovascular disease, type 2 diabetes, substance abuse, and dementia.

Overview of Zopiclone

Zopiclone is a non-benzodiazepine hypnotic agent that belongs to the class of drugs known as cyclopyrrolones. It was first introduced in Europe in the 1980s and is now available in many countries worldwide. Zopiclone acts by enhancing the effects of the neurotransmitter gamma-aminobutyric acid (GABA), which slows down the activity of the brain and helps the user fall asleep faster.

Development of Zopiclone

The development of zopiclone began in the late 1970s, with the aim of creating a safer alternative to benzodiazepines for the treatment of insomnia. The first clinical trials of zopiclone were conducted in the early 1980s, and the drug was approved for use in Europe in 1986. Since then, it has been approved for use in many other countries, including Canada, Australia, and New Zealand.

How Zopiclone Works

Zopiclone works by enhancing the effects of the neurotransmitter GABA. GABA is a neurotransmitter that slows down the activity of the brain and helps the user fall asleep faster. Zopiclone binds to the GABA receptor and enhances its effects, leading to a reduction in brain activity and an increase in sleep time.

Advantages of Zopiclone

Zopiclone has several advantages over benzodiazepines in the treatment of insomnia. It has a shorter half-life than benzodiazepines, which means that it is eliminated from the body more quickly and is less likely to cause daytime drowsiness. It also has a lower risk of dependence and withdrawal symptoms than benzodiazepines.

Side Effects of Zopiclone

Like all medicines, zopiclone can cause side effects. The most common side effects of zopiclone include drowsiness, dizziness, and headache. Other side effects may include dry mouth, nausea, and changes in appetite. In rare cases, zopiclone may cause allergic reactions, including rash, hives, and swelling of the face, tongue, and throat.

Precautions When Using Zopiclone

Zopiclone should only be used for short-term treatment of insomnia. It should not be used for longer than four weeks, as long-term use may lead to dependence and withdrawal symptoms. Zopiclone should also be used with caution in patients with a history of drug or alcohol abuse, as they may be at increased risk of dependence.

Conclusion

Zopiclone is an effective and safe treatment for insomnia when used properly. It has several advantages over benzodiazepines, including a shorter half-life and a lower risk of dependence and withdrawal symptoms. However, it should only be used for short-term treatment of insomnia and with caution in patients with a history of drug or alcohol abuse. If you are experiencing insomnia, talk to your healthcare provider about whether zopiclone is right for you.

References:

  1. Bertisch, S. M., Herzig, S. J., Winkelman, J. W., & Buettner, C. (2014). National use of prescription medications for insomnia: NHANES 1999-2010. Sleep, 37(2), 343-349.

  2. Sateia, M. J., Buysse, D., Krystal, A. D., Neubauer, D. N., & Heald, J. L. (2017). 0395 clinical practice guideline for the pharmacologic treatment of chronic insomnia in adults: An American Academy of Sleep Medicine Clinical Practice guideline. Sleep, 40(suppl_1).

  3. U.S. Department of Health and Human Services. (2023, March 8). Drug overdose death rates. National Institutes of Health. Retrieved March 15, 2023, from Drug Overdose Death Rates | National Institute on Drug Abuse (NIDA) (nih.gov)

4. Synapse: Global Drug Intelligence Database

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